Organism - University of Kentucky
Drug |Class |Use |Side Effects |Interactions |Other | |
|All Penicillins |All Penicillins |--- |Allergies | |Inhibit crosslinking in cell wall synthesis by PBP |
| | |Bactericidal | | |Short t1/2, Low toxicity & Renal Clearance |
| | | | | |Distributed in CSF only with meningitis |
|Penicilin V |β-Lactam |Oral |Allergies | |Some anaerobes, minor infections |
| |(Penicillin) | | | | |
| |(Standard Penicillin) | | | | |
|Methicillin |β-Lactam |Parenteral (IV) |Allergies | |β-Lactamase producing Staph |
| |(Penicillin) | |Nephrotoxic | | |
| |(Antistaphylococcal) | | | | |
|Nafcillin |β-Lactam |Parenteral (IV) |Allergies | |β-Lactamase producing Staph |
| |(Penicillin) | |Nephrotoxic | |Preferred over methicillin |
| |(Antistaphylococcal) | | | | |
|Dicloxacillin |β-Lactam |Oral |Allergies | |Mild local staph infections |
| |(Penicillin) | | | | |
| |(Antistaphylococcal) | | | | |
|Ampicillin |β-Lactam |Parenteral (IV) |Allergies, GI Upset | |Anaerobes, enterococci, Listeria |
| |(Penicillin) | |Superinfections | |Gram- rods & bacilli, (E. coli, H. inf, Salmonella) |
| |(Aminopenicillin) | |Non-allergic skin rashes | | |
|Amoxicillin |β-Lactam |Oral |Allergies, GI Upset | |Prophylactically by dentists |
| |(Penicillin) |URI, Sinusitis, Otitis & LRTI (DOC) |Superinfections | | |
| |(Aminopenicillin) | |Non-allergic skin rashes | | |
|Ticarcillin |β-Lactam | |Allergies | |Gram – (Klebsiella, Enterobacter, Pseudomonas) |
| |(Penicillin) | | | |Often combined with aminoglycoside (tobramycin) |
| |(Antipseudomonal) | | | |For hospitalized neutropenic patients |
|Pipercillin |β-Lactam | |Allergies | |Gram – (Klebsiella, Enterobacter, Pseudomonas) |
| |(Penicillin) | | | |Often combined with aminoglycoside (tobramycin) |
| |(Antipseudomonal) | | | |For hospitalized neutropenic patients |
|Augmentin |β-Lactam |Oral |Allergies, GI Upset | |Sinusitis, Pneumonia, Otitis, Meningitis, etc |
|(Amoxicillin & |(Penicillin) | |Superinfections | |Clavulanic Acid overcomes β-Lactamases |
|Clavulanic Acid) | | |Non-allergic skin rashes | | |
|1st Generation |β-Lactam |--- |Allergies & Nephrotoxic | |Gram +; Proteus, E. coli, Klebsiella (PEcK) |
|Cephalosporins |(1st Generation Cephalosporin) |Bactericidal |Superinfections, Alcohol Intorelance | |More resistant to β-Lactamases |
| | | |Bleeding, Serum Sickness | |Not effective on Listeria & enterococci |
|Cefazolin |β-Lactam |Parenteral |Allergies | |Surgical Prophylaxis (for skin microbes) |
| |(1st Generation Cephalosporin) | |Potentially nephrotoxic | |Bone Penetration |
|2nd Generation |β-Lactam |--- |Allergies | |Haemophilus, Enterobacter, Neisseria & PEcK |
|Cephalosporins |(2nd Generation Cephalosporin) |Bactericidal |Potentially nephrotoxic | |Less Gram + than 1st Generation |
|Cefuroxime |β-Lactam |Parenteral |Allergies | |Gets into CSF, Long t1/2 |
| |(2nd Generation Cephalosporin) | |Potentially nephrotoxic | |Bronchitis, Pneumonias, Immunocomprimised |
|Cefuroxime axetil |β-Lactam |Oral |Allergies | | |
| |(2nd Generation Cephalosporin) | |Potentially nephrotoxic | | |
|Cefoxitin |β-Lactam |Parenteral |Allergies | |Bacteroides, abdominal & gynecological sepsis |
| |(2nd Generation Cephalosporin) | |Potentially nephrotoxic | |Surgical Prophylaxis (for intestinal microbes) |
|3rd Generation |β-Lactam |--- |Allergies | |HENPEcK, Serratia, Enterics |
|Cephalosporins |(3rd Generation Cephalosporin) |Bactericidal |Potentially nephrotoxic | |Less Gram + than 2nd Generation |
|Cefixime |β-Lactam |Oral |Allergies | |Once Daily Dosing |
| |(3rd Generation Cephalosporin) | |Potentially nephrotoxic | | |
|Ceftazidime |β-Lactam |Parenteral |Allergies | |Pseudomonas |
| |(3rd Generation Cephalosporin) | |Potentially nephrotoxic | | |
|4th Generation |β-Lactam |--- |Allergies | |Very resistant to β-Lactamases |
|Cephalosporins |(4th Generation Cephalosporin) |Bactericidal |Potentially nephrotoxic | |Less Gram + than 3rd Generation |
|Imipenem |Carbapenem |Parenteral (IV) |GI Upset, rash | |Gram + & - & Anaerobes |
|(+ Cilastin) | |Reserved |Reaction at infusion site | |Gets in bones & CSF, Renal Clearance |
| | |Enterobacter (DOC) |Seizures with renal insufficiency | |Given with Cilastin to prevent inactivation |
|Aztreonam |Monobactam |Parenteral (IV) |Rash | |Gram - Rods |
| | | |Transaminase Elevation | |Renal Clearance |
| | | | | |Resistant to β-Lactamases |
|Vancomycin |Vancomycin |Parenteral (Slow IV) |Red Man Syndrome |Aminoglycosides |Prevents formation of polymers in cell wall |
| | |Oral (for colitis) |Fever, Chills, Phlebitis, Tachycardia | |Gram +, MRSA, Clostridium, Enterococci |
| | |Reserved |Hypotension, Shock, Flushing | |Renal secretion, Penetrates CSF with inflammation |
| | | |Allergies, Ototoxic, Nephrotoxic | | |
|Metronidazole |Nucleic Acid Synthesis Inhibitor |Oral |Nausea, Headache, Vertigo | |Fragments anaerobic DNA, must be reduced |
| | |Bactericidal |Alcohol Intolerance | |Gets into bone & CSF |
| | |Bacteroides (DOC) |Peripheral Neuropathy | |Liver & Renal Metabolism/Excretion; Enterocolitis |
|Fluoroquinolones |Nucleic Acid Synthesis Inhibitor |--- | | |Inhibit Gram - DNA replication; enters via porins |
|& |(Fluoroquinolones & Quinolones) |Bactericidal | | |Acts on gyrase/topoisomerase; Gets in Bone |
|Quinolones | | | | |Mycobacteria, Weakly on anaerobes, Gram + |
|Drug |Class |Use |Side Effects |Interactions |Other |
|Rifampin |Nucleic Acid Synthesis Inhibitor |Oral |Makes body fluids red |↓ Anticoagulants|Inhibits RNA Pol; Deacetylation for activation |
| | |Bactericidal |Hepatotoxic |↓ Contraceptives|Gram + & -, Mycobacteria, N. meningitides; CSF |
| | |Anti-TB |GI Upset, bleeding, flu-like |↓ |Hepatic metabolism, enterohepatic recirculation |
| | | | |Glucocorticoids | |
| | | | |↓ Estrogen | |
|Sulfonamide |Metabolic Inhibitor |Oral & Suppository |Renal problems (parent drug secreted) | |Binds dihydropteroate synthetase (similar to PABA) |
| |(Sulfonamide) |Bacteristatic | | |Actinomycetes, Chlamydia, E. coli, Proteus, Strep |
| | | | | |H. influenza, PCC; Enters CSF, Liver Metabolized |
|Trimethoprim |Metabolic Inhibitor |Oral |Same as sulfa | |Binds DHF reductase ;Concentrates in prostate & |
| | | |Bad for AIDS w/ PCCP (Stevens-Johnson) | |vaginal fluids; UTI, prostatitis, genital infxns, |
| | | |Permanent renal damage if ↓ function | |Legionella, Salmonella, “anythingitis” & PCCP |
|Aminoglycosides |Protein Synthesis Inhibitor |--- |Post-antibiotic effect | |Enters porins & requires O2 , DNA Misreading, |
| |Aminoglycoside |Bactericidal | | |Inhibit ribosomes on aerobic bacteria only |
| | |(Bacteriostatic for TB?) | | |Penetrates bone, NOT CSF; Renal excretion |
|Gentamycin |Protein Synthesis Inhibitor |Parenteral |Ototoxicity (worst of all aminoglycosides) | |Endocarditis (+ β-Lactam); Severe UTI |
| |Aminoglycoside | |Nephrotoxicity, vestibular damage | |Pseudomonas, Klebsiella, Proteus, Serratia, |
| | | |Neuromuscular paralysis (w/ ↑ doses) | |brucellosis, tularemia, peritonitis; Binds 30 & 50S |
|Tobramycin |Protein Synthesis Inhibitor |Parenteral |Ototoxicity, nephrotoxicity | |Similar to gentamycin, better w/ Pseudomonas |
| |Aminoglycoside | |vestibular damage | |Less w/ Serratia & enterococci |
| | | |Neuromuscular paralysis (w/ ↑ doses) | |Oftened combined with β-Lactam; Binds 30 & 50S |
|Tetracyclines |Protein Synthesis Inhibitor |--- |Bones & Teeth, Hepatotoxic, GI upset | |Binds 30S of ribosome, blocks tRNA access |
| |Tetracycline |Bacteristatic |Not for pregnant or children, Phototoxic | |Gram + & -, anaerobes, rickettsiae, Chlamydia, |
| | | | | |Legionella, Plasmodia, Gets in bones & CSF |
|Doxycycline |Protein Synthesis Inhibitor |Oral |Bones & Teeth, Hepatotoxic, GI upset |Antacids ↓ |Liver metabolism, Hepatic excretion |
| |Tetracycline | |Not for pregnant or children, Phototoxic |↓ Birth Control | |
| | | | |↑ Anticoagulants| |
|Macrolides |Protein Synthesis Inhibitor |Bacteristatic (some cidal) | |Clindamycin |Irreversibly bind 50S, inihibits translocation |
| |Macrolides | | |Chloramphenicol |Same spectrum as Penicillin G, Mycoplasma, Chlamydia, |
| | | | | |Neisseira, Haemophilus, Legionella |
|Clarithromycin |Protein Synthesis Inhibitor | |Ototoxicity |↑ Warfarin |Improved acid stability, same as above & Toxoplasma, |
| |Macrolides | | |↑ Steroids |M. leprae & avium, longer t1/2 |
| | | | |↑ Digoxin |Less GI upset, renal elimination, Inhibits P450 |
| | | | |↑ Carbamexzapime| |
| | | | |Others | |
|Azithromycin |Protein Synthesis Inhibitor |Legionella (DOC) |Ototoxicity | |Similar to above; once/day dose; well tolerated |
| |Macrolides | | | |Less GI upset, Few interactions |
| | | | | |Doesn’t inhibit P450 |
|Drug |Class |Use |Side Effects |Interactions |Other |
|Clindamycin |Clindamycin |Oral (well absorbed) & Parenteral |Diarrhea, Colitis, ↓ hematopoietic |Chloramphenicol |Binds 50S, prevents translocation |
|(Cleocin) | |Bactericidal |Inhibits NMJ |Macrolides |Gram + & - anaerobes; Gets in bone |
| | |Anaerobic Infections (DOC) | | |Metabolized in liver, excreted in bile |
|Chloramphenicol |Protein Synthesis Inhibitor |Oral & Parenteral |Gray Baby Syndrome, GI Upset |Macrolides |Binds 50S, prevents bond formation |
| |Chloramphenicol |Bacteristatic |↓ Clotting (↓ Vitamin K), Allergies |Clindamycin |Broad Spectrum, Gets in CSF |
| | |S. typhi, Abscesses, Mixed Infections |BM Depression, Black Tongue |Anticoagulants |Hepatic Metabolism (glucuronate), renal secretion |
| | | | |Anti-HIV meds | |
| | | | |Phenytoin | |
|Synercid |Protein Synthesis Inhibitor |Parenteral (slow IV) |Pain & Phlebitis at infusion site |↑ Calcium |Binds two sites on 50S, prevents translocation |
|(Quniupristin/ |Streptogramin |Bacteristatic (some cidal) |Arthalgias & Myalgias |Blockers |Gram +, Few Gram – (Moraxella & Neiserria) |
|Dalfopristin) | |Reserved for resistant Gram + | |↑ Cyclosporine |Hepatic elimination (conjugation) |
|Linezolid |Protein Synthesis Inhibitor |Oral |Thrombocytopenia, GI Upset, Headache | |Prevents formation of f-met tRNA w/ 70S |
| |Linezolid |Bacteristatic (some cidal) |Rash | |Gram +; non-enzymatic oxidation |
| | |Reserved for resistant Gram + | | |Renal Elimination |
|Isoniazid |Tuberculocidal |Oral |Peripheral Neuritis (Vitamin B6) | |Crosses BBB/CSF; Excreted in urine |
| |(Mycolic Acid Synthesis Inhibitor) | |Rash, fever, hepatotoxic | |Metabolized by N-acetyl transferase |
| | | |Hypersensitivity | | |
|Pyrazinamide |Tuberculocidal |Oral |Hepatitis | |Bacteriostatic |
| |(Mycolic Acid Synthesis Inhibitor?) | |Hyperuricemia | |Resembles Nicotinamide; Crosses BBB |
| | | | | |Metabolized in liver; renal excretion |
|Ethambutol |Tuberculocidal |Oral |Optic Neuritis (blurring, loss of green) | |CSF Distribution less than serum; Not metabolized |
| | | |Anaphylaxis, Dermatitis, Anorexia | |Must be monitered for visual acuity since optic |
| | | |Nausea | |neuritis is reversible |
|Rifapentine |Rifamycin | |Similar to Rifampin | |Similar to Rifampin |
| |Similar to Rifampin | | | |Easier dosing than Rifampin (once weekly) |
|Ofloxacin |Fluoroquinolone | |GI Upset, Photosensitivity | |Inhibits DNA Gyrase |
| |Tuberculocidal | |CNS Effects | |Bacteriocidal |
| |(2nd Line) | | | | |
|Kanamycin |Tuberculocidal |IM |Ototoxic | |Bacteriostatic |
| |(2nd Line) | |Renal toxic | | |
|Capreomycin |Tuberculocidal |IM |Ototoxic | |Bacteriostatic |
| |(2nd Line) | |Renal toxic | | |
|Ethionamide |Tuberculocidal | | | |Inhibitor of mycolic acid synthesis? |
| |(2nd Line) | | | |Bacteriostatic |
| | | | | |Few Drug Interactions |
|Cycloserine |Tuberculocidal | | | |Competes with D-Alanine in protein synthesis |
| |(2nd Line) | | | |Bacteriostatic |
|p-amino-salicylic acid |Tuberculocidal | | | |Competetive inhibitor of PABA/Folate Synthesis |
| |(2nd Line) | | | | |
|Clofazamine |Tuberculocidal |Oral |GI Effects | |Slow bacteriocidal effect on M. leprae |
| |(2nd Line) | |Crystalline deposits in intestine | | |
|Drug |Class |Use |Side Effects |Interactions |Other |
|Zanamavir |Antiviral |Antiviral (Influenza A) |Few | |Inhibits neuraminidase |
| |(Influenza A) |Oral inhalation | | |Can shorten or prevent symptoms |
|Amandtidine |Antiviral |Antiviral (Influenza A) |Anticholinergic effects | |Prevents viral uncoating |
| |(Influenza A) |Anti-Parkinson’s | | |Prevents infections of Influenza A |
| | | | | |Prone to drug resistance |
|Rimantidine |Antiviral |Antiviral (Influenza A) |Anticholinergic effects | |Prevents viral uncoating |
| |(Influenza A) |Anti-Parkinson’s | | |Prevents infections of Influenza A |
| | | | | |Prone to drug resistance |
|Acyclovir |Antiviral |Antiviral (Herpes) | | |Inhibits viral DNA synthesis, chain elongation |
| |(Herpes) |Oral or Parenteral (IV) | | |Renal clearance, requires Thymidine Kinase |
| | | | | |Guanosine analog, binds viral DNA Polymerase |
|Valacyclovir |Antiviral |Antiviral (Herpes) | | |Preffered over acyclovir for genital herpes & VZV |
| |(Herpes) |Oral | | |Valine ester of acyclovir, better absorption |
|Ganciclovir |Antiviral |Antiviral (Herpes) | | |Preferred for treatment of immunosuppressed |
| |(Herpes) |Oral | | |Guanasine analog |
| | | | | |More effective against CMV than acyclovir |
|Vidaribine |Antiviral |Antiviral (Herpes) | | |Purine nucleoside analog |
| |(Herpes) |Oral | | |Inhibits viral DNA Polymerase & ribonucleotide |
| | | | | |reductase |
|Ribavrin |Antiviral |Antiviral (Herpes) | | |Guanosine analog; only approved for RSV |
| |(Herpes) |Oral inhalation | | |Both DNA & RNA viruses |
| | | | | |Inhibits polymerases & 5’ capping |
|Ziduvidine |Antiviral |Antiviral (HIV) | | |Pyrimidine analog, targets reverse transcriptase |
| |Reverse Transcriptase Inhibitor |Oral | | |Gets in CSF, renal elimination |
| | | | | |Lacks 3’ OH – Chain Terminator |
|ddInosine |Antiviral |Antiviral (HIV) | | | |
| |Reverse Transcriptase Inhibitor | | | | |
|D4T |Antiviral |Antiviral (HIV) | | | |
| |Reverse Transcriptase Inhibitor | | | | |
|3TC |Antiviral |Antiviral (HIV) | | | |
| |Reverse Transcriptase Inhibitor | | | | |
|Azidiuridine |Antiviral |Antiviral (HIV) | | | |
| |Reverse Transcriptase Inhibitor | | | | |
|Neviripine |Antiviral |Antiviral (HIV) | | |Blocks active site of reverse transcriptase |
| |Non-nucleoside RTI | | | | |
|Delaviridine |Antiviral |Antiviral (HIV) | | |Blocks active site of reverse transcriptase |
| |Non-nucleoside RTI | | | | |
|Drug |Class |Use |Side Effects |Interactions |Other |
|Loviride |Antiviral |Antiviral (HIV) | | |Blocks active site of reverse transcriptase |
| |Non-nucleoside RTI | | | | |
|Phosphonophormate |Antiviral |Antiviral (HIV) | | |Blocks active site of reverse transcriptase |
| |Non-nucleoside RTI | | | |Pyrophosphate analog |
|Saquinavir |Antiviral |Antiviral (HIV) | | |Inhibit cleavage of pol & gag proteins by protease |
| |Protease Inhibitor | | | |Progeny virions lack ability to reproduce |
|Indinavir |Antiviral |Antiviral (HIV) | | |Inhibit cleavage of pol & gag proteins by protease |
| |Protease Inhibitor | | | |Progeny virions lack ability to reproduce |
|Ritonavir |Antiviral |Antiviral (HIV) | | |Inhibit cleavage of pol & gag proteins by protease |
| |Protease Inhibitor | | | |Progeny virions lack ability to reproduce |
|T20 |Antiviral |Antiviral (HIV) | | |Blocks HIV entry |
| |Fusion Inhibitor |Parenteral (IV) | | |Binds coil domain on gp41 |
|Miconazole |Imidazole |Antifungal |Altered drug metabolism/sterol synthesis | |Topical use only |
| |Sterol Synthesis Inhibitor |TInea corporis, Tinea pedis, |Teratogen | | |
| |(Lanosterol Demethylase Inhibitor) |Vaginal Candidosis |Burning, Itching, Irritation | | |
|Fluconazole |Triazole |Antifungal; DOC = Candidosis |Altered drug metabolism/sterol synthesis |Warfarin |Slower metabolism; Less effect on human sterols |
| |Sterol Synthesis Inhibitor |DOC = Cryptococcal Meningitis |Teratogen |Cyclosporine |Crosses BBB |
| |(Lanosterol Demethylase Inhibitor) |DOC = Coccidiodal Meningitis |Nausea, Vomiting, Rash |Phenytoin |Inhibits P450 |
| | | | |Lovastatin | |
| | | | |Protease | |
| | | | |Inhibitors | |
|Itraconazole | |Antifungal | | |Similar to fluconazole |
| | | | | |Sporanox |
|Clotrimazole | |Antifungal | | |Lotrimin, Mycelex |
| | |DOC = Oral Fungal Infections | | | |
|Econazole | |Antifungal | | |Spectrazole |
|Butoconazole | |Antifungal | | |Femstat |
|Tioconazole | |Antifungal | | |Vagistat |
|Oxiconazole | |Antifungal | | |Oxistat |
|Terbinafine |Allyamine |Antifungal |Allergic reactions if given orally | |Oral, Topical, Future use Systemically? |
| |Sterol Synthesis Inhibitor |Tinea Infections Nail Infections |Not for use if hepatic impairment | |Concentrates in skin and nails |
| |(Squalene Epoxidase Inhibitor) |Bronchial Aspergillosis? |Dose adjustment for renal impairment | | |
|Drug |Class |Use |Side Effects |Interactions |Other |
|Amphotericin B |Polyene Macrolide |Systemic Administration |Fever, Chills, Allergic Reaction | |Binds ergosterol, Significant Renal Toxicity |
| |Fungal Membrane Disruption |(Broad Spectrum Antifungal) |Renal Dysfunction, Hypotension, Hypokalemia,| |Not for oral use |
| | | |Anemia, Thrombophlebitis | | |
|Nystatin |Polyene Macrolide |Oral Candidosis |Highly toxic if given IV | |Bitter Taste |
| |Fungal Membrane Disruption |Topical Administration | | |Minimal Oral Absorption |
| | |(Broad Spectrum Antifungal) | | | |
|Flucytosine |Pyrimidine |Oral Antifungal |BM Depression | |Requires cytosine specific permease, Crosses BBB |
| |DNA & Protein Synthesis Inhibitor | |Nausea, Vomiting, Diarrhea | |Converted to 5-FU; Resistance via ↓ uptake |
| |(Thymidilate Synthase Inhibitor) | | | |Synergistic with Amphotericin B |
|Griseofulvin |Fungal Mitosis Inhibitor |Oral Antifungal |Drug Interactions | |Specific to fungi; Concentrates in skin |
| |(Binds Microtubules) |(Microsporum, Trichophyton & |Allergic Reactions, Headache, Nausea | |Induces P450 |
| | |Epidermophyton) |Liver Toxicity? | | |
|Mechlorethamine |Cancer Chemotherapeutic |Hodgkin’s Disease |Myelosuppressive - Leukopenic | |Electrophile, reacts with nucleophiles (guanine N7) |
| |Alkylating/Covalent Binding |IV |Mucosal, Reproductive toxicicity | |Most Reactive, short t1/2 |
| |(Nitrogen Mustard) | |Some Nausea, Vomiting & Anorexia | |Part of MOPP Regimen; CCNS |
|Melphalan |Cancer Chemotherapeutic |Myeloma, Breast, Ovary | | |Electrophile, reacts with nucleophiles (guanine N7) |
| |Alkylating/Covalent Binding |Oral & IV | | |Phenyl Stabilization, Longer t1/2 |
| |(Nitrogen Mustard) | | | |Amino Acid Derivative; CCNS |
|Chlorambucil |Cancer Chemotherapeutic |Oral & IV | | |Electrophile, reacts with nucleophiles (guanine N7) |
| |Alkylating/Covalent Binding | | | |Phenyl Stabilization, Least Myelosuppressive |
| |(Nitrogen Mustard) | | | |CCNS |
|Cyclophosphamide |Cancer Chemotherapeutic |Breast Carcinoma |Hemorrhagic Cystitis (treat w/ MESNA) | |Electrophile, reacts with nucleophiles (guanine N7) |
| |Alkylating/Covalent Binding |Lymphocytic Leukemia (ALL) |Myelosuppression, Nausea, GI Ulcers | |Hepatic Metabolism, Part of FAC Regimen |
| |(Nitrogen Mustard) |Oral & IV |Allopecia | |Toxicity due to Acryline; CCNS |
|Carmustine |Cancer Chemotherapeutic |Lymphomas, Brain, |BM Toxicity/Myelosuppression | |Lipophilic (Crosses BBB), Not cross resistant |
| |Alkylating/Covalent Binding |Meningeal Leukemias | | |Most Useful |
| |(Nitrosurea) |IV | | |CCNS |
|Lomustine |Cancer Chemotherapeutic |Lymphomas, Brain, |BM Toxicity/Myelosuppression | |Lipophilic (Crosses BBB), Not cross resistant |
| |Alkylating/Covalent Binding |Meningeal Leukemias | | |CCNS |
| |(Nitrosurea) |IV | | | |
|Semustine |Cancer Chemotherapeutic |Lymphomas, Brain, |BM Toxicity/Myelosuppression | |Lipophilic (Crosses BBB), Not cross resistant |
| |Alkylating/Covalent Binding |Meningeal Leukemias | | |CCNS |
| |(Nitrosurea) |IV | | | |
|Streptozocin |Cancer Chemotherapeutic |Lymphomas, Brain, |Renal/Hepatic Toxicicty | |Lipophilic (Crosses BBB), Not cross resistant |
| |Alkylating/Covalent Binding |Meningeal Leukemias | | |Natural Nitrosurea, Little BM Toxicity |
| |(Nitrosurea) |IV | | |CCNS |
|Busufan |Cancer Chemotherapeutic |Chronic Granulocytic Leukemia | | |CCNS |
| |Alkylating/Covalent Binding |Oral | | | |
| |(Alkyl Sulfonate) | | | | |
|Cisplatin |Cancer Chemotherapeutic | |Nephrotoxic - Irreversible Renal Fibrosis | |Least myelosuppressive of Class |
| |Alkylating/Covalent Binding | |Worst Nausea, Vomiting & Anorexia of all | |Synergize with other cancer drugs |
| |(Platinum Complex) | | | |Combination Therapy; CCNS |
|Carboplatin |Cancer Chemotherapeutic | |Nephrotoxic | |Least myelosuppressive |
| |Alkylating/Covalent Binding | | | |Synergize with other cancer drugs |
| |(Platinum Complex) | | | |Combination Therapy; CCNS |
|Drug |Class |Use |Side Effects |Interactions |Other |
|Triethylenemelamine |Cancer Chemotherapeutic | | | |CCNS |
| |Alkylating/Covalent Binding | | | | |
| |Ethlenimines | | | | |
|Thiotepa |Cancer Chemotherapeutic | | | |CCNS |
| |Alkylating/Covalent Binding | | | | |
| |Ethlenimines | | | | |
|Hexamethylmelamine |Cancer Chemotherapeutic | | | |CCNS |
| |Alkylating/Covalent Binding | | | | |
| |Ethlenimines | | | | |
|Dacarbazine |Cancer Chemotherapeutic |Hodgkin’s Disease | | |Part of ABVD Regimen |
| |Alkylating/Covalent Binding | | | |CCNS |
| |Triazine | | | | |
|Procarbazine |Cancer Chemotherapeutic |Hodgkin’s Disease |Carcinogenic? | |Part of MOPP Regimen |
| |Alkylating/Covalent Binding | | | |Lipophillic – Crosses BBB |
| | | | | |CCNS |
|Methotrexate |Cancer Chemotherapeutic |Choriocarcinoma, Lung, Breast |Myelosuppression, Nausea, GI Ulcers | |Reduces Folate for A,G,T synthesis (DHFR) |
| |Antimetabolite/DNA Syn. Inhibitor |ALL, Osteosarcoma |Cirrhosis (if chronic) | |Combat toxicity with Leucovorin; CCS-S |
| |Folic Acid Analog |Oral | | |Doesn’t cross BBB, Cures Choriocarcinoma |
|5-Fluorouracil |Cancer Chemotherapeutic |Breast Carcinoma |Myelosuppression/GI Ulceration | |Inhibit Pyrimidine Synthesis, Incorporated into DNA |
| |Antimetabolite/DNA Syn. Inhibitor |IV |Unique Neurologic Toxicity | |Thymidilate Synthetase Inhibitor, Part of FAC Reg |
| |Pyrimidine Analog | | | |Erratic Absorption;GI, Hepatic Degradation; CCS-S |
|Cytarabine |Cancer Chemotherapeutic |Acute Myelocytic Leukemia | | |Inhibit Pyrimidine Synthesis, Incorporated into DNA |
| |Antimetabolite/DNA Syn. Inhibitor |IV | | |Improper stacking due to 2’-OH; CCS-S |
| |Pyrimidine Analog | | | |Erratic Absorption;GI, Hepatic Degradation |
|Mercaptopurine |Cancer Chemotherapeutic |ALL, Immunosuppresives |Hyperuricemia |Allopurinol |Inhibitor of purine synthesis/HGRT Salvage |
| |Antimetabolite/DNA Syn. Inhibitor |Antiviral, Gout |Myelosuppressive (Gradual) | |CCS-S |
| |Purine Analog |IV | | | |
|Thioguanine |Cancer Chemotherapeutic |IV | | |Inhibitor of purine synthesis/HGRT Salvage |
| |Antimetabolite/DNA Syn. Inhibitor | | | |Less toxic than mercaptopurine |
| |Purine Analog | | | |CCS-S |
|Hydroxyurea |Cancer Chemotherapeutic |Cervix, Head, Neck, Lung |Myelosuppressive | |RNA Reductase Inhibitor; CCS-S |
| |Antimetabolite/DNA Syn. Inhibitor |IV | | |(Rate limiting DNA in synthesis) |
| |Ribonucleotide Reductase Inhibitor | | | |Synergistic with Radiotherapy |
|Vincristine |Cancer Chemotherapeutic |Hodgkin’s Disease, Leukemia |↓ Myelosuppresion & Epithelial | |Anti-mitotic; binds tubulin, preventing polymerization|
| |Natural Products/CCS Drugs |Breast Cancer |↑ NEUROTOXIC | |Given IV (30% oral availability) |
| |Vinca Alkaloids |IV | | |Part of MOPP; CCS-M |
|Vinblastine |Cancer Chemotherapeutic |Hodgkin’s Disease |↑ Myelosuppresion & Epithelial | |Part of ABVD |
| |Natural Products/CCS Drugs |Testicular Carcinomas |↓ Neurotoxic | |CCS-M |
| |Vinca Alkaloids |Lymphomas | | | |
|Vinorelbine |Cancer Chemotherapeutic | | | |CCS-M |
| |Natural Products/CCS Drugs | | | | |
| |Vinca Alkaloids | | | | |
|Paclitaxel |Cancer Chemotherapeutic |Leukemia, Lymphoma, Breast & Testicular|Myelosuppression | |Anti-mitotic; stabilizes microtubules, prevents |
|(Taxol) |Natural Products/CCS Drugs |Cancer | | |depolymerizatrion; Hepatic metabolism |
| | |IV | | |Antagonized by anti-metabolites; CCS-M |
|Drug |Class |Use |Side Effects |Interactions |Other |
|Doxorubicin |Cancer Chemotherapeutic |Hodgkin’s Disease |Myelosuprresive | |Causes DNA Breaks, Part of ABVD & FAC Regimen |
|(Adriomycin) |Natural Products/CCS Drugs |Solid Breast and Ovarian Cancers |Irreversible Cardiomyopathy | |Inhibits DNA Topoisomerase, Free Radicals |
| |Antibiotic | | | |Intercalates; CCS-S Phase? |
|Bleomycin |Cancer Chemotherapeutic |Hodgkin’s Disease |Minimal Myelosuppressive | |Causes DNA Fragmentation. Complexes with FeO2 |
| |Natural Products/CCS Drugs | |Pulmonary Fibrosis | |Combination Therapies, Part of ABVD Regimen |
| |Antibiotic | | | |CCS-G2 Phase? |
|Actinomycin D |Cancer Chemotherapeutic |Some Childhood Cancers |Very Myelosuppressive | |DNA Intercalation, Inhibits RNA Pol II |
| |Natural Products/CCS Drugs | | | |CCS-? |
| |Antibiotic | | | | |
|Etoposide |Cancer Chemotherapeutic |Testicular Cancer |Dose Limiting Myelosuppression | |From Mandrake (May Apple); Synergistic w/ Platins |
| |Natural Products/CCS Drugs | | | |Stimulates DNA Topoisomerase to cleave DNA |
| |Epipodophyllotoxin | | | |CCS-S-G2 Interface |
|L-Asparginase |Cancer Chemotherapeutic | |Hypersensitivity due to antigenicicty | |Only enzyme used for cancer |
|Elspar |Natural Products/CCS Drugs | | | |Depletes asparagines (inhibits protein synthesis) |
| |Enzyme | | | |Minimal BM & GI side effects |
|Hydrocortisone |Cancer Chemotherapeutic |Hematological Cancers |Metabolic/Catabolic Manifestations | |Receptor Mediated Immunosuppresion |
| |Hormone/Antihormone |Oral |Changes in fat distribution, muscle mass | | |
| |Adrenocorticosteroid | |Osteoperosis | | |
|Dexamethasone |Cancer Chemotherapeutic |Hematological Cancers |Metabolic/Catabolic Manifestations | |Receptor Mediated Immunosuppresion |
| |Hormone/Antihormone |Oral |Changes in fat distribution, muscle mass | | |
| |Adrenocorticosteroid | |Osteoperosis | | |
|Prednisone |Cancer Chemotherapeutic |Hodgkin’s Disease |Metabolic/Catabolic Manifestations | |Receptor Mediated Immunosuppresion |
| |Hormone/Antihormone |Hematological Cancers |Changes in fat distribution, muscle mass | |Part of MOPP Regimen |
| |Adrenocorticosteroid |Oral |Osteoperosis | | |
|Leuprolide |Cancer Chemotherapeutic |Prostatic Carcinoma |Changes in fat distribution, muscle mass | |GnRH agonist inhibits androgen synthesis |
| |Hormone/Antihormone | |Osteoperosis | |Not curative, but palliative |
| |Androgen Deprivation | | | |Second choice after surgery |
|Cyproterone |Cancer Chemotherapeutic |Prostatic Carcinoma |Changes in fat distribution, muscle mass | |Androgen receptor antagonist |
| |Hormone/Antihormone | |Osteoperosis | |Second choice after surgery |
| |Androgen Deprivation | | | | |
|Flutamide |Cancer Chemotherapeutic |Prostatic Carcinoma |Changes in fat distribution, muscle mass | |Inhibits translocation of androgen receptor |
| |Hormone/Antihormone | |Osteoperosis | |Second choice after surgery |
| |Androgen Deprivation | | | | |
|Tamoxifen |Cancer Chemotherapeutic |Mammary Carcinoma |Changes in fat distribution, muscle mass | |Competitive Inhibitor of estrogen receptors |
| |Hormone/Antihormone | |Osteoperosis | |Given for metastases |
| |Estrogen Deprivation | |Hot Flashes/Nausea | | |
|Interferon α |Cancer Chemotherapeutic |Hairy Cell Leukemia | | |Activates T Cells, Macrophages, NK Cells |
| |Biological Response Modifier | | | | |
| |Interferon | | | | |
|Interleukin-2 |Cancer Chemotherapeutic |Kidney Cancer | | |Modulates T Cell proliferation and generation of |
| |Biological Response Modifier | | | |Killer T Cells |
| |Interleukin | | | | |
|Filgrastim |Cancer Chemotherapeutic | | | |Counters myelosuppresion during chemo for ↑ dose |
| |Biological Response Modifier | | | |Stimulates Granulocytes |
| |G-CSF | | | | |
|Drug |Class |Use |Side Effects |Interactions |Other |
|Sargramostim |Cancer Chemotherapeutic | | | |Counters myelosuppresion during chemo for ↑ dose |
| |Biological Response Modifier | | | |Stimulates Granulocytes & Macrophages |
| |GM-CSF | | | | |
|Aprotonin |Protease Inhibitor |Cardiopulmonary Bypass Surgery | | |From Bovine Lung |
| |(Kallikrein Inhibitor) | | | | |
|Cortisol |Glucocorticoid |Acute Flare Ups Only |Immunosuppressive | |Work on Intracellular (DNA) Receptor |
| | | |CNS effects – Mood, behavior | |Directly Inhibits COX |
| | | |Na+ and fluid retention (hypertension) | |Indirectly inhibits COX & Lox by ↓ Arachidonic Acid |
|Prednisone |Glucocorticoid |Acute Flare Ups Only |Immunosuppressive | |Work on Intracellular (DNA) Receptor |
| | | |CNS effects – Mood, behavior | |Directly Inhibits COX |
| | | |Na+ and fluid retention (hypertension) | |Indirectly inhibits COX & Lox by ↓ Arachidonic Acid |
|Dexamethasone |Glucocorticoid |Acute Flare Ups Only |Immunosuppressive | |Work on Intracellular (DNA) Receptor |
| | | |CNS effects – Mood, behavior | |Directly Inhibits COX |
| | | |Na+ and fluid retention (hypertension) | |Indirectly inhibits COX & Lox by ↓ Arachidonic Acid |
|Cortisone |Glucocorticoid |Acute Flare Ups Only |Immunosuppressive | |Work on Intracellular (DNA) Receptor |
| | | |CNS effects – Mood, behavior | |Directly Inhibits COX |
| | | |Na+ and fluid retention (hypertension) | |Indirectly inhibits COX & Lox by ↓ Arachidonic Acid |
|Acetaminophen |Central COX Inhibitor |Antipyretic & Analgesic |Hepatic Toxicicty (esp. with alcohol) | |Not an NSAID; Poorly inhibits COX |
| | |(Useful when aspirin contraindicated) | | |No platelet function |
| | | | | |No effect on acid/base or uric acid |
|Aspirin |NSAID |Integument Analgesic, Migraine |Not for use with Peptic Ulcers; Reye’s | |COX Inhibitor (Covalently modifies COX1 & COX2) |
| |(Carboxylic Acid – Salicylate) |Antipyretic, Antiinflammatory (↑ dose) |Tinnitus, Deafness, Vertigo | |Suicide Inhibitor of COX1 & stimulator of LOX |
| | |Anticoagulant, Colon Cancer, MI |Alkalosis,Acidosis,Fever, Dehydration | |Highly Dose Dependent – Not for Gout! |
|Salicylic Acid |NSAID | | | | |
| |(Carboxylic Acid – Salicylate) | | | | |
|Methyl Salicylate |NSAID | | | | |
| |(Carboxylic Acid – Salicylate) | | | | |
|Indomethacin |NSAID |Anti-inflammatory |Toxic | |Inhibits prostaglandin inflammation of Gout |
| |(Acetic Acid) |Gout | | |Inhibits macrophage urate phagocytosis |
|Sulindac |NSAID |Breast Cancer? |Gastric Distress | |A prodrug – converted by P450 |
| |(Acetic Acid) | | | |Decreased incidence of breast cancer in animals |
|Etodolac |NSAID | |Toxic | |Some COX2 selectivity |
| |(Acetic Acid) | | | | |
|Mefenamic Acid |NSAID | |High incidence of diarrhea | |Little clinical use |
| |(Fenamic Acid) | | | | |
|Meclofenamic Acid |NSAID | |High incidence of diarrhea | |Little clinical use |
| |(Fenamic Acid) | | | | |
|Drug |Class |Use |Side Effects |Interactions |Other |
|Tolmetin |NSAID | | | |Similar to aspirin, but better tolerated |
|Ketorolac |NSAID |Analgesic | | |Poor inhibitor of inflammation |
| | |Allergic Conjunctivitis | | |Approved for topical, parenteral & oral use |
| | |Occular Inflammation | | |Short Term Use only |
|Diclofenac |NSAID |Rheumatoid Arthritis | | | |
| | |Osteoarthritis | | | |
| | |Ankylosing Spondylitis | | | |
|Ibuprofen |NSAID |Antiinflammatory, Migraine | | |Better tolerated than aspirin |
| |(Propionic Acid) |Analgesic, Antipyretic | | |Also for Ankylosing Spondylitis & Dysmenorrhea |
| | |Rheumatoid Arthritis & Osteoarthritis | | | |
|Naproxen |NSAID |Rheumatoid Arthritis |GI & CNS Side effects | |Better tolerated than Indomethacin |
| |(Propionic Acid) |Osteoarthritis |Not for pediatric use | |Especially good for menstral migraine prophylaxis |
| | |Migraine, Fever | | |As good as Methysergide for migraines |
|Fenoprofen |NSAID | | | | |
| |(Propionic Acid) | | | | |
|Ketoprofen |NSAID | | | | |
| |(Propionic Acid) | | | | |
|Flurbiprofen |NSAID | | | | |
| |(Propionic Acid) | | | | |
|Nimesulide |NSAID |Antiinflammatory | | |Poorly inhibits COX1 in seminal vessicles |
| |(Propionic Acid) | | | | |
|Celecoxib |NSAID |Rheumatoid | | |Reduced gastric toxicity |
| |(Selective COX2 Inhibitor) |Osteoarthritis | | | |
| |(1st Gen) | | | | |
|Rofecoxib |NSAID |Antiinflammatory |Increased risk of CV thrombosis | |Inhibits the inducible COX-2 |
| |(Selective COX2 Inhibitor) |Rheumatoid Arthritis |Renal Toxicity | |Longer t1/2 & smaller dose than Celecoxib (but qid) |
| |(1st Gen) |Osteoarthritis & Acute Pain | | | |
|Piroxicam |NSAID |Breast Cancer? | | |Extremely long t1/2 (57 hrs) |
| |(Enolic Acid) | | | |Suppressed breast cancer growth in animal models |
|Colchicine |Plant Alkaloid |Gout Diagnosic |Diarrhea, Nausea, Vomiting, Hair Loss | |Relieves pain & inflammation of gout, not analgesic |
| |(Autumn Crocus) |Gout (Inflammation Relief) |Abdominal Pain, BM Suppression | |Inhibits tubulin polymerization/LTB4 (Neutrophils) |
| | |Given 6 mos without 3-4 week “holiday” |
| | | | | |Only for not responsive to other prophylactics |
|Valproate/Divalproex |Anticonvulsants | |Weight Gain, Hair Loss, Tremor | | |
| | |Migraine Headache |Teratogen (Neural Tube Defects) | | |
| | | | | | |
|Drug |Class |Use |Side Effects |Interactions |Other |
|Retrovirus |Gene Therapy Virus |Minor Use (10%) |Mutagenesis/Cancer (Leukemia?) | |Requires target cells to have a specific receptor |
| |(RNA Virus) |SCID (γc gene) |Recombination with other retroviruses | |Only integrate into dividing cells |
| | | | | |Expression is long term; Particles quickly degraded |
|Adenoviruses |Gene Therapy Virus |Major Use (40%) |Inflammatory & Toxic Immune Response | |Controlled via helper protein requirement |
| |(DNA Virus) |Cystic Fibrosis (CFTR gene) |Viral Particles may be neutralized | |Can infect any cells, High Titers |
| | |Cancer (ONYX-015), Erythropoietin |Not long term | | |
|Conditionally Replicating |Gene Therapy Virus |Cancer (ONYX-015) |Inflammatory & Toxic Immune Response | |Controlled via helper protein requirement |
|Adenoviruses |(DNA Virus) | |Viral Particles may be neutralized | |Can infect any cells, High Titers |
| | | |Not long term | |Selectively lyses p53 deficient cells |
|Replication-Defective |Gene Therapy Virus |DMD |Less Immune Response | |Lacks viral genes; Packaged via helper cells |
|Adenovirus |(DNA Virus) | | | |Uses creatine kinase promoter (muscle specific) |
|Adeno-associated Virus |Gene Therapy Virus |Minor Use (10%) |Limited size capacity for genes | |Requires 3 plasmids & helper virus (more work) |
| |(DNA Virus) |Cystic Fibrosis (CFTR gene) |High Titers of pure virus is hard to get | |Can infect wide range of cells |
| | |DMD |Mutagenesis/Cancer; Semen Infection? | |Virus integrates into genome – Long Term |
|Cationic Liposomes |Gene Therapy Non-Viral Vector |Cystic Fibrosis (CFTR gene) |Relatively safe & noninfectious | |Plasmid coated with lipophilic molecules |
| | | |Not specific ,Transient | |Poorly understood; Doesn’t integrate |
| | | |Immune Response? | |No size limit; could use interfering RNA |
|Naked Plasmid |Gene Therapy |Cardiovascular Disease (VEGF-2) | | |Low cost? |
| | |Erythropoietin | | |Only transient expression |
| | |DNA Vaccine | | | |
|Ex Vivo |Gene Therapy |DMD |Few cells survive, Large gene size | |Uses retrovirus infection in culture then transplanted|
|Myoblast Transplant | | |Dystrophin expression lost | | |
| | | |Immune Response | | |
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