45. Diabetes mellitus drugs (continued) Flashcards Preview

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Flashcards in 45. Diabetes mellitus drugs (continued) Deck (107):
1

DM type 1 - treament strategies

1. low carbohydate diet
2. insulin replacement

2

DM type 2- treatment strategies

1. dietary modiciation
2. exercise for weight loss
3. oral agents
4. non - insulin injectables
5. insulin replacement

3

gestational diabetes mellitus - treatment strategies

1. dietary modification
2. exercise
3. insulin replacement ( if lifestyle modification dails)

4

gestational diabetes mellitus - insulin replacement is a part of the treatment strategy ?

only if lifestyle modification fails

5

insulin preparations - deug classes

1. rapid acting
2. short acting
3. intermediate acting
4. long acting

6

insulin preparations - side effects

1. hypoglycemia
2. rare hypersensitivity reaction
3. lipodystophy rare

7

insulin preparations - action

bind insulin receptor ( tyrosine kinase activity ) -->
1. LIver: increase glucose stored as glycogen
2. Muscle : increase glycogen and protein synthesis . Increase K+ uptake
3. Fat: Increase TG storage

8

insulin preparations - action on fat

Increase TG storage

9

insulin preparations - action on liver

increase glucose stored as glycogen

10

insulin preparations - action on muscles

increase glycogen and protein synthesis . Increase K+ uptake

11

insulin preparations - rapid acting - drugs

1. aspart
2. Lispro
Glulisine

12

insulin preparations - short acting - deugs

regular

13

insulin preparations - intermediate acting drugs

NPH

14

insulin preparations -long acting drugs

Determir
Glargine

15

insulin preparations - rapid acting - duration ?

2-5 h

16

insulin preparations -short acting - duration ?

4-8 h

17

insulin preparations -intermediate acting - duration ?

8-12 h

18

insulin preparations -long acting - duration ?

16-24 h

19

insulin preparations -rapid acting - clinical use

1. type 1 DM
2. type 2 DM
3. Gestational diabetes
POSTPRANDIAL GLUCOSE CONTROL

20

insulin preparations short-rapid acting - clinical use

1. type 1 DM
2. type 2 DM
3. Gestational diabetes
4. DKA (IV)
5. hyperkalemia ( +glucose)
6. stress hyperglycemia

21

insulin preparations -intermediate acting - clinical use

1. type 1 DM
2. type 2 DM
3. Gestational diabetes

22

insulin preparations -long acting - clinical use

1. type 1 DM
2. type 2 DM
3. Gestational diabetes
BASAL GLUCOSE CONTROL

23

Oral hypoglycemic drugs - classes

1. Biguanides
2. Sulfonylureas
3. Glitazones/ thiazolidinedione
4. Glp-1 analogs
5. DPP -4 inhibitors
6. AMylin analogs
7. SGLT -2 inhibitors
8. α-glucosidase inhibitors
9. Meglitinides

24

Oral hypoglycemic drugs - buguanides drugs ?

metformin

25

metformin action

exact mechanism unkwown
1. decreased gluconeogenesis
2. increased glycolysis
3. inreased peripheral glucose uptake
(increased insulin sensiticity

26

metformin clinical use

first line therapy intypw 2 DM ( causes modest weight loss

27

metformin can be used inpatients

without islet function

28

metformin - route of administration

oral

29

metformin- side effects

1. Gi upset
2. lactic acidosis ( in renal failure)

30

metformin is contraindicated in ... ( and why)

renal insufficiency
because of lactic acidosis

31

sulfonylureas - second generation drugs

1. glimepiride
2. glipizide
3.glypuride

32

sulfonylureas - first generation drugs

1. clorpropamide
2. tolbutamine

33

sulfonylureas - mechanism of action

close K+ channel in β cell membrane -->cell depolarizes --> insulin release via Ca2+ influx

34

sulfonylureas - clinical use

stimulate release of endogenous insullin in type 2 DM

35

sulfonylureas -type 1 DM?

useless - require some islet function

36

sulfonylureas - toxicities

1. increased risk of hypoglycemia in renal failure
2. first generation: disulfiram like reactioncemia

3. second generation : hypoglycemia
4. Weight gain

37

sulfonylureas in renal failure

increased risk for hypoclycemia

38

sulfonylureas - disulfiram like reaction ?

only with first generation drugs

39

Glitazone / thiazolidinediones - drugs

1. pioglitazone
2. rosiglitazone

40

Glitazone / thiazolidinediones - mechanism of action

increased insulin sensitivity in peripheral tissue . Binds PPAR-γ nuclear transcription regulator

41

Glitazone / thiazolidinediones - clinical use

used in monotherapy in type 2 DM or combined with other agents

42

Glitazone / thiazolidinediones - toxicity

1. weight gain
2. edema
3. hepatotoxicity
4. Heart failure
5. increased risk for fructures

43

Genes activated by PPAR-γ ---> so activation of PPAR- γ

- regulate fatty acid storage and glucose metabolism
-increase insulin sensitivity and levels of adiponectin

44

GLP-1 analogs - drugs

1. exenatide
2. Liraglutide

45

GLP-1 analogs - mechanism of action

1. icrease glucose depended insulin release
2. decrease glucagon release
3. decrease gastric emptying
4. increase satierty

46

GLP-1 analogs - clinical use

type 2 DM

47

GLP-1 analogs - toxicities

1. nausea
2. vomiting
3. pancreatitis
4. modest weight loss

48

DDP-4 inhibitors - drugs

- GLIPTIN
Linagliptin
2. Saxagliptin
3. Sitagliptin

49

DDP-4 inhibitors - mechanism of action

inhibits DDP-4 enzyme that deactivates GLP-1
1. increase glucose - dependent insulin release
2. decrease glucagon release
3. decrease gastric emptrying
4. icrease satiety

50

DDP-4 inhibitors - clinical use

type 2 DM

51

DDP-4 inhibitors - toxicities

Mild urinary or respiratory infections
wight neutral

52

Amylin analogs - drugs

Pramlinide

53

Amylin analogs - mechanism of action

1. decrease gastric emptying
2. decrease glucagon

54

Amylin analogs - clinical use

type 1 DM
type 2 DM

55

Amylin analogs - toxicitis

1. hypoglyemia
2. nausea
3. diarrhea

56

SGLT-2 inhibitors -drugs

-GLIFOZIN
1. Canagliflozin
2. Dapagliflozin
3. empagliflozin

57

SGLT-2 inhibitors - mechanism of action

block reabsorption of glucose in proximal convoluted tubule

58

SGLT-2 inhibitors - clinical use

type 2 DM

59

SGLT-2 inhibitors - side effects

1. Glucosuria
2. UTIs
3. vaginal yeast infection
4. hyperkalemia
5. dehydration ( orthostatic hypertension)

60

α- glucosidase inhibitors - drugs

1.acarbose
2. Miglitol

61

α- glucosidase inhibitors - toxicites

Gi disturbances

62

α- glucosidase inhibitors - clinical use

used as monotherapy in type 2 DM or in combination

63

α- glucosidase inhibitors - mechanism of action

inhibit intestinal brush - border a glucosidase --> delayed carbohydrate hydrolysis and glcuose absorption --> decrease postprandial hyperglycemia

64

acute hyperkalemia treatment

1. regular insulin
2. glucose

65

pralintide - class

amylin analg

66

block reabsorption of glucose in proximal convoluted tubule - drug

SLGT-2 inhibitors ( Canaglifolozin)

67

diabetes mellitus drug with vaginal yeast infenction as side effect

SLGT-2 inhibitors ( Canaglifolozin)

68

diabetes mellitus drug with mild respiratory or urinary infection as sife effect

DDP-4 inhibitors ( linagliptin, saxagliptin, sitagliptin)

69

diabetes mellitus drug that binf to PPAR- γ nuclear transcription

Glitazones/ thiazolidinediones ( pioglitazone, rosiglitazone)

70

SLGT-2 means

Sodium-glucose co transporter 2 inhibitor

71

Meglitinides - drugs

-Glinide
1. Nateglinide
2. Repaglinide

72

Meglitinides - mechanism of action

stimulate postprandial insulin release by binding to K+ channels on β-cells membranes ( different site from sulfonylureas)

73

Meglitinides - clinical use

used as monotherapy in DM 2 or combined with metformin

74

Meglitinides - side effects

1. weight gain
2. increased risk for hypoglycemia in renal failure

75

oral hypoglycemic drugs - drugs administrated through SC injection

1. GLp-1 analogs
2. Amylin analogs

76

• What is the basic treatment strategy for type 1 diabetes mellitus?

Low-carb diet, insulin replacement

77

• Name two α-glucosidase inhibitors. What is their mechanism of action?

Acarbose, miglitol; decrease postprandial hyperglycemia (brush border α-glucosidase inhibition delays sugar hydrolysis, glucose absorption)

78

• What is the basic treatment strategy for type 2 diabetes mellitus?

Insulin replacement therapy, oral agents, non-insulin injectables, dietary modification and exercise for weight loss

79

• In what population are α-glucosidase inhibitors used? What is their principal toxicity?

Type 2 diabetes mellitus (as monotherapy or in combination with other agents); gastrointestinal disturbances

80

• What is the basic treatment strategy for gestational diabetes mellitus?

Exercise, dietary modification, insulin replacement if lifestyle changes don't work

81

• A diabetic patient uses a drug that decreases gastric emptying and glucagon. Name the drug and three of its side effects.

Pramlintide (amylin analog); hypoglycemia, diarrhea, nausea

82

• Classify each insulin as rapid-, short-, long-, or intermediate-acting: NPH, glulisine, regular, lispro, glargine, aspart, detemir.

Rapid-acting: lispro, aspart, glulisine; short-acting: regular; long-acting: glargine, detemir; intermediate-acting: NPH

83

• In what populations may you prescribe amylin analogs? What is the mechanism of action?

Patients with type 1 or 2 diabetes; decreases gastric emptying and glucagon release

84

• Insulin binds insulin receptors, which have ____ signaling pathways.

Tyrosine kinase

85

• Give two examples of glucagon-like peptide-1 (GLP-1) mimetic drugs. What is the mechanism of action? What other drug class acts similarly?

Exenatide and liraglutide; increase insulin release and decrease glucagon release; DPP-4 inhibitors (linagliptin, saxagliptin, sitagliptin)

86

• What function does insulin have in each of these tissues: liver, muscle, fat?

Liver: increases glucose storage as glycogen; muscle: increases glycogen/protein synthesis and K+ uptake; fat: aids triglyceride storage

87

• The GLP-1 analogs and DPP-4 inhibitors have similar actions. How do their side effect profiles differ?

GLP-1 analogs can cause nausea, vomiting, pancreatitis; use of DPP-4 inhibitors can result in mild urinary or respiratory tract infection

88

• For which conditions is insulin generally an appropriate treatment? About what side effects should you warn patients before giving insulin?

DM1, DM2, gestational DM, DKA (IV), hyperkalemia (administer with glucose), stress hyperglycemia; hypoglycemia, hypersensitivity (rare)

89

• A diabetic has hypoglycemia, Other than insulin and second-generation sulfonylureas, which diabetes medication can cause hypoglycemia?

Pramlintide (amylin analog)

90

• A nondiabetic patient in the ICU is noted to have a blood glucose of 225 mg/dL. What medication is appropriate for this condition?

Insulin, which is effective in treating stress-induced hyperglycemia

91

• An oral drug increases insulin and decreases glucagon release. What drug classes can this belong to? Which population are they used in?

GLP-1 analogs (exenatide, liraglutide) and DPP-4 inhibitors (linagliptin, saxagliptin, sitagliptin); type 2 DM

92

• A patient with newly diagnosed type 2 DM is prescribed a biguanide. What is the mechanism of action, and what effect does it have?

The mechanism of metformin is unknown; insulin sensitizer (increases glycolysis and peripheral glucose uptake, decreases gluconeogenesis

93

• A diabetic uses a SGLT-2 inhibitor. What is the mechanism of action and what population is it used in? Name three side effects.

Canagliflozin blocks glucose reabsorption in the PCT; type 2 DM; glucosuria, UTIs, vaginal yeast infections

94

• A diabetic patient has no islet cell function. Which oral diabetic medication can be used? Name three side effects.

Metformin, because it increases sensitivity to glucose; modest weight loss, GI upset, lactic acidosis (most serious)

95

• A 68-year-old diabetic man with chronic renal disease becomes acidotic. What has he been taking?

Metformin—if metformin cannot be excreted, as in patients with renal impairment, medication buildup may lead to lactic acidosis

96

• A newly diagnosed type 2 diabetic man is prescribed the first-line oral agent. What common side effect should you warn him about?

Gastrointestinal upset, because the first-line oral agent is metformin

97

• Name two first-generation sulfonylureas. Name three second-generation sulfonylureas.

Tolbutamide, chlorpropamide; glyburide, glimepiride, glipizide

98

• A man with type 2 diabetes mellitus vomits and has facial redness after consuming alcohol. What class of diabetic drug is he likely taking?

First-generation sulfonylureas, which cause a disulfiram-like reaction with alcohol ingestion

99

• A type II diabetic patient is taking a drug that has hypoglycemia as a side effect. Describe the mechanism of action of this drug.

Sulfonylureas trigger endogenous insulin output by closing β cell membrane K+ channels (causes depolarization, Ca2+ influx, insulin output

100

• Will sulfonylureas work in type 1 diabetes mellitus?

No—these drugs require islet cell function and the ability to secrete endogenous insulin (defective in type 1 diabetes)

101

• A patient is prescribed pioglitazone. What class does it belong to?

Glitazones/thiazolidinediones (rosiglitazone also belongs to this class)

102

• How do glitazones/thiazolidinediones work?

They bind nuclear transcription regulator PPAR-γ (regulates FA storage/glucose metabolism), increasing insulin sensitivity/adiponectin level

103

• In what population are glitazones/thiazolidinediones prescribed? What are the main side effects of these drugs?
e

Type 2 diabetes mellitus (as monotherapy or in combination with other agents); weight gain, edema, hepatotoxicity, heart failure

104

• A diabetic patient takes insulin after meals to control glucose. What type of insulin is best suited to this purpose?

Rapid-acting insulins are best for postprandial glucose control

105

• A man takes a long-acting insulin at night before bed. What is the purpose of this drug? Name two drugs that this could be.

Basal glucose control; glargine, detemir

106

• A man has DKA. Which insulin preparation is he given, and how? What are two other indications (other than diabetes control) for this drug?

Regular insulin (short-acting) is given via IV in DKA; also used in hyperkalemia, stress hyperglycemia

107

• A woman has hyperkalemia. What treatment is she given to correct the electrolyte abnormality?
e

Regular insulin (short-acting) and glucose