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Year 1 HLB > Drug Treatment for CV Disease Hypertension > Flashcards

Drug Treatment for CV Disease Hypertension Flashcards

1
Q

What does inotropic mean?

A
  • force of contraction
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2
Q

Adrenergic receptors are part of the sympathetic nervous system, which GPCR do a1 receptors activate?

A
  • Gaq
  • contraction
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3
Q

Adrenergic receptors are part of the sympathetic nervous system, which GPCR do a2 receptors work on?

A
  • Gai
  • inhibition
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4
Q

Adrenergic receptors are part of the sympathetic nervous system, which GPCR do B1 and B2 receptors work on?

A
  • Gas
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5
Q

What are a few of the key functions of the a1 receptors of sympathetic system?

A
  • vasoconstriction of blood vessels
  • ⬆️ sweating
  • ⬆️ bladder sphincter contraction
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6
Q

What are a few of the key functions of the a2 receptors of sympathetic system?

A
  • inhibit release of acetylcholine and insulin
  • not required in fight of flight response
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7
Q

What are a few of the key functions of the b1 receptors of sympathetic system?

A
  • ⬆️ HR
  • ⬆️ contractility
  • ⬆️ renin release
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8
Q

What are a few of the key functions of the b2 receptors of sympathetic system?

A
  • ⬆️ vasodilation of skeletal muscle
  • ⬆️ bronchodilation in lungs
  • ⬆️ gluconeogenesis (glucose production from non carbs)
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9
Q

What is the intra cellular pathway for for B1 and B2 receptors?

A
  • adenylyl cyclase (AC) is released
  • AC converts ATP into cyclic AMP (cAMP) (2nd messenger)
  • cAMP activates protein kinase A (pKA)
  • pKA triggers phosphorylates in cell
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10
Q

How does propranolol work?

A
  • non selective B blocker
  • B receptor antagonist
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11
Q

What are the most common cardiac related used of propranolol?

A
  • hypertension
  • angina
  • arrhythmias
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12
Q

What is a common side effect of propranolol that can be observed in skeletal muscle?

A
  • tremor
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13
Q

What is a common use of propranolol that can be observed in in the brain?

A
  • anxiety
  • migraines
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14
Q

Although beta blockers can reduce BP, increase inotrophic force and redcue heart rate, what is one common cardiac side effect that can be observed?

A
  • bradycardia
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15
Q

Although beta blockers can be effective in the heart, what side effects can they have on the lungs, even if they are specific fo B1 receptors?

A
  • ⬆️ bronchoconstriction
  • ⬆️ breathlessness
  • can be dangerous in asthma patients
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16
Q

Although beta blockers can reduce BP, what are some of the common side effects, which are all generally due to due to lack of blood flow?

A
  • erectile dysfunction
  • cold hands/feet
  • fatigue
  • claudication (pain in calves)
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17
Q

Why are B1 selective blockers better than non-selective beta blockers?

A
  • ⬇️ side effects
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18
Q

What is the most commonly used B1 adrenergic antagonist in the UK that we need to know?

A
  • Bisoprolol
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19
Q

Why are beta blockers dangerous in diabetic patients?

A
  • hypoglycaemia causes ⬆️ release of adrenalin
  • patients experience symptoms associated with hypoglycaemia
  • adrenalin ⬆️ gluconeogenesis
  • beta blockers block adrenalin action
  • ⬆️ risk of hypoglycaemia
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20
Q

What are thiazide and thiazide like diuretic drugs?

A
  • drugs that inhibit reabsorption of Na+, K+ and Cl-
  • H20 loss is increased
  • reduced electrolytes and H2O - ⬇️ BP
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21
Q

What is the most commonly used thiazide in the UK that we need to know?

A
  • Bendroflumethiazide
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22
Q

How does Bendroflumethiazide work?

A
  • blocks Na+Cl- symporter
  • inhibits reabsorption of Na+ and Cl-
  • ⬆️ urine excretion
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23
Q

What is a symporter?

A
  • integral membrane protein
  • transports 2 different molecules across membrane
  • 1 molecule may use energy, 2nd piggy backs on this
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24
Q

In addition to blocking the Na+/Cl- symporter, there is another drug called Indapamide that is able to work through another mechanism, what is this additional mechanism that contributes to a reduction in blood pressure?

A
  • activates K+ ATPase channels in smooth muscle of blood vessels
  • ⬆️ K+ ATPase activation = ⬇️ L-type Ca2+ channel activation
  • reduces vasoconstrcition
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25
Q

What is the main thiazide drug that is able to inhibit Ca2+ release in smooth muscle of blood vessels and induce vasodilation that we need to know called?

A
  • Indapamide
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26
Q

What are the main positive effects on the kidneys of thiazides?

A
  • blocks Na+Cl- symporter
  • ⬇️ Na+ and Cl-
  • ⬆️ H2O loss
  • ⬇️ BP
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27
Q

What are some common side effects of thiazides in the kidney?

A
  • Hyponatraemia (⬇️ Na+)
  • Hypokalaemia (⬇️ K +)
  • Alkalosis (⬇️ H +)
  • Hypercalcaemia (⬆️ Ca2+)
  • Hypomagnesaemia (⬇️ Mg2+)
  • ⬆️ in uric acid (gout)
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28
Q

In addition to BP, what else can thiazides be used to treat?

A
  • oedema
  • ⬇️ Ca2+ in urine helps urinary tract stones
  • nephrogenic diabetes insipidus (⬇️ urine excretion)
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29
Q

a1 receptors work on the Gaq intracellular pathway, what is the normal pathway?

A
  • phospholipase cleaves Pip2 into IP3 and DAG
  • IP3 binds to sarcoplasmic reticulum and ⬆️ Ca2+ release
  • DAG and Ca2+ activate protein kinase C
  • protein kinase C phosphorylates inside cell
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30
Q

What is the most a1 receptor antagonist commonly used drug in UK, and the one we should know?

A
  • Doxazosin
  • a1 receptor antagonist
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31
Q

What is the main effect of Doxazosin?

A
  • vasodilation
  • ⬇️ BP
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32
Q

What are the 2 most common side effects in patients taking Doxazosin?

A

1 - postural hypotension (especially older patients)

  • patients stand up and blood pressure drops

2 - palpitations (reflex tachycardia)

  • HR increase to try and increase BP
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33
Q

Why are Ca2+ blockers an effective blood pressure medication?

A
  • Ca2+ is released into smooth muscle of blood vessels
  • ⬆️ Ca2+ causes vasoconstriction
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34
Q

What is the most commonly used Ca2+ blocker in the uk that we need to know?

A
  • Amlodipine
35
Q

In addition to Amlodipine, there are 2 other commonly used Ca2+ blockers, what are they called and used for most?

A
  • Diltiazem - angina
  • Verapamil - arrhythmias
36
Q

What is the mechanism of action of Ca2+ channel blockers?

A
  • block L type Ca2+ voltage gated channels
  • ⬇️ Ca2+ levels
  • vasodilation follows
37
Q

What Ca2+ channel blockers do to the arterioles?

A
  • ⬆️ vasodilation
38
Q

What Ca2+ channel blockers do to the heart?

A
  • ⬇️ force of contraction
39
Q

What Ca2+ channel blockers do to the SA and NA nodes?

40
Q

Does Amlodipine have any affect on cardiac contractility or SA/NA nodes?

A
  • no
  • only smooth muscle
41
Q

Does Diltiazem have any affect on smooth muscle, cardiac contractility or SA/NA nodes?

A
  • all 3 equally
42
Q

Does Verapamil have any affect on smooth muscle, cardiac contractility or SA/NA nodes?

A
  • small effect on smooth muscle vasodilation
  • large effect on contractility and SA/NA nodes
43
Q

In addition to smooth muscle, cardiac contractility and SA/NA nodes, what other uses may Ca2+ blockers have?

A
  • angina
  • raynauds syndrome (cold extremities)
  • arrhythmias
44
Q

What is the most common side effect of Ca2+ blockers?

A
  • oedema and ankle swelling
45
Q

Why do Ca2+ blockers cause oedema and ankle swelling?

A
  • ⬆️ hydrostatic pressure
  • osmotic and hydrostatic balance is offset
  • fluid remains in tissues rather than being reabsorbed
46
Q

What are some other common side effects of Ca2+ blockers?

A
  • palpitations (reflex tachycardia and postural hypotension)
  • constipation (GIT contractions)
  • flushing (blood flow to skin increases)
  • headache (lack of BP in brain)
  • exacerbation of heart failure (reduced inotrophic fgorce)
47
Q

Where is angiotensinogen, the precursor for angiotensin I produced?

48
Q

Where is renin produced?

49
Q

Where is angiotensin concerting enzyme predominantly produced?

50
Q

How is angiotensinogen turned into angiotensin I?

A
  • renin cleaves amino acids
51
Q

How does angiotensin I become angiotensin II?

A
  • angiotensin concerting enzyme (ACE) claves amino acids
52
Q

What is aldosterone?

A
  • mineralocorticoid steroid hormone
  • produced in zona glomerulosa of the adrenal cortex in the adrenal gland
53
Q

What is the function of aldosterone?

A
  • stimulates kidneys to retain
  • H2O follows Na+
  • ⬆️ Na+ and H20 = ⬆️ blood volume and ⬆️ vasoconstriction
54
Q

What is the anti-diuretic hormone (ADH), and where is it produced?

A
  • produced by hypothalamus
  • pituitary gland stores ADH
  • ADH signals kidneys to retain H2O (⬇️ urine excretion)
  • ADH triggers thirst so increased fluid intake
  • dilutes electrolytes in the plasma maintains osmolarity
55
Q

What are the main purpose of the renin-angiotensin-aldosterone system (RAAS) on vascular and cardiac function?

A
  • regulating blood volume and systemic vascular resistance
  • modulate cardiac output and arterial pressure
56
Q

What are angiotensin concerting enzyme (ACE) inhibitors?

A
  • inhibits conversion of angiotensin 1 to 2
57
Q

What is the effect of an angiotensin concerting enzyme (ACE) inhibitor on the lungs?

A
  • ⬇️ angiotensin 2
  • ⬆️ bradykinin (vasodilator)
58
Q

What is the most commonly used angiotensin concerting enzyme (ACE) inhibitor in the UK that we need to know?

59
Q

In addition to blood pressure, what other serious heart condition can angiotensin concerting enzyme (ACE) inhibitors be used to treat?

A
  • heart failure
  • reduce systemic vascular resistance and heart workload
  • ⬇️ preload and afterload
60
Q

What are some common side effects of angiotensin concerting enzyme (ACE) inhibitors?

A
  • dry cough, likely due to Bradykinin
  • renal impairment, especially if renal function is impaired
  • hyperkalaemia
61
Q

What do angiotensin 2 receptor inhibitors do??

A
  • inhibit the receptors of angiotensin II (Gaq)
62
Q

Why are angiotensin 2 receptor inhibitors better than angiotensin concerting enzyme (ACE) inhibitors in people who may already have a dry cough?

A
  • dry cough is significantly reduced
63
Q

What is the most commonly used angiotensin 2 receptor inhibitor in the UK that we need to know?

64
Q

What are aldosterone inhibitors able to do?

A
  • inhibit Na+ retention
  • ⬆️ Na+ excretion
  • K+ retained
65
Q

What is the most commonly used aldosterone inhibitor in the UK that we need to know?

A
  • Spironolactone
  • K+ must Stay, the S is for the name of the drug
66
Q

What hormone does the structure Spironolactone resemble in the body that has been attributed to the side effects of the drug?

A
  • Gynaecomastia (man boobs) - impaired renal function - hyperkalaemia (⬆️ K+)
67
Q

What are some of common causes of hypertension due to kidney problems?

A
  • chronic kidney disease - renal artery stenosis - aortic coarctation (narrowing of aorta above kidney)
68
Q

What are some of common causes of hypertension due to endocrine problems?

A
  • ⬆️ aldosterone - ⬆️ catecholamines - ⬆️ cortisol - ⬆️ growth hormone
69
Q

What can pregnancy and pre-eclampsia cause?

A
  • hypertension
70
Q

When treating patients with hypertension there are cut off values to determine when to treat patients. What is stage 1?

A
  • BP >140/90 mmHg
  • only treat if end organ damage or diabetes
71
Q

When treating patients with hypertension there are cut off values to determine when to treat patients. What is stage 2?

A
  • 160/100 mmHg
  • once confirmed with 24 BP monitor
72
Q

When treating patients with hypertension there are cut off values to determine when to treat patients. What is stage 3?

A
  • SBP >180 mmHg
  • treat immediately
73
Q

What are the common lifestyle treatment options patients should always be encouraged to follow?

A
  • ⬇️ weight
  • ⬇️ salt intake
  • ⬇️ alcohol intake
  • ⬆️ exercise
74
Q

In patients who are caucasian and younger than 55 years old what is the most common medication prescribed for hypertension?

A
  • ACE inhibitors OR angiotensin 2 receptor inhibitors
75
Q

In patients who have not responded to ACE inhibitors, angiotensin 2 receptor inhibitors, Ca2+ channel blockers or thiazide diuretics alone, what would be the next course of action?

A
  • ACE inhibitors or angiotensin 2 receptor inhibitors combined with a Ca2+ channel blocker
  • ACE inhibitors or angiotensin 2 receptor inhibitors combined with a thiazide diuretic
76
Q

In patients who do not responded stage 1 and 2 of treatment plans, what would be the next course of action?

A
  • ACE inhibitors or angiotensin 2 receptor inhibitors combined with a Ca2+ channel blocker and a thiazide diuretic
77
Q

In patients who are black of any age and >55 years old what is the most common medication prescribed hypertension?

A
  • Ca2+ channel blocker OR a thiazide diuretic
78
Q

In patients do not responded to stages 1-3 of the treatment plans for hypertension, what would be the next course of action?

A
  • further diuretic OR - alpha blocker OR - beta blocker OR - seek specialist advice
79
Q

Why are patients over 55 years old and black patients not prescribed ACE inhibitors or angiotensin 2 receptor inhibitors as the first line treatment for hypertension?

A
  • >55 years = ⬆️ side effects - black patients lack response
80
Q

In patients <80 years old what is the target blood pressure?

A
  • <140/90 mmHg
81
Q

In patients >80 years old what is the target blood pressure?

A
  • <150/90 mmHg
82
Q

In patients with diabetes what is the target blood pressure?

A
  • <135/85 mmHg
83
Q

What does ABCD relate to in the order of drugs given for hypertension?

A
  • A = ACE inhibitors / Angiotensin receptor inhibitors - B = beta blockers - C = L-type Ca2+ channel blockers - D = diuretics

Year 1 HLB (25 decks)

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