Pharmacology-Lecture 3

Front 1

Atropine
MOA?

Back 1

-Non-selective muscarinic antagonist
-High potency

Front 2

Scopolamine
MOA?

Back 2

-Potent muscarinic antagonist
-High CNS activity

Front 3

Pirenzepine
MOA?

Back 3

Selective for M1 subtype receptors

Front 4

Muscarinic Anagonists
Action on CNS (5)

Back 4

-Hallucinations
-Confusion
-Restlessness
-Irritability
-Psychosis like signs

Front 5

How to prevent muscarinic antagonists from entering the CNS?

Back 5

-Methylate N to get quaternary N

Front 6

Atropine's effect on CNS?
Dose?

Back 6

-Crosses BBB poorly
-Can see CNS effects with high dose

Front 7

Muscarinic Antagonists
Effect on Cardiovascular Heart
(3)

Back 7

-Blocks M2 receptor
-Releases vagal inhibition
-Increase HR

Front 8

Low dose effect of muscarinic agonists on heart?

Back 8

-May block presynaptic M2 receptor
-May see increased Ach release
-Brachycardia

Front 9

Muscarinic Antagonist Effect
Vasculature

Back 9

-Little or no effect
-M3 receptors there but no innervation and no Ach present

Front 10

Muscarinic Antagonist Effect
Eye (3)

Back 10

-Blocks M on circular and ciliary muscles
-Gives impaired accommodation (cycloplegia)
-Impaired mydriasis

Front 11

Muscarinic antagonists contraindicated for which patients? (1)

Back 11

-Patients with closed angle glaucoma
-Will results in loss of drainage from Schlemm and increased pressure
-No anticholinergic medication (including antihistamines)

Front 12

Muscarinic Antagonist Effect
GI tract and bladder (2)

Back 12

-Decreased tone leading to constipation and urinary retention
-Decreased GI secretions

Front 13

Muscarinic Antagonists Effect
Glands (5)

Back 13

-Inhibits secretions
-Decrease lacrimation
-Decrease sweating
-Decrease salivation
-Decrease bronchial secretions

Front 14

Atropine (muscarinic antagonists) Side Effects

Back 14

-Listed in specific body systems
-Plus photosensitivity
-Plus CNS signs

Front 15

Treat Atropine CNS side effects with? (1)

Back 15

-Physostigmine

Front 16

Uses of Muscarinic antagonists
-GI (1)
-Medication used? (1)

Back 16

-Ulcer patients
-Pirenzepine
-Helpful in conjunction with other ulcer medication
-NO atropine --> too many associated side effects

Front 17

Uses of Muscarinic Anatgonists
-Eye (1)
-Side Effects (2)

Back 17

-Eye exams
-Less potent agents
-SEs = photophobia and accommodation issues

Front 18

Uses of Muscarinic Antagonists
-Toxicity (1)

Back 18

-Cholinesterase Poisening
-Atropine blocks muscarinic effects
-Life saving in short term

Front 19

Uses of Muscarinic Antagonists
-Surgery (1)
-Effects (3)

Back 19

-Adjunct in anesthesia
-Decrease bronchial secretions
-Bronchodilation
-Anti-vagal effects

Front 20

Scopolamine
-Uses (1)
-Effects (4)

Back 20

-Anesthetic adjunct
-Drowsiness
-Fatigue
-Amnesia
-Euphoria

Front 21

Scopolamine
-Side effects (2)

Back 21

-Patients in pain can have delirium or intense reaction
-Limits use in this condition

Front 22

Pirenzepine
-MOA?
-Uses (1)

Back 22

-M1 selective
-Ulcers
-Used in conjunction with other medications

Front 23

Muscarinic Anatgonists Uses
-CNS? (2)

Back 23

-Anti-Parkinson Treatments (not primary treatment but provides some relief for tremor)
-Motion sickness

Front 24

Benztropine
-MOA?
-Uses (1)

Back 24

-Blocks muscarinic receptors in basal ganglia
-Useful in idiopathic and drug induced Parkinson states

Front 25

Scopolamine (patch)
-Uses in CNS?
-Side effects? (2)

Back 25

-Motion Sickness
-Very useful
-Best given prophylactically
-Side effects = Sedation and dry mouth

Front 26

Uses for Muscarinic Antagonists
-Urinary system (1)

Back 26

-Overactive bladder
-Symptoms of urgency and urinary frequency
-Incontinence
-Somewhat effective
-Use mild anti-cholinergic and cheap

Front 27

Uses for Muscarinic Antagonists
-Respiratory System (2)

Back 27

-Asthma patients
-COPD
-Produces bronchodilation

Front 28

Side effect of long-term atropine use in respiratory system?

Back 28

-Effects mucociliary clearance
-Not first line of treatment but can be used adjunctively

Front 29

Ipratropium
-Uses?
-MOA?
-Administration?

Back 29

-Muscarinic antagonist
-Used to produce bronchodilation
-Does NOT affect mucociliary clearance
-Oral, QID (4 times/day)

Front 30

Tiotropium
-Uses?
-Adminstration?
-Problem?

Back 30

-Produce bronchodilation
-COPD and asthma patients
-Inhalant
-Long duration (24 hours)
-Problem--4 times/day administration

Front 31

Summary of Muscarinic Antagonist uses (8)

Back 31

-Ulcer
-Eye exams
-Cholinesterase Poisoning
-Adjunct in Anesthesia
-Anti-Parkinson Treatments
-Motion sickness
-Overactive Bladder
-Asthma/COPD --> bronchodilation