Melatonin
JFDA label: Melaton Fast Dissolving Tablets
Mechanism of Action
Agonist of Melatonin receptor — Melatonin receptor agonist
| Target | Action | Gene / class |
|---|---|---|
| Melatonin receptor efficacy | AGONIST |
Indications
Approved
- Autistic Disorder — autism
- Sleep Initiation and Maintenance Disorders — insomnia
Off-label
- Acute Kidney Injury
- Alcohol-Related Disorders
- Anxiety
- Aortic Aneurysm
- Atrial Fibrillation
- Attention Deficit Disorder with Hyperactivity
- Barrett Esophagus
- Bipolar Disorder
- Brain Injuries
- Breast Neoplasms
- Burns
- Carcinoma, Non-Small-Cell Lung
- Child Development Disorders, Pervasive
- Cognitive Dysfunction
- Colitis, Ulcerative
- Delirium
- Dementia
- Dengue
- Depressive Disorder
- Depressive Disorder, Major
- Dermatitis, Atopic
- Enuresis
- Epilepsy
- Essential Hypertension
- Eye Neoplasms
- Fatigue
- Fibromyalgia
- Gastroesophageal Reflux
- Head and Neck Neoplasms
- Hemorrhage
- Hypertension
- Irritable Bowel Syndrome
- Keratosis, Actinic
- Melanoma
- Menopause
- Metabolic Syndrome
- Migraine Disorders
- Multiple Sclerosis, Relapsing-Remitting
- Myocardial Infarction
- Neoplasms
- Pain
- Parkinson Disease
- Periodontitis
- Prediabetic State
- Prognathism
- Reperfusion Injury
- Schizophrenia
- Severe Acute Respiratory Syndrome
- Sleep Wake Disorders
- Squamous Cell Carcinoma of Head and Neck
- Stroke
- Tooth Diseases
- Uveal Melanoma
- Wounds and Injuries
Adverse Reactions
Cardiac disorders (3)
Not Known Angina pectoris · Cardiac disorder · Palpitations
Vascular disorders (2)
Not Known Hot flush · Hypertension
Nervous system disorders (8)
Not Known Dizziness · Headache · Loss of consciousness · Memory impairment · Migraine · Paraesthesia · Somnolence · Syncope
Hepatobiliary disorders (4)
Not Known Hepatic enzyme increased · Hepatobiliary disease · Hyperbilirubinaemia · Liver function test abnormal
Renal and urinary disorders (4)
Not Known Haematuria · Polyuria · Proteinuria · Urinary tract disorder
Blood and lymphatic system disorders (2)
Not Known Leukopenia · Thrombocytopenia
Immune system disorders (2)
Not Known Hypersensitivity · Immune system disorder
Metabolism and nutrition disorders (3)
Not Known Hypertriglyceridaemia · Hypocalcaemia · Hyponatraemia
Gastrointestinal disorders (15)
Not Known Abdominal discomfort · Abdominal pain · Abdominal pain upper · Dry mouth · Dyspepsia · Flatulence · Gastrointestinal disorder · Gastrointestinal pain · Gastrointestinal sounds abnormal · Gastrointestinal tract irritation · Gastrooesophageal reflux disease · Nausea · Stomatitis · Thirst · Vomiting
Skin and subcutaneous tissue disorders (13)
Not Known Angioedema · Dermatitis · Dry skin · Eczema · Erythema · Hand dermatitis · Nail disorder · Oral mucosal blistering · Pruritus · Pruritus generalised · Rash · Rash generalised · Skin disorder
Musculoskeletal and connective tissue disorders (6)
Not Known Arthralgia · Arthritis · Back pain · Connective tissue disorder · Muscle spasms · Musculoskeletal discomfort
Psychiatric disorders (13)
Not Known Abnormal dreams · Aggression · Agitation · Anxiety · Depressed mood · Disorientation · Insomnia · Irritability · Libido increased · Mental disorder · Mood swings · Nightmare · Terminal insomnia
Eye disorders (4)
Not Known Eye disorder · Lacrimation increased · Vision blurred · Visual acuity reduced
Ear and labyrinth disorders (2)
Not Known Vertigo · Vertigo positional
Reproductive system and breast disorders (3)
Not Known Breast disorder · Galactorrhoea · Priapism
Infections and infestations (3)
Not Known Herpes zoster · Infection · Nasopharyngitis
Investigations (4)
Not Known Blood triglycerides increased · Laboratory test abnormal · Urine output increased · Weight increased
General disorders and administration site conditions (38)
Not Known Affect lability · Angiopathy · Asthenia · Breath odour · Chest pain · Disturbance in attention · Disturbance in sexual arousal · Dreamy state · Fatigue · Gastric disorder · Gastritis · Glycosuria · Infestation · Lethargy · Malnutrition · Menopausal symptoms · Mouth ulceration · Neck pain · Nervous system disorder · Nervousness · Night sweats · Nocturia · Oedema mouth · Pain · Pain in extremity · Prostatitis · Protein urine present · Prurigo · Psoriasis · Restless legs syndrome · Salivary hypersecretion · Shock · Stress · Tension · Tongue disorder · Tongue oedema · Tongue ulceration · Urethral disorder
Dosing
Source: openFDA
Warnings & Precautions
Source: openFDA
Warnings & Precautions
If pregnant or breast-feeding, ask a health professional before use. Keep out of reach of children. In case of overdose, get medical help or contact a Poison Control Center right away. Do not use if tamper evident seal is broken or missing. Store in a cool, dry place.
Pregnancy & Lactation
Lactation
Melatonin has no specific use during breastfeeding, and no data exist on the safety of maternal use of melatonin during breastfeeding.
Chemistry & Properties
| Formula | C13H16N2O2 |
|---|---|
| Molecular weight | 232.28 g/mol |
| IUPAC name | N-[2-(5-methoxy-1H-indol-3-yl)ethyl]acetamide |
| CAS | 73-31-4 |
| PubChem CID | 896 |
| InChIKey | DRLFMBDRBRZALE-UHFFFAOYSA-N |
| logP | 1.86 (XLogP 0.8) |
| Polar surface area | 54.12 Ų |
| H-bond acceptors / donors | 2 / 2 |
| Drug-likeness (QED) | 0.84 |
| Lipinski violations | 0 |
SMILES
COc1ccc2[nH]cc(CCNC(C)=O)c2c1Biology & Pharmacokinetics
Pharmacokinetics predicted
| Bioavailability | 70.0% |
|---|---|
| Half-life | 0.839 h |
| Volume of distribution | 1.027 L/kg |
| Protein binding | 51.2% |
| BBB penetrant | No |
Enzyme interactions
| Enzyme | Role | Detail |
|---|---|---|
| CYP1A2 | Inhibitor | Ki 12.000000000000007 µM |
| CYP1A2 | Substrate | — |
| CYP2B6 | Substrate | — |
| CYP2C19 | Substrate | — |
| CYP2C9 | Substrate | — |
| CYP2D6 | Substrate | — |
| CYP3A4 | Inhibitor | — |
Receptor binding (top 7)
| Target | Action | Affinity |
|---|---|---|
| MT1R | Binding | pKi 10.0 |
| MT2R | Binding | pKi 9.8 |
| Melatonin 1B (MTNR1B) | Binding | pKi 9.6 |
| Melatonin | Binding | pKi 9.4 |
| Melatonin 1A (MTNR1A) | Binding | pKi 9.4 |
| 5-HT2B (HTR2B) | Binding | pKi 5.2 |
| 5-HT2B receptor (HTR2B) | Antagonist | pKi 5.2 |
Transporters
BCRP (Inhibitor)BSEP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)MRP2 (Inhibitor)MRP3 (Inhibitor)MRP4 (Inhibitor)OAT3 (Inhibitor)OATP1B1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)Transporter(unspecified) (Substrate)
Drug–drug interactions (17, DDInter)
| Interacting drug | Severity | Management |
|---|---|---|
| Alpelisib | moderate | |
| Anagrelide | moderate | |
| Deferasirox | moderate | |
| Ifosfamide | moderate | |
| Lorlatinib | moderate | |
| Olaparib | moderate | |
| Osimertinib | moderate | |
| Rucaparib | moderate | |
| Teriflunomide | moderate | |
| Vemurafenib | moderate | |
| Warfarin | moderate | |
| Caffeine | minor | |
| Cimetidine | minor | |
| Diethylstilbestrol | minor | |
| Ethinylestradiol | minor | |
| Obeticholic acid | minor | |
| Osilodrostat | minor |
Registered Products (7)
| Brand | Form / strength | Pack | Agent | Citizen (JOD) |
|---|---|---|---|---|
| Melaton Fast Dissolving Tablets | Tablet 3.0 mg | 10 tab pack varies | Itqan Pharmaceutical Industries | 2.080 |
| Melaton Fast Dissolving Tablets | Tablet 5.0 mg | 10 tab pack varies | Itqan Pharmaceutical Industries | 2.630 |
| Melaton Fast Dissolving Tablets | Tablet 5.0 mg | 20 tab pack varies | Itqan Pharmaceutical Industries | 4.970 |
| Melaton Fast Dissolving Tablets | Tablet 3.0 mg | 30 tab pack varies | Itqan Pharmaceutical Industries | 5.890 |
| Meladaat | Tablet 5 mg/1BOX | 30 tab | Nairoukh Drug Store | 7.450 |
| Melaton Fast Dissolving Tablets | Tablet 5.0 mg | 30 tab pack varies | Itqan Pharmaceutical Industries | 7.450 |
| JP Melatonin 5mg softgel Capsules | Capsule melatonin 5 mg | 60 cap | Land Of Medicine Drug Store | 23.680 |