Amitriptyline

Indications
 Oral
Depression
Adult: Initially, 50-75 mg daily in divided doses or as a single dose at night. May increase dose gradually to 150 mg daily, if needed. Up to 300 mg daily may be used in severe cases.
Child: Adolescents(>16yr): 30-75 mg daily or in divided doses, preferably at bedtime.
Elderly: 30-75 mg daily or in divided doses, preferably at bedtime.
Oral
Nocturnal enuresis
Child: >11 yr: 25-50 mg at bedtime; 6-10 yr: 10-20 mg at bedtime. Treatment should not continue >3 mth.
Oral
Neuropathic pain
Adult: Initially, 10-25 mg daily at night, may increase to 75 mg daily if needed. Higher doses require specialist attention.
Oral
Prophylaxis of migraine
Adult: Initially, 10 mg at night. Maintenance: 50-75 mg at night.
Contraindications
 Hypersensitivity, use of MAO inhibitors within the last 14 days; acute recovery phase post-MI. Concurrent usage with cisapride.
Warnings / Precautions
 Bipolar illness, pregnancy, lactation elderly, CVS disease, renal or liver impairment, epilepsy, thyroid dysfunction, DM. Avoid abrupt withdrawal; urinary retention, prostatic hyperplasia; chronic constipation; angle-closure glaucoma; phaeochromocytoma. Monitor for signs of clinical worsening, suicidality or behavioural changes. May increase risks associated with electro-convulsive therapy. May affect ability to drive or operate machinery.
Adverse Reactions
 Postural hypotension, tachycardia, conduction disturbances. Dry mouth, wt gain, sour or metallic taste, stomatitis, constipation; blurring of vision, urinary retention, fatigue, dizziness, weakness, tremors, headache, confusion and delirium in elderly, sexual disturbances; peripheral neuropathy; urticaria, angioedema, sweating.
Potentially Fatal: Cardiac arrhythmias.
Overdose Reactions
 Symptoms: Excitement and restlessness with marked antimuscarinic effects, including dryness of the mouth, hot dry skin, dilated pupils, tachycardia, urinary retention and intestinal stasis. Severe symptoms include unconsciousness, convulsions and myoclonus, hyperreflexia, hypothermia, hypotension, metabolic acidosis, and respiratory and cardiac depression, with life-threatening cardiac arrhythmias that may recur some days after apparent recovery.
Drug Interactions
 Reduced effect of antihypertensives. Potentiates hypertensive effects of sympathomimetics. Concurrent use with altretamine may cause orthostatic hypotension. May increase adverse CV effects when used with amphetamines. May increase serum levels of carbamazepine. Increased risk of cardiac arrhythmias when used with β-agonists. Absorption may be reduced when used with cholestyramine, colestipol or sucralfate. Additive sedative effects when used with CNS depressants. Concurrent use with CYP2D6 inhibtors (e.g. chlorpromazine, delavirdine, fluoxetine, miconazole, paroxetine) may increase serum levels of amitriptyline. May increase antidiabetic effect of tolazamide, chlorpropamide or insulin. May reduce absorption of levodopa. Increased risk of neurotoxicity when used with lithium. Increased risk of seizures when used with tramadol. May increase anticoagulant effect of warfarin. May cause QT prolongation and fatal arrhythmias when used with drugs that prolong QT interval.
Potentially Fatal: Increased risk of QT prolongation and arrhythmias when used with cisapride. Serious adverse effects e.g. hyperpyrexia, hypertension, tachycardia, confusion, seizures and deaths may occur when used with MAO inhibitors.
See Below for More amitriptyline Drug Interactions
Food Interactions
 Alcohol may enhance adverse effects.
Mechanism of Actions
 Amitriptyline is a TCA that exerts its action by blocking neuronal re-uptake of noradrenaline and serotonin thus increasing synaptic concentration of serotonin and/or norepinephrine in the CNS.
Absorption: Readily absorbed from the GI tract (oral).
Distribution: Widely distributed; crosses the placenta; enters breast milk. Protein-binding: Extensive.
Metabolism: Extensively 1st-pass effect; demethylated hepatically to nortriptyline (active metabolite).
Excretion: Urine (as metabolites in free or conjugated form); 9-25 hr (elimination half-life).
Administration
 May be taken with or without food.
Storage Conditions
 Oral: Store at 20-25°C.
ATC Classification
 N06AA09 - amitriptyline ; Belongs to the class of non-selective monoamine reuptake inhibitors. Used in the management of depression.
Storage
 Oral: Store at 20-25°C.
Available As
  • Amitriptyline 10 mg
  • Amitriptyline 12.5 mg
  • Amitriptyline 25 mg
  • Amitriptyline 50 mg
  • Amitriptyline 75 mg

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