Propentofylline as a glia modulator
This glia modulator, Propentofylline, is the new kid on the block for the treatment of intractable neuropathic pain. Gliopathic pain is perhaps a better term for this pain, as the winding up phenomena is very much driven by activated glia. The search for glia modulators therefore is quite exciting. We work in our clinic with a number of glia modulators in treatment refractory neuropathic pain and sometimes with amazing results.
Propentofylline is a methylxanthine derivate with a wide spectrum of physiological actions, acting via cyclic AMP, phosphodiesterase, and adenosine receptors.
A number of in vitro and in vivo studies have demonstrated neuroprotective, anti pro liferative, and anti-inflammatory effects of propentofylline. It has shown efficacy in preclinical models of stroke, opioid tolerance, and acute and chronic pain.
Dementia, Schizophrenia and MS
Propentofylline also has been evaluated in dementia, and is by some seen as a potential adjuvant treatment for schizophrenia and multiple Scleroses.
However, one of the more exiting indications is neuropathic or gliopathic pain, as its mechanisms of action include a direct glia modulation to decrease astrocyte /glia reactivity, and modulating the release of pro inflammatory factors, as well as enhancement of astrocyte mediated glutamate clearance.
The authors of the chapter referred to here reviewed the literature that supports many protective actions of this molecule, and they suggest propentofylline as a potential therapeutic for the treatment of chronic pain.
- from these studies, we propose a CNS multi partite synaptic action of propentofylline that includes modulation of pre- and postsynaptic neurons, astrocytes, and microglia in the treatment of chronic pain syndromes, including, but not limited to, neuropathic pain.
Anti allodynic effect of propentofylline
To examine the neuroprotective effects op propentofylline, in an experimental animal model propentofylline was given intrathecally or systemically prior to nerve trans section. Compared to controls mechanical allodynia was less in the propentofylline groups.
Microglial and astrocytic activation was decreased in both propentofylline groups. Daily administration of propentofylline produced an approximately 50% reduction in astrocytic and microglial reactive changes. Similar findings were seen in a neuropathic pain model due to chemotherapy.
November 2010, Jan M. Keppel Hesselink, MD, PhD and David J. Kopsky, MD
‘Propentofylline, a glia modulator’
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 Sweitzer S, De Leo J. | Propentofylline: glial modulation, neuroprotection, and alleviation of chronic pain. | Handb Exp Pharmacol. | 2011;(200):235-50.
 Sweitzer SM, Schubert P, DeLeo JA. | Propentofylline, a glial modulating agent, exhibits antiallodynic properties in a rat model of neuropathic pain. | J Pharmacol Exp Ther. | 2001 Jun;297(3):1210-7.
 Sweitzer SM, Pahl JL, DeLeo JA. | Propentofylline attenuates vincristine-induced peripheral neuropathy in the rat. | Neurosci Lett. | 2006 Jun 12;400(3):258-61. Epub 2006 Mar 13.