CH2 Drug Action and Handling Flashcards
1
Q
_______ are designed to do one thing and nothing else
_______ are designed to do lots of different processes
A
- Drugs are designed to do one thing and nothing else
- Vitamins are designed to do lots of different processes
2
Q
Notes
A
- Dose effect curve
- Log dose-effect curve
- median effective dose, 50 % good, 50% no effect –> starting dose
- Potency: how many mg do you need to make something happen?
- Drug A vs drug B comparison –> both are equally efficacy… efficatious????
- Asparin: least potent (see chart)
- Which is least efficatious? Aspirin
- Which is the most potent? Morphine
- Which is most efficatious? Morphine, Demerol, Aspirin are all efficatious (See chart)
3
Q
Notes
A
- Median LD50, 50% great, 50% not so great
- We figure this out because we want to know what will kill you verses what will help
- Therapeutic Index, ratio of what will kill people 50% of the time/50% kill them
- ED50 vs LD50, the broader the spread between these two drugs the safer the drug (See TI chart)
- The bigger the TI the safer the drug
- (Next week start is Mechanism of drugs)
4
Q
Drugs are differentiated from inert chemicals, or chemicals necessary for ____ processes (such as vitamins).
A
life
5
Q
Drugs have the ability to act _____ in biologic systems to accomplish a desired effect.
A
selectively
6
Q
When drugs exert effects on _____ systems, we can ____ the response to the dose of the drug given.
A
biologic; measure
7
Q
If we plot the relationship of the dose of a drug vs. the intensity of the effect on a graph, we get a ______ curve.
A
dose-effect
8
Q
From the _____ effect curve, we may determine a drug’s relative potency and efficacy as compared to other similar drugs.
A
log-dose
9
Q
______ is a function of the amount of drug (the dose) needed to produce an effect.
A
Potency
10
Q
If drug A requires a smaller dose than drug B to produce the same effect, then drug A is more _____ than drug B.
A
potent
11
Q
______ is the maximum intensity of effect that can be produced by a drug, regardless of the dose.
A
Efficacy
12
Q
Once a specific dose produces the maximum effect, giving higher doses beyond that dose does not increase ______.
A
efficacy
13
Q
After the “______”, increasing the dose only increases the probability of adverse effects.
A
plateau
14
Q
According to the theraputic index, the dose required to produce a specified intensity of effect in 50% of the test subjects is termed the ________ (ED50)
A
Median Effective Dose
15
Q
The dose required to produce death in 50% of the test subjects is termed ______ (LD50)
A
Median Lethal Dose
16
Q
The ratio of a drug’s LD50 to its ED50 is known as the _______ (TI).
A
Therapeutic Index
17
Q
If the value of the TI is small (a “narrow TI”), then toxicity with the use of that drug is more ____ (monitor closely).
A
likely
18
Q
If the value of the TI is large ( a “wide TI”), then the drug will be considered ____ to use.
A
safer
19
Q
Drugs do not impart a new function to the organism but merely produce the same action as, or block the action of, an agent that already exists in the body is termed the ______
A
Mechanism of Action of Drugs
20
Q
Stimulation of receptors on a nerve generates an ______ and keeps the impulse going.
A
action potential
21
Q
Drugs may facilitate the action potential and _____ the impulse during its transmission from nerve to nerve (via neurotransmitters) and its final destination (the effector organ).
A
amplify
22
Q
Drugs may also ______ with the action potential and ____ or block the impulse during its transmission from nerve to nerve and its final destination.
A
interfere; weaken
23
Q
_____ are chemical structures that interact with both naturally occurring (endogenous) substances and drugs.
A
Receptors
24
Q
Interaction between receptors and drugs results in either _______ change or _____ of a secondary messenge
A
Conformation shape; release
25
\_\_\_\_\_\_\_\_: Allows the drug inside the cell to produce the effect
(Topic:Drug-Receptor Interaction)
Conformation shape change
26
\_\_\_\_\_\_\_\_: This messenger produces the effect
(Topic:Drug-Receptor Interaction)
Release of a secondary messenger
27
When a drug combines with a receptor, the end result is an ______ in function.
alteration
28
***A drug when producing an enhancement of the function is known as an \_\_\_\_\_\_\_***
***agonist***
29
***A drug when inhibiting a function is known as an \_\_\_\_\_\_\_.***
***antagonist***
30
***\_\_\_\_\_\_\_\_ counteract the action of agonists***
***Antagonists***
31
\_\_\_\_\_\_\_\_\_ (compete with agonists) bind to receptors but produce **NO** effect.
• With increased concentration of the \_\_\_\_\_, the competitive antagonist can be overcome.
(an antidote exists)
Ex: epinepherine vs. beta blocker
Competitive antagonists; agonist
32
\_\_\_\_\_\_\_\_ is the study of how a drug enters the body, circulates within the body and leaves the body and what factors influence its movements.
Pharmacokinetics
33
***Four major steps in the body's handling of a drug: “ADME”***
1. ***Absorption***
2. ***Distribution***
3. ***Metabolism***
4. ***Excretion***
34
The ________ of a drug affects both the onset and duration of drug activity.
route of administration
35
\_\_\_\_\_\_\_\_: The time it takes for the drug to have an effect
Onset of drug activity
36
\_\_\_\_\_\_\_: The length of time the drug continues to have an effect
Duration of drug activity
37
***Drugs may be given by ______ of administration in which the drug is placed directly in the GI tract.***
***enteral routes***
38
***The _____ and _____ are enteral routes of administration.***
***Oral route: Rectal route***
39
Advantages of the oral route administration:
1. ***\_\_\_\_\_ and simplest way to introduce a drug***
2. ______ and most convenient
3. _______ for absorption in small intestine
1. ***Safest***
2. Least expensive
3. Large area
40
Disadvantages of the oral route administration.
1. ______ onset of action
2. ______ can alter absorption
3. ***\_\_\_\_\_\_ blood levels than other routes***
4. Drugs may be ______ in GI tract (ie. insulin)
1. Slower
2. Food/pathology
3. ***Less predictable***
4. inactivated
41
***Advantages of Rectal route of administration***
1. ***Allows use of different dosage _____ –Suppositories, creams, enemas***
2. ***Used if patient is _____ or unconscious. –Used for local and systemic effects.***
1. ***forms***
2. ***vomiting***
42
Disadvantages of enteral route of administration:
1. Poor and/or irregular \_\_\_\_\_\_.
2. Poor patient \_\_\_\_\_\_
1. absorption
2. acceptance
43
***Drugs given by ________ routes of administration in which the drug bypasses the gastrointestinal tract.***
***parental***
44
***All of the following are examples of \_\_\_\_\_.***
* ***Intravenous (IV)***
* ***Intramuscular (IM)***
* ***Subcutaneous (SC)***
* ***Intradermal (ID)***
* ***Intrathecal (IT)***
* ***Intraperitoneal (IP) – Inhalation (IH)***
* ***Topical***
***Parenteral routes of drug administration***
45
***General Advantages fo Parenteral Routes of Administration are:***
1. ***\_\_\_\_\_\_\_, more predictable response***
2. ***Used for drugs which are _____ by GI tract – Used in emergencies, unconsciousness, nausea***
1. ***Rapid onset***
2. ***inactivated***
46
General disadvantages of Parenteral Routes of Administration:
1. ______ (if applicable) must be maintained
2. Administration may be more difficult or \_\_\_\_\_
3. ***Difficult to _____ the drug once administered***
1. Asepsis
2. painful
3. ***remove***
47
***Parenteral routes of administration may be _____ or \_\_\_\_\_\_\_\_.***
***topical; systemic***
48
Topical route is administration for _____ effects
1. _____ (steroid creams, anesthetic patches)
2. _____ (strips, chips and gels)
3. \_\_\_\_\_, ears, nose, throat (drops and sprays)
local
1. Skin
2. Subgingival
3. Eyes
49
Administration for systemic effects examples:
1. _____ (transdermal patches)
2. \_\_\_\_\_, buccal and translingual (nitroglycerin)
1. Skin
2. Sublingual
50
\_\_\_\_\_\_\_\_: As a drug is absorbed, distributed, metabolized and excreted, it must pass through various membranes
Drug-Membrane Transport
51
The ______ of drug that passes through a membrane and the _____ at which the drug passes are important.
amount; rate
52
The Drug-Membrane Transport helps determine the\_\_\_\_ and ____ of activity of the drug as well as any variation in individual response to the drug.
onset; duration
53
Name the three Physico-chemical factors that influence the passage of a drug across our body membranes:
1. Solubility (Water or Lipid)
2. Degree of ionization
3. pH
54
Lipid-soluble drugs easily move across body
membranes by _____ directly proportional to concentration gradient and degree of lipid solubility.
simple diffusion
55
\_\_\_\_\_ lipid soluble compounds attain high concentrations at the membrane and readily move across the membrane (from area of high concentration to area of low concentration).
Highly
56
Drugs that are weak _____ dissociate in solution and equilibrate into a non-ionized form and an ionized form.
electrolytes
57
The _____ form acts like a lipid-soluble compound and readily crosses body membranes
non-ionized
58
The\_\_\_\_\_ form acts like a water-soluble compound and crosses body membranes with difficulty
ionized
59
\_\_\_\_\_\_: The transfer of a drug from the route of administration to the systemic circulation.
Absorption
60
These factors should be considered for absorption at the site of administration:
1. Surface area
2. Blood perfusion
3. Membrane pH
61
\_\_\_\_\_\_ is the transfer of a drug from the site of absorption to the body tissues and ultimate site of action. The route of administration, membrane permeability and drug solubility must be taken into consideration.
Distribution
62
\_\_\_\_\_\_: Transformation of a drug from a lipid-soluble form to a more water-soluble form
Metabolism
63
Factors to consider for Metabolism:
1. Hepatic portal
2. Hepatic pathology effecting liver function
3. Age
4. Mechanisms of metabolism.
5. Drug Half-life
6. First-order kinetics
64
***What are the different mechanisms of metabolism?***
***1. Active to Inactive***
***2. Inactive to Active***
***3. Active to Active***
65
***\_\_\_\_ is when an active parent drug is transformed into an***
***inactive compound. It is the most common type of drug metabolism.***
***Active to inactive metabolism***
66
***\_\_\_\_\_\_ occurs when an inactive parent drug (prodrug) is***
***transformed into an active compound.***
***Inactive to Active***
67
***An _______ mechanism of metabolism occurs when an active parent drug is converted to a second active compound (active metabolite).***
***(Hint: this drug remains in its fat soluble state, is long lasting, and passes through the liver several times.***
***Active to active***
68
***A ______ is the time required for a drug’s concentration in***
***the blood to fall to half of its original level.***
***drug half-life***
69
***A drug’s half-life is determined by whether it exhibits _____ or ____ as it is metabolized.***
***• First-order kinetics***
***• Zero-order kinetics***
70
***Drugs that fall under the catergory of _____ have a constant half-life regardless of the dose administered. In other words the ____ percent of drug is eliminated per unit of time.***
***first-order kinetics; same***
71
***A ________ drug has a half-life that can vary based upon the***
***dose of drug administered.***
***Zero-order kinetics***
72
Good to know:
For some substances, the same amount of drug is eliminated per unit time. What this means is that with some drugs the liver enzyme systems can become saturated (overwhelmed). In these cases, the administration of a relatively large dose can lead to prolonged metabolism, prolonged activity and adverse effects.
This describes \_\_\_-order kinetics
Zero
73
Good to know:
Weight, age lifestyle, medications, and health status are all important to keep in mind when reviewing a health history.
Always keep in mind that not everyones liver functions the way that you think.
Good to know
74
***\_\_\_\_\_\_ is the elimination of a drug and/or its metabolites from the body.***
***Excretion***
75
What are the factors to consider with excretion?
HINT: involves the kidneys
-**Glomerular filtration**
## Footnote
(kidneys filter excess fluid & waste from blood)
**-Active tubular secretion**
(transfer of materials from peritubular capillaries to the renal tubular lumen with energy)
**-Passive tubular diffusion**
(transfer of materials from peritubular capillaries to the renal tubular lumen without energy)
76
***What are the five extra-renal routes of excretion?***
***Lungs***
***Bile***
***Mammary glands***
***Saliva***
***GCF***
77
Gases are excreted across the ____ tissue by simple diffusion (i.e. general anesthesia).
lung
78
Systemically absorbed drugs are secreted into the ___ and are eliminated in the feces.
bile
79
Drugs are excreted into breast milk through \_\_\_\_\_.
mammary glands
80
Drugs are secreted into the \_\_\_\_\_, swallowed and placed in the GI tract again (reciprocal absorption)
saliva
81
The excretion of \_\_\_\_\_is used in dentistry in treating periodontal disease
GCF (Gingival Crevecular Fluid)
82
What are the drug interactions/drug-food interactions during absorption?
**Effects on microflora:** Antibiotics and oral contraceptives
**Effects of chelation:** Tetracyclines and dairy products
83
What are the drug interactions/drug-food interactions during distribution?
Effects on plasma protein binding sites: Coumadin (warfarin) and aspirin
84
***What are the drug interactions/drug-food interactions during metabolism?***
***Liver enzyme induction: Dilantin (phenytoin), cigarette smoke***
***(speeds up liver function)***
85
What are the drug interactions/drug-food interactions during excretion?
Competition for excretion routes: Penicillin and methotrexate
86
***How should you determine the appropriate child's dose using Clarks Rule?***
***weight (lb) x Adult dose/150***
87
Good to know.
99% of the drug coumadin dose is absorbed in muscle. To counter this, the dosage has been increased. When Asprin is used in conjunction with coumadin, it extracts some of the absorbed coumadin from the muscle potentially causing an overdose.
Good to know.
88
When might a patient taking warfarin also take an aspirin?
this might occur in an older patient who takes a baby asprin a day in addition to a blood thinner. This is DANGEROUS
89
***What natual food causes medication to stay in your liver longer by slowing down liver function?***
***grapefruit juice***
90
Stimulating beta-2 receptors ONLY would result in which of the following?
a. increased salivation
b. decreased BP
c. bronchodilation
d. decreased heart rate
c.bronchodilation
91
The generic name is the name given to an approved drug by the pharmaceutical company that developed it.
True
False
False
92
Ionized compounds ( possessing a charge) are lipid soluble and easily passed through the bodies membranes.
True
False
False
93
Orally administered drugs are distributed to the liver first and are metabolized and inactivated to some extent before they reach general circulation and their intended sites of action. this effect is known as?
A) First-pass
B) Second-pass
C) Third-pass
D) Fourth-pass
A) First-pass
94
If drug A requires a smaller dose than drug B to produce 50% of the maximum effect, then drug A is less potent than drug B
True
False
False
95
Drugs work by imparting a new function to the host organism,a function that did not exist prior to the administration of the drug.
True
False
False
96
Which of the following government agencies requires quality standards in a drug manufacturing plants and determines what drugs may be sold only by prescription?
FDA
97
If an infant weighs 10 lbs and if the adult dose is 30 mg,according to clark's rule,the dose of the drug for the infant should be?
2mg
98
Which of the following is false when concerning routes of drug administration?
A) One disadvantage of IV is drug irretrievability
B) The rectal route is the most convenient way to introduce a drug for systemic effects
C) Topical applications are administered to the skin, oral mucosa,and also sublingually
D) None
B) The rectal route is the most convenient way to introduce a drug for systemic effects
99
Cardiovascular disease is complicated by the presence of co-morbid disease, such as diabetes hyperlipidemia
True
False
True
100
During first order kinetics, the same percent of drug is eliminated per unit time.
True
False
True
101
In one mechanism by which drugs are metabolized , an inactive parent drug may be transformed into an active compound . The inactive parent drug is called?
A) metabolite
B) inducer
C) inhibitor
D) prodrug
E) none
D) prodrug
102
Which of the following is false concerning the oral route of drug administration?
A) least expensive and most convenient route of administration.
B) safest and simplest way to introduce a drug to the body
C) more predictable blood vessels than other routes of administration.
D) large area if absorption in the small intestine.
E) none
C) more predictable blood vessels than other routes of administration.
103
The route of administration of a drug affects both the onset and duration of the response?
True
False
True
104
The median dose effect (ED50) is the dose of drug required to produce a specified intensity of effect in 50%of the test subjects.
True
False
True
105
The LD50 is the dose of a drug required to produce death in 50% of the test subjects.
True
False
True
106
In one mechanism by which drugs are metabolized, an active parent drug may be transformed into yet another active compound. This new compound is called an active metabolite.
True
False
True
107
***Four major steps in the body's handling of a drug: “ADME”***
1. ***Absorption***
2. ***Distribution***
3. ***Metabolism***
4. ***Excretion***
