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19 Cards in this Set

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Aspart
Rapid Acting Insulin

Mechanism:*Rapid acting Insulin --> mimic prandial release of insulin

Adverse Reaction:*Hypoglycemia *Autonomic hyperactivity when glucose <60-80 mg/dl

Clinical Use:*All type 1 DM patients *Type 2 DM patients not controlled by diet and oral hypoglycemic *Post-pancreatectomy diabetes *Gestational diabetes *DKA *Nonketoacidtotic hyperglycemic coma *not used alone *used with longer-acting insulin to assure proper glucose control.
Lispro
Rapid Acting Insulin

Mechanism:*Rapid acting Insulin --> mimic prandial release of insulin

Adverse Reaction:*Hypoglycemia *Autonomic hyperactivity when glucose <60-80 mg/dl

Clinical Use:*All type 1 DM patients *Type 2 DM patients not controlled by diet and oral hypoglycemic *Post-pancreatectomy diabetes *Gestational diabetes *DKA *Nonketoacidtotic hyperglycemic coma *not used alone *used with longer-acting insulin to assure proper glucose control.
Regular Insulin
Mechanism:*Binds insulin receptor --> activates tyrosine kinase --> phosphorylation of docking proteins and insulin receptor substrate 1-6 (IRS 1-6) --> IRS 1-6 bind other kinases to have cellular effects
*Rapidly lowers blood sugar

Adverse Reaction:*Hypoglycemia *Autonomic hyperactivity when glucose <60-80 mg/dl

Clinical Use:*Safe in pregnancy *All type 1 DM patients *Type 2 DM patients not controlled by diet and oral hypoglycemic *Post-pancreatectomy diabetes *Gestational diabetes *DKA *Nonketoacidtotic hyperglycemic coma
Neutral Protamine Hagedron (NPH) Isophane
Intermediate Acting Insulin

Mechanism:*Delayed absorption of insulin due to protamine --> extends action

Adverse Reaction:*Hypoglycemia *Autonomic hyperactivity when glucose <60-80 mg/dl

Clinical Use:*All type 1 DM patients *Type 2 DM patients not controlled by diet and oral hypoglycemic *Post-pancreatectomy diabetes *Gestational diabetes *Not for ketoacidosis or emergency hyperglycemia *used with regular insulin
Glargine
Long Acting Insulin

Mechanism:*Precipitation at injection site --> extends its action

Adverse Reaction:*Hypoglycemia *Autonomic hyperactivity when glucose <60-80 mg/dl

Clinical Use:*All type 1 DM patients *Type 2 DM patients not controlled by diet and oral hypoglycemic *Post-pancreatectomy diabetes *Gestational diabetes *DKA *Nonketoacidtotic hyperglycemic coma
Dethomir
Long Acting Insulin

Mechanism:*associates with tissue-bound albumin at injection site --> extends its action

Adverse Reaction:*Hypoglycemia *Autonomic hyperactivity when glucose <60-80 mg/dl

Clinical Use:*All type 1 DM patients *Type 2 DM patients not controlled by diet and oral hypoglycemic *Post-pancreatectomy diabetes *Gestational diabetes *DKA *Nonketoacidtotic hyperglycemic coma
Chlorpropamide
1st Generation Sulfanylurea

Mechanism:*↑insulin release from pancreatic B-cell. *Binds to sulfonylurea receptor --> inhibits ATP-sensitive K+ channel --> ↓ efflux of K+ --> depolarization --> open voltage-gated Ca channel --> ↑Ca influx --> release of preformed insulin

Adverse Reaction:*Hypoglycemia *Weight gain *potentiate ADH effects *alcohol induced flushing

Clinical Use:*Hyperglycemia control in type 2 diabetics who cannot control with diet alone.
Glimepiride
2nd generation Sulfanylurea

Mechanism:*↑insulin release from pancreatic B-cell. *inhibits ATP-sensitive K+ channel --> ↓ efflux of K+ --> depolarization --> open voltage-gated Ca channel --> ↑Ca influx --> release of preformed insulin

Adverse Reaction:*hypoglycemia *weight gain

Clinical Use:*Hyperglycemia control in type 2 diabetics who cannot control with diet alone.
Glipizide
2nd generation Sulfanylurea

Mechanism:*↑insulin release from pancreatic B-cell. *inhibits ATP-sensitive K+ channel --> ↓ efflux of K+ --> depolarization --> open voltage-gated Ca channel --> ↑Ca influx --> release of preformed insulin

Adverse Reaction:*hypoglycemia *weight gain

Clinical Use:*Hyperglycemia control in type 2 diabetics who cannot control with diet alone.
Glyburide
2nd generation Sulfanylurea

Mechanism:*↑insulin release from pancreatic B-cell. *inhibits ATP-sensitive K+ channel --> ↓ efflux of K+ --> depolarization --> open voltage-gated Ca channel --> ↑Ca influx --> release of preformed insulin

Adverse Reaction:*hypoglycemia *weight gain

Clinical Use:*Hyperglycemia control in type 2 diabetics who cannot control with diet alone.
Repaglinide
Meglitinides

Mechanism:*↑insulin release from pancreatic B-cell. *inhibits ATP-sensitive K+ channel --> ↓ efflux of K+ --> depolarization --> open voltage-gated Ca channel --> ↑Ca influx --> release of preformed insulin

Adverse Reaction:*hypoglycemia

Clinical use:*Control post-randial glucose elevation in type 2 diabetic patients *monotherapy or combination
Nateglinide
Meglitinides

Mechanism:*↑insulin release from pancreatic B-cell. *inhibits ATP-sensitive K+ channel --> ↓ efflux of K+ --> depolarization --> open voltage-gated Ca channel --> ↑Ca influx --> release of preformed insulin

Adverse Reaction: *Less hypoglycemia than other insulin secretagogue

Clinical use:*Control post-randial glucose elevation in type 2 diabetic patients *monotherapy or combination
Metformin
Biguanides

Mechanism:*Antihyperglycemic NOT hypoglycemic *↑AMP-kinase --> ↓Hepatic gluconeogenesis, ↓Renal gluconeogenesis, ↓Glucose absorption from GI tract

Adverse Reaction:*DOES NOT cause hypoglycemia *GI side effects *Lactic acidosis: ↓gluocneogenesis --> impairs hepatic metabolism of lactic acid *↓B12 absorption (long term)

Clinical use:*Type 2 diabetes *Insulin resistance *↓serum lipids *combination therapy
Pioglitazone
Thiazolidinediones

Mechanism:*PPAR-y activation --> ↑adiponectin --> ↑glucose transport into muscle and ↑fatty acid oxidation *↑insulin sensitivity

Adverse Reaction:*↑HDL *Fluid retention:anemia, weight gain, edema (obese at greatest risk) *rare hepatotoxicity

Clinical use:*Type 2 diabetes treatment *Type 2 diabetes prevention *monotherapy or combination
Rosiglitazone
Thiazolidinediones

Mechanism:*PPAR-y activation --> ↑adiponectin --> ↑glucose transport into muscle and ↑fatty acid oxidation *↑insulin sensitivity

Adverse Reaction:*↑HDL *Fluid retention:anemia, weight gain, edema (obese at greatest risk) *rare hepatotoxicity

Clinical use:*Type 2 diabetes treatment *Type 2 diabetes prevention *monotherapy or combination
Acarbose /Miglitol
Alpha-glucosidase inhibitors

Mechanism:*↓action of a-glucosidase -->↓intestinal absorption of carbohydrates, starch, dextrin and disaccharide --> ↓postrandial glucose

Adverse Reaction:*malabsorption *GI disturbance *No hypoglycemia when used alone

Clinical use:*Type 2 diabetes *monotherapy and in combination
Pramlintide
Amylin analog

Mechanism:*↓Glucagon release --> ↓gastric emptying

Adverse Reaction:*Hypoglycemia, GI symptoms

Clinical use:*Adjunctive mealtime administration in type 2 diabetes.
Exanatide
GLP-1 analog

Mechanism:*Synthetic analog of glucagon-like-polypeptide (GLP-1)
*Potentiates glucose-mediated insulin secretion --> ↓postrandial glucagon release, ↓gastric emptying, CNS anoretic effect

Adverse Reaction:*GI symptoms

Clinical use:*Adjunctive in type 2 diabetes.
Sitagliptin
Dipeptidyl peptidase -4 inhibitor

Mechanism:*Inhibits DPP-4 --> weight loss *DDP-3 degrades incretin and other GLP-1-like molecules

Adverse Reaction:*hypoglycemia

Clinical use:*Adjunctive in type 2 diabetes.