antibiotics summary by lajneh muststudy!!

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{,. - tS -*of ffLd-*r ,pq*' ffr***trffffi{e The &Iost Irnp ortant teeftxres - Notes t +-E ffir - t. EHS I rl

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Successful antimicrobial therapy occurs when an effective concentration of drug is delivered to the site of infection for a sufficient period of time. Minimum effective concentrations are those needed to inhibit growth (bacteriostatic concentration, MIC) or kill (bacteriocidal concentration, MBC) the pathogen in question.

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  • ' I fuwut, tfiis materin[ is not easy, a fot of drugs d a fot of information ; tsurfufiat I reaffy annt you to furoot dr' concentrate on ; is ufiat t saif aAout : rfi{Is$'tEqy r^v{poKI%A(I dl ZLEASE U@EKL rNE "Irfi s . . .,

    Dfr" !{nkaffi A[-Hanili . . .

    Dear colleagues ,As we all noticed , Dr. Hakam repeated that information a lot during his lectures, So,we decided to collect these * IMPORTANT INFORMATION ' and put them in thissummary !! -

    >> BUT please , note that this summary is USELESS without studying the lectures andunderstanding the whole concept.

    >> And please, note that the points in this sunmary are taken from OUR LECTURESand from OUR O1VN NOTES and from a summary done by our colleague in the 6,hyear ( Ruba Abu-HarfiIe ).

    >> SO, It is a STUDENTS'WORK from STUDENTS' SCOURCES , BLII we rried ourbest to make sure that this summary conrains (ALMOST) all IMpoRTANTinformation and is free of any mistakes ; but as we all know , nobody is perfect , Soplease , cooperate with us , and if you find any rnistakes in the summary or realize thatthere is an important information we forgot to include , please, inform us at :

  • s*q.y't gid{y't it 6*f

    '' VERY IMPORTANT...''lN Pharma Lectures...

    Done By :Shifa Summarizing group

    * n--:::l l:- /i^ ^a^^--l \o' rel, tc rlt rf , { ll I Htrl Isl dt r;e Bactericidat ." lnhibits ce[[ watl synthesis ." NOT effective against B-l,artarhase producing microbes.e ln case of renat faiture ) Dose must be reduced.e Absorption is nearty comptete parentatty BUT lM is irritant -

    *" Adverse EffeEEs :

    >> Allergy :Tvpg5_of allerev :A - lmmediate * Anapfuytaetie shoek !Treatment :

    . Potent airway ( By opening the mouth then giving oxygen )" Epinephrine ( lV or SC , EUT NOT lM+vasoconstrictor)" Hydrocortisone" Antihistamine

    ts - Acceleratede- Late rGctiora

    Penicillin Sensitivitv Test :B Give low concentration of penicittin intradermaty in one hand (Using insorime syringe).E lnject the other hand with distitted water.E Wait 1-2 min .

    "oR:E One or tow drops of penicittin in the eye .>> lf there is attergy ) Eye watering and the eye witt start itching .

    @@ Natural penicillin :

    * Benzvl Penicillin ( Penicillin G )o Drug of choice in :1- Streptococcus pneumonia ( Typicat pneumonia ), B-Haemolytic streptococci.2- Meningitis caused by Neisseria meningitidis.

  • ** By adding PROCAINE :>> Procainepenicitlin ) longer hatf life ( Detay the absorbance ).* Phenoxvmethvlpenicillin ( Penicillin V )

    . Administered oratty .o Used in mitd infections ( ) ln atl types of tonsittitis )

    " Benzathine Penicillin :Used in Depot preparations .

    . Used as a prophytactic drug in case of recurrent tonsittitis to prevent rheumatic fever .

    @@ Semi svnthetic :** fl-Lactamase Resistant:

    . Used against B-lactamase producing Staph. Aureus .

    **Extended Spectrum penicillin :* Amino penicillin :>> Ampicillln e nmoxicittin

    o Broad-spectrum.e Destroyed by lJ -tactamase enzyme .c Used in salmonetta infections .e Adverse effect * Diarrhea ,rash .Drug of choice in :1- Meningitis caused by l-l-inftuenza.2- Pregnant lady with pneumonia .

    >> Auementin ( Amoxicillin + Calvulanic acid)o NOT destroyed by B -tactamase enzyme.

    *cMines:" lnjectabte / Orat preparations

    * 3 rd Generatisn Cephalgsporines :o Active against gram -ve microorganisms .. Weii distributed>> Cross BBB & enters CNS + Used in meningitis caused by H-inftuenza.>> Cross the bones.) Used in osteomytitis .>> Cross the placenta.a Excreted by the kidneys ) Dose must be redriced in renat failure .

    * Ceftriax.r:ne & Cefoperazone :c Excreted in the bite ) coutd be given in renal failure .

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  • Adverse effects :1- Cross Attergy with Penicittin .2- Fal,se + ve glucose test in urine3- Disutphiram like reactions if taken with atcohol ) severe abdominat pain , headache

    &, vomiting

    Aminoqlvcosides:. NOT given oratty. ln patients with kidney impairment :) 1- Decrease the dose or 2- Give the doze at longer intervats.. They are highty concentrated in the inner ear and in the renal cortex.. Used against aerobic gram -ve microbes.o They have narrow therapeutic index.

    Adverse effects:1. Aototoxicity:

    r Auditory: tinnitus ) deafness.o Vestibutar: headache, dizziness, Ataxia

    2. Nephrotoxicity ) inabitity to concentrate urine. [Reversibte (doSe dependent)]3, Neurotoxicity (muscte paratysis)) apnea(inabitity to breath).4. Atlergic reaction ) haemotytic anemia .

    ,, (We can minimize the adverse effects by monitoring ptasma concentration )NOTE : Penicillins , cephalosporines & Aminoglicosides can cause Haemolytic anemia !!

    Preparations :- Streptomycin , Gentamycin , I Amikacin & Nitilmicin (broad-spectrum)] .- Neomycin :>> Coutd be given ORALLY or TOPICALLY .>> Prophytactic for Hepatic coma .

    lllacrolide Antibiotics :

    * Ervthromvcin:Enteric coated tabtets.

    . Does cross the ptacenta ) Not given during pregnancy E breastfeeding.

    . lt is metabotized by the [iver &. excreted in the bite.) Bimodat Distribution)1- stow metabotizers 2-rapid metabotizers

    3- Normat metabolizers ) (geneticatty determined)) lnter-individuat variations & inter-ethnic variations

    o lnhibitor of cyt p- 450 enzyme system

    Uses:. Diphtheria. Chtamydiatinfections. Atypical pneumonia caused by Mycoptasma pneumonia. Legionettosis ( caused by tegionetta pneumoniae )

  • . Prophytaxis: prior to dental protedures (with amoxicittin ] )to prevent SBE (Sub-acute BacteriaI Endocarditis)

    r Atternative to penicitlin in patient attergic to peniciltin.Adverse effects:

    1-Liver toxicity: acute chotestatic hepatitis (reversibte)>> Manifested by ) nausea, vomiting, jaundice.

    2-Ototoxicity.* Clarithromvcin :

    . Much better absorbed & distributed ) inctuding CNS." Lincomvcin & Clindamvcin:

    . Very effective against anaerobic gram( -ve or + ve ) bacteria (becteroid fragitis).. Very effective against staphytococcus Aureus.o Do penetrate bones ) used in osteomyetitis.. Can cause pseudomembranous cotitis.'

    Clindamycin ) Used in acne vutgaris with vitamin A.

    * ehbramphenicol :o Very active against anaerobic infections inctuding Bacteroid fragitis .e Metabotized in the liver by conjugation with gtucuronic acid or by reduction .* Decrease the dose in patien.ts with tiver faiture.

    Uses:1- ln Satmonetta infections . (typhoid fever)2- ln severe Rickettsial infections .3- ln bacteriat meningitis caused by H-inftuenzae.

    Adverse effects :'l- Bone marrow suppression :

    e Reversible erythroid suppression of bone marrow-.-'e lrreversible AplE$lg rnsrnl!

    /- Gray baby syndrome ..# lnhibitor of Cyt p-450 enzyme comp[ex ( interfere with other drugs'metabolism )

    Tetracvclines :" Broad-spectrum activity" Absorption is IMPAIRED by :- Mitk , Anticids , tron preparations

    *

    . G Wett distributed , inctuding CNS ..u Concentrated in thb liver & excreted in the bite ( given in renal faiture)

    U,ses :

    " Atypical pneumonia .e Chlamydial infections 8. Rickettsial infections .6 Acne vulgaris .

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  • Adverse reactions :1- GIT upset2- Permanent Brown discotoration of teeth .* They are contraindicated in young peopte.3- Do cross the ptacenta) They are contraindicated in pregnant tadies .4- Phototoxicity ( Doxycyclin )5- Vestibutar Ototoxicity ( lilinocyclin )6- Btack hairy tongue .

    Fluroauinolones : '. Broad-spectrum activity.. Wet[ absorbed oratty+ BUT absorption is impaired by antacids &. iron preparation.

    ' . Poorty enters CNS ." Used in atypical pneumonia

    Adverse effects :1- CNS side effects ( dizziness , headache )- NOT recommended in pregnancy.

    * Ciprofloxacine :Uses :

    1- UTI infections ( gonorrhea )2- GIT infections ( satmonetta &. shegetta )3- Respiratory infections4- ln osteomytitis .

    Sutfonamides & Trimethoprim :) They interfere with Folic Acid synthesis .

    u Sulfonamides enter the rxn in place of PABA .. Trimethoprim Inhibits DHF reductase in bacteria ." Both are bacteriostatic .

    " Sulfasalazine :" Poorly absorbed oratty.. Used in utcerative colitis ( inftammatory bowe[ disease )

    Adverse effect i1- Crystatl,uria (crystattized in the urinary tract )

    * Trimethoprim l. Given oratty or parenta[ty .. Used in UTI , Proastitis ft vaginatitis .

    " Co:Tr inloxqZo_lg_;. Bactericida[ .

    .- e- Wet[ absorbed & wetl distributed; including CNS .t

  • Uses :1- UTI . (E-coti , proteus , ktebsetta )2- Chest infections3- Pneumocysits carinii in patients with AIDS .4- Satmonetta & shegetta infections5- Chemoprophitaxis of UTI in women

    Adverse Effects:1 - Megatoptastic anemia( ) Fotic acid deficiency or Vitamin 812 deficiency .)

    Anti-Protozoal Drues :

    * Metronidazole : (flagyl)o Active against anaerobic microorganisms .) Used in empirical therapy" Broad-spectrum activity .o Given in renal faiture , BUT NOT in liver faiture () Decrease the dose ). Can cause disutphiram like effects when taken with atcohol .

    Adverse effects :1- Meta[tic taste in the mouth .2- Cotors the urine into red-broyrnish color .3- GIT upset.4- Dryness for the mouth & vagina .Uses :

    . ln giardiasis & amibiasis .

    . ln Bacteroid fragitis infections (anaerobic bacteria ).. Prgvention of post-surgical abdominai and pelvic infeciions ( after bowets'surgery ). ln treatment of peptic utcer caused by Heticobacter pytori .

    . ln treatment of utcerative gingivitis .n ln non-specific urithritis & vaginititis .

    Treatment of Tuberculosis (TBr :. Always use combination of drugs .) To prevent resistant .. Used to give streptomycin lM for 2 months .

    2 staees of therapv :1- initial phase:) Minimum 3 drugs* lsoniazid & Rifampin & other drugs .2-Continuation phase : ') Minimum 2 drugs.+ lsoniazid & Rifampin

  • " lsoniazid :. The most active drug in treatment of TB. lt inhibits the synthesis of mycotic acids. lt crosses BBB and enters to CNS.o Metabotized in liver by acetytation) Bimodal distribution1- slow acerylators 2- rapid acetylators

    Adverse effects :1- Peripheral neuritis ( peripheral neuropathy )) We give Pyridoxine (vitamin 86) with it.2- Liver impairment ) jaundice.) You shoutd atways do Liver Function Test ( LFT ), before & during therapy .* Rifampin :

    . Broad-spectrum activity ( against g+ & g- ). lt induces the cytochrome p-450 enzyme system) lt reduces the hatf tife of many drugs. Most of it is excreted in the feces ) can be given in renal faiture .. Cotors att body ftuids with orange-red cotor .. Fixed combination with isoniazid.o Chemo prophylactic in case of meningitis caused by H-inftuenzae.

    * Ethambutol :. Affecting ONLY Mycobacterium tubercutosis .. NOT given atone ) ( ln combination with lsoniazid & Rifampin )) Because drug resistant wi[[ devetop rapidty

    Adverse effects :1- Optic neuritis ( lnflammation of optic nerve ) ( + diminished visual acuity )>> Visuat fietd witt be narrowed, Tunnel vision , Lackdiscrimination between RED/GREEN .2- Increases uric acid concentration .

    * Pyrazinamide :. Used in combination therapy .. Used in short coarse therapy of TB.. Used in the initiat phase

    Adverse effects :1- Jaundice . ) tiver function must be checked .2- Hyperuricemia .

    Anti-l,Aalaria Druqs :The Staqes:1-Hepatic stage :. c Drugs used:

    >> Primaquine, Proguanit, Pyrimethamine .2-Blood stage :

    . Drugs used :>> Chtoroquine , Quinine , Meftoquin, Pyrimethamine, Proguani[

  • 3-Sexua[ stage :o Drugs used:>> Quinine , Chtoroquine , Primaquine , Mefloquin .

    * Chloroquine :Uses :1- ln acute attacks .2- ln chemoprophylaxis in alt forms of plasmodium .

    Adverse effects :. Hemotytic anemia, particularty in peopl,e with G-6-PDD (Gtucose-6-Phoshphate

    Dehydrogenase Deficiency )r Ototoxicity * irreversibte loss of hearing .. Cardiac arrhythmias (abnormat ECG )" Retinopathy ( irreversibte ).

    * Primaquine :. Atways shoutd be combined with btood schizonticide+ lt affects tissue stage &. sexual stages .Adverse effects :1-Hemotytic anemia in peopte with G-6-PDD .

    * Pvrimethamine & Proguanil :. lnhibit DHFR enzyme .(DiHydroFotate Reductase ). When combined with Sutfunamide ) synergistic effect.Fansidar >, Pyrimethamine + sutfonadoxine .. For hepatic ft blood stages + NOT for sexual stageAdverse efiect:1 - Megatoptastic anemia.

    u Quinine :" Used in btood &. sexual stages ( But NOT in hepatic stage )) we give Primaquine with it .

    Adverse effects :1- Hemotytic anemia in peopte with G-6-PDD2- Cinchoniraty (cinchonism ) ) ototoxicity .3- Cardiac arrhythmias .4- Btackwater fever (DlC, Haemogtobinuria , Dark urine , Azotemia ,Renal Faiture)

    * A{etloquine :e ii is used mainty in prophyiaxis thei-apy .

    Adverse effects :1- Cardiac arrhythmias .

    !

  • Anti-Viral Drues :* Aqyclovir :. lnhibits viral DNA synthesis .e Distributes we[[ in our bodies. Does cross the ptacenta ft is secreted in the mitk ." Given TOPICALL\' ( NOT wett absorbed oi-atty )Adverse effects :

    1- CNS side effects .' 2-. Reversibte renal dysfunction .

    Uses :

    " Herpes Simptex Virus lnfections. (HSV)" Varicetta - Zoster Virus lnfections.

    * Ganeiclovir :, Inhibits virat DNA synthesis ." Low bioavailabitity .' Used against CytoMegaloVirus (CMV).

    Adverse effects :

    1- Myetosuppression ( neutropenia , thrombocytopeniaV" CNS side effects

    ).

    * Foscarnet :Adverse effects :

    ' Nephrqtoxicity & Hypocatcemia* Paresthesia (toss of sensation in the periphery) .Uses ;

    " CMV retinitis ." Acyctovir- resistant HSV infections

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    a* Trifluridine :

    " Broad spectrum .o Used in keratoconjuctivitis &, Keratitis in eyes due to HSV types 1 or 7.

    * ldoxuridine :

    . lt is topicat therapy ( straight in eyes ) for Herpes Keratitis -

    ) Without treating coutd lead to btindness.* Amantadine & Rimantadine :

    . Affects influenza - A virus BUT NOT type B .o Excreted in kidney ) kidney function must be checked .. Embryogenic & teratogenic ) NOT given in pregnancy .o NOT given in epiteptic peopte.

    * Ribavirin :. Broad spectrum of antivirat activity .. Given oratty or lV." Embryogenic & teratogen'ic ) NoT given in pregnancy .

    Adverse effect :

    1 - Hyperbitirubinaemia.

    Drugs used in AIDS :* Zidovunadine :

    " Used against HIV 1 e.2.. Distributed very welt ) enters the CNS .

    Adverse effects :

    1- Bone marrow suppression (granutocytopenia & anemia )2- Myopathy.

    - The "ffi.u.V

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