nedocromil (Oral Inhalation)

Action and Spectrum

Actions and Spectrum: 

nedocromil, administered via oral inhalation, is used primarily for managing bronchial asthma, especially for the prophylaxis of asthma symptoms and to prevent bronchospasm. It belongs to the class of drugs known as mast cell stabilizers. nedocromil acts locally in the airways to prevent the release of inflammatory substances, particularly histamine, and leukotrienes, from mast cells.  

Action: 

• Mast cell stabilizer: nedocromil prevents mast cells from releasing inflammatory mediators when exposure to allergens or exercise triggers. This action helps reduce the sensitivity and hyper-reactivity of the airways, leading to a decrease in asthma symptoms. 
• Anti-inflammatory effects: By inhibiting the release of histamine and leukotrienes, nedocromil helps to reduce inflammation in the airways. Inflammation in the bronchial tubes can cause swelling, narrowing, and excessive mucus production, contributing to asthma symptoms. 
• Prophylactic use: nedocromil is not a quick-relief medication for acute asthma attacks. Instead, it is used as a preventive or prophylactic therapy to minimize the frequency and severity of asthma exacerbations. It is usually taken regularly to maintain control over asthma, even when the patient is symptom-free. 
• Long-term management: nedocromil is part of a comprehensive asthma management plan that may include other medications like bronchodilators (e.g., short-acting beta-agonists) for quick relief during acute episodes. 

Spectrum:  

nedocromil’s spectrum of action is specific to the airways and primarily focuses on asthma management. It is inpractical for treating other respiratory conditions like chronic obstructive pulmonary disease (COPD). The medication is not used for immediate relief during an acute asthma attack but for long-term prevention and control of asthma symptoms. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Heartburn 

Nausea 

Abdominal pain 

Headache 

Constipation 

Dry mouth 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

• Allergy or hypersensitivity: Individuals with known hypersensitivity or allergy to nedocromil or any of the components of the medication should not use it. Severe allergic reactions to the drug can occur in some cases, and immediate medical attention is required if this happens. 
• Acute bronchospasm: nedocromil is unsuitable for relieving acute bronchospasm or asthma attacks. It is a preventive medication and should not be used as a rescue inhaler during sudden breathing difficulties. Short-acting bronchodilators like albuterol are more appropriate for acute symptom relief. 
• Emergency use: nedocromil is not intended to manage life-threatening asthma attacks or status asthmaticus. In such situations, immediate medical attention and appropriate rescue measures should be taken. 
• Pregnancy and breastfeeding: The safety of nedocromil use during pregnancy and breastfeeding has not been well-established. Therefore, its use in pregnant or nursing women should be considered only if the potential advantages outweigh the risks and should be supervised by a healthcare professional. 
• Children under six years old: Safety and efficacy data in children under six years are limited, and nedocromil is not recommended for use in this age group. 
• Severe hepatic impairment: nedocromil is primarily metabolized in the liver, and its use may be contraindicated in individuals with severe liver dysfunction. Dosing adjustments may be necessary for patients with mild to moderate hepatic impairment. 

Caution 

• Acute asthma exacerbation: nedocromil is not intended to relieve acute asthma attacks or sudden worsening of asthma symptoms. Suppose a patient experiences a sudden onset of wheezing, breathlessness, chest tightness, or cough. In that case, they should seek immediate medical attention and use their prescribed rescue inhaler (short-acting bronchodilator) as advised by their healthcare provider. 
• Respiratory infections: During respiratory infections like the common cold or flu, the effectiveness of nedocromil may be reduced. Patients should be cautious and follow their healthcare provider’s advice during such infections, as additional asthma management measures may be necessary. 
• Underlying conditions: nedocromil may not be sufficient to control asthma symptoms in patients with severe asthma or those with other significant respiratory conditions. Close monitoring and adjustments in the treatment plan may be required for such individuals. 
• Allergy history: Individuals with a history of severe allergic reactions or anaphylaxis should use nedocromil cautiously. Although nedocromil is generally a mast cell stabilizer and not known to cause systemic allergic reactions, individual responses may vary. 
• Systemic absorption: Although nedocromil acts locally in the airways, some systemic absorption can occur. Caution should be exercised when prescribing nedocromil to patients with significant hepatic or renal impairment. 
• Pediatric use: While nedocromil is generally safe for older children, caution should be exercised in younger children. Safety and efficacy data in children under six years old are limited, and it is not recommended for use in this age group. 
• Pregnancy and breastfeeding: As with any medication, using nedocromil during pregnancy and breastfeeding should be carefully considered, and the potential benefits should outweigh the risks.  
• Drug interactions: As with any medication, you must inform your healthcare provider about all other medications, supplements, or herbal products you are taking. Drug interactions may occur, and caution should be exercised when combining nedocromil with other medications. 

Pregnancy / Lactation

Pregnancy consideration:  

US FDA pregnancy category: B 

Lactation:   

Excreted into human milk: Not known. 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

When administered via oral inhalation, nedocromil exerts its pharmacological effects as a mast cell stabilizer and anti-inflammatory agent. By inhibiting the release of the inflammatory mediators, like leukotrienes and histamine, from mast cells in the airways, nedocromil helps reduce bronchial hyper-responsiveness and inflammation in patients with asthma.

Its preventive action minimizes the frequency and severity of asthma exacerbations and symptoms, particularly in allergic asthma. However, nedocromil is not intended for immediate relief during acute asthma attacks, and its regular use is essential to maintain long-term asthma control as part of a comprehensive asthma management plan, which may include other medications like bronchodilators and corticosteroids. 

Pharmacodynamics: 

Mechanism of action: when administered via oral inhalation, nedocromil exerts its pharmacological effects primarily as a mast cell stabilizer. Its mechanism of action involves modulating the immune response and preventing the release of inflammatory mediators from mast cells in the airways.  

• Mast cell stabilization: nedocromil binds to specific receptors on mast cells, immune cells found in the airway tissues. By binding to these receptors, nedocromil stabilizes the mast cells, preventing them from releasing their stored inflammatory mediators in response to triggers like allergens, exercise, or irritants. 
• Inhibition of inflammatory mediators: When exposed to triggers, mast cells typically release substances like histamine, leukotrienes, and cytokines. These inflammatory mediators cause the airways to become inflamed, leading to bronchoconstriction (narrowing of the airways), excessive mucus production, and increased sensitivity to irritants. 
• Anti-inflammatory effect: By preventing the release of histamine, leukotrienes, and other inflammatory mediators, nedocromil reduces airway inflammation. This helps reduce swelling and mucus production, improving airflow and decreasing symptoms like wheezing and shortness of breath. 
• Bronchial hyper-responsiveness: Asthma is characterized by increased bronchial hyper-responsiveness, where the airways are overly sensitive and constrict in response to various stimuli. nedocromil helps to reduce this hyper-responsiveness by stabilizing mast cells and limiting the release of bronchoconstrictor substances. 

Pharmacokinetics: 

Absorption 

When administered via oral inhalation, nedocromil is absorbed locally in the airways. It acts topically on the bronchial mucosa, where it exerts its pharmacological effects to stabilize mast cells and avert the release of inflammatory mediators. 

Distribution 

After absorption in the airways, nedocromil does not significantly enter the systemic circulation. It remains primarily localized in the lung tissues, exerting anti-inflammatory and mast cell-stabilizing effects. 

Metabolism 

nedocromil undergoes minimal metabolism in the body. It is not extensively metabolized in the liver like some other medications. The drug’s low systemic exposure contributes to its favorable safety profile. 

Elimination and Excretion 

Since nedocromil is mainly confined to the lungs and not significantly absorbed into the bloodstream, its excretion occurs primarily through the respiratory system. Any residual amounts of the drug that are absorbed systemically undergo renal excretion as unchanged drugs and inactive metabolites. 

Adminstartion

Administration: 

Oral administration 

When used as an oral inhalation medication, nedocromil is typically available as a metered-dose inhaler (MDI).  

• Shake the inhaler: Before using the nedocromil inhaler, shake it well to ensure the medication is mixed correctly. 
• Prime the inhaler (if necessary): Some MDIs require priming, especially if they are new or have not been used for a while. Follow the manufacturer’s instructions for priming the inhaler. Usually, it involves releasing a few test sprays into the air to ensure the device is ready for use. 
• Breathe out: Hold the inhaler upright with the mouthpiece at the bottom and exhale fully to empty your lungs. 
• Position the inhaler: Place the inhaler’s mouthpiece between your teeth, with your lips forming a tight seal around it. Ensure that your tongue does not block the opening. 
• Inhale and actuate the inhaler: As you breathe slowly and deeply through your mouth, press firmly on the canister to release the one puff of nedocromil. This should be done at the beginning of inhalation to ensure the medication reaches your airways effectively. 
• Hold your breath: After inhaling the medication, remove the inhaler from your mouth and hold the breath for nearly 10 seconds, if possible, to allow the nedocromil to reach deep into your lungs. 
• Breathe out slowly: Exhale gently through your mouth. 
• Wait (if needed): If your healthcare provider has prescribed more than one puff, wait for the specified time (usually around 1 minute) before taking the next puff. Shake the inhaler again between puffs. 
• Rinse your mouth (if recommended): If your doctor advises you to do so, rinse your mouth with water following using the inhaler to prevent the development of oral thrush or other potential side effects. 
• Close the inhaler: Recap it properly to protect it from dust and contamination. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: nedocromil (Oral Inhalation) 

Pronounced: [ ne-doe-KROE-mil-in-hil-AYE-shun ] 

Why do we use nedocromil (Oral Inhalation) 

When administered via oral inhalation, nedocromil is primarily used for the prophylaxis or prevention of asthma symptoms. It is not a quick-relief medication for acute asthma attacks but a long-term control medication to manage and diminish the frequency and severity of asthma exacerbations.  

• Asthma prophylaxis: nedocromil is used to prevent asthma symptoms and diminish the frequency of asthma attacks in patients with mild-moderate persistent asthma. It helps control airway inflammation, which significantly contributes to asthma symptoms like wheezing, coughing, chest tightness, and shortness of breath. 
• Allergic asthma: nedocromil is particularly effective in patients with allergic asthma, where asthma symptoms are triggered by exposure to allergens like the pollen, dust mites, pet dander, or mold. It helps to stabilize mast cells and prevent the release of the inflammatory substances in response to allergen exposure. 
• Exercise-induced bronchoconstriction (EIB): nedocromil may be used to prevent exercise-induced bronchoconstriction, a condition where physical activity triggers bronchospasm and causes asthma-like symptoms. 
• As part of an asthma management plan: nedocromil is often prescribed with other asthma medications, such as short-acting bronchodilators (e.g., albuterol) for quick relief during acute attacks and inhaled corticosteroids for additional anti-inflammatory control.