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Amiloride | CAS No: 2609-46-3 | GMP-certified suppliers
A medication that serves as a potassium-sparing diuretic adjunct to thiazide therapy, managing hypertension and congestive heart failure by reducing potassium loss and supporting electrolyte balance.
Therapeutic categories
Primary indications
- For use as adjunctive treatment with thiazide diuretics or other kaliuretic-diuretic agents in congestive heart failure or hypertension
Product Snapshot
- Amiloride is an oral small molecule formulated primarily as film-coated tablets
- It is indicated for adjunctive treatment with thiazide diuretics or other kaliuretic-diuretic agents in congestive heart failure and hypertension
- The product is approved for use in the US and Canadian markets
Clinical Overview
Pharmacologically, amiloride functions by inhibiting sodium reabsorption in renal epithelial cells, specifically targeting the amiloride-sensitive sodium channels located on principal cells within the distal convoluted tubule and collecting duct. This inhibition reduces the electrochemical gradient that normally promotes the secretion of potassium and hydrogen ions into the tubular lumen. As a result, amiloride minimizes potassium loss typically induced by other diuretics, hence its classification as a potassium-sparing agent. Notably, amiloride's mechanism is independent of aldosterone antagonism and remains effective regardless of aldosterone presence.
Following administration, amiloride modulates sodium and water excretion, contributing to its antihypertensive and diuretic effects. Although detailed human ADME (absorption, distribution, metabolism, and excretion) profiles are limited in the provided data, the clinical use and dosing guidelines are well established based on its pharmacodynamic properties.
Safety considerations for amiloride include its potential to induce hyperkalemia, particularly when combined with other agents affecting potassium homeostasis such as ACE inhibitors or spironolactone. Patients should avoid potassium-containing salt substitutes during therapy. Monitoring of serum electrolytes is advised to mitigate the risk of electrolyte imbalances.
Amiloride was first approved for clinical use in 1967 and continues to be employed in cardiovascular therapeutics for patients requiring potassium conservation during diuretic treatment regimens. It is included in multiple drug categories such as epithelial sodium channel blockers and membrane transport modulators.
When sourcing amiloride as an active pharmaceutical ingredient, it is important to ensure compliance with pharmacopeial standards and regulatory requirements governing purity, impurity profiles, and batch-to-batch consistency. Supplier qualification and robust quality control measures are critical to maintain safety and efficacy in finished pharmaceutical products.
Identification & chemistry
| Generic name | Amiloride |
|---|---|
| Molecule type | Small molecule |
| CAS | 2609-46-3 |
| UNII | 7DZO8EB0Z3 |
| DrugBank ID | DB00594 |
Pharmacology
| Summary | Amiloride is a potassium-sparing diuretic that inhibits sodium reabsorption by blocking amiloride-sensitive sodium channels in the distal convoluted tubules and collecting ducts of the kidney. This action reduces sodium and water retention while minimizing potassium loss, independent of aldosterone activity. It is primarily used as an adjunct to other diuretics for managing hypertension and congestive heart failure. |
|---|---|
| Mechanism of action | Amiloride works by inhibiting sodium reabsorption in the distal convoluted tubules and collecting ducts in the kidneys by binding to the amiloride-sensitive sodium channels. This promotes the loss of sodium and water from the body, but without depleting potassium. Amiloride exerts its potassium sparing effect through the inhibition of sodium reabsorption at the distal convoluted tubule, cortical collecting tubule and collecting duct; this decreases the net negative potential of the tubular lumen and reduces both potassium and hydrogen secretion and their subsequent excretion. Amiloride is not an aldosterone antagonist and its effects are seen even in the absence of aldosterone. |
| Pharmacodynamics | Amiloride, an antikaliuretic-diuretic agent, is a pyrazine-carbonyl-guanidine that is unrelated chemically to other known antikaliuretic or diuretic agents. It is an antihypertensive, potassium-sparing diuretic that was first approved for use in 1967 and helps to treat hypertension and congestive heart failure. The drug is often used in conjunction with thiazide or loop diuretics. Due to its potassium-sparing capacities, hyperkalemia (high blood potassium levels) are occasionally observed in patients taking amiloride. The risk is high in concurrent use of ACE inhibitors or spironolactone. Patients are also advised not to use potassium-containing salt replacements. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Amiloride-sensitive sodium channel subunit alpha | Humans | inhibitor |
| Amiloride-sensitive sodium channel subunit beta | Humans | inhibitor |
| Amiloride-sensitive sodium channel subunit gamma | Humans | inhibitor |
ADME / PK
| Absorption | Readily absorbed following oral administration. |
|---|---|
| Half-life | Plasma half-life varies from 6 to 9 hours. |
| Metabolism | Amiloride is not metabolized by the liver but is excreted unchanged by the kidneys. |
| Route of elimination | Amiloride HCl is not metabolized by the liver but is excreted unchanged by the kidneys. About 50 percent of a 20 mg dose of amiloride HCl is excreted in the urine and 40 percent in the stool within 72 hours. |
Formulation & handling
- Amiloride is a small molecule suitable for oral tablet formulations with moderate water solubility and low lipophilicity.
- The compound requires administration with food to reduce gastrointestinal irritation and to minimize variability in absorption.
- Careful attention is needed to avoid use with potassium-containing products and natural licorice due to potential drug-nutrient interactions.
Regulatory status
| Lifecycle | The API is currently off-patent in both the US and Canada, with generic versions available and established market presence. Products containing the API are in the mature phase of their lifecycle in these regions. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Amiloride is manufactured by multiple companies specializing in generic drug production, with no evident originator brand dominating the marketplace. Its products are primarily available in North American markets, specifically the US and Canada. The absence of distinct branded products and the presence of various generic manufacturers suggest a mature market with existing generic competition post-patent expiry. |
|---|
Safety
| Toxicity | No data are available in regard to overdosage in humans. The oral LD<sub>50</sub> of amiloride hydrochloride (calculated as the base) is 56 mg/kg in mice and 36 to 85 mg/kg in rats, depending on the strain. The most likely signs and symptoms to be expected with overdosage are dehydration and electrolyte imbalance. |
|---|
- Handle with caution due to potential toxicity
- Oral LDâ‚…â‚€ ranges from 36 to 85 mg/kg in rodent models
- Overexposure may result in dehydration and electrolyte disturbances
Amiloride 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.
Amiloride (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.
Amiloride API manufacturers & distributors
Compare qualified Amiloride API suppliers worldwide. We currently have 4 companies offering Amiloride API, with manufacturing taking place in 4 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 |
|---|---|---|---|---|---|
| Anphar Labs. | Producer | India | India | CoA, WC | 5 products |
| Bioindustria | Producer | Italy | Italy | CEP, CoA, FDA, GMP | 12 products |
| Cambrex | Producer | Italy | Unknown | CoA, USDMF | 104 products |
| Veeprho Group | Producer | Czech Republic | Czech Republic | CoA | 138 products |
When sending a request, specify which Amiloride 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 Amiloride 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.
