PT Chapter 10-Basic Biopharmaceutics

Site of Action

Location where an administered drug produces an effect

Receptor

Cellular material at the site of action that interacts with the drug

Selective Action

Characteristic of a drug that makes its action specific to certain receptors and tissues

Objective of Drug Therapy

To deliver the right drug, in the right concentration, to the right site of action, and at the right time to produce the desired effect.

Agonist

Drugs that activate receptors to accelerate or slow normal cellular function.

Antagonist

Drugs that bind with receptors but do not activate them. They block receptor action by preventing other drugs or substances from activating them.

Biopharmaceutics

The study of the factors associated with drug products and the physiological processes, and the resulting systemic concentrations of the drugs.

Minimum Effective Concentration(MEC)

The blood concentration needed for a drug to produce a response.

Therapeutic Window

A drug's blood concentration range between its MEC and MTC

Onset of Action

The time MEC is reached and the response occurs

Minimum Toxic Concentration(MTC)

The upper limit of the therapeutic window. Drug concentrations above the ? increase the risk of undesired effects

Duration of Action

The time drug concentration is above the MEC

ADME Processes

Blood concentrations are the result of four simultaneously occurring processes: ?

Disposition

A term sometimes used to refer to all the ADME processes together

Elimination

The processes of metabolism and excretion.

Passive Diffusion

The movement of drugs from an area of higher concentration to lower concentration

Hydrophilic

Capable of associating with or absorbing water

Active Transport

The movement of drugs from an area of lower concentration to an area of higher concentration. Cellular energy is required.

Absorption

The movement of the drug from the dosage formulation to the blood.

Gastric Emptying Time

The time a drug will stay in the stomach before it is emptied into the small intestine.

Protein Binding

The attachment of a drug molecule to a plasma or tissue protein, effectively making the drug inactive, but also keeping it within the body.

Complexation

When different molecules associate or attach to each other.

Metabolite

The substance resulting from the body's transformation of an administered drug.

Enzyme

A complex protein that catalyzes chemical reactions

Enzyme Induction

The increase in hepatic enzyme activity that results in greater metabolism of drugs.

Enzyme Inhibition

The decrease in hepatic enzyme activity that results in reduced metabolism of drugs

Enterohepatic Cycling

The transfer of drugs and their metabolites from the liver to the bile in the gallbladder, then into the intestine, and then back into circulation

First Pass Metabolism

The substantial degradation of an orally administered drug caused by enzyme metabolism in the liver before the drug reaches systemic circulation

Glomerular Filtration

The blood filtering process of the nephron

molecular

When a drug produces an effect, it is interacting at a ? level with cellular material or structure.

True

True or False: Receptors are located on the surfaces of cell membranes and inside cells

receptor

When drug molecules bind with a ?, they can cause a reaction that stimulates or inhibits cellular functions

True

True or False: Receptors can be changed by drug use

Blood Concentrations

? are the result of four simultaneously occurring processes, absorption, distribution and excretion.

ionized

In solutions, when acids dissociate they become ?

unionized

In solutions, when bases dissociate, they become?

biological membranes

Besides the four ADME processes, a critical factor of drug concentration and effect is how drugs move through ?

Biological membranes

? are complex structures composed of lipids(fats) and proteins

Distribution

? involves the movement of a drug within a body once the drug has reached the blood.

Drug metabolism

? refers to the body's process of transforming drugs.

liver

The primary site of drug metabolism in the body is the ?

Enterohepatic Cycling

Occurs when a drug is secreted into the intestines along with the bile and reabsorbed back into the blood circulation

Bioequivalency

The comparison of bioavailaility between two dosage forms

Bioavailability

The relative amount of an administered dose that reaches the general circulation and the rate at which this occurs.

FDA

Government agency that requires drug manufacturers to perform bioequivalency studies on their products before they are approved for marketing.

Pharmaceutical Equivalent

Drug products that contain identical amounts of the same active ingredient in the same dosage form

Pharmaceutical Alternative

Drug products that contain the same active ingredient, but not necessarily the same salt form, amount, or dosage form.

Therapeutic Equivalent

Pharmaceutical equivalents that produce the same effects in patients.

lipid soluble

Unionized drugs are more ?

small intestine

Most drugs given orally are absorbed into the blood from the ?

intravenous

Which route of administratinon does not have an absorption step ?

by any route other than oral

To avoid first-pass metabolism, administer the drug ?

basic drug in high Ph urine

What circumstance will result in a drug undergoing urinary reabsorption

absolute

To determine the bioavailability of one product, it must be compared to another product. If the second product is an intravenous solution, the bioavailability is termed ?

Enterohepatic Cycling

The transfer of drugs and their metabolites from the liver to the bile in the gall bladder and then into the intestine

True

True or False: Antagonists bind to cell receptors but do not activate them.

False

True or False: Cell membranes generally absorb hydrophilic drugs more easily than hydrophobic ones

False

True or False:Most drugs and metabolites are excreted by the liver