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Valium
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Diazepam is used to treat anxiety and tension, and is the most effective benzodiazepine for treating muscle spasms. It is also used as a sedative premedication for various medical procedures, and to treat alcohol and opiate withdrawal symptoms.
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Diazepam can be administered orally, intravenously, intramuscularly, or as a suppository. When taken orally, diazepam is rapidly absorbed and shows a fast onset of action. Absorption is much slower and more erratic when diazepam is given as an intramuscular injection. Diazepam is highly lipid-soluble and therefore crosses the blood-brain barrier easily.
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Diazepam has a range of side effects which are common to most benzodiazepines. Most frequently encountered are:
- drowsiness
- depression
- impaired motor function
- impaired coordination
- impaired balance
- dizziness
- nervousness
- anterograde amnesia (especially pronounced in higher doses)
Paradoxical effects like irritability, insomnia, muscle cramps, and in extreme cases, even rage and violence may be seen (these require immediate withdrawal of the drug). It can lead to physiological tolerance and psychological addiction. It should be noted that up to 30% treated on a long-term basis develop a form of dependence known as 'low-dose-dependence', i.e. these patients do not need increasing doses to experience the feeling of 'well-being' caused by the drug. Withdrawal can only be accomplished with difficulty by a slow program (see below).
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- Diazepam increases the central depressive effects of alcohol, other hypnotics/sedatives (e.g. barbiturates), narcotics, and other muscle relaxants. The euphoriant effects of opioids may be increased, leading to increased risk of psychological dependence.
- Cimetidine, omeprazole, ketoconazole, and fluoxetine prolong the action of diazepam by inhibiting its elimination. Disulfiram may act in the same way. Dose reductions during long-term therapy may be necessary.
- Hormonal contraceptives ('the pill') significantly decrease the elimination of a major metabolite of diazepam (desmethyldiazepam).
- Cisapride may enhance the absorption of diazepam and therefore increase the sedative activities of diazepam.
- Smoking can enhance the elimination of diazepam and decrease its action.
- Small doses of theophylline (asthma medication) inhibit the action of Diazepam.
- Diazepam may block the action of levodopa used in the treatment of Parkinson's Disease.
- Diazepam may infrequently block the matabolism of phenytoin and therefore increase its actions and side-effects.
- Foods that acidify the urine can lead to faster renal elimination, reducing the drug levels and activity.
- There are conflicting reports as to whether food in general has any effects on the absorbtion and activity of diazepam
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A person who has consumed too much diazepam will display one or more of the following symptoms:
- Somnolence
- Mental confusion
- Diminished motor functions
- Coma
Diazepam overdose is considered a medical emergency and generally requires the immediate attention of medical personnel. The antidote for an overdose diazepam (or any other benzodiazepine) is flumazenil (AnexateŽ). Because flumazenil is a short-acting drug and the effects of diazepam can last for days, several doses of flumazenil may be necessary. Artificial respiration and stabilization of cardiovascular functions may also be necessary.
The oral LD50 (i.e. lethal dose) of diazepam in humans, if taken alone, is estimated to be 500mg or more. A case where a patient took 300mg resulted only in prolonged sleep and consecutive drowsiness for the next days without serious impairment of cardiac or respiratory functions. Overdoses of diazepam with alcohol and/or other depressants may be fatal.
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