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QuickView for Promethazine (compound)

Name: Promethazine
PubChem Compound ID: 110669
Description: A phenothiazine derivative with histamine H1-blocking, antimuscarinic, and sedative properties. It is used as an antiallergic, in pruritus, for motion sickness and sedation, and also in animals.
Molecular formula: C17H20N2S
Molecular weight: 284.42 g/mol
303-14-0; Isomethazine; 10H-Phenothiazine-10-ethanamine, N,N,beta-trimethyl-; Prothiazin; Phenothiazine, 10-(2-(dimethylamino)-1-methylethyl)-; Isopromethazine; Fen-Bridal; Isophenergan; N-(2-(Dimethylamino)-1-methylethyl)phenothiazine; 10-(2-Dimethylaminoisopropyl)phenothiazine.
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Name: Promethazine
Name (isomeric): DB01069
Drug Type: small molecule
Description: A phenothiazine derivative with histamine H1-blocking, antimuscarinic, and sedative properties. It is used as an antiallergic, in pruritus, for motion sickness and sedation, and also in animals.
Promethazin; Proazaimine; Promethazine Hcl; Promazinamide; Prometazine; Prothazin; Proazamine; Prothazine; Isopromethazine; Lilly 1516.
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Brand: Prometh Plain, Isophenergan, Aprobit, Prorex, Zipan-25, Lercigan, Phencen, Fargan, Valergine, Pyrethia, Fenetazina, Remsed, Provigan, Diphergan, Promethaine, Mymethazine Fortis, Hiberna, Promethegan, Vallergine, Diprozin, Romergan, Phargan, Protazine, Fenergan, Phensedyl, Duplamin, Phenergan Fortis, Phenargan, Dimapp, Diprazine, Fenazil, Prometasin, Promethacon, Synalgos, Procit, Histargan, Pilpophen, Prometh Fortis, Tanidil, Avomine, Fellozine, Thiergan, Allergan, Phenergan, Lergigan, Iergigan, Genphen, Pyrethiazine, Pipolphen, Prometazin, Dorme
Brand name mixture: Phenergan VC Expectorant Syrup(Phenylephrine hydrochloride + Potassium guaiacol sulphonate + Promethazine hydrochloride)
Category: Histamine H1 Antagonists, Antipruritics, Anti-Allergic Agents, Phenothiazine Derivatives
CAS number: 60-87-7
Indication: For the treatment of allergic disorders, and nausea/vomiting.
Pharmacology: Promethazine, a phenothiazine, is an H1-antagonist with anticholinergic, sedative, and antiemetic effects and some local anesthetic properties. Promethazine is used as an antiemetic or to prevent motion sickness.
Mechanism of Action: Like other H1-antagonists, promethazine competes with free histamine for binding at H1-receptor sites in the GI tract, uterus, large blood vessels, and bronchial muscle. The relief of nausea appears to be related to central anticholinergic actions and may implicate activity on the medullary chemoreceptor trigger zone.
Absorption: On average, 88% of a promethazine dose is absorbed after oral administration; however, the absolute bioavailability is only 25% because of first-pass clearance.
Protein binding: 93%
Biotransformation: Hepatic
Route of elimination: Promethazine hydrochloride is metabolized in the liver, with the sulfoxides of promethazine and N-desmethylpromethazine being the predominant metabolites appearing in the urine.
Half Life: 16-19 hours
Toxicity: Symptoms of overdose include mild depression of the central nervous system and cardiovascular system to profound hypotension, respiratory depression, unconsciousness, and sudden death. Other reported reactions include hyperreflexia, hypertonia, ataxia, athetosis, and extensor-plantar reflexes (Babinski reflex). LD50=55mg/kg (I.V. in mice)
Affected organisms: Humans and other mammals
Food interaction:
Take with food to reduce irritation. Avoid alcohol.
Drug interaction:
TerbinafineTerbinafine may reduce the metabolism and clearance of Promethazine. Consider alternate therapy or monitor for therapeutic/adverse effects of Promethazine if Terbinafine is initiated, discontinued or dose changed.
GrepafloxacinIncreased risk of cardiotoxicity and arrhythmias
LevofloxacinIncreased risk of cardiotoxicity and arrhythmias
MethamphetamineDecreased anorexic effect, may increase pyschotic symptoms
TramadolIncreased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
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