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Questions and Answers
What protozoal infection is commonly referred to as malaria?
What protozoal infection is commonly referred to as malaria?
Malaria
What is the genus of the protozoa that causes malaria?
What is the genus of the protozoa that causes malaria?
Plasmodium
Which of the following drugs is commonly used to prevent and treat malaria?
Which of the following drugs is commonly used to prevent and treat malaria?
What is a common side effect of chloroquine and hydroxychloroquine?
What is a common side effect of chloroquine and hydroxychloroquine?
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Primaquine is known to affect the parasite's mitochondria.
Primaquine is known to affect the parasite's mitochondria.
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What enzyme does pyrimethamine selectively inhibit?
What enzyme does pyrimethamine selectively inhibit?
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What is the primary site of action for quinine in the body?
What is the primary site of action for quinine in the body?
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Mefloquine is believed to increase the acidity of plasmodial food vacuoles, leading to cell rupture and death.
Mefloquine is believed to increase the acidity of plasmodial food vacuoles, leading to cell rupture and death.
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Where is chloroquine readily absorbed from?
Where is chloroquine readily absorbed from?
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What is the half-life of mefloquine?
What is the half-life of mefloquine?
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Primaquine is considered safe for use during pregnancy.
Primaquine is considered safe for use during pregnancy.
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Where is pyrimethamine primarily metabolized?
Where is pyrimethamine primarily metabolized?
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What is the primary route of excretion for quinine?
What is the primary route of excretion for quinine?
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What is the oral drug of choice for preventing and treating malaria?
What is the oral drug of choice for preventing and treating malaria?
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What alternative drug is used when chloroquine is not available?
What alternative drug is used when chloroquine is not available?
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What is the drug of choice to treat malaria caused by chloroquine-resistant strains?
What is the drug of choice to treat malaria caused by chloroquine-resistant strains?
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Which drug is commonly used in combination with chloroquine for treating malaria?
Which drug is commonly used in combination with chloroquine for treating malaria?
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What drug is used to treat malaria caused by resistant strains of Plasmodium falciparum?
What drug is used to treat malaria caused by resistant strains of Plasmodium falciparum?
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Which drug is considered the parenteral preferred treatment for malaria?
Which drug is considered the parenteral preferred treatment for malaria?
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Which of the following is a contraindication to using antimalarial drugs?
Which of the following is a contraindication to using antimalarial drugs?
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What are some common adverse effects associated with antimalarial drugs?
What are some common adverse effects associated with antimalarial drugs?
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Antimalarial drugs should be taken with food to minimize GI upset.
Antimalarial drugs should be taken with food to minimize GI upset.
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It is important to avoid consuming large quantities of alcohol while taking antimalarial drugs.
It is important to avoid consuming large quantities of alcohol while taking antimalarial drugs.
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What is the main mechanism of action for antiprotozoal drugs?
What is the main mechanism of action for antiprotozoal drugs?
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What antiprotozoal drug inhibits the enzyme dihydrofolate reductase?
What antiprotozoal drug inhibits the enzyme dihydrofolate reductase?
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What is a common side effect of metronidazole?
What is a common side effect of metronidazole?
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What is recommended for individuals who have a known allergy to antiprotozoal drugs?
What is recommended for individuals who have a known allergy to antiprotozoal drugs?
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What are some key things to remember when taking antiprotozoal medications?
What are some key things to remember when taking antiprotozoal medications?
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What do anthelmintic drugs target?
What do anthelmintic drugs target?
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What common side effects are often encountered with anthelmintic drugs?
What common side effects are often encountered with anthelmintic drugs?
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Anthelmintic drugs are usually safe for use in pregnant women.
Anthelmintic drugs are usually safe for use in pregnant women.
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What is the mechanism of action for alkylating agents?
What is the mechanism of action for alkylating agents?
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Alkylating agents are cell cycle-specific.
Alkylating agents are cell cycle-specific.
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What are some of the common adverse effects associated with alkylating agents?
What are some of the common adverse effects associated with alkylating agents?
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What is the mechanism of action for antimetabolites?
What is the mechanism of action for antimetabolites?
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Antimetabolites are most effective against rapidly dividing cells.
Antimetabolites are most effective against rapidly dividing cells.
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What common side effects are associated with antimetabolites?
What common side effects are associated with antimetabolites?
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Antimetabolites are contraindicated in pregnancy and lactation.
Antimetabolites are contraindicated in pregnancy and lactation.
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What is the primary mechanism of action for antineoplastic antibiotics?
What is the primary mechanism of action for antineoplastic antibiotics?
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Antineoplastic antibiotics are cell cycle-specific.
Antineoplastic antibiotics are cell cycle-specific.
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What is the mechanism of action for mitotic inhibitors?
What is the mechanism of action for mitotic inhibitors?
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Mitotic inhibitors are commonly administered orally.
Mitotic inhibitors are commonly administered orally.
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What are some of the most common adverse effects associated with mitotic inhibitors?
What are some of the most common adverse effects associated with mitotic inhibitors?
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What is the primary mechanism of action for hormones and hormone modulators?
What is the primary mechanism of action for hormones and hormone modulators?
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Hormones and hormone modulators are contraindicated in pregnancy and lactation.
Hormones and hormone modulators are contraindicated in pregnancy and lactation.
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What is the primary mechanism of action for cancer cell-specific agents?
What is the primary mechanism of action for cancer cell-specific agents?
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Cancer cell-specific agents are generally much more effective than traditional chemotherapy.
Cancer cell-specific agents are generally much more effective than traditional chemotherapy.
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Study Notes
Anti-infectives and Antineoplastic Agents
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Antimalarials
- Plasmodium is a genus of protozoal parasites
- Malaria is transmitted by the bite of the female Anopheles mosquito
- Major drugs used to prevent and treat malaria include chloroquine hydrochloride, chloroquine phosphate, hydroxychloroquine sulfate, mefloquine hydrochloride, primaquine phosphate, pyrimethamine, quinidine gluconate, and quinine sulfate
- Chloroquine and hydroxychloroquine disrupt protein synthesis
- Primaquine affects mitochondria
- Pyrimethamine inhibits dihydrofolate reductase
- Quinine incorporates into parasite DNA
- Mefloquine increases acidity of plasmodial food vacuoles
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Pharmacokinetics of Antimalarials
- Chloroquine is readily absorbed and concentrated in liver, spleen, kidney, and brain. Excretion is slow
- Mefloquine is a mixture of molecules
- Primaquine is readily absorbed and metabolized in the liver. Excretion mostly in the urine
- Pyrimethamine is readily absorbed and metabolized in the liver with peak levels within 2-6 hrs, half life 4 days.
- Quinine is rapidly absorbed and metabolized with a half-life of 4-6 hours, excreted in urine
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Indications of Antimalarial Drugs
- Chloroquine: drug of choice for all malaria strains
- Hydroxychloroquine: alternative to chloroquine
- Quinine: drug of choice for treating resistant strains of P. falciparum
- Primaquine: drug of choice with chloroquine to target P. malariae, P. vivax, and P. ovale
- Mefloquine: used to treat malaria caused by resistant strains of P. falciparum.
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Contraindications and Cautions of Antimalarials
- Known allergy to drugs
- Liver disease
- Alcoholism
- Lactation
- Pregnancy
- Retinal disease or damage
- Psoriasis or porphyria
- Damage to mucous membranes
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Adverse Effects of Antimalarials
- CNS effects: headache, dizziness, ataxia, loss of coordination, and peripheral neuropathy
- GI upset: nausea, vomiting, dyspepsia, and anorexia
- Hepatic dysfunction
- Dermatological effects: rash, pruritus, and possible hair loss
- Visual changes, possible blindness from retinal damage from the drug
- Ototoxicity
- Cinchonism may occur with high quinine levels
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Drug Interactions of Antimalarials
- Hydroxychloroquine and quinine may increase digoxin and cyclosporine levels.
- Mefloquine with beta blockers, quinine, quinidine, or other drugs prolonging cardiac conduction may produce ECG abnormalities or arrest
- Mefloquine with chloroquine may increase risk of seizures
- Mefloquine may reduce valproic acid levels
- Folic acid reduces antimicrobial effect of pyrimethamine
- Quinine may increase the effects of neuromuscular blockers leading to breathing difficulties
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Patient Teachings for Antimalarials
- Prophylactic doses of anti-malarials before, during, and after travel
- Drugs need to be taken with food or at mealtime to avoid GI discomfort
- Monitor for malaria symptoms after travel
- Notify doctor immediately of vision changes
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Antiprotozoals
- A diverse group acting on different pathways.
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Antiprotozoals' Indications
- Various infections including Pneumocystis carinii infections, amebiasis, giardiasis, trichomoniasis, toxoplasmosis, African trypanosomiasis, and leishmaniasis.
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Atovaquone Pharmacokinetics
- Slowly absorbed, protein bound
- Excreted through feces after 67 to 76 hours
- Metronidazole well-absorbed orally; metabolized in the liver, excretion occurs primarily in the urine after 8-15 hours.
- Pentamidine is well absorbed when given intravenously or intramuscularly. Excretion occurs primarily in the urine.
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Antiprotozoal Contraindications and Cautions
- Allergies
- Pregnancy
- Use caution with patients with CNS disease, hepatic disease, candidiasis, and women who are lactating
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Anthelmintics
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Action: Affect metabolic pathways unique to parasitic worms
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Indications: Treat infections caused by susceptible worms (albendazole, ivermectin, mebendazole, praziquantel, and pyrantel)
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Pharmacokinetics (Anthelmintics)
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Albendazole: poorly absorbed, metabolized in liver and excreted in urine.
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Ivermectin: readily absorbed, metabolized in the liver; excreted in feces. Ivermectin reaches peak levels in 4 hours
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Praziquantel: rapidly absorbed, metabolized in the liver, excreted in urine (within 1-3 hours)
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Pyrantel: poorly absorbed, mostly excreted in feces.
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Contraindications and Cautions (Anthelmintics)
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Known allergy to any drug, lactation, pregnancy
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Use caution in children under 2 years old
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Use caution in patients with renal or hepatic disease, severe diarrhea, and malnutrition.
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Adverse Effects (Anthelmintics)
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Abdominal discomfort
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Diarrhea
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Headache
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Dizziness
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Fever, shaking, chills, and malaise
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Rash, pruritus, and hair loss
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Renal failure and severe bone marrow depression
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Increased adverse effects with combined use of drugs
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Alkylating Agents
- Interfere with DNA processes to induce cell death
- Used mainly for slow-growing cancers
- Includes: altretamine, bendamustine, busulfan, carboplatin, carmustine, chlorambucil, cisplatin, cyclophosphamide, dacarbazine, ifosfamide, lomustine, mechlorethamine, melphalan, oxaliplatin, procarbazine, streptozocin, temozolomide
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Pharmacokinetics (Alkylating Agents)
- Absorption varies
- Little is known about tissue distribution
- Metabolized and sometimes activated in the liver.
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Contraindications and Cautions (Alkylating Agents)
- Pregnancy
- Lactation
- Known allergy to any of the drugs
- Bone-marrow suppression
- Renal or hepatic dysfunction
-
Adverse Effects (Alkylating Agents)
- Hematological effects (bone marrow suppression, leukopenia, thrombocytopenia, anemia, pancytopenia)
- GI effects (nausea, vomiting, anorexia, diarrhea, mucous membrane deterioration)
- Hepatic and renal toxicity
- Alopecia
- Increase in uric acid levels
-
Drug Interactions (Alkylating Agents)
- Use caution with drugs causing hepatic or renal toxicity
- Toxic to the liver: drugs adversely affect those metabolized in the liver
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Antimetabolites
- Mimic natural metabolites, impacting cell growth and division
- Useful for rapidly dividing cancers
- Includes: capecitabine, cladribine, clofarabine, cytarabine, floxuridine, fludarabine, fluorouracil, gemcitabine, mercaptopurine, methotrexate, pemetrexed, pentostatin, pralatrexate, thioguanine
-
Pharmacokinetics (Antimetabolites)
- Methotrexate: well absorbed and excreted in urine.
- Cytarabine, clofarabine, etc.: not well absorbed from GIT
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Contraindications and Cautions (Antimetabolites)
- Pregnancy
- Lactation
- Known allergy to drugs
- Bone marrow suppression
- Renal or hepatic impairment
-
Adverse Effects (Antimetabolites)
- Hematological effects (bone marrow suppression, leukopenia, thrombocytopenia, anemia, pancytopenia)
- Toxic GI effects (nausea, vomiting, anorexia, diarrhea, mucous membrane deterioration)
-
Drug Interactions (Antimetabolites)
- Use caution with drugs that cause hepatic or renal toxicity.
- Adverse effects when combined with drugs metabolized by liver or impacting liver
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Antineoplastic Antibiotics
- Selective toxicity against bacterial cells
- Also toxic to human cells
- Include: bleomycin, dactinomycin, daunorubicin, doxorubicin, epirubicin, idarubicin, mitomycin, mitoxantrone, valrubicin
-
Pharmacokinetics (Antineoplastic Antibiotics)
- Poorly absorbed from GIT
- Injected into site, metabolized in liver, excreted through urine
-
Contraindications and Cautions (Antineoplastic Antibiotics)
- Pregnancy
- Lactation
- Known allergy
- Bone marrow suppression
- Renal, hepatic impairment
-
Adverse Effects (Antineoplastic Antibiotics)
- Hematologic effects
- Toxic GI effects
-
Drug Interactions (Antineoplastic Antibiotics)
- Use caution with drugs causing liver or kidney toxicity.
-
Mitotic Inhibitors
- Interfere with cell division (mitosis)
- Useful for rapid-multiplying cells (cancers)
- Includes: cabazitaxel, docetaxel, eribulin, etoposide, ixabepilone, paclitaxel, teniposide, vinorelbine
-
Pharmacokinetics (Mitotic Inhibitors)
- Usually administered intravenously
- Metabolized in the liver and excreted in feces.
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Contraindications and Cautions (Mitotic Inhibitors)
- Pregnancy
- Lactation
- Known allergies
- Bone marrow suppression
- Renal or hepatic dysfunction
- Prolonged QT interval
-
Adverse Effects (Mitotic Inhibitors)
- Bone marrow suppression, leukopenia, anemia, thrombocytopenia
- GI effects: nausea, vomiting, anorexia, diarrhea
- Mucous membrane deterioration
- Hepatic or renal toxicity
- Alopecia, necrosis, cellulitis from extravasation
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Drug Interactions (Mitotic Inhibitors)
- Use caution with drugs known to cause liver or kidney toxicity.
-
Hormones and Hormone Modulators
- Block or interfere with receptor sites to prevent cancer growth
- Includes: abiraterone, anastrazole, bicalutamide, degarelix, enzalutamide, estramustine, exemestane, flutamide, fulvestrant, goserelin, histrelin, letrozole, leuprolide, megestrol, mitotane, nilutamide, tamoxifen, toremifene, triptorelin.
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Pharmacokinetics (Hormones and Hormone Modulators)
- Readily absorbed from the GIT
- Metabolized and excreted in the urine.
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Contraindications and Cautions (Hormones and Hormone Modulators)
- Pregnancy
- Lactation
- Hypersensitivity to a drug
- Hypercalcemia (for torimefene)
-
Adverse Effects (Hormones and Hormone Modulators)
- Menopause-associated effects (hot flashes, vaginal dryness, moodiness)
- Bone marrow suppression
- GI toxicity
- Hepatic dysfunction
- Hypercalcemia
- Increased risk of cardiovascular disease
- Adrenocortical insufficiency
-
Drug Interactions (Hormones and Hormone Modulators)
- Increased bleeding risk if used with oral anticoagulants.
-
Cancer Cell-Specific agents
- Effective against specific cancer cells
- Include protein tyrosine kinase inhibitors, EGFR inhibitors and proteasome inhibitors
- Specific targets for the drugs.
- Examples include imatinib, erlotinib, and bortezomib
-
Adverse Effects (Cancer Cell-Specific Agents)
- GI upset, muscle cramps, heart failure, fluid retention, and skin rash.
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