NISOLDIPINE

PRODUCT IDENTIFICATION

CAS NO. 63675-72-9, 103573-36-0, 103573-38-2

NISOLDIPINE

EINECS NO. 264-407-7
FORMULA C20H24N2O6
MOL WT. 388.42

H.S. CODE

2933.39.4100

TOXICITY

Oral Rat LD50: 1257mg/kg
SYNONYMS Nisoldipino; Nisocor; Nisoldipino; Nisoldipinum; Sular;
1,4-Dihydro-2,6- dimethyl-4-(2-nitrophenyl)-3,5-pyridine dicarboxylic acid, methyl 2-methylpropyl ester; Iosbutyl methyl-1,4-dihydro-2,6-dimethyl-4-(o- nitrophenyl)-3,5- pyridinedicarboxylate; Isobutyl 1,4-dihydro-5-methoxycarbonyl-2,6-dimethyl-4-(2-nitrophenyl)-3-pyridincarboxylate;
SMILES c1([C@@H]2C(=C(NC(=C2C(OC)=O)C)C)C(OCC(C)C)=O)c(cccc1) [N+](=O)[O-]

CLASSIFICATION

Antihypertensive agent, Calcium channel blocker, Cardiovascular Agent, Vasodilator agent, Dihydropyridine

EXTRA NOTES

A dihydropyridine calcium channel antagonist that acts as a potent arterial vasodilator and antihypertensive agent. It is also effective in patients with cardiac failure and angina.
L-type (CaV1.2) calcium channel blocker; dihydropyridine-type calcium channel blocker with selectivity for smooth muscle (CaV1.2b) over cardiac muscle (CaV1.2a). Arterial vasodilator and antihypertensive agent.

PHYSICAL AND CHEMICAL PROPERTIES

PHYSICAL STATE yellow crystalline powder
MELTING POINT 150 - 155 C
BOILING POINT  
SPECIFIC GRAVITY  
SOLUBILITY IN WATER Insoluble
pH soluble in acetone, ethanol and methanol
VAPOR DENSITY

 

AUTOIGNITION

 

log P 3.26 (Octanol-water)
VAPOR PRESSURE 3.04E-09 (mmHg at 25 C)
HENRY LAW CONSTANT 1.71E-13 (atm-m3/mole at 25 C)
OH RATE CONSTANT 1.17E-10 (cm3/molecule-sec at 25 C Atmospheric)

NFPA RATINGS

Health hazard: 1, Fire: 0, Reactivity Hazard: 0

REFRACTIVE INDEX

 

FLASH POINT  
STABILITY

Stable under ordinary conditions.

EXTERNAL LINKS & GENERAL DESCRIPTION

Wikipedia Linking

Google Scholar Search

Drug Information Portal (U.S. National Library of Medicine) - Nisoldipine

PubChem Compound Summary - Nisoldipine

http://www.nejm.org/doi/
The Effect of Nisoldipine as Compared with Enalapril on Cardiovascular Outcomes in Patients with Non-Insulin-Dependent Diabetes and Hypertension

Local:
Calcium ions are needed for electrical activity for the contraction of cardiac and smooth muscle and conduction of nerve cell. Calcium channel blocker is a drug which inhibits the entry of excess calcium into cells and/or prevents form the mobilization of calcium from intracellular stores, resulting in relaxation of blood vessel walls and cardiac muscle for blood to flow more freely, lowering blood pressure thereby reducing oxygen demand in the heart and relieving anginal pain. It is used in the treatment of angina, cardiac arrhythmias, and hypertension.

Some major calcium channel blockers upon chemical structure are:

  • Dihydropyridine calcium channel blockers ; Amlodipine, Lacidipine, Lercanidipine, Nicardipine, Nifedipine, Nisoldipine, Nitrendipine, Nimodipine.
  • Phenylalkylamine calcium channel blockers ; Gallopamil, Verapamil
  • Benzothiazepine calcium channel blockers Diltiazem
  • Diarylaminopropylamine ethers: Bepridil, Mibefradil
Nisoldipine is used in the treatment of high blood pressure. The chemical designation is 1,4-Dihydro-2,6-dimethyl-4-(2- nitrophenyl)-3,5- pyridine dicarboxylic acid, methyl 2-methylpropyl ester; It is a  yellow crystalline powder; insoluble in water , soluble in ethanol, ethyl acetate, chloroform; melting point 150 - 155 C; administered orally.
SALES SPECIFICATION

APPEARANCE

yellow crystalline powder

IDENTIFICATION

Complies Test A,B

ASSAY (HPLC)

98.0 - 102.0%

IMPURITY

1.0% max (Individual impurity: 0.5% max)

LOSS ON DRYING

1.0% max

HEAVY METALS

10ppm max

MELTING POINT

150 - 155 C

TRANSPORTATION
PACKING
 
HAZARD CLASS  
UN NO.  
SAFETY INFORMATION

HAZARD OVERVIEW

OSHA Hazards:Target Organ Effect, Harmful by ingestion., Harmful by skin absorption. Target Organs:Cardiovascular system.

GHS

 

SIGNAL WORD Warning

PICTOGRAMS

HAZARD STATEMENTS

H302 + H312 Harmful if swallowed or in contact with skin

PRECAUTIONARY STATEMENTS

P280 Wear protective gloves/ protective clothing.

EC DIRECTIVES

 

HAZARD CODES

Xn Harmful

RISK PHRASES

20/21/22:  Harmful by inhalation, in contact with skin and if swallowed

SAFETY PHRASES

36 Wear suitable protective clothing

PRICE INFORMATION