Dosing and uses of ProSom (estazolam)
Adult dosage forms and strengths
tablet: Schedule IV
- 1mg
- 2mg
Insomnia
1-2 mg PO qHs
Hepatic Impairment
Use caution; dose adjustment may be necessary
Pediatric dosage forms and strengths
Safety & efficacy not established
Geriatric dosage forms and strengths
Initial dose: 0.5 mg PO qDay in small elderly patients; healthy patients may receive 1 mg
ProSom (estazolam) adverse (side) effects
>10%
Somnolence (42%)
Headache (16%)
Asthenia (11%)
Neuromuscular & skeletal weakness
1-10%
Dizziness (7-8%)
Hypokinesia (7-8%)
Abnormal coordination (4%)
Hangover (3%)
Abnormal thinking (2%)
Flushing palpitation
Hangover effect
Euphoria
Hostility
Seizure
Sleep disorder
Rash
Urticaria
<1%
Angioedema
Sleep-driving (sleep-cooking, sleep eating, etc) may occur
Muscle spasm
Fever
Neck pain
Myalgia
Drug dependence may occur
Warnings
Contraindications
Documented hypersensitivity
Acute alcohol intoxication
Myasthenia gravis (allowable in limited circumstances)
Narrow angle glaucoma (questionable)
Severe respiratory depression
Depressed neuroses, psychotic reactions
IV use in shock, coma, depressed respiration, patients who recently received other respiratory depressants
Cautions
Use caution in respiratory diseases, sleep apnea, renal/hepatic disease, open-angle glaucoma (questionable), impaired gag reflex, clinical depression, suicide ideation, patients receiving other CNS depressants concurrently
Use caution in patients with history of drug abuse or acute alcoholism; tolerance, psychological and physical dependence may occur with prolonged use
Anterograde amnesia
May cause CNS depression that impairs mental and physical abilities
Hyperactive or aggressive behavior may occur
May impair ability to perform hazardous tasks
Pregnancy and lactation
Pregnancy category: X
Lactation: Enters breast milk/contraindicated
Minor tranquilizers should be avoided in 1st trimester of pregnancy due to increased risk of congenital malformations
Maternal use shortly before delivery is associated with floppy infant syndrome (good and consistent evidence)
Prenatal benzodiazepine exposure slightly increased oral cleft risk (limited or inconsistent evidence)
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of ProSom (estazolam)
Mechanism of action
Depresses all levels of CNS (eg, limbic and reticular formation), possibly by increasing membrane permeability to chloride ions, which in turn increases the inhibitory activity of GABA on neuronal excitability.
Pharmacokinetics
Half-Life: 10-24 hr
Duration: Variable
Peak Plasma Time: 0.5-1.6 hr
Protein Bound: 93%
Metabolism: Hepatic
Metabolites: Inactive
Excretion: Urine
Half-life elimination: 10-24 h, and peak action is 2 h
