ANTIBACTERIAL DRUGS 2 Flashcards
Nyatakan 2 jenis antibacterial agents yg merencant sintesis dinding sel
(1) Beta lactam antibiotik
- Penicillin,Cephalosporins,Carbapenem,
Monobactam
(2) Miscellaneous antibiotic
- Vancomycin & Bacitracin
Terangkan MOA beta lactam antibiotik
Ia akan mengikat pada PBP pada dinding sel bakteria lalu merencat enzim transpeptidase. Tanpa ikatan peptida antara NAM & NAM dalam dinding sel akn mybbkan struktur dinding sel tidak stabil. Maka, ini akan menyebbkan perbezaan tekanan osmotik lalu sel lysis
Nyatakan 5 jenis pengkelasan bagi penicillin
- Penicillin asli
- Penicillinase/Lactamase resistant penicillins (anti staph penicillin)
- Extended spectrum penicillin
- Antipseudomonal penicillins
- Combination of extended spectrum penicillins / antipseudomonal penicillin with beta lactamase inhibitor
Terangkan spectrum activity bagi (1) Penicillin asli
- active against gram (-) & (+) cocci, gram (+) bacilli & spirochetes
- sensitive to penicillinase enzymes
Cth : - Benzyl penicillin (Penicillin G) Benzathine Penicillin (Benzathine Penicillin G) Phenoxymethyl Penicillin (Penicillin V)
Terangkan spectrum activity bagi (2) Penicillinase / Lactamase resistant penicillin
- effective against beta lactamase producing stapylococci
- have low/no activity against other gram (+) & (-) organisms
- resistant to penicillinase enzymes
Cth: - Cloxacillin Flucloxacillin Nafcillin (not in FUKKM) Methicillin (Not available)
Terangkan spectrum activity bg (3) extended spectrum penicillin
- gram (+) coverage with extended coverage of more gram (-) bacteria
- Ampicillin more active on shigella & H.influenza
- Amoxicillin is more active against Salmonella & Streptococcal fecalis
- Sensitive to penicillinase enzyme
Cth : Ampicillin Amoxicillin Carbenicillin (not in FUKKM)
Terangkan spectrum activity (4) antipseudomonal penicillins
- broad spectrum but only used for pseudomonas,infection & ampicillin resistant proteus
- have activity against anaerobic gram (-) bacteria
- have synergistic effect when they are used with aminoglycosides
- sensitive to penicillinase enzymes
Cth :
Ticarcillin (not in
FUKKM)
Piperacillin
Terangkan spectrum activity (5) combination extended spectrum penicillins or antipseudomonal penicillin with beta lactamase inhibitor
- resistant pd penicillinase enzyme
Cth : Amoxicillin & clavulanic acid Ampicillin Sodium & Sulbactam Sodium Piperacillin & Tozabactam
Penicillin’s Indication
- Streptococcal infections, e.g. wound sepsis, acute throat infections, subacute bacterial endocarditis,.. etc.
- Staphylococcal infections of skin, mucous membrane and bone.
- Pneumococcal infections e.g. pneumonia.
- Syphilis and gonorrhoea.
- Meningococcal infections: Penicillin diffuses into the CSF only when the meninges are acutely inflamed.
- Typhoid and paratyphoid fevers: Ampicillin and Amoxycillin.
- Pseudomonas infection: Ticarcillin or Piperacillin
- Diphtheria and tetanus
- PROPHYLAXIS: prevent recurrent of Rheumatic fever and prevent subacute bacterial endocarditis
Penicillin Drug Interactions
- Bacteriostatic drug
- Antipseudomonal penicillin
with aminoglycoside - Methotrexate
- Oral Contraceptive Pills
Penicillin Adverse Effects
- Hypersensitivity
- Neurotoxicity and seizure in renal failure
patient - Neutropenia dan thrombocytopenia (Nafcillin)
- Interstitial nephritis (Methicillin)
- Hepatotoxicity- cholestatic jaundice(Coamoxiclav, Flucloxacillin)
Penicillin’s Warning & Precautionary Label
• Serious allergic reaction warning: Symptoms include a skin rash with or without blisters, flu-like symptoms
or swelling of your throat, tongue, or mouth.
• Severe diarrhea warning: This drug may cause diarrhea during and after your treatment with it due to Clostridium difficile.
• Prescription completion warning: If don’t complete
the prescription, this may cause resistance.
• Penicillins should be used with caution in individuals with histories of significant
allergies and/or asthma.
• Care should be taken to avoid intravenous or intra-arterial administration, or injection into or near major peripheral nerves or blood vessels, since such injections may produce neurovascular
damage.
Terangkan First Generation Cephalosporin
- do not penetrate to CSF
- senstive to beta lactamase enzyme
- active against (+) & with some (-)
Terangkan Second Generation Cephalosporin
- do not penetrate CSF
- used primarily in the management of urinary and respiratory tract,bone & soft tissue infections & prophylactically
- relatively resistant to beta lactamase
- gram (+) coverage with enhanced coverage of gram (-) bacteria
Terangkan Third Generation Cephalosporin
- can penetrate to CSF in the presence of meningitis
- excreted by kidney
- highly resistant to lactamase
- have long duration (12hrs) & ceftriaxone has longer duration (24hrs)
- effective against beta lactamase producing gram (+) coverage with excellent coverage of gram (-) bact & active against anaerobes
Terangkan Fourth Generation Cephalosporin
- can penetrate to CSF in presence of meningitis
- used primarily in the management of nosomial infections
- resistant to lactamase
- Cefepime has a powerful coverage against most gram (+) & gram (-) bact & anaerobes
Terangkan Fifth Generation Cephalosporin
- do not penetrate CSF
- used in management of complicated skin & soft tissue infections in adult resistant to vancomycin
- resistant to lactamase
- effective against MRSA less active against gram (-)
- no activity against pseudomonas
- less activity against SPACE organism
Cephalosporin Indication
• Severe undiagnosed sepsis especially in immunosuppressed patient.
• Treatment of infection of respiratory tract, urinary tract, skin, soft tissue,
bones and joints due to susceptible organisms.
• Gram-negative bacterial meningitis may be treated by cefotaxime (third
generation) and ceftriaxone that reach the C.N.S.
• Biliary infection: 3rd generation (cefoperazone or ceftriaxone).
• Gonorrhoea due to penicillin-resistant Gonococci. It is treated by single IM
injection of ceftriaxone.
• Pseudomonal infection when aminoglycosides are not desirable.
Cephalosporin Drug Interactions
IV ceftriaxone is added to any IV calcium-containing solution
(e.g. Ringer’s or parenteral nutrition) dangerous particulates of
ceftriaxone-calcium can result and precipitate in the lungs and
kidney. Separate between IV ceftriaxone and any IV calciumcontaining solution by at least 48 hours.
• Some third generation cephalosporins inhibit the enzyme aldehyde
dehydrogenase. If they are co-administered with alcohol,
acetaldehyde accumulates in blood leading to nausea and vomiting
(disulfiram-like reaction)
Cephalosporin Adverse Effects
- Hypersensitivity
- Nephrotoxic (1st gen with aminoglycoside and loop diuretic)
- Hypoprothrombinemia(3rd gen inhibit vit K epoxide reductase )
- Superinfection with C.difficile
Cephalosporin Warning & Precaution
• CONTRAINDICATION: Do not give cephalosporin to a person who allergy to beta lactam antibiotic/penicillin. • Prescription completion warning: If don’t complete the prescription, this may cause resistance.
Nyatakan 2 jenis & moa bg Miscellaneous Antibiotic
(1) Vancomycin - inhibits cell wall synthesis by binding to the D-Ala D-Ala terminal of the growing peptide chain during cell wall synthesis, resulting in inhibition of the transpeptidase which prevents further elongation & cross linking of the peptidoglycan matrix
- active againts gram (+) organism
(2) Bacitracin - inhibits the building of peptidoglycan unit (cell wall units)
- gram (+) bacteria
Terangkan Carbepenem
- cth ubat :
(i) imipenem+cilastatin - must combine to inhibit renal dihydropeptidase enzyme. If not, can lead to low urinary excretion & significant renal toxicity
(ii) meropenem, does not undergo metabolism by renal dihydropeptidase enzyme - last resort of many bacterial infections
- broad spectrum antibiotic that share similarity in structure & mechanism with penicillin
- highly resistant to beta lactamase
Terangkan Monobactam
- cth ubat : Aztreonam (Azactam)
- shared similarity in structure & mechanism with penicillin
- highly resistant to beta lactamase
- used as alternative to aminoglycosides in severe respiratory,urinary,biliary,GIT & female genital tracts infections
- has no cross sensitivity with penicllins or cephalosporins
- can be given to patients who allergic to penicillin
Vancomycin & Bacitracin Indication
Vancomycin : Indication: • treat serious MRSA infection in patient allergy to penicillin or cephalosporin. • Treat antibiotic associated enterocolitis • Adverse effect: • Red man syndrome • Ototoxicity • Nephrotoxicity
Bacitracin :
Indication: Only topically in combination with neomycin and polymyxin for minor skin infections due to serious
nephrotoxicity.
Carbapenem & Monobactam Adverse Effects
Carbapenem : - Blood disorders. • Seizures in high doses. Meropenem is less likely to provoke seizures. • G.I.T: nausea, vomiting.
Monobactam :
• Hematological effects
• Nephrotoxicity
• Pseudomembranous colitis
