Generation of the Action Potential
Nassir H. Sabah in Neuromuscular Fundamentals, 2020
The independence of the Na+ and K+ voltage-gated channels is strongly supported by the fact that different drugs can selectively block one channel and not the other. Thus, the voltage-gated Na+ channel of neurons is selectively blocked by tetrodotoxin (TTX), a potent toxin produced by symbiotic bacteria and found in many animal species, particularly aquatic animals such as the puffer fish. Local anesthetics, such as procaine, are synthetic drugs that, by blocking the voltage-gated Na+ channels of axons carrying pain signals, prevent pain-induced APs in the periphery from reaching the central nervous system and hence the brain centers responsible for the sensation of pain. The voltage-gated K+ channel in axons is selectively blocked by the synthetic drug tetraethylammonium (TEA).
Benzylpenicillin (Penicillin G)
M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson in Kucers’ The Use of Antibiotics, 2017
Occasionally, severe reactions, and even death, occurring during or shortly after an i.m. injection of procaine Pen G may result from accidental i.v. injection. These reactions are partly caused by microembolization of procaine Pen G particles to the lungs and brain, which produces hyperventilation, dilation of pupils, convulsions, and coma. Toxicity due to the procaine component of the drug is contributory. Early manifestations include marked anxiety, fever, hypertension, tachycardia, vomiting, and audiovisual hallucinations. In severe cases, there may be convulsions, abrupt hypotension, and cardiorespiratory arrest, which may simulate anaphylaxis. Galpin et al. (1974) recorded three patients to whom aqueous procaine Pen G was administered inadvertently by i.v. infusion. Within 15 minutes, one patient developed a generalized seizure and cardiorespiratory arrest with slow idioventricular rhythm, but recovered with resuscitation. The other two patients had acute anxiety, tachypnea, dizziness, and tinnitus.
Procaine
Anton C. de Groot in Monographs in Contact Allergy, 2021
Procaine is a local anesthetic of the ester type that has a slow onset and a short duration of action. It is mainly used for production of local or regional anesthesia, particularly for oral surgery. Procaine (like cocaine) has the advantage of constricting blood vessels which reduces bleeding, unlike other local anesthetics such as lidocaine. In pharmaceutical products, both procaine and procaine hydrochloride (CAS number 51-05-8, EC number 200-077-2, molecular formula C13H21CIN2O2) may be employed (1).
Pharmacological Treatments for Localized Provoked Vulvodynia: A Scoping Review
Published in International Journal of Sexual Health, 2023
Krisztina Bajzak, Alex Rains, Lisa Bishop, Michelle Swab, Michelle E. Miller, Gabrielle S. Logan, Victoria Jackman, Liam Jackman, Diana L. Gustafson
Subcutaneous procaine (a local anesthetic) and GIB with local anesthetic and steroid yielded promising results in case reports but follow-up studies with comparator groups have yet to be conducted. Enoxaparin, which is postulated to prevent neural proliferation and strengthen vestibular stroma, led to improved scores on the cotton swab test in an RCT, but other outcomes were not significantly different from placebo (Farajun et al., 2012.). Neither procaine nor enoxaparin were studied as independent interventions prior to 2010 (Andrews, 2011). The continued lack of evidence for injectable medications at present and the discomfort patients experience during administration may render these options less desirable. Despite side-effects and discomfort associated with administration of certain injectables, participants were surprisingly tolerant, with high rates of adherence and low dropout rates.
Can local infiltration of lidocaine reduce the postoperative atrial fibrillation rate in patients undergoing lobectomy for lung cancer?
Published in Acta Chirurgica Belgica, 2020
Certain local anesthetics such as procaine and lidocaine are used for neural therapy. Neural therapy involves the injection of local anesthetics into the autonomic nerve ganglia, peripheral nerves, scars, glands, and trigger points to treat chronic pain. Neural therapy is based on the theory that trauma, infection, or surgery can injure the autonomic nervous system and disturb the electrochemical or electromagnetic functions of tissues. Nerve cell injury (secondary to surgical or non-surgical trauma) increases neuronal excitability with greater firing of impulses. Neurogenic inflammation begins around sensitive veins and irritates the group C pain fibers. The irritated group C pain fibers cause ectopic impulses in both directions (forward and reverse). Local anesthetics raise the resting membrane potential; thus, the nerve is less likely to fire an impulse even with more stimuli. Lidocaine is effective for 3–7 days when used for neural therapy [21–25]. Zhang et al. reported that lidocaine administration in animal models decreased sympathetic nerve sprouting in the early stages of sympathetic sensory neuronal injury [26]. Xie et al. reported that infiltration of local anesthetics reduced or blocked sympathetic nerve sprouting [27]. This mechanism may explain the role of lidocaine infiltration in reducing the POAF rate after thoracotomy for lung cancer.
Emerging role of nanomedicine in the treatment of neuropathic pain
Published in Journal of Drug Targeting, 2020
Pankaj Bidve, Namrata Prajapati, Kiran Kalia, Rakesh Tekade, Vinod Tiwari
Local anaesthetics in the treatment of NeP are one of the conflicting issue [50–52]. S. Shankarappa and D. Kohane also suggested that prolong the release of local anaesthetics may hold a promising alternative in the treatment of NeP conditions [53]. Recently, much attention is focussed on locally acting agents which can reduce pain intensity by acting locally and thus avoid the systemic side effects like constipation, urinary retention, itching, sedation, addiction, tolerance and death due to overdose. Local anaesthetics like procaine, lidocaine and bupivacaine have started gaining attention in the treatment of chronic pain conditions. However, their use is limited because of their relatively short duration of action thus unable to provide the desired effects by prolonging nerve blockage, thus interrupting the transmission of pain signals towards CNS [54].
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