Melatonin (5-methoxy-N-acetyltryptamine)

What is Melatonin

Melatonin (5-methoxy-N-acetyltryptamine) is a neurohormone used to regulate circadian rhythm disruption which occurs in jet lag and sleep disorders such as delayed sleep phase syndrome, irregular sleep-wake disorder, shift-work sleep disorder, and non-24-hour sleep wake disorder in adults.

Melatonin appears to provide some benefit and few risks for the short-term treatment of sleep irregularities in pediatric patients with neurodevelopmental disorders. In pediatric patients, there is a role for the use of melatonin in children and adolescents with autism spectrum disorder (ASD) who have not responded to behavioral strategies to improve sleep.

Melatonin also has orphan drug status for neonatal hypoxic-ischemic encephalopathy. Although considered a dietary supplement in the U.S., melatonin is available by prescription in Europe under the brand name Circadin as a short-term monotherapy treatment for primary insomnia characterized by poor quality of sleep in patients 55 years of age or more.

According to the British Association for Psychopharmacology guidelines, extended-release melatonin is the first-choice treatment when a hypnotic is indicated in patients over 55 years of age.

Although the American Academy of Sleep Medicine (AASM) guidelines recommend against melatonin as a treatment for primary insomnia in adults due to a lack of reliable efficacy data, research is ongoing.

The effects of melatonin as a hormone were first noted in 1917; melatonin was subsequently isolated from the pineal gland of animals and used to produce commercial melatonin products.

Currently available melatonin products are primarily synthesized because of the potential for contamination from animal-based infectious prions and viruses, which may cause serious illness.

Products classified as dietary supplements should be used cautiously because rigid quality control standards are not required and substantial variability can occur in both potency and purity of marketed products.

Indications

  1. circadian rhythm disruption
  2. delayed sleep phase syndrome
  3. insomnia
  4. irregular sleep-wake disorder
  5. jet-lag
  6. migraine prophylaxis
  7. non-24-hour sleep-wake disorder
  8. shift work sleep disorder
  9. tinnitus

For the short-term treatment of insomnia

Side Effects

  1. abdominal pain
  2. abnormal dreams
  3. agitation
  4. amnesia
  5. anaphylactoid reactions
  6. angioedema
  7. anxiety
  8. arthralgia
  9. complex sleep-related behaviors
  10. confusion
  11. constipation
  12. depression
  13. diarrhea
  14. dizziness
  15. drowsiness
  16. dyspepsia
  17. flatulence
  18. fluid retention
  19. hallucinations
  20. headache
  21. hepatitis
  22. hot flashes
  23. hyperhidrosis
  24. hypothermia
  25. impaired cognition
  26. lethargy
  27. mania
  28. nausea
  29. nightmares
  30. nocturia
  31. palpitations
  32. pharyngitis
  33. pruritus
  34. psychosis
  35. pyrosis (heartburn)
  36. rash
  37. seizures
  38. sinus tachycardia
  39. somnambulism
  40. suicidal ideation
  41. vomiting

Monitoring Parameters

  • laboratory monitoring not necessary

Contraindications

  • angioedema
  • asthma
  • autoimmune disease
  • breast cancer
  • breast-feeding
  • children
  • coadministration with other CNS depressants
  • complex sleep-related behaviors
  • depression
  • diabetes mellitus
  • driving or operating machinery
  • endocrine disease
  • ethanol ingestion
  • geriatric
  • hepatic disease
  • infants
  • infertility
  • labor
  • neonates
  • neoplastic disease
  • neurological disease
  • obstetric delivery
  • organ transplant
  • pregnancy
  • reproductive risk
  • seizure disorder
  • suicidal ideation

Interactions

  • Abacavir; Dolutegravir; Lamivudine
  • Acetaminophen; Aspirin, ASA; Caffeine
  • Acetaminophen; Butalbital; Caffeine
  • Acetaminophen; Butalbital; Caffeine; Codeine
  • Acetaminophen; Caffeine
  • Acetaminophen; Caffeine; Dihydrocodeine
  • Acetaminophen; Caffeine; Magnesium Salicylate; Phenyltoloxamine
  • Acetaminophen; Caffeine; Phenyltoloxamine; Salicylamide
  • Acetaminophen; Codeine
  • Acetaminophen; Hydrocodone
  • Acetaminophen; Oxycodone
  • Acetaminophen; Tramadol
  • Alfentanil
  • Aliskiren; Amlodipine
  • Aliskiren; Amlodipine; Hydrochlorothiazide, HCTZ
  • Aliskiren; Hydrochlorothiazide, HCTZ
  • Amiloride; Hydrochlorothiazide, HCTZ
  • Amlodipine
  • Amlodipine; Atorvastatin
  • Amlodipine; Benazepril
  • Amlodipine; Celecoxib
  • Amlodipine; Hydrochlorothiazide, HCTZ; Olmesartan
  • Amlodipine; Hydrochlorothiazide, HCTZ; Valsartan
  • Amlodipine; Olmesartan
  • Amlodipine; Telmisartan
  • Amlodipine; Valsartan
  • Aspirin, ASA; Butalbital; Caffeine
  • Aspirin, ASA; Butalbital; Caffeine; Codeine
  • Aspirin, ASA; Caffeine; Dihydrocodeine
  • Aspirin, ASA; Caffeine; Orphenadrine
  • Aspirin, ASA; Carisoprodol; Codeine
  • Aspirin, ASA; Citric Acid; Sodium Bicarbonate
  • Aspirin, ASA; Oxycodone
  • Atenolol
  • Atenolol; Chlorthalidone
  • Azilsartan; Chlorthalidone
  • Barbiturates
  • Belladonna; Opium
  • Benazepril; Hydrochlorothiazide, HCTZ
  • Bendroflumethiazide; Nadolol
  • Benzhydrocodone; Acetaminophen
  • Benzodiazepines
  • Bepridil
  • Betamethasone; Calcipotriene
  • Bictegravir; Emtricitabine; Tenofovir Alafenamide
  • Bisoprolol; Hydrochlorothiazide, HCTZ
  • Bisphosphonates
  • Brompheniramine; Guaifenesin; Hydrocodone
  • Brompheniramine; Hydrocodone; Pseudoephedrine
  • Caffeine
  • Caffeine; Ergotamine
  • Calcipotriene
  • Calcitonin
  • Calcium Phosphate, Supersaturated
  • Calcium-channel blockers
  • Candesartan; Hydrochlorothiazide, HCTZ
  • Cannabidiol
  • Capmatinib
  • Captopril; Hydrochlorothiazide, HCTZ
  • Carbamazepine
  • Carbinoxamine; Hydrocodone; Phenylephrine
  • Carbinoxamine; Hydrocodone; Pseudoephedrine
  • Cardiac glycosides
  • Cenobamate
  • Cetirizine
  • Cetirizine; Pseudoephedrine
  • Chloral Hydrate
  • Chlorothiazide
  • Chlorpheniramine; Codeine
  • Chlorpheniramine; Dihydrocodeine; Phenylephrine
  • Chlorpheniramine; Dihydrocodeine; Pseudoephedrine
  • Chlorpheniramine; Guaifenesin; Hydrocodone; Pseudoephedrine
  • Chlorpheniramine; Hydrocodone
  • Chlorpheniramine; Hydrocodone; Phenylephrine
  • Chlorpheniramine; Hydrocodone; Pseudoephedrine
  • Chlorpromazine
  • Chlorthalidone
  • Chlorthalidone; Clonidine
  • Cimetidine
  • Ciprofloxacin
  • Clevidipine
  • Codeine
  • Codeine; Guaifenesin
  • Codeine; Phenylephrine; Promethazine
  • Codeine; Promethazine
  • COMT inhibitors
  • Conjugated Estrogens
  • Conjugated Estrogens; Bazedoxifene
  • Conjugated Estrogens; Medroxyprogesterone
  • Delafloxacin
  • Deutetrabenazine
  • Dextromethorphan; Promethazine
  • Dienogest; Estradiol valerate
  • Diethylstilbestrol, DES
  • Dihydrocodeine; Guaifenesin; Pseudoephedrine
  • Diltiazem
  • Diphenhydramine; Hydrocodone; Phenylephrine
  • Dolutegravir
  • Dolutegravir; Lamivudine
  • Dolutegravir; Rilpivirine
  • Drospirenone; Estradiol
  • Drospirenone; Ethinyl Estradiol
  • Drospirenone; Ethinyl Estradiol; Levomefolate
  • Edetate Calcium Disodium, Calcium EDTA
  • Edetate Disodium, Disodium EDTA
  • Elagolix; Estradiol; Norethindrone acetate
  • Eltrombopag
  • Enalapril; Felodipine
  • Enalapril; Hydrochlorothiazide, HCTZ
  • Eprosartan; Hydrochlorothiazide, HCTZ
  • Esketamine
  • Esterified Estrogens
  • Esterified Estrogens; Methyltestosterone
  • Estradiol
  • Estradiol Cypionate; Medroxyprogesterone
  • Estradiol; Levonorgestrel
  • Estradiol; Norethindrone
  • Estradiol; Norgestimate
  • Estradiol; Progesterone
  • Estramustine
  • Estrogens
  • Estropipate
  • Eszopiclone
  • Ethanol
  • Ethinyl Estradiol
  • Ethinyl Estradiol; Desogestrel
  • Ethinyl Estradiol; Ethynodiol Diacetate
  • Ethinyl Estradiol; Etonogestrel
  • Ethinyl Estradiol; Levonorgestrel
  • Ethinyl Estradiol; Levonorgestrel; Ferrous bisglycinate
  • Ethinyl Estradiol; Levonorgestrel; Folic Acid; Levomefolate
  • Ethinyl Estradiol; Norelgestromin
  • Ethinyl Estradiol; Norethindrone
  • Ethinyl Estradiol; Norethindrone Acetate
  • Ethinyl Estradiol; Norethindrone Acetate; Ferrous fumarate
  • Ethinyl Estradiol; Norethindrone; Ferrous fumarate
  • Ethinyl Estradiol; Norgestimate
  • Ethinyl Estradiol; Norgestrel
  • Ethotoin
  • Felodipine
  • Fenfluramine
  • Fentanyl
  • Fluoxetine
  • Fluoxetine; Olanzapine
  • Fluphenazine
  • Fluvoxamine
  • Fosinopril; Hydrochlorothiazide, HCTZ
  • Gabapentin
  • Gallium
  • Givosiran
  • Guaifenesin; Hydrocodone
  • Guaifenesin; Hydrocodone; Pseudoephedrine
  • Homatropine; Hydrocodone
  • Hydralazine; Hydrochlorothiazide, HCTZ
  • Hydrochlorothiazide, HCTZ
  • Hydrochlorothiazide, HCTZ; Irbesartan
  • Hydrochlorothiazide, HCTZ; Lisinopril
  • Hydrochlorothiazide, HCTZ; Losartan
  • Hydrochlorothiazide, HCTZ; Methyldopa
  • Hydrochlorothiazide, HCTZ; Metoprolol
  • Hydrochlorothiazide, HCTZ; Moexipril
  • Hydrochlorothiazide, HCTZ; Olmesartan
  • Hydrochlorothiazide, HCTZ; Propranolol
  • Hydrochlorothiazide, HCTZ; Quinapril
  • Hydrochlorothiazide, HCTZ; Spironolactone
  • Hydrochlorothiazide, HCTZ; Telmisartan
  • Hydrochlorothiazide, HCTZ; Triamterene
  • Hydrochlorothiazide, HCTZ; Valsartan
  • Hydrocodone
  • Hydrocodone; Ibuprofen
  • Hydrocodone; Phenylephrine
  • Hydrocodone; Potassium Guaiacolsulfonate
  • Hydrocodone; Potassium Guaiacolsulfonate; Pseudoephedrine
  • Hydrocodone; Pseudoephedrine
  • Hydromorphone
  • Ibritumomab Tiuxetan
  • Ibuprofen; Oxycodone
  • Isoniazid, INH
  • Isoniazid, INH; Pyrazinamide, PZA; Rifampin
  • Isoniazid, INH; Rifampin
  • Isradipine
  • Lasmiditan
  • Lemborexant
  • Levocetirizine
  • Levofloxacin
  • Levorphanol
  • Lofexidine
  • Lumateperone
  • Meperidine
  • Meperidine; Promethazine
  • Meprobamate
  • Mesoridazine
  • Mestranol; Norethindrone
  • Methadone
  • Methoxsalen
  • Methyclothiazide
  • Metolazone
  • Mexiletine
  • Morphine
  • Morphine; Naltrexone
  • Moxifloxacin
  • Nabilone
  • Neuromuscular blockers
  • Nicardipine
  • Nifedipine
  • Nimodipine
  • Nisoldipine
  • Norfloxacin
  • Obeticholic Acid
  • Ofloxacin
  • Omeprazole; Sodium Bicarbonate
  • Oxycodone
  • Oxymorphone
  • Peginterferon Alfa-2b
  • Perindopril; Amlodipine
  • Perphenazine
  • Perphenazine; Amitriptyline
  • Phenothiazines
  • Phenylephrine; Promethazine
  • Phosphorated Carbohydrate Solution
  • Phosphorus
  • Potassium Phosphate
  • Potassium Phosphate; Sodium Phosphate
  • Pregabalin
  • Prochlorperazine
  • Promethazine
  • Ramelteon
  • Remifentanil
  • Rifampin
  • Rucaparib
  • Sedating H1-blockers
  • Segesterone Acetate; Ethinyl Estradiol
  • Sodium Bicarbonate
  • Sodium Fluoride
  • Sodium Phosphate Monobasic Monohydrate; Sodium Phosphate Dibasic Anhydrous
  • Sufentanil
  • Suvorexant
  • Tacrine
  • Tapentadol
  • Tasimelteon
  • Tetracyclines
  • Thiabendazole
  • Thiazide diuretics
  • Thiethylperazine
  • Thioridazine
  • Thyroid hormones
  • tobacco
  • Tramadol
  • Trandolapril; Verapamil
  • Tricyclic antidepressants
  • Trientine
  • Trifluoperazine
  • Verapamil
  • Vitamin A
  • Vitamin D analogs
  • Warfarin
  • Zaleplon
  • Zileuton
  • Zolpidem
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