• Archives of Pharmacal Research
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• 제21권3호
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• pp.286-290
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• 1998

The abuse of zipeprol, an antitussive agent, was found to be most prevalent among young people in Korea. Because abusers take large doses of this drug for its hallucinogenic effects, fatalities from zipeprol overdose abuse have been on the rise since 1991. Since 1991, a total of 69 zipeprol-related deaths have occurred throughout the nation. A demographic study shows that in ninety six percent of cases involving zipeprol alone, the victims were in their teens and twenties. The mate/female ratio in zipeprol related death was 3.5:1. Most of these zipeprol-associated deaths occurred in the larger cities of Seoul and Inchon. The blood concentration of zipeprol ranged from 0.8 to $38.3{\mu}g/mL $in single drug involved deaths, while zipeprol varied from to 35.3 $0.1{\mu}g/mL $in zipeprol and dextromethorphan victims.

• 대한임상독성학회지
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• 제7권2호
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• pp.172-175
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• 2009

Zipeprol dihydrochloride is a non-opioid mucolytic, antitussive agent and it is frequently prescribed for respiratory symptoms such as cough and sputum. The main pharmacologic mechanisms of zipeprol are inhibition of superior laryngeal nerve stimulation and direct antagonism for stimulation of the bronchial receptors, which might have an effect for the drug's mucolytic action. Many cases of drug abuse with zipeprol have occurred world-wide due to the hallucinogenic effect of the drug. In Korea, zipeprol was reported to be the most commonly abused drug among young people for the 1990s. Zipeprol associated death was first reported since 1991 and 69 cases of death related to zipeprol abuse were further reported during 8 years (between 1991 and 1998). In addition to the hallucinogenic effect, dyspnea, extrapyramidal symptoms, seizure, cerebral edema have been reported as the signs and symptoms of toxic zipeprol overdose. However, zipeprol abuse is not common for old age people and non drug abusers. We report here on a fatal case of acute zipeprol poisoning in an eighty five year old drug addicted woman.

• 약학회지
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• 제36권3호
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• pp.191-198
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• 1992

The abuse of zipeprol, an antitussive agent, is prevalent among young people. Ten fatal cases of zipeprol concentration in blood after its abuse had caused death are disscussed. GC equipped with TSD was used to quantify the drug in postmortem blood and GC/MS to identify the metabolites in urine after preliminary test. The calibration curve of zipeprol was linear (r = 0.998) and the recoveries of zipeprol 5, 10 and $20\;{\mu}g$ added to 1 ml postmortem blood were $97.2{\pm}3.9$, $92.5{\pm}3.9$ and $86.9{\pm}4.6%$ respectively. The blood zipeprol concentration varied 2.9 to $24.69\;{\mu}g/ml$ in 10 fatal cases. All the deaths were young adults with the age of 16-21. Three metabolites were identified in drug abuser's urine, 2-methoxy-2-phenyl ethylpiperazine, 2-hydroxy-3-methoxy-3-phenyl propylpiperazine and a demethylated zipeprol.

• 약학회지
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• 제31권1호
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• pp.42-44
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• 1987

Ziperol, anti-tussive, is considerably bitter. Therefore, it is necessary to mitigate the bitterness in ziperol syrup for children. In this experiment, it was attempted to mitigate the bitterness of zipeprol by means of polymers such as $\beta$-cyclodextrin, arabic gum, HPMC(hydroxypropyl methylcellulose), PEG 2000(polyethyleneglycol 2000), PVP(polyvinylpyrrolidone). Caffeine was used as the reference standard of bitterness. In the result of this experiment, $\beta$-cyclodextrin, would mitigate the bitterness of zipeprol more largely than any other polymers. Arabic gum was the second choice which would mitigate the bitterness of zipeprol.

• Journal of Pharmaceutical Investigation
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• 제18권4호
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• pp.187-195
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• 1988

Poorly permeable $Eudragit^{\circledR}$ RS 100 polymer was used as a wall material for the microencapsulation of zipeprol dihydrochloride by a phase separation method from chloroform-cyclohexane system with 5% polyisobutylene in cyclohexane, and microcapsules obtained were evaluated in vitro by particle size analysis, scanning electron microscopy, drug release test and in vivo bioavailability test in rats. The mechanism of drug release from microcapsules appeared to fit Higuchi matrix model kinetics. The area under the first moment of plasma concentration-time curve of the microcapsules obtained was considerably increased (p<0.05) as compared with that from zipeprol dihydrochloride oral solution. Therefore, it may be suggested that $Eudragit^{\cirledR}$ RS 100 coated zipeprol dihydrochloride microcapsules can be used as a sustained release medication.

• Archives of Pharmacal Research
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• 제10권2호
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• pp.69-74
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• 1987

The characteristics of zipeprol-$\beta$-cyclodextrin system were studied by circular dichroism, competitive UV method and dialysis method. In this experiment, binding constants by competitive UV method, circular dichroism and dialysis method were 155 M$^{-1}$ 187 M$\^{-1}$/($\pm$ 5%) and 315 $^{-1}$, repectively. It shows that zipeprol forms 1:1 compelx with $\beta$-cyclodextrin by circular dichroism and 1:2 by dialysis method. pH profile shows that binding force seems to be a hydrophobic interaction. It is suggested that benzene ring be accomodated in the cavity of $\beta$-cyclodextrin.

• 대한핵의학회지
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• 제27권1호
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• pp.22-27
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• 1993

Drug abuse is widespread in worldwide and has been associated with neurologic complication. Zipeprol is one of the drugs which been abused for psychological satisfaction in some adolescents. This agent is non-opioid antitussive agent, which is not legally considered as being capable of creating dependence or abuse liability at therapeutic serum levels. But it has been reported that acute or chronic overdose create neurologic complication such as convulsion as well as dependence. Recently we experienced six zipeprol abusers who admitted due to convulsion and variable neurologic symptoms. The aim of our study was to determine the role of $^{99m}Tc$-HMPAO brain SPECT in those patients. EEG and brain CT showed no abnormal finding, but brain SPECT showed focal or multiple perfusion abnormalities in frontal, parietal, occipital cortex, basal ganglia, thalamus and especially at temporal cortex. These results suggest that brain SPECT may be a useful diagnostic tool to evaluate the cerebral dysfunction infused by zipeprol abuse.