antihypertensivedrugs

1. ANTIHYPERTENSIVE DRUGS Submitted to : Dr.M.N.Noolvi H.O.D. (P’ceutical chemistry) 1 ❑Submitted by: Kirti N patel M.pharm(IIIrd sem.) (P’ceutical chemistry)

2. : ❖Hypertension ➢ Hypertension is defined as either a sustained systolic blood pressure (SBP)of greater than 140 mm Hg or a sustained diastolic blood pressure of greater than 90 mm of Hg. ➢An agent that reduces high blood pressure is called as an ANTIHYPERTENSIVE. 2

3. ➢Prehypertension-systolic between 120 to 139 mm/Hg and diastolic between 80 to 89 mm/Hg. ➢ Effects of Hypertension ✓Increases risk of heart disease , heartfailure, kidney disease, blindness, and stroke. ✓ Primary Hypertension- No known reason. ✓Secondary Hypertension-due to some cause such as kidney disease, abnormalities of adrenal glands will try nonpharmacological methods first. 3

4. #Causes: It results from: Increased arterial resistance Reduced capacitance Increased peripheral vascular smooth muscle tone 4

5. Decrease in blood pressure Increased blood pressure Increased sympathetic activity Increased activation of β1 adrenoceptor s on heart Increased cardiac output Increased activation of α 1 adrenoceptors on smooth muscle Increased peripheral resistance Decreased renal blood flow Increased renin Increased angiotensin II Decreased GFR Increased aldosterone Increased Na-H2O Retention Increased blood volume 5

6. Miscellaneous α 2 receptor agonist α 1 r eceptor antagonist Calcium Channel blocker ACE Inhibitors Beta blockers Diuretics ANTI HYPERTENSIVE DRUGS 6

7. CLASSIFICATION OF DRUGS 1.ACE INHIBITORS Captopril,enalapril,lisinopril,perindopril,ramipril. 2.ANGIOTENSIN ANTAGONISTS Losartan,irbesartan,candesartan 3.CALCIUM CHANNEL BLOCKERS Verapamil,diltiazam,nifedipine,felodipine,amlodipine,lacidipine, 4.DIURETICS Thiazide=hydrochlorothiazide,chlorthalidone.indapamide High ceiling=furosemide K+ sparing=spironolactone.amiloride, 5.ß - ADRENERGIC BLOCKERS Propranolol,metaprolol,atenolol. 6 . +ß ADRENERGIC BLOCKERS Labetalol,carvedilol. 7 . - ADRENERGIC BLOCKERS prazosin.,terazosin,phentolamine 8.CENTRAL SYMPATHOLYTIC Clonidine,methyldopa 9.VASODILATORS Hydralazine,minoxidil sodium 7

8. ❖Diuretics Thiazide Type: Hydrochlorothiazide,Chlorothalidone,Bendroflume- thiazide,Trichloromethazide Potassium Sparing: Spironolactone,Amiloride,Triamterene Loop Diuretics: Furosemide,Ethacrynic Acid,Bumetanide,Torasemide 8

9. THIAZIDE DIURETICS Sodium,water retention Blood volume Cardiac output Peripheral resistance Decrease in blood pressure 9

10. ❖Potassium Sparing Diuretics: Includes: Spironolactone (a synthetic steroid that antagonizes aldosterone at intracellular cytoplasmic receptor site) Triamterene & Amiloride (blocks Na transport channels resulting in a decrease in Na/K exchange) 10

11. ❖Loop Diuretics: Inhibit the co-transport of Na/K/Cl in the luminal membrane in the ascending limb of the loop of Henle Examples:Furosemide,Bumetanide,Ethacrynic acid 11

12. ➢Beta Blockers: ➢Non-selective(β1/β2):Propranolol,Timolol Nadolol,Pindolol ✓propranolol structure ; 12

13. ✓ Sellecttiiveβ 1 1 :Atenolol,Acebutalol ✓Attenolol sttrructture; 13

14. Beta adrenoceptor blocker Activation of β1 receptors on the heart Renin Cardiac output Peripheral resistance Angiotensin II Aldosterone Na/Water retention Blood Volume Decrease in blood pressure 14

15. ➢Examples of ACE Inhibitors: Captopril Enalpril Lisinopril Ramipril 15

16. ❖ACE Inhibitors: ACE Inhibitors blocks the ACE that cleaves angiotensin-I to form the 16 potent vasoconstrictor angiotensin-II by reducing circulating angiotensin-II levels , ACE inhibitors also decrease secretion of aldosterone, resulting in decreased sodium & water retention.

17. ❑Angiotensin II receptor antagonist E.g.,losartan,irbesartan,candesartan, valsartan. Losartan Irbesartan 17

18. Angiotensin II receptor antagonist They produce vasodilation and block aldosterone secretion, thus lowering blood pressure and decreasing salt and water retention. 18

19. ➢Calcium channel blockers: Dihydropyridine:Nifedipine,nicardipine Phenylalkylamines:Verapamil Benzothiazepines:Diltiazem 19

20. Calcium channel blockers: It inhibits cellular influx of Ca, which is responsible for muscle contraction. Calcium channel blockers protect tissue by inhibiting entrance of Ca into cardiac & smooth muscle cells of coronary & systemic arterial beds. All Ca channel blockers are vasodilators that ultimately cause dilation of coronary & peripheral arteries,reduce heart rate. 20

21. ➢α-1 adrenergic receptors antagonist: ✓Decrease the peripheral vascular resistance & lower the arterial blood pressure by causing relaxation of both arterial & venous smooth muscle ✓Examples: Prazosin Doxazosin Terazosin 21

22. ❖α-2 adrenergic receptor agonist: Clonidine acts centrally to produce inhibition of sympathetic vasomotor centers. 22

23. ❖Miscellaneous α-methyl dopa Neuronal blockers (bretylium, guanethidine) ➢Bretylium 23

24. #Rauwolfia and derivatives (reserpine, deserpidine) reserpine 24

25. #Ganglionic blockers (guanadrel, mecamylamine) Guanadrel 25

26. #Non specific vasodilator (hydralazine, minoxidil) Hydralazine minoxidil 26

27. ❑Recent antihypertensive drugs AT1 ANTAGONIST ✓Olmesartan minoxidil ✓Azilsartan minoxidil 27

28. ➢Serotonin receptor antagonist Ketanserin: At higher conc. it inhibits α -1 adrenergic receptors. 28

29. ❖Endothelin receptor antagonist E.g.,ambrisentan,sitasenten,bosentan, darusentan. ✓Ambrisentan ✓Darusente n 29

30. ET-1 is a more potent vasoconstrictor than angiotensin II and has high affinity for the ETA receptor subtype which mediates the vasoconstriction characteristics of the Endothelin. 30

31. ➢Protein KinaseC inhibitors Staurosporin(antibiotic);it is a natural product isolated in 1977 from bacterium “streptomyces staurosporeus”. 31

32. ❑CALCIUM CHANNEL BLOCKER Cilnidipine Azelnidine Clevidipine 32

33. ❑BUCINDOLOL Non-selective β-blocker and weak α- blocker. Mild vasodilator. 33

34. ❑CHYMASE INHIBITORS Chymase inhibitors may be useful for preventing cardiovascular diseases and fibrosis via inhibition of angiotensin II formation and transforming growth factor-beta activation. E.g.,SPF-32629A 34

35. ❑PROSTACYCLINE ANALOGUE M/C:-Direct vasodilation of pulmonary and systemic arterial beds;also inhibits platelet aggregation. E.g.,Treprostinil 35

36. ❑CONTRAINDICATIONS Antihypertensive drugs are contraindicated in patients with known hypersensitivity to the individual drug ACEIs: Contraindicated in patients with impaired renal function, congestive heart failure, salt or volume depletion, bilateral stenosis, or angioedema, also during pregnancy or lactation Use of the ACEIs and the angiotensin II receptor blockers during the second and third trimester of pregnancy is contraindicated because use may cause fetal and neonatal injury or death 36

37. ❑SYNTHESIS OF NIFEDIPINE Claisen schmidt condensation 37

39. 39

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