Calculate the resulting drug concentration

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Intro: People say the dose makes the poison, actually, the dose determines the concentration, and the (local) concentration determines the toxicity (the poison). Antimicrobials exhibit selective toxicity because they target certain microbial enzymes / pathways not found in humans, but too much of anything can kill In vivo (in beings) and in situ (at the site), concentrations are increased by processes of drug Absorption and Distribution, while concentrations are decreased by processes of drug Metabolism and Elimination. Toxicity of a chemical is a function of its concentration over time, and is typically species-dependent. The range of concentrations at which a drug is effective, yet not harmful, is called its therapeutic window. Medication regimens (i.e. dose and frequency) are based on ADMET principles and are designed to achieve and sustain such drug concentrations at the site of action.

3b)Suppose a 100 kg person (~100 liters volume) ingests 5 pills at once, each with 2 grams of medication. Assuming 100% of the drug was instantly absorbed and evenly distributed, and drug metabolism and elimination are insignificant, calculate the resulting drug concentration in vivo (in milligrams per liter). (Realistically, if drug is not effective below this concentration, wont work in pill form!)

3b) The more potent microbial inhibitor would have an IC50 in the (micromolar / nanomolar / millimolar ) range; the more toxic antimicrobial drugs would have an LD50 in the (micromolar / nanomolar / millimolar ) range. Which drug concentration(s) could be suitable for drug therapy? (IC50 / LD50 / either / neither)

3c) Drugs with a large therapeutic window are considered (useless / safer / highly potent / prone to causing side effects). Which type of medication would likely have the most narrow therapeutic window? Consider drug targets, mechanisms of action and selective toxicity (anticancer / antimicrobial / herbicidal / antiparasitic / antifungal)

Reference no: EM1393694

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