• YAKHAK HOEJI
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• v.32 no.2
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• pp.101-111
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• 1988

$[^3H]$ Quinuclidinyl benzilate(QNB) binding assays were performed in the dog ventricular sarcolemma fraction enriched approx. 32-fold in sarcolemma compared to the starting homogenate to elucidate the effect of antihistaminics on cardiac muscarinic receptor. Chlorpheniramine(CHP) inhibited specific binding of $[^3H]$QNB and delayed the equilibrium binding. The rate constants at $37^{\circ}C$ for formation and dissociation of the QNB receptor complex were $0.38{\times}10^9\;M^{-1}$ and $1.6{\times}10^{-2}\;min^{-1}$, respectively. The mean value for the dissociation constant from the pairs of the rate constants was 43. 2 pM and this value was similar to the value(44.8pM) determined from Scatchard analysis. CHP decreased association rate constant, indicating increase in $K_D$ value. Decrease in affinity without affecting the binding site concentration$(B_{max})$ for $[^3H]$QNB binding by CHP was also demonstrated by Scatchard analysis. $K_i$ values for $H_i$-blockers that inhibited specific $[^3H]$QNB binding were $0.02{\sim}4.8{\mu}M$. Cimetidine with $K_i$ value of $230{\mu}M$, however, was ineffective in displacing $[^3H]$QNB binding at concentration of $50{\mu}M$. The Hill coefficient for $H_1$-blockers were about one. The results indicate that $H_1$-antihistaminics inhibit $[^3H]$ QNB binding by interaction with myocardiac muscarinic cholinergic receptor and anticholinergic side effects of these drugs are mainly due to this receptor blocking mechanism.

• YAKHAK HOEJI
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• v.58 no.5
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• pp.328-336
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• 2014

Anticholinergic drugs are included in the efficacy group of various antidepressants, antihistamines, antispasmodics like skeletal muscle relaxants. Elderly patients are often taking anticholinergic drugs due to various diseases such as sleep disorders and dysuria. But the use of anticholinergic drugs is restricted in guidelines such as Beers Criteria or STOPP due to the anticholinergic adverse effects including dry mouth, constipation, difficult urination, delirium, hallucinations and especially cognitive impairment. In this study, we investigated the usage of anticholinergic drugs in out-of-hospital prescription of 4,442 elderly patients. Results of the study were obtained that 32% (n=1,421) of overall patients were prescribed with 1~6 products (average 1.37) of anticholinergic drugs. 70.9% of the 1,421 patients (n=1,007) were prescribed with one drug, 22.7% (n=323) were two drugs and 4.9% (n=70) were three drugs. 27.1% of the 1,421 patients (n=430) were 70~74 years old patients who were the most commonly prescribed with anticholinergic drugs. Amitriptyline, chlorpheniramine, dimenhydrinate and quetiapine were most frequent component of ACB Score 3 drugs and amantadine, baclofen, carbamazepine, cyproheptadine and oxcarbazepine were most frequent of ACB Score 2 drugs. Anticholinergic Drug Scale (ADS) of individual patients presented one point (48.5%, n=689), 2 points (15.4%, n=219), more than 3 points (36.1%, n=513), and up to maximum 12 point (n=1). More than 2 points were more than half (51.5%, n=732). Therefore, additional prospective study in the use and adverse effects of anticholinergic drugs for elderly patients will be required. And national management such as DUR program will be required for elderly drug administration from now on.

• The Korean Journal of Pharmacology
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• v.27 no.2
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• pp.211-214
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• 1991

SJ-200 is an oral liquid preparation of acetaminophen, ibuprofen, Dl-methyleph edrine HCl, caffeine, chlorpheniramine maleate, guaifenesin and dextromethorphan HBr, which is indicated when there is a need to improve various cold symptoms such as headache, sore throat, fever, or cough etc. Thirty patients was enroled for this study fro June to July, 1991. They were given one bottle (30 ml) of SJ-200 t.i.d dy P.O for an average of one to seven days. 1) Twenty-eight patients (84.8%) were relieved from the symptoms of upper respiratory tract infection. 2) Side effects with this preparation occured in 8 patients924.2%) but in four patients, they were mild, which wee transienty by the discontinuation f the medication.

• Journal of Chest Surgery
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• v.23 no.2
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• pp.222-230
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• 1990

Protamine, a polycationic peptide extracted from fish, has been widely used for the reversal of anticoagulant action of heparin. However it may cause untoward circulatory side effects including hypotension and bradyarrhythmia. Nowadays, histamine and prostacyclin are regarded as one of the causative agents in the underlying mechanism of hemodynamic changes. To certify the possible role of histamine and prostacyclin, we observed simultaneous changes of the hemodynamic status, plasma concentration of thromboxane B, and circulating platelet count before and after intravenous injection of protamine. Experimental dogs, weighing 12-14kg, were divided into 2 groups; group A animals [n=10], were pretreated with indomethacin[2.5mg/kg] and group B animals[n=10] were pretreated with chlorpheniramine[0.5mg/kg] Heparin[3mg/kg] and protamine [3mg/kg] were administered sequentially in both groups. The results were as follows ; 1. The mean systemic arterial pressure was maintained well in groups A, whereas in group B it decreased from 165\ulcorner18mmHg to 138\ulcorner30mmHg[p<0.01] and 151\ulcorner21 mmHg[p<0.05] at 1 minute and 2 minutes after protamine injection. The mean pulmonary arterial pressure was not changed significantly in group A, whereas in group B it increased from 852 mmHg to 11\ulcorner3 mmHg[p<0.05], 11\ulcorner3 mmHg[p<0.05] and 10\ulcorner3 mmHg[p<0.05] at 1 minute, 3 minutes and 5 minutes after protamine injection. 2 The thromboxane B2 was not changed significantly in group A, whereas in group B it increased from 399\ulcorner401 \ulcornerg/ml to 744\ulcorner615 \ulcornerg/ml[p<0.05] and 814\ulcorner1070 \ulcornerg/ml [p<0.0 5] at 1 minute and 3 minutes after protamine injection without concomitant changes of pulmonary vascular resistance and pulmonary capillary wedge pressure. 3. The number of circulating platelet was not changed in group A, whereas in group B it decreased from 207100\ulcorner103600/\ulcornerl to 159700\ulcorner90900/\ulcornerl [p<0.05] at 1 minute after protamine injection, Although thromboxane B2 and platelet count were changed significantly after protamine injection, they did not cause the remarkable hemodynamic changes. Considering the above results, hemodynamic changes may be caused mainly by prostacyclin rather than thromboxane or platelet. Therefore, the pretreatment with cyclooxygenase inhibitor would be beneficial to prevent circulatory adverse effects of protamine for the patients undergoing cardiac surgery.

• YAKHAK HOEJI
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• v.54 no.5
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• pp.341-347
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• 2010

The majority of forensic autopsies in Korea are performed by the National Institute of Scientific Investigation (NISI), and the NISI has carried out about 4,000 cases annually. Total 4,578 autopsies were performed by NISI in 2009, among them 2,918 cases (64%) were carried out at main office of NISI in Seoul, which is in charge of Seoul, Incheon and Gyeonggi province. In this study we investigated pattern of drugs & poisons in autopsy cases for recent three years in Korea. Postmortem specimens (bloods, gastric contents, etc) from autopsy cases by main office of NISI during 2007~2009 were screened for drugs & poisons. Using laboratory information management system of NISI (iLIMS), the kinds of drugs & poisons and the frequency were investigated. As the results, 1,705 cases were negative to drugs & poisons, it occupied 58% of total 2,918 autopsy cases in 2009. During three years (2007~2009), the kinds of drugs & poisons detected in specimens were 206, 185 and 203, respectively, and top three drugs were atropine (anticholinergic), chlorpheniramine (antihistamine) and lidocaine (local anaesthetic/anti-arrythmic). These drugs were supposed to be used not so much for suicidal or homicidal purpose as for therapeutic purpose in hospital. Meanwhile cyanide showed the highest frequency of poisons during 2007~2009, and the frequency was 32 cases in 2009. In case of pesticides, poisoning by paraquat (herbicide, 17 cases) showed the highest frequency, and methomyl (insecticide, 9 cases) and glyphosate (herbicide, 7 cases) were followed. Finally we selected 62 drugs as target drugs for systematic toxicological analysis (STA) for Korea. Poisons such as pesticides, natural toxins, volatile compounds should be included for STA in further study.