Cholinergic receptor
| A | Action potentials on the alpha motor neuron release acetylcholine (Ach) from the axon terminal | |
| B |
Ach stimulates nicotinic cholinergic receptors on the muscle endplate |
|
| C |
Cholinergic receptors on the muscle endplate are cation channels |
|
| D |
Alpha motor neurons excite, and Renshaw cells inhibit, the muscle endplate |
All of the following statements regarding activity at the neuromuscular junction are true except:
| A |
Action potentials on the alpha motor neuron release acetylcholine (Ach) from the axon terminal |
|
| B |
Ach stimulates nicotinic cholinergic receptors on the muscle endplate |
|
| C |
Cholinergic receptors on the muscle endplate are cation channels |
|
| D |
Alpha motor neurons excite, and Renshaw cells inhibit, the muscle endplate |
There are no Renshaw cells at the neuromuscular junction. Renshaw cells inhibit motor neurons in the anterior gray horn of the spinal cord. Action potentials on the alpha motor neuron release acetylcholine (ACh) from the axon terminal. The ACh diffuses across the synaptic cleft and stimulates nicotinic receptors on the muscle endplate, generating an action potential that causes contraction of the muscle fiber. Cholinergic receptors on the muscle endplate are cation channels.
In Myasthenia gravis, antibodies are present against –
| A |
Muscarinic receptor proteins |
|
| B |
Nicotinic receptor proteins |
|
| C |
Protein actin |
|
| D |
Protein myosin |
Ans. is ‘b’ i.e., Nicotinic receptor proteins
o Myasthenia gravis is an autoimmune disorder due to development of antibodies against Nm type of nicotinic receptors.
Nicotine receptor sites include all of the following except-
| A |
Bronchial smooth muscle |
|
| B |
Adrenal medulla |
|
| C |
Skeletal muscle |
|
| D |
Sympathetic ganglia |
Ans. is ‘a’ i.e., Bronchial smooth muscle
- Smooth muscles have muscarinic receptors (M3 type).
| A |
Bethanechol |
|
| B |
Carbachol |
|
| C |
Pilocarpine |
|
| D |
Methacholine |
Ans. is ‘b’ i.e., Carbachol
o Amongst the given options carbachol has maximum nicotinic actions. It has nicotinic as well as muscarinic action.
All of the following are actions of muscarinic antogonists, except :
| A |
Decrease gastric secretions |
|
| B |
Decrease respiratory secretions |
|
| C |
Contract radial muscles of iris |
|
| D |
Fascilitates AV conduction |
Ans is ‘c’ i.e. Contract radial muscles of iris
- Radial muscles are innervated by sympathetic systems not by parasympathetic (muscarinic) system
Iris muscles that control the size of pupil
There are two types of muscles in iris that control the size of pupil:
- The iris sphincter or constrictor pupillae (circular muscles): These muscles are innervated by the parasympathetic system and cause constriction of pupil (miosis).
- The iris dilator or dilator pupillae (radial muscles): These muscles are innervated by sympathetic (a, adrenergic) system and cause dilatation of pupil (mydriasis)
- So, pupil size may be altered by following mechanisms by different ANS drugs:
A. Mydriasis (dilatation of pupil)
- Sympathomimetic drugs (a, agonists): By contraction of radial muscles (dilator).
- Antimuscarinic drugs: By blocking the action of circular muscles (pupillary sphincter).
B. Miosis (constriction of pupil)
- Parasympathomimetic (muscarinic) drgus: By stimulating the contraction of circular muscles (pupillary sphincter).
- Sympatholytic drugs (a, antagonists): By blocking the action of radial muscles (iris dilator) About other options
- Muscarinic antagonists (antimuscarinic drugs) decrease both gastric and respiratory (bronchial) secretions o Antimuscarinic drugs facilitate AV conduction (see previous explanations).
| A | Nicotinic receptor stimulation | |
| B |
Muscarinic receptor stimulation |
|
| C |
Muscarinic receptor inhibition |
|
| D |
a-receptor inhibition |
Ans. is ‘c’ i.e., Muscarinic receptor inhibition
Oxybutnin
o Oxybutynin is an anticholinergic drug.
o It is relatively selective for M3 receptors, so it has selective action on urinary bladder.
- Because of its vesicoselective action it is used for detrusor instability and urinary incontinence.
| A | Inhibiting nicotinic receptors at myoneural junction | |
| B |
Inhibiting nicotinic receptors at autonomic ganglion |
|
| C |
Producing depolarizing block |
|
| D |
By inhibiting reuptake of acetylcholine |
Ans. is ‘a’ i.e., Inhibiting nicotinic receptors at myoneural junction
o D-tubocurarine is a skeletal muscle relaxant that acts by competitive inhibition of NM receptors at neuron-muscular junction.
Dry mouth during antidepressant therapy is caused by blockade of –
| A |
Muscarinic acetylcholine receptors |
|
| B |
Serotonergic receptors |
|
| C |
Dopaminergic receptors |
|
| D |
GABA receptors |
Ans. is ‘a’ i.e., Muscarinic acetylcholine receptors
“Blurred vision, dry mouth, urinary hesitancy or retention, and constipation represent the most common antimuscarinic complaints”.
Nicotinic receptors are seen in all except:
September 2007
| A |
Neuromuscular junction |
|
| B |
Autonomic ganglia of autonomic nervous system |
|
| C |
Bronchial smooth muscle |
|
| D |
Brain |
Ans. C: Bronchial Smooth Muscle
The nicotinic cholinergic receptors are found in the neuromuscular junctions of somatic muscles; stimulation of these receptors causes muscular contraction. They are also found in the autonomic ganglia of autonomic nervous system and
central nervous system
Muscarinic receptors are found in:
M 1-brain M 2-heart
M 3-smooth muscle
M 4-smooth muscle, pancreatic acinar and islet tissue
| A | Muscarinic receptor proteins | |
| B |
Nicotinic receptor proteins |
|
| C |
Protein actin |
|
| D |
Protein myosin |
Myasthenia gravis
- It is an autoimmune neuromuscular disease leading to fluctuating muscle weakness and fatigue.
- It is an autoimmune disorder, in which weakness is caused by circulating antibodies that block acetylcholine receptors at the postsynaptic neuromuscular junction, inhibiting the excitatory effects of the neurotransmitter acetylcholine on nicotinic receptors throughout neuromuscular junctions.
- Myasthenia is treated medically with acetylcholinesterase inhibitors or immunosuppressants, and, in selected cases,thymectomy.
September 2009
| A |
Dopamine reuptake stimulator |
|
| B |
It is an antianxiety drug |
|
| C |
No precipitation of seizures |
|
| D |
Nicotinic receptor antagonist |
Ans. D: Nicotinic receptor antagonist
Bupropion/amfebutamone is an atypical antidepressant and smoking cessation aid.
It acts as a norepinephrine and dopamine reuptake inhibitor (NDRI), as well as alpha3 beta4-nicotinic receptor antagonist.
Bupropion belongs to the chemical class of aminoketones and is similar in structure to stimulants cathinone and diethylpropion, and to phenethylamines in general.
Bupropion is an effective antidepressant on its own but it is particularly popular as an add-on medication in the cases of incomplete response to the first-line selective serotonin reuptake inhibitor (SSRI) antidepressant.
Since it does not inhibit serotonin reuptake at all (or very insignificantly), bupropion does not cause weight gain or sexual dysfunction like the SSRI group of antidepressants.
It precipitates seizures
CMC (Vellore) 13
| A | Neostigmine | |
| B |
Pralidoxime |
|
| C |
Prazocin |
|
| D |
Naloxone |
Ans. Neostigmine
Acetylcholine acting on nicotinic receptors produces:
KCET 12
| A |
Contraction of skeletal muscle |
|
| B |
Secretion of saliva |
|
| C |
Bradycardia |
|
| D |
Pupillary constriction |
Ans. Contraction of skeletal muscle
Which of the following is an ionic channel ‑
| A |
α -1 receptors |
|
| B |
β – 1 receptors |
|
| C |
Nicotinic cholinergic receptors |
|
| D |
Muscarinic cholinergic receptors |
Ans. is ‘c’ i.e., Nicotinic cholinergic receptors
Varenicline acts by ‑
| A |
Partial nicotine receptor agonist |
|
| B |
Nicotine receptor antagonist |
|
| C |
Both agonist and antagonist at nicotine receptor |
|
| D |
None of the above |
Ans. is ‘a’ i.e., Partial nicotine receptor agonist
Varenicline
- It is partial agonist at the nicotine receptor.
- It is used in nicotine addicts.
| A |
NE & serotonin uptake inhibitor |
|
| B |
Antimuscarinic action on heart |
|
| C |
Only NE uptake inhibition |
|
| D |
Both NE uptake inhibition and antimuscarinic action on heart |
- The commonest cardiovascular effect of tricyclic antidepressant overdose is sinus tachycardia, which is attributable
- to the inhibition of norepincphrine reuptake and the anticholinergic action.
- However, the most important toxic effect of tricyclics is the slowing of depolarisation of the cardiac action potential by inhibition of the sodium current and this delays propagation of depolarisation through both myocardium and conducting tissue.
- This results in prolongation of the QRS complex and the PR/QT intervals with a predisposition to cardiac arrhythmias.
- This inhibition of sodium flux into myocardial cells can occur to such an extent that depressed contractility can result and this, coupled with the reduction in peripheral resistance, contributes to hypotension.
Muscarinic cholinergic receptors are seen at allsites, except ‑
| A | Stomach | |
| B |
CNS |
|
| C |
Neuromuscular junctio |
|
| D |
Glands |
Ans. is ‘c’ i.e., Neuromuscular junction
Cholinergic receptors
- There are two types of cholinergic receptors :
- Muscarinic → Found at – All postaganglionic parasympathetic sites, Few postaganglionic sympathetic sites (sweat gland & blood vessels), CNS.
- Nicotinic —4 Found at – Ganglia (both sympathetic and parasympathetic), Skeletal muscles, Adrenal medulla, CNS
|
|
Muscarinic receptors |
|
Nicotinic receptors |
|
Type |
Organ |
Type |
Organ |
|
M1 |
Gastric gland |
NM |
Neuromuscualr junction |
|
M2 |
Heart |
|
(Skeletal muscle) |
|
M3 |
Smooth muscles, glands and endothelium |
NN |
Ganglia, adrenal medulla |
|
M4 |
CNS |
|
|
|
M5 |
CNS |
|
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