PHARMACOLOGY
Session 1:
DRUG ACTION
JEFFERSON U. REVILLA, RN
3 PHASES
PHARMACEUTIC
PHARMACOKINETIC
PHARMACODYNAMIC
PHARMACEUTIC PHASE
Also known as DISSOLUTION
In GI tract, drugs need to be in solution to be absorbed
DISINTEGRATION
DISSOLUTION
EXCIPIENTS
PHARMACOKINETIC
PHASE
DISTRIBUTION (Pharmacokinetic Phase)
Is the movement of drug particles from
the GI tract to body fluids by
1. PASSIVE ABSORPTION
is the major process through
which drugs are absorbed into
the body. Does not require any
cellular energy.
2.ACTIVE ABSORPTION /
PINOCYTOSIS
is a process that uses energy (ATP)
to actively move a molecule across a
cell membrane.The molecule may
be large, and it is often a very
important process in drug excretion
in the kidney.
DISTRIBUTION (Pharmacokinetic Phase)
This is the process by which the drug
becomes available to body fluids and body
tissues.
- Blood flow
- Drug’s affinity to the tissue
- Protein binding effect
PROTEIN BINDING EFFECT
As drugs are distributed in the plasma,
many are bound to varying degree with
protein.
HIGHLY PROTEIN-BOUND DRUGS,
MODERATELY HIGH, MODERATELY,
LOW PROTEIN-BOUND DRUGS
The portion of the drug that is bound is
inactive because it is not available to
receptors, and the portion that remains
unbound is FREE (ACTIVE DRUG)
ONLY FREE DRUGS – are active and can
cause a pharmacologic response.
BLOOD BRAIN BARRIER
This is is semi-permeable membrane in the CNS that
protects the brain from foreign substances, drugs, and
pathogens.
Highly lipid- soluble drugs are able to cross the BBB (e.g,
antidepressants, osmotic diuretics, and anxiolytics)
METABOLISM / BIOTRANSFORMATION
(Pharmacokinetic Phase)
↓
Drugs absorbed into the intestine
↓
Drugs absorbed by the portal system
Liver (the most important site of drug metabolism) =
everything that is absorbed from the GI tract first enters the
↓
liver to detoxify many chemicals.
↓
Drugs bind to plasma protein in the circulation
Drug distributed throughout the body
HALF-LIFE
This refers to the time it takes for the amount of drug in the
body to be excreted to one half of the peak level it
previously achieved.
This is used to determine the appropriate timing for a drug
dose or the duration of a drug’s effect on the body.
Factors to consider in determining the half-life of a drug
include:
Absorption rate
Distribution to the tissues
Biotransformation
Excretion
EXCRETION (Pharmacokinetic Phase)
This is the removal of a drug from the
body.
Routes include the skin, saliva, lungs,
bile, and feces.
Kidneys play the most important role.
Creatinine clearance (CLcr) and blood
urea nitrogen (BUN) – common tests
used to determine renal functions
Glomerular filtration rate (GFR) – may
be the best test but it is expensive.
PHARMACODYNAMICS
This is the study of the mechanism of action of drugs in the
body and how they do it.
Drugs usually work in one or four ways:
To replace or act as substitutes for missing chemicals.
To increase or stimulate certain cellular activities.
To depress or slow cellular activities.
To interfere with the functioning of foreign cells, such as
invading microorgansims or neoplasms
(chemotherapeutic agents).
PHARMACODYNAMICS
Receptor sites
- Refers to specific areas at which many drugs are known to act on
cell membranes.
Lock (cell membrane) and key (enzyme) theory
Agonist interaction with receptor site
Competitive antagonism – some drugs react with receptor sites to
block normal stimulation, producing no effect
Noncompetitive antagonism – other drugs react with specific
receptor sites on a cell, and by reacting there, prevent the reaction of
another chemical with a different receptor site on the cell
SELECTIVE TOXICITY
- Refers to the ability of a drug to attack only those systems
found in foreign cells.
ex. Doxurubicin
FACTORS INFLUENCING
DRUG EFFECTS
JEFFERSON U. REVILLA, RN
WEIGHT
AGE
GENDER
PHYSIOLOGIC FACTORS
PATHOLOGICAL FACTORS
GENETIC FACTORS
IMMUNOLOGICAL FACTORS
PSYCHOLOGICAL FACTORS
ENVIRONMENTAL FACTORS
DRUG-DRUG INTERACTIONS
DRUG-FOOD INTERACTIONS
THANK YOU
FOR
LISTENING!!!
