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#3.

Basic Pharmacologic Principles


Dr. Erwin Taguinod


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.