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Test 5 Pharm (ch. 48-51)
Antidiabetic Agents
52
Pharmacology
Undergraduate 2
04/16/2011

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Cards

Term
Type I Diabetes
Definition
-insulin dependant, no beta cell production
Term
Type II Diabetes
Definition

-most common, some beta cell production, some insulin secretion

 

-tx w/ oral hypoglycemics

Term
Gestational Diabetes
Definition

-pregnancy induced by hormone changes

 

-may disappear after pregnancy, but some develop DM

Term
Drugs that elevate glucose levels
Definition
-thiazides, steroids, epinephrine
Term
Insulin
Definition

-protein secreted from beta cells in pancreas

 

-0.2-0.5 units/kg/day; the higher caloric intake, the more insulin secreted (obesity, stress, tissue insulin resistance)

 

-promotes uptake of glucose, converts to glycogen & stored in liver & muscle

 

-Normal serum glucose is 70-110; >180=glycosuria, polyuria

Term
Insulin derivatives
Definition

-beef/pork insulin (less allergenic)

 

-human insulin (DNA technology)-absorbed faster, shorter duration than beef/pork

 

-100 units/mL or 500 units/mL

 

-roll vial, don't shake

 

-WATCH HERBALS

Term
Insulin administration
Definition

-SQ or IV (only Regular), never oral (destroyed by gastric secretions)

 

-45-90 degree angle SQ

 

-heat/massage ^ absorption, cooling decreases absorption

 

-greatest absorption in abd & deltoid; thigh & buttock=lesser absorption

Term
Insulin precautions
Definition

-rotate injection sites to avoid lipodystrophy (more common in women & children)

 

-lipohypertrophy-raised bump/knot (more common in males)

 

-illness/stress increase demands for insulin; do not hold for illness

Term
Types of Insulin
Definition

-rapid-acting

-short-acting

-intermediate-acting

-long-acting

-combination

Term
Insulin side effects
Definition
-confusion, agitation, headache, tremors, hunger, weakness, lethargy, urticaria, redness, irritation at site
Term
Insulin adverse reactions
Definition
-tachycardia, hypoglycemic reaction, rebound hyperglycemia (Somogyi effect), lipodystrophy, anaphylaxis, shock
Term
Insulin drug-drug reactions
Definition

-hypoglycemia w/ aspirin, warfarin, alcohol, oral hypoglycemic, beta-blockers, TCA, MAOI, tetracycline

 

-hyperglycemia w/ thiazides, steroids, oral contraceptives, thyroid drugs, smoking

Term
Rapid-acting Insulin
Definition

-clear

-give no more than 5 mins before meal

-onset is 5-15 mins, peak is 30-60 mins, duration is 3-4 hours

-need intermediate type also to control glucose

 

-lispro (Humalog), insulin aspart (Novolog)

Term
Short-acting Insulin
Definition

-clear

 

-give 30 mins before meal

 

-onset 30-60 mins, peak 2-4 hours, duration 6-8 hours

 

-Humulin R - SQ & IV

Term
Intermediate-acting Insulin
Definition

-cloudy

-give in AM

-onset 1-2 hours, peak 6-12 hours, duration 18-24 hours

 

-NPH, Humulin N (protamine)-prolongs action, Lente, Humulin L (zinc)-slows onset & prolongs action,

Term
Long-acting Insulin
Definition

-Lantus

-Levemir

Term
insulin  glarnine (Lantus)
Definition

-long-acting insulin

 

-given at bedtime

 

-onset 1 hour, no peak, duration 24 hours

 

-pre-filled pen said to be more painful

Term
insulin detmir (Levemir)
Definition

-long-acting insulin

 

-peaks 6-8 hours, duration 12-24 hours

 

-pre-filled pen

Term
Combination insulin (premixed)
Definition

-do not need to refrigerate insulin pens for 10 days (hospital)

 

-Humulin 70/30 (70% NPH, 30% Regular)

 

-Novolin 70/30, Humulin 50/50, Humalog 75/25

Term
Insulin resistance
Definition

-antibodies develop over time, slowing onset of action & extending duration

 

-obesity contributes to insulin resistance

 

-can also develop insulin allergy (Human & Regular insulins have less allergic response)

Term
Storage of Insulin
Definition

-unopened vial are refrigerated

 

-opened vials kept at room temp for 4 weeks, 12 weeks in refrigerator

 

-less irritating to tissues if injected at room temp

 

-DO NOT FREEZE, do not place in heat/direct sunlight

 

-prefilled syringes kept in refrigerator and used w/ in 1-2 weeks (at home)

Term
Sliding Scale Insulin
Definition

-blood glucose checked before meals & bedtime

 

-insulin dose given according to glucose level

 

-rapid or short-acting insulin used for sliding scale (coverage)

Term
Hypoglycemic reaction/insulin shock
Definition

-occurs when more insulin is administered than what is needed

 

-s/s: nervous, trembling, cold/clammy skin, headache, lack of coordination, foggy thinking, combative, incoherent

 

-blood sugar < 60

 

-Tx: IV or oral glucose

Term
Dawn syndrome
Definition

-hyperglycemia on awakening

 

-headache, night sweats, nightmares

 

-increase bedtime insulin

Term
Somogyi syndrome
Definition

-hypoglycemia at 2-4 am

 

-reduce bedtime insulin

Term
Ketoacidosis
Definition

-fatty acids (ketones) are being used for energy due to sugar not being utilized

 

-s/s: thirst, polyuria, fruity breath, rapid & thready pulse, dry mucous membranes, Kussmaul respirations (deep, rapid, labored)

 

-blood sugar > 250

Term
Insulin Pens
Definition

-looks like fountain pen, more $$

 

-disposable, insulin-filled syringe

 

-disposable needle

 

-151-300 units in pen

 

-examples: Novolog Flex-Pen, Lantus Solostar, Humalog-Pen, Apidra OptiClik, Levemir FlexPen

Term
Insulin Pumps
Definition
-portable, insulin jet injectors, & implantable
Term
Portable Insulin pump
Definition

-external; needle SQ in abd, upper thigh, upper arm

 

-continuous SQ insulin infusion (CSII)

 

-battery operated

 

-Regular insulin only

 

-basal insulin (usually 3/day) w/ boluses for meals

 

-programmed by patient

 

-can be disconnected to bathe, swim; not for more than 1-2 hours

 

-even glucose levels w/ less hypoglycemia & long-term complications

Term
Insulin Jet Injectors
Definition

-delivered w/o needle

 

-sting, burning

 

-not for children or elderly

 

-$$

Term
Implantable Isulin Pump
Definition

-surgically implanted in abd (intraperitoneal or IV)

 

-delivers basal insulin and bolus doses w/ meals

 

-controlled glucose levels, less hypoglycemia

Term
Oral Antidiabetic Agents
Definition

-for Type II Diabetes only

 

-1st & 2nd generation Sulfonylureas

 

-nonsulfonylureas

 

-alpha-glucosidase inhibitors

 

-thiazolidinediones

 

-meglitinides

 

-incretin modifier

Term
1st Generation Sulfonylureas
Definition

-not common anymore

 

-stimulate beta cells in pancreas to secrete more insulin

 

-contraindicated in pregancy, lactation, DKA, infection/stress

 

-no alcohol...severe hypoglycemia

 

-warfarin, ASA, MAO, some NSAID (increase action)

-phenytoin, warfarin, steroids, INH (decrease action)

Term
1st Generation Suflonylurea Drugs
Definition

-Short-acting: tolbutamide (Orinase)-500-3000 mg/day in 2-3 doses

 

-Intermediate-acting: acetohexamide (Dymelor)-251 mg/day before breakfast

 

-tolazamide (Tolinase)-100-251 mg/day

 

-Long-acting: chlorpropamide (Diabinese)-100-510 mg/day; may cause fluid retention

Term
2nd Generation Sulfonylureas
Definition

-more common, work better than 1st generation

 

-increase tissue response to insulin

 

-decrease glucose production by liver

 

-greater hypoglycemic potential than 1st generation (elderly)

 

-longer duration, fewer side effects

 

-do not use w/ liver/renal issues

 

-less protein-binding issues w/ warfarin, ASA

 

-No alcohol

 

-drug-drug: same as 1st generation

Term
2nd Generation Sulfonylureas Drugs
Definition
-Amaryl, glipizide (Glucotrol, Glucotrol XL), Glyburide (Micronase, DiaBeta), glyburide micronized (Glynase)
Term
glimeperide (Amaryl)
Definition

-2nd generation sulfonylureas, directly stimulate beta cells

 

-improves post-prandial levels

 

-used w/ insulin in Type II

 

-SE: abd cramping, diarrhea

Term
Nonsulfonylureas
Definition

-biguanides

-alpha-glucosidase inhibitors

-thiazolidinediones

-meglitinides

-incretin modifier

Term
Biguanide
Definition
-metformin (Glucophage)
Term
*metformin (Glucophage)
Definition

-decreases liver production of glucose from stored glycogen

 

-decreases glucose absorption from small intestine

 

-increases insulin receptor sensitivity

 

-does not produce hyper- or hypoglycemia

 

-do not use w/ renal insufficiency

 

-hold drug 48 hours before & after IV contrast dye due to lactic acidosis or ARF

 

-dose: 510 mg qd, increase slowly

 

-SE: bloating, cramping, diarrhea

 

-adverse: malabsorption of B12

 

-many drug-drug reactions

Term
Alpha-Glucosidase Inhibitors
Definition
-acarbose (Precose), miglitol (Glyset)
Term
acarbose (Precose)
Definition

-inhibits enzyme in small intestine that releases glucose from complex carbs in diet; cannot absorb carbs & are passed through to large intestine

 

-no systemic effects

 

-used in conjunction w/ diet, 25 mg w/ meals

Term
miglitol (Glyset)
Definition

-absorbed from GI tract

 

-does not cause hypoglycemia unless taken w/ insulin or sulfonylurea

 

-25-100 mg w/ meals

 

-SE: GI

Term
Thiazolidinediones
Definition

-decrease insulin resistance & improve glucose control

 

-Actos, Avandia

Term
pioglitazone (Actos)
Definition

-may be combined w/ insulin or sulfonylureas

 

-SE: hepatotoxic; monitor LFTs

Term
rosiglitazone (Avandia)
Definition

-may be combined w/ metformin (Avandamet)

 

-SE: hepatotoxic, monitor LFTs, recent increase in cardiac deaths

Term
Meglitinides
Definition

-stimulate beta cells to release insulin

 

-short-acting

 

-do not use w/ liver dysfunction

 

-repaglinide (Prandin), nateglinide (Starlix); take before meals, may use w/ metformin (Glucophage)

Term
Incretin Modifier
Definition

-increase insulin secretion, reduce glucagon secretion

 

-reduces fasting & postprandial glucose levels

 

-sitagliptin (Januvia)-100 mg qd

Term
exenatide (Byetta)
Definition

-antidiabetic agent; improves beta-cell response

 

-injectable, not insulin, mimics incretin

 

-slows gastric emptying

 

-suppresses appetite --> weight loss

 

-SE: jittery

 

-5-10 mcg SQ before meal

Term
pramlintide (Symlin)
Definition

-antidiabetic agent

 

-never given in arm

Term
Glucagon
Definition

-emergency hyperglycemic agent

 

-treat insulin-induced hypoglycemia

 

-SQ, IM, IV; onset 5-20 mins

Term
diazoxide (Proglycem)
Definition

-hyperglycemic agent, related to thiazides

 

-treat hypoglycemia due to islet cell (pancreatic) cancer or hyperplasia

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