Why Does Fioricet Work for Headaches?

What causes headaches?

Doctors don’t fully understand what causes most headaches. They do know that the brain tissue and the skull are never responsible since they don’t have nerves that register pain. But the blood vessels in the head and neck can signal pain, as can the tissues that surround the brain and some major nerves that originate in the brain. The scalp, sinuses, teeth, and muscles and joints of the neck can also cause head pain.

When Fioricet enters the brain, it acts similarly to several other CNS depressants (e.g., alcohol, benzodiazepines) by enhancing the activity of a neurotransmitter called gamma-aminobutyric acid (GABA).  GABA inhibits or slows certain processes in the brain and creates a relaxed feeling.  For this reason, doctors frequently prescribe CNS depressants for their ability to promote sleep and reduce anxiety.

How Does Fioricet Work ?

  • Fioricet is a combination pain-reliever (analgesic) containing acetaminophen, butalbital, and caffeine.
  • Experts aren’t sure exactly how acetaminophen works, but suspect it blocks a specific type of cyclo-oxygenase (COX) enzyme, located mainly in the brain.
  • Butalbital belongs to the class of medicines called barbiturates. When used for pain due to tension headaches experts believe it works by relaxing muscle contractions and causing sedation via an enhancement of the inhibitory effects of GABA (a neurotransmitter that regulates communication between brain cells).
  • Caffeine is thought to enhance the pain-relieving effects of acetaminophen by up to 40%. In addition, it has vasoconstrictive properties, narrowing blood vessels in the brain thereby decreasing blood flow and oxygen tension (before a headache or a migraine, blood vessels tend to enlarge). This also helps to relieve pain.
  • Fioricet belongs to the class of medicines known as barbiturates because it contains butalbital. It may also be called a combination analgesic.

When to worry about a headache

You can take care of many types of headaches by yourself, and your doctor can give you medication to control most of the tougher headaches. But some headaches call for prompt medical care. Here are some warning signs for when you should worry about headaches:

  • Headaches that first develop after age 50
  • A major change in the pattern of your headaches
  • An unusually severe headache
  • Head pain that increases with coughing or movement
  • Headaches that get steadily worse
  • Changes in personality or mental function
  • Headaches that are accompanied by fever, stiff neck, confusion, decreased alertness or memory, or neurological symptoms such as visual disturbances, slurred speech, weakness, numbness, or seizures
  • Headaches that are accompanied by a painful red eye
  • Headaches that are accompanied by pain and tenderness near the temples
  • Headaches after a blow to the head
  • Headaches that prevent normal daily activities
  • Headaches that come on abruptly, especially if they wake you up
  • Headaches in patients with cancer or impaired immune systems

Types of headaches

There are more than 300 types of headaches, but only about 10% of headaches have a known cause. The others are called primary headaches. Here is a rundown on some major primary headaches.

Tension headaches

Occurring in about three of every four adults, tension headaches are the most common of all headaches. In most cases, they are mild to moderate in severity and occur infrequently. But a few people get severe tension headaches, and some are troubled by them for three or four times a week.

The typical tension headache produces a dull, squeezing pain on both sides of the head. People with strong tension headaches may feel like their head is in a vise. The shoulders and neck can also ache. Some tension headaches are triggered by fatigue, emotional stress, or problems involving the muscles or joints of the neck or jaw. Most last for 20 minutes to two hours.

If you get occasional tension-type headaches, you can take care of them yourself. Over-the-counter pain relievers such as acetaminophen (Tylenol, other brands) and nonsteroidal anti-inflammatories (NSAIDs) such as aspirin, naproxen (Aleve, other brands), or ibuprofen (Motrin, Advil, other brands) often do the trick, but follow the directions on the label, and never take more than you should. A heating pad or warm shower may help; some people feel better with a short nap or light snack.

If you get frequent tension-type headaches, try to identify triggers so you can avoid them. Don’t get overtired or skip meals. Learn relaxation techniques; yoga is particularly helpful because it can relax both your mind and your neck muscles. If you clench your jaw or grind your teeth at night, a bite plate may help.

If you need more help, your doctor may prescribe a stronger pain medication or a muscle relaxant to control headache pain. Many people with recurrent tension-type headaches can prevent attacks by taking a tricyclic antidepressant such as amitriptyline (Elavil, generic). Fortunately, most people with tension-type headaches will do very well with simpler programs.

Migraine

Migraines occur less often than tension headaches, but they are usually much more severe. They are two to three times more common in women than men, but that’s small consolation if you are among the 6% to 8% of all men who have migraines. And since a Harvard study of 20,084 men age 40 to 84 reported that having migraines boosts the risk of heart attacks by 42%, men with migraines should take their headaches to heart.

Neurologists believe that migraines are caused by changes in the brain’s blood flow and nerve cell activity. Genetics play a role since 70% of migraine victims have at least one close relative with the problem.

Migraine triggers. Although a migraine can come on without warning, it is often set off by a trigger. The things that set off a migraine vary from person to person, but a migraine sufferer usually remains sensitive to the same triggers. The table lists some of the most common ones.

Major migraine triggers

      • Changing weather: rising humidity, heat
      • Lack of sleep or oversleeping
      • Fatigue
      • Emotional stress
      • Sensory triggers: bright or flickering lights, loud noises, strong smells
      • Dietary triggers:
        • missing a meal
        • alcohol, especially red wine
        • chocolate
        • nitrates in cured meats and fish
        • aged cheese
        • an increase or decrease in caffeine
        • MSG (often present in Asian and prepared foods)

Migraine symptoms. Migraines often begin in the evening or during sleep. In some people, the attacks are preceded by several hours of fatigue, depression, and sluggishness or by irritability and restlessness. Because migraine symptoms vary widely, at least half of all migraine sufferers think they have sinus or tension headaches, not migraines.

About 20% of migraines begin with one or more neurological symptoms called an aura. Visual complaints are most common. They may include halos, sparkles or flashing lights, wavy lines, and even temporary loss of vision. The aura may also produce numbness or tingling on one side of the body, especially the face or hand. Some patients develop aura symptoms without getting headaches; they often think they are having a stroke, not a migraine.

The majority of migraines develop without an aura. In typical cases, the pain is on one side of the head, often beginning around the eye and temple before spreading to the back of the head. The pain is frequently severe and is described as throbbing or pulsating. Nausea is common, and many migraine patients have a watering eye, a running nose, or congestion. If these symptoms are prominent, they may lead to a misdiagnosis of sinus headaches.

Without effective treatment, migraine attacks usually last for four to 24 hours. When you’re suffering a migraine, even four hours is far too long — and that’s why early treatment for a migraine is so important.

Migraine treatment. If you spot a migraine in its very earliest stages, you may be able to control it with nonprescription pain relievers. Acetaminophen, aspirin, ibuprofen, naproxen, and a combination of pain medications and caffeine are all effective — if you take a full dose very early in the attack. The anti-nausea drug metoclopramide (Reglan) may enhance the activity of NSAIDs.

When prescription drugs are needed, most doctors turn to the triptans, which are available as tablets, nasal sprays, or as injections that patients can learn to give to themselves. Examples include sumatriptan (Imitrex), zolmitriptan (Zomig), and rizatriptan (Maxalt). Triptans provide complete relief within two hours for up to 70% of patients; the response is best if treatment is started early. Some patients require a second dose within 12 to 24 hours. Because the triptans can affect blood flow to the heart as well as the head, patients with cardiovascular disease should not use them. Patients who take antidepressants in the SSRI family should also avoid triptans.

Work with your doctor to find the migraine treatment that works best for you. Remember, though, that overuse can lead to rebound headaches and a vicious cycle of drugs and headaches. So, if you need treatment more than two or three times a week, consider preventive medications.

Migraine prevention. Some people can prevent migraines simply by avoiding triggers. Others do well with prompt therapy for occasional attacks. But patients who suffer frequent migraine attacks often benefit from preventive medications. Effective prescription drugs include beta blockers (such as propranolol, nadolol and atenolol), certain antidepressants (such as amitriptyline), and certain antiseizure medications (such topiramate and valproate). Difficult cases may benefit from referral to a headache specialist.

Fioricet is a medication that is being used more and more often for patients who are struggling with constant tension All kinds of Headache and migraines.

Since these types of All kinds of Headache have similar causes, they can easily be treated with the same type of medication. Before you start using this medication, though, you might be wondering exactly how and why it works on your body. Here’s some information on the main ingredients in Fioricet and what they do for your body.

Fioricet contains a combination of acetaminophen, butalbital, and caffeine. Acetaminophen is a pain reliever and fever reducer. Butalbital is in a group of drugs called barbiturates. It relaxes muscle contractions involved in a tension headache.

Caffeine is a central nervous system stimulant. It relaxes muscle contractions in blood vessels to improve blood flow.

fioricet Mechanism of action
fioricet Mechanism of action

Fioricet is used to treat tension headaches that are caused by muscle contractions.

Butalbital has generalized depressant effect on central nervous system and, in very high doses, has peripheral effects.

Butalbital Mechanism of Action
Butalbital Mechanism of Action

 

the mechanism of action of acetaminophen
the mechanism of action of acetaminophen

Acetaminophen has analgesic and antipyretic effects mediated by a metabolite which acts at cannabinoid receptors, contrary to popular belief it is not an anti-inflammatory at safe levels (it becomes toxic at doses above 1,000mg per dose and/or 3,000mg per day).

caffeine mechanism of action
caffeine mechanism of action

Caffeine is thought to produce constriction of cerebral blood vessels and serves to counteract the sedative effect of butalbital.

Butalbital has a half-life of about 35 hours. Acetaminophen has a half-life of about 1.25 to 3 hours, but may be increased by liver damage and after an overdose. Caffeine has a half-life of about 5 to 7 hours. Butalbital is a barbiturate that slows certain central nervous system (CNS) processes via its interaction with brain receptors for the inhibitory neurotransmitter GABA.

Acetaminophen is one of the main ingredients in this medication. It is a blood thinner that is often used as an over the counter pain reliever and fever reducer. Chances are likely that if you’ve struggled with All kinds of Headache for a while, you may have already tried taking acetaminophen under different brand names to reduce your pain. Chances are likely that it didn’t work for the worst of your All kinds of Headache. The reason that it works in Fioricet, though, is that it’s combined with two other ingredients: Butalbital and caffeine.

Butalbital is a barbiturate, a powerful medication used to relax the muscles and ease tension. This medication can make some people sleepy, so you should be careful about using Fioricet when you’re driving or operating heavy machinery. Many times tension All kinds of Headache and migraines are caused by the tension in neck and shoulder muscles. Since Butalbital helps ease this tension, it can get rid of one of the underlying causes for such All kinds of Headache.

Many people are surprised to learn that caffeine is a major active ingredient in Fioricet. This substance, though, actually can increase blood flow and help the nervous system function more smoothly. For this reason, it helps the body loosen up and can also ensure that the other two active ingredients are delivered to the proper spots in the body more quickly through the fast-flowing blood stream.

Before you purchase Fioricet from a pharmacy, you might want to check out the different options for ordering this effective headache and tension medication.

You can actually get better prices by purchasing it online. Plus, ordering them online is excellent because you can conveniently get your medications delivered right to your door. The discretion and ease involved in purchasing your pain relieving medication this way is unparalleled by what any regular pharmacy can offer. Before you decide to purchase your Fioricet, make sure you research other purchasing options that might save you time and money.

 

Buy White Fioricet Online

Fioricet is used to treat migraine and various forms of headache. Many doctors prescribe it to their patients because it is a sedative and a pain killer wrapped in one. When you have a prescription, you can buy Fioricet anywhere, but you should know that you should not exceed dosage prescribed by your doctor. However, if you have exceeded the dosage, you should call your doctor and tell him what side effects you are experiencing so he can help you out.

When you order Fioricet , you will get it in form of pills for oral usage of various shapes and colors. Usually it’s made in white or blue color, and the shape might be round or oval. Dosage is same for any of mentioned, 40mg, only shapes and colors are different.

    • Q: How do you ship orders?
    • A: We ship all orders by  USPS.

 

  • Q: Do you offer delivery on Saturdays?
  • A: Yes, The Express Mail option allows for delivery on Saturdays. Priority Mail does not. If it is Friday, and you want to see your order the next day, please select the Express Mail option.
  • Q: What is the difference between Priority Mail and Express Mail?
  • A: Express Mail is our fastest option; your order will normally be delivered within a day and will deliver on Saturday if needed. Priority Mail takes 2-3 days to deliver and does not deliver on Saturdays. Priority Mail and Express Mail for all orders within the 48 continental U.S. states.
  • Q: Do you ship Internationally?
  • A: Sorry we ship only within the U.S, we cannot ship Internationally at this time.

What you should know before you order fioricet online

Tell your doctor your medical history, especially of: serious liver disease, alcohol or narcotic dependence, emotional/mental conditions, heart disease (arrhythmias, recent MI), stomach/intestinal ulcers, any allergies. Acetaminophen may cause liver damage. Daily use of alcohol, especially when combined with acetaminophen, may increase your risk for liver damage.

Check with your doctor or pharmacist for more information. To prevent oversedation, avoid using alcohol and other sedative type medications while taking this. This drug may make you dizzy or drowsy; use caution engaging in activities requiring alertness such as driving or using machinery. Avoid alcoholic beverages.

This medication contains caffeine. Avoid drinking large amounts of caffeinated beverages while taking this medication as excessive nervousness and irritability can occur. This medication should be used during pregnancy only if clearly needed. Small amounts of this medication appear in breast milk. Consult your doctor before breast-feeding.

Doctors usually prescribe one pill of Fioricet to be taken on every four hours. You should not exceed six pills per day. You should not take Fioricet if you are using beta-blockers, because it can reduce or even negate their effect. At the start of treatment, you might feel drowsy, but the effects will disappear as time passes. You might encounter some side effects while on Fioricet treatment, including shaking / tremors, abdominal pain, vomiting, anxiousness and nausea. If you do encounter any of mentioned, you should contact your doctor so you can receive suitable replacement. If Fioricet is prescribed by doctor who knows your full medical history, side effects can be lowered to minimum or may never appear. Consequences of overdosing can be very serious, even fatal. You should not buy Fioricet if you are abusing alcohol or drugs.

There are many stores that offer Fioricet, but as we all know, you can get cheap Fioricet online very easily. Web stores usually have big discounts, and deliver the drug to your house, office or any other place you want it delivered to discreetly and quickly, which are the main reasons this drug has gotten so popular in such a short amount of time. Web stores tend to deliver your order as soon as possible, but it never takes more than one day. If you order Fioricet online today, it will be delivered either during the day or in the morning. When we think of advantages, it is fast, reliable, discreet, and you don’t even have to leave your house. All you have to do is place the order online and web store delivery will get your order sorted out. It is also important to mention that in some web stores you can buy fioricet overnight, so if you are using it for long time, there is no need to visit your doctor and ask him to prescribe it again.

Fioricet is a prescription drug which is used in treatment of headaches. It is actually a combination drug which combines three ingredients that work together and provide a relief of headache pain in tensions headaches, muscle contraction headaches and headaches that occur after post-dural puncture.

The first ingredient in Fioricet is butalbital. This is a barbiturate drug which is very rarely used alone but which has found its way into a number of combination drugs, including Fioricet. Since it is a barbiturate drug, it is a relatively potent analgesic, meaning that it provides relief from pain. It can also be dependency-forming, but in Fioricet it is not present in such large doses so as to cause dependency unless it is used improperly or for too long.

The second ingredient in Fioricet is acetaminophen, also known as paracetamol. It is one of the most basic and most common drugs in the world. It is also a painkiller which can be used to treat mild to moderate pain. On its own, it can be used in treatment of headaches and it is only logical that it was included in Fioricet. It can cause liver damage if it is used improperly and it is often included in medications to discourage overuse.

The third ingredient in Fioricet is a formulation of caffeine which is a common stimulant present in coffee and tea. It is used in Fioricet for two reasons. The first is that it can enhance the effects of the other two ingredients that provide the majority of analgesic effects and the second one is that it has been found to constrict blood vessels, especially in the brain. This can also provide substantial relief from pain that is associated with tension headaches.

Fioricet was developed specifically with headaches in mind. It has found other uses, however, although these uses are still considered off-label and investigational. For example, Fioricet is sometimes used in treatment of migraines and there are a lot of people for whom it has done wonders when their migraines are in question. Some people take Fioricet for back pain and other painful conditions. These are not common uses for this drug but we felt that we should mention them as well.

Fioricet is a relatively potent medication and it should be taken with utmost care. It is usually not the first line treatment for headaches due to its potency and the fact that it contains a barbiturate drug. It is used when less potent drugs have failed and/or when the pain is extremely severe.

Using Fioricet without your doctor recommending it is something that we would not advise and something that can be dangerous for some people. Also, using the drug improperly, for periods of time that are longer than recommended or in amounts larger than the recommended one can lead to adverse effects and serious dangerous effects on the health.

It should also be pointed out that the Fioricet formulation has changed. The old formulation included 50 mg of butalbital, 325 mg of acetaminophen and 40 mg a caffeine in the tablet. The new formulation is in form of capsules and it contains 50 mg of butalbital, 300 mg of acetaminophen and 40 mg of caffeine. As you can see, the amount of acetaminophen has been reduced due to new FDA guidelines concerning the limitation of acetaminophen amounts in combination drugs.

Fioricet is available online at various online pharmacies where you can order it and have them deliver the drug to your address. For many parts of the world, it is possible to have overnight delivery while there are parts where you will have to wait. The prices are lower online and when you find a reputable online pharmacy, you can safely and cheaply order Fioricet.

Fioricet DRUG INTERACTIONS:

Tell your doctor of all prescription and nonprescription drugs you may use, especially of: “blood thinners” Tell your doctor or pharmacist of all prescription and nonprescription drugs you may use that cause drowsiness such as: medicine for sleep (e.g., sedatives), tranquilizers, anti-anxiety drugs (e.g., diazepam), narcotic pain relievers (e.g., codeine), psychiatric medicines (e.g., phenothiazines such as chlorpromazine, or tricyclics such as amitriptyline), anti-seizure drugs (e.g., carbamazepine), muscle relaxants, antihistamines that cause drowsiness (e.g., diphenhydramine). Because this medication contains acetaminophen, check with your doctor or pharmacist before taking other medications containing acetaminophen which is commonly found in nonprescription pain relievers and cough-and-cold products. Read labels carefully to check ingredients. This drug may interfere with the effectiveness of birth control pills. Discuss using other methods of birth control with your doctor. Do not start or stop any medicine without doctor or pharmacist approval.

There are pharmacies that also participate in the affiliate programs. When you get Fioricet delivered overnight, you have the option of signing up for the affiliate program if you have your own website. The pharmacy will place banners and/or advertisements to their pharmacy. When someone clicks on your link to receive overnight fioricet no rx, you are credited on your account for the next time you want cheap fioricet next day delivery of your order. If you do your research, you will find the pharmacy that is just right for you.

If your choice in online pharmacies that offer those discounts to their customers does not have a secure and safe site, it will be of no use to you. Although most sites are safe that offer all of these different discounts, recheck them yourself. Make sure they have a secure encryption system in place so that when you send your credit card number and personal information across the Internet, no one receives it except the intended pharmacy. If that pharmacy has this type of security, they will display it very prominently on their site.

The site you choose should also have a very easy to navigate site. Many people looking to receive cheap Fioricet overnight are older and suffer from arthritis, diabetic neuropathy, fibromyalgia and chronic pain syndromes. They do not know how to use the computer like the younger generation. There is nothing worse than to get so aggravated with a site because they cannot navigate it that they move to another site.

Look for pharmacies that have 24/7 customer service representatives available, either by online chat, email that is answered within 24 hours or have telephone support. This is very important for that older generation when all they want to do is get Fioricet overnight cheap. A few kind words can alleviate any concerns that the customer may have.

Pharmacies that have overnight service use FedEx which delivers your discreet plain package that no one know what is in it except you. They do require that someone over the age of 18 must be present to sign for the order. This is for your benefit and the pharmacy to make sure you received your order.

Cheap Fioricet overnight is one of the best medications you can use for many painful conditions. It does not carry most of the side effects of narcotic pain relievers like Oxycontin, Hydrocodone and Vicodin. It is proving to rival those drugs because it mimics their effect on pain relieving signals that reach the brain.

What is Gabapentin ? What is your Experience with Gabapentin?

What is Gabapentin and What is Gabapentin Used for ?

Gabapentin is used with other medications to prevent and control seizures. It is also used to relieve nerve pain following shingles (a painful rash due to herpes zoster infection) in adults. Gabapentin is known as an anticonvulsant or antiepileptic drug.

OTHER USES: This section contains uses of this drug that are not listed in the approved professional labeling for the drug but that may be prescribed by your health care professional. Use this drug for a condition that is listed in this section only if it has been so prescribed by your health care professional.

Gabapentin may also be used to treat other nerve pain conditions (such as diabetic neuropathy, peripheral neuropathy, trigeminal neuralgia) and restless legs syndrome.

Gabapentin is an anti-epileptic medication, also called an anticonvulsant. It affects chemicals and nerves in the body that are involved in the cause of seizures and some types of pain.

Gabapentin is used in adults to treat nerve pain caused by herpes virus or shingles (herpes zoster).

The Horizant brand is also used to treat restless legs syndrome (RLS).

The Neurontin brand is also used to treat seizures in adults and children who are at least 3 years old.

Use only the brand and form of gabapentin that your doctor has prescribed. Check your medicine each time you get a refill at the pharmacy, to make sure you have received the correct form of this medication.

Gabapentin is also commonly prescribed for many off-label uses, such as treatment of restless leg syndrome, anxiety disorders, insomnia, and bipolar disorder. There are, however, concerns regarding the quality of the trials conducted and evidence for some such uses, especially in the case of its use as a mood stabilizer in bipolar disorder.

 

What is your Experience with Gabapentin?

This is a good question, in that it made me revisit this topic after a long time and gave me some new perspectives.

Firstly, some general comments:

  • FDA approval of any drug for any indication is always subject to updation
  • Non-approved usage of a medicine happens all the time; the only legal binding is that a company cannot promote/market an off-label use for a drug (this is my own conclusion, subject to correction)
  • FDA approval is not binding on countries other than the US

Now for some specific comments (I am quoting directly from this article: Gabapentin Therapy in Psychiatric Disorders: A Systematic Review, by Berlin, Butler, and Perloff (the points are so good, I didn’t bother editing or paraphrasing, except for some bolding and ellipsis)

  • Gabapentin was originally approved by the US Food and Drug Administration (FDA) for the treatment of partial seizures in 1993
  • Subsequent approval for postherpetic neuralgia in 2002
  • Within a decade of initial FDA approval, gabapentin’s second most common use became off-label prescription for psychiatric disorders (mainly for anxiety disorders)
  • Gabapentin’s use in psychiatric disorders has been shrouded in controversy, from the 1996 lawsuit against Warner-Lambert for promoting Neurontin for off-label indications, including psychiatric disorders
  • Gabapentin has a limited, generally well-tolerated side effect profile, and … has minimal drug-drug interactions
  • Gabapentin has … a proposed mechanism well-established for treating neuropathic pain and seizure
  • Numerous case reports and reviews suggest gabapentin’s potential efficacy as either monotherapy or adjunctive therapy in the treatment of bipolar disorder, depression, anxiety disorders, posttraumatic stress disorder (PTSD), alcohol dependence, and other types of drug abuse.

The authors then did a very thorough search for articles on studies, case reports or reviews looking into the (off-label) use of Gabapentin for various psychiatric conditions.

They conclude that:

  • Gabapentin does appear to provide benefit for some anxiety disorders, although randomized controlled trials have been limited to social phobia, anxiety in breast cancer, and perioperative anxiety.
  • To date, no studies exist for gabapentin efficacy in generalized anxiety disorder.
  • There is limited evidence to suggest the use of gabapentin in depression, PTSD, and OCD
  • Multiple studies suggest gabapentin has some efficacy in alcohol dependence, withdrawal, and craving.
  • As for gabapentin’s use in other types of substance dependence, there are no data to support its efficacy in cocaine or methamphetamine dependence.

Here is an application to the “21st meeting of the WHO Expert Committee on Selection and Use of Essential Medicines” for the inclusion of gabapentin on the WHO Model List of Essential Medicines, submitted by International Association for the Study of Pain (IASP), the Neuropathic Pain Special Interest Group (NeuPSIG) of the IASP, and the International Association of Hospice and Palliative Care (IAHPC), and supported by similar bodies in numerous other countries.

Here is the opening statement from this application:

We are applying for the inclusion of gabapentin as an analgesic agent for the management of neuropathic pain (central and peripheral) in adults. The medicine has regulatory approval for the treatment of several neuropathic pain states in adults by numerous stringent regulatory bodies (including the Food and Drug Administration [1] and European Medicines Agency [2]).

I am not aware of the outcome of this application (haven’t had the time to search for the relevant information).

To balance it all, here is a very good article (by Goodman & Brett): Gabapentin and Pregabalin for Pain — Is Increased Prescribing a Cause for Concern?

 taking a very critical look at all the off-label use of these medicines, the paucity of evidence, and the poor quality of research that exists in this particular area.

Finally, some personal comments from me:

  • Lack of evidence does not mean there is evidence of lack (of efficacy, for example)
  • Clinical Trials, including RCTs are good evidence, but still not absolute
  • Off-label use for any drug is between the doctor and the patient, with mutual understanding and informed consent
  • The use of Gabapentin as a sedative is neither well-studied, nor recommended.
  • Mild to moderate sedation is a common enough side-effect for patients and doctors to be tempted to use it that way; but if you have no other use for Gabapentin, then you are better off not taking it – there are many other better drugs for that.

Gabapentin is not Suitable for Children under 6 Years of Age

Gabapentin is not suitable for children under 6 years of age but, if it has been prescribed for a child who is older than this, check the label carefully to make sure you are giving the correct dose.

Gabapentin is FDA approved as an anti-convulsant for the treatment of Epilepsy and seizures resulting from other disorders. It is used to treat neuralgia and neuropathy, both of which are syptoms of many different diseases; such as, diabetic neuropathy or Shingles related neuralgia, among other disorders like fibromyalgia, as well as, physical trauma.

Dr.s also prescribe it for general anxiety and panic disorders, instead of more addicting benzodiazepines. and very recently it has been tried as a treatment for major depression and mood disorders.

It can help potentiate the efficacy of analgesic drugs, mostly opiate/opioid medications. It also helps mitigate the unpleasant side effects of withdrawal from opiates during titration and cessation of those drugs.  It can treat Restless Leg Syndrome (RLS).

It is not a controlled substance in the United States, and has a very low abuse potential, because it’s efficacy is dose dependent, with limited bioavailability and therefore, the higher the dose the less effective it is. It’s a gabapentinoid and it’s molecular structure is similar to that of GABA , making it a GABA analog, and it works by inhibiting Voltage-dependent Calcium channels (VDCC), it often is thought of as a GABA agonist, like benzodiazepines, but that is incorrect.

Take gabapentin exactly as prescribed by your doctor. Follow all directions on your prescription label. Do not take this medicine in larger or smaller amounts or for longer than recommended.

The Horizant brand of gabapentin should not be taken during the day.  For best results, take Horizant with food at about 5:00 in the evening.

Both Gralise and Horizant should be taken with food. Neurontin can be taken with or without food.

If you break a Neurontin tablet and take one half of it, take the other half at your next dose. Any tablet that has been broken should be used as soon as possible or within a few days.

Measure liquid medicine with a special dose-measuring spoon or medicine cup. If you do not have a dose-measuring device, ask your pharmacist for one.

If your doctor changes your brand, strength, or type of gabapentin, your dosage needs may change. Ask your pharmacist if you have any questions about the new brand you receive at the pharmacy.

Do not stop using gabapentin suddenly, even if you feel fine. Stopping suddenly may cause increased seizures. Follow your doctor’s instructions about tapering your dose.

Wear a medical alert tag or carry an ID card stating that you take gabapentin. Any medical care provider who treats you should know that you take seizure medication.

This medication can cause you to have a false positive urine protein screening test. If you provide a urine sample for testing, tell the laboratory staff that you are taking gabapentin.

Store at room temperature away from light and moisture.

  • Before starting this treatment, read the manufacturer’s printed information leaflet from inside the pack. The leaflet will give you more information about gabapentin and any possible side-effects from taking it.
  • Take gabapentin exactly as your doctor has told you to. You will be advised to take a small dose when you first start taking gabapentin and then to increase your doses over a few days as your body gets used to it. Your doctor or pharmacist will explain this to you and your dose will also be on the label of your pack.
  • Gabapentin is not suitable for children under 6 years of age but, if it has been prescribed for a child who is older than this, check the label carefully to make sure you are giving the correct dose.
  • You can take gabapentin before or after meals. Swallow the tablets/capsules with a drink of water.
  • Once you are taking a regular amount of gabapentin, try to take your doses at the same times each day. This will help you to avoid missing any of your doses.
  • If you do forget to take a dose, take it as soon as you remember, but do not take two doses together to make up for a forgotten dose.
  • If you need to take an antacid or indigestion remedy, do not take it during the two hours before and the two hours after you take gabapentin. This is because they interfere with the way gabapentin works.

Store the liquid medicine in the refrigerator. Do not freeze.

Gabapentin is Used primarily to Treat Seizures and Neuropathic Pain

Gabapentin is used primarily to treat seizures and neuropathic pain. It is also commonly prescribed for many off-label uses, such as treatment of anxiety disrders, insomnia, and bipolar disorder.

There are, however, concerns regarding the quality of the trials conducted and evidence for som such uses, especially in the case of its use as a mood stabilizer in bipolar disorder.

Seizures

Gabapentin is approved for treatment of focal seizures and mixed seizures. There is insufficient evidence for its use in generalized epilepsy.

Pain

A 2010 European Federation of Neurological Societies task force clinical guideline based on available evidence recommended gabapentin as a first-line treatment for diabetic neuropathy and postherpetic neuralgia with its highest level of evidence it also recommended gabapentin as a first-line treatment for central pain but with lower evidence. It also found good evidence that a combination of gabapentin and morphine or oxycodone or nortriptyline worked better than either drug alone; the combination of gabapentin and venlafaxine may be better than gabapentin alone.

A 2017 Cochrane review found evidence of moderate quality showing a reduction in pain by 50% in about 15% of people with postherpetic neuralgia and diabetic neuropathy. Evidence finds little benefit and significant risk in those with chronic low back pain. It is not known if gabapentin can be used to treat other pain conditions, and no difference among various formulations or doses of gabapentin was found.

A 2010 review found that it may be helpful in neuropathic pain due to cancer. It is not effective in HIV-associated sensory neuropathy and does not appear to provide benefit for complex regional pain syndrome.

A 2009 review found gabapentin may reduce opioid use following surgery, but does not help with post-surgery chronic pain. A 2016 review found it does not help with pain following a knee replacement.

It appears to be as effective as pregabalin and costs less.

All doses appear to result in similar pain relief.

Migraine

The American Headache Society (AHS) and American Academy of Neurology (AAN) guidelines classify gabapentin as a drug with “insufficient data to support or refute use for migraine prophylaxis. Furthermore, a 2013 Cochrane review concluded that gabapentin was not useful for the prevention of episodic migraine in adults.

Anxiety Disorders

Gabapentin has been used off-label for the treatment of anxiety disorders. However, there is dispute over whether evidence is sufficient to support it being routinely prescribed for this purpose.

 

Other Uses

Gabapentin may be useful in the treatment of comorbid anxiety in bipolar patients, (however not the bipolar state itself). Gabapentin may be effective in acquired pendular nystagmus and infantile nystagmus, (but not periodic alternating nystagmus). It is effective in hot flashes. It may be effective in reducing pain and spasticity in multiple sclerosis. Gabapentin may reduce symptoms of alcohol withdrawal (but it does not prevent the associated seizures).

There is some evidence for its role in the treatment of alcohol use disorder; the 2015 VA/DoD guideline on substance use disorders lists gabapentin as a “weak for” and is recommended as a second-line agent. Use for smoking cessation has had mixed results. Gabapentin is effective in alleviating itching in kidney failure (uremic pruritus) and itching of other causes. It is an established treatment of restless legs syndrome. Gabapentin may help sleeping problems in people with restless legs syndrome and partial seizures. Gabapentin may be an option in essential or orthostatic tremor.

Gabapentin is not effective alone as a mood-stabilizing treatment for bipolar disorder. There is insufficient evidence to support its use in obsessive compulsive disorder and treatment-resistant depression. Gabapentin does not appear effective for the treatment of tinnitus.

When Was Gabapentin Approved by the U.S. Food and Drug Administration (FDA) ?

About Gabapentin

There are many drugs used to treat anxiety. New studies are now showing that Gabapentin has been a successful treatment for individuals who suffer from anxiety. However, there are no randomized controlled trials on the effectiveness of this medication in generalized anxiety disorder (GAD), and there are only a few case reports.

People with GAD who take Gabapentin have shown to be less irritable, reduce the use of alcohol as self-medication, have fewer depression symptoms, feel less anxious anticipating the future, improve in phobic avoidance (going out in public more and experiencing a significant decrease in panic disorder and reduction of panic attacks).

Gabapentin is an anticonvulsant drug that is primarily used to treat seizures and the pain that follows after an episode of shingles. Gabapentin is considered an off-brand drug used to treat anxiety. Neurontin is the most common brand name for Gabapentin, as well as Horizant and Gralise. Gabapentin has shown to help people with sleeping better, as insomnia is a symptom of anxiety.

Side Effects of Gabapentin 

Like all medications, there are several side effects to taking Gabapentin. Side effects that you experience are relative to your personal reaction to the drug. Everyone is different, so you may not experience side effects that others do or don’t. Some side effects can be nausea, vomiting, tremors, dizziness, sleepiness, double vision, loss of control of bodily movements, fluid retention, difficulty speaking, jerky movements, unusual eye movements, double vision, and unsteadiness.

If you begin to experience any of these symptoms, speak with your doctor immediately. Get emergency help if you suspect you are having an allergic reaction like; swelling of your face, lips, tongue, or throat, hives, and difficulty breathing. If you notice that your symptoms are worsening, contact your doctor immediately. You may not notice symptoms until weeks after taking Gabapentin.

Is Gabapentin Approved by the U.S. Food and Drug Administration (FDA) ?

Gabapentin was originally approved by the U.S. Food and Drug Administration (FDA) in December 1993, for use as an adjuvant medication to control partial seizures (effective when added to other antiseizure drugs) in adults; that indication was extended to children in 2000. In 2004, its use for treating postherpetic neuralgia (neuropathic pain following shingles) was approved.

Gabapentin is best known under the brand name Neurontin manufactured by Pfizer subsidiary Parke-Davis. A Pfizer subsidiary named Greenstone markets generic gabapentin.

In December 2004 the FDA granted final approval to a generic equivalent to Neurontin made by the Israeli firm Teva.

Neurontin began as one of Pfizer’s best selling drugs; however, Pfizer has come under heavy criticism and serious litigation for its marketing of the drug.

They face allegations that, behind the scenes, Parke-Davis marketed the drug for at least a dozen supposed uses that the FDA had not approved.

Today it is a mainstay drug for migraines, even though it was not approved for such use in 2004.

What is Gabapentin Used for ?

Gabapentin comes as a capsule, a tablet, an extended-release (long-acting) tablet, and an oral solution (liquid) to take by mouth. Gabapentin capsules, tablets, and oral solution are usually taken with a full glass of water (8 ounces [240 milliliters]), with or without food, three times a day.

These medications should be taken at evenly spaced times throughout the day and night; no more than 12 hours should pass between doses. The extended-release tablet (Horizant) is taken with food once daily at about 5 PM. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take gabapentin exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.

Gabapentin extended-release tablets cannot be substituted for another type of gabapentin product. Be sure that you receive only the type of gabapentin that was prescribed by your doctor. Ask your pharmacist if you have any questions about the type of gabapentin you were given.

Swallow the extended-release tablets whole; do not cut, chew, or crush them.

If your doctor tells you to take one-half of a regular tablet as part of your dose, carefully split the tablet along the score mark. Use the other half-tablet as part of your next dose. Properly dispose of any half-tablets that you have not used within several days of breaking them.

If you are taking gabapentin to control seizures or PHN, your doctor will probably start you on a low dose of gabapentin and gradually increase your dose as needed to treat your condition. If you are taking gabapentin to treat PHN, tell your doctor if your symptoms do not improve during your treatment.

Gabapentin may help to control your condition but will not cure it. Continue to take gabapentin even if you feel well. Do not stop taking gabapentin without talking to your doctor, even if you experience side effects such as unusual changes in behavior or mood. If you suddenly stop taking gabapentin tablets, capsules, or oral solution, you may experience withdrawal symptoms such as anxiety, difficulty falling asleep or staying asleep, nausea, pain, and sweating. If you are taking gabapentin to treat seizures and you suddenly stop taking the medication, you may experience seizures more often. Your doctor may decrease your dose gradually over at least a week.

Your doctor or pharmacist will give you the manufacturer’s patient information sheet (Medication Guide) when you begin treatment with gabapentin and each time you refill your prescription. Read the information carefully and ask your doctor or pharmacist if you have any questions. You can also visit the Food and Drug Administration (FDA) website (http://www.fda.gov/Drugs) or the manufacturer’s website to obtain the Medication Guide.

Off-label use exposes patients to adverse effects and generally is not supported by evidence.

The only conditions for which gabapentinoid drugs are FDA-approved to manage pain are postherpetic neuralgia (both gabapentin and pregabalin [Lyrica]) and diabetic neuropathy, spinal cord injury, and fibromyalgia (pregabalin only). Nevertheless, use of these drugs has tripled during the past 15 years. This increase likely reflects gabapentinoid use for managing non–FDA-approved pain conditions, in part to avoid opioid use. In this review, researchers identified 34 placebo-controlled randomized trials (with ≈4200 patients) of gabapentinoids for noncancer, non–FDA-approved pain conditions. Most trials’ durations were 4 to 12 weeks.

Results of the review were as follows:

  • Only weak evidence supports use of gabapentin for diabetic neuropathy (only pregabalin is approved for this indication).
  • Minimal evidence supports use of gabapentin for nondiabetic painful neuropathies.
  • Studies of gabapentinoids for managing low back pain or sciatica have been largely negative.
  • Only minimal evidence supports a clinically meaningful benefit of off-label gabapentin use for fibromyalgia (for which pregabalin is approved).
  • Both gabapentin and pregabalin are approved for managing postherpetic neuralgia, but both are used often for acute zoster pain, for which studies have shown no benefit.
  • A small number of studies of gabapentinoid use for other pain syndromes (e.g., traumatic nerve injury, complex regional pain syndrome, burn injury, sickle cell pain) showed no clinically important benefits.

COMMENT

The markedly increased off-label use of gabapentinoids to manage pain has no or limited evidence of benefit. This practice is worrisome, especially given known high rates of side effects, including dizziness, somnolence, and unsteadiness. In addition, the authors note that patients often are prescribed gabapentinoids to avoid opioid use, but such patients sometimes still use opioids, either prescribed or illicit. The combination of gabapentinoids and opioids is associated with excess risk for opioid overdose.

Dr. Brett is an author of this article and is the Editor-in-Chief of NEJM Journal Watch General Medicine; however, he had no role in selecting or summarizing this article.

What is the Triggers of Migraine and How to Kick your Migraine away ?

“A migraine is like a tornado; it attacks fast without any warning and wreaks havoc. ”

Migraines usually start during the teenage years or early in adult life, affecting more women than men with a ratio of three to one. Migraines are caused from constricted (tightening) arteries that supply blood flow to the brain. When the arteries constrict, blood flow to the brain is reduced as well as the brains oxygen supply. The brain reacts by dilating (enlarging) arteries to meet the brain’s need for energy. The dilation spreads to the arteries in the neck and scalp and is the culprit of the pain in migraines.

If you live with migraines, make sure to have your Doctor rule out an underlying illness or other medical conditions that mimic migraines with the appropriate tests: for example , x-rays determining sinus infection, EEG for seizure activity or a CAT scan to detect blood clots or a brain tumor. Your Dr . may determine a drug to help ease your pain.

Eight Migraine Triggers

1 . Cerviogentic Headache:

Some people who have a tender neck and suffer from sore bone and joint problems are diagnosed with this type

2 . Temporomandibular Migraine:

Triggered by teeth grinding

3. Sinus Migraine:

Triggered by allergies and caused by excessive mucous and often accompanied by a fever. If you have this type of migraine, you may experience pain around both eyes and also may feel nauseated and sensitive to light.

4. Genetic Migraines:

Studies have lined a gene to people affected with migraines. Often when the gene for migraines is passed on to the next generation, the recipient will also experience headaches around the same age as the person who passed on the migraine.

5. Stress Migraine:

Stress can be a major contributing factor to the onset of a migraine. Type A personalities are more likely to experience migraines. Type A is ambitious, bright, perfectionist, emotionally repressed, cautious and has a decreased ability to manage stress. However , this is the easiest type of migraine to treat because a type A personality can acquire the skills necessary to manage stress.

6. Hormonal Migraine:

Fluctuating hormones in women are often the cause of migraines and can happen during menstrual cycles.

7. Cigarette Migraine

An equal opportunity source of migraines is because the nicotine alters blood vessels. High carbon monoxide levels in a person who smokes or even inhales second hand smoke can lead to a migraine.

8. Food Migraines

Food allergies are another factor that leads to migraines. However , migraine sufferers are able to eat chocolate without falling prey to a migraine. Some patients actually report relief from eating chocolate.

Foods that Can Cause Migraines

1 . Aged cheese such as Roquefort, Stilton and Sharp Cheddar
2 . Fermented Dairy such as Sour Cream, Buttermilk and Yogurt
3. Citrus: Oranges or Grapefruit, including juice
4. Nuts: Peanuts, Walnuts or Pecans
5. Legumes: Peas, Beans and Soy product 6. Onions and Garlic
7. Bananas
8. Pickled foods: picked herring is the most common instigator
9. MSG found in Chinese food
10. Alcohol

Now that you know the common triggers, also note that skipping meals also causes migraines. Skipping meals causes your blood sugar to drop, which in turn causes a migraine.

Six Ways to Kiss Your Migraine Goodbye

1 . Medicine

Medicines have been used for centuries to treat migraines. Today Dr’s prescribe Beta Blockers to treat migraines by maintaining adequate dilation of blood vessels. Antidepressants: The brain chemical ‘serotonin’ plays a role in migraine attacks because the levels of serotonin may cause or relieve migraine and that’s why Drs sometimes prescribe antidepressants for migraines. Antidepressants reduce migraine frequency by regulating serotonin levels in the brain. Other drugs are triptans available as an injection or nasal spray. This type of drug shuts down the inflammation and transmission of migraine pain.

Fioricet is the best medicine for the Migraine Treatment and make you get migraine go away.

2 . Surgical Treatment

Nerve stimulators have been used to control back and muscle pain and in 2003 a nerve stimulator was successfully used to treat chronic headaches. With nerve stimulation, one end of a wire is connected to a nerve that controls pain and the other is connected to a small battery powered generator. The patient controls the generator via a remote device. Once turned on, it disconnects the pain signal.

Not only do chronic migraine suffers face agonizing physical disabilities, they also have the psychological fear of not being able to earn a living or manage their home life because daily activities can suddenly become unbearable with the onset of a migraine.

3. Holistic Intervention

Rarely are people offered a non drug approach to treating migraines. Treating a migraine holistically not only can treat the migraine at onset but can also act as prevention.

Create a headache diary listing the 5 W’s.

A. Who were you with?
B. Where? Did someone irritate you? At work with glaring lights?
C. What? What medications were you on?
D. When? When did the headache start?
E. Why? Did some particular food or drink aggravate the situation? Did you get enough sleep?

4. Review your diary after 30 days and see if you can isolate the trigger.

5. Use heat to help dilate the blood vessels in the body. This must be done at direct onset of your migraine. Soak your hands in hot water for 20-30 minutes. As the migraine progresses and the blood vessels enlarge, apply ice to the back of the neck and forehead to help constrict capillaries that are pressing against the nerves.

6. Relaxation techniques

You can use relaxation techniques to manage stress. Research has found that people who consciously practice yoga daily for 30 – 45 minutes can learn to positively manipulate involuntary bodily responses like migraine pain. Studies have shown that relaxation practiced on a regular basis achieves a 45 to 80% reduction or elimination in both migraine severity and frequency. Yoga triggers a boost in the brain chemical serotonin, a neurotransmitter that is involved with your body’s anger, pain, sleep and migraine and can be a cure for headaches.

Frequent headaches are a sign that you are stressed out and it’s your body’s way of saying slow down and take care of me. Especially if you are a type A personality. My type A patients often say they can’t sit still and have a difficult time with the relaxation/mediation part of yoga. My reply? What’s more difficult to live with. Meditating daily or living with a migraine, a stroke or a heart attack? These are very real situations that afflict people with constricted arteries and that’s why it’s vital that you make time for your health.

Unfortunately for my patients, I often meet them after they’ve suffered from a condition of vascular abnormality. They are very motivated to participate because they have experienced what happens when blood flow to the heart or brain is compromised. Consequently they practice my techniques daily to reduce a recurrence.

Why not make time now? There are 1440 minutes in a day. 45 minutes a day practicing yoga is a wise investment in your health that offers a positive life style with increased energy without the use of toxic drugs polluting your liver and fewer Doctor visits which equals fewer co-payments. Yoga Chi for Energy DVD includes medically engineered relaxation techniques with an 11 minute meditation by a crackling fireplace.

Is Fioricet Effective for Migraines?

Sometimes. There is very little scientific research to show Fioricet can stop a migraine. It is intended to be used for tension-type (muscle tension) headaches, which are different from migraines.

There is good research to show acetaminophen is effective at stopping migraines. Unfortunately, the dose of acetaminophen that works best to stop a migraine is lower than the dose in Fioricet.

What are some of the dangers of taking Fioricet for migraine?

  • Fioricet can be habit-forming: Over time, your body can stop responding to a regular dose of Fioricet, which might push you to take a higher dose than you normally would. It is also possible to develop a dependency on Fioricet. In other words, you might begin to think you can’t feel normal without it. This might cause you to take Fioricet too frequently.
  • Too much Fioricet can make you dangerously sleepy: Butalbital is a relaxant, and it can be harmful when combined with other relaxants, including alcohol. In large doses this effect can be life-threatening. Additionally, because Fioricet contains acetaminophen and caffeine, you should not take it with Tylenol, cold medicines that contain acetaminophen, caffeine pills, or caffeine-containing beverages like coffee, soda, or energy drinks. Both acetaminophen and caffeine are also dangerous at high doses.
  • Stopping Fioricet quickly can cause withdrawal: If you’ve been taking Fioricet for a while, you could experience symptoms of withdrawal, including seizures, if you stop taking it suddenly. Talk to your provider about finding a way to lower your dose safely if this is a problem for you.
  • Taking Fioricet can increase your risk of headaches: Taking Fioricet frequently can cause a different sort of headache, called a medication-overuse headache. Also, when the caffeine in Fioricet wears off, some people get a rebound headache.
  • Too much Fioricet can damage your liver: The acetaminophen ingredient in Fioricet can cause damage to your liver if you take it too often. If you already have liver problems you should avoid Fioricet.
  • Fioricet is not a good choice for pregnant or nursing women: If you take Fioricet while you are pregnant, your newborn baby could experience withdrawal symptoms after they are born. Acetaminophen and caffeine carry their own risks during pregnancy. In addition, all three ingredients can be passed through the breastmilk to infants who are nursing. Fortunately, there are other medications you can take if you are pregnant or nursing and need treatment for your migraines.

When should you take Fioricet for migraine?

Fioricet is best when it is used for tension-type headaches, which are different from migraines.

Tension-type headaches, which are also known as muscle contraction headaches, usually feel like a steady tightness on both sides of the head. They don’t cause nausea or vomiting and don’t get worse with movement. Unlike migraines, tension-type headaches also don’t usually get worse with bright lights or loud sounds.

For migraines, safer and more effective medications are available (see next section). If nothing else works for you, Fioricet can be a back-up option.

Regardless of why you are taking it, Fioricet should only be used occasionally.

Off-label Use of Gabapentin

Gabapentin is an anticonvulsant prescription drug that goes by several brand names including, Neurontin, Gralise, Gabarone, and Fanatrex.

Gabapentin is used to help control partial seizures (convulsions) in the treatment of epilepsy. This medicine cannot cure epilepsy and will only work to control seizures for as long as you continue to take it.

Gabapentin is also used to manage a condition called postherpetic neuralgia, which is pain that occurs after shingles.

Gabapentin works in the brain to prevent seizures and relieve pain for certain conditions in the nervous system. It is not used for routine pain caused by minor injuries or arthritis. Gabapentin is an anticonvulsant.

This medicine is available only with your doctor’s prescription.

This product is available in the following dosage forms:

  • Capsule
  • Tablet
  • Solution
  • Suspension

It was approved by the FDA in December 1993 for the following main uses.

    1. Controlling certain types of seizures in people who have epilepsy
    2. Relieving nerve pain (think: burning, stabbing, or aches) from shingles
    3. Calming restless legs syndrome

Gabapentin is prescribed off-label for several conditions including:

    • migraine
    • anxiety disorders
    • fibromyalgia
    • bipolar disorder
    • insomnia

Gabapentin is also used off-label to treat chronic pain (as an alternative to opioid medications), alcohol use disorder (AUD), and substance use disorder (SUD).

Today there’s growing concern about increased misuse of gabapentin. Greater numbers of prescriptions means more access to gabapentin.

The risk of misuse is higher among those with an existing SUD — 15 to 22 percent. Overdose deaths have been reported when combined with other drugs.

Studies show an increase in overdose deaths in recent years linked to the rise in the number of overall prescriptions.

Certain drugs like opioids taken together increase the danger of overdose.

Several states are currently considering legislation to help stop this misuse. Many have put special monitoring requirements in place for gabapentin.

 

 

What is Fioricet?

If you’re struggling with constant All kinds of Headache, your doctor might prescribe you a medication called Fioricet.  This proprietary, brand name medication is actually a combination of other medications.

Fioricet is supplied in hard-gelatin capsule form for oral administration.

Each capsule contains the following active ingredients:

Butalbital, USP……………………50 mg
Acetaminophen, USP…………….300 mg
Caffeine, USP……………………..40 mg

Inactive Ingredients: sodium lauryl sulfate, talc, microcrystalline cellulose, stearic acid, FD&C red # 40, titanium dioxide, FD&C blue # 1,FD&C yellow # 6, gelatin.

The basic component is, surprisingly enough, acetaminophen, a common pain relieving medication that you can easily get over the counter. Since it’s mixed with another powerful medication, though, it’s something that you can only get by prescription.

The second ingredient in this medication is Butalbital, which is a barbiturate, commonly used to relieve muscle tension. Since many of the worst All kinds of Headache that you can get are actually caused by tense muscles in the neck and shoulders, this is a very helpful addition to a very helpful pain killer.

The formulation of this medication is accentuated with a dose of caffeine. Although caffeine doesn’t necessarily stop All kinds of Headache, it does have an effect on the central nervous system. It stimulates the veins and relaxes them, allowing blood to flow more freely. This, in and of itself, can have a mild pain relieving effect on All kinds of Headache. However, it’s mainly useful because it can help the other two drugs to be delivered to the body’s various systems more easily.

Fioricet is a medication that you need a prescription for, but you don’t necessarily have to buy it through traditional pharmacies. These days, online pharmacies are very popular for buying medications like these. It’s easy because you don’t have to actually go anywhere to get your medications. They can be delivered right to your door for a minimal cost.

Before you purchase Fioricet online, though, make sure that you’re getting it from a reputable online drugstore where you are assured of the quality of your medication and the quantity you’re going to get.

One of the main advantages of buying online is that you can save money, too, but make sure you’re getting what you pay for with this medication.

Many people who purchase Fioricet online find that they enjoy the utter privacy of it. No one needs to know that you’re suffering from All kinds of Headache, but you can get relief easily and quickly by having your medication delivered to your door. One you start taking this medication, you’ll see just how quickly and effectively it works on All kinds of Headache of all sorts, and you’ll be able to get rid of your All kinds of Headache more efficiently than ever before.

Fioricet Clinical Pharmacology

This combination drug product is intended as a treatment for tension headache.

It consists of a fixed combination of butalbital, acetaminophen, and caffeine. The role each component plays in the relief of the complex of symptoms known as tension headache is incompletely understood.

Pharmacokinetics

The behavior of the individual components butalbital apap caffeine  is described below.

Butalbital

Butalbital is well absorbed from the gastrointestinal tract and is expected to distribute to most tissues in the body. Barbiturates in general may appear in breast milk and readily cross the placental barrier. They are bound to plasma and tissue proteins to a varying degree and binding increases directly as a function of lipid solubility.

Elimination of butalbital is primarily via the kidney (59% to 88% of the dose) as unchanged drug or metabolites. The plasma half-life is about 35 hours. Urinary excretion products include parent drug (about 3.6% of the dose), 5-isobutyl-5-(2, 3-dihydroxypropyl) barbituric acid (about 24% of the dose), 5-allyl-5(3-hydroxy-2-methyl-1-propyl) barbituric acid (about 4.8% of the dose), products with the barbituric acid ring hydrolyzed with excretion of urea (about 14% of the dose), as well as unidentified materials. Of the material excreted in the urine, 32% is conjugated.

The in vitro plasma protein binding of butalbital is 45% over the concentration range of 0.5-20 mcg/mL. This falls within the range of plasma protein binding (20%-45%) reported with other barbiturates such as phenobarbital, pentobarbital, and secobarbital sodium. The plasma-to-blood concentration ratio was almost unity, indicating that there is no preferential distribution of butalbital into either plasma or blood cells.

 Acetaminophen

Acetaminophen is rapidly absorbed from the gastrointestinal tract and is distributed throughout most body tissues. The plasma half-life is 1.25 to 3 hours, but may be increased by liver damage and following overdosage. Elimination of acetaminophen is principally by liver metabolism (conjugation) and subsequent renal excretion of metabolites. Approximately 85% of an oral dose appears in the urine within 24 hours of administration, most as the glucuronide conjugate, with small amounts of other conjugates and unchanged drug.

Caffeine

Like most xanthines, caffeine is rapidly absorbed and distributed in all body tissues and fluids, including the CNS, fetal tissues, and breast milk.

Caffeine is cleared through metabolism and excretion in the urine. The plasma half-life is about 3 hours. Hepatic biotransformation prior to excretion results in about equal amounts of 1-methylxanthine and 1-methyluric acid. Of the 70% of the dose that is recovered in the urine, only 3% is unchanged drug.

Fioricet is indicated for the relief of the symptom complex of tension (or muscle contraction) headache.

Evidence supporting the efficacy and safety of this combination product in the treatment of multiple recurrent headaches is unavailable. Caution in this regard is required because butalbital is habit-forming and potentially abusable.

Before taking this medicine

Do not use Fioricet if you have taken an MAO inhibitor in the past 14 days. A dangerous drug interaction could occur. MAO inhibitors include isocarboxazid, linezolid, phenelzine, rasagiline, selegiline, and tranylcypromine.

You should not use Fioricet if you are allergic to acetaminophen, butalbital, or caffeine, if you have porphyria, or if you have recently used alcohol, sedatives, tranquilizers, or other narcotic medications.

To make sure Fioricet is safe for you, tell your doctor if you have:

  • liver disease, cirrhosis, a history of alcoholism or drug addiction, or if you drink more than 3 alcoholic beverages per day;
  • kidney disease;
  • asthma, sleep apnea, or other breathing disorder;
  • stomach ulcer or bleeding;
  • a history of skin rash caused by any medication;
  • a history of mental illness or suicidal thoughts; or
  • if you use medicine to prevent blood clots.

It is not known whether Fioricet will harm an unborn baby. If you use butalbital while you are pregnant, your baby could become dependent on the drug. This can cause life-threatening withdrawal symptoms in the baby after it is born. Babies born dependent on habit-forming medicine may need medical treatment for several weeks. Tell your doctor if you are pregnant or plan to become pregnant.

What should I avoid while taking Fioricet?

This medication can cause side effects that may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be awake and alert.

Avoid drinking alcohol. It may increase your risk of liver damage while taking acetaminophen.

Ask a doctor or pharmacist before using any other cold, allergy, pain, or sleep medication. Acetaminophen (sometimes abbreviated as APAP) is contained in many combination medicines. Taking certain products together can cause you to get too much acetaminophen which can lead to a fatal overdose. Check the label to see if a medicine contains acetaminophen or APAP.

While you are taking this medication, avoid taking diet pills, caffeine pills, or other stimulants (such as ADHD medications) without your doctor’s advice.

 Fioricet Side Effects

Frequently Observed

The most frequently reported adverse reactions are drowsiness, lightheadedness, dizziness, sedation, shortness of breath, nausea, vomiting, abdominal pain, and intoxicated feeling.

Infrequently Observed

All adverse events tabulated below are classified as infrequent.

Central Nervous System: headache, shaky feeling, tingling, agitation, fainting, fatigue, heavy eyelids, high energy, hot spells, numbness, sluggishness, seizure. Mental confusion, excitement, or depression can also occur due to intolerance, particularly in elderly or debilitated patients, or due to overdosage of butalbital.

Autonomic Nervous System: dry mouth, hyperhidrosis.

Gastrointestinal: difficulty swallowing, heartburn, flatulence, constipation.

Cardiovascular: tachycardia.

Musculoskeletal: leg pain, muscle fatigue.

Genitourinary: diuresis.

Miscellaneous: pruritus, fever, earache, nasal congestion, tinnitus, euphoria, allergic reactions.

Several cases of dermatological reactions, including toxic epidermal necrolysis and erythema multiforme, have been reported.

The following adverse drug events may be borne in mind as potential effects of the components of this product. Potential effects of high dosage are listed in the OVERDOSAGE  section.

Acetaminophen: allergic reactions, rash, thrombocytopenia, agranulocytosis.

Caffeine: cardiac stimulation, irritability, tremor, dependence, nephrotoxicity, hyperglycemia.

Fioricet Overdose

Following an acute overdosage of butalbital, acetaminophen, and caffeine, toxicity may result from the barbiturate or the acetaminophen. Toxicity due to caffeine is less likely, due to the relatively small amounts in this formulation.

Signs and Symptoms

Toxicity from barbiturate poisoning includes drowsiness, confusion, and coma; respiratory depression; hypotension; and hypovolemic shock.

In acetaminophen overdosage: dose-dependent, potentially fatal hepatic necrosis is the most serious adverse effect. Renal tubular necrosis, hypoglycemic coma, and coagulation defects may also occur. Early symptoms following a potentially hepatotoxic overdose may include: nausea, vomiting, diaphoresis, and general malaise. Clinical and laboratory evidence of hepatic toxicity may not be apparent until 48 to 72 hours post-ingestion.

Acute caffeine poisoning may cause insomnia, restlessness, tremor, and delirium, tachycardia and extrasystoles.

Treatment

A single or multiple drug overdose with this combination product is a potentially lethal polydrug overdose, and consultation with a regional poison control center is recommended. Immediate treatment includes support of cardiorespiratory function and measures to reduce drug absorption.

Oxygen, intravenous fluids, vasopressors, and other supportive measures should be employed as indicated. Assisted or controlled ventilation should also be considered.

Gastric decontamination with activated charcoal should be administered just prior to N-acetylcysteine (NAC) to decrease systemic absorption if acetaminophen ingestion is known or suspected to have occurred within a few hours of presentation. Serum acetaminophen levels should be obtained immediately if the patient presents 4 hours or more after ingestion to assess potential risk of hepatotoxicity; acetaminophen levels drawn less than 4 hours post-ingestion may be misleading. To obtain the best possible outcome, NAC should be administered as soon as possible where impending or evolving liver injury is suspected.

Intravenous NAC may be administered when circumstances preclude oral administration.

Vigorous supportive therapy is required in severe intoxication. Procedures to limit the continuing absorption of the drug must be readily performed since the hepatic injury is dose dependent and occurs early in the course of intoxication.

Fioricet Drug Interaction

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.

  • Riociguat

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

  • Alfentanil
  • Alprazolam
  • Amobarbital
  • Anisindione
  • Aprobarbital
  • Butabarbital
  • Carisoprodol
  • Chloral Hydrate
  • Chlordiazepoxide
  • Chlorzoxazone
  • Clarithromycin
  • Clonazepam
  • Clorazepate
  • Dantrolene
  • Darunavir
  • Diazepam
  • Dicumarol
  • Doxorubicin
  • Doxorubicin Hydrochloride Liposome
  • Esketamine
  • Estazolam
  • Ethchlorvynol
  • Etonogestrel
  • Flunitrazepam
  • Flurazepam
  • Halazepam
  • Imatinib
  • Iobenguane I 131
  • Isoniazid
  • Ketazolam
  • Lorazepam
  • Lormetazepam
  • Medazepam
  • Mephenesin
  • Mephobarbital
  • Meprobamate
  • Metaxalone
  • Methocarbamol
  • Methohexital
  • Midazolam
  • Nifedipine
  • Nitrazepam
  • Oxazepam
  • Peginterferon Alfa-2b
  • Pentobarbital
  • Phenindione
  • Phenobarbital
  • Phenprocoumon
  • Piperaquine
  • Pixantrone
  • Pneumococcal 13-Valent Vaccine, Diphtheria Conjugate
  • Prazepam
  • Primidone
  • Quazepam
  • Secobarbital
  • Sodium Oxybate
  • Temazepam
  • Thiopental
  • Trazodone
  • Triazolam
  • Ulipristal

Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

  • Acenocoumarol
  • Cannabis
  • Carbamazepine
  • Fosphenytoin
  • Lixisenatide
  • Ospemifene
  • Phenytoin
  • Prednisone
  • Warfarin
  • Zidovudine

What is a Fioricet High?

One of the key active ingredients responsible for the so-called Fioricet high is butalbital. Butalbital is a barbiturate that’s considered short-to-intermediate acting, and it can relieve symptoms of anxiety, reduce pain, relax muscles and act as a sedative. There are many neuropsychological effects of butalbital, some of which aren’t clearly understood to this day.

The belief is that the Fioricet high is caused by the fact that butalbital can increase the inhibition neurotransmitters in the brain called GABA. It can bind to certain receptor sites and ultimately central nervous system activity is depressed. This can lead to what feels like a buzz or to some people possibly a high.

So what does a Fioricet high feel like?

For the most part, it’s likely to feel similar to other central nervous system depressant effects. There is some evidence pointing to the fact that taking Fioricet can feel similar to the effects of drinking alcohol, particularly when the prescription drug is taken at higher levels.

The following are some of the common experiences that people say come along with a Fioricet high:

  • Fioricet can reduce anxiety and some people with anxiety disorders may take it for this reason, although this is not what it’s approved for. There is the potential for Fioricet to decrease feelings of anxiety even when it’s taken at a normal dose, and this is because of the impact of butalbital on GABA. For some people, a Fioricet high is actually just equated with a reduction in anxiety.
  • Depersonalization may be another effect of the so-called Fioricet high, although this isn’t necessarily something people find pleasant. It can lead to feelings of confusion and sluggishness, and this is one of the reasons Fioricet isn’t frequently used
  • Drowsiness and sedation may also be side effects of a Fioricet high, particularly when it’s taken in larger amounts. While Fioricet has a stimulant component which is caffeine when larger doses are taken the central nervous system depressant effects may override the stimulant effects.
  • Some people may obtain a sense of euphoria when taking Fioricet, although it’s not as pronounced as what would occur with something like prescription opioids. As with most other drugs, if someone does experience euphoria with a Fioricet high, it’s likely to dissipate after using the drug a few times as they build a tolerance.
  • While not everyone who takes Fioricet says they experience euphoria, some people say that it does improve their mood. This can be because of the GABA-related effects of butalbital, but also the inclusion of the acetaminophen and the caffeine. There’s also the element of stimulation that can occur with caffeine, so some people may feel this is a Fioricet high when they experience it.
  • Lightheadedness and dizziness are common side effects of Fioricet, and these may also be symptoms that people associate with a Fioricet high.
  • One of the primary reasons people will abuse Fioricet and take high doses is to achieve relaxation, which occurs because of the slowdown of the central nervous system. People who take this drug may feel relaxed and also tranquil. Some of this is because of the loosening up of muscles the drug can stimulate.

Not everyone will associate the use of this drug with the Fioricet high. Some of the factors that determine whether or not a person will experience a Fioricet high can include the dosage they take and their tolerance. Newer users may be more likely to experience what they would describe as the Fioricet high. Other factors that could influence this include the specific formulation of the drug and whether or not other substances are taken with it.

Some people may try to extract the butalbital from Fioricet and remove it from the caffeine and acetaminophen for a greater high. This is not only drug abuse, but might not even achieve the effects the person is looking for.

It’s important to realize that there can be serious and deadly consequences associated with trying to achieve a Fioricet high. This can include addiction, adverse reactions, brain damage, emotional crashes, and overdose. Since Fioricet has acetaminophen, if people abuse it to get high they may also sustain liver damage or failure.

How Gabapentin is Used ?

Gabapentin comes as a capsule, a tablet, an extended-release (long-acting) tablet, and an oral solution (liquid) to take by mouth.

Gabapentin is usually started at a low dose and then gradually increased. Be sure to follow your doctor’s instructions. A typical dose ranges between 900 mg and 1,800 mg daily, divided into three doses. You shouldn’t stop taking gabapentin suddenly. Be sure to talk to your doctor about the proper weaning procedure for the dose you’re taking.

Gabapentin capsules, tablets, and oral solution are usually taken with a full glass of water (8 ounces [240 milliliters]), with or without food, three times a day.

These medications should be taken at evenly spaced times throughout the day and night; no more than 12 hours should pass between doses. The extended-release tablet (Horizant) is taken with food once daily at about 5 PM. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take gabapentin exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.

Gabapentin extended-release tablets cannot be substituted for another type of gabapentin product. Be sure that you receive only the type of gabapentin that was prescribed by your doctor. Ask your pharmacist if you have any questions about the type of gabapentin you were given.

How Gabapentin Works

Gabapentin is believed to work by altering the release of glutamate and other neurotransmitters in your brain.1 Neurotransmitters send messages from one brain cell to another. Glutamate is really helpful for certain things, like learning new information. That’s because it gets your brain cells stirred up and active.

Kind of like a toddler with chocolate, though, if you have too much glutamate running around, your brain cells can become overstimulated. That can make all kinds of things go wrong.

Glutamate has more than one job, though. It also helps transmit pain signals in your brain and nerves. Too much glutamate may play a role in hyperalgesia, which essentially turns up the volume of pain.

Some diseases and conditions—including fibromyalgia—may interrupt this balance and let glutamate run amok. Gabapentin is believed to reduce your brain’s release of glutamate so the cells can calm down and your brain can function better.

Swallow the extended-release tablets whole; do not cut, chew, or crush them.

If your doctor tells you to take one-half of a regular tablet as part of your dose, carefully split the tablet along the score mark. Use the other half-tablet as part of your next dose. Properly dispose of any half-tablets that you have not used within several days of breaking them.

How Gabapentin is Used ?

If you are taking gabapentin to control seizures or PHN, your doctor will probably start you on a low dose of gabapentin and gradually increase your dose as needed to treat your condition. If you are taking gabapentin to treat PHN, tell your doctor if your symptoms do not improve during your treatment.

Gabapentin may help to control your condition but will not cure it. Continue to take gabapentin even if you feel well. Do not stop taking gabapentin without talking to your doctor, even if you experience side effects such as unusual changes in behavior or mood.

If you suddenly stop taking gabapentin tablets, capsules, or oral solution, you may experience withdrawal symptoms such as anxiety, difficulty falling asleep or staying asleep, nausea, pain, and sweating.

If you are taking gabapentin to treat seizures and you suddenly stop taking the medication, you may experience seizures more often. Your doctor may decrease your dose gradually over at least a week.

Your doctor or pharmacist will give you the manufacturer’s patient information sheet (Medication Guide) when you begin treatment with gabapentin and each time you refill your prescription. Read the information carefully and ask your doctor or pharmacist if you have any questions. You can also visit the Food and Drug Administration (FDA) website (http://www.fda.gov/Drugs) or the manufacturer’s website to obtain the Medication Guide.

Gabapentin is somewhat commonly prescribed as a fibromyalgia treatment. It’s available as a generic and is also sold under the brand names Neurontin, Horizant, and Gralise.

Gabapentin is not FDA approved for treating this condition, so it’s prescribed off-label. However, the drug is chemically related to Lyrica (pregabalin), which is approved for fibromyalgia. In fact, Lyrica is sometimes referred to as the “son of Neurontin.”

Gabapentin is classified as an anti-seizure drug. It’s used to treat epilepsy, neuropathy (pain from damaged nerves), restless legs syndrome, and hot flashes. Fibromyalgia pain is similar to neuropathy, but whether this condition involves nerve damage still isn’t clear.