Pharmacology for Dentistry

(Ben Green) #1
44 Section 1/ General Principles of Pharmacology

synergistic. In the synergism, the drugs can
have action in the same direction or when
given alone, one may be inactive. Synergism
can be additive or supradditive in nature.


ADDITIVE


When the effect of two drugs are in the
same direction. For example when aspirin
is combined with paracetamol the combined
effect is analgesic/antipyretic.


Another important example is
combination of theophylline and ephedrine
as bronchodilator, combination of
sulfonamides as antibacterial etc.


SUPRADDITIVE


In this the effect of combined therapy is
greater than the individual effect of the one
drug. Examples are:



  • Levodopa and peripheral dopa-
    decarboxylase inhibitor, carbidopa or
    benserazide in the treatment of
    parkinsonism.

  • Sulfonamide and trimethoprim (well
    known preparation ‘Septran’) as
    antibacterial.


DRUG ANTAGONISM

Antagonism describes the situation, when
one drug decreases or inhibits the action
of another. The antagonism may be physi-
cal in which the physical property of the
drug can affect the absorption of another
drug, chemical in which two drugs react
chemically and form a biologically inactive
compound. This type of reaction may be
used in the treatment of drug poisoning.
For example in cyanide poisoning nitrites
form methaemoglobin which has high af-
finity for cyanide radical and forms


cyanomethaemoglobin and after sodium
thiosulphate injection forms sodium thio-
cyanate which is easily excreted in urine.
On receptor basis, drug antagonism will
be of two types competitive and noncompeti-
tive antagonism.

COMPETITIVE ANTAGONISM
In competitive antagonism, the
antagonist binds with the same receptor as
agonist. If the log dose response curve with
agonist is obtained in the presence of
antagonist, it will be found that antagonist
has no effect of its own and there is parallel
rightward shift in the dose response curve
of agonist (Fig. 1.5.2) with no change in
shape, slope or maximum response.
In competitive antagonism, the
antagonist reduces affinity i.e. potency of the
agonist.
Example of competitive antagonism are:


  • Acetylcholine (as agonist) – atropine (as
    antagonist).

  • Acetylcholine – d-tubocurarine.

  • Isoprenaline – propranolol.


Fig. 1.5.2: Log dose response curve showing
competitive antagonism.
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