Lecture 91 - Pancreatic Hormones & Anti_DM Drugs Flashcards

1
Q

Insulin binds to its receptor — then what happens?

A
Insulin binds to alpha subunit 
Beta - tyrosine kinase domain 
Forms Tetramer; auto-phosph of Beta Domains 
Phosphorylation cascade 
Effects: 
	GLUT 4 Channel inserted in cell membrane  -- increased glucose uptake 
increased protein synthesis
increased TG storage 

Insulin Receptor is internalized and degraded

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2
Q

treatment regimen for T1DM

A

insulin analogs

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3
Q

what are the fast acting insulin analogs

what are the longer acting insulin analogs

A

Ultra short Acting - - Lispro, Aspart, Glulisine -

Long Acting
Glargine –
Detemir

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4
Q

complications of insulin analog use

A

hypoglycemia –
Insulin allergy – (eg if from pork)

lipodystrophy at injection site

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5
Q

what are the sulfonylureas

Mechanism of Sulfonylurea

A

Glimepiride, Glipizide, Glyburide

blocks the K+ channel in beta cells; depolarization; VGCC –> Insulin secretion

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6
Q

what is the sulfa-moeity free version of sulfonylureas

how else does it differ?

A

Sulfa Free= Meglitinides- Repaglinide (Prandin):

Weaker affinity and dissociates quickly

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7
Q

side effects of Sulfonylrurea

A

hypoglycemia

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8
Q

what classes of drugs are considered “hypoglycemic”,

which are “anti-hyperglycemia”

A

hypoglycemic – Insulin analogs and sulfonyl ureas – will drive down serum glucose no matter what

Metformin (Biguanides) – antihypergylcemic – drops blood glucose only in the setting of hyperglycemia

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9
Q

effects of metformin

A

Increased glycolysis;
Increased insulin sensitivity; reduces insulin resistance;

reduced GNG in the Liver;

Lowing of Glucose absorption in the Gut.

lowers Glucagon levels

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10
Q

side effects of metformin

contraindications:

other indications:

A

N/V/D/pain; anorexia

contra: renal, hepatic disease, alcoholism,

other indications: Insulin resistance in obese patients, PCOS, Prevention of DM in pre-DM, Getastational DM

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11
Q

name 2 Thiazolidinediones (TZD)

mechanism

A

Pioglitzone, Rosiglitazone

Mechanism: binds to PPAR-gamma nuclear transcription regulator
Genes involved with glucose and lipid metabolism

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12
Q

side effects and more serious complication of TZD use that has gotten in banned in Europe

A

Side effects: weight gain, edema, hepatotoxicity (P450s/drug interactions)

Bladder Cancer

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13
Q

alpha glucosidase inhibitors:

name 2

mechansim

A

Acarbose and miglitol –

Competitive Inhibition of Intestinal Alpha Glucosidase; therefore not breaking down starches to monosaccharides, therefore cannot absorp

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14
Q

side effect of glucosidase inhibitors

if pt becomes hypoglycemic on TZDs, how do you manage it?

A

Flatulence, Diarrhea, Abd pain

If patient is taking these drugs and have hypoglycemic episode; have to give monosaccharrides

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15
Q

Incretin based therapies can only be used in ___DM

A

t2DM bc they require pre-existing insulin

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16
Q

GLP1 Receptor Antagonist

name 2
mechanism
effects

A

Mechanism: Synthetic Analogs of GLP 1

Exanatide, Liraglutide

Increase Insulin; decrease Glucagon

glucose control and weight loss

17
Q

DPP4 Inhibition

name 3
mechanism

A

Sitagliptin, Vildagliptin, Saxagliptin

Inhibit degradation of Incretin Hormines

18
Q

SGTL2 Inhibition

name 2

mechaism

effects/side effects

contraindications

A

Canagliflozin. Farxiga,. Invoka

Mechanism: Block Glucose reabsorption in the Kidney (PCT)

		Effect: increased glucose excretion; osmotic diuresis; 

		Side effects: Diuresis, Dehydration, Weight Loss; 

contra: ERSD, CVD, Dialysis

19
Q

glucagon is secreted from___ cells of the pancreas and cause____

A

alpha cells

Increases Blood glucose at expense of hepatic glycogen stores

20
Q

clinical use of glucagon

A

Endocrine Dx – test beta cell effiency

beta blocker poisoning

Severe hypogylcemia if glucose not available