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Pharmacology II > Anti-diabetic Medications (Exam 1) > Flashcards

Anti-diabetic Medications (Exam 1) Flashcards

(114 cards)

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1
Q

MOA of sulfonylureas

A

increase peripheral glucose utilization
decrease hepatic gluconeogenesis
increase number and sensitivity of insulin receptors

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2
Q

sulfonylureas are associated with

A

weight gain

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3
Q

functions of amylin

A

suppresses appetite
inhibits glucagon release
slows gastric emptying

which decreases plasma glucose

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4
Q

2nd gen sulfonylureas should be used with caution in patients with

A

cardiovascular disease
elderly patients

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5
Q

glyburide

A

hepatic metabolism into products with very low hypoglycemic activity
re-titration required when switching from glyburide to other sulfonylureas

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6
Q

glyburide use is restricted for

A

hepatic impairment and renal insufficiency patients

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7
Q

glipizide

A

shortest half life (2-4 hrs)
MDD cannot exceed 40 mg
90% glipizide metabolized in liver, rest excreted unchanged in urine

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8
Q

Glucotrol XL

A

24 hour action ER glipizide

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9
Q

when should glipizide be ingested?

A

30 minutes before breakfast to minimize postprandial hyperglycemia

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10
Q

glipizide is contraindicated in patients with

A

significant hepatic impairment

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11
Q

glipizide is preferred over glyburide in ____________ due to its

A

elderly and renal impaired patients

lower potency and shorter duration of action

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12
Q

glimepiride

A

once daily use alone or combined with insulin
half life: 5-9 hours
completely metabolized by liver

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13
Q

glimepiride achieves ____________________________ of any sulfonylurea compound

A

blood glucose lowering with the lowest dosage

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14
Q

Repaglinide

A

non-sulfonylurea insulin secretagogue with hypoglycemic activity
dosed alone or with metformin

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15
Q

repaglinide can be given to individuals with _____________ allergy because it has no __________________

A

sulfur or sulfonylurea

sulfur in its structure

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16
Q

MOA of repaglinide

A

acts on beta cells to release insulin by regulating K efflux through K channels

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17
Q

how is repaglinide similar to sulfonylureas

A

two common binding sites, one unique binding sites

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18
Q

Repaglinide is cleared by ___________ with a plasma half life of _____________

A

hepatic CYP3A4

1 hour

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19
Q

what metabolized repaglinide?

where are the metabolites excreted?

A

CYP3A4 and CYP2C8

the bile

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20
Q

repaglinide is indicated for use in

A

controlling postprandial glucose excursions

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21
Q

when on repaglinide, if a meal is delayed/skipped or contains low carbs,

A

hypoglycemia could be at risk

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22
Q

drugs usable in renally impaired and elderly

A

repgalinide
nateglinide
glipizide

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23
Q

nateglinide MOA

A

stimulates rapid and transient release of insulin from B cells through closure of ATP sensitive K channel

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24
Q

Nateglinide works better when

A

combined with non-secretagogue oral agents (metformin)

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25
Nateglinide is metabolized in the liver by
CYP2C9 and CYP3A4
26
main adverse effect of nateglinide
hypoglycemia
27
when is nateglinide taken?
before a meal and reduces the postprandial rise in blood glucose levels
28
when is nateglinide absorbed? peak concentration? duration of action? half life?
20 minutes after oral administration less than 1 hour 4 hours 1 hour
29
metformin MOA
inhibits mitochondrial chain complex 1 which decreases ATP levels and activates AMPK inhibits hepatic gluconeogenesis and opposes the action of glucagon
30
how does metformin use lead to increase in lactic acid?
it inhibits glycerol 3 phosphate dehydrogenase which stimulates conversion of pyruvate to lactate
31
what transcription factors does metformin activate using AMPK pathway what happens when these factors are activated?
CBP (CREB-binding protein) CRTC2 (CREB-regulated transcription coactivator 2) decreased gluconeogenic gene expression
32
what is first line of therapy for T2DM?
metformin
33
metabolism of metformin
half life - 1.5-3hrs not bound to plasma proteins excreted by the kidneys as the active compound
34
metformin blocks ____________ and impairs the hepatic _________________
gluconeogenesis lactic acid metabolism
35
in renal insufficiency, the biguanide _____________ and thereby increases the risk of _______________
accumulates lactic acidosis
36
metformin is contraindicated if the
eGFR is less than 30ml/min
37
Metformin does not increase _____________ or provoke _______________
body weight hypoglycemia
38
metformin can be used in combination with
insulin secretagogues or thiazolidinediones
39
metformin decreases the risk of
macrovascular and microvascular disease
40
which group of people does metformin prevent new onset T2DM in?
middle aged obese persons with impaired glucose tolerance and fasting hyperglycemia
41
toxic effects of metformin
GI upsets diarrhea
42
how does metformin cause vitamin B12 deficiency?
it interferes with calcium dependent absorption of vitamin B 12 intrinsic factor complex after many years of use
43
Metaglip
metformin and glipizide
44
Kombiglyze
saxagliptin and metformin
45
avandaryl
rosiglitazone and glimepiride
46
actoplus met
pioglitazone and metformin
47
glucovance
metformin and glyburide
48
avandamet
rosiglitazone and metformin
49
duetact
pioglitazone and glimepiride
50
janumet
sitagliptin and metformin
51
prandimet
repaglinide and metformin
52
jentadueto
metformin and linagliptin
53
synjardy
empagliflozin and metformin
54
xigduo
dapagliflozin and metformin
55
ivonkamet
canagliflozin and metformin
56
3 isoforms of intracellular nuclear transcription factors of thiazolidinediones
alpha (PPARa) gamma (PPARy) beta/delta (PPARb/d)
57
PPARy is expressed on
liver, adipose tissue and muscle
58
by activating PPARy, TZDs promote
fatty acid uptake and storage in adipose tissue rather than skeletal muscle and liver
59
when PPAR alpha is activated
reduction in TG level involved in regulation of energy homeostasis
60
when PPAR gamma is activated
insulin sensitization enhances glucose metabolism
61
when PPAR b/d is activated
enhances fatty acid metabolism
62
humoral stimulants of insulin release
glucose mannose leucine arginine AA fatty acids
63
hormonal stimulants of insulin release
glucagon GLP-1 glucose dependent insulinotropic polypeptide cholecystokinin gastrin
64
neural stimulants of insulin release
beta adrenergic stimulation vagal stimulation
65
drug stimulants of insulin release
sulfonylureas meglinitide nateglinide isoproterenol acetylcholine
66
hormonal inhibitors of insulin release
somatostatin insulin leptin
67
neural inhibitors of insulin release
alpha sympathomimetic effect of catecholamines
68
drug inhibitors of insulin release
diazoxide phenytoin vinblastine colchicine
69
what lab values should you monitor while a patient is on metformin?
A1C eGFR
70
thiazolidinediones effects
increase insulin sensitivity decrease insulin resistance increase glucose utilization
71
pioglitazone has more significant ___________ compared to rosiglitazone
lipid-lowering
72
mechanism contributing to hypoglycemic effects of thiazolidinediones
increased expression of the glucose transporter GLUT4 increases ability to uptake glucose when stimulated by insulin
73
Pioglitazone
PPARa and PPARy activity absorbed in 2 hours MDD 45mg food delays uptake
74
Pioglitazone is metabolized by
CYP2C8 and CYP3A4
75
rosiglitazone
rapidly absorbed and highly protein bound once or twice a day metabolized by CYP2C8 and CYP2C9
76
rosiglitazone is known to increase ________________ and has no effect on
HDL, LDL, total cholesterol triglycerides
77
alpha glucosidase inhibitors MOA
competitively inhibit the intestinal membrane bound alpha glucosidase enzymes
78
alpha glucosidase inhibits effects
reduce post meal glucose excursions delay digestion and absorption of starch and dissacharides
79
alpha glucosidase inhibitors metabolism
NONE! Digital is eliminated renally unchanged
80
alpha glucosidase inhibitors are contraindicated in
people with IBD
81
adverse effects of alpha glucosidase inhibitors
GI disturbance excess undigested carbs --> increased bacterial digestion of polysaccharides
82
exenatide
derivative of extendin-4 peptide in Gila monster venom 53% homology with native GLP1 glycine substitution to reduce degradation by DPP4
83
liraglutide
soluble fatty acid-acylated GLP1 analog half life - 12 hours
84
dulaglutide
two GLP-1 analog molecules covalently linked to Fc fragment of human IgG4 protects the GLP1 moiety from inactivation by DPP4 HL - 5 days
85
albiglutide
human GLP-1 dimer fused to human albumin half life - 5 days
86
adverse effect of GLP1 agonists
increase the risk of pancreatitis
87
GLP1 effects
induces B cell growth stimulates insulin production reduces appetite
88
DPP-4 enzyme
acts on incretin hormones (mainly GLP1 and GIP) increase insulin secretion and decrease glucagon secretion
89
half life of GLP1
less than 2 minutes
90
half life of GIP
7 minutes in healthy people 5 minutes in people with type 2 diabetes
91
DPP-4 inhibitors mechanism results in
increase circulating GLP-1 increase insulin levels decrease glucagon levels
92
metabolism of sitagliptin and linagliptin
excreted unchanged in urine
93
metabolism of saxagliptin
metabolized by CYP3A4/5 major metabolite is a DPP4 inhibitor
94
adverse effects of DPP4 inhibitors
GI disturbance
95
SGLT2 accounts for __________ of glucose reabsorption
90%
96
inhibition of SGLT2 causes
loss of glucose (glycosuria) and loss of water (osmotic diuresis) no reabsorption of glucose
97
how many GLUT transporters are there?
there is now 5! GLUT5 helps absorb fructose from gut and kidney
98
what so SGLTs do?
freely filter glucose by the renal glomeruli and reabsorb in the proximal tubules
99
adverse effects of SGLT2 inhibitors
increased urination increased UTIs hypotension
100
metabolism of SGLT2 inhibitors
glucuronidation in the liver and kidneys by uridine diphosphate glucuronosyltransferase-1A9
101
amylin is __________________ with insulin from _______________
co-secreted pancreatic B cell
102
another name for amilyn
islet amyloid polypeptide
103
human amylin is unsuitable for ______________ because it ________________
pharmacological use forms amyloid plaques and fibers (potentially toxic)
104
MOA of amylin anaolgs
binds to amylin receptor in specific regions of the brain reduces glucagon release
105
amylin effects
inhibits glucagon secretion in alpha cells appetite suppression delays gastric emptying handles both endogenous and exogenous
106
amylin analogs are used for treatment in
Type 1 and 2 DM
107
insulin allergy
type 1 hypersensitivity local/systemic urticaria from histamine release by mast cells sensitized by anti-insulin IgE antibodies
108
immune insulin resistance
lower titer of circulating IgG anti-insulin antibodies that neutralize the action of insulin associated with other systemic autoimmune disorders like SLE
109
rapid acting analogs
lispro aspart glulisine inhaled insulin
110
short acting insulin
human regular
111
intermediate acting insulin
human NPH
112
concentrated human regular insulin
U500 human regular insulin
113
basal analogs
glargine detemir degludec
114
premixed products of insulin
NPH/regular 70/30 Lispro 50/50 Lispro 75/25 Aspart 70/30

Pharmacology II (18 decks)

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