pharm endo titus info.txt

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  1. Nonsteroidal Androgen Antagonists MOA
    antagonize androgen receptors in prostate tissue, blocking the action of DHT and reducing prostate growth. enzalutamide is the only pure antagonist (others such as bicalutamide exhibit some degree of AR agonist activity).
  2. Nonsteroidal Androgen Antagonists kinetics
    bicalutimade is preferred agent over flutamide due to its longer half life (T1/2 of 1 week means it is dose daily instead of TID like flutamide)
  3. Nonsteroidal Androgen Antagonists indications
    metastatic prostate cancer (palliative not curative)
  4. Nonsteroidal Androgen Antagonists contraindications
    hepatic impairment (hepatically metabolized)
  5. Nonsteroidal Androgen Antagonists side effects
    antiandrogenic (breast pain, gynecomastia, hot flashes), also hematuria, asthenia, and rash. flutamide severe diarrhea. nilutamide disulfiram-like reaction c alcohol.
  6. Androgens MOA
    mimic the actions of testosterone
  7. Androgens kinetics
    oral preparations undergo extensive first-pass metabolism. testosterone esters are more lipophilic, so are well absorbed in fat (injections). 17a-alkylated androgens aren't really used because, while they show reduced hepatic metabolism, they are less androgenic and more hepatotoxic.
  8. Androgens indications
    male hypogonadism, low libido, heavy menstrual bleeding.
  9. Androgens contraindications
    prostate cancer (androgens stimulate growth of prostate tissue)
  10. Androgens side effects
    fluid retention due to mild mineralcorticoid effect (androgens related to aldosterone). masculinization/amenorrhea in women.
  11. Androgen abuse
    CNS (aggression, depression), cardiovascular (HTN, athersclerosis, hypertrophy/fibrosis, sudden death), male endocrine (testicular atrophy, decreased sperm count, increased abnormal sperm, infertility), hepatic (increased liver enzymes, gallstones), musculoskeletal (short stature, tendon rupture), and skin effects (acne, baldness).
  12. Somatostatin Analogs MOA
    mimic the actions of somatostatin, which causes inhibition of hormone release in the anterior pituitary (GH, TSH), pancreas (glucagon, insulin), and GI (including gastrin, motilin, and VIP). they have a net effect of inhibiting growth/cell reproduction/cell regeneration.
  13. Somatostatin Analogs kinetics
    these are peptides -- must be injected (would be digested if given PO)
  14. Somatostatin Analogs indications
    suppression of other hormones (GH in acromegaly, VIP in carcinoid tumors, insulin or glucagon in islet cell tumors), variceal bleeding, s/p pancreatic surgery (reduce pancreatic secretions), severe refractory chemotherapy-induced diarrhea, hepatorenal syndrome
  15. Somatostatin Analogs contraindications
    caution with DM type 1 (can result in hypoglycemia due to altered glucose metabolism)
  16. Somatostatin Analogs side effects
    cardiovascular (bradycardia), GI (abdominal pain, N/D), CNS (HA, fatigue)
  17. Growth Hormone Antagonists MOA
    block the action of growth hormone at the GH receptor in the liver. this blocks the release of IGF-1, effectively blocking growth in bone and soft tissues.
  18. Growth Hormone Antagonists kinetics
    created by adding PEG-500 to GH, increasing T1/2 from 30 min to 2 days. this is a peptide -- must be injected (would be digested if given PO).
  19. Growth Hormone Antagonists indications
    acromegaly (GH-secreting pituitary adenoma), pts with elevated IGF-1
  20. Growth Hormone Antagonists contraindications
    hepatic impairment
  21. Growth Hormone Antagonists side effects
    elevated liver enzymes in 25%. CNS (pain), infection, flu-like syndrome.
  22. Adrenocorticotropic Hormones MOA
    analogous to hormone secreted by anterior pituitary that acts on the adrenal cortex, resulting in cortisol production.
  23. Adrenocorticotropic Hormones kinetics
    T1/2 of 10 minutes.
  24. Adrenocorticotropic Hormones indications
    diagnosis of adrenocortical insufficiency
  25. Adrenocorticotropic Hormone deficiency treatment
    mineralocorticoid deficiency (low aldosterone) is treated with fludrocortisone acetate. cortisol deficiency is treated with glucocorticoids.
  26. Thyroid Replacement MOA
    Supplement endogenous thyroxine (T4) supply. Some of the thyroxine is converted to triiodothyronine (T3 -- the more potent form) and rT3 (unknown significance) by monodeiodination in peripheral tissues.
  27. Thyroid Replacement kinetics
    T4 is the preferred replacement because it has a longer T1/2 (1 week -- so can be administered daily). Steady-state levels require about 35 days. Take on empty stomach x 30-60min (food/drink decrease absorption). T4 over 99% protein bound (TGB -- thyroid binding globulin).
  28. Thyroid Replacement indications
    hypothyroidism, myxedema coma (administer IV)
  29. Thyroid Replacement contraindications
    conditions where tachycardia is dangerous (CAD, aortic/mitral stenosis) (T4 has a lower potential for cardiotoxicity than T3)
  30. Thyroid Replacement interactions
    levothyroxine + inhibitors of 5'-deiodinase (corticosteroids, severe illness, starvation, amiodarone, iodinated contrast media) (5'-deiodinase converts T4 to T3; if it is inhibited, more is converted to rT3)
  31. Thyroid Replacement side effects
    hyperthyroidism, cardiac toxicity (especially T3), tachycardia, a-fib
  32. Antithyroids MOA
    thioamides block the synthesis of thyroid hormone by inhibiting thyroid peroxidase (liberates iodine for addition to tyrosine). ablative agents destroy the gland through radiation (thyroid takes up radioactive iodine, which gives off radiation that penetrates 2 mm around).
  33. Antithyroids kinetics
    thioamides require 3-4 weeks to see an effect because of precursor storage. carbimazole is a prodrug that is converted to methimazole.
  34. Antithyroids indications
    hyperthyroidism. PTU only for those intolerant of methimazole. radioactive iodine also thyroid cancer.
  35. Antithyroids contraindications
    pregnancy (thioamides caution as they penetrate placenta, ablative agents absolute because they will kill the fetal thyroid). children (ablative agents caution due to small increased risk of cancer).
  36. Antithyroids side effects
    thioamides rash, fever, arthralgias, and rarely agranulocytosis, hepatotoxicity, vasculitis. ablative agents rarely cancer, sialadenitis (inflammation of salivary gland) -- take radiations precautions! (avoid kids, pregnant women)
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pharm endo titus info.txt
2012-12-11 22:17:42
pharm endo titus info

pharm endo titus info.txt
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