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Nilvadipine | CAS No: 75530-68-6 | GMP-certified suppliers
A medication that manages hypertension, vasospastic angina, and chronic stable angina through vascular smooth muscle relaxation and coronary artery dilation.
Therapeutic categories
Primary indications
- For the management of vasospastic angina, chronic stable angina and hypertension
Product Snapshot
- Nilvadipine is available as an oral extended-release capsule formulation
- It is indicated for the management of vasospastic angina, chronic stable angina, and hypertension
- The product is approved in certain markets and also under investigational status in others
Clinical Overview
Pharmacologically, nilvadipine functions by selectively inhibiting the influx of extracellular calcium ions through voltage-gated L-type calcium channels located in myocardial and vascular smooth muscle membranes. This blockade reduces intracellular calcium concentration, leading to relaxation of vascular smooth muscle and consequent vasodilation. The resultant decrease in total peripheral resistance lowers systemic blood pressure and myocardial oxygen demand while improving oxygen supply through coronary artery dilation.
Key absorption, distribution, metabolism, and excretion (ADME) parameters for nilvadipine include hepatic metabolism primarily via cytochrome P450 enzymes, notably CYP3A4, with moderate inhibitory effects on CYP450 isoforms including CYP2A6, CYP2C8, CYP2C19, and CYP3A4. This metabolism profile necessitates careful consideration of drug-drug interactions. Nilvadipine has a moderate risk for QTc interval prolongation, which should be monitored clinically. Its bradycardic and hypotensive effects require attention in patients with compromised cardiac function or conduction abnormalities.
Safety considerations include potential adverse effects common to calcium channel blockers such as hypotension, peripheral edema, headache, and reflex tachycardia. Given its pharmacological profile, nilvadipine should be used cautiously in patients with significant hepatic impairment or those on concomitant CYP450-modulating agents.
Nilvadipine is marketed under various brand names globally and is approved in multiple regulatory contexts for cardiovascular indications. When procuring nilvadipine API, manufacturers and suppliers should ensure compliance with pharmacopeial standards for purity, residual solvents, and polymorphic form due to its influence on bioavailability and stability. Quality management should include verification of certificate of analysis (CoA), consistent batch-to-batch reproducibility, and adherence to regulatory guidelines within intended markets.
Identification & chemistry
| Generic name | Nilvadipine |
|---|---|
| Molecule type | Small molecule |
| CAS | 75530-68-6 |
| UNII | 0214FUT37J |
| DrugBank ID | DB06712 |
Pharmacology
| Summary | Nilvadipine is a dihydropyridine calcium channel blocker that inhibits the influx of extracellular calcium through voltage-dependent L-type and T-type calcium channels. This action reduces intracellular calcium levels in vascular smooth muscle cells, leading to arterial vasodilation, decreased systemic vascular resistance, and lowered blood pressure. It is primarily indicated for the management of vasospastic angina, chronic stable angina, and hypertension. |
|---|---|
| Mechanism of action | Nilvadipine inhibits the influx of extracellular calcium through myocardial and vascular membrane pores by physically plugging the channel. The decrease in intracellular calcium inhibits the contractile processes of smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload. |
| Pharmacodynamics | Nilvadipine is similar to other dihydropyridines including amlodipine, felodipine, isradipine, and nicardipine. Nilvadipine is used to treat Prinzmetal's angina, hypertension, and other vascular disorders such as Raynaud's phenomenon. By blocking the calcium channels, Nifedipine inhibits the spasm of the coronary artery and dilates the systemic arteries, results in a increase of myocardial oxygen supply and a decrease in systemic blood pressure. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Voltage-dependent L-type calcium channel subunit alpha-1C | Humans | inhibitor |
| Voltage-dependent calcium channel subunit alpha-2/delta-1 | Humans | inhibitor |
| Voltage-dependent L-type calcium channel subunit beta-2 | Humans | inhibitor |
Formulation & handling
- Nilvadipine is a small molecule suitable for oral administration, typically formulated as extended-release capsules.
- The compound exhibits low water solubility, which may require formulation strategies to enhance bioavailability.
- Nilvadipine shows no significant food interaction, allowing flexible dosing relative to meals.
Regulatory status
Nilvadipine is a type of Calcium Channel Blockers
Calcium channel blockers (CCBs) are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) widely used in the treatment of various cardiovascular conditions. CCBs work by blocking the influx of calcium ions into smooth muscle cells and cardiac muscle cells, leading to vasodilation and reduced cardiac contractility.
CCBs are commonly prescribed to manage hypertension (high blood pressure), angina (chest pain), and certain arrhythmias (irregular heart rhythms). They are also effective in treating Raynaud's disease and migraine headaches. These medications exert their therapeutic effects by selectively inhibiting L-type calcium channels in the heart and blood vessels.
By blocking calcium channels, CCBs help relax and widen blood vessels, reducing peripheral resistance and improving blood flow. This mechanism of action lowers blood pressure, relieves angina symptoms, and helps prevent certain types of abnormal heart rhythms.
Some well-known CCBs include amlodipine, nifedipine, diltiazem, and verapamil. These medications are available in various formulations, including immediate-release and extended-release tablets, as well as injectable solutions.
It's important to note that CCBs may cause certain side effects, such as dizziness, headache, flushing, and ankle swelling. They may also interact with other medications, so it's crucial to consult a healthcare professional before starting or changing any CCB therapy.
In summary, Calcium channel blockers are a subcategory of cardiovascular medications that inhibit calcium channels, resulting in vasodilation, decreased cardiac contractility, and overall therapeutic effects in conditions such as hypertension, angina, and arrhythmias. Proper medical supervision and individualized treatment plans are essential for optimizing the use of CCBs.
Nilvadipine (Calcium Channel Blockers), 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.
Nilvadipine API manufacturers & distributors
Compare qualified Nilvadipine API suppliers worldwide. We currently have 1 companies offering Nilvadipine API, with manufacturing taking place in 1 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 |
|---|---|---|---|---|---|
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
When sending a request, specify which Nilvadipine 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 Nilvadipine 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.
