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Questions and Answers
Which statement accurately describes the mechanism of action for metronidazole and tinidazole?
Which statement accurately describes the mechanism of action for metronidazole and tinidazole?
A pregnant woman is diagnosed with amebiasis and needs treatment, which drug is the most appropriate first-line option?
A pregnant woman is diagnosed with amebiasis and needs treatment, which drug is the most appropriate first-line option?
Which of the following best describes the therapeutic classification of iodoquinol?
Which of the following best describes the therapeutic classification of iodoquinol?
What is a significant limitation of using Emetine for treating amebiasis?
What is a significant limitation of using Emetine for treating amebiasis?
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Which of the following is a key difference between metronidazole and tinidazole in their application for treating trichomoniasis?
Which of the following is a key difference between metronidazole and tinidazole in their application for treating trichomoniasis?
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Which of the following is NOT a known mechanism of action for antiprotozoal drugs used to treat trypanosomiasis?
Which of the following is NOT a known mechanism of action for antiprotozoal drugs used to treat trypanosomiasis?
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A patient presents with late-stage African trypanosomiasis with CNS involvement. Which of the following drug options is most likely to be used?
A patient presents with late-stage African trypanosomiasis with CNS involvement. Which of the following drug options is most likely to be used?
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Which of the following drugs used to treat parasitic infections is also used topically to reduce unwanted facial hair in women?
Which of the following drugs used to treat parasitic infections is also used topically to reduce unwanted facial hair in women?
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What is the primary mode of transmission for African trypanosomiasis?
What is the primary mode of transmission for African trypanosomiasis?
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Which drug, used to treat trypanosomiasis, is thought to act by inhibiting polyamine biosynthesis?
Which drug, used to treat trypanosomiasis, is thought to act by inhibiting polyamine biosynthesis?
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Which of the following best describes the mechanism of Nifurtimox?
Which of the following best describes the mechanism of Nifurtimox?
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Which of the following drugs is characterized as a polysulfonated naphthyl urea?
Which of the following drugs is characterized as a polysulfonated naphthyl urea?
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Which of these is a characteristic of Trypanosoma cruzi infection?
Which of these is a characteristic of Trypanosoma cruzi infection?
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Which of the following medications is considered a first-line treatment for the early stage of West African trypanosomiasis?
Which of the following medications is considered a first-line treatment for the early stage of West African trypanosomiasis?
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What is the primary mechanism of action of miltefosine in treating leishmaniasis?
What is the primary mechanism of action of miltefosine in treating leishmaniasis?
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Which of these medications is known to treat both leishmaniasis and Primary Amebic Meningoencephalitis (PAM)?
Which of these medications is known to treat both leishmaniasis and Primary Amebic Meningoencephalitis (PAM)?
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Which of the following drugs used to treat Giardiasis has a disulfiram-like reaction as a potential side effect?
Which of the following drugs used to treat Giardiasis has a disulfiram-like reaction as a potential side effect?
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A patient with East African trypanosomiasis presents with central nervous system involvement. Which medication would be the MOST appropriate first-line option?
A patient with East African trypanosomiasis presents with central nervous system involvement. Which medication would be the MOST appropriate first-line option?
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Which of the following statements is correct regarding the mechanism of action of tinidazole?
Which of the following statements is correct regarding the mechanism of action of tinidazole?
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What is the treatment for Chagas disease, according to the provided text?
What is the treatment for Chagas disease, according to the provided text?
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Which of the following best describes the clinical manifestations of leishmaniasis?
Which of the following best describes the clinical manifestations of leishmaniasis?
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Which antimalarial drug's mechanism primarily involves affecting DNA synthesis?
Which antimalarial drug's mechanism primarily involves affecting DNA synthesis?
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A patient taking an anti malarial drug experiences hearing issues, visual disturbances, and CNS problems. Which medication is most likely the culprit?
A patient taking an anti malarial drug experiences hearing issues, visual disturbances, and CNS problems. Which medication is most likely the culprit?
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Which drug is specifically noted for being a prodrug converted into an active medication?
Which drug is specifically noted for being a prodrug converted into an active medication?
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Which medication used in the treatment of malaria might cause hemolysis with pregnancy as an adverse effect?
Which medication used in the treatment of malaria might cause hemolysis with pregnancy as an adverse effect?
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What is the primary mechanism of action for the combination of atovaquone and proguanil?
What is the primary mechanism of action for the combination of atovaquone and proguanil?
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Besides being a blood schizonticide, what is another notable characteristic of lumefantrine?
Besides being a blood schizonticide, what is another notable characteristic of lumefantrine?
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Which of the following anti-malarial drugs has its mechanism described as ‘unknown’ in the text?
Which of the following anti-malarial drugs has its mechanism described as ‘unknown’ in the text?
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Which of the following adverse effects are NOT commonly associated with antiprotozoal drugs?
Which of the following adverse effects are NOT commonly associated with antiprotozoal drugs?
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Which of the following is the primary way humans contract toxoplasmosis?
Which of the following is the primary way humans contract toxoplasmosis?
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Which statement accurately reflects the role of cats in the spread of toxoplasmosis?
Which statement accurately reflects the role of cats in the spread of toxoplasmosis?
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Why is Leucovorin administered in toxoplasmosis treatment?
Why is Leucovorin administered in toxoplasmosis treatment?
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What is the primary mechanism of action of Atovaquone?
What is the primary mechanism of action of Atovaquone?
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Which of the following diseases is NOT mentioned as being treated with Atovaquone?
Which of the following diseases is NOT mentioned as being treated with Atovaquone?
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What is a distinguishing feature of Pneumocystis jirovecii (PJP) that led to its reclassification?
What is a distinguishing feature of Pneumocystis jirovecii (PJP) that led to its reclassification?
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Which drug used in the treatment of Pneumocystis jirovecii pneumonia is also used in the treatment of Mycobacterium leprae infections?
Which drug used in the treatment of Pneumocystis jirovecii pneumonia is also used in the treatment of Mycobacterium leprae infections?
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What is the primary target of most drugs developed to combat malaria infection?
What is the primary target of most drugs developed to combat malaria infection?
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A patient presents with a mild intestinal amebiasis infection and is unable to tolerate metronidazole. Which of the following is the MOST appropriate alternative treatment?
A patient presents with a mild intestinal amebiasis infection and is unable to tolerate metronidazole. Which of the following is the MOST appropriate alternative treatment?
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A patient with a severe intestinal amebiasis infection is being treated with metronidazole and a luminal agent. If the patient is unable to tolerate tetracycline, which of the following should be used as an alternative?
A patient with a severe intestinal amebiasis infection is being treated with metronidazole and a luminal agent. If the patient is unable to tolerate tetracycline, which of the following should be used as an alternative?
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Which of the following best describes the dosing regimen for a patient with an asymptomatic amebiasis infection using Iodoquinol?
Which of the following best describes the dosing regimen for a patient with an asymptomatic amebiasis infection using Iodoquinol?
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A patient with hepatic amebic abscess is treated with metronidazole and a luminal agent. If metronidazole is not tolerated which drug should be used as an alternative?
A patient with hepatic amebic abscess is treated with metronidazole and a luminal agent. If metronidazole is not tolerated which drug should be used as an alternative?
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What is a distinguishing factor of the duration of metronidazole treatment in a severe intestinal infection compared to a hepatic abscess?
What is a distinguishing factor of the duration of metronidazole treatment in a severe intestinal infection compared to a hepatic abscess?
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For a patient with symptomatic amebiasis, what is the rationale for using a 'luminal agent' in addition to a tissue-acting amebicide such as metronidazole?
For a patient with symptomatic amebiasis, what is the rationale for using a 'luminal agent' in addition to a tissue-acting amebicide such as metronidazole?
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If a patient with a severe intestinal amebiasis infection is not able to take metronidazole, which other combination of drugs might be recommended?
If a patient with a severe intestinal amebiasis infection is not able to take metronidazole, which other combination of drugs might be recommended?
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A patient is diagnosed with an ameboma. Which of the following is the most likely treatment approach according to the provided text?
A patient is diagnosed with an ameboma. Which of the following is the most likely treatment approach according to the provided text?
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Flashcards
What is the mechanism of action of Metronidazole and Tinidazole in treating trichomoniasis?
What is the mechanism of action of Metronidazole and Tinidazole in treating trichomoniasis?
Metronidazole and Tinidazole are drugs used to treat trichomoniasis. They work by disrupting DNA's tertiary structure in anaerobic organisms and protozoal cells.
What is trichomoniasis and why is it important to treat both partners?
What is trichomoniasis and why is it important to treat both partners?
Trichomoniasis is a sexually transmitted infection caused by the parasite Trichomonas Vaginalis. It's important to treat both the infected person and their partner, even if the partner is asymptomatic.
What are Emetine and Dehydroemetine and how do they work?
What are Emetine and Dehydroemetine and how do they work?
Emetine and Dehydroemetine are systemic amebicides that are used to treat infections caused by Entamoeba histolytica. These drugs block the chain elongation of proteins in the parasite, but can have significant heart toxicity and are therefore reserved for severe cases.
What is amebic dysentery and how are its treatments classified?
What is amebic dysentery and how are its treatments classified?
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What is Iodoquinol and why is it used with caution?
What is Iodoquinol and why is it used with caution?
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Benznidazole
Benznidazole
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Pentamidine
Pentamidine
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Eflornithine
Eflornithine
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Sodium stibogluconate
Sodium stibogluconate
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Miltefosine
Miltefosine
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Metronidazole
Metronidazole
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Tinidazole
Tinidazole
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Trichomoniasis
Trichomoniasis
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African Trypanosomiasis
African Trypanosomiasis
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Chagas' Disease
Chagas' Disease
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Suramin
Suramin
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Melarsoprol
Melarsoprol
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Nifurtimox
Nifurtimox
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Antiprotozoal Agents
Antiprotozoal Agents
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What is Diloxanide furoate's mechanism of action?
What is Diloxanide furoate's mechanism of action?
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How does Iodoquinol work against Entamoeba histolytica?
How does Iodoquinol work against Entamoeba histolytica?
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What is the mechanism of action of Paromomycin against Entamoeba histolytica?
What is the mechanism of action of Paromomycin against Entamoeba histolytica?
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How does Metronidazole work against Entamoeba histolytica?
How does Metronidazole work against Entamoeba histolytica?
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What is the mechanism of action of Tinidazole against Entamoeba histolytica?
What is the mechanism of action of Tinidazole against Entamoeba histolytica?
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How do Dehydroemetine and Emetine work against Entamoeba histolytica?
How do Dehydroemetine and Emetine work against Entamoeba histolytica?
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What is the mechanism of action for Chloroquine in treating amebic liver abscesses?
What is the mechanism of action for Chloroquine in treating amebic liver abscesses?
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What are the alternative treatments for moderate to severe intestinal amebiasis?
What are the alternative treatments for moderate to severe intestinal amebiasis?
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Quinine
Quinine
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Proguanil
Proguanil
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Tafenoquine
Tafenoquine
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Atovaquone; Proguanil
Atovaquone; Proguanil
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Artemether; Lumefantrine
Artemether; Lumefantrine
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Plasmodium falciparum
Plasmodium falciparum
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Toxoplasmosis
Toxoplasmosis
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Pneumocystis jirovecii Pneumonia (PCP)
Pneumocystis jirovecii Pneumonia (PCP)
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Pyrimethamine
Pyrimethamine
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Atovaquone
Atovaquone
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Malaria
Malaria
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Atovaquone (Mepron)
Atovaquone (Mepron)
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Pyrimethamine
Pyrimethamine
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Study Notes
Antiprotozoal Agents and Anthelmintic Agents
- Anti-infective agents for parasitic infections
- CDC Drug Information:
- CDC Drug Service, Division of Host Factors, Center for Infectious Disease
- (404) 639-3670, 8 AM to 4:30 PM EST, Monday through Friday
- After-hour or holiday emergencies: (404) 639-2888
- Also 1-800-232-4636 (1-800-CDC-INFO)
Organisms
- Trypanosomiasis:
- Trypanosoma gambiense, T. brucei
- Causes African trypanosomiasis (sleeping sickness)
- Transmitted by tsetse flies
- Hemoflagellates
- Progressive and fatal disease
- Initially affects CNS (fever, lymphadenopathy, splenomegaly, myocarditis)
- Later, terminal cardiac failure
- Trypanosoma cruzi:
- Causes South American trypanosomiasis (Chagas' disease)
- Cardiomyopathy, megacolon, death are common
- Transmitted by blood transfusion
Treatments (Antiprotozoa)
- Suramin (CDC):
- Polysulfonated naphthyl urea
- Inhibits several parasitic enzymes
- Exact mechanism unknown
- Pentamidine:
- Inhibits DNA and RNA polymerase, oxidative phosphorylation
- Melarsoprol (Mel B, i.v.):
- Trivalent arsenical
- Binds to parasitic enzymes, particularly sulfhydryl groups (more sensitive to parasitic enzymes than the host)
- Used in later stages of CNS involvement
- Eflornithine (Ornidyl):
- FDA approved
- Parenteral formulation available through WHO
- Inhibits polyamine biosynthesis in Trypanosoma
- Effective for late-stage trypanosomiasis
- Wide range of hematological adverse effects
- Topical formulation (Vaniqa) available for reducing unwanted facial hair in women
- Nifurtimox (Lampit, CDC):
- Nitro-heterocyclic drug for T. cruzi
- Suppressive and possibly curative
- Produces intracellular free radicals that kill the organism
- Used in chronic stages with minimal effects
- Also used for Chagas disease (BENZNIDAZOLE)
Treatment of African Trypanosomiasis
- Reference: Katzung 14th Edition
- Table with First-Line and Alternative Drugs for West and East African Trypanosomiasis, distinguishing between early stage and CNS involvement
Leishmaniasis
- Visceral, cutaneous, and mucocutaneous forms
- Self-resolving cutaneous ulcers, mutilating mucocutaneous disease, lethal systemic illnesses
- Sodium stibogluconate (Pentostam):
- Parenteral
- Exact mechanism unknown
- Inhibits glycolysis and TCA cycle
- Can cause cardiac and pancreas issues
- Miltefosine (oral, Impavido):
- Orally active
- Mechanism binds to parasitic DNA/inhibits cytochrome c oxidase
- Also treats Naegleria fowleri infection (Primary Amebic Meningoencephalitis)
- Naegleria approved drug is Amphotericin B lipid formulations
Giardiasis
- Caused by Giardia lamblia (flagellate protozoa)
- Most infected people are asymptomatic
- Causes transient or persistent diarrhea
- Cysts are common in contaminated water
- Metronidazole (Flagyl):
- Binds to proteins and DNA of Giardia
- Antibacterial, Disulfiram-like reaction
- Tinidazole (Fasigyn, Tindamax):
- Amebicidal, bactericidal, trichomonicidal
- Disrupts DNA's tertiary structure, inhibiting nucleic acid synthesis
- Single dose treatment for Giardiasis
Trichomoniasis
- Caused by Trichomonas vaginalis
- 3 million women infected annually in the US
- Inhabits the genitourinary tract, causes vaginitis in women and urethritis in men
- Metronidazole (Flagyl, Metron):
- Oral single course is successful in treatment
- Partner treatment is necessary
- Resistant strains prevalent
- Tinidazole (Fasigyn, Tindamax):
- Amebicidal, bactericidal, trichomonacidal
- Disrupts DNA, inhibiting nucleic acid synthesis
- Other applications are for treating anaerobic bacterial infections
Amebiasis (Amebic Dysentery)
- Caused by Entamoeba histolytica
- Mild to severe dysentery, colitis
- Classified into Luminal, Systemic and Mixed amebicides
- Luminal amebicides:
- Iodoquinol (Diodoquin, Yodoxin)
- Alternative for asymptomatic carriers
- Myelo-optic neuropathy
- Paromomycin (aminoglycoside): Only against intestinal forms of E. histolytica
- First line for Amebiasis and Giardiasis in pregnancy
- Systemic amebicides:
- Emetine and Dehydroemetine
- Block chain elongation of proteins
- IM is preferred route
- Contraindicated in pregnancy, significant cardiotoxicity, reserved for extraintestinal amebiasis in patients who do not respond to or cannot receive metronidazole
Toxoplasmosis
- Causative organism: Toxoplasma gondii
- Cats and other felines are natural hosts
- Humans infected through raw meat, contaminated vegetables, direct contact with cats
- 70% of US adults seropositive
- Clinical symptoms: Lymphadenopathy, serious sickness (mostly in immunocompromised patients—encephalitis)
- Pyrimethamine and sulfonamide (sulfadiazine):
- Long-term use
- Leucovorin to counteract folate deficiency
- Atovaquone (Mepron):
- Synthetic hydroxy-naphthoquinone
- Inhibits mitochondrial ETC
- Orally administered
- Side effects include rash, fever
- Used in toxoplasmosis and AIDS patients (treat P. jirovecii pneumonia)
- Toxoplasmic encephalitis is common cause of death in people with AIDS
Pneumocystosis (PCP, PJP)
- Common life-threatening opportunistic infection in immunocompromised patients
- Molecular analysis of ribosomal RNA classified P. carinii as fungi
- TMP-SMZ: (discussed elsewhere)
- Pentamidine: Polymerase inhibition, and oxidative phosphorylation inhibition
- Atovaquone: Mitochondrial electron transport chain (ETC) inhibitor
- Dapsone: For treatment of mycobacterial infections
Malaria
- World's most devastating infectious disease with 300–500 million clinical cases and 3 million deaths per year
- Multi-drug resistance is major challenge in developing countries
- Drugs based on action against asexual erythrocytic forms
- Plasmodium falciparum (85%): Malignant tertian malaria, severe clinical signs, few relapses
- Plasmodium vivax: Benign tertian malaria, milder symptoms, dormant hepatic stage causes relapse
- Plasmodium ovale: Similar to P. vivax
- Plasmodium malariae: Quartan malaria; tropical; rare relapse
Antimalarial Drugs
- Erythrocytic Cycle:
- Rapid acting: Chloroquine, Quinine, Quinidine, Mefloquine, Halofantrine
- Slow acting: Proguanil, Pyrimethamine
- Exoerythrocytic Stage:
- Tissue schizonticides (prophylactic): Chloroguanide (Proguanil), Pyrimethamine
- Tissue schizonticides-preventing relapse: Primaquine
- Gametocides (prevents mosquito infection): Primaquine, Chloroquine, Quinine
Antimalarial Drugs (Specific Drugs)
- Detailed descriptions of different antimalarial drugs, mechanism of action, use, adverse effects
Anti-Worm Drugs (Anthelmintic)
- Infections mostly seen are intestinal nematodes (parasites, eggs, and larvae identified in feces)
- Cathartic prior to oral dosage may increase efficiency of treatment
- Toxic, Pregnancy, and GI ulcerations are contraindicated
- Nematodes (Roundworms):
- Mebendazole and Albendazole: inhibit microtubule synthesis, expelling parasite in feces
- Pyrantel pamoate: neuromuscular blocking agent, causing paralysis and release in intestinal tract
- Ivermectin: treats onchocerciasis and nematodes, hyperpolarization, causing paralysis and death of parasite
- Nematodes (Roundworms):
- Trematodes & Cestodes: - Niclosamide: inhibits oxidative phosphorylation, stimulates ATPase, treats Taenia - Praziquantel: increases calcium permeability, paralyzing worm musculature, treats Schistosoma and cysticercosis
Filariasis, Elephantiasis
- Diethylcarbamazine (Hetrazan): effective against microfilariae, not adult worms, affects microfilarial membranes and musculature by hyperpolarization
- Ivermectin, Albendazole
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Description
Test your knowledge on the mechanisms of action, therapeutic classifications, and limitations of various antiprotozoal drugs, including metronidazole, tinidazole, and iodoquinol. This quiz also covers treatment options for conditions like amebiasis and trypanosomiasis. Perfect for students studying pharmacology and infectious diseases.