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PHRM 845 final > Svensson Lectures > Flashcards

Svensson Lectures Flashcards

1
Q

Psychostimulants use & effects

A
  • activate CNS resulting in alertness, excitation, and elevated mood
  • stimulants play a major role in drug abuse crisis
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2
Q

Stimulants historical & medical use

A
  • Cocaine: reduce hunger & fatigue; anesthetic
  • ephedrine widely used for asthma & overall stimulant properties
  • nicotine smoking to treat asthma
  • amphetamines for various uses
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3
Q

Nicotine - MOA

A
  • activates nicotinic acetylcholinergic receptor
  • Na enters cell, K exits, which creates an action potential.
  • heterogeneity of subunits determines how many molecules of Ach bind to receptor
  • variation in receptor composition at different sites may influence physiological response
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4
Q

ACh vs Nicotine

A
  • both have charged amino groups and H bond acceptor groups
  • nicotine is membrane penetrable at physiological pH
  • nicotine is not degraded by acetylcholinesterase
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5
Q

partial agonist therapy

A
  • causes release of dopamine
  • highly addictive
  • nicotine replacement therapy relatively ineffective alone
  • varenicline partial agonist increases quit rate success
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6
Q

Cocaine MOA

A
  • antagonist of amine transporters: DAT, SERT, NET
  • DAT>= SERT > NET
  • prevents DA reuptake and increases DA concentration
  • also increases duration of dopamine action
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7
Q

Methamphetamine, Ecstasy, & Bath Salts – MOA

A
  • amphetamines/XTC/bath salts compete for reuptake (resemble endogenous DA, NE; they block DA reuptake and push out DA from vesicles)
  • increase extra-vesicular DA, reverse transport gradient
  • amphetamines are MAOi’s
  • activate Trace amine-associated receptor (TAAR1) which phosphorylates DAT and induces reverse transport function
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8
Q

Mesolimbic Dopamine System

A

key dopaminergic pathway that transports dopamine from the ventral tegmental area to the nucleus accumbens and amygdala

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9
Q

addiction liability

A
  • likelihood that a person using the drug will become addicted
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10
Q

sympathomimetic toxidrome

A

a constellation of signs/symptoms indicative of ingestion of psychostimulant

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11
Q

cocaine

A

a psychostimulant first isolated from cocoa leaves in 1857. primarily an inhibitor of dopamine transporter, preventing reuptake of DA released into synaptic cleft

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12
Q

Nicotine

A

most addictive substance in current use; activates nicotinic acetylcholinergic receptors
- (other psychostimulants directly enhance dopamine release and inhibit reuptake)

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13
Q

methamphetamine, ecstacy, MDMA

A

psychostimulants that primarily release endogenous DA

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14
Q

cathinones

A

derivatives of Khat plant (bath salts) that display similat activity to methamphetamine

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15
Q

dose-effect of psychostimulants

A

low dose - enhance wakefulness and vigilance

higher doses - increase agression, euphoria, and psychosis

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16
Q

chronic psychostimulant use effects

A
  • produce tremors, anxiety, paranoia, delusions, repetitive behavior, profuse dental decay, dilated cardiomyopathy
  • results in downregulation of DA receptors (return to baseline after period of abstinence)
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17
Q

Hallmarks of Sympathomimetic Syndrome

A

MATHS:
- mydriasis
- aggitation/arrhythmia/angina
- tachycardia
- hypertension/hyperthermia
- seizures/sweating

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18
Q

Hemp

A

a strain of cannabis that is grown for agricultural products and contains less than 0.3% THC

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19
Q

Marijuana

A

a strain of cannabis sativa that commonly contains 15-20% THC content for its psychoactive effects

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20
Q

Synthetic Marijuana

A

Illicit synthetic compounds that are analogs of THC and bind to CB1 receptor as full agonists producing similar psychoactive effects as THC

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21
Q

Endocannabinoid System

A

an endogenous system comprised of four components
1 cannabinoid receptors
2 ligands
3 endocannabinoid membrane transporters
4 synthetic and degradative enzymes
this system regulates immunity, memory, mood, pain, and perception

22
Q

THC

A

tetrahydrocannabinol is the primary euphoric component in marijuana is an agonist of CB1 and CB2 receptors of ECS

23
Q

CBD

A

cannabidoil is a non-euphoric natural cannabinoid widely marketed for variety of uses that is not an agonist for CB receptors

24
Q

Δ8-THC:

A

A euphoric componene in cannabis sativa that is increasingly present in the unregulated market

25
Q

Dronabinol/Marinol

A

schedule III FDA approved synthetic Δ9-THC in sesame oil indicated for AIDS-associated anorexia and refractory chemotherapy-related nausea and vomiting

26
Q

Nabilone/Cesamet

A

A schedule II FDA approved THC mimetic for chemotherapy induced N/V

27
Q

Cannabidoil/Epidolex

A

FDA approved form of CBD indicated for 2 rare seizure disorders, Dravet Syndrome and Lennox-Gastaut Syndrome

28
Q

Endocannabinoids and phytocannabinoids

A

primarly serve as retrograde regulators of neurotransmission
- inhibit release of GABA and glutamine

29
Q

Psychadelics

A

agents that produce non-ordinary and variable forms of conscious experiences.
- ex: changes in mood, thoughts, distorted perceptual sensations generally only experienced in dreams

30
Q

delusion

A
  • fixed, false belief unresponsive to logic
  • despite contrary evidence, a person in a delusional state cant let go of these convictions
  • paranoia is a common manifestation
31
Q

hallucination

A
  • a false perception arising from internal stimuli
  • creates a false reality
32
Q

illusion

A
  • a misperception of external stimuli
  • special perceptual experiences in which information arising from “real” stimuli leads to incorrect perception
  • distorts reality
  • misperceiving something that’s true
33
Q

visionary restructuralization

A

sensory illusions

34
Q

oceanic boundlessness

A

highly pleasurable state of self-dissolution

35
Q

anxious ego-dissolution

A

thought disorder leading to unpleasant state of anxiety and sense of loss of control

36
Q

LSD

A

lysergic acid is the most widely recognized classical psychedelic and is a derivative of tryptamine

37
Q

DMT

A

dimethyltryptamine is a naturally occuring psychedelic found in Ayahuasca Vine, haarvested in peruvian amazon

38
Q

Psilocybin

A

prodrug of psychedelic psilocin and found in over 200 types of mushrooms

39
Q

mescaline

A

phenethylamine psychedelic found in Peyote cactus and other plants that has amphetamine-like activity

40
Q

Ketamine

A

dissociative psychedelic that is an NMDA receptor antagonist and induces anesthesia and analgesia

41
Q

Dextromethorphan

A

antagonist of NMDA receptor, and SERT inhibitor
- commonly found in OTC cough syrups

42
Q

Phencyclidine

A

NMDA antagonist that is more potent than ketamine and sometimes used to lace tobacco or marijuana cigarettes

43
Q

Muscimol

A

agonist of GABAa found in Amanita muscaria
- dissociative psychedelic

44
Q

Alkyl nitrites

A

commonly known as ‘poppers’
- release nitric oxide
- AE arise from the production of methemoglobinemia

45
Q

Volatile solvents

A

compounds that are liquid at room temp but readily evaporate when exposed to air
- psychoactive volatile solvents affect numerous ion channels in CNS through GABAa potentiation.
– predominantly used by adolescents

46
Q

At common doses psychedelics induce ___

A

illusions rather than hallucinations

47
Q

classical psychedelics

A
  • derived from phenethylamine or tryptamine
  • act as agonist of 5HT2A receptor
  • ingestion results in increased global integration in the brain
48
Q

Primary adverse effects of classical psychedelics

A

acute dysphoric reaction or prolonged psychotic reactions

49
Q

dissociative anaesthetics

A

NMDA antagonists that induce anesthesia and analgesia

50
Q

Sudden Sniffing Death Syndrome

A

a lethal arrhythmia developed after inhilation of volitale solvent (toluene)

51
Q

Long-term volatile solvent inhalation

A
  • neurotoxic in both individuals who inhale them recreationally and via occupational exposure
52
Q
A

PHRM 845 final (4 decks)

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