ABSTRACT
PURPOSE: To compare the inhibitory effects of various tricyclic antidepressants (TCAs) on contractile response of the rat vas deferens to electrical stimulation of hypogastric nerve. MATERIALS AND METHODS: A total of forty Spraque Dawley rats (weight 300-350gm) were divided into 8 groups (n=5 in each): doxepine, amitriptyline, trimipramine, desipramine, imipramine, clomipramine, protriptyline, and prazosin treated groups. Before (baseline pressure) and 20 minutes after intravenous injection of each agent (0.1-, 1-, 10-, and 20-fold of therapeutic doses for human in each agent), the hypogastric nerves, iden tified under operative microscope, were electrically stimulated with rectangular pulses of 0.5 mseconds duration, 10 Hz, and 10 V for 10 seconds. Dose of drug administered was gradually increased in order of 0.1- to 20-fold dose. RESULTS: All drugs tested in this study caused dose-dependent inhibition of the rat intravasal pressure induced by the electrical stimulation of hypogastric nerve. Inhibitory potency of each drug was doxepine (88.5% and 96.5% at 10- and 20-fold dose)> OR = amitriptyline (76.8% and 91.8%)>clomipramine (66.7% and 74.4%)> OR =imipramine (48.2% and 67.0%)=prazosin (45.6% and 63.5%)=trimipramine (52.7% and 65.4%)> OR =desi pramine (45.3% and 49.0%)> protriptyline (18.9% and 19.9%). CONCLUSIONS: Inhibitory effects of TCAs on contractile response of the rat vas deferens to electrical stimulation of hypogastric nerve would increase in proportion to their potency of alpha1-adrenoceptor blocking actions.
Subject(s)
Animals , Humans , Rats , Amitriptyline , Antidepressive Agents, Tricyclic , Clomipramine , Desipramine , Doxepin , Electric Stimulation , Imipramine , Injections, Intravenous , Prazosin , Protriptyline , Trimipramine , Vas DeferensABSTRACT
Apesar de a cefaléia crônica diária (CCD) ser frequentemente observada na prática cefaliátrica, o interesse pelo seu estudo é recente. Foram estudados 52 pacientes (48 mulheres e 4 homens) com idade entre 13 e 71 anos, que preencheram os critérios diagnósticos propostos por Silberteins e col. (1994) para CCD primária. A análise das principais características clínicas permitiu o diagnóstico de três modalidades da CCD: migrânea transformada (n=39; 75 por cento), cefaléia do tipo tensinoal crônica (n=11; 21,1 por cento) e cefaléia diária persistente de início súbito (n=2; 3,9 por cento). Destes pacientes, 34 (65,4 por cento) utilizavam de modo excessivo medicaçoes sintomáticas e foram considerados como sofredores de cefaléia induzida por drogas. O esquema de tratamento utilizado incluiu, além da orientaçao à interrupçao das medicaçoes sintomáticas, o uso de amitriptilina isoladamente ou em associaçao ao propanolol, em doses crescentes, levando-se em conta a resposta e a tolerância a estes fármacos. Esse esquema revelou-se eficaz na diminuiçao da frequência da cefaléia na maioria dos pacientes com CCD. Os efeitos benéficos revelaram-se duradouros, persistindo mesmo após seis meses do início do acompanhamento. Na minoria dos pacientes na qual a terapêutica instituída nao obteve êxito, constatou-se, de forma estatisticamente significativa, a persistência do uso excessivo de medicaçao sintomáticas.
Subject(s)
Adult , Middle Aged , Female , Humans , Adolescent , Amitriptyline , Headache/diagnosis , Propranolol , Amitriptyline/therapeutic use , Chronic Disease , Drug Administration Schedule , Follow-Up Studies , Headache/drug therapy , Propranolol/therapeutic use , Prospective Studies , Trimipramine/therapeutic useSubject(s)
Adult , Dibenzazepines/therapeutic use , Doxepin/therapeutic use , Female , Humans , Male , Middle Aged , Peptic Ulcer/drug therapy , Trimipramine/therapeutic useABSTRACT
The level of y-aminobutyric acid (GABA) was determined in the brain of rats 1 hr. after i.p. injection of chlorpromazine, prochlorperazine, diazepam, trimipramine, methamphetamine and nikethamide. Diazepam increased, and, trimipramine and amphetamine decreased the brain GABA level over wide dose ranges. Low doses of chlorpromazine and prochlorperazine increased but high doses of the drugs reduced the GABA level. Low doses of nikethamide reduced whereas high doses increased the level of GABA. The effects of the drugs have been discussed in relation to the brain GABA level.
Subject(s)
Aminobutyrates/analysis , Animals , Brain Chemistry/drug effects , Chlorpromazine/pharmacology , Diazepam/pharmacology , Dose-Response Relationship, Drug , Methamphetamine/pharmacology , Nikethamide/pharmacology , Prochlorperazine/pharmacology , Psychotropic Drugs/pharmacology , Rats , Trimipramine/pharmacology , gamma-Aminobutyric Acid/analysisABSTRACT
The effect of different doses of trimipramine has been studied on the force of contraction of isolated kitten atria. Trimipramine produced dose dependent increase in the force of contraction of the atria. Pretreatment of kitten with reserpine or of the isolated atria with propranolol inhibited the positive inotropic effect of trimpramine. The positive inotropic action of trimipramine is probably due to the release and /or due to blocking the uptake of spontaneously released noradrenaline. Trimipramine was also found to potentiate the positive inotropic action of noradrenaline. This potentiation not only decreased in relation to the time of exposure of the isolated atria to trimipramine but also the action of noradrenaline was antagonised.