Aminophyllin 25mg/ml Inj, 20ml

Manufacturer HOSPIRA Active Ingredient Aminophylline(am in OFF i lin) Pronunciation am-in-OFF-i-lin
It is used to treat breathing problems. It may be given to you for other reasons. Talk with the doctor.
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Drug Class
Bronchodilator
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Pharmacologic Class
Xanthine derivative; Phosphodiesterase inhibitor; Adenosine receptor antagonist
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Pregnancy Category
Category C
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FDA Approved
Jan 1970
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Aminophylline is a medicine given by injection to help open up the airways in your lungs, making it easier to breathe. It's often used for severe asthma or other breathing problems. It works by relaxing the muscles around your airways and reducing inflammation.
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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 is 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 proper storage method.

Missing a Dose

If you miss a dose, contact your doctor to receive guidance on what to do next.
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Lifestyle & Tips

  • Avoid or limit caffeine intake (coffee, tea, soda, chocolate) as it can increase side effects like nervousness and heart palpitations.
  • Inform your doctor about all medications, supplements, and herbal products you are taking, as many can interact with aminophylline.
  • Do not smoke or stop smoking without discussing with your doctor, as smoking significantly affects how your body processes this medication.
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Available Forms & Alternatives

Dosing & Administration

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Adult Dosing

Standard Dose: Loading dose: 5-6 mg/kg IV over 20-30 minutes (based on ideal body weight). Maintenance dose: 0.5-0.7 mg/kg/hr IV infusion. Adjust based on clinical response and serum theophylline levels.
Dose Range: 0.5 - 0.7 mg

Condition-Specific Dosing:

smokers: Higher maintenance dose (e.g., 0.9 mg/kg/hr) due to increased clearance.
heartFailure: Lower maintenance dose (e.g., 0.2-0.3 mg/kg/hr) due to decreased clearance.
liverDisease: Lower maintenance dose (e.g., 0.2-0.3 mg/kg/hr) due to decreased clearance.
elderly: Lower maintenance dose (e.g., 0.3-0.6 mg/kg/hr) due to decreased clearance.
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Pediatric Dosing

Neonatal: Loading dose: 5-6 mg/kg IV over 20-30 minutes. Maintenance dose: 0.2 mg/kg/hr for 0-24 weeks post-natal age; 0.25 mg/kg/hr for 24-52 weeks post-natal age. Highly individualized due to variable clearance.
Infant: Loading dose: 5-6 mg/kg IV over 20-30 minutes. Maintenance dose: 0.4-0.7 mg/kg/hr (6-52 weeks).
Child: Loading dose: 5-6 mg/kg IV over 20-30 minutes. Maintenance dose: 0.8-1 mg/kg/hr (1-9 years); 0.7 mg/kg/hr (9-12 years).
Adolescent: Loading dose: 5-6 mg/kg IV over 20-30 minutes. Maintenance dose: 0.5-0.7 mg/kg/hr (12-16 years, non-smokers).
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Dose Adjustments

Renal Impairment:

Mild: No specific dose adjustment for theophylline itself, but monitor for accumulation of active metabolites (e.g., 3-methylxanthine).
Moderate: No specific dose adjustment for theophylline itself, but monitor for accumulation of active metabolites.
Severe: No specific dose adjustment for theophylline itself, but monitor for accumulation of active metabolites. Consider lower end of maintenance dose range.
Dialysis: Theophylline is dialyzable. Supplemental dosing may be required after hemodialysis. Peritoneal dialysis removes less. Monitor levels closely.

Hepatic Impairment:

Mild: Reduce maintenance dose by 25-50%. Monitor serum theophylline levels closely.
Moderate: Reduce maintenance dose by 50% or more. Monitor serum theophylline levels closely.
Severe: Reduce maintenance dose by 50-75%. Monitor serum theophylline levels closely. Avoid if possible.

Pharmacology

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Mechanism of Action

Aminophylline is a salt of theophylline, a xanthine derivative. Its primary mechanism of action is non-selective inhibition of phosphodiesterase (PDE), leading to increased intracellular cyclic AMP (cAMP) levels. This results in bronchodilation by relaxing bronchial smooth muscle. It also acts as an adenosine receptor antagonist, which may contribute to its bronchodilatory and anti-inflammatory effects. Additionally, it can enhance diaphragmatic contractility and stimulate the respiratory center.
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Pharmacokinetics

Absorption:

Bioavailability: 100% (IV)
Tmax: Not applicable (IV)
FoodEffect: Not applicable (IV)

Distribution:

Vd: 0.45 L/kg (range 0.3-0.7 L/kg)
ProteinBinding: 40-60%
CnssPenetration: Yes

Elimination:

HalfLife: Adults: 3-12 hours (non-smokers); Children: 1-5 hours; Neonates: 10-30 hours (highly variable based on age, smoking status, liver/heart function, and concomitant medications).
Clearance: Highly variable (e.g., 0.65 mL/min/kg in healthy adults, higher in smokers, lower in liver/heart failure).
ExcretionRoute: Renal (primarily as metabolites)
Unchanged: Approximately 10% (adults); higher in neonates (up to 50%).
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Pharmacodynamics

OnsetOfAction: Rapid (within minutes of IV administration)
PeakEffect: Within 30 minutes to 2 hours after IV administration (when steady state is approached)
DurationOfAction: Dependent on half-life, typically 4-8 hours for a single dose, but continuous infusion maintains effect.
Confidence: High

Safety & Warnings

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Side Effects

Urgent Side Effects: Seek Medical Help Right Away

While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:

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
+ An irregular 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. Although 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 unusual symptoms that bother you or persist, 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, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
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Seek Immediate Medical Attention If You Experience:

  • Severe nausea or vomiting
  • Persistent headache
  • Restlessness or irritability
  • Tremors or shaking
  • Fast or irregular heartbeat (palpitations)
  • Seizures (rare, but serious)
  • Confusion
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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 it is safe to take this medication with all your current medications and health conditions. Never start, stop, or change the dose of any medication without first consulting your doctor.
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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 this may require an adjustment to your medication dosage. 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 increased 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.
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Overdose Information

Overdose Symptoms:

  • Severe nausea and vomiting (often intractable)
  • Gastrointestinal bleeding
  • Severe headache
  • Agitation, irritability, restlessness
  • Tremors, muscle twitching
  • Hyperthermia
  • Tachycardia, supraventricular and ventricular arrhythmias
  • Hypotension
  • Seizures (generalized tonic-clonic)
  • Rhabdomyolysis
  • Hypokalemia
  • Metabolic acidosis

What to Do:

Seek immediate medical attention. Call 911 or your local emergency number. For advice, call a poison control center at 1-800-222-1222. Treatment may involve activated charcoal, gastric lavage, antiarrhythmics, anticonvulsants, and supportive care. Hemoperfusion or hemodialysis may be used for severe, life-threatening toxicity.

Drug Interactions

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Major Interactions

  • Adenosine (reduced effectiveness of adenosine)
  • Cimetidine (increased theophylline levels)
  • Ciprofloxacin (increased theophylline levels)
  • Erythromycin (increased theophylline levels)
  • Fluvoxamine (increased theophylline levels)
  • Zileuton (increased theophylline levels)
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Moderate Interactions

  • Allopurinol (high doses, increased theophylline levels)
  • Beta-blockers (antagonistic effects)
  • Carbamazepine (decreased theophylline levels)
  • Furosemide (increased theophylline levels, variable)
  • Lithium (decreased lithium levels)
  • Phenobarbital (decreased theophylline levels)
  • Phenytoin (decreased theophylline levels)
  • Rifampin (decreased theophylline levels)
  • St. John's Wort (decreased theophylline levels)
  • Thyroid hormones (increased theophylline clearance)
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Minor Interactions

  • Caffeine (additive CNS stimulation)
  • Oral contraceptives (increased theophylline levels, variable)

Monitoring

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Baseline Monitoring

Patient history (smoking status, liver/heart disease, concomitant medications)

Rationale: To determine appropriate initial dosing and identify potential drug interactions or conditions affecting clearance.

Timing: Prior to initiation of therapy

Baseline vital signs (heart rate, blood pressure)

Rationale: To establish baseline and monitor for cardiovascular adverse effects.

Timing: Prior to initiation of therapy

ECG

Rationale: To assess for pre-existing arrhythmias, especially in patients with cardiac disease.

Timing: Prior to initiation of therapy, especially in patients with cardiac risk factors

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Routine Monitoring

Serum Theophylline Levels

Frequency: Initially 24 hours after starting continuous infusion or 3 days after starting oral therapy, then as needed based on clinical response, dose changes, or suspected toxicity/inefficacy.

Target: 5-15 mcg/mL (for asthma/COPD, to minimize toxicity); 10-20 mcg/mL (historical, but often associated with higher toxicity risk).

Action Threshold: Levels >20 mcg/mL increase risk of toxicity; >30 mcg/mL associated with severe toxicity (seizures, arrhythmias). Adjust dose if outside target range.

Vital Signs (heart rate, blood pressure)

Frequency: Regularly during IV infusion, then as clinically indicated.

Target: Within normal limits for patient.

Action Threshold: Significant tachycardia, arrhythmias, or hypotension may indicate toxicity.

Electrolytes (Potassium, Magnesium)

Frequency: Periodically, especially in patients on diuretics or with risk factors for electrolyte imbalance.

Target: Within normal limits.

Action Threshold: Hypokalemia or hypomagnesemia can exacerbate cardiac toxicity.

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Symptom Monitoring

  • Nausea
  • Vomiting
  • Diarrhea
  • Headache
  • Insomnia
  • Irritability
  • Tremor
  • Palpitations
  • Seizures (severe toxicity)
  • Cardiac arrhythmias (severe toxicity)

Special Patient Groups

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Pregnancy

Aminophylline (theophylline) crosses the placenta. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Neonates exposed in utero may experience irritability, vomiting, and tachycardia. Monitor maternal and fetal heart rates.

Trimester-Specific Risks:

First Trimester: Limited data, but generally avoided unless clearly necessary.
Second Trimester: May be used if benefits outweigh risks, with careful monitoring.
Third Trimester: May be used, but monitor neonate for signs of toxicity (irritability, vomiting, tachycardia, apnea) as clearance is reduced in neonates.
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Lactation

Theophylline is excreted into breast milk. Infants may experience irritability, jitteriness, and poor sleep. Monitor breastfed infants for signs of toxicity. Consider alternative bronchodilators or administer theophylline immediately after breastfeeding to minimize infant exposure.

Infant Risk: Moderate risk (L3) - potential for infant irritability, jitteriness, poor sleep, and rarely, signs of toxicity if maternal levels are high.
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Pediatric Use

Dosing is highly individualized and complex due to significant age-related differences in metabolism and clearance. Neonates and young infants have significantly reduced clearance and prolonged half-lives, requiring lower doses and careful monitoring. Children (1-9 years) often have faster clearance than adults and may require higher mg/kg doses. Therapeutic drug monitoring is essential.

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Geriatric Use

Elderly patients may have reduced hepatic clearance of theophylline, leading to increased serum concentrations and a higher risk of toxicity. Start with lower doses and titrate slowly based on serum levels and clinical response. Monitor closely for adverse effects, especially cardiovascular and CNS effects.

Clinical Information

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Clinical Pearls

  • Aminophylline has a narrow therapeutic index; therapeutic drug monitoring (TDM) of serum theophylline levels is crucial for safe and effective use.
  • Many factors influence theophylline clearance, including age, smoking status, liver/heart disease, and concomitant medications, necessitating individualized dosing.
  • Toxicity symptoms can mimic underlying disease exacerbation (e.g., nausea, vomiting, tremor). Always consider toxicity when symptoms worsen or new symptoms appear.
  • IV aminophylline should be administered slowly via infusion pump to avoid rapid increases in serum levels and associated adverse effects (e.g., hypotension, arrhythmias).
  • Conversion from aminophylline to theophylline: 100 mg aminophylline is approximately equivalent to 79-86 mg anhydrous theophylline. Dosing is typically based on aminophylline salt, but serum levels reflect theophylline.
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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.
  • Inhaled corticosteroids (e.g., fluticasone, budesonide) for anti-inflammatory effects in asthma/COPD.
  • Systemic corticosteroids (e.g., prednisone, methylprednisolone) for acute exacerbations.
  • Anticholinergics (e.g., ipratropium, tiotropium) for bronchodilation, especially in COPD.
  • Leukotriene receptor antagonists (e.g., montelukast) for asthma maintenance.
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Cost & Coverage

Average Cost: Variable, typically low per 20ml vial
Generic Available: Yes
Insurance Coverage: Tier 1 or 2 (Generic)
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General Drug Facts

If your symptoms or health problems persist or worsen, it is essential to contact your doctor promptly. To ensure safe use, never share your medication with others, and do not take medication prescribed for someone else. Store all medications in a secure location, out of reach of children and pets, to prevent accidental ingestion. Dispose of unused or expired medications properly. Unless instructed to do so by a healthcare professional, do not flush medications down the toilet or pour them down the drain. If you are unsure about the correct disposal method, consult your pharmacist, who can also inform you about potential drug take-back programs in your area. Some medications may come with an additional patient information leaflet, which your pharmacist can provide. If you have any questions or concerns about your medication, discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately contact your local poison control center or seek emergency medical attention. Be prepared to provide information about the medication taken, the amount, and the time it occurred.