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Organic Medicine LEC > ENDOCRINE DRUGS - Anti-Diabetic Agents > Flashcards

ENDOCRINE DRUGS - Anti-Diabetic Agents Flashcards

1
Q

Gold standard to be taken for diabetes

A

insulin

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2
Q

Drugs taken when insulin is not yet required; helps in the utilization of insulin innately produced by the body

A

anti-glycemic agents

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3
Q

Complex disease characterized by uncontrolled glucose homeostasis associated with several minor and major complications

A

diabetes

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4
Q

3 cardinal signs of diabetes

A

polyuria, polyphagia, polydipsia

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5
Q

Cardinal sign of diabetes associated with excessive thirst

A

polydipsia

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6
Q

Cardinal sign of diabetes associated with excessive urination

A

polyuria

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7
Q

Cardinal sign of diabetes associated with excessive hunger

A

polyphagia

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8
Q

Type of diabetes which has a juvenile onset and is caused by absence or insufficiency of insulin produced

A

diabetes mellitus type 1

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9
Q

Type of diabetes which commonly has an adult-onset and is mainly caused by the body being desensitized to insulin despite the body’s normal production

A

diabetes mellitus type 2

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10
Q

Glucose intolerance from pregnancy

A

gestational diabetes

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11
Q

Type of diabetes which results from non-usual causes or from other disease present in the patient

A

secondary diabetes mellitus

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12
Q

Diabetes therapy is directed at maintaining _____

A

euglycemic states (normal blood sugar)

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13
Q

An endocrine peptide drug which is composed of 51 amino acids with 2 chains linked by a disulfide bond

A

insulin

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14
Q

Cells that produce insulin

A

beta cell of the pancreas

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15
Q

MOA: transports glucose to the muscles and adipose tissue with the release of glucose transporters (GLUT 4)

A

insulin

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16
Q

SAR: N and C terminals of Chain A and B are essential for insulin receptor binding

A

insulin

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17
Q

Insulin is produced via proteolytic modification of _______ which is formed by the removal of 24-amino acid from _______.

A

proinsulin, preproinsulin

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18
Q

T/F
The inactive form of insulin is prone to degradation.

A

F - only its active form is prone to degradation

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19
Q

Classification of insulin preparation:
Lispro

A

rapid-acting

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20
Q

Classification of insulin preparation:
Aspart

A

rapid-acting

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21
Q

Classification of insulin preparation:
Glulisine

A

rapid-acting

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22
Q

Classification of insulin preparation:
Human Insulin (Regular)

A

short-acting

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23
Q

Classification of insulin preparation:
Lente

A

intermediate-acting

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24
Q

Classification of insulin preparation:
NPH insulin (isophane)

A

intermediate-acting

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25
Q

Classification of insulin preparation:
Ultralente

A

long-acting

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26
Q

Classification of insulin preparation:
Detemir

A

long-acting

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27
Q

Classification of insulin preparation:
Glargine

A

long-acting

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28
Q

Agents that stimulate the release of insulin from pancreas

A

insulin secretagogues

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29
Q

Drug agents under insulin secretagogues

A

sulfonylureases and meglitinides

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30
Q

Secondary line of treatment for diabetes

A

sulfonylureases

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31
Q

MOA: Binds to sulfonylurea receptor 1 (SUR1) at ATP-sensitive K-channels and opens voltage-gated calcium leading to increased intracellular Ca and exocytotic release of insulin

A

sulfonylureases

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32
Q

SAR: small lipophilic R1, alkyl or aryl substituent R2, high dosing (low potency), short DOA, long plasma T1/2, high chance for ADR (hypoglycemia)
*include which generation

A

sulfonylureases - 1st generation

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33
Q

SAR: large p-(β-arylcarboxyamidoethyl) group at R1, high potency (low dosing), long DOA, rapid onset, short plasma T1/2, minimal ADR
*include which generation

A

sulfonylureases - 2nd generation

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34
Q

MOA: similar to sulfonylureases; Repaglinide binds to SUR1, SUR2A and SUR2B leading to extrapancreatic effects

A

meglitinides

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35
Q

Extrapancreatic effect of Repaglinide

A

cardiac smooth muscle relaxation

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36
Q

SAR: benzoic acid derivative of non-sulfonylurea moiety of glyburide/glibenclamide

A

meglitinides

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37
Q

Does repaglinide produce hyperinsulinemia

A

no

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38
Q

METABOLISM: CYP 2C8 and 3A4 hydroxylation of piperidine ring and glucuronidation

A

repaglinide

39
Q

METABOLISM: CYP 2C9 (70%) and 3A4 hydroxylation of isopropyl moiety.

A

nateglinide

39
Q

Compare DOA of repaglinide and nateglinide

A

repaglidine has a short DOA while nateglidine has a longer DOA

40
Q

Meaning of NPH from NPH insulin

A

neutral protamine hagedorn

41
Q

First line of treatment for diabetes coupled with lifestyle change

A

Biguanides

42
Q

Drug class that is highly distributed in the body and is excreted unchanged in the urine

A

Biguanides

43
Q

MOA: decreases gluconeogenesis; increases glycogenolysis and glycolysis; increases insulin sensitivity

A

Biguanides

44
Q

SAR: made of 2 linked guanidine moiety

A

Biguanides

45
Q

May cause GI discomfort, lactic acidosis and has metallic taste

A

Metformin

46
Q

Only biguanide approved for use

A

Metformin

47
Q

Meaning of PPAR

A

peroxisome proliferator activated receptor

48
Q

Controls gene expression to increase glucose transporter expression, leading to increased insulin sensitivity

A

PPAR agonist/insulin sensitizer

49
Q

PPAR agonist effect on glucogeonesis and fatty acids

A

decrease glucogenolysis, lowers fatty acids

50
Q

SAR: consists of thiazolidinedione

A

PPAR agonist/insulin sensitizer

51
Q

Needed for agonist activity of insulin sensitizers

A

R must be e para- substituted phenyl ring attached to pharmacophore with methylene bridge

52
Q

Metabolism: CYP2C9, with its metabolites still possessing agonist activity (longer DOA)

A

PPAR agonist/insulin sensitizer

53
Q

Only available glitazone in the market

A

Pioglitazone

54
Q

Useful for patients who can’t tolerate sulfonylurea and metformin

A

Pioglitazone

55
Q

PPAR agonist drug that is not used due to severe hepatoxicity

A

Troglitazone

56
Q

Limited availability due to cardiovascular effects

A

Rosiglitazone

57
Q

Enzyme made of maltase, sucrase, isomaltase and glucoamylase which breaks don carbohydrates

A

a-glucosidase

58
Q

Inhibits a-glucosidase to inhibit carbohydrate breakdown, preventing mono/disaccharide absorption which results to inhibition of post-prandial hyperglycemia

A

a-glucosidase inhibitor

59
Q

SAR: inhibitors that mimic the natural substrate of a-glucosidase by having same structures (polyhydroxy)

A

a-glucosidase inhibitors

60
Q

a-glucosidase inhibitor that is poorly absorbed

A

voglibose

61
Q

a-glucosidase inhibitor that is not metabolized hence, excreted unchanged

A

miglitol

62
Q

a-glucosidase inhibitor with a low oral bioavailability

A

acarbose

63
Q

Messenger that travel from stomach to pancreas to in the presence of food and signals insulin release

A

glucagon-like peptide 1 (GLP-1)

64
Q

30-31 amino acid peptide produced by prohormone convertase enzymes from proglucagon

A

glucagon-like peptide 1 (GLP-1)

65
Q

Indicated for additional therapy with metformin or sulfonyl urea to reach HbA1c < 7%

A

GLP-1 agonist

66
Q

Identify the drug class:

MOA: Mimicked molecule is released from the L cells of GIT in response to food. It promotes insulin secretion from pancreas.

A

GLP-1 agonist

67
Q

SAR: Analogs have penultimate amino acid modification to resit metabolism by dipeptidyl peptidase IV (DDP-IV)

A

GLP-1 agonist

68
Q

AA modification:
Penultimate Ala -> Gly

A

exanatide

69
Q

first isolated, self-regulating, longer T1/2 than GLP-1

A

exanatide

70
Q

AA modification:
Lys26 has a-glutamoyl-(N-a-hexadaconyl)
Lys34 is replaced by Arg34

A

liraglutide

71
Q

T1/2 is 11 hrs = increase albumin binding, may cause medullary thyroid cancer or multiple endocrine neoplasia syndrome

A

liraglutide

72
Q

AA modification
Fusion of 2 modified GLP-1 to albumin

A

albiglutide

73
Q

AA modification
Fusion of 2 N terminal GLP-1 analog to IgG4 Fc domain

A

dulaglutide

74
Q

T1/2 is 5 days = albumin moiety, may cause medullary thyroid cancer or multiple endocrine neoplasia syndrome

A

albiglutide and dulaglutide

75
Q

MOA: binds to active serine site of DPPV-IV, alternatives to GLP-I agonist analogs

A

DPP IV inhibitors

76
Q

SAR: has 3 pharmacophores: a-aminoacylpyrroline, xanthine and pyrimidine-2,4-dione

A

DPP IV inhibitors

77
Q

In SAR of DPP-IV inhibitors, this group binds to the active serine part of DPP-IV molecule

A

cyano group

78
Q

It can be taken alone or together with metformin or thiazolidinedione; rarely causes hypoglycemia

A

DPP IV inhibitors

79
Q

DPP IV inhibitor with piperazine fused pyrazole with a-aminoacyl moiety

A

sitagliptin

80
Q

DPP IV inhibitor with xanthine pharmacophore

A

linagliptin

81
Q

DPP IV inhibitor with pyrimidine-2,4-dione pharmacophore

A

alogliptin

82
Q

DPP IV inhibitors (2) with a-aminoacylpyroline pharmacophore

A

saxagliptin (parang may rocket) & vildagliptin

83
Q

Enzyme that metabolizes GLP-I

A

dipeptidyl peptidase IV (DPP IV)

84
Q

37-amino acid hormone released with insulin

A

amylin

85
Q

MOA: suppresses glucagon secretion, delays gastric emptying time, to modulate appetite centers which aids in maintaining glucose plasma level

A

amylin agonist

86
Q

SAR of Amylin agonist: ____ is an amylin agonist analog

A

pramlinitide

87
Q

Pramlintide is an analog which is ____ water soluble and has ____ aggregation

A

more; reduced

88
Q

SAR: Proline replacement for Ala25, Ser28, Ser29

A

amylin agonist

89
Q

Aids in reabsorption of glucose from renal proximal tubes

A

sodium glucose cotransporter (SGLT2)

90
Q

MOA: inhibits SGLT2 by binding to it, leading to decreased renal threshold for glucose which results in increased urinary glucose excretion

A

SGLT2 inhibitor

91
Q

SAR: has a phlorizin pharmacophore and a glucose moiety that binds to Thr156 and Lys157 moiety of the transporter

A

SGLT2 inhibitor

92
Q

Drug class not recommended for Type 1 diabetes and patients with renal impairment due to its side effect of frequent urination

A

SGLT2 inhibitor

93
Q

Empagliflozin, dapagliflozin and canagliflozin are part of this drug class

A

SGLT2 inhibitor

Organic Medicine LEC (5 decks)

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