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Methyldopa

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Methyldopa, antihypertensive drug, α Receptor agonists are commonly used in tablets. This product is a kind of stimulant for vascular motor center α- Receptors, thus inhibiting the external sensory nerve, producing a hypotensive effect, accompanied by slowing down the heart rate, reducing the cardiac output, dilating the arterioles, significantly reducing the resistance of peripheral blood vessels, and not significantly reducing the cardiac output during long-term application.

Product Overview

Methyldopa is a centrally acting antihypertensive agent that functions as an α₂-adrenergic receptor agonist. It is primarily used to manage hypertension during pregnancy and in patients with renal impairment. This document outlines its physicochemical properties, pharmacological effects, and regulatory compliance.

Basic Physicochemical Properties

PropertySpecificationTest Method
Chemical NameL-3-(3.4-Dihydroxyphenyl)-2-methylalanineIUPAC nomenclature
Molecular FormulaC₁₀H₁₃NO₄Elemental analysis
Molecular Weight211.21 g/molMass spectrometry
AppearanceWhite to pale yellow crystalline powderVisual inspection
Solubility (25°C)Sparingly soluble in water (~10 mg/mL)USP <911>

Pharmacological Profile

ParameterValue/DescriptionReference Standard
Mechanism of ActionConverted to α-methylnorepinephrine in CNSFDA label
Bioavailability~25% (oral)Clinical studies
Half-life (t₁/₂)1.5–2 hoursPharmacokinetic data
Protein Binding<15%In vitro studies
Excretion70% renal (unchanged)EMA assessment report

Therapeutic Applications & Dosage

Medical ConditionRecommended DosageMaximum Daily Dose
Hypertension (adults)250–2000 mg/day (divided doses)3000 mg
Hypertension in pregnancy500–2000 mg/day3000 mg
Hypertensive emergenciesIV formulation availablePer physician discretion

Pharmacopoeial Compliance

StandardRequirementCompliance Status
USP-NFMeets monograph standardsCompliant
Ph. Eur.Conforms to EP 10.0Compliant
BP 2023Meets British PharmacopoeiaCompliant
ICH Q3D (Impurities)Heavy metals <20 ppmCompliant
Residual SolventsClass 2/3 limits per ICH Q3CCompliant

Stability & Storage Conditions

ParameterSpecification
Storage temperature15–30°C (controlled room temp)
Shelf life24 months (unopened)
Light sensitivityProtect from light
PackagingAmber glass bottles or Alu-Alu blisters
Regulatory statusFDA/EMA-approved prescription drug

Conclusion

Methyldopa remains a safe and effective antihypertensive, particularly in pregnancy and renal impairment. Its unique CNS-mediated mechanism and established safety profile make it a preferred choice in specific patient populations.

Disclaimer: The above content is for reference and communication only among industry insiders, and does not guarantee its accuracy or completeness. According to relevant laws and regulations and the regulations of this website, units or individuals who purchase related items should obtain valid qualifications and qualification conditions.

Declaration: The products displayed on this website are intended exclusively for industrial applications or scientific research. They are not intended for medical, pharmaceutical, or food use. In accordance with applicable laws and regulations, purchasing organizations must hold valid qualifications and approvals.

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