Zolpidem

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Zolpidem (Stilnox, Ambien) belongs to a group of medicines called hypnotics (sleep producers). These medicines work by acting on the brain to cause sedation.

Insomnia is a difficulty in falling asleep or sleeping properly.

Zolpidem may be used for short-term treatment of insomnia. Sleeping problems do not usually last long and most people only need a short course of treatment.

Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Zolpidem.jpg

[edit] MECHANISM OF ACTION

Zolpidem is an hypnotic drug with short duration of action (up to 6 hours), chemically unrelated to the benzodiazepines. Zolpidem binds with high affinity to GABAA receptors containing an alpha-1 subunit (also known as BZ1- or w1-receptor subtypes), leading to a positive allosteric modulation that increase the affinity of γ-aminobutyric acid (GABA) to GABAA receptors.

The GABAA receptor is a pentameric ligand-gated ion channel. Upon activation, it selectively conducts Cl- through its pore, resulting in hyperpolarization of the neuron which reduces cell excitability.

Zolpidem has both a rapid absorption and onset of hypnotic action if taken on an empty stomach and a short elimination half-life (2-3 hours).

[edit] INDICATIONS

Zolpidem is indicated for the short-term treatment of insomnia characterized by difficulties with sleep initiation

[edit] DOSAGE

Recommended initial dose is 5 mg for woman and 5-10 mg for men, immediately before bedtime with at least 7-8 hours remainingbefore the planed time of awakening.

Geriatric patients and patients with hepatic impairment: Recommended dose is 5 mg for men and women

The effect of zolpidem may be slowed if taken with or immediately after a meal

[edit] CONTRAINDICATIONS

  • Hypersensitivity to the drug

[edit] WARNINGS AND PRECAUTIONS

  • CNS depressant effects: Impairs alertness and motor coordination. Instruct patients on correct use.
  • Need to evaluate for co-morbid diagnosis: Reevaluate if insomnia persists after 7 to 10 days of use (this may indicate the presence of a primary psychiatric or physical disorder).
  • Severe anaphylactic/anaphylactoid reactions: Angioedema and anaphylaxis have been reported. Do not rechallenge if such reactions occur.
  • “Sleep-driving” and other complex behaviors while not fully awake. Risk increases with dose and use with other CNS depressants and alcohol. Immediately evaluate any new onset behavioral changes.
  • Depression: Worsening of depression or suicidal thinking may occur. Prescribe the least amount of tablets feasible to avoid intentional overdose.
  • Respiratory Depression: Consider this risk before prescribing in patients with compromised respiratory function
  • Withdrawal, Rebound, Dependence and Tolerance: Continuous long-term use of Zolpidem is not recommended and should not exceed four weeks. Some loss of efficacy to the hypnotic effects of sedative/hypnotic agents may develop after repeated use for a few weeks. Use of Zolpidem may lead to the development of physical and psychological dependence. The risk of dependence increases with dose and duration of treatment. Withdrawal effects: Symptoms may occur with rapid dose reduction or discontinuation especially once physical dependence has developed.
  • Memory Impairment: Zolpidem may induce anterograde amnesia. The condition occurs most often several hours after ingesting the product and therefore to reduce the risk patients should ensure that they will be able to have an uninterrupted sleep of 7-8 hours.

[edit] INTERACTIONS

  • Food reduces absorption of zolpidem and its effect may be slowed if taken with or immediately after a meal
  • Avoid alcohol
  • Zolpidem may produce additive CNS depressant effects when co-administered with sedative Antihistamines, Anticonvulsants, Narcotic analgesics, Anesthetics, or psychotropic medications such as Antipsychotics (neuroleptics), Hypnotics, Anxiolytics/sedatives, and Antidepressants which themselves can produce CNS depression.
  • CYP3A4 inhibitors (like Ketoconazole): they increase zolpidem effects. Consideration should be given to using a lower dosage of zolpidem

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category C (US)
  • Zolpidem is excreted in human milk. Caution should be exercised when it's administered to a nursing woman

[edit] SIDE EFFECTS

The most common adverse effects are daytime drowsiness, dizziness and diarrhea.

Other possible side effects include: headache, nausea, vomiting, amnesia, agitation, nightmares and fatigue.

[edit] RELATED LINKS

Zolpidem (Stilnox, Ambien) Side Effects
Zolpidem Withdrawal and Detox

[edit] BIBLIOGRAPHY

[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)