Dothiepin (Dosulepin)

Indications
Oral
Depression
Adult: Initially, 25 mg tid, gradually increased to 50 mg tid if necessary, alternatively as a single dose at night. Up to 225 mg/day may be used in severe depression.
Elderly: Initially, 50-75 mg daily.
Contraindications
Hypersensitivity, recent MI, neonates, heart block, cardiac arrhythmias, mania, alcohol, other CNS depressants, severe liver disease, prostate disease, children.
Warnings / Precautions
Epilepsy, hypertension, glaucoma, urinary retention, gradual withdrawal, pregnancy, lactation, elderly.
Adverse Reactions
Cholestatic jaundice, sexual dysfunction, exacerbation of psychotic manifestation, cardiac arrhythmias, hypotension, dry mouth, constipation, disturbance of accommodation, tachycardia, postural hypotension, drowsiness, tremors and skin rash. Withdrawal symptoms with abrupt cessation: Insomnia, irritability and excessive sweating.
Potentially Fatal: Bone marrow depression, cardiac arrhythmias and agranulocytosis, reports of ventricular fibrillation and renal failure.
Drug Interactions
Barbiturates reduce antidepressant effect of dosulepin. Raised serum concentrations with methylphenidate. Cigarette smoking enhances metabolism. Increased risk of ventricular arrhythmias when used with drugs that prolong QT interval.
Potentially Fatal: Should not be given concurrently or within 14 days of stopping MAOIs. Potentiates catecholamines, sympathomimetics, narcotics and alcohol. Reduces hypotensive activity of bethanidine, guanethidine.
See Below for More dosulepin Drug Interactions
Mechanism of Actions
Also known as dothiepin. It inhibits the neuronal re-uptake of noradrenaline in the CNS. Its antidepressant activity appears to be related with inhibition of monoamine neurotransmitter re-uptake.
Absorption: Readily absorbed from the GI tract (oral).
Distribution: Enters breast milk.
Metabolism: Extensively hepatic via demethylation to desmethyldothiepin, S-oxidation.
Excretion: Urine (as metabolites), faeces (small amounts). Elimination half-life: 14-24 hr (dosulepin), 23-46 hr (metabolites).
ATC Classification
N06AA16 - dosulepin ; Belongs to the class of non-selective monoamine reuptake inhibitors. Used in the management of depression.
Available As
  • Dothiepin (Dosulepin) 10 mg
  • Dothiepin (Dosulepin) 100 mg
  • Dothiepin (Dosulepin) 150 mg
  • Dothiepin (Dosulepin) 25 mg
  • Dothiepin HCI 25 mg
  • Dothiepin (Dosulepin) 5 mg
  • Dothiepin (Dosulepin) 50 mg
  • Dothiepin HCI 50 mg
  • Dothiepin (Dosulepin) 75 mg
  • Dothiepin HCI 75 mg
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