Amitriptyline
From Wikipedia, the free encyclopedia
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Amitriptyline
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| Systematic (IUPAC) name | |
| 3-(10,11-dihydro-5H-dibenzo[[a,d]] cycloheptene-5-ylidene)-N, N-dimethyl-1-propanamine | |
| Identifiers | |
| CAS number | |
| ATC code | N06 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C20H23N |
| Mol. mass | 277.403 g/mol |
| Pharmacokinetic data | |
| Bioavailability | 40% |
| Metabolism | Hepatic |
| Half life | 12-24 hours |
| Excretion | Renal |
| Therapeutic considerations | |
| Pregnancy cat. |
C[1] |
| Legal status | |
| Routes | Oral |
Amitriptyline hydrochloride (sold as Elavil®, Tryptanol®, Endep®, Elatrol®, Tryptizol®, Trepiline®, Laroxyl®) is a tricyclic antidepressant drug. It is a white, odorless(but tastes like licorice),crystalline]] compound which is freely soluble in water and usually dispensed in tablet form.
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[edit] Mechanism of action
Amitriptyline inhibits serotonin and noradrenaline reuptake almost equally.
[edit] Uses
[edit] Approved
Amitriptyline is approved for the treatment of endogenous depression and involutional melancholia (depression of late life, which is no longer seen as a disease in its own right.Adult typical dosages are 75 to 200 mg daily, with half this initially for elderly or adolescents.
It may also be used to treat nocturnal enuresis (bed wetting). Children between the ages of 7 to 10 years having a dose of 10 to 20 mg, older children 25 to 50 mg at night. It should be gradually withdrawn at the end of the course, which overall should be of no more than 3 months.[2]
In some European countries it's also approved as prophylaxis for patients with frequent migraines (usually 25 to 75 mg).
[edit] Unapproved/Off-Label/Investigational
Amitriptyline may be prescribed for other conditions such as insomnia, migraine, rebound headache, chronic pain, postherpetic neuralgia (persistent pain following a shingles attack), fibromyalgia, vulvodynia, interstitial cystitis, irritable bowel syndrome, diabetic peripheral neuropathy, neurological pain, and painful paresthesias related to multiple sclerosis and as a preventative (prophylaxis) for patients with frequent migraines. It is also used in small (10 mg) doses to act as a painkiller and ease the effects of Carpal Tunnel Syndrome. Typically lower dosages are required for pain modification of 10 to 50 mg daily.[2]
Amitriptyline in very small doses (5 mg a day) is also sometimes prescribed to help ease the symptoms of chronic fatigue syndrome. It is thought to help combat symptoms of insomnia primarily, in addition to other selected symptoms of the affliction.
A randomized controlled trial published in June 2005 found that amitriptyline was effective in functional dyspepsia refractory to famotidine and mosapride combination therapy.[3]
[edit] Side effects
Common side effects of using amitriptyline are weight loss or gain, drowsiness, nervousness, and dizziness insomnia. Some rare side effects include tinnitus, hypotension, mania, psychosis, anticholinergic effects, heart block, arrhythmias, extrapyramidal symptoms, bone marrow depression, and hepatic toxicity.
[edit] Overdose
The symptoms and the treatment of an overdose are largely the same as for the other tricyclic antidepressants.
[edit] Footnotes
- ^ Professional Information Brochure - ELAVIL® (PDF). Retrieved on 2007-03-21.
- ^ a b British National Formulary 45 March 2003
- ^ Otaka M, Jin M, Odashima M, Matsuhashi T, Wada I, Horikawa Y, Komatsu K, Ohba R, Oyake J, Hatakeyama N, Watanabe S. "New strategy of therapy for functional dyspepsia using famotidine, mosapride and amitriptyline." Alimentary Pharmacology & Therapeutics. 2005 Jun;21 Suppl 2:42-6. PMID 15943846 Fulltext
[edit] References
- PubChem Substance Summary: Amitriptyline National Center for Biotechnology Information.
- TREPILINE®-10 TABLETS; TREPILINE®-25 TABLETS South African Electronic Package Inserts. 12 May 1978. Revised February 2004.
- SAROTEN® RETARD 25 mg Capsules; SAROTEN® RETARD 50 mg Capsules South African Electronic Package Inserts. December 1987. Updated May 2000.
