Neprosite
Neprosite Uses, Dosage, Side Effects, Food Interaction and all others data.
Acetylcysteine has a mucolytic activity through its free sulfhydryl group. It acts directly on the mucoproteins to open the disulfide bonds and thus lowers the viscosity of the mucous and facilitates its removal by the muco-cillary action and expectoration. Acetylcysteine improves the phagocytic capacity of the alveolar macrophages, thus protecting lungs from a variety of insults. Acetylcysteine is a precursor to glutathione, the most important intra & extra-cellular antioxidant (the safest & most convenient)
Acetylcysteine is indicated for mucolytic therapy and in the management of acetaminophen overdose. It has a short duration of action as it is given every 1-8 hours depending on route of administration, and has a wide therapeutic window. Patients should be counselled regarding diluting oral solutions in cola for taste masking, the risk of hypersensitivity, and the risk of upper gastrointestinal hemorrhage.
Taurine, whose chemical name is 2-aminoethanesulfonic acid, is one of the most abundant amino acids in several organs. It plays important role in essential biological processes. This conditional amino acid can be either be manufactured by the body or obtained in the diet mainly by the consumption of fish and meat. The supplements containing taurine were FDA approved by 1984 and they are hypertonic injections composed by cristalline amino acids.
The diet supplements containing taurine are formulated as a well-tolerated nitrogen source for nutritional support. Administration of diet supplements regulates the level of plasma amino acid concentration, nitrogen balance, weight and serum protein concentration to reach normal values, thus improving the nutritional status.
Trade Name | Neprosite |
Generic | Acetylcysteine + Taurine |
Weight | 150mg |
Type | Tablet |
Therapeutic Class | |
Manufacturer | Manfriday Lifesciences |
Available Country | India |
Last Updated: | September 19, 2023 at 7:00 am |
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Uses
Acetylcysteine is used for an adjunctive treatment for patients with abnormal, viscid or inspissated mucus secretions associated with conditions such as-
Acute and chronic bronchopulmonary disorders (e.g. pneumonia, bronchitis, emphysema, tracheobronchitis, chronic asthmatic bronchitis, tuberculosis, bronchiectasis, primary amyloidosis of the lung) Atelectasis caused by mucus obstruction Pulmonary complications of cystic fibrosis Pulmonary complications of thoracic and cardiovascular surgery Post-traumatic chest conditions.
It is effective in all respiratory airways disease causing formation of a dense secretion that cannot be or can only partially be expectorated such as acute and chronic bronchitis, laryngitis, sinusitis, tracheitis, infuenza & bronchial asthma. Acetylcysteine is also used for the treatment of Paracetamol overdose. Treatment option is optimal if given within 8 hours of Paracetamol ingestion.
Taurine is an ingredient found in mixture products indicated for nutritional support.
The use of diet supplements containing taurine is indicated for the nutritional support of infants and young pediatric patients requiring total parenteral nutrition via central or peripheral routes. The usage of diet supplements containing taurine prevents nitrogen and weight loss or to treat negative nitrogen balance in pediatric patients where the alimentary tract cannot be done through oral, gastrostomy or jejunostomy administration, there is impaired gastrointestinal absorption or protein requirements are substantially increased.
Neprosite is also used to associated treatment for these conditions: Acetaminophen Overdose, Chronic Rhinitis, Corneal Diseases, Corneal ulceration, Crusting Rhinitis, Keratopathy, Rhinitis, Sinusitis, Vasomotor Rhinitis, Acute Rhinitis, Subacute Rhinitis, Airway secretion clearance therapyTotal parenteral nutrition therapy
How Neprosite works
A number of possible mechanisms for the mucolytic activity of acetylcysteine have been proposed. Acetylcysteine's sulfhydryl groups may hydrolize disulfide bonds within mucin, breaking down the oligomers, and making the mucin less viscous. Acetylcysteine has also been shown to reduce mucin secretion in rat models. It is an antioxidant in its own right but is also deacetylated to cysteine, which participates in the synthesis of the antioxidant glutathione. The antioxidant activity may also alter intracellular redox reactions, decreasing phosphorylation of EGFR and MAPK, which decrease transcription of the gene MUC5AC which produces mucin.
In the case of acetaminophen overdoses, a portion of the drug is metabolized by CYP2E1 to form the potentially toxic metabolite N-acetyl-p-benzoquinone imine (NAPQI). The amount of NAPQI produced in an overdose saturates and depletes glutathione stores. The free NAPQI promiscuously binds to proteins in hepatocytes, leading to cellular necrosis. Acetylcysteine can directly conjugate NAPQI or provide cysteine for glutathione production and NAPQI conjugation.
The diet supplements containing taurine function by replacing the missing nutriments in the body. Taurine, as a single agent, presents different functions like substrate for formation of bile salts, cell volume regulation, modulation of intracellular calcium, cytoprotection of central nervous system, etc.
Dosage
Neprosite dosage
Acetylcysteine Tablet:
The dispersible tablet should be dissolved in 1/2 glass of water before use (preferably in the evening). The duration of treatment should be 5 to 10 days in the acute phase. It may be continued in the chronic state for up to 6 months or according to the advice of the physician.
As a mucolytic:
- Adults: 600 mg daily as a single dose.
- In Paracetamol overdose: Initially 140 mg/kg, followed by 70 mg/kg every 4 hours for an additional 17 doses. As an antidote, Acetylcysteine is reported to be very effective when administered within 8 hours of Paracetamol overdose, with the protective effect diminishing after this time. Initiation of treatment after a lapse of 15 hours has previously been thought to be ineffective, but recent studies suggest that beneficial results may still be obtained.
Acetylcysteine Respirator Solution:
The 20% solution may be diluted to a lesser concentration with either Sodium Chloride for injection, Sodium Chloride for inhalation, sterile water for injection, or sterile water for inhalation.
As a mucolytic:
Adult:
- 5-10 ml of 10% or 20% solution by nebulizer every 6-8 hr PRN.
Children:
- 1-11 months: 1-2 ml of 20% or 2-4 ml of 10% solution by nebulizer every 6-8 hr PRN.
- 12 months-11 years: 3-5 ml of 20% or 6-10 ml of 10% solution by nebulizer every 6-8 hr PRN.
- Below 12 years: 5-10 ml of 10/20% solution by nebulizer every 6-8 hr PRN.
Diagnostic Bronchograms: 1-2 ml of 20% or 2-4 ml of 10% solution 2-3 times by nebulization or by instillation intratracheally prior to procedure.
Nebulization tent or croupette: This form of administration requires very large volumes of the solution, occasionally as much as 300 ml during a single treatment period. If a tent or croupette must be used, the recommended dose is the volume of acetylcysteine (using 20%) that will maintain a very heavy mist in the tent or croupette for the desired period. Administration for intermittent or continuous prolonged periods, including overnight, may be desirable.
Direct Instillation: When used by direct instillation, 1-2 ml of a 20% solution may be given as often as every hour. When used for the routine nursing care of patients with tracheostomy, 1-2 ml of a 20% solution may be given every 1-4 hours by instillation into the tracheostomy.
Side Effects
Generally, Acetylcysteine is well tolerated. However, mild effects such as nausea, headache, tinnitus, urticaria, stomatitis, rhinorrhoea, chills, fever, bronchospasm may be observed. Occasional cases of nausea and dyspepsia, rare cases of urticaria may be observed.
Toxicity
Patients experiencing an overdose may present with vomiting, nausea, bronchospasm, periorbital angioedema, and hypotension. Treat patients with symptomatic and supportive measures. Hemodialysis may remove some acetylcysteine from circulation as it is somewhat protein bound.
The administration of taurine has been correlatefd to significant in the hypothalamus and the modification of neuroendocrine functions. Other than that, taurine administration in regular doses is reported by different articles and institutions to be safe.
Precaution
Acetylcysteine should be given in caution in asthma patients.
Interaction
After taking Acetylcysteine orally it increases the bioavailability of Amoxicillin, but shows no effect on Doxycycline and reduces the absorption of Cefalexin. Acetylcysteine seems to increase the effects of Nitroglycerin.
Volume of Distribution
The volume of distribution of acetylcysteine is 0.47 L/kg.
The distribution of taurine was studied under the two-compartment model and each one of the compartments gave a range for the volume of distribution of 299-353 ml/kg in compartment 1 and 4608-8374 ml/kg in compartment 2 in mice. Further studies in healthy indivudals gave a volume of distribution that ranged from 19.8 to 40.7 L.
Elimination Route
An 11 g dose in the form of an effervescent tablet for solution reaches a mean Cmax of 26.5 µg/mL, with a Tmax of 2 hours, and an AUC of 186 µg*h/mL.
Oral administration of taurine was studied and it reported dose-dependent values of AUC, Cmax and tmax wherein a dose of 1-30 mg/kg ranged from 89-3452 mcg min/L, 2-15.7 mcg min/ml and 15 min respectively. Further studies in healthy individuals gave an AUC, Cmax and tmax in the range of 116-284.5 mg h/L, 59-112.6 mg/L and 1-2.5 h.
Half Life
The mean terminal half life of acetylcysteine in adults is 5.6 hours and in pre-term neonates is 11 hours.
Oral administration of taurine in healthy individuals gave a plasma elimination half-life that ranged from 0.7-1.4 h.
Clearance
Acetylcysteine has a mean clearance of 0.11 L/hr/kg.
The clearance rate of orally administered taurine was reported to be dose-dependent wherein a dose of 1 mg/kg it presents a clearance rate of 11.7 ml min/kg, 10 mg/kg generates a clearance rate of 18.7 ml min/kg and a dose of 30 mg/kg reports a clearance rate of 9.4 ml min/kg. Further studies in healthy individuals generate a clearance rate that ranged from 14 to 34.4 L/h.
Elimination Route
An oral dose of radiolabelled acetylcysteine is 13-38% recovered in the urine in the first 24 hours, while 3% is recovered in the feces.
Taurine flows and gets distributed in veins and arteries and reports have observed the presence of a significant released of taurine in portally drained viscera, thus suggesting that the main elimination route of taurine is by the gut. This elimination route may be explained by the enterohepatic cycle of taurine.
Pregnancy & Breastfeeding use
Pregnancy Category B. Caution should be taken in case of pregnancy & lactation while using Acetylcysteine.
Contraindication
Known hypersensitivity to active ingredient. Also contraindicated in patients suffering from phenylketonuria and peptic ulcer.
Acute Overdose
Accidental overdose of Acetylcysteine may cause nausea, vomiting or diarrhea.
Storage Condition
Protect from light & moisture, store below 25° C. Keep all medicines out of the reach of children.
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