about Carbamazepine class, uses, side effects contraindications
Carbamazepine
Short Description
Carbamazepine belongs to a class of medications called anticonvulsants, and it works by decreasing abnormal electrical activity in the brain.
Category
Chemical class: Tricyclic iminostilbene derivative
Therapeutic class: Analgesic, anticonvulsant
Pregnancy category: C
Indications
To treat epilepsy (CARBATROL), (TEGRETOL-XR) Adults and children age 12 and over. Initial: 200 mg b.i.d. Increased weekly by 200 mg daily, if needed. Maximum: 1,600 mg daily in adults, 1,200 mg daily in children age 16 and over, and 1,000 mg daily in children ages 12 to 16. Children ages 6 to 12. Initial: 100 mg b.i.d. Increased weekly by 100 mg daily, if needed. Maximum: 1,000 mg daily. ORAL SUSPENSION Adults and children age 12 and over. Initial: 100 mg q.i.d. Increased weekly by 200 mg daily, if needed, given in divided doses t.i.d or q.i.d. Maximum: 1,600 mg daily in adults, 1,200 mg daily in children age 16 and over, and 1,000 mg daily in children ages 12 to 16. Children ages 6 to 12. Initial: 50 mg q.i.d. Increased weekly by 100 mg daily, if needed, given in divided doses t.i.d or q.i.d. Maximum: 1,000 mg daily. Children up to age 6. Initial: 10 to 20 mg/ carbamazepine 174 kg/day in divided doses q.i.d. Maximum: 35 mg/kg daily. Adults and children age 12 and over. Initial: 200 mg b.i.d. Increased weekly by 200 mg/day, if needed, given in divided doses t.i.d. or q.i.d. Maximum: 1,600 mg daily in adults, 1,200 mg daily in children age 16 and over, and 1,000 mg daily in children ages 12 to 16. Children ages 6 to 12. Initial: 100 mg b.i.d. Increased weekly by 100 mg daily, if needed, given in divided doses t.i.d. or q.i.d. Maximum: 1,000 mg daily. Children up to age 6. Initial: 10 to 20 mg/ kg daily in divided doses b.i.d. or t.i.d. Increased weekly, if needed, divided and given t.i.d. or q.i.d. Maximum: 35 mg/kg/day. To relieve pain in trigeminal neuralgia (CARBATROL), (TEGRETOL-XR),
Adults.Initial: 100 mg b.i.d. Increased by up to 200 mg daily, if needed, in increments of 100 mg every 12 hr. Maintenance: 400 to 800 mg/day. Maximum: 1,200 mg daily. ORAL SUSPENSION(100 MG/5 ML)
Adults.50 mg q.i.d. Increased by up to 200 mg daily, if needed, in increments of 50 mg q.i.d. Maintenance: 400 to 800 mg daily. Maximum: 1,200 mg daily. To treat acute manic and mixed episodes in bipolar disorder (EQUETRO)
Adults. Initial: 200 mg b.i.d., increased as needed in 200-mg increments. Maximum: 1,600 mg daily.
Contraindications
History of bone marrow depression; hypersensitivity to carbamazepine, tricyclic compounds, or their components; MAO inhibitor or nefazodone therapy Route Onset Peak Duration P.O. (all In 1 mo* Unknown Unknown forms)
Interactions
acetaminophen (long-term use): Increased metabolism, leading to acetaminopheninduced hepatotoxicity or decreased acetaminophen effectiveness acetazolamide, cimetidine, clarithromycin, danazol, diltiazem, erythromycin, fluconazole, fluoxetine, fluvoxamine, isoniazid, itraconazole, ketoconazole, loratadine, niacinamide, nicotinamide, propoxyphene, protease inhibitors, terfenadine, troleandomycin, valproate, verapamil: Increased blood carbamazepine level alprazolam, amitriptyline, bupropion, buspirone, citalopram, clobazam, clonazepam, clozapine, cyclosporine, delavirdine, desipramine, diazepam, dicumarol, doxycycline, ethosuximide, felodipine, glucocorticoids, haloperidol, itraconazole, lamotrigine, levothyroxine, lorazepam, methadone, methsuximide, midazolam, mirtazapine, nortriptyline, olanzapine, oral contraceptives, oxcarbazepine, phenytoin, praziquantel, protease inhibitors, quetiapine, risperidone, theophylline, tiagabine, topiramate, tramadol, triazolam, trazodone, valproate, warfarin, carbamazepine 175 C
Mechanism of Action
Normally, sodium moves into a neuronal cell by passing through a gated sodium channel in the cell membrane. Carbamazepine may prevent or halt seizures by closing or blocking sodium channels, as shown below, thus preventing sodium from entering the cell. Keeping sodium out of the cell may slow nerve impulse transmission, thus slowing the rate at which neurons fire. * For anticonvulsant use; 8 to 72 hr for use in trigeminal neuralgia. Cell exterior Sodium Open sodium channel Closed sodium channel Carbamazepine Neuronal cell membrane Cell interior ziprasidone, zonisamide: Decreased blood levels of these cisplatin, doxorubicin, felbamate, methsuximide, phenytoin, rifampin,
theophylline: Decreased blood carbamazepine level clomipramine, phenytoin, primidone: Increased blood levels of these felbamate: Decreased blood level of felbamate or carbamazepine isoniazid: Increased risk of carbamazepine toxicity and isoniazid hepatotoxicity lamotrigine, phenobarbital, primidone, tricyclic antidepressants,
valproic acid: Decreased blood levels of these , increased blood level of carbamazepine lithium: Increased risk of CNS toxicity nefazodone: Decreased nefazodone effectiveness and increased carbamazepine level nondepolarizing neuromuscular blockers: Possibly reduced duration or decreased effectiveness of neuromuscular blocker oral anticoagulants: Increased metabolism and decreased effectiveness of anticoagulant grapefruit juice: Increased blood carbamazepine level
alcohol use: Increased sedative effect
Side Efect
CNS: Chills, confusion, dizziness, drowsiness, fatigue, fever, headache, suicidal ideation, syncope, talkativeness, unsteadiness, visual hallucinations
CV: Arrhythmias, including AV block; edema; heart failure; hypertension; hypotension; thromboembolism; thrombophlebitis; worsened coronary artery disease
EENT: Blurred vision, conjunctivitis, dry mouth, glossitis, nystagmus, oculomotor disturbances, stomatitis, tinnitus, transient diplopia
ENDO: Syndrome of inappropriate ADH secretion, water intoxication
GI: Abdominal pain, anorexia, constipation, diarrhea, dyspepsia, elevated liver function test results, hepatitis, nausea, pancreatitis, vomiting
GU: Acute urine retention, albuminuria, azotemia, glycosuria, impotence, oliguria, renal failure, urinary frequency HEME:Acute intermittent porphyria, agranulocytosis, aplastic anemia, bone marrow depression, eosinophilia, leukocytosis, leukopenia, pancytopenia, thrombocytopenia
MS: Arthralgia, leg cramps, myalgia
RESP: Pulmonary hypersensitivity (dyspnea, fever, pneumonia, or pneumonitis)
SKIN: Aggravation of disseminated lupus erythematosus, alopecia, altered skin pigmentation, diaphoresis, erythema multiforme, erythema nodosum, exfoliative dermatitis, jaundice, Lyell’s syndrome, photosensitivity reactions, pruritic and erythematous rash, purpura, Stevens-Johnson syndrome, urticaria
Other: Adenopathy, lymphadenopathy
Cautions
Avoid using carbamazepine in patients with a history of hepatic porphyria because it may prompt an acute attack.
WARNING If patient has Asian ancestry, make sure he has been evaluated for the genetic allelic variant HLA-B 1502 before starting carbamazepine therapy. Patients positive for HLA-B 1502 shouldn’t take carbamazepine because the risk of serious, sometimes fatal, dermatologic reactions is ten times higher than in patients without this variant. Use carbamazepine cautiously in patients with impaired hepatic function because it’s mainly metabolized in the liver. Monitor liver function tests, as directed. Monitor patient closely for adverse reactions because many are serious. Periodically monitor blood carbamazepine level to assess for therapeutic and toxic levels; a blood level of 6 to 12 mcg/ml is optimal for anticonvulsant effects.
WARNING Monitor WBC and platelet counts monthly for first 2 months. Decreased counts may indicate bone marrow depression. Monitor patient closely for evidence of suicidal thinking or behavior, especially when therapy starts or dosage changes. Withdraw carbamazepine gradually to minimize risk of seizures. PATIENT SAFTY
Tell patient to take carbamazepine with food (except the oral suspension form, which shouldn’t be taken with other liquid or diluents). Warn patient about possible dizziness, blurred vision, and unsteadiness. Inform patient that coating of tablets isn’t absorbed and may appear in stool. carbamazepine 176 Advise patient not to crush or chew capsules or tablets. If he can’t swallow capsules whole, have him open them and sprinkle contents on food. Urge patient to wear sunscreen and protective clothing to reduce photosensitivity. Tell patient to report unusual bleeding or bruising, fever, rash, or mouth ulcers. Tell woman that drug decreases oral contraceptive effectiveness, and urge her to use different contraception. Because drug may cause fetal harm, tell her to notify prescriber about possible pregnancy. If she becomes pregnant during therapy, urge her to enroll in the antiepileptic drug pregnancy registry by calling 1-888-2332334. Explain that the registry is collecting information about the safety of antiepileptic during pregnancy. Instruct caregivers to watch patient closely for evidence of suicidal tendencies, especially when therapy starts or dosage changes, and to report such tendencies to prescriber immediately.
Trade Name & Company Name
effect of Carbamazepine in Pregnancy, Fetal Health
and Breast feeding
Pregnancy
. Anticonvulsant drugs should not be discontinued abruptly during Pregnancy
if used to prevent seizures, as there is a significant possibility of precipitating status epilepticus. There are no adequate reports or well-controlled studies of carbamazepine in pregnant women. It would seem advisable for women to continue medication during Pregnancy
using monotherapy at the lowest dose required to achieve seizure control. Polytherapy would seem best avoided where possible. Fetal Health
There are no adequate reports or well-controlled studies in human fetuses. Carbamazepine rapidly crosses the human placenta and accumulates in fetal organs, including the brain. Epidemiologic study suggests carbamazepine is a teratogen causing facial dysmorphism, spina bifida, distal phalange hypoplasia, and developmental delay. In prospective studies involving 1255 exposures, carbamazepine was associated with increased rates of neural tube, CV, urinary tract, and cleft palate anomalies. One overview (Cochrane) concluded the evidence is weak that carbamazepine is a teratogen as monotherapy. More recent epidemiologic evidence, however, concludes carbamazepine is a modest teratogen?less than phenytoin, but more than other anticonvulsant agents. The combination of carbamazepine with other antiepileptic drugs has a synergistic effect on the prevalence of birth defects. There is also concern that carbamazepine exposure increases the risk of neonatal intracranial hemorrhage. Rodent studies reveal an increased prevalence of talipes, cleft palate, and anophthalmos. Breastfeeding
Carbamazepine is excreted in human breast milk. Although it is generally considered safe for Breastfeeding women, neonatal sequelae reported include cholestatic hepatitis. The infant should 133 be monitored for possible adverse effects, the drug given at the lowest effective dose, and
the follwing drugs will increse Carbamazepine by inhepiting cyp450
amiodarone ; aprepitant ; atomoxetine ; boceprevir ; ceritinib ; chloramphenicol ; cimetidine ; ciprofloxacin ; clarithromycin ; crizotinib ; delaviridine ; diethyl-dithiocarbamate ; diltiazem ; entrectinib ; erythromycin ; esomeprazole ; fluconazole ; fluvoxamine ; gestodene ; grapefruit juice ; idelalisib ; imatinib ; indinavir ; itraconazole ; ivacaftor ; ketoconazole ; lesinurad ; letermovir ; mibefradil ; mifepristone ; nefazodone ; nelfinavir ; netupitant/palonosetron ; norfloxacin ; norfluoxetine ; omeprazole ; pantoprazole ; perampanel ; quercetin ; regorafenib ; ribociclib ; ritonavir ; rucaparib ; saquinavir ; simeprevir ; starfruit ; telaprevir ; telithromycin ; ticagrelor ; tucatinib ; verapamil ; voriconazole ;
the follwing drugs will decrease Carbamazepine by inhancing cyp450
barbiturates ; brigatinib ; carbamazepine ; clobazam ; dabrafenib ; efavirenz ; elagolix ; enzalutamide ; eslicarbazepine ; glucocorticoids ; letermovir ; lorlatinib ; modafinil ; nevirapine ; oxcarbazepine ; perampanel ; phenobarbital ; phenytoin ; pioglitazone ; rifabutin ; rifampin ; St. John's Wort ; telotristat ; troglitazone ; vemurafenib ;
trad drugs based on Carbamazepine
| Gen name | Trade name | Catagory name |
| carbamazepine | Carbatrol | Dibenzazepine anticonvulsants |
| carbamazepine | Carnexiv | Dibenzazepine anticonvulsants |
| carbamazepine | Epitol | Dibenzazepine anticonvulsants |
| carbamazepine | Equetro | Dibenzazepine anticonvulsants |
| carbamazepine | Tegretol | Dibenzazepine anticonvulsants |
| carbamazepine | Tegretol XR | Dibenzazepine anticonvulsants |
| Carbamazepine | CARBATOL 200MG TAB | |
| Carbamazepine | EPTOL 100MG-5ML ORAL SUSPENSION | |
| Carbamazepine | EPTOL 200 MG TAB | |
| Carbamazepine | FITZCALM 200MG TAB | |
| Carbamazepine | FITZECALM 100MG/5ML SUSP | |
| Carbamazepine | TEGRETOL 100 CHEW.TAB | |
| Carbamazepine | TEGRETOL 250 MG SUPPOSITORIES | |
| Carbamazepine | TEGRETOL SUSP 2% | |
| Carbamazepine | TEGRETOL TAB 200MG | |
other drugs from same cataogory