Diabetes PPT 6 Flashcards by Kiley Galindo

What is GLP-1 derived from?

Gila monster saliva

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Which form of GLP-1 is not injectable?

Semaglutide (rybelus)

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What is glycogenolysis?

Process which glycogen is metabolized into glucose, one of the main mechanisms by which the body produces endogenous glucose

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What is the incretin effect?

Oral glucose stimulates greater insulin production than IV glucose

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What are incretins?

They are gut derived peptides that are secreted in response to meals

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Mechanism of action of GLP-1

-stimulus glucose dependent insulin secretion
- suppressed post radial glycogen secretion
- slows gastric emptying
- inhibits food intake

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What are the two predominant incretin hormones

Glucose dependent insulinotropic polypeptide, also known as gastric inhibitory polypeptide
Glucagon like peptide 1 (GLP-1)

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What does GLP-1 do?

Enhances glucose dependent insulin secretion that results from oral
Suppressed inappropriate glucagon secretion
Promotes satiety, regulates rate of gastric emptying
Increased beta cell survival

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What does GIP do?

Sympathized and released by the K cells
Binds to receptors on the beta cells and adupoctyes
Enhanced insulin secretion
Increased beta cell survival
Increased uptake of fatty acid’s
No effect on
- glucagon
Gastric emptying
First approved with GLP-1

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Exanatide - short acting (Byetta, Bydureon) PD

Stimulates insulin production
Glucagon suppression
Enhanced safety
Slowed gastric emptying

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PK of exanatide

Absorbed equally from arm, abd, thigh
Peak concentration is 2 hours
Duration of action up to 10 hours
Excreted by kidneys
Dosage adjustment if CrCl is less and 30

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Indication of GLP-1

Monotherapy
Combination with sulfonylureas, metformin, TZDs or insulin

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Contraindications of GLP-1

Hypersensitivity to the drug or components
Type 1 DM
Treatment of diabetic ketoacodosis
Gastroparesis
Reglan use
Pancreatitis
History of thyroid cancer

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Cautions of exenatide

Not recommended in end stage renal disease or severe renal improvement
Hypoglycemia when used with a sulfonylurea
Possible long term consequences: induction of autoimmunity

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Adverse effects of exenatide

Nausea, hypoglycemia, vomiting, diarrhea, jitteriness, dizziness, headache and dyspepsia

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How does exenatide need to be administered?

5mcg BID titrate to 10 and only subq within 60 minutes prior to morning and evening meals

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Mechanism of action of DPP-4

Block the action of DPP4, that increase circulating GIP AND GLP1 levels which ultimately decreases Prost radial glucose excursions

What are the 4 DPP4 inhibitors

Sitagliptin
Saxagliptin
Linagliptin
Alogliptin

What is Sitagliptin

First DDP4 to be available
Oral, given mono or in combo with metformin, SFUs, or TZDs
Excreted in urine 87%
Low plasma protein binding, high volume of distribution
Half life is 12 hours

Dose implication of sitagliptins

Dose 100 mg daily for adults
Use in causation in geriatrics due to possible renal impairment
Pregnancy category B

Contraindications of Sitagliptin

Type one diabetes, diabetic, ketoacidosis, caution, and renal function, impairment, caution of history of pancreatitis when used with insulin (sulfonylurea) may need to lower dose of these drugs to reduce risk of hypoglycemia

Adverse reactions of Sitagliptin

Hypersensitivity reactions more common upper respiratory infection, headache abdominal pain arthralgia

What is Saxagliptin

For type 2 diabetes
Monotherapy / add on combination with metformin, sulfonylureas or TZDs

Dosing implications of Saxagliptin

2.5 mg and 5 mg tablets, max dose 5 mg a day Dose once daily No adjustment for CrCl No issues with geriatric

What does Saxagliptin interact with?

CYP 450 enzymes

Contraindications to Saxagliptin

Type 1 diabetes Diabetic keyoacidosis Caution in renal impairment

What is Linagliptin

Indicated for Type 2 diabetes Monotherapy / add on combination with metformin, sulfnylureas or TZDs

Dosing implications of Linagliptin

5 mg tabs once daily No dosing adjustment if CrCl is above 50 No safety issues in geriatric

Drug interactions of Linagliptin

Weak/moderate inhibitor CYP 3A4 Interactions: Rifampin Carbamazepine Phenytoin St. John’s wart

Adverse effects of Linagliptin

Hypoglycemia hypersensitivity, upper respiratory tract infection, headache, myalgia, no observed effect on renal function

Advantages of Alogliptin

It is more widely distributed than the other agents, and it has a longest half-life

What are the GLP-1 Mimetic drugs?

Liraglutide Dulaglutide Semaglutide Semaglutide (Rybelsus) - oral

What is the mechanism of actions of GLP-1 agonist?

Mimic GLP-1, enhancing insulin secretion and reducing glucagon release

What is the route of administration of GLP-1 Agonists?

Subq injection (daily or weekly)

What is the incretin effect?

It refers to the phenomenon in which oral glucose induces a greater insulin secretion compared to intravenous glucose when administer in equal amounts

What are the 2 predominant incretin hormones?

Gastric inhibitory polypeptide (GIP) and Glucagon like peptide 1 (GLP-1)

What enzyme inactivates GIP and GLP-1?

DPP4

What are the contraindications of GLP-1 receptor agonists?

Thyroid cancer and multiple endocrine neoplasia syndrome T2 (MEN 2)

What is a long term consequence of GLP-1?

Autoimmunity

What are the DPP-4 Inhibitor drugs?

Sitagliptin Saxagliptin Linagliptin Alogliptin

Which two GLP-1 receptor agonists are contraindicated for eGFR < 30?

Byetta and Bydureon