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Diazepam

Brands and Forms

  • Valium
    • tablet: 2mg, 5mg, 10mg
  • Diazepam
    • oral solution: 1mg/ml
    • injection: 5mg/ml
  • Diastat
    • rectal gel: 2.5mg, 10mg, 15mg, 20mg

Uses of Diazepam

Diazepam is used to treat states of anxiety, restlessness, agitation, and insomnia that can occur in a variety of psychiatric conditions, especially Anxiety Disorders. It cen be effective as monotherapy (ie. it can be used on its own without other medications) for Generalized Anxiety Disorder, Panic Disorder and Social Phobia, though in clinical practice it is more common for Diazepam to be used in combination with other medications, and mainly in instances where extra help is needed to control symptoms of anxiety, restlessness, agitation, and insomnia.

In general medicine, Diazepam is also used as a muscle relaxant, as a treatment for seizure disorders, and to induce sedation during surgical procedures.

How Diazepam Works

Diazepam is a benzodiazepine. It enhances the effects of GABA in the central nervous system by binding to GABA-A channels and making these channels more receptive to the actions of the brain's naturally occurring GABA.

Diazepam tends to produce a clinical effect lasting about 6-12 hours.

Cautions when Using Diazepam

Regular Diazepam use over a period of a few weeks can lead to tolerance, dependence and abuse. Ideally, this medication should be avoided in individuals with histories of substance abuse, or else used only with very close monitoring by the prescribing physician.

Caution should be used when Diazepam is taken by elderly individuals, as this medication can cause memory and concentration difficulties as well as confusion in these individuals, and also make them more prone to falls.

Stopping Diazepam abruptly after long-term regular use can lead to serious and potentially life-threatening withdrawal symptoms.

Diazepam should not be used by individuals with obstructive sleep apnea, especially if positive airway pressure (C-PAP) treatments are not being used, as this could lead to prolonged periods of apnea. Use with caution in individuals with other kinds of respiratory disease.

Diazepam should not be combined with alcohol due to the risk of excessive CNS depression.

People should not drive or operate heavy machinery while taking Diazepam.

Diazepam should not be used by individuals with narrow angle-closure glaucoma.

Dosing of Diazepam

When used on an as-needed basis for episodic symptoms of anxiety, restlessness, agitation or insomnia, the recommended starting dose of Diazepam is 2-5mg. Higher doses should be used only if it is found that the initial dose is not effective. At any dose, this medication can be expected to produce its effects within 30min and to last for 6-12 hours.

When used to control symptoms of anxiety or restlessness throughout the day, the recommended starting dose is 10mg/day, given in divided doses twice daily. Depending on the clinical effects, the dose can be increased by as much as 10mg/day every 3 days. Usually 20mg/day is required, but in some cases as much as 60mg/day may be needed.

When wanted to stop Diazepam after it has been used regularly for a prolonged period, the dose should be tapered gradually over a period of a few weeks so as to prevent the occurence of withdrawal symptoms.

When wanting to switch Diazepam to a different benzodiazepine, please refer to the Benzodiazepine Equivalency Table for information on dose conversion.

Onset of action

Therapeutic effects are immediate.

Kidney impairment

Initial recommended dose is 2-2.5mg once or twice daily, to be increased gradually as needed.

Liver impairment

Initial recommended dose is 2-2.5mg once or twice daily, to be increased gradually as needed.

Side-effects of Diazepam

Below is a list of most of the reported side-effects of Diazepam. Most of these side-effects occur in only a minority of individuals, and many also resolve with time while the medication is continued.

Cardiovascular: bradycardia; tachycardia; hypertension; palpitations; edema; hypotension.

Central Nervous System: drowsiness; fatigue/tiredness; sedation; memory impairment; cognitive impairment; light-headedness; decreased libido; dysarthria; confusional state; abnormal coordination; unsteadiness; disturbed attention; disorientation, paresthesia; dyskinesia; talkativeness; abnormal dreams; lethargy; hypesthesia; hypersomnia; malaise; weakness; headache; dizziness; tremor; insomnia; nightmares.

Dermatologic: rash.

Eyes, Ears, Nose and Throat: blurred vision; hearing disturbances.

Gastrointestinal: constipation; diarrhea; dry mouth; coated tongue; nausea; anorexia; vomiting elevated liver enzymes; liver impairment (rare).

Genitourinary: incontinence; changes in libido; urinary retention.

Hematologic: blood dyscrasias (including agranulocytosis, anemia, thrombocytopenia, leukopenia, neutropenia).

Psychiatric: depressed mood; apathy; disinhibitted behavior; dissociative symptoms; irritability (usually from withdrawal); anxiety (usually from withdrawal); restlessness (usually from withdrawal); mania (very rare); psychosis (very rare).

Respiratory: respiratory depression.

Common side-effects of Diazepam

Somnolence, dizziness, unsteadiness, imparied coordination, slowed thinking and reaction time.

Rare but serious side-effects of note of Diazepam

  • Liver damage can occur in very rare cases.
  • Blood dyscrasias (including agranulocytosis, anemia, thrombocytopenia, leukopenia, neutropenia) can occur very rarely.
  • See cautions above.

Diazepam withdrawal

Individuals who take Diazepam regularly over a period of a few weeks are at risk of developing a withdrawal syndrome if they stop the medication abruptly. The severity of the withdrawal symptoms will be proportional to the size of the Diazepam dose that was being used on a regular basis. With heavy use, most of the following symptoms could occur:

In the first stages of this syndrome, the individual will experience tremors, autonomic hyperactivity (sweating, fever, elevated blood pressure, rapid heart rate), anxiety, agitation, nausea, vomiting, and insomnia.

If left untreated, the next symptoms to appear are confusion and disorientation, hallucinations (mainly visual ones, but also auditory, tactile and olfactory) and delusions.

Seizures and cardiovascular collapse can then ensue, and are the most concerning symptoms.

This syndrome is considered a medical emergency. The main treatment is to restart the Diazepam at the most recent dose.

To prevent this syndrome, the dose of the medication should be reduced gradually over a period of a few weeks.

Diazepam overdose

Hypotension, drowsiness, confusion, somnolence, impaired coordination, diminished reflexes, lethargy, ataxia, hypotonia, coma, respiratory or cardiac arrest. Can be fatal.

Diazepam and pregnancy

Category D: benzodiazepines such as Diazepam have been associated with a risk of less than 1% of causing cleft lip or palette to the fetus when used in pregnancy [ref]. A fetus exposed to benzodiazepines in utero is also at risk for developing a withdrawal syndrome shortly after birth, which would require medical treatment. Diazepam should only be used in pregnancy if clearly needed and if benefits outweigh potential risks.

Medical Monitoring for Diazepam

Individuals taking Diazepam over prolonged periods of time should have their liver functions and complete blood counts measured periodically.

Drug Interactions with Diazepam

  • Diazepam should not be combined with alcohol due to the risk of excessive CNS depression.
  • Use caution when combining Diazepam with other medications that can cause sedation or CNS depression.
  • The effects of Diazepam can be intensified by Cimetidine, disulfiram, and oral contraceptives
  • Diazepam blood concentrations can be increased by azole antifungal agents (Itraconazole, Ketoconazole), Diltiazem, Fluvoxamine, Isoniazid, macrolide antibiotics (Erythromycin), Omeprazole, Nefazodone, non-nucleoside reverse transcriptase inhibitors (Delavirdine, Efavirenz), and protease inhibitors (Indinavir).
  • Diazepam blood concentrations can be decreased by rifamycins.
  • Diazepam can increase blood concentrations of Digoxin.