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pharmacology > Unit 1 bolded terms > Flashcards

Unit 1 bolded terms Flashcards

1
Q

pharmaceutic phase

A

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

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2
Q

excipients

A

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

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3
Q

disintegration

A

the breakdown of a tablet into smaller particles

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4
Q

dissolution

A

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

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5
Q

rate limiting

A

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

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6
Q

pharmacokinetics

A

the process of drug movement to achieve drug actions

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

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7
Q

passive absorption

A

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

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

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8
Q

active absorption

A

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

energy is required

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9
Q

pinocytosis

A

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

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10
Q

note on absorption:

A

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

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11
Q

first-pass effect

AKA hepatic first pass

A

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

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12
Q

bioavailability

A

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%

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13
Q

factors that alter bioavailability

A

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)

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14
Q

distribution

A

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

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15
Q

volume of distribution (Vd)

A

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

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16
Q

protein-bind effect

A

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

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17
Q

free drugs

A

drugs not bound to protein

only free drugs are active and can cause pharmacologic response

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18
Q

metabolism

A

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

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19
Q

half-life (t1/2)

A

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

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20
Q

elimination

A

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

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21
Q

elimination and pH

A

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

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22
Q

creatinine clearance (CLcr)

A

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

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23
Q

pharmacodynamics

A

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

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24
Q

dose response

A

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

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25
Q

onset of action

A

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

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26
Q

peak action

A

occurs when the drug reaches its highest blood or plasma concentration

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27
Q

duration of action

A

is the length of time the drug has a pharmacologic effect

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28
Q

time-response curve

A

evaluates 3 paramaters of drug action

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

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29
Q

receptor families

A

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

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30
Q

ligand-binding domain

A

the site on the receptor at which drugs bind

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31
Q

kinase-linked receptors

A

the ligand-binding domain for drug binding on the cell surface.

The drug activates the enzyme (inside the cell), and a response is initiated

32
Q

ligand-gated ion channels

A

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

33
Q

G-protein coupled receptor systems

A

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

34
Q

nuclear receptors

A

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

35
Q

agonists

A

drugs that produce a response

ex: Isoproterenol (Isuprel) stimulates beta1 and beta2 receptors, so it is anagonist

36
Q

antagonists

A

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

37
Q

nonspecific drugs

A

drugs that affect various sites

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

38
Q

nonselective drugs

A

drugs that affect various receptors

39
Q

categories of drug action

A

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)

40
Q

therpeutic index (TI)

A

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

41
Q

low therapeutic index

A

have a narrow margin of safety

42
Q

high therapeutic index

A

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

43
Q

therapeutic range

(therapeutic window)

A

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

44
Q

peak drug level

A

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

45
Q

peak drug level

A

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

46
Q

loading dose

A

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

47
Q

bolus

A

adminstering drug by IV push

48
Q

drop factor

A

number of drops per Ml

49
Q

macrodrip set

A

delivers large drops per mL

(10-20 gtt/mL)

If infusion rate is 100mL/h or more, macrodrip set is preferred

50
Q

microdrip set

A

small drops per mL

60 gtts/mL

if infusion rate is < 100 mL/h or client is a child, the microdrip set is preferred

51
Q

Keep vein open

(KVO)

A

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

52
Q

secondary IV line set

A

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

53
Q

IV push

A

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

54
Q

electronic intravenous (IV) regulators

A

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

55
Q

volumtric regulator

A

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

56
Q

nonvolumetric regulator

A

designed to infuse at a drop rate in drops per minute

57
Q

common progems associated with IV infusions

A

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

58
Q

patient-controlled analgesia (PCA)

A

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

59
Q

pediatric drug dosages differ b/c:

A

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

60
Q

two methods considered safe in administration of drugs to children:

(calculating dose)

A

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

61
Q

dosage per body weight

A

usually done in kg

divide weight in lbs by 2.2 to get weight in kg

62
Q

calculate pediatric dosage per body surface area

A

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)

63
Q

injection sites for peds

A

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

64
Q

The United States Pharmacopeia National Formulary (USP-NF)

A

the current 3 volume authoritative source for drug standards

an annual publication

65
Q

U.S> Food and Drug Administration (FDA)

A

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

66
Q

Durham- Humphrey Amendment to teh 1938 Act

A

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

67
Q

Kefauver-Harris Amendment to the 1938 Act

A

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

68
Q

The Controlled Substances Act

A

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

69
Q

controlled substances

A

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)

70
Q

Drug Enforcement Administration DEA

A

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

71
Q

Drug REgulation Reform Act

A

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

72
Q

The Food and Drug Administration Modernization Act

A

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

73
Q

Health Insurance Portability and Accountability Act (HIPAA)

A

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

74
Q

Pediatric Research Equity Act

A

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

75
Q

Medicare Prescription Drug Improvement and Modernization Act

A

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

pharmacology (10 decks)

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