Pharmaco Flashcards
What is the study of drugs?
pharmacology
What is the branch of pharmacology concerned with therapeutic agents used in the prevention, diagnosis, and treatment of disease in humans?
clinical pharmacology
True or false: drugs do NOT confer any new functions on a tissue or organ, they only modify existing functions.
true
What name describes the chemical structure of the drug?
chemical name
What name is the nonproprietary name of the drug that is general preferred but not always used?
generic name
What name is the trade name for a drug that is picked by the drug’s manufacturer and can only be used by the company that owns the name?
brand name
This refers to what the drug does to the body, including mechanism(s) of action and its effects
pharmacodynamics
This refers to what the body does to the drug and “ADME”
pharmacokinetics
This is a target that binds a drug or endogenous ligand and mediated the pharmacologic action
drug receptor
This refers to when the drug and the receptor are bound together and leads to the biological response
drug-receptor complex
True or false: the magnitude of the response to a drug is NOT proportional to the number of drug-receptor complexes
false
This refers to when all drug receptors are bound so no other complexes form
saturation
True or false: most drugs are lipid soluble
true
What type of molecule binds to the receptor and stimulates the biological response?
This usually mimics the response of the endogenous ligand.
agonist
This type of molecule blocks or reverses the effect of agonists and can also block the effects of endogenously produced compounds. It does not stimulate its own response.
antagonist
What type of molecule produces a biological response but it is not 100% effective even at high doses?
partial agonists
These are all reasons why ____ agonists are not as effective:
occupies all receptors but doesn’t active ligand binding site
opens ion channels differently or incompletely
can act as antagonist if given with full antagonist
partial agonists
What type of molecule competes for the same site on the receptor that the agonist wants?
competitive antagonist
What type of molecule opposes the action of the agonist without competing for the binding site and cannot be overcome by increase the concentration of the agonist?
noncompetitive antagonist
What type of molecule has the opposite effects of agonists by making receptors tilt toward the inactive state or decreasing the amount of time receptor ion channels are open?
inverse agonist
This is the maximal response a drug can pose
efficacy
This is a measure of the dose required to produce a response
potency
This is a measure of drug safety; lethal dose (LD)/ effective dose (ED)
therapeutic index
True or false: a therapeutic index that is larger/ wide is safer
true, more room for error
What value is referred to as a narrow therapeutic window?
2 or less
This refers to when two drugs with the opposite effects are given together
functional antagonism
This refers to when an antagonist is administered with an agonist
competitive antagonism
This refers to diminished response to the same drug over time and may be due to receptor desensitization or receptor down-regulation
tolerance
When the body quickly develops response to a drug and requires a higher dose for the same effect
tachyphylaxis
These are three reasons for _______ drug activity (increased or decreased?)
1. hyperactivity
2. potentiation
3. synergism
increased
This is an enhanced response to a drug
hyperactivity
This is the enhancement of one drug by another which has no effect on its own
potentiation
This is the production of a greater response by two drugs when given together, than each individually
synergism
What does LADME stand for?
Liberation
Absorption
Distribution
Metabolism
Excretion
What does liberation refer to?
how the drug was administered
This is the movement of the drug from the site where it was administered into the body
absorption
This refers to the amount of drug that is absorbed after oral administration compared with the amount of drug that is absorbed after intravenous (IV)
oral/ injection x 100
Bioavailability
Is absorption faster or slower if the drug is dissolved in aqueous solutions vs. oily solutions?
faster
Do smaller molecules absorb faster or slower than large ones?
faster
Can only the ionized or nonionized form of a drug cross membranes?
nonionized
Are acidic drugs nonionized in acidic or basic medium?
acidic
Are basic drugs nonionized in acidic or basic medium?
basic
Are more or less concentrated solutions absorbed faster?
higher concentrated
Is absorption faster or slower with increased surface area?
faster
Is absorption faster or slower in areas with more blood flow?
faster
This refers to the fact that drugs administered orally often are metabolized by the liver before reaching systemic circulation.
First Pass Effect/ Bioavailability
These are inactive drugs metabolized by the liver to the active form.
Prodrugs
This refers to the process in which an absorbed drug moves from the site of absorption to other areas of the body
distribution
What type of macromolecule do many drugs bind to when in the bloodstream?
plasma proteins, especially albumin
This is the process of converting a drug into another chemical called a metabolite
biotransformation/ metabolism
What is the major metabolizing organ?
the liver
Does biotransformation aim to make molecules more water-soluble or lipid-soluble for excretion?
more water- soluble/ hydrophilic
This phase of metabolism involves the cytochrome P-450 enzymes which introduces a polar functional group to increase renal elimination
Phase 1
What is the most important cytochrome P-450 enzyme involved in phase 1 of metabolism in the liver and metabolizes around 50% of drugs?
CYP3A4
In this phase of metabolism, acids are combined with the drug to increase polarity and therefore increase renal excretion
phase 2
Three processes of renal elimination of drugs include:
glomerular filtration
proximal tubular secretion
distal tubular reabsorption
What is the apparent volume in which a drug is dissolved? This assumes that a drug is evenly distributed and has not undergone metabolism or excretion.
Volume of distribution (Vd)
dose (mg)/ plasma concentration (mg/ mL)
volume of distribution (Vd)
This is the rate at which a drug is cleared from a volume of blood in a given time
Clearance (CL)
rate of drug elimination (mg/min)/ plasma concentration (mg/mL)
clearance (mL/ min)
Sum of the clearances from the various organs involved in drug metabolism and elimination
total body clearance
The % of drug that is lost or cleared from the blood per unit time
elimination rate
What is the fraction of a substance that is removed per unit time measured at any particular instant
elimination rate constant (ke)
This is the time it takes for the blood level drug to fall exactly half
half-life (t1/2)
When the drug accumulates until the amount administrated per unit time is equal to the amount eliminated per unit time (amount absorbed= amount cleared)
steady-state concentration (Css)
How many half-lives are needed to reach a steady-state?
5
5 x t1/2 = ?
Css- steady-state concentration
This is a single large dose of a drug that is used to raise the plasma concentration to a therapeutic level more quickly than would occur through repeated smaller doses
loading dose (LD)
constant amount of drug that is lost per unit time is under _______ order kinetics
zero
This refers to the fraction of drug removed during one pass through the liver
hepatic extraction rate
What is the study of genetic factors that affect drug responses?
pharmacogenomics
Refers to one of the alternate forms of a gene
allele
What is a series of alleles found in a linked locus on a chromosome?
haplotype
What is an inherited variation in the DNA sequence?
polymorphism
What refers to a variation in a single base pair within the DNA?
single nucleotide polymorphism (SNP)
Polymorphisms involved with larger stretches of DNA
structural variations (SV)
This alerts the immune system to target a pathogen for destruction and can possess SVs with high clinical significance
human leukocyte antigen (HLAs)
What is the most common phase 1 P450 enzyme in drug metabolism
CYP2D6
This phase 1 P450 enzyme has a preference for acidic drugs and polymorphism is more prevalent in Asian populations
CYP2C19
This phase 1 P450 enzyme has disproportional polymorphisms in the east asian and oceania populations
CYP2B6
Phase 2 enzymes are important in _______ and immunological treatments
cancer
UGT1A1 and TMPT are phase _____ enzymes
2
This enzyme is the rate limiting step in the pentos phosphate pathway, is a significant source of NADPH in the body, and deficiency is defined as less than 60% enzymes activity and is more prevalent in the African and Mediterranean populations and may lead to hemolysis.
G6PD
This is a genetic component that determines if sustained virologic response of anti-viral medication is likely and is more present in European populations
IFNL3
This refers to combination effects of multiple gene mutations on drug response
polygenic effects
HIV pts with the HLA-B*5701 gene variant have hypersensitivity to what drug?
abacavir (ziagen)
Pts of Asian descent with epilepsy, neurogia, or bipolar disorder with the HLA-B*1502 gene variant may develop Stevens-Johnson syndrome or toxic epidermal necrosis in response to what drug?
Carbamazepine (tegretol)
Pts with HIV must test CCR5 positive to use this drug
Maraviroc (selzentry)
Pts of Chinese, Thai, or Korean descent with renal impairment should not test positive for HLA-B*5801 to use this medication for gout
allopurinol
The CYP2C19 genotype should be tested for pts before taking what medication
Clopidogrel (plavix)
The CYP2D6 genotype should be tested before giving what medication
codeine
the CYP2C9 and VKORC1 genotype should be tested before giving what medication
warfarin (coumadin)
This phase of drug evaluation includes when experiments are done to define a drug’s mechanism of action, pharmacologic activity, and selectivity
pre-clinical phase: screening
In this phase of drug evaluation, clinical testing is carried out in human volunteers in three formal phases
clinical phase: clinical trials
This clinical phase is the first stage of testing in human subjects w/o target disease, it evaluates safety, determines dosage range, and identifies adverse reactions
Clinical phase 1
In this clinical phase, the new drug is studied in patients with the target disease and it determines the medication’s efficacy and the dose to be used in further trials
Clinical phase 2
In this clinical phase, the drug is tested in the formulation intended for the market in a much larger group of individuals with the target condition; this phase usually lasts 2-10 years
clinical phase 3
This clinical phase starts when the drug has been approved for the market and is being given to large numbers of pts.
clinical phase 4
