Antiprotozoal Agents is a class of pharmaceuticals used in treatment of protozoan infection Brief Introduction: Infections caused by protozoa are very

ry common in several parts of the world. Mostly are those in tropical areas. (e.g. Africa, Asia or South America) It is relatively rare in the United States. They may also survive and reproduce in any area where people live in very crowded and unsanitary conditions. Malaria It is a parasitic disease that has killed hundreds of millions of people and even changed the course of history. The courses of several African battles and the building of the Panama Canal were altered by outbreaks of malaria. It is spread via the bite of an Anopheles mosquito. ANTIMALARIALS DRUGS: Usually given in combination form to attack the plasmodium at various stages of its life cycle. It is possible to prevent the acute malarial reaction in individuals who have been infected by the parasite. Drugs in focus: Quinine (generic) The first drug found to be effective in the treatment of malaria. It may lead to severe diarrhea and a condition called CINCHONISM (nausea, vomiting, tinnitus and vertigo) w/c makes it less desirable than newer, less toxic drugs. It is metabolized in the liver, w/ a half-life of 4 to 5 hours and is excreted in the urine. It is toxic to the fetus and is classified as pregnancy category X. Chloroquine (Aralen) Currently the mainstay of antimalarial therapy. It is directly toxic to parasites that absorb it; it is acidic and it decreases the ability of the parasite to synthesize DNA leading to a blockage of reproduction. It is concentrated in the liver, spleen, kidney and brain and is excreted very slowly in the urine. Use in pregnancy and lactation should be restricted. Adverse Reaction: Hepatic toxicity, Permanent eye damage and Blindness. Hydroxychloroquine (Plaquenil) Inhibits parasite reproduction and by blocking the synthesis of protein production. Absorbed from the GI tract in 1 6 hours. Excreted slowly in the urine.

 Use during pregnancy and lactation should be restricted to situations where benefit clearly outweighs the potential risk to the fetus or neonate. Mefloquine (Lariam) Metabolism occurs in the liver; caution should be used in patients with hepatic dysfunction. Pregnancy should be avoided during and for 2 months after completion of therapy. It is teratogenic in preclinical studies. It is also crosses into breast milk and can be very toxic to the baby. Note: BREASTFEEDING SHOULD BE DISCONTINUED IF THIS DRUG IS ESSENTIAL FOR TREATMENT.

Primaquine (generic) Readily absorbed and metabolized in the liver. Excreted occurs primarily in the urine. Safety for use during pregnancy has not been established. Pyrimethamine (Daraprim) Readily absorbed from the GI tract within 2 6 hours. It is metabolized in the liver and has a half-life of 4 days. Other Protozoal Infections Amebiasis An intestinal caused by Entamoeba histolytica. Transmitted while the protozoan is in the cystic stage in fecal matter from which it can enter water and the ground. Early signs: Mild to Fulminate Diarrhea. Leishmaniasis Disease caused by the protozoan that is passed from the sand flies (promastigote) to human. These can cause serious lesions in the skin, viscera or the mucous membranes of the host. Trypanosomiasis Caused by the infection w/ Trypanosoma. Two parasitic protozoal species cause very serious and often fatal dses in humans: Trichomoniasis Trichomonas vaginalis, common cause of vaginitis. This infection is usually spread during sexual intercourse by men who have no signs and symptoms of infection. In women, this protozoan causes reddened, inflamed vaginal mucosa, itching, burning and yellowish green discharge. African Sleeping Sickness ( transmitted by tsetse fly) Chagas disease

Giardiasis Most commonly diagnosed intestinal parasite in the United states. Pneumocystis carinii Pneumonia (PCP) An endemic protozoan that cause illness in human. When an individuals immune system becomes suppressed, because of acquired AIDs, the use of immunosuppressant drugs, this parasite is able to invade the lungs. Leading to severe inflammation and the condition known as PCP. This dse is the most common opportunistic infection in patients with AIDS. Other Antiprotozoal Agents Atovaquone (Mepron) Active against PCP. It is excreted slowly through the feces w/ a half life of 67 76 hours. Use during pregnancy and lactation should be restricted to situations where benefit clearly outweighs the potential risk to the fetus or neonate. The safety and efficacy of atovaquone in children has not been established. Metronidazole (Flagyl, MetroGel, Noritate) Used to treat amebiasis, trichomoniasis and giardiasis is well absorbed orally reaching peak levels in 1-2 hours. Metabolized in the liver with a half-life of 8-15 hours. Use during pregnancy and lactation should be restricted to situations where benefit clearly outweighs the potential risk to the fetus or neonate. The safety and efficacy in children has not been established. Nitazoxanide (Alinia) Approved in 2005 for the treatment of diarrhea. Rapidly absorbed after oral administration reaching peak levels in 1-4 hours Metabolized in liver and excreted in urine. Pentamidine (NebuPent, Penian 300) Used as an inhalation agent and a systemic agent in the treatment of PCP. Readily absorbed through the lungs

Tinidazole (Tindamax) Approved in 2004 for the treatment of trichomoniasis, giardiasis and amebiasis. It should never be combined with alcohol and should be used cautiously with liver or renal dysfunction. Therapeutic Actions and Indications These antiprotozoal agents act to inhibit DNA synthesis in susceptible protozoa, leading to the inability to reproduce and subsequent cell death. These drugs are indicated for the treatment of infections caused by susceptible protozoa.

Contraindications and Cautions Contraindications: Presence of any known allergy or hypersensitivity to any of these drugs and pregnancy. WHY? Because drug effects on developing fetal DNA and proteins can cause fetal abnormalities and even death. Caution Should be used in the presence of (a)CNS dse., (b)Hepatic dse., (c) Candidiasis and (d)Lactation. WHY? A. Because of possible exacerbation when the drug affects the CNS. B. Because of possible exacerbation when hepatic drug effects occur. C. Because of the risk of super infections. D. Because these drugs may pass into breast milk and could have severe adverse effects on the infant. Adverse Effects

Adverse effects that can be seen with these antiprotozoal agents includes: CNS effects like Headache, Dizziness, Ataxia, Loss of coordination and Peripheral neuropathy. GI effects like Nausea, Vomiting, Diarrhea, Unpleasant taste, Cramps and changes in liver function. Superinfections also can occur when the normal flora is disrupted.