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Sunday, July 27, 2025

Carbocisteine


Carbocisteine (also known as carboxysteine) is a mucolytic agent used in the management of respiratory conditions associated with excessive or thick mucus production, particularly chronic obstructive pulmonary disease (COPD), chronic bronchitis, and otitis media with effusion. It works by modifying the structure of mucus, making it less viscous and easier to expel, thereby improving airway clearance and relieving symptoms of cough and chest congestion.

This professional profile outlines the complete pharmacological characteristics of carbocisteine, including brand names, mechanism of action, clinical uses, dosage, safety considerations, contraindications, adverse effects, precautions, and drug interactions, in accordance with reputable clinical guidelines.

Pharmacological Classification

  • Therapeutic class: Expectorant / Mucolytic

  • Pharmacologic class: Thiol derivative (non-sulphhydryl mucoregulator)

  • ATC code: R05CB03

Brand Names and Formulations

  • Mucodyne®, Visclair®, Bronkyl®, Exputex®, Steiromucil®, Carbocisteine Teva, Zephex®

  • Formulations:

    • Oral capsules: 375 mg, 500 mg

    • Oral solution/syrup:

      • Adults: 250 mg/5 mL, 750 mg/10 mL

      • Pediatric syrup: 125 mg/5 mL or 250 mg/5 mL

    • Oral sachets (granules for reconstitution): 750 mg

Mechanism of Action

Carbocisteine is a mucoregulator that acts by modifying the glycoprotein composition of mucus. It works by:

  • Breaking disulfide bonds in mucin proteins → decreasing mucus viscosity

  • Enhancing mucociliary clearance and promoting sputum expectoration

  • Restoring normal viscoelasticity of mucus, particularly in chronic inflammatory airway diseases

  • Indirectly reducing bacterial colonization and airway obstruction by improving mucus flow

Unlike N-acetylcysteine, carbocisteine does not contain a free sulfhydryl group, thus producing less sulfuric odor and taste, and potentially causing fewer gastric side effects.

Indications

Licensed Uses

  • Chronic obstructive pulmonary disease (COPD): adjunct to bronchodilators for mucus clearance

  • Chronic bronchitis and productive cough

  • Bronchiectasis

  • Otitis media with effusion (OME) in children

  • Sinusitis with mucous congestion

  • Tracheostomy care (off-label use for secretion clearance)

Dosage and Administration

Adults (including elderly)

  • Capsules:

    • Initial: 750 mg (2 capsules) three times daily

    • Maintenance: Reduce to 750 mg twice daily when symptoms improve

  • Oral syrup (250 mg/5 mL):

    • 15 mL three times daily initially, then 10 mL three times daily as maintenance

Children

  • Children 2–5 years: 2.5 mL of 250 mg/5 mL syrup, four times daily

  • Children 6–12 years: 5 mL of 250 mg/5 mL syrup, three times daily

  • Children <2 years: Not recommended (due to risk of bronchial obstruction)

Hepatic/Renal Impairment

  • No specific adjustment stated, but caution is advised in severe cases

Administration

  • Taken orally with or without food

  • Best taken after meals to minimize gastrointestinal side effects

  • Should be used consistently for optimal benefit, especially in chronic respiratory conditions

Pharmacokinetics

  • Absorption: Rapidly absorbed from the GI tract

  • Peak plasma level: ~2 hours after administration

  • Plasma half-life: Approximately 1.5–2 hours

  • Distribution: Widely distributed, especially to respiratory tract tissues

  • Metabolism: Hepatic conjugation

  • Excretion: Primarily renal as unchanged drug and metabolites

Contraindications

  • Known hypersensitivity to carbocisteine or any component of the formulation

  • Active peptic ulcer disease or gastrointestinal bleeding history

  • Children <2 years: Not recommended due to insufficient airway control mechanisms

Precautions and Warnings

  • Gastrointestinal bleeding: Use with caution in those with a history of ulcers; stop immediately if bleeding occurs

  • Bronchospasm: May occur in rare cases; discontinue if symptoms worsen

  • Elderly: Increased sensitivity to GI side effects

  • Diabetic patients: Sugar content in syrup formulations should be considered

  • Asthma patients: Monitor for paradoxical increase in cough or wheezing

  • Sputum volume increase: May occur initially due to improved mucolytic activity; not a cause for concern unless excessive or persistent

Adverse Effects

Common (1–10%)

  • Gastrointestinal discomfort

  • Nausea, diarrhea, abdominal pain

  • Rash, headache

Uncommon (<1%)

  • Vomiting

  • Dyspepsia, flatulence

  • Allergic skin reactions (e.g., urticaria)

Rare (<0.1%)

  • Gastrointestinal bleeding, peptic ulcers

  • Anaphylactic reactions

  • Fixed drug eruptions

  • Eosinophilia

  • Bronchospasm, dyspnea (especially in asthmatics)

Drug Interactions

  • Antitussives (e.g., codeine, dextromethorphan): Should not be used concurrently as they suppress cough and reduce mucus clearance

  • Alcohol: May increase gastric irritation risk when used with carbocisteine

  • Anticholinergics: May reduce mucociliary clearance, potentially reducing the effectiveness of mucolytics

  • No significant interactions with bronchodilators, antibiotics, corticosteroids, or antihistamines

Use in Pregnancy and Lactation

Pregnancy

  • Category B (UK):

    • No teratogenic effects noted in animal studies

    • Use only if clearly needed; avoid during first trimester unless benefits outweigh risks

    • Not contraindicated but should be used under medical supervision

Breastfeeding

  • Unknown if carbocisteine is excreted in breast milk

  • Use with caution; consider alternative if infant develops diarrhea or GI symptoms

Use in Special Populations

  • Children under 2 years: Contraindicated

  • Elderly: Generally well tolerated but start at the lowest effective dose

  • Renal impairment: Monitor closely; excretion is primarily renal

  • Hepatic impairment: No dose adjustment stated but caution advised

Patient Counseling Points

  • Emphasize regular use rather than occasional dosing for effectiveness

  • Take after meals to reduce risk of nausea or GI irritation

  • Report any bloody sputum, vomiting blood, or black stools immediately

  • Avoid combining with cough suppressants unless directed by a physician

  • Sugar-free and alcohol-free options are available for diabetic or pediatric patients

  • Increased mucus production early in therapy is a sign of action, not side effect

  • Ensure hydration, as water intake helps further liquefy mucus

  • Shake syrups well before use; follow dosage instructions carefully

Comparison with Other Mucolytics

  • N-acetylcysteine (NAC): Similar mucolytic effect, but more sulfurous taste/smell

  • Ambroxol: Also mucolytic and secretolytic; has additional analgesic effects

  • Bromhexine: Similar action but typically used in pediatric cough formulations

  • Carbocisteine is generally better tolerated than NAC in long-term use due to fewer GI side effects and improved palatability




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