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Amlodipine

Antihypertensive Agents
CATEGORIES

Antihypertensive Agents, Vasodilator Agents, Calcium Channel Blockers, Antianginal Agents


ALIASES

Amlodipine 1 A, Amlodipine Accord, Amlodipine Actavis, Amlodipine Alternova, Amlodipine Apotex, Amlodipine Arrow, Amlodipine Aurobindo, Amlodipine BMM Pharma, Amlodipine Bluefish, Amlodipine Essential Pharmaceuticals, Amlodipine Genericon, Amlodipine GL, Amlodipine Hexal, Amlodipine IVAX, Amlodipine Jubilant, Amlodipine Krka, Amlodipine Medical Valley, Amlodipine Medochemie, Amlodipine Orifarm, Amlodipine Orion, Amlodipine Ranbaxy, Amlodipine STADA®, Amlodipine Sandoz, Amlodipine Sopharma, Amlodipine Winthrop, Amlodipine ratiopharm, Amlodipine Teva, Amlodipine Vitabalans, Amlodipine/Valsartan Actavis, Amlodipine/Valsartan Apotex, Amlodipine/Valsartan Denk, Amlodipine/Valsartan EG, Amlodipine/Valsartan Genericon, Amlodipine/Valsartan HCS, Amlodipine/Valsartan Krka, Amlodipine/Valsartan Mylan, Amlodipine/Valsartan Sandoz, Amlodipine/Valsartan STADA, Amlodipine/Valsartan/Hydrochlorothiazide Krka, Candesartan/Amlodipine Krka, Olmesartan/Amlodipine Accord, Olmesartan/Amlodipine EG, Olmesartan/Amlodipine Krka, Olmesartan/Amlodipine Sandoz, Olmesartan/Amlodipine Teva, Perindopril/Amlodepine Krka, Perindopril/Amlodepine Teva, Perindopril/Amlodepine Stada, Ramipril/Amlodipine Actavis, Ramipril/Amlodipine Adamed, Ramipril/Amlodipine Apotex, Ramipril/Amlodipine Aristo, Ramipril/Amlodipine EG, Ramipril/Amlodipine Glenmark, Ramipril/Amlodipine Sandoz, Rosuvastatin/Amlodipine Krka, Acerycal, Afiten, Agen, Albis, Alea, Alneta, Altensil, Amaloris, Amelior, Amesos, Amlator, Amlipine, Amló, Amlober, Amlobesyl, Amlocard, Amlode, Amlodno, Amlodigamma, Amlodilan, Amlodinova, Amlozek, Amoratio, Amlorine, Amlobe, Amlodistad, Amloratio, Amlor, Amlori, Amlotan, Antacal, Apo-Amlo, Arplexam, Astucor, Astudal, Atordapin, Asbima, Astudal, Balzak, Belfor, Bevacomb, Bigital, Bivis, botinero, Caduet, Cantensio, Camdero, Capenon, Caramlo, Cardilopin, Co-Dalnessa, Concor, Copalia, Coveram, Coverlam, Coverdine, Dafiro, Dalnessa, Dalneva, Dicartil, Dipperam, Dironorm, Egiramlon, Exforge, Flutensif, Framsyl, Giant, Hipres, Норваск, Imprida, Istin, Istolde, Konverge, Lipertance, Lodip, Lodopin, Lopin, Lopridam, Milodimyl, Mixor, Normodipine, Nartivivancombi, Natrixam, Nelod, Nopidin, Nordip, Norvas, Norvasc, Olssa, Orcal, Perivasc, Piramil, Pharex Amlodipine, Prestalia, Prestance, Priamlo, Ramdacordia, Rameam, Ramelso, Ramomark, Reaptan, Sanoral, Rosmela, Rosvaden, Sevikar, Statriam, Sobycombi, Takawita, Teldipin, Telassmo, Tenloris, Tenox, Tezefort, Tonanda, Tonarssa, Triplixam, Tritace Combi, Triveram, Twynsta, Valsamix, Valsimia, Valtensam, Valticrom, Viacoram, Viacorlix, Vidonorm, Wamlox, Zabart, Zenicamo, Zorem


SUBSTANCES

amlodipine, amlodipine besylate, amlodipine maleate, amlodipine mesilate, amlodipine mesylate monohydrate


ENVIRONMENTAL CONCERN: MODERATE
Amlodipine is a long-acting 1,4-dihydropyridine calcium channel blocker. 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, amlodipine prevents calcium-dependent myocyte contraction and vasoconstriction. A second proposed mechanism for the drug’s vasodilatory effects involves pH-dependent inhibition of calcium influx via inhibition of smooth muscle carbonic anhydrase. Some studies have shown that amlodipine also exerts inhibitory effects on voltage-gated N-type calcium channels. N-type calcium channels located in the central nervous system may be involved in nociceptive signaling and pain sensation. Amlodipine is used to treat hypertension and chronic stable angina.

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MODERATE
The T-value in the score for hazard refers to acute toxicity and it is based on previous environmental information in Fass. Environmental information is missing on fass.se ( 2018-10-11 ). It is voluntary for manufacturers to provide information about environmental impact on fass.se. Underlying data for P and B are from assessment report.

Assessment report for Exforge HCT (amlodipine besylate/valsartan/hydrochlorothiazide) EMEA/CHMP/410729/2009
"AML (amlodipine, editorial remark) shows significant chronic toxicity to aquatic species and has potential to inhibit the microbial activity of activated sludge at high concentrations. It is not readily biodegradable and based on its physical-chemical properties and its high susceptibility to oxidative metabolism in higher organisms it is not expected to bio-accumulate. AML was found to be photolabile. The compound shows moderate adsorption to sludge and partitioning into sediments with only 5.3 to 6.0 % of applied radioactivity as parent substance found in sediments after 21 days." CHMP has requested additional data, see assessment report for Exforge HCT. Such data have not been found.

Below is Hazard and Risk from Fass environmental information for Norvasc (amlodipin) (downloaded 2011-04-06)


Hazard
Persistence: The substance is degraded slowly in the environment.

Bioaccumulation: The substance has the potential to be accumulated in aquatic organisms.

Acute toxicity: There is data for 3 trophic levels, lowest algae 100 microg/L.

Risk
The risk to the environment is insignificant.

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. Santos, L. H. M. L. M., M. Gros, S. Rodriguez-Mozaz, C. Delerue-Matos, A. Pena, D. Barcelóand M. C. B. S. M. Montenegro (2013). Contribution of hospital effluents to the load of pharmaceuticals in urban wastewaters: Identification of ecologically relevant pharmaceuticals. Science of The Total Environment 461–462 (0): 302-316.
  2. Godoy, A.A., Kummrow, F., Pamplin, P. (2015) Occurrence, ecotoxicological effects and risk assessment of antihypertensive pharmaceutical residues in the aquatic environment - A review. Chemosphere 138, 281-291.
  3. European Medicines Agency. European public assessment reports (EPAR).
  4. Goodpoint. Jämförande bedömning av miljörisk vid användning av kalciumantagonisterna amlodipin och felodipin. Stockholm: Goodpoint; 2018.