Anti-hypersensitive - b-blockers Flashcards
Of the list below, which drug is NOT one of the core B-blocker drug we need to be aware of?
1 - Doxazosin
2 - Bisoprolol
3 - Propranolol
4 - Carvedilol
1 - Doxazosin
- this is an alpha blocker
B-blockers, such as Bisoprolol, Propranolol and Carvedilol all bind with which receptor located primarily on cardiac tissue?
1 - alpha 1
2 - beta 1
3 - beta 2
4 - beta 3
2 - beta 1
B-blockers, such as Bisoprolol, Propranolol and Carvedilol primarily bind with beta 1 receptors located on cardiac tissue. Which of the GPCRs pathways does this activate?
1- Gq
2 - Gs
3 - Gi
4 - Gd
2 - Gs
- all B receptors use this pathway
Once catecholamines bind with B receptors they initiate the GPCR Gs. Organised the labels below to show what happens intraceulluarly:
1 - pKA can then phosphorylate inside cell
2 - AC takes 2 phosphates and becomes cyclic adenosine monophosphate (cAMP)
3 - adenylate cyclase (AC) is activate
4 - cAMP activates protein kinase A (pKA)
1 - adenylate cyclase (AC) is activate
2 - AC takes 2 phosphates and becomes cyclic adenosine monophosphate (cAMP).
3 - cAMP activates protein kinase A (pKA)
4 - pKA can then phosphorylate inside cell
What is the mechanism of action of B-blockers?
1 - selectively bind b1 receptors and compete with binding of noradrenaline and adrenaline
2 - non-selectively binds a1 and B1 receptors, inhibiting Acetylcholine binding
3 - selectively bind a-1 receptors and compete with binding of Acetylcholine
4 - non-selectively binds a1 and B1 receptors, inhibiting noradrenaline and adrenaline binding
1 - selectively bind a-1 receptors and compete with binding of noradrenaline and adrenaline
- this is a 2nd generation B-blocker so it is able to selectively bind at the post synapse
- reduces noradrenaline and adrenaline binding
B1 adrenergic receptors typically increase heart rate and contractility in the heart. The use of B-blockers is indicated in ischaemic heart disease (IHD), by improving prognosis in angina and acute coronary syndrome. How do B-blockers improve prognosis in IHD?
1 - increase HR and reduce contractility
2 - reduces HR and increase contractility
3 - increase HR and contractility
4 - decrease HR and contractility
4 - decrease HR and contractility
- this reduces the oxygen demand and cardiac workload, whilst increasing perfusion
B1 adrenergic receptors typically increase heart rate and contractility in the heart. The use of B-blockers is indicated in chronic heart failure (CHF). How do B-blockers improve prognosis in CHF?
1 - reduces parasympathetic stimulation
2 - reduces sympathetic stimulation
3 - increases parasympathetic stimulation
4 - increases sympathetic stimulation
2 - reduces sympathetic stimulation
B1 adrenergic receptors typically increase heart rate and contractility in the heart. The use of B-blockers is indicated in atrial fibrillation (AF) and supra-ventricular tachycardia (SVT). How to B-blockers improve prognosis in AF and SVT?
1 - prolong refractory period of AV node and terminate SVT
2 - reduce refractory period of AV node and terminate SVT
1 - prolong refractory period of AV node and terminate SVT
- essentially the heart cells cannot repolarise quickly enough to maintain AF
B1 adrenergic receptors typically increase heart rate and contractility in the heart. However, they can also be used as a 4th line treatment in resistive hypertension. Although complex, how is it thought that B-blockers are able to reduce hypertension?
1 - inhibit Ca2+ channels in smooth muscle
2 - inhibits renin release
3 - increases aldosterone release
4 - inhibits Angiotensin-converting enzyme
2 - inhibits renin release
- binds B1 receptors on juxtaglomerular cells
- less renin is releases, meaning reduced SVR
B1 adrenergic receptors typically increase heart rate and contractility in the heart. However, they can also be used for migraines. How is it thought that they are able to do this?
1 - reduced dopamine release
2 - reduced glutamate release
3 - reduced neuronal activity in noradrenergic excitability
3 - reduced neuronal activity in noradrenergic excitability
B1 adrenergic receptors typically increase heart rate and contractility in the heart. However, they can also be used in thyroid storm / thyrotoxicosis. How do they help alleviate this?
1 - reduce heart rate
2 - increase heart rate
3 - inhibits pituitary gland
1 - reduce heart rate
- reduces palpitations and tremor
- reduces B-adrenergic up regulation
B-blockers can cause a number of adverse events. Which of the following is NOT a common adverse event?
1 - fatigue
2 - cold extremities
3 - headaches
4 - incontinence
5 - GI upset
6 - sleep disturbance
7 - impotence
4 - incontinence
Which of the following conditions should B-blockers be avoided?
1 - COPD
2 - asthma
3 - diabetes
4 - crohns
2 - asthma
- can cause life threatening bronchospasm
- generally safe in COPD
In patients taking B-blockers for heart failure, should they be started on the normal dose?
- no
- should start on a reduced dose, as cardiac function may initially be impaired
Which of the following conditions are B-blockers ok to be used in?
1 - heart block
2 - severe hypotension
3 - significant hepatic failure
4 - diabetes
4 - diabetes