zaleplon 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| imidazopyrimidine or pyrazolopyrimidine derivatives, used as anxiolytics, sedatives, hypnotics | 2857 | 151319-34-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
an azabicyclo(4.3.0)nonane; a nonbenzodiazepine; one of the so-called of Z drugs (zopiclone, eszopiclone, zolpidem, and zaleplon) for which there is some correlation with tumors; a hypnotic with less marked effect on psychomotor functions compared to lorazepam
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 10 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Bocci G, Oprea TI, Benet LZ |
| EoM (Fraction excreted unchanged in urine) | 0.50 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.94 µM/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 |
| S (Water solubility) | 0.04 mg/mL | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 13, 1999 | FDA | PFIZER |
FDA Adverse Event Reporting System (Female)
| 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 | 103.38 | 23.12 | 52 | 1177 | 145621 | 63342172 |
| Somnambulism | 31.00 | 23.12 | 9 | 1220 | 5534 | 63482259 |
| Toxicity to various agents | 26.47 | 23.12 | 28 | 1201 | 247222 | 63240571 |
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
| 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 | 142.14 | 24.50 | 73 | 1276 | 245694 | 79497345 |
| Somnambulism | 31.92 | 24.50 | 9 | 1340 | 5712 | 79737327 |
| Toxicity to various agents | 29.73 | 24.50 | 36 | 1313 | 421504 | 79321535 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| 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 |
Drug Use | Suggest Off label Use Form| |View source of the data|
| 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 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 3.81 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| 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 |
External reference:
| 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 |
Pharmaceutical products:
| 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 | 0054-0084 | 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 | 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 | 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 |