Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/4306
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Morphine Sulfate (Tablet, Extended Release)
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MORPHINE SULFATE EXTENDED-RELEASE TABLETS ARE AN OPIOID AGONIST AND A SCHEDULE II CONTROLLED SUBSTANCE WITH AN ABUSE LIABILITY SIMILAR TO OTHER OPIOID AGONISTS. MORPHINE AND OTHER OPIOIDS USED IN ANALGESIA CAN BE ABUSED AND ARE SUBJECT TO CRIMINAL DIVERSION. MORPHINE SULFATE EXTENDED-RELEASE TABLETS ARE TO BE SWALLOWED WHOLE, AND ARE NOT TO BE BROKEN, CHEWED, DISSOLVED, OR CRUSHED. TAKING BROKEN, CHEWED, DISSOLVED, OR CRUSHED MORPHINE SULFATE EXTENDED-RELEASE TABLETS LEADS TO RAPID RELEASE AND ABSORPTION OF A POTENTIALLY FATAL DOSE OF MORPHINE. Physicians should individualize treatment in every case, initiating therapy at the appropriate point along a progression from non-opioid analgesics, such as non-steroidal anti-inflammatory drugs and acetaminophen to opioids in a plan of pain management such as those outlined by the World Health Organization, the Federation of State Medical Boards Model Guidelines, or the American Pain Society. Healthcare professionals should follow appropriate pain management principles of careful assessment and ongoing monitoring . Morphine sulfate extended-release tablets are a controlled-release oral formulation of morphine sulfate indicated for the management of moderate to severe pain when a continuous, around-the-clock analgesic is needed for an extended period of time. The controlled-release nature of the formulation allows it to be administered on a more convenient schedule than conventional immediate-release oral morphine products . However, morphine sulfate extended-release tablets do not release morphine continuously over the course of a dosing interval. The administration of single doses of morphine sulfate extended-release tablets on a q12h dosing schedule will result in higher peak and lower trough plasma levels than those that occur when an identical daily dose of morphine is administered using conventional oral formulations on a q4h regimen. The clinical significance of greater fluctuations in morphine plasma level has not been systematically evaluated. As with any potent opioid drug product, it is critical to adjust the dosing regimen for each patient individually, taking into account the patient's prior opioid and non-opioid analgesic treatment experience. Although it is clearly impossible to enumerate every consideration that is important to the selection of initial dose and dosing interval of morphine sulfate extended-release tablets, attention should be given to 1) the daily dose, potency, and precise characteristics of the opioid the patient has been taking previously (e.g., whether it is a pure agonist or mixed agonist/antagonist), 2) the reliability of the relative potency estimate used to calculate the dose of morphine needed [N.B. potency estimates may vary with the route of administration], 3) the degree of opioid tolerance, if any, and 4) the general condition and medical status of the patient. The following dosing recommendations, therefore, can only be considered suggested approaches to what is actually a series of clinical decisions in the management of the pain of an individual patient. During periods of changing analgesic requirements including initial titration, frequent contact is recommended between physician, other members of the healthcare team, the patient, and the caregiver/family.<br/>Conversion from Immediate-Release Oral Morphine to Morphine Sulfate Extended-Release Tablets: A patient's daily morphine requirement is established using immediate-release oral morphine (dosing every 4 to 6 hours). The patient is then converted to morphine sulfate extended-release tablets in either of two ways: 1) by administering one-half of the patient's 24-hour requirement as morphine sulfate extended-release tablets on an every 12-hour schedule; or, 2) by administering one-third of the patient's daily requirement as morphine sulfate extended-release tablets on an every eight hour schedule. With either method, dose and dosing interval is then adjusted as needed (see discussion below). The 15 mg tablet should be used for initial conversion for patients whose total daily requirement is expected to be less than 60 mg. The 30 mg tablet strength is recommended for patients with a daily morphine requirement of 60 mg to 120 mg. When the total daily dose is expected to be greater than 120 mg, the appropriate combination of tablet strengths should be employed.<br/>Conversion from Parenteral Morphine or Other Opioids (Parenteral or Oral) to Morphine Sulfate Extended-Release Tablets: Morphine sulfate extended-release tablets can be administered as the initial oral morphine drug product; in this case, however, particular care must be exercised in the conversion process. Because of uncertainty about, and intersubject variation in, relative estimates of opioid potency and cross tolerance, initial dosing regimens should be conservative. It is better to underestimate the 24-hour oral morphine requirement than to overestimate. To this end, initial individual doses of morphine sulfate extended-release tablets should be estimated conservatively. In patients whose daily morphine requirements are expected to be less than or equal to 120 mg per day, the 30 mg tablet strength is recommended for the initial titration period. Once a stable dose regimen is reached, the patient can be converted to the 60 mg or 100 mg tablet strength, or an appropriate combination of tablet strengths, if desired. Estimates of the relative potency of opioids are only approximate and are influenced by route of administration, individual patient differences, and possibly, by an individual's medical condition. Consequently, it is difficult to recommend any fixed rule for converting a patient to morphine sulfate extended-release tablets directly. The following general points should be considered, however. Physicians are advised to refer to published relative potency data, keeping in mind that such ratios are only approximate. In general, it is safer to underestimate the daily dose of morphine sulfate extended-release tablets required and rely upon ad hoc supplementation to deal with inadequate analgesia (see discussion which follows).<br/>Use of Morphine Sulfate Extended-Release Tablets as the First Opioid Analgesic: There has been no systematic evaluation of morphine sulfate extended-release tablets as an initial opioid analgesic in the management of pain. Because it may be more difficult to titrate a patient using a controlled-release morphine, it is ordinarily advisable to begin treatment using an immediate-release formulation (see Special Instructions for Morphine Sulfate Extended-Release 100 mg and 200 mg Tablets).<br/>Considerations in the Adjustment of Dosing Regimens: Whatever the approach, if signs of excessive opioid effects are observed early in a dosing interval, the next dose should be reduced. If this adjustment leads to inadequate analgesia, that is,���breakthrough���pain occurs late in the dosing interval, the dosing interval may be shortened. Alternatively, a supplemental dose of a short-acting analgesic may be given. As experience is gained, adjustments can be made to obtain an appropriate balance between pain relief, opioid side effects, and the convenience of the dosing schedule. In adjusting dosing requirements, it is recommended that the dosing interval never be extended beyond 12 hours because the administration of very large single doses may lead to acute overdose. (N.B. Morphine sulfate extended-release tablets are a controlled-release formulation; it does not release morphine continuously over the dosing interval.) For patients with low daily morphine requirements, the 15 mg tablet should be used.<br/>Special Instructions for Morphine Sulfate Extended-Release 100 mg and 200 mg Tablets: (For use in opioid-tolerant patients only.) Morphine sulfate extended-release 100 mg and 200 mg tablets are for use only in opioid-tolerant patients requiring daily morphine equivalent dosages of 200 mg or more for the 100 mg tablet and 400 mg or more for the 200 mg tablet. It is recommended that these strengths be reserved for patients that have already been titrated to a stable analgesic regimen using lower strengths of morphine sulfate extended-release tablets or other opioids.<br/>Supplemental Analgesia: Most patients given around-the-clock therapy with controlled-release opioids may need to have immediate-release medication available for exacerbations of pain or to prevent pain that occurs predictably during certain patient activities (including incident pain).<br/>Continuation of Therapy: The intent of the titration period is to establish a patient-specific daily dose that will provide adequate analgesia with acceptable side effects and minimal rescue doses (2 or less) for as long as pain relief is necessary. Should pain recur, the dose can be increased to re-establish pain control as outlined above. During chronic, around-the-clock opioid therapy, especially for non-cancer pain syndromes, the continued need for around-the-clock opioid therapy should be reassessed periodically (e.g., every 6 to 12 months) as appropriate.<br/>Cessation of Therapy: When the patient no longer requires therapy with morphine sulfate extended-release tablets, doses should be tapered gradually to prevent signs and symptoms of withdrawal in the physically dependent patient.<br/>Conversion from Morphine Sulfate Extended-Release Tablets to Parenteral Opioids: When converting a patient from morphine sulfate extended-release tablets to parenteral opioids, it is best to assume that the parenteral to oral potency is high. NOTE THAT THIS IS THE CONVERSE OF THE STRATEGY USED WHEN THE DIRECTION OF CONVERSION IS FROM THE PARENTERAL TO ORAL FORMULATIONS. IN BOTH CASES, HOWEVER, THE AIM IS TO ESTIMATE THE NEW DOSE CONSERVATIVELY. For example, to estimate the required 24-hour dose of morphine for IM use, one could employ a conversion of 1 mg of morphine IM for every 6 mg of morphine as morphine sulfate extended-release tablets. The IM 24-hour dose would have tobe divided by six and administered on a q4h regimen. This approach is recommended because it is least likely to cause overdose.
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Morphine is a pure opioid agonist whose principal therapeutic action is analgesia. Other members of the class known as opioid agonists include substances such as oxycodone, hydromorphone, fentanyl, codeine, and hydrocodone. Pharmacological effects of opioid agonists include anxiolysis, euphoria, feelings of relaxation, respiratory depression, constipation, miosis, cough suppression, and analgesia. Like all pure opioid agonist analgesics, with increasing doses there is increasing analgesia, unlike with mixed agonist/antagonists or non-opioid analgesics, where there is a limit to the analgesic effect with increasing doses. With pure opioid agonist analgesics, there is no defined maximum dose; the ceiling to analgesic effectiveness is imposed only by side effects, the more serious which may include somnolence and respiratory depression.<br/>Central Nervous System: The principal actions of therapeutic value of morphine are analgesia and sedation (i.e., sleepiness and anxiolysis). The precise mechanism of the analgesic action is unknown. However, specific CNS opiate receptors for endogenous compounds with opioid-like activity have been identified throughout the brain and spinal cord and are likely to play a role in the expression of analgesic effects. Morphine produces respiratory depression by direct action on brainstem respiratory centers. The mechanism of respiratory depression involves a reduction in the responsiveness of the brainstem respiratory centers to increases in carbon dioxide tension, and to electrical stimulation. Morphine 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. Morphine causes miosis, even in total darkness. Pinpoint pupils are a sign of narcotic overdose but are not pathognomonic (e.g., pontine lesions of hemorrhagic or ischemic origins may produce similar findings). Marked mydriasis rather than miosis may be seen with worsening hypoxia.<br/>Gastrointestinal Tract and Other Smooth Muscle: Morphine causes a reduction in motility associated with an increase in smooth muscle tone in the antrum of the stomach and in the duodenum. Digestion of food is delayed in the small intestine 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-effectsmay include a reduction in gastric, biliary and pancreatic secretions, spasm of the sphincter of Oddi, and transient elevations in serum amylase.<br/>Cardiovascular System: Morphine produces peripheral vasodilation which may result in orthostatic hypotension. Release of histamine can occur and may contribute to opioid-induced hypotension. Manifestations of histamine release and/or peripheral vasodilation may include pruritus, flushing, red eyes, and sweating.<br/>Endocrine System: Opioids 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. Thyroidstimulating hormone (TSH) has been shown to be both inhibited and stimulated by opioids.<br/>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.<br/>Pharmacodynamics: As with all opioids, the minimum effective plasma concentration for analgesia varies 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. The minimum effective analgesic concentration of morphine for any individual patient may increase over time due to an increase in pain, the development of new pain syndrome and/or the development of analgesic tolerance.<br/>Plasma Level-Analgesia Relationships: In any particular patient, both analgesic effects and plasma morphine concentrations are related to the morphine dose. In non-tolerant individuals, plasma morphine concentration-efficacy relationships have been demonstrated and suggest that opiate receptors occupy effector compartments, leading to a lag-time, or hysteresis, between rapid changes in plasma morphine concentrations and the effects of such changes. The most direct and predictable concentration-effect relationships can, therefore, be expected at distribution equilibrium and/or steady-state conditions. While plasma morphine-efficacy relationships can be demonstrated in non-tolerant individuals, they are influenced by a wide variety of factors and are not generally useful as a guide to the clinical use of morphine. The effective dose in opioid-tolerant patients may be significantly greater than the appropriate dose for opioid-naive individuals. Dosages of morphine should be chosen and must be titrated on the basis of clinical evaluation of the patient and the balance between therapeutic and adverse effects. For any fixed dose and dosing interval, morphine sulfate extended-release tablets will have at steady-state a lower Cand a higher Cthan conventional morphine.<br/>Concentration-Adverse Experience Relationships: Morphine sulfate extended-release tablets are associated with typical opioid-related adverse experiences. There is a general relationship between increasing morphine plasma concentration and increasing frequency of dose-related opioid adverse experiences such as nausea, vomiting, CNS effects, and respiratory depression. In opioid-tolerant patients, the situation is altered by the development of tolerance to opioid-related side effects, and the relationship is not clinically relevant. As with all opioids, the dose must be individualized , because the effective analgesic dose for some patients will be too high to be tolerated by other patients.
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Morphine sulfate extended-release 100 mg tablets are oval,film-coated, gray tablets, debossed���E���on one side and���100���on the other side, packaged as follows: NDC 58177-340-04 bottle of 100 tablets NDC 58177-340-09 bottle of 1000 tablets NDC 58177-340-11 unit dose package of 100 tablets (10 tablets per blister card) Morphine sulfate extended-release 200 mg tablets are oval, film-coated, brown tablets, debossed���E���on one side and���200���on the other side, packaged as follows: NDC 58177-380-04 bottle of 100 tablets NDC 58177-380-09 bottle of 1000 tablets NDC 58177-380-11 unit dose package of 100 tablets (10 tablets per blister card) Store at 20��-25��C (68��-77��F). [See USP Controlled Room Temperature.] Dispense in tight, light-resistant and child-resistant containers as defined in the USP. Healthcare professionals can telephone ETHEX Corporation's Medical Affairs Department (1-800-321-1705) for information on this product. CAUTIONDEA Order Form Required. Manufactured byKV Pharmaceutical Co. forETHEX CorporationSt. Louis, MO 63044 P5470-3 8/07
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WARNING: Morphine sulfate extended-release tablets contain morphine sulfate, an opioid agonist and a Schedule II controlled substance, with an abuse liability similar to other opioid analgesics. Morphine can be abused in a manner similar to other opioid agonists, legal or illicit. This should be considered when prescribing or dispensing morphine sulfate extended-release tablets in situations where the physician or pharmacist is concerned about an increased risk of misuse, abuse, or diversion. Morphine sulfate extended-release tablets are a controlled-release oral formulation of morphine sulfate indicated for the management of moderate to severe pain when a continuous, around-the-clock opioid analgesic is needed for an extended period of time. Morphine sulfate extended-release tablets are NOT intended for use as a prn analgesic. Morphine sulfate extended-release 100 mg and 200 mg tablets ARE FOR USE IN OPIOID-TOLERANT PATIENTS ONLY. These tablet strengths may cause fatal respiratory depression when administered to patients not previously exposed to opioids. MORPHINE SULFATE EXTENDED-RELEASE TABLETS ARE TO BE SWALLOWED WHOLE AND ARE NOT TO BE BROKEN, CHEWED, DISSOLVED, OR CRUSHED. TAKING BROKEN, CHEWED, DISSOLVED, OR CRUSHED MORPHINE SULFATE EXTENDED-RELEASE TABLETS LEADS TO RAPID RELEASE AND ABSORPTION OF A POTENTIALLY FATAL DOSE OF MORPHINE.
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dailymed-ingredient:black_iron_oxide,
dailymed-ingredient:carnauba_wax,
dailymed-ingredient:hypromellose,
dailymed-ingredient:lactose_monohydrate,
dailymed-ingredient:magnesium_stearate,
dailymed-ingredient:polyethylene_glycol,
dailymed-ingredient:polysorbate_80,
dailymed-ingredient:stearic_acid,
dailymed-ingredient:titanium_dioxide
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Morphine Sulfate
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Morphine Sulfate (Tablet, Extended Release)
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The adverse reactions caused by morphine are essentially those observed with other opioid analgesics. They include the following major hazards: respiratory depression, apnea, and to a lesser degree, circulatory depression, respiratory arrest, shock, and cardiac arrest.<br/>Most Frequently Observed: Constipation, lightheadedness, dizziness, sedation, nausea, vomiting, sweating, dysphoria, and euphoria. Some of these effects seem to be more prominent in ambulatory patients and in those not experiencing severe pain. Some adverse reactions in ambulatory patients may be alleviated if the patient lies down.<br/>Less Frequently Observed Reactions: Central Nervous System: Weakness, headache, agitation, tremor, uncoordinated muscle movements, seizure, alterations of mood (nervousness, apprehension, depression, floating feelings), dreams, muscle rigidity, transient hallucinations and disorientation, visual disturbances, insomnia, increased intracranial pressure Gastrointestinal: Dry mouth, biliary tract spasm, laryngospasm, anorexia, diarrhea, cramps, taste alteration, constipation, ileus, intestinal obstruction, dyspepsia, increases in hepatic enzymes Cardiovascular: Flushing of the face, chills, tachycardia, bradycardia, palpitation, faintness, syncope, hypotension, hypertension Genitourinary: Urine retention or hesitance, amenorrhea, reduced libido and/or potency Dermatologic: Pruritus, urticaria, other skin rashes, edema, diaphoresis Other: Antidiuretic effect, paresthesia, bronchospasm, muscle tremor, blurred vision, nystagmus, diplopia, miosis, anaphylaxis
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Morphine sulfate extended-release tablets are a controlled-release oral formulation of morphine sulfate indicated for the management of moderate to severe pain when a continuous, around-the-clock opioid analgesic is needed for an extended period of time. Morphine sulfate extended-release tablets are NOT intended for use as a prn analgesic. Morphine sulfate extended-release 100 mg and 200 mg tablet strengths are high dose, controlled-release, oral morphine formulations indicated for the relief of pain in opioid-tolerant patients only. Morphine sulfate extended-release tablets are not indicated for pain in the immediate postoperative period (the first 12 to 24 hours following surgery) for patients not previously taking the drug, because its safety in this setting has not been established. Morphine sulfate extended-release tablets are not indicated for pain in the postoperative period if the pain is mild, or not expected to persist for an extended period of time. Morphine sulfate extended-release tablets are only indicated for postoperative use if the patient is already receiving the drug prior to surgery or if the postoperative pain is expected to be moderate to severe and persist for an extended period of time. Physicians should individualize treatment, moving from parenteral to oral analgesics as appropriate (see American Pain Society guidelines).
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Morphine Sulfate
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