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. Antibiotics: Target 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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