Pharm Test 5

Question 1

Cholinergic Action sites

Answer 1

all pregang, para post gang, somatic skeletal, symp sweat glands

Question 2

Cholinergic Antagonists

Answer 2

1) selective muscarinic blockers (most used, still allow symp and NMJ)
2) ganglionic blockers (block all nicotinic receptors- all pre gang)
3) neuromuscular blocker (only effects NMJ)

Question 3

Antimuscarinics

Answer 3

1) atropine
2) scopolamine
3) iptratropium (atrovent)
4) benztropine (cogentin)
5) glycopyrrolate (robinul)

Question 4

Antimuscarinic Adverse Effects

Answer 4

tachycardia, dilation pupil, constipation, urinary retention

Question 5

Atropine Poisoning

Answer 5

hot as a hare (temp)
dry as a bone (low salivation)
blind as a bat (dilation)
red as a beat (flush face)
mad as a hatter (confusion)

Question 6

Ganglionic Blockers

Answer 6

Nicotine

Question 7

Neuromuscular Blocking Non vs Depolarizing

Answer 7

= anesthesia and tracheal intubation
Nondepolarizing- competitive binding, antagonist binds to nicotinic receptor, low doses can be overcome by increase ACh, no CNS
Depolarizing- agonist that binds to receptor and causes depolarization (like ACh), BUT channels stay open and can’t repolarize

Question 8

Neuromuscular Blocking Nondepolarize drugs

Answer 8

1) vercuronium
2) cisatracunum (nimbex)
3) pancuronium (pavulon)
4) rocuronium (zemuron)

reversual= sugammadex (bridion)
cholinesterase inhibitors (adverse effect)
enhances effect of non depolarize drugs- halogenated hydrocarbon anesthetics, ahminoglycosides antibiotic, calcium channel blockers

Question 9

Neuromuscular Blocking Depolarize drugs

Answer 9

1) succinylcholine (anectine) SUX

reversed by psuedocholinesterase in plasma (not NMJ)

Question 10

SUX Adverse Effects

Answer 10

1) malignant hyperthermia - hyper metabolism involving skeletal muscles (SUX)
2) apnea
3) hyperkalemia

Question 11

Adrenergic Receptors

Answer 11

(nor/epi) on symp effector organs

epi released by adrenal medulla 80%

Question 12

Sympathomimetics vs Sympatholytics

Answer 12

sympathomimetic- mimics sympathetic (activate adrenergic receptors)
sympatholytics- block activation of receptors

Question 13

Adrenergic Neurotransmission

Answer 13

1) synthesis- Na w/ tyrosine comes into cell, tyrosine becomes DOPA by tyrosine hydroxylase, and DOPA becomes dopamine (all within the neuron cytosol)
2) storage- dopamine transported into vesicle, dopamine becomes norepinephrine by dopamine b-hydroxylase
3) release- AP comes and Ca influx, release norepi
4) receptor binding- metabotropic (trigger cascade of second messengers)
5) removal- diffuses out of cleft, reuptake into neuron, goes into urine by catechol-O-methyltransferase
6) metabolism- in the neuron norepi is taken into vesicle, stays in cytosol, or oxidized by monoamine oxidase

Question 14

Alpha Affinities

Answer 14

epi >norepi»isoproterenol
alpha1- higher affinity for phenylephrine
alpha2- higher affinity for clonidine

Question 15

Beta Affinities

Answer 15

isoproterenol>epi>norepi
beta1- equal affinity to epi and norepi
beta2- higher affinity to epi than norepi
beta3- lipolysis, bladder muscle

Question 16

Alpha 1

Answer 16

on postsynaptic effector organ
activates G proteins to form second messengers
- DAG turns on intracellular proteins
-IP3 releases Ca from endoplasmic reticulum into cytosol
effects: increase vascular tone/vasoconstriction , bladder sphincter closure increase PVR, mydriasis

Question 17

Alpha 2

Answer 17

on presynaptic nerve endings= neg feedback with inhibitory auto receptors (mediate decrease in cAMP)
effects- decrease norepi/ACh/insulin

Question 18

Beta 1

Answer 18

beta receptors in heart

effects: tachycardia, contractility, renin release from kidney, lipolysis

Question 19

Beta 2

Answer 19

beta receptors in lungs

effects: pulm relax, lung vasodilation, decrease urine contraction, decrease PVR, increase glucose

Question 20

Perfusionists and Adrenergic receptors

Answer 20

alpha1- vasculature
aplha2- CNS feedback, treat HTN
beta1- heart
beta2- lungs

Question 21

Dopaminergic Receptors

Answer 21

D1/D2- mesenteric and renal vascular
D2- on presynaptic adrenergic neurons
effect all adrenergic receptors
main sites of action- brain, cardiovascular beta receptors for HR and contractility and PVR, renal vasodilation

Question 22

Receptor Desensitization

Answer 22

sequestration in cytosol
down regulation
phosphorylation