Diazepam; Uses, Dosage, Side Effects, Interactions, Pregnancy

Diazepam








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Diazepam is a benzodiazepine derivative with anti-anxiety, sedative, hypnotic and anticonvulsant properties. Diazepam potentiates the inhibitory activities of gamma-aminobutyric acid (GABA) by binding to the GABA receptor, located in the limbic system and the hypothalamus. This increases the frequency of chloride channel opening, allowing the flow of chloride ions into the neuron and ultimately leading to membrane hyperpolarization and a decrease in neuronal excitability.

A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of gamma-aminobutyric acid activity. It is used in the treatment of severe anxiety disorders, as a hypnotic in the short-term management of insomnia, as a sedative and premedicant, as an anticonvulsant, and in the management of alcohol withdrawal syndrome

Mechanism of Action of Diazepam

Benzodiazepines bind nonspecifically to benzodiazepine receptors which mediate sleep, affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.

Indications of Diazepam

Contra-Indications of Diazepam

  • low amount of albumin proteins in the blood
  • Alcohol Intoxication
  • drug abuse
  • Depression
  • Myasthenia Gravis
  • Wide-Angle Glaucoma
  • closed angle glaucoma
  • Severe Chronic Obstructed Lung Disease
  • Decreased Lung Function
  • Lung Disease
  • Liver Problems
  • Severe Liver Disease
  • Severe Renal Impairment
  • Temporarily Stops Breathing While Sleeping
  • Pregnancy
  • A Mother who is Producing Milk and Breastfeeding

Dosage of Diazepam

Strengths: 2 mg, 2.5 mg 5 mg, 10 mg, 15 mg, 20 mg, 5 mg/5 mL, 5 mg/mL;

Anxiety

  • 2 to 10 mg orally 2 to 4 times a day

Parenteral

  • Moderate Anxiety Disorders and Symptoms: 2 to 5 mg IM or IV, repeated in 3 to 4 hours if necessary
  • Severe Anxiety Disorders and Symptoms: 5 to 10 mg IM or IV, repeated in 3 to 4 hours if necessary

Muscle Spasm

  • 2 to 10 mg orally 3 to 4 times a day

Parenteral

  • 5 to 10 mg IM or IV, then 5 to 10 mg IM or IV in 3 to 4 hours if necessary

Alcohol Withdrawal

  • Initial dose: 10 mg orally 3 to 4 times a day for the first 24 hours
  • Maintenance dose: 5 mg orally 3 to 4 times a day as needed

Parenteral

  • 10 mg IM or IV once, then 5 to 10 mg IM or IV in 3 to 4 hours if necessary

Seizures

  • 2 to 10 mg orally 2 to 4 times a day

Rectal

  • Initial dose: 0.2 mg/kg rectally, rounded upward to the next available dose. A 2.5 mg rectal dose may be given as a partial replacement if patients expel a portion of the initial dose
  • If necessary, a second dose of 0.2 mg/kg may be given rectally 4 to 12 hours after the first dose.
  • Maximum Frequency: May be used to treating up to 1 seizure episode every 5 days, and no more than 5 episodes/month

Endoscopy or Radiology Premedication

  • Cardioversion: 5 to 15 mg IV once 5 to 10 minutes before the procedure

Endoscopic Procedures

  • IV: Usually less than 10 mg, but some patients require up to 20 mg IV, especially when narcotics are omitted
  • IV titration: The IV dose should be titrated to desired sedative response (e.g., slurring of speech) with slow administration immediately before the procedure.
  • IM: 5 to 10 mg IM once 30 minutes prior to the procedure

Status Epilepticus

Parenteral

  • Initial dose: 5 to 10 mg IV once, repeated at 10 to 15-minute intervals to a maximum dose of 30 mg if necessary

Side Effects of Diazepam

The most common

Common

Rare

Drug  Interactions of Diazepam

Diazepam may interact with following drugs, supplements, & may change the efficacy of drugs

Pregnancy & Lactation of Diazepam

FDA Pregnancy Category D

Pregnancy

You should not take Diazepam tablets if you are pregnant, planning to become pregnant or are breastfeeding. If you take Diazepam tablets late in your pregnancy or during labor your baby might have a low body temperature, floppiness, and breathing difficulties. If taken regularly during late pregnancy, your baby may develop withdrawal symptoms. Ask your doctor or pharmacist for advice before taking any medicine.

Breastfeeding 

The milk to plasma ratio ranged between 0.2 and 2.7. This drug may accumulate in breastfed infants, especially with repeated dosing or with acute use of rectal gel formulations.

Use is not recommended and a decision should be made to discontinue breastfeeding or discontinue the drug, taking into account the importance of the drug to the mother. Excreted into human milk.

References

 

Diazepam

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