Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

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

A

diabetes

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

3 cardinal signs of diabetes

A

polyuria, polyphagia, polydipsia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Cardinal sign of diabetes associated with excessive thirst

A

polydipsia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Cardinal sign of diabetes associated with excessive urination

A

polyuria

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Cardinal sign of diabetes associated with excessive hunger

A

polyphagia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Glucose intolerance from pregnancy

A

gestational diabetes

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

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

A

secondary diabetes mellitus

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Diabetes therapy is directed at maintaining _____

A

euglycemic states (normal blood sugar)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

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

A

insulin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Cells that produce insulin

A

beta cell of the pancreas

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

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

A

insulin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

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

A

insulin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

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

A

proinsulin, preproinsulin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

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

A

F - only its active form is prone to degradation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Classification of insulin preparation:
Lispro

A

rapid-acting

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Classification of insulin preparation:
Aspart

A

rapid-acting

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Classification of insulin preparation:
Glulisine

A

rapid-acting

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Classification of insulin preparation:
Human Insulin (Regular)

A

short-acting

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Classification of insulin preparation:
Lente

A

intermediate-acting

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

Classification of insulin preparation:
NPH insulin (isophane)

A

intermediate-acting

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Classification of insulin preparation: Ultralente
long-acting
26
Classification of insulin preparation: Detemir
long-acting
27
Classification of insulin preparation: Glargine
long-acting
28
Agents that stimulate the release of insulin from pancreas
insulin secretagogues
29
Drug agents under insulin secretagogues
sulfonylureases and meglitinides
30
Secondary line of treatment for diabetes
sulfonylureases
31
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
sulfonylureases
32
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
sulfonylureases - 1st generation
33
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
sulfonylureases - 2nd generation
34
MOA: similar to sulfonylureases; Repaglinide binds to SUR1, SUR2A and SUR2B leading to extrapancreatic effects
meglitinides
35
Extrapancreatic effect of Repaglinide
cardiac smooth muscle relaxation
36
SAR: benzoic acid derivative of non-sulfonylurea moiety of glyburide/glibenclamide
meglitinides
37
Does repaglinide produce hyperinsulinemia
no
38
METABOLISM: CYP 2C8 and 3A4 hydroxylation of piperidine ring and glucuronidation
repaglinide
39
METABOLISM: CYP 2C9 (70%) and 3A4 hydroxylation of isopropyl moiety.
nateglinide
39
Compare DOA of repaglinide and nateglinide
repaglidine has a short DOA while nateglidine has a longer DOA
40
Meaning of NPH from NPH insulin
neutral protamine hagedorn
41
First line of treatment for diabetes coupled with lifestyle change
Biguanides
42
Drug class that is highly distributed in the body and is excreted unchanged in the urine
Biguanides
43
MOA: decreases gluconeogenesis; increases glycogenolysis and glycolysis; increases insulin sensitivity
Biguanides
44
SAR: made of 2 linked guanidine moiety
Biguanides
45
May cause GI discomfort, lactic acidosis and has metallic taste
Metformin
46
Only biguanide approved for use
Metformin
47
Meaning of PPAR
peroxisome proliferator activated receptor
48
Controls gene expression to increase glucose transporter expression, leading to increased insulin sensitivity
PPAR agonist/insulin sensitizer
49
PPAR agonist effect on glucogeonesis and fatty acids
decrease glucogenolysis, lowers fatty acids
50
SAR: consists of thiazolidinedione
PPAR agonist/insulin sensitizer
51
Needed for agonist activity of insulin sensitizers
R must be e para- substituted phenyl ring attached to pharmacophore with methylene bridge
52
Metabolism: CYP2C9, with its metabolites still possessing agonist activity (longer DOA)
PPAR agonist/insulin sensitizer
53
Only available glitazone in the market
Pioglitazone
54
Useful for patients who can't tolerate sulfonylurea and metformin
Pioglitazone
55
PPAR agonist drug that is not used due to severe hepatoxicity
Troglitazone
56
Limited availability due to cardiovascular effects
Rosiglitazone
57
Enzyme made of maltase, sucrase, isomaltase and glucoamylase which breaks don carbohydrates
a-glucosidase
58
Inhibits a-glucosidase to inhibit carbohydrate breakdown, preventing mono/disaccharide absorption which results to inhibition of post-prandial hyperglycemia
a-glucosidase inhibitor
59
SAR: inhibitors that mimic the natural substrate of a-glucosidase by having same structures (polyhydroxy)
a-glucosidase inhibitors
60
a-glucosidase inhibitor that is poorly absorbed
voglibose
61
a-glucosidase inhibitor that is not metabolized hence, excreted unchanged
miglitol
62
a-glucosidase inhibitor with a low oral bioavailability
acarbose
63
Messenger that travel from stomach to pancreas to in the presence of food and signals insulin release
glucagon-like peptide 1 (GLP-1)
64
30-31 amino acid peptide produced by prohormone convertase enzymes from proglucagon
glucagon-like peptide 1 (GLP-1)
65
Indicated for additional therapy with metformin or sulfonyl urea to reach HbA1c < 7%
GLP-1 agonist
66
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.
GLP-1 agonist
67
SAR: Analogs have penultimate amino acid modification to resit metabolism by dipeptidyl peptidase IV (DDP-IV)
GLP-1 agonist
68
AA modification: Penultimate Ala -> Gly
exanatide
69
first isolated, self-regulating, longer T1/2 than GLP-1
exanatide
70
AA modification: Lys26 has a-glutamoyl-(N-a-hexadaconyl) Lys34 is replaced by Arg34
liraglutide
71
T1/2 is 11 hrs = increase albumin binding, may cause medullary thyroid cancer or multiple endocrine neoplasia syndrome
liraglutide
72
AA modification Fusion of 2 modified GLP-1 to albumin
albiglutide
73
AA modification Fusion of 2 N terminal GLP-1 analog to IgG4 Fc domain
dulaglutide
74
T1/2 is 5 days = albumin moiety, may cause medullary thyroid cancer or multiple endocrine neoplasia syndrome
albiglutide and dulaglutide
75
MOA: binds to active serine site of DPPV-IV, alternatives to GLP-I agonist analogs
DPP IV inhibitors
76
SAR: has 3 pharmacophores: a-aminoacylpyrroline, xanthine and pyrimidine-2,4-dione
DPP IV inhibitors
77
In SAR of DPP-IV inhibitors, this group binds to the active serine part of DPP-IV molecule
cyano group
78
It can be taken alone or together with metformin or thiazolidinedione; rarely causes hypoglycemia
DPP IV inhibitors
79
DPP IV inhibitor with piperazine fused pyrazole with a-aminoacyl moiety
sitagliptin
80
DPP IV inhibitor with xanthine pharmacophore
linagliptin
81
DPP IV inhibitor with pyrimidine-2,4-dione pharmacophore
alogliptin
82
DPP IV inhibitors (2) with a-aminoacylpyroline pharmacophore
saxagliptin (parang may rocket) & vildagliptin
83
Enzyme that metabolizes GLP-I
dipeptidyl peptidase IV (DPP IV)
84
37-amino acid hormone released with insulin
amylin
85
MOA: suppresses glucagon secretion, delays gastric emptying time, to modulate appetite centers which aids in maintaining glucose plasma level
amylin agonist
86
SAR of Amylin agonist: ____ is an amylin agonist analog
pramlinitide
87
Pramlintide is an analog which is ____ water soluble and has ____ aggregation
more; reduced
88
SAR: Proline replacement for Ala25, Ser28, Ser29
amylin agonist
89
Aids in reabsorption of glucose from renal proximal tubes
sodium glucose cotransporter (SGLT2)
90
MOA: inhibits SGLT2 by binding to it, leading to decreased renal threshold for glucose which results in increased urinary glucose excretion
SGLT2 inhibitor
91
SAR: has a phlorizin pharmacophore and a glucose moiety that binds to Thr156 and Lys157 moiety of the transporter
SGLT2 inhibitor
92
Drug class not recommended for Type 1 diabetes and patients with renal impairment due to its side effect of frequent urination
SGLT2 inhibitor
93
Empagliflozin, dapagliflozin and canagliflozin are part of this drug class
SGLT2 inhibitor

Organic Medicine LEC (5 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions