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CVS & IBL - Pharmacology ๐Ÿ’Š > L1: Antihypertensive drugs > Flashcards

L1: Antihypertensive drugs Flashcards

1
Q

Why should hypertension be treated even if it was asymptomatic?

A

a) Damage to the vascular epithelium, paving the path for atherosclerosis, IHD, or nephropathy due to high intra-glomerular pressure
b) Increased load on heart due to high BP can cause CHF

โ€ุงุฑุชูุงุน ุงู„ุถุบุท ุญุชู‰ ู„ูˆ ู…ุด ู…ุณุจุจ ุฃุนุฑุงุถ ู„ูƒู† ู…ู…ูƒู† ูŠุคุฏูŠ โ€ู„ุชุตู„ุจ
ุงู„ุดุฑุงูŠูŠู† ูˆู…ุดุงูƒู„ ููŠ ุงู„ูƒู„ูŠุฉ

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2
Q

What are the types of hypertension?

A
  • According to the cause:
  • Essential hypertension. โ€œPrimary (90%)โ€
  • Secondary hypertension

According to the degree:

  • Normal blood pressure โ‰ค120 โ‰ค80
  • Stage 1 Hypertension 140โ€“159 90โ€“99
  • Stage 2 Hypertension 160โ€“179 100โ€“109
  • Stage 3 Hypertension โ‰ฅ180 โ‰ฅ110
  • Isolated systolic hypertension>140 <90
    โ€œISH respond more to CCBsโ€

โ€œMore than stage 3 โ€”-> hypertensive emergencyโ€

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3
Q

What is essential hypertension?

A
  • A disorder of unknown origin affecting the blood pressure regulating mechanisms
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4
Q

What is secondary hypertension?

A
  • Secondary to other disease processes
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5
Q

What is the target blood pressure for hypertensive patients?

A
  • For most patients, the goal of therapy is to maintain BP < 140/90 .
  • In patients with DM or chronic kidney disease, BP should be < 130/80
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6
Q

What does blood pressure equals?

A
  • Blood Pressure = (CO) X (PVR)
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7
Q

How is blood pressure physiologically maintained?

A
  • Physiologically BP is maintained by
    1) Arterioles
    2) post capillary venules
    3) Heart
    4) Kidney (volume of intravascular fluid)
  • Baroreflex and renin-angiotensin- aldosterone system regulates the above 4 sites
  • Local agents like Nitric oxide
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8
Q

What is abnormal about baroreflex and Renal blood volume control system in hypertensive patient?

A
  • Baroreflex and renal blood-volume control system set at higher level
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9
Q

How do all antihypertensive drugs work?

A
  • All antihypertensives act via interfering with normal mechanisms.
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10
Q

How is hypertension generally treated?

A

1) Non-drug therapy or life style modification

2) Anti-hypertensive drugs

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11
Q

What is non-drug therapy of hypertension?

A

1) Non-drug therapy or life style modification:
- Sodium restriction and potassium and Mg supplementation.
- Stop smoking and avoid stress.

  • Exercise and Weight reduction of obese patients.
    Control of risk factors: e.g. DM, hyperlipidemia, and obesity.
  • Avoid drugs that โ†‘ BP e.g.: sympathomimetics, sodium-containing drugs, oral contraceptives, corticosteroids.
  • Patients failing to normalize BP after 2 weeks of nonpharmacological therapy should be considered for drug treatment in addition to non drug therapy
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12
Q

What are antihypertensive drugs?

A

First choice groups (commonly used drugs):

  • ACEIs
  • Beta-blockers โ€œ2nd Lineโ€
  • Calcium blockers
  • Diuretics

Second choice groups (used in special cases):

  • ฮฑ1- blockers: prazosin.
  • Combined ฮฑ and ฮฒ-blockers: labetalol.
  • Adrenergic neuron blockers: ฮฑ-methyldopa.
  • Vasodilators: hydralazine and diazoxide.
  • Central ฮฑ2 stimulants: clonidine.
  • Dopamine agonists: fenoldopam.
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13
Q

Should RAAS be inhibited?

A
  • Inhibition of RAAS will correct hypertension but also will โ†“ GFR and aggravate RF if renal ischemia was grave (S. creatinine is > 3 mg/dl).
  • So, if S. creatinine is up to 3 mg/dl (mild renal impairment) โ†’ you can safely block RAAS.
  • If creatinine>3 mg/dl (severe renal impairment) โ†’ blocking RAAS will aggravate RF.
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14
Q

what is the classification of ACE inhibitors?

A
  • SH-Containing drugs: Captopril

SH group may be responsible partially for immunological side effects โ€œATSLโ€ e.g. angioedema, taste changes, skin rash and leukopenia.

  • Non SH-Containing drugs: โœ“ Enalarpril โœ“ fosinopril โœ“ lisinopril โœ“ benazepril โœ“ ramipril

โ€œFELRBโ€

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15
Q

What is the mechanism of action of ACE inhibitors?

A
  • They inhibit Ang-converting enzyme leading to Inhibition of Ang-II formation.
  • Also they Prevent degradation of bradykinin which is a potent VD.
  • ACEIs have direct arterio-veno dilator effects.
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16
Q

What are the pharmacological effects of ACE inhibitors?

A

1) They โ†“ BP mainly by decreasing peripheral resistance
2) In presence of CHF, they โ†‘ COP due to reduction of both venous return (preload), and systemic BP (afterload).
3) They prevent cardiac remodeling โ€œafter MIโ€

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17
Q

What are the therapeutic uses of ACE inhibitors?

A

1) Systemic hypertension
2) Prevent LV remodeling after acute MI
3) Congestive heart failure (CHF)
4) Diabetic nephropathy & microalbuminuria

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18
Q

How do ACE inhibitors treat diabetic nephropathy and microalbuminuria?

A
  • They โ†“ renal changes complicating diabetic nephropathy (mesangial cell apoptosis, proliferation, and collagen synthesis)
  • thus reducing microalbuminuria (provided that renal impairment is not grave).
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19
Q

What are the adverse effects of ACE inhibitors?

โ€œNo reflex tachycardiaโ€

A

1) Dry Cough (the most common)
2) Angioedema (edema of the face and throat)
3) Aggravation of Proteinuria in patients with significant renal failure.
4) Taste changes
5) Orthostatic (First dose) hypotension
6) Teratogenesis (fetal pulmonary hypoplasia)
7) Skin rash.
8) Increased K+(hyperkalemia) due to โ†“aldosterone release. โ€œShould be used with K losing diureticsโ€

โ€œAOT ATSL DryKโ€

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20
Q

What are the precautions that should be followed while using ACE inhibitors?

A
  • Start with small dose at bedtime.
  • Frequent monitoring of kidney functions (S. creatinine) and potassium levels one week after treatment and then every 3 months.
  • Avoid use of K+ sparing diuretics.
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21
Q

What are the contraindications of ACE inhibitors?

A

1) Hypotension: when systolic BP is less than 95 mm Hg.
2) Severe renal failure or bilateral renal artery stenosis (SCr> 3 mg/dl).
3) Pregnancy and lactation.
4) Hyperkalemia.

5) Neutropenia, thrombocytopenia, or severe anemia.
โ€œSuppresses BMโ€

6) Immune problems.

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22
Q

What are examples of ARBs?

A

Losartan - Valsartan

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23
Q

What is the mechanism of action of ARBs?

A
  • They selectively block AT1 receptors.
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24
Q

How do ARBs have more efficacy than ACE inhibitors?

A
  • ACE inhibitors are Less effective because other enzymes rather than ACE can convert Ang-I into Ang-II
  • ARBs are More effective because it blocks AT-1 receptor, the final station responsible for Ang-II effects.
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25
Q

Is cough and angioedema common with ARBs?

A
  • Less frequent (they do notโ†‘bradykinins)
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26
Q

Give an example for direct renin inhibitor.

A

Aliskiren

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27
Q

What is a mechanism of action of Aliskirin?

A
  • It inhibits renin activity and consequently the RAAS.
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28
Q

When is Aliskiren used?

A
  • Aliskiren is a recently approved drug for treatment of hyperreninemic hypertension.
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29
Q

What is the rate limiting step in the formation of RAAS?

A
  • Activation of angiotensinogen into Ang-I by renin is the rate limiting step in formation of RAAS.
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30
Q

What is the efficiency and side effects of Aliskirin comparable to?

A
  • The efficacy and side effects of aliskiren are comparable to ACEIs and ARBs.
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31
Q

Revise the comparison between ACE inhibitors and ARBs

A

..

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32
Q

What is the mechanism of action of calcium channel blockers?

A
  • block L type voltage-gated Ca2+ channels.

โ€ Donโ€™t affect skeletal muscles as they have calcium from inside unlike cardiac and smooth muscles which have there calcium from outsideโ€

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33
Q

What is the classification of calcium channel blockers?

A

According to tissue selectivity

  • CCB with mainly cardiac effects: verapamil, diltiazem.
  • CCB with mainly vascular effects (dihydropyridines): nifedipine, amlodipine
  • CCB with main effect on other tissue: flunarizine, cinnarizine.
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34
Q

What is the mechanism of action of nifedipine and amlodipine?

โ€œAmlodipine has higher duration and lower efficacyโ€

A
  • selective blockade of vascular Ca channels leads to vasodilatation which lower PVR and BP
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35
Q

Which group of drugs has the highest smooth muscle relaxation and vasodilation action?

A
  • DHPs have highest smooth muscle relaxation and vasodilator action followed by verapamil and diltiazem
36
Q

What are the uses of Nifedipine /Amlodipine?

A
  • Hypertension
  • preterm labour
  • Peripheral vascular diseases

โ€œHPPโ€

37
Q

What are the adverse effects of Nifedipine /Amlodipine?

A
  • Hypotension with reflex tachycardia with short acting version (not with nifedipine SR or amlodipine)
  • Gum hyperplasia
  • Ankle edema (due to salt and water retention by stimulated aldosterone release as physiological adaptation to hypotension
    โœ“ Best managed by salt restriction, avoid prolonged standing and diuretics)

โ€œHGAโ€

38
Q

What are the contraindications of Nifedipine /Amlodipine?

A

1) Hypotension

2) Hypertrophic obestructive cardiomyopathy (HOCM)
(as reflex tachycardia increase outflow obstruction)

3) Unstable angina (as reflex tachycardia increases the work of the heart and cardiac demands which may precipitate MI)
4) Supraventrecular tachycardia (SVT) (as reflex tachycardia may precipitate VT)

โ€œHHATโ€

39
Q

What is the mechanism of action of Verapamil, diltiazem?

A
  • Blockade of Ca channels in the vasculature, heart muscle and the AV node
40
Q

What are the main effects of Verapamil, diltiazem?

A
  • Negative ionotropic and chronotropic effects in heart
41
Q

What are the uses of Verapamil, diltiazem?

โ€œContraindications of nifedipineโ€

A

1) Ischemic heart diseases (as they decrease work of the heart ,produce coronary vasodilatation and decrease Ca causing apoptosis around the site of infarction)

2) Cardiac arrhythmias SVT
(as they cause AVN delay protecting the ventricles from the high rate of atria)

3) HOCM (as they decrease the force of ventricle contraction decreasing aortic outlet outflow obstruction)
4) Hypertension โ€œlast use as they are more effiecint on the heartโ€

42
Q

What are the adverse effects of Verapamil, diltiazem?

A
  • Bradycardia and heart block
  • Worsening of heart failure โ€œunlike ACE inhibitorsโ€
  • Constipation โ€œDue to relaxationโ€
43
Q

What are the contraindications of Verapamil, diltiazem?

A
  • Bradycardia and heart block
  • Wolff-Parkinson-white syndrome (as they decrease AV nodal conduction, this stimulates passage of impulses through accessory conducting pathway between atria and ventricles causing atrioventricular re-entry tachycardia in WPWS)
44
Q

What are the drug interactions of Verapamil, diltiazem?

A
  • Caution for AV block with beta blockers, and digitalis (may precipitate heart block, nifedipine is best choice in such combination)
45
Q

What are the types of diuretics?

A

1) Thiazides: Hydrochlorothiazide, chlorthalidone
2) High ceiling: Furosemide
3) K+ sparing: Spironolactone, triamterene and amiloride

46
Q

What is the mechanism of action of diuretics?

A
  • Acts on Kidneys to increase excretion of Na and H2O โ†’ decrease in blood volume โ†’ decreased BP
47
Q

How is essential hypertension treated by diuretics?

A
  • Low dose of thiazide can be used as initial therapy in essential hypertension
  • Preferably should be used with a potassium sparing diuretic (for additive effect and correction of hypokalemia)
  • If therapy fails โ€“ another antihypertensive but do not increase the thiazide dose
48
Q

When are loop diuretics used for treatment of hypertension?

A
  • Loop diuretics are to be given when there is severe hypertension, complicated cases โ€“ CRF, CHF with retention of body fluids
49
Q

What are examples of beta blockers used in lowering blood pressure?

A
  • Propranolol is used in stage 1 and 2 HT alone or in combinations with a diuretic and/or vasodilator.
  • Labetalol can be given i.v. for hypertensive emergencies
50
Q

What is the mechanism of action of beta blockers and lowering blood pressure?

โ€œCRAB VPโ€

A

1) Decrease (C)OP (-ve inotropic and chronotropic)
2) Decrease (r)enin release
3) Decreased (NE) release (blocks presynaptic 2 receptors)
4) Reconditioning of (b)aroreceptors.
5) Increase (p)rostaglandins.
6) Some blockers have (v)asodilator properties.

51
Q

What is the classification of vasodilators?

A

Arterio- dilators
Veno- dilators
Mixed dilators

52
Q

What are arterial dilators, their mechanism of action and uses?

A
  • Nifedipine โ€“ Hydralazine โ€“ Minoxidilโ€“ Diazoxide
  • They dilate arteries and โ†“โ†“ BP (โ†’โ†“ afterload)
  • They are used in severe systemic hypertension.
53
Q

What are veno-dilators, their mechanism of action and uses?

A
  • Nitrates
  • They dilate mainly veinsโ†’โ†“ venous return (โ†’โ†“ preload) ๏ผ
  • They are used in acute pulmonary edema.
54
Q

What are mixed dilators, their mechanism of action and uses?

A
  • Na nitroprussideโ€“ Prazosin โ€“ ACEIs
  • They โ†“ preload & afterload
  • They are used in CHF.
55
Q

What are the general effects of vasodilators?

A
  • โ†“ B. P โ†’ reflex sympathetic ++ โ†’ ฮฒ1 ++โ†’ HT โ†’ โ†‘ all cardiac propertiesโ†’ โ†‘ HR (palpitation), โ†‘ COP blocked by Beta blockers.

Kidney

  • โ†‘ renin secretion.
  • cause salt & H2O retention.
56
Q

What is the mechanism of action of minoxidil?

A
  • direct arteriodilator by opening K+ channelsโ†’ hyperpolarization โ†’ relaxation of the vascular smooth ms.

โ€œPrevent APโ€

57
Q

What are the uses of minoxidil?

A
  • Chronic hypertension (oral) .
58
Q

What are the side effects of minoxidil?

A
  • stimulate hair growth (hypertrichosis), so it is used topically to prevent hair loss.
59
Q

What is the mechanism of hydralazine?

A
  • direct arterio-dilator.
60
Q

What are the uses of hydralazine?

A
  • severe hypertension and hypertension in pregnancy.
61
Q

What are the side effects of hydralazine?

A
  • SLE like syndrome in slow acetylators.
  • Mild arthritis,
  • Renal impairment
  • Skin rash.

โ€œAuto-immuneโ€

62
Q

What is the mechanism of diazoxide?

A
  • It is a direct arteriolo dilator by opening K+ channelsโ†’ hyperpolarization โ†’ relaxation of the vascular smooth ms.
63
Q

What are the uses of diazoxide?

A
  • It is given parenterally in hypertensive emergencies
64
Q

What is the mechanism of sodium nitroprusside?

A
  • It liberates nitric oxide (NO)โ†’โ†‘cGMPโ†’ dilatation of both arteries and veins
65
Q

What are the uses of sodium nitroprusside?

A
  • It is given by i.v. infusion in hypertensive emergency and acute heart failure
66
Q

What are the side effects of sodium nitroprusside?

A
  • It can be converted to cyanide and thiocyanate.

- Accumulation of cyanide is minimized by sodium thiosulfate or hydroxocobalamin (vitamin B12).

67
Q

What is the structure of Diazoxide related to?

A
  • Structurally related to thiazides but it is not diuretic
68
Q

What is the mechanism of action of fenoldopam?

A
  • It stimulates peripheral dopamine (D1) receptors in renal and mesenteric arteries, leading to VD and decrease peripheral resistance.

โ€œInc work of kidneyโ€

69
Q

What are the uses of fenoldopam?

A
  • It is used parenterally as a rapid-acting vasodilator to treat emergency hypertension in hospitalized patients.
70
Q

What are the drugs used in emergency hypertension?

A
  • Loop diuretics
  • Labetolol
  • Hydralazine
  • Diazoxide
  • Na Nitroprusside
  • Fenoldopam
71
Q

What is the drug used in essential HTN?

A
  • Patient <55 years old: ACEIs Patient
  • > 55 years old: CCBs โ€œas they are more likely to have heart problemsโ€
  • If not adequate, add thiazide or BB.
72
Q

What is the drug used in HTN + Pregnancy?

A

ฮฑ-methyldopa, Labetalol, Nifedipine, Hydralazine

73
Q

What is the drug used in HTN + Diabetic nephropathy?

A

ACE inhibitors

74
Q

What is the drug used in HTN + DM?

A

ACEIs - ARBs

โ€œBeta blockers are CIโ€

75
Q

What is the drug used in HTN + CKD?

A
  • S. creatinine<3 mg/dl: ACEIs

- S. creatinine>3 mg/dl: CCBs

76
Q

What is the drug used in HTN + CHF?

A

ACE inhibitors - diuretics

77
Q

What is the drug used in HTN + HF?

A

ACEIs - ARBs - Beta Blockers

78
Q

What is the drug used in HTN + BA?

A

CCBs

โ€œBeta blocker and ACEIs are CIโ€

79
Q

What is the drug used in HTN + Angina?

A

CCBs - beta-blockers

80
Q

What is the drug used in HTN + thyrotoxicosis, sympathetic overactivity, or young patient with high plasma renin?

A

Beta-blockers

โ€œTo reduce the work of the heartโ€

81
Q

What is the drug used in HTN + BPH?

A

ฮฑ1 blockers

82
Q

What is the drug used in pulmonary hypertension?

A

Endothelin receptor antagonists

83
Q

What is the drug used in post myocardial infarction hypertension?

A

Beta Blockers

84
Q

What is the drug used in dyslipidemias?

A

Alpha Blockers - CCBs - ACEIs - ARBs

85
Q

How is hypertensive emergency treated?

โ€œIn stepsโ€

A
  • Hospitalization
  • Reduction of BP should be in hours and not in minutes
  • Drugs commonly used:
    1. Na nitroprusside, labetalol, fenoldopam, by slow i.v. infusion. โ€œNLFFโ€
  1. Furosemide in volume overload (pulmonary edema & acute HF)
  2. Avoid Nifedipine, nitroglycerin, and hydralazine (rapid decrease of BP) โ€œNo NNHโ€

CVS & IBL - Pharmacology ๐Ÿ’Š (6 decks)

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