Endocrine Deck 2 Flashcards by Nathan Koranda

Biguanides

metformin (glucophage, glucophage XR)

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Metformin glucose

Decreases glucose production in liver, decreases GI glucose absorption, and improves insulin sensitivity by increasing peripheral glucose uptake and utilization
Does not stimulate insulin release for beta cells
Inhibits platelet aggregation and reduces blood viscosity

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Biguanide patients may

loose weight. mostly weight neutral

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Biguanide pharmacokinetics

Absorption: 50% to 60% after oral dosing; food decreases and delays absorption
Metabolism: no hepatic metabolism
Excreted by kidneys
Alcohol potentiates drug’s effect on lactate metabolism

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Metformin is different than sulfonera because it does not

stimulate insulin release from beta cells.

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Biguanides

Precautions and contraindications

Renal and hepatic disease

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Biguanides withold

drug 48 hours before and after procedures involving iodine-based contrast mediums.

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Biguanides watch

patients with vitamin B12 anemia/deficiency.

Biguanides are not recommended for children younger than 10 years of age.

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Biguanides

ADRs 
Metabolic (lactic acid) acidosis risk!
Lactic acidosis is rare, except in dehydration episodes.
Renal disease: Watch patients at risk for metabolic acidosis.
Liver disease: risk for lactic acidosis is increased.

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GI ADRs usually resolve

in 2 weeks after starting dose

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Biguanides rational drug slection

immediate release vs extended release
Type 2 DM: start with 500 mg twice/day and titrate up
If patients have not responded to 4 weeks of high dosing, consider adding oral sulfonylurea or other medication.

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Biguanides monitoring

assess renal function, ketones, HbA1C before starting dosing; check every 6 months. Patient education
Administration
ADRs: report diarrhea lasting more than 2 days, dehydration
Lifestyle management
Usually not the source of any hypoglycemia
Alert imaging staff about drug presence

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Alpha-Glucosidase Inhibitors examples

Acarbose (Precose), miglitol (Glyset)

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Alpha-Glucosidase Inhibitors

Pharmacodynamics

Inhibit the absorption of carbohydrate from GI tract, lowering the BG levels after meals

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Alpha-Glucosidase Inhibitors are not

monotherapy drugs

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Alpha-Glucosidase Inhibitors hypoglycemia treatment

Hypoglycemia treated with dextrose (honey, corn syrup), not sucrose

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Alpha-Glucosidase Inhibitors pharmacokinetics

Absorption: less than 2% of acarbose absorbed as active drug
Metabolized by intestinal bacteria and digestive enzymes (lots of gas production!)
Excreted by kidneys

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Alpha-Glucosidase Inhibitors Precautions and contraindications

Should not be used in patients with inflammatory bowel disease, or in those at risk for bowel obstruction or renal impairment
Should not be used during pregnancy
Not to be used in pediatric population

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Alpha-Glucosidase Inhibitors ADR

GI symptoms: flatulence, diarrhea, abdominal pain

Do not cause hypoglycemia

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Alpha-Glucosidase Inhibitors Drug interactions

Acarbose: digoxin
Miglitol: propranolol, ranitidine

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Alpha-Glucosidase Inhibitors

Clinical use and dosing

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Initial dose is 25 mg 3 times per day.

Increase dose in 4 to 8 week intervals.

Alpha-Glucosidase Inhibitors

Patient education

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Administration: should be taken with first bite of meal
ADRs: GI
Lifestyle: type 2 DM care

Thiazolidinediones examples

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Pioglitazone (Actos), rosiglitazone (Avandia)

Thiazolidinediones

Pharmacodynamics

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Improve target cell response to insulin by activating receptor cell proteins that improve insulin action
Increase utilization of insulin by liver and muscle cells and reduce liver glucose production

Thiazolidinediones | Pharmacokinetics

Absorption: rapid after oral dosing Metabolism: liver via CYP2C8 and 3A4 to both active and inactive metabolites; substrate inhibits CYP2C8, CYP2D6, induces weakly CYP3A4 Greater than 99% protein bound Excretion: in urine (15% to 30%) and feces as metabolites

Thiazolidinediones Precautions and contraindications

Chronic liver disease (heavy liver processing) Fluid retention: exacerbates heart failure (HF) FDA loosening restrictions, but still dangerous drug Not approved for children younger than age 18 years.

Thiazolidinediones | ADRs

cardiovascular (CV) – edema, upper respiratory infection, headache, fatigue Watch for signs of congestive heart failure (CHF), use with caution with patients with elevated liver enzymes Increased risk of bladder cancer with pioglitazone use

Thiazolidinediones | Drug interactions

Birth control requiring higher dosing of oral contraceptives Watch for drugs metabolized by CYP3A4: Coricidin, corticosteroids, ketoconazole

Thiazolidinediones | Monitoring:

liver enzymes at start of therapy, HgA1C

Rational drug selection | Thiazolidinediones

Careful selection of patient population Monotherapy or combination with sulfonylureas, insulin Initial dosing: 15 to 30 mg/day; maximum dosing: 45 mg/day Strong recommendation for endocrine co-management

Thiazolidinediones Patient education: once-daily dosing

Administration, ADRs, lifestyle management

Meglitinides examples

Nateglinide (Starlix), repaglinide (Prandin)

Meglitinides increase

insulin release from beta cells by closing potassium channels, which leads to the opening of calcium channels, and it is the influx of calcium that releases the insulin. Time in plasma is short, less than 2 hours, so these agents only lower postprandial BG levels.

Meglitinides precautions and contraindications

Precautions and contraindications Liver impairment Not approved in pediatric population

Meglitinide ADR

Hypoglycemia in vulnerable populations

Meglitinides | Drug interactions

CYP3A4 and CYP2C9 inducers increase meglitinide metabolism. | Antifungals (ketoconazole) and antimicrobials (erythromycin) inhibit metabolism, increasing risk for hypoglycemia.

Meglitinides | Rational drug selection: repaglinide

**For patients with postprandial hyperglycemia

Meglitinides | Monitoring and patient education

get baseline HbA1C, and recheck in 3 months Patient education Administration: no more than 30 minutes before a meal; hold if not eating ADRs Lifestyle management

DPP-4 Inhibitors known as

"Gliptins” | Sitagliptin (Januvia) and saxagliptin (Onglyza)

DPP-4 Inhibitors | Pharmacodynamics

Inhibits DPP-4 Breaks down GLP-1 and gastric inhibitory polypeptide, which are released in response to a meal Leads to increase in the secretion of insulin and suppresses the release of glucagon by the pancreas Promotes pre- and postprandial glucose levels Promotes mild weight loss in obese patients with diabetes

DPP-4 Inhibitors Precautions and contraindications

Renal dysfunction Pregnancy (check with obstetrician for necessity) Not approved in children

DPP-4 Inhibitors you will see a side effect of

weight loss in obese patients

DPP-4 Inhibitors ADR

ADRs: GI, headache

Precautions and contraindications | DPP-4 Inhibitors

Renal dysfunction Pregnancy (check with obstetrician for necessity) Not approved in children

DPP-4 Inhibitors | Drug interactions

Angiotensin-converting enzyme inhibitors: increased risk of angioedema

Monotherapy or in combination with other antidiabetic drugs

DPP-4 Inhibitors | Rational drug selection

Age: well-tolerated by older adults Weight/obesity: patients may lose weight Cost: more expensive than older drug families

DPP-4 Inhibitors | Monitoring

Renal function at baseline and annually | HbA1C every 3 months

DPP-4 Inhibitors | Patient education

Administration: taken once daily in the morning ADRs: well-tolerated Lifestyle: changes still needed

DPP-4 Inhibitors | Monitor for potential

thyroid medullary cancer concerns, especially in those with previous nodules

Endocrine Deck 2 Flashcards

(50 cards)