Malaria Drugs - Chapter 52 review
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Malaria Drugs - Chapter 52 review
Antiprotozoal Pharmacology Malaria
Antiprotozoal Drugs review on Chapter 52 Malaria Drugs
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.
•The parasites then enter the blood and parasitize erythrocytes.
What are the names of the "bugs" involved with Malaria infection?
What are the 3 main Malaria drug classifications?
–eliminates dormant or developmental liver forms
-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
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
QUININE - Contraindications?
What is QUININE toxicity known as?
Toxicity is known as
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
Intravascular hemolysis is the cause of blackwater fever.
QUININE - Interactions?
to prolong the prothrombin
–Do not administer concomitantly with
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
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
dark urine (because red blood cell breaking down)
PRIMAQUINE - Interactions
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
and marketed as
Atovaquone - Indications
Indicated for the treatment and
Atovaquone is also approved for the
P. jiroveci pneumonia
Atovaquone - Contraindications
– Allergy to the drug
Atovaquone - Adverse effects
fever, rash, nausea, vomiting, diarrhea, headache, and insomnia.
Atovaquone - Interactions
– coadministration of
will decrease plasma concentrations of atovaquone by 50%.
Name the antimalarial drug that is a
Name the antimalarial drugs that are called
What antimalarial drug is also classified as a
is a tissue schizonticide and also limits malaria transmission by acting as a
What Antifolate drugs inhibit dihydrofolate reductase?
PYRIMETHAMINE - Indications
against erythrocytic forms of susceptible strains of all four human malaria species.
Other anti-malarial agents
due to severity of adverse reactions.
PYRIMETHAMINE - Contraindications
PYRIMETHAMINE - Adverse effects
folic acid deficiency,
PYRIMETHAMINE - Interactions
increase risk of megaloblastic
PROGUANIL - Indications
–Formerly used in
combination with chloroquine
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?
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,
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 (
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
is the standard treatment for uncomplicated falciparum malaria in many areas.
Atremisinin - IV Treatment?
is used for complicated falciparum malaria,
will eventually replace IV quinine as the treatment of choice.
Artemisinins - Adverse effects