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Pharmacology Exam 3: Antimicrobials IV
antimicrobial IV pharm exam 3
126
Anatomy
Graduate
03/06/2011

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Term
Malaria is a ___ called ___ ___ that leads to nearly 3 million deaths per year. It has been eradicated from the U.S. but immigration and travel constitutes a health problem.
Definition
- parasite
- Plasmodium falciparum
Term
Attempts to eradicate malaria have failed b/c ___ developed .
Definition
resistance
Term
___-resistant and multi-drug resistant strains of __ _____ have spread and development of drug resistance has increased with malaria. The economic and political conditions in the third world countries contribute to the spread of this disease.
Definition
- Chloroquine-resistant
- P. falciparum (malaria)
Term
Malaria is a __ infection transmitted by the __ ___ ___.
Definition
- protozoan infection
- female Anopheles mosquito\
Term
There are 4 types of malaria, all transmitted by the female Anopheles mosquito, name them: Which type is life threatening?
Definition
1. Plasmodium falciparum
2. Plasmodium malariae
3. Plasmodium vivax
4. Plasmodium ovale

Plasmodium falciparum is the only deadly one
Term
3 methods of protection against malaria:
Definition
- using anti-mosquito measures
- taking drugs to prevent malaria
- avoiding the Anopheles mosquito bites
Term
All 4 types of malaria are diagnosed via __ ___.
Definition
blood smear
Term
___ is used for treatment of malaria. This drug is also used prophylactically.
Definition
Chloroquine
Term
the prophylactic drug to prevent malaria?
Definition
Chloroquine- also used as treatment
Term
___ is the drug used to treat P.vivax and P.ovale strains of malaria.
Definition
Primaquine
Term
Primaquine is used to treat what?
Definition
- P. ovale and P. vivax (strains of malaria)

Think "ovale and vivienne" are prim
Term
what is a good drug combination for treatment of malaria?
Definition
Sulfadoxine + Pyrimethamine
Term
What drug do you use for resistant strands of malaria?
Definition
Mefloquine

Mefloquine will "muffle" even the toughest "malaria"
Term
What is Mefloquine used for?
Definition
- resistant strands of malaria
Term
Chloroquine is highly effective against ____ forms of P.vivax, P.ovale, P.malaria, and P. falciparum. It has NO activity against ___ ___ forms.
Definition
- erythrocytic forms

- NO activity against latent tissue forms
Term
Chloroquine mechanism of action:
Definition
1. Chloroquine is concentrated in acidic food vacuoles
of the parasite, raising the pH. Parasite hydrolysis of
hemoglobin may be inhibited by chloroquine and analogs
leading to accumulation of toxic heme by-products
resulting in lysis of the cell membranes.
2. This drug also binds to DNA
3. Causes fragmentation of parasite RNA.
Term
Chloroquine is concentrated in ___ ___ ___ of the parasite, ___ the pH. Parasitic hydrolysis of hemoglobin may be ___ by chloroquine and analogs leading to accumulation of __ ___ by-products resulting in lysis of cell membranes. This drug also binds to ___ and causes fragmentation of ___ ___.
Definition
- acidic food vacuoles
- raising
- inhibited
- toxic heme products
- drug also binds to DNA
- causes fragmentation of parasitic RNA
Term
What drug has a similar mechanism to Chloroquine, but is the drug of choice for Chloroquine-resistant malaria?
Definition
- Mefloquine
Term
Sulfadoxine and Pyrimethamine ___ separate steps of the ___ __ resulting in ___ ___ of ___ ___ and production of __ ___. Wide spread resistance to this drug developed after it was overused.
Definition
- inhibit
- folate pathway
- synnergistic inhibition of DNA synthesis and production of folate precursors
Term
Toxicity and side effects seen with Sulfadoxine and Pyrimethamine (malaria tmt)?
Definition
- skin rash
- high doses>megaloblastic anemia
- 1:5000 patients develop severe or fatal cutaneous reactions
Term
Trypanosomiasis aka __ __ ____ ___ aka __ ___ __ ___.
Definition
- A.T. brucei gambiense
- West African sleeping sickness
Term
West African sleeping sickness is caused by what organism and is also called what?
Definition
- A.T. brucei gambiense

- Trypanosomiasis
Term
If CNS is NOT involved with Trypanosomiasis, then ___ and ___ are used for treatment.
Definition
- suramin
- pentamidine
Term
If CNS is involved with Trypanosomiasis, then _____ is used for treatment.
Definition
Melarsoprol
Term
Suramin, usually used in combination with ___ , for treatment of ____. Suramin works by ___ the parasite ___ ___.
Definition
- pentamidine
- trypanosomiasis
- inhibiting the parasite energy production
Term
Side effects of suramin:
Definition
- very toxic, especially in malnourished patients
- immediate reactions: nausea, vomiting, shock, loss of consciousness
- delayed reactions: optic atrophy, adrenal insufficiency, skin rash, hemolytic anemia
Term
what drug used for treatment of Trypanosomiasis can be very toxic, especially in malnourished patients?
Definition
- suramin
Term
3 uses of Pentamidine isoethionate:
Definition
- combined with suramin for treatment of A.T. brucei gambiense (Trypanosomiasis)
- 2nd choice drug for Leishmania donovani infections
- prophylactic treatment of Pneumocytosis carnii pneumonia (PCP)
Term
what is 2nd choice drug for Leishmania donovani?
Definition
- Pentamidine isoethionate
Term
what drug is used for prophylactic treatment of Pneumocytosis carnii pneumonia?
Definition
- Pentamidine isoethionate
Term
Pentamidine isoethionate mechanism of action?
Definition
- inhibits adenosine uptake
- binds DNA
- inhibits topoisomerase
Term
Toxicity and side effects of Pentamidine isoethionate?
Definition
- at therapeutic doses, toxicity is observed in 50% of patients
Term
American Trypanosomiasis is aka __ ___ and is caused by __ ____ infections. It is transmitted by the __ ___ ___ aka kissing bug/assassin bug. There is also ___ transmission or transmission via __ ___.
Definition
- Charga's Disease
- T. cruzi infections
- bloodsucking triatomid bug
- placenta
- blood transfusion
Term
Chargas disease aka ___ ____ caused by __ ___ infections from the ___ ____ bug.
Definition
- American Trypanosomiasis
- T. cruzi infections
- bloodsucking triatomid bug
Term
Symptoms of Charga's Disease/American Trypanosomiasis?
Definition
- acute fever in children
- chronic GI and heart problems in adults
Term
Treatment of Charga's Disease/American Tryponamosomiasis?
Definition
- Nifurtimox and Benznidazole: reduce severity of acute disease, but not effective on chronic infections
Term
Nifurtimox and Benznidazole are used for treatment of what?
Definition
American Trypanosomiasis aka Charga's Disease
Term
Nifurtimox (tmt of American Trypanosomiasis) has a similar mechanism of action to ____. These drugs get converted to ___ ___ which damage __, ___, and ___.
Definition
- Metronidazole
- free radicals
- membrane, enzymes, and DNA
Term
Side effects of Nifurtimox?
Definition
- hypersensitivity reactions
- nausea, vomiting, GI problems
- weight loss
- peripheral neuropathy
- CNS excitability
- supression of cell-mediated immune response
Term
Amebiasis. Entamoeba histolytica is transmitted by the ___ ___ route. Prevalence in U.S. is 2-4%, 480 million worldwide.
Definition
- fecal oral route
Term
Entamoeba histolytica, ___ are the only known host. Infection is common in poor hygenic condtions in what three groups of people?
Definition
- humans
1. low socioeconomic status
2. institutionalized individuals
3. male homosexuals
Term
With Entamoeba histolytica ___ forms of the parasite live as ____ in the ___ __ where they produce ____, but there is little harm to the host. Sometimes, the parasite will invade the ___ ___ producing mild to severe colitis called ___ ___. Some individuals develop ___ __ and ___ ___.
Definition
- trophozite forms
- commensals
- large intestine
- cysts
- intestinal mucosa
- amebic dysentery
- systemic disease
- liver abscess
Term
Drugs used to treat amebiasis are categorized as ___, ___, or ___ ___.
Definition
- luminal
- systemic
- mixed amebicides
Term
Luminal amebacides, like ___ ___, are only active against the ___ form of the amoeba.
Definition
- diloxanide furofate
- intestinal
Term
Systemic amebicides are effective only against ___ forms of amebiasis are only occasionaly used to treat ___ ___ __ or __ ___.
Definition
- invasive
- severe amebic dysentery
- hepatic abscesses
Term
Severe amebic dysentery is treated with ___ ___ called ___.
Definition
- systemic amebicide
- dehydroemetine
Term
Hepatic abscesses from severe amebiasis is treated with the ___ ___ , either ___ or ___.
Definition
- systemic amebicides
- dehydroemetine
- chloroquine
Term
___ __ are effective against parasites both in the GI lumen and in systemic tissues. ___ is the prototype here.
Definition
- Mixed amebicides
- Metronidiazole
Term
prototype mixed amebicide :
Definition
Metronidazole: converted to free radical and damages membranes, enzymes, and DNA
Term
Current first choice therapy for amebiasis is either _____ alone or ____ with ____ ____.
Definition
- metronidazole alone
- metronidazole with diloxanide furoate
Term
3 big uses of Metronidazole:
Definition
- tmt of amebiasis
- tmt of anaerobic bacterial infections
- tmt of UTIs
- may help with extraction of adult guinea worms in dracunculiasis
Term
Metronidazole has a very ___ spectrum of ____ and ___ activity.
Definition
- broad
- antiprotozoal
- antimicrobial
Term
Metronidazole is clinically effective against:
Definition
- trichomoniasis
- amebiasis
- giardiasis
Term
Metrodinazole is given via ___ for anaerobic cocci and anaerobic gram negative bacilli, and obligate anaerobic bacterial infections.
Definition
i.v.
Term
Because metronidazole is well absorbed, therapeutic concentrations may not reach the ___ ___, thus it is often combined with ___ ___ like ___ ___.
Definition
- large intestine
- luminal amebicide like diloxanide furoate
Term
drug that may help with extraction of guinea worms in dracunculiasis:
Definition
Metronidazole
Term
Metronidazole displays ___ ___ for ___ or ____ microorgansims and for ___ or ___ cells.
Definition
- selective toxicity
- anaerobic or microaerophillic
- anoxic or hyoxic cells
Term
Metronidazole accepts electrons from ___ and forms reactive ___ ___ that damage parasite DNA, proteins, and membranes.
Definition
- flavoproteins
- free radicals
Term
Toxicity and side effects of Metronidazole:
Definition
- headache
- nausea
- dry mouth and metallic taste
- disulfiram like reactions b/c interferes with alcohol metabolism
- high doses cause CNS and peripheral side effects
- use with caution if pt has CNS disease
- considered safe for pregnancy at therapeutic doses, but it is mutagenic and carcinogenic in rats at high doses
Term
if going to give patient Metronidazole, what should you warn patient of?
Definition
- it inhibits metabolism of alcohol, so alcohol will make them sick
Term
do not give metronidzole to patient with __ disease.
Definition
CNS
Term
Metrodinazole is __ and __ in rats, but is approved for pregnancy at therapeutic dosses.
Definition
- mutagenic and carcinogenic
Term
Diloxanide furoate is a ___ ___ that is ___ ___ well in the GI tract. It should be given ___. Its mechanism is unknown.
Definition
- luminal amebicide
- NOT absorbed
- orally
Term
toxicity and side effects of diloxanide furoate:
Definition
- well tolerated
- not recommended for pregnant women
Term
Paromycin is aonther ___ ___ that is given orally and NOT absorbed from the GI tract. It is an ___ that binds the ___ ribosome and inhibits ___ ___. It is generally well tolerated, but make cause __ and ___.
Definition
- luminal amebicide
- aminoglycoside
- 30s ribosome
- inhibits protein synthesis
- nausea and diarrhea
Term
What is Paromomycin?
Definition
- luminal amebicide
- aminoclycoside
- binds 30s ribosome and inhibits protein synthesis
- given orally
- not absorbed in GI tract
Term
Giadiasis aka ___ __ is a ___ ___ commonly reported intestinal infection in developing countries and the U.S.
Definition
- Giardia lamblia
- flagellated protozoan
Term
Most Giardia lamblia infections are ___, but may cause isolated cases or epidemcis of ____.
Definition
- asymptomatic
- diarrhea
Term
Giardiasis results from ___ contamination of food or water among travelers. Hikers and backpackers become infected by drinking contamined stream/lake water.
Definition
- fecal
Term
Amebiasis common among poor, institutionalized, and male homosexuals.

Giardiasis common among travelers, children in day care, instituinalized individuals, and male homosexuals.
Definition
Term
Human-to-human transmissin of giardiasis is common among ___ , ___ individuals, and __ ___.
Definition
- children in day care centers
- institutionalized individuals
- male homosexuals
Term
With Giardiasis ingested ___ transform into ___ ___ in the ___ GI tract.
Definition
- cysts
- motile trophozoites
- upper
Term
treatment of Giardiasis:
Definition
- chemotherapy with Metronidazole or Quinacrine
Term
Drug of choice for Giardiasis:
Definition
Metrodinazole
Term
what is Quinacrine?
Definition
- drug used to treat Giardiasis
Term
Quinacrine was initially used to treat ___, but also works against ___. It works by ___ into __ and ___ ___.
Definition
- malaria
- Giardiasis
- intercalating into DNA
- inhibiting flavoenzymes
Term
Side effects of Quinacrine:
Definition
- headache
- dizziness
- vomiting
- yellowing of skin
- black/blue nails
- toxic psychosis at high doses
- exacerbation of psoriasis
Term
Trichomoniasis is caused by the ___ ___ called ___ ___ that inhabtis the genitourinary tract and causes vaginitis and urethritis. Transmission occurs primarily by sexual contact. Over 3 million women are infected annualy in the USA.
Definition
- flagellated protozoan
- Trichomonas vaginalis
Term
Trichomoniasis is treated successfully with a __ dose of ____.
Definition
- single dose
- Metronidazole
Term
Reinfections of trichomoniasis commonly occur. Sexual partners must also be treated. In other countries, a related drug called ____ is often used.
Definition
Tinidazole
Term
Toxoplasmosis 4 routes of infection:
Definition
- ingestion of undercooked meat contaminated with tissue cysts
- ingestion of vegetable matter contaminated with soil containing infective oocysts
- direct oral contact with feces of cats shedding oocysts
- congenital infection from acutely infected mother
Term
Drug of choice for Toxoplasmosis:
Definition
Pyrimethadine + Sulfadoxine
- inhibit separate steps of folate pathway which inhibits DNA synthesis and production of folate precurors
- also used in treatment of malaria, but resistance developed
Term
Toxoplasmosis is treated with Pyrimethamine and Sulfadoxine, these two combined into one is called:
Definition
Fansidar
Term
Helminthic (worm) infections occur worldwide, but prevalence is greater in ____ regions.
Definition
tropical
Term
Helminthic worm pathogens for humans are classified into 2 groups:
Definition
1. Roundworms (nematodes)
2. Flatworms

REMEMBER RING WORM IS A FUNGAL INFECTION NOT A WORM
Term
what are the two types of flat worm?
Definition
- flukes/trematodes
- tape worms/cestodes
Term
Worm parasites vary with respect to life cycle,body structure, development, physiology, localization within the host, and susceptibility to chemotherapy.
Definition
Term
In the USA, helminthic infections are more common in ___, ___ __ regions like the __ states and ___ __, but they can occur in all regions of the country.
Definition
- humid, sub-tropical regions
- Southern states
- Gulf Coast
Term
People at risk for helminthic infections:
Definition
- pet owners
- children who play in or eat contaminated soil
- plumbers, construction workers, and miners who are exposed to moist untreated soil
- sunbathers who lie on wet contaminated sand
- eating undercooked meat (pork)containing parasite cysts
Term
Helmins, helminthos refers to worms.
Therefore, anthelminthic
or anthelmintic refers to drugs against worms.
Definition
Term
Antihelmintic drugs cause ___ or ___ of the worm leading to ___ of worms from the GI tract. These drugs also damage the ___ leading to partial ___ or ___ by immune reactions. They also interfere with ___.
Definition
- narcosis or paralysis of the worm leading to expulsion
- damage the cuticle leading to partial digestion or rejection by immune responses
- interfere with metabolism
Term
Nematodes (Roundworms):

(this list was not in red on powerpoint, but just in case, here it is)
Definition
Ascaris lumbricoides (Roundworm)
Necator americanus, Ancylostoma duodenale (Hookworm)
Trichuris trichiura (Whipworm)
Strongyloides stercoralis (Threadworm)
Enterobius vermicularis (Pinworm)
Trichinella spiralis
Filariae (Wuchereria bancrofti, Brugia malayi, Loa loa,
Onchocerca volvulus)
Dracunculus medinensis (Guinea or Dragon worm)
Term
Cestodes (Flatworms)

(also not in red on powerpoint)
Definition
Taenia saginata (beef tapeworm)
Taenia solium (pork tapeworm)
Diphyllobothrium latum
(fish tapeworm)
Hymenolepsis nana (dwarf tapeworm)
Term
Trematodes (Flukes)
(also not in red)
Definition
Blood flukes
Schistosoma haematobium, S. mansoni, S. japonicum
Lung flukes
Paragonimus westermani, P. kellicotti
Liver flukes
Clonorchis sinensis
Opisthorchis viverrini. O. felineus
Fasciola hepatica
Intestinal flukes
Fasciolopsis buski
Heterophyes heterophyes
Metagonimus yokogawai
Term
Treatment of roundworms/nematodes:
Definition
- Benzimidazoles (Mebendazole/Vermox and Albendazole/Zental)
- Pyrantal Pamoate
- Piperazine
- Ivermectin
Term
What are the two Benzimidazoles used to treat nematodes/round worm?
Definition
- Mebendazole (Vermox)
- Albenazole (Zental)
Term
Benzimadazoles is a __ spectrum antihelminthic against intestinal parasites. It is __ and ___ absorbed with lots of __ __ ___. It is also effective ___ against some ___ __ forms.
Definition
- broad
- variably and erratically absorbed
- first pass metabolism
- systematically
- tissue parasite forms
Term
Mebendazole, a ___, is highly effective for ___ infections and very valuable for ___ infections. It is always taken __. It is highly effective against the following infections:
Definition
- Benzimidazole
- nematode
- mixed
- orally
- ascaris, intestinal capillariasis,
enterobiasis, trichuriasis, and hookworm infections.
Term
Benzimidazoles (Mebendazole and Albendazole)) bind ___ to __ __ ___ and inhibit ___ ____. They also ___ __ ____.
Definition
- selectively to worm b-tubulin
- inhibit microtubule polymerization
- uncouple oxidative phosphorylation
Term
Mebendazole and Albendazole produce __ side effects with short term use. Albendazole is ___ and ___ in animals. IT IS CONTRAINDICATED IN PREGNANT WOMEN.
Definition
- few
- teratogenic and embryotoxic
Term
Pyrantal Pamoate is useful in humans as an alternative to ___ for ____ and ___. It is also highly effective in ___, __ __, and ___.
Definition
- mebendazole
- ascariasis (round worm) and enterobiasis (pin worm)
- Ancylostoma, N. americanus, and Trichostongylus
Term
___ ___ is widely used in veterinarian practice as a ___ spectrum antihelminitic against ____, ____, and ___ infections.
Definition
- Pyrantel Pamoate
- broad
- pinworm, roundworm, and hookworm
Term
Pyarantal Pamoate is ___ absorbed by oral adimistration, making it active against ___ parasites. It directly activates ___ receptors and inhibits ____. It acts as a ___ __ ___ causing parasite ___ and ___.
Definition
- poorly
- GI
- activates nicotinic recptors
- inhibits cholinesterases
- depolarizing neuromuscular blocker
- spasm and paralysis
Term
Side effects of pyrantal pamoate:
Definition
- oral use only
- transient GI upset
- headache
- dizziness
- rash
- fever

CAN BE LETHAL IF GIVEN PARENTERALLY
Term
why would you not ever give pyrantal pamoate via i.v.:
Definition
it can be lethal if given parenterally

MUST BE GIVEN PO
Term
Piperazine is an ___ __ choice for ___ and ___ infection.
Definition
inexpensive second
roundworm and pinworm
Term
Piperazine causes ___ of parasite skeletal muscle and the ___ worms get expelled ___.
Definition
paralysis
paralyzed
alive
Term
Piperazine is generally well tolerated but can be lethal at high doses.
Definition
Term
Ivermectin aka ___ is available from the ___.
Definition
- Mectizan
- CDC
Term
Ivermectin is the preferred drug for mass control and treatment of ____. It is also effective against nematodes including ____, ____, ___, and ___. (KNOW THESE IN RED).
Definition
- onchocerciasis (river blindness)
- nematodes (Roundworms)
including strongyloidiasis, ascariasis, trichuriasis,
and enterobiasis.
Term
Ivermectin is Available in U.S. for compassion use from
Merck, Sharp & Dohme.
Extensively used to control and treat a broad spectrum
of infections caused by nematodes, insects, ticks,
and mites that plague livestock and domestic animals.
Definition
Term
drug used to control nematode, insect, tick, and mite infections that plaque livestock and domestic animals?
Definition
Ivermectin
Term
Ivermectin ___nematodes and other insects by inducing a __ ___ of the musculature. It is thought to activate ____ ___or __ gated __ channels.
Definition
- immobilizes
- tonic paralysis
- invertebrate GABA or glutamate gated chloride channels
Term
Ivermectin side effects and toxicity:
Definition
Usually well tolerated
Fever, rashes headache or muscle or joint pain.
Adverse effects occur due to dying parasites.
Contraindicated in children < 5 years, pregnant women,
and patients with meningitis.
Term
Ivermectin is contraindicated in what 3 types of patients?
Definition
- children under 5
- pregnant women
- patients with meningitis
Term
Antihelminthic drugs for flatworms/cestodes:
Definition
Nicolsamide- used for tapeworm infection
Term
Niclosamide is used for ___ __ more specifically __ __ infections.
Definition
flat worm
tape worm
Term
Mechanism of Niclosamide:
Definition
- minimal GI absorption
- inhibition of oxidative phosphorylation
- stimulation of ATPase activity
- leads to depletion of ATP
Term
Niclosamide side effects are mild.
Definition
Term
____ is approved in the U.S. for treatment of schistosomiasis and liver fluke infection.
Definition
Praziquantel (aka Biltricide)(
Term
Praziquantal uses:
Definition
- tmt of schistomiasis
- tmt of liver fluke infection
- versatile safe drug used to treat infections with many other trematodes and cestodes
Term
Praziquantal works by ___ ___ ___ followed by ___ and ___ ___ possibly by ___ ___ permeability. Affected worms ___ from host tissues. Higher doses causes ___damage which activates host immune system.
Definition
- increasing muscular activity
- contraction and spastic paralysis
- increasing caclium
- detach
- tegumental
Term
Be careful with high doses of Praziquantal b/c ___ ___ may occur.
Definition
tegumental damage, which would activate host immune system
Term
Side effects and toxicity:
Definition
- GI discomfort
- headache
- muscle and joint aches
- more severe patients with heavy infestations
- indirect effects related to death of parasite
- avoid use in children under 4, pregnant women, and patients with ocular cysticercosis
Term
Praziquantal is contraindicated in which patients:
Definition
- children under 4
- pregnant women
- patients with ocular cysticercosis
Term
treatment of flukes:
Definition
Praziquantal (Biltricide)
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