Aminophylline

Source: Wikipedia, the free encyclopedia.
Aminophylline
Clinical data
AHFS/Drugs.comProfessional Drug Facts
MedlinePlusa601015
Pregnancy
category
  • AU: A
Routes of
administration		By mouth, intravenous therapy (IV)
ATC code
Legal status
Legal status
  • AU: S3 (Pharmacist only)
  • UK: P (
    Pharmacy medicines
    )
  • US: ℞-only[1]
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Protein binding60%
Elimination half-life7–9 hours
Identifiers
  • 1,3-Dimethyl-7H-purine-2,6-dione; ethane-1,2-diamine
JSmol)
  • Cn2c(=O)c1nc[nH]c1n(C)c2=O.Cn2c(=O)c1nc[nH]c1n(C)c2=O.NCCN
  • InChI=1S/2C7H8N4O2.C2H8N2/c2*1-10-5-4(8-3-9-5)6(12)11(2)7(10)13;3-1-2-4/h2*3H,1-2H3,(H,8,9);1-4H2 checkY
  • Key:FQPFAHBPWDRTLU-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Aminophylline is a compound of the bronchodilator theophylline with ethylenediamine in 2:1 ratio. The ethylenediamine improves solubility, and the aminophylline is usually found as a dihydrate.[2]

Aminophylline is less potent and shorter-acting than theophylline. Its most common use is in the treatment of airway obstruction from asthma or COPD. Aminophylline is a nonselective adenosine receptor antagonist and phosphodiesterase inhibitor.[3]

Medical uses

Intravenous aminophylline can be used for acute exacerbation of symptoms and reversible airway obstruction in

COPD, emphysema and chronic bronchitis. It is used as an adjunct to inhaled beta-2 selective agonists and systemically administered corticosteroids.[4]

Aminophylline is used to reverse regadenoson, dipyridamole or adenosine based infusions during nuclear cardiology stress testing. Aminophylline has also been reported to be effective in preventing slow heart rates during complex cardiovascular interventions (atherectomy of the right coronary artery).[5] It is also used in the treatment of heart block due to acute inferior myocardial infarction. It can also cause cardiac arrest.

Aminophylline has shown some promise as a bodyfat reducer when used as a topical cream.

anaphylactic shock.[7]

While it has been suggested for use in cardiac arrest evidence does not support a benefit.[8][9]

Side effects

Aminophylline can lead to theophylline toxicity. Aminophylline has been found to decrease the sedative effects of propofol[10] and decrease topiramate antiseizure action.[11]

Properties

It is more

alkaline. 1 g dissolves in 25 mL of water to give a clear solution; 1 g dissolved in 5 mL of water crystallizes upon standing, but redissolves when a small amount of ethylenediamine
is added. Insoluble in alcohol and in ether.

Pharmacology

Like other methylated xanthine derivatives, aminophylline is both a

  1. competitive nonselective
    innate immunity[15]
    and
  2. nonselective adenosine receptor antagonist.[16]

Aminophylline causes bronchodilation, diuresis†,

epinephrine
from adrenal medulla cells.
†Diuresis is caused by an increase in cAMP which acts in the CNS to inhibit the release of antidiuretic hormone (arginine-vasopressin).

Adenosine is an endogenous extracellular messenger that can regulate myocardial oxygen needs.

cardiac automaticity, and decrease β-adrenergic effects on contractility.[3][17] Adenosine also antagonizes chronotropic and ionotropic effects of circulating catecholamines.[18] Overall, adenosine decreases the heart’s rate and force of contraction, which increases blood supply to the cardiac muscle. Given specific circumstances this mechanism (which is intended to protect the heart) may cause atropine-resistant refractory bradyasystole.[3] Adenosine's effects are concentration-dependent. Adenosine’s receptors are competitively antagonized by methylxanthines such as aminophylline.[3][17][18] Aminophylline competitively antagonizes the cardiac actions of adenosine at the cell surface receptors.[17]
Thus, it increases heart rate and contractility.

Brand names

  • Euphyllin
  • Phyllocontin
  • Truphylline
  • Minomal R 175 mg tab
  • Minomal R 350 mg tab
  • Minomal SR 600 mg tab

References

  1. ^ "FDA-Approved Drugs Abbreviated New Drug Application (ANDA): 087242". fda.gov. October 26, 1983. Retrieved December 2, 2023.
  2. ^ "Aminophylline Professional Monograph". Drugs.com.
  3. ^
    PMID 12615581
    .
  4. ^ "Aminophylline Injection". Drugs.com. Retrieved 6 January 2018.
  5. ^ "Aminophylline for Preventing Bradyarrhythmias During Orbital or Rotational Atherectomy of the Right Coronary Artery". invasivecardiology.com. Archived from the original on 2020-08-03. Retrieved 2018-06-15.
  6. S2CID 988473
    .
  7. ^ Blackbourne LH. Surgical Recall. Lippincott Williams and Wilkins, 2009. pp169
  8. PMID 17652689
    .
  9. PMID 26593309
    .
  10. S2CID 29111498
    .
  11. PMID 17320861
    .
  12. PMID 11692087
    .
  13. PMID 18568240
    .
  14. PMID 9927365
    .
  15. ^
    PMID 15634873
    .
  16. PMID 3588607
    .
  17. ^
    PMID 9259053
    .
  18. ^
    PMID 9783508
    .

External links

  • "Aminophylline". Drug Information Portal. U.S. National Library of Medicine.
Retrieved from "https://en.wikipedia.org/w/index.php?title=Aminophylline&oldid=1220160783"