Promethazine HCI

Name: Promethazine HCI
Brand: MySkinRecipes
SKU: 127659
Price: 20000 THB
Availability: PreOrder

Drug Code: 127659

Strong H₁-histamine receptor antagonist; moderate muscarinic (anticholinergic) blockade; weak antagonism at 5-HT₂, D₂ and α-adrenergic receptors; non-competitive NMDA receptor antagonist

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Promethazine HCI

Strong H₁-histamine receptor antagonist; moderate muscarinic (anticholinergic) blockade; weak antagonism at 5-HT₂, D₂ and α-adrenergic receptors; non-competitive NMDA receptor antagonist

For Research Only

A. Chemical & Physical Properties

A1. Identity & Structure
- Empirical formula: C₁₇H₂₀N₂S·HCl
- IUPAC name: (RS)-N,N-Dimethyl-1-(10H-phenothiazin-10-yl)propan-2-amine monohydrochloride
A2. Molecular Weight & CAS
- CAS No.: 58-33-3
- M.W.: 320.88 g/mol
A3. pKa
- pKa (conjugate acid): 9.1
A4. Appearance & Stability
- White to faint-yellow crystalline powder; odorless; slow oxidation in air (blue discoloration)
A5. Solubility & pH
- Freely soluble in water (≥100 mg/mL at 25 °C) and soluble in alcohol
- Typical oral solution pH: 4.7–5.2

B. Pharmacology & Uses

B1. Mechanism of Action
- Strong H₁-histamine receptor antagonist; moderate muscarinic (anticholinergic) blockade; weak antagonism at 5-HT₂, D₂ and α-adrenergic receptors; non-competitive NMDA receptor antagonist
B2. Clinical Indications
- Allergic reactions (hay fever, urticaria)
- Nausea/vomiting (motion sickness, postoperative, chemotherapy)
- Sedation/insomnia
- Adjunct in common cold, hemolytic disease of the newborn
- Anxiety before surgery
B3. Routes & Dosage Forms
- Oral tablets: 12.5–25 mg
- Oral syrup: typically 6.25 mg/5 mL
- Rectal suppositories: 12.5 mg
- Injectable solution: 25 mg/mL

C. Pharmacokinetics

C1. Absorption
- ~88% absorbed; first-pass reduces absolute bioavailability to ~25%
C2. Distribution
- ~93% plasma protein bound
C3. Metabolism & Elimination
- Hepatic glucuronidation and sulfoxidation; t½ 10–19 h; excreted via urine and bile

D. Formulation Considerations

D1. pH & Buffering
- Maintain formulation pH 4.7–5.2 (e.g., citrate buffer) to ensure salt stability and solubility
D2. Light & Oxidation
- Protect from light/air; use amber glass or opaque containers to minimize blue oxidation

E. Safety & Side Effects

E1. Common AEs
- Sedation/drowsiness, dizziness, dry mouth, blurred vision, urinary retention
E2. Warnings & Contraindications
- Contraindicated in children < 2 years (respiratory depression), hypersensitivity, narrow-angle glaucoma, prostatic hypertrophy
- Caution in elderly (anticholinergic burden), hepatic/renal impairment

F. Regulatory Status

Prescription-only in the US; POM in the UK; OTC in Canada; S3 in Australia

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Promethazine HCI

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