Product Description
Codeine Phosphate
Codeine phosphate is the phosphate salt form of codeine, a naturally occurring opioid alkaloid derived from the opium poppy (Papaver somniferum). It’s a prodrug metabolized in the liver (primarily by CYP2D6 enzyme) into morphine, which provides its main analgesic effects. Chemically, it’s C₁₈H₂₁NO₃·H₃PO₄, with a molecular weight of 406.37 g/mol.
Medical Uses
- Pain relief: Mild to moderate pain (e.g., post-surgical, dental). Often combined with acetaminophen (e.g., Tylenol #3) or ibuprofen.
- Cough suppression: Antitussive in syrups (e.g., for dry coughs).
- Antidiarrheal: In low doses (e.g., as part of Lomotil with diphenoxylate).
Doses typically range from 15–60 mg every 4–6 hours for adults (max 360 mg/day), but ultra-rapid CYP2D6 metabolizers may experience toxicity at standard doses.
Pharmacology
| Property | Details |
|---|---|
| Class | Opioid agonist (μ-receptor partial agonist) |
| Onset | 30–60 min (oral); peak 1–2 hours |
| Duration | 4–6 hours |
| Half-life | 2.5–4 hours (codeine); 2–4 hours (morphine metabolite) |
| Bioavailability | ~50% oral (first-pass metabolism) |
| Excretion | Urine (10% unchanged; rest as metabolites) |
Side Effects & Risks
- Common: Drowsiness, constipation, nausea, dizziness, itching.
- Serious: Respiratory depression (dose-dependent; risk highest >200 mg/day), addiction/dependence, overdose (pinpoint pupils, coma).
- Contraindications: Respiratory depression, acute asthma, paralytic ileus, children <12 (FDA black box for cough/cold due to apnea risk), breastfeeding (morphine in milk).
- Interactions: CYP2D6 inhibitors (e.g., fluoxetine) reduce efficacy; sedatives/alcohol amplify depression.
Legal Status
Schedule II controlled substance in the US (high abuse potential); prescription-only worldwide. Overdose treated with naloxone.
Evidence Base
- WHO Essential Medicines List (analgesic).
- Studies (e.g., Cochrane reviews) show modest efficacy for pain/cough vs. placebo, inferior to stronger opioids like morphine.
- Genetic testing recommended for poor/ultra-rapid metabolizers (e.g., ~10% Caucasians poor; 1–2% ultra-rapid).
Fun Fact: Codeine was first isolated in 1832 by Pierre Jean Robiquet. Recreational use often involves extraction from OTC combo pills (e.g., “lean” with promethazine), but purity varies wildly.
Warnings:
- Illegal Sources: Dark web, street dealers, or unregulated foreign sites (e.g., from India/Mexico) risk counterfeits, fentanyl contamination, arrest, or death. US penalties: Up to 20 years prison/fines for trafficking.
- Global Trends: Interpol/FDA seize millions in illicit shipments yearly; purity often <50%.
- Safer Alternatives: For pain—ibuprofen/acetaminophen; cough—dextromethorphan (OTC).
Not medical/legal advice—check local laws (e.g., DEA.gov, EMA.europa.eu). If you need it for health reasons, talk to a doctor.
Additional Information
| Bottles | 3, 6, 12, 24, 48 |
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