Week 1 - Intro Flashcards
Why do PTs care about pharmacology?
Will work with people who are on medications so is good to be aware of the effects.
How do drugs impact rehab? (6)
- Response to Exercise
- Patient’s Pain Perception
- Participation and Motivation in Rehab
- Interaction with Modalities
- Side Effects Screening
- Understanding of current medical management in inter-professional care
What is an example of a drugs impacting rehab by response to exercise?
Cardiac agents limiting exercise.
What is an example of drugs impacting rehab by patient’s pain perception?
Pain management may be necessary to allow/encourage a patient to commit to PT.
What is an example of drugs impacting rehab by participation and motivation in rehab?
Pain management and antidepressants
What is an example of drugs impacting rehab by interactions with modalities?
Herbal supplements are drugs and can interact with regulated pharaceuticals.
SJW induction of metabolism.
Fentanyl patch and heat wraps.
What is an example of drugs impacting rehab by side effects screening?
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.
What is an example of drugs impacting rehab by understanding of current medical management in interprofessional care?
- Mainly editorial, perspective, commentary, observational, case-report driven articles found in PT-related journals.
- Controlled studies found in physician specialty-related literature.
What is the definition of a drug?
Any non-nutrient chemical which has a physiological effect on the body.
In what ways can a drug alter physiological function?
Increases the function or decreases it.
What are the three types of drugs?
1) Natural (doesn’t mean safe)
2) Semi-synthetic (start with known drug)
3) Synthetic (designed in lab)
Describe the semi-synthesis of amoxicillin. Why do it?
Penicillin G -> 6-aminopenicillanic acid -> Amoxicillin
- Improve potency
- Absorption (in GI tract)
- Stability (easier to formulate)
What is Pharacotherapeutics?
The use of specific drugs to prevent, treat, or diagnose disease.
What is Pharmacokinetics?
Study of how the body processes a drug.
What is Pharmacodynamics?
Analysis of drug mechanism and effects.
What is Toxicology?
Study of the harmful effects of chemicals.
What is a “Generic” (USAN - US adopted name) drug?
- 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
What is a Brand Name drug?
- Similar trade names for drugs in very different classifications.
- May not bear any resemblance to chemical or generic terminology.
What is Bioequivalncy?
- Same amount and type of active ingredients
- Same administration route
- Same pharmacokinetic profile
- Same therapeutic effect
Suffixes
?
What are the benefits to OTC drugs?
- Lower drug doses
- Increased availability/access
- Less Expensive (but may be more cost to patient?)
What are the negatives to OTC drugs?
- Possible interactions with prescription medications.
- May delay use of more effective medications or treatment (ibuprophen instead of PT)
- Adverse effects.
What are 3 purposes of drugs?
- Target a specific cell type or tissue type
- Some change cellular function to restore a normal state (psychiatric drugs)
- Some prevent diseases from occurring (statins prevent buildup of cholesterol)
What is a dose?
The amount of drug administered in a given formula.
What is the result of a given dose?
a given blood concentration. some linear relationship, blood concentration x2 = x2 dose
What is the result of a given blood concentration?
a given concentration at the target tissue.
Why is a given concentration at target tissue important?
Concentration must be large enough to produce a benefit without being toxic (exceptions like chemo)
What does a dose-response curve represent?
the dosage over which the drug is effective and peak effect/response that can be expected. Shape of curve and plateau indicate info re: binding of drug to cellular receptors.
What is a threshold dose?
Where response begins and increases in magnitude until a response plateau is reached.
What is a ceiling effect (maximal efficacy)?
the point at which there is no further response (even if dosage continues to be increased.)
What is efficacy?
Dosage ranges over which the drug has desired effect.
Magnitude of response increases as ____
dosage increases (up to some maximal effect)
What is potency?
Threshold dose that produces a given response.
Higher potency means ____
less of the compound is required to produce a given response.
Lower threshold dose =
increased potency
T/F: Potency or Maximum Efficacy can indicate a drug’s theraputic potential.
FALSE: neither potency nor maximum efficacy fully indicate a drugs therapeutic potential.
Graph: Which drug is more potent?
Drug “A”
Which drug has the greater maximal effect?
Drug “B”
What is a 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.
How do you calculate a therapeutic index?
TI = TD50/ED50
What is a therapeutic index (TI)?
calculated value to indicate drug safety.
- relative term, higher TI = considered safer
- prescription ages usually lower TIs
(extremely low TI wouldn’t be approved unless for cancer of perhaps HIV)
What is Median Effective Dose (ED50)?
The dose at which 50% of the population responded to a drug in a specific manner (response).
What is Median Toxic Dose (TD50)?
The dose at which 50% of the population exhibits the adverse effect/response.
What is the Median Lethal Dose (LD50)?
The dose that causes death in 50% of the animals studied.
What does the food and drug administration do?
- Began in the early 1900s
- Is a Drug Effective?
- Is a Drug Safe?
What is drug approval process?
- Clinical Testing Phases: I - IV
- 7-9 years (~1 billion dollars total cost)
- ‘Fast Track’ exists for life-threatening conditions or approval of a new indication ofr a known drug.
What are the phases for clinical testing?
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 popultion
Based on The Coprehensive Drug Abuse Prevention and Control Act. (1970) what are categories or “schedules” for?
classified according to potential for abuse.
Which schedule of drug has the highest abuse potential?
I
Which schedule of drug has the lowest abuse potential
V
Schedule I:
Abuse Potential -
Legal Use -
Example -
Schedule I:
Abuse Potential - highest
Legal Use - restricted to approved research or therapeutic use in very limited number of patients
Example - medical marijuana, coccaine
Schedule II:
Abuse Potential -
Legal Use -
Example -
Schedule II:
Abuse Potential - high
Legal Use - specific therapeutic purposes w/ prescription
Example - Opoids: morphine
Schedule III:
Abuse Potential -
Legal Use -
Example -
Schedule III:
Abuse Potential - mid-moderate possible physical/psychologic dependence
Legal Use - specific therapeutic purposes w/ prescription
Example - certain opiods: codeine combos; anabolic steroids
Schedule IV:
Abuse Potential -
Legal Use -
Example -
Schedule IV:
Abuse Potential - limited possible physical/psychologic dependence
Legal Use - specific therapeutic purposes w/ prescription
Example - Anti-Anxiety drugs; Other depressants and stimulants
Schedule V:
Abuse Potential -
Legal Use -
Example -
Schedule V:
Abuse Potential - lowest relative abuse potential
Legal Use - OTC
Example - cough medications; anti-diarrheal medications
What is pharmacodynamics?
How a drug affects the body (time course and intensity of effect)
What is pharmacokinetics?
How the body affects the drug (absoprtion, distribution, metabolism, and excretion)
What is therapeutic effects: subtherapeutic
not enough of the drug to see what you want to see
What is therapeutic effect: supratherapeutic
too much of the drug and get into more toxic effects
What does pharmacodynamics determine?
Optimal Therapy:
Sub-therapeutic –> Therpeutic Dose –> Toxicity
How does Sub-therapeutic –> Therpeutic Dose –> Toxicity correlate with blood plasma concentration of drug?
Increasing blood plasma concentration of drug with increase in dose
More potent drug = ___ drug required for a specific response
More potent drug = LESS drug required for a specific response
T/F: Potency = Efficacy
FALSE: Potency does not equal efficacy
What is efficacy?
drug’s ability to produce a desired response (inherent to drug)
What is effectiveness?
describes how useful the drug is (TI, ease of use)
more of a real world definition based on how difficult to take and the side effects
What is maximal efficacy (ceiling effect)? Example?
increase in dose produces no greater response than a lower dosage (saturate receptors)
(I.E. beta blockers for blood pressure control)
What goes into the nature of drug binding?
Sterics - must match fit
electronics - must match charges
What are the 4 factors of pharmacokinetics?
- Administration
- Absorption
- Distribution
- Elimination (also metabolism)
What are the routes of drug administration? (12)
- Sublingual
- Rectal
- Oral
- Inhaled
- Injection
- Intravenous
- Intra-arterial
- Sub-Cutaneous
- Intra-Muscular
- Transdermal
- Topical
- Intrathecal
Transdermal: Route for Rehabilitation Modalities - Phonophoresis and Iontophoresis
Used for inflammatory reason, really only time using drugs as PT
Phonophoresis - ultrasound
Iontophoresis - electrical conduction
Usually Oral
a. Enteral
b. ParaEnteral
a. Enteral
Easiest for self-administration
a. Enteral
b. ParaEnteral
a. Enteral
Bypass the GI system
a. Enteral
b. ParaEnteral
b. ParaEnteral
What are the two broad methods for entry?
a. Enteral
b. ParaEnteral
Generally safe, controlled entry to system
a. Enteral
b. ParaEnteral
a. Enteral
More predictable quantity
a. Enteral
b. ParaEnteral
b. ParaEntral
Absorbed by small intenstine
a. Enteral
b. ParaEnteral
a. Enteral
Drug must have high lipid solubility
a. Enteral
b. ParaEnteral
a. Enteral
What is “First Pass Effect”?
metabolism/destruction of drug in liver before reaching site of action, only fraction of does goes into blood stream. Blood supply dumping out of stomach and into SI (so sublingual wouldn’t have this)
Subject to first pass effect
a. Enteral
b. ParaEnteral
a. Enteral
Not subject to “First pass Effect”
a. Enteral
b. ParaEnteral
b. ParaEnteral
Examples: oral, sublingual, rectal
a. Enteral
b. ParaEnteral
a. Enteral
however sublingual is not subject to first pass
Examples: injection, IV, IA, Sub-Q, IM, TD, Topical, Intrathecal, Inhaled; Spine
a. Enteral
b. ParaEnteral
b. ParaEnteral
What is Bioavailability?
% of drug administered that reaches the blood stream
If you inject 100mg of a drug and 10mg makes it, what is the bioavailability?
10/100 = 10% bioavailability
What two factors affect bioavailability?
- Depends on route of administration and the drug’s ability to cross membrane barriers
- Depends on extent of first pass metabolism
Where can weak acids be absorbed?
stomach pH 1 to 3 - drugs are neutral / no overall electronic charge in stomach
Where can weak bases be absorbed?
Duodenum pH 5 to 7 (cannot passively go through lipid layer in stomach, not neutral in duodenum and be be absorbed where as acids cannot.
How are the vast majority of drugs absorbed?
Passive Divvusion
What are the 4 methods of drug absorption?
- Passive Diffusion
- Active Transport
- Facilitated Diffusion (ion or small molecule pumped out and back in)
- Endocytosis
What 4 things are involved with distribution or moving the drug throughout the body?
- Tissue Permeability
- Blood Flow
- Plasma Protein Binding
- Subcellular Protein Binding
What are 3 factors of tissue permeability?
- High lipid soluble molecules cross membranes more easily
- Solubility concerns
- Membrane permeability
What are the two factors of blood flow?
- Bloodstream will carry drugs to highly-perfused organs
2. Can be affected by disease
What are the two factors of plasma protein binding?
- Reversible bonds
2. Bound portion of drug doesn’t have therapeutic effect and is not elimated
What is a factor of subcellular protein binding?
Drug gets trapped within the cell (usually in the lysosome)
Example: anti-depressants
Positive artieriole pressure ____
draws drug via blood into tissue spaces
Negative venule pressure ____
pulls drug from tissue back into blood
Drug that is bound to plasma protein cannot leave the blood to distribute into tissues and is ___
inactive
Drug that is unbound (free) may distribute from blood to tissues and is ___
active
High Serum Protein Binding
Lots of drug will attach to protein but as it is absorbed from the blood into the tissues, drug will be released from protein to establish equilibrium.
Low Serum Protein Binding
Very soluble so will have a lot free in the blood and available to be absorbed into the tissues
What is Vd?
volume of distribution = amount of drug administered / concentration of drug in plasma
if Vd = Total amount of body water
uniform body distribution
if Vd > Total amount of body water
drug is being concentrated in the tissues
if Vd
drug is being retained in the bloodstream (due to plasma protein binding for example)
If you inject 100mg of a drug into 100ml of water and stir, Vd = ?
there will be 1.0mg/ml in the solution and can confirm this by drawing 1.0 mL of water, it will contain 1.0mg of drug
Now inject 100mg of a drug into an unknown volume and stir. If we draw 1.0m and find that there is 2.0 mg/mL, how much water was in the box (Vd)?
50mL
100mg/50mL = 2 mg/mL
Which schedule of drug has the highest abuse potential?
I
Which schedule of drug has the lowest abuse potential
V
Schedule I:
Abuse Potential -
Legal Use -
Example -
Schedule I:
Abuse Potential - highest
Legal Use - restricted to approved research or therapeutic use in very limited number of patients
Example - medical marijuana, coccaine
Schedule II:
Abuse Potential -
Legal Use -
Example -
Schedule II:
Abuse Potential - high
Legal Use - specific therapeutic purposes w/ prescription
Example - Opoids: morphine
Schedule III:
Abuse Potential -
Legal Use -
Example -
Schedule III:
Abuse Potential - mid-moderate possible physical/psychologic dependence
Legal Use - specific therapeutic purposes w/ prescription
Example - certain opiods: codeine combos; anabolic steroids
Schedule IV:
Abuse Potential -
Legal Use -
Example -
Schedule IV:
Abuse Potential - limited possible physical/psychologic dependence
Legal Use - specific therapeutic purposes w/ prescription
Example - Anti-Anxiety drugs; Other depressants and stimulants
Schedule V:
Abuse Potential -
Legal Use -
Example -
Schedule V:
Abuse Potential - lowest relative abuse potential
Legal Use - OTC
Example - cough medications; anti-diarrheal medications
What is pharmacodynamics?
How a drug affects the body (time course and intensity of effect)
What is pharmacokinetics?
How the body affects the drug (absoprtion, distribution, metabolism, and excretion)
What is therapeutic effects: subtherapeutic
not enough of the drug to see what you want to see
What is therapeutic effect: supratherapeutic
too much of the drug and get into more toxic effects
What does pharmacodynamics determine?
Optimal Therapy:
Sub-therapeutic –> Therpeutic Dose –> Toxicity
How does Sub-therapeutic –> Therpeutic Dose –> Toxicity correlate with blood plasma concentration of drug?
Increasing blood plasma concentration of drug with increase in dose
More potent drug = ___ drug required for a specific response
More potent drug = LESS drug required for a specific response
T/F: Potency = Efficacy
FALSE: Potency does not equal efficacy
What is efficacy?
drug’s ability to produce a desired response (inherent to drug)
What is effectiveness?
describes how useful the drug is (TI, ease of use)
more of a real world definition based on how difficult to take and the side effects
What is maximal efficacy (ceiling effect)? Example?
increase in dose produces no greater response than a lower dosage (saturate receptors)
(I.E. beta blockers for blood pressure control)
What goes into the nature of drug binding?
Sterics - must match fit
electronics - must match charges
What are the 4 factors of pharmacokinetics?
- Administration
- Absorption
- Distribution
- Elimination (also metabolism)
What are the routes of drug administration? (12)
- Sublingual
- Rectal
- Oral
- Inhaled
- Injection
- Intravenous
- Intra-arterial
- Sub-Cutaneous
- Intra-Muscular
- Transdermal
- Topical
- Intrathecal
Transdermal: Route for Rehabilitation Modalities - Phonophoresis and Iontophoresis
Used for inflammatory reason, really only time using drugs as PT
Phonophoresis - ultrasound
Iontophoresis - electrical conduction
Usually Oral
a. Enteral
b. ParaEnteral
a. Enteral
Easiest for self-administration
a. Enteral
b. ParaEnteral
a. Enteral
Bypass the GI system
a. Enteral
b. ParaEnteral
b. ParaEnteral
What are the two broad methods for entry?
a. Enteral
b. ParaEnteral
Generally safe, controlled entry to system
a. Enteral
b. ParaEnteral
a. Enteral
More predictable quantity
a. Enteral
b. ParaEnteral
b. ParaEntral
Absorbed by small intenstine
a. Enteral
b. ParaEnteral
a. Enteral
Drug must have high lipid solubility
a. Enteral
b. ParaEnteral
a. Enteral
What is “First Pass Effect”?
metabolism/destruction of drug in liver before reaching site of action, only fraction of does goes into blood stream. Blood supply dumping out of stomach and into SI (so sublingual wouldn’t have this)
Subject to first pass effect
a. Enteral
b. ParaEnteral
a. Enteral
Not subject to “First pass Effect”
a. Enteral
b. ParaEnteral
b. ParaEnteral
Examples: oral, sublingual, rectal
a. Enteral
b. ParaEnteral
a. Enteral
however sublingual is not subject to first pass
Examples: injection, IV, IA, Sub-Q, IM, TD, Topical, Intrathecal, Inhaled; Spine
a. Enteral
b. ParaEnteral
b. ParaEnteral
What is Bioavailability?
% of drug administered that reaches the blood stream
If you inject 100mg of a drug and 10mg makes it, what is the bioavailability?
10/100 = 10% bioavailability
What two factors affect bioavailability?
- Depends on route of administration and the drug’s ability to cross membrane barriers
- Depends on extent of first pass metabolism
Where can weak acids be absorbed?
stomach pH 1 to 3 - drugs are neutral / no overall electronic charge in stomach
Where can weak bases be absorbed?
Duodenum pH 5 to 7 (cannot passively go through lipid layer in stomach, not neutral in duodenum and be be absorbed where as acids cannot.
How are the vast majority of drugs absorbed?
Passive Divvusion
What are the 4 methods of drug absorption?
- Passive Diffusion
- Active Transport
- Facilitated Diffusion (ion or small molecule pumped out and back in)
- Endocytosis
What 4 things are involved with distribution or moving the drug throughout the body?
- Tissue Permeability
- Blood Flow
- Plasma Protein Binding
- Subcellular Protein Binding
What are 3 factors of tissue permeability?
- High lipid soluble molecules cross membranes more easily
- Solubility concerns
- Membrane permeability
What are the two factors of blood flow?
- Bloodstream will carry drugs to highly-perfused organs
2. Can be affected by disease
What are the two factors of plasma protein binding?
- Reversible bonds
2. Bound portion of drug doesn’t have therapeutic effect and is not elimated
What is a factor of subcellular protein binding?
Drug gets trapped within the cell (usually in the lysosome)
Example: anti-depressants
Positive artieriole pressure ____
draws drug via blood into tissue spaces
Negative venule pressure ____
pulls drug from tissue back into blood
Drug that is bound to plasma protein cannot leave the blood to distribute into tissues and is ___
inactive
Drug that is unbound (free) may distribute from blood to tissues and is ___
active
High Serum Protein Binding
Lots of drug will attach to protein but as it is absorbed from the blood into the tissues, drug will be released from protein to establish equilibrium.
Low Serum Protein Binding
Very soluble so will have a lot free in the blood and available to be absorbed into the tissues
What is Vd?
volume of distribution = amount of drug administered / concentration of drug in plasma
if Vd = Total amount of body water
uniform body distribution
if Vd > Total amount of body water
drug is being concentrated in the tissues
if Vd
drug is being retained in the bloodstream (due to plasma protein binding for example)
If you inject 100mg of a drug into 100ml of water and stir, Vd = ?
there will be 1.0mg/ml in the solution and can confirm this by drawing 1.0 mL of water, it will contain 1.0mg of drug
Now inject 100mg of a drug into an unknown volume and stir. If we draw 1.0m and find that there is 2.0 mg/mL, how much water was in the box (Vd)?
50mL
100mg/50mL = 2 mg/mL