IP 7 Lecture 8 | Use Disorder Classes & Mechanism of Actions

Heroin

Class 1

Full MOR Agonist

Naloxone / Naltrexone

Opioid Overdose Treatment

MOR Competitive Antagonist

Methadone

Opioid Withdrawal Treatment

Full MOR Agonist

Buprenorphine +/- Naloxone

Opioid Withdrawal Treatment

Partial MOR Agonist

Clonidine

Opioid Withdrawal Treatment

Alpha 2 Adrenergic Agonist

Lofexidine

Opioid Withdrawal Treatment

Alpha 2 Adrenergic Agonist

Cannabinoids

Class 1

Agonist at CB1 (CNS) & CB2 (Immune) GPCRs

Kratom / Mitragynine / 7-hydroxymitragynin & synthetic derivatives

Class 1

Nonselective MOR Partial Agonist

LSD / Lysergic acid diethylamide

Class 1

5HT1/2/5/6, DA2 agonist

Mescaline

Class 1

5HT1/2a agonist

GHB / Gamma-hydroxybutyric acid

Class 1

GABA(B) & GHBR agonist

Psilocybin

Class 1

5HT2a agonist

Nicotine

Class 2

nAChR Full Agonist

Ethanol

(Main MOA)

Class 2

Enhancement of GABA(A) receptor-operated channels

Disulfiram

EtOH Use Disorder Treatment

Aldehyde Dehydrogenase Inhibitor

Acamprosate

EtOH Use Disorder Treatment

GABAergic modulator, NMDA antagonist

Benzodiazepines

Class 2

GABA(A) Allosteric Modulation; Prolongs opening

Ketamine

Class 2

Metabolized to Nor_____, an NMDA antagonist

PCP / Phencyclidine

Class 2

NMDA antagonist, DA+NE+5-HT reuptake inhibitor

Amphetamines

Class 3

Increase Cytosolic DA, Reverse DA Transporter, Inhibits MAO

Cocaine

Class 3

Increase Cytosolic DA, Reverse DA Transporter, Inhibits MAO

MDMA / Ectasy

Class 3

Increases 5-HT, DA, NE Release

Reuptake Inhibitor / Reversal