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Drug Monographs
Treatment Regimens

Scientific Name:
LORAZEPAM
Brand Name(s):
Ativan

Drug Monograph

Pharmacology

Mechanism of Action

Benzodiazepines appear to potentiate the effect of gamma-aminobutyrate (GABA) (i.e., they facilitate inhibitory GABA neurotransmission) and other inhibitory transmitters by binding to specific benzodiazepine receptor sites.
Recent evidence suggest there are 2 benzodiazepine receptors, BZ1 and BZ2.
BZ1 is thought to be associated with sleep mechanisms.
BZ2 with memory, motor, sensory, and cognitive functions.
The activity of the benzodiazepines may involve the following sites:spinal cord (muscle relaxation); brain stem (anticonvulsant properties); cerebrellum (ataxia); limbic and cortical areas (emotional behavior);
Anxiolytic effects are distinct from nonspecific consequences of CNS depression (i.e. sedation and motor impairment).

Pharmacokinetics

Oral Absorption
90% to 93%
Distribution
highly lipid soluble; widely distributed in the body tissues; enters breast-milk; crosses the placenta
cross blood brain barrier? No information
Vd  ~1.5 L/kg 
PPB 85%
Metabolism
hepatic, simple 1-step inactivation, ~75% to the inactive lorazepam glucuronide; minor metabolite is 6-chloro-4-(O-chlorophenyl)-2,1-quinazolinone
Excretion
renally, ~65% to 80% appears in the urine as glucuronide; 1% exreted fecally
Urine: ~65% to 80% as glucuronide
Cl:  no information
t½  absorption: I.M.: 20 min; elimination: 10-20 hours (average: 12 hours); Lorazepam glucuronide: 15-18 hours

Side Effects

IMMEDIATE ONSET (hours to days)
   rare: cardiovascular: tachycardia, chest pain
   drowsiness, sedation, confusion
   xerostomia, constipation, diarrhea, nausea, vomiting
   blurred vision, dysarthria
EARLY ONSET  (days to weeks)
   increased or decreased appetite

Therapeutics

Approved Indications

• Short-term management of anxiety
OTHER ONCOLOGY USES (Not Approved)
Antiemetic for anxiety-related emesis associated with chemotherapy or radiotherapy

Routes

I.M.
I.V. (push or infusion)
oral
sublingual

IV Compatibility

no information

Dosing

Injection:
• Withdraw dose in syringe and add diluent to desired volume; invert syringe gently to mix contents.  Slow IV direct injection.
Oral:
• 0.5 mg to 2 mg po 15-30 minutes before chemotherapy (for antiemetic effects)
Sublingual:
• 0.5 mg to 2 mg SL 2-5 minutes before chemotherapy (for antiemetic effects)

Contraindications

hypersensitivity to lorazepam; comatose patient pregnancy patients with : pre-existing CNS depression, renal or hepatic impairment, narrow-angle glaucoma, severe uncontrolled pain, severe hypotension

Monitoring

Clinical Monitoring

NO RECOMMENDED TOXICITY RATINGS

Extravasation Hazard

No

Significant Interactions

may be cross-sensitivity with other benzodiazepines oral contraceptives (combination products) cigarette smoking levodopa, morphine, CNS-depressants, loxapine, MAO inhibitors, tricyclic antidepressants, antacids, rifampin, digoxin, scopolamine

Product Information

Commercial Product Description

Brand Name: Ativan® Green sublingual tablets with 0.5mg, white SL tablets with 1mg, blue SL tablets with 2mg Lorazepam Generic products White tablets with 0.5mg, 1mg, 2mg Lorazepam

Pharmaceutical Considerations

Tablets: 0.5 mg, 1 mg and 2 mg oral tablets; 0.5 mg, 1 mg and 2 mg sublingual tablets
Injection: 4mg/1mL vial

Note

HANDLING RISK LEVEL:

HAZARD RISK LEVEL 2
FDA Pregnancy Risk Factor D
• This drug must be handled using precautions outlined in CCNS Standard for Oral Systemic Therapy for Cancer
• Go to "Additional Information" tab (above) for links to CCNS Policies

Availability & Funding

Administrative Information (Nova Scotia)

CCNS Provincial Formulary Status- Community Level Take Home Prescription Pharmacare Formulary Status- Formulary



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