Rasagiline

Oral
Parkinson's disease

Patients who are concurrently receiving ciprofloxacin or other CYP1A2 inhibitors: Max: 0.5 mg once daily. Dosage and treatment recommendations may vary among countries and between individual products (refer to specific product guidelines).

Severe: Contraindicated. Dosage and treatment recommendations may vary among countries and between individual products (refer to specific product guidelines).

Rasagiline May be taken with or without food. Avoid tyramine-rich foods, beverages or dietary supplements & amines (from cough/cold prep).

Severe hepatic impairment. Concomitant use or within 14 days of discontinuing other MAOIs and pethidine. Concurrent use with St. John's wort.

Patient with psychotic disorders. Patients who smoke and those undergoing surgery. Avoid abrupt withdrawal. Concomitant use with ciprofloxacin or other CYP1A2 inhibitors, dextromethorphan, tramadol, methadone, propoxyphene, and cyclobenzaprine. Mild to moderate hepatic impairment. Pregnancy and lactation.

Significant: New or worsening changes in mental status and behaviour, including paranoid ideation, confusion, delusion, disorientation, hallucinations, psychotic-like or aggressive behaviour, agitation, and delirium; impulse control disorders (e.g. pathological gambling, binge eating, compulsive spending or buying, increased libido); somnolence, sudden sleep onset episodes or falling asleep while engaged in daily activities; dyskinesia, orthostatic hypotension (particularly when combined with levodopa); exacerbation of hypertension; increased risk of melanoma; symptom complex that resembles neuroleptic malignant syndrome (particularly during abrupt withdrawal or interruption of therapy).
Blood and lymphatic system disorders: Leucopenia.
Cardiac disorders: Angina pectoris.
Ear and labyrinth disorders: Vertigo.
Eye disorders: Conjunctivitis.
Gastrointestinal disorders: Dyspepsia, abdominal pain, nausea, vomiting, constipation, dry mouth, flatulence, gastroenteritis.
General disorders and administration site conditions: Fever, malaise.
Injury, poisoning and procedural complications: Fall.
Investigations: Decreased weight.
Metabolism and nutrition disorders: Decreased appetite.
Musculoskeletal and connective tissue disorders: Arthralgia, arthritis, neck pain, musculoskeletal pain.
Nervous system disorders: Headache, dystonia, paraesthesia.
Psychiatric disorders: Depression, abnormal dreams.
Renal and urinary disorders: Urinary urgency.
Respiratory, thoracic and mediastinal disorders: Rhinitis, influenza.
Skin and subcutaneous tissue disorders: Dermatitis, rash, ecchymoses.

PO: C

This drug may cause somnolence or sudden sleep onset episodes, if affected, do not drive or operate machinery.

Monitor blood pressure at baseline and periodically; liver and renal function at baseline and as clinically necessary. Perform periodic skin examinations to check for melanoma, usually by evaluating new or changing skin lesions. Closely monitor for signs of changes in mental status or behaviour, including suicidal ideation and compulsive behaviours.

Symptoms: Severe headache, drowsiness, dizziness, agitation, hallucinations, hyperactivity, hypomania, hyperpyrexia, hypertensive crisis, and serotonin syndrome. Management: Symptomatic and supportive treatment. Support respiration by managing the airway and providing supplemental oxygen or mechanical ventilation as needed. Closely monitor the body temperature and maintain fluid/electrolyte balance.

May increase the risk of dyskinesia or orthostatic hypotension with levodopa. May cause short episodes of psychosis or bizarre behaviour with dextromethorphan. May result in severe hypertensive reactions with sympathomimetics, including oral, nasal or ophthalmic decongestants and cold medicines that contain sympathomimetic amines (e.g. ephedrine, pseudoephedrine). Ciprofloxacin and other CYP1A2 inhibitors may increase the plasma levels of rasagiline by up to 2 fold. Renal clearance may be increased with entacapone. Potential reduction of therapeutic effects with dopamine antagonists (e.g. metoclopramide, antipsychotics that reduce central dopaminergic tone).
Potentially Fatal: Increased risk of serotonin syndrome with other MAOIs (e.g. selegiline, phenelzine, tranylcypromine), pethidine, tramadol, methadone, propoxyphene, cyclobenzaprine, and antidepressants (e.g. SSRIs, SNRIs, TCAs, tetracyclic antidepressants, triazolopyridine derivatives).

Increased risk of serotonin syndrome with St. John's wort. May result in a hypertensive crisis when taken with foods that contain very high amounts (>150 mg) of tyramine, such as aged or matured cheeses.

Description:
Mechanism of Action: Rasagiline is a potent, irreversible and selective inhibitor of monoamine oxidase B (MAO-B), an enzyme that regulates the degradation of dopamine. The inhibition of MAO-B increases the extracellular levels of dopamine in the striatum, thereby enhancing the dopaminergic activity and subsequently reducing symptomatic motor deficits in Parkinson's disease.
Onset: Irreversible MAO-B inhibition: Approx 1 week.
Pharmacokinetics:
Absorption: Rapidly absorbed from the gastrointestinal tract. Absolute bioavailability: Approx 36%. Time to peak plasma concentration: Approx 0.5-1 hour.
Distribution: Plasma protein binding: Approx 60-70%.
Metabolism: Extensively metabolised in the liver via N-dealkylation and hydroxylation by CYP1A2 isoenzyme to form several inactive metabolites.
Excretion: Mainly in the urine (62%, <1% as unchanged drug); faeces (7%). Elimination half-life: Approx 3 hours.

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 3052776, Rasagiline. https://pubchem.ncbi.nlm.nih.gov/compound/Rasagiline. Accessed Oct. 28, 2024.

Store between 15-30°C.

Antiparkinsonian Drugs

N04BD02 - rasagiline ; Belongs to the class of dopaminergic agents, monoamine oxidase B inhibitors. Used in the management of Parkinson's disease.

Anon. Rasagiline. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 04/10/2024.

Azilect 1 mg Tablets (Lundbeck Hong Kong). MIMS Hong Kong. http://www.mims.com/hongkong. Accessed 04/10/2024.

Brayfield A, Cadart C (eds). Rasagiline Mesilate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/10/2024.

Joint Formulary Committee. Rasagiline. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/10/2024.

Rasagiline 1 mg Tablets (Medreich PLC). MHRA. https://products.mhra.gov.uk. Accessed 04/10/2024.

Rasagiline Mesylate Tablet (Avet Pharmaceuticals Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 04/10/2024.

Rasagiline. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 04/10/2024.