3 - Muscarinic Agonists

Question 1

Diabetic autonomic neuropathy may _______

and affect _____

Answer 1

precede other complications

affect one or more organs

Question 2

Mechanisms of neuropathy

Answer 2

Metabolic nerve damage
neurovascular insufficiency
AI damage
Neurohormonal growth factor deficiency

Question 3

Clinically, the most important form of autonomic neuropathy

Answer 3

Caradiovascuar

Question 4

Common in patients with liver disease

Answer 4

Autonomic (mainly VAGAL) dysfunction

Exaggerated by alcohol abuse

Question 5

Advanced chronic liver disease is characterized by…

Answer 5

Peripheral arterial vasodilation

Increased plasma catecholamine concentrataions

Question 6

Botulism toxin MOA

Answer 6

cleaves SNAP-25 in the SNARE complex

Inhibiting release of Ach in vesicles

Question 7

Hyperthyroidism mimics ___________

Answer 7

hyperadrenergic state

Question 8

Hyperthyroidism heart rate is __ and ___

Answer 8

irregular and fast

Treat with Beta blockers

Question 9

Hyperthyroidism-related tachycardia is a contraindication for ____________

Answer 9

Muscarinic agonists (even though they decrease CO)

Can induce atrial fibrillation

Question 10

Graves disease etiology

Answer 10

AI disease against TSH receptor –> activation

Question 11

Crosstalk between Thyroid and Adrenal

Answer 11

Adrenal gland activation produces GC’s

GCs inhibit enzyme that converts T4 into active T3

Question 12

Effect of reduced body weight

Answer 12

Lower T3 and Sy ANS

Heightened PSy

Question 13

Hyperthyroidism causes _________ of adrenergic receptors

Answer 13

Desensitization

Question 14

Hypothyroidism causes _________ of adrenergic receptors

Answer 14

Sensitization

Question 15

Undiagnosed Hypothyroidism most common in women

Answer 15

iodine deficiency

Question 16

Hashimotos thyroiditis symptoms

Answer 16

Cold, dry skin, hair loss, slowed heart rate

Question 17

Cholinergic stimulation can reduce…

Answer 17

symptoms of neuropathic ANS disorders

Question 18

Effects of cholinergic stimulation

Answer 18

Increase of ureteral peristalsis
BP increase
Increased GI tone
Bronchoconstriction + mucus secretion
Increase glandular activity
Miosis, drainage of anterior chamber

Question 19

Types of drugs that increase cholinergic stimulation

Answer 19

AchEI’s

Muscarinic agents

Question 20

Muscarine was the first _______

Problem/sides?

Answer 20

parasympathomimetic

Can cross BBB and cause convulsions

Question 21

Direct acting Cholinergic recepor agonists are ______

Answer 21

Esters

Question 22

Examples of direct cholinergic agonists

Answer 22

Ach
Bethanechol
Carbachol
Methacholine

Question 23

What causes the polarity of direct receptor agonists?

Due to the polarity of direct agonists, they have…

Answer 23

The quaternary ammonium

limited CNS distribution and GI absorption

Question 24

Carbachol acts on which receptors

Answer 24

mAchR + nAchR

Question 25

Methacholine acts on which receptors

Answer 25

All, but mostly mAchR | "M"uscarinic for "M"ethacholine

Question 26

Risk with nAchR activity

Answer 26

Systemic fatal OD --> nicotinic receptors son diaphragm and IC's (still low risk d/t polarity)

Question 27

Ocular use for muscarinic agents

Answer 27

Treatment for glaucoma | reduces intra-ocular pressure

Question 28

Mechanisms for glaucoma

Answer 28

Overproduction of humor | Drainage canal blockage

Question 29

Which type of glaucoma is the emergency?

Answer 29

Closed angle | canal of schlemm occluded between iris and corneal/scleral layer

Question 30

Endothelial cells with ____ secete aq. humor

Answer 30

B2-AR

Question 31

____ blocks B2AR in the endothelial cells of the eye

Answer 31

Timolol | blocks without miosis or loss of accommodation

Question 32

Muscarinic agonsts for the treatment of glaucoma

Answer 32

Carbachol | Pilocarpine

Question 33

Carbachol is a ____ | PK?

Answer 33

Full agonist, longer acting 2-5 minute onset, can last 24h if intra-ocuar

Question 34

Pilocarpiine is a ____ | MOA?

Answer 34

``` Partial agonist (less headache) relieves Canal of Schlemm blockage ```

Question 35

Sides for pilocarpine

Answer 35

Sweating, salivation, diarrhea, mucus secretion Miosis (blurred vision, impaired night vision) Reduced BBB function (can enter CNS and cause epilepsy at higher doses!)

Question 36

Bethanecatechol use

Answer 36

Urinary retention | Post-op ileus (GI atony)

Question 37

Avoid bethanecatechol use in

Answer 37

bladder outlet obstruction (stones, BPH, tumor)

Question 38

Bethanecatechol MOA

Answer 38

muscarinic selective, doesnt bind to nicotinic resistant to AchE

Question 39

Cevimelie and pilocarpine uses

Answer 39

Xerostomia After head/neck radiation Sjogrens

Question 40

Nicotinic agonists for cessation

Answer 40

Nicotine (full agonist, protonated at acidic pH) | Varenicline (partial agonist of a4B2 nicotonic receptor, blocks nicotine from binding at the same time)

Question 41

Sides for Nicotine

Answer 41

Irritation at site, tachycaridia/arrhythmia, dyspnea

Question 42

Sides for Varenicline

Answer 42

GiT related | Dream stuff

Question 43

Varenicline reduces ________

Answer 43

effects of withdrawal