Ibudilast

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Ibudilast
Clinical data
Trade namesKetas, Pinatos, Eyevinal
AHFS/Drugs.comInternational Drug Names
Routes of
administration		By mouth (capsules),
topical (ophthalmic solution)
ATC code
Legal status
Legal status
Identifiers
  • 2-Methyl-1-(2-propan-2-ylpyrazolo[1,5-a]pyridin-3-yl)propan-1-one
JSmol)
  • CC(C)C(=O)c1c(nn2ccccc12)C(C)C
  • InChI=1S/C14H18N2O/c1-9(2)13-12(14(17)10(3)4)11-7-5-6-8-16(11)15-13/h5-10H,1-4H3 ☒N
  • Key:ZJVFLBOZORBYFE-UHFFFAOYSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

Ibudilast (development codes: AV-411 or MN-166) is an anti-inflammatory drug used mainly in Japan, which acts as a phosphodiesterase inhibitor, inhibiting the PDE4 subtype to the greatest extent,[1] but also showing significant inhibition of other PDE subtypes.[2][3]

Medical uses

In Japan, ibudilast oral capsules are approved for the treatment of asthma, and for improvement of dizziness secondary to chronic cerebral circulation impairment associated with sequelae of cerebral infarction.[4] Ibudilast ophthalmic solution is indicated for the treatment of allergic conjunctivitis and hay fever.[5]

It may have some use reducing methamphetamine,[6][7] opioid,[8] and alcohol[9] addiction.

Pharmacology

Ibudilast has

vasodilator[10] and neuroprotective effects,[11][12] and is mainly used in the treatment of asthma and stroke.[13] It inhibits platelet aggregation,[14] and may also be useful in the treatment of multiple sclerosis.[15]

Ibudilast crosses the

glial cell activation. This activity has been shown to make ibudilast useful in the treatment of neuropathic pain and it not only enhances analgesia produced by opioid drugs, but also reduces the development of tolerance.[16]

Pharmacodynamics

Ibudilast is principally a PDE4 inhibitor but has also been shown to act as an

potentiate the effects of TLR4 inactivation and/or vice versa, despite that some of their effects are shared, such as inflammation reducing properties.[19] TLR4 antagonists theoretically reverse the increase in pain and inflammation caused by most TLR4 agonists, which includes alcohol & many opiate or opioid drugs.[20]

References

  1. PMID 16313925
    .
  2. S2CID 7910607
    .
  3. PMID 16674936
    .
  4. ^ "Ketas (ibudilast) Capsules 10 mg. Prescribing Information" (PDF). Kyorin Pharmaceutical Co., Ltd. Archived from the original (PDF) on 30 August 2018. Retrieved 3 October 2016.
  5. ^ "Ketas (ibudilast) Eye Drops 0.01% Kisuri-no-Shiori (Drug Information Sheet)". Senju Pharmaceutical Co., Ltd. Retrieved 3 October 2016.
  6. ^ "Cure for Meth Addiction?". HuffPost. 2013-04-03.
  7. PMID 34913274
    .
  8. PMID 25975386
    .
  9. PMID 24215262
    .
  10. PMID 11607039
    .
  11. S2CID 29284554
    .
  12. PMID 12030794
    .
  13. S2CID 24917936
    .
  14. PMID 11369417
    .
  15. S2CID 34072005
    .
  16. S2CID 22321634
    .
  17. PMID 22776604
    .
  18. PMID 19679181
    .
  19. PMID 22735051
    .
  20. PMID 19607972
    .
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