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21 Cards in this Set

  • Front
  • Back

What are the two courses a drug can take upon entering the body?

The drug can either be absorbed or liberated before entering into the bloodstream (liberation is more likely for drugs that are ionized in the intestine and can't feely diffuse into the blood)

What is the concentration of drug in the plasma that we measure and what does this ignore?

Free drug, therefore ignoring drug in the plasma that is protein bound and also drug that has settled into extravascular spaces (i.e. the fat if lipophilic)


Which drugs are most likely to go through biotransformation/metabolism?

Drugs that are lipophilic and therefore won't stay in the urine

What influences oral drug efficacy?

Compliance, drug must properly release, drug must dissolve and mix with GI fluids, and it must be absorbed

What is the lag period in drug therapy?

The time it takes for the plasma concentration to rise to a level that begins to provide the therapeutic effect

What is the therapeutic window?

The plasma concentrations where the drug both gives the desired response and avoids the negative side effects

What causes the drug effectiveness to peak at a certain time point post administration?

This occurs when the rate of absorption is matched by the rate of metabolism (excretion if inactivated) and therefore the graph peaks and the rate is zero

Four methods by which a drug can cross a membrane?

Passive diffusion, facilitated diffusion, active transport and endocytosis



What is the driving force for passive diffusion and what drugs are favoured?

The driving force is the concentration gradient and more lipophilic drugs are favoured because they freely pass through the membrane

What is requirement for drugs that use facilitated diffusion?

They have to structurally mimic the endogenous substrate that uses the transporter

What is the advantage and disadvantage of facilitated diffusion?

The process enables the transport of larger more hydrophilic molecules although it is limited by the number of channels available

Why does active transport require energy?

It moves substances against a concentration gradient effectively concentrating them further



What are two common active transport systems, which functions for absorption and which for excretion?

SLC (absorption) and ABC (excretion) proteins




Not all SLC proteins are active transporters

What is the slowest form of absorption and what drugs rely on it?

The slowest method of absorption is endocytosis and it is utilized by protein based drugs



What is bioavailability?

The extent and rate of active drug reaching systemic circulation

What is important to know in addition to drug maximal concentration?

The amount of time it exists at that concentration for

In decreasing order which methods of administration produce the greatest bioavailability?

1. Intravenous


2. Intramuscular


3. Subcutaneous


4. Oral

What influences absorption for IM/SC injections?

The amount of perfusion to the respective tissue

How do GI tract features impact drug absorption?

The microflora can impact the absorbability of a drug along with the GI motility in certain disease states it is sped up so that absorption time is decreased

What five factors affect drug distribution?

Molecular size


Perfusion


pKa of drug and environment pH


Protein binding


Lipophilicity


blood-tissue barriers

Tissue Binding

Drug can bind to other macromolecules near the site of action (some drugs have greater propensity to bind bone and others fat)