Antibiotics

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