Peringatan Keamanan

Signs and symptoms of overdosage may include, alone or in combination, any of the following: 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.

Rasagiline

DB01367

small molecule approved

Deskripsi

Rasagiline is an irreversible inhibitor of monoamine oxidase and is used as a monotherapy in early Parkinson's disease or as an adjunct therapy in more advanced cases.

Struktur Molekul 2D

Berat 171.2383
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Rasagiline has a mean steady-state half life of 3 hours but there is no correlation of pharmacokinetics with its pharmacological effect because of its irreversible inhibition of MAO-B.
Volume Distribusi * 87 L
Klirens (Clearance) -

Absorpsi

Rasagiline is rapidly absorbed following oral administration. The absolute bioavailability of rasagiline is about 36%.

Metabolisme

Rasagiline undergoes almost complete biotransformation in the liver prior to excretion. In vitro experiments indicate that both routes of rasagiline metabolism are dependent on the cytochrome P450 (CYP) system, with CYP 1A2 being the major isoenzyme involved in rasagiline metabolism.

Rute Eliminasi

Rasagiline undergoes almost complete biotransformation in the liver prior to excretion. Glucuronide conjugation of rasagiline and its metabolites, with subsequent urinary excretion, is the major elimination pathway. After oral administration of 14C-labeled rasagiline, elimination occurred primarily via urine and secondarily via feces (62% of total dose in urine and 7% of total dose in feces over 7 days), with a total calculated recovery of 84% of the dose over a period of 38 days. Less than 1% of rasagiline was excreted as unchanged drug in urine.

Interaksi Makanan

3 Data
  • 1. Avoid St. John's Wort. Co-administration of rasagiline with this herb is contraindicated.
  • 2. Avoid tyramine-containing foods and supplements. Avoid food containing high amounts of tyramine (>150mg) as these may increase the risk of hypertensive reaction. Tyramine-containing foods include cheese, red wine, fava beans, pickled food, cured food, and alcoholic beverages.
  • 3. Take with or without food.

Interaksi Obat

1903 Data
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Rasagiline is combined with Levodopa.
Risperidone Rasagiline may increase the hypotensive activities of Risperidone.
Deferasirox The serum concentration of Rasagiline can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Rasagiline can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Rasagiline can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Rasagiline can be decreased when it is combined with Teriflunomide.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Rasagiline.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Rasagiline.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Rasagiline.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Rasagiline.
Magnesium sulfate The therapeutic efficacy of Rasagiline can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Rasagiline may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Rasagiline may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Rasagiline.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Rasagiline.
Orphenadrine Rasagiline may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Rasagiline may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Rasagiline.
Pramipexole Rasagiline may increase the sedative activities of Pramipexole.
Ropinirole Rasagiline may increase the sedative activities of Ropinirole.
Rotigotine Rasagiline may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Rasagiline.
Sodium oxybate Rasagiline may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Rasagiline may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Thalidomide Rasagiline may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Rasagiline may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Methylergometrine The risk or severity of hypertension can be increased when Methylergometrine is combined with Rasagiline.
Nicergoline The risk or severity of hypertension can be increased when Nicergoline is combined with Rasagiline.
Phenmetrazine The risk or severity of hypertension can be increased when Phenmetrazine is combined with Rasagiline.
Dutasteride The risk or severity of hypertension can be increased when Dutasteride is combined with Rasagiline.
Finasteride The risk or severity of hypertension can be increased when Finasteride is combined with Rasagiline.
Ephedrine The risk or severity of hypertension can be increased when Ephedrine is combined with Rasagiline.
Epicaptopril The risk or severity of hypertension can be increased when Rasagiline is combined with Epicaptopril.
Taxifolin The risk or severity of hypertension can be increased when Rasagiline is combined with Taxifolin.
1-benzylimidazole The risk or severity of hypertension can be increased when Rasagiline is combined with 1-benzylimidazole.
Dronedarone The risk or severity of hypertension can be increased when Rasagiline is combined with Dronedarone.
Amibegron The risk or severity of hypertension can be increased when Rasagiline is combined with Amibegron.
Nylidrin The risk or severity of hypertension can be increased when Rasagiline is combined with Nylidrin.
Solabegron The risk or severity of hypertension can be increased when Rasagiline is combined with Solabegron.
Saralasin The risk or severity of hypertension can be increased when Rasagiline is combined with Saralasin.
Tyramine The risk or severity of hypertension can be increased when Rasagiline is combined with Tyramine.
Adrafinil The risk or severity of hypertension can be increased when Rasagiline is combined with Adrafinil.
Etilefrine The risk or severity of hypertension can be increased when Rasagiline is combined with Etilefrine.
Synephrine The risk or severity of hypertension can be increased when Rasagiline is combined with Synephrine.
Dihydroergocornine The risk or severity of hypertension can be increased when Rasagiline is combined with Dihydroergocornine.
Amitraz The risk or severity of hypertension can be increased when Rasagiline is combined with Amitraz.
Atipamezole The risk or severity of hypertension can be increased when Rasagiline is combined with Atipamezole.
Ractopamine The risk or severity of hypertension can be increased when Rasagiline is combined with Ractopamine.
Anisodamine The risk or severity of hypertension can be increased when Rasagiline is combined with Anisodamine.
Tulobuterol The risk or severity of hypertension can be increased when Rasagiline is combined with Tulobuterol.
Dopexamine The risk or severity of hypertension can be increased when Rasagiline is combined with Dopexamine.
Siponimod The risk or severity of hypertension can be increased when Rasagiline is combined with Siponimod.
Idazoxan The risk or severity of hypertension can be increased when Rasagiline is combined with Idazoxan.
Ebselen The risk or severity of hypertension can be increased when Rasagiline is combined with Ebselen.
Higenamine The risk or severity of hypertension can be increased when Rasagiline is combined with Higenamine.
Reproterol The risk or severity of hypertension can be increased when Rasagiline is combined with Reproterol.
Tramazoline The risk or severity of hypertension can be increased when Rasagiline is combined with Tramazoline.
Octopamine The risk or severity of hypertension can be increased when Rasagiline is combined with Octopamine.
Fenozolone The risk or severity of hypertension can be increased when Rasagiline is combined with Fenozolone.
Dihydroergocristine The risk or severity of hypertension can be increased when Rasagiline is combined with Dihydroergocristine.
Norfenefrine The risk or severity of hypertension can be increased when Rasagiline is combined with Norfenefrine.
Dihydroergocryptine The risk or severity of hypertension can be increased when Rasagiline is combined with Dihydroergocryptine.
Oxyfedrine The risk or severity of hypertension can be increased when Rasagiline is combined with Oxyfedrine.
Terguride The risk or severity of hypertension can be increased when Rasagiline is combined with Terguride.
Xenon The risk or severity of adverse effects can be increased when Xenon is combined with Rasagiline.
Rimiterol The risk or severity of hypertension can be increased when Rasagiline is combined with Rimiterol.
Tretoquinol The risk or severity of hypertension can be increased when Rasagiline is combined with Tretoquinol.
Prenalterol The risk or severity of hypertension can be increased when Rasagiline is combined with Prenalterol.
Xamoterol The risk or severity of hypertension can be increased when Rasagiline is combined with Xamoterol.
Mefenorex The risk or severity of hypertension can be increased when Rasagiline is combined with Mefenorex.
Deoxyepinephrine The risk or severity of hypertension can be increased when Rasagiline is combined with Deoxyepinephrine.
Quinoline Yellow WS The risk or severity of hypertension can be increased when Rasagiline is combined with Quinoline Yellow WS.
Selpercatinib The risk or severity of hypertension can be increased when Rasagiline is combined with Selpercatinib.
Naxitamab The risk or severity of hypertension can be increased when Rasagiline is combined with Naxitamab.
Apraclonidine Rasagiline may increase the alpha-adrenergic activities of Apraclonidine.
Atomoxetine The risk or severity of adverse effects can be increased when Rasagiline is combined with Atomoxetine.
Betahistine The metabolism of Betahistine can be decreased when combined with Rasagiline.
Bezafibrate Rasagiline may increase the hepatotoxic activities of Bezafibrate.
Buprenorphine Rasagiline may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Bupropion The risk or severity of adverse effects can be increased when Rasagiline is combined with Bupropion.
Buspirone The risk or severity of hypertension can be increased when Rasagiline is combined with Buspirone.
Carbamazepine The risk or severity of adverse effects can be increased when Carbamazepine is combined with Rasagiline.
Cyclobenzaprine Cyclobenzaprine may increase the serotonergic activities of Rasagiline.
Cyproheptadine Rasagiline may increase the anticholinergic activities of Cyproheptadine.
Dextromethorphan The risk or severity of serotonin syndrome can be increased when Rasagiline is combined with Dextromethorphan.
Diethylpropion The risk or severity of adverse effects can be increased when Rasagiline is combined with Diethylpropion.
Domperidone The risk or severity of QTc prolongation, torsade de pointes, and cardiotoxicity can be increased when Rasagiline is combined with Domperidone.
Hydrocodone Rasagiline may increase the serotonergic and central nervous system depressant (CNS depressant) activities of Hydrocodone.
Hydromorphone Rasagiline may increase the serotonergic activities of Hydromorphone.
Isometheptene Rasagiline may increase the sympathomimetic activities of Isometheptene.
Levonordefrin Rasagiline may increase the hypertensive activities of Levonordefrin.
Lithium hydroxide The risk or severity of serotonin syndrome can be increased when Rasagiline is combined with Lithium hydroxide.
Lithium citrate The risk or severity of serotonin syndrome can be increased when Rasagiline is combined with Lithium citrate.
Maprotiline The risk or severity of adverse effects can be increased when Rasagiline is combined with Maprotiline.
Mianserin The risk or severity of adverse effects can be increased when Rasagiline is combined with Mianserin.
Esmirtazapine The risk or severity of adverse effects can be increased when Rasagiline is combined with Esmirtazapine.
Setiptiline The risk or severity of adverse effects can be increased when Rasagiline is combined with Setiptiline.
Aptazapine The risk or severity of adverse effects can be increased when Rasagiline is combined with Aptazapine.
Mequitazine Rasagiline may increase the anticholinergic activities of Mequitazine.
Methadone The risk or severity of serotonin syndrome can be increased when Rasagiline is combined with Methadone.

Target Protein

Amine oxidase [flavin-containing] B MAOB
Apoptosis regulator Bcl-2 BCL2

Referensi & Sumber

Synthesis reference: Jeffrey Sterling, David Lerner, Harel Rosen, Leonid Bronov, Dalia Medini-Green, Berta Iosefzon, Tirtsah Berger-Peskin, Ramy Lidor-Hadas, Eliezer Bahar, "Rasagiline formulations and processes for their preparation." U.S. Patent US07598420, issued October 06, 2009.
Artikel (PubMed)
  • PMID: 20600573
    Weinreb O, Amit T, Bar-Am O, Youdim MB: Rasagiline: a novel anti-Parkinsonian monoamine oxidase-B inhibitor with neuroprotective activity. Prog Neurobiol. 2010 Nov;92(3):330-44. doi: 10.1016/j.pneurobio.2010.06.008. Epub 2010 Jun 19.
  • PMID: 20517484
    Leegwater-Kim J, Bortan E: The role of rasagiline in the treatment of Parkinson's disease. Clin Interv Aging. 2010 May 25;5:149-56.
  • PMID: 18035186
    Chen JJ, Swope DM, Dashtipour K: Comprehensive review of rasagiline, a second-generation monoamine oxidase inhibitor, for the treatment of Parkinson's disease. Clin Ther. 2007 Sep;29(9):1825-49.

Contoh Produk & Brand

Produk: 80 • International brands: 0
Produk
  • Ag-rasagiline
    Tablet • 0.5 mg • Oral • Canada • Generic • Approved
  • Ag-rasagiline
    Tablet • 1 mg • Oral • Canada • Generic • Approved
  • Apo-rasagiline
    Tablet • 0.5 mg • Oral • Canada • Generic • Approved
  • Apo-rasagiline
    Tablet • 1 mg • Oral • Canada • Generic • Approved
  • Asn-rasagiline
    Tablet • 0.5 mg • Oral • Canada • Approved
  • Asn-rasagiline
    Tablet • 1 mg • Oral • Canada • Approved
  • Azilect
    Tablet • 1 mg/1 • Oral • US • Approved
  • Azilect
    Tablet • 1 mg/1 • Oral • US • Approved
Menampilkan 8 dari 80 produk.

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