Diabetes Meds Flashcards by Ashly Benson

Dx of DM

Fasting blood glucose >126 mg/dL
Non-fasting blood glucose >200 mg/dL
+ oral glucose tolerance test >200 mg/dL at 2-3 hours post bolus

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What testing should be done in non-obese adults who present with apparent type 2 diabetes?

Islet cell Ab
Insulin Ab
Glutamic acide decarboxylase Ab

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What drug inhibits glucose production by the LIVER and decreases insulin resistance?

Metformin

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What class of drugs increase secretion of insulin? What risk is associated with this?

Sulfonylureas and Meglitinides

Risk of hypoglycemia

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What drug class delays absorption of glucose by the INTESTINE?

Alpha-glucosidase inhibitor (doesn’t allow glucose to drop below 60)

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What class of drugs decreases insulin resistance?

Thiazolidinediones

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What promotes the release of insulin from the pancreas after a meal and what risk is associated with that?

DPP-4 inhibitors

Risk of hypoglycemia

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When might a patient be switched from oral DM medication to insulin?

During severe acute infections
Prior to an in-patient surgery for which the patient will be NPO (nothing per oral)
DM2 pts who become pregnant
Women who develop gestational DM

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What drug is a member of the Biguanide class of drugs?

Metformin (Glucophage) is the only member

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How does Metformin work?

Reduces hepatic glucose production.

Usually does not cause hypoglycemia.

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How are Metformin and the sulfonylureas (Glipizide/Glucotrol and Glyburide/Micronase) similar and different?

Similar: reduction of fasting serum glucose, non-fasting serum glucose and A1c levels.

Different: Metformin can cause weight loss.

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Metformin SE and risks

SE:

(1) MC abdominal cramping and nausea (reduced by using EX form)
(2) Metallic taste
(3) Lactic acidosis (rare/fatal)

Risk: B12 deficiency

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What population should’t be tx with Metformin?

Pt with impaired renal function/renal insufficiency

Serum creatinine >1.5 M >1.4 F

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How is Metformin dosed?

What is a general daily dose?

500, 850 or 1000 mg tab

Dosed 2x/day

Daily dose usually 1500-2000 mg

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What is the MOA of Sulfonylureas?

Stimulate intact beta cells of the PANCREAS to release more insulin.

Sulfonylurea interacts with ATP sensitive potassium channels in beta cell membrane. (Blocks K channel = Increased Ca release = more insulin release)

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What are the 2nd gen Sulfonylureas drugs?

Glipizide (Glucotrol)
Glyburide (Micronase, Diabeta)
Glimepiride (Amaryl)

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What is the most concerning adverse effect of Sulfonylureas?

Hypoglycemia (increased insulin release), esp in pts with impaired renal or hepatic function.

Weight gain is a common SE

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Are Sulfonylureas a long term tx for DM management?

No. They generally become ineffective at glucose control after 5-10 years of use.

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Who should not use the Sulfonylureas (Glipizide, Glyburidie, Glimepiride)?

Pt with sulfa drug allergies.

What is the MOA for the Meglitinides?

Stimulate beta cells to release insulin.

Also bind to ATP sensitive K channels on beta cells to increase insulin release. (Though structurally different from sulfonylureas)

What drugs are in the Meglitinide class?

NategLINIDE (Starlix) less effective

RepagLINDE (Prandin)

What are the SE of the Meglitinide class?

What drug class also has these SE?

Hypoglycemia and weight gain

Sulfonylureas

What drugs are the Meglitinide class commonly used with? avoided?

Combined use with Metformin or with a drug from the Glitazone class.

Avoid use with Sulfonylureas due to risk for hypoglycemia.

What is the dosing of Meglitinides and why?

3-4x/day: before each meal and if a meal is missed, the drug shouldn’t be taken.

Rapidly absorbed from the GI tract causing plasma insulin levels to peak within 30-60 minutes and rapidly cleared thereafter.

What is the MOA of Thiazolidinediones/Glitazones?

Improve insulin sensitivity in skeletal muscle cells, fat cells and liver cells. Decreases hepatic glucose production.

What risks are associated with the Thiazolidinediones/Glitazones?

Greater morbidity and mortality related to CV events. Increased risk of CHF. Increased risk of bladder CA. Reduced bone density. Increased risk of fracture. Weight gain. Especially controversial cardia events with Avandia.

What are the Thiazolidinediones/Glitazones?

Rosiglitazone (Avandia) Pioglitazone (ACTOS) Troglitazone (Rezulin)

What is the dosage for Glitazones? Char?

Once per day May take 6-14 weeks to achieve maximum effects. Avandia and ACTOS = monotherapy or in combination wtih Metformin or Sulfonylurea Only ACTOS is approved for use with Insulin.

How should pts on Glitazones be monitored?

LFT before tx, 1 month into tx and 3 months into tx. (look for rise in ALT)

What are the Alpha-glucosidase inhibitors and what are their MOA? Acarbose (Precose) Miglitol (Glyset)

Acarbose (Precose) Miglitol (Glyset) Inhibit the alpha-glucosidase enzymes that line the brush border of the sm. intestine, interfering with hydrolysis of carbohydrates and delaying absorption of glucose and other monosaccharides.

Alpha-glucosidase inhibitor dosage? Acarbose (Precose) Miglitol (Glyset)

Taken with each meal. Increased risk of hypoglycemia when taken with a Sulfonylurea or insulin.

Alpha-glucosidase inhibitor SE Acarbose (Precose) Miglitol (Glyset)

Abdominal pain Diarrhea Flatulence Due to osmotic effects and bacterial fermentation.

When taking Alpha-glucosidase inhibitors if hypoglycemia should occur, what must you tx with?

Glucose Alpha-glucosidase inhibitors interfere with breakdown of sucrose.

When are Alpha-glucosidase inhibitors CI? Acarbose (Precose) Miglitol (Glyset)

IBD Colonic ulceration Intestinal obstruction

What is the Dipeptidyl peptidase-4 (DPP-4) inhibitor and what is the MOA?

Sitagliptin/Januvia MOA: competitively inhibit the enzyme dipeptidyl peptidase 4 (DPP-4) which breaks down GLP-1 and GIP gastro hormones. GLP-1 and GIP potentiate secretion of insulin. By prohibiting their breakdown insulin secretion is potentiated and glucagon release by the pancreas is suppressed.

Sitagliptin/Januvia Positive SE Neg SE

Sitaglipitn/Januvia Positive SE: as blood glucose levels approach normal drug's effects diminish preventing hypoglycemia. Negative SE: Pancreatitis

Sitagliptin/Januvia Use

Sitagliptin/Januvia Monotherapy for DM2 or Combination therapy with Metformin, Sulfonylurea or TZD but NOT WITH INSULIN

Sitagliptin/Januvia Dose

25, 50, 100 mg tabs Typical dose is 100 mg once daily. Expensive $2-400/month

Pramlintide and Exenatide are new injectable drugs for DM1 and DM2. What are they?

Pramlintide: synthetic form of hormone amylin : produced with insulin by beta cells. Exenatide: synthetic version of exendin-4, a naturally occurring hormone isolated from the saliva of the Gila monster.

What is a common indication for Pramlintide/Symlin?

DM1 and DM2 pts on insulin who cannot reach goal level HgbA1c. *Insulin and Pramlintide cannot be combined in the same vial*

Pramlintide/Symlin pros and SE

Improve A1c levels w/o causing increased hypoglycemia or causing weight gain. May promote modest weight loss. SE: nausea

``` Insulin Rapid: Onset Peak Duration ```

Insulin Rapid: Onset

``` Insulin Short: Onset Peak Duration ```

``` Insulin Short: Onset .5-1 Peak 2-4 Duration 4-12 ```

``` Insulin Intermediate Onset Peak Duration ```

``` Insulin Intermediate Onset 1-3 Peak 6-10 Duration 10-18 ```

``` Insulin Long acting Onset Peak Duration ```

``` Insulin Long acting Onset 4-6 Peak "flat" Duration 24 ```