Diazepam – Mechanism of Action

Dosage Forms & Strengths

tablet: Schedule IV

  • 2mg
  • 5mg
  • 10mg

oral solution: Schedule IV

  • 1mg/1mL
  • 5mg/mL

rectal gel (Diastat Acudial): Schedule IV

  • 2.5mg/0.5mL
  • 10mg/2mL
  • 20mg/4mL

injectable solution: Schedule IV

  • 5mg/mL

intramuscular device: Schedule IV

  • 5mg/mL

intranasal spray (Valtoco): Schedule IV

  • 5mg/0.1mL
  • 7.5mg/0.1mL
  • 10mg/0.1mL
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Anxiety

Indicated for management of anxiety disorders or for short-term relief of the symptoms of anxiety

2-10 mg PO q6-12hr, OR

2-5 mg IV/IM q3-4hr if necessary, for moderate anxiety disorders; 5-10 mg IV/IM q3-4hr for severe anxiety disorders

Alcohol Withdrawal

Aid in symptomatic relief of acute agitation, tremor, impending or acute delirium tremens, hallucinations

10 mg PO q6-8hr during first 24hr; reduce to 5 mg PO q6-8hr PRN OR

10 mg IV/IM, initially may give additional doses of 5-10 mg IV q6-8hr as needed

Endoscopic Precedures

Adjunct use, if apprehension, anxiety or acute stress reactions present prior to endoscopic procedures

≤10 mg adequate; may give up to 20 mg IV, particularly when concomitant narcotics omitted; if IV cannot be used, 5-10 mg IM approximately 30 min prior to procedure

Titrate IV dosage to desired sedative response, such as slurring of speech, with slow administration immediately prior to procedure

Dosage of narcotics should be reduced by at least a third and in some cases may be omitted

Preoperative Sedation

If atropine, scopolamine or other premedications desired, they must be administered in separate syringes

10 mg (IM preferred) before surgery

Sedation in the ICU

5-10 mg IV 1-2 hours before surgery; 0.03-0.1 mg/kg q30min to 6hr

Muscle Spasm

May be used adjunctively for relief of skeletal muscle spasm due to reflex spasm to local pathology (eg, inflammation of the muscles or joints, secondary to trauma); spasm associated with local pathology, cerebral palsy, athetosis, stiff-man syndrome, or tetanus

2-10 mg PO q6-8hr PRN, OR

5-10 mg, IV/IM initially, THEN 5-10 mg q3-3hr, if necessary; administer larger doses for tetanus

Seizure Disorder

Indicated for acute treatment of intermittent, stereotypic episodes of frequent seizure activity (ie, seizure clusters, acute repetitive seizures) distinct from a patient’s usual seizure pattern

Used adjunctively in convulsive disorders, although it has not proved useful as the sole therapy

2-10 mg PO q6-12hr

Intranasal spray

  • 0.2 mg/kg intranasally as single dose
  • Adolescent or adult weight-based dosing
    • 14-27 kg: 5 mg (one 5-mg device); 1 spray in 1 nostril
    • 28-50 kg: 10 mg (one 10-mg device); 1 spray in 1 nostril
    • 51-75 kg: 15 mg (two 7.5-mg devices); 1 spray in each nostril
    • ≥76 kg: 20 mg (two 10-mg devices); 1 spray in each nostril
  • Second dose and maximum dose
    • Second dose: When required, may be administered after at least 4 hr after initial dose; if the second dose is administered, use a new blister pack of diazepam intranasal
    • Maximum dosage: Not to exceed 2 doses to treat a single episode
    • Treatment frequency: Do not use for more than 1 episode q5days and no more than 5 episodes/month

Diazepam gel (rectal)

  • 0.2 mg/kg PR or 10-20 mg as single dose
  • Rectal gel is measured in 2.5-mg increments from 2.5-20 mg/dose; calculate dose and round upward to next measurable dose
  • May prescribe second dose of diazepam rectal gel; when required, may be given 4-12 hr after first dose
  • Adolescent or adult weight-based dosing
    • 14-25 kg: 5 mg
    • 26-37 kg: 7.5 mg
    • 38-50 kg: 10 mg
    • 51-62 kg: 12.5 mg
    • 63-75 kg: 15 mg
    • 76-87 kg: 17.5 mg
    • 88-111 kg: 20 mg

Status Epilepticus

5-10 mg initially (IV preferred); injection may be repeated if necessary, at 10-15 minute intervals up to 30 mg maximum; may repeat in 2 to 4 hours if necessary; however, consider that residual active metabolites may persist

Use extreme caution in individuals with chronic lung disease or unstable cardiovascular status

Administer IV slowly; administer IM if IV administration impossible

OR

0.2-0.5 mg/kg PR; round up dose to nearest 2.5 mg increment; not to exceed 20 mg as single dose  

Cardioversion

5-15 mg IV within 5-10 min prior to procedure to relieve anxiety and tension and to reduce recall of procedure

Dosage Modifications

Renal impairment:

  • Oral: Data not available
  • No dose adjustment recommended unless administered for prolonged period; decrease dose in prolonged periods
  • Rectal gel: Not studied; use caution
  • Intranasal spray: Not studied

Hepatic impairment

  • Rectal gel: Not studied; use caution
  • Intranasal spray: Not studied
  • Prescribing information describes literature review showing diazepam 0.1-0.15 mg/kg IV had prolonged half-life by 2- to 5-fold in patients with alcoholic cirrhosis
  • Oral administration
    • Mild to moderate: Use with caution and consider dose adjustment; average half-life is increased in mild and moderate cirrhosis; average increase has been variously reported from 2-fold to 5-fold, with individual half-lives over 500 hr reported
    • Severe: Contraindicated

Dosing Considerations

Adjust dose periodically to reflect changes in patient’s age or weight

May use 2.5-mg dose as a partial replacement dose for patients who may expel a portion of first dose

Long-term (>4 months) effectiveness of diazepam has not been assessed by systematic clinical studies

Periodically reassess the efficacy for each patient

Once acute symptomatology has been properly controlled with diazepam injection, the patient may be placed on oral therapy if further treatment required

Discontinuation or dosage reduction

  • Use a gradual taper to discontinue diazepam tablets or reduce dosage to avoid withdrawal reactions
  • If any withdrawal reaction develops, consider pausing taper or increasing dose to previous tapered dosage level; subsequently decrease dose more slowly

Seizures (Orphan)

Intermittent use to control bouts of increased seizure activity or Dravet syndrome by various administrative routes

(بازدید 22 بار, بازدیدهای امروز 1 )

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