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mianserin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
serotonin receptor antagonists (mostly 5-HT2)	1796	24219-97-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: mianserin hydrochloride mianserin mianserine (+/-)-Mianserin mianserine hydrochloride mianserin HCl mianserine HCl	A tetracyclic compound with antidepressant effects. It may cause drowsiness and hematological problems. Its mechanism of therapeutic action is not well understood, although it apparently blocks alpha-adrenergic, histamine H1, and some types of serotonin receptors. Molecular weight: 264.37 Formula: C18H20N2 CLOGP: 4.01 LIPINSKI: 0 HAC: 2 HDO: 0 TPSA: 6.48 ALOGS: -3.06 ROTB: 0

Molecule

Description

Molfile Inchi Smiles

Synonyms:

mianserin hydrochloride
mianserin
mianserine
(+/-)-Mianserin
mianserine hydrochloride
mianserin HCl
mianserine HCl

A tetracyclic compound with antidepressant effects. It may cause drowsiness and hematological problems. Its mechanism of therapeutic action is not well understood, although it apparently blocks alpha-adrenergic, histamine H1, and some types of serotonin receptors.

Molecular weight: 264.37
Formula: C18H20N2
CLOGP: 4.01
LIPINSKI: 0
HAC: 2
HDO: 0
TPSA: 6.48
ALOGS: -3.06
ROTB: 0

Drug dosage:

Dose	Unit	Route
60	mg	O

ADMET properties:

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Property	Value	Reference
t_half (Half-life)	9.60 hours	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	6.48 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
EoM (Fraction excreted unchanged in urine)	5 %	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	3.40 mg/mL	Benet LZ, Broccatelli F, Oprea TI
BA (Bioavailability)	22 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
CL (Clearance)	21.90 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	13.75 L/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.05 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Jan. 1, 1976	YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

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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
Coma	199.77	31.27	102	5462	64262	63419196
Camptocormia	173.41	31.27	29	5535	280	63483178
Pleurothotonus	153.06	31.27	33	5531	1316	63482142
Hyponatraemia	149.82	31.27	103	5461	111797	63371661
Toxicity to various agents	123.85	31.27	129	5435	247121	63236337
Somnolence	109.27	31.27	104	5460	178581	63304877
Hepatocellular injury	104.44	31.27	50	5514	27331	63456127
Fall	102.11	31.27	147	5417	392187	63091271
Agranulocytosis	99.23	31.27	47	5517	25087	63458371
Cholestasis	98.04	31.27	49	5515	29385	63454073

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FDA Adverse Event Reporting System (Male)

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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
Cerebral artery thrombosis	100.10	26.17	22	3837	758	34952314
Coma	89.08	26.17	58	3801	45620	34907452
Brain scan abnormal	86.69	26.17	20	3839	860	34952212
Somnolence	62.87	26.17	69	3790	111047	34842025
Areflexia	62.20	26.17	20	3839	3011	34950061
Ischaemic stroke	58.62	26.17	32	3827	18218	34934854
Hepatocellular injury	52.77	26.17	32	3827	22179	34930893
Respiratory distress	49.98	26.17	37	3822	35628	34917444
Hemiplegia	45.97	26.17	20	3839	6952	34946120
Poikiloderma	45.88	26.17	9	3850	175	34952897

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FDA Adverse Event Reporting System (Geriatric)

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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
Coma	265.84	24.77	159	9295	100490	79634444
Somnolence	167.63	24.77	172	9282	238809	79496125
Camptocormia	151.40	24.77	29	9425	459	79734475
Hepatocellular injury	138.07	24.77	80	9374	47513	79687421
Poisoning deliberate	130.08	24.77	57	9397	18771	79716163
Cholestasis	128.79	24.77	79	9375	52030	79682904
Agranulocytosis	118.30	24.77	71	9383	44959	79689975
Pleurothotonus	117.97	24.77	32	9422	2484	79732450
Hyponatraemia	112.03	24.77	121	9333	177727	79557207
Fall	97.24	24.77	192	9262	487437	79247497

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N06AX03	NERVOUS SYSTEM PSYCHOANALEPTICS ANTIDEPRESSANTS Other antidepressants
CHEBI has role	CHEBI:176497	geroprotectors
CHEBI has role	CHEBI:35469	antidepressants
CHEBI has role	CHEBI:35640	adrenergic uptake inhibitors
CHEBI has role	CHEBI:35678	histamine agonists
CHEBI has role	CHEBI:35717	hypnotics
CHEBI has role	CHEBI:37890	alpha-adrenergic receptor blockaders
CHEBI has role	CHEBI:37955	H1 receptor antagonists
CHEBI has role	CHEBI:48279	serotonin antagonists
CHEBI has role	CHEBI:76779	post-proline endopeptidase inhibitors

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Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Major depressive disorder	indication	370143000

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.2	Basic
pKa2	1.03	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN	ANTAGONIST	Ki	8.17	WOMBAT-PK	IUPHAR
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN	ANTAGONIST	Ki	8.12	WOMBAT-PK	IUPHAR
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN	ANTAGONIST	Ki	8.52	WOMBAT-PK	IUPHAR
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		Ki	5.40	PDSP
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN		Kd	7.15	WOMBAT-PK
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	6.13	WOMBAT-PK
5-hydroxytryptamine receptor 6	GPCR	P50406	5HT6R_HUMAN		Ki	7.18	WOMBAT-PK
5-hydroxytryptamine receptor 7	GPCR	P34969	5HT7R_HUMAN		Ki	7.06	WOMBAT-PK
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN		IC50	6.39	CHEMBL
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		Ki	7.57	WOMBAT-PK

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External reference:

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ID	Source
004006	NDDF
004007	NDDF
135	IUPHAR_LIGAND_ID
18113	MMSL
203127	RXNORM
21535-47-7	SECONDARY_CAS_RN
250PJI13LM	UNII
2543	INN_ID
387565003	SNOMEDCT_US
395795008	SNOMEDCT_US

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Pharmaceutical products:

None