-
Inhibitor of murein polymer synthesis
Blocks Transglycosidase
Active against MRSA
First Choice for treating skin and soft tissue infections
Effective for treating pseudomembraneous colitis
Mutation at the D-Ala-D-Ala binding site leads to resistance against this drug
- Vancomycin
- Teicoplanin
- Tanclopenin
-
Natural penicillin
Treat infections caused by spirochetes (Treponema pallidum)
Used to treat syphilis
Most staphylococci and gonococci and some strains of pneumococci are now resistant to this drug
Penicillin G
-
Treat penicillin-resistant strains of staphylococci that elaborate penicillinase (B-lactamase)
They are not effective against MRSA
Penicillinase-resistant penicillins:
- Cloxacillin
- Dicloxacillin
- Nafcillin
- Oxacillin
-
Combined with a B-lactamase inhibitor
Active against Listeria monocytogenes and is used to treat meningitis
Can be combined with an aminoglycoside for the treatment of serious enterococall infections, such as enterococcal endocarditis
Ampicillin: an Aminopenicillin
-
Combined with a B-lactamase inhibitor
This drug specifically is used for prophylaxis of bacterial endocarditis in persons with heart valve defects.
Amoxicillin: an Aminopenicillin
-
Used to treat some strains of Pseudomonas aeruginosa
This drug can be combined with a B-lactamase inhibitor for the treatment of patients with intra-abdominal, skin and soft tissue, lower respiratory tract, complicated urinary tract, and gynecologic infections as well as febrile neutropenia
Antiseudomonal penicillins:
-
Enter CNS and are agents used in the treatment of meningitis
Used as a single-dose treatment for gonorrhea
3rd Generation Cephalosporins:
- Cefotaxime: renal tubular excretion
- Ceftriaxone (excreted in bile): used in patients with renal insufficiency
-
Advanced generation of Cephalosporin
Effective against MRSA
High affinity to PBPa2, a MRSA-specific PBP that has low affinity for other beta-lactam
drugs
Used for treating skin and soft tissue infection and community-acquired pneumonia
Ceftaroline
-
It is active against many aerobic G- bacteria
It lacks activity against G+ organism and anaerobes
Rarely shows cross-sensitivity with penicillins and cephalosporins and can usually be used in person allergic to other B-lactam antibiotics
Aztreonam
-
Used to treat a wide range of systemic infections, including endocarditis, pneumonia, urinary tract, pelvic, skin and soft tissue, and intra-abdominal infections
Carbapenems:
- Doripenem
- Ertapenem
- Imipenem/Cilastatin
- Meropenem
-
B-lactam drugs that inhibit molecular class A B-lactamases
These drugs have no antimicrobial activity by themselves but serve as surrogate substrates for B-lactamases when given with a penicillin antibiotic
Beta-lactamase inhibitors:
- Clavulanate
- Sulbactam
- Tazobactam
-
Drugs used in the inhibition of bacterial cell-wall synthesis
- Penicillins
- Cephalosporins
- Imipenem/Meropenem
- Aztreonam
- Vancomycin
-
Drugs used in the inhibition of bacterial protein synthesis
- Aminoglycosides
- Chloramphenicol
- Macrolides
- Tetracyclines
- Streptogramins
- Linezolid
-
Drugs used to inhibit nucleic synthesis
-
Drugs that inhibit folic acid synthesis
- Sulfonamides
- Trimethoprim
- Pyrimethamine
-
Penicillin used to treat Listeria monocytogenes
Ampicillin
-
Penicillin used to treat Borrelia burgdorferi
Amoxicillin
-
Penicillin used to treat H. pylori
Amoxicillin
-
Cephalosporins act very similar to Penicillins but they do not cover which organisms?
LAME
- Listeria monocytogenes
- Atypicals (Chlamydia, Mycoplasma)
- MRSA
- Enterococci
-
What is given with cilastatin, a renal dehydropeptidase inhibitor?
Imipenem
-
Which Aminoglycoside is used to treat tubercolosis?
Streptomycin
-
Which antibacterial agents should not be used during pregnancy?
- Aminoglycosides
- Fluoroquinolones
- Sulfonamides
- Tetracyclines
-
What folic acid inhibitor is generally used to treat urinary tract infections?
Sulfonamides
-
Antibacterial agent that is a direct inhibitor of nucleic acid synthesis?
Quinolones inhibit topoisomerase II (DNA gyrase)
-
What are the primary anti-tubercular drugs?
- Isoniazid
- Rifampin
- Ethambutol
- Pyrazinamide
-
Inhibitors of polymer synthesis
- Vancomycin
- Teicoplanin
- Tanclopenin
-
Penicillins
- Penicillin G
- Cloxacillin, Dicloxacillin, Nafcillin, Oxacillin
- Amoxicillin, Ampicillin, Piperacillin, Ticarcillin
-
Beta-lactamase inhibitors
- Clavulanate
- Sulbactam
- Tazobactam
-
Cephalosporins
- 3rd Generation: Cefotaxime, Ceftriaxone
- Advanced Generation: Ceftaroline
-
-
Carbapenems
End in "penem"
- Doripenem
- Ertapenem
- Imipenem/Cilastatin
- Meropenem
-
Antibacterials that are highly ionized and poorly absorbed
Poor penetration of the meninges
Must be administered parenterally for the treatment of systemic infections
Aminoglycosides: end in "mycin"
-
Most commonly used antibacterial agent used in the treatment of gram-negative bacterial infections?
Aminoglycosides: end in "mycin"
-
Aminoglycoside used to treat tuberculosis
Streptomycin
-
Most active aminoglycoside against strains of P. aeruginosa
Tobramycin
-
Antibacterial agent used in ointments and creams to prevent infections after minor skin trauma
Neomycin
-
Adverse effect of aminoglycosides?
Nephrotoxicity and ototoxicity (problem with hearing)
-
Class of antibacterials taht bind divalent and trivalent cations
These drugs do not work as effectively when taken with food?
Tetracyclines: end in "cycline"
-
Drugs of choice to treat Rocky Mountain spotted fever?
Tetracyclines
-
Broad-spectrum of drugs that inhibit the growth of many gram-positive and gram-negative organisms, rickettsia, spirochetes, mycoplasmas, and chlamydiae
Tetracylines
-
Tetracylines used to treat skin and soft tissue infections caused by MRSA
Doxycyline and minocycline
-
Tetracycline used for treating syphilis and malaria
Doxycycline
-
Adverse effects of Tetracyclines?
Nephrotoxicity and Hepatotoxicity
Aminoglycosides and other nephrotoxic drugs should be avoided in patients having treatment with these drugs
-
Tetracycline that can be used with patients with renal insufficiency?
Doxycycline
-
The prototype of macrolides
Erythromycin
-
Semisynthentic macrolides
Azithromycin and Clarithromycin
-
Class of antibacterials active against many gram-positive and gram-negative bacteria that cause upper respiratory tract infections and pneumonia
Macrolides
-
Most active macrolide against H.pylori
Clarithromycin
-
Adverse effects of macrolides
Jaundice and ototoxicity
-
Active against gram-positive cocci and anaerobic organism such as Bacteroides fragilis and Clostridium perfringens
Effective against MRSA
Used for prophylaxis of bacterial endocardiits if allergic to penicillins
Clindamycin
-
Side effect of Clindamycin?
Gastrointestinal super-infections caused by Clostridium difficile
-
Prevents formation of the 70s initiation complex
Cross-resistance with other class of antibiotics is unlikely
Linezoid
-
Linezolid is indicated for what?
Vancomycin-resistant E. faecium, Pneumonia caused by MRSA and MSSA
-
30s Protein Inhibitors
Aminoglycosides: End in "mycin"
- Amikacin
- Gentamicin
- Kanamycin
- Neomycin
- Streptomycin
- Tobramycin
Tetracyclines: End in "cycline"
- Chloretetracycline
- Demeclocycline
- Doxycycline
- Methacycline
- Minocycline
- Oxytetracycline
- Tetracycline
-
50s Protein Synthesis inhibitors
Macrolides: End in "mycin"
- Azithromycin
- Clarithromycin
- Dirithromycin
- Erythromycin
-
Most common compounds for treating human infections include?
Sulfisoxazole and Sulfamethoxazole
-
What is Sulfamethoxazole administer with to prevent urinary tract infections?
Trimethoprim
-
Adverse effect of sulfonamides?
Hemolytic anemia
-
The drug of choice to treat for pulmonary infections caused by Pneumocystis jiroveci?
Trimethoprim-Sulfamethoxazole
-
Quinolone indicated for urinary tract infections?
Norfloxacin
-
Most frequently used fluorquinolones used in the USA?
Ciprofloxacin
-
Drug class used to treat bacterial diarrhea and is effective in treating traveler's diarrhea?
Quinolones
-
Used to treat anthrax?
Ciprofloxacin
-
Adverse effects of fluoroquinolones?
Tendonitis and tendon rupture
Should not be prescribed to adolescents, young children, nursing mothers, and pregnant women
Some fluoroquinolones inhibit P450 which leads to drug to drug interactions
-
Inhibits the cell membrane of bacteria
Active against some strains of MRSA and VRE
Approved for treatment of MRSA skin and skin-structure infections that are a complication of surgery, diabetic foot ulcers, and burns
Daptomycin
-
Adverse effect of Daptomycin?
Muscle toxicity
Creatine phosphokinase levels should be monitored
-
Antifolate drugs
- Sulfamethoxazole
- Trimethoprim
- Trimethoprim-Sulfamethoxazole
-
Quinolones
End in "oaxcin"
- Ciprofloxacin
- Enoxacin
- Gemifloxacin
- Levofloxacin
- Moxifloxacin
- Norfloxacin
- Ofloxacin
-
Tuberculosis drug that is activated by mycobacterial catalase-peroxidase, an enzyme encoded by the katG gene
Drug inhibits fatty acid synthetase 2 (FAS2)
Isoniazid
-
Drug used to treat latent tuberculosis
It is also given to prevent TB in neonates and children who have had close contact with persons in who active TB was recently diagnosed
Isoniazid
-
Penetrates inflamed meninges and can be used in the treatment of tubercular meningitis?
Rifampin
-
Tuberculosis drug used to prevent meningococcal disease in individuals who have had close contact with Neisseria meningitidis
Rifampin
-
Tuberculosis drug that inhibits arabinosyltransferase, an enzyme involved in the synthesis of arabinogalactan
Ethambutol
-
Adverse effects of ethambutol
Optic neuritis and impaired red-green color discrimination
-
Most toxic anti-fungal
It is effective against a wide range of fungi
In spite of its toxic potential, this drug is the choice for the treatment of life-threatening systemic mycoses
Amphotericin
-
Antifungal for the treatment of Candida species?
Nystatin
-
Used to treat fungal blepharitis
Natamycin (topical use only)
-
Triazole used to treat fungal meningitis?
Fluconazole
-
What class of drugs inhibit CYP3A4 which leads to drug interactions.
Azoles especially Ketoconazole
-
Used in many systemic fungal infections especially meningitis.
This anti-fungal drug is combined with Amphotericin B because drug resistance develops rapidly when it is administered alone
Flucytosine
-
How do the Polyenes, an antifungal agent work?
Polyenes bind to ergosterol in the plasma membrane of fungal cells and form pores which leads to cell death.
-
Anti-viral used against HSV and VZV
A guanosine analog that lacks a true sugar moiety, is monophosphorylated in the cell by the herpes virus, encoded enzyme, thymidine kinase
Causes premature DNA-chain termination
Acyclovir
-
The prototypic antiherpetic therapeutic agent
In the IV form it is the most effective treatment for serious herpesvirus infections, including herpetic encephalitis and severe HSV and VZV infections in immunocompromised patients.
Acyclovir
-
The prodrug form of acyclovir
Valacyclovir
-
Anti-viral used against CMV diseases, including retinitis, esophagitis and colitis
Ganciclovir
-
Pro-drug form of ganciclovir
Valganciclovir
-
What types of Anti-HIV drugs have been approved?
Drugs that target:
- Viral attachment
- Fusion
- Reverse transcription
- Integration
- Maturation
-
What type of drugs are the foundation of chemotherapy for HIV infection?
NRTIs:
- Abacavir
- Didanosine
- Emtricitabine
- Lamivudine
- Stavudine
- Tenofovir
- Zidovudine
-
Directly inhibit reverse transcriptase
They do not require metabolic activation and they are not incorporated into viral DNA
NNRTIs:
- Delaviridine
- Efavirenz
- Etravirine
- Nevirapine
-
Antiviral that inhibits the metabolism of other PIs and is often combined with other PIs to increase their plasma levels and duration which is also known as boosted therapy
Ritonavir
-
P450 enzymes (CYP3A4) are inhibited by what anti-HIV drugs?
PIs: end in "navir"
- Amprenavir
- Atazanavir
- Darunavir
- Fosamprenavir
- Indinavir
- Lopinavir
- Nelfinavir
- Ritonavir
- Saquinavir
- Tipranavir
-
The attachment and fusion inhibitors
They are approved for treatment of HIV infection caused by drug-resistant strains
-
Binds to HIV glycoprotein 41 and blocks the fusion process of HIV-1
Enfuvirtide
-
Antagonist of chemokine co-receptor 5 (CCR5).
Binds to CCR5 and prevents interaction with HIV-1 glycoprotein 120 that is necessary for CCR5-tropic HIV-1 to enter cells
Maraviroc
-
First integrase inhibitor
Approved for the treatment of HIV-1 infection in adult patients who have HIV-1 strains that are resistant to multiple anti-retroviral agents and who show evidence of increased viral replication
Raltegravir
-
Drug of choice to treat Hepatitis B
Tenofovir
-
How does Interferon work?
May involve the induction of host cell enzymes that inhibit viral RNA translation, ultimately leading to the degradation of viral mRNA and tRNA
-
Adverse effect of Interferon
Flu-like symptoms
-
Hepatitis B drugs
- Tenofovir
- Adefovir
- Entecavir
- Lamivudine
- Telbivudine
-
In combination with Interferon-alpha-2b it is effective in chronic hepatitis C
Ribavirin
-
What compound is ribavirin converted which blocks RNA-dependent RNA polymerase?
Ribavirin-triphosphate
-
Newly approved hepatitis C virus (HCV) NS3/4A protease inhibitors
These drugs cannot be used alone
These drugs are combined with interferon and ribvirin
Indicated, in combination with peginterferon alfa and ribavirin, for the treatment of genotype chronic hepatitis C (CHC) in adult patients with compensated
liver disease, including cirrhosis, who are treatment-naïve or who have been previously treated with interferon-based treatment, including prior null responders, partial responders, and relapsers.
-
Tricyclic amine compounds that block M2 proton-selective ion channel and prevent acidification of influenza type A virus and the fusion of viral membranes and endosomes required for uncoating and transfer of viral nucleic acid into the host cell cytoplasm
They are not currently recommended for prophylaxis and treatment of influenza in the United States
Adamantanes: end in "mantadine"
-
Inhibit the enzyme neuraminidase in influenza A and B viruses
These drugs block the release of the influenza drug from the cell
Are active against essentially all strains of influenza A and B viruses, and they are active against most current strains including influenza A 2009 H1N1, 2009 H3N2, and the H5N1 avian influenza strain
Neuraminidase inhibitors: end in "mivir"
-
Drugs for Herpesvirus infections
- Acyclovir and Valacyclovir
- Grancivlovir and Valganciclovir
- Penciclovir and Famiciclovir
- Cidofovir
-
Drugs for treating hepatitis C
- Interferon
- Ribavirin
- Boceprevir
- Telaprevir
-
Drugs for influenza
- Amantadine
- Rimantadine
- Oseltamivir
- Zanamivir
-
Antiparasitic active against several anaerobic protozoa
Drug of choice for amebiasis, giardiasis, and trichomniasis
Metronidazole
-
Anti-malaria drug that block exoerythrocytic schizogony
Primaquine
-
Treatment of choice for the prevention of all types of malaria
It must be used with primaquine to eradicate Vivax or Ovale Malaria
Chloroquine
-
Anti-malarial drugs that interfere with heme polymerization
-
Anti-malarial drug used to prevent the treatment of chloroquine-resistant malaria
Mefloquine
-
Used to treat falciparum malaria
Artermisinin and its derivatives:
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