dye az e POKS
Mitran® Oral; Reposans-10®
Medilium®; Novo-Poxide; Solium®|
Management of anxiety disorder or for the short-term relief of symptoms of
anxiety; withdrawal symptoms of acute alcoholism; and preoperative apprehension
Hypersensitivity to this drug or any component of its formulation
(cross-sensitivity with other benzodiazepines may exist); narrow angle glaucoma
(not in product labeling: however, benzodiazepines are contraindicated);
Active metabolites with extended half-lives may lead to delayed accumulation
and adverse effects. Use with caution in elderly or debilitated patients,
pediatric patients, patients with hepatic disease (including alcoholics) or
renal impairment. Use with caution in patients with respiratory disease or
impaired gag reflex. Use with caution in patients with porphyria.
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 (lithium, phenothiazines). Effects with
other sedative drugs or ethanol may be potentiated. 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.
Benzodiazepines have 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, fatigue, ataxia, lightheadedness, memory
impairment, dysarthria, irritability
Endocrine & metabolic: Decreased libido, menstrual disorders
Gastrointestinal: Xerostomia, decreased salivation, increased or decreased
appetite, weight gain or loss
Genitourinary: Micturition difficulties
1% to 10%:
Central nervous system: Confusion, dizziness, disinhibition, akathisia,
Gastrointestinal: Increased salivation
Genitourinary: Sexual dysfunction, incontinence
Neuromuscular & skeletal: Rigidity, tremor, muscle cramps
Respiratory: Nasal congestion
Symptoms of overdose include hypotension, respiratory depression, coma,
hypothermia, cardiac arrhythmias
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. Respiratory depression may not be
CYP3A3/4 enzyme substrate
Increased toxicity: 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, rifabutin, rifampin,
troleandomycin, valproic acid, verapamil may increase the serum level and/or
toxicity of alprazolam; monitor for altered benzodiazepine response
Refrigerate injection; protect from light; incompatible when mixed
with Ringer's solution, normal saline, ascorbic acid, benzquinamide, heparin,
phenytoin, promethazine, secobarbital
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.
Duration: 48 hours to 1 week
Distribution: Vd: 3.3 L/kg; crosses the placenta; appears in
Protein binding: 90% to 98%
Metabolism: Extensive in the liver to desmethyldiazepam (active and
Half-life: 6.6-25 hours; End-stage renal disease: 5-30 hours; Cirrhosis:
Time to peak serum concentration: Oral: Within 2 hours; I.M.: Results in
lower peak plasma levels than oral
Elimination: Very little excretion in urine as unchanged drug
<6 years: Not recommended
>6 years: Anxiety: Oral, I.M.: 0.5 mg/kg/24 hours divided every 6-8 hours
Oral: 15-100 mg divided 3-4 times/day
I.M., I.V.: Initial: 50-100 mg followed by 25-50 mg 3-4 times/day as needed
Preoperative anxiety: I.M.: 50-100 mg prior to surgery
Alcohol withdrawal symptoms: Oral, I.V.: 50-100 mg to start, dose may be
repeated in 2-4 hours as necessary to a maximum of 300 mg/24 hours
Dosing adjustment in renal impairment: Clcr <10
mL/minute: Administer 50% of dose
Hemodialysis: Not dialyzable (0% to 5%)
Dosing adjustment/comments in hepatic impairment: Avoid use
Alcohol: Additive CNS effects, avoid use
Respiratory and cardiovascular status, mental status, check for
Therapeutic: 0.1-3 mg/mL (SI: 0-10
mmol/L); Toxic: >23
|Dental Health: Local
No information available to require special precautions
Effects on Dental Treatment|
>10% of patients will experience dry mouth which disappears with cessation
of drug therapy
Oral: Take exactly as directed (do not increase dose or frequency); may cause
physical and/or psychological dependence. Do not use excessive alcohol or 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, lightheadedness, impaired coordination, dizziness, or
blurred vision (use caution when driving or engaging in tasks requiring
alertness until response to drug is known); 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); or altered
sexual drive or ability (reversible). Report persistent CNS effects (eg,
euphoria, confusion, increased sedation, depression); chest pain, palpitations,
or rapid heartbeat; muscle cramping, weakness, tremors, rigidity, or altered
gait; or worsening of condition. Pregnancy/breast-feeding precautions:
Do not get pregnant while taking this medication; use appropriate barrier
contraceptive measures. Breast-feeding is not recommended.
Raise bed rails; initiate safety measures; aid with
Capsule, as hydrochloride: 5 mg, 10 mg, 25 mg
Powder for injection, as hydrochloride: 100 mg
Tablet: 10 mg, 25 mg
"Blood Concentrations and Clinical Findings Following Overdose of Chlordiazepoxide Alone and Chlordiazepoxide Plus Ethanol,"
Clin Toxicol, 1984, 22(5):433-46.
Burkhart KK and Kulig KW,
"The Diagnostic Utility of Flumazenil (A Benzodiazepine Antagonist) in Coma of Unknown Etiology,"
Ann Emerg Med, 1990, 19(3):319-21.
Hicks R, Dysken MW, Davis JM, et al,
"The Pharmacokinetics of Psychotropic Medication in the Elderly: A Review," J
Clin Psychiatry, 1981, 42(10):374-85.
"Toxicity in a Case of Acute and Massive Overdose of Chlordiazepoxide and Its Correlation to Blood Concentration,"
J Toxicol Clin Toxicol, 1989, 27(1-2):117-27.
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.
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