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amitriptyline

 
Dictionary: am·i·trip·tyl·ine   (ăm'ĭ-trĭp'tə-lēn') pronunciation

n.
A tricyclic antidepressant drug, C20H23N.

[Perhaps AMI(NO)- + alteration of TRYPT(OPHAN) + -YL + -INE2.]


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Oncology Encyclopedia:

Amitriptyline

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Definition

Amitriptyline is a medication used to treat various forms of depression, pain associated with the nerves (neuropathic pain), and to prevent migraine headaches. It is sold in the United States under the brand name Elavil.

Purpose

Amitriptyline helps relieve depression and pain. It is often used to manage nerve pain resulting from cancer treatment. Such injury to nerves causes a burning, tingling sensation. This medication, usually given at bedtime, helps patients sleep better.

Description

This medication is one of several tricyclic antidepressants. Amitriptyline acts to block reabsorption of chemicals that transmit nerve messages in the brain.

Recommended Dosage

Amitriptyline's usual adult dose for pain management is 10 mg to 150 mg at bedtime. Patients are generally started on a low dose. The amount of medication may be increased as needed. Side effects, such as a dry mouth and drowsiness, may make it difficult to increase the dose in older adults. Bedtime dosing helps the patient sleep. Doctors generally order 75 mg to 150 mg for depression. It is given at bedtime or in divided doses. It may take 30 days for the patient to feel less depressed. Pain relief is usually noticed sooner than the mood change. Teens and older adults usually receive a lower dose. If the nightly dose is missed, it should not be taken the next morning. Taking amitriptyline during waking hours could result in noticeable side effects. Patients should check with their doctor if the daily dose is missed. Those on more than one dose per day should take a missed dose as soon as it is noted. Patients should not take two doses at the same time. Injectable amitriptyline is available. It should not be used long-term. Patients should switch to tablets as soon as possible.

Precautions

Patients should not suddenly stop taking this medication. The dose should gradually be decreased, then discontinued. If the drug is abruptly stopped, the patient may experience headache, nausea, discomfort throughout the body, and a worsening of original symptoms. Amitriptyline's effects last for three to seven days after the medication has been stopped. Older adults usually are more prone to some side effects. These include drowsiness, dizziness, mental confusion, blurry vision, dry mouth, difficulty urinating, and constipation. Taking a lower dose may help resolve these problems. Patients may need to stop this medication before surgery.

Amitriptyline should not be given to anyone with allergies to the drug or to patients recovering from a heart attack. Patients taking MAO inhibitors, a different type of antidepressant, should not also use amitriptyline. It should be administered with caution to patients with glaucoma, seizures, urinary retention, an overactive thyroid, poor liver or kidney function, alcoholism, asthma, digestive disorders, an enlarged prostate, seizures, or heart disease. This medication should not be given to children under 12. Pregnant women should discuss the risks and benefits of this medication with their doctor. Fetal deformities have been associated with taking this drug during pregnancy. Women should not breastfeed while using amitriptyline.

Side Effects

Common side effects associated with amitriptyline include dry mouth, drowsiness, constipation, and dizziness or lightheadedness when standing. Patients can suck on ice cubes or sugarless hard candy to combat the dry mouth. Increased fiber in the diet and additional fluids may help the constipation. The dizziness is usually caused by a drop in blood pressure when changing position. Patients should slowly rise from a sitting or lying position if dizziness is noticed. Amitriptyline may increase the risk of falls in older adults. Patients should not drive or operate machinery or appliances while under the influence of this drug. Alcohol and other central nervous system depressants can increase drowsiness. Amitriptyline may also produce blurry vision and an irregular or fast heartbeat. Amitriptyline also may raise or lower blood pressure, or cause palpitations. This medication may increase or decrease diabetic patients' blood sugar levels. Amitriptyline may make patients' skin more sensitive to the sun. Patients should avoid direct sunlight, wear protective clothing, and apply sunscreen with a protective factor of 15 or higher.

Amitriptyline may increase appetite, cause weight gain, or produce an unpleasant taste in the mouth. It may also cause diarrhea, vomiting, or heartburn. Taking this medication with food may decrease digestive side effects. Other less likely side effects include muscle tremors, nervousness, impaired sexual function, sweating, rash, itching, hair loss, ringing in the ears, or changes in the make up of the patient's blood. Patients with schizophrenia may develop an increase in psychiatric symptoms.

Interactions

Patients should always tell all doctors and dentists that they are taking this medication. Amitriptyline may decrease the effectiveness of some drugs used to treat high blood pressure. Amitriptyline should not be taken with other antidepressants, epinephrine and other adrena-line-type drugs, or methylphenidate. Patients should not take over-the-counter medications without checking with their doctor. For instance, amitriptyline should not be taken with Tagamet (cimetidine) or Neo-Synephrine. Patients taking this drug should avoid the dietary supplements St. John's wort, belladonna, henbane and scopolia. Black tea may decrease the absorption of this drug. Patients should ingest the drug and tea at least two hours apart.

—Debra Wood, R.N.

 
Drug Info:

Amitriptyline

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Brand names: Elavil®Tryptanol™Vanatrip®

Chemical formula:



Amitriptyline Hydrochloride Oral tablet

What is this medicine?

AMITRIPTYLINE (a mee TRIP ti leen) is used to treat depression.
 
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
•an alcohol problem
•asthma, difficulty breathing
•bipolar disorder or schizophrenia
•difficulty passing urine, prostate trouble
•glaucoma
•heart disease or previous heart attack
•liver disease
•over active thyroid
•seizures
•thoughts or plans of suicide, a previous suicide attempt, or family history of suicide attempt
•an unusual or allergic reaction to amitriptyline, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding

How should I use this medicine?

Take this medicine by mouth with a drink of water. Follow the directions on the prescription label. You can take the tablets with or without food. Take your medicine at regular intervals. Do not take it more often than directed. If you have been taking this medicine regularly for some time, do not suddenly stop taking it. You must gradually reduce the dose or you may get severe side effects. Ask your doctor or health care professional for advice. Even after you stop taking this medicine it can still affect your body for several days.

A special MedGuide will be given to you by the pharmacist with each prescription and refill. Be sure to read this information carefully each time.

Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.

What may interact with this medicine?

Do not take this medicine with any of the following medications:
•arsenic trioxide
•certain medicines used to regulate abnormal heartbeat or to treat other heart conditions
•cisapride
•droperidol
•halofantrine
•MAOIs like Carbex, Eldepryl, Marplan, Nardil, and Parnate
•other medicines for mental depression
•phenothiazines like perphenazine, thioridazine and chlorpromazine
•pimozide
•probucol
•procarbazine
•sparfloxacin
•St. John's Wort
•ziprasidone

This medicine may also interact with the following medications:
•atropine and related drugs like hyoscyamine, scopolamine, tolterodine and others
•barbiturate medicines for inducing sleep or treating seizures, like phenobarbital
•cimetidine
•disulfiram
•ethchlorvynol
•thyroid hormones such as levothyroxine

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

Visit your doctor or health care professional for regular checks on your progress. It can take several days before you feel the full effect of this medicine.

Patients and their families should watch out for worsening depression or thoughts of suicide. Also watch out for sudden or severe changes in feelings such as feeling anxious, agitated, panicky, irritable, hostile, aggressive, impulsive, severely restless, overly excited and hyperactive, or not being able to sleep. If this happens, especially at the beginning of antidepressant treatment or after a change in dose, call your health care professional.

You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol may increase dizziness and drowsiness. Avoid alcoholic drinks.

Do not treat yourself for coughs, colds, or allergies without asking your doctor or health care professional for advice. Some ingredients can increase possible side effects.

Your mouth may get dry. Chewing sugarless gum or sucking hard candy, and drinking plenty of water will help.

This medicine may cause dry eyes and blurred vision. If you wear contact lenses you may feel some discomfort. Lubricating drops may help. See your eye doctor if the problem does not go away or is severe.

This medicine can make you more sensitive to the sun. Keep out of the sun. If you cannot avoid being in the sun, wear protective clothing and use sunscreen. Do not use sun lamps or tanning beds/booths.

If you are diabetic, check your blood sugar more often than usual, especially during the first few weeks of treatment with this medicine. This medicine can affect blood sugar levels. Call your doctor or health care professional for advice if you notice a change in the results of blood or urine glucose tests.

What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:
•allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
•abnormal production of milk in females
•breast enlargement in both males and females
•breathing problems
•confusion, hallucinations
•fast, irregular heartbeat
•fever with increased sweating
•muscle stiffness, or spasms
•pain or difficulty passing urine, loss of bladder control
•seizures
•suicidal thoughts or other mood changes
•swelling of the testicles
•tingling, pain, or numbness in the feet or hands
•yellowing of the eyes or skin

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•change in sex drive or performance
•constipation or diarrhea
•nausea, vomiting
•weight gain or loss

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medicine?

Keep out of the reach of children.

Store at room temperature between 20 and 25 degrees C (68 and 77 degrees F). Throw away any unused medicine after the expiration date.

Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

 
Veterinary Dictionary:

amitriptyline

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A tricyclic antidepressant in humans; used in dogs and cats to treat psychodermatosis and as an antipruritic.

 
 
Wikipedia:

Amitriptyline

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Amitriptyline
Systematic (IUPAC) name
3-(10,11-dihydro-5H-dibenzo[[a,d]]cycloheptene-5-ylidene)-N,N-dimethyl-1-propanamine
Identifiers
CAS number 50-48-6
ATC code N06AA09
PubChem CID 2160
IUPHAR ligand ID 200
DrugBank APRD00227
ChemSpider 2075
Chemical data
Formula C20H23N 
Mol. mass 277.403 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability 30–60% due to first pass metabolism
Protein binding > 90%
Metabolism Hepatic
CYP2C19, CYP1A2, CYP2D6
Half-life 10–50 hours, with an average of 15 hours
Excretion Renal
Therapeutic considerations
Pregnancy cat. D(US)
Legal status Prescription only
Routes Oral
 YesY(what is this?)  (verify)

Amitriptyline (Elavil, Tryptizol, Laroxyl, Sarotex, Lentizol) is a tricyclic antidepressant (TCA).[1] It is the most widely used TCA and has at least equal efficacy against depression as the newer class of SSRIs.[citation needed]

Contents

History

Amitriptyline, under the brand name Elavil, was developed by Merck and approved by the FDA on April 7, 1961 for the treatment of major depression in the United States.[2] It has seen widespread usage throughout the world ever since.

Indications

Approved

Amitriptyline is approved for the treatment of major depression, as well as clinical/endogenous depression and also involutional melancholia or "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 dose initially for elderly or adolescent patients.

Children between the ages of 7 to 10 years typically have 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 three months.[3]

Amitriptyline is used in ankylosing spondylitis for pain relief and in some European countries it is officially approved as a preventive for patients with frequent/chronic migraines, usually 25 to 75 mg. It is also used as a preventive for patients with recurring biliary dyskinesia (sphincter of Oddi dysfunction), usually 10 mg daily[4].

Unapproved/off-label

Amitriptyline may be prescribed for other conditions such as insomnia, post-traumatic stress disorder (PTSD),[5] migraine, rebound headache, chronic pain, tinnitus, chronic cough, postherpetic neuralgia (persistent pain following a shingles attack), carpal tunnel syndrome (CTS), fibromyalgia, vulvodynia, interstitial cystitis, male chronic pelvic pain syndrome, irritable bowel syndrome (IBS), diabetic peripheral neuropathy, neurological pain, laryngeal sensory neuropathy, and painful paresthesias related to multiple sclerosis and at low doses as a prophylaxis (preventive) for patients with chronic migraines.[6] Typically lower dosages are required for pain modification of 10 to 50 mg daily.[3]

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.[citation needed] Additionally, Amitriptyline is often used to relieve the pain of the Herpes Zoster virus, typically at a dose of between 10–20 mg at night.[citation needed]

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).[7]

Pharmacology

Amitriptyline acts primarily as a serotonin-norepinephrine reuptake inhibitor, with strong actions on the norepinephrine transporter, and moderate effects on the serotonin transporter.[8][9] It has negligible influence on the dopamine transporter and therefore does not affect dopamine reuptake, being nearly 1,000 times weaker on it than on serotonin.[9]

Amitriptyline additionally functions as a 5-HT2A, 5-HT2C, 5-HT6, 5-HT7, α1-adrenergic, H1, and mACh receptor antagonist, and σ1 receptor agonist.[10][11][12][13] It has also been shown to be a relatively weak NMDA receptor negative allosteric modulator at the same binding site as phencyclidine.[14] Amitriptyline inhibits sodium channels, L-type calcium channels, and Kv1.1, Kv7.2, and Kv7.3 voltage-gated potassium channels, and therefore acts as a sodium, calcium, and potassium channel blocker as well.[15][16][17]

Recently, amitriptyline has been demonstrated to act as an agonist of the TrkA and TrkB receptors.[18] It promotes the heterodimerization of these proteins in the absence of NGF and has potent neurotrophic activity both in-vivo and in-vitro in mouse models.[18]

Side effects

Common side effects of using amitriptyline are mostly due to its anticholinergic activity, including: weight gain, dry mouth, changes in appetite, drowsiness, muscle stiffness, nausea, constipation, nervousness, dizziness, blurred vision, urinary retention, insomnia and changes in sexual function. Some rare side effects include tinnitus, hypotension, mania, psychosis, sleep paralysis, hypnagogia, hypnopompia, 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 TCAs.

See also

References

  1. ^ Barbui C, Hotopf M (February 2001). "Amitriptyline v. the rest: still the leading antidepressant after 40 years of randomised controlled trials". The British Journal of Psychiatry : the Journal of Mental Science 178: 129–44. doi:10.1192/bjp.178.2.129. PMID 11157426. http://bjp.rcpsych.org/cgi/pmidlookup?view=long&pmid=11157426. 
  2. ^ Fangmann P, Assion HJ, Juckel G, González CA, López-Muñoz F (February 2008). "Half a century of antidepressant drugs: on the clinical introduction of monoamine oxidase inhibitors, tricyclics, and tetracyclics. Part II: tricyclics and tetracyclics". Journal of Clinical Psychopharmacology 28 (1): 1–4. doi:10.1097/jcp.0b013e3181627b60. PMID 18204333. http://meta.wkhealth.com/pt/pt-core/template-journal/lwwgateway/media/landingpage.htm?issn=0271-0749&volume=28&issue=1&spage=1. 
  3. ^ a b British National Formulary 45 (March 2003).
  4. ^ S. G. Hubscher et al. (2006). Functional biliary type pain syndrome. In P. J. Pasricha, W. D. Willis & G. F. Gebhart (Eds.), ' ' italics' ' Chronic Abdominal and Visceral Pain' 'italics' '. London: Informa Healthcare, pp. 459-461.
  5. ^ National Institute for Clinical Excellence: The Treatment of PTSD in Adults and Children
  6. ^ 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. 
  7. ^ 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:10.1111/j.1365-2036.2005.02473.x. PMID 15943846. http://www.ingentaconnect.com/content/bsc/apt/2005/00000021/A00201s2/art00008. 
  8. ^ http://www.cnsforum.com/content/pictures/imagebank/hirespng/antidep_uptake_specific.png
  9. ^ a b Tatsumi; Groshan, K; Blakely, RD; Richelson, E (1997). "Pharmacological profile of antidepressants and related compounds at human monoamine transporters". European journal of pharmacology 340 (2-3): 249–58. doi:10.1016/S0014-2999(97)01393-9. PMID 9537821.  edit
  10. ^ Owens; Morgan, WN; Plott, SJ; Nemeroff, CB (1997). "Neurotransmitter receptor and transporter binding profile of antidepressants and their metabolites". The Journal of pharmacology and experimental therapeutics 283 (3): 1305–22. PMID 9400006.  edit
  11. ^ Alan F. Schatzberg, Charles B. (2006). Essentials of clinical psychopharmacology. American Psychiatric Pub. p. 7. ISBN 1585622435, 9781585622436. 
  12. ^ Rauser; Savage, JE; Meltzer, HY; Roth, BL (2001). "Inverse agonist actions of typical and atypical antipsychotic drugs at the human 5-hydroxytryptamine(2C) receptor". The Journal of pharmacology and experimental therapeutics 299 (1): 83–9. PMID 11561066.  edit
  13. ^ Werling; Keller, A.; Frank, J.; Nuwayhid, S. (2007). "A comparison of the binding profiles of dextromethorphan, memantine, fluoxetine and amitriptyline: treatment of involuntary emotional expression disorder". Experimental neurology 207 (2): 248–257. doi:10.1016/j.expneurol.2007.06.013. PMID 17689532.  edit
  14. ^ Sills; Loo, PS (1989). "Tricyclic antidepressants and dextromethorphan bind with higher affinity to the phencyclidine receptor in the absence of magnesium and L-glutamate". Molecular pharmacology 36 (1): 160–5. PMID 2568580.  edit
  15. ^ Pancrazio; Kamatchi, GL; Roscoe, AK; Lynch C, 3rd (1998). "Inhibition of neuronal Na+ channels by antidepressant drugs". The Journal of pharmacology and experimental therapeutics 284 (1): 208–14. PMID 9435180.  edit
  16. ^ Zahradnik, I.; Minarovic, I.; Zahradnikova, A. (2008). "Inhibition of the cardiac L-type calcium channel current by antidepressant drugs". The Journal of pharmacology and experimental therapeutics 324 (3): 977–984. doi:10.1124/jpet.107.132456. PMID 18048694.  edit
  17. ^ Punke MA, Friederich P (May 2007). "Amitriptyline is a potent blocker of human Kv1.1 and Kv7.2/7.3 channels". Anesthesia and Analgesia 104 (5): 1256–64, tables of contents. doi:10.1213/01.ane.0000260310.63117.a2. PMID 17456683. http://www.anesthesia-analgesia.org/cgi/pmidlookup?view=long&pmid=17456683. 
  18. ^ a b Jang; Liu, X.; Chan, C.; Weinshenker, D.; Hall, R.; Xiao, G.; Ye, K. (2009). "Amitriptyline is a TrkA and TrkB receptor agonist that promotes TrkA/TrkB heterodimerization and has potent neurotrophic activity". Chemistry & biology 16 (6): 644–656. doi:10.1016/j.chembiol.2009.05.010. PMID 19549602.  edit

Further reading


 
 

 

Copyrights:

Dictionary. The American Heritage® Dictionary of the English Language, Fourth Edition Copyright © 2007, 2000 by Houghton Mifflin Company. Updated in 2009. Published by Houghton Mifflin Company. All rights reserved.  Read more
Oncology Encyclopedia. Gale Encyclopedia of Cancer. Copyright © 2006 by The Gale Group, Inc. All rights reserved.  Read more
Drug Info. Gold Standard. Copyright © 2008 by Gold Standard. All rights reserved.  Read more
Veterinary Dictionary. Saunders Comprehensive Veterinary Dictionary 3rd Edition. Copyright © 2007 by D.C. Blood, V.P. Studdert and C.C. Gay, Elsevier. All rights reserved.  Read more
Wikipedia. This article is licensed under the Creative Commons Attribution/Share-Alike License. It uses material from the Wikipedia article Amitriptyline Read more

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