Ken’s super efficacious, low fat, high calorie PHARM NOTES II½: The final frontier

UPDATED AntiCancer Drugs, Final Enhanced Edition

Subclass

/

Prototype

/

Variants

/

Clin

Pharm
/

Major Side FX

Alkylating Agents
Mustards
Triazenes
Platinum compounds / Mechlorethamine
Dacarbazine (DTIC)
Cisplatin (DDP) / Cyclophosphamide
Carboplatin / Rapid inactivation
Biotransformation required
P450 in liver
Renal clear / GI, BM, alopecia, extravasation
GI, BM, alopecia, hemorrhagic cystitis
modest BM, Nausea, emesis
Renal failure, ototox, neurotox, emesis, rare BM
More BM, rare nausea
Antibiotics / Doxorubicin
Bleomycin / Dantorubicin / Liver biotransformation
Renal clear / GI, BM, alopecia, cardiac damage, extravasation
Cardiac damage
Lung fibrosis, anaphylax, mucocutaneous
Plants
Vinca alkaloids
Epipodophyllotoxins
Yew Tree derivatives
Camptothecin
derivatives / Vincristine
Etoposide
Paclitaxel (TaxolR)
Irinotecan [CPT-11] / Vinblastine
Taxotere
(H20 soluble) / Hepatic clear, long t1/2
Short t1/2
Sched dependent, hep biotrans, renal clear
Pacitel:
Slow IV, liver metabolized, extensive nonrenal clearance
Prodrug, sched dependent / Neurotox, extravasation, little BM
BM, rare neurotox
GI, BM, neuropathy, vasomotor hypersensitivity
BM, hypersensitivity, hypotension, bradycardia, neuropathy, arthralgia/myalgia, severe alopecia, occasional hepatic dysfunction
GI, BM, mucosistis, alopecia
Antimetabolites
Purine analogs / Methotrexate
5-fluorouracil (5-FU)
Cytarbine(cytosine arabinoside; ara-c)
6-mercaptopurine (6-MP)
(watch interaction w/allopurinol) / Renal clear
Extensive metab.
Biotrans, sched. Dependent / GI, BM, liver dysfunc, mucositis
GI, BM
GI, BM, neurotox, mucositis
BM, liver damage
Associated drugs / Allopurinol (prevent uric acid nephropathy)
Hormones
Estrogens
Antiestrogen
Glucocorticoids
Progestins
Androgens (rarely
used)
Antiandrogens
LHRH/GNRH agonists / Estrogen, diethylstibestrol; DES
Tamoxifen
Prednisone (short t1/2)
Megestrol acetate (Megace)
Flutamide
Leuprolide,
goserelin (Zoladex)
octreotide acetate / Dexamethasone
(long ½) / Flushing, leukopenia, rare hypercalcemia
Multiple organ FX
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
Ribavirin / Rimantadine / Influenza A
RSV
Herpes Virus / Acyclovir (poor bioavailability)
Foscarnet
Ganciclovir / Famiciclovir
Valcyclovir (great bioavail)
Vidarabine (IV)
Idoxuridine / HSV-1, HSV-2, VZV, herpes encepalitis
HSV-1, HSV-2, VZV, herpes encepalitis in immunocomp.
HSV-1, HSV-2, VZV, herpes encepalitis, AND CMV retinitis
Topical herpes
CMV
HIV
Reverse Transriptase
Inhibitors
Protease Inhibitors
(all P450 inducers) / Zidovudine (AZT) (short t1/2)
Saquinavir
Atovaquone / Stavudine
Lamivudine
(both with long t1/2)
Ritonavir
Indinavir
Nelfinavir / 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

Sulfamethoxazole
Sulfasalazine
Sulfisoxazole
Sulfacetamide
Mafenide /

Various

/

Concentrates in brain/CSF

Used w/ Trimethoprim
GI tract, not absorbed well
Most effective drug used alone
Topically for eye
Topically for burn injury infect.

Inhibitor of Folate Reduction

/

Trimethoprim

/ /

Combination

/

Co-Trimoxazole

(trimethoprim + sulfamethoxazole) /

P.Carinii pneumonia

Neisseria gonorrhea

Neisseria Meningitidis

H. Influenzae

Strep pneumoniae
Legionella pneumophilia
E.Coli
Proteus Mirabilis
Salmonella typhi

Shigella

/

UTIs, RTIs, GI tract, gonorrhea, also P.carinii, Isospora Bella in HIV

*UTI- urinary tract infection, RTI- respiratory tract infections

Cell Wall Synthesis Blockers

Subclass

/

Prototype

/

Spectrum

/

Indications

Penicillins (b-lactam)
Natural Penicillins
(b-lactamase labile)
Antistaph Penicillins
(all beta-lactamase stable)
Extended Spectrum
Penicillins
(beta-lactamase labile)
Antipsuedomonas
Penicillins
(b-lactamase labile) / Penicillin G (IV)
Penicillin V (oral)
Cloxacillin
Dicloxacillin
Methicillin (most staph are resistant)
Nafcillin
Oxacillin
Ampicillin
Amoxicillin
Piperacillin
Mezlocillin
Carbenicillin
Azlocillin
Ticarcillin / Staph A (resistant)

Strep

Neisseria gonorrhea
N. Meningitidis

Treptonema pallidum

Leptotrichia Buccalis
Bacilus anthracis
Clostridium perfringes

Corynebac. Diptheriae

Listeria monocytogenes

Penicillinase producing Staph

Include all Pen G bugs plus:
H. Influenzae
Listeria monocytogenes
E.Coli
Proteus mirabilis
Samonella Typh
H. Influenzae

Pseudomonas aeruginosa

Enterobacter species

E.Coli

Proteus mirabilis / Pen G effective most anaerobes except B. Fragilis. Pen V less effective against gm (-) than Pen G (Neisseria, Haemophilus and some anerobes)
Indicate: Strep, pneumococcal inf (inc. pneumonia, meningitis, otitis), anaerobic inf, gonococcal inf, syphilis
Gm (-) Enterobacteriaceae ,
RTIs by H.Influenzae, uncomplicated UTIs
Use w/ Clavulanic Acid or Sulbactam to prevent penicillinases
For klebsiella use ticarcillin and clavulanic acid to fight penicillinases
Cephalosporins (b-lactam)
G1 (more gm + action
Less gm – action)
G2
G3 (no gm + action
Lots of gm – action)
G3 Achieves theraputic
levels in CSF / Cefazolin
Cefotetan
Cefoxitin
Cefamandole *odd Side FX
Cefixime
Cefotaxime
Cefoperazone *odd Side FX /

Staph, Strep

Anaerobic strep
Proteus mirabilis, E.Coli, Klebsiella peneumoniae (PEcK)
Some Streps,
H. Influenza, Enterobacter aerogenes, N. gonorrhea, and PEcK, so HEN PEcK

HEN PEcK and

Pseudomonas aeruginosa

Serratia Marcesans / Cefotetan also for B. fragilis
Cefotaxime drug of choice for H. Influenzae meningitis (lipophillic)
Carbapenems (b-lactam) / Imipenem (w/cilistatin to prevent
kidney metabolism)
Meropenem /

Penicillinase producing Gm + and Gm – as well as P. aeruginosa

/ Broadest Spectrum of the B-lactams, penicillinase resistant!
Monobactams (b-lactam) / Aztreonam /

Enterobacter species

P. aeruginosa / Narrow Spectrum for bactermia, UTIs, RTIs, osteomyelitis, skin suture infections
Other non b-lactam cell
wall synthesis blockers / Vancomycin (IV)
Bacitracin / Bactericidal: staph, strep Bacteriostatic: enterococci (use w/ aminoglycosides for bactericidal FX) ,
C. difficile
/ Only Gm + bacteria, not effective orally-good for psuedomembranous colitis by
C. difficile, drug of choice for Methicillin resistant S. aureus
Used topically for wide variety of Gm + organisms

Inhibitors of Protein Synthesis

Subclass

/

Prototype

/

Spectrum

/

Indications

Tetracyclines BROAD
(bind 30S)
(all tetracyclines, except
doxycycline[biliary excretion]
toxic to kidney) / Minocycline (lipophillic)
Doxycycline (lipophillic)
Tetracycline
Demclocycline /

Mycoplasma pneumoniae

Rickettsia rickettsii

Corynebacterium acnes
H. Inluenzae
Zibrio cholerae
Chamydia
Borrelia burgdorferi
Treponema pallidum
Helicobacter pylori / Preferred for Rocky Mountain fever, typhus, mycoplasma RTIs, chlamydia, NOT for UTIs anymore!
Doxyclycline for traveller’s diarrhea
Aminoglycosides
(bind 30S) / Gentamicin
Tobramycin
Netilmicin
Streptomycin
Amikacin
Neomycin
Kanamycin /

Pseudomonas aeruginosa

Vibrio cholerae
Yersinia pestis
Francisella tularensis

Enterobacter aerogenes

E. Coli

Klebsiella pneumoniae

Proteus
Serratia marcescens / ONLY for serious, aerobic bac
NOT for initial gm + therapy
Mostly effective vs. Aerobic gm – bacteria,
most staph, strep inhibited.
Complicated UTIs
Also for endocarditis from ennerococci or viridans, use Gentamicin due to streptomycin resistance.
Erythromycin BROAD
(binds 50S) /

All Pen G bugs, and is drug of choice for:

Mycoplasma peumonia
Treponema pallidum
Chlamydia
H. influenzae
Legionella pneumophilia
Corynebac diptheriae / Used to treat patients allergic to Penicillin
Chloramphenicol BROAD
(binds 50S) /

GREAT for B. fragilis

Chlamydiae, rickettsiae, mycoplsma / NOT for UTIs, RTIs, brucellosis, since quite toxic
Clindamycin
(binds 50S) /

Most gm + cocci, and gm – anaerobes, NOT gm – aerobes

B. fragilis / Penicillin alternative to penicillinase producing bugs
Spectinomycin
(binds 30S) /

Neisseria gonorrhoeae

/ ONLY for acute gonorrgea by penicillinase producing Neisseria

Quinolones and Urinary Tract Antiseptics

Subclass

/

Prototype

/

Spectrum

/

Indications

Quinolones
Fluoroquinolones
(blocks topo II) / Nalidixic acid
Norfloxacin
Ciprofloxacin
Sparfloxacin
Ofloxacin
Enoxacin
Lomefloxacin
Levofloxacin
Perfloxacin / H. Ingluenzae
Legionella pneumonphilia
Pseudomonas aeruginosa
Neisseria gonorrhea
Enterobacter
E.Coli
Klebsiella pneumoniae
Proteus mirabilis
Serratia marcescens
shigella / Most gm – bac in UTIs, gm + bac are resistant!
Norfloxacin stronger than nalidixic acid, effective vs. gm + and gm – and is for uncomplicated UTIs, prostatitis
Cipro more potant than norfloxacin,
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
(used in combo) / Isoniazid (INH) – NARROW
Rifampin – BROAD
Ethambutol
Pyrzainamide /

M. tuberculosis, M. kansasii

M. tuberculosis, M. kansasii
Also for leprosy, meningitis by N. meningitidis, or H. influenzae, also most Gm + bac, enteric species and anaerobes!
M. tuberculosis, M. kansasii
M. tuberculosis, M. kansasii
Tuberculosis Drugs (2nd
line of defense) / Ethionamide
Cycloserine /
Leprosy Drugs
(used in combo) / Rifampin
Dapsone
Clofazimine /

Bacteriostatic for M. leprae

/ Dapsone also for P. carinii in AIDS pts.

Anti Fungal Drugs

Subclass

/

Prototype

/

Spectrum

/

Indications

For SubQ and systemic / Amphotericin B – BROAD
Flucytosine (only w/ Ampho B)
Ketoconazole
Fluconazole, newer /

Candida, histoplasma capsulatum, cryptococcus, coccidioides, aspergillus, blastomyces

Systemic mycoses
Systemic and cutaneous mycoses
Candida, cryptococci, blastomyces, histoplasma / Requires acid pH, and Never w/ ketoconazole!
Choice for cryptococcal meningoencepalitis, disseminated histoplasmosis, coccidioidomycosis
For superficial infections / Griseofulvin (oral!)
Nystatin (oral only)
Miconazole, clotrimazole,
Econazole (all topical)
Tolnaftate (TinacinR) / Candida

Candida and ringworm

/ Topical candidiasis
Topical dermatophytes, but NOT candida

AntiHelmintic Drugs

Subclass

/

Prototype

/

Spectrum

/

Indications

Anti Nematodes / Mebendazole
Thiabendazole
Pyrantel pamoate
Diethylcarbamzine
Ivermectin /

Whipworm trichuris trichiura

Pinworm Enterobiu vermicularis
Hookworm Necator americanus Ancylostoma duodenale
Strongloidiasis
Trichinella spiralis
Roundworm Ascaris lumbricoides
Pinworm Enterobiu vermicularis
Hookworm Necator americanus
Filariasis Wuchereria bancrofti
Brugia malyi
Filariasis Onchocerca volvus / NOT during pregnancy
Anti Trematode / Praziquantel (CSF)
Oxamniquine
Metrifonate /

All forms of schistosomiasis

/ Most pts show no SEs
Largely replaced by praziquantel
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:

Entamoeba histolytica

Giardia lamblia

Trichomonas vaginalis / Also for anaerobic Gm + and Gm - bacteria
Luminal amebicides / Diloxanide furoate
Tetracycline
Paromycin /

Intestinal amebiasis

Only for intestinal/luminal forms of amebiasis and tapeworm / For asymptomatic passers of cysts
Systemic amebicides / Emetine
Dehydroemetine
Chloroquine / Malaria, liver trophozoites / Emetine, dehydroemetine alternates b/c toxicities
Leishmaniasis / Sodium stibgluconate /
Trypanosomiasis / Melarsoprol
Pentamidine
Nifurtimox
Suramin /

Trypanosomal infections

Trypanosoma rhodensiense,
T. brucei gambiense
Protozoal inf, including Pneumocystis carinii, and choice for nematologic state of T. brucei gambiense
Only for T. cruzi
African trypanosomiasis prophylaxis, CHOICE for filarial parasites like Onchocerca volvulus / For meningoencephalitis (gets to CNS)
Co-tramoxazole is preferred for P. carinii, Pentamidine is 2nd choice
Toxoplasmosis / Pyrimethamine
Sulfadiazine + pyrimethamine /
Malaria
Tissue schizontcide
Blood schizonticide
Blood shizontcide and
sporonticide / Primaquine
Chloroquine
Quinine (usually w/pyrimethamine, and sulfonamide)
Melfloquine
pyrimethamine / Primary exoerythrocytic :
P. falciparum, P vivax
Secondary exoerythrocytic :
P. vivax and P. ovale
Erythrocytic falciparum malaria, also for asexual form of P. vivax and P. falciparum
Multidrug resistant P. falciparum
P. falciparum,
with sulfonamide also for P. malariae and Toxoplasma / For resistant malarial strains