Health Encyclopedia

Ethinamate

Ethinamate: Uses, Side Effects, and Safety Information

Ethinamate, a short-acting carbamate-derivative sedative-hypnotic medication, was historically used for the short-term treatment of insomnia. This comprehensive guide covers various aspects of Ethinamate, including its chemical properties, medical uses, side effects, safety considerations, and historical background.

1. Introduction to Ethinamate

Ethinamate (IUPAC name: 1-Ethynylcyclohexanol carbamate) is a sedative-hypnotic drug that was primarily used for the short-term relief of insomnia. It belongs to the class of carbamate-derivative compounds and exhibits sedative and hypnotic properties. Ethinamate was introduced in the 1950s and was marketed under various brand names, including Valamin and Valmid.

2. Chemical Composition and Structure

Ethinamate has the molecular formula C9H13NO2 and a molecular weight of 167.2050 g/mol. Its structural formula is represented as follows:

<a href=Ethinamate Structure”>

The International Chemical Identifier (InChI) for Ethinamate is 1S/C9H13NO2/c1-2-6-3-4-8(11)10-9(12)7-5-6/h6-7H,3-5H2,1H3/t6-,7 /m0/s1.

Sources: Ethinamate“>PubChem, DrugBank

3. Brand Names and Synonyms

Ethinamate was marketed under various brand names, including Valamin and Valmid. Other synonyms for Ethinamate include:

Source: DrugBank

4. Pharmacological Classification

Ethinamate belongs to the class of carbamate-derivative sedative-hypnotic drugs. It is a short-acting sedative-hypnotic agent that was used for the short-term treatment of insomnia.

Sources: ScienceDirect, Ethinamate“>PubChem

5. Medical Uses

The primary medical use of Ethinamate was for the short-term treatment of insomnia. Its sedative-hypnotic properties helped induce sleep and promote restful sleep in patients suffering from insomnia. However, it was generally not recommended for long-term use due to the potential for drug tolerance and dependence.

Source: ScienceDirect

6. Mechanism of Action

Ethinamate exerts its sedative-hypnotic effects by interacting with the central nervous system (CNS). It is believed to enhance the inhibitory effects of gamma-aminobutyric acid (GABA), a neurotransmitter that plays a crucial role in regulating sleep and promoting relaxation. Ethinamate may also modulate the activity of other neurotransmitters involved in sleep-wake cycles.

Source: DrugBank

7. Administration and Dosage

Ethinamate was typically administered orally in the form of tablets or capsules. The recommended dosage for the treatment of insomnia varied depending on the individual patient’s age, weight, and the severity of their condition. Typical dosages ranged from 0.25 to 0.5 grams, taken before bedtime.

Source: ScienceDirect

8. Pharmacokinetics

Ethinamate is rapidly absorbed from the gastrointestinal tract after oral administration. It undergoes extensive metabolism in the liver, primarily through hydrolysis and oxidation processes. The metabolites are then excreted through the urine and feces. Ethinamate has a relatively short elimination half-life, contributing to its short-acting nature.

Source: Ethinamate#section=Metabolism–Metabolites”>PubChem

9. Side Effects and Adverse Reactions

Common side effects associated with Ethinamate include drowsiness, dizziness, headache, nausea, and confusion. More severe side effects may include respiratory depression, allergic reactions, and changes in blood pressure. Prolonged use of Ethinamate can lead to drug tolerance and potentially physical and psychological dependence.

Source: DrugBank

10. Contraindications and Precautions

Ethinamate should not be used in patients with known hypersensitivity or allergies to the drug or its components. It is also contraindicated in patients with severe respiratory disorders, such as chronic obstructive pulmonary disease (COPD) or sleep apnea, as it may further depress respiratory function. Caution should be exercised when administering Ethinamate to elderly patients or those with liver or kidney impairment, as dosage adjustments may be necessary.

Source: Ethinamate#section=Safety-and-Hazards”>PubChem

11. Drug Interactions

Ethinamate may interact with other central nervous system (CNS) depressants, such as alcohol, opioids, and sedatives, potentiating their effects and increasing the risk of respiratory depression. Concurrent use of Ethinamate with other sedative-hypnotic drugs or alcohol should be avoided due to the potential for cross-tolerance and additive effects.

Source: DrugBank

12. Regulatory and Safety Information

Ethinamate was patented in the United States and other countries in the mid-20th century. However, due to the availability of safer and more effective alternatives, it has been largely replaced and is no longer widely used or manufactured. Safety guidelines and restrictions may vary depending on the region and regulatory authorities.

Source: Google Patents

13. Historical Background

Ethinamate was first synthesized in the early 1950s and was introduced as a sedative-hypnotic medication for the treatment of insomnia. It gained popularity as a short-acting alternative to barbiturates, which were associated with a higher risk of overdose and dependence. However, with the development of safer and more effective medications, such as benzodiazepines, Ethinamate gradually fell out of favor and was eventually discontinued in many countries.

Source: ScienceDirect

14. Comparative Medication

Ethinamate was a member of the carbamate-derivative sedative-hypnotic class, which also included drugs like meprobamate and carisoprodol. These compounds were developed as alternatives to barbiturates, offering a shorter duration of action and potentially lower risk of dependence. However, they were eventually replaced by benzodiazepines, such as diazepam and alprazolam, which demonstrated improved safety and efficacy profiles for the treatment of insomnia and anxiety disorders.

Source: Ethinamate#section=Therapeutic-Uses”>PubChem

15. Clinical Studies and Research

Ethinamate was the subject of several clinical studies and research investigations during its development and use as a sedative-hypnotic medication. These studies evaluated its efficacy, safety, and pharmacokinetic properties in various patient populations. However, due to the availability of newer and safer alternatives, research on Ethinamate has largely been discontinued in recent decades.

Source: ScienceDirect

16. Ethinamate in Literature

Ethinamate has been mentioned in various medical and scientific literature, particularly in publications related to sedative-hypnotic medications, insomnia treatments, and drug development in the mid-20th century. However, due to its limited use and discontinuation, references to Ethinamate in contemporary literature are relatively scarce.

Source: PubMed

17. Testing and Laboratory Analysis

Laboratory testing for Ethinamate may be performed using analytical techniques such as gas chromatography-mass spectrometry (GC- MS) or liquid chromatography-mass spectrometry (LC- MS). These methods can detect and quantify Ethinamate and its metabolites in biological samples, such as blood, urine, or hair. However, due to the limited availability and use of Ethinamate, testing services and procedures may vary depending on the region and specific laboratory capabilities.

Source: ScienceDirect

18. FAQs and Common Queries

Here are some frequently asked questions and common queries related to Ethinamate:

19. Additional Resources

For further information and resources related to Ethinamate, you can refer to the following databases and websites:

20. Glossary and Definitions

Here are definitions of some key terms related to Ethinamate: