Peringatan Keamanan

The rat oral LD50 of metoclopramide is 750 mg/kg.L8465

Some symptoms of an overdose with metoclopramide include drowsiness, disorientation, and extrapyramidal reactions. Drugs that manage Parkinson's disease or anticholinergic drugs or antihistamines with anticholinergic properties A185174 should be employed to treat extrapyramidal symptoms. Normally, these symptoms subside within 24 hours.L8414 Unintentional overdose in infants receiving the oral solution of metoclopramide resulted in seizures, extrapyramidal symptoms, in addition to a lethargic state.

In addition, methemoglobinemia has been found to occur in premature and full-term neonates after a metoclopramide overdose. Intravenous methylene blue may treat metoclopramide-associated methemoglobinemia. It is important to note that methylene blue administration may lead to hemolytic anemia in patients who suffer from G6PD deficiency, which can result in fatality. Dialysis has not been shown to be effective in sufficiently eliminating metoclopramide in an overdose situation due to low plasma distribution of this drug.L8414

Metoclopramide

DB01233

small molecule approved investigational

Deskripsi

Diabetic gastroparesis is a condition that causes frequent nausea and vomiting, which has a negative impact on quality of life and poses a significant burden on the healthcare system.A184934 Metoclopramide is a dopamine antagonist used to treat nausea and vomiting that may be associated with diabetic gastroparesis in addition to gastroesophageal reflux disease (GERD). It can also be used to prevent nausea or vomiting associated with chemotherapy or certain surgical or diagnostic procedures.L8417

One unique property of this drug is that it does not increase gastric acid secretion. It is available in the oral tablet form or in solution, and can also be administered through the intravenous route.T683 Metoclopramide was initially approved by the FDA in 1980.A184922

Struktur Molekul 2D

Berat 299.796
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean elimination half-life of metoclopramide in people with healthy renal function ranges from 5 to 6 hours but is prolonged in patients with renal impairment. Downward dose adjustment should be considered.[A184886,A185153,L8414]
Volume Distribusi The volume of distribution of metoclopramide is approximately 3.5 L/kg. This implies a high level of tissue distribution. Metoclopramide crosses the placental barrier and can cause extrapyramidal symptoms in the fetus.[A185153,L8414]
Klirens (Clearance) The renal clearance of metoclopramide is 0.16 L/h/kg with a total clearance of 0.7 L/h/kg. Clinical studies showed that the clearance of metoclopramide may be reduced by up to 50% in patients with renal impairment.[A184886] After high intravenous doses, total metoclopramide clearance ranged from 0.31 to 0.69 L/kg/h.[A185159]

Absorpsi

Metoclopramide is rapidly absorbed in the gastrointestinal tract with an absorption rate of about 84%.A184886 The bioavailability of the oral preparation is reported to be about 40.7%, but can range from 30-100%.A184880,A184949 Nasal metoclopramide is 47% bioavailable.L14381 A 15mg dose reaches a Cmax of 41.0 ng/mL, with a Tmax of 1.25 h, and an AUC of 367 ng\*h/mL.L14381

Metabolisme

Metoclopramide undergoes first-pass metabolism and its metabolism varies according to the individual. This drug is metabolized by cytochrome P450 enzymes in the liver.A184880 CYP2D6 and CYP3A4 both contribute to its metabolism, with CYP2D6 being more heavily involved. CYP1A2 is also a minor contributing enzyme.A181352 The process of N-4 sulphate conjugation is a primary metabolic pathway of metoclopramide.A184886

Rute Eliminasi

About 85% of an orally administered dose was measured in the urine within 72 hours during a pharmacokinetic study. An average of 18% to 22% of 10-20 mg dose was recovered as free drug within 3 days of administration.L8414

Farmakogenomik

7 Varian
KCNH2 (rs1805123)

The presence of this polymorphism in KCNH2 may be associated with increased clinical efficacy with metoclopramide.

ADRA1D (rs2236554)

The presence of this polymorphism in ADRA1D may be associated with increased clinical efficacy with metoclopramide.

CYP2D6 (rs3892097)

Patients with this genotype have reduced metabolism of metoclopramide.

ABCB1 (rs1045642)

Patients with this polymorphism in ABCB1 may have a reduced response to clomipramine.

CYP2D6 (rs1080985)

Patients with this genotype have reduced metabolism of metoclopramide and may be at a higher risk of experiencing adverse events.

CYP2D6 (rs16947)

Patients with this genotype have reduced metabolism of metoclopramide and may be at a higher risk of experiencing adverse events.

KCNH2 (rs3815459)

The presence of this polymorphism in KCNH2 is associated with higher incidences of adverse events from metoclopramide treatment.

Interaksi Makanan

2 Data
  • 1. Avoid alcohol.
  • 2. Take before a meal. Co-administration with food decreases bioavailability - take 30 minutes before meals.

Interaksi Obat

2023 Data
Cyclosporine Metoclopramide can cause an increase in the absorption of Cyclosporine resulting in an increased serum concentration and potentially a worsening of adverse effects.
Deferasirox The serum concentration of Metoclopramide can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Metoclopramide can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Metoclopramide can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Metoclopramide can be decreased when it is combined with Teriflunomide.
Lorpiprazole The risk or severity of serotonin syndrome and neuroleptic malignant syndrome can be increased when Lorpiprazole is combined with Metoclopramide.
Reserpine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Reserpine.
Ziprasidone The risk or severity of adverse effects can be increased when Metoclopramide is combined with Ziprasidone.
Olanzapine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Olanzapine.
Clozapine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Clozapine.
Thiethylperazine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Thiethylperazine.
Sulpiride The risk or severity of adverse effects can be increased when Metoclopramide is combined with Sulpiride.
Loxapine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Loxapine.
Remoxipride The risk or severity of adverse effects can be increased when Metoclopramide is combined with Remoxipride.
Promazine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Promazine.
Prochlorperazine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Prochlorperazine.
Chlorpromazine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Chlorpromazine.
Haloperidol The risk or severity of adverse effects can be increased when Metoclopramide is combined with Haloperidol.
Triflupromazine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Triflupromazine.
Amoxapine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Amoxapine.
Fluphenazine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Fluphenazine.
Thioridazine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Thioridazine.
Moricizine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Moricizine.
Risperidone The risk or severity of adverse effects can be increased when Metoclopramide is combined with Risperidone.
Trifluoperazine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Trifluoperazine.
Perphenazine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Perphenazine.
Mesoridazine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Mesoridazine.
Acetophenazine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Acetophenazine.
Pimozide The risk or severity of adverse effects can be increased when Metoclopramide is combined with Pimozide.
Quetiapine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Quetiapine.
Aripiprazole The risk or severity of adverse effects can be increased when Metoclopramide is combined with Aripiprazole.
Chlorprothixene The risk or severity of adverse effects can be increased when Metoclopramide is combined with Chlorprothixene.
Alimemazine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Alimemazine.
Paliperidone The risk or severity of adverse effects can be increased when Metoclopramide is combined with Paliperidone.
Lithium cation The risk or severity of adverse effects can be increased when Metoclopramide is combined with Lithium cation.
Methotrimeprazine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Methotrimeprazine.
Periciazine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Periciazine.
Acepromazine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Acepromazine.
Aceprometazine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Aceprometazine.
Molindone The risk or severity of adverse effects can be increased when Metoclopramide is combined with Molindone.
Pipotiazine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Pipotiazine.
Thioproperazine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Thioproperazine.
Thiothixene The risk or severity of adverse effects can be increased when Metoclopramide is combined with Thiothixene.
Zuclopenthixol The risk or severity of adverse effects can be increased when Metoclopramide is combined with Zuclopenthixol.
Fluspirilene The risk or severity of adverse effects can be increased when Metoclopramide is combined with Fluspirilene.
Osanetant The risk or severity of adverse effects can be increased when Metoclopramide is combined with Osanetant.
Bifeprunox The risk or severity of adverse effects can be increased when Metoclopramide is combined with Bifeprunox.
Iloperidone The risk or severity of adverse effects can be increased when Metoclopramide is combined with Iloperidone.
BL-1020 The risk or severity of adverse effects can be increased when Metoclopramide is combined with BL-1020.
Cariprazine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Cariprazine.
Lumateperone The risk or severity of adverse effects can be increased when Metoclopramide is combined with Lumateperone.
Sertindole The risk or severity of adverse effects can be increased when Metoclopramide is combined with Sertindole.
Asenapine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Asenapine.
Amisulpride The risk or severity of adverse effects can be increased when Metoclopramide is combined with Amisulpride.
Lurasidone The risk or severity of adverse effects can be increased when Metoclopramide is combined with Lurasidone.
Perospirone The risk or severity of adverse effects can be increased when Metoclopramide is combined with Perospirone.
Amperozide The risk or severity of adverse effects can be increased when Metoclopramide is combined with Amperozide.
Cyamemazine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Cyamemazine.
Brexpiprazole The risk or severity of adverse effects can be increased when Metoclopramide is combined with Brexpiprazole.
Blonanserin The risk or severity of adverse effects can be increased when Metoclopramide is combined with Blonanserin.
Melperone The risk or severity of adverse effects can be increased when Metoclopramide is combined with Melperone.
Zotepine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Zotepine.
Brilaroxazine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Brilaroxazine.
Pipamperone The risk or severity of adverse effects can be increased when Metoclopramide is combined with Pipamperone.
Azaperone The risk or severity of adverse effects can be increased when Metoclopramide is combined with Azaperone.
Propiopromazine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Propiopromazine.
Tetrahydropalmatine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Tetrahydropalmatine.
Ecopipam The risk or severity of adverse effects can be increased when Metoclopramide is combined with Ecopipam.
Bromperidol The risk or severity of adverse effects can be increased when Metoclopramide is combined with Bromperidol.
Raclopride The risk or severity of adverse effects can be increased when Metoclopramide is combined with Raclopride.
Ritanserin The risk or severity of adverse effects can be increased when Metoclopramide is combined with Ritanserin.
Perazine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Perazine.
Benperidol The risk or severity of adverse effects can be increased when Metoclopramide is combined with Benperidol.
Prothipendyl The risk or severity of adverse effects can be increased when Metoclopramide is combined with Prothipendyl.
Tiapride The risk or severity of adverse effects can be increased when Metoclopramide is combined with Tiapride.
Butaperazine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Butaperazine.
Clothiapine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Clothiapine.
Sultopride The risk or severity of adverse effects can be increased when Metoclopramide is combined with Sultopride.
Chlorproethazine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Chlorproethazine.
Oxypertine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Oxypertine.
Thiazinam The risk or severity of adverse effects can be increased when Metoclopramide is combined with Thiazinam.
Veralipride The risk or severity of adverse effects can be increased when Metoclopramide is combined with Veralipride.
Trifluperidol The risk or severity of adverse effects can be increased when Metoclopramide is combined with Trifluperidol.
Moperone The risk or severity of adverse effects can be increased when Metoclopramide is combined with Moperone.
Thiopropazate The risk or severity of adverse effects can be increased when Metoclopramide is combined with Thiopropazate.
Fluanisone The risk or severity of adverse effects can be increased when Metoclopramide is combined with Fluanisone.
Mosapramine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Mosapramine.
Dixyrazine The risk or severity of adverse effects can be increased when Metoclopramide is combined with Dixyrazine.
Penfluridol The risk or severity of adverse effects can be increased when Metoclopramide is combined with Penfluridol.
Clopenthixol The risk or severity of adverse effects can be increased when Metoclopramide is combined with Clopenthixol.
Aripiprazole lauroxil The risk or severity of adverse effects can be increased when Metoclopramide is combined with Aripiprazole lauroxil.
Perphenazine enanthate The risk or severity of adverse effects can be increased when Metoclopramide is combined with Perphenazine enanthate.
Levosulpiride The risk or severity of adverse effects can be increased when Metoclopramide is combined with Levosulpiride.
Prilocaine The risk or severity of methemoglobinemia can be increased when Metoclopramide is combined with Prilocaine.
Carbidopa The therapeutic efficacy of Carbidopa can be decreased when used in combination with Metoclopramide.
Metixene The therapeutic efficacy of Metixene can be decreased when used in combination with Metoclopramide.
Trihexyphenidyl The therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Metoclopramide.
Procyclidine The therapeutic efficacy of Procyclidine can be decreased when used in combination with Metoclopramide.
Profenamine The therapeutic efficacy of Profenamine can be decreased when used in combination with Metoclopramide.
Biperiden The therapeutic efficacy of Biperiden can be decreased when used in combination with Metoclopramide.

Target Protein

5-hydroxytryptamine receptor 4 HTR4
5-hydroxytryptamine receptor 3A HTR3A
Muscarinic acetylcholine receptor M1 CHRM1
D(2) dopamine receptor DRD2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 7479521
    Tonini M, Candura SM, Messori E, Rizzi CA: Therapeutic potential of drugs with mixed 5-HT4 agonist/5-HT3 antagonist action in the control of emesis. Pharmacol Res. 1995 May;31(5):257-60.
  • PMID: 21278804
    Lee A, Kuo B: Metoclopramide in the treatment of diabetic gastroparesis. Expert Rev Endocrinol Metab. 2010;5(5):653-662.
  • PMID: 25672546
    van der Meer YG, Venhuizen WA, Heyland DK, van Zanten AR: Should we stop prescribing metoclopramide as a prokinetic drug in critically ill patients? Crit Care. 2014 Sep 23;18(5):502. doi: 10.1186/s13054-014-0502-4.
  • PMID: 6360466
    Bateman DN: Clinical pharmacokinetics of metoclopramide. Clin Pharmacokinet. 1983 Nov-Dec;8(6):523-9. doi: 10.2165/00003088-198308060-00003.
  • PMID: 30310300
    Avalos DJ, Sarosiek I, Loganathan P, McCallum RW: Diabetic gastroparesis: current challenges and future prospects. Clin Exp Gastroenterol. 2018 Sep 25;11:347-363. doi: 10.2147/CEG.S131650. eCollection 2018.
  • PMID: 27775961
    Lacy BE, Crowell MD, Mathis C, Bauer D, Heinberg LJ: Gastroparesis: Quality of Life and Health Care Utilization. J Clin Gastroenterol. 2018 Jan;52(1):20-24. doi: 10.1097/MCG.0000000000000728.
  • PMID: 19958151
    Mahajan HS, Gattani S: In situ gels of Metoclopramide Hydrochloride for intranasal delivery: in vitro evaluation and in vivo pharmacokinetic study in rabbits. Drug Deliv. 2010 Jan;17(1):19-27. doi: 10.3109/10717540903447194. Epub 2009 Dec 3.
  • PMID: 26425557
    Feyer P, Jahn F, Jordan K: Prophylactic Management of Radiation-Induced Nausea and Vomiting. Biomed Res Int. 2015;2015:893013. doi: 10.1155/2015/893013. Epub 2015 Sep 3.
Menampilkan 8 dari 16 artikel.
Textbook
  • Sasank Isola; Ninos Adams (2019). Metoclopramide, NIH StatPearls. Stat Pearls Publishing.

Contoh Produk & Brand

Produk: 239 • International brands: 13
Produk
  • Apo-metoclop Tab 10mg
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Apo-metoclop Tab 5mg
    Tablet • 5 mg • Oral • Canada • Generic • Approved
  • Gimoti
    Spray • 15 mg/0.07mL • Nasal • US • Approved
  • Mar-metoclopramide
    Tablet • 5 mg • Oral • Canada • Generic • Approved
  • Mar-metoclopramide
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Maxeran 5mg Tab
    Tablet • 5 mg / tab • Oral • Canada • Approved
  • Maxeran Liq
    Liquid • 1 mg / 1 mL • Oral • Canada • Approved
  • Maxeran-10 (10mg Tablet)
    Tablet • 10 mg / tab • Oral • Canada • Approved
Menampilkan 8 dari 239 produk.
International Brands
  • Cerucal
  • Degan
  • Elieten
  • Maxeran
  • Maxolon
  • METOZOLV
  • Plasil1
  • Plazilin
  • Pramin
  • Primperan

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul