Proglumide

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Proglumide
Proglumide.svg
Systematic (IUPAC) name
4-benzamido-5-(dipropylamino)-5-oxopentanoic acid
Clinical data
AHFS/Drugs.com International Drug Names
Legal status
  • ℞ (Prescription only)
Routes of
administration		 Oral
Pharmacokinetic data
Biological half-life ~24 hours
Identifiers
CAS Number 6620-60-6 YesY
ATC code A02BX06 (WHO)
PubChem CID: 4922
IUPHAR/BPS 893
ChemSpider 4753
UNII EPL8W5565D N
ChEBI CHEBI:32058 N
ChEMBL CHEMBL316561 N
Synonyms (RS)-N2-benzoyl-N,N-dipropyl-α-glutamine
Chemical data
Formula C18H26N2O4
Molecular mass 334.41 g/mol
  • O=C(NC(CCC(O)=O)C(N(CCC)CCC)=O)C1=CC=CC=C1
  • InChI=1S/C18H26N2O4/c1-3-12-20(13-4-2)18(24)15(10-11-16(21)22)19-17(23)14-8-6-5-7-9-14/h5-9,15H,3-4,10-13H2,1-2H3,(H,19,23)(H,21,22)
  • Key:DGMKFQYCZXERLX-UHFFFAOYSA-N
 NYesY (what is this?)  (verify)

Proglumide (Milid) is a drug that inhibits gastrointestinal motility and reduces gastric secretions. It acts as a cholecystokinin antagonist,[1] which blocks both the CCKA and CCKB subtypes.[2] It was used mainly in the treatment of stomach ulcers,[3][4] although it has now been largely replaced by newer drugs for this application.

An interesting side effect of proglumide is that it enhances the analgesia produced by opioid drugs,[5] and can prevent or even reverse the development of tolerance to opioid drugs.[6][7] This can make it a useful adjuvant treatment to use alongside opioid drugs in the treatment of chronic pain conditions such as cancer, where opioid analgesics may be required for long periods and development of tolerance reduces clinical efficacy of these drugs.[8][9]

Proglumide has also been shown to act as a δ-opioid agonist, which may contribute to its analgesic effects.[10]

Proglumide also works as a placebo effect amplifier for pain conditions. When injected visibly to a subject, its analgesic effect is bigger than a similarly administered placebo. When injected secretly, it does not have any effect, whereas standard pain drugs have an effect, even if they are administered without the subject's awareness.[11] The supposed mechanism is an enhancement of the neural pathways of expectation as a result of dopamine and endogenous opioids being suddenly released throughout numerous structures of the brain and spinal cord.

The ventral tegmental area is the structure believed to mediate proglumides analgesic and euphoric effects, however dozens of areas with a wide range of physical and psychological functions are implicated in the mediation of the placebo effect (this accounts for proglumides ability to produce physically measurable effects on vital signs such as heart rate, blood pressure, respiration rate, and tidal volume which can not be accounted for by its clinically insignificant δ-opioid affinity.

See also

References

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  1. REDIRECT Template:Peptide receptor modulators
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