Introduction Flashcards
the body of knowledge concerned with the action of chemicals on biologic systems
Pharmacology
area of pharmacology concerned with the use of chemicals in the prevention, diagnosis, and treatment of disease, especially in humans
Medical Pharmacology
he area of pharmacology concerned with the undesirable effects of chemicals on biologic systems.
Toxicology
describes the effects of the body on drugs, for example, absorption, metabolism, excretion, etc.
Pharmacokinetics
denotes the actions of the drug on the body, such as mechanism of action and therapeutic and toxic effects.
Pharmacodynamics
Many drugs found in nature are ___ molecules that create a basic (alkaline) pH in solution, usually as a result of amine groups in their structure.
Alkaloids
Many biologically important endogenous molecules and exogenous drugs are optically active; that is, (2)
they contain one or more asymmetric centers and can exist as enantiomers
such enantiomers may be metabolized at different rates in the body, with important clinical consequences.
Most drugs, however, have MWs between
100 and 1000
are often poorly absorbed and poorly distributed in the body
a. MWs smaller than 100
b. MWs larger than 1000
B
are rarely sufficiently selective in their actions
a. MWs smaller than 100
b. MWs larger than 1000
a. MWs smaller than 100
Bond found between drugs and receptors
covalent bonds
(which usually result in irreversible action)
electrostatic bonds (somewhat weaker reversible)
hydrogen bonds, van der waals, hydrophobic (weaker bonds)
Most protein drugs (“biologicals”) are commercially produced in
cell, bacteria, yeast cultures using recombinant DNA technology
If drugreceptor binding results in activation of the receptor molecule, the drug is termed
agonist
if inhibition results, the drug is considered an
antagonist
T or F
Few drugs are enzymes
True
Quantitation of the effects of drug receptor interaction as a function of dose (or concentration) yields
dose-response curves
provide information about the nature of the drug-receptor interaction
dose-response curves
These drugs do not act on endogenous receptors but on substrate molecules.
Enzymes (drugs)
Substances that act on biologic systems at the chemical (molecular) level and alter their functions
Drugs
The molecular components of the body with which drugs interact to bring about their effects
Drug Receptor
The phase of drug movement from the site of administration into the tissues
Distribution phase
The phase of drug inactivation or removal from the body by metabolism or excretion
Elimination phase
Absorption of material across a cell membrane by enclosing it in cell membrane material and pulling it into the cell, where it can be processed or released.
Endocytosis:
Expulsion of material from vesicles in the cell into the extracellular space
Exocytosis
Movement of a molecule (eg, drug) through the biologic medium
Permeation
The actions of a drug on the body, including receptor interactions, doseresponse phenomena, and mechanisms of therapeutic and toxic actions
Pharmacodynamics
The actions of the body on the drug, including absorption, distribution, metabolism, and elimination. Elimination of a drug may be achieved by metabolism or by excretion. Biodisposition is a term sometimes used to describe the processes of metabolism and excretion
Pharmacokinetics
A specialized molecule, usually a protein, that carries a drug, transmitter, or other molecule across a membrane in which it is not permeable, eg, Na+/K+ ATPase, serotonin reuptake transporter, etc
Transporter
An effect on the inheritable characteristics of a cell or organism—a mutation in the DNA; usually tested in microorganisms with the Ames tes
Mutagenic
An effect of inducing malignant characteristics
Carcinogenic
An effect on the in utero development of an organism resulting in abnormal structure or function; not generally heritable
Teratogenic
An inactive “dummy” medication made up to resemble the active investigational formulation as much as possible but lacking therapeutic effect
Placebo
A clinical trial in which the investigators—but not the subjects—know which subjects are receiving active drug and which are receiving placebos
Singleblind study
A clinical trial in which neither the subjects nor the investigators know which subjects are receiving placebos; the code is held by a third party
Doubleblind study
Investigational New Drug Exemption; an application for FDA approval to carry out new drug trials in humans; requires animal data
I N D
New Drug Application (NDA); seeks FDA approval to market a new drug for ordinary clinical use; requires data from clinical trials as well as preclinical (animal) data
N D A
Three parts of a clinical trial that are usually carried out before submitting an NDA to the FDA; adaptive trials, combining two or more phases, allow faster processing
Phases 1, 2, and 3 of clinical trials
A known standard therapy, to be used in addition to placebo, to evaluate the superiority or inferiority of a new drug in relation to the other drugs available
Positive control
Drugs developed for diseases in which the expected number of patients is small. Some countries bestow certain commercial advantages on companies that develop drugs for uncommon diseases
Orphan drugs
specific regions of receptor molecules provide the local areas responsible for drug binding. Such areas are termed
A. Inert binding sites
B. Receptor sites / recognition sites
B. Receptor sites / recognition sites
some drugs bind to some nonregulatory molecules in the body without producing a discernible effect. Such binding sites are termed
A. Inert binding sites
B. Receptor sites / recognition sites
A. Inert binding sites
T OR F
Receptor sites / recognition sites play an important role in buffering the concentration of a drug because bound drug does not contribute directly to the concentration gradient that drives diffusion
FALSE
inert binding sites play an important role in buffering the concentration of a drug because bound drug does not contribute directly to the concentration gradient that drives diffusion
T OR F
To produce useful therapeutic effects, most drugs must be absorbed, distributed, and eliminated
TRUE
To reach its receptors and bring about a biologic effect, a drug molecule
must travel from the site of administration (eg, the gastrointestinal tract) to the site of action (eg, the brain).
Drugs that do not readily diffuse through membranes may be transported across barriers by mechanisms that carry similar endogenous substances.
A. Aqueous diffusion
B. Lipid diffusion
C. Transport by special carriers
D. Endocytosis
C. Transport by special carriers
the passive movement of molecules through lipid bilayer cell membranes and other lipid barriers
A. Aqueous diffusion
B. Lipid diffusion
C. Transport by special carriers
D. Endocytosis
B. Lipid diffusion
not governed by Fick’s law and has a maximum capacity, that is, is saturable
A. Aqueous diffusion
B. Lipid diffusion
C. Transport by special carriers
D. Endocytosis
C. Transport by special carriers
process governed by Fick’s law.
A. Aqueous diffusion
B. Lipid diffusion
C. Transport by special carriers
D. Endocytosis
A. Aqueous diffusion
B. Lipid diffusion
occurs through binding of the molecule to specialized components (receptors) on cell membranes, with subsequent internalization by infolding of that area of the membrane. The contents of the resulting intracellular vesicle are subsequently released into the cytoplasm of the cell.
A. Aqueous diffusion
B. Lipid diffusion
C. Transport by special carriers
D. Endocytosis
D. Endocytosis
the passive movement of molecules through the watery extracellular and intracellular spaces. The membranes of most capillaries have small waterfilled pores that permit the aqueous diffusion of molecules up to the size of small proteins between the blood and the extravascular space.
A. Aqueous diffusion
B. Lipid diffusion
C. Transport by special carriers
D. Endocytosis
A. Aqueous diffusion
permits very large or very lipidinsoluble chemicals to enter cells. For example, large molecules such as proteins may cross cell membranes
A. Aqueous diffusion
B. Lipid diffusion
C. Transport by special carriers
D. Endocytosis
D. Endocytosis
Important
examples are transporters for ions (eg, Na+/K+ ATPase), for neurotransmitters (eg, transporters for serotonin, norepinephrine), for metabolites (eg, glucose, amino acids), and for foreign molecules (xenobiotics) such as anticancer drugs.
A. Aqueous diffusion
B. Lipid diffusion
C. Transport by special carriers
D. Endocytosis
C. Transport by special carriers
T OR F
Most neurotransmitters are released by exocytosis.
TRUE