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Therapeutics P2 Winter Semester > PHRM845-FINAL EXAM > Flashcards

PHRM845-FINAL EXAM Flashcards

Pharmacology of psychedelics and psychoactive inhalants

1
Q

What are psychedelics?

A

Produce non-ordinary and variable forms of conscious experiences. These include changes in mood, thoughts, and distorted perceptual sensations gradually only experienced in dreams.

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2
Q

What are hallucinogens?

A

-It has fallen into disfavor b/c these drugs rarely produce frank hallucinations at doses commonly used.

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3
Q

What are delusions?

A

-Fixed, false belief unresponsive to logic (logic will NOT take them out of it)
-Paranoia is a common manifestation
(ex: shooting their way into building to get breakfast)

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4
Q

What are hallucinations?

A

False perception arising from internal stimuli
-Creates a false reality (auditory or visual)
(ex: bears having tea party on roof)

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5
Q

What are illusions?

A

-Misperception of external stimuli
-Distorts reality (something is actually there)
(ex: bear is sitting in a chair–it is really a person)

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6
Q

What are the two classical psychedelics?

A

-Derivatives of phenethylamine
-Derivatives of tyramine

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7
Q

What are examples of dissociative psychedelics?

A

-Phencyclidine
-Ketamine
-Muscimol

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8
Q

Dimethyltryptamine (DMT)

A

-Naturally occurring classical psychedelic drug
-From Amazonian
-Aaron Rodgers popularized this

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9
Q

5-MeODMT

A

-Naturally occurring classical psychedelic drug
- 5-6x more potent than DMT
-Derivative of DMT
-Colorado River Toad has this

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10
Q

Psilocybin (psilocin)

A

-Naturally occurring classical psychedelic drug
-Magic mushrooms
-Psilocybin is a pro-drug of psilocin (via rapid dephosphorylation)

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11
Q

Mescaline combines MOA of ___ and ___

A

-LSD and MDMA

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12
Q

Phenethylamine

A

-Amphetamine-like (stimulant and psychedelic activity)
~MDMA and bath salts
-Increases release of 5-HT> DA, NE
-Empathogens/Entactogens (more hallucinogenic than stimulatory)
-Lowest potency (~500 mg)
-Long lasting (10-12h)
-Cross tolerance to LSD due to similar MOA
~Suspected interaction with serotonin system

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13
Q

Most classical psychedelics are agonists of ____.
We want to pretreat with ___ antagonists to block psychedelic effects.
**Exception ____ stimulates 5-HT release

A

5-HT2A
5-HT2A
MDMA

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14
Q

Psychedelic drugs markedly increase ____ integration in the CNS.

A

-Global
**shows connectivity across regions of the brain

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15
Q

Effects on the dimensions and subscales of the 5-dimension altered states of consciousness (5D-ASC) scale.
-What are the 3 main sections?

A

-Visionary restructuralization (sensory illusions)
-Oceanic boundlessness (highly pleasurable state of self dissolution)
-Thought disorder leading to unpleasant state (bad trip)–> anxious ego dissolution

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16
Q

What is audio-visual synsthesiae?

A

-Hear something and see colors
-Enhanced visual perception
-Falls under visionary restructuralization (sensory illusions)

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17
Q

What is spiritual experience?

A

-Can happen to pts even without a religious background
-Connected with world like never had before
-Falls under oceanic boundlessness (highly pleasurable state of self dissolution)

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18
Q

What is blissful state?

A

-Lost all cares/concerns
-Falls under oceanic boundlessness (highly pleasurable state of self dissolution)

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19
Q

What is disembodiment?

A

-Pt feels they are outside of their body
-Falls under thought disorder leading to unpleasant state (bad trip)

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20
Q

What is impaired control and cognition?

A

-Pt cannot control themselves
-Falls under thought disorder leading to unpleasant state (bad trip)

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21
Q

Psychedelic drug use adverse effects:
Short term:_____

A

Physiological
-Tachycardia
-HTN
-Tremors
-Dry mouth
-Nausea
-Hyperthermia
**NOT life-threatening; bigger issue is how people respond

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22
Q

Psychedelic drug use adverse effects:
Acute dysphoric:_____

A

Reaction
-Terrifying thoughts (impeding doom; separating from body and won’t get back in)
-Fear of insanity
-Fear of losing control
-Fear of death
**Likely have 2 therapists

23
Q

Psychedelic drug use adverse effects:
3rd phase:____

A

Psychotic reaction
-Flashbacks (hallucinogen persisting perception disorder; can last for years and they are usually negative)
-Enduring changes in personality (whole world view might change; how do you get consent for that?)
-Exacerbate underlying psychotic disorder
-Instigate prolonged psychotic disorder
-Rate of psychosis after LSD is 1-5%

24
Q

Psychedelic drug use can lead to rapid development of ___ on the ____ consecutive day; marked attenuation of effect

A

tolerance; 3rd
-Frequent use can lead to mood changes
-No evidence of addictive potential

25
Potential therapeutic uses of psychedelics
-Cancer related psychological distress -PTSD -Depression -SUD (alcohol)
26
Shortcomings of clinical trials for psychedelics
-Small sample size -Lack of or inadequate controls (private companies providing $$ with little/no oversight) -Many investigators/patients know which medication they received -What is the proper control group?--controlled sensory input? -Selection bias (those experienced with or comfortable with psychedelic drug use)
27
Over ____ % of volunteers are excluded from psilocybin trials because of previous experience/family hx. -How is the average person going to respond to them?
90% -We don't know
28
MOA of dissociative psychedelics
-NMDA receptor antagonists 1. Inhibit GABA release 2. Disinhibition of glutamate release (increases glu levels)-->excitatory
29
Overview of glutamate receptors -(competitive/noncompetitive) antagonist that enters when channel is open -NMDA receptors are primarily (presynaptic/postsynaptic) -NMDA receptors can also bind ____
-Noncompetitive -Post-synaptic -Glycine
30
Ionotropic glutamate receptors
-NMDA receptor antagonist -Induces anesthesia AND analgesia -Taken at high enough doses, don't feel pain so pt can injure themselves and not know it
31
Ketamine ('Special K')
-Prominent NMDA receptor antagonist -Racemic mixture (S+ is more active) -Fast and short acting (10-60 min) -Esketamine recently FDA approved for tx resistant depression -Used in opioid tolerant pts for chronic pain
32
Dextromethorphan (DXM)
-Prominent NMDA receptor antagonist -In cough syrup -Also serotonin reuptake inhibitor -Abused by ~4% of high schoolers -Doses for cough suppression are <60 mg, while 100-600 mg are used to induce "high"
33
Phencyclidine (PCP)
-NMDA antagonist ~More potent than ketamine ~Also DA D2 receptor agonist -Cigarette dipped in liquid PCP (more severe interaction with ketamine) ~Nicotine or marijuana cigarette ~Effect is 4-6h -Pts often unaware of cannabis laced with PCP -Severe dissociation and analgesia ~Self-mutilation without recognition (dissociation) -Provokes psychotic rxn -Misuse associated with violence and suicide
34
Muscimol
-Different from 'magic mushrooms' -GABA-A agonist-->can induce dissociative psychedelic effects -In contrast, benzos and alcohol of allosteric modulators
35
Psychoactive inhalants
-Often 1st substance of abuse with kids (easily accessible)
36
Liquid psychoactive inhalant examples
-Paint thinner -Paint remover -Dry-cleaning fluids -Gasoline -Glue -Correction, fluids -Felt-tip markers
37
Aerosol psychoactive inhalant examples
-Spray pain -Deodorant -Hair spray -Vegetable oil spray -Fabric protector spray
38
Gases psychoactive inhalant examples
-Chloroform -Nitrous oxide -Whipped cream cans -Butane lighters -Propane tanks -Refrigerants
39
Nitrites psychoactive inhalant examples
-Leather cleaner -Room deodorizer -Food preservatives
40
Inhalants can be misused in many ways. Provide ways of routes of administration
-Sniffing -Huffing (gives highest concentration)--soak cloth and hold over face -Bagging (spray into paper bag and breathe in) -Dusting (put dust remover spray nozzle into mouth)
41
Alkyl nitrites
-Commonly sold as "poppers" -Marketed as cleaning solutions and room deodorizers -Nitric oxide release results in smooth muscle relaxation, platelet inhibition, and change in gene expression -Relaxes anal sphincter, enhances erections, and gives pt euphoria -Highest abuse among gay men (25x) -Methemoglobinemia is greatest risk
42
Pharmacology of volatile solvents
-Widely used! -Volatile solvents are liquid at room temp and evaporate readily when exposed to air
43
Toluene
-Volatile solvent -Model glues, correction fluids, lacquer thinners, plastic cements, spray paints
44
Acetone
-Volatile solvent -Nail polish remover -Model glue -Rubber cements
45
Benzene
-Volatile solvent -Cleaning fluids, rubber cements, tire tube repair kits
46
Butane
-Volatile solvent -Cigarette lighters, hair spray, spray paint
47
Highest volatile solvent use is among ___
Adolescents, especially in isolated communities (access driven?)
48
____ is the most characterized of the volatile solvents. Not a lot of research on it, but alters activity of a wide range of ion channels.
-Toluene **GABA-A is the strongest channel that is potentiated
49
Acute effects (min) of volatile solvents
-Locomotor stimulation -Euphoria, exhilaration
50
Effects of high dose (>3000 ppm) of volatile solvents
-CNS depression -Slurred speech -Disorientation -Weakness -Sedation
51
Repeated exposure to toluene causes ___
Lipid accumulation
52
Risks of inhalant abuse
-Asphyxiation: from repeated inhalations that lead to high concentrations of inhaled fumes, which displace available O2 in lungs -Suffocation: from blocking air entering lungs when inhaling fumes from a plastic bag placed over the head -Convulsions/seizures: from abnormal electrical discharges in the brain -Coma: from brain shutting down all but most vital functions -Choking: from inhaling vomit after inhalant use -Fatal injury: from accidents including motor vehicle fatalities suffered while intoxicated
53
Based on independent studies performed over a 10-year period in 3 different states, the number of inhalant-related fatalities in the US is approximately ____ per year.
100-200 **Not clear how frequently it causes fatality
54
Sudden sniffing death syndrome
-Most concerning response -Development of fatal arrhythmias within minutes of inhalation -Compulsive use (some use it chronically) -Neurotoxicity ~Brain is smaller and fills less of the space inside the skull

Therapeutics P2 Winter Semester (29 decks)

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