Parkinsons disease is a CNS disorder of the basal ganglia that affects movement

and causes tremors, stiffness and slowing of body movement.

Rasagiline
Trade name: Azilect
Classification
Antiparkinson agents (therapeutic)
Monoamine oxidase type b inhibitors (pharmacologic)
Pregnancy Category C
Indications
Parkinson's disease (monotherapy and adjunctive to levodopa).
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's disease, allowing increase in function.
Pharmacokinetics
Absorption: 36% absorbed following oral administration.
Distribution: Readily crosses the blood-brain barrier.
Metabolism and Excretion: Extensively metabolized by the liver (CYP1A2
enzyme) to an inactive metabolite; less than 1% excreted in urine.
Half-life: 1.3 hr; does not correlate with duration of MAO-B inhibition.
ROUTE
PO

ONSET
rapid

PEAK
1 hr

DURATION
40 days*

Contraindications/Precautions

Hypersensitivity;

Concurrent meperidine, tramadol, methadone, sympathomimetic amines,

dextromethorphan, mirtazapine, cyclobenzaprine, cocaine, St. John's wort,
another MAO inhibitor;

Moderate to severe hepatic impairment;

Elective surgery requiring general anesthesia; allow 14 days after

discontinuation;

Pheochromocytoma;

Psychotic disorder.
Use Cautiously in:

Mild hepatic impairment ( blood levels);

OB: Use only if maternal benefit outweighs fetal risk;

Lactation: May inhibit lactation;
Pedi: Safety not established.

Adverse reactions/side effects

CNS: depression, dizziness, hallucinations, malaise, vertigo
EENT: conjunctivitis, rhinitis
Resp: asthma
CV: BP, chest pain, postural hypotension (may levodopa-induced hypotension),
syncope
GI: anorexia, dizziness, dyspepsia, gastroenteritis, vomiting
GU: albuminuria, libido
Derm: alopecia, ecchymosis, melanoma risk, rash
Endo: weight loss
Hemat: leukopenia
MS: arthralgia, arthritis, neck pain
Neuro: dyskinesia (may levodopa-induced dyskinesia), paresthesia
Misc: allergic reactions, flu-like syndrome, fall risk, fever
Drug-Drug interactions
Ciprofloxacin and other inhibitors of the CYP1A2 enzyme rasagiline
levels; dose adjustment is recommended.
Meperidine has resulted in life-threatening reactions when used with other MAO
inhibitors; wait at least 14 days after discontinuation of rasagiline to initiate
meperidine.
Similar reactions may occur with tramadol, methadone; concurrent use should
be avoided.
Concurrent use with dextromethorphan may result in psychosis/bizarre
behavior and should be avoided.
risk of adverse reactions with mirtazapine and cyclobenzapine; concurrent
use should be avoided.
Hypertensive crisis may occur with sympathomimetic
amines including amphetamines, cold products, and some weight loss
products containing vasoconstrictors such
aspseudoephedrine, phenylephrine, or ephedrine; avoid concurrent use.
risk of serotonin syndrome with tricyclic antidepressants, SSRI
antidepressants, SNRI antidepressants, and other MAO
inhibitors; rasagiline should be discontinued 14 days prior to initiation of
antidepressants ( fluoxetine should be discontinued 5 wk prior to rasagiline
therapy).
Hypertensive crisis may also occur when rasagiline is used with other MAO
inhibitors; allow at least 14 days between usage.

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

Risk of toxicity is with St. John's wort .

Route/Dosage
PO: (Adults) Monotherapy 1 mg daily; adjunct therapy 0.5 mg daily, may to 1
mg daily; concurrent ciprofloxacin or other CYP1A2 inhibitors 0.5 mg daily.
Hepatic Impairment
PO: (Adults) Mild hepatic impairment 0.5 mg daily.
Evaluation/Desired Outcomes
Improvement in symptoms of Parkinson's disease, allowing increase in function.
Reference
Vallerand, A., & Sanoski, C. (2014) Davis's drug guide for nurses (14th ed.)
F.A. Davis Company