Phenyltoloxamine has analgesic and anti-spasmodic properties of its own and is used in combination with paracetamol, aspirin and other salicylates and other drugs in proprietary preparations available over the counter for backache, muscle strains and similar conditions. In this respect, it is similar to a closely related antihistamine, orphenadrine, and both drugs are very closely related to diphenhydramine and to doxylamine, the latter of which is the active ingredient in NyQuil and many other cough preparations.
Phenyltoloxamine, like diphenhydramine and doxylamine, is an effective non-narcotic anti-tussive on its own but tends to be effective only for productive coughs as the anticholinergic action will exacerbate dry, unproductive coughs, so it is often combined with dextromethorphan, codeine, ethylmorphine, dihydrocodeine, or hydrocodone in cough suppressants both over the counter and prescription.
It is also used to discourage abuse in certain opiate analgesics due its unpleasant side effects at high doses. While therapeutic doses of phenyltoloxamine can generate mild to moderate euphoria as can many of its close chemical relatives, much higher doses have a side effect profile similar to that of atropine, which is also used in this fashion for tablets of diphenoxylate and morphine for oral administration.
Phenyltoloxamine is available in most countries, though it is rare in several western countries it remains widely used around the world, particularly in the developing world.
In the past it was not a controlled substance. It is no longer available OTC in the US. Some preparations contain opiates such as codeine or hydrocodone and are controlled. When used in preparations with acetaminophen it is generally over the counter.
Phenyltoloxamine combinations are sold under wide variety of preparations, brand names and dosages around the world:
Aceta-Gesic, Ed-Flex, Dologesic, Duraxin, Flextra-650, Novagesic, Pain-gesic, Phenylgesic - North America