Aminophylline is a drug combination consisting of bronchodilator theophylline and ethylenediamine in 2: 1 ratio. It is a kind of non-selective adenosine receptor blocker, histone deacetylase activator and phosphodiesterase inhibition. It is mainly indicated for the treatment of various kinds of lung diseases including asthma, COPD, chronic bronchitis and emphysema. Aminophylline exerts its effect through the component of theophylline in vivo. Theophylline can relax the smooth muscle of the bronchial airways and pulmonary blood vessels. It can competitively inhibits type III and type IV phosphodiesterase (PDE), which breaks down cyclic AMP in smooth muscle cells, possibly leading to bronchodilation. Theophylline also binds to the adenosine A2B receptor to block the adenosine mediated bronchoconstriction. Furthermore, during the inflammatory states, theophylline can activate the histone deacetylase to prevent transcription of inflammatory genes that require the acetylation of histones to initiate the transcription.
https://www.drugbank.ca/drugs/DB01223
https://en.wikipedia.org/wiki/Aminophylline
Aminophylline is a 2/1 mixture of theophylline and
ethylenediamine. It caused contact dermatitis in
industrial plants, in pharmacists, and in nurses.
Ethylenediamine is the sensitizer, and patch testing is
generally positive to both ethylenediamine and aminophylline,
but negative to theophylline.
white to slightly yellowish powder
Memcophylline,Memphis Co.
Bronchodilatator;Mastocytes degranulation inhibitor
Aminophylline exhibits vasodilatory and anti-inflammatory activity and is occasionally clinically used to treat chronic obstructive pulmonary disorder (COPD). In animal models of allergen-induced lung inflammation, aminophylline decreases levels of IL-5, IL-8, and eosinophils. It is mostly used to prepare solutions for intravenous injections.
Aminophylline is a bronchodilator and a non-selective phosphodiesterase (PDE) inhibitor.
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.
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.
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.
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.
Cardiovascular and respiratory collapse.
This drug is a 2:1 mixture of the alkaloid theophylline
and ethylenediamine (see below). It caused contact
dermatitis in industrial plants, pharmacists, and nurses.
Ethylenediamine is the sensitizer and patch testing is
generally positive to both ethylenediamine and aminophylline
and negative to theophylline.
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.
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.
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.
