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Doxylamine succinate is one of the many sedating antihistamines used by itself as a short-term sedative, in combination with other drugs as a night-time cold and allergy relief drug, in combination with the analgesics paracetamol and codeine as an analgesic / calmative preparation, and is prescribed in combination with vitamin B6 (pyridoxine) to prevent morning sickness in pregnant women.


Doxylamine is a member of the ethanolamine class of antihistamines and has anti-allergy power superior to almost every other antihistamine on the market, with the exception of diphenhydramine (Benadryl). It is also the most effective over-the-counter sedative available in the United Statesmarker, and is more sedating than some prescription hypnotics. One study found that doxylamine succinate is possibly more effective than the barbiturate phenobarbital for use as a sedative. For this reason, doxylamine has sometimes been used off label in a manner similar to diphenhydramine for the reduction of anxiety symptoms.

The dosage required to induce hypnosis (sleep) can be as low as 6.25 mg, but is usually effective in dosages of up to 25 mg. Higher doses are not recommended by the United States Food and Drug Administration, although single dosage recommendations of up to 50 mg are common in some countries, including Australia, where it is marketed under the names Restavit and Dozile.


The two main metabolites are desmethyldoxylamine and didesmethyldoxylamine.


Side effects

Doxylamine succinate is a potent anticholinergic and has a side-effect profile common to such drugs, including dry mouth, ataxia, urinary retention, and drowsiness.


Doxylamine succinate is generally safe for administration to healthy adults. Typical preparations that contain doxylamine range from 6.25 mg to 25.0 mg. The LD50 is estimated to be 50–500 mg/kg in humans. Symptoms of overdose may include dry mouth, dilated pupils, insomnia, euphoria, hallucinations, seizures, rhabdomyolysis, and death. Fatalities, while rare, have been recorded. Rarely, an overdose results in rhabdomyolysis and acute renal failure.


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