Lecture 3.5 Muscarinic Antagonists

Question 1

Antagonists for nicotinic receptors at SOMATIC nervous system are called ____ blockers. Antagoinsts for nicotinic receptors at the PANS/SANS are called ____ blockers

Answer 1

neuromuscular;

ganglionic

Question 2

M1, M3, and M5 receptors are G _ coupled and cause an increase in ____ concentration. M2 and M4 receptors are G __ coupled and cause a reduced amount of ___

Answer 2

q, calcium;

i, cAMP

Question 3

M2 receptors are expressed in ____ smooth muscle. they are coupled to ____ channels at allow ___ outflow to slow ____

Answer 3

cardiac; K+, K+, heart rate

Question 4

Eye effects of antimuscarinics: both are ___ receptor antagonists:

____ (pupil ____) by inhibiting the ____ ____ muscle

____ (loss of focus/regulation of lens thickness) by inhibiting the ____ muscle

Answer 4

M3;

Mydriasis, dilation, pupillary constrictor

cycloplegia, ciliary

Question 5

Antimuscarinics:
bladder ____ via the ___ receptor which mediates contraction of the bladder and the ____ Receptor which indirectly inhibits relaxation

Answer 5

relaxation, M3;

M2

Question 6

____ is an ACh antagonist used to reduce the effects of ____ by its antispasmodic agents and reduced acid secretion

Answer 6

mebeverine;

Irritable Bowel Syndrome

Question 7

muscarinic antagonists:

____ amines are mostly used in the GI tract and peripherally due to their ___ polaritiy

____ amines are used in the CNS and eye. they can cross the ____

Answer 7

quarternary, high;

tertiary, BBB

Question 8

long lasting tertiary amines (2):

which has higher CNS penetration?

Answer 8

atropine, scopalamine;

scopalamine

Question 9

high doses of scopalamine can produce _____. Withrdawl symptoms are due to a ____ effect (aka ____ of the receptors) and include nausea, headache, blurred vision. How can you reduce these symptoms?

Answer 9

hallucinations;
rebound, sensitization

symptoms can be reduced by leaving patch on for longer time

Question 10

Scopalamine is mainly used for ____ ____ as a patch. It can also be used surgery/obstetrics because it causes ____

Answer 10

motion sickness;

amnesia

Question 11

Short acting tertiary amines such as ____ and ____ are used for eye exams. These cause ___ and ____ bv blocking the pupillary constriction muscles and ciliary body

Answer 11

tropicamide, homatropine;

mydriasis, cycloplegia

Question 12

Nerves at the terminal end of the optic nerve are ____ and the first to be damaged by ____. (why we use dilator exams)

Answer 12

thinner, glaucoma

Question 13

types of urinary incontinence:
____ incontinence is due to laxity of the pelvic floor muscle; associated w/ heavy child birth. treat with _____

____ incontinence is due to a large volume intake

Answer 13

stress; adrenergic agonists;

functional

Question 14

Types of urinary incontinence:
Outflow incontinence is due to urinary retention secondary to ____ or bladder ____. Symptoms = nocturia, increased frequency. Treatment for each reason?

Answer 14

obstruction, atony;

treat obstruction with alpha antagonists;
treat atony with cholinergics

Question 15

Types of urinary incontinence:

Urge incontinence is due to ____ detrusor muscle activity. Symptoms = nocturia, increased frequency. Treatment?

Answer 15

increased;

anti-cholinergics

Question 16

Diabetic incontinence mechanisms:

1. overactive bladder -> ____ incontinence early in diabetes
2. cystopathy: decreased sensation, increased capacity –> ____ incontinence later
3. ____ diabetes = increased baby weight = damage pelvic floor

Answer 16

urge;
outflow;
gestational

Question 17

Diabetes incontinence mechanisms:
diabetes can lead to ____ ___ ___ –> retain water, nocturia;
____ is a common GI manifestation –> difficult to empty bladder;
increased risk of ____, leading to increase in urge/frequency

Answer 17

congestive heart failure;
constipation;
UTI

Question 18

muscarinic antagonists suppress involuntary bladder ____ and increase the maximal urine ____ that causes involuntary bladder ____

Answer 18

contraction; volume; contraction

Question 19

Incontinence drugs:

____ and ____ are M3 selective. They are ____ lasting

Answer 19

darifenacin, solifenacin

long

Question 20

Incontinence drugs:

tolterodine is ___ and ____ selective. It has ____ side effects that oxybutinin

Answer 20

M2, M3;

fewer

Question 21

Incontinence drugs:

oxybutynin is ___ and ___ selective. Most widely seen side effect ______

Answer 21

M1, M3;

dry mouth

Question 22

Probanthine is used to treat ____ disorders. It has a charged N that makes crossing the ____ difficult; ie it is peripherally restricted

Answer 22

gastric (ie spasms, NOT GERD);

gut

Question 23

2 drugs (besides atropine) used for IBS:

Avoid in ____ patients and avoid long term use

Answer 23

dicyclomine, hysocyamine;

glaucoma

Question 24

Ipratropium and tiotropium are used to treat ____. Ipra- is ____ acting and is used as a ____ inhaler. Tio- is ____ acting and used as a ____ inhaler

Answer 24

COPD;
short, rescue;
long, daily

Question 25

2 drugs used in treatment of parkinsons?

What receptor do they act on?

Answer 25

benztropine, trihexyphenidyl

M1 receptor

Question 26

Mechanism of action of benztropine: improve balance between ____ and _____ neurotransmission

Answer 26

ACh and dopa

Question 27

Antimuscarinics also block the extra ____ side effects of ______

Answer 27

pyramidal;

antipsychotics

Question 28

Drug classes with anticholinergic activity (4)

Answer 28

anti-psychotics, Tricyclic anti-depressants, anti-arrythmics, anti-histamines