Details of the Drug

General Information of Drug (ID: DML2NIB)

• Drug Name: Aminophylline
• Synonyms: Aminocardol; Aminodur; Aminofilina; Aminofillina; Aminophyllin; Ammophyllin; Cardiofilina; Cardiomin; Cardophylin; Cardophyllin; Carena; Cariomin; DOBO; Diaphilline; Diaphyllin; Diaphylline; Diophllin; Diophyllin; Diuxanthine; Ethophylline; Eufilina; Euphyllin; Euphylline; Euphyllinum; Eurphyllin; Euufilin; Euufillin; Genophyllin; Grifomin; Inophylline; Lasodex; Linampheta; Lixaminol; Metaphyllin; Metaphylline; Minaphil; Miofilin; Neophyiline; Norofilina; Peterphyllin; Phylcardin; Phyllindon; Phyllocontin; Phyllotemp; Somophyllin; Stenovasan; Syntophyllin; Theodrox; Theolamine; Theolone; Theomin; Theophyldine; Thephyldine; Truphylline; Vasofilina; A 1755; BY 108; Minomal(TN); Phyllocontin (TN); TH/100; Truphylline (TN)

Indication

Disease Entry	ICD 11	Status	REF
Bronchial asthma	CA23	Approved	[1]
Bronchitis	CA20	Approved	[2]
Lung cancer	2C25.0	Approved	[2]
Non-small-cell lung cancer	2C25.Y	Approved	[2]
Pulmonary disease	1B10-1F85	Approved	[2]
Pulmonary emphysema	CA21.Z	Approved	[2]
Severe asthma	CA23	Approved	[2]
Asthma	CA23	Phase 2	[3]

• Therapeutic Class: Bronchodilator Agents
• Affected Organisms: Humans and other mammals
• ATC Code:
  R03DA05: Aminophylline
  R03DA: Xanthines
  R03D: OTHER SYSTEMIC DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
  R03: DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
  R: RESPIRATORY SYSTEM
  R03DA05: Aminophylline
  R03DA: Xanthines
  R03D: OTHER SYSTEMIC DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
  R03: DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
  R: RESPIRATORY SYSTEM
  R03DA05: Aminophylline
  R03DA: Xanthines
  R03D: OTHER SYSTEMIC DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
  R03: DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
  R: RESPIRATORY SYSTEM
• Drug Type: Small molecular drug
• #Ro5 Violations (Lipinski): 0:
  Molecular Weight; 420.43
  Logarithm of the Partition Coefficient; Not Available
  Rotatable Bond Count; 1
  Hydrogen Bond Donor Count; 4
  Hydrogen Bond Acceptor Count; 8
• ADMET Property:
  Half-life: The concentration or amount of drug in body reduced by one-half in 7 - 9 hours [4]
  Vd: The volume of distribution (Vd) of drug is 0.3-0.7 L/kg []
• Chemical Identifiers:
  Formula: C16H24N10O4
  IUPAC Name: 1,3-dimethyl-7H-purine-2,6-dione;ethane-1,2-diamine
  Canonical SMILES: CN1C2=C(C(=O)N(C1=O)C)NC=N2.CN1C2=C(C(=O)N(C1=O)C)NC=N2.C(CN)N
  InChI: 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
  InChIKey: FQPFAHBPWDRTLU-UHFFFAOYSA-N
• Cross-matching ID:
  PubChem CID: 9433
  ChEBI ID: CHEMBL1370561
  CAS Number: 317-34-0
  UNII: 27Y3KJK423
  DrugBank ID: DB01223
  TTD ID: D03TYI
  INTEDE ID: DR0090
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Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Phosphodiesterase 3A (PDE3A)	TT06AWU	PDE3A_HUMAN	Inhibitor	[5]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 2E1 (CYP2E1)	DEVDYN7	CP2E1_HUMAN	Substrate	[6]
Cytochrome P450 1A2 (CYP1A2)	DEJGDUW	CP1A2_HUMAN	Substrate	[7]

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Aminophylline (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Metreleptin	DM1NOEK	Moderate	Decreased metabolism of Aminophylline caused by Metreleptin mediated inhibition of CYP450 enzyme.	Acute diabete complication [5A2Y]	[8]
Emapalumab	DMZG5WL	Moderate	Altered metabolism of Aminophylline due to Emapalumab alters the formation of CYP450 enzymes.	Adaptive immunity immunodeficiency [4A01]	[9]
Siltuximab	DMGEATB	Moderate	Altered metabolism of Aminophylline due to Siltuximab alters the formation of CYP450 enzymes.	Anemia [3A00-3A9Z]	[9]
Obeticholic acid	DM3Q1SM	Moderate	Decreased metabolism of Aminophylline caused by Obeticholic acid mediated inhibition of CYP450 enzyme.	Autoimmune liver disease [DB96]	[10]
Troleandomycin	DMUZNIG	Moderate	Decreased metabolism of Aminophylline caused by Troleandomycin mediated inhibition of CYP450 enzyme.	Bacterial infection [1A00-1C4Z]	[11]
Tucatinib	DMBESUA	Moderate	Decreased metabolism of Aminophylline caused by Tucatinib mediated inhibition of CYP450 enzyme.	Breast cancer [2C60-2C6Y]	[12]
Levonorgestrel	DM1DP7T	Moderate	Decreased metabolism of Aminophylline caused by Levonorgestrel.	Contraceptive management [QA21]	[13]
Stiripentol	DMMSDOY	Moderate	Decreased metabolism of Aminophylline caused by Stiripentol mediated inhibition of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[14]
Fosphenytoin	DMOX3LB	Moderate	Increased metabolism of Aminophylline caused by Fosphenytoin mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[15]
Cannabidiol	DM0659E	Moderate	Increased metabolism of Aminophylline caused by Cannabidiol mediated induction of CYP450 enzyme.	Epileptic encephalopathy [8A62]	[16]
Febuxostat	DMDEXQ0	Moderate	Decreased metabolism of Aminophylline caused by Febuxostat mediated inhibition of non-CYP450 enzyme.	Inborn purine/pyrimidine/nucleotide metabolism error [5C55]	[17]
Amobarbital	DM0GQ8N	Moderate	Increased metabolism of Aminophylline caused by Amobarbital mediated induction of CYP450 enzyme.	Insomnia [7A00-7A0Z]	[18]
Polyethylene glycol	DM4I1JP	Moderate	Increased risk of lowers seizure threshold by the combination of Aminophylline and Polyethylene glycol.	Irritable bowel syndrome [DD91]	[19]
Blinatumomab	DMGECIJ	Moderate	Decreased metabolism of Aminophylline caused by Blinatumomab mediated inhibition of CYP450 enzyme.	Mature B-cell lymphoma [2A85]	[20]
Exjade	DMHPRWG	Major	Decreased metabolism of Aminophylline caused by Exjade mediated inhibition of CYP450 enzyme.	Mineral absorption/transport disorder [5C64]	[21]
Ustekinumab	DMHTYK3	Moderate	Altered metabolism of Aminophylline due to Ustekinumab alters the formation of CYP450 enzymes.	Psoriasis [EA90]	[9]
Ixekizumab	DMXW92T	Moderate	Altered metabolism of Aminophylline due to Ixekizumab alters the formation of CYP450 enzymes.	Psoriasis [EA90]	[9]
Tocilizumab	DM7J6OR	Moderate	Altered metabolism of Aminophylline due to Tocilizumab alters the formation of CYP450 enzymes.	Rheumatoid arthritis [FA20]	[9]
Canakinumab	DM8HLO5	Moderate	Altered metabolism of Aminophylline due to Canakinumab alters the formation of CYP450 enzymes.	Rheumatoid arthritis [FA20]	[9]
Rilonacept	DMGLUQS	Moderate	Altered metabolism of Aminophylline due to Rilonacept alters the formation of CYP450 enzymes.	Rheumatoid arthritis [FA20]	[9]
Golimumab	DMHZV7X	Moderate	Altered metabolism of Aminophylline due to Golimumab alters the formation of CYP450 enzymes.	Rheumatoid arthritis [FA20]	[9]
Sarilumab	DMOGNXY	Moderate	Altered metabolism of Aminophylline due to Sarilumab alters the formation of CYP450 enzymes.	Rheumatoid arthritis [FA20]	[9]
Voxelotor	DMCS6M5	Moderate	Decreased metabolism of Aminophylline caused by Voxelotor mediated inhibition of CYP450 enzyme.	Sickle-cell disorder [3A51]	[22]

References

• [1] FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 081142.
• [2] Aminophylline FDA Label
• [3] Adenosine receptors: development of selective agonists and antagonists. Prog Clin Biol Res. 1987;230:41-63.
• [4] Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
• [5] Topical fat reduction from the waist. Diabetes Obes Metab. 2007 May;9(3):300-3.
• [6] Theophylline metabolism in human liver microsomes: inhibition studies. J Pharmacol Exp Ther. 1996 Mar;276(3):912-7.
• [7] Lack of effect of olanzapine on the pharmacokinetics of a single aminophylline dose in healthy men. Pharmacotherapy. 1998 Nov-Dec;18(6):1237-48.
• [8] Product Information. Myalept (metreleptin). Bristol-Myers Squibb, Princeton, NJ.
• [9] Cerner Multum, Inc. "UK Summary of Product Characteristics.".
• [10] Product Information. Ocaliva (obeticholic acid). Intercept Pharmaceuticals, Inc., New York, NY.
• [11] Amsden GW "Erythromycin, clarithromycin, and azithromycin: are the differences real?" Clin Ther 18 (1996): 56-72. [PMID: 8851453]
• [12] Product Information. Tukysa (tucatinib). Seattle Genetics Inc, Bothell, WA.
• [13] Gardner MJ, Tornatore KM, Jusko WJ, Kanarkowski R "Effects of tobacco smoking and oral contraceptive use on theophylline disposition." Br J Clin Pharmacol 16 (1983): 271-80. [PMID: 6626419]
• [14] EMEA. European Medicines Agency "EPARs. European Union Public Assessment Reports.".
• [15] Crowley JJ, Cusack BJ, Jue SG, et al "Cigarette smoking and theophylline metabolism: effects of phenytoin." Clin Pharmacol Ther 42 (1987): 334-40. [PMID: 3621789]
• [16] Cerner Multum, Inc. "Australian Product Information.".
• [17] Product Information. Uloric (febuxostat). Takeda Pharmaceuticals America, Lincolnshire, IL.
• [18] Bukowskyj M, Nakatsu K, Munt PW "Theophylline reassessed." Ann Intern Med 101 (1984): 63-73. [PMID: 6145380]
• [19] Product Information. Suprep Bowel Prep Kit (magnesium/potassium/sodium sulfates). Braintree Laboratories, Braintree, MA.
• [20] Product Information. Blincyto (blinatumomab). Amgen USA, Thousand Oaks, CA.
• [21] Product Information. Exjade (deferasirox). Novartis Pharmaceuticals, East Hanover, NJ.
• [22] Product Information. Oxbryta (voxelotor). Global Blood Therapeutics, Inc., South San Francisco, CA.