Pharm: Exam1 (wk 2 and wk 3 Pwrpts)

______ of pt visits in US result in perscriptions
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Terms in this set (144)
the dose that 50% of the pop experience adverse effectsmedian toxic dose (TD50)the dose that 50% of the animals tested diedMedian lethal dose (LD50)therapeutic index def and equationsindicate the drugs overall safety based on how high the number is; TI = TD50/ ED50when a drug has a small window in which it is effective and toxicNarrow therapeutic indexwhere do most drugs come fromsynthetic sourcesHow many in human trials4what is phase1 of human trialshealthy volunteers are studied to determine the drug safetywhat is phase2 of human trialssmall groups of pts are studied to determine effective dose range and is usually around 100what is phase3 of huan trialslarge human trial to determine the safety and efficacy in large pop sample sizewhat is phase 4 of human trialspost marketing drug surveillance for safety and efficacy; after drug already approved2 primary concerns of the FDA are...1. whether the drug is effective in treating certain conditions 2. whether the drug is reasonably safe for human usewhat is the generic name derived fromchemical namepercentage of errors in meds that are confusion on names25%what are 2 things in dosing and drug names you don t not usetrailing zeros and abbreviationsactonepotassium sparing diureticasethrombolyticazoleantifungalcainelocal anestheticcef/cephcephalosporin antibioticcillinpenicillin antibioticcort/olone.sonecorticosteroidscyclinetetracycline antibioticdipinecalum channel blockerololbeta blockerprazoleproton pump inhibitorprilace inhibitorprofenNSAIDsartanantiotensin 2 receptor blockeremideloop diureticsetronserotonin receptor bllockersatinHMG- CoA reductase inhibitorterolbeta agonistvirantiviralzepam/ zolambenzodiazepinebioequilvalent defwhen two drugs have the same active ingredients, same admin route and same pharmacokinetic profile as well as same drug typein order for FDA to pass a generic drug______ must be provedbioequivalencewhat 4 points must be proved in proving bioequivalencepharmaceutically equivalent; therapeutically bioequivalent; same conditions of use (indications); same labelinghaving an _______ allows generic drugs to be marketedAPI (active pharmaceutical ingredient)Bioavailibilitythe extent of amount to which the drug reaches the systemic circulationbioavailibility depends onthe drugs ability to cross membrane barriers and drug interactionsnearly 90% of bioeqiuvalence studies conducted during a 12 year period demonstrated a _____ % difference btw generic and name brandsless then 10what is the name of the groupings that tell how addictive a drug is and how does it workschedules; as number increases there is a decrease in risk for abusewhat does LADME stand forliberation, absoprtion, distribution, metabolism, and excretionLiberationrelease of a drug from its dosage form; only in solid dosage formsabsorptionrate at which a drug leaves it sit of admin and the extent to which this occursreceptors theoryexplains the actions of drugs that have a direct and reversible effect; proteins commonlyagoniststimulatory ; mimics endogenous compoundantagonistdrug inactive but it inhibits the action of the agonisttwo pathways drugs can be admin and their defalimentary -via digestive system non-alimentary- no digestive systemoral drug admin is the _______ but can lead to ______safest; GI irritationoral drug absorption occurs in the____ and bc of this must have a high degree of ____small intestine; lipid solubilityFirst pass effectoral meds are first transported to the liver and metabolized there before reaching target tissue, so must have high enough dose the liver is saturated and the drug can then reach target tissuewhat route of application is used for vomiting pt or unconscious ptrectalsublinguals how are they administeredplaced under the tonguehow is buccal meds takenplaced btw the cheek and gumsbuccal and sublingual meds are absorbed into___ and avoid______venous circulation; first pass metabolism2 limitations to inhaled meds1. difficulty regulating the dose 2. there is a proper techniquewith transdermal med do you want the drug to degrade in the dermis at allnowhat is a benefit of intramus meds v IVintramus does not have the increase in plasma levels that the IV doesWhat is the benefit of intramus meds v IVintramus will take longer to absorb and some of the med will be lost before it gets to the bloodwhich other method is subcutaneous similar tointramuswhere is intrathecal admin tothe spinal subarachnoid spaceVd=______/_______; stand foramount of drug admin/ concentration of drug in plasma; volume of distributionpassive distributionthe movement of substance either into or out of a cell down a concentration gradient without energyactive transport; and 3 characteristicsinvolves using membrane proteins to transport substances across he membrane; carrier specificity, expenditure of energy, ability to transport across a gradient4 factors affecting drug distributiontissue perm, blood flow, binding to plasma proteins, and binding to subcellular componentswhere can drugs be stored and what do they holdadipose- lipid soluble drugs bone- metals mus- organs-prodrug defa drug introed in an inactive form that becomes active when metabolized by enzymessites of drug metabolismliver (most common), kidney, lung, GI, skinenzyme inductionrepeated exposure leads to the body being able to better metabolize a drugwhat are the phase 1 drug metabolismsoxidation, reduction, hydrolysiswhat is the phase 2 metabolismconjugationoxidation defadding of O or sub of Hreduction defremoving O or adding Hhydrolysisoriginal compound is broken into separate partsconjugationsdrug is coupled to a endogenous compoundwhat is the functional unit of the kidneynephronwhat is the only compund tro be excreted from the kidneyspolar(hydrophilic)2 primary measures of drug elimination ratesClearance and half lifeclearance def; equationcan be organ clearance or system clearance; CL=Q (amt of bld passing through organ) [{Ci(drug in)-Co(drug out)}/ Ci]steady state concentrationthe point at which the elimination equals the rate of drug availability (3-5 half lives)what influences the amount or extent of drug absorptionsformation of insoluble salts; change in GI pHdrugs that increase metabolismenzyme inducersdrugs that decrease metabolismenzyme inhibitorswhat are analgesics used for; and the 2 categoriespaint treatment; nonopoid analgesics and opiod analgesicsopiod analgesics primary characteristic and exertionrelieve moderate to severe pain; CNSwhere do opioid analgesics secondarily actbrain and peripheral tissueswhat are the 3 types of endogenous opioid peptideendorphins, enkephalins, dynorphins3 primary classes of opioid receptors most aggressive to leastMU, Kappa, Delta4 classes of opioid agentsstrong agonists, mild to mod agonists, mixed agonists-antagonists, antagonistsagonists treat _____ pain and bind to ______ receptors; exsevere; mu opioid; morphine, fentanylmild to mod agonists treat ______ pain due to there afinity for ________; exmoderate ; CNS based opioid receptors; codeine, oxycodonemixed agonists-antagonists deliver ________ to divergent charactristics, so ____ is happening while _____ of another receptorat the same time; binding; inhibitionantagonists ___ opioid receptors with increase ____ for _______block all; affinity; me receptorsantagonists are used to treatoverdose and addictionopioids act at the spinal cord toinhibit painful impulses from being sent from the periphery tot he brain at the interneuronwhere are opioid receptors locateddistal end of the primary afferent neuronsG proteins defproteins that bind with guanin necleotides and reg cell activity and they link surface receptors to ion cannels or intracellular enzymeswhy is opioid analgesia uniqueit alter the perception of pain not eliminates itwhy are opioids used for the GI systemto slow bowel mobilityadverse effects of opioidsaddiction, tolerance, physical dependence, hyperalgesiadownreg causes endocytosis of_____ resulting in a loss of communication with_______opioid receptors; G proteins that transit info to interior of cellwhat is the first sign the opioid tolerance shows, when is it reversed, and how long does it last2-3wks, 2 wks, 1-2 wkshow long does withdrawl take to set in and when does it peak6-10hrs, 2/3 daywhat is one of the most addictive opioids and what is used to treat itheroin, methadone (milder withdrawl)NSAID effectsdecreases inflam reliece mild to mod pain decrease body temp decrease blood clotting by inhibiting plateletsEisosanoids refer toprostoglandins, thromboxanes, leukotrieneseicosanoids are made of ___-carbon fatty acid derivative and can be metabolized by _____ _____ systems20; several enzyme;prostoglandins poduced when _______ ______ suggesting they have a ____ rolecells damaged; protectiveprostoglandins promote____ by changing the _____ at the hypothalamusfever, set-point,prostoglandins increase the ___ of pain receptors and causes _____ ______sensitivty, platelet aggregationNSAIDS inhibit_____ and _____ synthesis by inhibiting_______ enzymeprostaglandin and thromboxane; cyclooxygenase (cox)cox 1 enzymesreg normal cell activity and maintain cellular homeostasiscox2 enzymesproduced primarily in injured cell which moderate pain and increase cappillary permhow are NSAIDS classifiedif they effect both COX enzymes or are speciic to COX 2 enzymesNon selective NSAIDS inhibitcox 1 enzymes; prostoglandinswhy is NSAIDS not given to childrencan cause reye syndrome - swelling of brain or liver that is often not caughtadverse effects of NSAIDSCI damage, Cardio probs (bc increase BP w/ cox 2 specific NSAIDS), liver pt be precautiousprostaglandins are _____ and help reg vascular tonevasoactive, relax it and inhibit thrombus formationa nonselective NSAID will result in balance btw...vasodilation and vasoconstrictioncelecoxibcox 2 inhibitorDiclofenaccox2 isoenzyme affinity that is more potent then most NSAIDSEtoldolaccox 2; analgesic, fewer side effects and GI sparringketorolacsimilar potenct to opioidsmeloxicamvery selective cox 2; fewer GI probspiroxicam45 hr half life which is taken once daily, good for active people and people with lots of medsnaproxensimilar to ibuprofen in performance and adverse reactionssulindacrenal sparing med but can produce more side effects on the GI then aspirinacetaminophen is a ....centrally acting analgesic and antiphyretic, not antiinflam, anticoag, and doesnt cause GI probsacetaminphen inhibitscox 3 (CNS prostaglandins) and cox 2(some but not fully understood)acetaminophen treat (2) and is bad formild to mod pain and fever; liver80-90% is bound to ____ while 10-20 is _____ the bodyplasma proteins; distributed throughout (what has the effect)acetaminophen and NSAIDS have...little effect on therapy except to modulate mild to moderate painthe newer NSAIDS inhibit _____ but still leave.....COX 2, beneficial prostoglandins that protect stomach and organs