midterm #1 Flashcards

1
Q

median effective dose ED50

A

dose that’s effective in 50% of individuals tested

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2
Q

median lethal dose LD50

A

dose that’s lethal in 50% of individuals tested

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3
Q

ionized molecules (3 + what percentage depends on (3))

A
  • when drug dissolved in a liquid, some of its molecules become ionized
  • ions not lipid-soluble, cannot cross membranes
  • percentage of ionized molecules depends on: drug acid/base, liquid acid/base, drug pKa (pH at which half its molecules are ionized)
  • faster absorption with lower percentage of ionized molecules!
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4
Q

first-pass metabolism

A

metabolism of drugs in the liver before the drug is distributed throughout the body

  • ingested drugs reach liver before arriving at the heart
  • only applies to drugs absorbed by the intestines
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5
Q

rates of elimination

A

first-order elimination:

  • half-life, asymptotic elimination rate
  • low toxicity

zero-order elimination:

  • constant elimination rate
  • as soon as toxicity is hit (e.g. alcohol, overdose response)
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6
Q

kidneys

A
  • maintain balance of water and salt
  • excrete unwanted molecules (e.g. liver metabolites)
  • filter out everything, then allow re-absorption of all that’s required
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7
Q

oral administration

A

stomach: impermeable, no distribution

intestines: permeable, distribution
- much easier absorption for lipid-soluble drugs

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8
Q

combination of absorption and elimination

A

rate of elimination (half-life) for any drug stayconstant, but absorption differs depending on administration route

-> resultant curve depends on administration

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9
Q

upregulation vs downregulation

A

upregulation:

  • increase in receptors/sensitivity/transmitter production
  • response to drugs blocking receptors

downregulation:

  • decrease in receptors/sensitivity/transmitter production
  • response to drugs activating receptors
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10
Q

blood-brain barrier: active vs passive diffusion

A

active:

  • transport, also against concentration gradients
  • requires energy

passive:

  • diffusion through channel protein
  • attaching to carrier protein
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11
Q

urinalysis and blood sampling

+ problems (3)

A

urinalysis: looks for metabolites
blood sampling: looks for drug itself

problems:

  • elimination time > detection time (cannot say when drug’s been taken)
  • length of drug use (metabolic deposits)
  • individual differences
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12
Q

tempering with drug tests

A

substitution: put in someone else’s urine
adulteration: change molecules, e.g. attach to fat
dilution: decrease concentration

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13
Q

potency
efficacy
effectiveness

A

potency: amount required to produce a given effect
efficacy: maximum response achievable for a given dose
effectiveness: ability to produce the therapeutic effect, taking into account secondary and side effects

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14
Q

therapeutic index

A

LD50/ED50 -> safety ratio, how safe a drug is

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15
Q

protective index

A

TD50/ED50 -> safety ratio
TD50: dose at which 50% of people have complaints
- reserved for humans

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16
Q

certain safety factor

A

LD1/ED99 -> where 99% have effect and 1% dies

- pertains to instant and not long-term use

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17
Q

pharmacological antagonism (2)

A

reduced effect due to presence of another drug

(1) competitive:
- at site of action
- need more drug to achieve max result (curve shifted to right)

(2) non-competitive:
- drug B binds to receptor or allosteric site, reduces receptor activity
- reduces max achievable result (decreased efficacy)

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18
Q

physiological antagonism

A

when substances produce different effects counteracting each other, via different binding sites and mechanisms

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19
Q

additive effects (2)

A

combined drug effects

(1) synergistic: combined effects are greater than their sum
(2) potentiation: ineffective drug becomes (more) effective in presence of another drug

20
Q

pharmacodynamic tolerance (2)

A

tolerance in CNS (number of receptors/neurotransmitters)

(1) protracted:
- after several exposures
- need more drug for same psychological effect (graded)

(2) acute / tachyphylaxis:
- after only one exposure
- psychological effects during intake, not elimination
- reduced subjective effect (threshold)

21
Q

pharmacokinetic tolerance

A

changes in metabolism resulting from constant concentrations in body

increases in rates of:

  • enzymes (enzyme induction)
  • elimination from body
22
Q

cross-tolerance + factors (2)

A

tolerance that extends to another drug

factors:

  • enzymes
  • CNS: site of action (downregulation), similar reward-feedback mechanism (upper limit for DA release)
23
Q

behavioural tolerance + factors (2)

A

adjustment and compensation as a result of experience

factors:

  • self-awareness
  • determination
24
Q

homeostasis

allostasis

A

homeostasis: internal equilibrium condition

allostasis: physiological changes to obtain homeostasis to adapt to severe environmental demands
- more permanent state with chronic illness or stress

25
cellular adaptation theory
cells adapt by changing the number of their receptors, not their sensitivity upregulation to avoid toxicity downregulation to increase sensitivity
26
opponent process theory: B-processes (3) problems (2)
B-processes: - pharmacodynamic tolerance - pharmacokinetic tolerance - environmental tolerance problems: - doesn't account for drug effects: zero-order elimination, tachyphylaxis, drugs not producing withdrawal - compensatory response is not a response but a state (allostasis, has separate mechanisms)
27
opioids (4) | dopamine (4)
opioids: - inherent - liking - subjective feeling of pleasure - cannot be conditioned dopamine: - learned - wanting - objective homeostatic response - can be conditioned
28
dependence | addiction
dependence: reliance - physiological requirement for homeostasis addiction: compulsion - psychological want/need (emotional impulse)
29
addictions: physical psychological
physical: continuation of use to avoid withdrawal - negative reinforcement psychological: - use motivated by craving - positive reinforcement
30
addictive personality? Keller's law impulsivity and addiction?
traits only appear to be assoicated with addiction bc publication bias for significant results not much evidence for impulsivity in addiction (also bc developmental pattern of impulsivity is not constant)
31
addiction: interaction models
1) disposition (nature) x environmental stress (nurture), vulnerability x stress 2) protective factors (friends, resilience, exercise) 3) time/events (developmental trajectory, window of vulnerability)
32
diathesis-stress model
model of risk for addiction - negative environmental factors - individual vulnerability - risk factors determine result - addictions are cause -> effect
33
differential susceptibility model
model of risk for addiction - positive and negative environmental factors - individual susceptibility, individual plasticity - result is plastic based on environment - buffers for addiction not to develop
34
drug effects
primary: drug - effect at targeted s.o.a. secondary: drug - effect at site other than targeted s.o.a. side: metabolite - effect at other than intended s.o.a. prodrug: metabolite - metabolite of prodrug acts at intended s.o.a.
35
additive/antagonistic for drugs/metabolites: enzyme inhibition enzyme induction
enzyme inhibition: drug B blocks, stops production of or decomposes enzymes for drug A - additive for drug - antagonistic for metabolites enzyme induction: drug B activates or facilitates production of enzymes for drug B - additive for metabolites - antagonistic for drug
36
role of dopamine
relating problem to solution motivation: dopamine depletion causes dishínhibition, facilitates action guidance: dopamine released for correct actions (conditioning, memory, repeating response) reinforcement: dopamine response to obtaining reward and to restoration fo homeostasis
37
hedonic homeostatic dysregulation
integrates physiology with psychological experience within-system adaptation: opponent process and incentive salience -> withdrawal makes pleasure of drug use more rewarding by comparison between-systems adaptation: allostasis -> chronic fluctuation enhances overall stress response, resulting in heightened preoccupation => at some point, drugs feel better because things generally feel worse
38
speed of absorption from parenteral administration
blood vessels > intraperitoneal > intramuscular > subcutaneous
39
pons: locus coeruleus and reticular formation
located in midbrain locus coeruleus: - reflexive processing of incoming sensory information reticular formation: - arousal, FFFS - selective attention - wakefulness (raphe nucleus: sleep, production of pertinent neurotransmitters)
40
reward circuitry: periaqueductal gray and ventral tegmental area
periaqueductal gray: - pain as a sensation - punishment (psychological) -> projects to PFC ventral tegmental area: - reward circuitry - pleasure
41
what she includes in midbrain (5)
``` pons - locus coeruleus - reticular formation periaqueductal gray VTA hippocampus amygdala ```
42
insula
consciousness, self-awareness, imagination
43
Addiction in DSM-IV and DSM-5
DSM-IV: - substance abuse (affects others) - substance dependence (affects yourself) DSM-5: - substance use disorder (affects anyone)
44
protein binding
when drug molecules bind to large proteins - permanent attachment, no crossing of membranes - temporary attachment, slow release of molecules into blood
45
differences drugs and natural reinforcers (2)
1) natural reinforcers have satiation mechanism that terminates their reinforcing effect (drugs don't) 2) drug reinforcement is much faster and more intense than natural reinforcers
46
what she includes in forebrain (4)
cerebral cortex insula thalamus hypothalamus
47
medulla oblongata
autonomic: - breathing, heart rate etc. - vomiting!