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Pharma- mechanisms of action-endocrine, GIT, MSK

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summerahmed's version from 2015-06-28 12:28

endocrine

Question Answer
insulin rapid acting, aspart, glulisine, lisprobind insulin receptor(tyrosine kinase activity), liver: increase glucose stored as glycogen. muscle: increase glycogen, protein synthesis, increase K uptake. fat: increase TG storage
insulin short acting, regularbind insulin receptor(tyrosine kinase activity), liver: increase glucose stored as glycogen. muscle: increase glycogen, protein synthesis, increase K uptake. fat: increase TG storage
insulin intermediate acting NPHbind insulin receptor(tyrosine kinase activity), liver: increase glucose stored as glycogen. muscle: increase glycogen, protein synthesis, increase K uptake. fat: increase TG storage
insulin Long acting, detemir, glarginebind insulin receptor(tyrosine kinase activity), liver: increase glucose stored as glycogen. muscle: increase glycogen, protein synthesis, increase K uptake. fat: increase TG storage
biguanide, metforminexact mechanism unknown, decreases gluconeogenisis, increase glycolysis, increase periopheral glucose uptake. increase insulin sensitivity
sulfonylureas, first generation:chlorpropramide, tolbutamide. 2nd generation: glimiperide, glipizide,gliburidecloses K channel in B cell memebrane, cell depolarizes, insulin release via Ca influx
glitazone, thiazolidinediones: pioglitazone, rosiglitazineincrease insulin sensitivity in peripheral tissue, bind to PPAR-gamma nuclear transcription regulator of fatty acid storage and glucose metabolism its activation increases insulin sensitivity and levels of adiponectin
GLP-1 analog: exenatide, liraglutideincrease insulin and decrease glucagin release
DPP-4 inhibitor: linagleptin, saxagliptin, sitagliptinincrease insulin and decrease glucagin release
amylin analog:pramlintidedecrease gastric emptying, decrease glucagon
SGLT-2 inhibitor: canagliflozinblock reabsorption of glucose n PCT
alpha- glucosidase inhibitors: acarbose, miglitolinhibit intestinal brush border alpha-glucosidase. delayed CHO absorption and decrease postprandial hyperglycemia
propylthiouracil, methimazoleblock thyroid peroxidase, inhibit the oxidation of iodide and the organification( coupling) of iodine, leads to inhibition of thyroid hormone synthesis, propylthiouracil: also block 5-deiododinase so decreases the perioheral conversion of T4 TO T3
levothyroxin T4, triiodothyronine T3thyroid hormone replacement
conivaptan, tolvaptanADH antagonists at V2 receptor to ttt SIADH
desmopressin acetatecentral DI
oxytocinstimulate labour, uterine contraction, milk let down and utrine hges
octreotide, somatostatinacromegalu, carcinoid syndrome, gastrinoma, esophegeal varices, glucagonoma
demeclocyclineADH antagonist of tetracycline family
beclomethasone, dexamethasone, fludrocortisone, hydrocortisone, methylpredinisolone, prednisone, triamcinilonemetabolic, catabolic, antiinflamatory, immunesuppressive effects. inhibition of phospholipase A2 and inhibition of transcription factor NF-KB
Cinacalcetsensetizes Ca sensing receptors (CaSR) in parathyroid gland to circulating Ca, so decreases PTH, given in hypercalceamia d2 1ry or 2ry hyperparathyroidism
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Gastrointestinal :

Question Answer
H2 blockers, cemitidine, ranitidine,famotidine, niztidinerevirsable blocking of histamine H2 receptordecreasing the H secretion by parietal cells
proton pump inhibitors, omeprazole,lansoprazole,esmoprazo9le, pantobrazole,dexlansoprazoleirrevirsable inhibition of the H/K atpase in stomach prietal cells
bisthmusbind to ulcer base providing physical protection and allowing HCO3 secretion to reestablish pH gradiengt in mucus layer
sacralfatebind to ulcer base providing physical protection and allowing HCO3 secretion to reestablish pH gradiengt in mucus layer
misoprostola PGE1 analog increase production and secretion of gastric mucus barrier . decreases acid production
octreotidelong acting somatostatin analog inhibit the action of many splanchnic vasoconstriction hormones
antacidsalumunium hydroxide, calcium carbonate, magnesium hydroxide.
osmotic laxative, magnesium hyroxide, magnesium citrate, polyethylene glycol, laculoseprovide osmotic load that draw water into the GI lumen
salfasalazinea combination of sulfapyridine(antibacterial) and 5aminosalycilic acid (antinflamatory) activated by colonic flora
odansetron5HT3 antagonist decrease vagal stimulation powerful central acting antiemetic
meteclopromideD2 receptor antagonist increase resting tone, contactility, LES tone motility does not influence colon transport time
orlistatinhibit gastric and pancreatic lipase decrease the breakdoen and the absorption of dietary fats
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MSK

Question Answer
acetamenophenreversibly inhibit COX mostly in CNS and inactivated peripherally
asprinirreversibly inhibit COX 1 and 2 by acetylation which decreases the synthesis of TXA2 and prostaglandins and increases the bleeding time and no effect on the PT. PTT.
celecoxibreversibly inhibit COX2 which is found in inflamatory cells and vascular endothelimand mediates pain and inflamation spares COX1 which helps maintain gastric mucosa thus doesnt have as corrisive effects as other NSAIDs do on the Gi lining spares platelet function because TXA2 production is dependant on COX1
NSAIDs, iboprofen, naproxen, indomethacin, ketorlac, diclofinacrevirsible inhibition of both COX1, 2 and block prostaglandins synthesis
bisphosphonate, alendronate, other dronatespyrophosphate analog dind hydroxy apetite n bone inhibiting the osteoclast activity
teriparatiderecombinant PTH analog given SC daily to increase the osteoblastic activity
allupurinolinhibit xanthine oxidase after being converted to allxanthine. decreses the cinversion of xanthine to uric acid also used in lymphome and leaukeamia to prevent tumor-lysis associated urate nephropathy. increases the concentration of azathioprine and 6MP because are normally metabllized by xantine oxidase
febuxostatinhibits xanthine oxidase
pegloticaserecombinant uricase that catalyzes the metabolism of uric acid to allantoin ( a more water soluble product )
probencidinhibits the reabsorption of uric acid in proximal convuluted tubules also inhibits the secretion of penicillin can ppt uric acid in calaciluli
anti gout NSAIDSnaproxen and indomethacin
cochicinebonds and stabilizes the tubulin to inhibit microtubulr polymarization impairing neutrophil chemotaxis and degranulation. it has acute prophylactic value
etanreceptTNF-ALPHA inhibitor. fusion protein (receptor for tnf-alpha + IGgFc) produced by recombinent DNA -decoy receptor
infliximab, adalimumabanti TNF-alpha monoclonal antibody
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reproductive :

Question Answer
leuprolideGnRH analog with agonist properties when used in pulsatile fashion. antagonist properties when used in continueous fashion ( downregulates GnRH receptor in pituitary decreases FSH and LH.
estrogen, ethinyl estradiol, DESm mestranolbind the estrogen receptors
clomipheneSERM antagonist estrogen receptor in hypothalamus, prevents normal feedback inhibition and increase the release of LH and FSH from pituitary which stimulates ovulation used to ttt infertility d2 anovulation.
tamoxifenantagonist on breast and agonist on bone and uterus
raloxifenantagonist at breast, uterus and agonist on bone used primiral;ity to ttt osteoprosis
anastrazolearomatase inhibitor used in postmenopausal females with ER +ve breast cancer
exemestanearomatase inhibitor used in postmenopausal females with ER +ve breast cancer
progestinsbind to progesterone receptor decrease the groth and increase vascularization of endometrium
mifepristone RU486competitive inhibition of progestin at progesterone receptors
oral contraceptivesestrogen and progesterone that inhibit LH and FSH and thus prevent estrogen surge no estrogen surge means no LH surge and no ovulation, progestin causes thickening of the cervical mucus therefore limiting the passage of the spern to the uterus. progestin also inhibits the endometrial growth and thus the endometrium is less prepared for the implantation of the ova
terbutalineB2 agonist that relaxes the uterus used to decrease the contactions frequency in women during labour
ritodrineB2 agonist that relaxes the uterus used to decrease the contactions frequency in women during labour
testosterone and methyltestosteroneagonist on androgen receptor
finastrideantiandrogen. 5areductase inhibitor decreases the conversion of testosterone to DHT. useful in benign prostatic hyperplasia and male pattern baldness)
flutamideantoandrogen. a nonsteroidal competitive inhibitor at androgen receptor used for prostate carcinoma
ketoconazole inhibit steroid synthesis by inhibition of 17,20 desmolase
spironolactoneinhibits steroid binding, 17 alpha hydroxylase and 17,20 desmolase
tamsulosina1 antagonist used to treat BPH by inhibiting smooth ms contaction selective for a1AD receptors found on prostate vs vascular a1B receptors
sildinafilm vardenafil, tadalafilinhibit PDE-5 leading to increase cGMP smooth ms relaxation in corpus cavernosum and increases the blood flow causing penile erection
minoxidildirect arteriolar vasodilator
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respiratory:

Question Answer
diphenhydramine1st generation. revirsable inhibition of H1 receptor
dimenhydrinate1st generation. revirsable inhibition of H1 receptor
chlorphenarmine1st generation. revirsable inhibition of H1 receptor
loratidine2nd generation of revirsable H1 blockers
fexofenadine2nd generation. revirsable inhibition of H1 receptor
desloratidine2nd generation. revirsable inhibition of H1 receptor
cetirixine2nd generation. revirsable inhibition of H1 receptor
guafensinexpectorant thins the recpiratory secretions but doesnt supress cough
n acetyl cysteinemucolytic. can loosen the mucus plug in CP by disrupting the disulfide bond also used as an antidote for acetamenophin toxicity
dextromethorphanantitussive antagonize NMDA glutamate receptor synthetic codeine analog has mild opiod effects when used in excess naloxone is used in overdose
pseudoephidrine, phenylephrinealpha adrenergic agonist used as nasal decongestant
endothelin receptor antagonistinduce busentan competitively antagonize endothelin 1 receptor decrease pulmonary vascular resistance.
PDE-5 inhibitorsinduce sildenafil inhibit c GMP PDE5and prolong vasodilatory effect of nitric oxide also used to treat eractile dysfunction
prostacyclin analogs, epoprostenol, iloprost, prostacyclin PGI2direct vasodilatory effects on pulmonary and systemic arterial vascular beds and inhibit platelet aggregation
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