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Diazepam Valium. Valium side effects, warnings, precautions, adverse effects, overdose, withdrawal symptoms and Valium natural alternatives. Before you begin the spiral down with this drug, try giving your body what it really wants.
Diazepam
Valium Withdrawal
Valium Side Effects
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Pharmacology
Anxiolytic - Sedative - Muscle Relaxant
Diazepam is a benzodiazepine with CNS depressant properties and a somewhat flatter dose-response slope than the sedative-hypnotic drugs. In laboratory animals, it produces, in varying doses, taming, disinhibitory, sedative, anticonvulsant, muscle relaxant, ataxic and hypnotic effects.
Diazepam is relatively devoid of autonomic effects and does not significantly reduce locomotor activity at low doses, or depress amphetamine-induced excitation. In high doses, it activates the drug metabolizing enzymes in the liver. Diazepam also possesses dependence liability and may produce withdrawal
symptoms, but has a wide margin of safety against poisoning.
Metabolism studies in animals and man have indicated that oral diazepam is rapidly absorbed from the gastrointestinal tract. Peak blood levels are reached within 1-2 hours after administration. The acute half-life is 6-8 hours with a slower decline thereafter, possibly due to tissue storage.
In humans, comparable blood levels of diazepam were obtained in maternal and cord blood indicating placental transfer of the drug. Diazepam may appear in human breast milk.
With the parenteral form, peak blood levels are reached within 15 minutes after i.v. administration and are of the same magnitude as after oral administration. The respective half-life is approximately 2-3 hours.
The distribution and fate of tritium-labeled diazepam in man has indicated that the drug has a rapid and extensive uptake by tissues. Although the radioactivity in the blood appears to represent mainly the intact drug, diazepam was shown to be excreted exclusively in the form of its metabolites. The two
major metabolites are oxazepam glucuronide and N-desmethylated diazepam.
Indications
The short-term 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 stress conditions and anxiety states with somatic expression.
In acute alcoholic withdrawal, diazepam may be useful in the symptomatic relief of acute agitation, tremor and impending acute delirium tremens.
As an adjunct for the relief of skeletal muscle spasm due to reflex spasm to local pathology, such as inflammation of the muscle and joints or secondary to trauma; spasticity caused by upper motor neuron disorders, such as cerebral palsy and paraplegia; athetosis and the rare stiff man syndrome.
Contraindications
Myasthenia gravis, known hypersensitivity to benzodiazepines. Not recommended for children under 6 months of age.
Warnings
Pregnancy:
Several studies have suggested an increased risk of congenital malformations associated with the use of diazepam, chlordiazepoxide and meprobamate during the first trimester of pregnancy. Therefore, the administration of diazepam is rarely justified in women of childbearing potential. If the drug is prescribed for a woman of childbearing
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.
Precautions
Geriatrics:
Elderly and debilitated patients or those with organic brain disorders have been found to be prone to CNS depression following even low doses. For these patients it is recommended that the dosage be limited to the smallest effective amount to preclude development of ataxia, oversedation or other possible adverse effects.
Use in 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 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.
Use in epileptic patients:
Since diazepam may exacerbate grand mal seizures in some patients, caution is required when it is used in epileptic patients. An adjustment may be necessary in their anticonvulsive medication. Abrupt withdrawal of diazepam in these patients should also be avoided.
Potentiation of drug effects:
Patients should be advised to abstain from alcohol and other CNS depressant drugs during treatment with diazepam. Phenothiazines, barbiturates, MAO inhibitors and other psychoactive drugs may potentiate the action of the drug and should not usually be given concurrently.
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.
Occupational Hazards:
Patients receiving diazepam should be advised to proceed cautiously whenever mental alertness and physical coordination 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 would be highly advisable.
Adverse Effects
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, changes in libido.
The more serious adverse reactions occasionally reported are leukopenia, jaundice, hypersensitivity and paradoxical reactions.
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.
Overdose
Symptoms:
Drowsiness, oversedation and ataxia. When the effects of 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 on respiration, pulse and blood pressure unless the overdosage
is extreme.
Treatment:
Gastric lavage may be beneficial if performed soon after oral ingestion of diazepam. If necessary, a CNS stimulant such as caffeine or methylphenidate may be administered with caution. Supportive measures should be instituted as indicated, such as, maintenance of an adequate airway, levarterenol for hypotension. Dialysis appears to be of
little value.
Dosage
Must be individualized according to diagnosis, severity of symptoms and degree of response. While the usual daily dosages given below will meet the needs of most patients, there will be some who may require higher doses. In the first few days of administration a cumulative effect of the drug may occur, and
therefore the dosage should be increased only after stabilization is evident.
Adults:
Symptomatic relief of anxiety and tension in psychoneurosis and anxiety reactions: 2 to 10 mg, 2 to 4 times daily depending upon severity of symptoms.
Symptomatic relief in acute alcohol withdrawal: 10 mg, 3 or 4 times during the first 24 hours, reducing to 5 mg, 3 or 4 times daily as needed.
Adjunctively for relief of skeletal muscle spasms: 2 to 10 mg, 3 to 4 times daily.
Elderly and debilitated patients, or in the presence of debilitating disease:
2 mg, 1 or 2 times daily initially; increase gradually as needed and tolerated.
Children (Because of varied responses, initiate therapy with lowest dose and increase as required. Not for use in children under 6 months):
1 to 2.5 mg, 3 or 4 times daily initially; increase gradually as needed and tolerated.
Do not prescribe or administer diazepam for periods in excess of 6 weeks, unless a definite need for utilizing this medication has been established by a follow-up medical examination.
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