Anti Hypertensives Flashcards by Iseoluwa Ojo

Hypertension is diagnosed if blood readings ___-___ or above on __________

140/90

Two different days

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Most common cardiovascular disease

Hypertension

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Hypertension is (Symptomatic or Asymptomatic?) in most cases.

Asymptomatic

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____________ people worldwide have hypertension

1.13 billion

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___% of adult population in the U.S have hypertension

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Hypertension is more prevalent where?
Nigeria or US

Nigeria

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Hypertension is More prevalent in Nigeria ___-___%.

25- 30

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Physiology of Blood pressure

BP = ___________ X _______

Cardiac Output X Peripheral Vascular Resistance.

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Physiology of Blood pressure

Arterial pressure affected by:

the ______ system (fast)

– the _______ system (hours or days)

the _______ (days or weeks)

autonomic nervous

renin-angiotensin

kidneys

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Classification of anti-hypertensive by site or mechanism

A. _______ drug
B.___________
C._________
D._________
E. _______
F. ________

Sympatholytic

Calcium channel blockers (CCB)

Angiotensin-converting enzyme Inhibitors(ACEI)

Angiotensin II receptor antagonists (ARB)

Vasodilators

Diuretics

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Mechanism of action

Sympatholytic drug

_______ of sympathetic activities and _______

Blockade

decrease in peripheral resistance

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Mechanism of action

Calcium channel blockers (CCB)
_______ of _______ in to _________ cells, resulting in a _______

inhibition

calcium influx

arterial smooth muscle ; decrease in peripheral resistance.

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Mechanism of action

Angiotensin-converting enzyme Inhibitors(ACEI)

_______ angiotensin converting enzyme that ______________ to _________

inhibits

hydrolyzes angiotensin I (Inactive) to angiotensin II (Active)

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Mechanism of action

Angiotensin II receptor antagonists (ARB)

______ Angiotensin II receptor, resulting in a _________________

Inhibit

decrease in peripheral resistance

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Mechanism of action

Vasodilators
Dilate arterial and venous blood vessels, resulting in a _______________

decrease in peripheral resistance.

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Mechanism of action

Diuretics
lower blood pressure by ________ and ________

depleting the body sodium and reducing blood volume

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Sympatholytic drugs

B1 selective blockers

List them

Acebutolol

Atenolol

Betaxolol

Bisoprolol Esmolol Metoprolol Nebivolol

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Sympatholytic drugs

Non-selective β1/β2

Listtttt

Carvedilol
Labetalol
nadolol
penbutolol
pindolol
Propanolol
Sotalol
Timolol

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Sympatholytic drugs

α Adrenergic receptor antagonist (alpha blockers):

Listtttt

Doxazosin
Phentolamine
Indoramin
Phenoxybenzamine

Prazosin
Terazosin
Tolazoline

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Sympatholytic drugs

Mixed adrenergic antagonist:

List 3

Carvedilol

Labetalol

Bucindolol

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Sympatholytic drugs

Centrally acting agent/ α2 receptor agonist:

List 5

α –Methyldopa
Clonidine
Guanabenz
Guanfacine
Moxonidine

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Sympatholytic drugs

Adrenergic neuron blockers:

Reserpine

Guanadrel

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Calcium channel blockers

Divided into 2

_________ which end with _____

_______ which includes _____

Dihydropyridines; pines

Non Dihydropyridines; diltaziem; verapamil

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Angiotensin-converting enzyme Inhibitors(ACEI):

Ends with

Pril

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Angiotensin II receptor antagonists Ends with

Sartan

Vasodilators Examples of Arterial vasodilators Examples of venous vasodilators

Hydralazine Minoxidil Diazoxide Sodium nitroprusside

List the types of diuretics

Loop Thiazide Thiazide-like Potassium sparing

Loop diuretics List 4

Furosemide Bumetanide Ethacrynic acid Torsemide

Thiazide diuretics List 3

Epitizide Hydrochlorothiazide Bendroflumethiazide

Thiazide-like diuretics

Indapamide Chlorthalidone Metolazone

Potassium sparing diuretics

Amiloride Triamterene Spironolactone Eplerenone

Potential drug targets: Beta blockers Alpha 1 blockers Alpha 2 agonist

Heart and juxtaglomerular cells Vascular smooth muscle Vasomotor center in the brain

Potential drug targets: Calcium channel blockers Diuretics Imidazoline receptor agonists

Vascular smooth muscle Vascular smooth muscle and kidney tubules Vasomotor center

Potential drug targets: ACE inhibitors Angiotensin 2 receptor antagonist Renin inhibitors Mineralocorticoid inhibitors

Vascular smooth muscle, Kidney tubules, Adrenal cortex Vascular smooth muscle, Kidney tubules, Adrenal cortex Kidney tubules Adrenal cortex

Lines of treatment of primary hypertension _______ may be effective treatment for about half of the patients with mild hypertension

Dietary salt restriction

The initial step in treating hypertension may be non-pharmacologic. T/F

Lines of treatment of primary hypertension ________ even without salt restriction normalizes blood pressure in up to ___% of ____ patients with mild to moderate hypertension.

Weight reduction; 70; obese

Regular exercise may also be helpful in some hypertensive patients. T/F

Lines of treatment of primary hypertension ______ are preferred in young patients, high renin hypertension and patients with tachycardia or angina and hypertension.

Beta-blockers

Black patients respond well to _______ and ________ than to _____ and _____

diuretics and calcium channel blockers beta- blockers and ACE inhibitors.

If mono-therapy is unsuccessful in hypertension , ____________ with _________ may be used.

combination of two drugs with different sites of action

Combination therapy in hypertension _____ diuretics may be used in conjunction with a _______, ________ or an _________________.

Thiazide; beta-blocker; calcium channel blocker ; angiotensin converting enzyme inhibitor

If hypertension is still not under control after combining two drugs, a third drug e.g. _______ such as ______ may be combined.

vasodilator such as hydralazine

When three drugs are required to treat hypertension, a _____, a _____ or an ______, and a ______ or _____ is effective

diuretic sympatholytic agents or an ACE inhibitor direct vasodilator or calcium channel block

The treatment of hypertensive emergencies is usually started with ______ given by ______ route at dose of 20-40mg. In addition, parenteral use of diazoxide, sodium nitroprusside, hydralazine, trimethaphan, labetalol can be indicated.

furosemide; parenteral

ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACEI) ACEI inhibit the activity of angiotensin- converting enzyme(ACE), an enzyme responsible for the ____________, a potent ___________.

conversion of angiotensin I into angiotensin II vasoconstrictor

ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACEI) ____________ is a prototype.

Captopril

ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACEI) They are given _____ daily and produce good _____ BP control. Very beneficial in patient with heart failure, diabetes, and CKD by preventing rapid progression and complications

once 24- hour

ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACEI) Mechanism of action ACE catalyses the cleavage of _______ from short peptides, thereby ‘converting’ the inactive ___________ to the potent vasoconstrictor angiotensin II . It also inactivates _______ – a vaso ______ peptide.

a pair of amino acids decapeptide angiotensin I bradykinin dilator

ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACEI) Mechanism of action ACEI lower blood pressure by reducing _________ and perhaps also by increasing vasodilator peptides, such as _______.

angiotensin II bradykinin

ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACEI) Mechanism of action Angiotensin II causes ______ secretion from the zona _____ of the adrenal _____ and inhibition of this contributes to the antihypertensive effect of ACE inhibitors.

aldosterone glomerulosa Cortex

ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACEI) Pharmacokinetics ACE inhibitors are all active when administered ____, but are _______ and are eliminated in the urine.

orally highly polar

ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACEI) Pharmacokinetics Enalapril are _____ and require ______ to __________ (e.g. _______).

prodrugs metabolic conversion active metabolites enalaprilat

ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACEI) Pharmacokinetics Many of these agents have (short or long?) half-lives permitting _______ dosing; _______ is an exception.

Long once daily captopril

Captopril has long half life T/F

F Its the exception

ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACEI) Adverse effects Renal failure (Functional) – in _______________ Rash Hyper_______

bilateral renal artery stenosis kalaemia

ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACEI) Adverse effects First-dose _______. Cough – Usually ___ cough, due to ________ Angio-oedema and _____ – due to _______

hypotension dry accumulation of bradykinin Urticaria; increased kinin

ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACEI) Adverse effects _______ – attributable to its sulphhydryl group ______ abnormality In Pregnancy;_______, so it is contraindicated in pregnancy

Proteinuria Taste fetal anomaly,

CALCIUM-CHANNEL BLOCKERS Calcium channel blockers (CCB) block the entry of calcium into muscle cells in artery walls blocking voltage-dependent Ca2 channels. T/F

CALCIUM-CHANNEL BLOCKERS used to treat ______ and ________ as well as hypertension.

angina and supraventricular tachydysrhythmias

CALCIUM-CHANNEL BLOCKERS Divided into ____ Classes. They are ______ muscle relaxant.

2 smooth

CALCIUM-CHANNEL BLOCKERS Mechanism of action Calcium-channel blockers inhibit Ca2 influx through ____-dependent __-type calcium channels. _________ Ca2 concentrations control the contractile state of actomyosin. Calcium-channel blockers therefore ____ arteriolar smooth muscle, reduce _________ and lower __________

voltage ;L Cytoplasmic relax; peripheral vascular resistance peripheral vascular resistance arterial blood pressure.

Effects of the following drugs on the heart rate Nifedipine Amlodipine Nimodipine Diltazem Verapamil

Increase Nothing Increase Nothing Decrease

ß-ADRENOCEPTOR ANTAGONISTS – B Blockers β-Adrenoceptors are subdivided into β1-receptors (_____), β2-receptors (______,_____) β3-receptors (some metabolic effects, e.g. in _______)..

heart blood vessels, bronchioles brown fat

ß-ADRENOCEPTOR ANTAGONISTS Mechanism of action Beta-adrenoceptors are coupled to a Gs-proteins activate  adenylyl cyclase  cAMP from ATP. Increased cAMP activates  cAMP-dependent protein kinase (PK-A) that  phosphorylated L-type calcium channels  calcium entry into the cell.  sarcoplasmic reticulum in the heart;  these actions increase inotropy (contractility). B Blockers blocks action above

ß-ADRENOCEPTOR ANTAGONISTS Mechanism of action Beta-adrenoceptors are coupled to a ___-proteins that activate _______ to produce ________ from _____ Increased cAMP activates  cAMP-dependent _________ that  ______ ____-type calcium channels  calcium entry into the cell.  sarcoplasmic reticulum in the heart;  these actions increase inotropy ( ________). B Blockers blocks action above

Gs adenylyl cyclase cAMP from ATP. protein kinase (PK-A) phosphorylated L contractility

ß-ADRENOCEPTOR ANTAGONISTS β-Adrenoceptor antagonists reduce cardiac output (via negative ____ and negative ______ effects on the heart), inhibit ____ secretion and some have additional central actions reducing ______ outflow from the central nervous system (CNS).

chronotropic inotropic renin sympathetic

ß-ADRENOCEPTOR ANTAGONISTS Adverse effects and contraindications – Intolerance – fatigue, cold extremities,______ – Airways obstruction – Contra-indicated in ______ – Decompensated _______ – β-adrenoceptor antagonists are contraindicated

erectile dysfunction asthma; heart failure

ß-ADRENOCEPTOR ANTAGONISTS Adverse effects and contraindications – β-adrenoceptor antagonists can mask symptoms of _____ and the rate of recovery is – Heart block – ——— heart block. – Metabolic disturbance - worsen _______ in __________

hypoglycaemia worsen glycaemic control ; type 2 diabetes mellitus

Diuretics help the kidneys to __________

eliminate excess salt and water from the body's tissues and blood.

______ and ———- diuretics should usually be the first choice when selecting a diuretic to treat hypertension.

thiazide and thiazide-like

thiazide and thiazide-like diuretics Possess ____ properties in addition to reducing intravascular fluid.

vasodilating

Diuretics Mechanism of action Thiazide diuretics inhibit _____________ in the _________________

reabsorption of sodium and chloride ions proximal part of the distal convoluted tubule.

Diuretics Mechanism of action _________ or __________ interferes with their antihypertensive effect.

Excessive salt intake or a low glomerular filtration rate

Diuretics Mechanism of action _________ is therefore probably important in determining their hypotensive action.

Natriuresis

Thiazides Mechanism: Location:

Inhibits reabsorption by Na+/Cl− symporter Distal convoluted tubules (DCT)

Loop diuretics Mechanism: Location:

Inhibits the Na-K-Cl symporter Medullary thick ascending limb

Potassium- sparing diuretics Mechanism: ____________ Spironolactone:———— Amiloride: ————— Location:

Inhibition of Na+/K+ exchanger: Spironolactone inhibits aldosterone action, Amiloride inhibits epithelial sodium channels Cortical collecting ducts

Adverse effects of diuretics • Metabolic and electrolyte changes involve: – Hypo______ – sometimes severe in elderly – hypokalaemia – due to _______ – hypo ________

natraemia Na – K ions exchange magnesaemia

Adverse effects of diuretics • Metabolic and electrolyte changes involve: -hyper_____/_____– most diuretics reduce ____ clearance. – hyper_______ – thiazides reduce ______ tolerance

uricaemia; Gout; urate glycaemia glucose

Adverse effects of Diuretics Idiosyncratic reactions, including _____ (which may be photosensitive) and _____, which may be ______ or ______

rashes; purpura thrombocytopenic or non-thrombocytopenic.

Adverse effects of Diuretics hyper______ – thiazides reduce urinary ________ clearance hyper_______ – _____ -dose thiazides cause a (small or large?) increase in plasma ______

calcaemia; calcium ion cholesterolaemia; high; small LDL cholesterol

Adverse effects of Diuretics _____ dysfunction. Increased plasma _____

Erectile renin

Mean arterial pressure(MAP) = ___________ or _________

DP + 1/3(SP – DP) DP + 1/3(PP)

ADVERSE EFFECTS of ACE inhibitors C – A – P – T – O – P – R – R – H -

C – Cough A – Angioedema P – Pregnancy contraindication T – Taste abnormality O – Orthostatic hypotension P – Proteinuria R – Rash R – Renal impairment/improvement H - Hyperkalemia

ADVERSE EFFECTS of ACE inhibitors C – _____ A – _____ P – ______ T – _______ O –_______ P – _______ R – ________ I-_______ L-__________

C1 esterase deficiency/cough Angioedema Potassium excess/ proteinuria Taste abnormality Orthostatic hypotension Pregnancy contraindications Renal artery stenosis Increases renin Leukopenia/liver toxicity

Methadone is a __________

Thiazide-like diuretic

Chlorthalidone is a _______

Thiazide like diuretic

Examples of venous vasodilators?

Sodium Nitroprusside Isosorbide Dinitrate Nitroglycerin

MECHANISM OF ACTION Hydralazine _________ of ————— which results in decreased PVR

Direct vasodilation of arteriolar smooth muscle

MECHANISM OF ACTION Minoxidil _____________ leading to ________ and __________ eventually causing arterial vasodilation

Binds and opens K+ channels leading to hyperpolarization and relaxation of smooth muscles

MECHANISM OF ACTION Diazoxide _____________ leading to ________ and __________ eventually causing arterial vasodilation

Binds and opens K+ channels leading to hyperpolarization and relaxation of smooth muscles

Mechanism of action of sodium nitroprusside?

Release of NO

Drug treatment of hypertension in pregnancy Remember her new lab method

Hydralazine- arterial vasodilator Nifedipine- calcium blocker Labetalol- non specific beta blocker Methyldopa- alpha 2 agonist

Thiocyanate toxicity is an identified adverse effect of ???

Sodium nitroprusside

Felasartan??

Doesn’t exist

AVP acts through ______ receptors in the _____

V2 Collecting duct

Eplerenone is a ???

Potassium soaring diuretic