Details
Stereochemistry | RACEMIC |
Molecular Formula | C13H16ClNO.ClH |
Molecular Weight | 274.186 |
Optical Activity | ( + / - ) |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CNC1(CCCCC1=O)C2=C(Cl)C=CC=C2
InChI
InChIKey=VCMGMSHEPQENPE-UHFFFAOYSA-N
InChI=1S/C13H16ClNO.ClH/c1-15-13(9-5-4-8-12(13)16)10-6-2-3-7-11(10)14;/h2-3,6-7,15H,4-5,8-9H2,1H3;1H
Molecular Formula | ClH |
Molecular Weight | 36.461 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | C13H16ClNO |
Molecular Weight | 237.725 |
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
https://www.ncbi.nlm.nih.gov/pubmed/23432384
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/23432384
Ketamine (brand name Ketalar) is a cyclohexanone derivative used for induction of anesthesia. Ketalar is indicated as the sole anesthetic agent for diagnostic and surgical procedures that do not require skeletal muscle relaxation; also, it is indicated for the induction of anesthesia prior to the administration of other general anesthetic agents. Ketamine blocks NMDA receptors through an interaction with sites thought to be located within the ion channel pore region. However, the complete pharmacology of ketamine is more complex, and it is known to directly interact with a variety of other sites to varying degrees. Recently, it was shown that inclusion of the NR3B subunit does not alter the ketamine sensitivity of recombinant NR1/NR2 receptors expressed in oocytes. Likewise, 100 μM ketamine produced only weak inhibition of the glycine-induced current of NR1/NR3A/NR3B receptors. The side effects of ketamine noted in clinical studies include psychedelic symptoms (hallucinations, memory defects, panic attacks), nausea/vomiting, somnolence, cardiovascular stimulation and, in a minority of patients, hepatoxicity. The recreational use of ketamine is increasing and comes with a variety of additional risks ranging from bladder and renal complications to persistent psychotypical behaviour and memory defects. Ketamine was first synthesized in 1962 by Calvin Stevens at Parke-Davis Co (now Pfizer) as an alternative anesthetic to phencyclidine. It was first used in humans in 1965 by Corssen and Domino and was introduced into clinical practice by 1970.
Originator
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27018176
Curator's Comment: Ketamine was first synthesized in 1962 by Calvin Stevens at Parke-Davis Co (now Pfizer) as an alternative anesthetic to phencyclidine. It was first used in humans in 1965 by Corssen and Domino and was introduced into clinical practice by 1970. # in 1962 Calvin Stevens at Parke-Davis Co (now Pfizer)
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2094124 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2858237 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | KETALAR Approved UseKetamine hydrochloride injection is indicated as the sole anesthetic agent for diagnostic and surgical procedures that do not require skeletal muscle relaxation. Ketamine hydrochloride is best suited for short procedures but it can be used, with additional doses, for longer procedures. Ketamine hydrochloride injection is indicated for the induction of anesthesia prior to the administration of other general anesthetic agents. Ketamine hydrochloride injection is indicated to supplement low-potency agents, such as nitrous oxide. Specific areas of application are described in the CLINICAL PHARMACOLOGY Section. Launch Date1970 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
2104 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8881626/ |
9 mg/kg single, nasal dose: 9 mg/kg route of administration: Nasal experiment type: SINGLE co-administered: |
KETAMINE plasma | Homo sapiens population: HEALTHY age: CHILD sex: UNKNOWN food status: UNKNOWN |
|
496 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8881626/ |
3 mg/kg single, nasal dose: 3 mg/kg route of administration: Nasal experiment type: SINGLE co-administered: |
KETAMINE plasma | Homo sapiens population: HEALTHY age: CHILD sex: UNKNOWN food status: UNKNOWN |
|
632 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8881626/ |
9 mg single, rectal dose: 9 mg route of administration: Rectal experiment type: SINGLE co-administered: |
KETAMINE plasma | Homo sapiens population: HEALTHY age: CHILD sex: UNKNOWN food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
148.3 mg × min/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8881626/ |
3 mg/kg single, intravenous dose: 3 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
KETAMINE plasma | Homo sapiens population: HEALTHY age: CHILD sex: UNKNOWN food status: UNKNOWN |
|
163.6 mg × min/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8881626/ |
9 mg/kg single, nasal dose: 9 mg/kg route of administration: Nasal experiment type: SINGLE co-administered: |
KETAMINE plasma | Homo sapiens population: HEALTHY age: CHILD sex: UNKNOWN food status: UNKNOWN |
|
76.4 mg × min/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8881626/ |
3 mg/kg single, nasal dose: 3 mg/kg route of administration: Nasal experiment type: SINGLE co-administered: |
KETAMINE plasma | Homo sapiens population: HEALTHY age: CHILD sex: UNKNOWN food status: UNKNOWN |
|
111.2 ng × min/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8881626/ |
9 mg single, rectal dose: 9 mg route of administration: Rectal experiment type: SINGLE co-administered: |
KETAMINE plasma | Homo sapiens population: HEALTHY age: CHILD sex: UNKNOWN food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
125 min EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8881626/ |
3 mg/kg single, intravenous dose: 3 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
KETAMINE plasma | Homo sapiens population: HEALTHY age: CHILD sex: UNKNOWN food status: UNKNOWN |
|
120 min EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8881626/ |
9 mg/kg single, nasal dose: 9 mg/kg route of administration: Nasal experiment type: SINGLE co-administered: |
KETAMINE plasma | Homo sapiens population: HEALTHY age: CHILD sex: UNKNOWN food status: UNKNOWN |
|
123 min EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8881626/ |
3 mg/kg single, nasal dose: 3 mg/kg route of administration: Nasal experiment type: SINGLE co-administered: |
KETAMINE plasma | Homo sapiens population: HEALTHY age: CHILD sex: UNKNOWN food status: UNKNOWN |
|
100 min EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8881626/ |
9 mg single, rectal dose: 9 mg route of administration: Rectal experiment type: SINGLE co-administered: |
KETAMINE plasma | Homo sapiens population: HEALTHY age: CHILD sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
0.5 mg/kg 1 times / day single, intravenous Studied dose Dose: 0.5 mg/kg, 1 times / day Route: intravenous Route: single Dose: 0.5 mg/kg, 1 times / day Sources: |
unhealthy, 18-65 years n = 126 Health Status: unhealthy Condition: major depressive disorder | bipolar disorder Age Group: 18-65 years Sex: M+F Population Size: 126 Sources: |
Other AEs: Dissociation... |
14 mg 8 times / day single, intranasal Highest studied dose Dose: 14 mg, 8 times / day Route: intranasal Route: single Dose: 14 mg, 8 times / day Sources: |
healthy, adult n = 34 Health Status: healthy Age Group: adult Sex: M Population Size: 34 Sources: |
Other AEs: Dizziness, Hyperhidrosis... Other AEs: Dizziness Sources: Hyperhidrosis Somnolence Hypoaesthesia Feeling abnormal Nausea Vomiting |
50 mg single, intranasal Dose: 50 mg Route: intranasal Route: single Dose: 50 mg Sources: |
unhealthy n = 19 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 19 Sources: |
Other AEs: Numbness, Blurred vision... Other AEs: Numbness (below serious, 2 patients) Sources: Blurred vision (below serious, 1 patient) Decreased appetite (below serious, 1 patient) Irritable (below serious, 1 patient) |
0.1 mg/kg single, intravenous Dose: 0.1 mg/kg Route: intravenous Route: single Dose: 0.1 mg/kg Sources: |
unhealthy n = 18 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 18 Sources: |
Other AEs: Headache, Nausea... Other AEs: Headache (below serious, 3 patients) Sources: Nausea (below serious, 2 patients) Vomiting (below serious, 1 patient) Depression (below serious, 1 patient) Diarrhea (below serious, 1 patient) Insomnia (below serious, 1 patient) Pain in extremity (below serious, 1 patient) Poor quality sleep (below serious, 1 patient) Suicidal ideation (below serious, 1 patient) Flushing (below serious, 1 patient) Hot flush (below serious, 1 patient) Increased appetite (below serious, 1 patient) White blood cell count decreased (below serious, 1 patient) |
0.2 mg/kg single, intravenous Dose: 0.2 mg/kg Route: intravenous Route: single Dose: 0.2 mg/kg Sources: |
unhealthy n = 20 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 20 Sources: |
Other AEs: Suicide attempt, Headache... Other AEs: Suicide attempt (serious, 1 patient) Sources: Headache (below serious, 2 patients) Vomiting (below serious, 1 patient) Depression (below serious, 1 patient) Dyspepsia (below serious, 2 patients) Tachycardia (below serious, 1 patient) Asthenia (below serious, 1 patient) Dermatitis contact (below serious, 1 patient) Fall (below serious, 1 patient) Hepatic enzyme increased (below serious, 1 patient) Loss of consciousness (below serious, 1 patient) Malaise (below serious, 1 patient) Overdose (below serious, 1 patient) Presyncope (below serious, 1 patient) Viral upper respiratory tract infection (below serious, 1 patient) |
0.5 mg/kg single, intravenous Dose: 0.5 mg/kg Route: intravenous Route: single Dose: 0.5 mg/kg Sources: |
unhealthy n = 22 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 22 Sources: |
Other AEs: Headache, Nausea... Other AEs: Headache (below serious, 1 patient) Sources: Nausea (below serious, 3 patients) Vomiting (below serious, 1 patient) Depression (below serious, 1 patient) Diarrhea (below serious, 1 patient) Pain in extremity (below serious, 1 patient) Suicidal ideation (below serious, 1 patient) Tooth abscess (below serious, 1 patient) Cough (below serious, 1 patient) Respiratory tract infection (below serious, 1 patient) Vertigo (below serious, 1 patient) |
0.5 mg/kg single, oral Dose: 0.5 mg/kg Route: oral Route: single Dose: 0.5 mg/kg Sources: |
unhealthy n = 3 Health Status: unhealthy Condition: Depression and Anxiety|Cancer Population Size: 3 Sources: |
Other AEs: Headache, Chest pain... Other AEs: Headache (below serious, 2 patients) Sources: Chest pain (below serious, 1 patient) |
1 mg/kg single, intravenous Dose: 1 mg/kg Route: intravenous Route: single Dose: 1 mg/kg Sources: |
unhealthy n = 20 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 20 Sources: |
Other AEs: Headache, Nausea... Other AEs: Headache (below serious, 3 patients) Sources: Nausea (below serious, 3 patients) Vomiting (below serious, 1 patient) Blood pressure increased (below serious, 2 patients) Insomnia (below serious, 1 patient) Poor quality sleep (below serious, 1 patient) Tachycardia (below serious, 1 patient) Dissociation (below serious, 1 patient) Dizziness (below serious, 1 patient) Hypertension (below serious, 1 patient) Upper respiratory tract infection (below serious, 1 patient) |
2.55 mg/kg single, intravenous (total daily dose) Dose: 2.55 mg/kg Route: intravenous Route: single Dose: 2.55 mg/kg Sources: |
unhealthy n = 10 Health Status: unhealthy Condition: Sepsis Population Size: 10 Sources: |
Other AEs: Pericardial effusion, Ventricular tachycardia... Other AEs: Pericardial effusion (serious, 1 patient) Sources: Ventricular tachycardia (serious, 1 patient) Delirium (below serious, 1 patient) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Dissociation | 0.5 mg/kg 1 times / day single, intravenous Studied dose Dose: 0.5 mg/kg, 1 times / day Route: intravenous Route: single Dose: 0.5 mg/kg, 1 times / day Sources: |
unhealthy, 18-65 years n = 126 Health Status: unhealthy Condition: major depressive disorder | bipolar disorder Age Group: 18-65 years Sex: M+F Population Size: 126 Sources: |
|
Dizziness | 14 mg 8 times / day single, intranasal Highest studied dose Dose: 14 mg, 8 times / day Route: intranasal Route: single Dose: 14 mg, 8 times / day Sources: |
healthy, adult n = 34 Health Status: healthy Age Group: adult Sex: M Population Size: 34 Sources: |
|
Feeling abnormal | 14 mg 8 times / day single, intranasal Highest studied dose Dose: 14 mg, 8 times / day Route: intranasal Route: single Dose: 14 mg, 8 times / day Sources: |
healthy, adult n = 34 Health Status: healthy Age Group: adult Sex: M Population Size: 34 Sources: |
|
Hyperhidrosis | 14 mg 8 times / day single, intranasal Highest studied dose Dose: 14 mg, 8 times / day Route: intranasal Route: single Dose: 14 mg, 8 times / day Sources: |
healthy, adult n = 34 Health Status: healthy Age Group: adult Sex: M Population Size: 34 Sources: |
|
Hypoaesthesia | 14 mg 8 times / day single, intranasal Highest studied dose Dose: 14 mg, 8 times / day Route: intranasal Route: single Dose: 14 mg, 8 times / day Sources: |
healthy, adult n = 34 Health Status: healthy Age Group: adult Sex: M Population Size: 34 Sources: |
|
Nausea | 14 mg 8 times / day single, intranasal Highest studied dose Dose: 14 mg, 8 times / day Route: intranasal Route: single Dose: 14 mg, 8 times / day Sources: |
healthy, adult n = 34 Health Status: healthy Age Group: adult Sex: M Population Size: 34 Sources: |
|
Somnolence | 14 mg 8 times / day single, intranasal Highest studied dose Dose: 14 mg, 8 times / day Route: intranasal Route: single Dose: 14 mg, 8 times / day Sources: |
healthy, adult n = 34 Health Status: healthy Age Group: adult Sex: M Population Size: 34 Sources: |
|
Vomiting | 14 mg 8 times / day single, intranasal Highest studied dose Dose: 14 mg, 8 times / day Route: intranasal Route: single Dose: 14 mg, 8 times / day Sources: |
healthy, adult n = 34 Health Status: healthy Age Group: adult Sex: M Population Size: 34 Sources: |
|
Blurred vision | below serious, 1 patient | 50 mg single, intranasal Dose: 50 mg Route: intranasal Route: single Dose: 50 mg Sources: |
unhealthy n = 19 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 19 Sources: |
Decreased appetite | below serious, 1 patient | 50 mg single, intranasal Dose: 50 mg Route: intranasal Route: single Dose: 50 mg Sources: |
unhealthy n = 19 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 19 Sources: |
Irritable | below serious, 1 patient | 50 mg single, intranasal Dose: 50 mg Route: intranasal Route: single Dose: 50 mg Sources: |
unhealthy n = 19 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 19 Sources: |
Numbness | below serious, 2 patients | 50 mg single, intranasal Dose: 50 mg Route: intranasal Route: single Dose: 50 mg Sources: |
unhealthy n = 19 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 19 Sources: |
Depression | below serious, 1 patient | 0.1 mg/kg single, intravenous Dose: 0.1 mg/kg Route: intravenous Route: single Dose: 0.1 mg/kg Sources: |
unhealthy n = 18 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 18 Sources: |
Diarrhea | below serious, 1 patient | 0.1 mg/kg single, intravenous Dose: 0.1 mg/kg Route: intravenous Route: single Dose: 0.1 mg/kg Sources: |
unhealthy n = 18 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 18 Sources: |
Flushing | below serious, 1 patient | 0.1 mg/kg single, intravenous Dose: 0.1 mg/kg Route: intravenous Route: single Dose: 0.1 mg/kg Sources: |
unhealthy n = 18 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 18 Sources: |
Hot flush | below serious, 1 patient | 0.1 mg/kg single, intravenous Dose: 0.1 mg/kg Route: intravenous Route: single Dose: 0.1 mg/kg Sources: |
unhealthy n = 18 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 18 Sources: |
Increased appetite | below serious, 1 patient | 0.1 mg/kg single, intravenous Dose: 0.1 mg/kg Route: intravenous Route: single Dose: 0.1 mg/kg Sources: |
unhealthy n = 18 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 18 Sources: |
Insomnia | below serious, 1 patient | 0.1 mg/kg single, intravenous Dose: 0.1 mg/kg Route: intravenous Route: single Dose: 0.1 mg/kg Sources: |
unhealthy n = 18 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 18 Sources: |
Pain in extremity | below serious, 1 patient | 0.1 mg/kg single, intravenous Dose: 0.1 mg/kg Route: intravenous Route: single Dose: 0.1 mg/kg Sources: |
unhealthy n = 18 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 18 Sources: |
Poor quality sleep | below serious, 1 patient | 0.1 mg/kg single, intravenous Dose: 0.1 mg/kg Route: intravenous Route: single Dose: 0.1 mg/kg Sources: |
unhealthy n = 18 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 18 Sources: |
Suicidal ideation | below serious, 1 patient | 0.1 mg/kg single, intravenous Dose: 0.1 mg/kg Route: intravenous Route: single Dose: 0.1 mg/kg Sources: |
unhealthy n = 18 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 18 Sources: |
Vomiting | below serious, 1 patient | 0.1 mg/kg single, intravenous Dose: 0.1 mg/kg Route: intravenous Route: single Dose: 0.1 mg/kg Sources: |
unhealthy n = 18 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 18 Sources: |
White blood cell count decreased | below serious, 1 patient | 0.1 mg/kg single, intravenous Dose: 0.1 mg/kg Route: intravenous Route: single Dose: 0.1 mg/kg Sources: |
unhealthy n = 18 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 18 Sources: |
Nausea | below serious, 2 patients | 0.1 mg/kg single, intravenous Dose: 0.1 mg/kg Route: intravenous Route: single Dose: 0.1 mg/kg Sources: |
unhealthy n = 18 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 18 Sources: |
Headache | below serious, 3 patients | 0.1 mg/kg single, intravenous Dose: 0.1 mg/kg Route: intravenous Route: single Dose: 0.1 mg/kg Sources: |
unhealthy n = 18 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 18 Sources: |
Asthenia | below serious, 1 patient | 0.2 mg/kg single, intravenous Dose: 0.2 mg/kg Route: intravenous Route: single Dose: 0.2 mg/kg Sources: |
unhealthy n = 20 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 20 Sources: |
Depression | below serious, 1 patient | 0.2 mg/kg single, intravenous Dose: 0.2 mg/kg Route: intravenous Route: single Dose: 0.2 mg/kg Sources: |
unhealthy n = 20 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 20 Sources: |
Dermatitis contact | below serious, 1 patient | 0.2 mg/kg single, intravenous Dose: 0.2 mg/kg Route: intravenous Route: single Dose: 0.2 mg/kg Sources: |
unhealthy n = 20 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 20 Sources: |
Fall | below serious, 1 patient | 0.2 mg/kg single, intravenous Dose: 0.2 mg/kg Route: intravenous Route: single Dose: 0.2 mg/kg Sources: |
unhealthy n = 20 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 20 Sources: |
Hepatic enzyme increased | below serious, 1 patient | 0.2 mg/kg single, intravenous Dose: 0.2 mg/kg Route: intravenous Route: single Dose: 0.2 mg/kg Sources: |
unhealthy n = 20 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 20 Sources: |
Loss of consciousness | below serious, 1 patient | 0.2 mg/kg single, intravenous Dose: 0.2 mg/kg Route: intravenous Route: single Dose: 0.2 mg/kg Sources: |
unhealthy n = 20 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 20 Sources: |
Malaise | below serious, 1 patient | 0.2 mg/kg single, intravenous Dose: 0.2 mg/kg Route: intravenous Route: single Dose: 0.2 mg/kg Sources: |
unhealthy n = 20 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 20 Sources: |
Overdose | below serious, 1 patient | 0.2 mg/kg single, intravenous Dose: 0.2 mg/kg Route: intravenous Route: single Dose: 0.2 mg/kg Sources: |
unhealthy n = 20 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 20 Sources: |
Presyncope | below serious, 1 patient | 0.2 mg/kg single, intravenous Dose: 0.2 mg/kg Route: intravenous Route: single Dose: 0.2 mg/kg Sources: |
unhealthy n = 20 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 20 Sources: |
Tachycardia | below serious, 1 patient | 0.2 mg/kg single, intravenous Dose: 0.2 mg/kg Route: intravenous Route: single Dose: 0.2 mg/kg Sources: |
unhealthy n = 20 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 20 Sources: |
Viral upper respiratory tract infection | below serious, 1 patient | 0.2 mg/kg single, intravenous Dose: 0.2 mg/kg Route: intravenous Route: single Dose: 0.2 mg/kg Sources: |
unhealthy n = 20 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 20 Sources: |
Vomiting | below serious, 1 patient | 0.2 mg/kg single, intravenous Dose: 0.2 mg/kg Route: intravenous Route: single Dose: 0.2 mg/kg Sources: |
unhealthy n = 20 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 20 Sources: |
Dyspepsia | below serious, 2 patients | 0.2 mg/kg single, intravenous Dose: 0.2 mg/kg Route: intravenous Route: single Dose: 0.2 mg/kg Sources: |
unhealthy n = 20 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 20 Sources: |
Headache | below serious, 2 patients | 0.2 mg/kg single, intravenous Dose: 0.2 mg/kg Route: intravenous Route: single Dose: 0.2 mg/kg Sources: |
unhealthy n = 20 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 20 Sources: |
Suicide attempt | serious, 1 patient | 0.2 mg/kg single, intravenous Dose: 0.2 mg/kg Route: intravenous Route: single Dose: 0.2 mg/kg Sources: |
unhealthy n = 20 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 20 Sources: |
Cough | below serious, 1 patient | 0.5 mg/kg single, intravenous Dose: 0.5 mg/kg Route: intravenous Route: single Dose: 0.5 mg/kg Sources: |
unhealthy n = 22 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 22 Sources: |
Depression | below serious, 1 patient | 0.5 mg/kg single, intravenous Dose: 0.5 mg/kg Route: intravenous Route: single Dose: 0.5 mg/kg Sources: |
unhealthy n = 22 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 22 Sources: |
Diarrhea | below serious, 1 patient | 0.5 mg/kg single, intravenous Dose: 0.5 mg/kg Route: intravenous Route: single Dose: 0.5 mg/kg Sources: |
unhealthy n = 22 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 22 Sources: |
Headache | below serious, 1 patient | 0.5 mg/kg single, intravenous Dose: 0.5 mg/kg Route: intravenous Route: single Dose: 0.5 mg/kg Sources: |
unhealthy n = 22 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 22 Sources: |
Pain in extremity | below serious, 1 patient | 0.5 mg/kg single, intravenous Dose: 0.5 mg/kg Route: intravenous Route: single Dose: 0.5 mg/kg Sources: |
unhealthy n = 22 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 22 Sources: |
Respiratory tract infection | below serious, 1 patient | 0.5 mg/kg single, intravenous Dose: 0.5 mg/kg Route: intravenous Route: single Dose: 0.5 mg/kg Sources: |
unhealthy n = 22 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 22 Sources: |
Suicidal ideation | below serious, 1 patient | 0.5 mg/kg single, intravenous Dose: 0.5 mg/kg Route: intravenous Route: single Dose: 0.5 mg/kg Sources: |
unhealthy n = 22 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 22 Sources: |
Tooth abscess | below serious, 1 patient | 0.5 mg/kg single, intravenous Dose: 0.5 mg/kg Route: intravenous Route: single Dose: 0.5 mg/kg Sources: |
unhealthy n = 22 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 22 Sources: |
Vertigo | below serious, 1 patient | 0.5 mg/kg single, intravenous Dose: 0.5 mg/kg Route: intravenous Route: single Dose: 0.5 mg/kg Sources: |
unhealthy n = 22 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 22 Sources: |
Vomiting | below serious, 1 patient | 0.5 mg/kg single, intravenous Dose: 0.5 mg/kg Route: intravenous Route: single Dose: 0.5 mg/kg Sources: |
unhealthy n = 22 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 22 Sources: |
Nausea | below serious, 3 patients | 0.5 mg/kg single, intravenous Dose: 0.5 mg/kg Route: intravenous Route: single Dose: 0.5 mg/kg Sources: |
unhealthy n = 22 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 22 Sources: |
Chest pain | below serious, 1 patient | 0.5 mg/kg single, oral Dose: 0.5 mg/kg Route: oral Route: single Dose: 0.5 mg/kg Sources: |
unhealthy n = 3 Health Status: unhealthy Condition: Depression and Anxiety|Cancer Population Size: 3 Sources: |
Headache | below serious, 2 patients | 0.5 mg/kg single, oral Dose: 0.5 mg/kg Route: oral Route: single Dose: 0.5 mg/kg Sources: |
unhealthy n = 3 Health Status: unhealthy Condition: Depression and Anxiety|Cancer Population Size: 3 Sources: |
Dissociation | below serious, 1 patient | 1 mg/kg single, intravenous Dose: 1 mg/kg Route: intravenous Route: single Dose: 1 mg/kg Sources: |
unhealthy n = 20 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 20 Sources: |
Dizziness | below serious, 1 patient | 1 mg/kg single, intravenous Dose: 1 mg/kg Route: intravenous Route: single Dose: 1 mg/kg Sources: |
unhealthy n = 20 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 20 Sources: |
Hypertension | below serious, 1 patient | 1 mg/kg single, intravenous Dose: 1 mg/kg Route: intravenous Route: single Dose: 1 mg/kg Sources: |
unhealthy n = 20 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 20 Sources: |
Insomnia | below serious, 1 patient | 1 mg/kg single, intravenous Dose: 1 mg/kg Route: intravenous Route: single Dose: 1 mg/kg Sources: |
unhealthy n = 20 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 20 Sources: |
Poor quality sleep | below serious, 1 patient | 1 mg/kg single, intravenous Dose: 1 mg/kg Route: intravenous Route: single Dose: 1 mg/kg Sources: |
unhealthy n = 20 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 20 Sources: |
Tachycardia | below serious, 1 patient | 1 mg/kg single, intravenous Dose: 1 mg/kg Route: intravenous Route: single Dose: 1 mg/kg Sources: |
unhealthy n = 20 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 20 Sources: |
Upper respiratory tract infection | below serious, 1 patient | 1 mg/kg single, intravenous Dose: 1 mg/kg Route: intravenous Route: single Dose: 1 mg/kg Sources: |
unhealthy n = 20 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 20 Sources: |
Vomiting | below serious, 1 patient | 1 mg/kg single, intravenous Dose: 1 mg/kg Route: intravenous Route: single Dose: 1 mg/kg Sources: |
unhealthy n = 20 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 20 Sources: |
Blood pressure increased | below serious, 2 patients | 1 mg/kg single, intravenous Dose: 1 mg/kg Route: intravenous Route: single Dose: 1 mg/kg Sources: |
unhealthy n = 20 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 20 Sources: |
Headache | below serious, 3 patients | 1 mg/kg single, intravenous Dose: 1 mg/kg Route: intravenous Route: single Dose: 1 mg/kg Sources: |
unhealthy n = 20 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 20 Sources: |
Nausea | below serious, 3 patients | 1 mg/kg single, intravenous Dose: 1 mg/kg Route: intravenous Route: single Dose: 1 mg/kg Sources: |
unhealthy n = 20 Health Status: unhealthy Condition: Treatment-Resistant Depression Population Size: 20 Sources: |
Delirium | below serious, 1 patient | 2.55 mg/kg single, intravenous (total daily dose) Dose: 2.55 mg/kg Route: intravenous Route: single Dose: 2.55 mg/kg Sources: |
unhealthy n = 10 Health Status: unhealthy Condition: Sepsis Population Size: 10 Sources: |
Pericardial effusion | serious, 1 patient | 2.55 mg/kg single, intravenous (total daily dose) Dose: 2.55 mg/kg Route: intravenous Route: single Dose: 2.55 mg/kg Sources: |
unhealthy n = 10 Health Status: unhealthy Condition: Sepsis Population Size: 10 Sources: |
Ventricular tachycardia | serious, 1 patient | 2.55 mg/kg single, intravenous (total daily dose) Dose: 2.55 mg/kg Route: intravenous Route: single Dose: 2.55 mg/kg Sources: |
unhealthy n = 10 Health Status: unhealthy Condition: Sepsis Population Size: 10 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
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Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
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likely | unlikely (co-administration study) Comment: Compared ketamine group with the control group, there were no significant difference for AUC of metroprolol, omeprazole and tolbutamide, it show that the ketamine may not induce or inhibit the activity of CYP1A2, CYP3A4 and CYP2B6 enzyme |
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likely | unlikely (co-administration study) Comment: Compared ketamine group with the control group, there were no significant difference for AUC of metroprolol, omeprazole and tolbutamide, it show that the ketamine may not induce or inhibit the activity of CYP1A2, CYP3A4 and CYP2B6 enzyme |
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likely | unlikely (co-administration study) Comment: Compared ketamine group with the control group, there were no significant difference for AUC of metroprolol, omeprazole and tolbutamide, it show that the ketamine may not induce or inhibit the activity of CYP1A2, CYP3A4 and CYP2B6 enzyme |
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yes [Ki 114.5 uM] | ||||
yes [Ki 22.7 uM] | ||||
yes [Ki 225.7 uM] |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/016812Orig1s046lbl.pdf#page=12 Page: 12.0 |
yes | |||
yes | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/016812Orig1s046lbl.pdf#page=12 Page: 12.0 |
yes |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
PubMed
Title | Date | PubMed |
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Ketamine-pancuronium-narcotic technic for cardiovascular surgery in infants--a comparative study. | 1975 Nov-Dec |
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Cardiovascular pathology possibly associated with ketamine/xylazine anesthesia in Dutch belted rabbits. | 1999 Apr |
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[Complications of anesthesia and their prevention in children with spastic cerebral palsy during ambulatory surgery]. | 1999 Jul-Aug |
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[Ketamine]. | 1999 Mar |
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Prolonged analgesic effect of ketamine, an N-methyl-D-aspartate receptor inhibitor, in patients with chronic pain. | 1999 May |
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Anticonvulsant efficacy of N-methyl-D-aspartate antagonists against convulsions induced by cocaine. | 1999 May |
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Midazolam attenuates ketamine-induced abnormal perception and thought process but not mood changes. | 2000 Sep |
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Interindividual differences in the analgesic response to ketamine in chronic orofacial pain. | 2001 |
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NMDA receptor blockade prevents nitroglycerin-induced headaches. | 2001 Jul-Aug |
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[Ketamine--dreams and realities]. | 2002 |
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Cognitive impairment after small-dose ketamine isomers in comparison to equianalgesic racemic ketamine in human volunteers. | 2002 Feb |
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Concentration-effect relationships for intravenous alfentanil and ketamine infusions in human volunteers: effects on acute thresholds and capsaicin-evoked hyperpathia. | 2002 Jan |
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The role of ketamine in preventing fentanyl-induced hyperalgesia and subsequent acute morphine tolerance. | 2002 May |
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Search of antimicrobial activity of selected non-antibiotic drugs. | 2002 Nov-Dec |
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Ketamine as an adjuvant to opioids for cancer pain. | 2003 |
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Ketamine for refractory status epilepticus: a case of possible ketamine-induced neurotoxicity. | 2003 Feb |
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[Anaesthesia for caesarean section. Comparison of two general anaesthetic regimens and spinal anaesthesia]. | 2003 Jan |
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Angina pain precipitated by a continuous subcutaneous infusion of ketamine. | 2003 Jan |
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Effects of the 5-HT2A agonist psilocybin on mismatch negativity generation and AX-continuous performance task: implications for the neuropharmacology of cognitive deficits in schizophrenia. | 2003 Jan |
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The effect of variable-dose diazepam on dreaming and emergence phenomena in 400 cases of ketamine-fentanyl anaesthesia. | 2003 Sep |
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[Expression of HSP70 induced by ketamine in the hippocampus of rat at different ages]. | 2004 Jul |
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Normal spatial and contextual learning for ketamine-treated rats in the pilocarpine epilepsy model. | 2004 May |
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Postanesthetic cerebellar dysfunction in cats. | 2004 May-Jun |
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Participation of adenosine system in the ketamine-induced motor activity in mice. | 2005 Jan-Feb |
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Safety of mixture of morphine with ketamine for postoperative patient-controlled analgesia: an audit with 1026 patients. | 2005 Jul |
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Severe refractory status epilepticus owing to presumed encephalitis. | 2005 Mar |
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Effect of N-methyl-D-aspartate receptor epsilon1 subunit gene disruption of the action of general anesthetic drugs in mice. | 2005 Mar |
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[Comparison of the suppressive effects of tramadol and low-dose ketamine on the patients with postoperative hyperalgesia after remifentanil-based anaesthesia]. | 2005 Oct |
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Induction of rat hepatic cytochrome P-450 by ketamine and its toxicological implications. | 2005 Sep |
Patents
Sample Use Guides
Intravenous Route:
The initial dose of Ketalar (ketamine hydrochloride injection) administered intravenously may range from 1 mg/kg to 4.5 mg/kg (0.5 to 2 mg/lb). The average amount required to produce five to ten minutes of surgical anesthesia has been 2 mg/kg (1 mg/lb).
Intramuscular Route:
The initial dose of Ketalar administered intramuscularly may range from 6.5 to 13 mg/kg (3 to 6 mg/lb). A dose of 10 mg/kg (5 mg/lb) will usually produce 12 to 25 minutes of surgical anesthesia.
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/25595994
Primary cultures of cortical neurons treated with ketamine (10 μM-10mM) at 3 days-in vitro (3 DIV) displayed a concentration-dependent decrease in expanded growth cones
Substance Class |
Chemical
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Record UNII |
O18YUO0I83
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Validated (UNII)
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Classification Tree | Code System | Code | ||
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FDA ORPHAN DRUG |
860021
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FDA ORPHAN DRUG |
901422
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DEA NO. |
7285
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CFR |
21 CFR 522.1222
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CFR |
21 CFR 522.1222B
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NCI_THESAURUS |
C245
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Code System | Code | Type | Description | ||
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DBSALT000396
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PRIMARY | |||
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C29142
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PRIMARY | |||
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100477-73-4
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SUPERSEDED | |||
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6121
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PRIMARY | |||
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SUB02830MIG
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PRIMARY | |||
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79499-52-8
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O18YUO0I83
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PRIMARY | |||
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650657
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PRIMARY | |||
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217-484-6
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PRIMARY | |||
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203184
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PRIMARY | RxNorm | ||
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CHEMBL742
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PRIMARY | |||
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1356009
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PRIMARY | |||
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81771-21-3
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96448-41-8
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15851
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PRIMARY | |||
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1867-66-9
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PRIMARY | |||
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DTXSID4040137
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PRIMARY | |||
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m6613
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PRIMARY | Merck Index | ||
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O18YUO0I83
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PRIMARY | |||
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KETAMINE HYDROCHLORIDE
Created by
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PRIMARY | Description: A white, crystalline powder; odour, characteristic. Solubility: Freely soluble in water and methanol R; soluble in ethanol (~750 g/l) TS; practically insoluble in ether R. Category: General anaesthetic. Storage: Ketamine hydrochloride should be kept in a well-closed container. Requirement: Ketamine hydrochloride contains not less than 98.5% and not more than the equivalent of 101.0% of C13H16ClNO,HCl, calculated with reference to the dried substance. | ||
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100000091352
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42551-62-2
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SUPERSEDED |
Related Record | Type | Details | ||
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ENANTIOMER -> RACEMATE | |||
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BASIS OF STRENGTH->SUBSTANCE |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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ENANTIOMER -> RACEMATE | |||
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BASIS OF STRENGTH->SUBSTANCE |
ASSAY (HPLC)
USP
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PARENT -> SALT/SOLVATE |
Related Record | Type | Details | ||
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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||
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
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