UPDATED AntiCancer Drugs, Final Enhanced Edition
Ken’s super efficacious, low fat, high calorie PHARM NOTES II½: The final frontier
UPDATED AntiCancer Drugs, Final Enhanced Edition
|Subclass |Prototype |Variants |Clin |Major Side FX |
| | | |Pharm | |
|Alkylating Agents | | | | |
|Mustards |Mechlorethamine | |Rapid |GI, BM, alopecia, extravasation |
| | | |inactivation | |
| | |Cyclophosphamide | |GI, BM, alopecia, hemorrhagic cystitis |
| | | |Biotransformati| |
| | | |on required |modest BM, Nausea, emesis |
|Triazenes |Dacarbazine (DTIC) | | |Renal failure, ototox, neurotox, emesis, |
|Platinum compounds |Cisplatin (DDP) | | |rare BM |
| | | |P450 in liver |More BM, rare nausea |
| | |Carboplatin | | |
| | | |Renal clear | |
| | | | | |
| | | | | |
|Antibiotics |Doxorubicin | |Liver |GI, BM, alopecia, cardiac damage, |
| | | |biotransformati|extravasation |
| | |Dantorubicin |on |Cardiac damage |
| |Bleomycin | | |Lung fibrosis, anaphylax, mucocutaneous |
| | | | | |
| | | |Renal clear | |
|Plants | | | | |
|Vinca alkaloids |Vincristine | |Hepatic clear, |Neurotox, extravasation, little BM |
| | | |long t1/2 | |
| | |Vinblastine | |BM, rare neurotox |
|Epipodophyllotoxins |Etoposide | |Short t1/2 |GI, BM, neuropathy, vasomotor |
| | | | |hypersensitivity |
|Yew Tree derivatives |Paclitaxel (TaxolR) |Taxotere |Sched | |
| | |(H20 soluble) |dependent, hep|BM, hypersensitivity, hypotension, |
| | | |biotrans, renal|bradycardia, neuropathy, |
| | | |clear |arthralgia/myalgia, severe alopecia, |
| | | | |occasional hepatic dysfunction |
| | | |Pacitel: | |
|Camptothecin |Irinotecan [CPT-11] | |Slow IV, liver |GI, BM, mucosistis, alopecia |
|derivatives | | |metabolized, | |
| | | |extensive | |
| | | |nonrenal | |
| | | |clearance | |
| | | | | |
| | | | | |
| | | |Prodrug, sched | |
| | | |dependent | |
|Antimetabolites |Methotrexate | |Renal clear |GI, BM, liver dysfunc, mucositis |
| | | | | |
| |5-fluorouracil (5-FU) | | |GI, BM |
| |Cytarbine(cytosine arabinoside; ara-c) | |Extensive |GI, BM, neurotox, mucositis |
|Purine analogs |6-mercaptopurine (6-MP) | |metab. | |
| |(watch interaction w/allopurinol) | | |BM, liver damage |
| | | |Biotrans, | |
| | | |sched. | |
| | | |Dependent | |
| | | | | |
|Associated drugs | |Allopurinol (prevent uric | | |
| | |acid nephropathy) | | |
|Hormones | | | | |
|Estrogens |Estrogen, diethylstibestrol; DES | | | |
|Antiestrogen |Tamoxifen | | |Flushing, leukopenia, rare hypercalcemia |
| | | | |Multiple organ FX |
|Glucocorticoids |Prednisone (short t1/2) |Dexamethasone | | |
| | |(long ½) | | |
|Progestins |Megestrol acetate (Megace) | | | |
|Androgens (rarely | | | | |
|used) |Flutamide | | | |
|Antiandrogens |Leuprolide, | | | |
|LHRH/GNRH agonists |goserelin (Zoladex) | | | |
| |octreotide acetate | | | |
|Misc agents |Procarbazine (Matulane) | | |GI, BM, disulfiram-like rxn, neurotox, |
| | | | |allergy, rash, carinogen |
Chemo section optimized for Ignarro final, includes only Bold or highlighted drugs, and includes Side FX and clinical pharmacology notes.
AntiViral Drugs
|Subclass |Prototype |Variants |Indications |
|Respiratory Virus |Amantadine |Rimantadine |Influenza A |
| |Ribavirin | |RSV |
|Herpes Virus |Acyclovir (poor bioavailability) |Famiciclovir |HSV-1, HSV-2, VZV, herpes encepalitis |
| | |Valcyclovir (great | |
| | |bioavail) |HSV-1, HSV-2, VZV, herpes encepalitis in |
| | |Vidarabine (IV) |immunocomp. |
| | | |HSV-1, HSV-2, VZV, herpes encepalitis, |
| |Foscarnet | |AND CMV retinitis |
| | | |Topical herpes |
| | |Idoxuridine |CMV |
| |Ganciclovir | | |
|HIV | | | |
|Reverse Transriptase |Zidovudine (AZT) (short t1/2) |Stavudine | |
|Inhibitors | |Lamivudine | |
| | |(both with long t1/2) | |
|Protease Inhibitors |Saquinavir |Ritonavir | |
|(all P450 inducers) | |Indinavir | |
| | |Nelfinavir | |
| | | | |
| |Atovaquone | |For oral P. Carinii pneuomia in |
| | | |Co-Trimoxazole intolerant pts. |
|Other drugs |Trifluridine |Fluorouracil |Topical Antivirals |
|Triple Therapy |AZT, + another Rev transcriptase inhibitor,| | |
| |+ protease inhibitor | | |
Folate Antagonists
|Subclass |Prototype |Spectrum |Indications |
|Inhibitors of Folate Syn |Sulfadiazine |Various |Concentrates in brain/CSF |
| |Sulfamethoxazole | |Used w/ Trimethoprim |
| |Sulfasalazine | |GI tract, not absorbed well |
| |Sulfisoxazole | |Most effective drug used alone |
| |Sulfacetamide | |Topically for eye |
| |Mafenide | |Topically for burn injury infect. |
|Inhibitor of Folate Reduction |Trimethoprim | | |
|Combination |Co-Trimoxazole |P.Carinii pneumonia |UTIs, RTIs, GI tract, gonorrhea, also |
| |(trimethoprim + sulfamethoxazole) |Neisseria gonorrhea |P.carinii, Isospora Bella in HIV |
| | |Neisseria Meningitidis | |
| | |H. Influenzae | |
| | |Strep pneumoniae | |
| | |Legionella pneumophilia | |
| | |E.Coli | |
| | |Proteus Mirabilis | |
| | |Salmonella typhi | |
| | |Shigella | |
*UTI- urinary tract infection, RTI- respiratory tract infections
Cell Wall Synthesis Blockers
|Subclass |Prototype |Spectrum |Indications |
|Penicillins (β-lactam) | | | |
|Natural Penicillins |Penicillin G (IV) |Staph A (resistant) |Pen G effective most anaerobes except |
|(β-lactamase labile) |Penicillin V (oral) |Strep |B. Fragilis. Pen V less effective |
| | |Neisseria gonorrhea |against gm (-) than Pen G (Neisseria, |
| | |N. Meningitidis |Haemophilus and some anerobes) |
| | |Treptonema pallidum | |
| | |Leptotrichia Buccalis |Indicate: Strep, pneumococcal inf |
| | |Bacilus anthracis |(inc. pneumonia, meningitis, otitis), |
| | |Clostridium perfringes |anaerobic inf, gonococcal inf, |
|Antistaph Penicillins |Cloxacillin |Corynebac. Diptheriae |syphilis |
|(all beta-lactamase stable) |Dicloxacillin |Listeria monocytogenes | |
| |Methicillin (most staph are resistant) | | |
| |Nafcillin |Penicillinase producing Staph | |
| |Oxacillin | | |
| | | | |
|Extended Spectrum |Ampicillin | | |
|Penicillins |Amoxicillin | | |
|(beta-lactamase labile) | | | |
| | |Include all Pen G bugs plus: |Gm (-) Enterobacteriaceae , |
| | |H. Influenzae |RTIs by H.Influenzae, uncomplicated |
| | |Listeria monocytogenes |UTIs |
|Antipsuedomonas |Piperacillin |E.Coli | |
|Penicillins |Mezlocillin |Proteus mirabilis |Use w/ Clavulanic Acid or Sulbactam to|
|(β-lactamase labile) |Carbenicillin |Samonella Typh |prevent penicillinases |
| |Azlocillin | | |
| |Ticarcillin | | |
| | | |For klebsiella use ticarcillin and |
| | |H. Influenzae |clavulanic acid to fight |
| | |Pseudomonas aeruginosa |penicillinases |
| | |Enterobacter species | |
| | |E.Coli | |
| | |Proteus mirabilis | |
|Cephalosporins (β-lactam) | | | |
|G1 (more gm + action |Cefazolin |Staph, Strep | |
|Less gm – action) | |Anaerobic strep | |
| | |Proteus mirabilis, E.Coli, | |
|G2 |Cefotetan |Klebsiella peneumoniae (PEcK) | |
| |Cefoxitin | |Cefotetan also for B. fragilis |
| |Cefamandole *odd Side FX |Some Streps, | |
| | |H. Influenza, Enterobacter | |
|G3 (no gm + action |Cefixime |aerogenes, N. gonorrhea, and |Cefotaxime drug of choice for H. |
|Lots of gm – action) |Cefotaxime |PEcK, so HEN PEcK |Influenzae meningitis (lipophillic) |
| |Cefoperazone *odd Side FX | | |
|G3 Achieves theraputic | |HEN PEcK and | |
|levels in CSF | |Pseudomonas aeruginosa | |
| | |Serratia Marcesans | |
|Carbapenems |Imipenem (w/cilistatin to prevent |Penicillinase producing Gm + |Broadest Spectrum of the B-lactams, |
|(…ƒ‚€€€}|{{zxwxwtrrpnmllkjihhggghi|kidney metabolism) |and Gm – as well as P. |penicillinase resistant! |
|β-lactam) |Meropenem |aeruginosa | |
|Monobactams (β-lactam) |Aztreonam |Enterobacter species |Narrow Spectrum for bactermia, UTIs, |
| | |P. aeruginosa |RTIs, osteomyelitis, skin suture |
| | | |infections |
|Other non β-lactam cell | | | |
|wall synthesis blockers |Vancomycin (IV) |Bactericidal: staph, strep |Only Gm + bacteria, not effective |
| | |Bacteriostatic: enterococci |orally-good for psuedomembranous |
| | |(use w/ aminoglycosides for |colitis by |
| | |bactericidal FX) , |C. difficile, drug of choice for |
| | |C. difficile |Methicillin resistant S. aureus |
| |Bacitracin | | |
| | | |Used topically for wide variety of Gm |
| | | |+ organisms |
Inhibitors of Protein Synthesis
|Subclass |Prototype |Spectrum |Indications |
|Tetracyclines BROAD |Minocycline (lipophillic) |Mycoplasma pneumoniae |Preferred for Rocky Mountain fever, |
|(bind 30S) |Doxycycline (lipophillic) |Rickettsia rickettsii |typhus, mycoplasma RTIs, chlamydia, |
| |Tetracycline |Corynebacterium acnes |NOT for UTIs anymore! |
|(all tetracyclines, except |Demclocycline |H. Inluenzae |Doxyclycline for traveller’s diarrhea |
|doxycycline[biliary excretion] | |Zibrio cholerae | |
|toxic to kidney) | |Chamydia | |
| | |Borrelia burgdorferi | |
| | |Treponema pallidum | |
| | |Helicobacter pylori | |
| | | | |
|Aminoglycosides |Gentamicin |Pseudomonas aeruginosa |ONLY for serious, aerobic bac |
|(bind 30S) |Tobramycin |Vibrio cholerae |NOT for initial gm + therapy |
| |Netilmicin |Yersinia pestis |Mostly effective vs. Aerobic gm – |
| |Streptomycin |Francisella tularensis |bacteria, |
| |Amikacin |Enterobacter aerogenes |most staph, strep inhibited. |
| |Neomycin |E. Coli |Complicated UTIs |
| |Kanamycin |Klebsiella pneumoniae |Also for endocarditis from ennerococci|
| | |Proteus |or viridans, use Gentamicin due to |
| | |Serratia marcescens |streptomycin resistance. |
|Erythromycin BROAD | |All Pen G bugs, and is drug of |Used to treat patients allergic to |
|(binds 50S) | |choice for: |Penicillin |
| | |Mycoplasma peumonia | |
| | |Treponema pallidum | |
| | |Chlamydia | |
| | |H. influenzae | |
| | |Legionella pneumophilia | |
| | |Corynebac diptheriae | |
|Chloramphenicol BROAD | |GREAT for B. fragilis |NOT for UTIs, RTIs, brucellosis, since|
|(binds 50S) | |Chlamydiae, rickettsiae, |quite toxic |
| | |mycoplsma | |
|Clindamycin | |Most gm + cocci, and gm – |Penicillin alternative to |
|(binds 50S) | |anaerobes, NOT gm – aerobes |penicillinase producing bugs |
| | |B. fragilis | |
|Spectinomycin | |Neisseria gonorrhoeae |ONLY for acute gonorrgea by |
|(binds 30S) | | |penicillinase producing Neisseria |
Quinolones and Urinary Tract Antiseptics
|Subclass |Prototype |Spectrum |Indications |
|Quinolones |Nalidixic acid | |Most gm – bac in UTIs, gm + bac are |
| | | |resistant! |
|Fluoroquinolones |Norfloxacin | | |
|(blocks topo II) |Ciprofloxacin |H. Ingluenzae |Norfloxacin stronger than nalidixic |
| |Sparfloxacin |Legionella pneumonphilia |acid, effective vs. gm + and gm – and |
| |Ofloxacin |Pseudomonas aeruginosa |is for uncomplicated UTIs, prostatitis|
| |Enoxacin |Neisseria gonorrhea | |
| |Lomefloxacin |Enterobacter |Cipro more potant than norfloxacin, |
| |Levofloxacin |E.Coli | |
| |Perfloxacin |Klebsiella pneumoniae | |
| | |Proteus mirabilis | |
| | |Serratia marcescens | |
| | |shigella | |
|Methenamine | | |Chronic therapy vs. UTIs. NEVER give |
| | | |sulfonamides w/ methenamine! Chemical |
| | | |rxns! |
|Nitrofurantoin | |Bacteriostatic vs. E.coli | |
AntiMycobacterial Drugs
|Subclass |Prototype |Spectrum |Indications |
|Tuberculosis Drugs |Isoniazid (INH) – NARROW |M. tuberculosis, M. kansasii | |
|(used in combo) |Rifampin – BROAD | | |
| | |M. tuberculosis, M. kansasii | |
| | |Also for leprosy, meningitis by| |
| | |N. meningitidis, or H. | |
| |Ethambutol |influenzae, also most Gm + bac,| |
| |Pyrzainamide |enteric species and anaerobes! | |
| | | | |
| | |M. tuberculosis, M. kansasii | |
| | |M. tuberculosis, M. kansasii | |
|Tuberculosis Drugs (2nd | | | |
|line of defense) |Ethionamide | | |
| |Cycloserine | | |
|Leprosy Drugs |Rifampin | |Dapsone also for P. carinii in AIDS |
|(used in combo) |Dapsone | |pts. |
| |Clofazimine |Bacteriostatic for M. leprae | |
Anti Fungal Drugs
|Subclass |Prototype |Spectrum |Indications |
|For SubQ and systemic |Amphotericin B – BROAD |Candida, histoplasma | |
| | |capsulatum, cryptococcus, | |
| |Flucytosine (only w/ Ampho B) |coccidioides, aspergillus, | |
| |Ketoconazole |blastomyces |Requires acid pH, and Never w/ |
| | |Systemic mycoses |ketoconazole! |
| |Fluconazole, newer |Systemic and cutaneous mycoses | |
| | | |Choice for cryptococcal |
| | | |meningoencepalitis, disseminated |
| | | |histoplasmosis, coccidioidomycosis |
| | |Candida, cryptococci, | |
| | |blastomyces, histoplasma | |
|For superficial infections |Griseofulvin (oral!) | | |
| |Nystatin (oral only) | |Topical candidiasis |
| |Miconazole, clotrimazole, |Candida | |
| |Econazole (all topical) | | |
| |Tolnaftate (TinacinR) |Candida and ringworm |Topical dermatophytes, but NOT candida|
AntiHelmintic Drugs
|Subclass |Prototype |Spectrum |Indications |
|Anti Nematodes |Mebendazole |Whipworm trichuris trichiura |NOT during pregnancy |
| | |Pinworm Enterobiu vermicularis | |
| | |Hookworm Necator americanus | |
| | |Ancylostoma duodenale | |
| |Thiabendazole | | |
| | | | |
| |Pyrantel pamoate |Strongloidiasis | |
| | |Trichinella spiralis | |
| | | | |
| |Diethylcarbamzine |Roundworm Ascaris lumbricoides | |
| | |Pinworm Enterobiu vermicularis | |
| |Ivermectin |Hookworm Necator americanus | |
| | | | |
| | |Filariasis Wuchereria bancrofti| |
| | |Brugia malyi | |
| | | | |
| | |Filariasis Onchocerca volvus | |
|Anti Trematode |Praziquantel (CSF) |All forms of schistosomiasis |Most pts show no SEs |
| |Oxamniquine | |Largely replaced by praziquantel |
| |Metrifonate | |Largely replaced by praziquantel |
|Anti Cestodes |Niclosamide |Taenia solium |CHOICE for most cestode and tapeworms |
AntiProtozoal Drugs
|Subclass |Prototype |Spectrum |Indications |
|Mixed amebicides |Metronidazole |CHOICE FOR: |Also for anaerobic Gm + and Gm - |
| | |Entamoeba histolytica |bacteria |
| | |Giardia lamblia | |
| | |Trichomonas vaginalis | |
|Luminal amebicides |Diloxanide furoate |Intestinal amebiasis |For asymptomatic passers of cysts |
| | | | |
| |Tetracycline | | |
| |Paromycin | | |
| | | | |
| | |Only for intestinal/luminal | |
| | |forms of amebiasis and tapeworm| |
|Systemic amebicides |Emetine | |Emetine, dehydroemetine alternates b/c|
| |Dehydroemetine | |toxicities |
| |Chloroquine | | |
| | |Malaria, liver trophozoites | |
|Leishmaniasis |Sodium stibgluconate | | |
|Trypanosomiasis |Melarsoprol |Trypanosomal infections | |
| | | | |
| | |Trypanosoma rhodensiense, |For meningoencephalitis (gets to CNS) |
| |Pentamidine |T. brucei gambiense | |
| | | |Co-tramoxazole is preferred for P. |
| | |Protozoal inf, including |carinii, Pentamidine is 2nd choice |
| | |Pneumocystis carinii, and | |
| |Nifurtimox |choice for nematologic state | |
| |Suramin |of T. brucei gambiense | |
| | | | |
| | |Only for T. cruzi | |
| | | | |
| | |African trypanosomiasis | |
| | |prophylaxis, CHOICE for | |
| | |filarial parasites like | |
| | |Onchocerca volvulus | |
|Toxoplasmosis |Pyrimethamine | | |
| |Sulfadiazine + pyrimethamine | | |
|Malaria | | | |
|Tissue schizontcide |Primaquine | | |
| | |Primary exoerythrocytic : | |
| | |P. falciparum, P vivax | |
| | |Secondary exoerythrocytic : | |
|Blood schizonticide |Chloroquine |P. vivax and P. ovale | |
| | | | |
| |Quinine (usually w/pyrimethamine, and |Erythrocytic falciparum |For resistant malarial strains |
| |sulfonamide) |malaria, also for asexual form | |
| | |of P. vivax and P. falciparum | |
| |Melfloquine | | |
|Blood shizontcide and | | | |
|sporonticide |pyrimethamine | | |
| | |Multidrug resistant P. | |
| | |falciparum | |
| | | | |
| | | | |
| | |P. falciparum, | |
| | |with sulfonamide also for P. | |
| | |malariae and Toxoplasma | |
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