Hydroxychloroquine (Dosing, Interaction, Side Effect, Administration, Etc..)

Adult Dose

:
General Dosage Information:
Each 200-mg

tablet of hydroxychloroquine sulfate

is equivalent to 155 mg base

Lupus erythematosus:

200

to

400 mg

orally once daily or divided twice daily; MAX 400 mg/day

Malaria:
Initial, 800 mg orally for 1

dose

followed by

400 mg

at 6, 24, and 48 hours after the

initial dose

(FDA

dosage

)
(Weighing greater than 31 kg) Weight-based dosage: 13 mg/kg (MAX, 800 mg) orally for 1 dose, followed by 6.5 mg/kg (MAX, 400 mg) orally at 6, 24, and 48 hours after the

first dose

(

FDA dosage

)
Concomitant medication (Plasmodium vivax or P ovale malaria), give in combination with primaquine phosphate 52.6 mg orally daily for 14 days (

guideline dosage

)

Malaria; Prophylaxis:

400 mg orally once weekly

on the same day each week beginning 2 weeks prior to travel to malarious area, continue on same day each week while in area and for 4 weeks after leaving area (FDA dosage)
Weight-based dosage: 6.5 mg/kg (MAX 400 mg) orally once weekly on the same day each week beginning 2 weeks prior to travel to malarious area, continue on same day each week while in area and for 4 weeks after leaving area (FDA dosage)

400 mg orally

once weekly beginning 1 to 2 weeks prior to travel to malarious area; continue on same day each week while in area and for 4 weeks after leaving area (guideline dosage)

Rheumatoid arthritis:
Initial,

400 to 600 mg orally once daily

or divided twice daily; maintenance, when a good response is obtained,

dosage may be reduced

50% to 200 to

400 mg once daily

or divided twice daily; MAX 600 mg or 6.5 mg/kg daily, whichever is lower

Pediatric Dose

:
General Dosage Information:
Each 200-mg

tablet of hydroxychloroquine

sulfate is equivalent to 155 mg base

Malaria:
(Greater than 31 kg) 13 mg/kg (MAX, 800 mg) orally for 1 dose, followed by 6.5 mg/kg (MAX,400 mg) orally at 6, 24, and 48 hours after the first dose (FDA dosage)
Concomitant medication (P vivax or P ovale malaria) give in combination with primaquine phosphate 0.8 mg/kg orally daily for 14 days (guideline dosage)

Malaria; Prophylaxis:
6.5 mg/kg (

MAX 400 mg

) orally once weekly on the same day each week beginning 2 weeks prior to travel to malarious area, continue on same day each week while in area and for 4 weeks after leaving area (

FDA dosage

)
6.45 mg/kg orally once weekly beginning 1 to 2 weeks prior to travel to malarious area; continue on same day each week while in area and for 4 weeks after leaving area;

Maximum dose

, 400 mg (

guideline dosage

)

Indications:
FDA-Labeled Indications:
Lupus erythematosus
Malaria
Malaria; Prophylaxis
Rheumatoid arthritis

Contraindications:
Hypersensitivity to 4-aminoquinoline compounds

Precautions:
Cardiovascular:
Cardiomyopathy, with fatalities, has been reported; monitoring suggested and discontinue

use

if suspected QT prolongation, ventricular arrhythmias, and torsades de pointes have been reported

Concomitant use:
Avoid

use with

other drugs that prolong QT interval

Dermatologic:
Severe exacerbation of psoriasis may occur; use not recommended
Dermatologic reaction may occur, particularly with concomitant

use of drugs

that have tendency to produce dermatitis

Endocrine and metabolic:
Severe and potentially life-threatening hypoglycemia, with loss of consciousness, may occur in patients treated with or without antidiabetic medications

Hematologic:
Porphyria may be exacerbated; use not recommended
Severe blood disorders, including aplastic anemia, agranulocytosis, leukopenia, and thrombocytopenia, may occur; monitoring recommended with prolonged therapy; consider discontinuation

Hepatic:
Give cautiously to patients with liver disease, alcoholism, or concomitant use of known hepatotoxic drugs;

dose adjustment

may be necessary

Musculoskeletal:
Proximal myopathy has been reported; monitoring recommended, especially with long-term therapy

Neurologic:
Neuropathy has been reported; monitoring recommended, especially with long-term therapy

Ophthalmic:
Irreversible retinal damage has been reported; increased risk in patients receiving doses larger than 6.5 mg/kg, duration of use greater than 5 years, subnormal glomerular filtration,

use of

tamoxifen citrate, or concurrent macular disease. Monitoring recommended, even after discontinuation of therapy, and discontinue

use if

suspected

Psychiatric:
Suicidal behavior, although rare, has been reported

Pregnancy Category:
Hydroxychloroquine: D (AUS)

Breastfeeding:
AAP:
Maternal medication usually compatible with breastfeeding.
Infant risk is minimal.

Drug interactions:
Contraindicated:
Aurothioglucose (theoretical)
Bepridil (probable)
Cisapride (probable)
Dronedarone (probable)
Mesoridazine (probable)
Pimozide (probable)
Piperaquine (probable)
Saquinavir (probable)
Sparfloxacin (probable)
Terfenadine (probable)
Thioridazine (probable)
Ziprasidone (probable)

Major:
Alfuzosin (probable)
Amiodarone (theoretical)
Amisulpride (theoretical)
Amitriptyline (probable)
Anagrelide (probable)
Apomorphine (probable)
Aripiprazole (probable)
Aripiprazole Lauroxil (theoretical)
Arsenic Trioxide (probable)
Asenapine (probable)
Astemizole (probable)
Atazanavir (probable)
Auranofin (theoretical)
Azithromycin (probable)
Bedaquiline (probable)
Buprenorphine (theoretical)
Buserelin (probable)
Ceritinib (theoretical)
Chloroquine (probable)
Chlorpromazine (probable)
Ciprofloxacin (probable)
Citalopram (probable)
Clarithromycin (probable)
Clofazimine (theoretical)
Clomipramine (probable)
Clozapine (probable)
Crizotinib (probable)
Cyclobenzaprine (probable)
Dabrafenib (probable)
Dasatinib (probable)
Degarelix (probable)
Delamanid (probable)
Desipramine (probable)
Deslorelin (probable)
Deutetrabenazine (theoretical)
Disopyramide (probable)
Dofetilide (probable)
Dolasetron (probable)
Domperidone (probable)
Donepezil (probable)
Doxepin (probable)
Droperidol (probable)
Ebastine (probable)
Efavirenz (theoretical)
Encorafenib (theoretical)
Entrectinib (theoretical)
Eribulin (probable)
Erythromycin (probable)
Escitalopram (probable)
Famotidine (probable)
Felbamate (probable)
Fingolimod (probable)
Flecainide (probable)
Fluconazole (probable)
Fluoxetine (probable)
Formoterol (probable)
Foscarnet (probable)
Fosphenytoin (probable)
Galantamine (probable)
Gatifloxacin (probable)
Gemifloxacin (probable)
Glasdegib (theoretical)
Gonadorelin (probable)
Goserelin (probable)
Granisetron (probable)
Halofantrine (probable)
Haloperidol (probable)
Histrelin (probable)
Hydroquinidine (probable)
Hydroxyzine (theoretical)
Ibutilide (probable)
Iloperidone (probable)
Imipramine (probable)
Inotuzumab Ozogamicin (theoretical)
Itraconazole (probable)
Ivabradine (probable)
Ivosidenib (theoretical)
Ketoconazole (probable)
Lapatinib (probable)
Lefamulin (theoretical)
Lenvatinib (theoretical)
Leuprolide (probable)
Levofloxacin (probable)
Lofexidine (probable)
Lumefantrine (probable)
Macimorelin (theoretical)
Mefloquine (probable)
Methadone (probable)
Methotrimeprazine (probable)
Metronidazole (probable)
Mifepristone (probable)
Mizolastine (probable)
Moricizine (probable)
Moxifloxacin (probable)
Nafarelin (probable)
Nelfinavir (probable)
Nilotinib (probable)
Norfloxacin (probable)
Octreotide (probable)
Ofloxacin (probable)
Olanzapine (probable)
Ondansetron (probable)
Osimertinib (theoretical)
Paliperidone (probable)
Panobinostat (theoretical)
Paroxetine (probable)
Pasireotide (probable)
Pazopanib (probable)
Pentamidine (probable)
Perphenazine (probable)
Pimavanserin (theoretical)
Pipamperone (probable)
Pitolisant (theoretical)
Posaconazole (probable)
Probucol (probable)
Procainamide (probable)
Prochlorperazine (probable)
Promethazine (probable)
Propafenone (probable)
Protriptyline (probable)
Quetiapine (theoretical)
Quinidine (probable)
Quinine (probable)
Ranolazine (probable)
Ribociclib (theoretical)
Rilpivirine (probable)
Risperidone (probable)
Ritonavir (probable)
Sertindole (probable)
Sertraline (theoretical)
Sevoflurane (probable)
Siponimod (theoretical)
Sodium Phosphate (probable)
Sodium Phosphate, Dibasic (probable)
Sodium Phosphate, Monobasic (probable)
Solifenacin (probable)
Sorafenib (probable)
Sotalol (theoretical)
Sulpiride (theoretical) Sultopride (probable)
Sunitinib (probable)
Tacrolimus (probable)
Tamoxifen (probable)
Telaprevir (probable)
Telavancin (probable)
Telithromycin (probable)
Tetrabenazine (probable)
Tizanidine (probable)
Tolterodine (probable)
Toremifene (probable)
Trazodone (probable)
Triclabendazole (theoretical)
Trimipramine (probable)
Triptorelin (probable)
Vandetanib (probable)
Vardenafil (probable)
Vemurafenib (probable)
Venlafaxine (probable)
Vilanterol (probable)
Vinflunine (probable)
Voriconazole (probable)
Vorinostat (probable)
Zotepine (probable)
Zuclopenthixol (theoretical)

Moderate:
Digoxin (probable)

Adverse effects:
Serious:
Cardiovascular:
Torsades de pointes

Endocrine metabolic:
Hypoglycemia (Severe)

Hematologic:
Agranulocytosis
Aplastic anemia
Thrombocytopenia

Musculoskeletal:
Disorder of muscle

Ophthalmic:
Retinal disorder (7.5%)

Otic:
Hearing loss

Other:
Angioedema




Mechanism of actions:
Systemic:
Antiprotozoal-Malaria: Unknown, but may be based on ability

hydroxychloroquine

to bind to and alter the properties of DNA. Also has been found to be taken up into the acidic food vacuoles of the parasite in the erythrocyte. This increases the pH of the acid vesicles, interfering with vesicle functions and possibly inhibiting phospholipid metabolism. In suppressive treatment, hydroxychloroquine inhibits the erythrocytic stage of development of plasmodia . In acute attacks of malaria, it interrupts erythrocytic schizogony of the parasite. Its ability to concentrate in parasitized erythrocytes may account for their selective toxicity against the erythrocytic stages of plasmodial infection.

Antirheumatic-Hydroxychloroquine is thought to act as a mild immunosuppressant, inhibiting the production of rheumatoid factor and acute phase reactants. It also accumulates in white blood cells, stabilizing lysosomal membranes and inhibiting the activity of many enzymes, including collagenase and the proteases that cause cartilage breakdown .

Pharmacokinetics:
Absorption:
Tmax, oral: 2.4 to 3.2 hours
Bioavailability, oral: 74.6%

Distribution:
Vd: 5522 L (blood); 44,257 L (plasma)
Vd (rheumatoid arthritis): 153 to 1650 L

Metabolism:
Hydroxychloroquine, Liver: extensive
Bisdesethylhydroxychloroquine: Active
Desethylchloroquine: Active
Desethylhydroxychloroquine: Active

Excretion:
Renal: 16 to 62% unchanged
Total body clearance: 9.8 to 45.1 L/hour

Elimination Half Life:
172.3 hours to 50 days

Administration:
Oral:
Take with food or milk

Monitoring:
Malaria:
Termination of acute malarial attack or absence of or reduced malarial parasite count on blood smear may indicate efficacy.

Systemic lupus erythematosus/rheumatoid arthritis:
Improvement in C-reactive protein levels and erythrocyte sedimentation rate may indicate efficacy.

Systemic lupus erythematosus/rheumatoid arthritis:
Resolution of signs and symptoms, improved range of motion, decreased early morning stiffness and painful/swollen joints may indicate efficacy.

Cutaneous lupus erythematosus:
Hydroxychloroquine blood concentrations, especially in unresponsive patients

Complete blood cell counts:
Periodically during prolonged therapy

Renal function:
In elderly patients

Ophthalmologic examinations:
Baseline; repeat annually in high risk patients, and every 5 years in patients without significant risk factors

Clinical signs and symptoms of cardiomyopathy, including use of appropriate diagnostic tools, such as ECG:
During treatment

Muscle strength and deep tendon reflexes:
Periodically during prolonged therapy

Clinical Teaching:
Side effects may include vertigo, tinnitus, visual field defects, color vision abnormalities, nausea, vomiting, fatigue, decreased appetite, headaches, dizziness, and irritability.
Tell patient to report symptoms of toxicity (eg, rash or visual changes).
Instruct patient to take drug with a meal or glass of milk.




Disclaimer:
For the Registered Medical Practitioner Only. We are not recommended for self medication. self medication is may harmful for health. We are only information about medicine.