Detail for Amitriptyline
Basic Information
DrugID 7
DrugName Amitriptyline
DrugDetail Amitriptyline hydrochloride is a dibenzocycloheptene-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, amitriptyline does not affect mood or arousal, but may cause sedation. In depressed individuals, amitriptyline exerts a positive effect on mood. TCAs are potent inhibitors of serotonin and norepinephrine reuptake. Tertiary amine TCAs, such as amitriptyline, are more potent inhibitors of serotonin reuptake than secondary amine TCAs, such as nortriptyline. 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. Amitriptyline may be used to treat depression, chronic pain (unlabeled use), irritable bowel syndrome (unlabeled use), diabetic neuropathy (unlabeled use), post-traumatic stress disorder (unlabeled use), and for migraine prophylaxis (unlabeled use).

http://www.drugbank.ca/drugs/DB00321

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

Indication For the treatment of depression, chronic pain, irritable bowel syndrome, sleep disorders, diabetic neuropathy, agitation and insomnia, and migraine prophylaxis.

http://www.drugbank.ca/drugs/DB00321

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
4-nitrophenol 2-hydroxylase No
5HT transporter No
Adenylate cyclase type 1 No
Albendazole monooxygenase No
Alpha-2A adrenergic receptor Yes
CYPIA2 Yes
CYPIIB6 No
CYPIIC8 No
CYPIID6 No
Cytochrome P450 Yes
Cytochrome P450 2D6 No
Cytochrome P-450 II C No
Cytochrome P450db1 No
D(1A) dopamine receptor Yes
D(1B) dopamine receptor No
D(2) dopamine receptor Yes
D(3) dopamine receptor Yes
G-protein coupled receptor 97 No
Histamine H1 receptor No
Histamine H2 receptor No
Monoamine transporter Yes
NET Yes
Potassium voltage-gated channel subfamily H member 2 No
Potassium voltage-gated channel subfamily KQT member 2 Yes
Sodium-dependent noradrenaline transporter No
Sodium-dependent serotonin transporter No
5-hydroxytryptamine 2A receptor No
5-hydroxytryptamine 1A receptor No
Delta-type opioid receptor No
Kappa-type opioid receptor Yes
High affinity nerve growth factor receptor Yes
BDNF/NT-3 growth factors receptor Yes
Alpha-1A adrenergic receptor No
Alpha-1D adrenergic receptor No
Muscarinic acetylcholine receptor M1 No
Muscarinic acetylcholine receptor M2 No
Muscarinic acetylcholine receptor M3 No
Muscarinic acetylcholine receptor M4 No
Muscarinic acetylcholine receptor M5 No
Potassium voltage-gated channel subfamily A member 1 Yes
Potassium voltage-gated channel subfamily D member 2 No
Potassium voltage-gated channel subfamily D member 3 No
serotonin transporter inhibitor No
noradrenalin transporter inhibitor No
PathWay