Endocrine: Diabetes Pharmacology

Three rapid acting insulin drugs
Lispro
Aspart
Glulisine

“Rapid drugs don’t LAG”

“Rapid drugs don’t LAG”
Mnemonic to remember the rapid acting insulin drugs:
Lispro
Aspart
Glulisine

Intermediate acting insulin drug
NPH

Long-acting insulin drugs
Glargine
Detemir

“Determined to act Glarge”

“Determined to Act Glarge”
Mnemonic to remember the long acting insulin drugs:
Glargine
Detemir

Clinical use for insulin drugs
T1DM
T2DM
Gestational diabetes
Life threatening hyperkalemia (K+ shift)
Stress induced hyperglycemia

Treatment for life-threatening hyperkalemia
Insulin

Name one biguanide drug
Metformin

Effects of metformin (biguanide)
Decrease GNG
Increase glycolysis
Increase peripheral glucose uptake (insulin sensitivity)

Two parts of T1DM treatment strategy
1. Low sugar diet
2. Insulin replacement
*T1DM patients must ALWAYS be on insulin

Three parts of treatment for T2DM
1. Dietary modification and weight loss
2. Oral hypoglycemic
3. Insulin replacement

First-line therapy for T2DM
Metformin (biguanide) – can be used in patients without islet function

What patients is metformin contraindicated in?
Renal failure patients (do not use in patienits with creatinine > 1.5 or with IV contrast because of renal injury)

Adverse affect of metformin
Lactic acidosis = can worsen renal failure

Name two first generation sulfonylureas
Tobutamine
Chlorpropamide

Name three second generation sulfonylureas
Glyburide
Glimepiride
Glipizide

Mechanism of sulfonylureas
Close K+ channel in beta-cell membrane so cell depolarizes = insulin release via Ca2+ influx

Name the drug: decreases GNG, increase glycogenolysis, increases peripheral glucose uptake
Metformin (biguanide)

Name the drug: Closes K+ channels which cause beta-cell depolarization and calcium influx and thus release of insulin granules
Sulfonylureas
First generation: Tolbutamide, Chlorpropamine
Second generation: Glyburide, Glimepiride, Glipizide

Why are sulfonylureas useless in T1DM patients?
Because they act on beta-islet cells by closing K+-ATP sensing channels; and in T1DM there are no functional islet cells left

Clinical use for sulfonylureas
Stimulate endogenous insulin release for T2DM patients (not used for T1DM because requires functional beta-islet cells)

Adverse effects of sulfonylureas
1st generation (tolbutamide, chlorpropamide) = disulfiram reaction
2nd generation = long-lasting hypoglycemia

Side effect of glyburide, glimepiride and glyburide
2nd generation sulfonyl ureas = long-lasting hypoglycemia

Name the drugs: Adverse effect includes long-lasting hypoglycemia
2nd generation sulfonlyureas = glyburide, glipizide, glimepiride

Name the drugs: Cause disulfuram like reaction
1st Generation sulfonylureas = tolbutamide, chlorpropamide

Name two glitazones/thiazolidinediones
Pioglitazone
Rosiglitazone

Mechanism of glitazones/thiazolidinediones
Pioglitazone, rosiglitazone = increase insulin SENSITIVITY in peripheral tissue by binding PPAR-gamma nuclear TF

What is PPAR-gamma and what effects does it have?
PPAR-gamma = nuclear TF which upregulates genes that increase FA storage and glucose metabolism

Clinical use for glitazones/thiazolidinediones
Monotherapy or combined therapy in T2DM

Name the drug: Bind and activate PPAR-gamma
Glitazones/Thiazolidinediones = Rosiglitazone, pioglitazone

Adverse effects of glitazones/thiazolidinediones
Weight gain
Edema
Hepatotoxicity
Heart failure

What diabetic drug should not be used in CHF patients?
Glitazones/thiazolidinedeiones = pioglitazone, rosiglitazones can cause:
1. Weight gain
2. Edema
3. Hepatoxicity
4. HEART FAILURE

Name the drug: Associated with causing heart failure
glitazones/thiazolidinediones

Name two alpha-glucosidase inhibitors
Acarbose
Miglitol

“Miglit Can’t eat CARBS”

“Miglit Can’t eat carbs”
Mnemonic to remember the two alpha-glucosidase inhibitors:
1. Miglitol
2. Acarbose

Mechanism of alpha-glucosidase inhibitors
Miglitol and acarbose work by inhibiting intestinal brush-border alpha-glucosidases (hydrolase that breaks down sugars) = so decreased glucose absorption after eating

Clinical use for miglitol and acarbose
Miglitol and acarbose are alpha-glucosidase inhibitors:
Use as monotherapy or in combination therapy for T2DM

Name the drug: Can cause GI disturbance
Alpha-glucosidase inhibitors = miglitol and acarbose

Name an amylin analog
Pramlintide

Mechanism of pramlintide (amylin analog)
Decreases glucagon

Diabetic drugs indicated only for T2DM
Sulfonylureas (require functional beta cells)
Glitazones/thiazolidinedeiones
Alpha-glucosidase inhibitors
GLP-1 analogs
DPP-4 inhibitors
Insulins

Diabetic drugs that can be used in T1DM
Insulins
Biguanides (metformin)
Amylin analogs (pramlintide)

Name two GLP-1 analogs
Exenatide
Liraglutide

Mechanism of exenatidem and liraglutide
Decrease glucagon secretion
Increase insulin secretion

Clnical indications for GLP-1 analogs (exenatide, liraglutide)
T2DM

Indications for amylin analogs
T1DM and T2DM

Difference between GLP-1 analogs and amylin analogs
Amylin (pramlintide) = decrease glucagon; T1DM and T2DM
GLP-1 (exenatide, liraglutide) = decrease glucagon AND increase insulin; T2DM online

Name two DPP-4 inhibitors
Linagliptin
Saxagliptin
Sitagliptin

What class of drugs are the “-gliptins”
DPP-4 analogs = Linagliptin, saxagliptin, sitagliptin

What class of drugs are the “-tides”
Amylin analogs = pramlintide
GLP-1 analogs = exenatide, liraglutide

What class of drugs are the “-amides”
1st generation sulfonylureas = Tolbutamide, chloropropamide

Mechanism of DPP-4 inhibitors
Linagliptin, saxagliptin and sitagliptin =
Increase insulin
decrease glucagon release

Name the drug: increase insulin release and decrease glucagon release
GLP-1 analogs = extenatide or liraglutide
DPP-4 inhibitors = linagliptin, saxagliptin, sitagliptin

Adverse effect of GLP-1 analog
Pancreatitis

Name the drug: can cause pancreatitis
GLP-1 analogs = exenatide, liraglutide

Name the drug: adverse effect includes mild urinary and respiratory infections
DPP-4 inhibitors

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Overview of diabetes mellitus often called DM. disorder of carbohydrates metabolism. CHO also affects protein and lipids. Type 1 diabetes. 10% of population- pancreatic beta cells are destroyed and cannot make insulin. WE WILL WRITE A CUSTOM ESSAY SAMPLE ON …

Current medications: Avandia (rosiglitazone) 2mg BID Glucophage (metformin) 500mg OD Lasix (furosemide) 40 mg daily Potassium supplements (KCl) 20 meq daily Lopressor (metoprolol) 25 mg BID Prinivil (lisinopril) 5 mg daily Allopurinol (zyloprim) 100mg daily Advair 1 inhalation BID He …

type 2 diabetes mellitus condition where there is an inadequate amount of insulin to meet daily requirements insulin is released in the body in response to the ingestion of carbohydrates WE WILL WRITE A CUSTOM ESSAY SAMPLE ON ANY TOPIC …

* Difference in Somatic and Autonomic Nervous System * The somatic nervous system consists of nerves that provide VOLUNTARY control over skeletal muscles * The autonomic nervous system exerts INVOLUNTARY control over the contraction of smooth muscle, cardiac muscle, and …

Physiologic Action of Insulin – Promotes entry of glucose into cells – Provides for the storage of glucose, as glycogen – Inhibits the breakdown of fat and glycogen – Increases protein synthesis and inhibits gluconeogenesis (production of “new” glucose from …

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