Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C11H18N4O4 |
| Molecular Weight | 270.285 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=NC=C(N1CC(O)CN2CCOCC2)[N+]([O-])=O
InChI
InChIKey=GAZGHCHCYRSPIV-UHFFFAOYSA-N
InChI=1S/C11H18N4O4/c1-9-12-6-11(15(17)18)14(9)8-10(16)7-13-2-4-19-5-3-13/h6,10,16H,2-5,7-8H2,1H3
| Molecular Formula | C11H18N4O4 |
| Molecular Weight | 270.285 |
| Charge | 0 |
| Count |
|
| Stereochemistry | RACEMIC |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Optical Activity | ( + / - ) |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/22184458Curator's Comment: description was created based on several sources, including: DOI: 10.5897/AJPP12.1353 | https://www.ncbi.nlm.nih.gov/pubmed/25070100 | https://newdrugapprovals.org/2015/08/11/morinidazole/ | https://www.ncbi.nlm.nih.gov/pubmed/24858695
Sources: https://www.ncbi.nlm.nih.gov/pubmed/22184458
Curator's Comment: description was created based on several sources, including: DOI: 10.5897/AJPP12.1353 | https://www.ncbi.nlm.nih.gov/pubmed/25070100 | https://newdrugapprovals.org/2015/08/11/morinidazole/ | https://www.ncbi.nlm.nih.gov/pubmed/24858695
Morinidazole is a novel third generation 5-nitroimidazole-class antimicrobial agent indicated for the treatment of anaerobic bacterial infections including appendicitis and pelvic inflammatory disease. Morinidazole is administered as a racemate. Morinidazole was approved by China Food and Drug Administration (CFDA) on February, 2014. The bactericidal activity of morinidazole, depends on the formation of a redox intermediate metabolite in the bacterium that causes DNA strand breakage, inhibits repair, and, ultimately leads to cell death. The main adverse effects (all are mild) relate to the drug are dizziness, drowsiness and nausea. Recent in vitro assays have demonstrated that higher antiparasitic potency is observed in S- morinidazole than in R-morinidazole.
Originator
Sources: https://www.pharmacodia.com/yaodu/html/v1/chemicals/c5d736809766d46260d816d8dbc9eb44.html
Curator's Comment: https://newdrugapprovals.org/2015/08/11/morinidazole/
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL1743319 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25070100 |
|||
Target ID: GO:0036473 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22184458 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | 迈灵达® (Mindlinga®) Approved UseMorinidazole is a nitroimidazoles antibiotic indicated for the treatment of bacterial infections including appendicitis and pelvic inflammatory disease (PID) caused by anaerobic bacteria. Launch Date2014 |
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| Curative | 迈灵达® (Mindlinga®) Approved UseMorinidazole is a nitroimidazoles antibiotic indicated for the treatment of bacterial infections including appendicitis and pelvic inflammatory disease (PID) caused by anaerobic bacteria. Launch Date2014 |
|||
Sources: DOI: 10.5897/AJPP12.1353 |
Curative | Unknown Approved UseUnknown |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
12514.09 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32152080/ |
500 mg single, intravenous dose: 500 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
MORINIDAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
10.8 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24820074/ |
500 mg single, intravenous dose: 500 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
MORINIDAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
11.2 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24820074/ |
500 mg single, intravenous dose: 500 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
MORINIDAZOLE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
76830.62 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32152080/ |
500 mg single, intravenous dose: 500 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
MORINIDAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
60.8 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24820074/ |
500 mg single, intravenous dose: 500 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
MORINIDAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
89.5 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24820074/ |
500 mg single, intravenous dose: 500 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
MORINIDAZOLE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
5.94 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32152080/ |
500 mg single, intravenous dose: 500 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
MORINIDAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
5.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24820074/ |
500 mg single, intravenous dose: 500 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
MORINIDAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
7.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24820074/ |
500 mg single, intravenous dose: 500 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
MORINIDAZOLE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
72.8% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24820074/ |
500 mg single, intravenous dose: 500 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
MORINIDAZOLE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
500 mg single, intravenous Studied dose Dose: 500 mg Route: intravenous Route: single Dose: 500 mg Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: unknown Food Status: UNKNOWN Sources: |
|
500 mg single, intravenous Studied dose Dose: 500 mg Route: intravenous Route: single Dose: 500 mg Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: unknown Food Status: UNKNOWN Sources: |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Pharmacokinetics of single-dose morinidazole in patients with severe renal impairment. | 2014-02 |
|
| Simultaneous determination of morinidazole and its carbonylation metabolite in human plasma: application to a pharmacokinetic study involving renal insufficiency patients and healthy volunteers. | 2013-03-25 |
|
| Metabolism and pharmacokinetics of morinidazole in humans: identification of diastereoisomeric morpholine N+-glucuronides catalyzed by UDP glucuronosyltransferase 1A9. | 2012-03 |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.pharmacodia.com/web/drug/1_477.html
500 mg (100 mL injection) twice daily every 6-8 hours continuously for 5-7 days
Route of Administration:
Intravenous
Minimum inhibitory concentration (MIC) of Morinidazole to several anaerobic bacteria: Peptostreptococcus anaerobius (0.25 mg/l); Veillonella parvula (0.31 mg/l); Actinomyces dentocariosus (0.25 mg/l); Porphyromonas gingivalis (2.0 mg/l); Bacteroides thetaiotaomicron (4.0); Prevotella melaninogenica (0.5 mg/l).
| Substance Class |
Chemical
Created
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TUPWG40JAL
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METABOLIC ENZYME -> SUBSTRATE |
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METABOLITE -> PARENT |
PLASMA; URINE
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METABOLITE -> PARENT |
URINE
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METABOLITE -> PARENT |
URINE
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METABOLITE -> PARENT |
URINE
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METABOLITE -> PARENT |
PLASMA; URINE
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METABOLITE -> PARENT |
URINE
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METABOLITE -> PARENT |
PLASMA; URINE
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PLASMA; URINE
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ACTIVE MOIETY |
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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| Biological Half-life | PHARMACOKINETIC |
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INTRAVENOUS INFUSION |
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| Tmax | PHARMACOKINETIC |
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INTRAVENOUS INFUSION |
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