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42 Cards in this Set

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  • Back
Pharmacology
Defines as a study of substances that interact with living systems through chemical processes.
Medical Pharmacology
The science of substances used to prevent, diagnose, and treat diseases. Deliberate therapeutic application
Toxicology
The branch of pharm that deals with the undesirable effects of chemicals on living systems
Materia Medica
The science of drug preparation and the medical use of drugs (precursor to pharm)
Pharmacogenomics
the relation of the individual's genetic makeup to his response to specific drugs- close to becoming a practical form of therapy.
agonist
activator
antagonist
inhibitor
receptor
regulatory molecule that interacts with a drug molecule (agonist/antagonist)
Chemical antagonist
interact with other drugs
osmotic agents
interact almost exclusively with water molecules.
xenobiotics
chemicals synthesized outside of the body
(xenos=stranger)
Toxins
Poisons of biological origin
Drug Size
Range from MW 7-60,000 but average range is 100-1000. Too small and it wont fit in the receptor and too large and it cant move about the body
Covalent Bonds
Very strong and usually irreversible in biological conditions, ex: aspirin and COX; DNA-alkylating agents chemotherapy.
Electrostatic Bonds
More common, vary from relatively strong to weaker hydrogen bonds and very weak van der Waals forces. All are weaker than covalent bonds
Hydrophobic bonds
Quite weak and important in the interaction of highly lipid soluble drugs with cell membranes
Chirality
Stereoisomerism; Usually one enantomer is more potent than another. One is also usually more susceptible to degradation by drug-metabolizing enzymes than the other. Drug transporters are stereoselective.
Rational Drug Design
using the characteristics of a known receptor to design a drug to fit that receptor.
Pharmocodynamics
Actions of the drug on the body. Determine the group and classification of the drug
Pharmocokinetics
The actions of the body on the drug. Govern absorption, distribution, and elimination of drugs
Pharmacodynamic Principles
Drug+Receptor-effector-->drug-receptor-effector complex-->effect
D+R-->drug-receptor complex-->effector molecule-->effect
D+R-->D-R complex-->activation of coupling molecules-->effector molecule-->effect
Inhibition of metabolism of endogenous activator-->increased activator--> increased effect
Agonist
Drugs that bind to and activate the receptor , which directly or indirectly brings about the effect
Receptor activation
Brings about a change in conformation . Some receptors incorporate effector machinery in the same molecule, so that the drug binding brings about the effect directly. Others are linked through intervening coupling molecules to a separate effector molecule.
Pharmacologic antagonist
bind to a receptor and compete with and prevent binding by other molecules. (ex: atropine blocking acetlycholine receptors)

Can be overcome by increasing the amount of agonist
Allosteric inhibitor
Bind to the same receptor molecule, but do not prevent binding of the agonist. More agonist wont overcome the allosteric inhibitor
Constitutive activity
Receptor activation occurring in the absence of agonist. May depend on receptor density, concentration of coupling molecules and the number of effectors in the system
Full-agonist
When administered at concentrations sufficient to saturate the pool, activate their receptor-effector system to the maximum extent capable.
Cause a shift of almost all the receptor pool to the Ra-D pool
Partial agonist
Do not evoke as great as a response as full-agonist. They do not stabilize the Ra configuration as fully.
Intrinsic efficacy
How well a drug stabilizes a Ra configuration. Low would be an example of a partial agonist
Neutral antagonism
Binds to the receptor site causes no change in the system (have no effect) until an agonist is present. Then the antagonist will block the receptor sites for the agonist and lower the effect.
Inverse agonist
The drug as a much higher affinity for the inactive state therefore stabilizing the Ri-D pool thereby reducing any constitutive activity. Effects are then opposite the effects of a normal agonist.
Receptors
Endogenous molecules that must be selective in choosing ligands (drugs) and must change its function when bound.
Prodrug
precursor chemical that is readily absorbed and distributed and then converted into the active drug by biological processes
Pharmacokinetic movement of drugs
Must be Absorbed into the blood, Distributed to its site of action, Permeate through barriers and Eliminated at a reasonable rate.
Permeation
-Aqueous Diffusion
-Lipid Diffusion
-Special Carriers
-Endocytosis/exocytosis
Aqueous Diffusion
Occurs within larger aqueous departments of the body (interstitial space, cytosol...) and across the endothelial membrane tight junction and endothelial lining of BV. Driven by concentration gradients and electrical fields if charged.
Lipid Diffusion
Most important limiting factor for drug permeation because they separate the aqueous compartments. Lipid:Aqueous partition coefficient of a drug is how readily it moves between aqueous and lipid media. (can also be dependent on pH)
Special Carriers
These molecules exist for substances that are too large or insoluble to diffuse passively. (peptides, AA and glucose). Use active transport/facilitated diffusion. Is inhibitable. Tend to be less selective when expelling foreign molecules
Multi-drug resistance-associated protein
transporter from the ABC family (ATP-binding cassette) excrete some drugs and their metabolites into urine and bile. Also responsible for some resistance in tumors to chemo drugs.
Endocytosis/Exocytosis
For very large substances.
-Bound to surface receptor
-Engulfed
-Carried into the cell by pinching off of new vesicle
-Released inside the cytosol
ex: intrinsic factor(B12)
Exo:
ex: neurotransmitter substances in nerve endings.
Fick's Law of Diffusion
The passive flux of molecules down a concentration gradient
Flux(molecules/unit time)= (C1 x C2) x Area x Permeability Coefficient /Thickness
C1=higher C2=lower concentration
Henderson-Hasselbalch Equation
log(Pronated/Unpronated)=pKa-pH
Used for weak acids and bases

Adjusting the pH of a solution (in the kidney) can change the reabsorption of that drug