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Metixene

Metixene structure

CAS No:
4969-02-2
Formula:
C20H23NS
Chemical Name:
Metixene
Synonyms:
Piperidine,1-methyl-3-(9H-thioxanthen-9-ylmethyl)-;Piperidine,1-methyl-3-(thioxanthen-9-ylmethyl)-;9H-Thioxanthene,piperidine deriv.;1-Methyl-3-(9H-thioxanthen-9-ylmethyl)piperidine;60 SJ 1977;Methixene;1-Methyl-3-[(thioxanthen-9-yl)methyl]piperidine;Metixene;Tremaril;Tremonil;Trest;(±)-Methixene;Metixen;114332-24-0
Categories:
Active Pharmaceutical Ingredients > Nervous System Drugs

Description

Solid

Metixene is a member of thioxanthenes and a member of piperidines. It has a role as an antiparkinson drug, a muscarinic antagonist and a histamine antagonist.|Metixene (or methixene) is a anticholinergic used as an antiparkinsonian agent.

Metixene Basic Attributes

Molecular Weight：

309.47

Exact Mass：

309.47

EC Number：

225-610-6

DSSTox ID：

DTXSID1047867

ATC Code：

N - Nervous system

Characteristics

PSA：

28.5

XLogP3：

4.7

Appearance：

Solid

Melting Point：

<25 °C

Boiling Point：

173 °C

Water Solubility：

soluble as HCl salt

Toxicity：

LD50 oral in mouse: 430mg/kg

Safety Information

Precautionary statement(s)：

P264, P270, P273, P301+P312, P330, P391, P501

Hazard Statements：

H302

GHS Classification：

|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P264, P270, P273, P301+P312, P330, P391, and P501|The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.

Toxicity

Toxicity Summary：

Signs of overdose include dilated and sluggish pupils, warm, dry skin, facial flushing, decreased secretions of the mouth, pharynx, nose, and bronchi, foul-smelling breath, elevated temperature, tachycardia, cardiac arrhythmias, decreased bowel sounds, urinary retention, delirium, disorientation, anxiety, hallucinations, illusions, confusion, incoherence, agitation, hyperactivity, ataxia, loss of memory, paranoia, combativeness, and seizures.

Drug Information

Drug Indication：

Used for the symptomatic treatment of parkinsonism.

Pharmacology：

Metixene is a tertiary antimuscarinic with actions similar to those of atropine; it also has antihistaminic and direct antispasmodic properties. It is used for the symptomatic treatment of parkinsonism, including the alleviation of the extrapyramidal syndrome induced by other drugs such as phenothiazines, but, like other antimuscarinics, it is of no value against tardive dyskinesias. Metixene has been discontinued.

Absorption：

Absorbed in the gastrointestinal tract following oral administration, however the extent of absorption is not known.

Metabolism/Metabolites：

Hepatic. Metabolism occurs via sulfoxydation and N-demethylation.

Mechanism of Action：

Parkinsonism is thought to result from an imbalance between the excitatory (cholinergic) and inhibitory (dopaminergic) systems in the corpus striatum. The mechanism of action of centrally active anticholinergic drugs such as metixene is considered to relate to competitive antagonism of acetylcholine at muscarinic receptors in the corpus striatum, which then restores the balance.

MeSH Entry Terms：

1-methyl-3-(thioxanthen-9-ylmethyl)- piperidine hydrochloride

Metixene Use and Manufacturing

Use Classification：

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:309.5
XLogP3:4.9
Hydrogen Bond Acceptor Count:2
Rotatable Bond Count:2
Exact Mass:309.15512091
Monoisotopic Mass:309.15512091
Topological Polar Surface Area:28.5
Heavy Atom Count:22
Complexity:349
Undefined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes