Antidiabetic Agents Flashcards
1
Q
Aspart
A
- Insulin/analog – rapid acting
- B28 Pro to Asp promotes absorption by preventing self association
- Hypoglycemia, lipodystrophy, insulin allergy/resistance
- Diabetes – subq for routine or IV for emergencies
2
Q
Detemir
A
- Insulin/analog – long acting
- C-terminal Thr B chain deleted and myristic acid attached to C-terminal Lys increases self aggregation and binding to albumin
- Hypoglycemia, lipodystrophy, insulin allergy/resistance
- Diabetes – subq for routine or IV for emergencies
3
Q
Glargine
A
- Insulin/analog – long acting
- A21 Asn to Gly, Arg added at B31 and B32 – soluble at acidic pH but precipitates at neutral pH
- Hypoglycemia, lipodystrophy, insulin allergy/resistance
- Diabetes – subq for routine or IV for emergencies
4
Q
Glulisine
A
- Insulin/analog – rapid acting
- B3 Asn to Lys, B29 Lys to Glu promotes absorption by preventing self association
- Hypoglycemia, lipodystrophy, insulin allergy/resistance
- Diabetes – subq for routine or IV for emergencies
5
Q
Lispro
A
- Insulin/analog – rapid acting
- B28 and B29 to Lys-Pro promotes absorption by preventing self association
- Hypoglycemia, lipodystrophy, insulin allergy/resistance
- Diabetes – subq for routine or IV for emergencies
6
Q
NPH
A
- Insulin/analog – intermediate acting
- Wild type amino acid sequence – protamine and insulin are in a complex
- Hypoglycemia, lipodystrophy, insulin allergy/resistance
- Diabetes – subq for routine or IV for emergencies
7
Q
Regular crystalline insulin
A
- Insulin/analog – short acting
- Wild type amino acid sequence
- Hypoglycemia, lipodystrophy, insulin allergy/resistance
- Diabetes – subq for routine or IV for emergencies
8
Q
Exenatide
A
- Incretin agonist – subq injection
- Increase insulin, decrease glucagon, decrease postprandial glucose
- Nausea, anorexia, headache, diarrhea, pancreatitis
- Diabetes
9
Q
Sitagliptin
A
- Inhibitor of incretin degradation - oral
- Increase insulin, decrease glucagon, decrease postprandial glucose
- Headache, increased infections, pancreatitis
- Diabetes
10
Q
Pramlintide
A
- Amylin analog – subq
- Inhibits glucagon secretion, has CNS-mediated anorectic effect
- Hypoglycemia, nausea, vomiting, anorexia
- Type 2 or with insulin for type 1
11
Q
Chlorpropamide
Tolbutamide
A
- Sulfonylurea – 1st generation (Chlor 60 hr, Tol 6-12 hr)
- Increase insulin secretion by decreasing K efflux from B cells in pancreas
- Hypoglycemia, sulfonylurea resistance, tachyphylaxis
- Diabetes - not as readily available
12
Q
Glipizide
Glyburide
Glimepiride
A
- Sulfonylurea – 2nd generation (10-24 hr)
- Increase insulin secretion by decreasing K efflux from B cells in pancreas
- Increase insulin secretion by decreasing K efflux from B cells in pancreas
- Hypoglycemia, sulfonylurea resistance, tachyphylaxis
- Diabetes - more potent and readily available
13
Q
Repaglinide
A
- Meglitinide (4-5 hr)
- Prevent efflux from B cells leading to increased insulin secretion (higher binding affinity)
- Hypoglycemia, use caution with renal/hepatic insufficiency
- Diabetes – more potent than sulfonylurea
14
Q
Nateglinide
A
- Phenylalanine analog (faster effect, less sustained)
- Increase insulin secretion by decreasing K efflux from B cells in pancreas
- Hypoglycemia, safer with renal failure
- Diabetes
15
Q
Metformin
A
- Biguanide
- Inactivate mitochondrial glycerophosphate dehydrogenase, antagonize actions of glucagon, activate AMP protein kinase
- GI discomfort, lactic acidosis, no hypoglycemia or weight gain
- First line therapy in type 2 diabetes
