Flashcards in Final Review Deck (112)
Diabetic agents that cause pancreatitis?
Exenatide - GLP-1 (incretin) analog
Sitaglipitin - DPP-IV inhibitor (inhibits incretin break down)
Diabetic agents that liver function needs to be monitored?
TZDs (Pioglitazone and Rosiglitazone) - increase insulin sensitivity [Pioglitazone has a good lipid profile, both also cause fluid retention]
Acarbose - a-glucosidase inhibitor
Inhibits gluconeogenic enzymes via AMPK -- weight loss os common
AE - B12 def, lactic acidosis, possible disulfiram rxn (in the sense that alcohol causes hypoglycemia and metformin decrease glucose production)
Binds SUR1 subunit and blocks ATP-sensitive K+ channels
1st gen - Chlorpropamide -- watch for SIADH and DISULFIRAM rxn
2nd gen - Glyburide, Glipizide, Glimepiride
AE - infections and osmotic imbalance
Growth hormone antagonist
Somatostatin analog - inhibits release of GH, TSH, glucagon, Insulin and gastrin
45x more potent in inhibiting GH release compared to somatostatin
2x more potent in reducing insulin secretion
t1/2 = 80 minutes
Octreotide acetate - long acting suspension given at 4 week intervals
Clinical application - reduce hormone-secretion tumor symptoms, localize neuroendocrine tumors, acute control of bleeding from esophageal varices
AE - nausea, vomiting, abdominal cramps, flatulence, steatorrhea, constipation, biliary sludge, gallstones, sinus bradycardia, vit B12 def (with long term use), pain at injection site (common)
Ganirelix and Cetrorelix
Desmopressin and Vasopressin?
ADH analogs -- MINIMAL V1 affinity (SM cells on efferent)
1. DOC for diabetes insupidus
2. Esophageal bleeding and colonic diverticular bleeding (vasopressin)
3. Coagulopathy tx in hemophilia A and vWF disease (Desmopressin)
AE - headache, nausea, abdominal cramps, allergic reaction
Glucocorticoid agonists and antagonists?
Hydrocortisone (Cortisol) [equal amt of anti-inflammatory and salt-retaining activity]
Triamcinolone (aerosol) [no salt retaining ability]
Dexamethasone [no salt retaining ability]
Mineralocorticoid agonists and antagonists?
Agonists... Aldosterone and Fludrocortisone
Antagonists... Spirnolactone (watch out for hyperkalemia)
Tx of cerebral edema and Hodgkins Lymphoma?
Cerebral edema = dexamethasone
Hodgkin's lymphoma = prednisone
Desmolase inhibitor - used to block all adrenal cortex hormones (ex. adrenal cancer)
Ketoconazole in tx of cushings and prostate cancer?
Non-selective inhibitor - inhibits desmolase, 17 hydrox and 17,20 lyase
11B hydroxylase inhibitor -- tx PREGNANT women with cushings
AE... salt and water retention, hirsutism, transient dizziness, GI disturbances
B blockers used in the treatment of hyperthyroidism?
Propranolol, Nadolol, Esmolol (short acting)
MOA - competitive block of B receptors inhibiting conversion of T4 to T3
With pts with asthma, can be given calcium channels instead (diltiazem and verapamil) as alternatives.
Oral Diatrizoate and IV iohexol?
iodinated radiocontrat media that suppress the conversion of T4 to T3 (5-deiodinase) in the peripheral tissue, kidney and liver. It is useful in rapidly reducing the T3 concentration in thyrotoxicosis.
Perchlorate, thiocyanate, pertechnetate?
Rarely used antithyroid drugs that inhibit iodide concentration in the gland by blocking the transportation of iodine in to the thyroid gland.
Possible development of APLASTIC ANEMIA.
Drugs that may provoke autoimmune/destructive inflammatory thyroiditis which can induce hypothyroidism?
2. INF-a and IL-2
3. Lithium - inhibits release of hormones and thyroid enlarge (hypothyroidism)
4. imatinib, sunitnib (TKRI-tyrosine kinase receptor decrease)
5. aminoglutethimide, sulfonylurea
Prostaglandins used for cervical ripening; uterine contractions; postpartum hemorrhage?
Cervical ripening and contraction = misoprostol (PGE1), Dinoprostone (PGE2)
Postpartum hemorrhage = misoprostol and Carboprost Tromethamine (PGF2 analog give IM administration)
-partial a-agonist and some serotonin receptor activity
-tx postpartum hemorrhage
-ergot alkaloid [says erg in the name..]
-contraindicated if pt has CV or cardiac issues
Magnesium sulfate - uncouples excitation-contraction in myometrium inhibiting AP - may cause resp depression or cardiac arrest in mom or baby
Indomethacin - NSAID - may cause oligohydramnios and close PDA early
Nifedipine - Calcium channel blocker - safer than other tocolytics
Atosiban - oxytocin competitive antagonists - not approved in the US
B2 adrenoceptor agonist - phosphorylation of SmMKLCK inhibiting its interaction with calcium-calmodulin complex -- black box warning in the US as it may cause maternal death
Fibroblast growth factor-23?
Produced by osteoblasts and osteoclasts. FGF-23 inhibits calcitriol (activated vit D) production decreasing calcium and phosphate reabsorption in the kidneys and intestines.
*PTH stimulates calcitriol (1a-hydroxylase) activity in kidney whereas FGF-23 inhibits it
-low levels cause bone anabolism
-high levels cause bone catabolism
AE - hypercalcemia, hypercalciuria, osteosarcoma
19-nor-1,25 - dihydroxyvitamin D2
vit D derivative used to treat psoriasis
Suppresses activity of osteoclasts and inhibits bone resorption. It inhibits osteoclastic activity via decreasing farnesyl pyrophosphate synthesis by disrupting mevalonate pathway decreasing osteoclast H+ ATPase.
Uses - osteoporosis and Paget's disease
AE - adhynamic bone, esophageal irritation (risk reduced by drinking water and remaining in upright position for 30 minutes after taking medication), osteonecrosis of jaw
Ex. Risedronate, Ibandronate, Pamidronate, Zoledronate -- all very similar to aledronate
Monoclonal antibody that binds RANKL (rank ligand). Binding to the RANKL leads to inhibition of osteoclastic activity.
Uses - osteoporosis
Subcutaneous every 6 months
AE - increase risk of infections