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Parasites: Using Prescription Drugs Against Parasites
Forum Description
Last Message  33min

Support forum for people interested in Drugs therapy, Prescription Medications therapy against parasites.


Some examples of drug therapy include:

Mebendazole (Vermox) -- roundworm, hookworm, pinworm
Thiabendazole (Mintezol) -- threadworm, pork worm
Metronidazole (Flagyl) -- giardiasis
Nitazoxanide (Alinia) -- giardiasis, cryptosporidiosis
Triclabendazole (Fasinex)


Drugs against Parasites: Vermox, Praziquantel, Biltricide, Artemisinin, Benzimidazole, Mebendazole, Triclabendazole, Thiabendazole, Albendazole, Fenbendazole, Malarone, Lariam, Atovaquone-Proguanil, Mefloquine, Chloroquine, Sulfadoxine-pyrimethamine, Quinine, Proguanil, Primaquine, Mefloquine, Halofantrine, Fansidar, Doxycycline, Atovaquone, Niclosamide


For all talk related to Pharmaceuticals used against Parasites, parasitic animals in humans, worms, tapeworms, ascaris, pin worms, whipworms, Protozoa, Helmints, Insects (Scabies lice etc.)


Triclabendazole (commercial name Fasinex) is a member of the Benzimidazole family of anthelmintics. The benzimidazole drugs share a common molecular structure, triclabendazole being the exception in having a chlorinated benzene ring but no carbamate group.

Triclabendazole displays high efficacy against both immature and adult liver fluke.

It is generally accepted that benzimidazoles like triclabendazole bind to beta-tubulin and prevent the polymerisation of the microtubules of which they are part.



Albenza

The medication Albenza (albendazole) belongs to a class of drugs called anthelmintics. Other names are Valbazen, Zybend and Albact.

Albenza is a broad-spectrum anthelmintic. Albenzais used to treat neurocysticercosis (caused by pork tapeworm) and in Taenia solium infection. Albenza can also be used to treat cystic hydatid disease (liver, lung, and peritoneum) brought by dog tapeworm.

Take 400mg tabs twice daily.

Albenza can cause rash and urticaria, hepatitis, Erythema multiforme, Stevens-Johnson syndrome, pancytopenia and agranulocytosis.

It has also been found to cause Kidney failure in rare cases.

Generic Albenza (Albendazole) 400mg is available in packs of 30, 60, 90, 120 and 240 pills.





Chemotherapeutic Agents, Antibiotics
Antibacterial compounds (procaryotes)
Antiparasitic agents (eucarytotes)
Antifungal compounds (eucarytotes)
Antiviral compounds
Anticancer compounds


Protozoa
Helmints
Insects (Scabies lice etc.)


Protozoa

Eucaryotes, unicellular (may exist in colonies)
Protozoa and algae (protocista)


Common Treatments of diseases caused by
amebia, giardia, trichomonas

Metronidazol
Flagyl®
Metronidazol®

The drug may also be effective against anaerobic bacteria.




List of Drugs used against Malaria
Anti - Malaria drugs (Plasmodium sp. Vektor: Anopheles moskito.)

Mal aria = bad air

Malaria kills a child every 30 sec.
90% in incidents sub-sahara Africa

Historic drugs
- Azodyes and salvarsan (1st synthetic effective drug)
- Quinine fra Cinchona (Kinabark)

Cinchona pubescens (Kinatre) from South America



List of Drugs used against Malaria
Quinolines (Anti - Malaria drugs)

Quinine
Kinin®
Meflokin
Lariam®
Klorokin
Klorokinfosfat®
Hydroksyklorokin
Plaquenil®



More active, less tox (comp Quinine)
Klorokin
P. palsifarum

Ferriprotoporphyrin IX: Binds to FPIX (metabolite from hemoglobine);



List of Drugs used against Malaria
Biguanides (Anti - Malaria drugs)


Proguanil (= Chloroguanide)
Paludrine®
Malarone® + Atovakvon
Pro-drug
Inhib. protozoan folate reduktase

Trimetoprim

Other biguanides
Klorhexidine



Atovakvon
Malarone® + proguanil.
Also other parasites (P. carinii)

Artemeter og Lumefandrin

Riamet®







List of Drugs used against Helmint infections (Round worms)

Eukaryotes – Invertebrates.

Animal parasites; ex Trichinella spiralis (trikiner).


Mebendazol
Vermox®
Benzimidazoles
Benzimidazole
Thiabendazole
Albendazole
Fenbendazole







List of Drugs used against Ectoparasites (insects) Lice, scabies etc

Permetrin
Nix®





Irreversible Inhibitors

Acetylcholine esterase
Not drugs, nerve gasses, insecticides etc.


Malation
Prioderm® lice




Fungicides / Fungistatika / Antimykotika

Chemotherapeutics / Antibiotics



Synthetic Antifungals
Azoles

Klotrimazol:

Canesten®, Klotrimazol® utvortes
Canesten®, vaginal behandlig


Ekonazol:

Pevaryl®, utvortes
Pevaryl®, vaginal behandlig


Miconazol:

Daktar®, utvortes
Daktar®, vaginal behandlig


Ketokonazol:
Itrakonazol:
Flukonazol
(Racemate)




Vorikonazol
SAR:





Allylic amines

Terbinafin
Lamicil®

Prevents formation of cell wall comp.
Accumulation of toxic squalene






Antimycotic Antibiotics
Polyenes
Proad spectrum. Some effect on certain protozoa.

Isolated, Streptomyces sp.

Binds to sterols in fungal cell membrane; cell leaks K+, small org. molecules

SAR:

Macrolaktone [26 eor 38-ring, Larger than macrolides ( erytromycin etc)]
Polyene (Macrolides not polyenes)
Several OH-groups
amino sugar, mykosamin
Bad water sol.






Nystatin A

toxic, bad oral avail;

Local treatment, mouth, GI tract


Amfotericin B

Systhemic infect (infusion)

Somewhat less tox.







Peptides


Caspofungin

Serious systhemic infect.

Semisynth. from prod. of fermentation ( Glarea lozoyensis)

Inhib. synth of b-1,3-D-glucan; cell wall comp. certain fungi


Few good inhib. of fungi cell wall comp.

compared to antibacterials






First effective drug: Streptomycin 1946


Treatment

Long time ≥6 mnds
Combination of drugs


Different stages of bacterial growth


DOT: Directly observed therapy







First-line drugs


Isoniazid

Isoniazid®


Mycolic acid


Long Chain ACP-Enoyl

Fatty Acid Reductase (inhA)







First-line drugs


Rifampicin

Rimactan®


Broad spectrum antibiotic

From Streptomyces sp

Inhib bacterial RNA polymerase

(p-p intract. naphtalene rings aromatic AA?)

Induce CYP2C; increased metabol. of certain anti AIDS drugs


Pyrazinamide


Mechanism not known


Ethambutol


Mechanism not fully known

Synth of cell wall comp.:

Inhib. arabinocyl transferase?

Arabinose,

Arabinomannan

and Lipoarabinomannan








Second-line drugs


Ethionamide


p-Aminosalicylic acid


Cycloserine

Isolated Spreptomyces sp


Mech. ≈ Isoniazide


PABA antimetabolite

Folic acid synth (≈antibact. sulfa)


Inhib. alanine racemase

and alanine ligase;

Inhib. peptidoglycan synth


Kanamycin

(aminoglycoside antibiotics)







Others


Quinolones


Oxazolidinones


Treatment of MAC infections


Clarithromycin

(Macrolide)



Other macrolides

Ethambutol

Quinolones

Rifabutin (Rifamycin)


ANTIMICROBIALS FOR EUKARYAL ORGANISMS



  • Anti-protozoal
    : they can interfere with ...

    • oxidative status, by producing R.O.S.



      • artemisinin / qinghaosu
        (a
        molecule with a pharmacophoric peroxide bond in a unique 1,2,4-trioxane
        heterocycle) : is a compound based on qinghaosu, or sweet wormwood. 1st
        isolated in 1965 by Chinese military researchers while seeking a new
        antimalarial treatment for Vietnamese troops fighting American forces, it
        cut the death rate by 97% in a malaria epidemic in Viet Nam in the early
        1990's. It is rapidly replacing quinine derivatives and later drugs
        against which the disease has evolved into resistant strains. To protect
        artemisinin from the same fate, it will be given as part of multidrug
        cocktails. Unicef, the United Nations Children's Fund, which procures
        drugs for the world's poorest countries, opposed its use during an
        Ethiopian epidemic in 2003, saying that there was too little supply and
        that switching drugs in mid-outbreak would cause confusion. Until
        recently, big donors like the United States and Britain had opposed  its
        use on a wide scale, saying it was too expensive, had not been tested
        enough on children and was not needed in areas where other malaria drugs
        still worked. In 2004 the new Global Fund for AIDS, Tuberculosis and
        Malaria has given 11 countries grants to buy artemisinin and has
        instructed 34 others to drop requests for 2 older drugs -- chloroquine and
        sulfadoxine-pyrimethamine -- and switch to the new one. The price of
        artemisinin cocktails has fallen from $2 per treatment to < 90 cents as
        more companies in China, India and Viet Nam have begun making them (older
        drugs cost only 20 cents)

        Pharmacodynamics : intraparasitic heme of
        infected erythrocytes irreversible catalyzes cleavage of the endoperoxide
        bridge. This is followed by intramolecular rearrangement to produce
        carbon-centered radicals that covalently modify (alkylation) and damage
        haem and proteins. Further artemisins interfere with the function of the
        sarcoplasmic-endoplasmic reticulum ATPase PfATP6 that generates
        energy in the malaria parasite.

        Semi-synthetic derivatives :

        • dihydroartemisin (DHA)

          • dihydroartemisinin with napthoquine and trimethoprim (DNP)



        • b-artemether (Artenam®;
          co-artemether / CGP 56697 / A-L in combination with
          lumefantrine (Coartem® (sold by
          Novartis to poor countries for 10 cents less than it costs to make),
          Riamet® (sold to European travelers for about $20))

        • artether

        • artesunate (Arenax®, Arsumax®, Falcigo®,
          Plasmotrim®)


        In some parts of Southeast Asia they are the only effective treatment
        for acute malaria. Notably, there is no evidence of drug resistance to any
        member of the artemisinin family of drugs. As a drug class, the
        artemisinins suffer from chemical (semi-synthetic availability, purity and
        cost), biopharmaceutical (poor bioavailability and limiting
        pharmacokinetics : they remain in the bloodstream for only a short time so
        have to be taken frequently) and treatment (non-compliance with long
        treatment regimens and recrudescence) issues that limit their therapeutic
        potential


        • although total synthesis of artemisinin is difficult and costly, the
          semi-synthesis of artemisinin or any derivative from microbially
          sourced artemisinic acid
          , its immediate precursor, could be a
          cost-effective, environmentally friendly, high-quality and reliable
          source of artemisinin. Saccharomyces cerevisiae has been
          engineered to produce high titres (up to 100 mg/l) of artemisinic acid
          using an engineered mevalonate pathway, amorphadiene synthase, and a
          novel cytochrome P450 monooxygenase (CYP71AV1) from A. annua that
          performs a 3-step oxidation of amorpha-4,11-diene to artemisinic acid.
          The synthesized artemisinic acid is transported out and retained on the
          outside of the engineered yeast, meaning that a simple and inexpensive
          purification process can be used to obtain the desired product. Although
          the engineered yeast is already capable of producing artemisinic acid at
          a significantly higher specific productivity than A. annua, yield
          optimization and industrial scale-up will be required to raise
          artemisinic acid production to a level high enough to reduce artemisinin
          combination therapies to significantly below their current pricesref.

        • RBx-11160, is a synthetic, slightly altered version of
          artemisinin. It only needs to be taken for around 3 days, and its simple
          structure means it should be at least 5 times cheaper to produce. Better
          solubility means the drug can be given orally or injected intravenously.
          Added stability means that less of the compound is broken down as it
          travels to the blood plasma, where the parasite lives. The new version
          is also more potent. When infected mice are given the drug, 95-100% of
          parasites disappear within four days. Conventional artemisinin drugs
          take a week to clear 95% of parasites. The drug entered preliminary
          human safety trials in Britain in July 2004. If the drug works well in
          people, it would probably be given in combination with a second drug,
          which would kill any parasites missed by RBx-11160ref.



      • nitrofurans

        • nifurtimox /
          3-methyl-4(5'-nitrofurfurylideneamino)-tetrahydro-4H-1,4-thiazine-1,1-dioxide
          / Bayer 2502
          (Lampit®)





    • mitochondrial electron transport

      • hydroxynaphtoquinones

        • atovaquone (Mepron®) : usually administered in
          combination with proguanil (ATQ/PG)
          (Malarone®)





    • heme polymerization to hemozoin

      • 4-aminoquinolines


        • quinine and its optical isomer quinidine
          .

        • chloroquine (Aralen® in combination with
          primaquine; once called Resochin®)
          phosphate, diphosphate or sulfate.

        • hydroxychloroquine (Plaquenil®)

        • amodiaquine (Basoquin®, CAM-AQ1®,
          Camoquin®, Camoquinal®, Flavoquin®,
          Fluroquine®, Miaquin®, SN-10,751®;
          Camoprima Infatabs® in combination with
          primaquine
          )

        • pyronaridine, a hydroxyanilino-benzonaphthyridine synthesized
          in China in 1970, which has been used for the treatment of P. vivax
          and P. falciparum for more than 20 years and has been shown
          to be effective in the treatment of falciparum malaria in children in
          Cameroon. It has more gastrointestinal side effects than chloroquine.
          There are insufficient data at present to recommend the use of
          pyronaridine for the treatment of malaria in non-immune travellers.



      • bisquinoline

        • piperaquine phosphate is an orally active bisquinoline
          discovered in the early 1960s and developed for clinical use in China in
          1973. In vitro testing in several laboratories has shown that
          piperaquine approximates chloroquine’s effects against sensitive
          parasites and is significantly more effective than chloroquine in
          treating resistant P. falciparum. In China, Vietnam and Cambodia,
          piperaquine is now available as a fixed combination with

          Prospective clinical trial data are pending.




      • 8-aminoquinolines

        • primaquine phosphate (Primaquine®; Aralen®
          in combination with chloroquine)

        • compound 80/53 / bulaquin (Aablaquine® in
          combination with chloroquine)

        • tafenoquine / WR 238605 (Etaquine®) (long-acting :
          half-life measured in weeks rather than hours)

        • sitamaquine / WR6026ref

        • NPC1161Cref



      • 8-hydroxyquinolines

        • iodoquinol / diiodohydroxyquin (Yodoxin®)

        • clioquinol / iodochlorhydroxyquin (nowadays used only as
          Zn
          chelator
          )



      • 4-quinoline-methanols

        • mefloquine chlorhydrate (Falcitab®, Lariam®)
          was isolated at the Walter Reed Army Institute of Research in 1963 for
          American troops in the Vietnamese conflict. In combination with
          pyrimethamine-sulfadoxine
          in Fansimef®

          Side effects : acute psychiatric syndrome
          (=>
          suicide
          )
          and

          post-malaria neurological syndrome (PMNS)
          .
          The Pentagon is studying 21 suicides committed in Iraq and Kuwait during
          Operation Iraqi Freedom (plus 5 more deaths in Iraq as possible
          suicides, and six deaths among soldiers in Iraq who killed themselves
          after returning to the United States). 4 of the 21 soldiers who
          committed suicide in Iraq or Kuwait came from units that took Lariam and
          1 tested positive for Lariam in the blood





    • antimetabolites

      • protozoal dihydropteroate synthetase

        • sulfones

          • dapsone / 4,4'-diaminodiphenylsulfone (Lapdap®
            in combination with chlorproguanil)



        • sulfonamides

          • sulfadiazine

          • sulfadoxine





      • protozoal DHF reductase (at concentrations far lower than those
        required to produce comparable inhibition of the mammalian enzymes) (antifols)
        work poorly against P. vivax

        • 2,4-diaminopyrimidines


        • aryl aminoalcohols

          • halofantrine (Halfan®)

            Side effects : QTc prolongation

          • lumefantrine / benflumetol (a fluorene derivative) (co-artemether
            / CGP 56697 / A-L
            (Coartem®, Riamet®) in
            combination with artemether)



        • proguanil / chloroguanide (Paludrine®)
          chlorhydrate => cycloguanil; usually administered in combination
          with atovaquone (Malarone®)

        • chlorproguanil (Lapudrine®; Lapdap® in
          combination with dapsone)



      • trypanothione reductase

        • melarsoprol / Mel B (Arsobal®) : binding to
          trypanothione (a glutathione analog) results in formation of melarsen
          oxide-trypanothione adduct (Mel T), a compound that is a potent
          competitive inhibitor of trypanothione reductase, thus affecting
          defenses against oxidative stress.



      • ornithine decarboxylase (ODC)

        • eflornithine / a-difluoromethylornithine
          (DFMO
          ) hydrochloride (Ornidyl®, Vaniga®) :
          also used to treat unwanted facial hair (UFH) in females.





    • suramin sodium (Germanin® / Bayer 205®) is
      a polysulfonated derivative of urea and has been widely used both to treat
      trypanosome infections and as a chemotherapeutic drug. Suramin has been
      shown to inhibit growth factor signaling pathways and inhibits death
      receptor-induced apoptosis in hepatoma and lymphoma cells in vitro
      and fulminant apoptotic liver damage in mice. It also inhibits the
      proapoptotic effect of chemotherapeutic drugsref



    • farnesyl diphosphate synthase (FPPS) inhibitors

      from

      Trypanosoma brucei
      ref

    • diamidines

      • pentamidine isethionate or methylate (Pentacarinate®,
        Pentam® or NebuPent®)

      • stilbamidine

      • dibromo propamidine isethiaote (Brolene®)

      • diminazine (Berenil®)



    • cell membrane stability

      • polyene macrolides



        • amphotericin B

          (AmB) deoxycholate (DAMB)
          (Amphocil®,
          Amphocin®, Fungilin®, Fungizone®,
          Intralipid®) : p
          arenteral administration of
          amphotericin B (AMB), a polyene antibiotic with strong antifungal
          activity, remains the therapy of choice for systemic mycoses. It is
          highly hydrophobic and is commonly administrated as desoxycholate
          amphotericin (DAMB), a detergent micelle complex. AMB binds
          preferentially to ergosterol in fungal plasma membranes, although it
          also interacts with animal cell sterols such as cholesterol, which
          accounts for known toxicityref1,

          ref2
          . DAMB therapy is associated
          with nephrotoxicity, central nervous system and liver damage, and side
          effects such as nausea and feverref1,

          ref2
          ,

          ref3
          . AMB, with its inherent low solubility in water and many
          organic solvents, shows relatively poor bioavailabilityref1,

          ref2
          . In order to increase the therapeutic index of AMB and
          reduce its associated toxicity, new lipid-based formulations have been
          developedref1,

          ref2
          ,

          ref3
          . These drug delivery systems, such as liposomal
          formulations, lipid complexes, lipid emulsions, and colloidal
          dispersions, have been introduced into clinical practice. But their use
          remains limited by cost, stability, and toxicityref1,

          ref2
          ,

          ref3
          ,

          ref4
          ,

          ref5
          ,

          ref6
          . Despite the improvement in therapeutic index for
          liposomal AMB formulations, the overall prognosis for patients with
          severe candidemia remains poor due to the inadequacy of treatments. The
          development of new, effective antifungal delivery systems for acute and
          prophylactic application remains an important objective. AMB is not
          significantly absorbed across the gastrointestinal tract in either
          detergent-solubilized form or in liposomal preparationsref.





          • amphotericin B lipid complex (ABLC) (Abelcet®)

          • amphotericin B colloidal dispersion (ABCD)
            (Amphotec®)

          • liposomal amphotericin B (LAMB) (AmBisome®,
            Fujisawa Healthcare, Inc.)

          • cochleates containing amphotericin B (CAMB)are
            a novel lipid-based delivery vehicle that have an advantage over
            existing formulations due to the stability of cochleates and their
            resistance to degradation in the gastrointestinal tract. Thus,
            cochleate preparations have the potential to delivery AMB orally.
            Cochleates are stable phospholipid-calcium precipitates comprised
            mainly of phosphatidylserine. They have a defined multilayered
            structure consisting of a continuous, solid, lipid bilayer sheet
            rolled up in a spiral, with no internal aqueous space. Papahadjopoulos
            et al. first described cochleates in 1975 as an intermediate in the
            preparation of large unilamellar vesiclesref.
            Cochleates have been used to deliver protein, peptide, and DNA for
            vaccine and gene therapy applications and have been used recently as a
            drug delivery systemref.
            CAMB have been shown to be highly protective in a mouse candidiasis
            model following parenteral administration. Because of the hydrophobic
            nature of AMB molecules, it was hypothesized that AMB would be
            localized in the unique, rigid lipid bilayers of the cochleates. This
            unique association should provide protection for AMB from degradation
            when exposed to harsh environmental conditions or enzymes. CAMB should
            be an ideal system to deliver amphotericin B orally. Initial
            biodistribution studies of CAMB administered orally in a mouse model
            showed that cochleates delivered therapeutic levels of AMB to target
            organsref








    • protein synthesis



      • tetracyclines
        ,

        azithromycin

        and

        clindamycin

        also have antiplasmodial activity, although in general their action is
        slow for malaria treatment (as opposed to prophylaxis); they are
        recommended only in combination with other antimalarial drugs



    • acridine derivatives

      • quinacrine hydrochloride



    • antimonial compounds

      • antimony (Sb)

      • stibine (SbH3)

      • lead sibocaptate

      • antimony trioxide (Sb2O3)

      • potassium antimony tartrate / antimony potassium tartrate (tartar
        emetic)

      • sodium antimony tartrate

      • sodium stibogluconate / sodium antimony gluconate (Pentostam®)
        (i.v.)

      • sodium antimony bis(pyrocatechol)-2,4-disulfate (C12H12Na5O23S4Sb)

      • meglumine antimonate (Glucantime®)





    • diloxanide furoate (Amoebyl®, Furamide®)



    • paromomycin

      sulfate
      (Humatin®) (nonabsorbed aminoglycoside)

    • fosmidomycin inhibits DOXP reductoisomerase (part of the 1-deoxy-D-xylulose
      5-

      phosphate / 2-C-methyl-D-erythritol 4-phosphate
      pathway (DOXP/MEP pathway) for non-mevalonate isoprenoid biosynthesis) in

      Mycobacterium tuberculosis

      and

      Plasmodium falciparum
      .


    • emetine


    • dehydroemetine (Mebadin®)

    • furazolidone (Furoxone®)

    • polyhexamethylene biguanide

    • nitroimidazoles

      • azomycin / 2-nitro-imidazole

      • benznidazole (Rochagan®)

      • metronidazole (1-(b-hydroxyethyl)-2-methyl-5-nitroimidazole)
        (Deflamon®, Flagyl®, Metrocream®,
        Metronidazolo®, Metrogel®, Noritate®,
        Protostat®, Vagilen®; Meclon 100® in
        combination with clotrimazole)

      • nimorazole (Naxogin®)

      • ornidazole (Tiberal®)

      • tinidazole (Fasigyn®)

      • secnidazole (Seczol-DS®)



    • Ru, Rh, and Pt complexes with azoles and Cu2+
      and Au+ clotrimazole and
      ketoconazole complexes are currently in
      development for therapy of

      Trypanosoma cruzi




    • Cola acuminata

      proanthocyanidins: a class of anti-trypanosomal compounds effective against


      Trypanosoma brucei
      ref



  • Anti-fungalref1,

    ref2
    : they can interfere with ...

      ... cell wall



      • pneumocandins / echinocandins inhibit cell wall glucan
        synthesis

        • anidulafungin / LY303366

        • caspofungin acetate (Cancidase®, MK-0991®)
          is a semisynthetic lipopeptide derivative of pneumocandin B0
          that inhibits (1,3)b-glucan synthase,
          preventing formation of b(1,3)-D-glucans
          in the fungal cell wall

        • micafungin / FK463




      ... cell membrane stability



      • polyene macrolides : bind to ergosterol (affinity is greater
        than for cholesterol) and create pores or channels.

        • tetraenes



          • nystatin

            (Mycostatin®, Nilstat®) active against
            Candida


            • liposomal nystatin (Nyotran®,
              Aronex Ltd., EE.UU.)





        • pentaenes

          • pentamycin



        • hexaenes

          • endomycin



        • heptaenes


        • candicidin



        • partricin


        • methylpartricin / mepartricin : a methyl ester of partricin,
          used chiefly in the treatment of vaginal and cutaneous candidiasis,
          applied topically.



      • azoles inhibit sterol 14-a-demethylase,
        a microsomal cytochrome P450-dependent enzyme system necessary for
        synthesis of ergosterol from lanosterol. Accumulation of 14-a-methylsterols
        lead to disruption of close packing of acyl chains of phospholipids,
        impairing the functions of membrane-bound enzymes.

        • imidazoles

          • bifonazole (Azolmen®, Bifazol®,
            Micospor®)

          • butoconazole nitrate (Femstat 3®)

          • clotrimazole (Antimicotico Same®, Canesten®,
            Lotremin®, Lotrimin®, Mycelex®,
            Gynelotrimin®, Gyno-canesten®, Mycelex-G®;
            Meclon®, Meclon 100® in combination with
            metronidazole)

          • econazole (Ganazolo®, Ifenec-Derm®,
            Ifenec-Ginec.®, Micos®, Pevaryl®,
            Pevaryl Gel®; Pevisone® in combination with
            triamcinolone)

            • econazole nitrate (Chemionazolo®, Chemionazolo
              Topic®, Dermazol®, Ecodergin®,
              Ecostatin®, Eco Mi®, Econazolo Gnr®,
              Econazolo Merck Generics®, Econazolo Pliva®,
              Ecorex®, Ecosteril®, Ganazolo®,
              Gyno-Pevaryl®, Ifenec Derm®, Ifenec Ginec.®,
              Micos®, Pevaril®, Pevaryl Lipogel®,
              Polinazolo®, Spectazole®)



          • enilconazole / imazalil (IMZ) (Clinafarm®,
            Imaverol®, Imazalil®)

          • fenticonazole (Falvin®, Fenzol®,
            Lomexin®)

          • isoconazole nitrate (Icaden®, Isogyn®,
            Travogen® cream, Gyno-Travogen®cream; Travocort®
            in combination with

            diflucortolone valerate
            )

          • ketoconazole (Nizoral®, Nizoral®
            Scalp Fluid, Nizoral® Shampoo, Extina®,
            silvadeneTriatop®). It also inhibits
            CYP11A1,
            CYP11B2,
            CYP17A1,
            and
            CYP51A1


          • miconazole (Pivanazolo®)

            • miconazole nitrate (Conofite®, Daktarin®,
              Daktarin Gel Orale®, Femeron®, Gyno-Daktarin®,
              Micatin®, Miconal®, Micotef 0.2% soluzione
              vaginale, Micotef 2% crema cutanea®, Micotef 2% gel orale®
              Micreme®, Miderm®, Monistat-Derm®,
              Nizacol®, Surolan®)



          • oxiconazole nitrate (Oxistat®)

          • sertaconazole (Ertaczo®, Sertacream®,
            Sertaderm®, Sertadie®, Sertagyn®)

          • sulconazole nitrate (Exelderm®)

          • tioconazole (Gyno-Trosyd®, Trosyd®,
            Trosyd Soluzione Unguele®Vagistat 1®)



        • triazoles

          • 'first-generation' triazoles

            • fluconazole (Diflucan®, Diflucan Gel®,
              Elazor®)

            • itraconazole (Sporanox®, Sporonox®,
              Triasporin®) : dilute in water, make oral cavity washings
              and then swallow

            • terconazole (Terazol®)



          • 'second-generation' triazoles

            • posaconazole / SCH 56592 (Noxafil®)

            • ravuconazole

            • voriconazole / UK-109,496 (Vfend®)







      • allylamines and other nonazole ergosterol biosynthesis inhibitors
        : fungal squalene epoxidase inhibitors

        • amorolfine (Loceryl®)

        • butenafine hydrochloride (Mentax®)

        • naftifine hydrochloride (Exoderil®, Naftin®,
          Suadian®) inhibits squalene-2,3-epoxidase and so fungal
          biosynthesis of ergosterol

        • terbinafine (Lamisil®)



      • praziquantel (Azinox®, Biltricide®, Cesol®,
        Distocide®, Pikiton®) : a pyrazinoisoquinoline that
        alters membrane permeability

      • myriocin / thermozymocidin / ISP-I from from Myriococcum
        albomyces
        is a serine palmitoyltransferase inhibitor. Inhibition of
        ceramide synthesis leads to a rapid and specific reduction in the rate of
        transport of glycosylphosphatidylinositol (GPI)-anchored proteins to the
        Golgi apparatus without affecting transport of soluble or transmembrane
        proteins. Inhibition of ceramide biosynthesis also quickly blocks
        remodelling of GPI anchors to their ceramide-containing



      • flavovirin



      ... DNA and RNA synthesis



      • flucytosine or 5-fluorocytosine (Ancobon®) :
        it crosses blood-brain barrier ==deamination (not in mammalian cells
        !!)==> 5-fluorouracil ==UMP pyrophosphorylase==> 5-fluorouridylic acid

          ==> 5-fluoroUTP ==> incorporated into RNA

          ==> 5-fluorodeoxyuridylic acid, an inhibitor of thymidylate synthase




      • metronidazole


      ... protein synthesis





      • fusidic acid

        inhibits eEF2

      • puromicin

      • polyoxorim

      • sparsomicin

      • cycloheximide (CHX)

      • blasticidin-S

      • anisomicin



      • Corynebacterium diphtheriae

        toxin

      • protease 2A in Enterovirus and Rhinovirus

      • protease L in Aphtovirus

      • protease E in Picornaviridae


      ... cytoskeleton





      • griseofulvin

        (Fulcin®, Fulvicin P/G®, Grisactin®,
        Grifulvin V®, Grisovin®, Likuden®)
        inhibits microtubule formation in mitotic spindle by binding to tubulin
        and MAPs. It may acts as a photosensitizer.

      • mebendazole disrupts microtubules


      ...O-glycosylations



      • tunicamicin inhibits the reaction between dolichol-P and
        UDP-GlcNAc, preventing all O-glycosylations.


      ... unknown



      • hydroxypyridone

        • ciclopiroxolamine (ciclopirox olamine) (systemic : Loprox®;
          topical : Dafnegin®, Penloc®; Batrafen) has a high
          affinity for trivalent metal cations. Ciclopirox olamine can be used to
          synchronize mammalian cells, but its mechanism of action is not
          understood well. The targets of ciclopirox olamine in S. cerevisiae
          appear to include multiple proteins that participate in various
          components of cellular metabolism, including DNA replication, DNA
          repair, and cellular transport. Three genes were cloned: a Fe/Cu
          reductase (FRE1/COS107), an oxidative stress response gene
          (YAP1/COS110), and a gene involved in signal transduction
          (YBR203W/COS111)ref.



      • thiocarbamates

        • tolciclate (Tolmicen®)

        • tolnaftate (Aftate®, Tinactin®,
          Tinaderm®, ...)



      • haloprogin (Halotex®)

      • undecylenic acid (Caldesene®, Cruex®,
        Desenex®, Dr Scholl's®, Egomycol®, Mycota®)

        • zinc undecenoate (Tineafax®)



      • benzoic acid (6%) and salicylic acid (3%) (Whitfield's ointment)

      • propionic acid and caprylic acid

      • natamycin (Natacyn®)

      • K+I-

      • miltefosine / hexadecylphosphocholine (Impavido®,
        Miltex®) (p.o.) inhibits CTP:PC cytidylyltransferase


      • diminazene (Berenil®)

      • chlordantoin : an antifungal agent
        effective against various fungi, including Candida albicans; used
        topically in the treatment of fungal infections of the vulvovaginal region
        and of the skin

      • lufenuron, a chitin synthetase inhibitor

      • Whitfield's ointment : benzoic acid 6%,
        salicylic acid 3%

      • Castellani's paint : carbol-fuchsin
        topical solution




  • Anti-helminticor
    dewormers
    (including helminthicides / helminthagogues and
    nematicides
    )


    • praziquantel (Biltricide® or Distocide®) a
      pyrazinoisoquinoline that increases membrane permeability of calcium and has
      a selective effect on the tegument of trematodes

    • clorsulon is a selective antagonist of fluke phosphoglycerate
      kinase and mutase

    • b-tubulin inhibitors => inhibit microtubule
      formation

      • benzimidazoles

        • albendazole (Albenza®,
          Valbazen
          ®)

        • fenbendazole (Panacur®,
          Safeguard®)

        • mebendazole (Telmin®,
          Vermox®)

        • oxfendazole (Benzelmin®)

        • thiabendazole (Mintezol®,
          Ominzole
          ®, Thiabendazole®)
          (E233)


        • triclabendazole (Fascinex®)
          is a fasciolicide



      • pro-benzimidazoles / prebenzimidazoles

        • febantel (Rintel®)







    • GABA-R

      agonist on nematode muscles => causes flaccid paralysis.

      • piperazine citrate (Multifuge®)

      • piperazine derivatives

          diethylcarbamazine (DEC) citrate (Filaribits®,
          Hetrazan®) blocks host, and possibly parasite, enzymes
          involved in arachidonic acid metabolism, and enhances the innate,
          nonspecific immune system.






    • paralysis of pharyngeal pumping

      • HC110R blockers

        • cyclooctadepsipeptides

          • PF1022A, the first anthelmintically active member, is a
            natural compound from the fungus Mycelia sterilia that belongs
            to the microflora of the leaves of the Camellia japonica.
            PF1022A contains 4 N-methyl-L-leucines,
            2 D-lactic acids and 2-D-phenyllactic
            acids arranged as a cyclic octadepsipeptide with an alternating
            L-D-L-configuration

          • emodepside is a semisynthetic derivative of PF1022A with a
            morpholine ring at each of the 2 D-phenyllactic
            acids in para position





      • glutamate-gated chloride (GluCl) channels activators =>

        • 16-membered macrocyclic lactons



          • avermectins


            • avermectin B1a / abamectin

            • 22,23-dihydroavermectin B1a
              / ivermectin
              (Eqvalan®,
              Furexel
              ®, Ivomec®,
              Mectizan® or Stromectol®) is an agonist of
              GABAA receptors found in the muscle and nerve cells of
              invertebrates and doesn't cross the BBB.





        • abamectin (Endecto®)

        • milbemycins

          • moxidectin (Cydectin®,
            Equest Oral Gel®, ProHeart®,
            ProHeart 6®, Quest®)

          • milbemycin oxime (Interceptor®, Sentinel®)



        • doramectin (Dectomax®)







    • AChE

      inhibitors :


      • metrifonate / trichlorfon (Bilarcil®)
        => dichlorvos / 2,2-dichlorovinyl dimethyl phosphate (DDVP)


      • haloxon (Loxon®)




    • N AChR
      agonists => spastic paralysis


      • imidazothiazoles

        • levamisole (LMS) /
          (--)-2,3,5,6-tetrahydro-6-phenylimidazo[2,1-b]thiazole

          (Decaris®, Levasol®, Tramisole®,
          Ripercol®, Ergamisol®) is also an

          immunomodulator


        • tetramisole / 2,3,5,6-tetrahydro-6-phenyl-imidazole[2,1-b]thiazole



      • tetrahydropyrimidines

        • morantel tartrate (Rumatel®,
          Rumital®)

        • pyrantel pamoate (Antiminth®,
          Combantrin®)





    • proton ionophores

      • salicylanilides

        • rafoxanide

        • oxyclozanide

        • brotianide

        • closantel



      • substituted phenol

        • nitroxynil





    • niclosamide (Niclocide®)

    • oxamniquine (Vansil®)

    • isometamidium (Samorin®)

    • homidium (Ethidium®,
      Novidium®)

    • ectoparasiticides (pediculocides and
      miticides / acaricides
      )


      • hexachlorophene (HCP)


      • lindane
        / g isomer of benzene hexachloride /
        hexachlorobenzene (HCB) / hexachlorocyclohexane (HCH)

        (Kwell
        ®, Scabene®,
        ...)

      • bithionol (Lorothidol®,
        Bitin
        ®)

      • pyrethroids are used in insecticide treated net (ITN) and in "zampirone"
        spirals (from the inventor's name Zampironi)

        • permethrin (Acticin®,
          Ambush®, Elimite®, Imperator/Peripel®
          (EC : 200-500 mg/m2), Nix®, Pounce®),
          a synthetic derivative of

          pyrethrins


        • alphacyano pyrethroids : more reported side effects than
          permethrin, but far more active, can be used at lower doses and last
          longer than permethrin.

          • alphacypermethrin (Alphacypermethrin
            TG
            ®, Alphacypermethrin 95% TG®,
            Alphaguard 10 EC
            ®, Alphaguard
            TG
            ®, Bitin®,
            Fendona
            ® (SC : 20-40 mg/m2),
            Prabal 100
            ®, Renegade®)
            is a racemic mixture of 2 isomers (1R cis S and 1Scis
            R isomers) out of the 8 cypermethrin isomers. It is 2-3 times more
            active than cypermethrin under field conditions. It is effective on a
            wide range of insects in a variety of crops at dosage of 7-30g a.i./ha.
            Alphacypermethrin has contact and stomach action and can be used on
            cereals, cotton, fruits, vegetables, flower crops, oilseeds, sugar
            beet, tea, tobacco, vines, etc. for the control of a variety of
            insects.




          • bifenthrin (SC) (Talstar®)

          • cyfluthrin (Solfac® (EW : 30-50 mg/m2))

          • deltamethrin (K-Othrine® (SC : 15-25 mg/m2),
            K-O Tab® (tablet : 1 per net), SPOTON® (1%
            S.C.))

          • lambdacyhalothrin (Hallmark®, ICON®
            (CS : 10-20 mg/m2))



        • etofenprox (Vectron® (EW : 200 mg/m2))
          is completely different from the pyrethroids. Activity similar to
          permethrin, but far less toxic than any of the pyrethoids.

        • flumethrin (Bayticol & Drastic Deadline®) 1% S.C.

        • zetacypermethrin (Fury 10EW®)

        • piperonyl butoxide

        • bioresmethrin

        • esfenvalerate (Sumi-alpha®)

        • fenvalerate

        • remethrin


        Formulations :


        • suspension concentrate (SC) : active ingredient is in the
          form of crystalline particles mixed with solvents. Because the active
          ingredient is in particles, it is less easily absorbed by net fibers or
          by the skin - this means that the insecticide is not only more readily
          available to kill mosquitoes, but is less toxic to people.

        • capsule suspension (CS) : microencapsulated formulation. The
          active ingredient is encased in microscopic plastic capsules suspended
          in water. Capsule suspension formulation are more pleasant to handle
          than emulsifiable concentrates, have almost no smell and remain
          effective for a longer period of time - they are however usually more
          expensive.

        • emulsifiable concentrate (EC) : insecticide is mixed with a
          solvent to give a clear solution that turns milky when mixed with water.
          Because the solvent allows the insecticide to more easily penetrate the
          skin they can be significantly more toxic. Many agricultural pesticides
          are EC. Except for permethrin, EC formulations of the others should not
          be used for treating nets.

        • emulsion in water (EW) : the active ingredient is dissolved
          in a synthetic oil mixed with water so the insecticide is in fine oil
          phase droplets suspended in water. The synthetic oil helps the active
          ingredient to adhere to the net fibers. It also masks the smell and
          irritancy of the active ingredient.

        • wettable powder (WP) : the pesticide is mixed with a carrier
          plus a wetting agent. Commonly used for indoor spraying (e.g. ICON), but
          flakes off too easily when applied to a net. Only deltamethrin is
          effective in WP formulations - but because the other formulations are so
          much better, this should only be used in an emergency.




      • malathion


      • benzyl benzoate

      • crotamiton / N-ethyl-o-crotonotoluidide (Eurax®)

      • crotamiton (Eurax®)

      • 5% sulfur in petrolatum

      • thiabendazole



    • soil fumigants

      • cyanide / hydrocyanic acid (HCN) / prussic acid ==mt
        rhodanese / thiosulfate sulfurtransferase
        ==> thiocyanate
        .

        Therapy for cyanide intoxications
        .

      • methyl bromide (MBr) : chloropicrin (CCl3NO2),
        a powerful stimulator of lacrimation, is added to fumigants as a warning
        of methyl bromide exposure. Side effects :

        prostate adenocarcinoma
        .

      • D-D (a mixture of 1,3-dichloropropene and
        1,2-dichloropropane
        )

      • 1,2-dibromo-3-chloropropane (DBCP) (ClCH2CHBrCH2Br)

      • ethylene dibromide / 1,2-dibromoethane (EDB)

      • phosphine (PH3)



    • organo phosphorous

      • phorate

      • fensulphothion

      • thionazin

      • dichlofenthion

      • disulfoton

      • diazinon

      • fenamiphos



    • carbamates

      • aldicarb

      • carbofuran

      • methomyl

      • nydate










MANUFACTURERS OF DRUGS USED TO TREAT PARASITIC INFECTIONS


albendazole – Albenza (GlaxoSmithKline)
Albenza (GlaxoSmithKline) – albendazole
Alinia (Romark) – nitazoxanide
AmBisome (Gilead) – amphotericin B, liposomal
amphotericin B – Fungizone (Apothecon), others
amphotericin B, liposomal – AmBisome (Gilead)
Ancobon (Valeant) – flucytosine
§ Antiminth (Pfizer) – pyrantel pamoate
• Aralen (Sanofi) – chloroquine HCl and chloroquine
phosphate
§ artemether – Artenam (Arenco, Belgium)
§ artemether/lumefantrine – Coartem, Riamet (Novartis)
§ Artenam (Arenco, Belgium) – artemether
§ artesunate – (Guilin No. 1 Factory, People’s Republic
of China)
atovaquone – Mepron (GlaxoSmithKline)
atovaquone/proguanil – Malarone (GlaxoSmithKline)
azithromycin – Zithromax (Pfizer), others
• Bactrim (Roche) – TMP/Sulfa
§ benznidazole – Rochagan (Brazil)
• Biaxin (Abbott) – clarithromycin
§ Biltricide (Bayer) – praziquantel
† bithionol – Bitin (Tanabe, Japan)
† Bitin (Tanabe, Japan) – bithionol
§ Brolene (Aventis, Canada) – propamidine isethionate
chloroquine HCl and chloroquine phosphate – Aralen
(Sanofi), others
clarithromycin – Biaxin (Abbott), others
• Cleocin (Pfizer) – clindamycin
clindamycin – Cleocin (Pfizer), others
Coartem (Novartis) – artemether/lumefantrine
crotamiton – Eurax (Westwood-Squibb)
dapsone – (Jacobus)
§ Daraprim (GlaxoSmithKline) – pyrimethamine USP
† diethylcarbamazine citrate (DEC) – Hetrazan
• Diflucan (Pfizer) – fluconazole
§ diloxanide furoate – Furamide (Boots, United Kingdom)
doxycycline – Vibramycin (Pfizer), others
eflornithine (Difluoromethylornithine, DFMO) – Ornidyl
(Aventis)
§ Egaten (Novartis) – triclabendazole
Elimite (Allergan) – permethrin
Ergamisol (Janssen) – levamisole
Eurax (Westwood-Squibb) – crotamiton
• Flagyl (Pfizer) – metronidazole
§ Flisint (Sanofi-Aventis, France) – fumagillin
fluconazole – Diflucan (Pfizer), others
flucytosine – Ancobon (Valeant)
§ fumagillin – Flisint (Sanofi-Aventis, France)
• Fungizone (Apothecon) – amphotericin
§ Furamide (Boots, United Kingdom) – diloxanide furoate
§ furazolidone – Furozone (Roberts)
§ Furozone (Roberts) – furazolidone
† Germanin (Bayer, Germany) – suramin sodium
§ Glucantime (Aventis, France) – meglumine antimonate
† Hetrazan – diethylcarbamazine citrate (DEC)
Humatin (Monarch) – paromomycin
§ Impavido (Zentaris, Germany) – miltefosine
iodoquinol – Yodoxin (Glenwood), others
itraconazole – Sporanox (Janssen-Ortho), others
ivermectin – Stromectol (Merck)
ketoconazole – Nizoral (Janssen), others
† Lampit (Bayer, Germany) – nifurtimox
Lariam (Roche) – mefloquine
§ Leshcutan (Teva, Israel) – topical paromomycin
levamisole – Ergamisol (Janssen)
lumefantrine/artemether – Coartem, Riamet (Novartis)
Malarone (GlaxoSmithKline) – atovaquone/proguanil
malathion – Ovide (Medicis)
mebendazole – Vermox (McNeil), others
mefloquine – Lariam (Roche)
§ meglumine antimonate – Glucantime (Aventis, France)
† melarsoprol – Mel-B
† Mel-B – melarsoprol
Mepron (GlaxoSmithKline) – atovaquone
metronidazole – Flagyl (Pfizer), others
§ miconazole – Monistat i.v.
§ miltefosine – Impavido (Zentaris, Germany)
§ Monistat i.v. – miconazole
NebuPent (Fujisawa) – pentamidine isethionate
Neutrexin (US Bioscience) – trimetrexate
§ niclosamide – Yomesan (Bayer, Germany)
† nifurtimox – Lampit (Bayer, Germany)
nitazoxanide – Alinia (Romark)
• Nizoral (Janssen) – ketoconazole
Nix (GlaxoSmithKline) – permethrin
§ ornidazole – Tiberal (Roche, France)
Ornidyl (Aventis) – eflornithine
(Difluoromethylornithine, DFMO)
Ovide (Medicis) – malathion
§ oxamniquine – Vansil (Pfizer)
§ Paludrine (AstraZeneca,
United Kingdom) – proguanil
paromomycin – Humatin (Monarch); Leshcutan (Teva,
Israel; (topical formulation not available in US)
Pentam 300 (Fujisawa) – pentamidine isethionate
pentamidine isethionate – Pentam 300 (Fujisawa),
NebuPent (Fujisawa)
† Pentostam (GlaxoSmithKline, United Kingdom) – sodium
stibogluconate
permethrin – Nix (GlaxoSmithKline), Elimite (Allergan)
§ praziquantel – Biltricide (Bayer)
primaquine phosphate USP
§ proguanil – Paludrine (AstraZeneca, United Kingdom)
proguanil/atovaquone – Malarone (GlaxoSmithKline)
§ propamidine isethionate – Brolene (Aventis, Canada)
§ pyrantel pamoate – Antiminth (Pfizer)
pyrethrins and piperonyl butoxide – RID (Pfizer), others
§ pyrimethamine USP – Daraprim (GlaxoSmithKline)
Qualaquin – quinine sulfate (Mutual Pharmaceutical Co/
AR Scientific)
* quinidine gluconate (Eli Lilly)
§ quinine dihydrochloride
quinine sulfate – Qualaquin (Mutual Pharmaceutical Co/AR Scientific)
Riamet (Novartis) – artemether/lumefantrine
• RID (Pfizer) – pyrethrins and piperonyl butoxide
• Rifadin (Aventis) – rifampin
rifampin – Rifadin (Aventis), others
§ Rochagan (Brazil) – benznidazole
* Rovamycine (Aventis) – spiramycin
† sodium stibogluconate – Pentostam (GlaxoSmithKline,
United Kingdom)
* spiramycin – Rovamycine (Aventis)
• Sporanox (Janssen-Ortho) – itraconazole
Stromectol (Merck) – ivermectin
sulfadiazine – (Eon)
† suramin sodium – Germanin (Bayer, Germany)
§ Tiberal (Roche, France) – ornidazole
Tindamax (Mission) – tinidazole
tinidazole – Tindamax (Mission)
TMP/Sulfa – Bactrim (Roche), others
§ triclabendazole – Egaten (Novartis)
trimetrexate – Neutrexin (US Bioscience)
§ Vansil (Pfizer) – oxamniquine
• Vermox (McNeil) – mebendazole
• Vibramycin (Pfizer) – doxycycline
• Yodoxin (Glenwood) – iodoquinol
§ Yomesan (Bayer, Germany) – niclosamide
• Zithromax (Pfizer) – azithromycin
* Available in the US only from the manufacturer.
§ Not available in the US; may be available through a compounding pharmacy (see footnote 4).
† Available from the CDC Drug Service, Centers for Disease Control and Prevention, Atlanta, Georgia 30333; 404-639-3670 (evenings, weekends,
or holidays: 770-488-7100).
• Also available generically.
Treatment Guidelines from The Medical Letter • Vol. 5 (Suppl) • 2007


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