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PHARM 3 > Antidiabetic agents > Flashcards

Antidiabetic agents Flashcards

1
Q

insulin secretion stimulated by

A

glucose
amino acids
gastrointestinal hormones - incretins

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2
Q

incretin effect

A

oral glucose results in higher insulin than glucose IV

incretins rleased by gut enhance insulin secretion

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3
Q

insulin lispro

A

rapid acting

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4
Q

inuslin aspart

A

rapid acting

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5
Q

insulin glulisine

A

rapid acting

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6
Q

rapid acting insulins

A

hexamers - slow absorption

mimic prandial release of insulin - given with longer acting insulin, 15 mins before meal

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7
Q

short acting insulin

A

soluble crystalline zinc insulin

given 30 mins before a meal

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8
Q

intermediate acting insulins

A

neutral protamine hagedorn
crystalline zinc insulin + protamine

BASAL CONTROL

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9
Q

insuline glargine

A

long acting

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10
Q

inuslin detemir

A

long acting

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11
Q

IV insulin given when

A

pts with ketoacidosis
peri-operative
during labor
ICU

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12
Q

inhaled insulin

A

peak reached in 12-15 mins and decline in 3 hours

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13
Q

inhaled insulin AE

A

cough, throat pain, hypoglycemia

should monitor pulmonary function

contraindicated in asthma, COPD, smokers

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14
Q

basal bolus insulin regimen

A

1 daily shot of glargine, detemir

doses of lispro, aspart, or glulisine for each meal

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15
Q

insulin pump therapy

A

glulisine
lispro
insulin

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16
Q

hypoglycemia management

A

sugar containing food

if severe – IV glucose infusion

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17
Q

insulin AE

A

allergic reaction - immediate hypersensitivity

lipodystrophy at injection site

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18
Q

drugs that cause hypoglycemia

A

ethanol - inhibits gluconeogenesis

b blockers - block effects of catecholamines on gluconeogenesis and glycogenolysis

salicylates - enhance beta cell sensitivity to glucose and potentiate insulin secretion

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19
Q

drugs that cause hyperglycemia by countering action of inuslin

A

epinepherine
glucocorticoids
atypical antipsychotics
HIV protease inhibitors

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20
Q

drugs that cause hyperglycemia by inhibition insulin secretion

A

phenytoin
clonidine
Ca ch blocker

diuretics can inhibit insulin secretion indirectly via depletion of K+

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21
Q

non-insulin anti-diabetic agents

A 
sulfonylureas, meglitinides
biguanides
thiazolidinediones
alpha-glucosidase inhibitors
incretin analogs
DPP-IV inhibitors 
amylin analogs
bile-acid sequestrants
SGLT-2 inhibitors
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22
Q

sulfonylureas

A

effective at reducing fasting plasma glucose and HbA1c

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23
Q

sulfonylurea MOA

A

stimulate insulin release from B cells

bind to SUR1 subunit - blocks ATP sensitive K+ channel in beta cell membrane

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24
Q

1st generation sulfonylurea

A

chlorpropamide

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25
Q

chlorpropamide

A

hypoglycemia common in elderly pt

hyperemic flush with alcohol (inhibition of aldehyde dehydrogenase)

can elicit SIADH - potentiates

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26
Q

2nd generation sulfonylurea

A

glyburide
glipizide
glimepiride

more potent than 1st generation
lack AE of 1st generation

overall have replaced 1st generation

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27
Q

glyburide

A

2nd generation - worst of three - causes hypoglycemia in users commonly

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28
Q

glipizide

A

shortest half life of potent agents

less likely to cause hypoglycemia

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29
Q

glimepiride

A

causes hypoglycemia in very very few pt’s

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30
Q

sulfonylurea AE

A

hypoglycemia

weight gain

31
Q

meglitinides

A

repaglinide
nateglinide

stimulate insulin release by SUR1 binding - inhibition of ATP sensitive K+ channel

(effect not as strong as sulfonylurea in reducing plasma glucose and HbA1c)

32
Q

meglitinides

A

rapid onset, short duration

postprandial glucose regulators

must be taken before meal

contain no sulfur - good for pt with sulfa allergy

33
Q

meglitinides AE

A

hypoglycemia – repaglinide
(less likely in nateglinide)

both have weight gain

34
Q

which meglitinide has a higher chance of hypoglycemia

A

repaglinide

35
Q

biguanides

A

metformin

does not increase insulin secretion or hypoglycemia

equivalent effect to sulfonylureas in reducing fasting glucose and HbA1c

36
Q

metformin MOA

A

1) inhibits gluconeogenesis inhibits GENE EXPRESSION of gluconeogenic enzymes - not direct inhibition of enzyme
2) increases insulin mediated glucose utilization in muscle and liver

– via activation of AMP-activated protein kinase
= insulin levels decline slightly

37
Q

metformin additional effects

A

dec plasma TG

dec body weight

38
Q

first line in NIDDM

A

metformin

can be used alone or in combo with sulfonylureas, Tzds, insulin

39
Q

metformin AE

A

mainly GI
may interfere with B12 absorption
fatal lactic acidosis

contraindicated with pt with renal disease, hepatic disease, hypoxia, alcoholism

40
Q

pioglitazone

A

thiazolidinediones

41
Q

rosiglitazone

A

thiazolidinediones

42
Q

thiazolidinediones

A

1) pioglitazone
2) rosiglitazone

“insulin sensitizers”

dec insulin resistance
agonist of PPAR-gamma (intracell receptors in muscle, fat, liver)

promotes glucose uptake and utilization
less effective than sulfonylureas and metformin in decreases FPG/HbA1c

43
Q

TZD PKA

A

because of gene regulation - slow onset of effect

44
Q

pioglitazone versus rosiglitazone

A

pioglitazone = greater improvements in HDL, TG, LDL size and concentration

45
Q

TZD AE

A 
fluid retention
exacerbation of CHF - spec class III or IV
46
Q

what is required to be monitored with TZD therapy

A

liver function

severe hepatic toxicity seen with first TZD released

47
Q

acarbose

A

alpha-glucosidase inhibitor

only one

48
Q

alpha-glucosidase inhibitor MOA

A

competitive inhibitor

1) dec postprandial digestion of starch and disacc
2) dec postprandial hyperglycemia and hyperinsulinemia
3) modest drop in HbA1c, FPG

49
Q

alpha-glucosidase inhibitor AE

A

GI

contraindicated in IBS, intestinal conditions

reversible hepatic enzyme elevation = requires LFT monitoring

50
Q

incretin analog

A

exenatide

glucagon like polypeptide-1 analog

51
Q

exenatide

A

GLP-1 analog

injectable

resistant to dipeptidyl peptidase IV

52
Q

exenatide MOA

A

1) enhances glucose dep insulin secretion
2) suppresses post prandial glucagon release
3) slows gastric emptying

used in NIDDM

53
Q

exentaide AE

A

n/v/d
acute pancreatitis
should not be used in pt with gastroparesis

54
Q

sitagliptin

A

DDP-IV inhibitor

increases circulating GLP-1 and insulin levels

improves glycemic control in adults with NIDDM

oral

55
Q

sitagliptin AE

A

pancreatitis

hypersensitivity (angioedema, anaphylaxis, stevens johnson)

56
Q

pramlintide

A

amylin analog - secreted with insulin from beta cells

inhibits food intake, gastric emptying, glucagon secretion

adjunct to insulin

57
Q

colesevelam

A

bile acid sequestrants

(lowers LDL cholesterol)

also used for NIDDM tx

oral

58
Q

Canagliflozin

A

SGLT-2 inhibitor

responsible for most reabsorption in PCT = BLOCKS - causing increased glucose excretion, dec blood glucose levels

oral

59
Q

canagliflozin AE

A

genital and UTIs

volume depletion d/t osmotic diuresis

inc serum creatinine

hyperkalemia, hypermagnesemia, hyperphosphatemia, hypotension

contraindicated in pt with GFR <45

60
Q

initial drug therapy for NIDDM

A

1st agent - metformin

only started if lifestyle intervention doesn’t reach HbA1c goals

61
Q

dual combination therapy

A

if monotherapy doesn’t reach goal at 3 months - second drug could be oral agent, exenatide, or insulin

(higher HbA1c = more insulin)

62
Q

triple combo therapy

A

most robust response will be with insulin - progressive beta cell loss - thus need to transition to inuslin

(favored when HbA1c >8.5%)

63
Q

transition to insulin

A

single injection of basal insulin

(either NPH, glargine, or detemir insulin can be used)

then uptitirate dose

if high postprandial glucose - add prandial insulin therapy with short acting (lispro, aspart, glulisine)

64
Q

most effective diabetic meds in lowering glycemia

A

insulin

65
Q

severe hyperglycemia

A

insulin used as initial therapy

1) significant hyperglycemic sxs
2) ketonuria
3) HbA1c >10%
4) random glucose >300

66
Q

DM and HTN tx

A

ACE-I or ARB

67
Q

antiplatelet agents in DM pt

A

ASA

68
Q

DM pt with albuminuria

A

ACE-I or ARB

69
Q

DM pt with neuropathic pain

A 
amitriptyline
pregabalin
gabapentin
duloxetine
venlafaxine
valproate
opioids
70
Q

DM pt with gastroparesis

A

metoclopramide

erythromycin

71
Q

DM pt with erectile dysfunction

A

PDE-5 inhibitors

72
Q

glucagon use

A

severe hypoglycemia (in pt taking insulin)

bowel radiology (relaxes intestine)

B blocker poisoning antidote

C-peptide test - testing residual beta cell function

73
Q

DOC for gestational DM

A

regular insulin

PHARM 3 (21 decks)

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