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Lidocaine
Systematic (IUPAC) name
2-(diethylamino)-
N-(2,6-dimethylphenyl)acetamide
Identifiers
CAS number 137-58-6
ATC code N01BB02 C01BB01 D04AB01 S02DA01 C05AD01
PubChem 3676
DrugBank APRD00479
Chemical data
Formula C14H22N2O 
Mol. mass 234. IUPAC Nomenclature is a system of naming Chemical compounds and of describing the science of Chemistry in general CAS registry numbers are unique numerical identifiers for Chemical compounds Polymers biological sequences mixtures and Alloys They are also referred to The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs It is controlled by the WHO Collaborating Centre for Drug A section of the Anatomical Therapeutic Chemical Classification System. A section of the Anatomical Therapeutic Chemical Classification System. A section of the Anatomical Therapeutic Chemical Classification System. A section of the Anatomical Therapeutic Chemical Classification System. A section of the Anatomical Therapeutic Chemical Classification System. PubChem is a Database of chemical Molecules The system is maintained by the National Center for Biotechnology Information (NCBI a component The DrugBank database available at the University of Alberta is a unique Bioinformatics and Cheminformatics resource that combines detailed drug (i A chemical formula is a way of expressing information about the Atoms that constitute a particular Chemical compound, and how the relationship between those atoms changes Carbon (kɑɹbən is a Chemical element with the symbol C and its Atomic number is 6 Hydrogen (ˈhaɪdrədʒən is the Chemical element with Atomic number 1 Nitrogen (ˈnaɪtɹəʤɪn is a Chemical element that has the symbol N and Atomic number 7 and Atomic weight 14 Oxygen (from the Greek roots ὀξύς (oxys (acid literally "sharp" from the taste of acids and -γενής (-genēs (producer literally begetteris the The molecular mass (abbreviated m of a substance, more commonly referred to as molecular weight and abbreviated as MW, is the Mass of one 34 g/mol
SMILES eMolecules & PubChem
Physical data
Melt. point 68 °C (154 °F)
Pharmacokinetic data
Bioavailability 35% (oral)
3% (topical)
Metabolism Hepatic, 90% CYP1A2-mediated
Half life 1. The melting point of a solid is the temperature range at which it changes state from solid to Liquid. In Pharmacology, bioavailability is used to describe the fraction of an administered Dose of unchanged drug that reaches the Systemic circulation, one of Drug metabolism is the Metabolism of drugs, their Biochemical modification or degradation usually through specialized enzymatic systems The liver is a vital organ in the human body and is present in Vertebrates and some other animals Cytochrome P450 1A2 (abbreviated CYP1A2) a member of the Cytochrome P450 mixed-function oxidase system is involved in the metabolism of Xenobiotics The biological half-life of a substance is the time it takes for a substance (drug radioactive nuclide or other to lose half of its pharmacologic physiologic or radiologic activity 5–2 hours
Excretion renal
Therapeutic considerations
Pregnancy cat.

A(AU)
Legal status

Prescription Only (S4)(AU) ?(US)
Routes IV, subcutaneous, topical

Lidocaine (INN) (pronounced /ˈlaɪdoʊkeɪn/) or lignocaine (former BAN) (/ˈlɪgnoʊkeɪn/) is a common local anesthetic and antiarrhythmic drug. Excretion is the process of eliminating waste products of Metabolism and other non-useful materials The kidneys are complicated organs that have numerous biological roles The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical if it is used as directed by the mother during For a topic outline on this subject see List of basic Australia topics. The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction The Standard for the Uniform Scheduling of Drugs and Poisons, abbreviated SUSDP, is a document used in the regulation of drugs and poisons in Australia. For a topic outline on this subject see List of basic Australia topics. The United States of America —commonly referred to as the In Pharmacology and Toxicology, a route Intravenous therapy or IV therapy is the giving of Liquid substances directly into a Vein. The subcutaneous tissue or subcutis is the layer of Loose connective tissue directly underlying the Dermis. In Medicine, a topical Medication is applied to body surfaces such as the Skin or Mucous membranes for example the Vagina An International Nonproprietary Name ( INN; also known as rINN, for recommended International Nonproprietary Name or pINN for proposed A British Approved Name ( BAN) is the official non-proprietary or generic name given to a Pharmaceutical Substance, as defined in the British Pharmacopoeia A local anesthetic is a drug that causes reversible Local anesthesia and a loss of Nociception. Antiarrhythmic agents are a group of Pharmaceuticals that are used to suppress fast rhythms of the Heart ( Cardiac arrhythmias) such as Atrial fibrillation Lidocaine is used topically to relieve itching, burning and pain from skin inflammations, injected as a dental anesthetic, and in minor surgery. The most commonly encountered lidocaine preparations are marketed by Abraxis Pharmaceutical Products under the brand names Xylocaine and Xylocard, and as 'Lanacane' topical ointment in the UK, though lidocaine is also found in many other proprietary preparations.

Contents

History

Lidocaine, the first amino amide-type local anesthetic, was first synthesized under the name xylocaine by Nils Löfgren in 1943. Amines are Organic compounds and Functional groups that contain a basic Nitrogen Atom with a Lone pair. In Chemistry, an amide is one of three kinds of Compounds (sometimes called acid amide the organic Functional group characterized Nils Löfgren was a Swedish Scientist who developed the anaesthetic Lidocaine (xylocaine in 1943. [1] His colleague Bengt Lundqvist made the first injection anesthesia experiments on himself. [1]It was first marketed in 1948. Year 1948 ( MCMXLVIII) was a Leap year starting on Thursday (link will display the 1948 calendar of the Gregorian calendar.

Pharmacokinetics

Lidocaine has a more rapid onset of action and longer duration of action than amino ester-type local anesthetics such as procaine. Amines are Organic compounds and Functional groups that contain a basic Nitrogen Atom with a Lone pair. Esters are a class of Chemical compounds and Functional groups Esters consist of an inorganic or organic Acid in which at least Procaine is a Local anesthetic drug of the Amino Ester group It is used primarily to reduce the pain of Intramuscular injection of It is approximately 90% metabolized in the liver by CYP1A2 (and to a minor extent CYP3A4) to the pharmacologically-active metabolites monoethylglycinexylidide and glycinexylidide. The liver is a vital organ in the human body and is present in Vertebrates and some other animals Cytochrome P450 1A2 (abbreviated CYP1A2) a member of the Cytochrome P450 mixed-function oxidase system is involved in the metabolism of Xenobiotics Cytochrome P450 3A4 (abbreviated CYP3A4) ( a member of the Cytochrome P450 mixed-function oxidase system is one of the most important enzymes involved in the metabolism Metabolomics is the "systematic study of the unique chemical fingerprints that specific cellular processes leave behind" - specifically the study of their small-molecule metabolite

The elimination half-life of lidocaine is approximately 1. Half-Life (computer-game page here It's already listed in the disambiguation page 5–2 hours in most patients. This may be prolonged in patients with hepatic impairment (average 343 minutes) or congestive heart failure (average 136 minutes). Liver failure is the inability of the Liver to perform its normal synthetic and metabolic function as part of normal physiology Heart failure is a Cardiac condition that occurs when a problem with the structure or function of the Heart impairs its ability to supply (Thomson et al. , 1973)

Pharmacodynamics

Anesthesia

Lidocaine alters depolarization in neurons, by blocking the fast voltage gated sodium (Na+) channels in the cell membrane[2]. Neurons (ˈnjuːɹɒn also known as neurones and nerve cells) are responsive cells in the Nervous system that process and transmit information Sodium channels are Integral membrane proteins that form Ion channels, conducting sodium ions ( Na+) through a cell's Plasma membrane With sufficient blockade, the membrane of the presynaptic neuron will not depolarize and so fail to transmit an action potential, leading to its anesthetic effects. In Neurophysiology, the action potential is a self-regenerating Wave of Electrochemical activity that allows Nerve cells to carry a signal Careful titration allows for a high degree of selectivity in the blockage of sensory neurons, whereas higher concentrations will also affect other modalities of neuron signaling.

Clinical use

Indications

Indications for the use of lidocaine include:

Topical lidocaine has been shown to relieve postherpetic neuralgia in some patients, although there is not enough study evidence to recommend it as a first-line treatment. Dysrhythmia redirects here For the American band see Dysrhythmia (band. Ventricular fibrillation ( V-fib or VF) is a condition in which there is uncoordinated contraction of the Cardiac muscle of the ventricles in the Ventricular tachycardia ( V-tach or VT) is a Tachycardia, or fast heart rhythm that originates in one of the ventricles of the Heart A cardiac arrest, also known as cardiorespiratory arrest, cardiopulmonary arrest or circulatory arrest, is the abrupt cessation of normal circulation of In Medicine, a topical Medication is applied to body surfaces such as the Skin or Mucous membranes for example the Vagina Postherpetic neuralgia (PHN is a Neuralgia caused by the Varicella zoster virus. A first-line treatment or first-line therapy is a Medical therapy recommended for the initial treatment of a Disease, sign or Symptom (Khaliq et al. , 2007)

Intravenous or intraosseous lidocaine is used to blunt the effects of laryngoscopy during rapid sequence intubation procedures, especially in cases of head injury. Intravenous therapy or IV therapy is the giving of Liquid substances directly into a Vein. Intraosseous infusion is the process of injection directly into the Marrow of the bone A laryngoscope ( Larynx + Scope) is a medical instrument that is used to obtain a view of the vocal folds and the glottis which is the space between the cords

Contraindications

Contraindications for the use of lidocaine include:

Adverse drug reactions

Adverse drug reactions (ADRs) are rare when lidocaine is used as a local anesthetic and is administered correctly. A heart block is a disease in the electrical system of the Heart. A sinoatrial block is a type of Heart block which involves an impairment of conduction at the Sinoatrial node. An adverse drug reaction (abbreviated ADR) or adverse drug event (abbreviated ADE) is an expression that describes the unwanted negative consequences Quinidine is a Pharmaceutical agent that acts as a Class I antiarrhythmic agent in the Heart. Flecainide acetate ( fle KAY nide) is a class Ic Antiarrhythmic agent used to prevent and treat tachyarrhythmias (abnormal fast rhythms of the Heart Disopyramide ( INN, trade names Norpace and Rythmodan) is an Antiarrhythmic Medication. Procainamide (proe-KANE-a-mide ( INN, trade names Pronestyl, Procan, Procanbid) is a Pharmaceutical Antiarrhythmic agent used for Antiarrhythmic agents are a group of Pharmaceuticals that are used to suppress fast rhythms of the Heart ( Cardiac arrhythmias) such as Atrial fibrillation Amiodarone is an Antiarrhythmic agent (medication used for irregular heart beat used for various types of tachyarrhythmias (fast forms of irregular heart beat both ventricular In Physiology and Medicine, hypotension refers to an abnormally low Blood pressure. Dysrhythmia redirects here For the American band see Dysrhythmia (band. Bradycardia, as applied to adult medicine is defined as a resting Heart rate of under 60 beats per minute though it is seldom symptomatic until the rate drops below 50 beat/min The rate of cardiac contraction is determined by the intrinsic rate of depolarisation of the cardiac cells An adverse drug reaction (abbreviated ADR) or adverse drug event (abbreviated ADE) is an expression that describes the unwanted negative consequences Most ADRs associated with lidocaine for anesthesia relate to administration technique (resulting in systemic exposure) or pharmacological effects of anesthesia, but allergic reactions can rarely occur. Allergy is a disorder of the Immune system often also referred to as Atopy. .

Systemic exposure to excessive quantities of lidocaine mainly result in central nervous system (CNS) and cardiovascular effects – CNS effects usually occur at lower blood plasma concentrations and additional cardiovascular effects present at higher concentrations, though cardiovascular collapse may also occur with low concentrations. In Vertebrates the central nervous system ( CNS) is the part of the Nervous system which is enclosed in the Meninges. This is an article about the rock music band "Circulatory System" Blood plasma is the Liquid component of Blood, in which the Blood cells are suspended CNS effects may include CNS excitation (nervousness, tingling around the mouth, tinnitus, tremor, dizziness, blurred vision, seizures) followed by depression, and with increasingly heavier exposure: drowsiness, loss of consciousness, respiratory depression and apnea). Tinnitus (tɪˈnaɪtəs or /ˈtɪnɪtəs/ from the Latin word for " Ringing " is the perception of sound within the human ear in the absence of corresponding An epileptic seizure is caused by excessive and/or hypersynchronous electrical Neuronal activity and is usually self-limiting In Medicine, hypoventilation (also known as respiratory depression) occurs when ventilation is inadequate ( hypo means "below" to perform needed Cardiovascular effects include hypotension, bradycardia, arrhythmias, and/or cardiac arrest – some of which may be due to hypoxemia secondary to respiratory depression. In Physiology and Medicine, hypotension refers to an abnormally low Blood pressure. Bradycardia, as applied to adult medicine is defined as a resting Heart rate of under 60 beats per minute though it is seldom symptomatic until the rate drops below 50 beat/min Dysrhythmia redirects here For the American band see Dysrhythmia (band. A cardiac arrest, also known as cardiorespiratory arrest, cardiopulmonary arrest or circulatory arrest, is the abrupt cessation of normal circulation of Chronic Hypoxia is a pathological condition in which the body as a whole ( generalized hypoxia) or region of the body ( tissue hypoxia) is deprived of adequate (Rossi, 2006)

ADRs associated with the use of intravenous lidocaine are similar to toxic effects from systemic exposure above. These are dose-related and more frequent at high infusion rates (≥3 mg/minute). Common ADRs include: headache, dizziness, drowsiness, confusion, visual disturbances, tinnitus, tremor, and/or paraesthesia. Tinnitus (tɪˈnaɪtəs or /ˈtɪnɪtəs/ from the Latin word for " Ringing " is the perception of sound within the human ear in the absence of corresponding Paresthesia (pron /ˌpɛɹɪsˈθiʒə/ paraesthesia in British English, pron Infrequent ADRs associated with the use of lidocaine include: hypotension, bradycardia, arrhythmias, cardiac arrest, muscle twitching, seizures, coma, and/or respiratory depression. In Physiology and Medicine, hypotension refers to an abnormally low Blood pressure. Bradycardia, as applied to adult medicine is defined as a resting Heart rate of under 60 beats per minute though it is seldom symptomatic until the rate drops below 50 beat/min Dysrhythmia redirects here For the American band see Dysrhythmia (band. A cardiac arrest, also known as cardiorespiratory arrest, cardiopulmonary arrest or circulatory arrest, is the abrupt cessation of normal circulation of An epileptic seizure is caused by excessive and/or hypersynchronous electrical Neuronal activity and is usually self-limiting In Medicine, a coma (from the Greek koma, meaning deep sleep is a profound state of Unconsciousness. (Rossi, 2006)

Insensitivity to lidocaine

Relative insensitivity to lidocaine runs in families. In hypokalemic sensory overstimulation, relative insensitivity to lidocaine has been described in people who also have attention deficit hyperactivity disorder. Hypokalemic sensory overstimulation is a form of Attention deficit hyperactivity disorder that has several similarities to disorders of ion channels in particular to the muscle Attention-Deficit Hyperactivity Disorder (ADHD is a neurobehavioral developmental disorder affecting about 3-5% of the world's population In dental anesthesia, a relative insensitivity to lidocaine can occur for anatomical reasons due to unexpected positions of nerves.

Dosage forms

Lidocaine, usually in the form of lidocaine hydrochloride, is available in various forms including:

Additive in cocaine

Lidocaine is often added to cocaine as a diluent. Prilocaine (ˈpraɪloʊkeɪn is a Local anesthetic of the Amino Amide type Phenylephrine or Neo-Synephrine is an α1-adrenergic receptor Agonist used primarily as a Decongestant, as an agent to dilate the Aloe vera, also known as the Medicinal Aloe, is a species of Succulent plant that probably originated in northern Africa. Cocaine ( benzoylmethyl ecgonine) is a Crystalline Tropane Alkaloid that is obtained from the leaves of the Coca plant A Diluent (also referred to as a dilutant or thinner) is a diluting agent [3] Cocaine numbs the gums when applied, and since lidocaine causes stronger gingival numbness, customers get the impression of high-quality cocaine when in actuality, the user is receiving a diluted product. The gingiva (sing and plur: gingiva) or gums, consists of the Mucosal tissue that lies over the Alveolar bone. [4]


References

  1. ^ a b Nils Löfgren (1948). Xylocaine: a new synthetic drug.  
  2. ^ Cattterall WA (2002). "Molecular mechanisms of gating and drug block of sodium channels". Novartis Found Symp 241: 206-32. PMID 11771647.  
  3. ^ Naissa Prévide Bernardo, Maria Elisa Pereira Bastos Siqueira, Maria José Nunes de Paiva, Patrícia Penido Maia (2003). "Caffeine and other adulterants in seizures of street cocaine in Brazil". International Journal of Drug Policy 14 (4): 331-334. doi:10.1016/S0955-3959(03)00083-5. A digital object identifier ( DOI) is a permanent identifier given to an Electronic document.  
  4. ^ http://bulk.resource.org/courts.gov/c/F2/599/599.F2d.635.78-5314.html


Cinematic References

Dictionary

lidocaine

-noun

  1. (medicine) A local anesthetic that is also used as a antiarrhythmic drug
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