rocaine Hydrochloride (CAS: 51-05-8) is the hydrochloride salt form of procaine, a benzoic acid derivative with local anesthetic and antiarrhythmic properties. Procaine binds to and inhibits voltage-gated sodium channels, thereby inhibiting the ionic flux required for the initiation and conduction of impulses. In addition, this agent increases electrical excitation threshold, reduces rate of rise of action potential and slows nerve impulse propagation thereby causing loss of sensation [1]. A local anesthetic of the ester type that has a slow onset and a short duration of action. It is mainly used for infiltration anesthesia, peripheral nerve block, and spinal block. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1016). Procaine has also been investigated as an oral entry inhibitor in treatment-experienced HIV patients [2].

Several analgesics are in use for pain control in patients with acute pancreatitis. Procaine hydrochloride (procaine) has a long tradition and is recommended by the German Society of Gastroenterology and Metabolic Diseases for pain treatment in patients with acute pancreatitis. There is no controlled trial showing that procaine could be effective for pain treatment. In an open, randomized, controlled trial, 107 patients (76 male, 31 female; mean age 45±12 years) were included and randomized either to receive procaine (n = 55) or pentazocine (n = 52) for pain relief. Procaine 2g/24 h was administered by continuous intravenous infusion, pentazocine 30 mg was administered every 6h as a bolus intravenous injection. Pentazocine was additionally administered on demand whenever required in patients of both treatment groups and its total consumption was recorded. Pain scores were assessed twice daily on a visual analogue scale. Patients receiving procaine were significantly more likely to request additional analgesics compared to patients treated with pentazocine alone, 98 vs. 44%, respectively (p < 0.001). Procaine did not reduce the amount of pentazocine required for pain control. The amount of pentazocine given in both groups was not statistically significantly different. Recorded pain scores were significantly lower (p < 0.001) in patients in the pentazocine group during the first 3 days of analgesic treatment. From day 4 on there was no significant difference in pain scores among the two groups.

In conclusion, intravenous application of procaine is ineffective for pain control in patients with acute pancreatitis. Side effects during procaine treatment were not observed but in the absence of a clinical benefit it should be removed from the guidelines as analgesic medication in acute pancreatitis. There is a need of studies to optimize analgesic therapy in acute pancreatitis [3].

Reference

[1] https://pubchem.ncbi.nlm.nih.gov/compound/Procaine-hydrochloride
[2] https://www.drugbank.ca/salts/DBSALT000551
[3] Kahl, S., S. Zimmermann, M. Pross, H. U. Schulz, U. Schmidt and P. Malfertheiner (2004). "Procaine Hydrochloride Fails to Relieve Pain in Patients with Acute Pancreatitis." Digestion 69(1): 5-9.