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Pharm Exam III
Calcium & Bone Rx's, Adrenal Steroids, Reprod. Hormone Tx's
| Question | Answer |
|---|---|
| What is Alendronate's trade name? | Fosamax |
| What is Alendronate's class? | Bisphophanate |
| What are some contraindications of bisphosphanates? | Do not take if: cannot sit or stand for 10-15 min, have esophageal dysmotility, kidney disease, low blood calcium, |
| What is the drug class bisphosphonates' mechanism of action? | Inhibiting osteoclast action and resorption of bone |
| How do bisphosphonates inhibit osteoclast activity? | Most important: prevent the attachment of osteoclast precursor cells to bone and also dec. metabolic activity of osteoclasts and their ability to resorb bone |
| How are bisphosphonates administered? | P.O. |
| What percentage of bisphophonate drugs are absorbed? | <5% if prior to eating and even less if already eaten |
| What instructions should be given to patients taking bisphophonates? | Take on an empty stomach with a full glass of water in the a.m. |
| Why do patients have to be upright after ingesting a bisphophonate? | To avoid esophageal erosion |
| What is Alendronate's and Risedronate's indication? | Paget's disease of bone, hypercalcemia and osteolytic bone lesions of mets |
| What is the difference between Aledronate and Risedronate? | Alendronate can cause mild, transient nausea, dyspepsia, constipation or diarrhea |
| How have the issues of gastric and esophageal irritation been diminished? | w/ once weekly, monthly, annual dosing regimens |
| In what patients does severe suppression of jaw bone turnover or osteonecrosis occur as a complication of bisphosphonate therapy? | In women with cancer |
| What is a calcimimetic drug? | Cinacalcet |
| What is the indication for Cinacalcet? | Treatment of secondary hyperparathyroidism in adult patients w/ chronic kidney disease patients on dialysis or tx'ing hypercalcemia in patients w/ parathyroid CA |
| What is the calcimimetic (Cinacalcet) MOA? | Acts to increase sensitivity of calcium-sensing receptors in the PTH gland to extracellular calcium, leads to decreased secretion of PTH & lowering serum calcium levels |
| What is calcitonin? | A hormone produced by the thyroid gland (c-cells) |
| What is the MOA of calcitonin? | To lower levels of calcium |
| How does calcitonin lower levels of calcium? | By promoting detachment of osteoclasts from bone |
| What cells in the thyroid produce calcitonin? | The parafollicular cells. |
| How should calcitonin be administered? | Parenterally or by nasal inhalation |
| How does calcitonin promote the detachment of osteoclasts from bone? | It binds directly to receptors on osteoclasts and increases c-amp levels leading to inhibition of osteoclast activity, decreasing bone reportion, lowering serum calcium concentrations and reducing bone pain |
| What is a long-term effect of calcintonin therapy? | Reducing the number of osteoclasts and decreasing bone formation |
| What is the indication for calcitonin therapy? | Osteoporosis, Paget's dz of bone, and hypercalcemia |
| What type of patients is calcitonin used in? | Post-menopausal women (in menopause over 5 yrs) who can't take estrogen |
| What drug class is calcitonin in? | Calcium Hormone |
| What drug class does Teriparatide belong to? | Calcium Hormone |
| What is Teriparatide's sub-class? | Parathyroid Hormone Agonist |
| What is Teriparatide? | It is a recombinant form of PTH |
| How is Teriparatide administered? | Sub-cut (1x/day) |
| What does Teriparatide do? | It stimulates new bone formation on trabecular and cortical bone surfaces by preferentially stimulating osteoblastic activity over osteoclastic activity |
| How does Teriparatide differ from PTH? | Teriparatide increases markers of bone formation, skeletal mass, and bone strength, but too much continuous PTH stims bone resportion and detrimental to skeleton |
| What does Teriparatide do to calcium, phosphorous and 1,25 dihydroxyvitamin D? | It elevates serum calcium and vitamin D and transient lower serum phosphorous and phosphaturia |
| What is a contraindication for Teriparatide? | If at increased risk for osteosarcoma such as Paget's bone dz or unexplained elevations of serum phophatase |
| Who should take Teriparatide? | Post-menopausal women with osteoporosis or men at high risk for fracture |
| Why is Teriparatide is black box Rx? | B/c it can increase risk of osteosarcoma |
| What sub-class are Calcium carbonate and Calcium Citrate under? | Minerals |
| What is the indication for Calcium carbonate and calcium citrate? | Prevention and treatment of osteoporosis |
| Why is calcium citrate recommended over calcium carbonate in the elderly? | Elderly patients tend to have decreased stomach acid; Calcium citrate does not require stomach acid for absorption while calcium carbonate does |
| What is the primary treatment for hypocalcemia? | Calcium citrate and calcium carbonate |
| What subclass 1 does cholecalciferol belong to? | Steroid hormone |
| What sub-class 2 does cholecalciferol belong to? | Vitamin D |
| What is the indication for cholecalciferol? | Vitamin D deficiency, osteoporosis, malabsorption, hypoparathyroidism, refractory rickets |
| What is cholecalciferol the pre-cursor of? | 1,25-dihydroxyvitamin D3 |
| What does cholecalciferol do? | Increases absorption of calcium and resorption of bone, and helps to maintain normal bone mineralization by maintaining adequate calcium-phosphorous concentrations in blood |
| What is an aderve effect of calcium minerals? | Most common: constipation |
| How can calcium induced constipation be avoided? | Ingesting enough fiber |
| What should calcium not be taken with and why? | Fiber laxatives b/c they decrease calcium absorption |
| What can excess doses of Vitamin D lead to? | Hypercalcemia & hypercaliuria |
| What Rx's can calcium decrease the absorption of? | Cipro, fluoride, phenytoin, and tetracycline |
| How far apart should calcium and tetracycline, phenytoin, fluoride, and cipro be taken | 2 hours |
| What drug inhibits vitamin D absorption? | Cholestyramine |
| What Rx's can induce enzymes to metabolize Vitamin D? | Barbituates and phenytoin |
| What class does Raloxifene belong to? | Estrogens |
| What is Raloxifene's sub-class? | SERM - Selective Estrogen Receptor Modulator |
| What is the indication for Raloxifene? | Prevention and treatment of osteoporosis in post-menopausal women - only SERM indicated |
| What are some adverse effects of Raloxifene? | Hot flashes, VTE's, hypertriglyceridemia |
| Why is estrogen no longer considered a first-line therapy for prevention of osteoporosis? | Concerns about increased breast cancer and VTE dz |
| What does Raloxifene do? | Mimics estrogen by reducing bone resorption, inhibiting IL-1, IL-6, TNF, |
| Why does Raloxifene have the adverse side effects it has? | b/c though it activates estrogen bone receptors, it has antiestrogen effects on other tissues |
| Conjugated Equine estrogen and estradiol belong to what class and sub-class? | Estrogens and estrogen agonists |
| How is estradiol administered? | Via oral, vaginal tabs, or vaginal ring |
| What are conjugated equine estrogens? | Sulfate esters of estrone and equilin |
| What is conjugated equine estrogen derived from? | Urine of pregnant mares |
| Do conjugate equine estrogens have little first pass metabolism? | Yes |
| What are conjugated equine estrogens converted to in the liver? | Sulfate and glucuronide conjugates |
| Where is estradiol and estrone and equilin (conjugated equine estrogen) metabolized? | In the liver into sulfate and glucuronide |
| How are the estrogen agonists excreted? | Via urine and very lil in feces |
| What are estrogen preparations' indications? | Primary Hypogonadism, menopause |
| What are adverse effects of estrogen agonists? | Changes in libido, N/V, anorexia |
| What are major serious adverse effects of estrogens? | Hypertension, VTE, gallbladder dz |
| Why do estrogen agonists cause HTN? | b/c angiotensinogen synthesis is promoted |
| When are estrogens contra-indicated? | During pregnancies and in women w/ fibroids |
| What patient profiles should used estrogens w/ great caution? | Those w/ hepatic dz, endometriosis, VTE, or hypercalcemia |
| What types of steroid hormones do the adrenals produce? | Mineralcorticoids, glucocorticoids, and adrenal androgens |
| What two hormones affect the secretion of adrenal steroids? | ACTH and CRH |
| How is it that cortisol is able to exert both glucocorticoid and mineralcorticoid actions? | B/c although the glucocorticoid receptors have a high affinity for cortisol and low one for aldosterone, the Mineralcorticoid receptors have high affinity for both aldosterone and cortisol |
| What is the most frequent use of glucocorticoids in clinical practice? | To relieve inflammation by giving supraphysiologic doses of them |
| What is a loss common use of glucocorticoids and mineralcorticoids? | As replacement Tx in treatment of adrenal insufficiency and treatment of adrenogenital syndromes |
| What is the major mineralcorticoid in humans? | Aldosterone |
| What is Fludrocortisone? | A mineralcorticoid |
| When is Fludocortisone used? | In treating primary adrenal insufficiency - Addison's Dz to supplement the mineralocorticoid effect of hydrocortisone Tx |
| What determines whether fludrocortison is needed? | Continued presence of hyperkalemia after adequate doses of hydrocortisone |
| How is Fludrocortison administered? | Orally 1 x/day in a.m. |
| How are glucocorticoids classified? | Basis of their duration of action |
| What is cortisol? | The major glucocorticoid in humans |
| What is cortisol called when used as a pharmaceutical? | Hydrocortisone |
| What are hydrocortisone, prednisone and dexamethasone classifed as? | Glucocorticoid receptor agonists |
| What is the short-acting glucocorticoid? | Hydrocortisone |
| What is the intermediate-acting glucocorticoid? | Prednisone |
| What is the long-acting glucocorticoid? | Dexamethasone |
| How much more potent is Prednisone than cortisol (aka hydrocortisone)? | 4-5 x's more potent |
| How much more potent is dexamethasone when compared to cortisol? | 30 x's more potent |
| What kind of enzumes do glucocorticoids induce? | Those involved in gluconeogenesis |
| Why can glucocorticoid insufficiency lead to hypoglycemia during stress? | Because glucocorticoids promote glucose formation and have an anti-insulin effect |
| What other areas do glucocorticoids affect? | Enzymes for protein catabolism and lipolysis, and inhibition of glucose uptake by adipose tissue |
| What can glucocorticoids lead to on a patient's appearance? | Abnormal fat distribution and muscle wasting |
| What are glucocorticoid's anti-inflammatory effects due to? | Multi actions on several types of leukocytes |
| Activation of what leukocytes is suppressed by glucocorticoids? | T lymphocytes |
| What do glucocorticoids suppress in activated T helper cells | Cytokines |
| By suppressing the production of cytokines by T helper cells, what do glucocorticoids prevent? | Recruitment of eosinphils and antibody production by B cells |
| What do glucocorticoids prevent mast cells, basophils and eosinophils from releasing? | Chemical mediators of inflammation such as histamine, prostaglandins, leukotrienes, vasodilation and edema |
| Glucocorticoids suppress what types of tissue and cells? | lymphoid tissues and red. lymphocytes, monocytes, eosinophils, and basophils |
| What cells are increased in concentration by glucocorticoids? | PMN's, Erythrocytes, Platelets |
| What effect do glucocorticoids have on vitamin D? | Antagonize it therefore contributing to osteoporosis |
| What two hormone's secretion are reduced by glucocorticoids? | TSH and FSH |
| What enhances glucocorticoid potency? | Introduction of a double bond at 1,2 position or of a hydroxul or methyl group at the 16 position, as well as a substitution to fluorine at the 9 position |
| Is Fludrocortisone short or long-acting? | Short acting |
| What are the indications for glucocorticoids? | For the diagnosis and treatment of adrenal diseases and other (rheum, etc) |
| How is an addisonian crisis treated? | As a medical emergency treated promptly w/ IV hydrocortisone for up to 48 hrs |
| How is hydrocortisone administered? | Orally and mimicking circadian secretion of cortisol - 2/3 in a.m., 1/3 in p.m. |
| How is Cushing's syndrome Dx'd? | By low-dose dexamethasone test |
| How is dexamethasone used to test for Cushing's syndrome? | A single dose of dexamethasone is given orally at 11 pm - this should suppress ACTH release by the pituitary thus causing cortisol levels to decrease under 5 micrograms/dL |
| What will happen in a patient with Cushing's if given dexamethasone? | Their cortisol levels will not drop b/c dexamethasone won't be able to suppress ACTH |
| When is a high dose dexamethasone suppression test administered? | To differentiate bet. adrenal hyperplasia and other causes of hyperadrenocorticism |
| What type of cancers are glucocorticoids used for? | Lymphocytic leukemias and lymphomas |
| What type of derm issues can glucocorticoids be used for? | For pruritis, psoriasis |
| In what disorder are glucocorticoids considered the drugs of choice for managing? | Sarcoidosis |
| Are orally administered glucocorticoids lipid soluble and well absorbed by the gut? | Yes |
| What are glucocordicoids highly bound to while in the circulation? | corticosteroid-binding globulin and albumin |
| What does a mineralcorticoid do? | It's an adrenal steroid that promotes Na reabsorption and K excretion in DISTAL nephron |
| What is the usual dosage of Fludrocortisone? | 50-100 mcg/day |
| If there is minor stress, should there be dosage adjustment of Fludrocortisone? | No |
| For major stress (ER surgery) what should happen with the glucocorticoid dosing? | Dosing should be increased to 200-300 mcg and .9% saline disposes of need for extra Fludrocortisone |
| What are side effects of glucocorticoid Tx? | muscle wasting, glucose intolerance, depression, osteoporosis, dermal fragility, growth arrest if child, immunosuppression/ infection susceptibility, wt. gain |
| What are potential side effects of Fludrocortisone (a mineralcorticoid)? | Hypernatriemia (therefore HTN, Edema, CHF), Hypokalemia |
| What does long term Tx w/ pharm dosing of glucocorticoids do? | Suppresses the hypothalamimic-pituitary-adrenal axis by (-) feedback on hypothalamus & pituitary - therefore adrenal glands involute |
| How does the hypothalamic-pituitary adrenal axis cover? | From top down as adrenal has to grow back |
| Who is at low risk for HPA axis suppression? | Any patient taking glucocorticoids at any dosage for less than 2-3 wks |
| Who is at high risk for HPA axis suppression? | Anyone on >20 mg of prednisone for > 3 wks |
| What class/sub-class does Tamoxifen belong to? | Estrogens - Antagonist |
| What class/sub-class does Clomiphene belong to? | Estrogens - Antagonist |
| What drug class/ sub-class does Conjugated equine estrogen belong to? | Estrogens - Agonist |
| What drug class/sub-class does Letrozole belong to? | Estrogens - Antagonist |
| What class/sub-class does Estradiol belong to? | Estrogens - Agonist |
| What class/sub-class does Anastrozole belong to? | Estrogens- Anti-estrogens |
| What class/sub-class does Raloxifene belong to? | Estrogens - Antagonist |
| What class/sub-class does Danazol belong to? | Estrogens - Anti-estrogen |
| What are the two Aromatase inhibitors? | Anastrazole and Letrozole |
| What are the two estrogen anti-neoplastic drugs? | Tamoxifen and Anastrazole |
| What class/sub-class does Choriogonadotropin belong to? | Gonadotropins/ infertility drugs |
| What class/sub-class does Lupotropin belong to? | Gonadotropins/ infertility drugs |
| What class/sub-class does Methyltesterone belong to? | Androgen/ Androgen Agonist |
| What class/sub-class does Finasteride belong to? | Androgen/ Anti-Androgens/ 5 alpha reductase inhibitor |
| What class/sub-class does Flutamide belong to? | Androgen/ Anti-Androgens/ Androgen R. Antagonist/Anti-Neoplastic |
| What class/sub-class does Medroxyprogesterone belong to? | Progestins/ Progesterone Agonist |
| What class/sub-class does Norethindrone belong to | Progestin/Progesterone Agonist |
| What class/sub-class does Progesterone belong to? | Progestin/Progesterone Agonist |
| What are the two gonadotropins? | LH and FSH |
| What does LH do in a man? | Stimulates Leydig cells |
| What do Leydig cells (found in males) produce? | Testosterone |
| What does FSH do in males? | Stimulates Sertoli cells |
| What do Sertoli cells do in males? | Sertoli cells cause spermatogenesis with the aid of testosterone produced by the Leydig cells |
| What does FSH stimulate in females? | Granulosa cells to make Estradiol, Inhibin, and Ovulation |
| What does inhibin inhibit? | FSH |
| What type of receptors are on Gonadotropins? | GPCR's |
| What is Lutropin? | recombinant LH |
| What is Choiogoandotropin? | recombinant hCG |
| What drug has a longer t1/2, Choriogonadotropin or Lutropin? | Choriogonadotropin |
| What is the indication for using Choriogonadotropin or Lutropin? | Infertility in both sexes - hypogonadotropic hypogonadism |
| What effect do Choriogonadotropin and Lutropin have in females? | Induce ovulation for IVF |
| What are other indications for using Choriogonadotropin and Lutropin in males? | Cryptochidism and Dx'ing intersex XY (tests if able to produce Testosterone |
| What are adverse side effects of gonadotropins in females? | Local rxns (if not recombinant), multiple gestations, Ovarian hyperstimulation syndrome (inc. coagulation DIC), or risk of ovarian tumors |
| What are adverse side effects of administering gonadotropins in males? | Site rxn or gynecomastia |
| What has greater affinity for Androgen receptors, testosterone or DHT? | DHT (10x's more affinity) |
| What do androgens do to the urogenital tract during development? | Cause change of labia to scrotum under influence of Testosterone |
| Are androgens essential for spermatogenesis? | Yes |
| What does adrenal DHEA metabolize into? | T., DHT, E2 |
| Why is 5 alpha reductase important in males? | It helps to convert testosterone into DHT |
| Why can most testosterone not be administered orally? | It undergoes first-pass metabolism |
| Why can methyltestosterone be administered orally? | b/c it is resistant to hepatic metabolism |
| Should methyltestosterone be given for hypogonadism? Why or why not? | Methyltestosterone should not be administered for hypogoandism b/c it is hepatotoxic |
| Who tends to abuse androgens? | Body builders, athletes |
| Where is testosterone converted to DHT? | In prostate, hair follicles, & skin |
| What is testosterone converted to in the liver? | Androstenedione and other metabolites, incl. sulfact and glucuronide |
| How are testosterone metabolites excreted? | 90% via urine |
| What do estrogens and progesterone do to serum lipoprotein levels | Estrogen lower LDL and increases HDL while progesterone increases LDL and decreases HDL |
| When are estrogen and progestin adminstered simultaneously? | When used as HRT |
| Does Estradiol have good bioavailability? | Yes |
| What are the most serious side effects of Estrogens? | Thromboembolic disease, HTN, and gall bladder dz |
| In who are estrogens contraindicated? | Pregnant women and women w/ uterine fibroids |
| What diseases are cause for caution when administering Estrogens? | HTN, Thromboembolic Dz, hepatic dz, hypercalcemia |
| How is progesterone metabolized? | First pass metabolism |
| How are progesterones administered if first pass metabolism is taking place? | Orally |
| Do progesterones have long t1/2? | No, short |
| How is medroxyprogesterone administered? | Orally or IM |
| How were the oral bioavailability and t1/2 extended in progesterone meds? | Esters of progesterone were developed |
| How are progesterones excreted? | Via urine after converting into pregnandiol glucuronide in the liver |
| What are the indications for progesterone? | Suppress ovarian fuction (dysmenorrhea, endometriosis, uterine bleeding) |
| How can progesterone meds be used to suppress ovarian fxn? | By producing feedback inhibition to pituitary to stop gonadotropin from being released |
| What is progesterone's half life? | 5 minutes |
| What is Norethindrone's half life (Progesterone agonist)? | 7-24 hrs. |
| What class of 19-norprogestins does Norethindrone belong to? | Estranes. |
| What are the indications for Estrogens? | Relief of menopausal Sx's, Primary hypogonadism |
| What is conjugated equine estrogen mostly used for? | As HRT |
| What type of metabolism do Androgens undergo? | 1st pass |
| Given that Androgens go thru 1st pass metabolism, how are they administered? | parenterally or transdermally |
| What has a longer half-life, Testosterone or Methyltestosterone? | Methyltestosterone |
| What are most testosterone preps used for? | Hypogonadism caused by primary testicular failure or 2ndary to hypopituitarism |
| What can inappropriate abuse of androgens lead to? | tendon rupture, hepatic dysfunction, cholestatic jaundice |
| Danazol is an androgen that is anti-estrogenic, why is it used for? | Tx: fibrocystic breast dz, endometriosis, autoimmune dz |
| How is danazol administered? | Orally |
| What is Danazol's t/2? | 5 hrs |
| What is Danazol's MOA? | Acts on pituitary to reduce LH and FSH secretion |
| What is an androgen synthesis inhibitor? | Finasteride |
| What is Finasteride's MOA? | Blocks 5 alpha reductases |
| What is the indication for Finasteride? | BPH and male pattern baldness |
| What is an adverse effect of Finasteride? | Sexual dysfunction |
| What drug is known as an Androgen Receptor Antagonist? | Flutamide |
| What is Flutamide's MOA? | Competitively inhibits Androgen Receptors |
| What is a major adverse effect of Flutamide? | Hepatoxocity |
| What are the indications for using Flutamide? | Hirsutism, prostate cancer |
| Are estrogens cognition protectants? | Yes |
| What form of estrogen is used most? | Ethinyl estradiol |
| What is ethinyl estradiol's t1/2? | 20 hrs |
| What is the form of estrogen used most in OCP's? | Ethinyl Estradiol |
| What is clomiphene's t1/2? | 5 days |
| What is the indication for using clomiphene? | To treat anovulatory infertility |
| What is clopmipheen's MOA? | It causes negative feedback being sent to pituitary causing pituitary to increase LH and FSH secretion thereby inducing ovulation |
| What rate of women have multiple births? | 5-12% |
| What is Tamoxifen's t1/2? | 7 days - long |
| What is most active form of Tamoxifen? | Its metabolites CYP3A4 and CYP2D6 |
| What is Tamoxifen's indication? | Treat estrogen receptor positive breast cancer |
| In what tissues does Tamoxifen acts as an estrogen receptor antagonist? | in CNS and breast |
| How does Tamoxifen act in uterus, bone, and lipid metabolism? | As an estrogen agonist |
| Raloxifene acts as Tamoxifen in that it antagonizes breast and CNS estrogen R. but how does it differ? | Raloxifene, unlike Tamoxifen also acts as an antagonist in uterine tissue |
| What is Raloxifene's primary indication? | Prevent osteoporosis, reduces risk of breast ca |
| What are adverse effects of Raloxifene? | Hot flashes, endometrial hyperplasia, thrombosis |
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