Aminophylline

THERAPEUTIC GROUP: Other systemic drugs for obstructive airway disorders

IndicationsAction mechanismStudies and clinical effectiveness Usage and dosage instructionsWarnings Pregnancy and lactationInteractionsContraindicationsUndesirable effects

Indications Aminophylline

Aminofillin is generally used in the treatment of bronchial asthma and lung diseases with a bronchial spastic component.

Mechanism of action Aminophylline

Aminofillin is a drug obtained from the chemical association between theophylline and ethylenediamine, characterized by its high solubility in an aqueous environment as opposed to pure theophylline, whose alkaloid chemical nature, considerably limits its hydrophilicity, thus making it less suitable for therapeutic purposes

Following oral or parenteral administration, Aminofillin performs a therapeutic action comparable to that of Theophylline, thus leading to inactivation of the enzyme phosphodiesterase with consequent increase in concentrations of cyclic intracellular AMP and subsequent bronchodilation.

The aforementioned activity, combined with the antihistamine activity, effective in reducing the edema associated with the asthmatic condition and the hypersecretion of mucus, determines a clear improvement of the airway patency, thus ensuring an effective restoration of normal ventilatory capacities.

Methylxanthine derivatives, after a hepatic metabolism, are eliminated in the urine.

Studies carried out and clinical efficacy

AMINOFILLINA IN INTENSIVE THERAPY DEPARTMENTS

Pulm Pharmacol Ther. 2013 Mar 19. pii: S1094-5539 (13) 00075-8. doi: 10.1016 / j.pupt.2013.03.001. [Epub ahead of print]

Study demonstrating that the association with corticosteroid therapy and with Aminophylline beta agonists is associated with a statistically significant improvement in vital functions in small patients admitted to the pediatric resuscitation center.

AMINOFILLINA ACTION MECHANISM

Drug Deliv. 2013 Oct 23. [Epub ahead of print]

Experimental study that demonstrates how the treatment with Aminophylline can determine an important bronchial dilatatory effect at the level of the upper respiratory tract, causing a suppression of inflammation and allergic symptoms in small sensitized laboratory animals.

AMINOFILLINA AND RECTAL ADMINISTRATION

Int J Pharm. 2009 Sep 8; 379 (1): 119-24. doi: 10.1016 / j.ijpharm.2009.06.017. Epub 2009 Jun 23.

Work that tries to overcome the limits related to the pharmacokinetic variations associated with the administration of Aminophylline by rectal way through the introduction of devices able to guarantee a controlled release of the drug.

Method of use and dosage

Aminofillin is found in vials for intravenous use of 240 mg per 10 ml, in vials for intramuscular use of 350 mg per 2 ml of solution or in 350 mg suppositories of Aminophylline.

The therapeutic scheme reserved for the treatment of patients suffering from asthma or respiratory diseases with a bronchospastic component, is the responsibility of the doctor after having carefully evaluated the patient's state of health and the best route of administration.

The dosages will therefore depend on the method of administration and on the physio-pathological characteristics of the patient.

Warnings Aminophylline

Aminophylline therapy must necessarily be defined and supervised during the entire therapeutic process by a doctor experienced in the treatment of respiratory diseases, in order to identify any side effects or potential contraindications to the use of this drug promptly.

Particular caution should be reserved for cardiopathic, hypertensive, hypoxemic or hyperthyroid patients, or those suffering from altered hepatic and renal function or in therapy with inducing drugs / inhibitors of liver enzymes such as cigarette smoke, due to the altered metabolism to which it would encounter Aminophyllin with its biological consequences.

Given the altered and irregular absorption profile of the Aminofillin following rectal administration, this method of administration should be avoided in cases of emergency.

It is recommended to keep the medicine out of the reach of children.

PREGNANCY AND BREASTFEEDING

Although there is no experimental evidence on the toxicity of aminophyllin or theophylline for fetal health, it would still be advisable to avoid the use of this drug during pregnancy.

The ability of Theophylline, the main metabolite of Aminofillin, to concentrate in breast milk, instead extends the contraindications to the use of this drug even during breastfeeding.

Interactions

Patients taking Aminophylline should avoid the simultaneous intake of active ingredients with inducing / inhibiting activity on cytochromial enzymes such as erythromycin, TAO, lincomycin, clindamycin, allopurinol, cimetidine, influenza vaccine, propranolol, phenytoin, anticonvulsants, cigarette smoke and products based on Hypericum perforatum.

Contraindications Aminophylline

Aminofillin is contraindicated in patients with hypersensitivity to theophylline or other xanthine derivatives, hypersensitivity to lidocaine, severe heart disease and hypertensive states and during lactation.

Undesirable effects - Side effects

Administration of Aminophylline could result in transient side effects such as nausea, vomiting, epigastric pain, headache, irritability, tachycardia, insomnia and tachypnea.

Fortunately, the incidence of severe metabolic and cardiovascular side effects is rarer.