SITI HAJAR BINTI ZUBER

A145518
PDR/YEAR 2


PHARMACOLOGY : TUTORIAL 1

A . First pass effect is always associated to oral drug administration . What is first pass
effect and its relationship with bioavailability .
Answer :
As drug was administered orally , absorption occurred across gut wall , and the portal
blood delivered the drug to the liver prior to entry into the systemic circulation . First
pass effect is when the drug is either metabolized in gut wall , portal blood but most
commonly in the liver , where liver is responsible for metabolism before the drug
reaches the systemic circulation . Liver can excrete the drug into the bile , thus allowing
first-pass effect . It is heavily related to bioavailability as any sites that contribute to the
metabolism of drug before it reaches systemic circulation reduce its bioavailability , as
the drug had been metabolized and less available in systemic circulation .

B . What are the factors that can influence drugs bioavailability ?
Answer :
Factors that can influence drugs bioavailability are extent of absorption of drugs , first-
pass effect , rate of absorption of drugs and clearance .






C . Briefly explain and justify the trend lines for pentobarbital given orally in aqueous
solution compared to tablet (acid) formulation .
Answer :
The trend line for pentobarbital given orally in aqueous solution increases significantly
before one hour and drop quite a lot as it continue decreasing for another hour . While
for tablet acid formulation , the trend line shows continuous increasing at time range of
two hours without dropping .
The differences are due to differences in size and solution of both dosage . For drug in
aqueous state , the time of action indeed very short as the concentration of drugs was
higher , indicating that the drug reaches plasma in short amount of time , and yet , it
decreases faster as it had been metabolized and ready to be eliminated . The drug
doesnt stay for long in the plasma after it reaches the maximum concentration .
Bioavailability of aqueous drug is at maximum state .
For drug administered in form of tablet acid formulation , the time of action is long
considering the concentration of drug which increasing continuously and slow duration
as it takes two hours to reach sufficient concentration . Yet , it takes times to be
eliminated for clearance as it takes time to be metabolized in the plasma , considering
the state of drug administered . The drug does stay for long in plasma , ready to be
metabolise but not yet ready to be eliminated . It doesnt reach maximum concentration
, or maximum efficacy due to reduced first pass effect , because it may be metabolized
in other part of body before it reaches systemic circulation . Bioavailability of drug also
decrases due to reduced concentration of drugs reaching plasma .