Rx Gabapentin and Fioricet For Nerve Pain and Headache Relief

Neurontin (Generic Name: Gabapentin)  is approved to prevent and control partial seizures, relieve postherpetic neuralgia after shingles and moderate-to-severe restless legs syndrome. Learn what side effects to watch for, drugs to avoid while taking gabapentin, how to take gabapentin and other important questions and answers. Gabapentin is available in both branded and generic forms.

Gabapentin is frequently prescribed off-label for a variety of conditions outside its primary approvals for epilepsy and nerve pain. Gabapentin (Neurontin) is not a medication that would make the FDA proud. Less than 1% of its outpatient use is for an FDA indication, and a good portion of the off-label use takes place in psychiatry.

These trends sparked a backlash in the 2000s, when Pfizer paid a $1.3 billion fine for misleading marketing practices. Recent reports of misuse of gabapentin and its GABAergic cousin, pregabalin (Lyrica), have added to those concerns. In this article, we’ll look at where gabapentin fits in psychiatric practice.

What is Fioricet and What it is Used for ?

Fioricet is a combination medication containing butalbital, acetaminophen, and caffeine. It’s taken by mouth as needed, typically every 4 hours, to treat tension headaches. But it’s not a first-choice option because it can become habit-forming and can worsen headaches if taken too frequently.

How Does Fioricet Works ?

Fioricet is a combination of three medications that work together to help relieve headache pain.

  • Butalbital is a barbiturate that works by raising the levels of chemicals that cause your brain to relax.
  • Acetaminophen is an analgesic. It stops the production of certain chemicals in your brain, which can help relieve pain.
  • Caffeine is an adenosine antagonist. It blocks a natural chemical in your body called adenosine. It’s unclear exactly how caffeine works to treat headaches, but it’s thought to boost the pain-relieving activity of acetaminophen.

What Is Fioricet Used For ?

Fioricet is primarily approved for treating tension headaches, but it is sometimes used off-label to manage other conditions. “Off-label” refers to the use of a medication for purposes other than those approved by regulatory agencies like the FDA. These off-label uses are based on a doctor’s judgment and the medication’s known pharmacological effects.

Common Off-Label Uses of Fioricet

  1. Migraine Headaches
    • Fioricet is occasionally prescribed for migraines, although it is not FDA-approved for this purpose.
    • Caution is advised because frequent use may lead to medication overuse headaches or dependence.
  2. Cluster Headaches
    • Fioricet may be prescribed to alleviate pain during cluster headache episodes due to its sedative and muscle-relaxing properties. However, it is not a first-line treatment.
  3. Anxiety or Sleep Disorders
    • The butalbital component of Fioricet has sedative effects, so it is sometimes used to manage anxiety or as a short-term sleep aid.
    • This use is risky due to the potential for dependence.
  4. Neck and Muscle Tension
    • The muscle-relaxing properties of butalbital may help alleviate pain associated with neck stiffness or muscle tension.
  5. Post-Concussion Headaches
    • Fioricet is occasionally prescribed for headaches following a concussion or mild traumatic brain injury. However, its use in such cases is controversial due to the risk of side effects and overuse.
  6. Dental Pain or Post-Dental Surgery Pain
    • In rare cases, Fioricet might be prescribed for pain related to dental issues or recovery from dental procedures, especially if the pain includes a tension-like component.
  7. Chronic Daily Headaches
    • Some physicians prescribe Fioricet off-label for managing chronic daily headaches, though long-term use is discouraged because of the risk of dependency and rebound headaches.

Typical dosing for Fioricet

There are several manufacturers and brand names of this medication. The dose might differ slightly and each pill might contain different amounts of acetaminophen depending on which manufacturer and formulation of the medication you’re using.

Be sure to check your prescription for specific instructions. In general:

Fioricet and its generic: Each pill contains 50 mg of butalbital, 300 mg of acetaminophen, and 40 mg of caffeine.

  • Adults and children 12 years and older: The typical dose is 1 to 2 capsules by mouth every 4 hours as needed for pain. The maximum dose is 6 capsules in a 24-hour period.

Zebutal, Esgic, and generic tablets: Each pill contains 50 mg of butalbital, 325 mg of acetaminophen, and 40 mg of caffeine.

  • Adults and children 12 years and older: The typical dose is 1 to 2 capsules or tablets by mouth every 4 hours as needed for pain. Don’t take more than 6 pills in a 24-hour period.

Vtol LQ oral solution: Each tablespoonful (15 mL) contains 50 mg of butalbital, 325 mg of acetaminophen, and 40 mg of caffeine.

  • Adults and children 12 years and older: The typical dose is 15 mL (1 tablespoon) to 30 mL (2 tablespoons) by mouth every 4 hours. Don’t take more than 90 mL (6 tablespoons) in a 24-hour period.

What is gabapentin Neurontin approved for?

Gabapentin is used to:

  • Prevent and control partial seizures. Gabapentin can be used in adults and children age 3 and older who have partial seizures.
  • Relieve nerve pain following shingles in adults. Shingles is a painful rash that develops many years after you’ve had chickenpox. The virus that causes chickenpox stays dormant in a portion of your spinal nerve root called the dorsal root ganglion. For whatever reason, this otherwise dormant virus gets reactivated — usually by stress — causing a shingles rash. Nerve pain following a case of shingles is called postherpetic neuralgia (PHN).
  • Treat moderate-too-severe primary restless legs syndrome.

The branded gabapentin products Neurontin and Gralise are approved for partial seizures and PHN. The branded gabapentin enacarbil product Horizant is approved for restless legs syndrome and PHN.

Gabapentin capsules, tablets, and oral solution are used along with other medications to help control certain types of seizures in people who have epilepsy. Gabapentin capsules, tablets, and oral solution are also used to relieve the pain of postherpetic neuralgia (PHN; the burning, stabbing pain or aches that may last for months or years after an attack of shingles). Gabapentin extended-release tablets (Horizant) are used to treat restless legs syndrome (RLS; a condition that causes discomfort in the legs and a strong urge to move the legs, especially at night and when sitting or lying down).

Gabapentin is in a class of medications called anticonvulsants. Gabapentin treats seizures by decreasing abnormal excitement in the brain. Gabapentin relieves the pain of PHN by changing the way the body senses pain. It is not known exactly how gabapentin works to treat restless legs syndrome.

How should Gabapentin be used?

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 (https://www.fda.gov/Drugs) or the manufacturer’s website to obtain the Medication Guide.

What dosage strengths and forms does Gabapentin come in?

Capsules

100 mg
Each hard gelatin Coni-Snap capsule with white opaque body and cap printed with “PD” on one side and “Neurontin/100 mg” on the other contains 100 mg of gabapentin. Nonmedicinal ingredients: cornstarch, lactose, and talc; capsule shell: FD&C Blue No. 2, gelatin, red iron oxide, silicon dioxide, sodium lauryl sulfate, titanium dioxide, and yellow iron oxide.

300 mg
Each hard gelatin Coni-Snap capsule with yellow opaque body and cap printed with “PD” on one side and “Neurontin/300 mg” on the other contains 300 mg of gabapentin. Nonmedicinal ingredients: cornstarch, lactose, and talc; capsule shell: FD&C Blue No. 2, gelatin, red iron oxide, silicon dioxide, sodium lauryl sulfate, titanium dioxide, and yellow iron oxide.

400 mg
Each hard gelatin Coni-Snap capsule with orange opaque body and cap printed with “PD” on one side and “Neurontin/400 mg” on the other contains 400 mg of gabapentin. Nonmedicinal ingredients: cornstarch, lactose, and talc; capsule shell: FD&C Blue No. 2, gelatin, red iron oxide, silicon dioxide, sodium lauryl sulfate, titanium dioxide, and yellow iron oxide.

Tablets

600 mg
Each white, elliptical, film-coated tablet with “Neurontin 600” printed on one side contains 600 mg of gabapentin. Nonmedicinal ingredients: ammonium hydroxide, black iron oxide, candelilla wax, copolyvidone, cornstarch, hydroxypropyl cellulose, magnesium stearate, poloxamer 407 NF, and talc.

800 mg
Each white, elliptical, film-coated tablet with “Neurontin 800” printed on one side contains 800 mg of gabapentin. Nonmedicinal ingredients: candelilla wax, copolyvidone, cornstarch, hydroypropylcellulose, hypromellose, magnesium stearate, poloxamer 407 NF, red iron oxide, yellow iron oxide, and talc.

The Dosages of Off-Label Usages of Gabapentin

In case of emergency/overdose

In case of overdose, call the poison control helpline at 1-800-222-1222. Information is also available online at https://www.poisonhelp.org/help. If the victim has collapsed, had a seizure, has trouble breathing, or can’t be awakened, immediately call emergency services at 911.

Symptoms of overdose may include the following:

  • double vision
  • slurred speech
  • drowsiness
  • diarrhea

How should I take gabapentin?

  • Take Gralise tablets with your evening meal. Swallow tablets whole with a full glass of water. Don’t chew, break or crush.
  • Take Horizant tablets with food. Swallow tablets whole with a full glass of water. Don’t chew, break or crush.
  • Take other forms of gabapentin with or without food.
  • Neurontin and generic forms of Neurontin tablets may be broken into two pieces. You can take the second half for your next dose. Don’t use the half-tablet beyond 28 days after the whole tablet was cut or broken.
  • Carefully measure the liquid formulation of gabapentin using the measuring device that comes with the drug. If you did not receive a measuring device, please ask your pharmacist for a medication-measuring device.
  • If you take an aluminum or magnesium-containing antacid, such as Maalox®, Mylanta®, Gelusil®, Gaviscon®, or Di-Gel®, wait at least two hours before taking your next dose of gabapentin.
  • Take gabapentin exactly as prescribed by your healthcare provider.

Are there any serious interactions with gabapentin and other medications?

Serious breathing problems can happen if you take gabapentin with drugs that cause severe sleepiness or decreased awareness. Some examples include narcotic opioids, anti-anxiety medicines, antidepressants, and antihistamines. If you are 65 years of age or older and/or have a condition that affects your lungs, such as chronic obstructive pulmonary disease (COPD), there is an increased risk for breathing problems. Watch for increased sleepiness or decreased breathing when you start taking gabapentin or when the dose is increased. Get help right away if you develop breathing problems.

Seek immediate medical attention if these symptoms develop:

  • Confusion.
  • Unusual dizziness or lightheadedness.
  • Slowed, shallow or trouble breathing.
  • Unresponsiveness (can’t wake up).
  • Bluish-colored or tinted skin, especially on lips, fingers or toes.

What other medications and products can interact with gabapentin?

There may be an interaction between gabapentin and any of the following:

  • alcohol
  • antacids containing magnesium or aluminum
  • antihistamines (e.g., cetirizine, doxylamine, diphenhydramine, hydroxyzine, loratadine)
  • antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine, risperidone)
  • azelastine
  • benzodiazepines (e.g., alprazolam, diazepam, lorazepam)
  • brimonidine
  • buprenorphine
  • buspirone
  • butorphanol
  • calcium carbonate
  • cannabis
  • chloral hydrate
  • clonidine
  • entacapone
  • eszopiclone
  • general anesthetics (medications used to put people to sleep before surgery)
  • mefloquine
  • methadone
  • metoclopramide
  • mirtazapine
  • muscle relaxants (e.g., baclofen, cyclobenzaprine, methocarbamol, orphenadrine)
  • nabilone
  • narcotic pain relievers (e.g., codeine, hydrocodone,  morphine, oxycodone)
  • orlistat
  • pramipexole
  • ropinirole
  • rotigotine
  • scopolamine
  • other seizure medications (e.g., carbamazepine, clobazam, ethosuximide, levetiracetam, phenobarbital, phenytoin, primidone, topiramate, valproic acid, zonisamide)
  • tapentadol
  • thalidomide
  • tramadol
  • trazodone
  • tricyclic antidepressants (e.g., amitriptyline, imipramine)
  • zolpidem
  • zopiclone

Can I drink alcohol while taking gabapentin?

Avoid drinking alcohol while taking gabapentin. Drinking alcohol with gabapentin could increase sleepiness or dizziness.

What else do I need to know about gabapentin?

Never stop taking gabapentin without talking to your healthcare provider first. Stopping gabapentin suddenly can cause serious problems, including increasing your risk of seizures (if you are taking gabapentin to control seizures) or not improving your symptoms (if taking gabapentin for other indications). Also, never change your dose without talking to your provider first. Always take gabapentin exactly as prescribed.

Don’t drive, operate heavy machinery or do other dangerous activities after taking gabapentin until you know how it affects you.

Read the full prescription information leaflet that comes with your medication. Never hesitate to ask your healthcare provider or pharmacist if you have any questions about gabapentin.

Stop taking Neurontin and seek immediate medical attention if any of the following occur:

  • hallucinations (seeing or hearing things that aren’t there)
  • loss of consciousness
  • signs of a serious allergic reaction (e.g., swelling of face or throat, hives, or difficulty breathing)
  • signs of a severe skin reaction such as blistering, peeling, a rash covering a large area of the body, a rash that spreads quickly, or a rash combined with fever or discomfort
  • slow, shallow, or weak breathing
  • thoughts of hurting yourself or others
  • worsening seizures

Can I take gabapentin if I’m pregnant or thinking of becoming pregnant?

It’s unknown if gabapentin can harm your unborn baby. For this reason, talk to your healthcare provider as soon as you know you are pregnant. You and your healthcare provider will determine if you should take gabapentin during your pregnancy or change to a different medication.

Does gabapentin pass into breast milk?

Yes, gabapentin does pass into breast milk. If you are breastfeeding or planning to breastfeed, talk with your healthcare provider about breastfeeding or medication options.

Is gabapentin a narcotic or controlled substance?

Gabapentin is not a narcotic. It’s not classified as a controlled substance in most states. (Kentucky, West Virginia, Michigan, Tennessee, and Virginia have reclassified gabapentin as a Schedule V controlled substance). Gabapentin is not an opioid.

Is gabapentin addictive?

Gabapentin is not addictive, but this doesn’t mean that gabapentin can’t be abused. A small number of studies have reported misuse and abuse of gabapentin.

Does gabapentin cause withdrawal symptoms?

Gabapentin withdrawal symptoms have been reported since the drug was approved. However, the individuals in these reports experienced symptoms after discontinuing higher-than-recommended doses of gabapentin and for uses for which the drug was not approved.

What’s known about gabapentin and overdose?

Overdoses on gabapentin have been reported. Individuals experienced double vision, slurred speech, drowsiness, diarrhea and sluggishness.