Antibiotics

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Penicillin V & G

Back 1

V = Oral, G = IV
Mech: bind penicillin binding proteins and block cross-linking of peptidoglycan. --> autolysis of cell

Toxicity: Hypersensitivity, (hemolytic anemia)

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Penicillinase-resistant penicillins
(Methicillin, Nafcillin, Dicloxicillin)

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Mech: Same as penicillin (Blocking of peptidoglycan cross-linking). β-lactamase resistant because they have BULKIER R GROUP.

Use: S. aureus (not MRSA)

Toxicity: Hypersensitivity
Methicillin: Interstitial Nephritis (important)

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Aminopenicillins (Ampicillin & Amoxicillin)

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Mech: Same as penicillin (block peptidoglycan cross-linking). Often CLAVULINIC ACID is added to give β-lactamase Resistance.

Use: Gram + and Gram neg Rods. Mnemonic: H. Flu, E. Coli, Listeria, Proteus, Salmonella. Aminopenicillin HELPS to kill enterococci (also killed by aminopenicillins)

Toxicity: Hypersensitivity, PSEUDOMEMBRANOUS COLITIS
Ampicillin has characteristic rash

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Ticarcillin, Carbenicillin, Piperacillin

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Antipseudomonal penicillins

Mech: same as penicllin (block peptidoglycan cross-linking)

Use: PSEUDOMONAS, and gram neg rods. Can also be used with clavulinic acid (β-lactamase inhibitor).

Toxicity: Hypersensitivity

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Clavulinic acid

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β-lactamase inhibitor that is often added to aminopenicillins and antipseudomonal penicillins to extend coverage.

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Bacteriostatic Antibiotics

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ECSTaTiC about Bacteriostatics
E = Erythromycin
C = Clindamycin
S = Sulfamethoxazole
T = Trimethoprim
T = Tetracycline
C = Chloramphenicol

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Bactericidal Antibiotics

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"Very Finely Proficient at Cell Murder"
V = Vancomycin
F = Fluoroquinolones
P = Penicillin
A = Aminoglycosides
C = Cephalosporins
M = Metronidazole

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Cephalosporins

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Mech: Bactericidal antibiotic that prevents cross-linking of peptidoglycan (like penicillin) but is more resistant to β-lactamases.

Toxicity: Hypersensitivity (5-10% cross-over with penicillin).
With aminoglycosides: ↑ NEPHROTOXICITY
With Alcohol: Disulfiram-like reaction. blocks acetaldehyde dehydrogenase --> acetaldehyde buildup and hang-over symptoms. ONLY Cephalosporins with METHYLTHIOTETRAZOLE group i.e. cefamandole

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1st Generation Cephalosporins

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Cefazolin, Cefalexin "ZoLex watch"

Use: Gram pos cocci, Proteus, E. Coli, Klebsiella (PEcK)

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2nd Generation Cephalosporins

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Cefoxitin, Cefaclor, cefuroxime "Fox ClorOx)

Use: HEN PEcKS - H. Flu, Enterobacter, Neisseria, Proteus, E. coli, Klebsiella, Serratia

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3rd Generation Cephalosporins

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"Tri to Tax Taz"
Ceftriaxone, Ceftaxime, Ceftazidime
Use: Serious Gram NEGATIVE infections. Meningitis because they penetrate blood brain barrier.

Ceftriaxone is treatment of choice for N. Gonorhea

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4th Generation Cephalosporins

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Cefepime

Use: Pseudomonas and Gram + organisms

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Aztreonam

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Mech: Inhibit peptidoglycan synthesis, RESISTANT to β-lactamases. Monobactam

Use: Gram negative rods. Penicillin-allergy + Renal Failure (not tolerant of aminoglycosides)

Toxicity: None

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Imipenem // Meropenem

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Mech: Carbapenem. Blocks cell wall synthesis.

Use: Active against Gram pos cocci, gram neg rods, anaerobes. Drug of Choice for ENTEROBACTER.

Toxicity SIGNIFICANT. SEIZURES, skin rash, GI disturbance.

Notes:
Imipenem MUST be given with CILASTATIN; cilastatin inhibits renal dihydropeptidase I and ↓ inactivation in renal tubules.
Meropenem less toxic, less risk of seizures

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Vancomycin

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Mech: Bactericidal Antibiotic. Inhibits cell wall formation by binding D-Ala D-Ala in cell wall precursors.

Use: Gram + multi-drug resistant organisms. MRSA and C. Difficile

Toxicity: Nephrotoxic, Ototoxic, Thrombophlebitis. RED MAN Syndrome - diffuse flushing

Mech of Resistance (VRE): Change in peptides from D-ala D-ala to D-ala D-Lac

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Antibiotics that act on 30s Ribosome

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Aminoglycosides (bacteriocidal)
Tetracyclines (bacteriostatic)

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Antibiotics that act on 60s Ribosome

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CELL
C = Clindamycin, Chloramphenicol (Bacteriostatic)
E = Erythromycin (Bacteriostatic)
L = Linezolid (Bacteriostatic)
L = Lincomycin

"Buy AT 30, CELL at 50"

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Aminoglycosides

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"mycins" - Streptomycin, Gentamicin, Tobramycin, Neomycin, AMIKACIN (not fit with the others)

Mech: Inhibit formation of Initiation complex and cause misreading of mRNA. REQUIRE O2 UPTAKE. NOT USEFUL AGAINST ANAEROBES.

Use: Gram Neg Rod Infections.
Neomycin for bowel surgery.

Toxicity: Nephrotoxic (↑↑ with cephalosporins. Ototoxic (↑↑ with furosemide). Teratogenic

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Tetracyclines

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Tetracycline, Doxycycline, Demeclocycline, Minocycline

Mech: Bacteriostatic. Bind 30s prevent attachment of tRNA.

Use: Vibrio, Acne, Chlamydia, Ureaplasma, Urealyticum, Mycoplasma, Tularemia, H. Pylori, Borrelia, Rickettsia. "VACUUM THe Bed Room"

Toxicity: Discoloration of teeth, inhibition of bone growth, Photosensitivity (KNOW THESE)

Important NOTE: Doxycycline FECALLY eliminated. use with patients with RENAL FAILURE. (↓↓ absorption with milk, antacids, iron supplements)

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Macrolides

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"-romycins" - Erythromycin, azithromycin, clarithromycin

Mech: Blocks translocation and thereby protein synthesis. Bind 23s of 50s subunit.

Use: URI, Pneumonia (Mycoplasma, Legionella, S. Pneumoniae), STDs (Neisseria, Chlamydia). M. Avium Intracellulare prophylaxis

Toxicity: GI discomfort. ↑↑ concentrations of theophylline and ORAL ANTICOAGULANTS. Also acute cholestatic hepatitis and eosinophilia/rash.

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Chloramphenicol

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Mech: Inhibits peptidyltransferase (50s). Bacteriostatic

Use: Meningitis (not used often due to toxicity)

Toxicity: Aplastic Anemia, Grey Baby Syndrome (premature infants because they lack UDP-glucuronyl transferase)

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Clindamycin

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Mech: Blocks Peptide bond formation (50s). Bacteriostatic

Use: Anaerobic Infections ABOVE DIAPHRAGM

Toxicity: C. difficile overgrowth (pseudomembranous colitis).

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Sulfonamides

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Sulfamethoxazole, Sulfisoxazole, Sulfadiazine.

Mech: Para-aminobenzoic acid antimetabolite (PABA). Inhibit dihydropteroate synthesis. Bacteriostatic

Use: Gram +, Gram -, Nocardia, Chlamydia. SMX for simple UTI

Toxicity: Hypersensitivity, tubulointerstitial nephritis.
HEMOLYSIS in G6PD patients
KERNICTERUS in infants
Displaces drugs from albumin (warfarin --> ↑ effect)

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Trimethoprim

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Mech: Bacterial Dihydrofolate Reductase Inhibitor. Bacteriostatic

Use NOTE: used with sulfonamides (TMP-SMX) as a SEQUENTIAL BLOCK of FOLATE SYNTHESIS.

Uses: Recurrent UTIs, PCP prophylaxis, Salmonella & Shigella.

Toxicity: Megaloblastic anemia, Leukopenia, Granulocytopenia (folinic acid may ↓)

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Sulfa Drug Cross-Reactivities

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Sulfasalazine
Sulfonylureas
Thiazide Diuretics
Acetazolamide
Furosemide

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Fluoroquinolones

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"-floxacin" - Ciprofloxacin, Norfloxacin, ofloxacin, ENOXACIN and NALIDIXIC ACID (exceptions to rule)

Mech: Inhibition of DNA gyrase (Topoisomerase II). Bactericidal.
DO NOT TAKE WITH ANTACIDS

Use: Gram Neg ROD infections of GI/GU tracts.

Toxicity: GI upset, superinfection, headache dizziness, skin rash

C/I: Pregnant women and Children. --> Damage to cartilage. adults --> tendonitis and rupture. Kids --> leg cramps/myalgias

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Metronidazole

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Mech: DNA damage via toxic metabolites. Bactericidal. ANTIPROTOZOAL

Use: Giardia, Entamoeba, Trichomonas, Gardnerella, Anaerobes, H. Pylori (part of triple therapy)

Toxicity: Disulfiram-like reaction with alcohol (↑↑ hangover-sx). Metallic Taste

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Polymixins

Back 28

Polymixin B, Polymixin E

Mech: Bind bacterial cell membrane. Disrupts osmotic gradient, basic proteins that act like detergents.

Use: Resistant Gram Neg Infections

Toxicity: Neurotoxicity, Acute Renal Tubular Necrosis

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TB Treatment and Prophylaxis

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Prophylaxis: Isoniazid (INH)
Treatment: Isoniazid (INH-SPiRE)
Streptomycin
Pyrimethamine
Isoniazid
Rifampin
Ethambutol

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Ethambutol

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Toxicity: Red-Green Color Blindness Optic Neuropathy

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M. avium intracellulare Prophylaxis and Treatment (MAC)

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Prophylaxis: Azithromycin
Treatment: Azithromycin, Rifampin, Ethambutol, Streptomycin (similar to TB)

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M. Leprae Treatment

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No Prophylaxis
Treatment: Dapsone (Sulfonamide), Rifampin, Clofazimine

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Isoniazid (INH)

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Mech: ↓ mycolic acid synthesis.

Use: TB. Only one that can be used solo.

Toxicity: B6 deficiency --> Neurotoxicity. Hepatotoxicity.

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Rifampin

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Mech: Inhibits DNA-dependent RNA Polymerase

Use: TB, delays resistance to dapsone with M. Leprae. MENINGOCOCCAL and HiB PROPHYLAXIS.

Toxicity: ↑ Cyt P-450. Orange body fluids, hepatotoxicity.

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Resistance to Penicillins / β-lactams

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β-lactamases or Altered penicillin binding proteins (MRSA)

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Resistance to Aminoglycosides

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Acetylation, Adenylation, Phosphorylation

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Resistance To Vancomycin

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Change from D-Ala D-Ala to D-Ala D-Lac --> ↓ affinity

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Resistance to Chloramphenicol

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Acetylation

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Resistance to Macrolides

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Methylation of rRNA near binding site

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Resistance to Tetracyclines

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↓ uptake or ↑ transport out of cell

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Resistance to Sulfonamides

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Altered enzyme, ↓ uptake, or ↑ PABA synthesis

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Resistance to Quinolones

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Altered DNA Topoisomerase II (Gyrase) or ↓ uptake

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Prophylaxis for Meningococcal infection

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Rifampin

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Prophylaxis for Gonorrhea

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Ceftriaxone

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Prophylaxis for Syphilis

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Penicillin G

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Prophylaxis of UTIs

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TMP-SMX

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Prophylaxis of PCP pneumonia

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TMP-SMX

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Prophylaxis of Endocarditis with surgical procedures

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Penicillins

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Treatment of MRSA

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Vancomycin

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Treatment of VRE

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Linezolid and Streptogramins (quinupristin/dalfopristin)

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Amphotericin B

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Mech: Binds ergosterol and forms pores in membrane

Use: Systemic Mycoses (Crypto, Blasto, Histo, Coccidioides, Aspergillus, Candida), and intrathecally for fungal meningitis. DOES NOT CROSS BBB.

Toxicity: Nephrotoxicity, Arrhythmias, Anemia (due to nephrotoxicity), IV Phlebitis, Hypotension.
Hydration ↓ Nephrotoxicity

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Nystatin

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Mech: Binds to ergosterol and forms pores.

Use: Swish and swallow for oral thrush. Topical for vaginal or diaper candidiasis.

Toxicity: Too Toxic for systemic use.

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Azoles

Back 53

Ketoconazole, Fluconazole, Voriconazole, Miconazole

Mech: Inhibit ergosterol synthesis

Use: Systemic Mycoses
Fluconazole - Cryptococcal Meningitis (AIDS) and Candidal infections
Ketoconazole - Blasto, Histo, Candida, and Coccidiodes
Other Azoles - topical infections
Toxicity: ↓ Cyt P-450 (↑ drug concentrations), and GYNECOMASTIA

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Flucytosine

Back 54

Mechanism: Converted to 5-FU to inhibits DNA synthesis

Use: Systemic fungal infections as add on to Amphotericin

Toxicity: Bone Marrow Suppression, N/V/D

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Caspofungin

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Mech: Inhibits Cell Wall Synthesis by inhibiting β-GLUCAN (not cell membrane, CELL WALL)

Use: Invasive ASPERGILLOSIS

Toxicity: Flushing, GI disturbances

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Terbinafine

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Mech: Inhibits Squalene Epoxide (fungal enzyme)
Use: Dermatophytes

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Griseofulvin

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Mech: Interferes with Microtubules. Disrupts M-Phase

Use: Oral Tx of Superficial infections. Inhibits growth of dermatophytes

Toxicity: Teratogenic, ↑ Cyt-P450 (↓↓ drug levels), carcinogenic, confusion

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Amantadine

Back 58

Mech: Blocks viral penetration/uncoating by buffering pH of endosome. Releases dopamine from intact nerve terminals

Use: Prophylaxis and Treatment of Influenza A; also used in treatment of Parkinson's disease

Toxicity: Slurred Speech, Ataxia, Dizziness

Mechanism of Resistance: Mutated M2 protein. 90% of all strains are resistant to Amantadine. Know it as a Parkinson's drug.

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Rimantadine

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Amantadine derivative with fewer side effects because does not cross BBB. Therefore, not useful in Parkinson's disease.

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Zanamivir, Oseltamivir

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Mech: Inhibit Influenza Neuraminidase. Decreases release of viral progeny.

Use: Influenza A & B

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Ribavirin

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Mech: Inhibits synthesis of GUANINE nucleotides by competitively inhibiting IMP Dehydrogenase.

Use: Hepatitis C and RSV

Toxicity: HEMOLYTIC ANEMIA and TERATOGENESIS (SEVERE)

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Acyclovir

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Use: HSV, VZV, EBV
Prophylaxis in IC patients
NOT EFFECTIVE FOR LATENT FORMS

Mech: Guanosine Analog that is Monophosphorylated by viral thymidine kinase --> Triphosphate by cellular enzymes. Preferentially inhibits VIRAL DNA polymerase by terminating chain (since it is a guanosine derivative)

Toxicity: Well tolerated

Mech of Resistance: Lack of Thymidine Kinase

Front 63

Ganciclovir

Back 63

Use: CMV
Prophylaxis in IC patients
Mech:Guanosine Analog that is phosphorylated by CMV viral kinase.

Toxicity: Leukopenia, Neutropenia, Thrombocytopenia, Renal Toxicity. LESS SELECTIVE for HOST enzymes than acyclovir, hence more toxic effects.

Mech of Resistance: Mutated CMV DNA Polymerase or Lack of CMV Viral Kinase

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Foscarnet

Back 64

Mech: Viral DNA Pol Inhibitor. Binds to pyrophosphate binding site of enzyme. DOES NOT REQUIRE ACTIVATION BY KINASE

Use: 2nd-line for CMV Retinitis (1st line Ganciclovir). Acyclovir-resistant HSV.

Toxicity: Nephrotoxic.

Mech of Resistance: Mutated DNA Polymerase

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Protease Inhibitors

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"-navir" - Saquanivir, Ritonavir, Indinavir, Nelfinavir, Amprenavir

Mechanism: Block HIV Protease of progeny virions.

Use: Integral part of HAART.

Toxicity: GI intolerance, HYPERGLYCEMIA, Lipodystrophy.
INDINAVIR causes THROMBOCYTOPENIA

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Nucleoside Reverse Transcriptase Inhibitors

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Zidovudine (AZT or ZDV),
Didanosine (ddI)
Zalcitabine (ddC)
Lamivudine (3TC)
Stavudine (d4T)
Abacavir

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Non-Nucleoside Reverse Transcriptase Inhibitors

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Nevirapine
Efavirenz
Delavirdine

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Reverse Transcriptase Inhibitors General Information

Back 68

Mech: Inhibit HIV Reverse Transcriptase. Prevent incorporation of HIV DNA into host genome.

Use: Integral Part of HAART.

Toxicity: Bone Marrow Suppression (neutropenia, anemia), Peripheral Neuropathy
Nucleosides: Lactic Acidosis
Non-Nucleosides: Rash
ZIDOVUDINE: MEGALOBLASTIC ANEMIA

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HAART (Highly Active Anti-Retroviral Therapy)

Back 69

Use: HIV Treatment

Components: at least a PROTEASE inhibitor and a REVERSE TRANSCRIPTASE INHIBITOR.

Started when patients have CD4 <500 cells/mm3 or ↑ viral load.

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Zidovudine

Back 70

Nucleoside Reverse Transcriptase Inhibitor.

Use: General Prophylaxis in contacts of patients with HIV. Prophylaxis in Pregnancy to ↓ fetal transmission.

Toxicity: Megaloblastic Anemia (specific to ZDV), bone marrow suppression (neutropenia, anemia), peripheral neuropathy, and lactic acidosis

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Treatment for Bone Marrow Suppression caused by RT Inhibitors

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GM-CSF and Epo

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Fusion Inhibitors

Back 72

Enfuvirtide

Mech: bind gp41 subuint; inhibit conformational Δ required for fusion with CD4 cells.

Use: Patients with ↑ viral replication while on HAART. Used in combination with other drugs

Toxicity: Hypersensitivity, ↑ risk of bacterial pneumonia, injection site reactions

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Interferons

Back 73

Mech: human leukocyte glycoprotein that blocks viral RNA and DNA synthesis. Inhibits ribonuclease that degrades viral mRNA

Toxicity: Neutropenia

Interferons are DIRECTLY toxic to VIRUSES

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Use for Interferon α

Back 74

IFN α is used for Chronic Hepatitis B and C. and Kaposi's Sarcoma

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Use for Interferon β

Back 75

IFN β is used for Multiple Sclerosis

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Use for Interferon γ

Back 76

IFN γ is used for NADPH oxidase deficiency to activate more Mφ

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Antibiotics to Avoid During Pregnancy and Why? (9 - 7 antibacterials, 1 antifungal, 1 antiviral)

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Sulfonamides - Kernicterus
Aminoglycosides - Ototoxicity
Fluoroquinolones - Cartilage Damage
Erythromycin - Acute Cholestatic Hepatitis. (nor Clarithromycin)
Metronidazole - Mutagenesis
Tetracyclines - Inhibition of Bone Growth and Yellow Teeth
Ribavirin - Teratogenic
Griseofulvin - Teratogenic
Chloramphenicol - Grey Baby Syndrome

"SAFE Moms Take Really Good Care"