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Aminophylline

Basic information Description References Safety Supplier Related

Aminophylline Basic information

Product Name:
Aminophylline
Synonyms:
  • AMinophylline(Phyllocontin, Truphylline)
  • Theophylline-ethylenediaMine anhydrous COS
  • (Theophylline)2 Ethylenediamine, Theophylline hemiethylenediamine complex, 3,7-Dihydro-1,3-dimethyl-1H-purine-2,6-dione, cmpd. with 1,2-ethanediamine (2:1)
  • Aminophylline,99%
  • Theophylline-e
  • Aminophylline hydrat
  • AMINOPHYLLINE
  • THEOPHYLLINE COMPOUND WITH ETHYLENEDIAMINE
CAS:
317-34-0
MF:
2C7H8N4O2.C2H8N2
MW:
420.43
EINECS:
206-264-5
Product Categories:
  • Somopphyllin, Aminocadol, Phyllocontin
  • Miscellaneous Biochemicals
  • API's
Mol File:
317-34-0.mol
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Aminophylline Chemical Properties

Melting point:
269-270 °C
storage temp. 
Inert atmosphere,Store in freezer, under -20°C
solubility 
H2O: 3.7 mg/mL solutions should be freshly prepared.
pka
pKa 5.0 (Uncertain)
form 
powder
color 
white to off-white
Water Solubility 
soluble
Merck 
14,465
CAS DataBase Reference
317-34-0(CAS DataBase Reference)
EPA Substance Registry System
1H-Purine-2,6-dione, 3,7-dihydro-1,3-dimethyl-, compd. with 1,2-ethanediamine (2:1) (317-34-0)
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Safety Information

Hazard Codes 
Xn,C
Risk Statements 
22-42/43-34-36/37/38-20/21/22
Safety Statements 
45-36/37/39-26-23-36
RIDADR 
UN 2811 6.1/PG 3
WGK Germany 
3
RTECS 
XH5600000
10-23
TSCA 
Yes
HazardClass 
6.1(b)
PackingGroup 
III
HS Code 
29339900
Hazardous Substances Data
317-34-0(Hazardous Substances Data)
Toxicity
LD50 orally in mice: 540 mg/kg (Thompson, Warren)

MSDS

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Aminophylline Usage And Synthesis

Description

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.

References

https://www.drugbank.ca/drugs/DB01223 https://en.wikipedia.org/wiki/Aminophylline

Description

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.

Chemical Properties

white to slightly yellowish powder

Originator

Memcophylline,Memphis Co.

Uses

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.

Uses

Bronchodilatator;Mastocytes degranulation inhibitor

Uses

Aminophylline is a bronchodilator and a non-selective phosphodiesterase (PDE) inhibitor.

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.

Contact allergens

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.

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.

Aminophylline Preparation Products And Raw materials

Raw materials

AminophyllineSupplier

HUBEI JINGCHENG CHEMICAL Gold
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J & K SCIENTIFIC LTD.
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Adamas Reagent, Ltd.
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400-600-9262
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LGM Pharma
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1-(800)-881-8210
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inquiries@lgmpharma.com
Chemsky(shanghai)International Co.,Ltd.
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021-50135380
Email
shchemsky@sina.com