Prologation of drug action

PHARMACOLOGY
DEPARTMENT
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Prolonged duration of action of the drug

reduces the frequency of administration and
improves patient compliance.

Various methods to prolong the duration of

drug action are:

1.For orally administered drugs:

*By giving the drug in enteric coated form, e.g. erythromycin.

*By using sustained release preparations, e.g. tab diclofenac SR
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2.For parenterally administered drugs:

*By decreasing the vascularity of the

absorbing surface:
Achieved by adding a vasoconstrictor to the
drug, e.g. adrenaline with local anaesthetics.
Felypressin is an alternative to adrenaline.

*By decreasing the solubility:

Decreasing the solubility of the drug by
combining it with a water-insoluble compound.
e.g.
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Injection penicillin G has a duration of action

of 4-6hrs

Injection penicillin G + procaine: Procaine

penicillin G has a duration of action of 12-
24hrs.

Injection penicillin G + benzathine penicillin G

has a duration of action of 3-4 wks
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*Injecting the drug in oily solution:

e.g. depot progestins

*Pellet implantation: e.g. Norplant for

contraception.

*Pilocarpine ocusert, progestasert and

transdermal patch.
*By increasing the plasma protein binding of
the drug.
e.g. sulphadiazine is less bound to plasma
proteins and has duration of action of 6hrs.
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Sulphadoxine is highly protein bound and so

has a duration of action of 1wks

*By inhibiting drug metabolism:

Anticholinesterases prolong the duration of
action of Ach by inhibiting cholinesterases

*By delaying renal excretion of the drug.

e.g. penicillin/cephalosporins with probenecid
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Summary
The duration of action of drug can be prolonged
by interfering with the pharmacokinetic
processes, i.e. by

1. Slowing absorption

2. Using a more plasma protein bound derivative

3. Inhibiting metabolism

4. Delaying excretion.
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