Support forum for people interested in Drugs therapy, Prescription Medications therapy against parasites. ANTIMICROBIALS FOR EUKARYAL ORGANISMS In some parts of Southeast Asia they are the only effective treatment Prospective clinical trial data are pending. ... cell wall ... cell membrane stability ... DNA and RNA synthesis ==> 5-fluoroUTP ==> incorporated into RNA ... protein synthesis ... cytoskeleton ...O-glycosylations ... unknown diethylcarbamazine (DEC) citrate (Filaribits®, Formulations :
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)
: they can interfere with ...
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 :
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))
Plasmotrim®)
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
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.
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.
3-methyl-4(5'-nitrofurfurylideneamino)-tetrahydro-4H-1,4-thiazine-1,1-dioxide
/ Bayer 2502 (Lampit®)
combination with proguanil (ATQ/PG)
(Malarone®)
quinine and its optical isomer quinidine.
primaquine; once called Resochin®)
phosphate, diphosphate or sulfate.
Camoquin®, Camoquinal®, Flavoquin®,
Fluroquine®, Miaquin®, SN-10,751®;
Camoprima Infatabs® in combination with
primaquine)
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.
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
Duo-Cotecxin®)
trimethoprim
and primaquine
trimethoprim
and primaquine (China-Vietnam 4 (CV4®),
which was followed by CV8® (the same components as CV4 but
in increased quantities)
trimethoprim
(Artecom®)P
in combination with chloroquine)
combination with chloroquine)
half-life measured in weeks rather than hours)
Zn
chelator)
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
in combination with chlorproguanil)
required to produce comparable inhibition of the mammalian enzymes) (antifols)
work poorly against P. vivax
sulfadoxine in Fansidar®, in
combination with dapsone in Maloprim®)
amethopterin (4-amino-10-methylfolate) / methotrexate (MTX)
trimethoprim
Side effects : QTc prolongation
/ CGP 56697 / A-L (Coartem®, Riamet®) in
combination with artemether)
chlorhydrate => cycloguanil; usually administered in combination
with atovaquone (Malarone®)
combination with dapsone)
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.
(DFMO) hydrochloride (Ornidyl®, Vaniga®) :
also used to treat unwanted facial hair (UFH) in females.
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 bruceiref
Pentam® or NebuPent®)
amphotericin B
(AmB) deoxycholate (DAMB) (Amphocil®,
Amphocin®, Fungilin®, Fungizone®,
Intralipid®) : parenteral 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.
(Amphotec®)
Fujisawa Healthcare, Inc.)
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
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
emetic)
(i.v.)
paromomycin
sulfate (Humatin®) (nonabsorbed aminoglycoside)
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
(Deflamon®, Flagyl®, Metrocream®,
Metronidazolo®, Metrogel®, Noritate®,
Protostat®, Vagilen®; Meclon 100® in
combination with clotrimazole)
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 bruceiref
ref1,
ref2 : they can interfere with ...
synthesis
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
than for cholesterol) and create pores or channels.
nystatin
(Mycostatin®, Nilstat®) active against
Candida
Aronex Ltd., EE.UU.)
partricin
used chiefly in the treatment of vaginal and cutaneous candidiasis,
applied topically.
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.
Micospor®)
Lotremin®, Lotrimin®, Mycelex®,
Gynelotrimin®, Gyno-canesten®, Mycelex-G®;
Meclon®, Meclon 100® in combination with
metronidazole)
Ifenec-Ginec.®, Micos®, Pevaryl®,
Pevaryl Gel®; Pevisone® in combination with
triamcinolone)
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®)
Imaverol®, Imazalil®)
Lomexin®)
Travogen® cream, Gyno-Travogen®cream; Travocort®
in combination with
diflucortolone valerate)
Scalp Fluid, Nizoral® Shampoo, Extina®,
silvadeneTriatop®). It also inhibits
CYP11A1,
CYP11B2,
CYP17A1,
and
CYP51A1
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®)
Sertaderm®, Sertadie®, Sertagyn®)
Trosyd Soluzione Unguele®Vagistat 1®)
Elazor®)
Triasporin®) : dilute in water, make oral cavity washings
and then swallow
: fungal squalene epoxidase inhibitors
Suadian®) inhibits squalene-2,3-epoxidase and so fungal
biosynthesis of ergosterol
Distocide®, Pikiton®) : a pyrazinoisoquinoline that
alters membrane permeability
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
it crosses blood-brain barrier ==deamination (not in mammalian cells
!!)==> 5-fluorouracil ==UMP pyrophosphorylase==> 5-fluorouridylic acid
==> 5-fluorodeoxyuridylic acid, an inhibitor of thymidylate synthase
fusidic acid
inhibits eEF2
Corynebacterium diphtheriae
toxin
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.
UDP-GlcNAc, preventing all O-glycosylations.
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.
Tinaderm®, ...)
Desenex®, Dr Scholl's®, Egomycol®, Mycota®)
Miltex®) (p.o.) inhibits CTP:PC cytidylyltransferase
effective against various fungi, including Candida albicans; used
topically in the treatment of fungal infections of the vulvovaginal region
and of the skin
salicylic acid 3%
topical solution
or
dewormers (including helminthicides / helminthagogues and
nematicides)
pyrazinoisoquinoline that increases membrane permeability of calcium and has
a selective effect on the tegument of trematodes
kinase and mutase
formation
Valbazen®)
Safeguard®)
Vermox®)
Ominzole®, Thiabendazole®)
(E233)
is a fasciolicide
GABA-R
agonist on nematode muscles => causes flaccid paralysis.
Hetrazan®) blocks host, and possibly parasite, enzymes
involved in arachidonic acid metabolism, and enhances the innate,
nonspecific immune system.
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
morpholine ring at each of the 2 D-phenyllactic
acids in para position
avermectins
/ 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.
Equest Oral Gel®, ProHeart®,
ProHeart 6®, Quest®)
AChE
inhibitors :
=> dichlorvos / 2,2-dichlorovinyl dimethyl phosphate (DDVP)
N AChR
agonists => spastic paralysis
(--)-2,3,5,6-tetrahydro-6-phenylimidazo[2,1-b]thiazole
(Decaris®, Levasol®, Tramisole®,
Ripercol®, Ergamisol®) is also an
immunomodulator
Rumital®)
Combantrin®)
Novidium®)
miticides / acaricides)
lindane
/ g isomer of benzene hexachloride /
hexachlorobenzene (HCB) / hexachlorocyclohexane (HCH)
(Kwell®, Scabene®,
...)
Bitin®)
spirals (from the inventor's name Zampironi)
Ambush®, Elimite®, Imperator/Peripel®
(EC : 200-500 mg/m2), Nix®, Pounce®),
a synthetic derivative of
pyrethrins
permethrin, but far more active, can be used at lower doses and last
longer than permethrin.
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.
K-O Tab® (tablet : 1 per net), SPOTON® (1%
S.C.))
(CS : 10-20 mg/m2))
is completely different from the pyrethroids. Activity similar to
permethrin, but far less toxic than any of the pyrethoids.
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.
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.
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.
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.
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
rhodanese / thiosulfate sulfurtransferase==> thiocyanate.
Therapy for cyanide intoxications.
a powerful stimulator of lacrimation, is added to fumigants as a warning
of methyl bromide exposure. Side effects :
prostate adenocarcinoma.
1,2-dichloropropane)
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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