Peringatan Keamanan

Oral administration of metoprolol to rats presents an LD50 in the range of 3090 to 4670 mg/kg. Cases of overdose have reported bradycardia, hypotension, bronchospasm, and cardiac failure. In the case of an overdose, gastric lavage is recommended followed by specific treatment according to symptoms.FDA label

Metoprolol is not reported to be carcinogenic nor mutagenic nor to impair fertility. The only event registered is the increase of macrophages in pulmonary alveoli and slight biliary hyperplasia. When metoprolol was given for long periods of time on the highest dose, there was evidence of small benign lung tumors.FDA label

Metoprolol

DB00264

small molecule approved investigational

Deskripsi

Metoprolol is a selective beta-1 blocker commonly employed as the succinate and tartrate derivatives depending if the formulation is designed to be of immediate release or extended release.A175159, L5530 The possibility of the generation of these formulations comes from the lower systemic bioavailability of the succinate derivative.T274 To this date, it is one of the preferred beta-blockers in general clinical guidelines and it is widely prescribed in the Netherlands, New Zealand, and the US.A175162 Metoprolol was developed since 1969 by US Pharmaceutical Holdings I and FDA approved in 1978.L5527

Struktur Molekul 2D

Berat 267.3639
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The immediate release formulations of metoprolol present a half-life of about 3-7 hours.[A175141]
Volume Distribusi The reported volume of distribution of metoprolol is 4.2 L/kg.[T274] Due to the characteristics of metoprolol, this molecule is able to cross the blood-brain barrier and even 78% of the administered drug can be found in cerebrospinal fluid.[L5536]
Klirens (Clearance) The reported clearance rate on patients with normal kidney function is 0.8 L/min. In cirrhotic patients, the clearance rate changes to 0.61 L/min.[A175171]

Absorpsi

When metoprolol is administered orally, it is almost completely absorbed in the gastrointestinal tract.A175141 The maximum serum concentration is achieved 20 min after intravenous administration and 1-2 hours after oral administration. The bioavailability of metoprolol is of 100% when administered intravenously and when administered orally it presents about 50% for the tartrate derivative and 40% for the succinate derivative.T274 The absorption of metoprolol in the form of the tartrate derivative is increased by the concomitant administration of food.T274

Metabolisme

Metoprolol goes through significant first-pass hepatic metabolism which covers around 50% of the administered dose.A175141 The metabolism of metoprolol is mainly driven by the activity of CYP2D6A175162 and to a lesser extent due to the activity of CYP3A4. The metabolism of metoprolol is mainly represented by reactions of hydroxylation and O-demethylation.L5530

Rute Eliminasi

Metoprolol is mainly excreted via the kidneys. From the eliminated dose, less than 5% is recovered unchanged.A175141

Farmakogenomik

3 Varian
ADRB1 (rs1801252)

Patients with this genotype have a greater reduction in blood pressure with metoprolol.

CYP2D6 (rs3892097)

Patients with this genotype have reduced metabolism of metoprolol.

ADRB1 (rs1801253)

Patients with this genotype have a greater reduction in blood pressure with metoprolol.

Interaksi Makanan

3 Data
  • 1. Avoid alcohol.
  • 2. Avoid natural licorice.
  • 3. Take with food.

Interaksi Obat

1709 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Metoprolol is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Metoprolol is combined with Levodopa.
Risperidone Metoprolol may increase the hypotensive activities of Risperidone.
Ceritinib Metoprolol may increase the bradycardic activities of Ceritinib.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Metoprolol.
Alfuzosin Alfuzosin may increase the hypotensive activities of Metoprolol.
Amifostine Metoprolol may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Metoprolol.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Metoprolol.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Metoprolol.
Obinutuzumab Metoprolol may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Metoprolol.
Rituximab Metoprolol may increase the hypotensive activities of Rituximab.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Metoprolol.
Doxapram Doxapram may decrease the antihypertensive activities of Metoprolol.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Metoprolol.
Naratriptan Naratriptan may decrease the antihypertensive activities of Metoprolol.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Metoprolol.
Dutasteride Dutasteride may decrease the antihypertensive activities of Metoprolol.
Epicaptopril Epicaptopril may decrease the antihypertensive activities of Metoprolol.
1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Metoprolol.
Amineptine Amineptine may decrease the antihypertensive activities of Metoprolol.
Naluzotan Naluzotan may decrease the antihypertensive activities of Metoprolol.
Nitrous oxide Nitrous oxide may decrease the antihypertensive activities of Metoprolol.
Cinitapride Cinitapride may decrease the antihypertensive activities of Metoprolol.
Tyramine Tyramine may decrease the antihypertensive activities of Metoprolol.
Ifenprodil Ifenprodil may decrease the antihypertensive activities of Metoprolol.
Butriptyline Butriptyline may decrease the antihypertensive activities of Metoprolol.
Oxaprotiline Oxaprotiline may decrease the antihypertensive activities of Metoprolol.
Atipamezole Atipamezole may decrease the antihypertensive activities of Metoprolol.
Tetrahydrocannabivarin Tetrahydrocannabivarin may decrease the antihypertensive activities of Metoprolol.
Piclozotan Piclozotan may decrease the antihypertensive activities of Metoprolol.
Idazoxan Idazoxan may decrease the antihypertensive activities of Metoprolol.
Tramazoline Tramazoline may decrease the antihypertensive activities of Metoprolol.
Amitriptylinoxide Amitriptylinoxide may decrease the antihypertensive activities of Metoprolol.
Dibenzepin Dibenzepin may decrease the antihypertensive activities of Metoprolol.
Quinupramine Quinupramine may decrease the antihypertensive activities of Metoprolol.
Trichloroethylene Trichloroethylene may decrease the antihypertensive activities of Metoprolol.
Fenozolone Fenozolone may decrease the antihypertensive activities of Metoprolol.
Melitracen Melitracen may decrease the antihypertensive activities of Metoprolol.
Lofepramine Lofepramine may decrease the antihypertensive activities of Metoprolol.
Xenon Xenon may decrease the antihypertensive activities of Metoprolol.
Iprindole Iprindole may decrease the antihypertensive activities of Metoprolol.
Buflomedil Buflomedil may decrease the antihypertensive activities of Metoprolol.
Imipramine oxide Imipramine oxide may decrease the antihypertensive activities of Metoprolol.
Mefenorex Mefenorex may decrease the antihypertensive activities of Metoprolol.
Quinoline Yellow WS Quinoline Yellow WS may decrease the antihypertensive activities of Metoprolol.
Isoflurane Isoflurane may decrease the antihypertensive activities of Metoprolol.
Remifentanil Remifentanil may decrease the antihypertensive activities of Metoprolol.
Desflurane Desflurane may decrease the antihypertensive activities of Metoprolol.
Sufentanil Sufentanil may decrease the antihypertensive activities of Metoprolol.
Halothane Halothane may decrease the antihypertensive activities of Metoprolol.
Finasteride Finasteride may decrease the antihypertensive activities of Metoprolol.
Sevoflurane Sevoflurane may decrease the antihypertensive activities of Metoprolol.
Flibanserin Flibanserin may decrease the antihypertensive activities of Metoprolol.
Diethyl ether Diethyl ether may decrease the antihypertensive activities of Metoprolol.
Alfentanil Alfentanil may decrease the antihypertensive activities of Metoprolol.
Fentanyl Fentanyl may decrease the antihypertensive activities of Metoprolol.
Lurasidone Lurasidone may decrease the antihypertensive activities of Metoprolol.
Dimetacrine Dimetacrine may decrease the antihypertensive activities of Metoprolol.
Selpercatinib Selpercatinib may decrease the antihypertensive activities of Metoprolol.
Naxitamab Naxitamab may decrease the antihypertensive activities of Metoprolol.
Propofol Propofol may decrease the antihypertensive activities of Metoprolol.
Cannabidiol The metabolism of Metoprolol can be decreased when combined with Cannabidiol.
Tianeptine Tianeptine may decrease the antihypertensive activities of Metoprolol.
Siponimod Siponimod may decrease the antihypertensive activities of Metoprolol.
Protriptyline Protriptyline may decrease the antihypertensive activities of Metoprolol.
Opipramol Opipramol may decrease the antihypertensive activities of Metoprolol.
Amiodarone The therapeutic efficacy of Metoprolol can be increased when used in combination with Amiodarone.
Bupivacaine The serum concentration of Bupivacaine can be increased when it is combined with Metoprolol.
Dipyridamole Dipyridamole may increase the bradycardic activities of Metoprolol.
Disopyramide Disopyramide may increase the bradycardic activities of Metoprolol.
Dronedarone Dronedarone may increase the bradycardic activities of Metoprolol.
Fingolimod Metoprolol may increase the bradycardic activities of Fingolimod.
Floctafenine The risk or severity of adverse effects can be increased when Metoprolol is combined with Floctafenine.
Mepivacaine The serum concentration of Mepivacaine can be increased when it is combined with Metoprolol.
Methacholine Metoprolol may increase the bronchoconstrictory activities of Methacholine.
Midodrine The therapeutic efficacy of Midodrine can be decreased when used in combination with Metoprolol.
Propafenone The risk or severity of adverse effects can be increased when Propafenone is combined with Metoprolol.
Regorafenib Regorafenib may increase the bradycardic activities of Metoprolol.
Reserpine Reserpine may increase the hypotensive activities of Metoprolol.
Deserpidine Deserpidine may increase the hypotensive activities of Metoprolol.
Guanethidine Guanethidine may increase the hypotensive activities of Metoprolol.
Rivastigmine Metoprolol may increase the bradycardic activities of Rivastigmine.
Brexpiprazole The metabolism of Brexpiprazole can be decreased when combined with Metoprolol.
Eliglustat The metabolism of Metoprolol can be decreased when combined with Eliglustat.
Porfimer sodium Metoprolol may increase the photosensitizing activities of Porfimer sodium.
Verteporfin Metoprolol may increase the photosensitizing activities of Verteporfin.
Mirabegron Mirabegron may decrease the antihypertensive activities of Metoprolol.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Metoprolol.
Nicorandil Nicorandil may increase the hypotensive activities of Metoprolol.
Molsidomine Molsidomine may increase the hypotensive activities of Metoprolol.
Insulin argine Metoprolol may increase the hypoglycemic activities of Insulin argine.
Dorzolamide Metoprolol may increase the hypotensive activities of Dorzolamide.
Bimatoprost Metoprolol may increase the hypotensive activities of Bimatoprost.
Unoprostone Metoprolol may increase the hypotensive activities of Unoprostone.
Remikiren Remikiren may increase the hypotensive activities of Metoprolol.
Guanadrel Guanadrel may increase the hypotensive activities of Metoprolol.
Minoxidil Metoprolol may increase the hypotensive activities of Minoxidil.
Candoxatril Metoprolol may increase the hypotensive activities of Candoxatril.

Target Protein

Beta-1 adrenergic receptor ADRB1
Beta-2 adrenergic receptor ADRB2
Beta adrenergic receptor ADRB1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 30422518
    Morris J, Dunham A: Metoprolol .
  • PMID: 26252585
    Silberstein SD: Preventive Migraine Treatment. Continuum (Minneap Minn). 2015 Aug;21(4 Headache):973-89. doi: 10.1212/CON.0000000000000199.
  • PMID: 30248178
    Bahar MA, Kamp J, Borgsteede SD, Hak E, Wilffert B: The impact of CYP2D6 mediated drug-drug interaction: a systematic review on a combination of metoprolol and paroxetine/fluoxetine. Br J Clin Pharmacol. 2018 Dec;84(12):2704-2715. doi: 10.1111/bcp.13741. Epub 2018 Sep 24.
  • PMID: 7333059
    Regardh CG, Jordo L, Ervik M, Lundborg P, Olsson R, Ronn O: Pharmacokinetics of metoprolol in patients with hepatic cirrhosis. Clin Pharmacokinet. 1981 Sep-Oct;6(5):375-88. doi: 10.2165/00003088-198106050-00004.
Textbook
  • ISBN: 1-57340-221-4
    Frishman W., Cheng-Lai A. and Nawarskas J. (2005). Current cardiovascular drugs (4th ed.). Current medicine LLC.
  • Jones & Bartlett (2016). 2016 Nurse's drug handbook (15th ed.). Jones and Bartlett Publishers Inc..
  • ISBN: 0-471-98598-8
    Saeb-Parsy K., Assomull R., Khan F., Saeb-Parsy K. and Kelly A. (1990). Instant Pharmacology. Willey.

Contoh Produk & Brand

Produk: 1204 • International brands: 4
Produk
  • Aa-metoprolol SR
    Tablet, extended release • 100 mg • Oral • Canada • Generic • Approved
  • Aa-metoprolol SR
    Tablet, extended release • 200 mg • Oral • Canada • Generic • Approved
  • Ag-metoprolol-L
    Tablet • 25 mg • Oral • Canada • Generic • Approved
  • Ag-metoprolol-L
    Tablet • 50 mg • Oral • Canada • Generic • Approved
  • Ag-metoprolol-L
    Tablet • 100 mg • Oral • Canada • Generic • Approved
  • Apo-metoprolol
    Tablet • 50 mg • Oral • Canada • Generic • Approved
  • Apo-metoprolol
    Tablet • 100 mg • Oral • Canada • Generic • Approved
  • Apo-metoprolol
    Tablet • 25 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 1204 produk.
International Brands
  • Corvitol — Berlin-Chemie AG / Menarini Group
  • Minax — Alphapharm Pty Limited
  • Selokeen — AstraZeneca
  • TOPROL-XL — Lanett Company, Inc

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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