Acetylcholine Receptor Agonist

Question 1

Name the three plant alkaloids

Answer 1

muscarine
nicotine
pilocarpine

Question 2

where is the principal location of M1 receptors ?

Answer 2

Autonomic ganglia
presynaptic nerve terminal
CNS

Question 3

M1Receptor
1. what is its mechanism of signal transduction ?
2. Effects of activated M1 receptor

Answer 3

1. Increased IP3
2. Modulation of neurotransmission

Question 4

M2 Receptor
1. what are the effects of the activation of the M2 receptor ?
2. where is the principal location of M2 receptor ?

Answer 4

1. slowing heart rate and conduction
2. Cardiac tissue and cardiac conducting tissue (SA and AV nodes)

Question 5

Name the two classifications of acetylcholine receptor agonist ?

Answer 5

1. Direct-acting agonist
2. Indirect acting agonist

Question 6

what classification of cholinergic receptor agonist increase the synaptic concentration of acetylcholine by INHIBITING the enzyme cholinesterase

Answer 6

Indirect- Acting -AGONISTS

Question 7

Bethanecol
1. what cholinergic receptor specificity does this drug interact with ?
2. route of adm for Bethanecol ?
3. Is Bethanecol easily hydrolyzed by cholinesterase ?
4. Indication/ clinical use of this drug ?

Answer 7

1. Muscarinic receptors
2. oral and subcutaneous
3. no
4. gastrointestinal and urinary stimulation

Question 8

Give a few examples of direct-acting agonists

Answer 8

choline esters (AcH)
plant alkaloids
synthetic drugs ( cevimeline and varenicline

Question 9

Two direct-acting Cholinergic AGONIST
that act on both mucarinic and nicotinic receptors

Answer 9

1. Acetylcholine
2. Carbachol

Question 10

Synthetic acetylcholine examples (drugs)

Answer 10

Bethanecol and Carbachol

Question 11

Most common principal subtypes of M receptors found in tissues are what types of M receptors ?

Answer 11

M1 M2 and M3

Question 12

Cevimeline
1. directly act on which receptor ?
2. clinical use/ indication for ?
3. adverse effects of Cevimeline ?
4. this drug is to be used cautiously on patients with what conditions ?

Answer 12

1. synthetic direct acting M receptor agonist
2. treats DRY mouth with Sjorgen syndrome
3. increased sweating, nausea, visual disturbances caused by drug induced miosis
4. asthma or cardiac arrhythmias

Question 13

Carbachol
1. is used for (indication of clinical use)

Answer 13

1. instilled ocularly to produce miosis during opthalmic surgery or cataract surgery

Question 14

Pilocarpine
1 . and 2. effects and indication of pilocarpine
3. when used to treat open-angle glaucoma what actions does pilocarpine do ?

Answer 14

1. the effect of pilocarpine has greater affinity for muscarinic receptors than nicotinic receptors.
2. Can produce ALL the effects of muscurinic receptor stimulation
3. lowers intra-ocular pressure by increasing the outflow of aqueous humor

Question 15

effects of bethanechol

Answer 15

selectively activates M receptors
stimulate bladder and GI w/o affecting HR or BP