RAZADYNE ER
Clinical safety rating: caution
Comprehensive clinical and safety monograph for RAZADYNE ER (RAZADYNE ER).
Reversible, competitive acetylcholinesterase inhibitor, increasing acetylcholine concentrations in the synaptic cleft of the central nervous system, particularly enhancing cholinergic neurotransmission in the cerebral cortex and hippocampus.
| Metabolism | Primarily metabolized by CYP2D6 and CYP3A4 to multiple metabolites; also undergoes glucuronidation. |
| Excretion | Renal: 95% as unchanged drug and metabolites; Fecal: 5% |
| Half-life | Terminal half-life approximately 7-8 hours; clinical context: supports twice-daily dosing |
| Protein binding | 18% bound to plasma proteins (primarily albumin) |
| Volume of Distribution | 1.1 L/kg; clinical meaning: indicates moderate tissue distribution |
| Bioavailability | Oral ER: 100% relative to immediate-release; absolute bioavailability 90-100% |
| Onset of Action | Oral: 30-60 minutes after a dose |
| Duration of Action | 12 hours; clinical notes: cognitive effects may require 2-4 weeks of therapy to manifest |
16 mg orally once daily in the morning; may increase to 24 mg once daily after minimum of 4 weeks; maximum dose 24 mg/day.
| Dosage form | CAPSULE, EXTENDED RELEASE |
| Renal impairment | CrCl 51-80 mL/min: no adjustment. CrCl 30-50 mL/min: maximum dose 16 mg/day. CrCl <30 mL/min: contraindicated. |
| Liver impairment | Child-Pugh A: maximum 16 mg/day. Child-Pugh B: maximum 16 mg/day. Child-Pugh C: not recommended. |
| Pediatric use | Not approved for use in pediatric patients. |
| Geriatric use | No specific dose adjustment required; monitor for adverse effects and tolerability. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for RAZADYNE ER (RAZADYNE ER).
| Breastfeeding | Not known if galantamine is excreted in human milk. M/P ratio not available. A decision should be made to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother. Galantamine is excreted in rat milk (concentrations 3 times maternal plasma). |
| Teratogenic Risk | Pregnancy Category B. Animal studies (rats, rabbits) at doses up to 16 and 22 times the maximum human dose (MHD) showed no evidence of fetal harm. However, no adequate, well-controlled studies in pregnant women. Use only if clearly needed. Potential for fetal acetylcholine receptor activation; risk may be increased in third trimester due to maternal cholinesterase inhibition. |
■ FDA Black Box Warning
No FDA black box warning.
| Common Effects | Diarrhea Stomach pain Dryness in mouth Headache Dizziness Flatulence Weakness Flu like symptoms |
| Serious Effects |
["Hypersensitivity to galantamine or any excipient","Severe hepatic impairment (Child-Pugh score >9)","Severe renal impairment (CrCl <9 mL/min)"]
| Precautions | ["Cardiovascular: bradycardia, heart block, syncope due to vagotonic effects","Gastrointestinal: nausea, vomiting, diarrhea, anorexia, weight loss","Genitourinary: urinary outflow obstruction","Neurologic: seizures, extrapyramidal symptoms","Pulmonary: exacerbation of asthma or COPD"] |
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| Fetal Monitoring | Monitor for excessive cholinergic effects (bradycardia, hypotension, seizures) in mother. Fetal monitoring: consider fetal heart rate monitoring if near term due to potential for uterine hyperstimulation (theoretical). No specific fetal monitoring guidelines. |
| Fertility Effects | No human fertility studies. In animal studies, no adverse effects on fertility or reproductive performance in rats at doses up to 16 mg/kg/day (about 16 times MHD). Galantamine may cause cholinergic side effects that could theoretically affect reproductive function. |