Chemoterapeutics of synthesis Flashcards
Arsenic derivatives
Antihistominic tto
Electivity on: parasitic flagellates and helmints
Bistuth derivatives
Antihistominic tto Derivatives: carbonates, salicylates... Spectrum:Diarrhea therapy w colibacillosus and spirochetes; weak on trypanosoma Carbonates of busmuth: antiacid effect Comercial: Bivatol, Bistrimate
Tripaflavin (adriflavine, Gonacrin, Flavacridium…)
Antihistominic tto
Acridine derivatives
In hematosporidiosis: nutualosis babesiosis. babesiolosis
NO actv in: theiloriosis and anaplasmosis
Locally in gynecology
Rivanol (aethacridini lactas)
Antihistominic tto
Acridine derivatives
Mode of action: antiseptic and bactericidal against strepto and staphilococcus
Not irritatin, no disturbance of phagocytosis
No lost f(x) in precense of blood serum
Ethacrynic acid
Antihistominic tto
Acridine derivatives
Mode of action: diuretic similar activity to furosamide
Spectrum: active against streptococcus
Side effects: ototoxicity, enteritis and vomiting
Edericin, Reomax, Taladren…
Bovoflavine
Antihistominic tto Acridine derivatives Mixture of 3 acridine derivatives Ointment in genital tract in cattle Spectrum: genital trichomonasis Side effects: balanophositis and balanitis
Atebrin
Antihistominic tto
Acridine derivatives
Humans: tto 4 malaria
Vet: tto 4 protozooses
Quinacrine
Antihistominic tto
Acridine derivatives
Spectrum: in trichomoniasis and giardasis
Side effects: anorexia, vomiting, enteritis, skin pigmentation, hepatotoxicity
Naganole
Anttitrypanomiasis tto
Acridine derivatives
To 4 try
Antimony (Sb) derivatives
Trypasonomiasis Tto
Similar mode of action to arsenic (active against flagells and helmints), organic and inorganic derivative have antivomiting and expectorant actv
Spectrum: trypanosomyasis, filariasis, has 3valent derivatives as well as pentavalent derivatives
- Antimosan: antihelmintic actv in ruminants
- Neoanimosan: dicroceliosis in sheep, Fuadin
- Antimony potassium tartrate
- Stibosan and Stibophen: some animals due to therapy can develop several degrees of inmunity against the parasite (trypanosomiasis)
Diamidines
Trypasonomiasis Tto
Babesia tto
Mode of action: babesicidal and antibact actv (the presence of 2 groups of guanylama guanylamadin separaden by a chain of paraffinic hydrocarbon-> trypanocide actv)
side effect: may increase internal muscle movs
Phenamide Isethionate
Antibabesia Tto
Diaminide
Effective in: babesiosis in cattle. horses and dogs
Spectrum: strong action i Theileria evansi and T.burucei
Stilbamine and Pentamidine
Trypasonomiasis Tto
Diaminide
Toxic (preferred pentamidine to treat human trypasonomiasis)
Amicarbalide isothionate
Antibabesia Tto
Diaminide
Spectrum: active on babesia ssp but not very in B.canis
Used 4 preinmunity by controling clinical symptoms (NOT definitive elimination)
Side effects: hb level declines much after 48h, small reactions at injection site
Nitrothiazole group
Antihistomonas tto
Mode of action: presence of nitro group under the influence of nitroreductase developed by mmoo-> into toxic producrts
Resistance can b installed and its crossed
Nithiazide (Hepzide)
Nitrothazole group
Antihistomonas tto
Spectrum: efficient against histomoniasis and trichomoniasis in birds
Homidium Halogenates
Antihistomonas tto
Amino - phenantridium compound
mode of action: trypanocide actv
spectrum: T.congolense and T.vivax
side effects: severe local reactions or laminitis
Homidium Novidum
Isometamidium chloride
Tryponosomiasiss tto
Amino - phenantridium compound
Mode of action: trypanocide
Spectrum: T. vivax and congolense + T.evansi
side effects: local reactions and necrosis
Berenil
Tryponosomiasiss tto
Aceturat diminazen compounds (triazine)
Good antiseptc action
Spectrum: trypanosomiasis (v effectuve) and moderate effcets on T. brucei
Disapareance of symptoms in animals w babesia
side effects:
- in horses injuries and severe irritation on injection site
- overdose: respiratory ans digestive problems, aniety and hypotension
Commercials: Berenilum, Azidin
Antricid
Tryponosomiasiss tto Quinapyramin compounds Trypanocide (inhibits parasitc growth phase ans cell division) Spectrum: Trypanosoma spp Commercial: antricid, quiropiramin
Suramin
Tryponosomiasiss tto
Quinapyramin compounds
Spectrum: T. evansi, brucei, equinum, equiperdium
Meium toxicity= has a narrow therapeutic index
Saprosan (dichloroxyquinaldine)
Antitrichomonas tto
Oxyquinolone derivatives
Antibacterial, intestinal antifungal and antiprotozoan
Spectrum: enterococci, staphylococci, streptococci
Saprometin
Antitrichomonas tto
Oxyquinolone derivatives
Iodisept
Antitrichomonas tto
Oxyquinolone derivatives
Vioform in the tto of enteritis and enterocolitis
Decoquinate and Nequinate in coccidiosis
Methylene Blue
Antitrichomonas tto
Thiazine derivatives
mode of action: influences tissue redox processes
Local antiseptic and urine permeability testing agent
Traumatic wounds, arthritis, mouth ulcers, injuries…
Rapid distribution
Pioctatin
Antitrichomonas tto
Triphenylmetane derivatives
Intensive antiseptic properties that decrease w organic substances
Wounds, ulcers, sores, wet ezcema, dermatomycosis
Nitrofuran derivatives
Antitrichomonas tto
Action: interfiring enzymatic oxidative processes
Bacteriostatic (bactericidal)
Spectrum: G+/-, Trichomonas, Giardia,, Amoeba, Eimeria, (NO Proetus)
Side effects: parenterally can cause: enteritis, eosinophilia, peripheral polineuritis, optic nerve damage
Commercial: Furoxona,Clorovit
Nitrofuran
Antitrichomonas tto
Nitrofuran derivatives
Spectrum: G+ some G- pathogenic protozoa (coccidia, trichomonas)
In obstetris and gynecology, mastitis, GET
Commercial: Nitrofural, D¡Furacin, Furacilin
Furazolidone
Antitrichomonas tto
Nitrofuran derivatives
In avian and swine salmonellosis and colibacilosis in piglets, Histomoniasis, avian coccidiosis, giardasis, edema disease…
Commercial: Furazolidone, Galifuran
Nitrofurazone
Antitrichomonas tto
Nitrofuran derivatives
Active: antiprotozoal, G+/-
Spectrum: digstive affections caused by salmonella
Clioquinol
Antitrichomonas tto
Quinoxaline derivatives
Mild enteritis, restoring eurobiosis, dysentery
uterine path, powders, ointments
Chlorquinaldol
Antitrichomonas tto
Quinoxaline derivatives
Mode of action: synergizises associated w carbadox, oxytetracycline, sulfonamides
Really good absorption Indic: diahrrea, swine atrophic rinitis and septics dermatitis
Olaquindox
Antitrichomonas tto
Quinoxaline derivatives
used mainly in piglets
Trypan Blue
Antibabesian Tto
Benzidine derivatives
Spectrum: B. equis, bovis, gibsony
animal remains a carrier
diffuses well, stains body and milk
Side effects afetr injection:
- Resp disorders
- Heavy sweating and chills
Commercial: Tripasin Tripanblau
Quinolone Carbonic acid derivatives (quinolones)
Action: Bloking bact DNA gyrase (their presence blocks the negative spiral phase in the bacterial chromosome, determined by DNA gyrase-> results in small fragments of nonf(x) DNA-> bact death)
Spectrum: G+, E. coli, proteus, Pseudomonas, Mycoplasma
Activity: bactericidal= at bact nuclear level, which pry the dna and idstorts its functions
Side effects: GI disorders, central nervous manifestations, erratic, some arthopatic effects in young animals
Commercials: Gramurin (Oxolinic acid)
Quinolone Carbonic acid derivatives (quinolones)
Action: Bloking bact DNA gyrase (their presence blocks the negative spiral phase in the bacterial chromosome, determined by DNA gyrase-> results in small fragments of nonf(x) DNA-> bact death)
Spectrum: G+, E. coli, proteus, Pseudomonas, Mycoplasma
Activity: bactericidal= at bact nuclear level, which pry the dna and idstorts its functions
Side effects: GI disorders, central nervous manifestations, erratic, some arthopatic effects in young animals
Commercials: Gramurin (Oxolinic acid)
Nalidixic acid
Quinolone
Spectrum: limited and deep-> G- on enterobacter and Klebsiella; less active on P.aureiginosa and G+ (not active)
Big part inactivates in the liver via oxidation and conjugation reactions
Side effects. DIGESTIVE IRRITATION, liver diseases
Oxolinic acid
Quinolone
Spectrum and mode of act: similar to nalidixc but less toxic
Side effects: same plus photosensitization
ommercial: Gramurin
Flumequine
Fluorinated quinilone derivatives
Antimicrobial effect: due to the whole molecule, halogens are liberated in trace amounts
Spectrum: G+/- (very effective on E. coli, salmonella, proteus, klebsiella
Activity: bactericidal, bacteriolitic
Side effects: cartillage damage and hepatotoxicity
Commercial: Imequil 10% soluble powder
Cinoxacine
Fluorinated quinilone derivatives
Antimicrobial effect: due to the whole molecule, halogens are liberated in trace amounts
Spectrum: G+/-
Activity: bactericidal, bacteriolitic
Similar to oxolinic acid and flumequine, not used yet ina animals
EnroFloxacin
Fluorinated quinilone derivatives
Antimicrobial effect: due to the whole molecule, halogens are liberated in trace amounts
Spectrum: G+/- (exclusevily anaerobes)
Activity: bactericidal, bacteriolitic
Side effects: non toxic neither at x10 - 40 times dose, articular cartilage damage in dogs
Ciprofloxacin and Norfloxacin
Fluorinated quinilone derivatives
Antimicrobial effect: due to the whole molecule, halogens are liberated in trace amounts
Spectrum: G+/-
Activity: bactericidal, bacteriolitic
Danofloxacin
Fluorinated quinilone derivatives
Antimicrobial effect: due to the whole molecule, halogens are liberated in trace amounts
Spectrum: G+/- (V good i pneumonia caused by Haemophillus spp)
Activity: bactericidal, bacteriolitic
New w promising uses
Major constitutens:
- ibafloxacin
- Sparfloxacin
- Difloxacin
