Promethazine

Drug Overview

Promethazine is a synthetic antihistamine primarily used to alleviate allergy symptoms, prevent motion sickness, and provide preoperative sedation. This medication exhibits both anticholinergic and anti-5-HT (serotonin) mechanisms, blocking H1 histamine receptors to reduce allergic reactions such as redness, swelling, and itching, while also suppressing the central nervous system to produce sedative and antiemetic effects. Clinically, it is widely used to control preoperative anxiety, chemotherapy-induced nausea, and severe allergic rhinitis or urticaria.

The pharmacological properties of promethazine make it a versatile treatment tool. However, due to potential side effects such as drowsiness, patients should avoid driving or operating machinery after use. This medication must be prescribed by a physician, and dosage or usage should not be adjusted independently.

Brand Names and Generic Name

The generic name of this drug is Promethazine. Common commercial brand names include Phenergan and Promethegan. Different countries or regions may have other brand names, but the generic ingredient and mechanism of action remain the same. Patients should verify that the active ingredient on the medication label is promethazine when using the drug.

Drug Classification

Promethazine is classified as a first-generation antihistamine (H1 receptor antagonist), with additional anticholinergic and weak dopamine receptor antagonist effects. It is also categorized as an antiemetic and central nervous system depressant, used to treat and prevent various symptoms. Due to its sedative effects, it is also considered part of anxiolytic medications.

Indications

The main indications for promethazine include:

  • Itching and redness caused by allergic dermatitis, urticaria, or contact dermatitis
  • Nausea and vomiting post-chemotherapy, radiation therapy, or surgery
  • Motion sickness caused by travel by plane or vehicle
  • Preoperative sedation or pre-anesthetic preparation

In certain cases, this drug may also be used to treat seizures following epilepsy or as an adjunct therapy for epilepsy. However, its use must be evaluated by a physician, especially for children or patients with neurological conditions.

Common Side Effects

Mild side effects include:

  • Dry mouth
  • Dizziness
  • Drowsiness
  • Constipation

These symptoms usually resolve within a few hours. If they persist or worsen, medical advice should be sought.

Serious side effects require immediate medical attention:

  • Difficulty breathing or chest tightness
  • Irregular heartbeat or abnormal blood pressure
  • Severe skin inflammation or blistering
  • Confusion or muscle weakness

Patients experiencing these symptoms should stop medication immediately and seek emergency medical assistance.

Warnings and Precautions

Contraindications and high-risk groups: Those with the following conditions should not use this medication:

  • Allergy to promethazine or other antihistamines
  • Severe liver or kidney impairment
  • History of epilepsy or seizure risk
  • Closed-angle glaucoma or urinary obstruction

Pregnancy and breastfeeding: Use during pregnancy should only occur if absolutely necessary, as it may pose risks to the fetus. During breastfeeding, it may inhibit milk production and the drug could pass into breast milk, potentially affecting the infant. The U.S. FDA classifies this medication as Category C, indicating animal studies show risk, but human data are insufficient.

Black Box Warning

The U.S. FDA has issued a black box warning for this drug, stating:

  • Use in children under 2 years old may cause respiratory depression or death, and is prohibited
  • Combining with other sedatives can increase central nervous system depression
  • Long-term use may lead to tardive dyskinesia

Prescribers must strictly adhere to age and dosage restrictions.

Drug Interactions

Using with the following medications may increase the risk of adverse effects:

  • Opioid analgesics (morphine, fentanyl): enhanced respiratory depression
  • Tricyclic antidepressants (amitriptyline): increased anticholinergic side effects (e.g., difficulty urinating)
  • Alcohol or sedatives (e.g., zolpidem): increased drowsiness and impairment

Patients should inform their healthcare provider of all medications they are taking, including prescription drugs, over-the-counter medicines, and herbal supplements.

Combining with monoamine oxidase inhibitors (MAOIs) may cause hypertensive crises; at least 14 days should pass after stopping MAOIs before starting promethazine. Co-administration with anticonvulsants may reduce their efficacy, requiring dose adjustments.

Dosage and Administration

Dosages are adjusted based on age and symptoms:

  • Adults for allergies: 25-50 mg per dose, with a maximum daily dose of 100 mg
  • Children for nausea: 1 mg per kg of body weight every 6 hours
  • Preoperative sedation: 25-50 mg injected 1-2 hours before surgery

Oral formulations should be swallowed whole, not chewed or broken.

Injectable forms must be administered by healthcare professionals. Intravenous injections should be administered slowly (over 5 minutes). Extended-release capsules should be taken intact to maintain efficacy; breaking the capsule may cause blood concentration fluctuations.

Missed Dose Management

If a dose is missed, it should be taken as soon as remembered. If it is close to the next scheduled dose, skip the missed dose and resume the regular schedule. Do not double doses to make up for a missed one, as this can lead to toxicity.

If missed doses cause symptoms to recur (e.g., severe nausea), contact a healthcare provider to evaluate whether medication adjustments are necessary. If more than 12 hours have passed since the missed dose, resume the normal dosing schedule at the next dose and monitor symptoms closely.

Overdose Management

Overdose may cause severe central nervous system depression, with symptoms including:

  • Deep coma or unresponsiveness
  • Rapid breathing or respiratory failure
  • Hyperthermia or hypothermia
  • Muscle rigidity or involuntary convulsions

If overdose is suspected, seek immediate medical attention and bring the medication container for reference.

Emergency treatments include gastric lavage, activated charcoal to adsorb unabsorbed drug, and ventilatory support. Severe cases may require antihistamines or intravenous calcium gluconate to relieve seizures. Patients should not attempt to treat overdose themselves; go to the emergency room immediately.

 

Frequently Asked Questions

What are the differences between oral syrup and injectable promethazine in usage?

Oral syrup should be taken according to the physician's instructions, usually before bedtime or after meals to reduce gastrointestinal discomfort. Injectable forms must be administered by healthcare professionals in medical settings and cannot be self-administered. After injection, observe for allergic reactions such as rash or difficulty breathing.

What should I do if I feel drowsy after taking promethazine?

Drowsiness is a common side effect. Avoid driving or operating machinery after taking the medication. If drowsiness persists for several days or significantly affects daily life, consult a healthcare provider for dosage adjustment. Avoid alcohol or sleeping pills to prevent worsening drowsiness.

What drug interactions should I be aware of when using promethazine?

Using with other antihistamines, sedatives, or painkillers may increase drowsiness. Combining with MAOIs may cause blood pressure abnormalities. Inform your doctor of all current medications, including over-the-counter drugs and herbal supplements.

Can patients with glaucoma use promethazine?

Promethazine may worsen closed-angle glaucoma and should be avoided by such patients. For open-angle glaucoma, the doctor will evaluate intraocular pressure before deciding on use and recommend regular eye monitoring.

Is promethazine safe during pregnancy or breastfeeding?

Use during pregnancy should be avoided unless absolutely necessary, as it may pose risks to the fetus. During breastfeeding, the drug may pass into breast milk and affect the infant. Consult a healthcare provider before use to assess potential impacts on the baby. If necessary, adjust feeding times or dosage accordingly.

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