- Generic Name
- DrugBank Accession Number
Metixene (or methixene) is a anticholinergic used as an antiparkinsonian agent.
- Small Molecule
- Average: 309.468
- Chemical Formula
- External IDs
- 60 SJ 1977
Used for the symptomatic treatment of parkinsonism.Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.
- Contraindications & Blackbox Warnings
- Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.
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.
- 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.
Target Actions Organism AMuscarinic acetylcholine receptorantagonist Humans
Absorbed in the gastrointestinal tract following oral administration, however the extent of absorption is not known.
- Volume of distribution
- Protein binding
Hepatic. Metabolism occurs via sulfoxydation and N-demethylation.
- Route of elimination
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.
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.
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction 1,2-Benzodiazepine 1,2-Benzodiazepine may increase the central nervous system depressant (CNS depressant) activities of Metixene. Acetazolamide Acetazolamide may increase the central nervous system depressant (CNS depressant) activities of Metixene. Acetophenazine Acetophenazine may increase the central nervous system depressant (CNS depressant) activities of Metixene. Aclidinium The risk or severity of adverse effects can be increased when Metixene is combined with Aclidinium. Adenosine The risk or severity of Tachycardia can be increased when Metixene is combined with Adenosine. Agomelatine Agomelatine may increase the central nervous system depressant (CNS depressant) activities of Metixene. Alfentanil The risk or severity of adverse effects can be increased when Metixene is combined with Alfentanil. Alimemazine Alimemazine may increase the central nervous system depressant (CNS depressant) activities of Metixene. Alloin The therapeutic efficacy of Alloin can be decreased when used in combination with Metixene. Almotriptan Almotriptan may increase the central nervous system depressant (CNS depressant) activities of Metixene.Identify potential medication risksEasily compare up to 40 drugs with our drug interaction checker.Get severity rating, description, and management advice.Learn more
- Food Interactions
- Not Available
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Product Ingredients
Ingredient UNII CAS InChI Key Metixene hydrochloride FRK5BSL54S 7081-40-5 RSXZRFHNNTTWCB-UHFFFAOYSA-N
- International/Other Brands
- Cholinfall / Methixart / Tremaril / Tremarit
- ATC Codes
- N04AA03 — Metixene
- Drug Categories
- Chemical TaxonomyProvided by Classyfire
- This compound belongs to the class of organic compounds known as thioxanthenes. These are organic polycyclic compounds containing a thioxanthene moiety, which is an aromatic tricycle derived from xanthene by replacing the oxygen atom with a sulfur atom.
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Sub Class
- Direct Parent
- Alternative Parents
- Diarylthioethers / Aralkylamines / Piperidines / Benzenoids / Trialkylamines / Azacyclic compounds / Organopnictogen compounds / Hydrocarbon derivatives
- Amine / Aralkylamine / Aromatic heteropolycyclic compound / Aryl thioether / Azacycle / Benzenoid / Diarylthioether / Hydrocarbon derivative / Organic nitrogen compound / Organonitrogen compound
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- piperidines, thioxanthenes (CHEBI:51024)
- Affected organisms
- Humans and other mammals
- CAS number
- InChI Key
- IUPAC Name
- General References
- Link [Link]
- Novartis pharmaceuticals corp
- Not Available
- Dosage Forms
Form Route Strength Tablet
- Not Available
- Not Available
- Experimental Properties
Property Value Source melting point (°C) < 25 °C PhysProp boiling point (°C) 173 °C at 7.00E-02 mm Hg PhysProp water solubility Soluble as HCl salt Not Available logP 4.7 Not Available
- Predicted Properties
Property Value Source Water Solubility 0.000102 mg/mL ALOGPS logP 5.51 ALOGPS logP 5.06 ChemAxon logS -6.5 ALOGPS pKa (Strongest Basic) 9.34 ChemAxon Physiological Charge 1 ChemAxon Hydrogen Acceptor Count 1 ChemAxon Hydrogen Donor Count 0 ChemAxon Polar Surface Area 3.24 Å2 ChemAxon Rotatable Bond Count 2 ChemAxon Refractivity 97.17 m3·mol-1 ChemAxon Polarizability 35.67 Å3 ChemAxon Number of Rings 4 ChemAxon Bioavailability 1 ChemAxon Rule of Five No ChemAxon Ghose Filter Yes ChemAxon Veber's Rule Yes ChemAxon MDDR-like Rule No ChemAxon
- Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9825 Blood Brain Barrier + 0.995 Caco-2 permeable + 0.7863 P-glycoprotein substrate Substrate 0.81 P-glycoprotein inhibitor I Inhibitor 0.51 P-glycoprotein inhibitor II Inhibitor 0.8379 Renal organic cation transporter Inhibitor 0.8034 CYP450 2C9 substrate Non-substrate 0.7575 CYP450 2D6 substrate Substrate 0.7452 CYP450 3A4 substrate Non-substrate 0.5709 CYP450 1A2 substrate Non-inhibitor 0.8941 CYP450 2C9 inhibitor Non-inhibitor 0.9516 CYP450 2D6 inhibitor Inhibitor 0.9146 CYP450 2C19 inhibitor Non-inhibitor 0.9025 CYP450 3A4 inhibitor Non-inhibitor 0.951 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.6914 Ames test Non AMES toxic 0.8216 Carcinogenicity Non-carcinogens 0.9644 Biodegradation Not ready biodegradable 0.973 Rat acute toxicity 2.4059 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.6823 hERG inhibition (predictor II) Inhibitor 0.8044
- Mass Spec (NIST)
- Not Available
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
- Protein group
- Pharmacological action
- Curator comments
- Metixene has widespread antimuscarinic effects, but the data is currently limited on the exact receptors and their subunits.
- General Function
- Phosphatidylinositol phospholipase c activity
- Specific Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
|Muscarinic acetylcholine receptor M1||P11229|
|Muscarinic acetylcholine receptor M2||P08172|
|Muscarinic acetylcholine receptor M3||P20309|
|Muscarinic acetylcholine receptor M4||P08173|
|Muscarinic acetylcholine receptor M5||P08912|
- Authors unspecified: Evaluation of an antispasmodic agent. Methixene hydrochloride (Trest). JAMA. 1966 Mar 7;195(10):851. doi: 10.1001/jama.1966.03100100103030. [Article]
- ABRUZZI W: THE USE OF METHIXENE HYDROCHLORIDE TO RELIEVE FUNCTIONAL GASTROINTESTINAL DISORDERS. J New Drugs. 1965 Mar-Apr;5(2):109-13. doi: 10.1002/j.1552-4604.1965.tb00233.x. [Article]
- Clarke S, Hay GA, Vas CJ: Therapeutic action of methixene hydrochloride on Parkinsonian tremor and a description of a new tremor-recording transducer. Br J Pharmacol Chemother. 1966 Feb;26(2):345-50. doi: 10.1111/j.1476-5381.1966.tb01913.x. [Article]
- Norris JW, Vas CJ: Mehixene hydrochloride and parkinsonian tremor. Acta Neurol Scand. 1967;43(4):535-8. doi: 10.1111/j.1600-0404.1967.tb05760.x. [Article]
Drug created on June 13, 2005 13:24 / Updated on October 03, 2021 00:38