Bronchodilator: Muscarinic Antagonist Flashcards
How many types of cholinergic receptors are there?
1 - 5
2 - 4
3 - 3
4 - 2
4 - 2
- muscarinic and nicotinic
In the sympathetic nervous system, which neurotransmitter is released at the preganglionic neuron at the pre-synapse?
1 - acetylcholine
2 - noradrenaline
3 - dopamine
4 - serotonin
1 - acetylcholine
Acetylcholine is released at the preganglionic neuron. Which receptor does acetylcholine bind with at the post synapse of a neuron?
1 - nicotinic receptors
2 - adrenergic receptors
3 - muscarinic receptors
4 - GABA receptors
1 - nicotinic receptors
In the parasympathetic nervous system, which neurotransmitter is released at the postganglionic neuron where it stimulates its target tissue/cells?
1 - acetylcholine
2 - noradrenaline
3 - dopamine
4 - adrenaline
1 - acetylcholine
Acetylcholine is released at the postganglionic neuron where it comes into contact with target tissue/cells Which receptor does acetylcholine bind with at the post synapse of a neuron?
1 - nicotinic receptors
2 - adrenergic receptors
3 - muscarinic receptors
4 - GABA receptors
3 - muscarinic receptors
There are 5 types of muscarinic receptors M1-M5. M1, M3 and M5 all bind with the same GPCR, which one is this?
1 - Gaq
2 - Gai
3 - Gas
1 - Gaq
- M1 also has a little Gai and Gas
There are 5 types of muscarinic receptors M1-M5. M2 and M4 all bind with the same GPCR, which one is this?
1 - Gaq
2 - Gai
3 - Gas
2 - Gai
Gaq GPCR are present on alpha 1 receptors and become active when binding with adrenaline and/or noradrenaline. Organise the following intracellular pathway that occurs when these receptors become active?
1 - IP3 binds with the endoplasmic reticulum and opens Ca2+ channels, leading to increased intracellular Ca2+ and depolarisation
2 - pKC can then phosphorylate target proteins and induce cellular activity
3 - phospholipase C (PLC) becomes activated located in the cell membrane
4 - DAG binds protein kinase C (pKC) which becomes active due to increased Ca2+
5 - PLC cleaves hospholipid called phosphatidylinositol 4,5-bisphosphate (PIP2) forming inositol trisphosphate (IP3), which is soluble and diffuses freely in the cytoplasm, and the other part is diacylglycerol (DAG), bound to the cell membrane
3 - phospholipase C (PLC) becomes activated located in the cell membrane
5 - PLC cleaves hospholipid called phosphatidylinositol 4,5-bisphosphate (PIP2) forming inositol trisphosphate (IP3), which is soluble and diffuses freely in the cytoplasm, and the other part is diacylglycerol (DAG), bound to the cell membrane
1 - IP3 binds with the endoplasmic reticulum and opens Ca2+ channels, leading to increased intracellular Ca2+ and depolarisation
4 - DAG binds protein kinase C (pKC) which becomes active due to increased Ca2+
2 - pKC can then phosphorylate target proteins and induce cellular activity
Muscarinic receptors M2 and M4 have Gai GPCR present. What is the function of the Gai GPCRs?
1 - accentuates the activity of adenylyl cyclase
2 - inhibits adenylyl cyclase
3 - inhibits phospholipase C
4 - inhibits phospho kinase C
2 - inhibits adenylyl cyclase
- essentially inhibits the intracellular pathway of Gas
What is the main purpose of the muscarinic M3 receptors present on smooth muscle in the lungs?
1 - vasodilates smooth muscles
2 - increased permeability of epithelial cells
3 - reduced mucous secretion
4 - induces smooth muscle contraction
4 - induces smooth muscle contraction
- part of parasympathetic nervous system, so involved in rest
Which of the following is the short acting muscarinic antagonist (SAMA) drug do we need to know about?
1 - Formoterol
2 - Ipratropium bromide
3 - Salbutamol
4 - Serevent
2 - ipratropium bromide
Which 2 of the following is the long acting muscarinic antagonist (LAMA) drug do we need to know about?
1 - Formoterol
2 - Ipratropium bromide
3 - Tiotropium
4 - Aclidinium bromide
3 - Tiotropium
4 - Aclidinium bromide
What is the mechanism of action for SAMA and LAMA medications?
1 - inhibit Gas GPCR
2 - inhibit Gaq GPCR
3 - agonist of Gas GPCR
4 - agonist of Gaq GPCR
2 - inhibit Gaq GPCR
- compete with ACh at the post synapse
- essentially have anti-parasympathetic effects
Ipratropium bromide is the SAMA, and Tiotropium and Aclidinium bromide are the LAMAs. Which muscarinic receptor do these drugs target, and which GPCR is present there in lung tissue?
1 - M1 with Gas
2 - M1 with Gaq
3 - M3 with Gaq
4 - M3 with Gas
3 - M3 with Gaq
- essentially reduce/stop bronchoconstriction
- BUT not as effective as Salbutamol (SABA)
The SAMA, Ipratropium bromide typically has two key indications, which are?
1 - chronic preventer in COPD
2 - acute reliever in COPD for acute breathlessness or COPD exacerbation
3 - chronic asthma alongside LABA and inhaled corticosteroid
4 - acute severe asthma alongside salbutamol (SABA)
2 - acute reliever in COPD for acute breathlessness or COPD exacerbation
4 - acute severe asthma alongside salbutamol (SABA)
- generally given via a nebuliser
Which of the following are Tiotropium and Aclidinium bromide, LAMAs indicated in the use of?
1 - prevent breathlessness and exacerbations in COPD in combination with LABA
2 - chronic asthma were LABA and inhaled corticosteroid is insufficient
3 - COPD with features of asthma, combined with LABA and inhaled corticosteroid
4 - all of the above
4 - all of the above
Ipratropium bromide is a muscarinic antagonist of M3, how long can these drugs take to alleviate symptoms and last for?
S = Start
L = Last for
1 - S = 10 mins and L = 3h
2 - S = 30 mins and L = 6h
3 - S = 30 mins and L = 10h
4 - S - 1h and L = 6h
2 - S = 30 mins and L = 6h
- 30 minutes before effective
- 6 hours lasting
Ipratropium bromide is a short acting muscarinic antagonist (SAMA). COPD patients use this daily. How is this drug generally administered in COPD patients?
1 - inhaled using green inhaler (reliever)
2 - inhaled using nebuliser
3 - inhaled using gas re-breathe mask
4 - inhaled using red inhaler
- generally inhaler
- 20-40 μg taken 4 times daily (qds)
Is ipratropium bromide, a muscarinic antagonist, given as a daily inhaler for asthma and COPD?
- no
- just COPD
When is Ipratropium bromide, a short acting muscarinic antagonist (SAMA), given to asthma and COPD patients through a nebuliser?
1 - when they don’t respond to salbutamol (SABA)
2 - when they don’t respond to Formoterol or Salmeterol (LABA)
3 - exacerbations of asthma or COPD symptoms
3 - exacerbations of asthma or COPD symptoms
Is Ipratropium bromide (SAMA) or Salbutamol (SABA) a more effective bronchodilator?
- Salbutamol a SABA
Tiotropium and Aclidinium bromide are long acting muscarinic antagonist (LAMA), and ipratropium bromide is the SAMA. In addition to inducing vasodilation of the smooth muscle in the lungs, what other function do they have in the lungs?
1 - reduce mucus production
2 - modulates mast cells
3 - enhances O2 delivery
4 - inhibits IgE production
1 - reduce mucus production
- enhance mucocillary escalator
Why can the use of SABA and SAMA be effective?
- SABA enhances sympathetic
- SAMA reduces parasympathetic
- essentially both result in bronchodilation
Tiotropium and Aclidinium bromide are long acting muscarinic antagonist (LAMA), how long can these drugs generally last for?
1 - 3-6h
2 - 6-12h
3 - 12-16h
4 - 12-24h
4 - 12-24h
- only need to be prescribed once daily
Aclidinium bromide and tiotropium are long acting muscarinic antagonist (LAMA). How are these drugs generally administered?
1 - inhaled
2 - orally
3 - intravenously
4 - suppository
1 - inhaled
Aclidinium bromide and tiotropium are long acting muscarinic antagonist (LAMA). What are the 2 indications for the use of LAMA drugs?
1 - acute asthma and COPD
2 - COPD and chronic asthma
3 - bronchiectasis and COPD
3 - bronchiectasis and chronic asthma
2 - COPD and chronic asthma
SAMA and LAMA drugs work on the muscarinic receptors which are part of the para-sympathetic system. There may be some side effects, but why are these rare?
1 - large dose of drug is unable to bind M3 receptors
2 - minimal concentration of drug enter systemic circulation
3 - minimal drug is effective once inhaled
2 - minimal concentration of drug enter systemic circulation
if side effects are present, it could be almost anything:
As anti-parasympathetic drugs, SAMA and LAMA can have a broad range of effects. Which of the following is NOT typically one of these?
1 - dry mouth
2 - bradycardia
3 - blurred vision
4 - closed-angle glaucoma
5 - urinary retention
6 - cardiac arrhythmias
7 - taste disturbance
8 dizziness
epistaxis
2 - bradycardia
- typically results in tachycardia and arrhythmias
