rasagiline

Contraindicated in:

Hypersensitivity;
Concurrent use of meperidine, tramadol, methadone, or another MAO inhibitor;
Moderate to severe hepatic impairment;
Elective surgery requiring general anesthesia;
Pheochromocytoma;
Psychotic disorder.

Use Cautiously in:

Mild hepatic impairment;
OB: Safety not established in pregnancy;
Lactation: Safety not established in breastfeeding;
Pedi: Safety and effectiveness not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

CV: orthostatic hypotension (may ↑ levodopa-induced hypotension), ↑BP, chest pain, syncope

Derm: alopecia, ecchymosis, MELANOMA, rash

EENT: conjunctivitis, rhinitis

GI: anorexia, dizziness, dyspepsia, gastroenteritis, vomiting

GU: ↓libido, albuminuria

Hemat: leukopenia

Metab: weight loss

MS: arthralgia, arthritis, neck pain

Neuro: depression, dizziness, drowsiness, dyskinesia (may ↑ levodopa-induced dyskinesia), hallucinations, impulse control disorders (gambling, sexual), malaise, paresthesia, sleep driving, vertigo

Resp: asthma

Misc: fever, flu-like syndrome

Interactions ⬆ ⬇

Drug-drug:

Meperidine, tramadol, methadone, or other MAO inhibitors may ↑ risk of serotonin syndrome; concurrent use contraindicated.
CYP1A2 inhibitors, including ciprofloxacin, may ↑ levels and risk of toxicity; dose adjustment recommended.
Dextromethorphan may ↑ risk of psychosis/bizarre behavior; avoid concurrent use.
↑risk of adverse reactions with mirtazapine and cyclobenzapine; avoid concurrent use.
Hypertensive crisis may occur with sympathomimetic amines, including amphetamines, pseudoephedrine, phenylephrine, or ephedrine; avoid concurrent use.
↑risk of serotonin syndrome with tricyclic antidepressants, SSRIs, and SNRIs; rasagiline should be discontinued ≥14 days prior to initiation of antidepressants (fluoxetine should be discontinued ≥5 wk prior to rasagiline therapy).

Drug-Natural Products:

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

Drug-Food:

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

Availability ⬆ ⬇

(Generic available)

Tablets: 0.5 mg; 1 mg

Route/Dosage ⬆ ⬇

PO (Adults ): Monotherapy or as adjunct therapy in patients not taking levodopa: 1 mg once daily; Concurrent levodopa therapy: 0.5 mg once daily; may ↑ to 1 mg once daily; Concurrent use of ciprofloxacin or other CYP1A2 inhibitors: 0.5 mg once daily.

Hepatic Impairment

PO (Adults ): Mild hepatic impairment: 0.5 mg once daily.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Irreversibly inactivates monoamine oxidase (MAO) by binding to it at type B (brain sites); inactivation of MAO leads to increased amounts of dopamine available in the CNS.
Differs from selegiline by its nonamphetamine characteristics.

Therapeutic effects:

Improvement in symptoms of Parkinson disease, allowing increase in function.

Classifications ⬆ ⬇

Therapeutic Classification: antiparkinson agents

Pharmacologic Classification: monoamine oxidase type b inhibitors

Pharmacokinetics ⬆ ⬇

Absorption: 36% absorbed following oral administration.

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

Metabolism/Excretion: Extensively metabolized by the liver primarily by the CYP1A2 isoenzyme to an inactive metabolite; <1% excreted in urine.

Half-Life: 1.3 hr; does not correlate with duration of MAO-B inhibition.

Time/Action Profile ⬆ ⬇

ROUTE	ONSET	PEAK	DURATION
PO	rapid	1 hr	40 days*

*Recovery of MAO-B function.

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 take next dose as scheduled the following day. Do not double doses or discontinue abruptly; may cause ↑ 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 has been discontinued; they may precipitate a hypertensive crisis. Instruct patient to contact health care provider immediately if symptoms of hypertensive crisis (chest pain, tachycardia, bradycardia, severe headache, stiff/sore, nausea, vomiting, sweating, photosensitivity, enlarged pupils) or serotonin syndrome (mental changes [agitation, hallucinations, coma], autonomic instability, hyperreflexia, incoordination, nausea, vomiting, diarrhea) occur.
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. Caution patient to avoid use of St. John's wort and analgesics meperidine, tramadol, or methadone during therapy.
Caution patient to avoid elective surgery requiring general anesthesia, cocaine, or local anesthesia containing sympathomimetic vasoconstrictors within 14 days of discontinuing rasagiline. If surgery is necessary sooner, benzodiazepines, rocuronium, fentanyl, morphine, and codeine may be used cautiously.
Caution patient to change positions slowly to minimize orthostatic hypotension. Older adults are at ↑ risk.
Caution patient to notify health care provider if new agitation; aggression; delirium; hallucinations; or new or ↑ gambling, sexual, or other intense urges occur.
Inform patient that rasagiline 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 immediately if severe headache, neck stiffness, heart racing, or palpitations occur.
Rep: Advise women of reproductive potential to notify health care providers if pregnancy is planned or suspected or if breastfeeding.

Pronunciation ⬆ ⬇

Code ⬆

NDC Code

0093- Teva Pharmaceuticals USA, Inc.
- 0093-3060- Rasagiline
  - 0093-3060-56- 30 TABLET in 1 BOTTLE (0093-3060-56)

0093- Teva Pharmaceuticals USA, Inc.
- 0093-3061- Rasagiline
  - 0093-3061-56- 30 TABLET in 1 BOTTLE (0093-3061-56)

16714- NorthStar RxLLC
- 16714-770- Rasagiline
  - 16714-770-01- 30 TABLET in 1 BOTTLE (16714-770-01)

16714- NorthStar RxLLC
- 16714-771- Rasagiline
  - 16714-771-01- 30 TABLET in 1 BOTTLE (16714-771-01)

33342- Macleods Pharmaceuticals Limited
- 33342-308- Rasagiline
  - 33342-308-07- 30 TABLET in 1 BOTTLE (33342-308-07)

33342- Macleods Pharmaceuticals Limited
- 33342-309- Rasagiline
  - 33342-309-07- 30 TABLET in 1 BOTTLE (33342-309-07)

42571- Micro Labs Limited
- 42571-220- RASAGILINE
  - 42571-220-05- 500 TABLET in 1 BOTTLE (42571-220-05)

42571- Micro Labs Limited
- 42571-220- RASAGILINE
  - 42571-220-10- 1000 TABLET in 1 BOTTLE (42571-220-10)

42571- Micro Labs Limited
- 42571-220- RASAGILINE
  - 42571-220-30- 30 TABLET in 1 BOTTLE (42571-220-30)

42571- Micro Labs Limited
- 42571-221- RASAGILINE
  - 42571-221-05- 500 TABLET in 1 BOTTLE (42571-221-05)

42571- Micro Labs Limited
- 42571-221- RASAGILINE
  - 42571-221-10- 1000 TABLET in 1 BOTTLE (42571-221-10)

42571- Micro Labs Limited
- 42571-221- RASAGILINE
  - 42571-221-30- 30 TABLET in 1 BOTTLE (42571-221-30)

47781- Alvogen, Inc.
- 47781-683- Rasagiline
  - 47781-683-30- 30 TABLET in 1 BOTTLE, PLASTIC (47781-683-30)

47781- Alvogen, Inc.
- 47781-690- Rasagiline
  - 47781-690-30- 30 TABLET in 1 BOTTLE, PLASTIC (47781-690-30)

62135- Chartwell RX, LLC
- 62135-676- Rasagiline
  - 62135-676-30- 30 TABLET in 1 BOTTLE (62135-676-30)

62135- Chartwell RX, LLC
- 62135-677- Rasagiline
  - 62135-677-30- 30 TABLET in 1 BOTTLE (62135-677-30)

67877- Ascend Laboratories, LLC
- 67877-259- Rasagiline
  - 67877-259-30- 30 TABLET in 1 BOTTLE (67877-259-30)

67877- Ascend Laboratories, LLC
- 67877-260- Rasagiline
  - 67877-260-30- 30 TABLET in 1 BOTTLE (67877-260-30)

72162- Bryant Ranch Prepack
- 72162-2383- RASAGILINE
  - 72162-2383-3- 30 TABLET in 1 BOTTLE (72162-2383-3)

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Indications ⬇

Contraind./Precautions ⬆ ⬇