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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.
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.
| Property | Specification | Test Method |
|---|---|---|
| Chemical Name | L-3-(3.4-Dihydroxyphenyl)-2-methylalanine | IUPAC nomenclature |
| Molecular Formula | C₁₀H₁₃NO₄ | Elemental analysis |
| Molecular Weight | 211.21 g/mol | Mass spectrometry |
| Appearance | White to pale yellow crystalline powder | Visual inspection |
| Solubility (25°C) | Sparingly soluble in water (~10 mg/mL) | USP <911> |
| Parameter | Value/Description | Reference Standard |
|---|---|---|
| Mechanism of Action | Converted to α-methylnorepinephrine in CNS | FDA label |
| Bioavailability | ~25% (oral) | Clinical studies |
| Half-life (t₁/₂) | 1.5–2 hours | Pharmacokinetic data |
| Protein Binding | <15% | In vitro studies |
| Excretion | 70% renal (unchanged) | EMA assessment report |
| Medical Condition | Recommended Dosage | Maximum Daily Dose |
|---|---|---|
| Hypertension (adults) | 250–2000 mg/day (divided doses) | 3000 mg |
| Hypertension in pregnancy | 500–2000 mg/day | 3000 mg |
| Hypertensive emergencies | IV formulation available | Per physician discretion |
| Standard | Requirement | Compliance Status |
|---|---|---|
| USP-NF | Meets monograph standards | Compliant |
| Ph. Eur. | Conforms to EP 10.0 | Compliant |
| BP 2023 | Meets British Pharmacopoeia | Compliant |
| ICH Q3D (Impurities) | Heavy metals <20 ppm | Compliant |
| Residual Solvents | Class 2/3 limits per ICH Q3C | Compliant |
| Parameter | Specification |
|---|---|
| Storage temperature | 15–30°C (controlled room temp) |
| Shelf life | 24 months (unopened) |
| Light sensitivity | Protect from light |
| Packaging | Amber glass bottles or Alu-Alu blisters |
| Regulatory status | FDA/EMA-approved prescription drug |
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.
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