Active Substance: Lisinopril (as dihydrate).
Overview
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This medicine contains an important and useful components, as it consists of
Lisinopril (as dihydrate)is available in the market in concentration
Aminophylline
- **Caution in Patients with Heart Issues**: Aminophylline should be used with caution in patients with a history of heart disease, particularly arrhythmias and heart failure, as it can potentially exacerbate these conditions. - **Liver Dysfunction**: In cases of impaired liver function, dosage adjustments may be necessary because the drug is metabolized in the liver. Regular liver function tests should be conducted. - **Renal Impairment**: It’s essential to monitor renal function closely in patients with renal impairment, as the drug is excreted through the kidneys, and reduced kidney function may lead to increased drug levels and potential toxicity. - **Epilepsy and Seizures**: Aminophylline can lower the seizure threshold, so it should be used with caution in patients with epilepsy or a history of seizures. - **Pregnancy**: It falls under the FDA pregnancy category C, which means that while it may be prescribed during pregnancy, only if clearly needed, it should be used under strict medical supervision. - **Breastfeeding**: Aminophylline passes into breast milk, and although no significant adverse effects have been reported, its use in breastfeeding mothers should be approached cautiously and only when absolutely necessary. - **Elderly Patients**: Older adults may be more sensitive to the effects of aminophylline, particularly its cardiovascular and central nervous system effects. Close monitoring and dose adjustments may be required.
- **Chronic Obstructive Pulmonary Disease (COPD)**: Aminophylline is commonly used as an adjunct in managing the symptoms of COPD, particularly for relief from bronchospasm and as a bronchodilator. - **Asthma**: Aminophylline is indicated for the treatment of asthma, especially in patients who do not respond well to conventional bronchodilators or corticosteroids. - **Acute Bronchospasm**: In cases of acute exacerbation of asthma or other chronic lung diseases, aminophylline can be used to relax bronchial smooth muscles and facilitate airflow. - **Apnea in Premature Infants**: Aminophylline has been used in neonatal care to treat apnea in premature infants by stimulating respiratory drive. - **Other Respiratory Conditions**: It may also be considered in managing respiratory distress syndromes, such as in conditions of premature infants and other conditions where increased bronchodilation is beneficial.
- **Hypersensitivity**: Contraindicated in patients who are hypersensitive to aminophylline, theophylline, or any other methylxanthines. - **Severe Heart Disease**: Contraindicated in patients with severe coronary artery disease or those with arrhythmias that cannot be controlled by other means. - **Severe Liver or Kidney Dysfunction**: Due to its metabolism in the liver and excretion through the kidneys, aminophylline is contraindicated in patients with severe hepatic or renal failure. - **Peptic Ulcer Disease**: Patients with active peptic ulcers should avoid aminophylline as it may exacerbate the condition due to its stimulating effects on gastric acid secretion. - **Severe Seizure Disorders**: Since aminophylline can lower the seizure threshold, its use is contraindicated in patients with a history of severe or uncontrolled seizures. - **Hyperthyroidism**: Due to its stimulant effects, aminophylline should be avoided in patients with hyperthyroidism as it may exacerbate symptoms such as tachycardia and nervousness.
- **Common Side Effects**: - Nausea and vomiting - Headache - Insomnia - Dizziness - Tremors - Tachycardia (increased heart rate) - Palpitations - Gastrointestinal upset - **Serious Side Effects**: - Seizures (due to CNS stimulation) - Cardiac arrhythmias, including ventricular arrhythmias - Hypotension or hypertension - Hypokalemia (low potassium levels) - Hepatotoxicity (liver damage) - Renal impairment - **Allergic Reactions**: - Rash - Itching - Anaphylaxis (though rare) - **Drug Toxicity**: - Signs of aminophylline toxicity include nausea, vomiting, diarrhea, tachycardia, seizures, and in severe cases, cardiac arrest. - Increased plasma concentration of the drug, particularly when the drug is taken with interacting agents, can increase the risk of toxicity.
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- **Bronchodilation**: Aminophylline works by relaxing bronchial smooth muscles, thereby widening the airways, making it easier to breathe. This is especially beneficial in respiratory conditions like asthma and COPD. - **Phosphodiesterase Inhibition**: Aminophylline is a phosphodiesterase inhibitor. It inhibits the breakdown of cyclic AMP (cAMP), increasing intracellular cAMP levels, which leads to smooth muscle relaxation and vasodilation. - **Anti-inflammatory Effects**: By increasing cAMP, aminophylline can also reduce the inflammatory response in the airways, helping reduce swelling and mucus production in the lungs. - **Central Nervous System Stimulation**: Aminophylline has mild CNS stimulant effects, which may contribute to its ability to improve respiratory drive in conditions like apnea in premature infants. - **Diuretic Effect**: Due to its action on the kidneys, aminophylline can cause increased urine production, which is a mild diuretic effect. This can help in cases of fluid retention.
- **Drug Interactions**: - **Cimetidine**: Cimetidine can increase the plasma concentration of aminophylline, raising the risk of toxicity. Monitoring and dose adjustment are necessary. - **Antibiotics (e.g., Erythromycin, Ciprofloxacin)**: Certain antibiotics, especially macrolides like erythromycin, and fluoroquinolones like ciprofloxacin, can increase aminophylline levels, leading to potential toxicity. - **Beta-blockers**: When combined with beta-blockers, aminophylline's bronchodilatory effects may be reduced, as beta-blockers can cause bronchoconstriction. - **Anticonvulsants (e.g., Phenytoin, Phenobarbital)**: These drugs can reduce the effectiveness of aminophylline by increasing its metabolism, thereby lowering its plasma concentration. - **Alcohol**: Alcohol consumption may potentiate the CNS side effects of aminophylline, such as dizziness and drowsiness, and increase the risk of dehydration and electrolyte disturbances. - **Other Xanthines (e.g., Theophylline)**: Taking other xanthines alongside aminophylline can increase the risk of toxicity due to additive effects on the central nervous system and heart.
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- **Initial Dosage**: - The usual loading dose is 6 mg/kg body weight, given intravenously (IV), followed by a maintenance dose. - **Maintenance Dose**: - The typical maintenance dose ranges from 0.5 mg/kg/hr to 1 mg/kg/hr, administered intravenously. The exact dose depends on the patient’s age, condition, and response to therapy. - Oral doses range from 400 mg to 800 mg per day, divided into two to three doses. The dose may need to be adjusted based on the patient's therapeutic response and serum drug levels. - **Adjustments**: - In patients with liver or kidney dysfunction, dose reductions may be necessary, and therapeutic drug monitoring is essential. - Plasma levels should ideally be maintained between 10-20 mcg/mL to avoid toxicity.
- **For Asthma or COPD**: - Initial IV dose: 5 mg/kg as a loading dose, followed by a maintenance infusion of 0.5-1 mg/kg/hr, depending on the child's response. - Oral doses: Typically range from 10-15 mg/kg per day, divided into two or three doses. - **For Apnea in Premature Infants**: - The usual starting dose is 3 mg/kg IV, which can be repeated after 24 hours if necessary. - The maintenance dose for premature infants is often around 1 mg/kg every 6 to 8 hours, with adjustments based on clinical response.
- **Renal Impairment**: - In patients with renal insufficiency, aminophylline should be used with caution. - Dosing adjustments may be needed based on the severity of renal dysfunction. In cases of significant renal impairment (e.g., in patients with chronic kidney disease), the usual dose of aminophylline should be reduced. - Monitoring of drug levels and renal function is recommended to avoid accumulation and toxicity. - **Dialysis**: Aminophylline is dialyzable, and in cases of severe overdose or toxicity, hemodialysis may help remove the drug from the system.
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