Week 1 Flashcards
(161 cards)
1
Q
What are some ways that drugs might impact rehab?
A
• Response to Exercise • Patient’s Pain Perception • Participation & Motivation in Rehab • Interactions with Modalities • Side Effects Screening • Understanding of current medical management in interprofessional care
2
Q
How can drugs impact a person’s response to exercise?
A
Cardiac agents limiting exercise
3
Q
How can drugs affect a patient’s pain perception which impacts rehab?
A
Pain management may be necessary to allow/encourage a
patient to commit to PT
4
Q
How can drugs affect a patient’s participation and motivation in rehab?
A
- Pain management
* Antidepressants
5
Q
What are the possible drug interactions with modalities that can affect therapy?
A
• Herbal supplements are drugs
and can interact with regulated
pharmaceuticals
• SJW can cause an induction of metabolism
• Fentanyl patch can be affected by heat wraps
6
Q
How should drug side effects screening be done?
A
• PT is an important part of integrated health care • Prolonged, regular patient contact • Need to be aware of adverse drug events that are/are not related to PT interventions
7
Q
What is a drug?
A
Any non-nutrient chemical which has a physiological effect
on the body
8
Q
What are the functions of a drug?
A
Alters Physiologic Function
• + increases the function
• (-) or decreases it
9
Q
What are the different possible drug types?
A
- Natural
- Semi-synthetic
- Synthetic
10
Q
What does a PT need to know about drugs?
A
Target Understanding Drug(s) • Basic Principles • Mechanism of Action • Patient Response • Interactions w/ PT Interventions
11
Q
What are the pharmacology areas of study?
A
• Pharmacotherapeutics
- Pharmacokinetics
- Pharmacodynamics
• Toxicology
12
Q
What is pharmacotherapeutics?
A
The use of specific drugs to to prevent, treat, or diagnose a disease
13
Q
What is toxicology?
A
Study of the harmful effects of
chemicals
14
Q
What is pharmacokinetics?
A
Study of how the body processes a drug. How the body affects the drug
15
Q
What is pharmacodynamics?
A
How a drug affects the body (time course and intensity of effect)
16
Q
What are the concepts included in pharmacokinetics?
A
- Absorption
- Distribution
- Elimination
17
Q
What are the concepts included in pharmacodynamics?
A
- Systemic Effects
- Cellular Effects
18
Q
What are the characteristics of a generic drug?
A
• Often the easiest way to refer to a drug
• Typically less expensive
• Should meet *BioEquivilancy criteria
• Even with testing patients
don’t always respond the same as to Brand Name
19
Q
What is included in the BioEquivilancy criteria?
A
Same amount & type of active ingredients
• Same administration route
• Same pharmacokinetic profile
• Same therapeutic effect
20
Q
What are the characteristics of a brand name drug?
A
- Similar trade names for drugs in very different classifications!
- May not bear any resemblance to to chemical or generic terminology
21
Q
What is the generic name of cialis?
A
Tadalafil
22
Q
What is the generic name of tylenol?
A
Acetaminophen” and “paracetamol”
23
Q
What is the generic name of OxyContin?
A
Oxycodone
24
Q
What is the generic name of Zithromax?
A
Azithromycin
25
What is the generic name of Sudafed?
Pseudoephedrine
26
What type of drugs have the suffix -azine?
Antipsychotics, neuroleptic, antiemetic
27
What type of drugs have the suffix -azole?
Antifungal
28
What type of drugs have the suffix -azepam?
Antianxiety drugs
29
What type of drugs have the suffix -barbital / -bital?
Barbiturate sedative hypnotics
30
What type of drugs have the suffix -caine?
Lidocaine (local anesthetics)
31
What type of drugs have the suffix -cillin?
Penicillin (antibiotics)
32
What type of drugs have the suffix -cycline?
Tetracycline (antibiotic protein synthesis inhibitor)
33
What type of drugs have the suffix -mycin, -micin?
Erythromycin (aminoglycoside inhibiting antibiotic)
34
What type of drugs have the suffix -navir, -vir?
Saquinavir (protease inhibitor (antiviral, i.e. HIV, Hepatitis B, C))
35
What type of drugs have the suffix -olol?
Propanolol (Beta-adrenergic blocker)
36
What type of drugs have the suffix -oxin?
Digoxin (cardiac glycosides)
37
What type of drugs have the suffix -ine?
Caffeine (Xanthine derivatives, stimulants)
38
What type of drugs have the suffix -pril?
Ramipril (ACE Inhibitor)
39
What type of drugs have the suffix -statin?
Lovastatin (HMG-CoA reductase inhibitors)
40
What are the advantages of over the counter drugs?
Lower drug doses
• Increased availability/access
• Less expensive
41
What are the disadvantages of over the counter drugs?
* Possible interactions with prescription medications
* May delay use of more effective medications or treatments
* Adverse effects
42
What are the concepts of drug therapy?
* Target a specific cell type or tissue type
* Some change cellular function to restore a normal state
* Some prevent diseases from occurring (statins)
43
What is a drug dose?
The amount of drug administered in a given formulation
44
What is the mechanism of a drug dose?
• A given dose results in a
given blood concentration
• A given blood concentration results in a given concentration at the target tissue
• Concentration must be large enough to produce a beneficial response- *without being toxic
45
What is a threshold drug dose?
Where a drug response begins & increases in magnitude until a
response plateau is reached
46
What is a Ceiling Effect (Maximal Efficacy) drug dose?
The point at which there is no further response (even if dosage continues to be increased).
47
What are the characteristics of the efficacy of a drug dose response?
* Dosage ranges over which the drug has desired effect
| * Magnitude of response increases as dosage increases (up to some maximum effect).
48
What are the characteristics of the potency of a drug dose response?
• Threshold dose that produces a given response
• Higher Potency means less of the compound is required to produce a given response
• lower threshold dose = inc
potency
49
What are the characteristics of the quantal dose-response curve?
• % of the population who exhibit a specific response relative to the dose of the drug
• looks at variations in drug responses due to individual
differences within the clinical population
50
What are the characteristics of the therapeutic index?
```
(TI=TD50/ED50)
• Calculated value to indicate drug safety
• Relative Term
• High TI=considered safer
• Prescription agents usually lower TIs
```
51
What are the different drug safety reference points used?
• Median Effective Dose
(ED50)
• Median Toxic Dose (TD50)
• Median Lethal Dose (LD50)
52
What is the median effective dose (ED50) of a drug?
The dose at which 50% of the population respond to a drug in a specified manner (response)
53
What is the median toxic dose (TD50) of a drug?
The dose at which 50% of the
population exhibits the adverse
effect/response.
54
What is the median lethal dose (LD50) of a drug?
The dose that causes death in 50% of the animals studied.
55
What is the role of the FDA in a drug?
* Is a Drug Effective?
| * Is a Drug Safe?
56
What is the FDA drug approval process?
* Clinical Testing Phases: 0-IV
* 7-9 years (~ 1 billion dollars total cost)
** ‘Fast Track’ exists for life-threatening conditions or approval of a new indication for a known drug
57
What is the abuse potential, legal use and example of a drug that falls under the controlled substance schedule 1?
```
• Abuse potential: highest
• Legal use: Restricted to
approved research or therapeutic use in very limited # of patients
• Example: Medical marijuana,
cocaine
```
58
What is the abuse potential, legal use and example of a drug that falls under the controlled substance schedule 2?
• Abuse potential: high
• Legal use: specific
therapeutic purposes w/ prescription
• Example: Opiods- morphine
59
What is the abuse potential, legal use and example of a drug that falls under the controlled substance schedule 3?
• Abuse potential: mild moderate possible physical/
psychologic dependence
• Legal use: specific
therapeutic purposes w/ prescription
• Example: Certain Opiods: codeine combos; Anabolic
steroid
60
What is the abuse potential, legal use and example of a drug that falls under the controlled substance schedule 4?
• Abuse potential: limited possible physical/psychologic
dependence
• Legal use: specific therapeutic purposes w/ prescription
• Example: Anti-Anxiety drugs; Other depressants & stimulants
61
What is the abuse potential, legal use and example of a drug that falls under the controlled substance schedule 5?
* Abuse potential: lowest relative abuse potential
* Legal use: OTC
* Example: Cough medications; Anti-diarrheal medications
62
What are the phases of the drug development and approval process by the FDA?
- Pre-Clinical Testing: lab animals
- Phase I: Clinical Testing: healthy subjects
- Phase II: Limited target population
- Phase III: Large target population
- New Drug Approval (NDA)
- Phase IV: Monitor general
population
63
What are the features of pharmacodynamics?
- Potency
- Efficacy
- Therapeutic Effect on the body (Subtherapeutic, Supratherapeutic, Therapeutic index)
- Side Effects (Toxic effects, adverse effects)
- Receptors( how drugs have their impact on the body)
64
What dose of a drug provides optimal therapy?
Therapeutic Dose
65
Potency does not equal ___
Potency does not equal *efficacy*
66
What does a more potent drug mean?
Less drug required for a specific response
67
What is the efficacy of a drug?
The drug’s ability to produce a desired response
68
What is the effectiveness of a drug?
Describes how useful the drug is (TI, ease of use)
69
What are the features of pharmacokinetics?
- Administration
- Absorption
- Distribution
- Elimination
70
What are the characteristics of s a drug/receptor structure?
* Nature of drug binding
| * Sterics and electronics
71
What is sterics?
The study of how drug shape and size can impact the ability of the drug to have an effect at the cellular level
72
What are the characteristics of a drug delivered through the enteral(through the GI) system?
```
• Usually oral
• Easiest for self-administration
• Generally safe, controlled entry to system
• Absorbed by small intestine
• Drug must have high lipid
solubility
• “First Pass Effect”- metabolism/destruction of
drug molecule in liver before
reaching its site of action
• Examples: oral, sublingual,
rectal
```
73
What are the characteristics of a drug delivered through the paraenteral(not through the GI) system?
```
• Bypass the GI system
• More direct route to target
site
• More predictable quantity
• Not subject to “First Pass
Effect”
• Examples: injection, IV, IA,
Sub-Q, IM, TD, Topical,
Intrathecal, Inhaled;
```
74
What are the advantages and disadvantages of the oral route of delivering medication?
- Advantages: Easy, safe, convenient
| - Disadvantages: Limited or erratic absorption of some drugs; chance of first pass inactivation in liver
75
What are the advantages and disadvantages of the sublingual route of delivering medication?
- Advantages: Rapid onset; not subject to first pass inactivation
- Disadvantages: Drug must be easily absorbed from oral mucosa
76
What are the advantages and disadvantages of the rectal route of delivering medication?
- Advantages: Alternative to Oral Route; local effect on rectal tissues
- Disadvantages: Poor or incomplete absorption; chance of rectal irritation
77
What are the advantages and disadvantages of the inhalation route of delivering medication?
- Advantages: Rapid onset; direct application for respiratory
disorders; large surface area for systemic absorption
- Disadvantages: Chance of tissue irritation; patient compliance sometimes a problem;
78
What are the advantages and disadvantages of the injection route of delivering medication?
- Advantages: Provides more direct administration to target
tissues; rapid onset
- Disadvantages: Chance of infection if sterility is not maintained
79
What are the advantages and disadvantages of the topical route of delivering medication?
- Advantages: Local effects on surface of skin
| - Disadvantages: Only effective in treating outer layers of the skin
80
What are the advantages and disadvantages of the transdermal route of delivering medication?
- Advantages: Introduces drug into body without breaking the skin; can provide steady, prolonged delivery via medicated patch
- Disadvantages: Drug must be able to pass through dermal layers intact
81
What is the “Bioavailability” of a drug?
% of drug administered that reaches the bloodstream
82
What are the characteristics of the “Bioavailability” of a drug?
* Depends on route of administration & the drug’s ability to cross membrane barriers
* Depends on extent of first pass metabolism
83
What are the BioAvailability factors of a drug?
• Body Membrane Structure &
Function
• Drug Movement across Membrane Barriers
• Active Transport
84
What are the different methods in which a drug can be distributed throughout the body?
- Tissue permeability
- Blood flow
- Plasma protein binding
- Subcellular protein binding
85
What are the characteristics of the tissue permeability method of drug distribution throughout the body?
* Highly lipid soluble molecules cross membranes more easily
* Solubility concerns
* Membrane permeability
86
What are the characteristics of the blood flow method of drug distribution throughout the body?
• Bloodstream will carry drugs
to highly perfused organs
• Can be affected by disease
87
What are the characteristics of the plasma protein binding method of drug distribution throughout the body?
* Reversible bonds
| * Bound portion of drug doesn’t have a therapeutic effect and is not eliminated
88
What are the characteristics of the subcellular protein binding method of drug distribution throughout the body?
• Drug gets trapped within
the cell (usually in the lysosome)
• Example: antidepressants
89
What does the negative venule pressure of the body do to a drug?
Pulls the drug from tissues back into the blood
90
What does the positive arteriole pressure of the body do to a drug?
It draws drugs via blood into tissue spaces
91
What is an inactive drug?
A drug that is bound to plasma protein and cannot leave the blood to distribute into tissues
92
What is an active drug?
A drug that is unbound (free) and may distribute from blood to tissues
93
What is the volume distribution of a drug?
Amount of drug administered /
| Concentration of drug in plasma
94
What happens when the volume distribution of a drug is equal to the total amount of body water?
Leads to uniform body
| distribution
95
What happens when the volume distribution of a drug is greater than the total amount of body water?
Leads to the drug being concentrated in the tissues
96
What happens when the volume distribution of a drug is less than the total amount of body water?
Leads to the drug being retained in the bloodstream
(due to plasma protein binding
for example)
97
Where are the drug storage areas in the body?
```
• Adipose Tissue: primary site;
example: anesthetics
• Bone: toxic agents; example: lead
• Muscle: long-term storage;
example: anti-malarials
• Organs: often liver & kidneys;
example: anti-microbials
```
98
What are the characteristics of controlled release drug delivery?
• Decreases the number of doses/day; Sustains dose
throughout night
• Examples: beta blockers, analgesics, Parkinson's Drugs
99
What are the characteristics of implanted reservoir drug delivery?
• Locations: abdomen, spinal cord
• Examples: muscle relaxers, analgesics, anesthetics,
hormones
100
What are the characteristics of targeted cell & tissue delivery drug delivery?
* Attaching antibodies to drugs
| * Examples: Brentuximab vedotin for Hodgkin Lymphoma
101
What are the forms of drug elimination?
- Biotransformation
- Excretion
- Combination
102
What is the biotransformation form of drug elimination?
Chemical altering of a drug to a metabolite via
enzymes to deactivate that drug
• Aka: Metabolism
103
What are the characteristics of excretion form of drug elimination?
Excreting the active form of a drug
104
What are the characteristics of combination form of drug elimination?
A combination of biotransformation & excretion
105
What is the cellular mechanism of biotransformation?
- Oxidation
- Reduction
- Hydrolysis
- Conjugation
106
What is included in the oxidation portion of the cellular mechanism of biotransformation?
```
(+) O2
• (-) H
• Usual Method via enzymes
• DMMS
• Endoplasmic smooth reticulum
• Example: Ibuprofen, Acetaminophen, Diazepam
• Phase I reaction
```
107
What is included in the reduction portion of the cellular mechanism of biotransformation?
* (-) O2
* (+) H
* happens in cell cytoplasm via enzymes
* Phase I reaction
108
What is included in the hydrolysis portion of the cellular mechanism of biotransformation?
```
• Original compound is
broken into separate parts
• Enzymes at several sites in
body are responsible
• Phase I reaction
```
109
What is included in the conjugation portion of the cellular mechanism of biotransformation?
• Drug or metabolite bi- product of one of other
mechanisms is coupled into and endogenous substance;
• These enzymes responsible for conjugation are found on
endoplasmic reticulum and in
cytoplasm
• Phase II reaction
110
Where does drug metabolism occur?
* Liver Primary Location
| * Lungs, Kidneys, GI, Skin
111
How does drug metabolism occur?
Biotransformation
112
What are the other factors that plays into drug metabolism?
* Tissue/Organ damage
* Metabolic inhibitors
* Enzyme Induction
113
What is competitive inhibition of metabolism?
The inhibition of the enzyme that metabolizes a specific drug reducing, because it is being metabolized by another drug
114
What is the cycle of enzyme induction?
- Prolonged use of drug leads to
- Increased enzyme production or decreased degradation leads to
- Increased rate of drug metabolism leads to
- Decreased therapeutic effect leads to
- Tolerance=Need for increased
doses of same drug to produce
same effect leads to
- Can then extend effect to other drugs as well.
*the cycle just keeps going*
115
What is the process by which drugs get excreted at the kidneys?
```
- Metabolized drug (metabolite)
reaches nephron -->
- Filtration at the glomerulus -->
- Travels to the proximal convoluted tubule -->
- Loop of Henle -->
- Proximal convoluted tubule -->
- Collecting ducts -->
- Leaves body as urine
```
116
What are the factors that affect excretion?
```
• Reabsorption
• Polarity of metabolite
• Ionized=Polar
• Polar drugs tend to
be excreted
• Non-Polar drugs tend to be reabsorbed into body versus being excreted
```
117
Drugs are metabolized via biotransformation primary at
| the ___ and ____
Drugs are metabolized via biotransformation primary at
| the *liver & lungs.*
118
Drugs engage with cellular receptors to impact
| ____.
Drugs engage with cellular receptors to impact *metabolism.*
119
__ and ____ are properties that affect drug elimination rates.
*Clearance rate and half-time* are properties that affect drug
elimination rates.
120
Dosing schedules can vary dramatically & can impact
| ____
Dosing schedules can vary dramatically & can impact
| *functional capacity (rehabilitation process)*
121
Agonistic-antagonist concept is related to ____
Agonistic-antagonist concept is related to *receptor activity*
122
What does an increased stimulation of receptors result in?
A decrease in receptor numbers/function. Desensitization/ down-regulation
123
What does a decreased stimulation of receptors result in?
Increased receptor numbers. Supersensitivity
124
What does a drug that falls in the antagonist classification do in reference to agonist?
Prevents the agonist from binding to the receptor and exerting a physiologic effect
125
What is the function of an agonist class drug?
Drug capable of binding to a
| receptor and activating change in the cell’s function
126
What are the characteristics of an agonist class drug?
• Has both affinity & efficacy
• ‘Partial Agonists’ create a less
than optimal response even though they are capable of occupying receptors
127
What is the function of an antagonist class drug?
Drug capable of binding to a
| receptor but unable to create change in the receptor cell’s function
128
What are the characteristics of an antagonist class drug?
```
Has affinity, but not activity
• Occupy valuable receptor site
thereby “blocking” agonists from
binding
• Example: beta blockers
• Competitive or Irreversible
```
129
What is the difference between a competitive and an irreversible antagonist class drug?
Competitive antagonists can be
displaced with higher concentrations of a drug agonist, but Irreversible
antagonists form permanent bonds that prevent Agonists from binding
130
What is the dose response of a drug essentially proportional to?
Response is essentially proportional to the # of receptors occupied by the drug; (generally speaking)
• Not always a linear relationship
131
What are the factors that can affect the dose response of a drug?
* Affinity
| * Receptor signal transmission
132
What are the ways to determine the rate of drug elimination of a drug from the body?
* Clearance (CL)
| * Half-Life
133
What is clearance (CL) drug elimination rate?
Can describe one organ or all organs ability to clear a drug: CL=Q X ((Ci- Co)/Ci
134
What is drug elimination rate: clearance dependent on?
On organ ability to extract
| drug from plasma & perfusion
135
Systemic clearance is equal to ____
Sum of individual organ CLs
136
What are the factors that affects drug elimination rate: clearance?
* Blood Flow to Organ (Q)
* Extraction Ratio- the fraction of drug removed from the plasma as it passes through the organ (Ci-Co)
* Concentration (Ci)
137
What are the characteristics of the half- life drug elimination rate?
* Duration of activity of the compound in the body
* The amount of time required for 50% of the drug remaining in the body to be eliminated
* A function of both Clearance & Volume of Distribution (Vd)
138
What is are drug elimination rates?
Parameters used to indicate the rate at which a drug is usually eliminated so that dosages may be adjusted accordingly
139
What are the characteristics of the clearance drug elimination rate?
* Units of mL/min suggest drug is being removed from a specific volume of blood
* This is not a good physical description of what is happening
140
What is a continuous administration dosing schedule?
Matching the rate of administration with the rate of drug elimination (clearance) once the desired plasma concentration is achieved
141
What is an interval administration dosing schedule?
Dosage is adjusted to provide an average plasma concentration over the dosing period.
142
What is the main feature of an interval administration dosing schedule?
Dosing interval (time in hours) will affect size of dosage needed to maintain same relative plasma concentration
143
What are the factors that affects the variations of a drug response?
- Genetic Factors
- Disease
- Drug Interactions
- Age
- Diet
- Sex
- Other Factors
144
What are the patient related factors that can affect the response to a drug?
- Geriatrics
- Age/sex
- Concomitant disease
- Diet/nutrition
- Environment
- Smoking/alcohol
145
What are the drug related factors that can affect the response to a drug?
- Dose/dosing times
- Half life
- Oral availability
- Routes of elimination
- Therapeutic index
- Interaction mechanism
146
What is a receptor?
A cellular component where a drug binds and initiates a chain of biochemical events
147
What are the characteristics fo a surface receptor?
* Located outer cell membrane
| * Responsive to amino acid peptides, or amine compounds
148
Surface receptors recognize and effect change by...?
1. Ion channel/Membrane Permeability
2. Enzymatic Effects
3. Regulatory Protein Links
149
Surface membrane phospholipids have ___ heads and ___ tails
Surface membrane phospholipids have *hydrophilic* heads and *hydrophobic* tails
150
What is an example of the mechanism of surface receptor: Receptors + Ion Channels?
(ACh) Acetylcholine example: ACh binds to receptor which activates opening pore in membrane allowing Sodium (Na) in.
151
What is an example of the mechanism of surface receptor: Enzymes + Receptors?
Protein tyrosine kinases: outer surface stimulation activates inner surface wall enzymatic process
152
What is an example of the mechanism of surface receptor: regulatory proteins + receptors
Proteins are located on inner surface of membrane; G Proteins when stimulated then activates enzymes or Ion channels. 2nd Messenger System
153
What are the characteristics of intracellular receptors?
```
• Located at cytoplasm & nucleus
• A specific interaction mechanism for Hormones
• Examples: thyroid hormones,
steroids
• Generally control gene
expression when activated
```
154
What affects the successful binding of a drug and a receptor?
* Drug size
* Drug shape/fit: Key-Lock analogy
* Affinity
* Presence of Allosteric Modulators- local modulators that affect affinity of receptor portion of bond
155
What is is affinity that affects the successful binding of a drug and a receptor?
Electrostatic attraction between a drug & receptor; related the
drug amount required to bind to the unoccupied receptors (if affinity is low, higher concentrations may be needed)
156
What does a drug binding to a receptor do?
Binding causes a change in shape or configuration of receptor which starts a cascade of events
157
What is drug selectivity?
A drug that affects only one type of cell or tissue & produces a specific physiologic response
158
What is the sub-typing of receptor populations based on?
Binding preferences, structure, and function
159
How many types of subtypes of histamine receptors are there?
4
160
How many types of subtypes of muscarinic receptors are there?
5
161
What is the main difference between a selective and non-selective drug?
A selective drug only mostly provide beneficial effects with minimal side effects, non-selective drugs produce both beneficial effects and side effects
