Stem definition | Drug id | CAS RN |
---|---|---|
imidazopyrimidine or pyrazolopyrimidine derivatives, used as anxiolytics, sedatives, hypnotics | 2857 | 151319-34-5 |
Dose | Unit | Route |
---|---|---|
10 | mg | O |
Property | Value | Reference |
---|---|---|
BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
EoM (Fraction excreted unchanged in urine) | 0.50 % | Benet LZ, Broccatelli F, Oprea TI |
MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.94 ยตM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
BA (Bioavailability) | 31 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Vd (Volume of distribution) | 1.30 L/kg | Lombardo F, Berellini G, Obach RS |
CL (Clearance) | 16 mL/min/kg | Lombardo F, Berellini G, Obach RS |
fu (Fraction unbound in plasma) | 0.40 % | Lombardo F, Berellini G, Obach RS |
t_half (Half-life) | 1.10 hours | Lombardo F, Berellini G, Obach RS |
Date | Agency | Company | Orphan |
---|---|---|---|
Aug. 13, 1999 | FDA | PFIZER |
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 |
---|---|---|---|---|---|---|
Completed suicide | 76.22 | 22.94 | 42 | 1007 | 131847 | 50472228 |
Somnambulism | 31.45 | 22.94 | 9 | 1040 | 4915 | 50599160 |
Toxicity to various agents | 24.79 | 22.94 | 26 | 1023 | 212473 | 50391602 |
None
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 |
---|---|---|---|---|---|---|
Completed suicide | 114.70 | 24.48 | 63 | 1116 | 224351 | 64273202 |
Somnambulism | 32.19 | 24.48 | 9 | 1170 | 5132 | 64492421 |
Toxicity to various agents | 28.47 | 24.48 | 34 | 1145 | 363479 | 64134074 |
None
Source | Code | Description |
---|---|---|
ATC | N05CF03 | NERVOUS SYSTEM PSYCHOLEPTICS HYPNOTICS AND SEDATIVES Benzodiazepine related drugs |
FDA MoA | N0000000196 | GABA A Agonists |
MeSH PA | D000927 | Anticonvulsants |
MeSH PA | D002491 | Central Nervous System Agents |
MeSH PA | D002492 | Central Nervous System Depressants |
MeSH PA | D018682 | GABA Agents |
MeSH PA | D018757 | GABA Modulators |
MeSH PA | D006993 | Hypnotics and Sedatives |
MeSH PA | D018377 | Neurotransmitter Agents |
CHEBI has role | CHEBI:35474 | anti-anxiety agents |
CHEBI has role | CHEBI:35488 | central nervous system depressants |
CHEBI has role | CHEBI:35623 | anticonvulsants |
CHEBI has role | CHEBI:35717 | hypnotics |
FDA PE | N0000175728 | Central Nervous System Depression |
FDA EPC | N0000183360 | gamma-Aminobutyric Acid A Receptor Agonist |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Initial insomnia | indication | 59050008 | |
Disorders of initiating and maintaining sleep | indication | 194437008 | |
Depressive disorder | contraindication | 35489007 | |
Hepatic failure | contraindication | 59927004 | |
Sleep apnea | contraindication | 73430006 | DOID:0050847 |
Decreased respiratory function | contraindication | 80954004 | |
Sleep automatism | contraindication | 247962006 | |
Psychiatric Disturbance | contraindication | ||
Chronic Obstructive Pulmonary Disease with Bronchospasms | contraindication |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 3.81 | Basic |
None
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
GABA-A receptor alpha-2/beta-3/gamma-2 | Ion channel | POSITIVE ALLOSTERIC MODULATOR | EC50 | 5.79 | WOMBAT-PK | CHEMBL | |||
GABA-A receptor alpha-1/beta-2/gamma-2 | Ion channel | POSITIVE ALLOSTERIC MODULATOR | EC50 | 6.53 | WOMBAT-PK | SCIENTIFIC LITERATURE |
ID | Source |
---|---|
4021177 | VUID |
N0000148625 | NUI |
D00530 | KEGG_DRUG |
4021177 | VANDF |
C0251504 | UMLSCUI |
CHEBI:10102 | CHEBI |
CHEMBL1521 | ChEMBL_ID |
DB00962 | DRUGBANK_ID |
C085665 | MESH_SUPPLEMENTAL_RECORD_UI |
5719 | PUBCHEM_CID |
4345 | IUPHAR_LIGAND_ID |
7312 | INN_ID |
S62U433RMH | UNII |
261654 | RXNORM |
136698 | MMSL |
31278 | MMSL |
8288 | MMSL |
d04452 | MMSL |
007833 | NDDF |
116104009 | SNOMEDCT_US |
387012004 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Zaleplon | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-0084 | CAPSULE | 5 mg | ORAL | ANDA | 25 sections |
Zaleplon | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-0085 | CAPSULE | 10 mg | ORAL | ANDA | 25 sections |
ZALEPLON | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21695-105 | CAPSULE | 10 mg | ORAL | NDA | 24 sections |
ZALEPLON | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21695-376 | CAPSULE | 5 mg | ORAL | NDA | 24 sections |
zaleplon | HUMAN PRESCRIPTION DRUG LABEL | 1 | 29300-131 | CAPSULE | 5 mg | ORAL | ANDA | 23 sections |
zaleplon | HUMAN PRESCRIPTION DRUG LABEL | 1 | 29300-132 | CAPSULE | 10 mg | ORAL | ANDA | 23 sections |
zaleplon | HUMAN PRESCRIPTION DRUG LABEL | 1 | 33261-454 | CAPSULE | 10 mg | ORAL | ANDA | 17 sections |
zaleplon | HUMAN PRESCRIPTION DRUG LABEL | 1 | 33261-486 | CAPSULE | 5 mg | ORAL | ANDA | 17 sections |
Zaleplon | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42043-210 | CAPSULE | 5 mg | ORAL | ANDA | 26 sections |
Zaleplon | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42043-211 | CAPSULE | 10 mg | ORAL | ANDA | 26 sections |
zaleplon | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42254-130 | CAPSULE | 5 mg | ORAL | ANDA | 16 sections |
zaleplon | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42254-147 | CAPSULE | 10 mg | ORAL | ANDA | 16 sections |
zaleplon | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42254-189 | CAPSULE | 5 mg | ORAL | ANDA | 16 sections |
ZALEPLON | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43063-505 | CAPSULE | 5 mg | ORAL | ANDA | 26 sections |
ZALEPLON | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43063-505 | CAPSULE | 5 mg | ORAL | ANDA | 26 sections |
zaleplon | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43063-783 | CAPSULE | 10 mg | ORAL | ANDA | 23 sections |
Zaleplon | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43063-912 | CAPSULE | 10 mg | ORAL | ANDA | 25 sections |
zaleplon | HUMAN PRESCRIPTION DRUG LABEL | 1 | 45865-541 | CAPSULE | 10 mg | ORAL | ANDA | 24 sections |
zaleplon | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50090-1564 | CAPSULE | 10 mg | ORAL | ANDA | 23 sections |
ZALEPLON | Human Prescription Drug Label | 1 | 52959-957 | CAPSULE | 10 mg | ORAL | ANDA | 23 sections |
Sonata | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-4431 | CAPSULE | 10 mg | ORAL | NDA | 14 sections |
Sonata | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-5139 | CAPSULE | 5 mg | ORAL | NDA | 14 sections |
ZALEPLON | Human Prescription Drug Label | 1 | 54868-5908 | CAPSULE | 10 mg | ORAL | ANDA | 26 sections |
ZALEPLON | Human Prescription Drug Label | 1 | 54868-5909 | CAPSULE | 5 mg | ORAL | ANDA | 26 sections |
ZALEPLON | Human Prescription Drug Label | 1 | 57237-239 | CAPSULE | 5 mg | ORAL | ANDA | 26 sections |
ZALEPLON | Human Prescription Drug Label | 1 | 57237-240 | CAPSULE | 10 mg | ORAL | ANDA | 26 sections |
ZALEPLON | HUMAN PRESCRIPTION DRUG LABEL | 1 | 61919-629 | CAPSULE | 10 mg | ORAL | ANDA | 14 sections |
zaleplon | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63629-3405 | CAPSULE | 10 mg | ORAL | ANDA | 23 sections |
ZALEPLON | Human Prescription Drug Label | 1 | 65862-214 | CAPSULE | 5 mg | ORAL | ANDA | 26 sections |
ZALEPLON | Human Prescription Drug Label | 1 | 65862-215 | CAPSULE | 10 mg | ORAL | ANDA | 26 sections |