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  1. 1. DRUG INFORMATION ON ZOHYDRO ER GENERIC NAME:Hydrocodone Bitartrate Extended relese Capsule BRAND NAME: ZOHYDRO ER APPROVED DATE: 25 October 2013 MARKETED COMPANY: Zogenixinc., INDICATION:Chronic pain management MECHANISM OF ACTION: Hydrocodone is a semi-synthetic opioid agonist with relative selectivity for the mu-opioid receptor, although it can interact with other opioid receptors at higher doses. Hydrocodone acts as a full agonist, binding to and activating opioid receptors at sites in the peri-aquaductal and peri-ventricular gray matter, the ventro-medial medulla and the spinal cord to produce analgesia. The analgesia, as well as the euphorant, respiratory depressant and physiologic dependence properties of μ agonist opioids like hydrocodone, result principally from agonist action at the μ receptors PHARMACOKINETICS : Absorption Zohydro ER capsules exhibit peak plasma concentrations occurring approximately 5 hours after dose administration was administered with a high-fat meal. Distribution Although the extent of protein binding of hydrocodone in human plasma has not been definitely determined, structural similarities to related opioid analgesics suggest that hydrocodone is not extensively protein bound. As most agents in the 5-ring morphinangroup of semi-synthetic opioids bind plasma protein to a similar degree range 19% [hydromorphone]to 45% [oxycodone]), hydrocodone is expected to fall within this range. Metabolism Hydrocodone exhibits a complex pattern of metabolism, including N-demethylation, Odemethylation, and 6-keto reduction to the corresponding 6-α-and 6-β-hydroxy metabolites. CYP3A4 mediated N-demethylation to norhydrocodone is the primary metabolic pathway of hydrocodone with a lower contribution from CYP2D6 mediated Odemethylation to hydromorphone. Hydromorphone is formed from the O-demethylation of hydrocodone and may contribute to the total analgesic effect of hydrocodone. Excretion Hydrocodone and its metabolites are eliminated primarily in the kidneys, with a mean
  2. 2. apparent plasma half-life after Zohydro ER administration of approximately 8 hours. PHARMACODYNAMICS: Central Nervous System The principal therapeutic action of hydrocodone is analgesia. In common with other opioids, hydrocodone causes respiratory depression, in part by a direct effect on the brainstem respiratory centers. The respiratory depression involves a reduction in the responsiveness of the brain stem respiratory centers to both increases in carbon dioxide tension and electrical stimulation. Opioids depress the cough reflex by direct effect on the cough center in the medulla. Hydrocodone causes miosis, even in total darkness. Pinpoint pupils are a sign of opioid overdose but are not pathognomonic. Gastrointestinal Tract and Other Smooth Muscle Hydrocodone 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. Cardiovascular System Hydrocodone may produce release of histamine with or without associated peripheral vasodilation. Manifestations of histamine release and/or peripheral vasodilation may include pruritus, flushing, red eyes, sweating, and/or orthostatic hypotension. DOSE: The recommended dose is a 200 mg subcutaneous injection at Week 0, followed by 100 mg at Week 2 and then maintenance therapy with 100 mg every 4 weeks. DOSAGE FORM: Extended Relese Capsule CONTRAINDICATION: respiratory depression acute or severe bronchial asthma or hypercarbia paralytic ileus hypersensitivity to any components of Zohydro ER or the active ingredient, hydrocodone bitartrate
  3. 3. ADVERSE DRUG REACTION: Constipation Nausea Somnolence Fatigue Headache Dizziness Dry m outh Vomiting Pruritus Abdominal pain Edema peripheral Upper respiratory tract infection Muscle spasms Urinary tract infection Back pain and tremor. DRUG -DRUG INTERACTION: CNS depressants: Increased risk of respiratory depression, hypotension, profound sedation, coma or death. When combined therapy with CNS depressant is contemplated, the dose of one or both agents should be reduced Mixed Agonists/Antagonists: May precipitate withdrawal or decrease analgesic effect if given concurrently with Zohydro ER. The use of MAO inhibitors or tricyclic antidepressants with Zohydro ER may increase the effect of either the antidepressant or Zohydro ER. WARNING& PRECAUTION: Misuse, abuse, and diversion: Zohydro ER is an opioid agonist and a Schedule II controlled substance with a high potential for abuse similar to fentanyl, methadone, morphine, oxycodone, and oxymorphone. Interactions with CNS depressants: Concomitant use may cause profound sedation, respiratory depression, and death. If coadministration is required, consider dose reduction of one or both drugs. Elderly, cachectic, debilitated patients, and those with chronic pulmonary disease: Monitor closely because of increased risk for life-threatening respiratory depression. Patients with head injury or increased intracranial pressure: Monitor for sedation and respiratory depression. Avoid use of Zohydro ER in patients with impaired consciousness or coma susceptible to intracranial effects of CO2 retention. Prolonged gastric obstruction: May occur in patients with gastrointestinal obstruction.
  4. 4. Concomitant use of CYP3A4 inhibitors may increase opioid effects. Impaired mental/physical abilities: Caution must be used with potentially hazardous activities. STORAGE: Store at 25° C (77° F); excursions permitted to 15°–30° C (59°–86° F) REFERENCE: FDA APPROVED DRUG 2013 WWW.RxLIST.COM WWW.DRUGS.COM