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MALARIA DISEASE AND CHLOROQUINE DRUG

Presented By:

Date:

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Introduction

Malaria is a serious disease caused by plasmodium (parasite).
Female anopheles mosquito spreads the parasite thro’ bite (Daily et al., 2022).
Malaria is common in tropical regions especially in Sub-Sahara Africa.
If not treated quickly, causes death mainly among the children (Daily et al., 2022).
Symptoms: fever, headache, muscle ache, fatigue, nausea, vomiting and diarrhea.
Treated using Chloroquine and other approved anti-bacterial drugs.

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Disease Process

Malaria is transmitted by the female anopheles mosquito and caused by the plasmodium (parasitic bacteria).

Plasmodium’s life cycle involves two different hosts, humans and mosquito (Daily et al., 2022).

When the mosquito bites the first infected person, the malaria parasites move into its bloodstream and it serves as a temporary host. When the infected mosquito bites the uninfected individual, the malaria parasites move from the mosquito into the bloodstream of the uninfected person (Daily et al., 2022).

The second person hosts the malaria parasites which moves to the liver and other body tissues.

While in the body of the second host, the parasites enter the leucocytes (red blood cells) where they rapidly reproduce resulting to rupture of the cell. As the cell ruptures, the young parasites remain suspended in the blood flowing around the body (Daily et al., 2022).

When the mosquito bites again the infected person and moves to bite another uninfected person, malaria spreads in the society.

Failure to address it in time is fatal, and is associated with the massive death of children in Africa. The cycle repeats itself as demonstrated on the image.

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Drug Class

Selected drug class: Chloroquine phosphate.
Used to prevent and treat malaria.
Also used to treat protozoa-infected liver infections.
Therefore classified under antimalarials and amebicides.
Was used to treat COVID-19 in some patients.
Applied differently based on age, purpose and severity of disease.
Not recommended for expectant women.

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Pharmacokinetics

Chloroquine is quickly absorbed after administration.
Dealkylated via cytochrome P450 enzymes (CYP) into pharmacologically active desethylchloroquine and bisdesethylchloroquine (Abd‐Rahman et al., 2020).
Peak plasma concentration - 2-5 hours; 60% bound to plasma proteins.
Concentrated most in liver, spleen, kidney, lungs and leucocytes (red blood cells) (Abd‐Rahman et al., 2020).
Selective accumulation occurs in retina; ocular toxicity.
T1/2 life = 3-10 days and increases to 20-60 days.
Parent drug and metabolites are excreted via urine.
Small amount persist in urine months after discontinuation.

Chloroquine is quickly absorbed into the body after oral administration.

It’s dealkylated via cytochrome P450 enzymes (CYP) into pharmacologically active desethylchloroquine and bisdesethylchloroquine for metabolic action (Abd‐Rahman et al., 2020).

The peak plasma concentration occurs in 2-5 hours, with 60 percent bound to plasma proteins.

The drug is concentrated in liver, spleen, kidney, lungs and leucocytes (red blood cells) where it’s needed most to fight the malaria bacteria in the body (Abd‐Rahman et al., 2020).

Selective accumulation of Chloroquine may occur in retina, resulting to worsened condition.

The drug’s t1/2 life is 3-10 days and increases to 20-60 days as drug takes effect.

The parent drug and metabolites are excreted via urine. However, small amount persist in urine months after discontinuation, especially when over-dosage occurs.

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Pharmacodynamics

Adult dosage: 300 mg base (500 mg salt), once/week.
Children: 5 mg/kg base (8.3 mg/kg salt) (maximum is adult dose), once/week (CDC, n.d.).
Prevention dosage: 1-2 weeks before travel; once/week during travel and for 4 weeks after.
Administered orally; absorbed rapidly; widely distributed in body tissues (liver, kidney, eyes, lungs and heart).
Retained in tissues and traverses placenta to embryo.
Metabolism: inhibits the action of heme polymerase and causes toxic heme buildup in Plasmodium.
Has long duration of action (T1/2 = 20-60 days).
Excretion via urine; elimination T1/2 = 3-5 days.

Dosing

Adult dosage: 300 mg base (500 mg salt), once/week.

Children: 5 mg/kg base (8.3 mg/kg salt) (maximum is adult dose), once/week (CDC, n.d.).

Prevention dosage: 1-2 weeks before travel; once/week during travel and for 4 weeks after.

Chloroquine is administered orally; absorbed rapidly and widely distributed in body tissues (liver, kidney, eyes, lungs and heart) (Daily et al., 2022).

The drug is retained in tissues and traverses placenta to reach the embryo.

Metabolism: Chloroquine inhibits the action of heme polymerase and causes toxic heme to buildup in Plasmodium (Abd‐Rahman et al., 2020). This ruptures and kills the plasmodium; thereby, fighting them in the body.

When taken, it has a long duration of action inside the body (T1/2 = 20-60 days).

It’s excreted from the body through urine. The elimination takes T1/2 = 3-5 days.

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Product Description, Use, Side Effects, Adverse Reactions and Safety Issues

Chloroquine is an antibacterial and amebicides drug.

Use: prevent and treat malaria and protozoan-liver infections.

Chloroquine is an antibacterial and amebicides drug.

It’s used in preventing and treating malaria and protozoa-caused liver infections.

The common side effects and adverse reactions associated with Chloroquine are:

Nervous system - Headache, dizziness, vertigo (spinning head), tinnitus (ringing ears) and peripheral polyneuropathy (numbness in hands and feet) (Daily et al., 2022).
Heart – Cardiomyopathy (heart experiences difficulty pumping the blood) and conduction disorders (QT interval enlargement).
Gastrointestinal - Loss of appetite, nausea, diarrhea and abdominal pain (Daily et al., 2022).
Skin - Rash, cutaneous hyperpigmentation (skin darkens), pruritus (itchy skin), Acute generalized exanthematous pustulosis (AGEP) and Stevens-Johnson syndrome (painful rash which spreads and blisters).
Eye – Retinopathy
Muscles - muscle weakness
Toxicity, especially in children.

The main safety issues is the abnormal heart rhythms like:

QT interval prolongation
Ventricular tachycardia (extreme rapid heart rate).

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Ethnic, Cultural, and Genetic Differences in Patients

Ethnic beliefs of some communities bar them from using modern medication to treat illnesses.
Some cultures forbid taking foreign malaria drugs and recommends prayers by religious leaders.
Genetic mutation causes resistance to Chloroquine; thus affecting its efficacy (Daily et al., 2022).
For instance, Chloroquine is no longer effective in treating malaria in many parts of Africa due to genetic mutation & drug resistance.

Ethnic beliefs of some communities bar them from using modern medication to treat illnesses.

In fact, some cultures forbid taking foreign malaria drugs and recommend visiting the religious leaders for prayers. Sick individuals are to have been cursed and encouraged to use local herbs which are ineffective in treating or preventing malaria.

The rapid genetic mutation of malaria-causing bacteria and the patient’s genetic mutation causes resistance to Chloroquine; thus affecting the efficacy of the drug (Daily et al., 2022).

For instance, Chloroquine is no longer effective in treating malaria in many parts of Africa due to genetic mutation and widespread genetic resistance to Chloroquine drug.

The patients’ resistance to drug due ethnic and cultural beliefs pose serious safety risks and adversely impact the efficacy of Chloroquine in treating and preventing malaria (Daily et al., 2022).

The genetic mutation of the malaria-causing bacteria makes it resistant to Chloroquine, thereby, affecting the efficacy of the drug in treating malaria.

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Success Evaluation

The success of the drug in treating malaria will be established by:

Monitoring the effectiveness of the drug in treating a malaria patient.
Monitoring the side effects and adverse reactions of the drug on patient.
Little to no adverse reactions will reflect success.
Monitoring the persistence and severity of the symptoms after administering the drug (Doyno et al., 2021).
Monitoring the recovery speed of the patients under dosage.

The success of the drug in treating malaria will be established by:

Monitoring the effectiveness of the drug in treating a malaria patient. A high treatment score rate will reflect greater effectiveness and achievement of the desired outcome (Doyno et al., 2021).
Monitoring the side effects and adverse reactions of the drug on patient. Little to no adverse reactions will reflect success while numerous adverse reactions/side effects will manifest failure to achieve the desired outcome.
Monitoring the persistence and severity of the symptoms after administering the drug. According to Doyno et al. (2021), if the symptoms persist and patient’s condition worsen, the goal is not achieved.
Monitoring the recovery speed of the patients under dosage. Faster recovery shows the drug is effective and slow recovery

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Conclusion

Malaria is a serious disease that poses extreme risks to individuals if not addressed early enough.
The Chloroquine is an essential antimalarial drug for preventing and treating malaria.
The pharmacokinetics and pharmacodynamics of the Chloroquine makes it an effective malaria treating drug.
This drug is rapidly absorbed, distributed across body tissues and applied by body to fight the malaria.
Its associated with side effects and adverse reactions that must be outlined to patients to promote their safety.
The ethnic, cultural and genetic factors are the key aspects hindering the success of Chloroquine in malaria treatment.

What are your thoughts on reducing genetic resistance to Chloroquine drug?

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References

Abd‐Rahman, A. N., Marquart, L., Gobeau, N., Kümmel, A., Simpson, J. A., Chalon, S., ... & McCarthy, J. S. (2020). Population pharmacokinetics and pharmacodynamics of chloroquine in a plasmodium vivax volunteer infection study. Clinical Pharmacology & Therapeutics, 108(5), 1055-1066.
CDC (n.d.). Choosing a drug to prevent malaria: Chloroquine. https://www.cdc.gov/malaria/travelers/drugs.html
Daily, J. P., Minuti, A., & Khan, N. (2022). Diagnosis, Treatment, and Prevention of Malaria in the US: A Review. JAMA, 328(5), 460-471.
Doyno, C., Sobieraj, D. M., & Baker, W. L. (2021). Toxicity of chloroquine and hydroxychloroquine following therapeutic use or overdose. Clinical Toxicology, 59(1), 12-23.