Pharmacology > Hypertension > Flashcards

Hypertension Flashcards

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1
Q

Name the major risk factors for cardiovascular disease (CVD)

A 
Diabetes mellitus
Hypertension
Obesity
Smoking
Dyslipidemia
Family hx of primary hypertension or premature CVD in men <55yo and women <65yo
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2
Q

Name examples of target organ damage (TOD) seen in hypertensive disease

A

Left ventricular hypertrophy
Microalbuminuria
Elevated creatinine levels

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3
Q

Name associated clinical conditions (ACC) of hypertensive disease

A 
Ischaemic heart disease
- angina
- prior myocardial infarction
Heart failure
Stroke/TIA
Chronic kidney disease
Retinopathy
Peripheral arterial disease
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4
Q

What is the cause of a treatment-resistant state in hypertensive disease?

A

Vascular damage

Renal damage

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5
Q

Each 2mmHg rise in SBP is assoc with increased risk of mortality due to?

A

7% from heart disease

10% from stroke

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6
Q

Complications of hypertension

A 
Stroke (60-70%)
Heart failure (50%)
Heart attack (25%)
Kidney failure (20%)
Dementia
Sexual dysfunction
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7
Q

Epidemiology of hypertension

A

Influenced by age + lifestyle factors
50% of those over 60yo have HT
As population ages, HT and required treatment increases

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8
Q

Clinical signs of high blood pressure?

A 
Fatigue
Decreased activity tolerance
Dizziness
Palpitations
Angina
Dyspnoea
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9
Q

Organs that undergo target organ damage from hypertensive disease?

A

CVS (heart and blood vessels)
Kidneys
Nervous system
Eyes

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10
Q

Definition of primary hypertension

A

AKA essential hypertension
95% of hypertensive cases
Idiopathic

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11
Q

Definition of secondary hypertension

A 
Secondary to other potentially rectifiable causes
Less common (5%)
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12
Q

Lifestyle change recommendations to reduce blood pressure and/or cardiovascular risk factors in hypertensive disease

A

Salt intake (restrict 5-6g/day)
Moderate alcohol intake (limit to 20-30g/day men OR 10-20g/day women)
Increase vegetables, fruit
Low fat dairy intake
BMI (<25kg/m2)
Waist circumference (men <102cm/40in; women<88cm/34in)
Exercise (>30min/day 5-7 days/week)

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13
Q

Hypertension pharmacotherapy options

A 
Central agents
Catecholamine inhibitors
Vasodilators
Aldosterone blockers
Diuretics
ACE inhibitors
Angiotensi-1 receptor blockers
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14
Q

Factors influencing pharmacotherapy choice to treat hypertension

A

Concomitant diseases
Patient’s ethnicity
Drug profile S/E
Allergy

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15
Q

Thiazides
Type
Examples
Mechanism of action

A

Low ceiling diuretics
Hydrochlorothiazide, chlorthalidone

Main: Inhibit Na+ and Cl- transporter in distal convoluted tubules -> increased Na+ and Cl- excretions
Other:
a) weak inhibitors of carbonic anhydrase -> increased HCO3- excretion
b) increased K+/Mg2+ excretion
c) decreased Ca2+ excretion

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16
Q

Thiazides
Type
Examples
Mechanism of action

A

Low ceiling diuretic
Hydrochlorothiazide, chlorthalidone, chlorothiazide, indapamide, metozalone

Main: Inhibit Na+ and Cl- transporter in distal convoluted tubules -> increased Na+ and Cl- excretions
Other:
a) weak inhibitors of carbonic anhydrase -> increased HCO3- excretion
b) increased K+/Mg2+ excretion
c) decreased Ca2+ excretion

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17
Q

What is the brand name of hydrochlorothiazide?

A

Microzide

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18
Q

What is the brand name of chlorothiazide?

A

Diuril

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19
Q

Name potential side effects of thiazides

A 
Hypokalemia
Hypovolemia
Hyperuricemia
Metabolic adverse drug reaction (ADR) -> mostly after high dose -> impaired glucose tolerance + dyslipidaemia
Erectile dysfunction
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20
Q

Aldosterone receptor blockers
Type
Examples
Mechanism of action

A

Potassium sparing diuretics
Spirinolactone

Binds and blocks aldosterone receptors -> reduce Na+ and water reabsorption -> decreased SVR -> decreased BP

Considered a weak diuretic
Often used on cinjunction w/ more potent K+ depleting diuretics

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21
Q

Name potential side effects of aldosterone receptor blockers

A 
If patient has renal impairment, uses ACE drugs or potassium supplement -> MONITOR CLOSELY for hyperkalemia
Gynecomastia
Amenorrhoea
Post-menopausal bleeding
Dizziness
Cramps
Nausea
Diarrhea
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22
Q

Calcium channel blockers
Examples
Mechanism of action

A

Amlodipine, nifedipine, verapamil

Act on voltage dependent Ltype Ca2+ channels -> reduce Ca2+ influx -> smooth muscle relaxation + vasodilation
Effectively treat systolic HT
Potentially superior to other antiHT for stroke prevention
Effective in patient’s with comorbid conditions e.g Reynaud’s, migraine
Particularly effective in the elderly and african americans

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23
Q

Which class of antihypertensive drug is particularly effective in the elderly and african americans?

A

Calcium channel blockers

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24
Q

Which class of antihypertensive drug effectively treats systolic hypertension?

A

Calcium channel blockers

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25
Which class of antihypertensive drug is the potentially superior antiHT drug for stroke prevention?
Calcium channel blockers
26
Which class of antihypertensive drug is effective in patient's with comorbid conditions e.g Raynaud's, migraine?
Calcium channel blockers
27
Classification of calcium channel blockers
Phenylalkylamines Benzothiazepines Dihydroxypyridines
28
Classification of calcium channel blockers | Phenylalkylamines
Verapamil
29
Classification of calcium channel blockers | Benzothiazepines
Diatezem
30
Classification of calcium channel blockers | Dihydropyridines
``` 1st generation - nifedipine 2nd generation - isradipine - nicardipine - felodipine 3rd generation - amlodipine ```
31
Cardiovascular effects of diatezem
``` Calcium channel blocker (benzothiazepines) Vasodilation +++ Suppression of cardiac contractility ++ Automaticity suppression (SA node) +++++ Conduction suppression (AV node) ++++ ```
32
Cardiovascular effects of verapamil
``` Calcium channel blocker (phenylalkylamines) Vasodilation ++++ Suppression of cardiac contractility ++++ Automaticity suppression (SA node) +++++ Conduction suppression (AV node) +++++ ```
33
Cardiovascular effects of nifedipine
``` Calcium channel blocker (dihydropyridines) Vasodilation +++++ Suppression of cardiac contractility + Automaticity suppression (SA node) + Conduction suppression (AV node) 0 ```
34
Cardiovascular effects of amlodipine
``` Calcium channel blocker (dihydropyridines) Vasodilation +++++ Suppression of cardiac contractility + Automaticity suppression (SA node) + Conduction suppression (AV node) 0 ```
35
``` Which of the following drugs results in the most vasodilation? Verapamil Diatazem Nifedipine Amlodipine ```
Nifedipine Amlodipine (the dihyropyridines)
36
``` Which of the following drugs results in the least vasodilation? Verapamil Diatazem Nifedipine Amlodipine ```
Verapamil
37
``` Which of the following drugs results in the most suppression of cardiac contractility? Verapamil Diatazem Nifedipine Amlodipine ```
Diatazem
38
``` Which of the following drugs results in the least suppression of cardiac contractility? Verapamil Diatazem Nifedipine Amlodipine ```
Nifedipine | Amlodipine
39
``` Which of the following drugs results in the most automaticity suppression? Verapamil Diatazem Nifedipine Amlodipine ```
Verapamil | Diatzaem
40
``` Which of the following drugs results in the least automaticity suppression? Verapamil Diatazem Nifedipine Amlodipine ```
Nifedipine | Amlodipine
41
``` Which of the following drugs results in the most conduction suppression? Verapamil Diatazem Nifedipine Amlodipine ```
Diatazem
42
``` Which of the following drugs results in the least conduction suppression Verapamil Diatazem Nifedipine Amlodipine ```
Nifedipine | Amlodipine
43
What are potential side effects of dihydropyridines?
``` Peripheral oedema Reflex tachycardia Flushing Headache Hypotension ```
44
What are potential side effects of non-dihydropyridines?
Constipation | Conduction abnormalities
45
Angiotensin converting enzyme (ACE) inhibitors Examples Mechanism of action
Enalapril, benazepril, captopril, lisinopril, fosinopril, quinapril, ramipril, moexipril, trandolapril, perindopril Prevents conversion of angiotensin I -> angiotensin II -> prevents vasoconstriciton + aldosterone release
46
What are advantages of using ACE inhibitors?
Reduce mortality in left ventricular dysfunction Prevent progressive post-infarct cardiac failure Reduce cardiovascular outcomes in high risk patient Reno-protective in diabetics + renal disease w/ proteinuria Lack deleterious effect on glucose tolerance + blood lipids
47
What are side effects of using ACE inhibitors?
``` Dry cough Angioedema Hyperkalemia First dose hypotension Reversible taste disturbance ```
48
What are contraindications for using ACE inhibitors?
Renal artery stenosis | Pregnancy
49
When must one take caution when using ACE inhibitors?
Pre-existing eGFR <20
50
ACE-inhibitors versus angiotensin receptor blockers (ARB)
ARBs do not prevent bradikinin inactivation -> less dry cough + angioedema 75% ACE-I vs 95% AB RAAS blockade No difference in clinical endpoints Choice of therapy guided by cost + tolerability
51
Angiotensin receptor blockers | Examples
Losartan, valsarta, irbesartan, telmisartan, candesartan, eprosartan
52
Direct vasodilators
Hydralazine Minoxidil Sodium nitroprusside Diazoxide
53
Direct vasodilators | Mechanism of action of hydralazine
Dilates arterioles but not veins
54
Direct vasodilators | Mechanism of action of minoxidil
Opens K+ channels in smooth muscles with its active metabolite
55
Direct vasodilators | Mechanism of action of sodium nitroprusside
Increases intracellular GMP ad dilates both aa and vv
56
Direct vasodilators | Mechanism of action of diazoxide
Stimulates opening of K+ channels
57
Which direct vasodilator is a powerful vasodilator for treatment of hypertensive emergencies? And an alternative to this?
Sodium nitroprusside | Can also use diazoxide
58
Centrally acting agents Examples Mechanism of action Side effects
Alpha agonists, adrenergic receptor blockers Stimulates central alpha 2 receptors which results in inhibiting efferent sympathetic activity Should be used 3rd/4th line Can be addictive (e.g clonidine, methyldopa) Sedation, orthostatic hypotension
59
Centrally acting agents Clonidine Mechanism of action S/E
Alpha-2 agonist -> reduces norepinephrine production w/o stimulating sympathetic nervous system -> vasodilation -> decreased BP S/E sedation, dry mouth, Na+ retention, water retention
60
Centrally acting agents Alpha-methyldopa Mechanism of action S/E
Alpha-methylnorepinephrine stored in neurosecretory vesicles instead of NE -> released -> alpha-receptor agonist S/E sedation, lassitude, nightmares, lactation (due to dopaminergic neuron inhibition)
61
Examples of beta 1 selective adrenergic receptor blockers
Atenolol, bisoprolol, metoprolol
62
Examples of beta 1 + 2 adrenergic receptor blockers
Propanolol (lipophilic)
63
Examples of alpha, beta 1 and beta 2 receptor blockers
Carvedilol (lipophilic), labetolol
64
What is the name of the active metabolite of alpha-methyldopa?
Alpha-methylnorepinephrine
65
What is the significance of a lipophilic adrenergic receptor blocker?
Can cross the blood brain barrier
66
Name mortality reducing beta blockers
Carvedilol Bisoprolol Nebivilol Metoprolol
67
Atenolol Class Caution Contraindications
4th line antihypertensive - ONLY use in pt with comorbid angina or uncontrolled hypertension Cardioselective beta blocker (least lipophilic) Caution: elderly, renal failure Contraindications: asthma, symptomatic cardiac failure, Av block, bradycardia
68
When is the only time you give atenolol as antihypertensive treatment?
ONLY use in pt with (1) comorbid angina or (2) uncontrolled hypertension
69
Why do you take caution when prescribing atenolol to an elderly or renal failure patient?
Excreted unchanged in urine | Can accumulate if low GFR
70
How is carvedilol excreted?
Via bile
71
What is the use of beta blockers in COPD patient with severe hypertension?
Benefit versus risk assessment | Little reversibility + not severe COPD -> carvedilol benefit outweighs bronchospasm risk
72
Definition and classification of severe hypertension
SBP>180mmHg and DBP >110mmHg 1. Asymptomatic severe 2. Hypertensive urgency 3. Hypertensive emergency
73
Definition of asymptomatic severe hypertension
SBP>180mmHg and DBP >110mmHg Asymptomatic No TOD No ACC
74
Definition of hypertensive emergency
SBP>180mmHg and DBP >110mmHg | Assoc w/ acute and ongoing damage to kidneys, brain, heart, eyes or vascular system
75
What grade retinopathy qualifies as TOD during hypertensive emergency
Grade 3/4
76
Definition of hypertensive urgency
SBP>180mmHg and DBP >110mmHg Severe headache, SOB, oedema No immediate life-threatening neuro, renal, eye or cardiac complications
77
``` Glyceryl trinitrate Drug class Mechanism of action Side effects Contraindications ```
Organ nitrates Venodilation -> decrease preload via coronary vasodilation SE: hypotension, headache CI: hypertrophic obstructive cardiomyopathy (HOCM)
78
Which common drug does glyceryl trinitrate interact with?
Sildenafil (potentiates vasodilation) | PDE5 inhibitor with tadalafil, verdenafil
79
``` Furosemide Drug class Mechanism of action Side effects Caution ```
High ceiling loop diuretic Inhibits Na+ and Cl- reabsorption in the ascending limb of Henle -> venodilation -> decreased venous return IV is very fast acting SE:: hypotension, hypovolemic shock, ototoxicity if given in large IV doses therefore give slow at 4mg/min
80
Why must you give furosemide slowly at 4mg/min?
Can cause hypotension, hypovolemic shock, ototoxicity if given in large IV doses
81
How does decreased renal function affect furosemide treatment?
Patient requires a higher dose
82
What site do organic acids compete with drug transport for?
Lumen side of ascending limb of Henle
83
Special populations to consider in antihypertensive treatment
``` Africans Left ventricular hypertrophy (LVH) Elderly Pregnancy Children/adolescents ```
84
What is important to remember when providing african patients with anti-hypertensive treatment?
Response to diuretics + CCB > ACE-I, ARB, beta blockers | Angioedema 2x-4x more
85
What is important to remember when providing elderly patients with anti-hypertensive treatment?
Isolated systolic hypertension Same general principles Thiazide/CCB may be better tolerated
86
What is important to remember when providing pregnant patients with anti-hypertensive treatment?
Methyldopa, beta-blockers + vasodilators (hydralazine) are options Avoid ACE-Is and ARBs
87
What is important to remember when providing left ventricular hypertrophy patients with anti-hypertensive treatment?
Aggressive BP control allows LVH to regress but NOT w/ hydralazine or minoxidil
88
What is important to remember when providing children/adolescent patients with anti-hypertensive treatment?
Avoid ACE-I or ARBs in pregnant or sexually active girls
89
Safest anti-hypertensive options for pregnant woman with pre-existing hypertension?
Methyldopa Nifedipine Labetalol Diuretics + beta blockers still C/I from 2nd trimester because of fetal growth retardation and electrolyte imbalances
90
Pre-eclampsia Time of onset Clinical presentation Treatment
Usually after 20 weeks of pregnancy Hypertension, oedema, proteinuria,hyperuricemia Bed rest + antiHT
91
Pre-eclampsia | Complications
``` Convulsions Cerebral haemorrhage Abruptio placentae Pulmonary oedema Renal failure ```
92
Recommended anti-hypertensives in heart failure
Diuretic Beta blocker ACE-I ARB
93
Recommended anti-hypertensives in post MI
Beta blocker | ACE-I
94
Recommended anti-hypertensives in high coronary disease risk
Diuretic Beta blocker ACE-I CCB
95
Recommended anti-hypertensives in diabetes
Diuretic ACE-I ARB CCB
96
Recommended anti-hypertensives in chronic kidney disease
ACE-I | ARB
97
Recommended anti-hypertensives in recurrent stroke prevention
Diuretic | ACE-I
98
"Compelling indications" for a drug means?
Literature has proven it superior treatment in that medical situation
Pharmacology
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