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Pharmacology II Exam 5 MOAs
Pharmacology II Exam 5 MOAs
60
Pharmacology
Professional
04/26/2012

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Term
Eicosanoids
Definition
Derived from fatty acids that make up cell membranes, cell-specific, exert complex control over bodily systems (inflammation, vasoconstriction, vasodilation, coagulation, pain, fever)
Term
Cyclooxygenase (COX) Products
Definition
Prostaglandins (PG), Prostacyclin (PGI2), Thrmoboxane (TX); collectively know as the prosanoids, a subclass of eicosandoids
Term
Lipoxygenase (LOX) Product
Definition
Leukotrienes
Term
MOA of Eicosanoid Production
Definition
Arachadonic acid is released from the phospholipids of the cell membrane under certain circumstances. It is acted on by COX to produce prostaglandins, prostocyclin, and thromboxane. AA is acted upon by LOX to produce leukotrienes.
Term
PGE2
Definition
Bronchodilation, inhibits gastric acid secretion and increases mucus production, contracts pregnant uterine muscle, induces fever, sensitizes nervous system to pain, promotes inflammation
Term
PGF2α
Definition
Contracts uterine muscle, lowers intraocular pressure,
Term
PGE1
Definition
contracts pregnant uterine muscle, relaxes smooth muscle of the corpora cavernosa
Term
PGI2
Definition
Bronchodilation, Inhibit gastric acid secretion and increases mucus production, sensitizes nervous system to pain, opposes TX by decreasing platelet adhesion
Term
Dinoprostone
Definition
Mimics the action of PGE2 which is released during natural labor and causes cervical ripening (vaginal gel or insert); vaginal suppository is for pregnancy termination in 2nd trimester and evacuation of uterine contents
Term
Carboprost Tromethamine
Definition
Mimics PGF2α which is produced by the uterus in the event there has been no implantation, causing uterine contraction which expels the products of conception
Term
Misoprostol
Definition
Mimics PGE1 which inhibits gastric acid secretion and stimulates mucus and bicarbonate secretion providing a gastroprotective effect
Term
Alprostadil (erectile dysfunction)
Definition
Mimics PGE1 which causes smooth muscle relaxation in the corpus cavernosa and corpus spongiosa
Term
Alprostadil (patency of DA)
Definition
Mimics PGE1 which causes vasodilation of the DA and prevents/reverses it from closing after birth
Term
Epoprstenol, Iloprost, Treprostenil
Definition
Mimics PGI2 which causes direct vasodilation of pulmonary and systemic arterial vascular beds and inhibition of platelet aggregation
Term
NSAIDs
Definition
Reversibly (except for aspirin) inhibits COX 1&2 resulting in a decrease in prostaglandin formation
Term
NAPQI
Definition
toxic metabolite of APAP metabolism that builds up after GSH levels are depleted from conjugation leading to hepatic toxicity through reactions with hepatic proteins and nucleic acids
Term
Colchicine
Definition
binds tubulin and inhibits its polymerization thus stopping leukocyte migration, phagocytosis, and cytokine release
Term
Uricorsic Agents (Probenecid, Sulfinpyrazone)
Definition
Competitively inhibit uric acid reabsorption in the proximal convoluted tubule thereby promoting its excretion
Term
Allopurinol
Definition
an isomer of xamthine oxidase that competitively ; it is metabolized to oxypurinol which is also a competitive inhibitor of xanthine oxidase
Term
Febuxostat
Definition
a non-purine non-competitive inhibitor of xanthine oxidase, the enzyme responsible for converting hypoxanthine to xanthine and then to uric acid thereby lowering UA levels
Term
Antacids
Definition
bases that react with stomach HCL forming salt and water and increasing pH
Term
H2-Receptor Antagonists
Definition
Block the H1 receptors on the surface of parietal cells which leads to reduced acid production
Term
Proton Pump Inhibitors (PPIs)
Definition
Block the proton pump (H+/K+ ATPase) in the parietal cells suppressing the secretion of protons in the the gastric lumen
Term
Sucralfate
Definition
reacts with HCL in stomach when the negatively charged sucrose sulfate binds to the positively charged proteins in the base of ulcers or erosions forming a paste-like material that creates a barrier and restricts further damage; also stimulates mucosal prostaglandin and bicarbonate secretion
Term
Bismuth Subsalicylate
Definition
Coats ulcers and erosions creating a protective layer against acid and pepsin and has a direct antimicrobial action and binds enterotoxins. Also provides antisecretory effect reducing diarrhea and anti-inflammatory action.
Term
Metoclopramide
Definition
Inhibits D2 receptors increasing esophageal peristaltic activities and enhancing gastric emptying; when activated, D2 receptors usually inhibit smooth muscle stimulation
Term
Neostigmine
Definition
cholinesterase inhibitor that enhances ACh levels and increases gastric, small intestine, and colonic emptying
Term
Bulk Forming Laxatives
Definition
absorb liquid in the intestines and swell stimulating intestinal muscle peristalsis resulting in elimination
Term
Stool Surfactants
Definition
reduce the surface tension of the oil-water interface of stool resulting in enhanced water incorporation and stool softening
Term
Lubricant Laxatives (mineral oil)
Definition
eases passage of stool by retarding colonic absorption of fecal water thus softening stool
Term
Osmotic Laxatives
Definition
soluble compounds that create an osmotic gradient and pull water into the intestine resulting in increased stool liquidity
Term
Lactulose
Definition
nonabsorbable disaccharide, metabolized by GI bacteria into acetic and formic acids that exert osmotic effect
Term
Castor Oil
Definition
ricinoleic acid containing agent that acts in the small intestine and reduces net absorption of fluid and electrolytes and stimulate peristalsis
Term
Lubiprostone
Definition
PEG1 derivative that stimulates chloride channels in the small intestine increasing release of chloride-rich fluids into the intestine thereby softening stool, increasing motility, and promotingn spontaneous bowel movements
Term
Opioid receptor antagonists (Methylnaltrexone, Alvimopan)
Definition
blocks opioid binding at the μ-opioid receptor in the GI tract and inhibits opioid-induced decrease in gastrointestinal motility and delay in gastrointestinal transit time decreasing opioid-induced constipation
Term
Opioid Agonists (Loperamide, Diphenoxylate)
Definition
act on the μ-opioid receptors in the large intestine and restricts GI motility and GI propulsion, decreasing intestinal transit time allowing for more water to be absorbed out of the fecal matter and slowing of the colonic mass movement
Term
Octreotide
Definition
somatostatin analog that inhibits the secretion of hormones (gastrin, chlecstokinin, secretin) and reduces intestinal fluid secretion as well as pancreatic and gallbladder secretions slowing GI motility
Term
Dicyclomine, Hyoscyamine
Definition
muscarinic receptor blockers that block binding of ACh on the surface of smooth muscle cells of the intestine causing relaxation
Term
Alosetron
Definition
serotonin (5-HT3) receptor antagonist that blocks GI 5-HT3 receptors and reduces pain, abdominal discomfort, urgency, and diarrhea associated with IBS
Term
Aminosalicylates
Definition
act locally in the colon to decrease inflammation by modulating the COX and LOX derived chemical mediators, interfering with cytokine production, inhibiting cellular functions of NK cells and macrophages, and acting as free radical scavengers
Term
Ondanestron, Granisetron, Dolasetron, Palonosetron
Definition
serotonin (5-HT3) receptor antagonist blocks the 5-HT3 receptor on both peripheral vagal nerve terminals and in the central chemoreceptor trigger zone
Term
Aprepitant, Fosaprepitant
Definition
blocks neurokinin 1 (NK1) receptors in the vomiting center
Term
Prochlorperazine, Droperidol, Metoclopramide, Trimethobenzamide
Definition
D2 receptor antagonists that work in the chemoreceptor trigger zone
Term
Scopolamine
Definition
muscarinic receptor antagonist that works on receptors in vestibular system
Term
Ursodiol
Definition
Suppresses hepatic synthesis and secretion of cholesterol, inhibits intestinal absorption of cholesterol, and accumulates in bile effectively solubilizing cholesterol
Term
Triptans
Definition
agonists of the 5-HT(1B & 1D) serotonin receptors in the cerebral and meningeal vessel causing vasoconstriction and reduction in the release of pro-inflammatory neuropeptides
Term
Zafirlukast, Montelukast
Definition
Competitive inhibitor at leukotriene receptor cys-LT1 block bronchoconstriction and inflammation
Term
Zileuton
Definition
inhibits 5-lipoxygnase (LOX) and reduces leukotriene production
Term
Methylxanthines
Definition
nonselective inhibitors of cyclic nucleotide phosphodiesterase enzymes (PDEs), which catalyze the hydrolysis of cyclic nucleotides (ultimately increases levels of cAMP and cGMP and has many effects, most importantly relaxes smooth muscle and reduces activity of immune cells)
Term
Roflumilast
Definition
PDE4 inhibitor; inhibition of this enzyme increases cAMP levels and reduces the activity of immune cells
Term
Atropine, Ipratropium
Definition
muscarinic receptor antagonists that competitively inhibit ACh blocking the contraction of airway smooth muscle and the increase in airway mucus
Term
Acetylcysteine
Definition
Reduces disulfide bonds within proteins which decreases viscosity of mucus
Term
Dornase Alfa
Definition
an enzyme that breaks down DNA decreasing polymerization which decreases mucus viscosity
Term
Bacitracin
Definition
Peptide antibiotic that interferes with cell wall synthesis
Term
Gramicidin
Definition
Peptide antibiotic that alters cell wall permeability
Term
Mupirocin
Definition
inhibits isoleucine t-RNA synthetase, which inhibits protein synthesis
Term
Retapamulin
Definition
protein synthesis inhibitor due to interaction with unique site on 50S subunit of the bacterial ribosome that inhibits peptidyl transferase function
Term
Polymixin B Sulfate
Definition
detergent – increases bacterial cell wall permeability, resulting in cell lysis (like gramicidin)
Term
Neomycin, Gentamicin
Definition
protein synthesis inhibitors
Term
Lindane
Definition
neurotoxin; binds to picrotoxin site of GABA-A receptors; disrupts chloride channels, which disrupts GABA neurotransmission
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