Valium (Diazepam)

VALIUM® ROCHE® INJECTION

Roche

Diazepam

Anxiolytic – Sedative

Action And Clinical Pharmacology: Diazepam is an anxiolytic-sedative drug useful in the symptomatic relief of anxiety and tension states. It has also adjunctive value in the relief of certain neurospastic conditions and in certain cases, its anticonvulsant activity has been found useful in controlling status epilepticus.

Peak blood levels after the i.v. administration of diazepam injection are reached within 15 minutes as compared to 1 hour after a single oral dosing and are of the same magnitude. The acute half-life is 2 to 3 hours with a slower decline thereafter, possibly due to tissue storage. Repeated doses further increase blood levels. In humans, comparable blood levels of diazepam injection were obtained in maternal and cord blood indicating rapid placental transfer of the drug.

Indications And Clinical Uses: In the symptomatic management of mild to moderate degrees of anxiety in conditions dominated by tension, excitation, agitation, fear or aggressiveness, such as may occur in: psychoneurosis; anxiety reactions due to stressful conditions; and anxiety states with somatic expression.

Diazepam is indicated parenterally when a rapid response is desired and has been found useful: in acute anxiety or tension states related to stressful conditions or non-psychotic emotional disorders; to alleviate the symptoms of acute alcoholic withdrawal, including delirium tremens; as an adjunct in relieving anxiety states that may be present before minor surgical procedures or prior to esophagoscopy and gastroscopy (when used under conditions in which resuscitative measures are available); to control prolonged seizure activity (status epilepticus) including severe recurrent seizures (see Precautions); for the relief of muscle spasm in cerebral palsy, athetosis, the rare stiff man syndrome and adjunctively in tetanus; as premedication for relief of anxiety states prior to surgical procedures (i.m. route) or cardioversion (i.v. route).

Contra-Indications: Myasthenia gravis, infants, known hypersensitivity to the drug. tag_WarningWarnings

Manufacturers’ Warnings In Clinical States: Diazepam injection should not be administered to patients in shock or coma. Rare reports of apnea or cardiac arrest have been noted, usually following i.v. administration, especially in elderly or very ill patients and those with limited pulmonary reserve. Duration is generally brief. Resuscitative facilities should be available. Since lingual obstruction of the airway may occur, particularly in children and in the elderly, caution is required to maintain a free airway in patients receiving diazepam.

Rapid injection or the use of veins with too small a lumen carries the risk of thrombophlebitis. I.V. injection should be directly into a large lumen vessel, such as an antecubital vein, and the ampul solution should be administered slowly (e.g. 5 mg/minute).

Intra-arterial injection must be carefully avoided on account of the danger of necrosis.

Diazepam should not be diluted with parenteral fluids. One exception is when it is considered essential to administer it in a large volume of fluids (see i.v. Infusion under Dosage).

Do not mix or dilute diazepam injection with other solutions or drugs.

Precautions: Geriatrics: Elderly and debilitated patients and those with organic brain disorders have been found to be prone to CNS depression following even low doses. For these patients diazepam injection should be used with caution and in low doses to preclude development of ataxia, sedation or other possible adverse effects.

Emotional Disorders: Diazepam is not recommended in the treatment of psychotic or severely depressed patients. Precautions are indicated for severely depressed patients or those who show any evidence of impending depression, particularly the recognition that suicidal tendencies may be present and protective measures may be necessary.

Since excitement and other paradoxical reactions may result from the use of the drug in psychotic patients, it should not be used in ambulatory patients suspected of having psychotic tendencies.

Pregnancy: Diazepam injection should not be used during the first trimester of pregnancy except if absolutely necessary.

Obstetrics: The safety and efficacy in obstetrics have not yet been established.

Use before Bronchoscopy and Laryngoscopy: Since there are insufficient data available to establish the safety of diazepam prior to bronchoscopy and laryngoscopy, its use is not recommended.

Use before Gastroscopy, Esophagoscopy, Cardioversion and Surgical Procedures: Diazepam should be used only under conditions in which safeguards are available should laryngospasm and circulatory or respiratory depression occur. Concurrent use of narcotics and barbiturates with diazepam may produce a potentiation of effect and, when such combinations are used, appropriate reduction of dosage is required.

Use in Status Epilepticus: Diazepam is not recommended as a substitute for standard anticonvulsant medication in the long-term control of epilepsy. Appropriate anticonvulsant therapy should be instituted or continued when necessary, as soon as possible after interruption of the status epilepticus. Although diazepam is used to control status epilepticus, it may occasionally induce or aggravate seizures in some patients with convulsive disorders.

Potentiation of Drug Effects: Careful consideration should be given if diazepam is to be combined with other psychotropic agents (phenothiazines, barbiturates, MAO inhibitors and other antidepressants) because the pharmacological action of these agents might potentiate the action of diazepam.

Patients should be advised to abstain from alcohol during treatment with diazepam.

In view of possible adverse reactions and potentiation of effects, patients should be advised to abstain from CNS depressant drugs during treatment with diazepam.

Drug Dependence: Abrupt cessation of large doses of diazepam after prolonged periods may precipitate acute withdrawal symptoms and, in these cases, the drug should be discontinued gradually. Caution should be exercised when it is considered necessary to administer diazepam to addiction-prone individuals.

Interference with Serum Creatinine Phosphokinase Determinations: As with a number of other i.m. dosage forms, i.m. administration of diazepam (but not oral or i.v. administration), can lead to a rise in serum creatinine phosphokinase activity. A maximum level is usually noticed between 12 and 24 hours after i.m. injection. These elevated readings should be taken into account in the event of differential diagnosis of myocardial infarction.

Occupational Hazards: General: After parenteral administration, ambulation should be delayed at least 1 or 2 hours or until complete alertness is restored. Patients receiving diazepam should be advised to proceed cautiously wherever mental alertness and physical co-ordination are required.

The usual precautions in treating patients with impaired renal and hepatic functions should be observed. If diazepam is administered for protracted periods, periodic blood counts and liver function tests may be advisable.

Adverse Reactions: The most common adverse effects reported are drowsiness and ataxia.

Other reactions noted less frequently are fatigue, dizziness, nausea, blurred vision, diplopia, vertigo, headache, slurred speech, tremors, hypoactivity, dysarthria, euphoria, impairment of memory, confusion, depression, incontinence or urinary retention, constipation, skin rash, generalized exfoliative dermatitis, hypotension, tachycardia, flushing, hematuria, changes in libido, pain at the site of injection and phlebitis following i.v. administration.

The more serious adverse reactions occasionally reported are leukopenia, jaundice, hypersensitivity and paradoxical reactions. Circulatory and respiratory depression may follow rapid i.v. administration.

Paradoxical reactions such as hyperexcited states, anxiety, excitement, hallucinations, increased muscle spasticity, insomnia, rage, as well as sleep disturbances and stimulation, have been reported: should these occur, the drug should be discontinued.

Minor changes in EEG patterns have been observed in patients on diazepam therapy. These changes consist of low to moderate voltage fast activity, 20 to 30 cycles/second and are of no known significance.

In animals, i.m. administration has produced localized irritation of tissue at injection sites and some thickening of veins after i.v. use. A mild hemolytic effect was observed in in vitro and in vivo tests in dogs.

Symptoms And Treatment Of Overdose: Symptoms and Treatment: The main symptoms of overdosage are drowsiness, oversedation and ataxia. When the effects of the drug overdosage begin to wear off, the patient exhibits some jitteriness and overstimulation. The cardinal manifestations of overdosage are drowsiness and confusion, reduced reflexes and coma. There are minimum effects of respiration, pulse and blood pressure unless the overdosage is extreme.

Gastric lavage may be beneficial if performed soon after oral ingestion. If necessary, a CNS stimulant such as caffeine or methylphenidate may be administered with caution. Supportive measures should be instituted as indicated: maintenance of an adequate airway, levarterenol for hypotension. Dialysis appears to be of little value.

Dosage And Administration: Valium Roche Injection is used without diluent for both the i.m. and i.v. routes. The i.m. route should be preferred whenever the indication and urgency of the clinical situation permit. The i.m. route is indicated when diazepam injection is used as premedication to relieve anxiety states prior to surgical procedures (usually 30 to 45 minutes before the procedure. The i.v. route is indicated when diazepam injection is used prior to cardioversion.

While dosage should be individualized for maximum beneficial effect, as a general rule the usual dose for both the i.v. and i.m. routes is:

Acute anxiety or tension states related to stressful conditions or nonpsychotic emotional disorders: 2 to 10 mg i.m. or i.v. Repeat in 3 to 4 hours, if necessary.

Acute alcoholic withdrawal: To alleviate the symptoms of acute alcoholic withdrawal including delirium tremens: 10 mg i.m. or i.v. initially, then 5 to 10 mg in 3 to 4 hours, if necessary.

Minor surgical procedures including esophagoscopy and gastroscopy: As an adjunct in relieving anxiety states that may be present before these procedures: 5 to 10 mg i.m. or i.v. approximately 30 minutes prior to procedures.

For the relief of muscle spasm in cerebral palsy, athetosis, the rare “stiff man syndrome” and adjunctively in tetanus: 5 to 10 mg i.m. or i.v. initially; then 5 to 10 mg in 3 to 4 hours, if necessary. For tetanus, larger doses may be required.

Status epilepticus including severe recurrent seizures: For the control of prolonged seizure activity: 5 to 10 mg i.v. (preferred route) initially. Repeat in 2 to 4 hours if necessary.

Premedication to surgical procedures: For the relief of anxiety states (if atropine, scopolamine or other premedication are desired, they must be administered in separate syringes): 10 mg i.m. (preferred route), 1 to 2 hours before surgery.

Cardioversion: To relieve anxiety and tension: 5 to 15 mg i.v. within 5 to 10 minutes prior to the procedure.

Children: Depending on age and severity of symptoms, 2 to 10 mg i.m. or i.v. or 1 mg/4.5 kg.

Elderly and debilitated: (see Precautions and Adverse Effects) 2 to 5 mg i.m. or i.v.

I.M.: Diazepam injection should be injected deeply into the muscle.

I.V.: Diazepam injection should be administered slowly, i.e., 5 mg/minute.

In acute conditions, the injection may be repeated within 1 hour although an interval of 3 to 4 hours is usually satisfactory. Generally not more than 30 mg should be given in an 8 hour period.

I.V. Infusion: (see Warnings). Not more than 40 mg (8 mL of ampul solution) should be added to 500 mL of infusion solution (normal saline or 5% dextrose in water). The solution should be freshly made up and used within 6 hours.

Over 50% of the diazepam in the infusion solution may be adsorbed onto the walls of plastic containers. Therefore, only infusion solutions in glass containers can be administered.

Adsorption onto plastic drip tubing causes an initial significant and variable reduction (up to 40% or more) of delivered diazepam concentration which then gradually rises over the next few hours. The drip rate should be frequently titrated against the patient’s condition.

Bolus allows a more accurate and rapid titration of dosage than slow i.v. infusion. It is therefore to be preferred in the management of acute problems.

Availability And Storage: Each mL contains: diazepam 5 mg. Nonmedicinal ingredients: benzoic acid, benzyl alcohol, ethanol, propylene glycol, sodium benzoate and sodium hydroxide. Sodium:

VALIUM® ROCHE® INJECTION Roche Diazepam Anxiolytic – Sedative

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