ADV. Pharmacology Exam 1-Part 1

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Paracelsus
who is the father of pharmacology and said “all things are poison and nothing is without poison, only the dose permits something not to be poisonous” DOSE MAKES THE POISON (1493-1541)
Pharmacology
study of interactions of substances with living systems via a biochemical process; applied science; built on knowledge of all other basic sciences
biochemical process in relation to pharmacology
binding to regulatory molecules, activating or inhibiting normal biochemical/physiological processes of the patient, the invading organisms, abnormal cells (cancer), etc.
Pharmacokinetics, Pharmacodynamics, Pharmacotherapeutics, Pharmacocognosy, Pharmacogenetics/Pharmacogenomics, and Toxicology
what are the subgroups associated with pharmacology?
Pharmacokinetics
how the body handles a drug; Absorption, Distribution, Metabolism, and Excretion; impact of systemic pathology and drug dosing such as patients with liver or renal failure
Pharmacodynamics
how drugs produce their effects (desired, toxic); mechanisms of action; interactions between drugs and their receptors; structure activity relationships (SAR); key-lock concept
Pharmacotherapeutics
the clinical use of drugs in the prevention, diagnosis, and treatment/management of diseases or modification of physiology; determination of proper drug and dosage for INDIVIDUAL patients
Toxicology
study of poisons and poisonings including treatment; toxic doses of drugs
Pharmacogenetics/Pharmacogenomics
study of clinical testing of genetic variation that gives rise to differing response to drugs; polymorphisms in drug metabolism, receptors, expression or suppression of genes; personalized medicine
Drugs
these are substances used for prevention of diseases, diagnoses of diseases, treatment and management of diseases; changes the level of biological system’s functionality but CANNOT ALTER the nature of its function
How do drugs act?
via receptors to produce a mechanism of action
Drugs and Receptors
A)these are molecules that interact with specific molecular components of an organism to cause biochemical and physiologic changes within an organism
B)these are macromolecules, upon binding to a drug, mediate those biochemical and physiologic changes
physical nature of drugs
can be solid, liquid or gas; influences the route of administration
carbohydrates, lipids, proteins
3 examples of organic compounds (physical nature of drugs)
lithium, iron, copper
3 examples of inorganic elements (physical nature of drugs)
Aspirin, lidocaine, codeine
3 examples of weak acids or bases (organic drugs) (physical nature of drugs)
physical properties of drug
What determines drug diffusion, absorption, route of administration?
100-1000 molecular weight
What is the range of molecular weight a large drug can be?
lithium
what is the smallest known drug?
chelating agents; stops heparin from working by chelating with another drug
A few types of drugs act via NON-RECEPTOR mechanism…name an example
stereoisomerism
this is a phenomenon of chirality-like putting a glove on another hand; mirror images of the same compound; molecules that have the same molecular formula and sequence of bonded atoms but differ only in 3d orientation of their atoms in space
racemic mixture
a mixture that has equal amounts of left and right handed enantiomers of a chiral molecule
metabolism (enzymes are steroselective)
drug transporters
pharmacokinetics (half life, duration of action and efficacy, toxicity)
what are the different areas that are considered steroselective?
Drug Receptors
these union/interactions result in (mediate) biochemical and physiologic changes within an organism; they play a regulatory role and are macromolecular proteins
primary structure
this protein structure level is a protein amino acid sequence
secondary structure
this protein structure level is when nearby amino acids in polypeptides interact with each other
tertiary structure
this protein structure level is when amino acids that are relatively apart interact with each other
quaternary structure
this protein structure level is when 2 or more polypeptides interact with each other
twisted, folded, hydrophobic, hydrophilic, chemical
Receptors are proteins that are ______ and ______, have ________ centers and ________exteriors with unique binding sites and ______characteristics
neurotransmitters
autocoids
hormones
receptors mediate the actions of endogenous chemical signals which include these 3….
neurontransmitters: ach, norepinephrine, dopamine
autocoids: histamine
hormones: cortisol, insulin, T3 T4
Give one example of each…neurotransmitter, autocoids, and hormones
enzymes
receptors could be ______, transport proteins, and structural proteins
concentration, complexes
the receptor’s affinity for binding a drug determines the __________ of the drug required to form a certain number of drug-receptor _______.
number, receptors
the total _______ of ________ may limit the maximal effect a drug may produce
specificity
drugs have a specific molecular size, shape and electrical charge, which determines its avidity for a particular receptor…what’s this called??
chemical structure of a drug
changes in what of a drug can dramatically increase or decrease a new drug’s affinity for different classes of receptors with resulting alterations in therapeutic and toxic effects?
covalent bonding (extremely strong)
electrostatic (hydrogen bonds, van der waals)
hydrophobic
what are types of bonding forces (drug-receptor binding)? (3)
Acetylcholine, Adrenergic, Histamine
What are the 3 main types of receptors talked about in class?
nicotinic (Nn, Nm), muscarinic (M1M2M3M4M5)
What are 2 subclasses of acetylcholine receptors?
alpha (a1a2a3) beta (b1b2b3)
What are 2 subclasses of adrenergic receptors?
allosteric binding site
a drug binding site adjacent (near to) agonist’s binding site (in the same receptor molecule)?
allosteric activator
drugs acting at the allosteric site that FACILITATE the action of agonist?
allosteric inhibitor
drugs acting at the allosteric site that INHIBITOR the action of an agonist?
agonist
molecules that bind to a receptor that causes a change in the activity of that target
full agonist
molecules binding to a receptor that produces the maximum effect possible
partial agonist
molecules that bind to a receptor that produces sub-maximal effects
inverse agonist
molecules that bind to a receptor that causes an active target to become inactive
antagonist
this is a molecule that inhibits or blocks the target from being activated
competitive and non-competitive
what are 2 types of antagonists?
1)transmembrane ion channel
2)transmembrane receptors coupled w/ G proteins
3)transmembrane receptors with enzymatic cytoplasmic domains
4) intracellular receptors
5) extracellular enzymes
6) cell surface adhesion receptors
What are 6 of the major structural types of receptors? (do not list ach, adrenergic or histamine)
Transmembrane ion channel
this type of receptor has channels that allow the passage of ions and other hydrophilic molecules across the membrane; types include ligand gated, voltage gated and 2nd messenger regulated.
ligand gated channel
this type of channel can be extracellular, within the channel or intracellular; i.e.: nicotinic acetylcholine receptor
cellular response with ligand gated channel can happen in milliseconds, much faster than other molecular signaling systems
what is the biggest difference between the time elapsed between the binding of a ligand-gated channel and the cellular response to other molecular signaling mechanisms?
open, closed, refractory and inactivated
what are the 4 states an ion channel can be in?
local anesthetics
what blocks sodium conductance, preventing the propagation of an action potential?
benzodiazepenes
what drug class is known to potentiate the inhibitory action of GABA, increase chloride conductance resulting in hyper polarization of the cell?
Transmembrane G Protein-coupled Receptors
this type of receptor is the most abundant, receptors are at the the extracellular surface of cell membrane, and receptors transverse the membrane and has intracellular domains that interact with G proteins
1) extracellular ligand couples with cell surface receptor
2)activation of G protein
3)then changes the activity of an effector element
what are the 3 components (usually having to do with amplification) of the transmembrane G-protein coupled receptors?
longer
drugs that bind to transmembrane G protein coupled receptors only bind to its receptor for a short time but the downstream effect is _______.
via the 2nd messenger systems
How does the G-protein receptor activation allow the signal to be amplified??
Transmembrane receptors with Enzymatic cytosolic domains
what type of a receptor transduces an extracellular ligand binding interaction in an intracellular action via receptor-linked enzymatic domain? This is receptor also has 5 types based on cytoplasmic mechanisms
Intracellular receptors
what type of receptor binds drugs that are small lipophilic molecules that could include receptors that are transcription factors, structural proteins, enzymes, signal transduction molecules and has clinical implications of delayed response (lag) 30 minutes to several hours and the effects of a drug that binds can persist for hours or days after drug is cleared or stopped?
extracellular receptors
What type of receptors include acetylcholinesterase and angiotensin-converting enzymes?
cell surface adhesion receptors
what type of receptors are called integrins and include cell-cell adhesion involved in areas such as coagulation, inflammation, immune cells, cancer cells and diseases such as multiple sclerosis?
receptor desensitization
repeated or continuous administration of an agonist or antagonist that leads to changes in the responsiveness of a receptor-USUALLY REVERSIBLE
tolerance(s)
a gradual decrease in drug responses
tachyphylaxis
a rapid (acute) decrease or diminishing drug response
Receptor Down-Regulation
this is produced by agonist-induced decreases in receptor biosynthesis and increases in receptor internalization and degradation, usually occurs over hours to days
Receptor Up-Regulation
this happens when there is a decrease in neurotransmitter ACh quantal release and/or denervation or nerve damage
Dose-Response Curve
the response to a drug that is proportional to the concentration (#) of receptors that are bound (occupied) by the drug. Example: if 50% of receptors are bound then there is a 50% effect.
Emax: E=efficacy
when ALL receptors are bound/occupied; determined by the nature of the receptor and its associated effector system; an agonist can produce this if the dose is taken at HIGH levels; only used in the graded-dose response curve
EC50: Potency
the measure of how much is needed for an effect; it is expressed as the concentration or dose required to produce 50% of the maximum effect; denotes the amount of a drug needed to get this response.
Graded-dose Response
increasing concentration of drug not based on population;when the response of a particular receptor-effector system is measured against increasing concentration of a drug; determines Emax and EC50 of a particular drug; X axis: increasing drug concentration, Y axis: response or drug effect
percentage %
In a graded dose response, the response with each dose of drug is described in terms of a ______ of the maximal response and its plotted against the log dose of a drug
Drug A
If 25mg of drug A produces a maximum response and 50mg of drug B produces the same maximum response, which is more potent?
Quantal Dose Response
a population-based response; where the response is elicited with each dose of a drug as described in terms of the cumulative percentage of subjects exhibiting an ALL or NONE EFFECT and is plotted against the log dose of drug; X axis-frequency or % of individuals responding and Y axis: dose of drug
Both, but the values are not identical
Can POTENCY be determined using graded dose response or quantal dose response measurements?
Graded-Dose Response Values
Match these values with the appropriate dose response method: EC50 and KD (affinity for receptors)
Quantal-Dose Response Values
Match these values with the appropriate dose response method: ED50, TD50, LD50 (50% of the effect in population studied)
Therapeutic Window
the range of drug doses that elicits a therapeutic response, without unacceptable adverse effects (toxicity); dosages range from the minimum effective therapeutic concentration (dose) and the minimum toxic concentration (dose)–clinically relevant to the index of safety
Therapeutic Index
A ratio of TD50 (or LD50) to the ED50 (TD50/ED50)=_____; a large range indicates a safe drug and a small range indicates a relatively toxic drug
Certain Safety Factor (CSF)
calculated from quantal-dose response relationship for a therapeutic effect and toxic effect; defined as the ratio between the dose that is lethal in 1% (LD1) and the dose that produces therapeutic effect in 99% of subjects (ED99)

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