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Felodipine

Antihypertensive Agents
CATEGORIES

Antihypertensive Agents, Anti-Arrhythmia Agents, Vasodilator Agents, Calcium Channel Blockers, Dihydropyridines


ALIASES

Felodipin Actavis, Felodipin AstraZeneca, Felodipin HEXAL, Felodipin Hexal, Felodipin Mylan, Felodipin Orifarm, Felodipin STADA®, Felodipin Sandoz, Felodipin Teva, Hydac®, Logimat, Logimat forte, Logimax, Logimax forte, Logimax®, Logimax® forte, Plendil®


SUBSTANCES

felodipine


ENVIRONMENTAL CONCERN: HIGH
Felodipine is a long-acting 1,4-dihydropyridine calcium channel blocker (CCB)b. It acts primarily on vascular smooth muscle cells by stabilizing voltage-gated L-type calcium channels in their inactive conformation. By inhibiting the influx of calcium in smooth muscle cells, felodipine prevents calcium-dependent myocyte contraction and vasoconstriction. Felodipine is the most potent CCB in use and is unique in that it exhibits fluorescent activity. In addition to binding to L-type calcium channels, felodipine binds to a number of calcium-binding proteins, exhibits competitive antagonism of the mineralcorticoid receptor, inhibits the activity of calmodulin-dependent cyclic nucleotide phosphodiesterase, and blocks calcium influx through voltage-gated T-type calcium channels. Felodipine is used to treat mild to moderate essential hypertension.

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HIGH
The T-value in the score for hazard refers to acute toxicity. Underlying data for P, B and T are from Fass.se.

Levels of felodipine measured in the environment in Sweden are estimated to be high enough to give therapeutic levels in fish, based on the fat solubility. Mechanism based data is missing.

Felodipine is included in the Stockholm County Council's table of pharmaceuticals with risk for negative environmental impact according to the environmental programme 2017-2021. Felodipine has been detected in treated wastewater in Stockholm County at the beginning of the last five-year period (2012-2016).

Below is Hazard and Risk from Fass environmental information for Plendil (felodipine) (downloaded 2018-05-23)


Hazard
Persistence: "Felodipine is not readily biodegradable." and is potentially persistent.

Bioaccumulation: Log P = 3.86.

Acute toxicity: There are data for 3 trophic levels, lowest for fish 0.05 mg/L. 

Risk
PEC/PNEC is based on sales data in Sweden in 2014. PEC/PNEC = 0.74, which gives the risk low, i.e. consideration has not been given to measured levels in the environment.

Suggestions on how to reduce the release of felodipine
Concrete proposals on how to work to reduce emissions of environmentally harmful pharmaceuticals on the list have been developed in close cooperation with the Stockholm Drug and Therapeutics Committee's expert advice. The action proposals were developed from an environmental perspective. The patient's best always goes first and several pharmaceuticals on the list are also included in the Wise List. However, for such pharmaceuticals, there may be measures that could reduce the environmental impact.

Concrete proposal for felodipine
• Felodipine is not recommended in the Wise List.

Comparative assessment of environmental risk with the use of calcium antagonists amlodipine and felodipine in Sweden (Report Goodpoint 2018)
Amlodipine is estimated to be much less fat soluble (log P = 2.1) than felodipine (log P = 4.5). Experimental data (methodology partially unclear) suggests a slightly smaller difference (amlodipine log P = 3.04; felodipine 3.8 to 3.86). Although there are some uncertainties about the exact fat solubility of the substances, both chemical data and comparable data indicate that felodipine is more ecotoxic than amlodipine.

Amlodipine, recommended in the Wise List, is better from an environmental point of view than felodipine.

REFERENCES

  1. Fass.se för vårdpersonal
  2. Goodpoint. Prioritering av läkemedel med miljörisk inom SLL. Stockholm: Goodpoint; 2016. Rapport LS 2016–0634.
  3. IVL Swedish Environmental Research Institute Ltd. Fick J, Lindberg RH, Kaj L, Brorström-Lundén E. Results from the Swedish National Screening Programme 2010. Subreport 3. Pharmaceuticals.
  4. IVL Swedish Environmental Research Institute Ltd Fick J, Lindberg RH, Fång J, Magnér J, Kaj L, Brorström-Lundén E. Screening 2014. Analysis of pharmaceuticals and hormones in samples from WWTPs and receiving waters. Rapport C 135.
  5. Fick J, Lindberg RH, Tysklind M, Larsson DG. Predicted critical environmental concentrations for 500 pharmaceuticals. Regul Toxicol Pharmacol. 2010;58:516-23.
  6. SLL. Sammanställning av läkemedelsprovtagningar - Bearbetning av regional försäljningsstatistik av läkemedel samt datamaterial från Stockholms läns landstings mätprogram för läkemedelssubstanser i vattenmiljö, 2012–2016.
  7. Stockholms läns landsting. Förteckning över miljöbelastande läkemedel med åtgärdsförslag framtagen inom ramen för SLL:s miljöprogram 2017–2021.
  8. Goodpoint. Jämförande bedömning av miljörisk vid användning av kalciumantagonisterna amlodipin och felodipin. Stockholm: Goodpoint; 2018.
  9. Socialstyrelsen. Statistikdatabas för läkemedel.
  10. Stockholms läns landsting. Janusinfo: Läkemedelsuppföljning