2293535
Descrição
FlashCards por lola_smily, atualizado more than 1 year ago
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Criado por lola_smily
mais de 9 anos atrás
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| Questão | Responda |
| histidine | |
| histamine | |
| khellin antihistaminic inhibit histamine release chromone moiety from ammi visnaga bronchodilatory effect (don't reverse bronchoconstriction) | |
| cromolyn sodium antihistaminic inhibit histamine and SRS-A release (locally) bis-chromone no bronchodilatory and antihistaminic effects strictly prophylactic low oral bioavailability (poor absorption) by inhalation (for allergic rhinitis) topically: eye drops (for allergic conjunctivitis) 5-30 min before attack if chronic use: tolerance | |
| nedocromil sodium antihistaminic inhibit histamine release chromone derivative by inhalation: aerosol (for prophylaxis of asthma) ophthalmic solution (for seasonal, perennial allergic conjunctivitis) | |
| lodoxamide antihistaminic mast cell stabilizer (inhibit immediate hypersensitivity reaction) topically: eye (for conjunctivitis) | |
| pemirolast potassium antihistaminic inhibit histamine release pyrimidone | |
| phenbenzamine H1 antihistaminic ethylenediamine SE: sedation, drowsiness, impair mental activity | |
| Tripelennamine H1 antihistaminic ethylenediamine SE: sedation, drowsiness, impair mental activity | |
| pyrilamine H1 antihistaminic ethylenediamine local anesthetic effect (tongue numbness) SE: sedation, drowsiness, impair mental activity | |
| thonzylamine H1 antihistaminic ethylenediamine SE: sedation, drowsiness, impair mental activity | |
| methapyrilene H1 antihistaminic ethylenediamine SE: sedation, drowsiness, impair mental activity | |
| antazoline H1 antihistaminic ethylenediamine SE: sedation, drowsiness, impair mental activity | |
| Diphenhydramine H1 antihistamine ethanolamine ether antihistaminic, antiemetic, antitussive, marked sedation, anticholinergic, antidyskinetic SE: sedation, drowsiness | |
| bromodiphenhydramine H1 antihistamine ethanolamine ether more lipid soluble, more potent antihistaminic, antiemetic, antitussive, marked sedation, anticholinergic, antidyskinetic SE: sedation, drowsiness | |
| chlorodiphenhydramine H1 antihistamine ethanolamine ether more lipid soluble, more potent antihistaminic, antiemetic, antitussive, marked sedation, anticholinergic, antidyskinetic SE: sedation, drowsiness | |
| Doxylamine H1 antihistamine ethanolamine ether most potent CNS depressant hypnotic agent no abuse potential SE: sedation, drowsiness | |
| Carbinoxamine H1 antihistamine ethanolamine ether potent - (rotoxamine)> + (available as racemic mixture) SE: sedation, drowsiness | |
| clemastine H1 antihistamine aminoalkyl ether RR more potent long DOA less anticholinergic less sedation | |
| clemastine H1 antihistamine aminoalkyl ether RR more potent long DOA less anticholinergic less sedation | |
| setastine H1 antihistaminic aminoalkyl ether | |
| cyclizine H1 antihistamine piperazine derivative for nausea, vomiting (from motion sickness and radiation sickness) cyclizine lactate IM injection moderately potent prolonged DOA anticholinergic effects | |
| Chlorcyclizine H1 antihistamine piperazine derivative antiallergic (for urticaria and hay fever) more lipophilic moderately potent prolonged DOA anticholinergic effect | |
| Hydroxyzine H1 antihistaminic piperazine derivative marked sedation antiemetic, antiallergic (for pruritis) at high dose: for anxiety and emotional stress moderately potent prolonged DOA anticholinergic effects | |
| Cetirizine H1 antihistamine piperazine derivative 2nd generation ionized --> less absorbed antinauseant moderately potent prolonged DOA anticholinergic effects | |
| Meclizine H1 antihistamine piperazine derivative for nausea (from motion sickness and radiation sickness) moderately potent prolonged DOA anticholinergic effects | |
| buclizine H1 antihistamine piperazine derivative for nausea (from motion sickness and radiation sickness) moderately potent prolonged DOA anticholinergic effects | |
| oxatomide H1 antihistamine piperazine derivative antimuscarinic, mast cell stabilizer (less release of histamine) moderately potent prolonged DOA anticholinergic effects | |
| chlorpheniramine H1 antihistamine propylamine derivative 10X > potent than pheniramine + > - longer acting than pheniramine t 1/2 = 12-15 h | |
| Dexchloropheniramine H1 antihistamine propylamine derivative dextropheniramine | |
| bromopheninramine H1 antihistamine propylamine derivative 10X > potent than pheniramine + > - longer acting than chlorpheniramine t 1/2 = 25h | |
| Dexbromopheniramine H1 antihistamine propylamine derivative | |
| E-pyrrobutamine (pyronil) H1 antihistamine propylamine unsaturated pheniramine potent (E (165X) > Z) t1/2 = 12h --> long acting | |
| triprolidine H1 antihistamine propylamine unsaturated pheniramine potent (E (100X) > Z) t1/2 = 12h --> long acting | |
| demethindine H1 antihistamine propylamine unsaturated pheniramine potent (- > +) | |
| phenindamine H1 antihistamine propylamine unsaturated pheniramine moderately potent cause CNS stimulation, insomnia | |
| Promethazine H1 antihistamine tricyclic phenothiazine moderately potent antiemetic, antianxiety pronounced sedation potentiate analgesics long DOA drowsiness | |
| pyrathiazine H1 antihistamine tricyclic phenothiazine moderately potent antiemetic, antianxiety pronounced sedation potentiate analgesics long DOA drowsiness | |
| trimeprazine H1 antihistamine tricyclic phenothiazine less antihistaminic, more neuroleptic activity (spacer 3 C) moderately potent antiemetic, antianxiety pronounced sedation potentiate analgesics long DOA drowsiness | |
| methdiazine H1 antihistamine tricyclic phenothiazine less antihistaminic, more neuroleptic activity (spacer 3 C) moderately potent antiemetic, antianxiety pronounced sedation potentiate analgesics long DOA drowsiness | |
| pimethixene H1 antihistamine tricyclic thioxanthene derivative orally active | |
| methixene H1 antihistamine tricyclic moderately potent anticholinergic usefull in parkinson | |
| cyproheptadine H1 antihistamine tricyclic anticholinergic antiserotonergic appetite stimulating effect for anorexia nervosa | |
| azatadine H1 antihistamine tricyclic aza isostere potent long acting anticholinergic | |
| ketotifen H1 antihistamine tricyclic potent mast cell stabilizer topically (for seasonal allergic conjunctivitis) nasal spray (for allergic rhinitis) | |
| terfenadine H1 antihistamine 2nd generation less or no: anticholinergic, sedation low affinity to adrenergic and serotonergic effects QT prolongation, torsade de pointes give fexofenadine | |
| fexofenadine H1 antihistamine 2nd generation less or no: anticholinergic, sedation low affinity to adrenergic and serotonergic effects active safer | |
| ebastine H1 antihistamine 2nd generation potent long acting less or no: anticholinergic, sedation low affinity to adrenergic and serotonergic effects from terfenadine | |
| cetirizine H1 antihistamine 2nd generation metabolite of hydroxyzine levo (30X): levocetirizine > dextro less or no: anticholinergic, sedation low affinity to adrenergic and serotonergic effects | |
| loratadine H1 antihistamine 2nd generation metabolite of azatadine long acting tricyclic less or no: anticholinergic, sedation low affinity to adrenergic and serotonergic effects forms desloratadine | |
| acrivastine H1 antihistamine 2nd generation metabolite of tripolidine lacks CNS effects less or no: anticholinergic, sedation low affinity to adrenergic and serotonergic effects | |
| mizolastine H1 antihistamine 2nd generation long acting less or no: anticholinergic, sedation low affinity to adrenergic and serotonergic effects metabolized into inactive | |
| astemizole H1 antihistamine 2nd generation less or no: anticholinergic, sedation low affinity to adrenergic and serotonergic effects | |
| carebastine H1 antihistamine 2nd generation less or no: anticholinergic, sedation low affinity to adrenergic and serotonergic effects | |
| desloratadine H1 antihistamine 2nd generation less or no: anticholinergic, sedation low affinity to adrenergic and serotonergic effects | |
| burimamide H2 antihistamine 1st generation antiulcer thiurea derivative poor oral bioavailability low potency for GERD treatment | |
| metiamide H2 antihistamine 1st generation antiulcer thiourea derivative orally active potent agranulocytosis for GERD treatment | |
| cimetidine H2 antihistamine 1st generation antiulcer cyanoguanidine derivative orally active potent antiandrogenic effect, CYP inhibition metabolized to S-oxide (inactive) for GERD treatment | |
| Ranitidine H2 antihistamine 2nd generation antiulcer orally active (30-80% bioavailable) potent (4-10X more than cimetidine) weaker inhibitor of CYP enzymes no antiandrogenic effects renal elimination metabolized: N-desmethyl, S-oxide, N-oxide for GERD treatment | |
| nizatidine H2 antihistamine 2nd generation antiulcer orally active (75-100% bioavailable) potent (5-18X more than cimetidine) not an inhibitor of CYP enzymes no antiandrogenic effects renal elimination metabolized: N-desmethyl, S-oxide, N-oxide for GERD treatment | |
| famotidine H2 antihistamine 2nd generation antiulcer orally active (40-45% bioavailable) more potent not an inhibitor of CYP enzymes no antiandrogenic effects for GERD treatment | |
| omeprazole antiulcer proton pump inhibitor (H+/K+ ATPase) 2-pyridylmethylsulfinylbenzimidazole derivative irreversible inhibitors for activation: acidic media--> sulfenic acid, sulfenamide (active, bind irreversibly by covalent bond) metabolites: methyl hydroxylation, O-demethylation (CYP2C19) sulfoxidation (CYP3A4) clearance: R(+) --> rapidly, metabolized by CYP2C19 S(-)--> esomeprazole, metabolized by CYP3A4 | |
| Esomeprazol antiulcer proton pump inhibitor(H+/K+ ATPase) 2-pyridylmethylsulfinylbenzimidazole derivative irreversible inhibitors S (-) omeprazole metabolized by CYP3A4 | |
| tenatoprazole antiulcer proton pump inhibitor(H+/K+ ATPase) irreversible inhibitors imidazopyridine derivative | |
| lansoprazole antiulcer proton pump inhibitor(H+/K+ ATPase) 2-pyridylmethylsulfinylbenzimidazole derivative irreversible inhibitors | |
| Rabeprazole antiulcer proton pump inhibitor(H+/K+ ATPase) 2-pyridylmethylsulfinylbenzimidazole derivative irreversible inhibitors thio ether | |
| pantoprazole antiulcer proton pump inhibitor(H+/K+ ATPase) 2-pyridylmethylsulfinylbenzimidazole derivative irreversible inhibitors | |
| misoprostol antiulcer semisynthetic prostaglandin E1 derivative ester prodrug abotifacient agent (causes abortion) de-esterification --> active metabolite (not by 16-hydroxydehydrogenase) abuse potential | |
| prostaglandin E1 antiulcer maintain mucosal integrity, protect gastric wall | |
| sucralfate antiulcer aluminium hydroxide complex of octasulfate ester of sucrose small amount absorbed systematically synthesize: prostaglandin, bicarbonate, epidermal, fibroblast growth factors decrease absorption of: H2 antihistamine, quinolone antibiotic, phenytoin, warfarin | |
| carbenoxolone antiulcer steroid like from licorice mineralocorticoid activity (SE) inhibit PG inactivation | |
| pirenzepine antiulcer anticholinergic selective M1 receptor antagonist decrease GI acid secretion, intestinal mobility | |
| telenzepine antiulcer anticholinergic selective M1 receptor antagonist decrease GI acid secretion, intestinal mobility | |
| steroid backbone | |
| steroid template | |
| phenantrene | |
| cholestane template | |
| 5-beta-cholestane cis isomer | |
| 5-beta-cholestane cis isomer | |
| 5-alpha-cholestane trans isomer | |
| 5-alpha-cholestane trans isomer precursor of cholesterol | |
| 5-alpha-pregnane steroid precursor of progesterone and hydrocortisone (cortisol) | |
| 5-alpha-androstane steroid precursor of testosterone and dehydroepiandrosterone | |
| 5-alpha-estrane steroid precursor of estradiol | |
| cholesterol steroid adrenocorticoid cholest-5-en-3-beta-ol formed from acetyl CoA and acetoacetyl CoA forms pregnenolone, bile acids (glycocholic acid, taurocholic acid) | |
| progesterone steroid adrenocorticoid pregn-4-ene-3,20-dione | |
| hydrocortisone (cortisol) steroid adrenocorticoid 11-beta-17-alpha-21-trihydroxy-pregn-4-ene-3,20-dione short acting active metabolized to cortisone, inactive metabolites orally: completely absorbed (>95% bioavailability) t1/2 = 1-2h IM (acetate): slowly absorbed longer duration of action intrarectally: poorly absorbed | |
| testosterone steroid 17-beta-hydroxyandrost-4-ene-3-one | |
| dehydroepiandrosterone DHEA steroid | |
| 17-beta-estradiol steroid 1,3,5(10)-estratien-3,17-beta-diol | |
| cortisone steroid 17-alpha-21-dihydroxypregn-4-ene-3,11,20-trione natural short acting t1/2= 1-1.5h active orally/ IM (21-acetate): slowly absorbed, longer duration SE: Na/H2O retention, K excretion, increase gastric acid secretion, gluconeogenesis, increase nitrogen excretion | |
| estrone steroid 1,3,5(10)-estratrien-3-ol-17-one | |
| pregnenolone steroid adrenocorticoid metabolite of oxidation of cholesterol active | |
| aldosterone steroid adrenocorticoid from cholesterol active | |
| 11-epicortisol steroid first analogue | |
| hydrocortisone acetate steroid mineralocorticoid and glucocorticoid act. for replacement therapy (adrenocortical deficiency) for rheumatoid arthritis --> caus abnormal metabolic function SE: Na/H2O retention, K excretion, increase gastric acid secretion, gluconeogenesis, increase nitrogen excretion | |
| hydrocortisone cypionate steroid 21-(3-cyclopentylpropionate) ester water insoluble orally mineralocorticoid and glucocorticoid act. for replacement therapy (adrenocortical deficiency) for rheumatoid arthritis --> caus abnormal metabolic function SE: Na/H2O retention, K excretion, increase gastric acid secretion, gluconeogenesis, increase nitrogen excretion | |
| hydrocortisone butyrate steroid 17-alpha-butyrate-ester topically mineralocorticoid and glucocorticoid act. for replacement therapy (adrenocortical deficiency) for rheumatoid arthritis --> caus abnormal metabolic function SE: Na/H2O retention, K excretion, increase gastric acid secretion, gluconeogenesis, increase nitrogen excretion | |
| hydrocortisone buteprate steroid 17-alpha-butyrate, 21-propionate ester mineralocorticoid and glucocorticoid act. for replacement therapy (adrenocortical deficiency) for rheumatoid arthritis --> caus abnormal metabolic function SE: Na/H2O retention, K excretion, increase gastric acid secretion, gluconeogenesis, increase nitrogen excretion | |
| hydrocortisone valerate steroid 17-alpha-valerate ester topically mineralocorticoid and glucocorticoid act. for replacement therapy (adrenocortical deficiency) for rheumatoid arthritis --> caus abnormal metabolic function SE: Na/H2O retention, K excretion, increase gastric acid secretion, gluconeogenesis, increase nitrogen excretion | |
| hydrocortisone sodium succinate steroid 21-sodium succinate ester extremely water soluble IV/IM slowly and incompletely hydrolyzed t1/2= 30minmineralocorticoid and glucocorticoid act. for replacement therapy (adrenocortical deficiency) for rheumatoid arthritis --> caus abnormal metabolic function SE: Na/H2O retention, K excretion, increase gastric acid secretion, gluconeogenesis, increase nitrogen excretion | |
| hydrocortisone sodium phosphate steroid 21-sodium phosphate ester extremely water soluble IV/IM completely and rapidly metabolized t1/2= 10min mineralocorticoid and glucocorticoid act. for replacement therapy (adrenocortical deficiency) for rheumatoid arthritis --> caus abnormal metabolic function SE: Na/H2O retention, K excretion, increase gastric acid secretion, gluconeogenesis, increase nitrogen excretion | |
| fludrocortisone steroid orally active high glucocorticoid activity increase stability of 11-beta-OH if Br at 9: increase 11X glucocorticoid, increase 300-800X mineralocorticoid for adrenocortical insufficiency: addison's disease | |
| fludrocortisone acetate steroid orally active high glucocorticoid activity increase stability of 11-beta-OH if Br at 9: increase 11X glucocorticoid, increase 300-800X mineralocorticoid for adrenocortical insufficiency: addison's disease | |
| prednisolone steroid delta 1-hydrocortisone longer acting more glucocorticoid act (3-4) than mineralocorticoid act. (1) 4-5X more potent less salt retention | |
| 6-beta-hydroxyprednisolone steroid metabolite of prednisolone active | |
| 16-alpha-hydroxyprednisolone steroid metabolite of prednisolone active | |
| 20-hydroxyprednisolone steroid metabolite of prednisolone inactive | |
| Prednisolone acetate steroid delta corticosteroid | |
| prednisolone t-butylacetate steroid delta corticosteroid | |
| prednisolone sodium phosphate steroid delta corticosteroid | |
| methylprednisolone steroid methyl corticoid 6-alpha-methyl analogue of prednisolone potent glucocorticoid negligible mineralocorticoid | |
| methylprednisolone 21-acetate steroid methyl corticoid | |
| methylprednisolone sodium succinate steroid methyl corticoid | |
| triamcinolone steroid 9-alpha fluro-16-alpha OH prednisolone more potent less water retention SE: anorexia, weight loss, nausea, dizziness, muscle weakness | |
| Dexamethasone steroid 9-alpha fluro-16-alpha methyl higher stability of 20-keto group 5X more potent as anti-inflammatory (compared to prednisolone, hydrocortisone) SE: excessive appetite, weight gain, abdominal distention | |
| Dexamethasone 21-acetate steroid | |
| dexamethasone sodium phosphate steroid | |
| betamethasone steroid 9-alpha fluro-16-beta CH3 no advantage same potency, same SE as dexamethasone | |
| flurandrenolide steroid topical glucocorticoid high activity high lipid solubility (acetonides) potent local/topical antiinflammatory effect (for short duration) metabolized in liver excreted in bile or urine | |
| fluocinolone acetonide steroid topical glucocorticoid high activity high lipid solubility (acetonides) potent local/topical antiinflammatory effect (for short duration) metabolized in liver excreted in bile or urine | |
| fluocinonide steroid topical glucocorticoid high activity high lipid solubility (acetonides) potent local/topical antiinflammatory effect (for short duration) metabolized in liver excreted in bile or urine | |
| halcinonide steroid topical glucocorticoid high activity high lipid solubility (acetonides) potent local/topical antiinflammatory effect (for short duration) metabolized in liver excreted in bile or urine | |
| desonide steroid topical glucocorticoid high lipid solubility (acetonides) potent local/topical antiinflammatory effect (for short duration) metabolized in liver excreted in bile or urine | |
| amcinonide steroid topical glucocorticoid high activity high lipid solubility (acetonides) potent local/topical antiinflammatory effect (for short duration) metabolized in liver excreted in bile or urine | |
| clobetasol propionate steroid topical glucocorticoid high activity high lipid solubility very potent local/topical antiinflammatory effect (for short duration) metabolized in liver excreted in bile or urine | |
| alcometasone steroid topical glucocorticoid low potent (for chronic use) metabolized in liver excreted in bile or urine | |
| flumethasone steroid topical glucocorticoid high activity potent local/topical antiinflammatory effect (for short duration) metabolized in liver excreted in bile or urine | |
| diflorasone diacetate steroid topical glucocorticoid high activity high lipid solubility very potent local/topical antiinflammatory effect (for short duration) metabolized in liver excreted in bile or urine | |
| desoximetasone steroid topical glucocorticoid high activity high lipid solubility potent local/topical antiinflammatory effect (for short duration) metabolized in liver excreted in bile or urine | |
| beclomethasone steroid topical glucocorticoid high lipid solubility potent local/topical antiinflammatory effect (for short duration) metabolized in liver excreted in bile or urine | |
| beclomethasone dipropionate steroid topical glucocorticoid high lipid solubility very potent local/topical antiinflammatory effect (for short duration) 5000X more potent than hydrocortisone 500X more potent than betamethasone 5X more potent than fluocinolone acetonide or triamcinolone acetonide metabolized in liver excreted in bile or urine | |
| halobetasol propionate steroid topical glucocorticoid high lipid solubility very potent local/topical antiinflammatory effect (for short duration) 6% systemically absorbed metabolized in liver excreted in bile or urine | |
| diflucortolone pivalate steroid topical glucocorticoid high activity high lipid solubility potent local/topical antiinflammatory effect (for short duration) metabolized in liver excreted in bile or urine | |
| prednicarbate steroid topical glucocorticoid low potency (for chronic use) metabolized in liver excreted in bile or urine | |
| fluorometholone acetate steroid topical glucocorticoid high activity high lipid solubility potent local/topical antiinflammatory effect (for short duration) metabolized in liver excreted in bile or urine | |
| triamcinolone acetonide steriod inhaled/intranasal corticosteroid high activity high potency | |
| flunisolide steriod inhaled/intranasal corticosteroid high activity high potency | |
| fluticasone propionate steriod inhaled/intranasal corticosteroid high activity high potency | |
| budesonide steriod inhaled/intranasal corticosteroid high potency | |
| mometasone furoate steriod inhaled/intranasal corticosteroid | |
| androstenedione steroid precursor of testosterone and estradiol | |
| estrone steroid precursor of estradiol | |
| testosterone steroid precursor of estradiol | |
| estradiol steroid estra-1,3,5(10)-triene-3,17beta-diol most potent | |
| estriol steroid metabolite of estradiol least active least potent | |
| estradiol steroid estrogen derivative | |
| estriol steroid estrogen derivative | |
| estrone steroid estrogen derivative | |
| estradiol 3-benzoate steroid estrogen derivative prodrug IM | |
| estradiol 17-valerate steroid estrogen derivative prodrug IM | |
| estradiol 17-cypionate steroid estrogen derivative prodrug IM | |
| ethinyl estradiol steroid estrogen derivative orally active similar potency to estradiol (injection) more potent (15-20X) than estradiol (orally) | |
| mestranol ethinyl estradiol 3-methylether steroid estrogen derivative prodrug oral contraceptive metabolized to ethinyl estradiol | |
| quinestrol steroid estrogen derivative 3-cyclopentyl ether of ethinyl estradiol prodrug most orally active long acting hydrolyzed by dealkylation lipid soluble (stored in body fat), slowly released | |
| sodium estrone sulfate steroid conjugated estrogen hydrolyzed to estrone | |
| equilin sodium sulfate steroid conjugated estrogen low activity (unsaturation in ring B) | |
| sodium equilenin sulfate steroid conjugated estrogen low activity (unsaturated ring B) | |
| piperazine estrone sulfate steroid conjugates estrogen salt | |
| diethylstilbestrol non steroidal estrogen orally active slowly metabolized long term use in pregnancy: increase risk of breast cancer diphosphate form used for: prostate cancer | |
| dienestrol nonsteroidal estrogen | |
| benzestrol non steroidal estrogen no double bonds | |
| hexestrol non steroidal estrogen no double bonds trans better | |
| coumestrol phytoestrogen natural plant substance from legumes | |
| genistein phytoestrogen natural plant substance from soybean and clover example of flavonoids | |
| daidzein phytoestrogen natural plant substance from soybean example of flavonoids | |
| tamoxifen estrogen antagonist antiestrogen orally active Z isomer SERM (selective estrogen receptor modifier) estrogen antagonist in breast (for estrogen dependent breast cancer) estrogen agonist in uterus and bones metabolized by CYP3A4, 2D6 | |
| N-demethyltamoxifen metabolite of tamoxifen by 3A4 active | |
| 4-hydroxytamoxifen metabolite of tamoxifen by 2D6 more active than tamoxifen | |
| toremifene antiestrogen triphenylethylene chlorotamoxifen metabolized by CYP3A4, deamination-hydroxylation in liver (caution if liver disease) SE: hot flashes, nausea, platelet reduction, endometrial cancer | |
| N-demethyltoremifene metabolite of toremifene by CYP3A4 active | |
| ospemifene metabolite of toremifene by deamination-hydroxylation active | |
| enclomiphene antiestrogen E isomer stimulate ovulation in women desiring pregnancy | |
| zuclomiphene antiestrogen Z isomer stimulate ovulation in women desiring pregnancy | |
| raloxifene antiestrogen benzothiophene SERM estrogen antagonist: on endometrium and breast tissues estrogen agonist: on bones and cardiovascular to treat and prevent osteoporosis in postmenopausal extensive first pass metabolism (to active) --> low oral bioavailability | |
| fulvestrant pure antiestrogen hydrophobic side chain poor oral bioavailability IM prevent growth of tamoxifen resistant breast cancer metabolized to active and less active for pregnant women taking anticoagulant/ have thrombocytopenia SE: GI symptoms, headache, hot flashes | |
| exemestane aromatase (estrogen biosynthesis) inhibitor steroidal derivative (type 1 inhibitors) 10-beta-propynylestr-4-ene-3,17-dione for breast cancer decrease estrogen: 85-95% in 2-3 days no CYP effect metabolite: 17-hydroxy metabolite --> active, higher affinity to receptor | |
| formestane aromatase (estrogen biosynthesis) inhibitor irreversible inhibitor steroidal derivative (type 1 inhibitors) 4-hydroxyandrostenedione for breast cancer given parenterally (no oral activity) | |
| anastrozole aromatase (estrogen biosynthesis) inhibitor triazole (type 2 inhibitors) selective first line in advanced breast cancer in postmenopausal women decrease estrogen: 80% in 2 weeks long t1/2 = 50h (once daily) metabolized to inactive inhibit CYP 1A2, 2C9, 3A4 | |
| letrozole aromatase (estrogen biosynthesis) inhibitor triazole (type 2 inhibitors) selective decrease estrogen: 75-90% in 2-3 days metabolized to inactive | |
| progesterone steroid female sex hormone t1/2= 5-10min renally excreted: glucuronide (miscarriage index), sulfate conjugate (5-beta-pregnanediol) | |
| 20-alpha/beta-hydroxyprogesterone steroid metabolite of progesterone by reduction of 20 ketone | |
| 5-beta-pregnanediol steroid metabolite of progesterone by reduction of 4,5 double bond | |
| 6-alpha-hydroxyprogesterone steroid metabolite of progesterone by hydroxylation at C6 | |
| ethisterone steroid testosterone derivative 17-alpha alkyl derivative orally active | |
| dimethisterone steroid testosterone derivative 17-alpha alkyl derivative orally active | |
| 19-norprogesterone steroid testosterone derivative | |
| norethindrone steroid 19-nortestosterone derivative potent (10x > norethynodrel) orally active | |
| norethindrone acetate steroid 19-nortestosterone derivative orally administered/ transdermally metabolized by deacetylation (rapidly,completely) in GI and liver--> norethindrone | |
| norethynodrel steroid 19-nortestosterone derivative potent orally active | |
| ethynodiol diacetate steroid 19-nortestosterone derivative prodrug | |
| norgestrel steroid 19-nortestosterone derivative orally active (oral contraceptives) | |
| levonorgestrel steroid 19-nortestosterone derivative active isomer orally active (OC) weak androgenic activity no glucocorticoid, mineralocorticoid act. | |
| norgestimate steroid levonorgestrel derivative prodrug metabolized to 2 active metabolites (norelgestromine (in intestine, liver), levonorgestrel (in liver)) in mono, triphasic OC few androgenic SE | |
| desogestrel steroid levonorgestrel derivative prodrug metabolized rapidly to active metabolite (etenogestrel) in intestinal mucosa and first pass oral bioavailability: 84% in mono and triphasic OC few androgenic SE | |
| etonogestrel steroid levonorgestrel derivative active metabolite of desogestrel | |
| gestodene steroid levonorgestrel derivative oral bioavailability: 100% (not prodrug) excellent progesterone receptor binding affinity in mono and triphasic OC--> small increase in triglyceride/total cholest levels | |
| 17-alpha-acetoxyprogesterone steroid progesterone derivative limited activity orally undergoes 6-alpha hydroxylation | |
| medroxyprogesterone acetate steroid progesterone derivative 25X active > ethisterone orally administered completely, rapidly metabolized by first pass (deacetylation) --> medroxyprogesterone (metabolized like progesterone) metabolites excreted in urine (glucuronide conjugates) | |
| megestrol acetate steroid progesterone derivative from medroxyprogesterone acetate progestin activity for treatment of breast, endometrial cancer/ hormone dependent carcinoma | |
| dienogest steroid 19-nortestosterone estrane skeleton, C17 cyanomethyl group, C9,10 double bond in OC preparation | |
| drospirenone steroid 19-norprogesterone from spironolactone antimineralocorticoid activity (5x affinity to receptor > aldosterone) antiandrogenic action progestin activity (10% of levonorgestrel) | |
| elcometrine steroid 19-norprogesterone derivative potent SQ (100x more potent than orally), intravaginally, transdermally antiestrogenic action no androgenic/antiandrogenic activity | |
| nomegestrol acetate steroid 19-norprogesterone derivative better selectivity, more potent (than medroxyprogesterone acetate) in OC preparations no glucocorticoid/antimineralocorticoid/ androgenic act has significant antiandrogenic action | |
| trimegestone steroid 19-norprogesterone derivative most potent high affinity to progesterone receptor weak affinity to mineralocorticoid receptor no glucocorticoid/androgenic/ antiandrogenic act metabolic hydroxylation --> metabolites with progestogenic action | |
| mifepristone steroid progesterone antagonist orally active rapidly absorbed bioavailability: 70% antiglucocorticoid act metabolism: mono,di-dealkylation, 17-propyl hydroxylation-->inactive metabolite fecal elimination (83%) for hormone dependent breast cancer | |
| onapristone steroid progesterone antagonist less antiglucocorticoid act for hormone dependent breast cancer | |
| telapristone acetate steroid progesterone antagonist for hormone dependent breast cancer | |
| ulipristal acetate steroid progesterone antagonist very high affinity to progesterone receptor (selective) reduce effect of hormonal contraceptive delay/inhibit ovulation alter endometrium to prevent uterine implantation metabolism: mono --> active, di-dealkylation | |
| testosterone steroid male sex hormone from androstenedione do nitrogen retention: increasing the rate of protein synthesis and muscle mass, decrease in the rate of protein catabolism have androgenic activity (development of male reproductive tissues) / anabolic activity (cell growth,protein synthesis..) | |
| 5-alpha-dihydrotestosterone steroid metabolite of testosterone most potent endogenous androgen | |
| 17-alpha-methyltestosterone steroid testosterone derivative DOA: 24h | |
| oxymesterone steroid testosterone derivative | |
| methandrostenolone steroid testosterone derivative | |
| fluoxymesterone steroid testosterone derivative DOA: 24h | |
| testosterone 17-beta-propionate steroid testosterone derivative DOA: 1-2w | |
| testosterone 17-beta-enanthate steroid testosterone derivative depot ester DOA: 2-4 w | |
| testosterone 17-beta-undecanoate steroid testosterone derivative DOA: 10h | |
| testosterone 17-beta-cyclopentylpropionate (cypionate) steroid testosterone derivative depot ester DOA: 2-4 w | |
| oxandrolone steroid 17-alkylated derivative 2-oxasteroid analogue with lactone moiety 3x anabolic act (>17-methyltestosterone) slight androgenic act | |
| stanozolol steroid 17-alkylated derivative pyrazole derivative anabolic act | |
| testolactone steroid 17-alkylated derivative 18-oxasteroid anabolic act little androgenic act irreversible aromatase inhibitor | |
| norethandrolone steroid 19-norandrogens better anabolic act | |
| nandrolone decanoate steroid 19-norandrogen IM slow hydrolysis | |
| nandrolone phenylpropionate steroid 19-norandrogen IM slow hydrolysis | |
| methenolone acetate steroid potent anabolic act no alkyl on C17 orally/injection | |
| oxymetholone steroid 17-alkylated derivative anabolic act | |
| chlortestosterone acetate steroid anabolic act | |
| ethylestrenol steroid 17-alkylated derivative anabolic act | |
| desoxymethyltestosterone steroid illegal anabolic agent difficult to trace | |
| tetrahydrogestrinone steroid illegal anabolic agent difficult to trace to build up cattle | |
| gestrinone steroid illegal anabolic agent difficult to trace | |
| trenbolone steroid illegal anabolic agent difficult to trace | |
| 3-trifluoromethyl-4-nitroaniline antiandrogens precursor | |
| flutamide antiandrogens nonsteroidal synthetic Competitive inhibitors (to testosterone and DHT) of androgen receptor given 3x/day | |
| bicalutamide antiandrogens nonsteroidal synthetic orally active Competitive inhibitors (to testosterone and DHT) of androgen receptor metabolized: hydroxyl metabolite -->active (in liver) less hepatotoxicity SE: vasomotor flushing, gynecomastia, decreases libido, decreased potency | |
| nilutamide antiandrogens nonsteroidal synthetic Competitive inhibitors (to testosterone and DHT) of androgen receptor SE: vasomotor flushing, gynecomastia, decreases libido, decreased potency, hepatotoxicity | |
| hydroxyflutamide metabolite of flutamide more potent antiandrogen | |
| finasteride steroid 5-alpha reductase inhibitor (tightly) irreversible competitive inhibition relatively selective for type II potent slow t1/2=30d 1mg suppress DHT (70% in plasma, 85-90% in prostate in 24h) metabolism: CYP3A4 (liver) elimination: renal (40%), fecal | |
| dutasteride steroid 5-alpha reductase inhibitor (tightly) irreversible competitive inhibition for 2 types orally active more potent 0.5mg/day for 2w suppress DHT (90% in plasma) to treat BPH metabolism: CYP3A4 (liver), parahydroxy metabolite --> active elimination: renal, fecal (40%) |
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