complete information about antihypertensive drugs

1. UNDER THE GUIDENCE OF:
Ms. G. USHA SREE
Asst.Prof
Dept. Of Pharmaceutical Analysis.
SEMINAR BY:
SUSHMITHA.K
11T21R0070.
CMR COLLEGE OF PHARMACY

2. Contents
 Introduction
 Classification of hypertension
 Types
 Signs and symptoms
 Causes
 Classification
 Treatment
 Conclusion
 References

3. Introduction
Hypertension
Systolic Blood
Pressure (SBP)
Diastolic Blood
Pressure (DBP)
> 140 mmHg > 90 mmHg

4. Classification of hypertension:
Systolic B.P. Diastolic B.P.
Normal < 120 <80
Pre Hypertension 120-139 80-89
Stage I 140-159 90-99
Stage II ≥160 ≥100

5. sphygmomanometer

6. Types
Types of
Hypertension
Essential Secondary
disorder of unknown origin affecting the
Blood Pressure regulating mechanisms
Secondary to other disease processes

7. Signs and symptoms
 Severe headache
 Fatigue or confusion
 Vision problems
 Chest pain
 Difficulty in breathing
 Irregular heartbeat
 Blood in urine
 Pounding in your chest, neck or ears
 Hypertensive crisis may lead to heart attack or stroke

8. Causes

9. A.Primary Hypertension
 It is present in 95%of the population
No defective cause
Build of fatty deposits inside arteries (atherosclerosis)
Thickening of artery walls
Excessive contraction of small arteries (arterioles)

10. B. Secondary hypertension
 It occurs in about 5-10% of the population
 It develops through manifestation of other medical problems
like
 Renal problems
 Harmonal disorders
 Heart problems
 Sleep apnea
 Over the counter drugs
 Obsety
 Alcohol
 Genitics
 stress

11. Mechanisms for controlling blood
pressure
 1. Baroreceptors and the sympathetic nervous
system
 2. The Humoral Renin Angiotensin
Aldosterone System

12. Baroreceptors and the sympathetic nervous
system

14. Classification:
ANTI-HYPERTENSIVE DRUGS
Diuretics ACE Inhibitor
Angiotensin
receptor
Blocker
Direct
Renin
Inhibitor
Calcium
channel
Blocker
Alpha
Adrenergic
Blockers
Beta
Adrenergic
Blockers
α + β
Adrenergic
Blockers
Central
Sympatholytic
Vasodil-
ators
Thiazide,
High-
ceiling,
K+ sparing
Losartan,
Valsartan
Aliskiren
Verapamil,
Diltiazem,
Nifedipine
Prazosin,
Terazosin,
Doxazosin
Propronolo
Metaprolol
Atenolol
Labetalol,
Carvedilol
Clonidine
Methyldopa
Hydralazine,
Minoxidil
Sodium
nitroprusside
Captopril
Enalapril
lisnopril

15. DIURETICS
 Diuretics can be used as first-line drug therapy for
hypertension.
 Prevent stroke, myocardial infraction and congestive
heart failure.
 Diuretics are superior to β-blockers for treating
hypertension in older patients.
 Diuretics are classified in to:
Thiazide diuretics
High ceiling diuretics and
K + sparing diuretics

16. Thiazide diuretics
 The diuretic of choice for uncomplicated hypertension.
Mechanism of action:

17. Pharmacokinetics:
 Orally active.
 Absorption and elimination rates may vary.
 All thiazides are ligands and compete with uric acid for
elimination.
Therapeutic uses:
• Particularly useful in treatment of black and elderly
patients.
 They decreases blood pressure in both supine and
standing position.
 They do not cause reflex tachycardia or reduce the
cardic output.

18. Adverse effects:
 Thiazides diuretics induce hypokalemia and
hypouricemia in 70% of patients and hypoglycemia in
10% of patients.
 Acute gout disorders may be triggered.
 Hypomagnesaemia may also occur.
 Serum potassium levels should be monitored closely
in patients who are predisposed to cardiac
arrhythmias.

19. High ceiling diuretics
 Furosimide, the prototype of this class, is a strong
diuretic.
 They cause decreased renal vascular resistance and
increased renal blood flow.
 They are more liable to cause fluid and electrolyte
imbalance, weakness and other side effects.
 Indicated in hypertension only when it is
complicated by :
Chronic renal failure.
Coexisting refractory congestive heart failure.

20. Potassium sparing diuretics
 Spironolactone, amiloride, eplerenone lower blood
pressure slightly.
 They are used only in conjunction with a thiazide
diuretic to prevent K+ loss and to aggument the
anti-hypertensive action.
 Hyperkalemia should be watched when K+ sparing
diuretics are used with ACE inhibitors/ARBs.

21. Angiotensin converting enzyme (ACE)
inhibitors
Mechanism of action:
Angiotensin-I
Angiotensin-II
Angiotensin-II
Na+ and water level
Angiotensin
converting
enzyme
Cardiac work
and blood
pressure

22. Pharmacokinetics:
 Orally well absorbed.
 Prescence of food in stomach reduces its
bioavailability.
 Penetration in brain is poor.
 It is partly metabolized and excreted unchanged in
urine.
 The plasma t1/2 is 2 hours.
Therapeutic uses:
 Hypertension
 Chronic congestive heart failure
 Diabetic nephropathy

23. Adverse effects:
 Dry persistent cough
 Skin rashes, fever, altered taste, hypotension and
hyperkalemia.
 Potassium levels must be monitored.
 They can induce fetal malformation.
 Contraindications:
Severe renal artery stenosis.
Aortic stenosis
Coarctation of the aorta.
pregnancy.

24. Direct Renin Inhibitor
o Aliskiren is a selective renin inhibitor.
Mechanism of action:

25. Pharmacokinetics:
 It is administered orally, but bioavailability is very low.
 It is mainly eliminated in faeces, small amount in urine.
 The plasma t1/2 is >24 hours.
Therapeutic uses:
 It lowers blood pressure as effective as ARBs, ACE
inhibitors and thiazides.
 Combined with diuretics, calcium-channel blockers, ACE
inhibitors, and with ARBs.
Adverse effects:
 Dyspepsia, abdominal pain, loose motions, headache, and
dizziness.
 Acute hypotension, hyperkalaemia, cough, angioedema
 It is contraindicated during pregnancy.

26. Calcium Channel Blockers
 Calcium channel blockers are recommended when the
preferred first-line agents are ineffective or
contraindicated.
 They are effective in treating hypertension in patients
with angina or diabetics.
Three important classes of Calcium channel blockers
are:
 Diphenylalkylamines: Verapamil (a hydrophilic
papaverine congener)
 Benzothiazepine: Dilthiazem (hydrophilic)
 Dihydropiridines: Nifedipine (lipophilic)

27. Mechanism of action:

28. Verapamil:
 It dilates arterioles and has some α-adrenergic
blocking activity.
 It has significant effect in both cardiac and vascular
smooth muscle cells.
 It is used to treat angina, supra ventricular
tachyarrthymias and migraine and cluster headache.
 Adverse effects are nausea, constipation and
bradycardia.
 Interactions- i. It should not be given with β-blockers
ii. It increases plasma digoxin level
iii. It should not be used along with
other cardiac depressants like quinidine.

29. Pharmacokinetics:
 Most of calcium-channel blockers have short half-lives (3-
8hours) following an oral dose.
 Amlodipine has a very long half life.
Therapeutic uses:
 Used as one of the first line monotherapy.
 They are preferred in elderly and black hypertensive
patients.
 Useful in treatment of asthma, angina.
Adverse effects:
 Constipation occurs in 10% 0f patients with verapamil.
 Dizziness, fatigue are more frequent with verapamil.
 Verapamil should be avoided in patients with congestive
heart failure due to its negative ionotropic and
dromotropic effects.
 Nifedipine cause gingival enlargement.

30. TREATMENT OF HYPERTENSION
 Hypertension is treated by:
Combination therapy
Oral therapy
Parentral therapy.

31. ANTI-HYPERTENSIVE COMBINATIONS
 Amlodipine 5mg + Lisnopril 5mg - AMLOPRES-L,
LISTRIL-AM
 Amlodipine 5mg + Atenolol 50mg – AMCARD-AT,
AMLOPIN-AT, AMLOPRES-AT
 Amlodipine 5mg + Enalopril 5mg – AMACE, AMTAS-E
 Atenolol 25mg or 50mg + Chlorthalidone 12.5mg –
TENOCLOR, TENORIC
 Enalapril 10mg + Hydrochlorothiazide 25mg –
ENACE-D, VASONORM-H
 Rampril 2.5mg + Hydrochlorothiazide 12.5mg –
CARDACE-H
 Losartan 50mg + Hydrochlorothiazide 12.5mg –
LOSAR-H, TOZAARH-H, LOSACAR-H

32. ANTI-HYPERTENSIVES TO BE AVOIDED DURING
PREGNANCY:
SL.NO DRUGS RISK
1. ACE Inhibitors, ARBs Foetal damage
2. Diuretics Reduce blood volume, placental infraction
3. Nonselective β-blockers neonatal bradycardia, hypoglycaemia.
4. Sodium nitroprusside Contraindicated in eclampsia.
SL.NO. DRUGS
1. Methyldopa
2. Dihydropyridine
3. Cardio selective beta-blocker
4. Prazosin, clonidine
ANTI-HYPERTENSIVES FOUND SAFER DURING
PREGNANCY:

33. HYPERTENSIVE EMERGENCIES AND URGENCIES:
 Cerebrovascular accident or head injury with high
blood pressure
 Hypertensive encephalopathy
 Hypertensive acute left ventricular failure and
pulmonary edema
 Unstable angina or myocardial infraction with raised
blood pressure
 Dissecting aortic aneurysm
 Acute renal failure with raised blood pressure
 Eclampsia
 Hypertensive episodes in pheochromocytoma.

34.  ORAL THERAPY:
NIFEDIPINE:
 10 mg soft geletine capsules
 Oral or sub-lingual administration for every 30 mins
 Causes fall in blood pressure, myocardial infraction or
stroke
CAPTOPRIL:
 25 mg orally for every 1-2 hours
 Response is variable
 Carries risk of excessive hypotension
CLONIDINE:
 100 µg orally for every 1-2 hours
 Produces sedation
 Rebound rise in blood pressure on stopping the drug.

35. PARENTRAL THERAPY:
SL.NO. DRUG Route of administration
and dose
1. Sodium nitroprusside Intravenous, 20-30µg/min
2. Glyceryl trinitrate Intravenous, 5-20 µg/min
3. Esmolol Intravenous,50-10µg/kg/min
4. Phentolamine Intravenous, 5-10 mg
5. Furosemide Oral/Intravenous,20-80 mg

36. Preparations available:
 Captopril (generic, capotus)
Oral-12.5, 25,100 mg tablets.
Parenteral (Enalaprilat)-12.5 mg/ml for injection
 Losartan (lozaar)
Oral- 25, 50,100 mg tablet
 Verapamil (generic, calan, Isoptin)
Oral- 40, 80, 120 mg tablet
 Diltiazem (generic, cardizem)
Oral- 30, 60, 90, 120 mg tablet
Parenteral- 5 mg/ml for injection
 Nitroprusside (generic, Nitropress)
Parenteral- 50 mg/vial.

37. Conclusion:
 Hypertension is a common disorder in adults.
 Now a days it was common problem seen in youngsters
mainly due to changes in life style modifications,
obesity and hereditary.
 Maintenance of a healthy life style and proper follow
up of non-pharmacological treatment like food habits,
regular exercise can overcome the usage of anti
hypertensive drugs.
 Normalize blood pressure and prevent complications.

38. References:
 Barar F.S.K, Anti-Hypertensive drugs. Essentials of
Pharmcotherapeutics, 2007.4th edition. Pg. 239-249.
 Lippincott Williams and Wilkins, Anti-Hypertensive drugs.
Pharmacology, 2012.5th. Pg. 227-242.
 Rang and Dale, Anti-Hypertensive drugs. Pharmacology,
2007.6th edition. Pg. 311-312.
 Satoskar R.S, Bhandarkar S.D, Nirmala N.Rege, Anti-
Hypertensive drugs. Pharmacology and
Pharmcotherapeutics, 2009.21th edition. Pg. 404-433.
 Tripathi KD, Anti-Hypertensive drugs. Essentials of
Medicinal Pharmacology, 2013.7th edition. Pg. 558-574.
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