May cause hypertension (including severe hypertensive syndromes) at recommended doses
May exacerbate hypertension; antihypertensive drugs may require dosage adjustment
May cause hypotension, especially orthostatic
May cause serotonin syndrome when used with antidepressants
Daytime drowsiness and somnolence reported during activities of daily living
May cause or exacerbate dyskinesia; decreasing the levodopa dose may lessen or eliminate this side effect
Hallucinations and psychotic-like behavior reported
Impulse control/compulsive behaviors reported; case reports describe patients with intense urges to gamble, increased sexual urges, intense urges to spend money, or binge eat
Withdrawal-emergent hyperpyrexia and confusion reported with rapid dose reduction of drugs that increase central dopaminergic tone; this is characterized by elevated temperature, muscular rigidity, altered consciousness, and autonomic instability
Lactation
There are no data on presence of drug in human milk or effects on breastfed infant; in rats, rasagiline was shown to inhibit prolactin secretion; the clinical relevance in humans is unknown, and there are no data on effects of rasagiline on prolactin secretion in humans
The developmental and health benefits of breastfeeding should be considered along with mother?s clinical need for therapy and potential adverse effects on breastfed infant from drug or from underlying maternal condition
Indication
Parkinson Disease
Contra Indication
Severe hepatic impairment. Concomitant use w/ other MAOIs and pethidine w/in 14 days after discontinuation of therapy; St John's wort.
FDA has not yet classified the drug into a specified pregnancy category.
Mode of Action
Rasagiline is a potent, irreversible monoamine oxidase (MAO)-B selective inhibitor which may cause an increase in extracellular levels of dopamine in the striatum, leading to reduced symptomatic motor deficits of Parkinson's disease.
Interaction
Increased plasma levels w/ potent CYP1A2 inhibitors (e.g. ciprofloxacin). Increased clearance w/ entacapone.
Potentially Fatal: Increased risk of non-selective MAO inhibition w/ other MAOIs and pethidine that may lead to hypertensive crises.
Pregnancy Category Note
Pregnancy
There are no adequate data on developmental risks associated with use in pregnant women; in animal studies, oral administration to rats during gestation and lactation resulted in decreased survival and reduced body weight in offspring at doses similar to those used clinically; when administered to pregnant animals in combination with levodopa/carbidopa, there were increased incidences of fetal skeletal variations in rats and increases in embryofetal death and cardiovascular abnormalities in rabbits
Lactation
There are no data on presence of drug in human milk or effects on breastfed infant; in rats, rasagiline was shown to inhibit prolactin secretion; the clinical relevance in humans is unknown, and there are no data on effects of rasagiline on prolactin secretion in humans
The developmental and health benefits of breastfeeding should be considered along with mother?s clinical need for therapy and potential adverse effects on breastfed infant from drug or from underlying maternal condition
Adult Dose
Parkinson Disease
Monotherapy: 1 mg PO qDay
Adjunct without levodopa: 1 mg PO qDay
Adjunct to levodopa: 0.5 mg PO qDay initially, may increase to 1 mg/day if needed and tolerated; consider reducing levodopa dose
Hepatic impairment
Mild (Child-Pugh A): Not to exceed 0.5 mg/day
Moderate-to-severe (Child-Pugh B/C): Do not use
Child Dose
<18 years: Safety and efficacy not established
Renal Dose
Renal impairment: No dosage adjustment required for mild-to-moderate; not studied in severe
Administration
May be taken with or without food. Avoid tyramine-rich foods, beverages or dietary supplements & amines (from cough/cold prep).
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