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Naltrexone 4.5mg (can split in 1/2 or 1/4 for titration)

Naltrexone 4.5mg (can split in 1/2 or 1/4 for titration) is a prescriber-directed weight-management medication option. It should be used as part of a broader care plan that includes nutrition, activity, contraindication screening, and monitoring.

TrocheAs prescribedRx Only503A Compounded

Low-dose naltrexone (LDN) 4.5 mg is a compounded oral capsule formulated to allow flexible dosing via splitting for gradual titration protocols. This formulation specifically enables initiation at sub-therapeutic doses (e.g., 1.125 mg or 2.25 mg) with stepwise upward titration to the full 4.5 mg maintenance dose — an approach used to minimize initial side effects (sleep disturbance, nausea) in sensitive patients or those initiating LDN for autoimmune and inflammatory conditions. Genesis Compounding prepares this as a prescription-only, patient-specific 503A compounded preparation; LDN is not FDA-approved at this dose for any indication. Note: splitting a capsule requires careful technique; the prescriber should confirm the patient understands the method.

Active IngredientPharmacologic Role
Naltrexone 4.5 mg (dividable capsule)Opioid receptor antagonist at low dose; transient opioid and TLR4/TLR9 receptor blockade followed by rebound endorphin upregulation and microglial regulation — providing immune-modulating and anti-inflammatory effects in chronic conditions when used at sub-standard doses during titration.

Oral capsule — with titration splitting option: To split, open the capsule carefully and divide the powder contents onto a clean surface, measuring half or one-quarter by volume. Mix the appropriate portion with a small amount of water or food as directed. The full capsule may be swallowed intact once the target dose (4.5 mg) is reached. Take once daily at bedtime for all dose levels. Swallow with water. Consistent bedtime administration is recommended for all dosing levels.

Prescribers should confirm the appropriate splitting method with the dispensing pharmacy and ensure the patient has been counseled on accurate dose division technique.

Titration schedule is prescriber-determined. A common stepwise approach:

  • Week 1–2: 1.125 mg (1/4 capsule) at bedtime
  • Week 3–4: 2.25 mg (1/2 capsule) at bedtime
  • Week 5–6: 3.375 mg (3/4 capsule) at bedtime
  • Week 7+: 4.5 mg (full capsule) at bedtime
  • For some conditions (e.g., MS), maintenance may remain at 3 mg per prescriber direction.

Identical to Naltrexone 4.5 mg (ID 160). All dose levels share the same mechanism; lower doses during titration produce proportionally less receptor blockade and a milder rebound endorphin effect, allowing immune system adjustment before reaching full therapeutic dosing.

Identical to Naltrexone 4.5 mg (ID 160). The titration-enabling format is particularly valuable for patients with: autoimmune conditions prone to initial immune activation responses, Hashimoto's thyroiditis (where sudden immune modulation may require rapid thyroid medication adjustment), multiple sclerosis, fibromyalgia, and chronic fatigue syndrome — all of whom may benefit from gradual dose escalation.

Identical to Naltrexone 4.5 mg (ID 160).

Contraindications:

  • Concurrent opioid analgesics (any dose — will precipitate withdrawal)
  • Physiologic opioid dependence
  • Severe hepatic failure

Common Side Effects: Vivid dreams, insomnia (initial weeks), mild nausea, headache — all dose-dependent and typically milder during titration phase.

Store at room temperature (20–25°C), away from moisture, heat, and light. Once opened for dose splitting, use the divided portion immediately and discard any remainder that cannot be adequately measured or preserved. Observe the beyond-use date assigned by Genesis Compounding.

Why would I split the capsule instead of taking the full dose?

Gradual titration minimizes the likelihood of initial side effects — particularly sleep disruption and vivid dreams — that sometimes occur when LDN is started at the full 4.5 mg dose. Starting low and slowly increasing allows your immune system to adjust and improves long-term tolerability.

How do I accurately split a capsule?

Open the capsule carefully over a clean surface. Divide the powder visually or by weight into halves or quarters. Mix with a teaspoon of water or applesauce for the partial dose, or transfer directly to your mouth and swallow with water. Your prescriber or pharmacist will provide specific technique guidance. For more accurate dosing, ask your prescriber whether separate lower-strength capsules (e.g., 1.5 mg or 2.25 mg) would be more appropriate.

Are there advantages to having separate lower-dose capsules versus splitting?

Yes — separate pre-measured capsules for each titration step are more accurate and easier to use than splitting. If splitting proves difficult, discuss with your prescriber whether Genesis Compounding can prepare individual capsules at the intermediate titration strengths.

Is this FDA-approved?

No. LDN at any dose below 50 mg is not FDA-approved. This is a prescriber-directed, patient-specific 503A compounded preparation.

Clinical References

Authoritative sources reviewed in preparing this clinical summary. Provided for prescriber reference; not a substitute for the prescriber’s clinical judgment.

The Use of Low-Dose Naltrexone as a Novel Anti-Inflammatory Treatment
Clinical Rheumatology / PMC, 2014
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Low-Dose Naltrexone as a Treatment for Chronic Fatigue Syndrome — BMJ Case Reports
BMJ Case Reports, 2020
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Naltrexone — DailyMed Label Search
DailyMed / NLM
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