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House Pharmacology > Anti Hypertensives > Flashcards

Anti Hypertensives Flashcards

1
Q

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

A

140/90

Two different days

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2
Q

Most common cardiovascular disease

A

Hypertension

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3
Q

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

A

Asymptomatic

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4
Q

____________ people worldwide have hypertension

A

1.13 billion

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5
Q

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

A

18

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6
Q

Hypertension is more prevalent where?
Nigeria or US

A

Nigeria

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7
Q

Hypertension is More prevalent in Nigeria ___-___%.

A

25- 30

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8
Q

Physiology of Blood pressure

BP = ___________ X _______

A

Cardiac Output X Peripheral Vascular Resistance.

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9
Q

Physiology of Blood pressure

Arterial pressure affected by:

the ______ system (fast)

– the _______ system (hours or days)

the _______ (days or weeks)

A

autonomic nervous

renin-angiotensin

kidneys

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10
Q

Classification of anti-hypertensive by site or mechanism

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

A

Sympatholytic

Calcium channel blockers (CCB)

Angiotensin-converting enzyme Inhibitors(ACEI)

Angiotensin II receptor antagonists (ARB)

Vasodilators

Diuretics

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11
Q

Mechanism of action

Sympatholytic drug

_______ of sympathetic activities and _______

A

Blockade

decrease in peripheral resistance

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12
Q

Mechanism of action

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

A

inhibition

calcium influx

arterial smooth muscle ; decrease in peripheral resistance.

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13
Q

Mechanism of action

Angiotensin-converting enzyme Inhibitors(ACEI)

_______ angiotensin converting enzyme that ______________ to _________

A

inhibits

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

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14
Q

Mechanism of action

Angiotensin II receptor antagonists (ARB)

______ Angiotensin II receptor, resulting in a _________________

A

Inhibit

decrease in peripheral resistance

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15
Q

Mechanism of action

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

A

decrease in peripheral resistance.

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16
Q

Mechanism of action

Diuretics
lower blood pressure by ________ and ________

A

depleting the body sodium and reducing blood volume

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17
Q

Sympatholytic drugs

B1 selective blockers

List them

A

Acebutolol

Atenolol

Betaxolol

Bisoprolol Esmolol Metoprolol Nebivolol

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18
Q

Sympatholytic drugs

Non-selective β1/β2

Listtttt

A

Carvedilol
Labetalol
nadolol
penbutolol
pindolol
Propanolol
Sotalol
Timolol

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19
Q

Sympatholytic drugs

α Adrenergic receptor antagonist (alpha blockers):

Listtttt

A

Doxazosin
Phentolamine
Indoramin
Phenoxybenzamine

Prazosin
Terazosin
Tolazoline

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20
Q

Sympatholytic drugs

Mixed adrenergic antagonist:

List 3

A

Carvedilol

Labetalol

Bucindolol

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21
Q

Sympatholytic drugs

Centrally acting agent/ α2 receptor agonist:

List 5

A

α –Methyldopa
Clonidine
Guanabenz
Guanfacine
Moxonidine

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22
Q

Sympatholytic drugs

Adrenergic neuron blockers:

A

Reserpine

Guanadrel

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23
Q

Calcium channel blockers

Divided into 2

_________ which end with _____

_______ which includes _____

A

Dihydropyridines; pines

Non Dihydropyridines; diltaziem; verapamil

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24
Q

Angiotensin-converting enzyme Inhibitors(ACEI):

Ends with

A

Pril

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25
Q

Angiotensin II receptor antagonists

Ends with

A

Sartan

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26
Q

Vasodilators

Examples of Arterial vasodilators

Examples of venous vasodilators

A

Hydralazine Minoxidil Diazoxide

Sodium nitroprusside

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27
Q

List the types of diuretics

A

Loop
Thiazide
Thiazide-like
Potassium sparing

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28
Q

Loop diuretics

List 4

A

Furosemide

Bumetanide

Ethacrynic acid

Torsemide

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29
Q

Thiazide diuretics

List 3

A

Epitizide

Hydrochlorothiazide

Bendroflumethiazide

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30
Q

Thiazide-like diuretics

A

Indapamide

Chlorthalidone

Metolazone

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31
Q

Potassium sparing diuretics

A

Amiloride

Triamterene

Spironolactone

Eplerenone

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32
Q

Potential drug targets:

Beta blockers
Alpha 1 blockers
Alpha 2 agonist

A

Heart and juxtaglomerular cells

Vascular smooth muscle

Vasomotor center in the brain

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33
Q

Potential drug targets:

Calcium channel blockers

Diuretics

Imidazoline receptor agonists

A

Vascular smooth muscle

Vascular smooth muscle and kidney tubules

Vasomotor center

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34
Q

Potential drug targets:

ACE inhibitors

Angiotensin 2 receptor antagonist

Renin inhibitors

Mineralocorticoid inhibitors

A

Vascular smooth muscle, Kidney tubules, Adrenal cortex

Vascular smooth muscle, Kidney tubules, Adrenal cortex

Kidney tubules

Adrenal cortex

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35
Q

Lines of treatment of primary hypertension

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

A

Dietary salt restriction

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36
Q

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

T/F

A

T

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37
Q

Lines of treatment of primary hypertension

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

A

Weight reduction; 70; obese

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38
Q

Regular exercise may also be helpful in some hypertensive patients.

T/F

A

T

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39
Q

Lines of treatment of primary hypertension

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

A

Beta-blockers

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40
Q

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

A

diuretics and calcium channel blockers

beta- blockers and ACE inhibitors.

41
Q

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

A

combination of two drugs with different sites of action

42
Q

Combination therapy in hypertension

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

A

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

43
Q

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

A

vasodilator such as hydralazine

44
Q

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

A

diuretic

sympatholytic agents or an ACE inhibitor

direct vasodilator or calcium channel block

45
Q

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.

A

furosemide; parenteral

46
Q

ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACEI)

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

A

conversion of angiotensin I into angiotensin II

vasoconstrictor

47
Q

ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACEI)

____________ is a prototype.

48
Q

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

A

once

24- hour

49
Q

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

a pair of amino acids

decapeptide angiotensin I

bradykinin

dilator

50
Q

ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACEI)
Mechanism of action

ACEI lower blood pressure by reducing _________ and perhaps also by increasing vasodilator peptides, such as _______.

A

angiotensin II

bradykinin

51
Q

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.

A

aldosterone

glomerulosa
Cortex

52
Q

ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACEI)
Pharmacokinetics

ACE inhibitors are all active when administered ____, but are _______ and are eliminated in the urine.

A

orally

highly polar

53
Q

ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACEI)
Pharmacokinetics

Enalapril are _____ and require ______ to __________ (e.g. _______).

A

prodrugs

metabolic conversion

active metabolites

enalaprilat

54
Q

ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACEI)
Pharmacokinetics

Many of these agents have (short or long?) half-lives permitting _______ dosing; _______ is an exception.

A

Long

once daily

captopril

55
Q

Captopril has long half life

T/F

A

F

Its the exception

56
Q

ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACEI)
Adverse effects

Renal failure (Functional) – in _______________

Rash

Hyper_______

A

bilateral renal artery stenosis

kalaemia

57
Q

ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACEI)

Adverse effects

First-dose _______.

Cough – Usually ___ cough, due to ________

Angio-oedema and _____ – due to _______

A

hypotension

dry

accumulation of bradykinin

Urticaria; increased kinin

58
Q

ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACEI)
Adverse effects

_______ – attributable to its sulphhydryl group

______ abnormality

In Pregnancy;_______, so it is contraindicated in pregnancy

A

Proteinuria

Taste

fetal anomaly,

59
Q

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

60
Q

CALCIUM-CHANNEL BLOCKERS

used to treat ______ and ________ as well as hypertension.

A

angina and supraventricular tachydysrhythmias

61
Q

CALCIUM-CHANNEL BLOCKERS

Divided into ____ Classes.
They are ______ muscle relaxant.

62
Q

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 __________

A

voltage ;L

Cytoplasmic

relax; peripheral vascular resistance peripheral vascular resistance

arterial blood pressure.

63
Q

Effects of the following drugs on the heart rate

Nifedipine
Amlodipine
Nimodipine
Diltazem
Verapamil

A

Increase
Nothing
Increase
Nothing
Decrease

64
Q

ß-ADRENOCEPTOR ANTAGONISTS – B Blockers

β-Adrenoceptors are subdivided into

β1-receptors (_____),
β2-receptors (______,_____)
β3-receptors (some metabolic effects, e.g. in _______)..

A

heart

blood vessels, bronchioles

brown fat

65
Q

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

66
Q

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

A

Gs

adenylyl cyclase

cAMP from ATP.

protein kinase (PK-A)

phosphorylated

L

contractility

67
Q

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).

A

chronotropic

inotropic

renin

sympathetic

68
Q

ß-ADRENOCEPTOR ANTAGONISTS

Adverse effects and contraindications
– Intolerance – fatigue, cold extremities,______

– Airways obstruction – Contra-indicated in ______

– Decompensated _______ – β-adrenoceptor antagonists are contraindicated

A

erectile dysfunction

asthma; heart failure

69
Q

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 __________

A

hypoglycaemia

worsen

glycaemic control ; type 2 diabetes mellitus

70
Q

Diuretics help the kidneys to __________

A

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

71
Q

______ and ———- diuretics

should usually be the first choice when selecting a diuretic to treat hypertension.

A

thiazide and thiazide-like

72
Q

thiazide and thiazide-like diuretics

Possess ____ properties in addition to reducing intravascular fluid.

A

vasodilating

73
Q

Diuretics Mechanism of action

Thiazide diuretics inhibit _____________ in the _________________

A

reabsorption of sodium and chloride ions

proximal part of the distal convoluted tubule.

74
Q

Diuretics Mechanism of action

_________ or __________ interferes with their antihypertensive effect.

A

Excessive salt intake or a low glomerular filtration rate

75
Q

Diuretics Mechanism of action

_________ is therefore probably important in determining their hypotensive action.

A

Natriuresis

76
Q

Thiazides

Mechanism:

Location:

A

Inhibits reabsorption by Na+/Cl− symporter

Distal convoluted tubules (DCT)

77
Q

Loop diuretics

Mechanism:

Location:

A

Inhibits the Na-K-Cl symporter

Medullary thick ascending limb

78
Q

Potassium- sparing diuretics

Mechanism: ____________
Spironolactone:————
Amiloride: —————

Location:

A

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

Cortical collecting ducts

79
Q

Adverse effects of diuretics

• Metabolic and electrolyte changes involve:

– Hypo______ – sometimes severe in elderly

– hypokalaemia – due to _______

– hypo ________

A

natraemia

Na – K ions exchange

magnesaemia

80
Q

Adverse effects of diuretics
• Metabolic and electrolyte changes involve:

-hyper_____/_____– most diuretics reduce ____ clearance.
– hyper_______ – thiazides reduce ______ tolerance

A

uricaemia; Gout; urate

glycaemia

glucose

81
Q

Adverse effects of Diuretics

Idiosyncratic reactions, including _____ (which may be photosensitive) and _____, which may be ______ or ______

A

rashes; purpura

thrombocytopenic or non-thrombocytopenic.

82
Q

Adverse effects of Diuretics

hyper______ – thiazides reduce urinary ________ clearance

hyper_______ – _____ -dose thiazides cause a (small or large?) increase in plasma ______

A

calcaemia; calcium ion

cholesterolaemia; high; small

LDL cholesterol

83
Q

Adverse effects of Diuretics

_____ dysfunction.

Increased plasma _____

A

Erectile

renin

84
Q

Mean arterial pressure(MAP) = ___________ or _________

A

DP + 1/3(SP – DP)

DP + 1/3(PP)

85
Q

ADVERSE EFFECTS of ACE inhibitors

C –
A –
P –
T –
O –
P –
R –
R –
H -

A

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

86
Q

ADVERSE EFFECTS of ACE inhibitors

C – _____
A – _____
P – ______
T – _______
O –_______
P – _______
R – ________
I-_______
L-__________

A

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

87
Q

Methadone is a __________

A

Thiazide-like diuretic

88
Q

Chlorthalidone is a _______

A

Thiazide like diuretic

89
Q

Examples of venous vasodilators?

A

Sodium Nitroprusside

Isosorbide Dinitrate
Nitroglycerin

90
Q

MECHANISM OF ACTION
Hydralazine

_________ of ————— which results in decreased PVR

A

Direct vasodilation of arteriolar smooth muscle

91
Q

MECHANISM OF ACTION
Minoxidil

_____________ leading to ________ and __________ eventually causing arterial vasodilation

A

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

92
Q

MECHANISM OF ACTION
Diazoxide

_____________ leading to ________ and __________ eventually causing arterial vasodilation

A

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

93
Q

Mechanism of action of sodium nitroprusside?

A

Release of NO

94
Q

Drug treatment of hypertension in pregnancy

Remember her new lab method

A

Hydralazine- arterial vasodilator

Nifedipine- calcium blocker

Labetalol- non specific beta blocker

Methyldopa- alpha 2 agonist

95
Q

Thiocyanate toxicity is an identified adverse effect of ???

A

Sodium nitroprusside

96
Q

Felasartan??

A

Doesn’t exist

97
Q

AVP acts through ______ receptors in the _____

A

V2

Collecting duct

98
Q

Eplerenone is a ???

A

Potassium soaring diuretic

House Pharmacology (50 decks)

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