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ORG MED LEC


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[Front]


1 A __ that blown in to Fleming's lab while he was on vacation in 1928 changed the course of medicine forever. 2 Fleming named the substance __ after the mould __.
[Back]


1 fungal spore 2 Penicillin, Penicillium notatum

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__ managed to produce larger amounts of penicillin and tested it on __
1 E. Chain and H. Florey (1930 to 1940s) (Nobel Prize 1945) 2 Mice
A substance is classified as antibiotic if the ff. conditions are met:
1. It is a product of metabolism 2. It is a synthetic product produced as a structural analog of a naturally occurring antibiotic. 3. It ANTAGONIZES GROWTH or survival of one or more species of microorganisms. 4. It is effective in LOW concentrations.
Antibiotics’ other attributes:
1. Exhibit sufficient SELECTIVE TOXICITY to be decisively effective against pathogenic microorganism or neoplastic tissue, without causing significant toxic effects 2. Chemical is STABLE enough to be isolated, processed and stored for a reasonable length of time without deterioration of potency. 3. RATE of biotransformation and elimination of antibiotic should be SLOW enough to allow a convenient dosing schedule, yet rapid and complete enough to facilitate removal of the drug from the body soon after administration is discontinued.
Classification of Antibiotics
1 Based on Mode of Action (Bacteriostatic, Bactericidal) 2 Based on spectrum of action (Broad spectrum, Narrow spectrum)
Broad Spectrum antibiotics list
1) Carbapenems 2) Chloramphenicol 3) 2nd, 3rd, 4th Gen Cephalosporins 4) 3rd gen fluoroquinolones 5) Broad spectrum penicillin 6) Tetracyclines
Narrow Spectrum antibiotics list
1 Penicillin G and V 2 Lincosamides (Clindamycin) 3 Glycopeptides (Vanco and Teicoplanin) 4 Streptogramins 5 Rifamycins 6 Daptomycins
Cell wall synthesis inhibitors
B-lactams, Glycopeptides, Bacitracin, Fosfomycin, Alafosfalin,
DNA Gyrase inhibitors
1 Quinolones 2 Coumermycin antibiotics
Protein Synthesis Inhibitors
Tetracyclines, Aminoglycosides, Macrolides, Lincosamides, Amphenicols, Pleuromutilins, Oxazolidinones
They have a macrolide structure
1 erythromycin 2 oleandomycin
Contain closely related amino sugar moieties
1 Streptomycins 2 Kanamycins, 3 Neomycins, 4 Paromomycins, 5 Gentamicins
Large group of polypeptides
1 bacitracins 2 tyrothricin 3 polymyxin BTP
1 Penicillin G other name 2 Penicillin V other name
1 Benzylpenicillin 2 Phenoxymethyl
What are the methods of Bacterial Resistance in Beta lactam type of drugs?
1 Efflux pumps 2 Beta-lactamases enzyme hydrolyze the amide bond of Beta-lactam ring (Inactivation) 3 Mutation of genes, altering the active sites and production of PBPs (penicillin binding proteins) 4 Closure of Porins 5 Impaired penetration of drug to target PBPs
It is in the general structure of penicillin
6-aminopenicillanic acid (6-APA)
Penam Nomenclature 1 CA-SYSTEM 2 USP-SYSTEM
1) 1-thia-4-aza-bicyclo[3.2.0]-7-heptane (Assign 1 to sulfur) 2) 4-thia-1-aza bicyclo [3.2.0]-7-heptane (Assign 1 to Nitrogen, 4 is sulfur)
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Penicillin side effects
ABCD-SSS 1 ANAPHYLAXIS 2 BLACK TONGUE 3 DIARRHEA 4 SKIN RASH 5 STOMACH UPSET 6 SEIZURES
Staphcillin side effects
Interstitial nephritis
Imipenem-Cilastatin
Seizures, allergic rxns, Toxic metabolite cause nephrotoxicity
Antipseudomonal penicillin (Extended spectrum)
CAROXYPENICILLIN AND UREIDOPENICILLIN 1 Carbenicillin 2 Ticarcillin 3 Piperacillin 4 Mezlocillin CTPM
Antistaphylococcal penicillin (RESISTANCE TO Beta-Lactamase)
1 Methicillin 2 Nafcillin 3 Oxacillin 4 Cloxacillin 5 Dicloxacillin
ACID RESISTANT PENICILLINS
VODKA Penicillin V Oxacillin Dicloxacillin Cloxacillin Amoxicillin
PENICILLINASE RESISTANT PENICILLINS
CONDOM Cloxacillin Oxacillin Naphcillin Dicloxacillin Oxacillin Methicillin
Tx of choice for gonorrhea
Ampicillin + Probenecid
In the repository forms of penicillin 1 Suspension of penicillin in __ 2 Suspension in __
1 Peanut oil or sesame oil with white beeswax 2 Vegetable oil with Aluminum monostearate or Aluminum distearate
Repository FORMS (IM) of penicillin
1 Penicillin G procaine (Crysticillin, Duracillin, Wycillin) 2 Penicillin G benzathine (Permapen)
Isoxazoyl Penicillins:
Oxacillin, Cloxacillin, Dicloxacillin
Agent of choice against Haemophilus influenzae infections
Ampicillin, 6-(d-α-aminophenylactemidopenicillanic acid) BN: Omniphen, Amcill, Principen
Treatment of choice for gonorrhea
Ampicillin + Probenecid
P-hydroxy analog of ampicillin better GI absorption than ampicillin introduced in 1974,
Amoxicillin 6-[d-(-)-α-amino-para-hydroxyphenylacetamido]penicillanic acid BN: Amoxil
Prodrugs of ampicillin
Hetacillin, Bacampicillin, Cyclacillin HBC
Ureidopenicillins
Piperacillin-most potent, Azlocillin, Mezlocillin
1 isolated three principal antibacterial activity: 2 three principal antibacterial activity:
1 1948: Abraham and Newton 2 Cephalosporin P1, Cephalosporin N, Cephalosporin C
1 Drug of choice for surgical prophylaxis 2 Active against H influenza but not Serratia or B fragilis
1 Cefazolin 2 Cefaclor, cefamandole, cefonicid, cefuroxime, ceforanide
1 Second gen cephalosporin
1 Cefuroxime 2 Cefaclor 3 Cefoxitin
Thurd gen cephalosporin
Ceftriaxone Cefotaxime Ceftazidime
Clavulanate acid
Streptomyces clavuligerus
Cephalosporin N
C. salmosynnematum
Cephalosporins
Cephalosporium spp.
Thienamycin
Streptomyces cattleya
Monobactam
Saprophytic soil bacteria in Japan and US