First Aid Antimicrobials

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Penicillin

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Mechanism- Bind PBPs, Block transpeptidase cross-linking of cell wall, activate autolytic enzymes.
Clinical use- G+, syphilis
Toxicity- Hypersensitivity hemolytic anemia

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Methicillin, nafcillin, dicloxacillin

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Mechanism- Same as penicillin but penicillinase resistant because of bulkier R group.
Use- S. aureus (NAFCILLIN!!!)
Toxicity- Hypersensitivity. Methicillin causes interstitial nephritis

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Ampicillin, Amoxicillin

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Mechanism- Same as penicillin, penicillinase sensitive, wider spectrum. Amoxicillin > ampicillin oral bioavailability.
Use- Extended-spectrum (G+, G-, H. influ, E. coli, L. monocytogenes, Proteus, Salmonella, enterococci), neonatal infections and UTIs!!
Toxicity: Ampicillin rash, pseudomembranous colitis
Can combine with clavulanic acid to protect against beta-lactamase

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Ticarcillin, Carbenicillin, Piperacillin

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Mechanism- Same as penicillin. Extended spectrum.
Use- PSEUDOMONAS and Gram negative rods, Anaerobes
Toxicity- Hypersensitivity

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Beta-lactamase inhibitors

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clavulanic acid, sulbactam, tazobactam
Added to penicillin antibiotics to protect against destruction by beta-lactamase.

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Cefazolin, Cephalexin

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1st generation cephalosporins
Use- PEcK (Proteus, E. coli, Klebsiella) + GPC (skin flora, surgery prophylaxis)
Toxicity- Hypersensitivity with penicillins, nephrotoxicity with aminoglycosides, disulfiram-like reaction with ethanol.

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Cefoxitin, Cefaclor, Cefuroxime

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2nd generation cephalosporins
Use- HEN PEcK- H. Flu, Enterbacter, Neisseria, Proteus, E. coli, Klebsiella. + GPC
Toxicity- Hypersensitivity with penicillins, nephrotoxicity with aminoglycosides, disulfiram-like reaction with ethanol.

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Ceftriaxone, Cefotaxime, Ceftazidime

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3rd generation cephalosporins
Use- Serious GN infections resistant to other beta-lactams; cefriaxone is for meningitis and gonorrhea, ceftazidime is for pseudomonas. NOT LISTERIA.
Toxicity- Hypersensitivity any may cross-react with penicillins, nephrotoxicity with aminoglycosides, disulfiram-like reaction with ethanol.

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Generations of cephalosporins

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First - Gram+
Second +/-
Third broadest spectrum
Fourth - mostly gram positive

First you must get your PhD and don't be fazed by the challenge. After that you want to invite your Family who will wear FUR coats and your FOXY cousin will drink TEA. Third = tri = T

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Aztreonam

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Mechanism- Monobactam resistant to beta-lactamases; Binds to PBP3 to inhibit cell wall synthesis, synergistic with aminoglycosides. NO cross-allergy with penicillins.
Use- GNRs ONLY- used in patients who are allergic to penicillin and those with renal insufficiency who cannot tolerate AGs.
Toxicity- GI upset

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Imipenem/cilastatin, meropenem

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Mechanism- Beta-lactamase resistent carbapenem. Imipenem is always administered with cilastatin (inhibits renal dihydropeptidase I) to decrease inactivation of drug in the renal tubules.
Use- GPC, GNR, ANAEROBES (wide-spectrum). Empiric.
Toxicity- GI distress, skin rash, CNS toxicity (not meropenem)- significant toxicity limits use

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Vancomycin

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Mechanism- Inhibit cell wall mucopeptide formation by binding to D-ala-D-ala.
Use- GP ONLY; serious multi-drug resistant organisms (MRSA, enterococci, C. difficile oral, coag negative endocarditis)
Toxicity- Nephrotoxicity, Ototoxicity, Thrombophlebitis, diffuse flushing (red man syndrome- pretreat with antihistamines, not an allergic reaction and not a contraindication to use). Resistance by D-ala-D-ala to D-ala-D-lac

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mnemonic for 30S vs. 50s protease inhibitors

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buy AT 30, CCEl at 50
A = aminoglycosides
T = tetracyclines

C= chloramphenicol, clindamycin,
E = erythromycin
L = linezolid

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Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin

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Aminoglycosides
Mechanism- Bactericidal; inhibit formation of initiation complex and cause misreading of mRNA. Require O2 for uptake so are INEFFECTIVE against anaerobes.
Use- Severe GNR infections. Synergistic with Beta-lactam antibiotics. Use neomycin for bowel surgery.
Toxicity- Nephrotoxicity (esp with ceph), Ototoxicity (esp with loop diuretics), Teratogen, neuromuscular paralysis
Resistance- Transferase enymes inactivate by phosphorylation, acetylation, or adenylation.

Mean, GNATS canNOT kill anaerobes

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Tetracycline, Doxycycline, Demeclocycline, Minocycline

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Mechanism- Static; bind to 30S and prevent attachment of aminoacyl-tRNA; limited CNS penetration. Doxy is fecally eliminated and can be used in patients with renal failure. DON'T TAKE WITH DIVALENT cations - Milk, antacids, Fe (prevent absorption)
Use- Vibrio, Acne, Chlamydia, Ureaplasma, Urealyticum, Mycoplasma, Tularemia, H. pylori, Borellia burgdorferi, Rickettsia (can accumulate intracellularly)
Toxicity- GI distress, discoloration of teeth and inhibition of bone growth in children, photosensitivity. CX in pregnancy! Minocycline can cause blue pigmentation of skin
Resistance- Decreased uptake into cells or increased efflux out of cell by plasmid-endcoded transport pumps

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Erythromycin, Azithromycin, Clarithromycin

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Macrolides
Mechanism- Block translocation by binding 23S of the 50S ribosomal subunit. Static
Use- atypical pneumonia (mycoplasma, chlamydia, legionella), URIs, STDs, GPC, Neisseria
Toxicity- *Prolonged QT interval/ torsades (erythromycin), GI discomfort, acute cholestatic hepatitis,* eosinophilia, skin rashes. Increases serum concentration of theophyllines and oral anticoagulants
Resistance- Methylation of the 23S rRNA binding site

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Chloramphenicol

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Mechanism- Inhibits 50S peptidyltransferase activity. Static
Use- Meningitis (H. flu, Neisseria, S. pneumo).
Toxicity- Anemia, aplastic anemia, gray baby syndrome (lack liver UDP-glucuronyl transferase)
Resistance- Plasmid-encoded acetyltransferase inactivates drug

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Clindamycin

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Mechanism- Blocks peptide bond formation at 50S ribosomal subunit. Bacteriostatic
Use- ANAEROBIC (above diaphragm- B. fragilis, C. perfringes) in aspiration pneumonia
Toxicity- Pseudomembranous colitis, fever, diarrhea

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Sulfonamides (SMX, Sulfdiazine, fulfisoxazole)

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Mechanism- PABA antimetabolites that inhibit Dihydropteroate synthetase.
Use- Hypersensitivity, hemolysis if G6PD deficient, nephrotoxicity (TIN), photosensitivity, kernicterus in infants, displace other drugs from albumin (warfarin)
Resistance- altered enzyme, decreased uptake, increased PABA synthesis

Serum sickness Type III -> fibrinoid necrosis -> decreased C3

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trimethoprim

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Mechanism- Inhibits bacterial DHFR
Use- TMP-SMX used for UTIs, Shigella, Salmonella, PCP pneumonia, leprosy
Toxicity- Megalobastic anemia, leukopenia, granulocytopenia (alleviate with leucovorin rescue)

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Ciprofloxacin, norfloxacin, ofloxacin, sparfloxacin, moxifloxacin, gatifloxacin, enoxacin (fluoroquinolones), nalidoxic acid (quinolone)

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Mechanism- Inhibit DNA gyrase (Topo II). Cidal. Dont take with antacids.
Use- GNRs of UTI and GI tracts. PSEUDOMONAS, Neisseria, GP
Toxicity- GI upset, superinfections, rash, headache, dizziness, CX in pregnant women and children because damage to articular cartilage. Tendonitis and rupture in adults (dont run), leg cramps, myalgias
Resistance- Chromosome-encoded mutation in DNA gyrase

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Metronidazole

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Mechanism- Forms free radical toxic metabolites in the bacterial cell that damage DNA. Cidal, antiprotozoal
Use- Giardia, Entamoeba, Trichomonas, Gardnerella, ANAEROBES (below diaphragm), H. Pylori
Toxicity- *Disulfiram reaction with alcohol, headache, metallic taste,* parasthesias, dizziness, GI

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Polymyxins- Polymyxin B, Colistimethate (E)

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Mechanism- Bind to cell membranes of bacteria and disrupt their osmotic properties. Catatonic and act like detergents (basic).
Use- Resistance GN infections. ONLY TOPICAL, PSEUDOMONAS skin infections
Toxicity- Neurotoxicity, ATN

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Pyrazinamide

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Mechanism- Only effective in acidic pH of phagolysosomes where TB engulfed by macrophages is found.
Toxicity- Hepatotoxicity

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Ethambutol

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Mechanism- Decreases carbohydrate polymerization of mycobacterium cell wall by blocking arabinosyltransferase
Toxicity- Optic neuropathy

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Isoniazid

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Mechanism- Decreased synthesis of mycolic acids. Bacterial catalase-peroxidase needed to convert INH to active metabolite. Similar in structure to B6 (competes in the synthesis of GABA and increases B6 excretion). Different INH half-lives in fast vs. slow acetylators
Use- MTB. Can be used as solo prophylaxis if the person has no evidence of clinical disease.
Toxicity- Neurotoxicity (peripheral neuropathy- Prevent with pyridoxine, B6), hepatotoxicity, lupus.

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Rifampin

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Mechanism- Inhibits DNA-dependent RNAP
Use- MTb, delays resistance to dapsone for leprosy, meningococcal prophylaxis and chemoprophylaxis in contacts of children with H. flu
Toxcity- Increases P450, *orange body fluids*

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Amphotericin B

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Mechanism- Binds ergosterol and forms membrane pores to allow leakage of electrolytes.
Use- Serious systemic mycoses, Crypto, Blasto, Cocci, Aspergillus, Histo, Candida, Mucor. Intrathecally for funal meningitis (does not cross BBB)
Toxicity- Fever/chills, hypotension, nephrotoxicity (dec GFR- hydration reduces this), arrhythmias (dec K and Mg), anemia, IV phlebitis. Liposomal Amphotericin B reduces toxicity.
can be used with flucytosine for cryptococcal meningitis

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Nystatin

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Mechanism- Same as Amphotericin B. Used topically because it is too toxic for systemic use. (No-a-statin)
Use- Swish and swallow for oral candidiasis, topical for diaper rash or vaginal candidiasis

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Fluconazole, ketoconazole, clotrimazole, micronazole, itraconazole, voriconazole

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Azoles
Mechanism- Inhibit fungal sterol synthesis by inhibiting the P450 enzyme that converts lanosterol to ergosterol.
Use- Systemic mycoses: fluconazole for crypo meningitis and candidal infections. Ketoconazole for blasto, cocci, histo, candida albicans, HYPERCORTISOLISM (inhibits desmolase). Clotrimazole and miconazole for topical fungal infections. Itraconazole for Sporothrix.
Toxicity- Hormone synthesis inhibition (gynecomastia), liver dysfunction (inhibits P450), fever, chills

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Flucytosine

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Mechanism- inhibits DNA/RNA synthesis by conversion to 5-FU.
Use- Systemic fungal infections (candida, crypto) + amphotericin B
Toxicity- N/V/D, BM suppression

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Caspofungin

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Mechanism- inhibits cell wall synthesis by inhibiting synthesis of beta-glucan
Use- Invasive asperillosis
Toxicity- GI, flushing

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Terbinafine

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Mechanism- Inhibits squalene epoxidase -> squalene toxic to fungi
Use- Determatophytoses (ESP onchomycosis)

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Griseofulvin

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Mechanism- Interferes with microtubules function to disrupt mitosis. Deposits in keratin containing tissues (nails).
Use- Oral for superficial infections; dermatophytes (tinea, ringworm) - grisely-o-falvin because of toxicity
Toxicity- Teratogenic, carcinogenic, confusion , headaches, increases P450 and warfarin metabolism

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Rimantadine

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Mechanism- Blocks penetration/uncoating (M2) and causes DA release from intact nerve terminals
Use- Prophylaxis and treatment for influenza A ONLY; PD
Toxicity- Ataxia, dizziness, slurred speech, anticholinergic
Resistance- Mutated M2 protein (% influenza A are resistant)
RIMANTIDINE has fewer side effects, but doesnt cross BBB (cant use for PD)

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Zanamivir, oseltamivir

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Mechanism- Inhibit influenzae neuraminidase to decrease the progeny
Use- Influenza A and B, H1N1, H5N1

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Ribavirin

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Mechanism- Inhibits synthesis of guanine nucleotides by competitively inhibiting IMP DH
Use- RSV, chronic hepatitis C
Toxicity- Hemolytic anemia, Severe teratogen (inhaled powder concern for people handling on Step)

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Acyclovir

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Mechanism- Monophosphorylated by HSV/VZV thymidine kinase and acts as a guanosine analog. Cellular enzymes create triphosphate. Inhibits viral DNA polymerase by chain termination
Use- VZV (use famciclovir), HSV, EBV. No effect on latent forms of VZV and HSV
Resistance- lack of viral TK
Toxicity: rarely nephrotoxicity

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Ganciclovir

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Mechanism- 5'-monophosphate formed by a CMV viral kinase or HSV/VZV TK. Guanosine analog. Triphosphate formed by cellular kinase. Inhibits viral DNAP.
Use- CMV (esp in IC patients)
Toxicity- Leukopenia, neutropenia, thrombocytopenia, renal toxicity.
Resistance- Mutated CMV DNAP or lack of viral kinase
Valganciclovir is a prodrug of ganciclovir and has better oral bioavailability

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Foscarnet

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Mechanism- DOES NOT REQUIRE ACTIVATION BY VIRAL KINASE. Inhibits viral DNAP by binding to pyrophosphate site
Use- CMV retinitis when ganciclovir fails.
Resistance- mutated DNAP

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-navir

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HIV Protease inhibitors
Mechanism- Inhibits protease, which cleaves the polypeptide products of HIV mRNA into their functional parts. So maturation of new viruses is halted
Toxicity- Hyperglycemia, GI, lipodystrophy, thrombocytopenia (indinavir), inhibits P450, pancreatitis (Ritonavir), nephrolithiasis (indinavir)

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Zidovudine (ZDV/AZT), Didanosine, Zalcitabine, Stavudine, Lamivudine, Abacavir

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Mechanism- Competitively inhibit nucleotide binding to RT and terminate the DNA chain (lack 3'OH group). Need to be phosphorylated by TK. ZDV for pregnancy
Toxicity- Hypersensitivity (Abacavir), BM suppression (reversed with G-CSF and EPO), peripheral neuropathy (Didanosine, stavudine, zalcitabine), lactic acidosis, megaloblastic anemia (ZDV), GI, hepatic steatosis (didanosine, stavudine)

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Nevirapine, Efavirenz, Declaviridine

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Mechanism- Bind to RT at a site different from NRTIs. DO NOT REQUIRE P-ATION
Toxicity- BM suppression (reversed with G-CSF and EPO), peripheral neuropathy, rash, GI, false positive for cannabinoids and confusion (efavirenz)

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Enfuvirtide

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Mechanism- Bind gp41 to inhibition conformational change required for fusion with CD4 cells, blocking entry and replication. Used in patients with persistent viral replication despite antiretroviral therapy.
Toxicity- Hypersensitivity, reactions at subcutaneous injection site, increased risk of bacterial pneumonia

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Raltegravir

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Integrase inhibitor preventing HIV genome integration

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Cidofovir

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Mech: inhibits viral DNA polymerase- does not require phosphorylation
uses: CMV retinitis
toxicity: nephrotoxicity

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Antibiotics to avoid in pregnancy

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Countless SAFE Momes Take Really Good Care
Clarithromycin -embryotoxic
Sulfonamides - kernicterus
Aminoglycosides- ototoxicity
Fluoroquinolones- caritlage damage
Metronidazoles - mutagenic
Tetracyclines - discolored teeth, inhibition of bone growth
Ribavirin - teratogenic
Griseofulvin - teratogenic
Chloramphenicol - "gray baby"

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Interferons

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Glycoproteins to block replication of RNA and DNA
IFN-alpha chronic HepB/C, Kaposi's sarcoma
IFN-beta - MS
IGN-gamma - NADPH deficiency (chronic granulomatous disease)

toxicity is neutropenia

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Chloroquine

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Blocks plasmodium heme polymerase
toxicity - retinopathy, G6PD hemolysis

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Antihelminth therapy

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Bendazoles - increase glucose uptake
Pyrantel pamoate - nicotinic receptor agonist paralyzes worm
Ivermectin - increases GABA transmission paralyzes wrom
Praziquantel - increase Ca influx