Antimicrobial Spectrum of Resistance Pharmocokinetic Preparations and similar drugs Indications and Side effects

drugs activity peculiarities contraindications

Penicillins
Penicillin-G Gram positive: cocci Is broken Destroyed by Sod. Penicillin G Streptococal, Local irritancy
(benzyl penicillin) (Streptococci, down by gastric acid Pot penicillin G for oral use Pneumococcal, Allergic reactions
Pneumococci, Staph.
Aureus, gonococci),
penicillinase Very rapid renal Procaine penicillinG inj. Meningococcal, Superinfections
bacilli (B. antracis, C. excretion (t=12-24 hrs) Staphilococcal, Arachnoiditis in
diphtheriae, Clostridia, It’s administered Fortified procaine penicillinG infections, intrathecal inj.
Listeria, Spirochetes) i/m inj. gonorrhoea,
Benzathine penicillinG (t=2-4 syphilis,
weeks) diphtheria,
Phenoxymethyl penicillin prophylactic uses
(Penicillin V) - acid stable, is
used only orally
Cloxacillin Less active than PnG Penicillinase Acid resistant, Oxacillin Nafcillin
resistant incompletely Dicloxacillin -hepatitis,
Not resistant to absorbed from Flucloxacillin are not neutropenia
gram negative gut marketed in India
beta-lactamase Nafcillin - partially acid
resistant, permeate blood-brain
barrier
Ampicillin Gram positive, Is broken Oral absorption is Bacampcillin – prodrug, better Contraindicated Diarrhea, raches
(aminopenicillin) sensitive to PnG, gram down by incomplete, but tissue penetration, less to the patients
negative: H.
influenzae, E. coli,
penicillinase adequate, incidence of diarrhea with
Proteus, Salmonella permeate blood- Amoxicillin – better oral hypersensivity to
and Shigella brain barrier absorption, less incidence of PnG
diarrhea, less active Shigella
and H influenzae
Carbenicillin Pseudomonas Is broken Destroyed by Carbenicillin-indanyl – acid Serious inf. Bleeding
(carboxypenicillin) aeruginosa and indole down by gastric acid, used stable, used orally in u.t.i. Pseudomonas or (interfering
positive Proteus
penicillinase i. v. Ticarcillin – more potent Proteus (burns, platelet function)
septicemia, u.t.i.)
Piperacillin Pseudomonas Mezlocillin – similar to Neutropenic
(ureidopenicillin) aeruginosa and indole ticarcillin patients with
positive Proteus, 8
times more potent then
serious gram –
carbenicillin, active infections, burns
 against Klebsiella
Clavulanic acid Beta-lactamase Oral absorption Augmentin, enhabcin, Sever infections
inhibitor and amonate – amoxicillin +
bioavailability is clavulanic acid
60%
Sulbactam Beta-lactamase Given Sulbacin – ampicillin+
inhibitor parenterally sulbactam
Tazobactam – similar to
sulbactam
Cephalosporins
Fist generation: Gram+: Streptococci, Not resistant to Cefazolin – i.m., Cephalothin – resistant to As alternative to painfull injection,
Cefazolin Meningococci, Staph. beta-lactamase i.v. beta-lactamase, injected i.v. PnG, gram- diarrhea,
Aureus, gonococci, C.
Cephalexin diphtheriae, Clostridia,
Cephalexin – Cephaloridine – infections, hypersensivity
Listeria, Actinomyces, effective orally nephrotoxicity (withdrawn) surgical reactions,
Klebsiella, E. coli, prophylaxis, bleeding,
Proteus mirbilis, meningitis,
Salmonella, Shigella, gonorrhoea,
H. influenzae
typhoid,
Second generation -«- , Enterobacter, Resistant to Cefuroxime – is Cefuroxime axetil – effective
indol+ Proteus, septicemias
Cefuroxime beta-lactamase injected i.m. orally (gram-)
Bacteroides
Cefaclor Cefaclor – per os
Third generation Less effective on Resistant to Permeate through Cefoperazone, Ceftriaxone –
Cefotaxime gram+, but effective beta-lactamase blood-brain hypoprothrombinemia
against gram-:
Ceftriaxone Pseudomonas
barrier Ceftazidime – neutropenia,
Ceftazidime aeruginosa, thrombocytopenia
Cefoperazone Bacteroides
Ceftizoxime
Cefixime
Fouth generation More potent against Resistant to Cefepime Serious and
Cefpirome gram+ and gram- beta-lactamase hospital acquired
bacteria
infections,
septicemias,
lower respiratory
tract infections
Imipenem Gram+ coci, Resistant to Hydrolysed by Cilastatin – reversible Serious hospital
enterobacteriacea, Ps. beta-lactamase dehydropeptidase inhibitor of dehydropeptidase acquired
aeruginosa, Listeria,
 Cl.difficile of kidneys, inj. infections
I.v.
Aztreonam Gram- enteric bacilli, Resistant to i.m., i.v. 6-12 Lack of cross sensivity with hospital acquired
Klebsiella, beta-lactamase hourly other beta-lactam AB infections of
Pseudomonas, Serratia
urinary, bilary, gi
and female genital
tract
Erythromycin Gram+ and a few Almost all Acid labile – Roxitromycin, clarithromycin Aternative to Well tolerated, gut
gram-: cocci, Str., N. bacteria enteric coated (broader spctrum) – long PnG, atypical problems, rashes,
gonorrhoeae, Clostr.,
C. diphteriae, Listerai,
develop tablets, widely acting acid stable, spectrum is pneumonia- hearing
Micoplasma, H. resistance distributed in similar but it’s more potent, Mycoplasma and impairment,
influenzae, Chlamifdia, body, don’t cross better absorption, tissue Legionella inhibits hepatic
, Rickeytsia etc. blood-brain b. penetration and gastric oxidation of
tolerance many drugs (not
Azithromycin – expanded about
spectrum, intracellular azythromycin)
penetration
Clindamycin Similar to Good oral Lincomycin – less potent, Anaerobic and Diarrhea and
erythromycin: most absorption more toxic mixed infections: pseudomembra-
gram+ coci,
actinomyces,
abdominal, pelvic nous enterocolitis
Toxoplasma, anaerobes and lung
– Bact. fragilis abscesses
Vancomycin Penicillin substitute After i.v. inj. is Antibiotic Deafness, kidney
widely associated damage (dose
distributed, it si pseudo- related), fall in BP
not absorbed membranous (histamine
orally enterocolitis release)
Tetracycline Practically all types of Develops Effective orally, Oxytetracycline (1st g.) Contraindications: Suppression of
m.o. except fungi and slowly but milk, iron Demeclocycline (2nd g) pregnancy, bone growth,
viruses
preparations, Methacycline (2nd g) lactation, in brown color of
antacids and Doxycycline, Minocycline (3rd children, together teeth,
other food, cont. g) food doesn’t influence with diuretics, in phototoxicity,
metal ions impair adsorption renal or hepatic local irritation,
abs., bond to insufficiency, can allergic reactions,
plasma proteins cause liver and kidney
superinfections damage, photo-
 sensibilisation
Cloramphenicol Gram+ and gram-: Develops Well absorbed Cloramphenicol palmitate Second choice Aplastic anaemia,
cocci, Str., Salmonella, gradually in from gut, 50-60% used orally (susp) drug, avoid agranulocytosis,
B. pertussis, Klebsiella,
anaerobes inc. Bact.
most bacteria bond to plasma Cloramphenicol succinate for repeated courses, thrombocytopenia,
Fragilis, Micoplasma, proteins, widely parenteral administration regular blood irritation,
H. influenzae, distributed counts hypersensivity,
Chlamidia, , Rickeytsia superinfections
etc.
Streptomycin Aerobic gram- bacili Many It is neither Streptomycin sulfate Tuberculosis, Ototoxicity
organisms absorbed nor Neomycin – broader spectrum, subacute bacterial (cochlear and
develop rapid destroyed in gut, used only orally or topically endocarditis, vestibular
resistance rapidly absorbed plague, tularemia damage),
in i.m. injection nephrotoxicity,
Gentamicin More potent, than Develops Administered Tobramycin – less toxic, more First line neuromuscular
streptomycin, broader slowly i.m. active against Proteus, aminoglycoside blockade
spectrum: Ps.
aeruginosa, Proteus, E.
Pseudomonas, AB (the
coli, Klebsiella, Sisomicin – more active cheapest):
Enterobacter, Serratia, against Proteus, Pseudomonas, respiratory inf.,
ineffective against M. Klebsiella, Enterobacter other inf., SABA
tuberculosis, Netilmicin – broader
spectrum, effective against
many gentamicin resistant m.
Amikacin – the broadest
spectrum (including M.
tuberculosis
Polimyxin B Gram- bacteria only No cross No absorption Colistin is more potent against Skin infections, Systemic: flushing
exept Proteus, Serratia resistance from gut, used Pseudomonas, Salmonella, burns, otitis, and paresthesias
and Neisseria
mainly topically Shigella, used mainly orally conjunctivitis etc. (liberation of
and orally Bacitracin – active against cuased by gram- histamine), kidney
gram+, used topically Diarrea, enteritis damage,
Tyrothricin - active against etc. neurological
gram+ and few gram-, used disturbances,
topically neuromuscular
blockade
Nitrofurantoin Mainly E. coli Develops Well absorbed Furadantin Urinary tract Nausea and
slowly orally infections diarrhea
Nalidixic acid Gram-: E. coli, Develops Absorbed orally, Urinary Neurological
Proteus, Klebsiella, rabidly bound to plasma antiseptic, toxicity: headache,
Enterobacter, Shigella
proteins, diarrhea drowsiness,
metabolized in vertigo,
liver (active), parkinsonism like
high symptoms,
concentrations in leucopoenia etc.
urine
Ciprofloxacin Aerobic gram- bacilli, Develops High tissue Norfloxacin – less potent, used Blind therapy but ~10%, mild
especially slowly permeability, can for urinary, genital tract inf. not for mild or Gut pr., diarrhea is
entrobacteriacea and
Neisseria
be used orally Ofloxacin – more potent gram+ cases, infrequent
and i.v. against gram+ typhoid CNS: dizziness,
Pefloxacin (1st gen.) – more anxiety, insomnia
lipid soluble Skin: rash,
Lomefloxacin – single daily photosensivity etc.
administration Increase plasma
Sparfloxacin – gram+, concentrations of
anaerobes and mycobacteria, warfarin,
phototoxic reactions theophyllin,
Levofloxacin (2nd gen.)- caffeine, NSAIDs
improved activity and enhance toxicity
phkinetics, interactions
Sulfonamides Gram+ and gram- Develops Rapidly absorbed Short acting (4-8 hr) U.t.i., Trachoma Common: nasea,
bacteria, actinomyces, from gut, highly Sulfadiazine, Sulfisoxazole and inclusion vomiting,
Nocardia, toxoplasma,
Chlamidia
protein bond are Intermed. acting (8-12 hr) conjunctivitis, epigasric pain.
longer acting, Sulfamethoxazole, lymphgranuloma Crystalluria,
widely Sulfamoxole venereum, haemolysis,
distributed in Long acting (7 days) malaria, thrombocytopenia
body, excreted by Sulfadoxine, toxoplasmosis, etc., allergic
kidneys Sulfamethopyrazine nocardiosis, burns reactions,
Topical: Sulfacetamide sod., hepatitis,
Silver sulfadiazine photosensibili-
sation etc.
Cotromoxasole