First Pass Effects/ First Pass Metabolism:
- It is defined as the loss of drug through biotransformation before it enters systemic circulation. It may occur through intestine or liver.
a. Intestinal-first pass effect:
- In this type, drug is metabolized in the GI tract by enzymes present either in gut mucosa or lumen before they are absorbed.
- Microorganism in GI tract also inactivate some drugs.
- Such drugs are not suitable by oral administration due to poor bioavailability.
b. Hepatic first-pass effect:
- In this type, drugs are suitably absorbed across the GI tract and enter portal circulation.
- But, they are rapidly and significantly metabolized during the first passage through liver.
- Ex; nitroglycerine, propranolol