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USMLE - Pharm
Kaplan Section 6 - Inflammatory Drugs - Anti-5HTs, Anti-Prostaglandins
| Question | Answer |
|---|---|
| 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:
christinapham
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