Trade names Dothep, Prothiaden Routes of
administration Oral CAS ID 113-53-1 Bioavailability 30% | Pregnancy
category AU: C ATC code N06AA16 (WHO) Molar mass 295.45 g/mol Protein binding 84% | |
 | ||
AHFS/Drugs.com International Drug Names Legal status AU: S4 (Prescription only)
US: ℞-only | ||
Dosulepin (INN, BAN) formerly known as dothiepin (USAN), and marketed under the brand names Prothiaden, Dothep, Thaden, and Dopress, is a tricyclic antidepressant that is used in several European and South Asian countries, as well as Australia, South Africa, and New Zealand. It is not used in the United States.
Contents
- How to pronounce dosulepin
- Medical uses
- Adverse effects
- Contraindications
- Drug interactions
- Overdose
- Mechanism of action
- Pharmacokinetics
- References
How to pronounce dosulepin
Medical uses
Dosulepin is used for the treatment of major depressive disorder and neuropathic pain. Dosulepin is only TGA- and MHRA-approved for the treatment of major depressive disorder. There is clear evidence of the efficacy of dosulepin in psychogenic facial pain, though the drug may be needed for up to a year.
Adverse effects
Common adverse effects:
Less common adverse effects:
Contraindications
Contraindications include:
Drug interactions
Dosulepin can potentiate the effects of alcohol and at least one death has been attributed to this combination. TCAs potentiate the sedative effects of barbiturates, tranquillisers and CNS depressants. Guanethidine and other adrenergic neurone blocking drugs can have their antihypertensive effects blocked by dosulepin. Sympathomimetics may potentiate the sympathomimetic effects of dosulepin. Due to the anticholinergic and antihistamine effects of dosulepin anticholinergic and antihistamine medications may have their effects potentiated by dosulepin and hence these combinations are advised against. Dosulepin may have its postural hypotensive effects potentiated by diuretics. Anticonvulsants may have their efficacy reduced by dosulepin due to its ability to reduce the seizure threshold.
Overdose
The symptoms and the treatment of an overdose are largely the same as for the other tricyclic antidepressants. Dosulepin may be particularly toxic in overdose compared to other TCAs. The onset of toxic effects is around 4–6 hours after dosulepin is ingested. In order to minimise the risk of overdose it is advised that patients only receive a limited number of tablets at a time so as to limit their risk of overdosing. It is also advised that patients are not prescribed any medications that are known to increase the risk of toxicity in those receiving dosulepin due to the potential for mixed overdoses. The medication should also be kept out of reach of children.
Mechanism of action
Dosulepin is a tricyclic antidepressent.
Pharmacokinetics
Dothiepin is readily absorbed from the small intestine and is extensively metabolised on first-pass through the liver into its chief active metabolite, northiaden (desmethyldosulepin). Peak plasma concentrations of between 30.4 ng/mL to 278.8 ng/mL occur within 2–3 hours of oral administration. It is distributed in breast milk and crosses the placenta and blood-brain barrier. It is highly bound to plasma proteins (84%), and has a whole-body elimination half-life of 51 hours.