Lecture 1 Flashcards
_______________ is the study of how a drug moves through the body over time. It encompasses absorption, distribution, metabolism, and excretion (ADME).
Pharmacokinetics
Importance of Pharmacokinetics
- Ensures drugs are ________and __________.
- Helps tailor drug dosing to _____________ patients.
- Guides drug development and optimization.
safe and effective
individual
Key Parameters of Pharmacokinetics
_______________: Amount of drug in the bloodstream.
Time: Duration since drug administration.
AUC (_____________): Total drug exposure over time.
Cmax: Maximum drug concentration.
_______: Time taken for the drug’s concentration to halve (half-life).
Concentration
Area Under the Curve
T½
Applications of Pharmacokinetics
Dose _________.
__________ prediction.
Drug-drug interaction assessments.
Personalized medicine strategies
optimization
adverse effect
NCA (___________________)
Directly analyzes concentration-time data.
Does not assume a particular model or number of
compartments.
Common parameters: AUC (Area Under Curve), Cmax
(Maximum Concentration), T½ (Half-life).
Non-compartmental analysis
______________________
Considers a group or population of individuals.
Determines variability in drug concentration profiles
among the population.
Useful in drug development and approval processes.
Population PK
Major Course Objective
To equip you with the tools you need (knowledge of PK!) to determine the proper dose; a dose that will be therapeutic but not toxic in an individual patient possessing a particular set of physiological characteristics
This course has accomplished its purpose only IF:
YOU CAN DO FIVE RIGHTS!
The Five Rights
Right Drug
Right Dose
Right Patient
Right Route
Right Time
Why Study pharmacokinetics?
How much?
How often?
What factors affect response?
What happens between dosing and effect ?
Dynamic relationship between drug, drug product, and the pharmacologic effect
Relationship Between Man and Drug
Dosage _________
Exposure to Drug within _____________
Desired and Adverse effects
Regimen
Body
What happens between dosing and effect?
Pharmacological effects correlated to the _____________ in plasma
drug concentration
What happens between dosing and effect?
Plasma drug concentration: An excellent predictor of _________
drug action
_____________________
Fate of the drug in the body, What the body does to the drug?, The science of the kinetics of ADME (drug absorption, distribution, and elimination (i.e., metabolism and excretion)
Pharmacokinetics
_________________________
* The actions of the drug in the body
* Mechanisms of drug actions
* What drug does to the body?
* Relationship between the drug concentration at the site of action (receptor) and pharmacologic response
Pharmacodynamics (PD)
What is Pharmacokinetics?
The study of the time course of drug absorption and disposition
(distribution and elimination)
* _______________ – rapid and not reversible
* _____________ – rapid and reversible
* Elimination – metabolism and excretion
Absorption
Distribution
Pharmacokinetic Processes
A(bsorption) D(istribution) M(etabolism) E(xcretion)
Four pharmacokinetic processes
Clinical PK ?
Application of PK principles to the safe and effective drug therapy; Pharmacotherapy
Primary goal: enhancing ___________-and decreasing toxicity of a patient’s drug therapy
Multidisciplinary approach to individually optimized dosing strategies based on the patient’ s disease state and patient-specific considerations
efficacy
Why Clinical PK ?
Because all drugs exhibit ____________ effects
* Successful drug therapy achieved by optimally balancing desirable and undesirable effects
* Optimal therapy achieved by:
* Selection of appropriate drug choice
* Accurate disease diagnosis
* Knowledge of clinical state of patient
* Pharmaco-therapeutic management of
disease
undesirable
Why Clinical PK ?
Key Questions:
How _____? Magnitude of therapeutic and toxic responses are functions of dose
How ________? (Time) Magnitude of effect eventually declines following a single dose
How _________? (Cost) Magnitude of side effects, toxicity and cost depend on duration of therapy
much
often
long
Practical focus: Relationship of drug concentrations to drug response
Toxic
Potentially Toxic
Therapeutic
Potentially Subtherapeutic
Subtherapeutic
Therapeutic Drug Monitoring (TDM)
Boundaries between sub-therapeutic, therapeutic and toxic drug concentrations are not absolute
Factors that cause variability in (Cp) and pharmacologic response:
Individual ability to metabolize and eliminate drug (_________), Drug absorption variability, ________ state, ________ states ( extremes of age,obesity), Drug interactions
genetics, disease, physiologic
Therapeutic Drug Monitoring (TDM)
Clinical PK applied to TDM for very ___________ drugs (those with a narrow therapeutic range)
TDM: the use of plasma drug concentration data to develop ______and ______ drug regimens
IF performed properly, the achievement of therapeutic concentrations of a drug will be more rapidly and safely than with the empiric dose changes
TDM along with the observation of clinical effects: the safest approach to optimal drug therapy
Drugs frequently monitored: aminoglycosides, anticonvulsants, and those used in cancer chemotherapy
potent drugs
safe and effective
Process of making drug dosing decisions
A diagnosis is made
A drug is selected
Dosage schedule is designed to reach
a target plasma concentration
Drug is administered
Patient assessments are performed
Drug concentrations are determined
A PK model applied and clinical judgment is used
MTC: Minimum Toxic Concentration
MEC: Minimum Effective Concentration; barely produce an effect
________: reflects the minimum concentration of drug needed at the receptor to produce the desired pharmacological effect
MEC
______: The concentration needed to just barely produce a toxic effect
MTC
PK is the science of the kinetics of _____, whereas clinical PK considers the applications of PK to ___________
ADME
drug therapy
- The quantitative measurement of drug concentrations in the plasma is important to obtain relevant data of systemic _____________
drug exposure
The plasma drug concentration versus time profile provides:
The basic data from which various PK models can be developed that predict the time course of drug action, or adverse response
Enables the development of individualized therapeutic dosage regimens
