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Determinants of Response to

Drugs

By: Dr. Arlene Maceren Diaz M.D ,FPSECP


Pharmacology Dept.
S.W.U MHAM College of Medicine
A. Biologic Variation
A. Hypersusceptibility or Drug intolerance
Exaggerated response to an ordinary dose of
a drug (supersensitivity)
B. Idiosyncrasy – extreme susceptibility of an
individual to an expected pharmacologic
action of the drug
C. Drug Allergy – is a response that results from
a previous exposure to a drug; it is mediated
by an immunologic mechanism
Biologic Variation
Drug Allergy – is a response that results from a
previous exposure to a drug; it is mediated by an
immunologic mechanism
1. Immediate or anaphylactic drug allergy
-Anaphylaxis, urticaria, angio-neurotic
edema, drug fever, asthma

2. Delayed drug allergy reaction – serum


sickness, contact dermatitis
Drug Allergy
First Exposure

Stimulate
Drug PRODUCTION
Y

OF IgE

IgE settles at
mast cell surface
Drug Allergy
2nd exposure

O Y
Drug
Ag + Ab
Antigen O
reaction

Release of
Degranulation of substances of
mast cell
anaphylaxis
Drug

Acts as
antigen
B. Disease process or pathological
condition that influence response

A. liver disease

B. renal disease
C. Presence of other Drugs
1.Summation
C.I.a. – Additive effect-when two(2)
drugs are given and half of each dose
used simultanously elicits the same
effect as the full dose of either drug use
alone.
Example:
A. Additive Effect = ½ + ½ = 1
Narcotic Analesic =
Codiene = 60 mgs

Aspirin = Non-steroidal Anti-inflammatory = 325 mg


Analgesic

Combine
Aspirin + Codiene
Paralgin or codalgine
=
Stronger analgesic
Lesser GIT Lesser resp. with anti-
irritation depression inflammatory effect
C.I.b. Synergism – If the response is greater
than that of the full dose of either drug

Synergism = 1 + 1 = 3

Trimethoprim = Cotrimoxazole
Sulfamethoxazole +

Extended Broad spectrum


Narrow Spectrum
spectrum
antibiotic
antibiotic
C.1.c- Potentiation = if a second drug
which has no effect , increases the effect of
the first drug. 1+ 0 = 2
Clavulanic Acid
Amoxycillin + = C0-Amoxyclav
(augmentin)

AntibacterialActivity Beta Lactamase Antibacterial,


but easily destroyed inhibitor,BUT but resistant to
by Beta-Lactamase HAS NO the destruction
producing bacteria Antibacterial of Beta
activity -Lactamase
II. Antagonism 1 + 1 = 0
- Diminishing response by opposing actions of 2 drugs

N I ST AG
AGO ON
IS
T
ANTAGONIST
AGONIST

Physiological Effect No Effect


Kinds of antagonism

4. Chemical – one drug is rendered inert or inactive


by precipitation, conjugation, oxidation

6. Physiological antagonism – 2 drugs have


opposing action on the same physiologic sites

8. Competitive antagonism – when 2 drugs will


compete on a certain receptor cell and the
antagonist displaces the other drug from the
receptor site.
Example:
D. Antagonism = 1 + 1 = 0
Competitive Antagonism

1 2

Naloxone
Heroin Addiction Antagonist
Agonist Resp.
depression
Opiate
receptor
Example:
D. Antagonism = 1 + 1 = 0
Competitive Antagonism

OUT

Antagonist
Naloxone displaces
Heroin Heroin from receptor
Reversal
Agonist
of effects
esp. resp.
depression
IV. Pharmacokinetic antagonism – drugs may affect
efficacy of other drugs by:

a. Altered absorption from GIT


b. Reduce binding to plasma protein
c. Altered renal excretion
d. Inhibition of metabolic degradation
e. Induction of metabolic degradation

Altered dose
– response due to special features of drug
metabolism.

a. Tolerance
b. Tachyphylaxis
c. Cumulative effect
TOLERANCE- when there is a diminishing response
to an ordinary dose of a drug that is administer
over a period of time
Causes :
3. Drug inactivation by the liver microsomal
enzyme- this called pharmacokinetic tolerance or
drug disposition tolerance.
2. When there are less receptor sites available
receptor downregulation.
Cross –tolerance=when an individual develops tolerance
to a group of drugs which are pharmacogically related.
Example: If a patient develop tolerance to diazepam
(valium); which belongs to a class called
benzodiazepines he may also develop to another
benzodiazepine drug.

Tachyphylaxis = a rapidly developing tolerance,or a


phenomenom of acute acquired tolerance.
• Cumulative effect – the effects of previously
administered doses is superimposed to the
effects of succeeding doses.
causes:
3. Absorption of the drug is more rapid than
excretion
2. Drug metabolism is slow in cases of liver
disease
3. There is normal absorption but slow
excretion of the drug such as in renal failure

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