Aralen

In case of overdose, call your local poison control center at 1-800-222-1222. If the victim has collapsed or is not breathing, call local emergency services at 911.

Storage

Oral

25°C (may be exposed to 15–30°C) in tight container.136

For all uses of Aralen:

• Tell all of your health care providers that you take Aralen. This includes your doctors, nurses, pharmacists, and dentists.
• A very bad eye problem has happened with this medicine. This may lead to long-lasting eyesight damage. The risk may be higher in older people if Aralen is used for a long time or if a higher dose of this medicine is used. Talk with the doctor.
• Have an eye exam as you have been told by your doctor.
• Be careful if you have G6PD deficiency. Anemia may happen.
• Have your blood work checked if you are on Aralen for a long time. Talk with your doctor.
• Talk with your doctor before you drink alcohol.
• Some other drugs may need to be taken at some other time than this medicine. If you take other drugs, check with your doctor or pharmacist to see if you need to take them at some other time than Aralen.
• If you are taking cyclosporine, talk with your doctor. You may need to have your blood work checked more closely while you are taking it with this medicine.
• This medicine may make you sunburn more easily. Use care if you will be in the sun. Tell your doctor if you sunburn easily while taking this drug.
• Low blood sugar has happened with Aralen. Sometimes, this has been very bad and could be life-threatening. Talk with the doctor.
• Check your blood sugar as you have been told by your doctor.
• A very bad and sometimes deadly reaction has happened with this medicine. Most of the time, this reaction has signs like fever, rash, or swollen glands with problems in body organs like the liver, kidney, blood, heart, muscles and joints, or lungs. Talk with the doctor.
• Keep away from children. Accidental exposure may cause death. If a child takes Aralen (chloroquine) by accident, get medical help right away.
• If you are 65 or older, use this medicine with care. You could have more side effects.
• Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using Aralen while you are pregnant.

Preventing malaria:

• Other measures are needed along with this medicine including using screens, bed netting, insect repellent (10% to 35% DEET), and permethrin spray on clothing and nets. Avoid spraying most insect repellents on children. Lower evening and night-time outdoor activity.
• If you are a pregnant woman and traveling to a malaria infested place, talk to your doctor about the risks first.

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

For all uses of Aralen:

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
• Signs of liver problems like dark urine, feeling tired, not hungry, upset stomach or stomach pain, light-colored stools, throwing up, or yellow skin or eyes.
• Signs of low blood sugar like dizziness, headache, feeling sleepy, feeling weak, shaking, a fast heartbeat, confusion, hunger, or sweating.
• Change in eyesight, eye pain, or very bad eye irritation.
• Trouble controlling body movements.
• Restlessness.
• Seizures.
• Mood changes.
• Change in how you act.
• Not able to sleep.
• Feeling confused.
• Hallucinations (seeing or hearing things that are not there).
• Change in hearing.
• Ringing in ears.
• Muscle pain or weakness.
• A burning, numbness, or tingling feeling that is not normal.
• Fever or chills.
• Sore throat.
• Any unexplained bruising or bleeding.
• Feeling very tired or weak.
• A very bad skin reaction (Stevens-Johnson syndrome/toxic epidermal necrolysis) may happen. It can cause very bad health problems that may not go away, and sometimes death. Get medical help right away if you have signs like red, swollen, blistered, or peeling skin (with or without fever); red or irritated eyes; or sores in your mouth, throat, nose, or eyes.
• Heart problems like heart failure and certain very bad abnormal heartbeats have happened with this medicine. Sometimes, these heart problems have been deadly. Call your doctor right away if you have a fast or abnormal heartbeat; very bad dizziness or passing out; or shortness of breath, a big weight gain, or swelling in the arms or legs.

Preventing malaria:

• Fever that happens while in or after coming back from the malaria area.

Aralen, chloroquine phosphate, USP, is a 4-aminoquinoline compound for oral administration. It is a white, odorless, bitter tasting, crystalline substance, freely soluble in water.

Aralen is an antimalarial and amebicidal drug.

Chemically, it is 7-chloro-4-[[4-(diethylamino)-1-methylbutyl]amino]quinoline phosphate (1:2) and has the following structural formula:

Each tablet contains 500 mg of chloroquine phosphate USP, equivalent to 300 mg chloroquine base.

Inactive Ingredients: Carnauba Wax, Colloidal Silicon Dioxide, Dibasic Calcium Phosphate, Hydroxypropyl Methylcellulose, Magnesium Stearate, Microcrystalline Cellulose, Polyethylene Glycol, Polysorbate 80, Pregelatinized Starch, Sodium Starch Glycolate, Stearic Acid, Titanium Dioxide.

Chloroquine is rapidly and almost completely absorbed from the gastrointestinal tract, and only a small proportion of the administered dose is found in the stools. Approximately 55% of the drug in the plasma is bound to nondiffusible plasma constituents. Excretion of chloroquine is quite slow, but is increased by acidification of the urine. Chloroquine is deposited in the tissues in considerable amounts. In animals, from 200 to 700 times the plasma concentration may be found in the liver, spleen, kidney, and lung; leukocytes also concentrate the drug. The brain and spinal cord, in contrast, contain only 10 to 30 times the amount present in plasma.

Chloroquine undergoes appreciable degradation in the body. The main metabolite is desethylchloroquine, which accounts for one fourth of the total material appearing in the urine; bisdesethylchloroquine, a carboxylic acid derivative, and other metabolic products as yet uncharacterized are found in small amounts. Slightly more than half of the urinary drug products can be accounted for as unchanged chloroquine.

Microbiology

Chloroquine is an antimalarial agent. While the drug can inhibit certain enzymes, its effect is believed to result, at least in part, from its interaction with DNA. However, the mechanism of plasmodicidal action of chloroquine is not completely certain.

Chloroquine is active against the erythrocytic forms of Plasmodium vivax. Plasmodium malariae, and susceptible strains of Plasmodium falciparum (but not the gametocytes of P. falciparum). It is not effective against exoerythrocytic forms of the parasite.

In vitro studies with trophozoites of Entamoeba histolytica have demonstrated that chloroquine also possesses amebicidal activity comparable to that of emetine.

Resistance of Plasmodium falciparum to chloroquine is widespread and cases of Plasmodium vivax resistance have been reported.

Hematological Effects/Laboratory Tests

Complete blood cell counts should be made periodically if patients are given prolonged therapy. If any severe blood disorder appears which is not attributable to the disease under treatment, discontinuance of the drug should be considered.

The drug should be administered with caution to patients having G-6-PD (glucose-6 phosphate dehydrogenase) deficiency.

Auditory Effects

In patients with preexisting auditory damage, chloroquine should be administered with caution. In case of any defects in hearing, chloroquine should be immediately discontinued, and the patient closely observed (see ADVERSE REACTIONS).

Hepatic Effects

Since this drug is known to concentrate in the liver, it should be used with caution in patients with hepatic disease or alcoholism or in conjunction with known hepatotoxic drugs.

Central Nervous System Effects

Patients with history of epilepsy should be advised about the risk of chloroquine provoking seizures.

Drug Interactions

Antacids and kaolin: Antacids and kaolin can reduce absorption of chloroquine; an interval of at least 4 hours between intake of these agents and chloroquine should be observed.

Cimetidine: Cimetidine can inhibit the metabolism of chloroquine, increasing its plasma level. Concomitant use of cimetidine should be avoided.

Ampicillin: In a study of healthy volunteers, chloroquine significantly reduced the bioavailability of ampicillin. An interval of at least two hours between intake of this agent and chloroquine should be observed.

Cyclosporine: After introduction of chloroquine (oral form), a sudden increase in serum cyclosporine level has been reported. Therefore, close monitoring of serum cyclosporine level is recommended and, if necessary, chloroquine should be discontinued.

Mefloquine: Co-administration of chloroquine and mefloquine may increase the risk of convulsions.

The blood concentrations of chloroquine and desethylchloroquine (the major metabolite of chloroquine, which also has antimalarial properties) were negatively associated with log antibody titers. Chloroquine taken in the dose recommended for malaria prophylaxis can reduce the antibody response to primary immunization with intradermal human diploid-cell rabies vaccine.

Pregnancy

See WARNINGS, Usage in Pregnancy.

Nursing Mothers

Because of the potential for serious adverse reactions in nursing infants from chloroquine, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the potential clinical benefit of the drug to the mother.

The excretion of chloroquine and the major metabolite, desethylchloroquine, in breast milk was investigated in eleven lactating mothers following a single oral dose of chloroquine (600 mg base). The maximum daily dose of the drug that the infant can receive from breastfeeding was about 0.7% of the maternal start dose of the drug in malaria chemotherapy. Separate chemoprophylaxis for the infant is required. See DOSAGE AND ADMINISTRATION.

Pediatric Use

See WARNINGS and DOSAGE AND ADMINISTRATION.

Geriatric Use

Clinical studies of Aralen did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. However, this drug is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection and it may be useful to monitor renal function.

1. Malaria Deaths Following Inappropriate Malaria Chemoprophylaxis – United States, 2001. MMWR Weekly, 2001; 50(28): 597–599.
2. Ullberg S, Lindquist N G, Sjostrand S E: Accumulation of chorioretinotoxic drugs in the foetal eye. Nature 1970; 227: 1257.

Manufactured for:
sanofi-aventis U.S. LLC
Bridgewater, NJ 08807

Revised September 2008

© 2008 sanofi-aventis U.S. LLC

You should not use this medication if you are allergic to chloroquine or hydroxychloroquine (Plaquenil), or if you have a history of vision changes or damage to your retina caused by chloroquine or similar anti-malaria medications.

To make sure chloroquine is safe for you, tell your doctor about your other medical conditions, especially:

• psoriasis;
• porphyria;
• liver disease;
• alcoholism;
• epilepsy or other seizure disorder;
• glucose-6-phosphate dehydrogenase (G6PD) deficiency; or
• a history of problems with your vision or hearing.

It is not known whether chloroquine will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant while using this medication.

Malaria is more likely to cause death in a pregnant woman. If you are pregnant, talk with your doctor about the risks of traveling to areas where malaria is common.

It is not known whether chloroquine passes into breast milk or if it could harm a nursing baby. You should not breast-feed while you are using chloroquine.

Your pharmacist can provide more information about chloroquine.

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.

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Special Senses

Maculopathy and macular degeneration have been reported and may be irreversible (see WARNINGS); irreversible retinal damage in patients receiving long-term or high-dosage 4-aminoquinoline therapy; visual disturbances (blurring of vision and difficulty of focusing or accommodation); nyctalopia; scotomatous vision with field defects of paracentral, pericentral ring types, and typically temporal scotomas, e.g., difficulty in reading with words tending to disappear, seeing half an object, misty vision, and fog before the eyes. Reversible corneal opacities have also been reported.

Nerve type deafness; tinnitus, reduced hearing in patients with preexisting auditory damage.

Skeletal muscle myopathy or neuromyopathy leading to progressive weakness and atrophy of proximal muscle groups, which may be associated with mild sensory changes, depression of tendon reflexes and abnormal nerve conduction, have been noted.

Hepatitis, increased liver enzymes, anorexia, nausea, vomiting, diarrhea, abdominal cramps.

Rare reports of erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, exfoliative dermatitis and similar desquamation-type events. Pleomorphic skin eruptions, skin and mucosal pigmentary changes; lichen planus-like eruptions, pruritus, urticaria, anaphylactic/anaphylactoid reaction including angioedema; drug rash with eosinophilia and systemic symptoms (DRESS syndrome); photosensitivity and hair loss and bleaching of hair pigment.

Rarely, pancytopenia, aplastic anemia, reversible agranulocytosis, thrombocytopenia and neutropenia.

Convulsive seizures, mild and transient headache, polyneuritis. Acute extrapyramidal disorders (such as dystonia, dyskinesia, tongue protrusion, torticollis) (see WARNINGS and OVERDOSAGE). Neuropsychiatric changes including psychosis, delirium, anxiety, agitation, insomnia, confusion, hallucinations, personality changes, and depression.

Rarely, hypotension, electrocardiographic change (particularly, inversion or depression of the T-wave with widening of the QRS complex), and cardiomyopathy.

Read the entire FDA prescribing information for Aralen (Chloroquine)