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Volibris

MiljöinformationReceptstatusFörmånsstatus
GlaxoSmithKline

Filmdragerad tablett 5 mg
(Ljusrosa, fyrkantig, konvex, filmdragerad tablett med "GS" präglat på ena sidan och "K2C" på den andra sidan .)

Antihypertensiva medel, övriga antihypertensiva medel

Aktiv substans:
ATC-kod: C02KX02
Läkemedel från GlaxoSmithKline omfattas av Läkemedelsförsäkringen.
  • Vad är miljöinformation?

Miljöpåverkan (Läs mer om miljöpåverkan)

Ambrisentan

Miljörisk: Risk för miljöpåverkan av ambrisentan kan inte uteslutas då ekotoxikologiska data saknas.
Nedbrytning: Det kan inte uteslutas att ambrisentan är persistent, då data saknas.
Bioackumulering: Ambrisentan har låg potential att bioackumuleras.


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Detaljerad miljöinformation


Environmental Risk Classification


Predicted Environmental Concentration (PEC)

PEC is calculated according to the following formula:

PEC (μg/L) = (A*109*(100-R)/(365*P*V*D*100) = 1.5*10-6*A(100-R)


PEC = 0.0000417 μg/L


Where:

A = 0.278 kg (total sold amount API in Sweden year 2016, data from Quintiles IMS). Reduction of A may be justified based on metabolism data.

R = 0% removal rate (conservatively, it has been assumed there is no loss by adsorption to sludge particles, by volatilization, hydrolysis or biodegradation)

P = number of inhabitants in Sweden = 9 *106

V (L/day) = volume of wastewater per capita and day = 200 (ECHA default) (Reference 1)

D = factor for dilution of waste water by surface water flow = 10 (ECHA default) (Reference 1)


Predicted No Effect Concentration (PNEC)

Ecotoxicological studies

Green Algae:

No data


Water flea:

Acute toxicity

No data


Water flea:

Chronic toxicity

No Data


Fish:

Acute toxicity

No data

Chronic toxicity

No Data


Other ecotoxicity data:

No data


PNEC cannot be calculated because data is not available for all three (algae, crustacean and fish) of the short-term toxicity endpoints.


Environmental risk classification (PEC/PNEC ratio)

According to the European Medicines Agency guideline on environmental risk assessment of medicinal products (EMA/CHMP/SWP/4447/00), use of ambrisentan is unlikely to represent a risk for the environment, because the predicted environmental concentration (PEC) is below the action limit 0.01 μg/L (Reference 2).


Degradation

Biotic degradation

Ready degradability:

No data

Inherent degradability:

No Data

Abiotic degradation

Hydrolysis:

No data


Photolysis:

No data


Justification of chosen degradation phrase:

There are no degradation available for ambrisentan. The phrase “The potential for persistence of ambrisentan cannot be excluded, due to lack of data” is thus chosen.


Bioaccumulation

Partitioning coefficient:

Log Dowcalculated = 0.56 @ pH 7 (Reference 4)


Justification of chosen bioaccumulation phrase:

Since log Dow < 4, the substance has low potential for bioaccumulation.


Excretion (metabolism)

Ambrisentan Ambrisentan is glucuronidated via several UGT isoenzymes (UGT1A9S, UGT2B7S and UGT1A3S) to form ambrisentan glucuronide (13%). Ambrisentan also undergoes oxidative metabolism mainly by CYP3A4 and to a lesser extent by CYP3A5 and CYP2C19 to form 4-hydroxymethyl ambrisentan (21%) which is further glucuronidated to 4-hydroxymethyl ambrisentan glucuronide (5%). The binding affinity of 4-hydroxymethyl ambrisentan for the human endothelin receptor is 65-fold less than ambrisentan. Therefore at concentrations observed in the plasma (approximately 4% relative to parent ambrisentan), 4-hydroxymethyl ambrisentan is not expected to contribute to pharmacological activity of ambrisentan.


Ambrisentan and its metabolites are eliminated primarily in the bile following hepatic and/or extra-hepatic metabolism. Approximately 22% of the administered dose is recovered in the urine following oral administration with 3.3% being unchanged ambrisentan. Plasma elimination half-life in humans ranges from 13.6 to 16.5 hours (Reference 3).


PBT/vPvB assessment

Ambrisentan does not fulfil the criteria for PBT and/or vBvP.


All three properties, i.e. ‘P’, ‘B’ and ‘T’ are required in order to classify a compound as PBT (Reference 1). Ambrisentan does not fulfil the criteria for PBT and/or vBvP based on a log Dow < 4.


Please, also see Safety data sheets on

http://www.msds-gsk.com/ExtMSDSlist.asp.


References

  1. ECHA, European Chemicals Agency. 2008 Guidance on information requirements and chemical safety assessment.

  2. FASS.se, Environmental Classification of Pharmaceuticals. 2012 Guidance for pharmaceutical companies.

  3. Pharmacokinetic properties: Metabolism and Elimination. Summary of Product Characteristics Volibis (Ambrisentan). GlaxoSmithKline plc, October 2014.

  4. Chemaxon /LogD. December 2014. Instant J Chem, ChemAxon Ltd.