2 -Lactams

Penicillins
Important
Name Notable adverse effects Drug Interactions Other info
Indications
Administered with an Pneumococci, N. gonorrheae,
Urticaria, severe pruritus,
Drug of choice for AMINOGLYCOSIDE to and S. aureus are RESISTANT
Penicillin G fever, joint swelling,
SYPHILIS. treat ENTEROCOCCAL (PRSP). PARENTERAL.
hemolytic anemia, nephritis,
ENDOCARDITIS.
and anaphylaxis
Oral bioavailability
significantly reduced
PSEUDOMEMBRANOUS Oropharyngeal
Penicillin V by food. Should be ORAL
COLITIS due to C. DIFFICILE. infections.
taken 1 -2 hours
Antibiotic mediated
before or after meals.
endogenous infection.
Nafcillin Methicillin is the prototype,
Oxacillin, rarely used due to
Cation toxicity due to Antistaphylococcal
Cloxacillin NEPHROTOXIC POTENTIAL.
administration as salts.
Dicloxacillin Are penicillinase-RESISTANT.
Wider spectrum than penicillin
Syngergistic with
Listeria, E. coli, M. G.
aminoglycosides for
Ampcillin High incidence of skin rashes catarrhalis, and H. Cleared partly by biliary
Listeria and
influenzae excretion.
Enterococci.
UTI, Meningitis,
Given with
Sinusitis, otitis, and Great oral bioavailability.
Amoxicillin penicillinase inhibitors
Lower Resp. Tract Highest of Pencillins.
to improve half-life
infection
Frequently used with
aminoglycosides or UP superior against P.
Gram-negative
fluoroquinolones for aeruginosa.
Ureidopenicillin bacteremia,
infections outside CP superior against Klebsiella.
(UP) and pneumonia, post-burn
urinary tract.
carboxypenicillin infection, and
THESE TWO ARE CALLED
(CP) penicillin-resitant
GIVEN WITH ANTIPSEUDOMONAL
UTI.
AMINOGLYCOSIDE TO PENICILLINS
TREAT
 PSEUDOMONAL
INFECTION
ALL PENICILLINS (POOR PENETRATION INTO CNS UNLESS THERE IS INFLAMMATION, CROSSES PLACENTAL BARRIER BUT NOT
TERATOGENIC, POOR PENETRATION INTO BONE, EYE, AND PROSTATE). PROBENECID INCREASES HALF-LIFE DUE TO IMPAIRED
TUBULAR SECRETION.
Cephalosporins
Important Drug
Gen Name Adverse effects Other info
Indications Interactions
Drug of choice from Increased
Cefazolin prophylaxis for nephro-toxicity Choice for patients
(Others are Cephalexin, orthopedic, when given allergic to penicillin.
1st
Cephapirin, cefaloridine, abdominal, and with an Least toxic, does not
cefadroxil) pelvic surgery aminoglycoside. penetrate CNS.
(Cefazolin).
Cefotetan and Have more anaerobic
Cefoxitin May elicit May be useful as
Cefamandole and gram negative
2nd (Others are Cefaclor, Cefprozil, hypersensitivity prophylaxis in GI
(acetaldehyde activity than 1st
and Cefuroxime, Cefotetan) reaction in patients sugery (Cefoxitin).
accumulation , generation.
allergic to penicillin.
Drug of choice for disulfram-like
Local pain and Almost all penetrate
GONORRHEA effect
thrombophlebitis in BBB (NOT
(Cefotriaxone (hangover))
parenteral cefoperazone and
[parenteral], Also
preparation. cefixime).
cefixime [oral]) antivitamin K
Cefotriaxone, Cefotaxime,
effects that thin
3rd Cefpodoxime, Increased activity
Useful anti- blood and cause
Ceftibuten, Cefdinir towards Gram-
pseudomonal bleeding
negative.
activity (Cefotetan)
Useful in treating
(Ceftazidime)
bacterial meningitis.
Increased activity Cephalosporins
towards given with
 PNEUMOCOCCI aminoglycoside
(CEFTRIAXONE are used to
AND CEFOTAXIME) treat
Cefepime (increased pseudomonal
pseudomonal meningitis.
activity, decreaed
pneumococcal)
Many cross BBB and
Cefepime Cefpirome
4th are efective in
Cefpirome (increased
meningitis
pneumococcal,
decreased
pseudomonal
activity)
GOOD TISSUE PENETRATION (INCLUDING BONE), LESS SUSCEPTIBLE TO PENICILLINASES. MRSA ALSO RESISTANT TO
CEPHALOSPORINS
Carbapenems
Name Adverse Effects Indications Drug Int. Other
Cilastatin
inhibits
formation of
toxic
Drug of choice for E. faecalis. metabolite by
Metabolite is
Imipenem/Cilastatin, Penicillinase producing gram inactivating
Skin Rash, Seizures (high nephrotoxic
(others are meropenem, positive and negative bacteria. renal
doses), and hypotension
ertapenem) Anaerobes and Pseudomonas. dipeptidase.
 Monobactams
Name Adverse Effects Indications Drug Int. Other
Phlebitis, skin rash,
Aztreonam Enterobacteria Non-allergenic
superinfection, vertigo
Other Cell Wall Synthesis Inhibitors (Non--Lactam)
Name Adverse Effects Indication Drug Int. Other
Increases
Red man, red neck Penicillin-resistant,
Vancomycin aminoglycoside
syndrome MRSA
nephrotoxicity
High nephrotoxicity,
Wide variety of gram
Bacitracin limited to TOPICAL Bactoprenol inhibition
positive bacteria
APPLICATION
May be synergistic with
B-lactams and
Fosfomycin Gram negative UTIs Inihibits NAM synthesis
quinolones in specific
tissues
Tremors, seizures, Second-line drug for M.
Cycloserine
psychosis (potential) tuberculosis
Vancomycin-resitant
May cause myopathy
Daptomycin staphylococci and
(CK monitoring)
enterococci
 PROTEIN SYNTHESIS INHIBITORS
Tetracyclines
Name Adverse Effects Indication Drug Int. Other
Tetracycline of
choice in patients
Deposition in growing bone
with RENAL
and primary teeth
INSUFFICIENCY.
(staining) in small children.
Rocky-mountain
Contraindicated for
Doxycycline spotted fever Fecal excretion Good distribution to
pregnant and nursing
(rickettsiae), tissues except CSF.
women (tooth enamel
cholera, tick-borne
dysplagia), and young
Lyme. Malaria Absorption impaired by
children (crown
PREVENTION and divalent cations, antacids,
deformation)
amoebiasis dairy products and
treatment alkaline pH.
Superinfection and colitis
Helicobacter
Tetracycline pylori duodenal Absorption impaired by food.
Kidney toxicity when given
and gastric ulcers
with diuretics. IV injection
Minocycline ALL TETRACYCLINES
may cause
BIND TO 30S
thrombophlebitis. Fatal
RIBOSOMAL SUBUNIT.
acute degeneration of liver.
Meningococcal
High levels achieved in tears
carrier state
and saliva
 Aminoglycosides
Names Adverse Effects Indication Drug Int. Other
Irreversible ototoxicity and With broad Cell wall synthesis
neurotoxicity may occur with ANY spectrum B-lactam inhibitors enhance
aminoglycoside. for serious gram transport of drug into
negative bacilli bacterial cells.
All are parenterally
Nephrotoxicity in the form of acute infection (namely
administered (except
tubular necrosis (Gentamycin and P. aeruginosa) Block initiation complex
NEOMYCIN is
Tobramycin more commonly). (IF) formation. Cause
TOPICAL)
Are active against misreading of mRNA.
Amikacin and kanamycin more aerobic and Inihibit translocation.
Once daily dosing
prone to auditory impairment. facultative
recommended to
Amikacin anaerobic bacilli. Do not penetrate BBB or
reduce toxic
Gentamycin Vestibular impairment more likely enter vitreous humor.
accumulation.
Kanamycin with gentamycin and tobramycin. Inactive against
Necilmycin anaerobes and Renal filtration is main
Poor oral
Streptomycin Crosses placenta and may cause CN gram positive excretory mechanism.
bioavailability (highly
Tobramycin VIII damage in fetus. (except
polar drugs)
Neomycin staphylococci) Loop diuretics may
Factor V antagonism (bleeding). increase ototoxicity.
ALL
Rarely used alone,
AMINOGLYCOSIDES
Curare-like neuromuscular but for Yersinia Amphotericin B,
BIND TO 30S
blockade. Pestis (plague) and Cephalosporins and
RIBOSOMAL
tularemia they are. Vancomycin increase
SUBUNIT
Skin rash more commonly with odds for nephrotoxicity.
Neomycin (topical)
 Macrolides
Name Adverse Effects Indication Drug Int. Other
Thrombophlebitis with IV Crosses placenta, poor
injection BBB crossing,
Mycoplasma infection,
accumulates in
community acquired
Cholestatic jaundice, macrophages.
pneumonia, ALL MACROLIDES
hypersensitivity to esterified
Erythromycin Legionnaires disease, BIND TO 50S
form. Biliary excretion and
all forms of Chlamydial RIBOSOMAL
liver metabolism
infections, Diphtheria SUBUNIT. INHIBIT
Ototoxicity (high doses)
and pertussis. TRANSLOCATION.
METABOLITES
GI distress INHIBIT CYP450
Macrocyclic lactone
More chlamydial Stable to gastric acid.
ring to which deoxy
affinity, Longest half-life and
sugars are attached.
Azithromycin mycobacterium avium largest Vd.
complex and
Macrolide resistance in
toxoplasma Biliary excretion
bacteria may be
Stable in gastric acid.
induced by macrolides
Chlamydial affinity, Kidney excretion and
by activation of
mycobacterium avium liver metabolism.
Clarithromycin GI distress macrolide-inducible
complex and
methylase which
toxoplasma. METABOLITES
modifies ribosomal
INHIBIT CYP450
binding site.
Quinupristin/ Hyperbillirubinemia, arthralgia, Vancomycin-resistant Penetrates
dalfopristin myalgia enterococcus faecium macrophages and PMN.
Multidrug resistant
Linezolid Thrombocytopenia
gram positives
 Ketolides
Name Adverse Effects Indication Drug Int. Other
Equal to azithromycin
Penicillin resistant
against atypical
microbes.
Telithromycin pathogens (H.
Macrolide resistant
influenzae)
microbes.
Other protein synthesis inhibitors
Name Adverse Effects Indication Drug Int. Other
Drug of choice for
severe anaerobic
infections in abdomen,
female genital tract and
aspiration pneumonia,
used with
Inhibits formation of
cephalosporins and
ribosomal initation
aminoglycosides. Good tissue and bone
complex.
Neutropenia penetration.
Interferes with
Prophylaxis of
translocation reaction.
Clindamycin Superinfection endocarditis in valve Not to CSF.
(pseudomembranous disease patients who
Identical binding site to
colitis) with C. difficile. are allergic to Biliary and urinary
that of erythromycin
penicillin. excretion.
(30S RIBOSOMAL
Pneumocystis carinii
SUBUNIT)
pneumonia in AIDS
patients with
primaquine.
AIDS related
toxoplasmosis with
pyrimethamine.
 Bone marrow toxicity
at high levels (inhibits
mamallian ribosome)
Crosses BBB and
Blood dyscrasias placenta readily.
(aplastic anemia,
thrombocytopenia, 60% protein bound
Rocky mountain
granulocytopenia)
spotted fever and
Inactivated by hepatic
Typhus.
Superinfections (C. UGT.
difficile associated
Back-up for Salmonella
diarrhea) Weakly inhibits
and pneumococcal and
pseudomembranous CYP2C9 and CYP3A4
meningococcal
Chloramphenicol colitis
infection in penicillin
Decreases metabolism
sensitive patients.
Gray (Gray baby) of anti-convulsants and
syndrome-circulatory barbiturates.
Ineffective for
collapse, cyanosis, MI,
chlamydia and P.
abdominal distension, Rifampin and
aeruginosa.
coma and death. barbiturates increase
Accumlated metabolism of
Topically for eye
chloramphenicol. chloramphenicol.
infections
(increased risk in
patients with Decrease sulfonylureas
decreased hepatic metabolism.
function.

Glositis, stomatitis,
angioedema.
 PROTEIN SYNTHESIS INHIBITORS
Sulfonamides (Inhibitors of Folate Synthesis)
Name Adverse Effects Indications Drug Int. Other
Sulfamethoxazole Photosensitivity Useful in treating UTIs Rarely given alone
Exfoliative dermatitis Bladder infection, ear
Sulfisoxazole
Hemolytic/aplastic infection, meningitis
anemia First line treatment for
Granulocytopenia acute toxoplasmosis Sulfadiazine combined
Daraprim Thrombocytopenia DHFR inhibitor with pyrimethamine
Anti-protozoal agents
Urinary tract disorder Blocks folinic acid Sulfadoxine combined
Fansidar Precipitation of drug Anti-malarial agent
formation with pyrimethamine
crystals at NEUTRAL Ulcerative colitis,
OR ACIDIC pH. enteritis and other Given ORALLY (NON-
Sulfasalazine (crystalluria, inflammatory bowel ABSORBABLE)
hematuria, disorders
Sulfacetamide obstruction) Bacterial conjunctivitis Topical eye solution
Prevent by hydration Adjunctive drug in
Sodium-sulfacetamide and alkalinize urine. treating trachoma Topical agents
(chlamydia)
STEVEN-JOHNSON
SYNDROME-
detachment of
epidermis from dermis
Prevention of sepsis in
Mafenide-acetate KERNICTERUS in Topical agents
burns and wounds
newborns-sulfa
displace billirubin from
albumin, allowing high
[blood] to pass into
 CNS and cause damage.
Become lethargic with
episodes of spasticity.
May lead to
OPISTHOTONUS or
RETROCOLIS
(hyperextended neck)
SULFONAMIDES ARE BACTERIOSTATIC
Dihydrofolate Reductase Inhibitors
Name Adverse Effects Indications Drug Int. Other
Megaloblastic anemia,
leukopenia,
granulocytopenia AND
UTIs, Travelers Distributes well to CSF.
BONE MARROW
Diarrhea. Weak base,
TOXICITY may be
Combined with concentrates in acidic
prevented by folinic 20-50 times more
Trimethoprim sulfamethoxazole or environments.
acid (LEUCOVORIN) potent than
(and Pyrimethamine) dapsone for
administration. sulfonamides
prophylaxis and Usually used in
treatment of combination with
Mammalian DHFR
Pneumocystis sulfonamides.
inhibition (more a
problem with
pyrimethamine)
 Combination Drugs
Name Adverse Effects Indication Drug Int. Other
IV administration to
treat P. carinii
pneumonia Synergistic effect
Broader bacterial
Cotrimoxazole Folate deficiency Gram negative (inhibition of two
spectrum than SULFAS
(Trimethoprim Pancytopenia in HIV bacterial sepsis sequential steps in THF
Prosthatic and vaginal
+Sulfamethoxazole) patients synthesis)
fluid accumulation
Pneumonia, travelers
diarrhea, ear infection
and UTI

DNA INHIBITORS
Quinolones
Name Adverse Effects Indication Drug Int. Other
Nalidixic Acid Useful only for UTI, Prophylaxis before Inhibit DNA Gyrase and
systemic effective transurethral surgery Topoisomerase IV
levels were not
achieved
Fluoroquinolones
Name Adverse Effects Indication Drug Int. Other
Ciprofloxacin Reversible Drug of choice for Warfarin, caffeine, Most active against
arthropathies, treatment and antacids, medicines GRAM NEGATIVE (P.
including tendinous prophylaxis for with iron or zinc, aeruginosa)
rupture. ANTHRAX. didanosine, and
sucralfate interfere
Gastroenteritis with with fluoroquinolones.
severe diarrhea Bronchodilators
(theophylline,
 Effective for aminophylline)
chlaymidial urethritis Cimetidine interferes
and cervicitis. with elimination
Levofloxacin Effective for Superior activity
chlamydial urethritis against GRAM
and cervicitis POSITIVE (S.
pneumoniae)
Norfloxacin Least active of the
fluoroquinolones
against gram positive
and gram negative
Ofloxacin May worsen muscle E. coli prostatitis and
weakness in STDs, EXCEPT
myasthenia gravis SYPHILIS
leading to death
Lomefloxacin UTIs and bronchitis
due to H. influenza and
M. catarrhalis
Moxifloxacin Used for tuberculosis
and other
mycobacterial
infections (also, cipro
and levo)
Respiratory Gram positive and Examples are
fluoroquinolones gram negative atypical Levo-, gati-, gemi-,
pneumonias moxifloxacin. Upper
(chlamydia, and lower respiratory
mycoplasma, tract infections.
legionella)
Trovafloxacin Intra-abdominal
 infections
ALL FLUOROQUINOLONES (EXCEPT FOR MOXIFLOXACIN) ARE EFFECTIVE IN TREATING UTI EVEN WHEN ORGANISM IS
MULTI-DRUG RESISTANT (PSEUDOMONAS). ALSO EFFECTIVE FOR SALMONELLA, E.COLI, SHIGELLA, AND CAMPYLOBACTER