IC5

Question 1

where are beta 1 receptors found

Answer 1

predominantly in the heart

Question 2

what is the mechanism of beta 1 receptors

Answer 2

NE binds to receptor –> increase camp –> activates protein kinase A –> increase Ca2+ release via L type calcium channelh

Question 3

what are the outcomes of activation of beta 1 receptor

Answer 3

increase contractility, heart rate and conduction velocity

Question 4

what does beta blockers do

Answer 4

reduce heart rate, conduction velocity and contractility

Question 5

where are beta 2 receptors found

Answer 5

bronchus and smooth muscle

Question 6

what is the mechanism of beta 2 receptor

Answer 6

NE binds –> increase in camp –> inhibit MLCK –> reduce phosphorylation of MLC –> reduce contraction of SM –> relaxation of arteriole vessel

bronchodilation

Question 7

what could beta 2 receptors lead to

Answer 7

bronchoconstiction and thus asthma attack for asthmatics

Question 8

what is the general mechanism of alpha 1 receptors

Answer 8

activates IP3 calcium release –> vasoconstriction due to activation of MLCK

Question 9

what is the mechanism for alpha 2 receptor in sm

Answer 9

bind and decrease camp –> decrease inhibition of MLCK –> vasoconstriction

Question 10

what is the moa of alpha 2 in cns

Answer 10

inhibit SNS –> reduce TPR and thus reduce BP

Question 11

what are the alpha agents you use for htn

Answer 11

alpha 1 antagonists
alpha 2 agonists

Question 12

what are some se of beta blockers

Answer 12

cns
bradycardia
hypotension
av nodal block
bronchospasm

Question 13

___ lipophilic the more cns effects

Answer 13

more

Question 14

what is the lead compound for beta 1 receptor blockers

Answer 14

dichloroisoproterenol

Question 15

what are the structures for beta blockers now and how does it come about

Answer 15

aryloxypropanolamine

addition of oxymethylene group (och2)

Question 16

what are the structural requirements of BB

Answer 16

at least 1aromatic carbocycle or heteroaromatic ring system

secondary chiral OH and amine attached to the ring

aryloxypropanolamine structure

Question 17

which BB is not a racemix mixture

Answer 17

timolol

Question 18

the __ stereoisomer is more active and binds to the receptor

Answer 18

s

Question 19

how do you tell which is a selective and which is a non-selective BB apart

Answer 19

selective has the thing in para position while non-selective is in meta/ortho position

note this is only for those that are aryloxypropanolamine

Question 20

more lipophilic BB ___ half life

Answer 20

shorter

Question 21

what is the MOA of alpha 1 receptor blockers

Answer 21

selectively and competitively bind to receptor on SM –> inhibit SNS –> vasodilation of arteries and veins

Question 22

what is the MOA of alpha 2 receptor agonist

Answer 22

inhibits SNS –> reduce TPR and decrease BP

Question 23

what structure is necessary for activity in alpha 2 agonist

Answer 23

not imidazoline ring

phenyl ring with at least 1 O-Cl or Me group

Question 24

what are examples of mixed alpha and beta blockers

Answer 24

labetalol

carvedilol

Question 25

how many chiral carbons does carvedilol have

Answer 25

1

Question 26

is carvedilol a racemix micture

Answer 26

yes

Question 27

what does the s and r isomer of carvedilol do

Answer 27

S : alpha and non-selective beta blocker R : alpha 1 blocker

Question 28

how many chiral carbons does labetalol have

Answer 28

2

Question 29

how does blocking beta 1 and alpha 1 help

Answer 29

b1 : reduces HR and CO a1 : leads to vasodilation via TPR reduction

Question 30

what do diuretics do

Answer 30

increases production of urine and inihits the tubular reabsorption of sodium

Question 31

inhibition of sodium leads to ___

Answer 31

diuresis

Question 32

what are the diuretics and where do they act

Answer 32

CAI - proximal convoluted tubule osmotics - proximal convulted tubule + thin descending limb of loop of henle loop : ascending limb of loop of henle thiazide : distal convoluted tubule K+ sparring : collecting tubule

Question 33

acetazolamide is a

Answer 33

CAI

Question 34

mannitol is a

Answer 34

osmotic

Question 35

frusemide, bumetamide and torsemide is a

Answer 35

loop diuretic

Question 36

side effects of loop diuretics

Answer 36

hypokalemia

Question 37

chlorothiazide, hydrochlorothiazide are

Answer 37

thiazide diuretics

Question 38

metolazone and indapamide are

Answer 38

thiazide like diuretics

Question 39

side effects of thiazide class

Answer 39

hyponatraemia hypokalemia metabolic alkalosis Hypercalcemia Hypomagnesemia hyperglycemia hyperuricemia

Question 40

amiloride and triamterene are

Answer 40

ENac

Question 41

spironolactone and eplerenone are

Answer 41

mra

Question 42

side effect of mra

Answer 42

gynaecomastia

Question 43

what is the parent structure in mra

Answer 43

androstane + spiro-lactone substitutent

Question 44

what is the parent structure in thiazides

Answer 44

thiadiazine

Question 45

what is the parent structure in loop

Answer 45

sulfonamide scaffold

Question 46

what is the parent structure in CAI

Answer 46

thiadiazole

Question 47

what is the parent structure in ENAc

Answer 47

pteridine

Question 48

why is the sulphonamide group acidic

Answer 48

ew effect of O pulls lp of electron on N towards itself --? deficient in electron --> H leaves as H+

Question 49

what makes chlorothiazides more active

Answer 49

lipophilic group at c3 of 3,4-dihydro derivative

Question 50

what is necessary for thiazide activity

Answer 50

ewg at c6

Question 51

chlorthalidone contains a

Answer 51

phthalimidine

Question 52

indapamide contains a

Answer 52

chlorobenzamide and a methylindoline group

Question 53

most of the beta blockers are aryloxypropanolamines except ___ which is a ___

Answer 53

sotalol arylethanolamine