Antidote for Restyl/Alprazolam is:March 2010, March 2013
Ans. B: FlumazenilPharmacokinetics of alprazolamWell absorbed (90%) from the GI tract; absorption is slower with extended-release tabletsWidely distributed, crosses blood-brain barrier. Probably crosses the placenta and enters breast milk. Accumulation is minimalMetabolized by the liver (CYP3A4 enzyme system) to an active compound that is subsequently rapidly metabolizedHalf life is 12 hourUses of alprazolamTreatment of Generalized Anxiety Disorder (GAD)Panic DisorderManagement of anxiety associated with depressionManagement of symptoms of premenstrual syndrome (PMS)Insomnia, irritable bowel syndrome (IBS) and other somatic symptoms associated with anxietyUsed as an adjunct with acute mania, acute psychosis.ActionsActs at many levels in the CNS to produce anxiolytic effectMay produce CNS depressionEffects may be mediated by GABA, an inhibitory neurotransmitter.Contra-indicated inHypersensitivityCross-sensitivity with other benzodiazepines may existPre-existing CNS depressionSevere uncontrolled painAngle-closure glaucoma, obstructive sleep apnea, pulmonary diseasePregnancy and lactationConcurrent itraconazole or ketoconazole.Lactation: Use in pregnancy or lactation may cause CNS depression, flaccidity, feeding difficulties, and seizures in infantUse cautiously inRenal Impairment, Hepatic dysfunction.Concurrent use with nefazodone, fluvoxamine, cimetidine, fluoxetine, hormonal contraceptives, propoxyphene, diltiazem, isoniazid, erythromycin, clarithromycin, grapefruit juice.History of suicide attempt or alcohol/drug dependence, debilitated patients.Pediatric age: Safety and efficacy not established. Decreased dosage and frequent monitoring required.Geriatric age: Elderly patients have increased sensitivity to benzodiazepines. Appears on Beers list and is associated with increased risk of falls and excessive CNS effects.InteractionsAlcohol, antidepressants, other benzodiazepines, antihistamines and opioid analgesics -concurrent use results in CNS depressionHormonal contraceptives, disulfiram, fluoxetine, isoniazid, metoprolol, propoxyphene, propranolol and valproic acid metabolism of alprazolam, blood levels and its actions (dose adjustments may be necessary)CYP3A4 inducers (rifampin, carbamazepine, or barbiturates)CYP3A4 inhibitors (erythromycin, ketoconazole, itraconazole, fluvoxamine, cimetidine, nefazodone)Toxicity and overdosageFlumazenil is the antidote for alprazolam toxicity or overdose. (Flumazenil may induce seizures in patients with a history of seizures disorder or who are on tricyclic antidepressants.)
Protamine sulphate
Flumazenil
EDTA
BAL