PMOC-Incomplete PDF

 Gues Usebioes Anti-Infectives > Salvarson Arsphenamine Paul Erlich , HCl Compound 606 (anti-syphilis OH NHL g -...

 Gues Usebioes Anti-Infectives > Salvarson Arsphenamine Paul Erlich , HCl Compound 606 (anti-syphilis OH NHL g - As ,Selective Toxicity Father of Chemotherapy - 0H HCl Salvarsan O Atoxyl/ Na Arsanilate Arsphenamine 1 To - Nat NH2 > - sleeping sickness Arsphenamine Terms Germicide-anti-infective used locally Anti-sepsis-anti-infective used in living tissues Disinfection-anti-infective used on inanimate objects Decontamination-marked reduction of microorganisms Sanitation - reduction of microbial load on an inanimate object to a level acceptable for public use Sterilization - destruction of all types including spores , , of microbes w/ virus at low chance of survival Pasteurization killing - microbes by hot water/steam & 65-100 C °  a) based on chemical type 3 Classificatin a · b) based on biological property c) based on therapeutic indication LOCAL Antiinfectives Mechanism of Actions : Formalin a) Coagulation 3 Denaturation Strong : Alcohol of Proteins coagulators Phenol Denaturant : heneacida bases I b) Injury to Cell Wall Cationic surfactants 2) Inhibition of Enzymes Oxidizing agents 3 Heavy metal (Hg-containing) salts d) Chemical entagonism Binders Based on Chemical Classification 1) Alcohols & Related Compounds 2) Phenol 3 Derivatives 3) Oxidizing agents 2) Halogen-containing compounds 3) Cationic surfactants 6) Miscellaneous 1) Alcohols & Related Compounds MOA: Protein precipitation/coagulation SAR : ↑potency = ↑ # of C until 18 ↑ potency I branching = Hierarchy of potency 10 720730 Exemption Isopropyl Of : a) Methy Ol aka Methanol / Carbinol (Wood OH Alt g 8 Il [O] H-'- I Los , It-C- > H-C- OH Formaldehyde/formalin formic a methano b) EthylOH aka Rectified Ethanol Grain OH SpiritusVil alicates spirit Wineirit Preparations Ol 25 % antipyretic - It I 60-90% germicidal - H - C C It - 78% disinfectant - it it 95% - commercial , forms azeotrope w/H2O @78 2 co. Use Denatured 4 impurities ; completely denatured - by methanol benzene UsesAlleviates pain (external) weak vasodilator Synthesis Hydration of Ethene · · · ↓ narcotic potency · carminative Fermentation by Yeast · · Mild Sedative (internal) · solvent c) Isopropyl OH aka Rubbing OH H I Ou I Preparations H- C - C - C-H 5 95 % -bacteriCIDAL - it it it 40 % = 60% C isop. etOlt C C 68-72 % disinfectant · ot Uses Synthesis · Disinfectant/antiseptic · H2S04-catalyzed Hydration of Propylene · Astringent C · Rubefacient HaSoy CH3 Mild localanesthetic H2w C ot · C H2 d) Azeotropic Esopropyl OH gauze pads for sterilization of skin prior to L used on hypodermic injection e) Dehydrated OH aka Absolute OH contains NLT 99 % w/w ethyl OH L prepared by azeotropic distillation of etOl & benzene f) Diluted OH 9) Glycerin aka Glycerol L Ethyl OH + H20 L 11 2 3. - propanetriol C C - - C (4) 42%) o ot of - ↓ 1st polyhydric OH that can yield on aldose or before L used as solventa humectant h) Ethylene Oxide C ⑧ ↓ C2Hy0 C gas sterilent for temperature-sensitive equipment I ↳ Treactivity explodes in air & 3-80% = L (+ 790 % CO2 + 10% Ethylene = Carboxide = (x) explode oxide MOA · Alkylation of proteins nucleic a ↑ carcinogenicity = (non-selective) i) Formaldehyde aka Formalin Formol Methanal , , It - C H - ~ disinfectant for moms/clothing/surgical (10% inH20) instruments but is irritating lol I - NLT37% w/ Methanol to prevent ↓ out usually contains polymerization paraformalin MOA ~ Direct non-specific alkylation of nucleophilic fx groups like SH NH , OH in , proteins 3 nucleic a to form carbina j) Glutaraldehyde aka Glutarol , Pentanedial H i C H , C C C Ha C H - superior to formaldehyde - - - - - & L effective against all microbes spores virus , , I' if it ~ for equipment that cannot be autoclaved k) Commercial Glutaraldehyde L in an alkaline buffer & contains 2 % glutaraldehyde buffered at pH 7 3-8. - stable and retains 80% activity after 30 days 2) Phenol & Derivatives MOA : Protein precipitant 3 denaturant SAR ↑ activity (t) Ro Xgroup @ PARA position : = a) Phenol aka Carbolic Phenic. OH I E A ↳ soluble in 1: 13H20 g ↓ Tchance to form Extectic mixtures Uses · Germicide as a protoplasmic poison Actions · Local anesthetic but corrosive/caustic M dose lysis well wall = · Antiseptic Joseph Lister = ↓ dose denature/ precipitate : protein * Phenol = ratio of disinfectant to the dilution of phenol required to kill a given coefficient strain of Salmonella typhi b) Liquified Phenol-10% H2 H 1) P-chlorophenol To / ~ external antiseptic anti-irritant w/ camphor in liquid petrolatum ↓ Phenol coefficient -4 d) Chloro-m-xylenol aka PC-MX Metasep , ↓ non-irritating antiseptic broad-spectrum antifungal Bentibactericidal ↳ ↳ OH 2 % in shampoos cl ↓ for finea infx such as athletes foot b jock itch 2) Hexachlorophene aka Phisohex , Gamophen Surgicon , ~ 2, 2-methylenebis (3 ,4 6-trichloro) pheno. 2) L antiseptic for G(+) , i -x41 G O 2-3 % in soaps creams shampoo ~ , , Cl of on '2 ↳ Contraindicated for infants 3 burn PX (CII) ↓ SAR : ↑ C1 ↑ potency = causes Neurotoxicity ↑ # phenol d) Cresol ↓ from coalta/petrolatum via alkaline , acidification fractional distillation , extraction into acid medium H OH OH I ~ CH3 I O g O CH3 its OH e) Chlorocresol O I preservative CH L CH3 f) Thymol aka Isopropylm-cresol I O ~ from oil of thyme - OH I ↳ anti-fungal in solutions dusting for tinea  9) Resorcinol aka M-dihydroxybenzene Resorcin , L weak antiseptic P L KERATOLYTIC O - ↓ Ol 1-3% in solutions ↓ & 10-25 % in pastes/ointments forskitions h) Hexylresorcinol USP aka 4-hexylresorcinol , mild anesthetic for throat lozenges ↓ antiseptic & bactericidal Ol fungicidal L surfactant O i) Eugenol aka 4-allyl-2-methoxyphenol OH ↓ local anesthetics mouth wash Ib antiseptic O L Dental analgesic in toothache L drops I from clove 3) Oxidizing Agent MOA : Enzyme inhibition & lysis SAR N/A : a Hydrogen Peroxide (H2O) L short-acting germicide L liberates O2 I bubble/froth 2 susceptible to Catalase > H20 - + 02 b) Carbamide Peroxide aka Gly-Oxide 9 9 H202 LH202 + Urea/Carbamide complex HaN NH2 usually 12 6% carbamide anhydr as. in peroxide cerin ~ liberates H202 in the presence of He O Uses skin whitener Antiseptic · For oral ulcers 2) Benzoyl Peroxide aka Benoxyl Oxy 5 Oxy , - , 10 ,Vanoxide unstable chemic ally ↳ · Keratolytic keratogenic + for acne (5-10%) [ - (sloughing) (proliferation) T 4) Halogen-containing Compounds - MOA : Halogenation & oxidation SAR ↑Hhalogens ↑ activity : = 4a.. Iodine-containing Compounds/ Todophors MOA : Protein inactivation via iodination of aromatic amino a Oxidation of Sl groups 9 Todoform ala Triiodomethane It I L bactericidal fungicidal I C T - - - I b) Iodine (12) I ↳ oldest germicide as fincture 3 liniment Preparations Iodine fincture = 2 % iodine (Nal) in 50% alcohol Strong Iodine solution = 5 % iodine (KI) in water (Lugol's soln) Iodine Soln. = 2% iodine (Nal) in water c) Povidone Iodine USP - , surfactant polymer + iodine (10 ) % ↓ non-ionic polyvinyl pyrolidone (prp) Slowly liberates iodine ~ non-toxic, non-irritating , non-staining.b Chlorine-containing Compounds 4. MOA : Protein inactivation via chlorination of amide, 3 Oxidation of Sl groups Holl Optimal & pH7 0. ( HCIO or ( imide, amidines a) Halazone 1 p. chlor sulfinoylbenzoic a used primarily in drinking water -N 6) Chloroazodin aka Azochloramid - Cl N N , N-dichlorodicarbonamidine HzN II Ni N ↓ (t) glyceryltriacetate wound NH2 i - > dressing long lasting due to show rx w/ H2 c)Oxychlorosene Na aka Chlorpactin (liberates HC0 wI rapid action against fungi , GI bacteria spores , , virus L powder for reconstitution o used as 0 1-0 5 % solution.. 10 1-0 2% for vology sopthalmology.. 5) Cationic Surfactants anionic - cationic zwitterion MOA : lysis of cell walls SAR : Usually are quaternary NHy cmpds. PROPERTIES : ADVANTAGES DISADVANTAGES · Broad speetem GI w/ · (x) Activity on SPORES keratolytic property Inactivated ANIONS by · ↑ H20 solubility · soap · I toxicity · Detergent · stable · bodily fluid · non-staining/corrosive a) Benzalkonium Chloride aka Cephiran chloride ↳ alkylbenzyldimethyl ammonium detergent emulsifying , wettinga _ agent C "New Merthiolate" b) Methylbenzethonium chloride ala Diaparane L benzyldimethy/[2-[2-[[4(1 3-tetramethylbutyl)toyl]oxyJethoxyJ ethyl) NHy Ch 1 3,. , for diaper rash caused by ammoniagenes T c) Benzethonium chloride USP aka Phemerol chloride , ↳ similar to benzalkonium chloride Preparations 1 : 5000 = irrigation member as ~ Cl- 1 : 750 = Skin antisepsis 1 : 500 = fincture 6) Cetylpyridinium chloride aka Ceeprin L-hexadecylpyridinium chloride NT used in lozenges , troches , mouthwashes for local action : most active among alky/pyridinium derivatives e) Chlorhexidine aka Hibiclens -Y ~ most active among biguanide antibacterials HNFY - yNH from Great Britain YNH preoperative skin disinfection wound irrigation Lused in I also available in mouthwashes , Y Nit W di 6) Miscellaneous 6a. Dyes Gentian violet Triphenylmethane - Basic fuchsin Thiazine-methylene blue Cationic dyes - for G+ bacteria a) Gentian violet aka Hexamethyl-p-rosaniline CI ↓ Green powder/flake crystal violet mea lineH w/ metallic sheen [1- Use sed ↓ for yeastto Nt as vaginal suppository topical for it · 1-3% ringworm yeast in I · oral solution for strongyloidiasis oxyuriasis (threadworm) N b) Basic Fuchsin mixture of the chlorides of rusaniline 3 prosaniline [1- I green crystalline with a metallic appearance HN NH2 powder soln aka Castellani's it ↳ component of Carbol-Fuchsin paint I CH3 "for ringworm & finea pedis NH2 2) Methylene Blue , USP aka Urised ↳ (dimethylamino) phenazathionium chloride 3 , 7. bis - ↓ weak antiseptic bacteriSTATIC , for cystitis 3 urethritis i ~ -colors the urine 3 stool blue green / 6b · Mercurials (Hg) MOA : enzume I inhibition ACTIONS: BacterioSTATIC via binding to SH (X) effective when taken internally TOXICITY: Tirritating ↓ (X) used inactivated by today proteins (t)Thio compounds TREA : such as Cysteine (x) effective , on spores Dimercaprol (BAL) a) Elemental Mercury ↳ for localized infx and syphilis b) Mercuric Chloride (Hg(12) aka Corrosive (Mercury (11) Chloride) sublimate antiseptic c) Mercurous Chloride (Hgz((z) aka Mineral (Mercury (1) Chloride Chancleon Calome d) Ammoniated Mercury (Hg(NH2) (1) ala White Precipitate L for skin conditions like psoriasis , impetigo , ringworm e) Mercuric Oxide (Hg) L treats inflammation of the eye f) Organomercurials ↳ can be one of two : · having I C-Hgbond does NOT = ionize readily having Hg-heteroatoms ionize=PARTIALLY or COMPLETELY 9) Mitromersal aka Metaphen CH3 I 23-hydroxymercury-4-nitro-o-creso ↓ the Na salt has an inner salt structure g is = in wi the inner shell electrons of Hy occupied are o non-irritating & non staining infx Lantiseptic for skin ocular I replaced by superior agents h) Thimerosal ,USP aka Merthiolate Nat 10'-S o La-carboxyphenyl (-thio) ethylmercury sodium salt - ~ weak barteriSTATIC Hg antiseptic ↳ topical ointment/soln ~ Replaced by Benzalkonium Chloride 6c. Preservatives prevent the growth of microbes I Ideal Characteristic : · Effective against all microbes non-toxic · compatible w/ other components in a preparation · has stable shelf-life a) P-hydroxybenzoic a (PARABENS) i OH Lanti-fungal low toxicity , rapidly hydrolyzes into active forms Of SAR : P action ↑ MW = where : Methyl = more effective against MOLDS ester effective against YEAST Propyl : more O 11 Examples g CH3 methy-p-hydroxybenzoate Methyl Paraben = Of  21 b) Chlorobutanol Cl-OH L 1.1 , 1-trichloro-2-methyl-2-propano Cl LbacteriSTATIC wI camphor-like odor c) Benzyl alcohol aka Phenyl Carbinol - found unesterified Phenyl methanol O Ol of jasmine in oil ↓ found in esterified acetic , cinnamic , 3 benzoica in gumbenzoin , storax resin , peru3 tolu balsam -used as preservative in vials of injections &most prominently in Bacti Stinjection ( a 1-4 % in H20 or saline ~ TOX12 in infants GASPING SYNDROME= 2) Phenylethyl alcohol is Sorbic I found oil , rose oil in orange OH ↓ 2 4-hexadienoic a , PERFUMERY & used in Lusually as Potassium sorb ate 2) Benzoic a g found II gumbenzoin perus to ↳ in , balsam QOH OH ~ more effective in foods I or and. products in low pharm put g f) Sodium benzoate II & used as preservative in acidic &y Nat Ot liquid preparations I where it releases benzoica ~ 1st FDA-approved food preservative 9) Sodium Propionate ONat antifungal preservative most effective at how ! I pH h) Phenylmercuric nitrate Qu - 0- ↓ used 1 : 10000 to 1: 50000 as - d to preserve injectables against bacteria Hg I ↳ Bacteriostatic ↑ : serum ⑧zog Belg  Antifungal Drugs treat fungal infx such ringworm candida cryptococcus · as : , , Cineal (Mycoses) TYPES CA DX superficial Malassezia furfur Pityriasis/tinea versicolor cutaneous Trichophyton Epidermophyton , Dermatophytosis ,Candidiasis of Microsporum Candida , the skin 3 oal membrane North Blasto., fungal Blastomyroses dermatitidis Blastomycosis systemic Pneumonia American - Coccidioides immitis Coccidioidomycosis-Valley fever Histoplasma Capsulatum bats fever but Mimic Histoplasmosis ~ , , Spelunkar's dy Paracoccidioides brasiliensis Paracoccidioidomycosis- Brazilian fever Sorth Ameri Blastoms Opportunistic Aspergillus sp - Aspergillosis Candida sp. Candidiasis minic Cryptococcus neoformons Cryptococcosis - lung CA Mucormycetes Zygomycosis Anti-fungal agents · Fatty a · Polyenes · Allylamines · Phenols · Azoles · Antibiotics 1) Fatty Acids (for dermatophytes Mus: Insertion & leakage into bilayer SAR: ↑MW Ivolatility * activity = = * Related to SEBUM natural antifungal : O a) Propionica 3 - Il Las Na or Casalt Ol L preservative 6) Na caprylate · 82 0 - Na ↳ from coconut/palm oil ' c) Zinc caprylate - 82 ↳ L topical fungicide ' In 3 Zinc adds astringent intersees ~ O Il d Linc propionate - 32 8 fungicide in adhesive tape O Il In 8 e) Undecylenic /Undecenoic a aka Decency/Cruex-112 I made by the destructive of castor HO distillation oil ↳ ↳ for diaper rash as Na undecylenate O f) Triacetin aka Glyceryl triacetate Enzactie , Fungacetic.. o' g O II L action is due to acetic a formation via esterase cleaving o L self-limiting as esterases are inactivated at pl 24 ! 9) Salicylica Of OH Lantiseptic Keratolytic (6% ) I ~ (t)benzoic Whitfield's : HO - (6%) ointment O in petrolatum 2) Phenols MOA : Protein precipitant 3 denaturant SAR ↑ @ PARA position activity (t) R X group : = or 'eg. CH3 Le g (I. a) Haloprogin , USP Cl G I : for superficial finea infx Cl Cl L photosensitive b) Ciclopirox Olamine o cutaneous Ol ~ louse ne a se wit = I -2ouse onchomycosis = ~ MOA depletes amino : a CI c) Clioquino I ,- ~ substitute for jodo form · for atpic dermatitis 3) Nucleoside Antifungals MOA : Insertion Flucytosine/5-fluorocytosine aka Ancobon NHz Lorally active 2 prone to resistance , Veryerrow spectrum F for Candida systemic fluoro cytosine ~ e g.. · Cryptococrus (t) Amphotericin = Cryptococcal meningitis (t> Itraconazole : chromoblastomycosis - prodig inactive (X) protein 4 FUMP > RNA- synthesis deamina Fu - 5 7. & bind to (x) DNA ? FdUMP -( > - active thymidylate synthesis Synthetase produces thymine 4) Polyenes -major components) wall false membrane MOA : Bind Ergosterol T cellular leakage = to = components SAR Contains NLT2 double and a lactone too : bonds 2 Groups (Based Groups based # of double bonds on # of C) on 26 membered Natamycin (Pimaricin) - Natamycin Pentaene = Nystatin Hexaene = 38 membered Amphotericin B 3 Nystatin - Amphotericin B Heptaene = ↓ broad spectrum but are not preferred · toxicity ↓ chemical stability LHz 1 · for systemic use , due to : 9) Amphotericin (Fungizone) B ↓ from Streptomyces Modosus a Lamphoteric = most effective systemicfungal especially ~ in a agent immuni PY ~ administered IV comp. as A/E phlebitis : hemolytic = leaches cholesterol nephrotoxicity activity from RBC chills b) Nystatin (Mycostatin) L Aglycone mystatinolide = ~ for Candida not readily absorbed Preparations Ointment , cream = cutaneous mucocutaneous powder Vaginal tablets = Vaginaldidiasis Tablets 3 troches = Oral /61 candidiasis (t) Tetracycline = prevents moniliagrowth caused by tetracycline therapy  2) Naturyan (Pimaricin ( - smallest polyene ↓ from Strep Natalensis. - Lamphoteric & for superficial intx of eye 5) Griserfulvin MOA : interferes mitotic spindle activity binds fomicrotubules & from Penicillium griseofluum ↓ for systemic of finea that are treatment and dermato refractory -phytes ↓oral absorption : ↑ fatty meals ↓ deposited to skin to prevent re-infx squaler > Imosted - - > egostro > - fragh - cell wall 6) Allylamines MOA : Squalene epoxidase inhibitor SAR VN atom : Unaphthalene Vally T & Cidal = dermatophytes L Static = yeast Cl a) Nattifine (Naftin) N L as 1 % topical cream/yel for fines F (Lamisil) b) Terbinafine 2 Las 1 % cream for finea N ~↑ potent I than Nattifine may be used orally  Aftate, NP 2 =) 2) Tolnaftate (Tinactie - , E Las 1% aerosol 1% cream 1 % powder 1 soln L cidal in action ↓ a thioester of B naphthol in ty ~ (t) fingernails to prevent 7) Azoles MOA : Lanoster) 14a demethylase inhibitor plasma is < 10 %,↑ penetration FLO, M binding Cerebrospinal fluid L(X) hepatic metabolism I ~ (x) affected bya food F weakly basic @ amine moiety 3 lipophilic @benzene 6) Echinocanadius & Pneumocanadius ↳ natural products relatively new L non-competitive 1 3-beta-d-glucan synthase MOA : , inhibitor of ↳ L - fungin forms stabilizing glucan polymers in cell wall 9) Aureobasidin A & cyclic depsipeptide & from fermentation of Arreobasidin pullulan ~ MOA : noncompetitive of inositol phosphorylceramiea Synthase & for spingolipid biosynthesis Episerie Beg Es  Synthetic vs Antibiotics Antibacterials ↓ I - - I 1) Quinolones (-oxacin) · Nalidixic · Sparfloxacin · Norfloxacin · Comefloxacin · Cinoxacin · Oxofloxacin · Lerofloxacin 1, 4-dihydro-1-0x0 3-pyridine COOH - MUA (-) DNA/Topoisomers : e Rij go : (-) GABA Ro1 /- Cool receptors 113 SAR : Reno B : T potency QLT Mpolarity ( ) meth : R1 = + cyclopropyl eth Pe ins : calky/3 ary1) (x) R2= () substitution otherwise : activity UTI , for C33(y (-) substitution = polyvalent : (t) Chelatesw/ cations Ri = (t) X , OH NH2 , , methoxy ↳ 2/1 wI Ee * ↓ phototoxicity. Sparfloxacin e g. Antacids : (x) anaerobes R = (t) F = fluoroquinolone ↑Spectrum : RE = ( ) + Piperazine = A basic : ↑ crystalluria a) Nalidixic (Negbam Wintomylon) , [MI L for GC) not for Pseudomonas R8 = (t) X , alkyl, methoxy , ~ its 7-hydroxy is active metabolite Lphototoxicity e.. g Comefloxacin A)E : · QT prolongation. Bitter/metallic · Rash/pruritus taste · Hepatotoxicity.Tendon rupture or Phototoxicity chondrotoxicity Earthropathy ↓ photosensitivity 8) #7 why, ↑ Quinolie 9) TIF Antavid : effect , 2) Prototype 11) MOA = (2) T/F : Quin = ↑ polar 13) T/F = Quin = 6 (t) 14) Quinolines are usually used for what dy is) Brid gen 2) Nitrofurans ~ derivatives of 5-nitro-2-furaldehyde SAR activity : = nitro & C5 A/E : carcinogenicity mutagenicity a) Nitrofurazone ~ ((+ ) (-) broad spectrum but not fungi 20 2 %. soln ointments, supp. , 1) Furazolidone L 3'[5-nitrofurylidenelamino]-2-oxazolodinone ~ anti-bacterial & antiprotozoal i e.. Giardia lamblic 1) aldehyde dehydrogenase 2) Nitrofurantoin & disrupts bacterial enzymes LG(t)(-) L common for UTI , but colors brown the urine ~ available in large crystalline ↑61 = form tolerance 3) Methenamine&its salts L Urothropin Uritone , active ~ ~ Y hydrolyzed into NHy formaldehyde ~ requires acidifying e.. g NH4Cl , Na biphosphate agent L used as urinary antiseptic ~ crease - > urea > - NHy-basic = alkalosis,indigestion (t) Acetohydroxamic a (Lithostat) a) Methenamine mandelate furnishes its own acidity hamount of mandelic disturbances L a is enovyn  2) Methenamine hippurati readily - absorbed orally & concentrated in urinam bladder 4) Phenazopyridine H21 colors urineOrange t L A20 brick red color = = & local analgesic effect ; given in combination L (t) Sulfisoxazole (A20-Gantrisin) 5) Anti-tubercular Agents CA : Mycobacterium = acid-fast resistant alkali alcohols = tuberculosis aerobic to , unusual cell wall 2/1 % lipid a) Isonicotinic hydrazide/Isoniazid (INH) ↓ Cidal = replicating ~ static = non-replicating ~ MOA = () mycolic a synthesis 2 activemetabolite : N-acety lisoniazid ~ undergoes Acetylation ~ A/E : peripheralritis(t) Pyridoxine (Vit Bul. : seizures : hepatotoxic b) Ethionamide ~ for th resistant to INH > MOA C-) mycolic a : c Pyrazinamide (PLA) (pyrazinecarboxamide ~ Prodrug converted to pyrazinoic via pyrazinamidase T & MOA : interfere wh uric a excretion L AlE porphyria alteration of : = heme production d) Ethambotol -only active against dividing mycobacteria not given alone ~ Dextro 16x active) meso arabinoscrase > MOA : () LA/E Retrobulbar : neuritis : Green-red color blindness e) p- Aminosalicylic a ↓ not effective de to resistance > MOA : St folic a synthesis f) Clofazamine LA20 red = ~ for leprosy-resistant to Dapsone ↓ for ulcers by M vicerons. 9) Ritampin/Rifampicin -from Streptomyces mediterranei L MOA : (-) DNA-dependent RNA polymerase & most active agent far TB LAlE hepatotoxicity : Lextensive enterohepatic recycling I must be given on empty stomach enzyme inducer L Lorange to red brown powder h) Rifabutin Linferior to Ritampin due to ↓ plasma % i) Cycloserine ~ from Strep Orchidaces as Dextroisomer L Racemic form is more potent ↓ in cholic form , analogorsto D-alanine L MOA: C) cell wall synthesis j) Capreomycin combination of 4 cyclic where la 3 16 polypeptides are dominant ~ from Strep Capreolus · L MOA: -) peptide protein synthesis inhibitor (70s) C.) cell wall synthesis ↓ AlE ototoxicity : , renal dysfunction k) Streptomycin ↓ from Strep grisers - -given IM ↓ not given : ↑ resistance alone ↳ MOA (-) protein : (12s) synthesis sensitization L AlE : = wear dermatitis glores POP QUIZ 1) Arabinosyltransferace inhibitor 2) Methenamine requires environment 3) Nitroform for Giardiasis D AlE Ethambrtol 5) Antidote for IN 9) Korte of Steptomy in E) Inhib · of DNA dependit RNA poly meuse 8) Active agent of Methenamine 9) color of 120 10) Sorce of caproomyin 1) Anti-leprosy +cntiTB 12) Mycolic in inhib. a) Sulfonamides-Pontusil - p- Aminobenzoic CPABA) MOA : () Dihydropteroate - (x) DNA DHDS 1 ( Sulfonamida Synthase dihydrofolic (DHDS) DHERI) Trimethoprim SAR : tetrahydrofolic T QLT : "basic AlE crystalleria : ↓ DiVA Purines - > /absorbed in Ionized forne a) Sulfamethazine L soluble ina urine b) Sulfapyridine se ~ Trisk for Kidog dney-acetylsufapyridin ~ 1st drug effective for pneumonia 2) Sulfamethoxazole & related to sulfsoxazole (+ ) Trimethoprim Cotrimoxazole L = Pneumocystis ~ DOC for carinii d Sulfacetamide Na ↓ topical can be repeated A solubility due to (Na salt) , e) Sulfisoxazole Diolamine acute otitis ↓ (t) Erythromycin = f) Triple Sulfa & Sulfabenzamide Sulfacetamide , , Sulfathiazole Vaginal cream for H Naginitis ↳ - 9) Mafenide acetate 3 true sulfanilamide;for Clostridium welchii non-absorbable ↳ not a - AOL : burns n) Silver sulfadiazine ↳ for Pseudomonas Spp - i) Sulfusalazine (+ ) S ↳ broken down into m-aminusalicylic a ↳ sulfapyridine AE : for intestinal Ulcerative SJS 3 for reduction of bowel ~ e. g. Steuer ohnson infx colitis flora Syndrome 7) Dihydrofolate Reductase inhibitors a) Trimethoprim ~ MOA : ↓ (t) Sulfamethoxazole- Cotrimoxazole (synergistic) 6) Sulfones ↓ L effective than sulfonamides ↓ have cross-resistance a) Dapsone ↳ for dermatitis , leprosy/Hansen's dy - AlE : hemolytic anemia in those w/G6PD deficiency 9) Antiprotozoal agent a) Metronidazole & for acuted carrier 67) , anaerobic cocci stages , L DOC for TAG (trichomoniasis , amoebiasis , giardiasis) LDOC for Clostridium colitis defficile & has Disulfiram-like effects available as powder for reconstitution (96hr) b) Diloxanide Lesters: eutamide d furamide (non polar = ↑activity for asymptomatic of E histolytica & giardia ~. carriers cysts ↓ for invasives extraintefina (not given as sig a requires hydrolysis to function ~ c) Todoquino (Yodoxin Diodoquin Diquinol) , , ↓ local/ contact mobicide a ~ AlE optic neuritis 3 peripheral neuritis : d) Emetine alkaloid from Ipecacuanha ↓ for severe amebiasis balantidiasis flukes , L used in combination e) Pentamidine isethionate (RebuPent Pentam 300) , ~ DOC for prophylaxis of P Carinii. -alternative for Suramin for African , Kala-azar babesiosis , sleeping sickness ~ A/E HTN : when given rapidly f) Atoraquone ~* lipophilic 3H20 soluble for P Carinii , T gondi ↳.. Land line for mild-moderate P carinii. 9) Eflornithine & MOA: C) Ornithine decarboxylase ↓ for African sleeping dx mening o encephalic stage , of T brucei - ↳ seizures in 8% h) Nifurtimox 1) Na stibogluconate only agent for To cruzi 2DOC for leishmaniasis -pentavalent antimonial compound i) Benznidazole nitro imidazole for Chaya's dy 1) Suramin Na ~ AlE peripheral : b bone marrow LMW bisurea w/ 6 sulfonic a neuropathy suppression 2 for ex & prophylaxis of trypano somiasis j) Melarsoprol - for meningoencephalic " +- gambiens/rhodonsience - ~ DOC for late stage African trypanosomiasis L prepared via pentavalent arsanilate reduction 10) Anthelmintic BOTOX () X : a) Piperazine citrate ↳ for pinworms roundworm MOA (-) ACk flaccid ↓ : = rx paralysis b) Diethylcarbamazine citrate L DOC for Bancrofti's filariasis' Onchocersiasis ~ A/E pruritus & facial edema : ) Pyrantel Pamoate & DOC for ascariasis enterobasis hookworm , , -MOA: depolarizing spastic neuromuscular blocker = paralysis d) Thiabendazole ↳ for strongyloides , toxocariasis , larva migrans uncicariasis ascariasis fungi , , ~ anti-inflam-3 analgesic pyretic LAlE : NV SJS shock tinnitus , , (Stevens-Johnson) syndrome > MOA : -) helminth fumarate reductase e) Mebendazole (Vermox) against most intestinal nematodes ↳ active ~ MOA L glucose uptake : f) Albendazole ↳ for Taenia solium 3 Echinococcus granulosus 2 abs : fatty meal g) Niclosamide L preferred for Thenia sp. < requires Saline purge after use  h) Bithionol chlorinated bis-phenol ~ DOC for Fasciolopsis sp. i) Oxamniquine (Vansi ~ for Schistosoma mansoni taken food w/ j) Praziquantel ↳ for Schistosoma Clonurchis sinensis k) Ivermectin ~ for reterinary practice @tidose nematodes Barthopods