1. a1receptor

arterioles, veins, glands, eye, intestine,myocardiumvasoconstriction, decreased glandular secretion,constriction of radial muscle, decreased motility

2. a2receptor

CNS post and post synaptic terminals - b islet cellsin pancreas, larger vessels, skin, mucosa, kidneydecreased sympathetic outflow from brain,decreased NE release, decreased islet cellsecretion

3. aa of each4. ACh stored in storage vesicles. Ca release causes

vesicles to fuse with the plasma membrane andrelease ACh. diffuses through synaptic cleft andmay bind to nicotinic receptors on muscle cells ormuscarinic receptors on ganglionic synapses ofthe ANSrapidly hydrolyzed in the synaptic cleft

5. AC PC before meals, after meals.6. active

transportenergy and transport carrier needed - ATPactivity is necessary to transport a drug against aconcentration gradient in these cases

7. Additiveeffects

response elicited by combined drugs is EQUAL tothe combined response of the individual drugs -linear - two drugs where each has CNSdepressants - antidepressants and alcohol

8. AdjustedBodyWeightequation

ideal body weight + 0.4(actual body weight - idealbody weight)

9. AdverseDrugEvents

injuries resulting from medication use includingphysical harm, mental harm, or loss of function.ADE's (compared to medication errors) are a moredirect measure of patient harm

10. AdverseDrugReaction

Any response to a drug which is noxious andunintended, and which occurs at doeses normallyused in man for prophylaxisis, diagnosis, ortherapy of a disease, or for the modification ofphysiological function. Becomes an ADE if theresinjury

11. Agonists change cellular physiology by binding tointracellular receptors or plasma membranes -must be present at more than one binding site fora significant change to occur. weak agonist must bind to many more receptorsto produce the same effect as a strong agonistmixed - fails to produce maximal effects evenwhen all of the receptors are occupied by thepartial agonist

12. Alphareceptors

present in the neurons in the vascular smoothmuscle - a1 in the myocardium, a2 in largerblood vessels (skin mucosa, gut, kidney).arteriolar vasoconstriction

13. Alteredabsorption

When a combination of two or more drugsimpedes or inhibits the absorption of one ormore of the drugs being taken/administered.Drugs may inhibit absorption of other drugsacross physiological membranesantibiotics - take on an empty stomach and notwith anacids

14. Alteredexcretion

drugs may act on the kidneys to reduce orenhance excretion of specific drugs-adding mannitol to cisplatinum therapyminimizes renal tubular damage - the diureticeffect of mannitol prevents prolongedcisplatinum time and contact with the renaltubes

-probenecid inhibits active tubular secretion ofpenicilillin

15. Alteredmetabolism

interactions can occur when P450 enzymes areinhibited or induced

16. anabolic conserves energy, decreases heart rate,stimulates GI function, rest and digest, PNSpredominates

17. Antagonism durg inhibits the effect of another drug. Naloxone and morphine (narcan)cardiovascular and respiratory depression willbe reversed

18. ATC around the clock19. B1 receptor heart: myocardial tissue and conduction system

increased HR, increased contractility, increasedconduction velocity, increased automaticity

20. B2receptors

trachea, broncioles, bronchi, uterus, arterioles(except brain and skin), veins, vascular smoothmuscle, livertracheal/bronchial relaxation, uterinerelaxation, circulatory dilation

21. best passthroughplasmamembranes

lipid soluble drugs that are composed ofsmaller molecules which are not ionized

22. BetaReceptors

b1 in myocardial tissue which leads toincreased cardiac contractility and heart rate.B3 located in vascular smooth muscle tissues inthe bronchi and liver. stiumulation leads tocoronary and peripheral vasodilation andbronchodilation

23. BID two times a day

Pharmacology Exam 1Study online at quizlet.com/_11d3nv

24. carrierassisteddiffusion

noncovalent binding of drugs to carrierswhich facilitate diffusion.

25. catabolic extends energy - increases HR, dilatesbronchi, decreases secretions, Fight or Flight,increase tissue oxygenation and cardiacoutput, SNS predominates

26. categories ofpregnancyrisk factors

A: no risk to fetus B: no risk in animal studies but no humanstudies or animal studies are bad buthuman studies are fineC: adverse animal studies and no controlledstudies for women or studies in women andanimals are not available. weigh risks vbenefitsD: positive evidence of human fetal risk butbenefits are worth it (life threateningsituation)X: risk in pregnant women totally outweighsany benefit. kids and animals are deformed.drug is totally contradicted

27. CC with meals28. Chelation aluminum, magnesium, calcium, iron

containing medications can irreversibly bindto antibiotics like doxycycline or oralantibiotic thereby reducing the amount ofdrug absorbed

29. Clinicallysignificantdruginteractions

more likely to occur between substrates andeither inhibitors or inducers of the same CYPenzyme

30. ClinicalPharmacology

effects of drugs on physiologic systems andor patients

31. Competitionfor serumproteinbinding

drugs that bind to serum proteins maycompete with other drugs for the proteinbinding sites. Displacement of drug A fromserum proteins by drug B may increase theconcentration of unbound drug A in theserum

if serum albumin levels are significantlydecreased the amount of free drug will beincreased

32. competitveantagonism

antagonist competes with agonists forreceptor sites. high doses of agonist canovercome antagonism

33. continuousinfusion

the serum concentration of the drug willreach steady state after 4 to 5 half lives.increasing the rate of infusion will increasethe serum concentration of the drug, but willnot shorten the time needed to achievesteady state levels

34. Creatinineclearancecalculation

Males = (140-age) x body weight in kg/72xreported SCr

Females = CrCl for males x 0.85

less than 30 is super bad! adjust for anythingless than 50

35. CYP3A4Inducers

carbamazepinephenobarbitalphenytoinrifampin

increase metabolic rate, serum drug levelsdecrease

36. CYP3A4Inhibitors

ketoconazoleerthyromycingrapefruit juiceritonavir

decrease metabolic rate, drug level increases37. CYP3A4

Substratesnifedipineerythromycinmidazolamtestosterone

38. CYPenzymes areinvolved inthemetabolismof whatpercentageof drugs

75% of all drugs

39. CYPInduction

occurs in response to the presence of achemical which is metabolized by P450 - moreenzyme is produced to handle the chemicalload. Once the enzyme is induced, it willmetabolize the inducing agent more rapidly.inducers are drugs that induce the productionof one or more CYP enzymes.Other drugs metabolized by the enzyme willalso metabolize more quickly.

40. CYPinhibition

CYP inhibitor drug competitvely binds to theactive site on the enzyme, preventing thenormal enzyme bindnig and routinemetabolism from occuring. Inhibitors are drugs which inhibit one or moreCYP enzymes

41. cytochromeP450

liver microsomal drug oxidation/reductionsystem is responsible for the metabolism ofmany drugs. isoenzymes are located in the ERof hepatocytes, gastric mucosa, and elsewhere.ETC uses NADPH as a proton carrier, a drugbound the cytocrome p450 can beoxidized/reduced

42. DC discontinue43. Diagnostic

drugsused to aid in examination, evaluation, anddiagnosis of the patient or a patient condition- contrast media, adenosine, fluorescein

44. Dissociationconstant (Kd)

describes the degree of a drugs affinity forthe receptor site - concentration of drug insolution necessary for 50% of given receptorsto be occupied

45. Distributionhalf life

decrease in the drug serum concentration ofthe drug as it is distributed through the body

46. Do notabbreviate

U - units, micrograms, QD, QOD, SC, Trailingzero or lack of leading zero. TIW - three timesof week, D/C - discharge. HS - half strength.cc- cubic centimeters. MS MSO4 MgSO4.

47. dopamine postganglionic sympathetic transmitter inrenal blood vessels

48. dopaminergicreceptors

mainly in the renal and mesentericvasculature, lead to different responsesbased on degree of stimulation.

49. Drug substance intended for use in the diagnosis,cure, mitigation, treatment, or prevention of adisease.other than food that is intended to affect thestructure or any function of the body

50. Drugabsorption

transfer of drug from its site of administrationto the bloodstream.

51. Drugabsorptionfor topicalophthalmicmedications

membranes are lipophilic so highly watersoluble drugs do not generally pass well.ionization makes a drug less lipid soluble.

52. drug bindingto receptorsites causes

1. activation of cellular function (DNAtranscription, steroid production, stimulationof RBC production)2. inhibition of cellular fxn (inhibition ofprotein synthesis, inhibition of DNAsynthesis)3. activation of biochemical processes (cAMP,Ca, etc which transduce a signal stimulatedby a drug)4. opening or closing of ionic channels(stimulation/inhibition of Na or K channels)

53. drugdeposition

some drugs can deposit in specific tissuesand accumulate there which may result inslower drug release or eventual changes inthe tissues.amiodarone - optic neuritis and can depositin cornea (heart med)doxycycline - localize in specific organs andtissues including bone, liver, spleen andteeth

54. Drugdistribution

process by which a drug leaves the bloodstream and enters the extracellular fluid andthen the cells of the tissues.

55. drug efficacy degree to which a drug is able to inducemaximal effects. used to compare drugs withdifferent mechanisms of action

56. drug factorsthat affectabsorptionthroughtissues andmembranes

formulation, molecular weight, ionizatio,solubility.absence or presence of food in the stomach,changes in concentration of stomach acidity,peristaltic activity, degree of blood flowin/around the GI tract topical drugs: skin thickness, location,available circulation.

57. drugformulationdepends on:

capability of the drug to pass through body'sbarriers (oral must pass through GI wallsand blood vessel walls)intended use of the drug (setting - hospital voptometrist)clinical situation (urgency)first pass effect

58. drugidiosyncracy

unusual or unexpected response to a drug(allergy, etc)

59. drugmonograph

drug name, pharmacologic category, use,pregnancy and lactation info, safety,mechanism, dynamics/kinetics,contraindications, warnings andprecautions, adverse reactions, druginteractions, dosage, administration, storage,forms

60. drug potency amount of drug required to produce 50% ofthe maximal response that the drug iscapable of inducing. used to compare drugsin the same class

61. Drug stability more than just the expiration date - howstable in different dosage forms, stability indifferent physiological environments(different PH, steam from shower, etc)drugs like insulin arent effective orallybecause they are denatured by stomach'sPH

62. Duration ofaction

the period of time in which the concentrationof the drug is in the therapeutic range andthe desired clinical effects of the drug areevident. half life, drug metabolism, andexcretion are related

63. effectiveconcentration

concentration of a drug which induces aspecified clinical effect in 50% of the subjectsto whom the drug is administered.

64. Elimination halflife

decrease in drug serum concentrationas the result of metabolic and excretionprocesses - unique for elimination halflife to exceed distribution half life.

65. Factors that affectdrug distribution

permeability of tissues/membranes -propofol - rapid and extensivelydistributed in body and quickly crossesblood brain barrier. trop - rapidlyabsorbed through the cornea to blockthe sphincter

serum protein binding - when drugsbind to albumin or other serum proteinsthe amount of free unbound drug isreduced. protein bound drugs canreach higher concentrations betweenthe blood and tissues - decreased freeserum means theres less available drugto concentrate a target organ

66. first pass effect liver gets first pass at metabolizing drugsbefore it passes to other organs- doesnot occur with injection, oral doses mustbe a lot greater

67. gtt drop68. half life the amount of time that it takes for 50%

of the serum level or plasmaconcentration of a drug to be eliminatedor to attain 50% steady stateconcentrations. steady state -input=output.

69. H.S. at bedtime70. hydrophillic

channelsmolecular weight below 200 are able todiffuse along concentration gradient bycrossing through aqueous channels

71. hypoalbuminemia can affect drug serum concentrationand target tissue concentrations- maynot have full expected drug action

72. Ideal Body Weight males: 50kg + 2.3 kg per inch over 5 feetfemales: 45.5 kg + 2.3 kg per inch over 5feet

73. IH inhilation - medications intended forabsorption through pulmonary capillarybeds - systemic absorption may occurwhich is not always desirable. rapid andimmediate effects. dose can be titrated,localized for lungs. Most addictive route.patients may have difficulty regulatingdose.

74. IM injection into intramuscular tissue andsubsequent absorption through capillariesinto the systemic circulation. formulation affetsthe rate, onset, and duration. good for oilyvehicles or irritating substances. better selfadministration than IV.can be painful or causeintramuscular hemorrhage.

75. include on aprescription

patient name, date of birth, medication,strength (mg), amount (1 tab), frequency, howmuch, route, refills, date, sign.

76. INJ inject77. intermittent

doseserum concentration peaks are the high pointsin the concentration fluctuations, troughs arethe low points.

78. Intradermal between the non-vascular epidermis layerand the subcutaneous layer - enters systemiccirculation through the capillaries

79. irreversibleantagonism

compete with agonists for agonist bindingdomain and bind permanently with thereceptor

80. Isoenzymesresponsiblefor P450catalyzedreactions

CYP3A4/5 - most commonCYP2D6CYP2C8/9CYP1A2

81. IV intravenous - continuous or intermittent. drugsolubility, formulation, and drug solutioncompatability may limit the ability of somedrugs to be administered .immediate effects, ideal if dosed in largevolumes.unsuitable for oily or poorly absorbedsubstances - bolus injection may lead toadverse effects.

82. Lbs to Kg 2.2lb/kg83. lethal dose concentration of drug which induces death in

50% of subjects to which the drug isadministered

84. Liverfunctiontests

ALT (most specific)ASTalkaline phosphatase levels

85. Loadingdose

therapeutic drug levels can be reached morerapidly generally by administering an initialloading dose - the first dose of drug that iscalculated to be higher than the doses that willfollow. loading doses are given to reachtherapeutic serum drug concentrations morequickly than administering routineintermittent doses.

86. maitenancedoses

routine doses that keep steady state drugserum concentrations in therapeutic range

87. major modes ofdrug excretion

renal: occur within the glomeruli andthe renal tubesHepatobiliary excretion - liver > gallbladder > bile>fecesFecal - clearance through intestine >fecesDrug deposition, serum derived fluids,perspiration

88. margin of safety margin between therapeutic dose andthe lethal dose

89. Medication Error preventable event that may cause orlead to inappropriate medication use orpatient harm while the medication is inthe control of the health careprofessional, patient, or consumer. Suchevents may be related to professionalpractice, health care products,procedures, and systems includingprescribing, order communicaion,product labeling, packaging, andnomenclature, compounding(preparation), dispensing, distribution,administration, education, monitoringand use

90. Medication Errors mistakes occuring in the medication useprocess, regardless of whether an injuryoccured or whether the potential forinjury was present (before it becomesan ADE)

91. medicationhistory list

medication, dose, taken how often, forwhat reason, prescribed by

92. Microsomal(membranebound)OXIDATION

phase 1

hydroxylationdealkylationoxidationpolarizing atom exchange

93. MicrosomalMembrane boundREDUCTION

azoreductionnitroreduction

94. Most common andpreventablecauses ofmedication errors

ambiguous medical notations -misinterpretation may lead to mistakesthat result in patient harm.

95. Most rapidonset/mostbioavailability

intravenous, intramuscular,subcutaneous, oral, rectal, inhalation,transdermal

96. non competitveantagonism

antagonist binds to sites other than theagonistic binding domain. high doses ofagonists can not overcome theantagonist

97. Non microsomaloxidation andreduction

alcohol oxidation (NAD+)alcohol reduction (NADH)

98. Norepinephrine primary transmitter at most sympatheticpostganglionic nerve endings.synthesized from tyrosine. can bind witha1, b1 or b2 adrenergic receptors.reuptake into nerve terminal. releasedinto

99. P450 inducer phenobarbital, rifampin, andcarbazepine can increase the synthesisof more CYP iso - decreases the plasmaconcentration of the drug

100. P450 inhibitor omeprazole is a potent inhibitor of threeof the CYP isoenzymes responsible forwarfarin metabolism - more warfarinaround = more anticoagulation

erythromycin, ketoconazole, andritonavir cimetidine blocks the metabolism oftheophylline

grapefruit juice inhibits CYP3A4 leadingto higher levels of nifedipine,clarithromycin, and simvastatin

101. Parasympathetic- cranial sacral

cardiac and smooth muscle, gland cells,nerve terminals.ACh - AChlong preganglionic short postganglionicganglia within or near target organsminimal preganglionic fiber branchinglimited distribution and descreteresponse

102. Parasympathetictransmission

ACh transmits all parasympatheticsignals to end organs like heart andlungs by binding to muscarinic receptors

103. Parenteral bypass the gastrointestinal tract for medabsorption

104. passive diffusion quick for small, nonionic, lipophilic drugmolecules. slow for larger ionichydrophilic molecules

105. Pharmacodynamics properties of drug effects,including time to onset of action,time to reach peak effects,duration of action, and expectedtimes for drug clearance. can beimpacted by pharmacokineticchanges What the drug does to the bodyie. dilated pupil

106. Pharmacogenetics relationships between geneticfactors and drug response

107. Pharmacogenomics relation of an individual's geneticmakeup to his or her response tospecific drugs

108. Pharmacokinetics(ADME)

distinct processes and factorswhereby drugs are absorbed,distributed, biotransformed,metabolized, and excreted fromthe bodyWhat the body does to a drug.

109. Pharmacology the study and science of theeffects of drugs on organisms andsystems

110. Pharmacotherapeutics the use of drugs for therapeuticpurposes

111. Phase 2 reactions glucuronide conjugationethereal sulfate conjugationacetylationtransulfurationglutathione conjugation

112. Phases of drugmetabolism

Phase 1 - drugs are oxidized orreduced to a more polar formPhase 2 - a polar molecular groupis conjugated to the drug whichsubstantially increases its polarity

113. Physiologic DrugDependence

occurs when the body physicallydevelops reliance on a drug.Abrupt drug discontinuance canlead to adverse effects includingwithdrawl, rebound, etc.prednisone, clonidine

114. pKa for weak bases pKa = pH + log (BH)/Bwhen pH>pKa for weak base theuncharged deprotonated formpredominates

115. pKa weak acids pH + log (HA)/A

pH

129. referral plan SBAP - situation, background, assessment,plan

130. renal excretion blood urea nitrogen and serum creatininelevels, maybe GFR. SCr (rate the kidneyscan clear creatinine) is much moresensitive indicator of renal function thanthe BUN.

131. sig directions to be written on lable132. ss one half133. steady state between 4 and 5 half lives134. subcutaenous beneath the cutaneous layer of the skin.

enters systemic circulation through thecapillaries. aqueous solution has prompteffects, depot perparations are slow andsustained. suitable for slow released drugsor poorly soluble suspensions. unsuitablefor large volumes.

135. Sublingual placed under tongue for absorptionthrough sublingual capillaries. don't useabbreviation. most erratically orincompletely absorbed. bypasses first passeffect and destruction by stomach acid

136. Substrates drugs which are metabolized by one ormore CYP enzymes

137. Sympathetic -thoracolumbar

sweat glands (ACh - ACh), cardiac andsmooth muscle, nerve terminals (ACh - NE),renal vascular smooth muscle (ACh, D),skeletal muscle (no post synaptic area, AChstraight to muscle)

short preganglionic, long post ganglionic,ganglia close to spinal cord, extensivepreganglionic fiber brancing, widedistribution, diffuse response

138. Syngerism the response elicited by combined drugs isGREATER than the combined responses ofindividual drugs(1+1=3)vancomycin causes cell wall damage andgentamicin has more penetration to treatbacterial endocarditiscombination is more effective

139. therapeuticeffect

desired pharmacological effects of a drug

140. therapeuticindex

measure of the safety of a drug calculatedby dividing the lethal dose by the effectiveconcentration

141. TID three times a day142. tolerance decreased effectiveness of a drug over

time with repeated use

143. Topical local administration of meds:ophthalmicdermatologicnasal - through mucous membranes into thenasal capillary bedsvaginal (PV) - local effectsotic - usually for local effect

144. Transdermal patch - slow and sustained absorption.bypasses the first pass effect, ideal for drugsthat are quickly eliminated from the body.ideal for lipophilic drugs. some patients maybe allergic, may have delayed delivery.

145. Treatmentdrugs

used in the therapeutic management ofdisease or medical conditionsmoxifloxacin for bacterial conjunctivitis.

146. Type AReactions

85-90% of all ADRs. These can affect anyindividual, given sufficient dose andexposure, and are predictable from theknown pharmacologic properties of a drug.Diarrhea in response to antibiotics

147. Type BReactions

10-15% of ADRs. hypersensitivity reactions,mediated by immunologic or other types ofmechanisms which occur in a susceptiblesubgroup of patients - signs and symptomsthat are different than the action of the drugand usually not predicted. Anaphylaxis, skinrashes, or immune mediatedthrombocytopenia

148. UD as directed149. Ung ointment150. WA while awake151. When to use

adjustedbody weight

weight is more than 20% over ideal bodyweight (10-20kg difference is significant)

Pharmacology Exam 1