Benidipine

Benidipine is an antihypertensive agent belonging to Calcium channel blocker.

Benidipine is a dihydropyridine calcium channel blocker indicated for the management of hypertension and angina pectoris.

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. Benidipine is highly bound to plasma proteins and the bound form can account for even 98% of the administered dose. 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. 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.

Benidipine shows common side effects like Headache, Dizziness, Constipation, Skin rash, Decreased blood pressure, Nausea Light-headedness, Palpitations, edema, etc.

Benidipine is available in the form of Oral tablets.

Benidipine is available in India, US, UK, Ireland, Europe, China and Japan.

Benidipine belonging to the Calcium channel blocker act as an antihypertensive agent.

Benidipine is a triple calcium channel inhibitor by inhibiting L, N, and T-type calcium channels. 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.

The data on the Onset of action and Duration of Action of Benidipine is not available.

The Tmax was found within 2 hours following the administration of Benidipine.

Binedipine is available in the form of Oral Tablet.

Binedipine Tablet and take orally usually once or two times a day.

It is a long-acting calcium channel blocker class of medicine which are used to treat hypertension. By blocking the influx of Calcium ions through voltage-gated L-type Ca channels to the peripheral vascular smooth muscle cells, coronary smooth muscle cells and the myocardial cells causes dilatation of vascular endothelium, decrease peripheral resistance and reduce myocardial oxygen demand. It markedly relaxes arterioles and milder effects on veins, decrease afterload, and increase cardiac index.

Benidipine is an antihypertensive agent. Benidipine is a calcium channel blocker. Large vessel stiffness is one of the leading causes of elevated blood pressure in individuals. As a result, Benidipine is used to decrease blood pressure by relaxing the blood vessels. Benidipine is also used to alter the heart rate, which will reduce chest pain by allowing more blood to flow to the heart muscle.

Benidipine is approved for use in the following clinical indications

• Hypertension

Benidipine is a medicine that is used for the management of hypertension (high blood pressure).

• Angina pectoris

Benidipine is used for the treatment of angina pectoris (a type of chest pain caused by reduced blood flow to the heart). It promotes the relaxation of blood vessels which decreases blood pressure and strain on the heart.

• Hypertension

Adult: 2-4 mg once daily increased to 8 mg once daily, if necessary.

• Angina pectoris
• Adult: 4 mg twice daily.

Benidipine is available in the form of Oral Tablet.

Grapefruit is not recommended to consume while taking Benidipine. It may lead to more severe side effects such as headache, dizziness, and swelling.

Benidipine is contraindicated in patients with

● Allergies to compounds of Benidipine

● Liver impairment: Make appropriate adjustments in dosage or find alternatives if suffering from liver-related issues

● Hypotension: May cause a lowering of blood pressure for those already suffering from low blood pressure.

• Hypotension or cardiogenic shock

Benidipine is not recommended for use when you have low blood pressure or cardiogenic shock (a life-threatening condition where your heart abruptly stops pumping blood). Using this medicine will further decrease your heart’s ability to pump blood and reduce your blood pressure and heart rate drastically.

• Liver disease

Benidipine should be used with caution if you have liver problems due to the increased risk of severe side effects. This medicine is broken down and absorbed in the liver. If you take this medicine while you have pre-existing liver problems, it may worsen your condition further

• Coronary artery disease

Benidipine should be used with extreme caution if you have coronary artery disease (a condition where the blood vessels of your heart are damaged). This medicine may weaken the contractions of your heart and slow down the heart rate which may worsen the condition and lead to other serious consequences.

Avoid consumption of alcohol along with Benidipine to avoid unpleasant side effects like light-headedness, dizziness, and drowsiness.

Benidipine is not recommended to be used if you are breastfeeding as it may harm your infant.

Benidipine is not recommended to be used in pregnancy as it may cause harm to your developing fetus

Consumption of grapefruit juice is not recommended during treatment with Benidipine as it can increase the absorption of this medicine. This could lead to excessive lowering of blood pressure or worsen side effects.

• Palpitation, facial flushing, hot flushes, chest pressure sensation, headache, dizziness, sleepiness, constipation, nausea, abdominal discomfort, oedema, malaise, tinnitus, redness and warm feeling in the fingers, shoulder stiffness, increased frequency of micturition. Hypersensitive reactions e.g. rash and itching. Elevation of SGOT, SGPT, alkaline phosphatase, total bilirubin, creatinine, and uric acid.

● Beta-blockers: Potentiate the antihypertensive effect of Benidipine

● Diuretics: Potentiate the antihypertensive effect of Benidipine

● Digoxin: It can increase the serum concentration of Digoxin

● Cimetidine: Inhibit the metabolism of Benidipine

The common side effect of Benidipine include the following

• Headache, Dizziness, Constipation, Skin rash, Decreased blood pressure, Nausea Light-headedness, Palpitations, edema.

• Pregnancy

Pregnancy Category

Benidipine is not recommended to be used in pregnancy as it may cause harm to your developing foetus.

• Nursing Mothers

Benidipine is not recommended to be used if you are breastfeeding as it may harm your infant

• Pediatric Use

Benidipine is not recommended for use in children below 18 years of age as the safety and efficacy of the use of this medicine are not clinically established

• Geriatric Use

Benidipine should be used with caution in old people due to the increased risk of very low blood pressure. Blood pressure needs to be monitored regularly while using this medicine. start the treatment at low doses and increase the dose based on the response.

Information is not available.

Pharmacodynamic

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 anti-atherosclerotic effects of benidipine.

Pharmacokinetics

• 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.

• Distribution

Benidipine is highly bound to plasma proteins and the bound form can account for even 98% of the administered dose.

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.

• Metabolism and Excretion

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.

• https://www.mims.com/india/drug/info/benidipine?type=full&mtype=generic#atc-class
• https://go.drugbank.com/drugs/DB09231
• https://www.practo.com/medicine-info/benidipine-2046-api
• https://www.lybrate.com/medicine/benidipine
• https://pharmeasy.in/molecules/benidipine-129#precautionsAndWarnings