nal-TREX-one

Therapeutic Classification: alcohol abuse therapy adjuncts

Pharmacologic Classification: opioid antagonists

• Management of opioid dependence.
• Management of alcohol dependence.

• Competitively blocks the effects of opioids, including CNS and respiratory depression, without producing any agonist (opioid-like) effects.
• Mechanism in managing alcohol dependence may involve the endogenous opioid system.

• Blocks the effects of opioids in previously dependent patients.
• Reduced alcohol-dependent behavior.

Absorption: Well absorbed orally, but undergoes extensive first pass hepatic metabolism resulting in 5–40% bioavailability. Well absorbed following IM administration.

Distribution: Enters breast milk.

Metabolism/Excretion: Extensively metabolized by the liver. Major metabolite (6–beta-naltrexol) has opioid antagonist activity. Metabolites are excreted in urine.

Half-life: Oral: Naltrexone — 4 hr; 6–beta-naltrexol — 13 hr; IM: Naltrexone — 5–10 days; 6–beta-naltrexol — 5–10 days.

(opioid blockade)

†Determined by blockade of effects of 25 mg heroin IV.

Contraindicated in:

• Hypersensitivity
• Concurrent use of opioid analgesics or physiologic opioid dependence
• Acute opioid withdrawal
• Positive urine screen for opioids
• Failure of a naloxone challenge test

Use Cautiously in:

• History of hepatic impairment/damage
• Moderate to severe renal impairment
• History of depression or suicidal behavior/attempt
• OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk
• Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant
• Pedi: Safety and effectiveness not established in children.

CV: palpitations.

Derm: skin rash.

EENT: hoarseness, runny/stuffy nose, sinus problems, sneezing.

GI: HEPATOTOXICITY, abdominal cramps/pain, nausea, constipation, ↓ appetite, diarrhea, vomiting.

GU: delayed ejaculation, erectile dysfunction.

Hemat: eosinophilia, thrombocytopenia.

Local: injection site reactions.

MS: muscle/joint pain.

Neuro: SUICIDAL IDEATION, anxiety, fatigue, headache, insomnia, nervousness, depression, dizziness, ↑ energy, sedation.

Resp: EOSINOPHILIC PNEUMONIA (INJECTION), cough.

Misc: chills, ↑ thirst.

Drug-Drug:

• Concurrent use with thioridazine may ↑ CNS depression.
• May prevent therapeutic effects of opioid analgesics, antidiarrheals, and antitussives.

Opioid Dependence

• PO (Adults): Following a negative naloxone challenge and 7–10 days of opioid abstinence (longer for methadone), initial dose is 25 mg. If opioid withdrawal does not occur within 1 hr, additional 25 may be given. Maintenance dose is 50 mg daily as a single dose or 50 mg once daily on weekdays and 100 mg on Saturday or 100 mg every other day or 150 mg every third day or 100 mg on Monday and Wednesday and 150 mg on Friday.
• IM (Adults): 380 mg every 4 wk or once monthly.

Alcohol Dependence

• PO (Adults): 50 mg daily as a single dose or 50 mg once daily on weekdays and 100 mg on Saturday or 100 mg every other day or 150 mg every third day or 100 mg on Monday and Wednesday and 150 mg on Friday.
• IM (Adults): 380 mg every 4 wk or once monthly.

(Generic available)

• Tablets: 50 mg;
• Suspension for injection: 380 mg/vial;

• Assess patient for last time opioids or alcohol were taken. Patient must be free from opioids for 7–10 days prior to initiation of therapy. Naltrexone does not eliminate withdrawal symptoms (anxiety, sleeplessness, yawning, fever, sweating, teary eyes, runny nose, goose bumps, shakiness, hot or cold flushes, muscle aches, muscle twitches, restlessness, nausea and vomiting, diarrhea, stomach cramps). If physical dependence on opioids is possible, a Naloxone Challenge Test should be used. Patients transitioning from buprenorphine, buprenorphine/naloxone, or methadone are also at risk for developing withdrawal symptoms.
• Monitor closely for changes in behavior that could indicate the emergence or worsening of suicidal thoughts or behavior or depression.
• Assess for signs of eosinophilic pneumonia (dyspnea, hypoxia, coughing, wheezing). Advise patient to seek treatment immediately if these symptoms occur.

• May cause ↑ liver enzymes; monitor periodically during therapy.
  • May cause ↑ eosinophil and ↓ platelet counts.

• Naltrexone should be used in conjunction with a comprehensive alcohol or drug program. Patient should not be actively drinking at the time of naltrexone initiation.
  • If emergent analgesia is required for pain management, regional analgesia, conscious sedation with a benzodiazepine, and use of non-opioid analgesics or general anesthesia are recommended. If opioid analgesics are required, the amount may be greater than usual and the respiratory depression deeper and more prolonged. A rapidly acting opioid that minimizes the duration of respiratory depression is recommended.
• PO: Administer as directed. A number of dose schedules have been used.
• IM: Must be administered by a health care professional every 4 wk or once a mo. Suspend using only diluent and needle supplied. A spare administration needle is provide in case of clogging. Do not substitute other components. Allow drug to reach room temperature, approximately 45 min, before preparing. To ease mixing, firmly tap vial on a hard surface, ensuring powder moves freely. Using the 1/2 inch preparation needle, withdraw 3.4 mL of clear diluent and inject into microsphere vial. Mix by shaking vigorously for approximately 1 min. Suspension is milky white without clumps and moving freely up and down the wall of the vial. Immediately after suspension, withdraw 4.2 mL of suspension using same preparation needle. Remove preparation needle and replace with 1 1/2 or 2 inch administration needle for immediate use. Prior to administration, tap syringe to release any bubbles, then gently push plunger until 4 mL of suspension remains in syringe. Activate safety sheath by pressing against hard surface to cover needle. Store in refrigerator, do not freeze; may be kept at room temperature for 7 days.
  • Administer IM into the gluteal muscle using pre-packaged 1 1/2- or 2–inch needle specifically designed for this drug. Avoid IV subcut or administration into fatty tissue.
  • If a dose is missed, patient should receive dose as soon as possible.

• Instruct patient to take naltrexone as directed. Inform patients that there are potentially serious consequences and possibly death if they try to overcome the effects of naltrexone with higher doses of opioids.
• May cause dizziness. Advise patient to avoid driving and other activities requiring alertness until effects of the medication are known.
• Encourage patient and family to be alert for emergence of anxiety, agitation, panic attacks, insomnia, irritability, hostility, impulsivity, akathisia, hypomania, mania, worsening of depression and suicidal ideation, especially during early antidepressant therapy. Assess symptoms on a day-to-day basis as changes may be abrupt. If these symptoms occur, notify health care professional.
• Inform patient of the risk of hepatic injury. Advise patient to notify health care professional if signs of acute hepatitis (abdominal pain lasting more than a few days, white bowel movements, dark urine, or yellowing of eyes) occur; naltrexone should be discontinued.
• Advise patient and family that patient may be more sensitive to lower doses of opioids after naltrexone treatment stops, when next dose is due, and if a dose is missed. Advise patients that they will not perceive any effects of small doses of opioids and may not experience the same effects from opioid-containing analgesics, antidiarrheals, or antitussives. May lead to overdose including serious injury, coma, or death.
• Educate patients and caregivers on how to recognize respiratory depression and emphasize the importance of calling 911 or getting emergency medical help right away in the event of a known or suspected overdose. Inform patients and caregivers about various ways to obtain naloxone as permitted by individual state naloxone dispensing and prescribing requirements or guidelines (by prescription, directly from a pharmacist, or as part of a community-based program).
• Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.
• Advise patient to carry identification to alert medical personnel of naltrexone therapy.
• IM: May cause injection site reactions (cellulitis, induration, hematoma, abscess, sterile abscess, necrosis). Advise patient to monitor injection site and notify health care professional if pain, swelling, tenderness, induration, bruising, pruritus or redness at the injection site occurs and does not improve or worsens within 2 wk. Promptly refer patients with worsening injection site reactions to a surgeon.

• The blockade of the effects of exogenously administered opioids.
• Management of alcoholism.

naltrexone (Injection): Vivitrol

ReVia

NDC Code^*

• 0406- SpecGx LLC
  • 0406-1170- NALTREXONE HYDROCHLORIDE
    • 0406-1170-01- 100 TABLET, FILM COATED in 1 BOTTLE (0406-1170-01)

• 0406- SpecGx LLC
  • 0406-1170- NALTREXONE HYDROCHLORIDE
    • 0406-1170-03- 30 TABLET, FILM COATED in 1 BOTTLE (0406-1170-03)

• 16729- Accord Healthcare, Inc.
  • 16729-081- Naltrexone Hydrochloride
    • 16729-081-01- 100 TABLET, FILM COATED in 1 BOTTLE (16729-081-01)

• 16729- Accord Healthcare, Inc.
  • 16729-081- Naltrexone Hydrochloride
    • 16729-081-10- 30 TABLET, FILM COATED in 1 BOTTLE (16729-081-10)

• 42291- AvKARE, Inc.
  • 42291-632- Naltrexone Hydrochloride
    • 42291-632-30- 30 TABLET, FILM COATED in 1 BOTTLE (42291-632-30)

• 47335- Sun Pharmaceutical Industries, Inc.
  • 47335-326- NALTREXONE HYDROCHLORIDE
    • 47335-326-08- 100 TABLET, FILM COATED in 1 BOTTLE (47335-326-08)

• 47335- Sun Pharmaceutical Industries, Inc.
  • 47335-326- NALTREXONE HYDROCHLORIDE
    • 47335-326-18- 1000 TABLET, FILM COATED in 1 BOTTLE (47335-326-18)

• 47335- Sun Pharmaceutical Industries, Inc.
  • 47335-326- NALTREXONE HYDROCHLORIDE
    • 47335-326-83- 30 TABLET, FILM COATED in 1 BOTTLE (47335-326-83)

• 47335- Sun Pharmaceutical Industries, Inc.
  • 47335-326- NALTREXONE HYDROCHLORIDE
    • 47335-326-88- 100 TABLET, FILM COATED in 1 BOTTLE (47335-326-88)

• 50090- A-S Medication Solutions
  • 50090-2866- Naltrexone Hydrochloride
    • 50090-2866-0- 30 TABLET, FILM COATED in 1 BOTTLE (50090-2866-0)

• 50090- A-S Medication Solutions
  • 50090-3929- NALTREXONE HYDROCHLORIDE
    • 50090-3929-0- 30 TABLET, FILM COATED in 1 BOTTLE (50090-3929-0)

• 51224- TAGI Pharma Inc.
  • 51224-206- Naltrexone Hydrochloride
    • 51224-206-30- 30 TABLET, FILM COATED in 1 BOTTLE (51224-206-30)

• 51224- TAGI Pharma Inc.
  • 51224-206- Naltrexone Hydrochloride
    • 51224-206-50- 100 TABLET, FILM COATED in 1 BOTTLE (51224-206-50)

• 53217- Aidarex Pharmaceuticals LLC
  • 53217-261- Naltrexone Hydrochloride
    • 53217-261-30- 30 TABLET, FILM COATED in 1 BOTTLE (53217-261-30)

• 63629- Bryant Ranch Prepack
  • 63629-1046- Naltrexone Hydrochloride
    • 63629-1046-1- 30 TABLET, FILM COATED in 1 BOTTLE (63629-1046-1)

• 63629- Bryant Ranch Prepack
  • 63629-1047- Naltrexone Hydrochloride
    • 63629-1047-1- 100 TABLET, FILM COATED in 1 BOTTLE (63629-1047-1)

• 65757- Alkermes, Inc.
  • 65757-300- VIVITROL
    • 65757-300-01- 1 KIT in 1 CARTON (65757-300-01) * 4 mL in 1 VIAL, GLASS (65757-302-02) * 4 mL in 1 VIAL, GLASS (65757-304-03)

• 68071- NuCare Pharmaceuticls, Inc.
  • 68071-2156- Naltrexone Hydrochloride
    • 68071-2156-3- 30 TABLET, FILM COATED in 1 BOTTLE (68071-2156-3)

• 68084- American Health Packaging
  • 68084-291- NALTREXONE HYDROCHLORIDE
    • 68084-291-21- 30 BLISTER PACK in 1 BOX, UNIT-DOSE (68084-291-21) > 1 TABLET, FILM COATED in 1 BLISTER PACK (68084-291-11)

• 68094- Precision Dose Inc.
  • 68094-853- Naltrexone Hydrochloride
    • 68094-853-62- 3 BLISTER PACK in 1 CARTON (68094-853-62) > 10 TABLET, FILM COATED in 1 BLISTER PACK

• 68788- Preferred Pharmaceuticals Inc.
  • 68788-7084- Naltrexone Hydrochloride
    • 68788-7084-1- 100 TABLET, FILM COATED in 1 BOTTLE (68788-7084-1)

• 68788- Preferred Pharmaceuticals Inc.
  • 68788-7084- Naltrexone Hydrochloride
    • 68788-7084-2- 20 TABLET, FILM COATED in 1 BOTTLE (68788-7084-2)

• 68788- Preferred Pharmaceuticals Inc.
  • 68788-7084- Naltrexone Hydrochloride
    • 68788-7084-3- 30 TABLET, FILM COATED in 1 BOTTLE (68788-7084-3)

• 68788- Preferred Pharmaceuticals Inc.
  • 68788-7084- Naltrexone Hydrochloride
    • 68788-7084-6- 60 TABLET, FILM COATED in 1 BOTTLE (68788-7084-6)

• 68788- Preferred Pharmaceuticals Inc.
  • 68788-7084- Naltrexone Hydrochloride
    • 68788-7084-9- 90 TABLET, FILM COATED in 1 BOTTLE (68788-7084-9)

• 69364- Complete Pharmacy and Medical Solutions
  • 69364-3143- Naltrexone
    • 69364-3143-6- 6 BLISTER PACK in 1 BOX (69364-3143-6) > 1 IMPLANT in 1 BLISTER PACK

• 70518- REMEDYREPACK INC.
  • 70518-1146- Naltrexone Hydrochloride
    • 70518-1146-0- 30 TABLET, FILM COATED in 1 BLISTER PACK (70518-1146-0)

• 70518- REMEDYREPACK INC.
  • 70518-1312- NALTREXONE HYDROCHLORIDE
    • 70518-1312-0- 30 TABLET, FILM COATED in 1 BLISTER PACK (70518-1312-0)

• 71335- Bryant Ranch Prepack
  • 71335-0014- Naltrexone Hydrochloride
    • 71335-0014-1- 30 TABLET, FILM COATED in 1 BOTTLE (71335-0014-1)

• 71335- Bryant Ranch Prepack
  • 71335-0014- Naltrexone Hydrochloride
    • 71335-0014-2- 90 TABLET, FILM COATED in 1 BOTTLE (71335-0014-2)

• 71335- Bryant Ranch Prepack
  • 71335-0014- Naltrexone Hydrochloride
    • 71335-0014-3- 60 TABLET, FILM COATED in 1 BOTTLE (71335-0014-3)

• 71335- Bryant Ranch Prepack
  • 71335-0014- Naltrexone Hydrochloride
    • 71335-0014-4- 45 TABLET, FILM COATED in 1 BOTTLE (71335-0014-4)

• 71335- Bryant Ranch Prepack
  • 71335-0014- Naltrexone Hydrochloride
    • 71335-0014-5- 120 TABLET, FILM COATED in 1 BOTTLE (71335-0014-5)

• 71335- Bryant Ranch Prepack
  • 71335-0014- Naltrexone Hydrochloride
    • 71335-0014-6- 15 TABLET, FILM COATED in 1 BOTTLE (71335-0014-6)

• 76519- H.J. Harkins Company Inc.
  • 76519-1160- NALTREXONE HYDROCHLORIDE
    • 76519-1160-5- 15 TABLET, FILM COATED in 1 CONTAINER (76519-1160-5)