Alprazolam


Full Generic Medicine Info
Dosage/Direction for Use

Oral
Short-term management of anxiety
Adult: In patients with moderate or severe anxiety states, or anxiety associated with depression: As conventional tab, orally-disintegrating tab, oral solution: 0.25-0.5 mg tid, may be increased as necessary every 3-4 days to a total of 3 or 4 mg daily. Treatment duration: 8-12 weeks, including a tapering off process.
Elderly: As conventional tab, orally-disintegrating tab, oral solution: 0.25 mg 2-3 times daily, may be increased gradually if needed and tolerated.
Hepatic impairment: Severe: Contraindicated.

Oral
Panic disorder with or without agoraphobia
Adult: As conventional tab, orally-disintegrating tab, oral solution: Initially, 0.5 mg tid, may be increased in increments of not more than 1 mg daily every 3-4 days; if required, doses of up to 10 mg daily may be used. As extended-release tab: Initially, 0.5-1 mg once daily, may be increased in increments of not more than 1 mg daily every 3-4 days; doses of up to 3-6 mg daily may be used.
Elderly: As conventional tab, orally-disintegrating tab, oral solution: Initially, 0.25 mg 2-3 times daily. As extended-release tab: Initially, 0.5 mg once daily. All doses may be increased gradually if needed and tolerated.
Hepatic impairment: Severe: Contraindicated.

Special Populations: Debilitated patients: As conventional tab, orally-disintegrating tab, oral solution: 0.25 mg 2-3 times daily, may be increased gradually if needed and tolerated. As extended-release tab: Initially, 0.5 mg once daily, may be increased gradually if needed and tolerated.
Administration
May be taken with or without food. Side effects eg sleepiness/drowsiness may be reduced if taken immediately after meals.
Contraindications
Myasthenia gravis, severe respiratory insufficiency, sleep apnoea syndrome, acute narrow-angle glaucoma. Severe hepatic impairment. Concomitant use with potent CYP3A4 inhibitors (e.g. ketoconazole, itraconazole).
Special Precautions
Patients with depression, suicidal tendencies, psychiatric or personality disorder, respiratory disease, history of drug abuse or acute alcoholism. Patients who are debilitated, obese, smoker, or at risk of falls. Concomitant use with opioids. Avoid abrupt withdrawal. Renal and mild to moderate hepatic impairment. Elderly. Pregnancy and lactation. Patient Counselling This drug may cause drowsiness, sedation, amnesia, impaired concentration or muscle function, if affected, do not drive or operate machinery. Monitoring Parameters Monitor CV and respiratory status.
Adverse Reactions
Significant: Suicidal ideation, CNS depression, anterograde amnesia, psychiatric and paradoxical reactions, interdose symptoms (e.g. early morning anxiety, breakthrough anxiety), sleep-related activities (e.g. sleep-driving, cooking, eating or making phone calls while asleep), tolerance, abuse, psychological and physical dependence; rebound or withdrawal symptoms including seizures. Cardiac disorders: Palpitations, chest pain. Endocrine disorders: Hyperprolactinaemia. Eye disorders: Blurred vision. Gastrointestinal disorders: Constipation, dry mouth, nausea, vomiting, increased salivation. General disorders and administration site conditions:Ataxia, lethargy, fatigue, irritability. Hepatobiliary disorders: Jaundice, abnormal hepatic function, hepatitis. Investigations: Weight increased or decreased, increased intraocular pressure. Metabolism and nutrition disorders: Decreased or increased appetite. Musculoskeletal and connective tissue disorders: Muscle weakness, arthralgia, myalgia. Nervous system disorders: Sedation, somnolence, headache, dizziness, memory impairment, balance disorder, abnormal coordination, tremor. Psychiatric disorders: Depression, insomnia, confusional state, anxiety, disorientation, nervousness, dysarthria, disturbance in attention, hypersomnia, decreased or increased libido. Renal and urinary disorders: Incontinence, difficulty in micturition. Reproductive system and breast disorders: Sexual dysfunction, irregular menstruation. Respiratory, thoracic and mediastinal disorders: Nasal congestion, dyspnoea, rhinitis. Skin and subcutaneous tissue disorders: Dermatitis, rash, pruritus. Vascular disorders: Hypotension.
Overdosage
Symptoms: Somnolence, confusion, impaired coordination, diminished reflexes, coma and death. Management: Symptomatic and supportive treatment. Induce vomiting within 1 hour of ingestion if the patient is conscious or consider gastric lavage with protected airway if the patient is unconscious. May administer activated charcoal to reduce absorption if there is no advantage in gastric emptying. Flumazenil may be given as an antidote.
Drug Interactions
Enhanced CNS depressant effects with other anxiolytics or sedatives, antipsychotics (neuroleptics), hypnotics, antidepressants, narcotic analgesics, antiepileptic drugs, anaesthetics, sedative antihistamines. Increased plasma concentrations with CYP3A4 inhibitors (e.g. nefazodone, fluvoxamine, cimetidine, fluoxetine, propoxyphene, oral contraceptives, sertraline, paroxetine, diltiazem, isoniazid, macrolide antibiotics such as erythromycin, clarithromycin, troleandomycin). May enhance metabolism with CYP3A4 inducers (e.g. ritonavir, carbamazepine). May increase plasma concentrations of digoxin.
Potentially Fatal: Enhanced CNS depressant effect of opioids. Increased plasma concentration with potent CYP3A4 inhibitors (e.g. ketoconazole, itraconazole and other azole-type antifungals).
Food Interaction
Enhanced CNS depressant effects with alcohol. May increase bioavailability with grapefruit juice.
Action
Alprazolam binds to stereospecific benzodiazepine receptors on the postsynaptic GABA neuron at several sites within the CNS, including the limbic system and reticular formation. Enhancement of the GABA inhibitory effect on neuronal excitability results by increased neuronal membrane permeability to Cl ions, which results in hyperpolarisation (a less excitable state) and stabilisation. Benzodiazepine receptors and effects appear to be linked to the GABA-A receptors but does not bind to GABA-B receptors.
Absorption: Readily absorbed from the gastrointestinal tract. Bioavailability: 84-92% (immediate-release tab); 90% (extended-release tab). Time to peak plasma concentration: 1-2 hours (immediate-release tab); approx 9 hours (extended-release tab); 1.5-2 hours (orally-disintegrating tab).
Distribution: Crosses placenta and enters breast milk. Volume of distribution: 0.84-1.42 L/kg (immediate-release tab). Plasma protein binding: Approx 80%, mainly to albumin.
Metabolism: Extensively metabolised in the liver by CYP3A4 isoenzyme into α-hydroxyalprazolam and 4-hydroxyalprazolam metabolites, and an inactive benzophenone metabolite.
Excretion: Via urine (as unchanged drug and metabolites). Elimination half-life: 11.2 hours; 6.3-26.9 hours (immediate-release tab); 10.7-15.8 hours (extended-release tab); 12.5 hours (orally-disintegrating tab).
Storage
Oral: Store between 20-25°C. Protect from moisture.
CIMS Class
ATC Classification
N05BA12 - alprazolam ; Belongs to the class of benzodiazepine derivatives anxiolytics. Used in the management of anxiety, agitation or tension.
Disclaimer: This information is independently developed by CIMS based on alprazolam from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to CIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, CIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2021 CIMS. All rights reserved. Powered by CIMSAsia.com
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