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2-[benzyl(methyl)amino]ethylmethyl-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 479.5 g/mol |
2 | Physical appearance | Solid |
3 | Melting point | 136-138oC |
4 | Solubility | 2.2 mg/L |
5 | Octanol/water partition coefficient | 3.82 |
5 | Presence of ring | Dihydropyridine, phenyl |
6 | Number of chiral centers | 1 |
i. Nicardipine inhibits the influx of calcium across the vascular smooth muscles and myocardial muscles cells membranes through deformation of the channel, inhibition of ion-control gating mechanism and by interfering with release of calcium ions.
ii. There is decrease in the contractile processes of the smooth muscles of myocardium.
iii. Dilation of coronary and systemic arteries, there is increase in the oxygen supply to myocardial muscles.
iv. Due to this, there is decrease in the total peripheral resistance and decrease in the systemic blood pressure and afterload.
General structure activity of dihydropyridines calcium channel blockers can be summarized as:
Methyl ester of ß-aminocrotonic acid is reacted with 2-methyl-2-benzylaminoethyl ester of acetoacetic acid gives nicardipine. [1]
Nicardipine is used for the treatment of:
Side effects of Nicardipine are:
Q.1 Which of the following statements are correct related with the physicochemical properties of drug Nicardipine?
I. Molecular weight: 302.11 gm/mol
II. Physical appearance: solid
III. Melting point: 136-138 oC
a) I, II, III
b) I, II
c) II, III
d) I, III
Q.2 Match the following of the drugs with their correct IUPAC names.
i. Nicardipine | A. (2R)-2-{2-[(1R)-1-(4-chlorophenyl)-1-phenylethoxy]ethyl}-1-methylpyrrolidine |
ii. Lansoprazol | B. 2-[[3-methyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl]methylsulfinyl]-1H-benzimidazole |
iii. Clemastine | C. 2-[benzyl(methyl)amino]ethylmethyl-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate |
iv. Isoxicam | D. [(2R,3S)-1,3,4-trinitrooxybutan-2-yl]nitrate |
a) i-B, ii-C, iii-D, iv-A
b) i-D, ii-C, iii-B, iv-A
c) i-D, ii-B, iii-A, iv-C
d) i-B, ii-A, iii-D, iv-C
Q.3 Mechanism of action of drug Nicardipine includes?
I. Inhibition of calcium influx across the vascular smooth muscles and myocardial muscles cells membranes
II. Activation of gunaylate cyclase enzyme
III. Active synthesis of cGMP
IV. Decrease in total peripheral resistance
a) I, III, IV
b) I, IV
c) II, III
d) I, II, III, IV
Q.4 Correct sequence for True/false for the classification of the drug can be?
a) TFFT
b) FFTT
c) FFTF
d) TTTT
Q.5 Which of the following statements related with the SAR of dihydropyridines calcium channel blockers is/are correct?
a) R1 should be unsubstituted.
b) R1 should be easily detachable group.
c) Basic amino ethyl ether chain at R2 increases the potency of drug, while H/aryl group results in loss of activity of drug.
d) All of the above
Q.6 Type of rings present in the structure of nicardipine?
I. Dihydropyridine
II. Phenyl
III. Dihydrofuran
IV. Cyclobutane
a) II, IV
b) I , II
c) III, IV
d) IV
Q.7 Side effect of drug Nicardipine is/are?
a) Dizziness
b) Headache
c) Allergic reactions
d) All of the above
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ANSWERS
1-c
2-c
3-b
4-b
5-d
6-b
7-d
REFERENCES
[1] Vardanyan R, Hruby V. Synthesis of essential drugs. Elsevier; 2006 Mar 10.
The post NICARDIPINE Synthesis, SAR, MCQ,Structure,Chemical Properties and Therapeutic Uses appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.
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