CHEMOTHERAPY

Problems arises with use antimicrobial drugs are 1.Toxicity 2.Resistance 3.Superinfection Combination of drugs Cidal+cidal = synergistic(sulpha+TMP) Cidal+static = Antagonistic Static+static =Additive Post antibiotic effect high with aminoglycosides Biphasic effect Quinolones

Synthetic AMA
Sulphonamides :-structural similarity with PABA MOA:-Inhibit Folic acid synthesis,competitive inhibition of PABA

Classification 1.Systemic:Short acting:-Sulphadiazine,Sulphamerazine,Sulphathiazole Intermediate acting:Sulphadimidine,Sulphamethoxazole,Sulphaphenazole Long acting:Sulphadimethoxine,Sulphaethoxypyridazine,Sulphabromethazine 2.GUT ACTING Phthalyl sulphathaizole,Succinyl sulphathiazole,Sulphaguanidine, Sulphasalazine 3.TOPICAL SULPHONAMIDE Mefinide,Silver sulphadiazine 4.OPHTHALMIC :Sulphacetamide

TOXICITY:- crystallurea Potentaited sulphonamides:Sulphamethoxazole+Trimethoprim(5:1) combination results in sequential blockade of folic acid synthesis. Trimethoprim inhibit conversion of DHF to THF by inhibiting enzyme THFR

Quinolones:1st generation :- Nalidixic acid(narrow spectrum) Flouroquinolones(Broad spectrum):Norfloxacin,Ciprofloxacin,Pefloxacin,Marbofloxacin,Orbi,Enro,Da nofloxacin Veterinary use:-Enrofloxacin MOA:- Inhibit DNA gyrase enzyme Toxicity:- Joint arthropathy

NITROFURANS
Nitrofurazone,Nitrofurantoin,Furazolidone, MOA:- Inhibit energy metabolism Used topically BETALACTAM ANTIBIOTICS Penicillins,Cephalosporins,lactamase inhibitors,other lactam antibiotics MOA:-Inhibit peptitoglycan synthesis there by inhibiting the cell wall synthesis Classification:1)Natural penicillin:-Benzyl penicillin,Acid resistant:-Penicillin V 2)Semisynthetic Penicillin:-Penicillinase resistant penicillin Eg:- Oxacillin,Cloxacillin,Methicillin,Naficillin

3)Broad spectrum Penicillins:Ampicillins,Amoxycillin Prodrugs of Ampicillin:-Hetacillin,Becampicillin,Talampicillin 4)Others:- Mecillinam(Amidocillin only for Gram negative bacteria) Extended spectrum :- Carbencillin,Ticarcillin 5) Beta lactamase inhibitors/Potentiated penicillins Clavulanic acid(Suicide inhibitors) Amoxycllin+ Clavulanicacid:- AUGMENTIN Sulbactam Tazobactam

CEPHALOSPORINS 1st Generation:- Cephalothin,Cefazolin,Cephalexin,Cefedroxil 2nd generation :- Cefuroxime,cefaclor,Cefomandol 3rd generation:-Cefotaxim,Ceftiofur,Cefopearzone,Ceftriaxone 4th generation :- Cefepime,Cefperome CARBAPENEMS IMIPENEM:-Most broad spectrum lactam antibiotic Cilastatin inactivates Renal dehydropeptidase there by prevent deactivation of imipenem Meropenam:- No need of cilastatin MONOBACTAM Aztreonam-Gram negative enteric bacilli

AMINOGLYCOSIDES Streptomycin:-Waksman 1944- from Streptomyces griseus Gentamicin-Micromonospora purpurea Kanamycin- Streptomyces kanamyceticus Tobramycin-S.tenebrarius Amikacin:- Semisynthetic from Kanamycin Sisomicin-Micromonospora.inyonensis Netilmicin Semisynthetic from Sisomycin MAO:-Inhibit 30S ribosomal subunits-Misreading of mRNA codone Toxicity:- Nephrotoxicity,Ototoxicity,NM blockade

TETRACYCLINS S.Aureofaciens:-Chlortetracyclins Broad spectrum more active against Gram positive bacteria Short acting:-Oxytetracyclins,Chlortetracyclins Intermediate acting :-Demeclocyclins Long acting:- Doxycyclins,Minocyclins MOA:- Inhibit protein synthesis by inhibiting 30S ribosomal subunit Side effects:- Superinfection,irritation,Calcium chelation,Hypotension

CHLORAMPHENICOL S.Venezualae, Bacteriostatic,Broad spectrum, Highly lipid soluble. MOA:-Inhibit protein synthesis Bind with 50S ribosomal unit Toxicity Aplastic Anemia(Para nitro group) Less toxic Thiamphenicol,Floufenicol Macrolides Erythromycin- S.erythreus Broad spectrum Azithromycin,Dirithromycin,Roxithromycin,Tilmicosin,Tylosin MOA:- Inhibit protein synthesis by inhibiting ribosomal subunit Oleandrmycin,Troleandromycin

LINCOSAMIDES AND MONOGLYCOSIDES MOA:-Inhibit protein synthesis by inhibiting 50S ribosome Side effect:- Psuedomembraneous colitis bu cl.difficile MISCELLANEOUS Polymixin:- B.polymyxa Vancomycin:-Glycopeptide Rifamycin:-S.mediterranei(gram ve) Rifampicin:-Semisynthetic rifamycin MOA:- inhibit DNA dependant RNA polymerase,Gram positive bacteria

ANTHELMINTHICS Antinematodal 1)Benzimidazoles- Thiabebdazole,Albendazole,fenbendazole MOA:- Inhibit polymerisation of tubulin ,Inhibit fumerate reductase 2)Benzimidazole prodrugs:- Febantel,Netobimin,Thiophanate 3)Macrocyclic lactones:- Ivermectin,Doramectin MOA :-Binds glutamate gated chloride channels 4) Imidazothiazoles:- Tetramizoles,Levamisole MOA :- Stimulate aaans-susained muscle contraction 5)Tetrahydropyrimidines:-Pyrantel,Morantel MOA:-Neromuscular blocking agents

6)Piperazines(GABA agonists):- Piperazine,DEC 7)Miscellaneous:- Phenothiazines ANTICESTODAL 1)Isoquinolones:- Praziquantel,epsiprantel MOA:- Interfering with regulation of calcium concentration 2)Salicylanides :- Niclosamides MOA:- Inhibit oxidative phosphorylation 3)Substitiuted phenols:-Dichlorphen MOA :-Inhibit oxidative phosphorylation 4)Benzimidazoles 5)Natural agents:- Kamala(Mallotus philippensis),Arecolin

ANTI TREMATODAL DRUGS 1)Substitiuted phenols:-Dichlorphen,Nitroxynil,Bithional 2)Salicylanides :- Niclosamide,Closantel,Rafoxanide,Oxyclosanide 3)Aromatic amides:-Deamphenitide MAO:-Vaculation of tegument ogfmparasite