Details of the Drug

General Information of Drug (ID: DMGFWSM)

• Drug Name: Zaleplon
• Synonyms: Sonata; Zalaplon; Zerene; CL 284846; L 846; L846; LJC 10846; ZAL 846; AZ-007; CL 284,846; CL-284846; CL284,846; L-846; LJC-10846; SKP-1041; Sonata (TN); Staccato-zaleplon; Starnoc (TN); ZAL-846; Zaleplon [USAN:INN]; Zaleplon (JAN/USAN/INN); N-[3-(3-cyanopyrazolo[1,5-a]pyrimidin-7-yl)phenyl]-N-ethylacetamide; N-(3-(3-Cyanopyrazolo(1,5-a)pyrimidin-7-yl)phenyl)-N-ethylacetamide; 3'-(3-Cyanopyrazolo(1,5-a)pyrimidin-7-yl)-N-ethylacetanilide; 3'-(3-Cyanopyrazolo(1,5-alpha)pyrimidin-7-yl)-N-ethylacetanilide

Indication

Disease Entry	ICD 11	Status	REF
Insomnia	7A00-7A0Z	Approved	[1], [2]

• Therapeutic Class: Hypnotics and Sedatives
• Drug Type: Small molecular drug
• #Ro5 Violations (Lipinski): 0:
  Molecular Weight (mw); 305.33
  Topological Polar Surface Area (xlogp); 1
  Rotatable Bond Count (rotbonds); 3
  Hydrogen Bond Donor Count (hbonddonor); 0
  Hydrogen Bond Acceptor Count (hbondacc); 4
• ADMET Property:
  Absorption: The drug is rapidly and completely absorbed following oral administration [3]
  BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [4]
  Clearance: The clearance of drug is 1 L/h/kg [5]
  Elimination: 0.5% of drug is excreted from urine in the unchanged form [4]
  Half-life: The concentration or amount of drug in body reduced by one-half in 1 hours [6]
  Metabolism: The drug is metabolized via the aldehyde oxidase [3]
  MRTD: The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 0.9366 micromolar/kg/day [7]
  Unbound Fraction: The unbound fraction of drug in plasma is 0.4% [6]
  Vd: The volume of distribution (Vd) of drug is 1.4 L/kg [5]
• Chemical Identifiers:
  Formula: C17H15N5O
  IUPAC Name: N-[3-(3-cyanopyrazolo[1,5-a]pyrimidin-7-yl)phenyl]-N-ethylacetamide
  Canonical SMILES: CCN(C1=CC=CC(=C1)C2=CC=NC3=C(C=NN23)C#N)C(=O)C
  InChI: InChI=1S/C17H15N5O/c1-3-21(12(2)23)15-6-4-5-13(9-15)16-7-8-19-17-14(10-18)11-20-22(16)17/h4-9,11H,3H2,1-2H3
  InChIKey: HUNXMJYCHXQEGX-UHFFFAOYSA-N
• Cross-matching ID:
  PubChem CID: 5719
  ChEBI ID: CHEBI:10102
  CAS Number: 151319-34-5
  DrugBank ID: DB00962
  TTD ID: D09DWL
  INTEDE ID: DR1725
  ACDINA ID: D00738

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
GABA(A) receptor alpha-1 (GABRA1)	TT1MPAY	GBRA1_HUMAN	Modulator	[8]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Substrate	[9]
Cytochrome P450 3A5 (CYP3A5)	DEIBDNY	CP3A5_HUMAN	Substrate	[10]
Cytochrome P450 3A7 (CYP3A7)	DERD86B	CP3A7_HUMAN	Substrate	[10]
Aldehyde oxidase (AOX1)	DEAWHS8	AOXA_HUMAN	Substrate	[11]

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Zaleplon (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Arn-509	DMT81LZ	Moderate	Increased metabolism of Zaleplon caused by Arn-509 mediated induction of CYP450 enzyme.	Acute myeloid leukaemia [2A60]	[39]
Oliceridine	DM6MDCF	Major	Additive CNS depression effects by the combination of Zaleplon and Oliceridine.	Acute pain [MG31]	[40]
Posaconazole	DMUL5EW	Moderate	Decreased metabolism of Zaleplon caused by Posaconazole mediated inhibition of CYP450 enzyme.	Aspergillosis [1F20]	[39]
Telithromycin	DMZ4P3A	Moderate	Decreased metabolism of Zaleplon caused by Telithromycin mediated inhibition of CYP450 enzyme.	Bacterial infection [1A00-1C4Z]	[41]
Pexidartinib	DMS2J0Z	Moderate	Increased metabolism of Zaleplon caused by Pexidartinib mediated induction of CYP450 enzyme.	Bone/articular cartilage neoplasm [2F7B]	[42]
Tucatinib	DMBESUA	Moderate	Decreased metabolism of Zaleplon caused by Tucatinib mediated inhibition of CYP450 enzyme.	Breast cancer [2C60-2C6Y]	[43]
Dihydrocodeine	DMB0FWL	Major	Additive CNS depression effects by the combination of Zaleplon and Dihydrocodeine.	Chronic pain [MG30]	[44]
Esketamine	DMVU687	Moderate	Additive CNS depression effects by the combination of Zaleplon and Esketamine.	Depression [6A70-6A7Z]	[45]
Cenobamate	DMGOVHA	Moderate	Increased metabolism of Zaleplon caused by Cenobamate mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[46]
Fosphenytoin	DMOX3LB	Minor	Increased metabolism of Zaleplon caused by Fosphenytoin mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[47]
Itraconazole	DMCR1MV	Moderate	Decreased metabolism of Zaleplon caused by Itraconazole mediated inhibition of CYP450 enzyme.	Fungal infection [1F29-1F2F]	[48]
Sulfinpyrazone	DMEV954	Minor	Increased metabolism of Zaleplon caused by Sulfinpyrazone mediated induction of CYP450 enzyme.	Gout [FA25]	[47]
Rifampin	DMA8J1G	Moderate	Increased metabolism of Zaleplon caused by Rifampin mediated induction of CYP450 enzyme.	HIV-infected patients with tuberculosis [1B10-1B14]	[47]
Rifapentine	DMCHV4I	Minor	Increased metabolism of Zaleplon caused by Rifapentine mediated induction of CYP450 enzyme.	HIV-infected patients with tuberculosis [1B10-1B14]	[47]
Saquinavir	DMG814N	Moderate	Decreased metabolism of Zaleplon caused by Saquinavir mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[49]
Etravirine	DMGV8QU	Moderate	Increased metabolism of Zaleplon caused by Etravirine mediated induction of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[50]
Berotralstat	DMWA2DZ	Moderate	Decreased metabolism of Zaleplon caused by Berotralstat mediated inhibition of CYP450 enzyme.	Innate/adaptive immunodeficiency [4A00]	[51]
PF-06463922	DMKM7EW	Moderate	Increased metabolism of Zaleplon caused by PF-06463922 mediated induction of CYP450 enzyme.	Lung cancer [2C25]	[52]
Allopregnanolone	DMNLHAC	Moderate	Additive CNS depression effects by the combination of Zaleplon and Allopregnanolone.	Mental/behavioural/neurodevelopmental disorder [6E20-6E8Z]	[53]
Lasmiditan	DMXLVDT	Moderate	Additive CNS depression effects by the combination of Zaleplon and Lasmiditan.	Migraine [8A80]	[54]
Flibanserin	DM70DTN	Moderate	Additive CNS depression effects by the combination of Zaleplon and Flibanserin.	Mood disorder [6A60-6E23]	[55]
Thalidomide	DM70BU5	Moderate	Additive CNS depression effects by the combination of Zaleplon and Thalidomide.	Multiple myeloma [2A83]	[56]
Nilotinib	DM7HXWT	Moderate	Decreased metabolism of Zaleplon caused by Nilotinib mediated inhibition of CYP450 enzyme.	Myeloproliferative neoplasm [2A20]	[57]
Levomethadyl Acetate	DM06HG5	Major	Additive CNS depression effects by the combination of Zaleplon and Levomethadyl Acetate.	Opioid use disorder [6C43]	[44]
Apraclonidine	DMO4PVE	Moderate	Additive CNS depression effects by the combination of Zaleplon and Apraclonidine.	Optic nerve disorder [9C40]	[58]
Oxymorphone	DM65AGJ	Major	Additive CNS depression effects by the combination of Zaleplon and Oxymorphone.	Pain [MG30-MG3Z]	[40]
Dezocine	DMJDB0Y	Major	Additive CNS depression effects by the combination of Zaleplon and Dezocine.	Pain [MG30-MG3Z]	[40]
Abametapir	DM2RX0I	Moderate	Decreased metabolism of Zaleplon caused by Abametapir mediated inhibition of CYP450 enzyme.	Pediculosis [1G00]	[59]
Lefamulin	DME6G97	Moderate	Decreased metabolism of Zaleplon caused by Lefamulin mediated inhibition of CYP450 enzyme.	Pneumonia [CA40]	[60]
Lonafarnib	DMGM2Z6	Moderate	Decreased metabolism of Zaleplon caused by Lonafarnib mediated inhibition of CYP450 enzyme.	Premature ageing appearance [LD2B]	[61]
Enzalutamide	DMGL19D	Moderate	Increased metabolism of Zaleplon caused by Enzalutamide mediated induction of CYP450 enzyme.	Prostate cancer [2C82]	[62]
Temsirolimus	DMS104F	Moderate	Increased plasma concentrations of Zaleplon and Temsirolimus due to competitive inhibition of the same metabolic pathway.	Renal cell carcinoma [2C90]	[63]
Dexamethasone	DMMWZET	Minor	Increased metabolism of Zaleplon caused by Dexamethasone mediated induction of CYP450 enzyme.	Rheumatoid arthritis [FA20]	[47]
Larotrectinib	DM26CQR	Moderate	Decreased metabolism of Zaleplon caused by Larotrectinib mediated inhibition of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[45]
Fostamatinib	DM6AUHV	Moderate	Decreased metabolism of Zaleplon caused by Fostamatinib mediated inhibition of CYP450 enzyme.	Thrombocytopenia [3B64]	[64]

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Allura red AC dye	E00338	33258	Colorant
FD&C blue no. 1	E00263	19700	Colorant
FD&C blue no. 2	E00446	2723854	Colorant
Hydrazine yellow	E00409	164825	Colorant
Quinoline yellow WS	E00309	24671	Colorant
Sodium lauryl sulfate	E00464	3423265	Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Stearic acid	E00079	5281	Emulsifying agent; Solubilizing agent; Viscosity-controlling agent; lubricant
Beta-D-lactose	E00099	6134	Diluent; Dry powder inhaler carrier; Lyophilization aid
Eisenoxyd	E00585	56841934	Colorant
Ferric hydroxide oxide yellow	E00539	23320441	Colorant
Ferrosoferric oxide	E00231	14789	Colorant
Lactose monohydrate	E00393	104938	Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate	E00208	11177	lubricant
Propylene glycol	E00040	1030	Antimicrobial preservative; Humectant; Plasticizing agent; Solvent
Silicon dioxide	E00670	Not Available	Anticaking agent; Opacifying agent; Viscosity-controlling agent
Titanium dioxide	E00322	26042	Coating agent; Colorant; Opacifying agent

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Zaleplon 10 mg capsule	10 mg	Oral Capsule	Oral
Zaleplon 5 mg capsule	5 mg	Oral Capsule	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

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