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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 Caucasian 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 only)

Derm: rash

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

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 only), 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, Valium, Valtoco

Contr. Subst. Schedule

Schedule IV (C-IV)

Code

NDC Code