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diprophylline 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| N-methylated xanthine derivatives | 976 | 479-18-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A THEOPHYLLINE derivative with broncho- and vasodilator properties. It is used in the treatment of asthma, cardiac dyspnea, and bronchitis.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 1 | g | O |
| 1 | g | P |
| 1 | g | R |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 235.99 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 90 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 0.42 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 4.80 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 1.70 hours | Lombardo F, Berellini G, Obach RS |
| S (Water solubility) | 330 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 7, 1951 | FDA |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | R03DA01 | RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES OTHER SYSTEMIC DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES Xanthines |
| ATC | R03DA51 | RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES OTHER SYSTEMIC DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES Xanthines |
| ATC | R03DB01 | RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES OTHER SYSTEMIC DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES Xanthines and adrenergics |
| MeSH PA | D001993 | Bronchodilator Agents |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D010726 | Phosphodiesterase Inhibitors |
| MeSH PA | D014665 | Vasodilator Agents |
| MeSH PA | D018927 | Anti-Asthmatic Agents |
| MeSH PA | D019141 | Respiratory System Agents |
| CHEBI has role | CHEBI:35523 | bronchodilator agent |
| CHEBI has role | CHEBI:35620 | vasodilator agent |
| CHEBI has role | CHEBI:50218 | EC 3.1.4.* (phosphoric diester hydrolase) inhibitor |
| CHEBI has role | CHEBI:51371 | muscle relaxant |
Related Drugs by ATC class:
R03DA Xanthines 9 drugs
R03DB Xanthines and adrenergics 4 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Bronchospasm | indication | 4386001 | |
| Chronic bronchitis | indication | 63480004 | DOID:6132 |
| Pulmonary emphysema | indication | 87433001 | |
| Asthma | indication | 195967001 | DOID:2841 |
| Asthma night-time symptoms | indication | 395022009 | |
| Asthma management | indication | 406162001 | |
| Asthma-chronic obstructive pulmonary disease overlap syndrome | indication | 10692761000119107 | |
| Chronic Obstructive Pulmonary Disease with Bronchospasms | off-label use | ||
| COPD Associated with Chronic Bronchitis | off-label use | ||
| Gastritis | contraindication | 4556007 | DOID:4029 |
| Suicidal thoughts | contraindication | 6471006 | |
| Alcoholism | contraindication | 7200002 | |
| Hyperammonemia | contraindication | 9360008 | |
| Peptic ulcer | contraindication | 13200003 | DOID:750 |
| Hepatic encephalopathy | contraindication | 13920009 | DOID:13413 |
| Myocardial infarction | contraindication | 22298006 | DOID:5844 |
| Glaucoma | contraindication | 23986001 | DOID:1686 |
| Hyperthyroidism | contraindication | 34486009 | DOID:7998 |
| Depressive disorder | contraindication | 35489007 | |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Conduction disorder of the heart | contraindication | 44808001 | |
| Chronic heart failure | contraindication | 48447003 | |
| Disorder of cardiovascular system | contraindication | 49601007 | DOID:1287 |
| Heart disease | contraindication | 56265001 | DOID:114 |
| Hepatic failure | contraindication | 59927004 | |
| Poisoning by phenobarbital | contraindication | 64921004 | |
| Substance abuse | contraindication | 66214007 | |
| Psychotic disorder | contraindication | 69322001 | |
| Hepatic coma | contraindication | 72836002 | DOID:12550 |
| Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
| Sleep apnea | contraindication | 73430006 | DOID:0050847 |
| Cor pulmonale | contraindication | 83291003 | DOID:8515 |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Angina pectoris | contraindication | 194828000 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Benign prostatic hyperplasia | contraindication | 266569009 | |
| Dyspnea | contraindication | 267036007 | |
| Anemia | contraindication | 271737000 | DOID:2355 |
| Pregnancy, function | contraindication | 289908002 | |
| Thrombocytopenic disorder | contraindication | 302215000 | DOID:1588 |
| Neutropenic disorder | contraindication | 303011007 | DOID:1227 |
| Angle-closure glaucoma | contraindication | 392291006 | DOID:13550 |
| Breastfeeding (mother) | contraindication | 413712001 | |
| Chronic myocardial ischemia | contraindication | 413844008 | DOID:3393 |
| Disorder of coronary artery | contraindication | 414024009 | |
| Myocardial ischemia | contraindication | 414795007 | DOID:3393 |
| Porphyria | contraindication | 418470004 | |
| Smokes tobacco daily | contraindication | 449868002 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 12.63 | acidic |
| pKa2 | 13.91 | acidic |
| pKa3 | 1.66 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| cGMP-inhibited 3',5'-cyclic phosphodiesterase A | Enzyme | INHIBITOR | CHEMBL | CHEMBL | |||||
| cAMP-specific 3',5'-cyclic phosphodiesterase 4B | Enzyme | INHIBITOR | WOMBAT-PK | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4018443 | VUID |
| N0000146767 | NUI |
| D00691 | KEGG_DRUG |
| 4018443 | VANDF |
| C0013360 | UMLSCUI |
| CHEBI:4728 | CHEBI |
| X0T | PDB_CHEM_ID |
| CHEMBL1752 | ChEMBL_ID |
| CHEMBL221190 | ChEMBL_ID |
| DB00651 | DRUGBANK_ID |
| 3182 | PUBCHEM_CID |
| C010130 | MESH_SUPPLEMENTAL_RECORD_UI |
| 3714 | RXNORM |
| 3397 | MMSL |
| 4648 | MMSL |
| d00759 | MMSL |
| 000609 | NDDF |
| 32370002 | SNOMEDCT_US |
| 386183006 | SNOMEDCT_US |
| D004400 | MESH_DESCRIPTOR_UI |
| 1365 | INN_ID |
| 7070 | IUPHAR_LIGAND_ID |
| 263T0E9RR9 | UNII |
Pharmaceutical products:
None