Consists of Codeine, Paracetamol
Actions of Codeine (Codoliprane enfant) in details
Codeine (Codoliprane enfant) Sulfate is an opioid analgesic, related to morphine, but with less potent analgesic properties. Codeine (Codoliprane enfant) is selective for the mu receptor, but with a much weaker affinity than morphine. The analgesic properties of Codeine (Codoliprane enfant) have been speculated to come from its conversion to morphine, although the exact mechanism of analgesic action remains unknown.
Effects of the Central Nervous System (CNS)
The principal therapeutic action of Codeine (Codoliprane enfant) Sulfate is analgesia. Although the precise mechanism of the analgesic action is unknown, specific CNS opiate receptors and endogenous compounds with morphine-like activity have been identified throughout the brain and spinal cord and are likely to play a role in the expression and perception of analgesic effects. Some other CNS effects of Codeine (Codoliprane enfant) include anxiolysis, euphoria, and feelings of relaxation. Codeine (Codoliprane enfant) Sulfate causes respiratory depression, in part by a direct effect on the brainstem respiratory centers. Codeine (Codoliprane enfant) Sulfate and other related opioids depress the cough reflex by direct effect on the cough center in the medulla. Codeine (Codoliprane enfant) Sulfate may also cause miosis.
Effects on the Gastrointestinal Tract and on Other Smooth Muscle
Gastric, biliary and pancreatic secretions may be decreased by Codeine (Codoliprane enfant). Codeine (Codoliprane enfant) also causes a reduction in motility and is associated with an increase in tone in the antrum of the stomach and duodenum. Digestion of food in the small intestine is delayed and propulsive contractions are decreased. Propulsive peristaltic waves in the colon are decreased, while tone is increased to the point of spasm. The end result may be constipation. Codeine (Codoliprane enfant) can cause a marked increase in biliary tract pressure as a result of the spasm of the sphincter of Oddi. Codeine (Codoliprane enfant) may also cause spasms of the sphincter of the urinary bladder.
Effects on the Cardiovascular System
Codeine (Codoliprane enfant) produces peripheral vasodilation which may result in orthostatic hypotension and fainting. Release of histamine can occur, which may play a role in opioid-induced hypotension. Manifestations of histamine release and/or peripheral vasodilation may include pruritus, flushing, red eyes, and sweating.
Endocrine System
Opioid agonists such as Codeine (Codoliprane enfant) Sulfate have been shown to have a variety of effects on the secretion of hormones. Opioids inhibit the secretion of ACTH, cortisol, and luteinizing hormone (LH) in humans. They also stimulate prolactin, growth hormone (GH) secretion, and pancreatic secretion of insulin and glucagons in humans and other species, rats and dogs. Thyroid stimulating hormone (TSH) has been shown to be both inhibited and stimulated by opioids.
Immune System
Codeine (Codoliprane enfant) has been shown to have a variety of effects on components of the immune system in in vitro and animal models. The clinical significance of these findings is unknown.
How should I take Codeine (Codoliprane enfant)?
Follow all directions on your prescription label. Codeine (Codoliprane enfant) can slow or stop your breathing. Never use Codeine (Codoliprane enfant) in larger amounts, or for longer than prescribed. Tell your doctor if the medicine seems to stop working as well in relieving your pain.
Codeine (Codoliprane enfant) may be habit-forming, even at regular doses. Never share this medicine with another person, especially someone with a history of drug abuse or addiction. MISUSE OF NARCOTIC MEDICINE CAN CAUSE ADDICTION, OVERDOSE, OR DEATH, especially in a child or other person using the medicine without a prescription. Selling or giving away Codeine (Codoliprane enfant) is against the law.
Take Codeine (Codoliprane enfant) with food or milk if it upsets your stomach.
Measure liquid medicine with a special dose-measuring spoon or medicine cup. If you do not have a dose-measuring device, ask your pharmacist for one.
Drink 6 to 8 full glasses of water daily to help prevent constipation while you are taking Codeine (Codoliprane enfant). Do not use a stool softener (laxative) without first asking your doctor.
Do not stop using Codeine (Codoliprane enfant) suddenly after long-term use, or you could have unpleasant withdrawal symptoms. Ask your doctor how to avoid withdrawal symptoms when you stop using Codeine (Codoliprane enfant).
Store at room temperature away from moisture and heat.
Keep track of the amount of medicine used from each new bottle. Codeine (Codoliprane enfant) is a drug of abuse and you should be aware if anyone is using your medicine improperly or without a prescription.
After you have stopped using this medication, flush any unused pills down the toilet. Disposal of medicines by flushing is recommended to reduce the danger of accidental overdose causing death. This advice applies to a very small number of medicines only. The FDA, working with the manufacturer, has determined this method to be the most appropriate route of disposal and presents the least risk to human safety.
Codeine (Codoliprane enfant) administration
Oral:
Oral solution [Canadian product]: Administer with an accurate measuring device (calibrated oral syringe or measuring cup); do not use a household teaspoon or tablespoon to measure dose (overdosage may occur).
Controlled-release tablets: Codeine (Codoliprane enfant) Contin [Canadian product]: Tablets should be swallowed whole; do not chew, dissolve, or crush. All strengths may be halved, except the 50 mg tablets; half tablets should also be swallowed intact.
Bariatric surgery: Some institutions may have specific protocols that conflict with these recommendations; refer to institutional protocols as appropriate. Switch to IR formulation (tablet or oral suspension).
Injection [Canadian product]: May be administered by IM or SubQ injection.
Codeine (Codoliprane enfant) pharmacology
Mechanism of Action
Codeine (Codoliprane enfant) is an opioid agonist, related to morphine, but with less potent analgesic properties. Codeine (Codoliprane enfant) is selective for the mu receptor, but with a much weaker affinity than morphine. The analgesic properties of Codeine (Codoliprane enfant) have been speculated to come from its conversion to morphine, although the exact mechanism of analgesic action remains unknown.
Effects of the Central Nervous System (CNS): The principal therapeutic action of Codeine (Codoliprane enfant) is analgesia. Although the precise mechanism of the analgesic action is unknown, specific CNS opiate receptors and endogenous compounds with morphine-like activity have been identified throughout the brain and spinal cord and are likely to play a role in the expression and perception of analgesic effects. Other CNS effects of Codeine (Codoliprane enfant) include anxiolysis, euphoria, and feelings of relaxation. Codeine (Codoliprane enfant) causes respiratory depression, in part by a direct effect on the brainstem respiratory centers. Codeine (Codoliprane enfant) and other related opioids depress the cough reflex by direct effect on the cough center in the medulla. Codeine (Codoliprane enfant) may also cause miosis.
Effects on the Gastrointestinal Tract and on Other Smooth Muscle: Gastric, biliary and pancreatic secretions may be decreased by Codeine (Codoliprane enfant). Codeine (Codoliprane enfant) also causes a reduction in motility and is associated with an increase in tone in the antrum of the stomach and duodenum. Digestion of food in the small intestine is delayed and propulsive contractions are decreased. Propulsive peristaltic waves in the colon are decreased, while tone is increased to the point of spasm. The end result may be constipation. Codeine (Codoliprane enfant) can cause a marked increase in biliary tract pressure as a result of the spasm of the sphincter of Oddi. Codeine (Codoliprane enfant) may also cause spasms of the sphincter of the urinary bladder.
Effects on the Cardiovascular System: In therapeutic doses, Codeine (Codoliprane enfant) does not usually exert major effects on the cardiovascular system. Codeine (Codoliprane enfant) produces peripheral vasodilation which may result in orthostatic hypotension and fainting. Release of histamine can occur, which may play a role in opioid-induced hypotension. Manifestations of histamine release and/or peripheral vasodilation may include pruritus, flushing, red eyes, and sweating.
Endocrine System: Opioid agonists have been shown to have a variety of effects on the secretion of hormones. Opioids inhibit the secretion of ACTH, cortisol, and luteinizing hormone (LH) in humans. They also stimulate prolactin, growth hormone (GH) secretion, and pancreatic secretion of insulin and glucagons in humans and other species, rats and dogs. Thyroid stimulating hormone (TSH) has been shown to be both inhibited and stimulated by opioids.
Immune System: Opioids have been shown to have a variety of effects on components of the immune system in in vitro and animal models. The clinical significance of these findings is unknown.
Pharmacodynamics
Codeine (Codoliprane enfant) plasma concentrations do not correlate with Codeine (Codoliprane enfant) brain concentrations or relief of pain.
The minimum effective concentration varies widely and is influenced by a variety of factors, including the extent of previous opioid use, age and general medical condition. Effective doses in tolerant patients may be significantly higher than in opioid-naïve patients.
Pharmacokinetics
Absorption: Codeine (Codoliprane enfant), when administered as Codeine (Codoliprane enfant) sulfate, is absorbed from the gastrointestinal tract with maximum plasma concentration occurring 60 minutes post administration.
Food Effects: When 60 mg Codeine (Codoliprane enfant) sulfate was administered 30 minutes after ingesting a high fat/high calorie meal, there was no significant change in the rate and extent of absorption of Codeine (Codoliprane enfant).
Steady-state: Administration of 15 mg Codeine (Codoliprane enfant) sulfate every four hours for 5 days resulted in steady-state concentrations of Codeine (Codoliprane enfant), morphine, morphine-3-glucuronide (M3G) and morphine-6-glucuronide (M6G) within 48 hours.
Distribution: Codeine (Codoliprane enfant) has been reported to have an apparent volume of distribution of approximately 3-6 L/kg, indicating extensive distribution of the drug into tissues. Codeine (Codoliprane enfant) has low plasma protein binding with about 7-25% of Codeine (Codoliprane enfant) bound to plasma proteins.
Metabolism: About 70-80% of the administered dose of Codeine (Codoliprane enfant) is metabolized by conjugation with glucuronic acid to Codeine (Codoliprane enfant)-6-glucuronide (C6G, about 60%) and via O-demethylation to morphine (about 5-10%) and N-demethylation to norcodeine (about 10%) respectively. UDP-glucuronosyltransferase (UGT) 2B7 and 2B4 are the major enzymes mediating glucurodination of Codeine (Codoliprane enfant) to C6G. Cytochrome P450 2D6 is the major enzyme responsible for conversion of Codeine (Codoliprane enfant) to morphine (about 5-10%) and P450 3A4 is the major enzyme mediating conversion of Codeine (Codoliprane enfant) to norcodeine. Morphine and norcodeine are further metabolized by conjugation with glucuronic acid. The glucuronide metabolites of morphine are morphine-3-glucuronide (M3G) and morphine-6-glucuronide (M6G). Morphine and M6G are known to have analgesic activity in humans. The analgesic activity of C6G in humans is unknown. Norcodeine and M3G are generally not considered to possess analgesic properties.
Elimination: Approximately 90% of the total dose of Codeine (Codoliprane enfant) is excreted through the kidneys, of which approximately 10% is unchanged Codeine (Codoliprane enfant). Plasma half-lives of Codeine (Codoliprane enfant) and its metabolites have been reported to be approximately 3 hours.
Actions of Paracetamol (Codoliprane enfant) in details
Pharmacology: Paracetamol (Codoliprane enfant) exhibits analgesic and antipyretic activity by inhibiting prostaglandin synthesis. It produces analgesia by elevating the pain threshold and antipyresis through action on the hypothalamic heat-regulating center.
In therapeutic doses, Paracetamol (Codoliprane enfant)'s analgesic and antipyretic action is comparable to that of aspirin. Paracetamol (Codoliprane enfant) does not adversely affect platelet function and hemostasis.
Pharmacokinetics: Paracetamol (Codoliprane enfant) is rapidly and completely absorbed after oral administration. Peak plasma concentrations occur between 15 min to 2 hrs after ingestion. The absolute oral bioavailability of Paracetamol (Codoliprane enfant) is about 80% and is independent of dose in the range of 5-20 mg/kg.
Paracetamol (Codoliprane enfant) is not bound to plasma proteins to any extent. The concentrations of Paracetamol (Codoliprane enfant) in saliva are similar to those in plasma. Concentrations in whole blood are up to 20% higher and in breast milk about 20% lower than the plasma concentration. Paracetamol (Codoliprane enfant) crosses the placenta.
Paracetamol (Codoliprane enfant) is extensively metabolized in the liver and the total body clearance is about 5 mL/kg/min. The clearance of Paracetamol (Codoliprane enfant) is reduced and the half-life increased following a hepatotoxic overdose. Prolongation of half-life beyond 4 hrs usually indicates impending liver damage.
Two to five percent of a therapeutic dose of Paracetamol (Codoliprane enfant) is excreted unchanged in the urine. Its renal clearance is about 10 mL/min and is weakly dependent on urine flow rate but not on pH.
Paracetamol (Codoliprane enfant) administration
May be taken with or without food.
Paracetamol (Codoliprane enfant) pharmacology
The analgesic, antipyretic, and anti-inflammatory effects of aspirin are due to actions by both the acetyl and the salicylate portions of the intact molecule as well as by the active salicylate metabolite. Paracetamol (Codoliprane enfant) directly and irreversibly inhibits the activity of both types of cyclo-oxygenase (COX-1 and COX-2) to decrease the formation of precursors of prostaglandins and thromboxanes from arachidonic acid. This makes aspirin different from other NSAIDS (such as diclofenac and ibuprofen) which are reversible inhibitors. Salicylate may competitively inhibit prostaglandin formation. Paracetamol (Codoliprane enfant)'s antirheumatic (nonsteroidal anti-inflammatory) actions are a result of its analgesic and anti-inflammatory mechanisms; the therapeutic effects are not due to pituitary-adrenal stimulation. The platelet aggregation–inhibiting effect of aspirin specifically involves the compound's ability to act as an acetyl donor to the platelet membrane; the nonacetylated salicylates have no clinically significant effect on platelet aggregation. Paracetamol (Codoliprane enfant) affects platelet function by inhibiting the enzyme prostaglandin cyclooxygenase in platelets, thereby preventing the formation of the aggregating agent thromboxane A2. This action is irreversible; the effects persist for the life of the platelets exposed. Paracetamol (Codoliprane enfant) may also inhibit formation of the platelet aggregation inhibitor prostacyclin (prostaglandin I2) in blood vessels; however, this action is reversible.
References
- DailyMed. "CODEINE SULFATE: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
- NCIt. "Codeine Phosphate: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).
- EPA DSStox. "Codeine: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).
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Information checked by Dr. Sachin Kumar, MD Pharmacology
