| Identification | Back Directory | [Name]
DOTHIEPIN HCL | [CAS]
897-15-4 | [Synonyms]
Altapin
Depresym
DOTHIEPIN HCL
DOSULEPIN HCL
Dothiepin-d6 HCl
dosulepinchloride
dosulepinhydrochloride
prothiadenhydrochloride
DOTHIEPIN HYDROCHLORIDE
Dothiepin·hydrochloric acid
Dosulepin hydrochloride CRS
trans-Dosulepin hydrochloride
DOTHIEPINHYDROCHLORIDEMONOHYDRATE
Dothiepin (cis/trans) hydrochloride solution
DOSULEPIN HYDROCHLORIDE (DOTHIEPIN HYDROCHLORIDE)
3-dibenzo(b,e)thiepin-11(6h)-ylidene-n,n-dimethyl-1-propanaminhydrochlor
n,n-dimethyldibenzo(b,e)thiepin-delta(sup11(6h),gamma)-propylaminehydrochlo
3-dibenzo[b,e]thepin-11(6H)-ylidine-N,N-dimethyl-1-propanamine hydrochloride
11-(3-dimethylaminopropylidene)-6,11-dihydrodibenzo(b,e)thiepinehydrochlorid
11-(3-Dimethylaminopropylidene)-6,11-dihydrodibenzo[b,e]thiepin hydrochloride
1-Propanamine, 3-dibenzob,ethiepin-11(6H)-ylidene-N,N-dimethyl-, hydrochloride
11-(3-DiMethylaMinopropylidene)-6,11-dihydrodibenzo(b,e)thiepine hydrochloride
(E)-3-[Dibenzo[b,e]thiepin-11(6H)-ylidene]-N,N-dimethyl-1-propanamine·hydrochloride | [EINECS(EC#)]
212-978-8 | [Molecular Formula]
C19H22ClNS | [MDL Number]
MFCD00941484 | [MOL File]
897-15-4.mol | [Molecular Weight]
331.9 |
| Chemical Properties | Back Directory | [Appearance]
White or faintly yellow, crystalline powder. | [Melting point ]
218-221℃ | [storage temp. ]
?20°C | [solubility ]
Freely soluble in water, in alcohol and in methylene chloride. | [form ]
neat | [CAS DataBase Reference]
897-15-4 |
| Hazard Information | Back Directory | [Chemical Properties]
White or faintly yellow, crystalline powder. | [Uses]
Monoamine reuptake inhibitor; tricyclic antidepressant | [Biological Activity]
Dothiepin hydrochloride is a 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 |
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