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209 Cards in this Set

  • Front
  • Back
Cell Wall Biosynthesis
Glycopeptides
Structured around a heptapeptide with covalently linked side chains with sugar additions
Bacteriostatic against Gram+ cocci
Bactericidal for Gram+ rods
Including penicillinase producers and methicillin-resistant strains
Not effective against Gram-
Last resort for some strains of C. difficile
Binds D-Ala-D-Ala terminus of the murine monomer (substrate)
Red Man syndrome
Vancomycin
Cell Wall Biosynthesis
Glycopeptides
Structured around a heptapeptide with covalently linked side chains with sugar additions
Extended half-life elimination
Once daily dosing, fewer side effects
No pain or tissue necrosis after intramuscular injection
No ototoxicity
Teicoplanin
β-Lactams
Bactericidal, require actively growing infection
Inhibition by binding the enzyme

Penicillins
Natural Penicillins
Common feature is the 6-aminopenicillanic acid nucleus composed of a thiazolide ring fused to a β-lactam ring
Most active penicillins against Gram+
Only 1/3 of oral dose absorbed
Add procaine or benzathine to delay absorption from IM injection site
Add probenecid to delay elimination
Penicillin G
β-Lactams
Bactericidal, require actively growing infection
Inhibition by binding the enzyme

Penicillins
Natural Penicillins
Common feature is the 6-aminopenicillanic acid nucleus composed of a thiazolide ring fused to a β-lactam ring
Acid stable form with better absorption after oral administration
Penicillin V
β-Lactams
Bactericidal, require actively growing infection
Inhibition by binding the enzyme
Penicillinase-Resistant Penicillins
Resist β-lactamase produced by S. aureus and S. epidermidis
Gram+ only
Resistance related to failure to bind to penicillin binding proteins
Not given orally
Methicillin
β-Lactams
Bactericidal, require actively growing infection
Inhibition by binding the enzyme
Penicillinase-Resistant Penicillins
Resist β-lactamase produced by S. aureus and S. epidermidis
Gram+ only
Cloxacillin
β-Lactams
Bactericidal, require actively growing infection
Inhibition by binding the enzyme
Extended Range Penicillins
First penicillins effective against Gram-
For E.coli, P. mirabilis, H. influenzae, Salmonella, Shigella, Neisseria
More completely absorbed after oral admin than ampicillin
Amoxicillin
β-Lactams
Bactericidal, require actively growing infection
Inhibition by binding the enzyme
Extended Range Penicillins
First penicillins effective against Gram-
For E.coli, P. mirabilis, H. influenzae, Salmonella, Shigella, Neisseria
Ampicillin
β-Lactams
Bactericidal, require actively growing infection
Inhibition by binding the enzyme
Anti-Pseudomonal Penicillins (2)
Carboxylated derivatives extend range of ampicillin to P. aeruginosa, indole positive Proteus, and Enterobacter
Carbenicillin
Ticarcillin
β-Lactams
Bactericidal, require actively growing infection
Inhibition by binding the enzyme
Anti-Pseudomonal Penicillins
N-acyl derivatives
Pipericillin
β-Lactams
Bactericidal, require actively growing infection
Inhibition by binding the enzyme
Cephalosporins
Similar basic structure and mode of action to the penicillins
Can cause bleeding due to bleeding disorders or Vitamin K deficiency
First Generation
Narrow spectrum, against Staph and Strep
Surgical prophylaxis
Not effective for MRSA
Cefazolin
β-Lactams
Bactericidal, require actively growing infection
Inhibition by binding the enzyme
Cephalosporins
Similar basic structure and mode of action to the penicillins
Can cause bleeding due to bleeding disorders or Vitamin K deficiency
Second Generation
Increased action against Gram- like E. coli and Proteus
Decreased action against Gram+
Effective for H. influenzae and K. pneumoniae
For community acquired pneumonia
Cefuroxime
β-Lactams
Bactericidal, require actively growing infection
Inhibition by binding the enzyme
Cephalosporins
Similar basic structure and mode of action to the penicillins
Can cause bleeding due to bleeding disorders or Vitamin K deficiency
Second Generation
Increased action against Gram- like E. coli and Proteus
Decreased action against Gram+
B. fragilis and other anaerobes
Prophylaxis during intra-abdominal surgery (2)
Cefotetan
Cefoxitin
β-Lactams
Bactericidal, require actively growing infection
Inhibition by binding the enzyme
Cephalosporins
Similar basic structure and mode of action to the penicillins
Can cause bleeding due to bleeding disorders or Vitamin K deficiency
Second Generation
Increased action against Gram- like E. coli and Proteus
Decreased action against Gram+
• Sometimes classes as a carbacephem
Loracarbef
β-Lactams
Bactericidal, require actively growing infection
Inhibition by binding the enzyme
Cephalosporins
Similar basic structure and mode of action to the penicillins
Can cause bleeding due to bleeding disorders or Vitamin K deficiency
Third Generation
Good penetration of CNS, bone, lungs, urinary tract
High activity against Gram-
• Choice for N. gonorrhea and B. burgdorferi
Ceftriazone
β-Lactams
Bactericidal, require actively growing infection
Inhibition by binding the enzyme
Cephalosporins
Similar basic structure and mode of action to the penicillins
Can cause bleeding due to bleeding disorders or Vitamin K deficiency
Third Generation
Good penetration of CNS, bone, lungs, urinary tract
High activity against Gram-
• For multidrug-resistant Gram- infections, such as P. aeruginosa (2)
Ceftazidime
Cefoperazone
β-Lactams
Bactericidal, require actively growing infection
Inhibition by binding the enzyme
Cephalosporins
Similar basic structure and mode of action to the penicillins
Can cause bleeding due to bleeding disorders or Vitamin K deficiency
Fourth Generation
• Better against Gram+ because of resistance to β-lactamases
Cefepime
β-Lactams
Bactericidal, require actively growing infection
Inhibition by binding the enzyme
Carbapenems
Extremely broad spectrum
Resistant to β-lactamases, not resistant to metallo-β-lactamases
Given in combination with cilastatin, a dipeptidase inhibitor
Imipenem
β-Lactams
Bactericidal, require actively growing infection
Inhibition by binding the enzyme
Carbapenems
Extremely broad spectrum
Less susceptible to hydrolysis by renal tubule dipeptidase
Less nephrogenic
Meropenem
β-Lactams
Bactericidal, require actively growing infection
Inhibition by binding the enzyme
Monobactams
Excellent against Gram-, poor against Gram+
Can be used instead of aminoglycoside
The only one that does not show cross-allergenicity with other β-lactam antibiotics
Aztreonam
Antibiotics; Nucleic Acid biosynthesis
Sulfonamides
Broad spectrum
Structural analogs and competitive antagonists of PABA at dihydropteroate synthase
Sulfisoxazole
Sulfamethoxazole
Antibiotics; Nucleic Acid biosynthesis
Benzylpyrimidines
Broad Spectrum
Selective inhibitor of bacterial dihydrofolate reductase
Trimethoprim
Antibiotics; Cell Membrane potential; Lipopeptides
Spectrum
For complicated skin and skin structure infections
Retains activity against resistant Gram+
Binds to membranes and forms membrane channels in a Ca2+ dependent manner
Pharmacokinetics
IV only
Excreted by kidney
Does not cross blood-brain barrier
Daptomycin (Cubicin)
Antibiotics
Protein Synthesis 30S
Glycylcyline
Binds 30S. Prevents binding of aminoacyl tRNA
Bacteriostatic against Gram+ and Gram-, especially for tetracycline resistance
Binds 30s and inhibits binding of the aminoacyl-tRNA into the A site
Tigecycline
Antibiotics
Protein Synthesis 30S
Aminoglycosides
Bind 30S. Interfere with initiation complex and cause misreading of mRNA
Contains amino sugars linked to an aminocyclitol ring by glycosidic bonds
Broad spectrum bacteridical against Gram-
Inner membrane transport is oxygen-dependent--not effective for anaerobes
Binds the 16S rRNA in the 30S subunit, interferes with formation of the initiation complex
Enhanced activity with β-lactams
Streptomycin
Antibiotics
Protein Synthesis 30S
Tetracyclines
Bind 30S, prevent binding of aminoacyl tRNA
Bacteriostatic against Gram+ and Gram- aerobes and anaerobes
Binds 30S, prevents binding of aminoacyl-tRNA during protein synthesis
Crosses plasma membrane by active transport (2)
Tetracycline
Doxycycline
Antibiotics
Protein Synthesis 50S
Oxazoladinones
Bind 50S, prevents formation of initiation complex
Bacteriostatic against Gram positive strains
Prevents formation of the initiation complex and 70S ribosomal complex
Binds 50S subunit and prevents protein synthesis
Mutations of the 23 S rRNA prevent binding of the drug
Inhibits MAO
Linezolid
Antibiotics
Protein Synthesis 50S
Chloramphenicols
Binds 50S to inhibit peptidyl transferase
Not used in the US
Broad spectrum
Binds reversibly to the 50S subunit to prevent binding of the aminoacyl tRNA in the A site
Gray baby syndrome
Chloramphenicol
Antibiotics
Protein Synthesis 50S
Macrolides
Binds 50S, inhibits translocation
Inactivated by gastric acid, but absorbed in upper small intestine
MLSB determinants create resistance (3)
Erythromycin
Clarithromycin
Azithromycin
Antibiotics
Protein Synthesis 50S
Lincosamides
Binds 50S, inhibits translocation
Bacteriostatic against Gram+ and anaerobes
Binds the P and A sites of the 50S rRNA
Does not reach the CNS
Resistance due to ribosomal methylation (MLSB)
Clindamycin
Antibiotics
Protein Synthesis 50S
Type B streptogramins
Binds 50S, inhibits translocation
Bactericidal against Gram+
Binds 50S and inhibits 50S translocation step; same site as macrolides
Streptogramin B (guinupristin)
Antibiotics
Protein Synthesis 50S
Type B streptogramins
Binds 50S, inhibits translocation
Bactericidal against Gram+
Induces a conformation change in the 50S rRNA
Streptogramin A (dalfopristin)
Antibiotics
Protein Synthesis 50S
Type B streptogramins
Binds 50S, inhibits translocation
Combo of Streptogramin A and B
Synercid
Antibiotics
Protein Synthesis 50S
Ketolides
Binds 50S, inhibits translocation
Gram + and Gram-
Binds 50S, similar to macrolides
Liver toxicity and failure (critical adverse effect)
Telithromycin
Antibiotics; DNA replication or Transcription
Fluoroquinolones
Bactericidal,
Primarily for Gram-
Inhibits DNA gyrase (topoisomerase II), preventing relaxation of supercoiled DNA
Primary for Gram+
Inhibits topoisomerase IV (2)
Ciprofloxacin
Levofloxacin
Antibiotics; Nitroimidazole
For anaerobes
Nitro group of nitrosohydroxyl amino moiety is reduced causing DNA strand breaks
Metronidazole
Antibiotics; RNA replication or Transcription
Rifamycin
Inhibits RNA synthesis
Non-covalently binds to the β subunit of the DNA-dependent RNA polymerase
Oral preparation
Good CNS penetration
Deacetylated in the liver
Induces CYP3A4
Rifampin
Antibiotics; RNA replication or Transcription
Rifamycin
Inhibits RNA synthesis
Non-covalently binds to the β subunit of the DNA-dependent RNA polymerase
For traveler's diarrhea
Not absorbed from GI
Rifaximin
Antivirals, Penetration and Uncoating;
Interfere with viral uncoating by blocking viral M2 proton channel
For prophylaxis of influenza A (2)
Amantadine
Rimantidine
Antivirals, Penetration and Uncoating;
Saturated fatty alcohol that inhibits fusion of viral envelope to cell membrane
For HSV-1
Docosanol
Antivirals, Penetration and Uncoating;
• 36 residue synthetic peptide gp41 that blocks fusion of HIV to lymphocytes
Enfuvirtide
Antivirals, Assembly and Release;
Prophylaxis and treatment of influenza A and B
Inhibits viral neuraminidase, inhibiting cleavage of sialic acid
Blocks budding of new virus (2)
Zanamivir (Relenza)
Oseltamivir
Antivirals; Humanized Monoclonal Antibodies;
Directed against the F protein of RSV
Approved for prophylactic treatment of RSV
Palivizumab
Antivirals; Viral Nucleic Acid Synthesis;
Inhibits thymidylate synthetase and feedback inhibits other steps in pyrimidine biosynthesis
Drug of choice for the treatment of herptetic conjunctival keratitis
Trifluidine
Antivirals; Viral Nucleic Acid Synthesis;
Synthetic nucleoside whose phosphorylated form inhibits inosine monophosphate dehydrogenase
For RSV and hepatitis C (with interferon alphas)
Ribavirin
Antivirals; Viral Nucleic Acid Synthesis;
Guanosine analogue that is phosphorylated by thymidine kinase and inhibits viral DNA polymerase. Causes chain termination
Drug of choice for herpes encephalitis and chickenpox
Acyclovir
Antivirals; Viral Nucleic Acid Synthesis;
Prodrug form of acyclovir that is converted to acyclovir during first-pass metabolism
Reduces transmission of HSV-2 by 50%
Valacyclovir (Valtrex)
Antivirals; Viral Nucleic Acid Synthesis;
Acyclovir analogue that is effective for treatment of herpes labialis
Penciclovir
Antivirals; Viral Nucleic Acid Synthesis;
• Prodrug form of penciclovir, used to treat herpes labialis and genital herpes
Famciclovir
Antivirals; Viral Nucleic Acid Synthesis;
Acyclic guanine nucleoside analogue phosphorylated by CMV ULP& phosphotransferase
For severe CMV infections in immunocompromised hosts and CMV retinitis
Ganciclovir (Cytovene)
Antivirals;
Nucleoside reverse transcriptase inhibitors (NRTIs)
Can cause lactic acidosis as a result of mitochondrial toxicity
Synthetic thymidine analogue that competes with dTTP for binding to reverse transcriptase
Prolongs the lives of patients with AIDS
Decreases transmission of virus from mother to fetus
Zidovudine (AZT)
Antivirals;
Nucleoside reverse transcriptase inhibitors (NRTIs)
Can cause lactic acidosis as a result of mitochondrial toxicity
Deoxyadenosine analog that can cause peripheral neuropathy and fatal pancreatitis
Didanosine (ddI)
Antivirals;
Nucleoside reverse transcriptase inhibitors (NRTIs)
Can cause lactic acidosis as a result of mitochondrial toxicity
Can be used for hepatitis B (2)
Lamivudine (3TC)
Emtricitabine (FTC)
Antivirals;
Nucleoside reverse transcriptase inhibitors (NRTIs)
Can cause lactic acidosis as a result of mitochondrial toxicity
Can cause peripheral neuropathy (2)
Stavudine (d4T)
Zalcitabine (ddC)
Antivirals;
Nucleoside reverse transcriptase inhibitors (NRTIs)
Can cause lactic acidosis as a result of mitochondrial toxicity
Guanosine analog with less hematopoietic toxicity than AZT
Can cause rash and anaphylaxis--don't rechallenge
Abacavir
Antivirals;
Nucleoside reverse transcriptase inhibitors (NRTIs)
Can cause lactic acidosis as a result of mitochondrial toxicity
Guanine nucleoside analogue
Inhibits HBV reverse transcriptase and HBV DNA polymerase
Entevacir
Antivirals;
Nucleoside reverse transcriptase inhibitors (NRTIs)
Can cause lactic acidosis as a result of mitochondrial toxicity
Thymidine analogue
Inhibits HBV reverse transcriptase and HBV DNA polymerase
Telbivudine
Antivirals; Nucleotide reverse transcriptase inhibitors;
Acyclic nucleoside phosphonate that as a diphosphate inhibits HIV reverse transcriptase
Does not require nucleoside kinase activity
Tenofovir disoproxil
Antivirals; Nucleotide reverse transcriptase inhibitors;
Acyclic nucleoside phosphonate
For resistant CMV retinitis or smallpox vaccine reactions
Cidofovir
Antivirals; Nucleotide reverse transcriptase inhibitors;
For continuous use treatment of HBV
Adefovir
Antivirals; Non-Nucleoside reverse transcriptase inhibitors;
Can cause serious heptatotoxicity
Nevirapine
Antivirals; Non-Nucleoside reverse transcriptase inhibitors;
Crosses blood brain barrier
Efavirenz
Antivirals; Drug of choice for acyclovir-resistant herpes in AID patients
Inhibits HSV and CMV-encoded DNA polymerase, HIV reverse transcriptase
Foscarnet
Antivirals; Protein Synthesis;
HIV protease inhibitors
Bind to catalytic site of HIV protease, blocking cleavage of gag-pol precursor
Should only be used in combination therapy
Associated with lipodystrophies
Inhibit CYP3A4
Use in low doses to alter pharmakokinetics of a second protease inhibitor
Ritonavir
Antivirals; Protein Synthesis;
HIV protease inhibitors
Bind to catalytic site of HIV protease, blocking cleavage of gag-pol precursor
Should only be used in combination therapy
Associated with lipodystrophies
Inhibit CYP3A4
• OK to rechallenge with drug after rash resolves (2)
Amprenavir Fosamprenavir
Antivirals; Protein Synthesis;
HIV protease inhibitors
Bind to catalytic site of HIV protease, blocking cleavage of gag-pol precursor
Should only be used in combination therapy
Associated with lipodystrophies
Inhibit CYP3A4
• Lowest incidence of lipodystrophies
Atazanavir
Antivirals; Protein Synthesis;
HIV protease inhibitors
Bind to catalytic site of HIV protease, blocking cleavage of gag-pol precursor
Should only be used in combination therapy
Associated with lipodystrophies
Inhibit CYP3A4
• Ritonavir and Lopinavir combo
Kaletra
Antivirals; Interferons;
For Hep B anc C and a variety of malignancies
Major effect at the level of viral protein synthesis
Interferon alphas
Antivirals; Antisense Oligonucleotides;
Antisense oligonucleotide complimentary to IE2 of CMV
Binds IE2 mRNA, thus reducing expression
For CMV retinits in AIDS patients
Fomivirsen
Antifungals;
Cell Membranes
Polyenes
Conjugated double bond system with a macrolide ring
Bind to sterols and perturb membrane structure
Soluble enough for IV admin
Can cause impaired renal function
Amphotericin B
Antifungals;
Cell Membranes
Polyenes
Conjugated double bond system with a macrolide ring
Bind to sterols and perturb membrane structure
• Insoluble, used for superficial infections and GI infections
Nystatin
Antifungals;
Cell Membranes
Azoles
For superficial and systemic fungal infections
Inhibit 14-α-demethylase which is involved in ergosterol biosynthesis
Suitable for oral use
Drug of choice for Candida esophagitis
Fluconazole
Antifungals;
Cell Membranes
Azoles
For superficial and systemic fungal infections
Inhibit 14-α-demethylase which is involved in ergosterol biosynthesis
Suitable for oral use
Ketoconazole
Antifungals;
Cell Membranes
Azoles
For superficial and systemic fungal infections
Inhibit 14-α-demethylase which is involved in ergosterol biosynthesis
Suitable for oral use
Choice of treatment for dermatophytoses and onychomycosis
Itraconazole
Antifungals;
Cell Membranes
Azoles
For superficial and systemic fungal infections
Inhibit 14-α-demethylase which is involved in ergosterol biosynthesis
Drug of choice for resistant candidiasis
Posoconazole
Antifungals;
Cell Membranes
Azoles
For superficial and systemic fungal infections
Inhibit 14-α-demethylase which is involved in ergosterol biosynthesis
Drug of choice for treatment of invasive aspergillosis
Voriconazole
Antifungals;
Allylamines
Inhibits fungal squalene epoxidase
For tinea infections
Terbinafine
Antifungals; Pyridones
Pyridone antifungal agent that inhibits uptake of essential extracellular nutrients
Only approved drug for topical treatment of dermatophyte infections
Ciclopirox olamine
Antifungals; Echinocandins
Noncompetitive inhibitors of β-(1,3)-β-D-glucan synthase, responsible for a cell-wall component
For candidiasis and invasive aspergillosis
Caspofungin
Antifungals; Echinocandins
Noncompetitive inhibitors of β-(1,3)-β-D-glucan synthase, responsible for a cell-wall component
For candidiasis
Micafungin
Antifungals; Nucleic Acid synthesis
Cytosine analogue
Frequent resistance, so must use with amphotericin B
Flucytosine
Antifungals
Mitotic inhibitors
Insoluble compound that disrupts microtubule function resulting in aberrant mitoses
For fungal infections of the skin, hair, and nails
Griseofulvin
Chemotherapy; Alkylating Agents; Nitrogen mustards
Alkylate DNA, primarily at the N-7 position of guanine
• Stable enough for oral administration
Melphalan
Chemotherapy; Alkylating Agents; Nitrogen mustards
Alkylate DNA, primarily at the N-7 position of guanine
• Similar to melphalan
Chlorambucil
Chemotherapy; Alkylating Agents; Nitrogen mustards
Alkylate DNA, primarily at the N-7 position of guanine
Must be activated by CYP2C9 to aldophosphamide
Reduced hepatotoxicity
Cyclophosphamide
Chemotherapy; Alkylating Agents; Nitrogen mustards
Alkylate DNA, primarily at the N-7 position of guanine
• Cyclophosphamide derivative used for testicular cancer
Ifosfamide
Chemotherapy; Alkylating Agents; Ethylenimines
Reactive ethylenimonium ring is already formed
For breast and ovarian cancer
Thiotepa
Chemotherapy; Alkylating Agents; Alkylsulfonates
• Bifunctional methanesulfonate
Busulfan
Chemotherapy; Alkylating Agents; Nitrosoureas
Chloroethylnitrosureas
Heterobifunctional compounds that are capable of alkylation, DNA crosslinking, and carbamoylation of proteins
Lipid soluble agents that disappear rapidly from plasma (2)
Carmustine (BCNU)
Lomustine (CCNU)
Chemotherapy; Alkylating Agents; Triazenes
Inhibits RNA and protein synthesis more than DNA synthesis
No alkylating specificity
Dacarbazine (DTIC)
Chemotherapy; Alkylating Agents; Triazenes
Does not require hepatic activation
For anaplastic astrocytoma
Temozolomide
Chemotherapy; Alkylating Agents; Others
Platinum coordination complex, chloride ions dissociate
For testicular cancer, ovarian carcinoma, and head and neck cancers
Cisplatin (Platinol)
Chemotherapy; Alkylating Agents; Others
• Cisplatin analogue that is not cross-resistant
Oxaliplatin
Chemotherapy; Alkylating Agents; Others
• Cisplatin analogue that has substantially less renal toxicity
Carboplatin
Chemotherapy; Alkylating Agents; Others
Nonspecific alkylator after metabolic activation
For Hodgkin's disease
Procarbazine
Chemotherapy; Natural Products; Vinca Alkaloids
Two of the most potent plant-derived antitumor agents
Binds tubulin, favoring depolymerization
Resistance due to MDR
Vincristine
Vinblastine
Chemotherapy; Natural Products;
Vinca Alkaloids
• Semisynthetic derivative of vinblastine with increased specificity for microtubules
Vinorelbine
Chemotherapy; Natural Products;
Taxanes
Treatment of breast and ovarian cancer when chemotherapy has failed
Inhibits disassembly of microtubules, blocking reorganization
Resistance due to MDR
Paclitaxel (Taxol)
Chemotherapy; Natural Products;
Taxanes
• Semisynthetic analogue of paclitaxel
Docetaxel
Chemotherapy; Natural Products;
Epipodophyllotoxins
Semisynthetic glycosidic derivatives from a mandrake plant
Inhibit topoisomerase II
For Hodgkin's disease, diffuse histiocytic lymphoma, and small cell carcinoma of the lung (2)
Etoposide (VP-16)
Teniposide (VM-26)
Chemotherapy; Natural Products;
Camptothecin derivatives
Inhibit topoisomerase I
• Prodrug effective in the treatment of metastatic colorectal cancer
Irinotecan
Chemotherapy; Natural Products;
Camptothecin derivatives
Inhibit topoisomerase I
• For treatment of ovarian and small cell lung carcinoma
Topotecan
Chemotherapy; Natural Products;
Antibiotics
Composed of a planar phenoxazone to which identical polypeptides are attached
Intercalates between adjacent G:C base pairs
Inhibits RNA at low, RNA and DNA at high concentrations
Causes radiation sensitization
Dactinomycin (acinomycin D)
Chemotherapy; Natural Products;
Antibiotics
DNA and iron binding region
S peptide binds to DNA, leading to depurination and depyrimidation
Resistance due to bleomycin hydrolase
Bleomycin
Chemotherapy; Natural Products;
Antibiotics
• Cause DNA intercalation and introduce single strand breaks (3)
Daunorubicin
Doxorubicin
Mitoxantrone
Chemotherapy; Natural Products;
Antibiotics
Anthracyclines
• Iron chelator that inhibits free radical formation and can be used to reduce cardiac damage
Dexrazoxane
Chemotherapy; Antimetabolites; General
Folic acid analogue, inhibits dihydrofolate reducatase (DHFR)
Inhibits dUMP-->dTMP
Affects pyrimidine biosynthesis and purine ring structure
Resistance is due to increased DHFR activity and reduced transport
Methotrexate
Chemotherapy; Antimetabolites; General
• Effectively aborts MTX toxicity by supplying reduced folate to cells
Leucovorin
Chemotherapy; Antimetabolites; General
Inhibits ribonucleotide reductase, inhibits DNA synthesis, and blocks cells at the G1/S boundary
For a variety of malignancies
Bone marrow suppression
Hydroxyurea
Chemotherapy; Antimetabolites;
Pyrimidine analogues
Prototype pyrimidine analogue
5-FdUMPis a potent suicide inhibitor of thymidylate synthase (TS)
Resistance due to overexpression of TS
5-FU
Chemotherapy; Antimetabolites;
Pyrimidine analogues
5-FU prodrug catalyzed by thymidine phosphorylase
For metastatic breast and colon cancer
Capecitabine
Chemotherapy; Antimetabolites;
Pyrimidine analogues
Good activity against advanced breast cancer, non-small-cell lung cancer, pancreatic adenoma, and ovarian carcinoma
Gemcitabine
Chemotherapy; Antimetabolites;
Pyrimidine analogues
Inhibits DNA methyltransferases resulting in hypomethylation
Effective for treatment of myelodysplastic syndrome
Azacitidine
Chemotherapy; Antimetabolites;
Pyrimidine analogues
Cytidine analogue effective in the treatment of hematologic malignancies
Inhibits DNA polymerase
Resistance due to decreased cytosine kinase activity
Cytosine arabinose
Chemotherapy; Antimetabolites;
Purine Analogues
Prototypic purine analogues
Converted to mononucleotides which feedback inhibit de novo purine synthesis
Converted to triphosphates which are incorporated into DNA and RNA
Resistance due to HPRT mutations or overexpression of TPMT(2)
6-mercaptopurine
6-thioguanine
Chemotherapy; Antimetabolites;
Purine Analogues
Inhibits adenosine deaminase, resulting in the accumulation of dATP
For hairy cell leukemia
Pentostatin
Chemotherapy; Others;
Enzymes
Converts asparagine to aspartate
Deprives cells of the essential amino acid
Asparaginase
Chemotherapy; Others;
Tyrosine Kinase Inhibitors
Competitively blocks the ARP-binding site of the c-able kinase in CML
Can cause congestive heart failure
Imatinib mesyltate (Gleevec)
Chemotherapy; Others;
Tyrosine Kinase Inhibitors

Inhibit EGF receptor-associated tyrosine kinase
For treatment of non-small cell carinoma of the lung and pancreatic cancer (2)
Erlotinib
Gefitinib
Chemotherapy; Others; Antibodies
Directed against the EGF receptor
For head and neck and metastatic colorectal cancer
Cetuximab
Chemotherapy; Others; Antibodies
Induces antibody-dependent cell-mediated cytotoxicity
For treatment of p185-her2 positive breast cancer
Trastuzumab (Herceptin)
Chemotherapy; Others; Antibodies
Directed against the VEGF receptor
Inhibits angiogenesis
Bevacizumab
Chemotherapy; Others; Antibodies
Anti-CD20 antibody that promotes complement mediated lysis of malignant B-cells in CD-20 positive non-Hodgkin's B cell lymphoma
Can result in HBV reactivation
Rituximab
Chemotherapy; Others; Antibodies
• Directed against myeloid cell surface antigen CD33
Gemtuzumab ozogamicin (Mylotarg)
Chemotherapy; Others;
Biologic Response modifiers
• Histone deacetylase inhibitor used to treat primary cutaneous T cell lymphoma
Vorinostat
Chemotherapy; Others;
Biologic Response modifiers
• Proteasome inhibitor used for treatment of multiple myeloma and mantel cell lymphoma
Bortezomib
Chemotherapy; Others;
Biologic Response modifiers
• First line therapy for promyelocytic leukemia
All-trans-retinoic acid (vitamin A)
Chemotherapy; Others;
Biologic Response modifiers
Bisphosphonates useful for the treatment of hypercalcemia and osteolytic bone lesions in multiple myeloma
Inhibit osteoclast activity and induce osteoclast apoptosis (2)
Pamidronate
Zoledronate
Cancer Chemotherapy; Hormonal Agents; Breast Cancer
Antiestrogens
Prevents binding to the Estrogen Receptor in a competitive fashion
Can reduce total cholesterol and preserve bone density
Tamoxifen
Cancer Chemotherapy; Hormonal Agents; Breast Cancer
Antiestrogens
Selective estrogen receptor modulator (SERM)
Just as effective as tamoxifen with fewer side effects
Raloxifen
Cancer Chemotherapy; Hormonal Agents; Breast Cancer
True Estrogen Receptor Antagonists;
Pure estrogen receptor antagonist
For postmenopausal women whose cancer is unresponsive to tamoxifen
Fulvestrant (Faslodex)
Cancer Chemotherapy; Hormonal Agents; Breast Cancer
Aromatase inhibitors
Inhibits the conversion of cholesterol to pregnenolone, reducing all classes of steroids
Inhibits conversion of androstenedione into estrone and estradiol
Aminoglutethimide
Cancer Chemotherapy; Hormonal Agents; Breast Cancer
Aromatase inhibitors
Selective and irreversible inhibitor of aromatase
As effective as tamoxifen for advanced breast cancer, first line therapy
Anastrozole
Cancer Chemotherapy; Hormonal Agents; Breast Cancer
Aromatase inhibitors
Selective and irreversible inhibitors of aromatase
First line therapy after tamoxifen (2)
Letrozole
Exemestane
Cancer Chemotherapy; Hormonal Agents; Breast Cancer
Progesterone Agonists
• Benefit likely due to suppression of adrenal steroid synthesis and estrogen receptor levels (2)
Megestrol
Medroxyprogesterone
Cancer Chemotherapy; Hormonal Agents; Breast Cancer
Gonadotropin-releasing hormone agonists
Prolonged use leads to desensitization of FSH and LH-producing cells
Can be used for metastatic breast cancer or prostate cancer
Leuprolide
Goserelin
Cancer Chemotherapy; Hormonal Agents; Breast Cancer
Others
• Antibody against HER2/erb-2, a member of the epidermal growth factor receptor family
Trastuzumab (Herceptin)
Cancer Chemotherapy; Hormonal Agents; Breast Cancer
Others
For advanced breast cancer expressing high levels of HER-2 that no longer respond to trastuzumab
Tyrosine kinase inhibitor
Lapatinib (Tykerb)
Cancer Chemotherapy; Hormonal Agents; Prostate Cancer
Non-steroidal anti-androgens
Prevents the binding of endogenous androgens to the androgen receptor
Pure androgen antagonist
Flutamide
Cancer Chemotherapy; Hormonal Agents; Prostate Cancer
Non-steroidal anti-androgens
More effective in prostate cancer than flutamide
Less likely to cause diarrhea or other side effects
Bicalutamide
Cancer Chemotherapy; Hormonal Agents; Prostate Cancer
Steroidal anti-androgens
• Occasionally used for prostate cancer (2)
Megestrol
Medroxyprogesterone
Cancer Chemotherapy; Hormonal Agents; Prostate Cancer
Gonadotropin-releasing hormone agonists
Equivalent antitumor effects in prostate cancer as surgical castration or diethylstilbestrol treatment (2)
Leuprolide
Goserelin
Cancer Chemotherapy; Hormonal Agents; Prostate Cancer
Gonadotropin-releasing hormone agonists
Suppressive effects on LH and FSH production
Numerous side effects
Diethylstilbestrol
Cancer Chemotherapy; Hormonal Agents; Prostate Cancer
Adrenal enzyme synthesis inhibitor
• Inhibits P450 enzymes involved in steroid biosynthesis
Ketoconazole
Mycobacterial Treatments;
First-line Agents
Combine the greatest level of efficacy with an acceptable level of toxicity
Primary drug for chemotherapy of tuberculosis
Inhibits the synthesis of mycolic acids
Intracellular and Extracellular levels are similar
Administer with pyridoxine B6
Activated by catalase peroxidase on the KatG gene
Isoniazid
Mycobacterial Treatments;
First-line Agents
Combine the greatest level of efficacy with an acceptable level of toxicity
Given in combination with INH
Inhibits bacterial DNA dependent RNA polymerase
Causes an orange-red coloration of urine
Reduces the half-life of many drugs
Rifampin
Mycobacterial Treatments;
First-line Agents
Combine the greatest level of efficacy with an acceptable level of toxicity
Acts as a long-acting rifampin
Avoid in pregnancy or HIV
Rifapentine
Mycobacterial Treatments;
First-line Agents
Combine the greatest level of efficacy with an acceptable level of toxicity
Inhibits the synthesis of arabinogalactan
Few side effects except for optic neuritis
Do not give to children
Ethambutol
Mycobacterial Treatments;
First-line Agents
Combine the greatest level of efficacy with an acceptable level of toxicity
Inhibits mycobacterial fatty acid synthase I gene involved in mycolic acid synthesis
Contraindicated with liver disease or gout
Pyrazinamide
Mycobacterial Treatments;
Second-line Agents
Fluoroquinolones
Levofloxacin
Moxifloxacin
Ofloxacin
Mycobacterial Treatments;
Second-line agents
Does not kill intracellular microbes
Causes ototoxicity and nephrotoxicity
Streptomycin
Mycobacterial Treatments;
Second-line agents
Inhibits the synthesis of mycolic acids (similar to INH)
Causes intense gastric irritation
Ethionamide
Mycobacterial Treatments;
Second-line agents
Similar to sulfonamides
High concentrations are reached in the urine
Aminosalicylic Acid (PAS)
Mycobacterial Treatments;
Second line agents
• Irreversible inhibitor of alanine racemase and D-Ala-D-ALA synthetase
agents
Cycloserine
Mycobacterial Treatments;
Other drugs
All are given parenterally
There is some cross-resistance between these antibiotics (4)
Capreomycin
Viomycin
Kanamycin
Amikacin
Mycobacterial Treatments;
Mycobacterium avium complex
• Standard to prevent drug resistance (3)
Clarithromycin, Azithromycin, Ethambutol
Mycobacterial Treatments;
Mycobacterium avium complex
• May be necessary to add to the drug regime (3)
Rifabutin, Clofazimine, Quinolone
Mycobacterial Treatments;
Hansen's disease
Paucibacillary with 5 or few lesions
Inhibits folate synthesis, same as the sulfonamides
Can cause hemolysis
Dapsone
Mycobacterial Treatments;
Hansen's disease
Paucibacillary with a single skin lesion (3)
Rifampin
Minocycline
Ofloxacin
Mycobacterial Treatments;
Hansen's disease
Multibacillary with 6 or more lesions
• Acts very slowly, mechanism of action unknown
Clofazimine
Mycobacterial Treatments;
Hansen's disease
Others
• Mandatory use of two contraceptives and monthly pregnancy test
Thalidomide
Antimalarials; Arylaminoalcohols
Rapidly kill blood stage of P. falciparum
DOC for acute severe disease
Cardiotoxicity
Quinidine
Antimalarials; Arylaminoalcohols
Rapidly kill blood stage of P. falciparum
DOC for most P. falciparum regions
Prophylaxis of MDR malaria in the US
Neuropsychiatric concerns, contraindicated in seizure patients
Mefloquine
Antimalarials;
4-aminoquinolones
Kills blood stage parasites by accumulating in the acid vacuole of the parasite and interfering with heme polymerase
P. falciparum resistance
DOC for Rx and Px for non-P.falciparum malaria
Chloroquine
Antimalarials;
8-aminoquinolones
For hypnozoites in the liver
Terminal prophylaxis
Contraindicated for G-6-PD deficiency and pregnancy
Primaquine
Antimalarials;
Antibiotics
For blood stage treatment
Slow acting but effective
DOC for prophylaxis in mefloquine resistant P.falciparum areas
Doxycycline
Antimalarials;
Combination chemicals
Combo proguanil and atovaquone
For uncomplicated multi-drug resistant P.falciparum
There are concern of development to proguanil resistance
Malarone
Antimalarials;
Individual Drugs
Quinine
Quinidine
Cinchona Alkaloids
Antimalarials; Individual Drugs
• Rapid acting blood schizonticide indicated for the treatment of mild-to-moderate P.falciparum and P. vivax
Halofantrine HCl (phenanthrenemethanol)
Antimalarials; Individual Drugs
Extracts from Chinese medicinal plants
Most rapidly acting of all antimalarials
Artemisinin Derivatives
Antimalarials; Individual Drugs
Combo that inhibits dihydrofolate reductase and conversion of PABA
For chloroquine-resistant P.falciparum
Fansidar (Pyrimethamine-Sulfadoxine)
Antiparasitics
Amebiasis
Lumenal Drug
Liberates iodine which is the active amebicide
Iodoquinol
Antiparasitics
Amebiasis
Lumen drug
Aminoglycoside antibiotic, acts on protein synthesis
Paromomycin
Antiparasitics
Amebiasis
Mixed amebicide
Acts as an electron sink to prevent the terminal electron transport system from reoxidizing NADH to NADPH
Avoid during pregnancy
Metronidazole
Antiparasitics
Cryptosporidiosis
Inhibits pyruvate-ferredoxin oxidoreductase
Nitazoxanide
Antiparasitics
Cyclosporiasis
TMP/SMZ
Antiparasitics
Giardiasis
85-95% effective
Mixed amebicide
Acts as an electron sink to prevent the terminal electron transport system from reoxidizing NADH to NADPH
Avoid during pregnancy
Metronidazole
Antiparasitics
Giardiasis
Available in pediatric suspension
Inhibits pyruvate-ferredoxin oxidoreductase
Nitazoxanide
Antiparasitics
Giardiasis
Used to treat pregnant women
Paromomycin
Antiparasitics
Isosporiasis
TMP/SMZ
Antiparasitics
Trichomoniasis
Drug of choice
Mixed amebicide
Acts as an electron sink to prevent the terminal electron transport system from reoxidizing NADH to NADPH
Avoid during pregnancy
Metronidazole
Antiparasitics
Trichomoniasis
Restores the acidic environment
Vinegar douches
Antiparasitics
AIDS patients
Toxoplasmosis
• Folate antagonist
Pyrimethamine with sulfadiazine
Antiparasitics
AIDS patients
Toxoplasmosis
• Folic acid supplement to prevent bone marrow suppression
Leucovorin
Antiparasitics
AIDS patients
Toxoplasmosis
• Antibiotics prophylactic treatment
TMP/SMZ
Antiparasitics
AIDS patients
Toxoplasmosis
• Prophylactic treatment (3)
Pyrimethamine Dapsone Leucovorin
Antiparasitics
AIDS patients
Pneumocystosis (PCP)
• Drug of choice but high incidence of adverse reactions
TMP/SMZ
Antiparasitics
AIDS patients
Pneumocystosis (PCP)
• Second line drugs of choice (2)
Pentamidine
Atovaquone
Antiparasitics
AIDS patients
Pneumocystosis (PCP)
• Prophylactic treatment, necessary in AIDS patients (2)
TMP/SMZ
Aerosolized pentamidine
Antiparasitics
AIDS patients
Protozoan infections
Inhibitory analog of ubiquinone which interferes with mitochondrial electron transport
Atovaquone
Antiparasitics
AIDS patients
Protozoan infections
Causes selective breaks in the kinetoplast mini-circle DNA of trypanosomes
Can cause diabetes
Pentamidine isethionate
Antiparasitics
Babesiosis (2)
Clindamycin
Quinine
Antiparasitics
African Trypanosomiasis
T. brucei gambiense
• Initial stage
Pentamidine
Antiparasitics
African Trypanosomiasis
T. brucei gambiense
Late stage
Arsenical, which reacts with sulfhydryl groups in protein
Very toxic
Melarsoprol
Antiparasitics
African Trypanosomiasis
T. brucei gambiense
Late stage and relapses
Suicide inhibitor of ornithine decarboxylase
Eflornithine
Antiparasitics
African Trypanosomiasis
T. brucei rhodesiense
Initial stage
Inhibits large numbers of enzymes
Suramin
Antiparasitics
African Trypanosomiasis
T. brucei rhodesiense
Late stage and relapses
Melarsoprol
Antiparasitics
Chagas Disease
Amastigotes and extracellular mastigote
Converted to a superoxide radical and a peroxide
Nifurtimox
Antiparasitics
Leishmaniasis
Drug of choice in the US
Trivalent form inhibits the parasite's phosphofructokinase
Sodium stibogluconate
Antiparasitics
Leishmaniasis
Second line for mucocutaneous or visceral leishmaniasis
Amphotericin B
Antiparasitics
Leishmaniasis
Second line for cases which are resistant
Pentamidine
Antihelminthics
Nematode infections
Benzimadozoles
Useful with highly infected populations
Contra-indicated in pregnancy
Mebendazole
Antihelminthics
Nematode infections
Benzimadozoles
Has replaced other drugs as the drug of choice for a number of intestinal helminths
Contra-indicated in cirrhosis or pregnancy
Albendazole
Antihelminthics
Nematode infections
Benzimadozoles
Treatment for Strongyloides stercoralis (threadworm)
Thiabendazole
Antihelminthics
Nematode infections
Others
For pinworm and hookworm
Depolarizing neuromuscular blocker leading to release of acetylcholine and persistent nicotinic stimulation
Pyrantel pamoate
Antihelminthics
Antifilarial Agents
• May have an effect on the surface coat of the parasite
Diethylcarbamazine
Antihelminthics
Antifilarial Agents
Highly potent and broad spectrum antihelminthic activity
Causes an influx of chloride ions through specific channels
Ivermectin
Antihelminthics
Schistosomiasis and Tapeworm infections
Broad spectrum against schistosomes, and drug of choice for tapeworms
Increases permeability to calcium ions
Praziquantel
Antihelminthics
Schistosomiasis and Tapeworm infections
Second drug of choice for tapeworms
Potent inhibitor of fumarate reductase, blocking ATP production
Niclosamide