Usage
This combination is not a standard clinical practice. Potassium glycerophosphate is a nutritional supplement, while promethazine is an antihistamine, sedative, and antiemetic. Some formulations, particularly cough syrups, include both ingredients. Promethazine is used to treat allergic rhinitis, allergic conjunctivitis, motion sickness, nausea and vomiting associated with surgery or other medical conditions. It is also employed for sedation and control of pain and anxiety before and after surgical procedures.
Pharmacological Classification:
- Promethazine: Phenothiazine, antihistamine (H1 receptor antagonist), antiemetic, sedative.
- Potassium glycerophosphate: Nutritional supplement.
Alternate Names
- Promethazine: Phenergan, Promethegan. Numerous brand names exist, especially for combination products containing promethazine.
- Potassium Glycerophosphate: Often combined with other ingredients; therefore, numerous brand names might contain it.
- Combination: Tox Expectorant, Phenomet, Promyoz (and others).
How It Works
Promethazine:
- Pharmacodynamics: Competes with histamine for H1 receptors, primarily in the central nervous system, leading to reduced allergy symptoms. Exerts anticholinergic effects, contributing to sedation, dry mouth, and blurred vision. Also possesses antiemetic properties through its action on the chemoreceptor trigger zone in the brain.
- Pharmacokinetics: Readily absorbed after oral administration. Extensively metabolized in the liver via CYP450 enzymes, notably CYP2D6. Excreted in urine and feces.
Potassium Glycerophosphate:
- The precise mechanisms are not fully elucidated. Thought to act as a source of phosphate for cellular energy processes and potassium for maintaining neuronal function. Clinical evidence of its efficacy is limited.
Mode of Action (Promethazine):
- Receptor Binding: Antagonizes H1 histamine receptors.
- Enzyme Inhibition/Neurotransmitter Modulation: May inhibit dopamine receptors to some extent, contributing to its antiemetic action.
- Elimination Pathways: Primarily hepatic metabolism via CYP450 enzymes, followed by renal and fecal excretion.
Dosage
No established dosage guidelines exist for the combination. The following pertains to promethazine when used independently. Dosage must be individualized, considering patient factors, the condition being treated, and route of administration.
Standard Dosage
Adults:
- Allergy: 12.5 mg orally before meals and at bedtime, or 25 mg at bedtime.
- Motion Sickness: 25 mg twice daily, starting 30-60 minutes before travel.
- Nausea/Vomiting: 25 mg initially, then 12.5-25 mg every 4-6 hours as needed.
Children:
- 2 years and older: Dosage based on weight (0.5 mg/pound or 1.1 mg/kg) or 12.5-25 mg for various indications (allergy, motion sickness, nausea/vomiting). Administer every 4-6 hours as needed.
- Under 2 years: Not recommended.
Special Cases:
- Elderly Patients: Start with lower doses and titrate cautiously.
- Renal Impairment: No specific dosage adjustments. Monitor closely.
- Hepatic Dysfunction: Use cautiously; dosage adjustment may be necessary.
- Patients with Comorbid Conditions: Individualize based on specific conditions and potential drug interactions.
Clinical Use Cases
- Intubation/Surgical Procedures/Mechanical Ventilation/ICU Use: As an adjunct for sedation or antiemetic effect. Dosage is individualized.
- Emergency Situations: Not a first-line agent.
Dosage Adjustments
Adjustments are based on patient response, renal/hepatic function, and concurrent medications.
Side Effects
Common Side Effects:
- Drowsiness
- Dizziness
- Dry mouth
- Blurred vision
- Constipation
Rare but Serious Side Effects:
- Neuroleptic malignant syndrome (NMS)
- Extrapyramidal symptoms (EPS)
- Agranulocytosis
- Seizures
- Respiratory depression (especially in children under 2)
Long-Term Effects:
- Tardive dyskinesia (with prolonged use)
Adverse Drug Reactions (ADR):
Contraindications
- Promethazine: Hypersensitivity to promethazine or other phenothiazines; comatose state; children younger than 2 years. Use with extreme caution in narrow-angle glaucoma, prostatic hypertrophy, bladder neck obstruction, pyloroduodenal obstruction, bone marrow depression, liver disease, respiratory impairment, Reye’s syndrome. Avoid concomitant use with solid potassium chloride formulations.
- Potassium glycerophosphate: Hyperkalemia, severe renal failure.
Drug Interactions
- Promethazine: CNS depressants (increased sedation); anticholinergics (additive anticholinergic effects); MAOIs (prolonged and intensified anticholinergic and hypotensive effects); alcohol. Avoid solid potassium chloride formulations. Numerous other interactions exist; consult a comprehensive drug interaction resource.
- Potassium glycerophosphate: Potassium-sparing diuretics, ACE inhibitors, ARBs (increased risk of hyperkalemia).
Pregnancy and Breastfeeding
- Promethazine: Pregnancy Category C. Use only if benefit outweighs risk. Avoid use near term. Not recommended during breastfeeding.
- Potassium glycerophosphate: Insufficient data.
Drug Profile Summary (Promethazine)
- Mechanism of Action: H1 receptor antagonist, anticholinergic, antiemetic.
- Side Effects: Drowsiness, dizziness, dry mouth, extrapyramidal symptoms, NMS.
- Contraindications: See above.
- Drug Interactions: See above.
- Pregnancy & Breastfeeding: Category C; not recommended.
- Dosage: See above.
- Monitoring Parameters: Respiratory rate, mental status, blood pressure.
Popular Combinations
No established clinically relevant combinations for potassium glycerophosphate and promethazine exist. They happen to be included in some cough and cold medications, but their combined use isn’t a standard therapeutic practice.
Precautions
Refer to Contraindications and Drug Interactions. Pre-screening for allergies, renal/hepatic dysfunction. Caution in elderly patients and children. Avoid alcohol. May impair alertness; restrict driving and operating machinery.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Potassium Glycerophosphate + Promethazine?
A: No standard dosage exists for the combination. Dosing must be determined based on the individual components and indications.
Q2: What are the primary uses of promethazine?
A: Allergies, motion sickness, nausea and vomiting, sedation.
Q3: Can promethazine be given to children under 2 years old?
A: No, it is contraindicated due to the risk of respiratory depression.
Q4: What are the signs of neuroleptic malignant syndrome (NMS)?
A: High fever, muscle rigidity, altered mental status, autonomic instability.
Q5: What are the common side effects of promethazine?
A: Drowsiness, dizziness, dry mouth, blurred vision, constipation.
Q6: Does promethazine interact with alcohol?
A: Yes, concomitant use can potentiate CNS depression. Alcohol should be avoided.
Q7: Can promethazine be used during pregnancy?
A: Pregnancy Category C. Use only if the potential benefit justifies the risk to the fetus.
Q8: Is promethazine safe to use while breastfeeding?
A: Not recommended. It can cause sedation in infants.
Q9: What is the role of potassium glycerophosphate in this combination?
A: Primarily considered a nutritional supplement; its efficacy is not well-established.
Q10: Are there any specific monitoring parameters for patients on promethazine?
A: Respiratory rate, especially in children, mental status changes, and blood pressure should be monitored.