Details of Hydroxychloroquine Sulfate Medicine Tablets usable for COVID-19 treatment
Common name:
hydroxychloroquine sulfate tablets
Product Name:
Hydroxychloroquine Sulfate Tablets (Fanle)
English name:
Hydroxychloroquine Sulfate Tablets
Main ingredients: Hydroxychloroquine sulfate.
Chemical name:
2-[[4-[(7-chloro-4-quinolinyl) amino] pentyl] ethylamino] -ethanol sulfate
Molecular weight:
C18H28ClN3O
Properties: This product is a film-coated tablet, which is
white or almost white after removing the coating.
Indications / Functional indications: This product is used
for the following diseases that are not satisfied with the potential serious
effects of drugs: rheumatoid arthritis, juvenile chronic arthritis, discoid
lupus erythematosus and systemic lupus erythematosus, and caused by sunlight Or
exacerbated skin lesions.
[pecification model: 0.1g * 14 tablets (Funle)
What is the Usage and Dosage of Hydroxychloroquine Sulfate?
Oral The first dose for adults (including
the elderly) is 0.4g each time, taken in divided doses. When the efficacy is no
longer improved, the dose can be reduced to 0.2g to maintain. During
maintenance, if the treatment response weakens, the maintenance dose should be
increased to 0.4 g per day. For details, please refer to the instruction
manual.
What are the Adverse Reactions of Hydroxychloroquine Sulfate?
4-Aminoquinoline compounds may undergo
the following reactions during long-term treatment, but the types and incidence
of adverse reactions of different compounds may be different.
(1) Central
nervous system reactions: excitement, nervousness, mood changes, nightmares,
mental illness, headache, dizziness, dizziness, tinnitus, nystagmus,
neurological deafness, convulsions, ataxia.
(2) Neuromuscular reaction:
extraocular muscle paralysis, skeletal muscle weakness, deep tendon reflex
disappeared or decreased.
(3) Eye reaction:
i. Ciliary body: dysregulation with symptoms of blurred
vision. This response is dose-dependent and can be reversed after withdrawal.
ii. Cornea: transient edema, punctate to linear turbidity,
decreased corneal sensitivity. Common reversible corneal changes with or without
symptoms (blurred vision, halos around the light, photophobia). Keratosis may
have appeared as early as 3 weeks after starting treatment. The incidence of
corneal changes and visual side effects of hydroxychloroquine seems to be much
lower than that of chloroquine.
iii. Retina: macular edema, atrophy, abnormal pigmentation
[the appearance of "bull" s-eye "in light pigment spots], the
foveal reflection disappeared, and after exposure to bright light (light stress
test) Macular recovery time increases, and the retinal threshold for red light
in the macular, paramacular, and surrounding retinal areas increases.
Other
fundus changes include paleness and atrophy of the optic nerve head, thinning
of the arterioles of the retina, disorder of fine-grained pigments around the
retina, and the appearance of a protruding choroid at a later stage.
iv. Visual field
defect: blind spots around or near the center, blind spots with reduced visual
acuity, and rare visual stenosis.
The most common visual symptoms attributed to
retinopathy are: difficulty reading and seeing (missing words, letters, or
parts of objects), photophobia, blurred vision from a distance, blurred or
darkened areas in the center or surrounding visual field, flashes and scratches
line.
Retinopathy appears to be dose-related and occurs from several months
(rare) to several years of treatment once a day; a few cases have been reported
years after the antimalarial treatment stopped.
The 4-aminoquinoline compound
was used to treat malaria once a week, and no retinopathy was seen in long-term
application. Patients with retinal changes may have visual symptoms or no
symptoms (with or without visual field changes), and visual blind spots or
visual field defects without retinal changes are rare.
Retinopathy will progress
even after the drug is stopped. There are many patients with early retinopathy
(macular pigmentation, sometimes with central and visual field defects) that
completely disappear or relieve after treatment is stopped.
The appearance of a
central and parablind spot (sometimes called: anterior macular degeneration) on
the red optotype is a sign of early retinal dysfunction, which is usually
reversible after drug withdrawal.
A few cases of retinal changes have been
reported in patients who received only hydroxychloroquine, usually including
changes in retinal pigmentation found during regular eye examinations, and
visual defects in some cases.
One case of delayed retinopathy with visual loss
has been reported, occurred after discontinuation of hydroxychloroquine.
iv. Skin reactions: hair whitening, hair loss, itching, skin and mucous membrane
pigmentation, rashes (urticaria, measles-like, moss-like, maculopapular,
purpura, centrifugal circular erythema and exfoliative dermatitis).
v. Hematological reactions: such as individuals with aplastic
anemia, agranulocytosis, leukopenia, thrombocytopenia, and glucose-6-phosphate
dehydrogenase (G-6-PD) deficiency.
vi. Gastrointestinal reactions: loss of appetite, nausea,
vomiting, diarrhea and abdominal cramps.
vii. Others: weight loss, burnout, deterioration or
acceleration of porphyria, and non-photosensitive psoriasis. Local reports of
rare cardiomyopathy, its relationship with hydroxychloroquine is not yet clear.
Contraindication (Hydroxychloroquine Sulfate)
(1) It is contraindicated in patients with retina or visual
field changes caused by 4-aminoquinoline compound treatment;
(2) patients who are known to be allergic to 4-aminoquinoline
compound are contraindicated.
(3) Pregnant women and lactating women are prohibited.
What should be kept in mind while taking Hydroxychloroquine Sulfate?
(1) This product should be placed out of reach of children.
(2) The use of this product in patients with psoriasis and
porphyria can aggravate the original disease.
Therefore, this product should not be used in these patients,
unless according to the judgment of the physician, the patient's benefit will
exceed its possible risks.
(3) The physician should be fully familiar with the
entire contents of this manual before prescribing this product.
(4) Some
patients receiving long-term or high-dose treatment have been observed to have
irreversible retinal damage. Retinopathy has been reported to be
dose-dependent.
(5) Take this product for initial (baseline) and regular (once
every 3 months) eye examinations (including visual acuity, slit lamp output, ophthalmoscopy
and visual field examination).
(6) If there are any abnormal signs of visual
acuity, visual field or macular area of the retina (such as pigment changes,
loss of foveal reflex) or any visual symptoms (such as flashes and streaks),
and cannot be adjusted with difficulty or corneal opacity completely.
When
interpreting, the drug should be stopped immediately and the possible progress
should be closely observed. Even after stopping treatment, retinal changes (and
visual disturbances) may still progress.
(7) All patients treated with this
product for long-term treatment should be regularly followed up and checked,
including examination of knee and ankle reflexes, as well as any signs of
muscle weakness. If muscle weakness is found, the drug should be discontinued.
(8) Patients with liver disease or alcoholism, or when combined with drugs
known to have liver toxicity, should be used with caution.
(9) For patients who
have been treated with this product for a long time, blood count should be
performed regularly. If there are any serious blood disorders that cannot be
attributed to the disease being treated, you should consider stopping the
medication. Patients who lack G-6-PD (glucose-6-phosphate dehydrogenase) should
use this drug with caution.
(10) Skin reactions may occur when taking this
product. Therefore, due attention should be paid to any patients receiving
drugs that have a clear tendency to produce dermatitis.
(11) Recommended
methods for early diagnosis of "hydroxychloroquine sulfate retinopathy"
include:
i. Use ophthalmoscope to check the macular for subtle pigment disorders
or loss of foveal reflex, and
ii. Use a small red optotype to check the center
and see if the field of view Blind spots around or in the central chamber, or
determine the retinal threshold for red.
Any unexplained visual symptoms, such
as flashes or streaks, should also be suspected as a possible manifestation of
retinopathy.
(12) When severe poisoning symptoms occur due to overdose or
allergies, it is recommended to give ammonium chloride orally (adult 8g daily,
divided doses), 3 or 4 days a week, after stopping treatment for several months
because urine acidifies It can increase renal excretion of 4-aminoquinoline
compounds by 20% to 90%.
However, caution should be exercised in patients with
impaired renal function and or metabolic acidosis.
Please read the instructions
carefully and follow the doctor's instructions.
Hydroxychloroquine Sulfate Children's Medication
At present, there has not been a
systematic and reliable clinical trial of children's medication. The
effectiveness and safety of children's medication have not been established, so
it is not recommended for children.
Hydroxychloroquine Sulfate Medication for Elderly Patients
The study was not conducted
and there are no reliable references.
[Medication for pregnant women and lactating women]
Hydroxychloroquine can pass through the placenta: There is limited information
about the application of hydroxychloroquine during pregnancy.
It should be
noted that 4-aminoquinine in therapeutic doses is associated with central
nervous system damage, including ototoxicity (auditory and vestibular toxicity,
congenital deafness), retinal bleeding and retinal pigmentation. Therefore,
pregnant women should avoid the use of hydroxychloroquine, and only use it when
the doctor judges that the benefit of the patient's prevention and treatment of
the drug is greater than the possible harm.
After intravenous injection of
radioactively labeled quinol into pregnant CBA mice, the drug can quickly pass
through the placenta, selectively accumulate in the melanin structure of the
fetal rat eye, and remain in the eye tissue until the drug is released from
other 5 months after site exclusion.
Women who are breastfeeding should use
hydroxychloroquine with caution, because a small amount of hydroxychloroquine
can be secreted in breast milk, and infants are known to be very sensitive to
the toxic effects of 4-aminoquinoline.
Hydroxychloroquine Sulfate Drug interactions
There are reports of hydroxychloroquine
increasing plasma digoxin levels: patients receiving combination therapy should
closely monitor their serum digoxin levels.
Although there are no special
reports, hydroxychloroquine may also have chloroquine interacting with several
known drugs, including aminoglycoside antibiotics that can enhance its ability
to directly block neuromuscular junctions. Cimetidine inhibits its metabolism
and thus increases the plasma concentration of anti-malarial drugs.
It antagonizes the
effects of neostigmine and pyristamine.
It weakens the body's initial immune
antibody response to intradermal injection of human diploid cell rabies
vaccine.
Antacids may reduce the absorption of hydroxychloroquine, so it is
recommended that the use of this product and antacids should be separated by 4
hours.
Hydroxychloroquine may enhance the effect of hypoglycemic drugs, so the
combination of drugs can be considered to reduce the dose of insulin and
hypoglycemic drugs.
Hydroxychloroquine Sulfate Overdose
4-aminoquinoline complex can be absorbed quickly
and completely after oral administration.
If inadvertently overdose, or in
small doses of sensitive patients, poisoning symptoms can appear within 30
minutes, such as headache, drowsiness, visual acuity, cardiovascular failure,
convulsions, and even sudden early respiratory and cardiac arrest.
The
electrocardiogram showed atrial arrhythmia, nodular rhythm, prolonged
interventricular conduction time, and progressive bradycardia led to
ventricular fibrillation and / or cardiac arrest. Mainly for symptomatic
treatment, the stomach contents should be emptied as soon as possible by
vomiting (at home, before being transported to the hospital) or gastric lavage.
Within 30 minutes after taking the medicine, after the gastric lavage, guide
the person through the gastric tube to at least 5 times the amount of activated
carbon powder to inhibit the further absorption of the medicine.
If the patient
has convulsions, it should be controlled before gastric lavage. If convulsions
are caused by brain stimulation, ultra-short-acting barbiturates can be used
with caution, however, if they are caused by hypoxia, oxygen therapy should be
given and artificial ventilation should be used.
In case, hypotension shock occurs,
vascular tension should be used drug. In view of the importance of respiratory
support, the patient should undergo tracheal intubation or tracheotomy if the
disease requires after gastric lavage.
Blood replacement can be used to reduce
the concentration of 4-aminoquinoline in blood. Patients who survive the acute
phase should be closely observed for at least 6 hours even if they have no
symptoms.
Patients who overdose or are sensitive to drugs should be
supplemented with fluids and given ammonium vapor for a few days (adult 8g per
day, divided use) to acidify the urine and promote the excretion of the drug
from the urine.
Pharmacology and Toxicology
The exact mechanism of action
of hydroxychloroquine is not fully understood, and may include interaction with
Ryukyu and interference with enzyme activity (including phosphatase,
NADH-cytochrome C reductase, cholinesterase, protease and Hydrolytic enzymes), binding
to DNA, stabilizing the lysosomal membrane, inhibiting the formation of
prostaglandins, inhibiting the chemotaxis of polymorphonuclear cells and the
role of phagocytic cells, interfering with the formation of monocyte
interleukin-1 and inhibiting The release of oxides.
Pharmacokinetics
According to foreign literature reports:
Hydroxychloroquine has pharmacological effects, pharmacokinetics and metabolic
processes similar to chloroquine. After oral administration, hydroxychloroquine
is quickly and almost completely absorbed.
In a study, after giving healthy
volunteers a single dose of 0.4g of hydroxychloroquine, the average peak plasma
concentration ranged from 53 to 208ng / ml, with an average level of 105ng /
ml. The average time to reach peak plasma concentration was 1.83 hours.
According to the time after administration, the average plasma elimination
half-life changes as follows: ~ 10, 10 ~ 48, 48 ~ 504 hours after the peak
plasma concentration is 5.9 hours, 26.1 hours and 299 hours, respectively.
Parent compounds and metabolites are widely distributed in the body, and
elimination is mainly through urine. In one study, a 3% dose was observed in 24
hours.
Storage of Hydroxychloroquine Sulfate
Sshading, sealed and stored.
General Common Package of Hydroxychloroquine Sulfate: 0.1g * 14 pieces / box.
Validity Period: 36 months
Popular Manufacturer: Shanghai Shangyao Zhongxi Pharmaceutical Co.,
Ltd. (formerly Shanghai Zhongxi Pharmaceutical Co., Ltd.)
Approval number: National Pharmaceutical Standard H19990263
Author's Bio
Name: Ian Skyler
Education: MBBS, MD
Occupation: Medical Doctor
Specialization: Community Medicine, General Surgery, Natural Treatment
Experience: 18 Years as a Medical Practitioner
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