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Doxylamine is a first generation antihistamine and anticholinergic
Doxylamine is a first generation antihistamine affecting histamine at H1 receptors. In addition, it has powerful anticholinergic effects.
 
 
In addition, doxylamine is a very powerful hypnotic- even outclassing some prescription medicines. It's capable of causing very severe parasomnia with long-term usage.




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=== '''Medical Uses''' ===
=== '''Medical Uses''' ===


 
Doxylamine is used with pyridoxine to prevent morning sickness. It's also used as a sleep aid useful for alleviating short-term insomnia, and is a useful anti-tussive agent.
It is used in the combination drug Pyridoxine/doxylamine to treat nausea and vomiting of pregnancy.
 
As of 2004, doxylamine and diphenhydramine were the agents most commonly used to treat short term insomnia. As of 2008, antihistamines were not recommended by the American Academy of Sleep Medicine for treatment of chronic insomnia "due to the relative lack of efficacy and safety data.".
 




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=== '''Side Effects''' ===
=== '''Side Effects''' ===


Doxylamine succinate is a potent anticholinergic and has a side-effect profile common to such drugs, including dry mouth, ataxia, urinary retention, drowsiness, memory problems, inability to concentrate, hallucinations, psychosis, and a marked increased sensitivity to external stimuli. Like many hypnotics, it should not be combined with other antihistamines,[citation needed] such as cetirizine (Zyrtec) or diphenhydramine (Benadryl), as this combination can increase the risk of serious side effects. Using doxylamine over a long period of time is not recommended. However, the drug is not addictive, and withdrawal effects are unlikely to be experienced with prolonged use.
* Ataxia
 
* Dry mouth
* Urinary Retention
* Short-term Memory Failure
* Inability to Concentrate
* Hallucinations




Revision as of 23:39, 30 March 2017

Doxylamine is a first generation antihistamine affecting histamine at H1 receptors. In addition, it has powerful anticholinergic effects.


Medical Uses

Doxylamine is used with pyridoxine to prevent morning sickness. It's also used as a sleep aid useful for alleviating short-term insomnia, and is a useful anti-tussive agent.


Metabolites

The primary metabolites of doxylamine are-

  • N-desmethyldoxylamine
  • N,N-didesmethyldoxylamine
  • doxylamine N-oxide

Side Effects

  • Ataxia
  • Dry mouth
  • Urinary Retention
  • Short-term Memory Failure
  • Inability to Concentrate
  • Hallucinations


Toxicity

Doxylamine succinate is generally safe for administration to healthy adults. The median lethal dose (LD50) is estimated to be 50–500 mg/kg in humans. Symptoms of overdose may include dry mouth, dilated pupils, insomnia, night terrors, euphoria, hallucinations, seizures, rhabdomyolysis, and death. Fatalities have been reported from doxylamine overdose. These have been characterized by coma, tonic-clonic (or grand mal) seizures and cardiorespiratory arrest. Children appear to be at a high risk for cardiorespiratory arrest. A toxic dose for children of more than 1.8 mg/kg has been reported. A 3-year old child died 18 hours after ingesting 1,000 mg doxylamine succinate. Rarely, an overdose results in rhabdomyolysis and acute renal failure.

Studies of doxylamine's carcinogenicity in mice and rats have produced positive results for both liver and thyroid cancer, especially in the mouse. The carcinogenicity of the drug in humans is not well studied, and the IARC lists the drug as "not classifiable as to its carcinogenicity to humans".


References

https://www.ncbi.nlm.nih.gov/pubmed/1975634

https://toxnet.nlm.nih.gov/cgi-bin/sis/search/a?dbs+hsdb:@term+@DOCNO+5184

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