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Antiparastic Agents/Antifunal Agents/RAAS/diuretics
Some antiparastic & antifungal drugss!
28
Bartending
Undergraduate 1
10/27/2011

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Term
chloroquine
Definition
-blood schitzonticide
-weak base gets trapped in vacuoles and prevents hematin crystallization
resistane due to mutated efflux transporter
-prophylaxis & treatment in pregnancy
-radical cure w/ primaquine
-LOTS of resistance
ADVERSE-can cause rash
Term
quinine/quinidine
Definition
-blood schitzonticide
-same MOA as chloroquine
-clinical cure of chloroquine resistant falciparum malaria w/ antibiotic
-NOT used for prophylaxis
-CYP3A4 interactions
ADVERSE cinchonism, prolongation of QT, thrombocytopenia/HUS, hypoglycemia
Term
artemether
Definition
-blood schitzonticide
-good for resistance types
-gametocidal activity-eradication
-heme iron cleaves bridge forming free radicals
-rapid absorption & short half life
-first line MDR falciparum
-replaces quinidine for sever malaria and chloroquine in pregnant
-ADVERSE--neurotoxic, embryotoxicity
Term
Atovaquone
Definition
-blood schitzonticide
-interferes w/ electron transport
-treat/prophylaxis of chloroquine-resistant
ADVERSE-rash
Term
Pyrimethamine
Definition
-blood schitzonticide
-MOA-inhibits DHFR
-use for chloroquine resistant falciparum
-intermittent preventative therapy in Africa
ADVERSE-high dose can cause folic acid deficiency
Term
Primaquine
Definition
-Liver schizonticide
-radical cure of vivax/ovale
-terminal/primary prophylaxis
-bad for G6PD deficient--greater chance of anemia
-don't use in pregnant
Term
metronidazole
Definition
-systemic antiprotozoal
-prodrug converted into DNA damaging metabolite via nitrite reduction
-use in trichomoniasis, giard, aembia
-use w/ luminal amebicide (e.g. paramyocin or iodoquinol)
Term
Paramyocin
Definition
-luminal amebicide
-binds 30S of E. hisolytica
-used w/ metronidazole
ADVERSE-GI distress
Term
Albendazole
Definition
-Antihelminthic
-inhibits B tubulin-No DNA replication or motility
-First pass to active form
-empty stomach = intestinal nematodes
-fat meal = tissue parasitess
-treat neurocysticerosis
-ADVERSE-liver toxicity, teratogenic
Term
Praziquantel
Definition
Antihelminthic
-MOA-inc. permability to Ca++
-DOA for schistosomiasis
-ADVERSE-well tolerated
Term
Pyrantel pamoate
Definition
MOA-neuromuscular blockage
-effective only in GI
-broad spectrum
Term
Ivermectin
Definition
-MOA-paralysis via activation of glutamate-gated Cl- channels
-broad spectrum
-treat onchocerciasis
ADVERSE-Mazzotti rxn & teratogenic
Term
flucytosine
Definition
Antifungal
-taken up by permease transporter & converted to fluorouracil by cytosine deaminase
-inhibits DNA synthesis by inhibiting thymidylate synthase
-Narrow spectrum-systemic candidiasis
-combo w/ amphotericin B
-PK-well absorbed-CNS penetraton
ADVERSE-hematologic/hepatotixicity
-can inhibit CYP3A4
FUNGISTATIC
Term
Griseofulvin
Definition
Antifungal mitosis inhibitor
MOA--disrupts mitotic spindle
FUNGISTATIC
-treats dermatophytic infections
-was first line, NOT ANYMORE!
ADVERSE-headaches, porphyria
Term
terbinafine
Definition
FUNGICIDAL
allylamine squalene epoxidase inhibitor antifungal
topical use for ringworm, onchomycosis
ADVERSE--skin rxns, hepatotoxic
Term
itraconazole
Definition
14a-sterol demethylase inhibitor
prevents lanosterol to ergosterol
-broad spectrum
-systemic & superficial mycoses
ADVERSE-mild rxns, cardiac suppression, drug interactions via CYPs
Term
amphotericin B
Definition
inhibits fungal membrane stability
-MOA-binds ergosterol
broad spectrum
ADVERSE
-cytokine storm, renal toxicity, myelosuppresion
Term
caspofungin
Definition
inhibits fungal cell wall synthesis
-MOA--non-comp. inhibitor of D-glucan synthesis
FUNGICIDAL
use for aspergillosis and systemic candidiasis
Term
acetazolamide/methazolamide
Definition
-carbonic anhydrase inhibitor
-SOA-proximal tubule
-inc. delivery of NaCl to macula dense--reduces RBF and GFR
-open angle glaucoma, epilepsy, altitude sickness
ADVERSE--hypokalemia, renal stones, hepatic encephalopathy, reduced exretion of organic bases
toxicity w/ sulfonamides
Term
furosemid/torsemide/bumetanide
Definition
Na,K,Cl symport inhibitors
SOA-thick ascending limb
-abolishes potential differences that drives paracellular transport of Ca++ and Mg++
-decreases uric acid excretion
-reduces kidney's ability to conc. urin and dilute urine
-inc. RBF & stimulates renin release
-delivered by OAT1
-short half live--causes post-diuretic Na+ retention
-For--hypercalcemia, hyponatremia, edema, CHF, edema of neprhotic syn.
-ADVERSE-hyperuricemia, hyperglycemia, hyponatremia & hypokalemia, ototoxicity
NSAIDS reduce efficacy
Term
chlorothiazide, chlorthalidone, metolazone
Definition
Na+/Cl- symport inhibitors
-SOA--distal convoluted tubule
-efficacy reduced w/ low GFR (unlike loops)
-dec. Ca++ excretion
-affects ability to dilute urine
-delivered by OAT1
-for-htn, edema, diabetes insipidus, calcium nephorlithiasis & osteoporosis
ADVERSE-hypokalemia, hyponatremia, hyperuricema, ED, interxns w/NSAIDS, quinidine
Term
triamterene/amiloride
Definition
k+ sparing diuretic
-SOA-late distal tubule
-EnaC inhibitors
abolish potential for K+ excretion
-Liddle syndrome & cystic fibrosis
-hyperkalemia
Term
spironolactone/eplerenone
Definition
K+ sparinge
Aldosterone antagonist
abolish potential for K+ excretion
-primary hyperaldosteronism, hepatic cirrhosis, CHF
ADVERSE-hyperkalemia
Spironolactone-gynecomastia, impotence, hirsutism, dec. libido
Term
mannitol
Definition
osmotic diuretic
SOA-loop of henle, renal tubules
MOA-inc. osmolality of tubular fluid
-inc. extracellular volume
inc. all electrolyte excretion
-inc. RBF
-used for disequilibrium syndrome, CSF, intraocular pressure
ADVERSE-no heart failure or cranial bleeding
Term
Demeclocyline/Tolvaptan
Definition
MOA--competitive V2 receptor antagonists
-inc. free water excretion w/ no effect on electrolyte or renal dynamics
-used for hyponatremia w/ SIADH,
ADVERSE
-demeclocyline-like tetracycline
-tolvaptan-GI, hyperglycemia, pyrexia
Term
catopril/enalapril
Definition
inhibit RAAS function
MOA-inhibits ACE
-vasodilation
-inc. renin release, ANGI levels, decreased aldosterone, prevents bad heart stuff
Uses-htn, CHF, myocardial infarction, diabetic nephropathy
ADVERSE--hypotension, cough, angioedema, hyperkalemia, renal failure, fetopathic potential, rash
Drug interxns--antacids, NSAIDS, K+ sparing diuretics
Term
losartan
Definition
angiotensin receptor blocker
-competitive inhibitor
-inhibits aldosterone secretion
-increases AngII, blocks AT1 receptor activation better than ACE inhibitors
Uses-htn, renoprotecion in diabetes, CHF
ADVERSE-teratogenic, hyperkalemia, hypotension
Term
aliskiren
Definition
direct renin inhibitor
overcomes problem of conversion of AngI to II that isn't blocked by ACE inhibitors
-decreases PRA but inc. renin
-no effect on bradykinin
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