Drug intelligence / Profile preview

caffeine + codeine + paracetamol

Development stage
Unknown
Lead developer
Taro
Modality
Small Molecules
Administration
Oral
01

Overview

Rokacet is a fixed-dose combination analgesic containing paracetamol (acetaminophen), caffeine, and codeine phosphate. Developed and manufactured by Taro Pharmaceuticals, it is marketed in Israel as an over-the-counter medication for the relief of mild-to-moderate pain (such as headache, migraine, and toothache), cough, and fever accompanied by pain. A stronger prescription-only formulation, Rokacet Plus, is also available. Paracetamol acts as an analgesic and antipyretic by weakly inhibiting cyclooxygenase (COX-1 and COX-2) pathways. Codeine is a centrally acting weak opioid analgesic that is metabolized in the liver by CYP2D6 to morphine, which then acts as an agonist at mu-type opioid receptors to impair pain transmission. Caffeine acts as a central nervous system stimulant and analgesic adjuvant by antagonizing adenosine receptors (primarily A1 and A2a), enhancing the pain-relieving effects of paracetamol. Rokacet has been evaluated in clinical settings, including a pilot trial in Israel as a rescue analgesic for postoperative pain following impacted wisdom tooth extraction.

Brand names
AnalgilasaCodasolveRatio-LenoltecRokacetRokacet PlusSolpadeine MaxSolpadeine PlusTeva-Lenoltec No 3Tylenol No. 1
Other names
acetaminophen + caffeine + codeineacetaminophen + caffeine + codeine phosphatecaffeine + codeine + paracetamolcaffeine + codeine phosphate + paracetamolparacetamol + caffeine + codeineparacetamol + caffeine + codeine phosphate
02

Targets

ADORA1 (Adenosine receptor A1 subtype)ADORA2A (Adenosine A₂A Receptor)ADORA2B (Adenosine A2B receptor)ADORA3 (Adenosine A3 receptor)DOR (Opioid Receptor Delta 1)KOR (Kappa opioid receptor)MOR (Mu opioid receptor)PGHS-1 (Prostaglandin G/H Synthase 1)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)

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