Drug Treatment for CV Disease Hypertension Flashcards
(83 cards)
1
Q
What does inotropic mean?
A
- force of contraction
2
Q
Adrenergic receptors are part of the sympathetic nervous system, which GPCR do a1 receptors activate?
A
- Gaq
- contraction
3
Q
Adrenergic receptors are part of the sympathetic nervous system, which GPCR do a2 receptors work on?
A
- Gai
- inhibition
4
Q
Adrenergic receptors are part of the sympathetic nervous system, which GPCR do B1 and B2 receptors work on?
A
- Gas
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
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
7
Q
What are a few of the key functions of the b1 receptors of sympathetic system?
A
- ⬆️ HR
- ⬆️ contractility
- ⬆️ renin release
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)
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
10
Q
How does propranolol work?
A
- non selective B blocker
- B receptor antagonist
11
Q
What are the most common cardiac related used of propranolol?
A
- hypertension
- angina
- arrhythmias
12
Q
What is a common side effect of propranolol that can be observed in skeletal muscle?
A
- tremor
13
Q
What is a common use of propranolol that can be observed in in the brain?
A
- anxiety
- migraines
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
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
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)
17
Q
Why are B1 selective blockers better than non-selective beta blockers?
A
- ⬇️ side effects
18
Q
What is the most commonly used B1 adrenergic antagonist in the UK that we need to know?
A
- Bisoprolol
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
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
21
Q
What is the most commonly used thiazide in the UK that we need to know?
A
- Bendroflumethiazide
22
Q
How does Bendroflumethiazide work?
A
- blocks Na+Cl- symporter
- inhibits reabsorption of Na+ and Cl-
- ⬆️ urine excretion
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
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
25
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?
- Indapamide
26
What are the main positive effects on the kidneys of thiazides?
- blocks Na+Cl- symporter
- ⬇️ Na+ and Cl-
- ⬆️ H2O loss
- ⬇️ BP
27
What are some common side effects of thiazides in the kidney?
- Hyponatraemia (⬇️ Na+)
- Hypokalaemia (⬇️ K +)
- Alkalosis (⬇️ H +)
- Hypercalcaemia (⬆️ Ca2+)
- Hypomagnesaemia (⬇️ Mg2+)
- ⬆️ in uric acid (gout)
28
In addition to BP, what else can thiazides be used to treat?
- oedema
- ⬇️ Ca2+ in urine helps urinary tract stones
- nephrogenic diabetes insipidus (⬇️ urine excretion)
29
a1 receptors work on the Gaq intracellular pathway, what is the normal pathway?
- 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
30
What is the most a1 receptor antagonist commonly used drug in UK, and the one we should know?
- Doxazosin
- a1 receptor antagonist
31
What is the main effect of Doxazosin?
- vasodilation
- ⬇️ BP
32
What are the 2 most common side effects in patients taking Doxazosin?
1 - postural hypotension (especially older patients)
- patients stand up and blood pressure drops
2 - palpitations (reflex tachycardia)
- HR increase to try and increase BP
33
Why are Ca2+ blockers an effective blood pressure medication?
- Ca2+ is released into smooth muscle of blood vessels
- ⬆️ Ca2+ causes vasoconstriction
34
What is the most commonly used Ca2+ blocker in the uk that we need to know?
- Amlodipine
35
In addition to Amlodipine, there are 2 other commonly used Ca2+ blockers, what are they called and used for most?
- Diltiazem - angina
- Verapamil - arrhythmias
36
What is the mechanism of action of Ca2+ channel blockers?
- block L type Ca2+ voltage gated channels
- ⬇️ Ca2+ levels
- vasodilation follows
37
What Ca2+ channel blockers do to the arterioles?
- ⬆️ vasodilation
38
What Ca2+ channel blockers do to the heart?
- ⬇️ force of contraction
39
What Ca2+ channel blockers do to the SA and NA nodes?
- ⬇️ HR
40
Does Amlodipine have any affect on cardiac contractility or SA/NA nodes?
- no
- only smooth muscle
41
Does Diltiazem have any affect on smooth muscle, cardiac contractility or SA/NA nodes?
- all 3 equally
42
Does Verapamil have any affect on smooth muscle, cardiac contractility or SA/NA nodes?
- small effect on smooth muscle vasodilation
- large effect on contractility and SA/NA nodes
43
In addition to smooth muscle, cardiac contractility and SA/NA nodes, what other uses may Ca2+ blockers have?
- angina
- raynauds syndrome (cold extremities)
- arrhythmias
44
What is the most common side effect of Ca2+ blockers?
- oedema and ankle swelling
45
Why do Ca2+ blockers cause oedema and ankle swelling?
- ⬆️ hydrostatic pressure
- osmotic and hydrostatic balance is offset
- fluid remains in tissues rather than being reabsorbed
46
What are some other common side effects of Ca2+ blockers?
- 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
Where is angiotensinogen, the precursor for angiotensin I produced?
- liver
48
Where is renin produced?
- kidneys
49
Where is angiotensin concerting enzyme predominantly produced?
- in lungs
50
How is angiotensinogen turned into angiotensin I?
- renin cleaves amino acids
51
How does angiotensin I become angiotensin II?
- angiotensin concerting enzyme (ACE) claves amino acids
52
What is aldosterone?
- mineralocorticoid steroid hormone
- produced in zona glomerulosa of the adrenal cortex in the adrenal gland
53
What is the function of aldosterone?
- stimulates kidneys to retain
- H2O follows Na+
- ⬆️ Na+ and H20 = ⬆️ blood volume and ⬆️ vasoconstriction
54
What is the anti-diuretic hormone (ADH), and where is it produced?
- 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
What are the main purpose of the renin-angiotensin-aldosterone system (RAAS) on vascular and cardiac function?
- regulating blood volume and systemic vascular resistance
- modulate cardiac output and arterial pressure
56
What are angiotensin concerting enzyme (ACE) inhibitors?
- inhibits conversion of angiotensin 1 to 2
57
What is the effect of an angiotensin concerting enzyme (ACE) inhibitor on the lungs?
- ⬇️ angiotensin 2
- ⬆️ bradykinin (vasodilator)
58
What is the most commonly used angiotensin concerting enzyme (ACE) inhibitor in the UK that we need to know?
- Ramipril
59
In addition to blood pressure, what other serious heart condition can angiotensin concerting enzyme (ACE) inhibitors be used to treat?
- heart failure
- reduce systemic vascular resistance and heart workload
- ⬇️ preload and afterload
60
What are some common side effects of angiotensin concerting enzyme (ACE) inhibitors?
- dry cough, likely due to Bradykinin
- renal impairment, especially if renal function is impaired
- hyperkalaemia
61
What do angiotensin 2 receptor inhibitors do??
- inhibit the receptors of angiotensin II (Gaq)
62
Why are angiotensin 2 receptor inhibitors better than angiotensin concerting enzyme (ACE) inhibitors in people who may already have a dry cough?
- dry cough is significantly reduced
63
What is the most commonly used angiotensin 2 receptor inhibitor in the UK that we need to know?
- Losartan
64
What are aldosterone inhibitors able to do?
- inhibit Na+ retention
- ⬆️ Na+ excretion
- K+ retained
65
What is the most commonly used aldosterone inhibitor in the UK that we need to know?
- Spironolactone
- K+ must Stay, the S is for the name of the drug
66
What hormone does the structure Spironolactone resemble in the body that has been attributed to the side effects of the drug?
- Gynaecomastia (man boobs) - impaired renal function - hyperkalaemia (⬆️ K+)
67
What are some of common causes of hypertension due to kidney problems?
- chronic kidney disease - renal artery stenosis - aortic coarctation (narrowing of aorta above kidney)
68
What are some of common causes of hypertension due to endocrine problems?
- ⬆️ aldosterone - ⬆️ catecholamines - ⬆️ cortisol - ⬆️ growth hormone
69
What can pregnancy and pre-eclampsia cause?
- hypertension
70
When treating patients with hypertension there are cut off values to determine when to treat patients. What is stage 1?
- BP \>140/90 mmHg
- only treat if end organ damage or diabetes
71
When treating patients with hypertension there are cut off values to determine when to treat patients. What is stage 2?
- 160/100 mmHg
- once confirmed with 24 BP monitor
72
When treating patients with hypertension there are cut off values to determine when to treat patients. What is stage 3?
- SBP \>180 mmHg
- treat immediately
73
What are the common lifestyle treatment options patients should always be encouraged to follow?
- ⬇️ weight
- ⬇️ salt intake
- ⬇️ alcohol intake
- ⬆️ exercise
74
In patients who are caucasian and younger than 55 years old what is the most common medication prescribed for hypertension?
- ACE inhibitors OR angiotensin 2 receptor inhibitors
75
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?
- 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
In patients who do not responded stage 1 and 2 of treatment plans, what would be the next course of action?
- ACE inhibitors or angiotensin 2 receptor inhibitors combined with a Ca2+ channel blocker and a thiazide diuretic
77
In patients who are black of any age and \>55 years old what is the most common medication prescribed hypertension?
- Ca2+ channel blocker OR a thiazide diuretic
78
In patients do not responded to stages 1-3 of the treatment plans for hypertension, what would be the next course of action?
- further diuretic OR - alpha blocker OR - beta blocker OR - seek specialist advice
79
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?
- \>55 years = ⬆️ side effects - black patients lack response
80
In patients \<80 years old what is the target blood pressure?
- \<140/90 mmHg
81
In patients \>80 years old what is the target blood pressure?
- \<150/90 mmHg
82
In patients with diabetes what is the target blood pressure?
- \<135/85 mmHg
83
What does ABCD relate to in the order of drugs given for hypertension?
- A = ACE inhibitors / Angiotensin receptor inhibitors - B = beta blockers - C = L-type Ca2+ channel blockers - D = diuretics
