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Etizolam | CAS No: 40054-69-1 | GMP-certified suppliers
A medication that treats generalized anxiety disorder with depression, panic disorder, and insomnia by providing anxiolytic and sedative benefits for central nervous system conditions.
Therapeutic categories
Primary indications
- Indicated for the treatment of generalized anxiety disorder with depression, panic disorder and insomnia
Product Snapshot
- Etizolam is available as oral solid dosage forms including tablets and capsules, as well as liquid solutions or drops
- It is primarily used for the management of generalized anxiety disorder with depression, panic disorder, and insomnia
- The compound is currently in the experimental stage and lacks formal regulatory approvals such as FDA or EMA clearance
Clinical Overview
Pharmacodynamically, etizolam acts as a full agonist at the benzodiazepine binding site of gamma-aminobutyric acid type A (GABA-A) receptors, potentiating GABAergic neurotransmission throughout the central nervous system. Binding occurs at receptors containing gamma 2 and alpha subunits (alpha 1, 2, 3, or 5). The sedative effects are primarily mediated via alpha-1 subunit-containing receptors, while anxiolytic effects are linked to alpha-2 and alpha-3 subunits. Etizolam exhibits 6 to 10 times greater potency than diazepam in human clinical studies. Additionally, etizolam acts as a selective antagonist at the platelet-activating factor receptor (PAFR), inhibiting PAF-induced platelet aggregation and modulating bronchoconstriction and hypotension.
Regarding absorption, distribution, metabolism, and excretion (ADME), etizolam is metabolized primarily by cytochrome P450 enzymes, including CYP3A4, CYP2C18, and CYP2C19 isoforms. This metabolism profile suggests potential for drug interactions mediated by these enzymes.
Safety considerations involve typical CNS depressant risks such as sedation, cognitive impairment, potential for dependence, and withdrawal phenomena consistent with benzodiazepine class agents. Etizolam’s unique receptor activity and clinical profile require careful evaluation in therapeutic contexts, particularly due to variable regulatory status worldwide.
From an API sourcing and quality perspective, etizolam requires stringent adherence to pharmacopeial standards relevant to benzodiazepine derivatives, including control of impurity profiles and confirmation of stereochemistry. Manufacturers should ensure compliance with Good Manufacturing Practices (GMP) and verify enzyme-mediated metabolic stability through robust analytical techniques to support formulation development and regulatory submissions.
Identification & chemistry
| Generic name | Etizolam |
|---|---|
| Molecule type | Small molecule |
| CAS | 40054-69-1 |
| UNII | A76XI0HL37 |
| DrugBank ID | DB09166 |
Pharmacology
| Summary | Etizolam is a selective full agonist at the benzodiazepine binding site of GABA-A receptors, enhancing GABAergic inhibitory transmission by facilitating chloride ion influx. It exhibits high affinity for receptors containing alpha-1, alpha-2, and alpha-3 subunits, mediating sedative and anxiolytic effects. Additionally, etizolam acts as a specific antagonist at platelet-activating factor receptors, inhibiting PAF-induced platelet aggregation and related physiological responses. |
|---|---|
| Mechanism of action | Etizolam is selectively a full agonist at GABA-A receptors to increase GABAergic transmission and enhance GABA-induced Cl- currents . It is reported to bind to the benzodiazepine binding site which is located across the interface between the alpha and gamma subunits. Benzodiazapines are reported to only bind to receptors that contain gamma 2 and alpha 1/2/3/5 subunits . Alpha-1-containing receptors mediate the sedative effects of etizolam whereas alpha-2 and alpha-3 subunit-containing receptors mediate the anxiolytic effect . Etizolam shows high potency and affinity towards GABA-A receptor with alpha 1 beta 2 gamma 2S subunit combination . By binding to the regulatory site of the receptor, etizolam potentiates GABA transmission by facilitating the opening of GABA-induced chloride channels . Etizolam is a specific antagonist at PAFR. It inhibits PAF-induced platelet aggregation by inhibiting PAF binding to the receptors located on the surface of platelets with an IC50 of 22nM . |
| Pharmacodynamics | Etizolam is a CNS depressant with anxiolytic, anticonvulsant, sedative-hypnotic and muscle relaxant effects. It acts on the benzodiazepine site of the GABA-A receptor as an agonist to increase inhibitory GABAergic transmission throughout the central nervous system. Studies indicate that etizolam mediates its pharmacological actions with 6 to 10 times more potency than that of diazepam. Clinical human studies performed in Italy showed clinical effectiveness of etizolam in relieving symptoms in patients with generalized anxiety disorders with depressive symptoms [A19772, A19773, A19774]. Etizolam also mediates imipramine-like neuropharmacological and behavioral effects, as well as minor effects on cognitive functioning. It is shown to substitute the actions of a short-acting barbiturate, pentobarbitol, in a drug discrimination study . Etizolam is an antagonist at platelet-activating-factor (PAF) receptor and attenuates the recurrence of chronic subdural hematoma after neurosurgery in clinical studies . It is shown to inhibit PAF-induced bronchoconstriction and hypotension . |
Targets
| Target | Organism | Actions |
|---|---|---|
| GABA(A) Receptor | Humans | positive allosteric modulator |
| GABA(A) Receptor Benzodiazepine Binding Site | Humans | ligand |
| Platelet-activating factor receptor | Humans | antagonist |
ADME / PK
| Absorption | Etizolam is well absorbed from the intestines with a biological bioavailability of 93% following oral administration. After a single oral dosing of 0.5mg etizolam, it takes approximately 0.9 hours to reach the peak plasma concentration of 8.3 ng/mL . |
|---|---|
| Half-life | The average elimination half life of etizolam following a single oral dose of 0.5mg is 3.4 hours but may be increased up to 17 hours depending on the rate of metabolism . The main metabolite α-hydroxyetizolam displays a longer elimination half life of 8.2 hours . |
| Metabolism | Biotransformation of etizolam is extensive and involves hydroxylation and conjugation . The main metabolite formed via 1'-hydroxylation is α-hydroxyetizolam which retains pharmacological activity comparable to that of the parent drug, indicating that the action of metabolites may contribute to the clinical effects of etizolam . CYP3A4 is predicted to be the main CYP enzyme responsible for mediating etizolam metabolism. CYP2C18 and CYP2C19 are also involved in the metabolic pathways [L884, A19775]. |
| Route of elimination | In a rat study, the amounts of etizolam excreted was 30% in urine was 70% in feces, while the values in a mouse study were 40% in urine and 60% in feces . |
| Volume of distribution | Apparent distribution volume was 0.9 ± 0.2 L/kg following a single oral doing of 0.5mg etizolam . |
Formulation & handling
- Etizolam is a small molecule intended for oral administration, primarily available as tablets, capsules, and oral solutions.
- The compound exhibits low water solubility and moderate lipophilicity (LogP 4.06), which may influence formulation strategies for bioavailability optimization.
- No specific peptide or biologic characteristics apply; standard chemical stability and handling protocols for small molecules should be observed.
Regulatory status
Safety
| Toxicity | Major adverse effects include drowsiness, sedation, muscle weakness and incoordination, fainting, headache, confusion, depression, slurred speech, visual disturbances and changes in libido and tremor . Flumazenil is a competitive antagonist of GABA-A receptors and can be also used to reverse the effect of etizolam overdosage. Etizolam demonstrates no effects on fertility, development and teratogenicity . LD50 values of etizolam when delivered orally, intraperitoneally, and subcutaneously are 3509mg/kg, 825mg/kg, and >5000mg/kg in rats, respectively, and 3070mg/kg, 783mg/kg and 5000mg/kg in mice, respectively [MSDS]. |
|---|
- Etizolam exposure may result in central nervous system effects including sedation, muscle weakness, and incoordination
- Use caution to prevent accidental ingestion or inhalation due to potential for drowsiness and neurological impairment
- Flumazenil can be utilized as an antagonist in case of overdose
Etizolam is a type of Hypnotics and sedatives
Hypnotics and sedatives belong to the pharmaceutical API category that plays a crucial role in the field of medicine. These compounds are specifically designed to induce sleep, reduce anxiety, and promote relaxation in patients. With their sedative properties, hypnotics and sedatives are commonly prescribed to treat sleep disorders, insomnia, and certain psychiatric conditions.
Pharmaceutical companies produce hypnotics and sedatives as active pharmaceutical ingredients (APIs), which are the key components responsible for the desired therapeutic effects. These APIs are carefully synthesized and formulated to ensure optimal efficacy and safety in patients. Common examples of hypnotics and sedatives include benzodiazepines, barbiturates, and non-benzodiazepine sedative-hypnotics.
The development of hypnotics and sedatives involves rigorous research and testing to ensure their effectiveness and minimize potential side effects. These APIs work by targeting specific receptors in the central nervous system (CNS), such as GABA receptors, which help regulate neuronal activity and promote sedation. By modulating these receptors, hypnotics and sedatives can produce a calming effect, induce sleep, and alleviate symptoms of anxiety and restlessness.
It is important to note that the use of hypnotics and sedatives should be carefully monitored by healthcare professionals, as they can have potential side effects, such as drowsiness, impaired coordination, and dependence. Additionally, these medications may interact with other drugs, necessitating caution and proper dosage adjustments.
In summary, hypnotics and sedatives are a vital category of pharmaceutical APIs used to promote sleep, reduce anxiety, and induce relaxation. Their precise mechanisms of action on the CNS receptors contribute to their therapeutic effects, making them valuable tools in managing sleep disorders and certain psychiatric conditions.
