Drug Discovery, Pharmacokinetics and ADME

Which of the following is NOT one of the three main phases of drug discovery?

The pharmacokinetics phase of drug discovery includes the disintegration of a pill in the GI tract.

List the four main topics that pharmacokinetics addresses.

The process by which orally taken drugs pass from the mouth, throat, and stomach into the upper and lower intestines is known as drug ___________.

Match the following processes with their descriptions:

Why is a balance of hydrophilic and hydrophobic character required for a drug to be absorbed?

According to Lipinski's Rule of Five, orally active drugs generally obey at least two of the rules.

State three of the rules outlined in Lipinski's Rule of Five regarding molecular properties for orally active drugs.

A drug designed to remain in the GI tract is made highly ______ to avoid being absorbed into the bloodstream.

Match the following terms with their definitions.

According to Veber's parameters, what property of a molecule is considered important for drug absorption?

According to Veber's parameters, all rotatable bonds are counted when considering a molecule's effect on drug absorption.

According to parameters discussed, name two factors that would make a drug more easily absorbed in the body

After a drug crosses the gut wall, it enters the ______ and is distributed throughout the body.

Match the following:

What is the 'first-pass effect'?

The blood-brain barrier allows polar drugs to easily enter the brain.

What is the main factor affecting the distribution that prevents polar drugs from entering the brain?

Drugs are seen as ______ chemicals by the body, leading to metabolic processes that modify them.

Match the processes of metabolism and if they interfere or prevent binding interactions with a traget:

Why are non-polar molecules modified by enzyme-catalyzed reactions in the liver?

Drug metabolites are always more active than the original drug.

Provide one sentence outlining the importance of phase I reactions.

Cytochrome P450 enzymes catalyze phase I ______ reactions, which are important in drug metabolism.

Match the terms of the metabolic reactions and their definitions.

What is the primary role of cytochrome P450 enzymes in drug metabolism?

Individuals have the same types and amounts of cytochrome P450 enzymes in their livers.

How can some drugs affect the activity of cytochrome P450 enzymes and what are the consequences of this interaction?

In phase II metabolism, molecules such as glucuronic acid are added to drugs by ______ enzymes.

Identify drug-drug interactions:

Why are drugs ideally designed to be resistant to metabolism?

The 'first-pass effect' applies to drugs administered by injection or inhalation.

Mention three routes of drug excretion.

Metabolic reactions often increase the ______ of drugs to facilitate their excretion.

Indicate where the following route of excretion occur:

Why do hydrophobic structures get reabsorbed down the concentration gradient?

Sublingual administration involves injecting a drug under the skin

What is the name of the drug administration method for anti-asthmatics and general anaethetics?

The gastrointestinal tract (GIT) consists of the mouth, throat, stomach, and the small and ______ intestines.

Match the method of drug administration and it's features:

Which property makes very polar drugs unlikely to cross-cell membranes?

Drugs entering the blood supply through the lungs are largely affected by first-pass metabolism in the liver.

What is meant by the "half life of a drug"?

In order to achieve slow and constant release of a drug and avoid 'spikes' of blood concentration levels, the drug is delivered through the system of ______.