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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Results for tacrine
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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.]
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: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.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?
atropineWhat 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.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:Where can I keep my medicine?
Keep out of reach of children in a container that small children cannot open.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.
Drug that halts or reverses memory loss temporarily in some individuals with Alzheimer's disease, but does not alter the course of the disease.
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Tacrine
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| Systematic (IUPAC) name | |
| 1,2,3,4-tetrahydroacridin-9-amine | |
| Identifiers | |
| CAS number | |
| ATC code | N06 N06DA01 |
| PubChem | |
| DrugBank | |
| 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. | |
| 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.
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
Other newer cholinesterase inhibitors, such as donepezil, are now preferred over tacrine.
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.
| Anticholinesterases (N06DA, N07AA) | |
|---|---|
| Carbamates | Ambenonium - Demecarium - Stigmine (Neostigmine, Physostigmine, Pyridostigmine, Rivastigmine) |
| Other | Galantamine - Metrifonate - Donepezil - Tacrine - Edrophonium |
| Psychoanaleptics: anti-dementia drugs (N06D) | |
|---|---|
| Anticholinesterases | Tacrine - Donepezil - Rivastigmine - Galantamine |
| Other | NMDA receptor antagonist (Memantine) - Ginkgo biloba |
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