CVS Pharmacology 1: Antihypertensives-1. Flashcards

1
Q

Hypertension is an important risk factor for which conditions? (4)

A

1- heart disease.
2- stroke.
3- chronic kidney disease.
4- organ damage.

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2
Q

The risk of organ damage is directly related to what?

A

The extent of elevation of BP.

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3
Q

List the 4 classifications of hypertension?

A

1- normal: <120 and <80.
2- elevated: 120-139 or 80-89.
3- stage 1 hypertension: 140-159 or 90-99.
4- stage 2 hypertension: >= 160 or >=100.

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4
Q

List the 2 types of hypertension, and their etiology?

A

1- essential hypertension (90% cases).
2- secondary hypertension (10-15%).

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5
Q

List the 7 lifestyle modifications that can decrease blood pressure?

A

1- weight reduction.
2- increase in physical activity.
3- dietary sodium reduction.
4- limited fat intake.
5- increased fibre intake.
6- restriction on alcohol consumption.
7- stopping tobacco products.

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6
Q

Arterial blood pressure is directly proportional to what?

A

Directly proportional to cardiac output and peripheral vascular resistance.

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7
Q

Most antihypertensives lower BP by reducing _______ ____ and/or decreasing _______ _______.

A

Reducing cardiac output and/or decreasing peripheral resistance.

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8
Q

Cardiac output and peripheral resistance are controlled by what?

A

1- baroreflexes.
2- RAAS.

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9
Q

List the 10 classifications of antihypertensives?

A

1- diuretics.
2- ACE inhibitors.
3- angiotensin (AT1 receptor) blockers (ARB).
4- direct renin inhibitor.
5- calcium channel blockers.
6- Beta adrenergic blockers.
7- beta and alpha adrenergic blockers.
8- alpha adrenergic blockers.
9- central sympatholytics.
10- vasodilators.

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10
Q

List the 3 types of diuretics?

A

1- thiazides.
2- high ceiling “loop diuretics”.
3- K+ sparing.

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11
Q

List 3 examples of thiazides?

A

1- hydrochlorothiazide.
2- chlorthalidone.
3- indapamide.

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12
Q

Give an example of high ceiling “loop diuretics”?

A

Furosemide.

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13
Q

List 2 examples of K+ sparing?

A

1- spironolactone.
2- amiloride.

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14
Q

List 6 examples of ACE inhibitors?

A

1- captopril.
2- enalapril.
3- lisinopril.
4- perindopril.
5- ramipril.
6- fosinopril.
All end with “pril”.

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15
Q

List 5 examples of ARB?

A

1- losartan.
2- candesartan.
3- irbesartan.
4- valsartan.
5- telmisartan.
All end with “sartan”.

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16
Q

List an example of direct renin inhibitor?

A

Aliskiren.

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17
Q

List 7 examples of CCBs?

A

1- verapamil.
2- diltiazem.
3- nifedipine.
4- felodipine.
5- amlodipine.
6- nitrendipine.
7- lacidipine.

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18
Q

List 3 examples of Beta adrenergic blockers?

A

Non selective: propranolol.
Beta 2 selective: metoprolol, atenolol.

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19
Q

List 2 examples of beta and alpha adrenergic blockers?

A

Labetalol,
Carvedilol.

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20
Q

List 5 alpha adrenergic blockers?

A

1- prazosin.
2- terazosin.
3- doxazosin.
4- phentolamine.
5- phenoxybenzamine.

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21
Q

List 2 central sympatholytics?

A

1- clonidine.
2- alpha-methyldopa.

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22
Q

List the 2 groups of vasodilators, and give examples of them?

A

1- arteriolar: hydralazine, minoxidil, diazoxide.
2- arteriolar + venous: sodium nitroprusside.

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23
Q

Alpha adrenergic blockers work on which type of BP?

A

Peripheral BP.

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24
Q

Central sympatholytics work on which receptor?

A

Alpha 2 antagonist, stimulates the alpha 2 receptor in the brain.

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25
Q

Which type of antihypertensives are used in emergencies and in resistant hypertension?

A

Vasodilators.

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26
Q

Which vasodilator is used in emergency in 180mmHg and above with impending organ damage?

A

Sodium nitroprusside.

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27
Q

Which antihypertensives can be used as first-line drug therapy?

A

Diuretics, specifically thiazides.

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28
Q

Which type of investigations should be done in all patients receiving diuretics?

A

Routine serum electrolyte monitoring.

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29
Q

List the actions of diuretics?

A

Lower blood pressure by increasing Na and water excretion > which causes a decrease in extracellular volume, decrease in cardiac output and renal blood flow.

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30
Q

What happens to plasma volume and peripheral resistance with long term treatment of diuretics?

A

Plasma volume approaches a normal value, but peripheral resistance decreases.

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31
Q

Which type of drugs are often combined with thiazides?

A

Potassium-sparing diuretics.

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32
Q

Thiazide diuretics are particularly useful in the treatment of which groups of patients?

A

Black or elderly patients.

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33
Q

Thiazides are not effective in patients with which conditions, and what may be required in these patients?

A

Not effective in patients with inadequate kidney function (creatinine clearance <50 mL/min), loop diuretics may be required in these patients.

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34
Q

List the 4 adverse effects of diuretics?

A

1- hypokalemia.
2- hypomagnesemia.
3- hyperuricemia (can cause gout).
4- hyperglycemia (interferes with blood glucose management).

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35
Q

Which type of investigation should be done in patients who are taking diuretics and are predisposed to cardiac arrhythmias?

A

Serum potassium levels.

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36
Q

Loop diuretics act even in patients with poor ____ _____ or who have no responded to ____ or other _____.

A

Patients with poor renal function or who have not responded to thiazides or other diuretics.

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37
Q

What do loop diuretics do to renal vascular resistance and renal blood flow?

A

Decrease renal vascular resistance and increased renal blood flow.

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38
Q

Loop diuretics increase the ___ Content of urine, whereas thiazide diuretics decrease it.

A

Ca2+.

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39
Q

List the 2 groups of potassium-sparing diuretics?

A

1-inhibitors of epithelial sodium transport at the late distal and collecting ducts.
2- aldosterone-receptor antagonists.

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40
Q

List the 2 potassium sparing diuretics that are inhibitors of epithelial sodium transport at the late distal and collecting ducts?

A

Amiloride and triamterene.

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41
Q

List the 2 potassium sparing diuretics that are aldosterone-receptor antagonists?

A

Spironolactone and eplerenone.

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42
Q

List an adverse effect of spironolactone?

A

Gynecomastia, blocks testerone.

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43
Q

List a benefit of spironolactone?

A

Diminishing of the cardiac remodeling (caused by aldosterone) that occurs in heart failure.
(Good for cardiac patients).

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44
Q

How do ACE inhibitors lower blood pressure?

A

By reducing peripheral vascular resistance without reflexively increasing cardiac output, rate, or contractility.

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45
Q

What effects do ace inhibitors have on sodium and water retention?

A

By reducing circulating angiotensin 2 levels, ACE inhibitors also decrease the secretion of aldosterone, resulting in decreased sodium and water retention.

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46
Q

Which drugs are first line drugs in all grades of hypertension?

A

ACE inhibitors.

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47
Q

ACE inhibitors are highly effective and first choice drugs in _______ and _______ hypertension.

A

Renovascular and resistant hypertension.

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48
Q

ACE inhibitors are particularly suitable for which type of hypertension patients?

A

Diabetic hypertensives.
They decrease proteinuria of diabetic nephropathy.

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49
Q

List 7 therapeutic uses of ACE inhibitors?

A

1- no postural hypotension.
2- safe in asthmatics, diabetics and peripheral vascular disease patients.
3- secondary hyperaldosteronism and K+ loss due to diuretics is prevented.
4- no rebound hypertension on withdrawal.
5- left ventricular hypertrophy is reversed.
6- no hyperuricaemia, no deleterious effect on plasma lipid profile.
7- minimum worsening of quality of life parameters like general wellbeing, work performance, sleep, sexual performance ect.

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50
Q

List the 8 adverse effects of ACE inhibitors?

A

1- hypotension.
2- hyperkalaemia.
3- dry cough.
4- rashes, urticaria.
5- angioedema.
6- dysgeusia.
7- foetopathic.
8- acute renal failure: in patients of bilateral renal artery stenosis.

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51
Q

What causes dry cough with ACE inhibitors?

A

Not dose related, appears to be caused by inhibition of bradykinin/substance P breakdown in the lungs of susceptible individuals.

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52
Q

Angiotensin 2 receptor blockers block which receptor?

A

Block the AT1 receptors.

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53
Q

ARBs differ from ACE inhibitors in what?

A

Don’t increase bradykinin levels.

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54
Q

ARBs are contraindicated in which group of people?

A

Pregnant women because they are fetotoxic.

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55
Q

Which drug is a selective renin inhibitor, used for the treatment of hypertension?

A

Aliskiren.

56
Q

List the adverse effects of Aliskiren?

A

1- Causes diarrhea, especially at higher doses.
2- Cough and angioedema.

57
Q

List Aliskiren contraindications?

A

Pregnancy.

58
Q

How do calcium channel antagonists work?

A

They block the inward movement of calcium by binding to L-type calcium channels > causes vascular smooth muscle to relax, dilating mainly arterioles.

59
Q

Where do calcium channel blockers block calcium?

A

In the heart and smooth muscle of the coronary and peripheral vasculature.

60
Q

CCBs are recommended first line agents in which group of people?

A

Blacks.

61
Q

List the 3 classes of CCBs?

A

1- diphenylalkylamines.
2- benzothiazepines.
3- dihydropyridines.

62
Q

Give an example of diphenylalkylamines CCBs?

A

Verapamil.

63
Q

Give an example of benzothiazepine CCBs?

A

Diltiazem.

64
Q

Give an example of dihydropyridines?

A

First generation: nifedipine.
Second generation: isradipine, felodipine, amlodipine, nitrendipine, nimodipine, lacidipine, lercanidipine.
(All end with dipine).

65
Q

Which class of CCBs works in the blood vessels only?

A

Dihydropyridines.

66
Q

Which classes of CCBs work both in the blood vessels and the heart?

A

1- diphenylalkylamines.
2- benzothiazepines.

67
Q

CCBs are safe to treat hypertension in which cases?

A

COPD and peripheral vascular disease.

68
Q

CCBs have an _____ effect and therefore don’t require the addition of a ______.

A

Natriuretic effect, don’t require addition of a diuretic.

69
Q

List the 8 therapeutic uses of CCBs?

A

1- hypertension.
2- Angina pectoris.
3- cardiac arrhythmias.
4- hypertrophic cardiomyopathy.
5- premature labor.
6- nocturnal leg cramps.
7- raynaud’s episodes.

70
Q

Which CCBs can be used for PSVT and supraventricular arrhythmias?

A

Verapamil and diltiazem .

71
Q

Which CCB can be used for premature labor?

A

Nifedipine.

72
Q

Which CCB can be used for nocturnal leg cramps?

A

Verapamil.

73
Q

Which CCB can be used for Raynaud’s episodes?

A

DHPs (Dipines).

74
Q

List the 7 AE of CCBs?

A

1- palpations, flushing, ankle edema.
2- hypotension, headache, drowsiness and nausea.
3- first degree AV block (with the CCBs that work on the heart).
4- constipation.
5- urine voiding difficulty in elderly males.
6- GER may be worsened.
7- gingival hyperplasia.

75
Q

Which CCB causes urine voiding difficulty in elderly males?

A

Nifedipine.

76
Q

Which CCB may worsen GER?

A

All DHPs.

77
Q

Which CCB can cause gingival hyperplasia?

A

Nifedipine.

78
Q

Which CCBs should be avoided in heart failure and AV block? And why?

A

Verapamil and diltiazem, due to negative inotropic effect.

79
Q

How do beta blockers affect cardiac output, central sympathetic outflow from the CNS and release of renin from kidneys?

A

Decreases cardiac output.
Decreases sympathetic outflow from the CNS.
Inhibits the release of renin from the kidneys.

80
Q

Which receptors does propranolol work on?

A

Acts on both beta 1 and beta 2 receptors.

81
Q

Which receptors do metoprolol and atenolol work on?

A

Selective blockers of beta 1 receptors.

82
Q

Which type of beta blockers are preferred in asthmatics?

A

Selective beta blockers.

83
Q

Beta blockers are more effective in which race group?

A

Whites more than blacks.

84
Q

List contraindications of beta blockers?

A

1- severe COPD.
2- 1st and 2nd degree heart block.
3- severe peripheral vascular disease.

85
Q

List the conditions that may coexist with hypertension in which beta blockers are useful in treating?

A

1- supraventricular tachyarrhythmia.
2- previous MI.
3- angina pectoris.
4- migraine headache.
5- chronic heart failure.

86
Q

List 5 adverse effects of beta blockers?

A

1- bradycardia.
2- hypotension.
3- fatigue, lethargy, insomnia, and hallucinations.
4- decrease libido and cause impotence.
5- alternations in serum lipid patterns; decrease in HDL and increase in TGs.

87
Q

Abrupt withdrawal of beta blockers causes what?

A

May induce angina, myocardial infarction, or sudden death in patients with ischemic heart disease.

88
Q

How do alpha blocking agents affect TPR and BP?

A

They decrease TPR and BP.

89
Q

What often occurs at the onset of treatment with increase in dose of alpha blocking agents?

A

Reflex tachycardia and postural hypotension.

90
Q

List alpha blocking agents?

A

Prazosin, doxazosin, terazosin.

91
Q

Which receptor do alpha blocking agents work on?

A

Competitive blockers of alpha 1 adenoreceptors.

92
Q

Labetalol and carvedilol act on which receptors?

A

They block alpha 1, beta 1 and beta 2 receptors.

93
Q

List the 4 therapeutic effects of labetalol?

A

1- rapid BP reduction in hyperadrenergic states.
2- cheese reaction.
3- clonidine withdrawl.
4- eclampsia.

94
Q

Which additional properties does carvedilol have?

A

Antioxidant/ free radical scavenging properties.

95
Q

Cavedilol is used for what?

A

Long term treatment of CHF, and is approved as an antihypertensive as well.

96
Q

List 2 centrally acting adrenergic drugs?

A

Clondine.
Methyldopa.

97
Q

Clondine and methyldopa act on which receptors?

A

Both drugs are alpha 2 adrenergic receptor agonists.

98
Q

How do centrally acting adrenergic drugs affect sympathetic outflow from the brain to the CVS?

A

They decrease it.

99
Q

What is the route of administration of centrally acting adrenergic drugs?

A

Both are absorbed orally.
Clondine is also available as a transdermal patch.

100
Q

How does clonidine affect renal blood flow?

A

Does not decrease renal blood flow.

101
Q

Clonidine is used for the treatment of which?

A
  • used for hypertension has not responded adequately to treatment with two or more drugs.
  • useful in the treatment of hypertension complicated by renal disease.
102
Q

List the 3 adverse effects of clonidine?

A

1- can cause sodium and water retention (Add diuretic).
2- sedation and drying of the nasal mucosa.
3- rebound hypertension on abrupt withdrawal.

103
Q

Rebound hypertension caused by clonidine abrupt withdrawal is due to what?

A

Supersensitivity of adrenergic receptors caused by chronic clonidine-induced reduction in sympathetic outflow.

104
Q

List 4 vasodilators?

A

1- hydralazine.
2- minoxidil.
3- diazoxide.
4- sodium nitroprusside.

105
Q

How do vasodilators affect TPR and BP?

A

Decrease TPR and BP.

106
Q

Vasodilators produce ____ _____ of the heart?

A

Reflex stimulation.

107
Q

Reflux stimulation of vasodilators cause which AE?

A

1- angina pectoris.
2- myocardial infarction.
3- cardiac failure.
In predisposed individuals.

108
Q

How do vasodilators affect plasma renin concentration?

A

Increase plasma renin concentration, resulting in sodium and water retention.

109
Q

Undesirable side effects of vasodilators can be blocked by concomitant use of what?

A

Diuretics and a beta blocker.

110
Q

Which antihypertensives are given when a patient has stable IHD?

A

1- beta blocker.
2- ACE inhibitor.
3- ARBs.
4- CCBs.

111
Q

Which antihypertensives are given when a patient has diabetes?

A

1- diuretics.
2- ACEI.
3- ARBs.
4- CCBs.

112
Q

Which antihypertensives are given when a patient has recurrent stroke?

A

1- diuretics.
2- ACEI.
3- ARBs.

113
Q

Which antihypertensives are given when a patient has HF?

A

1- diuretics.
2- beta blockers.
3- ACEI.
4- ARBs.
5- aldosterone receptor antagonist.

114
Q

Which antihypertensives are given when a patient has previous MI?

A

1- beta blocker.
2- ACEI.
3- aldosterone receptor antagonist.

115
Q

Which antihypertensives are given when a patient has CKD?

A

1- ACEI.
2- ARBs.

116
Q

The goal of antihypertensive therapy is to reduce what?

A

Cardiovascular and renal morbidity and mortality.

117
Q

Antihypertensive therapy is indicated in cases where:
- SBP _______ or DBP _______ (at age 60 or more).
- SBP _______ or DBP _______ (at age <60).

A
  • SBP >= 150 mmHg or DBP >= 90mmHg (at age 60 or more).
  • SBP >= 140 mmHg or DBP >= 90mmHg (at age <60).
118
Q

Current recommendation is to initiate therapy with a _____ _____, ____ ______, ___ or ____.

A

Thiazide diuretic, ACE inhibitor, ARB or CCB.

119
Q

What do we do if BP is inadequately controlled after 1 month of therapy?

A

Either increase dose or add another drug.
Add a third drug if 2 drugs don’t control the BP.

120
Q

If SBP is greater than 20mmHg or DBP is 10mmHg above goal, we start with how many drugs?

A

Start with 2 drugs.

121
Q

List the 3 drug combinations in hypertension?

A

1- fully additive drug combinations (preferred combination).
2- questionable drug combinations.
3- preferred combinations with patients with associated conditions.

122
Q

Give 4 examples of fully additive drug combinations?

A

1- diuretics + beta blocker.
2- diuretics + ACEI.
3- CCB + beta blocker.
4- CCB + ACEI.

123
Q

List 4 questionable drug combinations?

A

Non-additive:
1- beta blocker + ACEI.
2- ARB + ACEI.

Side effect additive:
3- beta blocker + verapamil.
4- alpha blocker + CCB.

124
Q

What is the preferred antihypertensive combinations in patients with angina?

A

Beta blocker + CCB.

125
Q

What is the preferred antihypertensive combinations in patients with HF?

A

Diuretic + ACEI.

126
Q

What is the preferred antihypertensive combinations in patients with diabetes?

A

ACEI + CCB.

127
Q

What is the preferred antihypertensive combinations in patients with COPD?

A

Diuretic + CCB.

128
Q

List the drugs which increase plasma renin activity?

A

Diuretics, vasodilators, CCBs, ACEI.

129
Q

List the drugs which lower plasma renin activity?

A

Beta blockers, clonidine, methyldopa.

130
Q

Why should we avoid combining verapamil or diltiazem with beta blockers?

A

Because of marked tachycardia, AV block can occur.

131
Q

Definition: BP that remains elevated despite administration of an optimal three drug regimen that includes a diuretic?

A

Resistant hypertension.

132
Q

List the 4 causes of resistant hypertension?

A

1- poor compliance.
2- excess ethanol intake.
3- concomitant conditions (diabetes, obesity, sleep apnea, hyperalsosteronism, high salt intake, metabolic syndrome).
4 concomitant medications (sympathomimetics, NSAIDs, corticosteroids), insufficient dose, use of drugs with similar mechanism of action.

133
Q

What defines hypertensive emergencies?

A

Systolic BP > 180 or diastolic > 120mmHg, with evidence of impending or progressing end organ end damage.

134
Q

Mean BP should be lowered by no more than _% over a period of ___ or a few ___ and then ___ to not lower than ________ mmHg.

A

Mean BP should be lowered by no more than 25% over a period of mins or a few hrs and then gradually to not lower than 160/100 mmHg.

135
Q

List the 9 drugs employed in hypertensive emergencies?

A

1- sodium nitroprusside.
2- glyceryl trinitrate.
3- hydralazine.
4- esmolol.
5- phentolamine.
6- labetalol.
7- fenoldopam.
8- furosemide.
9- nicardipine.