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Pharmacology > Anti-hypertensive drugs > Flashcards

Anti-hypertensive drugs Flashcards

1
Q

List the classes of anti-hypertensive drugs (10)

A

1) Diuretics
2) Angiotensin-converting Enzyme (ACE) inhibitors
3) Angiotensin (AT1) blockers
4) Centrally acting
5) ß-adrenergic blockers
6) ß and α – adrenergic blockers
7) α – adrenergic blockers
8) Calcium Channel Blockers (CCB)
9) K+ Channel activators
10) Vasodilators

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2
Q

Diuretics MOA

A

diuresis – depletion of Na+ and body fluid volume – decrease in cardiac output

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3
Q

examples of diuretics used in hypertension.

A

thiazide- hydroclorothiazide
high ceiling-furosemides
potassium sparing diuretics

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4
Q

Thiazide diuretics – adverse effects

A

hint; hypers and hypoes
hypovolemia
hypokalemia
hyperuricemia
hyperglycemia
hyperlipidemia

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5
Q

K+ sparing diuretics as Anti-HTN

A

useful in combination therapy with thiazide,
Moduretic (Amiloride + HCT) is popular one

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6
Q

thiazide as Anti-HTN

A

Modified thiazide: indapamide
Indole derivative, long duration of action, It is a lipid neutral.

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7
Q

Loop diuretics as Anti-HTN

A

Used only in complicated cases – CRF, CHF marked fluid retention cases

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8
Q

Angiotensin Converting Enzyme (ACE) Inhibitors

A

Captopril,
Lisinopril
Enalapril
Ramipril

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9
Q

Captopril MOA

A

and abolishes pressor action of Angiotensin-I and not Angiotensin-II and does not block AT receptors

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10
Q

PKinetics of Captopril

A

Available only orally, 70% - 75% is absorbed
Partly absorbed and partly excreted unchanged in urine
Food interferes with its absorption
Half life: 2 Hrs, but action stays for 6-12 Hrs

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11
Q

Captopril – Pharmacological actions

A

Lowers PVR and thereby mean, systolic and diastolic BP
Initially correlates with renin-angiotensin status but chronic administration is independent of renin activity.
No effect on Cardiac output, contractility, heart rate
Postural hypotension is not a problem
Renal blood flow is maintained – greater dilatation of vessels

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12
Q

Indications for ACE inhibitors

A

diabetic nephropathy
myocardial infraction
heart failure
systolic dysfunction

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13
Q

Captopril – Adverse effects

A

Cough
Hyperkalemia
Hypotension
Acute renal failure
teratogenic
Angioedema
Rashes, urticaria
altered taste
Neutripenia

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14
Q

Contraindications for captopril

A

Pregnancy,
bilateral renal artery stenosis,
hypersensitivity
hyperkalaemia

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15
Q

Enalapril

A

It’s a prodrug – converted to enalaprilat
Advantages over captopril:
Longer half life
only ACE inhibitor available intravenously, Absorption not affected by food.

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16
Q

Ramipril

A

It is also a pro-drug with long half life
Tissue specific – Protective of heart and kidney
Uses: Diabetes with hypertension, CHF, AMI and cardio protective in angina pectoris

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17
Q

Lisinopril

A

It’s a lysine derivative
Not a prodrug
Slow oral absorption
Absorption not affected by food and not metabolized – excrete unchanged in urine
Long duration of action

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18
Q

Angiotensin Receptor Blockers (ARBs)

A

Losartan-specific AT1 blocker

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19
Q

Losartan (ARBs) MOA

A

These drugs block the AT1 receptors, decreasing the activation of AT1 receptors by angiotensin II and block aldosterone secretion, thus lowering blood pressure and decreasing salt and water retention.

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20
Q

Theoretical superiority over ACEIs

A

Cough & angioedema is rare –
no interference with bradykinin and other ACE substrates
Complete inhibition of AT1 – alternative remains with ACEs
Result in indirect activation of AT2 – vasodilatation (additional benefit)
Clinical benefit of ARBs over ACEIs – not known

21
Q

Pharmacokinetic of losartan

A

Absorption not affected by food but unlike ACEIs its bioavailability is low
High first pass metabolism
Highly bound to plasma protein

22
Q

ADRs of ARB (losartan)

A

like ACE Inhibitors

23
Q

Beta-adrenergic blockers

A

Non selective: Propranolol, nadolol
Cardioselective: Metoprolol, atenolol

24
Q

Beta-adrenergic blockers MOA

A

reduce blood pressure primarily by decreasing cardiac output. They may also decrease sympathetic outflow from the (CNS) and inhibit the release of renin from the kidneys, thus decreasing the formation of angiotensin II and the secretion of aldosterone.

25
Q

Adverse effects of beta-adregenic blockers

A

Bradycardia
BP drop
Bronchoconstriction
Cough, cognitive defects
Lipid metabolism disturbance,loss of libido
tiredness-fatigue
Vivid dreams

                         HINT;     BBC TV London
26
Q

Advantages of cardio-selective over non-selective

A

preferred over non-selective beta blockers in patients with;
In asthma
In diabetes mellitus
In peripheral vascular disease

27
Q

PKinetics of Beta-adregenic blockers

A

The β-blockers are orally active for the treatment of hypertension.
Propranolol undergoes extensive and highly variable first-pass metabolism. Oral β-blockers may take several weeks to develop their full effects. metoprolol, and propranolol are available in intravenous formulations.

28
Q

Αlpha-adrenergic blocker prototype

A

PRAZOSIN
Specific alpha-1 blockers like prazosin, terazosin and doxazosin are used

29
Q

Αlpha-adrenergic blockers MOA

A

BlockReduction in peripheral resistance and mean BP
Does not produce tachycardia.

30
Q

Adverse effects of alpha-bk

A

postural hypotension
Fluid retention in monotherapy
Headache,
dry mouth,
weakness,
blurred vision, rash, drowsiness and failure of ejaculation in males

31
Q

advantages of prazosin

A

improvement of carbohydrate metabolism – diabetics, lowers LDL and increases HDL, symptomatic improvement in BHP

32
Q

Classes of calcium channel blockers

A

check your note

33
Q

Calcium Channel Blockers – Mechanism of action

A

block L-type calcium channels, causing vascular smooth muscle to relax, dilating mainly arterioles. Calcium channel blockers do not dilate veins

34
Q

Advantages of CCB

A

no adverse metabolic effects
Can be given to asthma, angina and PVD patients
No renal and male sexual function impairment
No teratogenic effect

35
Q

ADRs of CCB

A

hypotension and heart failure
cardiac depression + dizziness
pulmonary oedema
constipation
gingival hyperplasia

hint; Happy DEC

36
Q

. Pharmacokinetics of CCB

A

Most of these agents have short half-lives following an oral dose. Sustained-release preparations are available and permit once-daily dosing. Amlodipine has a very long half-life and does not require a sustained-release formulation.

37
Q

Vasodilators - Hydralazine MOA:

A

hydralazine molecules combine with receptors in the endothelium of arterioles – NO release – relaxation of vascular smooth muscle – fall in BP

38
Q

ADR of hydralazine

A

anginal attack
Tachycardia
Increased Renin secretion- Na+ and water retention
These effects are countered by administration of beta blockers and diuretics

39
Q

Vasodilators - Minoxidil MOA

A

Pro-drug and converted to an active metabolite which acts by hyperpolarization of smooth muscles and thereby relaxation of SM causing vasodilation.

Powerful vasodilator, mainly 2 major uses – antihypertensive and alopecia
Rarely indicated in hypertension
More often in alopecia to promote hair growth

40
Q

Sodium Nitroprusside MOA

A

RBCs convert nitroprusside to NO causing vasodilation

41
Q

Uses of vasodilators

A

: Hypertensive Emergencies

42
Q

ADRs of Vasodilators

A

palpitation, pain abdomen, disorientation, psychosis, weakness and lactic acidosis.

43
Q

examples of vasodilators

A

hydralazine
sodium nitroprusside
minoxidil

44
Q

Centrally acting drugs

A

Methyldopa
Clonidine

45
Q

Alpha-Methyldopa: a prodrug
Precursor of Dopamine and NA
Mode of action?

A

Converted to alpha- methyl noradrenaline which acts on alpha-2 receptors in brain and causes inhibition of adrenergic outflow in medulla – fall in PVR and fall in BP

46
Q

Various adverse effects of alpha-Methyldopa

A

cognitive impairment, drowsiness and sedation
postural hypotension, positive coomb`s test etc.
Useful in hypertension during pregnancy

47
Q

Treatment of Hypertension in pregnancy,
list the drugs to avoid (4) and safe drugs (4)

A

No drug is safe in pregnancy
Avoid diuretics, propranolol, ACE inhibitors, Sodium nitroprusside etc
Safer drugs: Hydralazine, Methyldopa, cardioselective beta blockers and prazosin

48
Q

drugs used for Hypertensive Emergencies

A

Sodium Nitroprusside
Hydralazine
Labetalol

Pharmacology (11 decks)

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