Aminophylline 25mg/ml Inj, 10ml
It is used to treat breathing problems. It may be given to you for other reasons. Talk with the doctor.
Drug Class
Bronchodilator
Pharmacologic Class
Xanthine Derivative
Pregnancy Category
C
FDA Approved
Jan 1970
DEA Schedule
Not Controlled
Overview
What is this medicine?
Aminophylline is a medicine given by injection (into a vein) to help open up the airways in your lungs. This makes it easier to breathe, especially during severe asthma attacks or flare-ups of chronic lung conditions like COPD. It works by relaxing the muscles around your airways and reducing inflammation.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. It's essential to follow the instructions carefully. This medication is administered as an infusion into a vein over a period of time.
Storing and Disposing of Your Medication
If you need to store this medication at home, consult with your doctor, nurse, or pharmacist to determine the best storage method.
Missing a Dose
If you miss a dose, contact your doctor to receive guidance on what to do next.
To use this medication correctly, follow your doctor's instructions and read all the information provided. It's essential to follow the instructions carefully. This medication is administered as an infusion into a vein over a period of time.
Storing and Disposing of Your Medication
If you need to store this medication at home, consult with your doctor, nurse, or pharmacist to determine the best storage method.
Missing a Dose
If you miss a dose, contact your doctor to receive guidance on what to do next.
Lifestyle & Tips
- Avoid caffeine-containing products (e.g., coffee, tea, cola, chocolate) as they can increase the risk of side effects like nervousness, tremors, and heart palpitations.
- Inform your doctor if you smoke, as smoking can significantly affect how your body processes this medication, requiring dose adjustments.
- Report any new medications, over-the-counter drugs, or herbal supplements to your healthcare provider, as many can interact with aminophylline.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
Loading dose: 5-6 mg/kg IV over 20-30 minutes (if not on theophylline). Maintenance dose: 0.5-0.7 mg/kg/hr IV infusion, adjusted based on clinical response and serum levels.
Dose Range:
0.2 - 1 mg
Condition-Specific Dosing:
nonSmokerHealthy:
0.5 mg/kg/hr
smoker:
0.8 mg/kg/hr
congestiveHeartFailure:
0.2-0.3 mg/kg/hr
liverDisease:
0.2-0.3 mg/kg/hr
Pediatric Dosing
Neonatal:
Loading dose: 5-6 mg/kg IV over 20-30 minutes. Maintenance dose: 0.2 mg/kg/hr IV infusion. Monitor serum levels closely due to highly variable and prolonged half-life.
Infant:
Loading dose: 5-6 mg/kg IV over 20-30 minutes. Maintenance dose (6 weeks-6 months): 0.5 mg/kg/hr IV infusion. Monitor serum levels closely.
Child:
Loading dose: 5-6 mg/kg IV over 20-30 minutes. Maintenance dose (1-9 years): 0.8-1 mg/kg/hr IV infusion. Monitor serum levels closely.
Adolescent:
Loading dose: 5-6 mg/kg IV over 20-30 minutes. Maintenance dose (9-16 years): 0.7 mg/kg/hr IV infusion. Monitor serum levels closely.
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment required, but monitor for accumulation of active metabolites.
Moderate:
No specific dose adjustment required, but monitor for accumulation of active metabolites.
Severe:
No specific dose adjustment required, but monitor for accumulation of active metabolites and increased sensitivity to adverse effects.
Dialysis:
Theophylline is dialyzable. Supplemental dosing may be required after hemodialysis. Monitor serum levels.
Hepatic Impairment:
Mild:
Consider 25% reduction in maintenance dose. Monitor serum levels closely.
Moderate:
Reduce maintenance dose by 25-50%. Monitor serum levels closely.
Severe:
Reduce maintenance dose by 50-75%. Monitor serum levels closely and frequently.
Pharmacology
Mechanism of Action
Aminophylline is a salt of theophylline, a xanthine derivative. Its primary mechanisms of action include non-selective phosphodiesterase inhibition (leading to increased intracellular cAMP, resulting in bronchodilation and anti-inflammatory effects), adenosine receptor antagonism (blocking bronchoconstriction and inflammatory mediator release), and enhancement of histone deacetylase activity (reducing inflammatory gene expression).
Pharmacokinetics
Absorption:
Bioavailability:
100%
Tmax:
Not applicable (IV administration)
FoodEffect:
Not applicable (IV administration)
Distribution:
Vd:
0.4-0.6 L/kg
ProteinBinding:
40-60%
CnssPenetration:
Yes
Elimination:
HalfLife:
Highly variable: Adults (non-smokers): 7-12 hours; Children (1-9 years): 2-5 hours; Neonates: 10-30 hours; Smokers: 4-5 hours; Patients with CHF/liver disease: 15-30 hours.
Clearance:
0.04-0.06 L/kg/hr (variable based on age, smoking, disease states)
ExcretionRoute:
Renal (primarily as metabolites)
Unchanged:
Approximately 10% (adults)
Pharmacodynamics
OnsetOfAction:
Rapid (within minutes) after IV administration
PeakEffect:
30-60 minutes after IV administration
DurationOfAction:
Varies with half-life, typically 4-8 hours in adults with normal clearance
Confidence:
Medium
Safety & Warnings
Side Effects
Serious Side Effects: Seek Medical Help Immediately
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical attention right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of low potassium levels, including:
+ Muscle pain or weakness
+ Muscle cramps
+ Abnormal heartbeat
Signs of high blood sugar, such as:
+ Confusion
+ Feeling sleepy
+ Unusual thirst or hunger
+ Frequent urination
+ Flushing
+ Rapid breathing
+ Fruity-smelling breath
Muscle pain or weakness
Fast or abnormal heartbeat
Severe dizziness or fainting
Upset stomach or vomiting
Irritability
Seizures
Shakiness
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor:
Restlessness
Headache
Trouble sleeping
Stomach pain or diarrhea
* Frequent urination
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical attention right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of low potassium levels, including:
+ Muscle pain or weakness
+ Muscle cramps
+ Abnormal heartbeat
Signs of high blood sugar, such as:
+ Confusion
+ Feeling sleepy
+ Unusual thirst or hunger
+ Frequent urination
+ Flushing
+ Rapid breathing
+ Fruity-smelling breath
Muscle pain or weakness
Fast or abnormal heartbeat
Severe dizziness or fainting
Upset stomach or vomiting
Irritability
Seizures
Shakiness
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor:
Restlessness
Headache
Trouble sleeping
Stomach pain or diarrhea
* Frequent urination
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Severe or persistent nausea and vomiting
- Persistent headache
- Rapid or irregular heartbeat (palpitations)
- Tremors or shaking
- Restlessness or agitation
- Dizziness
- Seizures (rare but serious)
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced as a result of the allergy.
All medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This information will help your doctor and pharmacist assess potential interactions between this medication and other substances you are taking.
* Any existing health problems, as this medication may interact with certain conditions.
To ensure your safety, it is crucial to verify that this medication can be taken safely with all your current medications and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced as a result of the allergy.
All medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This information will help your doctor and pharmacist assess potential interactions between this medication and other substances you are taking.
* Any existing health problems, as this medication may interact with certain conditions.
To ensure your safety, it is crucial to verify that this medication can be taken safely with all your current medications and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. This drug may interfere with certain laboratory tests, so be sure to notify your healthcare providers and lab personnel that you are taking it.
Regular blood tests will be necessary, as directed by your doctor. Discuss any concerns or questions you have with your doctor. If you have diabetes, it is crucial to closely monitor your blood sugar levels while taking this medication.
To minimize potential side effects, limit your consumption of caffeine-containing products, such as tea, coffee, and cola, as well as chocolate, as combining these with this drug may cause nervousness, shakiness, and a rapid heartbeat. Before consuming alcohol, consult with your doctor to discuss any potential risks.
If you start or stop using tobacco or marijuana, inform your doctor, as your dosage may need to be adjusted. If you become ill, develop a fever, or experience a worsening of a chronic condition, consult with your doctor promptly.
Individuals 60 years of age or older should exercise caution when taking this medication, as they may be more susceptible to side effects. Similarly, if the patient is a child under 1 year of age, this medication should be used with caution, as the risk of side effects may be higher in this age group.
If you are pregnant, plan to become pregnant, or are breastfeeding, inform your doctor, as it is necessary to discuss the potential benefits and risks of this medication to both you and your baby.
Regular blood tests will be necessary, as directed by your doctor. Discuss any concerns or questions you have with your doctor. If you have diabetes, it is crucial to closely monitor your blood sugar levels while taking this medication.
To minimize potential side effects, limit your consumption of caffeine-containing products, such as tea, coffee, and cola, as well as chocolate, as combining these with this drug may cause nervousness, shakiness, and a rapid heartbeat. Before consuming alcohol, consult with your doctor to discuss any potential risks.
If you start or stop using tobacco or marijuana, inform your doctor, as your dosage may need to be adjusted. If you become ill, develop a fever, or experience a worsening of a chronic condition, consult with your doctor promptly.
Individuals 60 years of age or older should exercise caution when taking this medication, as they may be more susceptible to side effects. Similarly, if the patient is a child under 1 year of age, this medication should be used with caution, as the risk of side effects may be higher in this age group.
If you are pregnant, plan to become pregnant, or are breastfeeding, inform your doctor, as it is necessary to discuss the potential benefits and risks of this medication to both you and your baby.
Overdose Information
Overdose Symptoms:
- Severe nausea and vomiting (often intractable)
- Persistent headache
- Restlessness, agitation, irritability
- Tremors, muscle twitching
- Hyperthermia
- Tachycardia (rapid heart rate)
- Cardiac arrhythmias (e.g., supraventricular tachycardia, ventricular ectopy, ventricular fibrillation)
- Hypotension (low blood pressure)
- Seizures (generalized tonic-clonic)
- Hypokalemia
- Hyperglycemia
- Metabolic acidosis
What to Do:
Immediately stop the aminophylline infusion. Seek emergency medical attention. Management is supportive and may include activated charcoal (if recent oral ingestion), antiemetics for nausea/vomiting, benzodiazepines for seizures, antiarrhythmics for cardiac dysrhythmias, and correction of electrolyte imbalances (e.g., potassium). Hemoperfusion or hemodialysis may be considered in severe, life-threatening toxicity.
Drug Interactions
Contraindicated Interactions
- Tizanidine (due to significant increase in tizanidine levels via CYP1A2 inhibition)
Major Interactions
- Cimetidine (increases aminophylline levels)
- Ciprofloxacin (increases aminophylline levels)
- Erythromycin (increases aminophylline levels)
- Fluvoxamine (increases aminophylline levels)
- Propranolol (increases aminophylline levels and antagonizes bronchodilation)
- Phenytoin (decreases aminophylline levels)
- Rifampin (decreases aminophylline levels)
- Phenobarbital (decreases aminophylline levels)
- Carbamazepine (decreases aminophylline levels)
Moderate Interactions
- Allopurinol (high doses, increases aminophylline levels)
- Oral contraceptives (increase aminophylline levels)
- Verapamil (increases aminophylline levels)
- Diltiazem (increases aminophylline levels)
- Influenza vaccine (may increase aminophylline levels)
- Isoniazid (may decrease aminophylline levels)
- Lithium (aminophylline may decrease lithium levels)
Minor Interactions
- Not typically categorized for aminophylline due to narrow therapeutic index and significant interactions.
Monitoring
Baseline Monitoring
Theophylline serum concentration
Rationale: To guide initial dosing, especially if patient has received theophylline within 24 hours.
Timing: Before starting infusion, if recent theophylline use.
Liver function tests (LFTs)
Rationale: Aminophylline is primarily metabolized by the liver; hepatic impairment requires dose adjustment.
Timing: Prior to initiation.
Renal function tests (RFTs)
Rationale: To assess kidney function, though renal excretion of unchanged drug is minor, metabolites are renally cleared.
Timing: Prior to initiation.
Baseline ECG
Rationale: To assess for pre-existing arrhythmias, as aminophylline can cause cardiac effects.
Timing: Prior to initiation.
Routine Monitoring
Theophylline serum concentration
Frequency: Initially 30 minutes after loading dose, then 12-24 hours after starting maintenance infusion or with any dose change. Subsequently, every 24 hours or as clinically indicated.
Target: 10-20 mcg/mL (for bronchodilation); 5-15 mcg/mL (for COPD)
Action Threshold: Levels >20 mcg/mL indicate potential toxicity; levels <10 mcg/mL may indicate subtherapeutic effect. Adjust dose accordingly.
Vital signs (heart rate, blood pressure, respiratory rate)
Frequency: Every 1-4 hours, or as per institutional protocol for IV infusions.
Target: Normal physiological ranges
Action Threshold: Significant tachycardia, arrhythmias, hypotension, or increased respiratory distress.
ECG monitoring
Frequency: Continuous or frequent intermittent monitoring, especially in patients with cardiac disease or signs of toxicity.
Target: Normal sinus rhythm
Action Threshold: Development of arrhythmias (e.g., supraventricular tachycardia, ventricular ectopy).
Electrolytes (especially potassium)
Frequency: Daily or as clinically indicated.
Target: Normal serum potassium levels (3.5-5.0 mEq/L)
Action Threshold: Hypokalemia (may be exacerbated by aminophylline).
Symptom Monitoring
- Nausea
- Vomiting
- Headache
- Insomnia
- Restlessness
- Tremors
- Palpitations
- Dizziness
- Seizures
- Cardiac arrhythmias
Special Patient Groups
Pregnancy
Aminophylline is classified as Pregnancy Category C. It crosses the placenta. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Maternal serum levels should be monitored closely, as clearance may be altered during pregnancy.
Trimester-Specific Risks:
First Trimester:
Limited data, but potential for fetal exposure.
Second Trimester:
Potential for fetal exposure; monitor maternal levels.
Third Trimester:
Potential for fetal exposure; clearance may be reduced in late pregnancy, increasing maternal and fetal levels. Neonatal irritability and tachycardia have been reported.
Lactation
Aminophylline is excreted into breast milk. The American Academy of Pediatrics considers theophylline (and thus aminophylline) to be compatible with breastfeeding, but caution is advised. Monitor breastfed infants for signs of toxicity.
Infant Risk:
L3 (Moderately Safe). Potential for infant irritability, insomnia, jitteriness, and tachycardia. Monitor infant for signs of toxicity, especially in neonates or if maternal levels are high.
Pediatric Use
Pediatric patients, especially neonates and infants, have highly variable pharmacokinetics and significantly reduced clearance compared to older children and adults. This necessitates individualized dosing, careful titration, and frequent monitoring of serum aminophylline levels to avoid toxicity due to the narrow therapeutic index.
Geriatric Use
Geriatric patients may have reduced hepatic clearance of aminophylline, leading to increased serum concentrations and a higher risk of adverse effects. Start with lower doses and titrate slowly based on clinical response and serum levels. Monitor closely for signs of toxicity, particularly cardiac and CNS effects.
Clinical Information
Clinical Pearls
- Aminophylline has a narrow therapeutic index; therapeutic and toxic doses are very close. Serum level monitoring is essential for safe and effective use.
- Many factors influence aminophylline clearance, including age, smoking status, diet, and concomitant medications. Individualize dosing and monitor closely.
- Due to its narrow therapeutic index and the availability of safer, more effective bronchodilators (e.g., beta-agonists, corticosteroids), aminophylline is now less commonly used and typically reserved for severe cases or when other therapies are inadequate.
- Patients should be advised to avoid or limit caffeine intake during aminophylline therapy to prevent additive CNS and cardiac stimulation.
- Be vigilant for signs of toxicity, which can range from mild GI upset and headache to life-threatening arrhythmias and seizures.
Alternative Therapies
- Short-acting beta-2 agonists (e.g., albuterol, levalbuterol) for acute bronchospasm.
- Long-acting beta-2 agonists (e.g., salmeterol, formoterol) for maintenance therapy.
- Systemic corticosteroids (e.g., prednisone, methylprednisolone) for acute exacerbations.
- Inhaled corticosteroids (e.g., fluticasone, budesonide) for maintenance therapy.
- Anticholinergics (e.g., ipratropium, tiotropium) for COPD and some asthma cases.
Cost & Coverage
Average Cost:
Varies widely, typically low per 10ml vial
Generic Available:
Yes
Insurance Coverage:
Tier 1 or 2 (generic)
General Drug Facts
If your symptoms or health problems persist or worsen, it is essential to contact your doctor for further evaluation and guidance. To ensure safe and effective treatment, never share your medication with others, and do not take medication prescribed for someone else.
Store all medications in a secure location, out of the reach of children and pets, to prevent accidental ingestion. Properly dispose of unused or expired medications by checking with your pharmacist for guidance on the best disposal method. Unless instructed to do so, avoid flushing medications down the toilet or pouring them down the drain, as this can harm the environment. Many communities have drug take-back programs, which your pharmacist can help you locate.
Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about your medication, consult with your doctor, nurse, pharmacist, or other healthcare provider.
In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. Be prepared to provide critical information, including the name of the medication, the amount taken, and the time it was taken, to ensure prompt and effective treatment.
Store all medications in a secure location, out of the reach of children and pets, to prevent accidental ingestion. Properly dispose of unused or expired medications by checking with your pharmacist for guidance on the best disposal method. Unless instructed to do so, avoid flushing medications down the toilet or pouring them down the drain, as this can harm the environment. Many communities have drug take-back programs, which your pharmacist can help you locate.
Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about your medication, consult with your doctor, nurse, pharmacist, or other healthcare provider.
In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. Be prepared to provide critical information, including the name of the medication, the amount taken, and the time it was taken, to ensure prompt and effective treatment.