safinamide

Contraindicated in:

Hypersensitivity;
Concurrent use of other MAO inhibitors;
Concurrent use of opioids, SNRIs, TCAs, cyclobenzaprine, methylphenidate, amphetamine, or St. John’s wort;
Concurrent use of dextromethorphan;
Severe hepatic impairment;
Psychotic disorder;
Lactation: Lactation.

Use Cautiously in:

Retinal disease;
Moderate hepatic impairment;
OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk;
Pedi: Safety and effectiveness not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

CV: hypertension, orthostatic hypotension

EENT: visual changes

GI: ↑liver enzymes, nausea

Neuro: dyskinesia, ↑fall risk, anxiety, drowsiness, hallucinations, impulse control disorders (gambling, sexual, binge eating), insomnia, paresthesia, psychosis, sleep attacks, sleep driving

Resp: cough

Misc: hypersensitivity reactions

Interactions ⬆ ⬇

Drug-drug:

MAO inhibitors, including linezolid and isoniazid, may ↑ risk of hypertensive crises; concurrent use contraindicated; separate administration by ≥14 days.
Meperidine, methadone, tramadol, SSRIs, SNRIs, TCAs, cyclobenzaprine, methylphenidate, or amphetamine may ↑ risk of serotonin syndrome; concurrent use contraindicated; separate administration by ≥14 days; SSRIs may be used at the lowest dose possible.
Dextromethorphan may result in psychosis/bizarre behavior; concurrent use contraindicated.
Hypertensive crisis may occur with cough and cold products containing sympathomimetic amines, including pseudoephedrine and phenylephrine; monitor patient’s BP closely.
May ↑ levels and risk of toxicity of imatinib, irinotecan, lapatinib, methotrexate, mitoxantrone, rosuvastatin, sulfasalazine, and topotecan; monitor closely for adverse effects.
Dopamine antagonists, including antipsychotics and metoclopramide, may ↓ effectiveness.

Drug-Natural Products:

St. John's wort may ↑ risk of serotonin syndrome; concurrent use contraindicated.

Drug-Food:

Ingestion of foods containing high amounts of tyramine (>150 mg) (e.g., cheese) may result in hypertensive crisis.

Availability ⬆ ⬇

(Generic available)

Tablets: 50 mg; 100 mg

Route/Dosage ⬆ ⬇

PO (Adults ): 50 mg once daily; after 2 wk, may ↑ dose to 100 mg once daily.

Hepatic Impairment

PO (Adults ): Moderate hepatic impairment: Do not exceed 50 mg/day; Severe hepatic impairment: Contraindicated.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Irreversibly inhibits monoamine oxidase B, which leads to ↑ dopamine levels in the CNS.

Therapeutic effects:

Increased amount of “on” time without dyskinesia or with nontroublesome dyskinesia.

Classifications ⬆ ⬇

Therapeutic Classification: antiparkinson agents

Pharmacologic Classification: monoamine oxidase type b inhibitors

Pharmacokinetics ⬆ ⬇

Absorption: 95% absorbed following oral administration.

Distribution: Extensively distributed to the tissues; readily crosses the blood-brain barrier.

Metabolism/Excretion: Extensively metabolized by hydrolytic oxidation or oxidative cleavage to inactive metabolites; 76% excreted in urine (primarily as inactive metabolites).

Half-Life: 20–26 hr.

Canadian Brand Names ⬆ ⬇

Time/Action Profile ⬆ ⬇

( plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	2–3 hr	24 hr

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication. Advise patient to read Patient Information before starting therapy.
Instruct patient to omit missed doses and to take next scheduled dose at usual time the following day. Do not double doses. Do not discontinue abruptly; may cause elevated temperature, muscular rigidity, altered consciousness, and autonomic instability.
Caution patient to avoid alcohol, CNS depressants, and foods or beverages containing tyramine (see Food Sources for Specific Nutrients) during and for ≥2 wk after therapy discontinued; they may precipitate a hypertensive crisis. Contact health care provider immediately if symptoms of hypertensive crisis or serotonin syndrome develop.
Instruct patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care provider before taking any new medications, including St. John’s wort, cough or cold products containing dextromethorphan, and the analgesics meperidine, tramadol, or methadone during therapy.
Inform patient that safinamide may cause falling asleep while engaged in activities of daily living, including the operation of motor vehicles, conversations, and eating. Notify health care provider if periods of daytime sleepiness occur.
Advise patient to notify health care provider if new or ↑ gambling, sexual, or other impulse control disorders or psychotic-like behaviors occur.
Advise patient to have regular ophthalmic exams during therapy and to notify health care provider if visual changes occur.
Rep: Advise women of reproductive potential to notify health care provider if pregnancy is planned or suspected or if breastfeeding.

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Indications ⬇

Contraind./Precautions ⬆ ⬇