Adult: For patients with neurotic/reactive cases, endogenous and psychotic depression, and depression accompanied by anxiety or agitation: Initially, 50 mg 2-3 times daily, may be increased to 100 mg 2-3 times daily by the end of 1st week according to the patient's response and tolerability. Usual effective dose: 200-300 mg daily. If no response occurs after using 300 mg daily dose for at least 2 weeks, may further increase the dose up to a Max of 400 mg daily. In hospitalised patients who are refractory to antidepressant therapy and with no history of seizures, doses may be cautiously increased up to a Max of 600 mg daily in 2-3 divided doses. Once the effective dose is achieved, doses ≤300 mg may be given once daily at bedtime; doses >300 mg daily should be divided. Elderly: Initially, 25 mg 2-3 times daily, may be increased to 50 mg 2-3 times daily by the end of 1st week according to the patient's response and tolerability. Usual effective dose: 100-150 mg daily. If no response is observed, doses may be cautiously increased further up to a Max of 300 mg daily. Once the effective dose is achieved, doses ≤300 mg may be given once daily at bedtime.
Cách dùng
Amoxapine May be taken with or without food.
Chống chỉ định
Acute recovery phase after MI. Concomitant use or within 14 days of discontinuing MAOIs.
Thận trọng
Patient with bipolar disorder, risk factors for seizures (e.g. history of seizures, head trauma, brain damage, alcoholism); decreased gastrointestinal motility, paralytic ileus, urinary retention, benign prostatic hyperplasia, xerostomia, visual problems, angle-closure glaucoma, increased intraocular pressure; history of CV disease (e.g. tachycardia, previous MI, stroke), cerebrovascular disease, hypovolaemia, diabetes mellitus. Consider treatment discontinuation, when possible, before undergoing electroconvulsive therapy (ECT); concurrent treatment may increase the risks associated with ECT. Avoid abrupt withdrawal. Renal and hepatic impairment. Elderly. Pregnancy and lactation.
Tác dụng không mong muốn
Significant: Suicidal ideation and behaviour, worsening of depression, unusual changes in behaviour; shift from mania to hypomania, CNS depression; extrapyramidal symptoms, including pseudoparkinsonism, akathisia, tardive dyskinesia, and acute dystonic reactions; anticholinergic effects (e.g. blurred vision, xerostomia, constipation, urinary retention); bone fractures, ocular effects (e.g. mild pupillary dilation which may trigger angle-closure glaucoma attacks), orthostatic hypotension; withdrawal symptoms (following abrupt discontinuation). Cardiac disorders: Palpitations. Gastrointestinal disorders: Nausea. General disorders and administration site conditions: Oedema, fatigue, weakness. Investigations: Increased serum prolactin; changes in EEG patterns. Metabolism and nutrition disorders: Increased appetite. Nervous system disorders: Drowsiness, dizziness, headache, ataxia, tremors. Psychiatric disorders: Anxiety, insomnia, nervousness, confusion, restlessness. Skin and subcutaneous tissue disorders: Diaphoresis, rash. Potentially Fatal: Neuroleptic malignant syndrome.
This drug may cause drowsiness or dizziness, if affected, do not drive or operate machinery.
Chỉ số theo dõi
Monitor blood pressure, heart rate, weight, BMI, and blood glucose. Perform ECG in patients at risk of QT-prolongation. Closely monitor for signs of suicidal ideation, clinical worsening, or unusual changes in behaviour at the start of therapy and during dose adjustments. Assess for signs of parkinsonism or abnormal involuntary movements.
Quá liều
Symptoms: Grand mal convulsions, acidosis, status epilepticus, and coma. Acute tubular necrosis, myoglobinuria, rhabdomyolysis, and renal failure may occur. Management: Symptomatic and supportive treatment. May induce emesis followed by gastric lavage in conscious patients; thereafter, activated charcoal may be given to reduce the absorption. Prevent or control seizures with standard anticonvulsant therapy (e.g. diazepam, phenytoin). Establish adequate airway or provide assisted ventilation in comatose patients. Treatment for non-drug-induced renal dysfunction may be done in case renal impairment occurs.
Tương tác
May enhance the effects of other CNS depressants and barbiturates. May increase the serum concentration with cimetidine. May increase the risk of paralytic ileus with anticholinergic agents. Potentially Fatal: Increased risk of serotonin syndrome with MAIOs.
Tương tác với thức ăn
Increased risk of serotonin syndrome with St. John's wort. May potentiate the CNS depressant effects of alcohol.
Tác dụng
Description: Mechanism of Action: Amoxapine, a dibenzoxazepine tricyclic antidepressant, is the N-desmethyl derivative of loxapine. The exact mechanism of action has not been fully elucidated, but it is known to reduce the reuptake of serotonin and norepinephrine. It also has a dopamine receptor-blocking effect. Onset: Initial antidepressant effect: Within 1-2 weeks. Pharmacokinetics: Absorption: Rapidly and well absorbed from the gastrointestinal tract. Time to peak plasma concentration: Approx 90 minutes. Distribution: Enters breastmilk. Volume of distribution: 0.9-1.2 L/kg. Plasma protein binding: Approx 90%. Metabolism: Extensively metabolised in the liver via hydroxylation into 2 active metabolites, 7-hydroxyamoxapine and 8-hydroxyamoxapine; further conjugated into glucuronides. Excretion: Via urine (as glucuronide metabolites). Elimination half-life: 8 hours (amoxapine); 30 hours (8-hydroxyamoxapine).
Đặc tính
Amoxapine Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 2170, Amoxapine. https://pubchem.ncbi.nlm.nih.gov/compound/Amoxapine. Accessed Nov. 25, 2024.
N06AA17 - amoxapine ; Belongs to the class of non-selective monoamine reuptake inhibitors. Used in the management of depression.
Tài liệu tham khảo
Amoxapine Tablet (Actavis Pharma, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 15/11/2024.Amoxapine Tablet (Chartwell RX, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 03/10/2024.Amoxapine. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 03/10/2024.Anon. Amoxapine. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 03/10/2024.Brayfield A, Cadart C (eds). Amoxapine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/10/2024.