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Nitrendipine

Nitrendipine structure

CAS No:
39562-70-4
Formula:
C18H20N2O6
Chemical Name:
Nitrendipine
Synonyms:
3,5-Pyridinedicarboxylic acid,1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-,3-ethyl 5-methyl ester;3,5-Pyridinedicarboxylic acid,1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-,ethyl methyl ester;BAY-e 5009;Nitrendipine;Bayotensin;Baypress;(±)-BAY E 5009;(±)-Nitrendipine;Nitrepin;Nitrendipin;Bylotensin;Deiten;Nidrel;Cardif;Baylotensin;86052-02-0;146904-08-7
Categories:
Active Pharmaceutical Ingredients > Circulatory System Drugs

Description

Nitrendipine is a calcium channel blocker with marked vasodilator action.Target: Calcium ChannelNitrendipine is a dihydropyridine calcium channel blocker. It is used in the treatment of primary hypertension to decrease blood pressure. Nitrendipine blocked Ca2+ currents very potently, with half-block by subnanomolar concentrations. The concentration dependence of block had the form expected for 1:1 binding, with an apparent dissociation constant (Kd) of 0.36 nM. In contrast, when cells we

Solid

Nitrendipine is a dihydropyridine that is 1,4-dihydropyridine substituted by methyl groups at positions 2 and 6, a 3-nitrophenyl group at position 4, a ethoxycarbonyl group at position 3 and a methoxycarbonyl group at position 5. It is a calcium-channel blocker used in the treatment of hypertension. It has a role as a calcium channel blocker, an antihypertensive agent, a vasodilator agent and a geroprotector. It is a C-nitro compound, a dihydropyridine, an ethyl ester, a diester, a member of dicarboxylic acids and O-substituted derivatives and a methyl ester.|Nitrendipine is a calcium channel blocker with marked vasodilator action. It is an effective antihypertensive agent and differs from other calcium channel blockers in that it does not reduce glomerular filtration rate and is mildly natriuretic, rather than sodium retentive.|A calcium channel blocker with marked vasodilator action. It is an effective antihypertensive agent and differs from other calcium channel blockers in that it does not reduce glomerular filtration rate and is mildly natriuretic, rather than sodium retentive.

Nitrendipine Basic Attributes

Molecular Weight：

360.36

Exact Mass：

360.36

EC Number：

254-513-1

NSC Number：

758466

DSSTox ID：

DTXSID0023373

ATC Code：

C - Cardiovascular system

HScode：

2933399090

Characteristics

PSA：

110

XLogP3：

2.9

Appearance：

yellow to green powder

Density：

1.2±0.1 g/cm3

Melting Point：

158 °C

Boiling Point：

464.8°C at 760 mmHg

Flash Point：

249.5±28.7 °C

Refractive Index：

1.554

Water Solubility：

soluble in DMSO (17.5 mg/ml), methanol (15 mg/ml), ethyl acetate, and ethanol (25 mM). Insoluble in water.

Storage Conditions：

Store at RT

Toxicity：

LD50 in mice, rats (mg/kg): 39, 12.6 i.v.; 2540, >10000 orally (Hoffmann)

Collision Cross Section：

182.2 Å² [M+H]+ [CCS Type: TW, Method: Major Mix IMS/Tof Calibration Kit (Waters)]|181.9 Å² [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

Safety Information

Transport codes：

NONH for all modes of transport

wgk germany：

hazard class code：

20/21/22

safety instructions：

RTECS Number：

US5653000

Marks：

Stability/Shelf Life：

Stable at normal temperatures and pressures.

Precautionary statement(s)：

P261-P280

Hazard Statements：

H312 + H332

GHS Classification：

|Warning|H312 (84.42%): Harmful in contact with skin [Warning Acute toxicity, dermal]|P201, P202, P261, P271, P280, P281, P302+P352, P304+P312, P304+P340, P308+P313, P312, P322, P363, P405, and P501|Aggregated GHS information provided by 156 companies from 4 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Toxicity

Protein Binding：

> 99%

Drug Information

Drug Indication：

For the treatment of mild to moderate hypertension

Pharmacology：

Nitrendipine, a dihydropyridine calcium-channel blocker, is used alone or with an angiotensin-converting enzyme inhibitor, to treat hypertension, chronic stable angina pectoris, and Prinzmetal's variant angina. Nitrendipine is similar to other peripheral vasodilators. Nitrendipine inhibits the influx of extra cellular calcium across the myocardial and vascular smooth muscle cell membranes possibly by deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum. The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.

MeSH：

Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS. (See all compounds classified as Antihypertensive Agents.)|A class of drugs that act by selective inhibition of calcium influx through cellular membranes. (See all compounds classified as Calcium Channel Blockers.)|Drugs used to cause dilation of the blood vessels. (See all compounds classified as Vasodilator Agents.)

Mechanism of Action：

By deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, Nitrendipine inhibits the influx of extracellular calcium across the myocardial and vascular smooth muscle cell membranes The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.

MeSH Entry Terms：

Balminil

Nitrendipine Use and Manufacturing

Nitrendipine is a dihydropyridine calcium channel blocker. Nitrendipine is used in the treatment of primary (essential) hypertension to decrease blood pressure. Antihypertensive.

Computed Properties

Molecular Weight:360.4
XLogP3:2.9
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:7
Rotatable Bond Count:6
Exact Mass:360.13213636
Monoisotopic Mass:360.13213636
Topological Polar Surface Area:110
Heavy Atom Count:26
Complexity:661
Undefined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

Material

Methyl acetoacetate

Drug Function and Efficacy

This product is a dihydropyridine calcium channel blocker that inhibits the transmembrane calcium ion influx of vascular smooth muscle and myocardium. It mainly acts on blood vessels, causing the dilation of systemic blood vessels such as coronary arteries and renal arterioles, producing a hypotensive effect.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Nitrendipine Tablets
Ingredients	The main ingredient of this product is: Nitrendipine.
Indication	1. a-receptor blockers: Most patients can enhance the antihypertensive effect by taking this drug together, and can reduce the tachycardia that occurs after the drug lowers blood pressure; however, some patients may induce and aggravate systemic hypotension, heart failure and angina pectoris. 2. Angiotensin-converting enzyme inhibitors are well tolerated when taken together, and the antihypertensive effect is enhanced. 3. Long-acting nitrates are well tolerated when taken together, but there is still a lack of literature evaluating the effectiveness of this combination in controlling angina pectoris. 4. Digitalis: Some studies suggest that taking this drug can increase the plasma concentration of digoxin taken together, by an average of 45%. Some studies believe that it does not increase the plasma concentration and toxicity of digoxin. It is suggested that we should monitor the blood concentration of digoxin when using it for the first time, adjusting the dose or stopping the use of nitrendipine to prevent digoxin overdose or underdose. 5. Coumarin anticoagulants: There is no report that co-administration of nitrendipine can increase the prothrombin time of coumarin anticoagulants. At present, the interaction between them cannot be confirmed. 6. Cimetidine: Since cimetidine can mediate the inhibition of liver cytochrome P450 enzymes and change the first-pass effect of nitrendipine, it is recommended that patients who are taking cimetidine should pay attention to the adjustment of drug dosage when taking nitrendipine in combination.
Specifications	10mg
Manufacturer	Shanghai Hengshan Pharmaceutical Co., Ltd.

Nitrendipine Tablets
Ingredients	The main ingredient of this product is nitrendipine.
Indication	1. beta-receptor blockers: The combination of this drug can enhance the antihypertensive effect in most patients and reduce the tachycardia that occurs after the product lowers blood pressure; however, some patients may induce and aggravate systemic hypotension, heart failure and angina pectoris. 2. Angiotensin-converting enzyme inhibitors: The combination is well tolerated and the antihypertensive effect is enhanced. 3. Long-acting nitrates: The combination is well tolerated, but there is still a lack of literature evaluating the effectiveness of this combination in controlling angina pectoris. 4. Digitalis: Some studies suggest that taking this drug can increase the plasma concentration of digoxin in combination, with an average increase of 45%. Some studies believe that it does not increase the plasma concentration and toxicity of digoxin. It is suggested that we should monitor the blood concentration of digoxin when using it for the first time, adjusting the dose or stopping the use of nitrendipine to prevent digoxin overdose or underdose. 5. Coumarin anticoagulants: There is no report that the combination of nitrendipine can increase the prothrombin time of coumarin anticoagulants. At present, the interaction between them cannot be confirmed. 6. Cimetidine: Since cimetidine can mediate the inhibition of liver cytochrome P450 enzymes and change the first-pass effect of nitrendipine, it is recommended that patients who are taking cimetidine should pay attention to the adjustment of drug dosage when taking nitrendipine in combination.
Specifications	10mg
Manufacturer	Hubei Huquan Pharmaceutical Co., Ltd.

Nitrendipine
Ingredients	Nitrendipine
Manufacturer	China Resources Double-Crane Pharmaceutical Co., Ltd.

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Registered Holders

株式会社パーマケム・アジア

Japan
Active
Lesheng Pharmaceutical Shijiazhuang Co., Ltd.

China
Active
Fuxiang (Dalian) Pharmaceutical Co., Ltd.

China
Active

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