pharmacology

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111 Terms

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define ligand
any molecule that binds to a receptor
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define endogenous ligand
ligand (naturally in body) normally produced by the body that binds a receptor (neurotransmitters)
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define exogenous ligand
ligand introduced into the body (drugs)
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Define agonist
ligand that activates receptors
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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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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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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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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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define binding affinity
"strength" of binding between ligand and receptor
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A higher concentration for a low or high affinity drug/ligand?
LOW affinity drug/ligand
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A lower concentration for a low or high affinity drug/ligand?
HIGH affinity drug/ligand
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if high & low affinity are both at equal concentration...?
higher affinity drug binds to more receptors than low affinity
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Kd (Affinity constant)
Dissociation constant. On graph it is the ligand concentration at which 1/2 receptors bound
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low Kd = ___ affinity & why?
high affinity cuz need less concentration of ligand
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high Kd = ______ affinity & why?
low affinity cuz need higher concentration to reach 100% binding
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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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EC50 stands for?
Concentration of the drug required to produces 50% of maximal effect; measures efficacy
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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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a ____ agonist has ___ efficacy then a ____ agonist
a partial agonist has lower efficacy than a full agonist
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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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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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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
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
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ED 50 (effective dose)
the dose where drug shows 50% of max effectiveness
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therapeutic index
distance between LD50 & ED50 \n (lethal dose & effective dose)
distance between LD50 & ED50 \n (lethal dose & effective dose)
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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)
the safer the drug (over the counter drugs)
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narrow therapeutic index means?
overdose is easier (needs higher regulation)
overdose is easier (needs higher regulation)
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TD50 (toxic dose)
dose where drug causes some toxicity (harm) in 50% of subjects
dose where drug causes some toxicity (harm) in 50% of subjects
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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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define functional tolerance
targeted receptors adapt
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functional tolerance: antagonist
neurons may express MORE receptors if drug is an antagonist
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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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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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define addiction
chronic relapsing disorder characterized by compulsive drug seeking behavior

-physical dependence, tolerance, & sensitization do not equal addiction
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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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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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2) intraperitoneal (IP)
inject into abdominal cavity
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3) intramuscular (IM)
inject into muscle
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4) subcutaneous (SQ); slowest
inject under skin
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Routes of administration of drugs: inhalation

1. gases
2. smokes
3. solids
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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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Routes of administration of drugs: slower routes

1. oral (ingested)
2. transdermal
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slower routes: oral (ingested)
absorbed mostly through intestines, then through capillaries
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slower routes: transdermal
not readily absorbed through epidermis (skin)
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Typical Antipsychotics effectiveness
1st generation/typical in 1950s \n decrease positive effects of schizophrenia (hallucinations, delusions) \n -ex: chlorpromazine, haloperidol
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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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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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atypical antipsychotics mechanism
antagonist on 5-HT2 (serotonin), D1 (excitatory dopamine), D2, and α1 (norepinephrine) receptors
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antidepressants
used to treat affective (mood) disorders
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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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antidepressants: MAOIs
monoamine oxidase inhibitors \n -block monoamine (enzyme) from breaking down/degradation of DA, NE, & 5-HT
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antidepressants: TCA's
Tricyclic Antidepressants \n -block reuptake of NE & 5-HT
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Anxiolytics (Benzodiazepines) \n -depressants
ex: xanax, valium, Ativan
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Anxiolytics: Benzodiazepines effectiveness \n -depressants
anxiety & panic
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Anxiolytics: Benzodiazepines side effects

\-depressants
tolerance, cross tolerance, interaction w/ alcohol, high abuse potential
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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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Alcohol side effect \n -depressants
\-addiction \n -tolerance \n -physical dependence
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alcohol mechanism
agonist (activates) GABA receptors (also, DA, opioid, & NMDA receptors
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Some structural effects of alcoholism are...
reversible since studies show improvements in MRI scans after one month of no alcohol
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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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endogenous opioids in brain?
endorphins, enkephalins, dynorphins
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Heroin \n -opioids
\-structurally similar to morphine (convert to morphine in brain) \n -produces euphoria, highly addictive
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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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Nalaxone
opioid antagonist that rapidly reverses overdose
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Cannabinoids: cannabis effectiveness
therapeutic uses: anxiety, pain (chronic>acute), chemotherapy side effects, glaucoma, epilepsy, MS (multiple sclerosis), spasticity
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Cannabinoids: cannabis side effects
feelings of relaxation, hunger, sometimes paranoia
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Cannabinoids: cannabis mechanism
agonist at CB1 & CB2 cannabinoid receptors (GPCRs)
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stimulants: nicotine side effects
increase alertness, heart rate, blood pressure, digestion
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stimulants: nicotine
mildly neuroprotective in Parkinson's, Alzheimer's, MCI (mild cognitive impairment)
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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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stimulants: Caffeine side effects
increase blood pressure, tolerance, physical dependence
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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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Stimulant: Amphetamines
increase alertness, motivation, endurance, euphoria \n -longterm lead to schizoid behavior
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Stimulant: Amphetamines side effects
increased blood pressure, tolerance, physical dependence
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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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Stimulants: Cocaine
creates euphoric state, increases endurance
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Stimulants: Cocaine side effects
long term use lead to psychosis, neurodegeneration, altered brain activity
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Stimulants: cocaine mechanism
\-DAT (transporter) antagonist \n -blocks monoamine NT reuptake (especially DA)
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Empathogen: MDMA
promising treatment for PTSD
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Empathogen: MDMA side effects
\-social, empathic, visual, euphoric (pos) \n -neurotoxic to thermoregulatory systems (risk of hyperthermia; neg)
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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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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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psychedelics: LSD mechanism
agonist at 5-HT2a receptor which is highly expressed in visual cortex
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Dissociative: PCP and Ketamine
developed as anesthetics in 1960s \n -used in vet clinics & children in hospitals
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Dissociative: PCP and ketamine side effects
produce dreamlike state, detachment from reality, separation between consciousness & sensory inputs
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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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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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Reward circuitry:dopamine
\-DA=key NT affected by addictive drugs \n -DA released from VTA neurons into nucleus accumbens
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Reward circuitry:
drugs like stimulants, opioids, etc directly or indirectly activate mesocorticolimbic neural circuit that mediates reward & pleasure