You are currently viewing Zolpidem: Side effects, MOA, Uses, Contraindications
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Overview of Zolpidem

Zolpidem is a non-benzodiazepine sedative and hypnotic drug but mainly produces hypnotic effect-decreases sleep latency & duration of sleep time increases in insomnia. It is classified as an imidazopyridine.

Mechanism of action

The non-benzodiazepine hypnotics bind selectively to BZD binding site on GABAa receptors and facilitate GABA-mediated neuronal inhibition ( due to enhance membrane hyperpolarization)  and finally produce CNS depression.

zolpidem

Adverse effect

  • Atypical thinking & behavior
  • Hallucination
  • Nightmare
  • Somnolence
  • Somnambulism
  • Headache
  • Nausea
  • Vomiting
  • Dizziness
  • Vertigo
  • Drowsiness
  • Asthenia
  • Ataxia
  • Rebound insomnia
  • Amnesia (memory loss)
  • GI disturbance (diarrhea)
  • Upper and lower respiratory tract infection
  • Fatigue
  • Visual disturbance
  • Increased ALT serum concentrations
  • Abnormal liver function test
  • Hepatitis
  • Anaphylactic reactions
  • Angioedema
  • Sleep-driving

Uses of zolpidem

  • Short-term management of insomnia
    • In adults: as immediate release tab: 5-10 mg immediately before bedtime. Maximum 10 mg/day. The maximum duration of time is 4 weeks including tapering
    • In elderly: as immediate release tab: 5 mg immediately before bedtime. The maximum duration of time is 4 weeks including tapering
  • Renal impairment: 5 mg immediately before bedtime.
  • Hepatic impairment (mild to moderate): 5 mg immediately before bedtime.
  • Sedative and hypnotic

Pharmacokinetics

  • Absorption: Rapidly absorbed from the GI tract when a drug is taken orally.
  • Distribution: widely distributed and enters the breast milk, the protein binding capacity ranges from 45% to 80%.
  • Metabolism: Extensively hepatic; converted to less active N-oxide and inactive N-desmethylzolpidem. Undergoes decarboxylation to inactive metabolites. The plasma half-life is around 2 hours and has a short duration of action.
  • Excretion: urine, feces (as unchanged drug and metabolites), and lungs and saliva have a little role for excretion.

Contraindications

  • Severe hepatic impairment
  • Myasthenia gravis
  • Respiratory failure
  • Severe sleep apnea syndrome
  • Pregnancy and lactation

Interaction of Zolpidem

  • Flumazenil reverses the sedative and hypnotic effects of zolpidem
  • Increased depressant effects with CNS depressants agents such as sedatives, alcohol, antihistamines.
  • Additive effect on decreased alertness & psychomotor performance with drugs imipramine and chlorpromazine.
  • Increased plasma concentration with itraconazole, ketoconazole & other CYP3A4 inhibitors.
  • May decrease plasma concentration with CYP3A4 inducers e.g. carbamazepine.
  • Reduced hypnotic effects with Rifampicin
  • Increased risk of prolonged sedation and respiratory depression with ritonavir.

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