Carbamazepine

From WikiMD's Wellnesspedia

What is Carbamazepine?[edit | edit source]

  • Carbamazepine (Carbatrol; Epitol; Equetro; Tegretol;Tegretol-XR) is an anticonvulsant and specific analgesic used alone or in combination with other medications to control certain types of seizures in people with epilepsy.
  • It is also used to treat trigeminal neuralgia.
Carbamazepine
Carbamazepine 3D
Carbamazepine Structural Formulae


What are the uses of this medicine?[edit | edit source]

Carbamazepine (Carbatrol; Epitol; Equetro; Tegretol;Tegretol-XR) is used:

Epilepsy:

  • Partial seizures with complex symptomatology (psychomotor, temporal lobe).
  • Generalized tonic-clonic seizures (grand mal).
  • Mixed seizure patterns which include the above, or other partial or generalized seizures.

Trigeminal Neuralgia:

Limitations of Use:

  • This drug is not a simple analgesic and should not be used for the relief of trivial aches or pains.

How does this medicine work?[edit | edit source]

  • Carbamazepine (kar" ba maz' e peen) is an iminostilbene that is chemically related to tricyclic antidepressants and unrelated in structure to other anticonvulsants.
  • Carbamazepine suppresses spread of seizure activity by reduction in the post-tetanic potentiation of synaptic transmission.
  • Carbamazepine is chemically unrelated to other anticonvulsants or other drugs used to control the pain of trigeminal neuralgia.
  • The mechanism of action remains unknown.
  • The principal metabolite of carbamazepine, carbamazepine-10, 11-epoxide, has anticonvulsant activity as demonstrated in several in vivo animal models of seizures.

Who Should Not Use this medicine ?[edit | edit source]

This medicine cannot be used in patients:

What drug interactions can this medicine cause?[edit | edit source]

  • Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.

Be sure to mention any of the following:

  • nefazadone or certain non-nucleoside reverse transcriptase inhibitors (NNRTIs) such as delavirdine (Rescriptor)
  • acetazolamide (Diamox)
  • albendazole (Albenza)
  • alprazolam (Panax)
  • aminophylline
  • anticoagulants ('blood thinners') such as apixaban (Eliquis), dabigatran (Pradaxa), edoxaban (Savaysa), rivaroxaban (Xarelto), and warfarin (Coumadin, Jantoven)
  • antidepressants such as amitriptyline (Elavil), bupropion (Wellbutrin, Zyban), buspirone (BuSpar), citalopram (Celexa), clomipramine (Anafranil), desipramine (Norpramin), fluoxetine (Prozac, Sarafem), fluvoxamine (Luvox), mirtazapine (Remeron), nortriptyline (Pamelor)
  • antifungals such as fluconazole (Diflucan), itraconazole (Onmel, Sporanox), ketoconazole, and voriconazole (Vfend); aprepitant (Emend)
  • aripiprazole (Abilify)
  • buprenorphine (Butrans, Sublocade)
  • bupropion (Aplenzin, Wellbutrin, Zyban)
  • cimetidine (Tagamet)
  • ciprofloxacin
  • isplatin (Platinol)
  • corticosteroids such as dexamethasone and prednisolone (Prelone)
  • clarithromycin (Biaxin, in Prevpac)
  • clonazepam (Klonopin)
  • clozapine (Clozaril)
  • cyclophosphamide
  • cyclosporine (Gengraf, Neoral, Sandimmune)
  • dalfopristin and quinupristin (Synercid)
  • danazol (Danocrine)
  • dantrolene (Dantrium)
  • diltiazem (Cardizem, Diltzac, Tiazac, others)
  • diuretics (water pills)
  • doxorubicin (Adriamycin, Rubex)
  • doxycycline (Vibramycin)
  • erythromycin (E.E.S., E-Mycin, Erythrocin)
  • eslicarbazepine (Aptiom)
  • everolimus (Afinitor, Zortress)
  • felodipine (Plendil)
  • haloperidol (Haldol)
  • HIV protease inhibitors including atazanavir (Reyataz), indinavir (Crixivan), lopinavir (in Kaletra), nelfinavir (Viracept), ritonavir (Norvir, in Kaletra), and saquinavir (Fortovase, Invirase)
  • ibuprofen (Advil)
  • imatinib (Gleevec)
  • isoniazid (INH, Laniazid, in Rifater)
  • levothyroxine (Levoxyl, Synthroid)
  • lithium (Lithobid)
  • loratadine (Claritin)
  • lorazepam (Ativan)
  • loxapine (Adasuve)
  • certain medications to treat malaria such as chloroquine (Aralen) and mefloquine
  • medications for anxiety or mental illness
  • other medications for seizures such as ethosuximide (Zarontin), felbamate (Felbatol), fosphenytoin (Cerebyx)
  • lamotrigine (Lamictal), methsuximide (Celontin), oxcarbazepine (Trileptal), phenobarbital, phensuximide (Milontin) (not available in the US), phenytoin (Dilantin, Phenytek), primidone (Mysoline), tiagabine (Gabitril), topiramate (Topamax), and valproic acid (Depakene, Depakote)
  • lapatinib
  • methadone (Dolophine, Methadose)
  • midazolam
  • niacinamide (nicotinamide, Vitamin B3)
  • olanzapine
  • omeprazole
  • oxybutynin
  • propoxyphene (Darvon)
  • praziquantel (Biltricide)
  • quetiapine
  • quinine
  • rifampin (Rifadin, Rimactane)
  • risperidone
  • sedatives
  • sertraline (Zoloft)
  • sirolimus
  • sleeping pills
  • tacrolimus (Prograf)
  • tadalafil (Adcirca, Cialis)
  • temsirolimus (Torisel)
  • terfenadine (Seldane) (not available in the US)
  • theophylline (Theo-24, Theochron, others)
  • ticlopidine
  • tramadol (Ultram)
  • tranquilizers
  • trazodone
  • troleandomycin (TAO)
  • verapamil (Calan, Verelan)
  • zileuton (Zyflo)
  • ziprasidone (Geodon),
  • zonisamide (Zonegran)
  • acetaminophen (Tylenol)
  • Your doctor will probably tell you not take carbamazepine with these medications
  • Also, tell your doctor if you are taking a monoamine oxidase (MAO) inhibitor such as isocarboxazid (Marplan), linezolid (Zyvox), methylene blue, phenelzine (Nardil), selegiline (Eldepryl, Emsam, Zelapar), and tranylcypromine (Parnate), or if you have stopped taking an MAO inhibitor within the past 14 days.

Is this medicine FDA approved?[edit | edit source]

  • Carbamazepine was approved for use in epilepsy in the United States in 1968 and it is still in common use with more than 2 million prescriptions being written yearly.

How should this medicine be used?[edit | edit source]

Recommended dosage:

Epilepsy: Adults And Children Over 12 Years Of Age:

  • Initial: 200 mg b.i.d. Increase at weekly intervals by adding up to 200 mg/day using a t.i.d. or q.i.d. regimen until the optimal response is obtained.
  • Dosage generally should not exceed 1000 mg daily in children 12 to 15 years of age, and 1200 mg daily in patients above 15 years of age.
  • Doses up to 1600 mg daily have been used in adults in rare instances.
  • Maintenance: Adjust dosage to the minimum effective level, usually 800 to 1200 mg daily.

Children 6 to 12 years of age:

  • Initial: 100 mg b.i.d. Increase at weekly intervals by adding up to 100 mg/day using a t.i.d. or q.i.d. regimen until the optimal response is obtained.
  • Dosage generally should not exceed 1000 mg daily.
  • Maintenance: Adjust dosage to the minimum effective level, usually 400 to 800 mg daily.

Children Under 6 Years Of Age:

  • Initial: 10 to 20 mg/kg/day b.i.d. or t.i.d. Increase weekly to achieve optimal clinical response administered t.i.d. or q.i.d.
  • Maintenance: Ordinarily, optimal clinical response is achieved at daily doses below 35 mg/kg.

Trigeminal Neuralgia:

  • Initial: On the first day, 100 mg b.i.d., for a total daily dose of 200 mg.
  • This daily dose may be increased by up to 200 mg/day using increments of 100 mg every 12 hours for tablets, only as needed to achieve freedom from pain.
  • Do not exceed 1200 mg daily.
  • Maintenance:
  • Control of pain can be maintained in most patients with 400 to 800 mg daily.
  • However, some patients may be maintained on as little as 200 mg daily, while others may require as much as 1200 mg daily.

Administration:

  • Carbamazepine comes as a tablet, a chewable tablet, an extended-release (long-acting) tablet, an extended-release capsule, and as a suspension (liquid) to take by mouth.
  • The regular tablet, chewable tablet, and suspension are usually taken two to four times a day with meals.
  • The extended-release tablet (Tegretol XR) is usually taken twice a day with meals.
  • The extended-release capsule (Carbatrol, Equetro) is usually taken twice a day with or without meals.
  • To help you remember to take carbamazepine, take it at around the same times every day.
  • Swallow the extended-release tablets whole; do not split, chew, or crush them.
  • The extended-release capsules may be opened and the beads inside sprinkled over food, such as a teaspoon of applesauce or similar food.
  • Do not crush or chew the extended-release capsules or the beads inside them.
  • Shake the suspension well before each use to mix the medication evenly.
  • Your doctor will start you on a low dose of carbamazepine and gradually increase your dose.

What are the dosage forms and brand names of this medicine?[edit | edit source]

This medicine is available in fallowing doasage form:

  • As tablets of 200 mg

This medicine is available in fallowing brand namesː

  • Carbatrol; Epitol; Equetro; Tegretol;Tegretol-XR

What side effects can this medication cause?[edit | edit source]

The most common side effects of this medicine include:

Carbamazepine may cause serious side effects, including:

  • confusion
  • rash
  • fast, slow, or pounding heartbeat
  • yellowing of the skin or eyes
  • vision changes
  • fatigue
  • swelling of your face, eyes, eyelids, lips, or tongue
  • difficulty swallowing or breathing
  • headache, new or increased number of seizures, difficulty concentrating, confusion, weakness, or unsteadiness
  • severe rash
  • dark urine
  • pain on the right side of your stomach area
  • loss of appetite

What special precautions should I follow?[edit | edit source]

  • Carbamzepine may interact with some drugs. Therefore, patients should be advised to report to their doctors the use of any other prescription or non-prescription medications or herbal products.
  • Caution should be exercised if alcohol is taken in combination with carbamazepine therapy, due to a possible additive sedative effect.
  • Since dizziness and drowsiness may occur, patients should be cautioned about the hazards of operating machinery or automobiles or engaging in other potentially dangerous tasks.
  • Complete pretreatment blood counts, including platelets and possibly reticulocytes and serum iron, should be obtained as a baseline. If a patient in the course of treatment exhibits low or decreased white blood cell or platelet counts, the patient should be monitored closely. Discontinuation of the drug should be considered if any evidence of significant bone marrow depression develops.
  • Carbamazepine should be discontinued, based on clinical judgement, if indicated by newly occurring or worsening clinical or laboratory evidence of liver dysfunction or hepatic damage, or in the case of active liver disease.
  • Baseline and periodic eye examinations, including slit-lamp, funduscopy, and tonometry, are recommended since many phenothiazines and related drugs have been shown to cause eye changes.
  • Baseline and periodic complete urinalysis and BUN determinations are recommended for patients treated with this agent because of observed renal dysfunction.
  • Thyroid function tests have been reported to show decreased values with carbamazepine administered alone.
  • Hyponatremia has been reported in association with carbamazepine use, either alone or in combination with other drugs.
  • Interference with some pregnancy tests has been reported.
  • Carbamazepine should be used with caution in patients with a mixed seizure disorder that includes atypical absence seizures, since in these patients carbamazepine has been associated with increased frequency of generalized convulsions.
  • AV heart block, including second and third degree block, have been reported following, carbamazepine treatment. This occurred generally, but not solely, in patients with underling EKG abnormalities or risk factors for conduction disturbances.
  • Hepatic effects, ranging from slight elevations in liver enzymes to rare cases of hepatic failure have been reported.
  • Multi-organ hypersensitivity reactions occurring days to weeks or months after initiating treatment have been reported in rare cases. Discontinuation of carbamazepine should be considered if any evidence of hypersensitivity develops.
  • Hypersensitivity reactions to carbamazepine have been reported in patients who previously experienced this reaction to anticonvulsants including phenytoin and phenobarbital. A history of hypersensitivity reactions should be obtained for a patient and the immediate family members. If positive, caution should be used in prescribing carbamazepine.
  • Severe dermatologic reactions, including toxic epidermal necrolysis (Lyell’s syndrome) and Stevens-Johnson syndrome, have been reported with carbamazepine. These reactions have been extremely rare. However, a few fatalities have been reported.
  • The used of carbamazepine should be avoided in patients with a history of hepatic porphyria. Carbamazepine administration has also been demonstrated to increase porphyrin precursors in rodents, a presumed mechanism for the induction of acute attacks of porphyria.
  • As with all antiepileptic drugs, carbamazepine should be withdrawn gradually to minimize the potential of increased seizure frequency.
  • Carbamazepine can cause fetal harm when administered to a pregnant woman.
  • Carbamazepine and its epoxide metabolite are transferred to breast milk. Because of the potential for serious adverse reactions in nursing infants from carbamazepine, a decision should be made whether to discontinue nursing or to discontinue the drug.
  • Carbamazepine is a well established cause of clinically apparent liver injury which can be severe and even fatal.
  • If you are having surgery, including dental surgery, tell the doctor or dentist that you are taking carbamazepine.
  • If you have fructose intolerance (an inherited condition in which the body lacks the protein needed to break down fructose [a fruit sugar found in certain sweeteners such as sorbitol]), you should know that the oral suspension is sweetened with sorbitol. Tell your doctor if you have fructose intolerance.

What to do in case of emergency/overdose?[edit | edit source]

Symptoms of overdosage may include:

Management of overdosage: In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

  • Overdose related information is also available online at poisonhelp.org/help.
  • In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
  • There is no specific antidote.
  • Elimination Of The Drug: Induction of vomiting.
  • Gastric lavage. Even when more than 4 hours have elapsed following ingestion of the drug, the stomach should be repeatedly irrigated, especially if the patient has also consumed alcohol.
  • Measures To Reduce Absorption: Activated charcoal, laxatives.
  • Measures To Accelerate Elimination: Forced diuresis.
  • Dialysis is indicated only in severe poisoning associated with renal failure. Replacement transfusion is indicated in severe poisoning in small children.
  • Respiratory Depression: Keep the airways free; resort, if necessary, to endotracheal intubation, artificial respiration, and administration of oxygen.
  • Hypotension, Shock: Keep the patient’s legs raised and administer a plasma expander. If blood pressure fails to rise despite measures taken to increase plasma volume, use of vasoactive substances should be considered.
  • Convulsions: Diazepam or barbiturates.
  • Respiration, cardiac function (ECG monitoring), blood pressure, body temperature, pupillary reflexes, and kidney and bladder function should be monitored for several days.
  • If evidence of significant bone marrow depression develops, the following recommendations are suggested:

(1) stop the drug, (2) perform daily CBC, platelet, and reticulocyte counts, (3) do a bone marrow aspiration and trephine biopsy immediately and repeat with sufficient frequency to monitor recovery.


Can this medicine be used in pregnancy?[edit | edit source]

  • Pregnancy Category D.
  • Carbamazepine can cause fetal harm when administered to a pregnant woman.


Can this medicine be used in children?[edit | edit source]

  • The safety of carbamazepine in children has been systematically studied up to 6 months.

What are the active and inactive ingredients in this medicine?[edit | edit source]

Active ingredients:

  • CARBAMAZEPINE

Inactive ingredients:

  • LACTOSE MONOHYDRATE
  • CELLULOSE, MICROCRYSTALLINE
  • HYPROMELLOSE
  • ETHYLCELLULOSE
  • CROSCARMELLOSE SODIUM
  • MAGNESIUM STEARATE

Who manufactures and distributes this medicine?[edit | edit source]

Manufactured by:

  • Taro HAWTHORNE, NY or Apotex Indianapolis, IN

What should I know about storage and disposal of this medication?[edit | edit source]

  • Store at controlled room temperature 15°-30°C (59°-86°F) (see USP).
  • Store in a dry place.
  • Protect from moisture.


Carbamazepine Resources

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