Drugs of Abuse Flashcards
Psychoactive substances that powerfully alter perceptions, mood, and otehr cognitive processes
Hallucinogen
Diethylpropion
type of drug?
What blocks metabolism and what does this mean?
- Methyl group blocks MAO metabolism so this is going to be longer acting compared to one without the methyl
- Anorexic agent tertiary amine
drugs that distort perceptions of sight and sound and produce feelings of detachment from the environment and self
Dissociatives
Weed, Ketamine
phendimetrazine
type?
locked?
- Anorexic agent
- locked conformer
If there is a methoxy group present or something similar what should you know?
Know that its not a stimulant
For CNS activity what do you not want?
- 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
Lorcaserin
type
MOA
- Selective 5-HT2C
- Anorexic agent
Purine are?
R1=CH3
R2=CH3
R3 = H
Theophylline
R1=H
R2=CH3
R3 = CH3
Theobromine
R1=CH3
R2=CH3
R3 = CH3
Caffeine
Purines are analeptics
Hallucinogen, Stimulant or Empathogenic?
Empathogenic
Hallucinogen, Stimulant or Empathogenic?
Hallucinogen
- Lysergic acid derivatives – LSD
- Phenylethylamines – Mescaline
- Indolealkylamines – Dimethyltryptamine
- Other indole derivatives – Harma alkaloids
These are known as?
Classical Hallucinogens
drugs that cause hallucinations: apparent sights, sounds or other sensual experiences that do not actually exist or do not exist for other people.
Hallucinogens
Seritonergics
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.
Psychotomimetics/ Hallucinogens
SAR for amphetamine like stimulants and DOM-like action of phenylisopropylamines
Ketone increases potency for both.
Methylphenidate
DOA
Treatment?
- ADD med
- shorter acting compared to others in class
- Amphetamine like
Lisdexamphetamine
- Prodrug contains lysine within structure
SAR of indolealkylamines and related agents
Need alpha carbon substitution to block MAO metabolism or di substitution on the Nitrogen
SAR of stimulants S configuration=?
R=?
What other things
- S= Stimulant
- R= Hallucinogen
- Adding methyl group increases potency
- 2>1>>>3
Marijuana can produce impairment in?
Performance, Memory, learning
What are th black box warnings for ADHD stimulants?
Theres 2
- 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).
- U.S. Boxed Warning (ADHD Stimulant drugs): Potential for drug dependency exists; prolonged use may lead to drug dependency
Cannabinoid SAR
Metabolism?
- 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
Halluncinogen, Stimulant or Empathogenic?
Stimulant
2a =
2b =
2c=
- Hallucination
- Cardiac
- Weight loss
Adderall
BOOM
Number 1 abused substance?
Caffeine
Hallucinogen pharmacological substances
- Cannabinoids
- NMDA antagonists, anticholinergics
- Ecstacy and others
Cannabinoids on the market?
- Dronabinol
- Nabilone
Phentermine
type
special?
- Anorexic agent
- Disubstitution on the alpha carbon reduces MAO metabolism and reduced CNS activity switching it from stimulant to anorexic agent.
What is the number one metabolite for amphetamine?
What else can it be metabolized to though?
- Amphetamine
- Can also be metabolized to carboxylic acid and hydroxyamine
Benzphetamine is a?
Switching what changes the action of this.
- Anorexic agent
- Tertiary nitrogen or larger substituent like the benzyl ring on this one switches it from a stimulant to an anorexic agent.
Classical hallucinogen posses what general structure?
What are the two major categories?
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
Rimonabant
type of drug
MOA
Anorexic
Cannabinoid inverse agonist
