Question

Discuss protein binding, what it means, what are the implications of a drug protein binding percentage and how the protein binding impacts how drugs may interact with each other and the subsequent effect on the patient (provide 2 explicit examples). And, then explain what will happen if the patient is malnourished.

what are ED50 , LD50, TD50: and explain in detail why the matter. Please give 2 examples of each.

Answer 1

Discuss protein binding, what it means,	Protein binding: when a drug enters a body it has to go through process of digestion and in some cases directly enters blood and in others makes its passage to blood. Now, once in blood there are protein polypeptides present in the blood freely these drugs are attracted and attach themselves to these polypeptides this makes them non available for cells. The remaining drug is then accepted by various receptors in the various cells. In this way the drug enters the cells and causes desired effects. Considering this fact the protein polypeptides lessens the cells gateway for drug acceptance, lesser the protein binding the more desired effect of drug
what are the implications of a drug protein binding percentage	Drug Protein binding percentage: the less the drug binds to the protein polypeptides the more it is available and accepted by the cells and desired effects are achieved and if there is more binding then the desired affect is not achieved.
and how the protein binding impacts how drugs may interact with each other	The protein binding directly affects pharmacokinetics and pharmacodynamics of the drug. Decreased plasma protein binding leads to an increase in free plasma fraction causing an increase in volume of distribution and a shorter elimination half-life.
and the subsequent effect on the patient (provide 2 explicit examples).	The binding of drug to plasma proteins is a major determinant of drug disposition. When a drug is bound to the plasma proteins, it is not actively distributed to the site of action to interact with the target tissues. Example warfarin – highly protein bound Phenyl-butazone – low protein bound Combined can cause bleeding disorder
And, then explain what will happen if the patient is malnourished.	If a person is malnourished and has less plasma protein then he requires less dosage of drug as less dosage will cause more effect as there are no loss of drug to the protein
what are ED50 , LD50, TD50: and explain in detail why the matter. Please give 2 examples of each.	ED 50 stands for Median Effective Dose 50% that means the dosage which leads to maximum effect can also be a half life or a drug LD 50 stands for Median Lethal Dose 50 % it is the dose which causes maximum illeffect and potential dangerous to the human life TD 50 stands for Median Toxic effect 50% it is the dose at which some clinically relevant toxic effect is reported. Drugs with small therapeutic time are Warfarin Lithium Digoxin Means small doses don’t give desired effect as they are more protein bound and hence should be given in bolus but there is a constant fear of LD 50 and TD 50 which has a small window and hence strict observation and care is required.