Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0017536 (giardiasis)
 1,714 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Tinidazole has been reported to be highly effective against trichomoniasis, giardiasis and amoebiasis. In vitro, tinidazole is more active against trichomonads than metronidazole and possesses antiprotozoal activity at least comparable to metronidazole against Entamoeba histolytica, Tinidazole gives higher serum levels in animals following oral administration than metronidazole and is well distributed in organs and tissues. When tinidazole or metronidazole is given to healthy volunteers at a dose of 2g orally, the serum level of tinidazole at 48h is considerably higher than that of metronidazole. At 72h tinidazole is still present but metronidazole is not. These pharmacokinetic differences result from the longer half-life of tinidazole. These findings suggest that tinidazole might prove to be more useful than metronidazole in the treatment of protozoal infections when given in once daily oral doses of 2g.
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PMID:Aspects of the pharmacology and pharmacokinetics of nitroimidazoles with special reference to tinidazole. 35 May 61

Metronidazole which has been widely used for many years in the treatment of trichomoniasis, amoebiasis and giardiasis, has recently been shown to be active against anaerobic bacteria. Serum, cerebrospinal fluid and tissue concentrations bactericidal for Bacteroides species are attained after usual dosages given orally or intravenously or higher dosages given rectally (suppository). Prospective studies have demonstrated that the addition of metronidazole to regimens for pre-operative bowel preparation, decreases the frequency of postoperative infection and eliminates anaerobic infection. Similarly, anaerobic infection after acute appendicectomy or hysterectomy has been virtually eliminated by metronidazole given before and up to 1 week after surgery. Metronidazole has been successfully used in the treatment of anaerobic infections of the chest, head, gastrointestinal and female genitourinary tract, and of anaerobic septicaemia and bacteraemia. Metronidazole is the most active agent available against obligate anaerobes and is likely to be of major value in the treatment of serious infections due to these organisms. Although the absence of formal comparative trials in many areas of use makes it difficult to clearly state the relative therapeutic efficacy of metronidazole, compared with other drugs such as clindamycin, chloramphenicol or penicillin, it is nevertheless a very effective agent in the treatment and prevention of anaerobic infections.
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PMID:Metronidazole in anaerobic infections: a review of its activity, pharmacokinetics and therapeutic use. 36 99

An open multicentre trial was undertaken in 8 countries to assess the efficacy and tolerance of short course treatment regimens of tinidazole Trichomoniasis: of 859 patients with trichomonal vaginitis given a 2g single dose of tinidazole 717 (95.2%) were cured. Side-effects occurred in 82 patients (9.5%) and in 12 were regarded as severe. Giardiasis: of 74 children with symptomatic giardiasis given tinidazole in a single dose of approximately 50 mg/kg body weight, 65 (88%) were parasitologically and symptomatically cured. 2 (2.7%) complained of side-effects, none of which was severe. Intestinal amoebiasis: of 502 patients, comprising 458 adults and 44 children, with symptomatic intestinal amoebiasis who received tinidazole as a single daily dose on 2 to 3 consecutive days, 477 (95%) were parasitologically cured with complete or marked improvement in symptoms. Side-effects occurred in 50 patients (10%) and in 11 were regarded as severe. Amoebic liver abscess: 82 patients were given tinidazole in single doses of 2g on 3 consecutive days. The response was rated as excellent in 60 and good in 17 (overall cure 93.9%). Side-effects occurred in 9 patients (10.9) and in 2 were regarded as severe. These findings confirm the efficacy and tolerance of short regimens of tinidazole given in single daily doses.
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PMID:Tinidazole in the treatment of trichomoniasis, giardiasis and amoebiasis. Report of a multicentre study. 65 95

Tinidazole, a synthetic imidazole derivative, has been used in the oral treatment of several protozoal infections - trichomoniasis, giardiasis and amoebiasis. Among the protozoal organisms inhibited by tinidazole are Trichomonas vaginalis, Trichomonas foetus, and Entamoeba histolytica. In vitro, tinidazole has been shown to possess antiprotozoal activity at least comparable to, and in some cases greater than, metronidazole. Tinidazole also has activity against some Gram-negative anaerobic bacilli, including Bacteroides spp. Following oral administration of a 2g dose, like metronidazole serum levels peak in about 2 hours but persist for longer. Any clinical significance of the longer plasma half-life (tinidazole 12.5h; metronidazole 7.3h) has yet to be demonstrated. Tinidazole is approximately 20% bound to plasma proteins. Only unchanged drug has been found in the plasma and urine of tinidazole-treated subjects, although metabolites have been detected in animal studies. A single 2g dose of tinidazole has been shown to be effective therapy in vaginal trichomoniasis and in urogenital trichomoniasis in males. Single-dose therapy in general offers advantages in regard to convenience, and in the treatment of a sexually transmissible disease such as trichomoniasis, single-dose therapy facilitates compliance of patient and sexual partner. In comparative studies, tinidazole, in both single-dose and traditional multiple-dose regimens, has been shown to be equivalent and often superior to other antitrichomonal agents, including metronidazole. In intestinal amoebiasis, tinidazole has been evaluated after both once-a-day and multiple daily dose regimens, with the former giving slightly better results. When both metronidazole and tinidazole were administered in multiple daily dose regimens, the two agents yielded similar cure rates; in one study fewer tinidazole-treated patients required a second course. Tinidazole has also been successful in some cases of amoebic liver abscess, but an advantage over metronidazole has not been demonstrated. Results in the treatment of giardiasis, especially with the single-dose regimen, are promising, and in one study, tinidazole proved effective in infections resistant to metronidazole. Even in large doses, tinidazole has been well tolerated, although rarely vomiting may occur and the patient may need to be re-treated with a multiple dose regimen.
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PMID:Tinidazole: a review of its antiprotozoal activity and therapeutic efficacy. 95 9

Metronidazole was first introduced for the treatment of trichomoniasis. Its therapeutic use has subsequently been expanded to include amoebiasis, giardiasis and, more recently, anaerobic infections. Most of the early pharmacokinetic studies employed nonspecific assays such as microbiological and chemical assays. These assays were not able to differentiate the parent drug from the metabolites or other interfering substances. Pharmacokinetic data obtained through the use of specific chromatographic techniques provide the basis for this review of recent pharmacokinetic findings concerning metronidazole and other nitroimidazole antibiotics. When given intravenously or orally at usual recommended doses, metronidazole attains concentrations well above the minimum inhibitory concentrations for most susceptible micro-organisms. The drug has an oral bioavailability approaching 100%. Rectal and vaginal administration results in a smaller amount of drug absorption and lower serum concentrations. Metronidazole has limited plasma protein binding but can attain very favourable tissue distribution, including into the central nervous system. The drug is extensively metabolised by the liver to form 2 primary oxidative metabolites: the hydroxy and acetic acid metabolites. The kidney is responsible for the elimination of only a small amount of the parent drug; however, normal excretion of the 2 metabolites is dependent on the integrity of kidney function. The metabolism of metronidazole was found to vary among patient groups. Preterm and term infants have lower total body clearance (CL) and prolonged elimination half-lives. However, children older than 4 years old were observed to have pharmacokinetic parameters similar to those in adults. Reduced CL was also observed in children who are malnourished. Elderly patients have reduced renal excretion of both the parent drug and hydroxy metabolite. Pharmacokinetic parameters in pregnant patients were not significantly different from those in nonpregnant women; however, the drug is distributed into breastmilk and the infant will be exposed to the drug through the nursing mother. Patients undergoing gastrointestinal surgery or having enteric diseases and those who are hospitalised or critically ill also have altered pharmacokinetics. Metabolism of the drug is reduced in patients with liver dysfunction, giving delayed production of metabolites. In contrast, renal failure has little effect on the elimination of the parent drug, but affects the excretion of the metabolites more significantly. Haemodialysis was found to remove a substantial amount of the metronidazole while the effect of peritoneal dialysis was more limited. Energy and protein deficient diets as well as occupational exposure to gasoline did not alter metronidazole pharmacokinetics. However, the effect of alcohol consumption on metronidazole CL requires further study.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:Clinical pharmacokinetics of metronidazole and other nitroimidazole anti-infectives. 147 3

The tetracyclines are effective in the treatment of Chlamydia, Mycoplasma pneumoniae, and rickettsial infections and also can be used for gonococcal infections in patients unable to tolerate penicillin. These drugs may cause gastrointestinal irritation, diarrhea, phototoxic dermatitis, and vestibular damage, and fatal reactions due to hepatotoxicity have occurred in pregnant women. Chloramphenicol has a broad spectrum of bacteriostatic activity, but its association with suppression of the bone marrow and aplastic anemia has relegated it to a historical role. Erythromycin is the drug of choice for the treatment of infections caused by M. pneumoniae, Legionella species, group A beta-hemolytic streptococci, and Streptococcus pneumoniae. The frequency of serious adverse effects associated with the use of erythromycin is low; dose-related epigastric distress may occur. Clindamycin is bactericidal to most nonenterococcal gram-positive aerobic bacteria and many anaerobic microorganisms. Although historically it was a frequent cause of antibiotic-associated diarrhea and colitis, clindamycin is considered an excellent alternative to beta-lactam antibiotics for treatment of many staphylococcal infections, and it has therapeutic utility in anaerobic infections and in several protozoan infections in immunosuppressed patients. Metronidazole is efficacious for treating nonpulmonary anaerobic infections, various parasitic infections (trichomoniasis, amebiasis, and giardiasis), nonspecific vaginitis, and Clostridium difficile-mediated colitis. With use of metronidazole, mild side effects such as epigastric discomfort, diarrhea, reversible neutropenia, and allergic-type cutaneous reactions may occur.
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PMID:Tetracyclines, chloramphenicol, erythromycin, clindamycin, and metronidazole. 174 96

Sexual activity is the primary method of transmission for several important parasitic diseases and has resulted in a significant prevalence of enteric parasitic infection among male homosexuals. The majority of parasitic sexually transmitted diseases involve protozoan pathogens; however, nematode and arthropod illnesses are also included in this group. Trichomoniasis, caused by Trichomonas vaginalis, is the most common parasitic STD. Infection with this organism typically results in the signs and symptoms of vaginitis. Trichomoniasis can be diagnosed in the office setting by performing a microscopic evaluation of infected vaginal secretions and can be successfully treated with metronidazole. Both pediculosis pubis, caused by the crab louse Pthirus pubis, and scabies, caused by the itch mite Sarcoptes scabiei, present with severe pruritus. A papular or vesicular rash and linear burrows seen in the finger webs and genital area are characteristic of scabies. Pediculosis pubis is diagnosed by observing adult lice or their nits in areas that bear coarse hair. The diagnosis of scabies is confirmed by scraping suspicious burrows and viewing the mite or its byproducts under the microscope. Lindane, 1% used in treating scabies, is also very effective for treating pediculosis pubis. Synthetic pyrethrins, also applied as a cream or lotion, are less toxic alternatives for the treatment of either condition. Oral-anal and oral-genital sexual practices predispose male homosexuals to infection with many enteric pathogens, including parasitic protozoans and helminths. The most common of these parasitic infections are amebiasis, caused by Entamoeba histolytica, and giardiasis caused by Giardia lamblia. Both entities may cause acute or chronic diarrhea, as well as other abdominal symptoms. Most gay men with amebiasis are asymptomatic, and invasive disease in this group is extremely rare. Both amebiasis and giardiasis can be diagnosed on the basis of microscopic examination of stool specimens, although duodenal aspiration is occasionally necessary to confirm a diagnosis of giardiasis. Multiple treatment regimens exist for amebiasis. Iodoquinol is a good choice for asymptomatic cyst carriers, whereas the combination of metronidazole plus iodoquinol is used for symptomatic patients. Quinacrine and metronidazole are both efficacious in the treatment of giardiasis.
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PMID:Sexually transmitted parasitic diseases. 201 32

In recent years it has been apparent that many of the known antiparasitic drugs produce free radicals. Intracellular reduction followed by autooxidation yielding O.-2 and H2O2 has been suggested as the mode of action of nifurtimox on Trypanosoma cruzi and as the basis of its toxicity in mammals. On the other hand, free radical intermediates that do not generate oxygen-reduction products under physiological conditions have been found in the metabolic pathways of other antiparasitic nitro compounds (benznidazole, metronidazole, and other 5-nitroimidazoles) used in the treatment of diseases such as Chagas' disease, trichomoniasis, giardiasis, balantidiasis, amebiasis, and schistosomiasis. In these cases, as well as in the case of niridazole (used in the treatment of schistosomiasis), covalent binding or other interactions of the intermediates of nitroreduction with parasite macromolecules are possibly involved in their toxicity. Redox cycling of these compounds under aerobic conditions appears to be a detoxification reaction by inhibiting net reduction of the drugs.
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PMID:Free radical metabolism of antiparasitic agents. 301 65

Cryptosporidiosis, giardiasis, trichomoniasis, and distemper were diagnosed in a 6-month-old female Siberian Husky pup. Poor growth rate, mucopurulent ocular and nasal discharges, and diarrhea were observed. Results of immunologic studies revealed decreased serum IgG concentration and undetectable serum IgA concentration. Cultured lymphocytes yielded a less-than-adequate response to mitogen stimulation. The serum also contained a factor that suppressed mitogen stimulation in control cultured lymphocytes.
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PMID:Cryptosporidiosis associated with immunosuppression attributable to distemper in a pup. 325 52

Metronidazole, a nitroimidazole derivative, is a unique antimicrobial agent that is active against both bacterial and parasitic organisms, although only the anaerobic members of these groups are susceptible. It has been used for the treatment of trichomoniasis for almost 30 years and is also effective in amebiasis and giardiasis. More recently, metronidazole has emerged as a principal agent for the treatment of anaerobic infections. It is highly effective against all species of anaerobes except certain non-spore-forming gram-positive bacilli and cocci and is the only agent rapidly bactericidal against the Bacteroides fragilis group. The hydroxy metabolite is 65% as effective as metronidazole and may play a major therapeutic role. Clinical studies have substantiated its efficacy for prophylaxis during elective colorectal surgical procedures and the treatment of deep abdominal sepsis (usually in combination with another agent such as an aminoglycoside). Metronidazole is the treatment of choice for bacterial vaginosis and seems to be as effective as vancomycin for treatment of Clostridium difficile-related diarrhea and colitis. Good blood levels are produced after both oral and intravenous administration, and side effects are infrequent and minimal. Metronidazole should not be taken during the first trimester of pregnancy because of concerns about mutagenicity. Tinidazole and ornidazole are recently developed nitroimidazole derivatives that have even greater antimicrobial activity than metronidazole.
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PMID:Symposium on antimicrobial agents. Metronidazole. 331 51


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