PubMed · 5645606
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1968-03-08. Protriptyline (Vivactil)--another antidepressant.. https://pubmed.ncbi.nlm.nih.gov/5645606/
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The purpose of this review is to present relatively detailed information on the characteristics of tricyclic antidepressants, mainly amitriptyline hydrochloride and doxepin hydrochloride, for use as an integral part of the safe and effective management of fibromyalgia and, to a lesser extent, other chronic pain syndromes. Data sources include MEDLINE searches in English, relevant reference books and textbooks, my personal database and library, as well as personal clinical experience. I discuss these data with regard to the pharmacologic characteristics, mechanisms of action, adverse effects, and precautions involved with the use of tricyclic antidepressants. Additional information is given on drug selection and dosage titration. Much emphasis is placed on the fact that while tricyclic antidepressants play a major role in the management of fibromyalgia and other chronic pain syndromes, lifestyle alterations (eg. physical reconditioning and exercise), as well as behavior modification, are also vital to a successful outcome in management.
The effects of antidepressants given in a single dose or repeatedly (10 mg/kg p.o., twice daily, 14 days) on binding to dopamine D2 receptors in the striatum and limbic forebrain of Wistar male rats were studied. [3H]N-0437, (2-(N[2,3(n)-3H]propyl-N-(2-thiofuranyl)-2'-ethylamino) -5-hydroxy-1,2,3,4-tetrahydronaphthalene), a dopamine D2 receptor agonist, was used as a ligand. Already a single dose of imipramine and fluoxetine caused a statistically significant decrease in the affinity of the ligand for dopamine D2 receptors in the striatum, but only at 72 h after drug administration. Also at 72 h after the single dose of mianserin a significant increase in the density of dopamine D2 receptors was observed. Repeated imipramine, amitriptyline and mianserin increased the affinity for dopamine D2 receptors in the striatum and in the limbic forebrain. Repeated fluoxetine increased that affinity in the striatum, but decreased it in the limbic forebrain. The density of dopamine D2 receptors was increased by the repeated administration of the antidepressants studied in the limbic forebrain, but was not changed in the striatum. The results obtained in the present study are in good agreement with the previously reported enhancement of behavioural responsiveness to dopamine and dopamine stimulants (dopamine D2 up-regulation) evoked by repeated treatment with antidepressants.
For the system kappa-carrageenan/amitriptyline it is shown that the degree of binding of amitriptyline is closely related to the carrageenan conformation as regulated by the counterions (Na+ or K+). The adsorption becomes much more pronounced when the carrageenan molecule is in the helix form (counterion K+) than when it has a coil conformation (counterion Na+). Furthermore, for the helical state the adsorption becomes strongly cooperative. It is also shown experimentally that the release from the adsorbed state has a conversion temperature at about 42 degrees C (helix-coil transition). The effect is also related to the linear charge density. For iota-carrageenan with a higher charge density the adsorption is strong and cooperative both in the presence of Na+ and K+ ions.