Rasagiline Mesylate

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Overview

What is Rasagiline Mesylate?

Rasagiline mesylate tablets contain rasagiline (as the mesylate), a propargylamine-based drug indicated for the treatment of idiopathic Parkinson’s disease. It is designated chemically as: 1H-Inden-1-amine, 2, 3-dihydro-N-2-propynyl-, (1R)-, methanesulfonate. The molecular formula of rasagiline mesylate is (CHN)CHSO and its molecular weight is 267.34.

Its structural formula is:

Rasagiline mesylate is a white to off-white powder, freely soluble in water or ethanol and sparingly soluble in isopropanol. Each rasagiline mesylate tablets for oral administration contains rasagiline mesylate equivalent to 0.5 mg or 1 mg of rasagiline base.

Each Rasagiline mesylate tablet also contains the following inactive ingredients: lactose monohydrate, pregelatinised starch, corn starch, talc, stearic acid, and citric acid monohydrate.

What does Rasagiline Mesylate look like?

What are the available doses of Rasagiline Mesylate?

Rasagiline mesylate tablets 0.5 mg: White to off-white, round, flat, beveled tablets, debossed with “R1” on one side and plain on the other side containing, as the active ingredient, rasagiline mesylate equivalent to 0.5 mg of rasagiline base.

Rasagiline mesylate tablets 1 mg: White to off-white, round, flat, beveled tablets, debossed with “R2” on one side and plain on the other side containing, as the active ingredient, rasagiline mesylate equivalent to 1 mg of rasagiline base.

What should I talk to my health care provider before I take Rasagiline Mesylate?

How should I use Rasagiline Mesylate?

Rasagiline mesylate tablets are indicated for the treatment of Parkinson’s disease (PD).

What interacts with Rasagiline Mesylate?

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What are the warnings of Rasagiline Mesylate?

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What are the precautions of Rasagiline Mesylate?

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What are the side effects of Rasagiline Mesylate?

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What should I look out for while using Rasagiline Mesylate?

Rasagiline is contraindicated for use with meperidine, tramadol, methadone, propoxyphene and MAO inhibitors (MAOIs), including other selective MAO-B inhibitors, because of risk of serotonin syndrome [See Warnings and Precautions (5.2)]. At least 14 days should elapse between discontinuation of rasagiline and initiation of treatment with these medications.

Rasagiline is contraindicated for use with St. John’s wort and with cyclobenzaprine.

Rasagiline is contraindicated for use with dextromethorphan because of risk of episode of psychosis or bizarre behavior.

What might happen if I take too much Rasagiline Mesylate?

In a dose escalation study in patients on chronic levodopa therapy treated with 10 mg of rasagiline there were three reports of cardiovascular side effects (including hypertension and postural hypotension) which resolved following treatment discontinuation. Although no cases of overdose have been observed with rasagiline during the clinical development program, the following description of presenting symptoms and clinical course is based upon overdose descriptions of nonselective MAO inhibitors.

The signs and symptoms of nonselective MAOI overdose may not appear immediately. Delays of up to 12 hours after ingestion of drug and the appearance of signs may occur. The peak intensity of the syndrome may not be reached until for a day following the overdose. Death has been reported following overdose; therefore, immediate hospitalization, with continuous patient observation and monitoring for at least two days following the ingestion of such drugs in overdose, is strongly recommended.

The severity of the clinical signs and symptoms of MAOI overdose varies and may be related to the amount of drug consumed. The central nervous and cardiovascular systems are prominently involved.

Signs and symptoms of MAOI 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.

There is no specific antidote for rasagiline overdose. The following suggestions are offered based upon the assumption that rasagiline overdose may be modeled after nonselective MAO inhibitor poisoning. Treatment of overdose with nonselective MAO inhibitors is symptomatic and supportive. Respiration should be supported by appropriate measures, including management of the airway, use of supplemental oxygen, and mechanical ventilatory assistance, as required. Body temperature should be monitored closely. Intensive management of hyperpyrexia may be required. Maintenance of fluid and electrolyte balance is essential. For this reason, in cases of overdose with rasagiline, dietary tyramine restriction should be observed for several weeks to reduce the risk of hypertensive tyramine reaction.

A poison control center should be called for the most current treatment guidelines.

A postmarketing report described a single patient who developed a nonfatal serotonin syndrome after ingesting 100 mg of rasagiline in a suicide attempt. Another patient who was treated in error with 4 mg rasagiline daily and tramadol also developed a serotonin syndrome. One patient who was treated in error with 3 mg rasagiline daily experienced alternating episodes of vascular fluctuations consisting of hypertension and orthostatic hypotension.

How should I store and handle Rasagiline Mesylate?

Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F) [see USP Controlled Room Temperature].Rasagiline Mesylate Tablets 0.5 mg:White to off-white, round, flat, beveled tablets, debossed with “R1” on one side and plain on the other side. Supplied as bottles of 30 tablets (NDC 47781-138-30)Rasagiline Mesylate Tablets 1 mg:White to off-white, round, flat, beveled tablets, debossed with “R2” on one side and plain on the other side. Supplied as bottles of 30 tablets (NDC 47781-139-30).Storage:Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature].Rasagiline Mesylate Tablets 0.5 mg:White to off-white, round, flat, beveled tablets, debossed with “R1” on one side and plain on the other side. Supplied as bottles of 30 tablets (NDC 47781-138-30)Rasagiline Mesylate Tablets 1 mg:White to off-white, round, flat, beveled tablets, debossed with “R2” on one side and plain on the other side. Supplied as bottles of 30 tablets (NDC 47781-139-30).Storage:Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature].Rasagiline Mesylate Tablets 0.5 mg:White to off-white, round, flat, beveled tablets, debossed with “R1” on one side and plain on the other side. Supplied as bottles of 30 tablets (NDC 47781-138-30)Rasagiline Mesylate Tablets 1 mg:White to off-white, round, flat, beveled tablets, debossed with “R2” on one side and plain on the other side. Supplied as bottles of 30 tablets (NDC 47781-139-30).Storage:Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature].Rasagiline Mesylate Tablets 0.5 mg:White to off-white, round, flat, beveled tablets, debossed with “R1” on one side and plain on the other side. Supplied as bottles of 30 tablets (NDC 47781-138-30)Rasagiline Mesylate Tablets 1 mg:White to off-white, round, flat, beveled tablets, debossed with “R2” on one side and plain on the other side. Supplied as bottles of 30 tablets (NDC 47781-139-30).Storage:Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature].Rasagiline Mesylate Tablets 0.5 mg:White to off-white, round, flat, beveled tablets, debossed with “R1” on one side and plain on the other side. Supplied as bottles of 30 tablets (NDC 47781-138-30)Rasagiline Mesylate Tablets 1 mg:White to off-white, round, flat, beveled tablets, debossed with “R2” on one side and plain on the other side. Supplied as bottles of 30 tablets (NDC 47781-139-30).Storage:Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature].

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Clinical Information

Chemical Structure

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Clinical Pharmacology

Rasagiline is a selective, irreversible MAO-B inhibitor indicated for the treatment of idiopathic Parkinson’s disease. The results of a clinical trial designed to examine the effects of rasagiline on blood pressure when it is administered with increasing doses of tyramine indicates the functional selectivity can be incomplete when healthy subjects ingest large amounts of tyramine while receiving recommended doses of rasagiline. The selectivity for inhibiting MAO-B diminishes in a dose-related manner.

MAO, a flavin-containing enzyme, is classified into two major molecular species, A and B, and is localized in mitochondrial membranes throughout the body in nerve terminals, brain, liver and intestinal mucosa. MAO regulates the metabolic degradation of catecholamines and serotonin in the CNS and peripheral tissues. MAO-B is the major form in the human brain. In ex vivo animal studies in brain, liver, and intestinal tissues, rasagiline was shown to be a potent, irreversible monoamine oxidase type B (MAO-B) selective inhibitor. Rasagiline at the recommended therapeutic dose was also shown to be a potent and irreversible inhibitor of MAO-B in platelets. The precise mechanisms of action of rasagiline are unknown. One mechanism is believed to be 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.

Non-Clinical Toxicology

Rasagiline is contraindicated for use with meperidine, tramadol, methadone, propoxyphene and MAO inhibitors (MAOIs), including other selective MAO-B inhibitors, because of risk of serotonin syndrome [See Warnings and Precautions (5.2)]. At least 14 days should elapse between discontinuation of rasagiline and initiation of treatment with these medications.

Rasagiline is contraindicated for use with St. John’s wort and with cyclobenzaprine.

Rasagiline is contraindicated for use with dextromethorphan because of risk of episode of psychosis or bizarre behavior.

Many drugs affect thyroid hormone pharmacokinetics and metabolism (e.g., absorption, synthesis, secretion, catabolism, protein binding, and target tissue response) and may alter the therapeutic response to Levothyroxine sodium tablets, USP. In addition, thyroid hormones and thyroid status have varied effects on the pharmacokinetics and actions of other drugs. A listing of drug-thyroidal axis interactions is contained in Table 2.

The list of drug-thyroidal axis interactions in Table 2 may not be comprehensive due to the introduction of new drugs that interact with the thyroidal axis or the discovery of previously unknown interactions. The prescriber should be aware of this fact and should consult appropriate reference sources (e.g., package inserts of newly approved drugs, medical literature) for additional information if a drug-drug interaction with levothyroxine is suspected.

Drug-Food Interactions

Carcinogenesis, Mutagenesis, and Impairment of Fertility

Pregnancy - Category A

Hypothyroidism during pregnancy is associated with a higher rate of complications, including spontaneous abortion, pre-eclampsia, stillbirth and premature delivery. Maternal hypothyroidism may have an adverse effect on fetal and childhood growth and development. During pregnancy, serum T levels may decrease and serum TSH levels increase to values outside the normal range. Since elevations in serum TSH may occur as early as 4 weeks gestation, pregnant women taking Levothyroxine sodium tablets, USP should have their TSH measured during each trimester. An elevated serum TSH level should be corrected by an increase in the dose of Levothyroxine sodium tablets, USP. Since postpartum TSH levels are similar to preconception values, the Levothyroxine sodium tablets, USP dosage should return to the pre-pregnancy dose immediately after delivery. A serum TSH level should be obtained 6-8 weeks postpartum.

Thyroid hormones cross the placental barrier to some extent as evidenced by levels in cord blood of athyreotic fetuses being approximately one-third maternal levels. Transfer of thyroid hormone from the mother to the fetus, however, may not be adequate to prevent hypothyroidism.

Nursing Mothers

Exacerbation of hypertension may occur during treatment with rasagiline. Medication adjustment may be necessary if elevation of blood pressure is sustained. Monitor patients for new onset hypertension or hypertension that is not adequately controlled after starting rasagiline.

In Study 3, rasagiline (1 mg/day) given in conjunction with levodopa, produced an increased incidence of significant blood pressure elevation (systolic > 180 or diastolic > 100 mm Hg) of 4% compared to 3% for placebo [see Adverse Reactions (6.1)].

When used as an adjunct to levodopa (Studies 3 and 4), the risk for developing post-treatment high blood pressure (e.g., systolic > 180 or diastolic >100 mm Hg) combined with a significant increase from baseline (e.g., systolic > 30 or diastolic > 20 mm Hg) was higher for rasagiline (2%) compared to placebo (1%).

Dietary tyramine restriction is not required during treatment with recommended doses of rasagiline. However, certain foods that may contain very high amounts (i.e., more than 150 mg) of tyramine that could potentially cause severe hypertension because of tyramine interaction (including various clinical syndromes referred to as hypertensive urgency, crisis, or emergency) in patients taking rasagiline, even at the recommended doses, due to increased sensitivity to tyramine. Patients should be advised to avoid foods containing a very large amount of tyramine while taking recommended doses of rasagiline because of the potential for large increases in blood pressure including clinical syndromes referred to as hypertensive urgency, crisis, or emergency. Rasagiline is a selective inhibitor of MAO-B at the recommended doses of 0.5 or 1 mg daily. Selectivity for inhibiting MAO-B diminishes in a dose-related manner as the dose is progressively increased above the recommended daily doses.

The following adverse reactions are described in more detail in the Warnings and Precautions section of the label:

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Reference

This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"

While we update our database periodically, we cannot guarantee it is always updated to the latest version.

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Professional

Clonazepam Description Each single-scored tablet, for oral administration, contains 0.5 mg, 1 mg, or 2 mg Clonazepam, USP, a benzodiazepine. Each tablet also contains corn starch, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and povidone. Clonazepam tablets USP 0.5 mg contain Yellow D&C No. 10 Aluminum Lake. Clonazepam tablets USP 1 mg contain Yellow D&C No. 10 Aluminum Lake, as well as FD&C Blue No. 1 Aluminum Lake. Chemically, Clonazepam, USP is 5-(o-chlorophenyl)-1,3-dihydro-7-nitro-2H-1,4-benzodiazepin-2-one. It is a light yellow crystalline powder. It has the following structural formula: C15H10ClN3O3 M.W. 315.72

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Interactions

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