Ralect Tablet

Ralect tablet is indicated as monotherapy or as adjunct therapy for the treatment of Parkinson’s disease (PD).

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. The way it acts is related to its MAO-B inhibitory activity, 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 seen in models of dopaminergic motor dysfunction.

The recommended dose is 1 mg orally once daily as monotherapy or as adjunct therapy in patients not taking levodopa. In patients taking levodopa, with or without other PD drugs (e.g., dopamine agonist, amantadine, anticholinergics), the recommended initial dose of Rasagiline is 0.5 mg once daily. If the patient tolerates the daily 0.5 mg dose, but a sufficient clinical response is not achieved, the dose may be increased to 1 mg once daily. When Rasagiline is used in combination with levodopa, a reduction of the levodopa dose may be considered, based upon individual response. The recommended dose of Rasagiline should not be exceeded because of risk of hypertension.

Pediatric use: The safety & effectiveness in pediatric patients have not been established.

Geriatric use: There were no significant differences in the safety profile of the geriatric & nongeriatric patients.

Side effects include joint pain, mild headache, depressed mood, dizziness, spinning sensation, hair loss, mild skin rash, numbness or tingly feeling, dry mouth, loss of appetite, constipation, diarrhea, stomach pain or upset, vomiting, weight loss etc.

Pregnancy category C. Caution should be exercised when prescribing to pregnant women. Experimental data indicated that Rasagiline inhibits prolactin secretion and, thus, may inhibit lactation. It is not known whether Rasagiline is excreted in human milk. Caution should be exercised when Rasagiline is administered to a breastfeeding mother.

Hypertension: Exacerbation of hypertension may occur during treatment with Ralect. Medication adjustment may be necessary if elevation of blood pressure is sustained. Dietary tyramine restriction is not required during treatment with recommended doses of Ralect. However, certain foods that may contain very high amounts (more than 150 mg) of tyramine that could potentially cause severe hypertension because of tyramine interaction in patients taking Ralect, even at the recommended doses, due to increased sensitivity to tyramine. In that case, patients should be advised to avoid foods containing a very large amount of tyramine.

Serotonin Syndrome: Serotonin syndrome has been reported with concomitant use of an antidepressant (e.g., SSRIs, SNRIs, tricyclic & tetracyclic antidepressants, Triazolopyridine antidepressants) and a nonselective MAOI (e.g., phenelzine, tranylcypromine) or selective MAO-B inhibitors, such as Ralect.

Ciprofloxacin or other CYP1A2 Inhibitors: Patients taking concomitant ciprofloxacin or other CYP1A2 inhibitors should not exceed a dose of Ralect 0.5 mg once daily.

Hepatic impairment: Patients with mild hepatic impairment should be given the dose of Ralect 0.5 mg once daily. Ralect should not be used in patients with moderate or severe hepatic impairment.

The concomitant use of Ralect and fluoxetine or fluvoxamine should be avoided. At least five weeks should
elapse between discontinuation of fluoxetine and initiation of treatment with Ralect. At least 14 days should elapse between discontinuation of Ralect and initiation of treatment with fluoxetine or fluvoxamine.

The concomitant use of Ralect and dextromethorphan or sympathomimetics such as, those present in nasal and oral decongestants or cold medicinal product containing ephedrine or pseudoephedrine is not recommended.

During the clinical development program the occurrence of cases of melanoma prompted the consideration of a possible association with Ralect. The data collected suggests that Parkinson's disease and not any medicinal products in particular, is associated with a higher risk of skin cancer (not exclusively melanoma). Any suspicious skin lesion should be evaluated by a specialist.

Signs and symptoms of Ralect overdose may include drowsiness, dizziness, faintness, irritability, hyperactivity, agitation, severe headache, hallucinations, trismus, opisthotonos, convulsions and coma; rapid and irregular pulse, hypertension, hypotension and vascular collapse; precordial pain, respiratory depression and failure, hyperpyrexia, diaphoresis, and cool, clammy skin.

Treatment: There is no specific antidote for Ralect overdose. The following suggestions are offered: Respiration should be supported by appropriate measures, including management of the airway, use of supplemental oxygen, and mechanical ventilator assistance, as required. Body temperature should be monitored closely. Intensive management of hyperpyrexia may be required. Maintenance of fluid and electrolyte imbalance is essential. For this reason, in cases of overdose with Ralect, dietary tyramine restriction should be observed for several weeks to reduce the risk of hypertensive tyramine reaction. Moreover, a poison control center should be called for the most current treatment guidelines.

Antiparkinson drugs

Store at temperature not exceeding 30ºC in a dry place. Protect from light. Keep out of reach of children. To be sold by retail on the prescription of a registered physician only.