Īlprazolam is affected by drugs that inhibit or induce CYP3A4. Using alprazolam with CNS depressants, especially opioids, increases the risk of respiratory depression, low blood pressure, and death. Alprazolam should be avoided if possible by anyone with pulmonary disease. Ĭontraindications to alprazolam include patients with known alprazolam or benzodiazepine hypersensitivity or known allergies to any of its components in the drug dosage form. Since there is a potential for serious adverse reactions for breastfed neonates and infants, lactating women are advised against breastfeeding if treated with alprazolam. The effects of alprazolam on milk production and lactation are unknown. Sedation and withdrawal symptoms are reported in breastfed neonates/infants exposed to alprazolam via breastmilk. Limited reports from published literature show the presence of alprazolam in human breast milk. Available data of published observational studies of pregnant women exposed to alprazolam have not related alprazolam-associated risk of miscarriage, major congenital disabilities, or adverse maternal or fetal outcomes. As benzodiazepines can cross the placenta, clinicians should observe newborns for signs/symptoms of sedation, respiratory depression, feeding problems, and neonatal withdrawal syndrome and manage them appropriately. Maternal exposure to alprazolam in the later trimester of pregnancy may result in sedation (lethargy, respiratory depression, hypotonia) and withdrawal symptoms (irritability, hyperreflexia, restlessness, tremors, feeding difficulties, and inconsolable crying, and) in the neonate. Clinicians are encouraged to register their patients by calling the National Pregnancy Registry for Psychiatric Medications. A pregnancy exposure registry is established to monitor pregnancy outcomes in women exposed to alprazolam when pregnant. Īlprazolam is categorized as pregnancy category D medicine. In patients with long-term chronic alprazolam use, one should switch to a longer-acting benzodiazepine such as clonazepam or diazepam and titrate down gradually this results in fewer withdrawal side effects. The suggested method is that the daily dosage reduction is not more than 0.5 mg every three days, and some patients may require an even slower dosage reduction. The dosage should be gradually reduced in all patients when discontinuing therapy or decreasing the daily dosage. Oral dosage forms (extended-release tablets): 0.5 mg orally once a dayĪs a result of the danger of withdrawal, avoid abrupt discontinuation of treatment. Oral dosage forms (immediate-release tablets/orally disintegrating tablets): 0.25 mg orally two or three times daily The safety and effectiveness of alprazolam are not being established in pediatric patients. The mean plasma half-life of alprazolam is about 11.2 hours in healthy adults. The bioavailability of oral alprazolam averages 80 to 100%.Īlprazolam is 80% bound to serum protein, mainly albumin.Īlprazolam is metabolized in the liver by cytochrome P450 3A4 (CYP3A4) to 4-hydroxyalprazolam and alpha-hydroxyalprazolam metabolites.Īlprazolam and its metabolites are filtered out by the kidneys and excreted in the urine. Īlprazolam is rapidly absorbed after oral administration with a peak plasma concentration at 1 to 2 hours. When bound to the GABA-A receptor, the major inhibitory neurotransmitter GABA mediates the calming or inhibitory effects of alprazolam on the human nervous system. Benzodiazepine binding sites appear to exhibit coupling with GABA-A receptors, enhancing the effects of gamma-aminobutyric acid (GABA) by increasing GABA affinity at the GABA-A receptor. Also, research suggests that BNZ-1 receptors affect sedation and anti-anxiety, while the BNZ-2 affects muscle relaxation, anticonvulsant activity, memory, and motor coordination. ![]() ![]() Studies in mice suggest that the alpha-1 subunit mediates sedation, amnesia, and ataxic effects of benzodiazepines, and alpha-2 and alpha-3 subunits mediate anxiolytic and muscle-relaxing effects of benzodiazepines. The benzodiazepine binding site is between the alpha-1 and gamma-2 subunits. A common GABA-A receptor in the CNS is comprised of two alpha-1 subunits, two beta-2 subunits, and one gamma-2 subunit. This receptor is comprised of five subunits, e.g., alpha, beta, gamma, delta, epsilon, rho, etc. Benzodiazepines bind to the GABA-A receptor. Alprazolam belongs to a class of psychoactive medications called benzodiazepines.
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