Stem definition | Drug id | CAS RN |
---|---|---|
quinoline derivatives | 2266 | 90-34-6 |
Dose | Unit | Route |
---|---|---|
15 | mg | O |
Property | Value | Reference |
---|---|---|
BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
EoM (Fraction excreted unchanged in urine) | 1 % | Benet LZ, Broccatelli F, Oprea TI |
MRTD (Maximum Recommended Therapeutic Daily Dose) | 2.89 ยตM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
BA (Bioavailability) | 96 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Vd (Volume of distribution) | 4 L/kg | Lombardo F, Berellini G, Obach RS |
CL (Clearance) | 5.80 mL/min/kg | Lombardo F, Berellini G, Obach RS |
t_half (Half-life) | 7.10 hours | Lombardo F, Berellini G, Obach RS |
Date | Agency | Company | Orphan |
---|---|---|---|
Jan. 23, 1952 | FDA | SANOFI AVENTIS US |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Methaemoglobinaemia | 64.92 | 55.44 | 9 | 56 | 2033 | 50603026 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Methaemoglobinaemia | 182.50 | 45.91 | 30 | 264 | 2641 | 29571592 |
Cyanosis | 49.20 | 45.91 | 13 | 281 | 11254 | 29562979 |
Drug clearance increased | 46.12 | 45.91 | 6 | 288 | 97 | 29574136 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Methaemoglobinaemia | 223.39 | 46.23 | 36 | 379 | 4312 | 64494005 |
None
Source | Code | Description |
---|---|---|
ATC | P01BA03 | ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS ANTIPROTOZOALS ANTIMALARIALS Aminoquinolines |
FDA EPC | N0000175482 | Antimalarial |
MeSH PA | D000890 | Anti-Infective Agents |
MeSH PA | D000962 | Antimalarials |
MeSH PA | D000977 | Antiparasitic Agents |
MeSH PA | D000981 | Antiprotozoal Agents |
CHEBI has role | CHEBI:38068 | antimalarials |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Vivax malaria | indication | 27052006 | DOID:12978 |
Ovale malaria | off-label use | 19341001 | DOID:12919 |
Pneumocystosis jiroveci pneumonia | off-label use | 415125002 | DOID:11339 |
Plasmodium Ovale Malaria Prevention | off-label use | ||
Hemolytic anemia | contraindication | 61261009 | DOID:583 |
Anemia due to enzyme deficiency | contraindication | 111577008 | |
Deficiency of glucose-6-phosphate dehydrogenase | contraindication | 124134002 | DOID:2862 |
Deficiency of cytochrome-b>5< reductase | contraindication | 124184009 | |
Pregnancy, function | contraindication | 289908002 | |
Neutropenic disorder | contraindication | 303011007 | DOID:1227 |
Bone marrow depression | contraindication | 307762000 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 10.77 | Basic |
pKa2 | 3.96 | Basic |
None
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 4.67 | WOMBAT-PK | |||||
Sodium-dependent serotonin transporter | Transporter | Ki | 8.08 | DRUG MATRIX | |||||
Hemoglobin subunit alpha | Secreted | WOMBAT-PK | |||||||
Amine oxidase [flavin-containing] B | Enzyme | IC50 | 4.02 | CHEMBL | |||||
Ribosyldihydronicotinamide dehydrogenase [quinone] | Enzyme | IC50 | 5.12 | CHEMBL | |||||
Cytochrome P450 1A2 | Enzyme | IC50 | 6.74 | DRUG MATRIX | |||||
Amine oxidase [flavin-containing] A | Enzyme | IC50 | 4.12 | CHEMBL | |||||
Glucose-6-phosphate 1-dehydrogenase | Enzyme | WOMBAT-PK | |||||||
Heat shock protein HSP 90-alpha | Cytosolic other | IC50 | 8.22 | WOMBAT-PK | |||||
Aryl hydrocarbon receptor | Transcription factor | IC50 | 5.33 | WOMBAT-PK | |||||
Serine hydroxymethyltransferase, mitochondrial | Enzyme | IC50 | 6.36 | CHEMBL | |||||
Reverse transcriptase/RNaseH | Enzyme | IC50 | 4 | CHEMBL | |||||
Reverse transcriptase | Enzyme | IC50 | 4 | CHEMBL | |||||
Chloroquine resistance transporter | Transporter | IC50 | 4.17 | CHEMBL |
ID | Source |
---|---|
4019903 | VUID |
N0000147988 | NUI |
D02126 | KEGG_DRUG |
63-45-6 | SECONDARY_CAS_RN |
4018229 | VANDF |
4019903 | VANDF |
C0033126 | UMLSCUI |
CHEBI:8405 | CHEBI |
1PQ | PDB_CHEM_ID |
CHEMBL506 | ChEMBL_ID |
CHEMBL43128 | ChEMBL_ID |
DB01087 | DRUGBANK_ID |
D011319 | MESH_DESCRIPTOR_UI |
4908 | PUBCHEM_CID |
9952 | IUPHAR_LIGAND_ID |
218 | INN_ID |
MVR3634GX1 | UNII |
8687 | RXNORM |
386 | MMSL |
5354 | MMSL |
d00351 | MMSL |
002941 | NDDF |
004904 | NDDF |
36391008 | SNOMEDCT_US |
426320005 | SNOMEDCT_US |
429663004 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Primaquine Phosphate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0024-1596 | TABLET, FILM COATED | 15 mg | ORAL | NDA | 21 sections |
Primaquine Phosphate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 33261-671 | TABLET | 15 mg | ORAL | ANDA | 18 sections |
PRIMAQUINE PHOSPHATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42291-510 | TABLET, FILM COATED | 15 mg | ORAL | ANDA | 17 sections |
Primaquine Phosphate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43063-225 | TABLET, FILM COATED | 15 mg | ORAL | NDA | 21 sections |
Primaquine Phosphate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43063-225 | TABLET, FILM COATED | 15 mg | ORAL | NDA | 21 sections |
Primaquine Phosphate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43063-721 | TABLET | 15 mg | ORAL | ANDA | 22 sections |
PRIMAQUINE PHOSPHATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50742-191 | TABLET, FILM COATED | 15 mg | ORAL | ANDA | 18 sections |
Primaquine Phosphate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60429-035 | TABLET | 15 mg | ORAL | ANDA | 22 sections |
Primaquine Phosphate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 76385-102 | TABLET | 15 mg | ORAL | ANDA | 22 sections |