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PDA II - Classes/MoA

Exam 1

QuestionAnswer
tesamorelin acetate (Egrifta) GHRH agonist stimulates synthesis and secretion of GH - approved for HIV lipodystrophy, AP function testing
octreotide (Sandostatin) somastatin analog - trtmt for excess GH - acts by inhibiting release, not synthesis of GH
sandostatin LAR somastatin analog - slow release formula for excess GH - acts by inhibiting release not sysnthesis of GH
lanreotide (Somatuline LA) somastatin analog - for excess GH IM every 10-14 days
Somatuline Autogel (lanreotide) somastatin analog - for excess GH
pegvisomant (Somavert) GH receptor antagonist - effective but concern it will decrease negative feedback by GH and increase size of tumor
irradiation for excess GH - kills all tissue, not selective for tumor --> not ideal
GH tumor removal surgery for GH secreting tumor - must be a large tumor
somatropin (Humatrope, Nutropin, Serostim) identical to human GH - treatment for dwarfism - may be used for AIDS wasting
mecasermin (Increlex) recombinant form of IGF-1 - tx for laron dwarfism
bromocriptine (Parlodel) somewhat selective D2 agonist - tx for high PRL
cabergoline (Dostinex) selective D2 agonist - tx for high PRL - better tolerated
oxytocin (Pitocin) induce or augment labor in last trimester
oxytocin (Pitocin) promote milk letdown
oxytocin (Pitocin) reduce or prevent postpartum hemorrhage
water restriction (short term) tx for SIADH - need to stop increasing blood volume
lithium or demecycline (long term) tx for SIADH - can inhibit effect of ADH by a post receptor mechanism
dDAVP (Desmopressin) vasopressin agonist - 3000x times more selective for V2 over V1 - tx for: central DI, nocturnal enuresis
tovaptan (Samsca) selective V2 antagonist BOXED WARNING - sodium monitoring
convipatan (Vaprisol) V1/V2 antagonist - only available as IV
testosterone short acting parenteral
testosterone propionate short acting parenteral
testosterone enanthate long acting parenteral
testosterone cypionate long acting parenteral
Androderm TRANSDERMAL androgenic agent
Androgel, Fortesta GEL androgenic agent
Striant BUCCAL androgenic agent
Axiron SOLUTION/SPRAY andro. agent - apply to underarm
methyl testosterone (Android) orally active andro agent
fluoxymesterone (Androxy) orally active andro agent
oxandrolone (Oxandrin) orally active andro agent
prazosin (Minipress) alpha blocker - work on a-receptors located on the sphincter of the bladder neck and urethra --> block receptors to help lessen restriction
terazosin (Hytrin) alpha blocker - work on a-receptors located on the sphincter of the bladder neck and urethra --> block receptors to help lessen restriction
tamsulosin (Flomax) alpha blocker - work on a-receptors located on the sphincter of the bladder neck and urethra --> block receptors to help lessen restriction
silodosin (Rapaflow) alpha blocker - work on a-receptors located on the sphincter of the bladder neck and urethra --> block receptors to help lessen restriction
alfuzosin (Uroxatral) alpha blocker - work on a-receptors located on the sphincter of the bladder neck and urethra --> block receptors to help lessen restriction
finasteride (Prsocar, Propecia) 5 alpha-reductase inhibitor - blocks the enzyme required to convert ttone to DHT (stops cause of prostate enlargemt) **pregnant don't touch crushed tabs
dutasteride (Avodart) 5 alpha-reductase inhibitor - blocks the enzyme required to convert ttone to DHT (stops cause of prostate enlargemt) **pregnant do not handle!!!
combo of a-blockers and 5HT reductase inhibitors used together to treat BPH to get greater efficacy?
flutamide (Eulexin) androgen antagonist - blocks androgen receptor (ttone & DHT) but also blocks neg feedbk so there's an increase in circulating ttone! DOESN'T WORK WELL + SIDE EFFECTS
alpha blockers work fastest for BPH! (relief within two days) 5HT reductase drugs can take up to 6 months (takes time to reduce prostate size)
alprostadil (Caverject - injection) (MUSE - urethral suppository) prostaglandin E1 agonists - tx for ED - PG cause DIRECT vasodilation without arousal
sildenafil (Viagra, Revatio) phosphodiesterase 5 inhibitors - tx for ED - PDE5 is the enzyme that breaks down cGMP and decreases blood flow, if we inhibit it, vasodilation stays longer
tadalafil (Cialis, Adcirca) phosphodiesterase 5 inhibitors - tx for ED - PDE5 is the enzyme that breaks down cGMP and decreases blood flow, if we inhibit it, vasodilation stays longer
vardenafil (Levitra, Staxyn) phosphodiesterase 5 inhibitors - tx for ED - PDE5 is the enzyme that breaks down cGMP and decreases blood flow, if we inhibit it, vasodilation stays longer
avanfil (Stendra) phosphodiesterase 5 inhibitors - tx for ED - PDE5 is the enzyme that breaks down cGMP and decreases blood flow, if we inhibit it, vasodilation stays longer
Cialis (tadalafil) PDE5 inhib approved for BPH - can treat ED and BPH with one drug! - inhibits cGMP
Viagra (sildenafil) tx for sexual dysfunction in women - for pts who have delayed/absent orgasm? but doesn't affect libido
sildenafil tx for pulmonary arterial hypertension (PAH) - not a very common form of hypertension?
saw palmetto tx for BPH? - not sure if it works
ethinyl estradiol orally active estrogen cmpd used in OC's
mestranol prodrug of ethinyl estradiol
tamoxifen (Nolvadex) SERM breast = ANTAgonist bone = partial AGonist uterus = partial AGonist (can lead to uterine cancer)
toremifene (Fareston) SERM breast = ANTAgonist bone = partial AGonist uterus = partial AGonist (can lead to uterine cancer) *** less agonist action than tamox
raloxifene (Evista) SERM breast = ANTAgonist uterus = ANTAgonist bone = partial AGonist -> tx for osteo, no cancer risk
clomiphene (Clomid) SERM cis is estrogenic, trans is anti-est
mini pills progestin only - primary action to inhibit ovulation by negative fdbk to hypothalamus and AP - also acts by altering endometrium
medroxyprogesterone (Depo Provera) injection every 3 months for contraception
enonogestrel (Implanon) implanted inside upper arm for contra - effective up to 3 years fertility restored promptly
combination OCs progestins added to limit growth of endometrium and promote menses = results in lighter menses
progesterone tx for endometriosis - limits endo growth!
laproscopy surgery to help endometriosis
danazol (Danocrine) decreases FSH and LH and blocks synthesis of est and progest; has weak androgenic activity; causes amenorrhea - tx for endometriosis
progesterone suppress spontaneous abortion
progesterone added into HRT to promote mensses and protect from uterine cancer
0.75 levonorgestrel (Next Choice) progesterone emergency contraceptive - inhib tubular transport of sperm use within 72 hours of sex
1.5 levonorgestrel (Plan B) progesterone emergency contraceptive - inhib tubular transport of sperm use within 72 hours of sex
ulipristal (Ella) partial agonist at progesterone receptors (selective progesterone receptor modulator) - inhibit ovulation/implantation effective up to 5 days after sex
mifepristone (Mifeprex) competitive antagonist at progest recpt. - abortifacient!~!!!! given up to 6 weeks since menses give PG called misoprotol a couple days after to cause uterine contractions
ethinyl estradiol/etonogestrel (NuvaRing) release of steroids is zero order! major effect = inhib of ovulation also affects uterine composition
ethinyl estradiol/norelgestromin (Ortho Evra) release of steroids is zero order! major effect = inhib of ovulation also affects uterine composition
clomiphene (Clomid) fertility = estrogen antagonist competes with estrogen for binding sites in hypo, AP, and ovary -> body releases more LHRH -> more FSH and LH (increase in FSH may result in developmt/release of more than one egg)
goserelin (Zoladex) GnRH AGonist used to suppress LH/FSH - tx for prostate cancer, decr ttone
leuprolide (Lupron) GnRH AGonist used to suppress LH/FSH - tx for endometriosis, decr progest
nafarelin GnRH AGonist used to suppress LH/FSH - tx for precocious puberty given intranasally
cetrorelix GnRH ANTAGonist - may be used in assisted reproduction to suppress premature LH surges -> helps improve implantation - also used as prostate cancer trmt
ganirelix GnRH ANTAGonist - may be used in assisted reproduction to suppress premature LH surges -> helps improve implantation - also used as prostate cancer trmt
levothyroxine (Synthroid) 100% T4 - tx for hypothyroidism
methimazole (Tapazole) thiourea - tx for hyperthyroidism tautomerism = required for binding decrease thyroid peroxidase reactions, decr iodine organification, decr coupling of iodotyrosines (MITS & DITS
carbimazole thiourea - tx for hyperthyroidism tautomerism = required for binding decrease thyroid peroxidase reactions, decr iodine organification, decr coupling of iodotyrosines (MITS & DITS
propylthiouracil (PTU) thiourea - tx for hyperthyroidism ***decr peripher deiodination (PTU ONLY)*** also decr thyroid peroxidase, iodine organification, and coupling of iodotyrosines
radioactive iodine (I131) tx for hyperthyroidism selectively taken up by thryoid - radiation destroys the gland
subtotal thyroidectomy removing part of the gland by surgery - tx for hyperthy risks involved
iodide high conc decr synthesis & release of T3/T4 - used ONLY prior to thyroid surgery
B-blockers as adjuncts tx for hyperthyroidism - may help relieve some of the cardiac manifestations: decr HR, BP, anxiety, tremors
osteoporosis treatments calcium, vit D, calcitonin, bisphosphonates, estrogens, SERMS, androgens, intermittent PTH
etidronate 1st gen bisphosphonate - inhibit resorption at higher doses inhib bone mineralization (NOT WANTED)
clodronate 1st gen bisphosphonate - inhibit resorption at higher doses inhib bone mineralization (NOT WANTED)
pamidronate 2nd gen bisphosphonate -incorporation of aminoalkyl side chain at Cl increase anti-resorptive potency 10=fold **allows for separation between antiresorptive and bone mineralization effects!
alendronate (Fosamax) 2nd gen bisphosphonate -incorporation of aminoalkyl side chain at Cl increase anti-resorptive potency 10=fold **allows for separation between antiresorptive and bone mineralization effects!
risedronate (Actonel) 3rd gen bisphosphonate - incorporation of a nitrogen heterocycle at Cl further enhances anti-resorptive potency
zoledronate (Reclast) 3rd gen bisphosphonate - incorporation of a nitrogen heterocycle at Cl further enhances anti-resorptive potency
ibandronate (Boniva) cross between 2nd & 3rd gen bisphosph
all bisphosphonates (very strong acids!) mech = incorporated into the bone matrix, inhibits further osteoclast activity when encountered - also decrease bone turnover, does reduce bone loss but may effect quality
calcitonin (Miacalcin) action is to lower plasma Ca levels - decr osteoclast activity - decr kidney reabsorp???
estrogen/SERMs inhibit osteoclast activity
teriparatide recombinant formulation of PTH (34 AA sequence identical to N terminal) - stimulate osteoblast function, incr GI Ca absorption, incr renal tubular reabsorp of Ca -> increased bone mineral density and bone mass! possibly bonce cancer though :(
lithium and demeclocycline impair V2 receptor function - can lead to nephrogenic DI - inhibit effects of ADH by post receptor mech
hydrocortisone gcoid activity = 1 mcoid = 1 SHORT ACTING, DOC for replacement?
prednisolone gcoid = 4 mcoid = 0.8 INTERMEDIATE, anti-infl/immunosupp
fludrocortisone gcoid 10 mcoid 125 SHORT, used for mcoid effects
dexamethasone gcoide 25 mcoid ZERO LONG, anti-infl/immunosupp
cortisone gcoid 0.8 mcoid 0.8 SHORT, cheap/inactive
corticosterone gcoid 0.3 mcoid 15 SHORT acting
prednisone gcoid 4 mcoid 0.8 INTERMEDIATE, inactive
methylprednisolone gcoid 5 mcoid 0.5 INTERMEDIATE, anti-infl/immunosupp
triamcinolone gcoid 5 mcoid ZERO INTERMEDIATE, more toxic
betamethasone gcoid 25 mcoid ZERO LONG, anti-infl/immunosupp
aldosterone gcoid ZERO mcoid 500!!!!!!!!! endogenous steroid
systemic gcoid dosage forms oral, IV, IM
topical gcoid dosage forms drops (for eyes, nose), ointments, creams, inhalatns - for local effect
systemic uses for gcoids rheumatoid arthritis, allergies, GI diseases, immunosupp for organ transplant
topical uses for gcoids skin diseases, ocular diseases, asthma
Created by: astephens5
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