Carbocisteine

Carbocisteine is an antioxidant belonging to Mucolytic agent.

Carbocisteine is a expectorant mucolytic used in the relief of COPD and other conditions associated with increased mucus viscosity.

Carbocisteine is Rapidly and well absorbed from the gastrointestinal tract. Bioavailability: <10%. It penetrates into the lung tissue and respiratory mucus. Volume of distribution: Approx 60-105 L and get Metabolised via acetylation, decarboxylation, and sulfoxidation. It get excreted Via urine (as unchanged drug and metabolites). Elimination half-life: 1.87 hours (range: 1.4-2.5 hours).

The Tmax of Carbocisteine was found within Approx 2 hour.

Carbocisteine shows common side effects like Gastrointestinal bleeding. Gastrointestinal disorders: Nausea, vomiting, diarrhoea, epigastric.

Carbocisteine is available in the form of , capsules and oral solutions.

Carbocisteine is available in India, Germany, Canada, Italy.

Carbocisteine is a mucolytic agent. The muco-regulatory mechanism of carbocisteine is not completely understood. It has been shown to reduce goblet cell hyperplasia, therefore plays a role in the management of disorders characterised by abnormal mucus.

Carbocisteine is available in the form of capsules and solutions.

Carbocisteine is a expectorant mucolytic used in the relief of COPD and other conditions associated with increased mucus viscosity.

The hypersecretion of mucus characterizes serious respiratory conditions including asthma, cystic fibrosis (CF), and chronic obstructive pulmonary disease (COPD). It blocks bacterial adherence to cells, preventing pulmonary infections.Glycoproteins (fucomucins, sialomucins and sulfomucins) regulate the viscoelastic properties of bronchial mucus. Increased fucomucins can be found in the mucus of patients with COPD. Carbocisteine serves to restore equilibrium between sialomucins and fucomucins, likely by intracellular stimulation of sialyl transferase enzyme, thus reducing mucus viscosity.

Carbocisteine is approved for use in the following clinical indications

• Relief of respiratory mucus COPD and other conditions associated with increased mucus viscosity.

Oral

As a mucolytic

Adult: As adjunctive therapy in respiratory tract disorders characterised by excessive, viscous mucus secretions (including COPD): Initially, 2,250 mg daily in divided doses, may be decreased to 1,500 mg daily in divided doses when a satisfactory response is obtained.

Child: 2-5 years Usual dose: 62.5-125 mg 4 times daily or 200 mg daily in 2 divided doses; 6-12 years Usual dose: 100 mg or 250 mg tid. Dosage recommendations may vary among individual products and between countries.

Carbocisteine is available in various strengths as 125 mg/5 mL, 60 ml, 50 mg/ml, 375 mg

Carbocisteine is available in the form of , solution, syrup, tablet.

Active peptic or duodenal ulcer. Children <2 years.

• Common Adverse effects

Gastrointestinal bleeding. Gastrointestinal disorders: Nausea, vomiting, diarrhoea, epigastric.

• Less Common Adverse effects

Anaphylactic reactions, fixed drug eruption.

• Rare Adverse effects

Bullous dermatitis (e.g. Stevens-Johnson syndrome, erythema multiforme).

Enhances the penetration of antibiotic agents (e.g. amoxicillin, erythromycin, cefuroxime) into bronchial secretions.

The common side effects of Carbocisteine include the following Stevens-Johnson syndrome, toxic epidermal necrolysis (TEN), acute generalised exanthematous pustulosis.

Symptoms: Gastrointestinal disturbances such as gastralgia, nausea, and vomiting.

Management: Supportive treatment. May perform gastric lavage, then closely observe the patient.

Pharmacodynamic

Due to its mucolytic effects, carbocisteine significantly reduces sputum viscosity, cough, dyspnea and fatigue. Additionally, it prevents pulmonary infections by decreasing accumulated mucus in the respiratory tract; this is especially beneficial in preventing exacerbations of COPD caused by bacteria and viruses. It has in-vitro anti-inflammatory activity with some demonstrated action against free radicals.

Pharmacokinetics

• Absorption: Carbocisteine is rapidly absorbed in the gastrointestinal tract when taken orally with peak serum concentrations achieved within 1 to 1.7 hours
• Distribution: Carbocisteine penetrates well into the lung and bronchial secretions
• Metabolism: Almost completely metabolised to a variety of hydroxylated metabolites, including Carbocisteine and dibromanthranilic acid. Undergoes extensive hepatic first-pass metabolism.
• Excretion: Metabolic pathways for carbocisteine include acetylation, decarboxylation, and sulfoxidation, leading to the formation of pharmacologically inactive carbocisteine derivatives. Significant variability exists in metabolism due to genetic polymorphism in sulfoxidation capacity. Two cytosolic enzymes are responsible for the metabolism of carbocisteine: cysteine dioxygenase and phenylalanine 4-hydroxylase.About 30% to 60% of an orally administered dose is detected unchanged in the urine.

• https://www.rxlist.com/dopram-drug.htm
• https://www.mims.com/india/drug/info/Carbocisteine ?type=full&mtype=generic
• https://go.drugbank.com/drugs/DB00561
• https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7003846/