Peringatan Keamanan

The intraperitoneal LD50 in rats is 170mg/kg and in mice is 160mg/kg.L11338 The subcutaneous LD50 in rats is 400mg/kg and in mice is 240mg/kg.L11338 The oral LD50 in mice is 255mg/kg.L11338

Patients experiencing an overdose of promethazine may present with mild central nervous system and cardiovascular depression, hypotension, respiratory depression, unconciousness, hyperreflexia, hypertonia, ataxia, athetosis, extensor-plantar reflexes, convulsions, dry mouth, flushing, gastrointestinal symptoms, and fixed, dilated pupils.L4000 Treat overdoses with symptomatic and supportive treatment, which may include activated charcoal, sodium sulfate, magnesium sulfate, controlled ventilation, diazepam, intravenous fluids, vasopressors, norepinephrine, phenylephrine, anticholinergic antiparkinsonian agents, diphenhydramine, barbiturates, or oxygen.L4000

Promethazine

DB01069

small molecule approved investigational

Deskripsi

Promethazine, originally known as 3,277 R.P., is an N-dimethylaminopropyl derivative of phenothiazine that was developed in France in 1946.A189901 Promethazine antagonizes a variety of receptors, allowing it to be used for a number of indications including allergic reactions, pain, sedation, nausea, and vomiting.A189907,A190153,A190159,A190150,A190171

Promethazine was granted FDA approval before 29 March 1951.A190177,L4000

Struktur Molekul 2D

Berat 284.419
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half life of promethazine is approximately 12-15h.[A189925]
Volume Distribusi The volume of distribution of promethazine is approximately 970L or 30L/kg.[A189925]
Klirens (Clearance) The intravenous clearance of promethazine is approximately 1.14L/min.[A189925] The renal clearance of promethazine is 5.9mL/min and the renal clearance of promethazine sulfoxide is 90.4mL/min.[A189925]

Absorpsi

A 25mg dose of intramuscular promethazine reaches a Cmax of 22ng/mL.A189925 Intravenous promethazine reaches a Cmax of 10.0ng/mL, with a Tmax of 4-10h, and an AUC of 14,466ng\*h/mL.A189925 Oral promethazine is only 25% bioavailable due to first pass metabolism.A189925 Oral promethazine reaches a Cmax of 2.4-18.0ng/mL, with a Tmax of 1.5-3h, and an AUC of 11,511ng\*h/mL.A189925

Metabolisme

Promethazine is predominantly metabolized to promethazine sulfoxide, and minorly to desmethylpromethazine and a hydroxy metabolite.A183788,A189925 Hydroxylation of promethazine is predominantly mediated by CYP2D6.A183788

Rute Eliminasi

An intravenous dose of promethazine is 0.64% eliminated in the urine as the unchanged parent drug, 0.02-2.02% in the urine as desmethylpromethazine, 10% in the urine as promethazine sulfoxide.A189925

Interaksi Makanan

1 Data
  • 1. Avoid alcohol. Alcohol may increase the sedation caused by promethazine.

Interaksi Obat

2055 Data
Buprenorphine Promethazine 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 Promethazine.
Dronabinol The serum concentration of Dronabinol can be increased when it is combined with Promethazine.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Promethazine.
Hydrocodone Promethazine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Magnesium sulfate The therapeutic efficacy of Promethazine can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Promethazine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Promethazine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Promethazine.
Orphenadrine Promethazine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Promethazine 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 Promethazine.
Rotigotine Promethazine may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Promethazine.
Sodium oxybate Promethazine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Promethazine 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 Promethazine.
Thalidomide Promethazine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Promethazine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Aclidinium The risk or severity of adverse effects can be increased when Promethazine is combined with Aclidinium.
Mianserin Mianserin may increase the anticholinergic activities of Promethazine.
Mirabegron The risk or severity of urinary retention can be increased when Promethazine is combined with Mirabegron.
Potassium chloride The risk or severity of gastrointestinal ulceration can be increased when Promethazine is combined with Potassium chloride.
Pramlintide The risk or severity of reduced gastrointestinal motility can be increased when Pramlintide is combined with Promethazine.
Secretin porcine The therapeutic efficacy of Secretin porcine can be decreased when used in combination with Promethazine.
Tiotropium The risk or severity of adverse effects can be increased when Promethazine is combined with Tiotropium.
Topiramate The risk or severity of hyperthermia and oligohydrosis can be increased when Promethazine is combined with Topiramate.
Umeclidinium The risk or severity of adverse effects can be increased when Promethazine is combined with Umeclidinium.
Amisulpride Promethazine may increase the antipsychotic activities of Amisulpride.
Quinagolide The therapeutic efficacy of Quinagolide can be decreased when used in combination with Promethazine.
Sulpiride Promethazine may increase the antipsychotic activities of Sulpiride.
Benzylpenicilloyl polylysine Promethazine may decrease effectiveness of Benzylpenicilloyl polylysine as a diagnostic agent.
Betahistine The therapeutic efficacy of Betahistine can be decreased when used in combination with Promethazine.
Hyaluronidase (ovine) The therapeutic efficacy of Hyaluronidase (ovine) can be decreased when used in combination with Promethazine.
Hyaluronidase (human recombinant) The therapeutic efficacy of Hyaluronidase (human recombinant) can be decreased when used in combination with Promethazine.
Hyaluronidase The therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Promethazine.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Promethazine.
Lithium hydroxide Lithium hydroxide may increase the neurotoxic activities of Promethazine.
Lithium citrate Lithium citrate may increase the neurotoxic activities of Promethazine.
Mequitazine Promethazine may increase the arrhythmogenic activities of Mequitazine.
Thiopental The risk or severity of adverse effects can be increased when Promethazine is combined with Thiopental.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Promethazine.
Atazanavir Promethazine can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Bosutinib Promethazine can cause a decrease in the absorption of Bosutinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cefditoren Promethazine can cause a decrease in the absorption of Cefditoren resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cefpodoxime Promethazine can cause a decrease in the absorption of Cefpodoxime resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cefuroxime Promethazine can cause a decrease in the absorption of Cefuroxime resulting in a reduced serum concentration and potentially a decrease in efficacy.
Dabrafenib The serum concentration of Promethazine can be decreased when it is combined with Dabrafenib.
Dasatinib Promethazine can cause a decrease in the absorption of Dasatinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Delavirdine Promethazine can cause a decrease in the absorption of Delavirdine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Dexmethylphenidate The therapeutic efficacy of Dexmethylphenidate can be decreased when used in combination with Promethazine.
Erlotinib Promethazine can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Fosamprenavir Promethazine can cause a decrease in the absorption of Fosamprenavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Gefitinib Promethazine can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Indinavir Promethazine can cause a decrease in the absorption of Indinavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Itraconazole Promethazine can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ledipasvir Promethazine can cause a decrease in the absorption of Ledipasvir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Methylphenidate The therapeutic efficacy of Methylphenidate can be decreased when used in combination with Promethazine.
Nelfinavir Promethazine can cause a decrease in the absorption of Nelfinavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Nilotinib Promethazine can cause a decrease in the absorption of Nilotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Pazopanib The therapeutic efficacy of Pazopanib can be decreased when used in combination with Promethazine.
Rilpivirine Promethazine can cause a decrease in the absorption of Rilpivirine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Risedronic acid Promethazine can cause an increase in the absorption of Risedronic acid resulting in an increased serum concentration and potentially a worsening of adverse effects.
Saquinavir Promethazine can cause an increase in the absorption of Saquinavir resulting in an increased serum concentration and potentially a worsening of adverse effects.
Glycopyrronium The risk or severity of adverse effects can be increased when Promethazine is combined with Glycopyrronium.
Linezolid The risk or severity of serotonin syndrome can be increased when Linezolid is combined with Promethazine.
Epinephrine Promethazine may decrease the vasoconstricting activities of Epinephrine.
Phenindione The risk or severity of adverse effects can be increased when Promethazine is combined with Phenindione.
4-hydroxycoumarin The risk or severity of adverse effects can be increased when Promethazine is combined with 4-hydroxycoumarin.
Ethyl biscoumacetate The risk or severity of adverse effects can be increased when Promethazine is combined with Ethyl biscoumacetate.
Clorindione The risk or severity of adverse effects can be increased when Promethazine is combined with Clorindione.
Diphenadione The risk or severity of adverse effects can be increased when Promethazine is combined with Diphenadione.
Tioclomarol The risk or severity of adverse effects can be increased when Promethazine is combined with Tioclomarol.
Metyrosine The risk or severity of extrapyramidal symptoms and CNS depression can be increased when Metyrosine is combined with Promethazine.
Metoclopramide The risk or severity of adverse effects can be increased when Metoclopramide is combined with Promethazine.
Tedizolid phosphate The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Promethazine.
Botulinum toxin type A The risk or severity of adverse effects can be increased when Promethazine is combined with Botulinum toxin type A.
Glucagon Promethazine may increase the gastrointestinal motility reducing activities of Glucagon.
Botulinum toxin type B The risk or severity of adverse effects can be increased when Promethazine is combined with Botulinum toxin type B.
Mirtazapine Promethazine may increase the serotonergic activities of Mirtazapine.
Mesalazine The therapeutic efficacy of Mesalazine can be decreased when used in combination with Promethazine.
Eluxadoline The risk or severity of constipation can be increased when Promethazine is combined with Eluxadoline.
Ramosetron The risk or severity of constipation can be increased when Promethazine is combined with Ramosetron.
Ethanol Promethazine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Promethazine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Promethazine.
Sibutramine The risk or severity of adverse effects can be increased when Promethazine is combined with Sibutramine.
Nefazodone The risk or severity of adverse effects can be increased when Promethazine is combined with Nefazodone.
Zimelidine The risk or severity of adverse effects can be increased when Promethazine is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Promethazine is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Promethazine is combined with Milnacipran.
Desvenlafaxine The risk or severity of serotonin syndrome can be increased when Desvenlafaxine is combined with Promethazine.
Seproxetine The risk or severity of adverse effects can be increased when Promethazine is combined with Seproxetine.
Levomilnacipran The risk or severity of serotonin syndrome can be increased when Promethazine is combined with Levomilnacipran.
Indalpine The risk or severity of adverse effects can be increased when Promethazine is combined with Indalpine.
Alaproclate The risk or severity of adverse effects can be increased when Promethazine is combined with Alaproclate.
Citalopram The risk or severity of QTc prolongation can be increased when Promethazine is combined with Citalopram.
Amphetamine Amphetamine may decrease the sedative activities of Promethazine.
Phentermine Phentermine may decrease the sedative activities of Promethazine.
Benzphetamine Benzphetamine may decrease the sedative activities of Promethazine.

Target Protein

Histamine H1 receptor HRH1
D(2) dopamine receptor DRD2
Muscarinic acetylcholine receptor M1 CHRM1
Muscarinic acetylcholine receptor M2 CHRM2
Muscarinic acetylcholine receptor M3 CHRM3
Muscarinic acetylcholine receptor M4 CHRM4
Muscarinic acetylcholine receptor M5 CHRM5
Alpha adrenergic receptor ADRA1A
Histamine H2 receptor HRH2
P2 Purinoceptors LPAR4
Voltage-gated sodium channel alpha subunit SCN1A
Voltage-gated Potassium Channels KCND1
Calmodulin CALM1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 18886695
    HALPERN BN, HAMBURGER J: A new synthetic anti-histamine substance derived from phenothiazine; phenergan, 3,277 R.P. Can Med Assoc J. 1948 Oct;59(4):322-6.
  • PMID: 31335081
    Southard BT, Al Khalili Y: Promethazine .
  • PMID: 8946477
    Nakamura K, Yokoi T, Inoue K, Shimada N, Ohashi N, Kume T, Kamataki T: CYP2D6 is the principal cytochrome P450 responsible for metabolism of the histamine H1 antagonist promethazine in human liver microsomes. Pharmacogenetics. 1996 Oct;6(5):449-57.
  • PMID: 6849764
    Taylor G, Houston JB, Shaffer J, Mawer G: Pharmacokinetics of promethazine and its sulphoxide metabolite after intravenous and oral administration to man. Br J Clin Pharmacol. 1983 Mar;15(3):287-93. doi: 10.1111/j.1365-2125.1983.tb01501.x.
  • PMID: 24350243
    Cantisani C, Ricci S, Grieco T, Paolino G, Faina V, Silvestri E, Calvieri S: Topical promethazine side effects: our experience and review of the literature. Biomed Res Int. 2013;2013:151509. doi: 10.1155/2013/151509. Epub 2013 Nov 19.
  • PMID: 27315330
    He LL, Wang ZX, Wang YX, Liu XP, Yang YJ, Gao YP, Wang X, Liu B, Wang X: Studies on the interaction between promethazine and human serum albumin in the presence of flavonoids by spectroscopic and molecular modeling techniques. Colloids Surf B Biointerfaces. 2016 Sep 1;145:820-829. doi: 10.1016/j.colsurfb.2016.06.001. Epub 2016 Jun 2.
  • PMID: 31643746
    Authors unspecified: Promethazine .
  • PMID: 25841474
    Smith HS, Cox LR, Smith BR: Dopamine receptor antagonists. Ann Palliat Med. 2012 Jul;1(2):137-42. doi: 10.3978/j.issn.2224-5820.2012.07.09.
Menampilkan 8 dari 11 artikel.

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