Diazepam 5mg/ml Inj, 10ml

Manufacturer NOVAPLUS Active Ingredient Diazepam Injection(dye AZ e pam) Pronunciation dye-AZ-e-pam
WARNING: This drug is a benzodiazepine. The use of a benzodiazepine drug along with opioid drugs has led to very bad side effects. Side effects that have happened include slowed or trouble breathing and death. Opioid drugs include drugs like codeine, oxycodone, and morphine. Opioid drugs are used to treat pain and some are used to treat cough. Talk with the doctor.If you are taking this drug with an opioid drug, get medical help right away if you feel very sleepy or dizzy; if you have slow, shallow, or trouble breathing; or if you pass out. Caregivers or others need to get medical help right away if the patient does not respond, does not answer or react like normal, or will not wake up. Benzodiazepines can put you at risk for drug use disorder. Misuse or abuse of this drug can lead to overdose or death, especially when used along with certain other drugs, alcohol, or street drugs. Drug use disorder can happen even if you take this drug as your doctor has told you. Get medical help right away if you have changes in mood or behavior, suicidal thoughts or actions, seizures, or trouble breathing.You will be watched closely to make sure you do not misuse this drug or develop drug use disorder.Benzodiazepines may cause dependence. Lowering the dose or stopping this drug all of a sudden may cause withdrawal. This can be life- threatening. The risk of dependence and withdrawal are raised the longer you take this drug and the higher the dose. Talk to your doctor before you lower the dose or stop this drug. You will need to follow your doctor's instructions. Get medical help right away if you have trouble controlling body movements, seizures, new or worse behavior or mood changes like depression or thoughts of suicide, thoughts of harming someone, hallucinations (seeing or hearing things that are not there), losing contact with reality, moving around or talking a lot, or any other bad effects.Sometimes, withdrawal signs can last for several weeks to more than 12 months. Tell your doctor if you have anxiety; trouble with memory, learning, or focusing; trouble sleeping; burning, numbness, or tingling; weakness; shaking; muscle twitching; ringing in the ears; or any other bad effects. @ COMMON USES: It is used to relax muscles.It is used to treat alcohol withdrawal.It is used to treat anxiety.It is used to help control certain kinds of seizures.It may be given to you for other reasons. Talk with the doctor.
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Drug Class
Anxiolytic, Sedative-Hypnotic, Anticonvulsant, Skeletal Muscle Relaxant
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Pharmacologic Class
Benzodiazepine, GABA-A receptor agonist
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Pregnancy Category
Category D
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FDA Approved
Nov 1963
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DEA Schedule
Schedule IV

Overview

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What is this medicine?

Diazepam injection is a medicine that works on your brain and nerves to calm you down. It's used for conditions like severe anxiety, seizures (like status epilepticus), and muscle spasms. It helps to relax your body and mind quickly.
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How to Use This Medicine

To use this medication correctly, follow your doctor's instructions and carefully read all accompanying information. Adhere to the dosage instructions provided by your healthcare team. This medication is administered via injection into a muscle or vein.

For proper storage and disposal, consult with your doctor, nurse, or pharmacist to determine the best approach if you need to store this medication at home.

If you miss a dose, contact your doctor promptly to receive guidance on the next steps to take.
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Lifestyle & Tips

  • Avoid alcohol and other sedating medications (e.g., opioids, sleeping pills) unless specifically instructed by your doctor, as this can cause dangerous breathing problems and extreme drowsiness.
  • Do not drive or operate heavy machinery until you know how this medication affects you, as it can cause drowsiness and dizziness.
  • Do not stop this medication suddenly if you have been taking it regularly, as this can lead to withdrawal symptoms, including seizures. Your doctor will help you taper off slowly if needed.

Dosing & Administration

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Adult Dosing

Standard Dose: Varies by indication. For severe anxiety: 2-10 mg IV/IM, repeat in 3-4 hours if needed. For status epilepticus: 5-10 mg IV, repeat every 10-15 minutes up to 30 mg total.
Dose Range: 2 - 30 mg

Condition-Specific Dosing:

severeAnxiety: 2-10 mg IV/IM, repeat in 3-4 hours if needed.
acuteAlcoholWithdrawal: 10 mg IV/IM initially, then 5-10 mg in 3-4 hours if needed.
statusEpilepticus: 5-10 mg IV, repeat every 10-15 minutes up to 30 mg total. Max 30 mg in 8 hours.
muscleSpasm: 5-10 mg IV/IM, repeat in 3-4 hours if needed.
preEndoscopicProcedure: 5-10 mg IV, 30 minutes prior to procedure.
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Pediatric Dosing

Neonatal: Not established (use with extreme caution, risk of respiratory depression).
Infant: Status Epilepticus (30 days to <5 years): 0.2-0.5 mg slow IV every 2-5 minutes, up to 5 mg total.
Child: Status Epilepticus (>=5 years): 1 mg slow IV every 2-5 minutes, up to 10 mg total.
Adolescent: Similar to adult dosing, but start with lower doses and titrate carefully.
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Dose Adjustments

Renal Impairment:

Mild: No specific adjustment needed.
Moderate: No specific adjustment needed, but monitor for increased sedation.
Severe: Use with caution; monitor closely for prolonged sedation and respiratory depression.
Dialysis: Not significantly dialyzable; monitor for prolonged effects.

Hepatic Impairment:

Mild: Reduce dose by 50% or use lower end of dosing range.
Moderate: Reduce dose significantly (e.g., 50-75%) and monitor closely.
Severe: Contraindicated due to risk of hepatic encephalopathy and prolonged sedation.

Pharmacology

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Mechanism of Action

Diazepam binds to stereospecific benzodiazepine receptors on the postsynaptic GABA-A neuron at several sites within the central nervous system (CNS), including the limbic system, reticular formation, and cerebral cortex. It enhances the inhibitory effects of gamma-aminobutyric acid (GABA), the primary inhibitory neurotransmitter in the CNS, by increasing the frequency of chloride channel opening. This leads to hyperpolarization of the neuronal membrane, decreasing neuronal excitability and producing anxiolytic, sedative, hypnotic, anticonvulsant, and muscle relaxant effects.
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Pharmacokinetics

Absorption:

Bioavailability: 100% (IV); 90% (oral); Variable and erratic (IM)
Tmax: 1-5 minutes (IV); 0.5-1.5 hours (IM)
FoodEffect: Not applicable for injection; for oral, food can delay absorption but not extent.

Distribution:

Vd: 0.8-1.0 L/kg (adults); higher in neonates
ProteinBinding: 98% (primarily to albumin)
CnssPenetration: Yes

Elimination:

HalfLife: Diazepam: 20-100 hours (highly variable, longer in elderly and liver disease); Desmethyldiazepam: 30-100 hours
Clearance: 0.2-0.5 mL/min/kg
ExcretionRoute: Renal (primarily as conjugated metabolites); small amount in feces.
Unchanged: <1%
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Pharmacodynamics

OnsetOfAction: 1-5 minutes (IV); 15-30 minutes (IM)
PeakEffect: 5-10 minutes (IV)
DurationOfAction: 15-60 minutes (acute anticonvulsant/sedative effect); residual sedative effects can last much longer (hours to days) due to active metabolites.

Safety & Warnings

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BLACK BOX WARNING

Concomitant use of benzodiazepines 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. Follow patients for signs and symptoms of respiratory depression and sedation. The risks of abuse, misuse, and addiction with benzodiazepines can lead to overdose or death. Physical dependence can occur with prolonged use; abrupt discontinuation can lead to withdrawal symptoms, including seizures.
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Side Effects

Urgent Side Effects: Seek Medical Help Right Away

Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical attention immediately:

Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Shortness of breath
Change in balance
Feeling confused
Hallucinations (seeing or hearing things that are not there)
Memory problems or loss
Severe dizziness or fainting
Muscle spasms
Twitching
Trouble sleeping
Changes in eyesight
Slurred speech
Severe upset stomach, vomiting, or loss of appetite that persists
Suicidal thoughts or actions (especially if you have a history of suicidal thoughts or actions)
New or worsening symptoms of depression, nervousness, restlessness, irritability, panic attacks, or mood changes

If you are receiving this medication through injection (I.V.), be aware that it may cause tissue damage if the drug leaks from the vein. Inform your nurse immediately if you experience:

Redness
Burning
Pain
Swelling
Blisters
Skin sores
Leaking of fluid at the injection site

Other Possible Side Effects

Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to report any concerns to your doctor. If you experience any of the following side effects, contact your doctor or seek medical attention if they bother you or persist:

Feeling sleepy
Feeling tired or weak
Muscle weakness
Irritation at the injection site

This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
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Seek Immediate Medical Attention If You Experience:

  • Severe drowsiness or difficulty waking up
  • Slow, shallow, or difficult breathing
  • Confusion or unusual thoughts/behavior
  • Slurred speech
  • Unsteadiness or difficulty walking
  • Yellowing of skin or eyes (jaundice)
  • Signs of an allergic reaction (rash, itching, swelling, severe dizziness, trouble breathing)
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Before Using This Medicine

Before Taking This Medication: Important Information to Share with Your Doctor

It is essential to inform your doctor about the following:

Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
Certain health conditions, including:
+ Breathing problems
+ Glaucoma
+ Liver disease
+ Myasthenia gravis
+ Sleep apnea
If you have a history of psychosis
Recent consumption of large amounts of alcohol or use of medications that may cause drowsiness, such as phenobarbital or certain pain medications like oxycodone
If you are breast-feeding or plan to breast-feed, as you may need to avoid nursing while taking this medication
If the patient is a child, as this medication may not be suitable for all ages of children

This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health conditions. Never start, stop, or change the dose of any medication without consulting your doctor first.
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Precautions & Cautions

It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.

Before operating a vehicle or engaging in activities that require alertness and clear vision, ensure you understand how this medication affects you. Avoid consuming alcohol while taking this drug, as it may exacerbate its effects.

Prior to using marijuana, other forms of cannabis, or prescription and over-the-counter (OTC) medications that may impair your reactions, consult with your doctor. If you experience changes in the frequency or severity of seizures after initiating this medication, notify your doctor promptly.

This medication may cause drowsiness and reduced alertness, increasing the risk of falls, particularly in older adults. If you have concerns, discuss them with your doctor. Do not alter the dosage or discontinue this medication without consulting your doctor, as this may lead to seizures.

If you are taking this medication long-term, your doctor may recommend regular blood tests to monitor your condition. Prolonged use or high doses of this medication may result in tolerance, reducing its effectiveness. If you suspect this medication is no longer working as intended, contact your doctor. Avoid exceeding the prescribed dose.

Some formulations of this medication may contain benzyl alcohol. If possible, avoid products containing benzyl alcohol in newborns and infants, as high doses can cause serious side effects, particularly when combined with other medications containing benzyl alcohol. Consult your doctor to determine if this product contains benzyl alcohol.

If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects. Similarly, if the patient is a child, exercise caution when administering this medication, as the risk of certain side effects may be higher in this population.

This medication may pose a risk to the unborn baby if taken during pregnancy. If you become pregnant or are already pregnant while taking this medication, notify your doctor immediately. Taking this medication late in pregnancy may increase the risk of respiratory or feeding problems, low body temperature, or withdrawal symptoms in the newborn. Discuss the potential risks with your doctor.
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Overdose Information

Overdose Symptoms:

  • Extreme drowsiness
  • Confusion
  • Slurred speech
  • Slowed reflexes
  • Lack of coordination
  • Profound sedation
  • Respiratory depression (slow or stopped breathing)
  • Hypotension
  • Coma

What to Do:

Seek immediate medical attention. Call 911 or Poison Control at 1-800-222-1222. Overdose may require supportive care, including respiratory support, and potentially administration of flumazenil (a benzodiazepine antagonist), though flumazenil carries risks, especially in patients with chronic benzodiazepine use or seizure disorders.

Drug Interactions

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Contraindicated Interactions

  • Strong CYP3A4/2C19 inhibitors (e.g., fluvoxamine, ketoconazole, itraconazole, voriconazole, cimetidine, fluoxetine, omeprazole) - relative contraindication, requires significant dose reduction and close monitoring.
  • Opioids (concomitant use is a Black Box Warning, not an absolute contraindication but requires extreme caution and avoidance if possible).
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Major Interactions

  • Other CNS depressants (e.g., alcohol, barbiturates, other benzodiazepines, tricyclic antidepressants, antihistamines, antipsychotics, general anesthetics) - increased risk of profound sedation, respiratory depression, coma, and death.
  • CYP3A4/2C19 inhibitors (e.g., diltiazem, verapamil, grapefruit juice) - increased diazepam levels.
  • CYP3A4/2C19 inducers (e.g., rifampin, carbamazepine, phenytoin) - decreased diazepam levels.
  • Phenytoin - variable effect on phenytoin levels (increase or decrease).
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Moderate Interactions

  • Digoxin - may increase digoxin levels.
  • Levodopa - may decrease levodopa efficacy.
  • Theophylline - may antagonize sedative effects of diazepam.
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Minor Interactions

  • Not available

Monitoring

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Baseline Monitoring

Respiratory rate, heart rate, blood pressure

Rationale: To establish baseline vital signs and assess for pre-existing respiratory compromise.

Timing: Prior to administration.

Level of consciousness/Sedation score (e.g., Ramsay Sedation Scale)

Rationale: To establish baseline mental status and guide titration.

Timing: Prior to administration.

Liver function tests (ALT, AST, bilirubin)

Rationale: Diazepam is extensively metabolized by the liver; baseline assessment is important, especially in patients with suspected hepatic impairment or for long-term use.

Timing: Prior to initiation, if clinically indicated.

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Routine Monitoring

Respiratory rate, oxygen saturation

Frequency: Every 5-15 minutes during acute administration and for several hours post-administration, then as clinically indicated.

Target: Respiratory rate: 12-20 breaths/min; SpO2: >92-94%

Action Threshold: Respiratory rate <10 breaths/min, SpO2 <90%, or signs of respiratory distress; administer oxygen, consider reversal agent (flumazenil) if appropriate, provide ventilatory support.

Blood pressure, heart rate

Frequency: Every 5-15 minutes during acute administration and for several hours post-administration, then as clinically indicated.

Target: Within patient's normal range.

Action Threshold: Significant hypotension or bradycardia; provide supportive care.

Level of consciousness/Sedation score

Frequency: Every 5-15 minutes during acute administration and for several hours post-administration, then as clinically indicated.

Target: Desired level of sedation (e.g., calm, drowsy but arousable).

Action Threshold: Excessive sedation (e.g., unarousable, stupor); reduce dose, consider reversal agent (flumazenil) if appropriate.

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Symptom Monitoring

  • Excessive sedation
  • Respiratory depression (slow, shallow breathing)
  • Hypotension
  • Paradoxical reactions (agitation, hallucinations, aggression, especially in pediatric or elderly patients)
  • Signs of withdrawal (anxiety, insomnia, tremors, seizures) if abruptly discontinued after prolonged use.

Special Patient Groups

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Pregnancy

Category D. Avoid use during pregnancy, especially during the first trimester and near term, due to potential risks to the fetus and neonate.

Trimester-Specific Risks:

First Trimester: Increased risk of congenital malformations (e.g., cleft lip/palate) if used during the first trimester, though data are conflicting.
Second Trimester: Potential for fetal CNS depression and growth restriction with prolonged use.
Third Trimester: Risk of 'floppy infant syndrome' (hypotonia, lethargy, feeding difficulties, hypothermia, respiratory depression) if used near term. Risk of neonatal withdrawal syndrome (irritability, hypertonia, tremors, feeding difficulties, seizures) if used chronically during pregnancy.
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Lactation

Excreted into breast milk. Use with caution. Monitor breastfed infant for sedation, poor feeding, and weight gain.

Infant Risk: L3 (Moderately Safe). Potential for infant sedation, lethargy, and poor feeding. Long half-life of diazepam and its active metabolites can lead to accumulation in the infant. Consider alternative agents or monitor infant closely.
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Pediatric Use

Use with extreme caution, especially in neonates and infants, due to increased risk of respiratory depression and paradoxical reactions (e.g., hyperactivity, agitation). Dosing must be carefully calculated based on weight and age. Not recommended for routine anxiety in children.

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Geriatric Use

Increased sensitivity to the sedative and respiratory depressant effects. Reduced metabolism and elimination lead to prolonged half-life and accumulation. Start with lower doses (e.g., 50% of adult dose) and titrate slowly. Increased risk of falls, cognitive impairment, and paradoxical reactions.

Clinical Information

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Clinical Pearls

  • IV administration should be performed slowly (max 5 mg/min) into a large vein to minimize the risk of venous irritation, thrombophlebitis, and hypotension.
  • IM administration is not preferred for acute indications (e.g., status epilepticus) due to slow and erratic absorption.
  • Diazepam injection contains propylene glycol and ethanol, which can cause adverse effects (e.g., metabolic acidosis, hyperosmolarity, renal dysfunction) with high doses or prolonged infusions, especially in neonates or patients with renal impairment.
  • Tolerance, physical dependence, and withdrawal symptoms can occur with prolonged use. Tapering is necessary upon discontinuation.
  • Paradoxical reactions (e.g., agitation, aggression, hallucinations) can occur, especially in children, elderly, or patients with psychiatric disorders.
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Alternative Therapies

  • For anxiety: Buspirone, SSRIs, SNRIs, hydroxyzine.
  • For status epilepticus: Levetiracetam, fosphenytoin, valproic acid (non-benzodiazepine anticonvulsants).
  • For muscle spasm: Baclofen, tizanidine, cyclobenzaprine (other skeletal muscle relaxants).
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Cost & Coverage

Average Cost: Varies widely, typically $5-$50 per 10ml vial (50mg)
Generic Available: Yes
Insurance Coverage: Generally covered by most insurance plans as a Tier 1 or Tier 2 generic medication.
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General Drug Facts

If your symptoms or health problems persist or worsen, it is essential to contact your doctor promptly. To ensure safe use, never share your medication with others, and do not take medication prescribed for someone else. Store all medications in a secure location, out of reach of children and pets, to prevent accidental ingestion. Dispose of unused or expired medications properly. Unless instructed otherwise, do not flush medications down the toilet or pour them down the drain. If you are unsure about the correct disposal method, consult your pharmacist for guidance. Many communities offer drug take-back programs, which can be a safe and convenient way to dispose of unwanted medications.

This medication is accompanied by a Medication Guide, a patient fact sheet that provides important information about its use. Read this guide carefully when you first receive your medication, and review it again each time your prescription is refilled. If you have any questions or concerns about your medication, discuss them with your doctor, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately contact your local poison control center or seek emergency medical attention. Be prepared to provide information about the medication taken, the amount, and the time it was taken, as this will help healthcare professionals provide appropriate care.