Pharm 41 Drugs Used In Diabetes

Front 1

Cleavage of proinsulin produces insulin and what other product?

The absence of this indicates what?

Back 1

C-peptide

exogenous administration of insulin

Front 2

What is insulin's mechanism of signal transduction?

Back 2

Insulin + tyrosine kinase receptor --> autophosphorylation --> IRS-1 binds receptor and is phosphorylated --> SH2-proteins bind IRS-1 --> translocation of GLUT-4 (PI-3 kinase activity), gene expression in nucleus (PI-3 kinase and p21ras G-protein activity)

Front 3

Rapid-acting insulins?

Clinical Use?

Back 3

Lispro, Aspart, Glulisine

control of postprandial glucose levels, emergency tx of diabetic ketoacidosis

Front 4

Short acting insulin?

Clinical use?

Back 4

Regular insulin

IV in emergencies, SQ in normal maintenance regimens (must be taken 1h before meal)

Front 5

Intermediate-acting insulins?
Characteristics?

Back 5

NPH
Combination regular insulin and protamine, delayed onset and peak of action

Front 6

Long-acting insulins?

Characteristics?

Back 6

Glargine, detemir

peakless basal insulin level lasting more than 20h w/o causing hypoglycemia

Front 7

Tx for hypoglycemia d/t excessive insulin effect?

Back 7

Prompt admin of glucose or glucagon

Front 8

What are the classes of non-insulin antidiabetic drugs?

Back 8

Sulfonylureas
Biguanides
Thiazolidinediones
α-glucosidase inhibitors

Front 9

MOA of sulfonylureas?

Back 9

Close K channels in B cell membrane --> cell depolarization --> increase Ca --> insulin release

Front 10

2G sulfonylureas?

Characteristics?

Back 10

glyburide, glipizide, glimepiride

more potent than 1G

Front 11

1G sulfonylureas?

characteristics?

Back 11

tolbutamide, chlorpropamide

Chlorpropamide has long duration
Extensively bound to serum proteins (drugs that compete for protein binding may enhance hypoglycemic effects)

Front 12

Newest class of insulin secretagogues?

Characteristics?

Back 12

Repaglinide (meglitinide), nateglinide

rapid onset, short duration

Front 13

Most common side effects of all insulin secretagogues?

Back 13

hypoglycemia, weight gain

Front 14

Actions of metformin?

Significance?

Back 14

inhibit hepatic gluconeogenesis, stimulate glucose uptake and glycolysis in peripheral tissue, slow glucose absorption in GI, reduce plasma glucagon levels.

Does not cause hypoglycemia or weight gain

Front 15

Which of the treatments for Type II diabetes cause weight gain?

Back 15

insulin, insulin secretagogues, and thiazolidinediones

Front 16

Toxic effects of metformin?

Back 16

GI distress (nausea, diarrhea), lactic acidosis

Front 17

Thiazolidinediones?

MOA?

Back 17

Rosiglitazone, pioglitazone

1. Increase insulin sensitivity by activating PPAR-γ receptor (which regulates txn of proteins for CHO and lipid metabolism)
2. Increase glucose uptake in adipose and muscle
3. Inhibit hepatic gluconeogenesis

Front 18

Toxic effects of thiazolidinediones?

Back 18

Fluid retention (anemia, edema, may increase risk for CHF)
Liver toxicity (induce CYP450)

Front 19

α-glucosidase inhibitors?

MOA?

Back 19

Acarbose, miglitol

CHO analogs that inhibit α-glucosidase (converts CHOs in intestines to saccharides that can be absorbed - do not affect fasting blood glucose)

Front 20

Toxic effects of α-glucosidase inhibitors?

Back 20

flatulence, diarrhea, abd pain from increased fermentation of unabsorbed CHO

Front 21

How would you treat a pt experiencing hypoglycemia from taking an α-glucosidase inhibitor?

Back 21

Oral dextrose (glucose), NOT sucrose (will not be absorbed)

Front 22

MOA of pramlintide?

Clinical use?

Back 22

analog of amylin (pancreatic hormone), suppresses glucagon release, slows gastric emptying, CNS anorexogenic

Used w/ insulin for postprandial glucose control

Front 23

Toxic effects of pramlintide?

Back 23

hypoglycemia, GI upset

Front 24

Which antidiabetic drug is a synthetic analog of glucagon-like peptide-1?

Back 24

Exenatide

Front 25

MOA of Exenatide?

Back 25

Augment glucose-stimulated insulin release from beta cells, retard gastric emptying, inhibit glucagon secretion, and produce a feeling of satiety

Front 26

Clinical use of Exenatide?

Back 26

Combination with metformin or sulfonylurea for type 2 DM

Front 27

Toxic effects of Exenatide?

Back 27

GI upset (esp nausea)
hypoglycemia when combined with sulfonylurea

Front 28

MOA of Sitagliptin?

Back 28

inhibits dipeptidyl peptidase-4 (DPP4) which degrades GLP-1 and other incretins, thus, has same effects as Exenatide

Front 29

Toxic effects of Stagliptin?

Back 29

HA, nasopharyngitis, URI

Front 30

Treatment regimen for type 2 DM?

Back 30

Insulin-action-augmenting drug (metformin, thiazolidinedione, or α-glucosidase inhibitor)
+
insulin-supply-augmenting drug (insulin secretagogue or insulin)

Front 31

Actions of glucagon?

Back 31

Acts through G protein-coupled receptors in heart, sm. muscle and liver to increase HR and contractility, increase hepatic glycogenolysis and gluconeogenesis, relaxes sm. muscle (esp in gut)

Front 32

What drug is used to treat severe hypoglycemia in diabetics, but requires intact hepatic glycogen stores?

Back 32

Glucagon

Front 33

Which antidiabetic drugs promote the release of endogenous insulin?

Back 33

Sulfonylureas (tolbutamide, chlorpropamide, glyburide, glipizide, glimepiride)
Repaglinide
Nateglinide

Front 34

Why should pts with renal or liver dz, or alcoholism not receive metformin?

Back 34

Increased risk of lactic acidosis

Front 35

Which antidiabetic drugs are taken at the beginning of a meal to delay the absorption of CHOs?

Back 35

α-glucosidase inhibitors
(Acarbose, Miglitol)

Front 36

What non-diabetic condition is also treated using glucagon?

Back 36

Beta-blocker-induced cardiac depression