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 | |

................
................

In order to avoid copyright disputes, this page is only a partial summary.

Google Online Preview   Download