QUIZLET Unit 1 - Intro to Pharmacology (pom75) Flashcards
pom75
body of knowledge concerned with the action of chemicals on biologic systems, especially by binding to regulatory molecules (receptors) and activating or inhibiting normal body processes.
Pharmacology
Body of knowledge where pharmacology originated
Botany
True or False
Drugs can either activate or inhibit a body process.
True
True or False
With the advancement of technology, drug production has greatly evolved from natural (plant-based) to a lot of synthetic products.
True
Improperly used drugs result to what type of effect?
Toxic effects
Emphasizes the therapeutic or “good effects” of drugs
Pharmacology
Effect of the drug to the body
Pharmacodynamics
Focuses on the adverse effects of drugs
Toxicology
Area of pharmacology concerned with the use of chemicals in the prevention (vitamins or vaccines), diagnosis (some drugs can differentiate disease entities, such as naproxen test), and treatment of disease, especially in humans.
Medical Pharmacology
Effect of body on the drugs
How the body manages the drug, if it will be excreted or absorbed
Pharmacokinetics
True or False?
The drug could reach its target receptors, whether that is its intended receptor (therapeutic effects) or the unintended.
True
Specific molecule in the biologic system that plays a regulatory role
Receptor
Area of knowledge that focuses on what happens when the drug is excreted from our body or is thrown into the environment.
Environmental Pharmacology
Finds the exact mechanism of action of drugs and identifies certain receptors
Pharmacogenomics
Area of pharmacology concerned with the undesirable effects of chemicals on biologic systems
Toxicology
Any substance that brings about a change in biologic
function through chemical actions.
Drug
Why individuals react differently with the same drug
Pharmacogenetics
Molecular weight (MW) of most drugs
Between 100-1000
Chemical substances that are completely foreign, meaning there is no similar composition of this specific chemical composition within our body
Not synthesized by the body
Xenobiotics
Drugs with 100 MW
For selective binding
Reason: It has a smaller receptor; hence, larger particles will not readily attach to it.
T/F
Drugs are given at a site proximal from the intended site of action, but it eventually reaches their intended site of action.
False
distant from the intended site of action dapat
Drugs with 1,000 MW
For traversing to different barriers of the bofy
Drugs with >1,000 MW are given where?
Directly at the site of action
Affects the movement of drugs from one compartment to another.
Drug size and molecular weight
Drugs with >1,000 MW
Cannot move within the body
Precursor to pharmacology
Materia medica
True or False
Most drugs are ACHIRAL
false
All drugs are chiral and exist in enantiomeric paors
Science of drug preparation and medical use of drug
Materia medica
Determines the duration of action
Drug Receptor Bonds
Chemical forces or bonds through which the drug
interacts with the receptors
Drug Receptor Bonds
True or False
Weaker bonds are more selective bonds
True
Are electrostatic bonds weaker than covalent bonds?
Yes
Strongest and irreversible type of drug receptor bonds
Covalent
Most common drug receptor bond that is also based on difference of charges
Electrostatic bonds
Weakest among the drug receptor bonds
Hydrophobic bonds
Pharmacokinetic principles
ADME (Absorption, Distribution, Metabolism, Elimination)
Prodrug
Binds to and activates the receptor
agonist
Activates receptor-effector system to the maximum extent (Ra-D pool){activated form}
Full Agonist
Pharmacodynamic principles
Agonists, Antagonists Constitutive Activity, Allosteric modulators
Binds to the same receptors and activate them in the same way but do not evoke the maximum response
Partial agonist
True or False
When an agonist is present, it can activate the receptor-effector system
True
Effect of inverse agonist on the constitutive activity
Increase, Decrease, Maintain
Decrease
Binds to a receptor, compete with and prevent binding by other molecule
Antagonist
Drug has a stronger affinity for the Ri pool (nonfunctional form)
Inverse agonist
An agonist that results in effects that are opposite of the
effects produced by conventional agonists
Inverse Agonist
Effect of antagonist on the constitutive activity
Increase, Decrease, Maintain
Maintain
Does constitutive activity occur in the presence or absence of the agonist
ABSENCE
Some of the receptor pool must exist in Ra (active) form even without a ligand or drug attaching to it
Constitutive activity
Binds to a site on the receptor molecule separate from the agonist binding site
Allosteric modulators
Are allosteric modulators competitive or non-competitive?
Non-competitive
Movement of molecules through the watery extracellular and intracellular space
Aqueous Diffusion
An allosteric modulator that increases the response to agonis
Allosteric activator
An inactive precursor that must be administered and converted to the active drug by biologic process inside the body
Prodrug
An allosteric modulator that decreases the response to agonist
Allosteric inhibitor
Is there an increase or decrease in response when an ANTAGONIST is bound to the receptor?
NEITHER.
There will be NO change in response. Constitutive activity is maintained.
Allosteric modulators bind to a different binding site? True or false
True
True or False
Not all drugs have allosteric modulators
True
Movement of drug molecules into and within the biologic environment
Permeation
Most important limiting factor for drug permeation
Lipid Diffusion
Movement of molecules through membranes and other lipid structures
Lipid Diffusion
governed by Fick’s law
Aqueous diffusion, Lipid diffusion
Drugs transported across barriers by mechanisms that carry similar endogenous substances (amino acid, peptides, glucose)
Transport by Special Carriers
These are receptors with no discovered ligands:
orphan receptors
True or False
Partial agonists have low intrinsic efficacy
True
Mechanism by which Vitamin B12 and Iron with transferrin are absorbed in cells
Endocytosis
Allosteric inhibition can be overcome by increasing the dose of agonist.
False
T/F
Action of antagonists/inhibitors can be overcome by increasing the dosage of the agonist
True
Mechanism by which neurotransmitters are released
Exocytosis
Law that predicts the movement of molecules across a barrier
Fick’s Law of Diffusion
True or False
Drug absorption is faster in organs with larger surface areas (eg, small intestine) than from organs with smaller absorbing areas (eg, stomach)
True
True or False
Drug absorption is faster from organs with thin membrane barriers (eg, lungs) than those with thick barriers (eg, skin)
True
Aqueous solubility of a drug is a function of the __________ (degree of ionization, polarity) of the molecule
electrostatic charge
The concentration difference is ______ proportional to the rate of permeation of the drug.
Directly or Inversely
Directly
(the higher the concentration difference in the different compartments, the faster is the rate of permeation)
This is a fixed value, a measure of the mobility of the drug in the medium of the diffusion path. It is an intrinsic factor property of the drug
Permeability coefficient
Thickness is _____ proportional to permeation
Inversely
(the thicker the membrane, the slower the permeation)
true or false
pH of the medium determines the fraction of molecules charged (ionized) versus uncharged
(nonionized)
true
T/F
The more polar, the harder to traverse through the lipid membrane.
True
Water molecules are attracted to charged drug molecules which forms?
An aqueous shell around them
Many drugs are weak acids and bases?
T/F
true
Neutral, more lipid-soluble form of WA and WB
Protonated weak acid
Unprotonated weak base
Neutral molecule that can form a cation (+ charged) by combining with a proton (hydrogen ion)
Weak base
Neutral molecule that can reversibly dissociate into an anion (- charged) and a proton (hydrogen ion)
Weak acid
Which is more polar? WA or WB
WB (therefore it is more ionized)
Nitrogen atom of a neutral amine has how many atoms and pair/s of unshared electrons?
3 atoms and 1 pair of unshared electrons
Amount absorbed into the systemic circulation of the amount of drug administered
Bioavailability
First pass effect is avoided in what routes of administration?
IV
IM
Sub Q (Subcutaneous)
Route of administration where there is partial avoidance of the first pass effect
Rectal (Suppository)
Route of administration where delivery is closest to the target tissue and results to rapid absorption
Inhalation
Application to the skin or mucous membrane of the eye, nose, throat, airway, or vagina for local effect
Topical
Application to the skin for systemic effect
Ex. Nicotine patch
transdermal
Route of administration where Rate of absorption occurs very slowly
transdermal
T/F
High blood flow = maximized absorption
True
Weak basic drugs are excreted faster in alkaline urine.
False
Weak basic drugs are excreted faster in acidic urine
Induced dipole interactions between the drug and its receptor:
Electrostatic
Covalent
Hydrophobic
None of the choices
Electrostatic
Plays a major role in deciding whether that drug is appropriate therapy for a particular symptom or disease
PK or PD?
Pharmacodynamics
Important in the choice of administration of a particular drug for a particular patient
PK or PD
Pharmacokinetics
Drug receptor interactions exhibited by lipid-soluble drugs
Covalent
Electrostatic
Hydrophobic
Hydrophobic
T/F
Quaternary amines are permanently charged thus are always water soluble
True
T/F
Quaternary amines are permanently charged thus are always lipid soluble
false
Concerned with the mechanism of action
PK or PD
Pharmacodynamics
Determines the group in which the drug is classified
PK or PD
Pharmacodynamics
Drug molecules that are bound to plasma proteins can permeate aqueous pores.
True or false
False
Transport of drugs that use special carriers can be saturated and inhibited.
T/F
True
Makes possible the calculation of loading and
maintenance doses being given to patients
pharmacokinetics
basic principles of pharmacokinetics
absorption, distribution, metabolism, excretion (ADME)
what will dictate the pharmacological effect?
drug concentration at site of action
movement of the drug from the site of administration to the bloodstream (being the plasma)
Absorption
Distribution
Metabolism
Excretion
absorption
drug metabolism and elimination can be collectively known as
drug clearance
Drug absorption is dependent on
route of administration
patient factors
drug properties
formulations
Peak Plasma Concentration (Cmax) is reached when?
drug absorption rate = drug clearance rate
- drug absorption rate 2. peak time
directly proportional
inversely proportional
no relationship
directly proportional
Bioavailability is computed by
Area Under (“plasma concentration vs time”) Curve or AUC
Unique for a particular drug in a particular patient
effective drug concentration
Space in the body that will contain a particular amount of drug
volume of distribution (Vd)
Ability of the body to eliminate the drug
clearance (CL)
Measure of apparent space in the body available to contain the drug
volume of distribution (Vd)
Amount of drug in the body to the plasma/serum concentration
volume of distribution (Vd)
when a lot of the drug is bounded to the peripheral tissues, there will be ____ amount of drug in the plasma
lesser
when there is high drug concentration found in the extravascular compartments of the body, the drug has a greater volume of _____
distribution
When drugs are binded to the plasma proteins, diffusion is much more limited
true
false
true
Clearance (CL) is dependent on
drug
organs of elimination of the patient
blood flow
rate of elimination compared to plasma concentration
clearance
- rate of drug elimination
- drug concentration
directly proportional
inversely proportional
no relationship
directly proportional
Drugs in the zero order kinetics
PAA
Phenytoin
Alcohol
Aspirin
Elimination rate is constant
First-order elimination
Zero-order elimination
Zero-order elimination
time required for the amount of drug to fall by 50%
half-life
state wherein rate of drug administration is equal to the rate of drug elimination
steady state
