Anti-microbials 22/8/10 Medsafe PY Mindmaps A-Z Format: TYPE OF PATHOGEN Name (alphabetical order) - class - activity against - dose - issues with use -> gaps in cover ANTI-BACTERIALS Amikacin - aminoglycoside - Gram –ve organisms (including Pseudomonas) + some Gram +ve cover - 7.5mg/kg Q12 hrly (titrated to troughs) - nephrotoxic, ototoxic, peripheral neuritis, neuromuscular blockade potentiation -> Amoxycillin - moderate-spectrum penicillin - gram +ve + improved cover against gram –ve bacilli - 1g Q4 hrly - rash with EBV -> staphylococcus and gram negatives Amoxycillin-clavulanate - broad spectrum penicillin - gram +ve’s, anaerobes, aerobic gram –ve bacilli - 1.2g Q6 hrly - platelet dysfunction, blood dyscrasias -> MRSA Ampicillin - broad spectrum penicillin - Gram +ve and Gram –ve organisms (ineffective against Beta-lactamase producers) - 500mg IV Q4 hourly - GI upset, rash -> staphylococcus and gram negatives Azithromycin - macrolide - anaerobes and non-enteric gram negatives - 10mg/kg LD Q24hrly -> 5mg/kg on subsequent days - nephritis, hepatitis Jeremy Fernando (2011) -> gram positive, atypical mycobacteria and Toxoplasma Aztreonam - monobactam - aerobic gram –ve including Pseudomonas - 2g Q6 hrly - phlebitis, hepatitis, thrombocytopaenia -> gram positives Benzylpenicillin - a narrow spectrum penicillin - gram +ve (streptococcus pneumoniae, listeria) - 1-5g/day in divided doses - increased Na+, decreased K+, GI upset – pseudomembranous colitis, seizures, nephritis, blood dyscrasias -> inactivated by beta-lactamases -> most staph’s are resistant -> streptococcus pneumonia increasing resistance Cefepime - 4th generation cephalosporin - gram +ve and gram –ve cover and anaerobes - 2g Q8 hourly - GI upset, rash Ceftazidime - 3rd generation cephalosporin (beta-lactam) - gram –ve and anaerobes, some gram +ve - 2-6g/24 hours in 2 to 3 divided doses (30-100mg/kg/day in divided doses) -> reduced gram positive cover Cefuroxime - 2nd generation cephalosporin with anti-haemophilus cover - gram +ve’s + improved gram –ve cover - adults 1.5g Q8 hrly, paediatrics 50mg/kg Q6hrly Ceftriaxone - 3rd generation cephalosporin - reduced gram +ve with improved gram –ve cover (improved CSF penetration) - 50mg/kg Q24hrs - reduce in renal failure Cephazolin - 1st generation cephalosporin + beta lactam resistant, all induce ESBL producers - gram +ve and some gram –ve cover - 15mg/kg Q8 hrly - 3-6% cross reactivity with penicillins Ciprofloxacin - 2nd generation quinolone - predominately gram –ve cover (Pseudomonas) - 300mg Q12 hourly - growing cartilage damage, achilles tendonitis, QT prolongation -> no anaerobic or gram positive cover Clarithromycin - macrolide - helicobacter pylori and mycobacterium avium complex Jeremy Fernando (2011) - 500mg Q12 hrly - hepatitis Clindamycin - lincosamide - gram +ve’s, anaerobes, some non-enteric gram negative (Helicobacter), intracellular organisms (mycobacterium avium complex) - high bone, bile and urine concentrations) - 2-4mg/kg Q6 hrly - GI upset, elevated LFT’s, blood dyscrasias Colistin (polymyxin E) - polymixin antibiotic - gram –ve rods and New Delhi metallo-B-Lactamase mutli-resistant Enterobacteriaceae - two forms with different dosing regimes - nephrotoxic and neurotoxic -> gram negatives not reliably covered: Proteus, Providencia, Serratia, Neisseria, Moraxella, Helicobacter, Brucella, Burkholderia, Stenotrophomonas (some strains) Co-trimoxazole - sulphamethoxazole + trimethoprim - sulphonamide - gram +ve and gram –ve cover and protozoan - covers Pneumocystitis jiroveci, Stentrophomonas maltophila, Listeria monocytogenes, Norcardia - 25-100mg/kg of sulphamethoxazole Q6 hrly (dose varies -> consult ID) - SJS, blood dyscrasias, influenzae like symptoms, Doxycycline - tetracycline - gram +ve and gram –ve but widespread resistance - good cover for Chlamydophila, Mycoplasma, Rickettseiae, Spirocheataes, Brucella, Coxiella brunetii - 200mg LD -> 100mg Q24 hrly - oesophagitis, tooth discolouration in kids, photosensitivity, pancreatitis, hepatitis Erythromycin - macrolide - gram +ve, anaerobes, non-enteric gram –ve infections, intracellular organisms - 20mg/kg/day in divided doses - long QT, monomorphic VT, pancreatitis, nephrotoxicity, hepatitis Flucloxacillin - narrow spectrum penicillin with anti-staph cover - staph (beta lactamase resistant) - 50-100mg/kg/day - cholestatic jaundice Fusidic acid - chemically related to the cephalosporins - penicillin resistant staphylococcal infections (endocarditis and bone infections) - 1g Q8hrly - GI upset, jaundice, rashes Gentamicin - aminoglycoside - aerobic gram –ve’s + pseudomonas coverage Jeremy Fernando (2011) - 3-5mg/kg LD -> titrate to trough - nephrotoxic, ototoxic, peripheral neuritis, neuromuscular blockade potentiation Imipenem-cilastatin - carbapenem - broad spectrum gram +ve, gram –ve and anaerobic cover - 500mg Q6 hrly - hepatitis, CNS stimulation, rashes -> MRSA, VISA, VRSA, atypical pneumonia’s. Linezolid - oxazolidinone - gram +ve’s (including multi resistant staphylococci and enterococci) - 600mg Q12 hrly - blood dyscrasias, GI upset, headache, dry mouth Meropenem - carbapenem - broad spectrum gram +ve, gram –ve and anaerobic cover - up to 2g Q8 hrly (40mg/kg) - hepatitis, CNS stimulation, rashes -> MRSA, VISA, VRSA, Enterococcus faecium, Stenotrophomonas and many Pseudomonas, atypical pneumonia’s Metronidazole - nitroimidazole - anaerobes and protozoa (including Trichomonas, Giardia and Entamobea) - 7.5mg/kg Q8 hrly - GI upset, rash, dark urine Moxifloxacin - 3rd generation quinolone - gram –ve, gram +ve, anaerobic and intracellular organisms of atypical pneumonia - 400mg Q24 hrly - growing cartilage damage, achillies tendonitis, QT prolongation -> Pseudomonas Nitrofurantoin - E.coli, Enterococcus, Staph aureus, Citerobacter, Klebsiella - 100mg QID PO (5-7mg/kg/day) - GI upset, headache, flatus Norfloxacin - 2nd generation quinolone - predominantly gram –ve cover - 400mg Q12 hourly - growing cartilage damage, Achilles tendonitis, QT prolongation Pipericillin-Tazobactam (Tazocin) - broad spectrum penicillin - gram +ve’s, anaerobes, aerobic gram –ve bacilli (superior enterococcal cover) - 4.5g Q8hrly - platelet dysfunction, blood dyscrasias -> MRSA, VISA, VRSA, multi-resistant gram negatives Quinupristin/dalfopristin - streptogramins Jeremy Fernando (2011) - VRSA, VRE, gram positive bacilli (Enterococcus faecium), gram negative aerobes (Neiserria and Moraxella), intracellular organisms - 7.5mg/kg Q8 hrly - arthalgia, myalgia, GI upset, headaches Rifampicin - rifamycin - gram +ve and gram –ve, mycobacterium tuberculosis and atypical mycobacteria - 10-20mg/kg/day - drug reactions: warfarin, OCP, cyclosporine, orange secretions, hepatitis, nephritis, thrombocytopaenia Roxithromycin - macrolide - gram +ve, anaerobes and some non-enteric gram-negative infections, intracellular organisms - 300mg Q24 hrly - hepatitis Teicoplanin - glycopeptide - MRSA, MRSE, gram +ve, good cover against streptococcus pneumoniae and C.difficile - 400mg LD -> 400mg @ 12 hours -> 400mg Q24 hrs - nephrotoxicity, blood dyscrasias, ototoxicity Telavancin - derivative of vancomycin - gram +ve’s (including MRSA) - 10mg/kg Q24 hrs - GI upset, metallic taste, headache, foamy urine Tetracycline - tetracyclines - chlamydia, rickettsia, spirochaete, brucella, mycoplasma, leptospirosis - 500mg Q12hrly - stained teeth in children, renal impairment, GI upset, hepatic impairment Tigecycline - glycylcycline - gram +ve’s (VRE, MRSA, MRSE), gram –ve’s (ESBL), anaerobes - 100mg LD -> 50mg Q12 hrly - GI upset, similar to tetracyclines Tircarcillin - carboxypenicillin (often in combination with clavulanate) - gram –ve organisms (especially Pseudomonas) - 3000mg/200mg (tircarcillin/clavulanate) Q4-8 hourly - increased Na+, decreased K+, GI upset – pseudomembranous colitis, seizures, nephritis, blood dyscrasias Tobramycin - aminoglycoside - aerobic gram –ve’s + Pseudomonas coverage - 3-5mg/kg/day in 3 divided doses -> monitor - nephrotoxic, ototoxic, peripheral neuritis, neuromuscular blockage prolongation Vancomycin Jeremy Fernando (2011) - glycopeptide derivative MRSA, MRSE, gram +ves, pencillin resistant streptococcus pneumoniae and C. difficile 10mg/kg LD -> dose of plasma concentration red man syndrome, ototoxic, nephrotoxic Jeremy Fernando (2011) ANTI-VIRAL Acyclovir - guanosine analogue - viral DNA polymerase inhibitor - anti-HSV - 10mg/kg Q8hrly - rashes, GI upset, hepatic and renal impairement, blood dyscrasias, CNS symptoms Alpha-interferon - interferon - used hepatitis B and C and many other diseases - SC injection - complex dosing - flu like symptoms, GI upset, haemodynamic instability, blood dyscrasias Amantadine - M2 channel inhibitor -> disruption of dissociation of viral matrix and riobnucleoprotein - anti-viral and anti-parkinsonian drug - anti-HSV and anti-influenza - for anti-influenzae: 100mg/day - GI upset, convulsions, hallucinations Famciclovir - guanosine analogue - anti-HSV - 1500mg OD PO (requires renal adjustment) - well tolerated Foscarnet - guanosine analogue - inhibitor of viron DNA polymerase - anti-CMV - 20mg/kg IV LD -> 20-120mg/kg according to renal function - GI upset, renal failure, hypocalcaemia, convulsions Gancicilovir - inhibition of CMV DNA polymerase - anti-CMV - administered as a prodrug (valganciclovir) - 5mg/kg Q12hrly IV - blood dyscrasias, rash, hepatorenal impairment, GI upset Valaciclovir - guanosine analogue - anti-HSV - 1000mg TDS PO - headache, nausea, SOB Oseltamivir - neuraminidase inhibitor - anti-influenzae - 75mg BD PO - GI upset Ribavirin - guanosine analogue Jeremy Fernando (2011) - DNA synthesis inhibitor -> active against many RAN and DNA viruses RSV and Lassa fever 20mg/mL nebulised for 12-18 hours for 3-7 days anaemia, worsening respiratory failure Jeremy Fernando (2011) ANTI-FUNGALS Amphortericin B - polyene - all Candida species except C.lustanae + anti-protozoan - 0.5-1mg/kg Q24 hr - nephrotoxic, hepatotoxic, GI upset, blood dyscrasias Caspafungin - echinocandin - all Candida species, Aspergillus - 70mg LD -> 50mg Q24 hrly - GI upset, headache, myalgia, increase in LFT’s, Fluconazole - azole - Candida albicans and Cryptococcus - 50-400mg Q24 hr - GI upset, hepatic dysfunction, arrhythmias Itraconazole - azole - broader anti-fungal activity than fluconazole but not as much as voriconazole – Candida albicans, Cryptococcus, aspergillus - 200mg Q12 hrly for 4 doses -> 200mg Q24 hrly - increased LFT’s, GI upset Nystatin - polyene - Candida albicans - topical application Voriconazole - azole - broadspectrum anti-fungal – Candida albicans, glabrata, krusei, Cryptococcus, Aspergillus - 6mg/kg Q12 hourly (loading for 24 hours) -> 4mg/kg Q12 hourly - transient visual disturbance, fever, rash, GI upset Jeremy Fernando (2011) ANTI-PARASITES Albendazole - benzimidzole - anti-nematode and cestode (worms) - 800mg PO in divided doses (give with fatty meal or grape juice -> increases bioavailability) - GI upset, headache, dizziness, hepatic impairment, pancytopaenia Ivermectin - synthetic antibiotic derivative - anti-nematode - 200-400mcg/kg - side effects related to parasitic load in host Mebendazole - benzimidzole - anti-nematode and cestode (worms) - 100mg OD PO - minimal side-effects Metronidazole - nitroimidazole - anaerobes and protozoa (including trichomonas, giardia and entamobea) - 7.5mg/kg Q8 hrly - GI upset, rash, dark urine Jeremy Fernando (2011) ANTI-PROTOZOANS Aretemether + Lumefantrine - anti-malarial - 20/120mg - complex dosing Artesunate - IV anti-malarial - 2.4mg/kg IV Q 12 hrly Atrovaquone + proguanil - anti-malarial - 250/100mg - complex dosing Clindamycin - lincosamide - gram +ve’s and anaerobes (high bone, bile and urine concentrations) - 2-4mg/kg Q6 hrly - GI upset, elevated LFT’s, blood dyscrasias Doxycycline - tetracycline - gram +ve and gram –ve but widespread resistance - 200mg LD -> 100mg Q24 hrly - oesophagitis, tooth discolouration in kids, photosensitivity, pancreatitis, hepatitis Mefloquine - anti-malarial - 15mg/kg LD -> 500mg Q6 hrly Quinine sulphate - anti-malarial - IV 20mg/kg LD over 4 hours -> 10mg/kg Q 8hourly - take with doxycycline or clindamycin or atovaquone+proguanil or mefloquine Jeremy Fernando (2011)