Product Overview
[Drug Name]
Generic Name: Benidipine Hydrochloride Tablets
Trade Name: Yuanzhi Benidipine Hydrochloride Tablets 4mg*12 Tablets
Pinyin Full Code: YuanZhi YanSuanBeiNiDiPingPian 4mg*12 Tablets
[Main Ingredient]
The active ingredient of this product is benidipine hydrochloride.
[Properties]
This product is a film-coated tablet. After removing the coating, it appears microscopically yellow-green.
[Indications/Main Functions]
Essential hypertension.
[Specifications]
4mg*12 tablets
[Dosage and Administration]
Oral administration after breakfast. The adult dosage is generally 2mg-4mg (1/2-1 tablet) once daily. The dosage should be adjusted based on age and symptoms. If the effect is unsatisfactory, the dosage can be increased to 8mg (2 tablets) once daily. Patients with severe hypertension should take 4-8mg (1-2 tablets) once daily.
[Adverse Reactions]
Use of this drug from its approval until October 1997 A survey was conducted with a total sample size of 4,679 patients. Of these, 219 patients (47%) experienced side effects and 361 experienced abnormal clinical test values. Major side effects included palpitations in 24 (0.5%), facial flushing in 22 (0.5%), and headache in 20 (0.4%). 1. Serious Adverse Reactions: Liver Function Impairment and Jaundice (Unknown Frequency): Sometimes, liver function impairment and jaundice values, such as those associated with sconAP and YOTP, may occur. Therefore, careful observation is recommended. If abnormalities occur, discontinue the drug and implement appropriate measures. Other Adverse Reactions: The following side effects may occur, so careful observation is recommended. If abnormalities occur, reduce the dose or discontinue the drug, and implement appropriate measures. If the side effects listed in bold occur, discontinue the drug.
[Contraindications]
Patients with cardiogenic shock [may worsen symptoms]. Pregnant women or women who may become pregnant [see [Use in Pregnant and Lactating Women]]
[Drug Interactions]
1. Other Antihypertensive Drugs: Enhanced antihypertensive effect, may cause excessive lowering of blood pressure. 2. Digoxin: Inhibits renal tubular digoxin secretion, increasing blood digoxin concentrations. May cause digitalis poisoning. 3. Cimetidine: Cimetidine inhibits liver microsomal calcium antagonist metabolizing enzymes, while also reducing gastric acid and increasing drug absorption. May cause excessive lowering of blood pressure. 4. Rifampicin: Rifampicin induces liver drug metabolizing enzymes, promoting calcium antagonist metabolism, which may reduce benidipine blood concentrations and weaken the antihypertensive effect. 5. Grapefruit Juice: Grapefruit juice inhibits the metabolism of this drug in the liver, increasing blood concentrations. Increased blood pressure. May cause excessively lower blood pressure.
[Precautions]
1. Use with caution (the following patients should use this medication with caution): ① Patients with excessively low blood pressure ② Patients with severe liver damage [may worsen liver damage] ③ Elderly patients [see (Use in Elderly Patients)]
2. Important Basic Precautions ① There have been reports of worsening symptoms with sudden discontinuation of calcium antagonists. Therefore, when discontinuing this medication, the dosage should be gradually reduced and careful observation should be made. Patients should not stop taking this medication without a physician's guidance. ② This medication may cause excessively low blood pressure, including transient unconsciousness. If such symptoms occur, appropriate measures should be taken, such as reducing the dosage or discontinuing the medication. ③ Dizziness may occur due to the antihypertensive effect. Therefore, caution should be exercised when working at heights or operating hazardous machinery, such as driving a car.
3. Instructions for Use: ① When splitting, the dose should be taken as soon as possible after splitting (store in dark and use within 60 days after splitting). ② When dispensing medications packaged in PTP packaging, instruct the patient to remove the medication from the PTP sheet before taking it. [There have been reports of patients accidentally swallowing PTP sheets, causing the hard, sharp corners to pierce the esophageal mucosa, leading to perforation and serious complications such as mediastinitis.]
4. Other Precautions: Patients undergoing CAPD (continuous ambulatory peritoneal dialysis) have been reported to sometimes experience turbid dialysis fluid. Therefore, it is important to carefully distinguish this from other conditions such as peritonitis. Please read the instructions carefully and follow your doctor's instructions.
[Pediatric Use]
Safety for premature infants, newborns, infants, toddlers, or children has not been established (no experience).
[Elderly Use]
Generally, the elderly Patients should avoid excessive blood pressure reduction. Therefore, elderly patients with hypertension should start with a low dose (2 mg/day) and carefully monitor their medication progress. Caution is recommended for medication administration.
[Overdose]
Overdose may cause an excessive decrease in blood pressure. If severe hypotension occurs, appropriate measures should be taken, such as elevating the lower limbs, administering fluids, or administering pressor medications. Furthermore, due to the high protein binding rate of this drug, dialysis is ineffective.
[Pharmacology and Toxicology]
Pharmacological Action: This drug binds to the DHP binding site of membrane potential-dependent calcium channels on cell membranes, inhibiting calcium influx and thereby dilating coronary and peripheral blood vessels. It is speculated that this drug primarily enters the cell membrane and binds to the DHP binding site. Furthermore, studies of this drug's inhibitory effect on isolated vasoconstriction and its binding to DHP have shown that this drug can inhibit calcium ion influx and dilate coronary and peripheral blood vessels. Site affinity, etc., prove that this product has a strong affinity for the DHP binding site and a very slow dissociation rate, so it shows a sustained pharmacological effect, and is not correlated with blood drug concentration. () Antihypertensive effect When spontaneously hypertensive rats, DOCA salt hypertensive rats, and renal hypertensive dogs are orally administered with this product, a slow-onset and long-lasting antihypertensive effect can be seen. No drug resistance is observed with long-term administration. Oral administration of this product once a day to patients with primary hypertension can produce a 24-hour stable antihypertensive effect without affecting the diurnal variation of blood pressure. 2 Anti-anginal effect This product significantly improves experimental angina pectoris in rats and cardiac dysfunction and ischemic electrocardiogram changes caused by ischemia-reperfusion of large coronary arteries. Oral administration of this product to patients with exertional angina pectoris can significantly improve ischemic changes (decreased ST on the electrocardiogram) caused by exercise load. ( 3) Effect on maintaining renal function: When this product is continuously administered orally to spontaneously hypertensive rats with renal insufficiency (5/6 nephrectomy), it can show a hypotensive effect and improve renal function. This product can significantly increase renal blood flow in patients with essential hypertension. When this product is administered orally to patients with chronic renal insufficiency accompanied by hypertension, it can significantly increase creatinine clearance and urea nitrogen clearance, maintain renal function, and toxicity studies: Subacute toxicity: Humans and mice were continuously orally administered 0.38, 1.325, 50, and 10 mg/kg for 3 months. Fat deposition in the liver (from the marginal zone to the middle zone of the liver lobule) was observed in the group above 6 mg/kg, but it can be recovered or has a tendency to recover after drug withdrawal. The non-toxic dose is 1.5 mg/kg. The maximum continuous oral administration of this product is 0.17, 0.5, 15, 3, 6, and 12 mg/kg for 3 months. , the heart rate and heart weight increased in the group above 1.5mg/kg, and atrioventricular block was observed at 6mg/kg. The non-toxic dose is 0.5mg/kg. Chronic toxicity: Rats were orally administered 3075 and 1.56mg/kg of this product for 12 months continuously. The thymus weight decreased and the liver edge was blunted in the group above 075mg/kg. The heart, lung and spleen weight increased in the group above 1.5mg/kg. 6mg/Kg inhibited weight gain and increased liver and kidney weight was observed. Dogs were orally administered 004002, 01, 038, 15, and 6mg/g of this product for 12 months continuously. The heart rate increased and gingival hyperplasia was observed in the group above 1.5mg/kg. Atrioventricular block was observed at 6mg/kg, but no pathological changes were found in the heart by histopathological examination. Reproduction Toxicity: Oral administration of this drug to rats during the pre-pregnancy and early gestation period at 3-50 mg/kg and 50 mg/q resulted in a slight decrease in the number of corpora lutea. However, the number of implantations and fetal numbers in all treatment groups showed no difference compared to the control group, and the fetuses developed well. Oral administration of this drug to rats during the organogenesis period at 6-35 mg/kg and to domestic animals at 6-100 mg/kg resulted in a slight increase in fetal mortality at 35 mg/kg and an increase in embryonic death at 100 mg/kg, but no teratogenicity was observed. Oral administration of this drug to rats during the perinatal and lactation period at 6-35 mg/kg resulted in a prolonged gestation period at 25 mg/kg or above, a prolonged delivery time and an increased number of stillborn pups at 35 mg/kg, and an inhibition of pup weight gain during lactation at 12 mg/kg or above.
