Janssen; patent expires 2008.
Mild to moderate Alzheimer’s dementia.
Used off-label for both mild cognitive impairment and severe dementia.
Acetylcholinesterase inhibitor, stimulates nicotine receptors.
Immediate-release (IR): 4 mg white, 8 mg pink, 12 mg orange-brown tablets.
Extended-release (ER): 8 mg white, 16 mg pink, 24 mg orange-brown capsules.
Oral solution available in 4 mg/mL strength.
IR: start at 4 mg BID, increase to 8 mg BID after four weeks. If needed, increase to 12 mg BID after another 4 weeks.
ER: start at 8 mg QD, increase to 16 mg QD after four weeks. If needed, increase to 24 mg QD after another 4 weeks.
You may need to decrease the dose in both hepatic and renal impairment.
Most common: nausea, appetite loss, diarrhea.
FDA advisory noted a higher mortality rate in patients with mild cognitive impairment (MCI) taking Razadyne (1.5%) versus those randomly assigned to placebo (0.5%).
May aggravate stomach ulcers (potential class effect of all cholinesterase inhibitors).
Pregnancy risk category B.
Paxil and other 2D6 inhibitors may increase levels.
3A4 inducers such as Tegretol may decrease levels
Metabolized hepatically by P450 2D6 and 3A4.
Half-life 7 hours.
Most clinicians use the ER version exclusively because it can be dosed once a day.