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Anti-Diabetes Drugs
IUSM
23
Pharmacology
Professional
10/08/2014

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Cards

Term
insulin formulations
Definition
Class: anti-diabetes

Mechanism: activates insulin receptors on target tissues, clear glucose from the blood and to increase anabolic activity in the liver/adipose/skeletal muscle

Indication: Type 1 and 2

Contraindications: hypersensitivity to insulin

Adverse effects: HYPOGLYCEMIA, INSULIN-SHOCK

Administration: subcutaneous or IV, continuous pumps rapid/short acting only

Absorption: differ in peaks and durations
Term
insulin shock
Definition
admin of inulsin in absence of adequate carbohydrate intake
Symptoms: impaired neurologic functions, inability to concentrate, slurred speech, lack of coordination, staggering, mimics alcohol intoxication
Tx: glucose (tablet, candy bar, fruit juice) or glucagon admin
Term
rapid-acting insulins
Definition
lispro, aspart, glulisine
[Humalog, novolog, apidra]
Term
short-acting insulins
Definition
regular
[Regular]
Term
intermediate-acting insulins
Definition
NPH
[Humulin, novolin, iletin]
Term
long-acting insulins
Definition
detemir, glargine
[levemir, lantus]
Term
acarbose
Definition
Class: anti-diabetes, alpha-glucosidase inhibitor

Mechanism: inhibit alpha-glucosidase in SI, delays carb digestion and absorption, smaller spike in postprandial glucose

Indications: adjunct to diet and exercise to improve glycemic control in DM2

Contraindications: diabetic ketoacidosis, disease of colon, chronic intestinal disease w/ digestion or absorption issues, breastfeeding

Adverse effects: GI UPSET (FLATULENCE, N, D), low serum iron levels; smaller risk of hypoglycemia/lactic acidosis/weight gain

Administration: oral three times a day with first bite of meal
Term
canagliflozin
Definition
Class: anti-diabetes, SGLT2 inhibitor

Mechanism: inhibit SGLT2 in proximal renal tubules, reduce reabsorption of filtered glucose, increased excretion of glucose, reduced plasma glucose

Indications: adjunct to diet and exercise to improve glycemic DM2

Contraindication: renal impairment

Adverse effects: yeast infection, UTI, enhanced serum potassium

Administration: oral admin 1x daily
Term
exenatide
Definition
Class: anti-diabetes, incretin, GLP1-receptor agonist

Mechanism: agonist at GLP1R, pontentiate glucose-mediated insulin secretion and supporess postprandial glucagon release

Indication: adjunct to diet and exercise to improve glycemic control in DM2

Contraindication: Type 1DM, diabetic ketoacidosis, renal impairment, severe GI disease, breastfeeding

Adverse effects: GI disturbance (dyspepsia, N, V, D), pancreatitis

Administration: subcutaneous injection
Term
glipizide
Definition
Class: anti-diabetes, insulin secretagogue, sulfonylureas

Mechanism: increase release of insulin; close ATP-sensitive K+ channels, depolarizes cell and triggers insulin release

Indications: adjunct to diet and exercise to improve glycemic control in adults with DM2 that have functioning beta cells

Contraindications: type 1DM, diabetic ketoacidosis, endothelin receptor antagonist, pregnancy/breastfeeding


Adverse effects HYPOGLYCEMIA, WEIGHT GAIN, disulfiram-like reactions, GI upset, (N,V,D, anorexia, hunger)

Administration: oral, once daily
Term
glucagon
Definition
Class: anti-diabetes

Mechanism: reduces hypoglycemia by activating catabolic actions in the liver to increase blood glucose, relaxes smooth muscle of GI tract

Indications: severe hypoglycemia 2* to excessive insulin

Contraindication: patients with pheochromocytoma or insulinoma, hypoglycemia 2* to starvation, adrenal insufficiency, chronic hypoglycemia

Adverse effects: N, V, hypotension

Administration: IV, IM, subcutaneous; give with carbs
Onset: 1-10minutes
Duration: 9-32 mintues
Term
metformin
Definition
Class: anti-diabetes, insulin sensitizer

Mechanism: suppresses gluconeogenesis in liver, increase insulin-dependent peripheral glucose utilization; AMP-activated kinase

Effects: increase liver insulin sensitivity, decrease plasma glucose and triglyceride load

Indications: adjunct to diet and exercise to improve glycemic control in Type 2DM; including those with beta cell loss

Contraindications: renal disease (serum creatinine >1.5mg/dL, shock, acute MI, septicemia), acidosis, hypoxia, pregnancy/breastfeeding

Adverse effects: LACTIC ACIDOSIS
Term
pioglitazone
Definition
Class: anti-diabetes, insulin sensitizer, thiazolidinediones

Mechanism: activate nuclear peroxisome proliferator activate receptor (PARA-gamma), alters lipid metabolism and glucose metabolism, increasing insulin sensitivity at target tissues

Indications: adjunct to diet and exercise to improve glycemic control in DM2

Contraindications: class III/IV failure, hepatic disease (P450 metabolized), pregnancy/breastfeeing

Adverse effects: INCREASE HDL, LDL AND TOTAL CHOLESTEROL, SLIGHT INCREASE IN ISCHEMIC EVENTS (MI AND AGINA), WEIGHT GAIN, fluid retention, bladder cancer
Term
repaglinide
Definition
Class: anti-diabetes, insulin secretagogue, meglitinides

Mechanism: closed ATP-sensitive K+ channels, depolarizes cell, triggers insulin release [distinct binding sight]

Indications: adjunct to diet and exercise to improve glycemic control; controls postprandial hyperglycemia w/o risk of long-lasting hypoglycemia

Contraindications: type 1DM, diabetic ketoacidosis, endothelin receptor antagonist, pregnancy/breastfeeding

Adverse effects HYPOGLYCEMIA, WEIGHT GAIN, disulfiram-like reactions, GI upset, (N,V,D, anorexia, hunger)
Term
rosiglitazone
Definition
Class: anti-diabetes, insulin sensitizer, thiazolidinediones

Mechanism: activate nuclear peroxisome proliferator activate receptor (PARA-gamma), alters lipid metabolism and glucose metabolism, increasing insulin sensitivity at target tissues

Effects: decrease lipolysis, decrease free fatty acids, increase insulin sensitivity

Indications: adjunct to diet and exercise to improve glycemic control in DM2

Contraindications: class III/IV failure, hepatic disease (P450 metabolized), pregnancy/breastfeeing

Adverse effects: INCREASE HDL, LDL AND TOTAL CHOLESTEROL, SLIGHT INCREASE IN ISCHEMIC EVENTS (MI AND AGINA), WEIGHT GAIN, fluid retention
Term
sitagliptin
Definition
Class: anti-diabetes, incretin, DPP4-inhibitor

Mechanism: inhibit DPP4 (enzyme for break down GLP1 to GIP), increases concentration of endogenous incretins, increase insulin release from beta cells

Contraindication: type 1 DM, diabetic ketoacidosis, severe GI disease, breastfeeding

Adverse effects: GI disturbance (dyspepsia, N, V, D), pancreatitis

Administration: oral
Term
aspart
Definition
Class: anti-diabetes, insulin formation

Rapid acting (1hr peak)
Term
glulisine
Definition
Class: anti-diabetes, insulin formation

Rapid-acting (1hr peak)
Term
lispro
Definition
Class: anti-diabetes, insulin formation

Rapid-acting (1hr peak)
Term
regular R
Definition
Class: anti-diabetes, insulin formation

Short-acting (4hr peak)
Term
NPH
Definition
Class: anti-diabetes, insulin formation

Intermediate-acting (4-7hr peak)
Term
detemir
Definition
Class: anti-diabetes, insulin formation

Long-acting
Term
glargine
Definition
Class: anti-diabetes, insulin formation

Long-acting (peakless)
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