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Transcript
Antibacterial Drugs: **Mechanisms of action ( site of action ) 1. Nucleic acid synthesis inhibition: e.g Sulphonamides, trimethoprim, quinolones, nitrofurantoin, refampicin. • 2.Protein synthesis inhibition:e.g. • Macrolides, aminoglycosides, Chloramphenicol, tetracycline 3. Cell wall synthesis inhibition: e.g Vancomycin, cephalosporins, penicillins ** The β – lactam antibiotics: • These are the pencillines and cephalosporines whose basic structure include β – lactam ring Resistance is commonly due to bacterial enzyme called β – lactamases (( pencillinase and cephalosporinase )) which can cleave the ring and inactivate the antibiotic. ** The penicillins: • All penicillins are bactericidal with wide range of activity for both gram +ve and certain gram –ve organism • It should never given interathecally Their adverse effects include: • • • • • skin rash anaphylaxis drug fever interstitial nephritis haemolysis ** Benzylpenicllin: • It is rapidly absorbed following intramuscular injection and excreted by the kidneys withen few hours and addition of probenecid will delay its excreation and allow smaller doses with less frequent ** Procain Penicillin: • addition of procainamide, • given i.m, • Active against: streptococci, meningococci, anthrax, tetanus, syphilis and diphtheria. ** Phenoxymethyl penicillin (( Penicillin V )) • Incompletely absorbed from the stomach • Active against: streptococci . ** Cloxacillin & flucloxacillin • They are stable to staphylococcal β – lactimases • For oral therapy flucloxacillin is superior to cloxacillin ** Temocillin: •It is active against pencillinase producing gram –ve bacilli. ** Ampicillin; • It has a bactericidal action against both gram +ve and certain gram –ve organisms • It is susceptible to degradation by β – lactimase and not well absorbed with food. • Skin rash in patients with infectious mononucleosis ** Amoxycillin: • It is an analog of ampicillin which has similar antibacterial spectrum but it is more reliably absorbed from GIT ** Augmentin • It is a combination of amoxicillin and sodium clavulanate • Clavulanic acid is a potent inhibitors for many β – lactemases and it can protect amoxicillin from inactivation by them. ** Ticarcillin: • It is an analogue of carbencillin with more activity against Pseudomonus spp. • A combination of ticarcillin and clavulanic acid is called Timentin. ** Mezlocillin, azlocillin and pipracillin; • They have a wider range of activity and more effective against many gram –ve bacilli. The Cephalosporins; • 1st generation e.g cephalexin, cephradin • 2nd generation e.g cephaclor, cefuroxime • 3rd generation e.g cefotaxime, cephitrixone • 4th generation e. g cefepime, cefpirome • Wide range of activity • 10 % of penicillin sensitive may als allergic to them ** Imipenem: • Β- lactam antibiotic with a very broad spectrum which include aerobic and anaerobic gram +ve and gram –ve organisms. The Macrolide antibiotics ** Erythromycin: • Used in treatment of infection caused by gram +ve organisms in penicillin allergic patients. • It is effective in Whooping cough, pneumonia, mycoplasma and Chlamydia. • S/E : diarrhea, vomiting, abdominal pain, and cholestatic jaundice. **Clarithromycin: • Greater activity than erythromycin and higher tissue concentration ** Azithromycin: • More activity against gram –ve organisms including H. Influenzae. ** Spiromycin: • A macrolide used in treatment of Txoplasmosis. • The Tetracyclines: is a bacteriostatic agent used in Brucellosis, mycoplasma, typhus fever, Q – fever • It should not prescribed for pregnant female, children and patients with renal failure. The aminoglycosides: • They include gentamycin, streptomycin, amikacin • Active against gram –ve bacilli • Streptomycin has anti TB and used in treatment of Brucellosis • They are nephrotoxic and ototoxic • Neomycin is too toxic to be given parantraly and used orally in hepatic encephalopathy. *** Chloramphenicol: • It is effective in enteric fever and against H. Influenzae • It may cause pancytopenia • It should never be given to premature infant or to the newborn because of the risk of development of gray baby syndrome. *** Clindamycin / Lincomycin • Effective against most gram +ve organisms including penicillin resistant staphylococci • It pentrate well into bones so it is useful for osteomyelitis and effective in lung abscess • Common cause of pseudomembranous colitis ** Sodium fusidate • It is useful in infection caused by penicillin resistant staphylococci • It is well absorbed and the oral rout can be used instead the parenteral rout ** Spectinomycin • Used for treatment of gonorrhoea if penicillin is contraindicated because of allergy or bacterial resistance. Vancomycin and teicoplanin: • Used for serious staphylococcal infection including methicillin resistant and it is used in antibiotic associated colitis. • They are nephrotoxic and ototoxic ** Sulphonamides/ Trimethoprim / Co – trimoxazol • Used in treatment of cystitis, UTI, typhoid fever and pneumonia • S/E skin rash, nephritis and haemolysis *** Quinolone antibiotics • Ciprofloxacin is the most important one • Effective against aerobic gram –ve bacilli. • Used in treatment of typhoid fever, UTI, gonorrhoea • They are contraindicated in children and pregnancy ** Metronidazole • Effective against anaerobic bacteria and intestinal protozoa e.g Giardia Lambelia and Entameba histilytica. ** Tinidazole •It is similar to metronidazole but with longer half life *** Antituberculous • Refampicin, • INH, • Pyrazinamide, • Ethambutol and • Streptomycin drugs *** Antifungal drugs • For topical application: Nystatin, Clotrimazol • For oral administration: Ketoconazole, Grisofulvin • For intravenous infusion: Amphotericin, Flucytocin *** Antiviral drugs • Acyclovir: effective against herpes simplex and H. zoster • Famciclovir: antiherpes agent with activity against E B virus and hepatitis B virus • Ganciclovir: antiherpes agent with activity against cytomegalovirus • Amantadine: used for prophylaxis of influenza A. • Ziduvidine used for HIV infection. • Ribavirine: against RNA viruses e.g Influenza, RSV Antiparasitic drugs: • Antimalarial: Chloroquine, premaquine, proguanil • Anti intestinal protozoa: Metronidazole, tinidazole • Antihelmenth drugs: Mebendazole, Albendazole • Antibilharzial agents: Praziquantel.