Term
| inhibitors of HMG-CoA reductase, reduce LDL levels by increasing hepatic uptake of LDL, VLDL, and remnants; reduce susceptibility of lipoproteins to oxidation; given at night for maximal effect; have relatively short half-lives |
|
Definition
|
|
Term
| rhabdomyolysis (requires UA for myoglobin), hepatotoxicity, neuropathy, mild GI symptoms, HA, rash, insomnia |
|
Definition
| adverse effects of statins |
|
|
Term
| hepatotoxicity, pregnancy/nursing mothers, drug interactions w/ coumarin and gemfibrozil |
|
Definition
| contraindications of statins |
|
|
Term
| cationic polymers that bind anionic bile acids in the intestinal lumen, activate hepative uptake of LDL to cause fall in plasma LDL; for use only where LDL is elevated; reduce LDL 10-20%; raise HDL 3-5%; reduce major coronary events and coronary heart disease mortality; side effects include increased TG levels and GI distress |
|
Definition
|
|
Term
|
Definition
| contraindications of bile sequestrants |
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|
Term
| blocks intestinal absorption of cholesterol by inhibiting NPC1L1 protein; inhibits cholesterol absorption by ~55%; reduces LDL ~18% |
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Definition
|
|
Term
| decrease synthesis of VLDL; increase HDL; have complex mechanism of action involving PPARalpha agonism and altered gene expression; 90% absorbed w/ fast plasma peak concentration; >95% albumin bound; increase ApoA1 and 2; decrease ApoC3; require incredible fluid consumption with medication |
|
Definition
|
|
Term
| myalgias, rhabdomyolysis, increased incidence of gallstones, increased ALT/AST, GI distress |
|
Definition
| adverse effects of fibrates/fibric acids |
|
|
Term
| increased rhabdomyolysis w/ statin drugs, severe renal or hepatic disease; interact w/ warfarin to cause increased bleeding; interact w/ cyclosporine to increase cyclosporine clearance and cause acute transplant rejection |
|
Definition
| contraindications of fibrates |
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|
Term
| reduces VLDL and LDL w/o effect on synthesis of cholesterol or excretion of bile acids; most effective agent for raising HDL (30-40%); requires 2g dose and has short half-life |
|
Definition
|
|
Term
| first choice therapy for heterozygous familial hypercholesterolemia; acid-neutralizing effect cancels GI upset |
|
Definition
| niacin + resin combination |
|
|
Term
| has maximum effectiveness for combo therapy |
|
Definition
|
|
Term
| more effective in combo but increase incidence of gallstones |
|
Definition
|
|
Term
| statin + bile acid sequestrants for lipid-lowering; statin + cholesterol absorption inhibitor (Vytorin) |
|
Definition
|
|
Term
| considered "riskier" combo, for combined dyslipidemias, has greater potential for myopathies |
|
Definition
|
|
Term
| for combined dyslipidemia, increase risk of myopathy, considered "riskier" |
|
Definition
|
|
Term
| "riskier" combo, used for combined dyslipidemia |
|
Definition
| statin + niacin + fibric acid |
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|
Term
| promote healing of gastric ulcers, treat GERD and hypersecretory (zollinger-ellison syndrome), also to reduce risk of duodenal ulcer recurrence associated w/ H. pylori; exist as prodrugs, enter parietal cells and accumulate w/ canaliculi; bind irreversibly with the sulfhydryl groups on the pump and force their re-synthesis |
|
Definition
|
|
Term
| made into "delayed release" oral dosage forms by being gastric-resistant; elimination half life is 1-2 hrs but duration of action is 24-48 hrs; metabolized by CYP2C19 and CYP3A4; variants of CYP2C19 can have poor metabolism of this class; hepatic disease reduces clearance while renal does not; requires several doses to achieve maximum suppression (2-5 days to suppress 70%) |
|
Definition
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|
Term
| do not give with acid-suppressing medications; hypergastrinemia in 5-10% of users; decreased absorption of Vit B12 (questionable); inhibition of CYP enzymes increases half life of other drugs |
|
Definition
| adverse effects/contraindications of PPIs |
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|
Term
| reversibly compete w/ histamine for binding to H2 receptors on the basolateral membrane of parietal cells; suppress basal acid secretion; effects are dose related; examples: cimetidine, ranitidine, famotidine, nizatidine |
|
Definition
|
|
Term
| gynecomastia and impotence in males (inhibited metabolism of estrogen at CYP); increased half life of other drugs using CYPs; tolerance possibly due to secondary hypergastrinemia; acid rebound requires terminal dosage to be tapered |
|
Definition
| negative effects of H2 receptor antagonists |
|
|
Term
| synthetic analog of PGE1; binds to EP3 receptors on parietal cells and inhibits acid secretion; stimulates secretion of mucin and bicarbonate; increases mucosal blood flow |
|
Definition
|
|
Term
| undergoes extensive first-pass metabolism to deesterified acid; food and antacids delay absorption; effective w/in 30 min and peak at 60-90; duration = 3 hrs; renal elimination w/ half life = 20-40 min; requires frequent dosing |
|
Definition
| pharmacokinetics of misoprostol |
|
|
Term
| diarrhea (30%), exacerbation of IBD, abortifacent |
|
Definition
| adverse effects of misoprostol |
|
|
Term
| sulfated polysaccharide w/ aluminum hydroxide; cross-linking in acidic pH yields sticky polymer that adheres to mucosa and ulcerated surfaces; not used for peptic ulcer; used in inflammatory conditions that do not respond well to PPIS and also stress ulcers; adverse effects: affect gastric absorption of drugs and can cause constipation (2%) |
|
Definition
|
|
Term
| neutralize acid but do not inhibit secretion; raise gastric pH to 3.5; duration of action is short and determined by acid-combining ability and length of stay in stomach |
|
Definition
| dynamics and kinetics of antacids |
|
|
Term
| highly effective and inexpensive antacid; has short duration of action, delivers 12 mEq of sodium/gram, causes alkalosis w/ excessive use, and produces CO2 |
|
Definition
|
|
Term
| has rapid onset and long duration for drug class, provides calcium; causes local (constipation, acid rebound, gas) and systemic (elevated plasma calcium, alkalosis) effects |
|
Definition
|
|
Term
| does not form gas; adverse effects include: diarrhea, increase plasma magnesium in patients w/ altered kidney function, and can lead to CNS toxicity |
|
Definition
|
|
Term
| additional class of antacid; limited by constipation, neurotoxicity due to Al- exposure w/ chronic renal disease, myopathy, reduced phosphate reabsorption from gut, ultimately weakens bone by draining Ca |
|
Definition
|
|
Term
| drug effectively neutralizes acid w/ fewer side effects by canceling constipation and diarrhea; GI effects are actually diminished but not zero; exposure to 2 cations becomes problem w/ renal dysfunction |
|
Definition
|
|
Term
| particle size determines efficacy; tablets are less effective than liquid; cause enhanced dissolution of weak bases and enteric coatings of capsules; decrease absorption of penicillin/tetracycline; alter urinary excretion of drugs by altering pH |
|
Definition
| therapeutic considerations of antacids |
|
|
Term
| either: 1) PPI/H2 antagonist + amoxicillin + clarithromycin/metronidazole or 2) PPI + tetracycline + bismuth sulfate + metronidazole; requires 7 day course |
|
Definition
| treatment of H. pylori infection |
|
|
Term
| enhance coordinated GI motility and transit of material in the GI tract; not direct stimulators of smooth muscle but rather influence activation of innervation to the gut (increase contractility); 2 classes currently used include dopamine receptor antagonists and motilin-mimetics |
|
Definition
|
|
Term
| considered prokinetic drug, not available in US, D2R antagonist, enhances Ach release by antagonizing inhibitory effect of dopamine on cholinergic nerves to GI muscle; inhibits emesis via CTZ (in CNS) and in the stomach; no extrapyramidal effects (does not cross BBB well), may enhance prolactin release; used for gastroparesis and N/V from dysmotility |
|
Definition
|
|
Term
| increases tone of lower esophageal sphincter and antral/small intestine contractions, facilitates gastric emptying, has no effect on lower GI motility; considered D2R antagonist and mixed 5HT3R antagonist/5HT4R agonist; used for gastroparesis, postoperative ileus, and N/V caused by dysmotility |
|
Definition
|
|
Term
| extrapyramidal effects by inhibition of D2 receptors in CNS, tardive dyskinesia |
|
Definition
| adverse effects of metoclopramide |
|
|
Term
| acts like peptide that enhances gastric emptying; erythromycin is example; improves diabetic gastroparesis; no significant effect on lower GI; can enhance small bowel motility in ileus w/ high dose; tolerance can develop |
|
Definition
|
|
Term
| target chemoreceptor trigger zone (5HT-3R, D2R, and opioid Rs) and solitary tract nucleus (histamine Rs, AchR, and 5HT-3R); classes include: H1 anti-histamines, metoclopramide, phenothiazines, ondonsetron, marijuana, and glucocorticoids |
|
Definition
|
|
Term
| target H1 receptor, include: diphenhydrinate, diphenhydramine, meclizine, and promethazine; depress labyrinth excitability at brainstem, good for motion sickness; adverse effects involve CNS depression |
|
Definition
|
|
Term
| blocks 5HT3Rs, used for N/V from chemo/post-op/radiation; eliminated by liver w/ half-life at 6hrs; anti-emetic effect persists after drug is eliminated; adverse effects: allergic rxn, constipation, diarrhea, fever, HA (effects not common) |
|
Definition
|
|
Term
| synthetic or natural delta-9-tetrahydrocannabinol, stimulates receptors at or around emesis center (CB1R), highly lipid soluble, readily absorbed PO; has extensive first-pass metabolism so bioavailability ~10-20%; essentially 100% hepatic metabolism; highly bound to plasma protein; large volume of distribution; used for emesis and stimulation of appetite in cachexic pts; adverse effects: central sympathomimetic, "highs," paranoia, abstinence syndrome |
|
Definition
|
|
Term
| mechanism not clear; adjuncts for nausea in cancer pts, suppress inflammation and prostaglandin production |
|
Definition
| glucocorticoids as anti-emetics |
|
|
Term
| anti-diarrheal drugs, absorb water, include bulk-forming agents like carboxymethylcellulose/psyllium/kaolin/attapulgite/kaolin-pectin and bismuth |
|
Definition
|
|
Term
| anti-diarrheals, slow motility and/or secretion; include opioids such as loperamide, diphenoxylate, and difenoxin |
|
Definition
| antimotility/antisecretory agents |
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|
Term
| forms oxychloride and salicylic acid in stomach acid; compound travels through intestine while SA is absorbed (reduces cramps?); thought to be anti-secretory, anti-inflammatory, and antibacterial; used for traveler's diarrhea and H. pylori combo tx; known to blacken stool and tongue |
|
Definition
|
|
Term
| decrease intestinal motility through mu R, decrease intestinal secretion through delta R, decrease intestinal absorption through mu and delta Rs; include camphorated opium tincture and laudanum as older versions; current ones are loperamide, diphenoxylate, and difenoxin |
|
Definition
| opioids as anti-motility drugs |
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|
Term
| acts at mu R, 50 X more potent than morphine against diarrhea, poor penetration of CNS, OTC use for no more than 48 hours; can cause CNS depression in OD; use caution in children due to CNS sensitivity; do not use w/ active inflammatory disease of colon |
|
Definition
|
|
Term
| chemical relatives of meperidine; second is active metabolite of first; not as potent as loperamide and can cause CNS effects; have abuse potential |
|
Definition
| diphenoxylate and difenoxin |
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|
Term
| drugs that increase secretion of fluid, decrease absorption of fluid, and increase osmolality in the colon |
|
Definition
|
|
Term
| include anthraquinones, diphenylmethanes, castor oil, and dioctyl sodium succinate |
|
Definition
| agents increasing secretion |
|
|
Term
| made up of aloe, rhubarb, cascara segrada, and senna; effective in 8-12 hours; activated in colon; increase fluid secretion; often cause cramps and may get into breastmilk; cause "lazy bowel syndrome" with abuse |
|
Definition
|
|
Term
| phenolphthalein (withdrawn, carcinogenic) and bisacodyl; can cause inflammation of bowel |
|
Definition
|
|
Term
| acts as stool softener; surfactant, stimulates secretions; marginally useful in constipation but widely used |
|
Definition
|
|
Term
| decreases absorption of fluid, lubricates lumen of GI tract; effective in short-term use; adverse effects in long-term use include: inflammation from systemic absorption, aspiration PNA, decreased absorption of fat-soluble vitamins, and leakage |
|
Definition
|
|
Term
| include bran, methylcellulose, psyllium, and agar; not digested and therefore not absorbed; swell in presence of water which stimulates peristalsis; no cramping/lazy bowel/dependence; impaction possible |
|
Definition
| fiber and hydrophilic colloids |
|
|
Term
| increases osmolality, rapid onset, draws fluid from ECF which fills the gut and stimulates peristalsis, can be enemas |
|
Definition
| saline (w/ magnesium sulfate, milk of magnesia, etc) |
|
|
Term
| increases osmolality, hydrolyzed in gut to organic acids |
|
Definition
|
|
Term
| made up of long-chain PEGs, isotonically balanced, widely used for colon cleansing before GI procedures, patients must drink 4 liters of solution over 3-4 hours |
|
Definition
| PEG electrolyte solutions |
|
|
Term
| inhibition or activation of gene expression, blockade of intracellullar signaling, receptor antagonism, chemical neutralization, co-stimulation modulation, blockade of synthesis, diminish release, and inhibit immune response |
|
Definition
| drug strategies for suppressing immunity/inflammation |
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|
Term
| used with other agents to prevent/treat transplant rejection (ex: high doses of methylprednisolone IV for acute transplant rejection), effective in GVHD, used in autoimmune dxs, extensive long-term use limited by toxicity |
|
Definition
|
|
Term
| inhibitor of T-cell mediated immunity, binds to cyclophilin and inhibits production of IL-2 (calcineurin is inactive and cannot phosphorylate nuclear receptors); used for transplants and in combination with glucocorticoids and antimetabolites; used in severe rheumatoid arthritis; problems: nephrotoxicity, HTN (~50% of renal tx pts), tremor, hyperlipidemia, and hirsutism |
|
Definition
|
|
Term
| given PO or IV, oral absorption is slow w/ low bioavailability; extensive drug interactions due to CYP3A use; cannot eat grapefruit!!! |
|
Definition
| pharmacokinetics of cyclosporine |
|
|
Term
| more potent immunosuppressant; binds to FKBP; metabolized by CYP3A; used for transplant and rescue therapy in rejection episodes; problems: nephrotoxicity, neurotoxicity, etc; requires therapeutic drug monitoring |
|
Definition
|
|
Term
| binds to FKBP but does not inhibit calcineurin; blocks IL-2 receptor signaling and arrests cell division; side effects: hyperlipidemia, leukopenia, and thrombocytopenia; used for prophylaxis in transplantation and in pts with high risk for nephrotoxicity; consider drug interactions w/ CYP3A |
|
Definition
|
|
Term
| prodrug of purine analog mercaptopurine which inhibits gene translation; side effects: bone marrow suppression, susceptibility to infection, gout (altering purine levels!) |
|
Definition
|
|
Term
| first inhibits IMPDH (rate-limiting enzyme in guanosine formation) while second is prodrug w/ higher bioavailability; preferentially acts on lymphocytes due to IMPDH pathway for purine synthesis; used for transplant rejection w/ glucocorticoids and calcineurin inhibitors but NOT azathioprine; major side effects: vomiting, diarrhea, leukopenia, and increased risk for infection |
|
Definition
| mycophenolic acid and mycophenolic mofetil |
|
|
Term
| folate analog used as anticancer drug, in RA, and GVHD; has cytotoxic and anti-inflammatory activity |
|
Definition
|
|
Term
| polyclonal Abs from rabbit injected w/ thymocytes; Abs to T-cell antigens deplete circulating lymphocytes; used for induction of immunosuppression and acute renal rejection; can be used for withdrawal of calcineurin inhibitors; side effects: cytokine release syndrome (fever, HA, tremor, N/V, malaise, general weakness) |
|
Definition
|
|
Term
| mouse monoclonal Ab against human CD3; depletes T-cells; indicated for organ transplant rejection; major side effect is cytokine release syndrome; production of Abs to drug occurs in host; potentially fatal pulmonary edema, CV collapse, and arrhythmias occur |
|
Definition
|
|
Term
| humanized anti-CD25 mouse monoclonal Abs; first given prophylactically for renal transplants and with other immunosuppressants; bind to IL-2 Rs on activated T-cells (second has higher affinity); side effects are infection and anaphylaxis |
|
Definition
|
|
Term
| human monoclonal Ab against B lymphocyte stimulator; side effects are infection, severe allergic reactions, and cardiac problems |
|
Definition
|
|
Term
| CTLA-4 fusion protein; binds to B7-1 and B7-2 to prevent co-stimulation; used for RA; should not be used w/ TNFalpha inhibitors |
|
Definition
|
|
Term
| congener of abatacept; increased affinity for B7 complexes |
|
Definition
|
|
Term
| major endogenous steroid w/ glucocorticoid activity; hydroxyl at 11 position |
|
Definition
|
|
Term
| have carbonyl bonds at 11 carbon so compounds inactive until metabolized by 11beta hydroxysteroid dehydrogenase |
|
Definition
|
|
Term
| 4-6 times more potent than cortisol for anti-inflammatory activity; have low mineralocorticoid activity |
|
Definition
| prednisolone/methylprednisolone |
|
|
Term
| has higher mineralocorticoid activity; in glucocorticoid class |
|
Definition
|
|
Term
| greater than 18 times more potent than cortisol w/ no mineralocorticoid activity |
|
Definition
|
|
Term
| prototypes used to treat asthma, have fewer systemic effects; include: fluticasone, beclomethasone, flunisolide, and triamcinolone; can cause hoarseness and oral candidiasis |
|
Definition
|
|
Term
| bind to Type 2 receptor and is transported to nucleus to bind with GREs; antagonize insulin action and promote gluconeogenesis; increase muscle catabolism; augments GH action on lipolysis (increase triglycerides); decrease inflammatory response; reduce cytokine release; reduce production of eicosanoids |
|
Definition
| mechanisms of action of glucocorticoids |
|
|
Term
| well-absorbed from GI tract; cortisol is highly bound to protein but synthetics are not; lipophilic compounds; metabolized by liver and extrahepatic enzymes; note: prednisone safe in pregnancy because fetal liver lacks 11b hydroxysteroid dehydrogenase |
|
Definition
| pharmacokinetics of glucocorticoids |
|
|
Term
| replacement therapy; anti-inflammatory and immune suppression (do not improve underlying disease); asthma treatment when inhaled; topical for psoriasis and dermatitis; depot injections for arthritis and gout |
|
Definition
|
|
Term
| increased susceptibility to infection, increased glucose and diabetes, secondary hyperparathyroidism, osteoporosis, edema, suppression of linear bone growth in children, steroid psychosis, Cushing's syndrome, withdrawal "rebound," and myopathy |
|
Definition
| toxic side effects of glucocorticoids |
|
|
Term
| tend to have more systemic toxicity since they inhibit hepatic P450s; include: mitotane, aminoglutethimide, ketoconazole, metyrapone, and trilostane |
|
Definition
| drugs inhibiting steroid synthesis |
|
|
Term
| used as antineoplastic agent in adrenal tumors; toxic to adrenocortical cells |
|
Definition
|
|
Term
| blocks cholesterol side chain cleavage; dose dependent GI and neuro side effects as well as rash; causes frank adrenal insufficiency |
|
Definition
|
|
Term
| antifungal agent; primarily inhibits steroid 17a hydroxylase; most effective inhibitor of steroid biosynthesis in pts w/ Cushing's disease; major side effect is hepatic dysfunction |
|
Definition
|
|
Term
| acts as mineralocorticoid antagonist |
|
Definition
|
|
Term
|
Definition
| short-acting B2 selective agonists for asthma |
|
|
Term
| salmeterol, formoteral, indacaterol |
|
Definition
| long-acting B2 agonists for asthma |
|
|
Term
| methylxanthine, used as maintenance therapy for asthma/COPD; not used as much unless pt has cardiac problems; relaxes smooth muscle, increases cAMP, and blocks adenosine A2 receptors; side effects: insomnia, agitation, tachycardia, tremor; can be used in status epilepticus |
|
Definition
|
|
Term
| muscarinic R antagonist; quaternary so minimizes CNS effects; used in COPD and asthma w/ other bronchodilators; useful for pts that cannot take B2 agonists |
|
Definition
|
|
Term
| glucocorticoid inhaled daily to suppress airway inflammation |
|
Definition
| beclomethasone diproprionate |
|
|
Term
| inhibitors of mast cell degranulation; stabilize mast cells by unknown mechanism; used by inhalation to prevent mild to moderate asthma attacks; used w/ glucocorticoids to prevent moderately severe asthma; do NOT relieve acute sxs |
|
Definition
|
|
Term
| act as leukotriene R antagonists; prevent actions of cysteinyl leukotrienes at CysLT1 Rs; given orally for prophylactic treatment of mild asthma; rare side effects: pulmonary infiltrates, neuropathy, skin rashes, and vasculitis (similar to Churg-Strauss syndrome) |
|
Definition
|
|
Term
| 5-lipoxygenase inhibitor; inhibits formation of all LOX products; given orally for prophylaxis of mild asthma; can elevate liver enzymes in ~5% of pts |
|
Definition
|
|
Term
| humanized monoclonal IgE Ab; binds to Fc domain of IgE so it cannot interact w/ R; administered IV or subQ every 2-4 weeks; reduces airway responsiveness and decreases need for other asthma drugs; concern for infection and pain at injection site |
|
Definition
|
|
Term
| inhibits phosphodiesterase 4; increases cAMP; administered for severe COPD; use limited by side effects (HA, N/V, acute pancreatitis, acute renal failure, a-fib) |
|
Definition
|
|
Term
| H1R antagonists; well-absorbed from GI tract; widely distributed to body (especially CNS); extensively metabolized; side effects: sedation, dizziness, lassitude, fatigue, nervousness, insomnia, tremor, loss of appetite, N/V, dryness of mouth, cough (anticholinergic responses), and hypersensitivity reactions; class includes diphenhydramine, chlropheniramine, pyrilamine, hydroxyzine, and doxepin |
|
Definition
| first generation antihistamines |
|
|
Term
| H1R antagonists; well-absorbed but do not distribute to CNS; metabolized by P450s and have drug interactions; side effects: no anticholinergic responses, minimal sedation, and drowsiness; include: cetirizine, loratadine, desloratadine, and fexofenadine |
|
Definition
| second generation antihistamines |
|
|
Term
| acute allergic reactions, reduce itching, diminish sxs of cold/flu; select few used for prophylaxis and treatment of motion sickness; diphenhydramine can reduce early Parkinson's symptoms; N/V; somnolence |
|
Definition
| therapeutic actions of antihistamines |
|
|
Term
| causes platelet aggregation, constriction of vascular smooth muscle in splanchnic/renal/pulmonary/cerebral vasculature, positive inotropic and chronotropic action, stimulates small intestine motility, inhibits stomach smooth muscle, sensitizes small-diameter sensory neurons, affects sleep/cognition/temp regulation/motor activity |
|
Definition
| 5-hydroxytryptamine actions |
|
|
Term
| 5HT1 R agonists, thought to have direct vasoconstrictor action on intracranial blood vessels and presynaptic inhibition on sensory neurons; class includes: sumatriptan, naratriptan, rizatriptan, zolmitriptan, and almotriptan; drugs of choice for migraine tx; not for long-term use; administered by injection, orally, or nose spray |
|
Definition
|
|
Term
| either agonists or antagonists at multiple receptors; have agonist action at 5HTR; side effects: nausea, vasoconstriction w/ ischemia, leg weakness, and muscle pain; contraindicated in pregnancy, CAD, PAD, liver/renal disease; class includes: ergotamine, dihydroergotamine, and methysergine |
|
Definition
|
|
Term
| used for prophylaxis of migraines; long-term use can cause pts to develop retroperitoneal/cardiac/pulmonary fibrosis; do not give for more than 6 months |
|
Definition
|
|
Term
| used as prophylactic for migraines; requires gradual increase in dosing; side effects: acute myopia, glaucoma, decreased sweating/hyperthermia, metabolic acidosis, cognitive dysfunction, psychiatric/behavioral disturbances, somnolence, and fatigue |
|
Definition
|
|
Term
| synthetic PGE1, used to maintain maternal/fetal blood flow; possible role in impotence tx |
|
Definition
|
|
Term
| PGE1 analog approved to promote ulcer healing |
|
Definition
|
|
Term
| drug for parturition, prostin E2 synthetic, formulated as suppository |
|
Definition
|
|
Term
| irreversibly inhibits COX isomers; used for pain relief, fever reduction, anti-inflammatory, and prophylactic risk reduction for MI by anti-platelet effects; has significant toxicity and poisoning potential; affects acid-base balance; not for use in: ulcer pts, those w/ allergies, pts w/ clotting dxs, pregnancy, gout, and viral infections in children/young adults |
|
Definition
|
|
Term
| para-aminophenol derivative; weak anti-inflammatory agent; weak effects on platelets and no change in bleeding time; no uricosuric effects; no alterations in acid-base balance; minimal effects on GI; used for analgesia and antipyresis; risk for fatal hepatic necrosis w/ acute overdose; can cause skin rash and rarely leukopenia |
|
Definition
|
|
Term
| antidote for acute acetaminophen toxicity; replenishes glutathione that metabolite has used up, prevents necrosis |
|
Definition
|
|
Term
| has marked anti-inflammatory action; not used much due to high toxicity; in indole and indene acetic acid class |
|
Definition
|
|
Term
| arylproprionic acid; fewer GI side effects for NSAID; requires more frequent dosing |
|
Definition
|
|
Term
| arylproprionic acid; twice a day dosing |
|
Definition
|
|
Term
| COX2 inhibitor; has limited adverse effects due to R selectivity; contraindicated in pts w/ sulfa sensitivity; reports of excessive GI bleeding/ulceration; removed from market due to potential cardiotoxicity |
|
Definition
|
|
Term
| Ab to TNFalpha, used for Crohn's disease and RA; reported to cause anaphylaxis or lupus-like reaction on rare occasions |
|
Definition
|
|
Term
| Ab to TNFalpha; for RA, Crohn's, psoriasis, and ankylosing spondylitis |
|
Definition
|
|
Term
| Ab to TNFalpha; for RA, psoriatic arthritis, and ankylosing spondylitis |
|
Definition
|
|
Term
| humanized monoclonal Ab to alpha4 integrin; used for Crohn's and relapsing MS |
|
Definition
|
|
Term
| construct of TNFalpha R binding site for RA, Crohn's |
|
Definition
|
|
Term
| used in management of progressive RA that is unresponsive to other txs; can relieve pain and stiffness but do not arrest joint degeneration; side effects limit usage, include: metallic taste, stomatitis, diarrhea, abdominal pain/cramping, rash, dermatitis, thrombocytopenia, aplastic anemia, agranulocytosis, and acute tubular necrosis |
|
Definition
|
|
Term
| useful in relieving acute gout attacks; effective in prophylaxis; not uricosuric; inhibits migration of granulocytes to inflamed area; major side effects: N/V, diarrhea, abdominal pain; long-term use increases incidence of blood dyscrasias |
|
Definition
|
|
Term
| increase clearance and excretion of uric acid by decreasing reabsorption; pt needs to drink lots of water to alkalinize the urine and prevent precipitation of uric acid in renal tubules |
|
Definition
| probenecid and sulfinpyrazone |
|
|
Term
| competitive antagonists of xanthine oxidase; reduce formation of uric acid |
|
Definition
| allopurinol and febuxostat |
|
|
Term
| broad term; substance that can produce morphine-like effects that are blocked by R antagonists; can be endogenous, naturally occuring, semisynthetic, and synthetic |
|
Definition
|
|
Term
| alkaloids in opium and their natural and semi-synthetic derivatives |
|
Definition
|
|
Term
| beta endorphin, dynorphin, and enkephalins |
|
Definition
| endogenous opioid peptides |
|
|
Term
| 3 subtypes, act at G proteins to decrease adenylyl cyclase activity, open a subclass of K channels, and close Ca channels |
|
Definition
|
|
Term
| analgesia, anti-tussive, treatment of diarrhea/dysentery, and special anesthesia/sedation |
|
Definition
| therapeutic actions of opioids |
|
|
Term
| agonist at mu opioid receptor, has some effect at kappa and delta; used for analgesia and cough suppression; many routes of administration; use caution in neonates and pts w/ chronic kidney dx; problems: resp depression, constipation, abuse potential, N/V (~40%), histamine release |
|
Definition
|
|
Term
| allows for slow rise in serum levels to avoid "rush" sensation; has prolonged effect; patient can independently control intake; less drug is needed to prevent recurrence of pain than to relieve it |
|
Definition
| controlled release formulation of morphine |
|
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Term
| readily absorbed; significant first-pass metabolism; low bioavailability; delay absorption of other PO drugs; rapid distribution; onset/duration influenced by lipophilicity |
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Definition
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Term
| signs include: pinpoint pupils, resp depression, coma; accompanied by hypotension, hypoglycemia, and hypothermia |
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Definition
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Term
| agonist at mu opioid R; some effects at delta; more potent than morphine; used for analgesia (post-op, labor, chronic pain, anesthetic adjuvant); very lipid soluble; can be used as transdermal patch; problems: resp depression, constipation, abuse potential; HOWEVER no release of histamine, less vasodilation/orthostatic hypotension |
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Definition
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Term
| mu R agonist; rapid onset (1-1.5min); ester linkage susceptible to esterases and therefore very short half-life; analgesic for moderate to severe pain and anesthesia adjunct; problem is resp depression |
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Definition
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Term
| agonist at mu, some effects at others; metabolized to compound w/ antimuscarinic effects so pupils DILATE instead of constrict; not as frequently used due to unpredictable metabolism; problems: resp depression, constipation, abuse potential, seizure potential, antimuscarinic effects (negative inotropic action, tachycardia) |
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Definition
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Term
| drug that is metabolized to morphine, very lipid soluble; not more potent but faster acting; produces sensations of warmth, taste, high, or intense pleasure; sedates; no clinical use |
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Definition
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Term
| agonist at mu; racemic mixture blocks NMDA Rs and monoaminergic reuptake transporters; binds extravascularly and is slowly released; long half-life; used for analgesia of difficult-to-treat pain and relief of opioid dependence; problems: resp depression, prolonged QT-based arrhythmias (rare); may be involved in as many as 1/3rd of all prescription opioid-related deaths! |
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Definition
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Term
| mixed agonist/antagonist; partial agonist at mu; antagonist at kappa; has long duration due to slow dissociation; used for analgesia for difficult-to-treat pain and opioid dependence; decreased severity of resp depression and constipation; RESISTANT to naloxone reversal; concern about abuse potential |
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Definition
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Term
| mixed agonist/antagonist; agonist at kappa; antagonist at mu; used in analgesia of severe pain and pre-op medication; limited resp depression and constipation; increased HR and BP at high doses; dysphoria due to kappa R activity; combination w/ naloxone reduces misuse as injectable |
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Definition
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Term
| prodrug that is metabolized to morphine; agonist at mu w/ slight action at delta and kappa; produces less analgesia than morphine; used as analgesic, anti-tussive, and antidiarrheal; can cause constipation but resp depression is rarely a problem |
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Definition
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Term
| D-isomer of codeine analog but no activity at opioid Rs; NMDA R antagonist but also binds at other undetermined sites; used as anti-tussive; relatively safe at prescribed doses; OD: tachycardia, agitation, psychosis, seizure, ataxia, coma |
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Definition
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Term
| used for acute and chronic pain; active at all receptors but mostly mu; available in formulation w/ acetaminophen or NSAIDs and in slow-release; concern for abuse through injecting ground-up tablets |
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Definition
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Term
| antagonizes opioid action; used for opioid OD; given IV; formulated w/ buprenorphine and pentazocine to prevent abuse; watch for relapse due to short duration of action |
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Definition
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Term
| antagonizes opioid action; give PO; long duration of action; reduces craving for alcohol in alcoholics; need much higher dosage to reverse buprenorphine OD |
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Definition
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Term
| orally active w/ many metabolites; weak MOR agonist; inhibits NE and serotonin reuptake; activates alpha adrenergic Rs; used for mild to moderate pain; has low risk of resp depression and abuse but associated w/ seizures and serotonin syndrome |
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Definition
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Term
| rapidly acting anticoagulant; accelerates antithrombin 3 rxns; used for DVT, PE, acute arterial occlusion, a-fib, and prophylaxis (use lower doses); administered IV or intermittent injections; complications: bleeding, thrombocytopenia; closely monitor pts w/ high bleeding risk; potential allergy risk due to porcine source |
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Definition
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Term
| depolymerized heparin; limited approvals for hip and knee replacements; greater bioavailability subQ; longer half-life; does not require monitoring; contraindicated in pts w/ HIT |
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Definition
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Term
| prevention of DVT in ortho pts and for tx of DVT and PE; synthetic polysaccharide; administered subQ; much less thrombocytopenia; contraindicated in renal dysfunction |
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Definition
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Term
| polycationic protein that forms stable complex w/ heparin; rapidly reverses effects of heparin |
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Definition
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Term
| acts by inhibiting synthesis of factors 2, 7, 9, and 10 by blocking Vit. K epoxide reductase; slow onset of action; good for prophylaxis and treatment; complications: hemorrhage (requires close monitoring when starting and w/ heparin co-administration); drug-drug interactions by CYP; causes necrosis in pts w/ Protein C deficiency; never use in pregnancy and situations where hemorrhage potential is greater than clinical benefits; avoid use in uncontrolled alcohol/drug abuse or unsupervised dementia/psychosis |
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Definition
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Term
| recombinant protein almost identical to natural peptide; IV administration; cleared renally; used in HIT; Abs may develop |
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Definition
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Term
| recombinant; subQ bid; prophylactic for post-op DVT in hip replacement |
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Definition
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Term
| 20 AA analog which is reversible inhibitor of thrombin R; IV administration for percutaneous coronary intervention for pts at risk of HIT |
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Definition
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Term
| small molecule inhibitor of thrombin R; IV administration; metabolized in liver so OK FOR USE IN RENAL PTS; useful in HIT |
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Definition
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Term
| first orally available DTI; indicated for stroke prevention in non-valvular a-fib; cleared by renal excretion; used in knee replacement |
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Definition
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Term
| HAVE NO KNOWN ANTIDOTE TO ACTION |
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Definition
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Term
| phosphodiesterase and adenose reuptake inhibitor; prevents degradation of cAMP to AMP and ultimately platelet activation; complication: HA |
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Definition
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Term
| chimeric monoclonal Ab directed against human GP2b-GP3a; blocks receptor for fibrinogen; adjunct tx for MI prevention in stenting or angioplasty; not for use in pts w/ abnormal bleeding |
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Definition
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Term
| synthetic peptide that blocks GP2b-GP3a in a reversible manner; used as adjunct tx to prevent MI in several scenarios; IV admin; short half-life and action (4-24hrs); NOT FOR USE W/ RENAL DYSFUNCTION |
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Definition
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Term
| nonpeptide tyrosine analog; specific to GP2b-GP3a and blocks fibrinogen binding; NOT FOR USE W/ HEPATIC DYSFUNCTION |
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Definition
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Term
| first generation drug of class; restricted to tx of acute cerebral ischemia; antiplatelet action through ADP-R; adjunct tx to prevent stenting thrombosis; oral admin.; higher incidence of neutropenia/agranulocytosis |
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Definition
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Term
| better tolerated; administered to pts w/ atherosclerotic vascular dx; prevention of MI in pts who cannot tolerate aspirin; contraindications: current pathological bleeding, CABG, prior TIA or stroke |
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Definition
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Term
| more potent ADP-R inhibitor; increased risk of bleeding; oral admin. |
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Definition
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Term
| isolated from beta-hemolytic bacteria; activates tissue plasminogen; requires large loading dose; allergic rxn can occur; overwhelms homeostatic inhibitory controls; do not use w/ suspicion of intracranial bleed or recent heparin use |
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Definition
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Term
| recombinant t-PA; binds to fresh thrombi; poor activator of plasminogen in absence of fibrin-binding; increases conversion of plasminogen to plasmin |
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Definition
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Term
| lysine analog; inhibitor of plasmin; treats toxicity/OD of streptokinase and alteplase |
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Definition
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