Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/1859
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Hydromorphone Hydrochloride (Tablet)
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Hydromorphone hydrochloride tablets (2 mg, 4 mg, 8 mg): The usual starting dose for hydromorphone hydrochloride tablets is 2 mg to 4 mg, orally, every 4 to 6 hours. Appropriate use of the hydromorphone hydrochloride tablets must be decided by careful evaluation of each clinical situation. A gradual increase in dose may be required if analgesia is inadequate, as tolerance develops, or if pain severity increases. The first sign of tolerance is usually a reduced duration of effect. Patients with hepatic and renal impairment should be started on lower starting dose .
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Hydromorphone hydrochloride is a pure opioid agonist with the principal therapeutic activity of analgesia. A significant feature of the analgesia is that it can occur without loss of consciousness. Opioid analgesics also suppress the cough reflex and may cause respiratory depression, mood changes, mental clouding, euphoria, dysphoria, nausea, vomiting and electroencephalographic changes. Many of the effects described below are common to this class of mu-opioid agonist analgesics which includes morphine, oxycodone, hydrocodone, codeine and fentanyl. In some instances, data may not exist to distinguish the effects of hydromorphone hydrochloride tablets from those observed with other opioid analgesics. However, in the absence of data to the contrary, it is assumed that hydromorphone hydrochloride tablets would possess all the actions of mu-agonist opioids.<br/>Central Nervous System: The precise mode of analgesic action of opioid analgesics is unknown. However, specific CNS opiate receptors have been identified. Opioids are believed to express their pharmacological effects by combining with these receptors. Hydromorphone depresses the cough reflex by direct effect on the cough center in the medulla. Hydromorphone depresses the respiratory reflex by a direct effect on brain stem respiratory centers. The mechanism of respiratory depression also involves a reduction in the responsiveness of the brain stem respiratory centers to increases in carbon dioxide tension. Hydromorphone causes miosis. Pinpoint pupils are a common sign of opioid overdose but are not pathognomonic (e.g., pontine lesions of hemorrhagic or ischemic origin may produce similar findings).Marked mydriasis rather than miosis may be seen with hypoxia in the setting of hydromorphone hydrochloride overdose.<br/>Gastrointestinal Tract and Other Smooth Muscle: Gastric, biliary and pancreatic secretions are decreased by opioids such as hydromorphone. Hydromorphone causes a reduction in motility associated with an increase in tone in the gastric antrum and duodenum. Digestion of food in the small intestine is delayed propulsive contractions are decreased. Propulsive peristaltic waves in the colon are decreased, and tone may be increased to the point of spasm. The end result is constipation. Hydromorphone can cause a marked increase in biliary tract pressure as aresult of spasm of the sphincter of Oddi.<br/>Cardiovascular System: Hydromorphone may produce hypotension as a result of either peripheral vasodilation or release of histamine, or both. Other manifestations of histamine release and/or peripheral vasodilation may include pruritis, flushing, and red eyes.<br/>Pharmacokinetics and Metabolism: The analgesic activity of hydromorphone hydrochloride is due to the parent drug hydromorphone. Hydromorphone is rapidly absorbed from the gastrointestinal tract after oral administration and undergoes extensive first-pass metabolism. Exposure of hydromorphone (Cand AUC) is dose-proportional at a dose range of 2 and 8 mg. In vivo bioavailability following single-dose administration of the 8 mg tablet is approximately 24% (coefficient of variation 21%).<br/>Absorption: After oral administration of hydromorphone hydrochloride 8 mg tablets, peak plasma hydromorphone concentrations are generally attained within��to 1 hour.<br/>Food effects: In a study conducted with a single 8 mg dose of hydromorphone (2 mg hydromorphone hydrochloride immediate release tablets), food lowered Cby 25%, prolonged Tby 0.8 hour, and increased AUC by 35%. The effects may not be clinically relevant.<br/>Distribution: At therapeutic plasma levels, hydromorphone is approximately 8-19% bound to plasma proteins. After an intravenous bolus dose, the steady state of volume distribution [mean (%cv)] is 302.9 (32%) liters.<br/>Metabolism: Hydromorphone is extensively metabolized via glucuronidation in the liver, with greater than 95% of the dose metabolized to hydromorphone-3-glucuronide along with minor amounts of 6-hydroxy reduction metabolites.<br/>Elimination: Only a small amount of the hydromorphone dose is excreted unchanged in the urine. Most of the dose is excreted as hydromorphone-3-glucuronide along with minor amounts of 6-hydroxy reduction metabolites. The systemic clearance is approximately 1.96 (20%) liters/minute. The terminal elimination half-life of hydromorphone after an intravenous dose is about 2.3 hours.<br/>Special Populations: Hepatic Impairment After oral administration of hydromorphone at a single 4 mg dose (2 mg hydromorphone hydrochloride immediate release tablets), mean exposure to hydromorphone (Cand AUC) is increased 4-fold in patients with moderate (Child-Pugh Group B) hepatic impairment compared with subjects with normal hepatic function. Due to increased exposure of hydromorphone, patients with moderate hepatic impairment should be started at a lower dose and closely monitored during dose titration. Pharmacokinetics of hydromorphone in severe hepatic impairment patients has not been studied. Further increase in Cand AUC of hydromorphone in this group is expected. As such, starting dose should be even more conservative. Use of oral liquid is recommended to adjust the dose . Renal Impairment After oral administration of hydromorphone at a single 4 mg dose ( 2 mg hydromorphone hydrochloride immediate release tablets), exposure to hydromorphone ( Cand AUC) is increased in patients with impaired renal function by 2-fold in moderate (CLcr = 40 - 60 mL/min) and 3-fold in severe (CLcr<30 mL/min) renal impairment compared with normal subjects (CLcr>80 mL/min). In addition, in patients with severe renal impairment hydromorphone appeared to be more slowly eliminated with longer terminal elimination half-life (40 hr) compared to patients with normal renal function (15 hr). Patients with moderate renal impairment should be started on a lower dose. Starting doses for patients with severe renal impairment should be even lower. Patients with renal impairment should be closely monitored during dose titration. Use of oral liquid is recommended to adjust the dose . Pediatrics Pharmacokinetics of hydromorphone have not been evaluated in children. Geriatric Age has no effect on the pharmacokinetics of hydromorphone. Gender Gender has little effect on the pharmacokinetics of hydromorphone. Females appear to have higher C(25%) than males with comparable AUCvalues. The difference observed in Cmay not be clinically relevant. Pregnancy and nursing mothers Hydromorphone crosses the placenta. Hydromorphone is also found in low levels in breast milk, and my cause respiratory compromise in newborns when administered during labor and delivery.
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Hydromorphone hydrochloride tablets, USP, for oral administration, are supplied as follows: 2 mg: Round, flat face, beveled-edge blue tablet, debossed���E���on one side and���2���on the other side.100 Count Bottle������������������������������..NDC 58177-620-041000 Count Bottle������������������������������NDC 58177-620-09100 Count Unit Dose Packs������������������.NDC 58177-620-11 4 mg: Round, flat face, beveled-edge tan tablet, debossed���E���on one side and���4���on the other side.100 Count Bottles������������������������������NDC 58177-621-041000 Count Bottles���������������������������.NDC 58177-621-09100 Count Unit Dose Packs������������������NDC 58177-621-11 8 mg: Round, flat face, beveled-edge white tablet, debossed���E���on one side and���8���through partial bisect on the other side.100 Count Bottle������������������������������..NDC 58177-449-041000 Count Bottle������������������������������NDC 58177-449-09100 Count Unit Dose Packs������������������NDC 58177-449-11
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Hydromorphone Hydrochloride
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Hydromorphone Hydrochloride (Tablet)
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The major hazards of hydromorphone hydrochloride tablets include respiratory depression and apnea. To a lesser degree, circulatory depression, respiratory arrest, shock and cardiac arrest have occurred. The most frequently observed adverse effects are light-headedness, dizziness, sedation, nausea, vomiting, sweating, flushing, dysphoria, euphoria, dry mouth, and pruritus. These effects seem to be more prominent in ambulatory patients and in those not experiencing severe pain.<br/>Less Frequently Observed with Opioid Analgesics:<br/>General and CNS: Weakness, headache, agitation, tremor, uncoordinated muscle movements, alterations of mood (nervousness, apprehension, depression, floating feelings, dreams), muscle rigidity, paresthesia, muscle tremor, blurred vision, nystagmus, diplopia and miosis, transient hallucinations and disorientation, visual disturbances, insomnia, increased intracranial<br/>Cardiovascular: Flushing of the face, chills, tachycardia, bradycardia, palpitation, faintness, syncope, hypotension, hypertension<br/>Respiratory: Bronchospasm and laryngospasm<br/>Gastrointestinal: Constipation, biliary tract spasm, ileus, anorexia, diarrhea, cramps, taste alteration<br/>Genitourinary: Urinary retention or hesitancy, antidiuretic<br/>Dermatologic: Urticaria, other skin rashes, diaphoresis.
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Hydromorphone hydrochloride tablets are indicated for the management of pain in patients where an opioid analgesic is appropriate.
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Hydromorphone Hydrochloride
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