Drugs online research references
Eur J Pharmacol. 1980 Oct 3;67(1):41-6.
High affinity binding of tricyclic antidepressants to histamine H1-receptors: fact and artifact.
Taylor JE, Richelson E.
Six tricyclic antidepressants were tested for their ability to inhibit the binding of the histamine H1-receptor antagonist [3H]pyrilamine to membrane fractions from whole rat brain. Calculated inhibition constants (Ki) for the antidepressants were in the range of 2.6 x 10(-11) to 2.3 x 10(-7) M and correlated very well with their equilibrium dissociation constants derived from biological assays of the H1-receptor. Increasing the concentration of receptors present in the binding assay resulted in an overestimation of the calculated Ki's for doxepin, amitriptyline, and nortriptyline, but not for the lower affinity compounds of the series, imipramine, protriptyline, and desipramine. These results indicate: (1) the importance of receptor concentration in determining the potency of compounds which competitively inhibit, with very high affinity, the binding of a radioactively labeled ligand; (2) the need to correlate binding data with biological data.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6106553&dopt=Abstract
J Clin Psychiatry. 1982 Feb;43(2):66-9.
Plasma concentrations of tricyclic antidepressants in clinical practice.
Hollister LE.
Plasma concentrations of four tricyclic antidepressant drugs were monitored in 180 patients. Plasma concentrations incongruent with dose suggested noncompliance at some time among 20% of the patients. Plasma concentrations correlated poorly with dose except with amitriptyline. Plasma concentration of drug and active metabolite, in the case of imipramine and amitriptyline, tended to be higher in ng/ml than the daily dose in mg; the converse was true for nortriptyline and desipramine. Most patients achieved "therapeutic"plasma concentrations at doses of 150 mg/day. However, "therapeutic" plasma concentrations did not correlate well with clinical response.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=7056706&dopt=Abstract
J Immunoassay. 1985;6(1-2):11-22.
Radioimmunoassay of tricyclic antidepressant and some phenothiazine drugs in forensic toxicology.
Robinson K, Smith RN.
A radioimmunoassay suitable for screening blood and urine samples for tricyclic antidepressant and some phenothiazine drugs in forensic toxicology is described. The assay displays a remarkably broad spectrum of cross-reactivity that enables therapeutic or subtherapeutic levels of most tricyclic antidepressants and a number of phenothiazines in blood to be detected. The antiserum is commercially available and the radioligand, a radioiodinated conjugate of N-acetyl-L-histidine and nortriptyline, is easily prepared. Blood samples require prior extraction to reduce the background but urine may be assayed directly. 75 microliters of blood or 100 microliter of urine are required. Haemolysis or decomposition of the samples, common anticoagulants and sodium fluoride do not affect the results. Data for 57 compounds are presented.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2410459&dopt=Abstract
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