Ropivacaine
Encyclopedia
Ropivacaine (icon) is a local anaesthetic drug belonging to the amino amide
group. The name ropivacaine refers to both the racemate and the marketed S-enantiomer
. Ropivacaine hydrochloride is commonly marketed by AstraZeneca
under the trade name
Naropin.
was noted to be associated with cardiac arrest
, particularly in pregnant women. Ropivacaine was found to have less cardiotoxicity than bupivacaine in animal models.
, epidural
and intrathecal
anaesthesia in adults and children over 12 years. It is also indicated for peripheral nerve block and caudal epidural in children 1–12 years for surgical pain. It is also sometimes used for infiltration anaesthesia for surgical pain in children.
Ropivacaine is often co-administered with fentanyl for epidural analgesia, for example in pregnant women during labour
.
s (ADRs) are rare when it is administered correctly. Most ADRs relate to administration technique (resulting in systemic exposure) or pharmacological effects of anesthesia, however allergic
reactions can rarely occur.
Systemic exposure to excessive quantities of ropivacaine 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. CNS effects may include CNS excitation (nervousness, tingling around the mouth, tinnitus
, tremor, dizziness, blurred vision, seizure
s) followed by depression (drowsiness, loss of consciousness, respiratory depression and apnea
). Cardiovascular effects include hypotension
, bradycardia
, arrhythmias, and/or cardiac arrest
– some of which may be due to hypoxemia
secondary to respiratory depression.
, there is evidence that Intralipid
, a commonly available intravenous lipid emulsion, can be effective in treating severe cardiotoxicity secondary to local anaesthetic overdose in animal experiments and in humans.
Amide
In chemistry, an amide is an organic compound that contains the functional group consisting of a carbonyl group linked to a nitrogen atom . The term refers both to a class of compounds and a functional group within those compounds. The term amide also refers to deprotonated form of ammonia or an...
group. The name ropivacaine refers to both the racemate and the marketed S-enantiomer
Enantiomer
In chemistry, an enantiomer is one of two stereoisomers that are mirror images of each other that are non-superposable , much as one's left and right hands are the same except for opposite orientation. It can be clearly understood if you try to place your hands one over the other without...
. Ropivacaine hydrochloride is commonly marketed by AstraZeneca
AstraZeneca
AstraZeneca plc is a global pharmaceutical and biologics company headquartered in London, United Kingdom. It is the world's seventh-largest pharmaceutical company measured by revenues and has operations in over 100 countries...
under the trade name
Trade name
A trade name, also known as a trading name or a business name, is the name which a business trades under for commercial purposes, although its registered, legal name, used for contracts and other formal situations, may be another....
Naropin.
History
Ropivacaine was developed after bupivacaineBupivacaine
Bupivacaine is a local anaesthetic drug belonging to the amino amide group. AstraZeneca commonly markets it under various trade names, including Marcain, Marcaine, Sensorcaine and Vivacaine.-Indications:...
was noted to be associated with cardiac arrest
Cardiac arrest
Cardiac arrest, is the cessation of normal circulation of the blood due to failure of the heart to contract effectively...
, particularly in pregnant women. Ropivacaine was found to have less cardiotoxicity than bupivacaine in animal models.
Indications
Ropivacaine is indicated for local anaesthesia including infiltration, nerve blockNerve block
Regional nerve blockade, or more commonly nerve block, is a general term used to refer to the injection of local anesthetic onto or near nerves for temporary control of pain. It can also be used as a diagnostic tool to identify specific nerves as pain generators...
, epidural
Epidural
The term epidural is often short for epidural analgesia, a form of regional analgesia involving injection of drugs through a catheter placed into the epidural space...
and intrathecal
Intrathecal
Intrathecal is an adjective that refers to something introduced into or occurring in the space under the arachnoid membrane of the brain or spinal cord...
anaesthesia in adults and children over 12 years. It is also indicated for peripheral nerve block and caudal epidural in children 1–12 years for surgical pain. It is also sometimes used for infiltration anaesthesia for surgical pain in children.
Ropivacaine is often co-administered with fentanyl for epidural analgesia, for example in pregnant women during labour
Childbirth
Childbirth is the culmination of a human pregnancy or gestation period with the birth of one or more newborn infants from a woman's uterus...
.
Contraindications
Ropivacaine is contraindicated for IV regional anaesthesia (IVRA). However, new data suggested that both Ropivacaine (1.2-1.8mg/kg in 40ml) and levobupivacaine (40ml of 0.125% solution) can be used, because they have less cardiovascular and central nervous system toxicity than racemic bupivacaine (Basic of Anesthesia, Robert Stoelting, page 289).Adverse effects
Adverse drug reactionAdverse drug reaction
An adverse drug reaction is an expression that describes harm associated with the use of given medications at a normal dosage. ADRs may occur following a single dose or prolonged administration of a drug or result from the combination of two or more drugs...
s (ADRs) are rare when it is administered correctly. Most ADRs relate to administration technique (resulting in systemic exposure) or pharmacological effects of anesthesia, however allergic
Allergy
An Allergy is a hypersensitivity disorder of the immune system. Allergic reactions occur when a person's immune system reacts to normally harmless substances in the environment. A substance that causes a reaction is called an allergen. These reactions are acquired, predictable, and rapid...
reactions can rarely occur.
Systemic exposure to excessive quantities of ropivacaine mainly result in central nervous system
Central nervous system
The central nervous system is the part of the nervous system that integrates the information that it receives from, and coordinates the activity of, all parts of the bodies of bilaterian animals—that is, all multicellular animals except sponges and radially symmetric animals such as jellyfish...
(CNS) and cardiovascular effects – CNS effects usually occur at lower blood plasma
Blood plasma
Blood plasma is the straw-colored liquid component of blood in which the blood cells in whole blood are normally suspended. It makes up about 55% of the total blood volume. It is the intravascular fluid part of extracellular fluid...
concentrations and additional cardiovascular effects present at higher concentrations, though cardiovascular collapse may also occur with low concentrations. CNS effects may include CNS excitation (nervousness, tingling around the mouth, tinnitus
Tinnitus
Tinnitus |ringing]]") is the perception of sound within the human ear in the absence of corresponding external sound.Tinnitus is not a disease, but a symptom that can result from a wide range of underlying causes: abnormally loud sounds in the ear canal for even the briefest period , ear...
, tremor, dizziness, blurred vision, seizure
Seizure
An epileptic seizure, occasionally referred to as a fit, is defined as a transient symptom of "abnormal excessive or synchronous neuronal activity in the brain". The outward effect can be as dramatic as a wild thrashing movement or as mild as a brief loss of awareness...
s) followed by depression (drowsiness, loss of consciousness, respiratory depression and apnea
Apnea
Apnea, apnoea, or apnœa is a term for suspension of external breathing. During apnea there is no movement of the muscles of respiration and the volume of the lungs initially remains unchanged...
). Cardiovascular effects include hypotension
Hypotension
In physiology and medicine, hypotension is abnormally low blood pressure, especially in the arteries of the systemic circulation. It is best understood as a physiologic state, rather than a disease. It is often associated with shock, though not necessarily indicative of it. Hypotension is the...
, bradycardia
Bradycardia
Bradycardia , in the context of adult medicine, is the resting heart rate of under 60 beats per minute, though it is seldom symptomatic until the rate drops below 50 beat/min. It may cause cardiac arrest in some patients, because those with bradycardia may not be pumping enough oxygen to their heart...
, arrhythmias, and/or cardiac arrest
Cardiac arrest
Cardiac arrest, is the cessation of normal circulation of the blood due to failure of the heart to contract effectively...
– some of which may be due to hypoxemia
Hypoxia (medical)
Hypoxia, or hypoxiation, is a pathological condition in which the body as a whole or a region of the body is deprived of adequate oxygen supply. Variations in arterial oxygen concentrations can be part of the normal physiology, for example, during strenuous physical exercise...
secondary to respiratory depression.
Treatment of overdose: "Lipid rescue"
As for bupivacaineBupivacaine
Bupivacaine is a local anaesthetic drug belonging to the amino amide group. AstraZeneca commonly markets it under various trade names, including Marcain, Marcaine, Sensorcaine and Vivacaine.-Indications:...
, there is evidence that Intralipid
Intralipid
Intralipid is a brand name for the first safe fat emulsion for human use, approved in 1962 in Europe and invented by Professor Arvid Wretlind, Sweden. The FDA initially would not approve the product due to prior experience with another fat emulsion. It was approved in the United States in 1972...
, a commonly available intravenous lipid emulsion, can be effective in treating severe cardiotoxicity secondary to local anaesthetic overdose in animal experiments and in humans.