BIO200H5 Lecture Notes - Lecture 15: Mmp2, Metastasis, Cytotoxicity
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Ex; some drugs may be too hydrophobic (high logp) or too hydrophilic (low logp). Pro-moiety should be safe after metabolized away, and also be. Rapidly cleared (so that it doesn"t accukmulate) * uncaps this. The drug should show a greater bioavailability that the prodrug. Decarboxylase enzymes are present in neurons but also in bloodstream, meaning some levodopa will reach the blood, meaning the maximum amount of levodopa isn"t going to the brain, where it needs to be. If given on its own it"ll have a low bioavailability because it gets converted to dopamine in blood and intestines (only 1-3% reaches brain) When you have dopamine that is in blood, it can cause off target effects such as arrhythmia and nausea. Is co-administered carbidopa, which is a decarboxylase inhibitor, it increases lifespan of levodopa as the drug, enhancing the distribution of levodopa to the target tissue. (about 10% reaches brain)
