kaplan neuro pp notes
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Opioid analgesics (eg morphine)bull have duality of action J em es is bybull activating receptors that d ecreasebull pain transmission and i emesis bybull activati ng receptors in the CTZ
Drugs for nausea and vomiting include
bull bull 5HT3 (a serotonin receptor-see following chapter) antagonists ondansetron
bull (commonly used in cancer chemotherapy) granisetronbull bull DA antagonists prochlorperazine metoclopramide (also
used in cancerbull chemotherapy also prokinetic in GERD)bull bull H1 antagonists diphenhydramine meclizine promethazinebull bull Muscarinic antagonists scopolaminebull bull Cannabinoids dronabinolbull bull NK1 -receptor antagonist aprepitant (NK1 is a receptor to
substance P)
bull SHT1(a-hJbull bull Found in the CNS (usually inhibitory) and smooth muscle (excitatorybull or inhibitory)bull bull Drug buspironebull - Partial agonist at 5HT Ia receptors -7 anxiolytic (generalized anxietybull disorder [GAD] )bull bull Drug sumatriptan and other triptansbull Agonist at 5HT ld receptors in cerebral vessels -7j migraine painbull Side effects of-triptans possible asthenia chest or throat pressurebull or pain
bull 5HT2(a-c)bull bull Found in CNS (excitatory)bull bull In periphery activation -7 vasodilation contraction of gastrointestinalbull bronchial and uterine smooth muscle and platelet aggregationbull bull Drugsbull 5HT3bull - Olanzapine and other atypical antipsychotics antagonist at 5HT labull receptors in CNS -7j symptoms of psychosisbull - Cyproheptadinebull 0 5HT 2 antagonist used in carcinoid other gastrointestinal tumorsbull and postgastrectomy also used for anorexia nervosabull 0 Has marked H1 -blocking action used in seasonal allergiesbull bull Found in area postrema peripheral sensory and enteric nervesbull bull Mechanism of action activation opens ion channels (no secondbull messengers)bull bull Drugs ondansetron and -setronsbull Antagonists -7j emesis in chemotherapy and radiation andbull postoperatively
bull Ergonovinebull bull Mechan ism of action uterinebull smooth muscle contractionbull bull Use given intramuscularly afterbull placenta l d elivery
bull Ergot alkaloidsbull - Ergotaminebull 0 Mechanism of actionbull Ergotamine acts as partial agonists at both a and SHT2 receptorsbull in the vasculature and possibly in the CNSbull Vasoconstrictive actions to decrease pulsation in cerebral vesselsbull may be relevant to acute actions of ergotamine during migrainebull attackbull 0 Uses ergotamine used in acute attacksbull 0 Side effects gastrointestinal distress prolonged vasoconstrictionbull 1048703 ischemia and gangrene abortion near termbull bull In addition to the -triptans and ergotsbull - Analgesics ASA (+- caffeine or butabarbital) other NSAIDs acetaminophenbull (+- caffeine) oral or injectable opioid-analgesics andbull butorphanol (spray)bull - Prophylaxis propranolol verapamil amitriptyline valproic acid
bull Bridge to Physiologybull Prostaglandins (PGs) are cytoprotectivebull in the stomach dilate renal vasculaturebull contract the uterus and maintain thebull ductus arteriosus Thrombaxane (TxA2)bull causes platelet aggregation GI PGsbull and platelets TxA2s are synthesizedbull by COX 1 (constitutive) COX 2bull (inducible) synthesizes PGs involvedbull in inflammation fever and pain Bothbull enzymes synthesize renal PGs -7 i RBFbull 1048703 M
- Slide 1
- Slide 2
- Slide 3
- Drugs for nausea and vomiting include
- Slide 5
- Slide 6
- Slide 7
- Slide 8
- Slide 9
- Slide 10
- Slide 11
- Slide 12
- Slide 13
- Slide 14
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Drugs for nausea and vomiting include
bull bull 5HT3 (a serotonin receptor-see following chapter) antagonists ondansetron
bull (commonly used in cancer chemotherapy) granisetronbull bull DA antagonists prochlorperazine metoclopramide (also
used in cancerbull chemotherapy also prokinetic in GERD)bull bull H1 antagonists diphenhydramine meclizine promethazinebull bull Muscarinic antagonists scopolaminebull bull Cannabinoids dronabinolbull bull NK1 -receptor antagonist aprepitant (NK1 is a receptor to
substance P)
bull SHT1(a-hJbull bull Found in the CNS (usually inhibitory) and smooth muscle (excitatorybull or inhibitory)bull bull Drug buspironebull - Partial agonist at 5HT Ia receptors -7 anxiolytic (generalized anxietybull disorder [GAD] )bull bull Drug sumatriptan and other triptansbull Agonist at 5HT ld receptors in cerebral vessels -7j migraine painbull Side effects of-triptans possible asthenia chest or throat pressurebull or pain
bull 5HT2(a-c)bull bull Found in CNS (excitatory)bull bull In periphery activation -7 vasodilation contraction of gastrointestinalbull bronchial and uterine smooth muscle and platelet aggregationbull bull Drugsbull 5HT3bull - Olanzapine and other atypical antipsychotics antagonist at 5HT labull receptors in CNS -7j symptoms of psychosisbull - Cyproheptadinebull 0 5HT 2 antagonist used in carcinoid other gastrointestinal tumorsbull and postgastrectomy also used for anorexia nervosabull 0 Has marked H1 -blocking action used in seasonal allergiesbull bull Found in area postrema peripheral sensory and enteric nervesbull bull Mechanism of action activation opens ion channels (no secondbull messengers)bull bull Drugs ondansetron and -setronsbull Antagonists -7j emesis in chemotherapy and radiation andbull postoperatively
bull Ergonovinebull bull Mechan ism of action uterinebull smooth muscle contractionbull bull Use given intramuscularly afterbull placenta l d elivery
bull Ergot alkaloidsbull - Ergotaminebull 0 Mechanism of actionbull Ergotamine acts as partial agonists at both a and SHT2 receptorsbull in the vasculature and possibly in the CNSbull Vasoconstrictive actions to decrease pulsation in cerebral vesselsbull may be relevant to acute actions of ergotamine during migrainebull attackbull 0 Uses ergotamine used in acute attacksbull 0 Side effects gastrointestinal distress prolonged vasoconstrictionbull 1048703 ischemia and gangrene abortion near termbull bull In addition to the -triptans and ergotsbull - Analgesics ASA (+- caffeine or butabarbital) other NSAIDs acetaminophenbull (+- caffeine) oral or injectable opioid-analgesics andbull butorphanol (spray)bull - Prophylaxis propranolol verapamil amitriptyline valproic acid
bull Bridge to Physiologybull Prostaglandins (PGs) are cytoprotectivebull in the stomach dilate renal vasculaturebull contract the uterus and maintain thebull ductus arteriosus Thrombaxane (TxA2)bull causes platelet aggregation GI PGsbull and platelets TxA2s are synthesizedbull by COX 1 (constitutive) COX 2bull (inducible) synthesizes PGs involvedbull in inflammation fever and pain Bothbull enzymes synthesize renal PGs -7 i RBFbull 1048703 M
- Slide 1
- Slide 2
- Slide 3
- Drugs for nausea and vomiting include
- Slide 5
- Slide 6
- Slide 7
- Slide 8
- Slide 9
- Slide 10
- Slide 11
- Slide 12
- Slide 13
- Slide 14
-
bull SHT1(a-hJbull bull Found in the CNS (usually inhibitory) and smooth muscle (excitatorybull or inhibitory)bull bull Drug buspironebull - Partial agonist at 5HT Ia receptors -7 anxiolytic (generalized anxietybull disorder [GAD] )bull bull Drug sumatriptan and other triptansbull Agonist at 5HT ld receptors in cerebral vessels -7j migraine painbull Side effects of-triptans possible asthenia chest or throat pressurebull or pain
bull 5HT2(a-c)bull bull Found in CNS (excitatory)bull bull In periphery activation -7 vasodilation contraction of gastrointestinalbull bronchial and uterine smooth muscle and platelet aggregationbull bull Drugsbull 5HT3bull - Olanzapine and other atypical antipsychotics antagonist at 5HT labull receptors in CNS -7j symptoms of psychosisbull - Cyproheptadinebull 0 5HT 2 antagonist used in carcinoid other gastrointestinal tumorsbull and postgastrectomy also used for anorexia nervosabull 0 Has marked H1 -blocking action used in seasonal allergiesbull bull Found in area postrema peripheral sensory and enteric nervesbull bull Mechanism of action activation opens ion channels (no secondbull messengers)bull bull Drugs ondansetron and -setronsbull Antagonists -7j emesis in chemotherapy and radiation andbull postoperatively
bull Ergonovinebull bull Mechan ism of action uterinebull smooth muscle contractionbull bull Use given intramuscularly afterbull placenta l d elivery
bull Ergot alkaloidsbull - Ergotaminebull 0 Mechanism of actionbull Ergotamine acts as partial agonists at both a and SHT2 receptorsbull in the vasculature and possibly in the CNSbull Vasoconstrictive actions to decrease pulsation in cerebral vesselsbull may be relevant to acute actions of ergotamine during migrainebull attackbull 0 Uses ergotamine used in acute attacksbull 0 Side effects gastrointestinal distress prolonged vasoconstrictionbull 1048703 ischemia and gangrene abortion near termbull bull In addition to the -triptans and ergotsbull - Analgesics ASA (+- caffeine or butabarbital) other NSAIDs acetaminophenbull (+- caffeine) oral or injectable opioid-analgesics andbull butorphanol (spray)bull - Prophylaxis propranolol verapamil amitriptyline valproic acid
bull Bridge to Physiologybull Prostaglandins (PGs) are cytoprotectivebull in the stomach dilate renal vasculaturebull contract the uterus and maintain thebull ductus arteriosus Thrombaxane (TxA2)bull causes platelet aggregation GI PGsbull and platelets TxA2s are synthesizedbull by COX 1 (constitutive) COX 2bull (inducible) synthesizes PGs involvedbull in inflammation fever and pain Bothbull enzymes synthesize renal PGs -7 i RBFbull 1048703 M
- Slide 1
- Slide 2
- Slide 3
- Drugs for nausea and vomiting include
- Slide 5
- Slide 6
- Slide 7
- Slide 8
- Slide 9
- Slide 10
- Slide 11
- Slide 12
- Slide 13
- Slide 14
-
bull 5HT2(a-c)bull bull Found in CNS (excitatory)bull bull In periphery activation -7 vasodilation contraction of gastrointestinalbull bronchial and uterine smooth muscle and platelet aggregationbull bull Drugsbull 5HT3bull - Olanzapine and other atypical antipsychotics antagonist at 5HT labull receptors in CNS -7j symptoms of psychosisbull - Cyproheptadinebull 0 5HT 2 antagonist used in carcinoid other gastrointestinal tumorsbull and postgastrectomy also used for anorexia nervosabull 0 Has marked H1 -blocking action used in seasonal allergiesbull bull Found in area postrema peripheral sensory and enteric nervesbull bull Mechanism of action activation opens ion channels (no secondbull messengers)bull bull Drugs ondansetron and -setronsbull Antagonists -7j emesis in chemotherapy and radiation andbull postoperatively
bull Ergonovinebull bull Mechan ism of action uterinebull smooth muscle contractionbull bull Use given intramuscularly afterbull placenta l d elivery
bull Ergot alkaloidsbull - Ergotaminebull 0 Mechanism of actionbull Ergotamine acts as partial agonists at both a and SHT2 receptorsbull in the vasculature and possibly in the CNSbull Vasoconstrictive actions to decrease pulsation in cerebral vesselsbull may be relevant to acute actions of ergotamine during migrainebull attackbull 0 Uses ergotamine used in acute attacksbull 0 Side effects gastrointestinal distress prolonged vasoconstrictionbull 1048703 ischemia and gangrene abortion near termbull bull In addition to the -triptans and ergotsbull - Analgesics ASA (+- caffeine or butabarbital) other NSAIDs acetaminophenbull (+- caffeine) oral or injectable opioid-analgesics andbull butorphanol (spray)bull - Prophylaxis propranolol verapamil amitriptyline valproic acid
bull Bridge to Physiologybull Prostaglandins (PGs) are cytoprotectivebull in the stomach dilate renal vasculaturebull contract the uterus and maintain thebull ductus arteriosus Thrombaxane (TxA2)bull causes platelet aggregation GI PGsbull and platelets TxA2s are synthesizedbull by COX 1 (constitutive) COX 2bull (inducible) synthesizes PGs involvedbull in inflammation fever and pain Bothbull enzymes synthesize renal PGs -7 i RBFbull 1048703 M
- Slide 1
- Slide 2
- Slide 3
- Drugs for nausea and vomiting include
- Slide 5
- Slide 6
- Slide 7
- Slide 8
- Slide 9
- Slide 10
- Slide 11
- Slide 12
- Slide 13
- Slide 14
-
bull Ergonovinebull bull Mechan ism of action uterinebull smooth muscle contractionbull bull Use given intramuscularly afterbull placenta l d elivery
bull Ergot alkaloidsbull - Ergotaminebull 0 Mechanism of actionbull Ergotamine acts as partial agonists at both a and SHT2 receptorsbull in the vasculature and possibly in the CNSbull Vasoconstrictive actions to decrease pulsation in cerebral vesselsbull may be relevant to acute actions of ergotamine during migrainebull attackbull 0 Uses ergotamine used in acute attacksbull 0 Side effects gastrointestinal distress prolonged vasoconstrictionbull 1048703 ischemia and gangrene abortion near termbull bull In addition to the -triptans and ergotsbull - Analgesics ASA (+- caffeine or butabarbital) other NSAIDs acetaminophenbull (+- caffeine) oral or injectable opioid-analgesics andbull butorphanol (spray)bull - Prophylaxis propranolol verapamil amitriptyline valproic acid
bull Bridge to Physiologybull Prostaglandins (PGs) are cytoprotectivebull in the stomach dilate renal vasculaturebull contract the uterus and maintain thebull ductus arteriosus Thrombaxane (TxA2)bull causes platelet aggregation GI PGsbull and platelets TxA2s are synthesizedbull by COX 1 (constitutive) COX 2bull (inducible) synthesizes PGs involvedbull in inflammation fever and pain Bothbull enzymes synthesize renal PGs -7 i RBFbull 1048703 M
- Slide 1
- Slide 2
- Slide 3
- Drugs for nausea and vomiting include
- Slide 5
- Slide 6
- Slide 7
- Slide 8
- Slide 9
- Slide 10
- Slide 11
- Slide 12
- Slide 13
- Slide 14
-
bull Ergot alkaloidsbull - Ergotaminebull 0 Mechanism of actionbull Ergotamine acts as partial agonists at both a and SHT2 receptorsbull in the vasculature and possibly in the CNSbull Vasoconstrictive actions to decrease pulsation in cerebral vesselsbull may be relevant to acute actions of ergotamine during migrainebull attackbull 0 Uses ergotamine used in acute attacksbull 0 Side effects gastrointestinal distress prolonged vasoconstrictionbull 1048703 ischemia and gangrene abortion near termbull bull In addition to the -triptans and ergotsbull - Analgesics ASA (+- caffeine or butabarbital) other NSAIDs acetaminophenbull (+- caffeine) oral or injectable opioid-analgesics andbull butorphanol (spray)bull - Prophylaxis propranolol verapamil amitriptyline valproic acid
bull Bridge to Physiologybull Prostaglandins (PGs) are cytoprotectivebull in the stomach dilate renal vasculaturebull contract the uterus and maintain thebull ductus arteriosus Thrombaxane (TxA2)bull causes platelet aggregation GI PGsbull and platelets TxA2s are synthesizedbull by COX 1 (constitutive) COX 2bull (inducible) synthesizes PGs involvedbull in inflammation fever and pain Bothbull enzymes synthesize renal PGs -7 i RBFbull 1048703 M
- Slide 1
- Slide 2
- Slide 3
- Drugs for nausea and vomiting include
- Slide 5
- Slide 6
- Slide 7
- Slide 8
- Slide 9
- Slide 10
- Slide 11
- Slide 12
- Slide 13
- Slide 14
-
bull Bridge to Physiologybull Prostaglandins (PGs) are cytoprotectivebull in the stomach dilate renal vasculaturebull contract the uterus and maintain thebull ductus arteriosus Thrombaxane (TxA2)bull causes platelet aggregation GI PGsbull and platelets TxA2s are synthesizedbull by COX 1 (constitutive) COX 2bull (inducible) synthesizes PGs involvedbull in inflammation fever and pain Bothbull enzymes synthesize renal PGs -7 i RBFbull 1048703 M
- Slide 1
- Slide 2
- Slide 3
- Drugs for nausea and vomiting include
- Slide 5
- Slide 6
- Slide 7
- Slide 8
- Slide 9
- Slide 10
- Slide 11
- Slide 12
- Slide 13
- Slide 14
-
- Slide 1
- Slide 2
- Slide 3
- Drugs for nausea and vomiting include
- Slide 5
- Slide 6
- Slide 7
- Slide 8
- Slide 9
- Slide 10
- Slide 11
- Slide 12
- Slide 13
- Slide 14
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