Abtics by Dr San

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Abtics by Dr San

  1. 1. Dr STSA
  2. 2. Antibiotics - chemical substances originally produced by various species of micro-organisms (bacteria, fungi, actinomycetes) that in high dilution suppress the growth or cause death of other microorganismsObjective of Rx- For curative - eradication by lethal effect,inhibit growth & multiplication,phagocytosis For preventive
  3. 3. Bacteria Antimicrobial agents 3
  4. 4. Bacteriostatic• inhibiting the growth or multiplication of bacteriaBactericidal• lethal effect on mature bacteria /kill the bacteriaAntibacterial spectrum• list of bacteria which are normally susceptible to antibacterial action of a particular agent (group or particular organisms)
  5. 5. Antimicrobial agents 5
  6. 6. Antimicrobial agents 6
  7. 7. C Antimicrobial agents 7
  8. 8. Classification based on their Mechanism of Actions1. Drugs that inhibit the synthesis of bacterial cell walls eg.Penicillins, Cephalosporins, Vancomycin Clotrimazole2. Agents that act directly on the cell membrane eg‘.Nystatin, Amphotericin Antimicrobial agents 8
  9. 9. Cont-3. Drugs inhibiting microbial protein synthesis by their effect on bacterial ribosomes(A) disrupt the function of 30S or 50S ribosomal subunits to reversibly inhibit protein synthesis (mainly bacteriostatic) eg – Chloramphenicol, Tetracyclines, Macrolides, Clindamycin, Lincomycins(B) agents that bind irreversibly to 30s ribosomal subunit (mainly bactericidal) – Aminoglycosides eg. Gentamicin Antimicrobial agents 9
  10. 10. 4. Drugs that affect nucleic acid metabolism eg.Rifampicin,Fluoroquinolones,Griseofulvin Metronidazole5. The antimetabolites - Drugs affecting the intermediary metabolism which are essential to micro-organisms Sulfonamides Competitive antagonist of Para-aminosalicylic acid PABA (PAS) Trimethoprim inhibit DHFA-reductase enzyme Pyrimethamine
  11. 11. • MOA -inhibit the bact:cell wall syn by binding to protein,inhibit crosslinking enz ∆ autolysis
  12. 12. Classification of Penicillins1. Penicillin G - Benzyl penicillins(a) Penicillin G- Crystalline I.V (Aqueous Pen G as K+ salt and Na+ salt) (2,50000 to 10,00000 units IM, IV)(b) Penicillin G -Procaine suspension (3,00000 to 6,00000 units IM)(c) Penicillin G -Benzathine suspension (0.6 to 1.2 mega units IM)2. Penicillins V (oral) Phenoxymethyl penicillin(250-500mg)3. Penicillinase-resistant penicillins (Anti-staph) Cloxacillin – orally,IM, IV Flucloxacillin Dicloxacillin, Oxacillin Antimicrobial agents 12
  13. 13. • Methicillin - use as a laboratory tool for identification of methicillin - resistant - Staphylococcus aureus (MRSA)(MRSA = resistance to all the penicillinase-resistant penicillins and cephalosporins) (Vancomycin is a drug of choice in MRSA)4. Broad spectrum penicillins Ampicillin Amoxicillin5. Antipseudomonal penicillins Carboxypenicillins - Carbenicillin Indanyl (oral), Ticarcillin Ureidopenicillins - Piperacillin6. Penicillin β-lactamase inhibitor combination Co-amoxiclav (Amoxicillin + clavulanic acid)
  14. 14. Pen GOrganisms Usage Dosage/Route gram(+)ve cocci Infections caused by Crystalline- IV(except penicillanase -non-β-lactamase- 30 mg/kg6Hproducing )staph producing staphylococci, (1mg=1667u) -pneumococci -pneumococci Severe inf:50 mg/kg 6H (max 2G)12 H/6H-Streptococci -Streptococcal pneumo: Procaine-IM 25-50 mg/kg 12H/OD - Prophylatic Tx:* (Max 1.2-2.4G) Benzathine –IMgram (-) cocci - meningococci, 25mg/kg OD,3-4wkly- meningococci, gonococcigonococcinon-β-lactamase- non-β-lactamase-producing anaerobes producing anaerobes
  15. 15. Organisms Usage Dosage/Routegram (+) bacilli – Diphtheria C/pen 30-50mg/kg 6H C. diphtheriae, Infection due to B. anthracis, Bacillus anthracis Clostridium, Clostridium species Actinomyces -Actinomyces* and other gram-positive rodsspirochetes Treponema pallidum C/pen “ (syphilis) and many other spirochetes Prophylatic Tx
  16. 16. Pen VOrganisms Usage Dosage/Route•gram (+)ve cocci o minor infections oral(except penicillinase (streptococcal pha- 15 mg/kg 6H (125-producing ryngitis) 250mg)staphylococci)* narrow antibacterial o prophylaxis of 12.5 mg/kg 12 Hspectrum streptococcal infection following rheumatic fever and pneumococcal infection (following splenectomy) fusospirochetel infection (gingivostomatitis)
  17. 17. Pen resistent penOrg Usage Dosagemore effective against staphylococcal Cloxacillin – orally,IM, IVpenicillinase producing infections-skin,LRIT 15 mg/kg 6H 12H,4-6H, 25- 50mg/kg- staphylococci Flucloxacillin 12.5-25 mg/kg 6H 25-50 mg/kg 8H,6Hless effective than pen. Gand pen. V against Grampositive bacteriaSome strains of Gram H. influenzae, E. coli,negative bacteria gonococci, Klebsiella
  18. 18. Aminopenicillins (Ampicillin, Amoxicillin)Org Usage Dosagegram (-)ve, (+)ve bacteria URTI (sinusitis, otitis Oral/I.M/I.V(H. influenza, E.coli and Proteus media, acute 10-25 mg/kg 6H /8Hmirabilis) exacerbations of severe -50mg/kg chronic bronchitis & epiglottitis) Lower RTI, UTI, Biliary tract‴Listeria monocytogen Meningitis, Salmonella infection (Enteric fever) H. pylorisensitive against Penicillin - β-lactamaseβ-lactamase producing inhibitor combinationstrains of G (+)ve & G (–)vebacteria*.Staph,Gono, (Clavulanic acid orH. influenzae, E coli, Klebsiella, Sulbactam)Proteus, 20-25 mg/kg IM,IV 6H Bacteroides fragalis, Moraxellacatarrhalis
  19. 19. Vancomycin Antimicrobial agents 19
  20. 20. Red man syndromeAntimicrobial agents 20
  21. 21. Mechanism of Action• similar to penicillin , bactericidal, inhibit bacterial cell wall synthesis Classification of Cephalosporins I. The first generation cephalosporins Cefalexin Cefadroxil Cefazolin II. The secondgeneration cephalosporins Cefuroxime axetil ,Cefaclor (Oral) Cefuroxime Cefoxitin IV,IM• Cefotetan
  22. 22. III. Third generation Cefixime(oral) Cefotaxime Ceftriaxone IV,IM CeftazidimeIV. Fourth generation Cefepime (I.V)
  23. 23. The First Gen:CephaloDrug Theraputic advantage DosageGram- positive cocci upper and lower RTI Cefalexin- 7.5mg/kg 6h(except MRSA) Cefadroxil 15-25mg/kg 12h CefazolinGram-negative bacteria urinary tract infectionEcoli,Kleb,Proteus surgical prophylaxisOral cavity anaerobiccoccisome β lactamase skin and soft tissueproducing strains infections owing to (e.g, Staphylococcus) S. aureus and S. pyogens
  24. 24. The second gen:cephaloGram + ve RTI (oral) Cefuroxime axetil 10- 15 mg/kg bd Cefaclor 15mg/kg 8hanaerobes (Bacteroids anaerobic infection Cefuroxime ivfragilis) -pelvic inflammatory 25-50 mg/kg 8,12,6 hr disease, -Intra-abdominal inf, - diabetic footGram-ve bacteria G (-)ve bacterial(< 3rdG)(Neisseria,H.influenzae,Enterobacter Proteus,E.coli, Klebsiella)
  25. 25. The third gen:cephaloless active against G + ve DOC for serious Cefotaxime iv infn 25-50mg/kg-12 h (Septicaemia,Pneu 8 h/6 h monia,Meningitis) Ceftriaxone -iv,im 25-50mg/kg 12h,8h Oral-Cefixime 5mg/kg od Cefpodoxime ″ bdmore active against G -ve Enteric fever Severe Lyme’s d/s Gonococcalmuch more activeenterobacteriaceae &β-lactamase producingstrainss/a (H. influenzae &Neisseria)some - active against P.aerug Ceftaxidime iv,im 15-25mg/kg 8h
  26. 26. The forth generation• Cefepime (I.M ,IV) 25-50 mg/kg 12h
  27. 27. Antimicrobial agents 27
  28. 28. Untoward Effects1. Hypersensitivity is most common cross hypersensitivity & resistant < 10% Caution – Penicillin allergic patient2. Nephrotoxicity - ↑ with aminoglcosides3. Renal tubular necrosis (Cephaloridine, Cephalothin)4. Intolerance to alcohol (disulfiram –like reaction) Antimicrobial agents 28
  29. 29. MACROLIDEAntibacterial Activity Therapeutic Uses DosageG +ve (same as Pen G) alternative to penicillins in Erythromycin strep pharyngitis, Oral 10-15mg/kg 6h staph infections, tetanus, syphilis, 25 mg/kg 6h Bacterial endocarditis , Rheumatic fever Diphtheria, Pertussis,Chlamydia trachomatis, Chlamydial infections,Mycoplasma, Mycoplasma p’nia,Legionella, Legionnaires’ disease Campylobacter infectionsluminal amoebicide Intestinal amoebiasis
  30. 30. Mycobacterium Mycobacterial infection Azithromycin 15mg/kg D1 7.5mg/kg D2-5more potent than Eradication of H.pylori Chlarithromycinerythromycin in peptic ulcerstrept, staph,ChlamydiaMycoplsma andH.pylori
  31. 31. Untoward Effects- not common• cholestatic hepatitis is common with erythromycin estolate (esp. in pregnancy)• allergy, GI disturbances, arrhythmia*• reversible hearing lossContraindication• liver disease, pregnancyDrug InteractionErythromycin and clarithromycin inhibit CYP3A4potentiate the effects of digoxin, theophylline & valproate
  32. 32. LINCOSAMINES (Lincomycin and Clindamycin)Antibacterial Activity Therapeutic Uses DosageAnaerobic bacteria peritonitis, Lincomycin(Bacteroides species, pelvic inflammation 10mg/kg 8h oralClostridium) IM or IV (over 1h) 10 -20mg/kg (over 2h)6h Gram +ve bacteria – Bony infections Clindamycinmore effective - osteomyelitis, 6mg/kg 6h oral(Staph. aureus) sinusitis, periosteitis, IV over 30min,IM 12h periodontitis 10 -20mg/kg 8h Aspiration pneumonia, Lung abscessGram - ve bacteriaLess effective
  33. 33. Untoward Effects of Lincosamines• Diarrhoea (superinfection)• Pseudomembranous colitis due to Clostridium difficile which produces enterotoxin(Tx –metronidazole)• Hypersensitivity (rare);• Granulocytopenia, thrombocytopenia,• Stevens -Johnson Syndrome (can occur, but not common)
  34. 34. Antibact Rx Dose& Routea wide range of G(+)& (-) IV 1g every 6 hours for 4Salmonella Enteric fever weeks in enteric feverShigella, Bacterial meningitis Chloramphenicol sodiumV . cholerae H.influenza, succinate (1g vial) I.M, I.VH.influenza N.meningitidisBordetella pertussis Strep. PneumoniaeBrucella, Rickettsia, Anaerobic infections Orally - Chloramphenicolanaerobic bacteria Rickettsial infection 25mg/kg/D (typhus fever, Q fever (250 - 500 mg) 6 - 8 hourly Brucellosisless effect onStaphylococcus Ophthalmic infection Eye drop- 2-6 H Ear Ear drop- 6H
  35. 35. Untoward Effectsless selective toxicity; may inhibit protein synthesis of mammalian tissues1. Haematological toxicity - bone marrow depression(a) true toxic reaction - dose related, common with prolong therapy or large dose - anaemia, leucopenia, thrombocytopenia(b) Idiosyncratic manifestation - not dose related (occurs in genetically susceptible patients) - aplastic anaemia --- can be fatal
  36. 36. 2. Grey (gray) syndrome (Gray baby Syndrome)• in premature and newborn infants• due to ineffective conjugation & poor renal excretion with dose above 50 mg/kg/day• dose should be limited to 50 mg/kg/day in full term infants and 25 mg/kg/day in premature infants3. Superinfection (oral or vaginal candidiasis) due to alteration of normal microbial flora4. Haemolysis in G6PD deficient patients (dose-related)
  37. 37. Antimicrobial spectrum Theraputic advantage Dosage Mainly active against Genta IV,IM Gram - ve bacteria UTI 7-8 mg/kg/D1,then(Pseudomonas, Shigella, G -ve bacillary infect: 5mg/kg 12H E.coli, Proteus, H.influ, Gonorrhoea Neonate5-7.5mg/kg/d Brucella, Klebsiella) Bowel sterilization 24H active against some Topical – Streptomycin IM 20- Gram +ve wounds,burns,dermatitis 30mg/kg (max:1G)OD Intestinal amoebiasis Amikacin IV,IM Mycobacteria TB Prem -15mg/kg/D(Streptomycin, Amikacin, D17.5mg/kg OD Netilmicin, Kanamycin) Term-15mg/kg/D OD Anaerobic bacteria are 1 wk to 10yr -15 mg/kg resistant to Netilmicin IV,IM aminoglycosides 1wk-10yr= 8mg/kg/D1 then 6mg/kgOD ,>10yr = 7 in D1 then 5mg/kg Neonate5 mg/kg/D OD
  38. 38. Unwanted effects1. Ototoxicity• irreversible results from progressive destruction of vestibular or cochlear sensory cells(a) Vestibular dysfunction (Gentamicin, Streptomycin, Netilmicin)(b) Auditory dysfunction – Kanamycin , Amikacin (potent diuretics potentiate ototoxicity) 2. Nephrotoxicity• due to accumulation of aminoglycosides in the proximal tubular cells3. Neuromuscular blockade (reversible)due to inhibition of prejunctional releaseof ACh(Aminoglycosides potentiate d-tubocurarine)4. Others• rare - hypersensitive reactions• vague feelings of paraesthesia of the lips or circumoral region• prolong use -- superinfection, diarrhoea, malabsorption can occur with neomycin
  39. 39. I. First Generation Quinolones• Nalidixic acidII. Second Generation Quinolones• Norfloxacin• CiprofloxacinIII. New fluoroquinolones• Gatifloxacin• Moxifloxacin
  40. 40. • MOA• Bactericidal• Block bact synthesis by inhibiting bact DNA gyrase and topoisomerase• Antibact spectrum-- E.coli,Salmonella,Shigella,Enterobacter,Campylo- bacter,Neisseria Pseudomonas(Ciprofloxacin) Staph( not MRSA) Strep,Chlamydia,Mycoplasma,Legionella,Mycobact
  41. 41. Clinical Uses of Fluoroquinolones1. Urinary tract infections (Norfloxacin)2. Prostatitis (Norfloxacin, Ciprofloxacin, Ofloxacin)3. Sexually transmitted diseases (Not for Treponema pallidum )4. Gastrointestinal & abdominal infections – Traveller’s diarrhoea – Shigellosis (Norfloxacin, Ciprofloxacin, Ofloxacin) – Enteric fever (Ciprofloxacin, Ofloxacin)5. Bone, Joint & soft tissue infections ( osteomyelitis caused by Staph &G-ve rods)6.Others M.avium complex (in AIDS) MDR TB7. Meningococcal Prophylaxis
  42. 42. • Dosage Ciprofloxacin- oral= 5-10 mg/kg 12H IV = 4-7 mg/kg 12 H Norflox = 10 mg/kg 12H Prophylaxis 15 mg/kg oral single
  43. 43. Side effectsGenerally well tolerated• nausea, abdominal discomfort, diarrhoea, headache, dizziness, allergy, photosensitivity• cartilaginous erosion in foetus and children (arthropathy) and tendonitis --- limited used in children age <14 years and pregnancy• Increse BUSE• Transient ↑ in Liver enzymes,Bilirubin• Disturbance in vision,taste and smell• Risk of haemolysis in G6PD def;
  44. 44. • Drug interaction- Cipro,Ofloxa ,Peflox inhibit the metabolism of Theophylline
  45. 45. • Bacteriostatic• Competitive inhibitor of dihydropteroate synthase which is responsible for the incorporation of PABA (para-aminobenzoic acid) which is essential for the formation of folic acid (pteroylglutamic acid)
  46. 46. Antibact spectrum Theraputic applicationG+ve and –ve except 1.Urinary tract infectionpseudo,proteus 2.Other Gram-positive and Gram-negative infections (in penicillin allergic patients)Chlamydia trachomatis Trachoma & conjunctivitisToxoplasma (Sulfacetamide) Ulcerative colitis - Sulfasalazine Local infections: Dermatitis – Sulfapyridine Burns - Sulfamylon, Silver SulfadiazinePneumocystis carinni Prophylaxis for HIV associated opportunistic infectionMalaria parasites Chloroquine resistant malaria (Pyrexine = Sulfadoxine + Pyrimethamine)
  47. 47. Untoward Effects1. Renal toxicity• a local reaction with short-acting sulfonamides (high doses)• may precipitate in the urine(obstruction,haematuria)2. Haemopoietic reactions Anaemia-haemolytic/aplastic,granulocytopenia H’lysis in G6PD def: Neonatal jaundice in new-born babies(especially in last trimester—Haemolytic jaundice) antimicrobial agents III 47
  48. 48. Untoward Effects3. Allergic reactions --- skin rashes, exfoliative dermatitis, photosensitivity --- more severe with long acting sulfonamides• Stevens-Johnson Syndrome- mucosal, dermal, genital and occular lesions; joint pain, high fever, oedema, ulcerations of the lips and tongue- erythema multiforme on skin of hands and thighs- severe urethritis and balanitis in males antimicrobial agents III 48
  49. 49. • Synergists of Sulfonamides1. Trimethoprim 80mg +  Sulfamethoxazole 400 mg
  50. 50. MOA of Cotrimoxazole• Sulfonamides are the competitive antagonist of PABA. They inhibit the incorporation of paraaminobenzoic acid(PABA) to folic acid.• Trimethoprim is a dihydrofolic acid reductase inhibitor. It prevents the reduction of dihydrofolate to tetrahydrofolate.• Inhibition of two consequent steps in the synthesis of DNA and RNA of bacteria when a sulfonamide and trimethoprim are used together.(Sequential Blockade)• Two bacteriostatic compounds act synergistically and become bactericidal
  51. 51. antimicrobial agents III 51
  52. 52. Antibacterial spectrum Rx uses DosageStreptococci, (1)Urinary tract TMP 1.5-3mg/kg 12HStaphylococci, infections IV ,OralNeisseria (2) Respiratory tract PCP Tx 250mg/m2 statE. coli, infections 150mg/m 2 8H (3) Gonococcal ProphylaxisSalmonella, Shigella, infections for UTI- 5 mg/kg oralEnterobacter Proteus, (4) Enteric fever PCP- 5mg/kg 3days/wkKlebsiella, Brucella, (5) MalariaChlamydia (CQ resistant falciparumexcept Pseudomonas malaria)aeruginosa (6) BrucellosisPneumocystis carinii (7) Pneumocystis carinii infection in AIDS PatientUntoward effects-Same as S’.Megaloblastic A with prolonged Rx
  53. 53. Cont - Synergists of S’2. Pyrimethamine also an inhibitor of DHFA reductase enzyme of malarial parasites andtoxoplasmaPyrexine (or) Fansidar = Sulfadoxine 500 mg + Pyrimethamine 25 mg Therapeutic Uses --- Malaria, Toxoplasmosis
  54. 54. 3. Tetracycline• in combination with sulfonamides produce synergistic effects because both are bacteriostatic drugs4. Penicillin:• although bactericidal, it produces a synergistic effect when used in combination with sulfonamides.
  55. 55. Drug Interactions with Sulfonamides• warfarin, sulphonylureas,diphenylhydantoin(1) potentiation of action of other drugs due to competition at plasma protein binding site (drug displacement interaction)(2) inhibition of metabolism antimicrobial agents III 55
  56. 56. Metronidazole (Nitroimidazole-antiprotozoal)• MOA- Effect on nucleic acid metabolism Potent antibacterial ,anaerobes , Bacteroides and Clostridium sp• Theraputic advantage• Anaerobic or mixed intraabdominal infection- Extraluminal amoebiasis - 30-50mg/kg/d oral- Amoebic liver abscess - 7.5to 30mg/kg iv 12H/8H x7-10 days- Trachomonal vaginitis- Clostridium defficile colitis- Brain abscess
  57. 57. • Side-effects- GI disturbance,metallic taste,peripheral neuropathy, seizures Interacting drugs- Alcohol- Warfarin  increase anticoagulant effect (enzyme inhibition)
  58. 58. TETRACYCLINES Broad spectrum bacterostaticAntimicrobial spectrum Tx - Infections with DosageGram+ ve and –veBacteriaRickettsiae,Mycoplasma, Rickettsia oral –Chlamydia Mycoplasma pneumonia 250-500 mg/ 6HSpirochetes Non-specific urethritis ( >8yrs) (Treponema, Leptospira, Trachoma,Syphilis,STD Eye ointment-Borrelia), Leptospirosis, Lymes apply 8HVibrio cholerae CholeraH.pylori Combination Tx GU/DUE.histolytica AmoebiasisMalaria parasites CQ resistant P.fless effect on Strep,Staph, PneunococciNot effective against –Pseudomonas,Proteus,Salmonella
  59. 59. Anti-TB Adverse effects1st line Peripheral neuroIN(A)H 10mg/kgoral od ( recommended-B6 20- 30mg/D ) TBM 15 -20mg/kg Hepatotoxicity,RashRifampincin* 10-15 mg/kg Hepatitis.nephritis,ITP 20-30mg/kg oralPZA Hepatitis,Interstitial nephritisEthambutol 25mg/kg oral Retrobulbar neuritis,yellow-Streptomycin 20-30 mg/kg IM green colour vision defect Ototoxic,Nephrotoxic2nd lineCapreomycin 20mg/kg oral OtotoxicityCycloserine 5-10mg/kg oral CNS toxicityEthionamide 15mg/kg oral HepatotoxicAzitho/clarithromycin
  60. 60. Bactericidal drugs- Penicillins- Cephalosporins-Other -lactam antibiotics- Aminoglycosides- Rifampicin- Fluoroquinolones- Cotrimoxazole- Metronidazole
  61. 61. Bacteriostatic drugs- Chloramphenicol- Tetracycline- Erythromycin- Clindamycin- Lincomycin- Sulphonamides
  62. 62. Broad-spectrum Antibiotics- Broad-spectrum penicillins (Aminopenicillins and Antipseudomonal penicillins)- Coamoxiclav- the second, third and fourth generationCephalosporins- Tetracyclines- Chloramphenicol- Rifampicin- Cotrimoxazole
  63. 63. Antipseudomonal Agents- Carbenicillin, Carbenicillin indanyl- Ticarcillin- Piperacillin- The third generation cephalosporins- The fourth generation cephalosporins- Amikacin, Netilmycin- Fluoroquinolones- Polymyxin - topical application for wounds
  64. 64. Anti-infective agents which can be used for Staphylococcus- Penicillinase resistant penicillins(Cloxa,Flucloxacillin)- AUGMENTIN (Coamoxiclav) (Amoxicillin + Clavulanic acid)- TIMENTIN (Ticarcillin + Clavulanic acid)- UNASYN (Ampicillin + Sulbactam)- ZOSYN (Piperacillin + Tazobactam)- Some first & second generation Cephalosporins- third & fourth generation Cephalosporins- Erythromycin- Vancomycin- Rifampicin- some fluoroquinolones
  65. 65. Anti-infective agents for anaerobic bacteria- Metronidazole- Lincomycin, Clindamycin- Chloramphenicol- Fluoroquinolones- the third & fourth generation cephalosporins
  66. 66. Empiric antimicrobial Rx (based on site of Infection)SOI Pathogens DOC AlternativeMeningitis Ampi+3rd Cepha Ampi(Cotri)+3rd Ce-Neonate (+Aminogly)-Child C/Pen C.Pen+ +Cefotaxime or Chloram CeftraxonePneumonia-Neonate Ampi+3rd Cepha-Younger child C/Pen Ampi -sulbactam Cefotaxime or Ceftraxone-Older child Macrolides Quinolines
  67. 67. SOI Pathogens DOC AlternativeIE Vancomy+Genta Pen-resistant acute pen+GentaSBE Pen G+ Genta Vanco+ GentaSeptic arthritis Ceftriaxone Ampi+SulbactamAcute OM,Sinusitis Amoxil Amoxil+Sulbact Cefuroxime TMP-SMZCellulitis Pen-resistant pen Vancomycin ClindamycinPeritonitis 3rd cephalo+Metro CarbapenemSepticemia 3rd cephalo+Vanco Antipseudo+Amino(Granulocytopenia) 3rd cepha/ceftazidimeSepsis d/t UTI 3rd cephalo±GentaSepsis d/t GIT 3rd cephalo +MetroNeo sepsis Early -- Ampi+Genta Late - Ampi+Genta+Clox/Van rd
  68. 68. STSA
  69. 69. Antiviral drugs1.Nucleoside Acyclovir* HSV1,2 Herpes-oral,genitalAnalogues* 20mg/kg iv VZV HS-Encephalitis(synthesis of DNA 100mgodx 5 d CMV Varicella(immu ↓)&RNA) Ginclovir EB CMV retinitis, Cidofovir HHV6 Pneumonitis Hepa C 2.Amantadine 100mg OD Influenza A,B Influenza A-H1N1Rimantadine 200mg OD H1N1,H1N2,(penetration of cell) H1N33.Foscanet CMV,VZV CMV retinitis in HIV p/t(DNA &RNAsyn:) HSV(Aciclovir20mg/kg iv over 30’ resist)
  70. 70. 4.Immunomodulator Hepatitis B &C Chronic hepatitis BInterferon α HPV &C(inhibit the transcription) CGDPlavizumab RSV RSV Bronchiolitis5.Ribavarin RSV RSV Bronchiolitis(aerosol-20mg/ml 12- Pn’ia18hrly)(oral5-50mg)6.Neuraminidase Influenza A & B Influenza A & BInhibitors(release of virus)Zanamivir/Oseltamivir
  71. 71. 7.Antiretroviral HIV Side effectsNRTI-competative inhibit:activated i/c by A,neutropenia,myopathyphosphorylationZidovudine(2mg/kg) Pancreatitis,Periph neuro,DDidanosine(ddI ) Peri neuro,pancreatitis,rashDideoxycytidine(ddC) Peri neuro,A,LipoatrophyStavudine(d4T) Headche,N,abdo painLamivudine(3TC) Hepa BAdefovirNNRTI-inhibit viral HIVreplication by direct binding to RTNevaripine Rash,Steven syn,Hepatitis120mg/m2 daily oral
  72. 72. Protease Inhibitors-Interfere with post-translationalprocessing of HIV Asymptomatic hyper bili-precursor proteins rubinemia,GI disturbanceEg.Ritonavir Skin,hair changes IndinavirDose-500mg/m2 8H oral
  73. 73. Major adverse effects1. Nephrotoxicity eg. Foscarnet, Amantadine2. Neurotoxicity - seizures eg. Nucleoside analogues, Amantadine(high dose),INFs3. E imbalance- hypo K,hypo &hyper Ca eg.Foscarnet4. Hypo & hypertension eg. INFs5.Bone marrow supression- neutropenia eg. INFs,Aciclovir6.GI disturbance eg.INFs
  74. 74. 7. Flu like syndrome- F,fatigue, myalgia• eg. INFs8. Teratogenic eg.Aciclovir,Ginciclovir9.Hepatic steatosis eg. NRTI
  75. 75. How Does These Drugs Works…
  76. 76. Management in babies born to infected mothers Scenarios Therapy- HIV mother on HAART Zidovudine- HIV mother started on zidovudine at 14-28 2mg/kg/dose QIDx 6wksweeks gestation OR 4mg/kg/does BDx6 wks-HIV mother at delivery with inadequate Single doseprophylaxis (<4 weeks) Nevirapine +-Infant born to HIV mother without prophylxis Zidovudine 2mg/kg/dose QID 6 weeks OR 4mg/kg/does BD 6 weeks
  77. 77. Antifungal agents based on route of administration1.SystemicFor deep fungal infection Amphotericin B (I.V)(oral/parenteral) Flucytosine (oral) Imidazoles and Triazoles -Ketoconazole, Itraconazole -FluconazoleFor superficial fungal infections Griseofulvin (Oral)2.Topical antifungal agents Clotrimazole (CANESTEN) - Miconazole -Econazole -Ketoconazole -Nystatin (MYCOSTATIN)Miscellaneous MYCODERM
  78. 78. Drug Dose & Rx Side effects PreparationAmpho.B IV 1.5 mg/kg/d Local &systemic- Hypersensitivity(fungistatic/fungicid Intrathecal Meningitis,Endocardit Nephrotoxical) Oral 100mg 6h is due to Liver impairment Cream,ointment Cryptococcus Anaemia,Hypo-k Local installation Coccidioides Histoplasma Candida, Blastomyces AspergillusGriseofulvin 5-7mg/kg oral Broad spectrum Photosensitivity(fungiststic) Topical Microsporum,Epider Porphyria mophyton, Trichophyton Headache (Dermatophytosis) Hepatitis Superficial ringworm infestation (Tineacaptis,Tinea corporis,Tinea pedis)
  79. 79. Imidazole 5mg/kg oral,cream Supercial & Deep N,V,Pruritus,Rash,Ketoconazole 7.5-15mg/kg iv 8H Candida HepatitisMiconazole Topical,vg cream Dermatophytes Fluid & H2O(broadspectrum) (Teniasis,Pityriasis retension versicolar) Gynaecomastia Seborric dermatitisFluconazole (penetrate readily to Dermatophytosis Itchiness,burning, CSF) 3-6mg/kg oral Candidasis Rash /iv CryptococcusItraconazole 2-4mg/kg oral AspergillosisClotrimazole Vaginal tab Candidasis No serious(fungistatic) 1%cream,oral Dermatophytosis systemic side effectNystatin Cream,ointment Candidasis(oral No systemic side(fungistatic/cid Vg tab thrush,GI,vaginal, effectal) Oral Skin)
  80. 80. Summary• Ampho B –drug of choice except candida• Griseofulvin –drug of choice for dermatophytes except aspergillus• Fluconazole ,Miconazole _ for candida/dermatophytes• Nystatin _ for candida
  81. 81. Anti-protozoal drugs• Antmalarial drugs1. 4 Aminoquinolones CQ2. 8- Aminoquinolones Primaquine3. Arylamino alcohols Quinine, Mefloquine4. Anti-folates Sulphadoxine,Pyrimethamine5. Quinghaosu Artemisin
  82. 82. Blood schizontocides Alleviate symptoms-a/c attack Photosensitivity,n,v,reti-CQ Oral 10mg/kg x 3d nal damageQuinine Oral 8.3mg/kg x7-10 d Tinnitus,Hglycemia Iv 20mg/kgx4h,8.3mg/kg 8H HypotensionMefloquine 15mg/kg stat,10mg/kg a/f 6-8hr (cinchonism) (Prophylaxis- 5mg/kg wkly) Postural Hypotension Cardiac conduct defectArtesunate Oral 5mg/kg D1,2.5mg/kg D2- Relatively safe D3 IV,IM 2mg/kg then 1 mg/kg 6HArtemether IM 3.2mg/kg stat 1.6 mg/kg dailySporontocidesPyrimethamine ProphylaxisPrimaguineProguanil
  83. 83. Tissue schizointocides To prevent parasites becoming established in the LiverPyrimethamine 25mg tab* 0.3mg/kg daily X14 d CI –PregnancyPrimaquine 3.5mg/kg oral H’lysis in G6PDdef,BM˅,Proguanil alopeciaHypnozoiticides To prevent relaspePrimaquineGametocidesPrimaquine 0.7mg/kg od
  84. 84. Mgt of Pl.falciparum(Paed:protocol)• Uncomplicated • Complicated1st line- 1st lineArtesunate odx3D IV Artesunate bdodMefloquine od 2nd lineAlternate: IV Quinine oralArtemether/lumefantrine Doxycycline/Clindamycin2nd lineQunineClindamycin
  85. 85. AntihelminthicsDrugs Rx advantage Mode of Action Adverse EffectsMebendazole Trichuriasis Broad spectrum, inhibit Worm migration50-100mg BDx Enterobiasis microtubules, glucose (rare)3D Ascariasis absorption  immobilization deathAlbendazole Trichuriasis200-400mg single Enterebiasis Ascariasis HookwormPyrantel pamoate Trichuriasis Depolarization of the Mild abdominal pain10-11mg/kg OD Ascariasis neuromuscularRepeat in D14 Enterobiasis (Neuromuscular blocking agent)Levamizole Ascariasis Immunostimulants Abdominal pain3mg/kg Enterobiasis Paralysis of the muscle of the worm – expelled byRepeat in 1 wk Hookworm peristalsisIvermectin Hookworm, filariasis, Membrane Abdominal0.15-0.4mg/kg strongyloides hyperpolarization ; distension , paralysis wheeze, TOCThiabendazole Hookworm200-400mg OD
  86. 86. • References:- Paed:Protocol (2nd edition)- Nelson Text Book (19th edition)- Basic and Clinical Pharmacology(11th edition)- Basic Medical Science(Easterbrook-3rd edition)

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