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85 Cards in this Set
- Front
- Back
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Eicosanoids
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Made from arachidonic acid
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Products of cyclooxygenase pathway?
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Prostaglandins, prostacyclin, thromboxane
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Produces of lipoxygenase pathway?
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Lipoxins, leukotrienes
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Products of cytochrome P450 epoxygenase
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Epoxyeicosatetraenoic acids (EETS)
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What drug inhibits phospholipase A2?
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corticosteroid
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Ankylosing spondylitis, RA, osteoarthritis
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Corticosteroids indirectly inhibit phospholipase A2
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What are the pro-inflammatory eicosanoids
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Prostacyclins + thromboxanes
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What are the non-inflammatory eicosanoids
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Lipoxins + protacyclins
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What are examples of NSAIDS?
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Aspirin, indomethacin, ibuprofen, sulindac, naproxen, celecoxib
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What are examples of corticosteroids?
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Prednisone, examethasone, triamcinolone
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What are examples of inhibitors of leukotrienes
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Zafirlukast, montelukase, zileuton
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What is the MOA of corticosteroids
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Induce synthesis of lipocortin -> cause inhibiton of phospholipase A2 -> shuts down everything
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What are examples of inhibitors of thromboxanes
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Dozoxiben, pirmagrel, ridogrel
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What are the clinical uses of corticosteroids?
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Asthma, arthritis, SLE -> leads to ↓ bone density (Osteoperosis)
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Side effect of corticosteroids
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Hyperglycemia-> insulin resistance -> hyperthyroidism(inhibits kidneys from reabsorbing calcium, inhibits vitamin D), ulcers, osteoperosis
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H1 receptor
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IgE -> Gq coupled receptor in smooth muscle -> IP3 + DAG -> ↑ Ca2+ -> pain, itching in the skin, bronchoconstriction, and vasodilation (NO) -> opening gaps in permeability barrier -> edema
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H2 receptor
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Gs-coupled receptor -> ↑ cAMP -> ↑ gastric acid secretion by parietal cells in the stomach -> cardiac stimulant effect -> ↓ histamine relase from mast cells (negative feed back)
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What are the 4 ways to release histamine?
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1. Immunologic (IgE -> type I hypersensitivity), 2. mechanical (Na+ causes release of histamine from granules when mast cells are injured), 3. vancomycin (red man syndrome), 4. venom (immune reaction)
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What is the function of endogenous histamines
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1. Immune system, 2. CNS, 3. gastric acid secretion, 4. neurotransmitters
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Alkylamines
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2nd gen anti-histamines - Acrivastine
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Piperidines
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2nd gen anti-histamines -Loratadine, desloratadine, levocabastine, ebastine, mizolastine, fexofenadine
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Phthalazinones
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2nd gen anti-histamines -Azelastine
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Piperazines
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2nd gen anti-histamines -cetirizine
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Pt w/ allergic rhinitis and allergic urticaria
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Certirizine, acrivastin, loratadine, fexofenadine - 2nd Gen H1 anti-histamines; side effect = somnolence, dry mouth, headache, fatigue
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What is the MOA of 2nd generation anti-histamines
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Selective for the blood -> dosent enter the CNS as much -> less drowsiness
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What is the MOA of H2 antagonist?
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H2 antagonist -> reduce gastric acid secretion
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What drugs are the H2 blockers?
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Cimetidine, ranintidine, fomotidine, nisatidine
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What are the side effects of the H2 blockers
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Diarrhea, headache, fatigue, and constipation
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Pt has acid-peptic disease, especially duodenal ulcer. What anti-histamine drugs was given to treat this?
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H2 blockers - cimetidine, ranitidine, fomotidine, nisatidine
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5-HT1A,B,D, receptor
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Brain -> mediate synaptic inhibition via ↑ K+ conductance -> Gi -> ↓ cAMP -> sedation
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5-HT4
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Gastrointestinal tract -> plays a role in intestinal motility -> Go do do
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5-HT3
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CNS (chemoreceptive vomiting area, peripheral sensory and enteric nerves). Antagonists here = anti-emetics
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Buspirone
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5HT1A -> anxiolytic agent (relieves antiety w/o sedative, hypnotic, and euphoric effects!!!) -> no driving impairment; Side effects = tachycardia, palpitation, nervousness, GI distress and parasthesia
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Sumatriptan
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5HT1D/1B -> first line treatment in acute migraine + cluster headaches; Contraindication = coronary artery diesase-> may cause coronary artery spasm
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Naratriptan and eletriptan
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Contraindication = hepatic and renal insufficiency
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Cisapride
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5HT4 -> treats irritable bowel syndrome + constipation -> makes u go toilet
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Ondansetron
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5-HT3 receptor blockers and have important antiemetic actions in the area postrema of the medulla and also on peripheral sensory and enteric nerves -> GOOD to prevent N/V in chemotherapy
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Ethanolamines
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1st generation anti-histamines - diphenhydramine, carbinoxamine, celemastine, dimenhydrinate
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Phenothiazine
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1st generation anti-histamines - Promethiazine
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Piperazines
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1st generation anti-histamines - Hydroxyzine, cyclizine, and meclizine
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Piperidines
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1st generation anti-histamines - Cyprohetadine, phenindamine
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Alkylamine
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1st generation anti-histamines - Chlorpheniramine, brompheniramine
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Ethelenediamine
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1st generation anti-histamines - Pyrilamine, tripelennamine
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What H1 blockers are used to treat motion sickness?
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1. Diphenhydramine, dimenhydrinate, 3. cyclizine, 4. meclizine, 5. promethazine
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What H1 blocker is used to treat cheomotherapy induced vomiting?
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Diphenhydramine
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Side effect of diphenhydramine and promethazine
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Sedation
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Side effect of promethazine
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Orthostatic hypertension - causes alpha-adrenoceptor blockade -> ↓ BP
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What is the MOA of 1st gen anti-histamines?
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Inverse agonsits -> enters both blood and CNS; side effect = enters CNS and causes sedation
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What is the clinical application of thromboxanes antagonists
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Blood thinning (similar to aspirin) - but unlike aspirin its reversible
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What are the adverse effects of dazoxiben, pirmagrel, ridogrel
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Bleeding (anti-thromboxane)
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What is the MOA of NSAIDS
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Permeates into synovial joints -> inhibits platelets/suppresses inflamamtion -> analgesic + anti-pyretic
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What is the side effects of NSAIDS
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Diclofenac + sulindac - Gastric irritation, nephrotoxicity, hepatotoxicity
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Which NSAIDS are COX1> COX2
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Indomethacin, sulindac
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Which NSAIDS are COX1=COX2
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Meclofenamate, ibuprofen
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Which NSAIDS are COX1< COX2
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Celecoib, rofecoxib
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What are the propinoic acid drugs?
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Ibuprofen, naproxen, ketoprofen, flurprofen
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Indomethacin
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Inhibits prostacyclin (PGI2) -> inhibits dilation -> closes patent ductus arteriosus in newborns
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Diclofenac
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Treats endometriosis - seposatory to treat mensturation
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Sulidac
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produrg
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Piroxiam
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Long half-life -> More GI bleeding vs aspirin - used for RA, osteoarthritis, 1 ° dysmenorrhea
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What is the advantage of COX2 inhibitor? Disadvantage
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Advantage = no GI bleeding, disadvantage == causes MI
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What are the clinical applications of COX2 inhibitors
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Osteoarthrits, RA, 1 ° dysmenorrheal, acute pain in adults familial adenomatosus polyposis
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What is the MOA of acetaminophen
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COX3 inhibition
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What is the adverse effects of acetaminophen
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Hepatotoxicity-> metabolite of acetominophen can cause ROS damage in glutathione, nephrotoxicity, and hypothermia
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What is the MOA of zileuton
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Lipoxygenase inhibitor -> inhibits produciton of leukotrienes
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What is the clinical application of zileuton
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Asthma
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What is the side effect of lipoxygenase inhibitors
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Urticaria, abdominal discomfort, dizziness, and insomnia
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What are prostanoids
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Eicosanoids that are natural or synthetic that are used as medicine
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What drugs are Leukotriene receptor antagonists?
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Montelukast, zafirlukast(anti-eicosanoids)
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What is the clinical applications of montelukast and zafirlukast?
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Chronic asthma, perennial allergic rhinitis (montelukast), seasonal allergic rhinitis(montelukast)
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What are the adverse effects of montelukast and zafirlukast?
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Leukotriene receptor antagonist -> GI distress, hallucination, agitation, allergic granulomatosis angiitis, hepatitis
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Dysmennorrhea
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PGE2 + PGF2alpha -> uterus has high expression of these 2 PG
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What molecules can terminate pregnancy(abortion) at any stage secondary to uterine contraction
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PGE2(dinoprostone) + PGF2alpha
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What are the uses for dinoprostone
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Dinoprostone = PGE2; 1. induction of labor at term (ripens cervix), 2. missed abortion(dead fetus but system is continuing like the fetus is still alive), 3. benign hydatidiform mole(blank egg implants on accident)
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What is the side effects of dinoprostone
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Prolonged vaginal bleeding + menstrual cramps if used for menstrual regulation or early abortion(aka 1st trimester)
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What drug is a synthetic dervitive for PGE1?
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Misoprostol
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What is the molecules in the morning after pill?
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Misoprostol (PGE1) (leads to uterine contraction) + mifepristone(competitive inhibitor of progesterone)-> induction of uterine contraction
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What is the use of misoprostol?
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Peptic ulcers (NSAID induced)
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What is the uses of carboprost(15-methl PGF-2alpha)
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1. 2nd trimester abortion, 2. resistant postpartum hemorrhage
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What are the adverse effects of carboprost (15-methyl-PGF-2alpha)
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GI disturbances, dystonia, pulmonary edema
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Alprostadil
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A PGE1 agonist -> used to treat erectile dysfunction (ED) or maintenance of patent ductus arteriorsus
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What is the route of administration of alprostadil?
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Intracavernosal injection or urethral suppository
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Treprostinil
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Synthetic PGI2 -> causes vasodilation -> treats pulmonary hypertension(directly inhaled thus localized); side effect = hypotension
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Epoprostenol
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Synthetic PGI2 -> causes vasodilation -> treats pulmonary hypertension(directly inhaled thus localized); side effect = hypotension, rash, GI disturbances, muscle pain
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What is the treatment for dysenorrhea?
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NSAIDS -Aspirin blocks generation of PGE2 and PGF2alpha -> prevents menstrual pain
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