aminofilina

What is aminophylline?

 

Aminophylline is a bronchodilator.

Aminophylline works in several ways: it relaxes the muscles of the lungs and thorax to allow more air to enter, decreases the sensitivity of the lungs to allergens and other substances that cause inflammation, and increases the contractions of the diaphragm to attract more air to the lungs. lungs

 

Description.

Aminophylline is converted to Theophylline systemically; 1 mg of aminophylline = 0.8 mg of Theophylline.

Bronchodilator and anti-inflammatory effects; respiratory, cardiac, and CNS stimulant

 

Uses of aminophylline:

Aminophylline is used to treat breathing problems: the symptoms of asthma, bronchitis, and emphysema.

This medication should not be used to treat severe outbreaks of difficulty breathing.

 

 

What should I know about aminophylline?

Do not crush or chew any prolonged-release formulation of aminophylline. Swallow the entire medication. It is specially formulated to release slowly into your body.

Ask your pharmacist if you do not know if your medication is a prolonged-release formulation.

Call your doctor immediately if you have nausea, vomiting, insomnia, restlessness, seizures, increased heart rate, or headache. These could be signs of too much aminophylline in the blood.

Do not start or stop smoking without your doctor’s knowledge. Smoking can affect your dose.

Do not take more of this medication than prescribed without consulting your doctor. Seek medical attention if you have difficulty breathing.

 

Who should not take aminophylline?

Before taking this medication, tell your doctor if you have:

  • A stomach ulcer
  • Seizures or epilepsy.
  • High blood pressure, a heart problem, or any heart disease.
  • Fluid in your lungs.
  • A thyroid condition
  • Liver disease
  • Kidney disease

 

What should I avoid while taking aminophylline?

Be careful when driving, operating machinery, or performing other dangerous activities. Aminophylline may cause dizziness or drowsiness. If you experience dizziness or drowsiness, avoid these activities.

Do not start or stop smoking without your doctor’s approval. Smoking changes the way your body uses aminophylline and may need a dose adjustment.

Avoid changing your dose or changing the schedule of your daily doses.

Do not change the brand, generic form, or formulation (tablet, capsule, liquid) of aminophylline you are taking without your doctor’s approval. Different brands or formulations may require different doses.

Avoid eating excessive amounts of food on the grill or grill. Doing so can also change the dose of aminophylline you need.

Avoid drinks with caffeine such as coffee, tea, and cola drinks. Aminophylline is chemically related to caffeine, and you may experience some side effects if you consume too much caffeine.

 

Side effects of aminophylline.

If you experience any of the following serious side effects, stop taking aminophylline and seek emergency medical attention:

  • An allergic reaction (difficulty breathing, closing of the throat, swelling of the lips, tongue or face, or hives).
  • Convulsions
  • Increased or irregular heartbeat.
  • Severe nausea or vomiting.

 

Other, less serious side effects may also occur, although not expected at the appropriate doses. Continue to take aminophylline and talk to your doctor if you experience

  • Mild nausea
  • Decreased appetite or weight loss.
  • Restlessness, tremor, or insomnia.
  • Headache.
  • Stunning or dizziness

 

Dosage information of aminophylline.

The usual dose in adults for acute asthma:

Loading dose: 6 mg / kg in 100 to 200 ml IV fluid intravenously once for 20 to 30 minutes.

Maintenance dose (after loading dose):

otherwise healthy non-smokers: Adult: 0.7 mg / kg / h Continuous intravenous infusion

Young adult smoker: 0.9 mg / kg / h Continuous intravenous infusion

Patient with cor pulmonale or congestive heart failure: 0.25 mg / kg / h Continuous intravenous infusion

Oral: (Patient not receiving aminophylline or Theophylline)

Loading dose: 6.3 mg / kg orally once

Maintenance dose (after loading dose):

Healthy non-smoking adult: 12.5 mg / kg / day in divided doses. Do not exceed 1,125 mg / day.

Young adult smoker: 19 mg / kg / day in divided doses.

Patient with cor pulmonale or congestive heart failure: 6.25 mg/kg/day in divided doses.

Do not exceed 500 mg/day.

Usual geriatric dose for asthma – Acute:

Patient not receiving aminophylline or theophylline:

loading dose: 6 mg / kg in 100 to 200 ml IV fluid intravenously once for 20 to 30 minutes.

Maintenance dose (after loading dose): 0.2 to 0.3 mg / kg / h of continuous intravenous infusion.

Oral: patient not receiving aminophylline or Theophylline:

loading dose: 6.3 mg / kg orally once.

Maintenance dose (after loading dose): 1.7 to 2 mg/kg orally every 8 hours.

Usual pediatric dose for apnea of ​​prematurity:

<= four weeks: (IV or oral, all amounts based on aminophylline): loading dose: (patient not receiving aminophylline or Theophylline): 5 to 6 mg/kg once – if IV, dilute in IV fluid and Administer intravenously once to 30 minutes.

Maintenance dose: 3 to 8 mg / kg / day divided every 6 to 12 hours. Usual pediatric dose for asthma: acute: IV: (all doses are based on aminophylline and the patient not receiving aminophylline or Theophylline): Loading dose: 6 mg/kg diluted in IV liquid intravenously once for 20 30 minutes.

Maintenance dose (after loading dose): 6 weeks to 6 months: 0.5 mg / kg / hour of continuous intravenous infusion. 6 months to 1 year: 0.6 to 0.7 mg / kg / hour continuous intravenous infusion. 1 year to 9 years: 1 to 1.2 mg / kg / h continuous intravenous infusion.

9 years to 12 years: 0.9 mg / kg / h continuous intravenous infusion. > 12 years: 0.7 mg / kg / h of continuous intravenous infusion.

Oral: (patient not receiving aminophylline or Theophylline):

loading dose: 6.3 mg / kg orally once.

Maintenance dose (after loading dose):

> = 42 <182 days: 12 to 13.5 mg / kg / day in divided doses.

> = 6 <12 months: 15 to 22.5 mg / kg / day in divided doses. > = 1 year to <9 years: 25 to 30 mg / kg / day in divided doses.

> = 9 years to <12 years: 17 to 20 mg / kg / day in divided doses. > = 12 to <16 years: 15 to 17 mg / kg in divided doses. > = 16 years: 6.25 to 20 mg / kg divided orally every 6 hours.

 

What other drugs will affect aminophylline?

Aminophylline interacts with many other drugs. Tell your doctor and pharmacist about all other medications you are taking, including herbal remedies, vitamins, and other non-prescription items.

The following medications can increase the levels of aminophylline in the blood, which produces dangerous side effects:

Alcohol;

Cimetidina (Tagamet, Tagamet HB);

 

Fluoroquinolonic antibiotics such as enoxacin (Penetrex), lomefloxacin (Maxaquin), ciprofloxacin (Cipro), norfloxacin (Noroxin) and ofloxacin (Floxin);

  • Clarithromycin (Biaxin) and erythromycin (Ery-Tab, EES, E-Mycin, others).
  • Disulfiram (Antabuse).
  • Estrogens (Ogen, Premarin, and many other types).
  • Fluvoxamine (Luvox).
  • Metotrexato (Folex, Rheumatrex).
  • Mexiletine (Mexitil) y propafenone (Rythmol).
  • Propranolol (Inderal).
  • Tacrine (Cognex).
  • Ticlopidine (Ticlid).
  • Verapamil (Verelan, Calan, Isoptin).

 

The following drugs can lower the levels of aminophylline in your blood, leading to poor asthma control:

  • Aminoglutetimida (Cytadren).
  • Carbamazepina (Tegretol).
  • Isoproterenol (Isuprel).
  • Moricizine (Ethmozine).
  • Fenobarbital (Luminal, Solfoton).
  • Phenytoin (Dilantin)
  • Rifampin (Rifadin).
  • Sucralfate (Carafate).

In addition to the drugs mentioned above, others may also have interactions with aminophylline affecting your condition.

Talk to your doctor and pharmacist before taking any medication with or without a prescription.

 

Side effects of aminophylline

Applies to aminophylline: oral solution, oral tablet, extended-release tablet

Other dosage forms:

Intravenous solution

Along with its necessary effects, aminophylline can cause some unwanted effects. Although not all of these side effects can occur, if they do occur, they may need medical attention.

Check with your doctor immediately if you experience any of the following side effects while taking aminophylline:

  • Cracks in the skin.
  • Loss of body heat.
  • Red and swollen skin.
  • Scaly skin.
  • Acne.
  • Incidence unknown.
  • Breast pain or discomfort.
  • Dizziness.
  • Fainting.
  • Rapid, slow, or irregular heartbeat.
  • Increase in the volume of urine.
  • Daze.
  • Persistent vomiting
  • A solid or fast heartbeat.
  • Convulsions
  • Instability.

Get emergency help immediately if you have any of the following symptoms of overdose while taking aminophylline:

 

Symptoms of overdose

  • Abdominal or stomach pain, blurry vision.
  • Confusion.
  • Confusion about identity, place, and time.
  • Dark-colored urine.
  • Decrease in the frequency of urination.
  • Decrease in urine.
  • Diarrhea.
  • difficulty urinating (dribbling)
  • dizziness, fainting, or lightheadedness when suddenly rising from a lying or sitting.
  • Dry mouth.
  • Heartbeat or rapid, solid, or irregular pulses.
  • Increased thirst.
  • Irregular heartbeat.
  • Loss of appetite
  • humor changes.
  • Muscle cramps or spasms.
  • Muscle pain or stiffness.
  • Nausea or vomiting.
  • Nervousness.
  • Numbness or tingling in the hands, feet, or lips.
  • Pain or discomfort in the arms, jaw, back, or neck.
  • pain when urinating, tremors in the legs, arms, hands, or feet.
  • Difficulty breathing.
  • Perspiration.
  • unusual tiredness or weakness
  • Vomiting of blood or material that looks like ground coffee.
  • Fever.

 

Some side effects of aminophylline can occur and usually do not require medical attention. These side effects may go away during treatment as your body adjusts to the medication.

In addition, your health professional can tell you about ways to prevent or reduce some of these side effects.

 

Check with your healthcare professional if any of the following side effects continue or are bothersome or if you have any questions about them:

  • Headache.
  • Irritability.
  • Restlessness.
  • Insomnia.
  • Problems to sleep.

 

Maximum dosage

Theophylline has a narrow therapeutic index. The maximum dose is individualized depending on the control of the concentration of the medicinal drug and the evaluation of the efficacy and safety parameters.

The following are some general guidelines for chronic use (doses expressed as Theophylline):

 

Adults

<60 years: individual dose; 400 mg/day PO if there are risk factors for a decrease in clearance or it is impossible to control the recommended serum concentration. > = 60 years: 400 mg / day PO.

 

Geriatric

400 mg / day PO.

 

Teenagers

> = 16 years: individualized dose; 400 mg / day PO if there are risk factors for a decrease in clearance or it is impossible to control the recommended serum concentration.

<16 years: individualized dose; 16 mg/kg/day up to 400 mg / day PO if there are risk factors for a decrease in clearance or it is not possible to control the recommended serum concentration.

 

Children’s Individualized dose; 16 mg / kg / day up to 400 mg / day PO if there are risk factors for a decrease in clearance or the recommended serum theophylline concentration can not be controlled.

 

Infants: You must individualize the dose. Neonates, You must individualize the dose.

 

Generic Storage

Discard the product if it contains particulate material or is cloudy or discolored. Discard the unused portion.

Do not store for later use. Protect from light

Store at room temperature controlled (between 68 and 77 degrees F) – Store inbox until the time of use Contraindications/precautions Theophylline can alter the results of some standard laboratory tests.

Serum levels of glucose, uric acid, free fatty acids (cholesterol, HDL), and urinary excretion of free cortisol can reportedly be increased.

In addition, transient decreases in triiodothyronine levels were reported.

 

The clinician should be aware of these alterations and should weigh the clinical importance of these changes for the benefits of theophylline therapy.

 

Cardiac arrhythmias, heart disease, cor pulmonale, coronary artery disease, heart failure, myocardial infarction.

Patients with heart disease should be monitored more closely for adverse reactions to Theophylline.

Lower doses may be necessary for patients with congestive heart failure, including cor pulmonale, due to decreased theophylline clearance (> = 50% decrease).

In addition, Theophylline may exacerbate existing cardiac arrhythmias and should be used with caution in patients at risk.

Similarly, because Theophylline can increase oxygen demand, it should be carefully prescribed in patients with coronary artery disease, especially those with a history of myocardial infarction.

 

Hipotiroidismo, edema pulmonar, sepsis, shock

Patients with hypothyroidism, acute pulmonary edema, sepsis with multiple organ failure, or shock may have decreased theophylline clearance.

Any patient with the above conditions should be carefully monitored while receiving Theophylline.

 

Cystic fibrosis, hyperthyroidism

Increased theophylline clearance may occur in patients with hyperthyroidism or cystic fibrosis.

Hypercalcemia has been reported in a patient with the hyperthyroid disease at therapeutic concentrations of Theophylline.

Any patient with cystic fibrosis or thyroid conditions should be carefully monitored while receiving Theophylline.

 

Acidemia

Patients with uncorrected acidemia may increase the volume of theophylline distribution due to a decrease in plasma protein binding.

Unbound serum theophylline concentrations should be controlled in these patients to avoid toxicity.

 

Cholestasis, liver disease, hepatitis, babies, neonates, kidney failure

Since Theophylline is hepatic metabolized, doses may be reduced in patients with moderate to severe liver diseases, such as cirrhosis, acute hepatitis, cholestasis, or alcoholic liver disease.

Patients who consume ethanol regularly but do not show manifest hepatic dysfunction may require higher than average doses.

The elderly may also have reduced hepatic metabolism, and their doses should generally be lower with careful titration.

Doses should be reduced in infants less than one year, especially premature infants, due to less developed liver metabolism.

 

Smoking

It has been shown that tobacco smoking increases the clearance of Theophylline by approximately 50% in young adult tobacco smokers and around 80% in elderly tobacco smokers.

In addition, passive exposure to smoke can cause an increase in the clearance of Theophylline by up to 50%.

Because the effect of tobacco on liver microsomal enzymes is unrelated to the nicotine component, sudden cessation of smoking may result in reduced elimination of Theophylline, despite the initiation of nicotine replacement products.

After a week of abstinence from chronic smoking, clearance of Theophylline may decrease by approximately 40%, increasing serum theophylline concentrations.

Serum theophylline concentrations should be carefully monitored when changes occur in smoking status.

 

Fever, hypoxemia

It has been reported that prolonged fever reduces the clearance of Theophylline.

Lower doses should be considered in these conditions. Theophylline should also be used with caution in patients with a respiratory infection or severe hypoxemia.

Gastritis, gastroesophageal reflux disease (GERD), hiatal hernia, peptic ulcer disease

Since Theophylline can stimulate gastric secretions, it should be used with caution in patients with gastritis or active peptic ulcer disease.

Theophylline can aggravate symptoms related to hiatal hernia or gastroesophageal reflux disease (GERD).

 

Prostatic hypertrophy

Theophylline relaxes smooth muscle and can increase urinary retention, so it should be used with caution in patients with prostatic hypertrophy. The use of Theophylline can initially cause a diuretic effect.

 

The pregnancy

Theophylline is classified as a category C drug for pregnancy risk by the FDA.

Theophylline is not teratogenic in humans, but use during pregnancy can lead to potentially dangerous concentrations of Theophylline and serum caffeine in neonates and tachycardia, irritability, and other symptoms of theophylline toxicity.

A decrease in theophylline clearance was reported during the third trimester of pregnancy.

The selection of any pharmacological treatment for asthma control during pregnancy should include the specific needs of the patient, based on an individual evaluation and consideration of the possible benefits or risks to the fetus.

 

Breast-feeding

Theophylline is excreted in breast milk in concentrations similar to the serum concentration of the mother.

Neonates whose mothers take Theophylline during pregnancy or breastfeeding should be carefully monitored.

Babies fed breast milk whose mothers take Theophylline may experience irritability or other mild signs of toxicity; however, serious adverse events are unlikely to occur unless the mother has toxic serum concentrations.

 

Hypersensitivity to corn

Theophylline is contraindicated in patients who have demonstrated a hypersensitivity reaction to Theophylline or any component in the commercial product.

Part of the Theophylline premixed in intravenous infusions of dextrose can be manufactured with corn or corn products and may be contraindicated in patients with corn hypersensitivity.

 

Convulsive disorder

Theophylline should be used with caution in patients with a history of seizure disorder due to the risk of aggravating their condition.

 

Geriatric

Clearance of Theophylline is reduced by 30% in healthy senior adults versus younger adults; Clearance can be reduced even more significantly if there are concurrent disease states or other factors that reduce elimination.

The benefits and risks of using Theophylline or aminophylline and the need for more intensive control of serum theophylline concentrations in adult patients over 60 years of age should be carefully considered.

If the total daily dose is not appropriately reduced, severe and potentially fatal theophylline toxicity may occur.