pCure Labs
LABS

Search substance info

Amitriptyline

Adrenergic Uptake Inhibitors
CATEGORIES

Adrenergic Uptake Inhibitors, Analgesics, Non-Narcotic, Antidepressive Agents, Tricyclic


ALIASES

ADT, Amitriptylin "DAK", Amitriptylin Abcur, Amitriptyline Hydrochloride, Laroxyl, Saroten®, Triptyl, Tryptizol, Tryptizol Frosst, Tryptizol®, Latilin, Levate, Maxitrip, Redomex, Saroten, Sarotex, Sarotex Retard, Syneudon, Tryptanol, Tryptizol, Uxen Retard


SUBSTANCES

amitriptyline, amitriptyline chloride


ENVIRONMENTAL CONCERN: MODERATE
Amitriptyline hydrochloride is a dibenzocycloheptene-derivative tricyclic antidepressant (TCA). TCAs are structurally similar to phenothiazines. They contain a tricyclic ring system with an alkyl amine substituent on the central ring. In non-depressed individuals, amitriptyline does not affect mood or arousal, but may cause sedation. In depressed individuals, amitriptyline exerts a positive effect on mood. TCAs are potent inhibitors of serotonin and norepinephrine reuptake. Tertiary amine TCAs, such as amitriptyline, are more potent inhibitors of serotonin reuptake than secondary amine TCAs, such as nortriptyline. TCAs also down-regulate cerebral cortical β-adrenergic receptors and sensitize post-synaptic serotonergic receptors with chronic use. The antidepressant effects of TCAs are thought to be due to an overall increase in serotonergic neurotransmission. TCAs also block histamine-H1 receptors, α1-adrenergic receptors and muscarinic receptors, which accounts for their sedative, hypotensive and anticholinergic effects (e.g. blurred vision, dry mouth, constipation, urinary retention), respectively. See toxicity section below for a complete listing of side effects. Amitriptyline may be used to treat depression, chronic pain (unlabeled use), irritable bowel syndrome (unlabeled use), diabetic neuropathy (unlabeled use), post-traumatic stress disorder (unlabeled use), and for migraine prophylaxis (unlabeled use).

Read More

MODERATE
Underlying information about P, ​​B, T and risk comes from Fass. Amitriptyline's major metabolite is nortriptyline. See also nortriptyline.

Below is Hazard and Risk from Fass environmental information for Amitriptylin Abcur (downloaded 2018-11-06)


Hazard
Persistence: No data.

Bioaccumulation: Log Kow = 4.92 (unknown method).

Toxicity: No data.

Risk
Risk of environmental impact of amitriptyline cannot be excluded, since no ecotoxicity data are available.

Pharmaceutical analyses of water in Stockholm County and nationally in Sweden
Amitriptyline has been found in treated wastewater (up to 24 ng/L), surface water (up to 9.1 ng/L) and sludge (up to 170 microg/kg dry weight) at national measurements. The IVL report also presents results from regional screening programs. Amitriptyline has been found in treated wastewater (over 20 ng/L) in Stockholm County during the last five-year period (2012-2016).

Article Fick J et al. 2010
Critical effect concentration (CEC) for amitriptyline is 48 ng/L. Log P is set to 4.9.

REFERENCES

  1. Fass.se för vårdpersonal
  2. 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.
  3. SLL. Sammanställning av läkemedelsprovtagningar - Bearbetning av regional försäljningsstatistik av läkemedel samt datamaterial från Stockholms läns landstings mätprogram för läkemedelssubstanser i vattenmiljö, 2012–2016.
  4. Fick J, Lindberg RH, Tysklind M, Larsson DG. Predicted critical environmental concentrations for 500 pharmaceuticals. Regul Toxicol Pharmacol. 2010;58:516-23.