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Pharma > Oral Hypoglycemic Agents > Flashcards

Oral Hypoglycemic Agents Flashcards

1
Q

Reduces hepatic insulin resistance
Reduces gluconeogenesis by as much as 75%
Decreases FASTING glucose levels

HbA1C reduction: 1-2%

A

Metformin

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2
Q

Immediate release Merformin
Half life:
Peaks:

A

2-6 hours

1 hour after intake

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3
Q

Extended release Merformin
Half life:
Peaks:

A

4-8 hours

7 hours

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4
Q

Merformin clearance and metabolism:

A

Renal

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5
Q

Metformin AE

A

GI intolerance: Nausea, diarrhea, crampy abdominal pain and dysgeusia
Vit B12 deficiency

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6
Q

NO Hypoglycemia
Promotes weight loss/Neutral
Improvement in microvascular and macrovascular complications
Reduces LDL and procoagant factors

A

Metformin

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7
Q

Potential SE for Metformin

A

Lactic acidosis

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8
Q

Metformin is CI in:

A 
CKD 
GFR < 30 ml/min/1.73m2 
Use with caution if: GFR <50 ml/min/1.73m2
Hepatic insufficiency
Heavy alcohol abuse
Hypoxia
Acute illness
Surgical indications
Dehydration 
Use of contrast dyes
Decompensated CHF
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9
Q

Metformin cab be used if the GFR is more

A

than > 30 ml/min

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10
Q

Reduction of Metformin dose should be done if GFR is

A

<45 ml/min

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11
Q

A biguanide first line oral agent for T2DM
Decreases hepatic glucose production
Decreases intestinal glucose absorption

Inhibits the mitochondrial enzyme glycerophosphate dehydrogenase -> decreased hepatic gluconeogenesis

A

Metformin

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12
Q

Activates
AMP-activated protein kinase (AMPK) enzyme -> decreased gluconeogenesis
Increased insulin sensitivity

A

Metformin

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13
Q

“glitazone”

A

Thiazolidinedione

Rosiglitazone, Pioglitazone

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14
Q

Increases glucose utilization
Decreases glucose production in adipose, muscle and liver

Increases body’s sensitivity to insulin

A

Thiazolidinedione (glitazone)

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15
Q

Ligands of peroxisome proliferator activated receptor gamma (PPAR-Y) an intranuclear receptor that regulates gene transcription

Slow improvement in glucose control

HbA1C reduction: 0.5-1.4%

A

Thiazolidinedione glitazone

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16
Q

PPAR-Y upregulates the hormone for increased insulin sensitivity and fatty acid oxidation

A

Adiponectin

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17
Q

Pioglitazone half life:

A

3-4 h

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18
Q

Activation of PPAR-Y by thiazolidinedione glitazone increases the differentiation and number of

A

adipocytes

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19
Q

Thiazolidinedione glitazone SE

A

decreases serum TAG
weight gain esp if combined with sulfonylurea or insulin
fluid retention

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20
Q

Thiazolidinedione glitazone also upregulates the receptor in peripheral tissues

A

GLUT4 increasing glucose uptake

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21
Q

Thiazolidinedione glitazone clearance

A

Renal 15-30
Fecal >60

Metabolized with hydroxylation and oxidation

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22
Q

Thiazolidinedione glitazone advantages:

A

Red progression of decreasing intimal medial thickness
Decreased rates of in-stent restenosis in PCI
Normalization of vascular endothelial function
Improvement in fibrinolytic and coagulation parameters, reduction in inflammatory markers
Treatment of fatty liver

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23
Q

Thiazolidinedione glitazone CI:

A

Not to be used for patients with ACTIVE hepatocellular disease
AST > 2.5x upper limit of normal

Caution against patients with CHF NYHA 3 and 4

Increased fracture rates due to dec osteoblast formation

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24
Q

Patients taking thiazolidinedione glitazone have inc risk for edema due increased Na reabsorption at the renal tubules especially if:

A 
those treated with insulin
with preexisting edema
women
obese patients
known IHD, HF, diastolic dysfunction, renal insufficiency
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25
Q

Because thiazolidinedione glitazone are intranuclear receptor agents, the decrease in glucose will take effect after

A

several days

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26
Q

Islet amyloid polypeptide analogues

Decreases glucagon
Decreases gastric emptying
Decreases appetite

A

Amylin Pramlintide

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27
Q

Used in both type 1 and type 2 dm to control post prandial glucose spike

A

Amylin analogue Pramlintide

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28
Q

Pramlintide SE

A

Hypoglycemia
GI (nausea, vomiting, anorexia)

subcutaneous

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29
Q

Inhibits alpha glucosidase enzymes decreasing the conversion of disaccharides into absorbable monosaccharides in the brushborder of the intestine

A

Alpha glucosidase inhibitors Acarbose and Miglitol

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30
Q

These delay carbohydrate absorption blunting postprandial glucose spike by 30-50%

HbA1C reduction: 0.5 - 0.8%

A

Alpha glucosidase inhibitors
Acarbose
Miglitol

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31
Q

Acarbose half life:

A

2 hours

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32
Q

Alpha glucosidase inhibitors acarbose and miglitol SE:

A

GI: diarrhea, flatulence, abdominal pain due to fermentation of undigested carbohydrate by gut bacteria

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33
Q

Alpha glucosidase inhibitors

Acarbose and Miglitol, Voglibose are CI in

A

Patients with chronic intestinal conditions particularly inflammatory bowel disease

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34
Q

“flozin”

A

SGLT2 inhibitor

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35
Q

Inhibits reabsorption of glucose in renal tubules via SGLT2

Increases excretion of glucose in the urine

HbA1C reduction: 0.5-1.5%

A

SGLT2 inhibitor flozin

36
Q

SLGT2 inhibitors act on this segment of the kidney

A

S1 segment of proximal tubule

90 reabsorption

37
Q

SGLT2 flozin AE

A

UTI due to inc urine glucose concentration

38
Q

Dapagliflozin half life:

A

12.9 h

39
Q

Canagliflozin half life:

A

10-13 h

40
Q

Empagliflozin half life:

A

5.6-13.1 h

41
Q

SGLT2 flozin advantage:

A

Loss of calories (weight loss of 2-3kg)
80-85 g glucose/d
Decreases systolic blood pressure 2-3mmHg

42
Q

SGLT2 flozin CI:

A 
Renal insufficiency
Induces osmotic diuresis
UTI
Candida infection 
Euglycemic ketoacidosis (inc glucagon)
Signals for increased fracture (patients with osteoporosis)
43
Q

Cleaved from proinsulin in secretory granule released with endogenous secretion of insulin

A

C peptide

44
Q

C peptide is measured only when

A

Body produces endogenous insulin

45
Q

Insulin can be used in hyperkalemia because

A

It promotes entry of K into cells via inc Na/KATPase in skeletal muscle

46
Q

Insulin
Rapid acting
Short duration

Helpful for controlling rapid post prandial glucose spike

A

Glulisine
Aspart
Lispro

GAL

47
Q

Insulin
Delayed onset
Intermediate duration of action

Administered IV becomes immediate for DKA and hyperkalemia

A

Regular insulin

Neutral Protamine Hagedorn (more delayed)

48
Q

Insulin
Long acting
Provide a steady background level of insulin

For stable effect 2x daily

A

Detemir

Glargine (no peak) 24h

49
Q

Most common complication of insulin therapy

A

Hypoglycemia

50
Q

Taken orally to stimulate endogenous insulin release in beta cells

A 
Sulfonylurea 
Glyburide
Glipizide
Glibenclamide
Glimepiride
51
Q

Bind the ATP dependent K channel on beta cells -> release of endogenous insulin

A

Sulfonylurea
Gliburide
Glipizide

52
Q

1st gen of sulfonylurea “amide”

Long duration rarely used

A

Tolbutamide

Chlorpropamide

53
Q

2nd gen sulfonylurea “ride”
Smaller dosing
Long duration of action

A

Glyburide

Glimepiride

54
Q

Sulfonylurea with shortest duration of action and

Less risk of hyperglycemia

A

Glipizide

55
Q

“glinide”

A

Meglitinde

56
Q

Non sulfa drugs that Bind K channels shutting them off leading to depolarization of beta cell and release of endogenous insulin

Measures C peptide

Like sulfonylurea but rapid onset and shorter duration of action

A

Meglitinide glinide
Repaglinide
Nateglinide

57
Q

Can be used in patients with allergies to sulfa

A

Meglitinide
Repaglinide
Nateglinide

58
Q

Carry significant risk of hypoglycemia and weight gain

A

Sulfonylurea Gliburide Glipizide

Meglitinide Repaglinide

59
Q

“Tide”

A

GLP 1 agonists

60
Q

Activate glucagon-like peptide GLP-1 receptor (increased insulin release and satiety, dec glucagon release and gastric emptying)

A

GLP-1 agonist

Exenatide

61
Q

Innibits dipeptidyl peptidase-4 DPP-4 inhibitors “gliptin” prevent breakdown of GLP-1

Increasing levels of GLP-1 (increased insulin release and satiety, decreased glucagon release and gastric emptying)

A

DPP-4 inhibitors gliptin

62
Q

DPP-4 inbibitors gliptin can increase the risk of

A

nasopharyngitis

upper respiratory tract infections

63
Q

GLP-1 agonists can cause

A

Pancreatitis
Necrotizing Pancreatitis
Thyroid cell C tumor

Exenatide
Exendin-4
Taspoglutide

64
Q

Do not cause hypoglycemia

A

GLP-1 agonist tide

DPP-4 inhibitor gliptin

65
Q

Sulfonylurea Gliburide Glipizide SE:

A

Hypoglycemia

Weight gain >/= 2 kg

66
Q

Sulfonylurea gliburide glipizide CI:

A

Sulfa allergy
Cross reactivity with other drugs such as carbonic anhydrase inhibitors, loop diuretics, thiazide
Severe renal failure and liver failure
Clearance highly dependent on renal function
Blunting of ischemic preconditioning

67
Q

Short acting
Dose with meal has better post prandial control
HbA1C reduction: 1-1.5%

Duration: 1/2 hour

Change fat distribution by decreasing visceral fat and increasing peripheral fat

A

Meglitinide

68
Q

Meglitinide is completely metabolized by

A

biotransformation and conjugation by glucoronic acid
90% recovered in feces
8% in urine

69
Q

Meglitinide SE

A

Risk of hypoglycemia (elderly)
Weight gain (~5 lb)
Should be used with caution in patients with Chronic Liver Disease

70
Q

Synthetic form found in saliva of Gila monster

Reduces both fasting and PPG

T1/2: 2-4 hours

HbA1C reduction: 0.8 - 1.1%

Nausea, vomiting, diarrhea

A

Exenatide

GLP 1 Agonist

71
Q

Acylated anogue of GLP1

97% homology to GLP1
T1/2: 9-14 hours

HbA1c reduction: 1.6%

Weight loss: 2.5 kg/30 weeks

A

Liraglutide

GLP1 agonist

72
Q

Prandial GLP-1

Potent GLP-1 receptor agonist

HbA1c reduction: 1.7%

Weight loss

A

Lixesenatide

73
Q

Increase insulin secretion
Decrease glucagon release
Delay gastric emptying
Supress appetite

A

DPP-IV inhibitors liptin

74
Q

Orally active

Selective inhibitors of DPP-IV

A

DPP-IV inhibitors gliptin

Sitagliptin - 12.5 hours half life
Linagliptin - 12.5 hours half life 
Vildagliptin
Saxagliptin
Septagliptin
Allogliptin
75
Q

DPP-IV inhibitors adverse effects

A

Nasopharyngitis because substance P is also a substrate for DPP-IV whose levels get elevated, GIT distress and diarrhea

76
Q

Insulin enhancers

A

Sulfonylurea
Meglitinide
Drugs with incretin effect: DPP-4 inhibitors; GLP-1 analogues

77
Q

Insulin sensitizers

A

Metformin

Thiazolidinedione

78
Q

Sulfonylurea adverse effects

A 
Hypoglycemia
Weight gain
Blood - agranulocytosis, thrombocytopenia, BM aplasia, RBC aplasia, hemolytic anemia 
Skin - SJS 
GI - nausea, vomiting, heart
Liver abnormal function test
79
Q

Thiazolidinedione SE

A 
Edema
Weight gain 
Dilution anemia 
Bladder Cancer 
Liver enzyme elevations rare 
GI discomfort
80
Q

Thiazolidinedione CI

A 
Heart disease NYHA III/IV
Pregnancy
Breastfeeding
Children
Fluid retention/signs and symptoms of heart failure
81
Q

Phenylalanine meglitinide derivative

A

Nateglinide

82
Q

2 incretin molecules inhibited by DPP4 Dipeptidyl Peptidase 4

A

Glucose Like Peptide 1 GLP-1

Gastric Inhibitory Peptide Glucose Dependent Insulonitropic Peptide GIP

83
Q

SGLT 2 with improved CV risk

GLP-1

A

Empagliflozin (Jardiance)
Canagliflozin (Invokana)

Liraglutide (Victoza)

84
Q

GLP is secreted by

Potent inhibition of gastric emptying
Potent inhibition of glucagon

Promotes Beta cell growth

Reduces appetite and body weight

A

L cells of distal GI tract (ileum and colon)

85
Q

GIP is secreted by

A

K cells of proximal GI tract (duodenum and proximal jejunum)

86
Q

Vacuolization and PAS positive glycogen accumulation within cytoplasm of tubular epithelial cells in DM

A

Armanni Ebstein lesion

87
Q

Oral antihypoglycemic for patients with CKD because it is excreted through bile and gut

A

Linagliptin

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