Drug information of rasagiline

rasagiline


Rasagiline is an irreversible inhibitor of monoamine oxidase and is used as a monotherapy in early Parkinson's disease or as an adjunct therapy in more advanced cases.

Mechanism of effect

The precise mechanisms of action of rasagiline is unknown. One mechanism is believed to be related to its MAO-B inhibitory activity, which causes an increase in extracellular levels of dopamine in the striatum.

Pharmacodynamic

Rasagiline is a propargylamine and an irreversible inhibitor of monoamine oxidase (MAO). MAO, a flavin-containing enzyme, regulates the metabolic degradation of catecholamines and serotonin in the CNS and peripheral tissues. It is classified into two major molecular species, A and B, and is localized in mitochondrial membranes throughout the body in nerve terminals, brain, liver and intestinal mucosa. MAO-A is found predominantly in the GI tract and liver, and regulates the metabolic degradation of circulating catecholamines and dietary amines.

 MAO-B is the major form in the human brain and is responsible for the regulation of the metabolic degradation of dopamine and phenylethylamine. At the recommended therapeutic doses, Rasagiline was also shown to be a potent and irreversible inhibitor of MAO-B in platelets.

Pharmacokinetics

Absorption

Peak Plasma Time: 1 hr

Onset of action: Within 1 hr

Bioavailability: 36%

Distribution

Protein Bound: 88-94%

Vd: 87 L

Metabolism

Via liver, primarily CYP1A2 (in vitro data)

Metabolites: 1-aminoindan, 3-hydroxy-N-propargyl-1-aminoindan, 3-hydroxy-1-aminoindan

Elimination

Half-life: 1.3-3 hr

Excretion: 62% urine; 7% feces

Drug indications

parkinson

Dosage

Adult : 1 mg PO qDay

Alerts

  • 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
  • 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

Points of recommendation

  • Avoid driving and doing other tasks or actions that call for you to be alert until you see how rasagiline affects you.
  • To lower the chance of feeling dizzy or passing out, rise slowly if you have been sitting or lying down. Be careful going up and down stairs.
  • Do not stop taking rasagiline all of a sudden without calling your doctor. You may have a greater risk of side effects. If you need to stop rasagiline, you will want to slowly stop it as ordered by your doctor.
  • Some foods and drinks like cheese and red wine, when taken with rasagiline, may cause very risky effects such as sudden high blood pressure. To avoid these problems, get a list of foods to avoid.
  • Some people have fallen asleep during activities like driving, eating, or talking. Some people did not feel sleepy and felt alert right before falling asleep. This has happened up to 1 year after rasagiline was started. If you fall asleep during activities, do not drive or do other tasks or actions that call for you to be alert while you take rasagiline. Call your doctor right away if this happens or you feel very sleepy.
  • High or low blood pressure may happen with rasagiline. Have your blood pressure checked as you have been told by your doctor.
  • If you are taking rasagiline and have high blood pressure, talk with your doctor before using OTC products that may raise blood pressure. These include cough or cold drugs, diet pills, stimulants, ibuprofen or like products, and some natural products or aids.
  • The chance of a type of skin cancer called melanoma may be raised in people with Parkinson's disease. It is not known if rasagiline may also raise the chance. Have skin exams while you take rasagiline. Talk with your doctor.
  • Talk with your doctor before you drink alcohol.
  • Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using rasagiline while you are pregnant.
  • Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.

Pregnancy level

C

Related drugs

safinamide , Selegiline , Apomorphine


Ask a Pharmacist


User's questions
    No comments yet.