Drugs- Insulin and oral hypoglycemic agents (Martin) Flashcards

Question

what is TDI

Answer 1

0.3-0.5 units/kg/day and titrate to glycemic targets

Answer 2

1) 2/3 of the total dose is given before breakfast - - 2/3 of this is NPH - - 1/3 is Regular (injection #1) 2) 1/3 of the total dose is taken later in the day - - 1/3 of this is Regular taken just before dinner (injection #2) - -2/3 of this dose is NPH taken at bedtime (injection #3)

Answer 3

Dawn phenomena: both normal and diabetic patients have an increased requirement for insulin in the early morning, making the kinetics and timing of the evening dose of insulin extremely important.

Answer 4

A pre-breakfast dose of Glargine (or detemir) and rapid-acting or regular insulin is taken along with additional doses of rapid-acting or regular insulin at lunchtime and dinnertime. Glargine insulin provides a basal requirement for insulin, while the rapid acting insulin meets the postprandial demand. To achieve more uniform basal levels, the dose of basal insulin is sometimes divided into morning and evening doses.

Answer 5

a system composed of a battery-operated pump and a computer than can program the pump to deliver predetermined amounts of insulin from a reservoir to a subcutaneous inserted catheter or needle. These systems are portable and designed to deliver basal amounts of insulin throughout the day as well as meal-related bolus injections that the patient can initiate at 0-30 minutes prior to food intake. Regular, aspart, glulisine, and lispro insulin can be used in subcutaneous infusion pumps

Answer 6

to determine long term hyperglycemic control “Normal values” vary from laboratory to laboratory but usually range from 4% to 6% in nondiabetic patients. Each 1% increase in HbA1c can reflect an increase of 25 to 35 mg/dL in mean blood glucose concentration. HbA1c < 6.5% is a recommended target.

Answer 7

abdomen absorption is fastest from this site

Answer 8

Insulin glargine should not be mixed with any other form of insulin.

Answer 9

can slow absorption of the regular insulin

Answer 10

due to 1) inappropriate dose, 2) mismatch of time of injection vs food intake, 3) exercise-induced increased glucose utilization, or 4) other factors that increase the sensitivity to insulin (adrenal insufficiency, pituitary insufficiency). The more rigorous the attempt to achieve euglycemia, the greater the risk of hypoglycemia.

Answer 11

Decreased insulin secretion b. Counter-regulatory hormones released at glucose <=70 mg/dL (epinephrine, glucagon, GH, cortisol, norepinephrine). c. Autonomic symptoms: sweating, hunger, paresthesias, palpitations, tremor, anxiety. d. Neuroglycopenia symptoms: difficulty concentrating, confusion, weakness, drowsiness, a feeling of warmth, dizziness, blurred vision, and loss of consciousness.

Answer 12

normally, glucagon is the predominant counter-regulatory hormone. In Type 1 DM of long duration, glucagon secretion in response to hypoglycemia becomes deficient and epinephrine becomes the dominant glucose-mobilizing hormone. However, if the patient also suffers from autonomic neuropathy, the epinephrine response is also deficient and night-time severe hypoglycemia can result in convulsions and coma.

Answer 13

Treatment of Hypoglycemia: consists of ingesting glucose. If severe, IV glucose or glucagon injections can be employed.

Answer 14

The most frequent allergic reactions are IgE-mediated local cutaneous reactions, but occasionally patients may develop a life-threatening anaphylactic reaction or insulin resistance due to circulating IgG antibodies.

Answer 15

Diabetic ketoacidosis (DKA) is a serious condition that often calls for constant intravenous infusion of insulin. (Only regular or ultra-short acting insulins can be given IV). A relatively low dose of insulin (0.1 U/ kg /hr) is usually sufficient to inhibit lipolysis and gluconeogenesis completely and to produce near-maximal stimulation of glucose uptake. Blood glucose levels fall by about 10%/hr; the acidosis is corrected more slowly. Appropriate replacement of fluid and electrolytes is an integral part of the therapy. *** Insulin must be administered by SQ injection prior to discontinuing IV infusions because of the short plasma t1/2 of insulin.

Answer 16

perioperative control and childbirth

Answer 17

ethanol b-blockers- salicylates

Answer 18

β-antagonists pose a risk of hypoglycemia because of their capacity to inhibit the effects of catecholamines on gluconeogenesis and glycogenolysis. These agents also mask the sympathetically mediated symptoms associated with the fall in blood glucose, e.g., tremors and palpitations.

Answer 19

inhance pancreatic b-cell sensitivity to glucose and potentiate insulin secretion

Answer 20

inhibits gluconeogenesis

Answer 21

direct hyperglycemic effect

Answer 22

hyperglycemia by inhibiting insulin secretion

Answer 23

deplete K+ and indirectly inhibit insulin secretion

Answer 24

metformin The rare patient in which metformin is contraindacated may begin therapy with a sulfonylurea, insulin, or pioglitazone It is now recommended that the initial step of treatment for newly diagnosed Type 2 DM should be lifestyle changes to decrease weight and to increase activity along with metformin therapy.

Answer 25

no!! they must be treated with insulin

Answer 26

has an antihyperglycemic action; not a hypoglycemic action. Unlike the sulfonylurea drugs, it does not directly effect insulin release. It does not cause hypoglycemia even at high doses. Metformin appears to produce the following effects: • reduces hepatic glucose output by inhibiting gluconeogenesis * increases insulin action in peripheral tissues (increases anaerobic glycolysis), i.e., decreases insulin resistance * increases glucose uptake and utilization by muscle * reduces intestinal absorption of glucose

Answer 27

sulfonylurea or a TZD

Answer 28

Because metformin is an insulin sparing agent and does not cause weight gain or provoke hypoglycemia, it offers advantages over sulfonylureas and insulin in treating obese, insulin-resistant patients. It also has a a significant lipid-lowering effect, i.e., it decreases total cholesterol, LDL, and triglycerides.

Answer 29

abdominal discomfort, anorexia, nausea, metallic taste, and diarrhea.

Answer 30

Metformin should not be administered to patients with renal impairment, hepatic disease, a history of lactic acidosis, cardiac failure, or chronic hypoxic lung disease because of the concern for the development of lactic acidosis.

Answer 31

E. Metformin is usually administered two to three times daily with meals. It is rapidly absorbed and cleared through the kidneys.

Answer 32

use in caution with elderly pt's with renal failure and others predisposed to hypoglycemia

Answer 33

glipizide glyburide glimepriride

Answer 34

Sulfonylureas bind to and block an ATP-sensitive K+ channel. Blockade of this channel reduces K+ conductance causing membrane depolarization and influx of Ca2+ through voltage-sensitive Ca2+ channels. Ca2+ influx leads to insulin secretion. Initially (first few months of treatment), fasting plasma insulin levels and insulin responses to oral glucose are increased. With chronic administration, circulating insulin levels decline to those that existed before treatment, but, reduced plasma glucose levels are maintained.

Answer 35

increased numbers of insulin receptors, increased glucose transporters, and purported enhanced tissue responsiveness to insulin. Hepatic gluconeogenesis is suppressed. Whether these are direct effects of the sulfonylurea drugs or a result of lower blood glucose levels is controversial.

Answer 36

Primary failure to respond to sulfonylureas occurs in 20%-25% of patients. Secondary failure occurs at a rate of approximately 10% - 15% per year due to progressive β-cell failure and insulin resistance or because of poor compliance.

Answer 37

100x more potent

Answer 38

All of the sulfonylureas are metabolized by the liver and the metabolites are excreted in the urine. These drugs should be administered with caution in patients with either renal or hepatic insufficiency.

Answer 39

recently diagnosed over 30 not overtly obese have residual B-cell function fasting blood glucose <300

Answer 40

30% - most often due to dietary noncompliance add metformin to regimen or treat with insulin Replacing one sulfonylurea agent with another sulfonylurea is unlikely to produce substantially different results and is not recommended.

Answer 41

hypoglycemia, including coma - most often in elderly with impaired hepatic or renal function - can mimic cerebrovascular accident - treat with glucose or glucagon Nausea, vomiting ``` Cholestatic jaundice Hyponatremia agranulocytosis aplastic anemia generalized hypersensitivity rxns ```

Answer 42

may enhance the action of sulfonylureas by causing hypoglycemia.

Answer 43

type I DM sulfa allergies pregnant or nursing mothers significant hepatic or renal insufficiency

Answer 44

non-sulfonylurea rapid acting insulin releasing agents includes Repaglinide and Nateglinide

Answer 45

Meglitinides binds to the ATP-sensitive potassium channel on pancreatic beta cells at a different site than sulfonylureas. The subsequent depolarization of the beta cell opens the calcium channel and rapidly increases insulin secretion. Thus, these drugs are sometimes called non-sulfonylurea secretagogues.

Answer 46

developed to manage meal related glucose loads The rapid action of these drugs (taken right before a meal) makes them useful for patients who are erratic eaters. For example, if a meal is skipped so is that dose of drug and hypoglycemia is avoided. Only the first phase of insulin secretion is stimulated because of the rapid metabolism of the drugs. monotherapy OR combined with metformin

Answer 47

Adverse effects are comparable to sulfonylureas but these drugs should be used cautiously in the elderly and those with liver dysfunction. They can cause hypoglycemia, must be taken three times a day (i.e., with meals), and are expensive

Answer 48

acarbose miglitol MOA: oligosaccharide analogs that bind to the intestinal brush border enzymes that digest complex sugars -competitive inhibition of sugar digestion by these drugs delays the absorption of carbohydrates and limits postprandial rise in glucose

Answer 49

newly diagnosed type II pt's with mild hyperglycemia used by themselves they do NOT cause hypoglycemia , if combined with insulin or sulfonylureas, these drugs increase the risk of hypoglycemia.

Answer 50

flatulence diarrhea GI upset due to undigested carbohydrates can lead to poor patient compliance

Answer 51

Diabetic ketoacidosis cirrhosis inflammatory bowel disease colonic ulcers partial intestinal obstruction

Answer 52

insulin sensitizers -Pioglitazone indicated as an adjunct to diet and exercise or for concomitant use with a sulfonylurea or insulin to improve glycemic control

Answer 53

bind to nuclear transcription factors that may be involved in the insulin receptor signaling cascade (PPAR-gamma site) resensitize tissues to insulin TZDs increase glucose uptake and glucose oxidation in both muscle and adipose tissue, while reducing hepatic glucose output and lipid synthesis in muscle and fat cells. Insulin release is not directly stimulated.

Answer 54

reduce insulin resistance improve peripheral action of insulin * reduce hyperglycemia by increasing glucose uptake (may increase insulin responsive genes and increase GLUT-1 and GLUT-4 transport proteins. * reduce hepatic glucose production * produce a small improvement in serum lipids, decrease triglycerides, FFA, increase HDL, in increase large “fluffy” LDL.

Answer 55

• When taken with insulin, allow reduction in insulin dose or facilitate discontinuation of insulin.

Answer 56

Current data suggest that liver toxicity may be less of a problem with these drugs. Pioglitazone may cause moderate weight gain, edema and mild anemia, all due at least partly to fluid retention. Fractures (particularly in women) - distal upper or lower limb Black box warning--> fluid retention with resultant CHF

Answer 57

amylin analog Amylin is a naturally occurring 37-amino acid peptide that is normally co-secreted with insulin from the pancreatic β-cells. Amylin secretion is delayed or diminished in both Type 1 and Type 2 diabetics. Pramlintide is a synthetic analog of amylin that has improved physical properties that make it more stable in solution, thus rendering it more suitable for mass production, storage, and use

Answer 58

* suppression of endogenous glucagon production, especially in the postprandial state. * reduction of postprandial hepatic glucose production. * reduction of gastric emptying time. * centrally-mediated induction of satiety * reduction of postprandial glucose levels

Answer 59

This agent is most useful for patients who experience wide glycemic swings or those who are insulin-resistant and require large amounts of insulin.

Answer 60

Pramlintide is delivered by subcutaneous injection before meals and cannot be mixed with insulin. Thus, use of pramlintide requires additional 2 to 3 injections per day. Adverse effects include increased risk of hypoglycemia and nausea. Other side effects include decreased appetite, vomiting, stomach pain, tiredness, dizziness, or indigestion.

Answer 61

* glucose-dependent enhancement of endogenous insulin secretion and perhaps insulin sensitivity. * inhibition of endogenous glucagon secretion. * possible appetite suppression and satiety induction. * reduction in speed of gastric emptying. * possible stimulation of islet growth, differentiation and regeneration. reduces HbA1 c levels, post prandial glucose, and weight

Answer 62

approved for use with metformin alone, a sulfonylurea alone, or in combination with metformin and a sulfonylurea

Answer 63

nausea, vomiting, diarrhea, upper resp symptoms incidents of hypoglycemia are low The biggest drawback is the need for additional twice-daily subcutaneous injections. POSSIBle pancreatitis

Answer 64

"gliptin's" block the enzyme that breaks down the two incretin hormones glucagon peptide like peptide 1 (GLP-1) and GIP which help regulate glucose metabolism via increased insulin release, suppressed glucagon release and delayed gastric emptying

Answer 65

the "flozins" SGLT2, a membrane protein expressed mainly in the kidney, transports filtered glucose from the proximal renal tubule into tubular epithelial cells. SGLT2 inhibitors decrease renal glucose reabsorption and increase urinary glucose excretion, resulting in a reduction in blood glucose levels. associated with genital infections and UTI's

Answer 66

phase 1 rapid rise and fall phase 2 slower, more gradual release

Answer 67

5-15 minutes degraded in the liver, degraded in the kidney

Answer 68

by facilitated diffusion by GLUT

Answer 69

in pancreas and liver

Answer 70

muscle and fat cells

Answer 71

inappropriate dose mismatch of time of injection versus food intake exercise induced glucose demand increase need for insulin

Answer 72

glucose | glucagon

Drugs- Insulin and oral hypoglycemic agents (Martin) Flashcards

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