Peringatan Keamanan

LD50 (mouse) is 730mg/kg and LD50 (rat) is 1,300mg/kg. Signs of toxicity include hypertension, drowsiness, dizziness, confusion, tremors, headache, agitation, muscle rigidity and seizures A31903. The effects of moclobemide alone in overdose are negligible, even with high volume ingestion. However, moclobemide overdose with a serotonergic agent (even in small, therapeutic doses) can cause severe serotonin toxicity. The elimination half-life is prolonged by two to four times in overdose, compared with that found in healthy volunteers given therapeutic doses A31903.

Moclobemide

DB01171

small molecule approved investigational

Deskripsi

A reversible monoamine oxidase inhibitor (MAOI) selective for isoform A (RIMA) used to treat major depressive disorder. Most meta-analyses and most studies indicate that in the acute management of depression, moclobemide is more efficacious than placebo medication and similarly efficacious as tricyclic antidepressants (TCA) or selective serotonin reuptake inhibitors (SSRIs). Due to negligible anticholinergic and antihistaminic actions, moclobemide has been better tolerated than tri- or heterocyclic antidepressants A31901.

Struktur Molekul 2D

Berat 268.739
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 1-2 hours (4 hours in cirrhotic patients); metabolites are renally excreted
Volume Distribusi 1-1.5 L/Kg [L1350]
Klirens (Clearance) Clearance of 30-78 L/h [L1350], mainly excreted in urine.

Absorpsi

Well absorbed from the gastrointestinal tract (> 95%). The presence of food reduces the rate but not the extent of absorption. Hepatic first-pass metabolism reduces bioavailability to about 56% following administration of one dose, but increases to 90% with steady-state dosing as a result of saturation of the first pass effect. Peak plasma concentrations are reached within 0.3 - 1 hours following oral administration with a terminal half-life of 1.6h L1350.

Metabolisme

Moclobemide is almost completely metabolized in the liver by Cytochrome P450 2C19 and 2D6. Moclobemide is a substrate of CYP2C19. Although it acts as an inhibitor of CYP1A2, CYP2C19, and CYP2D6 A31901.

Rute Eliminasi

Moclobemide is almost completely renally excreted L1350.

Interaksi Makanan

3 Data
  • 1. Avoid excessive or chronic alcohol consumption.
  • 2. Avoid tyramine-containing foods and supplements. Avoid excess consumption (<100mg) of tyramine. Food that contains tyramine includes yogurt, aged cheese, ripe bananas, wine, and sourdough bread.
  • 3. Take after a meal.

Interaksi Obat

1541 Data
Cilostazol The serum concentration of Cilostazol can be increased when it is combined with Moclobemide.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Moclobemide.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Moclobemide.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Moclobemide.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Moclobemide.
Magnesium sulfate The therapeutic efficacy of Moclobemide can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Moclobemide may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Moclobemide may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Moclobemide.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Moclobemide.
Orphenadrine Moclobemide may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Moclobemide 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 Moclobemide.
Pramipexole Moclobemide may increase the sedative activities of Pramipexole.
Ropinirole Moclobemide may increase the sedative activities of Ropinirole.
Rotigotine Moclobemide may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Moclobemide.
Sodium oxybate Moclobemide may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Moclobemide may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Thalidomide Moclobemide may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Moclobemide may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Dabrafenib The serum concentration of Moclobemide can be decreased when it is combined with Dabrafenib.
Desmopressin The risk or severity of hypertension can be increased when Desmopressin is combined with Moclobemide.
Icosapent The risk or severity of hypertension can be increased when Icosapent is combined with Moclobemide.
Mesalazine The risk or severity of hypertension can be increased when Mesalazine is combined with Moclobemide.
Methylergometrine The risk or severity of hypertension can be increased when Methylergometrine is combined with Moclobemide.
Nabumetone The risk or severity of hypertension can be increased when Nabumetone is combined with Moclobemide.
Ketorolac The risk or severity of hypertension can be increased when Ketorolac is combined with Moclobemide.
Tolmetin The risk or severity of hypertension can be increased when Tolmetin is combined with Moclobemide.
Fenoprofen The risk or severity of hypertension can be increased when Fenoprofen is combined with Moclobemide.
Sulindac The risk or severity of hypertension can be increased when Sulindac is combined with Moclobemide.
Sulfasalazine The risk or severity of hypertension can be increased when Sulfasalazine is combined with Moclobemide.
Carprofen The risk or severity of hypertension can be increased when Carprofen is combined with Moclobemide.
Phenmetrazine The risk or severity of hypertension can be increased when Phenmetrazine is combined with Moclobemide.
Diflunisal The risk or severity of hypertension can be increased when Diflunisal is combined with Moclobemide.
Meclofenamic acid The risk or severity of hypertension can be increased when Meclofenamic acid is combined with Moclobemide.
Oxaprozin The risk or severity of hypertension can be increased when Oxaprozin is combined with Moclobemide.
Balsalazide The risk or severity of hypertension can be increased when Balsalazide is combined with Moclobemide.
Dutasteride The risk or severity of hypertension can be increased when Dutasteride is combined with Moclobemide.
Finasteride The risk or severity of hypertension can be increased when Moclobemide is combined with Finasteride.
Ephedrine The risk or severity of hypertension can be increased when Moclobemide is combined with Ephedrine.
Magnesium salicylate The risk or severity of hypertension can be increased when Moclobemide is combined with Magnesium salicylate.
Salsalate The risk or severity of hypertension can be increased when Moclobemide is combined with Salsalate.
Choline magnesium trisalicylate The risk or severity of hypertension can be increased when Moclobemide is combined with Choline magnesium trisalicylate.
Antrafenine The risk or severity of hypertension can be increased when Moclobemide is combined with Antrafenine.
Tiaprofenic acid The risk or severity of hypertension can be increased when Moclobemide is combined with Tiaprofenic acid.
Epicaptopril The risk or severity of hypertension can be increased when Moclobemide is combined with Epicaptopril.
Taxifolin The risk or severity of hypertension can be increased when Moclobemide is combined with Taxifolin.
Oxyphenbutazone The risk or severity of hypertension can be increased when Moclobemide is combined with Oxyphenbutazone.
1-benzylimidazole The risk or severity of hypertension can be increased when Moclobemide is combined with 1-benzylimidazole.
Benoxaprofen The risk or severity of hypertension can be increased when Moclobemide is combined with Benoxaprofen.
Metamizole The risk or severity of hypertension can be increased when Moclobemide is combined with Metamizole.
Zomepirac The risk or severity of hypertension can be increased when Moclobemide is combined with Zomepirac.
Cimicoxib The risk or severity of hypertension can be increased when Moclobemide is combined with Cimicoxib.
Amibegron The risk or severity of hypertension can be increased when Moclobemide is combined with Amibegron.
Nylidrin The risk or severity of hypertension can be increased when Moclobemide is combined with Nylidrin.
Solabegron The risk or severity of hypertension can be increased when Moclobemide is combined with Solabegron.
Saralasin The risk or severity of hypertension can be increased when Moclobemide is combined with Saralasin.
Azapropazone The risk or severity of hypertension can be increased when Moclobemide is combined with Azapropazone.
Salicylamide The risk or severity of hypertension can be increased when Moclobemide is combined with Salicylamide.
Tyramine The risk or severity of hypertension can be increased when Moclobemide is combined with Tyramine.
Adrafinil The risk or severity of hypertension can be increased when Moclobemide is combined with Adrafinil.
Kebuzone The risk or severity of hypertension can be increased when Moclobemide is combined with Kebuzone.
Isoxicam The risk or severity of hypertension can be increased when Moclobemide is combined with Isoxicam.
Indoprofen The risk or severity of hypertension can be increased when Moclobemide is combined with Indoprofen.
Ibuproxam The risk or severity of hypertension can be increased when Moclobemide is combined with Ibuproxam.
Floctafenine The risk or severity of hypertension can be increased when Moclobemide is combined with Floctafenine.
Fenbufen The risk or severity of hypertension can be increased when Moclobemide is combined with Fenbufen.
Etofenamate The risk or severity of hypertension can be increased when Moclobemide is combined with Etofenamate.
Etilefrine The risk or severity of hypertension can be increased when Moclobemide is combined with Etilefrine.
Epirizole The risk or severity of hypertension can be increased when Moclobemide is combined with Epirizole.
Benzydamine The risk or severity of hypertension can be increased when Moclobemide is combined with Benzydamine.
Synephrine The risk or severity of hypertension can be increased when Moclobemide is combined with Synephrine.
Moxisylyte The risk or severity of hypertension can be increased when Moclobemide is combined with Moxisylyte.
Dexibuprofen The risk or severity of hypertension can be increased when Moclobemide is combined with Dexibuprofen.
Dexketoprofen The risk or severity of hypertension can be increased when Moclobemide is combined with Dexketoprofen.
Droxicam The risk or severity of hypertension can be increased when Moclobemide is combined with Droxicam.
Tolfenamic acid The risk or severity of hypertension can be increased when Moclobemide is combined with Tolfenamic acid.
Firocoxib The risk or severity of hypertension can be increased when Moclobemide is combined with Firocoxib.
Clonixin The risk or severity of hypertension can be increased when Moclobemide is combined with Clonixin.
Morniflumate The risk or severity of hypertension can be increased when Moclobemide is combined with Morniflumate.
Talniflumate The risk or severity of hypertension can be increased when Moclobemide is combined with Talniflumate.
Dihydroergocornine The risk or severity of hypertension can be increased when Moclobemide is combined with Dihydroergocornine.
DL-Methylephedrine The risk or severity of hypertension can be increased when Moclobemide is combined with DL-Methylephedrine.
Amitraz The risk or severity of hypertension can be increased when Moclobemide is combined with Amitraz.
Robenacoxib The risk or severity of hypertension can be increased when Moclobemide is combined with Robenacoxib.
Tepoxalin The risk or severity of hypertension can be increased when Moclobemide is combined with Tepoxalin.
Atipamezole The risk or severity of hypertension can be increased when Moclobemide is combined with Atipamezole.
Flunixin The risk or severity of hypertension can be increased when Moclobemide is combined with Flunixin.
Ractopamine The risk or severity of hypertension can be increased when Moclobemide is combined with Ractopamine.
Tulobuterol The risk or severity of hypertension can be increased when Moclobemide is combined with Tulobuterol.
Dopexamine The risk or severity of hypertension can be increased when Moclobemide is combined with Dopexamine.
Idazoxan The risk or severity of hypertension can be increased when Moclobemide is combined with Idazoxan.
Ebselen The risk or severity of hypertension can be increased when Moclobemide is combined with Ebselen.
Higenamine The risk or severity of hypertension can be increased when Moclobemide is combined with Higenamine.
Reproterol The risk or severity of hypertension can be increased when Moclobemide is combined with Reproterol.
Theodrenaline The risk or severity of hypertension can be increased when Moclobemide is combined with Theodrenaline.
Tinoridine The risk or severity of hypertension can be increased when Moclobemide is combined with Tinoridine.
Tramazoline The risk or severity of hypertension can be increased when Moclobemide is combined with Tramazoline.
Alclofenac The risk or severity of hypertension can be increased when Moclobemide is combined with Alclofenac.

Target Protein

Amine oxidase [flavin-containing] A MAOA
Monoamine oxidase MAOA
Amine oxidase [flavin-containing] B MAOB

Referensi & Sumber

Artikel (PubMed)
  • PMID: 12595913
    Bonnet U: Moclobemide: therapeutic use and clinical studies. CNS Drug Rev. 2003 Spring;9(1):97-140. doi: 10.1111/j.1527-3458.2003.tb00245.x.
  • PMID: 7781267
    Gram LF, Guentert TW, Grange S, Vistisen K, Brosen K: Moclobemide, a substrate of CYP2C19 and an inhibitor of CYP2C19, CYP2D6, and CYP1A2: a panel study. Clin Pharmacol Ther. 1995 Jun;57(6):670-7. doi: 10.1016/0009-9236(95)90230-9.
  • PMID: 12968990
    Isbister GK, Hackett LP, Dawson AH, Whyte IM, Smith AJ: Moclobemide poisoning: toxicokinetics and occurrence of serotonin toxicity. Br J Clin Pharmacol. 2003 Oct;56(4):441-50.

Contoh Produk & Brand

Produk: 21 • International brands: 1
Produk
  • Dom-moclobemide Tablets 150mg
    Tablet • 150 mg • Oral • Canada • Generic • Approved
  • Dom-moclobemide Tablets 300mg
    Tablet • 300 mg • Oral • Canada • Generic • Approved
  • Manerix
    Tablet • 150 mg • Oral • Canada • Approved
  • Manerix
    Tablet • 300 mg • Oral • Canada • Approved
  • Manerix Tab 100mg
    Tablet • 100 mg / tab • Oral • Canada • Approved
  • Moclobemide
    Tablet • 100 mg • Oral • Canada • Approved
  • Moclobemide
    Tablet • 150 mg • Oral • Canada • Approved
  • Moclobemide
    Tablet • 300 mg • Oral • Canada • Approved
Menampilkan 8 dari 21 produk.
International Brands
  • Aurorix

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