How Do Opioid Agonists Work?

How do opioid agonists work?

Opioid agonists are medications used for the short-term management of moderate-to-severe acute pain. Opioid agonists relieve pain by stimulating opioid receptors. Opioid receptors are protein molecules on nerve cell (neuron) membranes in the central and peripheral nervous systems.

Opioid receptors mediate the body’s response to most hormones and some of their functions include modulating pain, stress response, respiration, mood, and emotion. Opioid agonists stimulate mu-opioid receptors, one of the five types of opioid receptors in the human body.

Opioid agonists work by binding to mu-opioid receptors and inhibiting the release of chemicals (neurotransmitters) that transmit pain signals between the neurons.

How are opioid agonists used?

Opioid agonists are administered as intravenous (IV) injections, only in hospitals or health care facilities. Opioid agonists are used to treating moderate-to-severe acute pain that is severe enough to require IV opioids when alternative treatments are inadequate.

What are side effects of opioid agonists?

Side effects of opioid agonists may include the following:

  • Nausea
  • Vomiting
  • Dizziness
  • Hypoxia (inadequate oxygen in tissues)
  • Somnolence (drowsiness)
  • Pruritus (itching)
  • Constipation
  • Sedation
  • Back pain
  • Decreased oxygen saturation in the blood

Information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with other medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.

What are names of some opioid agonist drugs?

Generic and brand names of opioid agonist drugs include:


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