173 DM drugs

Question 1

insulin receptor type and mechanism of action once bound

Answer 1

receptor tyrosine kinase –> tyrosine phosphorylation activates…

1) phophoinositide-3 kinase pathway –> glycogen synthesis AND GLUT4 into membrane
2) Ras/MAP kinase pathway –> cell growth and differentiation

Question 2

is insulin anabolic or catabolic? what transporter is insulin dependent? what tissue has it?

Answer 2

anabolic in liver, muscle, fat

GLUT4

muscle and adipose

Question 3

what happens to glycogen, triglycerides, and proteins with an insulin deficiency?

Answer 3

broken down to provide fuel –> hyperglycemia –> osmotic diuresis, dehydration –> low cerebral bloodf low –> coma and death

also get ketone bodies –> metabolic acidosis

Question 4

short acting insulins names? Difference?

Answer 4

regular + “LAG”
lispro
aspart
glulisine

the bottom 3 are faster onset - take before meal and last while meal is digested

asapart and gluilisine are used for CSII

Question 5

longer acting insulin

Answer 5

NPH (neutral protamine hagedorn) - protamine slows absorption

Glargine - acidic so can’t mix

detemir - binds albumin

1-2 x day w/ short acting insulin

Question 6

insulin regimens

Answer 6

basal/bolus - long acting at night or morning w/ premeal short acting insulin

split-mixed - pre breakfast and pre dinner injections - combo of short and long acting

Question 6

insulin SE

Answer 6

hypoglycemia

Question 7

ketoacidosis rx

Answer 7

hyperglycemia responds more rapidly than acidosis

Question 8

insulin-induced hypoglycemia rx

Answer 8

1 glucose - oral,iv

alternatives:

glucagon - sc, im, iv –> GPCR –> cAMP –> increases hepatic glucose production

diazoxide - opens K channel, decreases insulin

Question 9

sulfonylureas

• suffix
• mechanism
• use
• toxicity

Answer 9

_ride (glyburide)
_amide
_zide (glipizide)

blocks K channel –> depol –> insulin release

DM2 (requires islet fxn)

hypoglycemia (esp old with bad liver/kidney)

Question 10

DPP-4 inhibitors

• suffix
• mechanism
• use
• toxicity

Answer 10

_agliptin

–I serine protease dpp-4 which stops it from blocking GLP-1 (thus allows GLP-1 to fxn) –> increases Insulin AND lowers glucagon

DM2

UTI, respiratory infections

Question 11

Biguanides

• drug
• mechanism
• use
• toxicity

Answer 11

metformin

AMP kinase –> decreases gluconeogenesis, increases glucose uptake

monotherapy, 1st line for DM2 (can be used in those without islet fxn)

GI upset, lactic acidosis (careful in those w/ renal failure)

Question 12

GLP mimetics

• suffix
• mechanism
• use
• toxicity

Answer 12

__tide (NOT _lintide) - exenatide, liraglutide

GPCR –> cAMP –> PKA –> Ca –> insulin release AND lowers glucagon release

DM 2

nausea, vomiting, pancreatitis

Question 13

thiazolidinediones

• suffix
• mechanism
• use
• toxicity

Answer 13

_litazone (pioglitazone)

binds PPAR –> promotes transcription of insulin sensitive genes in liver, muscle, adipose –> increases insulin sensitivity

DM2

weight gain, edema, hepatotoxicity, heart failure

Question 14

a-glucosidase inhibitors

• drugs
• mechanism
• use
• toxicity

Answer 14

acarbose
miglitol

–I glucosidase at brush border –> decreased glucose absorption

DM2

GI pain

Question 15

amylin analogs

• drug
• mechanism
• use
• toxicity

Answer 15

pramlintide

mimics amylin in hindbrain –> slows gastric emptying –> decreases glucose concentrations after meals AND decreases glucagon

DM1 and 2

hypoglycemia, nausea, diarrhea

Question 16

what increases glucose excretion?

Answer 16

SGLT2 inhibitor - canagliflozin

Question 17

what drug is used first in DM?

Answer 17

metformin

if A1C not <7% at 3-4 months, add 2nd drug