Pharmacology of Local Anesthetic Agents

Covino, Benjamín G.; Giddon, Donald B.

doi:10.1177/00220345810600080903

Cited by 66 publications

(56 citation statements)

References 3 publications

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“…On the contrary, procaine binds poorly to proteins and possesses a short half-life. 10 LAs bind also to plasma proteins, albumin (low affinity), and α-1-acid glycoprotein (high affinity), leading to the same effects as tissue proteins. 11 The duration of drug's action is also related to its structure, length, and the groups present.…”

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confidence: 99%

“…10,12 The salt, being a weak base, can exist in solution as an un-ionized free base, which is more lipophilic, or as a positively charged cation; both species are involved in the process of conduction blocking. 10,13 The base crosses the neuronal bilayer more easily, and thus is preferred for optimal penetration. 10 The percentage of drug in the two forms depends on its pK a and the environmental pH.…”

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confidence: 99%

“…10,13 The base crosses the neuronal bilayer more easily, and thus is preferred for optimal penetration. 10 The percentage of drug in the two forms depends on its pK a and the environmental pH. Each drug has a characteristic pK a , with ester type LAs typically having a higher value than the amide type.…”

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confidence: 99%

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From micro- to nanostructured implantable device for local anesthetic delivery

Zorzetto

Brambilla

Marcello

et al. 2016

IJN

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Local anesthetics block the transmission of painful stimuli to the brain by acting on ion channels of nociceptor fibers, and find application in the management of acute and chronic pain. Despite the key role they play in modern medicine, their cardio and neurotoxicity (together with their short half-life) stress the need for developing implantable devices for tailored local drug release, with the aim of counterbalancing their side effects and prolonging their pharmacological activity. This review discusses the evolution of the physical forms of local anesthetic delivery systems during the past decades. Depending on the use of different biocompatible materials (degradable polyesters, thermosensitive hydrogels, and liposomes and hydrogels from natural polymers) and manufacturing processes, these systems can be classified as films or micro- or nanostructured devices. We analyze and summarize the production techniques according to this classification, focusing on their relative advantages and disadvantages. The most relevant trend reported in this work highlights the effort of moving from microstructured to nanostructured systems, with the aim of reaching a scale comparable to the biological environment. Improved intracellular penetration compared to microstructured systems, indeed, provides specific drug absorption into the targeted tissue and can lead to an enhancement of its bioavailability and retention time. Nanostructured systems are realized by the modification of existing manufacturing processes (interfacial deposition and nanoprecipitation for degradable polyester particles and high- or low-temperature homogenization for liposomes) or development of novel strategies (electrospun matrices and nanogels). The high surface-to-volume ratio that characterizes nanostructured devices often leads to a burst drug release. This drawback needs to be addressed to fully exploit the advantage of the interaction between the target tissues and the drug: possible strategies could involve specific binding between the drug and the material chosen for the device, and a multiscale approach to reach a tailored, prolonged drug release

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confidence: 99%

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From micro- to nanostructured implantable device for local anesthetic delivery

Zorzetto

Brambilla

Marcello

et al. 2016

IJN

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“…19 Hydrophobicity appears to be a primary determinant of intrinsic anesthetic potency because the anesthetic molecules must penetrate the nerve membrane and must bind at a partially hydrophobic site on the sodium channel. [20][21][22][23] Clinically this may not be true as in all circumstances as vasodilatation and tissue redistribution properties also affect the potency. 24 Factors influencing local anesthetic action Dosage; Onset of action of a local anesthetic quickens as the concentration or dose of the drug is increased.…”

Section: Fig 5: Sedation Score Distribution In Study Groupmentioning

confidence: 99%

Efficacy of Adding Fentanyl to Lignocaine – Adrenaline Combination in Supraclavicular Brachial Plexus Block for Upper Limb Orthopedic Surgeries a Multi - Center Study

Varkey¹,

Alexander²,

C³

2015

jemds

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BACKGROUND:Brachial plexus block is a suitable alternative to general anesthesia for surgeries of upper limb and it can be performed even in patients who are not adequately fit for general anesthesia. The significance of brachial plexus block has increased in recent years due to renewed interest in day care surgery. Lignocaine hydrochloride has been used extensively for brachial plexus block and it has the disadvantage of having short duration of action. Opioids when added to anesthetic mixtures may improve and prolong the action of local anesthetics during peripheral nerve blocks. Such postoperative pain control can reduce both narcotic requirements and narcotic induced side effects. Studies have shown the efficacy of opioids as analgesic adjuvants in prolonging the duration of brachial plexus block. With this background in mind, this study was conducted to compare the onset and duration of sensory and motor block produced by a mixture of lignocaine and adrenaline with that produced by a mixture of fentanyl, lignocaine and adrenaline. Aims: To assess the effectiveness of addition of fentanyl to a mixture of lignocaine and adrenaline in prolonging the duration of analgesia and motor block for upper limb orthopedic surgeries. MATERIALS AND METHODS:This multi-center randomized control study was conducted in two tertiary care centers in 80 patients underwent elective upper limb orthopedic surgeries and they were allocated into two groups of 40 each group L and group F. the classical approach of supraclavicular brachial plexus block. Drug used were 30ml of lignocaine 1.5%+adrenaline 5mcg/ml +0.5ml normal saline in group L and 30ml of lignocaine 1.5% + adrenaline 5mcg/ml + fentanyl 50mcg in group F. Adequacy of block was assessed by the pin prick test and temperature test. Motor power was assessed by the modified Lowett scale. Sedation was monitored using the modified Ramsay scale. An assessment was made for onset of analgesia, onset of motor block, duration of analgesia, duration of motor block and occurrence of any side effects during the first 24 hours of the postoperative period. Subjective assessment of post-operative analgesia was done by direct questioning of the patient and by a five point pain scores. Data's were analyzed using computer software, Statistical Package for Social Science (SPSS) 16th version. OBSERVATION AND RESULTS: The mean onset of sensory block in the lignocaine group was 6.6±1.52 and in the lignocaine-fentanyl group 10.22±2.58. The mean onset of motor block was 8±1.97 in the lignocaine group and 11.39±3.57 in lignocaine-fentanyl group. The mean duration of sensory block was 105.73±9.45 in lignocaine group and 170.28±12.28 in lignocaine-fentanyl group. The mean duration of motor block motor block was 95.93±10.65 in lignocaine group and 178.33±12.37 in the lignocaine-fentanyl group. CONCLUSION: Addition of fentanyl to lignocaine-adrenaline in brachial plexus blocks will significantly delay the onset of sensory and motor block and significantly prolongs the duration of sensory and mo...

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“…As blood and brain levels of local anesthetic concentration increase, generalized tonic-clonic reactions occur. 67 When plasma concentrations of local anesthetic in the CNS increase further, both inhibitory and excitatory pathways (being more resistant to the effects of local anesthetic toxicity) are inhibited, which leads to CNS depression, reduced levels of consciousness, and eventually coma.…”

Section: Local Anesthetic In the Surgical Woundmentioning

confidence: 99%