Ibudilast
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| Trade names | Ketas, Pinatos, Eyevinal |
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By mouth (capsules), topical (ophthalmic solution) |
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| ECHA InfoCard | 100.164.881 |
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| Formula | C14H18N2O |
| Molar mass | 230.31 g/mol |
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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, but also showing significant inhibition of other PDE subtypes.
Ibudilast has bronchodilator, vasodilator and neuroprotective effects, and is mainly used in the treatment of asthma and stroke. It inhibits platelet aggregation, and may also be useful in the treatment of multiple sclerosis.
Ibudilast crosses the blood–brain barrier and suppresses 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.
It may have some use reducing methamphetamine and alcohol addiction.
Ibudilast is listed as being an antagonist at the toll-like receptor 4 (TLR4) This likely play an immense part in its effect, specifically its synergy with opioid drugs, its anti-inflammatory effect, and its own painkilling effect. It is unknown if the PDE4-inhibiting properties potentiate the effects of TLR4 inactivation and/or vice versa, despite that some of their effects are shared, such as inflammation reducing properties.
TLR4 antagonists theoretically reverse the increase in pain and inflammation caused by most TLR4 agonists, which include many opiate and opioid drugs.
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Wikipedia