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44 Cards in this Set
- Front
- Back
Clinical use of dinoprostone?
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Dinopristone is approved for use to ripen the cervix before induction of labor with oxytocin.
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Dinoprostone is analog of what type of prostaglandin?
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PGE2
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Route of administration of dinoprostone?
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A suppository containing 20 mg of dinoprostone should be inserted high into the vagina. The patient should remain in the supine position for ten minutes following insertion.
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Clinical use of misoprostol?
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• Misopristol has been used extensively with the progesterone mifepristone as an extremely effective and saft abortificient combination in Europe.
• Misoprostol is approved in the US for the prevention of peptic ulcers in patients who must take high doses of NSAIDS for arthritis and who have a history of ulcer associated with this use. |
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Misoprostol is analog of what type of prostacyclin?
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PGE1
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Route of administration?
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• vaginal
• oral • sublingual |
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What type of prostacyclin are given as an infusion to maintain patency of ductus arteriosus?
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PGE1
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Clinical use of epoprostenol?
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Approved for use in severe pulmonary hypertension and to prevent platelet aggregation in dialysis machines.
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Epoprostenol is what type of prostacyclin?
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PGI2
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Clinical use of alprostadil?
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Used in the treatment of impotence by injection into the cavernosa.
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Alprostadil is what type of prostacyclin?
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PGI1
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Clinical use of latanoprost, travoprost and bimatoprost?
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Extensively for the topical treatment of glaucoma. These agents apparently increase the outflow of aqueous humor, thus reducing intraocular humor.
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Latanoprost, travoprost and bimatoprost are derivatives from what prostacyclin?
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PGF2 alpha
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Zafirlukast and montelukast are inhibitors at what receptor?
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LTD4
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What is zileuton?
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Zileuton is a selective inhibitor of lipooxygenase and some cyclooxygenase inhibitors exert a mild inhibitory effect on leukotriens synthesis.
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Serotonin is produced from what?
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tryptophan and stored in vesicles of the enterochromaffin cells of the gut and neurons in the CNS and ENS. Serotonin is also stored in platelets.
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After release, serotonin is metabolized by what?
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MAO (monoamine oxidase)
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Where do you find the different serotonin receptors?
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5-HT1 brain
5-HT2 brain, peripheral tissue 5-HT3 CNS (vomiting center) 5-HT4 GI tract |
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Name some serotonin drugs used in headache symptoms and acute migraine!
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The “Triptans”!
• sumatriptan • naratriptan |
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Administration of sumatriptan?
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orally
parenterally |
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Administration of naratriptan?
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orally
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Sumatriptan and naratriptan are agonists or antagonists?
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agonists
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Sumatriptan and naratriptan are agonist at what agonist?
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5-HT1D
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Tegaserod is an agonist or antagonist?
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agonist
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Tegaserod is an agonist of what receptor?
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5-HT4 in the colon
(Additionally, tegaserod is a 5-HT2B receptor antagonist) |
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Tegaserod was approved and briefly marketed for use in Irritable Bowel Syndrome (IBS) and chronic constipation, but is no longer used. Why?
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Because of cardiovascular toxicity, its use is now restricted.
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Route of administration of tegaserod?
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orally
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SSRI are important anti-depressive drugs that act to increase activity at central serotogenic synapses by inhibiting what structure?
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SERT (serotonin reuptake inhibitor)
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The “setron” drugs – ondansetron, granisetron, dolasetron and alosetron are agonists or antagonists?
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antagonists
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The “setron” drugs – ondansetron, granisetron, dolasetron and alosetron act on what receptor?
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5-HT3
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When do you take ondansetron, granisetron, dolasetron and alosetron?
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They are anti-emetic and have important actions in the vomiting center (area postrema) of the medulla oblongata so take them before chemotherapy or… after a really awesome party!
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Angiotensin II is a potent vasoconstrictor or vasodilator?
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vasoconstrictor
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Angiotensin II stimulates release of what important hormone?
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aldosterone
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All the effects of angiotensin II is due to stimulation of what receptor?
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AT1 receptor
(AT2 receptor appears to mediate vasodilation via NO and is probably most important during fetal development.) |
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The AT1 receptor is Gs, Gi or Gq?
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Gq
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What drugs can you take to antagonize angiotensin II?
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• ACE inhibitors (captopril, enalapril)
• ARBs - Angiotensin II receptor blockers (losartan, valsartan) |
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Route of administration of ACE inhibitors and ARBs?
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oral
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What is aliskiren?
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A newer oral drug inhibiting renin.
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Bradykinin is a potent vasodilator or vasoconstrictor?
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vasodilator
(it antagonizes the effects of angiotensin II) |
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Bradykinin is one of several vasodilator kinins produced from kiniogen by what family of enzymes?
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kallikreins
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Bradykinin act at what receptors?
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• B1
• B2 |
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These receptor of bradykinin are Gs, Gi or Gq?
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Like AT1 receptor of angiotensin II they are Gq.
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Where do you find COX-1?
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In many tissues. (non-inflammatory)
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Where do you find COX-2?
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In inflammatory cells.
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