Alprazolam: Comprehensive Guide
Drug Name
Generic Name
Alprazolam
Brand Name(s)
Pakistan: Xanax, Alprax, Algan
India: Trika, Alzolam, Alprax
US: Xanax, Niravam
UK: Xanax (Note: Alprazolam is not widely available in the UK and is prescribed under strict regulations)
Pharmacological Class
Class
Anxiolytic
Subclass
Benzodiazepine
Mechanism of Action
Alprazolam enhances the effects of gamma-aminobutyric acid (GABA), a neurotransmitter that inhibits activity in the brain, producing a calming effect. It binds to GABA-A receptors, increasing the affinity of GABA for these receptors and thereby enhancing its inhibitory effects.
Indications
Primary Indications
- Generalized Anxiety Disorder (GAD)
- Panic Disorder
- Anxiety associated with depression
Off-label Uses
- Insomnia
- Premenstrual Syndrome (PMS)
- Agoraphobia
Dosage and Administration
Standard Dosage
The initial dose for anxiety is typically 0.25 to 0.5 mg taken three times daily. The dose can be gradually increased based on patient response and tolerability, up to a maximum of 4 mg per day.
Route of Administration
Oral
Special Populations
Pediatric: Not recommended for use in children.
Geriatric: Lower doses may be required due to increased sensitivity and reduced hepatic function.
Pharmacokinetics
Absorption
Alprazolam is well absorbed with peak plasma concentrations occurring 1-2 hours after administration.
Distribution
Widely distributed, with about 80% of the drug bound to plasma proteins.
Metabolism
Primarily metabolized in the liver by CYP3A4 enzymes.
Excretion
Excreted mainly in urine as metabolites.
Half-life
Approximately 11.2 hours in healthy adults.
Contraindications
Alprazolam is contraindicated in patients with known hypersensitivity to the drug or other benzodiazepines. It should not be used in patients with acute narrow-angle glaucoma, or in those taking ketoconazole or itraconazole.
Warnings and Precautions
Alprazolam has a high potential for abuse and dependence. It should be used with caution in patients with a history of substance abuse. Sudden discontinuation can lead to withdrawal symptoms. Caution is also advised in patients with respiratory disorders, liver impairment, or depression.
Side Effects
Common Side Effects
- Drowsiness
- Dizziness
- Fatigue
- Dry mouth
- Constipation
- Increased appetite
Serious Side Effects
- Severe allergic reactions
- Seizures
- Jaundice
- Depression
- Suicidal thoughts or behaviors
Drug Interactions
Major Interactions
- Ketoconazole
- Itraconazole
- Other benzodiazepines
Moderate Interactions
- Opioid analgesics
- Barbiturates
- Antidepressants
Minor Interactions
- Antacids
- Oral contraceptives
Pregnancy and Lactation
Pregnancy Category
Category D: There is positive evidence of human fetal risk, but potential benefits may warrant use of the drug in pregnant women despite potential risks.
Breastfeeding Considerations
Alprazolam is excreted in breast milk and may have adverse effects on the nursing infant. Breastfeeding is not recommended while using alprazolam.
Patient Counseling Information
Key Points for Patients
- Inform patients about the potential for dependence and abuse.
- Advise patients to avoid alcohol and other CNS depressants while taking alprazolam.
- Discuss the importance of adhering to the prescribed dosing regimen and not abruptly discontinuing the medication.