Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C12H16N2S.ClH |
| Molecular Weight | 256.795 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CC1=CC=CC(C)=C1NC2=NCCCS2
InChI
InChIKey=QYEFBJRXKKSABU-UHFFFAOYSA-N
InChI=1S/C12H16N2S.ClH/c1-9-5-3-6-10(2)11(9)14-12-13-7-4-8-15-12;/h3,5-6H,4,7-8H2,1-2H3,(H,13,14);1H
DescriptionCurator's Comment: description was created based on several sources, including:
https://www.ncbi.nlm.nih.gov/pubmed/3062194 | http://www.ema.europa.eu/docs/en_GB/document_library/Maximum_Residue_Limits_-_Report/2009/11/WC500015345.pdf | https://www.drugs.com/vet/rompun-xylazine-100-mg-ml-injectable.html
Curator's Comment: description was created based on several sources, including:
https://www.ncbi.nlm.nih.gov/pubmed/3062194 | http://www.ema.europa.eu/docs/en_GB/document_library/Maximum_Residue_Limits_-_Report/2009/11/WC500015345.pdf | https://www.drugs.com/vet/rompun-xylazine-100-mg-ml-injectable.html
Xylazine was developed as an antihypertensive agent. During clinical studies in people xylazine was found to have excessive central nervous system depressant effects and it was subsequently introduced for veterinary use as a sedative, analgesic and relaxant. Xylazine is a potent alpha-2 adrenergic agonist. Xylazine in horses and Cervidae may occasionally cause slight muscle tremors, bradycardia with partial A-V heart block and a reduced respiratory rate. Movement in response to sharp auditory stimuli may be observed.
CNS Activity
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL3602 |
9.5 µM [IC50] | ||
Target ID: CHEMBL270 |
9.0 µM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Rompun Approved UseRompun™ (xylazine) should be used in horses and Cervidae when it is desirable to produce a state of sedation accompanied by a shorter period of analgesia. Launch Date1995 |
|||
| Primary | Rompun Approved UseRompun™ (xylazine) should be used in horses and Cervidae when it is desirable to produce a state of sedation accompanied by a shorter period of analgesia. Launch Date1995 |
Doses
| Dose | Population | Adverse events |
|---|---|---|
1000 mg single, intramuscular Abused dose Dose: 1000 mg Route: intramuscular Route: single Dose: 1000 mg Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: |
Disc. AE: CNS depression, Respiratory depression... AEs leading to discontinuation/dose reduction: CNS depression Sources: Respiratory depression Tachycardia Premature ventricular contractions Hyperglycemia Electrocardiogram change |
2400 mg single, intramuscular Abused dose Dose: 2400 mg Route: intramuscular Route: single Dose: 2400 mg Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: |
Disc. AE: CNS depression, Respiratory depression... AEs leading to discontinuation/dose reduction: CNS depression Sources: Respiratory depression Hypertension Hyperglycemia Ecchymosis |
400 mg single, oral Abused dose |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: |
Disc. AE: CNS depression, Respiratory depression... AEs leading to discontinuation/dose reduction: CNS depression Sources: Respiratory depression Hypotension (grade 1) Bradycardia Hyperglycemia Incontinence urinary Miosis Premature ventricular contractions |
1500 mg single, intramuscular Overdose Dose: 1500 mg Route: intramuscular Route: single Dose: 1500 mg Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: |
Disc. AE: CNS depression, Respiratory depression... AEs leading to discontinuation/dose reduction: CNS depression Sources: Respiratory depression Hypertension Bradycardia Hyperglycemia Miosis |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| CNS depression | Disc. AE | 1000 mg single, intramuscular Abused dose Dose: 1000 mg Route: intramuscular Route: single Dose: 1000 mg Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: |
| Electrocardiogram change | Disc. AE | 1000 mg single, intramuscular Abused dose Dose: 1000 mg Route: intramuscular Route: single Dose: 1000 mg Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: |
| Hyperglycemia | Disc. AE | 1000 mg single, intramuscular Abused dose Dose: 1000 mg Route: intramuscular Route: single Dose: 1000 mg Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: |
| Premature ventricular contractions | Disc. AE | 1000 mg single, intramuscular Abused dose Dose: 1000 mg Route: intramuscular Route: single Dose: 1000 mg Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: |
| Respiratory depression | Disc. AE | 1000 mg single, intramuscular Abused dose Dose: 1000 mg Route: intramuscular Route: single Dose: 1000 mg Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: |
| Tachycardia | Disc. AE | 1000 mg single, intramuscular Abused dose Dose: 1000 mg Route: intramuscular Route: single Dose: 1000 mg Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: |
| CNS depression | Disc. AE | 2400 mg single, intramuscular Abused dose Dose: 2400 mg Route: intramuscular Route: single Dose: 2400 mg Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: |
| Ecchymosis | Disc. AE | 2400 mg single, intramuscular Abused dose Dose: 2400 mg Route: intramuscular Route: single Dose: 2400 mg Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: |
| Hyperglycemia | Disc. AE | 2400 mg single, intramuscular Abused dose Dose: 2400 mg Route: intramuscular Route: single Dose: 2400 mg Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: |
| Hypertension | Disc. AE | 2400 mg single, intramuscular Abused dose Dose: 2400 mg Route: intramuscular Route: single Dose: 2400 mg Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: |
| Respiratory depression | Disc. AE | 2400 mg single, intramuscular Abused dose Dose: 2400 mg Route: intramuscular Route: single Dose: 2400 mg Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: |
| Bradycardia | Disc. AE | 400 mg single, oral Abused dose |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: |
| CNS depression | Disc. AE | 400 mg single, oral Abused dose |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: |
| Hyperglycemia | Disc. AE | 400 mg single, oral Abused dose |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: |
| Incontinence urinary | Disc. AE | 400 mg single, oral Abused dose |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: |
| Miosis | Disc. AE | 400 mg single, oral Abused dose |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: |
| Premature ventricular contractions | Disc. AE | 400 mg single, oral Abused dose |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: |
| Respiratory depression | Disc. AE | 400 mg single, oral Abused dose |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: |
| Hypotension | grade 1 Disc. AE |
400 mg single, oral Abused dose |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: |
| Bradycardia | Disc. AE | 1500 mg single, intramuscular Overdose Dose: 1500 mg Route: intramuscular Route: single Dose: 1500 mg Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: |
| CNS depression | Disc. AE | 1500 mg single, intramuscular Overdose Dose: 1500 mg Route: intramuscular Route: single Dose: 1500 mg Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: |
| Hyperglycemia | Disc. AE | 1500 mg single, intramuscular Overdose Dose: 1500 mg Route: intramuscular Route: single Dose: 1500 mg Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: |
| Hypertension | Disc. AE | 1500 mg single, intramuscular Overdose Dose: 1500 mg Route: intramuscular Route: single Dose: 1500 mg Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: |
| Miosis | Disc. AE | 1500 mg single, intramuscular Overdose Dose: 1500 mg Route: intramuscular Route: single Dose: 1500 mg Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: |
| Respiratory depression | Disc. AE | 1500 mg single, intramuscular Overdose Dose: 1500 mg Route: intramuscular Route: single Dose: 1500 mg Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Effects of Anethum graveolens L. seed extracts on experimental gastric irritation models in mice. | 2002-12-19 |
|
| Effects of treatment with oxytocin, xylazine butorphanol, guaifenesin, acepromazine, and detomidine on esophageal manometric pressure in conscious horses. | 2002-12 |
|
| In vitro effects of oxytocin, acepromazine, detomidine, xylazine, butorphanol, terbutaline, isoproterenol, and dantrolene on smooth and skeletal muscles of the equine esophagus. | 2002-12 |
|
| Cardiopulmonary effects of xylazine and acepromazine in pregnant cows in late gestation. | 2002-12 |
|
| Central sympathetic blockade ameliorates brain death-induced cardiotoxicity and associated changes in myocardial gene expression. | 2002-12 |
|
| Male and female rats express similar blood pressure responses to "push-pull" gravitational stress. | 2002-12 |
|
| Similar half-octave TTS protection of the cochlea by xylazine/ketamine or sympathectomy. | 2002-12 |
|
| Changes in hepatic and renal enzyme concentrations and heart and respiratory rates in new zealand white rabbits after anesthetic treatments. | 2002-11 |
|
| Rapid degradation of dominant-negative Rab27 proteins in vivo precludes their use in transgenic mouse models. | 2002-10-28 |
|
| Enhancement of alpha-adrenoceptor-mediated responses in prostate of testosterone-treated rat. | 2002-10-25 |
|
| Infusion of guaifenesin, ketamine, and medetomidine in combination with inhalation of sevoflurane versus inhalation of sevoflurane alone for anesthesia of horses. | 2002-10-15 |
|
| Clinical comparison of xylazine and medetomidine for premedication of horses. | 2002-10-15 |
|
| A comparison of balloon injury models of endovascular lesions in rat arteries. | 2002-09-27 |
|
| The scotopic threshold response of the dark-adapted electroretinogram of the mouse. | 2002-09-15 |
|
| Xylazine-induced attenuation of dorsal displacement of the soft palate associated with epiglottic dysfunction in a horse. | 2002-08-01 |
|
| Ultrasonographic evaluation of reticular motility in cows after administration of atropine, scopolamine and xylazine. | 2002-08 |
|
| Effects of electrical stimulation of the inferior colliculus on 2f1-f2 distortion product otoacoustic emissions in anesthetized guinea pigs. | 2002-08 |
|
| Evaluation of anesthesia effects in a rat animal model using otoacoustic emission protocols. | 2002-08 |
|
| Measurements of tumor tissue oxygen tension using a time-resolved luminescence-based optical oxylite probe: comparison with a paired survival assay. | 2002-08 |
|
| The effects of xylazine, detomidine, acepromazine and butorphanol on equine solid phase gastric emptying rate. | 2002-07 |
|
| Murine models of chronic Pseudomonas aeruginosa lung infection. | 2002-07 |
|
| Differential effects of anesthetics on mitochondrial K(ATP) channel activity and cardiomyocyte protection. | 2002-07 |
|
| Effect of general anesthesia and minor surgical trauma on urine and serum measurements in horses. | 2002-07 |
|
| Investigation of neurotransmission in vas deferens from alpha(2A/D)-adrenoceptor knockout mice. | 2002-07 |
|
| Cardiovascular phenotypes of kinin B2 receptor- and tissue kallikrein-deficient mice. | 2002-07 |
|
| The induction of hyperthermia in rabbit liver by means of duplex stainless steel thermoseeds. | 2002-06-28 |
|
| Periodate-treated, non-anticoagulant heparin-carrying polystyrene (NAC-HCPS) affects angiogenesis and inhibits subcutaneous induced tumour growth and metastasis to the lung. | 2002-06-05 |
|
| Use of azaperone and zuclopenthixol acetate to facilitate translocation of white-tailed deer (Odocoileus virginianus). | 2002-06 |
|
| Effects of ketamine-xylazine and isoflurane on insulin sensitivity in dehydroepiandrosterone sulfate-treated minipigs (Sus scrofa domestica). | 2002-06 |
|
| Impact of anesthesia on cardiac function during echocardiography in mice. | 2002-06 |
|
| Orthogonal polarisation spectral imaging as a new tool for the assessment of antivascular tumour treatment in vivo: a validation study. | 2002-05-20 |
|
| Use of the anesthetic combination of tiletamine, zolazepam, ketamine, and xylazine for neutering feral cats. | 2002-05-15 |
|
| Arthroscopic removal of dorsoproximal chip fractures of the proximal phalanx in standing horses. | 2002-05-08 |
|
| Comparison of epidural anaesthesia with lignocaine or xylazine in cats. | 2002-05 |
|
| Effects of propofol as an anaesthetic agent in adult lions (Panthera leo): a comparison with two established protocols. | 2002-04 |
|
| Respiratory mechanics in mice: strain and sex specific differences. | 2002-04 |
|
| Anesthesia affects the disposition of [18F]fluoro-A-85380: a PET study in monkeys. | 2002-04 |
|
| Thiram inhibits angiogenesis and slows the development of experimental tumours in mice. | 2002-03-04 |
|
| [Castration of male lambs and calves: explanations and comments of art. 65 TSchV]. | 2002-03 |
|
| Modulation of contraction by alpha(2A/D)-adrenoceptors in mouse aorta: evidence employing knockout technology. | 2002-03 |
|
| Spatial buffering during slow and paroxysmal sleep oscillations in cortical networks of glial cells in vivo. | 2002-02-01 |
|
| Early effects of tribromoethanol, ketamine/xylazine, pentobarbitol, and isoflurane anesthesia on hepatic and lymphoid tissue in ICR mice. | 2002-02 |
|
| Colonoscopy in mice. | 2002-01 |
|
| Neurohormonal and metabolic effects of medetomidine compared with xylazine in beagle dogs. | 2002-01 |
|
| Assessing the emetic potential of PDE4 inhibitors in rats. | 2002-01 |
|
| Changes in the acoustically evoked activity in the inferior colliculus of the rat after functional ablation of the auditory cortex. | 2002 |
|
| Semen collection from mice: electroejaculation. | 2002 |
|
| Adaptations to iron deficiency: cardiac functional responsiveness to norepinephrine, arterial remodeling, and the effect of beta-blockade on cardiac hypertrophy. | 2002 |
|
| Anesthesia protocol for hyperpnea-induced airway obstruction in the guinea pig. | 2001-10 |
|
| Optimization of intraperitoneal injection anesthesia in mice: drugs, dosages, adverse effects, and anesthesia depth. | 2001-10 |
Patents
Sample Use Guides
Horse Dosage:
Intravenously–0.5 mL/100 lbs body weight (0.5 mg/lb)
Intramuscularly–1.0 mL/100 lbs body weight (1.0 mg/lb)
Route of Administration:
Other
GLP-compliant studies on mutagenicity included Salmonella-microsomal assay with and without metabolic activation (0.4 to 12 mg of Xylazine on plate, with and without metabolic activation), mammalian forward point mutation assay (HPRT locus) in Chinese hamster lung cells (V79) (2 to 40 ug of Xylazine per ml, with metabolic activation and 62 to 1250 ug of Xylazine per ml, without metabolic activation). The compound to be devoid of mutagenic potential.
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| Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C29709
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DTXSID6040248
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m11547
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1366222
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68554
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C75050
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CHEMBL297362
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NGC3S0882S
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149566
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ACTIVE MOIETY
SUBSTANCE RECORD
