Adverse Drug Reaction Classification System

Pharmaceutical Information
Drug Name Methyldopate hydrochloride
Drug ID BADD_D01426
Description Methyldopa, or α-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(α)-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-α-methyldopa and L-α-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]
Indications and Usage For use in the treatment of hypertension.
Marketing Status Prescription; Discontinued
ATC Code C02AB01
DrugBank ID DB00968
KEGG ID D08205
MeSH ID D008750
PubChem ID 17276
TTD Drug ID D0BA6T
NDC Product Code 52423-0100; 16729-031; 42185-7001; 15894-0038; 16729-030; 67628-3001
Synonyms Methyldopa | alpha-Methyldopa | alpha Methyldopa | alpha-Methyl-L-Dopa | alpha Methyl L Dopa | Alphamethyldopa | Meldopa | Methyldopate | Dopegyt | Dopergit | Dopegit | Sembrina | Apo-Methyldopa | Apo Methyldopa | Dopamet | Aldomet | Hydopa | Nu-Medopa | Nu Medopa
Chemical Information
Molecular Formula C12H18ClNO4
CAS Registry Number 2508-79-4
SMILES CCOC(=O)C(C)(CC1=CC(=C(C=C1)O)O)N.Cl
Chemical Structure
ADR Related Proteins Induced by Drug
ADR Term Protein Name UniProt AC TTD Target ID PMID
Not AvailableNot AvailableNot AvailableNot AvailableNot Available
ADRs Induced by Drug
ADR Term ADReCS ID ADR Frequency (FAERS) ADR Severity Grade (FAERS) ADR Severity Grade (CTCAE)
Abdominal distension07.01.04.001--
Amenorrhoea21.01.02.001; 05.05.01.002--
Angina pectoris24.04.04.002; 02.02.02.002--
Aphthous ulcer07.05.06.002--Not Available
Arthralgia15.01.02.001--
Asthenia08.01.01.001--Not Available
Blood urea increased13.13.01.006--Not Available
Bradycardia02.03.02.002--Not Available
Breast enlargement21.05.04.001--Not Available
Cardiac failure congestive02.05.01.002--Not Available
Choreoathetosis17.01.01.003--Not Available
Colitis07.08.01.001--
Constipation07.02.02.001--
Depression19.15.01.001--
Diarrhoea07.02.01.001--
Dizziness24.06.02.007; 17.02.05.003; 02.01.02.004--
Dry mouth07.06.01.002--
Eosinophilia01.02.04.001--
Facial paralysis17.04.03.008--Not Available
Flatulence07.01.04.002--
Granulocytopenia01.02.03.003--Not Available
Gynaecomastia21.05.04.003; 05.05.02.003--
Haemolytic anaemia01.06.03.002--Not Available
Headache17.14.01.001--
Hepatitis09.01.07.004--Not Available
Hyperprolactinaemia05.03.01.002--Not Available
Jaundice09.01.01.004; 01.06.04.004; 23.03.03.030--Not Available
Joint swelling15.01.02.004--Not Available
LE cells present13.06.01.001--Not Available
Leukopenia01.02.02.001--Not Available
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