Exam 1 Flashcards
Pharmacology
-study of drug
-the actions and effects on living organisms
Psychopharmacology
specific class of drugs that effects thinking, mood, and behavior
Neuroharmacology
specific class of drugs that effect neurons and NS
Neuropsychopharmacology
how drugs interact with neurons and their effect with thinking, mood, and behavior
how to study neuropsychopharmacology
-study effects of the drug on the NS
-use drugs as a tool to study functions of the NS (EX: dopamine and reward system with cocaine)
drugs are ___ and have ___ effects
variable, multiple
what does pharmacological mean?
how drugs effect behavior when introduced to the NS
what does neurophysiological mean?
whats happening at synapse and activity of neurons
what does psychological mean?
the effects of conditioning
-EX: addiction
what are psychoactive drugs?
biologically active substance that chemically alters cell structure or function of neurons which in turn, effects mood, thinking, and behavior
-alters transmission b/w neurons
-excite or inhibit normal function
what is behavior?
any activity/change that can objectively measured
the pyramid of behavior? (big -> small)
groups if individuals
individual
system
organ
tissue
cell
molecules
ion
what type of cells regulate behavior?
specialized cells
what are the three specialized cells?
sensory, neural, effector
what do sensory cells do?
transduce environmental signal into biochemical signal
what do neural cells do?
-info processing
-transmit, integrate, store
what does transmit mean?
moving info from one place to another
what does integrate mean?
receiving many signals to produce one signal
what do neurons regulate?
behavior and homeostasis
route of the signal
sensory cell -> sensory neuron -> interneuron -> motor neuron -> effector
what is an effector?
contain sensory cells that excite or inhibit the motor neuron
-need to be in optimal range (no extremes)
what is drug action?
the way the drug interacts with cells and neurons
-open/close channels
-activate enzymes
what are drug effects and what are the different types of effects?
the result of drug action
-specific
-nonspecific
-therapeutic
-side
what produces specific drug effects?
drug-receptor interactions
what produces non-specific drug effects?
environment (weather, diet)
what is the difference between therapeutic and side effects?
therapeutic: desired effect
side: undesired effects
what are the four different ways to name a drug?
-chemical
-generic
-trade
-street (sland)
what is the chemical name of a drug?
describes molecular structure
-IUPAC ID
what is the generic name of a drug?
official name
-no paten on drug
what is the trade name of a drug?
brand name
-paten
-proprietary name
are the generic and trade name capitalized?
generic name: NO
trade name: YES
what is the street name of a drug?
rapidly changes with generations
what is the chemical, generic, trade, and street name of amphetamine?
chem: dl-2-amino-1phenylpropane
gen: dl-amphetamine
trade: Benzedrine
street: speed, bennies, whites
what is the chemical, generic, trade, and street name of valium?
chem: 7-chloro-1-methyl-5-phenyl-3H-1,4-benzodiazepin-2[1H[-one
gen: diazepam
trade: Valium
street: tranks, downer, blues, yellows
what is the chemical, generic, trade, and street name of Lunesta (sleep aid)?
chem: very very long
gen: eszopiclone
trade: Lunesta
street: zombie pills
how are drugs classified?
depending on goals
what are the 5 classifications of drugs?
-CNS stimulants
-CNS depressants
-Analgesics
-Hallucinogens
-Psychotherapeutics
what are examples of CNS stimulants?
cocaine, ampthetamine, caffeine
what are examples of CNS depressants?
barbiturates, alcohol
what are analegesics and some examples of them?
-they make you sleepy
-morphine, codeine, heroin
what are hallucinogens and some examples of them?
-they distort perception and mood
-LSD, mescaline, psilocybin
what are pyschotherapeutics and some examples of them?
-they help regulate mood (depression and anxiety)
-Prozac, Thorazine
what are the three types of drug equivalences?
-chemical equivalence
-biological equivalence
-clinical equivalence
what is chemical equivalence?
-same chemical compound
-same drug effects
-effects same systems
-different drug name
what is biological equivalence?
-different chemical compound
-same or similar drug effects
-effects same systems
what is biological equivalence?
-different chemical compound
-same or similar drug effects
-effects same systems
what is clinical equivalence?
-different chemical compound
-same drug effect
-effects different systems
what is the Controlled Substance Act (1970)?
created 5 schedules categorized by abuse potential (not addiction) and medicinal value
what is schedule 1?
-high abuse
-no medicinal value
-not prescribed and tightly regulated
what is schedule 2?
-high abuse
-accepted medicinal value
-can prescribe, but no refills
what is schedule 3?
-moderate abuse potential
-accepted medicinal value
-5 refills over 6 months
what is schedule 4?
-low abuse potential
-5 refills over 6 months
what is schedule 4?
-low abuse potential
-accepted medicinal value
-5 refills over 6 months
what is schedule 5?
-lowest abuse potential
-accepted medicinal value
-5 refills over 6 months
what is the controlled substance analogue enforcement act? (1986)
tweeking an illegal drug is restricted
-bath salts, synthetic pot
why is alcohol hard to classifiy?
effects depend on dose
what happens with a low dose of alcohol?
behavioral excitement
what happens with a high dose of alcohol?
behavioral inhibition
what schedule is ADHD and what drug is used to treat it?
-treat with Ritalin (methylphenidate) which is a stimulant
-schedule 2
drugs affect __(all / some)__ cells
all!!!!!
how were drugs initially discovered most of the time?
by luck or by accident
what was chlorpromazine initially used for and what is it used for now?
initially: sedative for surgery
now: treats schizophrenia
what was lithium initially used for and what is it used for now?
initially: psychological conditioning
now: treats mania & bipolar
what is an example of how plant extract is used for drugs?
poppy plant was used as morphine
what are me too drugs and designer drugs?
when chemists alter the structure of a popular patented drug by making small adjustment to sell for their own profit
how long does it take for a drug to get approved?
10 years
how much money does it take to develop a drug?
$2.8B
how long does a patent last and does the patent start before or after approval?
20 years
-starts before it is approved
what act set stringent regulations on drugs?
Food, Drugs, and Cosmetics Act
what is a patent?
absolute property rights
-defined by chemical name
what are some considerations to take in before making a drug?
-medical need
-commercial potential
-if it is easy to mass produce
what are Orphan Drugs?
drugs that affect less than 200,000 people
-rare diseases
what was the act and incentive for orphan drugs to be produced?
Orphan Drugs Act
-added 7 years of paten after FDA approval
-encourages production of drugs for rare diseases
what was the percentage increase of Epi-Pen by Mylan and the years of the increase?
increased 450% from 2009-2014
how much more was the drug by Epi-pen in those years?
$124 to now $609
what was the CEO salary increase for Epi-pen and who is the CEO?
CEO: Heather Bresch
$2.5M -> $18M
what was the percentage increase of Daraprim (AIDs treatment) and the years of the increase?
increased by 5000% from 2010-2015
how much more was the drug in those years for Daraprim?
$1 to now $750
who is the CEO who made Daraprim?
Martin Shkreli
why did the prices of the drugs increase by so much?
research and development prices weren’t increasing
-more money in the CEO’s pocket
what does the new law to combat price gauging for drugs do?
allows Medicare to negotiate prices
how long does animal testing take?
5 years
why do they do animal testing?
looking at…
-toxicity
-carcinogenicity (cancer risk)
-teratogenicity (malformation of embryo)
what does pharmacological testing do?
observes behavior on a single trait
what happens after animal testing?
human clinical trials after FDA approval
how long does the first phase of a human clinical trial take?
1.5 years
what size group does the first phase of a human clinical trial test?
small group of 20-100 HEALTHY people
what is the first phase of a human clinical trial looking at?
how the drugs affects the human body
-safety and dosage
what percentage of drugs pass the first phase of a human clinical trial?
70%
how long does the second phase of a human clinical trial take?
2 years
what size group does the second phase of a human clinical trial test?
test medium size group of 100-1,000 people of DIAGNOSED patients
what is the second phase of a human clinical trial looking at?
the efficacy and side effects
what percentage of drugs pass the second phase of a human clinical trial?
33%
what size group does the third phase of a human clinical trial test?
large group of 1,000-3,000 DIAGNOSED patients
what is the third phase of a human clinical trial looking at?
appropriate dosage and adverse rxns
what percentage of drugs pass the third phase of a human clinical trial?
25-30%
what does the fourth phase of human clinical trials test and what is the group size?
safety of drug post-marketing
-occurs AFTER FDA approves the drug
-real world setting
-ongoing and never stops
what is pharmacokinetics?
what body does to the drug
-administration, absorption, distribution, and fate
what is pharmacodynamics?
what the drug does to the body
-drug interaction with target tissues
what do drugs absorb into?
the circulatory system
how do drugs absorb into the circulatory system?
-systematic administration (blood)
-crosses through membranes
what are the two types of administration routes?
enteral (thru GI tract)
parenteral (all other routes)
what is the most common route of administration?
oral (enteral)
oral (enteral) route
-per Os (PO)
-absorbs across GI membrane
what are the negatives of oral (enteral)?
-highly variable depending on previous meal
-first pass metabolism (can reduce effect)
-must have cooperation of patient
-can recall (throw up)
oral (parenteral) types
sublingual (under tongue)
transbuccal (chewing tobacco)
oral (parenteral) sublingual
absorb through mucous and salivary glands
-nitroglycerin, buprenophine
oral (parenteral) transbuccal
absorb through mouth lining
IV Injection
-directly into bloodstream
-rapid onset
-high peak
-short duration
IM Injection
-takes 10-30 min
-dissolved in aqueous and oil substances
-location is important
IM Injection dissolved in an aqueous solution
high peak
short duration
IM Injection dissolved in an oil solution
short peak
long duration
IM injection in deltoid
rapid distribution
IM injection in glute
slow distribution due to further away location to main vessels
-used for lg. volumes
SC Injection
-under skin
-insulin
-slow onset
-low peak
-long duration
negatives of SC injection
variable
limited volume
skin irritations
IP injection
-peritoneal cavity of abdomen
-similar to IM kinetics wise
-high peak
-short duration
-can deliver large amounts
-used in animal research
injection in CSF around spinal cord
epidural
intrathecal
epidural
injection outside dura mater
intrathecal
injection inside subarachnoid space
intracerebroventricular
injection in CSF
intracranial
injection into brain
what is curare drug an example of and what does it show?
injection into brain
-peripheral -> paralysis
-central -> convulsions
-shows that different areas have drastically different effects
inhalation
-gases, vapor, smoking, aerosols, huffing
-enter through capillaries in lungs
-large surface area
-rapid onset
-high peak
-short effects
does inhalation or IV injection have a more rapid onset?
IV injection
does IM injection or PO have a more rapid onset?
IM injection
Intranasal
-particles of drug snorted through nose
-absorption through mucous
-single membrane
-bypasses BBB and goes through CSF
-no 1st pass metabolism
-rapid onset (15-30 min)
-similar to IM and IP
does intranasal or inhalation have a more rapid onset?
Inhalation
Infusion Pump
-insulin
-patient-controlled analgesia
Pellets
-release drug overtime
-Nexplanon
Topical
-absorbed through skin/mucous
-transdermal patches
-suppositories
Transdermal Patches
-topical
-slow continuous release
Suppositories
-topical
-rectal or vaginal
-poor and unpredictable absorption
Ultra-Sound Mediated
-low and intense frequency
-increase size of skin pores
-insulin
Iontophoresis
-weak electrical current
-pushes/pulls molecules across skin
what factors help determine choice of drug route?
-patient characteristics
-concentration in blood
-amount delivered
-rapidity of onset
-duration and magnitude of effects
what does a rapid onset mean kinetics wise?
high magnitude, short duration
what does slow onset mean kinetics wise?
low magnitude, long duration
when is absorption complete?
when conc. at target site = conc. at administration site
what types of membranes controls absorption?
cell membranes, capillary walls, BBB, placental barrier
what other factors can control administration rate?
-route
-bioavailability
-individual differences
-solubility
lipid bilayer
-barrier
-semipermeable
fluid mosaic model
-phospholipids
-proteins
phospholipid bilayer
-phosphate heads = hydrophilic
-lipid tails = hydrophobic
passive diffusion
-non-gated
-intercellular spaces
-lipid soluble molecules (nonpolar)
-no energy
facilitated diffusion
-gated channel
-no energy
active transport
-energy
-metabolic pumps
-polar
what do capillaries do and what are they?
exchange materials b/w blood and cells
-one cell thick
-typically leaky
-contain pores (non-gated)
what are capillaries composed of?
intercellular cleft
fenestra
pinocytosis
what is the BBB?
-barrier b/w blood and brain
-contain capillaries and astrocytes
-selectively permeable (nonpolar)
-water soluble (polar)
-maintains stable CNS environment
-keeps CNS chemicals in
what is different about the capillaries in the BBB?
-less leaky
-no intercellular cleft or fenestra
-water-soluble molecules (polar) can’t pass through
when is the BBB fully developed?
at 2 years old
what weakens the BBB?
trauma
infection
age
the BBB __(is/is not)__ continuous
is not
what areas in the BBB interact with blood?
area postrema (brainstem)
median eminence (hypothalamus)
what is special about the area postrema?
contains a chemical trigger zone
-safety mechanism
-keeps a stable amount of blood
what type of neurons monitor the blood in the CTZ of area postreme?
dopaminergic neurons
what does the median eminence do?
release neurohormones into the blood
what does the placental membrane do?
exchange nutrients and wastes with mom
-less selective than BBB
what can cause danger to the placental membrane?
due to underdeveloped BBB in a fetus
-high risk of toxicity
-lack enzymes for metabolism
-teratogens
what are teratogens?
chemicals that can cause birth defects
-alc, nic, coke
-can lead to low O2 levels (hypoxia)
what is solubility?
the ability to dissolve in a medium
lipid soluble
easily crosses membrane
non-polar
water soluble
won’t cross membrane
polar
what does ionization do to solubility?
decreases lipid solubility
-dependent on pH of fluid and pKa of drug
ion trapping
-increases ionization
-traps drug in a compartment
-slows onset
-decreases peak
-prolongs effects
what is maintained when the drug gets redistributed after being ‘trapped’?
ratio is maintained
what type of molecule is best at absorption?
-small
-lipid soluble
-low ion trapping
-pKa matches fluid pH
what is depot binding?
similar to ion trapping except NO ionization
-drug disperses in 1-2min
-drug isn’t metabolized
how does depot binding work?
-silent receptors
-nonselective binding
negatives of depot binding
-decreases bioavailability
-slows onset
-lower magnitude
-longer effects
what are silent receptors?
holds drug but produces no effect
what is nonselective binding?
prevents drug from reaching target
-competition for sites
-drug interaction increases bioavailability
-occurs when bound to organs, muscles, fat, and plasma proteins (albumin)
when does redistribution occur?
when the drug is released from depot binding, protein binding, and ion trapping
-ratio is maintained
-slow and prolonged drug effects
what is drug clearance?
eliminating drug from system through the liver
-immediate and long term
what three things are involved in drug clearance?
-biotransformation by changing structure of drug
-elimination by kidneys through urine
-when it falls less than effective dose
what is half life?
measure of how long a drug stays in your system
-two types (1st order, 0 order)
what is 1st order half life?
-majority
-constant FRACTION eliminated
-small % of clearance sites occupied
what is 0 order half life?
-constant AMOUNT eliminated regardless of concentration
-all clearance sites occupied
-EX: alcohol (1/2 oz eliminated / hour regardless how much initially was drank)
what is plasma half life?
the time it takes for blood levels to drop by half
-distribution and elimination half life
what is the half life of dexedrine and cocaine?
dexedrine: 10 hrs
cocaine: 1 hr
what happens if you wait too long b/w doses?
can’t feel it, decrease in concentration
what happens if you don’t wait long enough b/w doses?
increase of toxic effects
how many administrations are needed for plasma half life?
5
what is biotransformation?
-metabolism by enzymes
-inactive or active
-initially in the liver
-elimination as unchanged or a metabolite
-two phases (1 & 2)
what is a metabolite?
drug is altered
phase 1 of biotransformation
non-synthetic modification
-reduction rxn (hydrolysis, pick up e-)
-oxidation rxn (lose e-, most common)
phase 2 of biotransformation
synthetic modification
-something is added on
-inactive metabolites
-conjugation (enzyme action; glucuronide)
-highly ionized (ion trapping and elimination)
Of the money spent to address illegal drug use, what percentage does the United States spend on prevention?
for every $100 spent, only $3 is spent on prevention
what is the most addictive drug in the world?
nicotine
Dr. Benjamin Rush was the first to speak out on the dangers of which commonly used drug?
alcohol
What was the average amount of pure liquor consumed by Americans in 1830 and how does it compare with the amount consumed today?
1830’s: 5 gallons per year
-which is 3x more than what we consume today
What two developments greatly increased the incidence of medical opiate addiction in the 19th century?
-isolation of morphine
-popularization of hypodermic medication
What was the primary medical use of opium and its extracts?
-daily struggles to make them feel better
-recreational use
What occurred in 1914 that was a key factor in the creation of a black market for drugs in the United States?
Harrison Narcotics Act of 1914
-put tight control on drugs
What event in 1917 set the stage for the passage of prohibition of alcohol in the United States?
alcohol was illegal for recreational use
-US was fighting Germany in WW1
Harry Anslinger of the Food and Drug Administration was a key player in outlawing the use of this commonly used substance?
marijuana
What federal legislation passed in 1951 was the first to set mandatory prison sentences for marijuana and narcotics?
Bog’s Act
Which late 20th century U.S. president declared the “war on drugs”?
Ronald Regan
What development in the mid-1980s dramatically increased the use of cocaine in minority and low-income populations.
development of crack
-was very affordable
What percentage of today’s prison population is incarcerated for drug and alcohol- related crimes?
50-60%
How many deaths occur as a result of all illicit drug use compared to smoking cigarettes?
illicit drugs: 4,600 have died
smoking: 400,000 die per year
what is the #1 factor in freshman college failure, date rape, and domestic violence?
alcohol abuse
