【缺藥訊息】 公告日期：2024/10/11。 缺藥品項：Notholic 錠 缺藥原因：原料短缺。 配套措施：用罄關檔停用，本品預計12月底恢復供貨。

Alcohol use disorder, Opioid use disorder

Opioid Antagonist
Naltrexone (a pure opioid antagonist) is a cyclopropyl derivative of oxymorphone similar in structure to naloxone and nalorphine (a morphine derivative); it acts as a competitive antagonist at opioid receptor sites, showing the highest affinity for mu receptors.

1.Absorption: Oral: Almost complete
2.Distribution: Vd: ~1350 L; widely throughout the body but considerable interindividual variation exists
3.Metabolism: Extensively metabolized via noncytochrome-mediated dehydrogenase conversion to 6-beta-naltrexol (primary metabolite) and related minor metabolites; glucuronide conjugates are also formed from naltrexone and its metabolites
4.Protein binding: 21%
5.Excretion: Primarily urine (as metabolites and small amounts of unchanged drug)

Hypersensitivity to naltrexone or any component of the formulation; current physiological opioid dependence or current use of opioid analgesics (including partial opioid agonists); acute opioid withdrawal; failure to pass naloxone challenge or positive urine screen for opioids.

Information related to the use of naltrexone for the treatment of opioid use disorder during pregnancy is limited.

Naltrexone and the 6-beta-naltrexol metabolite are present in breast milk. The decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother.

1.Cardiovascular: Syncope ((13%)
2.Gastrointestinal: Abdominal pain (11%), anorexia ((14%), change in appetite ((14%), decreased appetite ((14%), diarrhea (13%), nausea (33%), vomiting (14%)
3.Hepatic: Increased serum aspartate aminotransferase (2% to 14%) (table 1), increased serum transaminases (20%)
4.Local: Induration at injection site (35%) (table 3), injection-site reaction (69%, including injection-site nodule and swelling at injection site) (table 4), pain at injection site (17%) (table 5), tenderness at injection site (45%)
5.Nervous system: Anxiety (12%), asthenia (23%), dizziness ((13%), headache (25%), insomnia ((14%), sleep disorder ((14%)
6.Neuromuscular & skeletal: Arthralgia ((12%), arthritis ((12%), increased creatine phosphokinase in blood specimen (11% to 39%), joint stiffness ((12%)
7.Respiratory: Pharyngitis (11%)

Alcohol use disorder, moderate to severe
Oral: 50 mg once daily; may increase to 100 mg once daily after 1 week based on response and tolerability. Some experts initiate with 25 mg once daily for several days before increasing to 50 mg once daily.,
Opioid use disorder, mild to severe
Oral (alternative route): Initial: 25 mg once daily for 1 to 3 days; if no withdrawal signs occur, administer 50 mg once daily thereafter.

1.Mild impairment: No dosage adjustment necessary.
2.Moderate-to-severe impairment: No dosage adjustment provided in manufacturer's labeling (has not been studied); use with caution since naltrexone and its primary metabolite are primarily excreted in urine.

1.Mild to moderate impairment: No dosage adjustment necessary.
2.Severe impairment: No dosage adjustment provided in manufacturer's labeling; naltrexone AUC increased ~5- and 10-fold in patients with compensated or decompensated hepatic cirrhosis respectively. Use is not recommended in acute hepatitis or hepatic failure.