Detail for Clomipramine
Basic Information
DrugID 29
DrugName Clomipramine
DrugDetail Clomipramine, the 3-chloro analog of imipramine, is a dibenzazepine-derivative tricyclic antidepressant (TCA). TCAs are structurally similar to phenothiazines. They contain a tricyclic ring system with an alkyl amine substituent on the central ring. In non-depressed individuals, clomipramine does not affect mood or arousal, but may cause sedation. In depressed individuals, clomipramine exerts a positive effect on mood. TCAs are potent inhibitors of serotonin and norepinephrine reuptake. Tertiary amine TCAs, such as clomipramine, are more potent inhibitors of serotonin reuptake than secondary amine TCAs, such as nortriptyline and desipramine. TCAs also down-regulate cerebral cortical ??-adrenergic receptors and sensitize post-synaptic serotonergic receptors with chronic use. The antidepressant effects of TCAs are thought to be due to an overall increase in serotonergic neurotransmission. TCAs also block histamine-H1 receptors, ??1-adrenergic receptors and muscarinic receptors, which accounts for their sedative, hypotensive and anticholinergic effects (e.g. blurred vision, dry mouth, constipation, urinary retention), respectively. See toxicity section below for a complete listing of side effects. Clomipramine may be used to treat obsessive-compulsive disorder and disorders with an obsessive-compulsive component (e.g. depression, schizophrenia, Tourette??s disorder). Unlabeled indications include panic disorder, chronic pain (e.g. central pain, idiopathic pain disorder, tension headache, diabetic peripheral neuropathy, neuropathic pain), cataplexy and associated narcolepsy, autistic disorder, trichotillomania, onchophagia, stuttering, premature ejaculation, and premenstrual syndrome. Clomipramine is rapidly absorbed from the gastrointestinal tract and demethylated in the liver to its primary active metabolite, desmethylclomipramine.

http://www.drugbank.ca/drugs/DB01242

http://en.wikipedia.org/wiki/Clomipramine

Indication May be used to treat obsessive-compulsive disorder and disorders with an obsessive-compulsive component (e.g. depression, schizophrenia, Tourette??s disorder). Unlabeled indications include: depression, panic disorder, chronic pain (e.g. central pain, idiopathic pain disorder, tension headache, diabetic peripheral neuropathy, neuropathic pain), cataplexy and associated narcolepsy (limited evidence), autistic disorder (limited evidence), trichotillomania (limited evidence), onchophagia (limited evidence), stuttering (limited evidence), premature ejaculation, and premenstrual syndrome.

http://www.drugbank.ca/drugs/DB01242

Structure Click to see the orginal picture.
Interaction
Drug Name PMIDLink Reference
Fluconazole Marchetti O., Moreillon P., Glauser M.P., Bille J., Sanglard D. (2000) Potent synergism of the combination of fluconazole and cyclosporine in Candida albicans. Antimicrobial Agents and Chemotherapy 44:2373-2381.
Target
TargetName References EssentialGene? Link
(R)-limonene 6-monooxygenase No
5HT transporter No
5-HT-2 Yes
Adenylate cyclase type 1 No
Albendazole monooxygenase No
CYPIA2 Yes
CYPIID6 No
Cytochrome P450 Yes
Cytochrome P450 2D6 No
Cytochrome P-450 II C No
Cytochrome P450db1 No
D(2) dopamine receptor Yes
Glutathione S-transferase P No
Histamine H2 receptor No
N(1),N(8)-bis(glutathionyl)spermidine reductase No
NET Yes
Sodium-dependent serotonin transporter No
5-hydroxytryptamine 2A receptor No
5-hydroxytryptamine 2B receptor No
5-hydroxytryptamine 2C receptor No
Sodium-dependent noradrenaline transporter No
Transporter Yes
serotonin transporter inhibitor No
noradrenalin transporter inhibitor No
PathWay