B5-003 Diabetes Mellitus Drugs Flashcards
bind receptors to:
* increase glucose storage as glycogen in liver
* increase glycogen and protein synthesis in muscle
* increase TG storage in fat
* increase K+ uptake at the cell membrane
what drug class
insulin preparations
rapid acting insulin preparations
Lispro
Aspart
Glulisine
no LAG
intermediate acting insulin preparation
NPH
long acting insulin preparations
determir
glargine
very long acting insulin preparation
degludec
adverse effects of insulin preparations
4
- hypoglycemia
- lipodystrophy
- hypersensitivity rxn
- weight gain
inhibits mGPD causing the inhibition of hepatic gluconeogenesis and the action of glucagon
metformin
increases glycolysis, peripheral glucose uptake, and insulin sensitivity
metformin
adverse effects of metformin
- GI upset
- lactic acidosis (caution with renal insufficiency)
- B12 deficiency
- weight loss
- activates PPAR-y to increase insulin sensitivity and levels of adiponectin
- leads to regulation of glucose metabolism and FA storage
pioglitazone
adverse effects of pioglitazone
- weight gain
- edema
- HF
- increased risk of fractures
pioglitazone has a delayed onset of action of […]
duration
several weeks
what 2 drugs work to increase insulin sensitivity
pioglitazone
metformin
what drugs work to increase insulin secretion?
2 groups
sulfonylureas
meglitinides
close K+ channels in pancreatic B cell membrane causing the cell to depolarize and increasing insulin release via the Ca+ influx
sulfonylureas
meglitinides
1 gen sulfonylureas
2
chlorpropamide
tobutamide
2nd gen sulfonylureas
2
glipizide
glyburide
meglitinides
2
nateglinide
repaglinide
adverse effect of 1st gen sulfonylureas
disulfram-like reaction
rarely used
adverse effects of 2nd gen sulfonylureas and meglitinides
- hypoglycemia (greater in renal insufficiency)
- weight gain
what drug classes work to increase glucose-induced insulin secretion?
GLP-1 analogs
DPP-4 inhibitors
- decrease glucagon release
- delay gastric emptying
- increase glucose-dependent insulin release
- decrease appetite
GLP-1 analogs
adverse effects of GLP-1 analogs
- nausea/vomiting
- pancreatitis
- weight loss
- increased satiety
GLP-1 analogs
3
exenatide
liraglutide
semaglutide
-glutide
DPP-4 inhibitors
3
linagliptin
saxagliptin
sitagliptin
inhibit enzyme that deactivates GLP-1, giving similar effects as GLP-1 analogs
DPP-4 inhibitors
adverse effects of DDP-4 inhibitors
- RTIs and UTIs
- pancreatitis
- weight neutral
- increased satiety
what drug classes work to decrease glucose absorption?
2
SGLT2 inhibitors
a-glucosidase inhibitors
-flozins
SGLT2 inhibitors
-gliptin
DDP-4 inhibitors
-glinide
meglitinides
block reabsorption of glucose in proximal convoluted tubule
SGLT2 inhibitors
adverse effects of SGLT2 inhibitors
- glucosuria (UTI, GU infection)
- dehydration –> hypotension
- weight loss
- caution with renal insufficiency
a-glucosidase inhibitors
2
acarbose
miglitol
- inhibit intestinal brush-border enzymes causing delayed carbohydrate hydrolysis and glucose absorption
- decreases postprandial hyperglycemia
a-glucosidase inhibitors
adverse effects of a-glucosidase inhibitors
GI upset- flatulence, bloating, etc
pramlintide is a
amylin analog
Pramlintide
decreases glucagon release and delays gastric empyting
promotes satiety
pramlintide
adverse effects of pramlintide
- hypoglycemia
- nausea
- increased satiety
which medications are not recommended in renal insufficiency?
4
- a-glucosidase inhibitors
- SGLT2 inhibitors
- meglitinides, sulfonylureas
- metformin
goal
fasting glucose:
2 hr post prandial:
HbA1C:
fasting glucose: 90-120
2 hr post prandial: below 150
HbA1C: 7
- takes a couple hours to reach peak
- effective for about 6 hrs
which type of insulin
short (regular)
- onset within 30-45 min
- shorter duration of action
which type of insulin
rapid acting
no LAG
- slower onset
- duration of about 12 hrs
which type of insulin
intermediate NPH
very long half lives to stabilize insulin long term
which type of insulin
long acting
treatment of DKA
IV insulin (0.1) + glucose to prevent hypoglycemia
fluids and electrolytes
bind to SUR1 to close the K/ATP channel
sulfonylureas
meglitinides
bind to SUR1 with higher affinity so less dose required
sulfonylureas Gen 2
contraindications of sulfonylureas
- DM1
- pregnancy/breastfeeding
- significant hepatic/renal insufficiency
really cheap DM2 option
sulfonylureas
-glinide
meglitide
first line therapy for DM2
metformin
-glitazone
thiazolidinediones
PPARy agonists with PPARa agonist activity
thiazolidinediones
removed from market due to hepatotoxicity
troglitazone
- promote transport of serum lipids to adipose
- promote insulin sensitivity
thiazolidinediones
adverse effects of thiazolidinediones
- weight gain
- hepatotoxicity
- CHF
incretins (GLP and GIP) are released from L cells in the
ileum
-glutide
GLP-1 analog
GIP analog that activates both GLP-1 and GIP receptors
tirezepatide
mounjaro
principles of combination therapy
- different MOA
- target different proteins
advantages: lower doses, fewer adverse effects
options for DM 2 monotherapy
4
- metformin
- GLP-1
- SGLT2
- DDP-4
add others as needed to get target A1C, add insulin last if needed
second choice agents in DM2 therapy
2
sulfonylureas
TZDs
metformin requires […] daily dosing
twice
sulfonylureas and DDP4i offer […] daily dosing
once
what drug classes are contraindicated in patients with a hx of pancreatitis?
GLP-1 and DPP-4i
inhibits GI glycosidases leading to an increas in the accumulation of complex sugars in the GI tract
a-glucosidase i
cause flatulence and diarrhea
a-glucosidase inhibi.
has a sulfonamide structure and is contraindicated in patients with sulfa allergies
glyburide