• 약학회지
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• 제14권1_2호
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• pp.1-14
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• 1970

Seventeen N,N/sup I/-disubstituted thiourea derivatives were synthesized by the Hugershof reaction and reported. Antitumor activities of the synthesized compounds against ascitic Ehrlich Carcinoma and ascitic sarcoma 180 were reported. It was found that 1,1/sup I/-(p-Phenylene)-3,3/sup I/-bis (2-carboxyphenyl)-2,2/sup I/-dithiourea was considerably active against ascitic Ehrlich Carcinoma and Sarcoma 180 respectively. 1-(2-Carboxyphenyl)-3-(p-ethoxyphenyl)-2 thiourea was active against ascitic Sarcoma 180. 1-Salicyloyl-3-(p-ethoxyphenyl)-2-thiourea and 1,1/sup I/-(p-Phenylene)-3,3/sup I/-bis(2-hydroxyethyl)-2,2/sup I/-dithiourea were active against ascitic Ehrlich Carcinoma. Antitubercular activities of the synthesized compounds against Mycobacterium tuberculosis H/sub 37/ R/sub v/ were also reported. It was found that 1-Isonicotinyl-4-cyclohexyl-3-thiosemicarbazide was considerably active at 100 .mu.g/ml. 1,1/sup I/-(p-Phenylene)-3,3/sup I/-bis(2-hydroxyethyl)-2,2/sup I/-dithiourea and 1-Salicyloyl-3-(p-ethoxyphenyl)-2-thiourea were active at 1000 .mu.g/ml respectively. Antibacterial activities of nine compounds of the synthesized compounds against S. aureus and E. Coli were reported. It was found that 1,1-(p-Phenylene)-4,4/sup I/-bis(isonicotinyl)-2,2/sup I/-dithiosemicarbazide and 1-Isonicotinyl-4-cyclohexyl-3-thiosemicarbazide were considerably active against S. aureus and E. Coli respectively. 1-(6-Methyl-2-benzothiazolyl)-3-(1-naphthyl)-2-thiourea was active against S. aureus. 1,1/sup I/-(p-Phenylene)-3,3/sup I/-bis (2-hydroxyethyl)-2,2/sup I/-dithiourea was active against E. Coli.

• 셀메드
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• 제10권2호
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• pp.13.1-13.7
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• 2020

Arusa (Adhatoda vasica) is an important medicinal plant widely used in Unani system of medicine of (Family-Acanthaceae). The leaves of Adhatoda vasica contain several biologically active phytochemicals such as alkaloids, tannins, saponins, phenolics and flavonoids. It mainly consists of pyrroquinazoline, alkaloids, viz. vasicine, vasicol, vasicinone, peganine along with other minor constituents. The plant possesses diverse pharmacological activities, In Unani system of medicine, the drug is described as having dafa-e-tashannuj (anti-spasmodic), qatil-e-jarasim (antibiotic), mukhrij-e-balgham (expectorant), dafa-e-humma (antipyretic) properties due to which it is prescribed in a wide range of ailments like influenza, tuberculosis, bronchitis, gastric ulcers etc. Leaf juice is beneficial in the treatment of dysentery and diarrhoea. Various other activities like radio modulation, hypoglycaemic effect, cardiovascular protection, antitubercular, antiviral, hepatoprotective and antioxidant activity have also been reported.

• Tuberculosis and Respiratory Diseases
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• 제78권3호
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• pp.161-167
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• 2015

Tuberculosis (TB) remains a major global health problem, and the incidence of TB cases has not significantly decreased over the past decade in Korea. The standard short course regimen is highly effective against TB, but requires multiple TB-specific drugs and a long treatment duration. Recent studies using late-generation fluoroquinolones and/or high-dose rifapentine-containing regimens to shorten the duration of TB treatment showed negative results. Extending the treatment duration may be considered in patients with cavitation on the initial chest radiograph and positivity in sputum culture at 2 months of treatment for preventing TB relapse. Current evidence does not support the use of fixed-dose combinations compared to separate drugs for the purpose of improving treatment outcomes. All patients receiving TB treatment should be monitored regularly for response to therapy, facilitation of treatment completion, and management of adverse drug reactions. Mild adverse effects can be managed with symptomatic therapy and changing the timing of the drug administration, but severe adverse effects require a discontinuation of the offending drugs.

• Advances in pediatric surgery
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• 제12권2호
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• pp.244-250
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• 2006

Splenic abscess is a rare clinical condition with a reported incidence of 0.14 % to 0.70 % in various autopsy series. Primary tuberculosis of the spleen as a cause of splenic abscess is even rarer, especially in the antitubercular era. Infants and children have a higher predisposition to extra-pulmonary tuberculosis than adults and tend to develop severe extra-pulmonary disease such as miliary tuberculosis and meningitis. The diagnosis of tuberculosis in infants and children can be difficult because of nonspecific symptoms and clinical findings. Computed tomography establishes the diagnosis of splenic abscess and demonstrates the number and location of abscesses. Splenectomy is the standard of care in most clinical setting. We present a 4-year-old girl who had multiple tuberculosis splenic abscesses and was treated successfully with splenectomy.

• 약학회지
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• 제31권4호
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• pp.204-212
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• 1987

Rifampicin is an indispensable drug along with isoniazid for the control of tuberculosis and is usually prescribed as the combination of rifampicin and isoniazid. This paper is attemtped to investigate the interaction of rifampicin and isoniazid. Isoniazid was administered orally at a dose of 30mg/kg of rabbits pretreated with rifampicin 7.5mg/kg, 15mg/kg, and 30mg/kg, respectively twice daily for 9 days. The results are as follows: The blood level and relative bioavailability of isoniazid were decreased significantly (p<0.05) by rifampicin at a dose of 15mg/kg and 30mg/kg. The renal clearance of total isoniazid and ratio of its metabolites to isoniazid were increased significantly (p<0.05) by rifampicin at a dose of 15mg/kg and 30mg/kg. It seemed to be due to enzyme induction by rifampicin. Elimination rate constant ($\beta$) of isoniazid was increased and half life ($t_{1/2$\beta}$) was decreased by rifampicin pretreatment. Dosage regimen of isoniazid after long term administration of rifampicin should be adjusted carefully.

• 셀메드
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• 제9권4호
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• pp.3.1-3.6
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• 2019

Melissa parviflora Benth. is an aromatic perennial herb of Lamiaceae family. It is one of the most influencial plant and used from centuries in Unani system of medicine for the treatment of various malady such as Epilepsy (mirgi), hemiplegia (falij), migraine (shaqeeqa), insomnia (sehar), indigestion (sue hazm) and palpitation (khafqaan) etc. The Persian physician Avicenna endorsed it for heart problems. It has antitubercular, antipyretic, analgesic and stomachic properties, also used to remove bad breath from mouth, strengthen the gums but its main action is as a tranquillizer and nervine relaxant, it is greatly esteemed for its calming properties. Preliminary performed phytochemical analysis revealed that tannin, flavonoid and saponins are the major components of the plant extract. The plants containing saponins or flavonoids exhibit anticonvulsant activity whereas the flavonoids show various biological activities including antioxidant, anti-inflammatory and cytotoxic-antitumor etc. Keeping in view the tremendous medicinal importance of the plant Badranjboya in Unani Medicine, this review provides updated information on its phytochemistry, therapeutic uses and pharmacological properties.

• Tuberculosis and Respiratory Diseases
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• 제77권4호
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• pp.161-166
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• 2014

Since tuberculosis (TB) remains a major global health concern and the incidence of multi-drug resistant (MDR)-TB is increasing globally, new modalities for the detection of TB and drug resistant TB are needed to improve TB control. The Xpert MTB/RIF test can be a valuable new tool for early detection of TB and rifampicin resistance, with a high sensitivity and specificity. Late-generation fluoroquinolones, levofloxacin, and moxifloxacin, which are the principal drugs for the treatment of MDR-TB, show equally high efficacy and safety. Systemic steroids may reduce the overall TB mortality attributable to all forms of TB across all organ systems, although inhaled corticosteroids can increase the risk of TB development. Although fixed dose combinations were expected to reduce the risk of drug resistance and increase drug compliance, a recent meta-analysis found that they might actually increase the risk of relapse and treatment failure. Regarding treatment duration, patients with cavitation and culture positivity at 2 months of TB treatment may require more than 6 months of standard treatment. New anti-TB drugs, such as linezolid, bedaquiline, and delamanid, could improve the outcomes in drug-resistant TB. Nontuberculous mycobacterial lung disease has typical clinical and immunological phenotypes. Mycobacterial genotyping may predict disease progression, and whole genome sequencing may reveal the transmission of Mycobacterium abscessus. In refractory Mycobacterium avium complex lung disease, a moxifloxacin-containing regimen was expected to improve the treatment outcome.

• Journal of Pharmaceutical Investigation
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• 제9권3호
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• pp.1-8
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• 1979

The main route of metabolism of isonicotinic acid hydrazid (INH) in man is its conjugation with acetyl coenzyme A to form acetyl-INH. The reaction is catalyzed by an N-acetyl transferase in the liver. The acetylated drug can be excreted by the kidney more efficiently than INH, and the biological half-life of the drug in the body depends upon how rapidly the drug can be acetylated. This report measured the concentration of INH in the blood of 147 individuals 6 hours after they received a standard dose (9.8mg/kg) and plotted the data as a frequeney distribution hiotogram. There was bimodality, with a mean for one subpopulation at approximately $0.6{\sim}0.8\;mcg/ml.$, and a mean for the other subpopulation between 2.8 and 4.0mcg/ml. As might be expected slow acetylators of INH are more likely to develop a cumulative toxicity to the drug. The principle ,toxicity to INH is a peripheral neuritis but this adverse effect can be prevented by given extra pyridoxin to the patients, and the vitamin does not alter the antitubercular activity of INH. This report carried out that pyridoxine does not alter the ratio of free INH to the total INH in blood.

• Clinical and Experimental Pediatrics
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• 제59권1호
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• pp.43-46
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• 2016

We present a case of tuberculosis-associated hemophagocytic lymphohistiocytosis in a 14-year-old girl. The patient presented with weight loss, malaise, fatigue, prolonged fever, and generalized lymphadenopathy. Laboratory investigation revealed pancytopenia (white blood cells, $2,020cells/{\mu}L$; hemoglobin, 10.2 g/dL; platelets, $52,000cells/{\mu}L$), hypertriglyceridemia (229 mg/dL), and hyperferritinemia (1,420 ng/mL). Bone marrow biopsy showed a hypocellular bone marrow with a large numbers of histiocytes and marked hemophagocytosis; based on these findings, she was diagnosed with hemophagocytic lymphohistiocytosis. Polymerase chain reaction (PCR) with both the bone marrow aspiration and sputum samples revealed the presence of Mycobacterium tuberculosis. Antitubercular therapy with immune modulation therapy including dexamethasone and intravenous immunoglobulin was initiated. The results of all laboratory tests including bone marrow biopsy and PCR with both the bone marrow aspiration and sputum samples were normalized after treatment. Thus, early bone marrow biopsy and the use of techniques such as PCR can avoid delays in diagnosis and improve the survival rates of patients with tuberculosis-associated hemophagocytic lymphohistiocytosis.

• Archives of Pharmacal Research
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• 제26권10호
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• pp.778-784
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• 2003

N'-(1-alkyl-2,3-dihydro-2-oxo-1H-3-indolyliden)-4-pyridinecarboxylic acid hydrazide derivatives, 3(a-g), were synthesized in a trial to overcome the resistance developed with the therapeutic uses of isoniazid (INH). The lipophilicity of the synthesized derivatives supersedes that of the INH as expressed by Clog p values. The synthesized compounds and INH were tested against bovin, human sensitive and human resist strains of Mycobacterium tuberculosis. Compounds 3a, 3d, 3f and 3g with 1-unsubstituted, 1-propyl, 1-propynyl and 1-benzyl groups respectively exhibited equipotent growth inhibitory activity (MIC 10 $\mu$mol) against the tested strains as compared with INH however the later has no activity against human resist strain. Pharmacokinetic study revealed that the rate and extent of absorption of the tested derivatives (3d and 3f) significantly higher than that of INH (p＜0.05). The relative bioavailabilities ($F_R%$) were 183.15 and 443.25 for 3f and 3d respectively as compared to INH. These results preliminary indicate the possible use of the prepared derivatives for treatment of tuberculosis infections in order to overcome the resistance developed with INH.