N301 Q#1 Orientation to Pharm Week 1 Flashcards
(107 cards)
1
Q
What are the 3 properties of an “ideal” drug (in order of priority)?
A
- Effectiveness
- Safety
- Selectivity
2
Q
What is pharmacotherapy?
A
the reason why the drug is prescribed and the clinical indication for its use.
3
Q
What are pharmacotherapy drugs used for?
A
prevent diagnose relieve treat cure a disease
4
Q
Define drug
A
substance that interacts with a living organism to produce a biologic response
5
Q
What are the 4 steps of pharmacokinetics?
EACH DRUG HAS IT’S OWN CHARACTERISTICS OF…
A
- absorption
- distribution
- metabolism
- excretion
6
Q
Define absorption with relation to pharmacokinetics.
A
the process by which a drug moves from its site of administration into the venous or lymphatic circulation
7
Q
______: term used to describe the fraction of administered dose that reaches the systemic circulation and produces effects.
A
Bioavailability
8
Q
With rapid dissolution, a ___ onset will occur
A
quicker
9
Q
What are genetic variabilities to drug therapy response?
A
gender
age
ethnicity
race
10
Q
____: the delivery of the drug into any and all body compartments it drug can penetrate. (also begins where absorption ends)
A
Distribution
11
Q
Name Factors that influence the distribution of drugs.
A
Volume of distribution CO regional blood flow capillary permeability degree of plasma protein binding drug reservoirs (storage sites) drug concentration tissue affinity physiologic barriers
12
Q
When drugs bind to proteins they become ___.
When drugs are not bound to protein they become ___.
A
Inactive
active
13
Q
If a patient is anorexic and not ingesting protein, what affect will this have with drug distribution?
A
Increased unbound drug will lead to toxicity
14
Q
If a body builder has high serum protein levels what affect will this have on drug distribution and therapeutic benefit?
A
More bound drug means more inactive drug, won’t get therapeutic benefit.
15
Q
How do reservoirs impact drug distribution? for example, an obese person?
A
drug gets bound up in body tissue, can’t be accessed and won’t get therapeutic benefit.
16
Q
Abscesses and solid tumors are considered what barrier with regard to drug distribution?
A
physical barriers
17
Q
____ (or biotransformation), is the alteration or changing of a drug to more ionized or water soluble and less lipid soluble form called ___.
Most drug biotransformation takes place in the ___ while drug elimination takes place in the ____.
A
- metabolism
- metabolites
- liver
- kidney
18
Q
____: chemical form of a drug that is a product of one or more biochemical metabolic rxns. more ionized.
A
metabolite
19
Q
When acetaminophen is metabolized, what potentially harmful metabolites are formed? These metabolites cause injury to what organ?
A
hepatotoxic metabolites
liver
20
Q
Cytochrome P450 is a hepatic-drug metabolizing ___. Ie, it causes changes in the rate of metabolism of certain drugs that may require dosage changes. Common in ___. Using same pathway.
A
Enzyme
med-surg; drug-drug pathway.
21
Q
Demerol also has ___ that can be damaging.
A
metabolites
22
Q
What are 6 consequences of metabolism?
A
- Accelerated renal excretion of the drug
- Drug inactivation
- Increased Therapeutic Action
- Activation of pro drugs
- Increased toxicity
- decreased toxicity
23
Q
What is the most important consequence of metabolism?
A
Accelerated renal excretion of the drug
24
Q
- The kidney is the major organ of _____
- The kidney is unable to excrete drugs that are highly ___ soluble b/c the mlcls are too large.
- The conversion of lipid soluble drugs into more ___ (or less lipid soluble) drugs makes it possible for the kidneys to excrete many drugs.
A
- Elimination
- lipid
- polar
25
A pro-drug only become active thru?? If a drug only becomes active thru metabolism, will the drug every become active?
metabolism
| no
26
What is drug inactivation?
Conversion of drugs from active to inactive form via metabolism
27
____: when effectiveness of a drug is increased by metabolism
Increased Therapeutic Effect
28
With pain management, when codeine is converted to ___ by metabolism, this is an example of increased ___ effect. Tylenol 3 or 4 contains ___. ____ is the gold standard for pain management.
1. morphine
2. therapeutic
3. Codeine
4. Morphine
29
Metabolism can decrease toxicity by converting drugs into ____ forms.
Metabolism can increase the potential for harm by converting safe compounds into forms that are __.
1. inactive
| 2. toxic
30
With hepatic dysfunction, pts will have problems ____ drugs. They are therefore at greater risk for ___ damage and ___ effects of drug therapies.
1. metabolizing
2. liver
3. toxic
31
Urinary excretion is the result of what 3 processes?
1. Glomerular Filtration
2. Passive Tubular Reabsorption
3. Active Tubular Secretion
32
Glomerular Filtration moves drugs from the blood into ____ urine. Since large molecules can't pass, they do or do not undergo GF? So, if a drug is bound to albumin will it remain in the blood or be filtrated?
1. tubular
2. do not
3. remain in blood
33
With Passive Tubular Reabsorption, drug concentrations in the blood are higher or lower than the tubule?
lower
34
Will drugs that are NOT lipid soluble (ie ions and polar compounds) remain in the urine for secretion?
Lipid soluble drugs must be converted to more ___ forms. This reduces _____ reabsorption and ___ excretion.
1. Yes
2. polar
3. passive
4. increases
35
With active tubular secretion, what two classes of pumps are involved in renal excretion?
Tubule cells contain ____ which can act as a pump.
These pumps have a relatively high ___ and require ___ expenditure to move drugs.
1. Organic acids
2. Organic bases
3. P-glycoprotein
4. capacity; energy
36
The kidneys account for the majority of drug ____ so patients with renal dysfunction will have problems ___ drugs.
With renal failure, both the duration and ____ of drug responses may ____.
These patients are at risk for renal damage and ___ effects of therapies.
When the kidneys are healthy, they serve to limit the ___ of many drugs.
```
excretion, excreting
intensity
increase
toxic
duration
```
37
What is the objective of drug dosing?
maintain drug levels within therapeutic range; or enough drug is present to produce an effect w/o toxic results.
38
_____: plasma drug level below which therapeutic effects will not occur.
Minimum effective concentration (MEC)
39
____ concentration: plasma drug level at which toxic effects begin
toxic
40
What is the major barrier to passage through a cell?
| What are the 3 ways to cross a cell membrane?
cytoplasmic membrane (lipid bilayer)
1. via Channels or Pores
2. Transport Systems
3. Direct Penetration
41
Small compounds can pass through the lipid bilayer via ___ and ____. Ex. Na and K ion channels.
Very few drugs move this way!!
channels and pores
42
____ systems move drugs from one side of membranes to the other; some requiring energy. But they are ALL ____ for a specific drug. For example ____ transports drugs OUT of the cell.
1. Transport
2. Selective
3. P-Glycoprotein
43
Most drugs cannot directly penetrate a membrane because they are too ___ to pass through or lack a ___ system. Otherwise, they must be ____ soluble.
large
| lipid
44
____ molecules have an uneven distribution of electrical charge.
Molecules that have a net charge are called ___. Remember like dissolves ____. Polar molecules will dissolve in ___ solvents.
polar
ions.
like
polar
45
With ionization, acids tend to ionize ____ media. Bases tend to ionize ___ media.
basic
| acidic
46
With ____ drug mlcls will accumulate on the side where the pH most favors their ionization. Therefore, acidic drugs will accumulate on the ____ side and basic drugs will accumulate on the ___ side.
ion trapping or pH partitioning
alkaline
acidic
47
Acids are proton ___ and bases are proton ____
donors
| acceptors
48
Water soluble or lipid soluble drugs require more metabolism?
water soluble
49
Along with albumin, other plasma proteins that serve as drug reservoirs are lipoproteins and ___.
In addition, other drug reservoirs are bone, __, or other tissues.
alpha-1 acid glycoproteins
| fat
50
The blood-brain barrier is a ____ mechanism that opposes passage of most ions and large mlcl compds from the blood to the brain tissue. Drugs must be ____ soluble or have a ____ system to leave the blood and reach a site of action in the brain.
Selective
lipid
transport
51
Membranes of the ____ do not constitute an absolute barrier to the passage of drugs. ____ soluble drugs readily cross the membrane!
placenta
| Lipid
52
____ First Pass allows drugs to temporarily bypass the liver and allow drug to reach therapeutic levels. ___ is an example with rapid hepatic ____. **Nitroglycerin does or does not have effect if orally administered? When administered ___, it is absorbed directly into the systemic circulation bypassing the gut and portal vein.
```
Hepatic
Nitroglycerin
metabolism
Does NOT
sublingually
```
53
____: the evenly distributed concentration of a drug which occurs when the administration equals the rate of drug elimination. This is achieved in approx. ____ half lives. Also is independent or dependent of drug dosage size?
Steady state or plateau
4-5
independent
54
____: the time needed for the plasma concentration of a drug to be reduced by 50%
half-life
55
Dosing frequency is dependent on drug half life or steady state? Drugs with a short half life need __ dosing intervals while drugs with longer half life can have ____ intervals without loss of therapeutic effect.
half-life
short
longer
56
The shorter the dosing interval the ___ to steady state.
quicker
57
If a drug dose is QID then how many hours to reach steady state?
24-30 hours. (4 times a day= 6 hours per dose X 4-5 half-lives)
58
If a drug is administered weekly, how long to reach steady state?
4-5 weeks
59
___ concentration: highest serum level after admin.
___ concentration: lowest serum level after admin.
The goal is to keep (above) with therapeutic range: b/w the ___ and toxic level.
peak
trough
MEC
60
What limits fluctuations in drug levels?
continuous infusion
reducing dosage size
reducing dosage interval
61
True or False: The shorter the dosing interval the quicker to effectiveness or steady state.
True
62
If a drug has a long half life, a ____ dose is used to achieve plateau more quickly. It is a large ____ dose of a drug. After high drug levels have been established with (above), plateau can be maintained by giving ___ doses.
Loading
initial
smaller
63
Smaller doses administered following a loading dose are called _____.
maintenance doses.
64
Plateau will always be reached within ____ half lives (regardless of drug dosage). Patients do or do not reach plateau with loading dose? loading doses rapidly produce a drug level equivalent to the _____ level for a smaller dose.
4-5
do not
plateau
65
with drug admin d/c, __% of the drug is eliminated w/in 4 half lives?
96%
66
With parenteral admin, what are the advantages of IV use?
rapid onset and control (bypasses the GI tract)
larger fluid volumes (larger vessels)
use of irritant medications
67
Why are parenteral routes (IV) highly dangerous?
rapid onset and irreversibility
volume overload
infection
embolism
68
With IV parenteral route, what are two types?
Peripheral: limbs, skull
or
Central: jugular or subclavian (larger vessel, more surface area so less irritating with vessicants-acidic)
69
is IV, IM and SQ parenteral or enteral route?
parenteral
70
With IM route, what is advantage?
Viscous or irritating vessicants can be administered, depot preps (storage for slower release, use Z track method)
71
With enteral admin route, what area are drugs absorbed in?
stomach or small intestine
72
What factors influence absorption enterally?
gastric & intestinal pH
solubility and stability of drug
gastric emptying (ex. diabetics will have slower emtpying)
Coadmin of other drugs
73
Enteral is the most or least:
common?
Variable?
most common AND most variable
74
Tablets are ____ coated allowing for ___ release
enteric, sustained
75
Topical routes of admin include? they cause ___ vs. systemic effects.
sublingual, buccal and rectal.
| local
76
Do ideals drugs exist?
| What are the 3 most important characteristics of any drug?
in theory only, no such thing as the perfect drug.
Effectiveness
Safety
Selectivity
77
______: a drug that elicits the responses for which it is given.
Effectiveness
78
a ____ drug is one that cannot produce harmful effects, really NO SUCH thing.
Safe
79
____: drug property; elicits only the response for which it is given
Selective
80
The ideal drug is
1. _____ in action
2. predicable
3. ___ of admin
4. Free of drug ____
5. has chemical ____
6. has a simple _____ name
1. reversible (Ie can come of the receptor)
3. ease
4. interactions
5. stability
6. generic
81
What is the objective of drug therapy?
max benefit with minimum harm
82
With drug response, ____ size and route and ____ of administration are important.
dosage
| timing
83
If a preparations are ____ in bioavailability, if the drug is absorbed at the same ___ and the same extent.
equal
| rate
84
_____: once the drug has reached it's site of administration, the (same) determines the nature and ___ of the respond.
Pharmacodynamics
| intensity
85
With pharmacodynamics, the initial drug-____ interaction is followed by events that ultimately result in drug ____.
receptor
| response
86
Sources of individual variation include: drug ____, physiologic and pathologic ____ and ____ variables.
interactions
variables
genetic
87
An ___ effect is an effect other than the desired therapeutic effect while a ___ effect refers to a minor effect such as nausea.
adverse
| side
88
____ is a systemic reaction caused by contraction of smooth muscles and increased vascular ____.
Anaphylaxis
| permeability
89
Anaphylaxis is characterized by?
```
dyspnea
bronchospasm
laryngeal edema
cardiac dysrhythmias
seizures
```
90
The progression of anaphylaxis:
1. dyspnea
2. ___ spasm (stridor or wheezing)
3. ____ swelling
4. ___ result from electrical impulse issues
2. airway
3. larynx
4. seizures
91
____ or paradoxical response is an unusual or peculiar response to a drug. They occur b/c of ____ enzyme deficiencies that alter a the drug's metabolism.
Idiosyncratic
| GENETIC
92
Drug Toxicity occurs when drugs accumulate in the body and exceed the amount the body can ____ through metabolism and excretion.
eliminate
93
With _____ injury to the CNS is largely ____. This is largely due to high ____ rate, high ___ content and high ____ requirement.
neurotoxicity, irreversible
metabolic
lipid
circulatory
94
What are signs and symptoms of neurotoxicity? also the progression of neurotoxicity....
```
drowsiness
auditory/visual hallucinations
restlessness
nystagmus (eyes vibrate)
tonic-clonic seizures (grand mal)
```
95
____: when the liver is highly susceptible to toxicants. manifestations include: _____, jaundice, ____ liver enzymes and ____ infiltration of the liver.
Hepatotoxicity
Hepatitis
elevated
fatty
96
To test for liver toxicity, what blood tests are performed?
```
AST, ALT
Alkaline Phosphate (all liver fxn tests)
```
97
_____: the kidneys are highly susceptible to toxicity due to high vascularity (if they don't get oxygen and blood). This is chemically induced damage that manifests as ___ ___ necrosis. What blood test can indicate Acute tubular necrosis (or AKI)? You also want to monitor the _/_ and concentration of urine.
Nephrotoxicity
Acute tubular
Creatinine
Input/output
98
_____: when drugs affect the immune system. some cause _____ whereas others destroy immune system components. This is tested via CBC with ____.
immunotoxicity
Immunosuppression
differential
99
____: irregularities in cardiac rhythms and conduction, possibly heart damage. The cause is unknown; characteristics include?
Cardiotoxicity
| transient cardiac arrhythmias, depression of mycocardial fxn (affects distribution)
100
____: affect C8 and result in inner ear or auditory nerve damage. Structures that get damage include the cochlea, ___ and semicircular canals. This may be ____. Assess hearing loss and ___ or balance.
Ototoxicity
vestibule
irreversible
gait
101
Pharmacokinetic interactions include:
1. GI ____
2. Enzyme ____
3. Enzyme ____
4. Renal ____
5. ___pharmaceuticals
1. absorption
2. induction (less active, b/c enzyme more active)
3. inhibition (increased drug activity due to no unbound drug).
4. excretion
5. radio
102
____ Effect: when two or more like drugs are combined and the result is the sum of the individual drug's effects. Result is ____.
Additive
| Potentiation
103
____ effect: two or more unlike drugs are used to combine effect; outcome is greater than individual drugs activity alone. Result is ____.
Synergistic
| potentiation
104
_____: describes synergistic interaction with increased drug effect. This applies to both ___ and synergistic. The risk with potentiation is ___.
Potentiation
Additive
toxicity
105
___: affect is opposite of synergistic, therapeutic effect is less than either drug alone b/c 2nd drug either diminishes or cancels the effect of the 1st drug.
Antagonistic
106
____ effect: drugs effect exceeds its therapeutic level from additive or synergistic.
Toxic
107
Drug ____: result in chemical inactivation or physical reaction.
incompatibilities. Example: tetracycline and Dairy
