DIHYDROCODEINE TARTRATE

Originator

Bicodein,Uquifa

Manufacturing Process

The codein was reduced by hydrogen in the presence catalyst Pt (or Pd, or Ni) and 7,8-dihydrocodein was obtained.
To the 7,8-dihydrocodein tartaric acid was added and mixed, in the result 7,8- dihydrocodein bitartrate was obtained.

Therapeutic Function

Antitussive, Narcotic analgesic

Clinical Use

Analgesia

Drug interactions

Potentially hazardous interactions with other drugs
Angiotensin-II antagonists: concentration increased by telmisartan.
Anti-arrhythmics: concentration increased by amiodarone, dronedarone and propafenone (half maintenance dose of digoxin).
Antidepressants: concentration reduced by St John’s wort - avoid.
Antifungals: increased toxicity if hypokalaemia occurs with amphotericin; concentration increased by itraconazole.
Antimalarials: concentration possibly increased by quinine, hydroxychloroquine and chloroquine; increased risk of bradycardia with mefloquine
Antivirals: concentration increased by daclatasvir.
Calcium-channel blockers: concentration increased by diltiazem, lercanidipine, nicardipine, verapamil and possibly nifedipine; increased risk of AV block and bradycardia with verapamil.
Ciclosporin: concentration increased by ciclosporin.
Colchicine: possibly increased risk of myopathy
Diuretics: increased toxicity if hypokalaemia occurs; concentration increased by spironolactone and possibly potassium canrenoate.
Ticagrelor: concentration of digoxin increased.

Metabolism

Dihydrocodeine is metabolised in the liver via the cytochrome P450 isoenzyme CYP2D6, to dihydromorphine, which has potent analgesic activity, although the analgesic effect of dihydrocodeine appears to be mainly due to the parent compound; some is also converted via CYP3A4 to nordihydrocodeine.
Dihydrocodeine is excreted in urine as unchanged drug and metabolites, including glucuronide conjugates.

Raw materials

Preparation Products