Peringatan Keamanan

Generally well-tolerated when taken orally. The most common side effects, day-time drowsiness, headache and dizziness, appear to occur at the same frequency as with placebo. Other reported side effects include transient depressive symptoms, mild tremor, mild anxiety, abdominal cramps, irritability, reduced alertness, confusion, nausea, vomiting, and hypotension. Safety in Adults: Evidence indicates that it is likely safe to use in oral and parenteral forms for up to two months when used appropriately. Some evidence indicates that it can be safely used orally for up to 9 months in some patients. It is also likely safe to use topically when used appropriately. Safety in Children: Melatonin appeared to be used safely in small numbers of children enrolled in short-term clinical trials. However, concerns regarding safety in children have arisen based on their developmental state. Compared to adults over 20 years of age, people under 20 produce high levels of melatonin. Melatonin levels are inversely related to gonadal development and it is thought that exogenous administration of melatonin may adversely affect gonadal development. Safety during Pregnancy: High doses of melatonin administered orally or parenterally may inhibit ovulation. Not advised for use in individuals who are pregnant or trying to become pregnant. Safety during Lactation: Not recommended as safety has not be established.


Oral, rat: LD50 ≥3200 mg/kg

Melatonin

DB01065

small molecule approved nutraceutical vet_approved

Deskripsi

Melatonin is a biogenic amine that is found in animals, plants and microbes. Aaron B. Lerner of Yale University is credited for naming the hormone and for defining its chemical structure in 1958. In mammals, melatonin is produced by the pineal gland. The pineal gland is small endocrine gland, about the size of a rice grain and shaped like a pine cone (hence the name), that is located in the center of the brain (rostro-dorsal to the superior colliculus) but outside the blood-brain barrier. The secretion of melatonin increases in darkness and decreases during exposure to light, thereby regulating the circadian rhythms of several biological functions, including the sleep-wake cycle. In particular, melatonin regulates the sleep-wake cycle by chemically causing drowsiness and lowering the body temperature. Melatonin is also implicated in the regulation of mood, learning and memory, immune activity, dreaming, fertility and reproduction. Melatonin is also an effective antioxidant. Most of the actions of melatonin are mediated through the binding and activation of melatonin receptors. Individuals with autism spectrum disorders (ASD) may have lower than normal levels of melatonin. A 2008 study found that unaffected parents of individuals with ASD also have lower melatonin levels, and that the deficits were associated with low activity of the ASMT gene, which encodes the last enzyme of melatonin synthesis. Reduced melatonin production has also been proposed as a likely factor in the significantly higher cancer rates in night workers.

Struktur Molekul 2D

Berat 232.2783
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 35 to 50 minutes
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

The absorption and bioavailability of melatonin varies widely.

Metabolisme

Hepatically metabolized to at least 14 identified metabolites (identified in mouse urine): 6-hydroxymelatonin glucuronide, 6-hydroxymelatonin sulfate, N-acetylserotonin glucuronide, N-acetylserotonin sulfate, 6-hydroxymelatonin, 2-oxomelatonin, 3-hydroxymelatonin, melatonin glucuronide, cyclic melatonin, cyclic N-acetylserotonin glucuronide, cyclic 6-hydroxymelatonin, 5-hydroxyindole-3-acetaldehyde, di-hydroxymelatonin and its glucuronide conjugate. 6-Hydroxymelatonin glucuronide is the major metabolite found in mouse urine (65-88% of total melatonin metabolites in urine).

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Makanan

2 Data
  • 1. Avoid alcohol. Ingesting alcohol may reduce the effects of melatonin.
  • 2. Take after a meal. Administration of melatonin after eating slows the absorption and reduces the Cmax of melatonin.

Interaksi Obat

1017 Data
Deferasirox The serum concentration of Melatonin can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Melatonin can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Melatonin can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Melatonin can be decreased when it is combined with Teriflunomide.
Buprenorphine Melatonin may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Melatonin.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Melatonin.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Melatonin.
Hydrocodone Melatonin may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Melatonin.
Magnesium sulfate The therapeutic efficacy of Melatonin can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Melatonin may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Melatonin may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Melatonin.
Mirtazapine Melatonin may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Melatonin.
Orphenadrine Melatonin may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Melatonin may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Melatonin.
Pramipexole Melatonin may increase the sedative activities of Pramipexole.
Ropinirole Melatonin may increase the sedative activities of Ropinirole.
Rotigotine Melatonin may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Melatonin.
Suvorexant Melatonin may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Melatonin.
Thalidomide Melatonin may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Melatonin may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Isradipine The therapeutic efficacy of Isradipine can be decreased when used in combination with Melatonin.
Diltiazem The therapeutic efficacy of Diltiazem can be decreased when used in combination with Melatonin.
Trimethadione The therapeutic efficacy of Trimethadione can be decreased when used in combination with Melatonin.
Amlodipine The therapeutic efficacy of Amlodipine can be decreased when used in combination with Melatonin.
Nimodipine The therapeutic efficacy of Nimodipine can be decreased when used in combination with Melatonin.
Nisoldipine The therapeutic efficacy of Nisoldipine can be decreased when used in combination with Melatonin.
Lercanidipine The therapeutic efficacy of Lercanidipine can be decreased when used in combination with Melatonin.
Cinnarizine The therapeutic efficacy of Cinnarizine can be decreased when used in combination with Melatonin.
Ethosuximide The therapeutic efficacy of Ethosuximide can be decreased when used in combination with Melatonin.
Nicardipine The therapeutic efficacy of Nicardipine can be decreased when used in combination with Melatonin.
Verapamil The therapeutic efficacy of Verapamil can be decreased when used in combination with Melatonin.
Zonisamide The therapeutic efficacy of Zonisamide can be decreased when used in combination with Melatonin.
Felodipine The therapeutic efficacy of Felodipine can be decreased when used in combination with Melatonin.
Nitrendipine The therapeutic efficacy of Nitrendipine can be decreased when used in combination with Melatonin.
Perhexiline The therapeutic efficacy of Perhexiline can be decreased when used in combination with Melatonin.
Nifedipine The therapeutic efficacy of Nifedipine can be decreased when used in combination with Melatonin.
Amiodarone The therapeutic efficacy of Amiodarone can be decreased when used in combination with Melatonin.
Carvedilol The therapeutic efficacy of Carvedilol can be decreased when used in combination with Melatonin.
Bepridil The therapeutic efficacy of Bepridil can be decreased when used in combination with Melatonin.
Mibefradil The therapeutic efficacy of Mibefradil can be decreased when used in combination with Melatonin.
Nimesulide The therapeutic efficacy of Nimesulide can be decreased when used in combination with Melatonin.
Prenylamine The therapeutic efficacy of Prenylamine can be decreased when used in combination with Melatonin.
Cyclandelate The therapeutic efficacy of Cyclandelate can be decreased when used in combination with Melatonin.
Flunarizine The therapeutic efficacy of Flunarizine can be decreased when used in combination with Melatonin.
Fluspirilene The therapeutic efficacy of Fluspirilene can be decreased when used in combination with Melatonin.
Clevidipine The therapeutic efficacy of Clevidipine can be decreased when used in combination with Melatonin.
Methsuximide The therapeutic efficacy of Methsuximide can be decreased when used in combination with Melatonin.
Seletracetam The therapeutic efficacy of Seletracetam can be decreased when used in combination with Melatonin.
Nylidrin The therapeutic efficacy of Nylidrin can be decreased when used in combination with Melatonin.
Ziconotide The therapeutic efficacy of Ziconotide can be decreased when used in combination with Melatonin.
Dotarizine The therapeutic efficacy of Dotarizine can be decreased when used in combination with Melatonin.
Xylometazoline The therapeutic efficacy of Xylometazoline can be decreased when used in combination with Melatonin.
Nilvadipine The therapeutic efficacy of Nilvadipine can be decreased when used in combination with Melatonin.
Tranilast The therapeutic efficacy of Tranilast can be decreased when used in combination with Melatonin.
Fasudil The therapeutic efficacy of Fasudil can be decreased when used in combination with Melatonin.
Agmatine The therapeutic efficacy of Agmatine can be decreased when used in combination with Melatonin.
Fendiline The therapeutic efficacy of Fendiline can be decreased when used in combination with Melatonin.
Eperisone The therapeutic efficacy of Eperisone can be decreased when used in combination with Melatonin.
Trimebutine The therapeutic efficacy of Trimebutine can be decreased when used in combination with Melatonin.
Pinaverium The therapeutic efficacy of Pinaverium can be decreased when used in combination with Melatonin.
Barnidipine The therapeutic efficacy of Barnidipine can be decreased when used in combination with Melatonin.
Aranidipine The therapeutic efficacy of Aranidipine can be decreased when used in combination with Melatonin.
Azelnidipine The therapeutic efficacy of Azelnidipine can be decreased when used in combination with Melatonin.
Benidipine The therapeutic efficacy of Benidipine can be decreased when used in combination with Melatonin.
Cilnidipine The therapeutic efficacy of Cilnidipine can be decreased when used in combination with Melatonin.
Darodipine The therapeutic efficacy of Darodipine can be decreased when used in combination with Melatonin.
Efonidipine The therapeutic efficacy of Efonidipine can be decreased when used in combination with Melatonin.
Lacidipine The therapeutic efficacy of Lacidipine can be decreased when used in combination with Melatonin.
Manidipine The therapeutic efficacy of Manidipine can be decreased when used in combination with Melatonin.
Niguldipine The therapeutic efficacy of Niguldipine can be decreased when used in combination with Melatonin.
Niludipine The therapeutic efficacy of Niludipine can be decreased when used in combination with Melatonin.
Carboxyamidotriazole The therapeutic efficacy of Carboxyamidotriazole can be decreased when used in combination with Melatonin.
Naftopidil The therapeutic efficacy of Naftopidil can be decreased when used in combination with Melatonin.
Tetrahydropalmatine The therapeutic efficacy of Tetrahydropalmatine can be decreased when used in combination with Melatonin.
Vinpocetine The therapeutic efficacy of Vinpocetine can be decreased when used in combination with Melatonin.
Gallopamil The therapeutic efficacy of Gallopamil can be decreased when used in combination with Melatonin.
Bencyclane The therapeutic efficacy of Bencyclane can be decreased when used in combination with Melatonin.
Otilonium The therapeutic efficacy of Otilonium can be decreased when used in combination with Melatonin.
Terodiline The therapeutic efficacy of Terodiline can be decreased when used in combination with Melatonin.
Lidoflazine The therapeutic efficacy of Lidoflazine can be decreased when used in combination with Melatonin.
Penfluridol The therapeutic efficacy of Penfluridol can be decreased when used in combination with Melatonin.
Caroverine The therapeutic efficacy of Caroverine can be decreased when used in combination with Melatonin.
Dexverapamil The therapeutic efficacy of Dexverapamil can be decreased when used in combination with Melatonin.
Emopamil The therapeutic efficacy of Emopamil can be decreased when used in combination with Melatonin.
Lomerizine The therapeutic efficacy of Lomerizine can be decreased when used in combination with Melatonin.
Tetrandrine The therapeutic efficacy of Tetrandrine can be decreased when used in combination with Melatonin.
Dexniguldipine The therapeutic efficacy of Dexniguldipine can be decreased when used in combination with Melatonin.
WIN 55212-2 The therapeutic efficacy of WIN 55212-2 can be decreased when used in combination with Melatonin.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Melatonin.
Sodium oxybate Melatonin may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Succinic acid The excretion of Succinic acid can be decreased when combined with Melatonin.
Citrulline The excretion of Citrulline can be decreased when combined with Melatonin.
Pravastatin The excretion of Pravastatin can be decreased when combined with Melatonin.

Target Protein

Melatonin receptor type 1A MTNR1A
Melatonin receptor type 1B MTNR1B
Ribosyldihydronicotinamide dehydrogenase [quinone] NQO2
Estrogen receptor ESR1
Nuclear receptor ROR-beta RORB
Myeloperoxidase MPO
Eosinophil peroxidase EPX
Calreticulin CALR
Acetylserotonin O-methyltransferase ASMT
Calmodulin CALM1

Referensi & Sumber

Synthesis reference: Robert A. S. Welch, Keith Betteridge, "Method of stimulating cashmere growth on cashmere-producing goats using melatonin." U.S. Patent US4855313, issued August, 1986.
Artikel (PubMed)
  • PMID: 15992934
    Boutin JA, Audinot V, Ferry G, Delagrange P: Molecular tools to study melatonin pathways and actions. Trends Pharmacol Sci. 2005 Aug;26(8):412-9.
  • PMID: 15206778
    Caniato R, Filippini R, Piovan A, Puricelli L, Borsarini A, Cappelletti EM: Melatonin in plants. Adv Exp Med Biol. 2003;527:593-7.
  • PMID: 16217125
    Hardeland R: Antioxidative protection by melatonin: multiplicity of mechanisms from radical detoxification to radical avoidance. Endocrine. 2005 Jul;27(2):119-30.
  • PMID: 7773197
    Hattori A, Migitaka H, Iigo M, Itoh M, Yamamoto K, Ohtani-Kaneko R, Hara M, Suzuki T, Reiter RJ: Identification of melatonin in plants and its effects on plasma melatonin levels and binding to melatonin receptors in vertebrates. Biochem Mol Biol Int. 1995 Mar;35(3):627-34.
  • PMID: 18187545
    Ma X, Chen C, Krausz KW, Idle JR, Gonzalez FJ: A metabolomic perspective of melatonin metabolism in the mouse. Endocrinology. 2008 Apr;149(4):1869-79. doi: 10.1210/en.2007-1412. Epub 2008 Jan 10.
  • PMID: 11462772
    Reiter RJ, Acuna-Castroviejo D, Tan DX, Burkhardt S: Free radical-mediated molecular damage. Mechanisms for the protective actions of melatonin in the central nervous system. Ann N Y Acad Sci. 2001 Jun;939:200-15.

Contoh Produk & Brand

Produk: 23 • International brands: 8
Produk
  • Amerix Melatonin
    Tablet, chewable • 2.5 mg/1 • Oral • US
  • Circadin
    Tablet, extended release • 2 mg • Oral • EU • Approved
  • Circadin
    Tablet, extended release • 2 mg • Oral • EU • Approved
  • Circadin
    Tablet, extended release • 2 mg • Oral • EU • Approved
  • Circadin
    Tablet, extended release • 2 mg • Oral • EU • Approved
  • Essential Oil
    Oil • 2.5 mg/10mL • Cutaneous • US • OTC
  • Hypnosom
    Tablet • - • Oral • US
  • MAX Sleep Junior Childrens SLEEP AID
    Solution / drops • 1 mg/1mL • Oral • US
Menampilkan 8 dari 23 produk.
International Brands
  • Mela-T — Alacer Corp. (Canada)
  • Melatol — Elisium (Argentina)
  • Melatonin — Biomed International Products Corp., Nutravite Pharmaceuticals (2008) Inc., Viva Pharmaceutical Inc., Kripps Pharmacy Ltd., SunOpta Inc.
  • Nature'S Harmony — SunOpta Inc. (Canada)
  • Revital Melatonin — Chin Tai Ginseng Co., Ltd (Canada)
  • Rx Balance — SunOpta Inc. (Canada)
  • Sleep Right — SunOpta Inc. (Canada)
  • Vivitas — SunOpta Inc. (Canada)

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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