Allopathy
Prescription Required
DCGI (Drugs Controller General of India)
Schedule H
Seratrodast belongs to the pharmacological class Thromboxane A2 Receptor Antagonist
Seratrodast has been approved for relieving symptoms and also for the treatment and maintenance of episodes of asthma.
Seratrodast is rapidly absorbed with a steady state plasma concentration of 4.6–6 μg/ml obtained in about 3 to 4 hours. Seratrodast is cleared rapidly by the hepatic biotransformation
Seratrodast is available in the form of tablets and widely used in Japan, India and other Asian countries. Around 20% of the administered dose is said to be recovered in the urine with 60%of the dose in the form of conjugates.
The most common side effects related to the use of Seratrodast are headache, dizziness, drowsiness, nausea, liver or hepatic problems , palpitations etc.
Seratrodast is available in the form of tablets and widely used in Japan, India and other Asian countries.
Seratrodast belongs to the pharmacological class Thromboxane Receptor Antagonist
Seratrodast has been approved for relieving symptoms and also for the treatment and maintenance of episodes of asthma.
Seratrodast is available in tablets and should be swallowed whole with water
Seratrodast can be used in the treatment of:
- Asthma
Seratrodast can help to relieve symptoms and also for the treatment and maintenance of episodes of asthma.
Seratrodast is approved for use in the following clinical indications:
- Asthma
Seratrodast can be administered orally before/ after meals. The dosage and duration of treatment should be as per the clinical judgment of the treating physician.
40 mg , 80 mg.
Tablets
Smoking cessation and maintaining health is a must.
Caffeine should be avoided or limited to use as it might lead to the risk of nausea, palpitations, nervousness, rapid heartbeat, etc.
Alcohol should be avoided in the patient’s especially with an underlying liver disorder or liver dysfunction
Diet containing food with a high glycemic index, saturated and trans fat food, red and processed meat, added sugar, salt, preservatives, refined and high energy-dense foods, low fiber, low antioxidants, and vitamins needs to be restricted.
The dietary restrictions is needed to be individualized as per the patient's requirements.
Seratrodast maybe contraindicated during the co-administration with the following :
- Hypersensitivity to the ingredients of the medication
- Underlying liver disease
The adverse reactions related to Seratrodast can be categorized as:
Common
- Nausea
- Loss of Appetite
- Headache
- Dizziness
- Drowsiness
- Palpitations
- Malaise
- Constipation dry mouth
- Taste disturbances
- Abdominal pain
- Diarrhea
- Stomach discomfort
Rare
- Vomiting
- Thrombocytopenia
- Epistasis
- Bleeding tendency
- Insomnia
- Tremor
- Numbness
- Hot flushes
- Edema
The clinically relevant drug interactions of Seratrodast is briefly summarized here:
- Co-administration with paracetamol or with cepham antibiotics might cause an increase in the risk of liver disease or damage
- Co-administration with aspirin might cause increase in bioavailability of seratrodast
The common side effects of Seratrodast include the following:
- Headache
- Palpitations
- Drowsiness
- Hypersensitivity
- Hepatitis or liver infection
- GIT disturbances
Pregnancy
There is found to be no adequate and well-controlled studies in pregnant women. Seratrodast should be used during pregnancy only if the potential benefits outweighs the risks to the fetus
Nursing mothers
There is found to be no adequate and well-controlled studies in lactating women. Seratrodast should be used by nursing mothers only if the potential benefit outweighs the risks to the fetus
Pediatric
There is found to be no adequate and well-controlled studies in pediatric populations.
Pharmacodynamics
Seratrodast is said to be 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).
Pharmacokinetics
After a 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 suffering from 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 i.e. 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.
- Endo S, Akiyama K: Thromboxane A2 receptor antagonist in asthma therapy. Nihon Rinsho 1996 Nov;54(11):3045-8.
- Samara EE (1996). "Seratrodast (AA-2414)—A Novel Thromboxane-A2 Receptor Antagonist". Cardiovascular Drug Reviews. 14 (3): 272–85.
- Qian J, Locke C, Dean R, Killian A, Granneman GR ,et.al.(1996). "Single-dose and steady-state pharmacokinetics of seratrodast in healthy male and female volunteers".
