Carbocisteine
Carbocisteine Uses, Dosage, Side Effects, Food Interaction and all others data.
Carbocisteine reduces goblet cell hyperplasia and therefore plays a role in the management of disorders characterised by abnormal mucous. Carbocisteine loosens thick sputum effectively by reducing its viscosity and thereby helps to expectorate that mucus more easily from the respiratory tract. The mucolytic action happens in several mechanisms. It breaks the disulphide bonds, which cross-link certain glycoprotein molecules in the mucus, the mucus produced under the influence of Carbocisteine has high sialomucin and low fucomucin content. This combined effect ultimately reduces the viscosity of the sputum and increases its volume.
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.
| Trade Name | Carbocisteine |
| Generic | Carbocisteine |
| Carbocisteine Other Names | carbocisteína, Carbocisteine, L-carbocysteine, S-carboxymethylcysteine |
| Type | |
| Formula | C5H9NO4S |
| Weight | Average: 179.194 Monoisotopic: 179.025228471 |
| Protein binding | Plasma protein binding information for carbocisteine is not readily available in the literature. |
| Groups | Approved, Investigational |
| Therapeutic Class | Cough expectorants & mucolytics |
| Manufacturer | Typharm Limited |
| Available Country | United Kingdom |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Carbocisteine is used for- Acute bronchitis, Chronic bronchitis, Bronchial asthma, Upper respiratory tract inflammation (pharyngitis, laryngitis), Cystic fibrosis Bronchiectasis, Pulmonary tuberculosis, Drainage in chronic sinusitis and pneumonia, Drainage in otitis media in children.
Carbocisteine is also used to associated treatment for these conditions: Cough, Respiratory Illness, Excess mucus or phlegm, Airway secretion clearance therapy
How Carbocisteine works
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.
A study found that L-carbocisteine can inhibit damage to cells by hydrogen peroxide (H2O2) by activating protein kinase B (Akt) phosphorylation, suggesting that carbocisteine may have antioxidant effects and prevent apoptosis of lung cells. There is some evidence that carbocisteine suppresses NF-κB and ERK1/2 MAPK signalling pathways, reducing TNF-alpha induced inflammation in the lungs, as well as other inflammatory pathways. An in-vitro study found that L-carbocisteine reduces intracellular adhesion molecule 1 (ICAM-1), inhibiting rhinovirus 14 infection, thereby reducing airway inflammation.
Dosage
Carbocisteine dosage
Adult: Initially, 2.25 g daily in divided doses, then 1.5 g daily in divided doses as condition improves.
Child: 2-5 year: 62.5-125 mg 4 times daily; 6-12 year 250 mg tid.
Should be taken with food.
Side Effects
Gastrointestinal discomfort, nausea, diarrhoea, gastrointestinal bleeding, palpitation, dizziness, headache, heartburn and skin rash may occur.
Toxicity
The oral LD50 of carbocisteine in rats is >15000 mg/kg. An overdose with carbocisteine is likely to result in gastrointestinal discomfort with nausea and vomiting.
Precaution
No specific precaution is recommended but Carbocisteine should be used with caution in patients with a recent history of peptic ulcer and recurrent gastrointestinal bleeding.
Interaction
Neither hazardous nor therapeutically useful interactions have been reported.
Food Interaction
- Take with or without food.
Volume of Distribution
Carbocisteine penetrates well into the lung and bronchial secretions.
Elimination Route
Carbocisteine is rapidly absorbed in the gastrointestinal tract when taken orally with peak serum concentrations achieved within 1 to 1.7 hours.
Half Life
The plasma half-life of carbicostine is 1.33 hours.
Clearance
Clearance information for carbocisteine is not readily available in the literature.
Elimination Route
About 30% to 60% of an orally administered dose is detected unchanged in the urine.
Pregnancy & Breastfeeding use
There is no information on the use of Carbocisteine during lactation. While there are no reports of teratogenic effects, the manufacturers do not recommend the use of Carbocisteine in the first trimester.
Contraindication
Contraindicated in active peptic ulceration and in patients with hypersensitivity to the drug.
Acute Overdose
Symptoms: GI disturbance.
Management: May perform gastric lavage, followed by observation.
Storage Condition
Store in a cool and dry place protected from light.
Innovators Monograph
You find simplified version here Carbocisteine
Carbocisteine contains Carbocisteine see full prescribing information from innovator Carbocisteine Monograph, Carbocisteine MSDS, Carbocisteine FDA label
