What is Naltrexone?
Naltrexone is an active ingredient used for treatment of alcoholism and dehabituation to opiates. The product ingredient is Naltrexone hydrochloride (hcl).
The brand names of Naltrexone in United States are: Vivitrol, Revia, Depade.
Naltrexone Mechanism of Action (MOA)
An opioid antagonist that acts by specific competition with the receptors located in the CNS and peripheral, antagonizing the actions of opiates of exogenous administration.
Therapeutic indications, uses and benefits of Naltrexone
Alcoholism, opiate withdrawal accompanied by other therapeutic measures.
Dosage of Naltrexone
ORAL: Naltrexone 50 mg/1 Tablet
Adults:
A period of 7-10 days of abstinence from narcotic drugs should elapse before starting treatment (verified by urinalysis).
– Alcoholism: 50 mg/day, 3 months (longer periods may be necessary).
– Dehabituation to opiates: before starting to test naloxone.
Induction therapy: 25 mg, at an hour if there are no signs of abstinence another 25 mg: from the second day to complete the week 50 mg/day.
Maintenance therapy: 350 mg/week 2 options:
- First option: 50 mg/day.
- Second option: 2 doses of 50 mg on Mondays and Wednesdays and 3 doses on Fridays.
Do not exceed 150 mg/day.
Children and the elderly have not established efficacy and safety.
Method of administration
Oral use.
Administer preferably with meals.
Contraindications of Naltrexone
Hypersensitivity, severe renal and hepatic insufficiency, acute hepatitis, current dependence on opiates, concomitant with opiates, control + to opiates or not passing the naloxone test.
Warnings and Precautions with Naltrexone
- Liver and/or kidney failure.
- Liver tests at the beginning and periodically during treatment.
- In opiate addicts a withdrawal syndrome may be triggered.
- Warn the patient that high doses to cancel the blockage can cause acute poisoning, possibly fatal.
- Opioids (e.g. opiates in cough preparations, for the symptomatic treatment of colds or in antidiarrheal preparations) should not be used during treatment with this active ingredient.
- In emergency situations where opioid analgesics need to be administered to subjects on naltrexone treatment, the dose of opioid analgesics may be higher than usual, and the resulting respiratory depression may be deeper and longer, requiring adequate monitoring by trained personnel and in a hospital.
- Children and adolescents < 18 years, not recommended.
- Elderly, safe use for the treatment of opiate dependence in elderly patients has not been established.
Liver failure
Contraindicated with severe liver failure, acute hepatitis. Caution with hepatic insufficiency, at the beginning and periodically during treatment perform liver tests.
Renal insufficiency
Contraindicated with severe renal failure.
Caution with renal insufficiency.
Interactions with Naltrexone
- Association not recommended: opioid agonist analgesics, opioid agonist-antagonist analgesics and opioids in substitution treatment.
- Association to be considered: barbiturates and benzodiazepines.
- Drowsiness and lethargy have been reported after administration of naltrexone and thioridazine.
- In data from a safety and tolerability study of co-administration of naltrexone with acamprosate, administration of naltrexone was observed to significantly increase plasma levels of acamprosate in alcohol-dependent individuals. Interaction with other psychotropic drugs (e.g. disulfiram, amitriptyline, doxepin, lithium, clozapine, benzodiazepines) has not been investigated.
Pregnancy and Naltrexone
Animal studies have shown reproductive toxicity.
The potential risk in humans is unknown.
It will only be administered when, in medical judgment, the potential benefits outweigh the possible risks.
Breastfeeding
It is not known whether naltrexone or 6-beta-naltrexol are excreted in breast milk.
Breastfeeding is not recommended during treatment.
Effects on driving ability
The influence of naltrexone on the ability to drive and use machines is small or moderate.
Adverse reactions and side effects of Naltrexone
Headache, sleep disorder, restlessness, nervousness, abdominal pain, abdominal cramps.
Nausea, tendency to vomit, muscle and joint pain, weakness, thirst, dizziness, chills, increased perspiration, vertigo.
Increased tearing, chest pain, diarrhea, constipation, urine retention, rash.
Loss of appetite, delayed ejaculation, decreased sexual potency, anxiety.
Increased energy level, depression, irritability, mood swings.
⭐⭐⭐⭐⭐ VIDEO OF NALTREXONE/REVIA, VIVITROL, DEPADE (DRUG)
Source: The content of this active ingredient has been written taking into account the clinical and molecular information of all medicines authorised and marketed in the United States under the Unique Ingredient Identifier (UNII) by the Substance Registration System (SRS) of the Food and Drug Administration (FDA) and the United States Pharmacopeia (USP).
In order to know in detail the information authorized by the FDA for each drug, you should consult the corresponding medication guide authorized by the FDA.
Resources:
UNII: 5S6W795CQM
ChemIDplus
DrugPortal
PubChem CID:5360515
NCI Thesaurus: C62055