section name header

Pronunciation

dye-AZ-e-pam

Classifications

Therapeutic Classification: antianxiety agents, anticonvulsants, sedative/hypnotics, skeletal muscle relaxants (centrally acting)

Pharmacologic Classification: benzodiazepines

Indications

BEERS REMS


Action

  • Depresses the CNS, probably by potentiating GABA, an inhibitory neurotransmitter.
  • Produces skeletal muscle relaxation by inhibiting spinal polysynaptic afferent pathways.
  • Has anticonvulsant properties due to enhanced presynaptic inhibition.
Therapeutic effects:
  • Relief of anxiety.
  • Sedation.
  • Amnesia.
  • Skeletal muscle relaxation.
  • Decreased seizure activity.

Pharmacokinetics

Absorption: Rapidly absorbed from the GI tract. Absorption from IM sites may be slow and unpredictable. Well absorbed from rectal mucosa (90%) and nasal mucosa (97%). IV administration results in complete bioavailability.

Distribution: Widely distributed. Crosses the blood-brain barrier.

Metabolism/Excretion: Primarily metabolized in the liver via the CYP2C19 and CYP3A4 isoenzymes; the CYP2C19 isoenzyme exhibits genetic polymorphism; 5–20% of Asian patients and 3–5% of White and Black patients may be poor metabolizers and may have significantly diazepam concentrations and an risk of adverse effects. Some products of metabolism are active as CNS depressants.

Half-Life: Neonates: 50–95 hr; Infants (1 mo–2 yr): 40–50 hr; Children 2–12 yr: 15–21 hr; Children 12–16 yr: 18–20 hr; Adults: 20–50 hr (up to 100 hr for metabolites).

Time/Action Profile

( sedation)

ROUTEONSETPEAKDURATION
PO30–60 min1–2 hrup to 24 hr
IMwithin 20 min0.5–1.5 hrunknown
IV1–5 min15–30 min15–60 min
Rectal2–10 min1–2 hr4–12 hr

In status epilepticus, anticonvulsant duration is 15–20 min.

Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

CV: hypotension(IV)

Derm: rash

EENT: intraocular pressure, blurred vision, epistaxis(nasal spray), nasal congestion (nasal spray), nasal discomfort (nasal spray)

GI: constipation, diarrhea(may be caused by propylene glycol content in oral solution), nausea, vomiting.

Local: pain (IM), phlebitis(IV)

Metab: weight gain

Neuro: dizziness, drowsiness, lethargy, ataxia, depression, dysgeusia (nasal spray), hangover, headache, paradoxical excitation, slurred speech

Resp: RESPIRATORY DEPRESSION

Misc: physical dependence, psychological dependence, tolerance

Interactions

Drug-drug:

Drug-Natural Products:

Route/Dosage

Anxiety

Pre-Endoscopy

Pediatric Conscious Sedation for Procedures

Status Epilepticus/Acute Seizure Activity

Febrile Seizure Prophylaxis

Skeletal Muscle Relaxation

Alcohol Withdrawal

Availability

(Generic available)

Assessment

Lab Test Considerations:

Toxicity and Overdose:

Implementation

IV Administration:

Patient/Family Teaching

Evaluation/Desired Outcomes

US Brand Names

Diastat, Libervant, Valium, Valtoco

Contr. Subst. Schedule

Schedule IV (C-IV)

Code

NDC Code