Principles of Pharmacology Flashcards
1
Q
the legal right to prescribe drugs
A
prescriptive authority
2
Q
prescriptive authority for APRNs is determined by ____
A
state of residence/practice
3
Q
Schedule ___ - ____ controlled substances are included in TN APRN prescriptive authority
A
II-V
4
Q
TN Requirement for controlled substances prescription by APRNs
A
DEA #
5
Q
Rank of Quality of Evidence
A
- Systemic Reviews
- Critically-Appraised Topics/Articles
- RCTs
- Cohort Studies
- Case-Controlled Studies, Case Series, Reports
- Background Info/Expert Opinion
6
Q
how the drug moves through the body and what the body does to the drug
A
pharmacokinetics
7
Q
the progress of a drug from administration through the time it passes to the tissues until it becomes available for use by the body
A
absorption
8
Q
What determines route of the drug?
A
absorption and distribution
9
Q
Factors that affect ________:
route of administration
amount of blood flow
drug form
A
absorption
10
Q
_____ and _____ are the fastest oral administrations
A
buccal and sublingual
11
Q
rate and extent to which a drug enters the circulation and gains access to target tissue
● When a drug is dissolved, doesn’t survive liver passage, a fraction gets to the bloodstream → need for higher doses
● “What makes it to the bloodstream”
A
Bioavailability
12
Q
the speed of bloodstream entry affects max blood level after admin; rapid absorption increases this
A
peak blood level
13
Q
rapid absorption causes ______ peak blood level so APRN needs to consider this with ______ drugs
A
increases; IV push drugs
14
Q
____ membranes are easier for drugs to cross and cross the blood-brain barrier
A
lipid
15
Q
whether or not a drug binds and becomes inactive; drug action occurs through free, unbound drug
A
protein-binding
16
Q
(many in the liver) help normalize concentrations throughout the body, altered by disease states; in the plasma and encourages drug retention in systemic circulation→ appearance of high drug levels but it is not at the active site; binding is the basis for several drug interactions; cannot interact with their receptor; if strongly bound a small change in binding can → significant effects
A
plasma proteins
17
Q
hypothetical value that reflects the volume in which a drug would need to be dissolved to explain the relationship between dosage and blood levels.Tells where a drug might be distributed
A
volume distribution
18
Q
Drug that produces an effect similar to those produced by naturally occurring hormones, neurotransmitters, and other substances. Drug that interacts with receptors; has an attraction/affinity for receptor and stimulates it. A chemical that binds to a receptor andsdf activates the receptor to produce a biological response. Intrinsic activity: drug’s ability to initiate a response after receptor binding
A
agonists
19
Q
type of agonist that don’t need all available receptors to illicit max response, spare receptors are left over, not needed
A
full agonist
20
Q
bind and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist, even at maximal receptor occupancy.; between agonist/antagonist; max response < full agonist
A
partial agonist
21
Q
3 ways drugs pass across membranes:
A
- Channels/Pores
- Transport Systems (p-glycoproteins)
- Direct Penetration
22
Q
Transmembrane protein that transports a wide variety of drugs out of cells
A
P-Glycoprotein
23
Q
For most drugs, movement throughout the body is dependent on the drug’s ability to ________
A
directly penetrate membranes
24
Q
to directly penetrate membranes, a drug must be _____
A
lipophilic (lipid soluble)
25
Molecules that contain at least one atom of nitrogen and carry a positive charge at all times
Quaternary ammonium compounds
26
Acid is a proton donor: Tends to ionize in basic (alkaline) media
Base is a proton acceptor: Tends to ionize in acidic media
pH-dependent ionization
27
Acidic drugs accumulate on the alkaline side
| Basic drugs accumulate on the acidic side
Ion trapping (pH partitioning)
28
```
Factors affecting ______:
Rate of dissolution
Surface area
Blood flow
Lipid solubility
pH partitioning
```
absorption
29
Factors determining _____:
Blood flow to tissues
Exiting the vascular system
Entering cells
Distribution
30
drug has an affinity for receptor but displays little or no intrinsic activity, prevents the response from occurring. Chemical that binds to a receptor & blocks the action of the agonist
antagonist
31
type of antagonist that competes with agonist for receptor sites; binds reversibly to the receptor site; large agonist doses can overcome antagonist effect; agonist cannot bind to the receptor because the competitive antagonist is bound to the binding site where the agonist would have binded to.
competitive antagonist
32
type of antagonist that binds to receptor and blocks agonist effects; can’t reverse with large agonist dose.
Bind to the receptor somewhere else than the agonist binding site
noncompetitive antagonist
33
type of antagonist that binds directly to the agonist and prevents it from binding to the receptor.
Ex; heparin would be an agonist that is a blood thinner, and protamine binds directly to heparin that prevents it from working.
chemical antagonist
34
biotransformation, refers to body’s ability to change drug from dosage form to ↑water soluble form that can be excreted; several ways metabolized- into inactive metabolites (products) that are then excreted, conversion to active metabolites that can exert their own pharm action; prodrugs don’t become active until metabolized; most drugs metabolized by liver
metabolism
35
```
Factors affecting ______:
↓ by certain diseases
genetics
environment
development/age
```
metabolism
36
“family” of enzymes, each responsible for single type of metabolic reaction; most thoroughly studied drug metabolism reaction; catalyzes metabolism of a large variety of meds
CYP450
37
drugs that cause CYP450 to induce metabolism
inducers
38
Example of _______:
Tegetrol induces the CYP450 system which ↑ Metabolism of estrogen, which ↓ blood levels of estrogen & this could increase chance of pregnancy due to ↓ in contraceptive effect.
Inducer drug
39
drugs that cause CYP450 to inhibit metabolism
inhibitors
40
Example of ______:
Erythromycin inhibits the CYP450 system which reduces the metabolism of drugs. If you have decreased metabolism than drugs can build up in the system causing toxicity.
Inhibitor drug
41
Effect when _______:
competition occurs when two different drugs are metabolized by the same enzyme; often the enzyme can metabolize both drugs, sometimes one drug will be preferentially metabolized, delaying the metabolism and extending the half life of the competing drug
2 drugs use the same pathway
42
drugs induce CYP450 by causing an increased amount of CYP450 enzymes; this results in increased metabolism of the drug, therefore, decreased pharmacological effect of the drug; "enzyme increasers"
Enzyme Induction
43
substances that block the enzyme system which increases the pharmacological activity of the drug and other drugs. Grapefruit juice prevents enzymes in GI tract from breaking down other drugs and so other drugs end up having increased actions
Other EX: depakote, diflucan, tagamet, alcohol/binge drinking, cipro, flagyl, prilosec,sulfonamides, erythromycin
Enzyme Inhibitor
44
drugs that can be administered as inactive drugs; don’t become active until they’re metabolized
prodrug
45
drug that increases metabolism and the need for an increased dosage of the drug to be effective.
ultra-rapid metabolizer
46
extra gain function alleles produce lots of enzyme to metabolize the drug → drug being gone quickly → ↓ area under the curve (AUC), ↓side effects, ↓ possibility of cure
active drugs
47
extra gain function alleles produce lots of enzyme to metabolize the drug → drug active quickly
prodrug
48
normal functioning alleles produce enzymes to metabolize drug; active → drug gone; prodrug→ drug active
extensive metabolizer
49
: one functioning allele, one loss of function allele. May lead to excessive accumulation of the metabolite (also resulting in toxic levels)
intermediate metabolizer
50
can cause accumulation of the drug and potentially toxic levels and therefore, the need for a reduced dosage.
○ Active→ two loss of functioning alleles produce little of no enzyme to metabolize drug → drug keeps hanging out → ↑AUC, ↑side effects, ↑possibility of cure, ↑risk for toxicity
○ Prodrug→ may fail to become active; ↓side effects because it lacks action
poor/intermediate (slow) metabolizer
51
metabolism by the liver following oral administration; liver contains high amounts of drug metabolizing enzymes and because it is the first organ encountered by drugs once absorbed from the GI tract
Hepatic First-Pass
52
Time it takes for plasma concentration of drug to fall to half of original values; for half of drug to be eliminated; knowing it helps determine how frequently drug should be taken
● Factors: rates of absorption, metabolism, and excretion
Half-Life (Dosing Intervals)
53
a drug given only once is eliminated almost completely after 4-5 half-lives; if administered at regular intervals it reaches a steady concentration/state after about 4-5 half lives; steady state occurs when the rate of administration = rate of excretion
Intervals
54
efficacy is the expression of the maximum effect a drug can produce, ability of a drug to produce a maximum effect at any dosage; example: stronger drugs for pain → higher efficacy
Maximal efficacy
55
more easily and cross blood-brain barrier; consideration for lactation as these can affect quantity and quality of breastmilk; vitamins A, D, E, and K are fat-soluble and deficiency only occurs after prolonged period of deprivation
lipid solubility
56
potency is the expression of how much drug is needed to produce a biological response; describes the difference in concentration or dosage of different drugs required to produce a similar effect; relative potency is used to express the biological activity of a sample preparation compared to a standard preparation
relative potency
57
this type of hypersensitivity respons is antibody mediated, specifically IgE and the products of tissue mast cells and mediated release of histamine from mast cell
Does not occur with the first exposure to a medication. Antibodies are built up and sit on mast cells - and then on next exposures histamine is activated and mast cells rupture
EX: anaphylaxis, hives that are raised/itchy
Type I Hypersensitivity Reaction
58
this type of hypersensitivity response is antibody mediated, specifically IgG and IgM
Type II Hypersensitivity Reaction
59
this type of hypersensitivity response is antibody mediated, specifically IgG and IgM but is NOT TISSUE SPECIFIC
forms large, sticky molecules
Type III Hypersensitivity Reaction
60
this type of hypersensitivity response is cell mediated, specifically T cells, and causes a localized inflammatory reaction; response that has no antibody involvement, only T cells
(from the T-cells found mostly in the skin) or delayed hypersensitivity. Delayed onset from 48-72 hours or up to 1 week in the first exposure but sooner in subsequent exposure
EX: poison ivy...rash, dermatitis,
Type IV Hypersensitivity Reaction
61
drugs that have side effects that can cause significant disabilities in the elderly; cause dry mouth (MANY different drugs)
anticholinergic
62
Risk factors for torsades with ________ drugs:
● Female; advanced age; recent conversion from Afib with these drugs; electrolyte imbalance; especially hypokalemia; hypomagnesemia and hypokalemia; diuretic use (electrolyte imbalances); hepatic and renal dysfunction; bradycardia; underlying heart disease; high drug concentration; digitalis therapy
QT prolonging
63
1. Goal of therapy: what pathology should be altered?
2. Related drug classes: what categories of drugs are available to treat the pathology and how are the categories different?
3. Mechanism of action: how do the different drugs address the pathology?
4. Distinguishing features of specific drugs in the class.
5. How does the drug get in the body? How well is it absorbed?
6. How is the drug distributed and metabolized in the body? What are influencing factors?
7. How does the drug leave the body? Are there issues with clearance or excretion?
8. Safety profile of the chosen drug: Side effects, drug interactions, pregnancy, breastfeeding, patient education for correct use?
Eight Standard Questions for Safe and Effective Prescribing
64
Rx of Schedule ___ Drugs:
No refills, No telephone orders unless true emergency ; f/u with written RX within 7 days, Electronic ok with specific software & secure ID process (Narcotics, Stimulants, Depressants)
II
65
Rx of Schedule ___ Drugs:
RX must be rewritten after 6 months or 5 refills, telephone or fax RX ok
(Narcotics, stimulants, depressants, anabolic steroids, testosterone)
III
66
Rx of Schedule ___ Drugs:
RX must be rewritten after 6 months or 5 refills, telephone or fax RX ok BUT penalties for illegal possession are different
(Pentazocine, phentermine, benzodiazepines, meprobamate)
IV
67
Rx of Schedule ___ Drugs:
Same as all RX drugs, may be dispensed without RX unless regulated by the state
(Loperamide, diphenoxylate, cough meds with <200 mg/100mL Pregabalin
V
68
Process in which the embryo forms develops and undergoes organogenesis.
Embryogensis
69
Examples of _____:
ACE inhibitors, androgens, ABTs (tetracycline, doxycycline, streptomycin, warfarin, methotrexate, anti-thyroid drugs, DES (hormone), statins, accutain, cytotec, alcohol
Drugs to avoid in pregnancy
70
Synthroid (Hypothyroidism) Meds usually need to be ___ in pregnancy
increased
71
Fat-Soluble Vitamins
A, D, E, K
72
Fat-soluble vitamins are stored in the ____ and ___
liver and fatty tissue
73
condition in which a mega dose of fat-soluble vitamin is consumed
hypervitaminosis
74
water-soluble vitamins are largely excreted by ____
the kidney
75
foods that claim to have a medicinal effect on health, also referred to as functional foods. However, they are not interchangeable; functional foods are foods that have health benefits, whereas these include dietary supplements.
nutraceuticals
76
water-soluble vitamins are largely excreted by ____
the kidney
77
Intake of ______ is assoaciated with a statistically significant decrease in levels of fasting plasma glucose, total cholesterol, LDL-C, and triglyceride levels, and an increase in HDL-C levels.
However, it has not been shown to have a significant effect on hemoglobin A1c.
Cinnamon
78
Metformin use & a strict vegan diet can predispose patients to _____ deficiency
B12
79
______-rish foods include dark green vegetables (spinach), dried legumes (chickpeas), and fruits (avocado).
Folic Acid
80
Folic Acid dose to decrease NTD is ____ to _____ mg daily in healthy women and _____ mg daily in women who have had previous birth with NTD and or women with diabetes who could become pregnant.
0.4- 0.8
| 4
81
Which medications are folic acid antagonist and require additional supplementation?
(methotrexate, valproic acid)
82
AACE recommends: _____ to _____ IU of vitamin D daily is required to maintain a 25-OH vitamin D level at 30 ng/ml or above.
1000-2000
83
Sources of ______:
direct sunshine to the bare skin! Also, fatty fish like tuna, mackerel, & salmon, and fortified foods including dairy products, orange juice, soy milk, cereals, cheese, & egg yolks.
Vitamin D
84
Vitamin D is ___ soluble
fat
85
25-OH vitamin D level of between 20 to 50 ng/ml is safe and effective for bone health. However, the AACE recommendation is: it would be appropriate to use a range from ___ to ___ for most patients as an optimal and safe range.
30-50
86
_____ promotes calcium absorption and is essential for normal mineralization of the bone.
It also modulates cell growth, has a role in neuromuscular & immune function, & reduces inflammation
Vitamin D
87
_______ is antithrombotic, anti-inflammatory and hypolipidemic & therefore may help treat & prevent numerous conditions.
Their use in preventing CVD and even reducing cardiovascular events in patients with pre-existing cardiovascular disease has been shown to be likely effective.
Safety shown up to 3 grams daily. Made from young fish, before toxins build-up.
Omega 3 Fatty Acid
88
May be helpful in treating some of the common symptoms seen in IBS such as the abdominal pain or flatulence.
Heartburn is the main adverse effect.
Peppermint Oil
89
Used for numerous gastrointestinal symptoms and are found to be effective for various conditions.
Shown to reduce the risk of antibiotic-associated diarrhea.
***Avoid in those that are immunocompromised.***
Probiotics
90
May be teratogenic if pregnant momma takes more than RDA.
| It is also a fat-soluble vitamin
Vitamin A
91
Fat Soluble Vitamins
A, D, E, K
92
Vitamin C supports the absorption of this.
| It can be tough on the stomach and can be constipating.
Iron
93
Food sources in addition to dairy include sardines, spinach, tofu, and select nuts.
For maximum absorption, it is best to divide doses up and not take more than 500-700 mg at a time.
Calcium
94
______ is the most absorbable type of Calcium and must be taken on an empty stomach.
Calcium citrate
95
A greater percentage of _____ iron is absorbed than ______ iron
heme/ non-heme
96
heme iron is found in _____
| non-heme iron is found in _____
meat/ plant products
97
heme iron is found in _____
| non-heme iron is found in _____
animal products/ plant products
98
The ______ form of iron is more easily absorbed into the intestinal mucosal cells but must be converted into the ferric form for transport in the plasma.
ferrous
99
All _____ preparations are better absorbed in an acidic environment, which is why clients are counseled to take it between meals, with vitamin C (orange juice), and distant from any ingestion of dairy products, antacids (separated by 4 hours), quinolones, or tetracycline (which actually inactivates it).
Iron
100
Taking _____ supplementation with food can result in as much as a 2/3 reduction in its absorption.
Iron
101
Treat iron-deficiency anemia for _____ months to restore ferritin stores.
3-6
102
The typical dose of for iron-deficiency anemia is Ferrous Sulfate ____ PO ___ between meals with orange juice for 3-6 months.
325 mg PO TID
103
"AVOID M"istakes
```
Allergies?
Vitamins and herbs?
Old drugs and OTC (as well as current)?
Interactions?
Dependence? Do you need a contract?
Mendel - family history of benefits or problems with any drugs?
```
104
Example of Type ___ Reaction:
| Angio edema, anaphylaxis
1
105
Example of Type ___ Reaction:
| heparin induced thrombocytopenia
2
106
Example of Type ___ Reaction:
(antibody-dependent cytotoxicity)
heparin induced thrombocytopenia
2
107
Example of Type ___ Reaction:
(immune complex hypersensitivity)
arthus reaction to tetanus
3
108
Example of Type ___ Reaction:
(cell-mediated, delayed)
drug rash, eosinophilia
4
109
Example of Type ___ Reaction:
(probably mast cell degranulation by non-IgE)
opiate analgesis direct mast cell activation
pseudo allergy
110
Pharmacokinetic alterations due to _____:
increased gastric pH
slower peristalsis resulting in increased length of the time for absorption to occur
decreased muscle mass
decreased total body water (10-15%), which results in the decreased distribution of water-soluble drugs.
Aging
111
recommended laboratory test to review to analyze renal function
estimated glomerular filtration rate (eGFR)
112
_____ may have a higher rate of metabolism, drugs may become less protein bound, and distribution is affected by a higher concentration of water
Children
113
1. Define the patient's problem
2. Specify the therapeutic objective
3. Choose the treatment
4. Start the treatment
5. Educate the patient
6. Monitor effectiveness
WHO's Model of Rational Prescribing
114
the amount of agonist needed to elicit a desired response. Think of overdose- carfentanil (elephant tranquillizer) it is 100 Xs as potent as the same amount of fentanyl, 5,000 times as potent as heroin, and 10,000 times as potent as morphine
potency
115
The margin of safety that exists between the dose needed for the desired effect and the dose that produces unwanted and possibly dangerous side-effects. In general, the narrower this margin, the more likely it is that the drug will produce unwanted effects.
therapeutic index
116
Increasing the metabolic pathway and results in less action of drug- the drugs exits the body faster.
enzyme induction
117
Results in decreased metabolism and result in increased pharmacologic action of drug. The drug stays in the body longer.
enzyme inhibitor
118
pharmacologically inactive medications that are metabolized into an active form within the body. Codeine is an example.
prodrug
119
Someone who metabolized at an ultra fast rate. For example, if a particular CYP450 variation makes someone a rapid metabolizer of a drug, he or she may process it so fast that the drug won’t have a chance to reach optimal blood levels, leading to limited amounts of drug that can act on the patient’s system. However if a drug is a pro drug (like codeine) and the patient is an ultra rapid metabolizer- there is a sudden very lare amount of active drug and the patient can overdose.
ultra rapid metabolizer
120
Many drugs bind to protein in the blood. Drugs bound to the protein are not active. The proteins do not release the drug until saturated.
protein-binding
121
food which is formulated to be consumed or administered enterally under medical supervision and which is intended for the specific dietary management of a disease or condition for which distinctive nutritional requirements, based on recognized scientific principles, are established by medical evaluation. This category is considered to be very limited. These medical foods are "...specially formulated and processed (as opposed to a naturally occurring foodstuff used in a natural state) for the patient who is seriously ill or who requires the product as a major treatment modality." These foods are exempted from the nutrition labeling required on other non-medical foods.
medicinal foods
122
The percentage of the recommended daily allowance (RDA) for a nutrient is usually listed on the product label. ("the levels of intake of essential nutrients considered, in the judgment of the Food and Nutrition Board on the basis of available scientific knowledge, to be adequate to meet the known nutritional needs of practically all healthy persons").
It is important to remember:
RDAs are developed for healthy persons under normal conditions. Pregnant women, persons with chronic debilitating diseases, alcoholics, teenagers, and infants may have specific and additional needs and requirements.
The RDAs have a known margin of safety. If your client is generally healthy and obtaining 70% of the RDA for a particular nutrient, the possibility of a deficiency is remote.
RDA
123
A list of medications that frequently cause side effects when administered to elderly patients. Among the medications on the list are those that cause prominent neuropsychiatric, renal, and anticholinergic side effects.
It is important to know that these are guidelines and not prescribing protocols. In other words, these are both good tools to use to help you identify red flags and to identify necessary monitoring but they are not the final word on medication appropriateness. As the prescriber, you will need to consider potential risk, benefits, and alternatives.
BEERS criteria
124
a substance such as a food, drug, chemical agent, or even a natural component in the environment that causes malformations by damaging fetal growth, structure, or development... characterized by their effect and the time in gestation the exposure occurs.
The drug must cause a characteristic set of malformations.
It must act only during a specific window of vulnerability (for example, during organogenesis).
The incidence of malformations should increase with increasing dosage and duration of exposure.
teratogen
125
In drug metabolism when the concentration of drug is greatly reduce before it reaches systemic circulation. This is related to drugs that are orally administered.
hepatic first pass
126
A life threatening syndrome marked by a
prolonged QT interval with episodes of
electrocardiographic torsades de pointes.
This condition may be acquired as a result of drug administration.
Usuallyit is caused by a combination of drugs that prolong Qt- so check interactions. Additional risk include low K, low magnesium and bradycardia.
QT prolongation
127
maximum effect that a drug can produce regardless of dose.
maximal efficacy
128
The time required for a quantity to reduce to half its initial value. Should a drug's half-life be very short, it would mean that the dosage would be given more frequently, to keep the levels in the body up and have a consistent therapeutic effect.
If the drug is dosed at an intermittent dosing interval equal to this single half life, a predictable pattern of fluctuation and accumulation at chronic multiple dosing occurs, where the plasma concentration can be expected to fall in half during each dosing interval (fluctuation), and the multiple dosing steady-state levels of drug at any time during the dosing interval will be twice the levels of drug at that same time following the first dose (accumulation).
half-life
