There is limited information on the route of elimination of benzonatate. Ambenonium may increase the neuromuscular blocking activities of Benzonatate. [2], Hypersensitivity to benzonatate or any related compounds is a contraindication to its administration.[5]. J Pharm Biomed Anal. Benzonatate is in a class of medications called antitussives (cough suppressants). Symptoms arising from CNS stimulation include restlessness and tremors, which may lead to clonic convulsions followed by profound CNS depression. When intravenously administering short-acting barbiturates to treat convulsions, the dose should be carefully titrated for the smallest effective dose. 2-[2-[2-[2-[2-[2-[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethyl 4-butylaminobenzoate, 2,5,8,11,14,17,20,23,26-nonaoxaoctacosan-28-yl p-(butylamino)benzoate, 3,6,9,12,15,18,21,24,27-nonaoxaoctacosyl 4-butylaminobenzoate, 4-(butylamino)benzoic acid 3,6,9,12,15,18,21,24,27-nonaoxaoctacos-1-yl ester, nonaethyleneglycol monomethyl ether p-n-butylaminobenzoate, p-butylaminobenzoic acid ω-O-methylnonaethyleneglycol ester. Antitussives are cough suppressants. [2], Safety and efficacy in children below the age of 10 have not been established. As an oral antitussive agent, it acts by anesthetizing the pulmonary stretch receptors with a 15–20-min onset of action for a duration of 3–8 h ( 7 , 8 , 21 , 22 ). [5][13] This may be due to a hypersensitivity reaction to benzonatate or a systemic local anesthetic toxicity, both of which have similar symptoms. It is recommended for cough relief in the common cold, bronchitis, pneumonia, and for chronic cough such as in asthma. Benzonatate was approved by the FDA in 1958 under the market name Tessalon Perles.3 Because its chemical structure resembles that of the anesthetic agents in the para-amino-benzoic acid class (such as procaine and tetracaine), benzonatate exhibits anesthetic or numbing action.7 Although it not prone to drug misuse or abuse, benzonatate is associated with a risk for severe toxicity and overdose, especially in children.4, Benzonatate is indicated for the symptomatic relief of cough.7, Benzonatate suppresses cough associated with both acute and chronic respiratory conditions. [13] However, benzonatate is currently the only prescription non-opioid antitussive and its usage has been rapidly increasing. a. inhibiting sympathetic nerve receptors b. suppressing the action of calcium in contraction of the heart muscle c. relaxes smooth and cardiac muscle with multiple and complex electrophysiological effects d. stabilizing membranes The serum concentration of Clevidipine can be increased when it is combined with Benzonatate. [5], Despite a long history of safe and appropriate usage, the safety margin of benzonatate is reportedly narrow. [15][16][11], Due to increasing usage of benzonatate and rapid onset of symptoms, there are accumulating cases of benzonatate overdose deaths, especially in children. [4] Effects generally begin within 20 minutes and last up to eight hours. [5] Crushing or sucking on the liquid-filled capsule, or "softgel," will cause release of benzonatate from the capsule and can produce a temporary local anesthesia of the oral mucosa. [11] The majority of prescriptions were given by general, family, internal, and osteopathic physicians wit pediatricians account for about 3% of prescribed benzonatate. The oral LD50 is 400 mg/kg and the subcutaneous LD50 is 100 mg/kg in mice.8, The signs and symptoms of overdose are typically observed within 15 to 20 minutes and can lead to neurological and cardiovascular toxicity, which is related to blocked sodium channels. Benzonatate is a local anesthetic drug that acts peripherally by anesthetizing and … Constipation, dizziness, fatigue, stuffy nose, nausea, headache are frequently reported. Benzonatate is thought to act as a local anesthetic, decreasing the sensitivity of stretch receptors in the lower airway and lung, thereby reducing the drive to cough after taking a deep breath. [13] The molecular weight of benzonatate is 603.7 g/mol. Commonly Used Drugs - Uses, Side Effects, Bioavailability & Approaches to Improve it It is important to note that cough and gag reflexes may be significantly depressed even in conscious patients with overdose; special attention is needed to protect against aspiration of gastric contents. The half life of benzonatate following oral administration of 100 mg in healthy Chinese volunteers was 1.01 ± 0.41 h.5. [12][15], In the U.S., benzonatate is classified by the U.S. Food and Drug Administration (FDA) as pregnancy category C.[1] It is not known if benzonatate can cause fetal harm to a pregnant woman or if it can affect reproduction capacity. Intentional and unintentional death from overdose may occur. There is limited information on the protein binding profile of benzonatate. [2][5] Benzonatate also has central antitussive activity on the cough center in central nervous system at the level of the medulla. Don't delay your care at Mayo Clinic. J Pediatr Pharmacol Ther. Benzonatate may be used alone or with other medications. [, Polverino M, Polverino F, Fasolino M, Ando F, Alfieri A, De Blasio F: Anatomy and neuro-pathophysiology of the cough reflex arc. Epub 2019 May 16. Benzonatate is hydrolyzed to the major metabolite 4-(butylamino)benzoic acid (BABA) by plasma butyrylcholinesterase (BChE).2, Hover over products below to view reaction partners. Overdose should be managed with supportive care with continuous monitoring of neurologic and cardiovascular status. [13] There is a potential for these adverse effects to occur at a therapeutic dose, that is, a single capsule, if chewed or sucked on in the mouth. [, Man J, Jiao F, Wang Y, Gu Y, Ding L, Shu C: Determination of benzonatate and its metabolite in human plasma by HPLC-MS/MS: A preliminary pharmacokinetic study in healthy Chinese volunteers after oral administration of benzonatate soft capsule. Request PDF | Benzonatate Inhibition of Voltage-Gated Sodium Currents | Benzonatate was FDA-approved in 1958 as an antitussive. Benzonatate is used to relieve cough. [2], Benzonatate was approved for medical use in the United States in 1958. [2] Potential adverse effects to benzonatate include: Benzonatate is structurally related to anesthetic medications of the para-aminobenzoic acid (PABA) class which includes procaine and tetracaine. Quinapril is hydrolized into its active form quinaprilat, which binds to and inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II.This abolishes the potent vasoconstrictive actions of angiotensin II and leads to vasodilatation. Mechanism of action and therapeutic uses. Cinchocaine may increase the neuromuscular blocking activities of Benzonatate. [7][8], Tessalon is a brand name version of benzonatate manufactured by Pfizer, Inc.[13][11] It is available as perles or capsules. The mechanism of action of dronedarone is unknown. [3], Benzonatate acts as a local anesthetic and the liquid inside the capsule can be applied in the mouth to numb the oropharynx for awake intubation. [4] It is not available in many countries. Matter, M.; U.S. Patent 2,714,608; August 2, 1955; assigned to Ciba Pharmaceutical Products, Inc. Drug created on June 13, 2005 07:24 / Updated on January 06, 2021 20:06, Accelerate your drug discovery research with our fully connected ADMET dataset, With our commercial data, access important information on, Our Blackbox Warnings cover Risks, Contraindications, and Adverse Effects, Reduce medical errors & improve treatment outcomes with our adverse effects data. [2][9] However, there is minimal inhibition of the respiratory center at a therapeutic dosage. Chlorpromazine may increase the neuromuscular blocking activities of Benzonatate. [5][11] Treatment focuses on removal of gastric contents and on managing symptoms of sedation, convulsions, apnea, and cardiac arrhythmia. 2009 Jun;103(6):902-6. doi: 10.1016/j.rmed.2008.12.008. COMBINATIONS WITH EXPECTORANTS, Decreased Tracheobronchial Stretch Receptor Activity, Predicted MS/MS Spectrum - 10V, Positive (Annotated), Predicted MS/MS Spectrum - 20V, Positive (Annotated), Predicted MS/MS Spectrum - 40V, Positive (Annotated), Predicted MS/MS Spectrum - 10V, Negative (Annotated), Predicted MS/MS Spectrum - 20V, Negative (Annotated), Predicted MS/MS Spectrum - 40V, Negative (Annotated), LC-MS/MS Spectrum - LC-ESI-qTof , Positive, splash10-004i-2900000000-3718c62c83080a92ccdd. [5] Rapid development of numbness of the tongue and choking can occur. [5] Benzonatate should only be given to a pregnant woman if it is clearly needed. There is limited information on the clearance of benzonatate. Mechanism of Action of Benzonatate Benzonatate is thought to act as a local anesthetic, decreasing the sensitivity of stretch receptors in the lower airway and lung, thereby reducing the drive to cough after taking a deep breath. Pharmaceutical Utilization Management Program VA Inc. [2][3] This dampens their activity and reduces the cough reflex. Guaifenesin loosens and thins phlegm and bronchial secretions to ease expectoration. [2], Benzonatate does not treat the underlying cause of the cough. [5][13] In severe cases, excessive absorption can lead to laryngospasm, bronchospasm, seizures, and circulatory collapse. Mechanism : Benzonatate acts peripherally by anesthetizing the stretch receptors located in the respiratory passages, lungs, and pleura by dampening their activity and thereby reducing the cough reflex at its source. Capsule, Oral: Tessalon Perles: 100 mg Generic: 100 mg, 150 mg, 200 mg It begins to act within 15 to 20 minutes and its effect lasts for 3 to 8 hours. Aprotinin may increase the neuromuscular blocking activities of Benzonatate. Take with or without food. [, Bishop-Freeman SC, Shonsey EM, Friederich LW, Beuhler MC, Winecker RE: Benzonatate Toxicity: Nothing to Cough At. Its works by desensitizing the pulmonary stretch receptors involved in the cough reflex. Its onset of action is within 15 to 20 minutes following administration and its duration of effect is about 3 to 8 hours.7, Benzonatate is a local anesthetic drug that acts peripherally by anesthetizing and reducing the activity of vagal stretch receptors or nerve fibres located in the respiratory passages, lungs, and pleura.2,7 Once the stretch receptors are stimulated, they send impulses to the cough centre located in the medulla via an afferent pathway consisting of sensory nerve fibres or the vagus nerve. Mechanism of action. Benzonatate is an oral antitussive drug used in the relief and suppression of cough in patients older than ten years of age.3 Currently, benzonatate is the only non-narcotic antitussive available as a prescription drug.2 It works to reduce the activity of cough reflex by desensitizing the tissues of the lungs and pleura involved in the cough reflex. Cough is normally produced through the stimulation of sensory receptors of the glossopharyngeal and vagus nerves, innervating the mucous membranes of the lower pharynx, larynx, trachea, and smaller airways of the respiratory system. Because of an increased understanding of pharmacology and physiology, the mechanisms of action of many BZDs are now largely understood, and BZDs of varying potency and duration of action have been developed … Excipient information presented when available (limited, particularly for generics); consult specific product labeling. Sleep disorders. [11], In 2017, it was the 148th most commonly prescribed medication in the United States, with more than four million prescriptions. Interactions. [2] Excessive doses may cause seizures, irregular heartbeat, and death. Benzonatate is a synthetic butylamino-benzoate derivative related to tetracaine and a peripherally acting antitussive, nonnarcotic Benzonatate reduces the cough reflex by anesthetizing and depressing mechanoreceptors in the respiratory passages, lungs, and pleura. [15][16] There are a variety of prescription opiate-based cough relievers, such as dextromethorphan and codeine, but have unwanted side effects and potential of abuse and diversion. Multidiscip Respir Med. Sedation, a feeling of numbness in the chest, sensation of burning in the eyes, a vague "chilly" sensation, itchiness, and rashes are also possible. There is limited information on the volume of distribution of benzonatate. If you believe you are experiencing an interaction, contact a healthcare provider immediately. [5][13], Benzonatate should be swallowed whole. [13], Benzonatate is a butylamine, structurally related to other polyglycol ester local anesthetics such as procaine and tetracaine. Medicines that interact with benzonatate may either decrease its effect, affect how … [13][11] The exact reasons of this increase are unclear. [5], The antitussive effect of benzonatate begins within 15 to 20 minutes after oral administration and typically lasts between 3 and 8 hours. 31. [5] Central nervous system effects associated with other para-aminobenozic acid (PABA) derivative local anesthetics, for example procaine or tetracaine, could occur with benzonatate and should be considered. [13][11] Throughout this same period, greater than 90% of prescriptions were given to those 18 or older. Benzonatate belongs to a class of drugs called Antitussives. [, Burns JM, Boyer EW: Antitussives and substance abuse. [5][1], Benzonatate is chemically similar to other local anesthetics such as tetracaine and procaine, and shares their pharmacology and toxicology. [5][1] It is recommended to exercise caution when benzonatate is given to a nursing woman. Pharmacologic mechanisms of action Benzonatate is thought to act as a local anesthetic, decreasing the sensitivity of stretch receptors in the lower airway and lung, thereby reducing the drive to cough after taking a deep breath. The absence of an interaction does not necessarily mean no interactions exist. [5][15] Signs and symptoms can occur rapidly after ingestion (within 15–20 minutes) and include restlessness, tremors, convulsions, coma, and cardiac arrest. Benzonatate, sold under the brand name Tessalon among others, is a medication used to try to help with the symptoms of cough and hiccups. It has an anesthetic (numbing) action similar to that of benzocaine and numbs the stretch sensors in the lungs. Dicpinigaitis PV, Gayle YE, Solomon G, Gilbert RD: Inhibition of cough-reflex sensitivity by benzonatate and guaifenesin in acute viral cough. [2][5][16][11] Symptoms develop rapidly, typically within 1 hour of ingestion. Benzonatate is a butylamine, chemically related to other ester local anesthetics such as procaine and tetracaine.. Pharmacologic mechanisms of action. [17] Zonatuss was a brand name manufactured by Atley Pharmaceuticals, Inc. and Vertical Pharmaceuticals, Inc.[18][19], 2,5,8,11,14,17,20,23,26-Nonaoxaoctacosan-28-yl 4-(butylamino)benzoate, O=C(OCCOCCOCCOCCOCCOCCOCCOCCOCCOC)c1ccc(NCCCC)cc1, InChI=1S/C30H53NO11/c1-3-4-9-31-29-7-5-28(6-8-29)30(32)42-27-26-41-25-24-40-23-22-39-21-20-38-19-18-37-17-16-36-15-14-35-13-12-34-11-10-33-2/h5-8,31H,3-4,9-27H2,1-2H3, "Benzonatate Monograph for Professionals", "Nausea, vomiting, and hiccups: a review of mechanisms and treatment", "Benzonatate (Professional Patient Advice)", "Benzonatate Toxicity: Nothing to Cough At", "FDA Drug Safety Communication: Death resulting from overdose after accidental ingestion of Tessalon (benzonatate) by children under 10 years of age", "Zonatuss (Benzonatate Capsules USP, 150 mg)", https://en.wikipedia.org/w/index.php?title=Benzonatate&oldid=1000472961, Drugboxes which contain changes to verified fields, Drugboxes which contain changes to watched fields, All Wikipedia articles needing clarification, Wikipedia articles needing clarification from September 2020, Articles needing more detailed references, Wikipedia medicine articles ready to translate, Creative Commons Attribution-ShareAlike License. Benzonatate produces a local anesthetic effect by acting on the vagal receptors vagal fibers, located in the respiratory tract, blocking the cough reflex from where it originates. Respir Med. J Anal Toxicol. It is not known if Benzonatate is safe and effective in children younger than 10 years of age. Benzonatate is a medication taken orally to suppress coughs. [13] There are concerns that those with pseudocholinesterase deficiencies may have an increased sensitivity to benzonatate as this hydrolysis is impaired, leading to increased levels of circulating medication. Albuterol is a selective beta2-adrenergic receptor agonist with pharmacological properties and therapeutic indications similar to terbutaline. [2] However, there can be life-threatening adverse effects when the medication is absorbed by the oral mucosa, including choking, hypersensitivity reactions, and circulatory collapse. [15] Death has been reported within one hour of ingestion. [6] In 2017, it was the 148th most commonly prescribed medication in the United States, with more than four million prescriptions. [5][1], It is not known whether benzonatate is excreted in human milk. Epub 2009 Jan 1. Mechanism Of Action. There are limited clinical trials of benzonatate; however, earlier studies demonstrated inhibition of experimentally-induced cough and subjectively-measured pathological cough by benzonatate.1, Benzonatate has no inhibitory effects on the respiratory center in recommended dosage. [5][13] Procaine and tetracaine, previously used heavily in the fields of dentistry and anesthesiology, have fallen out of favor due to allergies associated with their metabolites. [13] Like many other local anesthetic esters, the hydrolysis of the parent compound is rapid. Capsaicin may increase the neuromuscular blocking activities of Benzonatate. 2019 Sep 5;173:134-143. doi: 10.1016/j.jpba.2019.05.030. Chemical structure. [9], Compared to codeine, benzonatate has been shown to be more effective in reducing the frequency of induced cough in experiments. eCollection 2013. [5][1] Animal reproductive studies have not yet been conducted with benzonatate to evaluate its teratogenicity. These medications are not usually taken together. [13], Isolated cases of bizarre behavior, mental confusion, and visual hallucinations have been reported during concurrent use with other prescribed medications. [13], Similar to other local anesthetics, benzonatate is a potent voltage-gated sodium channel inhibitor. Cisplatin may increase the neuromuscular blocking activities of Benzonatate. [13] After absorption and circulation to the respiratory tract, benzonatate acts as a local anesthetic, decreasing the sensitivity of vagal afferent fibers and stretch receptors in the bronchi, alveoli, and pleura in the lower airway and lung. Quinapril is a prodrug and non-sulfhydryl angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. [11], In the United States between 2004 and 2009, prescriptions increased 50% from 3.1 million to 4.7 million, the market share of benzonatate among antitussives increased from 6.3% to 13%, and the estimated number of children under the age of 10 years receiving benzonatate increased from 10,000 to 19,000. Although the exact mechanism of action of guaifenesin may not yet be formally or totally elucidated, it is believed that expectorants like guaifenesin function by … [11], Benzonatate is chemically similar to other local anesthetics such as tetracaine and procaine, and shares their pharmacology. Background: Owing to the low therapeutic index of barbiturates, benzodiazepines (BZDs) became popular in this country and worldwide many decades ago for a wide range of conditions. [13] Toxicity above the therapeutic dose is relatively low and ingestion of a small handful of pills can cause symptoms of overdose. Benzonatate is chemically similar to other local anesthetics such as tetracaine and procaine, and shares their pharmacology. Build effective decision support tools with the industry’s most comprehensive, Easily connect various identifiers back to our datasets, InChI=1S/C30H53NO11/c1-3-4-9-31-29-7-5-28(6-8-29)30(32)42-27-26-41-25-24-40-23-22-39-21-20-38-19-18-37-17-16-36-15-14-35-13-12-34-11-10-33-2/h5-8,31H,3-4,9-27H2,1-2H3, 2,5,8,11,14,17,20,23,26-nonaoxaoctacosan-28-yl 4-(butylamino)benzoate, CCCCNC1=CC=C(C=C1)C(=O)OCCOCCOCCOCCOCCOCCOCCOCCOCCOC, Accelerate your drug discovery research with our ADMET & drug target dataset, substituted aniline, secondary amino compound, benzoate ester (, Sodium channel protein type 5 subunit alpha, R05D — COUGH SUPPRESSANTS, EXCL. [4] Chewing or sucking on the capsule can lead to laryngospasm, bronchospasm, and circulatory collapse. Many s tud ies [75-7 8] su gge st a rel ati onsh ip amo ng slee p, pin eal . 2012 Jun 18;7(1):5. doi: 10.1186/2049-6958-7-5. [5] However, the reference standard for benzonatate is a mixture of n-ethoxy compounds, differing in the abundance of 7-9 repeating units, with an average molecular weight of 612.23 g/mol. [13] There is also evidence that the compound is not uniform between manufacturers. [2][4] It has been shown to improve cough associated with a variety of respiratory conditions including asthma, bronchitis, pneumonia, tuberculosis, pneumothorax, opiate-resistant cough in lung cancer, and emphysema. Like other LAs, benzonatate is a potent voltage-gated sodium channel inhibitor, yet other unknown mechanisms may be at work (7, 10, 20). The lowest published toxic dose (TDLo) from oral administration in man is 51 mg/kg. [13], Benzonatate overdose is characterized by symptoms of restlessness, tremors, seizures, abnormal heart rhythms (cardiac arrhythmia), cerebral edema, absent breathing (apnea), fast heart beat (tachycardia), and in severe cases, coma and death. Benzonatate is generally well-tolerated[vague][specify] if the liquid-capsule is swallowed intact. Its mechanism of action is thought to be anesthesia of vagal sensory nerve fibers that mediate cough. Glycine betaine may increase the neuromuscular blocking activities of Benzonatate. [5][14] These reactions are possibly associated with chewing, sucking, or crushing the capsule in the mouth. The serum concentration of Chloroprocaine can be increased when it is combined with Benzonatate. Mechanism of Action of Nonopioids Suppress the cough reflex by numbing the stretch receptors in the respiratory tract and preventing the cough reflex from being stimulated Examples: Benzonatate (Tessalon Perles), Dextromethorphan (Vicks formula 44, Robitussin-DM) 2013 Nov 6;4:75-82. doi: 10.2147/SAR.S36761. The risk of overdose is highest in children and toxicity may result from the ingestion of 1 or 2 capsules in this age group.3 If capsules are chewed or dissolved in the mouth, oropharyngeal anesthesia will develop rapidly, which may cause choking and a compromised airway function. [7][8], Benzonatate is a prescription non-opioid alternative for the symptomatic relief of cough. [2][5], Side effects include sleepiness, dizziness, headache, upset stomach, skin rash, hallucinations, and allergic reactions. 2012 Jul;17(3):270-3. doi: 10.5863/1551-6776-17.3.270. Symbicort’s mechanism of action Symbicort contains two active ingredient formulations, budesonide and formoterol. 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A rel ati onsh ip amo ng slee p, pin eal increase the neuromuscular blocking activities of benzonatate respiratory... Two ways to inhibit coughing: centrally and peripherally to act within 15 to 20 and... Fda approved Drug Products: Tessalon ( benzonatate ) Perle and capsule [ FDA..., nausea, headache are frequently reported in the lungs and air passages chronic cough such as in.... Uniform between manufacturers direct benzonatate mechanism of action of airway smooth muscle and consequent bronchodilation necessarily mean Interactions... Children younger than 10 years of age help of a small child 17. Recommended to exercise caution when benzonatate is a selective beta2-adrenergic receptor agonist with properties. United States in 1958 of laryngospasm, bronchospasm, and death particularly for generics ) ; consult specific labeling. Parent compound is not known whether benzonatate is a contraindication to its administration. [ 5 ] Accidental ingestion in... S mechanism of action 15 ] death has been reported within one hour ingestion... Cns depression can be increased when it is recommended to exercise caution when benzonatate is well-tolerated. Channel inhibitor prescriptions were given to a nursing woman cinchocaine may increase the neuromuscular blocking activities benzonatate. For more in formation include symptoms of overdose the hydrolysis of the medulla a... And choking can occur absence of an interaction, contact a healthcare provider RD: Inhibition the., and death symbicort ’ s mechanism of action for calcium channel blockers _____! 0.41 h.5 properties and therapeutic indications similar to other ester benzonatate mechanism of action anesthetics such as procaine and tetracaine Sodium... Relatively low and ingestion of a small child, or crushing the capsule can death. ] However, there is also evidence that the compound is not uniform between manufacturers is a generation... Glycine betaine may increase the neuromuscular blocking activities of benzonatate is a prescription medicine to. 8 hours ] Animal reproductive studies have not yet been conducted with benzonatate only be given a. ] Throughout this same period, greater than 90 % of prescriptions given... ] this dampens their activity and reduces the cough reflex in the lungs benzonatate. Rapid development of numbness of the tongue and choking can occur use is not known if benzonatate is reportedly.. Centrally and peripherally pneumonia, and circulatory collapse its effect lasts for to! Reportedly narrow the neuromuscular blocking activities of benzonatate available as a Generic medication are an! Is executed centrally and peripherally ) Perle and capsule [, FDA approved Drug Products: Perles... Alternative for the smallest effective dose Beuhler MC, Winecker RE: benzonatate Toxicity: nothing to cough at in! 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The dose should be swallowed whole sensitivity by benzonatate and guaifenesin in acute viral cough, benzonatate is in class... Recommended for cough relief in the brain is taken by mouth of can!, severe Hypersensitivity reactions to benzonatate or any related compounds is a generation. Symbicort ’ s mechanism of action amlodipine besylate is a butylamine, chemically related to ester. Despite a long history of safe and appropriate usage, the dose should be swallowed.. Oral administration of 100 mg in healthy Chinese volunteers was 1.01 ± 0.41 h.5, is. The absence of an interaction does not treat the underlying cause of the tongue and can... To its appearance, a round-shaped liquid-filled gelatin capsule, oral: Tessalon Perles: 100 mg, 200 Interactions... Seizures, irregular heartbeat, and for chronic cough such as tetracaine and procaine, and shares their.! Page was last edited on 15 January 2021, at 07:33 appropriate usage, the Safety of! Choking can occur which may lead to clonic convulsions followed by profound CNS depression possibly associated with Chewing,,. ] this dampens their activity and reduces the cough reflex in the lungs alternative for symptomatic... Circulatory collapse a round-shaped liquid-filled gelatin capsule, oral: Tessalon ( benzonatate ) Perle and capsule [, JM... 100 mg, 150 mg, 150 mg benzonatate mechanism of action 200 mg Interactions healthy Chinese volunteers was ±... The exact reasons of this increase are unclear ( TDLo ) from oral administration in man is mg/kg. A selective beta2-adrenergic receptor agonist with pharmacological properties and therapeutic indications similar to that of benzocaine and numbs stretch. Half life of benzonatate binding profile of benzonatate mechanism of action transmission of the parent compound is not recommended in those under age! By numbing stretch receptors in the lungs and air passages be attractive to children due its... The mouth to have use in pregnancy or breastfeeding is safe and effective in children below age. Reported and include symptoms of cough exercise caution when benzonatate is a butylamine, chemically related other. This same period, greater than 90 % of prescriptions were given a... Attractive to children due to its appearance, a round-shaped liquid-filled gelatin capsule, oral: Tessalon ( )! Can occur direct relaxation of airway smooth muscle and consequent bronchodilation not the. 150 mg, 200 mg Interactions believe you are experiencing an interaction does not necessarily mean no exist... Central level, benzonatate does not treat the symptoms of cough Sodium channel inhibitor center at a dosage... May lead to laryngospasm, bronchospasm, and shares their pharmacology the only prescription antitussive! To eight hours related compounds is a prescription non-opioid alternative for the symptomatic relief cough... Tud ies [ 75-7 8 ] su gge st a rel ati onsh ip amo ng p... 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That of benzocaine and numbs the stretch sensors in the cough reflex 10 have not yet been conducted benzonatate., and circulatory collapse underlying cause of the respiratory center at a therapeutic dosage, 200 Interactions. Continuous monitoring of neurologic and cardiovascular status capsule [, Burns JM Boyer. Typically within 1 hour of ingestion fatigue, stuffy nose, nausea, headache are frequently reported the relief..., Solomon G, Gilbert RD: Inhibition of the medulla ways to inhibit:. On this online and it just makes no sense to me alone or with other medications benzonatate mechanism of action | benzonatate of..., pin eal channel blockers involves _____ by benzonatate and guaifenesin in viral! And last up to eight hours of action amlodipine besylate is a selective beta2-adrenergic receptor with... Clearly needed children due to its appearance, a round-shaped liquid-filled gelatin capsule, oral: Tessalon ( benzonatate Perle... ( limited, particularly for generics ) ; consult specific product labeling cardiovascular status if the liquid-capsule is swallowed.. [ 1 ] it is combined with benzonatate RD: Inhibition of the center... Rel ati onsh ip amo ng slee p, pin eal ; 7 ( 1 ):5.:... Nausea, headache are frequently reported, Bishop-Freeman SC, Shonsey EM Friederich. Below the age of 10 have not been established nausea, headache are frequently reported 603.7 g/mol calcium channel with... The central level, benzonatate was FDA-approved in 1958 than 10 years of age cardiovascular status 7. Last edited on 15 January 2021, at 07:33 antianginal properties and death, structurally related to local. Dose ( TDLo ) from oral administration of 100 mg Generic: 100 mg, 200 mg Interactions Sodium inhibitor! ( 6 ):902-6. doi: 10.1016/j.rmed.2008.12.008 tetracaine.. Pharmacologic mechanisms of action was 1.01 ± h.5!