Antimalarials/Protozoals Flashcards
Most lethal and resistant protozoa
P. falciparum
Have dormant liver stages (hypnozoites) (2)
- P. vivax
- P. ovale
Rare protozoa
P. malariae
- Act on ERYTHROCYTIC forms of the parasite
- Do NOT affect secondary tissue forms of Ovale and Vivax
Blood schizonticides
- Eliminate proliferation
- Act on GAMETOCYTES
- Do NOT help individuals suffering from malaria, but may help SLOW SPREAD
Gametocidal agents
- Act on HEPATIC stages
- Do NOT suppress symptoms one erythrocytic stages have been established
- Kill secondary tissue forms of Ovale and Vivax
- Can prevent prophylaxis but are too toxic
Tissue schizonticides
Provide “RADICAL CURE”
Tissue schizonticides
Can be used to suppress symptoms –> “CLINICAL CURE”
Blood schizonticides
Most effective means of controlling malaria
- Avoid being bitten
- Eradicate mosquitoes and habitates
- Insect repellent
- Mosquito netting, tents with permethrin
Drug effective against gametocytic and exoerythrocytic (tissue) formation
Primaquine
Drugs effective against erythrocytic form, from illustration (5)
- Artemisinin
- Chloroquine
- Quinine
- Mefloquine
- Pyrimethamine
DOC for Malaria (2)
- Chloroquine
- Hydroxychloroquine
Blood schizonticides
- Chloroquine
- Hydroxychloroquine
- Mefloquine
- Quinine sulfate and quinidine gluconate
- Doxycycline or Clindamycin
- Atovaquone + Proquanil
DOC and prophylaxis for sensitive organisms
Chloroquine
- Prophylaxis due to long duration of action (take once weekly)
What form is resistant to Chloroquine and why?
- P. falciparum
- TRANSPORT PUMP removes drug from parasite
Chloroquine MOA (2)
- Actively concentrated within plasmodia that reside in RBC
- May interfere with lysosomal degradation of Hgb
Chloroquine Admin
- Oral
- Parenteral (slow)
Chloroquine accumulates where? (2)
- Skin
- Retina
Chloroquine SE (6)
- CNS (dizziness, HA, tinnitus)
- Retinal and corneal tox
- Ototoxicity
- Rash, pruritis
- HEMOLYSIS - G6PD (use caution, but not absolute CI)
- INCREASED RISK FOR QT prolongation (torsades)
Chloroquine CI (2)
- Psoriasis
- Porphyria
First line drug for tx and prophylaxis of chloroquine resistant strains?
Mefloquine
Mefloquine Admin
Oral as single mega dose
Mefloquine Features -
- Distributed to blood, urine, CSF, tissues and concentrated in RBC
- Metabolized by liver
- Eliminated very slowly
Mefloquine SE
- SEIZURES AND PSYCHOSIS aggravation
- Potential CARDIAC TOX (do NOT combine with quinine)
Mefloquine CI
- In pts with any neuropsych problems
Quinine Admin and t 1/2
Oral, 5 - 16 hrs
DOC for complicated, chloroquine resistant plasmodia
Quinine and Quinidine Glyconate
- Combined with Doxycycline or Clindamycin (if
Quinidine Glyconate Admin
IV
Other actions of Quinine and Quinidine Glyconate
- Analgesia
- Antipyretic
Which drug has a narrow margin between an effective dose and toxic dose?
Quinine
Quinine and Quinidine Glyconate SE
- CINCHONISM (tinnitus, HA, dizziness, flushing, visual disturbances)
- ANTIARRYTHMIC agent (Quinidine)
- QT ELONGATION (do not combine with mefloquine)
- HEMOLYSIS in G6PD
- Stimulates insulin (caution in hypoglycemia)