ergoline and Pain

To compare the effectiveness and side effects of cabergoline with bromocriptine for the symptomatic treatment of cyclic mastalgia as a part of the premenstrual syndrome.. 140 women with premenstrual mastalgia were enrolled in this randomised, open-label trial. Two groups were created (bromocriptine and cabergoline) and consisted of 61 and 67 patients respectively at the end of trial. Bromocriptine was administered 5 mg daily during second half of the menstrual cycle. Cabergoline was administered 0.5 mg weekly during the second half of the cycle. Relief of pain was evaluated using a visual analog scale (VAS). The mean percentage decrease in score for all patients in each group was calculated. A 50% or greater decrease at the end of the third month from the basal VAS score was accepted as a positive response to drug therapy. Data regarding side effects were collected systematically with review of a symptom diary.. The positive response rates to treatment were similar (bromocriptine 66.6% and cabergoline 68.4%). The pain reduction rates for each month were also similar. Moreover, the pain reduction rate was maximum in the second month of treatment for both groups. Vomiting (28%), nausea (39%) and headaches (23%) recorded in the bromocriptine group were significantly more frequent than vomiting (4.5%), nausea (20.9%) and headache (6%) recorded in the cabergoline group (p=0.023, p=0.001, p=0.006 respectively). A difference in the rate of dizziness was not statistically significant (26.4% vs. 14.9%). There was no correlation between the baseline breast pain score and prolactin level but post-treatment pain reduction was well correlated with prolactin level.. Cabergoline is as effective as bromocriptine for the treatment of cyclic mastalgia but has minimal side effects compared to bromocriptine.

Topics: Adult; Analysis of Variance; Breast; Bromocriptine; Cabergoline; Drug Administration Schedule; Ergolines; Female; Hormone Antagonists; Humans; Middle Aged; Pain; Pain Measurement; Premenstrual Syndrome; Prolactin; Quality of Life; Severity of Illness Index; Treatment Outcome

Topics: Adult; Aged; Arteriosclerosis; Attention; Clinical Trials as Topic; Drug Evaluation; Ergolines; Female; Headache; Humans; Intracranial Arteriosclerosis; Male; Middle Aged; Nicotinic Acids; Pain; Raynaud Disease

Previous studies have suggested that the alpha2-adrenergic receptor antagonist yohimbine produced antinociceptive effects in the formalin test in rats. However, yohimbine is also an agonist at serotonin (5-HT)1A receptors, suggesting the possibility that the antinociceptive effects of yohimbine might be mediated via these receptors.. The purpose of the present studies was to evaluate the potential role of 5-HT(1A) receptors in mediating the antinociceptive effects of yohimbine.. The antinociceptive effects of yohimbine were evaluated using the formalin test in rats.. Yohimbine (2.5-10 mg/kg s.c.) produced dose-related antinociception during both phase I and phase II of the formalin test, and was approximately equipotent and equiefficacious to morphine. The selective 5-HT(1A) receptor antagonist WAY 100,635 (0.03-3.0 mg/kg s.c.) produced a partial reversal of yohimbine. In comparison, the selective 5-HT(1A) receptor agonist (+/-)8-hydroxy-dipropylaminotetralin HBr (8OH-DPAT; 1.0 mg/kg s.c.) also produced a dose-related antinociception in the formalin test, although 8OH-DPAT was completely reversed by WAY 100,635 (3.0 mg/kg s.c.). The antinociceptive effects of yohimbine were not antagonized by the 5-HT(1B/1D) antagonist GR 127935 (1.0 mg/kg and 3.0 mg/kg s.c.), the 5-HT2 antagonist LY53857 (1.0 mg/kg s.c.), or the 5-HT3 antagonist zatosetron (3.0 mg/kg s.c.).. The present results demonstrate that yohimbine produces a dose-related antinociception in the formalin test in rats which is mediated in part by the agonistic actions at 5-HT(1A) receptors.

Topics: 8-Hydroxy-2-(di-n-propylamino)tetralin; Adrenergic alpha-Antagonists; Animals; Benzofurans; Bridged Bicyclo Compounds, Heterocyclic; Dose-Response Relationship, Drug; Ergolines; Formaldehyde; Male; Nociceptors; Oxadiazoles; Pain; Pain Measurement; Piperazines; Pyridines; Rats; Rats, Sprague-Dawley; Receptor, Serotonin, 5-HT1D; Receptors, Serotonin; Receptors, Serotonin, 5-HT1; Serotonin Antagonists; Serotonin Receptor Agonists; Time Factors; Yohimbine

Male albino rats were tested for antinociception following injections (IP) with saline, quinpirole (Quin) (1 mg/kg), morphine sulfate (M.S.) (5 mg/kg), or both Quin and M.S. (1 mg/kg and 5 mg/kg, respectively). Quin reduced and M.S. increased tail-flick latency as compared to controls. Tail-flick latencies of the animals injected with both drugs were significantly reduced as compared M.S. alone. Quin increased blood glucose levels by 96 percent, as compared to saline controls. In competitive binding studies Quin displaced 3H-DAGO (IC50 = 29.8 microM). CD-1 mice demonstrated a naloxone-reversible analgesia following ICV Quin (100 micrograms). These data are consistent with the hypothesis that the hyperglycemic effects of Quin attenuate M.S. analgesia while the antinociceptive effects of Quin may be mediated through opioid receptors.

Topics: Animals; Blood Glucose; Brain Chemistry; Dopamine Agents; Dose-Response Relationship, Drug; Ergolines; Hyperglycemia; Injections, Intraventricular; Male; Morphine; Pain; Quinpirole; Rats; Rats, Inbred Strains; Receptors, Opioid; Receptors, Opioid, mu; Sensory Thresholds

The role played by dopamine D1 and D2 receptors in formalin test analgesia was explored by challenging D-amphetamine- and morphine-induced analgesia with mixed and selective D1 and D2 antagonists, and by examining the relative analgesic activity of mixed and selective D1 and D2 agonists. The mixed D1/D2 dopamine antagonist cis-flupenthixol (0.5 mg/kg), the D2 antagonist pimozide (0.5 mg/kg), and the D1 antagonist SCH 23390 (0.1 mg/kg) attenuated both D-amphetamine and morphine analgesia. The mixed D1/D2 agonist apomorphine and the selective D2 agonist quinpirole produced dose-dependent analgesia while the selective D1 agonist SKF 38393 was without effect. These data suggest that D1 receptors play an "enabling" role in D2 receptor-mediated analgesia in the formalin test.

Topics: 2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine; Analgesia; Animals; Apomorphine; Benzazepines; Dextroamphetamine; Dopamine Agents; Dopamine Antagonists; Dose-Response Relationship, Drug; Ergolines; Flupenthixol; Formaldehyde; Male; Morphine; Pain; Pimozide; Quinpirole; Rats; Receptors, Dopamine; Receptors, Dopamine D1; Receptors, Dopamine D2

The effects of icv 4 dopamine (DA) agonists on analgesia caused by iv l-tetrahydropalmatine (THP) 8 mg/kg or by electro-acupuncture (EA) were studied by using the potassium iontophoretic dolorimetry in rabbits. The results showed that both THP-induced analgesia and EA analgesia were markedly attenuated by icv of DA or apomorphine (Apo), 2 mixed D1/D2 agonists. Similar results were obtained when SKF-38393, a selective D1 agonist, was applied. On the contrary, quinpirole hydrochloride (Qui), a selective D2 agonist, was found to enhance the analgesic action of THP or EA. However, DA, Apo, SKF-38393 or Qui per se did not influence the baseline pain threshold. All these observations indicate that functional alterations in DA receptor activities may be involved in THP-induced analgesia and EA analgesia, in which D1 and D2 subtype receptors exert different roles.

Topics: 2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine; Acupuncture Analgesia; Alkaloids; Animals; Apomorphine; Berberine Alkaloids; Dopamine; Dopamine Agents; Electroacupuncture; Ergolines; Female; Injections, Intraventricular; Male; Pain; Pain Measurement; Quinpirole; Rabbits; Receptors, Dopamine; Receptors, Dopamine D1; Receptors, Dopamine D2; Sensory Thresholds; Stereoisomerism

It has been suggested that reduced activity in raphe-spinal serotonergic systems induces hyperalgesia. In rats, the serotonin antagonist metergoline (0.5 mg/kg intraperitoneally) reduced tail flick latency by 0.92 sec (p less than 0.001) and increased tail skin temperature by 2.4 degrees C (p less than 0.001) when measured 50 min after injection. Multiple regression analysis with tail flick latency as dependent variable and tail skin temperature and metergoline/vehicle as independent variables revealed a highly significant effect of tail temperature on tail flick latency. The increase of tail skin temperature explained a reduction of tail flick latency of 0.64 of the 0.92 sec observed [B = -0.267 +/- 0.034, t(37)= -7.75, p less than 0.0001]. When the effect on tail skin temperature was taken into account, metergoline reduced tail flick latency by 0.28 sec [B = -0.284 +/- 0.114, t(37) = -2.50, p less than 0.05]. Metergoline (0.5 and 2.0 mg/kg) did not significantly alter plantar paw skin temperature or the response temperature in the increasing temperature hot plate test. Thus, the observed effect of metergoline on tail flick latency is primarily due to an effect on tail skin temperature. The possibility exists that the remaining effect of metergoline may be due to inadequate correction for the skin temperature change, and it is concluded that the study provide no clear evidence for a tonic inhibition of nociception by serotonergic systems.

Topics: Animals; Body Temperature Regulation; Ergolines; Male; Metergoline; Nociceptors; Pain; Rats; Rats, Inbred Strains; Reaction Time

The effects of intrathecal injections of the D2 agonists apomorphine and LY171555 were studied on responses of ventrobasal neurones responding to noxious stimulation in the urethane anaesthetised rat. At a dose of 75 micrograms/kg the D2 agonists had little effect on a total of 18 thalamic neurones. A higher dose (100 micrograms/kg) produced a reversible reduction of thalamic nociceptive responses on 15 occasions. A transient fall in blood pressure usually accompanied the intrathecal injection of the agonists. These results suggest that dopamine can modulate the transmission of nociceptive information to the thalamus and also suggests a role in the processing of autonomic function.

Topics: Afferent Pathways; Anesthesia, General; Animals; Apomorphine; Ergolines; Injections, Spinal; Male; Pain; Quinpirole; Rats; Rats, Inbred Strains; Receptors, Dopamine; Receptors, Dopamine D2; Spinal Cord; Thalamus; Urethane

Topics: Aged; Antiparkinson Agents; Ergolines; Female; Humans; Hypotension; Male; Middle Aged; Nausea; Pain; Parkinson Disease; Pergolide; Spasm

Methergoline was administered for 5 consecutive days starting on the morning after delivery in the block of lactation in 30 patients. The efficacy of the drug was evaluated in terms of milk production, and mammary congestion and pain. The results obtained and the absence of side-effects showed that the drugs was very suitable for this purpose.

Topics: Drug Evaluation; Ergolines; Female; Humans; Lactation; Metergoline; Pain; Postpartum Period; Pregnancy

Topics: Adult; Breast Diseases; Bromocriptine; Ergolines; Female; Humans; Pain

Mastodynia has previously been treated with gestagens or gestagen-based ovulation inhibitors with only marginal success. No other satisfactory therapy was available and in the search for a better treatment, the effectiveness of long term administration of the prolactin inhibitor bromocryptine (CB 154) to 15 patients was evaluated. Five of the subjects exhibited mammary secretion as well as mastodynia which, accorind to palpatorial, cytological and X-ray criteria, was not caused by intraductal pathology. After two to four weeks treatment with 5 mg CB 154 per day ten patients recovered fully, three showed some improvement and two were totally resistant to the treatment. Plasma prolactin levels during the follicular stage measured prior to treatment were in the normal range. All the patients continued to ovulate during the course of treatment despite the irrefutable fact that prolactin release from the pituitary was inhibited. Since there was a similar inhibition of prolactin secretion in the two patients who were resistant to treatment, it would seem that prolactin though probably very important, cannot be the only decisive factor in the hormonal control of mystodynia. Further observations showed that the premenstrual syndrome can also be successfully treated with CB 154. Upon withdrawal of treatment the possibility or relapse must be considered.

Topics: Adult; Breast Diseases; Bromocriptine; Ergolines; Female; Humans; Middle Aged; Pain; Premenstrual Syndrome; Prolactin