The action of the drug on the human body is called Pharmacodynamics in Medical terminology. To produce its effect and to change the pathological process that is happening the body and to reduce the symptom or cure the disease, the medicine has to function in a specific way. The changes it does to the body at cellular level gives the desired result of treating a disease. Drugs act by stimulating or inhibiting a receptor or an enzyme or a protein most of the times. Medications are produced in such a way that the ingredients target the specific site and bring about chemical changes in the body that can stop or reverse the chemical reaction which is causing the disease.
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Codeine (Polery) Sulfate is an opioid analgesic, related to morphine, but with less potent analgesic properties. Codeine (Polery) is selective for the mu receptor, but with a much weaker affinity than morphine. The analgesic properties of Codeine (Polery) 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 (Polery) 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 (Polery) include anxiolysis, euphoria, and feelings of relaxation. Codeine (Polery) Sulfate causes respiratory depression, in part by a direct effect on the brainstem respiratory centers. Codeine (Polery) Sulfate and other related opioids depress the cough reflex by direct effect on the cough center in the medulla. Codeine (Polery) 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 (Polery). Codeine (Polery) 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 (Polery) can cause a marked increase in biliary tract pressure as a result of the spasm of the sphincter of Oddi. Codeine (Polery) may also cause spasms of the sphincter of the urinary bladder.
Effects on the Cardiovascular System
Codeine (Polery) 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 (Polery) 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 (Polery) 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 (Polery)?
Follow all directions on your prescription label. Codeine (Polery) can slow or stop your breathing. Never use Codeine (Polery) 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 (Polery) 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 (Polery) is against the law.
Take Codeine (Polery) 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 (Polery). Do not use a stool softener (laxative) without first asking your doctor.
Do not stop using Codeine (Polery) 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 (Polery).
Store at room temperature away from moisture and heat.
Keep track of the amount of medicine used from each new bottle. Codeine (Polery) 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 (Polery) administration
Administration of drug is important to know because the drug absorption and action varies depending on the route and time of administration of the drug. A medicine is prescribed before meals or after meals or along with meals. The specific timing of the drug intake about food is to increase its absorption and thus its efficacy. Few work well when taken in empty stomach and few medications need to be taken 1 or 2 hrs after the meal. A drug can be in the form of a tablet, a capsule which is the oral route of administration and the same can be in IV form which is used in specific cases. Other forms of drug administration can be a suppository in anal route or an inhalation route.
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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 (Polery) 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 (Polery) pharmacology
Pharmacokinetics of a drug can be defined as what body does to the drug after it is taken. The therapeutic result of the medicine depends upon the Pharmacokinetics of the drug. It deals with the time taken for the drug to be absorbed, metabolized, the process and chemical reactions involved in metabolism and about the excretion of the drug. All these factors are essential to deciding on the efficacy of the drug. Based on these pharmacokinetic principles, the ingredients, the Pharmaceutical company decides dose and route of administration. The concentration of the drug at the site of action which is proportional to therapeutic result inside the body depends on various pharmacokinetic reactions that occur in the body.
Mechanism of Action
Codeine (Polery) is an opioid agonist, related to morphine, but with less potent analgesic properties. Codeine (Polery) is selective for the mu receptor, but with a much weaker affinity than morphine. The analgesic properties of Codeine (Polery) 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 (Polery) 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 (Polery) include anxiolysis, euphoria, and feelings of relaxation. Codeine (Polery) causes respiratory depression, in part by a direct effect on the brainstem respiratory centers. Codeine (Polery) and other related opioids depress the cough reflex by direct effect on the cough center in the medulla. Codeine (Polery) may also cause miosis.
Effects on the Gastrointestinal Tract and on Other Smooth Muscle: Gastric, biliary and pancreatic secretions may be decreased by Codeine (Polery). Codeine (Polery) 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 (Polery) can cause a marked increase in biliary tract pressure as a result of the spasm of the sphincter of Oddi. Codeine (Polery) may also cause spasms of the sphincter of the urinary bladder.
Effects on the Cardiovascular System: In therapeutic doses, Codeine (Polery) does not usually exert major effects on the cardiovascular system. Codeine (Polery) 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 (Polery) plasma concentrations do not correlate with Codeine (Polery) 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 (Polery), when administered as Codeine (Polery) sulfate, is absorbed from the gastrointestinal tract with maximum plasma concentration occurring 60 minutes post administration.
Food Effects: When 60 mg Codeine (Polery) 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 (Polery).
Steady-state: Administration of 15 mg Codeine (Polery) sulfate every four hours for 5 days resulted in steady-state concentrations of Codeine (Polery), morphine, morphine-3-glucuronide (M3G) and morphine-6-glucuronide (M6G) within 48 hours.
Distribution: Codeine (Polery) 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 (Polery) has low plasma protein binding with about 7-25% of Codeine (Polery) bound to plasma proteins.
Metabolism: About 70-80% of the administered dose of Codeine (Polery) is metabolized by conjugation with glucuronic acid to Codeine (Polery)-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 (Polery) to C6G. Cytochrome P450 2D6 is the major enzyme responsible for conversion of Codeine (Polery) to morphine (about 5-10%) and P450 3A4 is the major enzyme mediating conversion of Codeine (Polery) 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 (Polery) is excreted through the kidneys, of which approximately 10% is unchanged Codeine (Polery). Plasma half-lives of Codeine (Polery) and its metabolites have been reported to be approximately 3 hours.
Actions of Pholcodine (Polery) in details
The action of the drug on the human body is called Pharmacodynamics in Medical terminology. To produce its effect and to change the pathological process that is happening the body and to reduce the symptom or cure the disease, the medicine has to function in a specific way. The changes it does to the body at cellular level gives the desired result of treating a disease. Drugs act by stimulating or inhibiting a receptor or an enzyme or a protein most of the times. Medications are produced in such a way that the ingredients target the specific site and bring about chemical changes in the body that can stop or reverse the chemical reaction which is causing the disease.
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Description: Pholcodine (Polery) is an anti-tussive agent that acts primarily on the CNS, causing depression of the cough reflex. It has mild sedative effect with little or no analgesic action.
Pharmacokinetics:
Absorption: Tmax: About 4-8 hr after oral admin.
Distribution: Protein binding: About 23.5%. Vd: About 36-49 L/kg.
Metabolism: Metabolised in the liver with little conjugation. No transformation to morphine.
Excretion: Elimination half-life: About 32-43 hr.
Pholcodine (Polery) administration
Administration of drug is important to know because the drug absorption and action varies depending on the route and time of administration of the drug. A medicine is prescribed before meals or after meals or along with meals. The specific timing of the drug intake about food is to increase its absorption and thus its efficacy. Few work well when taken in empty stomach and few medications need to be taken 1 or 2 hrs after the meal. A drug can be in the form of a tablet, a capsule which is the oral route of administration and the same can be in IV form which is used in specific cases. Other forms of drug administration can be a suppository in anal route or an inhalation route.
Use exactly as directed on the label, or as prescribed by your doctor. Do not use in larger or smaller amounts or for longer than recommended. This medicine is usually taken only for a short time until your symptoms clear up.
Do not take for longer than 7 days in a row. Talk with your doctor if your symptoms do not improve after 7 days of treatment, or if you have a fever with a headache or skin rash.
Do not crush, chew, or break an extended-release tablet. Swallow it whole. Breaking the pill may cause too much of the drug to be released at one time.
Measure liquid medicine with a special dose-measuring spoon or medicine cup, not with a regular table spoon. If you do not have a dose-measuring device, ask your pharmacist for one.
Do not give this medication to a child younger than 4 years old. Always ask a doctor before giving a cough or cold medicine to a child. Death can occur from the misuse of cough and cold medicines in very young children.
If you need surgery or medical tests, tell the surgeon or doctor ahead of time if you have taken this medicine within the past few days.
Store at room temperature away from moisture and heat. Do not allow the liquid form of this medicine to freeze.
Pholcodine (Polery) pharmacology
Pharmacokinetics of a drug can be defined as what body does to the drug after it is taken. The therapeutic result of the medicine depends upon the Pharmacokinetics of the drug. It deals with the time taken for the drug to be absorbed, metabolized, the process and chemical reactions involved in metabolism and about the excretion of the drug. All these factors are essential to deciding on the efficacy of the drug. Based on these pharmacokinetic principles, the ingredients, the Pharmaceutical company decides dose and route of administration. The concentration of the drug at the site of action which is proportional to therapeutic result inside the body depends on various pharmacokinetic reactions that occur in the body.
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Pholcodine (Polery) produces its ophthalmic and systemic actions by acting on alpha 1 adrenergic receptors in the pupillary dilator muscle and the vascular smooth musle, resulting in contraction of the dilator muscle and contraction of the smooth muscle in the arterioles of the conjunctiva and peripheral vasoconstriction. Pholcodine (Polery) decreases nasal congestion by acting on alpha 1 adrenergic receptors in the arterioles of the nasal mucosa to produce constriction.
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. "Pholcodine: 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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