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Description

Etizest (etizolam buy)

Commercial Name: Etizest
Principal Ingredient: Etizolam
Utilization: Sedative power and anti-anxiety effects
Available Dosage: 1mg
Category: Anti-Anxiety

Etizest (etizolam buy) In The Treatment Of Anxiety And Depressive Disorders

Introduction

Anxiety is a broad term used to define disorders that cause nervousness, fear, apprehension, and worry. It can lead to insomnia or lack of sleep. This article provides valuable information on the use of etizolam as an effective anxiolytic for the treatment of anxiety and insomnia.

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WHAT IS Etizest (etizolam buy)?

This drug is similar to benzodiazepine category of anxiolytics.

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Did you know?

This drug is generally given along with Escitalopram to treat major depressive disorders, social anxiety disorders,  disorders, depression, and panic disorders. It can also be used to treat psycho-somatic illnesses such as a headache, irritable bowel syndrome, and hypertension.

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What Is Etizest (etizolam buy) Prescribed For

This drug is primarily used for treating anxiety and also for the short-term management of insomnia. Apart from stress, it has also been used to treat

  • Cervical spondylosis
  • Lumbar disease
  • Cancer pain.
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Is Etizest (etizolam buy) safe to use?

Yes. Etizolam is considered safe to use. Although the use of this drug can cause mild side effects including

  • Drowsiness
  • Sleepiness
  • Muscle weakness
  • Vertigo
  • Headache
  • Confusion
  • Slurred speech
  • Change in libido
  • Uncontrolled shaking of arms or legs
  • Visual disturbances
  • Urinary retention/incontinence
  • Stomach discomfort and pain
  • Excessive salivation
  • Memory problems

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What are the lists of conditions in which this drug should not be employed?

People suffering from myasthenia gravis, narrow-angle glaucoma, pulmonary insufficiency, liver disease, porphyria or allergy should not take this drug.

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Can Etizolam be used during pregnancy and breastfeeding?

No.  This drug should not be used during pregnancy and breastfeeding. In case you become pregnant during treatment make sure you stop using this drug at the earliest or consult your practitioner for any other safer alternative therapy.

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Can Etizolam be taken on an empty stomach?

Etizolam can be taken with food or without food. Generally, it is required that you use this drug within 15 to 30 minutes following your meal.

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How do you use Etizolam?

Age, medical condition, and response to therapy determine the dosage of this drug. This drug is rapidly absorbed orally and should be swallowed wholly at a time. Make sure you don’t crush, chew or break the drug. Administer it with plenty of fluids. For best results take this drug at the fixed time as advised by your practitioner, at evenly spaced intervals to help maintain a specific dose of this medicine in the body.

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How to use Etizolam?

Make sure you follow the dosage prescribed by your physician. A dose of 0.25mg-0.5mg is generally prescribed for adults once to thrice daily. For panic attack and related disorders, 0.5 mg/twice/daily is the preferred dosage. Doses higher than 3 mg should not be employed. This drug is generally prescribed for a maximum duration of 12 weeks.

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Under which conditions should Etizolam not be taken?

It should be used with extreme caution in people suffering from depression, chronic psychoses, and phobias as it tends to cause suicidal thoughts, inclinations, personality disorders or organic brain syndrome. Use of this drug was also found to cause drowsiness, impairment of ideas, confusion, and perception. It is required that activities requiring mental alertness not be performed while taking this drug. Furthermore, this drug caused changes in the blood pressure by either lowering it or increasing it. Henceforth it is required that people having high blood pressure should use this drug with caution.

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Can Etizolam be stopped suddenly?

Convolutions, behavioral disorder, and tremor or anxiety are the possible adverse effects that can occur on the sudden withdrawal of the drug. In case you want to stop taking this medicine do it gradually over a period to avoid withdrawal symptoms.

What should be done in case of an overdose?

In case of an overdose, you need to contact your doctor immediately.

What are the drugs that can interact with Etizolam?

This drug was found to interact with CNS depressant, sedatives, sedating anti-histamines, anti-depressant, disulfiram, antipsychotics, cisapride, clozapine, opioid analgesics, cimetidine, diazoxide, muscle relaxants, proton-pump inhibitors, ACE II inhibitors, anti-epileptics,beta-blockers, and sodium nitroprusside.

Conclusion

Etizolam is the safest drug to treat anxiety and insomnia with very minimal adverse effects.

Safety Measures

  • Do not use this drug only based on the pharmacist’s advice, as it could worsen or lead to more complications.
  • Don’t risk your health with self-medication. Always take a doctor’s advice.
  • Do not stop the medication prescribed by your doctor all of a sudden.
  • Unless the doctor prescribes, do not break your drug schedule.
  • If you skip a dose, take it the next day at the same time.  Do not take a double dose.
  • Store the drug at a temperature below 35 degrees, away from light and moisture. Keep children and pets should be kept away from the drug.

Disclaimer

We hope we have been able to answer most of the common queries related to Etizolam, but if you have any significant queries and side effects, please do consult our panel of doctors. There can be further changes/updates regarding the drug based on future research.

References

  1. Casacchia M, Bolino F, Ecari U. Etizolam in the treatment of generalized anxiety disorder: a double-blind study versus placebo. Current medical research and opinion. 1990 Jan 1;12(4):215-23.
  2. De Candia MP, Di Sciascio G, Durbano F, Mencacci C, Rubiera M, Aguglia E, Garavini A, Bersani G, Di Sotto A, Placidi G, Cesana BM. Effects of treatment with etizolam 0.5 mg BID on cognitive performance: a 3-week, multicenter, randomized, double-blind, placebo-controlled, two-treatment, three-period, noninferiority crossover study in patients with anxiety disorder. Clinical therapeutics. 2009 Dec 1;31(12):2851-9.

Description

Etizolam is a thienodiazepine which is chemically related to benzodiazepine (BDZ) drug class; it differs from BDZs in having a benzene ring replaced with a thiophene ring. It is an agonist at GABA-A receptors and possesses amnesic, anxiolytic, anticonvulsant, hypnotic, sedative and skeletal muscle relaxant properties. Initially introduced in 1983 in Japan as treatment for neurological conditions such as anxiety and sleep disorders, etizolam is marketed in Japan, Italy and India. It is not approved for use by FDA in the US; however it remains unscheduled in several states and is legal for research purposes.

Type
Small Molecule
Groups
Experimental
Structure
Thumb
Weight
Average: 342.846
Monoisotopic: 342.070594897
Chemical Formula
C17H15ClN4S
Synonyms
  • 4-(o-Chlorophenyl)-2-ethyl-9-methyl-6H-thieno(3,2-f)-s-triazolo(4,3-a)(1,4)diazepine

PHARMACOLOGY

Indication
Indicated for the treatment of generalized anxiety disorder with depression, panic disorder and insomnia.
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
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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 2,3,4. 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 8. Etizolam is an antagonist at platelet-activating-factor (PAF) receptor and attenuates the recurrence of chronic subdural hematoma after neurosurgery in clinical studies 9. It is shown to inhibit PAF-induced bronchoconstriction and hypotension 5.
Mechanism of action
Etizolam is selectively a full agonist at GABA-A receptors to increase GABAergic transmission and enhance GABA-induced Cl- currents 1. 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 7. Alpha-1-containing receptors mediate the sedative effects of etizolam whereas alpha-2 and alpha-3 subunit-containing receptors mediate the anxiolytic effect 7. Etizolam shows high potency and affinity towards GABA-A receptor with alpha 1 beta 2 gamma 2S subunit combination 1. By binding to the regulatory site of the receptor, etizolam potentiates GABA transmission by facilitating the opening of GABA-induced chloride channels 7. 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 5.

TARGET ACTIONS ORGANISM
UPlatelet-activating factor receptor
antagonist
Humans
AGABA(A) Receptor
positive allosteric modulator
Humans
AGABA(A) Receptor Benzodiazepine Binding Site
ligand
Humans
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 9.
Volume of distribution
Apparent distribution volume was 0.9 ± 0.2 L/kg following a single oral doing of 0.5mg etizolam 9.
Protein binding
Not Available
Metabolism
Biotransformation of etizolam is extensive and involves hydroxylation and conjugation 9. 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 6. CYP3A4 is predicted to be the main CYP enzyme responsible for mediating etizolam metabolism. CYP2C18 and CYP2C19 are also involved in the metabolic pathways 9,5.

Hover over products below to view reaction partners

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 9.
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 9. The main metabolite α-hydroxyetizolam displays a longer elimination half life of 8.2 hours 6.
Clearance
Not Available
Adverse Effects
Learn about our commercial Adverse Effects data.
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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 8. 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 9. 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.
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