Conzip

— THERAPEUTIC CATEGORIES —
  • Narcotic analgesics
PAGE CONTENTS
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  • Generic Name & Formulations
  • Indications
  • Dosage and Administration
  • Contraindications
  • Boxed Warnings
  • Warnings/Precautions
  • Pharmacokinetics
  • Interactions
  • Adverse Reactions
  • Clinical Trials
  • Note
  • Patient Counseling

    • Conzip Generic Name & Formulations

    Legal Class

    CIV

    General Description

    Tramadol HCl 100mg, 200mg, 300mg; ext-rel caps.

    Pharmacological Class

    Opioid agonist.

    How Supplied

    Ext-rel caps—30

    Manufacturer

    Vertical Pharmaceuticals

    Generic Availability

    NO

    Mechanism of Action

    Tramadol is an opioid agonist and an inhibitor of reuptake of norepinephrine and serotonin. Although its mode of action is not completely understood, from animal tests, at least two complementary mechanisms appear applicable: binding of parent and M1 metabolite to µ-opioid receptors and weak inhibition of reuptake of norepinephrine and serotonin.

    Conzip Indications

    Indications

    Management of severe and persistent pain that requires an extended treatment period with a daily opioid analgesic and for which alternative treatment options are inadequate.

    Limitations of Use

    Due to risks of addiction, abuse, and misuse with opioids (can occur at any dosage or duration); increased risks of overdose and death with extended-release/long-acting opioid formulations, reserve for use in patients for whom alternative treatment options are ineffective, not tolerated, or otherwise inadequate to provide sufficient management of pain. 

    Conzip Dosage and Administration

    Adult

    Use lowest effective dose for shortest duration. Swallow whole. Take once daily with liquid; allow 24hrs in between doses. ≥18yrs: Not currently on tramadol: initially 100mg once daily; titrate up as needed by 100mg increments every 5 days. Currently on immediate-release tramadol: switch to ext-rel at total daily dose rounded down to nearest 100mg increment. Max 300mg/day. Elderly: titrate slowly; monitor. Conversion from other opioids: see full labeling. Concomitant use or discontinuation of CYP2D6 inhibitors, CYP3A4 inhibitors or inducers: monitor closely and consider dose adjustments (see full labeling). Withdraw gradually (esp. if opioid-dependent), taper by ≤10–25% every 2–4 weeks.

    Children

    <18yrs: not recommended.

    Conzip Contraindications

    Contraindications

    Children <12yrs. Post-op management in children <18yrs following tonsillectomy and/or adenoidectomy. Significant respiratory depression. Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment. Known or suspected GI obstruction, including paralytic ileus. During or within 14 days of MAOIs.

    Conzip Boxed Warnings

    Boxed Warning

    Serious and life-threatening risks from use of Conzip: Addiction, abuse, and misuse; Life-threatening respiratory depression; Accidental ingestion; Risks from concomitant use with benzodiazepines or other CNS depressants; Neonatal opioid withdrawal syndrome; Opioid analgesic risk evaluation and mitigation strategy (REMS); Ultra-rapid metabolism of tramadol and other risk factors for life-threatening respiratory depression in children; Interactions with drugs affecting CYP450 isoenzymes.

    Conzip Warnings/Precautions

    Warnings/Precautions

    Assess the potential need for access to naloxone when initiating and renewing therapy. Consider prescribing naloxone based on risk factors for overdose (eg, history of opioid use disorder, prior opioid overdose, household members or other close contacts at risk for accidental ingestion or overdose). Abuse potential (monitor). Life-threatening respiratory depression; monitor during initiation or following a dose increase. Accidental exposure may cause fatal overdose (esp. in children). Opioid-induced hyperalgesia (OIH) and allodynia; consider decreasing dose of current opioid or opioid rotation if OIH is suspected. Sleep-related breathing disorders (including central sleep apnea (CSA), sleep-related hypoxemia); consider dose reduction if CSA develops. Risk of life-threatening respiratory depression and death related to ultra-rapid metabolizers of tramadol (esp. in children for post-tonsillectomy and/or adenoidectomy pain). Avoid in adolescents 12–18yrs with conditions associated with hypoventilation (eg, post-op status, obstructive sleep apnea, obesity, severe pulmonary disease, neuromuscular disease, concomitant drugs that cause respiratory depression). COPD, cor pulmonale, decreased respiratory reserve, hypoxia, hypercapnia, or pre-existing respiratory depression; monitor and consider non-opioid analgesics. Adrenal insufficiency. Monitor for signs of hypotension when initiating or titrating dose. Head injury. Increased intracranial pressure, brain tumors; monitor. Seizure disorders. Avoid in depressed, suicidal, or addiction-prone patients; consider non-narcotic analgesics. Emotional disturbance. CNS depression. Impaired consciousness, coma, shock; avoid. Biliary tract disease. Acute pancreatitis. Hyponatremia. Hypoglycemia. Diabetes. Drug abusers. Severe hepatic (Child-Pugh Class C) or renal impairment (CrCl<30mL/min): not recommended. Ultra-rapid metabolizers (due to CYP2D6 polymorphism): avoid. Reevaluate periodically. Avoid abrupt cessation. Elderly (esp. >75yrs). Cachectic. Debilitated. Pregnancy; potential neonatal opioid withdrawal syndrome during prolonged use. Labor & delivery, nursing mothers: not recommended.

    REMS

    YES

    Conzip Pharmacokinetics

    Absorption

    Time to maximum plasma concentration: 10–12 hours. Mean maximum plasma concentration (after a 300mg single dose under fasting conditions): 308 ng/mL.

    Distribution

    Volume of distribution: 2.6 L/kg (males); 2.9 L/kg (females). Plasma protein bound: ~20%.

    Metabolism

    Hepatic (CYP3A4, CYP2D6).

    Elimination

    Renal (~30%). Half-life: ~10 hours (racemic tramadol).

    Conzip Interactions

    Interactions

    Concomitant other forms of tramadol or carbamazepine: not recommended. Increased risk of hypotension, respiratory depression, sedation with benzodiazepines or other CNS depressants (eg, non-benzodiazepine sedatives/hypnotics, anxiolytics, general anesthetics, phenothiazines, tranquilizers, muscle relaxants, antipsychotics, alcohol, other opioids); reserve concomitant use in those for whom alternative options are inadequate; limit dosages/durations to minimum required; monitor closely; consider prescribing naloxone if concomitant use is warranted. Risk of serotonin syndrome with serotonergic drugs (eg, SSRIs, SNRIs, TCAs, triptans, 5-HT3 antagonists, mirtazapine, trazodone, tramadol, cyclobenzaprine, metaxalone, MAOIs, linezolid, IV methylene blue); monitor and discontinue if suspected. Increased risk of seizures with SSRIs, SNRIs, anorectics, TCAs, cyclobenzaprine, promethazine, other opioids, MAOIs, naloxone, neuroleptics, and others that lower seizure threshold. Avoid concomitant mixed agonist/antagonist opioids (eg, butorphanol, nalbuphine, pentazocine) or partial agonist (eg, buprenorphine); may reduce effects and/or precipitate withdrawal symptoms. May be affected by CYP2D6 inhibitors (eg, amiodarone, quinidine, fluoxetine, paroxetine, bupropion). Potentiated by CYP3A4 inhibitors (eg, macrolides, azole antifungals, protease inhibitors). May potentiate serum amylase. Antagonized by CYP3A4 inducers (eg, rifampin, carbamazepine, phenytoin). May antagonize diuretics; monitor. Paralytic ileus may occur with anticholinergics. Monitor digoxin, warfarin.

    Conzip Adverse Reactions

    Adverse Reactions

    Nausea, constipation, dry mouth, somnolence, dizziness, vomiting; respiratory depression, severe hypotension, syncope, anaphylaxis or other hypersensitivity reactions (permanently discontinue if occur), OIH and allodynia, possible infertility (long-term use).

    Conzip Clinical Trials

    See Literature

    Conzip Note

    Not Applicable

    Conzip Patient Counseling

    See Literature

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