Medchem Test 1 Insulin

Front 1

how many AA make up insulin, proinsulin, and preproinsulin

Back 1

insulin - 51 (21 alpha 30 beta)
proinsulin - 86
preproinsulin - 109

Front 2

where does zinc bind to insulin and what does it do

Back 2

zinc complexes with insulin at the 10th amino acid of the beta chain for stabilization

Front 3

doing what decreases the activity of the alpha chain

Back 3

deleting GLY

Front 4

doing what eliminates activity of insulin

Back 4

cleavage of the S-S link between the alpha and beta chain

Front 5

doing what will decrease the activity of the entire insulin molecule

Back 5

removing AA at both C terminal ends

Front 6

removing of what AA has no effect on beef/pork insulin activity

Back 6

removal of ALA from the C terminal of the beta chain

Front 7

removing what AA on the beta chain has no effect on activity

Back 7

PHE or VAL on the N terminal end of the beta chain

Front 8

what are the rapid acting insulin and what are their effects

Back 8

lisipro
aspart
glulisine

faster onset of action, shorter duration, and less absorption variation

Front 9

how is lispro made

Back 9

transpose B28 w/ B29

Front 10

how is Aspart made

Back 10

transpose B28 w/ Asp

Front 11

how is Glulisine made

Back 11

transpose B3(Val) w/ Lys and B29(Lys) w/ Glu

Front 12

what are the long acting insulin

Back 12

glargine
detemir

Front 13

how is Glargine made

Back 13

transpose A21 (Asn) w/ Gly and add 2 Asp at the C terminal end of the Beta chain

Front 14

how is Determir made

Back 14

add myristic acid to B29
omit B30(Thr)

Front 15

what substitutions can go on R of Sulfonlyurea to make it 1st gen

Back 15

CH3, NH2, COCH3, SCH3, Br, I, Cl, CF3

Front 16

what substitutions can go on R' of Sulfonlyurea to make it 1st gen

Back 16

Aryl (Toxic)
NCH3 (Inactive)
NC2H5 (lowers activity)
3-6 carbons (active)

Front 17

how do Sulfonylureas work

Back 17

they bind to the SUR-1 receptor on the pancrease causing the K channel to close resulting in re-polarization leading to an influx of calcium that facilitates the release of insulin

Front 18

are Sulfonylureas acidc or basic

Back 18

acidic due to the nitrogen bound hydrogen between the oxygens

Front 19

what are the 1st gen Sulfonlyurea

Back 19

tolbutamide
tolazamide
acetohexamide
chlorpropamide

Front 20

what are the 2nd gen Sulfonlyurea and the generic names

Back 20

glipizide (glucotrol)
glyburide (diabeta, glynase, micronase)
glimepiride (amaryl)

Front 21

what are insulin secretagogues

Back 21

they stimulate beta cells to secrete insulin and are potassium channel inhibitors

Front 22

what are the insulin secretagogues

Back 22

repaglinide
nateglinide (starlix)

Front 23

how is a metabolite that is as potent as the parent molecule formed in nateglinide

Back 23

once an isoprene derivative is formed by the addition of a double bond

Front 24

how come all insulins are not the same

Back 24

the C terminal of all insulin will contain a varied amount of AA

Front 25

what is the t1/2 of insulin analogs

Back 25

the half life of all insulin analogs vary

Front 26

what do Biguanides do

Back 26

increase insulin binding to insulin Rc and increase glucose utilization

Front 27

are biguanides unstable in light, acidic/basic, and water soluble/insoluble

Back 27

unstable in light due to guanide group

basic molecule due to guanide group

water soluble

Front 28

what do Thiazolidinedions (TZD) do

Back 28

insulin sensitizer

specific PPAR gamma receptor aganist that regulates transcription of insulin responsive genes involved in glucose transport etc

Front 29

what does Acarbose do

Back 29

it is a alpha amylase and membrane bound alpha glucosidase inhibitor thereby preventing the further breakdown of carbs into glucose

Front 30

what is the generic name of Acarbose

Back 30

Precose

Front 31

what is the generic name of Miglitol

Back 31

Glyset

Front 32

what do Alpha glucosidase inhibitors do

Back 32

inhibit alpha glucosidase enzyme thereby stopping further carbohydrate breakdown

Front 33

how many metabolites does Glipizide form

Back 33

2 all of which are inactive

Front 34

how many metabolites does glyburide form

Back 34

3 all of which are inactive

Front 35

how many metabolites does glimepiride have

Back 35

2

the carboxylic one is inactive

Front 36

what molecules are light sensitve

Back 36

PTU (alpha beta unsaturated ketone)
MMI (due to basic nitrogen)
Metformin (due to Guanidine)
T4/T3
Glyburide,Glimepiride
TZD WITH AROMATIC NITROGENS

Front 37

what molecules are water soluble

Back 37

miglitol
acarbose
MMI
Metformin

Front 38

what molecules are water insoluble

Back 38

T4/T3
PTU
ALL THE TZD ARE WATER INSOLUBLE UNLESS IN SALT FORM
2ND GEN SULFONYLUREA

Front 39

what molecules are acidic

Back 39

all the 2nd gen sulfonylureas

Front 40

what molcules are basic

Back 40

metformin
miglitol
acarbose

Front 41

what are the side effects of Acarbose and Miglitol

Back 41

cause a lot of gas, diarrhea, and abdominal pain

DOESN'T ABSORB WELL FROM THE GI