Pharm
Hydroxychloroquine
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Hydroxychloroquine
, Plaquenil
See Also
Disease Modifying Antirheumatic Drug
Rheumatoid Arthritis
Malaria
Indications
Second-Line
DMARD
in
Rheumatoid Arthritis
Especially
Antinuclear Antibody
positive
May be used in triple combination with
Methotrexate
and
Sulfasalazine
Indicated in moderate to severe disease refractory to single conventional synthetic
DMARD
Systemic Lupus Erythematosus
Malaria Prophylaxis
and treatment
Regions without
Chloroquine
resistance, non-severe infections
Rheumatologic off-label uses
Dermatomyositis
Sjogren Syndrome
Sarcoidosis
Infectious off-label uses
Q Fever
NOT indicated in
COVID-19
outside of
Clinical Trial
s
Initial studies as of May 2020 suggest no benefit and adverse effect risk (including
QTc Prolongation
)
Contraindications
G6PD Deficiency
Risk of
Hemolytic Anemia
Mechanism
Antimalarial agent used in rheumatic disease
Modified
Chloroquine
to reduce
Retinopathy
risk
Blocks
Sodium
and
Potassium
channels
Dosing
Rheumatologic Disorder
s
Varies significantly based on use
Lower doses are used in infectious disease
Dosing: Adults
Initial: 400 to 600 mg (may consider starting at 200 mg) orally twice daily
Maximum: 600 mg/day
Expect symptom improvement by 2 to 4 months (discontinue if no effect by 6 months)
Taper after 1-2 years when stable to 200 mg orally daily
Dosing
Malaria
Malaria Prophylaxis
Start 1-2 weeks before travel and continue for 4 weeks after leaving
Malaria
endemic region
Adult: 400 mg salt (310 mg base) orally once weekly
Child: 6.5 mg/kg salt (5 mg/kg base up to adult dose) orally once weekly
Malaria
Treatment
Adult: 800 mg salt (620 mg base) to start, then 400 mg salt (310 mg base) at 6, 24 and 48 hours after initial dose
Child: 12.9 mg/kg salt (10 mg/kg base) to start, then 6.5 mg/kg salt (5 mg/kg mg base) at 6, 24 and 48 hours after initial dose
Precautions
One tablet may be lethal in children (lethal dose 30 mg/kg)
Considered safe in pregnancy (all trimesters), despite initially labeled category D
Adverse Effects
Eye-related Adverse Effects
Epithelial Keratopathy and other
Cornea
l disorders
Retinopathy
Uncommon to Rare (contrast with
Chloroquine
)
Neurologic adverse effects
Early toxicity (subsides within 2 weeks)
Irritability
Insomnia
Headache
Late toxicity requires medication discontinuation
Tinnitus
Decreased Hearing
acuity
Very rare toxicity
Myopathy
or muscular weakness
Other adverse effects
Confusion or
Delirium
Extrapyramidal Side Effect
s
Hallucination
s
Seizure
s
Gastrointestinal adverse effects
Increased stool frequency
Diarrhea
Bloating
Nausea
or
Vomiting
Endocrine Adverse Effects
Hypoglycemia
Hematologic Adverse Effects
Neutropenia
Pancytopenia
Electrolyte
adverse effects
Hypokalemia
(in toxicity)
Cardiovascular adverse effects
Palpitation
s
Hypotension
(in toxicity)
Premature Atrial Contraction
s
Cardiomyopathy
QRS Widening
(in toxicity)
QTc Prolongation
(with risk of
Ventricular Tachycardia
or
Drug-Induced Torsades de Pointes
)
Increased risk when combined with other agents causing
QTc Prolongation
(e.g.
Azithromycin
)
Pharmacokinetics
Onset: 2-4 hours after oral dose
Half-Life
: 20 to 40 days
Lethal dose in young children as low as 750 mg
Efficacy
Rheumatoid Arthritis
Response in 70-80% of cases
Response occurs in 3-6 months
Highest efficacy when used early in disease process
Safety
Considered safe in
Lactation
In pregnany, use if benefit outweighs risk
Monitoring
Routine
Eye Exam
every 6-12 months (including a baseline exam)
Complete Blood Count
(CBC) periodically
Management
Hydroxychloroquine
Overdose
or Toxicity
See
ABC Management
Activated Charcoal
if <1 hour from ingestion and patient maintaining own airway
Ventricular
Arrhythmia
Cardioversion
Lidocaine
Wide QRS
Bicarbonate (caution if
Hypokalemia
)
Hypokalemia
Potassium Replacement
(caution)
Seizure
s
Benzodiazepine
s
Hypotension
Norepinephrine
Other measures
ECMO
(refractory cardiovascular failure)
Resources
Hydroxychloroquine Tablet (DailyMed)
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=452092b4-7a8f-4d19-8113-f1c2a948d3d8
References
(2020) LexiComp, Hydroxychloroquine, accessed 5/6/2020
Tomaszekski (2020) Crit Dec Emerg Med 14(4):32
Matteson (2000) Mayo Clin Proc 75:669-74 [PubMed]
Pincus (1999) Clin Rheumatol 17(6 Suppl 18):S2-S124 [PubMed]
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