ethchlorvynol

Action and Spectrum

Actions and Spectrum: 

ethchlorvynol is a central nervous system depressant that exerts its effects by interacting with GABA receptors in the brain. GABA is an inhibitory neurotransmitter that helps regulate brain activity and promotes relaxation. ethchlorvynol is thought to enhance the inhibitory actions of GABA by binding to GABA receptors and increasing the flow of chloride ions into neurons.

This hyperpolarization of neurons dampens their activity, leading to sedation and sleepiness. ethchlorvynol was primarily used as a sedative-hypnotic medication to induce sleep and alleviate anxiety. It was used for short-term treatment of insomnia, especially in cases where other treatment options were ineffective. 

Drug Interaction

Adverse Reaction

Frequency defined 

fever, chills, or sore throat 

weakness in hands or feet 

pale skin 

double vision 

low body temperature 

overactive reflexes 

Black Box Warning

Black box warning: 

None 

Contraindication / Caution

Contraindications/caution: 

Contraindications: 

• Hypersensitivity: Individuals with known hypersensitivity or allergy to ethchlorvynol or related medications should avoid its use. 
• Respiratory Impairment: ethchlorvynol, like other sedative-hypnotics, can depress the central nervous system, including respiratory function. It may exacerbate respiratory conditions, especially those that involve impaired breathing. 
• Depression and Psychiatric Disorders: ethchlorvynol can potentially worsen symptoms of depression or other psychiatric disorders. It might interact with these conditions, leading to undesirable effects or reduced efficacy. 
• Substance Abuse or History of Addiction: Individuals with a history of substance abuse or addiction may be at higher risk for misuse or dependence on ethchlorvynol. 

Caution: 

• Depression and Mental Health Conditions: ethchlorvynol can potentially exacerbate symptoms of depression, anxiety, or other mental health conditions.  
• Respiratory Impairment: ethchlorvynol, like other sedative-hypnotics, can depress the central nervous system, including respiratory function. Individuals with respiratory conditions, such as chronic obstructive pulmonary disease (COPD), may be more susceptible to respiratory depression. 
• Concomitant Use with Other Depressants: The combined use of ethchlorvynol with other central nervous system depressants, such as alcohol, opioids, or other sedative medications, can lead to additive sedative effects and increase the risk of respiratory depression. 
• Elderly and Frail Patients: Older adults and individuals who are frail may be more sensitive to the sedative effects of ethchlorvynol, which can increase the risk of falls, fractures, and other adverse events. 
• Driving and Operating Machinery: ethchlorvynol can impair cognitive and motor skills. Individuals taking this medication should avoid activities that require mental alertness, such as driving or operating heavy machinery. 

Pregnancy / Lactation

Pregnancy consideration: Insufficient data available 

Lactation: Excretion of the drug in human breast milk is unknown 

Pregnancy category: 

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

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

Pharmacology: 

ethchlorvynol is thought to enhance the inhibitory actions of GABA by binding to GABA receptors and increasing the flow of chloride ions into neurons. This hyperpolarization of neurons dampens their activity, leading to sedation and sleepiness. 

Pharmacodynamics:  

• Central Nervous System Depression: By enhancing the effects of GABA, ethchlorvynol induces a state of central nervous system depression. This leads to various effects, including sedation, sleepiness, reduced anxiety, muscle relaxation, and an overall sense of calm. The drug’s ability to dampen neural activity contributes to its sedative and hypnotic properties. 
• Sedative and Hypnotic Effects: The increased GABAergic activity caused by ethchlorvynol leads to sedative and hypnotic effects. Sedation refers to reduced alertness and wakefulness, which can result in drowsiness and relaxation.  
• Anxiolytic Effects: ethchlorvynol’s enhancement of GABAergic activity can also have anxiolytic effects, reducing feelings of anxiety and stress. This is because GABA inhibits excitatory neurotransmission and helps balance brain activity. 

Pharmacokinetics: 

Absorption 

ethchlorvynol is well absorbed from the gastrointestinal tract after oral administration. Peak plasma concentrations are typically reached within 1 to 3 hours after ingestion. 

Distribution 

ethchlorvynol is highly lipid-soluble, allowing it to readily cross the blood-brain barrier and distribute throughout the central nervous system. It is distributed widely throughout the body, including the brain, adipose tissue, and other organs. 

Metabolism 

ethchlorvynol is extensively metabolized in the liver through oxidative processes. The primary enzyme in its metabolism is cytochrome P450 2A6 (CYP2A6). The metabolites of ethchlorvynol include inactive compounds. 

Elimination and Excretion 

The elimination half-life of ethchlorvynol is relatively long, ranging from approximately 8 to 24 hours. It is primarily excreted in the urine as metabolites. 

Adminstartion

Administration: 

Oral administration 

ethchlorvynol was taken orally with water. Taking the medication shortly before bedtime was usually recommended due to its soothing and hypnotic effects. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: ethchlorvynol 

Why do we use ethchlorvynol? 

ethchlorvynol is a sedative-hypnotic medication historically used to treat insomnia and anxiety.  

• Insomnia: ethchlorvynol was primarily used to induce sleep in individuals with insomnia. Its sedative effects were intended to help individuals fall asleep more efficiently and improve the quality and duration of sleep. 
• Anxiety: ethchlorvynol was also sometimes used to alleviate symptoms of anxiety or restlessness. Its soothing effects could help reduce anxiety in specific individuals.