Antiobiotics
Membrane integrity
Cell wall
B-lactam drugs
Polypeptides drugs
Glycopeptide drugs
Nucleic acid synthesis
Protein synthesis
Colistin AntiTetra- Chloroam- MacroAmino (plymixen Fungal glycosides cycline phenicol lides E) Drugs
Penicillins imidazole
Lincosemides
Fusidic acid
-Ketoconazole(oral) -Clotrimazole(all forms) -Fluconazlo/Itraconazloe
Cephalo sporins
Carbapenems
Monobactams
triazloe
-New/more effective/less toxic -oral/topical for systematic infections
polyenes
Large circular molecule consisting of hydrophilic & hydrophobic regions -Skin/hair infections
Nystatin
-Oral/topical -safe
AmphoTercin B
-systematic infections -IV mainly -Toxic
Essential metabolites synthesis
Sulfa -Nalidixic Quinodrugs acid Rifamycin lones -Nitro Rifampin Fluro- (sulfonafurantion quinoloes mides)
AntiTuber culosis drugs
-Ex:INH+streptomycin Ethambutol+rifampin
Cell wall
B-lactam drugs
Penicillins
Penicillin G Penicillin V *A*
Ampicillin Amoxacilllin *B*
Cephalosporins
First generation(1960s) Cephradine cephaexin Cephalothin
Second generation (1970s-1980s) Cefoxitin Cefuroxime
Polypeptide drugs
Carbapenems
Imipenem Entrapenem Meropenem
-For Nosocomial infections
Ticarcillin carbencillin Piperacillin *D*
Fourth generation (1995) cefepime
-Mainly against gram – ve Enteric bacteria. -used against: E.coli/Klebsiella/entero bacter/acinobacter/pse udomonas aeruginosa
-polyenes -bacteriocidal
-Broad spectrum -for serious/nosocomial
Third generation (1980s-1990s) Ceftrazidime cefotaxime Ceftriaxone
Aztreonam
-IV/IM
-IV/IM
-Bacetracin -Colistin (polymixen B)
-broad spectrum
-peniciliinase R
Infections Methicillin Oxacillin Cloxacillin Augmentin *C*
monobactams
-mainly against gram – ve Bacteria -bacteriocidal
-beaks down phospholipids of bacterial cell membrane changing membrane permeability. -very toxic( has side effects)
-used against:
-has amino & nitro groups
Pseudomonas aeruginosa
-used against:
-More effective than group *D*
MR-pathogens & Acinobacter(ca using septicemia) -nephrotoxic -oral/topical except on
Glycopeptides drugs
Vancomysin Teicoplanin
-used against: *ORSA *MRSA *Multi Renterococci(E.fecal is) *but not gram –Ve bacteria. -interfere with enzymes responsible for cross linking of peptidoglycan layer. -Inject able not oral. -useful in clinical practice.
-originated from orange filamentous fungus called (cephalosporium) -used for treatment of UT/RT/CSF/blood/intestinal/wound infections -They cant affect Anaerobic bacteria -They cant affect enterococcus group (UT infecting/naturally resistant to cephalosporin's)
Fisrt generation
-similar activity to ampicillin & amoxicillin -decreased usage by time -They have narrower spectrum than other drugs.
Cephalosporins
Second generation
-broad spectrum -affect Facultative anaerobic bacteria -used especially in surgeries
Third generation
-Mainly against G-ve bacteria -They are expected to be unavailable in the next 5 years.
Fourth generation
-Affect mainly Gve bacteria like pseudomonas -used in hospitals.
-not effective with developing bacteria -Broad spectrum
B lactam drugs side effects :sensitization/fever/serum sickness/penicillin allergy/anaphylactic shock/nephritis
Penicillin -Bactericidal -Affect + Anaerobic/narrow spec. -Injected (not orally since its inactivated by stomach acids) -1940-1941
*A*
*B*
*C*
-broad spectrum
Penicillin G
-Narrow spectrum
-1965
-From organsim ”penicillium notatum”
(-Ve)
-Affect facultative anaerobic bacteria found in intestine.
Penicillin V
*D*
-mid 70s -B lactamase susceptible. -For nosocomial infections.
-Bactericidal -Affect +Anaerobic/narrow spec. *C*
-can be taken orally (not inactivated) -1942-1943 -it’s a modified penicillin G
Methicillin
Oxacillin
Cloxacillin
Augmentin
-first drug produced to resist penicillinases -1960s -not used any more -unstable /inactivated at room temperature -has side effects -modified to oxacillin & cloxacillin
-narrow spectrum(+ve) -used in laboratory and Clinical Practise -used against ampicillin amoxicillin Penicllin G,V resistant bacteria -1960s
-Amoxacillin+clavulanic acid -Broad spectrum -Penicillinase resistant (due to The presenece of Clavulanic acid)
Protein synthesis
-Can be inhibited by bacterial Enzymes -IV/acid unstable
Tuberculosis
Intestinal infection
Meningitis sepsis
AminoGlysocides (30s subunit)
streptomycin
Neomycin Konamycin
Gentamycin Tobramycin Netilimycin Amikacin
TetraCyclines (30s subunit)
Doxycycline minocycline
-Broad spectrum. -Orally or injected (orally more common) -Not given to cildren Under 8 -For Ut/Rt infections Caused by mycoplasma ,clamydia and Legionella.
ChloramPhenicol (50s subunit)
MacroLides (5os subunit)
LincoSamides (50s subunit)
Erythromycin Clarithromycin azithromycin
-For UT/RT infections like Pneumonia & diphtheria -For mycoplasma/clamydia/ Staphylococcus/legionella Infections -inhibit peptidyl transferase activity & translocation of growing peptide to Ribosome -most applied orally/less IV
-Broad spectrum -block peptide bond formation -For intestinal/skin/respiratory /CNS infections Ie:Meningitis /septicemia/thyoid fever/ Aplastic anemia -can cross the blood brain barrier
Fusidic acid
-applied topically (creams/eye drops) -for skin infections -steroidal/prevent t-RNA translocation To ribosomes -not used in system. Infections very toxic -metronidazol(flagyl) is an example.
-For oral/bone infections -promotes the growth of colstridium Difficile causing pseudoMembranous colitis blood diarrhea( in colon) -used against strpt./staphy. infections
Anti fungal drugs: F/Cl/H/N groups….for Fungal infections caused bu yeast(candida… intestinal flora) & filamentous fungi (molds)…toxic drugs
Nucleic acid synthesis
Nalidixic acid
-affect mainly G-Ve Bacteria in UT. -for UT infections -used agains E.coli (responsible For 70%-80% of UT Infections) -Acts on DNA gyrase (type of DNA Polymerase)
Rifamycin
-prevent transcription by binding to RNA Polymerase -Broad spectrum -effective in killing IC Bacteria -used for serious infection Meningitis /brucellosis Not for simple RT infection (WHO) -Bacteria May produce enzyme affect B Subunits in RNA Polymerase Developing resistance to these drugs -less toxic then aminoglysocides.
quinolones
Norfloxacin
UT/RT infections
Ciprofloxacin
UT/RT(pneumonia)/ Intestinal/blood (septicemia) infections
Levofloxacin
Upper RT infections