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75 Cards in this Set
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Parathyroid hormone(PTH)
active when? does wut, and where? 1 |
active when blood Ca low
-increase blood Ca, decrease PO4 -if continual dose resorption bone -intermittant (OB active) kidney saves Ca Mg -lets go of PO4 and Na -also enhance Vit D to active |
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Teriparatide (PTH 1,34)
1 |
first 34AA of PTH
-for low intermittant stim OB and makes bone -SQ inject -for osteoporosis careful of- osteosarcoma (not used under 18) |
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Cinacalcet
1 |
treat hyper PTH with chronic kidney diease
Mech- increase Ca sensitivity at parathyriod gland so less PTH released and lower Ca levels in blood |
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Paricalcitrol
1 |
Vit D analog, always active
-selective action on PT that lowers PTH release -no direct effects on serum Ca or PO4 contraindicated if hypercalcemic or hyper vit Dic? ha |
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Vit D aka...
1 |
Cacitriol
need UV actived kidney (if PTH, low Ca or PO4) specific transport(stimed by estrogen) -increase intestinal aborp Ca an PO4 (most signif) -decrease renal excretion -up OC activity -down more PTH (neg feedback) |
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Calcitonin
2 |
opposite PTH
-act on osteoclast decreasing ruffled border -secreted by C cells (makes sense) -from salmon- longer DOA and more potent than human-calcimar -kidney increase excretion both PO4 and Ca -for hypercalemia -pagets(OC gone wild) -osteoporosis |
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glucocorticoids (&cortisol)
2 |
-down Ca absorp from GI
--antag vit D in GI -stim renal Ca excrete -help PTH -inhibit collagen form) -inhib GH release -aka favor OC |
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estrogens
2 |
fight for OB
-cause apoptosis OCs -keep Vit D alive -increase decoy OPG (which keeps the OB from activating OC) yea theyre traitors, think mind control |
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Bisphosphonates
overview type? how? 1st 2nd gen |
chelating agents (bind Ca) (non hormonal)
-stable to hydrolysis (expensive too) poor absorb (lots of negatives...charges) hang on bone til acid from OC comes then spring into action and fuck up the OC bastards! second gen-block enzyme and Gprotein and therfore signalling 1st gen- stop ATP formation at AMP and lead OC apotosis -for Osteoporosis -peridontal disease -malignant hypercalcemia -pagets |
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1st gen bisphos
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E-etidronate - no IV!
T C's |
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etidronate sodium
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1st gen bisphos
not IV equal OC and OB inhib not really used |
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2nd gen bisphoss
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have N!
A-alendronate P-pamidronate R-risedronate Z-zolendronate |
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Alendronate sodium
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2nd gen bis phos
-liquid prep less esophagus erosion -low doses slective inhib resorption (osteonecrosis of jaw |
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Pamidronate disodium
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2nd gen
IV only |
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Risedronate sodium
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2nd gen
potent so less (also less esophagus SE?) |
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Zolendronate
also reclast |
most potent agent
-for malignnant hypercalcemia -jaw osteonecrosis -reclast 1/year for osteoporosis |
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Bisphosphonates
side effects uses |
diarrhea, GI upset (its chelator!)
-flu like first IV -esophageal ulceration and esophagitis (TAKE W? WATER!!) atrial fib in sum women for Pagets, hyperCa, osteoporosis |
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Mithramycin
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original cancer therapy (1/10 dose)
-inhjibit OC binds DNA also chelator for hyperCa Pagets |
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Thiazides
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only duiretics up Ca reabsorp
enhance PTH effect in kidney for hypercaluria (too much Ca in urine) |
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flouride
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act stabilize hydroxyapatite crystal
takes place of OH inhib OCs w/ Ca will active OBs too long and get crippling florosis |
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Saline Diuresis
phosphate |
for hyperCa
rehydration up glomerlar filt then furosemide flushes Ca P-bind Ca form complex |
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hypocalcemia
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more sever than hyper
major problem tetany -w/ little Ca always muscle contracted |
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Natural estrogen
estradiol |
usual IM
high 1st pass micronized oral has better absorp |
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conjugated estrogens
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from mare urine
for hormone replacement |
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synthetic estradiol derivatives
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has triplle to delay breakdown
mostly contraceptives Ethinyl estradiol, methranol, quinestrol |
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nonsteroidal estrogens
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syn
oral diethylstilbestrol(DES)- do not use in prego chlortrianesene-TACE |
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selective estrogen receptor modulators
(SERMS) |
syn, nonstoeriodal
raloxifene- agonist bone antag -breast endometrium -treat osteo in postmenapause low breats endo cancers |
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Progesterone
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comped antag aldosterone
'progestins' sig. first pass metabs have sedative/hypnotic properties |
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micronized progesterone
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orally active
like estrogen |
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C-21 synthestics
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more like progesterone
regular endo (secreetions too) medrooxyprogesterone acetate- provera megestrol acetate-stim appetite in HIVs compete aldosterone (antags) no estrogen or androgen SE |
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C-19
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2 carbons gone
-diff endo -no prego gonadotropin inhibs some andro estro SE viscous secretions (hostile sperm) 1st gen progestins usually 'no' or 'nor' |
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2nd gen progestins
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no male gestation in deserts
ex- norgestimate, gestodene, desogestrel -sum andro decrease free testost lower andro effects! |
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Drospirenone
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3rd gen progestins/ combo w ethinyl estradiol
like spironolactone, block androgen recept preventing Na H2O retention -can cause hyperkalemia anti andro, minimize acne, oil skin, hirsuitism, weight gain |
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Danazol
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dan the man kicks her in the ovary while fondling her breast and finger in endo
weak progest and andro act direct ovary stop estrogen and progestin syn by cyp450 treat fibrocystic breast disease treat endometriosis SE from androgen effects |
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Clomiphene citrate
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if want prego
up FSH and LH release up ovulation chance SERM SE- hot flashes, breast tender, heavy days! visual symptom heat wave? combined w/ metformin and glitazones for fertitlit polycystic ovary syn |
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Tamoxifen
Toremifene Fulvestrant |
tam-DOC breast cancer
antag estro in breast partial ag in endo also prevent bone loss -in breast cancers estrogen recep positive -hot flashes tor-similar -fulvestrant is pure antag, think about it (can be used if resistant too) |
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Anastrozole
Letrozole Examestane |
anna let exams inhibit aromas
Ana and Let- compeditive reversible inhibs of aromatase (so less estrogen) Exam- irreversible aro inhib all if tamoxifin dont work for breast cancer |
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GnRH analogs
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Leuprolide
Nafarelin Gosrelin Histrelin |
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GnRH and Analog uses
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peptides
intermittant- stim FSH LH release (treat hy[ogonadism) continous-- inhibit FSH LH release -Leuprolide/Gosrelin-prostate cancer in men (more test, precip pain) -supress endo, give exo to correct timing fertilization |
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GnRH antag
Cetrorelix |
pure receptor antag
bind pituitary comped inhibit FSH/ LH release for invitro fertiliztion |
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Bromocriptine mesylate
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dopamine agonist D2
inhibit prolactin release for hyperprolactemia parkinsons carful- increase stroke risk pst partum woman not wantin to lactate |
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Oral contraceptives
Estrogen role progestin role how work |
E- ovulation inhib (no LH FSH released pit)
P- inhib GnRH -produce thick sperm hostile envir. (most) can change motility pattern w/i fallo tubes |
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OC
Combined |
E and P days 5-25 then placebo
99% |
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OC
sequential |
estrogen 15 then E n P for 5
discon! risk endo cancer |
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OC
conintous low dose progestin |
mini pill
not reliable ovulation inhib spottin and breakthrough bleedin 96% no estrogen SE |
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OC
phasic |
vary doses so like normal cycle
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OC
depot |
longlastin injections
Medroxyprogesteron acetate- depo-provera IM 1/ 3 month |
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OC
patch |
Ortho-Evra- once a week
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OC
subdermal implants |
small plastic tubes under skin (up to 5 yrs.)
po-cant be good for u |
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post-coital contraceptives
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prevent implantation, alter motility through fallopian
severe nausea vomitin high estrogen doses Plan B! |
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mifepristone
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progesterone antag
-inhib action progest on uterus -detach embryo from wall (abort!) used w/ misoprostol (prostaglandin) |
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SE OC
estrogen |
nausea, edema
migrane chloasma gall bladder (stones, disease) |
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SE OC
progestins |
breakthrough bleedin
depression C-19s -androgenic -liver function/ jaundice- cholestatic jaundice |
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Biochem alterations OC
estrogen |
up blood coagulation
up plasma proteins blood lipids good X-triglycerides |
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biochem alteration OC
progestins |
carb metab- up insulin release
blood lipids- C19 1st gen bafd 2nd gen good |
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Severe side effects OC
estrogen |
cardiovascualar
venous thromboembolic disease MI- by clottin factors liver-stop bile secretion flow cerebrovascualr disease |
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Servere effects OC
progestins |
MI- cuz decrease HDL (1st gen andro)
liver0 cholestatic jaundive |
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OC effect cancer
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combo reduce ovarian endo cancers!!
up breast cancer in yoth no DES durin prego |
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In males
LH and FSH cause? GH role? |
LH-->Leydig--> testosterone(which neg feedbacks)
GH is synergistic w/ syn of testost FSH-->Sertoli Cells-->ABP production (keeps testes high in testost) |
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Testosterone
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C-19
keeps babymakin priority accel growth before epiphysis close DHT more active form (5alph-reductase makes conversion) use aromatase to make estradiol |
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Testosterone
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98%- albumin and sex-hormone binding globuin bound
SHBG up-estrogen, thyriod hormone down- androgen and GH and fattys metab- testosterone (in liver)-- androstenedione-->andosterone |
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Testosterone effects
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high first pass
treat andro replacement therapy anabolic therapy |
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DHT dependant sites
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skin
prostate seminal vesicles epididymis hair follicle |
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oral androgens
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methyltestosterone
fluoxymesterone-has aromatase blockin |
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first pass avoiding androgens
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andriod cyborgs propriate w/ ethanol
esterfied prodrugs-IM -testosterone cypionate -proprionate -enanthate -undecanoate (NOT us) topical gel1% transdermal patch |
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abnormalities of testicular function
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cryptoorchism
-they didnt drop -irreverse damage spermy epithelium -up tumor -treat w/ surgery/ GnRH hormone also hypogonadism |
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hypogonadism
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failur before puberty- EUNICHISM
symptoms-tall,large hands feet, no muscle/ sex drive small penis treat-long lasting testosterone replacement failure after puberty due to- castration, testes atrphy,, disruption vascular supply treat oral testost |
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other uses testost
contraindicated |
steroid abuse
breast carcinoma anemias dwarfism osteoporosis prego steriod cancers children growth phase |
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androgen receptor antagonist
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spironolactone
-compeditively bind DHT and aldost -duiretic and hirsutism Flutamide, tid bicalutamide qd- less GI nilutamide- most toxic -pure androgen blockers -prostate carcinoma -blocks receptor but inhibit feedback so more LH and FSH releaed -need GnRH agonist continous to work -man boobs cyproterone -hirsutism -decrease man sex drive -acetate version more potent antiandrogen effect |
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Leuprolide
Goserelin Rafraelin Buserelin |
Leu goes w/ ralf on bus
androgen suppressant -agonist -initial spike then drop off if used pulsatile ups |
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Finasteride
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androgen supression
-propecia -inhibitor of 5-alp reductase type ii (66%) -less DHT -treat BPH also baldness -abnormal fetal development |
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dutasteride
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dude sterilizer (aka no DHT)
inibitor 5apl- reductase 90% reduction DHT type 2 reproductive tissue type 1 liver skin -abnoral fetal -BHP |
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ketoconazole
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antifungal
-blocks sum cyp450s(therefore sum andro syn) DOC for cushing syndrome |
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cimetidine
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andro supression
-inhib sum cyp450s -mild antiandrogen effect |
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male contraceptive
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gossypol
-from cotton -azoospermic and impair sperm motility -destroy sum seminiferous epi w/o major alteration -hypokalemia(transient paralysis) -diarrhea,edema,dyspnea -azoospefi.. develop over months -NOT RELIABLE |
