Know One Drug Erin Wu
I chose losartan.
For your molecule:
Note the primary indication, and a secondary indication (even if off label)
The primary indication is hypertension. It is also used for diabetic neuropathy and hypertension with left ventricular hypertrophy. Note and be able to draw the pharmacophore that appears to be responsible for activity. Losartan1 valsartan2
The molecule on the left is losartan and the metabolite is on the right. The metabolite is more active than losartan. The pharmacophore is the entire structure of losartan.
Note a possible or known change in a sub-structure for the molecule. What functional change(s), if any, results as a consequence of the structural change? (for example, is there a change in …show more content…
Describe the biotransformation (what enzyme performs this reaction, etc). If the major metabolite is unknown, predict a biotransformation.
Losartan and EXP3174 metabolite1
Losartan is converted to the EXP3174 metabolite by P450 isozymes (CYP3A4 & CYP2C9) The oxidation of the OH group in Losartan to a carboxylic acid.
The bioavailability or clearance can commonly be altered by a pathophysiologic change or co-administration of a second drug? Give an example of a disease/drug, drug/drug, or drug/food interaction with your molecule.
Concurrent use of Fluconazole and Losartan changes the bioavailability of Losartan. Bioavailability of Losartan increases since fluconazole is a potent inhibitor of the cytochrome P450 2C9, which metabolizes Losartan.
For your drug, draw a drug elimination curve for your drug alone and for the drug interaction mentioned above.
Are there any unique concerns related to ADME for your drug and do ADME characteristics accurately predict clinical activity?
Even though the time for peak plasma level is an hour, the onset of action of Losartan is six
I chose losartan.
For your molecule:
Note the primary indication, and a secondary indication (even if off label)
The primary indication is hypertension. It is also used for diabetic neuropathy and hypertension with left ventricular hypertrophy. Note and be able to draw the pharmacophore that appears to be responsible for activity. Losartan1 valsartan2
The molecule on the left is losartan and the metabolite is on the right. The metabolite is more active than losartan. The pharmacophore is the entire structure of losartan.
Note a possible or known change in a sub-structure for the molecule. What functional change(s), if any, results as a consequence of the structural change? (for example, is there a change in …show more content…
Describe the biotransformation (what enzyme performs this reaction, etc). If the major metabolite is unknown, predict a biotransformation.
Losartan and EXP3174 metabolite1
Losartan is converted to the EXP3174 metabolite by P450 isozymes (CYP3A4 & CYP2C9) The oxidation of the OH group in Losartan to a carboxylic acid.
The bioavailability or clearance can commonly be altered by a pathophysiologic change or co-administration of a second drug? Give an example of a disease/drug, drug/drug, or drug/food interaction with your molecule.
Concurrent use of Fluconazole and Losartan changes the bioavailability of Losartan. Bioavailability of Losartan increases since fluconazole is a potent inhibitor of the cytochrome P450 2C9, which metabolizes Losartan.
For your drug, draw a drug elimination curve for your drug alone and for the drug interaction mentioned above.
Are there any unique concerns related to ADME for your drug and do ADME characteristics accurately predict clinical activity?
Even though the time for peak plasma level is an hour, the onset of action of Losartan is six