Mean effective dosage: 5 to 6 mg/day, in 3 or 4 divided doses some patients may require as much as 10 mg/day.Įxtended release: 0.5 to 1 mg once daily titrate dose every 3 to 4 days in increments ≤1 mg/day (range: 3 to 6 mg/day). Immediate release tablet, oral concentrate, orally-disintegrating tablet: Initial: 0.5 mg 3 times daily titrate dose every 3 to 4 days in increments ≤1 mg/day. Patients requiring doses >4 mg/day should be increased cautiously. Periodic reassessment and consideration of dosage reduction is recommended.Īnxiety disorders: Oral: Immediate release tablet, oral concentrate, orally-disintegrating tablet: Initial: 0.25 to 0.5 mg 3 times daily titrate dose every 3 to 4 days usual maximum: 4 mg/day. Note: Titrate dose gradually as needed and tolerated. Hypersensitivity to alprazolam or any component of the formulation (cross-sensitivity with other benzodiazepines may exist) acute narrow-angle glaucoma concurrent use with ketoconazole, itraconazole, or other potent CYP3A4 inhibitors.Ĭanadian labeling: Additional contraindications (not in US labeling): Myasthenia gravis severe hepatic insufficiency severe respiratory insufficiency sleep apnea. Panic disorder (extended-release tablets, oral solution, orally-disintegrating tablets, immediate-release tablets): Treatment of panic disorder, with or without agoraphobia Contraindications Use: Labeled IndicationsĪnxiety disorders (immediate release tablet, oral concentrate, orally-disintegrating tablets): Treatment of generalized anxiety disorder (GAD), short-term anxiety and anxiety association with depression Special Populations NoteĬigarette smoking: Concentrations may be reduced by up to 50% in smokers. Maximal concentrations and half-life are approximately 15% and 25% higher in Asians. Obesity: 21.8 hours (range: 9.9 to 40.4 hours)Įlderly: 16.3 hours (range: 9 to 26.9 hours) Protein BindingĨ0% primarily to albumin Use in Specific Populations Special Populations: Race Orally-disintegrating tablet: 1.5 to 2 hours occurs ~15 minutes earlier when administered with water increased to ~4 hours when administered with a high-fat meal Half-Life EliminationĪdults: Mean: 11.2 hours (Immediate release range: 6.3 to 26.9 hours Extended release range: 10.7 to 15.8 hours) Orally-disintegrating tablet: Mean: 12.5 hours (range: 7.9 to 19.2 hours)Īlcoholic liver disease: 19.7 hours (range: 5.8 to 65.3 hours) Urine (as unchanged drug and metabolites) Time to PeakĮxtended release: Adolescents and Adults: ~9 hours, relatively steady from 4 to 12 hours (Glue 2006) decreased by 1 hour when administered at bedtime (as compared to morning administration) decreased by 33% when administered with a high-fat meal increased by 33% when administered ≥1 hour after a high-fat meal Hepatic via CYP3A4 forms two active metabolites (4-hydroxyalprazolam and α-hydroxyalprazolam ) and an inactive metabolite benzophenone metabolite, however, the active metabolites are unlikely to contribute to much of the pharmacologic effects because of their low concentrations and lesser potencies. Immediate release: V d: 0.84 to 1.42 L/kg (Greenblatt 1993) Metabolism Readily absorbed Extended release: Slower relative to immediate release formulation resulting in a concentration that is maintained 5 to 11 hours after dosing rate increased following night time dosing (versus morning dosing) Distribution Pharmacokinetics/Pharmacodynamics Absorption Benzodiazepines do not bind to GABA-B receptors. Benzodiazepine receptors and effects appear to be linked to the GABA-A receptors. This shift in chloride ions results in hyperpolarization (a less excitable state) and stabilization. Enhancement of the inhibitory effect of GABA on neuronal excitability results by increased neuronal membrane permeability to chloride ions. Generic: 0.5 mg, 1 mg, 2 mg, 3 mg Pharmacology Mechanism of Actionīinds to stereospecific benzodiazepine receptors on the postsynaptic GABA neuron at several sites within the central nervous system, including the limbic system, reticular formation. Xanax: 1 mg ĪLPRAZolam XR: 1 mg ĪLPRAZolam XR: 2 mg ĪLPRAZolam XR: 3 mg Excipient information presented when available (limited, particularly for generics) consult specific product labeling.ĪLPRAZolam Intensol: 1 mg/mL (30 mL)
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