AZILECT is a selective inhibitor of monoamine oxidase (MAO)-B at recommended doses of 0.5 or 1 mg daily. Dietary tyramine restriction is not ordinarily required with recommended doses of AZILECT. However, certain foods (e.g., aged cheeses, such as Stilton cheese) may contain very high amounts (i.e., > 150 mg) of tyramine and could potentially cause a hypertensive "cheese" reaction in patients taking AZILECT even at the recommended dose due to mild increased sensitivity to tyramine. The selectivity for inhibiting MAO-B diminishes in a dose-related manner as the dose is progressively increased above the recommended daily dose [see Warnings and Precautions (5.4), Clinical Pharmacology (12.3, and Information for Patients (17.3))].
2.1 Monotherapy
The recommended AZILECT dose for the treatment of Parkinson's disease patients is 1 mg administered orally once daily.
2.2 Adjunctive Therapy
The recommended initial dose is 0.5 mg administered orally once daily. If a sufficient clinical response is not achieved, the dose may be increased to 1 mg administered once daily.
Change of Levodopa Dose in Adjunct Therapy
When AZILECT is used in combination with levodopa, a reduction of the levodopa dosage may be considered based upon individual response. During the controlled trials of AZILECT as adjunct therapy to levodopa, levodopa dosage was reduced in some patients. In clinical studies, dosage reduction of levodopa was allowed within the first 6 weeks if dopaminergic side effects, including dyskinesia and hallucinations, emerged. In Study 1, levodopa dosage reduction occurred in 8% of patients in the placebo group and in 16% and 17% of patients in the 0.5 mg/day and 1 mg/day rasagiline groups, respectively. In those patients who had levodopa dosage reduced, the dose was reduced on average by about 7%, 9%, and 13% in the placebo, 0.5 mg/day, and 1 mg/day groups, respectively. In Study 2, levodopa dosage reduction occurred in 6% of patients in the placebo group and in 9% in the rasagiline 1 mg/day group. In patients who had their levodopa dosage reduced, the dose was reduced on average by about 13% and 11% in the placebo and the rasagiline groups, respectively.
2.3 Patients with Hepatic Impairment
AZILECT plasma concentrations will increase in patients with hepatic impairment. Patients with mild hepatic impairment should use 0.5 mg daily of AZILECT. AZILECT should not be used in patients with moderate or severe hepatic impairment [see Warnings and Precautions (5.3), Use in Specific Populations (8.6), and Clinical Pharmacology (12.3)].
2.4 Patients with Renal Impairment
Dose adjustment of AZILECT is not required for patients with mild or moderate renal impairment because AZILECT plasma concentrations are not increased in patients with moderate renal impairment. Rasagiline has not been studied in patients with severe renal impairment.
2.5 Patients Taking Ciprofloxacin or Other CYP1A2 Inhibitors
Rasagiline plasma concentrations are expected to double in patients taking concomitant ciprofloxacin and other CYP1A2 inhibitors. Therefore, patients taking concomitant ciprofloxacin or other CYP1A2 inhibitors should use 0.5 mg daily of AZILECT [see Warnings and Precautions (5.2), Drug Interactions (7.7), and Clinical Pharmacology (12.3)].
