Results for tacrine
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tacrine

  (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.]


 
 
Drug Info: Tacrine

Brand names: Cognex®



Tacrine capsules

What are tacrine capsules?

TACRINE (Cognex®) helps treat the symptoms associated with Alzheimer's disease or dementia. It is not a cure for Alzheimer's disease but offers improvement in memory, attention, reason, language, and the ability to perform simple tasks. Benefits are greater for mild to moderate symptoms seen in the early stages of the disease. Generic tacrine capsules are not yet available.

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

They need to know if you have any of these conditions:
• asthma or other lung disease
• difficulty passing urine
• head injury
• heart disease, slow heartbeat
• jaundice
• liver disease
• low blood pressure
• Parkinson's disease
• seizures (convulsions)
• severe headaches
• 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 take this medicine?

Take tacrine capsules by mouth. Follow the directions on the prescription label. Swallow the capsules with a drink of water. It is best to take tacrine on an empty stomach, at least 1 hour before or 2 hours after meals. 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 your prescriber's advice.

Contact your pediatrician or health care professional regarding the use of this medicine in children. Special care may be needed.

What if I miss a dose?

If you miss a dose, take it as soon as you can. If it is almost time for your next dose, take only that dose, Do not take double or extra doses.

What drug(s) may interact with tacrine?

• atropine
• benztropine
• caffeine
• cimetidine
• dicyclomine
• digoxin
• donepezil
• doxercalciferol
• female hormones, like estrogens
• fluvoxamine
• galantamine
• glycopyrrolate
• guarana
• haloperidol
• ipratropium
• leflunomide
• medications for motion sickness (examples: dimenhydrinate, meclizine, scopolamine)
• medicines that relax your muscles for surgery
• methotrexate
• non-steroidal antiinflammatory drugs (NSAIDs, such as ibuprofen)
• oxybutynin
• propantheline
• ramelteon
• riluzole
• rivastigmine
• theophylline
• trihexyphenidyl
• warfarin
• zileuton

Tell your prescriber or health care professional about all other medicines you are taking, including non-prescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.

What should I watch for while taking tacrine?

Visit your prescriber or health care professional for regular checks on your progress. Your prescriber will need to regularly check your blood to monitor the effect of the medication on your liver. Check with your prescriber or health care professional if there is no improvement in your symptoms or if they get worse.

Avoid alcohol while you are taking tacrine. Alcohol may increase the risk of getting liver damage. Also try to avoid smoking. Smoking tobacco may lessen tacrine's effectiveness. Ask your prescriber or health care professional for ways to help you stop smoking or drinking.

Drinking too much caffeine may make you feel nervous or may give you nausea while on this medication. Try to avoid caffeinated beverages like coffee and colas whenever you can.

You may get dizzy or feel faint. Do not drive, use machinery, or do anything that needs mental alertness until you know how tacrine affects you.

If you are going to have surgery tell your prescriber or health care professional that you are taking tacrine.

What side effects may I notice from taking tacrine?

Side effects that you should report to your prescriber or health care professional as soon as possible:
• changes in vision or balance
• 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
• skin rash or hives
• 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 prescriber or health care professional if they continue or are bothersome):
• diarrhea
• dry mouth
• indigestion
• loss of appetite
• nausea

Where can I keep my medicine?

Keep out of reach of children in a container that small children cannot open.

Store at room temperature between 15 degrees and 30 degrees C (59 degrees and 86 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.

 
(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
Tacrine2.png
Tacrine3d.png
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
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

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.

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]

Other newer cholinesterase inhibitors, such as donepezil, are now preferred over tacrine.


Overdosage/Toxicity

As stated above, overdosage of tacrine may giva rise to severe side effects such as nausea, vomiting, salivation, sweating, bradycardia, hypotension, collapse, and colvulsions. 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


 
 

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Copyrights:

Dictionary. The American Heritage® Dictionary of the English Language, Fourth Edition Copyright © 2007, 2000 by Houghton Mifflin Company. Updated in 2007. 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 GNU Free Documentation License. It uses material from the Wikipedia article "Tacrine" Read more

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