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doxapram 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 953 | 309-29-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A central respiratory stimulant with a brief duration of action. (From Martindale, The Extra Pharmocopoeia, 30th ed, p1225)
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.40 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 10.57 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 64 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 1.20 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 5.30 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 4.10 hours | Lombardo F, Berellini G, Obach RS |
| S (Water solubility) | 25 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.125 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.517 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 34.834 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 31.769 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 44.720 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 57.370 | % | High | 1 |
| herg | hERG pIC50 | 4.778 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 6.714 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 116.145 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 44.100 | % | High | 1 |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 1.644 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 86.896 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 45.750 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 6.442 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 1 | High | 1 | |
| pppb | Pig plasma protein binding (% unbound) | 66.410 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 155.239 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 83.110 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 49.420 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 986.279 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| June 23, 1965 | FDA | HIKMA MAPLE |
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 | R07AB01 | RESPIRATORY SYSTEM OTHER RESPIRATORY SYSTEM PRODUCTS OTHER RESPIRATORY SYSTEM PRODUCTS Respiratory stimulants |
| FDA PE | N0000009393 | Increased Medullary Respiratory Drive |
| MeSH PA | D000697 | Central Nervous System Stimulants |
| MeSH PA | D019141 | Respiratory System Agents |
| FDA EPC | N0000175716 | Respiratory Stimulant |
| CHEBI has role | CHEBI:35337 | central nervous system stimulant |
| CHEBI has role | CHEBI:35469 | antidepressant |
Related Drugs by ATC class:
R07AB Respiratory stimulants 8 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Decreased respiratory function | indication | 80954004 | |
| Post-Anesthesia Respiratory Depression | indication | ||
| Apnea in the newborn | off-label use | 13094009 | |
| Cerebral edema | contraindication | 2032001 | |
| Chronic obstructive lung disease | contraindication | 13645005 | DOID:3083 |
| Hyperthyroidism | contraindication | 34486009 | DOID:7998 |
| Pneumothorax | contraindication | 36118008 | |
| Artificial respiration | contraindication | 40617009 | |
| Paralysis | contraindication | 44695005 | |
| Conduction disorder of the heart | contraindication | 44808001 | |
| Low blood pressure | contraindication | 45007003 | |
| Fibrosis of lung | contraindication | 51615001 | DOID:3770 |
| Coronary arteriosclerosis | contraindication | 53741008 | DOID:3393 |
| Neuromuscular block, function | contraindication | 55394004 | |
| Flail chest | contraindication | 78011002 | |
| Injury of head | contraindication | 82271004 | |
| Epilepsy | contraindication | 84757009 | DOID:1826 |
| Leukopenia | contraindication | 84828003 | DOID:615 |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Decompensated cardiac failure | contraindication | 195111005 | |
| Asthma | contraindication | 195967001 | DOID:2841 |
| Cerebrovascular accident | contraindication | 230690007 | |
| Pulmonary thromboembolism | contraindication | 233935004 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Pheochromocytoma | contraindication | 302835009 | |
| Hypertensive urgency | contraindication | 443482000 | |
| Acute exacerbation of asthma | contraindication | 708038006 | |
| Physical Obstruction of Respiratory Tract | contraindication |
🐶 Veterinary Drug Use
| Species | Use | Relation |
|---|---|---|
| Cats | Stimulation of respiration during and after general anesthesia | Indication |
| Cats | Acceleration of awakening and return of reflexes after anesthesia | Indication |
| Cats | To initiate respiration following dystocia or caesarean section | Indication |
| Cats | Stimulation of respiration following dystocia or caesarean section | Indication |
| Dogs | Stimulation of respiration during and after general anesthesia | Indication |
| Dogs | Acceleration of awakening and return of reflexes after anesthesia | Indication |
| Dogs | To initiate respiration following dystocia or caesarean section | Indication |
| Dogs | Stimulation of respiration following dystocia or caesarean section | Indication |
| Horses | Stimulation of respiration during and after general anesthesia | Indication |
| Horses | Acceleration of awakening and return of reflexes after anesthesia | Indication |
🐶 Veterinary products
| Product | Applicant | Ingredients |
|---|---|---|
| Dopram-V Injectable | Boehringer lngelheim Animal Health USA Inc. | 1 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 7.03 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Potassium channel subfamily K member 3 | Ion channel | BLOCKER | CHEMBL | CHEMBL | |||||
| Potassium channel subfamily K member 9 | Ion channel | BLOCKER | CHEMBL | CHEMBL | |||||
| Cytochrome P450 2D6 | Enzyme | IC50 | 7 | DRUG MATRIX | |||||
| Potassium channel subfamily K member 3 | Ion channel | IC50 | 6.39 | CHEMBL | |||||
| Potassium channel subfamily K member 9 | Ion channel | IC50 | 4.80 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D07873 | KEGG_DRUG |
| 7081-53-0 | SECONDARY_CAS_RN |
| 4018416 | VANDF |
| 4019734 | VANDF |
| C0013084 | UMLSCUI |
| CHEBI:681848 | CHEBI |
| CHEMBL1754 | ChEMBL_ID |
| CHEMBL3989519 | ChEMBL_ID |
| DB00561 | DRUGBANK_ID |
| D004315 | MESH_DESCRIPTOR_UI |
| 3156 | PUBCHEM_CID |
| 7169 | IUPHAR_LIGAND_ID |
| 1462 | INN_ID |
| 94F3830Q73 | UNII |
| 202987 | RXNORM |
| 3192 | MMSL |
| 332 | MMSL |
| 4636 | MMSL |
| d00802 | MMSL |
| 001383 | NDDF |
| 004577 | NDDF |
| 28235004 | SNOMEDCT_US |
| 373339005 | SNOMEDCT_US |
| 84748003 | SNOMEDCT_US |
| 94F3830Q73 | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Dopram | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0641-6018 | INJECTION | 20 mg | INTRAVENOUS | NDA | 20 sections |
| DOXAPRAM HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51662-1404 | INJECTION | 20 mg | INTRAVENOUS | NDA | 12 sections |