Dosulepin

• C19H21NS ( dosulepin )
• C19H21NS · HCl ( dosulepin · hydrochloride)

N06AA16

White to slightly yellow crystalline powder ( dosulepin · hydrochloride)

Tricyclic antidepressant

• 295.45 g · mol -1 ( dosulepin )
• 331.92 g · mol -1 ( dosulepin · hydrochloride)

Slightly soluble in water, dichloromethane and ethanol ( dosulepin · hydrochloride)

Hydrochloride

Attention

260 mg · kg -1 ( LD50, Rat, oral, hydrochloride)

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Dosulepin ( INN) is a drug from the group of tricyclic antidepressants. It is usually used as a mixture of the cis- and the trans-isomer as the hydrochloride.

Pharmacology

Pharmacodynamics and pharmacokinetics

Dosulepin has the effect of doxepin. It inhibits the reuptake of the neurotransmitters serotonin and norepinephrine, in addition it also acts as an antagonist at histamine H1 and muscarinic receptor. It has a bioavailability of 30% and a half-life of 20 h metabolism via the liver.

Side effects

Common side effects ( <1% ) are: nausea, headache, constipation, dry mouth, sweating, dizziness, drowsiness, gastrointestinal disturbances, fine tremor.

In case of overdose dosulepin is more toxic than other tricyclics and leads to increased seizures and cardiac arrhythmias.

Indications

Dosulepin is approved for the treatment of retarded depression. Off label it is used for adjuvant therapy in chronic pain. Therapeutically useful doses range from 75 to 150 mg everyday, can possibly be increased to 300 mg. In patients with cardiovascular disease is a relative contraindication.

Trade names

Idom (D), Prothiaden ( in some European countries )

• With diazepam: Harmomed (A)