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promethazine (Phenergan, Farganesse)

Tradename: Phenergan. (promethazine hydrochloride) Indications: - adjunct to general anesthesia - preoperative, postoperative or obstetric sedation - prevention & control of nausea & vomiting - adjunct to analgesics for pain management (analgesia) - antihistamine for the prevention & treatment of motion sickness - apprehension [8] - allergies - allergic conconjuntivitis [8] - urticaria [8] Contraindications: 1) angle-closure glaucoma * 2) children < 2 years of age * [4] Caution: in children Dosage: 1) allergies: 25 mg PO QHS 2) nausea/vomiting: -> 1-2 mg/kg up to 25-50 mg PO/IM/PR every 4-6 hours 3) pre-operative sedation: 1-2 mg/kg up to 25-50 mg PO/IM/PR every 4-6 hours 4) post-op: 6.25-12.5 mg IV - dilute with 10 or 20 mL of normal saline - administer through a free-flowing IV [6] 5) children: 0.1-0.5 mg/kg IM/IV/PO/PR every 6 hours PRN Tabs: 12.5, 25, 50 mg. Syrup: 6.25 & 25 mg/5 mL. Suppository: 12.5, 25, 50 mg. Injection: 25 mg/mL (1 mL), 50 mg/mL (1 mL). Pharmacokinetics: 1) onset of sedative effect: a) within 20 minutes following oral, rectal or IM administration b) within 3-5 minutes after intravenous injection 2) metabolized by the liver 3) excreted as inactive drug in the urine & feces Adverse effects: 1) common (> 10%) - slight to moderate drowsiness - thickening of bronchial secretions 2) less common (1-10%) - headache, fatigue, increased appetite, increased weight, nervousness, dizziness, nausea, diarrhea, abdominal pain, dry mouth, pharyngitis, arthralgia 3) uncommon (< 1%) - angioedema, bronchospasm, depression, edema, epistaxis, hepatitis, myalgia, palpitations, paresthesias, photosensitivity, rash, hypotension, sedation, dizziness, paradoxical excitement, fatigue, insomnia, tremor, blurred vision, urinary retention, sedation (marked), dystonia, faintness with IV administration, irregular respiration 4) other - anticholinergic effects: - dry mouth - blurred vision - dizziness (rare) - sedation - extrapyramidal effects with high doses - hypotension may occur with rapid IV administration - jaundice - extravasation with IV use can lead to severe tissue damage including gangrene requiring amputation [6,7] - fatal respiratory depression has occurred * [4,5] - central nervous system depression - especially, children < 2 years of age [5] - seizures Drug interactions: 1) other CNS depressants 2) MAO inhibitors intensify anticholinnergic effects Laboratory: - promethazine in blood - promethazine in blood/urine - promethazine in serum/plasma/urine - promethazine in serum/plasma - promethazine in urine Mechanism of action: 1) agonist at the histamine H1 receptor 2) sedative, anti-motion sickness, & local anesthetic effects 3) antiemetic effects secondary to anticholinergic effects on the: a) vestibular apparatus b) chemoreceptor-trigger zone (CTZ) in the midbrain

Interactions

drug interactions drug adverse effects of H1 receptor antagonists

General

anti-emetic H1 receptor antagonist (antihistamine) phenothiazine

Properties

MISC-INFO: elimination route LIVER KIDNEY pregnancy-category C safety in lactation -

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  3. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  4. Prescriber's Letter 12(4): 2005 Use of Promethazine in Children Detail-Document#: 210411 (subscription needed) http://www.prescribersletter.com
  5. FDA Medwatch http://www.fda.gov/medwatch/safety/2006/safety06.htm#promethazine
  6. Prescriber's Letter 13(10): 2006 Antiemetics Used for Postoperative Nausea and Vomiting Detail-Document#: 221004 (subscription needed) http://www.prescribersletter.com
  7. FDA Medwatch Promethazine Hydrochloride Injection http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm182500.htm
  8. Deprecated Reference

Component-of

codeine/guaifenesin/promethazine codeine/phenylephrine/phosphate/promethazine codeine/phenylephrine/promethazine (Phenergan with phenylephrine & codeine) codeine/phosphate/promethazine codeine/promethazine (Phenergan with codeine) dextromethorphan/promethazine (Phenergan with dextromethorphan) meperidine/promethazine phenylephrine/promethazine (Phenergan with phenylephrine)