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Pharmacology II > Insulin and controlling blood glucose > Flashcards

Insulin and controlling blood glucose Flashcards

1
Q

Describe insulin and its role in metabolism

A

Physiologic role is nutrient metabolism

Made in pancreatic B-cells as pro-insulin

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2
Q

What is insulin’s mechanism of action?

A

Interacts with insulin receptors on cell membranes associated with tyrosine kinase.
Activation then leads to phosphorylation and activation og GTP binding proteins
Finally get transcription factors to be stimulated, affecting gene regulation
See metabolic effects with increasing glucose transport and glycogen synthetase

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3
Q

In diabetes mellitus, what is the difference between an absolute lack of insulin and just a lack of insulin?

A

Lack of insulin, is just that, not enough insulin

Absolute lack of insulin is the lack of beta cells

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4
Q

Describe type 1 Diabetes

A

Insulin dependent diabetes mellitus; apparent lack of insulin/decreased insulin sensitivity
Unrelated to diet/exercise.
Treated with insulin for a life time

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5
Q

Describe type 2 Diabetes

A

Non-insulin dependent diabetes mellitus

Treated with oral agents and possibly can resolve with diet/exercise

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6
Q

Can you inject human insulin?

A

Yes, cannot be absorbed and must be injected

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7
Q

What is the difference between the insulin preparations?

A

Duration of action

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8
Q

What are the insulin preparations?

A

Regular insulin - Humulin/Humalog - Short acting
Isophane insulin suspension - Humulin N/Novolin N; intermediate (18-24 hours)
Insulin glargine - Lantus

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9
Q

What are some toxicites with insulin and insulin preparations?

A

Hypoglycemia/Insulin Shock
CV symptoms - tachycardia, pallor, sweating
CNS symptoms - Tremor, nervousness, unrest, convulsions
Coma/death if not treated with glucose
Allergic hypersensitivity
Insulin resistance (but rare with use of human insulin)

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10
Q

Oral agents for controlling blood glucose require the patient to have something to work

A

Working beta cells

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11
Q

Is it type 1 or type 2 diabetes that tends to develop at 35?

A

Type 2; probably due to decreased sensitivity for insulin receptors/decreased efficiency of signal transduction of insulin-receptor complexes

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12
Q

People with type 2 diabetes can control their glucose through diet and exercise, true or false?

A

True

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13
Q

What is the general method of action for oral hypoglycemics?

A

Work to increase release of insulin from any remaining active beta cells instead of being an insulin replacement

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14
Q

Describe the sulfonylurea drugs

A

Bind to ATP dependent K channel to decrease K efflux, increase Ca++ influx, causing greater insulin upon stimulated release
Also cause increased sensitivity in peripheral tissues to insulin, more glucose uptake

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15
Q

Name the first and second generation sulfonylurea drugs

A 
Tolbutamide (Orinase)
Second generation:
	Glipizide (Glucotrol)
	Glyburide (Micronase)
	Glimepiride (Ammaryl)
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16
Q

What are toxicities of sulfoonyrea drugs?

A 
Profound hypoglycemia possible
Nausea
Rash
Blood disorders
Jaundice
Muscle weakness and ataxia
Dizziness and mental confusion
Allergic sensitivity to sulfa drugs
17
Q

How do secretagogues work?

A

Like sulfonyruleas, stimulating insulin from functioning beta cells.

18
Q

Describe secretagogues drugs

A

Short duration of action, use pre-prandial before eating

Can cause hypoglycemia (less than sulfyonureleas), nausea, dyspepsia, diarrhea

19
Q

Describe sulfa interactions with secretagogue drugs

A

Not possible

20
Q

Name the secretagogue drugs

A

Repaglinide (Prandin)

Nateglinide (Starlix)

21
Q

What drug classifications are considered to be antihyperglycemic?

A 
Biguanides
Alpha-glucosidase inhibitors
Thiazolidinediones
"Incretin mimicking"
"Gliptins"
22
Q

What drug is considered to be an oral biguanide?

A

Metformin (Glucophage)

23
Q

Describe the method of action for metformin

A

May decrease glucose output from liver (gluconeogenesis), increasing insulin action on muscle and fat to uptake into cell.

24
Q

What is the major toxicity seen with metformin?

A

Significant increase in lactic acidosis, can be fatal in those with renal insufficiency
Rarely see megaloblastic anemia
Commonly see diarrhea, nausea or other GIT symptoms

25
Q

What are the alpha glucosidsae inhibitors?

A

Acarbose (Glucobay)

Miglitol (Glyset)

26
Q

What is the mechanism of action for alpha-glucosidsae inhibitors?

A

Inhibition of enzymes that breakdown complex carbohydrates and delay/reduce absorption of monosaccharides

27
Q

What are the common toxicities with alpha glucosidase inhibitors?

A

Frequent GI disturbances, diarrhea, pain and gas

28
Q

How do Thiazolidinedione drugs work?

A

Increasing sensitivity of insulin receptors

29
Q

What is the method of action for thiazolidinedione drugs?

A

Believed to act on peroxisome proliferator activated receptors (PPAR) to increase gene transcription
Leads to increased uptake and utilization of glucose by tissues
(More glut-4 to transport, lipoprotein lipase to free glucose, fatty acid transporters and others)

30
Q

What drugs are thiazolidinedione drugs?

A

Rosiglitazone (Avandia)

Pioglitazone (Actos)

31
Q

What are common toxicities of thiazolidinedione drugs?

A

Weight gain/fluid retention

Infrequently can see hepatotoxicity, congestive heart failure, possible increased risk of CV events

32
Q

What is the method of action for Liraglutide and Exenatide?

A

Glucagon like peptide1 receptor agonist (GLP-1) that inhibits glucagon secretion, increasing insulin and delays gastric emptying; more incretin in the system

33
Q

What are common toxicities for Liraglutide and Exenatide?

A

Nausea, diarrhea and vomiting

Serious but uncommon: pancreatitis, thyroid carcinoma (liraglutide), anaphylactic reactions (exenatide)

34
Q

What are is the method of action of the ‘gliptins’?

A

Act as dipeptidyl peptidase 4 inhibitors (DPP-4) blocking breakdown of GLP-1
Acts to increase duration of incretin and see insulin release and inhibit glucagon release

35
Q

What drugs are ‘gliptins’?

A

Sitagliptin (Januvia)
Saxagliptin (Onglyza)
Linagliptin (Tradgenta)

36
Q

What toxicities are common with the ‘gliptins’?

A

Upper respiratory tract infection
Nasopharyngitis
Headache
Serious toxicities include - Pancreatitis or hypersensitivity

37
Q

What are the newest generation of glucose controlling medications method of action?

A

Inhibition of type 2 sodium-glucose transporters (SGLT2), prevents reabsorption of glucose from kidneys, keeps blood glucose low

Pharmacology II (10 decks)

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