|Diastat® Rectal Delivery System;
Diazemuls® Injection; Diazepam Intensol®; Dizac®
Injectable Emulsion; Valium® Injection; Valium®
|Apo®-Diazepam; Diazemuls®; E
Pam®; Meval®; Novo-Dipam; PMS-Diazepam;
Dental: Oral medication for preoperative dental anxiety; sedative component
in I.V. conscious sedation in oral surgery patients; skeletal muscle relaxant
Medical: Management of anxiety disorders; alcohol withdrawal symptoms;
skeletal muscle relaxant; convulsive disorders
Clinical effects on the fetus: Crosses the placenta. Oral clefts reported,
however, more recent data does not support an association between drug and oral
clefts; inguinal hernia, cardiac defects, spina bifida, dysmorphic facial
features, skeletal defects, multiple other malformations reported; hypotonia and
withdrawal symptoms reported following use near time of delivery
Breast-feeding/lactation: Crosses into breast milk
Clinical effects on the infant: Sedation; American Academy of Pediatrics
reports that USE MAY BE OF CONCERN.
Hypersensitivity to this drug or any component of its formulation
(cross-sensitivity with other benzodiazepines may exist); narrow angle glaucoma;
pregnancy; not for use in children <6 months of age (oral) or <30 days of
Diazepam has been associated with increasing the frequency of grand mal
seizures. Withdrawal has also been associated with an increase in the seizure
frequency. Use with caution with drugs which may decrease diazepam metabolism.
Use with caution in elderly or debilitated patients, patients with hepatic
disease (including alcoholics), or renal impairment. Active metabolites with
extended half-lives may lead to delayed accumulation and adverse effects. Use
with caution in patients with respiratory disease or impaired gag reflex.
Causes CNS depression (dose-related) resulting in sedation, dizziness,
confusion, or ataxia which may impair physical and mental capabilities. Patients
must be cautioned about performing tasks which require mental alertness (ie,
operating machinery or driving). Use with caution in patients receiving other
CNS depressants or psychoactive agents. Effects with other sedative drugs or
ethanol may be potentiated. The dosage of narcotics should be reduced by
approximately 1/3 when diazepam is added. Benzodiazepines have been associated
with falls and traumatic injury and should be used with extreme caution in
patients who are at risk of these events (especially the elderly).
Use caution in patients with depression, particularly if suicidal risk may be
present. Use with caution in patients with a history of drug dependence.
Benzodiazepines have been associated with dependence and acute withdrawal
symptoms on discontinuation or reduction in dose. Acute withdrawal, including
seizures, may be precipitated in patients after administration of flumazenil to
patients receiving long-term benzodiazepine therapy.
Diazepam has been associated with anterograde amnesia. Paradoxical reactions,
including hyperactive or aggressive behavior, have been reported with
benzodiazepines, particularly in adolescent/pediatric or psychiatric patients.
Does not have analgesic, antidepressant, or antipsychotic properties.
Central nervous system: Drowsiness, ataxia, amnesia, slurred speech,
paradoxical excitement or rage, fatigue, insomnia, memory impairment, headache,
anxiety, depression, vertigo, confusion
Endocrine & metabolic: Changes in libido
Gastrointestinal: Changes in salivation, constipation, nausea
Genitourinary: Incontinence, urinary retention
Local: Phlebitis, pain with injection
Neuromuscular & skeletal: Dysarthria, tremor
Ocular: Blurred vision, diplopia
Respiratory: Decrease in respiratory rate, apnea
Symptoms of overdose include somnolence, confusion, coma, hypoactive
reflexes, dyspnea, hypotension, slurred speech, impaired coordination
Treatment for benzodiazepine overdose is supportive. Rarely is mechanical
ventilation required. Flumazenil has been shown to selectively block the binding
of benzodiazepines to CNS receptors, resulting in a reversal of
benzodiazepine-induced CNS depression, but not respiratory depression.
CYP1A2 and 2C8 enzyme substrate, CYP3A3/4 enzyme substrate (minor), and
diazepam and desmethyldiazepam are CYP2C19 enzyme substrates
Cimetidine, ciprofloxacin, clarithromycin, clozapine, CNS depressants,
diltiazem, disulfiram, digoxin, erythromycin, ethanol, fluconazole, fluoxetine,
fluvoxamine, grapefruit juice, isoniazid, itraconazole, ketoconazole, labetalol,
levodopa, loxapine, metoprolol, metronidazole, miconazole, nefazodone,
omeprazole, phenytoin,protease inhibitors like amprenavir and ritonavir,
rifabutin, rifampin, troleandomycin, valproic acid, verapamil may increase the
serum level and/or toxicity of diazepam; monitor for altered benzodiazepine
Protect parenteral dosage form from light; potency is retained for up to 3
months when kept at room temperature; most stable at pH 4-8, hydrolysis occurs
at pH <3; do not mix I.V. product with other medications
Binds to stereospecific benzodiazepine receptors on the postsynaptic GABA
neuron at several sites within the central nervous system, including the limbic
system, reticular formation. Enhancement of the inhibitory effect of GABA on
neuronal excitability results by increased neuronal membrane permeability to
chloride ions. This shift in chloride ions results in hyperpolarization (a less
excitable state) and stabilization.
I.V. for status epilepticus:
Onset of action: Almost immediate
Duration: Short, 20-30 minutes
Absorption: Oral: 85% to 100%, more reliable than I.M.
Protein binding: 98%
Metabolism: In the liver
Parent drug: Adults: 20-50 hours, increased half-life in neonates, elderly,
and those with severe hepatic disorders
Active major metabolite (desmethyldiazepam): 50-100 hours, can be prolonged
Oral absorption is more reliable than I.M.
Conscious sedation for procedures: Oral: 0.2-0.3 mg/kg (maximum: 10 mg) 45-60
minutes prior to procedure
Sedation or muscle relaxation or anxiety:
Oral: 0.12-0.8 mg/kg/day in divided doses every 6-8 hours
I.M., I.V.: 0.04-0.3 mg/kg/dose every 2-4 hours to a maximum of 0.6 mg/kg
within an 8-hour period if needed
Infants 30 days to 5 years: I.V.: 0.05-0.3 mg/kg/dose given over 2-3 minutes,
every 15-30 minutes to a maximum total dose of 5 mg; repeat in 2-4 hours as
needed or 0.2-0.5 mg/dose every 2-5 minutes to a maximum total dose of 5
>5 years: I.V.: 0.05-0.3 mg/kg/dose given over 2-3 minutes every 15-30
minutes to a maximum total dose of 10 mg; repeat in 2-4 hours as needed
or 1 mg/dose given over 2-3 minutes, every 2-5 minutes to a maximum total
dose of 10 mg
Rectal: 0.5 mg/kg, then 0.25 mg/kg in 10 minutes if needed
Adolescents: Conscious sedation for procedures:
Oral: 10 mg
I.V.: 5 mg, may repeat with
dose if needed
Anxiety/sedation/skeletal muscle relaxation:
Oral: 2-10 mg 2-4 times/day
I.M., I.V.: 2-10 mg, may repeat in 3-4 hours if needed
Status epilepticus: I.V.: 5-10 mg every 10-20 minutes, up to 30 mg in an
8-hour period; may repeat in 2-4 hours if necessary
Rapid tranquilization of agitated patient (administer every 30-60 minutes):
Oral: 5-10 mg; average total dose for tranquilization: 20-60 mg
Elderly: Oral: Initial:
Anxiety: 1-2 mg 1-2 times/day; increase gradually as needed, rarely need to
use >10 mg/day
Skeletal muscle relaxant: 2-5 mg 2-4 times/day
Hemodialysis: Not dialyzable (0% to 5%); supplemental dose is not necessary
Dosing adjustment in hepatic impairment: Reduce dose by 50% in
cirrhosis and avoid in severe/acute liver disease
Alcohol: Additive CNS depression has been reported with benzodiazepines;
avoid or limit alcohol
Respiratory rate, heart rate, blood pressure with I.V.
Therapeutic: Diazepam: 0.2-1.5 mg/mL (SI: 0.7-5.3
mmol/L); N-desmethyldiazepam (nordiazepam): 0.1-0.5
mg/mL (SI: 0.35-1.8
False-negative urinary glucose determinations when using
|Dental Health: Local
No information available to require special precautions
Effects on Dental Treatment|
>10% of patients experience dry mouth or changes in
Take exactly as directed (do not increase dose or frequency); may cause
physical and/or psychological dependence. While using this medication, do not
use alcohol and other prescription or OTC medications (especially pain
medications, sedatives, antihistamines, or hypnotics) without consulting
prescriber. Maintain adequate hydration (2-3 L/day of fluids unless instructed
to restrict fluid intake). You may experience drowsiness, dizziness, or blurred
vision (use caution when driving or engaging in tasks requiring alertness until
response to drug is known); nausea, vomiting, loss of appetite, or dry mouth
(small frequent meals, frequent mouth care, chewing gum, or sucking lozenges may
help); constipation (increased exercise, fluids, or dietary fruit and fiber may
help). If medication is used to control seizures, wear identification that you
are taking an antiepileptic medication. Report CNS changes (confusion,
depression, increased sedation, excitation, headache, agitation, insomnia or
nightmares, dizziness, fatigue, or impaired coordination) or changes in
cognition; difficulty breathing or shortness of breath; changes in urinary
pattern; changes in sexual activity; muscle cramping, weakness, tremors, or
rigidity; ringing in ears or visual disturbances, excessive perspiration, or
excessive GI symptoms (cramping, constipation, vomiting, anorexia); worsening of
seizure activity, or loss of seizure control. Pregnancy/breast-feeding
precautions: Do not get pregnant while taking this medication; use
appropriate barrier contraceptive measures. Breast-feeding is not
Provide safety measures (ie, side rails, night light, and call button);
Gel, rectal delivery system (Diastat®):
Pediatric rectal tip (4.4 cm): 5 mg/mL (2.5 mg, 5 mg, 10 mg) [twin packs]
Adult rectal tip (6 cm): 5 mg/mL (10 mg, 15 mg, 20 mg) [twin packs]
Injection: 5 mg/mL (1 mL, 2 mL, 5 mL, 10 mL)
Dizac®: 5 mg/mL (3 mL)
Diazemuls®: 5 mg/mL (2 mL)
Solution, oral (wintergreen-spice flavor): 5 mg/5 mL (5 mL, 10 mL, 500 mL)
Solution, oral concentrate (Diazepam Intensol®): 5
mg/mL (30 mL)
Tablet: 2 mg, 5 mg, 10 mg
Klotz U, Avant GR, Hoyumpa A, et al,
"The Effects of Age and Liver Disease on the Disposition and Elimination of Diazepam in Adult Man,"
J Clin Invest, 1975, 55(2):347-59.
Marshall JD, Farrar HC, and Kearns GL,
"Diarrhea Associated With Enteral Benzodiazepine Solutions," J Pediatr,
Pomara N, Stanley B, Block R, et al,
"Increased Sensitivity of the Elderly to the Central Depressant Effects of Diazepam,"
J Clin Psychiatry, 1985, 46(5):185-7.
Reidenberg MM, Levy M, Warner H, et al,
"Relationship Between Diazepam Dose, Plasma Level, Age, and Central Nervous System Depression,"
Clin Pharmacol Ther, 1978, 23(4):371-4.
Rosman NP, Colton T, Labazzo J, et al,
"A Controlled Trial of Diazepam Administered During Febrile Illnesses to Prevent Recurrence of Febrile Seizures,"
N Engl J Med, 1993, 329(2):79-84.
Traeger SM and Haug MT 3d,
"Reduction of Diazepam Serum Half-Life and Reversal of Coma by Activated Charcoal in a Patient With Severe Liver Disease,"
J Toxicol Clin Toxicol, 1986, 24(4):329-37.
Votey SR, Bosse GM, Bayer MJ, et al,
"Flumazenil: A New Benzodiazepine Antagonist," Ann Emerg Med, 1991,
Zeltzer LK, Altman A, Cohen D, et al,
"Report of the Subcommittee on the Management of Pain Associated With Procedures in Children With Cancer,"
Pediatrics, 1990, 86(5 Pt 2):826-31.
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