Entivon

Uses

Entivon is a combination of medicines used to treat long-lasting (chronic) pain caused by nerve damage due to diabetes, shingles or spinal cord injury. It reduces pain and its associated symptoms such as mood changes, sleep problems, and tiredness. Pregabalin, an active ingredient of this medicine, is thought to work by interfering with pain signals that travel through the damaged nerves and the brain. It also contains nutritional supplements that improve nerve conduction. Taking Entivon regularly will improve your physical and social functioning and overall quality of life.

Entivon is also used to associated treatment for these conditions: Vitamin B12 Deficiency, Nutritional supplementationDiabetic Peripheral Neuropathic Pain (DPN), Epilepsies, Fibromyalgia, Generalized Anxiety Disorder (GAD), Neuropathic Pain, Partial-Onset Seizures, Peripheral Neuropathic Pain, Peripheral neuropathy, Postherpetic Neuralgia

How Entivon works

Although the mechanism of action has not been fully elucidated, studies involving structurally related drugs suggest that presynaptic binding of pregabalin to voltage-gated calcium channels is key to the antiseizure and antinociceptive effects observed in animal models.

By binding presynaptically to the alpha2-delta subunit of voltage-gated calcium channels in the central nervous system, pregabalin modulates the release of several excitatory neurotransmitters including glutamate, substance-P, norepinephrine, and calcitonin gene related peptide. In addition, pregabalin prevents the alpha2-delta subunit from being trafficked from the dorsal root ganglia to the spinal dorsal horn, which may also contribute to the mechanism of action.

Although pregabalin is a structural derivative of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), it does not bind directly to GABA or benzodiazepine receptors.

Dosage

Entivon dosage

For adults, take one capsule daily or as directed by a physician

• Pregabalin + mecobalamin should be taken as directed by your doctor.
• Swallow it whole with a glass of water. Do not cut, break or chew the medicine.
• It can be taken with or without food.
• It would be best if you took it at a fixed time for optimal results.
• You should not consume it more than that prescribed by your doctor.
• Do not stop the medicine abruptly on your own, as it can lead to diarrhoea, lack of sleep, nausea, fits. In case it has to be stopped, your doctor shall gradually decrease the dose.

Side Effects

Pregabalin + mecobalamin may have the following side effects:

• Dizziness
• Somnolence
• Blurred vision
• Diplopia
• Increased appetite
• Weight gain
• Dry mouth
• Constipation
• Vomiting
• Flatulence
• Euphoria
• Confusion
• Reduced libido
• Erectile dysfunction
• Irritability
• Vertigo
• Ataxia
• Tremor
• Dysarthria
• Paresthesia
• Fatigue
• Edema

Toxicity

In a systematic review that included 38 randomized controlled trials, there were 20 identified adverse effects that were significantly associated with pregabalin, most of which involve the central nervous system and cognition. The identified adverse effects include vertigo, dizziness, balance disorder, incoordination, ataxia, blurred vision, diplopia, amblyopia, somnolence, confusional state, tremor, disturbance in attention, abnormal thinking, asthenia, fatigue, euphoria, edema, peripheral edema, dry mouth, and constipation .

The most common symptoms of pregabalin toxicity (dose range includes 800 mg/day and single doses up to 11,500 mg) include somnolence, confusion, restlessness, agitation, depression, affective disorder and seizures.

Since there is no antidote for pregabalin overdose, patients should receive general supportive care. If appropriate, gastric lavage or emesis may help eliminate unabsorbed pregabalin (healthcare providers should take standard precautions to maintain the airway).

Pregabalin pharmacokinetic properties suggest that extra-corporeal elimination methods including haemodialysis, may be useful in situations of severe toxicity. However, there are cases where patients have presented with very high serum levels of pregabalin and have been successfully managed with supportive care alone.

Precaution

The medicine should not be used for months if there is no response at all after its use for a certain period of time.

Discontinuation of Pregabalin without tapering may produce insomnia, nausea, headache and diarrhea. So it should be tapered gradually over a minimum of 1 week rather than discontinued abruptly. Creatinine kinase may be elevated if treated with Pregabalin. It should be discontinued rapidly if myopathy is diagnosed or suspected or if creatinine kinase is elevated markedly.

Interaction

Decreased GI tract absorption with neomycin, aminosalicylic acid, H2-blockers and colchicine. Reduced serum concentrations with oral contraceptives. Reduced effects in anaemia with parenteral chloramphenicol.

Volume of Distribution

After oral administration of pregabalin, the reported apparent volume of distribution is roughly 0.5 L/kg.

Although pregabalin is not very lipophilic, it is able to cross the blood brain barrier(BBB). System L transporters facilitate the transport of large amino acids across the BBB and it has been confirmed that pregabalin is a substrate. This information suggests that system L transporters are responsible for pregabalin uptake into the BBB.

In rat models, pregabalin has been shown to cross the placenta.

Elimination Route

After oral dosing administered in the fasted state, pregabalin absorption is rapid, and extensive. Pregabalin oral bioavailability is reported to be ≥90% regardless of the dose. Cmax is attained within 1.5 hours after single or multiple doses, and steady state is attained within 24-48 hours with repeated administration. Both Cmax and AUC appear to be dose proportional.

Food decreases the rate of pregabalin absorption and as a result, lowers the Cmax by an estimated 25-30% and increases the Tmax to approximately 3 hours. However, the effect of food does not appear to impact the total absorption of pregabalin in a way that is clinically relevant. As a result, pregabalin can be administered with or without food.

Half Life

The elimination half life of pregabalin is 6.3 hours.

Clearance

In young healthy subjects the mean renal clearance is estimated to be 67.0 to 80.9 mL mL/min. Given pregabalin's lack of plasma protein binding, this clearance rate suggests that renal tubular reabsorption is involved.

Elimination Route

Pregabalin is almost exclusively eliminated in the urine.

Further, based on preclinical studies, pregabalin does not appear to undergo racemization to the R enantiomer in the body.

Pregnancy & Breastfeeding use

USFDA pregnancy category C. May be or may not be harmful to an unborn baby. Consult a healthcare provider if you are in gestation or plan to have a baby during Entivon treatment.

It is not known whether Entivon can pass through the breast milk or not. Nursing mothers should avoid breastfeeding while taking Entivon.

Contraindication

Hypersensitivity to any component of this product.

Pregabalin is contraindicated in patients with known hypersensitivity to Pregabalin or any of its components.

Special Warning

Take special precautions if you have the following conditions:

• Not to be given in patients w/ suspected vitamin B12 deficiency without first confirming diagnosis.
• Monitor blood regularly. Dose >10 mcg daily may produce a hematological response in patients w/ folate deficiency.
• Leber’s disease or tobacco amblyopia.

Interaction with other Medicine

Inform your doctor and pharmacist if you are taking or using any of these medicines:

• Vit B12
• Neomycin
• Aminosalicylic acid
• Histamine H2-antagonists
• Omeprazole
• Colchicine
• Oral contraceptives

Inform your doctor and pharmacist if you are taking any other medicines, including herbal tonics such as traditional Chinese medicines, supplements, and non-prescription medicines.

This list does not include all medicines that may interact with Pregabalin + mecobalamin.

Storage Condition

• Store at temperatures not exceeding 30°C.
• Store in a cool, dry place away from the reach of children.
• Do not use Pregabalin + mecobalamin that is expired or out of date.

Innovators Monograph

You find simplified version here Entivon