Efonidipine

Efonidipine is a Dihydropyridine belonging to the calcium channel blocker

Efonidipine is used in the symptomatic treatment of high blood pressure. It is also used in the treatment of angina pectoris.

The absorption ratio of radioactivity estimated from the sum of biliary and urinary excretions was found to be approximately 62%. The radioactivity was high in the gastrointestinal tract and liver, followed by the adrenal glands, suggesting high rates of metabolism in these regions. Efonidipine is mainly metabolized in the liver. Its metabolites are N-dephenylated Efonidipine (DPH), deaminated efonidipine (AL), and N-debenzylated Efonidipine (DBZ). Both metabolites behave as calcium antagonists. Efonidipine is also referred to as NZ-105 and has been found to be mainly eliminated by the biliary system.

The Tmax of Efonidipine was about 1.50-3.67 hours, and Cmax was about 9.66-66.91 ng/ml.

The common side effects are dizziness, drowsiness, headache, weakness, Nausea, strong irregular heartbeat, swelling, and dizziness upon standing.

Efonidipine is available in dosage forms, such as tablets.

Efonidipine is available in Europe, Japan, China, the USA, and India.

Efonidipine is a calcium channel blocker. It regulates blood pressure by relaxing the blood vessels and reducing the pressure on them, thereby making it easier for the heart to pump more blood throughout the body. In this way, it normalizes the blood pressure in patients with high blood pressure.

Efonidipine is available in the form of dosage forms, such as tablets.

Efonidipine tablets were taken orally with or without food.

Efonidipine is used in the symptomatic treatment of high blood pressure. It is also used in the treatment of angina pectoris.

Efonidipine is used to cure high blood pressure, also known as hypertension. The active constituent of this medicine belongs to the class of calcium channel-blocking agents. It reduces blood pressure by blocking the calcium channels, thus relaxing the blood vessels. This medication also works by reducing the pressure on blood vessels to make it for the heart to pump more blood in the body.

Efonidipine is approved for its use in the following clinical indications:

Hypertension

This medicine is used in the treatment of hypertension which is an elevation of the blood pressure caused by genetic and/or environmental factors.

Angina Pectoris

This medicine is used in the treatment of Angina Pectoris, which is a type of heart disease characterized by chest pain caused due to emotional stress and smoking.

Efonidipine is available in various dosage strengths: 20mg and 40mg.

Efonidipine is available in the form of dosage forms, such as tablets, injection.

Efonidipine is approved for the treatment of Angina pectoris

Eat plenty of fruits, vegetables, and whole grains. Choose lean proteins, such as skinless chicken, fish, and beans. Eat non-fat or low-fat dairy products, such as skim milk and low-fat yogurt. Avoid foods that contain high levels of sodium (salt).

Efonidipine may be contraindicated in the following.

Hypersensitivity, Severe hypotension, Cardiogenic shock, Left ventricular outflow tract obstruction, Heart failure after acute myocardial infarction.

Kidney:

Caution is advised among patients with kidney problems. Close monitoring of kidney function and adjustments of the dose of the medicine may be needed based on the clinical condition of the patient. However, if you have any renal problems, it is highly recommended that you consult a doctor before the consumption of this medicine.

Liver:

Caution is advised among people with liver problems. Dose adjustments of the tablet may be needed. If you have any hepatic problems, it is highly recommended that you consult doctor before the consumption of this medicine.

Category C: Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.

Salt Substitutes: Those who are taking Efonidipine should avoid sodium, calcium, and magnesium-rich foods. The salts may reduce the blood-pressure-lowering effect of Efonidipine.

The adverse reactions related to molecule Efonidipine can be categorized as

• Common Adverse effects: Headache (usually transitory), flushing, dizziness, nausea, vomiting and weakness
• Less Common adverse effects: Red, Itchy or watery eyes – These can be signs of conjunctivitis or a corneal ulcer, Painful sores (ulcers) on the eyes, skin or the lining of your mouth
• Rare Adverse effects: Tinnitus, Thrombocytopenia, Visual disturbances, Insomnia, Gynaecomastia, Elevated hepatic enzymes, Anxiety and depression

The clinically relevant drug interactions of Efonidipine are briefly summarized here.

Hypotensive interaction may occur with alcohol, TCAs, antihypertensives and other vasodilators.

Potentially Fatal: Enhanced hypotensive effect with sildenafil and other phosphodiesterase type-5 inhibitors.

Avoid taking medicine more than the prescribed dosage. If you notice any unusual or abnormal reactions after taking the tablet, promptly seek medical attention. Depending on the dosage of Efonidipine, symptoms vary in individuals, you may experience one or more of the following symptoms:

Bradycardia, Dysrhythmia, Marked hypotension, Excessive peripheral vasodilation, Reflex tachycardia, Cardiogenic shock

Pharmacodynamics:

Efonidipine is a calcium channel blocker that works by normalizing the blood pressure by relaxing the blood vessels and improves blood flow and oxygen in the body, thereby reducing the risk of getting chest pain. It prevents the entry of calcium from entering into the muscles, leading to muscle relaxation.

Pharmacokinetics:

• Absorption

The absorption ratio of radioactivity estimated from the sum of biliary and urinary excretions was found to be approximately 62% . The radioactivity was high in the gastrointestinal tract and liver, followed by the adrenal glands, suggesting high rates of metabolism in these regions.

• Metabolism:

Efonidipine is mainly metabolized in the liver. Its metabolites are N-dephenylated Efonidipine (DPH), deaminated efonidipine (AL) and N-debenzylated Efonidipine (DBZ). Both metabolites behave as calcium antagonists. In one study, the vasodilating capabilities of DBZ and DPH were about two-thirds and one-third respectively than that of the unmetabolized drug. Research suggests that the majority of the pharmacological effect after oral dosing of efonidipine hydrochloride is due to unchanged drug and its metabolites play little role in its therapeutic effect.

• Elimination

Efonidipine is also referred to as NZ-105 and has been found to be mainly eliminated by the biliary system

1. https://go.drugbank.com/drugs/DB09235
2. https://www.apollopharmacy.in/salt/EFONIDIPINE
3. https://pubchem.ncbi.nlm.nih.gov/compound/Efonidipine#section=MeSH-Pharmacological-Classification
4. https://www.medplusmart.com/product/efnocar-40mg-tab_efno0001