Central Nervous System. The precise mechanism of the analgesic action is unknown. However, specific CNS opioid receptors for endogenous compounds with opioid-like activity have been identified throughout the brain and spinal cord and are thought to play a role in the analgesic effects of this drug. A single-dose, double-blind, placebo- and dose-controlled study was conducted using OxyContin 10, 20, and 30 mg in an analgesic pain model involving patients with moderate to severe pain.
OxyContin doses of 20 mg and 30 mg produced statistically significant pain reduction compared to placebo. Oxycodone produces respiratory depression by direct action on brain stem respiratory centers. The respiratory depression involves both a reduction in the responsiveness of the brain stem respiratory centers to increases in CO 2 tension and to electrical stimulation.
Oxycodone depresses the cough reflex by direct effect on the cough center in the medulla. Antitussive effects may occur with doses lower than those usually required for analgesia. Oxycodone causes miosis, even in total darkness. Pinpoint pupils are a sign of opioid overdose but are not pathognomonic e. Marked mydriasis rather than miosis may be seen with hypoxia in the setting of oxycodone overdose [See Overdosage 10 ]. Gastrointestinal Tract and Other Smooth Muscle. Oxycodone causes a reduction in motility associated with an increase in smooth muscle 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 may be increased to the point of spasm resulting in constipation. Other opioid-induced effects may include a reduction in gastric, biliary and pancreatic secretions, spasm of sphincter of Oddi, and transient elevations in serum amylase.
Oxycodone may produce release of histamine with or without associated peripheral vasodilation. Opioids may influence the hypothalamic-pituitary-adrenal or -gonadal axes. Some changes that can be seen include an increase in serum prolactin, and decreases in plasma cortisol and testosterone.
Clinical signs and symptoms may be manifest from these hormonal changes. In vitro and animal studies indicate that opioids have a variety of effects on immune functions, depending on the context in which they are used. The clinical significance of these findings is unknown. Concentration — Efficacy Relationships. Studies in normal volunteers and patients reveal predictable relationships between oxycodone dosage and plasma oxycodone concentrations, as well as between concentration and certain expected opioid effects, such as pupillary constriction, sedation, overall subjective "drug effect", analgesia and feelings of "relaxation".
The minimum effective analgesic concentration will vary widely among patients, especially among patients who have been previously treated with potent agonist opioids. As a result, patients must be treated with individualized titration of dosage to the desired effect. Concentration — Adverse Reaction Relationships. There is a relationship between increasing oxycodone plasma concentration and increasing frequency of dose-related opioid adverse reactions such as nausea, vomiting, CNS effects, and respiratory depression.
In opioid-tolerant patients, the situation may be altered by the development of tolerance to opioid-related side effects. The dose of OxyContin must be individualized [see Dosage and Administration 2.
The activity of OxyContin is primarily due to the parent drug oxycodone. OxyContin is designed to provide delivery of oxycodone over 12 hours. Cutting, breaking, chewing, crushing or dissolving OxyContin impairs the controlled-release delivery mechanism and results in the rapid release and absorption of a potentially fatal dose of oxycodone.
Oxycodone release from OxyContin is pH independent. Upon repeated dosing with OxyContin in healthy subjects in pharmacokinetic studies, steady-state levels were achieved within hours. Oxycodone is extensively metabolized and eliminated primarily in the urine as both conjugated and unconjugated metabolites.
The apparent elimination half-life of oxycodone following the administration of OxyContin was 4. Plasma Oxycodone Concentration Over Time. Dose proportionality has been established for OxyContin 10 mg, 15 mg, 20 mg, 30 mg, 40 mg, 60 mg, and 80 mg tablet strengths for both peak plasma concentrations C max and extent of absorption AUC see Table 3.
Given the short elimination half-life of oxycodone, steady-state plasma concentrations of oxycodone are achieved within hours of initiation of dosing with OxyContin. In a study comparing 10 mg of OxyContin every 12 hours to 5 mg of immediate-release oxycodone every 6 hours, the two treatments were found to be equivalent for AUC and C max , and similar for C min trough concentrations.
Following intravenous administration, the steady-state volume of distribution Vss for oxycodone was 2. Once absorbed, oxycodone is distributed to skeletal muscle, liver, intestinal tract, lungs, spleen, and brain. Oxycodone has been found in breast milk [see Use In Specific Populations 8. Oxycodone is extensively metabolized by multiple metabolic pathways to produce noroxycodone, oxymorphone and noroxymorphone, which are subsequently glucuronidated.
Noroxycodone and noroxymorphone are the major circulating metabolites. CYP3A mediated N-demethylation to noroxycodone is the primary metabolic pathway of oxycodone with a lower contribution from CYP2D6 mediated O-demethylation to oxymorphone. Therefore, the formation of these and related metabolites can, in theory, be affected by other drugs see Drug-Drug Interactions. Noroxycodone exhibits very weak anti-nociceptive potency compared to oxycodone, however, it undergoes further oxidation to produce noroxymorphone, which is active at opioid receptors.
Although noroxymorphone is an active metabolite and present at relatively high concentrations in circulation, it does not appear to cross the blood-brain barrier to a significant extent. Oxymorphone is present in the plasma only at low concentrations and undergoes further metabolism to form its glucuronide and noroxymorphone. Oxymorphone has been shown to be active and possessing analgesic activity but its contribution to analgesia following oxycodone administration is thought to be clinically insignificant.
The enzymes responsible for keto-reduction and glucuronidation pathways in oxycodone metabolism have not been established. Oxycodone and its metabolites are excreted primarily via the kidney. The amounts measured in the urine have been reported as follows: free and conjugated oxycodone 8. The total plasma clearance was approximately 1. The reason for this difference is unknown [see Use In Specific Populations 8.
This was accompanied by an increase in sedation but not by differences in respiratory rate, pupillary constriction, or several other measures of drug effect. These differences are accompanied by increases in some, but not other, drug effects. Oxycodone is extensively metabolized by multiple metabolic pathways. Drugs that inhibit CYP3A4 activity, such as macrolide antibiotics e.
For example, a published study showed that the co-administration of the antifungal drug, voriconazole, increased oxycodone AUC and C max by 3. Similarly, CYP inducers, such as rifampin, carbamazepine, and phenytoin, may induce the metabolism of oxycodone and, therefore, may cause increased clearance of the drug which could lead to a decrease in oxycodone plasma concentrations, lack of efficacy or, possibly, development of an abstinence syndrome in a patient who had developed physical dependence to oxycodone.
The formation of oxymorphone may be blocked by a variety of drugs such as antipsychotics, beta blockers, antidepressants, etc. However, in a study involving ten subjects using quinidine, a known inhibitor of CYP2D6, the pharmacodynamic effects of oxycodone were unchanged.
The genetic expression of CYP2D6 may have some influence in the pharmacokinetic properties of oxycodone. The in vitro drug-drug interaction studies with noroxymorphone using human liver microsomes showed no significant inhibition of CYP2D6 and CYP3A4 activities which suggests that noroxymorphone may not alter the metabolism of other drugs that are metabolized by CYP2D6 and CYP3A4, and such blockade has not been shown to be of clinical significance with oxycodone.
In a second chromosomal aberration assay with human lymphocytes, no structural clastogenicity was observed either with or without metabolic activation; however, in the absence of metabolic activation, oxycodone increased numerical chromosomal aberrations polyploidy.
Oxycodone was not genotoxic in the following assays: Ames S. In a study of reproductive performance, rats were administered a once daily gavage dose of the vehicle or oxycodone hydrochloride 0. Male rats were dosed for 28 days before cohabitation with females, during the cohabitation and until necropsy weeks post-cohabitation.
Females were dosed for 14 days before cohabitation with males, during cohabitation and up to gestation day 6.
A double-blind, placebo-controlled, fixed-dose, parallel group, two-week study was conducted in patients with persistent, moderate to severe pain, who were judged as having inadequate pain control with their current therapy. In this study, OxyContin 20 mg, but not 10 mg, was statistically significant in pain reduction compared with placebo.
OxyContin oxycodone hydrochloride controlled-release Tablets 10 mg are round, white-colored, bi-convex tablets debossed with OP on one side and 10 on the other and are supplied as child-resistant closure, opaque plastic bottles of NDC and unit dose packaging with 10 individually numbered tablets per card; two cards per glue end carton NDC OxyContin oxycodone hydrochloride controlled-release Tablets 15 mg are round, gray-colored, bi-convex tablets debossed with OP on one side and 15 on the other and are supplied as child-resistant closure, opaque plastic bottles of NDC and unit dose packaging with 10 individually numbered tablets per card; two cards per glue end carton NDC OxyContin oxycodone hydrochloride controlled-release Tablets 20 mg are round, pink-colored, bi-convex tablets debossed with OP on one side and 20 on the other and are supplied as child-resistant closure, opaque plastic bottles of NDC and unit dose packaging with 10 individually numbered tablets per card; two cards per glue end carton NDC OxyContin oxycodone hydrochloride controlled-release Tablets 30 mg are round, brown-colored, bi-convex tablets debossed with OP on one side and 30 on the other and are supplied as child-resistant closure, opaque plastic bottles of NDC and unit dose packaging with 10 individually numbered tablets per card; two cards per glue end carton NDC OxyContin oxycodone hydrochloride controlled-release Tablets 40 mg are round, yellow-colored, bi-convex tablets debossed with OP on one side and 40 on the other and are supplied as child-resistant closure, opaque plastic bottles of NDC and unit dose packaging with 10 individually numbered tablets per card; two cards per glue end carton NDC OxyContin oxycodone hydrochloride controlled-release Tablets 60 mg are round, red-colored, bi-convex tablets debossed with OP on one side and 60 on the other and are supplied as child-resistant closure, opaque plastic bottles of NDC and unit dose packaging with 10 individually numbered tablets per card; two cards per glue end carton NDC OxyContin oxycodone hydrochloride controlled-release Tablets 80 mg are round, green-colored, bi-convex tablets debossed with OP on one side and 80 on the other and are supplied as child-resistant closure, opaque plastic bottles of NDC and unit dose packaging with 10 individually numbered tablets per card; two cards per glue end carton NDC Provide the following information to patients receiving OxyContin or their caregivers:.
Healthcare professionals can telephone Purdue Pharma's Medical Services Department for information on this product. Purdue Pharma L. Stamford, CT Read this Medication Guide before you start taking OxyContin and each time you get a refill. There may be new information. This Medication Guide does not take the place of talking to your healthcare provider about your medical condition or your treatment. What is the most important information I should know about OxyContin?
What should I tell my healthcare provider before taking OxyContin? OxyContin may not be right for you. Before taking OxyContin, tell your doctor if you:. If you take OxyContin right before your baby is born, your baby could have breathing problems at birth. Tell your healthcare provider about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements.
Sometimes the doses of medicines that you take with OxyContin may need to be changed if used together. Do not take other medicines without talking to your healthcare provider. Your healthcare provider will tell you if it is safe to take other medicines while you take OxyContin. Know the medicines you take. Keep a list of your medicines to show your healthcare provider and pharmacist. What should I avoid while taking OxyContin?
What are the possible side effects of OxyContin? OxyContin can cause serious side effects, including:. These can be signs or symptoms that you have taken too much OxyContin overdose or the dose is too high for you.
These symptoms may lead to serious problems or death if not treated right away. The most common side effects of OxyContin include:. Some of these side effects may decrease with continued use.
Talk with your healthcare provider if you continue to have these side effects. These are not all the possible side effects of OxyContin.
For a complete list, ask your healthcare provider or pharmacist. Constipation not often enough or hard bowel movements is a very common side effect of pain medicines opioids including OxyContin, and is unlikely to go away without treatment. Talk to your healthcare provider about dietary changes, and the use of laxatives medicines to treat constipation and stool softeners to prevent or treat constipation while taking OxyContin.
Call your doctor for medical advice about side effects. General information about OxyContin Medicines are sometimes prescribed for purposes other than those listed in a Medication Guide. Do not use OxyContin for a condition for which it was not prescribed. Never give your OxyContin to other people even if they have the same symptoms you have. Selling or giving away OxyContin may harm others, even causing death, and is against the law.
This Medication Guide summarizes the most important information about OxyContin. If you would like more information, talk with your healthcare provider. You can ask your healthcare provider or pharmacist for information about OxyContin that is written for health professionals. For more information about OxyContin, go to www. Active ingredient: oxycodone hydrochloride Inactive ingredients in all strengths: butylated hydroxytoluene BHT , hypromellose, polyethylene glycol , polyethylene oxide, magnesium stearate, titanium dioxide.
Always check to make sure that the medicine you are taking is the correct one. The dosage strength and appearance of each OxyContin tablet are as follows:. DailyMed will deliver notification of updates and additions to Drug Label information currently shown on this site through its RSS feed. DailyMed will deliver this notification to your desktop, Web browser, or e-mail depending on the RSS Reader you select to use.
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Drug Label Info. Approval: Monitor for decreased bowel motility in postoperative patients. Limitations of Usage OxyContin is not intended for use on an as-needed basis. OxyContin is not indicated for rectal administration. Attention should be given to: risk factors for abuse or addiction; including whether the patient has a previous or current substance abuse problem, a family history of substance abuse, or a history of mental illness or depression; the age, general condition and medical status of the patient; the patient's opioid exposure and opioid tolerance if any ; the daily dose, potency, and kind of the analgesic s the patient has been taking; the reliability of the conversion estimate used to calculate the dose of oxycodone; the special instructions for OxyContin 60 mg and 80 mg tablets, a single dose greater than 40 mg, or total daily doses greater than 80 mg [see Dosage and Administration 2.
A reasonable approach for converting from existing opioid therapy to OxyContin is as follows: Discontinue all other around-the-clock opioid drugs when OxyContin therapy is initiated. Divide the calculated hour oxycodone dose in half to approximate the every hour dose of OxyContin. Round down, if necessary, to the appropriate OxyContin tablet strengths available. Close observation and frequent titration are indicated until patients are stable on the new therapy.
For patients receiving high-dose parenteral opioids, a more conservative conversion is warranted. For example, for high-dose parenteral morphine, use 1. OxyContin is contraindicated in: patients who have significant respiratory depression patients who have or are suspected of having paralytic ileus patients who have acute or severe bronchial asthma patients who have known hypersensitivity to any of its components or the active ingredient, oxycodone.
Use OxyContin with extreme caution in patients with any of the following: significant chronic obstructive pulmonary disease or cor pulmonale other risk of substantially decreased respiratory reserve hypoxia hypercapnia pre-existing respiratory depression Respiratory depression induced by opioids typically follows a pattern entailing first a shift in CO 2 responsiveness of the CNS respiratory drive center, which results in a decrease in the urge to breathe, despite the presence of hypercapnia.
The following adverse reactions described elsewhere in the labeling include: Respiratory depression [see Boxed Warning, Warnings and Precautions 5.
Because these events are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure: abuse, addiction, overdose, death, amenorrhea, symptoms associated with an anaphylactic or anaphylactoid reaction, cholestasis, dental caries, increased hepatic enzymes, muscular hypertonia, hyponatremia, ileus, palpitations in the context of withdrawal , seizures, syndrome of inappropriate antidiuretic hormone secretion, and urticaria In addition to the events listed above, the following have also been reported, potentially due to the swelling and hydrogelling property of the tablet: choking, gagging, regurgitation, tablets stuck in the throat and difficulty swallowing the tablet.
Teratogenic Effects The effect of oxycodone in human reproduction has not been adequately studied. Central Nervous System Oxycodone produces respiratory depression by direct action on brain stem respiratory centers. Gastrointestinal Tract and Other Smooth Muscle Oxycodone causes a reduction in motility associated with an increase in smooth muscle tone in the antrum of the stomach and duodenum. Cardiovascular System Oxycodone may produce release of histamine with or without associated peripheral vasodilation.
Endocrine System Opioids may influence the hypothalamic-pituitary-adrenal or -gonadal axes. Immune System In vitro and animal studies indicate that opioids have a variety of effects on immune functions, depending on the context in which they are used. Concentration — Efficacy Relationships Studies in normal volunteers and patients reveal predictable relationships between oxycodone dosage and plasma oxycodone concentrations, as well as between concentration and certain expected opioid effects, such as pupillary constriction, sedation, overall subjective "drug effect", analgesia and feelings of "relaxation".
Concentration — Adverse Reaction Relationships There is a relationship between increasing oxycodone plasma concentration and increasing frequency of dose-related opioid adverse reactions such as nausea, vomiting, CNS effects, and respiratory depression. Plasma Oxycodone Concentration Over Time Dose proportionality has been established for OxyContin 10 mg, 15 mg, 20 mg, 30 mg, 40 mg, 60 mg, and 80 mg tablet strengths for both peak plasma concentrations C max and extent of absorption AUC see Table 3.
Impairment of Fertility In a study of reproductive performance, rats were administered a once daily gavage dose of the vehicle or oxycodone hydrochloride 0.
Adapted from Foley, KM. N Engl J Med, ; Dispense in tight, light-resistant container. Advise patients that OxyContin is designed to work properly only if swallowed whole. Taking cut, broken, chewed, crushed, or dissolved OxyContin Tablets can result in a fatal overdose.
Advise patients that OxyContin tablets should be taken one tablet at a time. Advise patients not to pre-soak, lick or otherwise wet the tablet prior to placing in the mouth. Take this medicine only as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered. This is especially important for elderly patients, who may be more sensitive to the effects of pain medicines.
If too much of this medicine is taken for a long time, it may become habit-forming causing mental or physical dependence. It is very important that you understand the rules of the Opioid Analgesic REMS program to prevent addiction, abuse, and misuse of oxycodone.
This medicine should also come with a Medication Guide and a patient information leaflet. Read and follow these instructions carefully. Read it again each time you refill your prescription in case there is new information. Ask your doctor if you have any questions. Oxycodone extended-release capsules or tablets should only be used by patients who have already been taking narcotic pain medicines, also called opioids.
These patients are called opioid-tolerant. If you are uncertain whether or not you are opioid-tolerant, check with your doctor before using this medicine. Measure the oral liquid concentrate with the calibrated dropper that comes with the package. Your doctor may have you mix the concentrate with a small amount of liquid or food. Carefully follow the instructions and take the medicine mixture right away.
Measure the oral liquid with a marked measuring spoon, oral syringe, or medicine cup. The average household teaspoon may not hold the right amount of liquid. Do not break, crush, cut, chew, or dissolve it. Do not pre-soak, lick, or wet the tablet before placing it in the mouth. Take one tablet at a time. Also, do not give this medicine through nasogastric or feeding tubes. Oxycodone extended-release capsules or tablets work differently from the regular oxycodone oral solution or tablets, even at the same dose.
For seniors: The kidneys of older adults may not work as well as they used to. For people at risk of misuse, addiction, or overdose: Using oxycodone can lead to addiction and misuse, which can result in overdose or death. Your doctor may prescribe naloxone, which is a drug used to treat an oxycodone overdose. Talk with your doctor or pharmacist about how to get or use naloxone. Oxycodone oral tablet is used for short-term or long-term treatment.
The length of treatment depends on how severe your pain is. If you stop taking the drug suddenly, you may have symptoms of withdrawal, which can include:. For this drug to work well, a certain amount needs to be in your body at all times. If you take too much: You could have dangerous levels of the drug in your body. Symptoms of an overdose of this drug can include:.
But if your symptoms are severe, call or go to the nearest emergency room right away. If you think you might be at risk of misuse or overdose, talk with your doctor about naloxone. What to do if you miss a dose: Take your dose as soon as you remember. But if you remember just a few hours before your next scheduled dose, skip the missed dose and go back to your regular dosing schedule. A prescription for this medication is not refillable.
You or your pharmacy will have to contact your doctor for a new prescription if you need this medication refilled. You and your doctor should monitor certain health issues.
This can help make sure you stay safe while you take this drug. These issues include:. Not every pharmacy stocks this drug. When filling your prescription, be sure to call ahead to make sure your pharmacy carries it. Many insurance companies require a prior authorization for this drug.
This means your doctor will need to get approval from your insurance company before your insurance company will pay for the prescription. There are other drugs available to treat your condition. Some may be better suited for you than others. Talk to your doctor about other drug options that may work for you. Disclaimer: Medical News Today has made every effort to make certain that all information is factually correct, comprehensive, and up-to-date.
However, this article should not be used as a substitute for the knowledge and expertise of a licensed healthcare professional. You should always consult your doctor or other healthcare professional before taking any medication.
The drug information contained herein is subject to change and is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. The absence of warnings or other information for a given drug does not indicate that the drug or drug combination is safe, effective, or appropriate for all patients or all specific uses.
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