click below
click below
Normal Size Small Size show me how
PDA II - Classes/MoA
Exam 1
| Question | Answer |
|---|---|
| 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 |