|
|
|
|
|
Tacrine
drug data and news
Tacrine drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
|
| Generic name | Tacrine | ||
| Brand Names/Synonyms | CS 12602; Cognex; Romotal; THA; Tacrine; Tetrahydroaminacrine; Tetrahydroaminoacridine; Tetrahydroaminocrin; Tetrahydroaminocrine | ||
| Indication | For the treatment of mild to moderate dementia of the Alzheimer's type | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Tacrine is a parasympathomimetic, specifically, a reversible cholinesterase inhibitor. Tacrine is indicated for the treatment of mild to moderate dementia of the Alzheimer's type. Tacrine is postulated to exert its therapeutic effect by enhancing cholinergic function. This is accomplished by increasing the concentration of acetylcholine through reversible inhibition of its hydrolysis by acetylcholinesterase. If this proposed mechanism of action is correct, tacrine's effect may lessen as the disease process advances and fewer cholinergic neurons remain functionally intact. There is no evidence that tacrine alters the course of the underlying dementing process. | ||
| Mechanism Of Action | Tacrine acts by elevating acetylcholine concentrations in the cerebral cortex by slowing the degradation of acetylcholine released by still intact cholinergic neurons. It does so by reversibly binding acetylcholinesterase. | ||
| Tacrine News (When available) |
Full Social Lives May Protect Against Alzheimer's Apr 29, 2006 | ||
| Dosage Forms | Not Available | ||
| Drug_Category | Cholinesterase Inhibitors; Nootropic Agents; Parasympathomimetics; ATC:N06AA18; ATC:N06DA01 | ||
| Absorption | Tacrine is rapidly absorbed. Absolute bioavailability of tacrine is approximately 17 ± 13%. | ||
| Interactions | Interactions for Tacrine: Drug-Drug Interactions Possible metabolic basis for interactions: Tacrine is primarily eliminated by hepatic metabolism via cytochrome P450 drug metabolizing enzymes. Drug-drug interactions may occur when Cognex is given concurrently with agents such as theophylline that undergo extensive metabolism via cytochrome P450 IA2. Theophylline. Coadministration of tacrine with theophylline increased theophylline elimination half-life and average plasma theophylline concentrations by approximately 2-fold. Therefore, monitoring of plasma theophylline concentrations and appropriate reduction of theophylline dose are recommended in patients receiving tacrine and theophylline concurrently. The effect of theophylline on tacrine pharmacokinetics has not been assessed. Cimetidine. Cimetidine increased the Cmax and AUC of tacrine by approximately 54% and 64%, respectively. Anticholinergics. Because of its mechanism of action, Cognex has the potential to interfere with the activity of anticholinergic medications. Cholinomimetics and Cholinesterase Inhibitors. A synergistic effect is expected when Cognex is given concurrently with succinylcholine, cholinesterase inhibitors, or cholinergic agonists such as bethanechol. Fluvoxamine. In a study of 13 healthy, male volunteers, a single 40 mg dose of tacrine added to fluvoxamine 100 mg/day administered at steady-state was associated with five- and eight-fold increases in tacrine Cmax and AUC, respectively, compared to the administration of tacrine alone. Five subjects experienced nausea, vomiting, sweating, and diarrhea following coadministration, consistent with the cholinergic effects of tacrine. Other Interactions. Rate and extent of tacrine absorption were not influenced by the coadministration of an antacid containing magnesium and aluminum. Tacrine had no major effect on digoxin or diazepam pharmacokinetics or the anticoagulant activity of warfarin. | ||
| Toxicity | Not Available | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | 1,2,3,4-tetrahydroacridin-9-amine | ||
| Chemical Formula | C13H14N2 | ||
| Molecular Weight | 198.264 g/mol | ||
| Smiles String | C1CCC2=NC3=CC=CC=C3C(=C2C1)N | ||
| Melting Point | 183.5 °C | ||
| Water Solubility | 217 mg/L | ||
| State | Solid (white solid) | ||
| LogP/Hphobicity | 2.298 | ||
| Isoelectric Point | 9.95 | ||
| Biotransformation | Hepatic. Cytochrome P450 1A2 is the principal isozyme involved in tacrine metabolism. The major metabolite, 1-hydroxy-tacrine (velnacrine), has central cholinergic activity. | ||
| Half Life | 2 to 4 hours | ||
| Protein Binding [%] | 55% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Tacrine.html http://www.rxlist.com/cgi/generic2/tacrine.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00690 | ||
| CAS Registry Number | 321-64-2 | ||
| KEGG Compound ID | C01453 | ||
| PubChem ID | SID:4630 | ||
| PharmGKB ID | PA451576 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | Not Available |
|
Home | About | Cancers | Treatment | Medications Copyright onconews.org 2005. All Rights Reserved. |