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Methyldopa | CAS No: 555-30-6 | GMP-certified suppliers
A medication that manages hypertension, including acute hypertensive crises, supporting reliable blood pressure control for diverse patient populations in key markets.
Therapeutic categories
Adrenergic AgentsAdrenergic AgonistsAdrenergic alpha-2 Receptor AgonistsAdrenergic alpha-AgonistsAgents Causing Muscle ToxicityAmines
Generic name
Methyldopa
Molecule type
small molecule
CAS number
555-30-6
DrugBank ID
DB00968
Approval status
Approved drug
ATC code
C02AB01
Primary indications
- Methyldopa is indicated for the management of hypertension as monotherapy or in combination with hydrochlorothiazide
- Methyldopa injection is used to manage hypertensive crises
Product Snapshot
- Methyldopa is available as an oral small‑molecule drug and as an injectable solution for acute care use
- It is used for hypertension management, including monotherapy, combination regimens, and hypertensive crises
- It is approved in the US and Canada for these indications
Clinical Overview
Methyldopa (CAS 555-30-6) is a centrally acting antihypertensive agent indicated for the management of hypertension, including use as monotherapy or in combination with hydrochlorothiazide. An intravenous formulation is used when oral therapy is not feasible and in the management of hypertensive crises. Clinically, methyldopa remains relevant in specific patient groups such as pregnant individuals and those with renal impairment, despite declining utilization due to newer agents.
Methyldopa is a prodrug and structural analog of DOPA. Its antihypertensive effect is mediated primarily through the metabolite alpha‑methylnorepinephrine, with minor contributions from alpha‑methylepinephrine. These metabolites act as agonists at central presynaptic alpha‑2 adrenergic receptors, reducing sympathetic outflow from the brainstem and lowering peripheral vascular resistance. Additional but limited pharmacological activity arises from inhibition of aromatic L‑amino acid decarboxylase by the L‑isomer, leading to reduced synthesis of catecholamines and serotonin.
Following oral administration, onset of blood‑pressure reduction typically occurs within 12 to 24 hours, with maximal effect in 4 to 6 hours. Blood pressure generally returns to baseline within 24 to 48 hours after discontinuation. After intravenous dosing, effects persist for approximately 10 to 16 hours. Methyldopa reduces plasma renin activity but has minimal direct effects on glomerular filtration rate, renal blood flow, or cardiac contractility. Occasional bradycardia may occur.
Safety considerations include potential sedation, dizziness, and rare hematologic or hepatic adverse reactions. Methyldopa can deplete central neurotransmitter stores, contributing to some of its tolerability limitations. Postural hypotension is generally infrequent compared with other central sympatholytics.
For API procurement, attention to stereochemical purity is important because the L‑isomer is pharmacologically active. Suppliers should provide validated controls for impurities, residual solvents, and degradation pathways to support formulation development and regulatory submissions.
Methyldopa is a prodrug and structural analog of DOPA. Its antihypertensive effect is mediated primarily through the metabolite alpha‑methylnorepinephrine, with minor contributions from alpha‑methylepinephrine. These metabolites act as agonists at central presynaptic alpha‑2 adrenergic receptors, reducing sympathetic outflow from the brainstem and lowering peripheral vascular resistance. Additional but limited pharmacological activity arises from inhibition of aromatic L‑amino acid decarboxylase by the L‑isomer, leading to reduced synthesis of catecholamines and serotonin.
Following oral administration, onset of blood‑pressure reduction typically occurs within 12 to 24 hours, with maximal effect in 4 to 6 hours. Blood pressure generally returns to baseline within 24 to 48 hours after discontinuation. After intravenous dosing, effects persist for approximately 10 to 16 hours. Methyldopa reduces plasma renin activity but has minimal direct effects on glomerular filtration rate, renal blood flow, or cardiac contractility. Occasional bradycardia may occur.
Safety considerations include potential sedation, dizziness, and rare hematologic or hepatic adverse reactions. Methyldopa can deplete central neurotransmitter stores, contributing to some of its tolerability limitations. Postural hypotension is generally infrequent compared with other central sympatholytics.
For API procurement, attention to stereochemical purity is important because the L‑isomer is pharmacologically active. Suppliers should provide validated controls for impurities, residual solvents, and degradation pathways to support formulation development and regulatory submissions.
Identification & chemistry
| Generic name | Methyldopa |
|---|---|
| Molecule type | Small molecule |
| CAS | 555-30-6 |
| UNII | M4R0H12F6M |
| DrugBank ID | DB00968 |
Pharmacology
| Summary | Methyldopa is converted to active metabolites that act as central alpha‑2 adrenergic receptor agonists, reducing sympathetic outflow from the brainstem. This decreases peripheral adrenergic signaling, producing its primary antihypertensive effect. It also weakly inhibits aromatic L‑amino acid decarboxylase, but this contributes minimally to its therapeutic action. |
|---|---|
| Mechanism of action | The exact mechanism of methyldopa is not fully elucidated; however, the main mechanisms of methyldopa involve its actions on alpha-adrenergic receptor and the aromatic L-amino acid decarboxylase enzyme, to a lesser extent. The sympathetic outflow is regulated by alpha (α)-2 adrenergic receptors and imidazoline receptors expressed on adrenergic neurons within the rostral ventrolateral medulla.Methyldopa is metabolized to α‐methylnorepinephrine via dopamine beta-hydroxylase activity and, consequently, alpha-methylepinephrine via phenylethanolamine-N-methyltransferase activity.Mediating the therapeutic effects of methyldopa, α‐methylnorepinephrine and α-methylepinephrine active metabolites are agonists at presynaptic alpha-2 adrenergic receptors in the brainstem. Stimulating alpha-2 adrenergic receptors results in the inhibition of adrenergic neuronal outflow and attenuation of norepinephrine release in the brainstem. Consequently, the output of vasoconstrictor adrenergic signals to the peripheral sympathetic nervous system is reduced, leading to a reduction in blood pressure. The L-isomer of alpha-methyldopa also reduces blood pressure by inhibiting aromatic L-amino acid decarboxylase, also known as DOPA decarboxylase, which is an enzyme responsible for the syntheses of dopamine and serotonin.Inhibiting this enzyme leads to depletion of biogenic amines such as norepinephrine. However, inhibition of aromatic L-amino acid decarboxylase plays a minimal role in the blood-pressure‐lowering effect of methyldopa. |
| Pharmacodynamics | Antihypertensive effects of methyldopa are mostly mediated by its pharmacologically active metabolite, alpha-methylnorepinephrine, which works as an agonist at central inhibitory alpha-adrenergic receptors.Stimulation of alpha-adrenergic receptors leads to decreased peripheral sympathetic tone and reduced arterial pressure.Methyldopa causes a net reduction in the tissue concentration of serotonin, dopamine, norepinephrine, and epinephrine. Overall, methyldopa lowers both standing blood pressure and especially supine blood pressure, with infrequent symptomatic postural hypotension. Methyldopa also reduces plasma renin activity but has negligible effects on glomerular filtration rate, renal blood flow, or filtration fraction. It also has no direct effect on cardiac function but in some patients, a slowed heart rate may occur. Following oral administration, blood-pressure-lowering effects are observed within 12 to 24 hours in most patients, and a maximum reduction in blood pressure occurs in 4 to 6 hours. Blood pressure returns to pre-treatment levels within 24 to 48 hours following drug discontinuation.Following intravenous administration, the blood-pressure-lowering effects of methyldopa last for about 10 to 16 hours. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Aromatic-L-amino-acid decarboxylase | Humans | inhibitor |
| Alpha-2A adrenergic receptor | Humans | agonist |
ADME / PK
| Absorption | Methyldopa is incompletely absorbed from the gastrointestinal tract following oral administration.In healthy individuals, the inactive D-isomer is less readily absorbed than the active L-isomer.The mean bioavailability of methyldopa is 25%, ranging from eight to 62%.Following oral administration, about 50% of the dose is absorbed and T<sub>max</sub> is about three to six hours. |
|---|---|
| Half-life | The plasma half-life of methyldopa is 105 minutes.Following intravenous injection, the plasma half-life of methyldopa ranges from 90 to 127 minutes. |
| Protein binding | Methyldopa is less than 15% bound to plasma proteins and its primary metabolite, O-sulfate metabolite, is about 50% protein bound.Following intravenous administration, approximately 17% of the dose in normal subjects were circulating in the plasma as free methyldopa. |
| Metabolism | Two isomers of methyldopa undergo different metabolic pathways.L-α-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 (α)-methyldopa mono-O-sulfate. Its other metabolites also include 3-O-methyl-α-methyldopa; 3,4-dihydroxyphenylacetone; α-methyldopamine; and 3-O-methyl-α-methyldopamine. These metabolites are further conjugated in the liver to form sulfate conjugates.After intravenous administration, the most prominent metabolites are alpha-methyldopamine and the glucuronide of dihydroxyphenylacetone, along with other uncharacterized metabolites. D-α-methyldopa, which is the inactive isomer of methyldopa, is also metabolized to 3-O-methyl-α-methyldopa and 3,4-dihydroxyphenylacetone to a minimal extent; however, there are no amines (α-methyldopamine and 3-O-methyl-α-methyldopamine) formed. |
| Route of elimination | Approximately 70% of absorbed methyldopa is excreted in the urine as unchanged parent drug (24%) and α-methyldopa mono-O-sulfate (64%),with variability.3-O-methyl-α-methyldopa accounted for about 4% of urinary excretion products. Other metabolites like 3,4-dihydroxyphenylacetone, α-methyldopamine, and 3-O-methyl-α-methyldopamine are also excreted in urine. Unabsorbed drug is excreted in feces as the unchanged parent compound.After oral doses, excretion is essentially complete in 36 hours. Due to attenuated excretion in patients with renal failure, accumulation of the drug and its metabolites may occur,possibly leading to more profound and prolonged hypotensive effects in these patients. |
| Volume of distribution | 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 , it crosses the placental barrier, appears in cord blood, and appears in breast milk. |
| Clearance | The renal clearance is about 130 mL/min in normal subjects and is decreased in patients with renal insufficiency. |
Formulation & handling
- Oral formulations are straightforward given good aqueous solubility and small‑molecule properties, with no meaningful food effect on absorption.
- The solid API is hygroscopic-sensitive and may require protection from moisture during processing and storage to maintain stability.
- IV solutions require control of pH and protection from oxidation to prevent discoloration and degradation during manufacture and holding.
Regulatory status
| Lifecycle | Marketed in Canada and the US, the API is in a mature phase in both markets, where lifecycle dynamics are largely shaped by scheduled or completed patent expiries. As patents expire, competition typically increases, signaling progression toward a post‑exclusivity market environment. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Methyldopa’s originator products, marketed under the Aldomet/Aldoril brands, indicate an established reference product lineage, with current supply largely maintained by numerous repackagers and generic manufacturers. The presence of branded products in the US and Canada, along with broad generic distribution, reflects mature global availability. Patent expiry occurred long ago, so the market already exhibits full generic competition with no exclusivity constraints. |
|---|
Safety
| Toxicity | The lowest published toxic dose via oral route is 44 gm/kg/3Y (intermittent) in a female. Oral LD<sub>50</sub> is 5000 mg/kg in rats and 5300 mg/kg in mice. Intraperitoneal LD<sub>50</sub> is 300 mg/kg in rats and 150 mg/kg in mice. 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. |
|---|
High Level Warnings:
- High oral LD50 values in rodents (about 5000–5300 mg/kg) indicate comparatively low acute oral toxicity, while substantially lower intraperitoneal LD50 values (150–300 mg/kg) reflect higher systemic toxicity with parenteral exposure
- Acute overexposure may involve pronounced CNS and gastrointestinal effects along with cardiovascular depression, highlighting the need for controls that limit excessive systemic uptake
- Documented toxic dose data (e
Methyldopa is a type of Antihypertensive agents
Antihypertensive agents are a crucial category of pharmaceutical active pharmaceutical ingredients (APIs) used to treat high blood pressure, also known as hypertension. These medications are designed to lower blood pressure and reduce the risk of associated cardiovascular complications.
Antihypertensive agents function by targeting various mechanisms involved in blood pressure regulation. Some common classes of antihypertensive agents include angiotensin-converting enzyme (ACE) inhibitors, angiotensin II receptor blockers (ARBs), beta-blockers, calcium channel blockers (CCBs), and diuretics.
ACE inhibitors work by inhibiting the enzyme responsible for converting angiotensin I to angiotensin II, a hormone that constricts blood vessels. ARBs, on the other hand, block the receptors to which angiotensin II binds, thereby preventing its vasoconstrictive effects.
Beta-blockers reduce blood pressure by blocking the effects of adrenaline and noradrenaline, which are responsible for increasing heart rate and constricting blood vessels. CCBs inhibit calcium from entering the smooth muscles of blood vessels, resulting in relaxation and vasodilation. Diuretics promote the elimination of excess fluid and sodium from the body, reducing blood volume and thereby lowering blood pressure.
Antihypertensive agents are typically prescribed based on the individual patient's condition and specific needs. They can be used alone or in combination to achieve optimal blood pressure control. It is important to note that antihypertensive agents should be taken regularly as prescribed by a healthcare professional and may require periodic monitoring to ensure their effectiveness and manage any potential side effects.
In summary, antihypertensive agents play a vital role in the management of hypertension by targeting various mechanisms involved in blood pressure regulation. These medications offer significant benefits in reducing the risk of cardiovascular complications associated with high blood pressure.
Methyldopa API manufacturers & distributors
Compare qualified Methyldopa API suppliers worldwide. We currently have 5 companies offering Methyldopa API, with manufacturing taking place in 3 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Apollo Healthcare Resourc... | Distributor | Singapore | Singapore | BSE/TSE, CEP, CoA, EDMF/ASMF, FDA, GMP, ISO9001, JDMF, KDMF, MSDS, USDMF, WC | 200 products |
| Arshine Pharmaceutical Co... | Distributor | China | China | BSE/TSE, CEP, CoA, FDA, GMP, MSDS, USDMF | 176 products |
| LGM Pharma | Distributor | United States | World | CEP, GMP, USDMF | 441 products |
| Zhejiang Chiral M.C. | Producer | China | China | CEP, CoA, FDA, USDMF, WC | 4 products |
| Zhejiang Wild Wind | Producer | China | China | CEP, CoA, USDMF, WC | 4 products |
When sending a request, specify which Methyldopa API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Methyldopa API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
Frequently asked questions about Methyldopa API
Sourcing
What matters most when sourcing GMP-grade Methyldopa?
The priority is confirming GMP compliance and alignment with US and Canadian regulatory expectations. Given Methyldopa’s mature, fully generic market, verifying the manufacturer’s quality track record and documentation is essential. It is also important to assess supply continuity, as availability is maintained through multiple generic producers and repackagers.
Which documents are typically required when sourcing Methyldopa API?
Request the core API documentation set: USDMF (5 companies), CEP (5 companies), CoA (4 companies), WC (3 companies), FDA (3 companies). Confirm versions and validity dates match the destination market to avoid delays in qualification.
Which manufacturers are known to produce Methyldopa API?
Known or reported manufacturers for Methyldopa: Arshine Pharmaceutical Co., Limited, Apollo Healthcare Resources (Singapore), LGM Pharma. Evaluate their GMP history, scale, and regional coverage before requesting dossiers or allocating demand.
How can I request quotes for Methyldopa API from GMP suppliers?
Submit quote requests through the supplier listings with your specs and required documents (specifications, target volume, delivery timeline, and destination). Providing consistent details upfront speeds comparable offers and clarifies technical feasibility.
Is a GMP audit report available for Methyldopa manufacturers?
Audit reports may be requested for Methyldopa: 0 GMP audit reports available. Confirm the scope and recency of any audit before relying on it for qualification decisions.
How many suppliers offer Methyldopa API on Pharmaoffer?
Reported supplier count for Methyldopa: 5 verified suppliers. Filter listings by certifications, regions, and delivery options to match your qualification plan.
Which countries are known to manufacture Methyldopa API?
Production countries reported for Methyldopa: China (3 producers), Singapore (1 producer). Knowing the manufacturing geography helps anticipate logistics lead times and import compliance needs.
Which certifications do suppliers of Methyldopa usually hold?
Common certifications for Methyldopa suppliers: USDMF (5 companies), CEP (5 companies), CoA (4 companies), WC (3 companies), FDA (3 companies). Always verify issuing authorities and expiry dates when reviewing audit packages.
Technical
What is Methyldopa (CAS 555-30-6) used for?
Methyldopa is used to manage hypertension, either alone or with hydrochlorothiazide. It is commonly selected for pregnant patients and individuals with renal impairment. An intravenous form is available when oral dosing is not possible or for hypertensive crises.
Which therapeutic class does Methyldopa fall into?
Methyldopa belongs to the following therapeutic categories: Adrenergic Agents, Adrenergic Agonists, Adrenergic alpha-2 Receptor Agonists, Adrenergic alpha-Agonists, Agents Causing Muscle Toxicity. This positioning helps teams compare alternative APIs, anticipate pharmacology expectations, and align early research priorities.
What conditions is Methyldopa mainly prescribed for?
The primary indications for Methyldopa: Methyldopa is indicated for the management of hypertension as monotherapy or in combination with hydrochlorothiazide, Methyldopa injection is used to manage hypertensive crises. These use cases frame the target patient populations and help prioritize formulation and safety evaluations.
How does Methyldopa work?
The exact mechanism of Methyldopa is not fully elucidated; however, the main mechanisms of Methyldopa involve its actions on alpha-adrenergic receptor and the aromatic L-amino acid decarboxylase enzyme, to a lesser extent. The sympathetic outflow is regulated by alpha (α)-2 adrenergic receptors and imidazoline receptors expressed on adrenergic neurons within the rostral ventrolateral medulla.Methyldopa is metabolized to α‐methylnorepinephrine via dopamine beta-hydroxylase activity and, consequently, alpha-methylepinephrine via phenylethanolamine-N-methyltransferase activity.Mediating the therapeutic effects of Methyldopa, α‐methylnorepinephrine and α-methylepinephrine active metabolites are agonists at presynaptic alpha-2 adrenergic receptors in the brainstem. Stimulating alpha-2 adrenergic receptors results in the inhibition of adrenergic neuronal outflow and attenuation of norepinephrine release in the brainstem. Consequently, the output of vasoconstrictor adrenergic signals to the peripheral sympathetic nervous system is reduced, leading to a reduction in blood pressure.
The L-isomer of alpha-Methyldopa also reduces blood pressure by inhibiting aromatic L-amino acid decarboxylase, also known as DOPA decarboxylase, which is an enzyme responsible for the syntheses of dopamine and serotonin.Inhibiting this enzyme leads to depletion of biogenic amines such as norepinephrine. However, inhibition of aromatic L-amino acid decarboxylase plays a minimal role in the blood-pressure‐lowering effect of Methyldopa.
What should someone know about the safety or toxicity profile of Methyldopa?
Methyldopa shows low acute oral toxicity in animals, but systemic exposure through parenteral routes is more toxic, as reflected by lower intraperitoneal LD50 values. Acute overexposure may cause central nervous system and gastrointestinal effects with cardiovascular depression. Clinically, sedation, dizziness, and rare hepatic or hematologic reactions are known safety considerations, and excessive neurotransmitter depletion can contribute to tolerability limits. Controls to prevent high systemic uptake are important, particularly when non‑oral exposure is possible.
What are important formulation and handling considerations for Methyldopa as an API?
Important considerations include controlling moisture exposure because the solid API is hygroscopic and can degrade if not properly protected during processing and storage. Oral products are generally uncomplicated to formulate due to good aqueous solubility and no meaningful food effect on absorption. For IV preparations, pH must be tightly controlled and solutions protected from oxidation to prevent discoloration and degradation.
Is Methyldopa a small molecule?
Methyldopa is classified as a small molecule. That classification shapes process design, impurity profiling, and analytical control strategies.
Are there special stability concerns for oral Methyldopa?
Yes. Oral Methyldopa is hygroscopic‑sensitive, so the solid API requires protection from moisture during processing and storage to maintain stability. Its good aqueous solubility supports straightforward oral formulation, and no special food‑related stability issues are noted.
Regulatory
Where is Methyldopa approved or in use globally?
Methyldopa is reported as approved in the following major regions: Canada, US. Understanding geographic coverage informs regulatory filings, supply planning, and risk assessments before escalating procurement.
What’s the regulatory and patent landscape for Methyldopa right now?
Methyldopa is an established antihypertensive active ingredient with regulatory status in the United States and Canada. Its original patent protections have long expired, and it is generally available for generic use. No current region‑specific exclusivities are indicated in the provided context.
Pharmaoffer
How does Pharmaoffer’s Smart Sourcing Service help with Methyldopa procurement?
Pharmaoffer's Smart Sourcing Service coordinates compliant suppliers, documentation, and competitive quotes for Methyldopa. It centralizes outreach, follow-ups, and document validation to shorten procurement timelines.
Is Methyldopa included in the PRO Data Insights coverage?
PRO Data Insights coverage for Methyldopa: 816 verified transactions across 205 suppliers and 176 buyers worldwide. Use the dataset to benchmark suppliers and monitor regulatory activity where available.
Where can I access the API market report for Methyldopa?
Market report availability for Methyldopa: Report Available. The report highlights demand trends, pricing drivers, and supplier landscape insights for procurement planning.
