Halofantrine: Difference between revisions
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'''Halofantrine''' is | {{Short description|Antimalarial medication}} | ||
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'''Halofantrine''' is an [[antimalarial drug]] used for the treatment of [[malaria]], a disease caused by [[Plasmodium]] parasites. It is particularly effective against the [[Plasmodium falciparum]] species, which is responsible for the most severe forms of malaria. Halofantrine is known for its ability to clear [[parasitemia]] rapidly, but its use is limited due to concerns about [[cardiotoxicity]] and [[drug interactions]]. | |||
==Pharmacology== | ==Pharmacology== | ||
Halofantrine works by inhibiting the | Halofantrine is a member of the [[phenanthrene methanol]] class of antimalarial drugs. It works by interfering with the parasite's ability to digest [[hemoglobin]], which is essential for its survival within the [[red blood cells]] of the host. The drug is administered orally and is absorbed in the [[gastrointestinal tract]]. | ||
===Mechanism of Action=== | |||
Halofantrine acts by inhibiting the polymerization of [[heme]] into [[hemozoin]], a process that is crucial for the detoxification of free heme, which is toxic to the parasite. By preventing this polymerization, halofantrine causes an accumulation of toxic heme, leading to the death of the parasite. | |||
===Pharmacokinetics=== | |||
The absorption of halofantrine is highly variable and is significantly increased when taken with food, particularly fatty meals. This can lead to unpredictable plasma concentrations and potential toxicity. The drug is metabolized in the [[liver]] by the [[cytochrome P450]] enzyme system, primarily CYP3A4, and is excreted in the [[bile]] and [[urine]]. | |||
== | ==Clinical Use== | ||
Halofantrine is used primarily in the treatment of uncomplicated malaria caused by [[Plasmodium falciparum]]. It is often reserved for cases where other antimalarial drugs, such as [[chloroquine]] or [[mefloquine]], are ineffective due to resistance. | |||
==Dosage== | ===Dosage and Administration=== | ||
The | The typical dosage regimen involves administering halofantrine in three doses, each six hours apart. This schedule is designed to maximize the drug's efficacy while minimizing the risk of adverse effects. | ||
== | ==Adverse Effects== | ||
The most significant adverse effect associated with halofantrine is its potential to cause [[cardiac arrhythmias]], particularly [[QT interval prolongation]]. This can lead to serious complications such as [[torsades de pointes]] and [[sudden cardiac death]]. Other side effects may include [[gastrointestinal disturbances]], [[headache]], and [[dizziness]]. | |||
==Interactions== | ==Drug Interactions== | ||
Halofantrine | Halofantrine should not be co-administered with other drugs that prolong the QT interval or with drugs that inhibit CYP3A4, as these interactions can increase the risk of cardiotoxicity. Patients should be monitored closely for any signs of cardiac dysfunction. | ||
== | ==Related Pages== | ||
* [[Malaria]] | * [[Malaria]] | ||
* [[Antimalarial medication]] | * [[Antimalarial medication]] | ||
* [[Plasmodium falciparum]] | * [[Plasmodium falciparum]] | ||
* [[Cardiotoxicity]] | |||
[[Category: | [[Category:Antimalarial agents]] | ||
[[Category: | [[Category:Phenanthrenes]] | ||
[[Category: | [[Category:Cardiotoxicants]] | ||
Latest revision as of 10:59, 23 March 2025
Antimalarial medication
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Halofantrine is an antimalarial drug used for the treatment of malaria, a disease caused by Plasmodium parasites. It is particularly effective against the Plasmodium falciparum species, which is responsible for the most severe forms of malaria. Halofantrine is known for its ability to clear parasitemia rapidly, but its use is limited due to concerns about cardiotoxicity and drug interactions.
Pharmacology[edit]
Halofantrine is a member of the phenanthrene methanol class of antimalarial drugs. It works by interfering with the parasite's ability to digest hemoglobin, which is essential for its survival within the red blood cells of the host. The drug is administered orally and is absorbed in the gastrointestinal tract.
Mechanism of Action[edit]
Halofantrine acts by inhibiting the polymerization of heme into hemozoin, a process that is crucial for the detoxification of free heme, which is toxic to the parasite. By preventing this polymerization, halofantrine causes an accumulation of toxic heme, leading to the death of the parasite.
Pharmacokinetics[edit]
The absorption of halofantrine is highly variable and is significantly increased when taken with food, particularly fatty meals. This can lead to unpredictable plasma concentrations and potential toxicity. The drug is metabolized in the liver by the cytochrome P450 enzyme system, primarily CYP3A4, and is excreted in the bile and urine.
Clinical Use[edit]
Halofantrine is used primarily in the treatment of uncomplicated malaria caused by Plasmodium falciparum. It is often reserved for cases where other antimalarial drugs, such as chloroquine or mefloquine, are ineffective due to resistance.
Dosage and Administration[edit]
The typical dosage regimen involves administering halofantrine in three doses, each six hours apart. This schedule is designed to maximize the drug's efficacy while minimizing the risk of adverse effects.
Adverse Effects[edit]
The most significant adverse effect associated with halofantrine is its potential to cause cardiac arrhythmias, particularly QT interval prolongation. This can lead to serious complications such as torsades de pointes and sudden cardiac death. Other side effects may include gastrointestinal disturbances, headache, and dizziness.
Drug Interactions[edit]
Halofantrine should not be co-administered with other drugs that prolong the QT interval or with drugs that inhibit CYP3A4, as these interactions can increase the risk of cardiotoxicity. Patients should be monitored closely for any signs of cardiac dysfunction.
