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Spironolactone | CAS No: 52-01-7 | GMP-certified suppliers
A medication that treats heart failure, hypertension, and diverse edema conditions while supporting the diagnosis and management of hyperaldosteronism to improve fluid balance and clinical stability.
Therapeutic categories
Primary indications
- Spironolactone is indicated for the treatment of the following conditions:
- NYHA Class III-IV heart failure and reduced ejection fraction to increase survival, manage edema, and reduce the need for hospitalization for heart failure
- Spironolactone is usually administered in conjunction with other heart failure therapies
Product Snapshot
- Oral small‑molecule formulation available mainly as tablets, capsules, suspensions, and limited topical forms
- Used for heart‑failure–related fluid management, hypertension add‑on therapy, edema of hepatic or renal origin, primary hyperaldosteronism, and other aldosterone‑driven conditions
- Approved in the US, Canada, and EU
Clinical Overview
Pharmacologically, spironolactone competitively inhibits aldosterone binding at mineralocorticoid receptors in the distal tubule and collecting duct. This antagonism decreases sodium reabsorption and promotes natriuresis while reducing potassium excretion. The drug increases renin and aldosterone levels through feedback mechanisms. Beyond mineralocorticoid antagonism, spironolactone and its metabolites display progestogenic and antiandrogenic effects through interaction with androgen, progesterone, and estrogen receptors. Anti‑inflammatory actions have also been described.
Absorption, metabolic pathways, and elimination profiles are dominated by extensive biotransformation to active metabolites, which contribute substantially to overall pharmacologic activity. These characteristics support once‑daily dosing in many clinical contexts, although regimen selection varies by indication and patient factors.
Safety considerations center on the risk of hyperkalemia, particularly in patients with renal impairment or those receiving concomitant agents that raise serum potassium. Endocrine‑related effects such as gynecomastia, menstrual irregularities, and breast tenderness reflect its hormonal receptor interactions. Monitoring of electrolytes and renal function is essential during therapy.
Notable global brands include long‑standing formulations introduced since its first approval in 1960. For API procurement, suppliers should provide consistent control of stereochemical integrity, impurity profiles, and particle characteristics, with documentation aligned to pharmacopeial and regulatory expectations for diuretic and hormone‑antagonist APIs.
Identification & chemistry
| Generic name | Spironolactone |
|---|---|
| Molecule type | Small molecule |
| CAS | 52-01-7 |
| UNII | 27O7W4T232 |
| DrugBank ID | DB00421 |
Pharmacology
| Summary | Spironolactone is a mineralocorticoid receptor antagonist that blocks aldosterone‑dependent sodium reabsorption and potassium secretion in the distal nephron, producing a potassium‑sparing diuretic effect. Its activity increases renin and aldosterone levels and extends to secondary targets, including androgen, progesterone, estrogen, and glucocorticoid receptors, contributing additional endocrine and anti-inflammatory actions. The drug’s pharmacodynamic profile centers on modulation of mineralocorticoid signaling, fluid balance, and select steroid receptor pathways. |
|---|---|
| Mechanism of action | Aldosterone is a key hormone in the renin-angiotensin-aldosterone system. By binding to the mineralocorticoid receptor at the distal tubules and collecting duct, it causes sodium reabsorption and potassium secretion, increases vascular stiffness and remodelling, and activates pro-inflammatory pathways. Spironolactone and its active metabolites are aldosterone antagonists that produce a potassium-sparing diuretic effect. They competitively bind to receptors at the aldosterone-dependent sodium-potassium exchange site in the distal convoluted renal tubule. Spironolactone causes increased amounts of sodium and water to be excreted while potassium is retained. Spironolactone acts both as a diuretic and as an antihypertensive drug by this mechanism. It may be given alone or with other diuretic agents that act more proximally in the renal tubule. |
| Pharmacodynamics | Spironolactone has a potassium-sparing diuretic effect. It promotes sodium and water excretion and potassium retention. It increases renin and aldosterone levels.Spironolactone is a mineralocorticoid receptor antagonist and has a low affinity for the glucocorticoid receptor.It also exhibits progestogenic and anti-androgenic actions as it binds to the androgen receptor and, to a lesser extent, estrogen and progesterone receptors.Spironolactone exhibits anti-inflammatory effects. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Mineralocorticoid receptor | Humans | antagonist |
| Glucocorticoid receptor | Humans | antagonist |
| Androgen receptor | Humans | antagonist |
ADME / PK
| Absorption | The mean time to reach peak plasma concentration of spironolactone and the active metabolite, canrenone, in healthy volunteers is 2.6 and 4.3 hours, respectively. Food increased the bioavailability of spironolactone (as measured by AUC) by approximately 95.4%. |
|---|---|
| Half-life | The mean half-life of spironolactone is 1.4 hours. The mean half-life values of its metabolites, including canrenone, TMS, and HTMS are 16.5, 13.8, and 15 hours, respectively. |
| Protein binding | Spironolactone and its metabolites are more than 90% bound to plasma proteins.Spironolactone and canrenone bind to serum albumin and alpha 1-acid glycoprotein. |
| Metabolism | Spironolactone is rapidly and extensively metabolized to form different metabolites. A group of metabolites are formed when sulfur of spironolactone is removed, such as [canrenone]. Sulfur is retained in another group of metabolites, including 7-alpha (α)-thiomethylspironolactone (TMS) and 6-beta (ß)-hydroxy-7-alpha (α)-thiomethylspirolactone (HTMS). Spironolactone is firstly deacetylated to 7-α-thiospironolactone.7-α-thiospironolactone is S-methylated to TMS, which is the primary metabolite,or dethioacetylated to canrenone.TMS and HTMS can be further metabolized. In humans, the potencies of TMS and 7-α-thiospirolactone in reversing the effects of the synthetic mineralocorticoid, fludrocortisone, on urinary electrolyte composition were approximately a third relative to spironolactone. However, since the serum concentrations of these steroids were not determined, their incomplete absorption and/or first-pass metabolism could not be ruled out as a reason for their reduced _in vivo_ activities. |
| Route of elimination | The metabolites are excreted primarily in the urine and secondarily in bile.Metabolites of spironolactone are excreted in urine (42-56%) and in the feces (14.2-14.6%). No unmetabolized spironolactone is present in the urine. |
Formulation & handling
- Low aqueous solubility (logP 3.64) requires solubility‑enhancing approaches for oral solid and suspension formulations.
- Oral administration shows a marked food effect, so development should consider consistent-with-food labeling and bioavailability variability.
- Suitable for oral and topical products as a stable solid small molecule with no special handling beyond standard protection from moisture and light.
Regulatory status
| Lifecycle | The API is in an early-to-mid lifecycle phase, supported by multiple U.S. patents expiring in 2036. With products marketed in the US, Canada, and the EU, the market remains protected from generic competition for more than a decade. |
|---|
| Markets | US, Canada, EU |
|---|
Supply Chain
| Supply chain summary | Spironolactone is an established therapy originally introduced by an originator company (historically G.D. Searle), and its supply landscape is now dominated by numerous generic manufacturers and repackagers, indicating a fully mature generic market. Branded and compounded formulations appear in the US, Canada, and EU, reflecting broad geographic availability. The compound‑specific patents listed extend to 2036, but these relate to newer formulation technologies rather than the long off‑patent active ingredient, so generic API and finished‑dose competition is already well established. |
|---|
Safety
| Toxicity | The oral LD<sub>50</sub> of spironolactone is greater than 1000 mg/kg in mice, rats, and rabbits. Acute overdosage of ALDACTONE may be manifested by drowsiness, mental confusion, maculopapular or erythematous rash, nausea, vomiting, dizziness, or diarrhea. Rarely, instances of hyponatremia, hyperkalemia,or hepatic coma may occur in patients with severe liver disease, but these are unlikely due to acute overdosage. Hyperkalemia may occur, especially in patients with impaired renal function. In case of an overdose, vomiting may be induced and gastric lavage may be instituted. As there is no specific antidote, treatment is supportive to maintain hydration, electrolyte balance, and vital functions. Patients who have renal impairment may develop hyperkalemia. In such cases, discontinue spironolactone. |
|---|
- Oral LD50 exceeds 1000 mg/kg in multiple species, indicating relatively low acute toxicity, though central nervous system effects and gastrointestinal disturbances have been observed at high exposures
- Overexposure can elicit electrolyte disturbances, including hyperkalemia, with elevated risk in the presence of renal impairment
- Rare severe responses reported in susceptible populations include hyponatremia and hepatic decompensation, reflecting the compound’s endocrine and hepatic metabolic liabilities
Spironolactone is a type of Diuretics
Diuretics, a subcategory of pharmaceutical active pharmaceutical ingredients (APIs), are compounds commonly used in the treatment of conditions such as hypertension, congestive heart failure, and edema. Diuretics, also known as water pills, function by increasing the production of urine, thereby promoting the excretion of excess water and electrolytes from the body.
There are several types of diuretics, including thiazide diuretics, loop diuretics, and potassium-sparing diuretics. Thiazide diuretics, such as hydrochlorothiazide, work by inhibiting the reabsorption of sodium and chloride in the kidneys, leading to increased urine production. Loop diuretics, such as furosemide, act on the loop of Henle in the kidneys to block the reabsorption of sodium and chloride, resulting in a more potent diuretic effect. Potassium-sparing diuretics, like spironolactone, help retain potassium in the body while still promoting diuresis.
These diuretic APIs are widely used in the pharmaceutical industry to formulate medications that effectively manage fluid retention and related conditions. They are available in various forms, including tablets, capsules, and intravenous formulations. Diuretics are often prescribed as part of combination therapies to enhance their effectiveness and minimize adverse effects.
It is important to note that the use of diuretics should be closely monitored by healthcare professionals due to potential side effects such as electrolyte imbalances, dehydration, and hypotension. Proper dosage and patient-specific considerations are crucial to ensure optimal therapeutic outcomes.
In conclusion, diuretics are a vital subcategory of pharmaceutical APIs used to treat conditions characterized by fluid retention. Their mechanisms of action vary, but they all facilitate increased urine production, assisting the body in eliminating excess fluids. The proper use of diuretics, in combination with medical supervision, can effectively manage various cardiovascular and renal conditions.
Spironolactone (Diuretics), classified under 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.
Spironolactone API manufacturers & distributors
Compare qualified Spironolactone API suppliers worldwide. We currently have 19 companies offering Spironolactone API, with manufacturing taking place in 5 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 |
| Aquatic Remedies Pvt Ltd | Producer | India | India | CoA | 35 products |
| Aurora Industry Co., Ltd | Distributor | China | China | BSE/TSE, CEP, CoA, GMP, ISO9001, MSDS, WC | 250 products |
| Caesar & Loretz GmbH (CAE... | Distributor | Germany | Unknown | BSE/TSE, CoA, GMP, ISO9001, MSDS | 211 products |
| Cerata Pharmaceuticals LL... | Producer | India | India | CoA, FDA, GMP | 34 products |
| Chr. Olesen Group | Distributor | Denmark | China | USDMF | 252 products |
| Duchefa Farma B.V. | Distributor | Netherlands | China | BSE/TSE, CoA, GMP, ISO9001, MSDS, WC | 170 products |
| G.D. Searle | Producer | United States | United States | CEP, CoA | 1 products |
| Gedeon Richter | Producer | Hungary | Unknown | CEP, CoA, FDA, GMP, USDMF | 48 products |
| Humble Healthcaare | Producer | India | India | CoA | 30 products |
| Metapharmaceutical Indust... | Producer | Spain | China | BSE/TSE, CEP, CoA, GMP, ISO14001, MSDS, WC | 21 products |
| Piramal Healthcare | Producer | United Kingdom | India | CoA, GMP | 31 products |
| Sanofi | Producer | France | Unknown | CEP, CoA, FDA, GMP, JDMF, USDMF | 93 products |
| Shaoxing Hantai Pharma | Distributor | China | China | CoA | 162 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CEP, CoA, FDA, GMP, ISO9001, MSDS, USDMF, WC | 757 products |
| Tianjin Jinjin | Producer | China | China | CEP, CoA, FDA, GMP, JDMF, USDMF | 12 products |
| Tianjin Tianmao | Producer | China | China | CoA | 6 products |
| Tianjin Tianyao | Producer | China | China | CEP, CoA, FDA, USDMF | 24 products |
| Zhejiang Shenzhou | Producer | China | China | CEP, CoA, FDA, GMP, USDMF, WC | 2 products |
When sending a request, specify which Spironolactone 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 Spironolactone 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.
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