Zolpidem 

Zolpidem is a derivative of  benzodiazepines or barbiturates. Zolpidem is a sedative-hypnotic drug that has been licensed for the short-term treatment of insomnia. Unlike benzodiazepines, zolpidem doesn’t seem to have any muscle- relaxant or anti-anxiety properties. With its brief half-life and lack of an active metabolite, zolpidem doesn’t seem to exacerbate daytime tiredness or sedation. Because of this, foreign visitors who need a sleep medication when hopping time zones have come to choose zolpidem.  

• In general, zolpidem should only be used for a week or less as a short-term insomnia therapy. 

Some patients may, however, occasionally require extended usage; in these situations, close supervision is required to avoid physical or psychological dependence. Like the benzodiazepines, zolpidem may be associated with dependence and abuse and is therefore regulated as a controlled substance by federal and state laws.

• Zolpidem tartrate is a non-benzodiazepine receptor modulator primarily used in the FDA- approved short-term treatment of insomnia aimed at patients with difficulty falling asleep.
• This drug decreases the time to fall asleep (sleep latency), increases the duration of sleep, and decreases the number of awakenings during sleep in patients with temporary (transient) insomnia.

What is the mechanism of action of zolpidem?

Zolpidem, the active moiety of zolpidem tartrate, is a hypnotic substance with a chemical structure that is not related to the structure of benzodiazepines, barbiturates, pyrrolopyridine, pyrazolopyrimidines, or other drugs exerting hypnotic effects. It interacts with a GABA-BZ receptor complex and shares various pharmacological properties with the benzodiazepine class of drugs.

Subunit binding of the GABAA receptor chloride channel macromolecular complex is thought to lead to the sedative, anticonvulsant, anxiolytic, and myorelaxant drug effects of zolpidem. The main regulatory site of the GABAA receptor complex can be found on its alpha (α) subunit and is called the benzodiazepine (BZ) or omega (ω) receptor. At least three different subtypes of the (ω) receptor have been identified to this date label.

• In contrast to benzodiazepine drugs, which are found to modulate all benzodiazepine receptors subtypes in a non-selective fashion, zolpidem binds the (BZ1) receptor specifically with a potent affinity for the alpha 1/alpha 5 subunits (in vitro) Label. More recent studies suggest that zolpidem binds primarily to the alpha 1, 2, and 3 subunits of the GABA receptor 11, 12, 13, and not the alpha 5 subunit.

The (BZ1) receptor is found primarily on the lamina IV of the brain, sensorimotor cortical regions, substantia nigra (pars reticulata), cerebellum molecular layer, olfactory bulb, ventral thalamic complex, pons, inferior colliculus, and globus pallidus. 

• Specific and selective binding of zolpidem on the (BZ1) receptor is not considered absolute; however, this binding could potentially explain the relative lack of myorelaxant and anticonvulsant activity in animal studies in addition to the preservation of deep sleep (stages 3 and 4) in human studies of zolpidem at hypnotic doses.

What is the recommended dose of zolpidem?

10 mg of zolpidem is the typical dosage before bed.

•  Patients shouldn’t take more than this. 

Seniors might only need five milligrams before bed. Since zolpidem absorbs quickly, it is best to take it no later than 30 minutes before going to bed.

What is the effect of an overdose of Zolpidem?

Zolpidem overdoses are rarely lethal. Zolpidem sometimes causes mortality when taken with other CNS depressants, particularly benzodiazepines, alcohol, narcotics, and barbiturates.   

Drowsiness, confusion, somnolence, weariness, dropped coordination, clumsiness while walking (ataxia), and sluggish reflexes are some of the mild indications of zolpidem overdose.  

When taken alone, zolpidem hardly causes death. When some drugs participate in zolpidem overdose, severe symptoms such as trouble breathing, slowing heart rate, decreased blood pressure, lack of coordination, and loss of consciousness lead to coma and death. 

• Every potential overdose should be considered an emergency at the ER. The prescription bottle of the drug along with any extra drugs linked to the overdose should also be brought, as the data on the prescription label can help the treating physician estimate the quantity of pills consumed.

What are the zolpidem side effects?

Sedation and drowsiness are the most often reported, particularly in the early stages of therapy. Other common symptoms include difficulty focusing and remembering things, a dissociative or “spacey” feeling, and trouble with coordination.  

• Constipation, dizziness, change in appetite, decreased interest in sexual intercourse. Suicidal thoughts or behaviors, hyperventilation, change in consciousness, confusion, loss of memory, Seizures, and palpitations.

What are the precautions taken with zolpidem usage?

After taking a single dose of zolpidem at night, alertness and coordination may be affected the next day. While using this drug, patients should be cautious when operating machinery or performing other duties requiring attentiveness.

• Seniors may be more severely affected since it may impair their reflexes and coordination, increasing the risk of falls and injuries.

Rarely may prolonged zolpidem use result in dependency. Given its extremely low potential for misuse, it is a preferred sedative-hypnotic medication for those with a history of drug or alcohol dependence.

•  There may be minimal withdrawal symptoms if zolpidem is suddenly stopped. Headache, nausea, lack of focus, tremor, cramping in the muscles, and disorientation are some of the symptoms of withdrawal.
• Co-administration  with other central nervous system (CNS) depressants such as alcohol, opioids, and barbiturates may exacerbate these CNS effects. So quit drinking while taking the drug.  

As other sedative-hypnotics, zolpidem acts centrally as a depressant and has the ability to lower breathing. Zolpidem has a minimal impact on respiratory function in healthy people, but it can lower a patient’s “respiratory drive,” or their capacity to breathe, in those with respiratory conditions such as emphysema and chronic obstructive pulmonary disease.

• Zolpidem should only be taken when needed for sleep. Do not take more than the prescribed dose.
• Zolpidem should not be taken with or immediately after meals.
• Keep the medication in the original labeled, light-resistant container, away from heat and moisture, to avoid drug degradation by them.
•  Keep zolpidem away from your children.

What are the possible drug interactions with zolpidem?

Zolpidem is recommended as One of the rare drugs with little or no clinically relevant drug interactions is zolpidem. Alcohol should not be used by zolpidem users, though, since this combination may worsen sleepiness and sedation.

How does zolpidem affect pregnancy and lactation?

• Zolpidem is classified as pregnancy category C.

Since zolpidem hasn’t been professionally studied in expectant mothers, nothing is known about its danger during pregnancy.

•  Zolpidem had some effect on bone growth in rats and rabbits, but no teratogenic effect—that is, no congenital malformation—was shown in animal reproduction tests.
•  If at all possible, avoid using zolpidem while pregnant.

Zolpidem should not be used by lactating mothers, as it will enter breast milk and be consumed by the unborn child. Breastfeeding should not begin or should be stopped if quitting the medication is not an option.