Rasagiline

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[edit] BRAND NAMES

[edit] STRUCTURE

Rasagiline.jpg

[edit] MECHANISM OF ACTION

Parkinson is a disease of the nervous system that mainly affects body movement. The three main symptoms are shaking (resting tremor), muscle stiffness (feeling of tension or tightness in the muscles) and slow and unsteady movement. People with Parkinson’s disease often walk with a shuffle as they have difficulty in initiating movement. Most of the movement-related symptoms of Parkinson's disease are caused by a lack of dopamine due to the loss of dopamine-producing cells in the substantia nigra in the brain.

Human cells contain two forms of monoamine oxidase, MAO-A and MAO-B. Both are found in the brain, but MAO-B is far more prevalent and is responsible for the breakdown of dopamine after its re-uptake from the synapse.

Rasagiline functions as a selective, irreversible MAO-B inhibitor which causes an increase in extracellular levels of dopamine in the striatum. The elevated dopamine level and subsequent increased dopaminergic activity are likely to mediate rasagiline’s beneficial effects in Parkinson's disease

[edit] INDICATIONS

Treatment of the signs and symptoms of idiopathic Parkinson’s disease as initial monotherapy and as adjunct therapy to levodopa

[edit] DOSAGE

  • Monotherapy: 1 mg once daily
  • As adjunct to levodopa: 0.5 mg once daily. Dose increase to 1 mg daily as required for sufficient clinical response.
  • Patients with mild hepatic impairment: 0.5 mg once daily should not be exceeded.
  • Patients taking ciprofloxacin or other CYP1A2 inhibitors: 0.5 mg once daily should not be exceeded.

[edit] CONTRAINDICATIONS

[edit] WARNINGS AND PRECAUTIONS

  • Risk of severe CNS toxicity (serotonin syndrome) when Rasagiline is combined with antidepressants.
  • Concomitant use of ciprofloxacin or other CYP1A2 inhibitors: Increase in rasagiline plasma concentrations. 0.5 mg rasagiline once daily should not be exceeded.
  • Patients with hepatic impairment: Increase in rasagiline plasma concentrations. Limit dose to 0.5 mg rasagiline in mild hepatic impairment. Rasagiline should not be used in patients with moderate or severe hepatic impairment.
  • Risk for Hypertensive Crisis and nonselective MAO inhibition above the recommended Doses.
  • Melanoma
  • Rasagiline may cause lower blood pressure, especially postural hypotension or increase blood pressure in different patients
  • Rasagiline may cause or exacerbate hallucinations or potentially other manifestations of psychotic-like behavior

[edit] INTERACTIONS

  • Meperidine: Risk of serious, sometimes fatal reactions from serotonin syndrome (Contraindicated).
  • Dextromethorphan: Risk of psychosis episodes or bizarre behavior (Contraindicated).
  • MAO inhibitors: Risk of non-selective MAO inhibition and hypertensive crisis (Contraindicated).
  • Antidepressants (SSRIs, SNRIs, tricyclic, tetracyclic, or triazolopyridine): Concomitant use not recommended.
  • Levodopa: See also Warnings and Precautions.
  • Ciprofloxacin and Other CYP1A2 Inhibitors: Increased rasagiline plasma levels possible. Increased risk of adverse events. Rasagiline 0.5 mg once daily should not be exceeded.

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category C (US). Rasagiline should be used only if the potential benefit justifies the potential risk to the fetus.
  • Nursing mothers: Rasagiline inhibits prolactin secretion and may inhibit milk secretion. It is not known whether rasagiline is excreted in human milk. Use with caution.

[edit] SIDE EFFECTS

  • Most common adverse reactions (treatment difference ≥ 3% greater than placebo); with monotherapy: flu syndrome, arthralgia, depression, dyspepsia.
  • Most common adverse reactions (treatment difference ≥ 3% greater than placebo); when used as adjunct to levodopa: dyskinesia, accidental injury, weight loss, postural hypotension, vomiting, anorexia, arthralgia, abdominal pain, nausea, constipation, dry mouth, rash, abnormal dreams, fall.

[edit] RELATED LINKS

Medications for the Treatment of Parkinson's Disease

[edit] BIBLIOGRAPHY

[edit] REFERENCES