Razadyne, Razadyne ER
Classifications: cholinesterase inhibitor; central acting; antidementia agent; Therapeutic: antialzheimer; antidementia; cholinesterase inhibitor
Prototype: Donezepril HCl
Pregnancy Category: B
4 mg, 8 mg, 12 mg tablets; 8 mg, 16 mg, 24 mg extended release capsules; 4 mg/mL oral solution
Competitive and reversible inhibitor of acetylcholinesterase which is the enzyme responsible for the hydrolysis (breakdown)
of the neurotransmitter, acetylcholine. The cholinergic system is known to be important in the processing needed for attention,
memory, and modulation of excitatory neurotransmission.
In Alzheimer's disease cholinesterase inhibitors are designed to offset loss of presynaptic cholinergic function, slowing
decline of memory and maintaining ability to perform functions of daily living.
Treatment of mild to moderate dementia of Alzheimer's type.
Hypersensitivity to galantamine. Not recommended with severe renal or hepatic impairment; lactation, or in children.
Bradycardia, heart block or other cardiac conduction disorders; asthma, COPD; potential bladder outflow obstruction; a history
of seizures or GI bleeding; concurrent use of drugs which slow the heart rate, drugs which may cause syncope, NSAIDs, or neuromuscular blocking agents during anesthesia, pregnancy (category B).
Route & Dosage
Adult: PO Initiate with 4 mg b.i.d. times at least 4 wks, if tolerated may increase by 4 mg b.i.d. q4wk to target dose of 12 mg b.i.d.
(816 mg b.i.d.)
Not recommended with severe hepatic impairment.
Clcr <9 mL/min: not recommended
- Give with meals (breakfast and dinner) to reduce the risk of nausea.
- Extended release capsules should be swallowed whole and not crushed or chewed.
- Make increases in dosage increments at 4-wk intervals.
- If drug is interrupted for several days or more, restart at the lowest dose and gradually increase to the current dose.
- Store at 15°30° C (59°86° F).
Adverse Effects (≥1%)Body as a Whole:
Weight loss, fatigue
, rhinitis, syncope, malaise, asthenia, fever. CNS:
Dizziness, headache, depression
, somnolence, tremor. CV:
Bradycardia, chest pain. GI: Nausea, vomiting,
diarrhea, anorexia, abdominal pain, dyspepsia, flatulence. Hematologic:
UTI, hematuria, incontinence. Nervous System:
Tinnitus, leg cramps. Other: Increased mortality in patients with mild cognitive impairment
Additive effects with other cholinesterase inhibitors
(e.g., succinylcholine, bethanecol
); cimetidine, erythromycin, ketoconazole, paroxetine
may increase levels and toxicity.
Rapidly and completely. Peak:
1 h. Distribution:
Mainly distributes to red blood cells. Metabolism:
In liver by CYP2D6 and CYP3A4. Elimination:
95% in urine. Half-Life:
7 h (4.410 h).
Assessment & Drug Effects
- Monitor cardiovascular status including baseline and periodic EKG and BP readings. Assess for postural hypotension.
- Monitor respiratory status; report worsening of preexisting asthma or COPD.
- Monitor I&O rates and pattern for urinary incontinence or urinary retention.
- Monitor appetite and food intake. Weigh weekly and report significant weight loss.
- Lab tests: Baseline ALT/AST, BUN and creatinine; periodic blood glucose, alkaline phosphatase, urinalysis, stool for occult
Patient & Family Education
- Report any of the following to a health care provider immediately: loss of weight, urinary retention, chest pain, palpitations,
difficulty breathing, fainting, dark stools, blood in the urine.