DOTHIEPIN HCL Chemical Properties

Melting point:

218-221℃

storage temp. 

-20°C

solubility 

Freely soluble in water, in alcohol and in methylene chloride.

CAS DataBase Reference

897-15-4

Safety Information

Hazard Codes 

F,T,Xn

Risk Statements 

11-23/24/25-39/23/24/25-22

Safety Statements 

7-16-36/37-45

RIDADR 

3249

HazardClass 

6.1(b)

PackingGroup 

III

DOTHIEPIN HCL Usage And Synthesis

Chemical Properties

White or faintly yellow, crystalline powder.

Uses

Dothiepin Hydrochloride is a tricyclic antidepressant.

Uses

Monoamine reuptake inhibitor; tricyclic antidepressant

Clinical Use

Tricyclic antidepressant

Drug interactions

Potentially hazardous interactions with other drugs
Alcohol: increased sedative effect.
Analgesics: increased risk of CNS toxicity with tramadol; possibly increased risk of side effects with nefopam; possibly increased sedative effects with opioids.
Anti-arrhythmics: increased risk of ventricular arrhythmias with amiodarone - avoid; increased risk of ventricular arrhythmias with disopyramide, dronedarone, flecainide or propafenone - avoid with dronedarone.
Antibacterials: increased risk of ventricular arrhythmias with moxifloxacin and possibly delamanid and telithromycin - avoid with moxifloxacin.
Anticoagulants: may alter anticoagulant effect of coumarins.
Antidepressants: enhanced CNS excitation and hypertension with MAOIs and moclobemide - avoid; concentration possibly increased with SSRIs; risk of ventricular arrhythmias with citalopram and escitalopram - avoid; possible increased risk of convulsions with vortioxetine.
Antiepileptics: convulsive threshold lowered; concentration reduced by carbamazepine, phenobarbital and possibly fosphenytoin, phenytoin and primidone.
Antimalarials: avoid with artemether/lumefantrine and piperaquine with artenimol.
Antipsychotics: increased risk of ventricular arrhythmias especially with droperidol, fluphenazine, haloperidol, pimozide, risperidone, sulpiride and zuclopenthixol - avoid; increased antimuscarinic effects with clozapine and phenothiazines; concentration increased by antipsychotics
Antivirals: increased risk of ventricular arrhythmias with saquinavir - avoid; concentration possibly increased with ritonavir.
Atomoxetine: increased risk of ventricular arrhythmias and possibly convulsions.
Beta-blockers: increased risk of ventricular arrhythmias with sotalol.
Clonidine: tricyclics antagonise hypotensive effect; increased risk of hypertension on clonidine withdrawal.
Dapoxetine: possible increased risk of serotonergic effects - avoid
Dopaminergics: avoid use with entacapone; CNS toxicity reported with selegiline and rasagiline.

Metabolism

Dosulepin hydrochloride is readily absorbed from the gastrointestinal tract, and extensively demethylated by first-pass metabolism in the liver to its primary active metabolite, desmethyldothiepin (also termed northiaden). Paths of metabolism also include S-oxidation. Dosulepin is excreted in the urine, mainly in the form of its metabolites; small amounts are also excreted in the faeces. Elimination half-lives of about 14-24 and 23-46 hours have been reported for dosulepin and its metabolites, respectively. Dose in renal impairment GFR (mL/min) 20-50 Dose as in normal renal function. 10-20 Start with small dose and titrate according to response. <10 Start with small dose and titrate according to response. Dose in patients undergoing renal replacement therapies APD/CAPD Not dialysed. Dose as in GFR<10 mL/ min. HD Not dialysed. Dose as in GFR<10 mL/ min. HDF/High flux Unknown dialysability. Dose as in GFR<10 mL/min. CAV/VVHD Unknown dialysability. Dose as in GFR=10-20 mL/min. Important drug interactions Potentially hazardous interactions with other drugs Alcohol: increased sedative effect. Analgesics: increased risk of CNS toxicity with tramadol; possibly increased risk of side effects with nefopam; possibly increased sedative effects with opioids. Anti-arrhythmics: increased risk of ventricular arrhythmias with amiodarone - avoid; increased risk of ventricular arrhythmias with disopyramide, dronedarone, flecainide or propafenone - avoid with dronedarone. Antibacterials: increased risk of ventricular arrhythmias with moxifloxacin and possibly delamanid and telithromycin - avoid with moxifloxacin. Anticoagulants: may alter anticoagulant effect of coumarins. Antidepressants: enhanced CNS excitation and hypertension with MAOIs and moclobemide - avoid; concentration possibly increased with SSRIs; risk of ventricular arrhythmias with citalopram and escitalopram - avoid; possible increased risk of convulsions with vortioxetine. Antiepileptics: convulsive threshold lowered; concentration reduced by carbamazepine, phenobarbital and possibly fosphenytoin, phenytoin and primidone. Antimalarials: avoid with artemether/lumefantrine and piperaquine with

DOTHIEPIN HCL(897-15-4)Related Product Information

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