Nitrazepam

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Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Nitrazepam.jpg

[edit] MECHANISM OF ACTION

Nitrazepam, 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.

Nitrazepam is an long-acting benzodiazepine, its half-life in human plasma reported to be in the range of 18-36 hours, averaging about 24 hours and and peak concentrations in plasma occur approximately 80 minutes following administration.

[edit] INDICATIONS

Short-term treatment of insomnia, which is severe, disabling or distressing, and when sleepiness during the day is acceptable.

[edit] DOSAGE

  • The recommended dose for most adults is 5 mg to 10 mg at bedtime.
  • For the elderly, the recommended dose is 2.5 mg to 5 mg at bedtime.

Treatment should begin with low doses, gradually increasing to the optimum level. The duration of treatment should be as short as possible

[edit] CONTRAINDICATIONS

  • Hypersensitivity to Nitrazepam or to any drug in the benzodiazepine class
  • Severe liver failure
  • Pregnancy and lactation
  • Myasthenia gravis (Nitrazepam could increase the muscle weakness)
  • Severe respiratory failure
  • Sleep apnoea syndrome (a condition where you stop breathing whilst asleep)

[edit] PRECAUTIONS

  • Do not drive or do other dangerous activities after taking Nitrazepam until you feel fully awake.
  • Do not drink alcohol
  • Caution is required in patients with chronic respiratory failure (risk of respiratory depression).
  • Use of benzodiazepines can lead to dependence. This risk increases with dose and duration of treatment.
  • Nitrazepam should not be used alone in treating depression with or without anxiety since it may induce suicide or aggressive behaviour.

[edit] INTERACTIONS

Benzodiazepines, including Nitrazepam, 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

[edit] SIDE EFFECTS

Common side effects include: Dizziness, drowsiness, unsteadiness and loss of coordination. Less frequently headache, confusion, vertigo, muscular weakness, changed libido, urinary incontinence or retention, skin rashes, visual and gastrointestinal upset and tiredness may be experienced

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

http://medsafe.govt.nz/profs/Datasheet/n/Nitradostab.pdf

[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)