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Tilidine, sold under the brand name Valoron among others, is a synthetic opioid analgesic, used mainly in BelgiumBulgariaGermanyLuxembourgSouth Africa, and Switzerland for the treatment of moderate to severe pain, both acute and chronic.

Its onset of pain relief after oral administration is about 10–15 minutes and peak relief from pain occurs about 25–50 minutes after administration.

Tilidin uses

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Tilidine is used in the form of hydrochloride or phosphate salt. In Germany, tilidine is available in a fixed combination with naloxone for oral administration (Valoron N and generics); the mixture of naloxone is claimed to lower the abuse liability of the opioid analgesic.

This is so that if people take the medication orally (which is the way they are meant to) the opioid blocker, naloxone, has minimal effects on them but if they inject it the naloxone becomes bioavailable and hence antagonises the effects of the tilidine producing withdrawal effects.

In Switzerland the original Valoron brand with only tilidine and no naloxone is also available.

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As well as its use as an analgesic, tilidine is also commonly used in Germany for treatment of restless legs syndrome. The reversed ester is also known and is also a prodrug.

Tilidine is a controlled substance in most countries, listed in the German BtMG, Austrian SMG, and in the USA under the Controlled Substances Act as ACSCN 9750 as a Narcotic under Schedule I, with an annual aggregate manufacturing quota of 10 grams in 2014.

It is used as the hydrochloride (free base conversion ratio 0.882) and HCl hemihydrate (0.858).

Tilidin effects

Its most common adverse effects are transient nausea and vomiting, dizziness, drowsiness, fatigue, headache and nervousness; less commonly, nausea and vomiting (after repeated dosing), hallucinations, confusion, euphoria, tremor, hyperreflexia, clonus and increased sweating.

Uncommonly, somnolence; rarely, diarrhoea and abdominal pain.

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