VOU Ube lI IIIa \ \ VIMVMIYS Medicinal isfy se @ Phan 6 Semestar Unit - 1 = Anlibiotics + * Grbroduebion of ardibiobics + The ferm antibicbic £3 deatved | fom fylo word | > Anki and bystics ambi anears Fo Kill ard Liabicg enoars | tackoua: > fh means any chemical) arobecule a Medicine whih ve | awed fo Kill Hhe bacleta Js called antibiokics » Pai + Bigtics b kill achat: > pnbibiotics ace prefaced fom Phe Killed and Attn hackera for Kinting He Shoge backeda: 7 the foot bacleta aas trobabed and sepiched by fhe gcierish Luies pashoc In \874- * They docrversd Phe Penfbier facletia info Phe plan: + kn 192g the Gros scientish Alexendo firming alas descoued the gical anbibinbice Renieibine uthich is obtained fram She penicillum mafehim in Hu plarl of Tabacco* Chosactoosts f Antibiotics > Mi He rrebebaltc product f the backria which is oblained fom the filled and Aiperuated bacleuag Mero- cagonisin: > Hb dynblebic product prohiced by sbuchwal analogue © al the necfurcally occuserg antibodies: . > pntibibe ace He synthebic Hhey ace propared with He teolh of taclerca in She Sab e + GE is the omega? fo growth of Ae swerival are f He v0re APecles 4 the amicao osganis7 + = > Aatibiolic axe ayjed fo Kill ox sufproyed Hue grout Ther haclertia cs Micsougaugm: > of ais used in uecy Dow concentrations-ar affected in Jou concenbyahion + 2 pty ubich we ased fo Kiel alt Aippe 4 Sachetia Guam +e of ~VeE Hey ace called tyoad gheckuan * fhey wee wed arly a spectre foclerta + Classiftcabon of ambibiabics > LY) Aecoading the spechnrm actly. av Accordg Jo He Mechanism f acho: 2D Aecealtg b the demoed Auchoc Xx RQRQRQG Va pp pa pPAP RPP PPR PP PPP? Fsoe UU TUF UNO kee dd eh a ee A) Broad spockrm anbibiobics - beara evompir Tefracyel ine 8 Remout speckarm /relibistios: priitin- 6 Sheplemyem Eayttrornychn ° Bacifractn Nystatin (2) precording fo Ihe anechaniam of acbin: C19 Ibarkih coh salt aynthesis er icisena Ceffalasparins Cyclosoame Vanomycm Baci#yacin Ui) abit Rakein agothesis Tebracycline a a on, jco| Exttre em ctendendgcin ("9 Causes Leakage from cell enemboare + > causes Laokoge farm Cell meminare or puypeph ies (b) folyencs Polgmyping esneh iad Bacifaacin Nash Colishin fayeOY) Cause cian 4 MRNA code ard affect penneabilchy < Amminapyembees £ baruycln G lamnyctn Nesmycin 2 drdbibit DNA Gyrase Engyrne Prooguirolores — ciprofloxacm os - soon [et Phawrecy | ow) gatodee with DNA Fumolson Reform Mebonidazsle wit) utith DNA Synthesis ~ Acyl Zindgvudme wits Interfere with arderemedeafarcy anehabohism onorides ones Parco Premtno Salicylic Acid etarbrbol odnefhomine Fatnedhopoim . (8) According fo Be Chemical ghuchwee - DANS i) P- Lackan Anbibiobies = Ry ioillins —_—— Ce hextasparen. #- Lackemase Morobactoms . Ci OPPPPPLCROCPEPPEPE PPR ITIUTALLLLAARATSURO UU Ooo eet \ ql \ Q PHGVIGY (9 Paaumnoglyeo3 ides Sbepfomycin Genkamyetn Neounycrn i. Konannycin Ket Phoara mw Tehacyelme = Onyfefrocyeline Doxycycline civ) Nébobenzene denivabive> sss a Chibsomphenical wy Buerolones and Flwogueralmes + 4 Noefloxocm Nabideric Add: cifsoflox actn Offoxacm ee (vid Mocrafides | Aciftomyoin { cm E rarer (pre) cit) guopfonamides vefoked cauge + Subfadio2me Subfamefoxazale Sulfones ( Dafsme) : faa amibnapalicyc lic Acid (As) wil) Piminopyrémidine - RycmeHamene ( Phypephide Pnitibiabtes > Biyanyxin Colistin Bacifracm ee 00 ClycopepBide % VanonycinOD Riyene Anbibintics = OD Oxacbinediroes = Zineztide («iD Nebofurean henivabive nif furxantamn Frocazabidine WD ibn ne ntl Temidazale ek OV) $midazale/Azoledenrabive {Qucsnecole Kplacomaze le Clafsiaezale Tlécnazale ete- OWED Nicobintc Acid deniatives qymwazid Lysagiramide VI other anbshialicg — Gruizeofubum Linc Viarnycin- Vamamuychn BALA APAAAA AMP APR APPPPPFIVFULTIFVRWIAAAAY£9 Locka Aenbthiaos + 7 Sud pobtbiclics mutch covdain She B- Laclam 207g 7 thon stnichure Shey axe cabled §- tackim anbtbikics - > AM) & Loclem anbibiokic anfain 4 anerbered f lactam mung whuch is fused Hough nitrogen and Sebrahedsal anthn alan fo gecond fyexocyclic reg - 2 Fray conta fowe membered tehocyelic ong tn athich the nifroyen Js fckroal is pocesent ard fuse subfor confaming sug JS present TAN es S08 a ua COOH >On the basis f Phere exompl — 1 fenwstn (ii) CephaLosfasums Gi). Huenamycm (9 clavvlanic Acid - 1) Piniciglns= B- Lackam scing is fused awith driorobidine surg (1) Cobhale sharers = P-tactam suing is fued with difydoathicaine eee yee e eee ee { y \ | (iin Friemomycin: = B- Lackor seerg £8 fused viith Pyridine scing ee IUUU US | | | 0 Clawdanic Acid = B- Lackam srg J fused autirth axazabidine it= Fenicibling & " i ae > Tn 1929 Scienfigt Alexender: flemming alas discouerd fhe Ps foest onbtbiabios Peneistin’ which is obfamed fm Hu @ peniciblrurm anafehrm tn He plimb 4 Tabacco e > fericillint cern be cauideed 03 améro deoivabiucr 4 = & prmeropeniciblonic acid (6APA) = eat iy ) 2 Coy ° 6-Pemins Penicillante Acid R net Hs a 4 re be ee Fe (romana) © ee INO > Tun engarmes fericiblinase [P- lactamase and Arnidase erage anglababise the penicillin 80 hoy Srbubtf the anode of ~ actim 4 penicilm: . é > Basically Penricilterase a P-Lactamase Js actondhe site fo & actin of - and pratdase LS ach one site action f 11» Chemisty 4 Perudlin + iH SH CHE R a8 Se < ae li —2>co0H » Renkeiflin P2222 22 AADRADee ? Fhe penicillin shucluw is He seven membered earparrd uthich antain fuo fuse otiy ? One 4 A) ard one J (BY. 7 AAS Tiidzabidine sing ard (8) 88 Locka xing > UY cornfams amide group at the pssibion aro Six: > gf confains Kefore scing at Fhe posibian mo Zeven > 4 ontaiws dd MeHuyl gaarh ab the position ro 3 (Huee). 2 GF confains Ahe carborylic aeid group ab He posibian n0Aub 2 Degradation 4 fenicillin + : Rel-Phewmecy coy R. NH: “é oh 4) CoO) 2 fenicillin i acid J HF Base jor Ma Peniciblenic Hy halysis ; Acylace Acid Hao feéc| etc j iT IL Cofening of Ptackim schng) fenamaldic Peroblic Acid ‘Acid Cs R ; aoe i Sr Pat oH ee cs He -_ CH3 + 7 obs Fenadic Acid door "ah Fenicitleatdchyde Remilloic Acid SUSEUSVTTU abred Prodiolss Acid + fenebloic Acid Base + Enger = re Ns RnicilbicAad Prnicibloatdetyde Clas sificabion Bend a sy Cg mys ae et 2. CooH feucilln C General Shucwe ) 1) Penic Mimase Susceptible Penicitline ». _ Poug - i r R | Renievllm- & Boy og Rentciin 7 Cod a 3 Perefficillin =| Tia 4 Perwcillinase Resizhant Renicillins Cpe “4 Meffacillin S Nakici m greener \ ape Na R= wi 4: Kel. Phasmacy ge reoane Teseerd toned termed bnceneeh tecaicd Waited eee \ | % APPRPELP PLPC PPP POP r TIT LT§sek UUs bd ddd ddd ddt © Oracitim R= Ro=H @ Cloyacillin Riz, Rezcl ® Dicloyaciflin R= &-cl (D Fleyecittin R= F f=c/ 3 Amino Renicilfins = tr Ro Ri fo. Arnpiciblm axed =4 ae Ri | I Aamonyetttin De | 0H KCL Phamac| v Carebony Pen iciblins os aie 7 | _R Ri fa Carchenicillm os -H | oak °° Grdemylcarcencillin — 5- Inderal an ee 5) Wide feniciblms + i) Wade jeer Ry ae HX) 14 Azbdblm Sn =H 18 Mezlecillm —SogcHg©) Miscebloneous > 10 Bumacwim mM) Azidaciblin 18) Talrmbeillin Y) Teoaxcillm : Sar of Reniciblins (Stuctwe Achiuidy Relationship ) Cr JH Ra ime . Oo B A = ‘oH J A)- Thiazolidine Ring B- B-Lactam Rh D- Benzyl, Sobsliled ace or hohescaryl group > 6 APA (6- Arnénopenicillane Acid ) 44 the mamerum shuchue' seopixement fue onbihackewal Ackrally: HN re CHy ° APA EPPA > Fe P-Laclamaxt af 6-APA Shruchute ace extential far 2 Takes Hei wruchue fon Heir antimicrobial activity quill be decvease [ret Pharmac} OPTI Kr KRrgae AAPP Par PP 222 aa ra ren0009sk eee ee eb sd dd ddd > AL He - pation d oe ai mata ta Withdranwers gop: then Meir anki anicsobtal ackrusty wll Le Increase > When cry bulky qaoup is ablach ob Phe 'R’ foaition Phen duc to sheacte fmdromnce B- Lacknrase er can't diziociate Me penicillin 20 Helse ability ail! be encrease > uhen ane add any polar group at the acefyl gaan Hun fhe gam negabrue ackruity Jz sreyease ard qpam-we actiuty is decyedse > pst mahural penicillirs ote deta sah abing utuch are ackhue compamd: Pode of Action f Penédllin = Kel Pharmac 2 ferucilirn setubit acleertal cellatall farmrabicn : * Calan defo is endl uc ets a lh > fepbidoglyomn 18 a componedt of cobt auall and if prowde seigid enechorical shobibily 44 urtue she Aighly cussed Liked Satbice wark shuchuce > Backsicidal in achion:* Cefplasparan i" ee a p-Laclam dattiotic decease St conlat ® Lackam #8 Lackam sing is fruied auith détydiabhiaring 204 Ry na oN ° [3 Ja oO coon = Classification z > Cabhaloshoan8 arte classified dnbo + different qooubs defending upan i12 generation system - 1) Hina Genexabion Cefalosp US 5 yahgy aclrusageinih guam ive tacleta and Sauer ackrutty against gram -ve tacieda: a Masrby achtue agains Machococei 4 Staphylococe! 2) Secard Genexobian Cofalesforint = 7 Troy axe amose ache = agonssf gm -ve Baceaia Shan 43 gereovcalin cephalospardnd eg > Bucs higher ackrubly againbh travmoftuls imfluerzac x ) ind Gonorabin Cfphesfexins ty haus road spits % 4 antibacterial acbrly + emg acktue agatnat amiades sesittint to 4% ard gr generation cefalospararns PPPP PIII ONDA M ON DM ERMA RED & & e&© Foncth Gererabin? 5 Ger abemlags canien hat CefaSozpaims - Ghenled spechum of ochiuily. » moeased sfoblly fram amid and Charmasormally reds fie P- Lachamase engyine > wed an Phe beokment f smfection due 45 aerable gm -ve pacitlt, scesistant 34 gretallan cepbalosparces (1) Fis} Genoration @falospootrs — Ry —CH,0C0CH3 = CHy0CaCH3 ey - Hg ~ CHyO. coc Hy — CHa fp is similar to penicillin > Cpbalosfrtru jnbitut Lacletial cell wall frmation > Gllwall & bacterta 44 exsertlad fut Hot momma growth and deuclofanent e Pepbidogeycan 43 a Combments 4 Cl wall and J} pooutde suged mechanical shablily by werue 4 3 fughby cv083 triked tathice auack sfruchute- = Bachesacidal m actin: > Infubile engymme - teansfephidase that range aboub cross Deve Ahchueen sth ghycme abvea exusteng dogbyem mn ok & 4h par f reuly ibe oe side effect? 0 Hypeconibritly Like aaftuplonis, shomiatha Oxganufocyfopenia , haematytre anaemia + 2) Loca jvoctfabion 3) Renal Toxicity . 4) Puulforam pike offect ez > Wepul fac anermingilts aching againks mentees ~~ prearmoceccl, H. trfuenga & Enferic gm-Ve baciblt- > Cephalexm — Used fax ure > Cefacly — Infeclion caged by H- grpluenzde . > Cophalathin sodtum - Register 4o penicillinase produced by ¢. rvs = Cofotaxime + Used fax ameningls gruenm cerbros imal fouid- = Afbizxime Sdnim ~ Used far emenirgtHis -Uke kbd dd ddddddié rTehaeylren [FEE Mare] * Becausedlis embibiahic ambiins fave cyclic sings 6 on He basis f thets shurchow Meir name ig Jeksacyelipesxting * He atl foure cycles ace ochahydromaphfacené Necleus » * This antibiotics 18 devtued from Hu Sheplamycese backeria: Secies (hy fermenfablor) ° * The tefacycline ankthiolic can fam Fhe salt with fhe seaclio with acid and Late x Foy carn alo wack with Hre some melats A! tq Co4 Fe a they fom the chelitte complex » Hus clas £ anbibiohios tdue Hnce diffesert Ayes f antbiokics Tehacysere, Ch lorkeFracyclint, xyfebsacyclme auich ae desvckued from the aclinomyeekos 4acterta - * grill only duo antibihics wa available fenicillin shreletomych Jhon all He disease 4 conbyalled by Hhese tun antrbiobes « + bub offer the diseruoy 4 febracyclin Hey axce quidely ged wa ont jokic : * Huy ae wor sable antibiotic x Ard if ues discrumeed by the scterdis} BM. Duggax in gta. 9° Prd He ne) Sehaoycline aniebiobics orylelacycline 43 discovered by the scientis (Ac Finlay) in (90> this antibiobic is dexoarad from Shreplomiyces afrrosus - cheriood Rohured Tehaagclines? oxy alghbty soluble freaky > Poser onrfrfafertic > Ave Sabuble nr solubiors of afkalt hycvoxides and cobmates Grd dilwhe salts.Fresabeutic Wes 2 Nery populase fase Lous dose cual and 2 Commrumichy acqputyed wonany rach snfecttans > opbhalavic nfechans > Upper sespiratary foact snfechios ele as Classification . > AU of He Hsacyelines fave fhe asic atrachuee shou telouwt « Name _& Re 1 Tehacycline -H - CH 2 chiovtehacycline -cl -CHy 3 Onybefeacy cline -H - cr D Pemeclocycline -el —H 3) Mefhacyel ne -H 6) Pocycyclme -H —H ~vpimocy cline NCO), oH Pe BA2AAPAPPPAAAPPADRAAARMRARAARARaAdDen_he ee eo ddd dd ddddl oe + Mechanism a Action = >The main aecharus debian df Hehacyelin 4s bind ath Hogas Subtmit of Ae Rdogore 2 Ard they stop HerRNA AL the site f an-RNAto She poten synthesis is shop tnside the bachertia and -backetio earns dead - gas Tebacy cline Airbibiotic: — m- RHA Sos sulurit Whee: RNA Block —~ loan SmPhesis hp uv Paclercia dead: Cotes ta AU ai) CH, City > Fhe fowe cyclic sfruchuce esserbial dare the acliuity if use change Herre Struchowe Like ncrease Loma bef cycle Hen Hheixt achwthy quill Le decreasee& ? The basic nucleus U polycyclic dckohydio, Nathacene, Grboramnd. atuch confaines Jang A,B,C: 0. avd essential far He activity > The Helo enol Lomasiem ab the avthon mo 4yand He Gutbsr ex % 3 18 good fut She ambitaclerial acknuly- E > when we add any cheriicad quoup ad the posibion mo 5x Hien Het acdfuily will be decrease’ a when ure we areHulation of He cortbor 0 Six Hhen She carcbon banding will be incsease > then ate add any (carbon) gap ab He position ma Seven Shen Preise patency ail be trcreare and anhibacteial actiuity ull he mroveare oe the presence & shang acid Hf we dehydrate acyctne 2 position no sik Phen If corund jrfo Fhe omyfetvacycline qe and Hho raw compard and «urbich 14 amare parrerful 2 A cla hype f fusion b/ut sarg A4B wttth x-oH goaup is qos ay foe He sclertion 4 actrutly - tenos arte Faw water soluble decovahies uttich am 9 PONTVAHHPUVHH HS 2 Tefracye be ouoccare by aminoatkyfation at Caxbmamide gasp ustrg mannich seacn liad : fine, bymecye ex. Rotiferacye| ao i a pect )o Kel Phomrac P<) fo : xxl if < CoN Ry oH @ OH O RD? g PPpPpPprraps Ppp ” vaSU kU e ld dd dd ddddl £ Arnhroglycasides + > The crme Armiroglyco sides 18 dewochued foom Auuo wards Amina Rad Clycontds: beanuse rn Mis ankibiabics Auo aN, iB potent ard ae cormecled with the soaile Drag b Mode on ambragtycaa ide Anlth ioc. > Pantroglycoside Js obfained fom Fhe differerh type 4 afrelrm.ces backeaja > The DS 2-deoy sheptaming— In a ambnoglycoside except shrephorryeme avd defydrashrepromyct whore He song 18 > Bbrefatedime- 2 Gramble 4 Arriraglycosides : ) Shepfomycm 11) Nearnycin ait) cm iv) Amntkacm ) Tobaamycm wi) Gendamycm wil) Bigomycm wid ; icin (ix) Spectinomycinictc : KCL Phrowmacy > Posh wudely sed agaist quan —ve entoie ee combinakion arith vancomycin J penteiblen- = Sheptamycm ts She oldest aminoglycosides anbcbiatic- 7 ese drugs axce walec goktble stable in sordion and amare achive at afkabine pH Stan ab acidic pH’7 In i940 the Scienbiah Wwerksman fins} f all dé&coueel Hus tacleta-fim actinomyces Species > He scecesued a moble pai2e fx fas wark om Shyeplamycrn « © chemitfoy / Consbihdion: > Fhe base > stoePforycm the fas an embicdat fosernitle ae AIH sg N42 e "Molecule fos a Jattuydiochbaide authich sndicates He e 3-Auhogen afoms amuf be baste- >= Gite hop + BAL —> CaiHggNqOjo' SHC! — ( Shrebtomyem C Coyspablire} — tittdiebow ite en > TUld acidic srycrokysie cheories Sheftarmycin Infs 2- products C= qamely — Stachbidire CCoHeNe%) and Shefbebiosarune ~ (C13 Hag) « CaithgNy%2 +449 = —> CoHigNe + Cate ghOg (Sfoepbhmycrn ) (Soeptidine) — ( Shephobiosdmme ) 2 Srucwe f F Shucdwo F Sreplamyem + ha . ra well 2 LE Gre soe 43 diario icybheine ieee > Sheptidéne » a : Shebtbiosamune - AARP PPP PPP P PPP Pry:eke bdddddddddl 2 Classifications i ime NH; i) Shrepbnmny cin: ite by rae Ha a. i oH HOH Hy 8 NH - 1 Hl OH Ho ey 2) Kemamychns (Kanfrex) Eee eeec edeesefecaneetuascL H Ny NA, on 1H HO OH NA, 3) Genkimycin + Ha, _ NACH, naa ea Og by Hy pre cH, cHy NH fit, = sar f Amirogty cosites: gn the ammaplycostde ab Bail hug onine gaaub and ome ‘gee 4s essential) far He achuily. NHCH progr ion nm i? [ek Pheamacy |]é& >. centoal sing £3 2-diory adxebhamine sn abl ennivoghycaihe © exepaf Shebhomuyern a buch it sheplidine 2 Mode af actin $ (a 7 AF deat uo amine sugal is essendial foc dcbrubhy ° e& @e Staeptamychn— 2 amino sugar . a Kanawycm - 3-Amno Sugate = > ra glycoside pad f a aminoglycoside Ayo Lap: - Bbrusrchwees poesert « = A) Panirasugare portion ue e- B) Hexose sung: = | e e e e& > peqntroglycoside are ackesicidal 4n action « a bird auith tho sibssarreh Dp pation of 99S Ribssre= caret ay es NA: eal ayninogly ostide op the trartation process and rab tel pin styrdhesi aed by orang rey pookefn Frees ho coll enerrBriare_gemnipermedbiltty. TX pe PPpppp pp p Pp p f GAPSkee keel ddd dd ddddé > Brand antibiabic specha agarrst quai quam tve and gram ve boctertia: > Shrephayein= rst commanly used fre treahment 4 Subercculosis: - Specbinomyctn- Fay Aeatment f goranrhoea: Cherractorabtc f /rntroglycosides Ankh iabies rea eee eh ae steel ce ae mes > Foashty absorbed from GIT + Poor penefrabion am crs > Gxcseled Hough adney > Faap sezistrnce developed Side offect= > Mpduce Nebaatoricity- Mode ef Acdion t ee > Elective against gm -ve baclercia « > drhibils polein synthesis - > Grfeotforss uth stborvclic acid amefabatlem > Mirceadry of cade sm m- RNA Jemplae Wes® ws ° Plaque si ? Moning itis > Bacteria: