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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
chlorpropamide
hypoglycemia common in elderly pt hyperemic flush with alcohol (inhibition of aldehyde dehydrogenase) can elicit SIADH - potentiates
26
2nd generation sulfonylurea
glyburide glipizide glimepiride more potent than 1st generation lack AE of 1st generation overall have replaced 1st generation
27
glyburide
2nd generation - worst of three - causes hypoglycemia in users commonly
28
glipizide
shortest half life of potent agents | less likely to cause hypoglycemia
29
glimepiride
causes hypoglycemia in very very few pt's
30
sulfonylurea AE
hypoglycemia | weight gain
31
meglitinides
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
meglitinides
rapid onset, short duration postprandial glucose regulators must be taken before meal contain no sulfur - good for pt with sulfa allergy
33
meglitinides AE
hypoglycemia -- repaglinide (less likely in nateglinide) both have weight gain
34
which meglitinide has a higher chance of hypoglycemia
repaglinide
35
biguanides
metformin does not increase insulin secretion or hypoglycemia equivalent effect to sulfonylureas in reducing fasting glucose and HbA1c
36
metformin MOA
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
metformin additional effects
dec plasma TG | dec body weight
38
first line in NIDDM
metformin can be used alone or in combo with sulfonylureas, Tzds, insulin
39
metformin AE
mainly GI may interfere with B12 absorption fatal lactic acidosis contraindicated with pt with renal disease, hepatic disease, hypoxia, alcoholism
40
pioglitazone
thiazolidinediones
41
rosiglitazone
thiazolidinediones
42
thiazolidinediones
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
TZD PKA
because of gene regulation - slow onset of effect
44
pioglitazone versus rosiglitazone
pioglitazone = greater improvements in HDL, TG, LDL size and concentration
45
TZD AE
``` fluid retention exacerbation of CHF - spec class III or IV ```
46
what is required to be monitored with TZD therapy
liver function severe hepatic toxicity seen with first TZD released
47
acarbose
alpha-glucosidase inhibitor | only one
48
alpha-glucosidase inhibitor MOA
competitive inhibitor 1) dec postprandial digestion of starch and disacc 2) dec postprandial hyperglycemia and hyperinsulinemia 3) modest drop in HbA1c, FPG
49
alpha-glucosidase inhibitor AE
GI contraindicated in IBS, intestinal conditions reversible hepatic enzyme elevation = requires LFT monitoring
50
incretin analog
exenatide | glucagon like polypeptide-1 analog
51
exenatide
GLP-1 analog injectable resistant to dipeptidyl peptidase IV
52
exenatide MOA
1) enhances glucose dep insulin secretion 2) suppresses post prandial glucagon release 3) slows gastric emptying used in NIDDM
53
exentaide AE
n/v/d acute pancreatitis should not be used in pt with gastroparesis
54
sitagliptin
DDP-IV inhibitor increases circulating GLP-1 and insulin levels improves glycemic control in adults with NIDDM oral
55
sitagliptin AE
pancreatitis hypersensitivity (angioedema, anaphylaxis, stevens johnson)
56
pramlintide
amylin analog - secreted with insulin from beta cells inhibits food intake, gastric emptying, glucagon secretion adjunct to insulin
57
colesevelam
bile acid sequestrants (lowers LDL cholesterol) also used for NIDDM tx oral
58
Canagliflozin
SGLT-2 inhibitor responsible for most reabsorption in PCT = BLOCKS - causing increased glucose excretion, dec blood glucose levels oral
59
canagliflozin AE
genital and UTIs volume depletion d/t osmotic diuresis inc serum creatinine hyperkalemia, hypermagnesemia, hyperphosphatemia, hypotension contraindicated in pt with GFR <45
60
initial drug therapy for NIDDM
1st agent - metformin | only started if lifestyle intervention doesn't reach HbA1c goals
61
dual combination therapy
if monotherapy doesn't reach goal at 3 months - second drug could be oral agent, exenatide, or insulin (higher HbA1c = more insulin)
62
triple combo therapy
most robust response will be with insulin - progressive beta cell loss - thus need to transition to inuslin (favored when HbA1c >8.5%)
63
transition to insulin
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
most effective diabetic meds in lowering glycemia
insulin
65
severe hyperglycemia
insulin used as initial therapy 1) significant hyperglycemic sxs 2) ketonuria 3) HbA1c >10% 4) random glucose >300
66
DM and HTN tx
ACE-I or ARB
67
antiplatelet agents in DM pt
ASA
68
DM pt with albuminuria
ACE-I or ARB
69
DM pt with neuropathic pain
``` amitriptyline pregabalin gabapentin duloxetine venlafaxine valproate opioids ```
70
DM pt with gastroparesis
metoclopramide | erythromycin
71
DM pt with erectile dysfunction
PDE-5 inhibitors
72
glucagon use
severe hypoglycemia (in pt taking insulin) bowel radiology (relaxes intestine) B blocker poisoning antidote C-peptide test - testing residual beta cell function
73
DOC for gestational DM
regular insulin

PHARM 3 (21 decks)

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