Azilect 1 mg Tablets

Brand Name

This therapeutic agent is commercially known as Azilect, a designation frequently encountered in neurological treatment settings.

International Non-Proprietary Name

The active compound is identified worldwide as rasagiline, adhering to the universal nomenclature established for pharmaceutical substances.

Form of Release

The medication is available exclusively in tablet form, designed for oral administration. It comes in a single strength of 1 milligram, offering a straightforward dosing option for patients requiring this therapy.

Composition

The primary ingredient is rasagiline mesylate, which drives the drug’s effectiveness through its action on specific enzymes. Supporting components in the tablets include mannitol, colloidal anhydrous silica, maize starch, pregelatinized starch, stearic acid, and talc. These excipients ensure proper tablet formation, stability, and ease of absorption once ingested.

Pharmacologic Properties

Pharmacodynamics

This treatment operates as a selective, irreversible inhibitor of monoamine oxidase type B (MAO-B), an enzyme that breaks down dopamine in the brain. By blocking MAO-B, the medication increases dopamine levels, a neurotransmitter essential for coordinating movement and mood. This elevation helps counteract the dopamine deficiency seen in certain neurological conditions, improving motor function without broadly affecting other monoamine systems. Its selectivity for MAO-B over MAO-A minimizes interference with dietary tyramine metabolism, reducing risks associated with less specific inhibitors.

Studies demonstrate that the drug enhances motor performance and may offer neuroprotective benefits by reducing oxidative stress in brain cells. While its primary role is symptomatic relief, some evidence suggests it could slow disease progression through mechanisms like mitochondrial protection. These effects make it a valuable tool in managing movement-related symptoms effectively.

Pharmacokinetics

Upon oral intake, the medication absorbs rapidly from the gastrointestinal tract, reaching peak plasma concentrations within 0.5 to 1 hour. Food, particularly high-fat meals, may delay absorption slightly but does not alter overall bioavailability, which exceeds 35 percent despite significant first-pass metabolism. This rapid uptake supports its once-daily administration schedule.

The substance distributes extensively, with a volume of distribution around 87 liters, indicating penetration into tissues including the brain. It binds to plasma proteins at about 88 to 94 percent, primarily albumin, influencing its availability for action. Metabolism occurs predominantly in the liver via cytochrome P450 enzyme CYP1A2, producing inactive metabolites like 1-aminoindan. The half-life is approximately 3 hours, though its irreversible binding to MAO-B extends its therapeutic duration beyond this period.

Excretion happens mainly through urine (over 60 percent as metabolites) and to a lesser extent via feces. Renal clearance plays a minor role, as the drug is largely transformed before elimination. This profile ensures sustained activity with consistent dosing, tailored to its enzyme-targeting mechanism.

Indications for Use

Conditions and Disorders

The medication is indicated for Parkinson’s disease, a chronic disorder characterized by dopamine loss in the brain. It is used as monotherapy in early stages to improve motor symptoms like tremors, rigidity, and slowness of movement. In advanced cases, it serves as an adjunct to levodopa therapy, enhancing dopamine availability and reducing "off" periods when symptoms worsen. This dual role supports patients across the disease spectrum.

Azilect provides consistent symptom management, helping individuals maintain daily activities longer. While primarily approved for Parkinson’s, some clinicians explore its potential in other dopamine-related conditions, though such uses remain investigational and lack widespread endorsement.

Contraindications

Conditions Prohibiting Use

The drug is contraindicated in patients with hypersensitivity to rasagiline or its components, as allergic reactions could range from skin irritation to severe systemic responses. It must not be used with other monoamine oxidase inhibitors, including non-selective MAOIs or MAO-A inhibitors like linezolid, due to risks of hypertensive crises from excessive monoamine buildup.

Individuals with pheochromocytoma, a rare adrenal tumor causing catecholamine surges, should avoid it, as the medication could exacerbate blood pressure spikes. Severe liver impairment also precludes its use, given its reliance on hepatic metabolism. Concurrent use with certain antidepressants, such as serotonin reuptake inhibitors, poses a risk of serotonin syndrome, necessitating careful evaluation before administration.

Method of Administration and Dosage

Administration Guidelines

The medication is taken orally once daily, with or without food, offering flexibility based on patient preference. Tablets should be swallowed whole with water, ideally at the same time each day to maintain steady therapeutic levels. Consistency in timing enhances its effectiveness given its enzyme-binding action.

Dosage for Adults and Children

For adults with Parkinson’s, the standard dose is 1 milligram daily, whether as monotherapy or alongside levodopa. No titration is typically required, simplifying its initiation. Pediatric use is not approved, as safety and efficacy in children have not been established through clinical studies, limiting its application to adults.

Dose Adjustments for Specific Conditions

In mild hepatic impairment, the standard 1-milligram dose is usually safe, but caution is advised due to altered metabolism. Moderate to severe liver dysfunction requires avoiding the drug entirely, as reduced clearance could lead to accumulation. Renal impairment does not necessitate adjustment, as kidney function has minimal impact on its elimination. Physicians should monitor patients with organ issues closely to ensure safe use.

Side Effects

Potential Adverse Reactions

Common reactions include headache, joint pain, and indigestion, often mild and linked to dopamine enhancement or gastrointestinal adjustment. Dyskinesia, or involuntary movements, may occur, particularly when combined with levodopa, reflecting amplified dopaminergic activity. Fatigue and insomnia also appear frequently, typically resolving with continued use.

Less common but notable effects involve hallucinations or confusion, especially in advanced disease stages or at higher dopamine levels. Orthostatic hypotension, a drop in blood pressure upon standing, may affect some patients, requiring monitoring. Rarely, severe skin reactions or impulse control disorders like compulsive behaviors emerge, necessitating immediate medical review if observed.

Overdose

Symptoms of Excessive Intake

Excessive dosing can lead to symptoms resembling MAOI overdose, including agitation, sweating, rapid heartbeat, and elevated blood pressure. Severe cases may progress to confusion, seizures, or coma due to neurotransmitter overload. Unlike classic MAOIs, tyramine-related hypertensive crises are less likely, but significant overdose still poses serious risks.

First Aid Measures

Cease administration immediately and seek emergency care. Activated charcoal may reduce absorption if given soon after ingestion, provided the patient is alert. No specific antidote exists, so treatment focuses on symptom management, such as controlling blood pressure or sedation for agitation. Vital signs should be stabilized with supportive care until professional help is available.

Drug Interactions

Effects on Other Medications

The medication can dangerously interact with other MAO inhibitors, amplifying monoamine levels and risking hypertensive emergencies. It may potentiate sympathomimetic drugs like decongestants, increasing blood pressure effects. Concurrent use with CYP1A2 inhibitors, such as ciprofloxacin, could raise its plasma levels, intensifying side effects, while inducers like smoking might reduce its efficacy.

Azilect heightens the risk of serotonin syndrome when paired with serotonergic drugs, including certain antidepressants or opioids like tramadol. Caution is also needed with levodopa, as it may exacerbate dyskinesia or hypotension, requiring dose adjustments of either therapy.

Compatibility with Alcohol and Food

Moderate alcohol use is generally tolerated, though excessive intake may worsen dizziness or hypotension. Unlike broader MAOIs, the drug does not require strict tyramine avoidance, but high-tyramine foods (e.g., aged cheeses) should be limited at very high doses or with interacting drugs. Food has little effect on absorption, allowing flexible timing.

Special Precautions

Use During Pregnancy and Breastfeeding

Data on pregnancy are limited, with no clear human evidence of safety or harm. Animal studies show no major fetal risks, but use should be restricted to cases where benefits outweigh uncertainties, under medical supervision. Its presence in breast milk is unknown, so breastfeeding mothers should consult a doctor, potentially pausing lactation during treatment.

Impact on Driving and Machinery Operation

The medication may cause dizziness, fatigue, or low blood pressure, particularly early in therapy or with levodopa. Patients should evaluate their response before driving or operating machinery, avoiding these activities if impaired. Caregivers may need to assist those with significant symptoms or side effects.

Considerations for Elderly and Pediatric Patients

Elderly patients tolerate the standard dose well in most cases, though age-related liver decline may warrant monitoring in moderate impairment. Azilect is not approved for children, as Parkinson’s rarely affects this group and pediatric studies are lacking, confining its use to adults.