Fundamentals of Pharmacology for Veterinary Technicians Chapter 14 6PRRWKHQGRSODVPLF UHWLFXOXP 1XFOHROXV 0LWRFKRQGULD 1XFOHXV &HOORUSODVPD PHPEUDQH &HOOZDOO 9DFXROH /\VRVRPH 5LERVRPHV &\WRSODVP &HQWULROHV $*ROJLDSSDUDWXV &KURPRVRPHV 5RXJKHQGRSODVPLFUHWLFXOXP Figure 14-1A Copyright © 2011 Delmar, Cengage Learning Fundamentals of Pharmacology for Veterinary Technicians Chapter 14 1XFOHRLG '1$ 3LOXV 5LERVRPHV )ODJHOOXP &DSVXOH &HOOZDOO &HOOPHPEUDQH 3ODVPLG '1$ &\WRSODVP % Figure 14-1B Copyright © 2011 Delmar, Cengage Learning Fundamentals of Pharmacology for Veterinary Technicians Chapter 14 6WHS 3URFHGXUH 5HVXOW 3ULPDU\VWDLQ$SSO\FU\VWDO $OOEDFWHULDVWDLQSXUSOH YLROHWVWDLQ SXUSOH 5LQVHVOLGH 0RUGDQW$SSO\*UDP VLRGLQH $OOEDFWHULDUHPDLQSXUSOH 5LQVHVOLGH 'HFRORUL]H$SSO\DFLGDOFRKRORUDFHWRQH 3XUSOHVWDLQLVUHPRYHGIURP JUDPQHJDWLYHFHOOV 5LQVHVOLGH &RXQWHUVWDLQ$SSO\VDIUDQLQ *UDPQHJDWLYHFHOOVDSSHDU VWDLQ UHG SLQNUHGJUDPSRVLWLYHFHOOV DSSHDUSXUSOH 5LQVHVOLGH Figure 14-2 Copyright © 2011 Delmar, Cengage 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Figure 14-13A Copyright © 2011 Delmar, Cengage Learning Fundamentals of Pharmacology for Veterinary Technicians Chapter 14 Figure 14-13B Copyright © 2011 Delmar, Cengage Learning Fundamentals of Pharmacology for Veterinary Technicians Chapter 14 &KHPLFDOVWUXFWXUHRIVHOHFWGLVLQIHFWDQWV $ 3KHQROVDQGSKHQROLFV +2 2+ &, &, &, &, + & + &, 2+ +2 &, SKHQRO RUWKRSKHQ\OSKHQRO KH[DFKORURSKHQH % 4XDWHUQDU\DPPRQLXPFRPSRXQGV &+ 1 &+ /RQJK\GURFDUERQFKDLQ &+ EHQ]DONRQLXPFKORULGH & $OGHK\GHV 2&+ &+ &+ &+ &+2 &+2 JOXWDUDOGHK\GH IRUPDOGHK\GH ' (WK\OHQHR[LGH ( $OFRKROV &+ 2 &+ &+ 2+ &+ 2+ &+ &+ HWK\ODOFRKRO &+ HWK\OHQHR[LGH LVRSURS\ODOFRKRO ) +DORJHQV 2 2 ² 1D >2&,@ +& 1 , VRGLXPK\SRFKORULWH SRYLGRQHLRGLQH * %LJXDQLGH &, 1+&1+&1+ &+ 1+&1+&1+ &, 1+ 1+ 1+ 1+ FKORUKH[LGLQH + 2[LGL]LQJDJHQWV 2 + 2+ 2 + 2 +&2 SHUDFHWLFDFLG K\GURJHQSHUR[LGH Figure 14-14 Copyright © 2011 Delmar, Cengage Learning Fundamentals of Pharmacology for Veterinary Technicians Chapter 14 Table 14-1 Mechanisms of Action of Antibiotic Drugs Action Effect Drug Examples Inhibition of cell wall Bactericidal effect by inhibition of an enzyme penicillins, cephalosporins, bacitracin, synthesis vancomycin, carbapenems, monobactams, aminocoumarins Alteration in cell membrane Bacteriostatic or bactericidal effect; as the polymyxin B permeability membrane permeability is increased, the loss of cellular substances causes cell lysis Inhibition of protein Bacteriostatic or bactericidal effects due to aminoglycosides, tetracyclines, interference interference with bacterial protein synthesis, chloramphenicol, fl orfenicol, macrolides, but not animal cell protein synthesis or lincomycins, aminocoumarins, diterpines inhibition of the steps of protein synthesis Interference with metabolism Bacteriostatic effects due to the deprivation of sulfonamides essential material for bacterial metabolism Nucleic acid impairmentBactericidal effects due to inhibition of nucleic quinolones, fl uoroquinolones acid enzymes Table 14-1 Copyright © 2011 Delmar, Cengage Learning Fundamentals of Pharmacology for Veterinary Technicians Chapter 14 Table 14-2 Classes of Antibiotics and Their Effectiveness Class of Action of Considerations Examples Antibiotic Antibiotic penicillins • Inhibit cell wall synthesis • Oral and injectable forms • penicillin V (V-Cillin K®), penicillin G • Bactericidal • Given orally, most procaine (Crystacillin®), penicillin G • Mainly work on gram+ absorption occurs in benzathine with penicillin G procaine bacteria; some gram– with stomach and small intestine (Dual Pen®) amoxicillin, ampicillin, • Rapidly distributed • amoxicillin (Amoxi-tabs®, Amoxi-drops®, ticarcillin, and carbenicillin • Give 1–2 hours before Biomox®, Robamox-V®) • Carbenicillin, ticarcillin, and eating • ampicillin (Polyfl ex®, Omnipen®) piperacillin are effective • ampicillin with sulbactam (Unasyn®) against Pseudomonas • amoxicillin with clavulinic acid bacteria (Clavamox®) • ticarcillin (Ticar®) • carbenicillin (Pyopen®, Geocillin®) • cloxacillin (Dari-Clox®, Orbenin-DC®) • dicloxicillin (Dynapen®, Pathocil®) • oxacillin (Add-Vantage®) • piperacillin (Pipracil®) • piperacillin with tazobactam (Zosyn®) • ticarcillin with clavulanate (Timentin®) • hetacillin (Hetacin-K®) • nafcillin (Nafcil®) cephalosporins • Inhibit cell wall synthesis • Oral and injectable forms • First generation: cephapirin (Cefa-Dri®, • Bactericidal • GI absorption not good; Cefa-lak®), cefadroxil (Cefa-drops®, Cefa- • First generation mainly usually administered tabs®), cefazolin (Kefzol®), cephalexin work on gram+ bacteria, parenterally (Kefl ex®) second through fourth • Well distributed to tissues, • Second generation: cefoxitin (Mefoxin®), generation work on gram+ except CNS cefaclor (Ceclor®), cefotetan (Cefotan®), and gram– bacteria with • Vomiting and diarrhea may cefuroxime (Ceftin®) fourth generation having occur when given on empty • Third generation: ceftiofur (Naxcel®, the broadest spectrum stomach Spectramast®, Excenel®), cefovecin (including Pseudomonas) • If animal is allergic to (Convenia®), cefoperazone (Cefobid®), • Can cross placenta penicillin, it may be allergic cefotaxine (Claforan®), cefpodoxine to cephalosporin (Simplicef®), ceftriaxone (Rocephin®) • Fourth generation: cefepime (Maxipime®) polypeptides • Inhibit either cell wall or • Absorption is poor; used for • polymyxcin B (found in Optiprime® cell membrane synthesis topical infections or wound ophthalmic ointment) • Bactericidal lavage • bacitracin (found in Mycitracin® and Trioptic® ophthalmic ointment) glycopeptides • Inhibit cell wall synthesis • Treats drug-resistant • vancomycin (Vancocin®) • Bactericidal Staphylococcus spp • Injectable form used in veterinary medicine (Continued ) Table 14-2 Copyright © 2011 Delmar, Cengage Learning Fundamentals of Pharmacology for Veterinary Technicians Chapter 14 Class of Action of ConsiderationsExamples Antibiotic Antibiotic carbapenems • Inhibit cell wall synthesis • Injectable form only • imipenem-cilastatin (Primaxin®) • Bactericidal • Broadest spectrum • meropenem (Merrem®) beta-lactam antibiotic • Used to treat resistant bacteria monobactams • Inhibit cell wall synthesis • Injectable form only • aztreonam (Azactam®) • Bactericidal • Gram-negative spectrum of activity aminoglycosides • Inhibit protein • Injectable form only (except • gentamicin (Gentocin®, Garacin®) synthesis[en] neomycin which is topical) • neomycin (Biosol®, Mycifradin®) • Bactericidal (concentration • Not absorbed readily from • amikacin (Amiglyde-V®, Amikin®) dependent) GI tract; usually given • tobramycin (Nebcin®) • Work