pharm 1 liner- endocrine Flashcards
recombinant growth hormone used in growth hormone deficiency
somatropin
somatostatin analog used for acromegaly, carcinoid, glucagonoma and other growth hormone producing pituitary tumors
octreotide
gonadotropin-releasing hormone (GnRH) analog used for infertility (agents with pulsatile admin), or uterine fibroids and endometriosis (antagonist with continuous admin to suppress gonadotropin production and down regulate GnRH receptor in pituitary)
leuprolide
competitive antagonists at gonadotropin releasing hormone receptors used to prevent LH surge during controlled ovarian hyper stimulation
ganirelix
Ergot dopamine agonist inhibits lactotroph cell growth and prolactin secretion that can be used to treat prolactinoma
bromocriptine
Synthetic human corticotropin used for diagnosis of adrenal insufficiency
cosyntropin
Agent used to stimulate uterine contraction and labor, milk letdowns, and control postpartum bleeding
oxytocin
Agent of choice for the treatment of hypothyroidism
levothyroxine (T4)
Mechanism of Levothyroxine
L-isomer of T4
Adverse effects of Levothyroxine
palpitations, arythmies, excessive sweating, heat intolerance
An isomer of T3 which may be used in myxedema coma
liothyronine (T3)
Thioamide agents used in hyperthyroidism
methimazole and propylthiouracil (PTU)
Thioamide extensively protein bound, less likely to cross placenta, inhibits peripheral conversion of T4 to T3 in high doses, and indicated for pregnant women in 1st trimester
propylthiouracil
Propylthiouracil (PTU) mechanism of action
inhibits thread peroxidase; blocks peripheral T4 to T3 conversion
A severe adverse effect of thioamide
agranulocytosis
Can be effective for short term therapy of thyroid storm, but after several weeks of therapy causes an exacerbation of hyperthyroidism
iodide salts (potassium iodide)
Permanently cures thyrotoxicosis, patients will need thyroid replacement therapy thereafter. Contraindicated in pregnancy
radioactive iodine
Used for the symptomatic treatment of thyrotoxicosis by blocking cardiac adverse effects as well as blocking peripheral T4 to T3 conversion
beta blockers such as propranolol and esmolol
Used for Addison’s disease, congenital adrenal hyperplasia inflammation, immune suppression, and asthma
glucocorticoids
Two short-acting glucocorticoids
hydrocortisone (cortisol), cortisone
Four intermediate-acting glucocorticoids
prednisone, predisolone, methylprednisolone, triamcinolone
Two long-acting glucocorticoids
betamethasone, dexamethasone
Two glucocorticoids with mineralocorticoid action
fludrocortisone, deoxycortisterone
Side effects of corticosteroids
Iatrogenic Cushing’s syndrome, hyperglycemia, impaired wound healing, osteoporosis, peptic ulcers, myopathy, adrenal suppression (> 2 week treatment)
Inhibits conversion of cholesterol to pregnenolone therefore inhibiting corticosteroid synthesis
aminoglutethimide
antigfungal agent used to inhibit adrenal and gonadal sterior synthesis
ketoconazole
selective inhibitor of 11-hydroxylation and interferes with cortisol and corticosterone synthesis; used for adrenal function tests and is the only adrenal-inhibiting medication that can be admin to pregnant women with bushings syndrome
metyrapone
Progesterone receptor antagonist used to induce abortion blocks glucocorticoid receptor at higher concentration
mifepristone (RU486)
Three rapid-acting insulin used for postprandial glycemia
aspart, lidpro, glulisine
Short-acting insulin used intravenously for ketoacidosis
regular insulin
Intermediate-acting insulin with variable pharmacokinetics; use is mostly replaced by long-acting insulin
neutral protamine hagedorn (NPH) insulin
Two long-acting insulin preparations that provide basal glycemia control
glargine, determir
Major side effect of insulin
insulin
Insulin receptor has
tyrosine kinase activity
first generation sulfonylurea that is relatively safe for elderly diabetics and patients with renal impairment due to its short half-life
tolbutamide
First generation sulfonylurea contraindicated in elderly diabetics because of prolonged long half-life
chloropropamide
Three second generation sulfonylureas
glyburide, glipizide, glimepiride
mechanism of action of sulfonylureas
Close K+ channels in beta cell membrane, depolarize cell, open voltage-gated Ca2+ channels, influx of Ca2+ release preformed insulin
Side effect specific to first generation sulfonylureas
disulfiram-like reactions with alcohol use
Second generation sulfonylureas is more potent than 1st generation and can eaily cause
hypoglycemia
Both first and second generation of sulonylureas can cause
allergy (sulfa)
How do Sulfonylureas affect body weight that is mediated by the insulin effects on adipose tissue
weight gain
A meglitinide insulin secretagogue that has no sulfur in its structure and may be used in type 2 diabetics with sulfonylurea allergy
repaglinide
A D-phenylalanine derivative insulin secretagogue that is useful for type 2 diabetics with very reduced renal function or elderly patients
nateglinide
mechanism of action of repaglinide and nateglinide
Close K+ channels, depolarize cell, open voltage-gated Ca2+ channels, release preformed insulin
First line drug for the treatment of type 2 diabetes mellitus
metformin
Mechanism of action of metformin
gluconeogenesis, peripheral glucose uptake; increase insulin sensitivity
Most serious side effect of metformin
lactic acidosis
Metformin is contradindicated in
renal insufficiency
The most common side effect of metformin is
GI distress/upset
Two thiazolidinediones
pioglitazone, rosiglitazone
Mechanism of action of thiazolidinediones
Activate PPAR-ɣ, transcription of insulin-responsive genes, GLUT4 glucose transporter, insulin sensitivity
Side effect of thiazolidinediones
Weight gain, edema, heart failure,macular edema, hepatotoxicity
Two alpha-glucosidase inhibitors
acarbose, miglitol
mechanism of a action of alpha-glucosidase inhibitors
Act on intestinal brush boder α-glucosidase, delay digestion and absorption of glucose, ↓post-prandial blood glucose
α-glucosidase inhibitors are contraindicated in
inflammatory bowel disease
Side effect of alpha-glucosidase inhibitors
flatulence, diarrhea, abdominal cramps
Four glucagon-like polypeptide-1 (GLP-1) analogs that increase insulin secretion and suppress postprandial glucagon release
eventide, liraglutide, albiglutide, dulaglutide
The most common side effect of GLP-1 analogs
nausea, vomiting
Three dipeptidyl peptidase-4 (DPP-4) inhibitors that reduce breakdown of glucagon-like polypeptide-1, resulting in increased insulin secretion and suppress postprandial glucagon release
citagliptin, saxagliptin, linagliptin
Oral antidiabetic drugs can increse the risk of UTI and respiratory infection
DPP-4 inhibitors
Amylin analog that delays gastric emptying and suppresses glucagon release
pramlinitide
Three sodium-glucose transporter 2 (SGLT2) inhibitors
canagliflozin, dapagliflozin, empagliflozin
Mechanism of action of sodium-glucose transporter 2 (SGLT2) inhibitors
inhibit SGLT2 and decrease glucose resorption in proximal collecting tubules
Main side effects of SGLT2 inhibitors
glycosuria, genital infections, UTI
SGLT2 inhibitors causes orthostatic hypothension due to
diuresis by glucose leading to dehydration
bisphosphonates
alendronate and -dronates
mechanism of action of bisphosphonates
inhibitors osteoclast activity and prevent bone resorption
uses of bisphosphonates
osteoporosis, parents disease, hypercalcemia
major side effects of bisphosphonates
corrosive esophagitis, osteonecrosis of jaw
first generation bisphosphonate when used long term causes osteomalacia
etidronate
may be used intranasal to decrease bone resorption
calcitonin (salmon prep)
vitamin given with calcium to ensure proper absorption (bone)
vitamin D
