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Medical Disclaimer: This information is for educational purposes only and is not a substitute for professional medical advice.
Benzodiazepine [EPC]
Chlordiazepoxide is a long-acting benzodiazepine primarily indicated for the management of anxiety disorders and the treatment of acute alcohol withdrawal symptoms. It functions by enhancing the inhibitory effects of GABA in the central nervous system.
Name
Chlordiazepoxide
Raw Name
CHLORDIAZEPOXIDE HYDROCHLORIDE
Category
Benzodiazepine [EPC]
Salt Form
Hydrochloride
Drug Count
6
Variant Count
46
Last Verified
February 17, 2026
RxCUI
905369, 905495, 905516, 889614, 889616, 856769, 856792
UNII
MFM6K1XWDK, 91ZQW5JF1Z, 6RZ6XEZ3CR, 26LUD4JO9K
About Chlordiazepoxide
Chlordiazepoxide is a long-acting benzodiazepine primarily indicated for the management of anxiety disorders and the treatment of acute alcohol withdrawal symptoms. It functions by enhancing the inhibitory effects of GABA in the central nervous system.
Detailed information about Chlordiazepoxide
This page is for informational purposes only and does not replace medical advice. Consult a qualified healthcare professional before using any medication containing Chlordiazepoxide.
Chlordiazepoxide, widely recognized by the historical brand name Librium, is a landmark medication in the field of psychopharmacology. It belongs to the benzodiazepine class of drugs, specifically identified as an anxiolytic (anti-anxiety) and sedative-hypnotic agent. Discovered by Leo Sternbach in 1955 and approved by the U.S. Food and Drug Administration (FDA) in 1960, Chlordiazepoxide was the first benzodiazepine to be introduced into clinical practice. Its discovery revolutionized the treatment of psychiatric disorders, providing a safer alternative to the barbiturates that were commonly used at the time.
Structurally, Chlordiazepoxide is a 1,4-benzodiazepine. It is characterized by its long duration of action, which is attributed to its complex metabolic pathway and the formation of several pharmacologically active metabolites. Healthcare providers typically prescribe this medication for the short-term relief of severe anxiety, preoperative apprehension, and the management of acute alcohol withdrawal syndrome. Because of its potential for dependence and abuse, it is classified as a Schedule IV controlled substance under the Controlled Substances Act in the United States.
Chlordiazepoxide exerts its therapeutic effects by modulating the activity of the central nervous system (CNS). At the molecular level, it acts as a positive allosteric modulator of the Gamma-Aminobutyric Acid type A (GABA-A) receptor complex. GABA is the primary inhibitory neurotransmitter in the mammalian brain, responsible for reducing neuronal excitability.
When Chlordiazepoxide binds to its specific site on the GABA-A receptor—located at the interface of the alpha and gamma subunits—it induces a conformational change in the receptor. This change increases the affinity of the receptor for GABA, leading to an increased frequency of chloride ion channel opening. The resulting influx of chloride ions hyperpolarizes the postsynaptic neuron, making it less likely to fire an action potential. This overall reduction in neuronal firing manifests clinically as sedation, muscle relaxation, anticonvulsant activity, and a significant reduction in anxiety. Unlike barbiturates, benzodiazepines like Chlordiazepoxide do not directly open the chloride channel in the absence of GABA, which contributes to their wider therapeutic index.
The pharmacokinetic profile of Chlordiazepoxide is complex due to its extensive hepatic metabolism and long-lived active metabolites. Understanding these parameters is crucial for healthcare providers when determining dosing intervals and monitoring for potential accumulation.
Chlordiazepoxide is FDA-approved for several clinical indications. Healthcare providers often select this medication when a long-acting benzodiazepine is required to provide sustained symptom relief.
Off-label uses, though less common today, have historically included the management of irritable bowel syndrome (often in combination with clidinium bromide) and certain types of muscle spasms, though other agents are now typically preferred for these conditions.
Chlordiazepoxide is available in several dosage forms to accommodate different clinical needs. The hydrochloride salt is the most common form used in these preparations.
> Important: Only your healthcare provider can determine if Chlordiazepoxide is right for your specific condition. The long-acting nature of this drug requires careful medical supervision, especially in populations prone to drug accumulation.
Dosage for Chlordiazepoxide must be highly individualized based on the severity of the condition being treated and the patient's clinical response. Healthcare providers typically aim for the lowest effective dose for the shortest duration possible.
Chlordiazepoxide is generally not recommended for use in children under the age of 6. For children over 6 years old, the following guidelines are typically followed:
While the kidneys primarily excrete the metabolites of Chlordiazepoxide, impaired renal function can lead to the accumulation of these active substances. Healthcare providers may reduce the frequency of dosing or the total daily dose in patients with significant renal dysfunction.
Since Chlordiazepoxide is extensively metabolized by the liver, patients with hepatic impairment (such as cirrhosis) are at a high risk of drug accumulation and toxicity. Lower doses and extended dosing intervals are usually required. In cases of severe hepatic failure, the use of Chlordiazepoxide may be contraindicated.
Geriatric patients are more susceptible to the sedative and ataxic (loss of coordination) effects of Chlordiazepoxide. The initial dose for elderly or debilitated patients is typically limited to 5 mg, taken two to four times daily. This population is at a significantly increased risk for falls and cognitive impairment when taking long-acting benzodiazepines.
If you miss a dose of Chlordiazepoxide, take it as soon as you remember. However, if it is almost time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not double the dose to catch up, as this increases the risk of excessive sedation and respiratory depression.
An overdose of Chlordiazepoxide is a medical emergency. Symptoms of overdose include extreme drowsiness, confusion, diminished reflexes, muscle weakness, and coma. In severe cases, particularly when combined with other CNS depressants like alcohol or opioids, fatal respiratory depression can occur.
> Important: Follow your healthcare provider's dosing instructions. Do not adjust your dose or stop taking this medication without medical guidance, as sudden discontinuation can lead to severe withdrawal symptoms.
As with all benzodiazepines, Chlordiazepoxide commonly affects the central nervous system. These effects are often dose-related and may diminish as the body adjusts to the medication.
> Warning: Stop taking Chlordiazepoxide and call your doctor immediately if you experience any of these serious symptoms.
Chlordiazepoxide carries several prominent FDA Black Box Warnings, the most serious level of warning issued by the FDA.
Report any unusual symptoms or side effects to your healthcare provider immediately. Regular monitoring of liver and blood function is recommended for patients on long-term therapy.
Chlordiazepoxide is a potent central nervous system (CNS) depressant. Its use requires careful medical supervision and a thorough understanding of the potential risks. It should only be used for the condition for which it was prescribed and should never be shared with others, as misuse can be fatal.
According to the FDA-approved labeling updated in 2020, Chlordiazepoxide carries warnings regarding the risks of serious harm when combined with opioids. This combination significantly increases the risk of fatal respiratory depression. Additionally, the FDA warns that benzodiazepines carry a high potential for abuse, misuse, and addiction. Physical dependence can occur even with prescribed use, making a gradual taper essential when discontinuing the medication to avoid severe withdrawal symptoms such as seizures and delirium tremens.
For patients prescribed Chlordiazepoxide for extended periods, healthcare providers typically require regular monitoring to ensure safety:
Chlordiazepoxide significantly impairs motor coordination, reaction time, and judgment. Patients should not drive, operate heavy machinery, or engage in hazardous activities until they are certain the medication does not make them drowsy or dizzy. This impairment is often more pronounced during the first few days of treatment or when the dose is increased.
Alcohol must be strictly avoided while taking Chlordiazepoxide. Alcohol is also a CNS depressant and acts synergistically with benzodiazepines, meaning the combination is much more dangerous than either substance alone. This combination can lead to severe respiratory depression, unconsciousness, and death.
Do not stop taking Chlordiazepoxide abruptly. Sudden cessation after regular use can trigger a withdrawal syndrome that ranges from mild (insomnia, irritability) to life-threatening (seizures, psychosis). Your healthcare provider will provide a tapering schedule, gradually reducing the dose over several weeks or months to allow the brain's receptors to readjust safely.
> Important: Discuss all your medical conditions, including any history of lung, liver, or kidney disease, with your healthcare provider before starting Chlordiazepoxide.
Certain medications should never be combined with Chlordiazepoxide due to the risk of life-threatening interactions.
Chlordiazepoxide may interfere with certain laboratory tests:
For each major interaction, the primary mechanism is usually pharmacodynamic (additive CNS depression) or pharmacokinetic (alteration of the CYP450 metabolic pathway). Management typically involves dose reduction, avoiding the interacting substance, or choosing an alternative medication with a different metabolic profile (such as Lorazepam, which does not rely on the CYP3A4 system).
> Important: Tell your doctor about ALL medications, supplements, and herbal products you are taking, including over-the-counter drugs.
In certain medical conditions, the risks of using Chlordiazepoxide far outweigh any potential benefits. In these cases, the medication must never be used.
These are conditions where Chlordiazepoxide should be used with extreme caution and only if the benefits clearly outweigh the risks.
Patients who have experienced a severe reaction to other benzodiazepines (such as Diazepam, Alprazolam, or Clonazepam) are highly likely to be cross-sensitive to Chlordiazepoxide. This is due to the shared chemical structure of the 1,4-benzodiazepine ring. If a patient is allergic to one member of this class, the entire class should generally be avoided unless otherwise directed by an allergist.
> Important: Your healthcare provider will evaluate your complete medical history and perform a risk-benefit analysis before prescribing Chlordiazepoxide.
Chlordiazepoxide is classified by the FDA as a Pregnancy Category D medication. This means there is positive evidence of human fetal risk based on adverse reaction data from investigational or marketing experience.
Chlordiazepoxide and its active metabolites are excreted into human breast milk. Because neonates and infants metabolize benzodiazepines much more slowly than adults, the drug can accumulate in the nursing infant's system. This can cause excessive sedation, poor feeding, and weight loss in the baby. Generally, breastfeeding is not recommended while taking this medication. If use is essential, the infant must be closely monitored for signs of CNS depression.
Safety and effectiveness in children under the age of 6 have not been established. In children over 6, Chlordiazepoxide should be used at the lowest effective dose. Pediatric patients may be more susceptible to paradoxical reactions, such as increased agitation or aggression. Long-term effects on physical and cognitive development in children are not well-studied.
According to the Beers Criteria for Potentially Inappropriate Medication Use in Older Adults, long-acting benzodiazepines like Chlordiazepoxide should generally be avoided in the elderly.
In patients with impaired kidney function, the excretion of the active metabolites (such as oxazepam) may be delayed. While the parent drug is primarily cleared by the liver, the buildup of metabolites can still lead to increased side effects. Healthcare providers typically monitor renal function and may adjust the dosing frequency accordingly.
Patients with liver disease (e.g., hepatitis, cirrhosis) require significant dose reductions. Because Chlordiazepoxide relies on the CYP450 system for its initial metabolism, even moderate hepatic impairment can double or triple the drug's half-life. In patients with a Child-Pugh score indicating severe impairment, the drug is often avoided in favor of benzodiazepines that do not require hepatic oxidation, such as Lorazepam or Oxazepam.
> Important: Special populations require individualized medical assessment and frequent monitoring by a healthcare professional.
Chlordiazepoxide is a positive allosteric modulator of the GABA-A receptor. It binds to a specific regulatory site on the receptor complex, which is distinct from the binding site of the endogenous neurotransmitter GABA. When Chlordiazepoxide is bound, it increases the frequency with which the associated chloride ion channel opens in response to GABA binding. This results in an increased influx of chloride ions into the neuron, causing hyperpolarization of the neuronal membrane. This state makes the neuron less sensitive to excitatory stimuli, effectively "quieting" the central nervous system. This action in the limbic system accounts for its anxiolytic effects, while its action in the reticular formation and cerebral cortex accounts for its sedative properties.
The pharmacodynamic effects of Chlordiazepoxide include anxiolysis, sedation, anticonvulsant activity, and skeletal muscle relaxation. The onset of action is relatively rapid (within 1-2 hours for oral doses), but because of its long-acting metabolites, the clinical effects can persist for several days after a single dose. Tolerance to the sedative effects typically develops within a few weeks of continuous use, but tolerance to the anxiolytic effects may develop more slowly or not at all in some patients.
| Parameter | Value |
|---|---|
| Bioavailability | ~100% (Oral) |
| Protein Binding | 96% |
| Half-life (Parent) | 5 - 30 hours |
| Half-life (Metabolites) | Up to 100+ hours |
| Tmax | 1 - 4 hours |
| Metabolism | Hepatic (CYP3A4); active metabolites |
| Excretion | Renal (<1% unchanged) |
Chlordiazepoxide is a member of the benzodiazepine class. Within this class, it is categorized as a long-acting agent. Related medications include Diazepam (Valium), which is also long-acting, and Lorazepam (Ativan), which is intermediate-acting. Its unique 4-oxide structure distinguishes it from later benzodiazepines, but its core mechanism remains consistent with the class profile.
Medications containing this ingredient
Common questions about Chlordiazepoxide
Chlordiazepoxide is primarily used for the short-term management of anxiety disorders and the relief of symptoms associated with acute alcohol withdrawal. Healthcare providers also prescribe it to reduce apprehension and provide sedation before surgical procedures. Because it is a long-acting benzodiazepine, it provides a steady level of medication in the bloodstream, which is particularly helpful for preventing the severe tremors and seizures seen in alcohol withdrawal. It works by enhancing the calming chemicals in the brain to reduce overactive nerve signaling. It is not intended for long-term use due to the risk of dependency.
The most common side effects reported by patients taking Chlordiazepoxide include drowsiness, dizziness, and a lack of muscle coordination known as ataxia. Many users also experience a sense of confusion or lightheadedness, especially during the first few days of treatment. These effects are dose-dependent and are often more pronounced in elderly patients. Some individuals may also notice mild nausea or constipation. If these symptoms become severe or persist, it is important to contact your healthcare provider for a dosage adjustment.
No, you should strictly avoid drinking alcohol while taking Chlordiazepoxide. Both substances are central nervous system depressants, and when taken together, they can dangerously enhance each other's effects. This combination significantly increases the risk of severe respiratory depression, extreme sedation, coma, and even death. Even small amounts of alcohol can impair your coordination and judgment more severely when this medication is in your system. Always consult your doctor before consuming any substance that may affect your nervous system while on this medication.
Chlordiazepoxide is generally considered unsafe during pregnancy, particularly during the first trimester, as it has been linked to an increased risk of birth defects. It is classified as FDA Pregnancy Category D, indicating that there is clear evidence of risk to the human fetus. Taking this medication late in pregnancy can also cause the baby to be born with 'floppy infant syndrome' or experience withdrawal symptoms after birth. If you are pregnant or planning to become pregnant, you must discuss alternative treatments with your doctor. The medication should only be used if the potential benefit to the mother outweighs the significant risk to the fetus.
For most patients, the effects of an oral dose of Chlordiazepoxide begin to be felt within 1 to 2 hours after administration. Peak levels of the medication in the bloodstream are typically reached within 1 to 4 hours. However, because the drug is converted into several long-acting active metabolites, its full therapeutic effect for conditions like chronic anxiety may take several days of consistent dosing to stabilize. For acute conditions like alcohol withdrawal, healthcare providers may use higher initial doses to achieve rapid symptom control. The duration of a single dose's effect can be quite long due to the slow elimination of its metabolites.
You should never stop taking Chlordiazepoxide suddenly, especially if you have been taking it for more than a few weeks. Abrupt discontinuation can lead to severe withdrawal symptoms, including tremors, sweating, insomnia, abdominal cramps, and life-threatening seizures. Because Chlordiazepoxide is long-acting, withdrawal symptoms may not appear for several days after the last dose. Your healthcare provider will create a tapering schedule to slowly reduce your dose over time. This gradual reduction allows your brain's chemistry to return to normal safely and minimizes the risk of rebound anxiety.
If you miss a dose of Chlordiazepoxide, you should take it as soon as you remember. However, if it is almost time for your next scheduled dose, you should skip the missed dose and continue with your regular schedule. Never take two doses at the same time to make up for a missed one, as this can lead to excessive sedation or respiratory depression. Keeping a consistent schedule helps maintain stable levels of the drug in your body. If you frequently miss doses, consider using a pill reminder or discussing a different dosing schedule with your healthcare provider.
Weight gain is not considered a common side effect of Chlordiazepoxide, but it can occur in some individuals. The medication's sedative effects may lead to decreased physical activity, which can contribute to weight changes over time. Additionally, some patients may experience changes in appetite as their anxiety levels decrease. While not as strongly associated with weight gain as some antipsychotics or antidepressants, any significant change in weight should be discussed with your doctor. They can help determine if the change is related to the medication or other lifestyle factors.
Chlordiazepoxide can interact with many other medications, some of which can be very dangerous. It should not be taken with opioids, other sedatives, or sleep medications unless specifically directed by a doctor, due to the risk of fatal respiratory depression. Other drugs, such as certain antacids (cimetidine) or antidepressants, can change how your body processes Chlordiazepoxide, leading to higher levels and more side effects. Always provide your healthcare provider with a complete list of all prescription drugs, over-the-counter medicines, and herbal supplements you are using. This allows them to check for potential interactions before you start treatment.
Yes, Chlordiazepoxide is available as a generic medication in several strengths, including 5 mg, 10 mg, and 25 mg capsules. Generic versions are typically much less expensive than the original brand-name version, Librium, while providing the same clinical benefits. The FDA requires generic drugs to have the same active ingredient, strength, dosage form, and route of administration as the brand-name drug. Most insurance plans cover the generic form of Chlordiazepoxide. You can discuss with your pharmacist or doctor whether the generic version is appropriate for your specific treatment plan.