| Term | Definition |
|---|
| In which RBCs does falciparum not grow? | S, F, and C |
| In which RBCs does vivax not grow | Duffy group |
| What is the DOC for al forms of malaria except chloroquine resistant malaria? | Chloroquine |
| What stage does chloroquine act on? | erythrocytic stage |
| Describe Chloroquine's absorption | well absorbed, concentrated in multiple parts of the body--excreted by kidney |
| What is chloroquine's mechanism of action? | Enters the parasite by energy dependent mechanism--accummulates in food vacuole--prevents polymerization of hemoglobin--breakdown of heme is toxic to parasite |
| How does chloroquine resistance occur? | pumped out via p-glycoprotein pump |
| In which organisms does chloroquine prophylaxis work best? | all forms of malaria except chloroquine resistant malaria |
| What are some uses of chloroquine? | Malaria, Chloroquine + emetine-->amebic liver abscess, Collagen vascular disorders (SLE, RA) |
| What are the common adverse effects of chloroquine? | NAMER--neuropathy, auditory problems, myocardial depression, exfoliative dermatitis, retinal damage + (bitter taste in mouth) |
| When is Chloroquine CI? | ****Porphorias, and Psoriasis---note: can be used in pregnancy |
| What is the MOA of primaquine? | cellular oxidant--forms a quinine-quinolone metabolite |
| Primaquine can exacerbate what? | G6PD defiency--> hemolysis! |
| What are some common side effects of primaquine? | ****Intravascular hemolysis in G6PD deficiency--GI effects, headache, MAP--metheglobinemia, Agranulocytosis, Pruritis |
| What is primaquine's effect on the acute phase of malaria? | Nothing, only affects the chronic phase |
| Sulfadoxine, dapsone, and atovaquone can be given for what? | PCP |
| What forms into cycloguanil to inhibit DHFR? | Proguanil (an antifolate)--pyramethamine also inhibits DHFR |
| Pyramethamine and sulfadoxine are used for what and what is their mechanism of action? | ****(Malaria and Toxoplasmosis)Synergistic blockade of Folate pathway--is used for prophylaxis in chloroquine sensitive areas |
| What are the adverse effects of pyramethamine and sulfadoxine? | ****Megaloblastic anemia d/t pyramethamine and crystalluria, hemolysis (in G6PD), SJS |
| What are proguanil and atovaquone given together for? | prophylaxis for Chloroquine resistant cases of falciparum |
| When is quinidine administered and how is it given? | given for serious infections of malaria and administered IV |
| Is quinine a DOC? | No, a second line drug but is used for severe and resistant infections |
| What is quinine's MOA? | it complexes/intercalates double stranded DNA and prevents seperation of the strands--prevents DNA replication and transcription of RNA |
| What is quinine often administered with? | Clindamycin, Pyramethamine, Doxycycline |
| What is quinine prophylactic against? | ****Nothing, it has too short a halflie |
| What are some uses of quinine? | Resistant or severe malaria, Nocturnal leg cramps, Myotonia congenita, sclerosing agent |
| What is cinchonism? | It is ass. with quinine--dizziness, headache, vertigo, tinnitus, blurred vision |
| What are some AE of quinine? | ****cinchonism, Cardiac conduction defects, black water fever (intravascular hemolysis), renal failure |
| What is the quinine triad? | Hypoglycemia, hypotension, cinchonism |
| What is mefloquine a derivative of? | quinine |
| What is mefloquine's MOA? | unknown |
| What is special about mefloquine's PK? | It has a long halflife (given 1ce a week) because it undergoes enterohepatic circulation |
| What is the first line drug for malaria prophylaxis? | Mefloquine |
| How often and when is mefloquine given? | Given once a week d/t long halfife, it is given 4 weeks prior to travel and week after |
| Does Mefloquine give prophylaxis ag. chloroquine resistant p. falciparum? | Yess, all types of malaria |
| What are common AE of mefloquine? | It causes cardiac conduction problems, psychiatric disorders (nightmares), seizures, and neurological symptoms |
| What is halofantrine used for? | It is used ag. all malaria inc. chloroquine resistant malaria |
| What is a common AE of halofantrine? | Cardiotoxicity d/t QT prolongation |
| Is halofantrine OK for pregnant women? | NO--it is embryotoxic |
| What is doxycycline used in malaria for | second line prophylaxis ag. chloroquine and mefloquine resistant P. falciparum |
| What are Artemethur and Artesunate used for? | Tx. of chloroquine resistant P. falciparum--NOT for prophylaxis d/t short halflife |
| Can artemethur and artesunate be used for prophylaxis? | No, short halfiflie |
| What is the MOA of artesunate and artemethur? | They are metabolized in the food vacuole of the parasite forming toxic reactive free radicals! |
| What is the MOA of atovaquone? | Inhibits ATP synthesis and ETC chain |
| What is the resistance like of atovaquone? | Nonexistant |
| What are some uses of atovaquone? | PCP, T. gondii (cyst and trophozoite), Malaria |
| What malarial drugs can be given to pregnant women? | ****Mefloquine if traveling to ch. r. area, or chloroquine or hydroxychloroquine if traveling to ch. s. area |
| What is an antifungal that blocks NA synthesis? | Flucytosine |
| What is an antifungal which disrupts microtubule formation? | Griseofulvin |
| What is an antifungal which disrupts the fungal cell wall synthesis? | Echinocandins |
| What are antifungals which alter the cell membrane permeability? | ****---BAAAN--Azoles, Polyenes (nystatin +Amphotheracin B), Allylamines and benzylamines |
| Which antifungals can be given systemically for subcutaneous and systemic mycosis? | ****Azoles, Amphotheracin B, Flucytosine, Echinocandins |
| What is the DOC for severe systemic mycoses? | Amphotheracin B |
| Is amphotheracin B broad spectrum? | Yes |
| What is the MOA of Amphotheracin B? | It binds to ergosterol-->pore formation-->increases cell membrane permeability-->electrolytes leak from cell-->cell death |
| Is Amphotheracin soluble? comment on its CNS penetration | No, it is insoluble--and thus must be given IV, it has poor CNS penetration |
| What is special about amphotheracin B's route of administration? | Given IV, but can be given intrathecally |
| What is the widest spectrum antifungal and the most important drug in systemic mycosis? | Amphotheracin B |
| What Is amphotheracin B a DOC for? | Aspergillus, Candida, Cryptococcus, Histoplasma, Mucor |
| What is the dose related toxicity of amphotheracin B? and how can it be avoided? | ****it is universal--fever, chills, muscle spasms, hypotension--it can be avoided by giving it slowly or previous administration of glucocorticoids, antihistamines, meperidine or antipyretics |
| What are the AE of Amphotheracin B? | ****Renal impairment-->anemia d/t dec. EPO, Intrathecal-->neurological sx, seizures |
| How can the amphotheracin B nephrotoxicity be avoided? | they are now packaged w/ lipid carriers--amphotec, abelcet, and ambisom--these have fewer nephrotoxic effects |
| What is flucytosine? | a synthetic pyrimidine antimetabolite? |
| Can flucytosine be given alone? | NO, it is given with amphotheracin B or itraconazole only (synergistic effects) |
| What is the MOA of flucytosine? | It is taken up by cytosine deaminase-->5-FU--5-FdUMP-->inhibits thymidilate synthetase-->blocks dTMP synthesis, and also 5-UTP formation-->inhibits protein synthesis |
| What are the clinical uses of flucytosine? | ****given only w/ amphotheracin B or flucytosine--used for MENINGITIS d/t Cryptococcus and candida! |
| What is an AE of flucytosine? | It can be metabolized by interstinal flora to 5-FU which can then cause bone marrow tox |
| Describe the toxicity of Azoles | They are rather non-toxic--minor GI upset but rather safe! |
| What are the two classifications of azoles and which drugs are involved in each group? | Imidazole: KMC--ketoconazole, mitraconazole, clomitrazole, and Trizoles (more sp. for P450)--Itraconazole, Posaconazole, voriconazole, fluconazole |
| What is the MOA of all azoles? | They all inhibit 14-a-sterol demethylase--which is a cytochrome P450 enzyme--inhibits Lanosterol to ergosterol-->disruption of membrane and increased permeability |
| How does ketoconazole affect the mammalian P450? what about at high doses? | inhibits it-->dec. tesosterone-->gynecomastia, dec. libido, loss of potency in men, and menstrual problems in women---------at high doses it inhibits cortisol and adrenal steroid synthesis |
| ****What does ketoconazole inhibit strongly? and what is the result of it? | CYP3A4--potentiates warfarin and cyclosporine |
| Is ketoconazole a weak acid? What does this mean in terms of absorption? | Yes, it is best absorbed at low pH and thus H2 inhibitors, PPIs, and antacids interfere with absorption |
| Is ketoconazole effective in meningeal mycoses? | No, it does not penetrate the CSF |
| How is ketoconazole administered? | It is NOT given systemically d.t its AE profile--given topically |
| What is special regarding fluconazole's PK | it is well absorbed in CSF and has a high oral availablility |
| What does fluconazole inhibit? | ****CYP3A4 moderately, and CYP2C9 strongly--increases plasma levels of phenytoin, zidovudine, and warfarin |
| What are the uses of fluconazole? | It is the DOC for esophageal, oropharyngeal, and vulvovaginal candida, coccoides, All kinds of cryptococcus |
| What is fluconazole ineffective ag? | ****Aspergillus or any filamentous fungi |
| What does itraconazole inhibit? and what is a major AE? | ****CYP3A4 strongly--it may cause fatal arrythmias when givne with cisapride or quinidine |
| Which drugs should not be given with itraconazole? | cisapride and quinidine |
| What inhibits the absorption of itraconazole? | antacids, H2 blockers, PPI's |
| Does itraconazole cross the BBB easily? | NO, it has poor CSF penetration |
| Which drug is used for dimorphic fungi such as blastomycoses, sporotrix, and histoplasma? | Itraconazole |
| What is itraconazole used for? | ****Dimorphic fungi, Aspergillus (voriconazole more for this though), used for dermatophytoses and onchomycoses |
| What is voriconazole used for? | MORE effective ag. aspergillus than itraconazole |
| What is voriconazole not used for? | Mucor! (neither is itraconazole or fluconazole) |
| What drug is mainly used to kill aspergillus? | voriconazole |
| What are some AE of voriconazole? | vision disturbances, inhibits CYP2C9, 2C19, 3A4 |
| which drug inhibits CYP2C9, CYP2C19, CYP3A4 | voriconazole |
| What is the azole used to kill mucor? | Posaconazole |
| What does Posaconazole inhibit? | CYP3A4 |
| Which azole has high hydrosolubility and high absorption? | voriconazole and fluconazole (this one has good CSF peentration also) |
| Which azole is eliminated via the renal system? | Fluconazole (all others eliminated via hepatic) |
| What is the structure of echinocandins? | large cyclic peptides linked to a long chain fatty acid |
| What are some names of echinocandins? | ____fungins (caspofungin, micafungin, anidulafungin) |
| What systemic antifungal is eff. ag. candida and aspergillus but NOT cryptococcus? | ****Echinocandins |
| What is the MOA of echinocandins? | Inhibits synthesis of B(1-3)-D-glucans in the fungal cell wall (analagous to penicillins)--> cell wall disrpution--> cell death |
| What are the systemic antifungals used for superficial mycoses? | GTKIF--griseogulvin, terbinafine, Ketoconazole, itra, flu |
| Which antifungal is only used for dermatophytosis? | Griseofulvin |
| Which antifungal drug accumuluates in keratin and is thus used only for skin, hair and nail infections? | Griseofulvin |
| What increases the absorption of griseofulvin? | fatty foods |
| What is the MOA of griseofulvin? | it disrupts the mitotic spindle--inhibits mitosis |
| What is an AE of griseofulvin? | INDUCES P450--increases metabolism of certain drugs such as warfarin |
| What kind of drug is terbinafine? | ****an allyllamine |
| How does terbinafine work? | it inhibits squalene epoxidase and prevents the synthesis of ergosterol--causes toxic accumulation of squalene |
| What are the AE of terbinafine? | gi upset, rash, headahce, TASTE disturbances |
| Which drug interactions is terbinafine ass. with? | NONe--no effect on P450 |
| What are the topical drugs for superficial mycoses? | Nystatin, KMC, terbinafine, naftifine, Ampho B |
| Which topical drugs are used for tinea cruris and tinea corporus? | ****naftifine, and terbinafine |
| Which topical antifungals are found OTC? | Clotrimazole, miconazole |
| What can ampho b. be used for topically? | cutaneous candida |
| What kind of drug is nystatin? | It is a polyene ab |
| What is the MOA of nystatin? | Similar to ampho B--also has same structure and resistance |
| What is special about nystatins administration route? | only given topically because it is too toxic if given systemically |
| What is special about PCP? | it lacks ergosterol and thus does nto respond to regular antifungals |
| What is the DOC for PCP? | Cotrimoxazole (tx. and prophylaxis) |
| What are some therapies for PCP? | ****DOC: cotrimoxazole, pentamidine, trimethoprim plus dapsone, primaquine plus clindamycin, atovaquone, prednisone or moderate-severe disease |
| What are two helminths that cannot evolve into adult worms in humans? | Strongyloides and Echinococcus |
| What describes an elongated roundworm that possess a complete digestive system, including a mouth and anus? | Nematode |
| What are leaf-shaped flatworms called? Do they have a digestive tract? | Trematodes, No |
| What is a worm that has a flat, segmented body that can attach to the host intestine? | Cestode |
| What are two ways antihelminths have their effect? | Locally or systemically |
| What are some systemic helmnithic reactions that respond weakly to antihelminthic drugs (4)? | cystercercosis, echinococcus, filiariasis, trichinosis |
| How do helminths express resistance? | THEY DONT! |
| What is a commonality with all antihelminthic drugs? | They are all CI in pregancy |
| What is the DOC for Echinococcus and cyctericosis? | Albendazole |
| What is the broad spectrum oral anti-helminthic given for pinworm, hookworm, ascariasis, trichuriasis, strongyloides and is the DOC for 2 others? | Albendazole |
| What are the benzidamoles? | Mebendazole, albendazole, thiabendazole |
| What is the mechanism of all the benzidamoles? (Mebendazole, albendazole, thiabendazole) | They all inhibit microtubule synthesis |
| Which antihelminthic drug causes fever, alopecia, elevated liver enzymes, and pancytopenia w/ long term use? | ****Albendazole |
| Treatment of what with which drug causes the following symptoms?--headache, vomiting, hyperthermia, convulsions? How can this condition be prevented? | Neurocysterocsis with albendazole, give corticoids prior to albendazole |
| Which antihelminthic drug should not be given during pregancy and to children < 2yoa? | albendazole |
| Which drug can be used to treat numerous nematodes--whipworm, hookworm, pinworm, roundworm? | Mebendazole |
| What is the major adverse effect of Mebendazole? | There is none--it is relatively free of AE other than abd. pain, and diarrhea |
| Who is Mebendazole CI in? | CIRRHOSIS pts, and children <2yoa |
| Which benzidamole is least popular? | Thiabendazole |
| Which drug was used to treat strongyloides, cutenous larva migrans and trichonosis? | Thiabendazole (CLM and strongyloides is now usually tx w. ivermectin) |
| Which antihelminthic drug causes dizziness, nausea, vomiting, anorexia--CNS disturbances, SJS, erythma multiforme--DEATH | ****Thiabendazole |
| Which antihelminthic drug is CI in pregnancy, liver and kidney disease? | Thiabendazole |
| What is the DOC for onchocercosis and strongyloides? | Ivermectin |
| What are some the main uses of Ivermectin (2DOC) and others? | Strongyloides, onchocercosis (river blindness), scabies, lice, CLM, ascariassi |
| Which drug is a gaba agonist which causes hyperpolarization and then paralysis of the worm? | Ivermectin |
| What is special regarding the PK of ivermectin? | given orally and does not cross BBB |
| In which pts. is Ivermectin CI? | In pts. with meningitis because may cross BBB--CNS effects, pregnancy, also those on benzodiazepines and barbituates (gaba agonists) |
| Which drug causes a fever, headache, dizziness, somnolescence, and hypotension after it kills its parasite? What is the reactino called? How can it be avoided? | Ivermectin--after killing microfilaria--Mazotti reaction, give corticoids |
| What is the indication for piperazine? | it is an alternate drug for ascariasis |
| What is piperazine's MOA? | GABA agonist |
| In which pts. is piperazine CI? | pregnancy and seizures |
| What is pyrantil pamoate's MOA? | it is a depolarizing NM agent which causes release of ACh and inhibition of cholinesterase--paralyzes worm--is expelled |
| For which worms is pyrantil pamoate effective? | eff. in roundworms and pin worms, mod. effective in hookworms |
| Is the antihelminthic pyrantil pamoate a systemic or local drug? | It is a local drug which kills the worms in the colon but not the eggs |
| What is the DOC for lyphatic filariasis and Loa Loa and tropical eosinophilia? | Diethylcarbazine |
| What is teh MOA of diethycarbazine? | unknown--but may involve arachodonic acid pathway |
| What is doxycycline used for as an anti-helminthic drugs? | It is used to kill wolbachia within wolcheria bancrofti--indirectly kills the bug (it can also be used in onchoceriasis) |
| What is the DOC for killing all schisostosomes? | Praziquantal |
| What is the DOC for most all trematode and cestode infections? | Praziquantal |
| Cystercosis can be killed by which two drugs? | Albendazole* and Praziquantal |
| What is the MOA of praziquantal? | it increases permeability of the cell membrane to calcium, resulting in paralysyis of the parasite, dislodement and death |
| Can praziquantal cross the BBB? | ****Yes--distrubutes there also |
| Which drug should not be be used for ocular cystercosis? Why? What is the preffered drug? | Praziquantal because it can cause destruction of the organism in the eye--damage!, Albendazole |
| What is the DOC for fasciola hepatica? | Bithionol |
| What can bithional be used to kill? | Fasciola--sheep liver fluke (DOC), Pulmonary paragonimus |
| What is the MOA of bithionol? | inhibits the helminth's ETC |
| What is the second line drug for most all cestode infections? | Niclosamide |
| What is the MOA of niclosamide? | ****Inhibits the parasites mitochondrial phosphorylation of ADP (look at the name!) |
| What is niclosamide effective at killing (at an anatomical level) | ****it will kill the cestode and its scolex but not the ova--requires a laxative to kill those |
| Which antihelminthic drug has a disulfuram like effect and thus alchohol should be avoided with its use? | Niclosamide |
| What are two major complications of amebiasis? | ****fulminating meningitis and granulomatous encephalitis |
| What is the dx if a person has minor sx and passes cysts? | Asx amebiasis |
| What are symptoms of mild-moderate amebic colitis? | Mild-moderate: ass. with recurrent diarrhea and abdominal cramps with mucous in stool but NO BLOOD--also tenderness is found along the colon on examination |
| What are sx of severe amebic colitis? | stools semi-formed, streaked with blood and mucous--hemorrhage and peritonitis |
| what are some sx of hepatic amebiasis | cought, pain in rt shoulder, aspirates from liver abscess, hepatic enlargment and pain |
| What is the mechanism of action of Metronidazole and Tinidazole | They both undergo reductive bioactivatino--pyruvate oxidoreductase (present in anerobes)-->form a cytotoxic byproduct-->toxic to DNA and protein |
| How is metronidazole eliminated? | Hepatically |
| What are the uses of Metronidazole? | GET GAP on the METRO, ulcerative colitis and leishmania |
| Which amebic drug is found to be a teratogen and carcinogen in animals but not humans? | ****metronidazole |
| What are the adverse effects of metronidazole? | ****dose dep. seizures, ataxia, urinary discoloration, GI irritation--DRYNESS OF MOUTH, INSOMNIA, STOMATITIS, Urethral burning, Metallic taste in mouth, disulfuram like effect |
| Which amebic drug has a disulfuram like effect with alcohol? | metronidazole |
| Which amebic drug potentiates coumarin anticoagulants? | Metronidazole |
| What are two amebic drugs that inhibit protein synthesis by blocking ribosomal movement? | ****emetine and dehydroemetine |
| What is special about the administration of emetine and dehdyrdoemetine? | they are only gfiven to inpatients |
| Which amebic drug can become concentrated in various organs and have a cumulative effect and cause AE? | Emetine |
| Does emetine have a narrow or wide range between therapeutic and toxic effect? | narrow |
| What is Emetine used for? | ****severe form of intestinal or extraintestinal amebiasis |
| What drug is a general protoplasmic poison? | emetine |
| Which drug affects the heart by causing cloudy swelling and necrosis? what can this lead to? | ****Emetin, it can lead to CHF, arrythmias, hypotension, retrosternal pain and abscess at the site of injection |
| What are some common AE of Emetine? | ****protoplasmic poison--nausea vomiting, diarrhea, muscular weakness, pain at the site of injection--fatigue, pruritic eruptions, urticaria |
| What is the MOA of diloxanide furoate? | Not known |
| How does diloxanide furoate work? | it is given orally, hydrolyzed in gut to diloxanide-->amebicidal effect, the furoate is then absorbed from the GI and excreted in urine |
| What are the uses of diloxanide furoate? | ****it is used for asx carriers or for moderate-severe intestnial amebiasis if given with other drugs |
| What are the AE of diloxanide furoate? | ****they are confined to the GI--nausea, vomiting, cramps, dryness of mouth, etc. Furoate--can cause pruritis, urticaria, and proteinuria |
| What is the MOA of iodoquinol | not known |
| What are the AE of iodoquinol? | ****they are rather mild unless at high doses-->systemic absorption-->PONT (periphral neuropathy, ototoxicity, nephrotoxicity, thyroid enlargement) |
| What are some CI of iodoquinol? | ****Thyroid and renal disease |
| Which is an indirect ameoba killer? how? | Tetracycline, it kills the flora it feeds on |
| Who is tetracycline CI in? | Children < 8yoa, and pregnancy |
| What is special about the PK of tetracycyline? | it chelates ca, mg, al-->nonabsorbable compounds |
| Is tetracycline given alone for killing amebas? | No, it is used as an adjunct |
| Which are the amebicidal drugs which are used as tissue amebecidal agents? | Chloroquine, emetine, and metronidazole |
| Which are the drugs which are used as luminal amebicidal agents? | Diloxanide fuoate, iodoquinol, paromomycin, tetracycline |
| What is the purpose of giving paromomycin in aids pts? | can kill cryptococcus |
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