06 - Autonomic, 07 - Cholinoreceptor-activating and cholinesterase inhibiting drugs

Question 1

Spinal roots of origin SANS

Answer 1

Thoracic T1-12
Lumbar L1-5
segments of SC

Question 2

Spinal roots of origin PANS

Answer 2

CN III, VII, IX, and X

sacral segments of spinal cord

Question 3

Location of ganglia SANS

Answer 3

paravertebral chains that lie along the spinal column, some along the anterior aspect of the abdominal aorta

Question 4

Location of ganglia PANS

Answer 4

most are located in the organs innervated, more distant from the spinal cord

Question 5

Preganglionic fibers SANS

Answer 5

short

Question 6

Preganglionic fibers PANS

Answer 6

long

Question 7

postganglioni fibers SANS

Answer 7

long

Question 8

postganglioni fibers PANS

Answer 8

short

Question 9

Pupils sympathetic effect/receptor

parasympathetic effect/receptor

Answer 9

mydriasis a1

miosis m3

Question 10

Heart rate sympathetic effect/receptor

parasympathetic effect/receptor

Answer 10

tachycardia B1

bradycardia M2

Question 11

Heart contractility sympathetic effect/receptor

parasympathetic effect/receptor

Answer 11

increased b1

decreased m1

Question 12

Blood vessels skin, splanchnic sympathetic effect/receptor

parasympathetic effect/receptor

Answer 12

constriction a1

no effect

Question 13

Blood vessels skeletal sympathetic effect/receptor

parasympathetic effect/receptor

Answer 13

dilation b2, m3

no effect

Question 14

bronchi sympathetic effect/receptor

parasympathetic effect/receptor

Answer 14

dilation b2

constriction m3

Question 15

GIT walls sympathetic effect/receptor

parasympathetic effect/receptor

Answer 15

relaxation a2, b2

contraction m3

Question 16

GIT spincters sympathetic effect/receptor

parasympathetic effect/receptor

Answer 16

contraction a1

relaxation m3

Question 17

GIT secretion sympathetic effect/receptor

parasympathetic effect/receptor

Answer 17

no effect

increased m1, m3

Question 18

bladder wall sympathetic effect/receptor

parasympathetic effect/receptor

Answer 18

relaxation b2

contraction m3

Question 19

bladder sphincter sympathetic effect/receptor

parasympathetic effect/receptor

Answer 19

contraction a1

relaxation m3

Question 20

uterus sympathetic effect/receptor

parasympathetic effect/receptor

Answer 20

contraction a1, relaxation b2

contraction m3

Question 21

penis sympathetic effect/receptor

parasympathetic effect/receptor

Answer 21

ejaculation a

erection m

Question 22

sweat glands sympathetic effect/receptor

parasympathetic effect/receptor

Answer 22

increased sweating a

no effect

Question 23

liver sympathetic effect/receptor

parasympathetic effect/receptor

Answer 23

gluconeogenesis, glycogenolysis a,b2

no effect

Question 24

fat cells sympathetic effect/receptor

parasympathetic effect/receptor

Answer 24

lipolysis b3

no effect

Question 25

kidney sympathetic effect/receptor | parasympathetic effect/receptor

Answer 25

increased renin b1 | no effect

Question 26

PLASMA mnemonic

Answer 26

``` for parasympathetic nervous system P-NS L-ong preganglionic fibers A-cetylcholine S-hort postganglionic fibers A-cetylcholine ```

Question 27

Point and shoot mnemonic

Answer 27

point (erection) = PNS | shoot (ejaculation) = SNS

Question 28

primary transmitter in all autonomic ganglia and at the synapses between parasympathetic postganglionic neurons and their effector cells primary transmitter at the somatic (voluntary) skeletal muscle neuromuscular junction

Answer 28

acetylcholine

Question 29

ACh is synthesized from acetyl CoA and choline by

Answer 29

ChAT | choline acetyltransferase

Question 30

choline transport is inhibited by

Answer 30

hemicholinium

Question 31

ACh is actively transported into vesicles for storage by

Answer 31

VAT | vesicle associated transporter

Question 32

VAT is inhibited by

Answer 32

vesamicol

Question 33

entry of calcium triggers interaction among

Answer 33

SNARE proteins | VAMPs and SNAPs

Question 34

toxin that alters synaptobrevins to prevent release of ACh

Answer 34

botulinum

Question 35

degradation of ACh into choline and acetate by

Answer 35

acetylcholinesterase

Question 36

degradation of ACh is inhibited by

Answer 36

inderect actin cholinomimetics | neostigmine, carbamates, and organophosphates

Question 37

Cholinomimetic drug types

Answer 37

direct acting - muscarinic (choline esters, alkaloids) - nicotinic indirect - edrophonium (short acting) - carbamates (intermediate to long) - organophosphates (very long)

Question 38

``` BETANECHOL class similar drug MOA uses SE ```

Answer 38

- cholinomimetic (direct-acting, muscarinic) - carbachol (act on both M and N receptors) - activates muscarinic M1-M3 receptors (act on M receptors only) - bladder and bowel atony (post-surgery or spinal cord injury) - cyclospasm, diarrhea, urinary urgency, vasodilation, reflex tachycardia, sweating

Question 39

``` PILOCARPINE class similar drug MOA uses SE ```

Answer 39

- cholinomimetic (direct-acting, muscarinic) - cevimeline (m3 selective) - activates muscarinic M3 receptors in ciliary muscle (increasing aqueous humor outflow) and salivary glands (increasing salivation) - glaucoma, sjorgren syndrome, sicca syndrome - miosis, blurring of vision (due to cyclospasm)

Question 40

Sjogren syndrome triad

Answer 40

xerostomia (dry mouth) xerophthalmia (dry eyes) RA

Question 41

``` NICOTINE class similar drug MOA uses SE ```

Answer 41

- cholinomimetic (direct-acting, nicotinic) - varenicline - activates nicotinic Ach receptors (Nn and Nm) - smoking cessation - generalized ganglionic stimulation (hypertension, tachycardia, nausea, vomiting, diarrhea) overdose leads to convulsions, paralysis, and coma

Question 42

Muscarinic toxicity CNS stimulation or depression?

Answer 42

stimulation

Question 43

Muscarinic toxicity eye

Answer 43

miosis, spasm of accomodation

Question 44

Muscarinic toxicity lungs

Answer 44

bronchoconstriction

Question 45

Muscarinic toxicity GIT/GUT

Answer 45

excessive GI and genitourinary smooth muscle activity

Question 46

Muscarinic toxicity increased secretory activity in

Answer 46

sweat glands airway GI tract lacrimal glands

Question 47

Muscarinic toxicity blood vessels

Answer 47

vasodilation

Question 48

Nicotinic toxicity ganglionic stimulation or depression?

Answer 48

stimulation

Question 49

Nicotinic toxicity blockade of

Answer 49

neuromuscular end plate depolarization leading to fasciculations and paralysis

Question 50

Nicotinic toxicity CNS stimulation or depression?

Answer 50

CNS stimulations (convulsions) followed by CNS depression

Question 51

MOA of indirect-acting cholinomimetics

Answer 51

- bind to cholinesterase and undergo prompt hydrolysis - alcohol portion released, acidic portion retained and released slowly - -- prevents binding and hydrolysis of endogenous ach - -- amplify ach effects wherever ach is released - no significant actions at uninnervated sites where ach is not normally released

Question 52

``` EDROPHONIUM class similar drug MOA uses SE ```

Answer 52

- cholinomimetic (indirect) [alcohol] - none - inhibits acetylcholinesterase, amplifies endogenously released ach - myasthenia gravis (tensilon test) - miosis, salivation, nausea, vomiting, diarrhea very short acting upon IV administration

Question 53

EDROPHONIUM | tensilon test

Answer 53

for differentiation of cholinergic crisis and myasthenic crisis improves muscle strength in myasthenic crisis weakens muscle strength in cholinergic crisis

Question 54

``` NEOSTIGMINE class similar drug MOA uses SE ```

Answer 54

- cholinomimetic (indirect) - pyridostigmine, physostigmine, ambenonium, demecarium (carbamates), echothiophate (organophosphate) - inhibits acetylcholinesterase, amplifies endogenously released ach - myasthenia gravis treatment, reversal of nondepolarizing neuromuscular blockade, glaucoma (physostigmine, echothiophate, demecarium) - miosis, salivation, nausea, vomiting, diarrhea, bradycardia

Question 55

NEOSTIGMINE | muscarinic effects are blocked by

Answer 55

atropine

Question 56

Other organophosphates: | insecticides

Answer 56

malathion | parathion

Question 57

Other organophosphates: | nerve gases

Answer 57

sarin tabun soman

Question 58

myasthenia gravis

Answer 58

``` autoimmune destruction of nicotinic ach receptors characterized by: - fluctuating muscle - weakness - ocular symptoms - bulbar symptoms - proximal muscle weakness ```

Question 59

differentiate myasthenic crisis from cholinergic crisis

Answer 59

myaesthenic crisis - acute worsening of symptoms due to infection, stress, or undermedication cholinergic crisis - excessive activation of cholinoreceptors (skeletal muscle weakness and parasymapthetic signs) due to overmedication

Question 60

``` RIVASTIGMINE class similar drug MOA uses SE ```

Answer 60

- cholinomimetic (indirect) - galantamine, donepezil, tacrine - inhibits acetylcholinesterase, amplifies endogenously released acetylcholine - alzheimer's disease - miosis, salivation, nausea, vomiting, diarrhea, bradycardia

Question 61

organophosphate poisoning signs and symptoms

Answer 61

DUMBBELSS ``` diarrhea urination miosis bronchospasm bradycardia excitation (skeletal muscle and CNS) lacrimation sweating salivation ```

Question 62

treatment of organophosphate poisoning

Answer 62

atropine | pralidoxime

Question 63

``` ATROPINE class similar drug MOA uses SE ```

Answer 63

- cholinergic antagonist (muscarinic) - blah - competitively blocks all muscarinic receptors - mydriatic, cyclopegic, antidote for organophosphate poisoning (first choice), bradycardia, hypersalivation, decrease airway secretion during general anesthesia - tachycardia, mydriasis, cyclopegia, skin flushing, delirium, hallucinations, urinary retention, constipation no effect on nicotinic signs of toxicity; notorious for causing hyperthermia

Question 64

``` PRALIDOXIME class similar drug MOA uses SE ```

Answer 64

- cholinesterase regenerator, antidote - blah - binds phosphorus of organophosphate, breaks organophosphate bond with cholinesterase - antidote for organophosphate poisoning and nerve gas poisoning (sarin, tabun) - muscle weakness - must be administered before 6-8 hours of organophosphate bond with cholinesterase occurs

Question 65

Cholinoreceptor blocker types

Answer 65

anticholinergic drugs - antimuscarinic - --M1-selective (pirenzepine) - --non-selective (atropine) - antinicotinic - --ganglion blockers (hexamethonium) - --neuromuscular blockers (tubocurarine) cholinesterase regenerators - oximes (pralidoxime)