Lesson Proper

Pharmacodynamics

 The study of the interactions between the chemical components of

living systems and the foreign chemicals, including drugs that enter
those systems.
 Drugs work as:
o Act/replacement to missing chemicals
o Increase/Decrease a certain cellular activity
o Interferes in the functioning of foreign cells (invading
microorganisms)

Receptor Sites

 Specific areas on cell membranes that react with certain chemicals

to cause an effect within the cell.
 Agonists – Drugs that interact directly with receptor sites to cause
the same activity that natural chemicals would do.
 Competitive Antagonists – Drugs that react with receptor sites to
block normal stimulation, producing no effect
 Non-Competitive Antagonists – Drugs that prevent the reaction of
another chemical with a different receptor site on a cell.

Selective Toxicity

 The ability of a drug to attack only those systems found in foreign

cells.
 Example: Penicillin - affects an enzyme system unique to bacteria,
causing bacterial cell death without disrupting normal human cell
functioning.
Pharmacokinetics

 The study of absorption, distribution, metabolism

(biotransformation), and excretion of drugs.
 Pharmacokinetic Considerations:
1. Onset of drug action
2. Drug half-life
3. Timing of the peak effect
4. Duration of drug effects
5. Metabolism/Biotransformation of the drug
6. The site of excretion

Critical Concentration

 The amount of a drug that is needed to cause a therapeutic effect

Loading Dose

 The use of a higher dose than what is usually used for treatment to
allow the drug to reach the critical concentration sooner
 Recommended if the desired effects are needed quickly

Dynamic Equilibrium

 The actual concentration that a drug reaches in the body results

from a dynamic equilibrium involving several processes
1. Absorption from the site of entry
2. Distribution to the active site
3. Biotransformation (metabolism) in the liver
4. Excretion from the body
I. Absorption
 Refers to what happens to a drug from the time it is
introduced to the body until it reaches the circulating fluids
and tissues.
 Factors That Affect Absorption of Drugs
o Intravenous - None: direct entry into the venous
system
o Intramuscular
1. Perfusion/blood flow to the muscle Fat content
2. Temperature of the muscle: cold causes
vasoconstriction (↓absorption), heat causes
vasodilation (↑absorption)
 o Subcutaneous
1. Perfusion/blood flow to the tissue
2. Tissue fat content
3. Temperature of the tissue: cold causes
vasoconstriction (↓absorption) ; heat causes
vasodilation (↑absorption)
o PO (oral)
1. Acidity of stomach
2. Length of time in stomach
3. Blood flow to gastrointestinal tract
4. Presence of interacting foods/drugs
o PR (rectal)
1. Perfusion/blood flow to the rectum
2. Lesions in the rectum
3. Length of time for absorption
o Mucous membranes (sublingual, buccal)
1. Perfusion/blood flow to the area
2. Mucous membranes integrity
3. Presence of food/smoking
4. Length of time in area
o Topical (skin)
1. Perfusion/blood flow to the area
2. Skin integrity
o Inhalation
1. Perfusion/blood flow to the area
2. Lung lining integrity
3. Proper administration capability
 Absorption Processes
o Passive Diffusion - major process through which drugs are
absorbed into the body. Does not require energy.
o Active Transport - a process that uses energy to actively
move a molecule across a cell membrane.
II. Distribution
 involves the movement of a drug to the body’s tissues
 factors that can affect distribution:
o Drug’s lipid solubility
o Ionization and the perfusion of the reactive tissue
 Blood–Brain Barrier
o An intricate protective system of cellular activity that
keeps foreign bodies away from the CNS.
 o Drugs that are highly lipid-soluble have higher chances
to penetrate this system and the CNS.
o Almost all antibiotics are not lipid soluble and cannot
cross the blood–brain barrier.
III. Biotransformation
 The process by which drugs are changed into new, less active
chemicals.
 Also known as drug metabolism
 First Pass Effect – A phenomenon of drug metabolism where
orally taken drugs’ concentration is greatly reduced before it
reaches the systemic circulation.
IV. Excretion
 The removal of a drug from the body. The skin, saliva, lungs,
bile, and feces are some of the routes used to excrete drugs.
 The kidney is the main organ for excretion
Half-life
 The time it takes for the amount of drug in the body to
decrease to one half of the peak level it previously achieved.

Factors influencing drug effects

1. Weight
2. Age
3. Gender
4. Physiological factors—diurnal rhythm, electrolyte balance,
acid–base balance, hydration
5. Pathological factors—disease, hepatic dysfunction, renal
dysfunction, gastrointestinal dysfunction, vascular disorders,
low blood pressure
6. Genetic factors
7. Immunological factors—allergy
8. Psychological factors—placebo effect, health beliefs,
compliance
9. Environmental factors—temperature, light, noise Drug
tolerance
10. Cumulation effects
11. Interactions
 Pediatric Doses
1. Fried’s Rule
 infant's dose ( <1 year) = infant's age (in months)
150 months
X average adult dose
 2. Young’s Rule
 child's dose (1–12 year) = child's age (in years)
child’s age (in yrs) + 12
X average adult dose
3. Clark’s Rule
 child's dose = weight of child (in pounds)
150
X average adult dose
4. Surface Area Rule
 child's dose = surface area of child (in square meters)
1.73
X average adult dose

Drug–Drug or Drug–Alternative Therapy Interactions

 This can occur in:
1. Absorption site – one drug prevents/enhances the absorption
of another drug.
Example: Tetracycline cannot be absorbed if the client
recently took calcium supplement/calcium products and
still present on the GI Tract.
2. Upon distribution – Drugs compete for the protein-binding
sites. One drug prevents the other drug to be transported to
reactive tissues
Example: Methotrexate, a chemotherapeutic drug, if taken
with aspirin, will be excreted a lot, because aspirin is more
competitive for the sites.
3. During Biotransformation – drugs can enhance/block the
metabolism other drugs.
Example: Warfarin’s biotransformation will be increased
when taken with barbiturates. This means that the client will
need higher doses in order to achieve a desired effect.
4. During Excretion – Drugs compete for excretion, therefore
leading to accumulation and toxic effects of the drugs least
excreted.
Example: Quinidine and Digoxin, when taken together,
affects the excretion of Digoxin. This leads to increased serum
level of Digoxin of the client, because digoxin cannot be
excreted.
5. The action site – drugs can be antagonistic to another drug,
meaning it can oppose the effect of one another, which leads
to no therapeutic effect.
 Example: Antihypertensive drugs’ effects are negated if
taken with antihistamines (anti-allergy), because
antihistamines elevate blood pressure. Also antidiabetic
medications, which lowers blood sugar, should not be taken
with the herb Ginseng, because it also lowers blood sugar,
but with little to no control, that will lead to loss of blood
sugar control.
Drug-Food Interaction
 Some food ↑ acid production, therefore speeding the breakdown
of drugs, that will ultimately prevent absorption and distribution
 Examples:
1. Tetracycline should not be taken with Iron and Calcium
2. Grapefruit juice affects liver enzymes for up to 48 hours, this
will ↑ or ↓ the serum level of drugs

Drug-Laboratory Test Interaction

 Some of the laboratory result ↓ or ↑, is caused by drugs, and not the
body’s own reaction or response
 Example: Dalteparin (used to prevent deep vein thrombosis after
abdominal surgery) may cause increased levels of the liver enzymes
aspartate aminotransferase and alanine aminotransferase with no
injury to liver cells or hepatitis.