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Active ingredient: Promethazine - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Anti-allergic Agents
  • Antipruritics
  • Phenothiazine Derivatives

Dosage Forms

  • Tablet
  • Suppository
  • Opthalmic drops
  • Syrup

Brands / Synonyms

Allergan; Aprobit; Atosil; Avomine; Dimapp; Diphergan; Diprazine; Diprozin; Dorme; Duplamin; Fargan; Fellozine; Fenazil; Fenergan; Fenetazina; Genphen; Hiberna; Histargan; Iergigan; Isophenergan; Isopromethazine; Lercigan; Lergigan; Lilly 1516; Mymethazine Fortis; Phargan; Phenargan; Phencen; Phenergan; Phenergan Fortis; Phensedyl; Pilpophen; Pipolphen; Proazaimine; Proazamine; Procit; Promazinamide; Prometasin; Prometazin; Prometh Fortis; Prometh Plain; Promethacon; Promethaine; Promethazin; Promethazine; Promethazine and Phenylephrine; Promethazine and Codeine; Promethazine and Dextromethorphan; Promethazine DM; Promethazine Hcl; Promethazine Plain; Promethazine VC; Promethazine, Phenylephrine and Codeine; Promethegan; Promethiazine; Promezathine; Prorex; Protazine; Prothazin; Prothazine; Provigan; Pyrethia; Pyrethiazine; Remsed; Romergan; Synalgos; Tanidil; Thiergan; Valergine; Vallergine; Zipan-25

Indications

For the treatment of allergic disorders, itching, nausea and 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.

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)

Biotrnasformation / Drug Metabolism

Hepatic

Contraindications

Injection: Promethazine is contraindicated in comatose states, in patients who have received large amounts of central-nervous-system depressants (alcohol, sedative hypnotics, including barbiturates, general anesthetics, narcotics, narcotic analgesics, tranquilizers, etc.), and in patients who have demonstrated an idiosyncrasy or hypersensitivity to promethazine.

Under no circumstances should promethazine be given by intra-arterial injection due to the likelihood of severe arteriospasm and the possibility of resultant gangrene

Promethazine HCl injection should not be given by the subcutaneous route; evidence of chemical irritation has been noted, and necrotic lesions have resulted on rare occasions following subcutaneous injection. The preferred parenteral route of administration is by deep intramuscular injection.

Syrup, Tablets and Suppositories: Phenergan Tablets and Suppositories are contraindicated for use in pediatric patients less than two years of age.

Phenergan Tablets and Suppositories are contraindicated in comatose states, and in individuals known to be hypersensitive or to have had an idiosyncratic reaction to promethazine or to other phenothiazines.

Antihistamines are contraindicated for use in the treatment of lower respiratory tract symptoms including asthma.

Drug Interactions

Injection:

Narcotics And Barbiturates: The CNS-depressant effects of narcotics are additive with promethazine hydrochloride.

Monoamine Oxidase Inhibitors (Maoi): Drug interactions, including an increased incidence of extrapyramidal effects, have been reported when some MAOI and phenothiazines are used concomitantly. Although such a reaction has not been reported with promethazine, the possibility should be considered.


Syrup, Tablets and Suppositories:

CNS Depressants - Phenergan Tablets and Suppositories may increase, prolong, or intensify the sedative action of other central-nervous-system depressants, such as alcohol, sedatives/hypnotics (including barbiturates), narcotics, narcotic analgesics, general anesthetics, tricyclic antidepressants, and tranquilizers; therefore, such agents should be avoided or administered in reduced dosage to patients receiving promethazine HCl. When given concomitantly with Phenergan Tablets and Suppositories, the dose of barbiturates should be reduced by at least one-half, and the dose of narcotics should be reduced by one-quarter to one-half. Dosage must be individualized. Excessive amounts of promethazine HCl relative to a narcotic may lead to restlessness and motor hyperactivity in the patient with pain; these symptoms usually disappear with adequate control of the pain.

Epinephrine - Because of the potential for Phenergan to reverse epinephrineís vasopressor effect, epinephrine should NOT be used to treat hypotension associated with Phenergan Tablets and Suppositories overdose.

Anticholinergics - Concomitant use of other agents with anticholinergic properties should be undertaken with caution.

Monoamine Oxidase Inhibitors (MAOI) - Drug interactions, including an increased incidence of extrapyramidal effects, have been reported when some MAOI and phenothiazines are used concomitantly. This possibility should be considered with Phenergan Tablets and Suppositories.

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