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Medical Disclaimer: This information is for educational purposes only and is not a substitute for professional medical advice.
Benzodiazepine [EPC]
Diazepam is a long-acting benzodiazepine used to treat anxiety, muscle spasms, seizures, and alcohol withdrawal. It works by enhancing the effects of GABA, a calming neurotransmitter in the central nervous system.
Name
Diazepam
Raw Name
DIAZEPAM
Category
Benzodiazepine [EPC]
Drug Count
6
Variant Count
116
Last Verified
February 17, 2026
RxCUI
197589, 197590, 197591, 309845, 104699, 104700, 801961, 801966, 309844, 309843, 2120550, 2272613, 2272619, 2272621, 2272622, 2272623, 2272624, 2272626, 2272627, 2272629, 2272630, 2272632, 2272633, 2272635, 2272636, 1807452, 801957, 1807459
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About Diazepam
Diazepam is a long-acting benzodiazepine used to treat anxiety, muscle spasms, seizures, and alcohol withdrawal. It works by enhancing the effects of GABA, a calming neurotransmitter in the central nervous system.
Detailed information about Diazepam
This page is for informational purposes only and does not replace medical advice. Consult a qualified healthcare professional before using any medication containing Diazepam.
In clinical practice, your healthcare provider may prescribe diazepam for a wide variety of conditions involving central nervous system (CNS) over-excitation. It is classified by the U.S. Drug Enforcement Administration (DEA) as a Schedule IV controlled substance due to its potential for abuse, misuse, and the development of physical dependence. Despite the emergence of newer agents, diazepam remains on the World Health Organization's (WHO) List of Essential Medicines because of its efficacy, versatility, and well-understood safety profile when used under strict medical supervision.
Diazepam exerts its therapeutic effects by modulating the activity of gamma-aminobutyric acid (GABA), which is the primary inhibitory neurotransmitter in the human brain. To understand how diazepam works at the molecular level, one must look at the GABA-A receptor complex. This receptor is a ligand-gated chloride ion channel. When GABA binds to its receptor, it opens the channel, allowing chloride ions to flow into the neuron. This influx of negative charge hyperpolarizes the cell, making it less likely to fire an action potential, effectively 'slowing down' brain activity.
Diazepam acts as a positive allosteric modulator. It does not bind to the same site as GABA itself; instead, it binds to a specific 'benzodiazepine site' located at the interface between the alpha and gamma subunits of the GABA-A receptor. By binding here, diazepam increases the frequency with which the chloride channel opens in response to GABA. It does not increase the duration of the opening, which is a key distinction from barbiturates. This enhancement of GABAergic inhibition results in the drug's characteristic five-fold clinical effects: anxiolytic (anxiety-reducing), sedative-hypnotic (sleep-inducing), anticonvulsant (seizure-stopping), muscle relaxant, and amnestic (memory-impairing).
Understanding how the body processes diazepam is crucial for managing its long-lasting effects and potential for accumulation.
Your healthcare provider may utilize diazepam for several FDA-approved indications:
Off-label uses, which are not FDA-approved but supported by clinical literature, may include the management of Meniere’s disease (for vertigo), stiff-person syndrome, and specific types of insomnia.
Diazepam is available in multiple delivery systems to suit different clinical needs:
> Important: Only your healthcare provider can determine if Diazepam is right for your specific condition. The choice of formulation and dosage depends on the severity of the condition and the patient's individual metabolic profile.
Dosage for diazepam must be strictly individualized to achieve maximum therapeutic benefit with the minimum effective dose. Your healthcare provider will determine the schedule based on your specific diagnosis and response.
Diazepam is approved for use in pediatric patients as young as 6 months of age for certain indications. It is generally not recommended for infants under 6 months due to the lack of safety data and the risk of respiratory depression.
While the kidneys excrete diazepam metabolites, significant dose adjustments are not always required for mild renal impairment. However, in severe renal failure, the accumulation of active metabolites can occur, necessitating a lower frequency of dosing or a smaller dose size to prevent toxicity.
Because diazepam is extensively metabolized by the liver, patients with cirrhosis or hepatitis require significant dose reductions. Liver dysfunction can double or triple the half-life of diazepam, leading to dangerous levels of sedation. Healthcare providers typically start with the lowest possible dose and monitor liver function tests (LFTs) closely.
In the elderly, the body's ability to clear benzodiazepines decreases. Furthermore, the risk of ataxia (loss of coordination) and over-sedation is much higher, which can lead to falls and hip fractures. Most guidelines suggest starting at 50% of the standard adult dose.
If you miss a dose, take it as soon as you remember. However, if it is almost time for your next scheduled dose, skip the missed dose and return to your regular dosing schedule. Do not 'double up' on doses to catch up, as this significantly increases the risk of respiratory depression and extreme lethargy.
A diazepam overdose can be life-threatening, especially if combined with alcohol or other CNS depressants.
> Important: Follow your healthcare provider's dosing instructions precisely. Do not adjust your dose or stop taking this medication without medical guidance, as sudden discontinuation can lead to severe withdrawal symptoms.
Most patients taking diazepam will experience some degree of central nervous system depression. These effects are often most pronounced during the first few days of treatment and may diminish as the body adjusts to the medication.
> Warning: Stop taking Diazepam and call your doctor immediately if you experience any of the following serious symptoms:
Prolonged use of diazepam (typically beyond 2-4 weeks) carries significant risks that must be discussed with a healthcare provider:
The FDA has issued several 'Black Box Warnings' for diazepam, the highest level of caution for a medication:
Report any unusual symptoms to your healthcare provider immediately. Monitoring for side effects is an ongoing part of your treatment plan.
Diazepam is a powerful medication that requires careful monitoring. It should never be shared with others, especially those with a history of substance abuse. Because of its long half-life, the effects of diazepam can persist for several days after the last dose is taken. Patients must be aware that their coordination and judgment may be impaired even if they feel 'normal.'
1. Opioid Interaction Warning: The use of benzodiazepines, including diazepam, and opioids may result in profound sedation, respiratory depression, coma, and death. Reserve concomitant prescribing of these drugs for use in patients for whom alternative treatment options are inadequate. Limit dosages and durations to the minimum required.
2. Addiction and Abuse Warning: Diazepam use, even at recommended doses, exposes users to the risk of abuse and addiction, which can lead to overdose and death. Before prescribing, healthcare providers should evaluate each patient’s risk and monitor them regularly.
3. Withdrawal Warning: To reduce the risk of withdrawal reactions, use a gradual taper to discontinue diazepam or reduce the dosage. Patients should be monitored for symptoms like autonomic instability and seizures during this process.
If you are on long-term diazepam therapy, your doctor may require regular testing:
Do not drive, operate heavy machinery, or engage in hazardous activities until you know how diazepam affects you. The drug significantly slows reaction times and impairs motor coordination. This effect is compounded if you are sleep-deprived or taking other sedating medications.
Alcohol must be strictly avoided. Alcohol and diazepam both depress the central nervous system. Combining them can lead to fatal respiratory failure, extreme sedation, and an increased risk of accidents. Even small amounts of alcohol can have an unpredictable and dangerous effect when combined with diazepam.
Never stop taking diazepam abruptly. Doing so can trigger a withdrawal syndrome that includes anxiety, insomnia, palpitations, tremors, and in severe cases, hallucinations and grand mal seizures. Your healthcare provider will design a tapering schedule, often reducing the dose by 10-25% every 1-2 weeks, to allow your brain chemistry to stabilize.
> Important: Discuss all your medical conditions, including any history of substance use or breathing problems, with your healthcare provider before starting Diazepam.
Certain medications should never be used with diazepam due to the risk of life-threatening complications:
Diazepam generally does not interfere with common clinical laboratory tests, although it may occasionally cause minor elevations in liver enzymes (ALT/AST) or alkaline phosphatase. If you are undergoing a urine drug screen, diazepam will test positive for benzodiazepines.
Mechanism of Interactions: Most interactions with diazepam are either pharmacodynamic (additive effects on the brain) or pharmacokinetic (interference with liver enzymes like CYP3A4).
Management Strategy: Your doctor may need to adjust your dose or choose an alternative medication. Always provide a full list of all substances you consume, including 'natural' supplements.
> Important: Tell your doctor about ALL medications, supplements, and herbal products you are taking before starting treatment with Diazepam.
There are several conditions where the risks of diazepam therapy clearly outweigh any potential benefits. In these cases, diazepam must NEVER be used:
In these scenarios, a healthcare provider will perform a careful risk-benefit analysis before prescribing diazepam:
Patients who are allergic to one benzodiazepine are highly likely to be allergic to others. If you have had a reaction to Valium, Xanax, Ativan, or Klonopin, you should inform your doctor immediately, as cross-sensitivity is a major clinical concern.
> Important: Your healthcare provider will evaluate your complete medical history and current physical state before determining if Diazepam is safe for you.
Diazepam is classified as FDA Pregnancy Category D. This means there is positive evidence of human fetal risk based on adverse reaction data from investigational or marketing experience.
Diazepam and its active metabolites pass into breast milk in significant quantities. Because infants (especially neonates) metabolize diazepam much more slowly than adults, the drug can accumulate in the baby's system. This may cause excessive somnolence (sleepiness), weight loss, and developmental delays in the nursing infant. Generally, breastfeeding is not recommended while taking diazepam.
Diazepam is FDA-approved for use in children as young as 6 months for anxiety and muscle spasms. However, children are more susceptible to the sedative effects and may experience paradoxical reactions (hyperactivity, aggression). Long-term effects on cognitive development and growth have not been extensively studied, so use should be limited to the shortest duration possible.
The American Geriatrics Society's Beers Criteria lists diazepam as a potentially inappropriate medication for older adults.
In patients with kidney disease, the active metabolite nordiazepam can accumulate. While not as dangerous as hepatic impairment, renal patients should be monitored for increased sedation. Diazepam is not significantly removed by hemodialysis because it is highly protein-bound.
The liver is the primary site of diazepam metabolism. In patients with mild to moderate hepatic impairment, the half-life is significantly prolonged. In severe hepatic impairment (Child-Pugh Class C), diazepam is contraindicated as it can precipitate hepatic coma. Dosage should be reduced by at least 50% in patients with known liver dysfunction.
> Important: Special populations require individualized medical assessment. Always inform your doctor if you are pregnant, planning to become pregnant, or nursing.
Diazepam is a classic 1,4-benzodiazepine that acts as a positive allosteric modulator of the GABA-A receptor. The GABA-A receptor is a pentameric structure (usually consisting of two alpha, two beta, and one gamma subunit) that forms a central chloride ion channel. Diazepam binds specifically to the interface between the alpha ($\\alpha_1, \\alpha_2, \\alpha_3,$ or $\\alpha_5$) and gamma ($\\gamma_2$) subunits.
This binding causes a conformational change in the receptor that increases its affinity for the neurotransmitter GABA. When GABA binds, the chloride channel opens more frequently, allowing an influx of chloride ions into the postsynaptic neuron. This hyperpolarization inhibits neuronal firing. The $\\alpha_1$ subunit is primarily associated with sedation and anticonvulsant effects, while the $\\alpha_2$ and $\\alpha_3$ subunits mediate anxiolytic and muscle-relaxant properties.
| Parameter | Value |
|---|---|
| Bioavailability | 93% - 100% |
| Protein Binding | 98% (primarily Albumin) |
| Half-life (Parent) | 20 - 50 hours |
| Half-life (Nordiazepam) | 30 - 100 hours |
| Tmax (Oral) | 0.5 - 1.5 hours |
| Metabolism | Hepatic (CYP3A4, CYP2C19) |
| Excretion | Renal (70%), Fecal (10%) |
Diazepam is a member of the Benzodiazepine class. Related medications include short-acting agents like Midazolam, intermediate-acting agents like Alprazolam (Xanax) and Lorazepam (Ativan), and other long-acting agents like Clonazepam (Klonopin) and Chlordiazepoxide (Librium).
Medications containing this ingredient
Common questions about Diazepam
Diazepam is primarily used to treat anxiety disorders, acute alcohol withdrawal symptoms, and muscle spasms. Your healthcare provider may also prescribe it as an adjunctive treatment for certain types of seizures or as a sedative before medical procedures. It works by enhancing the effects of GABA, a chemical in the brain that promotes calmness and relaxation. Because it is a long-acting medication, it is often preferred for conditions where a steady level of the drug is needed in the bloodstream. It is not intended for long-term use in treating everyday stress.
The most frequently reported side effects of diazepam include drowsiness, fatigue, muscle weakness, and a loss of coordination known as ataxia. Many patients feel 'sleepy' or 'clumsy' during the first few days of treatment as their body adjusts to the medication. Other common issues can include dry mouth, blurred vision, or slight confusion, particularly in older adults. If these symptoms are severe or do not go away, you should contact your healthcare provider. Because it causes sedation, you should avoid driving or operating machinery until you know how it affects you.
No, you must strictly avoid alcohol while taking diazepam. Both substances are central nervous system depressants, meaning they slow down brain activity and breathing. Combining them can lead to dangerous levels of respiratory depression, extreme sedation, coma, and even death. Alcohol also increases the risk of accidental falls and injuries while on diazepam. Even a small amount of alcohol can have a significantly magnified effect when this medication is in your system.
Diazepam is generally not recommended during pregnancy, especially during the first and third trimesters. It is classified as a Category D medication, meaning there is evidence of potential risk to the human fetus, such as an increased risk of cleft lip or palate. Use near the end of pregnancy can cause 'floppy infant syndrome,' where the newborn has trouble breathing, feeding, and maintaining body temperature. If you are pregnant or planning to become pregnant, discuss alternative treatments with your doctor immediately. Do not stop taking the medication abruptly without medical advice, as withdrawal can also be harmful.
When taken orally in tablet form, diazepam is absorbed quickly and usually begins to work within 30 to 90 minutes. For emergency situations like a continuous seizure, healthcare providers use intravenous (IV) diazepam, which works almost immediately, typically within 1 to 5 minutes. The rectal gel formulation also works rapidly for acute seizure clusters. While the onset is fast, the drug stays in your system for a very long time because of its long half-life and active metabolites. You may feel the effects for many hours or even days after a single dose.
You should never stop taking diazepam suddenly if you have been using it for more than a few weeks. Abruptly stopping can lead to a severe withdrawal syndrome because your brain has become accustomed to the drug's presence. Symptoms of withdrawal include extreme anxiety, tremors, sweating, insomnia, muscle cramps, and life-threatening seizures. To stop safely, your healthcare provider will create a tapering schedule to slowly lower your dose over several weeks or months. This allows your central nervous system to gradually readjust to the absence of the medication.
If you miss a dose of diazepam, take it as soon as you remember. However, if it is nearly time for your next scheduled dose, skip the missed dose and continue with your regular timing. Never take two doses at once to make up for a missed one, as this increases the risk of over-sedation and respiratory depression. If you find yourself frequently forgetting doses, talk to your pharmacist about using a pill organizer or setting an alarm. Consistency is key to maintaining the therapeutic effects of the drug.
Weight gain is not a common or direct side effect of diazepam for most patients. However, some individuals may experience changes in appetite or reduced physical activity due to the drug's sedative and muscle-relaxing effects, which could indirectly lead to weight changes. In some cases, patients may experience fluid retention or increased cravings for certain foods. If you notice significant or rapid weight gain while taking diazepam, you should discuss this with your healthcare provider to rule out other causes. Maintaining a balanced diet and monitoring your activity levels can help.
Diazepam has many significant drug interactions, so it is vital to tell your doctor about every medication you take. It is particularly dangerous to mix with opioids, barbiturates, or other sedatives due to the risk of fatal respiratory depression. Certain medications like cimetidine, omeprazole, and some antibiotics can slow down the clearance of diazepam from your body, leading to toxicity. Even herbal supplements like St. John's Wort or Kava can interfere with how diazepam works. Always consult your pharmacist before starting any new over-the-counter or prescription drug.
Yes, diazepam is widely available as a generic medication and is typically very affordable. The brand name Valium is still available, but the generic versions are bioequivalent, meaning they contain the same active ingredient and work the same way in the body. Generic diazepam comes in various forms, including tablets, oral solutions, and injectables. Because it is a generic drug, it is covered by most insurance plans and Medicare. Always ensure you are receiving the medication from a reputable, licensed pharmacy.