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Drug
Substances intended for use in the diagnosis, cure, mitigation, treatment, or prevention of disease
Local Effect
Obtained when the drug product is administered at the site where the pharmacological response is desired either by adsorption or penetration
Systemic Effect
Obtained when the drug released from the drug product enters the blood and/or lymphatic streams and is distributed within the body-or at least several organs-regardless of the site and route of administration
Dosage form (drug product)
Considered to be drug delivery systems that release and deliver drug to the site of action such that they produce the desired effect
Dosage form (drug product)
Designed specifically to meet the patient’s needs including palatability, convenience, and safety
Xenobiotics
Foreign compounds exposed to the biological system
Drug Product Performance
Release of the drug substance from the drug product either for local drug action or for drug absorption into the plasma for systemic therapeutic activity.
measured based on bioavailability
bioavailability
how well the drug is absorbed
biopharmaceutics 1
bioavailability + pharmaceutics 1
BIOPHARMACEUTICS
Provides the scientific basis for drug product design and drug product performance
BIOPHARMACEUTICS
The examination of the interrelationship of the:
physical/chemical properties the drug;
the drug product (dosage form) in which the drug is given and the;
route of administration
BIOPHARMACEUTICS
on the rate and extent of systemic drug absorption
physicochemical property of drug
stability of the drug within the product
drug must be aqueous or liquid form to be absorbed
LUNA
stomach
acidic environment
small intestine
basic environment
Dosage Form
manufacture of product
Dosage Form
rate of dissolution/ release of the drug at the absorption site
route of administration
Design of the drug product
Release of the drug from the drug product
route of administration 1
IV - 100% bioavailability
EV - less than 100% bioavailability
Per Oral - very minimal bioavailability because of first pass effect 1
Biopharmaceutics Therapeutic objective
For rapid relief of symptoms, slow extended action, or chronic use
For local or systemic action
Drug (active pharmaceutical ingredient, API)
Physicochemical properties (solubility, polymorphism, particle size)
Route of administration
Oral, topical, parenteral, inhalational, etc
Drug dosage and dosage regimen
Large or small dose, frequency of doses, patient acceptance, patient compliance
Type of drug product
Orally disintegrating, immediate release, extended release tablets
Transdermal, topical, parenteral, implant, etc
Excipients
Affect drug release
Method of manufacture
Variables in manufacturing process, including weighing, blending, release testing, sterility
Biopharmaceutics and designing drug products: CONSIDERATIONS
Therapeutic objective
Drug (active pharmaceutical ingredient, API)
Route of administration
Drug dosage and dosage regimen
Type of drug product
Excipients
Method of manufacture
PHARMACOKINETICS
A.D.M.E.
The science of the kinetics of drug absorption, distribution, and elimination (ie, metabolism and excretion)
pharmacon
drug
kinesis
movement
L.A.D.M.E
applicable to solid dosage forms
drug input process
increase in the plasma concentration of the drug inside the body
chronological in nature / sequential / sunod sunod in order
drug output process
decline in the plasma concentration
ex. per oral administration
simultaneously / sabay sabay nangyayari
Input processes
Liberation
Absorption
Liberation
the release of the drug from it's dosage form
disintegration - conversion to smallest particles
dissolution - powder/ small particles will be liquid/ aqueous. also known as rate limiting step
rate limiting step
slowest step in every process
Absorption
the movement of drug from the site of administration to the blood circulation
Absorption
Is the process of uptake of the compound from the site of administration into the systemic circulation
Output processes: Disposition of drugs
Distribution
Elimination
Metabolism
Excretion
Drug Disposition
A term used to describe drug distribution and elimination
Distribution
The process by which drug diffuses or is transferred from intravascular space to extravascular space (body tissues)
Distribution
Is the partitioning of drug molecules among numerous locations in the body
drug distribution 1
transfer of the drug from the systemic circulation to the target organs or site of action 1
Elimination
Refers to the irreversible removal of drug from the body by all routes of elimination (metabolism and excretion)
Elimination
Decline in plasma drug concentration observed after systemic drug absorption
Metabolism (Biotransformation)
Process by which the drug is chemically converted in the body to a metabolite //drug to inactive form // WIPE (water soluble, ionized, polar, excretion)
Metabolism (Biotransformation)
Usually an enzymatic process
Excretion
Removal of intact drug
feces/biliary excretion
high molecular weight drugs (exceeds 150), excreted thru
urine/renal
small particle size or molecular weight (>150) drug is excreted through the
ex. non volatile drugs
CLINICAL PHARMACOKINETICS
The application of pharmacokinetic methods to drug therapy
significance of clinical pharmacokinetics
Intra- and interindividual variations will frequently result in either a subtherapeutic or toxic response which may then require adjustment to the dosing regimen
Pharmacodynamics
Refers to the relationship between the drug concentration at the site of action (receptor) and pharmacologic response, including biochemical and physiologic effects that influence the interaction of drug with the receptor
Drug-receptor interaction
Combining of a drug molecule with the receptor for which it has affinity, and the initiation of a pharmacologic response by its intrinsic activity or efficacy
Pharmacokinetic-pharmacodynamic models
Constructed to relate plasma drug level to drug concentration at the site of action and establish the intensity and time course of the drug
Drug exposure
Refers to the dose (drug input to the body) and various measures of acute or integrated drug concentrations in plasma and other biological fluid
Drug response
Refers to direct measure of the pharmacologic effect of the drug
Drug responses measured:
Clinically remote biomarkers
Presumed mechanistic effect
Potential or accepted surrogate
Full range of short-term or long-term clinical effects related to either efficacy or safety
Clinically remote biomarkers
Receptor occupancy
Presumed mechanistic effect
ACE inhibition
Potential or accepted surrogate
Effects on blood pressure, lipids, or cardiac output
Toxicokinetics
Application of pharmacokinetic principles to the design, conduct, and interpretation of drug safety evaluation studies and in validating dose-related exposure in animals (eg., preclinical drug development)
toxicokinetics data obtained:
Aids in interpretation of toxicologic findings in animals and extrapolation of the resulting data to humans
Clinical toxicology
The study of adverse effects of drugs and toxic substances (poisons) in the body