NALTREXONE & TOPIRAMATE

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January 5, 2021

 

 

Naltrexone

Naltrexone is a medication used to treat Substance Use Disorders, primarily alcoholism and opioid abuse. The medication may be given daily by oral dosing (Brand Name: ReVia) or given monthly by intramuscular injection (Brand Name: Vivitrol). In some countries, subcutaneous implants are available as well. Naltrexone is metabolized in the liver and excreted from the body in the urine. Naltrexone and its active metabolite work by blocking (antagonizing) the various opioid receptors in the body. This blockade of opioid receptors have various effects including:
• lessening or blocking the effects of opiates (morphine, codeine) and opioids (heroin, Hydrocodone, Oxycodone, Fentanyl)
• blocking the effects of Dynorphin, an endorphin that lessens pain but also leads to drug/alcohol seeking behavior, learned helplessness, depression, and increased appetite.

Naltrexone has been shown useful primarily to decrease the cravings for:

• Alcohol
• Opiates
• opioids
• and other substances of abuse

Naltrexone also appears useful to decrease impulsive behaviors and such impulsive behaviors are often behind episodes of relapse. It also lessens the effects of opiates and opioids thus, not only lessening the reward of use, but possibly decreasing the risk of a catastrophic overdose.

Naltrexone therapy is recommended for at least one year; however, therapy should be individualized. Though it is unlikely that a patient would require less than one year of therapy; it is possible that a patient may require significantly longer. Factors that may influence length of Naltrexone therapy include, but are not limited to:
• strength of cravings
• history of impulsivity
• length of time abusing substances
• social supports
• mental health

Contraindications to Naltrexone Use

Naltrexone is considered a very safe medication in general and this is due to its very specific mechanism of action. The only absolute contraindications to the use of Naltrexone are allergy to it and severe liver failure. Relative contraindications to its use are severe hepatitis, liver cirrhosis, kidney failure and recent use of an opioid / opiate.

Possible Adverse Effects of Naltrexone:

• Liver Toxicity (rare)
• Depression
• Insomnia
• Nausea / Vomiting
• Anxiety
• Headache
• Fatigue / Sleepiness
• Rash
• Abdominal Pain (uncommon)
• Dizziness
• Change in Bowel Habits
• Less control of chronic pain

Topiramate

Topiramate is a medication used to treat Substance Use Disorders, primarily alcoholism and stimulant abuse. The medication is given by oral dosing. It was designed as and is used as an antiepileptic (anti-seizure) medicine; however, other uses such as for the treatment of substance abuse, Migraines, Bipolar Disorder, Borderline Personality Disorder (BPD), Post Traumatic Stress Disorder (PTSD), and some chronic pain syndromes have emerged. Topiramate is metabolized in the liver and excreted from the body in the urine.
Topiramate works by a fairly complex mechanisms of action. However, the sum of these mechanisms of action is to help improve regulation of nerve conduction. It is this regulation that leads to the various therapeutic effects of Topiramate. It is particularly important to note that the variety of conditions that Topiramate can treat make it especially effective in the therapy of Substance Use Disorders since they often may co-occur with Bipolar Disorders, BPD, PTSD and chronic pain.
The seizure prevention activity of Topiramate may also be of great use in preventing the convulsive disorders that may accompany alcohol withdrawal. Therefore, Topiramate may not only save a patient’s life by helping to treat their alcoholism; Topiramate may save a patient’s life by preventing alcohol withdrawal seizures and/or mitigating Delirium Tremens (DTs).

Topiramate therapy is recommended for at least one year; however, therapy should be individualized. Though it is unlikely that a patient would require less than one year of therapy; it is possible that a patient may require significantly longer. Factors that may influence length of Topiramate therapy include, but are not limited to:

• strength of cravings
• history of impulsivity
• length of time abusing substances
• social supports and mental health

Some patients that suffer from certain concomitant conditions may require Topiramate for life. Of note, Topiramate must be weaned off if it is discontinued after being used continuously for a month or more.

Contraindications to Topiramate Use

Topiramate is considered a relatively safe medication in general. The only absolute contraindications to the use of Topiramate are allergy to it, severe liver failure and pregnancy. Relative contraindications to its use are severe hepatitis, liver cirrhosis, kidney disease, history of kidney stones, suicidal ideation / severe depression, risk of severe bleeding, chronic low potassium, severe respiratory disease and concomitant powerful sedative use.

Possible Adverse Effects of Topiramate

 

  •  Severe Skin Reactions (rare)
  • Suicidal Behavior (rare)
  • Mental Illness (rare)
  • Nausea / Vomiting
  • Vision Problems
  • Headache
  • Fatigue / Sleepiness
  • Blood Cell Problems
  • Hyperthermia (rare)
  • Dizziness
  • Change in Bowel Habits
  • Low Potassium
  • Weight Loss / Anorexia
  • Taste Changes
  • Numbness
  • Tremor
  • Bone Density Loss
  • Anxiety / Nervousness
  • Abdominal Discomfort
  • Disorders of Metabolism
  • Glaucoma (rare)
  • Balance Problems
  • Problems with Concentration

Summary: Naltrexone & Topiramate

Naltrexone and Topiramate, either used together or individually, may provide excellent advantages when attempting to remain clean and sober. Each medication has its advantages and disadvantages; thus, consideration to which is used must take into account the individual patient’s medical history, current medications, social situation, psychiatric profile and substances of abuse.

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