Beniflo

Dosage Form & Strength

Hypertension, renal parenchymal hypertension In general, for adults, 2 to 4 mg of benidipine hydrochloride is orally administered once daily after breakfast. The dose may be adjusted according to the patient’s age and symptoms, but if the effect is insufficient, the dose can be increased up to 8 mg once a day. However, for severe hypertension, 4 to 8 mg should be orally administered once daily after breakfast. Angina In general, for adults, 4 mg of benidipine hydrochloride is orally administered twice daily after morning and dinner. The dose may be adjusted according to the patient’s age and symptoms.

Dosage in Special Population

Contraindicated in pregnancy and lactation

Indications

Beniflo is indicated for the treatment of hypertension and Angina Pectoris

Adverse Effects

The side effects include Dizziness, Orthostatic Hypotension, Headache, and Weakness. Apart from these, using Benidipine may further lead to Vertigo, Anemia, Renal Impairment and increase in blood potassium levels

Drug Interactions

With Cimetidine & Itraconazole: Blood pressure may drop excessively, It has been reported that cimetidine inhibits calcium channel blocker metabolizing enzymes in hepatic microsomes while lowering gastric acid and increasing drug absorption, Itraconazole may inhibit the metabolism of this drug in the liver and increase the blood concentration of this drug; with Rifampicin: The antihypertensive effect may be diminished: It has been reported that rifampicin induces drug-metabolizing enzymes in the liver, promotes metabolism of calcium channel blockers, and lowers blood levels

Mechanism of Action

Beniflo (Benidipine) suppresses the intracellular Ca influx by binding to the DHP binding site of the membrane voltage-gated Ca channel of the cell membrane, and dilates coronary and peripheral blood vessels. It is presumed that this drug has high transferability to the cell membrane and binds to the DHP binding site mainly through the cell membrane. Furthermore, by examining the inhibitory effect on excised vasoconstriction and the affinity for the DHP binding site, the drug to the DHP binding site It has been confirmed that the binding of the drug is strong and the dissociation rate is very slow, and the action is sustained with almost no correlation with the blood concentration of the drug Antihypertensive effect : When this drug was orally administered to spontaneously hypertensive rats, DOCA-salt hypertensive rats, and renal hypertensive dogs, the onset of action was slow and a long-lasting antihypertensive effect was observed. In addition, resistance did not occur even after long-term administration. In addition, when this drug was orally administered to patients with essential hypertension once daily, it showed a stable antihypertensive effect for 24 hours without affecting diurnal fluctuations in blood pressure Anti-angina effect: This drug significantly improved cardiac function decline and ischemic electrocardiographic changes due to experimental angina model (rat) and canine coronary artery ligation and reperfusion. In addition, when this drug was orally administered to patients with exertional angina, it showed an improving effect on ischemic changes due to exercise load (electrocardiogram ST decrease)

Pharmacokinetics

Cmax (2.25 ng / mL) Tmax (0.8 hr) T 1/2 (1.70 hr) Protein binding 98.46 to 98.93% Benidipine is mainly metabolized by CYP3A4 Excretion is 35% from urine and about 36% in feces The half life of Benidipine in Beniflo is 1.70 ± 0.70 hours

Drug Use in Pregnancy

Avoid administration to pregnant women or women who may be pregnant. [In animal studies,fetal toxicity has been reported, and administration at the end of pregnancy prolongs gestation and delivery time. ] It is desirable to avoid administration to lactating women, but if it is unavoidable, avoid lactation.

Drug Use in Renal Impairment

For patients with severe renal impairment (CLcr <30 mL/min/1.73 m2) not on hemodialysis,

Drug Use in Pediatric Population

Safety has not been established for low birth weight infants, newborns, infants, toddlers or children.

Drug Use in Geriatric Population

In general, excessive hypotension is not desirable for the elderly, so when using it for the elderly with hypertension, carefully observe the course, such as starting administration from a low dose (2 mg / day). However, it is desirable to administer it carefully.