Buy Ketamine HCL Crystal Powder online.A medication used for anesthesia to stop pain during surgeries.
DrugBank IDDB01221
TypeSmall Molecule
Therapeutic Categories
- Anesthetics, General
Mechanism of Action
- Glutamate receptor ionotropic, NMDA 3A
Antagonist
- 5-hydroxytryptamine receptor 3A
Potentiator
- Neuronal acetylcholine receptor subunit alpha-7
Antagonist
- + 2 more targets
Identification
- Summary
- Ketamine is a rapid-acting general anesthetic and NMDA receptor antagonist used for induction of anesthesia diagnostic and surgical procedures typically in combination with a muscle relaxant.Buy Ketamine HCL Crystal Powder online
- Brand Names
-
Ketalar
- Generic Name
- Ketamine
- DrugBank Accession Number
- DB01221
- Background
- Ketamine is an NMDA receptor antagonist with a potent anesthetic effect.6 It was developed in 1963 as a replacement for phencyclidine (PCP) by Calvin Stevens at Parke Davis Laboratories. It started being used for veterinary purposes in Belgium and in 1964 was proven that compared to PCP, it produced minor hallucinogenic effects and shorter psychotomimetic effects. It was FDA approved in 1970, and from there, it has been used as an anesthetic for children or patients undergoing minor surgeries but mainly for veterinary purposes.14
- Type
- Small Molecule
- Groups
- Approved, Investigational, Vet approved
- Structure
- Weight
- Average: 237.725
Monoisotopic: 237.092041846 - Chemical Formula
- C13H16ClNO
- Synonyms
-
- DL-ketamine
- Ketamina
- Kétamine
- Ketamine
- Ketaminum
- NMDA
- External IDs
-
- 100477-72-3
- NSC-70151
Pharmacology
- Indication
- Ketamine is indicated as an anesthetic agent for recommended diagnostic and surgical procedures. If skeletal muscle relaxation is needed, it should be combined with a muscle relaxant. If the surgical procedure involves visceral pain, it should be supplemented with an agent that obtunds visceral pain. Ketamine can be used for induction of anesthesia prior other general anesthetic agents and as a supplement of low potency agents.15,LabelReports have indicated a potential use of ketamine as a therapeutic tool for the management of depression when administered in lower doses.7 These reports have increased the interest for ketamine in this area and several clinical trials are launched for this indication.16,8Ketamine Crystals Order Online USA
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- Contraindications & Blackbox Warnings
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- Pharmacodynamics
- Ketamine is a rapid-acting general anesthetic producing an anesthetic state characterized by profound analgesia, normal pharyngeal-laryngeal reflexes, normal or slightly enhanced skeletal muscle tone, cardiovascular and respiratory stimulation, and occasionally a transient and minimal respiratory depression. The anesthetic state produced by Ketamine has been termed as “dissociative anesthesia” in that it appears to selectively interrupt association pathways of the brain before producing somesthetic sensory blockade. It may selectively depress the thalamoneocortical system before significantly obtunding the more ancient cerebral centers and pathways (reticular-activating and limbic systems).2Ketamine enhances descending inhibiting serotoninergic pathways and can exert antidepressive effects. These effects are seen in concentrations ten times lower than the needed concentration for anesthetic proposes. The effect of ketamine can be described as analgesic by the prevention of central sensitization in dorsal horn neurons as well as by the inhibition on the synthesis of nitric oxide. Ketamine can present cardiovascular changes and bronchodilatation.9
- Mechanism of action
- Ketamine interacts with N-methyl-D-aspartate (NMDA) receptors, opioid receptors, monoaminergic receptors, muscarinic receptors and voltage sensitive Ca ion channels. Unlike other general anaesthetic agents, ketamine does not interact with GABA receptors.5
Target Actions Organism AGlutamate receptor ionotropic, NMDA 3A antagonistHumans A5-hydroxytryptamine receptor 3A potentiatorHumans ANeuronal acetylcholine receptor subunit alpha-7 antagonistHumans ACholinesterase inhibitorHumans ANitric oxide synthase 1 inhibitorHumans USubstance-P receptor antagonistHumans UD(2) dopamine receptor agonistpartial agonistHumans UDelta-type opioid receptor binderHumans USodium-dependent noradrenaline transporter inhibitorHumans UKappa-type opioid receptor agonistHumans UMu-type opioid receptor binderHumans UMuscarinic acetylcholine receptor binderHumans U5-hydroxytryptamine receptor 2 antagonistHumans U5-hydroxytryptamine receptor 1 antagonistHumans - Absorption
- Ketamine absorption is very rapid and the bioavailability is around 93%. After the first pass metabolism, only 17% of the administered dose is absorbed.10 It distributes very rapidly and presents a distribution half-life of 1.95 min.12 The Cmax levels at peak reach 0.75 mcg/ml in plasma and 0.2 mcg/ml in cerebrospinal fluid.15
- Volume of distribution
- The apparent volume of distribution of the central compartment and at steady-state are 371.3 ml/kg and 4060.3 ml/kg, respectively.13
- Protein binding
- The plasma protein binding of ketamine accounts for 53.5% of the administered dose.12
- Metabolism
- Ketamine presents a mainly hepatic metabolism and its major metabolite is norketamine. The biotransformation of ketamine corresponds to N-dealkylation, hydroxylation of the cyclohexone ring, conjugation to glucuronic acid and dehydration of the hydroxylated metabolites for the formation of cyclohexene derivatives.10
Hover over products below to view reaction partners
- Route of elimination
- Pharmacokinetic studies have resulted in the recovery of 85-95% of the administered dose in urine mainly in the form of metabolites. Some other routes of elimination of ketamine are bile and feces. When administered intravenously the resultant recovery is distributed by 91% of the administered dose in urine and 3% in feces.15
- Half-life
- The reported half-life in preclinical studies for ketamine is 186 min.10
- Clearance
- The clearance rate of ketamine is high and of around 95 L/h/70kg.11
- Adverse Effects
-
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- Toxicity
- Preclinical studies related to the blocking of NMDA receptors have shown an increase in apoptosis in the developing brain which results in cognitive deficits when used for longer than 3 hours. Toxicity studies regarding carcinogenesis have not been performed. Regarding mutagenesis and fertility, ketamine showed to be clastogenic and to not have effects on fertility.Label
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
-
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.Buy ketamine – ketamine for sale – liquid ketamine for sale
- Food Interactions
-
- Avoid alcohol.
Products
-
Drug product information from 10+ global regionsOur datasets provide approved product information including:
dosage, form, labeller, route of administration, and marketing period. - Product Ingredients
-
Ingredient UNII CAS InChI Key Ketamine hydrochloride O18YUO0I83 1867-66-9 VCMGMSHEPQENPE-UHFFFAOYSA-N - International/Other Brands
- Ketaject (Bristol-Myers Squibb) / Ketanest (Parke Davis)
- Brand Name Prescription Products
-
- Generic Prescription Products
-
- Unapproved/Other Products
-
Categories
- ATC Codes
- N01AX03 — Ketamine
- Drug Categories
-
- Agents producing tachycardia
- Amino Acids
- Amino Acids, Acidic
- Amino Acids, Dicarboxylic
- Amino Acids, Peptides, and Proteins
- Analgesics
- Anesthetics
- Anesthetics, Dissociative
- Anesthetics, General
- Anesthetics, Intravenous
- Central Nervous System Agents
- Central Nervous System Depressants
- Cholinesterase Inhibitors
- Cyclohexanes
- Cycloparaffins
- Cytochrome P-450 CYP2B6 Substrates
- Cytochrome P-450 CYP2C8 Substrates
- Cytochrome P-450 CYP2C9 Substrates
- Cytochrome P-450 CYP3A Inducers
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inducers
- Cytochrome P-450 CYP3A4 Inducers (strength unknown)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Enzyme Inducers
- Cytochrome P-450 Substrates
- Drugs that are Mainly Renally Excreted
- Excitatory Amino Acid Agents
- Excitatory Amino Acid Agonists
- Excitatory Amino Acid Antagonists
- Miscellaneous General Anesthetics
- N-Methylaspartate, agonists
- N-Methylaspartate, antagonists & inhibitors
- Nervous System
- Neurotransmitter Agents
- NMDA Receptor Antagonists
- Peripheral Nervous System Agents
- Sensory System Agents
- Vasodilating Agents
- Chemical TaxonomyProvided by Classyfire
-
- Description
- This compound belongs to the class of organic compounds known as chlorobenzenes. These are compounds containing one or more chlorine atoms attached to a benzene moiety.
- Kingdom
- Organic compounds
- Super Class
- Benzenoids
- Class
- Benzene and substituted derivatives
- Sub Class
- Halobenzenes
- Direct Parent
- Chlorobenzenes
- Alternative Parents
- Aralkylamines / Aryl chlorides / Cyclic ketones / Dialkylamines / Organopnictogen compounds / Organochlorides / Organic oxides / Hydrocarbon derivatives
- Substituents
- Amine / Aralkylamine / Aromatic homomonocyclic compound / Aryl chloride / Aryl halide / Carbonyl group / Chlorobenzene / Cyclic ketone / Hydrocarbon derivative / Ketone
- Molecular Framework
- Aromatic homomonocyclic compounds
- External Descriptors
- secondary amino compound, monochlorobenzenes, cyclohexanones (CHEBI:6121)
- Affected organisms
-
- Humans and other mammals
Chemical Identifiers
- UNII
- 690G0D6V8H
- CAS number
- 6740-88-1
- InChI Key
- YQEZLKZALYSWHR-UHFFFAOYSA-N
- InChI
-
InChI=1S/C13H16ClNO/c1-15-13(9-5-4-8-12(13)16)10-6-2-3-7-11(10)14/h2-3,6-7,15H,4-5,8-9H2,1H3
- IUPAC Name
-
2-(2-chlorophenyl)-2-(methylamino)cyclohexan-1-one
- SMILES
-
CNC1(CCCCC1=O)C1=CC=CC=C1Cl
References
- Synthesis Reference
- John A. Flores, Kenton L. Crowley, “Process for the preparation of ketamine ointment.” U.S. Patent US5817699, issued June, 1995.US5817699
- General References
-
- Harrison NL, Simmonds MA: Quantitative studies on some antagonists of N-methyl D-aspartate in slices of rat cerebral cortex. Br J Pharmacol. 1985 Feb;84(2):381-91. [Article]
- Bergman SA: Ketamine: review of its pharmacology and its use in pediatric anesthesia. Anesth Prog. 1999 Winter;46(1):10-20. [Article]
- Bonanno FG: Ketamine in war/tropical surgery (a final tribute to the racemic mixture). Injury. 2002 May;33(4):323-7. [Article]
- Lankenau SE, Sanders B, Bloom JJ, Hathazi D, Alarcon E, Tortu S, Clatts MC: First injection of ketamine among young injection drug users (IDUs) in three U.S. cities. Drug Alcohol Depend. 2007 Mar 16;87(2-3):183-93. Epub 2006 Sep 18. [Article]
- Reboso Morales JA, Gonzalez Miranda F: [Ketamine]. Rev Esp Anestesiol Reanim. 1999 Mar;46(3):111-22. [Article]
- Ivani G, Vercellino C, Tonetti F: Ketamine: a new look to an old drug. Minerva Anestesiol. 2003 May;69(5):468-71. [Article]
- Yang Y, Cui Y, Sang K, Dong Y, Ni Z, Ma S, Hu H: Ketamine blocks bursting in the lateral habenula to rapidly relieve depression. Nature. 2018 Feb 14;554(7692):317-322. doi: 10.1038/nature25509. [Article]
- Kirby T: Ketamine for depression: the highs and lows. Lancet Psychiatry. 2015 Sep;2(9):783-4. doi: 10.1016/S2215-0366(15)00392-2. [Article]
- Xu J, Lei H: Ketamine-an update on its clinical uses and abuses. CNS Neurosci Ther. 2014 Dec;20(12):1015-20. doi: 10.1111/cns.12363. [Article]
- Clements JA, Nimmo WS, Grant IS: Bioavailability, pharmacokinetics, and analgesic activity of ketamine in humans. J Pharm Sci. 1982 May;71(5):539-42. [Article]
- Fanta S, Kinnunen M, Backman JT, Kalso E: Population pharmacokinetics of S-ketamine and norketamine in healthy volunteers after intravenous and oral dosing. Eur J Clin Pharmacol. 2015 Apr;71(4):441-7. doi: 10.1007/s00228-015-1826-y. Epub 2015 Mar 1. [Article]
- Kaka JS, Hayton WL: Pharmacokinetics of ketamine and two metabolites in the dog. J Pharmacokinet Biopharm. 1980 Apr;8(2):193-202. [Article]
- Pypendop BH, Ilkiw JE: Pharmacokinetics of ketamine and its metabolite, norketamine, after intravenous administration of a bolus of ketamine to isoflurane-anesthetized dogs. Am J Vet Res. 2005 Dec;66(12):2034-8. doi: 10.2460/ajvr.2005.66.2034. [Article]
- Ketamine [Link]
- Ketamine monograph [Link]
- Time magazine [Link]
- External Links
-
- Human Metabolome Database
- HMDB0015352
- KEGG Drug
- D08098
- KEGG Compound
- C07525
- PubChem Compound
- 3821
- PubChem Substance
- 46508295
- ChemSpider
- 3689
- BindingDB
- 50044140
- 6130
- ChEBI
- 6121
- ChEMBL
- CHEMBL742
- Therapeutic Targets Database
- DAP001148
- PharmGKB
- PA450144
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Ketamine
- FDA label
-
Download (228 KB)
- MSDS
-
Download (67.5 KB)
Clinical Trials
- Clinical Trials
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Pharmacoeconomics
- Manufacturers
-
Not Available
- Packagers
-
- Bedford Labs
- Ben Venue Laboratories Inc.
- Bioniche Pharma
- Hospira Inc.
- JHP Pharmaceuticals LLC
- Medisca Inc.
- Monarch Pharmacy
- Pharmedium
- Physicians Total Care Inc.
- Dosage Forms
- Prices
-
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
-
Property Value Source melting point (°C) 92.5ºC Medical toxicology of drug abuse. (2012) water solubility Soluble ‘MSDS’ logP 3.120 Medical toxicology of drug abuse. (2012) pKa 7.5 Ketamine monograph - Predicted Properties
-
Property Value Source Water Solubility 0.0464 mg/mL ALOGPS logP 2.69 ALOGPS logP 3.35 Chemaxon logS -3.7 ALOGPS pKa (Strongest Acidic) 19.77 Chemaxon pKa (Strongest Basic) 7.16 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 2 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 29.1 Å2 Chemaxon Rotatable Bond Count 2 Chemaxon Refractivity 65.55 m3·mol-1 Chemaxon Polarizability 24.97 Å3 Chemaxon Number of Rings 2 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber’s Rule Yes Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
-
Property Value Probability Human Intestinal Absorption + 0.9974 Blood Brain Barrier + 0.9826 Caco-2 permeable + 0.6326 P-glycoprotein substrate Substrate 0.5753 P-glycoprotein inhibitor I Non-inhibitor 0.5948 P-glycoprotein inhibitor II Non-inhibitor 0.8383 Renal organic cation transporter Non-inhibitor 0.6737 CYP450 2C9 substrate Non-substrate 0.6363 CYP450 2D6 substrate Substrate 0.8918 CYP450 3A4 substrate Substrate 0.7407 CYP450 1A2 substrate Non-inhibitor 0.7323 CYP450 2C9 inhibitor Non-inhibitor 0.7985 CYP450 2D6 inhibitor Non-inhibitor 0.6912 CYP450 2C19 inhibitor Non-inhibitor 0.5347 CYP450 3A4 inhibitor Non-inhibitor 0.8253 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.5426 Ames test Non AMES toxic 0.7223 Carcinogenicity Non-carcinogens 0.8878 Biodegradation Not ready biodegradable 0.9937 Rat acute toxicity 2.3939 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.8859 hERG inhibition (predictor II) Inhibitor 0.6047
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
-
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 152.3173949 predictedDarkChem Lite v0.1.0 [M-H]- 149.78523 predictedDeepCCS 1.0 (2019) [M+H]+ 152.3352949 predictedDarkChem Lite v0.1.0 [M+H]+ 152.14323 predictedDeepCCS 1.0 (2019) [M+Na]+ 152.3356949 predictedDarkChem Lite v0.1.0 [M+Na]+ 159.28464 predictedDeepCCS 1.0 (2019)