Alprax

• Generalized Anxiety Disorder (GAD): Treatment of symptoms of anxiety.
• Panic Disorder: With or without agoraphobia, to reduce frequency and severity of panic attacks.
• Anxiety associated with depression: Short-term management of anxiety symptoms occurring with depression.
• Off-label Uses: Occasionally used for situational anxiety and short-term insomnia related to anxiety.

• Adults:
• GAD: Start with 0.25 to 0.5 mg orally three times daily; may increase every 3 to 4 days as needed and tolerated; usual dose 1 to 4 mg/day in divided doses.
• Panic Disorder: Initial dose 0.5 mg orally three times daily; dose may be gradually increased every 3 to 4 days; usual dose range 3 to 6 mg/day.
• Elderly or debilitated patients:
• Start at 0.25 mg two or three times daily; titrate slowly to minimize sedation and cognitive impairment.
• Pediatrics: Safety and efficacy not established; use generally not recommended.
• Renal or Hepatic Impairment: Dose adjustment recommended; start at lower doses and titrate carefully.
• Route: Oral tablets or extended-release tablets; oral solution available.
• Duration: Typically short-term (2 to 4 weeks), with tapering to avoid withdrawal symptoms.

Alprazolam is a short-acting benzodiazepine that binds selectively to benzodiazepine receptors on the gamma-aminobutyric acid type A (GABA-A) receptor complex in the central nervous system. This binding enhances the affinity of GABA, the primary inhibitory neurotransmitter, resulting in increased frequency of chloride channel opening, neuronal hyperpolarization, and reduced neuronal excitability. These effects produce anxiolytic, sedative, muscle relaxant, and anticonvulsant properties, helping alleviate anxiety and panic symptoms.

• Absorption: Rapid and complete absorption after oral administration; peak plasma concentrations within 1 to 2 hours (immediate-release).
• Bioavailability: Approximately 80–90%.
• Distribution: Widely distributed throughout body tissues; crosses blood-brain barrier. Volume of distribution approx. 0.8–1.3 L/kg.
• Protein Binding: Approximately 80%.
• Metabolism: Hepatic metabolism mainly via CYP3A4 to active and inactive metabolites.
• Elimination Half-life: 11 to 16 hours in healthy adults; prolonged in elderly and hepatic impairment.
• Excretion: Primarily renal elimination of metabolites.

• Pregnancy: Category D — positive evidence of human fetal risk. Use during pregnancy is contraindicated unless benefits outweigh risks. Associated with risk of congenital malformations and neonatal withdrawal syndrome.
• Lactation: Alprazolam is excreted into breast milk and may cause sedation or feeding difficulties in infants. Breastfeeding is generally not recommended during treatment.

• Primary Class: Anxiolytic
• Subclass: Benzodiazepine (short-acting)

• Known hypersensitivity to alprazolam or other benzodiazepines.
• Acute narrow-angle glaucoma.
• Concurrent use with potent CYP3A4 inhibitors (e.g., ketoconazole, itraconazole).
• Severe respiratory insufficiency or sleep apnea (relative contraindication).
• Myasthenia gravis.

• Risk of dependence, tolerance, and withdrawal symptoms; use lowest effective dose for shortest duration.
• Avoid abrupt discontinuation; taper gradually.
• Use with caution in patients with history of substance abuse or psychiatric disorders.
• Increased sedation and respiratory depression risk when combined with CNS depressants, including alcohol and opioids.
• Use cautiously in elderly or debilitated patients; risk of falls and cognitive impairment.
• Monitor for paradoxical reactions such as increased anxiety or agitation.
• Respiratory depression possible, especially in compromised pulmonary function.

• Common: Drowsiness, sedation, dizziness, impaired coordination, memory impairment, dry mouth.
• Less common: Headache, gastrointestinal upset, changes in libido.
• Serious/rare: Paradoxical reactions (agitation, irritability), respiratory depression, dependence and withdrawal symptoms, hypotension (rare).

• CYP3A4 inhibitors (ketoconazole, itraconazole, erythromycin, grapefruit juice): Increase alprazolam levels, risk of toxicity.
• CYP3A4 inducers (rifampin, carbamazepine): Decrease alprazolam efficacy.
• Other CNS depressants: Additive sedation and respiratory depression risk (e.g., alcohol, opioids).
• No significant food interactions; avoid alcohol.

• Emphasis on limiting benzodiazepine use due to abuse potential.
• Avoid combining with opioids due to increased overdose risk.
• Guidelines recommend cognitive-behavioral therapy and SSRIs as first-line treatments for anxiety and panic disorders.
• Regulatory bodies advise lower dosing and careful monitoring in elderly.

• Store at 20°C to 25°C (68°F to 77°F).
• Protect from moisture and light.
• Keep tablets in original container tightly closed.
• Keep out of reach of children.