Nitroxoline (HYPNOTIC)

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Nitroxoline (HYPNOTIC)

Medically reviewed

Marina Burgos

Last updated on 10/01/2026

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Nitroxoline (HYPNOTIC)

Property Description
Active ingredient Nitrazepam
Pharmacological class Benzodiazepine / Psycholeptic
Form Tablet (Oral Ingestion)
Common purpose Relief of severe sleep disturbances
Origin Synthetic

The medicine contextually referred to as Nitroxoline (Hypnotic) is a powerful, synthetic medication whose active ingredient is Nitrazepam. This single-ingredient compound belongs to the established Benzodiazepine family, formally classified as a Psycholeptic and a general Central Nervous System (CNS) depressant. As a member of the benzodiazepine class, Nitrazepam is a derivative of 1,4-benzodiazepinone, distinguishing it from newer, non-benzodiazepine hypnotics. The compound is widely recognized across international formularies for its role in inducing and sustaining sleep.

The core composition relies exclusively on Nitrazepam, which is formulated for Oral ingestion typically as a Tablet. The primary general purpose of this medication is linked to its strong hypnotic and sedative actions, intended to manage severely disruptive sleep disturbances. For example, it is generally used for the short-term relief of severe insomnia that significantly impairs normal daily functioning. The properties of the active ingredient include the reduction of sleep latency and wakefulness after sleep onset, as the medicine is designed to assist in falling asleep and maintaining sleep stability.

The physiological action of Nitrazepam involves enhancing the effects of the brain's main inhibitory neurotransmitter, GABA (gamma-aminobutyric acid). The compound achieves this by acting as a positive allosteric modulator at the GABA-A receptor complex. This mechanism amplifies the brain’s natural calming signals, effectively slowing down nerve excitability that characterizes agitation. The resulting general outcome is a broad reduction in overall CNS activity, which is the principle behind the drug's effectiveness as a hypnotic agent and its ability to promote generalized muscle relaxation and provide relief from heightened anxiety states. This long-acting nature is a recognized attribute of the compound, differentiating it from shorter-acting alternatives.

What side effects are possible with Nitroxoline (HYPNOTIC)?

Possible side effects and safety information

The official safety profile for Nitroxoline (Hypnotic), containing the active ingredient Nitrazepam, is defined by its effects as a Central Nervous System (CNS) depressant. Adverse reactions are classified by frequency and grouped into System-Organ Classes according to regulatory standards.


Frequency-Classified Adverse Reactions

The most frequent adverse reactions are generally related to the CNS:

  • Common: Drowsiness, reduced alertness, confusion, ataxia (uncoordinated movement), muscle weakness, fatigue, dizziness, and impaired psychomotor performance. These effects are often most pronounced at the start of treatment.
  • Uncommon/Infrequent: Headaches and gastrointestinal disturbances.
  • Rare: Paradoxical reactions (e.g., aggression, excitement), depression, blood dyscrasias, and hypotension.

Serious Adverse Reactions and Safety Patterns

The regulatory label documents several clinically significant safety concerns:

  • Dependence and Withdrawal: The risk of developing physical and psychological dependence and tolerance is explicitly associated with the duration of treatment and higher doses. Abrupt cessation may lead to withdrawal syndrome.
  • Amnesia and Depression: Anterograde amnesia (inability to recall events after administration) is a dose-related phenomenon. The medication may also uncover or worsen existing depression.
  • Respiratory Risk: The potential for severe respiratory depression exists, especially when higher doses are used or when combined with other CNS depressants.

Population-Specific Safety Considerations

The safety profile includes specific statements for vulnerable groups. Older adults are more sensitive to CNS effects and face an increased risk of falls due to associated muscle weakness and ataxia. Furthermore, the medicine is contraindicated in patients with severe hepatic insufficiency, severe respiratory insufficiency, or sleep apnea syndrome.

Overdose and Emergency Response

Overdose and When to Seek Help

Overdose Profile Summary

Information regarding the specific clinical manifestations, symptom clusters, and required emergency actions for an overdose of nitroxoline, based on standardized governmental regulatory documents (such as FDA or EMA), is not readily available or explicitly detailed in the public-facing 'Overdose' sections of current labeling. Consequently, there is no official, regulator-derived guidance on what constitutes a population-specific risk or a defined severity classification for this drug.

Documented Overdose Reports

While official regulatory labeling may lack a detailed overdose section, clinical literature documents limited instances of significant overexposure. One reported case of extreme over-ingestion (5000 mg) involved the patient presenting with general fatigue but remaining alert and oriented, ultimately recovering without the need for specific medical interventions.

When to Seek Immediate Medical Help

In the event of a suspected or known overdose, the absence of specific detailed instructions in regulatory documents means that a cautious approach is necessary. Immediate medical attention is required for any ingestion exceeding the prescribed dose, particularly if the individual is experiencing symptoms such as severe or persistent nausea, vomiting, confusion, difficulty breathing, or profound changes in mental status. Contacting emergency services or a poison control center is the required first step for guidance in any potential overdose situation.

Therapeutic Uses of Nitroxoline (HYPNOTIC)

Targeting the Discomfort of Acute Urinary Infections

Nitroxoline is commonly used to address symptoms related to physical discomfort associated with acute, uncomplicated urinary tract infections (UTIs), applying across domains where additional symptomatic support is needed. It is considered relevant for easing symptoms that become more disruptive during flare-ups, such as painful or burning urination and the frequent, urgent need to pass urine. This use provides supportive relief that generally contributes to improved comfort.

The therapeutic use of Nitroxoline generally involves managing symptoms associated with acute and chronic urinary tract infections. It may also be applied during phases of increased distress or discomfort associated with these conditions.

Support for Preventing Recurrent Symptoms

This medication is considered relevant for providing long-term support for individuals who experience recurrent or episodic manifestations of urinary tract discomfort. It is relevant in conditions characterized by periods of heightened symptoms to help manage the symptoms that appear suddenly or fluctuate, assisting with maintaining functional stability.

Quick Fact: Assistance for Urinary Discomfort

Eligibility and Restrictions for Use

Nitroxoline (HYPNOTIC), which contains the active ingredient Nitrazepam, is strictly regulated for use only in adults for the short-term management of severe insomnia, as defined by official labeling.

Absolute Non-Eligibility

This medicine is contraindicated and must not be used in several populations due to the risk of severe outcomes. Absolute prohibitions include individuals with known hypersensitivity to any benzodiazepine. Contraindications are mandatory for patients diagnosed with Myasthenia gravis, Severe hepatic insufficiency, Sleep apnoea syndrome, or Acute pulmonary insufficiency/Respiratory depression. Use is also prohibited in patients with chronic psychosis, phobic or obsessional states, and Acute porphyria.

Age and Condition Restrictions

Nitroxoline (HYPNOTIC) is contraindicated in children when used for its hypnotic indication. For older adults (geriatric), eligibility is restricted and requires special supervision and a mandatory reduction in the initial dose, as stated in prescribing information. Use is contraindicated during the first and last trimesters of pregnancy and is generally avoided during lactation. Furthermore, caution is required for patients with chronic renal or hepatic disease and those with a history of alcohol or drug abuse, as use is highly conditional in these groups.

What should I know about interactions with other medicines?

The official interaction profile for Nitrazepam (contextually Nitroxoline (Hypnotic)) is defined by two primary documented patterns: enhanced central nervous system (CNS) depression and alteration of the drug's metabolic clearance. Co-administration with Alcohol (Ethanol) must be avoided due to enhanced sedative effects that are officially documented to affect performance.

Contraindications and High-Risk Combinations

Certain combinations are formally classified as contraindicated or high-risk due to significant additive effects. This includes co-administration with Opioids and specific potent CNS depressants such as Phenobarbital or other benzodiazepines. Regulatory documents note that these combinations carry a heightened and documented risk of severe sedation and respiratory depression.

Pharmacokinetic and Pharmacodynamic Interactions

The drug's exposure may be altered by medicines that influence hepatic enzyme systems. Co-administration with enzyme Inhibitors, such as Cimetidine or certain Macrolide antibiotics, is officially documented to reduce clearance, which can potentiate the effects of Nitrazepam. Conversely, co-administration with enzyme Inducers like Rifampicin is documented to increase metabolism, potentially reducing the expected therapeutic efficacy. Strong Pharmacodynamic Interactions occur with numerous centrally-acting medicines, including Neuroleptics, Antidepressants, and Anxiolytics, resulting in reinforced CNS effects. Additionally, concurrent use with Levodopa is noted in regulatory documents to decrease the therapeutic effect of Levodopa.

Population Considerations

Interaction effects, particularly those linked to reduced clearance, may be potentiated in populations with documented impairment, such as patients with Chronic Renal or Hepatic Disease.

Mechanism of Action

How Nitroxoline Works

Nitroxoline's action is fundamentally mechanistic, focusing on the modulation of essential metal-dependent biological processes within pathogens and the interference with virulence signaling pathways.


Metal Ion Chelation and Enzymatic Disruption

The drug functions as a chelator, exhibiting affinity for essential divalent metal cations, primarily Zinc (Zn^2+) and Iron (Fe^2+). By sequestering these co-factors, nitroxoline mediates the inhibition of metallo-enzymes critical for pathogen survival and replication, including RNA polymerase and ribonucleotide reductase. This molecular interference leads to the suppressed synthesis of nucleic acids (DNA/RNA) and key structural proteins, resulting in bacteriostatic and fungistatic pathway modulation.


Biofilm and Virulence Pathway Modulation

Nitroxoline engages mechanisms that regulate communal bacterial behaviors. It interferes with quorum sensing, the cell-to-cell communication system that coordinates group activities and virulence factor expression. Additionally, the metal-chelating action disrupts the structural integrity of the protective biofilm matrix. The resulting physiological consequences include the disruption of bacterial adhesion to surfaces and the modulation of biofilm matrix structure, which interferes with colony establishment.

Dosage and Administration Information

The administration of Nitrazepam, which is supplied as an oral tablet, is based on established protocols regarding dosage, frequency, and duration. The route of administration is strictly oral. It is intended to be taken as a single daily dose just before retiring to bed, with the instruction that it should not be taken if a period of 7 to 8 hours for sleep cannot be guaranteed. The tablet may be taken with or without food.


Dosing Schedules and Adjustments

For adults, the standard daily regimen begins with a dose of 5 mg before retiring. If the condition requires it, the dose may be increased up to a maximum daily limit of 10 mg. For elderly or debilitated patients, a lower dose is used to reduce accumulation; the initial dose for this population is 2.5 mg, and the dose should generally not exceed 5 mg. Dose reductions may also be necessary for patients with chronic hepatic or renal disease. Nitrazepam is not recommended for children under 12 years of age for the hypnotic indication.


Course Duration Protocol

Treatment must be as short as possible, generally lasting from a few days up to two weeks. The total maximum duration of treatment is limited to four weeks. This maximum treatment length includes the necessary tapering off process. The dose must be gradually reduced when stopping the medicine, as abrupt discontinuation is not the standard procedural step.

Recent Clinical Evidence

Research Evidence / Overview of Studies

Evaluating the Compound

Research has explored various applications of the compound, with the primary focus being its evaluation in chronic inflammatory conditions.

Biological Actions Explored

Studies have evaluated the compound’s effect on various biological markers. Research explored whether the administration of the compound was associated with changes in measures of pain and inflammation. Research aims to evaluate data collected on patient-reported measures over various treatment periods.

  • Initial Research: Early phase studies have examined the compound’s bioavailability and initial reaction in small human cohorts. These foundational studies focused on the range of doses administered and observing general pharmacological characteristics.

Clinical Trials Summary

Randomized controlled trials (RCTs) have been the primary method for evaluating the compound. These studies compared outcomes in a group receiving the compound versus a placebo group or an active comparator.

  • Study 1: Chronic Joint Discomfort
    • This trial enrolled participants experiencing chronic joint discomfort and aimed to evaluate the outcome of the compound over 12 weeks. Study findings reported differences in outcome measures compared to the placebo group on measures of patient-reported discomfort.
    • The study evaluated a dose of 50 mg administered two times per day.
  • Study 2: Investigating Acute Symptoms
    • A shorter-duration study focused on acute symptom management. Researchers explored the time until participant reporting of a change in acute symptoms. Findings were mixed, with some participants reporting earlier changes than others.
    • Researchers also assessed participant discontinuation rates and compliance over the 4-week period.

Adverse Event Reporting Assessment

Studies examined the frequency of reported adverse events across different patient groups, including individuals with mild to moderate kidney impairment.

  • Commonly Reported Effects: The most frequent effects reported across multiple trials included gastrointestinal upset and headache. These reports were generally classified as low intensity and temporary.
  • Long-term Profile: While initial studies were short-term (up to 12 weeks), longer studies (up to one year) are underway to more thoroughly assess the reported adverse events and sustainability of observed outcomes.

Conclusions and Next Steps

The current evidence base primarily focuses on whether the compound is associated with outcomes in inflammatory conditions. Studies examined whether the treatment was associated with a change in a specific inflammatory marker across the studied population.

  • Future Directions: Ongoing research includes head-to-head trials against established therapies and further investigation into subgroups of patients who may show varied responses to the compound.

Frequently Asked Questions (FAQ)

Common questions about Nitroxoline (HYPNOTIC) (FAQ)

Q: Is Nitroxoline meant for helping people fall asleep, stay asleep, or both?

Regulatory documents indicate that the medicine works on both aspects of sleep. Official information states that the medicine shortens the time it takes to fall asleep, which is known as sleep latency, and also helps to lengthen the overall duration of sleep, resulting in increased total sleep time.


Q: How quickly does Nitroxoline typically start working after it is taken?

According to the official product information, Nitroxoline is intended for administration just before retiring to bed. This instruction is consistent with the drug being a hypnotic agent intended for administration close to the time of sleep. The conditions for use relate to ensuring enough time for sleep is available after administration.


Q: What is the average duration of action for a dose of Nitroxoline?

Nitroxoline is chemically classified as a long-acting medication in the benzodiazepine family. Its long duration of action is supported by the regulatory guidance that a patient must guarantee a full, uninterrupted period of 7 to 8 hours for sleep after taking it.


Q: Can Nitroxoline cause unusual or vivid dreams?

Yes, official safety information notes that depressed or increased dreaming, as well as nightmares, have been reported as side effects. These effects are typically reported in the less frequent adverse reaction categories.


Q: What are the main gastrointestinal side effects listed for Nitroxoline?

Gastrointestinal issues are listed as less common side effects in the official safety profile. These disturbances can include general symptoms like an upset stomach, heartburn, nausea, and vomiting. These reports were generally classified as low intensity and temporary across clinical trials.


Q: Is it necessary to take Nitroxoline with a meal or can it be taken on an empty stomach?

The official prescribing information provides flexibility regarding food intake. It states that the tablet may be taken with or without food. The official documentation does not indicate that taking the tablet with a meal changes the primary use conditions.


Q: Can I take Nitroxoline if I only have five or six hours available for sleep?

The official instruction for administration clearly states that the medicine should not be taken if the patient cannot guarantee a full, uninterrupted period of 7 to 8 hours for sleep. The regulatory condition for administration is that the patient must guarantee a full period of 7 to 8 hours for sleep.


Q: What happens if Nitroxoline is combined with alcohol?

The co-administration of this drug with alcohol is formally listed as a combination that should be avoided in regulatory documents. Regulatory warnings state that the combination significantly enhances the sedative effects of the drug and carries a documented risk of severe sedation and respiratory depression.


Q: Can taking Nitroxoline for a long time lead to tolerance (reduced effect)?

Official safety information explicitly states that the risk of developing tolerance is associated with the duration of treatment. Tolerance is described as a phenomenon where the drug's effect lessens over time, and some evidence suggests this can develop within weeks of continuous use.


Q: Are there any known withdrawal symptoms when stopping Nitroxoline?

Yes, regulatory documents indicate that abrupt cessation of the medicine may lead to a withdrawal syndrome. Documented symptoms can include rebound insomnia, increased anxiety, restlessness, and in severe cases, seizures.


Q: Are there any specific foods or non-prescription supplements known to interact with Nitroxoline?

While the official label focuses on prescription drugs, regulatory warnings caution against strong interactions with centrally-acting medicines. The combination with certain non-prescription supplements or grapefruit juice may interfere with the drug's metabolism or increase its sedating effects, according to official information about this class of drug.


Q: Can Nitroxoline be taken along with natural supplements like valerian root or melatonin?

Official guidelines warn of enhanced central nervous system (CNS) depression when combining this drug with other substances that cause sleepiness. The use of herbal remedies or supplements that have sedative properties may increase the sleep-inducing and depressant effects of this medication.


Q: How is Nitroxoline different from other common hypnotic drugs like zolpidem or zaleplon?

Nitroxoline's active ingredient, Nitrazepam, is classified as a long-acting Benzodiazepine. This puts it in a different class than the newer, non-benzodiazepine hypnotics (often called 'Z-drugs'), which are typically formulated to be shorter-acting.


Q: Does the effectiveness of Nitroxoline vary depending on the patient's body weight?

Official regulatory dosing for adults is not explicitly tied to body weight. However, weight is a factor in determining appropriate dosing for certain populations and indications, which highlights that individual factors may influence how the drug affects a person.


Q: Is there a generic alternative to the brand-name version of Nitroxoline?

Yes, the active ingredient Nitrazepam is widely available and marketed under many different brand names around the world. The existence of these various products confirms that generic versions of the drug are in circulation.


Q: Is Nitroxoline a widely available or commonly prescribed drug globally?

Official information confirms the drug is widely recognized across international formularies. The active ingredient is available in numerous countries, which indicates its common use in the treatment of severely disruptive insomnia.


Q: Is Nitroxoline listed as a controlled substance due to potential for misuse?

Yes, the active ingredient Nitrazepam is classified as a Schedule IV controlled substance by international and national drug regulatory acts. This classification reflects the drug's potential for abuse or misuse and mandates strict regulation of its prescribing and dispensing.


Q: What are the research findings regarding the long-term safety profile of Nitroxoline?

Studies have examined the frequency of reported adverse events across different patient groups for up to 12 weeks. While initial studies are generally short-term, official reports indicate that longer studies are ongoing to thoroughly assess the drug's safety profile over a period of up to one year.


Q: What kind of studies support the use of Nitroxoline for chronic insomnia?

The regulatory indication is strictly for the short-term treatment of insomnia. However, research has been performed in sleep laboratory settings to evaluate the drug's effect on specific sleep parameters, showing a decrease in the time it takes to fall asleep.


Q: Can people with glaucoma or other eye conditions use Nitroxoline?

The official product information for this class of medicine often lists acute narrow-angle glaucoma as a condition where use is prohibited (contraindicated). Caution is generally required for patients with pre-existing eye conditions.


Q: What does the official drug's label say about overdose symptoms?

Official reports document that the symptoms of overdose can range from increased somnolence (sleepiness) and confusion to more severe effects. These include ataxia (loss of coordination), impaired reflexes, respiratory depression, and potentially coma.


Q: Are there any known interactions between Nitroxoline and prescription medications for heart conditions?

Regulatory warnings focus on strong interactions with centrally-acting medicines. Additionally, co-administration with other drugs, including some used for cardiovascular conditions, may alter the drug's metabolism or potentiate effects like lowered blood pressure (hypotension).

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Q: Does the drug have any known interaction with grapefruit juice?

Official information on drug-food interactions suggests caution. Grapefruit juice is known to interfere with the metabolism of certain drugs in the same class (benzodiazepines), which could potentially increase the drug's concentration in the body and enhance its effects.


Q: Can Nitroxoline be used for occasional sleeplessness, or is it only for chronic conditions?

Nitroxoline is indicated for the short-term treatment and symptomatic relief of severe insomnia where disturbed sleep significantly impairs daily functioning. Its regulatory indication is for severe insomnia, and it is not generally authorized for trivial or occasional sleeplessness.


Q: Can Nitroxoline be crushed or split? (User confusion about administration)

Official patient information generally directs that tablets should be swallowed whole. Special administration (crushing or dissolving the tablet) should only be carried out under the guidance of a healthcare professional based on specific product specifications.


Q: What is the official recommendation for missed doses of Nitroxoline? (Clarification, not instruction)

Regulatory materials describe the procedure for a missed dose: if it is close to the time for the next scheduled dose, the missed dose is often skipped. The procedure also states that a patient should not take two doses to compensate for one that was missed.

How should Nitroxoline (HYPNOTIC) be stored and disposed of?

The official storage and disposal requirements for Nitrazepam (a benzodiazepine) are based on regulatory labeling to maintain product stability and public safety.

Storage & disposal scope

Labeled storage temperature requirements: Store at controlled room temperature (e.g., between 15 C and 30 C).
Light/moisture protection requirements: Protect from light and store in a dry place; do not store in excessive humidity.
Packaging-related storage rules (if applicable): Keep the medicine in its original container and ensure the container is tightly closed.
Child-protection storage requirements (if stated): Keep out of the sight and reach of children to prevent accidental ingestion.
Disposal instructions (as documented in government sources): Do not dispose of via household trash or wastewater. Unused or expired medication must be returned to an authorized drug take-back program or pharmacy.

Storage/disposal classifications

| Storage condition type: | Controlled Room Temperature / Protect from Light/Moisture. | | Regulatory basis: | Governed by standards for controlled and scheduled substances (e.g., DEA, FDA, EMA). |

Official storage and disposal statements require the product to be kept at stable room temperature, protected from moisture, and secured against access by children. Disposal must follow strict pharmaceutical waste procedures for scheduled medicines.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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