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Calcium Channel Blockers

Calcium channel blockers (CCBs) also known as calcium antagonists. <br>They are first line antihypertensive drugs. They are also used to treat angina & used to lower blood pressure. Drug Name of CCBs is nifedipine, felodipine, Amlodipine.

Mainaksaha
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Calcium Channel Blockers

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  1. Calcium Channel Blockers Presented By MainakSaha

  2. Contents • Introduction • Mechanism Of Action • Classification of Calcium Channel Blockers • SAR OF 1,4-Dihydropyridine • Drug Name With Structure, IUPAC & Physical Properties • References

  3. Introduction • Calcium channel blockers (CCBs) also known as calcium antagonists. • Calcium channel blockers are drugs used to lower blood pressure. • They work by slowing the movement of calcium into the cells of the heart and blood vessel walls. Therefore it easier for the heart to pump and widens blood vessels. • As a result, the heart doesn't have to work as hard, and blood pressure lowers. • They are first line antihypertensive drugs. They are also used to treat angina.

  4. Mechanism Of Action • Calcium-channel blockers (CCBs) bind to L-type calcium channels located on the vascular smooth muscle, cardiac myocytes, and cardiac nodal tissue. • These channels are responsible for regulating the influx of calcium into muscle cells, which in turn stimulates smooth muscle contraction and cardiac myocytes contraction. • In cardiac nodal tissue, L-type calcium channels play an important role in pacemaker currents and in phase 0 of the action potentials. • Therefore, by blocking calcium entry into the cell, CCBs cause vascular smooth muscle relaxation (vasodilation), decreased myocardial force generation (negative inotropy), decreased heart rate (negative chronotropic), and decreased conduction velocity within the heart (negative dromotropic).

  5. Classification of Calcium Channel Blockers Isradipine Nicardipine Felodipine Phenylalkylamines Dihydropyridines Benzothiazepines Diltiazem Verapamil 1st Generation 2nd Generation 3rd Generation Nifedipine Amlodipine

  6. 1,4-Dihydropyridine ring is essential for activity SAR OF 1,4-Dihydropyridine • Substitution at nitrogen or oxidation or reduction of the ring reduce activity • A Phenyl substitution at R4 position is essential for activity • Ortho and meta position substitution is better for activity • 3, 5 position ester group is essential for activity • C-2 & C-6 methyl group is activity

  7. Drug Name With Structure, IUPAC & Physical Properties Physical Properties- Insoluble in water , soluble in acetone, methanol Half life 10-18 hrs No2 group is essential, Use in angina pectoris Slidely soluble in water , soluble in methanol Half life 34 hrs It has greater selectively of vascular smooth muscle Physical Properties- Nifedipine Amlodipine

  8. Physical Properties- Insoluble in water , soluble in acetone Half life 10-18 hrs Use in angina pectoris Felodipine

  9. References 1.Selvakumar. S , J. Dighade . S, R. Srinivasan MEDICINAL CHEMISTRY-II 2.https://www.cvpharmacology.com/vasodilator/CCB 3. K. G. Bothara “A text book Medicinal Chemistry – II”

  10. Thank You

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