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Czep F Actions |
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Description: Czep F 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 Czep F hydrochloride only as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered.
The dose of Czep F hydrochloride will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of Czep F hydrochloride. If your dose is different, do not change it unless your doctor tells you to do so.
The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.
If you miss a dose of Czep F hydrochloride, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.
Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.
Keep out of the reach of children.
Do not keep outdated medicine or medicine no longer needed.
Ask your healthcare professional how you should dispose of any medicine you do not use.
May be taken with or without food.
Czep F 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. Czep F 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. Czep F hydrochloride revealed a “taming” action with the elimination of fear and aggression. The taming effect of Czep F 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 Czep F 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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