), or tilidate
) (Valoron, Valtran, Tilidin) is a synthetic opioid
analgesic, used for treatment of moderate to severe pain, both acute and chronic. Considered a low- to medium-potency opioid, it has the oral potency of about 0.2, i.e., a dose of 100 mg p.o. is equianalgesic to approximately 20 mg morphine
sulfate orally. It is administered orally (by mouth), rectally (by a suppository
), or by injection
(s.c., i.m. or slowly i.v.) with single doses of 50 to 100 mg, the maximal daily dose being up to 600 mg.
Tilidine itself is only a weak opioid, but is rapidly metabolised in the liver and gut to its active metabolites nortilidine
, which are fairly potent, µ
It is manufactured by a Diels-Alder
reaction of 1-N,N-dimethylaminobuta-1,3-diene with ethyl atropate, yielding a mixture of isomers
, of which only the (E)-(trans
)-isomer is active and is separated subsequently from the mixture by precipitation
of the inactive (Z)-(cis
)-isomer as zinc complex
Tilidine is used in the form of hydrochloride
In Germany, tilidine is available in a fixed combination with naloxone
for oral administration (Valoron N and generics); the admixture of naloxone is claimed to lower the abuse
liability of the opioid analgesic.
Authorities in Germany have recently reported increased cases of Tilidine abuse. It remains unclear if this is empirically true.