|
|
| | DOTHIEPIN HCL Basic information |
| Product Name: | DOTHIEPIN HCL | | Synonyms: | DOTHIEPIN HCL;11-(3-dimethylaminopropylidene)-6,11-dihydrodibenzo(b,e)thiepinehydrochlorid;3-dibenzo(b,e)thiepin-11(6h)-ylidene-n,n-dimethyl-1-propanaminhydrochlor;dosulepinchloride;11-(3-DiMethylaMinopropylidene)-6,11-dihydrodibenzo(b,e)thiepine hydrochloride;Dothiepin (cis/trans) hydrochloride solution;3-dibenzo[b,e]thepin-11(6H)-ylidine-N,N-dimethyl-1-propanamine hydrochloride;dosulepinhydrochloride | | CAS: | 897-15-4 | | MF: | C19H22ClNS | | MW: | 331.9 | | EINECS: | 212-978-8 | | Product Categories: | Antidepressant | | Mol File: | 897-15-4.mol |  |
| | 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 |
| | DOTHIEPIN HCL Usage And Synthesis |
| Chemical Properties | White or faintly yellow, crystalline powder. | | Uses | Monoamine reuptake inhibitor; tricyclic antidepressant | | Uses | 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 |
| | DOTHIEPIN HCL Preparation Products And Raw materials |
|