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Tuesday, March 26, 2013
Stellate Ganglion Block as an Early Intervention in Sympathetically Maintained Headache and Orofacial Pain Caused by Temporal Arteritis
Pain Medicine
Article first published online: 17 JAN 2013
DOI: 10.1111/pme.12040
Introduction.
We report a case of temporal arteritis with a sympathetic component in the orofacial region, which responded to stellate ganglion blocks (SGBs).
Case.
An 81-year-old woman with limited mouth opening and pain upon chewing was referred to the Orofacial Pain Clinic at Nihon University Dental Hospital. The patient also presented with blurred vision and a burning sensation on the right side of her face. On clinical examination, the temporal artery was tender to palpation, and there was increased sensitivity in the temporal region bilaterally. The patient reported jaw pain and limited mouth opening. Laboratory examination showed elevations in erythrocyte sedimentation rate and C-reactive protein. The burning sensation was due to a sympathetic component, and SGBs substantially reduced both the burning sensation and right temporal pain. Blocking the sympathetic chain on the ipsilateral side also improved jaw movement. The patient was referred to a rheumatologist, after which she was admitted to hospital with a tentative diagnosis of temporal arteritis. Treatment with oral prednisone 30 mg daily was initiated, and the dose was tapered as her symptoms resolved.
Discussion.
The reason for the gradual pain relief after SGB is unclear, but we believe it was effective for ischemia in temporal arteritis because it led to dilation of affected arteries or suppression of inflammation/edema of the vascular wall.
Conclusion.
This case demonstrates that SGB may relieve pain related to temporal arteritis and sympathetically maintained headache and orofacial pain by reducing noxious stimulation peripherally and decreasing central pain transmission centrally.
Small Molecule Angiotensin II Type 2 Receptor (AT2R) Antagonists as Novel Analgesics for Neuropathic Pain: Comparative Pharmacokinetics, Radioligand Binding, and Efficacy in Rats
Pain Medicine
Article first published online: 14 MAR 2013
DOI: 10.1111/pme.12063
Abstract
Objective
Neuropathic pain is an area of unmet clinical need. The objective of this study was to define the pharmacokinetics, oral bioavailability, and efficacy in rats of small molecule antagonists of the angiotensin II type 2 receptor (AT2R) for the relief of neuropathic pain.
Design and Methods.
Adult male Sprague-Dawley (SD) rats received single intravenous (1–10 mg/kg) or oral (5–10 mg/kg) bolus doses of EMA200, EMA300, EMA400 or EMA401 (S-enantiomer of EMA400). Blood samples were collected immediately pre-dose and at specified times over a 12- to 24-hour post-dosing period. Liquid chromatography tandem mass spectrometry was used to measure plasma drug concentrations. Efficacy was assessed in adult male SD rats with a unilateral chronic constriction injury (CCI) of the sciatic nerve.
Results.
After intravenous administration in rats, mean (±standard error of the mean) plasma clearance for EMA200, EMA300, EMA400, and EMA401 was 9.3, 6.1, 0.7, and 1.1 L/hour/kg, respectively. After oral dosing, the dose-normalized systemic exposures of EMA400 and EMA401 were 20- to 30-fold and 50- to 60-fold higher than that for EMA300 and EMA200, respectively. The oral bioavailability of EMA400 and EMA401 was similar at ∼30%, whereas it was only 5.9% and 7.1% for EMA200 and EMA300, respectively. In CCI rats, single intraperitoneal bolus doses of EMA200, EMA300, and EMA400 evoked dose-dependent pain relief. The pain relief potency rank order in CCI rats was EMA400 > EMA300 > EMA200 in agreement with the dose-normalized systemic exposure rank order in SD rats.
Conclusion.
The small molecule AT2R antagonist, EMA401, is in clinical development as a novel analgesic for the relief of neuropathic pain.
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