Details
Stereochemistry | RACEMIC |
Molecular Formula | C19H22FN3O3 |
Molecular Weight | 359.3947 |
Optical Activity | ( + / - ) |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1CN(CCN1)C2=C(F)C(C)=C3C(=O)C(=CN(C4CC4)C3=C2)C(O)=O
InChI
InChIKey=AIJTTZAVMXIJGM-UHFFFAOYSA-N
InChI=1S/C19H22FN3O3/c1-10-8-22(6-5-21-10)15-7-14-16(11(2)17(15)20)18(24)13(19(25)26)9-23(14)12-3-4-12/h7,9-10,12,21H,3-6,8H2,1-2H3,(H,25,26)
Molecular Formula | C19H22FN3O3 |
Molecular Weight | 359.3947 |
Charge | 0 |
Count |
|
Stereochemistry | RACEMIC |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Optical Activity | ( + / - ) |
DescriptionCurator's Comment: description was created based on several sources, including
http://www.accessdata.fda.gov/drugsatfda_docs/nda/97/20-695_Raxar_Pharma.pdf | https://www.drugbank.ca/drugs/DB00365
Curator's Comment: description was created based on several sources, including
http://www.accessdata.fda.gov/drugsatfda_docs/nda/97/20-695_Raxar_Pharma.pdf | https://www.drugbank.ca/drugs/DB00365
Grepafloxacin is a monofluorinated quinolone with a cyclopropyl group at position 1, a 3-methyl-1piperazinyl group at position 7 and a methyl substitution at the 5 position, that was synthesized by Otsuka in Japan. It exhibited in vitro activity against a wide variety of both Gram-positive and Gram-negative bacteria including anaerobic species. The compound was reported to have a broad spectrum of activity, particularly against pathogens responsible for community-acquired respiratory infections including those caused by beta-lactam and macrolide-resistant strains of Streptococcus pneumoniae and Haemophilus influenzae. Japanese researchers also reported that unlike other quinolones, grepafloxacin reached high levels in the bile and might also be useful in the treatment of biliary tract infection. Grepafloxacin was administered once daily and did not require dosage adjustment for renal insufficiency, but grepafloxacin tablets were contraindicated in patients with hepatic failure. Otsuka Pharmaceutical signed a licensing agreement for grepafloxacin with GlaxoSmithKline. According to this agreement, GlaxoSmithKline had marketing rights to grepafloxacin in Europe, USA, and certain other markets. Otsuka retained rights for Japan and some Asian countries
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2363076 Sources: https://www.ncbi.nlm.nih.gov/pubmed/10824040 |
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Target ID: CHEMBL2094255 Sources: https://www.ncbi.nlm.nih.gov/pubmed/10824040 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Curative | RAXAR Approved UseRAXAR Tablets are Indicated for treatment of adults with mild to moderate infections caused by susceptible strains of the designated microorganisms in the infections listed below: Acute Bacterial Exacerbations of Chronic Bronchitis caused by Haemophilus influenzae, Streptococcus pneumoniae, or Moraxella catarrhalis. Community-acquired Pneumonia caused by Haemophilus influenzae, Streptococcus pneumoniae, Moraxella catarrhalis, or Mycoplasma pneumonia. Uncomplicated Gonorrhea (urethral In males and endocervical and rectal in females) caused by Neissen'a gononrhoeae. Nongonococcal Urethritis and Cervicitis caused by Chlamydia trachomatis Launch Date1997 |
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Curative | RAXAR Approved UseRAXAR Tablets are Indicated for treatment of adults with mild to moderate infections caused by susceptible strains of the designated microorganisms in the infections listed below: Acute Bacterial Exacerbations of Chronic Bronchitis caused by Haemophilus influenzae, Streptococcus pneumoniae, or Moraxella catarrhalis. Community-acquired Pneumonia caused by Haemophilus influenzae, Streptococcus pneumoniae, Moraxella catarrhalis, or Mycoplasma pneumonia. Uncomplicated Gonorrhea (urethral In males and endocervical and rectal in females) caused by Neissen'a gononrhoeae. Nongonococcal Urethritis and Cervicitis caused by Chlamydia trachomatis Launch Date1997 |
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Curative | RAXAR Approved UseRAXAR Tablets are Indicated for treatment of adults with mild to moderate infections caused by susceptible strains of the designated microorganisms in the infections listed below: Acute Bacterial Exacerbations of Chronic Bronchitis caused by Haemophilus influenzae, Streptococcus pneumoniae, or Moraxella catarrhalis. Community-acquired Pneumonia caused by Haemophilus influenzae, Streptococcus pneumoniae, Moraxella catarrhalis, or Mycoplasma pneumonia. Uncomplicated Gonorrhea (urethral In males and endocervical and rectal in females) caused by Neissen'a gononrhoeae. Nongonococcal Urethritis and Cervicitis caused by Chlamydia trachomatis Launch Date1997 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1.43 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
400 mg 1 times / day steady-state, oral dose: 400 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
GREPAFLOXACIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
2.63 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
800 mg 1 times / day steady-state, oral dose: 800 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
GREPAFLOXACIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
0.93 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
GREPAFLOXACIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
1.41 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered: |
GREPAFLOXACIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
2.26 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered: |
GREPAFLOXACIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
3.17 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
1200 mg single, oral dose: 1200 mg route of administration: Oral experiment type: SINGLE co-administered: |
GREPAFLOXACIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
0.47 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered: |
GREPAFLOXACIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
14.6 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
400 mg 1 times / day steady-state, oral dose: 400 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
GREPAFLOXACIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
32.2 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
800 mg 1 times / day steady-state, oral dose: 800 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
GREPAFLOXACIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
11.35 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
GREPAFLOXACIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
19.73 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered: |
GREPAFLOXACIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
27.69 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered: |
GREPAFLOXACIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
45.04 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
1200 mg single, oral dose: 1200 mg route of administration: Oral experiment type: SINGLE co-administered: |
GREPAFLOXACIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
5.08 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered: |
GREPAFLOXACIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
11.68 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
GREPAFLOXACIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
12.67 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered: |
GREPAFLOXACIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
12.25 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered: |
GREPAFLOXACIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
11.68 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
1200 mg single, oral dose: 1200 mg route of administration: Oral experiment type: SINGLE co-administered: |
GREPAFLOXACIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
10.14 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered: |
GREPAFLOXACIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
50% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
400 mg 1 times / day steady-state, oral dose: 400 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
GREPAFLOXACIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
50% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
800 mg 1 times / day steady-state, oral dose: 800 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
GREPAFLOXACIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
50% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
GREPAFLOXACIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
50% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered: |
GREPAFLOXACIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
50% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered: |
GREPAFLOXACIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
50% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
1200 mg single, oral dose: 1200 mg route of administration: Oral experiment type: SINGLE co-administered: |
GREPAFLOXACIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
50% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered: |
GREPAFLOXACIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
400 mg 1 times / day steady, oral Recommended Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, 47.7 years n = 207 Health Status: unhealthy Condition: infections Age Group: 47.7 years Sex: M+F Population Size: 207 Sources: |
Disc. AE: Nausea, Vomiting... AEs leading to discontinuation/dose reduction: Nausea (3 patients) Sources: Vomiting (1 patient) Taste perversion (2 patients) Dizziness (3 patients) Diarrhea (2 patients) |
600 mg 1 times / day steady, oral Recommended Dose: 600 mg, 1 times / day Route: oral Route: steady Dose: 600 mg, 1 times / day Sources: |
unhealthy, 48.4 years n = 204 Health Status: unhealthy Condition: infections Age Group: 48.4 years Sex: M+F Population Size: 204 Sources: |
Disc. AE: Nausea, Vomiting... AEs leading to discontinuation/dose reduction: Nausea (8 patients) Sources: Vomiting (4 patients) Taste perversion (5 patients) Dizziness (3 patients) Diarrhea (1 patient) |
200 mg 1 times / day steady, oral Recommended Dose: 200 mg, 1 times / day Route: oral Route: steady Dose: 200 mg, 1 times / day Sources: |
unhealthy, adult n = 86 Health Status: unhealthy Condition: lower respiratory tract infections or sexually transmitted infections Age Group: adult Sex: M+F Population Size: 86 Sources: |
Disc. AE: Nausea, Vomiting... AEs leading to discontinuation/dose reduction: Nausea (1.2%) Sources: Vomiting (1.2%) |
400 mg 1 times / day steady, oral Recommended Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, adult n = 1069 Health Status: unhealthy Condition: lower respiratory tract infections or sexually transmitted infections Age Group: adult Sex: M+F Population Size: 1069 Sources: |
Disc. AE: Bad taste, Nausea... AEs leading to discontinuation/dose reduction: Bad taste (0.3%) Sources: Nausea (0.8%) Vomiting (0.6%) Headache (0.3%) Dizziness (0.5%) Rash (0.2%) Tachycardia (<0.1%) |
600 mg 1 times / day steady, oral Recommended Dose: 600 mg, 1 times / day Route: oral Route: steady Dose: 600 mg, 1 times / day Sources: |
unhealthy, adult n = 1406 Health Status: unhealthy Condition: lower respiratory tract infections or sexually transmitted infections Age Group: adult Sex: M+F Population Size: 1406 Sources: |
Disc. AE: Bad taste, Nausea... AEs leading to discontinuation/dose reduction: Bad taste (1%) Sources: Nausea (2.6%) Vomiting (1.4%) Headache (0.6%) Dizziness (0.6%) Rash (0.6%) Tachycardia (0.14%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Vomiting | 1 patient Disc. AE |
400 mg 1 times / day steady, oral Recommended Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, 47.7 years n = 207 Health Status: unhealthy Condition: infections Age Group: 47.7 years Sex: M+F Population Size: 207 Sources: |
Diarrhea | 2 patients Disc. AE |
400 mg 1 times / day steady, oral Recommended Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, 47.7 years n = 207 Health Status: unhealthy Condition: infections Age Group: 47.7 years Sex: M+F Population Size: 207 Sources: |
Taste perversion | 2 patients Disc. AE |
400 mg 1 times / day steady, oral Recommended Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, 47.7 years n = 207 Health Status: unhealthy Condition: infections Age Group: 47.7 years Sex: M+F Population Size: 207 Sources: |
Dizziness | 3 patients Disc. AE |
400 mg 1 times / day steady, oral Recommended Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, 47.7 years n = 207 Health Status: unhealthy Condition: infections Age Group: 47.7 years Sex: M+F Population Size: 207 Sources: |
Nausea | 3 patients Disc. AE |
400 mg 1 times / day steady, oral Recommended Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, 47.7 years n = 207 Health Status: unhealthy Condition: infections Age Group: 47.7 years Sex: M+F Population Size: 207 Sources: |
Diarrhea | 1 patient Disc. AE |
600 mg 1 times / day steady, oral Recommended Dose: 600 mg, 1 times / day Route: oral Route: steady Dose: 600 mg, 1 times / day Sources: |
unhealthy, 48.4 years n = 204 Health Status: unhealthy Condition: infections Age Group: 48.4 years Sex: M+F Population Size: 204 Sources: |
Dizziness | 3 patients Disc. AE |
600 mg 1 times / day steady, oral Recommended Dose: 600 mg, 1 times / day Route: oral Route: steady Dose: 600 mg, 1 times / day Sources: |
unhealthy, 48.4 years n = 204 Health Status: unhealthy Condition: infections Age Group: 48.4 years Sex: M+F Population Size: 204 Sources: |
Vomiting | 4 patients Disc. AE |
600 mg 1 times / day steady, oral Recommended Dose: 600 mg, 1 times / day Route: oral Route: steady Dose: 600 mg, 1 times / day Sources: |
unhealthy, 48.4 years n = 204 Health Status: unhealthy Condition: infections Age Group: 48.4 years Sex: M+F Population Size: 204 Sources: |
Taste perversion | 5 patients Disc. AE |
600 mg 1 times / day steady, oral Recommended Dose: 600 mg, 1 times / day Route: oral Route: steady Dose: 600 mg, 1 times / day Sources: |
unhealthy, 48.4 years n = 204 Health Status: unhealthy Condition: infections Age Group: 48.4 years Sex: M+F Population Size: 204 Sources: |
Nausea | 8 patients Disc. AE |
600 mg 1 times / day steady, oral Recommended Dose: 600 mg, 1 times / day Route: oral Route: steady Dose: 600 mg, 1 times / day Sources: |
unhealthy, 48.4 years n = 204 Health Status: unhealthy Condition: infections Age Group: 48.4 years Sex: M+F Population Size: 204 Sources: |
Nausea | 1.2% Disc. AE |
200 mg 1 times / day steady, oral Recommended Dose: 200 mg, 1 times / day Route: oral Route: steady Dose: 200 mg, 1 times / day Sources: |
unhealthy, adult n = 86 Health Status: unhealthy Condition: lower respiratory tract infections or sexually transmitted infections Age Group: adult Sex: M+F Population Size: 86 Sources: |
Vomiting | 1.2% Disc. AE |
200 mg 1 times / day steady, oral Recommended Dose: 200 mg, 1 times / day Route: oral Route: steady Dose: 200 mg, 1 times / day Sources: |
unhealthy, adult n = 86 Health Status: unhealthy Condition: lower respiratory tract infections or sexually transmitted infections Age Group: adult Sex: M+F Population Size: 86 Sources: |
Rash | 0.2% Disc. AE |
400 mg 1 times / day steady, oral Recommended Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, adult n = 1069 Health Status: unhealthy Condition: lower respiratory tract infections or sexually transmitted infections Age Group: adult Sex: M+F Population Size: 1069 Sources: |
Bad taste | 0.3% Disc. AE |
400 mg 1 times / day steady, oral Recommended Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, adult n = 1069 Health Status: unhealthy Condition: lower respiratory tract infections or sexually transmitted infections Age Group: adult Sex: M+F Population Size: 1069 Sources: |
Headache | 0.3% Disc. AE |
400 mg 1 times / day steady, oral Recommended Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, adult n = 1069 Health Status: unhealthy Condition: lower respiratory tract infections or sexually transmitted infections Age Group: adult Sex: M+F Population Size: 1069 Sources: |
Dizziness | 0.5% Disc. AE |
400 mg 1 times / day steady, oral Recommended Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, adult n = 1069 Health Status: unhealthy Condition: lower respiratory tract infections or sexually transmitted infections Age Group: adult Sex: M+F Population Size: 1069 Sources: |
Vomiting | 0.6% Disc. AE |
400 mg 1 times / day steady, oral Recommended Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, adult n = 1069 Health Status: unhealthy Condition: lower respiratory tract infections or sexually transmitted infections Age Group: adult Sex: M+F Population Size: 1069 Sources: |
Nausea | 0.8% Disc. AE |
400 mg 1 times / day steady, oral Recommended Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, adult n = 1069 Health Status: unhealthy Condition: lower respiratory tract infections or sexually transmitted infections Age Group: adult Sex: M+F Population Size: 1069 Sources: |
Tachycardia | <0.1% Disc. AE |
400 mg 1 times / day steady, oral Recommended Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, adult n = 1069 Health Status: unhealthy Condition: lower respiratory tract infections or sexually transmitted infections Age Group: adult Sex: M+F Population Size: 1069 Sources: |
Tachycardia | 0.14% Disc. AE |
600 mg 1 times / day steady, oral Recommended Dose: 600 mg, 1 times / day Route: oral Route: steady Dose: 600 mg, 1 times / day Sources: |
unhealthy, adult n = 1406 Health Status: unhealthy Condition: lower respiratory tract infections or sexually transmitted infections Age Group: adult Sex: M+F Population Size: 1406 Sources: |
Dizziness | 0.6% Disc. AE |
600 mg 1 times / day steady, oral Recommended Dose: 600 mg, 1 times / day Route: oral Route: steady Dose: 600 mg, 1 times / day Sources: |
unhealthy, adult n = 1406 Health Status: unhealthy Condition: lower respiratory tract infections or sexually transmitted infections Age Group: adult Sex: M+F Population Size: 1406 Sources: |
Headache | 0.6% Disc. AE |
600 mg 1 times / day steady, oral Recommended Dose: 600 mg, 1 times / day Route: oral Route: steady Dose: 600 mg, 1 times / day Sources: |
unhealthy, adult n = 1406 Health Status: unhealthy Condition: lower respiratory tract infections or sexually transmitted infections Age Group: adult Sex: M+F Population Size: 1406 Sources: |
Rash | 0.6% Disc. AE |
600 mg 1 times / day steady, oral Recommended Dose: 600 mg, 1 times / day Route: oral Route: steady Dose: 600 mg, 1 times / day Sources: |
unhealthy, adult n = 1406 Health Status: unhealthy Condition: lower respiratory tract infections or sexually transmitted infections Age Group: adult Sex: M+F Population Size: 1406 Sources: |
Bad taste | 1% Disc. AE |
600 mg 1 times / day steady, oral Recommended Dose: 600 mg, 1 times / day Route: oral Route: steady Dose: 600 mg, 1 times / day Sources: |
unhealthy, adult n = 1406 Health Status: unhealthy Condition: lower respiratory tract infections or sexually transmitted infections Age Group: adult Sex: M+F Population Size: 1406 Sources: |
Vomiting | 1.4% Disc. AE |
600 mg 1 times / day steady, oral Recommended Dose: 600 mg, 1 times / day Route: oral Route: steady Dose: 600 mg, 1 times / day Sources: |
unhealthy, adult n = 1406 Health Status: unhealthy Condition: lower respiratory tract infections or sexually transmitted infections Age Group: adult Sex: M+F Population Size: 1406 Sources: |
Nausea | 2.6% Disc. AE |
600 mg 1 times / day steady, oral Recommended Dose: 600 mg, 1 times / day Route: oral Route: steady Dose: 600 mg, 1 times / day Sources: |
unhealthy, adult n = 1406 Health Status: unhealthy Condition: lower respiratory tract infections or sexually transmitted infections Age Group: adult Sex: M+F Population Size: 1406 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
yes | ||||
yes |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
yes | ||||
yes |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
PubMed
Title | Date | PubMed |
---|---|---|
Anti-toxoplasma activities of 24 quinolones and fluoroquinolones in vitro: prediction of activity by molecular topology and virtual computational techniques. | 2000 Oct |
|
Prediction of quinolone activity against Mycobacterium avium by molecular topology and virtual computational screening. | 2000 Oct |
|
Comparison of antimycobacterial activity of grepafloxacin against Mycobacterium avium with that of levofloxacin: accumulation of grepafloxacin in human macrophages. | 2001 Mar |
|
Torsades de pointes associated with fluoroquinolones: importance of concomitant risk factors. | 2004 Mar |
Patents
Sample Use Guides
RAXAR (Grepafloxacin) Tablets may be taken with or without meals. The usual dose for RAXAR is 400 mg or 600 mg orally every 24 hours. Sucralfate; antacids containing magnesium, calcium, or aluminum; multivitamins containing iron or zinc; or VIDEX (didanosine) chewable/buffered tablets or the pediatric powder for oral solution should not be taken within 4 hours before or 4 hours after taking grepafloxacin.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/9484871
The activity of grepafloxacin was evaluated against five isolates of Chlamydia pneumonia and 21 isolates of Chlamydia trachomatis. MICs were determined using a tissue culture incorporation technique in McCoy cell monolayers treated with Grepafloxacin. After 48–72 h incubation, cover slips were fixed in methanol and stained with an immunofluorescent monoclonal antibody against the major outer membrane protein. Grepafloxacin MIC range was 0.06–0.12 mg/L.
Substance Class |
Chemical
Created
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admin
on
Edited
Fri Dec 15 17:23:34 GMT 2023
by
admin
on
Fri Dec 15 17:23:34 GMT 2023
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Record UNII |
L1M1U2HC31
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Record Status |
Validated (UNII)
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Record Version |
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C795
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admin on Fri Dec 15 17:23:34 GMT 2023 , Edited by admin on Fri Dec 15 17:23:34 GMT 2023
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WHO-VATC |
QJ01MA11
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admin on Fri Dec 15 17:23:34 GMT 2023 , Edited by admin on Fri Dec 15 17:23:34 GMT 2023
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WHO-ATC |
J01MA11
Created by
admin on Fri Dec 15 17:23:34 GMT 2023 , Edited by admin on Fri Dec 15 17:23:34 GMT 2023
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119914-60-2
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admin on Fri Dec 15 17:23:34 GMT 2023 , Edited by admin on Fri Dec 15 17:23:34 GMT 2023
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PRIMARY | |||
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1330
Created by
admin on Fri Dec 15 17:23:34 GMT 2023 , Edited by admin on Fri Dec 15 17:23:34 GMT 2023
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83719
Created by
admin on Fri Dec 15 17:23:34 GMT 2023 , Edited by admin on Fri Dec 15 17:23:34 GMT 2023
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PRIMARY | RxNorm | ||
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72474
Created by
admin on Fri Dec 15 17:23:34 GMT 2023 , Edited by admin on Fri Dec 15 17:23:34 GMT 2023
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100000084239
Created by
admin on Fri Dec 15 17:23:34 GMT 2023 , Edited by admin on Fri Dec 15 17:23:34 GMT 2023
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L1M1U2HC31
Created by
admin on Fri Dec 15 17:23:34 GMT 2023 , Edited by admin on Fri Dec 15 17:23:34 GMT 2023
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SUB07965MIG
Created by
admin on Fri Dec 15 17:23:34 GMT 2023 , Edited by admin on Fri Dec 15 17:23:34 GMT 2023
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CHEMBL583
Created by
admin on Fri Dec 15 17:23:34 GMT 2023 , Edited by admin on Fri Dec 15 17:23:34 GMT 2023
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DTXSID2048321
Created by
admin on Fri Dec 15 17:23:34 GMT 2023 , Edited by admin on Fri Dec 15 17:23:34 GMT 2023
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DB00365
Created by
admin on Fri Dec 15 17:23:34 GMT 2023 , Edited by admin on Fri Dec 15 17:23:34 GMT 2023
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GREPAFLOXACIN
Created by
admin on Fri Dec 15 17:23:34 GMT 2023 , Edited by admin on Fri Dec 15 17:23:34 GMT 2023
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C075375
Created by
admin on Fri Dec 15 17:23:34 GMT 2023 , Edited by admin on Fri Dec 15 17:23:34 GMT 2023
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m5850
Created by
admin on Fri Dec 15 17:23:34 GMT 2023 , Edited by admin on Fri Dec 15 17:23:34 GMT 2023
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PRIMARY | Merck Index | ||
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C65817
Created by
admin on Fri Dec 15 17:23:34 GMT 2023 , Edited by admin on Fri Dec 15 17:23:34 GMT 2023
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7024
Created by
admin on Fri Dec 15 17:23:34 GMT 2023 , Edited by admin on Fri Dec 15 17:23:34 GMT 2023
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PRIMARY |
Related Record | Type | Details | ||
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SOLVATE->ANHYDROUS | |||
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ENANTIOMER -> RACEMATE | |||
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SALT/SOLVATE -> PARENT | |||
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SALT/SOLVATE -> PARENT | |||
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TARGET ORGANISM->INHIBITOR |
18 STRAINS; SOME LESS THE 8 ng/mL for many strains; MIC range listed
MIC90
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TRANSPORTER -> INHIBITOR | |||
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BINDER->LIGAND |
BINDING
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ENANTIOMER -> RACEMATE | |||
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SALT/SOLVATE -> PARENT |
Related Record | Type | Details | ||
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Volume of Distribution | PHARMACOKINETIC |
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Biological Half-life | PHARMACOKINETIC |
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