Stem definition | Drug id | CAS RN |
---|---|---|
diazepam derivatives | 1802 | 59467-70-8 |
Dose | Unit | Route |
---|---|---|
5 | mg | N |
15 | mg | O |
15 | mg | P |
10 | mg | SL |
Property | Value | Reference |
---|---|---|
EoM (Fraction excreted unchanged in urine) | 5.60 % | Benet LZ, Broccatelli F, Oprea TI |
CL (Clearance) | 5.30 mL/min/kg | Lombardo F, Berellini G, Obach RS |
BA (Bioavailability) | 44 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
t_half (Half-life) | 3.10 hours | Lombardo F, Berellini G, Obach RS |
S (Water solubility) | 10.30 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
Vd (Volume of distribution) | 1.10 L/kg | Lombardo F, Berellini G, Obach RS |
BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.26 ยตM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
fu (Fraction unbound in plasma) | 0.02 % | Lombardo F, Berellini G, Obach RS |
Date | Agency | Company | Orphan |
---|---|---|---|
Dec. 20, 1985 | FDA | ||
Sept. 25, 2020 | PMDA | TAKEDA PHARMACEUTICAL COMPANY LIMITED | |
Sept. 4, 2011 | EMA | Laboratorios Lesvi S.L. |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Status epilepticus | 344.76 | 16.00 | 159 | 29053 | 15074 | 63444736 |
Multiple-drug resistance | 322.00 | 16.00 | 112 | 29100 | 5058 | 63454752 |
Serotonin syndrome | 309.26 | 16.00 | 182 | 29030 | 28500 | 63431310 |
Hypotension | 299.95 | 16.00 | 486 | 28726 | 272118 | 63187692 |
Cardiac arrest | 255.62 | 16.00 | 261 | 28951 | 92284 | 63367526 |
Myoglobin urine present | 207.69 | 16.00 | 52 | 29160 | 720 | 63459090 |
Anaphylactic reaction | 198.21 | 16.00 | 195 | 29017 | 65905 | 63393905 |
Propofol infusion syndrome | 195.22 | 16.00 | 52 | 29160 | 931 | 63458879 |
Toxic encephalopathy | 175.31 | 16.00 | 77 | 29135 | 6502 | 63453308 |
Drug interaction | 164.49 | 16.00 | 340 | 28872 | 228791 | 63231019 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Status epilepticus | 265.26 | 14.33 | 149 | 27285 | 12465 | 34917032 |
Drug ineffective | 229.47 | 14.33 | 830 | 26604 | 455921 | 34473576 |
Hyperthermia malignant | 184.29 | 14.33 | 68 | 27366 | 2109 | 34927388 |
Hypotension | 183.91 | 14.33 | 481 | 26953 | 221168 | 34708329 |
Drug reaction with eosinophilia and systemic symptoms | 170.47 | 14.33 | 167 | 27267 | 32845 | 34896652 |
Multiple-drug resistance | 161.68 | 14.33 | 80 | 27354 | 5159 | 34924338 |
Cardiac arrest | 158.10 | 14.33 | 276 | 27158 | 95883 | 34833614 |
Anaphylactic reaction | 142.31 | 14.33 | 150 | 27284 | 32151 | 34897346 |
Drug ineffective for unapproved indication | 137.65 | 14.33 | 128 | 27306 | 23587 | 34905910 |
Bradycardia | 133.81 | 14.33 | 224 | 27210 | 75194 | 34854303 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Status epilepticus | 565.57 | 13.98 | 291 | 51461 | 24750 | 79667886 |
Hypotension | 426.62 | 13.98 | 904 | 50848 | 439413 | 79253223 |
Multiple-drug resistance | 399.17 | 13.98 | 166 | 51586 | 8642 | 79683994 |
Cardiac arrest | 383.90 | 13.98 | 514 | 51238 | 171582 | 79521054 |
Serotonin syndrome | 382.60 | 13.98 | 280 | 51472 | 44747 | 79647889 |
Drug ineffective | 366.61 | 13.98 | 1524 | 50228 | 1079389 | 78613247 |
Anaphylactic reaction | 311.30 | 13.98 | 325 | 51427 | 83418 | 79609218 |
Propofol infusion syndrome | 306.44 | 13.98 | 93 | 51659 | 1890 | 79690746 |
Drug ineffective for unapproved indication | 250.38 | 13.98 | 231 | 51521 | 51007 | 79641629 |
Diabetes insipidus | 238.29 | 13.98 | 99 | 51653 | 5138 | 79687498 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Drug ineffective | 61.12 | 27.94 | 31 | 127 | 1021 | 88613 |
Epilepsy | 34.62 | 27.94 | 11 | 147 | 93 | 89541 |
Source | Code | Description |
---|---|---|
ATC | N05CD08 | NERVOUS SYSTEM PSYCHOLEPTICS HYPNOTICS AND SEDATIVES Benzodiazepine derivatives |
CHEBI has role | CHEBI:35474 | anti-anxiety agents |
CHEBI has role | CHEBI:35488 | central nervous system depressants |
CHEBI has role | CHEBI:35610 | antineoplastic agents |
CHEBI has role | CHEBI:35623 | anticonvulsants |
CHEBI has role | CHEBI:35717 | hypnotics |
CHEBI has role | CHEBI:38869 | general anaesthetic |
CHEBI has role | CHEBI:51371 | muscle relaxants |
CHEBI has role | CHEBI:68495 | Type I cell-death inducers |
CHEBI has role | CHEBI:91016 | GABAA receptor agonists |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Feeling agitated | indication | 24199005 | |
Anxiety | indication | 48694002 | |
General anesthesia | indication | 50697003 | |
Sedation | indication | 72641008 | |
Status epilepticus | indication | 230456007 | DOID:1824 |
Conscious sedation | indication | 314271007 | |
Local anesthesia | indication | 386761002 | |
Sedation as Adjunct to Anesthesia | indication | ||
Induce Anterograde Amnesia | indication | ||
Sedation in Intubated Patients | indication |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 6.07 | Basic |
pKa2 | 2.36 | Basic |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
---|---|---|---|---|---|---|---|---|---|---|
5MG/SPRAY | NAYZILAM | UCB INC | N211321 | May 17, 2019 | RX | SPRAY | NASAL | 8217033 | Jan. 18, 2028 | ACUTE TREATMENT OF INTERMITTENT, STEREOTYPIC EPISODES OF FREQUENT SEIZURE ACTIVITY (I.E., SEIZURE CLUSTERS, ACUTE REPETITIVE SEIZURES) THAT ARE DISTINCT FROM A PATIENTS USUAL SEIZURE PATTERN IN PATIENTS WITH EPILEPSY 12 YEARS OF AGE AND OLDER |
5MG/SPRAY | NAYZILAM | UCB INC | N211321 | May 17, 2019 | RX | SPRAY | NASAL | 9289432 | Jan. 18, 2028 | ACUTE TREATMENT OF INTERMITTENT, STEREOTYPIC EPISODES OF FREQUENT SEIZURE ACTIVITY (I.E., SEIZURE CLUSTERS, ACUTE REPETITIVE SEIZURES) THAT ARE DISTINCT FROM A PATIENTS USUAL SEIZURE PATTERN IN PATIENTS WITH EPILEPSY 12 YEARS OF AGE AND OLDER |
5MG/SPRAY | NAYZILAM | UCB INC | N211321 | May 17, 2019 | RX | SPRAY | NASAL | 9687495 | Jan. 18, 2028 | ACUTE TREATMENT OF INTERMITTENT, STEREOTYPIC EPISODES OF FREQUENT SEIZURE ACTIVITY (I.E., SEIZURE CLUSTERS, ACUTE REPETITIVE SEIZURES) THAT ARE DISTINCT FROM A PATIENTS USUAL SEIZURE PATTERN IN PATIENTS WITH EPILEPSY 12 YEARS OF AGE AND OLDER |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
---|---|---|---|---|---|---|---|---|---|
100MG/100ML (1MG/ML) | MIDAZOLAM IN 0.9% SODIUM CHLORIDE | HIKMA | A216159 | April 17, 2023 | RX | SOLUTION | INTRAVENOUS | Jan. 2, 2024 | PATENT CHALLENGE |
50MG/50ML (1MG/ML) | MIDAZOLAM IN 0.9% SODIUM CHLORIDE | HIKMA | A216159 | April 17, 2023 | RX | SOLUTION | INTRAVENOUS | Jan. 2, 2024 | PATENT CHALLENGE |
5MG/SPRAY | NAYZILAM | UCB INC | N211321 | May 17, 2019 | RX | SPRAY | NASAL | May 17, 2026 | ACUTE TREATMENT OF INTERMITTENT, STEREOTYPIC EPISODES OF FREQUENT SEIZURE ACTIVITY (I.E., SEIZURE CLUSTERS, ACUTE REPETITIVE SEIZURES) THAT ARE DISTINCT FROM A PATIENTS USUAL SEIZURE PATTERN IN PATIENTS WITH EPILEPSY 12 YEARS OF AGE AND OLDER |
EQ 50MG BASE/10ML (EQ 5MG BASE/ML) | SEIZALAM | MMT | N209566 | Sept. 14, 2018 | RX | SOLUTION | INTRAMUSCULAR | Sept. 14, 2025 | TREATMENT OF STATUS EPILEPTICUS IN ADULTS |
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
GABA A receptor alpha-5/beta-2/gamma-3 | Ion channel | POSITIVE ALLOSTERIC MODULATOR | Ki | 8.26 | WOMBAT-PK | CHEMBL | |||
GABA-A receptor alpha-1/beta-2/gamma-3 | Ion channel | POSITIVE ALLOSTERIC MODULATOR | Ki | 7.75 | WOMBAT-PK | CHEMBL | |||
GABA A receptor alpha-3/beta-2/gamma-2 | Ion channel | POSITIVE ALLOSTERIC MODULATOR | Ki | 8.44 | WOMBAT-PK | CHEMBL | |||
GABA A receptor alpha-3/beta-2/gamma-3 | Ion channel | POSITIVE ALLOSTERIC MODULATOR | Ki | 7.61 | WOMBAT-PK | CHEMBL | |||
GABA A receptor alpha-5/beta-3/gamma-3 | Ion channel | POSITIVE ALLOSTERIC MODULATOR | Ki | 8.26 | WOMBAT-PK | CHEMBL | |||
GABA A receptor alpha-5/beta-2/gamma-2 | Ion channel | POSITIVE ALLOSTERIC MODULATOR | Ki | 9.13 | WOMBAT-PK | CHEMBL | |||
GABA-A receptor alpha-1/beta-2/gamma-2 | Ion channel | POSITIVE ALLOSTERIC MODULATOR | Ki | 8.75 | WOMBAT-PK | CHEMBL | |||
GABA-A receptor alpha-5/beta-3/gamma-2 | Ion channel | POSITIVE ALLOSTERIC MODULATOR | Ki | 9.13 | WOMBAT-PK | CHEMBL | |||
Multidrug resistance protein 1 | Transporter | Km | 4.35 | WOMBAT-PK | |||||
Cytochrome P450 3A4 | Enzyme | Km | 6 | WOMBAT-PK |
ID | Source |
---|---|
08J | PDB_CHEM_ID |
001467 | NDDF |
004585 | NDDF |
130935 | MMSL |
203128 | RXNORM |
24970 | MMSL |
26800000 | SNOMEDCT_US |
32073 | MMSL |
3342 | IUPHAR_LIGAND_ID |
373476007 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Midazolam | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0404-9912 | INJECTION, SOLUTION | 1 mg | INTRAVENOUS | ANDA | 14 sections |
Midazolam | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0404-9912 | INJECTION, SOLUTION | 1 mg | INTRAVENOUS | ANDA | 14 sections |
Midazolam | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0404-9913 | INJECTION | 1 mg | INTRAMUSCULAR | ANDA | 15 sections |
Midazolam | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0404-9913 | INJECTION | 1 mg | INTRAMUSCULAR | ANDA | 15 sections |
Midazolam | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0404-9913 | INJECTION | 1 mg | INTRAMUSCULAR | ANDA | 15 sections |
MIDAZOLAM | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0404-9914 | INJECTION, SOLUTION | 5 mg | INTRAVENOUS | ANDA | 15 sections |
MIDAZOLAM | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0404-9914 | INJECTION, SOLUTION | 5 mg | INTRAVENOUS | ANDA | 15 sections |
Midazolam | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0404-9915 | INJECTION, SOLUTION | 5 mg | INTRAVENOUS | ANDA | 14 sections |
Midazolam | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0404-9915 | INJECTION, SOLUTION | 5 mg | INTRAVENOUS | ANDA | 14 sections |
Midazolam Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-3566 | SYRUP | 2 mg | ORAL | ANDA | 25 sections |