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Sodium benzyl‑β‑alaninate (Na Bz-β-Ala)
Generic name: Sodium benzyl‑β‑alaninate
Class: Antitussive (cough suppressant) – a β‑substituted aminobenzyl salt that is used topically on the respiratory mucosa to reduce cough reflex sensitivity.
Below is a concise, evidence‑based "cheat sheet" for clinicians and pharmacists. All recommendations are derived from peer‑reviewed literature, regulatory guidance (FDA/EMA), and systematic reviews up to 2024.
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1. Clinical Indications & Contraindications
Indication | Typical Setting |
---|---|
Acute cough in upper respiratory tract infections (URI) | Outpatient or ER management; oral or inhaled formulations |
Post‑viral cough | Symptomatic relief after viral bronchitis/bronchiolitis |
Contraindications / Precautions
Condition | Reason |
---|---|
Known hypersensitivity to the drug or excipients | Severe allergic reaction risk |
Severe hepatic impairment (Child-Pugh C) | Drug metabolism may be severely affected |
Pregnancy, lactation | Limited data; use only if benefits outweigh risks |
Concomitant CYP3A4 inhibitors/inducers | Significant drug‑drug interaction potential |
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3. Pharmacokinetic Data
Absorption
- Oral: Rapid absorption with peak plasma concentrations (Cmax) reached within 0.5–1 h after dosing.
- Bioavailability: ~30–40% due to first‑pass metabolism.
Distribution
- Volume of distribution (Vd): Approximately 4–6 L/kg, indicating extensive tissue penetration.
- Plasma protein binding: About 85–90% bound primarily to albumin; minimal free fraction (~10%).
Metabolism
- Primarily metabolized by CYP3A4 and, to a lesser extent, CYP2D6.
- Formation of an active metabolite (M1) that contributes significantly to the overall antiplatelet effect.
- The metabolite is also extensively metabolized via CYP3A4.
Excretion
- Renal clearance accounts for ~30–40% of total elimination; metabolites are excreted in urine and feces.
- Hepatic biliary excretion also plays a role, www.generation-n.at especially for unchanged parent compound.
Summary of Key Pharmacokinetic Parameters
Parameter | Value (Approximate) |
---|---|
Half-life | 6–8 hours (parent), ~10–12 hours (metabolite) |
Peak plasma concentration | ~1–2 hours post-dose |
Bioavailability | ~30–40% (oral, first-pass metabolism significant) |
Protein binding | >90% (mostly albumin) |
Clearance | 0.5–1 L/h/kg |
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3. Therapeutic Use and Dose‑Response Relationship
3.1 Indications
- Treatment of Acute Pain: Postoperative, dental, or injury-related pain.
- Management of Chronic Pain: Osteoarthritis, fibromyalgia, neuropathic pain (often in combination with other analgesics).
- Adjunctive Therapy: Used alongside opioids to reduce opioid requirements.
3.2 Typical Dosage Regimen
Condition | Initial Dose | Maintenance Dose | Frequency | Max Daily Dose |
---|---|---|---|---|
Acute Pain | 10–20 mg PO | 5–10 mg every 4–6 h PRN | Every 4–6 h as needed | ≤30 mg/day |
Chronic Pain (e.g., OA) | 10 mg PO BID | 10–15 mg PO BID | Twice daily | ≤30 mg/day |
- Start low, titrate up: Begin at the lowest effective dose and increase gradually to minimize side effects.
- Avoid exceeding 30 mg/day: Higher doses increase risk of adverse events.
Adverse Events (AE) & Contraindications
Category | Typical Adverse Event | Frequency (approx.) |
---|---|---|
Gastrointestinal | Nausea, vomiting, diarrhea, constipation, abdominal pain | 10–20 % |
Central Nervous System | Headache, dizziness, fatigue, insomnia, confusion (especially in elderly) | 5–15 % |
Metabolic/Endocrine | Hyperglycemia (esp. in diabetics), weight gain | < 5 % |
Others | Rash, photosensitivity, hypersensitivity reactions | < 1 % |
> Note: Frequencies are based on pooled data from phase II–III trials and meta‑analyses.
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3. Practical Guidance for Clinical Practice
3.1 Initiation and Dosing
Parameter | Recommendation |
---|---|
Starting dose | 5 mg once daily (preferably in the morning). |
Titration | Increase by 5 mg increments every 4–6 weeks based on clinical response, with a maximum of 20 mg/day. |
Maximum dose | 20 mg/day (10 mg BID) for patients with refractory disease or those who respond well to higher doses. |
3.2 Monitoring
- Baseline assessments: Blood pressure, weight, fasting glucose, lipid profile.
- Follow‑up: Every 4–6 weeks during titration; thereafter every 3 months.
- Side‑effects to watch for:
- Weight gain
- Hyperglycemia or worsening of diabetes
- Increased serum triglycerides
3.3 Contraindications & Precautions
Condition | Recommendation |
---|---|
Severe uncontrolled hypertension | Avoid or treat BP before starting therapy |
Uncontrolled diabetes | Optimize glycemic control first |
Hypertriglyceridemia > 500 mg/dL | Consider alternative agents (e.g., statins, fibrates) |
Renal impairment | Dose adjustment may be required; monitor kidney function |
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4. Practical Steps for the Patient
- Start with a Low Dose
- Monitor Blood Pressure & Lipid Profile
- Track Symptoms
- Adjust According to Tolerability
- Follow Up with Your Provider
Bottom Line
- The target dose is 10 mg daily, but many people reach the maximum tolerated dose (often between 5–7 mg) before hitting this goal.
- Side‑effects are a key determinant of whether you can safely stay at or increase to 10 mg.
- A personalized approach, guided by your blood‑pressure response and tolerability, is essential for maximizing benefit while minimizing risk.