Zaleplon

Zaleplon is a sedative-hypnotic drug that was licensed for the short-term treatment of insomnia and is unrelated to barbiturates or benzodiazepines. At the suggested hypnotic dosages, zaleplon does not seem to have any muscle relaxant or antianxiety effects, in contrast to the benzodiazepines. Zaleplon does not seem to produce much sedation or sleepiness throughout the day and has a brief duration of action. It also doesn’t contain any active metabolites; therefore, Zaleplon has become a favorite among foreign visitors who need a sleep aid when hopping time zones. Zaleplon is generally recommended to treat insomnia for a maximum of one week, although certain individuals may occasionally require extended usage; in these situations, close observation is required to avoid physical or psychological dependence.

What is the mechanism of action of Zaleplon?

Zaleplon exerts its action through subunit modulation of the GABABZ receptor chloride channel macromolecular complex. Zaleplon also binds selectively to the brain omega-1 receptor located on the alpha subunit of the GABA-A/chloride ion channel receptor complex and potentiates t-butyl-bicyclophosphorothionate (TBPS) binding. 

While Zaleplon is a hypnotic agent with a chemical structure unrelated to benzodiazepines, barbiturates, or other drugs with known hypnotic properties, it interacts with the gamma-aminobutyric acid-benzodiazepine (GABABZ) receptor complex. Subunit modulation of the GABABZ receptor chloride channel macromolecular complex is hypothesized to be responsible for some of the pharmacological properties of benzodiazepines, which include sedative, anxiolytic, muscle relaxant, and anticonvulsive effects in animal models. Zaleplon also binds selectively to the CNS GABAA-receptor chloride ionophore complex at benzodiazepine (BZ) omega-1 (BZ1, ο1) receptors.

What is the recommended dose of Zaleplon?

The usual starting dose of zaleplon is 10 mg at bedtime, and it is rarely necessary to go beyond this amount.

• Maximum dose: 20 mg/day
• Seniors may require only 5 mg at bedtime. Zaleplon is rapidly absorbed and should be taken within 30 minutes before bedtime.
• Doses should be individualized.
• Efficacy was established in trials ranging from a single night to five weeks.

What happens when you take an overdose of Zaleplon?

If you develop any unusual or strange thoughts or behaviors while using Zaleplon, be sure to discuss them with your doctor. Some changes that have occurred in people using this medicine are like those seen in people who drink alcohol and then act in a manner that is not normal. Other changes may be more unusual and extreme, such as confusion, hallucinations (seeing, hearing, smelling, or feeling things that are not there), and unusual excitement, nervousness, or irritability.

Every potential overdose of Zaleplon 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 side effects associated with Zaleplon administration?

Memory impairment, sleepiness, and sedation are the most often reported adverse effects of zaleplon. Zaleplon is unlikely to cause daytime sedation or sleepiness due to its short half-life. A sense of dissociation (being “spacey”), memory loss, and poor coordination are other sporadic symptoms.

Symptoms like anxiety, blurred or double vision, chest pain, confusion about identity, place, and time, Discouragement, false or unusual sense of well-being, fast, irregular, pounding, or racing heartbeat or pulse, feeling sad or empty, Fever, general feeling of discomfort or illness, hives, skin rash, irritability, lack of appetite, lightheadedness, loss of interest or pleasure, not feeling like oneself, shakiness, and unsteady walk, tightness in the chest, trouble concentrating, trouble sleeping, trouble breathing, unsteadiness, trembling, or other problems with muscle control or coordination, and unusual weakness or tiredness.

What are the precautions taken when Zaleplon is taken?

Zaleplon may cause serious allergic reactions, including anaphylaxis and angioedema, which can be life-threatening and require immediate medical attention. Call your doctor right away if you have a rash, itching, hives, trouble breathing or swallowing, or any swelling of your hands, face, mouth, or throat while you are using this medicine.

Zaleplon will add to the effects of alcohol and other central nervous system (CNS) depressants (medicines that make you drowsy or less alert). Some examples of CNS depressants are antihistamines or medicine for hay fever, other allergies or colds, sedatives, tranquilizers, or sleeping medicines, prescription pain medicine or narcotics, medicine for seizures or barbiturates, muscle relaxants, or anesthetics, including some dental anesthetics. Check with your doctor before taking any of the above while you are using this medicine.

• Do not drive or do anything else that could be dangerous until you know how this medicine affects you.

This medicine may cause you to do things while you are still asleep that you may not remember the next morning. It is possible you could drive a car, sleepwalk, have sex, make phone calls, or prepare and eat food while you are asleep or not fully awake. Tell your doctor right away if you learn that any of these have happened.

Do not change your dose or stop using it without first checking with your doctor. Your doctor may want you to gradually reduce the amount you are using before stopping completely. Stopping this medicine suddenly may cause withdrawal side effects.

• After taking zaleplon for insomnia, you may have difficulty sleeping (rebound insomnia) for the first few nights after you stop taking it.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements.

• Zaleplon should be taken only when needed for sleep. Do not take more than the prescribed dose.
• If you miss a dose of this medicine, skip the missed dose and go back to your regular dosing schedule.
•  Do not take double doses.
• Use this medicine only when you cannot sleep. You do not need to keep a schedule for taking it.
• Store the medication in its originally labeled, light-resistant container, away from heat and moisture. 
• Heat and moisture may precipitate the breakdown of your medication, and the medication may lose its therapeutic effects.

• Keep your medication out of the reach of children.

What is the effect of Zaleplon on pregnancy and lactation?

• Zaleplon in pregnancy category C.

Since zaleplon hasn’t been professionally studied in pregnant mothers, nothing is known about the danger during pregnancy. Studies on animal reproduction have shown that zaleplon influences the formation of bones. It is not recommended to use zaleplon when pregnant. Zaleplon should not be given to nursing moms since it will enter their breast milk and be consumed by the unborn child. Nursing mothers should not begin or should be stopped if quitting the medication is not an option.

What are the possible drug interactions with Zaleplon?

Zaleplon is one of those few medications that has few or no clinically significant drug interactions. However, patients taking zaleplon should not consume alcohol because the combination may increase sedation and drowsiness.

Some medications can affect how zaleplon is metabolized (broken down). This can lead to increased side effects or make zaleplon less effective in some cases. Examples include carbamazepine (Tegretol), rifampin, and cimetidine (Tagamet HB).