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In horses, intravenous dosages of butorphanol Repeated administration of butorphanol at 1 mg/kg DOSAGE ranging from 0.05 to 0.4 mg/kg were shown to be (10 times the recommended dose) every four hours The recommended dosage in the horse is 0.1 mg 7. Popio, K.A. et al: “Hemodynamic and Respiratory eff ective in alleviating visceral and superfi cial pain for 48 hours caused constipation in one of two of butorphanol per kilogram of body weight Eff ects of Morphine and Butorphanol,” Clin. for at least 4 hours, as illustrated in the following horses. (0.05 mg/lb) by intravenous injection. This is Pharmacol. Ther. 23: 281–287, 1978. fi gure: equivalent to 5 mL of TORBUGESIC for each 1000 lbs 8. Robertson, J.T. and Muir, W.W.: “Cardiopulmonary Subacute Equine Studies body weight. Eff ects of Butorphanol Tartrate in Horses,” Am. J. Analgesic Eff ects of Butorphanol Given at Horses were found to tolerate butorphanol given The dose may be repeated within 3 to 4 hours Vet. Res. 42: 41–44, 1981. Various Dosages in Horses with Abdominal Pain intravenously at dosages of 0.1, 0.3 and 0.5 mg/kg but treatment should not exceed 48 hours. 9. Kalpravidh, M. et al: “Eff ects of Butorphanol, every 4 hours for 48 hours followed by once daily Pre-clinical model studies and clinical fi eld trials in Flunixin, Levorphanol, Morphine, Pentazocine injections for a total of 21 days. The only detectable horses demonstrate that the analgesic eff ects of and Xylazine in Ponies,” Am. J. Vet. Res. 45: drug eff ects were slight transient ataxia observed TORBUGESIC are seen within 15 minutes following 217–223, 1984. occasionally in the high dosage group. No clinical, injection and persist for about 4 hours. laboratory, or gross or histopathologic evidence of Distributed by: any butorphanol-related toxicity was encountered HOW SUPPLIED Zoetis Inc. in the horses. 50 mL vials TORBUGESIC (butorphanol tartrate) Kalamazoo, MI 49007 Veterinary Injection, 10 mg base activity per mL. INDICATIONS 10 mL vials TORBUGESIC (butorphanol tartrate) Made in Spain TORBUGESIC (butorphanol tartrate) is indicated for Veterinary Injection, 10 mg base activity per mL. the relief of pain associated with colic in adult horses Revised: March 2015 and yearlings. Clinical studies in the horse have Store at controlled room temperature 20°-25°C shown that TORBUGESIC alleviates abdominal pain (68°-77°F) with excursions between 15°-30°C (59°- associated with torsion, impaction, intussusception, 86°F). *Pain threshold in butorphanol-treated colicky horses relative spasmodic and tympanic colic and postpartum pain. to placebo controls. REFERENCES CLINICAL PHARMACOLOGY WARNINGS 1. Pircio, A.W. et al: “The Pharmacology of Comparative Pharmacology A defi nite dosage-response relationship was DO NOT USE IN HORSES INTENDED FOR HUMAN Butorphanol,” Arch. Int. Pharmacodyn. Ther. 220 (2): In animals, butorphanol has been demonstrated to NADA 135-780, Approved by FDA detected in that butorphanol dosage of 0.1 mg/kg CONSUMPTION. NOT FOR HUMAN USE. 231–257, 1976. be 4 to 30 times more potent than morphine and was more eff ective than 0.05 mg/kg but not 2. Dobkin, A.B. et al: “Butorphanol and Pentazocine pentazocine (Talwin®-V) respectively.1 diff erent from 0.2 mg/kg in alleviating deep CAUTION in Patients with Severe Postoperative Pain,” Clin. In humans,In horses, butorphanol intravenous has beendosages shown of tobutorphanol have Repeated administration of butorphanol at 1 mg/kg DOSAGE Torbugesic® abdominal pain. TORBUGESIC, a potent analgesic, should be used Pharmacol. Ther. 18: 547–553, 1975. 5 to 7ranging times the from analgesic 0.05 to activity 0.4 mg/kg of morphine were shown and to be (10 times the recommended dose) every four hours The recommended dosage in the horse is 0.1 mg 7. Popio, K.A. et al: “Hemodynamic and Respiratory BUTORPHANOL TARTRATE eff ective in alleviating visceral2,3 and superfi cial pain for 48 withhours caution caused with constipation other sedative in oneor analgesic of two drugs of butorphanol3. Gilbert, perM.S. kilogramet al: “Intramuscular of body weight Butorphanol Eff ects of Morphine and Butorphanol,” Clin. 20 times thatAcute of pentazocine. Equine Studies Veterinary Injection for at least 4 hours, as illustrated in the following horses.as these are likely to produce additive eff ects. (0.05 mg/lb)and byMeperidine intravenous in Postoperativeinjection. This Pain,” is Clin. Pharmacol. Ther. 23: 281–287, 1978. ButorphanolRapid has 15 intravenous to 20 times administration the oral antitussive of butorphanol at fi gure: There are no well-controlled studies using equivalentPharmacol. to 5 mL of Ther.TORBUGESIC 20: 359–364, for each 1976. 1000 lbs 8. Robertson, J.T. and Muir, W.W.: “Cardiopulmonary activity of codeinea dosage or of dextromethorphan 2 mg/kg (20 times in the dogs recommended 4 Subacutebutorphanol Equine Studies in breeding horses, weanlings and body weight.4. Cavanagh, R.L. et al: “Antitussive Properties of Eff ects of Butorphanol Tartrate in Horses,” Am. J. and guinea pigs.dosage) to a previously unmedicated horse resulted Analgesic Eff ects of Butorphanol Given at Horses foals.were Therefore,found to toleratethe drug butorphanol should not givenbe used in The dose Butorphanol,”may be repeated Arch. Int. within Pharmacodyn. 3 to 4 hoursTher. 220 (2): Vet. Res. 42: 41–44, 1981. CAUTION As an antagonist,in a brief butorphanol episode ofis inabilityapproximately to stand, muscle Various Dosages in Horses with Abdominal Pain intravenouslythese groups. at dosages of 0.1, 0.3 and 0.5 mg/kg but treatment258–268, should 1976. not exceed 48 hours. 9. Kalpravidh, M. et al: “Eff ects of Butorphanol, Federal law restricts this drug to use by or on the equivalent tofasciculation, nalorphine anda convulsive30 times more seizure potent of 6 seconds 1 every 4 hours for 48 hours followed by once daily Pre-clinical5. S churig,model studiesJ.E. et aland: “Eff clinical ect of fi eldBut trialsorphanol in and Flunixin, Levorphanol, Morphine, Pentazocine order of a licensed veterinarian. than pentazocine.duration and recovery within three minutes. injections for a total ofADVERSE 21 days. REACTIONSThe only detectable horses demonstrateMorphine onthat Pulmonary the analgesic Mechanics, eff ects ofArte rial and Xylazine in Ponies,” Am. J. Vet. Res. 45: CardiopulmonaryThe same depressant dosage administeredeff ects are minimal after 10 successive drug effIn ects clinical were trialsslight in transient horses, ataxiathe most observed commonly TORBUGESICBlood are P seenressure, within and 15Venous minutes Plasma following Histamine in 217–223, 1984. DESCRIPTION after treatmentdaily with 1 mg/kgbutorphanol dosages as demonstratedof butorphanol resulted 5 6,7 8 occasionallyobserved in the side high eff ect dosage was slightgroup. ataxia No clinical, which lasted injection andthe persistAnesthetized for about Dog,” 4 hours. Arch. Int. Pharmacodyn. TORBUGESIC (butorphanol tartrate) is a totally in dogs , humansonly in transientand horses. sedative eff ects. During the 10-day laboratory,3 to 10or minutes.gross or histopathologic evidence of Ther. 233: 296–304, 1978. Distributed by: synthetic, centrally acting, narcotic agonist- Unlike classicalcourse narcotic of administration agonist analgesics at 1 mg/kg which (10 times the any butorphanol-related toxicity was encountered 6. Nagashmina,HOW SUPPLIEDH. et al: “Respiratory and Zoetis Inc. antagonist analgesic with potent antitussive are associatedrecommended with decreases use inlevel) blood in twopressure, horses, the only in the horses.Marked ataxia was reported in 1.5% of the 50 mL vialsCir culatoryTORBUGESIC Eff ects (butorphanol of Intravenous tartrate) Butorphanol Kalamazoo, MI 49007 activity. It is a member of the phenanthrene reduction in detectableheart rate anddrug concomitant eff ects were release transient of behavioral 327 horses treated. Mild sedation was reported in Veterinaryand Injection, Morphine,” 10 mg baseClin. activity Pharmacol. per mL. Ther. 19: series. The chemical name is Morphinan-3, 14- histamine, butorphanolchanges typical does of not narcotic cause agonisthistamine activity. These 1 9% of the horses.INDICATIONS 10 mL vials735–745, TORBUGESIC 1976. (butorphanol tartrate) Made in Spain diol, 17-(cyclobutylmethyl)-, (-)-, (S- (R*, R*))-2,3- release. included muscle fasciculation about the head and TORBUGESIC (butorphanol tartrate) is indicated for Veterinary Injection, 10 mg base activity per mL. dihydroxybutanedioate (1:1) (salt). It is a white, Furthermore,neck, the dysphoria,cardiopulmonary lateral nystagmus,eff ects of ataxia and the relief of pain associated with colic in adult horses Revised: March 2015 crystalline,In horses, water intravenous soluble substancedosages ofhaving butorphanol a butorphanol Repeatedsalivation. are administration not distinctly of dosage-related butorphanol at but 1 mg/kg DOSAGE molecularranging weight from of 0.05 477.55; to 0.4 its molecularmg/kg were formula shown is to berather (10 reach times a ceilingthe recommended eff ect beyond dose) which every further four hours and yearlings.The recommended Clinical studies dosage in inthe the horse horse have is 0.1 mg 7.Store Popio, at controlledK.A. et al: “Hemodynamic room temperature and Respiratory 20°-25°C C21H29NO2eff ective•C4H6O6. in alleviating visceral and superfi cial paindosage for increases 48 hours result caused in relatively constipation lesser in eff oneects. of two shown ofthat butorphanol TORBUGESIC peralleviates kilogram abdominal of body pain weight (68°-77°F)Eff ects withof Morphine excursions and between Butorphanol,” 15°-30°C (59°-Clin. for at least 4 hours, as illustrated in the followingReproduction: horses. Studies performed in mice and associated(0.05 with mg/lb) torsion, by impaction, intravenous intussusception, injection. This is 86°F).Pharmacol. Ther. 23: 281–287, 1978. Chemicalfi gure: Structure rabbits*Pain revealed threshold no in evidence butorphanol-treated of impaired colicky fertility horses or relative spasmodicequivalent and tympanic to 5 mL colic of TORBUGESIC and postpartum for each pain. 1000 lbs 8. Robertson, J.T. and Muir, W.W.: “Cardiopulmonary to placebo controls. harm Subacuteto the fetus Equine due to Studies butorphanol tartrate.
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  • ADVANCED RELEASE EMCDDA Technical Report on the New Psychoactive Substance N,N- Diethyl-2-[[4-(1-Methylethoxy)Phenyl]Methyl]-5-N

    ADVANCED RELEASE EMCDDA Technical Report on the New Psychoactive Substance N,N- Diethyl-2-[[4-(1-Methylethoxy)Phenyl]Methyl]-5-N

    ADVANCED RELEASE EMCDDA technical report on the new psychoactive substance N,N- diethyl-2-[[4-(1-methylethoxy)phenyl]methyl]-5-nitro-1H- benzimidazole-1-ethanamine (isotonitazene) Explanatory note: In the interests of public health protection the EMCDDA is releasing this report before formal copy editing and page layout in the EMCDDA house style. The final report will be available on the EMCDDA website in due course. Authors: Michael Evans-Brown1, István Ujváry2, Joanna De Morais1, Rachel Christie1, Anabela Almeida1, Rita Jorge1, Ana Gallegos1, Roumen Sedefov1 1European Monitoring Centre for Drugs and Drug Addiction, Praça Europa 1, Cais do Sodré, 1249–289 Lisbon, Portugal 2iKem BT, Búza u. 32, Budapest 1033, Hungary Recommended citation: EMCDDA (2020), EMCDDA technical report on the new psychoactive substance N,N-diethyl-2-[[4-(1-methylethoxy)phenyl]methyl]-5-nitro-1H- benzimidazole-1-ethanamine (isotonitazene), EMCDDA, Lisbon. © European Monitoring Centre for Drugs and Drug Addiction, 2019 Praça Europa 1, Cais do Sodré, 1249–289 Lisbon, Portugal Tel: +351 211210200 Email: [email protected] Web: www.emcdda.europa.eu 1 Purpose The purpose of this technical report to provide an analyses of the available information on N,N-diethyl-2-[[4-(1-methylethoxy)phenyl]methyl]-5-nitro-1H-benzimidazole-1-ethanamine (commonly known as isotonitazene), an opioid analgesic that has recently emerged on the drug market in Europe, to support a risk assessment of the substance that has been requested by the European Commission in accordance with Article 5c of Regulation (EC) No 1920/2006 (as amended). Parts of this report were prepared under an EMCDDA contract (ref.