about Chloroquine class, uses, side effects contraindications
Chloroquine
Short Description
Hydroxychloroquine is primarily given to prevent and treat?malaria??but is not effective against all types of malaria.
It is also usually given in combination with other drugs to treat a number of autoimmune diseases, such as: systemic lupus erythematosus and rheumatoid arthritis. Hydroxychloroquine treatment for these diseases is usually given as a second line after the failure of the first-line drugs. in treating these diseases.
The drug is effective in patients with SLE against skin symptoms, and against arthritis.
Hydroxychloroquine is not intended for prolonged use in children and is permitted in patients with G6PD deficiency, but should be used with caution in these patients;?Because it and other antimalarials can cause?hemolytic?anemia in these patients.
Chloroquine is used to prevent and treat malaria. When this drug is taken orally, the drug is quickly absorbed and eliminates the disease within three days. As a precaution when going to an endemic area, the drug is given in a reduced dose.
Common side effects include: nausea, headache, diarrhea, abdominal cramps, and sometimes a rash. One of the most serious effects of chloroquine is its ability to damage the retina when taken continuously.
Category
Chemical class: 4-aminoquinoline compound
Therapeutic class: Antiprotozoal, antirheumatic, lupus erythematosus suppressant
Pregnancy category: C
Indications
To prevent malaria
Adults. 400 mg the same day of each week starting 2 wk before entering endemic area and continuing until departure from endemic area. If this isn’t possible, initially 800 mg in two divided doses 6 hr apart, followed 1 wk later with 400 mg and then 400 mg on same day of each week thereafter until departure from endemic area. Infants and children. 5 mg/kg the same day of each week, starting 2 wk before entering endemic area and continuing until departure from endemic area. If this isn’t possible, initially 10 mg/kg in two divided doses 6 hr apart, followed 1 wk later with 5 mg/kg and then 5 mg/kg on same day of each week thereafter until departure from endemic area. Maximum: Adult dosage. To treat acute attacks of malaria caused by Plasmodium vivax, P. malariae, P. ovale, and susceptible strains of P. falciparum
Adults. Initial: 800 mg, followed by 400 mg in 6 to 8 hr and 400 mg on next 2 consecutive days. Or, 800 mg given as a single dose or an initial dose of 10 mg base/kg (maximum, 620 mg base [800 mg]), followed by 5 mg base/kg (maximum, 310 mg base [400 mg]) 6 hr after first dose, 5 mg base/kg 18 hr after second dose, and 5 mg base/kg 24 hr after third dose. Infants and children. Initial: 10 mg base/kg (maximum, 620 mg base [800 mg]), followed by 5 mg base/kg (maximum, 310 mg base [400 mg]) 6 hr after first dose, 5 mg base/kg 18 hr after second dose, and 5 mg base/kg 24 hr after third dose. To treat chronic discoid and systemic lupus erythematosus
Adults. Initial: 400 mg once or twice daily for several weeks or months. Maintenance: 200 to 400 mg daily. To treat acute or chronic rheumatoid arthritis
Adults. Initial: 400 to 600 mg daily for 4 to 12 wk. Maintenance: 200 mg to 400 mg daily.
DOSAGE ADJUSTMENT For patients with rheumatoid arthritis who develop troublesome
Side Efect
, initial dosage decreased for 5 to 10 days and then gradually increased to optimum response level.
Mechanism of Action
May mildly suppress the immune system, inhibiting production of rheumatoid factor and acute phase reactants. Hydroxychloroquine also accumulates in WBCs, stabilizing lysosomal membranes and inhibiting enzymes such as collagenase and proteases that cause cartilage breakdown. These actions may decrease symptoms of rheumahydroxychloroquine sulfate 511 G H I toid arthritis and lupus erythematosus. Hydroxychloroquine also binds to and alters DNA of malaria parasite to prevent it from reproducing. It also may increase the pH of acid vesicles, which interferes with vesicle function and may inhibit parasitic phospholipid metabolism in erythrocytes, thereby halting plasmodial activity.
Contraindications
Hypersensitivity to 4-aminoquinoline compounds (including hydroxychloroquine), long-term therapy in children, retinal or visual changes related to 4-aminoquinoline compounds
Interactions
aurothioglucose: Increased risk of blood dyscrasias digoxin: Increased digoxin concentrations
Side Efect
CNS: Abnormal nerve conduction, ataxia, dizziness, emotional lability, headache, irritability, lassitude, nervousness, neuromuscular sensory abnormalities, nightmares, psychosis, seizures, vertigo
CV: Cardiomyopathy (prolonged high doses)
EENT: Abnormal pigmentation (bullseye appearance) or colored vision, blurred vision, central scotoma with decreased visual acuity, corneal deposits, decreased corneal sensitivity, diplopia, irreversible retinal damage (in lupus erythematosus or rheumatoid arthritis), halo vision, lassitude, macular edema or atrophy, nerve-related hearing loss, nystagmus, pericentral or paracentral scotoma, photophobia, retinal fundus changes, tinnitus, visual abnormalities
ENDO: Hypoglycemia
GI: Abdominal cramps, anorexia, diarrhea, elevated liver function test results, fulminant hepatic failure, nausea, vomiting
HEME: Agranulocytosis, aplastic anemia, hemolysis (in patients with glucose-6-phosphate dehydrogenase [G6PD] deficiency), leukopenia, thrombocytopenia
MS: Atrophy of proximal skeletal muscle groups, depressed tendon reflexes, muscle weakness
RESP: Bronchospasm
SKIN: Acute generalized exanthematous pustulosis, alopecia, altered mucosal and skin pigmentation, bleaching of hair, dermatitis (including exfoliative dermatitis), non–light-sensitive psoriasis, pruritus, psoriasis exacerbation, rash, Stevens-Johnson syndrome, urticaria
Other: Angioedema, porphyria, weight loss
Cautions
Use hydroxychloroquine cautiously in patients with G6PD deficiency, patients with hepatic disease or alcoholism, and patients taking hepatotoxic . Monitor children closely for adverse reactions because they’re especially sensitive to 4-aminoquinoline compounds. Observe patients with psoriasis closely because hydroxychloroquine may lead to severe psoriasis attack. Also monitor patients with porphyria closely because hydroxychloroquine may worsen it. Expect to use hydroxychloroquine in patients with psoriasis or porphyria only after risks and benefits have been considered. During prolonged therapy, obtain periodic blood cell counts, as ordered, to detect adverse hematologic effects. Expect to stop drug if severe adverse effects occur. Monitor patient’s vision when giving hydroxychloroquine for lupus erythematosus or rheumatoid arthritis because irreversible retinal damage may occur in some patients during long-term or high-dose therapy. Ask regularly about vision abnormalities, such as light flashes or streaks, that may indicate retinopathy. Expect patient to have an initial ophthalmologic examination, followed by examinations every 3 months. Report changes to prescriber immediately, and expect drug to be stopped. Retinal changes may progress even after therapy stops. Monitor patient on long-term therapy for muscle weakness and abnormal knee and ankle reflexes. If present, notify prescriber and expect drug to be stopped. Expect drug to be stopped if patient with rheumatoid arthritis shows no improvement, such as reduced joint swelling or increased mobility, in 6 months. If serious Side Efect
occur, notify prescriber immediately. Expect drug to be stopped. Also expect to give ammonium chloride (8 g daily in divided doses for adults) 3 or 4 days weekly for several months because acidification of urine hydroxychloroquine sulfate 512 increases renal excretion of drug. PATIENT SAFTY
Instruct patient to take drug with meals or milk to minimize stomach upset. Tell patient to take hydroxychloroquine exactly as prescribed because taking too much may cause serious Side Efect
and taking too little or skipping doses decreases effectiveness. Caution patient to notify prescriber about troublesome Side Efect
. Hydroxychloroquine dosage may need to be adjusted or drug stopped. Caution patient who takes drug for rheumatoid arthritis or lupus erythematosus about possible visual reactions and the need for periodic eye examinations. Tell patient to notify prescriber about abnormal visual changes, including blurred vision, halos around lights, and light flashes or streaks; explain that drug will need to be stopped. Tell patient receiving prolonged therapy about the need for periodic blood tests to detect adverse effects. Advise patient to notify prescriber if muscle weakness develops.
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effect of Chloroquine in Pregnancy, Fetal Health
and Breast feeding
Pregnancy
. There are no adequate reports or well-controlled studies in pregnant women. Hydroxychloroquine reduces serum lipids, including cholesterol, triglycerides, and LDLs. Some recommend discontinuing hydroxychloroquine in pregnant women with connective tissue diseases, even though it has long been used for malarial prophylaxis during Pregnancy
in malaria-infested areas. In one randomized trial, hydroxychloroquine was associated with a significant reduction in the number of flare episodes in women with SLE. Thus, it may be reasonable to continue the drug considering the terminal elimination t/2 may be up to 2mo, flares of SLE occur after discontinuation, and flares are detrimental to Pregnancy
outcome. Fetal Health
There are no adequate reports or well-controlled studies in human fetuses. While there is no substantive evidence of teratogenicity in rodents, hydroxychloroquine crosses the placenta and is deposited in pigmented fetal tissues. However, several large clinical series in women with either malaria or SLE are reassuring. Breastfeeding
There are no adequate reports or well-controlled studies in nursing women. The concentration of hydroxychloroquine entering human breast milk is apparently very low (3.2mcg in breast milk from a woman given 800mg over 48h) and should not pose a threat to the breastfed newborn. Pregnancy
. Chloroquine is closely related to hydroxychloroquine and has similar uses. A body of clinical experience suggests chloroquine is safe during Pregnancy
and improves outcome in women with active disease. In one study of 96 women with active malaria, chloroquine (10mg/kg) was given at time 0 and 24h and again at 48h (5mg/kg). The Tmaxafter the first dose was 3.5h, whereas plasma concentrations (CPmax) at 2, 28, and 52h were 204.36, 343.51, and 257.04ng/ml respectively. There was total parasitemia clearance before the end of 96h in all the subjects. In another study, the conversion of chloroquine to its major metabolite, desethylchloroquine, was increased in the 3rd trimester, suggesting the need for caution when considering the use of higher doses. Current study suggests there are more effective treatment options. Chloroquine is also used as an adjunct for the treatment of SLE in women who have failed to respond to first-line agents. Recent studies suggest it may have a role in the treatment of HIV, and thus may have a role in HIV-infected Side effects include agranulocytosis, thrombocytopenia, aplastic anemia, dermatitis, ototoxicity, vomiting, dizziness, diarrhea, and pruritus. Fetal Health
Chloroquine crosses the placenta, achieving an F:M ratio approximating 0.7-0.8. Fetal retinopathy was noted in some animal studies, but more recent investigation casts doubt on the association and suggests it is safe during the 1st trimester. No increase in spontaneous abortion or major birth defects is reported in humans. Breastfeeding Chloroquine enters human breast milk, achieving an M:P ratio ranging from 0.268 to 0.462. Some studies suggest it may actually be concentrated. However, it is generally considered compatible with breastfeeding.
the follwing drugs will increse Chloroquine by inhepiting cyp450
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the follwing drugs will decrease Chloroquine by inhancing cyp450
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trad drugs based on Chloroquine
| Gen name | Trade name | Catagory name |
| Chloroquine | CHLOROQUIN PHOSPHATE 80MG/5ML SYRUR | |
| Chloroquine | CHLOROQUINE | |
| Chloroquine | MALAREX SYRUP 120MG-5ML | |
| Chloroquine | MALAREX TABLETS 250mg | |
| Chloroquine | RESOCHIN TAB 250MG | |
| Hydroxychloroquine | PLAQUENIL 200MG TAB | |
other drugs from same cataogory
| Gen name | trade name | catogry |