- March 15, 2022
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Brand Name :
Chloroquine phosphate
Synonyms :
chloraquine, Chloroquinum, Cloroquina, Chlorochin
Class :
Antimalarials; Amino quinolones
Dosage Forms & Strengths
Tablet
250mg
500mg
16.6 mg of chloroquine phosphate is equivalent to 10 mg of chloroquine base
As prophylaxis for malaria in the areas where chloroquine resistance is not present
Do not exceed 500 mg salt (with 300 mg base) each week on the same day
Initiate the medicine 1-2 weeks before/during traveling
and 4 weeks later, leaving the endemic area
Treatment-
Indicated for acute malarial attacks due to P.vivax, P.ovale, P.malariae and a few strains of P.falciparum
Acute attack-
1000 mg salt (with 600 mg base) orally, then
500 mg salt (with 300 mg base) orally after 6-8 hours, later
500 mg salt (with 300 mg base) orally at 1st and 2nd day after the initial dose
A total dose of 2500 mg (with 1500 mg base) in 3 days is indicated
Extraintestinal Amebiasis
1000 mg salt (with 600 mg base) orally each day for 2 days
500 mg salt (with 300 mg base) each day for 14-21 days
(Off-label)
125-250 mg salt (with 75-150 mg base) orally twice weekly
Dosage Forms & Strengths
Tablet
250mg
500mg
16.6 mg of chloroquine phosphate is equivalent to 10 mg of chloroquine base
Indicated for extraintestinal amebiasis
1000 mg salt (with 600 mg base) orally each day for 2 days
500 mg salt (with 300 mg base) each day for 14-21 days
As prophylaxis for malaria in the areas where chloroquine resistance is not present
5 mg/kg orally each week
Do not exceed 500 mg salt (with 300 mg base) each week on the same day
Initiate the medicine 1-2 weeks before/during traveling
and 4 weeks later, leaving the endemic area
Treatment-
Indicated for acute malarial attacks due to P.vivax, P.ovale, P.malariae, and a few strains of P.falciparum
Acute attack-
1st dose- 10 mg base/kg (do not exceed 600 mg base/dose)
2nd dose- 6 hours later, 5 mg base/kg (do not exceed 300 mg base/dose)
3rd dose- 24 hours later the first dose, 5 mg base/kg (do not exceed 300 mg base/dose)
4th dose- 36 hours after the first dose, 5 mg base/kg (do not exceed 300 mg base/dose)
Total dose- 25 mg base/kg
Dose Modifications
Use chloroquine cautiously in hepatically impaired people who are alcoholic or conjunct with hepatotoxic drugs
Refer to the adult dosing
may have an increased QTc-prolonging effect when combined with chloroquine
may have an increased QTc-prolonging effect when combined with chloroquine
may have an increased QTc-prolonging effect when combined with chloroquine
may have an increased QTc-prolonging effect when combined with chloroquine
may have an increased QTc-prolonging effect when combined with chloroquine
chloroquine: they may diminish the serum concentration of antacids
chloroquine: they may diminish the serum concentration of antacids
chloroquine: they may diminish the serum concentration of antacids
chloroquine: they may diminish the serum concentration of antacids
chloroquine: they may diminish the serum concentration of antacids
Chloroquine reduces the serum concentrations of ampicillin. Apply at least 2 hours of gap between administration of chloroquine and ampicillin.
may decrease the therapeutic effect, when combined
may diminish the serum concentration when combined with chloroquine
may increase the QTc prolonging effect of QT-prolonging Class III Antiarrhythmics
may diminish the serum concentration of Antacids
may enhance the metabolism of clobetasol propionate.
It may enhance QTc interval when combined with lithium
cisapride's toxicity is increased by chloroquine’s effect on the QTc interval
may increase the QT-prolonging effect and enhance the risk of ventricular arrhythmias
kaolin decreases the absorption of chloroquine and reduces the serum concentration
may increase the QTc interval
may have an increased risk of rhabdomyolysis & myoglobinuria when combined with chloroquine
may increase the serum concentration of cardiac glycosides
may increase the serum concentration of cardiac glycosides
may increase the serum concentration of cardiac glycosides
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
QT-prolonging Miscellaneous Agents may increase the QTc-prolonging effect of chloroquine
QT-prolonging Miscellaneous Agents may increase the QTc-prolonging effect of chloroquine
QT-prolonging Miscellaneous Agents may increase the QTc-prolonging effect of chloroquine
QT-prolonging Miscellaneous Agents may increase the QTc-prolonging effect of chloroquine
may have an increased QTc-prolonging effect when combined with chloroquine
may have an increased QTc-prolonging effect when combined with chloroquine
may have an increased QTc-prolonging effect when combined with chloroquine
may have an increased QTc-prolonging effect when combined with chloroquine
It may enhance the levels when combined with tamsulosin by affecting CYP2D6 metabolism
tamoxifen increases the toxic or adverse effects of chloroquine
when ajmaline is used together with chloroquine, the risk or seriousness of QTc prolongation is enhanced
chloroquine has the potential to reduce the rate of excretion of idebenone, leading to an elevation in levels of serum
Combining tegafur with chloroquine can reduce tegafur’s metabolism
when both drugs are combined, there may be a reduced metabolism of paclitaxel
tamoxifen may enhance the toxic effects of chloroquine and the risk of retinal toxicity
QTc interval is increased both by lenvatinib and chloroquine
the effect of chloroquine is decreased by lorlatinib, by altering intestinal or hepatic CYP3A4 enzyme metabolism
it may increase the QT-c prolonging effect of QT-prolonging agents such as toremifene
osimertinib and chloroquine, when used simultaneously, increase the QTc interval
may enhance the risk of adverse/toxic effect of dapsone
may have an increased QTc prolongation when combined with chloroquine
chloroquine exerts pharmacodynamic antagonism, leading to a reduction in the effectiveness of the live rotavirus oral vaccine
when both drugs are combined, there may be increased toxicity of vorinostat by QTC interval
it alters the QTc interval and increases the toxicity of sorafenib
it increases the toxicity of octreotide by affecting the QTc interval
Actions and Spectrum:
Actions:
chloroquine is a medication that is primarily used to treat and prevent malaria. It works by interfering with the body’s growth and reproduction of the malaria parasite.
In addition to its use for malaria, chloroquine has also been used for other medical conditions, such as rheumatoid arthritis and lupus. It has been found to have anti-inflammatory properties and can help reduce pain and swelling associated with these conditions.
chloroquine is a member of a class of drugs known as antimalarials, which includes other medications such as quinine and mefloquine. It is effective against both the blood stage and liver stage of the malaria parasite.
Spectrum:
The spectrum of chloroquine refers to the range of organisms that it can be effective against. In addition to malaria, chloroquine has been used to treat other protozoal infections, such as amoebic dysentery and giardiasis. It has also been effective against certain viral infections, such as those caused by the Ebola virus.
Frequency not defined
Severe headache
Nausea
Vomiting
Diarrhea
Blurred vision
Urticaria
Erythema multiforme
Psychosis
Hypertension
Hypoglycemia
Anorexia
Pancytopenia
Neutropenia
Polyneuropathy
Delirium
Insomnia
Depression
Suicidal behavior
Hallucinations
Hypoglycemia
Black-Box Warning:
None
Contraindication/Caution:
Some of the contraindications and precautions of chloroquine include:
Allergy: chloroquine should not be used in individuals with a known allergy to chloroquine or related compounds.
Pregnancy consideration:
Not suitable for pregnant females
Breastfeeding warnings:
The benefits of lactation should outweigh the risks of the drug during the treatment.
Pregnancy category:
Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester.
Category B: No evidence of risk to the fetus is found in animal reproduction studies, and there are not enough studies on pregnant women.
Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for a human product; Pregnant women must take care of the potential risks.
Category D: There is adequate data with sufficient evidence of human fetal risk from various platforms. However, despite potential dangers may be used only in emergencies for potential benefits.
Category X: Drugs listed in this category outweigh the risks over benefits. The drug is not for pregnant women.
Category N: No data is available for the drug under this category.
Pharmacology:
chloroquine is a medication that belongs to a class of drugs known as antimalarials. It works by interfering with the growth and reproduction of the malaria parasite in the body.
chloroquine acts by accumulating in the acidic environment of the parasite’s digestive vacuole, where it binds to heme, a by-product of the parasite’s digestion of hemoglobin, and prevents its conversion into a form that is toxic to the parasite. This leads to the accumulation of toxic heme within the parasite, which eventually kills it.
In addition to its antimalarial activity, chloroquine has been found to have anti-inflammatory properties and can help reduce pain and swelling associated with conditions such as rheumatoid arthritis and lupus. It is thought to achieve this effect by interfering with the activity of immune cells and cytokines involved in inflammation.
chloroquine is rapidly absorbed after oral administration and reaches peak levels in the blood within 1-3 hours. It is distributed throughout the body, including to the liver, spleen, and kidneys, where it accumulates in higher concentrations than in other tissues. chloroquine is metabolized in the liver and excreted primarily in the urine.
chloroquine has a relatively long half-life, ranging from 1-2 months, and can persist in the body for weeks after a single dose. This means that it can be used as a prophylactic medication to prevent malaria, as well as a treatment for acute episodes of the disease.
Pharmacodynamics:
The pharmacodynamics of chloroquine involves its mechanism of action and effects on the body.
chloroquine is a medication that works by interfering with the DNA synthesis of the parasites that cause malaria. Specifically, it binds to the heme molecules released by the parasites when they break down hemoglobin and prevent the polymerization of heme, which is toxic to the parasites. This accumulation of heme results in the death of the parasite.
In addition to its effects on parasites, chloroquine also has immunomodulatory properties. It can inhibit the production and release of pro-inflammatory cytokines and chemokines, which are involved in the immune response to infections and can contribute to tissue damage and inflammation.
chloroquine also inhibits the activity of enzymes involved in the glycosylation of proteins, which is a process that can be involved in viral entry into host cells. This is one of the reasons why chloroquine has been investigated as a potential treatment for viral infections such as COVID-19.
Pharmacokinetics:
The bioavailability is 89%
The peak plasma concentration is achieved in 1-2 hours
The drug gets widely distributed in body tissues (like, the heart, eyes, kidneys, lungs, and liver)
Partially metabolized in the liver
The half-life is 3-5 days
The drug is excreted in urine
Administration:
chloroquine is typically administered orally, in the form of tablets or syrup. The dosage and duration of treatment depend on the condition being treated, the severity of the symptoms, and other individual factors such as age, weight, and medical history.
Patient information leaflet
Generic Name: chloroquine
Pronounced: KLOR-oh-kwin
Why do we use chloroquine?
chloroquine is a medication that has been primarily used to prevent and treat malaria, a mosquito-borne disease caused by a parasite. chloroquine works by killing the parasites that cause malaria by accumulating in the parasite’s food vacuoles, which are essential for the parasite’s survival.
chloroquine has also been used to treat other diseases, including autoimmune disorders such as rheumatoid arthritis and lupus, as well as certain types of infections caused by protozoa, such as amebiasis and giardiasis.
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