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Epoxide Actions |
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Description: Epoxide enhances activity of the inhibitory transmitter GABA in different parts of CNS by increasing neuronal-membrane permeability to chloride ions resulting to hyperpolarisation and stabilisation. It has some muscle relaxant and anticonvulsant activity.
Pharmacokinetics:
Absorption: Almost complete (oral); peak plasma concentrations after 1-2 hrs.
Distribution: Crosses the placenta, diffuses into CSF, enters breast milk. Protein-binding: 96%
Metabolism: Hepatic; converted to desmethyldiazepam.
Excretion: Urine (as unchanged drug and metabolites; faeces (conjugated metabolites); 5-30 hrs (elimination half-life).
Take this medication exactly as it was prescribed for you. Do not take the medication in larger amounts, or take it for longer than recommended by your doctor. Follow the directions on your prescription label.
Your doctor may occasionally change your dose to make sure you get the best results from this medication.
Epoxide should be used for only a short time. Do not take this medication for longer than 4 months without your doctor's advice.
Contact your doctor if this medicine seems to stop working as well in treating your symptoms.
Do not stop using Epoxide suddenly, or you could have seizures or unpleasant withdrawal symptoms. Talk to your doctor about how to avoid withdrawal symptoms when you stop using Epoxide.
To be sure this medication is not causing harmful effects, your blood and liver function may need to be tested on a regular basis. Do not miss any scheduled visits to your doctor.
Store Epoxide at room temperature away from moisture, heat, and light.
Keep track of how many pills have been used from each new bottle of this medicine. Benzodiazepines are drugs of abuse and you should be aware if any person in the household is using this medicine improperly or without a prescription.
May be taken with or without food.
Epoxide hydrochloride has antianxiety, sedative, appetite-stimulating and weak analgesic actions. The precise mechanism of action is not known. The drug blocks EEG arousal from stimulation of the brain stem reticular formation. It takes several hours for peak blood levels to be reached and the half-life of the drug is between 24 and 48 hours. After the drug is discontinued plasma levels decline slowly over a period of several days. Epoxide is excreted in the urine, with 1% to 2% unchanged and 3% to 6% as conjugate.
Animal
Pharmacology:
The drug has been studied extensively in many species of animals and these studies are suggestive of action on the limbic system of the brain, which recent evidence indicates is involved in emotional responses.
Hostile monkeys were made tame by oral drug doses which did not cause sedation. Epoxide hydrochloride revealed a “taming” action with the elimination of fear and aggression. The taming effect of Epoxide hydrochloride was further demonstrated in rats made vicious by lesions in the septal area of the brain. The drug dosage which effectively blocked the vicious reaction was well below the dose which caused sedation in these animals.
The LD50 of parenterally administered Epoxide hydrochloride was determined in mice (72 hours) and rats (5 days), and calculated according to the method of Miller and Tainter, with the following results: mice, IV, 123±12mg/kg; mice, IM, 366±7mg/kg; rats, IV, 120±7 mg/kg; rats, IM, greater than 160 mg/kg.
Effects on Reproduction:
Reproduction studies in rats fed 10, 20 and 80 mg/kg daily and bred through one or two matings showed no congenital anomalies, nor were there adverse effects on lactation of the dams or growth of the newborn. However, in another study at 100 mg/kg daily there was noted a significant decrease in the fertilization rate and a marked decrease in the viability and body weight of offspring which may be attributable to sedative activity, thus resulting in lack of interest in mating and lessened maternal nursing and care of the young. One neonate in each of the first and second matings in the rat reproduction study at the 100 mg/kg dose exhibited major skeletal defects. Further studies are in progress to determine the significance of these findings.
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Information checked by Dr. Sachin Kumar, MD Pharmacology
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