Term
| What is the basic structure of prostanoic acid? |
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Definition
| It has a 5-membered ring and a 20-C chain with a COOH group at one end and a CH3 group at the other end. |
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Term
| PG receptors are couple to |
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Definition
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Term
| What is the major source of AA? |
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Definition
| Cell membrane phospholipids |
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Term
| What enzyme converts cell membrane phospholipids to AA? |
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Definition
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Term
What enzyme converts AA to PGs? What enzyme converts AA to LTs? |
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Definition
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Term
| Which PGs are most important biologically? |
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Definition
| PGE, PGF, PGI, and thromboxane. PGG and PGH are simply intermediates. |
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Term
| What enzymes do NSAIDs inhibit? |
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Definition
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Term
| Discuss the adverse effects of NSAIDs. |
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Definition
NSAIDs inhibit COX, so PGs are not being made. If there are no PGs, then there is no cytoprotective function and GI irritation occurs. Another side effect is increased bleeding time. Since COX is inhibited, thromboxane is not made. If thromboxane is not made, there is nothing to hold the platelets together. |
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Term
| How do corticosteroids work? |
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Definition
| They act on their receptor intracellularly to produce lipomodulin. Lipomodulin inhibits phospholipase A. Therefore, there is no production of AA, which means there is no production of LTs or PGs. |
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Term
| How do PGs effect the CV system? |
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Definition
| They cause vasodilation to increase BP. This creates a reflex effect of increased CO and HR. |
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Term
T or F PGs maintain the patency of the ductus arteriosis if surgery is required after birth. |
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Definition
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Term
| Which PGs inhibit platelet aggregation? |
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Definition
|
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Term
| What do PGs and LTs do to bronchial smooth muscle? |
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Definition
PGs cause bronchial relaxation LTs cause bronchial constriction |
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Term
| What do PGs (F, I, and E)do to uterine muscle to prepare for pregnancy? |
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Definition
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Term
| What do PGs do to intestinal smooth muscle? |
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Definition
| They cause it to contract, which is why nausea and vomiting are common side effects. |
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Term
| How do PGs have cytoprotective effects? |
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Definition
| PGs inhibit secretion of gastric acid and pepsin and they stimulate mucous secretion. |
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Term
| What do PGs do to peripheral nerves? |
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Definition
| They sensitize them and inflict pain on them. |
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Term
T or F NSAIDs can be used to prolong labor. Explain. |
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Definition
| True, b/c NSAIDs inhibit PG produciton; and, if there's no PGs, then there's no uterine contractions. |
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Term
What is dinoprostone used for? |
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Definition
It can be used during the second trimester of pregnancy to induce abortion; it can also be used to induce labor. |
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Term
| What is dysmenorrhea? How could you treat it? |
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Definition
| It's painful menstruation. Since it is due to PGs, an NSAID could be used. |
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Term
| How is alprostadil (caverject) used for male impotence? |
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Definition
| It's a PG that is either injected or placed into the urethra. It causes vasodilation of the cavernosa to cause an erection. |
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Term
| What were the 3 mentioned uses of alprostadil? |
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Definition
| Tx of male impotence, inhibition of platelet aggregation, & maintenance of the ductus arteriosus. |
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Term
| What is epoprostenol's indication? How does it work? By what route is it adminstered? |
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Definition
| It is a prostacyclin that is given to treat pulmonary HTN. It causes vasodilation by relaxing smooth muscle. It has to be given by continuous IV infusion due to its short half life. |
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Term
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Definition
Pts on long-term NSAID therapy will have no PGs to protect the stomach. Cytotek is a synthetic PG that has cytoprotective effects. In addition, this synthetic form has little to no GI stimulant effects, whereas PGs do. PGs protect the stomach but they also stimulate the GI. |
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Term
| What is xalatan? What is it used for? How does it work? What is the warning for people using glaucoma? |
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Definition
| It is a long acting PG derivative used for open-angle glaucoma. It increases the outflow of aqueous humor to reduce intraocular pressure. You don't want to wear it with contacts. |
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Term
| What are the 3 classes of adrenal steroids? |
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Definition
| glucocorticoids, mineralocorticoids, and gonadal steroids |
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Term
| Discuss the regulation of glucocorticoids. |
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Definition
| When cortisol levels are high, they inhibit the hypothalamus from releasing CRH & they inhibit the anterior pituitary from releasing ACTH. W/o ACTH, the fasciculate reticularis won't produce any more cortisol. Everything is opposite for when cortisol levels are low. |
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Term
| Discuss the regulation of mineralocorticoids. |
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Definition
| If blood volume is down, B/P is down, sodium is down, and/or potassium is up, the JG cells will release renin. Renin will convert angiotensinogen to angiotensin I. ACE then converts angiotensin I to angiotensin II. Angiontensin II (a vasoconstrictor) then stimulates the glomerulus to secrete aldosterone which will cause reabsorption of Na and water in exchange for secretion of K and H+. |
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Term
| Describe the cellular mechanism of action for steriods. |
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Definition
| Steroids readily diffuse through the membrane and bind to receptors in the cytoplasm. Then, they become active once they dimerize. Then, they act as transcription factors. Proteins are produced to elicit a response associated with the steroid. |
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Term
| What are some serious side effects of glucocorticoids? What causes these side effects? |
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Definition
| Muscle wasting, osteoporosis, inhibition of growth if given to a child, and diabetes. Glucocorticoids stimulate gluconeogenesis by breaking down tissues (ie, muscle and bone) into glucose. The glucose then gets converted into glycogen in the liver for a net increase in glycogen synthesis. They can also inhibit peripheral glucose utilization, which could cause diabetes. |
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Term
| What is Cushing's syndrome? |
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Definition
| It's due to a hypersecretion of glucocorticoid that produces a characteristic fat redistribution. |
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Term
| What effect do glucocorticoids have on blood cells? |
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Definition
| They cause a reduction in WBCs, meaning some of the main side effects are infections. |
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Term
T or F Glucocorticoids are one of the most potent types of anti-inflammatory. T or F Extended use of glucocorticoids can cause depression |
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Definition
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Term
| How does long-term use of glucocorticoids lead to adrenal atrophy? |
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Definition
| When cortisol levels are high, the release of ACTH is inhibited. Decreased ACTH activity leads to adrenal atrophy. |
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Term
| What % of endogenous steroid is bound to CBG or albumin? How much of the steroid, then, is therapeutically active? |
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Definition
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Term
| What are the 3 ways you can prevent adrenal insufficiency (atrophy)? |
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Definition
| You can withdraw the drug slowly; you can give ACTH a week or so before the drug is discontinued; or, you can do alternate day therapy (on the day the drug is not taken, ACTH is being secreted). |
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Term
| What are some adverse side effects of drug-induced cushing's syndrome? |
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Definition
elevated blood glucose reduced WBCs - infection ulcers myopathy - weakness psychosis osteoporosis |
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Term
What is primary adrenal insufficiency? |
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Definition
| Primary is where the adrenal gland is damaged. Glucocorticoid and mineralocorticoid (or a drug that contains both) should be administered. |
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Term
| What is secondary adrenal insufficiency? |
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Definition
| The adrenal gland is okay; but, it's not being stimulated by ACTH. People w/ secondary insufficiencies should be given glucocorticoid. |
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Term
| What is congenital adrenal insufficiency? |
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Definition
People w/ this insufficiency tend to produce excessive testosterone. 90% of people w/ this insufficiency lack the enzyme, 21 beta-hydroxylase, and they need both glucocorticoid and mineralocorticoid. The other 10% lack the enzyme 11 beta-hydroxylase and they only need glucocorticoid. |
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Term
If a pt has rheumatoid arthritis, by what route of administration should they take their medicine? If a pt has osteoarthritis, by what ROA should they take their medicine? |
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Definition
RA occurs throughout the body, so the medicine should be taken PO. Osteoarthritis is usually confined to joints, so an injection into the joints should suffice. |
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Term
| Why is it important to be sure that ocular inflammation is not due to an infection? |
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Definition
| The steroid would get rid of the pain, but not the infection. In fact, it would encourage the infection by reducing WBCs. |
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Term
| What is aminoglutethimide? When would you use it? |
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Definition
It inhibits enzymes involved in the synthesis of all steroids. It's used for people who have an over-active adrenal gland (eg, people w/ Cushings). |
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Term
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Definition
| It is a competitive receptor antagonist of steroids. It has a similar structure to aldosterone and testosterone. So, it acts as a K-sparing diuretic and it inhibits androgenic effets, respectively. An example of androgenic effects would be hirsutism in women (growth of facial hair). |
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Term
Concerning spermatogenesis: What hormone does the hypothalamus release? What hormones does the anterior pituitary release? |
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Definition
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Term
What does FSH stimulate? What does LH stimulate? |
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Definition
seminiferous tubules leydig cells |
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Term
What happens when FSH stimulates the seminiferous tubules? What happens when LH stimulates the Leydig cells? |
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Definition
The seminiferous tubules begin spermatogenesis and secrete inhibin. The Leydig cells release testosterone. |
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Term
What does inhibin do? What does testosterone do? |
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Definition
Inhibin and testosterone inhibit the hypothalamus and anterior pituitary from secreting their respective hormones. Testosterone also stimulates the seminiferous tubules to begin spermatogenesis, and it also causes androgenic activity. |
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Term
| What are the 2 main hormones that are required for spermatogenesis? |
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Definition
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Term
What enzyme converts testosterone to dihydrotestosterone in the peripheral tissues? What enzyme converts testosterone to estradiol in the peripheral tissues? |
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Definition
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|
Term
T or F Testosterone is converted to inactive androsterone in the liver |
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Definition
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Term
T or F testosterone causes closure of the epiphysis |
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Definition
| false, estradiol does this. |
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Term
| 98% of testosterone in the circulation is bound to . Estradiol aslo binds to this protein. |
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Definition
| sex hormone-binding globulin |
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Term
| What is the cellular mechanism of action for testosterone? |
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Definition
| Testosterone readily diffuses into the cytoplasm where it gets converted to dihydrotestosterone by the enzyme 5a-reductase. Dihydrotestosterone then enters the nucleus & binds to a receptor. The dihydrotestosteron-receptor complex then act as transcription factors on DNA to produce biological activity. |
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Term
| In order for testosterone to be taken orally, what has to be done? |
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Definition
| the 17-OH group has to be alkylated |
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Term
| What type of ratio of anabolic to androgenic effects does a natural androgen like testosterone have? What about an anabolic steroid like oxandrolone? |
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Definition
|
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Term
| Who might an anabolic steroid be used in? |
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Definition
Burn patients & cancer patients who need to grow tissue. |
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Term
| What are 3 common side effects from anabolic steroids? |
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Definition
JET Jaundice Edema Testicular atrophy |
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Term
| In addition to being an aldosterone inhibitor, what does spironolactone do? |
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Definition
| It's an androgen-receptor antagonist |
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Term
| How can GnRH be used as a drug? |
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Definition
| It inhibits synthesis of LH. |
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Term
| How does finasteride work? What is it used for? |
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Definition
| It is a 5a-reductase inhibitor that prevents the conversion of testosterone to dihydrotestosterone. It's used for prostatic hypertrophy or male-pattern baldness. |
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Term
| Secretory regulation in females is similar to males. The hypothalamus secretes GnRH which stimulates the anterior pituitary to release LH and FSH. What hormones are released when LH and FSH stimulate the overy? |
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Definition
| Estradiol and progesterone |
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Term
T or F Release of LH and FSH occurs in a pulsatile manner |
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Definition
| True, and when we give LH and FSH as drugs, we have to give them in a pulsatile manner. |
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Term
| The increase of what hormone is thought to cause ovulation |
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Definition
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Term
| Explain the menstrual cycle with regards to LH, FSH, and follicular development |
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Definition
| In the beginning of the menstrual cycle, FSH is high. FSH stimulates multiple follicles, but only one will survive. As FSH decreases and LH increases, ovulation occurs about day 14. After ovulation, LH begins to decrease and the follicle becomes a corpus luteum. The corpus luteum atrophies when LH and FSH are no longer stimulating it to produce estrogen and progesterone. |
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Term
| Explain the menstrual cycle with regards to follicular development and the ovarian steroids |
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Definition
| As the follicles mature, they produce primarily estrogen. After ovulation, the follicle is developing into the corpus luteum. The corpus luteum begins secreting estrogen and progesterone. As LH and FSH begin to decrease, the corpus luteum atrophies. As a result, estrogen and progesterone levels fall. |
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Term
| Explain the menstrual cycle in regards to the ovarian steroids and the endometrium |
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Definition
| Menses occurs at the beginning of the cycle. As estrogen levels begin to rise, estrogen stimulates the uterine endometrium to grow and become thick (this is the follicular phase). After ovulation, progesterone levels begin to rise. The progesterone causes the uterine endometrium to become fertile. If the egg is not fertilized, the corpus luteum will atrophy (menstruation). If an ova does get fertilized, it will implant into the endometrium. |
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Term
Explain pregnancy with regards to Estrogen, Chorionic Gonadotropin, and progesterone |
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Definition
| After the fertilized egg implants itself into the endometrium, chorionic gonadotropin (HCG) is secreted. HCG takes the place of LH and FSH in order to keep the corpus luteum stimulated (remember that it atrophies if it's not stimulated). The corpus luteum has to remain stimulated in order to secrete estrogen and progesterone to maintain the placenta. Eventually, HCG is greatly reduced as the placenta becomes mature enough to secrete estrogen and progesterone. |
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Term
Explain the estrogen mechanism |
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Definition
| Estrogen readily diffuses across the membrane into the cytoplasm and it binds to a receptor. The estrogen-receptor complex then dimerizes before it acts as a transcription factor on DNA |
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Term
| Explain the two types of estrogen receptors. Also, which receptor does tamoxifen bind to? Raloxifene? |
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Definition
ER-alpha is found in reproductive tissue ER-beta is found in CV and bone Tamoxifen is an antagonist at ER-alpha Raloxifene is an agonist at ER-beta and an antagonist at ER-alpha. Raloxifene, then, is used for osteoporosis. |
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Term
Once estrogen gets into the bloodstream, what protein does it bind to? |
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Definition
| Sex hormone-binding globulin |
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|
Term
What is the most common side effect of estrogen as a drug? |
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Definition
|
|
Term
| What is SERM (selective estrogen receptor modifier)? |
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Definition
| SERM is a term used for numerous estrogen-like compounds that have different degrees of estrogen activity; some are estrogen agonists, some are estrogen antagonists, and some are agonists in some areas and antagonists in others. |
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Term
| Explain the SERM mechanism |
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Definition
Tamoxifen, an anti-estrogen SERM, is the example that will be used for this mechanism. Tamoxifen diffuses into the cytoplasm and competes w/ estrogen for the receptor. The ER complex then dimerizes and becomes a co-repressor that inhibits transcription. If it were an agonist it would become a co-activator and increase transcription. |
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Term
| What is the main side effect of anti-estrogens? |
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Definition
|
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Term
| What is anastrazole? How does it work? What is it used for? |
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Definition
| It inhibits estrogen synthesis by blocking aromatase. It's used for advanced breast cancer following tamoxifen. |
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Term
|
Definition
| It's an oral contraceptive that has good oral activity. |
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Term
What is RU-486? How does it work? What is it used for? |
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Definition
| It's an anti-progestin. It is a competitve antagonist that competes with progestin for the receptor. It is an abortion drug that prevents implantation of a fertilized ovum. |
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