Names and pronunciation
(sa-fin′-a-mide) Xadago
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Drug reference
(sa-fin′-a-mide) Xadago
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Func. class.: Antiparkinson agent
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Chem. class.: MAO type B inhibitor
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ACTION: The precise mechanism of action is unknown; one mechanism may be related to its MAO-B inhibitory activity, which causes an increase in DOPamine levels centrally
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USES: For adjunctive treatment to levodopa-carbidopa therapy in patients with Parkinson’s disease experiencing “off” episodes
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CONTRAINDICATIONS: Hyper- sensitivity, MAOI therapy Precautions: Abrupt discontinuation, alcoholism, breastfeeding, pregnancy, cata- racts, use with CNS depressants, dental work, diabetic retinopathy, hypertension, hepatic disease, impulse control problems, psychosis, schizophrenia, surgery, uveitis
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SIDE EFFECTS CNS: Drowsiness, dyskinesia, insomnia, impulse control symptoms, neuroleptic malignant syndrome, psychosis, serotonin syndrome CV: Orthostatic hypotension MISC: Cough, dyspepsia, cataracts
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INTERACTIONS • Increase: severe somnolence—anxio- lytics, sedatives, hypnotics, barbiturates, ALPRAZolam, clonazePAM, zolpidem, za- leplon; avoid using together • Increase: hypertension, hypertensive crisis—MAOIs, linezolid; do not use within 14 days of these products • Increase: serotonin syndrome—meper- idine, some other opioids; SNRIs; tricyclic antidepressants and other cyclic antide- pressants; triazolopyridine antidepressants; cyclobenzaprine; stimulants (methylpheni- date, amphetamines), dextromethorphan; use the lowest dose of safinamide • Decrease: safinamide effects—atypi- cal antipsychotics
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DOSAGE AND ROUTES • Adult: PO Initially, 50 mg/day. May in- crease after 2 wk to 100 mg/day based on need and tolerability. Max 100 mg/day
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Available forms: Tabs 50, 100 mg
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Administer: • Give at same time each day; may be given with or without food • If a dose is missed, take the next dose at the usual time on the following day • Food and drug interactions with safin- amide can be serious. Patients should avoid foods/beverages containing large amounts of tyramine
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Assess: • Parkinson’s disease: assess for changes before and during treatment; tremors, pin-rolling, movement, balance, anxiety, drooling, depression, delusions, hallucinations, insomnia, shuffling gait; decreasing of “off” periods • Mental status: affect, depression, mood, complete suicide assessment • Hypertension: Monitor for new-onset hypertension or hypertension not ade- quately controlled after starting product; adjust dose if needed; monitor for hyper- tension if used with sympathomimetics • Drug interactions: review before use; there are many serious reactions • Impulse control: Assess for new or wors- ening impulse control symptoms (gam- bling, increased sexual urges, binge eating, intense urges to spend money, or other in- tense urges); if these occur, dose reduction or discontinuation may be needed • Hepatic disease: monitor LFTs base- line and periodically in those with he- patic disease • Neuroleptic malignant syndrome– like symptoms: elevated temperature, muscular rigidity, altered consciousness, and autonomic instability; may occur with rapid dose reduction • Serotonin syndrome: nausea, vomit- ing, sedation, dizziness, diaphoresis (sweating), facial flushing, mental status changes, myoclonus, restlessness, shiv- ering, and hypertension. If serotonin syn- drome occurs, any serotonergic agents should be discontinued • Pregnancy/breastfeeding: may cause fetal harm; use in pregnancy only if the potential benefit outweighs fetal risk; do not use in breastfeeding, serious adverse reactions may occur
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • Impulse control: that symptoms (gam- bling, increased sexual urges, binge eat- ing, intense urges to spend money, or other intense urges) may occur; to re- port to provider • Not to drive or engage in hazardous activities until effect of product is known; drowsiness may occur • To take B/P regularly • To change position slowly to prevent orthostatic hypotension • To use product as prescribed; if discon- tinued abruptly, neuroleptic malignant syndrome–like symptoms may occur; to taper gradually; to take at same time of day; to take with levodopa-carbidopa • To use physical activity to maintain mobility, lessen spasms • Serotonin syndrome: to report dry, hot skin; fever, agitation, delirium, diarrhea; to avoid use with other serotonergic products • To avoid use of tyramine-containing products; give list to patient • Pregnancy/breastfeeding: to report if pregnancy is planned or suspected or if breastfeeding See Appendix B
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PHARMACOKINETICS Not highly protein bound, excreted via kidneys 5% (unchanged), 76% recov- ered in the urine; half-life 20-26 hr, peak 2-3 hr; inhibits intestinal breast cancer resistance protein (BCRP)
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• Adult: PO Initially, 50 mg/day. May in- crease after 2 wk to 100 mg/day based on need and tolerability. Max 100 mg/day
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