Anti-bacterial agents

Headshot of Joanna Breems, MD, FACP · Clinical Assistant Professor
Joanna Breems
MD, FACP · Clinical Assistant Professor
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Table of Contents

Penicillin beta-lactams

Penicillin (PCN)

  • Class(es)

    Penicillins/Beta-Lactams.

  • Clinical use(s)

    FDA approved: Syphilis, anthrax, listeria infections, meningococcal infections, pasteurella, serious gram-positive infections.
    Off-label/clinical use: CAP (children), group B strep, osteomyelitis, SSTI.

  • Mechanism(s) of action

    Bactericidal.
    Inhibits bacterial cell wall synthesis during active multiplication.

  • Key adverse effects

    Nausea, vomiting, diarrhea, seizure (rare).

  • Key drug/food interactions

    Tetracyclines (may ↓ effectiveness)
    Food (may ↓ peak penicillin concentrations)

  • Special considerations

    Renally adjusted: CrCl < 10 ml/min.

Amoxicillin (Amoxil)

  • Class(es)

    Penicillins/Beta-lactam antibiotic

  • Clinical use(s)

    FDA approved: Ear, nose and throat bacterial infection, skin and soft tissue infection
    Off-label/clinical use: Uncomplicated acute otitis media

  • Mechanism(s) of action

    Binds penicillin binding protein, which prevents cell wall synthesis

  • Key adverse effects

    Allergy (~10%), N/V/D (>1%)

  • Key drug/food interactions

    Concurrent use of PENICILLINS and TETRACYCLINES may decrease effectiveness.

  • Special considerations

    Available in oral form only. Contraindicated in serious hypersensitivity reactions to Beta Lactam antibiotics. Cross-sensitivity with cephalosporin antibiotics has been reported to be between .2% and 10%.

Ampicillin

  • Class(es)

    Penicillins/Beta-Lactams

  • Clinical use(s)

    FDA approved: Bacterial meningitis, gonorrhea, endocarditis, respiratory tract infection, sepsis, genitourinary/digestive tract infections.
    Off-label/clinical use: Bacterial endocarditis (prophylaxis), bacteremia associated with IV line.

  • Mechanism(s) of action

    Bactericidal.
    Inhibits cell wall synthesis by binding to one or more penicillin-binding proteins (PBPs).

  • Key adverse effects

    Diarrhea, anaphylaxis.

  • Key drug/food interactions

    Tetracyclines, bupropion/donepezil (lowers seizure threshold).

  • Special considerations

    Rapid infusion may cause seizures.
    Renally adjusted: CrCl < 50 ml/min.

Dicloxacillin (Dynapen)

  • Class(es)

    Penicillins/Beta-Lactams

  • Clinical use(s)

    FDA approved: Infection due to staph aureus (MSSA).
    Off-label/clinical use: Impetigo, SSTI.

  • Mechanism(s) of action

    Bactericidal.
    Inhibits cell wall synthesis by binding to one or more penicillin-binding proteins (PBPs).

  • Key adverse effects

    Neurotoxicity (high doses), hypokalemia, bone marrow suppression, diarrhea

  • Key drug/food interactions

    Tetracylines, bupropion/donepezil (lowers seizure threshold), Food (may ↓ dicloxacillin concentrations)

  • Special considerations

    CYP3A4 inducer

Nafcillin (Nafcil, Nallpen)

  • Class(es)

    Pencillins/Beta-Lactams

  • Clinical use(s)

    FDA approved: Confirmed MSSA—meningitis, endocarditis.
    Off-label/clinical use: Skin/soft tissue necrotizing infection, streptococcal skin infection, surgical site infection, catheter-related bacteremia.

  • Mechanism(s) of action

    Bactericidal.
    Inhibits cell wall synthesis by binding to one or more penicillin-binding proteins (PBPs).

  • Key adverse effects

    Neurotoxicity (high doses), hypokalemia, bone marrow suppression, diarrhea.

  • Key drug/food interactions

    Fentanyl, cyclosporine, tetracylines, Food (may ↓ nafcillin concentrations).

  • Special considerations

    CYP3A4 inducer.
    Dose adjust for severe renal and hepatic impairment.

Amoxicillin/Clavulanate (Augmentin)

  • Class(es)

    Aminopenicillins beta lactamase inhibitors

  • Clinical use(s)

    FDA approved: Acute otitis media, CAP, impetigo, SSTI, LRTI, sinusitis, UTI  
    Off-label/clinical use: Febrile neutropenia, streptococcal pharyngitis.

  • Mechanism(s) of action

    Amoxicillin: Inhibits bacterial cell wall synthesis by binding to one or more of the penicillin-binding proteins (PBPs).
    Clavulanic acid: Inactivates beta-lactamase enzymes.

  • Key adverse effects

    Diarrhea, nausea, vomiting

  • Key drug/food interactions

    Tetracyclines

  • Special considerations

    Renally adjusted: CrCl < 30 ml/min.
    Do not use ER and 875 mg tablet in HD patients and CrCl < 30 ml/min.
    Take with food.

Piperacillin/Tazobactam (Zosyn)

  • Class(es)

    Extended Spectrum Pencillins/Beta-Lactams.

  • Clinical use(s)

    FDA approved: Appendicitis, CAP/HAP, SSTI, pelvic inflammatory disease, peritonitis, puerperal endometritis.
    Off-label/clinical use: Bacteremia associated with IV line, febrile neutropenia, infectious disease of abdomen.

  • Mechanism(s) of action

    Piperacillin: Inhibits bacterial cell wall synthesis by binding to one or more of the penicillin-binding proteins (PBPs). Tazobactam: Inhibits many beta-lactamases.

  • Key adverse effects

    Diarrhea, nausea, headache, neutropenia.

  • Key drug/food interactions

    Tetracycline, vancomycin (↑ risk AKI).

  • Special considerations

    Renally adjusted: CrCl < 40 ml/min.

Meropenem (Merrem)

  • Class(es)

    Carbapenem.

  • Clinical use(s)

    FDA approved: Bacterial meningitis, SSTI, infection of the abdomen.
    Off-label/clinical use: Bacteremia associated w/ IV line, cystic fibrosis, febrile neutropenia, HAP.

  • Mechanism(s) of action

    Exerts bactericidal activity by inhibiting cell wall synthesis by penetrating the cell wall of most gram-positive and gram-negative bacteria to reach penicillin-binding–protein (PBP) targets.

  • Key adverse effects

    Diarrhea, N/V, rash, anemia, headache.

  • Key drug/food interactions

    Valproic acid, cholera vaccine, live typhoid vaccine, probenecid.

  • Special considerations

    Injection only.
    Renal impairment: CrCl <50 ml/min—dose adjust.

Aztreonam (Azactam)

  • Class(es)

    Monobactam.

  • Clinical use(s)

    FDA approved: Cystic fibrosis, disease w/ Gram negative bacteria, endometritis, female genital infection, SSTI, LRTI, peritonitis, sepsis, UTI.
    Off-label/clinical use: Meningitis, musculoskeletal infection, febrile neutropenia, gonorrhea, post-op prophylaxis, traveler’s diarrhea.

  • Mechanism(s) of action

    Bactericidal against gram-negative aerobic bacteria by binding to penicillin-binding protein-3(PBP-3), which results in inhibition of bacterial cell wall synthesis.

  • Key adverse effects

    Chest discomfort, ALT/AST elevation, SCr elevation, cough, congestion.

  • Key drug/food interactions

    Cholera vaccine.

  • Special considerations

    Injection and inhalation routes.
    Renal impairment: CrCl <30 ml/min—dose adjust.

Cephalosporins

Cephalexin (Keflex)

  • Class(es)

    1st-generation cephalosporin

  • Clinical use(s)

    FDA approved: Skin and soft tissue infection, osteomyelitis.
    Off-label/clinical use: Prophylaxis for bacterial endocarditis.

  • Mechanism(s) of action

    Binds to penicillin binding proteins in cell wall membrane.

  • Key adverse effects

    C. diff–associated diarrhea (CDAD), seizures (high doses especially in renal impairment)

  • Key drug/food interactions

    Concurrent use of loop diuretics or aminoglycosides may increase risk of renal toxicity.

  • Special considerations

    Can be taken with or without food. Taking cephalexin with food may decrease GI irritation. Available only in oral form (capsules, tablets, oral suspension).

Cefazolin (Ancef)

  • Class(es)

    1st-generation cephalosporin

  • Clinical use(s)

    FDA approved: Respiratory tract infections, endocarditis, intra-abdominal infections.
    Off-label/clinical use: Bacteremia associated with IV line, bacterial endocarditis (prophylaxis).

  • Mechanism(s) of action

    Bactericidal.
    Inhibits cell wall synthesis by binding to one or more penicillin-binding proteins (PBPs).

  • Key adverse effects

    Diarrhea, pruritis, anaphylaxis, Stevens-Johnson syndrome.

  • Key drug/food interactions

    Warfarin (may ↑ risk bleeding).

  • Special considerations

    Renally adjusted: CrCl < 54 ml/min. Available as injectable only.

Cefotaxime (Claforan)

  • Class(es)

    3rd-generation cephalosporin

  • Clinical use(s)

    FDA approved: Bacterial meningitis, bone/joint infections, intra-abdominal infections, LRTI, SSTI.
    Off-label/clinical use: Bacterial endocarditis, Lyme disease, salmonella.

  • Mechanism(s) of action

    Bactericidal.
    Inhibits cell wall synthesis by binding to one or more penicillin-binding proteins (PBPs).

  • Key adverse effects

    Diarrhea, vomiting, hypersensitivity.

  • Key drug/food interactions

    Warfarin (may ↑ risk bleeding).

  • Special considerations

    Renally adjusted: CrCl < 20 ml/min.

Cefdinir (Omnicef)

  • Class(es)

    3rd-generation cephalosporin

  • Clinical use(s)

    FDA approved: Acute bacterial otitis media, acute exacerbation chronic bronchitis, acute maxillary sinusitis, CAP, pharyngitis/tonsillitis, SSTI.
    Off-label/clinical use: Cystitis.

  • Mechanism(s) of action

    Bactericidal.
    Inhibits cell wall synthesis by binding to one or more penicillin-binding proteins (PBPs).

  • Key adverse effects

    Diarrhea, nausea.

  • Key drug/food interactions

    Warfarin (may ↑ risk bleeding).

  • Special considerations

    Renally adjusted: CrCl < 30 ml/min.
    Administer at least 2 hours before or after antacids/iron supplements.

Ceftriaxone (Rocephin)

  • Class(es)

    3rd-generation cephalosporin

  • Clinical use(s)

    FDA approved: Acute otitis media, bacterial meningitis, upper/lower respiratory tract infection, UTI.
    Off-label/clinical use: Syphillus, endocarditis.

  • Mechanism(s) of action

    Bactericidal.
    Inhibits cell wall synthesis by binding to one or more penicillin-binding proteins (PBPs)

  • Key adverse effects

    Diarrhea, hypersensitivity reaction, eosinophilia.

  • Key drug/food interactions

    Calcium-containing products.

  • Special considerations

    Calcium products precipitate ceftriaxone.
    Avoid in neonates.
    Combined renal/hepatic impairment: NTE 2 grams/day.

Ceftazidime (Fortaz)

  • Class(es)

    3rd-generation cephalosporin

  • Clinical use(s)

    FDA approved: Bacterial meningitis, bacterial sepsis, pneumonia, SSTI, osteomyelitis, LRTI, UTI.
    Off-label/clinical use: Bacterial endocarditis, chronic purulent otitis media.

  • Mechanism(s) of action

    Bactericidal.
    Inhibits cell wall synthesis by binding to one or more penicillin-binding proteins (PBPs).

  • Key adverse effects

    Diarrhea, anaphylaxis.

  • Key drug/food interactions

    Warfarin (may ↑ risk bleeding).

  • Special considerations

    Renally adjusted: CrCl < 50 ml/min.

Cefepime (Maxipime)

  • Class(es)

    4th-generation cephalosporin

  • Clinical use(s)

    FDA approved: Pneumonia, SSTI (uncomplicated), infectious disease of abdomen.
    Off-label/clinical use: Bacterial meningitis, infective endocarditis, peritoneal dialysis-associated peritonitis.

  • Mechanism(s) of action

    Bactericidal.
    Inhibits cell wall synthesis by binding to one or more penicillin-binding proteins (PBPs).

  • Key adverse effects

    Direct positive Coombs test, diarrhea.

  • Key drug/food interactions

    Warfarin (may ↑ risk bleeding).

  • Special considerations

    Renally adjusted: CrCl < 60 ml/min.

Other antibiotics

Clindamycin (Cleocin)

  • Class(es)

    Lincosamide

  • Clinical use(s)

    FDA approved: Bacterial disease (severe) Including susceptible infections due to anaerobic and aerobic gram positive organisms.
    Off-label/clinical use: Acne vulgaris (topical).

  • Mechanism(s) of action

    Inhibits protein synthesis at the level of the 50S ribosomal subunit.

  • Key adverse effects

    The most common reported AE is mild to moderate morbilliform-like skin rashes. High risk antibiotic for C. difficile associated diarrhea.

  • Key drug/food interactions

    Concurrent use of clindamycin and erythromycin may result in antagonistic antimicrobial effects.

  • Special considerations

    Patient should take capsules with a full glass of water to avoid esophageal irritation.

Metronidazole (Flagyl)

  • Class(es)

    Antiprotozoal, antibacterial and antihelminthic nitroimidazole agent

  • Clinical use(s)

    FDA approved: Infection due to anaerobic bacteria, trichomoniasis, bacterial vaginosis.
    Off-label/clinical use: Crohn's disease.

  • Mechanism(s) of action

    Bacteriocidal against anaerobes by hindering the DNA processes.

  • Key adverse effects

    Headache (5–18%), vaginitis (10–15%).

  • Key drug/food interactions

    Contraindications: Alcohol use during and for at least 3 days after metronidazole use. Disulfiram use within 2 weeks of therapy. Significantly increased risk of bleed with warfarin therapy.

  • Special considerations

    U.S. boxed warning: Metronidazole has been shown to be carcinogenic in mice and rats. Its use, therefore, should be reserved only for conditions for which it is approved. 

Doxycycline (Oracea)

  • Class(es)

    Tetracycline

  • Clinical use(s)

    FDA approved: Gram-negative infections (E. coli, Enterobacter aerogenes, Shigella spp., Acinetobacter spp., Klebsiella spp., bacteroides spp., Neisseria menginitidis); gram-positive infections (Streptococcus spp.).
    Off-label/clinical use: Cellulitis, bite-wound infection.

  • Mechanism(s) of action

    Inhibits protein synthesis by binding with the 30S and possibly 50S ribosomal subunit(s) of susceptible bacteria.

  • Key adverse effects

    Photosensitivity, diarrhea, nasopharyngitis.

  • Key drug/food interactions

    Penicillin, acitretin, methotrexate; food may decrease absorption.

  • Special considerations

    Take on empty stomach unless GI irritation occurs.

Vancomycin (Vancocin)

  • Class(es)

    Glycopeptide

  • Clinical use(s)

    FDA approved: C. difficile diarrhea, skin and soft tissue infection, infective endocarditis.
    Off-label/clinical use: Bacteremia.

  • Mechanism(s) of action

    Inhibits bacterial cell wall synthesis by blocking glycopeptide polymerization of the cell wall.

  • Key adverse effects

    Red man syndrome, nephrotoxicity, hyperkalemia, hypotension (accompanied by flushing).

  • Key drug/food interactions

    Aminoglycosides may enhance the nephrotoxic effect of vancomycin.

  • Special considerations

    Available in IV form for systemic infections. Systemic dosing is based on patient weight and renal function. Available in oral form for use in C. difficile diarrhea treatment.

Linezolid (Zyvox)

  • Class(es)

    Oxazolidinone

  • Clinical use(s)

    FDA approved: CAP, HAP, SSTI, VRE infection.
    Off-label/clinical use: Bacteremia associated with IV line, febrile neutropenia, infection of bone, infections disorder of joint, endocarditis.

  • Mechanism(s) of action

    Inhibits bacterial reproduction of aerobic gram-positive bacteria and certain gram-negative and anaerobic bacteria, by selectively binding to a site on the 23S ribosomal RNA of the 50S subunit, thereby preventing initiation complex formation with the 70S ribosomal subunit.

  • Key adverse effects

    Diarrhea, N/V.

  • Key drug/food interactions

    MAOIs, SSRIs, mirtazapine, carbidopa/levodopa.
    Avocado, bitter orange, tyramine containing foods.

  • Special considerations

    Injection only.
    Bacteriostatic against enterococci and staphylococci, and bactericidal for a majority of streptococci isolates.

Daptomycin (Cubicin)

  • Class(es)

    Cyclic lipopeptide

  • Clinical use(s)

    FDA approved: Bacteremia due to S. aureus, SSTI.
    Off-label/clinical use: Bacteremia associated with IV line, disease due to Gram positive bacteria, osteomyelitis, septic arthritis.

  • Mechanism(s) of action

    Binds to bacterial cell membranes and causes cell death by inducing rapid depolarization of the membrane potential, leading to disruption of DNA, RNA, and protein synthesis.

  • Key adverse effects

    Pruritis, rash, diarrhea, vomiting, insomnia.

  • Key drug/food interactions

    HMG CoA reductase inhibitors.

  • Special considerations

    Injection only.
    Renal impairment: CrCl <30 ml/min.—dose adjust.

Sulfamethoxazole-Trimethoprim (Bactrim)

  • Class(es)

    Sulfonamide antibiotic

  • Clinical use(s)

    FDA approved: Urinary tract infection, acute exacerbation of COPD.
    Off-label/clinical use: UTI prophylaxis.

  • Mechanism(s) of action

    Interferes with the production of folic acid.

  • Key adverse effects

    Urticaria, anorexia, N/V, hepatotoxcity (rare).

  • Key drug/food interactions

    Concurrent use with potassium-sparing drugs may result in increased risk of hyperkalemia. Concurrent use with warfarin significantly increases risk of bleed.

  • Special considerations

    For IV formulation, do not administer by IM injection, bolus, or rapid infusion.

Nitrofurantoin (Macrodantin, Macrobid)

  • Class(es)

    Nitrofurans

  • Clinical use(s)

    FDA approved: UTI treatment and prophylaxis.

  • Mechanism(s) of action

    Nitrofurantoin is reduced by bacterial flavoproteins to reactive intermediates, which inactivate or alter bacterial ribosomal proteins and other macromolecules.

  • Key adverse effects

    Common: Skin eruptions, consisting of macular lesions, maculopapular lesions, or urticarial lesions. The most common reaction in pediatric patients was peripheral polyneuropathy.

  • Key drug/food interactions

    Concurrent use of NITROFURANTOIN and FLUCONAZOLE may result in increased risk of hepatic and pulmonary toxicity.

  • Special considerations

    Contraindicated for CrCl < 60 ml/min. Limited data suggests it’s safe and effective down to CrCl = 30 ml/min.

Fosfomycin (Monurol)

  • Class(es)

    Phosphonic acid derivative

  • Clinical use(s)

    FDA approved: Uncomplicated UTI.
    Off-label/clinical use: Complicated UTI.

  • Mechanism(s) of action

    As a phosphonic acid derivative, fosfomycin inhibits bacterial wall synthesis (bactericidal) by inactivating the enzyme, pyruvyl transferase, which is critical in the synthesis of cell walls by bacteria.

  • Key adverse effects

    Diarrhea, nausea, headache.

  • Key drug/food interactions

    Cholera vaccine, lixisenatide.

  • Special considerations

    Supplied as powder for oral solution.

Gentamicin

  • Class(es)

    Aminoglycoside

  • Clinical use(s)

    FDA approved: Ophthalmic infections (eye drops), dermatologic infections (topical), infective endocarditis (systemic), synergy for gram-positive infections (systemic).
    Off-label/clinical use: Adjunctive therapy for febrile neutropenia, pelvic inflammatory disease.

  • Mechanism(s) of action

    Inhibits protein synthesis in bacteria at the level of the 30S ribosome.

  • Key adverse effects

    CNS: Ataxia, vertigo.
    EENT: Ototoxicity.
    GU: Nephrotoxicity.

  • Key drug/food interactions

    Loop diuretics increase incidence of ototoxicity.

  • Special considerations

    US Boxed Warning: May cause nephrotoxicity.
    US Boxed Warning: May cause neurotoxicity.
    Monitor patient’s renal function throughout therapy.

Ciprofloxacin (Cipro)

  • Class(es)

    Fluoroquinolone

  • Clinical use(s)

    FDA approved: Treatment of cystitis and pyelonephritis.

  • Mechanism(s) of action

    Inhibits nucleic acid synthesis via inhibition of DNA gyrase.

  • Key adverse effects

    Tendon rupture, C Difficile colitis.

  • Key drug/food interactions

    Contraindicated with strong CYP3A4 inhibitors and QT prolonging agents. Significantly increased risk of bleed with warfarin therapy.

  • Special considerations

    Available in systemic, ophthalmic, and otic forms. The FDA advises that the serious side effects associated with fluoroquinolones generally outweigh the benefits for patients with acute sinusitis, acute bronchitis, and uncomplicated urinary tract infections who have other treatment options.

Levofloxacin (Levaquin)

  • Class(es)

    Fluoroquinolone

  • Clinical use(s)

    FDA approved: CAP/HAP, complicated UTI, pyelonephritis, SSTI.
    Off-label/clinical use: Acute otitis media (recurrent), chlamydial infection, traveler’s diarrhea, tuberculosis.

  • Mechanism(s) of action

    Inhibits DNA-gyrase in susceptible organisms thereby inhibits relaxation of supercoiled DNA and promotes breakage of DNA strands.

  • Key adverse effects

    Diarrhea, headache, nausea, tendon rupture (rare).

  • Key drug/food interactions

    Avoid concurrent use QT prolonging medications, Warfarin (may ↑ risk bleeding).

  • Special considerations

    Risk of QT prolongation.
    Renally adjusted: CrCl < 49 ml/min.
    BBW: tendonitis/tendon rupture/peripheral neuropathy/CNS effects.

Clarithromycin (Biaxin)

  • Class(es)

    Macrolide

  • Clinical use(s)

    FDA approved: Bronchitis, AOM, CAP, Mycobacterium avium, SSTI, sinusitis, streptococcal pharyngitis.
    Off-label/clinical use: Anthrax, endocarditis prophylaxis, LRTI, legionnaires, Lyme disease, pertussis, spotted fevers.

  • Mechanism(s) of action

    Clarithromycin binds to the 50S ribosomal subunit of the 70S ribosome of susceptible organisms, thereby inhibiting bacterial RNA-dependent protein synthesis.

  • Key adverse effects

    Taste disturbance, N/V, diarrhea.

  • Key drug/food interactions

    Significant bleed risk with concurrent warfarin therapy. Concomitant use with HMG-CoA reductase inhibitors extensively metabolized by CYP3A4 (eg, lovastatin or simvastatin) contraindicated.

  • Special considerations

    Renal impairment: CrCl <30 ml/min.—dose adjust.

Azithromycin (Zithromax)

  • Class(es)

    Macrolide antibiotic

  • Clinical use(s)

    FDA approved: Acute otitis media (ophthalmic), community acquired pneumonia (oral or IV for inpatient).
    Off-label/clinical use: Bacterial endocarditis prophylaxis.

  • Mechanism(s) of action

    Inhibits protein synthesis at the level of the 50S ribosomal subunit.

  • Key adverse effects

    Injection site reaction (~6%), increased liver enzymes (~6%), QT interval prolongation.

  • Key drug/food interactions

    Avoid concomitant use with other QT prolonging agents. Increased risk of bleed with warfarin.

  • Special considerations

    Use contraindicated in patients with hepatic dysfunction. Separate oral administration from aluminum- or magnesium-containing antacids or decrease absorption may occur.

Antituberculars

Isoniazid (INH, Nydrazid)

  • Class(es)

    Antitubercular agent.

  • Clinical use(s)

    FDA approved: Active tuberculosis (HIV and non-HIV); inactive tuberculosis (HIV and non-HIV).
    Off-label/clinical use: Atypical mycobacterial infection; determination of acetylation rate.

  • Mechanism(s) of action

    Bactericidal.
    Inhibits synthesis of mycoloic acids, an essential component of the bacterial cell wall.

  • Key adverse effects

    Increased liver enzymes, neuropathy, neurotoxicity.

  • Key drug/food interactions

    Acetaminophen: ↑ risk hepatotoxicity.
    Food: ↓ bioavailabilty.

  • Special considerations

    Avoid administration with food.
    Use caution in severe renal/hepatic impairment.
    BBW: Hepatitis.

Pyrazinamide(PZD)

  • Class(es)

    Nicotinamide analogue, antitubercular agent.

  • Clinical use(s)

    FDA approved: Tuberculosis.
    Off-label/clinical use:

  • Mechanism(s) of action

    Bacteriostatic/bactericidal.
    Converted to pyrazinoic acid in susceptible strains of Mycobacterium which lowers pH of environment (exact mechanism unknown).

  • Key adverse effects

    Hyperuricemia, N/V, Arthralgia.

  • Key drug/food interactions

    Rifampin: Severe hepatic impairment.

  • Special considerations

    Renally adjusted: CrCl < 30 ml/min.

Ethambutol (Myambutol)

  • Class(es)

    Antitubercular agent.

  • Clinical use(s)

    FDA approved: Pulmonary tuberculosis (adjunct).
    Off-label/clinical use: Tuberculosis meningitis, MAC, nontuberculosis mycobacterial disease (M. kansasii).

  • Mechanism(s) of action

    It inhibits the synthesis of metabolites, subsequently impairing cell metabolism and cell multiplication eventually leading to cell death.

  • Key adverse effects

    Hepatotoxicity, anaphylaxis, optic neuritis.

  • Key drug/food interactions

    Aluminum-containing antacids (↓ serum concentrations of Ethambutol).

  • Special considerations

    Renally adjusted: CrCl < 30 ml/min.

Rifampin (Rifadin)

  • Class(es)

    Rifamycins, antitubercular agent.

  • Clinical use(s)

    FDA approved: Active or latent TB, meningococcal carriers.
    Off-label/clinical use: Endocarditis (prosthetic valve), osteomylitis.

  • Mechanism(s) of action

    Inhibits RNA synthesis by blocking RNA transcription.

  • Key adverse effects

    EENT: red discoloration of tears; GI: N/C, diarrhea, flatulence; GU: red urine.

  • Key drug/food interactions

    Rifampin stimulates liver enzymes, which may increase the metabolism and decrease the effectiveness of many other drugs.

  • Special considerations

    Part of a four drug regimen for the treatment of active TB (rifampin + isoniazid + pyrazinamide + ethambutol). Has activity against organisms which create biofilms.