Which neourotransmitter does methadone affect and how does the drug alter neurotransmission?

Essentials of Pharmacology for Health Professions
7th Edition
ISBN:9781305441620
Author:WOODROW
Publisher:WOODROW
Chapter27: Drugs And Older Adults
Section: Chapter Questions
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Which neourotransmitter does methadone affect and how does the drug alter neurotransmission?

Expert Solution
Step 1

Methadone is also known by it's brand names Dolophine and methadose.Route of administration of methadone drug is by mouth,intravenous insufflation , sublingual and rectal.It has rapid onset of action.Side effects include dizziness, sleeping,vomiting and sweating.

Step 2

Before understanding the mechanism of actions of methadone,we must understand how opioids work in our body.

Opioids have two inhibitory action.They act on;

  • Presynaptic nerve terminal
  • At postsynaptic neuron

Opioids block μ (mu) receptors,and hence prevents the secretion of γ-aminobutyric acid (GABA) which acts on dopaminergic neurons by and inhibits the dopamine release.This inhibition of opioids on GABA leads to increased release of dopaminergic neurons and thus increase in release of dopamine is responsible for addiction in opioids.

Step 3

So here comes the role of methadone drug which is commonly used in rehabilitation of people who are addicted with opioids drugs.

Methadone acts on the full  µ-opioid receptor (MOR) agonist and N-methyl-d-aspartate(NMDA) receptor Antagonist.

N-methyl -D-aspartate(NMDA) is an amino acid derivative which acts on NMDA receptor and mimic the action of glutamate.

Hence methadone acts as an antagonist against glutamate.Glutamate is main excitatory neurotransmitters of central nervous system.

Hence methadone affects glutamate neurotransmitter.

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