TACRINE Brand Name: Cognex CHEMICAL STRUCTURE:. MECHANISM OF ACTION: a weak base. (Pka, 10). 1 st generation of cholinesterase inhibitors. It Blocks both.

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Presentation transcript:

TACRINE Brand Name: Cognex CHEMICAL STRUCTURE:

MECHANISM OF ACTION: a weak base. (Pka, 10). 1 st generation of cholinesterase inhibitors. It Blocks both acetyl+butyryl cholinesterase. At !nerve ending: (-)MAO,d.GABA,I ! release of: nor epinephrine,dopamine,serotonin. It became the 1 st compound approved for treatment of AD in 1993.

INDICATION: M. to Mod.

DOSING INFORMATION: 1. ADULT DOSAGE ORALLY 10\4 mg times\day * IMPORTANT NOTE Pt.>>> liver function tests; esp.(ALT). empty stomach>>>if stomach upset occurs, within meals.

C. MAXIMUM DOSE

DRUG INTERACTIONS: A.Interactions with Foods: abp. reduced. B.Smoking increases the elimination. C.Interaction with other Medicines Theophylline (Theo-Dur, Uniphyl) Cimetidine (Tagamet)

PHARMACOKINETICS: ADME 1.Absorption:. ORAL,capsules/solution Bioavailability 20% 2. DISTRIBUTION : TOTAL PTN. BINDING: 55% 3.METABOLISM: LIVER, extensive within minuets METABOLITES:1-hydroxy-tacrine(Velnacrine), active.

4. EXCRETION: 1. BREAST MILK: variable 2. RENAL EXCRETION: Less than 3% 5. HALF-LIFE: 2 to 4 hours.

PRECAUTIONS  Concurrent use of NSAIDs.  History of asthma, current liver disease, gastric ulcer disease.  Pre-existing conduction defects, [bradyarrythymias].

CONTRAINDICATIONS A. hypersensitivity to anti cholinesterase agent. B. tacrine-induced hepatotoixty

ADVERSE REACTIONS a. HEMATOLOGIC EFFECTS anemia,leukopenia,thrombocytopenia,pancytope nia. b. CARDIOVASCULAR EFFECTS Arrhythmias: arterial fibrillation\flutter, palpitations, tachycardia\BRADYCARDIA. MI and severe conduction defects, HYPOTENSION.

c.CNS: 1.DIZZINESS:most common CNS side effect+ATAXIA+INSOMNIA+TREMOR. confusion freq. lead to drug withdrawal. 3.DELIRIUM: characteristic of Cholinergic excess ( muscle stiffness, weakness, hyperreflexia, extra pyramidal signs, stupor, severe slowing on EEG ).

d. GASTROINTESTINAL EFFECTS N, V, ABD.DISCOMFORT, BELCHING, DIARRHEA, ANOREXIA [with oral tacrine and are dose-dependent]....HEPATOTOXICITY : significant dose-related elevations in liver function tests and Jaundice.

وجزاكم الله خير OHO