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Chlorthalidone | CAS No: 77-36-1 | GMP-certified suppliers
A medication that supports hypertension management and helps reduce edema associated with heart failure, hepatic cirrhosis, corticosteroid therapy, and various renal disorders for broad clinical use.
Therapeutic categories
Primary indications
- Chlorthalidone is indicated in the management of hypertension either as the sole therapeutic agent or to enhance the effect of other antihypertensive drugs in the more severe forms of hypertension
- Chlorthalidone is indicated as adjunctive therapy in edema associated with congestive heart failure, hepatic cirrhosis, and corticosteroid and estrogen therapy
- Chlorthalidone has also been found useful in edema due to various forms of renal dysfunction, such as nephrotic syndrome, acute glomerulonephritis, and chronic renal failure
Product Snapshot
- Oral small‑molecule formulation supplied as various coated and film‑coated tablets
- Primary uses include hypertension management and adjunctive control of edema linked to cardiac, hepatic, or renal conditions
- Approved in the US and Canada for commercial supply
Clinical Overview
Its pharmacologic activity results from inhibition of the sodium‑chloride symporter in the cortical diluting segment of the distal nephron. Blockade of this transporter reduces sodium and chloride reabsorption, producing an osmotic diuresis that lowers extracellular fluid and plasma volume. Secondary increases in sodium delivery to the distal tubule enhance potassium excretion through sodium‑potassium exchange. The reduction in intravascular volume contributes to decreased cardiac output and blood pressure, though the full mechanism underlying sustained antihypertensive effects remains debated.
Chlorthalidone displays additional in vitro actions including reduced platelet aggregation and vascular permeability and promotion of angiogenesis, which may reflect modulation of carbonic anhydrase–dependent pathways. These pleiotropic effects are not fully characterized clinically but are notable within its pharmacologic profile.
Absorption is gradual, and the compound has a long elimination half‑life due to extensive erythrocyte binding, supporting once‑daily dosing in clinical practice. Renal excretion is the primary elimination pathway. Photosensitivity and electrolyte disturbances, particularly hypokalemia, hyponatremia, and hypomagnesemia, represent key safety considerations. Volume depletion, reduced glomerular filtration, and hyperuricemia may occur, especially at higher doses or in susceptible populations. Chlorthalidone should be used cautiously in patients with severe renal impairment or concurrent medications that affect electrolyte balance.
Chlorthalidone is marketed in several regions, with Hygroton being a commonly referenced brand. For API procurement, suppliers should provide evidence of impurity control consistent with pharmacopeial standards, stable polymorphic form, and validated processes ensuring reproducible potency and particle characteristics suitable for solid oral formulations.
Identification & chemistry
| Generic name | Chlorthalidone |
|---|---|
| Molecule type | Small molecule |
| CAS | 77-36-1 |
| UNII | Q0MQD1073Q |
| DrugBank ID | DB00310 |
Pharmacology
| Summary | Chlorthalidone inhibits the Na+/Cl− symporter in the cortical diluting segment of the nephron, reducing sodium and chloride reabsorption and producing a sodium‑driven diuresis. The resulting shifts in extracellular fluid volume contribute to its antihypertensive effects and increase distal sodium delivery, which promotes potassium excretion. It also interacts with carbonic anhydrase pathways, which may influence vascular permeability, platelet activity, and other cardiovascular pharmacodynamic features. |
|---|---|
| Mechanism of action | Chlorthalidone prevents reabsorption of sodium and chloride through inhibition of the Na+/Cl- symporter in the cortical diluting segment of the ascending limb of the loop of Henle.Reduction of sodium reabsorption subsequently reduces extracellular fluid and plasma volume via an osmotic, sodium-driven diuresis. By increasing the delivery of sodium to the distal renal tubule, Chlorthalidone indirectly increases potassium excretion via the sodium-potassium exchange mechanism. The exact mechanism of chlorthalidone's anti-hypertensive effect is under debate, however, it is thought that increased diuresis results in decreased plasma and extracellular fluid volume which therefore requires decreased cardiac output and overall lowers blood pressure.Chlorthalidone has also been shown to decrease platelet aggregation and vascular permeability, as well as promote angiogenesis in vitro, which is thought to be partly the result of reductions in carbonic anhydrase–dependent pathways. These pathways may play a role in chlorthalidone's cardiovascular risk reduction effects. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Carbonic anhydrase 1 | Humans | inhibitor |
| Solute carrier family 12 member 1 | Humans | inhibitor |
ADME / PK
| Half-life | 40-50 hours[FDA Label, A176327] |
|---|---|
| Protein binding | Approximately 75 percent of the drug is bound to plasma proteins, 58 percent of the drug being bound to albumin.[FDA Label] This is caused by an increased affinity of the drug to erythrocyte carbonic anhydrase. |
| Metabolism | Liver |
| Route of elimination | Approximately 50% of the administered dose is excreted unmetabolized through the kidney, and excretion is characterized by biphasic elimination with a rapid phase followed by a slow secretory phase. |
| Volume of distribution | Chlorthalidone has been shown to rapidly concentrate within erythrocytes and subsequently equilibrate via a slow diffusion back into the serum compartment, resulting in a large volume of distribution. |
Formulation & handling
- Oral small‑molecule diuretic typically formulated as solid tablets; low aqueous solubility may require disintegrant optimization to ensure reliable dissolution.
- Food increases bioavailability, so formulations should account for potential food‑dependent absorption variability.
- Chemically stable isoindolone solid; standard moisture control is generally sufficient during manufacture and storage.
Regulatory status
| Lifecycle | The API remains partly protected in the United States due to later‑expiring patents extending through 2031, despite several patents ending in 2025–2028. With sales in the United States and Canada, the market reflects a mature presence but continued U.S. patent coverage may limit full generic entry until the final expiry. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Chlorthalidone is supplied by numerous generic manufacturers and packagers, with no single originator dominating the current landscape, reflecting its long‑established use. Branded and generic products are widely available in North America, with noted markets in the United States and Canada. Existing U.S. patents extend into 2025–2031, but the presence of many active manufacturers indicates that core drug substance patents have already expired and generic competition is well established; remaining patents likely relate to specific formulations or combinations. |
|---|
Chlorthalidone 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.
Chlorthalidone (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.
Chlorthalidone API manufacturers & distributors
Compare qualified Chlorthalidone API suppliers worldwide. We currently have 10 companies offering Chlorthalidone 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 |
|---|---|---|---|---|---|
| AXXO GmbH | Distributor | Germany | World | CoA, GMP, GDP, MSDS, USDMF | 243 products |
| Chromo Labs. | Producer | India | India | CoA, USDMF | 11 products |
| Curia | Producer | United States | Italy | CEP, CoA, GMP, MSDS, USDMF | 106 products |
| Euticals | Producer | Italy | Unknown | CEP, CoA, FDA, GMP, USDMF | 48 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| Ipca Labs. | Producer | India | Unknown | CEP, CoA, FDA, GMP, KDMF, USDMF, WC | 69 products |
| Maithri Drugs | Producer | India | India | CEP, CoA, GMP, USDMF | 12 products |
| Menadiona, S.L. | Producer | Spain | Spain | CEP, CoA, GMP, ISO9001, MSDS, USDMF, WHO-GMP | 15 products |
| Mylan | Producer | India | India | CoA, USDMF | 201 products |
| Unichem Labs. | Producer | India | India | CoA, USDMF | 62 products |
When sending a request, specify which Chlorthalidone 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 Chlorthalidone 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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