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44 Cards in this Set

  • Front
  • Back
Clinical use of dinoprostone?
Dinopristone is approved for use to ripen the cervix before induction of labor with oxytocin.
Dinoprostone is analog of what type of prostaglandin?
PGE2
Route of administration of dinoprostone?
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.
Clinical use of misoprostol?
• 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.
Misoprostol is analog of what type of prostacyclin?
PGE1
Route of administration?
• vaginal
• oral
• sublingual
What type of prostacyclin are given as an infusion to maintain patency of ductus arteriosus?
PGE1
Clinical use of epoprostenol?
Approved for use in severe pulmonary hypertension and to prevent platelet aggregation in dialysis machines.
Epoprostenol is what type of prostacyclin?
PGI2
Clinical use of alprostadil?
Used in the treatment of impotence by injection into the cavernosa.
Alprostadil is what type of prostacyclin?
PGI1
Clinical use of latanoprost, travoprost and bimatoprost?
Extensively for the topical treatment of glaucoma. These agents apparently increase the outflow of aqueous humor, thus reducing intraocular humor.
Latanoprost, travoprost and bimatoprost are derivatives from what prostacyclin?
PGF2 alpha
Zafirlukast and montelukast are inhibitors at what receptor?
LTD4
What is zileuton?
Zileuton is a selective inhibitor of lipooxygenase and some cyclooxygenase inhibitors exert a mild inhibitory effect on leukotriens synthesis.
Serotonin is produced from what?
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.
After release, serotonin is metabolized by what?
MAO (monoamine oxidase)
Where do you find the different serotonin receptors?
5-HT1 brain
5-HT2 brain, peripheral tissue
5-HT3 CNS (vomiting center)
5-HT4 GI tract
Name some serotonin drugs used in headache symptoms and acute migraine!
The “Triptans”!
• sumatriptan
• naratriptan
Administration of sumatriptan?
orally

parenterally
Administration of naratriptan?
orally
Sumatriptan and naratriptan are agonists or antagonists?
agonists
Sumatriptan and naratriptan are agonist at what agonist?
5-HT1D
Tegaserod is an agonist or antagonist?
agonist
Tegaserod is an agonist of what receptor?
5-HT4 in the colon

(Additionally, tegaserod is a 5-HT2B receptor antagonist)
Tegaserod was approved and briefly marketed for use in Irritable Bowel Syndrome (IBS) and chronic constipation, but is no longer used. Why?
Because of cardiovascular toxicity, its use is now restricted.
Route of administration of tegaserod?
orally
SSRI are important anti-depressive drugs that act to increase activity at central serotogenic synapses by inhibiting what structure?
SERT (serotonin reuptake inhibitor)
The “setron” drugs – ondansetron, granisetron, dolasetron and alosetron are agonists or antagonists?
antagonists
The “setron” drugs – ondansetron, granisetron, dolasetron and alosetron act on what receptor?
5-HT3
When do you take ondansetron, granisetron, dolasetron and alosetron?
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! 
Angiotensin II is a potent vasoconstrictor or vasodilator?
vasoconstrictor
Angiotensin II stimulates release of what important hormone?
aldosterone
All the effects of angiotensin II is due to stimulation of what receptor?
AT1 receptor

(AT2 receptor appears to mediate vasodilation via NO and is probably most important during fetal development.)
The AT1 receptor is Gs, Gi or Gq?
Gq
What drugs can you take to antagonize angiotensin II?
• ACE inhibitors (captopril, enalapril)
• ARBs - Angiotensin II receptor blockers (losartan, valsartan)
Route of administration of ACE inhibitors and ARBs?
oral
What is aliskiren?
A newer oral drug inhibiting renin.
Bradykinin is a potent vasodilator or vasoconstrictor?
vasodilator

(it antagonizes the effects of angiotensin II)
Bradykinin is one of several vasodilator kinins produced from kiniogen by what family of enzymes?
kallikreins
Bradykinin act at what receptors?
• B1
• B2
These receptor of bradykinin are Gs, Gi or Gq?
Like AT1 receptor of angiotensin II they are Gq.
Where do you find COX-1?
In many tissues. (non-inflammatory)
Where do you find COX-2?
In inflammatory cells.