FUNDAMENTAL CONCEPTS OF PHARMACOLOGY:

DRUGS & THE BODY

LEARNING OBJECTIVES
 Describe how body cells respond to the presence of drugs that can
alter
their function.
 Outline the process of dynamic equilibrium that determines the
actual
concentration of a drug in the body.
 Explain the meaning of half-life of a drug and calculate the
half-life of given drugs.
 List factors that can influence the actual effectiveness of drugs
in the body.
 Define drug–drug, drug–alternative therapy, drug–food, and
drug–laboratory test interactions.

Pharmacodynamics, PD
- Drug action and mechanism
- is the study of what a drug does to the body

Pharmacokinetics, PK
- Absorption, Distribution, Metabolism, Excretion
- is the study of what the body does to a drug
- Basic Concepts: Pharmacokinetics = (drug/poison)+(Motion)
- Study of drug movement throughout the body
- the main processes involved: LADME
Basic Concepts:
Study of: Liberation, Absorption, Distribution, Metabolism,
Exretion of drugs
Critical concentration: A.K.A. Therapeutic serum level
Purpose of loading dose: to reach critical concentration early

LIBERATION - describes the way that a drug is realeased from its

administered/dosage form

ABSORPTION - the process of a drug moving from its site of delivery

into the bloodstream
- Factors that affect Drug Absorption:
Exercise: more blood flow to muscles, less to GIT-Slow
absorption pH: acidic drugs are best absorbed in acidic
environment
Solubility: liquids absorbed faster than solids
Blood flow: the richer the BS, the faster
Pain: slows down gastric emptying rate-slow absorption
Stress: may cause vasoconstriction-slow absorption
Food: may interfere with drug absorption

- Vital facts - Safest way to deliver drugs: Oral route

- Ideal time for giving oral drugs: 1hour ac/2hours
pc
- Gender differences:
Males - more muscles - reaches peak levels
faster

DISTRIBUTION - movement of a drug from its site of absorption to its

site of action
- Blood flow to tissues:
1st organs to receive drug:
Highly vascular organs - Eg: Liver, kidneys, brain

- Factors that affect Drug Distribution:

Plasma-protein binding: Plasma CHONs bring meds to their
binding sites/excretion
Blood volume: Lesser drug dose needed if FVD (+)
Obesity: Blood flows through fat slowly
Receptor combination

- Barriers to Drug Distribution

Blood brain barrier: drug must be lipid-soluble and loosely
attached to proteins
“Only lipid soluble drugs will get across blood-brain
barrier.”
Most antibiotics: Not lipid soluble
Placenta: Most drugs can pass thru the placenta

BIOTRANSFORMATION OF DRUG (Metabolism)

 - Vital facts:
Definition: Process by which a drug is converted to a less
active form
Major site: Liver
By-products: Metabolites
Types of metabolites: Active and inactive
Impaired metabolism in: Older age, liver disease

DISTRIBUTION:
The First-Pass Effect: a phenomenon of drug metabolism whereby
the concentration of a drug is greatly
reduced before it reaches the systemic
circulation

Drug taken orally → Absorbed via the small intestines →

Directly into the portal venous system → Drug is broken down into
metabolites by liver enzymes → Deactivate metabolites → Excreted
from the body → Activated metabolites → exerts effect on
tissues

EXCRETION:
- Vital Facts:
Definition: Process by which metabolites and drugs are
eliminated from the body
Common route of excretion: Urine
Other routes: Feces, saliva, seat, breast milk
Effect of old age: Decreased renal function

- Useful Concepts:
Half-life: t 1/2 (Half-life x 8 = removal from body)
- the time it takes for a medication to lose half
of its pharmacologic or physiologic effect

Determining the Impact of Half-Life on Drug Levels

*A patient is taking a drug that has a half-life of 12
hours. You are trying to determine when a 50mg dose of the
drug will be gone from the body:
 In 12 hours, half of the 50mg (25mg) would be in the
body.
 In another 12 hours (24 hours), half of 25 mg (12.5mg)
would remain in the body.
 After 36 hours, half of 12.5mg (6.25mg) would remain.
 After 48 hours, half of 6.25mg (3.125mg) would remain.
 After 60 hours, half of 3.125mg (1.56mg) would remain.
 After 72 hours, half of 1.56mg (0.78mg) would remain.
 After 84 hours, half of 0.78mg (0.39mg) would remain.
 Twelve more hours (for a total of 96 hours) would
reduce the drug amount to 0.195mg.
  Finally, 12 more hours (108 hours) would reduce the
amount of the drug in the body to 0.097mg, which would
be quite negligible.
 Therefore, it would take 4 1/2 to 5 days to clear the
drug from the body.

To calculate half-life: there is a formula but the easiest way to

decrease count
Example: half-life is 1 hour
Start 100%
1 hr. 50%
2 hrs. 25%
3 hrs. 12.5%
4 hrs. 6.25%
Half-life of ‘xyz’medication is 1 hr. After 3 hours,
what percentage of the medication will be left?
= 12.5%

Practice questions:
Half-life of 500mg medication is 2 hours.
A. After 8 hours, how many mg of the medication will be left?
= 31.25mg

B. How many hours it would take to clear the drug from the body?
= 24-26 hours

Peak level: 15-30 minutes after giving the dose

Trough level: 15-30 minutes before giving the next dose