Promethazine detailed information
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| Promethazine detailed information
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| Systematic (IUPAC) name | |
| N, N-dimethyl-1-(10H-phenothiazin-10-yl)propan-2-amine | |
| Identifiers | |
| CAS number | |
| ATC code | D04 R06AD02, R06AD05 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C17H20N2S |
| Mol. mass | 284.425 g/mol |
| Pharmacokinetic data | |
| Bioavailability | 88% absorbed but after first-pass metabolism reduced to 25% absolute bioavailability |
| Protein binding | 93% |
| Metabolism | Hepatic glucuronidation and sulfoxidation |
| Half life | 16-19 hours |
| Excretion | Renal and biliary |
| Therapeutic considerations | |
| Pregnancy cat. | |
| Legal status | |
| Routes | Oral, rectal, IV, IM |
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Promethazine is a first-generation H1 receptor antagonist antihistamine and antiemetic medication. It is a prescription drug in the United States, but is available over the counter in the United Kingdom, Switzerland, and many other countries (brand names Phenergan®, Promethegan®, Romergan, Fargan®, Prothiazine®).
Promethazine also has strong anticholinergic and sedative/hypnotic effects. Previously it was used as an antipsychotic, although it is generally not administered for this purpose now; promethazine has only approximately 1/10 of the antipsychotic strength of chlorpromazine.
Indications
- As sedative/hypnotic
- For preoperative sedation and to counteract postnarcotic nausea
- As antiallergic medication to combat hay fever, allergic rhinitis, etc. To treat allergic reactions it can be given alone or in combination with oral decongestants like pseudo-ephedrine.
- Together with codeine or dextromethorphan against cough
- As a motion sickness or seasickness remedy when used with Ephedrine or Pseudoephedrine.
- As an antipruritic (pruritus vulvae).
- To combat moderate to severe morning sickness and hyperemesis gravidarum.
Contraindications
- Promethazine should not be given to children under two years of age; there is potential for fatal respiratory depression in this age group.
- Hypersensitivity to Phenothiazines
- Closed angle glaucoma
- Intoxication with alcohol or other central depressants
- Severe hypotension or shock
- Coma due to any reason
- Severely impaired liver function
- Urine hesitancy due to enlargement of the prostate gland
Side effects
Typical side effects are:
- Blurred vision
- Confusion in the elderly
- Drowsiness, dizziness, fatigue, more rarely vertigo
- Dry mouth
- Seizures (extremely rare)
- Neuroleptic malignant syndrome (extremely rare)
- Respiratory depression in patients under age of 2 and in those with severely compromised pulmonal function
- Constipation
Dosage
Depending on disease and clinical condition (age, liver function):
- Mild to moderate cases of agitation: 25–50 mg orally, 3 to 4 times daily
- Insomnia: depending upon severity, 25–100 mg orally at bedtime
In pediatric patients doses as low as 5–10 mg, 3 times daily may suffice. For precise dosing syrup forms exist.
As an anti-emetic:
- Adult: 6.25 mg IV, or 12.5 mg IM
- Pediatric (greater than 2 years old): 0.25 mg/kg IV/ IM
Laboratory examinations
All patients should have their blood pressure measured frequently. During long-term therapy, blood cell counts, liver function studies, EKG, and EEG are recommended. The intervals should be determined according to the risk profile of the patient.
Recreational use
Promethazine is sometimes used as a recreational drug in conjunction with Codeine in prescription cough syrup. The mixture of Sprite and cough syrup with codeine, which is known as "purple drank", is popularized in the rap world, especially in the Houston area.[1]
External links
- Letter from Wyeth Pharmaceuticals to practitioners regarding use of Phenergan in under twos. (PDF format)
References
- Basic and Clinical Pharmacology, 9th ed (2004). Katzung, Bertram G. pp. 264–265.
Antipruritics (D04) | |
|---|---|
| Antihistamines for topical use | Thonzylamine - Mepyramine - Thenalidine - Tripelennamine - Chloropyramine - Promethazine - Tolpropamine - Dimetindene - Clemastine - Bamipine - Isothipendyl - Diphenhydramine - Chlorphenoxamine |
| Anesthetics for topical use | Lidocaine - Cinchocaine - Oxybuprocaine - Benzocaine - Quinisocaine - Tetracaine - Pramocaine |
de:Promethazin hu:Prometazin nl:Promethazine nn:Prometazin ja:プロメタジンsv:Prometazin th:โปรเมทาซีน
Acknowledgement and Attribution Regarding Sources of Content
Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .
