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Diazepam is a benzodiazepine derivative. Chemically, diazepam is 7-chloro-1,3-dihydro-1-methyl-5-phenyl-2H-1,4-benzodiazepin-2-one. It is a colorless crystalline compound, insoluble in water and has a molecular weight of 284.74. The solution is clear, colorless to slightly yellow.
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In animals, diazepam appears to act on parts of the limbic system, the thalamus and hypothalamus, and induces calming effects. Diazepam, unlike chlorpromazine and reserpine, has no demonstrable peripheral autonomic blocking action, nor does it produce extrapyramidal side effects; however, animals treated with diazepam do have a transient ataxia at higher doses. Diazepam was found to have transient cardiovascular depressor effects in dogs. Long-term experiments in rats revealed no disturbances of endocrine function. Injections into animals have produced localized irritation of tissue surrounding injection sites and some thickening of veins after intravenous use.
Indications and Usage for Diazepam Injection
Valium Diazepam 10mg 2ml Injection By Roche is indicated for the management of anxiety disorders or for the short-term relief of the symptoms of anxiety. Anxiety or tension associated with the stress of everyday life usually does not require treatment with an anxiolytic.
In acute alcohol withdrawal, diazepam may be useful in the symptomatic relief of acute agitation, tremor, impending or acute delirium tremens and hallucinosis.
As an adjunct prior to endoscopic procedures if apprehension, anxiety or acute stress reactions are present, and to diminish the patient’s recall of the procedures. (See WARNINGS.)
Diazepam is a useful adjunct for the relief of skeletal muscle spasm due to reflex spasm to local pathology (such as inflammation of the muscles or joints, or secondary to trauma); spasticity caused by upper motor neuron disorders (such as cerebral palsy and paraplegia); athetosis; stiff-man syndrome; and tetanus.
Diazepam Injection is a useful adjunct in status epilepticus and severe recurrent convulsive seizures.
Diazepam is a useful premedication (the IM route is preferred) for relief of anxiety and tension in patients who are to undergo surgical procedures. Intravenously, prior to cardioversion for the relief of anxiety and tension and to diminish the patient’s recall of the procedure.
Valium Diazepam 10mg 2ml Injection By Roche is contraindicated in patients with a known hypersensitivity to this drug; acute narrow angle glaucoma; and open angle glaucoma unless patients are receiving appropriate therapy.
When we use intravenously, we undertake the following procedures to reduce the possibility of venous thrombosis, phlebitis, local irritation, swelling, and, rarely, vascular impairment; We inject the solution slowly, taking at least one minute for each 5 mg (1 mL) we give; do not use small veins, such as those on the dorsum of the hand or wrist; we take extreme care to avoid intra-arterial administration or extravasation.
Do not mix or dilute Diazepam Injection with other solutions or drugs in syringe or infusion flask. If it is not feasible to administer diazepam directly IV, You should inject it slowly through the infusion tubing as close as possible to the vein insertion.
Extreme care must be used in administering Diazepam Injection, particularly by the IV route, to the elderly, to very ill patients, and to those with limited pulmonary reserve because of the possibility that apnea and/or cardiac arrest may occur. Concomitant use of barbiturates, alcohol or other central nervous system depressants increases depression with increased risk of apnea. Resuscitative equipment including that necessary to support respiration should be readily available.
Diazepam with narcotic effects
When we Use diazepam with a narcotic analgesic, we reduce the dosage of the narcotic by at least one-third and administer in small increments. In some cases the use of a narcotic is not so necessary.
We do not administer Diazepam Injection to patients in shock, coma, or in acute alcoholic intoxication with depression of vital signs. As is true of most CNS-acting drugs, we caution patients receiving diazepam against engaging in hazardous occupations requiring complete mental alertness, such as operating machinery or driving a motor vehicle.
Tonic status epilepticus has been precipitated in patients treated with IV diazepam for petit mal status or petit mal variant status.
Usage in Pregnancy: An increased risk of congenital malformations associated with the use of minor tranquilizers (diazepam, meprobamate, and chlordiazepoxide) during the first trimester of pregnancy has been suggested in several studies. Because use of these drugs is rarely a matter of urgency, their use during this period should almost always be avoided. The possibility that a woman of childbearing potential may be pregnant at the time of institution of therapy should be considered. We advise Patients that if they become pregnant during therapy or intend to become pregnant they should communicate with their physicians about the desirability of discontinuing the drug.
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In humans, we see measurable amounts of diazepam in maternal and cord blood, indicating placental transfer of the drug. Until additional information is available, We do not recommend Diazepam Injection for obstetrical use.
Use in Children: Efficacy and safety of parenteral diazepam has not been established in the neonate (30 days or less of age).
We also observe Prolonged central nervous system depression in neonates, apparently due to inability to biotransform diazepam into inactive metabolites.
In pediatric use, in order to obtain maximal clinical effect with the minimum amount of drug and thus to reduce the risk of hazardous side effects, such as apnea or prolong periods of somnolence, We recommend that you give the drug slowly over a three-minute period in a dosage not to exceed 0.25 mg/kg. After an interval of 15 to 30 minutes we can safely repeat the initial dosage. If, however, we dont see relief of symptoms after a third administration, we recommend adjunctive therapy appropriate to the condition.
Withdrawal symptoms of the barbiturate type have occurred after the discontinuation of benzodiazepines (see DRUG ABUSE AND DEPENDENCE section).
Although we bring seizures under control promptly, a significant proportion of patients experience a return to seizure activity, presumably due to the short-live effect of diazepam after IV administration. The physician should prepare to re-administer the drug. However, we do not recommend diazepam for maintenance, and once we bring seizures under control, we give consideration to the administration of agents useful in longer term control of seizures.
If we combine diazepam with other psychotropic agents or anticonvulsant drugs, we give careful consideration to the pharmacology of the agents to we employ, particularly when we know compounds which may potentiate the action of diazepam, such as phenothiazines, narcotics, barbiturates, MAO inhibitors, and other antidepressants. In highly anxious patients with evidence of accompanying depression, particularly those who may have suicidal tendencies, protective measures may be necessary. The usual precautions in treating patients with impaire hepatic function should be observe. The kidney excretes Metabolites of diazepam; to avoid their excess accumulation, we exercise caution in the administration to patients with kidney disfunction.
Since an increase in cough reflex and laryngospasm may occur with peroral endoscopic procedures, the use of a topical anesthetic agent, and the availability of necessary countermeasures are recommended.
Until additional information is available, We do not recommend Diazepam Injection for obstetrical use.
Diazepam injection has produced hypotension or muscular weakness in some patients particularly when used with narcotics, barbiturates, or alcohol.
Lower doses (usually 2 mg to 5 mg) should be used for elderly and debilitated patients.
Side effects most commonly reported were drowsiness, fatigue, and ataxia; venous thrombosis and phlebitis at the site of injection. Other adverse reactions less frequently reported include:
Central Nervous System: Confusion, depression, dysarthria, headache, hypoactivity, slurred speech, syncope, tremor, vertigo.
Gastrointestinal: Constipation, nausea.
Genitourinary: Incontinence, changes in libido, urinary retention.
Cardiovascular: Bradycardia, cardiovascular collapse, hypotension.
EENT: Blurred vision, diplopia, nystagmus.
Skin: Urticaria, skin rash.
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