Endocrine Deck 2 Flashcards

1
Q

Biguanides

A

metformin (glucophage, glucophage XR)

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2
Q

Metformin glucose

A

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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3
Q

Biguanide patients may

A

loose weight. mostly weight neutral

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4
Q

Biguanide pharmacokinetics

A

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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5
Q

Metformin is different than sulfonera because it does not

A

stimulate insulin release from beta cells.

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6
Q

Biguanides

Precautions and contraindications

A

Renal and hepatic disease

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7
Q

Biguanides withold

A

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

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8
Q

Biguanides watch

A

patients with vitamin B12 anemia/deficiency.

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

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9
Q

Biguanides

A
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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10
Q

GI ADRs usually resolve

A

in 2 weeks after starting dose

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11
Q

Biguanides rational drug slection

A

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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12
Q

Biguanides monitoring

A

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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13
Q

Alpha-Glucosidase Inhibitors examples

A

Acarbose (Precose), miglitol (Glyset)

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14
Q

Alpha-Glucosidase Inhibitors

Pharmacodynamics

A

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

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15
Q

Alpha-Glucosidase Inhibitors are not

A

monotherapy drugs

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16
Q

Alpha-Glucosidase Inhibitors hypoglycemia treatment

A

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

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17
Q

Alpha-Glucosidase Inhibitors pharmacokinetics

A

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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18
Q

Alpha-Glucosidase Inhibitors Precautions and contraindications

A

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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19
Q

Alpha-Glucosidase Inhibitors ADR

A

GI symptoms: flatulence, diarrhea, abdominal pain

Do not cause hypoglycemia

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20
Q

Alpha-Glucosidase Inhibitors Drug interactions

A

Acarbose: digoxin
Miglitol: propranolol, ranitidine

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21
Q

Alpha-Glucosidase Inhibitors

Clinical use and dosing

A

Initial dose is 25 mg 3 times per day.

Increase dose in 4 to 8 week intervals.

22
Q

Alpha-Glucosidase Inhibitors

Patient education

A

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

23
Q

Thiazolidinediones examples

A

Pioglitazone (Actos), rosiglitazone (Avandia)

24
Q

Thiazolidinediones

Pharmacodynamics

A

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

25
Q

Thiazolidinediones

Pharmacokinetics

A

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

26
Q

Thiazolidinediones Precautions and contraindications

A

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.

27
Q

Thiazolidinediones

ADRs

A

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

28
Q

Thiazolidinediones

Drug interactions

A

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

29
Q

Thiazolidinediones

Monitoring:

A

liver enzymes at start of therapy, HgA1C

30
Q

Rational drug selection

Thiazolidinediones

A

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

31
Q

Thiazolidinediones Patient education: once-daily dosing

A

Administration, ADRs, lifestyle management

32
Q

Meglitinides examples

A

Nateglinide (Starlix), repaglinide (Prandin)

33
Q

Meglitinides increase

A

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.

34
Q

Meglitinides precautions and contraindications

A

Precautions and contraindications
Liver impairment
Not approved in pediatric population

35
Q

Meglitinide ADR

A

Hypoglycemia in vulnerable populations

36
Q

Meglitinides

Drug interactions

A

CYP3A4 and CYP2C9 inducers increase meglitinide metabolism.

Antifungals (ketoconazole) and antimicrobials (erythromycin) inhibit metabolism, increasing risk for hypoglycemia.

37
Q

Meglitinides

Rational drug selection: repaglinide

A

**For patients with postprandial hyperglycemia

38
Q

Meglitinides

Monitoring and patient education

A

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

39
Q

DPP-4 Inhibitors known as

A

“Gliptins”

Sitagliptin (Januvia) and saxagliptin (Onglyza)

40
Q

DPP-4 Inhibitors

Pharmacodynamics

A

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

41
Q

DPP-4 Inhibitors Precautions and contraindications

A

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

42
Q

DPP-4 Inhibitors you will see a side effect of

A

weight loss in obese patients

43
Q

DPP-4 Inhibitors ADR

A

ADRs: GI, headache

44
Q

Precautions and contraindications

DPP-4 Inhibitors

A

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

45
Q

DPP-4 Inhibitors

Drug interactions

A

Angiotensin-converting enzyme inhibitors: increased risk of angioedema

46
Q

Angiotensin-converting enzyme inhibitors: increased risk of angioedema

A

Monotherapy or in combination with other antidiabetic drugs

47
Q

DPP-4 Inhibitors

Rational drug selection

A

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

48
Q

DPP-4 Inhibitors

Monitoring

A

Renal function at baseline and annually

HbA1C every 3 months

49
Q

DPP-4 Inhibitors

Patient education

A

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

50
Q

DPP-4 Inhibitors

Monitor for potential

A

thyroid medullary cancer concerns, especially in those with previous nodules