Pharm 5 - Antimuscarinics

Front 1

name some therapeutic uses of antimuscarinics in the CV system

Back 1

treats bradycardia, heart block (b/c atria and ventricles)

Front 2

name some therapeutic uses of antimuscarinics in the eye

Back 2

opthalmic examinations to dilate the eye

Front 3

name some therapeutic uses of antimuscarinics in the respiratory tract

Back 3

to treat asthma/COPD (causes the bronchila SM to relax and reduces secretions)

Front 4

name some therapeutic uses of antimuscarinics in the GI tract

Back 4

reduces motility and secretions

Front 5

name some therapeutic uses of antimuscarinics in the urinary tracts

Back 5

treats urinary urgency, incontinence, enuresis, renal colic

Front 6

name some therapeutic uses of antimuscarinics in the CNS

Back 6

treats parkinson disease, motion sickness, antipsychotic therapy

Front 7

name some therapeutic uses of antimuscarinics in cholinergic poisoning

Back 7

treats oranophosphate and muschroom poisoning

Front 8

describe the MoA of antimuscarinics

Back 8

competitive antagonists at muscarinic receptors

Front 9

most antimuscarinics have litler or no effect at nicotinic receptors, except for?

Back 9

propantheline

Front 10

the response of antimuscarinics largely depends on blocking existing ______________ tone.

Back 10

parasympathetic tone

Front 11

what are the 3 categories of antimuscarinics?

Back 11

natural occurring alkaloids
synthetic quaternary amines
synthetic tertiary amines

Front 12

naturally occurring alkaloids are 1._________ derivatives.
2. Name 3
3. can they pass the BBB?

Back 12

1. tropic acid dervatives
2. atropine, scopolamine (w/O group), homatropine (w/HOCH2 group)
3. yes b/c they are tertiary amines

Front 13

name 4 synthetic Quaternary amines (can't cross BBB)

Back 13

propantheline (gut and gall bladder hyperactivity)
glycopyrrolate (decrease gastric acid sec)
ipratropium (COPD)
tiotropium (COPD)

Front 14

name 4 synthetic tertiary amines (can cross BBB)

Back 14

pirenzepine (M1 receptor antagonists for peptic ulcers)
dicyclomine (non-sel for IBS)
tropicamide (to cause mydriasis and cycloplegia)
benztropine (for parkinson dz and SE of antiphsychotic drugs)

Front 15

what classes of antimuscarinics are well absorbed from the gut and mucous membranes

Back 15

alkaloids and tertiary amines

Front 16

what antimuscarinic can be absorbed transdermally?

Back 16

scopolamine

Front 17

what antimuscarinic's half-life is biphasic (2 h and 13 h)
with 50% metabolized, 50% excreted

Back 17

atropine

Front 18

order the responses to atropine from most to least sensitive:
1.eye, heart
2.gastric secretions
3. urinary tract, GI tract
4. Salivary, bronchial and sweat gland secretions

Back 18

4,3,1,2

Front 19

explain how you could get a paradoxycal response?

Back 19

b/c some receptors have intrinic activity in abosence of agonsit antagonist can have "inverse agonist' effects

**main reason is antagoist can also block presynapic receptors that regulat NT release (the feedback mech) so if you inhibit the feedback mech you keep on making the agonist NT

Front 20

1. main antimuscarinic drug for CV system
2. MoA
3. theraputic uses
4. effects
5. RoA
6. SE

Back 20

1. ATROPINE
2. bradycardia, heart block
3. increased HR (incr rate of SA node firing), increase AV node conduction
4. ROA intravenous
5. blurred vision, xerostomia, urinary rentenion, constipation delirium

Front 21

1. main antimuscarinic drug to causes mydriasis and cycloplegia?
2. MOA
3. therapeutic use
4. ROA
5. pharmacokinetics
6. SE
7. related drugs

Back 21

1. ATROPINE
2. non-selective muscarinic receptor antagonist
3. retinal examination, prevention of post-surgical synechia (where iris adheres to cornia)
4. topical
5. lasts 7-10d
6. photosensitive, blurred vision
7. scopolamine (3-7d), homatropine (1-3d), tropicamide (6h)

Front 22

1. antimuscarinic for the respiratory tract to prevent brochospasms
2. MOA
3. therapeutic use
4. ROA
5. pharmacokinetics
6. side effects
7. related compounds

Back 22

1. IPRATROPIUM
2. anagonist at all muscarinic receptors
3. asthma, COPD
4. inhalation
5. short durations, administered 4xday
6. xerostomia, cough
7. tiotropium, longer duration of action 1xday

Front 23

what other antimuscarinics are used preoperative to reduce bronchial secretions?

Back 23

glycopyrolate, scopolamine, atropine

Front 24

1. what antimuscarinics are used for IBS and minor diarrhea?
2. MOA
3. effects
4. ROA
5. SE
6. related cmpds

Back 24

1. DICYLOMINE
2. antagonist at M3 receptors
3. reduces contractile and secretory activity of gut
4. oral or parenteral
5. serostomia, dizziness, somnolence (near sleep), blurred vision
6. glycopyrrolate, propantheline, pirenzepine

Front 25

1. antimuscarinic used for incontinence
2.MOA
3. effects
4. ROA
5. SE
6. rel cmpds

Back 25

1. OXYBUTYNIN
2. muscarinic receptor antagonist, some selectivity for M3 receptors
3. recuces detrusor muscle tone/spasms
4. oral, IV, topical
5. tacycardia, sonstipation, increased intraocular pressure, serostomia, puritis (w/patch)
6. propantheline

Front 26

1. Antimuscarinic used for motion sickness and postoperative nausea
2. MOA
3. ROA
4. SE

Back 26

1. SCOPOLAMINE
2. non-sel muscarinic receptor antagonist
3. oral or transdermal patch, IM injection
4. sedation, tachycardia, blurred vision, serostomia, delirum

Front 27

what is an antimuscarinic used to treat extrapyramidal symptoms assoicated with Parkinson's dz and antipsychotic drug SE?

Back 27

benztropine

Front 28

1. antimuscarinic used for cholinergic (organophosphate) poisoning
2. MOA
3. effects
4. ROA
5. SE
6. used in conjuction with?
7. _________ used prophylactically

Back 28

1. PRALIDOXIME 2-PAM
2. removes irreversible inhibitors from acetylcholinesterase
3. regenerates cholinesterase activity, does not cross BBB, relieves skel muscle end plate blockade
4. intravenous
5. muscle weakness
6. atropine
7.pyridostigmine

Front 29

what are the general adverse effects/toxicity associated more prominently in infants and young children for antimuscarinics?

Back 29

blind as a bat (cycloplegia, mydriasis)
mad as a hatter (delirium, seizures)
dry as a bone (sweat glands, decreased secretion)
hot as a hare (decreased sweating)
red as a beet (reflex vasodilation)
the bowel and bladder lose their tone, the heart runs alone

Front 30

what is the treatment for antimuscarinic toxicity?

Back 30

diazepam, physostigmine help treat the symptoms