Malaria Drugs - Chapter 52 review
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Malaria method of transmission?
- Contracted after inoculation of
- plasmodium parasites into the blood stream by the bite of a female Anopheles
What are the two phases of Malaria infection?
- Primary Tissue phase
- •The parasites first undergo a primary
- developmental stage in the liver.
- Erythrocytic phase
- •The parasites then enter the blood and parasitize erythrocytes.
What are the names of the "bugs" involved with Malaria infection?
- P. falciparum
- P. malariae
- P. vivax
What are the 3 main Malaria drug classifications?
- Tissue schizonticide
- –eliminates dormant or developmental liver forms
- Blood schizonticide
- -eliminates blood parasites
- –kill sexual stages and
- prevents transmission to mosquitoes
Prevents polymerization of heme.
- –Intracellular accumulation of heme is
- toxic to the parasite.
What is the DOC for acute attacks of non-falciparum and sensitive falciparum malaria.
CHLOROQUINE - the drug of choice for what?
- acute attacks of non-falciparum and sensitive falciparum malaria.
- - prophylaxis of malaria caused by
- P. vivax, P. ovale, P. malariae,
- and susceptible strains of P. falciparum.
CHLOROQUINE - Toxicity
- –GI irritation, rash, headache, peripheral
- neuropathy, auditory impairment, toxic psychosis, and precipitation of porphyria attacks, retinal damage, hemolysis in G6PD deficiency
CHLOROQUINE - Interactions?
–When combined with mefloquine will increase the risk of seizures and ECG abnormalities.
CHLOROQUINE - Side Effects
- Hair bleaching with over-exposure to drug.
QUININE - MOA
From the bark of the cinchona tree...
- –Complexes with double-stranded DNA to
- prevent strand separation.
–Solely a blood schizonticide.
QUININE - Indications?
- –Used in the treatment of chloroquine-resistant
- falciparum malaria.
QUININE - Contraindications?
- in pregnancy
- –(Category X)
What is QUININE toxicity known as?
Toxicity is known as cinchonism.
What are the symptoms of QUININE cinchonism?
- GI distress, headache, vertigo, blurred
- vision, and tinnitus.
What is the drug classification for QUININE?
–eliminates blood parasites
QUININE - Side Effects
May cause hemolysis in G6PD deficient individuals.
What drug causes blackwater fever?
Intravascular hemolysis is the cause of blackwater fever.
QUININE - Interactions?
- –With coumadin to prolong the prothrombin
–Do not administer concomitantly with mefloquine
due to increased risk of cardiac arrest and seizures.
Related to quinine.
–Used for prophylaxis in all malarious areas except those resistant to chloroquine
MEFLOQUINE (LARIAM) - Indications
- Used to treat acute malaria caused
- by P. falciparum and P. vivax.
- **Does not eliminate the liver phase of
- P. vivax
MEFLOQUINE (LARIAM) - Contraindications
Contraindicated in patients with a history of psychiatric disease, and/or seizures.
MEFLOQUINE (LARIAM) - Interactions
Other quinine-like drugs can cause prolongation of the QT interval, and can cause seizures
MEFLOQUINE (LARIAM) - Adverse Effects
PRIMAQUINE - Classification
Also limits malaria transmission by acting as a gametocide.
PRIMAQUINE - Indications
- Used to eradicate the liver stage of
- P. ovale and P. vivax.
*Used in conjunction with a blood schizonticide.
PRIMAQUINE - MOA
Mechanism of action
–forms metabolites that are cellular oxidants.
PRIMAQUINE - Contraindications
PRIMAQUINE - Adverse Effects
- hemolytic anemia,
- cardiac arrhythmias,
- dark urine (because red blood cell breaking down)
PRIMAQUINE - Interactions
quinacrine decreases the metabolism of primaquine
Atovaquone - MOA
disrupts mitochondrial electron transport in plasmodia.
The ultimate metabolic effects of such blockade may include inhibition of nucleic acid and ATP synthesis
What is the name of the drug its used in fixed combination with, and what is the brand name of this combination?
Combined in a fixed combination with proguanil and marketed as Malarone.
Atovaquone - Indications
- Indicated for the treatment and
- chemoprophylaxis of falciparum malaria.
- Atovaquone is also approved for the
- treatment of P. jiroveci pneumonia.
Atovaquone - Contraindications
– Allergy to the drug
Atovaquone - Adverse effects
fever, rash, nausea, vomiting, diarrhea, headache, and insomnia.
Atovaquone - Interactions
– coadministration of rifampin, or tetracycline will decrease plasma concentrations of atovaquone by 50%.
Name the antimalarial drug that is a
Name the antimalarial drugs that are called
- MEFLOQUINE (LARIAM)
What antimalarial drug is also classified as a
is a tissue schizonticide and also limits malaria transmission by acting as a gametocide.
What Antifolate drugs inhibit dihydrofolate reductase?
PYRIMETHAMINE - Indications
–Acts slowly against erythrocytic forms of susceptible strains of all four human malaria species.
–Other anti-malarial agents are usually preferred due to severity of adverse reactions.
PYRIMETHAMINE - Contraindications
PYRIMETHAMINE - Adverse effects
- folic acid deficiency,
- GI distress
PYRIMETHAMINE - Interactions
- sulfonamides increase risk of megaloblastic
PROGUANIL - Indications
–Formerly used in combination with chloroquine for prophylaxis of malaria in the parts of Africa without widespread chloroquine resistance.
PROGUANIL - Contraindications
PROGUANIL - Adverse effects
–Megaloblastic anemia in patients with renal failure, mouth ulcers and alopecia
–Safe to use in pregnancy.
PROGUANIL - Interactions
–Oral contraceptive use prolongs the half-life of proguanil
FANSIDAR - MOA
Mechanics of action
–Sequential blockade of folate synthesis
What are the drug combinations used to make up the drug FANSIDAR?
- Combination of pyrimethamine
- and sulfadoxine
FANSIDAR - Indications
Intermittent preventative therapy in pregnant women and young children.
FANSIDAR - Adverse effects
- Stevens-Johnson syndrome (SJS),
- Toxic epidermal necrolysis (TENs)
FANSIDAR - Contraindications
- Hypersensitivity to the drug,
- sulfa allergy,
Halofantrine - Indication
- Effective against erythrocytic stages of all four types of malaria
- Not used for chemoprophylaxis
Halofantrine - Side effects
- Alters cardiac conduction,
- dose related prolongation of QT interval
Halofantrine - Contraindication
Contraindicated in pregnancy
available as a fixed dose combination
with what other drug? Brand name?
with artemether (Coartem)
Lumefantrine - Used to treat?
uncomplicated falciparum malaria,
Minimal cardiac toxicity
Artemisinins - MOA
Mech of action
- production of free radicals
- or inhibition of parasite calcium ATPase
Medication fun fact...
Used in China for over 2000 years
Atremisinin - Treatment
- combination therapy,
- is the standard treatment for uncomplicated falciparum malaria in many areas.
Atremisinin - IV Treatment?
- IV artesunate,
- is used for complicated falciparum malaria,
- will eventually replace IV quinine as the treatment of choice.
Artemisinins - Adverse effects
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