Amitriptyline
 |
|
|
Amitriptyline
|
|
| 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 | |
| ChemSpider | |
| 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. |
D(US) |
| Legal status | |
| Routes | Oral |
Amitriptyline (or Amitryptyline) hydrochloride (sold as Elavil, Tryptanol, Endep, Elatrol, Tryptizol, Trepiline, Laroxyl, Saroten, Triptyl) is a tricyclic antidepressant drug. It is a white, odorless (but tastes like licorice), crystalline compound which is freely soluble in water; it is usually dispensed in tablet form. In terms of its mechanism of action, amitriptyline inhibits serotonin[1] and noradrenaline reuptake almost equally.
Contents |
Uses
Amitriptyline is now used in the United States and UK to prevent migranes and vaginal swelling only in very small doses.
Approved
Amitriptyline is approved most commonly for the treatment of depression (clinical/endogenous depression, also involutional melancholia 'depression of late life', which is no longer seen as a disease in its own right). Adult typical dosages are 25 to 150 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 It should be gradually withdrawn at the end of the course, which overall should be of no more than 3 months.[2]
Amitriptyline is used in ankylosing spondylitis for pain relief and in some European countries it is officially approved as a preventive (prophylaxis) for patients with frequent/chronic migraines, usually 25 to 75 mg.
Unapproved/off-label/investigational use
Amitriptyline may be prescribed for other conditions such as insomnia, PTSD[3], migraine, rebound headache, chronic pain, chronic cough, postherpetic neuralgia (persistent pain following a shingles attack), carpal tunnel syndrome, fibromyalgia, vulvodynia, interstitial cystitis, male chronic pelvic pain syndrome, irritable bowel syndrome, diabetic peripheral neuropathy, neurological pain, and painful paresthesias related to multiple sclerosis and at low doses as a preventive (prophylaxis) for patients with frequent migraines.[4] Typically lower dosages are required for pain modification of 10 to 50 mg daily.[2]
Amitriptyline in low doses 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 that did not respond to a first-line treatment (famotidine or mosapride).[5]
Side effects
Common side effects of using amitriptyline are dry mouth, extreme weight gain, drowsiness, muscle stiffness, nausea, constipation, nervousness, dizziness, blurred vision and insomnia. Some rare side effects include tinnitus, hypotension, mania, psychosis, anticholinergic effects, heart block, arrhythmias, lip and mouth ulcers, extrapyramidal symptoms, depression, and hepatic toxicity.
Overdose
The symptoms and the treatment of an overdose are largely the same as for the other tricyclic antidepressants.
- Further information: Tricyclic antidepressant#Overdose
Footnotes
- ↑ Bendtsen L, Jensen R, Olesen J (September 1996). "A non-selective (amitriptyline), but not a selective (citalopram), serotonin reuptake inhibitor is effective in the prophylactic treatment of chronic tension-type headache". Journal of neurology, neurosurgery, and psychiatry 61 (3): 285–90. PMID 8795600.
- ↑ 2.0 2.1 British National Formulary 45 (March 2003).
- ↑ National Institute for Clinical Excellence: The Treatment of PTSD in Adults and Children
- ↑ Ziegler D, Hurwitz A, Hassanein R, Kodanaz H, Preskorn S, Mason J (1987). "Migraine prophylaxis. A comparison of propranolol and amitriptyline". Arch Neurol 44 (5): 486–9. PMID 3579659.
- ↑ Otaka M, Jin M, Odashima M, et al (June 2005). "New strategy of therapy for functional dyspepsia using famotidine, mosapride and amitriptyline". Aliment. Pharmacol. Ther. 21 (Suppl 2): 42–6. doi:. PMID 15943846. http://www.ingentaconnect.com/content/bsc/apt/2005/00000021/A00201s2/art00008.
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.
- AMITRIP Amitriptyline hydrochloride 10 mg, 25 mg and 50 mg Capsules Medsafe NZ Physician Data Sheet. November 2004.
- Endep Consumer Medicine Information, Australia. December 2005.
- MedlinePlus Drug Information: Amitriptyline. US National Institutes of Health. January 2008.
|
|||||||||||||||||||||||||||||||