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ANTIBIOTIC CLASSIFICATION

CELL WALL SYNTHESIS INHIBITORS


PENICILLINS
MECHANISM OF ACTION (MOA):
Beta lactam ring inhibits last step of cell wall synthesis, leading to osmotic rupture of
bacterial cells; Destruction of existing cell wall by bacterial autolysins (bactericidal).
DISTRIBUTION:
Broad distribution in the body. Penicillins have the ability to cross the placental barrier but
are not teratogenic. They are the least toxic drugs known.
SPECTRUM OF ACTIVITY
Penicillins are only active against bacteria with peptidoglycan cell walls (not active against
viruses, mycobacteria, protozoa and fungi).
Penicillins and aminoglycosides have synergistic effects when used together. The
penicillins break down the cell walls, allowing for easier entry of the aminoglycosides.
ADVERSE REACTIONS
1. hypersensitivity: drug most commonly associated with hypersensitivity reactions
ranging from mucocutaneous rash to anaphylaxis.
2. neurotoxicity: may cause seizures at higher doses
3. nephritis: may cause acute interstitial nephritis
4. diarrhea: due to alteration of the normal gut flora
5. hematologic: neutropenia, thrombocytopenia.
TYPES
1. NATURAL PENICILLINS
Penicillin VK (oral); Penicillin G benzathine (IM); Penicillin G aqueous (IM,IV); Penicillin G potassium (IM, IV)

Produced from the mold penicillum chrysogenum


SPECTRUM OF ACTIVITY:
- Gram Positive* (most potent gram positive coverage of all penicillins). Penicillin G covers non
-lactamase producing gram positive cocci: Staphylococcus, Streptococcus, Enterococcus;
Bacillus anthracis (Anthrax).
- Gram positive anaerobes above the diaphragm ex. Clostridium species (except for C. difficile).
- Others: Penicillin G covers Neisseria meningitidis (although it is gram negative); Treponema
pallidum (spirochete that causes syphilis).
INDICATIONS:
- Strep pharyngitis (both; Oral/dental infections* (Penicillin V)
- Syphilis* (Penicillin G). Group A & B streptococcal infections

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ANTIBIOTIC CLASSIFICATION
2. ANTI-STAPHYLOCOCCAL PENICILLINS
Oxacillin, Dicloxacillin, Nafcillin, Methicillin
SPECTRUM OF ACTIVITY:
- Narrow spectrum of activity: restricted to penicillinase (-lactamase)-producing
staphylococcus). Only group of PCNs vs. -lactamase on their own.*

- Covers some streptococci but (NOT active v MRSA, enterococcus or gram negatives).


INDICATIONS: staphylococcal skin/soft tissue infections.



3. AMINOPENICILLINS
Amoxicillin (PO); Ampicillin (PO, IM, IV)

SPECTRUM OF ACTIVITY:
- Gram positive: Staphylococcus aureus (not used against -lactamase producing organisms).
Active vs. enterococcus & Listeria monocytogenes.

- Gram negative: Escherichia coli, Haemophilus influenza, Proteus mirabilis, Salmonella,
Shigella.


INDICATIONS:
- UTIs in pregnancy, H. flu, E. coli, L. monocytogenes (Ampicillin is the drug of choice),
Streptococcus species (Group B Streptococcus), Proteus, Salmonella. Amoxicillin is the
drug of choice for infective endocarditis prophylaxis & acute otitis media.

4. AMINOPENICILLIN WITH BETA-LACTAMASE INHIBITOR


Amoxicillin/Clavulanate (Augmentin); Ampicillin/Sulbactam (Unasyn)
- Enhanced coverage including -lactamase gram negatives (Moraxella Catarrhalis, H.
Influenzae, E. coli), anaerobes* (ex. B. fragilis). gram positive organisms.

INDICATIONS:
- Augmentin: AOM, sinusitis, Acute bacterial exacerbations of chronic bronchitis
(ABECB); Dental infections, bite wounds (covers anaerobes associated with both).

- Unasyn: skin/soft tissue infections, intrabdominal/peritonitis. Beta lactam inhibitor
enhances Staphylococcal coverage.


5. ANTIPSEUDOMONAL PENICILLINS
Piperacillin/Tazobactam (Zosyn) (IV); Ticarcillin/Clavulanate (Timentin) (IV); Carbenicillin (PO).
Clavulanate, Sulbactam & Tazobactam are -lactamase inhibitors

- Broadest spectrum penicillins! Reserved for severe infections causes or suspected


pseudomonal infections. Doesnt cover atypicals (Legionella, Mycoplasma, Chlamydia).
Has poorer Klebsiella coverage.

- Carbenicillin (PO) Also covers E. coli, Proteus mirabilis & Pseudomonas. Carbenicillin
does not contain a beta-lactamase inhibitor.

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ANTIBIOTIC CLASSIFICATION

CEPHALOSPORINS
MECHANISM OF ACTION (MOA):
Structurally and functionally similar to the penicillin family with a beta-lactam ring but tend
to be effective against beta-lactamase producing bacteria.

SPECTRUM OF ACTIVITY
Categorized by generations based on their spectrum of activity. Increasing level of gram
negative activity & loss of gram positive activity as you go from 1st to 4th generation.

In general, cephalosporins are not effective against Enterococci, MRSA, L. monocytogenes or
clostridium difficile.


ADVERSE REACTIONS
1. Allergic reaction: 5-15% cross reactivity with penicillins (therefore should not be used in
any patient with an anaphylactic reaction to penicillins). 1-2% occurrence in patients
without a penicillin allergy.
2. Disulfiram-like reaction (due to blockage of the 2nd step in alcohol oxidation).

TYPES
1. 1ST GENERATION CEPHALOSPORINS
Cephalexin (Keflex) (PO), Cefazolin (Ancef) (IV), Cephadroxil (Duricef PO)


SPECTRUM OF ACTIVITY:
- Gram Positive cocci (including Beta-lactamase producing organisms), anaerobes
- Gram negatives rods: E. coli, Haemophilus influenza, Proteus mirabilus, Klebsiella pneumoniae


INDICATIONS:
- Ind: Skin, soft tissue infections (staph, strep), Surgical prophylaxis



2. 2ND GENERATION CEPHALOSPORINS

Cefaclor (Ceclor), Cefuroxime (Ceftin PO or Zinacef IV, IM), Cefoxitin (Mefoxin IV), Cefotetan


SPECTRUM OF ACTIVITY:
- Broader gram negative coverage (including H. flu, Neisseria spp, Moraxella catarrhalis).
Weaker gram positive coverage. Exception: Cefoxitin & Cefotetan have less H. flu coverage
compared to the other 2nd generations cephalosporins. Cefoxitin has excellent coverage against
Bacteroides fragilis.


INDICATIONS:
- Ind: Skin, Respiratory/ENT & urinary tract infections, anaerobic infections: Acute otitis
media, Pneumonia, UTIs, abdominal infections (anaerobes). Skin & soft tissue infections.

- Cefuroxime: acute epiglottitis, early Lyme disease.


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ANTIBIOTIC CLASSIFICATION
3. 3RD GENERATION CEPHALOSPORINS

Ceftriaxone (Rocephin) (IM/IV), Ceftazidime*, Cefibuten, Cefotaxime, Cefixime

SPECTRUM OF ACTIVITY:
- Broader gram negative coverage (similar to 2nd generation but also includes Serratia and enteric
organisms). .
- Good CNS penetration (esp Ceftriaxone)*. Ceftazidime has coverage vs. pseudomonas
INDICATIONS:
- Ind: Meningitis (good CNS penetration)*, Gonorrhea, Community acquired pneumonia
(hospitalized)

4. 4TH GENERATION CEPHALOSPORINS

Cefepime (Maxipime), Cefobid. Only IV formulations


SPECTRUM OF ACTIVITY:
- Gram negative coverage including Pseudomonas aeruginosa.
- Gram positive: only methicillin-susceptible organisms

5. 5TH GENERATION CEPHALOSPORINS


Ceftaroline (Teflaro)

SPECTRUM OF ACTIVITY:
- Broadest spectrum in the cephalosporin class: gram positive (including MRSA) & negatives

CARBAPENEMS
Imipenem/Cilastatin (IV); Meropenem (IV)

MECHANISM OF ACTION (MOA):


Synthetic beta-lactam antibiotic. Addition of cilastatin reduces inactivation of carbapenems
by the proximal renal tubule. Good CSF penetration.
SPECTRUM OF ACTIVITY
Broadest spectrum of all antibiotic classes
ADVERSE REACTIONS
1. Neurotoxic: lowers seizure threshold (especially with imipenem).
2. GI: nausea, vomiting, diarrhea.
3. Eosinophilia & neutropenia (however less likely than other beta lactams).
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ANTIBIOTIC CLASSIFICATION


MONOBACTAMS
Aztreonam (IV)


MECHANISM OF ACTION (MOA):
Beta-lactam antibiotic that inhibits and disrupts cell wall synthesis, however, it is a beta-
lactam with no cross reactivity with other beta lactam antibiotics.

SPECTRUM OF ACTIVITY
- Primarily gram negative only: including pseudomonas & Enterobacteriaceae.
- Lacks reliable activity against gram positive organisms & anaerobes.

ADVERSE REACTIONS
Generally nontoxic but side effects include: hepatitis, phlebitis & skin rashes.


VANCOMYCIN

MECHANISM OF ACTION (MOA):
Cell wall inhibition (by inhibition of phospholipids/peptidoglycans).

SPECTRUM OF ACTIVITY
- Gram only*: S. aureus (including Methicillin-Resistant Staphylococcus Aureus MRSA)*,
Methicillin-Resistant Staphylococcus epidermis (MRSE), S. pneumonia, Enterococcal
infections.
- Synergistic use with aminoglycosides

INDICATIONS
Restricted use by CDC.
- Oral: Clostridium difficile colitis (2nd line treatment for C. difficile colitis or 1st line for
severe C. difficile colitis). Oral Vancomycin otherwise has poor tissue penetration.
- IV: MRSA, MRSE infections.


ADVERSE REACTIONS
1. Red-Man syndrome: flushing due to histamine release if given too rapidly via IV.
Prevented by giving the infusion slowly over 1-2 hours. Severe histamine release may
lead to anaphylaxis in some patients.
2. Fevers/Chills; Phlebitis at the IV site
3. Ototoxicity & Nephrotoxicity: especially if given with other antibiotics with similar
adverse effects (such as aminoglycosides). Ototoxicity may be reversible in some cases.

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ANTIBIOTIC CLASSIFICATION
Nephrotoxic so used primarily as
topical preparation for wounds

BACITRACIN

Gram mainly*
Little effect v anaerobes, gram negative

POLYMYXIN

Nephrotoxic & neurotoxic IM/IV


Gram negative coverage

Changes cell membrane permeability of
Used topically, ophthalmic, otic
outer membrane of gram negatives

PROTEIN SYNTHESIS INHIBITORS


TETRACYCLINES
MECHANISM OF ACTION (MOA):
Binds to 30S ribosomal subunit, inhibiting bacterial protein synthesis (bacteriostatic).

DISTRIBUTION:
Broad tissue penetration (both orally & IV). Doxycycline is the ideal tetracycline for IV
administration. Doxycycline is the safest in the group for use in patients with renal
impairment.

SPECTRUM OF ACTIVITY
Broad spectrum of activity: good against gram positive, gram negative, atypical organisms
and organisms other than bacteria.
ADVERSE REACTIONS
1. Poor GI tolerance: may cause diarrhea and gastritis.
2. Deposition in calcified tissue: deposition in teeth causes teeth discoloration & may affect
growth (Not given in children < 8y of age).
3. Hepatotoxic (especially in pregnancy) - contraindicated in pregnancy.
4. Photosensitivity; vestibular side effects, pseudotumor cerebri.
5. Impaired absorption if given simultaneously c dairy products, Ca, Al, Mg, Fe.
6. Contraindicated in patients with renal impairment (except Doxycycline).


INDICATIONS
1. Broad spectrum of activity.

2. Doxycycline drug of choice: Chlamydia infections (including C. trachomatis STD/s,
pelvic inflammatory disease, lymphogranuloma venereum); Chlamydia pneumophila
pneumonia, Chlamydia psittaci), Mycoplasma pneumoniae, Lyme disease, Rocky
Mountain spotted fever, Vibrio cholera, Q fever, Bubonic plague, Cat scratch fever.
Acne.

3. Tetracycline & Minocycline used for acne.
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ANTIBIOTIC CLASSIFICATION

AMINOGLYCOSIDES
MECHANISM OF ACTION (MOA):
Binds to 30S ribosomal subunit, inhibiting bacterial protein synthesis (bactericidal).
Antibitiotics that are derived from the streptomycin end in mycin; those derived from
Micromonospora end in micin. Concentration-dependent bacterial killing.

DISTRIBUTION:
Varied tissue penetration. Aminoglycosides not good for CNS penetration. Needs to be
renally dose in patients with renal impairment. Reduced activity in sites with acidic pH.

SPECTRUM OF ACTIVITY
Gram negative aerobic bacilli only (including pseudomonas). There is synergistic effect
when combined with a beta lactam or vancomycin.

Not good for gram positive organisms or anaerobic organisms (aminoglycoside entry into
bacterial cells is via an oxygen-transport system).

INDICATIONS

AMINOGLYCOSIDES
Gentamicin

Neomycin

Same as above

Amikacin
(Amikin)
Streptomycin

- Used c ampicillin in neonatal meningitis


- Septic shock
- Pyelonephritis & complicated UTI
- Endocarditis (enterococcus)
- Yersinia, Tularemia
Topical (keratitis)
Nosocomial Pneumonia (given with 3rd gen.
cephalosporin)
- Bowel prep. Component of Neosporin, Cortisporin
- Otitis externa (do not use if TM cannot be visualized)
Restricted use by CDC (reserved for bad infections)

Tuberculosis, Tularemia, Yersinia pestis.

Tobramycin

- Gram negative (including Pseudomonas).


Aminoglycosides dont reliably cover gram
positives & anaerobes

- Not used for Neisseria infections commonly
Slightly activity v. pseudomonas
-

ADVERSE REACTIONS
1. Systemic toxicity: must monitor serum drug levels (via peak levels 30 - 60 minutes after
administration & trough levels before the administration of the subsequent dose (only
trough levels needed in once daily dosing). Contact dermatitis with topical neomycin.

2. Nephrotoxicity: due to acute tubular necrosis.

3. Ototoxicity: (vestibular & cochlear) due to accumulation in the organ of Corti with
subsequent destruction. Cautious use of Gentamicin with other ototoxic drugs such as:
cisplatin, furosemide, bumetanide, ethacrynic acid, high-dose NSAIDs.

4. Neuromuscular paralysis: due to decrease acetylcholine release at the presynapse and
decreased acetylcholine sensitivity at the post synaptic cleft. Increased incidence of
paralysis in patients with myasthenia gravis.
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ANTIBIOTIC CLASSIFICATION

MACROLIDES
MECHANISM OF ACTION (MOA):
Binds to 50S ribosomal subunit, inhibiting protein synthesis.

SPECTRUM OF ACTIVITY
Broad spectrum of activity: good against gram positive, gram negative, atypical organisms
and organisms other than bacteria.
MACROLIDE
Erythromycin

Azithromycin
(Zithromax)

Telithromycin
Clarithromycin
(Biaxin)

SPECTRUM OF ACTIVITY
- Bacteria lacking cell walls: (Mycoplasma),
Atypicals: Legionella, chlamydia.

- Campylobacter , H pylori

- Good vs. gram negative & positive
including Strep pneumo & GABH strep

INDICATIONS
- Strep throat (if allergic to PCN).
Has similar coverage to
Penicillin G (may also be used in
syphilis in patients with PCN
allergy).
- Community acquired pneumonia
- Corynebacterium diphtheriae
- Topical use in acne
- Safe in pregnancy

- Poor GI tolerance*
- Same as above plus H. flu and Moraxella - Community acquired pneumonia

Anti-inflammatory in lung
- Best atypical coverage (Mycoplasma,
- Acute bacterial exacerbations of
Chlamydia, Legionella)*
chronic bronchitis


- Less activity vs. staphylococci -& - 1 time 1g dose for Chlamydia
streptococci compared to Erythromycin
- Mycobacterium avium complex
- Similar to Azithromycin

Same as above with better activity than
- CAP, Legionella, H pylori
Erythromycin
- Sinusitis, bronchitis, ABECB


ADVERSE REACTIONS
1. Poor GI tolerance: may cause diarrhea and abdominal cramps. Erythromycin may cause
bile stasis.
2. Ototoxicity: may cause deafness (usually reversible).
3. Prolonged QT interval
4. Many drug-drug interactions esp Erythromycin (inhibits cytochrome P-450 so caution
in patients taking warfarin, theophylline, carbamazepine, statins as the concomitant use
may cause toxic levels of those drugs). Increased absorption of digoxin while on
macrolides can be seen.
5. Contraindications: pt on niacin or statins (increased muscle toxicity), hepatic
dysfunction

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ANTIBIOTIC CLASSIFICATION

CLINDAMYCIN
Oral & IV preparations
MECHANISM OF ACTION (MOA):
Lincosamide (binds to 50S ribosomal subunit), inhibiting protein synthesis. Bacteriostatic or
bactericidal depending on drug concentration and susceptibility of the bacteria.
SPECTRUM OF ACTIVITY
Covers gram , most anaerobes especially above diaphragm* (little gram negative). Has
some MRSA coverage (however there is increasing resistance). Resistance activity in
general is similar to that of erythromycin.
ADVERSE REACTIONS
1. C difficile colitis: due to altered flora & the fact that C. difficile is inherently resistant to
clindamycin leads to C. difficile overgrowth pseudomembranous colitis.
2. Dermatitis
3. May be toxic in patients with renal & hepatic impairment.

QUINUPRISTIN/DALFOPRISTIN (SYNERCID)
IV only (in dextrose solution) Streptogramin class of antibiotics
MECHANISM OF ACTION (MOA):
Both agents bind to separate sites of the 50S ribosomal subunit leading to synergistic
protein synthesis inhibition, making them bactericidal (hence the brand name).
SPECTRUM OF ACTIVITY
Covers mainly Gram positive: usually reserved for Vancomycin-resistant Enterococcus
faecium (not Enterococcus faecalis). Covers MRSA. Has limited gram negative activity
(covers Legionella). Effective against Mycoplasma.
ADVERSE REACTIONS
1. Thrombophlebitis: reduced if given in central line as opposed to a peripheral line.
2. Cytochrome P450 inhibition increased levels of carbamazepine, diltiazem, verapamil,
cyclosporine, indinavir & ritonavir.
3. Hyperbilirubinemia

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ANTIBIOTIC CLASSIFICATION

LINEZOLID
Oral & IV
MECHANISM OF ACTION (MOA):
Inhibits protein synthesis (50S ribosomal unit) Bacteriostatic vs Staphylococcus &
Enterococci (bactericidal vs Streptococcus & Clostridium perfringens).

SPECTRUM OF ACTIVITY
Mainly gram positive: (including MRSA, VRE, enterococcus faecium and faecalis). Also
covers atypical organisms: mycoplasma, chlamydia, legionella. Not good vs. gram
negatives.
VRE = Vancomycin Resistant Enterococcus.

ADVERSE REACTIONS
1. GI: N/V/D, headache, thrombocytopenia (especially with treatment duration >2 weeks).
2. MAO Inhibition (avoid large amounts of foods with tyramine and sympathomimetics).
3. Increased serotonin syndrome with selective serotonin reuptake inhibitors.

CHLORAMPHENICOL
MECHANISM OF ACTION (MOA):
Binds to 50S ribosomal subunit, inhibiting bacterial protein synthesis

DISTRIBUTION:
Broad tissue penetration (both orally & IV). Good CNS penetration.

SPECTRUM OF ACTIVITY
Broad spectrum of activity: good against gram positive, gram negative, anaerobes & other
organisms (ex. Rickettsiae). Because of it high incidence of toxicity, it is usually reserved
for severe anaerobic infections or other life threatening infections not responsive to other
antibacterials.

ADVERSE REACTIONS
1. Bone marrow suppression: reversible anemia, hemolytic anemia (especially if GPD
deficient), aplastic anemia.
2. Grey baby syndrome (due to abnormal mitochondrial activity in neonates due to drug)
leading to cyanosis (may be fatal).
3. Drug interactions: may increase levels of phenytoin, warfarin and chlorpropamide

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ANTIBIOTIC CLASSIFICATION

DNA OR RNA SYNTHESIS INHIBITORS


FLUOROQUINOLONES
The fluorinated quinolones (FQs) have a broad spectrum of activity, excellent
bioavailability, tissue penetration, prolonged half-lives

FLUOROQUINOLONES
2ND GENERATION: increased activity vs aerobic gram negative bacteria & good intracellular
penetration
Ciprofloxacin (Cipro)

- Best gram negative coverage of all FQ (Enteric


organisms, H flu, Neisseria, Campylobacter).
Excellent vs pseudomonas*
- Not active vs. S. pneumo (so not used in CAP)
or Enterococci
Better activity vs. gram positive

Newer FQ: above plus enhanced coverage of Staph
(aureus, epidermis, saprophyticus), S. pneumo

- UTI, pyelonephritis*
- Gastroenteritis*, PID
- Malignant OE, sinusitis
- Gonococcal arthritis
- Anthrax
Norfloxacin (Norflox)
- UTIs (not good for

systemic infections)
Ofloxacin (Floxin)
- as above
- ABECB, community acquired
pneumonia (CAP)
Lomefloxacin (Maxaquin)
Same as Ofloxacin
As above
3RD GENERATION: increased activity vs gram positive & atypical organisms
Levofloxacin (Levaquin) Better activity vs. gram positive (ex. S. pneumo)
- Pyelonephritis, prostatitis,
Respiratory FQ Used for CAP (Pneumonia)
urinary tract infections
- CAP
- Gonococcal, Gastroenteritis
Moxifloxacin (Avelox)
Best Gram positive, anaerobic & atypical - Respiratory: CAP, bronchitis,
coverage activity of all FQ
Sinusitis

- Intrabdominal infections
Poor Psuedomonal coverage
- Ophthalmic, Skin infections
Gatifloxacin (Tequin)
Same as Ofloxacin
ABECB, UTI, CAP



MECHANISM OF ACTION (MOA):
Inhibits bacterial topoisomerases which are necessary for DNA synthesis (concentration
bactericidal activity)
DNA gyrase inhibition removes excess positive supercoiling in the DNA helix
Primary target in gram-negative bacteria
Topoisomerase IV inhibition affects separation of interlinked daughter DNA molecules
Primary target for many gram-positive bacteria

ADVERSE REACTIONS
1. GI: may cause nausea, vomiting, diarrhea
2. Neurologic: may cause headaches, may evoke seizures in patients with epilepsy.
3. Articular cartilage derangements: may be associated c tendon rupture in adults.
contraindicated in pregnant females, children <18y.
4. Photosensitivity, may cause QT prolongation
5. May exacerbate Myasthenia gravis
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ANTIBIOTIC CLASSIFICATION

Effective only v. anaerobes/ protozoa*
- inraabdominal
- Anaerobes: B. fragilis, C. dificile,
- vaginitis/osis
- Protozoa: Entamoeba histolytica, Giardia
- pseudomembranous colitis
lamblia, trichomonads
- amoebic liver abscess
Inhibits DNA synthesis. Approved for 1st trimester. Disulfiram like reaction if used with ETOH, neurotoxicity,
metallic taste

METRONIDAZOLE

(Flagyl)
-

DAPTOMYCIN

Gram positive only: (including MRSA, VRE, enterococcus faecium and


faecalis), Used in complicated skin infections
MOA: Binds & depolarizes bacterial membranes, causing inhibition of protein, DNA & RNA synthesis (cyclic lipopeptide)
S/E: Muscle toxicity, GI, arthralgias. Inactivated by surfactant, so not used in the tx of pneumonias


INHIBITORS OF ESSENTIAL METABOLITES

TRIMETHOPRIM/SULFAMETHOXAZOLE
MECHANISM OF ACTION (MOA):
Folic acid inhibition


SPECTRUM OF ACTIVITY
Broad spectrum: gram negatives; Gram positives: Staphylococcus aureus: 2nd best PO
coverage vs MRSA* (Linezolid is 1st but is not used as commonly as TMP/SX).

Not active vs Group A strep* (so often added with cephalexin for empiric oral tx of MRSA
cellulitis where the cephalexin covers Streptococcus).


INDICATIONS
- Urinary tract infections, acute otitis media, Acute Bacterial Exacerbation of Chronic
Bronchitis (ABECB)
- Drug of choice for pneuomcystic pneumonia (P. jiroveci).

ADVERSE REACTIONS
1. Avoid in pregnancy & infants (both populations have increase folic acid requirements).
2. Dermatitis and rash; GI side effects
3. Hematologic abnormalities (due to folic acid inhibition).

IND: Only used for cystitis (not for pyelonephritis or other infections)
Gram positives, Gram negatives, Enterococcus spp.
MOA: excreted in urine, where its active metabolites attack multiple bacterial sites
S/E: Hypersensitivity pneumonitis, chronic pulmonary fibrosis

NITROFURANTOIN

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ANTIBIOTIC CLASSIFICATION

ANTIFUNGAL MEDICATIONS
POLYENE ANTIFUNGALS Nystatin (topical, oral); Amphotericin B
MOA: Binds to cell membrane sterols (increasing permeability/fragility of cell membrane)

Amphotericin B:
1. INDICATIONS: standard of tx for most invasive or life-threatening fungal infections*

2. SIDE EFFECTS: fever/chills during IV infusion, electrolyte abnormalities (K,Mg),
nephrotoxicity & hematologic toxicity (anemia), azotemia.

3. LIPID-BASED AMPHO B: - advantages: high tissue concentrations, decreased infusion-related
reactions, marked decrease in nephrotoxicity but VERY expensive.

Nystatin
1. INDICATIONS: mostly topical use (vaginal) & local treatment: oral candidiasis (thrush)
2. No drug Interactions. Poor oral bioavailability.


AZOLES ANTIFUNGALS

Imidazoles: Clotrimazole (Lotrimin), Ketoconazole (Nizoral), Econazole, Miconazole


Triazoles: Fluconazole (Diflucan), Itraconazole, Voriconazole


MOA: Inhibits ergosterol synthesis (essential for fungal cell membrane stability)

INDICATIONS: Candidiasis, Cryptococcus, Histoplasmosis, Coccidiomycosis, Tinea (topical)
Fluconazole drug of choice for noninvasive Candida & Cryptococcal infections, water
soluble, good for urine & CSF infxn*, renal elimination, doesnt inhibit cytochrome P450.

Voriconazole EXTENDED spectrum (covers Aspergillus). Voriconazole drug of choice for
invasive aspergillis*

Itraconazole: EXTENDED spectrum (covers Aspergillus). Drug of choice for noninvasive
histoplasmosis, blastomycosis, coccidiomycosis (S/E may cause CHF).

Ketoconazole & Itraconazole - lipid soluble, not into CSF, inhibits cp450.


SIDE EFFECTS

Fluconazole: Hepatitis, Nausea, rash, alopecia, headache.


Ketoconazole: Suppression of Testosterone & Cortisol (used to treat refractory Cushings)






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ANTIBIOTIC CLASSIFICATION

ALLYLAMINES Terbinafine (Lamisil); Butenafine (Mentax)


MOA: Inhibits ergosterol synthesis (by inhibiting squalene epoxidase).


INDICATIONS: Dermatophyte infections:

Onychomycosis: Terbinafine PO

Tinea (Corporis, Pedis, Cruris): Terbinafine or Butenafine topical




GRISEOFULVIN
MOA: Inhibits fungal cell mitosis preventing proliferation & function.

INDICATIONS:
Tinea infections: capitus, cruris, pedis, unguium.

ADVERSE REACTIONS:
- Give c fatty meals to increase absorption.
- Hepatitis
- Teratogenic: including males males must avoid attempting to conceive for 6 months p tx.


CASPOFUNGIN
MOA: Inhibits cell wall glucan synthesis. Echinocandins.

INDICATIONS:
includes azole- & Ampho-B-resistant strains of Aspergillis & Candidiasis

ADVERSE REACTIONS:
fever, thrombophlebitis, headache, LFTs, rash, flushing. only IV - very expensive

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