Diabetic Drugs

Question 1

C-peptide

Answer 1

released with insulin due to cleavage from same pro-peptide

Question 2

Insulin secretion phases

Answer 2

1) Priming phase - w/in 10 min. of food; required for normal insulin sensitivity; lost in Type 2 diabetes
2) Delayed phase - over hours

Question 3

Basal/bolus dosing

Answer 3

Basal - for steady state, b/w meals, overnight

Bolus - to prime for meals, limit post-prandial hyperglycemia

Question 4

Rapid acting insulin

Answer 4

• Lispro
• Aspart
• Glulisine

Question 5

Short acting insulin

Answer 5

Regular insulin; give 30 min before meal

Question 6

Intermediate acting insulin

Answer 6

• NPH
• protamine decreases solubility, incr. T1/2
• Basal insulin 2x/day

Question 7

Long-acting insulin

Answer 7

• Glargine - forms precip. at pH 7
• Detemir - binds albumin for slow release
• NEITHER of these can be mixed with other insulin preparations*

Question 8

Insulin S/E’s

Answer 8

• hypglycemia - rule of 15 - ingest 15g glucose, wait 15 min. and repeat until normal; glucagon kit if unable to swallow
• allergic rxns
• local lipoatrophy and lipohypertrophy at injection site

Question 9

Glyburide, Glipizide, Glimepiride (Gl__ide)

Answer 9

Sulfonylureas - stimulate insulin release by binding and inhibiting ATP-sensitive K+ channel in Beta cells

• Only useful in Type 2 who still have beta function
• S/E - weight gain, allergies
• Meglitinides have same mechanism but bind slightly different site

Question 10

Pioglitazone

Answer 10

Thiazolidinediones - improve insulin sensitivity by activating PPARv&raquo_space;PPARa>PPARB transcription factors that regulate FA metabolism

• promote adipocyte differentiation and storage of fat subcutaneously rather than in muscle, liver
• No assoc. hypoglycemia, can improve steatosis/NAFLD, insulin resist.
• S/E - takes wks to months for effect, wt. gain, LDL
• C/I - heart failure

Question 11

Metformin

Answer 11

Biguanide - improve insulin sensitivity, primarily in liver (decr. gluconeogen., incr. glucose uptake)

• No hypoglycemia, possible wt. loss, improved lipids
• S/E - lacticacidosis (C/I in renal/liver problems), GI, B12 deficiency

Question 12

alpha glucosidase inhibitor

Answer 12

decreases carb absorption by inhibiting breakdown of complex sugars

• response depends on diet
• If hypoglycemia occurs, cannot give oral sucrose but must be glucose

Question 13

Liraglutide

Answer 13

GLP-1 analog stimulates insulin release and beta cell growth, decreases glucagon, appetite, and gastric emptying
- Injectable, can cause pancreatitis; not recommended if MTC or MEN mutations

Question 14

Sitagliptin

Answer 14

DPP-IV inhibitor

• DPP-IV degrades GLP-1/G1P so this increases their levels
• stimulates insulin levels and B cell growth, decreases glucagon and appetite

Question 15

Dopamine agonist

Answer 15

Bromocriptine - may increase insulin sensitivity

S/E - dizziness, syncope, orthostasis

Question 16

Canagliflozin

Answer 16

SGLT-2 inhibitor - decreases glucose by decreasing renal threshold for glucose and increasing urinary glucose, causing mild diuresis

• S/E - ineffective if renal failure or low GFR, increased genital infections, hypotension
• glucose ‘floz’ out in pee