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QuickView for Methyldopa (compound)

Name: Methyldopa
PubChem Compound ID: 111128
Description: An alpha-2 adrenergic agonist that has both central and peripheral nervous system effects. Its primary clinical use is as an antihypertensive agent.
Molecular formula: C12H17NO4
Molecular weight: 239.268 g/mol
Alanine, 3-(3,4-dihydroxyphenyl)-2-methyl-, ethyl ester, L-; L-3-(3,4-Dihydroxyphenyl)-2-methylalanine ethyl ester; METHYLDOPATE; Ethyl 2-amino-3-(3,4-dihydroxyphenyl)-2-methylpropanoate; 6014-30-8
Name: Methyldopa
Name (isomeric): DB00968
Drug Type: small molecule
Description: An alpha-2 adrenergic agonist that has both central and peripheral nervous system effects. Its primary clinical use is as an antihypertensive agent.
Mk. b51; Methyldopa anhydrous; Alphamethyldopa; Methyldopate HCL; AMD; Alpha medopa; L-Methyl Dopa; Methyldopate
Brand: Aldoril D30, Becanta, Dopamet, Sedometil, Aldomin, Medomet, Apo-Methyldopa, Hyperpax, Sembrina, Baypresol, Methoplain, Aldoril 15, Bayer 1440 L, Presinol, Dopegyt, Dopatec, Aldometil, Medopal, Presolisin, Nu-Medopa, Grospisk, Aldoclor-250, Medopa, Hypolag, Aldomet, Novomedopa, Aldoril 25, Aldoril D50, Aldoclor-150, Medopren, Dopamethyperpax
Brand name mixture:
Supres 150 Tab(Chlorothiazide + Methyldopa), Novo-Doparil 15 Tab(Hydrochlorothiazide + Methyldopa), Apo Methazide 25(Hydrochlorothiazide + Methyldopa), Aldoril 15 Tab(Hydrochlorothiazide + Methyldopa), Novo-Doparil 25 Tab(Hydrochlorothiazide + Methyldopa), Apo Methazide 15(Hydrochlorothiazide + Methyldopa), Supres 250 Tab(Chlorothiazide + Methyl...
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Category: Sympatholytics, Adrenergic alpha-Agonists, Antihypertensive Agents
CAS number: 555-30-6
Indication: For use in the treatment of hypertension.
Methyldopa is an aromatic-amino-acid decarboxylase inhibitor in animals and in man. Only methyldopa, the L-isomer of alpha-methyldopa, has the ability to inhibit dopa decarboxylase and to deplete animal tissues of norepinephrine. In man the antihypertensive activity appears to be due solely to the L-isomer. About twice the dose of the racema...
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Mechanism of Action:
Although the mechanism of action has yet to be conclusively demonstrated, the resultant hypotensive effect is most likely due to the drug's action on the CNS. Methyldopa is converted into the metabolite, alpha-methylnorepinephrine, in the CNS, where it stimulates the central inhibitory alpha-adrenergic receptors, leading to a reduction in sympathet...
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Absorption: Absorption from the gastrointestinal tract is variable but averages approximately 50%.
Protein binding: Low (less than 20%).
Biotransformation: Hepatic, extensively metabolized. The known urinary metabolites are: a-methyldopa mono-0-sulfate; 3-0-methyl-a-methyldopa; 3,4-dihydroxyphenylacetone; a-methyldopamine; 3-0-methyl-a-methyldopamine and their conjugates.
Route of elimination: Methyldopa is extensively metabolized. The known urinary metabolites are: α-methyldopa mono-O-sulfate; 3-0-methyl-α-methyldopa; 3,4-dihydroxyphenylacetone; α-methyldopamine; 3-0-methyl-α-methyldopamine and their conjugates. Approximately 70 percent of the drug which is absorbed is excreted in the urine as methyldopa and its mono-O-sulfate conjugate. Methyldopa crosses the placental barrier, appears in cord blood, and appears in breast milk.
Half Life: The plasma half-life of methyldopa is 105 minutes.
Clearance: Renal cl=130 mL/min [healthy]
Toxicity: The oral LD50 of methyldopa is greater than 1.5 g/kg in both the mouse and the rat. Symptoms of overdose include bloating, constipation, diarrhea, dizziness, extreme drowsiness, gas, light-headedness, nausea, severely low blood pressure, slow heartbeat, vomiting, and weakness.
Affected organisms: Humans and other mammals
Food interaction:
Avoid alcohol.
No iron, zinc or fluoride within 2 hours of taking this medication.
May take Vitamin D.
Increase dietary intake of magnesium, folate, vitamin B6, B12, and/or consider taking a multivitamin.
Take without regard to meals.
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Drug interaction:
PseudoephedrineIncreased arterial pressure
EntacaponeEntacapone may increase the effect and toxicity of the sympathomimetic, methyldopa.
ProcaterolIncreased arterial pressure
PropranololPossible hypertensive crisis
EphedrineIncreased arterial pressure
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