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Stimulates all opioid receptors, used in severe pain; more effective IV; short half life; duration 4-6 hours; metabolized by CYP2D6 |
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Strong analgesic that acts on all opioid receptors; effective for severe pain; more potent than morphine |
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Stimulates mu receptors; long half-life; Maintenance tx of addicts |
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Mu agonist that causes euphoria; short-acting drug; metabolites cause seizures, so can't use in high doses or for long term; NO cough suppression; anticholinergic; less constipation, urinary retention; serotonin syndrome with MAOIs |
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Opioid that is lipid soluble and highly potent; short duration of action and half-life; HIGH abuse potential; used in short surgical procedures; can cause truncal rigidity if given rapidly IV; transdermal patches or lollipops; metabolized by CYP |
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Opioid Schedule 1 drug; very potent and gets into brain well; commonly abused; prodrug for morphine |
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Opioid prodrug used for moderate to severe pain; combined with acetaminophen; short half-life |
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Opioid used for moderate to severe pain; used also for Tourette's and restless leg syndrome; metabolized by CYP |
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Opioid used for moderate pain; also a cough suppressant; metabolized by CYP |
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Kappa receptor agonist; Mu receptor partial agonist; used for moderate pain; less sedating than other opioids; may cause dysphoria; low abuse potential |
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Partial agonist on mu receptors; ceiling effect, not much euphoria; absorbed from buccal mucosa; combined with naloxone, injected won't work |
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Oxycodone combined with acetaminophen |
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Weak mu agonist; inhibits NE/5-TH reuptake; causes seizures when combined with antidepressants, serotonin syndrome; low abuse potential |
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Mu receptor agonist, inhibits NE reuptake, stimulates a2 receptors; used for moderate to severe pain; also for neuropathic pain; schedule II |
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NO effect on mu receptors; only cough suppressant; Blocks NMDA receptors, which means abuse potential; decreases 5-HT uptake; cough syrup abuse in teenages, causes death |
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Opioid antagonist that is only injected; short acting |
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Oxycodone combined with aspirin |
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Opioid antagonist that is long-acting; will precipitate withdrawal; has liver toxicity; treatment of opioid addicts |
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Methylnaltrexone, Alvimopan |
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Definition
Opioid antagonists that are peripherally acting used for treatment of opioid induced constipation; DO NOT reverse centrally-mediated analgesia, respiratory depression; one is IV, the second oral |
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Analgesic gas not very soluble in the blood with a rapid induction; very potent and used in most anesthesia mixtures to speed induction; does not cause malignant hyperthermia; causes euphoria, relaxation, warmth |
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Potent slow induction inhaled anesthetic; not used very much any more; causes ventilatory depression and bronchodilates; inhibits gag reflex and cough reflex; sensitizes the heart to catecholamines, causes arrhythmias; can cause HEPATITIS; can cause malignant hyperthermia, tx with ? |
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Anesthetic gas that is faster than halothane; no heart changes, but can cause seizures; metabolism can cause fluoride and renal toxicity; not used very much |
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Potent inhaled anesthetic; very non-toxic; rapid induction and recovery, but bad taste so used only for perpetuation; decreases BP and increases HR; used in neurosurgery; potentiates neuromuscular blocking agents |
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Inhaled anesthetic that has rapid induction and recovery; low airway irritation and low toxicity; used in children; safest in CV disease |
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Very fast induction inhaled anesthetic; irritating to airway, don't use for induction; decreases BP and increases HR; causes respiratory depression and increases ICP; low toxicity |
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Short acting barbituate used in induction of anesthesia; CI for porphyria; little analgesia; severe respiratory depression |
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The perfect anesthetic; may facilitate GABA; fast acting and quick recovery IV, used for maintenance of anesthesia, can be used for short or long surgeries; causes some respiratory depression (don't necessarily have to ventilate the patient); anaphylaxis biggest side effect due to albumin in emulsion; lidocaine added to decrease pain on injection site |
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Fast acting IV anesthetic used for fast onset of action and short duration; causes hiccups, hypotension; can exacerbate seizures |
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Causes dissociative anesthesia and potent analgesic; binds to PCP site on NMDA receptor; increases HR and BP; causes emergence delirium in adults, tx with benzos; little N/V; used in vet med and children; drug of abuse (teens like drugs that act on NMDA receptors) |
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Increases release of DA; used to treat narcolepsy, ADHD; causes alertness, euphoria, excitement, appetite suppression; aggression, paranoia, delusions; increases BP Withdrawal is fatigue, increased appetite |
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Increases release of DA and NE in basal ganglia; may produce amphetamine psychosis Chronic use may cause neurotoxic damage, personality changes Intense craving, severe withdrawal Cardiac toxicity; weight loss, whiter skin, dental problems, seizures, stroke, organ damage, lack hygiene, bugs cause them to scratch and have open sores |
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CNS stimulant that inhibits DA and NE reuptake; ingredient in Coca-cola until 1903; CNS stimulation to cause alertness, euphoria, anxiety, hyperactivity; severe craving Can be used medically as a local anesthetic, vasoconstrictor Causes tachycardia, vasoconstriction, HTN, bronchodilation, increased body temp, dilated pupils Crack kind inhaled rapidly absorbed, very fast onset; crack babies retarded growth, stillbirths Chronic use causes reduction in overall brain activity; anxiety, insomnia, paranoia, hallucinations Bugs they try to get out Overdose causes Vtach, fibrillation; stroke, seizures Bromocriptine decreases craving |
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Activates nicotinic receptors in CNS and periphery; increases 5-HT and DA release; CNS increased arousal, appetite suppression Short half life Very reinforcing and highly addictive Bupropion used to decrease craving |
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Increases 5-HT activity by blocking reuptake and stimulating 5-HT receptors Produces feelings of peacefulness, empathy, closeness, trust; may be followed by confusion, depression, anxiety, paranoia Increases BP, HR; causes hyperthermia, dehydration, kidney failure Persistent memory loss may occur Decreased cerebral blood flow |
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Binds to presynaptic cannabinoid receptors; inhibits release of glutamate and ACh Quickly absorbed, lipophilic, which means stored in fat and long half life Mild euphoria, well being, altered sense of time, tranquility NO physical dependence; psychological dependence possible Decreased memory over time, amotivational syndrome, decreased testosterone and sperm production in males LBW, fetal malformations Medical uses: bronchodilation, antiemetic, appetite stimulation (Dronabinol), analgesia, decreased spasticity/ataxia/muscle weakness, decreased intraocular pressure Bath Salts synthetic cannabinoid receptor agonists; psychoactive effects |
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LDS, mescaline (mushrooms), psilocybin (peyote) |
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Acts on 5-HT receptors in brain Euphoria, visual hallucinations that last hours Bad trips and flashbacks Synesthesia--one sensory modality assumes characteristics of another NO dependence because they don't stimulate DA pathways |
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NMDA receptor antagonists used as general dissociative anesthetics Sensation of dissociation or floating Can produce psychosis, treat with haloperidol Analgesia accompanied by aggression, dangerous combination Increases BP |
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Ester-type local anesthetic; short-acting, used around URT; inhibits Na channels, and secondarily can increase DA and NE in the CNS; Schedule II |
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Ester-type local anesthetic; very lipophilic and pKa of 3.5, always in non-ionized form Used topically only to treat sunburn, minor burns, pruritis Risk of methemoglobinemia |
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First synthetic local anesthetic; ester-type; metabolized by pseudocholinesterases Short duration of action Metabolic product PABA inhibits sulfa drugs Used for infiltration anesthesia and diagnostic nerve blocks Minimal toxicity |
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Ester-type local anesthetic; slow onset of action; 10X stronger than procaine; causes severe toxicity in peripheral blocks Used in spinal and ophthalmological procedures |
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First amide-type local anesthetic; metabolized in liver by CYP Wide range of uses; perferred for infiltration blocks and epidural anesthesia Rapid onset Risk of TNS in spinal blocks Greater potency and duration than procaine |
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Amide-type local anesthetic; long duration of action; used for spinal and epidural anesthesia, infiltration blocks Greater cardiotoxicity than other amides More potent sensory than motor block, so better for labor in pregnancy |
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Amide-type local anesthetic; long-acting; enantiomer of bupivicaine Less lipid soluble, cleared more rapidly than bupivicane Metabolized by CYP Used for peripheral and epidural blocks Vasoconstricts at clinical doses |
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Amide-type local anesthetic; intermediate duration of action Highest rate of clearance of amides Methemoglobinemia due to metabolites Give methyl blue to treat CI in cardiac and respiratory diseases Limited to dental anesthetic |
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Amide-type local anesthetic; intermediate duration Not used in labor or topically, just peripheral |
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Amide-type local anesthetic; NOT used in US Toxic "" Number Test: measure of butyrylcholinesterase activity |
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Amide-type local anesthetic; long duration of action Rarely used Inverse differential block, motor before sensory block |
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Prostaglandin drug used for abortions, facilitating labor and treating dysmenorrhea; causes vasodilation, bronchial relaxation, and activates GI; initiates uterine contractions; can cause fever and facilitate bone resorption |
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Prostaglandin drug given by injection for tx of ED; can cause penile pain and priapism; also used in peds to keep ductus arteriosus open before surgery; causes vasodilation by decreasing intracellular Ca, bronchial muscle relaxation, activates GI, relaxes SM in corpus cavernosum, produces fever and facilitates bone resorption |
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Prostacyclin (Epoprostenol) |
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Prostaglandin drug used to relieve primary pulmonary HTN |
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Analog of prostaglandin F2a; increases resorption of aqueous humor; topical, one drop in the evening; can cause blurred vision, conjunctival hyperemia, irritation |
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Zileuton and Zafirlukast and Montelukast |
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Definition
LT receptor inhibitors that are used to treat asthma |
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PGE1 analog used to reduce gastric acid secretion in ulcers |
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Aspirin (acetasalycilic acid) |
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Nonselective, irreversible inhibitor of COX-1 and COX-2; causes analgesia, antipyretic, anti-inflammatory by inhibiting synthesis of factors involved in chronic inflammation and platelet effects; analgesia due to peripheral and CNS effects in hypothalamic area, also prevents sensitization of pain receptors to stimuli; lowers body temp only in situations where elevated body temp is due to conditions that raise the hypothalamic thermostat Fast oral absorption, slowly crosses BBB; rapidly hydrolyzed in plasma; competes with other drugs for plasma protein binding sites High doses metabolized by zero order kinetics Alkalinization of urine promotes excretion |
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Selective reversible COX-2 inhibitors; less GI adverse effects and platelet aggregation Increased risk of CV disease CI in GI disease, asthma, breast feeding, pregnancy, renal failure |
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Reduces PMNs, inhibits phospholipase A COX inhibitor Worst side effects because very potent |
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Potent COX inhibitor; decreased AA bioavailability; mostly GI side effects |
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COX inhibitor that can be used in postsurgical pain; can't be used for more than 5 days or see gastric ulcerations |
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COX inhibitor suitable for long term treatment Longest half life, best for fewer daily doses |
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COX inhibitor NSAID; recognize the name |
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Prodrug COX inhibitor Long half life |
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Very potent NSAID, produces a lot of GI sxs; not marketed |
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NOT inhibitor of peripheral COX enzyme; unknown mechanism of analgesia; NOT anti-inflammatory or anti-rheumatic Antipyretic and analgesic only Overdose causes fatal hepatic necrosis Hepatotoxicity can progress to encephalopathy and death Requires only 25 grams |
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Inhibition of phagocytosis; used to treat rheumatoid arthritis; decreases immune functions of macrophages because they eat this drug Causes bone marrow damage, enterocolitis |
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Used for rheumatoid disease and Wilson's disease; may be as effective as gold |
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Antihistaminic, anticholinesterase, antiprotease properties; used to treat rheumatoid disease |
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Used to treat RA and IBD; better tolerated, equally effective to gold |
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Antibody against TNF-a; used for Crohn's and RA; must be given IV |
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Antibody that is chimeric; binds to CD20; treats lymphoma and leukemia |
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Antibody against TNF-a; used to treat RA; 100% human peptide sequence |
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Fusion protein made by DNA technology; fake TNF-a receptor to inhibit TNF-a activity Administered subQ |
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Fully human fusion protein that competes with CD28 for APC binding; used to treat RA |
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Inhibits dihydroorotate dehydrogenase, used in de novo pyrimadine synthesis; inhibits induction of COX-2 Leukocytes pyrimidine 90% comes from de novo pathway, so inhibits leukocytes, but not other cells (which only use de novo pathway for 10%) |
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Inhibits lymphocyte purine synthesis; used to treat RA Prodrug GIven orally or IV |
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Interleukin-1 receptor antagonist; recombinant Used to treat RA Given subQ |
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Binds tubulin to inhibit assembly of microtubules; anti-inflammatory by inhibiting migration of PMNs Used in gout for acute attacks NO analgesic effect Effective 12-24 hours Side effects diarrhea |
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Uricosuric agent Maintain large urine volume to avoid kidney stone formation Give prophylactic colchicine to avoid initial gouty attack Decreases excretion of acidic compounds or metabolites |
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Inhibit xanthine oxidase Effective in primary and secondary gout Serious vasculitis, agranulocytosis and hypersensitivity reactions May provoke initial gouty attack Interacts with aluminum hydroxide, which decreases its absorption Increases effect of mercaptopurines, cyclophosphamide Inhibits elimination of chlorpropamide Inhibits metabolism of warfarin, probenecid Inhibits activation of fluorouracil |
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Urate oxidase found in fungi Converts uric acid to allantoin, which is highly soluble and eliminated Foreign protein, high antigenic so only useable once Used mostly in children |
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5-HT receptor agonist Decreases vasodilation of cerebral arteries If HA recurs, repeat dose Expensive Side effects of vasoconstriction CI pregnancy, tobacco smoking |
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Stimulates alpha-1 vasoconstriction and agonist of 5-HT receptors Most effective, specific for migraines More vasoconstriction than triptans |
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