DOCSLIB.ORG

Practical Pharmacy Is to Provide Accessible and Accurate Information on Medicines Issues for Front-Line Health Workers Who May Not Have Any Pharmaceutical Training

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
Practical Pharmacy Is to Provide Accessible and Accurate Information on Medicines Issues for Front-Line Health Workers Who May Not Have Any Pharmaceutical Training PPracticalractical PharmacyPharmacy For Developing Countries NOTE TO OUR READERS: The goal of Practical Pharmacy is to provide accessible and accurate information on medicines issues for front-line health workers who may not have any pharmaceutical training. This issue of Practical Pharmacy would be best used as a supplement to your national Tuberculosis (TB) guidelines. It is extremely important for all people involved in TB care to have access to the national treatment guidelines. We therefore encourage you to get in contact with your National TB Program Centre for these resources. We are aware, however, that in some countries it may be diffi cult to obtain copies of these guidelines; in some cases they may not even be available at all. Aside from national guidelines, another “must have” is the WHO Treatment of Tuberculosis Guidelines for National Programs 2003 (see the reference section on the fi nal page). These guidelines provide a comprehensive information on all aspects of TB treatment. WWhathat iiss TTuberculosisuberculosis Treatment of TB is carried out according to your national guidelines. You should refer to the Tuberculosis (TB) infection is caused by QUICK TIP! national guidelines for specifi c details about bacteria – bacilli called Mycobacterium treatment regimens and procedures of your Tuberculosis. When a person with The common symptoms of active country. We have summarised the most TB infection coughs or sneezes, they TB disease are common treatment regimens [see page 3]. These release tiny particles containing TB persistent cough, regimens are based on the characteristics and bacilli into the air. A person who is bloody sputum, proven effi cacy of the medicines, although exposed to the bacilli becomes infected weight loss or loss regimens may deviate from this under some if they inhale the airborne bacilli into of appetite, fatigue, circumstances (e.g. known resistance, their lungs. fever, or night sweats. pregnancy, treatment of children), or according TB infection or non-active TB means to local guidelines. that TB bacilli are in the body, but the immune system Reminder: Commonly used abbreviations is keeping them under control. Active TB, on the other hand, develops when the immune system cannot Isoniazid H INH keep the TB bacilli under control and the bacilli begin Rifampicin to multiply rapidly. When the bacteria become active, (aka Rifampin) R RIF a person becomes ill with TB, and this can occur Pyrazinamide Z PZA Ethambutol E EMB when the person’s immunity goes down or is reduced. Streptomycin S SM Conditions that can reduce a person’s immunity include: HIV, malnutrition, advancing age, or some Standard adult treatment regimens start with an other diseases. initial (or intensive) phase of two months, normally consisting of Isoniazid, Rifampicin, Pyrazinamide and People who have TB infection (non-active TB disease) Ethambutol. [See table 1, page 2] During the initial phase, are NOT infectious. However, people with untreated TB bacilli are killed rapidly, infectious patients quickly active TB are infectious, and must be treated as soon become non-infectious (usually within 2 weeks) and as possible. symptoms improve. This is followed by a continuation phase of 4 to 6 months, normally consisting of Isoniazid and Rifampicin (although sometimes HHowow iiss TTuberculosisuberculosis ttreated?reated? Isoniazid and Ethambutol are used). During the According to the World health Organization (WHO), continuation phase, the medicines eliminate remaining the aims of TB treatment are: bacilli and prevent subsequent relapse. • to cure the patient of TB, • to prevent death from active TB or its Dosing frequency late effects, QUICK TIP! Treatment may be administered daily, fi ve-times If not treated, a • to prevent relapse of TB, per week (Monday to Friday), or three-times per person with active • to decrease transmission of TB to TB can infect on week (usually Monday, Wednesday and Friday). others, average 10 to 15 This is decided by each national TB program. It • to prevent the development of people every year. must be noted that twice-weekly regimens are acquired drug resistance. no longer recommended. continued on page 2... PracticalPractical PharmacyPharmacy Issue 18:18: MarchMarch 22008008 1 Table 1: Common treatment regimens Initial Phase Continuation Phase New Cases 2 months HRZE 4 months HR or 6 months HE Retreatment Cases 2 months HRZE S 1 month HRZE 5 months HRE Chronic Cases and Drug- According to your national guidelines resistant TB Retreatment QUICK TIP! If a patient has undergone a course of TB treatment, Directly Observed Treatment Providing a and is found to have TB infection either at the (DOT) is currently the most supportive and end of the course (failure), or at some time in the recommended adherence effi cient service in future (relapse), they will need to be considered method. DOT entails having your facility is one for retreatment. This is an important time for you a patient’s treatment fully of the best aids to treatment adherence. to update the patient’s understanding of their TB observed by a treatment treatment, and to reassess and reinforce medication supporter. This ensures adherence. that every TB patient has the support of another concerned individual and guarantees better treatment The most common retreatment regimen is shown adherence. in the table above, and involves two months of an additional agent, the injectable aminoglycoside Streptomycin. However, some retreatment cases may have drug-resistant TB, so retreatment policies are entirely dependant on your national TB program and the laboratory resources that are available in your area. The best programs perform drug-susceptibility QUICK TIP! testing (DST), and this Empowerment of TB should be performed patients can also be before each patient begins assisted by encouraging Zellweger P. J. Library/ Image Health Lung Credit: a retreatment regimen. patients to interact with The treatment regimen one another, such as Supervision of drug intake at the TB hospital in Cotonou, Benin can later be adjusted through the daily visits “Because of the length of time the patient has to according to DST results to the health facility for DOT take treatment, completing TB treatment is a special and available second-line challenge and requires an unyielding sense of agents. commitment. This may be easy to sustain while the patient feels sick. However, after a few weeks of Adherence and DOT taking treatment, patients often feel better and see Adherence to TB no reason for continuing their treatment. It is thus treatment is not essential for health workers or treatment supporters easy due to the to be supportive and use the initial period to bond with heavy pill burden, the patient. This will enable them to build a strong the potential side- relationship in which the patient believes and trusts effects and the long advice given by the treatment supporter.” (Source: South African Guidelines) duration of treatment. Empowering the Reminder: DOT vs DOTS patients (and 1. DOT stands for Directly Observed Treatment, their families) with and is the strategy of having all of a TB patient’s information about TB medicine doses observed by a designated person is essential to allow (health care worker, or trained and supervised them to take positive community member) to help ensure adherence to control of their health therapy. and to give them Credit: Lung Health Image Library/Pierre Virot 2. DOTS stands for Directly Observed Treatment the best chance of Short-course refers to WHO’s comprehensive treatment success. A TB patient takes his medication “Internationally recommended policy package for From a public health TB control” to which countries are recommended point of view it is critical to stop both the spread of TB to adapt their TB programs (DOT is one element to others, and the development of drug resistance. of DOTS). PracticalPractical PharmacyPharmacy Issue 18:18: MarchMarch 22008008 2 TTuberculosisuberculosis MMedicinesedicines Table 2: Adult and children weight-based doses of fi rst-line medicines ONCE DAILY THREE TIMES WEEKLY Medication Potency Maximum Dose Dose and range Maximum Dose (common presentation) Dose and range (mg/kg) (mg) (mg/kg) (mg) Isoniazid (H) 5 10 High 300 600 (100, 300mg) (4-6) (8-12) Rifampicin (R) 10 10 High 600 600 (150, 300mg) (8-12) (8-12) Ethambutol (E) Adult: 15 Child: 20 30 Low 1600 2400 (100, 400mg) (15-20) (15-25) (25-35) Pyrazinamide (Z) 25 35 Low 2000 3000 (400mg) (20-30) (30-40) Streptomycin (S) 15 15 Low 1000 1000 (1g vial) (12-18) (12-18) Note: 1. Doses are based on WHO Guidelines (doses differ in some guidelines, but may be based on differently resourced settings) 2. Retreatment doses may be higher – refer to your national guidelines or WHO Drug-Resistant TB Guidelines • Pyridoxine (Vitamin B6) 10-30mg daily should always be given with isoniazid • WHO now discourages the use of thioacetazone because of the risk of side effects, especially for people living with HIV • For second-line medicines refer to the WHO Guidelines for the programmatic management of drug-resistant tuberculosis 2006 (available at http://www.who.int/tb/publications/en/ ) • No new TB medicines have been developed for the standard regimen since Credit: Lung Health Image Library/Pierre Virot Thiacetazone causes serious, sometimes the 1960s. This highlights the urgent need for medicines development for TB fatal, side effects in many HIV positive and other neglected diseases patients Fixed-Dose Combination tablets (FDCs) QUICK TIP! The use of FDCs makes TB treatment easier for both patients and healthcare workers. Soon after TB • For patients, FDCs reduce the number of tablets to take and help to minimise treatment is dosing errors, thereby improving adherence and reducing the chance of developing initiated, a patient’s resistance or side effects. health improves and • For healthcare workers, FDCs simplify dosing recommendations and weight-based their infectiousness declines.
Load more

Recommended publications
  • The Anthelmintic Niclosamide Is a Potent TMEM16A Antagonist That Fully Bronchodilates Airways
    bioRxiv preprint doi: https://doi.org/10.1101/254888; this version posted January 27, 2018. The copyright holder for this preprint (which was not certified by peer review) is the author/funder, who has granted bioRxiv a license to display the preprint in perpetuity. It is made available under aCC-BY-ND 4.0 International license. The anthelmintic niclosamide is a potent TMEM16A antagonist that fully bronchodilates airways Kent Miner1, Benxian Liu1, Paul Wang2, Katja Labitzke2,†, Kevin Gaida1, Jian Jeffrey Chen3, Longbin Liu3,†, Anh Leith1,†, Robin Elliott1, Kathryn Henckels1, Esther Trueblood4,†, Kelly Hensley4, Xing-Zhong Xia1, Oliver Homann5, Brian Bennett1, Mike Fiorino1, John Whoriskey1, Sabine Escobar1, Gang Yu1, Joe McGivern2, Min Wong1, Teresa L. Born1,†, Alison Budelsky1,†, Mike Comeau1, Dirk Smith1,†, Jonathan Phillips1, James A. Johnston1, Kerstin Weikl2,†, David 2 1,* 2,†.* 1,† ,* Powers , Deanna Mohn , Andreas Hochheimer , John K. Sullivan 1Department of Inflammation Research, Amgen Inc., Thousand Oaks, CA and Seattle, WA, USA 2Department of Therapeutic Discovery, Amgen Inc., Thousand Oaks, CA, USA and Regensburg, Germany 3Department of Medicinal Chemistry, Amgen Inc., Thousand Oaks, CA, USA 4Department of Comparative Biology and Safety Sciences, Amgen Inc., Seattle, WA, Thousand Oaks, CA and South San Francisco, CA, USA 5Genome Analysis Unit, Amgen Inc., South San Francisco, CA, USA †Present address; see Additional Information section *Corresponding authors. E-mails: [email protected] (J.K.S); [email protected] (A.H.); [email protected] (D.M.) Abstract There is an unmet need in severe asthma where approximately 40% of patients exhibit poor -agonist responsiveness, suffer daily symptoms and show frequent exacerbations. 2+ Antagonists of the Ca -activated-Cl¯ channel, TMEM16A, offers a new mechanism to bronchodilate airways and block the multiple contractiles operating in severe disease.
    [Show full text]
  • Anthelmintic Activity of Yeast Particle-Encapsulated Terpenes
    molecules Article Anthelmintic Activity of Yeast Particle-Encapsulated Terpenes Zeynep Mirza 1, Ernesto R. Soto 1 , Yan Hu 1,2, Thanh-Thanh Nguyen 1, David Koch 1, Raffi V. Aroian 1 and Gary R. Ostroff 1,* 1 Program in Molecular Medicine, University of Massachusetts Medical School, Worcester, MA 01605, USA; [email protected] (Z.M.); [email protected] (E.R.S.); [email protected] (Y.H.); [email protected] (T.-T.N.); [email protected] (D.K.); raffi[email protected] (R.V.A.) 2 Department of Biology, Worcester State University, Worcester, MA 01602, USA * Correspondence: gary.ostroff@umassmed.edu; Tel.: 508-856-1930 Academic Editor: Vaclav Vetvicka Received: 2 June 2020; Accepted: 24 June 2020; Published: 27 June 2020 Abstract: Soil-transmitted nematodes (STN) infect 1–2 billion of the poorest people worldwide. Only benzimidazoles are currently used in mass drug administration, with many instances of reduced activity. Terpenes are a class of compounds with anthelmintic activity. Thymol, a natural monoterpene phenol, was used to help eradicate hookworms in the U.S. South circa 1910. However, the use of terpenes as anthelmintics was discontinued because of adverse side effects associated with high doses and premature stomach absorption. Furthermore, the dose–response activity of specific terpenes against STNs has been understudied. Here we used hollow, porous yeast particles (YPs) to efficiently encapsulate (>95%) high levels of terpenes (52% w/w) and evaluated their anthelmintic activity on hookworms (Ancylostoma ceylanicum), a rodent parasite (Nippostrongylus brasiliensis), and whipworm (Trichuris muris). We identified YP–terpenes that were effective against all three parasites.
    [Show full text]
  • Antiparasitic Properties of Cardiovascular Agents Against Human Intravascular Parasite Schistosoma Mansoni
    pharmaceuticals Article Antiparasitic Properties of Cardiovascular Agents against Human Intravascular Parasite Schistosoma mansoni Raquel Porto 1, Ana C. Mengarda 1, Rayssa A. Cajas 1, Maria C. Salvadori 2 , Fernanda S. Teixeira 2 , Daniel D. R. Arcanjo 3 , Abolghasem Siyadatpanah 4, Maria de Lourdes Pereira 5 , Polrat Wilairatana 6,* and Josué de Moraes 1,* 1 Research Center for Neglected Diseases, Guarulhos University, Praça Tereza Cristina 229, São Paulo 07023-070, SP, Brazil; [email protected] (R.P.); [email protected] (A.C.M.); [email protected] (R.A.C.) 2 Institute of Physics, University of São Paulo, São Paulo 05508-060, SP, Brazil; [email protected] (M.C.S.); [email protected] (F.S.T.) 3 Department of Biophysics and Physiology, Federal University of Piaui, Teresina 64049-550, PI, Brazil; [email protected] 4 Ferdows School of Paramedical and Health, Birjand University of Medical Sciences, Birjand 9717853577, Iran; [email protected] 5 CICECO-Aveiro Institute of Materials & Department of Medical Sciences, University of Aveiro, 3810-193 Aveiro, Portugal; [email protected] 6 Department of Clinical Tropical Medicine, Faculty of Tropical Medicine, Mahidol University, Bangkok 10400, Thailand * Correspondence: [email protected] (P.W.); [email protected] (J.d.M.) Citation: Porto, R.; Mengarda, A.C.; Abstract: The intravascular parasitic worm Schistosoma mansoni is a causative agent of schistosomiasis, Cajas, R.A.; Salvadori, M.C.; Teixeira, a disease of great global public health significance. Praziquantel is the only drug available to F.S.; Arcanjo, D.D.R.; Siyadatpanah, treat schistosomiasis and there is an urgent demand for new anthelmintic agents.
    [Show full text]
  • Antiprotozoal and Antitumor Activity of Natural Polycyclic Endoperoxides: Origin, Structures and Biological Activity
    molecules Review Antiprotozoal and Antitumor Activity of Natural Polycyclic Endoperoxides: Origin, Structures and Biological Activity Valery M. Dembitsky 1,2,*, Ekaterina Ermolenko 2, Nick Savidov 1, Tatyana A. Gloriozova 3 and Vladimir V. Poroikov 3 1 Centre for Applied Research, Innovation and Entrepreneurship, Lethbridge College, 3000 College Drive South, Lethbridge, AB T1K 1L6, Canada; [email protected] 2 A.V. Zhirmunsky National Scientific Center of Marine Biology, 17 Palchevsky Str., 690041 Vladivostok, Russia; [email protected] 3 Institute of Biomedical Chemistry, 10 Pogodinskaya Str., 119121 Moscow, Russia; [email protected] (T.A.G.); [email protected] (V.V.P.) * Correspondence: [email protected]; Tel.: +1-403-320-3202 (ext. 5463); Fax: +1-888-858-8517 Abstract: Polycyclic endoperoxides are rare natural metabolites found and isolated in plants, fungi, and marine invertebrates. The purpose of this review is a comparative analysis of the pharmacological potential of these natural products. According to PASS (Prediction of Activity Spectra for Substances) estimates, they are more likely to exhibit antiprotozoal and antitumor properties. Some of them are now widely used in clinical medicine. All polycyclic endoperoxides presented in this article demonstrate antiprotozoal activity and can be divided into three groups. The third group includes endoperoxides, which show weak antiprotozoal activity with a reliability of up to 70%, and this group includes only 1.1% of metabolites. The second group includes the largest number of endoperoxides, Citation: Dembitsky, V.M.; which are 65% and show average antiprotozoal activity with a confidence level of 70 to 90%. Lastly, Ermolenko, E.; Savidov, N.; the third group includes endoperoxides, which are 33.9% and show strong antiprotozoal activity with Gloriozova, T.A.; Poroikov, V.V.
    [Show full text]
  • Marine Pharmacology in 1999: Compounds with Antibacterial
    Comparative Biochemistry and Physiology Part C 132 (2002) 315–339 Review Marine pharmacology in 1999: compounds with antibacterial, anticoagulant, antifungal, anthelmintic, anti-inflammatory, antiplatelet, antiprotozoal and antiviral activities affecting the cardiovascular, endocrine, immune and nervous systems, and other miscellaneous mechanisms of action Alejandro M.S. Mayera, *, Mark T. Hamannb aDepartment of Pharmacology, Chicago College of Osteopathic Medicine, Midwestern University, 555 31st Street, Downers Grove, IL 60515, USA bSchool of Pharmacy, The University of Mississippi, Faser Hall University, MS 38677, USA Received 28 November 2001; received in revised form 30 May 2002; accepted 31 May 2002 Abstract This review, a sequel to the 1998 review, classifies 63 peer-reviewed articles on the basis of the reported preclinical pharmacological properties of marine chemicals derived from a diverse group of marine animals, algae, fungi and bacteria. In all, 21 marine chemicals demonstrated anthelmintic, antibacterial, anticoagulant, antifungal, antimalarial, antiplatelet, antituberculosis or antiviral activities. An additional 23 compounds had significant effects on the cardiovascular, sympathomimetic or the nervous system, as well as possessed anti-inflammatory, immunosuppressant or fibrinolytic effects. Finally, 22 marine compounds were reported to act on a variety of molecular targets, and thus could potentially contribute to several pharmacological classes. Thus, during 1999 pharmacological research with marine chemicals continued
    [Show full text]
  • Effects of Long-Acting, Broad Spectra Anthelmintic Treatments on The
    www.nature.com/scientificreports OPEN Efects of long‑acting, broad spectra anthelmintic treatments on the rumen microbial community compositions of grazing sheep Christina D. Moon1*, Luis Carvalho1, Michelle R. Kirk1, Alan F. McCulloch2, Sandra Kittelmann3, Wayne Young1, Peter H. Janssen1 & Dave M. Leathwick1 Anthelmintic treatment of adult ewes is widely practiced to remove parasite burdens in the expectation of increased ruminant productivity. However, the broad activity spectra of many anthelmintic compounds raises the possibility of impacts on the rumen microbiota. To investigate this, 300 grazing ewes were allocated to treatment groups that included a 100‑day controlled release capsule (CRC) containing albendazole and abamectin, a long‑acting moxidectin injection (LAI), and a non‑treated control group (CON). Rumen bacterial, archaeal and protozoal communities at day 0 were analysed to identify 36 sheep per treatment with similar starting compositions. Microbiota profles, including those for the rumen fungi, were then generated for the selected sheep at days 0, 35 and 77. The CRC treatment signifcantly impacted the archaeal community, and was associated with increased relative abundances of Methanobrevibacter ruminantium, Methanosphaera sp. ISO3‑F5, and Methanomassiliicoccaceae Group 12 sp. ISO4‑H5 compared to the control group. In contrast, the LAI treatment increased the relative abundances of members of the Veillonellaceae and resulted in minor changes to the bacterial and fungal communities by day 77. Overall, the anthelmintic treatments resulted in few, but highly signifcant, changes to the rumen microbiota composition. Anthelmintic treatment of adult ewes is practiced by about 80% of sheep farmers in New Zealand1, and many of these treatments use active compounds with broad-spectrum persistent activity.
    [Show full text]
  • Identification of Pyrvinium, an Anthelmintic Drug, As a Novel Anti
    molecules Article Identification of Pyrvinium, an Anthelmintic Drug, as a Novel Anti-Adipogenic Compound Based on the Gene Expression Microarray and Connectivity Map Zonggui Wang 1, Zhong Dai 2,3, Zhicong Luo 2,3 and Changqing Zuo 2,3,* 1 Department of Biochemistry and Molecular Biology, Guangdong Medical University, Dongguan 523808, Guangdong, China 2 Guangdong Key Laboratory for Research and Development of Natural Drugs, Zhanjiang 524023, Guangdong, China 3 School of Pharmacy, Guangdong Medical University, Dongguan 523808, Guangdong, China * Correspondence: [email protected]; Tel.: +86-769-22896551 Received: 3 June 2019; Accepted: 27 June 2019; Published: 28 June 2019 Abstract: Obesity is a serious health problem, while the current anti-obesity drugs are not very effective. The Connectivity Map (C-Map), an in-silico drug screening approach based on gene expression profiles, has recently been indicated as a promising strategy for drug repositioning. In this study, we performed mRNA expression profile analysis using microarray technology and identified 435 differentially expressed genes (DEG) during adipogenesis in both C3H10T1/2 and 3T3-L1 cells. Then, DEG signature was uploaded into C-Map, and using pattern-matching methods we discovered that pyrvinium, a classical anthelminthic, is a novel anti-adipogenic differentiation agent. Pyrvinium suppressed adipogenic differentiation in a dose-dependent manner, as evidenced by Oil Red O staining and the mRNA levels of adipogenic markers. Furthermore, we identified that the inhibitory effect of pyrvinium was resulted primarily from the early stage of adipogenesis. Molecular studies showed that pyrvinium downregulated the expression of key transcription factors C/EBPa and PPARγ. The mRNA levels of notch target genes Hes1 and Hey1 were obviously reduced after pyrvinium treatment.
    [Show full text]
  • Parasiticides: Fenbendazole, Ivermectin, Moxidectin Livestock
    Parasiticides: Fenbendazole, Ivermectin, Moxidectin Livestock 1 Identification of Petitioned Substance* 2 3 Chemical Names: 48 Ivermectin: Heart Guard, Sklice, Stomectol, 4 Moxidectin:(1'R,2R,4Z,4'S,5S,6S,8'R,10'E,13'R,14'E 49 Ivomec, Mectizan, Ivexterm, Scabo 6 5 ,16'E,20'R,21'R,24'S)-21',24'-Dihydroxy-4 50 Thiabendazole: Mintezol, Tresaderm, Arbotect 6 (methoxyimino)-5,11',13',22'-tetramethyl-6-[(2E)- 51 Albendazole: Albenza 7 4-methyl-2-penten-2-yl]-3,4,5,6-tetrahydro-2'H- 52 Levamisole: Ergamisol 8 spiro[pyran-2,6'-[3,7,1 9]trioxatetracyclo 53 Morantel tartrate: Rumatel 9 [15.6.1.14,8.020,24] pentacosa[10,14,16,22] tetraen]- 54 Pyrantel: Banminth, Antiminth, Cobantril 10 2'-one; (2aE, 4E,5’R,6R,6’S,8E,11R,13S,- 55 Doramectin: Dectomax 11 15S,17aR,20R,20aR,20bS)-6’-[(E)-1,2-Dimethyl-1- 56 Eprinomectin: Ivomec, Longrange 12 butenyl]-5’,6,6’,7,10,11,14,15,17a,20,20a,20b- 57 Piperazine: Wazine, Pig Wormer 13 dodecahydro-20,20b-dihydroxy-5’6,8,19-tetra- 58 14 methylspiro[11,15-methano-2H,13H,17H- CAS Numbers: 113507-06-5; 15 furo[4,3,2-pq][2,6]benzodioxacylooctadecin-13,2’- Moxidectin: 16 [2H]pyrano]-4’,17(3’H)-dione,4’-(E)-(O- Fenbendazole: 43210-67-9; 70288-86-7 17 methyloxime) Ivermectin: 59 Thiabendazole: 148-79-8 18 Fenbendazole: methyl N-(6-phenylsulfanyl-1H- 60 Albendazole: 54965-21-8 19 benzimidazol-2-yl) carbamate 61 Levamisole: 14769-72-4 20 Ivermectin: 22,23-dihydroavermectin B1a +22,23- 21 dihydroavermectin B1b 62 Morantel tartrate: 26155-31-7 63 Pyrantel: 22204-24-6 22 Thiabendazole: 4-(1H-1,3-benzodiazol-2-yl)-1,3- 23 thiazole
    [Show full text]
  • The Mechanism of Action of Praziquantel: Can New Drugs Exploit Similar Mechanisms?
    The mechanism of action of praziquantel: can new drugs exploit similar mechanisms? Charlotte M. Thomas1,2 and David J Timson1,3* 1 School of Biological Sciences, Queen's University Belfast, Medical Biology Centre, 97 Lisburn Road, Belfast, BT9 7BL, UK. 2 Institute for Global Food Security, Queen’s University Belfast, 18-30 Malone Road, Belfast, BT9 5BN, UK. 3 School of Pharmacy and Biomolecular Sciences, University of Brighton, Huxley Building, Lewes Road, Brighton, BN2 4GJ, UK. *Author to whom correspondence should be addressed at School of Pharmacy and Biomolecular Sciences, University of Brighton, Huxley Building, Lewes Road, Brighton, BN2 4GJ. UK. Telephone +44(0)1273 641623 Fax +44(0)1273 642090 Email [email protected] 1 Abstract Praziquantel (PZQ) is the drug of choice for treating infection with worms from the genus Schistosoma. The drug is effective, cheap and has few side-effects. However, despite its use in millions of patients for over 40 years its molecular mechanism of action remains elusive. Early studies demonstrated that PZQ disrupts calcium ion homeostasis in the worm and the current consensus is that it antagonises voltage-gated calcium channels. It is hypothesised that disruption of these channels results in uncontrolled calcium ion influx leading to uncontrolled muscle contraction and paralysis. However, other experimental studies have suggested a role for myosin regulatory light chains and adenosine uptake in the drug’s mechanism of action. Assuming voltage-gated calcium channels do represent the main molecular target of PZQ, the precise binding site for the drug remains to be identified. Unlike other commonly used anti-parasitic drugs, there are few definitive reports of resistance to PZQ in the literature.
    [Show full text]
  • Marine Pharmacology in 2003–4: Marine
    Comparative Biochemistry and Physiology, Part C 145 (2007) 553–581 www.elsevier.com/locate/cbpc Marine pharmacology in 2003–4: Marine compounds with anthelmintic antibacterial, anticoagulant, antifungal, anti-inflammatory, antimalarial, antiplatelet, antiprotozoal, antituberculosis, and antiviral activities; affecting the cardiovascular, immune and nervous systems, and other miscellaneous mechanisms of action ⁎ Alejandro M.S. Mayer a, , Abimael D. Rodríguez b, Roberto G.S. Berlinck c, Mark T. Hamann d a Department of Pharmacology, Chicago College of Osteopathic Medicine, Midwestern University, 555 31st Street, Downers Grove, Illinois 60515, USA b Department of Chemistry, University of Puerto Rico, San Juan, Puerto Rico 00931, USA c Instituto de Quimica de Sao Carlos, Universidade de Sao Paulo, Sao Carlos, 13560-970, Brazil d School of Pharmacy, The University of Mississippi, Faser Hall, University, Mississippi 38677, USA Received 28 October 2006; received in revised form 29 January 2007; accepted 30 January 2007 Available online 9 February 2007 Abstract The current marine pharmacology review that covers the peer-reviewed literature during 2003 and 2004 is a sequel to the authors' 1998–2002 reviews, and highlights the preclinical pharmacology of 166 marine chemicals derived from a diverse group of marine animals, algae, fungi and bacteria. Anthelmintic, antibacterial, anticoagulant, antifungal, antimalarial, antiplatelet, antiprotozoal, antituberculosis or antiviral activities were reported for 67 marine chemicals. Additionally 45 marine compounds were shown to have significant effects on the cardiovascular, immune and nervous system as well as possessing anti-inflammatory effects. Finally, 54 marine compounds were reported to act on a variety of molecular targets and thus may potentially contribute to several pharmacological classes.
    [Show full text]
  • Mcintyre, Jennifer Ruth (2020) Genetic Markers of Anthelmintic Resistance in Gastrointestinal Parasites of Ruminants
    McIntyre, Jennifer Ruth (2020) Genetic markers of anthelmintic resistance in gastrointestinal parasites of ruminants. PhD thesis. https://theses.gla.ac.uk/79021/ Copyright and moral rights for this work are retained by the author A copy can be downloaded for personal non-commercial research or study, without prior permission or charge This work cannot be reproduced or quoted extensively from without first obtaining permission in writing from the author The content must not be changed in any way or sold commercially in any format or medium without the formal permission of the author When referring to this work, full bibliographic details including the author, title, awarding institution and date of the thesis must be given Enlighten: Theses https://theses.gla.ac.uk/ [email protected] Genetic Markers of Anthelmintic Resistance in Gastrointestinal Parasites of Ruminants Jennifer Ruth McIntyre BVM&S BVetSci(Hons) MRCVS Submitted in fulfilment of the requirements for the degree of Doctor of Philosophy Institute of Biodiversity, Animal Health and Comparative Medicine College of Medical, Veterinary and Life Sciences February 2020 © Jennifer Ruth McIntyre, 2020 2 Abstract Parasitic gastroenteritis is the primary production limiting disease of sheep in the UK and is a considerable welfare concern. A global problem, it is caused by nematode parasites and mixed species infections can be common. In the UK, the primary pathogen in growing lambs is Teladorsagia circumcincta, an abomasal parasite of small ruminants, causing severe pathology and reduced weight gain. T. circumcincta is expertly adapted to both the host and the farming year and control is extremely difficult. The majority of UK farmers will use anthelmintics to manage parasitic gastroenteritis.
    [Show full text]
  • Stromectol® (Ivermectin)
    TABLETS STROMECTOL® (IVERMECTIN) DESCRIPTION STROMECTOL* (Ivermectin) is a semisynthetic, anthelmintic agent for oral administration. Ivermectin is derived from the avermectins, a class of highly active broad-spectrum, anti-parasitic agents isolated from the fermentation products of Streptomyces avermitilis. Ivermectin is a mixture containing at least 90% 5-O­ demethyl-22,23-dihydroavermectin A1a and less than 10% 5-O-demethyl-25-de(1-methylpropyl)-22,23-dihydro­ 25-(1-methylethyl)avermectin A1a, generally referred to as 22,23-dihydroavermectin B1a and B1b, or H2B1a and H2B1b, respectively. The respective empirical formulas are C48H74O14 and C47H72O14, with molecular weights of 875.10 and 861.07, respectively. The structural formulas are: Component B1a, R = C2H5 Component B1b, R = CH3 Ivermectin is a white to yellowish-white, nonhygroscopic, crystalline powder with a melting point of about 155°C. It is insoluble in water but is freely soluble in methanol and soluble in 95% ethanol. STROMECTOL is available in 3-mg tablets containing the following inactive ingredients: microcrystalline cellulose, pregelatinized starch, magnesium stearate, butylated hydroxyanisole, and citric acid powder (anhydrous). CLINICAL PHARMACOLOGY Pharmacokinetics Following oral administration of ivermectin, plasma concentrations are approximately proportional to the dose. In two studies, after single 12-mg doses of STROMECTOL in fasting healthy volunteers (representing a mean dose of 165 mcg/kg), the mean peak plasma concentrations of the major component (H2B1a) were 46.6 (±21.9) (range: 16.4-101.1) and 30.6 (±15.6) (range: 13.9-68.4) ng/mL, respectively, at approximately 4 hours after dosing. Ivermectin is metabolized in the liver, and ivermectin and/or its metabolites are excreted almost exclusively in the feces over an estimated 12 days, with less than 1% of the administered dose excreted in the urine.
    [Show full text]