Seratrodast Tablets 80mg

Seratrodast Tablets 40mg
Seratrodast Tablets 80mg

DESCRIPTION

Seratrodast is an orally active quinone derivative and a potent TXA2 receptor antagonist used in the prophylactic management of asthma and treatment of allergic rhinitis.

Structure of Seratrodast

Chemical name:???-7-?3?5?6-trimethyl-1?4-benzoquinone-2-yl?-7-phenylheptanoic acid (?) 7-phenyl-7-(2,4,5-trimethyl-3,6-dioxocyclohexa-1,4-dien-1-yl)heptanoic acid

Molecular formula: C22 H26 O4

Molecular weight: 354.44

COMPOSITION

a) Seratrodast Tablets 40mg Taj Pharma

Each tablet contains:

Seratrodast???.. 40 mg

b) Seratrodast Tablets 80mg Taj Pharma

Each tablet contains:

Seratrodast???.. 80 mg

CLINICAL PHARMACOLOGY

Pharmacodynamics

Seratrodast is a potent, long-acting, stereospecific thromboxane A2/prostaglandin endoperoxide receptor antagonist. The R-(+)-enantiomer of Seratrodast is the pharmacologically active moiety. Seratrodast appears to exert its anti-inflammatory effects through antagonism of the thromboxane A2 receptor (TP receptor). In addition, seratrodast blocks the broncho-constrictor effects of PGF2?, PGD2 and 9?,1l?-PGF2 mediated through activation of thromboxane A2 receptor (TP receptor).

Pharmacokinetics

Following single and repeated oral administration, seratrodast is rapidly and dose-dependently absorbed. The peak plasma concentrations of seratrodast increase proportionally with dose reaching steady-state concentration within 7 days of administration. Following once-daily doses of 80mg for 15 days in patients with mild to moderate asthma, the peak plasma concentration of Seratrodast is 8.80 ?g/ml with an average Tmax of 2.4 hours. The area under the plasma concentration-time curve (AUC) for Seratrodast is 22.96 ?g.hr/ml and the average apparent volume of distribution is 33 litres.

Seratrodast has a high protein binding capacity (more than 99%). It is metabolized to 5-methyl hydroxy seratrodast and 4-hydroxyseratrodast by cytochrome P450 (CYP) isoenzymes. It is also partially (35%) glucuronidated in plasma and may be subjected to enterohepatic recycling.

Following oral administration of 40 to 120 mg/day in healthy subjects, the renal clearance of seratrodast ranges from 5.10 to 8.94 ml/hr (average 7.0 ml/hr) after a single dose and at steady-state respectively. The percentage of the dose excreted as unchanged drug in the urine ranges from 0.42% to 1.37% (average 0.83%) after a single dose and at steady-state. The plasma concentrations decline bi-exponentially with an average half-life of 20 and 36 hours after single and multiple administrations, respectively.

INDICATIONS

Setra is indicated in

  • Prophylactic management of mild to moderate asthma

DOSAGE AND ADMINISTRATION

  • An average dose of 80 mg once daily is recommended
  • Setra has been shown to be well-tolerated following repeated once-daily oral doses of up to a maximum of 320 mg
  • In elderly patients, the treatment should be started with a lower dose of 40mg/day

CONTRAINDICATIONS

  • Hypersensitivity to Seretra or any of the ingredients
  • Patients with hepatic failure

USE IN SPECIAL POPULATIONS

Pregnancy and Lactation

There are no adequate and well-controlled studies in pregnant women. Serena should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Serena should be avoided during lactation.

Pediatric Use (< 18 years of age)

The safety and efficacy of Seretra have not been established in children and should not be used in this age group.

WARNINGS AND PRECAUTIONS

Seretra may lead to an elevation in the levels of the hepatic enzymes. Therefore, it has to be administered with caution in patients with hepatic impairment.

DRUG INTERACTIONS

  • Use cautiously with other anti-inflammatory analgesics, cephalosporin antibiotics and drugs that have been reported to cause hemolytic anaemia.
  • As aspirin can compete for serum protein binding, it may increase the concentration of the unbound drug (seratrodast) by 26%.

ADVERSE EFFECTS

Adverse reactions are generally rare, but if present, range from mild to moderate in severity.

0.1 to 5% Less than   0.1% (rare)
Hypersensitivity Rash, Itching.
Hepatic Elevated liver enzymes
Gastrointestinal Nausea, loss of appetite, stomach discomfort, abdominal pain, diarrhoea, dry mouth Vomiting
Hematologic Anaemia Thrombocytopenia, epistaxis
Neuropsychiatric Drowsiness, headache Insomnia, tremor, numbness
Other Palpitations, malaise Hot flashes, oedema

OVERDOSAGE

There have been no reports of overdosage with Seretra. In cases of overdosage, the stomach should be emptied by aspiration and gastric lavage. Vital parameters should be managed symptomatically.

STORAGE

Store in a cool, dry and dark place. Keep out of reach of children.

PRESENTATION

A blister strip of 10 tablets.

Manufactured in India by:    
TAJ LIFE SCIENCES PVT. LTD.
Unit No. 214, Old Bake House,
Bake House Lane, Fort,
Mumbai-400001
at: Ahmedabad- Gujarat, INDIA.
Ho.NO.+91 8448 444 095
Toll Free Phone: (1800-222-434 / 1800-222-825)