Chlorpheniramine Potentiates the Analgesic Effect in Migraine of Usual Caffeine, Acetaminophen, and Acetylsalicylic Acid Combination

Abstract

Previous studies indicated that addition of the antihistaminic chlorpheniramine to the usual combination of acetylsalicylic acid, acetaminophen, and caffeine further increases their synergism both in terms of anti-inflammatory and analgesic effect. The present non-interventional study tested the superiority of two Algopirin® tablets, containing a total of 250 mg acetylsalicylic acid (ASA), 150 mg acetaminophen (paracetamol, PAR), 30 mg caffeine (CAF) and 4 mg chlorpheniramine (CLF) vs. a combination containing 250 mg ASA, 250 mg PAR, and 65 mg CAF recognized as “safe and effective” by FDA in treating migraine. Patients evaluated their pain intensity on the Visual Analog Scale—VAS(PI) before and 30, 60, 120, 180, and 240 min after drug intake. Interpretation of the pain curves as “survival pain curves” was considered as a method for direct comparison of the pain curves. This interpretation permitted the application of the log rank test for comparison of pain hazards. The results of the applied parametric and non-parametric statistical tests indicated significant differences between the main endpoints: both Areas Under Pain Curves and time to decrease of the pain intensity to less than 50% of the initial value comparisons highlighted that Algopirin® was more efficient in spite of smaller doses of PAR and CAF. Comparison of “survival of pain” led to the same conclusion concerning the superiority of Algopririn. Consequently, the addition of CLF permitted decreasing of ASA, PAR, and CAF doses as well as their potential side effects, without a loss of analgesic effect.

Antihistamine promotes electroacupuncture analgesia in healthy human subjects: A pilot study

“…Interestingly, in a clinical study, the addition of 4 mg chlorpheniramine effectively potentiated the analgesic effect of antimigraine medication combining acetylsalicylic acid (250 mg), paracetamol (150 mg) and caffeine (30 mg) compared with a tablet containing the usual combination of 250 mg acetylsalicylic acid, 250 mg paracetamol, and 65 mg caffeine. 40 Hence, the efficacy of our results may be due to the synergistic effect between EA and DCPA, rather than DCPA itself.…”

Effect of a New Synergistic Combination of Low Doses of Acetylsalicylic Acid, Caffeine, Acetaminophen, and Chlorpheniramine in Acute Low Back Pain

“…The maximum analgesic effect of ALG in LBP occurred between 1 and 2 h ( Figure 13A ). It is to note that the maximum analgesic effect in LBP appears to be delayed with about half an hour and approximately 10 times lower in intensity than the ALG effect in migraine (Voicu et al, 2017b) ( Figure 13B ). The peak plasma concentrations of ASA and PAR, the main active components of ALG, were reported as 15 min and 30 min (Muir et al, 1997).…”

“…Thus, clinical studies (Blendea et al, 2011; Enache et al, 2012) proved the noninferiority of a unique dose of Algopirin ® (ALG), an authorized combination of the four active containing 125 mg ASA, 75 mg PAR, 15 mg CAF, and 2 mg CLF (Voicu et al, 2016; Voicu et al, 2017a) vs. Excedrin ® , a fixed combination drug containing 250 mg ASA, 250 mg PAR, and 65 mg CAF. The extension study (Voicu et al, 2017b) also proved the superiority of two tablets of ALG vs. one tablet of Excedrin ® , though the doses of active components in the ALG treatment remained lower than in the case of Excedrin ® .…”