Opioid Receptor Antagonist

An opioid receptor antagonist is a drug that blocks the receptors the body's own opioids act on. Naloxone, nalmefene and naltrexone all work this way. Blocking the receptor lifts a brake those opioids hold on other systems.

One of those brakes reaches the hormones that run the cycle. An infusion of naloxone in the luteal phase made luteinizing hormone pulses faster and stronger.1 The body's own opioids hold those pulses back. In obese women with PCOS, now also named PMOS (Polyendocrine Metabolic Ovarian Syndrome), opioid blockade lowered the insulin response.2 Those women also had a skin sign of insulin resistance.

Low-dose naltrexone is a separate story. Its calming effect on inflammation appears to run through glial cells in the brain, not through opioid receptors. That use stays experimental.3

Cited in this entry

  1. Ropert JF, Quigley ME, Yen SS. Endogenous opiates modulate pulsatile luteinizing hormone release in humans. The Journal of Clinical Endocrinology and Metabolism. 1981. The Journal of Clinical Endocrinology and Metabolism. https://pubmed.ncbi.nlm.nih.gov/6780598/
  2. Givens JR, Kurtz BR, Kitabchi AE, Bittle JB, Karas JG, Mitchell JA, Howes JF. Reduction of hyperinsulinemia and insulin resistance by opiate receptor blockade in the polycystic ovary syndrome with acanthosis nigricans. The Journal of Clinical Endocrinology and Metabolism. 1987. The Journal of Clinical Endocrinology and Metabolism. https://pubmed.ncbi.nlm.nih.gov/3539980/
  3. Younger J, Parkitny L, McLain D. The use of low-dose naltrexone (LDN) as a novel anti-inflammatory treatment for chronic pain. Clinical Rheumatology. 2014. Clinical Rheumatology. https://doi.org/10.1007/s10067-014-2517-2

This content is for educational purposes only and does not constitute medical advice. Consult an RRM clinician or healthcare provider for guidance specific to your situation.