Problem Set 7B-2023 odst garwollel sHI SIGH bosta tosits Classwork- Bioavailability/Clearance oms mee adi novy ( 1. The following table shows pharmacokinetic interaction between allopurinol, used i treatment of gout, and 6-mercaptopurine (6-MP), an antineoplastic agent. The AU of 6-MP before and after pretreatment with allopurinol (100mg orally three times a days) following oral and IV administration of 0.8 mmole of 6-MP. Both drugs are eliminated by metabolism in the liver. Oral IV AUC of 6-MP (uM-min) before and after allopurinol treatme before 142 1207 after 716 1405 The half-life of 6-MP was not significantly changed by allopurinol treatment. Whe necessary, use blood/plasma concentration ratio of 0.6. a. Calculate the systemic clearance of 6-MP before and after allopurinol. b. Calculate the systemic blood clearance of 6-MP before and after allopurinol. c. Calculate bioavailability of 6-MP before and after allopurinol. d. Considering the effect of allopurinol on F of 6-MP, provide possible kinetic exp for the enhanced efficacy of 6-MP in the presences of allopurinol.

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Problem Set 7B - - 2023
Classwork- Bioavailability/Clearance
Oral
IV
toms amse adi novi
1. The following table shows pharmacokinetic interaction between allopurinol, used in
treatment of gout, and 6-mercaptopurine (6-MP), an antineoplastic agent. The AUC values
of 6-MP before and after pretreatment with allopurinol (100mg orally three times a day for 2
days) following oral and IV administration of 0.8 mmole of 6-MP. Both drugs are mostly
eliminated by metabolism in the liver.
boista tosits
AUC of 6-MP (uM-min) before and after allopurinol treatment
before
142
1207
The half-life of 6-MP was not significantly changed by allopurinol treatment. When
necessary, use blood/plasma concentration ratio of 0.6.
after
716
1405
a. Calculate the systemic clearance of 6-MP before and after allopurinol.
b. Calculate the systemic blood clearance of 6-MP before and after allopurinol.
Drug A
c. Calculate bioavailability of 6-MP before and after allopurinol.
d. Considering the effect of allopurinol on F of 6-MP, provide possible kinetic explanations
for the enhanced efficacy of 6-MP in the presences of allopurinol.
Drug B
Drug C
Transcribed Image Text:Problem Set 7B - - 2023 Classwork- Bioavailability/Clearance Oral IV toms amse adi novi 1. The following table shows pharmacokinetic interaction between allopurinol, used in treatment of gout, and 6-mercaptopurine (6-MP), an antineoplastic agent. The AUC values of 6-MP before and after pretreatment with allopurinol (100mg orally three times a day for 2 days) following oral and IV administration of 0.8 mmole of 6-MP. Both drugs are mostly eliminated by metabolism in the liver. boista tosits AUC of 6-MP (uM-min) before and after allopurinol treatment before 142 1207 The half-life of 6-MP was not significantly changed by allopurinol treatment. When necessary, use blood/plasma concentration ratio of 0.6. after 716 1405 a. Calculate the systemic clearance of 6-MP before and after allopurinol. b. Calculate the systemic blood clearance of 6-MP before and after allopurinol. Drug A c. Calculate bioavailability of 6-MP before and after allopurinol. d. Considering the effect of allopurinol on F of 6-MP, provide possible kinetic explanations for the enhanced efficacy of 6-MP in the presences of allopurinol. Drug B Drug C
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