Principle of Drug Action
DRUG ACTION - is called the pharmacodynamics and pharmacokinetics. The drugsthar enter the human tend tostimulate
certain receptors ,ion channels, act on enzymes or transporter protein
7 PRINCIPLES THAT ALTER THE PACE OF ONGOING ACTIVITY NOT IMPART NEW FUNCTION
Type of drug actions:
1. Stimulation
- Selective enhancement of level of activity of specialized Cells Eg. Adrenaline-heart,Pilocarpine-salivary glans
- Excessive Stimulation: followed by depression Eg.Picrotoxin: convulsions coma & respiratory depression
2. Depression
- Selective diminution of activity of specialized cells..Eg .Barbiturates – CNS Quinidine-heart
- Certain drugs stimulate one type of cells & depress the other. Eg. Acetylcholine
3. Irritation
- Non-selective,noxious effect; less specialized cell
- Mild: Stimulate function…Eg: Bitters increasing salivary & gastric secretion
- Strong: inflammation
4. Replacement
- Use of natural metabolites, hormones or congeners in their deficiency …Eg Levodopa –parkinsonism, Insulin-
diabetes mellitus, Iron –anemia
5. Cytotic Action
- Selective cytotoxic action for invading parasites or cancer cell…Eg.Anti-biotics, Anti-virals, anti cancer drugs
6. Anti-Microbial action
- Prevention , arrest and eradication of infections
- Acts specifically on causative agents
- Example: antibiotics
7. Modification of immune status
- Selective
- Enhancing or depressing the immune status
- Examples;Vaccines,Corticosteroids
DRUGS & THE BODY
The tablet or capsule taken by the mouth goes through 3 phases:
1. PHARMACEUTIC– the drug becomes solution so that it can cross a biologic membrane.
2 Pharmaceutic Phases of a Tablet:
a. Disintegration – breakdown of tablet into smaller particles
b. Dissolution – is the dissolving of smaller particles in GI fluid before absorption
2. PHARMACOKINETIC– how the body handles medication.
Composed of 4 phases
a. Absorption
b. Distribution
c. Metabolism (Biotransformation )
d. Excretion (elimination)
3. PHARMACODYNAMIC – the process by which the drug alters cell physiology or simply how drug changes the
body
PHARMACOKINETIC - Is the process of drug movement to achieve drug action involving 4 process.
1. Absorption
2. Distribution
3. Metabolism (Biotransformation )
4. Excretion (elimination)
1. Absorption
- is the movement of drug particles from the GI tract to body fluids by passive absorption, active absorption
and pinocytosis.
- The process by which the drug passes into the blood stream
The 3 major processes for drug absorption through GI membrane:
Passive absorption – movement from higher concentration to lower concentration
Active absorption – requires a carrier such as enzyme or protein to move the drug against a concentration
gradient. Energy is required.
Pinocytocis – is the process in which cells carry a drug across their membrane by engulfing the drug particles.
Factors affecting the rate of absorption:
a. Route of administration
b. Ability of medication to dissolve
c. Blood flow to the site of administration
d. Body surface area
e. Lipid solubility of medication
Bioavailability – sub category of absorption. It is the percentage of the administered drug dose that reaches the systemic
circulation.
Route of Administration through:
a. Skin – slow absorption due to physical make-up of the skin
b. Mucous membrane and respiratory airways- quickly absorbed because of the tissues contains many blood
vessels
c. Oral med- slow absorption because meds must pass through the GIT
d. Intravenous Injection- produces the most rapid absorption because the route provides immediate access to the
systemic circulation.
Availability of the medication to dissolve depends largely on its form or preparation
1. Solutions & suspensions – already in a liquid state are absorbed readily than tablets and capsules
2. Aid meds (like tablets)- absorbed readily because it pass through gastric mucosa.
When the site contains a rich blood flow supply, (under the tongue) meds are absorbed rapidly.
When medication are in contact with larger surface area, it will be absorbed at faster rate.
o Small intestine absorbed faster rather than the stomach
2. Distribution
- transportation of a drug from its site of absorption to its site of action
After the medication is absorbed, it is distributed within the body to tissues and organs ultimately to its site of
action
NOTE: The rate & extent of distribution depends on the physical & chemical properties of medications.
How is Medication distributed?
1. Through Circulation- carrying of medications though out the tissues and organs of the body after entering the
blood stream.
a. NOTE: When condition exist this will limit the blood flow of the intended sites of action because they are
poorly perfused (passing of blood). Ex: CHF clients have impaired circulation
2. Passage of drug to Plasma Membrane- depends on the membrane permeability
3. Protein Bounding
a. Free drugs are drugs not bound to protein, these drugs are active and can cause pharmacological
response
b. NOTE older adults have less albumin, thus they are prone to medication toxicity
Action of Drugs in the body
1. Drug half-life – is the time required for the elimination process to produce the concentration of the drug to one-
half of the initial administration or by 50%- called as elimination half life
Example
o Half life for an 8hrs.drug
o Initially: 100%
o After 8hrs = 50%
o After 16 hrs=25%
o After 24 hrs =12.5%
o After 32 hrs =6.25%
2. Onset of Action – the time after the administration when the body initially responds to the drug
a. The time it takes to reach the minimum effective concentration after a drug is administered.
3. Peak Plasma Level – the highest plasma level achieved by a single dose when the elimination rate of the drug
equals the absorption rate.
4. Plateau – a maintained concentration of drug in the plasma during a series of scheduled doses.
Duration of Action- the length of time the drug has pharmacologic effects.
Agonist – drugs that produce response
Specific Antagonist – drugs that inhibit or prevent/block the action of the agonist
Loading Dose – a large initial dose when immediate drug response is desired. This is given to
achieve concentration in the plasma.
EXAMPLE:
Digoxin- a digitalis preparation, requires a loading dose when first prescribed.
