Active ingredients: Aminophylline
AMINOMAL 350 mg / 2ml solution for injection
AMINOMAL 240 mg / 10 ml solution for injection
AMINOMAL suppositories
Aminomal package inserts are available for pack sizes: - AMINOMAL 350 mg / 2ml solution for injection, AMINOMAL 240 mg / 10ml solution for injection, AMINOMAL suppositories
- AMINOMAL? 0.67% oral solution
- AMINOMAL? 600 mg prolonged-release tablets
Why is Aminomal used? What is it for?
PHARMACOTHERAPEUTIC CATEGORY
Bronchodilator.
THERAPEUTIC INDICATIONS
Bronchial asthma - lung diseases with bronchial spastic component.
Contraindications When Aminomal should not be used
Hypersensitivity to theophylline and other xanthine derivatives. The preparation is contraindicated in nursing women. Acute myocardial infarction. Hypotensive states. Hypersensitivity to lidocaine (for intramuscular vials and suppositories).
Precautions for use What you need to know before taking Aminomal
Numerous factors can reduce the hepatic clearance of theophylline with increases in plasma drug levels. These include age, congestive heart failure, chronic obstructive lung disease, concomitant infections, the simultaneous administration of many drugs such as: erythromycin, TAO, lincomycin, clindamycin, allopurinol, cimetidine, influenza vaccine, propranolol. in these cases it may be necessary to reduce the theophylline dosage.
Administration of the product should be done with caution in the elderly, cardiopaths, hypertensive patients and in patients with severe hypoxemia, hyperthyroidism, chronic cor pulmonale, congestive heart failure, peptic ulcer, severe liver or kidney disease.
Interactions Which drugs or foods can modify the effect of Aminomal
Phenytoin, other anticonvulsants and cigarette smoking may increase theophylline clearance with reduced plasma half-life. In these cases it may be necessary to increase the theophylline dosage.
In the event of factors that may affect the theophylline clearance, monitoring of the blood concentration of the drug is recommended to control the therapeutic range of theophylline.
Theophylline should not be administered concomitantly with other xanthine preparations and caution requires the combination of theophylline and ephedrine or other bronchodilator sympathomimetics.
Preparations of hypericum perforatum should not be taken concomitantly with medicinal products containing oral contraceptives, digoxin, theophylline, carbamazepine, phenobarbital, phenytoin, due to the risk of decreased plasma levels and decreased therapeutic efficacy of oral contraceptives, digoxin , theophylline, carbamazepine, phenobarbital, phenytoin.
Plasma concentrations of theophylline may be decreased by concomitant administration of hypericum perforatum preparations. This is due to the induction of the enzymes responsible for drug metabolism by preparations based on hypericum perforatum which therefore should not be administered concomitantly with theophylline.
The induction effect may persist for at least 2 weeks after stopping treatment with hypericum perforatum products.
If a patient is concomitantly taking hypericum perforatum products, plasma theophylline levels should be monitored and therapy with hypericum perforatum products discontinued.
Plasma levels of theophylline may increase with discontinuation of hypericum perforatum. The theophylline dosage may need to be adjusted.
The use of Aminomal in pediatrics is not recommended.
Warnings It is important to know that:
Use in pregnancy
Although no negative effects of theophylline on fetal development have been detected, its use in pregnancy should be limited only to cases in which asthma constitutes a serious danger to the mother.
Dosage and method of use How to use Aminomal: Dosage
Rectally
No more than 1 suppository 3 times a day.Absorption by this route is irregular.
The use of this route is not indicated in emergency situations. During the hot season, before using the suppositories, immerse them, with their wrapping, for a few minutes in cold water.
Intravenously
This route is indicated in severe cases of bronchial asthma. In these cases, a slow infusion of a solution obtained by diluting 480 mg of Aminomal (equal to 2 ampoules of 240 mg in 10 mL) in 50 ml of a compatible solution for infusion is used (e.g. chlorosodium, glucose, levulosic solution ). The infusion rate should not exceed 25 mg / min. (3.6 mL / min. Of the solution thus prepared); the total dose administered cannot exceed 5.6 mg / kg (0.8 mL / kg of the solution thus prepared). This infusion can be followed by a maintenance infusion obtained by diluting 240 mg of Aminomal (equal to 1 vial of 240 mg in 10 mL) in 500 mL of a solution for infusion (see above). The rate of this maintenance infusion will be of:
- 0.9 mg / kg / hour (equivalent to 1.9 mL / kg / hour) in adults under 50 years of age, smokers;
- 0.45 mg / kg / hour (equal to 0.9 mL / kg / hour) in non-smoking adults under 50 years of age;
- 0.25 mg / kg / hour (equivalent to 0.5 mL / kg / hour) in adults with heart failure or hepatic impairment.
In any case, administration by the i.v. of Aminomal must be performed with the patient in supine position and with controlled slowness (15-20 minutes).
Intramuscularly
1 vial of 2 mL (350 mg of Aminomal), deeply injected after making sure that the needle has not accidentally entered the vein. The product exerts a local irritating action.
N.B .: the 2 mL intramuscular vials may sometimes contain crystals of the active ingredient. In this case it is advisable to immerse the vials in hot water in order to obtain complete solubilization. The 2 mL vials are for intramuscular use only and should not be injected into a vein even after dilution.
Side Effects What are the side effects of Aminomal
Nausea, vomiting, epigastric pain, headache, irritability, insomnia, tachycardia, ectopic beats, tachypnoea and occasionally albuminuria and hyperglycaemia may occur with the use of xanthine derivatives. In case of overdose, generalized tonic-clonic seizures and severe ventricular arrhythmias may occur. .
These manifestations may constitute the first signs of intoxication. The appearance of side effects may require the suspension of the treatment which can be resumed, if necessary, at lower doses after the disappearance of all signs and symptoms of toxicity.
Report any undesirable effect not described in this leaflet to your doctor or pharmacist.
Expiry and Retention
Warning: do not use the medicine after the expiry date indicated on the package
Vials: no special storage precautions
Suppositories: keep away from heat sources
Deadline "> Other information
COMPOSITION
350 mg / 2 mL vials (intramuscular use)
- aminophylline dihydrate mg 350 (equal to theophylline anhydrous mg 276.2)
- other components: lidocaine hydrochloride 20 mg, sodium chloride, water for injections.
240 mg / 10 mL vials (intravenous use)
- aminophylline dihydrate mg 240 (equal to theophylline anhydrous mg 189.5)
- excipients: sodium chloride; water for injections.
Suppositories
- aminophylline dihydrate mg 350 (equal to theophylline anhydrous mg 276.2)
- other components: lidocaine 20 mg, glycerides of saturated fatty acids.
PHARMACEUTICAL FORMS
- 6 vials of 350 mg / 2 mL (for intramuscular use)
- 3 ampoules of 240 mg / 10 mL (for intravenous use)
- 10 suppositories of 350 mg rectally
Source Package Leaflet: AIFA (Italian Medicines Agency). Content published in January 2016. The information present may not be up-to-date.
To have access to the most up-to-date version, it is advisable to access the AIFA (Italian Medicines Agency) website. Disclaimer and useful information.
01.0 NAME OF THE MEDICINAL PRODUCT -
AMINOMAL
02.0 QUALITATIVE AND QUANTITATIVE COMPOSITION -
350 mg / 2ml solution for injection (intramuscular use)
aminophylline dihydrate mg 350 (equal to theophylline anhydrous mg 276.2)
other components: lidocaine hydrochloride 20 mg, sodium chloride, water for injections.
240 mg / 10 ml solution for injection (intravenous use)
aminophylline dihydrate mg 240 (equal to theophylline anhydrous mg 189.5)
excipients: sodium chloride; water for injections.
Suppositories
aminophylline dihydrate mg 350 (equal to theophylline anhydrous mg 276.2)
other components: lidocaine 20 mg, glycerides of saturated fatty acids.
03.0 PHARMACEUTICAL FORM -
Ampoules for intravenous use (10 ml ampoules)
Ampoules for intramuscular use (2 ml ampoules)
Suppositories rectally
04.0 CLINICAL INFORMATION -
04.1 Therapeutic indications -
Bronchial asthma - lung diseases with bronchial spastic component.
04.2 Posology and method of administration -
Rectally
No more than 1 suppository 3 times a day. The absorption through this route is irregular. The use of this route is not indicated in emergency situations. During the hot season, before using the suppositories, immerse them, with their wrapping, for a few minutes in cold water.
Intravenously
This route is indicated in severe cases of bronchial asthma. In these cases, a slow infusion of a solution obtained by diluting 480 mg of Aminomal (equal to 2 ampoules of 240 mg in 10 ml) in 50 ml of a compatible solution for infusion (e.g. chloride sodium, glucose, levulosic solution) is used. ). The infusion rate should not exceed 25 mg / min. (3.6 ml / min. Of the solution thus prepared); the total dose administered cannot exceed 5.6 mg / kg (0.8 ml / kg of the solution thus prepared). This infusion can be followed by a maintenance infusion obtained by diluting 240 mg of Aminomal (equal to 1 ampoule of 240 mg in 10 ml) in 500 ml of a solution for infusion (see above). The rate of this maintenance infusion will be of:
0.9 mg / kg / hour (equal to 1.9 ml / kg / hour) in adults under 50 years of age, smokers;
0.45 mg / kg / hour (equal to 0.9 ml / kg / hour) in non-smoking adults under 50 years of age;
0.25 mg / kg / hour (equivalent to 0.5 ml / kg / hour) in adults with heart failure or hepatic impairment.
In any case, administration by the i.v. of Aminomal must be performed with the patient in supine position and with controlled slowness (15-20 minutes).
Intramuscularly
1 ampoule of 2 ml (350 mg of Aminomal), deeply injected after making sure that the needle has not accidentally entered the vein. The product exerts a local irritating action.
04.3 Contraindications -
Hypersensitivity to theophylline and other xanthine derivatives. The preparation is contraindicated in nursing women. Acute myocardial infarction. Hypotensive states. Hypersensitivity to lidocaine (for intramuscular vials and suppositories).
04.4 Special warnings and appropriate precautions for use -
The toxic effects of theophylline are usually related to serum levels above 20 mcg / ml. Above average blood levels may occur at conventional doses due to factors that can reduce hepatic clearance of theophylline with increases in plasma drug levels. These include age, congestive heart failure, chronic obstructive lung diseases, concomitant infections, the simultaneous administration of many drugs such as: erythromycin, TAO, lincomycin, clindamycin, allopurinol, cimetidine, influenza vaccine, propranolol. in these cases it may be necessary to reduce the theophylline dosage. Phenytoin, other anticonvulsants and cigarette smoking may increase theophylline clearance with reduced plasma half-life. In these cases it may be necessary to increase the theophylline dosage.
In the event of factors that may affect the theophylline clearance, monitoring of the blood concentration of the drug is recommended to control the therapeutic range of theophylline.
Absorption via the rectum is irregular: therefore the use of this route is not indicated in an emergency. During the hot season, before using the suppositories, immerse them, with their wrapping, for a few minutes in cold water.
Intravenous administration should be performed with the patient in a supine position and with controlled slowness (15-20 minutes).
Intromuscular administration should be carried out by injecting the drug deeply, after making sure that the needle has not accidentally entered the vein (the product exerts a local irritating action).
The 2 ml intromuscular vials may sometimes contain crystals of the active ingredient. In this case it is advisable to immerse the vials in hot water in order to obtain complete solubilization.
Keep out of reach of children.
Theophylline should not be administered simultaneously with other xanthine preparations and caution requires the association of theophylline and ephedrine or other bronchodilator sympathomimetics. The administration of the product should be done with caution in the elderly, cardiopaths, hypertensive patients and in patients with severe hypoxemia, hyperthyroidism. , chronic pulmonary heart, congestive heart failure, peptic ulcer, severe liver or kidney disease. The use of Aminomal in pediatrics is not recommended.
Preparations of hypericum perforatum should not be taken concomitantly with medicinal products containing oral contraceptives, digoxin, theophylline, carbamazepine, phenobarbital, phenytoin, due to the risk of decreased plasma levels and decreased therapeutic efficacy of oral contraceptives, digoxin , theophylline, carbamazepine, phenobarbital, phenytoin (see Section 4.5 Interactions).
04.5 Interactions with other medicinal products and other forms of interaction -
The simultaneous administration of many drugs such as: erythromycin, TAO, lincomycin, clindamycin, allopurinol, cimetidine, influenza vaccine, propranolol, can induce an increase in blood levels of theophylline as these substances reduce plasma clearance.
Phenytoin, other anticonvulsants and cigarette smoking may increase theophylline clearance with reduced plasma half-life. In these cases it may be necessary to increase the theophylline dosage.
Plasma concentrations of theophylline may be decreased by concomitant administration of hypericum perforatum preparations. This is due to the induction of the enzymes responsible for drug metabolism by preparations based on hypericum perforatum which therefore should not be administered concomitantly with theophylline.
The induction effect may persist for at least 2 weeks after stopping treatment with hypericum perforatum products.
If a patient is concomitantly taking hypericum perforatum products, plasma theophylline levels should be monitored and therapy with hypericum perforatum products discontinued.
Plasma levels of theophylline may increase with discontinuation of hypericum perforatum. The theophylline dosage may need to be adjusted.
04.6 Pregnancy and breastfeeding -
Although no negative effects of theophylline on fetal development have been detected, its use in pregnancy should be limited only to cases in which asthma constitutes a serious danger to the mother. The use is contraindicated in breastfeeding women.
04.7 Effects on ability to drive and use machines -
Treatment with theophylline does not induce negative effects on driving skills and the use of machines.
04.8 Undesirable effects -
With the use of xanthine derivatives, nausea, vomiting, epigastric pain, headache, irritability, insomnia, tachycardia, ectopic beats, tachypnea and occasionally albuminuria and hyperglycaemia may occur. In case of overdose, generalized tonic-clonic seizures and severe ventricular arrhythmias may occur. Such manifestations can be the first signs of intoxication. The appearance of side effects may require discontinuation of the treatment which can be resumed, if necessary, at lower doses after the disappearance of all signs and symptoms of toxicity.
04.9 Overdose -
In case of severe toxic effects, check heart rate (possibly E.C.G.) and respiratory rate, blood pressure and correct any electrolyte imbalances.
In case of convulsions administer benzodiazepines.
05.0 PHARMACOLOGICAL PROPERTIES -
05.1 "Pharmacodynamic properties -
Aminophylline FU is a combination product of theophylline with ethylenediamine and is much more water soluble than theophylline.
It is therefore particularly suitable for both oral and parenteral administration.
The pharmacodynamic properties are therefore entirely referable to theophylline, whose anti-bronchospastic activity is mainly related to the increase in intracellular cyclic AMP that it induces through the inactivation of the phosphodiesterase enzyme.
More recently, numerous clinical and experimental investigations have shown that theophylline also has the ability to perform an "inhibiting action" on the activation of the mast cell microtubular apparatus, causing an inhibition or reduction in the release of chemical mediators (histamine).
Furthermore, theophylline has a powerful stimulating effect on the respiratory center, which is particularly evident when the center itself is depressed, as in severe respiratory insufficiency.
05.2 "Pharmacokinetic properties -
Theophylline is rapidly absorbed from the gastrointestinal tract and the volume of distribution is very large (0.50 l / kg), indicating that the molecule reaches all parts of the body. Approximately 8% of theophylline is excreted unchanged in the urine, while the remainder is metabolised by the hepatic microsomal system and excreted by the same route as 1-3 dimethyluric acid and as 3-methylxanthine.
Therapeutically effective blood levels are between 10 and 20 mcg / ml.
05.3 Preclinical safety data -
The administration of aminophylline in toxic doses causes hyperexcitability, tachypnea, sometimes convulsions.
In mice, the LD50 is 410 mg / kg orally and 241 mg / kg intraperitoneally.
In rats, the LD50 is 300 mg / kg orally and 210 mg / kg intraperitoneally.
Aminophylline up to 100 mg / kg / day is perfectly tolerated for prolonged oral treatment (6 months) in rats and dogs: no treatment-dependent changes in the blood and in the main organs have been highlighted.
By administering aminophylline some subjects may experience a hypersensitivity towards ethylenediamine.
06.0 PHARMACEUTICAL INFORMATION -
06.1 Excipients -
350 mg / 2ml solution for injection (intramuscular use)
lidocaine hydrochloride 20 mg, sodium chloride 18 mg, water for injections q.s. to ml 2.
240 mg / 10 ml solution for injection (intravenous use)
sodium chloride 80 mg; water for injections q.s. at 10 ml.
Suppositories
lidocaine 20 mg, glycerides of saturated fatty acids to taste at mg 1915.
06.2 Incompatibility "-
Aminophylline does not show chemical incompatibility with other substances possibly associated in therapy.
06.3 Period of validity "-
- 240 mg / 10 ml solution for injection (i.v. use): 5 years
- 350 mg / 2ml solution for injection (IM use): 3 years
- Suppositories: 3 years
06.4 Special precautions for storage -
Vials:
No special storage precautions
Suppositories:
Keep away from heat sources
06.5 Nature of the immediate packaging and contents of the package -
Aminomal 240 mg / 10 ml - type I glass vials
Box of 3 vials for i.v.
Aminomal 350 mg / 2 ml - type I glass vials
Box of 6 vials for IM use
Aminomal suppositories - polyvinyl chloride valve
Box of 10 suppositories
06.6 Instructions for use and handling -
see point 4.2.
07.0 HOLDER OF THE "MARKETING AUTHORIZATION" -
MALESCI INSTITUTE FARMACOBIOLOGICO SpA
Via Lungo l "Ema, 7 - Bagno a Ripoli FI
08.0 MARKETING AUTHORIZATION NUMBER -
Aminomal 240 mg / 10 ml - 3 ampoules 011226026
Aminomal 350 mg / 2 ml - 6 ampoules 011226139
Suppositories 011226038
09.0 DATE OF FIRST AUTHORIZATION OR RENEWAL OF THE AUTHORIZATION -
AIC renewal: June 95, May 2000, May 2005.
10.0 DATE OF REVISION OF THE TEXT -
November 2007
