Apo-Lorazepam

Apo-Lorazepam

lorazepam

Manufacturer:

Apotex

Distributor:

Pharmaforte
Full Prescribing Info
Contents
Lorazepam.
Description
0.5 mg: Each tablet contains lorazepam 0.5 mg (500 μg). Energy: <1 kJ (0.15 kcal). Sodium: <1 mmol (0.1 mg). Gluten- and tartrazine-free.
1 mg: Each tablet lorazepam 1 mg. Energy: 1 kJ (0.3 kcal). Sodium: <1 mmol (0.2 mg). Gluten-and tartrazine-free.
Action
Pharmacotherapeutic Group: Anxiolytic-Sedative.
Pharmacology: Lorazepam is an active benzodiazepine with a depressant action on the CNS. It has anxiolytic and sedative properties which are of value in the symptomatic relief of pathologic anxiety in patients with anxiety disorders giving rise to significant functional disability but is not considered indicated in the management of trait anxiety.
Lorazepam is rapidly and completely absorbed after oral administration, reaching mean peak plasma levels at approximately 2 hours.
Lorazepam is rapidly conjugated to a glucuroride which has no demonstrable psychopharmacological activity and is excreted mainly in the urine. The serum half-life of the conjugate varied between 16 to 20 hours. Very small amounts of other metabolites and their conjugates have been isolated from urine and plasma.
Most of the drug (88%) is excreted in the urine, with 75% excreted as the glucuronide. At clinically relevant concentrations, approximately 85% of lorazepam is bound to plasma proteins.
Anterograde amnesia, a lack of recall of events during the period of drug action, has been reported and appears to be dose-related.
Indications/Uses
Lorazepam is useful for the short-term relief of manifestations of excessive anxiety in patients with anxiety neurosis.
Anxiety and tension associated with the stresses of everyday life usually do not require treatment with anxiolytic drugs.
Dosage/Direction for Use
The dosage must be individualized and carefully titrated in order to avoid excessive sedation or mental and motor impairment.
As with other anxiolytic sedatives, short courses of treatment should usually be the rule for the symptomatic relief of disability anxiety in psychoneurotic patients and the initial course of treatment should not last longer than 1 week without reassessment of the need for a limited extension. Initially, not more than 1 week's supply of the drug should be provided and automatic prescription renewals should not be allowed. Subsequent prescriptions, when required, should be limited to short courses of therapy.
Generalized Anxiety Disorder: Adults: 2 mg in divided doses of 0.5 and 1 mg or of 1 mg and 1 mg. The daily dosage should be carefully increased or decreased by 0.5 mg depending upon tolerance and response. The usual daily dosage is 2 to 3 mg. However, the optimal dosage may range from 1 to 4 mg daily in individual patients. Usually, a daily dosage of 6 mg should not be exceeded.
Geriatrics and Debilitated Patients: The initial daily dose should not exceed 0.5 mg and should be very carefully and gradually adjusted, depending upon tolerance and response.
Overdosage
Symptoms: With benzodiazepines, including lorazepam, symptoms of mild overdose include drowsiness, mental confusion and lethargy. In more serious overdoses, symptoms may include ataxia, hypotonia, hypotension, hypnosis, Stages I and III coma, and, very rarely death.
Treatment: In the case of an oral overdose, if vomiting has not occurred spontaneously and the patient is fully awake, emesis may be induced with ipecac syrup 20 to 30 mL. Gastric lavage should be instituted as soon as possible and 50 to 100 g of activated charcoal should be introduced to and left in the stomach.
General supportive therapy should be instituted as indicated. Vital signs and fluid balance should be carefully monitored. An adequate airway should be maintained and assisted respiration used as needed. With normally functioning kidneys, forced diuresis with i.v. fluids and electrolytes may accelerate elimination of benzodiazepines from the body. In addition, osmotic diuretics such as mannitol may be effective as adjunctive measures. In more critical situations, renal dialysis and exchange blood transfusions may be indicated. Published reports indicate that i.v. infusion of 0.5 to 4 mg of physostigmine at the rate of 1 mg/min may reverse symptoms and signs suggestive of central anticholinergic overdose (confusion, memory disturbance, visual disturbances, hallucinations, delirium); however, hazards associated with the use of physostigmine (i.e. induction of seizures) should be weighed against its possible clinical benefit.
Contraindications
In patients with myasthenia gravis or acute narrow angle glaucoma, and in those with known, hypersensitivity to benzodiazepines.
Warnings
Lorazepam is not recommended for use in depressive neurosis or in psychotic reactions. Because of the lack of sufficient clinical experience, lorazepam is not recommended for use in patients less than 18 years of age. It should not be used in children under 6 years of age. Since lorazepam has a CNS depressant effect, patients should be advised against the simultaneous use of other CNS depressant drugs. Patients should also be cautioned not to take alcohol during the administration of lorazepam because of the potentiation of effects that may occur.
Occupational hazards: Excessive sedation has been observed with lorazepam at standard therapeutic doses. Therefore, patients on lorazepam should be warned against engaging in hazardous activities requiring mental alertness and motor coordination, such as operating dangerous machinery or driving motor vehicles.
Pregnancy and Lactation: Safe use in pregnancy has not been established. Therefore, lorazepam is not recommended for use during pregnancy or lactation. Several studies have suggested an increased risk of congenital malformations associated with the use of the benzodiazepines, chlordiazepoxide and diazepam, and meprobamate, during the first trimester of pregnancy. Since lorazepam is also a benzodiazepine derivative, its administration is rarely justified in women of child-bearing potential. If the drug is prescribed to a woman of child-bearing potential, she should be warned to contact her physician regarding discontinuation of the drug if she intends to become or suspects that she is pregnant.
Special Precautions
Dependence Liability: Lorazepam should not be administered to individuals prone to drug abuse.
Caution should be observed in patients who are considered to have potential for psychological dependence. It is suggested that the drug should be withdrawn gradually if it has been used in high dosages.
Use in Mental and Emotional Disorders: Lorazepam is not recommended for the treatment of psychotic or depressed patients. Since excitement and other paradoxical reactions can result from the use of these drugs in psychotic patients, they should not be used in ambulatory patients suspected of having psychotic tendencies.
As with other anxiolytic-sedative drugs, lorazepam should not be used in patients with non-pathological anxiety. These drugs are also not effective in patients with characterological and personality disorders or those with obsessive-compulsive neurosis.
When using lorazepam, it should be recognized that suicidal tendencies may be present and that protective measures may be required.
Use in Patients with Impaired Renal or Hepatic Function: Since the liver is the most likely site of conjugation of lorazepam and since excretion of conjugated lorazepam (glucuronide) is a renal function, the usual precaution of carefully titrating the dose should be taken, should lorazepam be used in patients with mild to moderate hepatic or renal disease. In patients for whom prolonged therapy with lorazepam is indicated, periodic blood counts and liver function tests should be carried out.
Geriatrics: Elderly and debilitated patients, or those with organic brain syndrome, have been found to be prone to CNS depression after even low doses of benzodiazepines. Therefore, medication should be initiated with very low initial doses in these patients, depending on the response of the patient in order to avoid oversedation or neurological impairment.
Use In Pregnancy & Lactation
Safe use in pregnancy has not been established. Therefore, lorazepam is not recommended for use during pregnancy or lactation. Several studies have suggested an increased risk of congenital malformations associated with the use of the benzodiazepines, chlordiazepoxide and diazepam, and meprobamate, during the first trimester of pregnancy. Since lorazepam is also a benzodiazepine derivative, its administration is rarely justified in women of child-bearing potential. If the drug is prescribed to a woman of child-bearing potential, she should be warned to contact her physician regarding discontinuation of the drug if she intends to become or suspects that she is pregnant.
Adverse Reactions
The adverse reaction most frequently reported was drowsiness. Other reported adverse reactions are dizziness, weakness, fatigue and lethargy, disorientation, ataxia, anterograde amnesia, nausea, change in appetite, change in weight, depression, blurred vision and diplopia, psychomotor agitation, sleep disturbance, vomiting, sexual disturbance, headache, skin rashes, gastrointestinal, ear, nose and throat, musculo-skeletal and respiratory disturbances. Release of hostility and other paradoxical effects, such as irritability and excitability, are known to occur with the use of benzodiazepines. In addition, hypotension, mental confusion, slurred speech, oversedation and abnormal liver and kidney function tests and hematocrit values have been reported with these drugs.
Drug Interactions
If lorazepam is to be used together with other drugs acting on the CNS, careful consideration should be given to the pharmacology of the agents to be employed because of the possible potentiation of drug effects. The benzodiazepines, including lorazepam, produce CNS depressant effects when administered with such medications as barbiturates or alcohol.
Storage
Store in an air-tight container. Protect from light.
MIMS Class
ATC Classification
N05BA06 - lorazepam ; Belongs to the class of benzodiazepine derivatives anxiolytics. Used in the management of anxiety, agitation or tension.
Presentation/Packing
Tab 0.5 mg (white, round, identified APO on one side and 0.5 on the other side) x 500's. 1 mg (white, oblong, scored, identified APO 1) x 1000's.
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