Unit 1 bolded terms

Question 1

pharmaceutic phase

Answer 1

the drug becomes a solutation so that it can cross the biologic membrane

Question 2

excipients

Answer 2

used in drug preparation to allow the drug to take on a particular size and shape to enhance dissolution

AKA fillers and intert substances

Some additives in drugs, such as the ions K and Na in penicillin potassium and penicillin sodium, increase the absorbability of the drug

Question 3

disintegration

Answer 3

the breakdown of a tablet into smaller particles

Question 4

dissolution

Answer 4

the dissolving of the smaller particles in the GI fluid before absorption

Question 5

rate limiting

Answer 5

the time it takes the drug to disintegrate and dissolve to become available for the body to absorb it

generally, drugs are both disintegrated and absorved faster in acidic fluids with a pH of 1 or 2 rather than in alkaline fluids

both the very young and older adults have less gastric acidity; therefore drug absorption is generally slower for those drugs absorved primarily in the stomach

Question 6

pharmacokinetics

Answer 6

the process of drug movement to achieve drug actions

4 process: absorption, distribution, metabolism (or biotransformation), and excretion (or elimination)

Question 7

passive absorption

Answer 7

occurs mostly by diffusion (movement from higher concentration to lower concentration)

with diffusion, the drug does not require energy to move across the membrane

Question 8

active absorption

Answer 8

requires a carrier such as an enzyme or protein to move the drug against a concentration gradient

energy is required

Question 9

pinocytosis

Answer 9

process by which cells carry a drug across their membrane by enguling the drug particles

Question 10

note on absorption:

Answer 10

remember: drugs tha are lipid soluble and nonionized are absorved faster than water-soluble and ionized drugs

Question 11

first-pass effect

AKA hepatic first pass

Answer 11

the process in which the drug passes to the liver first

exampes of drugs with first-pass metabolism: warfarin (Coumadin) and morphine.

Lidocaine and some nitroglycerins are not given orally because they have extensive first-pass metabolism and therefore more of the dose would be destroyed

Question 12

bioavailability

Answer 12

is a subcategory of absorption. It is the percentage of the administered rug dose that reaches the systemic circulation

oral dose: less than 100%

intravenous route: usually 100%

Question 13

factors that alter bioavailability

Answer 13

1) drug form (tablet, capsule, sustained-release, liquid, transdermal pathc, rectal supossitory, inhalation
2) route of administration (oral, rectal, topical, parenteral)
3) GI mucosa and motility
4) food and other drugs
5) changes in liver metabolism caused by liver dysfunction or inadequate hepatic blood flow (but only if drug is metabolized in the liver)

Question 14

distribution

Answer 14

the process by which the drug becomes available to body fluids and body tissues

influenced by blood flow, the drug’s affinity to the tissue, and the protein-binding effect

Question 15

volume of distribution (Vd)

Answer 15

dependent on drug dose and its concentration in the body

drugs with larger volume of distribution have a longer half-life and stay in the body longer

Question 16

protein-bind effect

Answer 16

as drugs are distributed in the plasma, many are bound to varying degrees (percentage) with protein (primarily albumin)

>89% bound to protein: highly protein-bound drugs

61%-89%: moderately highly protein bound

30%-60% moderately protein bound

<30%: low protein bound

Low protein level decreases the number of protein-bind sites, leading to more free drug in plasma. Clients with liver or kidney disease, or who are malnourished, may have abnormally low serum albumin

some drugs bind with specific protein compenent: most anticonvulsants bind primarily to albumin. Most antidysrhythmics (e.g., lidocaine and quinidine) bind mostly to globulins

Question 17

free drugs

Answer 17

drugs not bound to protein

only free drugs are active and can cause pharmacologic response

Question 18

metabolism

Answer 18

drugs can be metabolized in both the GI tract and the liver

liver is the primary site for metabolism

most drugs are inactivated by liver enzymes and are then converted or transformed by hepatic enzymes to inactive metabolites

Question 19

half-life (t1/2)

Answer 19

of a drug is the time it takes for one half of the drug concentration to be eliminated

4-8 hr: short half-life

24 hours or longer: long half-life

administration of a drug for 3-5 half-lives saturates the bioligic system to the extent that intake of drug equals amt metabolized and excreted

Question 20

elimination

Answer 20

main route is through the kidneys

other routes include: bile, feces, lungs, saliva, sweat, and breast milk

kidneys filter free unbound drugs, water-soluble drugs, and drugs that are unchanged

protein-bound drugs cannot be filtered through the kidneys

lungs eliminate volatile drug substances and products metabolized to CO2 and H2O

Question 21

elimination and pH

Answer 21

Urine pH varies from 4.5-8

acidic urine promotes elimination of weak base drugs.

alkaline urine promotes elimination of weak acid drugs

Aspirin, a weak acid, is excreted rapidly in alkaline urine. If someone OD’s on aspirin, bicarbonate may be given to change urine pH to alkaline

Large quantities of cranberry juice can decrease urine pH, causing acidic urine and inhibiting the elimination of aspirin

Question 22

creatinine clearance (CLcr)

Answer 22

most accurate test to determine renal function

compaires the level of creatinine in the urine with the level of creatinine in the blood

creatinine is a metabolic byproduct of muscle that is excreted in the kidneys

CLcr test consists of 12 or 24 hour urine collection and blood sample

normal CLcr is 85-135 mL/min

Older adult clients may have creatinine clearance of 60 mL/min due b/c aging decreases muscle mass and results in a decrease in functioning nephrons

creatinine clearance varies with age and gender: lower values are expected in older adult and female clients b/c of their decreased muscle mass

A decrease in GFR results in an increase in serum creatinne and a decrease in urine creatinine clearance

Question 23

pharmacodynamics

Answer 23

the study of drug concentration and its effects on the body

drug response can cause a primary or secondary physiologic effect or both

primary effect is desirable, and the secondary effect may desirable or undesirable

Question 24

dose response

Answer 24

the relationship b/w the minimal versus the maximum amount of drug dose needed to produce the desired drug response.

some clients respond to a lower drug dose, whereas others need a high drug dose to elicit the desired response

Question 25

onset of action

Answer 25

is the time it takes to reach maximum effective concentration (MEC) after a drug is administered

Question 26

peak action

Answer 26

occurs when the drug reaches its highest blood or plasma concentration

Question 27

duration of action

Answer 27

is the length of time the drug has a pharmacologic effect

Question 28

time-response curve

Answer 28

evaluates 3 paramaters of drug action 1) onset of drug action 2) peak action 3) duration of action

Question 29

receptor families

Answer 29

1) kinase-linked receptors 2) ligand-gated ion channels 3) G proteincoupled receptor systems 4) nuclear receptors

Question 30

ligand-binding domain

Answer 30

the site on the receptor at which drugs bind

Question 31

kinase-linked receptors

Answer 31

the ligand-binding domain for drug binding on the cell surface. The drug activates the enzyme (inside the cell), and a response is initiated

Question 32

ligand-gated ion channels

Answer 32

the channel spans the cell membrane and, with this type of receptor, the channel opens, allowing for the flow of ions into and out of the cells. The ions are primarily Na and Ca

Question 33

G-protein coupled receptor systems

Answer 33

there are 3 components to this receptor response 1) the receptor 2) the G protein that binds with guanosine triphosphate (GTP) 3) the effector that is either an enzyme or an ion channel Drug activates the receptor. Receptor then activates G protein. G Protein then activates the effector

Question 34

nuclear receptors

Answer 34

found in the cell nucleus (not on the surface) of the cell membrane. Activation of receptors through the transcription factors is prolonged. With the first 3 receptor groups, activation of the receptors is rapid

Question 35

agonists

Answer 35

drugs that produce a response ex: Isoproterenol (Isuprel) stimulates beta₁ and beta2 receptors, so it is anagonist

Question 36

antagonists

Answer 36

drugs that block a response ex: cimetidine (Tagamet) blocks the histamine (H₂) receptor, thus preventing excess gastric acid secretion The effects of an antagoist can be determined by the inhibitory (I) action of the drug concentration on the receptor site IC₅₀ is the antagonist drug concentration required to inhibit 50% of the maximum biological response

Question 37

nonspecific drugs

Answer 37

drugs that affect various sites occurs when drugs act on receptors that can be found throughout the body

Question 38

nonselective drugs

Answer 38

drugs that affect various receptors

Question 39

categories of drug action

Answer 39

1) stimulation or depression (ex: drug stimulating or depressing the secretion of a gland) 2) replacement (ex: insulin) 3) inhibition or killing of organisms (ex: antibiotics) 4) irritation (ex: laxatives irritate the inner wall of the colon, thus increasing peristalsis and defecation)

Question 40

therpeutic index (TI)

Answer 40

estimates the margin of safety of a drug through the use of a ratio that measures the effective (therapeutic concentration) dose (ED) in 50% of persons or animals (ED₅₀) and the lethal dose in 50% of animals (LD₅₀) The closer the ratio is to 1, the greater the danger of toxicity TI = LD₅₀/ED50

Question 41

low therapeutic index

Answer 41

have a narrow margin of safety

Question 42

high therapeutic index

Answer 42

wide margin of safety and less danger of producing toxic effects Plasma drug levels do not need to be monitored routinely for drugs with a high TI

Question 43

therapeutic range | (therapeutic window)

Answer 43

therapeutic range of a drug concentration in plasma should be between the minimum effective concentration in the plasma for obtaining desired action and the minimum toxic concentration when the therapeutic range is given, it includes both protein-bound and unbound portions of the drug

Question 44

peak drug level

Answer 44

the lowest plasma concentration of a drug measures the rate at which the drug is eliminated trough levels are drawnimmediately before the next dose of drug is given

Question 45

peak drug level

Answer 45

the highest plasma concentration of a drug at a specific time peak drug levels indicate the rate of absorption if the drug is given orally,the peak time might be 1-3 hours after drug administration. If given IV, peak time might occur in 10 minutes a blood sample should be drawn at the proposed peak time, according to the route of administration

Question 46

loading dose

Answer 46

given when immediate drug response is desired large initial dose given to achieve a rapid minimum effective concentration in plasma after a large initial dose, a prescribed dosage per day is ordered

Question 47

bolus

Answer 47

adminstering drug by IV push

Question 48

drop factor

Answer 48

number of drops per Ml

Question 49

macrodrip set

Answer 49

delivers large drops per mL (10-20 gtt/mL) If infusion rate is 100mL/h or more, macrodrip set is preferred

Question 50

microdrip set

Answer 50

small drops per mL 60 gtts/mL if infusion rate is \< 100 mL/h or client is a child, the microdrip set is preferred

Question 51

Keep vein open | (KVO)

Answer 51

AKA to keep open (TKO) when IV fluids are given at a slow rate to keep the vein open reasons for ordering KVO: suspected or potential emergency situation for rapid administration of fluids and drugs and the need for an open line to give IV drugs at specified hours For KVO, a micro drip set (60gtt/mL) and 250 mL IV bag may be used. KVO is usually regulated to deliver 10mL/hr

Question 52

secondary IV line set

Answer 52

inserted into primary IV line set through a rubber port usually used when drugs are Rx to be administered 3-6 times a day in a small volume of IV fluid (50-100 mL) drug solution is usually infused over a period of 15 minutes to 1 hour This is called intermittent IV therapy

Question 53

IV push

Answer 53

meds that are given by IV injection route are calculated in the same manner as meds for IM injection clinically, it is the preferred route for clients with poor muscle mass or decreased circulation, or for a drug that is poorly absorbed from the tissues

Question 54

electronic intravenous (IV) regulators

Answer 54

pumps set to deliver Rx rate of IV solution if flow rate is obstructed, an alarm sounds flow rate set at mL/h pumps do not recognize infiltration the alarm does not sound until the pump has exerted its maximum pressure to overcome resistance

Question 55

volumtric regulator

Answer 55

delivers a specific volume of fluid at a specific rate, in mL per hour

Question 56

nonvolumetric regulator

Answer 56

designed to infuse at a drop rate in drops per minute

Question 57

common progems associated with IV infusions

Answer 57

**kinked tubing**- if tubing kinks, the flow is interrupted and the Rx amt of fluid will not be given. The access site can clot **infiltration**- fluid extravasates into the tissues and not into the vascular space. Trauma occurs to the tissues at the IV site **"free flow"**- refers to rapid infusion of IV fluids. faster than Rx. causes fluid overload. B/c of possiblity of "free flow," electronic infusion pumps are commonly used today

Question 58

patient-controlled analgesia (PCA)

Answer 58

objective of PCA: to provide a uniform serum concentration of the durg, avoiding peaks and valleys method designed to meet the needs of clients who require at least 24-48 hours of regular IM narcotic injections reasons to use PCA: 1) effective pain control w/o the cl feeling oversedated 2) considerable reduction in the amount of narcotic used (approx. 1/2 that of IM delivery) 3) cleints' feelings of having greater control over their pain

Question 59

pediatric drug dosages differ b/c:

Answer 59

neonates and infants have immature kidney and liver function, which delays metabolism and excretion of many drugs in neonates, drug absorption is different as a result of slow gastric emptying time decreased gastric acid secretion in children under 3 contributes to altered drug absorption neonates and infants have lower concentration of plasma proteins, which can cause toxicity with drugs that are highly protein bound young children have less total body fat and more body water; therefore lipid soluble drugs require smaller doses when less-than-normal fat is present water soluble drugs can require large doses b/c of a greater percentage of water

Question 60

two methods considered safe in administration of drugs to children: (calculating dose)

Answer 60

1) body weight 2) body surface area (BSA) or m²

Question 61

dosage per body weight

Answer 61

usually done in kg divide weight in lbs by 2.2 to get weight in kg

Question 62

calculate pediatric dosage per body surface area

Answer 62

Need the child's height and weigh nomogram can be used (specialized chart) the square root formula and be used BSA= (square root of) height (inches) x weight (lbs) ----------------------------------------------------- 3131 (constant)

Question 63

injection sites for peds

Answer 63

vastus lateralis: safe for neonates to adolescents (varying amount of meds can be injected, depending on age) rectus femoris: NOT safe for neonates and infants ventrogluteal: NOT safe for neonates, infants, or toddlers dorsal gluteal: NOT safe for neonates, infants, toddlers gluteus maximus: NOT safe for neonates, infants, toddlers deltoid: NOT safe for neonates and infants

Question 64

The United States Pharmacopeia National Formulary (USP-NF)

Answer 64

the current 3 volume authoritative source for drug standards an annual publication

Question 65

U.S\> Food and Drug Administration (FDA)

Answer 65

empowered by The Food, Drug, and Cosmetic Act of 1938 to monitor and regulate the manufacture and marketing of drugs FDA is responsible for ensuring that all drugs are tested for harmful effects, have labels with accurate info, and enclose with the drug packaging detailed literature that explains adverse effects Only drugs considered safe by the FDA are approved for marketing

Question 66

Durham- Humphrey Amendment to teh 1938 Act

Answer 66

Passed in 1952 distinguished b/w drugs that can be sold with or without a Rx and those that should not be refilled w/o a new Rx drugs that should not be refilled w/o a new Rx: narcotics, hypnotics, transquilizers

Question 67

Kefauver-Harris Amendment to the 1938 Act

Answer 67

passed in 1962 resulted from widely publicized thalidomide tragedy of the 1950's in which pregnant European women who took the sedative-hypnotic thalidomide during the first trimester of pregnancy gave birth to infants with extreme limb deformities tightened controls on drug safety, especially experimental drugs, and required that adverse reactions and contraindications be labeled and included in the literatue Also included provisions for the evaluation of testing methods used by manufacturers, the precess for withdrawal of approved drugs when safety and effectiveness were in doubt, and establishment of effectiveness of new drug before marketing

Question 68

The Controlled Substances Act

Answer 68

passed in 1970 designed to remedy problem of drug abuse several provisions: 1) the promotion of drug education and research into the prevention and tx of drug dependence 2) the strengthening of teh enforcement authority 3) the establishment of treatment and rehab facilities 4) designation of schedules, or categories, for controlled substances acordding to abuse liability

Question 69

controlled substances

Answer 69

are described in 5 schedules: schedule I: not approved for medical use ex: heroin, LSD, mescaline schedule II accepted medical use, high potential for drug abuse es: meperidine (Demerol), morphine, pentobarbital schedule III accepted medical use, may cause dependence, less abuse potential than II ex: codeine preparations, paregoric, nonnacotic drugs (pentazocine propoxyphene) schedule IV medically accepted, may cause dependence es: phenobarbital, benzodiazepines schedule V medically accepted drugs. very limited potential for dependence. Labeled C-V opioid controlled substances for diarrhea and cough (e.g., codeine in cough preparations)

Question 70

Drug Enforcement Administration DEA

Answer 70

became the nation's sole legal drug enforcement agency in 1983

Question 71

Drug REgulation Reform Act

Answer 71

passed in 1978 shortened the time in which a new drug could be developed and marketed. Protects pt rights and at the same time facilitates the investigational process and promotes research

Question 72

The Food and Drug Administration Modernization Act

Answer 72

passed in 1997 5 provisions: 1) review and use of new drugs is accelerated 2) drugs can be tested in children before marketing 3) clinical trial data are necessary for experimental drug use for serious or life-threatening health conditions 4) drug companies are required to give info on "off-label" drugs (non-FDA approved drugs) and their uses and costs 5) drug companies that plan to discontinue drugs must inform health professionals and clients at least 6 months before stopping production

Question 73

Health Insurance Portability and Accountability Act (HIPAA)

Answer 73

passed in 2003 sets the standards for the privacy of individually identifiable health info as of 2003. gives client more control over their health information

Question 74

Pediatric Research Equity Act

Answer 74

2003 FDA is authorized to require testing by drug manufacturers of the drugs and bioligc products for their safety and effectiveness in children One must not assume that children are small adults

Question 75

Medicare Prescription Drug Improvement and Modernization Act

Answer 75

2003 provides financial assistance to seniors to purchase needed Rx meds Cl responsible for monthly premium of $35 and $250 annual deductible. This benefit will pay 75% of total cost of Rx drugs up to a max of0