TOPNOTCH MEDICAL BOARD PREP PHARMACOLOGY MAIN HANDOUT BY DR.

YNS PEREYRA-
BORLONGAN, MD-MBA For inquiries visit www.topnotchboardprep.com.ph or
https://www.facebook.com/topnotchmedicalboardprep/ This handout is only valid for October 2022
PLE batch. This will be rendered obsolete for the next batch since we update our handouts regularly.
TOPNOTCH MEDICAL BOARD PREP PHARMACOLOGY MAIN DIGITAL HANDOUT BY MARIA YNA
PEREYRYA-BORLONGAN, MD-MBA Page 72 of 95 For inquiries visit www.topnotchboardprep.com.ph
or https://www.facebook.com/topnotchmedicalboardprep/ This handout is only valid for the
October 2022 PLE batch. This will be rendered obsolete for the next batch since we update our
handouts regularly. MNEMONIC: Anti-Pseudomonal Cephalosporins ANTI-PSEUDOMONAL
CEPHALOSPORINS Ceftazidime Cefepime Cefoperazone You can also use a general mnemonic in
classifying the generation of the cephalosporin: 1st Generation: Starts with CEPH. Including
DRO+ZOL. (CefaDROxil and CefaZOLin) they start in CEF but are 1st gen 2nd Generation: Starts with
CEF. Doesn’t end in -ONE and -IME, plus LORA ceFU!!!! (dapat with feelings na parang inaaway mo si
LORA! (LORAcarbef and Cefuroxime) 3rd Generation: Starts with CEF. Ends in -ONE and -IME. Plus
Moxi Dinir, Ditoren, Buten. 4th Generation: Cefipime, Cefipirome The higher the generation, the
greater the gram (-) coverage. In the exam, they can ask which drugs can have a coverage, therefore
it is important to know the gram stain of the organism and the possible drugs that can be given.
Remember that in micro-pharma, a lot of drugs can be given for different organisms. So be wise in
studying. Don’t memorize everything. All these drugs are Preg-cat B Dr. Rodriguez FIRST GENERATION
CEPHALOSPORINS Cefazolin, Cefadroxil, Cephalexin, Cephalothin, Cephapirin, Cephradine Uses
Infections due to GRAM POSITIVE COCCI (Staph and strep) UTI, Skin and soft tissue infection, bone
infections Cefazolin Surgical prophylaxis SE Hypersensitivity, Cross-allergenicity (partial with
Penicillins, complete with cephalosporins), Injection site reactions, Phlebitis, GI upset Notes
+Aminoglycosides: Nephrotoxicity Minimal activity against G- cocci, enterococci, MRSA and most G-
rods Para mas madali, diba ang mga (+) cocci ay usually nakikita sa skin, sa genito urinary tract. Kaya
look at the uses Dr. Rodriguez SECOND GENERATION CEPHALOSPORINS Cefaclor, Cefamandole,
Cefmetazole, Cefonicid, Cefuroxime, Cefprozil, Ceforanide, Cefoxitin, Cefotetan, Loracarbef Uses +
Coverage: Haemophilus, Enterobacter and Neisseria SE Same above Cefamandole, Cefotetan
Disulfiram reaction Notes • + aminoglycosides: Nephrotoxicity • Slight less activity against G+ but
extended G- activity Cefuroxime Improved action against pneumococcus and H. influenzae Cefotetan
and Cefoxitin Good activity against B. fragilis (abdominal and pelvic infections) THIRD GENERATION
CEPHALOSPORINS Cefoperazone, Cefotaxime, Ceftazidime, Ceftizoxime, Ceftriaxone, Cefixime,
Cefpodoxime Proxetil, Cefdinir, Cefditoren Pivoxil, Ceftibuten, Moxalactam Uses Decreased gram-
positive coverage. Increased gram negative activity (Pseudomonas, Bacteroides), against Providencia,
Serratia, Neisseria, Haemophilus; Ceftriaxone and Cefixime DOC for gonorrhea SE Same with first gen
but no Phlebitis. Cefoperazone Disulfiram reaction Notes • + aminoglycosides: Synergistic effect •
Slight less activity against G+ but extended G- activity All have renal excretion except Cefoperazone
and Ceftriaxone All penetrate BBB except Cefoperazone and Cefixime Has very good CNS penetration
Ceftriaxone Has very good action on pseudomonas Ceftazidime Most active against Penicillin
resistant S. pneumoniae Ceftriaxone and Cefotaxime FOURTH GENERATION CEPHALOSPORINS
Cefepime, Ceftaroline (5th in other references), Cefpirome Uses Wide coverage against gram(+) and
gram (-) bacteria Ceftaroline MRSA SE Same with first gen Notes • More resistant to beta-lactamase
produced by Enterobacter, Haemophilus, Neisseria and Pneumococcus • Resistant to beta-lactamase.
Broad G(-) activity NOVEL CEPHALOSPORINS CEFTOLOZANE • A novel Cephalosporin, usually
combined with Tazobactam, used for the treatment of complicated urinary tract and intraabdominal
infections; very good activity against Gram negative organisms including Pseudomonas aeruginosa,
most extended spectrum-B-lactamase-producing organisms and some anaerobes CEFIDEROCOL •
Siderophore Cephalosporin: entry into bacterial cells is by binding to iron, which is actively
transported into the bacterial cells. • Used to treat complicated urinary tract infections and
pneumonias when no other options are available; Indicated for the treatment of multi-drug-resistant
Gram negative bacteria including P. aeruginosa. • Common side effects include diarrhea, infusion site
reactions, constipation and rash. May also cause serious and life-threatening allergic reactions,
severe diarrhea caused by C. difficile and seizures. (Warning for higher mortality) MONOBACTAM
Aztreonam MOA Binds to penicillin-binding proteins. Inhibits transpeptidation in bacterial cell walls.
Uses Infections resistant to beta-lactamases produced by gram-negative rods, including Klebsiella,
Pseudomonas and Serratia Aztreonam is the silver bullet. It is design for gram negative rods.
Pseudomonas is a gram-negative rod. SE Gastrointestinal upset, Superinfection, Vertigo, Headache,
Hepatotoxicity, Skin rash Notes • Resistant to beta-lactamase • No cross-allergenicity with Penicillins
• No activity against gram-positive bacteria or anaerobes CARBAPENEMS IMIPENEM-CILASTATIN,
ERTAPENEM, MEROPENEM, DORIPENEM MOA Binds to penicillin-binding proteins. Inhibits
transpeptidation in bacterial cell walls. Uses Wide coverage against gram-positive and gram-negative
bacteria. For serious infections such as pneumonia and sepsis SE Hypersensitivity, Cross-allergenicity
(partial with Penicillins), GI upset, CNS toxicity (confusion, encephalopathy, seizures) Notes •
Cilastatin inhibits renal metabolism (Hydrolysis) of imipenem by Dihydropeptidase (thus given
together) • Reserved for serious life-threatening infections • Low susceptibility to B-lactamases •
Active against Pseudomonas and Acinetobacter EXCEPT Ertapenem • Partial cross-allergenicity with
Penicillins CARBAPENEM RESISTANCE • Production of carbapenemases (carbapenem-hydrolyzing
enzymes) is the most important mechanism of carbapenem resistance • Other methods of
resistance: Porins, efflux pumps, mutations in penicillin-binding proteins • One method of
circumventing carbapenem resistance is to add Beta-lactamase inhibitor in combination. BETA-
LACATAMASE INHIBITORS • Inhibits inactivation of Penicillins by bacterial beta-lactamase
(penicillinase) Clavulanic acid, Sulbactam, Tazobactam MOA Inhibits inactivation of Penicillins by
bacterial beta lactamase (penicillinase) Uses Infections against beta-lactamase producing gonococci,
streptococci, E. coli and H. influenzae SE Hypersensitivity, Cholestatic jaundice Notes • Usual
combinations include: Amoxicillin-Clavulanate, Ampicillin-Sulbactam, Piperacillin-Tazobactam • Most
active against plasmid encoded beta lactamases (Gonococci, Streptococci, E coli and H. Influenzae) •
Not good inhibitor of inducible chromosomal beta lactamases (Enterobacter, Pseudomonas, Serratia)
TOPNOTCH MEDICAL BOARD PREP PHARMACOLOGY MAIN HANDOUT BY DR. YNS PEREYRA-
BORLONGAN, MD-MBA For inquiries visit www.topnotchboardprep.com.ph or
https://www.facebook.com/topnotchmedicalboardprep/ This handout is only valid for October 2022
PLE batch. This will be rendered obsolete for the next batch since we update our handouts regularly.
TOPNOTCH MEDICAL BOARD PREP PHARMACOLOGY MAIN DIGITAL HANDOUT BY MARIA YNA
PEREYRYA-BORLONGAN, MD-MBA Page 73 of 95 For inquiries visit www.topnotchboardprep.com.ph
or https://www.facebook.com/topnotchmedicalboardprep/ This handout is only valid for the
October 2022 PLE batch. This will be rendered obsolete for the next batch since we update our
handouts regularly. NOVEL CARBAPENEMASE INHIBITORS Diazobicyclooctanes (DBOs) Share five-
membered diazabicyclooctane ring AVIBACTAM (Ceftazidime/ Avibactam) Used to treat complicated
urinary tract infections, complicated Intra-abdominal Infections (cIAI)and hospital-acquired bacterial
pneumonia, ventilator associated pneumonia. RELEBACTAM (Imipenem/ Relebactam) Broadly active
against a wide variety of Gram-negative pathogens, including Enterobacterales, P. aeruginosa and the
anaerobic Bacteroides spp. More importantly, it has demonstrated excellent activity against key
multidrug-resistant pathogens. Boronic acid derivatives Derived from boronic acid VABORBACTAM
(Meropenem/ Vaborbactam) • Active against E. coli, K. pneumoniae and E. cloacae complex. Used for
treatment of infections (urinary tract infection, hospital-acquired • pneumonia / ventilator-
associated pneumonia, complicated intra abdominal infections or bloodstream infection) caused by
carbapenem resistant Enterobacterales (CRE). OTHER CELL WALL INHIBITORS GLYCOPEPTIDES
Vancomycin, Teicoplanin, Dalbavancin, Telavancin MOA Inhibits cell wall synthesis by binding to the
D-Ala-D Ala terminus of nascent peptidoglycan → inhibit transglycosylation → prevent elongation
and cross-linking of peptidoglycan chain Uses Serious infections caused by drug-resistant gram
positive organisms (MRSA), sepsis, endocarditis & meningitis, Pseudomembranous colitis Teicoplanin
and Telavancin are not absorbed in the GIT à used for bacterial enterocolitis, SE Red Man syndrome,
Nephrotoxicity, Ototoxicity, Chills, Fever, Phlebitis Notes • Reserved for serious life-threatening
infections • Treat red man syndrome by slowing the rate of infusion • Use oral formulation for
Pseudomembranous colitis • Narrow spectrum • VRSA and VRE are due to D-Ala-D-Lactate formation
• Decrease dose for renally impaired patients • Dalbavancin has very long t½ (6-11 days) which
permits once-weekly dosing and is more active than Vancomycin PEPTIDE ANTIBIOTICS Bacitracin
MOA Interferes with a late stage in cell wall synthesis in gram-positive organisms Uses Infections due
to gram-positive bacteria SE Nephrotoxicity Notes Reserved for topical use only due to marked
nephrotoxicity CYCLOSERINE Cycloserine MOA Blocks incorporation of D-Ala into the pentapeptide
side chain of the peptidoglycan Uses Drug-resistant tuberculosis (2nd line drug) SE Neurotoxicity
(tremors, seizures, psychosis) Notes Only used as a second-line agent in TB Must knows: •
Vancomycin – D-Ala-D-Ala (Dala Dala niya yung Vanco!). Redman syndrome • Baci(+)racin – For gram
(+), (+)oxic, (+)opical use Dr. Rodriguez Drugs DAPTOMYCIN [B] POLYMYXIN B, Polymyxin E MOA
Binds to cell membrane causing depolarization and rapid cell death Cationic detergents. Attach to
and disrupt bacterial cell membrane, bind and inactivate endotoxin. Bactericidal. Uses Infections
caused by G (+) bacteria including sepsis and endocarditis Gram-negative bacteria. For salvage
therapy of Acinetobacter, Enterobacteriaceae and Pseudomonas aeruginosa SE Myopathy Monitor
Creatine Phosphokinase weekly to check for severity of myopathy Eosinophilia, fever, Nephrotoxicity,
Neurotoxicity, Rash, Urticaria Notes • More rapidly bactericidal than Vancomycin • Inactivated by
pulmonary surfactants so cannot be used against pneumonia • Proteus and Neisseria are resistant •
For Topical use only (to limit toxicity) • *Both are Preg Cat C QUICK REVIEW: 1. Penicillins resistant to
beta-lactamase 2. All penicillins are Static/Cidals? 3. Generation of Cefixime? 4. DOC for gonorrhea 5.
Penicillin that causes interstitial nephritis Answers (1) Methicillin, Oxacillin Nafcillin (Remember
Staph your BLAC on Monday) (2) Cidal – remember all that disrupt the wall are cidal) (3) 3rd gen (4)
Ceftriaxone (5) Methicillin Dr. Rodriguez SUPPLEMENT: OTHER DRUGS ACTING ON CELLWALL
FOSFOMYCIN Inactivates the enzyme UDP-N acetylglucosamine-3-enolpyruvyltransferase which is
important in peptidoglycan synthesis (very early stage of bacterial cell wall synthesis) → prevents
formation of N-acetylmuramic acid (a peptidoglycan precursor molecule); for uncomplicated UTI;
safe for pregnant patients; renal excretion; resistance emerges rapidly; synergistic with Beta lactam
and quinolones SUPPLEMENT: MNEMONICS – Drugs of Last Resort Which antibiotics are considered
drugs of