rasagiline (Rx)

Brand and Other Names:Azilect
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 0.5mg
  • 1mg

Parkinson Disease

Monotherapy: 1 mg PO qDay

Adjunct without levodopa: 1 mg PO qDay

Adjunct to levodopa: 0.5 mg PO qDay initially, may increase to 1 mg/day if needed and tolerated; consider reducing levodopa dose

Dosage Modifications

Coadministration with CYP1A2 inhibitors (eg, ciprofloxacin): Not to exceed 0.5 mg/day

Renal impairment: No dosage adjustment required for mild-to-moderate; not studied in severe

Hepatic impairment

  • Mild (Child-Pugh A): Not to exceed 0.5 mg/day
  • Moderate-to-severe (Child-Pugh B/C): Do not use

Dosing Considerations

Do not exceed recommended doses because of risk for hypertension

<18 years: Safety and efficacy not established

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Interactions

Interaction Checker

and rasagiline

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            Contraindicated (39)

            • apraclonidine

              rasagiline, apraclonidine. Mechanism: unknown. Contraindicated. Apraclonidine should not be used in patients receiving MAO inhibitors.

            • atomoxetine

              rasagiline increases effects of atomoxetine by pharmacodynamic synergism. Contraindicated. The use of atomoxetine with monoamine oxidase inhibitors (MAOIs) is contraindicated. Risk of acute hypertensive episode.

            • brimonidine

              rasagiline, brimonidine. Mechanism: unknown. Contraindicated. Brimonidine should not be used in patients receiving MAO inhibitors.

            • bupropion

              rasagiline and bupropion both increase dopaminergic effects. Contraindicated. Bupropion inhibits reuptake of dopamine and norepinephrine (NE), and MAOIs decrease metabolism of dopamine and NE; coadministration increases risk for hypertensive reactions; allow at least 14 days between discontinuation of MAOI and initiating bupropion

            • cyproheptadine

              rasagiline, cyproheptadine. Other (see comment). Contraindicated. Comment: MAO inhibitors may prolong and intensify the anticholinergic effects of antihistamines. Cyproheptadine may diminish the serotonergic effect of MAO inhibitors.

            • desvenlafaxine

              rasagiline and desvenlafaxine both increase serotonin levels. Contraindicated. At least 14 days should elapse between discontinuation of MAOIs and initiation of treatment with a serotonergic drug

            • deutetrabenazine

              rasagiline, deutetrabenazine. Either increases toxicity of the other by sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Contraindicated. Deutetrabenazine should not be used in combination with an MAOI, or within 14 days of discontinuing therapy with an MAOI.

            • dexmethylphenidate

              rasagiline increases effects of dexmethylphenidate by pharmacodynamic synergism. Contraindicated. Risk of acute hypertensive episode. Dexmethylphenidate use is contraindicated during treatment with MAOIs and also within a minimum of 14 days following discontinuation of treatment with an MAOI.

            • dextroamphetamine

              rasagiline increases effects of dextroamphetamine by pharmacodynamic synergism. Contraindicated. Risk of acute hypertensive episode. Coadministration is contraindicated during or within 14 days following the administration of MAOIs.

            • dextromethorphan

              rasagiline and dextromethorphan both increase serotonin levels. Contraindicated. Risk of psychosis episodes or bizarre behavior.

            • ephedrine

              rasagiline increases effects of ephedrine by pharmacodynamic synergism. Contraindicated. Risk of acute hypertensive episode.

            • fentanyl

              rasagiline increases toxicity of fentanyl by Other (see comment). Contraindicated. Comment: Avoid fentanyl in patients who require concomitant administration MAOIs, or within 14 days of stopping an MAOI. Severe and unpredictable potentiation by MAO inhibitors has been reported with opioid analgesics. .

            • fentanyl intranasal

              rasagiline increases toxicity of fentanyl intranasal by Other (see comment). Contraindicated. Comment: Avoid fentanyl in patients who require concomitant administration MAOIs, or within 14 days of stopping an MAOI. Severe and unpredictable potentiation by MAO inhibitors has been reported with opioid analgesics. .

            • fentanyl transdermal

              rasagiline increases toxicity of fentanyl transdermal by Other (see comment). Contraindicated. Comment: Avoid fentanyl in patients who require concomitant administration MAOIs, or within 14 days of stopping an MAOI. Severe and unpredictable potentiation by MAO inhibitors has been reported with opioid analgesics. .

            • fentanyl transmucosal

              rasagiline increases toxicity of fentanyl transmucosal by Other (see comment). Contraindicated. Comment: Avoid fentanyl in patients who require concomitant administration MAOIs, or within 14 days of stopping an MAOI. Severe and unpredictable potentiation by MAO inhibitors has been reported with opioid analgesics. .

            • isocarboxazid

              rasagiline and isocarboxazid both increase serotonin levels. Contraindicated. Increased risk of hypertensive crisis. At least 14 days should elapse between discontinuation of rasagiline and initiation of another MAOI or discontinuation of another MAOI and initiation of rasagiline.

            • levomilnacipran

              rasagiline and levomilnacipran both increase serotonin levels. Contraindicated. Concomitant use with MAOIs or within 14 days of discontinuing treatment with an MAOI is contraindicated.

            • lisdexamfetamine

              rasagiline increases effects of lisdexamfetamine by pharmacodynamic synergism. Contraindicated. Risk of acute hypertensive episode. Coadministration is contraindicated during or within 14 days following the administration of MAOIs.

              rasagiline, lisdexamfetamine. Either increases effects of the other by serotonin levels. Contraindicated. Do not use amphetamines during and within 14 days of discontinuation of monoamine oxidase inhibitors. .

            • meperidine

              rasagiline and meperidine both increase serotonin levels. Contraindicated. Risk of serious, sometimes fatal reactions from serotonin syndrome.

            • methadone

              rasagiline increases toxicity of methadone by unknown mechanism. Contraindicated. Risk of hypotension, hyperpyrexia, somnolence, or death.

            • methamphetamine

              rasagiline increases effects of methamphetamine by pharmacodynamic synergism. Contraindicated. Risk of acute hypertensive episode. Coadministration is contraindicated during or within 14 days following the administration of MAOIs.

            • methylphenidate

              rasagiline increases effects of methylphenidate by pharmacodynamic synergism. Contraindicated. Risk of acute hypertensive episode. Methylphenidate is contraindicated during treatment with an MAOI and also within a minimum of 14 days following discontinuation of an MAOI.

            • milnacipran

              rasagiline and milnacipran both increase serotonin levels. Contraindicated. Concomitant use with MAOIs or within 14 days of discontinuing treatment with an MAOI is contraindicated.

            • mirtazapine

              rasagiline and mirtazapine both increase serotonin levels. Contraindicated. Avoid combination within 14 days of MAOI use.

            • ozanimod

              rasagiline and ozanimod both increase sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Contraindicated. Coadministration of ozanimod with MAO-B inhibitors may decrease exposure of the active metabolites of ozanimod, which may inhibit MAO. The potential for a clinical interaction with MAO inhibitors has not been studied; however, the increased risk of nonselective MAO inhibition may lead to a hypertensive crisis. Allow at least 14 days to elapse between discontinuing ozanimod and initiating with MAO inhibitors.

            • phenelzine

              rasagiline and phenelzine both increase serotonin levels. Contraindicated. Increased risk of hypertensive crisis. At least 14 days should elapse between discontinuation of rasagiline and initiation of another MAOI or discontinuation of another MAOI and initiation of rasagiline.

            • phenylephrine PO

              rasagiline increases effects of phenylephrine PO by pharmacodynamic synergism. Contraindicated. Risk of acute hypertensive episode.

            • procarbazine

              rasagiline and procarbazine both increase serotonin levels. Contraindicated. At least 2 weeks should elapse between discontinuation of one MAOI and initiation of therapy with the other.

            • pseudoephedrine

              rasagiline increases effects of pseudoephedrine by pharmacodynamic synergism. Contraindicated. Risk of acute hypertensive episode.

            • safinamide

              rasagiline, safinamide. Either increases toxicity of the other by serotonin levels. Contraindicated. Coadministration increases risk of nonselective MAO inhibition, that may lead to hypertensive crisis. At least 14 days should elapse between discontinuating safinamide and initiating MAOIs.

            • selegiline

              rasagiline and selegiline both increase serotonin levels. Contraindicated. Increased risk of hypertensive crisis. At least 14 days should elapse between discontinuation of rasagiline and initiation of another MAOI or discontinuation of another MAOI and initiation of rasagiline.

            • solriamfetol

              rasagiline will increase the level or effect of solriamfetol by sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Contraindicated. Do no use solriamfetol during and/or within 14 days of discontinuing MAOI treatment. MAOIs irreversibly inhibit the enzyme monamine oxidase, an enzyme involved in the degradation of various monoamines, including dopamine and norepinephrine. Solriamfetol increases synaptic dopamine and norepinephrine.

            • St John's Wort

              rasagiline and St John's Wort both increase serotonin levels. Contraindicated.

            • tapentadol

              rasagiline increases toxicity of tapentadol by unknown mechanism. Contraindicated. Concomitant MAOI therapy within the last 14 days is contraindicated. Risk of hypotension, hyperpyrexia, somnolence, or death. .

            • tetrabenazine

              tetrabenazine, rasagiline. Other (see comment). Contraindicated. Comment: Risk of acute hypertensive episode; separate by 14 d. .

            • tramadol

              rasagiline and tramadol both increase serotonin levels. Contraindicated.

            • tranylcypromine

              rasagiline and tranylcypromine both increase serotonin levels. Contraindicated. At least 14 days should elapse between discontinuation of rasagiline and initiation of another MAOI or discontinuation of another MAOI and initiation of rasagiline.

            • vilazodone

              rasagiline, vilazodone. Either increases toxicity of the other by serotonin levels. Contraindicated. Coadministration with MAO inhibitors are contraindicated. Do not prescribe vilazodone within 14 days of discontinuing or starting an MAO inhibitor.

            • vortioxetine

              rasagiline increases toxicity of vortioxetine by serotonin levels. Contraindicated.

            Serious - Use Alternative (70)

            • abametapir

              abametapir will increase the level or effect of rasagiline by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug. For 2 weeks after abametapir application, avoid taking drugs that are CYP1A2 substrates. If not feasible, avoid use of abametapir.

            • alfentanil

              rasagiline increases toxicity of alfentanil by unknown mechanism. Avoid or Use Alternate Drug. May cause additive CNS depression, drowsiness, dizziness or hypotension, so use with MAOIs should be cautious; lower initial dosages of the analgesic are recommended followed by careful titration. Avoid combination within 14 days of MAOI use.

            • almotriptan

              almotriptan and rasagiline both increase serotonin levels. Avoid or Use Alternate Drug. Avoid combination within 14 days of MAOI use

            • amitriptyline

              rasagiline and amitriptyline both increase serotonin levels. Avoid or Use Alternate Drug. Severe CNS toxicity associated with hyperpyrexia has been reported with the combined treatment of an antidepressant and rasagiline. Avoid combination within 14 days of MAOI use.

            • amoxapine

              rasagiline and amoxapine both increase serotonin levels. Avoid or Use Alternate Drug. Severe CNS toxicity associated with hyperpyrexia has been reported with the combined treatment of an antidepressant and rasagiline. Avoid combination within 14 days of MAOI use.

            • benzhydrocodone/acetaminophen

              rasagiline increases toxicity of benzhydrocodone/acetaminophen by serotonin levels. Avoid or Use Alternate Drug. MAOI interactions with opioids may manifest as serotonin syndrome or opioid toxicity (eg, respiratory depression, coma). Opioids are not recommended for patients taking MAOIs or within 14 days of stopping MAOIs. If urgent opioid treatment needed, use test doses and frequent titration of small doses to treat pain while closely monitoring blood pressure and signs and symptoms of CNS and respiratory depression.

            • buprenorphine buccal

              rasagiline increases toxicity of buprenorphine buccal by unknown mechanism. Avoid or Use Alternate Drug. Risk of hypotension, hyperpyrexia, somnolence, or death.

            • buspirone

              rasagiline, buspirone. Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. Risk of acute hypertensive episode. Avoid combination within 14 days of MAOI use.

            • butorphanol

              rasagiline increases toxicity of butorphanol by unknown mechanism. Avoid or Use Alternate Drug. May cause additive CNS depression, drowsiness, dizziness or hypotension, so use with MAOIs should be cautious; lower initial dosages of the analgesic are recommended followed by careful titration. Avoid combination within 14 days of MAOI use.

            • ciprofloxacin

              ciprofloxacin will increase the level or effect of rasagiline by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug. Ciprofloxacin may increase rasagiline concentration resulting in increased adverse reactions. Patients should be closely monitored during concomitant use of these drugs.

            • citalopram

              rasagiline and citalopram both increase serotonin levels. Avoid or Use Alternate Drug. Combination may increase risk of serotonin syndrome or neuroleptic malignant syndrome-like reactions.

            • clomipramine

              rasagiline and clomipramine both increase serotonin levels. Avoid or Use Alternate Drug. Avoid combination within 14 days of MAOI use.

            • codeine

              rasagiline increases toxicity of codeine by unknown mechanism. Avoid or Use Alternate Drug. Risk of hypotension, hyperpyrexia, somnolence, or death.

            • desflurane

              rasagiline increases levels of desflurane by pharmacodynamic synergism. Avoid or Use Alternate Drug.

            • desipramine

              rasagiline and desipramine both increase serotonin levels. Avoid or Use Alternate Drug. Severe CNS toxicity associated with hyperpyrexia has been reported with the combined treatment of an antidepressant and rasagiline. Avoid combination within 14 days of MAOI use.

            • diphenoxylate hcl

              rasagiline increases toxicity of diphenoxylate hcl by unknown mechanism. Avoid or Use Alternate Drug. Chemical structure of diphenoxylate is similar to meperidine, concurrent use may precipitate hypertensive crises.

            • dolasetron

              dolasetron, rasagiline. Either increases toxicity of the other by serotonin levels. Avoid or Use Alternate Drug.

            • doxepin

              rasagiline and doxepin both increase serotonin levels. Avoid or Use Alternate Drug. Severe CNS toxicity associated with hyperpyrexia has been reported with the combined treatment of an antidepressant and rasagiline. Avoid combination within 14 days of MAOI use.

            • duloxetine

              rasagiline and duloxetine both increase serotonin levels. Avoid or Use Alternate Drug. Severe CNS toxicity associated with hyperpyrexia has been reported with the combined treatment of an antidepressant and rasagiline. Avoid combination within 14 days of MAOI use.

            • eletriptan

              eletriptan and rasagiline both increase serotonin levels. Avoid or Use Alternate Drug. Avoid combination within 14 days of MAOI use

            • escitalopram

              rasagiline and escitalopram both increase serotonin levels. Avoid or Use Alternate Drug. Severe CNS toxicity associated with hyperpyrexia has been reported with the combined treatment of an antidepressant and rasagiline. Avoid combination within 14 days of MAOI use.

            • fluoxetine

              rasagiline and fluoxetine both increase serotonin levels. Avoid or Use Alternate Drug. evere CNS toxicity associated with hyperpyrexia has been reported with the combined treatment of an antidepressant and rasagiline. Avoid combination within 14 days of MAOI use.

            • fluvoxamine

              fluvoxamine and rasagiline both increase serotonin levels. Avoid or Use Alternate Drug. Severe CNS toxicity associated with hyperpyrexia reported with combined treatment of antidepressant and rasagiline; avoid combination within 14 days of MAOI use

            • frovatriptan

              frovatriptan and rasagiline both increase serotonin levels. Avoid or Use Alternate Drug. Avoid combination within 14 days of MAOI use

            • givosiran

              givosiran will increase the level or effect of rasagiline by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of sensitive CYP1A2 substrates with givosiran. If unavoidable, decrease the CYP1A2 substrate dosage in accordance with approved product labeling.

            • granisetron

              granisetron, rasagiline. Either increases toxicity of the other by serotonin levels. Avoid or Use Alternate Drug.

            • hydrocodone

              rasagiline increases toxicity of hydrocodone by serotonin levels. Avoid or Use Alternate Drug. MAOI interactions with opioids may manifest as serotonin syndrome or opioid toxicity (eg, respiratory depression, coma). Opioids are not recommended for patients taking MAOIs or within 14 days of stopping MAOIs. If urgent opioid treatment needed, use test doses and frequent titration of small doses to treat pain while closely monitoring blood pressure and signs and symptoms of CNS and respiratory depression.

            • hydromorphone

              rasagiline increases toxicity of hydromorphone by unknown mechanism. Avoid or Use Alternate Drug. May cause additive CNS depression, drowsiness, dizziness or hypotension, so use with MAOIs should be cautious; lower initial dosages of the analgesic are recommended followed by careful titration. Avoid combination within 14 days of MAOI use.

            • imipramine

              rasagiline and imipramine both increase serotonin levels. Avoid or Use Alternate Drug. Severe CNS toxicity associated with hyperpyrexia has been reported with the combined treatment of an antidepressant and rasagiline. Avoid combination within 14 days of MAOI use.

            • iobenguane I 131

              rasagiline will decrease the level or effect of iobenguane I 131 by Other (see comment). Avoid or Use Alternate Drug. Based on the mechanism of action of iobenguane, drugs that reduce catecholamine uptake or that deplete catecholamine stores may interfere with iobenguane uptake into cells, and thus, reduce iobenguane efficacy. Discontinue interfering drugs for at least 5 half-lives before administration of either the dosimetry or an iobenguane dose. Do not administer these drugs until at least 7 days after each iobenguane dose.

            • ketamine

              rasagiline increases levels of ketamine by pharmacodynamic synergism. Avoid or Use Alternate Drug.

            • levorphanol

              rasagiline increases toxicity of levorphanol by unknown mechanism. Avoid or Use Alternate Drug. Risk of hypotension, hyperpyrexia, somnolence, or death.

            • linezolid

              rasagiline and linezolid both increase serotonin levels. Avoid or Use Alternate Drug. Linezolid may increase serotonin as a result of MAO-A inhibition. If linezolid must be administered, discontinue serotonergic drug immediately and monitor for CNS toxicity. Serotonergic therapy may be resumed 24 hours after last linezolid dose or after 2 weeks of monitoring, whichever comes first.

            • lorcaserin

              rasagiline and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • maprotiline

              rasagiline and maprotiline both increase serotonin levels. Avoid or Use Alternate Drug.

            • methylene blue

              methylene blue and rasagiline both increase serotonin levels. Avoid or Use Alternate Drug. Both methylene blue and rasagiline may increase serotonin as a result of MAO-A inhibition. If methylene blue must be administered, discontinue serotonergic drug immediately and monitor for CNS toxicity. Serotonergic therapy may be resumed 24 hours after last methylene blue dose or after 2 weeks of monitoring, whichever comes first.

            • metoclopramide intranasal

              rasagiline, metoclopramide intranasal. Either increases effects of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Avoid use of metoclopramide intranasal or interacting drug, depending on importance of drug to patient.

              metoclopramide intranasal increases toxicity of rasagiline by Other (see comment). Avoid or Use Alternate Drug. Comment: Metoclopramide may enhance the hypertensive effect of monoamine oxidase inhibitors.

            • midodrine

              rasagiline increases effects of midodrine by pharmacodynamic synergism. Avoid or Use Alternate Drug. Midodrine should not be given concurrently with monoamine oxidase inhibitors (MAOIs). Risk of acute hypertensive episode.

            • morphine

              rasagiline increases toxicity of morphine by unknown mechanism. Avoid or Use Alternate Drug. May cause additive CNS depression, drowsiness, dizziness or hypotension, so use with MAOIs should be cautious; lower initial dosages of the analgesic are recommended followed by careful titration. Avoid combination within 14 days of MAOI use.

            • nalbuphine

              rasagiline increases toxicity of nalbuphine by unknown mechanism. Avoid or Use Alternate Drug. May cause additive CNS depression, drowsiness, dizziness or hypotension, so use with MAOIs should be cautious; lower initial dosages of the analgesic are recommended followed by careful titration. Avoid combination within 14 days of MAOI use.

            • naratriptan

              naratriptan and rasagiline both increase serotonin levels. Avoid or Use Alternate Drug. Avoid combination within 14 days of MAOI use

            • nefazodone

              rasagiline and nefazodone both increase serotonin levels. Avoid or Use Alternate Drug. Do not use nefazodone in combination with a MAOI, or within 14 days of discontinuing treatment with a MAOI. Allow at least 1 week after stopping nefazodone before starting an MAOI.

            • netupitant/palonosetron

              netupitant/palonosetron, rasagiline. Either increases toxicity of the other by serotonin levels. Avoid or Use Alternate Drug.

            • nortriptyline

              rasagiline and nortriptyline both increase serotonin levels. Avoid or Use Alternate Drug. Severe CNS toxicity associated with hyperpyrexia has been reported with the combined treatment of an antidepressant and rasagiline. Avoid combination within 14 days of MAOI use.

            • ondansetron

              ondansetron, rasagiline. Either increases toxicity of the other by serotonin levels. Avoid or Use Alternate Drug.

            • oxycodone

              rasagiline increases toxicity of oxycodone by unknown mechanism. Avoid or Use Alternate Drug. May cause additive CNS depression, drowsiness, dizziness or hypotension, so use with MAOIs should be cautious; lower initial dosages of the analgesic are recommended followed by careful titration. Avoid combination within 14 days of MAOI use.

            • oxymorphone

              rasagiline increases toxicity of oxymorphone by unknown mechanism. Avoid or Use Alternate Drug. May cause additive CNS depression, drowsiness, dizziness or hypotension, so use with MAOIs should be cautious; lower initial dosages of the analgesic are recommended followed by careful titration. Avoid combination within 14 days of MAOI use.

            • palonosetron

              palonosetron, rasagiline. Either increases toxicity of the other by serotonin levels. Avoid or Use Alternate Drug.

            • paroxetine

              rasagiline and paroxetine both increase serotonin levels. Avoid or Use Alternate Drug. Severe CNS toxicity associated with hyperpyrexia has been reported with the combined treatment of an antidepressant and rasagiline. Avoid combination within 14 days of MAOI use.

            • pentazocine

              rasagiline increases toxicity of pentazocine by unknown mechanism. Avoid or Use Alternate Drug. May cause additive CNS depression, drowsiness, dizziness or hypotension, so use with MAOIs should be cautious; lower initial dosages of the analgesic are recommended followed by careful titration. Avoid combination within 14 days of MAOI use.

            • phendimetrazine

              rasagiline increases effects of phendimetrazine by pharmacodynamic synergism. Avoid or Use Alternate Drug. Phendimetrazine should not be administered during or within 14 days following the use of most MAOIs or drugs with MAO-inhibiting activity. Risk of acute hypertensive episode.

            • phentermine

              rasagiline increases effects of phentermine by pharmacodynamic synergism. Avoid or Use Alternate Drug. Phentermine should not be administered during or within 14 days following the use of most MAOIs or drugs with MAO-inhibiting activity. Risk of acute hypertensive episode. .

            • propofol

              rasagiline increases levels of propofol by pharmacodynamic synergism. Avoid or Use Alternate Drug.

            • protriptyline

              rasagiline and protriptyline both increase serotonin levels. Avoid or Use Alternate Drug. Severe CNS toxicity associated with hyperpyrexia has been reported with the combined treatment of an antidepressant and rasagiline. Avoid combination within 14 days of MAOI use.

            • rizatriptan

              rizatriptan and rasagiline both increase serotonin levels. Avoid or Use Alternate Drug. Avoid combination within 14 days of MAOI use

            • selegiline transdermal

              rasagiline and selegiline transdermal both increase serotonin levels. Avoid or Use Alternate Drug.

            • sertraline

              rasagiline and sertraline both increase serotonin levels. Avoid or Use Alternate Drug. Severe CNS toxicity associated with hyperpyrexia has been reported with the combined treatment of an antidepressant and rasagiline. Avoid combination within 14 days of MAOI use.

            • sevoflurane

              rasagiline increases levels of sevoflurane by pharmacodynamic synergism. Avoid or Use Alternate Drug.

            • sufentanil

              rasagiline increases toxicity of sufentanil by unknown mechanism. Avoid or Use Alternate Drug. May cause additive CNS depression, drowsiness, dizziness or hypotension, so use with MAOIs should be cautious; lower initial dosages of the analgesic are recommended followed by careful titration. Avoid combination within 14 days of MAOI use.

            • sufentanil SL

              rasagiline increases toxicity of sufentanil SL by serotonin levels. Avoid or Use Alternate Drug. MAOI interactions with opioids may manifest as serotonin syndrome or opioid toxicity (eg, respiratory depression, coma). Opioids are not recommended for patients taking MAOIs or within 14 days of stopping MAOIs. If urgent opioid treatment needed, use test doses and frequent titration of small doses to treat pain while closely monitoring blood pressure and signs and symptoms of CNS and respiratory depression.

            • sumatriptan

              sumatriptan and rasagiline both increase serotonin levels. Avoid or Use Alternate Drug. Avoid combination within 14 days of MAOI use

            • tedizolid

              tedizolid, rasagiline. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. Interaction with MAOIs were not studied in clinical trials; drugs within the same class(eg linezolid) are contraindicated with MAOIs.

            • trazodone

              rasagiline and trazodone both increase serotonin levels. Avoid or Use Alternate Drug. Trazodone should not be coadministered with a MAOI or within 14 days of discontinuing a MAOI. Similarly, a MAOI should not be given within 14 days of stopping trazodone.

            • trimipramine

              rasagiline and trimipramine both increase serotonin levels. Avoid or Use Alternate Drug. Severe CNS toxicity associated with hyperpyrexia has been reported with the combined treatment of an antidepressant and rasagiline. Avoid combination within 14 days of MAOI use.

            • umeclidinium bromide/vilanterol inhaled

              rasagiline and umeclidinium bromide/vilanterol inhaled both increase sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Avoid or Use Alternate Drug. Exercise extreme caution if vilanterol coadministered with MAOIs or TCAs, or within 2 weeks of discontinuation of these drugs; adrenergic agonist effects on the cardiovascular system may be potentiated

            • valbenazine

              rasagiline, valbenazine. Other (see comment). Avoid or Use Alternate Drug. Comment: Coadministration of valbenazine with MAOIs may increase monoamine neurotransmitter concentration in synapses, potentially increasing risk of serotonin syndrome or attenuating valbenazine effect.

            • venlafaxine

              rasagiline and venlafaxine both increase serotonin levels. Avoid or Use Alternate Drug. Severe CNS toxicity associated with hyperpyrexia has been reported with the combined treatment of an antidepressant and rasagiline. Avoid combination within 14 days of MAOI use.

            • vilanterol/fluticasone furoate inhaled

              rasagiline and vilanterol/fluticasone furoate inhaled both increase sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Avoid or Use Alternate Drug. Exercise extreme caution if vilanterol coadministered with MAOIs or TCAs, or within 2 weeks of discontinuation of these drugs; adrenergic agonist effects on the cardiovascular system may be potentiated

            • yohimbine

              rasagiline increases effects of yohimbine by pharmacodynamic synergism. Avoid or Use Alternate Drug. Risk of acute hypertensive episode. It is recommended to avoid yohimbine during MAOI therapy and for 2 weeks after the discontinuation of a MAOI.

            • zolmitriptan

              zolmitriptan and rasagiline both increase serotonin levels. Avoid or Use Alternate Drug. Avoid combination within 14 days of MAOI use

            Monitor Closely (62)

            • 5-HTP

              rasagiline and 5-HTP both increase serotonin levels. Modify Therapy/Monitor Closely.

            • armodafinil

              rasagiline increases effects of armodafinil by pharmacodynamic synergism. Use Caution/Monitor. Risk of acute hypertensive episode. Use caution when administering MAOIs and armodafinil.

            • benazepril

              rasagiline, benazepril. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Increases risk of hypotension.

            • bretylium

              rasagiline increases effects of bretylium by sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Modify Therapy/Monitor Closely. Bretylium produces release of catecholamines from nerve endings. This increased catecholamine release is potentiated by MAOIs.

            • buprenorphine subdermal implant

              rasagiline, buprenorphine subdermal implant. Either increases toxicity of the other by serotonin levels. Use Caution/Monitor. Concomitant use could result in life-threatening serotonin syndrome. If concomitant use is warranted, carefully observe the patient, particularly during treatment initiation, and during dose adjustment of the serotonergic drug. Discontinue buprenorphine if serotonin syndrome is suspected.

            • buprenorphine, long-acting injection

              rasagiline, buprenorphine, long-acting injection. Either increases toxicity of the other by serotonin levels. Modify Therapy/Monitor Closely. Concomitant use could result in life-threatening serotonin syndrome or opioid toxicity (eg, respiratory depression, coma). Buprenorphine long-acting injection is not recommended for patients taking MAOIs or within 14 days of stopping such treatment.

            • caffeine

              rasagiline increases effects of caffeine by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Risk of acute hypertensive episode.

            • cannabidiol

              cannabidiol, rasagiline. affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Owing to the potential for both CYP1A2 induction and inhibition with the coadministration of CYP1A2 substrates and cannabidiol, consider reducing dosage adjustment of CYP1A2 substrates as clinically appropriate.

            • captopril

              rasagiline, captopril. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Both drugs lower blood pressure. Monitor blood pressure.

            • cimetidine

              cimetidine will increase the level or effect of rasagiline by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor. Recommended dose of rasagiline is 0.5mg daily in combination with CYP1A2 inhibitors.

            • cocaine

              rasagiline and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • cyclobenzaprine

              rasagiline and cyclobenzaprine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • deferasirox

              deferasirox increases levels of rasagiline by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.

            • diethylpropion

              rasagiline increases effects of diethylpropion by pharmacodynamic synergism. Use Caution/Monitor. Risk of acute hypertensive episode.

            • difenoxin hcl

              rasagiline increases toxicity of difenoxin hcl by unknown mechanism. Use Caution/Monitor. Chemical structure of difenoxin is similar to meperidine, concurrent use with MAOIs may, in theory, precipitate a hypertensive crisis. Risk of hypotension, hyperpyrexia, somnolence, or death.

            • dihydroergotamine

              rasagiline and dihydroergotamine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • dihydroergotamine intranasal

              rasagiline and dihydroergotamine intranasal both increase serotonin levels. Modify Therapy/Monitor Closely.

            • dobutamine

              rasagiline increases effects of dobutamine by pharmacodynamic synergism. Use Caution/Monitor. Risk of acute hypertensive episode.

            • dopamine

              rasagiline increases effects of dopamine by pharmacodynamic synergism. Use Caution/Monitor. Risk of acute hypertensive episode.

            • epinephrine

              rasagiline increases effects of epinephrine by pharmacodynamic synergism. Use Caution/Monitor. Avoid concomitant use if possible. Caution is advised.

            • ergotamine

              rasagiline and ergotamine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • erythromycin base

              erythromycin base will increase the level or effect of rasagiline by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.

            • erythromycin ethylsuccinate

              erythromycin ethylsuccinate will increase the level or effect of rasagiline by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.

            • erythromycin lactobionate

              erythromycin lactobionate will increase the level or effect of rasagiline by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.

            • erythromycin stearate

              erythromycin stearate will increase the level or effect of rasagiline by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.

            • ethinylestradiol

              ethinylestradiol will increase the level or effect of rasagiline by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor. Recommended dose of rasagiline is 0.5mg daily in combination with CYP1A2 inhibitors.

            • fexinidazole

              fexinidazole will increase the level or effect of rasagiline by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.

            • glipizide

              rasagiline increases effects of glipizide by unknown mechanism. Use Caution/Monitor.

            • green tea

              green tea, rasagiline. Other (see comment). Use Caution/Monitor. Comment: Avoid combination or excessive consumption of green tea. Combination may increase risk of cardiac arrhythmias or severe hypertension can occur due to caffeine component of green tea.

            • insulin aspart

              rasagiline increases effects of insulin aspart by unknown mechanism. Use Caution/Monitor.

            • insulin detemir

              rasagiline increases effects of insulin detemir by unknown mechanism. Use Caution/Monitor.

            • insulin glargine

              rasagiline increases effects of insulin glargine by unknown mechanism. Use Caution/Monitor.

            • insulin glulisine

              rasagiline increases effects of insulin glulisine by unknown mechanism. Use Caution/Monitor.

            • insulin lispro

              rasagiline increases effects of insulin lispro by unknown mechanism. Use Caution/Monitor.

            • insulin NPH

              rasagiline increases effects of insulin NPH by unknown mechanism. Use Caution/Monitor.

            • isoniazid

              isoniazid will increase the level or effect of rasagiline by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor. Isoniazid shows only negligible inhibition of CYP1A2, caution is advised. Recommended dose of rasagiline is 0.5mg daily in combination with CYP1A2 inhibitors.

              rasagiline and isoniazid both increase serotonin levels. Modify Therapy/Monitor Closely.

            • isoproterenol

              rasagiline increases effects of isoproterenol by pharmacodynamic synergism. Use Caution/Monitor. Avoid concomitant use if possible. Caution is advised.

            • L-tryptophan

              rasagiline and L-tryptophan both increase serotonin levels. Modify Therapy/Monitor Closely.

            • lasmiditan

              rasagiline increases effects of lasmiditan by serotonin levels. Use Caution/Monitor. Coadministration may increase risk of serotonin syndrome.

            • levodopa

              rasagiline, levodopa. Mechanism: pharmacodynamic synergism. Modify Therapy/Monitor Closely. Risk of acute hypertensive episode.

            • levodopa inhaled

              levodopa inhaled increases effects of rasagiline by dopaminergic effects. Use Caution/Monitor. Coadministration of selective MAO-B inhibitors with levodopa may be associated with orthostatic hypotension.

            • lurasidone

              lurasidone increases effects of rasagiline by Other (see comment). Use Caution/Monitor. Comment: Potential for increased risk of hypotension with concurrent use. Monitor blood pressure and adjust dose of antihypertensive agent as needed.

            • metformin

              rasagiline will increase the level or effect of metformin by unspecified interaction mechanism. Use Caution/Monitor.

            • mexiletine

              mexiletine will increase the level or effect of rasagiline by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor. Recommended dose of rasagiline is 0.5mg daily in combination with CYP1A2 inhibitors.

            • midazolam intranasal

              midazolam intranasal, rasagiline. Either increases toxicity of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Concomitant use of barbiturates, alcohol, or other CNS depressants may increase the risk of hypoventilation, airway obstruction, desaturation, or apnea and may contribute to profound and/or prolonged drug effect.

            • modafinil

              rasagiline increases effects of modafinil by pharmacodynamic synergism. Use Caution/Monitor. Risk of acute hypertensive episode. Use caution when administering MAOIs and modafinil.

            • norepinephrine

              rasagiline increases effects of norepinephrine by pharmacodynamic synergism. Use Caution/Monitor. Risk of acute hypertensive episode.

            • oliceridine

              rasagiline, oliceridine. Either increases effects of the other by serotonin levels. Modify Therapy/Monitor Closely.

            • opium tincture

              rasagiline increases toxicity of opium tincture by unknown mechanism. Use Caution/Monitor. Risk of hypotension, hyperpyrexia, somnolence, or death.

            • peginterferon alfa 2a

              peginterferon alfa 2a will increase the level or effect of rasagiline by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor. Recommended dose of rasagiline is 0.5mg daily in combination with CYP1A2 inhibitors.

            • phenobarbital

              phenobarbital will decrease the level or effect of rasagiline by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.

            • phenylephrine

              rasagiline increases effects of phenylephrine by pharmacodynamic synergism. Use Caution/Monitor. Risk of acute hypertensive episode.

            • primidone

              primidone will decrease the level or effect of rasagiline by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.

            • rifampin

              rifampin will decrease the level or effect of rasagiline by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor. Rifampin is a relatively weak inducer of CYP1A2, caution is advised.

            • rucaparib

              rucaparib will increase the level or effect of rasagiline by affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP1A2 substrates, if clinically indicated.

            • SAMe

              rasagiline and SAMe both increase serotonin levels. Use Caution/Monitor.

            • stiripentol

              stiripentol, rasagiline. affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Stiripentol is a CYP1A2 inhibitor and inducer. Monitor CYP1A2 substrates coadministered with stiripentol for increased or decreased effects. CYP1A2 substrates may require dosage adjustment.

            • sumatriptan intranasal

              sumatriptan intranasal and rasagiline both increase serotonin levels. Modify Therapy/Monitor Closely.

            • tapentadol

              rasagiline and tapentadol both increase serotonin levels. Modify Therapy/Monitor Closely.

            • teriflunomide

              teriflunomide decreases levels of rasagiline by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.

            • tyramine

              rasagiline increases effects of tyramine by pharmacodynamic synergism. Use Caution/Monitor. Risk of acute hypertensive episode. Tyramine containing foods include cheese, red wine, caviar, herring, canned figs, fermented meats, fava beans, yeast extracts, miso, avocado.

            • zileuton

              zileuton will increase the level or effect of rasagiline by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor. Recommended dose of rasagiline is 0.5mg daily in combination with CYP1A2 inhibitors.

            Minor (1)

            • primidone

              rasagiline increases levels of primidone by decreasing metabolism. Minor/Significance Unknown. Theoretical interaction.

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            Adverse Effects

            >10%

            EPS (dyskinesia/dystonia) (18%)

            Headache (14%)

            Nausea (10-12%)

            1-10%

            Postural hypotension (6-9%)

            Constipation (4-9%)

            Weight loss (2-9%)

            Arthralgia (7%)

            Dyspepsia (7%)

            Xerostomia (2-6%)

            Depression (5%)

            Fall (5%)

            Flu-like syndrome (5%)

            Hallucination (4-5%)

            Conjunctivitis (3%)

            Fever (3%)

            Gastroenteritis (3%)

            Rhinitis (3%)

            Arthritis (2%)

            Bruising (2%)

            Malaise (2%)

            Neck pain (2%)

            Parasthesia (2%)

            Vertigo (2%)

            <1%

            CVA

            MI

            Bundle branch block

            Gastrointestinal hemorrhage

            Postmarketing Reports

            Skin and Subcutaneous Tissue Disorders: Melanoma

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            Warnings

            Contraindications

            Coadministration with meperidine, tramadol, methadone, and MAOIs, including other selective MAO-B inhibitors increases risk of serotonin syndrome; at least 14 days should elapse between discontinuation of rasagiline and initiation of treatment with these medications

            Coadministration with St. John’s wort and with cyclobenzaprine

            Coadministration with dextromethorphan because of risk of episode of psychosis or bizarre behavior

            Cautions

            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

            May exacerbate hypertension; antihypertensive drugs may require dosage adjustment

            May cause hypotension, especially orthostatic

            May cause or exacerbate dyskinesia; decreasing the levodopa dose may lessen or eliminate this side effect

            Withdrawal-emergent hyperpyrexia and confusion reported with rapid dose reduction of drugs that increase central dopaminergic tone; this is characterized by elevated temperature, muscular rigidity, altered consciousness, and autonomic instability

            Patients with Parkinson disease have a higher risk (2 to 6-fold higher) of developing melanoma than the general population; unclear if this is due to the disease or other factors (eg, drug therapy); monitor for melanomas frequently and on a regular basis

            Psychiatric effects

            • Hallucinations and psychotic-like behavior reported
            • The abnormal thinking and behavior can consist of one or more of a variety of manifestations including paranoid ideation, delusions, hallucinations, confusion, psychotic-like behavior, disorientation, aggressive behavior, agitation, and delirium
            • Patients should be informed of the possibility of developing hallucinations and instructed to report them to their healthcare provider promptly should they develop
            • Patients with a major psychotic disorder should ordinarily not be treated because of risk of exacerbating the psychosis with an increase in central dopaminergic tone; in addition, many treatments for psychosis that decrease central dopaminergic tone may decrease therapy effectiveness
            • Consider dose reduction or stopping medication if a patient develops hallucinations or psychotic-like behaviors while taking drug

            Falling asleep and somnolence

            • Daytime drowsiness and somnolence reported during activities of daily living
            • Prescribers should monitor patients for drowsiness or sleepiness, because some of the events occur well after initiation of treatment with dopaminergic medication
            • Prescribers should also be aware that patients may not acknowledge drowsiness or sleepiness until directly questioned about drowsiness or sleepiness during specific activities
            • Although many patients have reported somnolence while on therapy with rasagiline and other dopaminergic medications, some perceived that they had no warning signs, such as excessive drowsiness, and believed that they were alert immediately prior to activities that resulted in accidents
            • Before initiating treatment, patients should be advised of potential to develop drowsiness and specifically asked about factors that may increase risk with therapy such as concomitant sedating medications, presence of sleep disorders, and concomitant medications that increase rasagiline plasma levels (eg, ciprofloxacin)
            • If a patient develops significant daytime sleepiness or episodes of falling asleep during activities that require active participation (eg, driving a motor vehicle, conversations, eating), therapy should ordinarily be discontinued
            • If a decision is made to continue patients on therapy, advise them to avoid driving and other potentially dangerous activities; there is insufficient information to establish that dose reduction will eliminate episodes of falling asleep while engaged in activities of daily living

            Tyramine

            • Dietary tyramine restriction is not required during treatment with recommended doses; however, certain foods may contain very high amounts (ie, > 150 mg) of tyramine that could potentially cause severe hypertension, including various clinical syndromes referred to as hypertensive urgency, crisis, or emergency, in patients receiving therapy, even at 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 potential for large increases in blood pressure including clinical syndromes referred to as hypertensive urgency, crisis, or emergency

            Serotonin syndrome

            • Serotonin syndrome has been reported with concomitant use of an antidepressant (eg, selective serotonin reuptake inhibitors-SSRIs, serotonin-norepinephrine reuptake inhibitors-SNRIs, tricyclic antidepressants, tetracyclic antidepressants, triazolopyridine antidepressants) and a nonselective MAOI (eg, phenelzine, tranylcypromine) or selective MAO-B inhibitors, such as selegiline and rasagiline
            • Serotonin syndrome has been reported with concomitant use of rasagiline with meperidine, tramadol, methadone, or propoxyphene; rasagiline is contraindicated for use with meperidine, tramadol, methadone, propoxyphene, and MAO inhibitors (MAOIs), including other selective MAO-B inhibitors
            • In postmarketing period, potentially life-threatening serotonin syndrome reported in patients treated with antidepressants concomitantly with drug
            • Concomitant use with one of many classes of antidepressants (eg, SSRIs, SNRIs, triazolopyridine, tricyclic or tetracyclic antidepressants) not recommended [
            • The symptoms of serotonin syndrome have included behavioral and cognitive/mental status changes (eg, confusion, hypomania, hallucinations, agitation, delirium, headache, and coma), autonomic effects (eg, syncope, shivering, sweating, high fever/hyperthermia, hypertension, tachycardia, nausea, diarrhea), and somatic effects (eg, muscular rigidity, myoclonus, muscle twitching, hyperreflexia manifested by clonus, and tremor)
            • At least 14 days should elapse between discontinuation of rasagiline and initiation of treatment with a SSRI, SNRI, tricyclic, tetracyclic, or triazolopyridine antidepressant
            • Because of long half-lives of certain antidepressants (eg, fluoxetine and its active metabolite), at least five weeks (perhaps longer, especially if fluoxetine has been prescribed chronically and/or at higher doses) should elapse between discontinuation of fluoxetine and initiation of rasagiline

            Compulsive behavior

            • Impulse control/compulsive behaviors reported; case reports describe patients with intense urges to gamble, increased sexual urges, intense urges to spend money, or binge eat, and the inability to control these urges while taking one or more of the medications that increase central dopaminergic tone and that are generally used for the treatment of Parkinson’s disease
            • In some cases, although not all, these urges were reported to have stopped when the dose was reduced or the medication was discontinued; because patients may not recognize these behaviors as abnormal, it is important for prescribers to specifically ask patients or their caregivers about the development of new or increased gambling urges, sexual urges, uncontrolled spending, or other urges while receiving therapy
            • Consider dose reduction or stopping medication if a patient develops such urges while taking medication
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            Pregnancy & Lactation

            Pregnancy

            There are no adequate data on developmental risks associated with use in pregnant women; in animal studies, oral administration to rats during gestation and lactation resulted in decreased survival and reduced body weight in offspring at doses similar to those used clinically; when administered to pregnant animals in combination with levodopa/carbidopa, there were increased incidences of fetal skeletal variations in rats and increases in embryofetal death and cardiovascular abnormalities in rabbits

            Animal data

            • In pregnant rats administered rasagiline (0, 0.1, 0.3, 1 mg/kg/day) orally during gestation and lactation, offspring survival was decreased and offspring body weight was reduced at 0.3 mg/kg/day and 1 mg/kg/day (10 and 16 times plasma AUC in humans at MRHD); the no-effect dose (0.1 mg/kg) for adverse developmental effects is similar to the MRHD on a body surface area (mg/m2) basis; effect of drug on physical and behavioral development was not adequately assessed in this study

            Lactation

            There are no data on presence of drug in human milk or effects on breastfed infant; in rats, rasagiline was shown to inhibit prolactin secretion; the clinical relevance in humans is unknown, and there are no data on effects of rasagiline on prolactin secretion in humans

            The developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and potential adverse effects on breastfed infant from drug or from underlying maternal condition

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Monoamine oxidase inhibitor, selective Type-B; inhibits dopamine depletion in striatal region of the brain, which in turn reduces symptomatic motor deficits of Parkinson's disease

            Absorption

            Peak Plasma Time: 1 hr

            Onset of action: Within 1 hr

            Bioavailability: 36%

            Distribution

            Protein Bound: 88-94%

            Vd: 87 L

            Metabolism

            Via liver, primarily CYP1A2 (in vitro data)

            Metabolites: 1-aminoindan, 3-hydroxy-N-propargyl-1-aminoindan, 3-hydroxy-1-aminoindan

            Elimination

            Half-life: 1.3-3 hr

            Excretion: 62% urine; 7% feces

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            Images

            BRAND FORM. UNIT PRICE PILL IMAGE
            Azilect oral
            -
            1 mg tablet
            Azilect oral
            -
            0.5 mg tablet
            rasagiline oral
            -
            0.5 mg tablet
            rasagiline oral
            -
            1 mg tablet
            rasagiline oral
            -
            0.5 mg tablet
            rasagiline oral
            -
            0.5 mg tablet
            rasagiline oral
            -
            1 mg tablet
            rasagiline oral
            -
            1 mg tablet
            rasagiline oral
            -
            1 mg tablet
            rasagiline oral
            -
            0.5 mg tablet

            Copyright © 2010 First DataBank, Inc.

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            Patient Handout

            Patient Education
            rasagiline oral

            RASAGILINE - ORAL

            (ra-SA-ji-leen)

            COMMON BRAND NAME(S): Azilect

            USES: Rasagiline is used alone or with other medications (such as levodopa/carbidopa) to treat symptoms of Parkinson's disease. It can help improve symptoms such as shakiness, stiffness, and difficulty moving. It can also help reduce the amount of "off" time (periods of slow movement or stiffness).Rasagiline belongs to a class of drugs known as MAO inhibitors. It works by increasing the levels of certain natural substances in the brain (such as dopamine, norepinephrine, serotonin). Parkinson's disease is thought to be caused by too little dopamine in the brain.

            HOW TO USE: Take this medication by mouth with or without food as directed by your doctor, usually once daily.The dosage is based on your medical condition, response to treatment, and other medications you may be taking. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products). Do not increase your dose or take it more often than prescribed. Your condition will not improve any faster, and your risk of side effects will increase.Do not stop taking this medication without consulting your doctor. Some conditions may become worse when this drug is suddenly stopped. Your dose may need to be gradually decreased.A very serious high blood pressure reaction may rarely occur if you eat a large amount of tyramine while taking rasagiline and for 2 weeks after you stop it. Avoid foods that are high in tyramine, like aged cheeses (such as Stilton cheese). Consult your doctor or dietician about which foods you should avoid and if you do not feel well after eating or drinking certain foods while taking this medication. See also Side Effects section.Tell your doctor if this medication stops working well or if your condition gets worse.

            SIDE EFFECTS: Dizziness, drowsiness, joint pain, heartburn, nausea, dry mouth, weight loss, or stomach/abdominal pain may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.To reduce the risk of dizziness and lightheadedness, get up slowly when rising from a sitting or lying position, especially when you first start taking rasagiline.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: fainting, loss of balance, mental/mood changes (such as confusion, depression, hallucinations), worsening muscle stiffness/twitching/uncontrollable movements, swollen ankles/legs, easy bleeding/bruising, unusual strong urges (such as increased gambling, increased sexual urges).Some people taking rasagiline have fallen asleep suddenly during their usual daily activities (such as talking on the phone, driving). In some cases, sleep occurred without any feelings of drowsiness beforehand. This sleep effect may occur anytime during treatment with rasagiline even if you have used this medication for a long time. If you experience increased sleepiness or fall asleep during the day, do not drive or take part in other possibly dangerous activities until you have discussed this effect with your doctor. Your risk of this sleep effect is increased by using alcohol or other medications that can make you drowsy. See also Precautions section.This medication may increase serotonin and rarely cause a very serious condition called serotonin syndrome/toxicity. The risk increases if you are also taking other drugs that increase serotonin, so tell your doctor or pharmacist of all the drugs you take. Get medical help right away if you develop some of the following symptoms: fast heartbeat, hallucinations, loss of coordination, severe dizziness, severe nausea/vomiting/diarrhea, twitching muscles, unexplained fever, unusual agitation/restlessness.This drug may rarely cause an attack of extremely high blood pressure (hypertensive crisis), which may be fatal. Many drug and food interactions can increase this risk (see How to Use and Drug Interactions sections). Get medical help right away if any of these serious side effects occur: severe headache, fast/slow/irregular/pounding heartbeat, chest pain, neck stiffness/soreness, severe nausea/vomiting, sweating/clammy skin (sometimes with fever), widened pupils, vision changes (such as double/blurred vision), sudden sensitivity to light (photophobia).A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

            PRECAUTIONS: Before taking rasagiline, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: heart disease (such as coronary artery disease, heart attack, chest pain, heart failure), stroke, high blood pressure, severe/frequent headaches, liver disease, mental/mood disorders (such as schizophrenia, bipolar disorder, depression), diabetes, overactive thyroid, a certain kind of adrenal gland tumor (pheochromocytoma), sleep disorders.This drug may make you dizzy or drowsy. Alcohol or marijuana (cannabis) can make you more dizzy or drowsy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Limit alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis). See also Side Effects section.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.It is unknown if this drug passes into breast milk. Consult your doctor before breast-feeding.

            DRUG INTERACTIONS: See also How to Use section.Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Some products that may interact with this drug include: diet pills/appetite suppressants (such as diethylpropion), drugs for attention deficit disorder (such as atomoxetine, methylphenidate), apraclonidine, bupropion, buspirone, carbamazepine, cyclobenzaprine, deutetrabenazine, dextromethorphan, methyldopa, metoclopramide, certain supplements (such as tryptophan, tyramine), tetrabenazine, certain "triptans" used to treat migraine headaches (such as rizatriptan, sumatriptan, zolmitriptan), valbenazine.The risk of serotonin syndrome/toxicity increases if you are also taking other drugs that increase serotonin. Examples include street drugs such as MDMA/"ecstasy," St. John's wort, tramadol, certain opioid medications (such as fentanyl, meperidine, methadone, tapentadol), certain antidepressants (including maprotiline, mirtazapine, SSRIs such as fluoxetine/paroxetine, SNRIs such as duloxetine/venlafaxine, tricyclics such as amitriptyline/doxepin), among others. The risk of serotonin syndrome/toxicity may be more likely when you start or increase the dose of these drugs.Some products can interact with rasagiline if you take them together, or even if you take them weeks before or after taking rasagiline. Tell your doctor or pharmacist if you take anything in the list of products that may interact with this drug, or any of the products that increase serotonin, within 2 weeks before or after taking rasagiline. Also tell them if you have taken fluoxetine within 5 weeks before starting rasagiline. Ask your doctor how much time to wait between starting or stopping any of these drugs and starting rasagiline.Taking other MAO inhibitors with this medication may cause a serious (possibly fatal) drug interaction. Do not take any other MAO inhibitors (isocarboxazid, linezolid, metaxalone, methylene blue, moclobemide, phenelzine, procarbazine, safinamide, selegiline, tranylcypromine) during treatment with this medication. Most MAO inhibitors should also not be taken for two weeks before and after treatment with this medication. Ask your doctor when to start or stop taking this medication.Before using rasagiline, report the use of drugs that may increase the risk of extremely high blood pressure (hypertensive crisis) when combined with rasagiline, including herbal products (such as ephedra/ma Huang), allergy and cough-and-cold products (including dextromethorphan, decongestants such as phenylephrine/pseudoephedrine), and stimulants (such as amphetamines, ephedrine, epinephrine, phenylalanine). Rasagiline should not be used with any of these medications. Talk to your doctor or pharmacist for more details.Tell your doctor or pharmacist if you are taking other products that cause drowsiness including alcohol, marijuana (cannabis), antihistamines (such as cetirizine, diphenhydramine), drugs for sleep or anxiety (such as alprazolam, diazepam, zolpidem), muscle relaxants (such as carisoprodol), and opioid pain relievers (such as codeine, hydrocodone).

            OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may not appear for up to 12 hours and may include: irritability, restlessness, dizziness, drowsiness, sweating, fast heartbeat, headache, confusion, seizures.

            NOTES: Do not share this medication with others.Lab and/or medical tests (such as blood pressure) will be done while you are taking this medication. Keep all medical and lab appointments.People with Parkinson's disease may have an increased risk for developing skin cancer (melanoma). Tell your doctor right away if you have a mole that gets bigger or looks different, or if you have any other unusual skin changes. Ask your doctor if you should have regular skin exams.

            MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

            STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

            Information last revised September 2021. Copyright(c) 2021 First Databank, Inc.

            IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.