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tacrine (Cognex)

 

Classes: Acetylcholinesterase Inhibitors, Central

Dosing and uses of Cognex (tacrine)

 

Adult dosage forms and strengths

capsule

  • 10mg
  • 20mg
  • 30mg
  • 40mg

 

Alzheimer's Dementia

10-20 mg PO QID; no more than 160 mg/day

Monitor LFTs every other week from weeks 4-16, then q3Months

Take between meals, unless GI upset

 

Hepatic Impairment

LFTs >3-5x upper limit of normal, reduce dose to 10mg PO QID, monitor LFT's qWeek, resume dose titration and qoWeek monitoring when ALT return to normaL

LFT's >5x upper limit of normal, stop treatment monitor for symptom hepatitis, follow ALT until WNL's and rechallenge with initial dose 10 mg PO QID, monitor LFT's qweek, if after 6 weeks ALT wnl's may retry dose titration schedule, continue qweek ALT monitoring for 16 weeks then qmonths for 2 months then q3Months thereafter

 

Pediatric dosage forms and strengths

<18 years old: Safety & efficacy not established

 

Cognex (tacrine) adverse (side) effects

>10%

Incr LFT's (26-30%)

Nausea/vomiting (26-30%)

Diarrhea (15-20%)

Headache (11-15%)

Dizziness (11-15%)

 

1-10%

Dyspepsia (6-10%)

Anorexia (6-10%)

Abdominal pain (6-10%)

Myalgia (6-10%)

Confusion (6-10%)

Ataxia (6-10%)

Insomnia (6-10%)

Rhinitis (6-10%)

Rash (6-10%)

Fatigue (1-5%)

Weight loss (1-5%)

Constipation (1-5%)

Somnolence (1-5%)

Tremor (1-5%)

Anxiety (1-5%)

 

Warnings

Contraindications

Hypersensitivity

Drug-induced bilirubin >3 mg/dL [51.3 umol/L]

 

Pregnancy and lactation

Pregnancy category: C

Lactation: unknown

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Cognex (tacrine)

Half-Life: 2-4 hr

Peak Plasma Time: 1-2 hr

Bioavailability: 17%

Protein Bound: 55%

Vd: 349 L

Metabolism: hepatic P450 enzyme CYP1A2

Enzymes inhibited: CYP1A2

 

Mechanism of action

Centrally acting cholinesterase inhibitor