Peringatan Keamanan

The lowest published toxic dose via oral route is 44 gm/kg/3Y (intermittent) in a female. Oral LD50 is 5000 mg/kg in rats and 5300 mg/kg in mice. Intraperitoneal LD50 is 300 mg/kg in rats and 150 mg/kg in mice.L32704

Acute overdosage is characterized by acute hypotension and other presentations attributed to the brain and gastrointestinal dysfunction, such as excessive sedation, weakness, bradycardia, dizziness, light-headedness, constipation, distention, flatus, diarrhea, nausea, and vomiting. Symptomatic and supportive measures should be initiated in the event of methyldopa overdose. Overdosage following recent oral ingestion can be managed by gastric lavage or emesis, as well as infusions to limit further drug absorption. Cardiac rate and output, blood volume, electrolyte balance, paralytic ileus, urinary function and cerebral activity should be closely monitored. The use of sympathomimetic drugs such as levarterenol, epinephrine, and metaraminol bitartrate, or dialysis may be considered.L32614

Methyldopa

DB00968

small molecule approved

Deskripsi

Methyldopa, or ?-methyldopa, is a centrally acting sympatholytic agent and an antihypertensive agent.A231784 It is an analog of DOPA (3,4?hydroxyphenylanine), and it is a prodrug, meaning that the drug requires biotransformation to an active metabolite for therapeutic effects. Methyldopa works by binding to alpha(?)-2 adrenergic receptors as an agonist, leading to the inhibition of adrenergic neuronal outflow and reduction of vasoconstrictor adrenergic signals.A1499 Methyldopa exists in two isomers D-?-methyldopa and L-?-methyldopa, which is the active form.A232224

First introduced in 1960 as an antihypertensive agent, methyldopa was considered to be useful in certain patient populations, such as pregnant women and patients with renal insufficiency. Since then, methyldopa was largely replaced by newer, better-tolerated antihypertensive agents;A231784 however, it is still used as monotherapy L32614 or in combination with hydrochlorothiazide.L32619 Methyldopa is also available as intravenous injection, which is used to manage hypertension when oral therapy is unfeasible and to treat hypertensive crisis.L32624

Struktur Molekul 2D

Berat 211.2145
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The plasma half-life of methyldopa is 105 minutes.[L32614] Following intravenous injection, the plasma half-life of methyldopa ranges from 90 to 127 minutes.[L32624]
Volume Distribusi The apparent volume of distribution ranges between 0.19 and 0.32L/kg and the total volume of distribution ranges from 0.41 to 0.72L/kg. Since methyldopa is lipid-soluble [A231784], it crosses the placental barrier, appears in cord blood, and appears in breast milk.[L32614]
Klirens (Clearance) The renal clearance is about 130 mL/min in normal subjects and is decreased in patients with renal insufficiency.[L32614]

Absorpsi

Methyldopa is incompletely absorbed from the gastrointestinal tract following oral administration.A231789 In healthy individuals, the inactive D-isomer is less readily absorbed than the active L-isomer.A232224 The mean bioavailability of methyldopa is 25%, ranging from eight to 62%.A231789 Following oral administration, about 50% of the dose is absorbed and Tmax is about three to six hours.A232219, A231784

Metabolisme

Two isomers of methyldopa undergo different metabolic pathways.A232224 L-?-methyldopa is biotransformed to its pharmacologically active metabolite, alpha-methylnorepinephrine. Methyldopa is extensively metabolized in the liver to form the main circulating metabolite in the plasma, alpha (?)-methyldopa mono-O-sulfate. Its other metabolites also include 3-O-methyl-?-methyldopa; 3,4-dihydroxyphenylacetone; ?-methyldopamine; and 3-O-methyl-?-methyldopamine. These metabolites are further conjugated in the liver to form sulfate conjugates.L32614 After intravenous administration, the most prominent metabolites are alpha-methyldopamine and the glucuronide of dihydroxyphenylacetone, along with other uncharacterized metabolites.A231789 D-?-methyldopa, which is the inactive isomer of methyldopa, is also metabolized to 3-O-methyl-?-methyldopa and 3,4-dihydroxyphenylacetone to a minimal extent; however, there are no amines (?-methyldopamine and 3-O-methyl-?-methyldopamine) formed.A232224

Rute Eliminasi

Approximately 70% of absorbed methyldopa is excreted in the urine as unchanged parent drug (24%) and ?-methyldopa mono-O-sulfate (64%),A232219, L32614 with variability.3-O-methyl-?-methyldopa accounted for about 4% of urinary excretion products. Other metabolites like 3,4-dihydroxyphenylacetone, ?-methyldopamine, and 3-O-methyl-?-methyldopamine are also excreted in urine.A232219 Unabsorbed drug is excreted in feces as the unchanged parent compound.A231784 After oral doses, excretion is essentially complete in 36 hours.L32619 Due to attenuated excretion in patients with renal failure, accumulation of the drug and its metabolites may occur,A231784 possibly leading to more profound and prolonged hypotensive effects in these patients.A231789

Interaksi Makanan

1 Data
  • 1. Take with or without food. Drug pharmacokinetics is unaffected.

Interaksi Obat

1308 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Methyldopa is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Methyldopa is combined with Levodopa.
Risperidone Methyldopa may increase the hypotensive activities of Risperidone.
Ceritinib Methyldopa may increase the bradycardic activities of Ceritinib.
Ivabradine Methyldopa may increase the bradycardic activities of Ivabradine.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Methyldopa.
Alfuzosin Alfuzosin may increase the hypotensive activities of Methyldopa.
Amifostine Methyldopa may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Methyldopa.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Methyldopa.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Methyldopa.
Obinutuzumab Methyldopa may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Methyldopa.
Rituximab Methyldopa may increase the hypotensive activities of Rituximab.
Phentermine Phentermine may decrease the antihypertensive activities of Methyldopa.
Eletriptan Eletriptan may decrease the antihypertensive activities of Methyldopa.
Isoetharine Isoetharine may decrease the antihypertensive activities of Methyldopa.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Methyldopa.
Norepinephrine Norepinephrine may decrease the antihypertensive activities of Methyldopa.
Phenylephrine Phenylephrine may decrease the antihypertensive activities of Methyldopa.
Phenylpropanolamine Phenylpropanolamine may decrease the antihypertensive activities of Methyldopa.
Doxapram Doxapram may decrease the antihypertensive activities of Methyldopa.
Atropine Atropine may decrease the antihypertensive activities of Methyldopa.
Metaraminol Metaraminol may decrease the antihypertensive activities of Methyldopa.
Epinephrine Epinephrine may decrease the antihypertensive activities of Methyldopa.
Methoxamine Methoxamine may decrease the antihypertensive activities of Methyldopa.
Orciprenaline Orciprenaline may decrease the antihypertensive activities of Methyldopa.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Methyldopa.
Pseudoephedrine Pseudoephedrine may decrease the antihypertensive activities of Methyldopa.
Benzphetamine Benzphetamine may decrease the antihypertensive activities of Methyldopa.
Ritodrine Ritodrine may decrease the antihypertensive activities of Methyldopa.
Bitolterol Bitolterol may decrease the antihypertensive activities of Methyldopa.
Diethylpropion Diethylpropion may decrease the antihypertensive activities of Methyldopa.
Naratriptan Naratriptan may decrease the antihypertensive activities of Methyldopa.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Methyldopa.
Methoxyflurane Methoxyflurane may decrease the antihypertensive activities of Methyldopa.
Isoprenaline Isoprenaline may decrease the antihypertensive activities of Methyldopa.
Arbutamine Arbutamine may decrease the antihypertensive activities of Methyldopa.
Dutasteride Dutasteride may decrease the antihypertensive activities of Methyldopa.
Finasteride Finasteride may decrease the antihypertensive activities of Methyldopa.
Lisdexamfetamine Lisdexamfetamine may decrease the antihypertensive activities of Methyldopa.
Fenoterol Fenoterol may decrease the antihypertensive activities of Methyldopa.
Pirbuterol Pirbuterol may decrease the antihypertensive activities of Methyldopa.
Ephedra sinica root Ephedra sinica root may decrease the antihypertensive activities of Methyldopa.
Ephedrine Ephedrine may decrease the antihypertensive activities of Methyldopa.
Mephentermine Mephentermine may decrease the antihypertensive activities of Methyldopa.
Procaterol Procaterol may decrease the antihypertensive activities of Methyldopa.
Yohimbine Yohimbine may decrease the antihypertensive activities of Methyldopa.
Clenbuterol Clenbuterol may decrease the antihypertensive activities of Methyldopa.
Bambuterol Bambuterol may decrease the antihypertensive activities of Methyldopa.
MMDA MMDA may decrease the antihypertensive activities of Methyldopa.
Midomafetamine Midomafetamine may decrease the antihypertensive activities of Methyldopa.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Methyldopa.
4-Methoxyamphetamine 4-Methoxyamphetamine may decrease the antihypertensive activities of Methyldopa.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Methyldopa.
Tenamfetamine Tenamfetamine may decrease the antihypertensive activities of Methyldopa.
Chlorphentermine Chlorphentermine may decrease the antihypertensive activities of Methyldopa.
Dextroamphetamine Dextroamphetamine may decrease the antihypertensive activities of Methyldopa.
Phendimetrazine Phendimetrazine may decrease the antihypertensive activities of Methyldopa.
Solifenacin Solifenacin may decrease the antihypertensive activities of Methyldopa.
Epicaptopril Epicaptopril may decrease the antihypertensive activities of Methyldopa.
1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Methyldopa.
Flibanserin Flibanserin may decrease the antihypertensive activities of Methyldopa.
Indacaterol Indacaterol may decrease the antihypertensive activities of Methyldopa.
Amibegron Amibegron may decrease the antihypertensive activities of Methyldopa.
Naluzotan Naluzotan may decrease the antihypertensive activities of Methyldopa.
Cariprazine Cariprazine may decrease the antihypertensive activities of Methyldopa.
Solabegron Solabegron may decrease the antihypertensive activities of Methyldopa.
Esmirtazapine Esmirtazapine may decrease the antihypertensive activities of Methyldopa.
Vilazodone Vilazodone may decrease the antihypertensive activities of Methyldopa.
Nitrous oxide Nitrous oxide may decrease the antihypertensive activities of Methyldopa.
Xylometazoline Xylometazoline may decrease the antihypertensive activities of Methyldopa.
Isometheptene Isometheptene may decrease the antihypertensive activities of Methyldopa.
Levonordefrin Levonordefrin may decrease the antihypertensive activities of Methyldopa.
Naphazoline Naphazoline may decrease the antihypertensive activities of Methyldopa.
Saralasin Saralasin may decrease the antihypertensive activities of Methyldopa.
Tetryzoline Tetryzoline may decrease the antihypertensive activities of Methyldopa.
Cinitapride Cinitapride may decrease the antihypertensive activities of Methyldopa.
Lurasidone Lurasidone may decrease the antihypertensive activities of Methyldopa.
Tyramine Tyramine may decrease the antihypertensive activities of Methyldopa.
Adrafinil Adrafinil may decrease the antihypertensive activities of Methyldopa.
Ifenprodil Ifenprodil may decrease the antihypertensive activities of Methyldopa.
Hexoprenaline Hexoprenaline may decrease the antihypertensive activities of Methyldopa.
Etilefrine Etilefrine may decrease the antihypertensive activities of Methyldopa.
Cannabidiol Cannabidiol may decrease the antihypertensive activities of Methyldopa.
Olodaterol Olodaterol may decrease the antihypertensive activities of Methyldopa.
Cirazoline Cirazoline may decrease the antihypertensive activities of Methyldopa.
Synephrine Synephrine may decrease the antihypertensive activities of Methyldopa.
Iofetamine I-123 Iofetamine I-123 may decrease the antihypertensive activities of Methyldopa.
Racepinephrine Racepinephrine may decrease the antihypertensive activities of Methyldopa.
Amitraz Amitraz may decrease the antihypertensive activities of Methyldopa.
Medetomidine Medetomidine may decrease the antihypertensive activities of Methyldopa.
Xylazine Xylazine may decrease the antihypertensive activities of Methyldopa.
Atipamezole Atipamezole may decrease the antihypertensive activities of Methyldopa.
Ractopamine Ractopamine may decrease the antihypertensive activities of Methyldopa.
Romifidine Romifidine may decrease the antihypertensive activities of Methyldopa.
Detomidine Detomidine may decrease the antihypertensive activities of Methyldopa.
Tetrahydrocannabivarin Tetrahydrocannabivarin may decrease the antihypertensive activities of Methyldopa.
PF-00610355 PF-00610355 may decrease the antihypertensive activities of Methyldopa.
Ritobegron Ritobegron may decrease the antihypertensive activities of Methyldopa.

Target Protein

D(2) dopamine receptor DRD2
Aromatic-L-amino-acid decarboxylase DDC
Alpha-2A adrenergic receptor ADRA2A

Referensi & Sumber

Artikel (PubMed)
  • PMID: 19821316
    Mah GT, Tejani AM, Musini VM: Methyldopa for primary hypertension. Cochrane Database Syst Rev. 2009 Oct 7;(4):CD003893. doi: 10.1002/14651858.CD003893.pub3.
  • PMID: 17485976
    Sica DA: Centrally acting antihypertensive agents: an update. J Clin Hypertens (Greenwich). 2007 May;9(5):399-405.
  • PMID: 6104975
    van Zwieten PA: Pharmacology of centrally acting hypotensive drugs. Br J Clin Pharmacol. 1980;10 Suppl 1:13S-20S.
  • PMID: 31869135
    Gupta M, Al Khalili Y: Methyldopa .
  • PMID: 7047042
    Myhre E, Rugstad HE, Hansen T: Clinical pharmacokinetics of methyldopa. Clin Pharmacokinet. 1982 May-Jun;7(3):221-33. doi: 10.2165/00003088-198207030-00003.
  • PMID: 14163994
    BUHS RP, BECK JL, SPETH OC, SMITH JL, TRENNER NR, CANNON PJ, LARAGH JH: THE METABOLISM OF METHYLDOPA IN HYPERTENSIVE HUMAN SUBJECTS. J Pharmacol Exp Ther. 1964 Feb;143:205-14.
  • PMID: 4646774
    Au WY, Dring LG, Grahame-Smith DG, Isaac P, Williams RT: The metabolism of 14 C-labelled -methyldopa in normal and hypertensive human subjects. Biochem J. 1972 Aug;129(1):1-10. doi: 10.1042/bj1290001.
  • PMID: 6355433
    Tung CS, Goldberg MR, Hollister AS, Oates JA, Robertson D: Central and peripheral cardiovascular effects of alpha-methylepinephrine. J Pharmacol Exp Ther. 1983 Nov;227(2):484-90.
Menampilkan 8 dari 10 artikel.

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