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Brand Name :
Tremarit, Tremaril, Methixart, Cholinfall
Synonyms :
methixen, metixene
Class :
Anticholinergic Agents Anti-parkinson drugs
Dosage forms and strengths
Tremarit Tablets
5 mg
Indicated as monotherapy treatment
As hydrochloride: At the start, take 2.5 mg orally three times a day; adjust the dose incrementally based on clinical response up to a maximum of 15 to 60 mg a day, administered in divided doses
Not indicated
Refer adult dosing
When metixene and aclidinium are combined, the risk or seriousness of adverse events will rise
When metixene and alfentanil are combined, the risk or seriousness of adverse events will rise
When metixene and amitriptyline are combined, the risk or seriousness of adverse events will rise
When metixene and amobarbital are combined, the risk or seriousness of adverse events will rise
When metixene and amoxapine are combined, the risk or seriousness of adverse events will rise
When metixene and brompheniramine are combined, the risk or seriousness of adverse events will rise
Actions and Spectrum:
metixene, a pharmacological agent categorized as an anticholinergic medication, exhibits a distinct mode of action primarily centered around its interactions with muscarinic receptors within the autonomic nervous system.
As an anticholinergic, metixene competitively antagonizes the binding of acetylcholine to muscarinic receptors, thus obstructing the subsequent cellular signaling pathways facilitated by these receptors This action results in a reduction of cholinergic neurotransmission, leading to the suppression of parasympathetic nerve impulses.
Frequency not defined
Vertigo
ataxia
constipation
fever
acute glaucoma
Dryness of the mouth
rash
headache
nausea
blurred vision
Black Box Warning:
None
Contraindication/Caution:
Hypersensitivity: metixene is contraindicated in individuals with a history of hypersensitivity or allergic reactions to the drug or its components. Immediate allergic reactions have been reported in susceptible individuals, ranging from skin to systemic manifestations.
Urinary Retention: metixene is contraindicated in patients with urinary retention or related obstructive uropathy. The medication’s anticholinergic properties can impede detrusor muscle function, exacerbating urinary retention and potentially precipitating urinary bladder complications.
Gastrointestinal Obstruction: Patients presenting with gastrointestinal obstruction, including paralytic ileus, are contraindicated from using metixene. The drug’s anticholinergic effects can exacerbate the impaired peristaltic activity, potentially aggravating the underlying condition.
Prostatic Hypertrophy: metixene should be avoided in patients with prostatic hypertrophy or other obstructive urological conditions. The medication’s anticholinergic properties can exacerbate urinary symptoms and impede urinary flow in this patient population.
Pregnancy and Lactation: The safety of metixene administration during pregnancy and lactation has not been adequately established. Hence, the use of the drug is contraindicated in pregnant and breastfeeding individuals, unless the potential benefits outweigh the risks and are determined by a qualified healthcare professional.
Pediatric Population: metixene is generally not recommended for use in pediatric patients due to limited safety and efficacy data. Its use in this population group is contraindicated except under circumstances where potential benefits are considered to significantly outweigh potential risks, as determined by a medical practitioner.
Pregnancy warnings:
Pregnancy category: C
Lactation: Excreted into human milk is unknown
Pregnancy Categories:
Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester.
Category B: There were a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.
Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.
Category N: There is no data available for the drug under this category
Pharmacology:
metixene, a pharmacological agent categorized as an anticholinergic medication.
Pharmacodynamics:
metixene exerts its pharmacological effects primarily through antagonism of various receptors within the central nervous system. It acts as an antagonist at muscarinic acetylcholine receptors, exerting an anticholinergic effect that contributes to its therapeutic applications in the management of certain neurological and neuropsychiatric disorders. Additionally, metixene possesses affinity for α-adrenergic receptors, which may contribute to its modulatory effects on sympathetic nervous system activity.
Pharmacokinetics:
Absorption
metixene exhibits favorable absorption characteristics upon administration. Its oral bioavailability is well-documented, allowing for efficient uptake through the gastrointestinal tract. The compound’s absorption is facilitated by its lipophilic nature, enabling ready passage through biological membranes.
Distribution
Following absorption, metixene demonstrates a propensity for extensive distribution within bodily tissues. Its moderate volume of distribution suggests a significant distribution beyond the plasma compartment. The compound’s affinity for binding to plasma proteins, notably albumin, can influence its distribution and therapeutic availability.
Metabolism
metixene undergoes hepatic metabolism primarily via cytochrome P450 enzymes, notably the CYP2D6 and CYP3A4 isoforms. These enzymatic transformations lead to the formation of metabolites, which may possess altered pharmacological activities compared to the parent compound. The metabolic processes primarily involve hydroxylation and subsequent conjugation reactions.
Excretion and Elimination
metixene and its metabolites are eliminated predominantly through renal excretion. The compound’s renal clearance plays a significant role in determining its overall elimination rate.
Administration:
The administration is by oral route.
Patient information leaflet
Generic Name: metixene
Why do we use metixene?
Adjunctive Treatment for Parkinson’s Disease: As part of a comprehensive therapeutic regimen, metixene serves as an adjunctive agent in the management of Parkinson’s disease. By modulating neurotransmitter imbalances in the basal ganglia, metixene contributes to the mitigation of motor impairments and helps enhance patient mobility and functionality.
Management of Allergic Rhinitis: metixene’s anticholinergic attributes position it as a therapeutic option for alleviating symptoms associated with allergic rhinitis. Through the modulation of cholinergic pathways, metixene attenuates rhinorrhea, nasal congestion, and sneezing, Thereby, improving the quality of life for individuals affected by this condition.
Adjunctive Treatment for Schizophrenia: In conjunction with primary antipsychotic agents, metixene supplements the treatment regimen for schizophrenia. Its antagonism of specific dopamine receptors aids in ameliorating certain symptoms of the disorder, contributing to a more comprehensive management strategy.