Antimalarial Drugs

ANTIMALARIAL DRUGS

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·       Malaria is a life-threatening disease caused by Plasmodium parasites, transmitted to humans through the bites of infected Anopheles mosquitoes.

·       Antimalarial drugs are used to prevent and treat malaria.

Definition

·       Antimalarial drugs are medications used to prevent or cure malaria by inhibiting the growth and reproduction of Plasmodium parasites within the human body.

Classification

1.     Aminoquinolines

o   Chloroquine: Used for the treatment of non-resistant malaria.

o   Hydroxychloroquine: Similar to chloroquine, also used in autoimmune diseases.

2.     Artemisinin Derivatives

o   Artemether: Often combined with lumefantrine.

o   Artesunate: Used for severe malaria.

3.     Quinoline Methanols

o   Quinine: Used for chloroquine-resistant strains.

o   Mefloquine: Used for prophylaxis and treatment of drug-resistant malaria.

4.     Antifolates

o   Pyrimethamine: Often combined with sulfadoxine.

o   Proguanil: Often combined with atovaquone.

5.     Naphthoquinones

o   Atovaquone: Usually combined with proguanil.

6.     Antibiotics

o   Doxycycline: Used in combination therapy.

o   Clindamycin: Used as an alternative in certain cases.

Pharmacokinetics

·        Absorption: Rapidly absorbed from the gastrointestinal tract.

·        Distribution: Widely distributed, especially in the liver, spleen, kidneys, and lungs.

·        Metabolism: Metabolized in the liver.

·        Excretion: Primarily excreted in the urine.

Mechanism of Action

  1. Aminoquinolines:

    Prevent detoxification of heme by blocking hemozoin formation. This leads to accumulation of toxic heme in Plasmodium.

  2. Artemisinin Derivatives:

    Activated by heme to generate free radicals inside the parasite. These radicals damage parasite proteins and membranes, causing rapid death.

  3. Quinoline Methanols:

    Inhibit heme polymerization in Plasmodium's food vacuole, causing toxic heme buildup. This leads to oxidative damage and parasite death.

  4. Antifolates:
    Block folate synthesis and prevents DNA replication in the malaria parasite.

  5. Naphthoquinones:
    Inhibit mitochondrial electron transport in Plasmodium. This disrupts ATP production and causes parasite death.

  6. AntibioticsTarget the apicoplast and inhibit protein synthesis in the parasite. They act slowly and are used for malaria prophylaxis or combination therapy.

Uses

·        Prevention: Medications like chloroquine and doxycycline are used for prophylaxis in malaria-endemic areas.

· Treatment: Drugs like artemether-lumefantrine and quinine are used for treating active malaria infections.

·    Severe Cases: Intravenous artesunate is used for severe malaria.

Adverse Effects

·        Nausea and vomiting

·        Dizziness

·        Visual disturbances

·        Gastrointestinal disturbances

·        Headache

·        Rash

Contraindications

·        Known hypersensitivity to chloroquine

·        Retinal or visual field changes

·        Psoriasis

·  Hypersensitivity to artemether or other artemisinin derivatives

Role of Nurse

1.     Assessment

o   Obtain a thorough medical history including drug allergies and current medications.

o   Assess for signs and symptoms of malaria.

2.     Administration

o   Administer antimalarial drugs as prescribed.

o   Monitor for adverse effects during and after administration.

3.     Patient Education

o   Educate patients on the importance of medication adherence.

o   Inform about potential side effects and when to seek medical attention.

o   Advise on preventive measures such as mosquito nets and repellents.

4.     Monitoring

o   Monitor vital signs and symptoms to assess the effectiveness of the medication.

o   Conduct regular blood tests to monitor for potential side effects, such as liver function tests and complete blood counts.

5.     Documentation

o   Document the patient’s response to the medication.

o   Record any adverse effects and actions taken.

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