Levamisole, sold under the brand name Ergamisol among others, is a medication used to treat parasitic worm infections, specifically ascariasis and hookworm infections. It is taken by mouth.
Side effects may include abdominal pain, vomiting, headache, and dizziness. Use is not recommended during breastfeeding or the third trimester of pregnancy. Serious side effects may include an increased risk of infection. It belongs to the anthelmintic class of medications.
Levamisole was invented in 1966 in Belgium by Janssen Pharmaceuticals. It is on the World Health Organization's List of Essential Medicines. Levamisole is also used as a dewormer for cattle. |
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InChI=1S/C11H12N2S/c1-2-4-9(5-3-1)10-8-13-6-7-14-11(13)12-10/h1-5,10H,6-8H2/t10-/m1/s1 |
HLFSDGLLUJUHTE-SNVBAGLBSA-N |
C1CN2C[C@@H](N=C2S1)c1ccccc1 |
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environmental contaminant
Any minor or unwanted substance introduced into the environment that can have undesired effects.
(via 6-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b][1,3]thiazole )
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immunomodulator
Biologically active substance whose activity affects or plays a role in the functioning of the immune system.
immunological adjuvant
A substance that augments, stimulates, activates, potentiates, or modulates the immune response at either the cellular or humoral level. A classical agent (Freund's adjuvant, BCG, Corynebacterium parvum, et al.) contains bacterial antigens. It could also be endogenous (e.g., histamine, interferon, transfer factor, tuftsin, interleukin-1). Its mode of action is either non-specific, resulting in increased immune responsiveness to a wide variety of antigens, or antigen-specific, i.e., affecting a restricted type of immune response to a narrow group of antigens. The therapeutic efficacy is related to its antigen-specific immunoadjuvanticity.
EC 3.1.3.1 (alkaline phosphatase) inhibitor
An EC 3.1.3.* (phosphoric monoester hydrolase) inhibitor that interferes with the action of alkaline phosphatase (EC 3.1.3.1).
xenobiotic
A xenobiotic (Greek, xenos "foreign"; bios "life") is a compound that is foreign to a living organism. Principal xenobiotics include: drugs, carcinogens and various compounds that have been introduced into the environment by artificial means.
(via 6-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b][1,3]thiazole )
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antinematodal drug
A substance used in the treatment or control of nematode infestations.
antirheumatic drug
A drug used to treat rheumatoid arthritis.
immunomodulator
Biologically active substance whose activity affects or plays a role in the functioning of the immune system.
immunological adjuvant
A substance that augments, stimulates, activates, potentiates, or modulates the immune response at either the cellular or humoral level. A classical agent (Freund's adjuvant, BCG, Corynebacterium parvum, et al.) contains bacterial antigens. It could also be endogenous (e.g., histamine, interferon, transfer factor, tuftsin, interleukin-1). Its mode of action is either non-specific, resulting in increased immune responsiveness to a wide variety of antigens, or antigen-specific, i.e., affecting a restricted type of immune response to a narrow group of antigens. The therapeutic efficacy is related to its antigen-specific immunoadjuvanticity.
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View more via ChEBI Ontology
(6S)-6-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b][1,3]thiazole
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levamisol
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WHO MedNet
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lévamisole
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WHO MedNet
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levamisole
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WHO MedNet
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levamisolum
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WHO MedNet
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(−)-6-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b][1,3]thiazole
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ChEBI
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(−)-6-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole
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ChEBI
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(−)-tetramisole
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ChemIDplus
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(S)-(−)-levamisole
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ChemIDplus
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(S)-(−)-tetramisole
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ChEBI
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(S)-2,3,5,6-tetrahydro-6-phenylimidazo[2,1-b]thiazole
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ChEBI
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Ketrax
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KEGG DRUG
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Lepuron
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ChemIDplus
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Levomysol
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ChemIDplus
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Levovermax
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ChEBI
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Totalon
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ChEBI
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Wormicid
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ChemIDplus
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14769-73-4
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CAS Registry Number
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KEGG COMPOUND
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14769-73-4
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CAS Registry Number
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ChemIDplus
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4233256
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Reaxys Registry Number
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Reaxys
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Michaud K, Grabherr S, Shiferaw K, Doenz F, Augsburger M, Mangin P (2014) Acute coronary syndrome after levamisole-adultered cocaine abuse. Journal of forensic and legal medicine 21, 48-52 [PubMed:24365689] [show Abstract] Cocaine is a well known trigger of acute coronary syndromes. Over the last 10 years levamisole, a veterinary anthelminthic drug has been increasingly used as an adulterant of cocaine. Levamisole was used to treat pediatric nephritic syndrome and rheumatoid arthritis before being withdrawn from the market due to its significant toxicity, i.e. hematological complications and vasculitis. The major complications of levamisole-adultered cocaine reported up to now are hematological and dermatological. The case reported here is of a 25 year old man with a history of cocaine abuse who died at home after complaining of retrosternal pain. Postmortem CT-angiography, autopsy, and chemical and toxicological analyses were performed. An eroded coronary artery plaque was found at the proximal segment of the left anterior descending coronary artery. Two myocardial infarct scars were present in the left ventricle. Microscopic examination of the coronary artery revealed infiltration of eosinophils into the adventitia and intima. Toxicological examination confirmed the presence of cocaine and its metabolites in the peripheral blood, and of levamisole in the urine and pericardial fluid. Eosinophilic inflammatory coronary artery pathologies have been clinically linked to coronary dissection, hypersensitivity coronary syndrome and vasospastic allergic angina. The coronary pathology in the presented case could be a complication of levamisole-adultered cocaine use, in which an allergic or immune-mediated mechanism might play a role. The rise in cocaine addiction worldwide and the increase of levamisole adulterated cocaine highlights the importance of updating our knowledge of the effects of adultered cocaine abuse. | Xiao Y, Li J, Fu C (2014) A sensitive method for the determination of levamisole in serum by electrochemiluminescence. Luminescence : the journal of biological and chemical luminescence 29, 183-187 [PubMed:23649929] [show Abstract] A novel method was developed for the determination of levamisole by electrochemiluminescence. The method was based on electrochemiluminescence signal enhancement produced by Ru(bpy)(3)(2+), which reacted with the tertiary amine group of levamisole on a platinum electrode in 12 mmol/L borate buffer (pH 9). A linear relationship between the luminous intensity and concentration of levamisole in the range 0-1 × 10(-7) mol/L was obtained and the detection limit was 1.76 × 10(-11) mol/L. The method is sensitive, selective, simple and convenient. The method has been successfully applied to the analysis of levamisole in serum. | Tallarida CS, Egan E, Alejo GD, Raffa R, Tallarida RJ, Rawls SM (2014) Levamisole and cocaine synergism: a prevalent adulterant enhances cocaine's action in vivo. Neuropharmacology 79, 590-595 [PubMed:24440755] [show Abstract] Levamisole is estimated by the Drug Enforcement Agency (DEA) to be present in about 80% of cocaine seized in the United States and linked to debilitating, and sometimes fatal, immunologic effects in cocaine abusers. One explanation for the addition of levamisole to cocaine is that it increases the amount of product and enhances profits. An alternative possibility, and one investigated here, is that levamisole alters cocaine's action in vivo. We specifically investigated effects of levamisole on cocaine's stereotypical and place-conditioning effects in an established invertebrate (planarian) assay. Acute exposure to levamisole or cocaine produced concentration-dependent increases in stereotyped movements. For combined administration of the two agents, isobolographic analysis revealed that the observed stereotypical response was enhanced relative to the predicted effect, indicating synergism for the interaction. In conditioned place preference (CPP) experiments, cocaine produced a significant preference shift; in contrast, levamisole was ineffective at all concentrations tested. For combination experiments, a submaximal concentration of cocaine produced CPP that was enhanced by inactive concentrations of levamisole, indicating synergism. The present results provide the first experimental evidence that levamisole enhances cocaine's action in vivo. Most important is the identification of synergism for the levamisole/cocaine interaction, which now requires further study in mammals. | Suran J, Flajs D, Peraica M, Prevendar Crnić A, Speranda M, Božić F (2013) Pharmacokinetics of an immunomodulating dose of levamisole in weaned pigs. Acta veterinaria Hungarica 61, 376-382 [PubMed:23921349] [show Abstract] Levamisole has been shown to stimulate the immune response in immunocompromised humans and animals. However, its use as an adjuvant in immunocompromised weaned pigs prone to colibacillosis has only been experimentally tested but not yet officially approved. Therefore, the aim of these studies was to study the pharmacokinetics (PK) of an immunomodulating dose of levamisole in weaned pigs. For that purpose, 20 weaned crossbred pigs were divided into two treatment groups. In this parallel-design study, a single dose of levamisole (2.5 mg/kg body weight) was administered by the intramuscular (i.m.) or oral (p.o.) route. Statistically significant differences between the i.m. and p.o. routes in terminal beta rate constant (β), maximum plasma concentration (Cmax), area under the curve (AUC) for plasma concentration-time curve from time zero to infinity (AUC0-inf), area under the plasma concentration-time curve from time 0 to the last quantifiable time point (AUC0-t) were determined. Further research is needed to establish a relationship between the PK and the immunomodulating effect of levamisole in pigs. | Shea JL (2013) Bioanalytical methods for quantitation of levamisole, a widespread cocaine adulterant. Clinical chemistry and laboratory medicine 51, 205-212 [PubMed:23152411] [show Abstract] Abstract Levamisole is an anthelminthic that was first used as a de-worming agent in humans and animals. It has also been used to treat inflammatory conditions as well as certain types of cancer. Levamisole was discontinued for human use in the early 21st century due to toxic side effects including agranulocytosis and vasculitis. Recently, levamisole was discovered as a cocaine adulterant after reports emerged of drug users with the above disorders. As the prevalence of cocaine usage has grown in the last 15 years, measurement of levamisole in human samples has become increasingly important. This review focuses on the various bioanalytical methods available for the determination of levamisole in human plasma and urine. Earlier methods employed gas chromatography coupled with nitrogen-selective thermionic specific detection and nitrogen-phosphorus detection, as well as high performance liquid chromatography coupled with ultraviolet detection. In addition, gas chromatography-mass spectrometry (GC-MS) and high performance liquid chromatography-tandem mass spectrometry (LC-MS/MS) have also been described. Currently, GC-MS appears to be the method of choice however recent developments in the area of LC-MS/MS make this technology an attractive alternative. The merits of both GC-MS and LC-MS/MS for the determination of levamisole are evaluated on the basis of sample preparation, chromatographic separation conditions, run time, and analytical performance. In addition, emerging methods in this area are also reviewed. | Sanadgol H (2013) Levamisole usage as an adjuvant to hepatitis B vaccine in hemodialysis patients, yes or no? Nephro-urology monthly 5, 673-678 [PubMed:23577329] [show Abstract]
BackgroundHepatitis B virus (HBV) infection is much more common in hemodialysis patients than the general population. These patients have an impaired immune response to HBV vaccination; to that end there are certain studies that have evaluated levamisole as an immunomodulator agent improving HBV vaccination response rate in hemodialysis patients.ObjectivesIn the current review, we have assembled all of the results to determine whether lavamisole is of value as an adjuvant to HBV vaccination in hemodialysis patients.Materials and methodsScience Direct (Elsevier), ProQuest, Springer, MD Consult, BMJ Journals, Pubmed and Wiley were searched for levamisole application to HBV vaccination in hemodialysis patients. All studies revealed a seroconversion response level between levamisole plus HBV vaccine versus HBV vaccine alone.ResultsFrom 10 relevant studies, 5 studies fulfilled our inclusion criteria. Three of them suggested the significant benefit of adding levamisole to the HBV vaccine to increase augment seroprotection level in hemodialysis patients. Another study reported a decrease in seroprotection level and another study showed no significant difference caused by levamisole administration.ConclusionsDue to the limited number of studies evaluated, it is challenging to perform a definite decision about routinely administering levamisole in addition to the HBV vaccine for all hemodialysis patients. However, it does seem reasonable to recommend administration of levamisole for impaired immune response patients. | Abdul-Karim R, Ryan C, Rangel C, Emmett M (2013) Levamisole-induced vasculitis. Proceedings (Baylor University. Medical Center) 26, 163-165 [PubMed:23543977] [show Abstract] Levamisole-contaminated cocaine is an increasingly reported cause of a syndrome characterized by vasculitic skin lesions and immunologic abnormalities. With approximately 70% of cocaine in the United States now contaminated with levamisole, the incidence of this syndrome is likely to increase. We report two cases of this syndrome and review its clinical presentation, course, and prognosis. | Casale JF, Colley VL, Legatt DF (2012) Determination of phenyltetrahydroimidazothiazole enantiomers (Levamisole/Dexamisole) in illicit cocaine seizures and in the urine of cocaine abusers via chiral capillary gas chromatography-flame-ionization detection: clinical and forensic perspectives. Journal of analytical toxicology 36, 130-135 [PubMed:22337783] [show Abstract] Illicit cocaine laboratories in South America have been adding phenyltetrahydroimidazothiazole enantiomers (levamisole and/or tetramisole) to refined illicit cocaine for over 8 years. A chiral capillary gas chromatographic methodology is presented for phenyltetrahydroimidazothiazole enantiomer determination in illicit cocaine samples and in the urine of cocaine abusers. Illicit cocaine samples (N = 752) and urine specimens from cocaine abusers (N = 50) that contained phenyltetrahydroimidazothiazole were analyzed for enantiomeric composition. Legitimate commercial preparations of phenyltetrahydroimidazothiazole are either 100% levamisole or a 50:50 mixture of levamisole and dexamisole (tetramisole). Specimens that contain phenyltetrahydroimidazothiazole mixtures that are other than 50:50 preparations will be enhanced in one isomer over the other, and they are referred to as either "levamisole-enhanced" or "dexamisole-enhanced". Cocaine samples were found to contain levamisole (N = 495, 66%), tetramisole (N = 143, 19%), and levamisole-enhanced enrichment (N = 114, 15%); urine specimens contained levamisole (N = 23, 46%), levamisole-enhanced enrichment (N = 10, 20%), and dexamisole-enhanced enrichment (N = 13, 26%). The toxicological and forensic aspects of these findings are discussed. | Dy IA, Wiernik PH (2012) Cocaine-levamisole thrombotic vasculopathy. Seminars in thrombosis and hemostasis 38, 780-782 [PubMed:23041983] [show Abstract] The syndrome of cocaine-levamisole thrombotic vasculopathy is a tetrad of cutaneous manifestations, arthralgia, leukopenia, and positive antineutrophil cytoplasmic antigen (ANCA). Cocaine is cut with levamisole to potentiate its euphoric effects. However, along with this are the adverse reactions of levamisole such as fatal agranulocytosis, flu-like symptoms, and cutaneous thrombotic vasculopathy. High index of suspicion is needed for its diagnosis. This article will review on its toxicities, especially its prothrombotic effects. | Martin RJ, Robertson AP, Buxton SK, Beech RN, Charvet CL, Neveu C (2012) Levamisole receptors: a second awakening. Trends in parasitology 28, 289-296 [PubMed:22607692] [show Abstract] Levamisole and pyrantel are old (1965) but useful anthelmintics that selectively activate nematode acetylcholine ion channel receptors; they are used to treat roundworm infections in humans and animals. Interest in their actions has surged, giving rise to new knowledge and technical advances, including an ability to reconstitute receptors that reveal more details of modes of action/resistance. We now know that the receptors are plastic and may form diverse species-dependent subtypes of receptor with different sensitivities to individual cholinergic anthelmintics. Understanding the biology of the levamisole receptors is expected to inform other studies on anthelmintics (ivermectin and emodepside) that act on ion channels. | Martin RJ, Robertson AP (2007) Mode of action of levamisole and pyrantel, anthelmintic resistance, E153 and Q57. Parasitology 134, 1093-1104 [PubMed:17608969] [show Abstract] Here we review molecular information related to resistance to the cholinergic anthelmintics in nematodes. The amount of molecular information available varies between the nematode species, with the best understood so far being C. elegans. More information is becoming available for some other parasitic species. The cholinergic anthelmintics act on nematode nicotinic acetylcholine receptors located on somatic muscle cells. Recent findings demonstrate the presence of multiple types of the nicotinic receptors in several nematodes and the numerous genes required to form these multimeric proteins. Not only are the receptors the product of several genes but they are subject to modulation by several other proteins. Mutations altering these modulatory proteins could alter sensitivity to the cholinergic anthelmitics and thus lead to resistance. We also discuss the possibility that resistance to the cholinergic anthelmintics is not necessarily the result of a single mutation but may well be polygenic in nature. Additionally, the mutations resulting in resistance may vary between different species or between resistant isolates of the same species. A list of candidate genes to examine for SNPs is presented. | Scheinfeld N, Rosenberg JD, Weinberg JM (2004) Levamisole in dermatology : a review. American journal of clinical dermatology 5, 97-104 [PubMed:15109274] [show Abstract] Levamisole, an anthelmintic agent with a wide range of immunomodulatory actions, has been used successfully as monotherapy and an adjunct to treatment in a variety of diseases. Since 1990, combination therapy of levamisole and fluorouracil has played an important role in the treatment of resected Dukes stage C adenocarcinoma of the colon. Because of its immunomodulating effects levamisole has been used in a wide range of diseases with and without success. In dermatologic disease levamisole has been successfully used in the treatment of parasitic, viral and bacterial infections including leprosy, collagen vascular diseases, inflammatory skin diseases and children with impaired immune a variety of reasons. It has also been used in combination with other drugs for treating a number of dermatologic disorders, e.g. in combination with cimetidine for treating recalcitrant warts, with prednisolone for treating lichen planus, erythema multiforme and aphthous ulcers of the mouth. Adverse affects of levamisole are mild and infrequent and include rash, nausea, abdominal cramps, taste alteration, alopecia, arthralgia, and a flu-like syndrome. It can rarely cause agranulocytosis. More studies need to be undertaken to study the full potential of levamisole in dermatologic diseases. | Kutzler MA, Solter PF, Hoffman WE, Volkmann DH (2003) Characterization and localization of alkaline phosphatase in canine seminal plasma and gonadal tissues. Theriogenology 60, 299-306 [PubMed:12749943] [show Abstract] Alkaline phosphatase (AP) is a useful indicator of the presence of the sperm-rich (2nd) fraction in the canine ejaculate. Two AP isoenzymes originating from separate genes have been identified in the dog: tissue nonspecific (TNS) and intestinal. Bone, liver, and corticosteroid-induced AP are different isoforms of the TNS and intestinal isoenzymes. Using gel electrophoresis and levamisole inhibition assays, it was determined that seminal plasma AP (SAP) is a unique isoform of canine TNS AP whose glycosylation is distinct from either of the TNS AP isoforms commonly found in canine serum. Using immunocytochemistry, SAP activity was localized to the epididymal and seminiferous tubular epithelium. The ability to distinguish SAP from bone AP, liver AP and corticosteroid-induced AP could be beneficial to the practitioner in determining the quality of a semen sample. | Magnusson P, Farley JR (2002) Differences in sialic acid residues among bone alkaline phosphatase isoforms: a physical, biochemical, and immunological characterization. Calcified tissue international 71, 508-518 [PubMed:12232676] [show Abstract] High-performance liquid chromatography (HPLC) separates three human bone alkaline phosphatase (BALP) isoforms in serum; two major BALP isoforms, B1 and B2, and a minor fraction, B/I, which is composed on average of 70% bone and 30% intestinal ALP. The current studies were intended to identify an in vitro source of the BALP isoforms for physical, biochemical, and immunological characterizations. The three BALP isoforms were identified in extracts of human osteosarcoma (SaOS-2) cells, by HPLC, after separation by anion-exchange chromatography. All three BALP isoforms were similar with respect to freeze-thaw stability, solubility, heat inactivation, and inhibition by L-phenylalanine, L-homoarginine, and levamisole. The isoforms were also kinetically similar (i.e., maximal velocity and KM at pH 8.8 and pH 10.0). The isoforms differed, however, with respect to sensitivity to precipitation with wheat germ agglutinin (WGA), P < 0.001, but not Concanavalin A. At 3.0 mg/ml, WGA precipitated approximately 25% of B/I but more than 80% of B1 and B2. Molecular weights were estimated by native gradient gel electrophoresis: B/I, 126 kDa; B1, 136 kDa; and B2, 141 kDa. Desialylation with neuraminidase reduced the apparent sizes of B1 and B2 to 127 kDa (i.e., approximately to that of B/I). The total carbohydrate content was calculated to be 18 kDa, 28 kDa, and 33 kDa (i.e., 14%, 21%, and 23%) for the BALP isofonns, B/I, B1, and B2, respectively. The number of sialic acid residues was estimated to be 29 and 45, for each B1 and B2 homodimer, respectively. Apparent discrepancies between these estimates of molecular weight and estimates based on gel filtration chromatography were attributed to nonspecific interactions between carbohydrate residues and the gel filtration beads. All three BALP isoforms showed similar dose-dependent linearity in the commercial Alkphase-B and Tandem-MP Ostase immunoassays, r = 0.944 and r = 0.985, respectively (P < 0.001). In summary, our data indicate that B1 and B2 have more (or more reactive) sialic acid residues compared with B/I, which mainly explains the apparent differences in molecular weight. Future investigations will focus on the clinical and functional significance of the revealed differences in sialic acid residues. | Sanchez MR (2000) Miscellaneous treatments: thalidomide, potassium iodide, levamisole, clofazimine, colchicine, and D-penicillamine. Clinics in dermatology 18, 131-145 [PubMed:10701095] | Amery WK, Bruynseels JP (1992) Levamisole, the story and the lessons. International journal of immunopharmacology 14, 481-486 [PubMed:1618599] [show Abstract] The history of the use of levamisole in man is summarized, from its start as an anthelmintic in the early sixties, through its world-wide recognition as an immunotropic agent especially in the seventies and early eighties, and its return to clinical prominence in 1989-90 as an effective adjuvant treatment for operable colon cancer. The knowledge accumulated from experimental tumour models and from clinical use in various types of cancer, supplemented with the recent evidence obtained from large-scale controlled trials in resectable colon cancer is reviewed. It is speculated that we may not have seen the end of levamisole story yet; also, the role of serendipidity in drug research is emphasized. | Janssen PA (1991) Levamisole as an adjuvant in cancer treatment. Journal of clinical pharmacology 31, 396-400 [PubMed:2050823] | Drannik GN, Kolesnik NA (1982) [Use of levamisole in nephrological practice (a review of the literature)]. Vrachebnoe delo12-16 [PubMed:7051554] | Spreafico F (1980) Use of levamisole in cancer patients. Drugs 20, 105-116 [PubMed:6995092] | Miller MJ (1980) Use of levamisole in parasitic infections. Drugs 20, 122-130 [PubMed:6995094] [show Abstract] Levamisole is a drug of choice for treatment of ascariasis. With recommended dosages, it is virtually free of side effects. Single doses of 50 to 150mg will eliminate all parasites in 90 to 100% of ascariasis patients irrespective of worm burden. Activity against hookworms has been demonstrated for levamisole but the most effective treatment regimen has not been determined. Further drug trials are needed for better assessment of efficacy. Levamisole has little or no curative action on infections with whipworms and pinworms. It may have some activity against strongyloides but confirmatory studies are needed. It has been shown that levamisole has significant activity against microfilariae of Wuchereria bancrofti and Brugia malayi. It is not, however, as effective as diethylcarbamazine ('Hetrazan'), and side reactions are greater. In tolerated doses, levamisole does not have significant action on adult forms or microfilariae of Onchoceea volvulus. The drug applied topically, however, may find a place in treatment of ocular onchocerciasis. Limited trials with levamisole for toxoplasmosis and chronic cutaneous leishmaniasis have given promising results, and further studies are indicated. | Symoens J, Veys E, Mielants M, Pinals R (1978) Adverse reactions to levamisole. Cancer treatment reports 62, 1721-1730 [PubMed:365327] [show Abstract] The adverse reactions mentioned in 267 reports on levamisole are analyzed. Significant adverse reactions are agranulocytosis, skin rash, and febrile illness. They occur in a small subpopulation of patients only, predominantly those with rheumatoid arthritis. Other side effects rarely necessitate discontinuation of treatment. Levamisole did not appear to cause renal or liver toxicity. By means of a questionnaire, cases of blood dyscrasia were analyzed in detail. Agranulocytosis (less than 20% neutrophils) occurs most frequently in patients with rheumatic diseases, in women, and in HLA B27 genotypes. It is spontaneously reversible when treatment is discontinued. The bone marrow is not damaged. Thrombocytopenia has a course similar to that of agranulocytosis but it is very rare. Leukopenia (less than 3000 cells/mm3 but greater than 20% neutrophils) seems to differ from agranulocytosis in a number of ways and is not an indication to discontinue treatment. It is concluded that, if used under the close supervision of a physician, for those clinical situations in which levamisole has proven efficacy, the potential benefit to the patient outweighs the hazards and justifies its use. | Hozumi T, Iwaguchi T, Kitagawa H, Ozawa H (1978) Anticancer activity of isomers of 6-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole. Gan 69, 339-343 [PubMed:669135] [show Abstract] Three phenylimidazothiazole isomers, L-(-)-form (levamisole), D-(+)-form (dexamisole), and DL-(+/-)-form (tetramisole), modulate mouse and rat immune responsiveness. They depress the relapse of urinary bladder cancer, BC-47, when they are used with 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU) for treatment of rats bearing BC-47. Levamisole was the most effective isomer. Effectiveness of the isomers is expressed by their ability to enhance the number of plaque-forming cells to sheep red blood cells. They also stimulate the DNA synthesis of murine lymphocytes in vitro. | Wilton JM (1978) Levamisole in chronic inflammatory diseases. The Journal of rheumatology. Supplement 4, 101-113 [PubMed:366135] [show Abstract] The use of levamisole in a variety of non-rheumatoid chronic inflammatory diseases has been reviewed. Both the clinical responses and the in vivo and in vitro tests of immunological function during levamisole therapy are discussed in an attempt to correlate the immuno-stimulatory properties of the drug with any therapeutic effect. It was concluded that in many diseases there are conflicting reports on the usefulness of levamisole and that there were few correlates of the therapeutic and immunological effects of the drug. There was, however, evidence that the drug may prove clinically useful and more double-blind, multicentre controlled studies with adequate laboratory testing are needed. At present levamisole would appear to be useful in the treatment of Crohn's disease, recurrent oral ulceration, and herpes simplex infections. | Amery WK, Verhaegen H (1978) Effects of levamisole treatment in cancer patients. The Journal of rheumatology. Supplement 4, 123-135 [PubMed:366137] [show Abstract] Twenty-six controlled prognostic evaluations of the adjuvant use of levamisole in cancer are reviewed. The results favor intermittent administration of levamisole in a dosage that is adapted to the patient's weight or body surface. Early treatment is indicated, but synchronous treatment with cytotoxic therapies is to be avoided. The best results have been achieved in advanced but still potentially curable patients. Major toxicity occurs very seldom and measures are suggested to further characterize the few patients who are at risk of developing allergic agranulocytosis, a potentially life-threatening side effect. | Vanhoutte PM, Van Nueten JM, Verbeuren TJ, Laduron PM (1977) Differential effects of the isomers of tetramisole on adrenergic neurotransmission in cutaneous veins of dog. The Journal of pharmacology and experimental therapeutics 200, 127-140 [PubMed:189006] [show Abstract] Clinical observations indicate that dexamisole and levamisole, the isomers of tetramisole, cause mood elevation. Their effects on smooth muscle cells and adrenergic nerves were investigated in strips of dogs' saphenous veins. Dexamisole (2.5 X 10(-6) to 4 X 10(-5) M) augmented the contractile response to norepinephrine but depressed that to tyramine; cocaine inhibited the augmentation of the norepinephrine response. Levamisole (10(-5) M) did not alter the response to norepinephrine, but augmented that to tyramine. At 1.6 X 10(-4) M dexamisole, more than levamisole, depressed the responses to norepinephrine, tyramine and acetylcholine. Activation by K+ ions was not affected by the isomers. Preparations, incubated with 3H-norepinephrine, were mounted for superfusion, tension recording and determination of 3H-norepinephrine and metabolites in the superfusate. Dexamisole and levamisole augmented the 3H-norepinephrine overflow during nerve stimulation; levamisole decreased the efflux of deaminated metabolites. During tyramine-induced contractions, dexamisole depressed and levamisole augmented the efflux of 3H-norepinephrine; they reduced the appearance of metabolites. The increases in 3H-norepinephrine caused by the isomers during nerve stimulation were not seen after phenoxybenzamine. Dexamisole, more than levamisole, inhibited tissular uptake of 3H-norepinephrine. Levamisole, more than dexamisole, inhibited monoamine oxidase activity in vein homogenates. These interferences with release and disposition of norepinephrine may be related to the antidepressant properties of the tetramisole isomers. | Janssen PA (1976) The levamisole story. Progress in drug research. Fortschritte der Arzneimittelforschung. Progres des recherches pharmaceutiques 20, 347-383 [PubMed:827785] |
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