Doxylamine

Doxylamine Brand Names- Aldex AN | Doxytex | Unisom

What is Doxylamine

Doxylamine an H₁-receptor antagonist of the ethanolamine class, is primarily used as an OTC sedative in the short-term management of insomnia.

It was originally introduced in 1948 as a treatment for anaphylaxis and allergies and is still used alone and in combination with antitussives and decongestants for the temporary relief of cold and allergy symptoms.

Doxylamine, in combination with pyridoxine and dicyclomine, became available in 1956 for the treatment of nausea and vomiting during pregnancy. Dicyclomine was removed from the product in 1976 due to lack of efficacy as an antiemetic.

Doxylamine in combination with pyridoxine continued to be available under the brand name Bendectin until 1983 when litigation over possible teratogenetic effects resulted in its voluntary withdrawal by the manufacturer; however, the data regarding doxylamine do not support evidence of teratogenesis, either alone or in combination with pyridoxine.

The doxylamine-pyridoxine product is still available in Canada as Diclectin for use as an antiemetic during pregnancy.

Other common members of the ethanolamine class of antihistamines include carbinoxamine, clemastine, dimenhydrinate (a salt of diphenhydramine), and diphenhydramine.

Ethanolamine antihistamines are generally considered by many clinicians to be as effective in treating allergic rhinitis as newer antihistamines; however, their often significant CNS depressant effects limit their popularity for this purpose. In contrast, their pronounced sedative effects are very beneficial in the short-term treatment of insomnia.

Doxylamine was initially marketed for use before 1962, which is when Congress passed the amended Federal Food, Drug, and Cosmetic Act requiring that the FDA establish both safety and efficacy for all subsequently approved drugs.

Doxylamine products for the treatment of allergic rhinitis have not been formally evaluated by the FDA and are unapproved as marketed.

Doxylamine was FDA approved for the treatment of insomnia in October 1978.

Indications

• allergic rhinitis
• insomnia

For the short-term treatment of insomnia (less than 2 weeks)

Side Effects

1. abdominal pain
2. agitation
3. appetite stimulation
4. asthenia
5. ataxia
6. blurred vision
7. bradycardia
8. confusion
9. constipation
10. delirium
11. diarrhea
12. diplopia
13. dizziness
14. drowsiness
15. dyskinesia
16. dystonic reaction
17. fatigue
18. hallucinations
19. headache
20. hypotension
21. impaired cognition
22. insomnia
23. irritability
24. lethargy
25. myasthenia
26. mydriasis
27. palpitations
28. photosensitivity
29. restlessness
30. seizures
31. sinus tachycardia
32. tremor
33. urinary retention
34. weakness
35. xerophthalmia
36. xerostomia

Monitoring Parameters

• laboratory monitoring not necessary

Contraindications

• anticholinergic medications
• asthma
• bladder obstruction
• breast-feeding
• cardiac disease
• children
• chronic obstructive pulmonary disease (COPD)
• closed-angle glaucoma
• contact lenses
• driving or operating machinery
• geriatric
• GI obstruction
• hepatic disease
• ileus
• infants
• neonates
• peptic ulcer disease
• pregnancy
• prostatic hypertrophy
• pyloric stenosis
• urinary retention

Interactions

• Acetaminophen; Butalbital
• Acetaminophen; Butalbital; Caffeine
• Acetaminophen; Butalbital; Caffeine; Codeine
• Acetaminophen; Caffeine; Dihydrocodeine
• Acetaminophen; Codeine
• Acetaminophen; Dichloralphenazone; Isometheptene
• Acetaminophen; Hydrocodone
• Acetaminophen; Oxycodone
• Acetaminophen; Pentazocine
• Acetaminophen; Propoxyphene
• Acetaminophen; Tramadol
• Aldesleukin, IL-2
• Alfentanil
• Alosetron
• Amantadine
• Ambenonium Chloride
• Amobarbital
• Amoxapine
• Amphetamine
• Amphetamine; Dextroamphetamine
• Amphetamine; Dextroamphetamine Salts
• Anticholinergics
• Apomorphine
• Apraclonidine
• Aripiprazole
• Asenapine
• Aspirin, ASA; Butalbital; Caffeine
• Aspirin, ASA; Butalbital; Caffeine; Codeine
• Aspirin, ASA; Caffeine; Dihydrocodeine
• Aspirin, ASA; Caffeine; Orphenadrine
• Aspirin, ASA; Carisoprodol
• Aspirin, ASA; Carisoprodol; Codeine
• Aspirin, ASA; Oxycodone
• Atropine; Difenoxin
• Atropine; Diphenoxylate
• Atropine; Hyoscyamine; Phenobarbital; Scopolamine
• Azelastine
• Azelastine; Fluticasone
• Baclofen
• Barbiturates
• Belladonna Alkaloids; Ergotamine; Phenobarbital
• Belladonna; Opium
• Benzhydrocodone; Acetaminophen
• Benzodiazepines
• Benzphetamine
• Brompheniramine; Carbetapentane; Phenylephrine
• Brompheniramine; Guaifenesin; Hydrocodone
• Brompheniramine; Hydrocodone; Pseudoephedrine
• Buprenorphine
• Buprenorphine; Naloxone
• Buspirone
• Butabarbital
• Butorphanol
• Cannabidiol
• Capsaicin; Metaxalone
• Carbetapentane; Chlorpheniramine
• Carbetapentane; Chlorpheniramine; Phenylephrine
• Carbetapentane; Diphenhydramine; Phenylephrine
• Carbetapentane; Guaifenesin
• Carbetapentane; Guaifenesin; Phenylephrine
• Carbetapentane; Phenylephrine
• Carbetapentane; Phenylephrine; Pyrilamine
• Carbetapentane; Pseudoephedrine
• Carbetapentane; Pyrilamine
• Carbidopa; Levodopa; Entacapone
• Carbinoxamine; Hydrocodone; Phenylephrine
• Carbinoxamine; Hydrocodone; Pseudoephedrine
• Cariprazine
• Carisoprodol
• Cenobamate
• Cetirizine
• Cetirizine; Pseudoephedrine
• Chlorpheniramine; Codeine
• Chlorpheniramine; Dihydrocodeine; Phenylephrine
• Chlorpheniramine; Dihydrocodeine; Pseudoephedrine
• Chlorpheniramine; Guaifenesin; Hydrocodone; Pseudoephedrine
• Chlorpheniramine; Hydrocodone
• Chlorpheniramine; Hydrocodone; Phenylephrine
• Chlorpheniramine; Hydrocodone; Pseudoephedrine
• Chlorpromazine
• Chlorzoxazone
• Clobazam
• Clozapine
• Codeine
• Codeine; Guaifenesin
• Codeine; Phenylephrine; Promethazine
• Codeine; Promethazine
• COMT inhibitors
• Cyclobenzaprine
• Dantrolene
• Daratumumab; Hyaluronidase
• Desloratadine
• Desloratadine; Pseudoephedrine
• Deutetrabenazine
• Dexmedetomidine
• Dextroamphetamine
• Dextromethorphan; Promethazine
• Dihydrocodeine; Guaifenesin; Pseudoephedrine
• Diphenhydramine; Hydrocodone; Phenylephrine
• Disopyramide
• Donepezil
• Donepezil; Memantine
• Dronabinol
• Droperidol
• Entacapone
• Esketamine
• Eszopiclone
• Ethanol
• Etomidate
• Ezogabine
• Fenfluramine
• Fentanyl
• Flibanserin
• Fluoxetine; Olanzapine
• Fluphenazine
• Fospropofol
• Gabapentin
• Galantamine
• Guaifenesin; Hydrocodone
• Guaifenesin; Hydrocodone; Pseudoephedrine
• Halogenated Anesthetics
• Haloperidol
• Heparin
• Homatropine; Hydrocodone
• Hyaluronidase
• Hyaluronidase, Recombinant; Immune Globulin
• Hydantoins
• Hydrocodone
• Hydrocodone; Ibuprofen
• Hydrocodone; Phenylephrine
• Hydrocodone; Potassium Guaiacolsulfonate
• Hydrocodone; Potassium Guaiacolsulfonate; Pseudoephedrine
• Hydrocodone; Pseudoephedrine
• Hydromorphone
• Ibuprofen; Oxycodone
• Iloperidone
• Isocarboxazid
• Ketamine
• Lasmiditan
• Lemborexant
• Levocetirizine
• Levomethadyl
• Levorphanol
• Lithium
• Lofexidine
• Loratadine
• Loratadine; Pseudoephedrine
• Loxapine
• Lumateperone
• Lurasidone
• Magnesium Salts
• Maprotiline
• Meclizine
• Melatonin
• Meperidine
• Meperidine; Promethazine
• Mephobarbital
• Meprobamate
• Metaxalone
• Methadone
• Methamphetamine
• Methocarbamol
• Methohexital
• Metoclopramide
• Metyrapone
• Metyrosine
• Minocycline
• Mirtazapine
• Mitotane
• Molindone
• Monoamine oxidase inhibitors
• Morphine
• Morphine; Naltrexone
• Nabilone
• Nalbuphine
• Nefazodone
• Olanzapine
• Opiate Agonists
• Orphenadrine
• Oxycodone
• Oxymorphone
• Paliperidone
• Papaverine
• Paroxetine
• Pentazocine
• Pentazocine; Naloxone
• Pentobarbital
• Perampanel
• Perphenazine
• Perphenazine; Amitriptyline
• Phenelzine
• Phenobarbital
• Phentermine; Topiramate
• Phenylephrine; Promethazine
• Pimozide
• Pitolisant
• Pramipexole
• Pregabalin
• Primidone
• Procarbazine
• Prochlorperazine
• Promethazine
• Propofol
• Propoxyphene
• Quetiapine
• Ramelteon
• Rasagiline
• Remifentanil
• Risperidone
• Rituximab; Hyaluronidase
• Rivastigmine
• Ropinirole
• Rotigotine
• Safinamide
• Secobarbital
• Selegiline
• Sincalide
• Sodium Iodide
• Sodium Oxybate
• Solifenacin
• Sufentanil
• Suvorexant
• Tacrine
• Tapentadol
• Tasimelteon
• Tetrabenazine
• Thalidomide
• Thiopental
• Thioridazine
• Thiothixene
• Tizanidine
• Tolcapone
• Topiramate
• Tramadol
• Tranylcypromine
• Trastuzumab; Hyaluronidase
• Trazodone
• Tricyclic antidepressants
• Trifluoperazine
• Trimethobenzamide
• Trospium
• Vigabatrin
• Vilazodone
• Zaleplon
• Ziconotide
• Ziprasidone
• Zolpidem