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Pharmacology > Diabetes mellitus 2 > Flashcards

Diabetes mellitus 2 Flashcards

1
Q

Biguanide antidiabetic drugs

A

Metformin

Phenformin

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2
Q

Metformin - MoA

A

Decreases hepatic glucose output and glucose absorption from the gut. Reduces expression of genes for gluconeogenesis enzymes. Increases insulin sensitivity. Increases glucose uptake and usage in skeletal muscle & adipose tissue. Does NOT stimulate insulin secretion

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3
Q

Metformin - Clinical use

A

DM2 (1st line) esp obese pt with insulin resistance, or with hyperlipideamia
Prediabetics

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4
Q

Metformin - Special consideration and contraindications

A

May enable loss of weight
Duration of action: 18h
Used alone or in comb with a sulfonylurea, meglitinide, alpha gucosidase inh or incretin mimetic.
Contraind: renal/hepatic disease, alcoholism, predisposition for lactic acidosis

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5
Q

Metformin - Adverse effects

A

GI disturbances: diarrhea (30%)
Lactic acidosis (rare)
Weight loss

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6
Q

Metformin - Interactions

A

Cimetidine can inhibit metabolism of metformin

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7
Q

Phenformin - MoA

A

Binds to mitochondria and interfere with glucose oxidation –>lactic acidosis

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8
Q

Phenformin - Special consideration and adverse effects

A

NOT used: fatal lactic acidosis as risk!

Adverse: lactic acidosis

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9
Q

Thiazolidinediones

A

Pioglitazone

Rosiglitazone

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10
Q

Thiazolidinediones - MoA

A

Agonists of peroxisome proliferator-activated receptor-γ (PPAR- γ). Increases transcription of insulin responsive genes that control glucose metabolism (GLUT-4 transporters). Results in increased insulin sensitivity and decreased insulin resistance. Suppress hepatic glucose output

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11
Q

Thiazolidinediones - Clinical use

A

Adjunct to diet & exercise for DM2. Pt unwilling to use injectable agents.

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12
Q

Thiazolidinediones - Special considerations and Contraindications

A

Oral adm.
Greater effect on skeletal muscle and adipose tissue, lesser on liver.

Contraind: heart failure risk

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13
Q

Thiazolidinediones - Adverse effects

A

Edema, increased risk of heart failure
Increased body weight
Decrease bone mineral density, increases risk of osteoporosis and fractures in older women

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14
Q

Pioglitazone - MoA

A

Partial PPAR-receptor agonist

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15
Q

Pioglitazone - Clinical use

A

DM2 who cannot control disease with other oral drugs/unwilling to use insulin

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16
Q

Pioglitazone - Special considerations

A

Increased HDL and decreased triglycerides in serum more than rosiglitazone

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17
Q

Pioglitazone - Adverse effects

A

18 % risk of MI, stroke or death

Study: increased risk of bladder cancer

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18
Q

Rosiglitazone - MoA

A

Full PPAR-receptor agonist

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19
Q

Rosiglitazone - Special considerations

A

Increased LDL in serum more than pioglitazone

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20
Q

Rosiglitazone - Adverse effects

A

Increased risk for MI 43%.

Increased Cardiovascular death risk 64%.

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21
Q

α-Glucosidase inhibitors

A

Acarbose

Miglitol

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22
Q

α-Glucosidase inhibitors - MoA

A

Competitive inhibition of α-Glucosidase, delaying starch and disaccharide digestion. Also decreases glucose absorption. Decreases postprandial hyperglycemia

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23
Q

α-Glucosidase inhibitors - Clinical use

A

DM2 (usually in combo with other oral antidiabetic)

24
Q

α-Glucosidase inhibitors - Special consideration

A

Adm at first bite of meal.

25
Q

α-Glucosidase inhibitors - Adverse effects

A

Increased Flatulence, abd bloating

26
Q

Acarbose - Interactions

A

Increases bioavailability of metformin

27
Q

Miglitol - Interactions

A

Decreased Iron absorption

Decreased Absorption of ranitidine and propranolol

28
Q

GLP-1 mimetics

A 
Exenatide
Liraglutide
Albiglutide
Dulaglutide
Lixisenatide
29
Q

Incretin mimetics - MoA

A

Enhances effect of glucagon-like peptide-1 (GLP-1)

Stimulation of glucose-dependent insulin secretion, increased uptake of glucose by muscle and fat tissue, decreased glucagon secretion, slowed gastric emptying, increased satiety, and decreased food intake.

30
Q

Incretin mimetics - Clinical use

A

DIA2, comb with sulfonylurea or metformin –> improve A1C values and decreases body weight.

31
Q

Exenatide - Special consideration

A

Adm subcutn twice daily.
Once weekly injection.
Monitor for abd pain

32
Q

Exenatide - Adverse effects

A

Mild-moderate nausea, pancreatitis (pt with hypertriglycidemia/ gallstones). Abdominal pain

33
Q

Liraglutide and Albiglutide - Administration

A

Adm subc once daily

34
Q

Liraglutide - Adverse effects

A

Dose-dependent & treatment-duration-dependent thyroid C-cell tumor (study).
Increased Risk for pancreatitis

35
Q

Once weekly injected drugs

A

Exenatide, Albiglutide, Dulaglutide

36
Q

DPP-4 inhibitors

A

Sitagliptin
Linagliptin
Saxagliptin

37
Q

DPP-4 inhibitors - MoA

A

Increases GLP-1 levels: Stimulation of glucose-dependent insulin secretion, increased uptake of glucose by muscle and fat tissue, decreased glucagon secretion, slowed gastric emptying, increased satiety, and decreased food intake.

38
Q

DPP-4 inhibitors- Clincal use

A

DM2: improve glycemic control

39
Q

DPP-4 inhibitors- Special consideration

A

Well suited for old, frail people

Once daily oral adm

40
Q

DPP-4 inhibitors - Adverse effects

A

Joint and skeletal muscle pain
Nasopharyngitis
Rhinitis

41
Q

Sodium-glucose cotransporter 1 inhibitors

A

Canagliflozin
Dapagliflozin
Empagliflozin

42
Q

SGLT inhibitors - MoA

A

Inhibit SGL2: Decreased renal glucose reabsorption, Increased urinary glucose excretion, and lower blood glucose.

43
Q

SGLT inhibitors - Special consideration and Cotraindication

A

Efficacy dependent of glomerular filtration. Contraindication: pt with GFR <50mL/min

44
Q

SGLT inhibitors - Adverse effects

A

Weight loss, lower BP.
Increased incidence of UTI and genital yeast infections (because increased urinary glucose and facilitate growth of bacteria).
Volume depletion
Diabetic ketoacidosis
increased risk of osteoporosis and bone fractures (increased urinary calcium excretion)

45
Q

Canagliflozin and Dapagliflozin - Contraindication

A

Dehydration, heart failure, low BP, taking diuretics and ACE inhibitor.

46
Q

Canagliflozin and Dapagliflozin - Adverse effects

A

Acute renal injury (azotemia)

47
Q

Empagliflozin - Special consideration

A

Reduces progression to renal disease in DIA2 with high risk of cardiovascular event.

48
Q

Amylin analogue

A

Pramlintide acetate

49
Q

Amylin analogue - MoA

A

Antihyperglycemic effect
Decreases Rate of rise of blood glucose by slowing gastric emptying (Slows the rate at which food is delivered from the stomach to the intestines ), suppressing glucagon secretion and glucose output by the liver, Decreases appetite –> weight loss

50
Q

Amylin analogue - Clinical use

A

Weight loss and glycemic control in DM.

DM1 and DM2 on insulin treatment.

51
Q

Pramlintide acetate - Adverse effect

A

Hypoglycemia (esp in coadministration with insulin)

Nausea, anorexia, headache

52
Q

Dopamine agonist

A

Bromocriptine

53
Q

Bromocriptine - MoA

A

Resets disturbed circadian rhythm and reduces hepatic glucose output and serum triglycerides and free fatty acids.

54
Q

Bromocriptine- Clincal use

A

Hyperprolactinemia, Parkinson disease.

Study: Decreases insulin resistance and A1C

55
Q

Bromocriptine - Special consideration

A

Decreased Dopamine cause disturbances in circadian rhythm and can lead to insulin resistance, obesity and diabetes.
Should be taken with food

56
Q

Dopamine - Adverse effects

A

Nausea

Pharmacology (55 decks)

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