Etizolam

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Etizolam is a benzodiazepine analog indicated for the treatment of insomnia, anxiety or panic attacks. It has an anxiolytic action about 6 times greater than that of diazepam

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[edit] BRAND NAMES

[edit] STRUCTURE

Etizolam.jpg

[edit] MECHANISM OF ACTION

Etizolam, like other Benzodiazepines bind to specific sites on the gamma-aminobutyric acid-A (GABAA) receptors. This enhances the effects of GABA by increasing its affinity for the GABAA receptor.

Activation of the GABAA receptor, which is linked to a chloride channel (Cl-), results in an influx of Cl- into the neurone causing hyperpolarisation, which results in inhibitory effects on the central nervous system.

Benzodiazepines action on GABAA receptors appears to produce their anxiolytic, sedative, muscle relaxant, hypnotic and anticonvulsant actions.

Etizolam has an anxiolytic action about 6 times greater than that of diazepam. Etizolam produces, especially at higher dosages, a reduction in time taken to fall asleep, an increase in total sleep time and a reduction in the number of awakenings.

In men, peak time is at 3.2 hours, and half-life is about 6.2 hours. So it can be classified as a short-medium action bendodiazepine.

[edit] INDICATIONS

  • Short-term treatment of insomnia
  • Short-term treatment of anxiety or panic attacks, if a benzodiazepine is required

[edit] DOSAGE

  • For anxiety: 0,25-0,50 mg two or three times per day (maximum 2 mg per day)
  • For insomnia: 1 or 2 mg before bedtime

[edit] CONTRAINDICATIONS

  • Hypersensitivity to Etizolam or to any drug in the benzodiazepine class
  • Patients with acute narrow angle glaucoma.
  • Severe liver failure
  • Pregnancy and lactation
  • Myasthenia gravis (Etizolam could increase the muscle weakness)
  • Severe respiratory failure or sleep apnea syndrome

[edit] WARNINGS AND PRECAUTIONS

  • Do not drive or do other dangerous activities after taking Etizolam until you feel fully awake.
  • Avoid drinking alcohol
  • Respiratory depression may occur in benzodiazepine overdose
  • Use of benzodiazepines can lead to dependence. This risk increases with dose and duration of treatment and in patients with a history of alcohol or drug abuse.
  • Withdrawal symptoms like convulsions, tremor, abdominal and muscle cramps, vomiting, sweating, appetite decrease, weight loss, anxiety and insomnia were seen during benzodiazepines discontinuation. Etizolam should be reduced or discontinued gradually

[edit] INTERACTIONS

  • Benzodiazepines, including Etizolam, produce additive CNS depressant effects when co-administered with other medications which themselves produce CNS depression (e.g. barbiturates, alcohol, sedatives, tricyclic antidepressants, antipsychotics, skeletal muscle relaxants, antihistamines or narcotic analgesics and anaesthetics).

[edit] PREGNANCY AND LACTATION

  • Benzodiazepines can potentially cause fetal harm when administered to pregnant women. If Etizolam is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus. Because of experience with other members of the benzodiazepine class, Etizolam is assumed to be capable of causing an increased risk of congenital abnormalities when administered to a pregnant woman during the first trimester. Because use of these drugs is rarely a matter of urgency, their use during the first trimester should almost always be avoided.
  • Nursing mothers: Benzodiazepines are known to be excreted in human milk. It should be assumed that Etizolam is as well. Chronic administration of diazepam to nursing mothers has been reported to cause their infants to become lethargic and to lose weight. As a general rule, nursing should not be undertaken by mothers who must use Etizolam.

[edit] SIDE EFFECTS

Possible side effects include: drowsiness, fatigue and ataxia (lack of voluntary coordination of muscle movements)

[edit] RELATED LINKS

[edit] REFERENCES

Sedatives / Hypnotics / Anxiolytics
Benzodiazepines Benzodiazepines (Anxiolytics)‎ Alprazolam (Xanax)   Bromazepam (Lexotan, Lexotanil)   Chlordiazepoxide (Librium)   Clobazam (Frisium)   Clorazepate (Tranxene)   Clotiazepam (Rizen, Tienor)   Delorazepam (EN)   Diazepam (Valium)   Etizolam (Depas)   Ketazolam   Lorazepam (Ativan, Control, Lorans, Tavor, Temesta)   Lormetazepam (Noctamid)   Nordazepam (Nordaz)   Oxazepam (Serepax)   Prazepam (Demetrin, Lysanxia)
Benzodiazepines (Hypnotics) Brotizolam (Lendormin, Bondormin, Dormex, Sintonal, Noctilan)   Clobazam (Frisium)   Estazolam (Esilgan, ProSom)   Etizolam (Depas, Pasaden, Etilaam, Etizest)   Flunitrazepam (Rohypnol)   Flurazepam (Dalmadorm, Dalmane, Felison, Flunox, Valdorm)   Ketazolam (Anseren, Anxon)   Lorazepam (Ativan, Control, Lorans, Tavor, Temesta)   Lormetazepam (Loramet, Minias, Noctamid, Pronoctan, Evamyl)   Midazolam (Dormicum, Hypnovel)   Nitrazepam (Mogadon, Nitrados, Numbon, Radedorm, Alodorm)   Nordazepam (Madar, Nordaz, Stilny, Tranxilium N)   Temazepam (Normison, Restoril, Tenox, Temaze)   Triazolam (Halcion, Hypam, Rilamir)
Non-Benzodiazepine Hypnotics Eszopiclone (Lunesta)   Zolpidem (Ambien, Stilnox, Hypnogen, Sanval, Stilnoct, Zoldem, Zolsana)   Zopiclone (Imovane, Zimovane)
Melatonin agonists Melatonin (Circadin)   Ramelteon (Rozerem)
Orexin agonists Suvorexant (Belsomra)