Amitriptyline HCL 549-18-8
Amitriptyline Hydrochloride is an oral and parenteral tertiary amine tricyclic antidepressant. It is structurally related to the thioxanthene antipsychotics such as thiothixene. Amitriptyline Hydrochloride is also related to the skeletal muscle relaxant cyclobenzaprine, although amitriptyline is not believed to possess muscle-relaxant properties. Amitriptyline Hydrochloride is metabolized to nortriptyline, an active metabolite that is also marketed separately.
Clinically, Amitriptyline Hydrochloride is used to treat depression, pain of neuropathic origin, attention-deficit hyperactivity disorder, functional enuresis in children, panic disorder, social anxiety disorder, and to manage some eating disorders.
Amitriptyline Hydrochloride’s innovator is Merck & Co.-Global and is known world-wide by the brand names: Elavil and Vanatrip.
The precise action of tricyclic antidepressants is not fully understood, but it is believed that the most important effect is the decreased reuptake of norepinephrine and serotonin. Amitriptyline Hydrochloride appears to exert effects on both norepinephrine and serotonin (5-HT), although the selective-acting desipramine is a more potent inhibitor of norepinephrine transport. Amitriptyline Hydrochloride is metabolized to nortriptyline, which accounts for most of the norepinephrine-reuptake inhibition after Amitriptyline Hydrochloride administration. Nortriptyline itself also possesses antidepressant activity. Additional hydroxy metabolites apparently are active as well.
Monoamine oxidase is not inhibited by either Amitriptyline Hydrochloride or nortriptyline. Tricyclic antidepressants do not affect dopamine reuptake. Varying degrees of sedation can be produced, and the seizure threshold can be lowered. Amitriptyline Hydrochloride possesses strong anticholinergic activity. Cardiac dysrhythmias can result from the direct quinidine-like effect on cardiac function combined with anticholinergic activity and norepinephrine potentiation. Changes in sex hormone concentrations and blood glucose can result from Amitriptyline Hydrochloride's effect on the endocrine system.
Initially, the oral dosage is 25-75 mg per day. Amitriptyline Hydrochloride comes in tablets of 10 mg, 25 mg, 50 mg, 75 mg, 100 mg and 150 mg.
Amitriptyline Hydrochloride was approved by the FDA in 1961.
General data on Amitriptyline Hydrochloride Active Pharmaceutical Ingredient
CAS Registry: 549-18-8
ATC: N06AA09
Molecular Formula: C20H23N, HCl
Molecular Weight: 313.9
Pharmacopoeias:In Chin., Eur., Int., Jpn, and US
| Systematic (IUPAC) name: | |
|---|---|
| Amitriptyline HCL CAS number: | 549-18-8 |
| ATC code: | N06AA09 |
| PubChem: | |
| DrugBank: | |
| Formula: | C20H23N, HCl |
| Molecular mass: | 313.9 g/mol |
| Amitriptyline HCL Assay/Purity: | Typically NLT 98% |
