alprazolam XANAX
Class: Benzodiazepine/TriazoloFDA Indications: Panic Disorder, Anxiety Disorders
Off-Label Use: Insomnia, Alcohol Withdrawal, Preanesthetic, PMDD, Depression
Prescribing
FDA Schedule IVForms: 0.25, 0.5, 1, 2mg tablet
Dose Range: 0.25-10 mg/day
Starting: 0.25-0.5 mg tid; titrate dose q3-4 days; Patients requiring doses >4 mg/day should be increased cautiously.
Stopping: Abrupt discontinuation should be avoided. Daily dose may be decreased by 0.5 mg q3 days; however, some patients may require a slower reduction.
Precautions
Contraindications: Acute narrow angle glaucoma, sleep apneaSerious Side Effects: Overdose can result in hypotension, respiratory depression, and coma
Side Effects: constipation, dysarthria, sedation/somnolence, dizziness, confusion, disequilibrium, ataxia, lightheadedness, weakness/asthenia, decreased libido, increased appetite, weight gain
Pharmacokinetics
t½: 12 (9-20)° TMAX: 1-2°Absorption Rate: Medium
Lipid Solubility: Moderate
Substrate of: 3A4; 1A2
Inhibits: ∅ ; Induces: ∅
Active Metabolites: ∅
DDIs
- - CNS depression with combined use of opioids
- - 3A4 inhibitors can ↑ levels; likewise, 3A4 inducers can ↓ levels
Misc
- - ↑ stage 2 and ↓ stages 1, 4 and REM sleep
- - low degree of sedation
- - withdrawal sx may be especially severe
- - antidpressant effect
Special Populations
Category D—↑ risk of oral cleft by 0.01%, use just before delivery associated with floppy infant syndrome, 3rd trimester use can cause withdrawal in newborns
Low incidence of infant toxicity and AEs associated with benzodiazepine use during breastfeeding. Benzodiazepines with shorter half-lives (i.e., lorazepam, alprazolam, and oxazepam) have been found to be very low in breast milk
T½ ↑ ≈ 45%; initiate at 0.25 mg bid-tid
2019 BEE℞S Recommendation: Avoid. Older adults have increased sensitivity to benzodiazepines and decreased metabolism of long- acting agents; in general, all benzodiazepines increase risk of cognitive impairment, delirium, falls, fractures, and motor vehicle crashes in older adults. May be appropriate for seizure disorders, RBD, benzodiazepine withdrawal, EtOH withdrawal, severe GAD, and periprocedural anesthesia.
Renal insufficiency has a quantitatively small influence on pharmacokinetics; no dosage adjustments provided in the manufacturer's labeling
T½ ↑ ≈ 73% in patients with alcohol liver disease
References
Use Of Psychiatric Medications During Pregnancy And LactationXanax Package Insert
Goodman & Gilman's The Pharmacological Basis Of Therapeutics, Ch 5.
Alprazolam Kinetics In Patients With Renal Insufficiency.
An Updated Unified Pharmacophore Model Of The Benzodiazepine Binding Site On GABAAR
UpToDate
Neonatal Benzodiazepines Exposure During Breastfeeding