Diuretics: Site of action & Mechanism

 Osmotic Diuretics: =/=> water reabsorption throughout the tubules, but mostly in the
proximal tubule (mannitol)
 Carbonic Anhydrase Inhibitors: proximal tubule, =/=> C.A (acetazolamide,
dorzolamide)
 Loop Diuretics: thick ascending loop of Henle, =/=> Na+/K+/2Cl- transporter
(furosemide, ethacrynic acid)
 Thiazides: early distal tubule, =/=> Na+/Cl- symporter (hydrochlorothiazide,
indapamide)
 K+ sparing agents: distal nephron (late distal tubule + colecting ducts). Aldosterone
receptor antagonist (spironolactone) or =/=> Na+/K+ exchange by =/=> of Na+ channels
(amiloride, triamterene)

This drugs Inhibit...

 Leflunomide: Dihydroorotate Dehydrogenase (DH) [Carbamoyl phosphate --> Orotic
Acid]
 Mycophelonate: Inositol Monophosphate (IMP) DH
 Ribavirin: IMP DH [IMP --> GMP]
 Hydroxyurea: Ribonucleotide Reductase [UDP --> dUDP]
 6-MP (& Azathioprine): PRPP Amidotrasnferase (de novo purine synthesis) [PRPP -->
5-phopsphoribosylamine --> IMP]
 Allopurinol: non-competitive inhibitor of Xanthine Oxidase [Xanthine --> Uric Acid].
Allosteric Inhibitor of PRPP Amidotrasnferase
 5-FU: Thymidylate synthase [dUMP --> dTMP]
 Pyrimethamine: Dihydrofolate (DHF) Reductase
 Trimethoprim: DHF Reductase
 Methotrexate: DHF Reductase [DHF --> THF = no dUMP --> dTMP]
 Rifampin: DNA dependant RNA polymerase [inhibits sigma (promoter) and rho
(terminator)] in RNA transcription
 Actinomycin: RNA polymerase 2, RNA polymerase α2ββ
 α-amanitin (amanita phalloid mushroom): RNA polymerase 2
 Quinolones: DNA topoisomerase II (DNA gyrase
 Fomepizole: alcohol dehydrogenase
 Disulfiram: acetaldehyde dehydrogenase
 Beta-lactams: peptidoglycan cross-linking in cell wall
 Glycopeptides: peptidoglycan formation by binding D-ala-D-ala portion on cell wall
 Aminoglycosides: initiation complex in protein synthesis & translocation
 Linezolid: initiation complex in protein synthesis
 Streptogramins: aminoacyl-tRNA (aa incorporation) in protein synthesis
 Tetracylins: aminoacyl-tRNA (aa incorporation) in protein synthesis
 Cloramphenicol: peptide bond formation in protein synthesis
 Macrolides: translocation in protein synthesis
 Lincosamides: translocation in protein synthesis
 Fluoroquinolones: DNA topoisomerase II (DNA gyrase) & DNA topoisomerase IV
 Sulfonamides: dihydropteroate synthase
 Trimethoprim: dihydrofolate reductase
 Rifampin, Rifabutin (rifamycins): DNA-dependant RNA-polymerase
 Ethambutol: arabinosyltransferase, inhibits synthesis of arabingalactan, no cell wall.
 INH: synthesis of mycolic acids, need bacterial catalase-peroxidase, encoded by KatG
gene. Resistant if deletion of KatG gene
 Azoles: 14alpha-demethylase, thus inhibits ergosterol synthesis from lanosterol
 Flucytosin: DNA/RNA synhesis, active metabolite inhibits thymidilate synthase (5-FC
--> cytosine deaminase --> 5-FU --> 5- Fd-UMP)
 Echinocandins (-fungin): beta glucan, thus inhibit cell wall synthesis
 Terbinafine: squalene epoxidase, thus inhibit the formation of squalene epoxide from
squalene
 Griseofulvin: mitosis, interferes microubule fx.
 Chloroquine: detoxification of heme into hemozoin; heme accumulates, heme toxic for
plasmodia.

Parasitology - Treatment
 Metronidazole: Giardia lamblia, Trichomona vaginalis, Entamoeba hystolytica
 Nitazoxanide: Cryptosporidium
 Pyrimethamine + Sulfadiazine: Toxoplasma gondii
 Suramin: Trypanosma bruceii (blood borne)
 Melarsoprol: Trypanosoma bruceii (CNS)
 Nifurtimox or Benznidazole: Trypanosoma cruzi
 Amphotericin B: Naegleria fowleri, Leishmania donovani
 Sodium stibogluconate (Pentavalent Antimony): Leishmania donovani
 Cloroquine: Plasmodium falciparum, Plasmodium malariae
 Cloroquine + Primaquine: Plasmodium ovale, Plasmodium vivax
 Quinidine (IV): severe Plasmodium infx
 Mefloquine or Atovaquone/Proguanil: Plasmodium resistant
 Atovaquone + Azythromycin: Babesia
 Diethylcarbamazine (DEC): Loa loa, Wucheria bancrofti
 Ivermectin: Onchocerca volvulus, Strongyloides stercolaris
 Bendazoles or Pyrantel Pa M oate: Enterobius vermicularis, Ascaris lumbricoides,
Ancylostoma duodenale, Necator americanus (ne M atodes)
 M ebendazole: Toxocara canis
 Albendazole: Strongyloides stercolaris, Toxocara canis, neurocysticercosis,
Echinococcus granulosus.
 P raziquantel: Taenia solium, Schistosoma, Diphylobotrium latum, Clonorchis (P
latyhelminthes)

Drugs Contraindicated in BREAST Feeding

usmleaid:

B: Bromocryptin, Benzodiazepines.
R: Radioactive Isotopes, Rizatripan
E: Ergotamine, Ethosuximide
A: Amiodarone, Amphetamines
S: Stimulant Laxatives, Sex Hormones
T: Tetracyclins, Tretinoin