Antidote for Restyl/Alprazolam is: March 2010, March 2013
Ans. B: Flumazenil Pharmacokinetics of alprazolam Well absorbed (90%) from the GI tract; absorption is slower with extended-release tablets Widely distributed, crosses blood-brain barrier. Probably crosses the placenta and enters breast milk. Accumulation is minimal Metabolized by the liver (CYP3A4 enzyme system) to an active compound that is subsequently rapidly metabolized Half life is 12 hour Uses of alprazolam Treatment of Generalized Anxiety Disorder (GAD) Panic Disorder Management of anxiety associated with depression Management of symptoms of premenstrual syndrome (PMS) Insomnia, irritable bowel syndrome (IBS) and other somatic symptoms associated with anxiety Used as an adjunct with acute mania, acute psychosis. Actions Acts at many levels in the CNS to produce anxiolytic effect May produce CNS depression Effects may be mediated by GABA, an inhibitory neurotransmitter. Contra-indicated in Hypersensitivity Cross-sensitivity with other benzodiazepines may exist Pre-existing CNS depression Severe uncontrolled pain Angle-closure glaucoma, obstructive sleep apnea, pulmonary disease Pregnancy and lactation Concurrent itraconazole or ketoconazole. Lactation: Use in pregnancy or lactation may cause CNS depression, flaccidity, feeding difficulties, and seizures in infant Use cautiously in Renal 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. Interactions Alcohol, antidepressants, other benzodiazepines, antihistamines and opioid analgesics -concurrent use results in CNS depression Hormonal 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 overdosage Flumazenil 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