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54 Cards in this Set

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  • Back
What is the mechanism of action of Propylthiouracil and methimazole?
Inhibits organification of I --> I2, and inhibits coupling of thyroid hormone synthesis. So cant combine DIT + DIT or MIT with DIT.
This drug can inhibit organification and coupling of thyroid hormones. It also decreases peripheral converstion of T4 to T3
What are the main side effects of PTU and methimazole?
Skin rash
Aplastic anemia
What is the effect of radioactive iodine?
It is taken up by thyroid follicular cells and emits beta particle destroying thyroid follicular cells.
MC side effect of radioactive iodine?
Hypothyroidism. So patient would need to take levothyroxine
What does levothyroxine (T4) do?
T4 is converted into T3 at the target tissue.
What are the clinical useses of levothyroxine and triiodothyronine?
Hypothyroidism and myxedema
What are the side effects of levothyroxine?
Tachycardia, heat intolerance, tremors.
How long does it take for levothyroxine and T3 to work and achieve a steady state?
6-8 weeks
What can be used to treat thyroid storm?
Iodine because it inhibits the iodination of tyorisine. After several weeks, however, the thyroid gland will nto respond to iodide treatment, so this agent is used only in short term therapy. Also can use PTU because it blocks peripheral conversion of T4 to T3.
What are some long acting glucocorticoids?
Bethamethasone and Dexamethsaone
What are some indications for using glucocorticoids?
Inflammation, allergies, asthma, and replacement therapy for adrenocortical insufficiency and CAH.
What is the mechanism of action of glucocorticoids?
Binds to intracellular cytoplasmic receptors causing change in gene transcription and causing a physiologic response.
What are some effects of glucocorticoids?
Causes neutrophilia, decreases lymphocytes in the blood, stimulates gluconeogenesis, stimulates protein catabolism to incresae amino acids, and inhibits phospholipase A2.
Side effects of glucocorticoids
Adrenal suppression, Muscle wasting, Osteoporosis, hyperglycemia, increased susceptibility to infections.
What can happen if you use steroids chronically and then abruptly stop the drug?
Can lead to adrenal insufficiency leading to hypotension and shock.
What is dexamethasone used for?
Used in cerebral edema because it has long half-life in the CNS
Where is bethamethasone used?
Used in preterm labor to induce fetal lung surfactant synthesis
Fludrocortisone mechanism
Acts on distal renal to increase sodium reabsorption and K+ secretion. Use in Addison's disease or salt wasting syndrome.
What is cell mechanism of vasopressin (ADH) and desmopressin?
Binds to V2 receptors on kidneys' collecting tubules leading to increased water reabsorption. It can also act on V1 in vascular smooth muscle, causing headaches, bronchoconstriction, and tremor..
What conditions are vasopressin contraindicated in?
CHF, asthma, epilepsy; Used in central DI; NOT nephrogenic!!!!
What are the toxicities associated with vasopressin?
Water intoxication and hyponatremia.
What is the action of oxytocin?
Stimulates smooth muscle contraction in the uterus, cervix, and myoepithelial cells.
What are the indications to use oxytocin?
Controls hemorrhage after labor, used in incomplete abortion, and milk let-down.
What are the side effects of oxytocin?
water retention and hyponatremia, uterine rupture, and hypertensive crisis.
What are the indications to use somatostatin and octeotride?
Diarrhea due to VIP and acromegaly, carcinoid, gastrinoma, or glucagonoma.
What is mechanism of octeotride?
Somatostatin analog that blocks GH, TRH, Glucagon, insulin, VIP, secretin, and seretonin.
When do you use Growth Hormone?
For patients with GH deficiency and Turner's syndrome? XO
What is the mechanism of orlistat?
Alters fat metabolism by inhibiting pancreatic lipases. Without pancreatic cant convert TG --> FFA + glycerol, so cant absorb FFA, and are excreted undgisted.
What is the clinical use of orlistat?
Long-term obesity management
What is toxicity of orlistat?
Steatorrhea, GI discomfort, reduced absorption of fat-soluble vitamins (A, D, E, K, headache.
What is the mechanism of subitramine?
Serotinin and NE reuptake inhibitor.
What is subitramine used for?
Short term and long term obesity management.
What is the toxicity of subitramine?
HTN and tachycardia
What are the short acting Insulin agent?
Lispro, Aspart, and Regular Insulin. Short acting preparations are typically injected before meals to mimic physiologic bolus of insulin.
When are intermediate and long acting insulin agents given?
Typically given at bed time to mimic basal insulin output seen in normal individuals. NPH is intermediate acting. Lente and Ultralente are long acting.
What is the mechanism of insulin?
A) Increases storage of glucose as glycogen in the liver.
B) Facilitates TG storage.
C) Decreases intracellular lipolysis
D) Stimulates glycogen and protein synthesis in muscle
E) Stimulates K+ uptake in muscle.
What is the toxicity of insulin?
Hypoglycemia and hypokalemia
What is so special about insulin glargine?
It has rapid onset of action, relatively constant rate of release (no troughs or peaks), and long duration of action!
What are the first generation sulfonylureas?
Tolbutamide and Chlorpropamide (TC)
What are the second generation sulfonylureas?
Glyburide, Glimiperide, and Glipizde (GGG)
What is the mechanism of action of sulfonylureas?
1. Binds to Sulfonyureal receptors on B cell causing closure of K+ channel. This leads to depolarization and subsequent Calcium influx leading to insulin release.
What are the toxicities of sulfonylureas?
Can lead to hypoglycemia, hypokalemia, and sulfa allergy.
What are the contraindications of glyburide?
Because it is a sulfonylurea, it cannot be used in pregnant women becuase it can cross the placenta and deplete insulin from the fetal pancreas.

2. Also contraindicated in renal or hepatic insufficiency because its accumulation can lead to hypoglycemic episodes.
What is one example of a biguanide?
What is the action of metformin?
It inhibits gluconeogenesis in the liver!
What is the main side effect of metformin?
It causes anion-gap metabolic acidosis.
Why is the importance of metformin?
It actually lowers weight, so it is considered the hardcore drug of choice in newly diagnosed type II diabetes. And it does NOT produce allergy to sulfa drugs.
What is the mechanims of action of glitazones?
It increases cell response to insulin
What are the side effects of glitazones (rosiglitazone and pioglitazone)?
Weight gain and hepatotoxicity!
What are some examples of alpha-glucosidase inhibitor?
Acarbose and Miglitol
What is the mechanism of action of acarbose and miglitol?
Inhibits alpha-glucosidase which normally hydrolyzes polysacchardies. Inhibiting this enzyme leads to decreased absorption of starches and polysacchardies and a decreased plasma glucose after a meal?
What are the side effects of acarbose?
NOT hypoglycemia. It causes flatulence, diarrhea, and abdominal cramping!
Consumption of alcohol while taking this drug can cause a disulfuram-like reaction (severe nause/vomiting) and hypotension?
Chlorpropamide: a first generation sulfonylurea