Stem definition | Drug id | CAS RN |
---|---|---|
beta-lactamase inhibitors | 2492 | 68373-14-8 |
Dose | Unit | Route |
---|---|---|
1 | g | P |
Property | Value | Reference |
---|---|---|
MRTD (Maximum Recommended Therapeutic Daily Dose) | 285.97 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
Vd (Volume of distribution) | 0.32 L/kg | Lombardo F, Berellini G, Obach RS |
CL (Clearance) | 5.10 mL/min/kg | Lombardo F, Berellini G, Obach RS |
fu (Fraction unbound in plasma) | 0.62 % | Lombardo F, Berellini G, Obach RS |
t_half (Half-life) | 1.10 hours | Lombardo F, Berellini G, Obach RS |
Date | Agency | Company | Orphan |
---|---|---|---|
Dec. 31, 1986 | FDA | PFIZER |
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 |
---|---|---|---|---|---|---|
Enterocolitis haemorrhagic | 89.50 | 20.58 | 23 | 5915 | 1544 | 53341584 |
Hepatic function abnormal | 81.77 | 20.58 | 51 | 5887 | 36848 | 53306280 |
Pyrexia | 73.18 | 20.58 | 147 | 5791 | 403046 | 52940082 |
Drug eruption | 69.38 | 20.58 | 40 | 5898 | 25054 | 53318074 |
Klebsiella infection | 59.54 | 20.58 | 25 | 5913 | 7901 | 53335227 |
Renal impairment | 47.08 | 20.58 | 52 | 5886 | 83266 | 53259862 |
Enterococcal infection | 44.14 | 20.58 | 20 | 5918 | 7578 | 53335550 |
Lemierre syndrome | 41.29 | 20.58 | 8 | 5930 | 144 | 53342984 |
Disseminated intravascular coagulation | 40.52 | 20.58 | 26 | 5912 | 19693 | 53323435 |
Infective aneurysm | 37.80 | 20.58 | 9 | 5929 | 440 | 53342688 |
Fatigue | 36.51 | 20.58 | 18 | 5920 | 730488 | 52612640 |
Linear IgA disease | 35.46 | 20.58 | 11 | 5927 | 1459 | 53341669 |
Toxic epidermal necrolysis | 34.04 | 20.58 | 25 | 5913 | 23525 | 53319603 |
Pneumonia aspiration | 33.67 | 20.58 | 29 | 5909 | 34272 | 53308856 |
Arthralgia | 32.71 | 20.58 | 5 | 5933 | 439778 | 52903350 |
Interstitial lung disease | 32.08 | 20.58 | 36 | 5902 | 58586 | 53284542 |
Multiple organ dysfunction syndrome | 31.86 | 20.58 | 35 | 5903 | 55642 | 53287486 |
Culture stool positive | 30.07 | 20.58 | 7 | 5931 | 310 | 53342818 |
Pneumonia | 29.70 | 20.58 | 106 | 5832 | 407063 | 52936065 |
Pathogen resistance | 28.10 | 20.58 | 14 | 5924 | 6546 | 53336582 |
Eosinophilic pneumonia acute | 27.95 | 20.58 | 7 | 5931 | 423 | 53342705 |
Premature delivery | 27.52 | 20.58 | 23 | 5915 | 26081 | 53317047 |
Crystal nephropathy | 27.50 | 20.58 | 8 | 5930 | 853 | 53342275 |
Acute disseminated encephalomyelitis | 26.96 | 20.58 | 6 | 5932 | 217 | 53342911 |
Pseudomembranous colitis | 26.80 | 20.58 | 11 | 5927 | 3280 | 53339848 |
Sepsis | 24.74 | 20.58 | 52 | 5886 | 146377 | 53196751 |
Red blood cells urine positive | 24.59 | 20.58 | 10 | 5928 | 2914 | 53340214 |
Candida infection | 24.06 | 20.58 | 21 | 5917 | 25252 | 53317876 |
Platelet count decreased | 23.88 | 20.58 | 43 | 5895 | 108056 | 53235072 |
Chorioretinopathy | 22.89 | 20.58 | 7 | 5931 | 886 | 53342242 |
Proteus infection | 22.75 | 20.58 | 7 | 5931 | 904 | 53342224 |
Acute generalised exanthematous pustulosis | 22.22 | 20.58 | 14 | 5924 | 10267 | 53332861 |
Klebsiella test positive | 21.88 | 20.58 | 7 | 5931 | 1026 | 53342102 |
Implant site hypersensitivity | 21.66 | 20.58 | 4 | 5934 | 55 | 53343073 |
Neuromuscular block prolonged | 21.54 | 20.58 | 6 | 5932 | 547 | 53342581 |
Shock haemorrhagic | 21.09 | 20.58 | 13 | 5925 | 9170 | 53333958 |
Septic shock | 20.95 | 20.58 | 30 | 5908 | 62199 | 53280929 |
Systemic candida | 20.82 | 20.58 | 9 | 5929 | 3048 | 53340080 |
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 |
---|---|---|---|---|---|---|
Hepatic function abnormal | 120.38 | 18.58 | 94 | 7761 | 44746 | 32460925 |
Pneumonia | 73.12 | 18.58 | 219 | 7636 | 355033 | 32150638 |
Enterocolitis haemorrhagic | 72.81 | 18.58 | 21 | 7834 | 990 | 32504681 |
Pneumonia aspiration | 54.38 | 18.58 | 58 | 7797 | 41098 | 32464573 |
Interstitial lung disease | 53.55 | 18.58 | 72 | 7783 | 64929 | 32440742 |
Cardiac septal defect | 51.29 | 18.58 | 12 | 7843 | 244 | 32505427 |
Hangover | 49.86 | 18.58 | 16 | 7839 | 1083 | 32504588 |
Pathogen resistance | 46.87 | 18.58 | 29 | 7826 | 9481 | 32496190 |
Kidney duplex | 45.79 | 18.58 | 12 | 7843 | 394 | 32505277 |
Pyrexia | 43.44 | 18.58 | 172 | 7683 | 319796 | 32185875 |
Drug eruption | 42.53 | 18.58 | 36 | 7819 | 19130 | 32486541 |
Rash | 41.82 | 18.58 | 128 | 7727 | 209205 | 32296466 |
Klebsiella infection | 38.39 | 18.58 | 24 | 7831 | 7988 | 32497683 |
Incision site pain | 36.76 | 18.58 | 15 | 7840 | 2022 | 32503649 |
Toxic epidermal necrolysis | 36.37 | 18.58 | 34 | 7821 | 20559 | 32485112 |
Wound dehiscence | 31.92 | 18.58 | 16 | 7839 | 3480 | 32502191 |
C-reactive protein increased | 31.79 | 18.58 | 48 | 7807 | 48054 | 32457617 |
Clostridium test positive | 31.64 | 18.58 | 14 | 7841 | 2303 | 32503368 |
Drug-induced liver injury | 30.16 | 18.58 | 33 | 7822 | 24030 | 32481641 |
Stevens-Johnson syndrome | 29.46 | 18.58 | 29 | 7826 | 18680 | 32486991 |
Liver disorder | 29.04 | 18.58 | 37 | 7818 | 31617 | 32474054 |
Multiple-drug resistance | 27.93 | 18.58 | 15 | 7840 | 3760 | 32501911 |
Pseudomembranous colitis | 27.88 | 18.58 | 14 | 7841 | 3058 | 32502613 |
Death | 27.80 | 18.58 | 31 | 7824 | 382486 | 32123185 |
Septic shock | 27.43 | 18.58 | 55 | 7800 | 68934 | 32436737 |
Pneumonia bacterial | 25.57 | 18.58 | 21 | 7834 | 10695 | 32494976 |
Megacolon | 24.99 | 18.58 | 11 | 7844 | 1787 | 32503884 |
Acute generalised exanthematous pustulosis | 24.81 | 18.58 | 17 | 7838 | 6596 | 32499075 |
Lymphocyte count decreased | 24.81 | 18.58 | 28 | 7827 | 21091 | 32484580 |
Enterococcus test positive | 24.79 | 18.58 | 9 | 7846 | 885 | 32504786 |
Fungaemia | 24.31 | 18.58 | 12 | 7843 | 2527 | 32503144 |
Stenotrophomonas test positive | 24.26 | 18.58 | 7 | 7848 | 330 | 32505341 |
Platelet count decreased | 23.67 | 18.58 | 71 | 7784 | 114520 | 32391151 |
Respiratory failure | 23.66 | 18.58 | 68 | 7787 | 107114 | 32398557 |
Rebound effect | 23.58 | 18.58 | 11 | 7844 | 2045 | 32503626 |
Alanine aminotransferase increased | 22.62 | 18.58 | 55 | 7800 | 78424 | 32427247 |
Multiple organ dysfunction syndrome | 22.35 | 18.58 | 51 | 7804 | 69803 | 32435868 |
Renal impairment | 21.91 | 18.58 | 60 | 7795 | 91912 | 32413759 |
Red blood cells urine positive | 21.87 | 18.58 | 10 | 7845 | 1776 | 32503895 |
Pulmonary alveolar haemorrhage | 21.40 | 18.58 | 16 | 7839 | 7113 | 32498558 |
Coagulopathy | 21.38 | 18.58 | 25 | 7830 | 19552 | 32486119 |
Off label use | 21.01 | 18.58 | 136 | 7719 | 306184 | 32199487 |
Kounis syndrome | 20.94 | 18.58 | 10 | 7845 | 1958 | 32503713 |
Aspartate aminotransferase increased | 20.70 | 18.58 | 48 | 7807 | 66381 | 32439290 |
Arteriospasm coronary | 20.14 | 18.58 | 11 | 7844 | 2849 | 32502822 |
Paradoxical drug reaction | 20.01 | 18.58 | 11 | 7844 | 2885 | 32502786 |
Toxicity to various agents | 20.01 | 18.58 | 9 | 7846 | 178032 | 32327639 |
Disseminated intravascular coagulation | 19.55 | 18.58 | 26 | 7829 | 23150 | 32482521 |
Fall | 19.00 | 18.58 | 12 | 7843 | 196189 | 32309482 |
Blood creatine phosphokinase increased | 18.96 | 18.58 | 37 | 7818 | 45439 | 32460232 |
White blood cell count increased | 18.88 | 18.58 | 35 | 7820 | 41367 | 32464304 |
Protein urine present | 18.88 | 18.58 | 13 | 7842 | 5084 | 32500587 |
Condition aggravated | 18.88 | 18.58 | 81 | 7774 | 155580 | 32350091 |
Source | Code | Description |
---|---|---|
ATC | J01CG01 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE BETA-LACTAM ANTIBACTERIALS, PENICILLINS Beta-lactamase inhibitors |
FDA MoA | N0000000202 | beta Lactamase Inhibitors |
MeSH PA | D000900 | Anti-Bacterial Agents |
MeSH PA | D000890 | Anti-Infective Agents |
MeSH PA | D065093 | beta-Lactamase Inhibitors |
MeSH PA | D004791 | Enzyme Inhibitors |
FDA EPC | N0000175930 | beta Lactamase Inhibitor |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Infection of skin AND/OR subcutaneous tissue | indication | 19824006 | |
Infection due to Escherichia coli | indication | 71057007 | |
Rhinoscleroma | indication | 72409005 | DOID:11336 |
Cholangitis | indication | 82403002 | DOID:9446 |
Female genital tract infection | indication | 125585007 | |
Infectious disease of abdomen | indication | 128070006 | |
Infection due to Enterobacteriaceae | indication | 128945009 | |
Bacterial peritonitis | indication | 197171003 | |
Infection due to Staphylococcus aureus | indication | 406602003 | |
E. Coli Gynecological Infections | indication | ||
Klebsiella Pneumoniae Peritonitis | indication | ||
E. Coli Peritonitis | indication | ||
Skin and Skin Structure Bacteroides Fragilis Infection | indication | ||
Bacteroides Gynecological Infections | indication | ||
Inflammatory Disease of Female Pelvic Organs | indication | ||
Skin and Skin Structure Acinetobacter Infection | indication | ||
Bacteroides Peritonitis | indication | ||
Skin and Skin Structure Proteus Infection | indication | ||
Intra-Abdominal E. Coli Abscess | indication | ||
Streptococcal meningitis | off-label use | 4510004 | DOID:11574 |
Pyrexia of unknown origin | off-label use | 7520000 | |
Bacterial pneumonia | off-label use | 53084003 | DOID:874 |
Infection of bone | off-label use | 111253001 | |
Meningococcal meningitis | off-label use | 192644005 | |
Sepsis of the newborn | off-label use | 206376005 | |
Human bite - wound | off-label use | 262555007 | |
Diverticulitis of gastrointestinal tract | off-label use | 271366000 | |
Neonatal meningitis | off-label use | 276674008 | |
Dog bite - wound | off-label use | 283734005 | |
Cat bite - wound | off-label use | 283782004 | |
Infective otitis media | off-label use | 312218008 | |
Diabetic Foot Infection | off-label use | ||
Kidney disease | contraindication | 90708001 | DOID:557 |
Infectious mononucleosis | contraindication | 271558008 | DOID:8568 |
Pseudomembranous enterocolitis | contraindication | 397683000 |
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 3.1 | acidic |
None
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Serine beta-lactamase-like protein LACTB, mitochondrial | Enzyme | IC50 | 5.01 | WOMBAT-PK | |||||
Beta-lactamase TEM | Enzyme | INHIBITOR | Ki | 6.10 | CHEMBL | CHEMBL | |||
Beta-lactamase | Enzyme | IC50 | 4.18 | CHEMBL | |||||
Beta-lactamase SHV-1 | Enzyme | IC50 | 5.41 | CHEMBL | |||||
Beta-lactamase | Enzyme | IC50 | 6 | CHEMBL | |||||
Beta-lactamase OXA-1 | Enzyme | IC50 | 4.66 | CHEMBL | |||||
Beta-lactamase | Enzyme | IC50 | 4.57 | CHEMBL | |||||
Beta-lactamase | Enzyme | IC50 | 5.21 | CHEMBL | |||||
Beta-lactamase | Enzyme | IC50 | 7.12 | CHEMBL | |||||
Carbapenem-hydrolizing beta-lactamase SFC-1 | Enzyme | IC50 | 4.64 | CHEMBL | |||||
Beta-lactamase GES-13 | Enzyme | IC50 | 6.43 | CHEMBL | |||||
Class D beta-lactamase | Unclassified | IC50 | 4.92 | CHEMBL | |||||
Beta-lactamase | Enzyme | IC50 | 5.62 | CHEMBL | |||||
Beta-lactamase | Enzyme | IC50 | 5.95 | CHEMBL | |||||
Beta-lactamase | Enzyme | IC50 | 5.11 | CHEMBL | |||||
Beta-lactamase | Enzyme | IC50 | 5.40 | CHEMBL | |||||
Beta-lactamase TEM | Enzyme | Ki | 6.10 | WOMBAT-PK | |||||
ADC-18 protein | Enzyme | IC50 | 4.93 | CHEMBL | |||||
Beta-lactamase 1 | Enzyme | IC50 | 4.60 | CHEMBL | |||||
Beta-lactamase | Enzyme | IC50 | 5.52 | CHEMBL | |||||
Beta-lactamase | Enzyme | IC50 | 5.19 | CHEMBL | |||||
Beta-lactamase | Enzyme | IC50 | 5.52 | CHEMBL |
ID | Source |
---|---|
4019937 | VUID |
N0000148022 | NUI |
D02223 | KEGG_DRUG |
69388-84-7 | SECONDARY_CAS_RN |
4019381 | VANDF |
4019937 | VANDF |
C0038665 | UMLSCUI |
CHEBI:9321 | CHEBI |
0RN | PDB_CHEM_ID |
CHEMBL403 | ChEMBL_ID |
DB09324 | DRUGBANK_ID |
CHEMBL1200944 | ChEMBL_ID |
D013407 | MESH_DESCRIPTOR_UI |
130313 | PUBCHEM_CID |
4845 | INN_ID |
10769 | IUPHAR_LIGAND_ID |
S4TF6I2330 | UNII |
10167 | RXNORM |
5520 | MMSL |
d04403 | MMSL |
002811 | NDDF |
002812 | NDDF |
398916003 | SNOMEDCT_US |
412516007 | SNOMEDCT_US |
96008003 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
UNASYN | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0049-0013 | INJECTION, POWDER, FOR SOLUTION | 0.50 g | INTRAMUSCULAR | NDA | 26 sections |
UNASYN | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0049-0014 | INJECTION, POWDER, FOR SOLUTION | 1 g | INTRAMUSCULAR | NDA | 26 sections |
UNASYN | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0049-0024 | INJECTION, POWDER, FOR SOLUTION | 50 mg | INTRAMUSCULAR | NDA | 25 sections |
UNASYN | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0049-0031 | INJECTION, POWDER, FOR SOLUTION | 0.50 g | INTRAMUSCULAR | ANDA | 26 sections |
UNASYN | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0049-0032 | INJECTION, POWDER, FOR SOLUTION | 1 g | INTRAMUSCULAR | ANDA | 26 sections |
Ampicillin and Sulbactam | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0409-2689 | INJECTION, POWDER, FOR SOLUTION | 0.50 g | INTRAVENOUS | ANDA | 25 sections |
Ampicillin and Sulbactam | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0409-2987 | INJECTION, POWDER, FOR SOLUTION | 1 g | INTRAVENOUS | ANDA | 25 sections |
Ampicillin and Sulbactam | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0641-6116 | INJECTION, POWDER, FOR SOLUTION | 0.50 g | INTRAVENOUS | ANDA | 24 sections |
Ampicillin and Sulbactam | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0641-6117 | INJECTION, POWDER, FOR SOLUTION | 1 g | INTRAVENOUS | ANDA | 24 sections |
Ampicillin and Sulbactam | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0641-6118 | INJECTION, POWDER, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 24 sections |
Ampicillin and Sulbactam | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0641-6119 | INJECTION, POWDER, FOR SOLUTION | 0.50 g | INTRAVENOUS | ANDA | 25 sections |
Ampicillin and Sulbactam | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0641-6120 | INJECTION, POWDER, FOR SOLUTION | 1 g | INTRAVENOUS | ANDA | 25 sections |
Ampicillin and Sulbactam | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0641-6121 | INJECTION, POWDER, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 24 sections |
Ampicillin and Sulbactam | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0641-6122 | INJECTION, POWDER, FOR SOLUTION | 125 mg | INTRAVENOUS | ANDA | 25 sections |
Ampicillin and Sulbactam | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0641-6123 | INJECTION, POWDER, FOR SOLUTION | 125 mg | INTRAVENOUS | ANDA | 25 sections |
ampicillin and sulbactam | HUMAN PRESCRIPTION DRUG LABEL | 2 | 25021-142 | INJECTION, POWDER, FOR SOLUTION | 0.50 g | INTRAVENOUS | ANDA | 25 sections |
ampicillin and sulbactam | HUMAN PRESCRIPTION DRUG LABEL | 2 | 25021-143 | INJECTION, POWDER, FOR SOLUTION | 1 g | INTRAVENOUS | ANDA | 25 sections |
ampicillin and sulbactam | HUMAN PRESCRIPTION DRUG LABEL | 2 | 25021-144 | INJECTION, POWDER, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 25 sections |
Ampicillin and Sulbactam | HUMAN PRESCRIPTION DRUG LABEL | 2 | 36000-094 | INJECTION, POWDER, FOR SOLUTION | 0.50 g | INTRAVENOUS | ANDA | 26 sections |
Ampicillin and Sulbactam | HUMAN PRESCRIPTION DRUG LABEL | 2 | 36000-095 | INJECTION, POWDER, FOR SOLUTION | 1 g | INTRAVENOUS | ANDA | 26 sections |
Ampicillin and Sulbactam | HUMAN PRESCRIPTION DRUG LABEL | 2 | 44567-150 | INJECTION, POWDER, FOR SOLUTION | 1 g | INTRAVENOUS | ANDA | 23 sections |
Ampicillin and Sulbactam | HUMAN PRESCRIPTION DRUG LABEL | 2 | 44567-210 | INJECTION, POWDER, FOR SOLUTION | 0.50 g | INTRAVENOUS | ANDA | 23 sections |
Ampicillin and Sulbactam | HUMAN PRESCRIPTION DRUG LABEL | 2 | 44567-211 | INJECTION, POWDER, FOR SOLUTION | 1 g | INTRAVENOUS | ANDA | 23 sections |
Ampicillin and Sulbactam | HUMAN PRESCRIPTION DRUG LABEL | 2 | 44567-212 | INJECTION, POWDER, FOR SOLUTION | 5 g | INTRAVENOUS | ANDA | 21 sections |
Ampicillin and Sulbactam | Human Prescription Drug Label | 2 | 55150-116 | INJECTION, POWDER, FOR SOLUTION | 0.50 g | INTRAMUSCULAR | ANDA | 23 sections |
Ampicillin and Sulbactam | Human Prescription Drug Label | 2 | 55150-117 | INJECTION, POWDER, FOR SOLUTION | 1 g | INTRAMUSCULAR | ANDA | 23 sections |
Ampicillin and Sulbactam | Human Prescription Drug Label | 2 | 55150-118 | INJECTION, POWDER, FOR SOLUTION | 50 mg | INTRAVENOUS | ANDA | 23 sections |
Ampicillin and Sulbactam | Human Prescription Drug Label | 2 | 55150-178 | INJECTION, POWDER, FOR SOLUTION | 0.50 g | INTRAVENOUS | ANDA | 22 sections |
Ampicillin and Sulbactam | Human Prescription Drug Label | 2 | 55150-179 | INJECTION, POWDER, FOR SOLUTION | 1 g | INTRAVENOUS | ANDA | 22 sections |
ampicillin and sulbactam | HUMAN PRESCRIPTION DRUG LABEL | 2 | 66794-206 | INJECTION, POWDER, FOR SOLUTION | 0.50 g | INTRAVENOUS | ANDA | 13 sections |