Pharmacology Test 2 L2 Cholinergic Agonists/cholinesterase Inhibitors

Front 1

Where are muscarinic receptors located? what action?

Back 1

in smooth muscle, these simulate parasympathetic activation

Front 2

What are muscarinic receptors linked to?

Back 2

these are linked to G-proteins

Front 3

What are nicotinic receptors linked to?

Back 3

these are FAST ACTING, and linked to sodium channels

Front 4

Where are nicotinic receptors located?

Back 4

autonomic ganglia N(n) Brain N(n) and Skeletal Muscle N(m)

Front 5

What kinds of receptors does acetylcholine effect?

Back 5

this acts on both Muscarinic AND Nicotinic receptors

Front 6

What will ACh IV infusion do to the body?

Back 6

this will simulate parasympathetic output

Front 7

What types of receptors do Methacholine and Carbachol stimulate?

Back 7

Both Muscarinic and Nicotinic

Front 8

What receptors does Bethanechol (urecholine) stimulate?

Back 8

selective fro Muscarinic receptors ONLY

Front 9

Where does bethanechol usually act on? where does it NOT act?

Back 9

this affects GI and Bladder

DOES NOT ENTER BRAIN (so it leaves brain muscarinic receptors alone)

Front 10

What are Alkaloids? what receptors do they affect?

Back 10

these are Tertiary amines, that are well absorbed into the brain.
Specific for Muscarinic receptors

Front 11

What is Pilocarpine? What does it affect?

Back 11

this is an Alkaloid, affects muscarinic receptors.

affects sweat and salivary glands

Front 12

What is Varenicline?

Back 12

this is an alkaloid that is selective for nicotinic receptors

Front 13

What does muscarinic receptor stimulation do to the iris?

Back 13

this constricts it, causing Miosis

Front 14

What does muscarinic receptor stimulation do to the ciliary muscle?

Back 14

this contracts it, for near vision

Front 15

What does muscarinic receptor stimulation do to the intraocular pressure?

Back 15

this lowers it, but opening the trabecular meshwork, once the ciliary muscle is contracted

Front 16

What does cholinergic stimulation do to the Heart?

Back 16

Affects the Atrium, SLOWING heart rate

Front 17

What does cholinergic stimulation do to the conduction in the heart?

Back 17

this decrease conduction in the AV node

Front 18

What does cholinergic stimulation do to the cardiac tissue?

Back 18

M2 receptors located in heart muscle will decrease NE output

Front 19

What does cholinergic stimulation do to the peripheral blood vessels?

Back 19

Stimulating M3 receptors, causes vasodilation (by NO release)

Front 20

What does MUSCARINIC AGONIST do to the cardiovascular system?

Back 20

VERY LITTLE

Front 21

What are the effects of cholinergic agents, acting on muscarinic receptors in the respiratory system?

Back 21

this will casue Bronchoconstriction, can be very severe in asthmatics

Front 22

What does methacoline do?

Back 22

this is used to diagnose asthma, as a strong cholinergic agent, this acts of muscarinic receptors

Front 23

What are the effects of cholinergic agents, acting on muscarinic receptors in the GI system?

Back 23

Increase secretion and peristalsis

Front 24

what does bethanechol do?

Back 24

This has profound GI effects, increasing secretion and motility

Front 25

What are the effects of cholinergic agents, acting on muscarinic receptors in the Gastic glands?

Back 25

this increase secretion

Front 26

What are the effects of cholinergic agents, acting on muscarinic receptors in the salivation?

Back 26

This increases salivation profoundly

Front 27

What does pilocarpine do to salivary glands?

Back 27

this increase salivation- it is a muscarinic agonist

Front 28

What are the effects of cholinergic agents, acting on muscarinic receptors in the GU system?

Back 28

this stimulates urination (stimulates detrusor, relaxes trigone/sphincer)

Front 29

What does bethanechol do the the GU system?

Back 29

this simulates urination

Front 30

What are the effects of cholinergic agents, acting on muscarinic receptors in the Glands?

Back 30

this causes sweating and secretion

Front 31

What drug is used to reduce intraocular pressure? how does it work?

Back 31

Pilocarpine

this is a muscarinic agonist- causes constriction of the cillary muscles, opening up the canal of schlem

Front 32

What drug is used to stimulate peristalsis?

Back 32

Bethanechol, a muscarinic agonist

Front 33

What drug is used to simulate urinary voiding?

Back 33

Bethanechol

Front 34

What drug is used to treat dry mouth?

Back 34

Pilocarpine

Front 35

What does cevimeline do? what is it like?

Back 35

this is like pilocarpine ( a muscarinic agonist)

but it it selective for M3 ONLY- so it increases salivation, without increasing sweating

Front 36

What are some of the major side effects of muscarinic agonists?

Back 36

Diarrhea
Abdominal Cramps
Salivation/Sweating
Asthma
Tight Bladder

Front 37

What is the major contraindication of taking Muscarinic agonists?

Back 37

peptic ulcer

Front 38

Where are nicotinic receptors located?

Back 38

Autonomic ganglia, brain, skeletal muscle

Front 39

What kind of receptors are nicotinic receptors?

Back 39

these are ligand gated ion channels for Na+ and Ca+

Produce DEPOLARIZATION

Front 40

What happens to nicotinic receptors with constant stimulation?

Back 40

they desensitize very rapidly

Front 41

What do low doses of nicotine do in the brain?

Back 41

this leads to alertness and attention

Front 42

what do high doses of nicotine cause?

Back 42

vomiting, tremor, convulsions

Front 43

how does nicotine become addictive?

Back 43

this causes dopamine release from the nucleus accumbens and prefrontal cortex

Front 44

What are the cardiac effects of nicotine?

Back 44

ths will increase BP and HR, but may have spells of vagal bradycardia

Front 45

What are the GI/GU effects of nicotine?

Back 45

this causes parasympathetic effects- Vomiting, Nausea, Diarrhea, and urination

Front 46

What does nicotine do to the NMJ?

Back 46

this causes Initial stimulation of skeletal muscle

Front 47

what can too much nicotine do to the NMJ?

Back 47

this can cause flaccid paralysis- by desensitization of the nicotinic receptors

Front 48

What are the side effects of nicotine toxicity?

Back 48

Vomiting
Convulsions (from CNS stimulation)
Paralysis (from NMJ desenitization)
and HTN/ arrhythmias

Front 49

What treats nicotine poisoning?

Back 49

Atropine (blocks the muscarinic receptors)
Anticonvulsants (prevents CNS siezure)
Artificial respiration

Front 50

What does Chantix (varenicline) do?

Back 50

this is partial agonists against nicotinic A4B2 receptors

it substitutes for nicotine (in CNS im assuming)- Also as it is a partial agonist, it blocks nicotine effects

Front 51

What are the Side effects of Chantix?

Back 51

this has CNS side effects- like sleep disturbance, vivid nightmares, psychosis, mania, anxiety, and suicidal ideation

Front 52

What type of drugs are Neostigmine and Physostigimne?

Back 52

these are carbamates (reversible cholinesterase inhibitors)

Front 53

What do cholinesterase inhibitors do?

Back 53

these inhibit the breakdown of ACh- keeping it in the synaptic cleft

Front 54

What are cholinesterase inhibitors good for?

Back 54

these are good for diseases in which cholinergic inputs have decreased

Front 55

What do carbamates do?

Back 55

These bind to cholinesterase (but are stable)- and reversible!

(these are neostigmine and physostigmine)

Front 56

Describe Neostigmine

Back 56

this is a quaternary amine- cannot cross BBB (this is a carbamate)

medium duration 30min-6 hours

Front 57

Describe Physostigmine

Back 57

This is a teritary amine, easily orally absorbed. causes bad side effects.
30min-6 hour duration

can be used to treat glacoma

Front 58

What is edrophonium? how is it given?

Back 58

this is a INJECTED quaternary ammonium alcohol. Reversible binds cholinesterase for 5-10 min

Front 59

When must 2-PAM be added?

Back 59

before the aging of an organopthosephate occurs.

Front 60

What do anticholinesterase drugs do in the brain?

Back 60

in low doses, increase memory via M1/Nn

high doses- desnsitization of Nn and convulsions/ respiratory arrest

Front 61

What do anticholinesterase drugs do in the eye, respiratory tract, GI, and GU?

Back 61

these enhance the parasympathetic nature of these organs.

so simulates muscarinic agents

Front 62

What do anticholinesterase drugs do in the the Cardio vascular syste?

Back 62

this increases parasympathetic responses mostly

Front 63

What do anticholinesterase drugs do in the NMJ

Back 63

LOW concentrations increase strength of NMJ firing

High- toxic/ NMJ blockade

Front 64

What does Neostigmine do? What disease does it treat?

Back 64

This is a quaternary amine, does not penetrate BBB.
Treats myasthenia gravis

Direct stimulation effect on NMJ

Front 65

What does Edrophonium do? used for?

Back 65

this is a anticholinesterase drug, used to diagnose myastenia gravis

Front 66

What does Physostigmine do?

Back 66

this goes directly in the eye to treat glaucoma

Front 67

What do Donepezil and rivastimine do? what parent drug are they like? What do they treat?

Back 67

these are like physostigmine- (so they are a tertiary amine anticholinesterases)

These treat Alzheimers disease

Front 68

What is Echothiopate?

Back 68

this is an oragnophosphate, used for glaucoma emergencies

Front 69

What type of drugs are DFP, Soman, and Sarin?

Back 69

these are highly lipid solubile organophosphates

Front 70

how are parathion and malation different than other organophosphates?

Back 70

they require enzymes to convert them before they are toxic

Front 71

What drugs treat Myasthenia gravis? (3 of them)

Back 71

neostigmine, pyridostmine, ambenouim

Front 72

How much atropine should you inject into a pt?

Back 72

enough until the pupils dilate