Cognex
Cognex - General Information
A cholinesterase inhibitor that crosses the blood-brain barrier. Cognex has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer&
Pharmacology of Cognex
Cognex is a parasympathomimetic, specifically, a reversible cholinesterase inhibitor. Cognex is indicated for the treatment of mild to moderate dementia of the Alzheimer's type. Cognex 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.
Cognex for patients
Cognex Interactions
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.
Cognex Contraindications
Cognex® is contraindicated in patients with known hypersensitivity to tacrine or acridine derivatives.
Cognex® is contraindicated in patients previously treated with Cognex® who developed treatment-associated jaundice: a serum bilirubin >3 mg/dL; and/or those exhibiting clinical signs or symptoms of hypersensitivity (eg, rash or fever) in association with ALT/SGPT elevations.
Additional information about Cognex
Cognex Indication: For the treatment of mild to moderate dementia of the Alzheimer's type.
Mechanism Of Action: Cognex 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.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Tacrine
Synonyms: Tetrahydroaminacrine; Tetrahydroaminoacridine; Tetrahydroaminocrin; Tetrahydroaminocrine; THA
Drug Category: Cholinesterase Inhibitors; Nootropic Agents; Parasympathomimetics
Drug Type: Small Molecule; Approved
Other Brand Names containing Tacrine: Cognex; Romotal;
Absorption: Tacrine is rapidly absorbed. Absolute bioavailability of tacrine is approximately 17 ± 13%.
Toxicity (Overdose): Overdosage with cholinesterase inhibitors can cause a cholinergic crisis characterized by severe nausea/vomiting, salivation, sweating, bradycardia, hypotension, collapse, and convulsions. Increasing muscle weakness is a possibility and may result in death if respiratory muscles are involved. The estimated median lethal dose of tacrine following a single oral dose in rats is 40 mg/kg, or approximately 12 times the maximum recommended human dose of 160 mg/day.
Protein Binding: 55%
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
Dosage Forms of Cognex: Capsule Oral
Chemical IUPAC Name: 1,2,3,4-tetrahydroacridin-9-amine
Chemical Formula: C13H14N2
Tacrine on Wikipedia: https://en.wikipedia.org/wiki/Tacrine
Organisms Affected: Humans and other mammals
