PHARMACOKINETICS - describes the absorption, distribution, metabolism and excretion of inhaled and or injected drugs.
PHARMACODYNAMICS - describes the responsiveness of receptors to drugs and the mechanism by which these effects occurs.
PHARMACOKINETICS
DRUG IONIZATION Ionized Nonionized
DRUG ABSORPTION - rate at which a drug leaves its site of administration. - membrane transport
ROUTE OF ADMINISTRATION
DRUG DISTRIBUTION pH of the drugs environment degree of ionization dissociation constant (pKa) protein binding molecular weight lipid solubility
Protein binding - determines the concentration of the drug in the plasma and various other tissues. - acts as a temporary reservoir for a drug that prevents large flactuations in the concentration of the unbound or free drugs. - Albumin, a1-acid glycoproteins
ION TRAPPING
REDISTRIBUTION and STORAGE
DRUG METABOLISM - converts pharmacologically active, lipid soluble drugs to water soluble and often inactive metabolites. - may also result in conversion of an inactive form (prodrug) to an active drug
Phase I Reaction oxidation, reduction, hydrolysis Phase II Reaction conjugation
DRUG EXCRETION
PHARMACOKINETIC PARAMETERS
Clearance - volume of plasma cleared of drug (mL/min) by renal excretion or metabolism, or both in the liver or other organs.
Volume of Distribution - Vd is a calculated number (i.e.,dose of drug administered IV, divided by the plasma concentration) that reflects the apparent volumes of the compartments that constitutes the compartmental model for that drug
Elimination Half-Time - the time necessary for the plasma concentration of drug to decrease 50% during elimination phase.
Context-Sensitive Half-Time - describes the time necessary for the drug concentration to decrease to a predetermined percentage (e.g., 50%, 60%, 80%) after discontinuation of a continuous IV infusion of a specific duration.
Effect-Site Equilibration - the delay between the IV administration of a drug and the onset of its clinical effect reflects the time necessary for the circulation to deliver the drug to its site of action.
Bioavailability - the amount of active drug that is absorbed and reaches the systemic circulation.
PHARMACODYNAMICS
RECEPTORS - are excitable transmembrane proteins that are responsible for transduction of biologic signals. - voltage sensitive ion channels ligand-gated ion channels transmembrane receptors
RECEPTOR AGONIST and ANTAGONISTS AGONIST - a drug that initiates pharmacologic effects after combining with the receptor. - when bound to receptor, induce stimulatory or inhibitory effects that mimic endogenous hormones and neurotransmitters.
ANTAGONIST - bind to receptors but are not capable of eliciting a pharmacologic response. - prevents receptor mediated agonist effects by occupying agonist sites
THERAPEUTIC INDEX - the ratio between the lethal dose (LD50) in 50% of patients and the effective dose (ED50) in 50% of patients. - the higher the therapeutic index of a drug, the safer it is for clinical administration because the LD is far above the ED.
DRUG TOLERANCE - present when a large dose of a drug is required to elicit an effect that is usually produced by the smaller (therapeutic)dose of the drug.
TACHYPHLAXIS
DRUG DEPENDENCE - a psychic or physical state characterized by behavioral responses that include a compulsion to take the drug on a continuous or periodic basis to experience its psychic effects and sometimes to avoid the discomfort of its absence.