Efient* 5 mg film-coated tablets. Efient 10mg film-coated t(十)
to 40% higher in healthy subjects and patients with a body weight of <60 kg compared to those weighing 60 kg. Prasugrel should be used with caution in patients with a body weight of <60 kg due to the potential risk of bleeding in this population (see section 4.4).
Ethnicity: In clinical pharmacology studies, after adjusting for body weight, the AUC of the active metabolite was approximately 19% higher in Chinese, Japanese, and Korean subjects compared to that of Caucasians, predominantly related to higher exposure in Asian subjects <60 kg. There is no difference in exposure among Chinese, Japanese, and Korean subjects. Exposure in subjects of African and Hispanic descent is comparable to that of Caucasians. No dose adjustment is recommended based on ethnicity alone.
Gender: In healthy subjects and patients, the pharmacokinetics of prasugrel are similar in men and women.
Children and adolescents: Pharmacokinetics and pharmacodynamics of prasugrel have not been eva luated in a paediatric population (see section 4.2).
5.3 Preclinical safety data
Non-clinical data reveal no special hazard for humans based on conventional studies of safety pharmacology, repeat-dose toxicity, genotoxicity, carcinogenic potential, or toxicity to reproduction. Effects in non-clinical studies were observed only at exposures considered sufficiently in excess of the maximum human exposure indicating little relevance to clinical use.
Embryo-foetal developmental toxicology studies in rats and rabbits showed no evidence of malformations due to prasugrel. At a very high dose (>240-times the recommended daily human maintenance dose on a mg/m2 basis) that caused effects on maternal body weight and/or food consumption, there was a slight decrease in offspring body weight (relative to controls). In pre- and post-natal rat studies, maternal treatment had no effect on the behavioural or reproductive development of the offspring at doses up to an exposure 240-times the recommended daily human maintenance dose (based on mg/m2).
No compound-related tumours were observed in a 2-year rat study with prasugrel exposures ranging to greater than 75-times the recommended therapeutic exposures in humans (based on plasma exposures to the active and major circulating human metabolites). There was an increased incidence of tumours (hepatocellular adenomas) in mice exposed for 2 years to high doses (>75-times human exposure), but this was considered secondary to prasugrel-induced enzyme induction. The rodent-specific association of liver tumours and drug-induced enzyme induction is well documented in the literature. The increase in liver tumours with prasugrel administration in mice is not considered a relevant human risk.
6. PHARMACEUTICAL PARTICULARS
6.1 List of excipients
Tablet Core:
Microcrystalline cellulose
Mannitol (E421)
Croscarmellose sodium
Hypromellose (E464)
Magnesium stearate
Film-Coat:
Lactose monohydrate
Hypromellose (E464)
Titanium dioxide (E171)
Triacetin (E1518)
Iron oxide red (E172) [10mg tablets only]
Iron oxide yellow (E172)
Talc
6.2 Incompatibilities
Not applicable.
6.3 Shelf life
2 years.
6.4 Special precautions for storage
This medicinal product does not require any special temperature storage conditions. Store in the original package to protect from air and moisture.
6.5 Nature and contents of container
Aluminium foil blisters in cartons of 14, 28, 30, 30 (x1), 56, 84, 90 (x1) and 98 table |
