Pharm Ch 1

0.0(0)
learnLearn
examPractice Test
spaced repetitionSpaced Repetition
heart puzzleMatch
flashcardsFlashcards
Card Sorting

1/202

flashcard set

Earn XP

Description and Tags

Biology

Study Analytics
Name
Mastery
Learn
Test
Matching
Spaced

No study sessions yet.

203 Terms

1
New cards
How does a student develop a "story" about a drug, rather than try to memorize isolated facts about every single drug?
Associate, Ask, Predict
2
New cards
What does "Associate" mean, regarding a drug's story?
Associate each drug class with info you already know.
3
New cards
What does "Ask" mean, regarding a drug's story?
Ask yourself why some drugs are shots and others are pills, why some are taken 4x and some 2x per day, and why the info is important enough to be in the book.
4
New cards
What does "Predict" mean, regarding a drug's story?
Predict the actions, clinical uses, side effects, and drug interactions based only on its mechanism of action.
5
New cards
What should you envision about a drug?
Envision the course of events that would occur as it enters the body.
6
New cards
What does "formulation" mean?
The drug preparations made by companies that can be administered orally, i.v., or another route.
7
New cards
What are the 5 factors that the drug formulation depends on?
"The barriers the drug can pass. The setting in which the drug will be used. The urgency of the medical situation. The stability of the drug. The first pass effect."
8
New cards
What are barriers that drugs must pass?
Any anatomical structure they must get through in order to reach the bloodstream or target area. IV drugs have no barriers, but pills must pass through the GI tract and the blood vessel wall to get to the blood.
9
New cards
What are some settings in which drugs can be used?
Hospital vs. home
10
New cards
What setting is appropriate to administer an IV?
Hospital
11
New cards
What drugs can be administered in a home setting?
Pills (aspirin)
12
New cards
Why are drug formulations selected based on medical urgency?
The delay before onset of action varies; an IV antibiotic works faster than the same drug administered orally.
13
New cards
How are drug formulations affected by the stability of the drug?
Drugs that are destroyed by acid (such as the proteins found in insulin for diabetics) are not effective if taken orally because of stomach acid
14
New cards
What is the first pass effect?
Oral medicines are absorbed into the portal vein, which goes to the liver before being distributed to the body. The liver deactivates many medicines during this first pass, so they cannot be taken orally.
15
New cards
Name 9 routes of drug administration and their medical abbreviations
Oral (PO)
Sublingual, Rectal (PR)
Inhalation
Topical
Transdermal
Intravenous (IV)
Intramuscular (IM)
Subcutaneous (SubQ or SC)"
16
New cards
Which 5 routes of administration are most compatible with drugs that are self-administered?
Oral (PO)
sublingual
inhalation
topical
transdermal
17
New cards
What two problems must oral drugs be able to overcome?
Gastric acidity and must permeate the gut lining
18
New cards
Oral drugs are affected by what two things?
Gastric emptying and intestinal motility
19
New cards
What is the key feature that allows a drug to be administered by the sublingual route?
Must have good absorption through the capillary bed under the tongue.
20
New cards
What is the advantage of sublingual drugs over oral drugs?
Gastric acidity and gut-permeability are not needed.
21
New cards
When are rectal drugs mainly used?
For unconscious or vomiting patients or small children.
22
New cards
What is the problem with the rectal route?
Absorption is unreliable
23
New cards
Can topical drugs be administered systematically?
No, they are usually toxic except for topical use
24
New cards
Topical agents can be applied to what parts of the body?
Skin, eyes, nose, vagina, ears
25
New cards
What is a transdermal patch?
The drug is on a patch that is applied to the skin, and it is able to penetrate to the dermis to be absorbed in the blood vessels there. Few drugs are capable of using this route.
26
New cards
What does "parenteral" refer to?
Drugs that are administered in ways other than the gastro-intestinal tract.
27
New cards
What are the 3 advantages of parenteral drugs?
"More rapid absorption
More predictable absorption
More accurate dose selection"
28
New cards
What are the 4 disadvantages of parenteral drugs?
"Need for strict asepsis
Risk of infection
Pain
Local irritation"
29
New cards
What are the 3 parenteral routes of administration?
"Intravenous (IV)
Intramuscular (IM)
Subcutaneous (SubQ, SC)"
30
New cards
What are the advantages of IV drugs?
"Rapid onset of action, Useful in emergencies, Useful for unconscious patients"
31
New cards
What is a disadvantage that is unique to IV drugs?
Drug must be soluble in water to be used as an IV drug.
32
New cards
What factor influences the rate of absorption of Intramuscular (IM) and SubQ drugs?
"Oil-based preparations are absorbed slowly
Aqueous preparations are absorbed rapidly"
33
New cards
What is a disadvantage that is unique to SubQ drugs?
Only non-irritating drugs can be used.
34
New cards
What is the half-life of a drug?
The amount of time required for the blood concentration of a drug to decrease by 50% after the drug administration has stopped.
35
New cards
What does the distribution half-life reflect?
The rapid decline in plasma drug concentration as a dose of drug is distributed throughout the body.
36
New cards
What is the speed of the elimination half-life of a drug?
It is much slower, reflecting the metabolism and excretion of the drug.
37
New cards
How many half-lives pass before the serum concentration of a drug reaches steady state?
Several
38
New cards
How long do you have to wait before you can draw blood to measure the peak, trough or plasma levels of a drug?
Wait until the 4th or 5th half-life
39
New cards
If the half-life of a drug is 4 hours, how many hours do you have to wait before measuring its level in the blood?
After 4 hours, 50% of the drug will be left in the body (first half-life); it will take four more hours to metabolize 50% of the remaining drug; the body will now have 25% of the original dose remaining. After the 3rd half-life, the body will have 12.5% of the drug left. After the 4th half-life there will be 6.25% left, and 16 hours will have passed. Draw blood at 16-20 hours after drug administration to measure within the 4th - 5th half-life.
40
New cards
How can therapeutic levels of a drug be obtained more rapidly?
By delivering a loading dose followed by maintenance doses.
41
New cards
What is a loading dose?
An initial dose of drug that is higher than subsequent doses.
42
New cards
What is a maintenance dose?
The doses of drug that maintain a steady state plasma concentration in the therapeutic range.
43
New cards
What is a dosing regimen?
Route
amount
frequency the drug is given
44
New cards
What influences the onset and duration of drug action?
The dosing regimen
45
New cards
What is the onset of a drug?
The amount of time it takes a drug to begin working.
46
New cards
What routes have the fastest and slowest onset?
IV drugs are fastest onset
oral drugs are slowest
47
New cards
What is the duration of a drug?
The length of time for which a drug is therapeutic.
48
New cards
What does the duration of a drug usually correspond to?
The half-life of the drug
49
New cards
When would the duration of a drug not correspond to its half-life?
When the drug binds irreversibly to its receptor
50
New cards
What is the duration of a drug dependent upon?
The metabolism and excretion of the drug.
51
New cards
Will increasing the rate of IV infusion decrease the time needed to reach steady state?
No; it always takes 4-5 half-lives of continuous IV infusion to reach steady state.
52
New cards
Will increasing the rate of IV infusion increase the plasma drug concentration at steady state?
Yes (see page 3 in book if you bought it). Instead of administering x-mg per hour, increasing infusion to 2x-mg will result in drug concentration being doubled at steady state (when the graph levels off)
53
New cards
What is the peak and trough of a drug?
When a drug is administered intermittently, there will be peaks (high points of fluctuation) and troughs (low points of fluctuation) See page 3 in book
54
New cards
Are toxic effects most likely to occur during peaks or troughs?
Peaks
55
New cards
Is lack of drug effects more likely to occur during peaks or troughs?
Troughs
56
New cards
Is post-operative pain more likely to return just before a second dose of morphine or midway between the first and second dose?
Just before the second dose
57
New cards
What does pharmacotherapeutic mean?
What the drug is used for
58
New cards
What does pharmacodynamics mean?
How the drug affects the organism
59
New cards
What does pharmacokinetics mean?
How the organism affects the drug (duration of the drug)
60
New cards
What are the 4 phases in pharmacokinetics, in order?
"Absorption
Distribution
Metabolism
Excretion/Clearance"
61
New cards
What are four transport mechanisms that a drug can use to cross membranes?
"Passive diffusion
Facilitated diffusion
Aqueous channels
Active transport"
62
New cards
In which of the four transport mechanisms is energy used?
Active transport
63
New cards
In which of the four transport mechanisms is a carrier protein needed?
"Facilitated diffusion
Active transport"
64
New cards
What are the 4 drug-associated factors that influence absorption?
"Ionization state
Molecular weight
Solubility (water vs lipid soluble)
Formulation (solution vs tablet)"
65
New cards
What is the patient-associated factor that influences drug absorption?
Depends on route of administration
66
New cards
Regarding patient-associated factors that influence absorption: What are 3 ways that absorption of oral medicines is affected by the patient?
"The presence of food in the GI tract slow absorption of oral meds.
Excess or decreased stomach acidity affects absorption of oral meds.
Decreased blood flow to the GI tract slows absorption of oral meds."
67
New cards
What are 3 things that affect drug distribution?
"Membrane permeability
Plasma protein binding
Depot storage"
68
New cards
For a drug to enter an organ, what must the drug do?
It must permeate all membranes that separate that organ from the site of drug administration.
69
New cards
What is the Blood-Brain Barrier (BBB)?
The brain has protective cells that do not let most drugs through. That limits the number of drugs available to treat brain and spinal cord disorders, including anxiety and convulsions.
70
New cards
What common medicine for anxiety and convulsions can cross the BBB?
Benzodiazepines (valium)
71
New cards
What two areas of the body have membranes that many anti-cancer drugs cannot cross?
Brain and testes
72
New cards
What reduces the amount of free (unbound) drug in the blood?
Plasma proteins that bind to the drugs, such as albumin.
73
New cards
What molecules reach equilibrium between the blood and tissues?
Free (unbound) drugs
74
New cards
How does a decrease in free drug in the serum (because it is bound) affect the target organ?
It causes a decrease in the amount of the drug that can enter the target organ.
75
New cards
What does depot storage mean?
The location in the body where the drug accumulates
76
New cards
What is an example of a lipophilic drug that is a sedative used during surgery?
thiopental
77
New cards
How does the weight of the patient affect lipophilic drugs?
An obese patient will feel the sedation effects of thiopental for a longer time after administration
78
New cards
What is an example of a calcium-binding antibiotic? Where does it accumulate?
Tetracycline; it accumulates in the bones and teeth.
79
New cards
What is the meaning of "apparent" volume of distribution (Vd)?
It is a calculated value that describes the nature of drug distribution.
80
New cards
What does volume distribution (Vd) mean?
The volume that would be required to contain the administered dose if that does was evenly distributed at the concentration measured in plasma.
81
New cards
Where would you predict a drug is located if it has a (Vd) of 3-5 liters?
Since there are only 5 liters of blood in the body, this drug is probably 100% in the plasma
82
New cards
Where would you predict a drug is located if it has a (Vd) of 16 liters?
It is likely distributed in plasma plus interstitial fluid.
83
New cards
Where would you predict a drug is located if it has a (Vd) of 50 liters?
It is likely sequestered in a depot because the body only contains about 40-46 liters of fluid.
84
New cards
What has to happen to most drugs before they can be excreted?
They must be biotransformed, or metabolized
85
New cards
In pharmacology, what does "metabolism" refer to?
Making a drug more polar (water soluble)
86
New cards
When a drug is rendered water soluble, what does it often result in?
It often results in drug inactivation (but not always)
87
New cards
What is a parent drug and a metabolite?
The parent drug is the one that is administered. The metabolite is the one that the body renders water soluble.
88
New cards
Is a metabolite less active or more easily excreted then the parent drug?
Not necessarily
89
New cards
What two things can be transformed by metabolic reactions?
"Active drug → less active or inactive drug
Less active or inactive drug→ More active drug"
90
New cards
What is a ProDrug?
An inactive or less-active drug
91
New cards
Drug and toxin metabolism is divided into what two reactions?
Phase I and Phase II
92
New cards
What happens in Phase I reactions?
Drugs are oxidized or reduced (H+ is taken off or added) to make them more polar.
93
New cards
What happens in Phase II reactions?
A Polar group, such as glutathione, is conjugated to the drug, which makes it more polar.
94
New cards
What system in the liver is responsible for the metabolism of most drugs?
The P450 system
95
New cards
How does Phase I occur in the liver?
Cytochrome P450 (absorbs light at 450 nm) is an enzyme in the liver cells. Through the electron transport chain, a drug bound to cytochrome P450 can be oxidized (lose a H+) or reduced (gain a H+). The H+ comes from NADPH.
96
New cards
What happens when a drug enters the body that can be metabolized by P450?
Cytochrome P450 is induced (increases in amount and activity) to handle the chemical load
97
New cards
What happens when a person has been on one drug for a while, and then an additional new drug is administered?
Cytochrome P450 production is increased, which works to inactivate the new drug, and the leftover enzyme will also deactivate more of the old drug. So the effectiveness of the old drug decreases.
98
New cards
What is a common example of P450 induction?
Alcohol tolerance. At first, two drinks make the person tipsy. But when drinking frequently, P450 metabolizes the alcohol faster, so it takes more alcohol to feel the effect.
99
New cards
How does daily alcohol consumption affect the effectiveness of other drugs?
Cytochrome P450 induction has occurred from the alcohol, so the enzyme will degrade other drugs faster than someone who drinks less frequently. So they need a higher dose of medicines.
100
New cards
How is patient safety affected by the percentage of drug that binds to plasma proteins like albumin?
If a drug is mostly bound by albumin, there is very little in free form, which is the form that causes the effect. Giving an additional drug that displaces the first drug from albumin will cause more of the first drug to be in free form, which might be toxic. See picture page 5 of book.