What Is Barnidipine?

Barnidipine, also known as melodipine, is a chemical. Chemical name ( 4S ) -2,6-dimethyl-4- (m-nitrophenyl) -1,4-dihydropyridine-3,5-dicarboxylic acid (3S) -1-benzyl-3 -Pyrrolidinyl-methyl ester, the molecular formula is C ₂₇ H ₂₉ N ₃ O ₆ , and the molecular weight is 491.553600. The main clinical treatment is primary hypertension and angina pectoris.

Chinese name: Banidipine
Foreign name: Barnidipine

CAS number: 104713-75-9
Molecular formula: C27H29N3O6

Brief introduction of balidipine compounds

Bannidipine Basic Information

Chinese name

Chinese alias: (4S) -2,6-dimethyl-4- (m-nitrophenyl) -1,4-dihydropyridine-3,5-dicarboxylic acid (3S) -1-benzyl-3 -Pyrrolidinyl-methyl ester

English name: (+)-(3'S, 4S) -1-Benzyl-3-pyrrolidinyl methyl 1,4-dihydro-2,6-dimethyl-4- (3-nitrophenyl) -3,5-pyridinedicarboxylate

English alias: (4S) -2,6-Dimethyl-1,4-dihydro-4- (3-nitrophenyl) pyridine-3,5-dicarboxylic acid 5-methyl 3-[(3S) -1-benzylpyrrolidin-3- yl] ester;

CAS number: 104713-75-9

Molecular formula: C ₂₇ H ₂₉ N ₃ O ₆

Chemical structure:

Molecular weight: 491.553600

Exact mass: 491.20600

PSA: 113.69000

LogP: 4.61020 ^[1]

Physical properties of Barnidipine

Density: 1.31 g / cm ³

Boiling point: 614.5ºC at 760 mmHg

Refractive index: 1.628

Vapor pressure: 4.94E-15mmHg at 25 ° C ^[1]

Banidipine use

This product is a new dihydropyridine calcium antagonist with strong vasodilation and antihypertensive effects. ^[1]

Banidipine drug name

Chinese name

English name: Barnidipine

Alias: Melodipine, Hypoca, Mepinodipine.

English aliases: Barnidipine Hydrochloride, Hypoca, Mepirodipine Hydrochloride

Banidipine pharmacodynamics

Dihydropyridine calcium antagonists. It can dilate blood vessels, increase coronary flow, reduce blood pressure, and has a strong and long-lasting effect. It is well absorbed after oral administration, and reaches the peak plasma concentration after 1 to 6 hours. t1 / 2 is about 10 hours. This product is a potent and long-acting dihydropyridine calcium antagonist antihypertensive drug. It has a strong inhibitory effect on the inflow of calcium ions, reduces the amount of calcium ions in the cells, thereby relaxing and expanding the blood vessels, reducing the peripheral vascular resistance and exerting a significant antihypertensive effect. Its strength is 5 times that of nicardipine. ^[2]

Pharmacokinetics of Banidipine

Oral absorption is good, effective after 1-1.6 hours after oral administration, 10 mg / kg orally, C _max is 3-4.4 ng / ml, and the antihypertensive effect can be maintained for more than 10 hours; it is widely distributed, and the concentration in kidney, liver and stomach It is high in plasma and lowest in brain; it is metabolized slowly in the liver, but it is eliminated slowly in other organs. Repeated administration has no accumulation effect, and metabolites are excreted by feces. ^[2]

Clinical application of Banidipine

It is used for the treatment of mild, moderate and severe hypertension, and combined with -blocker antihypertensive drugs or diuretics can enhance the efficacy. ^[2]

Banidipine Toxic Side Effects

This product has small toxic and side effects, and is well tolerated. The more common adverse reactions include flushing, headache, palpitations, mild hypotension and rapid pulse. ^[2]

Banidipine indications

hypertension. ^[2]

Bannidipine dosage

Oral: 5-15mg / time, once / d.

Preparations and specifications

Each capsule contains three specifications of this product: 5, 10, and 15 mg. ^[2]

Banidipine disabled for caution

Patients with severe liver dysfunction should be used with caution. Elderly patients should not excessively lower blood pressure. Administration should start at a low dose and should be taken under careful supervision.

It is not suitable for pregnant women or women who may be pregnant, because it has been reported that this product can inhibit fetal growth and development and can enter the milk of animals. Therefore, lactating women should not take this product. When necessary, patients should be advised to stop lactating. The safety of this product to children has not been determined. ^[2]

Barnidipine adverse reactions

Transaminase, uric acid, urea nitrogen, and creatinine may be elevated, and medication should be discontinued in such cases. If a hypersensitivity reaction (erythema, rash, or jaundice) occurs, the drug should be discontinued. Other possible adverse reactions include nausea, vomiting, constipation, fever, facial flushing, palpitations, edema, weakness, discomfort, headache, chest pressure, dizziness, tinnitus, and elevated serum creatine phosphate kinase (CRK). ^[2]

Barnidipine interaction

The combination of this product with other antihypertensive drugs can enhance the efficacy. It has been reported that other calcium antagonists such as nifedipine can increase the plasma concentration of digoxin. It has also been reported that the use of such drugs with cimetidine can lead to enhanced efficacy. ^[2]

Banidipine expert review

The antihypertensive effect and safety of this product alone or combined with diuretics were evaluated in 91 patients with essential hypertension in the long term. The results showed that the antihypertensive effect of this product was stable and no drug resistance was found. The two groups had similar effects. More than 80% are effective for treatment. Another group of 42 patients with essential hypertension clinical trials, given this product alone and combined with -blockers, can effectively reduce blood pressure, 70.4% and 91.7% of patients' original blood pressure, respectively, no night The blood pressure was excessively reduced and the blood pressure lowering effect continued to 24 hours, which suggests that it is suitable for administration once a day. ^[2]