28 Sep Gabapentin (Neurontin) Addiction
When Neurontin was the new drug on the block, physicians believed that they had found a real breakthrough drug to help patients with all kinds of nerve pain. The drug had fewer side effects and drug interactions than current ones on the market and was classified as non-addictive, which meant you did not have to keep extensive records on it every time you prescribed it.[i] Soon Neurontin was generating over $4 billion a year in sales.[ii]
Then the trouble began. A whistle-blower from the drug’s manufacturer claimed the company was spinning data on the drug’s effectiveness and using illegal means to promote its off-label uses among physicians. When the dust settled from civil and criminal lawsuits, Pfizer paid out $572 million to claimants.[iii] But not to worry. As soon as Neurontin became a cheap drug available generically, Pfizer marketed a close cousin of it named Lyrica, which today generates $3 billion a year in sales.[iv]
What is Gabapentin?
Gabapentin is an analog of gamma-aminobutyric acid (GABA), a neurotransmitter that slows down the activity of nerve cells in the brain. This means that gabapentin has a similar structure and is made up of similar chemicals as GABA, although its effect on the body is not the same. The scientists who developed gabapentin were deliberately trying to mimic GABA.
Gabapentin does not convert into GABA, does not inhibit it, does not alter the uptake of dopamine, and does not interact with GABA receptor cells.[v] How gabapentin works and how it relieves pain and suppresses seizures is unknown. One theory is that it increases the level of GABA by increasing the activity of glutamic acid decarboxylase, an enzyme responsible for the synthesis of GABA.[vi]
The chemical name for gabapentin is 2-[1-(aminomethyl) cyclohexyl]acetic acid and its molecule looks like this:
Gabapentin is not a Controlled Substance, that is, one that the United States federal government classifies as having potential for addiction and regulates under the Comprehensive Drug Abuse and Control Act of 1970. However, gabapentin shares characteristics of addictive drugs in that it produces a withdrawal syndrome and certain psychoactive effects. Its cousin drug, pregabalin, is a Schedule V Controlled Substance.
What are the Medical Uses of Gabapentin?
The United States Food and Drug Administration approved Neurontin for the treatment of seizures in adults and children, especially as a supplemental drug used for the same purpose. In 2002, the FDA approved it for treatment for pain from shingles. Horizant and Gralise are extended release versions of gabapentin that were approved for shingles pain in 2012.[vii] Gabapentin was also approved for restless leg syndrome in 2011.[viii]
When gabapentin was first introduced, doctors were excited about it because it had few side effects and drug interactions compared to competing remedies, and because it was not metabolized through the liver but rather excreted through the kidneys.[ix] Physicians began to prescribe it off-label for various conditions, including hot flashes during menopause, pain from fibromyalgia, bi-polar disorder, pain after polio, neuropathic pain, complex regional pain syndrome, trigeminal neuralgia, migraines, alcohol and drug withdrawal seizures, and diabetic neuropathy.[x] Later it was proven that the manufacturers of this drug had exaggerated claims about its effectiveness for various conditions.[xi] Pregabalin, commonly sold as Lyrica, is a newer drug now prescribed for nerve pain, epilepsy and fibromyalgia, and it has largely replaced gabapentin.[xii]
The usual dose for people over 12 years old who have epilepsy is 300mg three times a day. This can be increased to 1800mg a day. Doctors prescribe the drug to children with epilepsy based on their body weights.[xiii]
For post-herpetic neuralgia (shingles), the dose is the same as for epilepsy. For adults with restless leg syndrome, the dose is 600mg taken at five o’clock in the evening.[xiv]
Dosages for people with kidney problems may be different than these.[xv]
If you break a gabapentin tablet in order to take just half, you need to use the rest of the pill as your next dosage or else discard it.[xvi]
One unusual aspect of gabapentin is that its bioavailability decreases with the dose. For example, if you take 900mg, 60% is available to your body, but if you take 4800mg, that drops to only 27%.[xvii]
What are the Side Effects of Gabapentin?
The most common side effects of gabapentin are drowsiness, unsteadiness, sleepiness, loss of coordination, clumsiness, vision changes, and dry mouth.[xviii] Some people report the following rare side effects: edema, weight gain, swollen hands and feet, headaches, diarrhea, trouble thinking, abnormal thoughts, suicidal thoughts, fever, ataxia, diplopia, flu symptoms, shortness of breath, chest pain, mouth sores, chills, nausea, coughing, tremor, and other cold symptoms.
If you experience certain symptoms, you should call your doctor immediately because they can be a sign of a serious health condition. These can be black tarry stools, dark urine, tiredness, chest pain, suicidal mood, swollen glands, unusual bruising, rashes, or signs of an infection such as fever, cough and sore throat.[xix]
Children react to gabapentin differently than adults. They may experience behavioral changes, moodiness, hyperactivity, overly emotional states, and restlessness.[xx]
What Drugs Interact with Gabapentin?
In general, you should not take gabapentin products with medicines that slow down the central nervous system and make you drowsy. These may be anti-histamines, narcotic painkillers, sleeping pills, muscle relaxants, anti-anxiety medications, and drugs for depression and seizures.[xxi] Gabapentin products will react with drugs used during surgeries, even dental procedures.[xxii] Do not take gabapentin products with morphine (Kadian, MS Contin), naproxen (Aleve) or hydrocodone (Lortab, Vicodin).[xxiii]
Drugs containing gabapentin will interact with ketorolac, aluminum carbonate, aluminum hydroxide, aluminum phosphate, dihydroxyaluminum amino acetate, dihydroxyaluminum sodium carbonate, ginkgo, magaldrate, magnesium carbonate, magnesium hydroxide, magnesium trislicate, and morphine sulfate liposome. If you combine gabapentin with tobacco and alcohol and then take certain other drugs, you may cause an unpleasant or difficult reaction.[xxiv]
If you take any common antacids like Maalox and Di-Gel that contain aluminum or magnesium, you need to wait two hours before taking gabapentin.[xxv]
Which People Should not Take Gabapentin?
Gabapentin products have not been determined safe for pregnant or breast-feeding women or children, even though doctors sometimes prescribe it for children with epilepsy. People with histories of depression, mood or mental disorders, and kidney diseases usually do not take gabapentin because it can make these conditions worse.[xxvi] These drugs are used with caution for people with liver or heart diseases.[xxvii]
What Lawsuits Have Ensued Over Gabapentin?
At first the United States Food and Drug Administration approved Neurontin for only for epilepsy but by the year 2000, 78% of prescriptions that doctors wrote for Neurontin were for conditions other than seizure disorders. The new drug was widely prescribed “off label” for more than a dozen conditions, including fibromyalgia, nerve pain, migraines, menopausal symptoms, bipolar disorder, and even attention deficit disorder in children.[xxviii] Between 2000 and 2004, Neurontin was generating $1 to $4 billion in sales a year for its manufacturers, which were first Warner-Lambert and later Pfizer drug companies.[xxix]
In 2002, Dr. David Franklin, an employee of Warner-Lambert, went to authorities to report that his company was promoting Neurontin for uses not approved by the FDA. While it is not illegal for doctors to prescribe drugs for unapproved uses, it is illegal for a drug company to advertise and promote them for unapproved uses. [xxx] Dr. Franklin testified that Warner-Lambert paid to doctors to present themselves as authors of studies written by non-doctors employed by the company. He said that the company also paid doctors to speak to other doctors about the off-label uses of Neurontin, and offered physicians expensive retreats and dinners at expensive restaurants to promote the drug.[xxxi]
As criminal and civil lawsuits were filed against the company, more negative information came out. Pfizer had apparently delayed or suppressed publication of studies that were negative or neutral about Neurontin, and exaggerated any positive claims. For example, three double-blind studies showed that Neurontin did not improve the symptoms of bipolar patients any better than sugar pills, but the company manipulated the studies and how symptoms were defined in evaluating the success of Neurontin. Of the 12 studies of the drug’s effect on migraine headaches, two negative ones went unpublished, and some of the positive studies involved only patients who had taken 2400mg or more of the drug.[xxxii] In other studies, patients could easily figure out that they were not in the placebo group, and ordinarily this would have meant that the study could not be published. Company spokespeople denied all the charges, but Pfizer ended up paying out $430 million in claims to states enrolled in the Medicaid program.[xxxiii] In 2011, Judge Patti Saris of the U.S. District Court in Boston ordered Pfizer to pay Kaiser Health $142.1 million for duping the company into prescribing Neurontin for migraines and bipolar disorder.[xxxiv]
In 2004, gabapentin became available as a cheap generic drug,[xxxv] which drastically reduced its value as a money-maker for Pfizer. Pfizer introduced a similar but more potent drug called Lyrica, which was approved by the FDA in December 2004. Lyrica was approved for seizure disorders and pain from fibromyalgia, but it is now prescribed for many other conditions “off-label,” especially all kinds of chronic pain. Today Lyrica ranks 19th among all prescription drugs, and generates more than $3 billion a year for Pfizer.[xxxvi]
What are the Risks of Taking Gabapentin?
Gabapentin doubles the risk for suicidal thoughts and behaviors, but the risk is still low. In one study of 27,863 patients on Neurontin and 16,029 on a placebo, 0.43% of the ones on the real drug became suicidal compared to 0.24% on the sugar pill.[xxxvii]
Gabapentin has some potential for abuse because it has psychoactive effects. Once you have been on it for a while, you may experience a difficult withdrawal syndrome when you try to stop taking it.
Gabapentin causes drowsiness and incoordination, which means that you are at an increased risk for accidents, and probably should not drive when you take this medication.[xxxviii]
Gabapentin increases the risk for sudden death after seizures in patients who have epilepsy. It can cause certain dangerous and sometimes even fatal reactions. Symptoms of this condition can be fever, rash, painful lymph glands in the neck and armpit, unusual bleeding, and yellow eyes and skin.[xxxix] Both of these reactions are extremely rare.
Gabapentin may slightly increase your risk for cancer.[xl]
Does Gabapentin Show up on Urine Tests?
Gabapentin has a half-life of about five to seven hours, which means it should completely clear the body within 38 hours. Standard urine tests do not test for it because it is not a controlled substance.
What is a Gabapentin Overdose?
Symptoms of a gabapentin overdose may be appearing drunk and disoriented, with slurred speech and double vision.[xli] Such overdoses are very rare.
What is Gabapentin Withdrawal or Discontinuation Syndrome?
When gabapentin was first introduced, scientists believed that it could not cause a withdrawal syndrome. Since that time, there have been many case studies of people who experienced such difficult symptoms when they tried to stop using the drug that many had to go back on it. For example, one 81 year old woman with bipolar disorder took Neurontin for five years, and developed severe cold symptoms when she stopped. On the tenth day after stopping Neurontin in a gradual way, she had terrible chest pain, hypertension, and mental changes that were difficult to manage. She was back to normal within one day of taking the drug again.[xlii]
In another case study, a 53-year-old woman vomited a black substance like coffee grounds and developed abdominal pain and black stools after stopping gabapentin. By days four and five, she developed restlessness, anxiety, agitation, disorientation, confusion, headaches, and extreme sensitivity to light. When her doctor administered gabapentin again, she was calm and normal within a day.[xliii] Another such study found that a 41-year-old male developed insomnia, headaches, heart palpitations, and excessive sweating after stopping Neurontin, but his symptoms went away when he went back on it.[xliv]
It has now been proven that gabapentin can build up in the body and cause a severe withdrawal syndrome similar to the ones for benzodiazepines and alcohol. The syndrome can last for weeks and even months, depending on the levels you took the drug and for how long you took it. Symptoms are agitation, confusion, disorientation, sensitivity to light, headaches, heart palpitations, and hypertension, chest pain. If you were taking gabapentin for epilepsy, your seizures will probably come back. Some people develop seizures during withdrawal even if they never had one before.[xlv]
What is Gabapentin Addiction?
In theory, gabapentin should not be addictive because it has no affinity for the nerve receptors associated with addictions to marijuana, benzodiazepines or opiates. It was marketed as non-addictive, but post-marketing studies showed that some people were abusing it. In the early 2000s, the drug was being sold to thousands of people with sales were over a billion dollars a year. Some of these patients were asking their doctors to increase their amounts (self-escalation) as they developed physical dependencies on Neurontin. When they tried to quit, they entered a withdrawal syndrome that caused them to go back to the drug. The new conclusion about gabapentin, as one expert put it, “The dependence and abuse potential for gabapentin has not been evaluated in human studies.”[xlvi]
The United States Drug Enforcement Agency does not list gabapentin as a drug of concern, even though it is being sold on the Internet illegally. Its street name is “morontin” because it makes you “dopey.”
What Treatments are Available for Gabapentin Addiction?
Because the withdrawal syndrome for this drug can produce unpleasant and even dangerous symptoms, you need to consult your doctor or an addiction specialist at a drug rehabilitation clinic about how you can safely stop taking the drug. The usual method is to wean a patient from the drug by gradually lowering the dosage, but this does not always prevent the withdrawal syndrome.[xlvii] If you have tried unsuccessfully to quit taking gabapentin, you should seek professional help.
The state-of-the-art treatment for drug addiction is to enter a residential treatment center where your withdrawal can be done under medical supervision. If you are addicted to other drugs or alcohol as well as gabapentin, your detoxification process will become even more complicated.
Once you have completed detoxification and your body is completely clear of drugs, you need to remain at the center for a few weeks or more so that you can undergo therapy to learn to live a drug-free life. You will work one-on-one with a therapist who can help you with any psychological problems you may have that contribute to your drug abuse. You may learn how to deal stress through non-pharmaceutical means such as running or other sports, yoga, meditation, journaling and so forth. You may have classes in the chemistry of drugs and why they can get such a hold on people’s lives. You will learn how to avoid relapsing into drug abuse or alcoholism, even if you have a genetic tendency or long family history of such problems. Most drug rehab programs offer activities that are fun to do as well as ways of self-exploration, such as social gatherings, sightseeing, outdoor sports, and participating in art, drama and music. Once you return home, you usually remain in support meetings in your community and in individual and family counseling to help you stay on track.
How Can I Tell if I am Addicted to Gabapentin?
If you can answer yes to any of these questions, you may want to consider talking to your family physician or an addiction specialist at a residential treatment center about your concerns with gabapentin.
- Are you taking gabapentin without a doctor’s prescription?
- Do you ask your doctor to keep increasing your dose?
- Do you buy gabapentin from the Internet or other illegal sources?
- Do you experience withdrawal symptoms when you stop taking gabapentin?
- Have you tried to quit taking gabapentin on your own but failed?
- Do you consider yourself to be someone who abuses drugs or alcohol?
- Do you use gabapentin along with alcohol or other drugs as a way of treating emotional pain?
- Are you taking gabapentin even though you experience unpleasant side effects and even though you are unsure if it is effective for you?
- If money were no object, would you enter an intense program to help you deal with drug problems?
- Do your friends or family members criticize you because of your drug abuse?
- Do you feel guilty about how you use drugs?
- Are you trying to cut down on your use of gabapentin or other drugs?
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