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Chloroquine (Nivaquine, Resochin)

Chloroquine is a medication primarily used to prevent and treat malaria, a mosquito-borne infectious disease caused by parasites. It works by interfering with the growth and reproduction of the malaria-causing parasites in the red blood cells of the human body. Chloroquine is also used in the treatment of certain autoimmune diseases like rheumatoid arthritis and lupus erythematosus.

Chloroquine (Nivaquine) was the first drug used for the treatment of malaria. It is effective against the blood stages of the malaria parasite and penetrates into most tissues. It is effective against Plasmodium ovale and malaria and susceptible strains of vivax and falciparum.

It may also be used for the prophylaxis of malaria in travelers visiting endemic areas. However, it is not effective in preventing relapse and should not be used in severe and complicated cases like cerebral malaria. It is also used to treat extraintestinal amebiasis and discoid lupus erythematosus (off-label use)

Chloroquine use in the COVID-19 infection (Wuhan Coronavirus infection - Nivaquine and Coronavirus):

Chloroquine phosphate has also been recommended in the treatment algorithm of Upper respiratory tract infection and pneumonia caused by COVID-19 infection (Wuhan Coronavirus infection). In COVID-19 infection (Wuhan Coronavirus infection), it is given with either oseltamivir or Darunavir. See chloroquine doses below.

Chloroquine dose in Adults

Note: It is comparable to 150 mg of chloroquine base in 250 mg of chloroquine phosphate.

Chloroquine dose for the chemoprophylaxis of malaria:

The usual dose is 500 milligrams (which equals 300 milligrams of the active ingredient) once a week, on the same day each week.
You start taking it 1 to 2 weeks before you might be exposed to malaria, and you keep taking it while you're in an area where malaria is common.
After leaving that area, you continue taking it for another 4 weeks.
This schedule helps make sure you're protected against malaria during and after your time in a place where the disease is a risk.

Chloroquine dose for the treatment of uncomplicated Malaria:

With chloroquine, you take it by mouth.
On the first day, you take a higher dose: 1 gram (which equals 600 milligrams of the active ingredient).
Then, you take a lower dose: 500 milligrams (which equals 300 milligrams of the active ingredient) 6, 24, and 48 hours after the first dose.
This schedule helps make sure the medicine works effectively against the malaria parasites.

Note: It's important to note that for treating certain types of malaria caused by P. vivax and P. ovale, you need to take another medication along with chloroquine, typically an 8-aminoquinoline like primaquine, as per the CDC guidelines from 2013. This combination therapy is necessary to effectively treat these specific types of malaria.

Chloroquine dose for the treatment of Extraintestinal amebiasis:

With chloroquine, you take it by mouth.
For the first two days, you take a higher dose: 1 gram (which equals 600 milligrams of the active ingredient) each day.
After that, you take a lower dose: 500 milligrams (which equals 300 milligrams of the active ingredient) each day.
You continue this lower dose for at least 2 to 3 weeks.

Chloroquine dose as off-label use in Lupus erythematosus:

It's important to note that it's not typically the first choice of medication.

To reduce the risk of retinal toxicity, the maximum daily dose of chloroquine phosphate should not exceed 2.3 milligrams per kilogram of body weight per day, based on your actual weight.
Sometimes, to achieve doses between whole tablets, you might need to split tablets or adjust how often you take them.

Chloroquine phosphate dose in COVID-19 associated pneumonia:

Darunavir 800 mg/Cobiestat 150 mg once day for two weeks together with Chloroquine Phosphate 500 mg twice daily for five days.

Chloroquine phosphate dose in COVID-19 associated upper respiratory tract infection:

5 days of taking 500 mg twice day additionally 150 mg of oseltamivir twice daily for five days.

Chloroquine dose in Children

Note: Chloroquine phosphate is used to represent the dose. 10.6 mg of chloroquine base is the same as 16.6 mg of chloroquine phosphate.

Chloroquine Dose for the Malaria:

Malaria Chemoprophylaxis:

Infants, Children, and Adolescents take it orally.
- Dosage: 8.3 milligrams per kilogram of chloroquine phosphate once a week, on the same day each week.
- Maximum dose: 500 milligrams of chloroquine phosphate per dose.
- Start taking it 1 to 2 weeks before possible exposure.
- Keep taking it while in an area where malaria is common.
- Continue for at least 4 weeks after leaving the malaria-prone area.
- If starting treatment is delayed, double the initial loading dose (16.6 milligrams per kilogram, up to 1,000 milligrams of chloroquine phosphate) and split into 2 doses 6 hours apart.
- Continue this regimen for 8 weeks after leaving the malaria-prone area. (CDC 2014)

Treatment for Acute Attack, Uncomplicated Malaria:

Infants, Children, and Adolescents take it orally.
- Initial dose: 16.6 milligrams per kilogram of chloroquine phosphate (maximum initial dose: 1,000 milligrams of chloroquine phosphate).
- Followed by 8.3 milligrams per kilogram of chloroquine phosphate (maximum dose: 500 milligrams of chloroquine phosphate per dose) at 6, 24, and 48 hours after the initial dose, totaling 4 doses. (CDC 2013)

Chloroquine dose in the Treatment of Extraintestinal amebiasis and liver abscess:

In children and adolescents:

Use chloroquine orally.
The dosage is 16.6 milligrams per kilogram of chloroquine phosphate per dose, once daily.
This is usually combined with metronidazole or tinidazole for 21 days.
After this initial treatment, paromomycin or iodoquinol may be prescribed.
The maximum dose is 1,000 milligrams of chloroquine phosphate per dose.

Pregnancy Risk Factor C

Chloroquine and its byproducts pass from the mother to the baby through the placenta and can be found in the newborn's cord blood and urine.
Studies have shown that these substances can still be detected in cord blood up to around 89 days after the mother's last dose.
When used in recommended doses to prevent malaria during pregnancy, chloroquine hasn't been linked to increased risks for the baby.
However, getting malaria while pregnant can lead to problems like premature birth, miscarriage, and stillbirth.
Because malaria can be more severe in pregnant women and pose risks to both mother and baby, it's generally advised for pregnant women and those planning to become pregnant to avoid traveling to places where malaria is common.
If travel can't be avoided, chloroquine can be used to prevent malaria.
In regions where malaria is sensitive to chloroquine, it's also recommended for treating pregnant women who have uncomplicated malaria.
And if the malaria is caused by chloroquine-sensitive parasites like P.vivax or P. ovale, pregnant women should stay on chloroquine prevention throughout their pregnancy.
Chloroquine can be used during all trimesters of pregnancy, but due to changes in the body during pregnancy, some aspects of how chloroquine works might be different.

Use during breastfeeding:

Chloroquine and its metabolite can pass into breast milk.
In one study, when 11 nursing women with malaria were given a single dose of chloroquine 600 mg, the highest daily dose to the breastfeeding baby was about 0.7% of the mother's dose.
However, the actual amount in breast milk can vary depending on factors like the mother's dose, dosing schedule, how it's given, and how it's measured.
Calculations based on different studies suggest that the baby might get anywhere from 0.9% to 9.5% of the mother's dose of chloroquine and 0.19% to 2.5% of the dose of its metabolite.
Generally, it's considered safe for breastfeeding when the baby gets less than 10% of the mother's dose.
Guidelines say it's okay to breastfeed when using normal doses of chloroquine for malaria or rheumatic disorders.
But babies who get chloroquine through breast milk should be watched for issues like anemia and jaundice, especially if they're premature or less than a month old, and breastfeeding isn't recommended for babies who lack an enzyme called G-6-PD.
If there's a chance the baby could have a severe reaction, the doctor might suggest stopping breastfeeding or stopping the medicine, considering how important it is for the mother's treatment.
But relying only on breast milk wouldn't give enough protection if the baby needs treatment for malaria.
In that case, the baby should be treated directly with chloroquine.

Chloroquine dose in renal disease:

Normal Kidney Function (GFR ≥10 mL/minute):
- No need to adjust the dosage.
Severely Impaired Kidney Function (GFR <10 mL/minute):
- Administer half of the usual dose.
For Patients Undergoing Hemodialysis or Peritoneal Dialysis:
- Give half of the usual dose.
For Patients Undergoing Continuous Renal Replacement Therapy (CRRT):
- No need to adjust the dosage.

Chloroquine Dose in Liver disease:

There aren't specific dosage adjustments for people with liver problems in the manufacturer's instructions.
It's important to be careful when using the medication in these cases.

Common Side Effects of chloroquine:

Cardiovascular:
- Atrioventricular block
- Bundle branch block
- Cardiac arrhythmia
- Cardiomyopathy
- ECG changes including prolonged QRS and QTc intervals, T-wave inversion, or depression
- Hypotension
- Torsades de pointes
- Ventricular fibrillation
- Ventricular tachycardia
Central nervous system:
- Agitation
- Anxiety
- Confusion
- Depressed deep tendon reflex
- Delirium
- Depression
- Extrapyramidal reactions like dystonia, dyskinesia, and protrusion of the tongue, torticollis),
- Hallucination
- Headache
- Insomnia
- Motor dysfunction
- Personality changes
- Polyneuropathy
- Psychosis
- Seizure
- Suicidal tendencies
Dermatologic:
- Alopecia
- Bleaching of hair
- Blue-gray skin pigmentation
- Erythema multiforme
- Exacerbation of psoriasis
- Exfoliative dermatitis
- Lichen planus
- Pleomorphic rash
- Pruritus
- Skin
- Photosensitivity
- Stevens-Johnson syndrome
- Toxic epidermal necrolysis
- Urticaria
Endocrine & metabolic:
- Hypoglycemia
Gastrointestinal:
- Abdominal cramps
- Anorexia
- Diarrhea
- Nausea
- Vomiting
Hematologic & oncologic:
- Reversible Agranulocytosis
- Aplastic anemia
- Hemolytic anemia especially in G6PD-deficient patients
- Neutropenia
- Pancytopenia
- Thrombocytopenia
Hepatic:
- Hepatitis
- Increased liver enzymes
Hypersensitivity:
- Anaphylactoid reaction
- Anaphylaxis
- Angioedema
Immunologic:
- DRESS syndrome
Neuromuscular & skeletal:
- Myopathy
- Neuromuscular disease
- Proximal myopathy
Ophthalmic:
- Accommodation disturbances
- Blurred vision
- Reversible Corneal opacification
- Irreversible Macular degeneration
- Maculopathy which may be irreversible
- Nocturnal amblyopia
- Retinopathy (may be irreversible in some patients on long term therapy)
- Transient scotomata
- Visual field defects
Otic:
- Sensorineural Deafness
- hearing loss, particularly in people with auditory damage already
- Tinnitus

Contraindications to Chloroquine use include:

If someone is allergic to chloroquine or similar medications, or if they have any sensitivity to the ingredients in the medication, they shouldn't take it.
Additionally, if they have any eye problems, especially ones affecting their vision or the retina, that aren't related to acute malaria, they should avoid using chloroquine for other conditions.

Warnings and Precautions

Cardiovascular effects

Chloroquine can have serious effects on the heart.
Long-term use at high doses can lead to a condition called cardiomyopathy, which can cause heart failure and, in some cases, be fatal.
If signs or symptoms of cardiomyopathy appear, like difficulty breathing or swelling in the legs, the medication should be stopped.
Also, if heart rhythm problems like bundle branch block or AV block are diagnosed, chloroquine should be discontinued due to its potential to worsen these conditions.
Chloroquine can also affect the heart's electrical activity, leading to QT prolongation, torsades de pointes, and potentially fatal ventricular arrhythmias, especially with high doses.
It's important to be cautious when using chloroquine in patients with heart disease, a history of abnormal heart rhythms, low potassium or magnesium levels, slow heart rate, or when taking other medications that can prolong the QT interval.
According to the American Heart Association, chloroquine is considered a major contributor to heart problems.

Extrapyramidal effects:

Chloroquine can sometimes cause acute extrapyramidal disorders, which affect movement and muscle control.
These effects usually go away once the medication is stopped or with treatment to relieve symptoms.

Hematologic effects

Chloroquine can cause rare but serious blood-related reactions like agranulocytosis, aplastic anemia, neutropenia, pancytopenia, and thrombocytopenia.
It's important to monitor blood counts regularly during long-term treatment.
If severe blood disorders occur that aren't related to the underlying disease being treated, it may be necessary to stop using chloroquine.

Hypoglycemia:

Patients taking chloroquine, with or without other diabetes medications, have experienced severe hypoglycemia, which can lead to loss of consciousness.
It's important to advise patients about the risk of hypoglycemia and the signs and symptoms associated with it.

Neuromuscular effects:

Chloroquine can sometimes lead to skeletal muscle myopathy or neuromyopathy, which causes progressive weakness and shrinking of certain muscle groups, especially those close to the center of the body.
It's essential to regularly check muscle strength, especially in these central muscle groups, during long-term treatment.
If weakness is noticed, it's important to stop the therapy.

Toxicity to the retina:

Chloroquine and hydroxychloroquine, when used for a long time at high doses, can lead to retinal toxicity, which might cause permanent damage to the retina.
This risk is more significant in those who use these medications for more than five years, take high daily doses, have kidney problems, are using tamoxifen, have a lower body weight, or have existing macular disease.
To minimize this risk, it's recommended not to exceed a daily dose of 2.3 milligrams per kilogram of actual body weight.
Previous advice to use ideal body weight is no longer recommended, as very thin individuals were found to have an increased risk of retinal toxicity.
The American Academy of Ophthalmology suggests baseline screening for retinal toxicity and yearly screenings after five years of use, or sooner if major risk factors are present.

Auditory damage

Chloroquine should be used cautiously in patients with existing hearing problems.
If any hearing issues are noticed while taking the medication, it's important to stop using it right away.

G6PD deficiency:

The use of chloroquine in patients with G6PD deficiency, a condition that can lead to hemolytic anemia, is advised with caution according to the manufacturer's instructions.
However, there's limited evidence supporting this risk.
Many experts believe that chloroquine is likely safe when used in typical doses for patients with WHO Class II and III G6PD deficiency.
Safety data for patients with Class I G6PD deficiency, the more severe form associated with chronic hemolytic anemia, is generally lacking.
A trial in West Africa involving mostly Class III deficient patients found no cases of hemolysis after using standard doses of chloroquine.
Moreover, the American College of Rheumatology guidelines don't mention the need to check G6PD levels before starting treatment with chloroquine.

Hepatic impairment

Chloroquine should be used carefully in patients with liver problems, alcoholism, or those taking other medications that can harm the liver.

Porphyria

Patients with porphyria should be cautious when using chloroquine, as it may worsen symptoms of the condition.

Psoriasis:

Patients with psoriasis should use chloroquine cautiously, as it might make their symptoms worse.

Seizure disorder:

Patients with a history of seizure disorders should be cautious when using chloroquine, as it may potentially trigger seizures.

Chloroquine: Drug Interaction

Note: Drug Interaction Categories:

Risk Factor C: Monitor When Using Combination
Risk Factor D: Consider Treatment Modification
Risk Factor X: Avoid Concomitant Use

Risk Factor C (Monitor therapy).
Androgens	May increase the hypoglycemic effects of Blood Glucose Lowering Agents. Danazol is an exception.
Antidiabetic Agents	Possibly makes hypoglycemia-associated agents more effective.
Antipsychotic Agents (Phenothiazines).	Antipsychotic Agents' serum levels can be raised by antimalarial drugs (Phenothiazines).
Aprepitant	High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Beta-Blockers	Antimalarial Aminoquinolines may reduce Beta-Blocker metabolism. Exceptions: Atenolol, Carteolol Ophthalmic; Levobunolol. Metipranolol. Nadolol. Sotalol.
Bosentan	Could decrease serum levels of CYP3A4 substrates (High Risk with Inducers).
Cardiac Glycosides	Antimalarial Aminoquinolines may raise serum levels of Cardiac Glycosides.
Cimetidine	Increases the serum level of Chloroquine
CloBAZam	High risk of Inhibitors increasing serum concentrations of CYP2D6 Substrates
Clofazimine	High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Moderate CYP2D6 inhibitors	Might decrease metabolism of CYP2D6 substrates (High Risk with Inhibitors).
Moderate CYP3A4 Inducers	Could lower serum concentrations of CYP3A4 substrates (High Risk with Inducers).
Moderate CYP3A4 inhibitors	Might decrease metabolism of CYP3A4 substrates (High Risk with Inhibitors).
Deferasirox	Could lower serum concentrations of CYP3A4 substrates (High Risk with Inducers).
Duvelisib	High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Erdafitinib	Could lower serum concentrations of CYP3A4 substrates (High Risk with Inducers).
Erdafitinib	High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Fosaprepitant	High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Fosnetupitant	High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Haloperidol	Haloperidol's QTc-prolonging effects can be amplified by other QT-prolonging substances (Moderate risk). Be sure to keep an eye out for QTc interval prolongation or ventricular arrhythmias when these medications are taken together. There may be additional risk factors in patients who are at increased risk for QTc prolongation.
Herbs (Hypoglycemic properties)	May intensify the hypoglycemic effects of agents associated with hypoglycemia.
Hypoglycemia-Associated Agents	May increase other hypoglycemia-associated agents' hypoglycemic effects.
Imatinib	High risk of Inhibitors increasing serum concentrations of CYP2D6 Substrates
Larotrectinib	High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Local Anesthesia	Agents associated with methemoglobinemia may intensify the negative or toxic effects of local anaesthetics. Risk of methemoglobinemia could rise.
Maitake	Potential to enhance blood glucose lowering agents' hypoglycemic effects.
Monoamine Oxidase Inhibitors	Potential to enhance blood glucose lowering agents' hypoglycemic effects.
Netupitant	High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Nitric Oxide	May intensify the toxic/unfavorable effects of agents associated with methemoglobinemia. Methemoglobinemia risk may rise when these drugs are combined. Monitoring patients for symptoms like hypoxia and cyanosis is crucial when nitric oxide is coupled with other substances that can lead to methemoglobinemia. Do not use lidocaine or prilocaine.
Ondansetron	Ondansetron's QTc-prolonging effects could be amplified by other QT-prolonging substances (Moderate risk). Watch for QTc interval prolongation or cardiac arrhythmias when using these medications together. There may be additional risk factors in patients who are at increased risk for QTc prolongation.
Palbociclib	High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Panobinostat	High risk of Inhibitors increasing serum concentrations of CYP2D6 Substrates
Peginterferon Alfa-2b	Inhibitors carry a high danger. may reduce the level of CYP2D6 substrates in serum. Serum levels of CYP2D6 Substrates may rise after administration of peginterferon Alf-2b.
Pegvisomant	Might increase the hypoglycemic effects of Blood Glucose Lowing Agents.
Pentamidine (Systemic)	Pentamidine (Systemic) may intensify the effects of other drugs that cause QTc prolongation (Moderate risk). Watch for QTc interval prolongation or cardiac arrhythmias when using these medications together. There may be additional risk factors in patients who are at increased risk for QTc prolongation.
Perhexiline	Perhexiline may be increased by CYP2D6 Substrates. Perhexiline can increase serum concentrations of CYP2D6 substrates (High Risk with Inhibitors).
Praziquantel	By lowering the level of chloroquine in the serum, praziquantel may be lessened.
Prilocaine	Methemoglobinemia Associated Agents can intensify Prilocaine's toxic/unfavorable effects. Methemoglobinemia risk can be raised when these drugs are combined. Keep an eye out for symptoms like hypoxia and cyanosis in patients when prilocaine is taken with other drugs that can result in methemoglobinemia. Infants receiving lidocaine or prilocaine shouldn't be administered lidocaine or prilocaine.
Primaquine	The serum concentration of Primaquine could be increased by taking chloroquine.
Prothionamide	Might increase the hypoglycemic effects of Blood Glucose Lowing Agents.
QT-prolonging Antidepressants (Moderate risk)	Miscellaneous QT-prolonging substances could intensify the QTc-prolonging effects (moderate risk). When these medications are taken combined, keep an eye out for cardiac arrhythmias or a prolonged QTc interval. There may be additional risk factors in patients who are at increased risk for QTc prolongation.
QT-prolonging Antipsychotics (Moderate Risk)	Miscellaneous QT-prolonging substances (Moderate risk) can intensify the QTc prolonging action. Antipsychotics that extend QT (Moderate risk). When these medications are taken combined, keep an eye out for cardiac arrhythmias or a prolonged QTc interval. There may be additional risk factors in patients who are at increased risk for QTc prolongation. But there is one: pimozide.
QT-prolonging Class IC Antiarrhythmics (Moderate Risk)	Miscellaneous QT-prolonging substances (Moderate risk) can intensify the QTc prolonging action. Antiarrhythmics of class IC that prolong QT with a modest risk. When these medications are taken combined, keep an eye out for cardiac arrhythmias or a prolonged QTc interval. There may be additional risk factors in patients who are at increased risk for QTc prolongation.
QT-prolonging Kinase Inhibitors (Moderate Risk)	Miscellaneous QT-prolonging substances could intensify the QTc-prolonging effects (moderate risk). When these medications are taken combined, keep an eye out for cardiac arrhythmias or a prolonged QTc interval. There may be additional risk factors in patients who are at increased risk for QTc prolongation.
QT-prolonging Miscellaneous Agents (Moderate Risk)	It might intensify Chloroquine's QTc-extension effects. When these medications are taken combined, keep an eye out for cardiac arrhythmias or a prolonged QTc interval. There may be additional risk factors in patients who are at increased risk for QTc prolongation. The exception is domperidone.
QT-prolonging Moderate CYP3A4 Drug Inhibitors (Moderate risk)	The effects of several medicines that prolong QT (moderate risk) may also prolong QTc. QT-prolonging Moderate CYP3A4 Drug Inhibitors (Moderate risk) may cause a rise in the serum levels of QT-prolonging Other Drugs (Moderate risk). When these medications are taken combined, keep an eye out for cardiac arrhythmias or a prolonged QTc interval.
Quinolone Antibiotics for QT-prolonging (Moderate risk)	QT-prolonging Quinolone antibiotics may somewhat increase the effect's propensity to extend QTc. When these medications are taken combined, keep an eye out for cardiac arrhythmias or a prolonged QTc interval. There may be additional risk factors in patients who are at increased risk for QTc prolongation.
Quinolones	May intensify blood glucose lowering agents' hypoglycemic effects. Blood glucose lowering agents' therapeutic benefits can be lessened by quinolones. Using quinolones in conjunction with diabetes medication may result in issues controlling blood sugar.
Rabies Vaccine	The therapeutic effects of Rabies Vaccine may be diminished by the use of chloroquine.
Salicylates	Might increase the hypoglycemic effects of Blood Glucose Lowing Agents.
Sarilumab	Could lower serum concentrations of CYP3A4 substrates (High Risk with Inducers).
Selective Serotonin Reuptake inhibitors	Might increase the hypoglycemic effects of Blood Glucose Lowing Agents.
Siltuximab	Could lower serum concentrations of CYP3A4 substrates (High Risk with Inducers).
Simeprevir	High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Sodium Nitrite	The toxic/unfavorable effect of sodium nitrite can be increased by methemoglobinemia associated agents. The likelihood of substantial methemoglobinemia could rise when these medications are combined.
Tamoxifen	Chloroquine's toxic/unfavorable effects can become more pronounced. Retinal toxicities are more likely when tamoxifen or chloroquine are used together.
Tocilizumab	Could lower serum concentrations of CYP3A4 substrates (High Risk with Inducers).
Risk Factor D (Regard therapy modification)
Abiraterone Acetate	High risk of Inhibitors causing an increase in serum concentrations of CYP2D6 substrates. When possible, avoid concurrent use of abiraterone and CYP2D6 Substrates with a narrow therapeutic index. If concurrent use cannot be avoided, closely monitor patients for signs and symptoms of toxic effects.
Ampicillin	The serum concentration of Ampicillin may be decreased by chloroquine. Management: To minimize the potential adverse effects of chloroquine upon ampicillin bioavailability, it is recommended that you separate ampicillin and chloroquine for at least two hours.
Antacids	Chloroquine serum levels may drop as a result. To minimise potential unfavourable effects on chloroquine bioavailability, administer antacids and chloroquine at least 4 hours apart.
Asunaprevir	High risk of Inhibitors increasing serum concentrations of CYP2D6 Substrates
Bacampicillin	Bacampicillin serum concentration may be decreased by chloroquine. Management: The Chloroquine prescribing info recommends that ampicillin and chloroquine be administered separately for at least two hours. This is to minimize any negative effects of chloroquine upon ampicillin bioavailability. Bacampicillin is an ampicillin prodrug.
Cholera Vaccine	Cholera vaccine may be less effective if it is administered with chloroquine. Administration: Cholera vaccine should be administered at least 10 days before starting chloroquine.
Strong CYP2D6 inhibitors	Might decrease metabolism of CYP2D6 substrates (High Risk with Inhibitors).
Strong CYP3A4 Inducers	May increase metabolism of CYP3A4 substrates (High Risk with Inducers). Management: You may consider a different drug to replace one of the interacting drugs. Some combinations might be contraindicated. Consult appropriate manufacturer labeling.
Strong CYP3A4 inhibitors	Might decrease metabolism of CYP3A4 substrates (High Risk with Inhibitors).
Dabrafenib	High risk of Inducers causing a decrease in serum CYP3A4 substrates. Management: If possible, seek alternatives to the CYP3A4 substrate. Concomitant therapy should be avoided if possible. Monitor the clinical effects of the substrate carefully (especially therapeutic effects).
Dacomitinib	High risk of Inhibitors causing an increase in serum concentrations of CYP2D6 substrates. Management: Do not use dacomitinib concurrently with CYP2D6 Substrates that have a narrow therapeutic Index.
Dapsone (Systemic)	Antimalarial medications may intensify Dapsone Systemic's toxic/unfavorable effects. Dapsone and antimalarial medication usage together can worsen hemolytic responses. The toxic/unfavorable effects of antimalarial agents may be increased by systemic. Dapsone and antimalarial medications taken together may worsen hemolytic responses. Patients who lack methemoglobin reductase (G6PD), glucose-6-phosphate hydrogenase (G6PD), or haemoglobin M should be closely monitored.
Dapsone (Topical).	Antimalarial drugs can make Dapsone Topical more toxic or harmful. Hemolytic responses are becoming more likely. Treatment: Carefully watch for hemolytic responses and concurrent topical dapsone or antimalarial medication use. Patients who lack glucose-6-phosphate hydrogenase may be more susceptible to harmful hematologic responses.
Domperidone	The QTc-prolonging effects of Domperidone might be amplified by QT-prolonging drugs (moderate risk). Management: Consider different combinations to this one. If the medicine combination is used, keep an eye out for QTc interval prolongation or cardiac arrhythmias. There may be additional risk factors in patients who are at increased risk for QTc prolongation.
Enzalutamide	High risk of Inducers causing a decrease in serum concentrations of CYP3A4 substrates. Management: Avoid concurrent use of enzalutamide and CYP3A4 substrates with a narrow therapeutic index. You should exercise caution when using enzalutamide or any other CYP3A4 sub-substance.
Kaolin	Chloroquine serum levels may drop as a result. The best way to prevent kaolin from negatively affecting chloroquine's bioavailability is to administer the two drugs apart for at least 4 hours.
Lanthanum	Chloroquine serum levels may drop as a result. Administration: Take chloroquine either right away after or two hours after lanthanum.
Lorlatinib	High risk of Inducers causing a decrease in serum concentrations of CYP3A4 substrates. Management: Do not use lorlatinib concurrently with any CYP3A4 Substrates. Even a slight decrease in serum concentrations could cause therapeutic failure or serious clinical consequences.
MiFEPRIStone	High risk of Inhibitors causing an increase in serum concentrations of CYP3A4 substrates. Management: Minimize doses of CYP3A4 substrates, and monitor for increased concentrations/toxicity, during and 2 weeks following treatment with mifepristone. Avoid dihydroergotamine and ergotamine.
Mitotane	High risk of Inducers causing a decrease in serum concentrations of CYP3A4 substrates. Treatment: Patients receiving mitotane may require significant adjustments in the dosage of CYP3A4 Substrates.
Pitolisant	High risk of Inducers causing a decrease in serum concentrations of CYP3A4 substrates. Management: Avoid combining pitolisant and a CYP3A4 substrat with a low therapeutic index. Pitolisant should not be mixed with other CYP3A4 sub-substances.
Agents that prolong QT (Highest risk)	Might intensify Chloroquine's QTc-extension effects. Management: Alternative pairings may be taken into account. If the combo is utilised, keep an eye out for QTc interval prolongation or cardiac arrhythmias. There may be additional risk factors in patients who are at increased risk for QTc prolongation.
St John's Wort	High risk of Inducers causing a decrease in serum CYP3A4 Substrates. Management: You may consider a different drug to replace one of the interacting drugs. Some combinations might be contraindicated. Consult appropriate manufacturer labeling.
Stiripentol	High risk of Inhibitors causing an increase in serum concentrations of CYP3A4 substrates. Management: Avoid stiripentol use with CYP3A4 Substrates that have a narrow therapeutic Index. This is to avoid adverse effects and toxicities. Monitoring of any CYP3A4 substrate that is used with stiripentol should be closely done.
Risk Factor X (Avoid Combination)
Agalsidase Alfa	Chloroquine can decrease the therapeutic effects of Agalsidase Alfa.
Agalsidase Beta	Chloroquine can decrease the therapeutic effects of Agalsidase beta.
Artemether	Antimalarial drugs may have unfavourable or hazardous side effects that can get worse. Management: Unless there are no other treatment options available, artemether/lumefantrine (combination product) should not be used with other antimalarials.
Conivaptan	High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Fusidic Acid (Systemic).	High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Idelalisib	High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Lumefantrine	Antimalarial medications may intensify Lumefantrine's harmful or severe effects. Management: Unless there are no other treatment options available, artemether/lumefantrine (combination product) should not be used with other antimalarials.
Mefloquine	Mefloquine's toxic/adverse effects may be exacerbated by antimalarial aminoquinolines (Antimalarial). Particularly, QTc-prolongation risk and convulsions risk may increase. The serum concentrations of Aminoquinolines (Antimalarial) may be increased by Mefloquine. Management: If possible, avoid concurrent use and wait at least 12 hours before you start mefloquine administration.
Pimozide	QTc-prolonging agents may have a moderate risk of increasing their QTc-prolonging effects (Moderate Risk).
QT-prolonging Strong CYP3A4 Antiinhibitors (Moderate risk)	QTc-prolonging effects of various QT-prolonging substances could be increased (Moderate risk). Serum concentrations of QT-prolonging Miscellaneous Agents can rise in response to QT-prolonging Strong CYP3A4 Drug Inhibitors (Moderate risk).

Monitor:

Neuromuscular Function Evaluation:

Periodically assess neuromuscular function during prolonged therapy.

Blood Tests:

Regularly check complete blood counts (CBC) in patients on long-term therapy.

Eye Exams:

Conduct an ophthalmologic examination at the beginning of treatment, including a fundus examination within the first year.
Perform visual fields and spectral-domain optical coherence tomography (SD OCT) if maculopathy is present.
Start annual eye screenings after 5 years of chloroquine use, or sooner if there are significant risk factors.

How to administer Chloroquine?

Administration with Meals:

Take chloroquine with meals to reduce the likelihood of gastrointestinal (GI) upset.

Masking Bitter Taste:

Chloroquine phosphate tablets can be mixed with chocolate syrup or enclosed in gelatin capsules to disguise the bitter taste.

Mechanism of action Chloroquine:

Chloroquine works by binding to and blocking DNA and RNA polymerase, crucial enzymes for parasite growth.
It also disrupts the metabolism and the use of hemoglobin by parasites, and it blocks the effects of prostaglandins.
Inside the parasite's acidic vesicles, chloroquine increases the pH, which stops parasite growth.
It might work by interacting with ferriprotoporphyrin IX, causing damage to the parasite's membranes, and it could interfere with the creation of nucleoproteins.

Absorption:

Chloroquine is absorbed rapidly and almost completely after oral administration.

Distribution:

It distributes widely throughout the body tissues, including the eyes, heart, kidneys, liver, white blood cells, and lungs, where it remains for a prolonged period.

Protein Binding:

Approximately 55% of chloroquine is bound to proteins in the bloodstream.

Metabolism:

It undergoes partial metabolism in the liver to its main metabolite, desethylchloroquine.

Half-life:

The half-life of chloroquine is between 3 to 5 days.

Time to Peak Serum Concentration:

After oral administration, chloroquine reaches peak serum concentration within 1 to 2 hours.

Excretion:

It is primarily excreted in the urine, with approximately 70% of the drug and about 35% as unchanged chloroquine.
Acidification of urine can increase elimination. Small amounts of the drug may still be present in the urine months after stopping therapy.

International brands of Chloroquine Phosphate:

A-CO
Alexoquine
Antimal
Aralen
Aralen Phosphate
Arechin
Arquin
Avloclor
Avloquin
Bidimalaquin
Cadiquin
Chemochin
Chlorochin
Chlorofoz
Chloromax
Chlorquin
Clit
Clo-Kit Junior
Clorochina Bayer
Clorochina Bifosfato
Crocan
Delagil
Demoquine
Dichinalex
Diroquine
Heliopar
Heroquine
Klarquine
Klorokinfosfat
Lagaquin
Malachlo
Malaquin
Malarex
Malarivon
Malarquine
Malaviron
Malquin
Maquine
Nivaquine
Paludol
Quinacris
Resochin
Resochina

Chloroquine brand names in Pakistan:

Chloroquine Inj 40 Mg/Ml
Bentaquine	Trigon Pharmaceuticals Pakistan (Pvt) Ltd.
Chloroquinephosphate	Elko Organization (Pvt) Ltd.
Chloroquinephosphate	Pliva Pakistan (Pvt) Limited
Chloroquinephosphate	Dosaco Laboratories
Chloroquinephosphate	Lahore Chemical & Pharmaceutical Works (Pvt) Ltd
Chloroquinephosphate	Munawar Pharma (Pvt) Ltd.
Chloroquinephosphate	P.D.H. Pharmaceuticals (Pvt) Ltd.
Chloroquinephosphate	Irza Pharma (Pvt) Ltd.
Chloroquinephosphate	Geofman Pharmaceuticals
Cilaquine	Harmann Pharmaceutical Laboratories (Pvt) Ltd.
Malaquine Injection	Karachi Pharmaceutical Laboratory
Mb-Quin	Multinational Buisness Link

Chloroquine Injection 5 Mg/5ml
Chloroquine	Harmann Pharmaceutical Laboratories (Pvt) Ltd.

Chloroquine Injection 65 Mg/Ml
Chloroquinephosphate	Shifa Laboratories.(Pvt) Ltd.

Chloroquine Injection 64.5 Mg/Ml
Chloroquine	Orient Laboratories

Chloroquine Syrup 50 Mg/5ml
Asoquin	Hassan Pharmaceuticals (Pvt) Ltd.
Benaquin	Krka-Pak Pharmaceutical & Chemical Works
Binaquine	Karachi Pharmaceutical Laboratory
Chloroquine	Rakaposhi Pharmaceutical (Pvt) Ltd.
Chloroquinephosphate	Pharmawise Labs. (Pvt) Ltd.
Chloroquinephosphate	Jawa Pharmaceuticals(Pvt) Ltd.
Cloquin	W.Woodward Pakistan (Pvt) Ltd.
Daviquin	Davis Pharmaceutical Laboratories
Deloquin	Delux Chemical Industries
Devoquine	Don Valley Pharmaceuticals (Pvt) Ltd.
Eroqeen Syrup	Eros Pharmaceuticals
Geniquin	Genera Pharmaceuticals
Hiquin	Hizat Pharmaceutical Industries (Pvt) Ltd.
Kciquine	Karachi Chemical Industries
Liskochin	Lisko Pakistan (Pvt) Ltd
Malaban	Rakaposhi Pharmaceutical (Pvt) Ltd.
Malaquine	Polyfine Chempharma (Pvt) Ltd.
Moxiquin	Syntex Pharmaceuticals
Nafaquine	Nafar Pharmaceuticals Lab. (Pvt) Ltd.
Nivaquin-P	Sanofi Aventis (Pakistan) Ltd.
Phosoquine	Hamaz Pharmaceutical (Pvt) Ltd.
Proquine	Progressive Laboratories

Chloroquine Syrup 81 Mg/5ml
Quine	Libra Pharmaceuticals (Pvt) Ltd

Chloroquine Syrup 100 Mg/5ml
Rubaquin	Life Pharmaceutical Company

Chloroquine Susp 50 Mg/5ml
Neoquin	Neo Medix

Chloroquine Paed Tab 80 Mg
Chloroquinephosphate	Ardin Pharmaceuticals

Chloroquine Tablets 40 Mg
Chloroquinephosphate	Geofman Pharmaceuticals

Chloroquine Tablets 80 Mg
Benaquin	Krka-Pak Pharmaceutical & Chemical Works
Binaquine	Karachi Pharmaceutical Laboratory
Chloroquinetablets	Irza Pharma (Pvt) Ltd.
Chloroquinetablets	Dosaco Laboratories
Chloroquinetablets	Harmann Pharmaceutical Laboratories (Pvt) Ltd.
Chloroquinetablets	Unexo Labs (Pvt) Ltd.
Chloroquinetablets	Pharmacare Laboratories (Pvt) Ltd.
Chloroquinetablets	Pliva Pakistan (Pvt) Limited
Chloroquinetablets	Lisko Pakistan (Pvt) Ltd
Chloroquinephosphate	Shifa Laboratories.(Pvt) Ltd.
Chloroquinephosphate	Jawa Pharmaceuticals(Pvt) Ltd.
Chloroquinephosphate	Munawar Pharma (Pvt) Ltd.
Chloroquinephosphate	Albro Pharma
Chloroquinephosphate	Ideal Pharmaceutical Industries
Faroquin	Flow Pharmaceuticals (Pvt) Ltd.
Hiquin	Hizat Pharmaceutical Industries (Pvt) Ltd.
Pharoquine	Pharmacare Laboratories (Pvt) Ltd.
Proquine	Progressive Laboratories
Seroquine	Semos Pharmaceuticals (Pvt) Ltd.

Chloroquine Tablets 150 Mg
Chloroquinephosphate	Geofman Pharmaceuticals
Devoquine	Don Valley Pharmaceuticals (Pvt) Ltd.
Tagaquin	Tagma Pharma (Pvt) Ltd.

Chloroquine Tablets 200 Mg
Fooquine	Alfalah Pharma (Pvt) Ltd.
Remoquin	Syntex Pharmaceuticals

Chloroquine Tablets 200 Mg
Fooquine	Alfalah Pharma (Pvt) Ltd.
Remoquin	Syntex Pharmaceuticals.

Chloroquine (Nivaquine, Resochin)

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