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Promethazine



Promethazine
Systematic (IUPAC) name
N, N-dimethyl-1-(10H-phenothiazin-10-yl)propan-2-amine
Identifiers
CAS number 60-87-7
ATC code D04AA10 R06AD02, R06AD05
PubChem 4927
DrugBank APRD00601
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.

C(AU) C(US)

Legal status

P(UK) -only(US)
(injection POM(UK))

Routes Oral, rectal, IV, IM

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, Farganesse, Prothiazine, Avomine, Atosil, RhinathioL).

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.

Additional recommended knowledge

Contents

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. In the UK promethazine is drug of first choice being preferred as an older drug with which there is a greater experience of use in pregnancy (second line being metoclopramide or prochlorperazine).[1] Whilst in the US, Zofran (ondansetron) is the usual drug of choice, though the high cost is prohibitive for some women.

Contraindications

  • Promethazine should not be given to children under two years of age; there is potential for fatal respiratory depression in this age group.[2]
  • 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
  • Euphoria (very rare with high IV doses and/or coadministration with opioids/CNS depressants)


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" or "Sizzurp", is popularized in the rap world, especially in the Houston area.[3] It is also sometimes used to counteract nausea caused by illicit opioid use. Promethazine is referred to as "zazz" on Baltimore streets, as in "let's get zazzed".

References

  • (2004) Basic and Clinical Pharmacology, 9th ed, Katzung, Bertram G., pp. 264–265. 
 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Promethazine". A list of authors is available in Wikipedia.
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