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Medicinal Chem > Drugs of Abuse > Flashcards

Drugs of Abuse Flashcards

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1
Q

Psychoactive substances that powerfully alter perceptions, mood, and otehr cognitive processes

A

Hallucinogen

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2
Q

Diethylpropion

type of drug?

What blocks metabolism and what does this mean?

A
  • Methyl group blocks MAO metabolism so this is going to be longer acting compared to one without the methyl
  • Anorexic agent tertiary amine
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3
Q

drugs that distort perceptions of sight and sound and produce feelings of detachment from the environment and self

A

Dissociatives

Weed, Ketamine

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4
Q

phendimetrazine

type?

locked?

A
  • Anorexic agent
  • locked conformer
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5
Q

If there is a methoxy group present or something similar what should you know?

A

Know that its not a stimulant

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6
Q

For CNS activity what do you not want?

A
  • Dont want substituent on ring
  • Dont want tertiary nitrogen
  • Dont want a long chain on the alpha carbon
    • Can have methyl or ethyl but propyl is too big
  • If it as any of these things CNS activity is decreased
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7
Q

Lorcaserin

type

MOA

A
  • Selective 5-HT2C
  • Anorexic agent
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8
Q

Purine are?

R1=CH3

R2=CH3

R3 = H

Theophylline

R1=H

R2=CH3

R3 = CH3

Theobromine

R1=CH3

R2=CH3

R3 = CH3

Caffeine

A

Purines are analeptics

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9
Q

Hallucinogen, Stimulant or Empathogenic?

A

Empathogenic

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10
Q

Hallucinogen, Stimulant or Empathogenic?

A

Hallucinogen

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11
Q
  • Lysergic acid derivatives – LSD
  • Phenylethylamines – Mescaline
  • Indolealkylamines – Dimethyltryptamine
  • Other indole derivatives – Harma alkaloids

These are known as?

A

Classical Hallucinogens

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12
Q

drugs that cause hallucinations: apparent sights, sounds or other sensual experiences that do not actually exist or do not exist for other people.

A

Hallucinogens

Seritonergics

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13
Q

Are those which upon administration of a single effective dose (a) consistently produce changes in thought, mood, and perception with little memory impairment, (b) produce little stupor, narcosis, or excessive stimulation, (c) produce miminal autonomic side effects, and (d) are nonaddicting.

A

Psychotomimetics/ Hallucinogens

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14
Q

SAR for amphetamine like stimulants and DOM-like action of phenylisopropylamines

A

Ketone increases potency for both.

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15
Q

Methylphenidate

DOA

Treatment?

A
  • ADD med
  • shorter acting compared to others in class
  • Amphetamine like
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16
Q

Lisdexamphetamine

A
  • Prodrug contains lysine within structure
17
Q

SAR of indolealkylamines and related agents

A

Need alpha carbon substitution to block MAO metabolism or di substitution on the Nitrogen

18
Q

SAR of stimulants S configuration=?

R=?

What other things

A
  • S= Stimulant
  • R= Hallucinogen
  • Adding methyl group increases potency
  • 2>1>>>3
19
Q

Marijuana can produce impairment in?

A

Performance, Memory, learning

20
Q

What are th black box warnings for ADHD stimulants?

Theres 2

A
  1. U.S. Boxed Warning (ADHD Stimulant drugs): Use has been associated with serious cardiovascular events including sudden death in patients with preexisting structural cardiac abnormalities or other serious heart problems (sudden death in children and adolescents; sudden death, stroke and MI in adults).
  2. U.S. Boxed Warning (ADHD Stimulant drugs): Potential for drug dependency exists; prolonged use may lead to drug dependency
21
Q

Cannabinoid SAR

Metabolism?

A
  • Adding 11- OH group increases potency
  • Moving 9-10 dbl bond to 9-8 increases potency
  • Replace penyl with a 1,1 dimethylheptyl increases potency
  • Major metabolite Allylic hydroxylation at 11 group
  • Omega minus one
  • Conjugation at phenol
22
Q

Halluncinogen, Stimulant or Empathogenic?

A

Stimulant

23
Q

2a =

2b =

2c=

A
  • Hallucination
  • Cardiac
  • Weight loss
24
Q

Adderall

A

BOOM

25
Q

Number 1 abused substance?

A

Caffeine

26
Q

Hallucinogen pharmacological substances

A
  • Cannabinoids
  • NMDA antagonists, anticholinergics
  • Ecstacy and others
27
Q

Cannabinoids on the market?

A
  • Dronabinol
  • Nabilone
28
Q

Phentermine

type

special?

A
  • Anorexic agent
  • Disubstitution on the alpha carbon reduces MAO metabolism and reduced CNS activity switching it from stimulant to anorexic agent.
29
Q

What is the number one metabolite for amphetamine?

What else can it be metabolized to though?

A
  • Amphetamine
  • Can also be metabolized to carboxylic acid and hydroxyamine
30
Q

Benzphetamine is a?

Switching what changes the action of this.

A
  • Anorexic agent
  • Tertiary nitrogen or larger substituent like the benzyl ring on this one switches it from a stimulant to an anorexic agent.
31
Q

Classical hallucinogen posses what general structure?

What are the two major categories?

A

Ar-C-C-N

  • Where Ar is a substitued phenyl, 3-indolyl, 3-indoyl moiety, C-C is an ethyl or branched ethyl chain, N is primary, secondary, or tertiary amine
  • indolealkylamine IAAs, phenylalkylamines (PAAs), These have different SARs

Classical agents meet the hollister definition and also bind to 5-HT2 receptors

32
Q

Rimonabant

type of drug

MOA

A

Anorexic

Cannabinoid inverse agonist

Medicinal Chem (15 decks)

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