2. ANS drugs

Question 1

Choline enters from ECF by sodium-dependent membrane carrier( blocked by

Answer 1

hemicholinium

Question 2

Acetylcholine(Ach) is transported from cytoplasm to storage vesicles by antiporter(to be blocked by

Answer 2

vesamicol

Question 3

ACh release can be blocked by

Answer 3

botulinum toxin

Question 4

Dopamine is transported into vesicle by high-affinity carrier mechanism(inhibited by

Answer 4

reserpine

Question 5

Release of norepinephrine can be blocked by

Answer 5

guanethidine and bretylium

Question 6

Reuptake 1of NE is the most important mechanism for termination which can be blocked by

Answer 6

cocaine and tricyclic antidepressants

Question 7

Cholinomimetic drugs divided into

Answer 7

Divided into: cholinoceptor-activating(direct) and cholinesterase inhibiting drugs(indirect)

Question 8

Direct-acting drugs can be divided on the basis of chemical structure into:

Answer 8

Esters of choline, and
Alkaloids

Question 9

Esters of choline:

Answer 9

acetylcholine, methacholine, carbachol, bethanechol

Question 10

ACh has virtually no therapeutic applications because it

Answer 10

is hydrolyzed rapidly by AChE and pseudocholinesterases and diffuseness of its actions

Question 11

Alkaloids:

Answer 11

muscarine, pilocarpine, nicotine, and lobeline

Question 12

Esters of choline are
hydrophillic or hydrophobic

Answer 12

hydrophillic so not absorbed rapidly

Question 13

Tertiary alkaloids are well absorbed from most sites of administration except

Answer 13

muscarine

Question 14

ACh released from activation of parasympathetic NS can activate:

Answer 14

1) muscarinic receptors on effector organs,

2) interact with muscarinic receptors on nerve terminals to inhibit release of NTs

3) ACh can also activate nicotinic receptors

Question 15

organ system effects og cholinomimetics

Answer 15

eye - miosis/ contaction which facilitate flow of aqueous humour

CVS- decrease in heart rate direct effect
increase reflex effect
decrease peripheral resistance

respa- broncho constriction

GIT - increased motility

GUT - increase voiding

Question 16

Indirect-acting cholinomimetics types

Answer 16

1) Simple alcohols bearing quaternary ammonium group e.g. edrophonium
2) Carbamic acid esters of alcohols bearing
tertiary or quaternary ammonium groups e.g. physostigmine, neostigmine, pyridostigmine, ambenonium…)
3) Organic derivatives of phosphoric acid (organophosphates) e.g. isoflurophate, echothiophate,malathion, parathion,sarin,tabun…)

Question 17

based on absorption best to worst

Answer 17

physostigmine well absorbed
organophosphates except echthiophate well absorbed
Quaternary amines poorly absorbed

Question 18

Binding to the active site of the enzyme is

Answer 18

reversible for edrophonium and carbamic acid esters of alcohols bearing tertiary or Quaternary ammonium compounds(reversible AChE inhibitors)

irreversible for organophosphates

Question 19

The process termed as aging

Answer 19

(breaking of one of oxygen-phosphorus bonds of the inhibitor) further strengthens the phosphorus-enzyme bond

Question 20

antidote for aging or organophosphate poisoning

Answer 20

oxime regenerators or cholinesterase regenerators
split enzyme phosphate bond before aging

Question 21

duration of action shortest to longest

Answer 21

edrophonium short
organophospahte long

Question 22

clinical use
eye
git
gut
skeletal
anti muscarnic drug intoxication
CNS

Answer 22

treatment of glaucoma open angle

post op ileus congenital megacolon
bethanecol

urine retention
bethanechol and neostigmine

myastenia gravis- edrophonium for diagnosis
-carvamic acid estres for treatment

physostigmine

alzheimers

Question 23

Cholinoceptor antagonists are divided into:

Answer 23

muscarinic, and
nicotinic antagonists

Question 24

muscarnic antagonists divided into

Answer 24

teritiary ammonium and quaternary ammonium cpds

Question 25

tertiary amines include

Answer 25

atropine, scopolamine, dicyclomine, pirenzepine, benztropine,

Question 26

Quaternary ammonium agents:

Answer 26

propantheline, glycopyrrolate, ipratropium, tiotropium….

Question 27

Tertiary amines or quats well absorbed from the GIT and conjuctival membranes

Answer 27

teritiary

Question 28

Mechanism of action of anti muscarnics

Answer 28

atropine causes reversible blockade of the actions of ACh at muscarinic receptors

They compete for the common binding site

Atropine does not distinguish between sub types of muscarinic receptors

Question 29

…………..exhibit relative selectivity

Answer 29

pirenzepine for M1

Question 30

organ system effects
eye
cvs
respa
git
gut
sweat glands
CNS

Answer 30

eye mydriasis and cycloplegia

cvs tachycardia and block vasodilation

respa bronco dilation

git reduced motilty and secretion

gut relaxed detrusor

sweat glands no sweat atropine fever

cns sedative effect

Question 31

clinical use
cns
eye
git
cvs
respa
gut

Answer 31

cns
parkinsons -benz and trihex
motion sickness- scopolamine

eye
measuring refractive error - tropicamide

git
treat pud and diarrhea

cvs
treat bradycardia

respa
treat asthma - ipratropine and tiotro

Gut
treat urinary urgency

Question 32

Nicotinic rec. antagonists are divided into:

Answer 32

Ganglion blockers
Neuromuscular blockers

Question 33

Ganglion blockers include

Answer 33

hexamethonium, mecamylamine, trimethaphan

Question 34

organ system effects
cns
cvs
eye
git
gut
sweat gland

Answer 34

cns
mecamylamine cross bbb and cause sedation

cvs
tachycardia
reduce bp

eye
mydryasis and cycloplegia

git
reduced motility

gut
urine retention
impaired sex function

sweat gland
ihibited

Question 35

therapeutic use of gang. blockers

Answer 35

limited
used for short term bp lowering

Question 36

2 types of NM blockers

Answer 36

depolarizing and non depolarizing

Question 37

non depolarizing based on time effective

Answer 37

long term
tubucurarine
pancuronium
dexacurium

intermediate
vecucorium
atracorium

short
mivacorium

Question 38

depolarizing blockers

Answer 38

succinylcholine
decamethonium

Question 39

3 types of sympatomimetic drugs

Answer 39

direct
indirect
mixed

Question 40

direct sympatomimetics

Answer 40

epinephrine,
norepinephrine,
phenylephrine.
Isoproterenol,
salbutamol,
clonidine,.

Question 41

indirect symp mimetics

Answer 41

amphetamine
tyramine

Question 42

Mixed-acting

Answer 42

ephedrine

Question 43

based on selectivity
alpha 1 selective

Answer 43

phenylephrine,methoxamine

Question 44

Alpha2 selective: ..

Answer 44

clonidine, methylnorepinephrine

Question 45

Beta1 selective:

Answer 45

dobutamine

Question 46

Beta2 selective:

Answer 46

albuterol(salbutamol), terbutaline, salmeterol..

Question 47

organ system effect
cvs
eye
respa
git
gut
exocrine glands
metabolism
cns

Answer 47

cvs
tachycardia
increase bp
alpha 1 and 2 vasoconstrict
b2 vasodilate

eye
mydriasis

respa
bronchodilate

git
decrease motility

gut
yterus alpha and beta 1 relax’bladder and sphinicter retention

Question 48

Adrenoceptor blocking drugs divided into

Answer 48

Alpha rec antagonists- block alpha
Beta rec. antagonists-block beta

Question 49

Alpha rec antagonists divided into
based on selectivity

Answer 49

Alpha1 selective blockers: prazosin, doxazosin, terazosin, tamsulosin

Alpha2 selective blockers: yohimbine

non selective
phentolamine, phenoxybenzamine

Question 50

Alpha1 antagonists are given

Answer 50

orally
Prazosin is the prototype
Doxazosin and terazosin are congeners of prazosin
have higher bioavailability and longer half-lives

Question 51

Beta receptor antagonists divided based on selectivity

Answer 51

Non-selective antagonists: propranolol, nadolol, pindolol, timolol, sotalol,labetalol,etc

Beta1 selective antagonists: metoprolol(prototype), acebutolol, atenolol, betaxolol, bisoprolol, celiprolol,esmolol
ABEAM

partial agonists activity: acebutolol, celiprolol, pindolol,etc

Question 52

all beta blockers are reversible or irreversible

Answer 52

reversible