Endocrine Pharmacology Flashcards
treatment strategies for type 1 diabetes mellitus
low carb diet insulin replacement
Ram
treatment strategies for type 2 diabetes mellitus
dietary modification and exercise for weight loss oral agents non insulin injectables insulin replacement
treatment strategies for gestational diabetes
dietary modifications exercise insulin replacement if lifestyle modification fails
name the 7 types of insuline
Lispro Aspart Glulisine regular NPH detemir glargine
which type of insulin is short acting?
only Regular insulin
which types of insulin are rapid acting?
Lispro
Aspart
Glulisine
“no LAG”
which insulins are intermediate acting?
only NPH
which insulins are long acting?
detemir
glargine
insulin, rapid acting–mechanism
binds insulin receptor (tyrosine kinase activity) rapidly, no LAG
liver: inc glucose stored as glycogen
muscle: inc glycogen, protein synthesis, inc K+ uptake
fat: inc triglyceride storage
insulin, rapid acting–use
Type I DM
type 2 DM
GDM (postprandial glucose control)
insulins, short acting–use
Type I DM
type 2 DM
GDM
DKA (IV)
hyperkalemia (+ glucose)
stress hyperglycemia
insulin, intermediate acting–use
Type 1 DM
type 2 DM
GDM
insulin, long acting–use
type 1 DM
type 2 DM
GDM (basal glucose control)
insulin–toxicity
hypoglycemia
lipodystrophy
rare hypersensitivity rxns
what drug is included in the drug class Biguanides and acts as an oral hypoglycemic drug?
metformin
biguanides–action
(metformin)
exact mechanism unknown
dec gluconeogenesis
inc glycolysis
inc peripheral glucose uptake (inc insulin sensitivity)
biguanides–use
(metformin)
oral
first line therapy in type 2 DM
causes modest weight loss
can biguanides (metformin) be used for patients w/o islet function?
yes (T1DM)
biguanides–toxicity
(metformin)
GI upset
most serious adverse rxn is lactic acidosis
when is biguanides (metformin) contraindicated?
renal insufficiency, b/c can lead to lactic acidosis
name the first generation sulfonylureas
chlorpropamide
tolbutamide
name the second generation sulfonylureas
glimepiride
glipizide
glyburide
sufonylureas–mechanism
close K+ channel in beta cell membrane –> cell depolarizes –> insulin release via inc Ca 2+ influx
sulfonylureas–use
stimulate release of endogenous insulin in type 2 DM
can sulfonylureas be used in type 1 DM?
no, becuase requires some islet fcn to work
sulfonylureas–toxicity
risk of hypoglycemia inc in renal failure
weight gain
first generation sulfonylureas–toxicity
disulfiram like effects
second generation sulfonylureas–toxicity
hypoglycemia
name glitazones/thiazolidinediones
pioglitazone
rosiglitazine
glitazones/thiazolidinediones–mechanism
inc insulin sensitivity in peripheral tissue
binds to PPAR-gamma nuclear transcription regulator which activates genes to regulate fatty acid storage and glucose metabolism
glitazones/thiazolidinediones–use
used as monotherapy in type 2 DM or combined with insulin, biguanides, or sulfonylureas
safe to use in renal impairment
glitazones/thiazolidinediones–toxicity
weight gain
edema
hepatotoxicity
HF
inc risk of fractures
name meglitinides
nateglinide
repaglinide
meglitinides–mechanism
stimulate postprandial insulin release by binding to K+ channels on beta cell membranes (different site than sulfonylureas)
meglitinides–use
used as a monotherapy in type 2 DM or combined with metformin
meglitinides–toxicity
hypoglycemia (inc risk with renal failure)
weight gain
name GLP-1 analogs
exenatide
liraglutide (SC injection)
GLP-1 analogs–mechanism
inc glucose dependent insulin release
dec glucagon release
dec gastric emptying
inc satiety
GLP-1 analogs–use
Type 2 DM
GLP-1 analogs–toxicity
nausea
vomiting
pancreatitis
modest weight loss
name the DPP-4 inhibitors
linagliptin
saxagliptin
sitagliptin
DPP-4 inhibitors–mechanism
inhibits DPP-4 enzyme that deactivates GLP-1, so…
inc glucose dependent insulin release
dec glucagon release
dec gastric emptying
inc satiety
DPP-4 inhibitors–use
Type 2 DM
DPP-4 inhibitors–toxicity
mild urinary or respiratory infections
weight neutral
name the amylin analogs
pramlintide (sc injection)
amylin analogs–mechanism
dec gastric empyting
dec glucagon
amylin analogs–use
Type 1 DM
type 2 DM
amylin analogs–toxicity
hypoglycemia (in setting of mistimed prandial insulin)
nausea
name the sodium glucose transporter 2 (SGLT-2) inhibitors
canagliflozin
dapagliflozin
empagliflozin
SGLT 2 inhibitors–mechanism
block reabsorption of glucose in PCT
SGLT 2 inhibitors–use
type 2 DM
SGLT 2 inhibitors–toxicity
glucosuria
UTIs
vaginal yeast infections
hyperkalemia
dehydration (ortostatic hypotension)
name the alpha glucosidase inhibitors
acarbose
miglitol
alpha glucosidase inhibitors–mechanism
inhibit intestinal brush border alpha-glucosidases
delayed carbohydrate hydrolysis and glucose absorption –> dec postprandial hyperglycemia
alpha glucosidase inhibitors–use
type 2 DM
alpha glucosidase inhibitors–toxicity
GI disturbances
name the thionamides
propylthiouracil (PTU)
methimazole
thionamides–mechanism
block thyroid peroxidase–inhibits the oxidation of iodide and organification (coupling) or iodine –> inhibition of thyroid hormone synthesis
what does propylthiouracil block and what is the result?
(thionamides)
blocks 5’-deiodinase
causes dec peripheral conversion of T4 to T3
thionamides–use
hyperthyroidism
propylthiouracil (PTU) blocks peripheral conversion and is used in pregnancy
thionamides–toxicity
skin rash
agranulocytosis (rare)
aplastic anemia
hepatotoxicity
adverse effect of methimazole
(thionamides)
possible teratogen–can cause aplasia cutis
drug names for T4 and T3
T4: levothyroxine
T3: triiodothyronine
levothyroxine, triiodothyronine–mechanism
thyroid hormone replacement
levothyroxine, triiodothyronine–use
hypothyroidism
myxedena
used off label as weight loss supplements
levothyroxine, triiodothyronine–toxicity
tachycardia, heat intolerance, tremors, arrhythmias
name the hypothalamic/pituitary drugs
ADH antagonists–conivaptan, tolvaptan
desmopressin acetate
GH
oxytocin
somatostatin (octreotide)
name 2 ADH Antagonists
conivaptan
tolvaptan
ADH antagonists–use
SIADH–block action of ADH at V2 receptor
desmopressin acetate–use
central (not nephrogenic) DI
GH–use
GH deficiency
turner syndrome
oxytocin–use
stimulate labor, uterine contractions, milk let down
controls uterine hermorrhage
somatostatin (octretide)–use
acromegaly
carcinoid syndrome
gastrinoma
glucagonoma
esophageal varices
demeclocycline–mechanism
ADH antagonist (member of tetracycline family)
demeclocycline–use
SIADH
demeclocycline–toxicity
nephrogenic DI
photosensitivity
abnormalities of bone and teeth
name the glucocorticoids
beclomethasone
dexamethasone
hydrocortisone
methlprednisolone
prednisone
triamcinolone
glucocorticoids–mechanism
metabolic, catabolic, anti-inflammatory, and immunosuppressive effect mediated by interactions with glucocorticoid response elements
inhibition of phospholipase A2
inhibition of transcription factors such as NK-kappaB
glucocorticoids–use
adrenal insufficiency
inflammation
immunosuppression
asthma
glucocorticoids–toxicity
iatrogenic cushing syndrome
adrenocortical atrophy
peptic ulcers
steroid diabetes
steroid psychosis
cataracts
adrenal insufficiency if stop drug abruptly after chronic use
Iatrogenic Cushing Syndrome
HTN
weight gain
mon facies
truncal obesity
buffalo hump
thinning of skin
striae
acne
osteoporosis
hyperglycemia
amenorrhea
immunosuppression
fludrocortisone-mechanism
synthetic analog of aldosterone with little glucocorticoid effects
fludrocortisone–use
mineralocorticoid replacement in primary adrenal insufficiency
fludrocortisone–toxicity
similar to glucocorticoids
edema
exacerbation of heart failure
hyperpigmentation
cinacalcet–mechanism
sensitizes Ca2+ sensing receptor (CaSR) in parathyroid gland to circulating Ca2+ –> dec PTH
cinacalcet–use
primary or secondary hyperparathyroidism
cinacalcet–toxicity
hypocalcemia
