Alprazolam


Thông tin thuốc gốc
Chỉ định và Liều dùng
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.

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.
Special Patient Group
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.
Hepatic Impairment
Severe: Contraindicated.
Cách dùng
May be taken with or without food. Side effects eg, sleepiness/drowsiness may be reduced if taken immediately after meals.
Chống chỉ định
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).
Thận trọng
Patients with depression, suicidal tendencies, psychiatric or personality disorder, respiratory disease, history of drug abuse or acute alcoholism. Patients who are debilitated, obese, smokers, or at risk of falls. Concomitant use with opioids. Avoid abrupt withdrawal. Renal and mild to moderate hepatic impairment. Elderly. Pregnancy and lactation.
Phản ứng phụ
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 admin 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.
Thông tin tư vấn bệnh nhân
This drug may cause drowsiness, sedation, amnesia, impaired concentration or muscle function, if affected, do not drive or operate machinery.
MonitoringParameters
Monitor CV and respiratory status.
Quá liều
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.
Tương tác
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 effects of opioids. Increased plasma concentrations 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.
Tác dụng
Description: 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.
Pharmacokinetics:
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).
Đặc tính

Chemical Structure Image
Alprazolam

Source: National Center for Biotechnology Information. PubChem Database. Alprazolam, CID=2118, https://pubchem.ncbi.nlm.nih.gov/compound/Alprazolam (accessed on Jan. 20, 2020)

Bảo quản
Store between 20-25°C. Protect from moisture.
Phân loại MIMS
Phân loại ATC
N05BA12 - alprazolam ; Belongs to the class of benzodiazepine derivatives anxiolytics. Used in the management of anxiety, agitation or tension.
References
Alprazolam Solution, Concentrate (Roxane Laboratories, Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 26/11/2014.

Alprazolam Solution, Concentrate (West-Ward Pharmaceuticals Corp.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 15/08/2019.

Alprazolam Tablet (Sun Pharma Global FZE). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 26/11/2014.

Alprazolam Tablet, Extended Release (Actavis Elizabeth LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 26/11/2014.

Alprazolam Tablet, Extended Release (Aurobindo Pharma Limited). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 15/08/2019.

Alprazolam Tablet, Orally Disintegrating (Par Pharmaceutical, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 15/08/2019.

Anon. Alprazolam. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 15/08/2019.

Anon. Alprazolam. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 15/08/2019.

Buckingham R (ed). Alprazolam. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 15/08/2019.

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