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Questions and Answers
Which of the following is a characteristic of M2 receptors in the CNS?
Which of the following is a characteristic of M2 receptors in the CNS?
- Neutral
- Excitatory
- Inhibitory (correct)
- Stimulatory
What is the effect of M3 receptors on the smooth muscles?
What is the effect of M3 receptors on the smooth muscles?
- Hyperpolarization
- Relaxation
- Contraction (correct)
- No effect
Which of the following is a cholinomimetic that acts directly on cholinergic receptors?
Which of the following is a cholinomimetic that acts directly on cholinergic receptors?
- Cevemiline
- Bethanechol (correct)
- Neostigmine
- Pilocarpine
What is the effect of M3 receptors on the eye?
What is the effect of M3 receptors on the eye?
Which of the following is a classification of cholinomimetics?
Which of the following is a classification of cholinomimetics?
What is the effect of M2 receptors on the heart?
What is the effect of M2 receptors on the heart?
What is the mechanism of action of cholinesterase inhibitors?
What is the mechanism of action of cholinesterase inhibitors?
What is the effect of M3 receptors on exocrine glands?
What is the effect of M3 receptors on exocrine glands?
What is the primary therapeutic use of Pilocarpine?
What is the primary therapeutic use of Pilocarpine?
Which of the following is a therapeutic use of Neostigmine?
Which of the following is a therapeutic use of Neostigmine?
What is the primary mechanism of action of Cholinomimetics?
What is the primary mechanism of action of Cholinomimetics?
What is the primary difference between 3ry Amines and 4ry Amines?
What is the primary difference between 3ry Amines and 4ry Amines?
What is the antidote for competitive NMBs?
What is the antidote for competitive NMBs?
What is the primary adverse effect of cholinomimetics on the CNS?
What is the primary adverse effect of cholinomimetics on the CNS?
What is the characteristic of Neostigmine in terms of its absorption?
What is the characteristic of Neostigmine in terms of its absorption?
What is the primary therapeutic use of Physostigmine?
What is the primary therapeutic use of Physostigmine?
What is the primary difference between Muscarinic and Nicotinic receptors?
What is the primary difference between Muscarinic and Nicotinic receptors?
Which of the following Cholinesterase Inhibitors is used to antagonize central and peripheral effects of atropine?
Which of the following Cholinesterase Inhibitors is used to antagonize central and peripheral effects of atropine?
What is the effect of Cholinesterase Inhibitors on skeletal muscle power?
What is the effect of Cholinesterase Inhibitors on skeletal muscle power?
What is the characteristic of Irreversible Cholinesterase Inhibitors?
What is the characteristic of Irreversible Cholinesterase Inhibitors?
What is the primary effect of Physostigmine on the eye?
What is the primary effect of Physostigmine on the eye?
Which of the following Cholinesterase Inhibitors is an analogue of Neostigmine with a longer duration of action and fewer visceral side effects?
Which of the following Cholinesterase Inhibitors is an analogue of Neostigmine with a longer duration of action and fewer visceral side effects?
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Study Notes
Choline Esterase Inhibitors
- Reversible inhibitors: Edrophonium (ultra-short acting), Neostigmine (intermediate acting), and Pyridostigmine (long-acting)
- Irreversible inhibitors: Organophosphates, which are highly lipid soluble and absorbed from all sites of the body, even skin
Mechanism of Action
- Cholinesterase inhibitors bind to the enzyme acetylcholinesterase, preventing the breakdown of acetylcholine
- This leads to an increase in acetylcholine levels, enhancing neurotransmission at cholinergic synapses
Muscarinic Effects
- M2 receptors: inhibitory in CNS, slow heart rate, and decrease contractility
- M3 receptors:
- Smooth muscle contraction
- Bronchospasm
- GIT and urinary bladder contraction
- Eye: miosis, accommodation, and increased aqueous drainage
- Exocrine glands: increased secretion
- Vascular endothelium: NO release, vasodilation, and decreased blood pressure
Classification of Cholinomimetics
- Directly acting: Choline esters, Natural alkaloids
- Indirectly acting: Reversible and irreversible inhibitors
Therapeutic Uses of Cholinomimetics
- 3ry Amines:
- Hair tonic: Pilocarpine
- Alzheimer's disease: Donepezil and Rivastagmine
- Atropine toxicity: Physostigmine
- Dry eye and mouth: Pilocarpine and Cevemiline
- Miotics in glaucoma: Pilocarpine and Physostigmine
- 4ry Amines:
- Post-operative: Neostigmine and Bethanechol
- Megacolon/prokinetic: Bethanechol
- Myasthenia gravis: Pyridostigmine
- Antidote for competitive NMBs: Neostigmine
- Diagnosis of Myasthenia gravis: Edrophonium (ultra-short acting)
Adverse Effects and Contraindications
- CNS: Irritability, convulsions
- Eye: Miosis, lid twitches, brow ache, and frontal headache
- Exocrine: Lacrimation, salivation, and increased HCl secretion
- CVS: Bradycardia, hypotension, cardiac arrest, and infarction
- Respiratory: Bronchospasm and increased secretion
- GI: Urination, diarrhea, colic, nausea, and vomiting
- Muscular: Fasciculations and paralysis in toxic doses
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