Chapter 1 Flashcards by Giana Honorio

psychopharmacology

study of actions of substances and their effects on mood, cognition, and behavior

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neuropharmacology

study of substance-induced brain changes at the physiological, receptor, biochemical, and molecular levels

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pharmacokinetics

how our bodies affect the actions of a substance (ADME)

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ADME

absorption, distribution, metabolism, elimination

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pharmacodynamics

how a substance affects our bodies and brains

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How do substances cause molecular changes in a cell?

substances are ligands that selectively act on receptors or target sites

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therapeutic effect

when substance-receptor interaction produces desired physiological/behavioral changes

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side effects

other effects that accompany the desired/main effect

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physiological factors affecting substance action

dose and chemical structure of substance

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bioavailability

amount of the substance in the blood that is free to bind at a target site

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inactivation

body changes substance to make it easier to get rid of through excretion

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types of administration

oral
intravenous
instramuscular
intraperitoneal
inhalation
subcutaneous
topical
transdermal
epidural

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effect of drug administration type

drug concentration varies based on administration type

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factors affecting absorption

membrane structure
lipid soluble substances
ionized substances
pH
pKa
higher absorption of organs (small intestines)
size of individual
sex

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pKa

pH of aqueous solution at which 50% of the substance would be ionized

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selective barriers to substances

fenestrae (pores; allow substance to move from blood plasma to ECF fairly freely)

blood brain barrier (prevents certain compounds from entering the brain)

placenta (separates blood of mother from fetus)

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acute toxicity

high substance level in mother is amplified in fetus

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teratogens

induce developmental abnormalities

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substance depots

substances can bind at inactive sites where no physiological effect is initiated

can have major impact on substance magnitude and duration

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first-order kinetics

metabolism/biotransformation that occurs at an exponential rate

50% of substance removes at each time interval

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zero-order kinetics

metabolism/biotransformation that occurs at a constant rate

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half-life

t (1/2) ; time required to remove 50% of substance in blood

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type I biotransformation

nonsynthetic

oxidation (loss of H or gain of O)

reduction (gain of H or loss of O)

hydrolysis (split H2O into H+ and OH-)

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type II biotransformation

synthetic reactions

combine substance with some other molecule to inactivate or ionize it

enzyme induction

increase in liver enzymes can lead to tolerance because metabolism is sped up

enzyme inhibition

inhibit enzyme activity and reduce metabolism of other substances can cause more intense or prolonged effect

substance competition

two substances compete for the same enzyme an elevated concentration of either drug reduces the metabolic rate of the second, causing potentially toxic levels

genetic polymorphism

genetic variation produces a variety of active forms proteins can explain why some individuals need higher or lower doses than others to achieve the same effect

how are drugs excreted?

mostly through the kidneys also sweat, saliva, feces, breast milk, breath

conditions needed for drugs to be excreted

water soluble and ionized

how does pH affect excretion

drugs w/ opposite pH of tubular urine are more ionized and less easily reabsorbed, so they are excreted more easily

conformational change

change in receptors due to ligands temporarily binding to them initiates a cascade of biochemical events

up regulation of receptors

number of receptors increasing due to absence of substance

down regulation of receptors

number of receptors decrease due to abundance of substance

why is it important to design substances that bind to one subtype of receptors?

fewer side effects

what causes a drug action/effect?

agonist-receptor interaction

agonist

ligand that activates the receptor has affinity and efficacy

affinity

ability to bind or fit into receptor high affinity = best fit = strong drug effect

antagonist

ligands that bind to receptors but do not cause effect can have high affinity but still no efficacy

competitive antagonist

ligand and antagonist compete for one receptor

noncompetitive antagonist

ligand and antagonist bind to different receptors but activation is still stopped minimal effects upstream or downstream of receptor sites

types of receptor competition

physiological antagonism (two drugs cancel out each other’s effects) additive effects (outcome is sum of two reactions) potentiation (both drugs together has greater results than the singular effect of either)

orthosteric site

where ligands bind to activate receptor

what effect? no ligand in orthosteric site no ligand in allosteric site

no signal / closed

what effect? no ligand in orthosteric site ligand in allosteric site

no signal / closed

what effect? ligand in orthosteric site positive allosteric modulator in allosteric site

increased signaling / enhanced opening

what effect? ligand in orthosteric site negative allosteric modulator in allosteric site

decreased signaling / smaller opening

what effect? ligand in orthosteric site neutral allosteric modulator in allosteric site

unaltered signaling

dose response curves

used to compare amount of biological response for a given dosage the closer the curves are on the x-axis, the less safe it is for that effect

ED(50)

dose that produces half the maximal effect (ED(100)) ED(100) can be toxic so middle effect is desired

potency

absolute amount needed to produce the effect

TD(50)

dose at which 50% of people suffer a toxic/undesirable effect

formula for TI

therapeutic index = TD(50) / ED(50)

tolerance

needing higher dose of substance after repeated use can be due to physiological mechanisms generally reversible depending on dose and frequency of use rates differ depending on substance

cross tolerance

tolerance to one substance builds tolerance for another

acute tolerance

rapid, after one use

metabolic tolerance

aka substance disposition tolerance repeated use decreases amount of substance that reaches the target tissue

pharmacodynamic tolerance

aka cellular tolerance change in neuronal function or receptor regulation

behavioral tolerance

tolerance showed in environment/behavior but not in a neuronal or cellular level