Trade Names:Razadyne- Tablets 4 mg (as base)- Tablets 8 mg (as base)- Tablets 12 mg (as base)- Oral Solution 4 mg/mL
Trade Names:Razadyne ER- Capsules, extended-release 8 mg (as base)- Capsules, extended-release 16 mg (as base)- Capsules, extended-release 24 mg (as base)
Reminyl (Canada)Reminyl ER (Canada)May enhance cholinergic function by increasing acetylcholine.
Absolute bioavailability is about 90%. T max is about 1 h. Food decreases C max 25% and delayed T max 1.5 h.
Mean Vd is 175 L. Protein binding is 18%.
Metabolized by hepatic CYP-450 2D6 and 3A4 enzymes and glucuronidated.
T ½ is about 7 h. Approximately 95% is excreted in urine and 5% in feces.
AUC increased 37% and 67% in moderate and severe renal function impairment.
Hepatic Function ImpairmentCl decreased about 25% in moderate (Child-Pugh 7 to 9) hepatic function impairment.
ElderlyConcentrations are about 30% to 40% higher.
GenderCl is about 20% lower in women than in men.
CYP2D6 poor metabolizersApproximately 35% increase in AUC of unchanged drug and 25% decrease in median Cl.
Treatment of mild to moderate dementia of the Alzheimer type.
Standard considerations.
In patients with moderately impaired hepatic function (Child-Pugh score 7 to 9) and those with moderate renal function impairment, the dose should not exceed 16 mg/day. Not recommended for patients with severe renal (CrCl less than 9 mL/min) or severe hepatic function impairment (Child-Pugh 10 to 15).
Immediate-Release Tablets and Oral SolutionAdultsPO 4 mg twice daily. May increase to 8 mg twice daily after 4 wk. A further increase to 12 mg twice daily may be attempted after min 4 wk at previous dose.
Extended-Release TabletsAdultsPO 8 mg/day. Increase to 16 mg/day after min 4 wk. A further increase to 24 mg/day may be attempted after min 4 wk at previous dose.
Store at controlled room temperature (59° to 86°F). Do not freeze oral solution.
May act synergistically with galantamine.
CYP2D6 inhibitors (eg, amitriptyline, fluoxetine, fluvoxamine, quinidine)May decrease galantamine Cl.
Erythromycin; ketoconazole; paroxetineMay elevate galantamine levels, increasing the risk of adverse reactions.
None well documented.
Chest pain, hypertension (at least 2%); bradycardia, syncope (2%).
Dizziness, somnolence (9%); headache (8%); depression (7%); fatigue, insomnia (5%); tremor (3%); agitation, anxiety, confusion, hallucinations (at least 2%).
Purpura (at least 2%).
Nausea (24%); vomiting (13%); diarrhea (12%); anorexia (9%); abdominal pain, dyspepsia (5%); constipation (at least 2%); flatulence (at least 1%).
UTI (8%); hematuria (3%); urinary incontinence (at least 2%).
Anemia (3%).
Weight decrease (7%).
Rhinitis (4%); bronchitis, coughing, upper respiratory tract infection (at least 2%).
Asthenia, back pain, falling, injury, peripheral edema (at least 2%).
Category B .
Undetermined.
Safety and efficacy not established.
Use with caution in patients with moderately impaired function; not recommended in severe impairment.
Use with caution in patients with moderately impaired function; not recommended in severe impairment.
May occur.
May cause bradycardia and/or AV block. All patients should be considered at risk for adverse reactions or cardiac conditions.
The beneficial effects of galantamine are lost when the drug is discontinued.
May increase gastric acid secretion.
Use with caution in patients with a history of severe asthma or obstructive pulmonary disease.
May cause generalized convulsions.
Cholinergic crisis (eg, bradycardia, collapse, convulsions, defecation, GI cramping, hypotension, lacrimation, muscle weakness, respiratory depression, salivation, severe nausea, sweating, urination, vomiting).
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