Pharmacology · Benzodiazepines
Alprazolam !
A triazolobenzodiazepine used for panic disorder and anxiety. Anxiety between doses, dependence and withdrawal are particular concerns.
Updated 2026-11-01
The figure shows alprazolam itself bound to the human GABA-A receptor (α1β3γ2L) with GABA.
Mechanism of action
Alprazolam binds the benzodiazepine site of the GABA-A receptor and makes GABA open the chloride channel more often, reducing anxiety and panic attacks. CYP3A4 breaks it down, so strong CYP3A inhibitors raise its levels sharply.
- Binds the benzodiazepine site of the GABA-A receptor
- GABA opens the chloride channel more often
- Fear circuits are damped: fewer panic attacks
Pharmacokinetics
- Absorption
- Peak about 1 to 2 hours after a dose by mouth
- Metabolism
- By CYP3A4 to 4-hydroxy- and alpha-hydroxyalprazolam
- Half-life
- About 11 hours on average, with wide variation
Indications
- Panic disorder, with or without agoraphobia Panic disorder →
- Generalized anxiety disorder (short-term) Generalized anxiety disorder →
Adverse effects
Common
- Drowsiness and light-headedness
- Poor coordination
- Memory problems
- Anxiety between doses or early in the morning in panic disorder
Contraindications
- Hypersensitivity to benzodiazepines
- Use with strong CYP3A inhibitors such as ketoconazole or itraconazole
Key interactions
- Opioids
- Profound sedation, respiratory depression, coma and death
- Alcohol and other central nervous system depressants
- Additive sedation and breathing depression
- Strong CYP3A inhibitors (ketoconazole, itraconazole)
- Much higher alprazolam levels: contraindicated
- CYP3A inducers (carbamazepine, phenytoin)
- Lower alprazolam levels
- Digoxin
- Digoxin levels may rise
What is monitored
- Sedation and breathing, especially with opioids
- Signs of misuse, dose escalation or early refills
- Withdrawal symptoms during tapering
Administration and safety
- Given by mouth; immediate- and extended-release tablets are not interchangeable
- Controlled medicine: stored securely and counted
- Tapered gradually when stopped
Nursing care
- Before each dose, check level of alertness, breathing rate and oxygen saturation
- Ask about opioids, alcohol and other sedatives
- Prevent falls, especially in older adults (unsteadiness, confusion)
- Teach not to drive or drink alcohol and not to stop the medicine suddenly
- Teach to avoid grapefruit and to report other new medicines (CYP3A)
Pregnancy and breastfeeding
Use late in pregnancy can cause sedation and withdrawal symptoms in the newborn, who is watched after birth.
Test yourself
Think of the answer, then tap the question to see it.
Which antifungals are contraindicated with alprazolam, and why?
Ketoconazole and itraconazole: they block CYP3A4 and raise alprazolam levels sharply.
What is interdose anxiety with alprazolam?
Early-morning or between-dose anxiety in panic disorder as levels fall.
What can a rapid dose reduction of alprazolam cause?
Withdrawal reactions, including seizures.
Related drugs
Related conditions
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Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: DailyMed - ALPRAZOLAM tablet (DailyMed (U.S. National Library of Medicine), 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026); 6HUO: CryoEM structure of human full-length heteromeric alpha1beta3gamma2L GABA(A)R in complex with alprazolam (Xanax), GABA and megabody Mb38. (RCSB Protein Data Bank, 2019).
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Representative model, for educational purposes only.