장기(또는, 영향을 받은 알려진 모든 장기를 명시)에 손상을 일으킴(노출되어도 특정 표적장기 독성을 일으키지 않는다는 결정적인 노출경로가 있다면 노출경로를 기재)
특정 표적장기 독성 - 1회 노출
구분 1
위험
P260, P264, P270, P307+P311, P321,P405, P501
예방조치문구:
P210
열·스파크·화염·고열로부터 멀리하시오 - 금연 하시오.
P260
분진·흄·가스·미스트·증기·...·스프레이를 흡입하지 마시오.
P280
보호장갑/보호의/보안경/안면보호구를 착용하시오.
P301+P310
삼켰다면 즉시 의료기관(의사)의 진찰을 받으시오.
P311
의료기관(의사)의 진찰을 받으시오.
트리미프라민 C화학적 특성, 용도, 생산
용도
Antidepressant.
정의
ChEBI: A dibenzoazepine that is 10,11-dihydro-5H-dibenzo[b,f]azepine substituted by a 3-(dimethylamino)-2-methylpropyl group at the nitrogen atom. It is used as an antidepressant.
World Health Organization (WHO)
Trimipramine, a tricyclic antidepressant was introduced in 1961
for the management of endogenous depression. Much of the adverse effects are
caused by its antimuscarinic actions. These include dry mouth, cardiac
arrhythmias, central nervous system disturbances, blood disorders and risk of
suicide. The risk of suicide and dangers related to overdosage led Norwegian
Medicines Control Authority to put the higher strength formulation under
prescribing restriction in 1992. The risk of death following overdosage is
apparently higher for products containing tricyclic compounds as compared with
nontricyclic products.
Pharmacokinetics
Trimipramine is one of the antidepressants with the most pronounced differences in pharmacokinetics caused
by the CYP2D6 genetic polymorphism. Its bioavailability and systemic clearance depended
significantly on the CYP2D6 isoform with a linear dose relationship. Its mean bioavailability was 44% in
individuals without CYP2D6 (poor metabolizers) but 16 and 12% in those individuals with two and three active
genes of CYP2D6 (fast and ultrafast metabolizers), respectively. Consequently, the mean total clearances of
the oral dose were 27, 151, and 253 L/hour in poor, extensive, and ultrarapid metabolizers, respectively. The
44% bioavailability combined with low systemic clearance of trimipramine in poor metabolizers of CYP2D6
substrates results in a very high exposure to trimipramine with the risk of adverse drug reactions. On the
other hand, the presystemic elimination may result in subtherapeutic drug concentrations in carriers of
CYP2D6 gene duplications with a high risk of poor therapeutic response
Clinical Use
Although trimipramine has the weakest binding affinity for the monoamine transporters, it shares the pharmacological and toxicity actions of the other TCAs and is used primarily in the
treatment of depression.