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At least 649 records · Page 36Linked to original sources
PubMed2000

Effects of agonist-antagonist opioids in humans trained in a hydromorphone/not hydromorphone discrimination.

The purpose of this study was to examine the discrimination of agonist-antagonist opioids in humans trained in a two-choice hydromorphone/not hydromorphone discrimination. Eight adult male volunteers with histories of opioid abuse who were not currently physically dependent were trained to discriminate the mu receptor agonist hydromorphone (3 mg/70 kg, i.m.) ("Drug A") from a "Not Drug A" training condition (saline placebo). Volunteers received financial reinforcement for correct responses. After training, generalization dose-effect curves for hydromorphone, butorphanol, pentazocine, nalbuphine, and buprenorphine were determined. Other subjective, behavioral, and physiological measures were concurrently collected in all sessions. In generalization testing hydromorphone and buprenorphine produced dose-related increases in hydromorphone-appropriate responses. Pentazocine produced an inverted U-shaped dose-response curve with complete substitution at 32 mg/70 kg but not at 64 mg/70 kg. Butorphanol and nalbuphine did not completely substitute for hydromorphone at any dose tested. These results differ from an earlier two-choice, Drug A versus Drug B (hydromorphone/saline) discrimination study. After Drug/Not Drug instructions the behavioral discriminations of agonist-antagonist opioids were more consistent with their putative agonist activities at the mu opioid receptor and with their subjective effects profiles than was the case after Drug A versus Drug B instructions. These results suggest that instructions are an important factor in the outcome of human drug discrimination studies.

Adult↗
PubMedDate not supplied

[The effect of narcotic analgesics on nociceptive reactions of a visceral and somatic nature].

The experiments on conscious cats showed that buprenorphine given in 0.0125 and 0.025 mg/kg selectively inhibited motor, emotional and hemodynamic manifestations of pain induced by stimulation of the splanchnic nerve. The analgetic effect of morphine, tramal, pentazocine and butorphanol was equally demonstrated on visceral and somatic pain models, but the drugs elevated the baseline blood pressure and produced no (morphine, pentazocine) or moderate (tramal, butorphanol) antihypertensive effects in various nociceptive stimuli.

Analgesics, Opioid↗
PubMed1990

Discriminative stimulus effects of opioid agonists in morphine-dependent pigeons.

Discriminative stimulus effects of opioid agonists were studied in morphine-dependent (10.0 mg/kg/day) pigeons discriminating among i.m. injections of morphine (10.0 mg/kg), saline and naltrexone (0.032 mg/kg) while responding under a fixed ratio schedule of food presentation. Morphine and naltrexone occasioned responding on the respective correct keys in a dose-related manner with complete generalization (greater than or equal to 90% correct) occurring with doses of morphine larger than 10.0 mg/kg and doses of naltrexone larger than 0.001 mg/kg. Several opioid mu and kappa agonists were studied in dependent pigeons and in morphine-abstinent pigeons (i.e., 30-hr morphine-deprived). The opioid mu agonist etonitazene substituted completely for morphine in dependent pigeons; in abstinent pigeons a small dose of etonitazine reversed withdrawal and larger doses substituted for morphine. Some opioid agonists did not substitute completely for morphine in dependent pigeons and partially (nalbuphine, meperidine) or completely (butorphanol, buprenorphine) reversed withdrawal in abstinent pigeons. In contrast, the opioid kappa agonists trans-3,4-dichloro-N-methyl-N(2-[1-pyrrolidinyl]cyclohexyl) benzeneacetamide methanesulfonate and bremazocine did not substitute for morphine or for naltrexone in dependent pigeons and did not reverse withdrawal in abstinent pigeons. Moreover, in dependent pigeons buprenorphine, butorphanol and nalbuphine, but not trans-3,4-dichloro-N-methyl-N(2-[1-pyrrolidinyl]cyclohexyl)benzeneace tam ide methanesulfonate, antagonized the discriminative stimulus effects of morphine and of naltrexone. These results confirm in morphine-dependent pigeons qualitative differences in discriminative stimulus effects among mu and kappa opioid agonists and support the notion that differences among agonists under some conditions can result from variations in efficacy.

Animals↗
PubMed1989

Discriminative stimulus effects of mu and kappa opioids in the pigeon: analysis of the effects of full and partial mu and kappa agonists.

Pigeons were trained to discriminate a dose of either 0.01 mg/kg of bremazocine or 0.05 mg/kg of fentanyl from water using a two-key drug discrimination procedure. During tests of substitution, the selective kappa-opioid agonists bremazocine, U50, 488 and tifluadom substituted for the bremazocine stimulus, whereas the less selective kappa-opioid agonists ethylketocyclazocine, levallorphan, proxorphan and nalorphine substituted for the fentanyl stimulus. The full mu-opioid agonists fentanyl, morphine, I-methadone and levorphanol, as well as the partial agonists nalbuphine, butorphanol and buprenorphine, substituted for the fentanyl stimulus. Compounds with partial-opioid agonist effects, namely nalbuphine, butorphanol, buprenorphine, proxorphan, levallorphan and nalorphine, produced 50% fentanyl-appropriate responding at doses 25 to 369.2 times smaller than the doses required to decrease response rates to 50% of control values. In contrast, the full mu-opioid agonists fentanyl, morphine, I-methadone and levorphanol produced 50% fentanyl-appropriate responding at doses only 1.3 to 10.9 times smaller than those required to decrease response rates by 50%. During tests of antagonism, both naloxone and Mr2266 produced a dose-dependent attenuation of the stimulus effects of bremazocine and fentanyl, whereas beta-funaltrexamine antagonized the stimulus effects of fentanyl but not bremazocine. Although bremazocine has been reported to have mu-opioid antagonist effects, it failed to antagonize the stimulus effects of the training dose of fentanyl. The present investigation establishes further that pigeons can discriminate selective kappa-opioid agonists from mu-opioid agonists and that in pigeons the classification of numerous opioid compounds on the basis of their kappa-like or mu-like stimulus effects differ from those in rat and monkey. In addition, under the drug discrimination procedure the actions of compounds classified as partial-opioid agonists can be differentiated from those of full mu-opioid agonists on the basis of the ratio of the dose required to engender fentanyl-like stimulus effects to the dose required to reduce response rates.(ABSTRACT TRUNCATED AT 250 WORDS)

3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cycloh↗
PubMed1987

Evaluation of the receptor selectivities of opioid drugs by investigating the block of their effect on urine output by beta-funaltrexamine.

The effects of a series of opioid drugs on urine output in the water-loaded rat were studied and also the block of those effects by the irreversible opioid receptor antagonist, beta-funaltrexamine (beta-FNA). Fentanyl, d-propoxyphene, profadol, bromadoline, buprenorphine and nalbuphine produced only a decrease in urine output, which was antagonised by pretreatment with beta-FNA, 40 mg/kg s.c., 24 hr beforehand. These drugs were thus characterized as selective mu receptor agonists. U-50,488, tifluadom, Mr2034, proxorphan, ethylketocyclazocine and butorphanol all produced an initial decrease in urine output, which was antagonized by beta-FNA, and therefore probably mu receptor mediated, followed by a beta-FNA insensitive diuretic effect, which was probably kappa receptor mediated. For U-50,488, tifluadom, Mr2034 and proxorphan the threshold dose for increasing urine output was lower than that for decreasing it, suggesting that these four compounds are kappa-selective agonists. For ethylketocyclazocine and butorphanol, the threshold doses for producing both effects were similar, suggesting that these two drugs are non-selective agonists. SKF 10,047 produced a diuretic effect at low dose-levels, which may be kappa receptor mediated, and a beta-FNA insensitive decrease in urine output at higher dose-levels, which may suggest a sigma receptor mediated effect.

Animals↗
PubMed1978

Discriminative effects of cyclazocine in the squirrel monkey.

In order to characterize the discriminative stimulus properties of cyclazocine squirrel monkeys were trained to discriminate between intramuscular injections of 0.1 mg/kg of cyclazocine and drug vehicle in a discrete-trial avoidance paradigm in which a response on one of two levers would prevent or terminate the delivery of a mild electric shock to the tail. Behavior was considered to be under stimulus control when the monkeys completed at least 22 trials of a 25-trial session on the appropriate choice lever after they received cyclazocine or vehicle. Stimulus generalization (i.e., dose-response) curves were then determined for a variety of drugs over a broad range of doses. The following analgesics with narcotic antagonist properties produced stimulus control of behavior comparable to that produced by 0.1 mg/kg of cyclazocine: ketocyclazocine (0.1 mg/kg), butorphanol (1.0 mg/kg), oxilorphan (3.0 mg/kg) and levallorphan (3.0 mg/kg). Time course experiments revealed that the duration of complete stimulus control was relatively short: 1 hour after 0.1 mg/kg of cyclazocine and 3.0 mg/kg of oxilorphan and 0.5 hour after 0.1 mg/kg of ketocyclazocine. Naloxone produced a dose-related antagonism of the stimulus control by cyclazocine and butorphanol which was complete at 1.0 mg/kg. In contrast, as much as 10 mg/kg of naloxone only partially blocked stimulus control by ketocyclazocine and failed to modify stimulus control by oxilorphan and levallorphan. The monkeys showed partial generalization to other drugs with activity as narcotic agonists, antagonists or both (e.g., morphine, naloxone, pentazocine, nalbuphine, nalmexone and nalorphine), but little or no generalization to the nonopioid psychoactive drugs, d-amphetamine, mescaline, pentobarbital and scopolamine. This discrimination paradigm appears to have potential as a model for the quantitative assessment of the discriminative stimulus properties of narcotic antagonist analgesics.

Animals↗
PubMed1980

Interactions between narcotic agonists, partial agonists and antagonists evaluated by schedule-controlled behavior.

The effects of morphine, butorphanol, cyclazocine, ketocyclazocine, ethylketocyclazocine, and SKF-10,047 were tested, alone and in conjunction with naloxone or naltrexone, in rats responding under a fixed-interval, 5-min schedule of food presentation. Except for naloxone and naltrexone, all of the drugs decreased the average rate of responding in a dose-dependent manner. The rate-decreasing effects of morphine were markedly antagonized by naltrexone, while the effects of SKF-10,047 or high doses of cyclazocine were not antagonized by naltrexone or naloxone. Naltrexone and naloxone were able to antagonize the effects of butorphanol, ketocyclazocine, ethylketocyclazocine and low doses of cyclazocine, but these drugs were considerably more difficult to antagonize than was morphine. Thus, the interactions between these drugs and the narcotic antagonists allow the classification of the drugs into three groups, based on a marked shift, a moderate shift or no shift in the dose-response curve. This classification is consistent with the hypothesis of Martin et al., (Journal of Pharmacology and Experimental Therapeutics, 197: 517-532, 1976) regarding distinct receptors for morphine and related drugs (mu agonists), ketocyclazocine and ethylketocyclazocine (kappa agonists) and SKF-10,047 (sigma agonist).

Analgesics, Opioid↗
PubMed1993

Precipitated withdrawal by pentazocine in methadone-maintained volunteers.

Pentazocine is a partial mu agonist opioid with one-half to one-sixth the parenteral analgesic potency of morphine. The purpose of this study was to characterize the effects of pentazocine in comparison to naloxone (an opioid antagonist), hydromorphone (an opioid mu agonist) and saline in methadone-dependent volunteers by using the same experimental methods used previously in the study of the opioid analgesics buprenorphine, butorphanol and nalbuphine. In a residential laboratory, five volunteer male opioid abusers, maintained on 30 mg p.o. of methadone daily, underwent pharmacological challenges 2 to 3 times per week. Pharmacological challenges consisted of a double-blind i.m. injection of: pentazocine (dose range 7.5-120 mg), hydromorphone (5 and 10 mg), naloxone (0.1 and 0.2 mg) or saline. Injections were given 20 hr after the last dose of methadone. Measures included physiological indices and self-reports and observer ratings of drug effects. Naloxone and hydromorphone produced characteristic antagonist-like and agonist-like effects, respectively, on subjective, observer and physiological indices. Pentazocine produced primarily antagonist-like effects, with higher doses (> = 60 mg) producing significant elevations of visual analog scale ratings of Drug Effects, Bad Effects and Sick; of observer ratings of piloerection, restlessness and adjective scores of opioid withdrawal; as well as increases in blood pressure, heart rate and pupil diameter and decreases in skin temperature. Similar to the previous study of butorphanol, the specific profile of effects produced by pentazocine differed from that produced by naloxone, suggesting non-mu effects may modulate the mu effects of pentazocine.

Adult↗
PubMed1993

Agonist and antagonist effects of mixed action opioids in the pigeon drug discrimination procedure: influence of training dose, intrinsic efficacy and interanimal differences.

The stimulus effects of selective, high efficacy mu opioids and mixed action opioids with varying degrees of intrinsic efficacy at the mu receptor were examined in pigeons trained to discriminate between saline and either 0.056 (low) or 0.18 (high) mg/kg of fentanyl. The stimulus profiles produced by the various opioids could be separated into three groups: 1) opioids that substituted completely for both training doses of fentanyl, with steep slopes and little interanimal differences in the lowest dose (lowest discriminable dose) that produced complete substitution (fentanyl, morphine and l-alpha-acetylmethadol); 2) opioids that substituted completely for the low training dose and produced high levels of substitution for the high training dose, with relatively shallow slopes and interanimal differences in the lowest discriminable dose (butorphanol, buprenorphine, ethylketocyclazocine, ketocyclazocine, proxorphan, (-)-pentazocine and (-)-metazocine); and 3) opioids that substituted completely for the low training dose, with relatively shallow slopes and large interanimal differences in the lowest discriminable dose. Each of these opioids also antagonized the high-dose fentanyl stimulus with large interanimal differences in the lowest antagonist dose (nalbuphine, nalorphine, (-)-cyclorphan, (-)-cyclazocine, (-)-n-ally-normetazocine and levallorphan). These patterns of substitution and antagonism most likely reflect differences in the intrinsic efficacy of these drugs at the mu receptor, with low intrinsic efficacy associated with shallow dose-effect functions, large interanimal differences in the drug's lowest discriminable dose and low levels of substitution for the high-dose fentanyl stimulus. During antagonism tests with naloxone, two patterns were observed: 1) opioids against which naloxone had apparent pA2 values of approximately 7.0, with little interanimal differences and with the slopes of the Schild plots approximating -1.0 (fentanyl and morphine) and 2) opioids against which naloxone had apparent pA2 values an order of magnitude higher, with large interanimal differences and with the slopes of Schild plots being relatively shallow (butorphanol, nalbuphine, nalorphine and levallorphan). The present findings emphasize the importance of training dose, intrinsic efficacy and interanimal differences when analyzing drug discrimination data.

Animals↗
PubMed1993

Repetitive injectable anesthesia in a 27-year-old horse.

A 27-year-old horse was anesthetized 3 times a week for 4 weeks, to facilitate cobalt therapy of a squamous cell carcinoma in the left paranasal sinus. Limitations of facilities required transport of the anesthetized horse to and from the cobalt therapy room, therefore, injectable anesthesia was used. Initially, the horse was preanesthetized with xylazine (at 1.1 mg/kg IV) and butorphanol (0.04 mg/kg IV). After 3 anesthetic episodes, the xylazine dose was reduced to 0.4 mg/kg IV and the butorphanol was deleted from the regimen. Tiletamine-zolazepam (1.1 mg/kg IV) was used for induction and maintenance of anesthesia (although on 2 occasions a bolus of ketamine was used to maintain immobility). The length of the procedure varied from 10-45 minutes, and the recovery times to sternal and standing varied from 23-76 and 55-105 minutes respectively. Although numerous complications might be expected given the age of this horse and the physiologic and metabolic demands of repetitive injectable anesthetics, none were observed.

Anesthesia, Intravenous↗
PubMedDate not supplied

[Chronopharmacological features of the pain-relieving effects of analgesics].

The circadian and ultradian rhythms of threshold pain sensitivity to different nociceptive stimuli-thermal (tail-flick) and mechanical (tail pressure)--were revealed by cosinor analysis in male rats without or after drug administration. The minimal pain sensitivity to mechanical pressure was observed during the first half of the dark phase, that to thermal stimulus during the first half of the light phase. Biorhythms of thermal pain sensitivity of mice and rats are characterized by the same parameters. Opioid receptor morphine, buprenorphine, butorphanol, morphoceptin, and U-50,488H showed individual day patterns of analgesia, which depended on the type of nociceptive stimuli. The most distinct shifts of the acrophase of circadian rhythm from the control were observed after morphine, butorphanol, and U-50,488H. A conclusion is made that drug interaction with kappa-opiate receptors contributes to the regulation of pain sensitivity biorhythms.

Analgesics↗
PubMed1997

Discriminative stimulus effects of opioids in pigeons trained to discriminate fentanyl, bremazocine and water: evidence of pharmacological selectivity.

The purpose of the present investigation was to examine the discriminative stimulus effects of opioids with activity at mu and kappa opioid receptors, in pigeons trained to discriminate the mu opioid fentanyl, the kappa opioid bremazocine and water in a three-choice discrimination task. The apparent pkB values obtained for naloxone as an antagonist of the stimulus effects of fentanyl were higher than those obtained against the bremazocine stimulus. The mu opioids morphine and l-methadone substituted for the fentanyl stimulus, the kappa opioids U50,488 and U69,593 substituted for the bremazocine stimulus, and the non-opioid pentobarbital failed to substitute for either the fentanyl or bremazocine stimulus. A series of opioids with activity at both the mu and kappa opioid receptor sites, including nalorphine, butorphanol, buprenorphine, nalbuphine, ethylketocyclazocine, (-)-ketocyclazocine, (-)-n-allylnormetazocine (NANM) and levallorphan, produced high levels of substitution for the fentanyl stimulus without producing appreciable levels of substitution for the bremazocine stimulus. At doses that did not substitute for the fentanyl stimulus, (-)-NANM, levallorphan, nalorphine and nalbuphine partially antagonized the bremazocine stimulus (i.e. produced responding on the water key). Butorphanol and buprenorphine also antagonized the bremazocine stimulus, although this effect was evidenced only at doses that substituted for the fentanyl stimulus. In contrast, even when tested up to doses that markedly decreased rates of responding, ethylketocyclazocine and (-)-ketocyclazocine failed to antagonize the bremazocine stimulus. The present findings indicate that in this three-choice task the fentanyl-like substitution patterns produced by opioids with activity at both the mu and kappa opioid receptors are similar to those reported in pigeons trained to discriminate either fentanyl or bremazocine from saline (i.e. two-choice tasks). In this task, however, the level of kappa antagonist activity evidenced by these opioids was considerably less than that obtained in pigeons trained to discriminate bremazocine from saline.

Analgesics↗
PubMed1998

[Evaluation of preincisional mexiletine administration to alleviate postoperative pain].

Mexiletine, an antiarrhythmic agent, was preincisionally administered intravenously for the purpose of reducing postoperative pain. Twenty-eight female patients for mastectomy were studied. The patients were divided into three groups. Group 1 received no mexiletine. Group 2 received bolus administration of mexiletine 1 mg.kg-1 with additional continuous administration of 1 mg.kg-1.hr-1 for 75 minutes. Group 3 received bolus administration of mexiletine 2 mg.kg-1. The requirement of butorphanol as a postoperative analgesic within 1 hour after mastectomy in Group 3 was significantly lower than that in Group 1 (P < 0.05), but butorphanol requirement in Group 2 was not significantly lower than that in Group 1. Plasma mexiletine concentration was slightly higher in Group 3 (1.7 micrograms.ml-1) than that in Group 2 (1.0 microgram.ml-1) immediately after the intravenous mexiletine administration, although there was no significant difference. The results indicate that mexiletine 2 mg.kg-1 as preoperative bolus administration maintains its plasma concentration above 1.7 micrograms.ml-1, and is clinically effective for reducing the postoperative pain after mastectomy.

Adult↗
PubMed1995

A pilot project in office-based diagnostic esophagogastroduodenoscopy comparing two nonintravenous methods of sedation and anesthesia.

OBJECTIVE: To evaluate the performance and findings of diagnostic esophagogastroduodenoscopy (EGD) procedures in a primary care office setting, comparing two nonintravenous methods of sedation and anesthesia. DESIGN: A consecutive case series of patients with appropriate indications referred over a 13-month period for the EGD procedure was studied. Procedure outcomes and patient acceptance were evaluated following the procedure. SETTING: Patients were referred from community primary care physician offices to another community private office. PATIENTS: Medically stable adult patients with indications for nonemergent EGD were referred for evaluation. INTERVENTION: Esophagogastroduodenoscopy was performed in an office setting using small-caliber (7.9-mm or 9.0-mm) fiberoptic endoscopes. Patients were given either diazepam orally and ketorolac tromethamine intramuscularly or triazolam orally and butorphanol tartrate spray intranasally as sedation prior to the procedure. MAIN OUTCOME MEASURES: Clinical findings observed, histopathologic results, complications, oxygen desaturation, cardiac dysrhythmias, and length of procedures were recorded. Patients reported pain and satisfaction scores on a linear numeric scale following the procedure. RESULTS: No major complications were noted in this study population. Seventy-three percent (52/71) of all patients rated their discomfort during the office-based EGD procedure as mild, with 49% (35/71) giving the lowest possible pain score rating. Ninety-six percent (68/71) of all patients rated their satisfaction with the procedure as high, with 65% (46/71) reporting the highest possible level of satisfaction. The study did not demonstrate a significant difference in patient comfort or satisfaction between the two methods of nonintravenous sedation. CONCLUSIONS: Two alternative methods to intravenous sedation and anesthesia appear to create adequate comfort and satisfaction for patients undergoing EGD and merit future study and consideration.

Administration, Intranasal↗
PubMed1991

Discriminative stimulus effects of spiradoline, a kappa-opioid agonist.

This study represents the initial step in assessing the discriminative effects of spiradoline (U62,066), a potent congener of the selective kappa-opioid agonist, U50,488. Separate groups of rats were trained to discriminate between SC injections of saline and either 3.0 mg/kg spiradoline or 3.0 mg/kg morphine in a discrete-trial shock-avoidance/escape procedure. Spiradoline-trained rats generalized completely to U50,488 (ED50S for spiradoline and U50,488 were 0.66 and 8.71 mg/kg, respectively), but selected the choice lever appropriate for saline in generalization tests with graded doses of morphine, phencyclidine, and agonist-antagonist opioids with varying degrees of kappa activity, ethylketocyclazocine, nalorphine, and butorphanol. Morphine-trained rats did not generalize to spiradoline. Naltrexone (0.01 or 0.1 mg/kg) blocked surmountably the discriminative effects of both spiradoline and morphine, but was approximately 10-fold less potent against spiradoline. These results indicate that the discriminative effects of spiradoline are mediated by kappa-opioid receptors; meaningful mu-opioid and PCP/sigma components of action were not in evidence. The potency and apparent pharmacological selectivity of spiradoline suggest the potential value of this drug for studying kappa-opioid-mediated stimulus control of behavior.

3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cycloh↗
PubMedDate not supplied

The nucleus paragigantocellularis and opioid withdrawal-like behavior.

Participation of the nucleus paragigantocellularis (PGi) in mediation of opioid withdrawal was examined in conscious, unrestrained, non-opioid-dependent rats, using electrical stimulation of the PGi. A characteristic series of behaviors, which resembled those seen during naloxone-precipitated withdrawal from dependence on the opioid agonist, butorphanol, was elicited during 30 min of PGi stimulation. Thus, the behavioral syndrome has been termed opioid withdrawal-like. Simultaneous microdialysis measurement of glutamate within the locus ceruleus indicated a positive correlation between extracellular glutamate concentrations and behavioral responses. Behavioral responses were inhibited by 50% during reverse dialysis perfusion of the locus ceruleus with the glutamate receptor antagonist, kynurenic acid, without any effect on glutamate concentrations. Thus, increases in locus ceruleus glutamate partially mediate opioid withdrawal-like behavior. Intracerebroventricular (i.c.v.) injections of the opioid antagonist, naloxone, or of the mu-selective (beta-funaltrexamine) or the delta-selective (naltrindole) opioid antagonists decreased, but did not abolish, stimulation-induced behavioral responses. Similar i.c.v. injections of the kappa-selective antagonist, nor-binaltorphimine, had no effect on behavioral responses to PGi stimulation. Activation of the PGi by electrical stimulation can elicit behaviors similar to those observed during opioid withdrawal. Moreover, additional levels of complexity are evident in the neuropharmacology of PGi stimulation-induced opioid withdrawal-like behavior.

Animals↗
PubMed1994

Recent advances in the acute management of migraine and cluster headaches.

I have discussed the pharmacokinetics, efficacies, and side effects of the various nonnarcotic drugs available for the treatment of patients who have headache. Sumatriptan, the newest one, is expensive but may be cost-effective for those who have failed traditional migraine treatment, who visit the ER frequently, who have potential for drug abuse, or who have to miss time from school or work due to the headache. Studies are in progress to compare sumatriptan with other available drugs such as DHE-45 and to determine its possible role in the prophylaxis of migraine. A new 5-HT1D receptor agonist with more efficacy and fewer side effects may be developed in the future. When sumatriptan and DHE-45 are contraindicated due to hypertension or coronary artery disease, other drugs such as metoclopramide, ketorolac, and butorphanol can be used as alternatives.

Analgesics↗
PubMed1983

The effect of the opioid-benzodiazepine, tifluadom, on ingestive behaviors.

A large body of evidence has suggested a role for the endogenous opiates and their receptors in the regulation of appetite. In this study, we report on the effects of tifluadom, a noval opiate with a benzodiazepine-like structure and preferential activity at the kappa opiate receptor, on ingestive behaviors. Tifluadom increases food intake in rats without altering water intake. Tifluadom's effect on feeding is more potent than that of morphine or ketocyclazocine and equivalent to that of butorphanol. The effect is partially resistant to naloxone antagonism. Tifluadom is more potent when administered subcutaneously than when given intraperitoneally. These data provide further support for the concept that kappa opiate receptors represent an important component of the natural feeding drive.

Animals↗