L-22 Antiprotozoal Drugs Quiz
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Questions and Answers

Which statement accurately describes the mechanism of action for metronidazole and tinidazole?

  • They interfere with the electron transport chain, leading to ATP production inhibition, but not disrupting DNA or nucleic acid synthesis.
  • They disrupt the tertiary structure of DNA and inhibit nucleic acid synthesis. (correct)
  • They inhibit protein synthesis by blocking chain elongation.
  • They primarily target the cell membrane of protozoal cells, causing lysis.
  • A pregnant woman is diagnosed with amebiasis and needs treatment, which drug is the most appropriate first-line option?

  • Iodoquinol, as it is safe to use in pregnant women.
  • Paromomycin, due to its safety profile and effectiveness against intestinal forms. (correct)
  • Emetine, due to its effectiveness against extraintestinal amebiasis.
  • Metronidazole, as the most widely used systemic amebicide.
  • Which of the following best describes the therapeutic classification of iodoquinol?

  • Mixed amebicide targeting both intestinal and extraintestinal infections.
  • First-line systemic amebicide for amebiasis in pregnancy.
  • Luminal amebicide used as an alternative for asymptomatic carriers. (correct)
  • Systemic amebicide used for severe dysentery.
  • What is a significant limitation of using Emetine for treating amebiasis?

    <p>It has a high risk of cardiotoxicity and is contraindicated in pregnancy. (A)</p> Signup and view all the answers

    Which of the following is a key difference between metronidazole and tinidazole in their application for treating trichomoniasis?

    <p>Tinidazole is effective against resistant strains of trichomoniasis, whereas metronidazole is not. (C)</p> Signup and view all the answers

    Which of the following is NOT a known mechanism of action for antiprotozoal drugs used to treat trypanosomiasis?

    <p>Stimulation of host cell growth. (D)</p> Signup and view all the answers

    A patient presents with late-stage African trypanosomiasis with CNS involvement. Which of the following drug options is most likely to be used?

    <p>Melarsoprol (D)</p> Signup and view all the answers

    Which of the following drugs used to treat parasitic infections is also used topically to reduce unwanted facial hair in women?

    <p>Eflornithine (B)</p> Signup and view all the answers

    What is the primary mode of transmission for African trypanosomiasis?

    <p>Tsetse fly bites (A)</p> Signup and view all the answers

    Which drug, used to treat trypanosomiasis, is thought to act by inhibiting polyamine biosynthesis?

    <p>Eflornithine (B)</p> Signup and view all the answers

    Which of the following best describes the mechanism of Nifurtimox?

    <p>Production of intracellular free radicals (A)</p> Signup and view all the answers

    Which of the following drugs is characterized as a polysulfonated naphthyl urea?

    <p>Suramin (C)</p> Signup and view all the answers

    Which of these is a characteristic of Trypanosoma cruzi infection?

    <p>Megacolon (C)</p> Signup and view all the answers

    Which of the following medications is considered a first-line treatment for the early stage of West African trypanosomiasis?

    <p>Pentamidine (D)</p> Signup and view all the answers

    What is the primary mechanism of action of miltefosine in treating leishmaniasis?

    <p>Binding to parasitic DNA and inhibition of cytochrome c oxidase (B)</p> Signup and view all the answers

    Which of these medications is known to treat both leishmaniasis and Primary Amebic Meningoencephalitis (PAM)?

    <p>Miltefosine (C)</p> Signup and view all the answers

    Which of the following drugs used to treat Giardiasis has a disulfiram-like reaction as a potential side effect?

    <p>Metronidazole (A)</p> Signup and view all the answers

    A patient with East African trypanosomiasis presents with central nervous system involvement. Which medication would be the MOST appropriate first-line option?

    <p>Melarsoprol (A)</p> Signup and view all the answers

    Which of the following statements is correct regarding the mechanism of action of tinidazole?

    <p>Disrupts DNA's tertiary structure and inhibits nucleic acid synthesis in anaerobic organisms (B)</p> Signup and view all the answers

    What is the treatment for Chagas disease, according to the provided text?

    <p>Benznidazole (B)</p> Signup and view all the answers

    Which of the following best describes the clinical manifestations of leishmaniasis?

    <p>Can include a self-resolving cutaneous ulcer, a mutilating mucocutaneous disease, or a lethal systemic illness. (D)</p> Signup and view all the answers

    Which antimalarial drug's mechanism primarily involves affecting DNA synthesis?

    <p>Quinine (A)</p> Signup and view all the answers

    A patient taking an anti malarial drug experiences hearing issues, visual disturbances, and CNS problems. Which medication is most likely the culprit?

    <p>Quinine (B)</p> Signup and view all the answers

    Which drug is specifically noted for being a prodrug converted into an active medication?

    <p>Proguanil (D)</p> Signup and view all the answers

    Which medication used in the treatment of malaria might cause hemolysis with pregnancy as an adverse effect?

    <p>Quinine (C)</p> Signup and view all the answers

    What is the primary mechanism of action for the combination of atovaquone and proguanil?

    <p>Inhibition of the ETC and folate reductase (C)</p> Signup and view all the answers

    Besides being a blood schizonticide, what is another notable characteristic of lumefantrine?

    <p>It is an organochloride. (D)</p> Signup and view all the answers

    Which of the following anti-malarial drugs has its mechanism described as ‘unknown’ in the text?

    <p>Tafenoquine (B)</p> Signup and view all the answers

    Which of the following adverse effects are NOT commonly associated with antiprotozoal drugs?

    <p>Hypertension (A)</p> Signup and view all the answers

    Which of the following is the primary way humans contract toxoplasmosis?

    <p>Ingestion of raw or undercooked meat containing cysts and vegetables carrying oocytes. (B)</p> Signup and view all the answers

    Which statement accurately reflects the role of cats in the spread of toxoplasmosis?

    <p>Cats are the only animals capable of shedding oocytes that can infect other animals, including humans. (B)</p> Signup and view all the answers

    Why is Leucovorin administered in toxoplasmosis treatment?

    <p>To prevent or reduce folate deficiency caused by pyrimethamine and sulfonamide usage. (B)</p> Signup and view all the answers

    What is the primary mechanism of action of Atovaquone?

    <p>It inhibits the mitochondrial electron transport chain (ETC) and related processes. (D)</p> Signup and view all the answers

    Which of the following diseases is NOT mentioned as being treated with Atovaquone?

    <p>Malaria (D)</p> Signup and view all the answers

    What is a distinguishing feature of Pneumocystis jirovecii (PJP) that led to its reclassification?

    <p>Its molecular analysis of ribosomal RNA, which indicated it is a fungus. (C)</p> Signup and view all the answers

    Which drug used in the treatment of Pneumocystis jirovecii pneumonia is also used in the treatment of Mycobacterium leprae infections?

    <p>Dapsone (A)</p> Signup and view all the answers

    What is the primary target of most drugs developed to combat malaria infection?

    <p>The merozoite form in the red blood cells. (A)</p> Signup and view all the answers

    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?

    <p>Tetracycline plus a luminal agent. (B)</p> Signup and view all the answers

    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?

    <p>Emetine or Dehydroemetine (C)</p> Signup and view all the answers

    Which of the following best describes the dosing regimen for a patient with an asymptomatic amebiasis infection using Iodoquinol?

    <p>650 mg three times daily for 21 days. (C)</p> Signup and view all the answers

    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?

    <p>Emetine or Dehydroemetine followed by chloroquine. (C)</p> Signup and view all the answers

    What is a distinguishing factor of the duration of metronidazole treatment in a severe intestinal infection compared to a hepatic abscess?

    <p>The duration is the same for both (C)</p> Signup and view all the answers

    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?

    <p>To eradicate any remaining cysts in the lumen of the intestine. (B)</p> Signup and view all the answers

    If a patient with a severe intestinal amebiasis infection is not able to take metronidazole, which other combination of drugs might be recommended?

    <p>Tinidazole, emetine, and iodoquinol. (A)</p> Signup and view all the answers

    A patient is diagnosed with an ameboma. Which of the following is the most likely treatment approach according to the provided text?

    <p>Metronidazole and a luminal agent (A)</p> Signup and view all the answers

    Flashcards

    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?

    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?

    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?

    Amebic dysentery is a severe form of intestinal infection caused by Entamoeba histolytica. It can be treated with various drugs, which are classified based on their site of action.

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    What is Iodoquinol and why is it used with caution?

    Iodoquinol is a luminal amebicide that is used as an alternative to treat asymptomatic carriers of Entamoeba histolytica. It should be used with caution as it can cause myelo-optic neuropathy.

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    Benznidazole

    A medication used to treat Chagas disease, which is caused by the parasite Trypanosoma cruzi.

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    Pentamidine

    A medication used to treat West African trypanosomiasis, a disease caused by the parasite Trypanosoma brucei gambiense.

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    Eflornithine

    A medication used to treat both early and CNS stages of West African trypanosomiasis.

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    Sodium stibogluconate

    A medication used for the treatment of Leishmaniasis, a disease caused by parasites of the genus Leishmania.

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    Miltefosine

    An oral medication for the treatment of Leishmaniasis.

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    Metronidazole

    A medication for the treatment of Giardiasis, an intestinal infection caused by the parasite Giardia lamblia.

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    Tinidazole

    An effective drug for treating Giardiasis, Trichomoniasis, and Amebiasis.

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    Trichomoniasis

    A sexually transmitted disease caused by the parasite Trichomonas vaginalis.

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    African Trypanosomiasis

    African trypanosomiasis, also known as sleeping sickness, is caused by Trypanosoma gambiense and T. brucei. Transmitted by tsetse flies. Causes progressive symptoms including fever, enlarged lymph nodes, and ultimately, CNS involvement. It's usually fatal without treatment.

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    Chagas' Disease

    Chagas' disease, or South American Trypanosomiasis, is caused by Trypanosoma cruzi. Transmitted through insects or blood transfusions. Characterized by fever, inflammation, and ultimately heart, digestive, and nervous system damage. Can be fatal.

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    Suramin

    Suramin is a polysulfonated naphthyl urea used to treat African trypanosomiasis. It inhibits several parasitic enzymes, although the exact mechanism is complex.

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    Melarsoprol

    Melarsoprol is a trivalent arsenical drug used in late-stage African trypanosomiasis. It inhibits key parasitic enzymes by binding to sulfhydryl groups. Has severe side effects. Only used in late-stage disease.

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    Nifurtimox

    Nifurtimox is a nitro-heterocyclic drug used to treat Chagas' disease. It works by producing free radicals inside the parasite, leading to its death. Used in chronic stages with limited effectiveness.

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    Antiprotozoal Agents

    Antiprotozoal agents are drugs that target and kill protozoan parasites. They are crucial for managing and treating various diseases caused by these parasites.

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    What is Diloxanide furoate's mechanism of action?

    A luminal amebicide that works by interfering with the parasite's ability to form cysts and helps eliminate Entamoeba histolytica from the gut.

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    How does Iodoquinol work against Entamoeba histolytica?

    Iodoquinol is a luminal amebicide that works by interfering with the parasite's iodine metabolism and helps eliminate Entamoeba histolytica from the gut.

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    What is the mechanism of action of Paromomycin against Entamoeba histolytica?

    Paromomycin is an aminoglycoside antibiotic that works by inhibiting protein synthesis in Entamoeba histolytica and helps eliminate the parasite from the gut.

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    How does Metronidazole work against Entamoeba histolytica?

    Metronidazole is a systemic amebicide that works by interfering with DNA synthesis in Entamoeba histolytica and effectively kills the parasite.

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    What is the mechanism of action of Tinidazole against Entamoeba histolytica?

    Tinidazole is a systemic amebicide that works by interfering with DNA synthesis in Entamoeba histolytica and effectively kills the parasite.

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    How do Dehydroemetine and Emetine work against Entamoeba histolytica?

    Dehydroemetine and Emetine are systemic amebicides that work by inhibiting protein synthesis in Entamoeba histolytica and effectively kill the parasite. However, their use is limited due to potential cardiovascular toxicity.

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    What is the mechanism of action for Chloroquine in treating amebic liver abscesses?

    Chloroquine is an antimalarial drug that is used in treating amebic liver abscesses. It works by disrupting the parasite's ability to break down heme.

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    What are the alternative treatments for moderate to severe intestinal amebiasis?

    Tetracycline, Erythromycin, and Luminal agents are used to eliminate the parasite from the gut.

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    Quinine

    A type of antimalarial drug that works by inhibiting DNA synthesis, effective against chloroquine-resistant strains of Plasmodium falciparum.

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    Proguanil

    A drug used in combination with chloroquine for malaria prophylaxis, known to inhibit DHF reductase.

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    Tafenoquine

    Approved for a single-dose radical cure of Plasmodium infections, the mechanism of action is unknown.

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    Atovaquone; Proguanil

    An antimalarial combination consisting of atovaquone and proguanil, effective against Plasmodium falciparum.

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    Artemether; Lumefantrine

    This artemisinin combination drug is effective against both drug-sensitive and drug-resistant Plasmodium falciparum.

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    Plasmodium falciparum

    A type of antimalarial drug that exhibits high resistance to single agents but potent synergistic effects when combined with other medications.

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    Toxoplasmosis

    A parasitic infection caused by the protozoan Toxoplasma gondii, which is commonly found in cats and can be transmitted to humans through contact with infected cat feces, undercooked meat, or contaminated water.

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    Pneumocystis jirovecii Pneumonia (PCP)

    A life-threatening opportunistic infection frequently seen in immunocompromised individuals, primarily caused by the fungus Pneumocystis jirovecii.

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    Pyrimethamine

    A common antimalarial drug that interferes with the parasite's ability to synthesize folate, a vital nutrient for its growth and development.

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    Atovaquone

    A drug used in the treatment of both toxoplasmosis and pneumocystosis. It inhibits mitochondrial electron transport, a crucial pathway for energy production in cells.

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    Malaria

    A serious parasitic disease primarily spread by infected mosquitos, causing symptoms like fever, chills, and sweating. The deadliest form, caused by Plasmodium falciparum, can be particularly dangerous.

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    Atovaquone (Mepron)

    A synthetic drug used to treat some parasitic infections, including toxoplasmosis and pneumocystosis, by disrupting mitochondrial electron transport.

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    Pyrimethamine

    A drug often used in combination with Sulfadiazine to treat toxoplasmosis. It is a folate synthesis inhibitor, preventing the parasite from making essential folate.

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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
    • 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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    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.

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