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45 Cards in this Set
- Front
- Back
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Histamine
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immed allergic & inflam rxn
Gastirc acid secretion modest anaphylaxis |
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histamine - 2
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most in mast cells
ECL of stomach w/ IgE release - CA+2 dept (type 1) inhib some B and T cell functions |
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histamine - 3
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H1-H4
GPCR |
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H1
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smooth m, endothelium, Brain (postsynaptic)
Ip3 system |
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h2
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gastic mucosa, cardiac m, mast cells, brain
Brain (postsyn) cAMP production (some ip3) |
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h3
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presyn brain, myenteric plex
inhib camp Decrease of Histamine |
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h4
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Bone marrow
chemotatic effects on eosionphils |
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histamine use
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test for brncohial hyperreativity
Dont Give to ASTHMA, ucler disease, GI bleedin |
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histamine antagonists
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Epi + adernergic drugs
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histamine release inhibitors
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cromolyn, nedocromil, theophylline (asthma)
B2- agnonist glucocorticoids |
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h1 - first generation
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STRONG sedative (kids may get excited!)
block autonomic receptors effective 4-6 hrs (cept meclizine) reversilbe comp inhib (some inverse agonists) go in CNS readily active metabolites - degrade by liver |
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h1- second generation
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much less sedating
less complete distrib in CNS some inhib release from mast/basophils |
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h1-first gen
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Cyproheptadine
Diphenhydramine* Meclizine Promethazine |
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h1-sec gen
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Cetirizine*
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h1 actions
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STRONG INHIB EDEMA & ITCHING
STRONG ANTINAUSEA |
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h1 actions 2
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antipark (due to anti-musc actions)
Diphenhdramine Supress antipsych drugs sideeffects urinary rent/blurred vision (atroppine like) a-recp blocker cyproheptadine (block serotonine) potent anestheics (1st gen) |
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h1 uses
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rhiitis (hay fever) & urticaria (B4 exposure)
limited effective angioedema & anaphalx 1st gen - MOTION SICKNESS PREVENTION!! (Diphen & Promethazine) |
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h1 tox (not second gen)
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sleepy, restleness, insomina, tremors, halluc, seizures
GI - dry mouth/const CVS - hypotension bluured vision/urinary rention increased appetite - cyproheptadine |
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contraindications h1
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preg, children, heptaic disease, tacharrythmias
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h2
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hard to get into CNS, but in all organs
CIMETIDINE Ranitidine, Famotidine |
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h2 actions
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comp inhibitors of parietal cells (gastic a & pepsin)
Stops NOCURTAL inhib camp |
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h2 - cimetidine
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inhibit cp450
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h2 USES
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GERD, heartburn (USE B4 MEALS)
PEP ulcers (do not treat caused by NSAIDS and H. pylori) Esophagitis |
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h2 tox
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headache, confusion
elevated liver enz IMPOTENCE cp450 (clearance of other drugs) |
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h2 contraindications
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renal impairment/disease
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SEROTONIN
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released from blood clots - induce vasoconstion
90% in EEC cells after syn - rapidly stored/inactivated (MAO) mediator in migrane headaches stored in platelets of blood mood,sleep, BP, vomit, pain percp |
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Serotonin Agonists
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Buspirone - anxiety
Ergonovine - postpart bleed Ergotamine - migranes LSD - hallucinagin Metoclopramide - GI disorders |
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Serotonin Ag - 1B/1D
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Eletriptan
Naratriptan Sumatriptan* - nasal Zolmitriptan - nasal |
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Serotonin Antag
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Butyrophenones
Cyproheptadine Ketanserin Ondasetron Phenothiazines Phenoxybenzamine Ritanserin |
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Serotonin Ag - 1B/1D
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cerebrl/meng vessels (vasoconstriction)
neurons - presyn inhib receptors SEVERE ACUTE MIGRANES Sumatriptan - cluster headaches |
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serotonin tox
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ting, warmth, dizzy, neck pain, myo infarcts
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serotonin contraindic
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Cereb vasc disease, perip vasc diease, heart disease
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serotonin Antag
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Butyrophenones - nonselc schzio
Cyproheptadine - sedation Ketanserin - plate aggrg Ondasetron - nasuea chemo Phenothiazines - nonselc schzio Phenoxybenzamine - inhib 5ht2 Ritanserin - bleeding time & TXH formation |
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Ergot Alkalods
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spon abortions, hallucinations, vasospasm = gangrene
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Ergot Use
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Migrane pain (first sign of attack)
post part bleeding hyperprolactiema |
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ergot tox
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TI is narrow
prolonged vasospam drowsy hallucinations |
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Eicosanoids
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lipid-derieved
Prostanoids (PG and TA (TXA2) Leukotines (LT) |
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To use AA for Eicoansoids
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must be relased by Phosopholipase A2 (epi, angioten II bradykinin promote
glucocorticods inhib |
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COX
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Cox 1 - PG all cels - houskeepin
cox 2 - PGH inducible (inflam, fever, cancer) inhib by NSAIDS AA - PGG2 - PGH2 |
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LOX
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AA metabolized by 5, 12, 15 lipgen
= Hpete - HETE & LT LTC4 & LTD4 (broncoconstrictors) |
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Eico
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Short 1/2 life
GPCR misoprotsol - 30-60 mins others 2-5 mins |
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eico clincial
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inhib syn (cox-2 target)
change diet to change fatty A precursors |
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Prostagladins
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Alprostadil PGE1 DA patency (erectile dysf)
Carboprost Tromethamine- PGF2a - 2nd tri abortion, postpart hemmo - Dinoprostone - PGE2 mole, abortion, labor induction Epoprostenol - PGI2 - pulm hyperten, lung/heart transplants Latanoprost - PGF2a - glaucoma, brown pigments Misoprostol - PGE1 - abortions, NSAIDS ulcers, (tox = sepsis vag) |
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Lipid Autacoid Inhibitors
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Glucocorticoids - all known pathways
Cromolyn - eicosaniod release Montelukast & Zafirlukast - LT recp NSAIDs Zileuton - LOX |
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LA inhibtor - uses
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Asthma
Bartters syndome - decresed sent to angioten (nml to Low - BP) cell-med organ rejections!! delayed closure of DA (PGE2) painful menstraution (PGE2, PGF2a) inflamation - arthritis thrombosis - asprin - irrvs binding |
