14. Drug Absorption of Various
Oral Preparations
Liquids, elixirs, syrups Fastest
Suspension solutions
Powders
Capsules
Tablets
Coated tablets
Enteric-coated tablets Slowest
Dr LOKENDRA SHARMA
15. Pharmacokinetics: Absorption
The rate at which a drug leaves its site of
administration, and the extent to which
absorption occurs.
– Bioavailability
– Bioequivalent
Dr LOKENDRA SHARMA
16. Pharmacokinetics: Metabolism
(also known as Biotransformation)
The biologic transformation of a drug into an
inactive metabolite, a more soluble
compound, or a more potent metabolite.
Liver (main organ)
Kidneys
Lungs
Plasma
Intestinal mucosa
Dr LOKENDRA SHARMA
17. Pharmacokinetics: Metabolism
Factors that decrease metabolism:
Cardiovascular dysfunction
Renal insufficiency
Starvation
Obstructive jaundice
Slow acetylator
Erythromycin or ketoconazole drug therapy
Dr LOKENDRA SHARMA
19. Pharmacokinetics: Metabolism
Delayed drug metabolism results in:
Accumulation of drugs
Prolonged action of the effects of the drugs
Stimulating drug metabolism causes:
Diminished pharmacologic effects
Dr LOKENDRA SHARMA
20. Pharmacokinetics: Excretion
The elimination of drugs from the body
Kidneys (main organ)
Liver
Bowel
– Biliary excretion
– Enterohepatic circulation
Dr LOKENDRA SHARMA
21. Pharmacokinetics
Half-Life
The time it takes for one half of the original amount
of a drug in the body to be removed.
A measure of the rate at which drugs are removed
from the body.
Dr LOKENDRA SHARMA
22. Pharmacodynamics
Drug actions:
The cellular processes involved in the drug and
cell interaction
Drug effect:
The physiologic reaction of the body to the drug
Dr LOKENDRA SHARMA
23. Pharmacodynamics
Onset
The time it takes for the drug to elicit a
therapeutic response
Peak
The time it takes for a drug to reach its maximum
therapeutic response
Duration
The time a drug concentration is sufficient to elicit
a therapeutic response
Dr LOKENDRA SHARMA
24. Pharmacodynamics:
Mechanisms of Action
The ways by which drugs can produce
therapeutic effects:
Once the drug is at the site of action, it can modify
the rate (increase or decrease) at which the cells or
tissues function.
A drug cannot make a cell or tissue perform a
function it was not designed to perform.
Dr LOKENDRA SHARMA
25. Pharmacotherapeutics: Monitoring
The effectiveness of the drug therapy must be
evaluated.
One must be familiar with the drug’s
intended therapeutic action (beneficial)
The drug’s unintended but potential side
effects (predictable, adverse drug reactions).
Dr LOKENDRA SHARMA
30. Pharmacotherapeutics: Monitoring
Interactions may occur with other drugs or food
Drug interactions: the alteration of action of
a drug by:
– Other prescribed drugs
– Over-the-counter medications
– Herbal therapies
Dr LOKENDRA SHARMA
32. Pharmacotherapeutics: Monitoring
Medication Misadventures
Adverse drug events
ALL are preventable
Medication errors that result in patient harm
Adverse drug reactions
Inherent, not preventable event occurring in the
normal therapeutic use of a drug
Any reaction that is unexpected, undesirable, and
occurs at doses normally used
Dr LOKENDRA SHARMA
33. Pharmacotherapeutics: Monitoring
Some adverse drug reactions are classified as
side effects.
Expected, well-known reactions that result in little
or no change in patient management
Predictable frequency
The effect’s intensity and occurrence is related to
the size of the dose
Dr LOKENDRA SHARMA
37. Dr L K Sharma
Oral
• Disadvantages
– Sometimes inefficient - only part of the drug may
be absorbed
– First-pass effect - drugs absorbed orally are initially
transported to the liver via the portal vein
– irritation to gastric mucosa - nausea and vomiting
38. Dr L K Sharma
Oral
• Disadvantages cont.
– destruction of drugs by gastric acid and digestive
juices
– effect too slow for emergencies
– unpleasant taste of some drugs
– unable to use in unconscious patient
39. Dr L K Sharma
First-pass Effect
• The first-pass effect is the term used for the hepatic
metabolism of a pharmacological agent when it is
absorbed from the gut and delivered to the liver via
the portal circulation. The greater the
first-pass effect, the less the agent will
reach the systemic circulation when the agent is
administered orally
40. Dr L K Sharma
First-pass Effect cont.
Magnitude of first pass hepatic effect:
Extraction ratio (ER)
ER = CL liver / Q ; where Q is hepatic
blood flow (usually about 90 L per hour.
Systemic drug bioavailability (F) may be
determined from the extent of absorption
(f) and the extraction ratio (ER):
F = f x (1 -ER)
42. Dr L K Sharma
1. unconscious patients and children
2. if patient is nauseous or vomiting
3. easy to terminate exposure
4. absorption may be variable
5. good for drugs affecting the bowel such
as laxatives
6. irritating drugs contraindicated
Rectal
43. Dr L K Sharma
Parenteral Routes
– Intravascular (IV, IA)- placing a drug directly into
the blood stream
– Intramuscular (IM) - drug injected into skeletal
muscle
– Subcutaneous - Absorption of drugs from the
subcutaneous tissues
– Inhalation - Absorption through the lungs