Carbocisteine - Uses, Efficacy, Side Effects, Pharmacology, and Warnings

Overview

Carbocisteine also referred to as Carbocystine, sorts with the class of drugs called mucolytics. Mucolytics are the pharmaceutical class of drug agents that involve a mucus or sputum clearance from the areas of the upper and lower airways. So, Carbocisteine aids in the clearance and prevention of increased secretion of mucus in the airways and helps relieve certain sequelae of respiratory infections in individuals with chronic obstructive pulmonary disease (COPD). COPD includes increased sputum secretion, cough, and breathing difficulties as primary concerns.

Carbocisteine allows or helps the sufferers in bringing up the sputum more easily with airflow clearance and clear breathing. This drug was first addressed in the year 1951, and it came into existence and medical use in the year 1960. Carbocisteine is not approved by the Food and Drug Administration (FDA) currently. Nevertheless, It is approved for medical use in several countries, including Europe, Asia, and South America.

How Does Carbocisteine Work?

Carbocisteine is used to treat and prevent respiratory system diseases that are associated with viscid mucus resulting in airway obstruction. Carbocisteine is known to possess mucolytic and expectorant actions. So, it aids in thinning and loosening the mucus, thereby reducing the viscosity of the mucus. As a result, it clears chest congestion and allows the individuals to clear up the mucus easier. Addedly, it helps relieve cough, breathing difficulties, and other respiratory problems.

Prescriptions:

• COPD: Chronic obstructive pulmonary disease (COPD) is a progressive yet long-term inflammatory condition of the lungs. It refers to a range of conditions presenting symptoms associated with airway obstruction and breathing concerns. Cough and increased sputum production are the predominant symptoms of COPD.

• Bronchiectasis: Bronchiectasis is a chronic lung condition characterized by the widening and deterioration of the airway due to the accumulation of excess mucus, making the lungs more susceptible to infections. The common signs of bronchiectasis are persistent cough with sputum and shortness of breath.

• Cystic Fibrosis: Cystic fibrosis is a type of inherited disorder that causes severe degrees of damage to the lungs and digestive system with other organ systems. Cystic fibrosis is likely to influence and damage the cells involved in the production of sweat, mucus (sputum), and digestive secretions.

What Are the Precautions and Warnings of Carbocisteine?

The drug Carbocisteine can induce unwanted or undesired adverse reactions in specified populations. So, people in specific states should be cautious and take the required considerations.

• Allergy: Rarely, Carbocisteine can precipitate severe and potentially life-threatening allergic or hypersensitivity reactions. The allergic reaction can be with rash, hives, exanthema, and acute swelling. One should immediately seek doctors or emergency care in this instance. Moreover, it is not recommended to take Carbocisteine medication with a past known history of allergy because it might result in serious events.

• Pregnancy: The studies are inadequate and inappropriate in describing the usage and effects of the drug Carbocisteine on pregnant women. Nevertheless, the medication is significantly not advised during pregnancy, particularly during the first trimester period of pregnancy. Healthcare providers might consider adjunct therapy based on the requirements of mucolytic in the person.

• Lactation: The limited studies are on the use of Carbocisteine in lactating women. Also, the potential risk to the child during Carbocisteine intervention in breastfeeding does not have much effect. So, it can be taken during the lactation period. Though, be cautious and inform the physician if one is breastfeeding so that the healthcare providers, before prescribing, will consider certain other factors such as the mother’s clinical requisite of mucolytics, the significance of breastfeeding, and any underlying maternal condition. Addedly, the doctors could consider other treatments in regard to the severity of respiratory conditions.

• Pediatrics: Carbocisteine is not strictly recommended for infants under two years of age since it is attributable to cause certain risks. The studies validating the use of this medication in children are quite less in quantity and quality.

Carbocisteine and Its Dosages

Route of Administration:

Oral

Drug Form and Strengths:

• Carbocisteine comes in forms such as capsules, liquid solutions, and syrup.

• The dose strength of the capsule is 375 mg, while the liquid and syrup are formulated in bottles with 5 ml of a solution containing 250 mg of Carbocisteine.

• The Carbocisteine liquid is also available in sachets with 10 ml containing 750 mg of Carbocisteine.

Drug Dosages

The following is the usual recommended dose of Carbocisteine in its varied forms and strengths. These doses can be modified according to certain determinants by the healthcare provider.

Carbocisteine for Adults

• Capsule: Two capsules of 375 mg of Carbocisteine three times a day. The dosage is reduced to one 375 mg capsule for about four times a day.

• Syrup and Liquid Solution: 15 ml of Carbocisteine syrup three times a day. The dosage can be reduced to 10 ml of syrup three times a day.

• Liquid (Sachets): One sachet of Carbocisteine three times a day. With symptom improvement, the dosage is decreased to one sachet twice daily.

Carbocisteine for Children

• Two to Four Years: Carbocisteine syrup of 1.25 ml to 2.5 ml four times a day.

• Five to 12 Years: 5 ml of Carbocisteine syrup three times a day.

• 12 to 17 Years: Initially, 15 ml of Carbocisteine syrup three times a day. The dosage is reduced to 10 ml of syrup three times a day with improvement in symptoms.

For Patients,

What Is Chronic Obstructive Pulmonary Disease?

Chronic obstructive pulmonary disease (COPD) is a common respiratory disease causing problems with airflow and breathing. It refers to a group of inflammatory lung diseases occurring in the chronic form, which causes obstruction in the airflow from the lungs. In addition, it presents long-term respiratory symptoms interfering with daily life. Emphysema and chronic bronchitis are common conditions resulting in COPD. Emphysema is a lung condition where the air sacs have deteriorated and are damaged, causing breathlessness. And chronic bronchitis is a long-term inflammatory disease of breathing tubes called the bronchi. It causes a productive cough in distinct episodes and extent. The primary cause of the condition is long-term exposure to irritant compounds, particularly cigarette smoke. The most common signs and symptoms of COPD are listed below.

• Wheezing.

• Shortness of breath.

• Chest tightness.

• Chronic cough with mucus or sputum production (the sputum can be yellow, white, or greenish).

• Recurrent respiratory infections.

• Fatigue.

• Unexpected weight loss.

• Swelling in certain parts of lower extremities.

When Is COPD Considered Serious?

Chronic obstructive pulmonary disease is a progressive, severe, preventable, and treatable condition. The worldwide prevalence of COPD is estimated to be about seven percent to 11 percent. Men are more likely to get COPD than women. The pathogenesis of the condition involves several aspects, including increased mucus secretion, airway and lung inflammation, and oxidative stress. Other organs of the system can be involved in this condition in addition to the primary organ lungs. So, people with this condition may have depression, malnutrition, and low pounds in the advanced stage. COPD can progress from mild to severe in gradual means. COPD can cause serious health problems, sometimes leading to life-threatening complications. Moreover, COPD is considered the fourth leading cause of world death. So, it is vital to get effective and early intervention with the means of preventing and treating this deadly condition.

How Does Carbocisteine Help Treat the Symptoms of COPD?

The major symptoms of COPD include severe coughs and difficulty breathing. This is due to the hypersecretion or accumulation of mucus (sputum) in the airways and lungs. Carbocisteine treats cough and certain other respiratory ailments associated with chronic obstructive pulmonary disease. Carbocisteins is a mucolytic drug. So, it helps in thinning and eliminating the mucus substance from the airways. It presents the mucolytic property in the nose, breathing pipe, and lungs. As a result, the obstructed airways are cleared. The drug Carbocisteine also possesses anti-inflammation and antioxidation properties addressing the inflammation and oxidative stress in the lungs. So, as this drug helps clear chest congestion and accompanies signs like chesty coughs and difficulty breathing, one can breathe without any concerns.

How to Take Carbocisteine?

Not every person has similar effects with the medication. Carrbocisteine influences every individual in contrary means. Also, certain medications are likely to induce reactions in people with underlying conditions, drugs, and other states. The doctors prescribe capsules or syrups and dosages accordingly. The drug Carbocisteine is given based on age (adult or pediatric), COPD stage to be treated, the severity of the cough, and underlying medical illnesses. The prescribed medication should be taken according to the physician’s instructions and the manufacturer’s label information described on the package.

What Are the Things to Consider and Tell the Doctor Before Taking Carbocisteine?

• Inform the healthcare providers if in case of allergy to Carbocisteine or any other ingredients of the prescribed medicine.

• Also, inform if one ever had a previous history of allergic reactions to any other medications.

• Convey the doctor about the medication one takes regularly or intermittently. This includes pharmaceutical drugs, nutritional supplements, herbal supplements, and vitamins.

• Tell the doctor in case one has or ever had any medical illnesses or conditions.

• So, inform the doctor if a previous history of stomach ulcer was there.

• The doctor must know if the person is pregnant or has any plans for pregnancy.

• Inform the doctor if one is lactating.

Directions to Take Carbocisteine:

• One must thoroughly read the manufacturer’s printed details, which include comprehensive information about the drug Carbocisteine and how to take it.

• One must take the Carbocisteine medication exactly according to the prescribed dose given by the doctor. So, it should not be taken in more or fewer dosages.

• Take the dosage at a similar time every day.

• Carbosisteine can be taken with or without food.

• The capsules and liquid medication are to be taken orally.

• Take the capsule wholly with a glass of water. Do not chew them.

• Take the liquid medication or syrup with the appropriate dosage. The syrup comes with a measuring spoon or syringe.

• Do not hold or bring to a stop taking the Carbocisteine medication unless the doctor says.

• One should complete the drugs as long as it is prescribed, though with the symptoms improving.

How to Store Carbocisteine?

Store the Carbocisteine medications at room temperature, away from heat, moisture, and sunlight. So, one can save the medicine between 20 and 25 degree Celsius. Any medication and tablets should be kept away from the reach of children.

How to Dispose of the Drug Carbocisteine?

One should dispose of unused, unrequired, or expired medicines in a safe method. This medication, be it capsule or liquid medicine, should not be flushed in the toilet, thrown in the community trash, poured into the channel, or stored in the house bin. The safest method of disposing of Carbocisteine medication is with the local or community recycling procedure. One should reach out to common safe disposal ways in the community in case of any doubts.

In Case of an Overdose of Carbocisteine:

Mucolyte in overdosage significantly causes gastrointestinal disturbances such as nausea, vomiting, and gastralgia. Reach out to the emergency helpline or healthcare providers nearby when excessive amounts of the drug Carbocisteine are taken or suspect your loved ones with a Carbocisteine overdose.

In Case of Missed Dose of Carbocisteine:

One can take the missed dose of Carbocisteine right after one has the thought. Nevertheless, if the time is nearing the next or the other dose, one can forget the missed one and intake the next dose. This is applicable to both the capsules and liquid syrups. Moreover, one should ask the doctor if one misses more than one dosage.

How Effective Is Carbocisteine?

Carbocisteine is a safe and effective drug in treating respiratory ailments in people with chronic obstructive pulmonary disease. Clinical studies show that Carbocisteine is efficient and well-tolerated in COPD treatment. It has potency and efficacy in anti-inflammation, mucolytic, and antioxidation. In addition to the mucolytic effect, the antioxidation and anti-inflammation properties of Carbocisteine have a vital part in long-term therapy in COPD. Consequently, this drug has shown a significant effect on exacerbations. So, it markedly reduced the number of exacerbations in people with COPD. Therefore, it is considered one of the drugs of choice for the prevention of the common cold and exacerbation, particularly in COPD individuals.

What Are the Side Effects of Carbocisteine?

Carbocisteine is a safe and effective medication to take, though, it induces fewer common side effects even with normal dosages. The adverse effects of this drug occur less commonly with about one in ten people. Not everyone under Carbocisteine encounters side effects. The following are considered mild and common side effects which can be resolved on their own over days. These symptoms do not generally discontinue the intervention. But, one should consider and seek professional help if the symptoms stay for a longer span and become bothersome.

• Diarrhea.

• Nausea.

• Stomach upset.

• Headache.

Serious Side Effects:

The serious adverse effects are less common but can be potentially dangerous. Hence, one should stop taking the drug Carbocisteine and contact the healthcare providers right away when experiencing any of the following symptoms.

1. Severe allergic reactions:

• Hives.

• Rashes.

• Itching.

• Tightness in the chest.

• Shortness of breath.

• Swelling of the lips, face, tongue, mouth, or throat.

2. Signs of decline in blood sugar:

• Drowsiness.

• Dizziness.

• Fainting.

• Headache.

• Chills.

• Tremors.

• Excessive sweating.

• Increased hunger.

3. Blood in the stools.

4. Irregular heartbeat.

5. Blood in the vomit or vomit seems like coffee grounds.

6. Poop is black and tarry.

For Doctors,

Clinical Data of Carbocisteine:

Drug name: Carbocisteine.

Other names: S- carboxymethyl-L-cysteine.

Drug class: Mucolytics.

Route of administration: Oral.

Chemical formula: C5H9NO4S

Molar mass: 179.19 g.mol-1

Indications

• Carbocisteine is available in over-the-counter and prescription formulas.

• It is indicated in clearing the airway secretion in conditions related to increased mucus viscosity.

• It is used in the respiratory relief of chronic obstructive pulmonary disease (COPD).

Associated Conditions:

• Respiratory illness.

• Cough.

• Excess mucus or phlegm.

Associated Therapies:

• Airway secretion clearance therapy.

What Is the Pharmacology of Carbocisteine?

Chemistry

Carbocisteine is chemically known as S-carboxymethyl-L-cysteine. It is an L-cysteine thioether which shows that in the L-cysteine compound, the hydrogen part of the thiol group is replaced by means of the carboxymethyl group. Hence, it is a non-proteinogenic L alpha amino acid. Addedly, it is a conjugate acid of a compound S-carboxymethyl-L-cysteine.

Mechanism of Action

Serious respiratory conditions, including cystic fibrosis, asthma, and chronic obstructive pulmonary disease, are primarily characterized by increased mucus secretion or mucus hypersecretion. As a result, bacterial adherence is blocked and thus prevents pulmonary infections. The glycoproteins such as sialomucins, fucomucins, and sulfomucins enhance the viscoelastic dynamics of bronchial mucus. Therefore, individuals with COPD can be detected with an increase in fucomucins in the mucus. The drug Carbocisteine concentrates and works on the restoration of equilibrium between these sialomucins and fucomucins by means of intracellular provocation of the enzyme called sialyl transferase. As a result, the mucus viscosity is reduced.

One particular study depicts that L-carbocisteine can potentially suppress that damage by influencing hydrogen peroxide in the cells through the activation of protein kinase B phosphorylation. This shows that Carbocisteine possesses antioxidant properties and also indulges in the prevention or inhibition of apoptosis of the lung cells. There is certain other evidence presenting the anti-inflammatory effect of Carbocisteine. They show that it inhibits signaling pathways NF-κB and ERK1/2 MAPK and diminishes the lung inflammation that is caused by TNF-alpha. It is also known to influence other inflammatory pathways in the system. According to one in-vitro study, L-carbocisteine is involved in the reduction of intracellular adhesion molecule-1 and suppression of rhinovirus infection 14, with eventual reduction or alleviation of the inflammation concerning the airways.

Pharmacodynamics

• Carbocisteine is a mucolytic drug that addresses and helps alleviate cough, dyspnea, and sputum viscosity because of its mucolytic effect.

• The drug reduces the build-up of mucus or increased mucus secretion and thereby prevents pulmonary infections. This quality of Carbocisteine is effective in cases of COPD exacerbations that pathogens induce.

• In addition, Carbocisteine possesses an in-vitro anti-inflammatory effect.

Absorption

• Carbocisteine is rapidly and effectively absorbed in the gastrointestinal tract following an oral administration.

• The total peak serum concentration is attained in about one to 1.7 hours.

Distribution

• Carbocisteine effectively penetrates the lung tissue as well as bronchial secretions.

Metabolism

• The metabolism of Carbocisteine is attained by acetylation, decarboxylation, and sulfoxidation. As a result, pharmacologically inactive metabolites of Carbocisteine are produced.

• In addition, there can be consequential mutability in the metabolism that can be attributed to the genetic polymorphism in the competence of sulfoxidation.

• So, the metabolic pathways are quite complex, with a broad variation between individuals.

• The cytosolic enzymes responsible for Carbocisteine metabolism include phenylalanine 4-hydroxylase and cysteine dioxygenase.

• The clinical response between individuals can be in contrary fashion in case of reduced metabolism causing increased Carbocisteine exposure. This can be attributed to the effects of genetic polymorphisms on the enzymes responsible for metabolism.

• Sulfoxidation is considered the predominant metabolic pathway of the whole process.

Elimination

• An unchanged form of the administered dose is seen in the urine following an oral administration.

• It can be from 30 percent to 60 percent.

Half-life and Clearance

• The plasma half-life of the drug Carbocisteine is about 1.33 hours.

Contraindications:

• Active forms of peptic or duodenal ulcer.

• Children below two years of age.

Adverse Drug Reactions:

Significant Effects:

• Gastrointestinal bleeding.

Immune System Disorders:

• Fixed drug eruption (dermatological manifestations of drug reactions).

• Anaphylactic reactions (severe allergic reactions).

Gastrointestinal Disorders:

• Nausea.

• Vomiting.

• Epigastric discomfort.

• Diarrhea.

Skin and Subcutaneous Tissue Disorders:

• Rashes.

• Bullous dermatitis in rare instances.

Special Precautions:

• Precautions are to be taken in patients with chronic bronchial asthma, gastroduodenal ulcers, and respiratory failure.

• Precautions are to be taken while prescribed for specified populations- pregnancy, children, and lactation.

• Carbocisteine is known to induce gastrointestinal bleeding when used with certain concomitant medications.

• It is not recommended to be used in conjunction with antitussives and other drugs that dry out the bronchial secretions.

What Are the Potential Drug Interactions of Carbocisteine?

Carbocisteine is a mucolytic agent that helps with the reduction of the sputum viscosity. The drug is known to interact with 18 distinct drugs. So, The following drugs show the potential interactions with the increase in risk and severity of adverse reactions when in conjugation with Carbocisteine.

• Cefotetan.

• Acetohexamide.

• Chlorpropamide.

• Disulfiram.

• Chloramphenicol.

• Gliclazide.

• Glimepiride.

• Glipizide.

• Glibornuride.

• Glipizide.

• Glyburide.

• Gliquidone.

• Griseofulvin.

• Ketoconazole.

• Metronidazole.

• Griseofulvin micro size.

• Procarbazine.

• Tolazamide.

• Tolbutamide.