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Details

Stereochemistry ABSOLUTE
Molecular Formula C21H19BrN4O2
Molecular Weight 439.3055
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of REMIMAZOLAM

SMILES

Cc1cnc2[C@]([H])(CCC(=O)OC)N=C(c3cc(ccc3-n12)Br)c4ccccn4

InChI

InChIKey=CYHWMBVXXDIZNZ-KRWDZBQOSA-N
InChI=1S/C21H19BrN4O2/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/h3-6,8,10-12,17H,7,9H2,1-2H3/t17-/m0/s1

HIDE SMILES / InChI

Molecular Formula C21H19BrN4O2
Molecular Weight 439.3055
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

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.

Approval Year

Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
1882 ng/mL
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
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
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
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
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
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
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
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
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:
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
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:
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:
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
Other AEs: Hypotension, Hypertension...
Other AEs:
Hypotension (39%)
Hypertension (20%)
Bradycardia (11%)
Diastolic hypertension (10%)
Tachycardia (8%)
Diastolic hypotension (8%)
Systolic hypertension (5%)
Sources:
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:
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
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:
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:
unhealthy, adults
n = 31
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 31
Sources:
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:
33.16 mg single, intravenous
Highest studied dose
Dose: 33.16 mg
Route: intravenous
Route: single
Dose: 33.16 mg
Sources:
unhealthy
n = 1
19.058 mg single, intravenous (mid range)
Studied dose
Dose: 19.058 mg
Route: intravenous
Route: single
Dose: 19.058 mg
Sources:
unhealthy
n = 165
Health Status: unhealthy
Population Size: 165
Sources:
Other AEs: Hypoxia, Bradycardia...
Other AEs:
Hypoxia (15.8%)
Bradycardia (9.7%)
Hypotension (53.9%)
Sources:
20 mg single, intravenous
Studied dose
Dose: 20 mg
Route: intravenous
Route: single
Dose: 20 mg
Sources:
unhealthy
Other AEs: QT interval prolonged...
28.43 mg single, intravenous (mid range)
Studied dose
Dose: 28.43 mg
Route: intravenous
Route: single
Dose: 28.43 mg
Sources:
unhealthy
n = 6
Other AEs: Hypoxia, Hypotension...
9.686 mg single, intravenous (mid range)
Studied dose
Dose: 9.686 mg
Route: intravenous
Route: single
Dose: 9.686 mg
Sources:
unhealthy
n = 459
Health Status: unhealthy
Population Size: 459
Sources:
Other AEs: Hypoxia, Bradycardia...
Other AEs:
Hypoxia (14.6%)
Bradycardia (7%)
Hypotension (40.3%)
Sources:
0.2 mg/kg single, intravenous
Studied dose
Dose: 0.2 mg/kg
Route: intravenous
Route: single
Dose: 0.2 mg/kg
Sources:
unhealthy
n = 25
Health Status: unhealthy
Condition: upper endoscopy
Population Size: 25
Sources:
Other AEs: Hypoxia...
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:
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
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:
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
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:
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
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:
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
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:
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
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:
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
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:
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
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:
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
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:
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
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:
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
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:
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
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:
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
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:
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
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:
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
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:
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
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:
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
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:
unhealthy, adults
n = 296
Health Status: unhealthy
Condition: colonoscopy
Age Group: adults
Sex: M+F
Population Size: 296
Sources:
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:
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
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:
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
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:
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
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:
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
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:
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
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:
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
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:
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
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:
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
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:
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
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:
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
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:
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
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:
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
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:
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
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:
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
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:
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
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:
unhealthy, adults
n = 303
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 303
Sources:
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:
unhealthy, adults
n = 31
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 31
Sources:
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:
unhealthy, adults
n = 31
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 31
Sources:
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:
unhealthy, adults
n = 31
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 31
Sources:
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:
unhealthy, adults
n = 31
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 31
Sources:
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:
unhealthy, adults
n = 31
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 31
Sources:
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:
unhealthy, adults
n = 31
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 31
Sources:
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:
unhealthy, adults
n = 31
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 31
Sources:
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:
unhealthy, adults
n = 31
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 31
Sources:
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:
unhealthy, adults
n = 31
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 31
Sources:
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:
unhealthy, adults
n = 31
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 31
Sources:
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:
unhealthy, adults
n = 31
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 31
Sources:
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:
unhealthy, adults
n = 31
Health Status: unhealthy
Condition: Bronchoscopy
Age Group: adults
Sex: M+F
Population Size: 31
Sources:
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:
unhealthy
n = 165
Health Status: unhealthy
Population Size: 165
Sources:
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:
unhealthy
n = 165
Health Status: unhealthy
Population Size: 165
Sources:
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:
unhealthy
n = 165
Health Status: unhealthy
Population Size: 165
Sources:
QT interval prolonged
20 mg single, intravenous
Studied dose
Dose: 20 mg
Route: intravenous
Route: single
Dose: 20 mg
Sources:
unhealthy
Hypoxia 33%
28.43 mg single, intravenous (mid range)
Studied dose
Dose: 28.43 mg
Route: intravenous
Route: single
Dose: 28.43 mg
Sources:
unhealthy
n = 6
Hypotension 50%
28.43 mg single, intravenous (mid range)
Studied dose
Dose: 28.43 mg
Route: intravenous
Route: single
Dose: 28.43 mg
Sources:
unhealthy
n = 6
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:
unhealthy
n = 459
Health Status: unhealthy
Population Size: 459
Sources:
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:
unhealthy
n = 459
Health Status: unhealthy
Population Size: 459
Sources:
Bradycardia 7%
9.686 mg single, intravenous (mid range)
Studied dose
Dose: 9.686 mg
Route: intravenous
Route: single
Dose: 9.686 mg
Sources:
unhealthy
n = 459
Health Status: unhealthy
Population Size: 459
Sources:
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:
unhealthy
n = 25
Health Status: unhealthy
Condition: upper endoscopy
Population Size: 25
Sources:
Overview

Overview

Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no [IC50 29.2 uM]
no [IC50 578 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >600 uM]
no [IC50 >600 uM]
no [IC50 >600 uM]
no [IC50 >600 uM]
no [IC50 >600 uM]
no [IC50 >600 uM]
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
weak [IC50 10 uM]
weak [IC50 100 uM]
weak [IC50 100 uM]
weak [IC50 >100 uM]
yes [IC50 500 uM]
yes [IC50 500 uM]
yes [IC50 >50 uM]
yes [Inhibition 100 uM]
yes [Inhibition 100 uM]
yes [Inhibition 100 uM]
Drug as victimTox targets
Substance Class Chemical
Created
by admin
on Sat Jun 26 14:36:26 UTC 2021
Edited
by admin
on Sat Jun 26 14:36:26 UTC 2021
Record UNII
7V4A8U16MB
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
REMIMAZOLAM
INN   WHO-DD  
USAN   INN  
Official Name English
METHYL 3-((4S)-8-BROMO-1-METHYL-6-(PYRIDIN-2-YL)-4H-IMIDAZO(1,2-A)(1,4)BENZODIAZEPIN-4-YL)PROPANOATE
Systematic Name English
REMIMAZOLAM [USAN]
Common Name English
4H-IMIDAZO(1,2-A)(1,4)BENZODIAZEPINE-4-PROPANOIC ACID, 8-BROMO-1-METHYL-6-(2-PYRIDINYL)-, METHYL ESTER, (4S)-
Systematic Name English
CNS-7056
Code English
4H-IMIDAZOL(1,2-A)(1,4)BENZODIAZEPINE-4-PROPIONIC ACID, (S)-
Common Name English
REMIMAZOLAM [INN]
Common Name English
ONO-2745
Code English
REMIMAZOLAM [WHO-DD]
Common Name English
Classification Tree Code System Code
DEA NO. 2846
Created by admin on Sat Jun 26 14:36:27 UTC 2021 , Edited by admin on Sat Jun 26 14:36:27 UTC 2021
NCI_THESAURUS C1012
Created by admin on Sat Jun 26 14:36:27 UTC 2021 , Edited by admin on Sat Jun 26 14:36:27 UTC 2021
Code System Code Type Description
INN
9232
Created by admin on Sat Jun 26 14:36:27 UTC 2021 , Edited by admin on Sat Jun 26 14:36:27 UTC 2021
PRIMARY
MESH
C522201
Created by admin on Sat Jun 26 14:36:27 UTC 2021 , Edited by admin on Sat Jun 26 14:36:27 UTC 2021
PRIMARY
NCI_THESAURUS
C152187
Created by admin on Sat Jun 26 14:36:27 UTC 2021 , Edited by admin on Sat Jun 26 14:36:27 UTC 2021
PRIMARY
WIKIPEDIA
REMIMAZOLAM
Created by admin on Sat Jun 26 14:36:27 UTC 2021 , Edited by admin on Sat Jun 26 14:36:27 UTC 2021
PRIMARY
RXCUI
2383941
Created by admin on Sat Jun 26 14:36:27 UTC 2021 , Edited by admin on Sat Jun 26 14:36:27 UTC 2021
PRIMARY
PUBCHEM
9867812
Created by admin on Sat Jun 26 14:36:27 UTC 2021 , Edited by admin on Sat Jun 26 14:36:27 UTC 2021
PRIMARY
DRUG BANK
DB12404
Created by admin on Sat Jun 26 14:36:27 UTC 2021 , Edited by admin on Sat Jun 26 14:36:27 UTC 2021
PRIMARY
EVMPD
SUB178714
Created by admin on Sat Jun 26 14:36:27 UTC 2021 , Edited by admin on Sat Jun 26 14:36:27 UTC 2021
PRIMARY
FDA UNII
7V4A8U16MB
Created by admin on Sat Jun 26 14:36:27 UTC 2021 , Edited by admin on Sat Jun 26 14:36:27 UTC 2021
PRIMARY
CAS
308242-62-8
Created by admin on Sat Jun 26 14:36:27 UTC 2021 , Edited by admin on Sat Jun 26 14:36:27 UTC 2021
PRIMARY
Related Record Type Details
SALT/SOLVATE -> PARENT
EXCRETED UNCHANGED
URINE
SALT/SOLVATE -> PARENT
BINDER->LIGAND
BINDING
Related Record Type Details
METABOLITE INACTIVE -> PARENT
PLASMA
METABOLITE -> PARENT
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ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC