pharmacology

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1

define ligand

any molecule that binds to a receptor

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2

define endogenous ligand

ligand (naturally in body) normally produced by the body that binds a receptor (neurotransmitters)

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3

define exogenous ligand

ligand introduced into the body (drugs)

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4

Define agonist

ligand that activates receptors

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5

Define antagonist

ligand that has no effect on its own but blocks binding of exogenous ligand (neurotransmitter receptor blocker)

-competes w/ endogenous ligand

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6

Define non-competitive ligand

binds to site other than endogenous ligand binding site & modulates receptor activity (non-competitive inotropic neurotransmitter receptor blocker)

-have agonist or antagonist properties

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7

Define affinity

The strength of attraction between drug and receptor at any drug concentration concentration or firmness w/ which drug binds to receptor

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8

Define efficacy

(intrinsic activity) is the ability of a drug to illicit a pharmacological response (physiological) when interaction occurs w/ a receptor (relationship between response & occupancy of receptor)

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9

define binding affinity

"strength" of binding between ligand and receptor

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10

A higher concentration for a low or high affinity drug/ligand?

LOW affinity drug/ligand

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11

A lower concentration for a low or high affinity drug/ligand?

HIGH affinity drug/ligand

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12

if high & low affinity are both at equal concentration...?

higher affinity drug binds to more receptors than low affinity

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13

Kd (Affinity constant)

Dissociation constant. On graph it is the ligand concentration at which 1/2 receptors bound

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14

low Kd = ___ affinity & why?

high affinity cuz need less concentration of ligand

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15

high Kd = ______ affinity & why?

low affinity cuz need higher concentration to reach 100% binding

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16

Define efficacy simpler def

max effect a drug can produce regardless of dose; ability of drug-bound receptor to produce a full response

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17

EC50 stands for?

Concentration of the drug required to produces 50% of maximal effect; measures efficacy

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18

a full agonist has a _____ efficacy & produces _____

response while occupying a relatively low proportion of receptors

a full agonist has a high efficacy & produces a full response while occupying a relatively low proportion of receptors

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19

a ____ agonist has ___ efficacy then a ____ agonist

a partial agonist has lower efficacy than a full agonist

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20

explain selectivity of a drug

-common for some drugs to bind to many receptor types or bind to several members of same neurotransmitter receptor class

-less common for drugs to selectivity bind to 1 or 2 receptors

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21

Why are relative affinities of a drug at diff receptors exploited?

to adjust the dose down so only highest affinity receptors are bound & activated ("targeted") minimize side effects

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22

Evaluate dose response curves.

linear segment starts low, increases then levels off as it approaches max value (sigmoidal relationship) between dose & effect

- w/in limits increasing dose=increase desired effect

<p>linear segment starts low, increases then levels off as it approaches max value (sigmoidal relationship) between dose &amp; effect</p><p>- w/in limits increasing dose=increase desired effect</p>
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23

ED 50 (effective dose)

the dose where drug shows 50% of max effectiveness

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24

therapeutic index

distance between LD50 & ED50 \n (lethal dose & effective dose)

<p>distance between LD50 &amp; ED50 \n (lethal dose &amp; effective dose)</p>
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LD 50 (lethal dose)

dose of drug at which is lethal (death) in 50% of subjects

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wide therapeutic index means?

the safer the drug (over the counter drugs)

<p>the safer the drug (over the counter drugs)</p>
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27

narrow therapeutic index means?

overdose is easier (needs higher regulation)

<p>overdose is easier (needs higher regulation)</p>
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TD50 (toxic dose)

dose where drug causes some toxicity (harm) in 50% of subjects

<p>dose where drug causes some toxicity (harm) in 50% of subjects</p>
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Define psychoactive drugs

exogenous ligand that in small amounts alters experiences, emotion, mood, attention...

-natural or synthetic

-agonist, antagonist, or non-competitive ligand

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Define tolerance

decrease in effect of drug after repeated use; over time need higher dose to get same effect

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define metabolic tolerance

body gets better at eliminating drug

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32

define functional tolerance

targeted receptors adapt

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33

functional tolerance: antagonist

neurons may express MORE receptors if drug is an antagonist

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34

functional tolerance: agonist

neurons may express LESS receptors if drug is an agonist

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define physical dependence

stop using drugs leads to physical withdrawal symptoms

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36

define psychological dependence

stop using drugs leads to psychological withdrawal symptoms; anxiety, distress

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Define withdrawal

actual symptoms after stop using drug; specific symptoms depend on drug

ex: fatigue after stop using caffeine

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38

define addiction

chronic relapsing disorder characterized by compulsive drug seeking behavior

-physical dependence, tolerance, & sensitization do not equal addiction

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39

rate of absorption for injections: highest to lowest

  1. intravenous (IV); fastest

  2. intraperitoneal (IP)

  3. intramuscular (IM)

  4. subcutaneous (SQ); slowest

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40

rate of absorption for injections depends on?

density of capillaries/blood flow

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  1. intravenous (IV); fastest

inject into vein

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42
  1. intraperitoneal (IP)

inject into abdominal cavity

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43
  1. intramuscular (IM)

inject into muscle

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  1. subcutaneous (SQ); slowest

inject under skin

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45

Routes of administration of drugs: inhalation

  1. gases

  2. smokes

  3. solids

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46

inhalation: gases

lungs - a lot of surface area exposed to air and capillaries

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inhalation: smokes

different from gas because includes vapor and ash particles, but absorbed similarly

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inhalation: solids

inhaled through nose; not as efficient as lungs

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49

Routes of administration of drugs: slower routes

  1. oral (ingested)

  2. transdermal

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50

slower routes: oral (ingested)

absorbed mostly through intestines, then through capillaries

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51

slower routes: transdermal

not readily absorbed through epidermis (skin)

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52

Typical Antipsychotics effectiveness

1st generation/typical in 1950s \n decrease positive effects of schizophrenia (hallucinations, delusions) \n -ex: chlorpromazine, haloperidol

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53

Typical Antipsychotics side effects

- dry mouth \n -hypotension \n -dystonia (involuntary muscle contraction) \n -tardive dyskinesia (repetitive movement) \n -Parkinsonism \n -weight gain

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Typical Antipsychotics mechanism

antagonist. (block) D2 receptors (inhibitory dopamine)

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55

atypical antipsychotics

2nd gen/1980s \n (ex: olanzapine & risperidone)

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atypical antipsychotics effectiveness

decrease positive (hallucinations) & negative symptoms in schizophrenia (delusions, catatonia)

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atypical antipsychotics side effects

hypotension, diabetes, weight gain

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58

atypical antipsychotics mechanism

antagonist on 5-HT2 (serotonin), D1 (excitatory dopamine), D2, and α1 (norepinephrine) receptors

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59

antidepressants

used to treat affective (mood) disorders

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60

Antidepressants: SSRIs & SNRIs

-selective serotonin reuptake inhibitors & serotonin & norepinephrine reuptake inhibitors \n \n block reuptake of 5-HT &/or NE (norepinephrine); antagonist at SERT & NET (transporters) \n increase serotonin activity

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61

antidepressants: MAOIs

monoamine oxidase inhibitors \n -block monoamine (enzyme) from breaking down/degradation of DA, NE, & 5-HT

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62

antidepressants: TCA's

Tricyclic Antidepressants \n -block reuptake of NE & 5-HT

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63

Anxiolytics (Benzodiazepines) \n -depressants

ex: xanax, valium, Ativan

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64

Anxiolytics: Benzodiazepines effectiveness \n -depressants

anxiety & panic

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65

Anxiolytics: Benzodiazepines side effects

-depressants

tolerance, cross tolerance, interaction w/ alcohol, high abuse potential

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66

Anxiolytics: Benzodiazepines mechanism

-depressants

bind to non-NT site on GABAa receptors, enhance Cl- currents triggered by GABA \n \n -non competitive agonist, increase GABA signaling

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67

Alcohol side effect \n -depressants

-addiction \n -tolerance \n -physical dependence

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68

alcohol mechanism

agonist (activates) GABA receptors (also, DA, opioid, & NMDA receptors

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69

Some structural effects of alcoholism are...

reversible since studies show improvements in MRI scans after one month of no alcohol

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70

Opioid side effects

\n AKA opiate \n -euphoria \n -tolerance \n -physical dependence \n -cross tolerance \n -respiratory depression \n -constipation \n -high abuse potential

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Opioid mainly acts on...

reward areas of the brain (nucleus accumbens)

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72

endogenous opioids in brain?

endorphins, enkephalins, dynorphins

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73

Heroin \n -opioids

-structurally similar to morphine (convert to morphine in brain) \n -produces euphoria, highly addictive

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74

Heroin mechanism \n -opioids

-(agonist) acts on μ-opioid receptors in VTA (ventral tegmental area) & nucleus accumbens, parts of mesocorticolimbic DA pathway involved in reward/reinforcement \n \n -activates μ-opioid receptors hyperpolarizes (Cl- in) GABAergic neurons & inhibits GABA release onto DA neurons=increase DA in VTA (inhibits inhibition)

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75

Nalaxone

opioid antagonist that rapidly reverses overdose

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76

Cannabinoids: cannabis effectiveness

therapeutic uses: anxiety, pain (chronic>acute), chemotherapy side effects, glaucoma, epilepsy, MS (multiple sclerosis), spasticity

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77

Cannabinoids: cannabis side effects

feelings of relaxation, hunger, sometimes paranoia

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78

Cannabinoids: cannabis mechanism

agonist at CB1 & CB2 cannabinoid receptors (GPCRs)

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79

stimulants: nicotine side effects

increase alertness, heart rate, blood pressure, digestion

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80

stimulants: nicotine

mildly neuroprotective in Parkinson's, Alzheimer's, MCI (mild cognitive impairment)

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81

stimulants: nicotine mechanism

agonist at nicotinic acetylcholine receptor (AChRs) in CNS & autonomic ganglia (higher bind affinity AChR>ACh) \n \n -activates DA in VTA (reward)

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82

stimulants: Caffeine side effects

increase blood pressure, tolerance, physical dependence

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83

stimulants: caffeine mechanism

\n adenosine receptor (AR) antagonist on pre-synaptic terminals \n \n -adenosine=drowsy \n -activated AR inhibit monoamine & ACh (acetylcholine)

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84

Stimulant: Amphetamines

increase alertness, motivation, endurance, euphoria \n -longterm lead to schizoid behavior

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85

Stimulant: Amphetamines side effects

increased blood pressure, tolerance, physical dependence

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86

Stimulant: Amphetamines mechanism

Increase DA & NE, levels at the synapse (by acting w/in axon terminals) and decreasing reuptake \n \n -DAT reverse transport send NT out instead of back

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87

Stimulants: Cocaine

creates euphoric state, increases endurance

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88

Stimulants: Cocaine side effects

long term use lead to psychosis, neurodegeneration, altered brain activity

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89

Stimulants: cocaine mechanism

-DAT (transporter) antagonist \n -blocks monoamine NT reuptake (especially DA)

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90

Empathogen: MDMA

promising treatment for PTSD

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91

Empathogen: MDMA side effects

-social, empathic, visual, euphoric (pos) \n -neurotoxic to thermoregulatory systems (risk of hyperthermia; neg)

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92

Empathogen: MDMA mechanism

-agonist at 5-HT2a receptors, 5-HT1B & SERT (transporter) \n -inc release of DA, NE, 5-HT, oxytocin

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93

psychedelics: LSD (lysergic acid diethylamide) side effect

-distorts visual perception, induces feeling of creativity \n -may cause long term changes in mood/personality

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94

psychedelics: LSD mechanism

agonist at 5-HT2a receptor which is highly expressed in visual cortex

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95

Dissociative: PCP and Ketamine

developed as anesthetics in 1960s \n -used in vet clinics & children in hospitals

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96

Dissociative: PCP and ketamine side effects

produce dreamlike state, detachment from reality, separation between consciousness & sensory inputs

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97

Dissociative: PCP (phencyclidine; aka angel dust)mechanism

antagonist of NMDA receptor-type glutamate receptors, inhibits DA reuptake \n \n -induces depersonalization, schizoid behaviors, hallucinations, aggressions

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98

Dissociative: Ketamine (Special K) mechanism

competitive antagonist of NMDA receptor-type glutamate receptors, inhibits DA reuptake \n \n -medical use: anesthetic, pain killer, rapid long-lasting antidepressant (one dose lasts for weeks)

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99

Reward circuitry:dopamine

-DA=key NT affected by addictive drugs \n -DA released from VTA neurons into nucleus accumbens

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100

Reward circuitry:

drugs like stimulants, opioids, etc directly or indirectly activate mesocorticolimbic neural circuit that mediates reward & pleasure

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