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tacrine

 
Dictionary: tac·rine   (tăk'rēn, -rĭn) pronunciation
n.
A drug that halts or reverses memory loss temporarily in some individuals with Alzheimer's disease, but does not alter the course of the disease.

[t(etrahydro)- (TETRA- + HYDRO-) + ACR(ID)INE.]


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Drug Info: Tacrine
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Brand names: Cognex®

Chemical formula:



Tacrine Hydrochloride Oral capsule

What is this medicine?

TACRINE (TAK reen) is used to treat mild to moderate dementia caused by Alzheimer's disease.
 
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:
•difficulty passing urine
•heart disease, slow heartbeat
•jaundice
•liver disease
•lung or breathing disease, like asthma
•seizures
•stomach or intestinal disease, ulcers or stomach bleeding
•an unusual or allergic reaction to tacrine, 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 glass of water. Follow the directions on the prescription label. It is best to take this medicine on an empty stomach, at least 1 hour before or 2 hours after meals. If this medicine upsets your stomach, you can take it with food. Take your doses at regular intervals. Do not take your medicine more often than directed. Continue to take your medicine even if you feel better. Do not stop taking except on the advice of your doctor or health care professional.

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?

•atropine
•benztropine
•cimetidine
•dicyclomine
•donepezil
•fluvoxamine
•galantamine
•glycopyrrolate
•ipratropium
•medicines for motion sickness like dimenhydrinate, meclizine, scopolamine
•medicines that relax your muscles for surgery
•NSAIDs, medicines for pain and inflammation, like ibuprofen or naproxen
•oxybutynin
•propantheline
•rivastigmine
•theophylline
•tolterodine
•trihexyphenidyl

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. Your doctor will need to regularly check your blood to monitor the effect of this medicine on your liver. Check with your doctor or health care professional if there is no improvement in your symptoms or if they get worse.

Avoid alcohol while you are taking this medicine. Alcohol may increase the risk of getting liver damage. Also try to avoid smoking. Smoking tobacco may lessen the effect of this medicine. Ask your doctor or health care professional for ways to help you stop smoking or drinking.

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.

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
•changes in vision
•dark yellow or brown urine
•diarrhea, if it is severe or does not stop
•dizziness, fainting spells, or falls
•increase in frequency of passing urine, or incontinence
•muscle pains
•nervousness, agitation, or increased confusion
•pain in the stomach or abdomen
•slow heartbeat, or palpitations
•sweating
•uncontrollable movements
•vomiting
•yellowing of 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):
•diarrhea
•dry mouth
•indigestion
•loss of appetite
•nausea

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 reach of children.

Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Protect from moisture. 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.

Medical Dictionary: tac·rine
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(tăk'rēn', -rĭn)
n.

Drug that halts or reverses memory loss temporarily in some individuals with Alzheimer's disease, but does not alter the course of the disease.

Wikipedia: Tacrine
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Tacrine
Systematic (IUPAC) name
1,2,3,4-tetrahydroacridin-9-amine
Identifiers
CAS number 321-64-2
ATC code N06AA18 N06DA01
PubChem 1935
DrugBank APRD00690
ChemSpider 1859
Chemical data
Formula C13H14N2 
Mol. mass 198.264 g/mol
Pharmacokinetic data
Bioavailability 2.4–36% (oral)
Protein binding 55%
Metabolism Hepatic (CYP1A2)
Half life 2–4 hours
Excretion Renal
Therapeutic considerations
Pregnancy cat.

C (Au), C (U.S.)

Legal status

S4 (Au), POM (UK), ℞-only (U.S.)

Routes Oral, rectal
 Yes check.svgY(what is this?)  (verify)

Tacrine is a parasympathomimetic and a centrally acting cholinesterase inhibitor (anticholinesterase). It was the first centrally-acting cholinesterase inhibitor approved for the treatment of Alzheimer's disease, and was marketed under the trade name Cognex. Tacrine was first synthesised by Adrien Albert at the University of Sydney.

Contents

Clinical use

Tacrine was the prototypical cholinesterase inhibitor for the treatment of Alzheimer's disease. Studies have found that it may have a small beneficial effect on cognition and other clinical measures, though adequate study data is limited and the clinical relevance of these findings is unclear.[1][2]

The use of tacrine is limited by poor oral bioavailability, the necessity for four-times daily dosing, and considerable adverse drug reactions (including nausea, diarrhea, urinary incontinence and hepatotoxicity) such that few patients could tolerate therapeutic doses.[3]

Overdosage/Toxicity

As stated above, overdosage of tacrine may give rise to severe side effects such as nausea, vomiting, salivation, sweating, bradycardia, hypotension, collapse, and convulsions. Tertiary anticholinergics, such as atropine, may be used as an antidote for overdose.

Major form of metabolism is in the liver via hydroxylation of benzylic carbon by CYP450. This forms the major metabolite 1-hydroxy-tacrine (velnacrine) which is still active.

References

  1. ^ Qizilbash N, Whitehead A, Higgins J, et al. Cholinesterase inhibition for Alzheimer disease: a meta-analysis of the tacrine trials. JAMA 1998;280(20):1777-82. PMID 9842955
  2. ^ Rang HP, Dale MM, Ritter JM, Moore PK. Pharmacology, 5th edition. Edinburgh: Churchill Livingstone; 2003.
  3. ^ Sweetman S, editor. Martindale: the complete drug reference, 34th ed. London: Pharmaceutical Press; 2004. ISBN 0-85369-550-4

See also


 
 
Learn More
Dementia: Alternative treatment
Tacrine Hydrochloride Oral capsule
Cholinesterase inhibitors

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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
Drug Info. Gold Standard. Copyright © 2008 by Gold Standard. All rights reserved.  Read more
Medical Dictionary. The American Heritage® Stedman's Medical Dictionary Copyright © 2002, 2001, 1995 by Houghton Mifflin Company Read more
Wikipedia. This article is licensed under the Creative Commons Attribution/Share-Alike License. It uses material from the Wikipedia article "Tacrine" Read more