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Primaquine response

MedGen UID:
1002537
Concept ID:
CN322745
Sign or Symptom
Drug:
primaquine
MedGen UID:
994881
Concept ID:
CN315036
Pharmacologic Substance
 
Genes (locations): CYP2D6 (22q13.2); G6PD (Xq28)

Definition

Primaquine is a potent antimalarial medication indicated for the radical cure of malaria caused by Plasmodium vivax (P. vivax) and Plasmodium ovale (P. ovale) species. Malaria is a blood borne infection caused by infection of Plasmodium parasites that is spread by mosquitos. The P. vivax and P. ovale species present a particular challenge to treat because the parasitic life cycle includes a dormant, liver-specific stage that is not susceptible to other antimalarial medications. Thus, primaquine is often used with other therapies such as chloroquine or artemisinin-based medicines that target the reproductive, active forms of the parasite. Primaquine is also used to prevent transmission of malaria caused by Plasmodium falciparum (P. falciparum) species. A single, low dose (SLD) of primaquine has gametocidal activity, which does not cure the individual but does provide malaria transmission control. Primaquine is a pro-drug that must be activated by the cytochrome P450 (CYP) enzyme system. Metabolism by the cytochrome P450 member 2D6 (CYP2D6) and cytochrome P450 nicotinamide adenine dinucleotide phosphate (NADPH):oxidoreductase (CPR) generates 2 hydroxylated active metabolites that generate hydrogen peroxide (H2O2). This causes significant oxidative stress to the malarial parasite and the host human cells. Individuals who are glucose-6-phosphate dehydrogenase (G6PD) deficient are particularly susceptible to oxidative stress and may experience acute hemolytic anemia (AHA). Before starting a course of primaquine, individuals should be tested for G6PD deficiency to ensure safe administration. According to the FDA-approved drug label, individuals with severe G6PD deficiency should not take primaquine. The World Health Organization (WHO) recommends that individuals with G6PD deficiency should be treated with a modified course of primaquine therapy. The recommended course for individuals with G6PD deficiency is a single dose once per week for 8 weeks, while the standard course is daily administration for 14 days. The Clinical Pharmacogenetics Implementation Consortium (CPIC) reports that the risk of adverse effects of primaquine therapy for G6PD-deficient individuals is dose-dependent, with the SLD regimen presenting the least risk. Primaquine is contraindicated during pregnancy and is not recommended for breastfeeding individuals when the G6PD status of the baby is unknown. Primaquine is not approved for individuals under 6 months of age. Individuals with acute illness that are prone to granulocytopenia or individuals taking another hemolytic medication are also contraindicated from taking primaquine. [from Medical Genetics Summaries]

Professional guidelines

PubMed

Hanboonkunupakarn B, White NJ
Br J Clin Pharmacol 2022 Feb;88(2):374-382. Epub 2020 Aug 1 doi: 10.1111/bcp.14474. PMID: 32656850Free PMC Article
Weyant RB, Kabbani D, Doucette K, Lau C, Cervera C
Expert Opin Pharmacother 2021 Aug;22(12):1579-1592. Epub 2021 Apr 19 doi: 10.1080/14656566.2021.1915989. PMID: 33870843
Ashley EA, Poespoprodjo JR
Lancet Child Adolesc Health 2020 Oct;4(10):775-789. doi: 10.1016/S2352-4642(20)30127-9. PMID: 32946831

Curated

Gammal et al, Expanded Clinical Pharmacogenetics Implementation Consortium Guideline for Medication Use in the Context of G6PD Genotype. 2 Sept 2022. Clin Pharmacol Ther.

DailyMed Drug Label, PRIMAQUINE PHOSPHATE tablet, film coated, 2021

Therapeutic recommendations

From Medical Genetics Summaries

This section contains excerpted 1 information on gene-based dosing recommendations. Neither this section nor other parts of this review contain the complete recommendations from the sources.

2021 Statement from the US Food and Drug Administration (FDA):

Due to the risk of hemolytic anemia in patients with G6PD deficiency, G6PD testing has to be performed before using primaquine. Due to the limitations of G6PD tests, physicians need to be aware of residual risk of hemolysis and adequate medical support and follow-up to manage hemolytic risk should be available.

Primaquine should not be prescribed for patients with severe G6PD deficiency…

In case of mild to moderate G6PD deficiency, a decision to prescribe primaquine must be based on an assessment of the risks and benefits of using primaquine. If primaquine administration is considered, baseline hematocrit and hemoglobin must be checked before treatment and close hematological monitoring (e.g. at day 3 and 8) is required. Adequate medical support to manage hemolytic risk should be available.

When the G6PD status is unknown and G6PD testing is not available, a decision to prescribe primaquine must be based on an assessment of the risks and benefits of using primaquine. Risk factors for G6PD deficiency or favism must be assessed. Baseline hematocrit and hemoglobin must be checked before treatment and close hematological monitoring (e.g. at day 3 and 8) is required. Adequate medical support to manage hemolytic risk should be available.

Please review the complete therapeutic recommendations that are located here: (1).

2022 Statement from the Clinical Pharmacogenetics Implementation Consortium (CPIC)

It is recommended to avoid primaquine at standard (or higher) anti-relapse dosages of 0.25–0.5 mg/kg daily for 14 days for the treatment of P. vivax or P. ovale in G6PD deficiency. For the anti-gametocyte treatment of Plasmodium falciparum malaria, the single-dose regimen of 0.25 mg/kg is considered safe and effective (low to no risk in G6PD deficiency). For the treatment of P. vivax or P. ovale malaria for radical cure of liver-stage infections, 0.75 mg/kg once weekly for 8 weeks (WHO) or 45 mg for adults once weekly for 8 weeks (CDC) is considered in the medium risk category, and patients should be monitored closely for hemolysis… No dose of primaquine is considered safe in patients who are G6PD deficient with CNSHA and thus should be avoided.

Please review the complete therapeutic recommendations that are located here: (3).

2020 Statement from Health Canada:

Hemolytic anemia and G6PD deficiency

Due to the risk of hemolytic anemia in G6PD deficient patients, G6PD testing has to be performed before using primaquine. […] Due to the limitations of G6PD tests, physicians need to be aware of residual risk of hemolysis and adequate medical support and follow-up to manage hemolytic risk should be available. Observe particular caution in individuals with a personal or family history of hemolytic anemia.

In case of mild to moderate G6PD deficiency, a decision to prescribe primaquine must be based on an assessment of the risks and benefits of using primaquine; if primaquine administration is considered, the dosage regimen should be adapted accordingly (see DOSAGE AND ADMINISTRATION) and close hematological monitoring is required.

[….]

CYP2D6 genotype:

Based on non-clinical data, primaquine activity probably depends on the formation CYP2D6 metabolite(s). Therefore, CYP2D6 polymorphism may be associated with variability in clinical response to primaquine.

Limited clinical data reported more elevated treatment failure rates in patients with CYP2D6 poor or intermediate metabolizer status than in patients with normal/extensive metabolizer status (see ACTION AND CLINICAL PHARMACOLOGY).

In case of treatment failure, after checking patient’s compliance to treatment, it may be useful to reconsider potential concomitant use of CYP2D6 inhibitors (see DRUG INTERACTIONS) and to assess the patient’s CYP2D6 status if feasible. For poor CYP2D6 metabolizers, alternative treatment should be considered.

Please review the complete therapeutic recommendations that are located here: (5).

1 The FDA labels specific drug formulations. We have substituted the generic names for any drug labels in this excerpt. The FDA may not have labeled all formulations containing the generic drug. Certain terms, genes and genetic variants may be corrected in accordance with nomenclature standards, where necessary. We have given the full name of abbreviations, shown in square brackets, where necessary.

Supplemental Content

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    Clinical resources

    Practice guidelines

    • PubMed
      See practice and clinical guidelines in PubMed. The search results may include broader topics and may not capture all published guidelines. See the FAQ for details.

    Curated

    • CPIC, 2022
      Gammal et al, Expanded Clinical Pharmacogenetics Implementation Consortium Guideline for Medication Use in the Context of G6PD Genotype. 2 Sept 2022. Clin Pharmacol Ther.
    • DailyMed Drug Label, 2021
      DailyMed Drug Label, PRIMAQUINE PHOSPHATE tablet, film coated, 2021

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