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Benidipine | CAS No: 105979-17-7 | GMP-certified suppliers
A medication that effectively manages hypertension, renoparenchymal hypertension, and angina pectoris by providing sustained cardiovascular and renal benefits with a favorable safety profile.
Therapeutic categories
Primary indications
- Benidipine is a potent and long-lasting drug indicated for the treatment of cardiovascular diseases such as hypertension, renoparenchymal hypertension and angina pectoris
Product Snapshot
- Benidipine is an oral small molecule formulation available in film-coated tablet form
- It is primarily indicated for cardiovascular conditions including hypertension, renoparenchymal hypertension, and angina pectoris
- The compound is currently in the experimental stage and lacks approval from major regulatory agencies
Clinical Overview
Benidipine is indicated for the management of cardiovascular disorders, primarily hypertension, renoparenchymal hypertension, and angina pectoris. Its clinical utility stems from potent and sustained reductions in both systolic and diastolic blood pressure accompanied by a decrease in heart rate. Additionally, benidipine has been observed to reduce urinary protein excretion and serum triglyceride levels, providing potential renal and lipid profile benefits.
Pharmacologically, benidipine acts as a tri-type calcium channel blocker by inhibiting L-, N-, and T-type calcium channels. This broad blockade is associated with its long-lasting activity, attributed to a high affinity for dihydropyridine binding sites within cell membranes. Its vascular selectivity is notable, predominantly affecting peripheral blood vessels, which contributes to its antihypertensive action.
Beyond hemodynamic effects, benidipine demonstrates antioxidative properties and promotes nitric oxide production, which collectively contribute to cardioprotective and anti-atherosclerotic effects. It also suppresses the expression of adhesion molecules and inhibits proliferation of vascular smooth muscle and mesangial cells. Stimulation of osteoblast differentiation has been reported, indicating potential benefits beyond cardiovascular systems.
Benidipine is metabolized primarily through cytochrome P450 enzymes, including CYP3A4 and CYP3A5, and is both a substrate and moderate inhibitor of these isoforms. This necessitates caution when co-administered with other agents affecting CYP3A activity due to potential drug-drug interactions. As a calcium channel blocker, benidipine carries risks consistent with this class, including bradycardia and hyperkalemia, and has been categorized as a moderate risk agent for QTc interval prolongation.
For API sourcing, stringent quality control is essential to ensure chemical purity, consistent polymorphic form, and absence of related impurities. Given its pharmacological potency and CYP-mediated metabolism, suppliers should provide comprehensive documentation on manufacturing processes, batch-to-batch consistency, and stability profiles to meet global regulatory standards.
Identification & chemistry
| Generic name | Benidipine |
|---|---|
| Molecule type | Small molecule |
| CAS | 105979-17-7 |
| UNII | 4G9T91JS7E |
| DrugBank ID | DB09231 |
Pharmacology
| Summary | Benidipine is a long-acting calcium channel blocker targeting L-, N-, and T-type voltage-dependent calcium channels with vascular selectivity for peripheral blood vessels. Its pharmacodynamic profile includes blood pressure reduction, decreased heart rate, and modulation of nitric oxide production, contributing to cardioprotective and anti-atherosclerotic effects. Additional actions involve antioxidative activity, suppression of vascular smooth muscle cell proliferation, and renal protective effects. |
|---|---|
| Mechanism of action | Benidipine is a tripe calcium channel inhibitor by inhibiting L, N and T type calcium channel. It presents a very long-lasting activity that can be explained by its high affinity for cell membranes from the DHP binding site; this characteristic indicated a long-lasting pharmacological activity of benidipine. The additional property of benidipine is the vascular selectivity towards peripheral blood vessels. |
| Pharmacodynamics | Benidipine reduces systolic and diastolic blood pressure as well as to present decreases in heart rate pulse after treatment. It is reported also a decrease urinary protein excretion and serum triglycerides. Different studies have shown benidipine anti-oxidative activity, stimulation of NO production, suppression of adhesion molecules expression, stimulation of osteoblast differentiation, suppression of the proliferation of vascular smooth muscle cells and mesangial cells, as well as myocardial protection. The enhancement of NO production is associated with the cardioprotective and antiartheriosclerotic effects of benidipine. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Voltage-dependent L-type calcium channel | Humans | antagonist |
| Voltage-dependent N-type calcium channel subunit alpha-1B | Humans | antagonist |
| Voltage-dependent T-type calcium channel | Humans | antagonist |
ADME / PK
| Absorption | Benidipine is rapidly absorbed after oral administration reaching a maximum concentration within 2 hours. The short period of time needed for maximum concentration to get reached is a particular characteristic of benidipine when compared with other calcium channel blockers. The registered maximum concentration and AUC are dose-dependent and it can go from 0.55-3.89 ng/ml and 1.04-6.7 ng.h/ml respectively when administered in a dose of 2-8 mg. |
|---|---|
| Half-life | The elimination half-life of benidipine is registered to be of approximate 1 hour. |
| Protein binding | Benidipine is highly bound to plasma proteins and the bound form can account for even 98% of the administered dose. |
| Metabolism | Benidipine is almost completely metabolized in the liver. From different reports, it is thought that benidipine is mainly metabolized by CYP3A. Some of the formed metabolites are N-desbenzylbenidipine and dehydrobenidipine. Analysis on the formation of metabolites has indicated that the metabolism is mainly performed by CYP3A4 and CYP3A5. |
| Route of elimination | The percentage of urinary excretion after oral administration is of approximate 36% of the administered dose. Most of the remaining dose is excreted in feces, making bile excretion the major elimination pathway of benidipine. From the eliminated drug, none of it is expressed in the form of the unchanged drug. |
| Volume of distribution | Benidipine is highly distributed to the tissues mainly in the liver and kidneys and plasma. It does not present a high accumulation following repeated oral administrations. |
Formulation & handling
- Benidipine is a lipophilic, poorly water-soluble small molecule typically formulated for oral administration as film-coated tablets.
- The solid form of Benidipine requires formulation strategies addressing low aqueous solubility to enhance bioavailability.
- Handling considerations should include protection from moisture due to low water solubility but no specific peptide or biologic instability concerns apply.
Regulatory status
Safety
| Toxicity | In preclinical studies, the LD50 of benidipine ranged from 87-384 mg/kg which is more than 100 times the needed dose to achieve anti-hypertensive action. There were no significant changes in histopathological heart examination. Benidipine showed no carcinogenic, antigenicity, teratogenic or mutagenic properties. |
|---|
- Benidipine exhibits low acute toxicity with an LD50 range of 87-384 mg/kg in preclinical studies
- No evidence of carcinogenicity, antigenicity, teratogenicity, or mutagenicity was observed
- Histopathological evaluation revealed no significant cardiac tissue alterations at tested doses
Benidipine 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.
Benidipine (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.
Benidipine API manufacturers & distributors
Compare qualified Benidipine API suppliers worldwide. We currently have 3 companies offering Benidipine API, with manufacturing taking place in 2 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 |
|---|---|---|---|---|---|
| Ildong Pharmaceutical | Producer | South Korea | South Korea | CoA, JDMF | 4 products |
| Lusochimica | Producer | Italy | Italy | CoA, JDMF | 23 products |
| Recordati S.p.A. | Producer | Italy | Italy | CoA, JDMF | 18 products |
When sending a request, specify which Benidipine 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 Benidipine 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.
