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USMLE - Pharm

Kaplan Section 6 - Inflammatory Drugs - Anti-5HTs, Anti-Prostaglandins

QuestionAnswer
Ondansetron Anti-emetic. 5HT3 antagonist. Commonly used in cancer therapy.
Granisetron Anti-emetic. 5HT3 antagonist.
Prochlorperazine Anti-emetic. DA antagonist.
Metoclopramide Anti-emetic. DA antagonist. Commonly used in cancer therapy.
Diphenhydramine Anti-emetic. H1 antagonist.
Meclizine Anti-emetic. H1 antagonist.
Promethazine Anti-emetic. H1 antagonist.
Scopolamine M antagonist
Dronabinol Cannabinoid
Aprepitant NK1 receptor antagonist. NK1 - receptor to substance P
Where is serotonin made and stored? In GI cells, neurons, and in platelets
How is serotonin metabolized? by MAO type A
T or F: all 5HT receptor subtypes are G-protein-coupled No. 5HT3 is coupled directly to an ion channel. The rest are G-protein-coupled.
Which serotonin receptors are found in the CNS? 5HT 1 (inhibitory) and 5HT 2 (excitatory) and 5HT3 (area postrema)
What receptor does Buspirone affect? 5HT1a
What is Buspirone used for? GAD - generalized anxiety disorder
What receptor does Sumatriptan affect? "triptan" is migraine drug (vasoconstriction of cerebral vessels --> dec pulsation --> decreases pain). 5HT1d
What is a unique adverse effect of Sumatriptan? asthenia (feeling of weakness without loss of strength); chest/throat pressure or pain
How does activation of 5HT2 in the periphery affect smooth muscle? 1. vasodilation, 2. contraction of smooth muscle in the following: GI, bronchi, uterus
What type of 5HT receptor is associated with platelet aggregation? 5HT2
Olanzapine 5HT2A antagonist in CNS, dec sx's of psychosis
Cyproheptadine 5HT2 antagonist in CNS, used for GI tumor and anorexia nervosa
What is special about the activity of cyproheptadine? 5HT2 antagonist as well as H1 antagonist
Odansetron 5HT3 antagonist in CTZ as well as in GI tract --> dec emesis in chemo and radiation
Where do you find 5HT4? GI smooth muscle and myenteric nerves
Tegaserod 5HT4 agonist, give to IBD pts if they're experiencing constipation as well
Ergonovine causes uterine sm muscle contraction --> given after placental delivery
Ergotamine a and 5HT2 agonist; vasoconstriction --> dec pulsation in cerebral vessels--> dec pain in migraine attacks; used in acute attacks
Methysergide a and 5HT2 agonist; vasoconstriction --> dec pulsation in cerebral vessels--> dec pain in migraine attacks; used prophylactically for migraines
Adverse effects of Ergotamine 1. GI distress, 2. prolonged vasoconstriction --> ischemia and gangrene 3. abortion near term
Adverse effects of Methysergide 1. GI distress, 2. prolonged vasoconstriction --> ischemia and gangrene 3. abortion near term 4. fibroplasia (abnormal increase of fibrous tissue)
Name the drugs that can be used for migraines 1. "triptans" (like sumatriptan), 2. ergots (like ergonovine and ergotamine), 3. analgesics (ASA, NSAIDs, acetaminophen, opioid analgesics, butorphanol (opioid analgesic, nasal spray)
Name the prophylactic drugs for migraines 1. Bblockers, 2. CCB's, 3. carbamazepine (anticonvulsant, block fast Na channels), 4. NSAIDs, 5. gabapentin (block voltage gated Ca channels), 6. methysergide, 7. valproic acid, 8. TCA's
Why do NSAIDs induce ulcers? NSAIDs block cyclooxygenase --> PGE1 not made (PGE1 has protective action on gastric mucosa) --> ulcers
How do you treat NSAID-induced ulcers? Use misoprostol (analog of PGE1)
What drug can maintain the patency of the ductus arteriosus? What is the mechanism? Alprostadil is analog of PGE1. Causes vasodilation --> Relaxes the ductus arteriosus in early postnatal life and supports its patency when continuously infused i.v. in neonates with congenital heart defects who depend on a patent ductus for survival.
What is ductus arteriosus? connection between the pulmonary artery and the aortic arch that allows most of the blood from the right ventricle to bypass the fetus' fluid-filled compressed lungs
What drug can you use in male impotence? Alprostadil is analog of PGE1. Causes vasodilation --> treats male impotence.
Alprostadil is analog of PGE1. Causes vasodilation --> treats male impotence. no. Can only use as abortifacient!
What is PGE2 used for? uterine smooth muscle contraction.
What drugs can be used for cervical ripening? misoprostol (PGE1 analog) or dinoprostone (PGE2)
What drugs can be used as abortifacient? (in conjunction with mifepristone, RU486) misoprostol (PGE1 analog) or dinoprostone (PGE2)
How is RU486 an abortifacient? antagonizes the endometrial and myometrial effects of progesterone. leads to trophoblast detachment, resulting in decreased production of hCG, which in turn causes decreased production of progesterone by the corpus luteum
Why should RU486 be followed by a prostaglandin? anti-progesterone to cause trophoblast detachment, then need uterine smooth muscle contraction to expel
Dinoprost PGF2alpha - uterine and bronchiolar smooth muscle contraction. Abortifacient with RU486.
Carboprost PGF2alpha - uterine and bronchiolar smooth muscle contraction. Abortifacient with RU486.
What happens to PGE2 and PGF2a in primary dysmenorrhea? both increase. NSAIDs help --> may be due to NSAID inhibition of prostaglandin synthesis.
Lantanoprost decreases intraocular pressure --> used in treatment of glaucoma
Epoprostenol PGI2 (prostacyclin): platelet stabilizer and vasodilator --> used in primary pulm HTN
How do thromboxanes (TXA2) affect platelets Causes platelet aggregation
What do thromboxanes do to smooth muscle? Vasoconstriction and bronchoconstriction
How do prostacyclins (PGI2) affect platelets? Causes platelet stabilization (inhibits aggregation)
Created by: Missy Kratz Missy Kratz on 2008-03-20



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