Benfotiamine + Folic Acid + Methylcobalamin + Pregabalin + Vitamin B6

Usage

This combination medication is primarily prescribed for the management of neuropathic pain, a type of chronic pain caused by nerve damage or dysfunction. Examples of conditions causing neuropathic pain include diabetic neuropathy, post-herpetic neuralgia (nerve pain following shingles), and spinal cord injury. It may also be used for nerve pain resulting from vitamin B deficiencies.

This drug’s pharmacological classifications include:

• Analgesic: Pregabalin component for pain relief
• Anticonvulsant: Pregabalin component for seizure control (although this combination is not typically used as a primary anticonvulsant)
• Nutritional Supplement: Vitamin B components (Benfotiamine, Folic Acid, Methylcobalamin, Vitamin B6) supporting nerve health.

The mechanism of action involves multiple pathways: Pregabalin modulates calcium channels in nerve cells, reducing the release of neurotransmitters associated with pain signals. B vitamins support nerve function and myelin production, facilitating nerve regeneration and protection.

Alternate Names

There is no single international nonproprietary name (INN) for this combination. It’s often referred to by its constituent components. Brand names vary regionally; some examples include Neurofast, Nervijen, Nervijen-P, Upcyte-P, Pedwin, Meganeuron PG, and Pregamer Plus.

How It Works

Pharmacodynamics:

• Pregabalin: Binds to the alpha-2-delta subunit of voltage-gated calcium channels in the central nervous system, decreasing the release of neurotransmitters like glutamate, noradrenaline, and substance P, reducing neuronal excitability and pain signal transmission.
• B Vitamins: Benfotiamine, a fat-soluble form of thiamine (B1), enhances transketolase activity, a crucial enzyme in the pentose phosphate pathway, protecting nerves from glucose toxicity. Methylcobalamin (B12) and pyridoxine (B6) are involved in myelin synthesis and nerve regeneration. Folic acid (B9) is essential for DNA synthesis and cell division, supporting nerve cell function.

Pharmacokinetics:

• Pregabalin: Rapidly absorbed orally, reaching peak plasma concentrations within 1 hour. It is minimally metabolized and primarily excreted unchanged in the urine. The half-life is approximately 6 hours.
• B Vitamins: These are water-soluble and absorbed variably in the gastrointestinal tract. They undergo metabolic conversion in the liver and are excreted primarily in the urine.

Elimination Pathways: Pregabalin is mainly excreted renally. B vitamins are primarily eliminated renally, with some metabolic conversion in the liver.

Dosage

Dosage is determined by the physician based on individual patient needs and response.

Standard Dosage

Adults: Typical dosages may involve pregabalin 75-150 mg twice daily, combined with varying doses of B vitamins depending on the specific formulation.

Children: Safety and efficacy have not been established in children below 12 years of age. Dosage adjustments are needed in children based on weight, age and medical condition.

Special Cases:

• Elderly Patients: Dosage adjustments may be necessary due to age-related decline in renal function.
• Patients with Renal Impairment: Pregabalin dosage must be reduced based on creatinine clearance.
• Patients with Hepatic Dysfunction: Caution advised in patients with severe liver disease, and dosage adjustments may be required for pregabalin.
• Patients with Comorbid Conditions: Careful evaluation is necessary for patients with heart problems, chronic pulmonary insufficiency, suicidal tendencies, or a history of substance abuse.

Clinical Use Cases

The dosage for this combination drug is not typically modified for specific medical settings like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations. In these cases, pain management is individualized based on the patient’s condition and usually involves different medications tailored to acute needs.

Dosage Adjustments

Dose modifications are essential for patients with renal or hepatic impairment. Dosage adjustments are made for pregabalin based on creatinine clearance (renal) and liver function tests (hepatic).

Side Effects

Common Side Effects

Dizziness, drowsiness, tiredness, nausea, vomiting, blurred vision, dry mouth, peripheral edema, weight gain, difficulty concentrating.

Rare but Serious Side Effects

Allergic reactions (anaphylaxis, bronchospasm), angioedema, suicidal thoughts, changes in mental status.

Long-Term Effects

Weight gain, peripheral edema, cognitive impairment (with prolonged pregabalin use), potential for dependence with pregabalin.

Adverse Drug Reactions (ADR)

Angioedema, anaphylaxis, suicidal ideation, severe CNS depression (with concomitant use of CNS depressants).

Contraindications

Hypersensitivity to any component of the medication.

Drug Interactions

Pregabalin may interact with other CNS depressants (alcohol, opioids, benzodiazepines, antihistamines), enhancing their sedative effects. It can also interact with certain anticonvulsants (e.g., phenytoin, phenobarbital). Antacids might reduce pregabalin absorption. B vitamins, especially folic acid, may interfere with some medications, including certain antibiotics and anticonvulsants.

Pregnancy and Breastfeeding

Pregabalin is categorized as Pregnancy Category C (animal studies have shown adverse effects, human data limited). Use during pregnancy should be considered only if the potential benefit outweighs the risk to the fetus. B vitamins are generally considered safe during pregnancy and lactation, but high doses should be avoided.

Drug Profile Summary

• Mechanism of Action: Pregabalin modulates calcium channels, reducing neuronal excitability. B vitamins support nerve function, myelin production, and nerve regeneration.
• Side Effects: Dizziness, drowsiness, nausea, peripheral edema, weight gain.
• Contraindications: Hypersensitivity.
• Drug Interactions: CNS depressants, anticonvulsants, antacids.
• Pregnancy & Breastfeeding: Pregabalin-use with caution. B vitamins-generally safe.
• Dosage: Varies based on individual needs and renal function.
• Monitoring Parameters: Pain levels, neurological function, renal function, blood glucose (in diabetics), mood changes.

Popular Combinations

This combination itself represents a popular therapeutic approach for neuropathic pain, combining pharmacological pain control with nutritional nerve support. Other drugs like Alpha Lipoic Acid are sometimes added to this combination in some formulations.

Precautions

*Renal and hepatic function must be assessed before starting treatment. *Patients should be monitored for mood changes and suicidal ideation, especially those with a history of depression. *Alcohol should be avoided due to additive CNS depressant effects. * Caution should be exercised in patients with chronic pulmonary insufficiency.

FAQs (Frequently Asked Questions)

Q1: What is the recommended dosage for Benfotiamine + Folic Acid + Methylcobalamin + Pregabalin + Vitamin B6?

A: Dosage varies based on individual patient needs and the specific formulation. Pregabalin is commonly started at 75 mg twice daily and may be increased to 150 mg twice daily. B vitamin dosages vary depending on the product.

Q2: How does this combination medication relieve neuropathic pain?

A: Pregabalin works by modulating calcium channels, reducing pain signal transmission. B vitamins support nerve health, promote myelin production, and aid in nerve regeneration.

Q3: Can this combination be used in pregnant or breastfeeding women?

A: Pregabalin should be used with caution during pregnancy only if the benefit outweighs the potential risk. B vitamins are generally safe but very high doses should be avoided. Consult a physician before use during pregnancy or breastfeeding.

Q4: What are the common side effects patients should be aware of?

A: Dizziness, drowsiness, tiredness, nausea, weight gain are the common side effects.

Q5: What are the major drug interactions with this combination?

A: Avoid alcohol and other CNS depressants. Interactions with anticonvulsants are also possible. Consult a doctor before taking antacids along with this medication.

Q6: Are there any contraindications to using this medication?

A: Known hypersensitivity to any component of the medication is a contraindication.

Q7: How long does it take for this medication to be effective?

A: Initial pain relief might be seen within a few weeks but optimal effects might require 2-3 months of regular use.

Q8: Can patients stop taking this medication abruptly?

A: No, abrupt discontinuation of pregabalin can lead to withdrawal symptoms like nausea, anxiety, and insomnia. Dosage should be tapered down gradually under medical supervision.

Q9: What should a patient do if they miss a dose?

A: Take the missed dose as soon as remembered unless it is close to the next scheduled dose. Do not double the dose.

Q10: Can this combination be used in children?

A: Safety and efficacy have not been established for children under 12 years. Dosage adjustment is important based on the child’s weight and medical condition.