Adult: For the treatment of depression and associated anxiety: Initially, 25 mg tid or 75 mg daily as a single dose at night. Dose may be gradually increased to 150 mg daily if needed. In severe depression for patients in the hospital setting, higher doses of up to 225 mg daily may be given. Elderly: Initially, 50-75 mg daily. Half the usual adult dose may be adequate to achieve a satisfactory clinical response.
What are the brands available for Dosulepin in Hong Kong?
Qualiaden
Vick-Thiaden
Hepatic Impairment
Severe: Contraindicated.
Administration
Dosulepin May be taken with or without food.
Contraindications
Acute recovery phase after MI, heart block of any degree or other cardiac arrhythmias; manic phase of bipolar disorder. Severe hepatic impairment. Concomitant use with or within 14 days of discontinuing MAOIs.
Special Precautions
Patient with history of suicidal activity/ideation, mania, or psychosis; epilepsy, predisposition for seizures (e.g. history of seizures, head trauma, brain damage, alcoholism, receiving agents which may reduce seizure threshold); glaucoma, diabetes mellitus, thyroid dysfunction (e.g. hyperthyroidism, receiving thyroid supplements), prostatic hypertrophy, urinary retention; decreased gastrointestinal motility, paralytic ileus, xerostomia, or visual problems; history of CV disease (e.g. tachycardia, previous MI, stroke); risk factors for orthostatic hypotension or those who would not tolerate transient hypotensive episodes (e.g. cerebrovascular disease, CV disease, hypovolaemia, receiving drugs that may predispose to hypotension or bradycardia). Patients undergoing surgery. Avoid abrupt withdrawal. Renal and mild to moderate hepatic impairment. Elderly. Pregnancy and lactation.
Adverse Reactions
Significant: Suicidal thoughts and behaviour, worsening of depression or psychosis, CNS depression; anticholinergic effects (e.g. blurred vision, xerostomia, constipation, urinary retention), increased risk of CV toxicity (e.g. cardiac arrhythmias, conduction disorders, cardiac failure, circulatory collapse), orthostatic hypotension, weight gain; ophthalmologic effects (e.g. may accumulate in the pigmented area of the eye, exacerbation of glaucoma), may alter glucose regulation, bone fractures; withdrawal reactions (following abrupt discontinuation). Rarely, bone marrow suppression. Cardiac disorders: Tachycardia, palpitations. Gastrointestinal disorders: Nausea, vomiting. General disorders and administration site conditions: Fatigue. Investigations: EEG pattern changes. Nervous system disorders: Drowsiness, dizziness, tremor, ataxia, epileptiform seizures, extrapyramidal symptoms including speech difficulties. Psychiatric disorders: Nervousness, insomnia, confusion. Reproductive system and breast disorders: Change in libido. Skin and subcutaneous tissue disorders: Rash, diaphoresis. Vascular disorders: Hypotension. Potentially Fatal: Serotonin syndrome.
Patient Counseling Information
This drug may cause drowsiness, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor blood pressure and pulse rate (before and during treatment initiation); mental status, CBC, blood glucose, weight, BMI; ECG particularly in elderly, with high doses, and/or in patients with pre-existing CV disease. Perform ophthalmologic exam regularly for visual acuity and colour fields during prolonged treatment. Closely monitor for signs of clinical worsening, suicidal ideation, or unusual changes in behaviour (particularly at the beginning of treatment or during dose adjustments).
Overdosage
Symptoms: Dry mouth, widely dilated pupils, visual hallucinations, paralytic ileus, hyperreflexia, hypothermia, drowsiness, loss of consciousness, ataxia, muscle twitching, delirium, excitement, restlessness, sinus tachycardia, urinary retention, and respiratory or metabolic alkalosis. In severe cases, convulsions, myoclonus, hypotension, cardiac arrhythmias, and respiratory or cardiac depression may occur. Management: Ensure adequate airway, ventilation, and oxygenation. Correct hypoxia and acid-base imbalances with assisted ventilation and IV Na bicarbonate as necessary. May administer activated charcoal within 2 hours of ingestion. Administer IV diazepam or lorazepam to control seizures. Monitor blood pressure, pulse, and cardiac rhythm for at least 6 hours following ingestion.
Drug Interactions
May potentiate the effects of anticholinergics, antihistamines, narcotic analgesics, epinephrine, and norepinephrine. May increase the risk of arrhythmias and hypotension with anaesthetics. May decrease the hypotensive effect of debrisoquine and guanethidine. May decrease plasma concentration with barbiturates. May increase plasma concentration with methylphenidate, phenothiazines, and oral contraceptives. May antagonise the anticonvulsant effect of antiepileptic drugs. May increase the risk of QT prolongation and/or ventricular arrhythmias with other agents that prolong QT interval (e.g. certain antipsychotics and antibiotics). Potentially Fatal: Increased risk of serotonin syndrome with MAOIs, SSRIs, and buprenorphine.
Food Interaction
May potentiate the CNS depressant effects of alcohol. Increased risk of serotonin syndrome with St. John's wort.
Action
Description: Mechanism of Action: Dosulepin, a thioanalogue of amitriptyline, is a tricyclic antidepressant (TCA). It inhibits the reuptake of norepinephrine and serotonin (5-hydroxytryptamine) by the presynaptic neuronal membrane, thereby increasing their synaptic concentration in the CNS. Synonym(s): Dothiepin. Pharmacokinetics: Absorption: Readily absorbed from the gastrointestinal tract. Time to peak plasma concentration: Approx 2-3 hours. Distribution: Enters breast milk (small amounts). Plasma protein binding: 84%. Metabolism: Extensively demethylated via first-pass metabolism in the liver to the active metabolite desmethyldothiepin (northiaden). Excretion: Via urine (50-60% as metabolites); faeces (15-40%). Elimination half-life: Biphasic: Approx 15-18 hours (1st phase); 50 hours (mean whole body elimination).
Chemical Structure
Dosulepin Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5282426, Dothiepin. https://pubchem.ncbi.nlm.nih.gov/compound/Dothiepin. Accessed Oct. 29, 2024.
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