Chemical Properties
white to slightly yellowish powder
Uses
Aminophylline is a bronchodilator and a non-selective phosphodiesterase (PDE) inhibitor.
Uses
Bronchodilatator;Mastocytes degranulation inhibitor
Originator
Memcophylline,Memphis Co.
Definition
ChEBI: Aminophylline is a mixture comprising of theophylline and ethylenediamine in a 2:1 ratio. It has a role as a bronchodilator agent and a cardiotonic drug. It contains a theophylline and an ethylenediamine.
Manufacturing Process
A mixture of 198 g (1 mol) theophylline and 60-78 g (0.75-1 mol)
ethylenediamine hydrate in 300 g of water was stirred at 50°C and then the
mixture was concentrated in vacuo. The product (aminophylline) was
separeted by suction filtration. Aminophylline was used as an aqueous
solution.
Brand name
Phyllocontin
(Purdue Frederick); Somophyllin (Fisons); Truphylline (G
& W);Afonilum;Aminomal;Aminophylline injection;Aminophylline mudrane;Aminophylline oral;Amino-slow;Amnivent;Asmafilin;Cardophylline;Carine;Colonofilin;Corfilamine;Corophylline;Corphyllamin;Duraphyllin;Escophylline;Eudiamine;Euphyllin 0.48;Euphyllin retard;Euphylllin cr;Euphylllina;Fadfilina;Godafilin;Jaa aminophylline;Mini-lix;Mudrane gg;Mundiphyllin;Palaran;Palaron;Pecram;Pecran;Peterphylin;Phyllotemp;Planphylline;Somophyllin-12;Syntophyllin;Teophyllamin;Thodrox;Variaphylline.
Therapeutic Function
Diuretic, Cardiac stimulant, Smooth muscle relaxant,
Vasodilator
World Health Organization (WHO)
Aminophylline, the ethylenediamine salt of theophylline, was
introduced many years ago as a treatment for asthma and is listed in the 8th WHO
Model List of Essential Drugs. It has been recognized for some 10 years that
aminophylline preparations are not interchangeable because bioavailability can
vary considerably. The resulting variability in drug absorption can lead to adverse
effects including irritation of the mucosa. Allergic reation can also be an adverse
effect of aminophylline. Theophylline functions similarly but is considered less of
an irritant.
Hazard
Cardiovascular and respiratory collapse.
Clinical Use
Reversible airways obstruction
Acute severe asthma
Veterinary Drugs and Treatments
The theophyllines are used primarily for their bronchodilatory effects,
often in patients with myocardial failure and/or pulmonary
edema. While they are still routinely used, the methylxanthines
must be used cautiously due to their adverse effects and toxicity.
Drug interactions
Potentially hazardous interactions with other drugs
Antibacterials: increased concentration with
azithromycin, clarithromycin, erythromycin,
ciprofloxacin, norfloxacin and isoniazid; decreased
erythromycin levels if erythromycin is given
orally; increased risk of convulsions if given with
quinolones; rifampicin accelerates metabolism of
aminophylline.
Antidepressants: concentration increased by
fluvoxamine - avoid or halve theophylline dose and
monitor levels; concentration reduced by St John’s
wort - avoid.
Antiepileptics: metabolism increased by
carbamazepine, phenobarbital and primidone;
concentration of both drugs increased with
fosphenytoin and phenytoin.
Antifungals: concentration increased by fluconazole
and ketoconazole.
Antivirals: metabolism of aminophylline increased
by ritonavir; concentration possibly increased by
aciclovir.
Calcium-channel blockers: concentration increased
by diltiazem and verapamil and possibly other
calcium-channel blockers.
Deferasirox: concentration of aminophylline
increased.
Feboxostat: use with caution.
Interferons: reduced metabolism of aminophylline.
Tacrolimus: may increase tacrolimus levels.
Ulcer-healing drugs: metabolism inhibited by
cimetidine; absorption possibly reduced by sucralfate.
Metabolism
Aminophylline is metabolised to theophylline in vivo.
Theophylline is excreted in the urine as metabolites,
mainly 1,3-dimethyluric acid and 3-methylxanthine, and
about 10% is excreted unchanged.
