Peringatan Keamanan

Patients experiencing an overdose may present with hypotension and reflex tachycardia.L10833 Treat overdose with cardiac and respiratory monitoring, frequent blood pressure measurement, elevation of extremities to treat hypotension, and possible administration of vasopressors.L10833 Hemodialysis is not expected to be useful as levamlodipine is highly protein bound.L10833

Levamlodipine

DB09237

small molecule approved investigational

Deskripsi

Levamlodipine, also known as S-amlodipine, is a pharmacologically active enantiomer of amlodipine, an antihypertensive medication.L10833 Levamlodipine belongs to the dihydropyridine group of calcium channel blockers.L10833 This medication was first marketed in Russia and India before being granted FDA approval.L1484 The names S-amlodipine and levamlodipine may be used interchangeably as both substances are the same, however.L10833 As a racemic mixture, amlodipine contains (R) and (S)-amlodipine isomers, but only (S)-amlodipine as the active moiety possesses therapeutic activity.A188940

Levamlodipine was granted FDA approval on 19 December 2019.L10833

Struktur Molekul 2D

Berat 408.88
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Levamlodipine has a half life of 30-50h.[L10833]
Volume Distribusi The volume of distribution of levamlodipine is similar to amlodipine.[A32034] The volume of distribution of amlodipine is 21L/kg.[A175327,A175336]
Klirens (Clearance) The oral clearance of S-amlodipine besylate is 6.9±1.6mL/min/kg and the oral clearance of S-amlodipine maleate is 7.3±2.1mL/min/kg.[A32034]

Absorpsi

Oral levamlodipine has a Tmax of 6-12h and a bioavailability of 64-90%.L10833 Absorption of levamlodipine is not significantly affected by food.L10833 20mg or oral s-amlodipine besylate reaches a Cmax of 6.13±1.29ng/mL with a Tmax of 8.4±3.6h and an AUC of 351±72h\*ng/mL.A32034 20mg or oral s-amlodipine maleate reaches a Cmax of 5.07±1.09ng/mL with a Tmax of 10.7±3.4h and an AUC of 330±88h\*ng/mL.A32034

Metabolisme

Levamlodipine is 90% metabolized to inactive metabolites.L10833 Incubation with liver microsomes has shown that this metabolism is primarily mediated by CYP3A4.A32032 Levamlodipine's dehydrogenation to a pyridine metabolite (M9) is the most important metabolic pathway in human liver microsomes.A32032 This derivative can be further oxidatively deaminated or O-dealkylated, but does not appear to undergo O-demethylation like racemic amlodipine.A32032

Rute Eliminasi

Levamlodipine is 60% eliminated in urine with 10% eliminated as the unmetabolized drug.L10833

Interaksi Makanan

1 Data
  • 1. Take with or without food. Co-administration with food does not affect bioavailability.

Interaksi Obat

1238 Data
Alfuzosin Alfuzosin may increase the hypotensive activities of Levamlodipine.
Amifostine Levamlodipine may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Levamlodipine.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Levamlodipine.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Levamlodipine.
Obinutuzumab Levamlodipine may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Levamlodipine.
Rituximab Levamlodipine may increase the hypotensive activities of Rituximab.
Desmopressin Desmopressin may decrease the antihypertensive activities of Levamlodipine.
Phentermine Phentermine may decrease the antihypertensive activities of Levamlodipine.
Midodrine Midodrine may decrease the antihypertensive activities of Levamlodipine.
Eletriptan Eletriptan may decrease the antihypertensive activities of Levamlodipine.
Bethanidine Bethanidine may decrease the antihypertensive activities of Levamlodipine.
Isoetharine Isoetharine may decrease the antihypertensive activities of Levamlodipine.
Methysergide Methysergide may decrease the antihypertensive activities of Levamlodipine.
Atomoxetine Atomoxetine may decrease the antihypertensive activities of Levamlodipine.
Etomidate Etomidate may decrease the antihypertensive activities of Levamlodipine.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Levamlodipine.
Protriptyline Protriptyline may decrease the antihypertensive activities of Levamlodipine.
Norepinephrine Norepinephrine may decrease the antihypertensive activities of Levamlodipine.
Phenylephrine The risk or severity of hypertension can be decreased when Levamlodipine is combined with Phenylephrine.
Phenylpropanolamine Phenylpropanolamine may decrease the antihypertensive activities of Levamlodipine.
Promazine Promazine may decrease the antihypertensive activities of Levamlodipine.
Droperidol Droperidol may decrease the antihypertensive activities of Levamlodipine.
Chlorpromazine Chlorpromazine may decrease the antihypertensive activities of Levamlodipine.
Nortriptyline Nortriptyline may decrease the antihypertensive activities of Levamlodipine.
Amoxapine Amoxapine may decrease the antihypertensive activities of Levamlodipine.
Doxapram Doxapram may decrease the antihypertensive activities of Levamlodipine.
Atropine Atropine may decrease the antihypertensive activities of Levamlodipine.
Lisuride Lisuride may decrease the antihypertensive activities of Levamlodipine.
Metaraminol Metaraminol may decrease the antihypertensive activities of Levamlodipine.
Guanabenz Guanabenz may decrease the antihypertensive activities of Levamlodipine.
Dexmedetomidine Dexmedetomidine may decrease the antihypertensive activities of Levamlodipine.
Sumatriptan Sumatriptan may decrease the antihypertensive activities of Levamlodipine.
Thioridazine Thioridazine may decrease the antihypertensive activities of Levamlodipine.
Phentolamine Phentolamine may decrease the antihypertensive activities of Levamlodipine.
Nicergoline Nicergoline may decrease the antihypertensive activities of Levamlodipine.
Sufentanil Sufentanil may decrease the antihypertensive activities of Levamlodipine.
Methoxamine Methoxamine may decrease the antihypertensive activities of Levamlodipine.
Trimipramine Trimipramine may decrease the antihypertensive activities of Levamlodipine.
Isoflurane Isoflurane may decrease the antihypertensive activities of Levamlodipine.
Propiomazine Propiomazine may decrease the antihypertensive activities of Levamlodipine.
Tolazoline Tolazoline may decrease the antihypertensive activities of Levamlodipine.
Orciprenaline Orciprenaline may decrease the antihypertensive activities of Levamlodipine.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Levamlodipine.
Trifluoperazine Trifluoperazine may decrease the antihypertensive activities of Levamlodipine.
Dobutamine Dobutamine may decrease the antihypertensive activities of Levamlodipine.
Pseudoephedrine Pseudoephedrine may decrease the antihypertensive activities of Levamlodipine.
Benzphetamine Benzphetamine may decrease the antihypertensive activities of Levamlodipine.
Ritodrine Ritodrine may decrease the antihypertensive activities of Levamlodipine.
Terbutaline Terbutaline may decrease the antihypertensive activities of Levamlodipine.
Flupentixol Flupentixol may decrease the antihypertensive activities of Levamlodipine.
Omapatrilat Omapatrilat may decrease the antihypertensive activities of Levamlodipine.
Remifentanil Remifentanil may decrease the antihypertensive activities of Levamlodipine.
Bitolterol Bitolterol may decrease the antihypertensive activities of Levamlodipine.
Almotriptan Almotriptan may decrease the antihypertensive activities of Levamlodipine.
Phenoxybenzamine Phenoxybenzamine may decrease the antihypertensive activities of Levamlodipine.
Diethylpropion Diethylpropion may decrease the antihypertensive activities of Levamlodipine.
Acetylsalicylic acid Acetylsalicylic acid may decrease the antihypertensive activities of Levamlodipine.
Naratriptan Naratriptan may decrease the antihypertensive activities of Levamlodipine.
Rizatriptan Rizatriptan may decrease the antihypertensive activities of Levamlodipine.
Formoterol Formoterol may decrease the antihypertensive activities of Levamlodipine.
Dopamine Dopamine may decrease the antihypertensive activities of Levamlodipine.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Levamlodipine.
Albuterol Salbutamol may decrease the antihypertensive activities of Levamlodipine.
Guanfacine Guanfacine may decrease the antihypertensive activities of Levamlodipine.
Methoxyflurane Methoxyflurane may decrease the antihypertensive activities of Levamlodipine.
Ergoloid mesylate Ergoloid mesylate may decrease the antihypertensive activities of Levamlodipine.
Isoprenaline Isoprenaline may decrease the antihypertensive activities of Levamlodipine.
Arbutamine Arbutamine may decrease the antihypertensive activities of Levamlodipine.
Doxepin Doxepin may decrease the antihypertensive activities of Levamlodipine.
Halothane Halothane may decrease the antihypertensive activities of Levamlodipine.
Rescinnamine Rescinnamine may decrease the antihypertensive activities of Levamlodipine.
Propafenone The risk or severity of bradycardia can be increased when Levamlodipine is combined with Propafenone.
Pergolide Pergolide may decrease the antihypertensive activities of Levamlodipine.
Desflurane Desflurane may decrease the antihypertensive activities of Levamlodipine.
Sevoflurane The risk or severity of hypotension can be increased when Sevoflurane is combined with Levamlodipine.
Clomipramine Clomipramine may decrease the antihypertensive activities of Levamlodipine.
Ergometrine Ergometrine may decrease the antihypertensive activities of Levamlodipine.
Lisdexamfetamine Lisdexamfetamine may decrease the antihypertensive activities of Levamlodipine.
Arformoterol Arformoterol may decrease the antihypertensive activities of Levamlodipine.
Fenoterol Fenoterol may decrease the antihypertensive activities of Levamlodipine.
Pirbuterol Pirbuterol may decrease the antihypertensive activities of Levamlodipine.
Ephedra sinica root Ephedra sinica root may decrease the antihypertensive activities of Levamlodipine.
Ephedrine Ephedrine may decrease the antihypertensive activities of Levamlodipine.
Mephentermine Mephentermine may decrease the antihypertensive activities of Levamlodipine.
Procaterol Procaterol may decrease the antihypertensive activities of Levamlodipine.
Yohimbine Yohimbine may decrease the antihypertensive activities of Levamlodipine.
Methotrimeprazine Methotrimeprazine may decrease the antihypertensive activities of Levamlodipine.
Clenbuterol Clenbuterol may decrease the antihypertensive activities of Levamlodipine.
Bambuterol Bambuterol may decrease the antihypertensive activities of Levamlodipine.
MMDA MMDA may decrease the antihypertensive activities of Levamlodipine.
Midomafetamine Midomafetamine may decrease the antihypertensive activities of Levamlodipine.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Levamlodipine.
4-Methoxyamphetamine 4-Methoxyamphetamine may decrease the antihypertensive activities of Levamlodipine.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Levamlodipine.
Tenamfetamine Tenamfetamine may decrease the antihypertensive activities of Levamlodipine.
Chlorphentermine Chlorphentermine may decrease the antihypertensive activities of Levamlodipine.
Dextroamphetamine Dextroamphetamine may decrease the antihypertensive activities of Levamlodipine.
Metamfetamine Metamfetamine may decrease the antihypertensive activities of Levamlodipine.

Target Protein

Voltage-dependent L-type calcium channel subunit alpha-1C CACNA1C
Voltage-dependent L-type calcium channel subunit alpha-1D CACNA1D
Nitric oxide synthase 3 NOS3
Nitric oxide synthase, inducible NOS2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 24301608
    Zhu Y, Wang F, Li Q, Zhu M, Du A, Tang W, Chen W: Amlodipine metabolism in human liver microsomes and roles of CYP3A4/5 in the dihydropyridine dehydrogenation. Drug Metab Dispos. 2014 Feb;42(2):245-9. doi: 10.1124/dmd.113.055400. Epub 2013 Dec 3.
  • PMID: 19450464
    Liu Z, Zheng X, Yang X, Wang E, Wang J: Affinity and specificity of levamlodipine-human serum albumin interactions: insights into its carrier function. Biophys J. 2009 May 20;96(10):3917-25. doi: 10.1016/j.bpj.2008.12.3965.
  • PMID: 7986667
    Laufen H, Leitold M: Enantioselective disposition of oral amlodipine in healthy volunteers. Chirality. 1994;6(7):531-6. doi: 10.1002/chir.530060704.
  • PMID: 25966690
    Striessnig J, Ortner NJ, Pinggera A: Pharmacology of L-type Calcium Channels: Novel Drugs for Old Targets? Curr Mol Pharmacol. 2015;8(2):110-22.
  • PMID: 1532771
    Meredith PA, Elliott HL: Clinical pharmacokinetics of amlodipine. Clin Pharmacokinet. 1992 Jan;22(1):22-31. doi: 10.2165/00003088-199222010-00003.
  • PMID: 2943308
    Faulkner JK, McGibney D, Chasseaud LF, Perry JL, Taylor IW: The pharmacokinetics of amlodipine in healthy volunteers after single intravenous and oral doses and after 14 repeated oral doses given once daily. Br J Clin Pharmacol. 1986 Jul;22(1):21-5.
  • PMID: 24683248
    Liu F, Qiu M, Zhai SD: Tolerability and effectiveness of (S)-amlodipine compared with racemic amlodipine in hypertension: a systematic review and meta-analysis. Curr Ther Res Clin Exp. 2010 Feb;71(1):1-29. doi: 10.1016/j.curtheres.2010.02.005.

Contoh Produk & Brand

Produk: 11 • International brands: 5
Produk
  • Conjupri
    Tablet • 1.25 mg/1.25mg • Oral • US • Approved
  • Conjupri
    Tablet • 2.5 mg/2.5mg • Oral • US • Approved
  • Conjupri
    Tablet • 5 mg/5mg • Oral • US • Approved
  • Conjupri
    Tablet • 1.25 mg/1 • Oral • US • Approved
  • Conjupri
    Tablet • 2.5 mg/1 • Oral • US • Approved
  • Conjupri
    Tablet • 5 mg/1 • Oral • US • Approved
  • Conjupri
    Tablet • 5 mg/5mg • Oral • US • Approved
  • Conjupri
    Tablet • 2.5 mg/1 • Oral • US • Approved
Menampilkan 8 dari 11 produk.
International Brands
  • Asomex — Emcure Pharmaceutical Ltd
  • Conjupri
  • EsCordi Cor — Actavis Pharma
  • Eslo — Zuventus Healthcare Ltd.
  • Espin — Intas Pharmaceuticals Ltd

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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