Cloperastine Fendizoate also called Cloperastine or Cloperastin and Cloperastine hydrochloride
is an antitussive and antihistamine. It is used as a cough suppressant and used to treat cough in
cold, acute bronchitis, chronic bronchitis, bronchiectasis, and lung tuberculosis. It is approved
for sale in Japan, Hong Kong, and in parts of the European Union. It suppresses cough by
acting on the central nervous system.
Cloperastine Fendizoate is sold under the brand names Hustazol, Nitossil, and Seki among
Friedrich Bossert, Wolf Vater, Kurt Bauer filed for the first patents back in 1971. It was first
approved for sale in Japan in 1972, followed by its first launch in Italy in 1981. It is not approved
for sale in the USA.
Dosage and Administration
Cloperastine Fendizoate is available as a cough syrup. The usual recommended dose for adults
is 0.1 to 0.2 g per dose, taken orally, three times a day. The pediatric dose for children below 2
years is 2.5 mg and for children from 2 to below 4 years, the dose is 2.5 to 5 mg, for children
between 4 to 7 years, the dose is 5 to 10 mg, taken orally, three times a day. The doctor will
adjust the dose based on the condition of the patient, the response to the drug, and the severity
of the symptoms.
The price of Cloperastine Fendizoate
The price of one injection of 1ml in a 10mn DMSO solution costs USD 25 in the international
market. The API ingredient version of this medicine costs around USD 50 for a supply of 98%
pure powder of Cloperastine HCL.
How does it work?
Cloperastine Fendizoate’s precise mechanism of action has not been fully understood or
established. However, several other studies on its biological activities show that it involved the
ligand of the σ1 receptor (Ki = 20 nM), which is likely an agonist of GIRK channel blocker and a
potent antihistamine (Ki = 3.8 nM for the H1 receptor, and anticholinergic properties.
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