Anti-Protazoals

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A. Paromomycin (Humatin)
B. Iodoquinol (Yodoxin)
C. Nitazoxanide (Crytaz)
D. Chloroquine (Aralen)
E. Metronidazole (Flagyl)
F. Tinadazole (Tindamax)
G. Pyrimethamine (Daraprim) + Sulfadiazine (generic)

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Antiprotozoal Drugs

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A. Mebendazole (Vermox)
B. Thiobendazole (Mintezol)
C. Pyrantel (Pin-Rid)
D. Ivermectin (Stromectol)
E. Praziquantel (Biltricide)
F. Albendazole (Albenza)

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Anthelmintic Drugs:

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A. Chloroquine (Aralen)
B. Quinine (generic)
C. Mefloquine (Larium)
D. Primaquine (generic)
E. Pyrimethamine (Daraprim)
Pyrimethamine + Sulfadoxine (Fansidar)
F. Atovaquone + Proquanil (Malarone)
G. Doxycycline (generic. Vibramycin)

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Antimalarial Drugs:

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Used to treat enteric parasites; poorly absorbed from the GI tract & side- effects limited to GI upsets & diarrhea.

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Luminal Amebicides

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Paromomycin (Humatin) & Iodoquinol (Yodoxin) are _______________________

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Luminal Amebicides

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An amino- glycoside antibiotic effective vs amoeba & bacteria; unknown MOA.

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Paromomycin (Humatin)

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Only for invasive forms of Entamoeba that cause amebic dysentery.

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Systemic Amebicides

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Chloroquine (Aralen) is a

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Systemic Amebicide

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This drug acts by concentrating in parasite food vacuole, ↓ polymerization of heme, the breakdown product of hemoglobin, into hemozoin. Heme is higly reactive & causes oxidative damage to the parasite.***

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Chloroquine (Aralen):

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This drug is used for Amebic dysentery & liver abscess
Used with a luminal amebicide to prevent relapse.

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Chloroquine

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Adverse reactions of this drug in high doeses include hypotension, EKG changes; confusion, psychosis, seizures, Ototoxicity, retinopathy

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Chloroquine

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these drugs are Effective vs enteric & systemic form of the disease

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Mixed Amebicides

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The prototype Mixed Amebicide is

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Metronidazole (Flagyl)

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This drug is selective vs anaerobic organisms e.g. Trichomoniasis vaginalis, E. histolytica & G. Lambli

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Metronidazole (Flagyl)

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MOA of Metronidazole (Flagyl) is this?

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it is reduced to a highly reactive free radical which denatures DNA

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This is the DOC for amebic dysentery it is usually given w/ a luminal amebicide to ↑ activity.

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Metronidazole (Flagyl)

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Side effects of this drug include Nausea, dry mouth, metallic taste. Disulfuram-Like Reaction with alcohol vasodilation, severe headache, profuse sweating

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Metronidazole (Flagyl)

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DOC of Giardiasis

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Metronidazole (Flagyl)

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Drug of choice for Trichomoniasis

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metronidazole (Flagyl)

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A nitroimidazole effective for amebiasis, giardiasis & trichomoniasis.
MOA: Acts by forming free radicals and denatures DNA.

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Tinadazole (Tindamax)

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Effective for toxoplasmic encephalitis in AIDS.

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Pyrimethamine (Daraprim) + Sulfadiazine(generic)

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MOA: Acts synergistically to inhibit two sequential steps in synthesis of folic acid which is required for DNA synthesis

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Pyrimethamine (Daraprim) + Sulfadiazine(generic)

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Used to treat roundworms, esp. pinworms.

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Mebendazole (Vermox)

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MOA: ↓↓ polymerization of tubulin & synthesis of microtubules ↓↓ glucose uptake & oxidative phosphorylation

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Mebendazole (Vermox)

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Minimally absorbed; rapidly metabolized.
May cause abdominal pain, V, D.

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Mebendazole (Vermox)

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For various roundworms & pinworms.

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Pyrantel (Pin-Rid):

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MOA: A depolarizing neuromuscular blocker→ muscle paralysis of worms→ detachment & expulsion
↓↓ AChE → ↑ spastic paralysis

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Pyrantel (Pin-Rid):

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This roundworm & Pinworm treatment may have side effects of, NVD, abdominal cramps, headache, dizziness & rash.

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Pyrantel (Pin-Rid)

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Rx of choice for strongyloidiasis (threadworm). It is most common among kids in rural south & in institutionalized pts in unsanitary conditions. Also for Onchocerciasis (river blindness)

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Ivermectin (Stromectol)

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MOA: Activates glutamate-gated Cl– channels → hyperpolarization & paralysis of the nematode’s muscle → death & expulsion. This type of Cl – Channels is found only in invertebrates. Cestodes (tapeworms) do NOT have R for this Rx.

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Ivermectin (Stromectol)

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Adverse reactions:
Mazotti Reaction: fever, dizziness, rash, D, weakness, pruritis, joint & muscle pain, hypotension, tachycardia & edema.
- Occurs in 5-30% of patients; generally mild, well-tolerated & of short duration.
- NSAIDs & steroids relieve symptoms of the reaction.

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Ivermectin (Stromectol)

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Rx of choice for schistosomiasis (blood flukes), which is generally carried to the U.S. from S. America, Caribbean, China or Philippines. also effective for intestinal cestode

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Praziquantel (Biltricide)

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MOA: ↑ worm’s cell membrane
permeability to CA 2+ → ↑ Ca 2+ → spastic paralysis & detachment

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Praziquantel (Biltricide)

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Common side effects of this Rx for schistosomiasis is Malaise, anorexia NV, headache, drowsiness, dizziness.

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Praziquantel (Biltricide):

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Indicated for pork tapeworms and cestodal infx., e.g. neurocysticercosis , hydatid disease

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Albendazole (Albenza):

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MOA: ↓↓ polymerization of tubulin

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Albendazole (Albenza)

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this drug indicated for pork tapeworms and cestodal infx May cause epigastric distress, NVD, headache, dizziness, insomnia

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Albendazole (Albenza)

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A blood schizontocide effective vs all forms of malaria except the exoerythrocytic tissue stages of plasmodium

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Chloroquine (Aralen):

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MOA: Prevents polymerization of heme → oxidative damage

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Chloroquine (Aralen)

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High doses of this anti-malarial can cause hypotension, confusion, psychosis, ototoxicity, retinopathy

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Chloroquine (Aralen)

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High doses of this anti-malarial can cause hypotension, confusion, psychosis, ototoxicity, retinopathy

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Chloroquine (Aralen)

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Resistence to Chloroquine (Aralen) is common, if suspected, use ________ b/c falciparum can be fatal

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Mefloquine

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this drug is also used for rheumatoid arthritis (anti-inflammatory activity)

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Chloroquine (Aralen)

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A cinchona alkaloid from the bark of the S. American cinchona tree & is the stereoisomer of quinidine. It is more toxic & less effective than chloroquine.

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Quinine (generic)

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MOA: Same as chloroquine

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Quinine (generic)

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Uses: A blood schizontocide for acute attack -- not prophylaxis.

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Quinine (generic)

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Side effects of this antimalarial includes:

Cinchonism:
Mild: Tinnitus, headache, NVD, blurred, vision, rash, urticaria
Severe (rare): Widen QRS complex, AV block, V-tachycardia
2) Hyperinsulinemia → hypoglycemia (common) – moniter sugar

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Quinine

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A blood schizontocide reserved for chlorquine & multi-Rx resistant strains of P. falciparum

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Mefloquine (Larium)

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MOA: Same as chloroquine
B. Side effects:
Mild: NVD, headache, dizziness, rash
Serious: Depression, psychosis, seizure

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Mefloquine (Larium)

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Caution: Can exacerbate epilepsy & psychiatric disorders → convulsions, anxiety, paranoid, depression. Suicide Warning !!

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Mefloquine (Larium)

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A blood & tissue schizontocide that is also effective vs P. vivax & P. ovale. It can prevent relapse from these organisms but is ineffective vs erythrocytic stages of P. falciparum

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Primaquine (generic):

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MOA: Unknown
B. Adverse reactions of this antimalarial include:
1) Nausea, epigastric pain, cramps.
2) Methemoglobinemia → cyanosis

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Primaquine (generic)

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TEST patients for G6PD levels before using this Rx. Patients with ↓ G6PD → acute hemolysis & hemolytic anemia. African-Americans are at greater risk.

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Primaquine

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MOA is that it ↓↓ DHF Reductase
B. Generally used with a sulfonamide for sequential block of folic acid synthesis → ↓ Resistence

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Pyrimethamine (Daraprim)

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This drug is pyrimethamine + sulfadoxine, a long acting sulfonamide used for acute attack.

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Fansidar

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MOA of sulfadoxine

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↓↓ Dihydropteridine synthase

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SE of this antimalarial Rx are mostly due to the sulfa. They include--SLE, Steven-Johnson syndrome, serum sickness, hepatitis

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sulfadoxine

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For prophylaxis & acute attacks, including chloroquine-resistant strains of P. falciparum

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Atovaquone + Proguanil (Malarone)

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This drug acts to disrupt mitochondrial electron transport

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Atovaquone

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MOA:
a. Metabolite (cycloguanil) inhibits bifunctional DHFR-thymidylate synthetase
b. Parent Rx ↑ atovaquone effect

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Proquanil

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This antimalarial combination is generally well-tolerated.
Side effects include abdominal pain, NVD, headache
Reversible ↑ liver enzyme

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Atovaquone + Proguanil (Malarone):