U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C21H19BrN4O2.C7H8O3S
Molecular Weight 611.507
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of REMIMAZOLAM TOSYLATE

SMILES

CC1=CC=C(C=C1)S(O)(=O)=O.COC(=O)CC[C@@H]2N=C(C3=NC=CC=C3)C4=CC(Br)=CC=C4N5C(C)=CN=C25

InChI

InChIKey=UNLWPYSYFQLJSV-LMOVPXPDSA-N
InChI=1S/C21H19BrN4O2.C7H8O3S/c1-13-12-24-21-17(7-9-19(27)28-2)25-20(16-5-3-4-10-23-16)15-11-14(22)6-8-18(15)26(13)21;1-6-2-4-7(5-3-6)11(8,9)10/h3-6,8,10-12,17H,7,9H2,1-2H3;2-5H,1H3,(H,8,9,10)/t17-;/m0./s1

HIDE SMILES / InChI
Molecular Formula C7H8O3S
Molecular Weight 172.202
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE
Molecular Formula C21H19BrN4O2
Molecular Weight 439.305
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Description

Remimazolam is an intravenous benzodiazepine sedative-hypnotic with rapid onset and offset of action. This compound undergoes organ-independent metabolism to an inactive metabolite. Like other benzodiazepines, remimazolam can be reversed with flumazenil to rapidly terminate sedation and anesthesia. Phase I and II clinical trials have shown that remimazolam is safe and effective when used for procedural sedation. Phase III clinical trials have been completed investigating efficacy and safety in patients undergoing bronchoscopy and colonoscopy. The developer of this drug has suggested that intensive care unit sedation (beyond 24 hours) could be another possible indication for further development, since it is unlikely that prolonged infusions or higher doses of remimazolam would result in accumulation and extended effect.

CNS Activity

Originator

Approval Year

2020
742
Targets

Targets

Primary TargetPharmacologyConditionPotency
Agonist
2678
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
1882 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/22190555/
0.1 mg/kg single, intravenous
dose: 0.1 mg/kg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
REMIMAZOLAM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
6095 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/22190555/
0.3 mg/kg single, intravenous
dose: 0.3 mg/kg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
REMIMAZOLAM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
189.2 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/22190555/
0.01 mg/kg single, intravenous
dose: 0.01 mg/kg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
REMIMAZOLAM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
105.3 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/22190555/
0.1 mg/kg single, intravenous
dose: 0.1 mg/kg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
REMIMAZOLAM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
339.3 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/22190555/
0.3 mg/kg single, intravenous
dose: 0.3 mg/kg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
REMIMAZOLAM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
11.49 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/22190555/
0.01 mg/kg single, intravenous
dose: 0.01 mg/kg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
REMIMAZOLAM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
0.794 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/22190555/
0.1 mg/kg single, intravenous
dose: 0.1 mg/kg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
REMIMAZOLAM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
0.72 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/22190555/
0.3 mg/kg single, intravenous
dose: 0.3 mg/kg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
REMIMAZOLAM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
0.597 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/22190555/
0.01 mg/kg single, intravenous
dose: 0.01 mg/kg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
REMIMAZOLAM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
Doses

Doses

DosePopulationAdverse events​
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://pubmed.ncbi.nlm.nih.gov/29723512/
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
https://pubmed.ncbi.nlm.nih.gov/29723512/
Other AEs: Bradypnea, Hypoxia...
Other AEs:
Bradypnea (1.4%)
Hypoxia (1%)
Respiratory depression (0.3%)
Nausea (1.7%)
Vomiting (1%)
Headache (1.7%)
Dizziness (1%)
Presyncope (0.7%)
Hematocrit decreased (0.3%)
Infections and infestations (0.7%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/29723512/
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29723512/
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29723512/
Other AEs: Hypotension, Hypertension...
Other AEs:
Hypotension (39%)
Hypertension (20%)
Bradycardia (11%)
Diastolic hypertension (10%)
Tachycardia (8%)
Diastolic hypotension (8%)
Systolic hypertension (5%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29723512/
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
Disc. AE: Bradycardia, Hypertension...
Other AEs: Hypotension, Hypertension...
AEs leading to
discontinuation/dose reduction:
Bradycardia (0.33%)
Hypertension (0.33%)
Hypotension (0.33%)
Hypoxia (0.33%)
Respiratory rate increased (0.33%)
Other AEs:
Hypotension (grade 1, 33%)
Hypertension (grade 1, 28%)
Diastolic hypertension (grade 1, 25%)
Systolic hypertension (grade 1, 22%)
Hypoxia (grade 1, 22%)
Respiratory rate increased (grade 1, 14%)
Diastolic hypotension (grade 1, 14%)
Nausea (grade 1, 4%)
Bradycardia (grade 1, 4%)
Pyrexia (grade 1, 4%)
Headache (grade 1, 3%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
unhealthy, adults
n = 31
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 31
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
Other AEs: Hypotension, Hypertension...
Other AEs:
Hypotension (58%)
Hypertension (42%)
Respiratory acidosis (19%)
Diastolic hypertension (10%)
Systolic hypertension (6%)
Bradycardia (3%)
Respiratory rate decreased (3%)
Diastolic hypotension (3%)
Blood pressure diastolic increased (3%)
Blood pressure increased (3%)
Blood pressure systolic increased (3%)
Upper respiratory tract infection (3%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
33.16 mg single, intravenous
Highest studied dose
Dose: 33.16 mg
Route: intravenous
Route: single
Dose: 33.16 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
unhealthy
n = 1
Health Status: unhealthy
Population Size: 1
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
19.058 mg single, intravenous (mid range)
Studied dose
Dose: 19.058 mg
Route: intravenous
Route: single
Dose: 19.058 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
unhealthy
n = 165
Health Status: unhealthy
Population Size: 165
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
Other AEs: Hypoxia, Bradycardia...
Other AEs:
Hypoxia (15.8%)
Bradycardia (9.7%)
Hypotension (53.9%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
20 mg single, intravenous
Studied dose
Dose: 20 mg
Route: intravenous
Route: single
Dose: 20 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
Other AEs: QT interval prolonged...
Other AEs:
QT interval prolonged
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
28.43 mg single, intravenous (mid range)
Studied dose
Dose: 28.43 mg
Route: intravenous
Route: single
Dose: 28.43 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
unhealthy
n = 6
Health Status: unhealthy
Population Size: 6
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
Other AEs: Hypoxia, Hypotension...
Other AEs:
Hypoxia (33%)
Hypotension (50%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
9.686 mg single, intravenous (mid range)
Studied dose
Dose: 9.686 mg
Route: intravenous
Route: single
Dose: 9.686 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
unhealthy
n = 459
Health Status: unhealthy
Population Size: 459
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
Other AEs: Hypoxia, Bradycardia...
Other AEs:
Hypoxia (14.6%)
Bradycardia (7%)
Hypotension (40.3%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
0.2 mg/kg single, intravenous
Studied dose
Dose: 0.2 mg/kg
Route: intravenous
Route: single
Dose: 0.2 mg/kg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
unhealthy
n = 25
Health Status: unhealthy
Condition: upper endoscopy
Population Size: 25
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
Other AEs: Hypoxia...
Other AEs:
Hypoxia (24%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
AEs

AEs

AESignificanceDosePopulation
Hematocrit decreased 0.3%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://pubmed.ncbi.nlm.nih.gov/29723512/
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
https://pubmed.ncbi.nlm.nih.gov/29723512/
Respiratory depression 0.3%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://pubmed.ncbi.nlm.nih.gov/29723512/
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
https://pubmed.ncbi.nlm.nih.gov/29723512/
Infections and infestations 0.7%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://pubmed.ncbi.nlm.nih.gov/29723512/
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
https://pubmed.ncbi.nlm.nih.gov/29723512/
Presyncope 0.7%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://pubmed.ncbi.nlm.nih.gov/29723512/
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
https://pubmed.ncbi.nlm.nih.gov/29723512/
Dizziness 1%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://pubmed.ncbi.nlm.nih.gov/29723512/
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
https://pubmed.ncbi.nlm.nih.gov/29723512/
Hypoxia 1%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://pubmed.ncbi.nlm.nih.gov/29723512/
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
https://pubmed.ncbi.nlm.nih.gov/29723512/
Vomiting 1%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://pubmed.ncbi.nlm.nih.gov/29723512/
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
https://pubmed.ncbi.nlm.nih.gov/29723512/
Bradypnea 1.4%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://pubmed.ncbi.nlm.nih.gov/29723512/
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
https://pubmed.ncbi.nlm.nih.gov/29723512/
Headache 1.7%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://pubmed.ncbi.nlm.nih.gov/29723512/
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
https://pubmed.ncbi.nlm.nih.gov/29723512/
Nausea 1.7%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://pubmed.ncbi.nlm.nih.gov/29723512/
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
https://pubmed.ncbi.nlm.nih.gov/29723512/
Diastolic hypertension 10%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29723512/
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29723512/
Bradycardia 11%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29723512/
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29723512/
Hypertension 20%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29723512/
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29723512/
Hypotension 39%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29723512/
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29723512/
Systolic hypertension 5%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29723512/
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29723512/
Diastolic hypotension 8%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29723512/
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29723512/
Tachycardia 8%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29723512/
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29723512/
Bradycardia 0.33%
Disc. AE
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
Hypertension 0.33%
Disc. AE
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
Hypotension 0.33%
Disc. AE
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
Hypoxia 0.33%
Disc. AE
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
Respiratory rate increased 0.33%
Disc. AE
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
Diastolic hypotension grade 1, 14%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
Respiratory rate increased grade 1, 14%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
Hypoxia grade 1, 22%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
Systolic hypertension grade 1, 22%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
Diastolic hypertension grade 1, 25%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
Hypertension grade 1, 28%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
Headache grade 1, 3%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
Hypotension grade 1, 33%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
Bradycardia grade 1, 4%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
Nausea grade 1, 4%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
Pyrexia grade 1, 4%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 to 75 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30292760/
Diastolic hypertension 10%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
unhealthy, adults
n = 31
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 31
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
Respiratory acidosis 19%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
unhealthy, adults
n = 31
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 31
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
Blood pressure diastolic increased 3%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
unhealthy, adults
n = 31
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 31
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
Blood pressure increased 3%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
unhealthy, adults
n = 31
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 31
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
Blood pressure systolic increased 3%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
unhealthy, adults
n = 31
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 31
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
Bradycardia 3%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
unhealthy, adults
n = 31
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 31
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
Diastolic hypotension 3%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
unhealthy, adults
n = 31
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 31
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
Respiratory rate decreased 3%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
unhealthy, adults
n = 31
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 31
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
Upper respiratory tract infection 3%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
unhealthy, adults
n = 31
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 31
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
Hypertension 42%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
unhealthy, adults
n = 31
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 31
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
Hypotension 58%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
unhealthy, adults
n = 31
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 31
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
Systolic hypertension 6%
10 mg 1 times / day multiple, intravenous (median)
Recommended
Dose: 10 mg, 1 times / day
Route: intravenous
Route: multiple
Dose: 10 mg, 1 times / day
Co-administed with::
fentanyl(50 ug intravenous; 25 ug every 5 to 10 minutes were allowed until analgesia was adequate)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
unhealthy, adults
n = 31
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 31
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212295s000lbl.pdf
Hypoxia 15.8%
19.058 mg single, intravenous (mid range)
Studied dose
Dose: 19.058 mg
Route: intravenous
Route: single
Dose: 19.058 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
unhealthy
n = 165
Health Status: unhealthy
Population Size: 165
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
Hypotension 53.9%
19.058 mg single, intravenous (mid range)
Studied dose
Dose: 19.058 mg
Route: intravenous
Route: single
Dose: 19.058 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
unhealthy
n = 165
Health Status: unhealthy
Population Size: 165
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
Bradycardia 9.7%
19.058 mg single, intravenous (mid range)
Studied dose
Dose: 19.058 mg
Route: intravenous
Route: single
Dose: 19.058 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
unhealthy
n = 165
Health Status: unhealthy
Population Size: 165
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
QT interval prolonged
20 mg single, intravenous
Studied dose
Dose: 20 mg
Route: intravenous
Route: single
Dose: 20 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
Hypoxia 33%
28.43 mg single, intravenous (mid range)
Studied dose
Dose: 28.43 mg
Route: intravenous
Route: single
Dose: 28.43 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
unhealthy
n = 6
Health Status: unhealthy
Population Size: 6
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
Hypotension 50%
28.43 mg single, intravenous (mid range)
Studied dose
Dose: 28.43 mg
Route: intravenous
Route: single
Dose: 28.43 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
unhealthy
n = 6
Health Status: unhealthy
Population Size: 6
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
Hypoxia 14.6%
9.686 mg single, intravenous (mid range)
Studied dose
Dose: 9.686 mg
Route: intravenous
Route: single
Dose: 9.686 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
unhealthy
n = 459
Health Status: unhealthy
Population Size: 459
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
Hypotension 40.3%
9.686 mg single, intravenous (mid range)
Studied dose
Dose: 9.686 mg
Route: intravenous
Route: single
Dose: 9.686 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
unhealthy
n = 459
Health Status: unhealthy
Population Size: 459
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
Bradycardia 7%
9.686 mg single, intravenous (mid range)
Studied dose
Dose: 9.686 mg
Route: intravenous
Route: single
Dose: 9.686 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
unhealthy
n = 459
Health Status: unhealthy
Population Size: 459
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
Hypoxia 24%
0.2 mg/kg single, intravenous
Studied dose
Dose: 0.2 mg/kg
Route: intravenous
Route: single
Dose: 0.2 mg/kg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
unhealthy
n = 25
Health Status: unhealthy
Condition: upper endoscopy
Population Size: 25
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212295Orig1s000MedR.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inhibitor
1587
inhibitor
1767
inhibitor
1852
inhibitor
1612

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP2B6
810

CYP2C8
911

CYP2C19
1478

CYP1A2
1524

OAT3
642

OCT2
647

OATP1B1
788

OATP1B3
706

OAT1
599

BCRP
699

P-gp
1461

BSEP
402

MATE1
306

MATE2
263

MRP2
383

MRP3
157

MRP4
204
CYP1A2
1054

OATP1B1
406

OATP1B3
350

BCRP
561

P-gp
1537

UGT
192
CYP1A2
701
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP2C8
965
 no [IC50 29.2 uM]
CYP2C8
965
 no [IC50 578 uM]
CNS7054
3
CYP2B6
1001
 no [IC50 >100 uM]
CYP2C19
1553
 no [IC50 >100 uM]
CYP2C9
1819
 no [IC50 >100 uM]
CYP2D6
1891
 no [IC50 >100 uM]
CYP3A4
1925
 no [IC50 >100 uM]
CYP1A2
1692
 no [IC50 >600 uM]
CNS7054
3
CYP2B6
1001
 no [IC50 >600 uM]
CNS7054
3
CYP2C19
1553
 no [IC50 >600 uM]
CNS7054
3
CYP2C9
1819
 no [IC50 >600 uM]
CNS7054
3
CYP2D6
1891
 no [IC50 >600 uM]
CNS7054
3
CYP3A4
1925
 no [IC50 >600 uM]
CNS7054
3
BCRP
773
 no
BCRP
773
 no
CNS7054
3
BSEP
403
 no
CNS7054
3
CYP1A2
1692
 no
CYP1A2
1692
 no
CNS7054
3
MATE1
308
 no
CNS7054
3
MATE2
263
 no
CNS7054
3
MRP2
475
 no
MRP2
475
 no
CNS7054
3
MRP3
207
 no
MRP3
207
 no
CNS7054
3
MRP4
238
 no
MRP4
238
 no
CNS7054
3
OAT1
603
 no
OAT1
603
 no
CNS7054
3
OCT2
648
 no
CNS7054
3
P-gp
1650
 no
P-gp
1650
 no
CNS7054
3
OATP1B1
803
 weak [IC50 10 uM]
OATP1B3
715
 weak [IC50 100 uM]
OCT2
648
 weak [IC50 100 uM]
OAT3
644
 weak [IC50 >100 uM]
OATP1B1
803
 yes [IC50 500 uM]
CNS7054
3
OATP1B3
715
 yes [IC50 500 uM]
CNS7054
3
OAT3
644
 yes [IC50 >50 uM]
CNS7054
3
BSEP
403
 yes [Inhibition 100 uM]
MATE1
308
 yes [Inhibition 100 uM]
MATE2
263
 yes [Inhibition 100 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
BCRP
561
 likely
CNS7054
3
P-gp
1537
 likely
CNS7054
3
CYP1A2
1054
 no [IC50 63.3 uM]
BCRP
561
 no
OATP1B1
406
 no
OATP1B1
406
 no
CNS7054
3
OATP1B3
350
 no
OATP1B3
350
 no
CNS7054
3
UGT
192
 yes
CNS7054
3
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1647
hERG
1647
CNS7054
3
Sourcing

Sourcing

Vendor/AggregatorIDURL
Achemtek
0102-013440
http://www.achemtek.com/308242-62-8
Acorn PharmaTech
ACN-029380
http://www.acornpharmatech.com/
Ambinter
Amb24053933
http://www.ambinter.com/reference/24053933
Aurora Fine Chemicals LLC
A24.140.976
http://online.aurorafinechemicals.com/info?ID=A24.140.976
AvaChem Scientific
4523B
http://www.avachem.com/productSearch.asp?4523B
Boerchem
BC600571
http://www.boerchem.com/?product_43406.html
Chem Scene
CS-0003605
http://www.chemscene.com/308242-62-8.html
ChemFish Tokyo co.,ltd
9867812
http://www.chemfish.co.jp/index.php?id=3934&project=product
Chemspace
CSSB00032005504
https://chem-space.com/CSSB00032005504
DC Chemicals
DC7009
http://www.dcchemicals.com/product_show-CNS_7056.html
Hairui
RESA034
http://www.hairuichem.com/en/product/308242-62-8.html
Lab Network
LN01310290
https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01310290
MedChem Express
HY-14867
https://www.medchemexpress.com/remimazolam.html
MuseChem
I009004
https://www.musechem.com/product/I009004.html
Smolecule
S541196
http://www.smolecule.com/products/s541196
Synblock Inc
SB17134
http://www.synblock.com/product/308242-62-8.html
THE BioTek
bt-280042
https://www.thebiotek.com/product/inhibitors/bt-280042
THE BioTek
bt-340262
https://www.thebiotek.com/product/others/bt-340262
Substance Class Chemical
Created
by admin
on Sat Dec 16 10:18:23 GMT 2023
Edited
by admin
on Sat Dec 16 10:18:23 GMT 2023
Record UNII
9J7J08A8LT
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
REMIMAZOLAM TOSYLATE
Common Name English
4H-IMIDAZO(1,2-A)(1,4)BENZODIAZEPINE-4-PROPANOIC ACID, 8-BROMO-1-METHYL-6-(2-PYRIDINYL)-, METHYL ESTER, (4S)-, 4-METHYLBENZENESULFONATE (1:1)
Systematic Name English
Remimazolam tosilate [WHO-DD]
Common Name English
REMIMAZOLAM TOSILATE
Common Name English
METHYL (4S)-8-BROMO-1-METHYL-6-(2-PYRIDINYL)-4H-IMIDAZO(1,2-A)(1,4)BENZODIAZEPINE-4-PROPANOATE 4-METHYLBENZENESULFONATE (1:1)
Systematic Name English
Code System Code Type Description
NCI_THESAURUS
C179563
Created by admin on Sat Dec 16 10:18:23 GMT 2023 , Edited by admin on Sat Dec 16 10:18:23 GMT 2023
PRIMARY
CAS
1425904-79-5
Created by admin on Sat Dec 16 10:18:23 GMT 2023 , Edited by admin on Sat Dec 16 10:18:23 GMT 2023
PRIMARY
PUBCHEM
71608022
Created by admin on Sat Dec 16 10:18:23 GMT 2023 , Edited by admin on Sat Dec 16 10:18:23 GMT 2023
PRIMARY
FDA UNII
9J7J08A8LT
Created by admin on Sat Dec 16 10:18:23 GMT 2023 , Edited by admin on Sat Dec 16 10:18:23 GMT 2023
PRIMARY
Related Record Type Details
Structure of REMIMAZOLAM
PARENT -> SALT/SOLVATE
Related Record Type Details
Structure of REMIMAZOLAM
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