What is Pregabalin?

Pregabalin is known and marketed through brands like Azlain and Lyrica. Pregabalin is a medication that is used in management of epilepsy. Established under the category of anticonvulsants – controls/prevents seizures. As such, Pregabalin usually requires a triplicate prescription from your doctor before it can be filled at the pharmacy.

It is the first antiepileptic agent to receive FDA-approved labeling since 1999. It is indicated and prescribed for several reasons: First is for neuropathic relief that is associated after a spinal injury. Central neuropathic pain is pain that is induced by a disease or a lesion in the central nervous area. It usually happens to stroke patients or patients that have had a spinal cord injury. In most cases, it is treated with anti-depressants, various anticonvulsants, opioids, and cannabinoids. Second, in treatment of fibromyalgia – a long-term condition that causes pain, stiffness in the muscles, tenderness, fatigue and difficulty in sleeping.

Truth be told, no medication works perfectly for fibromyalgia. The initial step to start the treatment of this condition is incorporating change into lifestyle. This includes going on daily exercises with stretching and strengthening components and figuring out a good sleeping scheme to prevent fibromyalgia symptoms such as mood or sleep disorders. Third, it is used for neuropathic pain – pain which arises from damaged nerves. It usually occurs in arms, hands, fingers and even legs or feet.

Neuropathic pain may also be associated with diabetes and postherpetic neuralgia which usually presents burning, stabbing and aches that last for months or years after the onset of shingles. Lastly, it can be used as an adjunct treatment in partial onset seizures that present in adults and even children who are 1 month old the least. Pregabalin is usually for adults and not to be taken by people who are below 18 except for special cases like partial onset seizures. Buy cheap Pregabalin UK. Gabapentin and Pregabalin side-by-side as indicated for Migraine; Migraines happen all the time. Sometimes it can even last up to 3 days. One of the chemicals that play a role in migraines is Gamma Amino Butyric Acid (GABA) where it affects how you perceive pain.

However, there is no FDA approved statement that these medications when used together can manage migraines. It is only termed as an off-label use meaning there is no standard dosage or guidelines on how the mechanism of the combination happens. Other off-label indications of Pregabalin include opiate withdrawal, restless legs syndrome (RLS), and sleeping problems. Pregabalin comes in a tablet form with variants of 25mg, 50mg, 75mg, 100mg, 150mg, 200mg and 300mg hard capsules. The color of the capsules differ depending on the manufacturers. Stored in room temperature between 59°F and 86°F (15°C and 30°C). Best to keep it away from light and avoid moist environments like bathrooms.

How does it work?

Pregabalin falls under the class of GABA (gamma aminobutyric acid) analogs. GABA (gamma aminobutyric acid) analogs work by slowing down impulses in the brain that usually results to seizures. Even though the structure of pregabalin is similar to gamma-aminobutyric acid (GABA), it does not necessarily mean that it will bind to GABA receptors. By binding pre-synaptically to the alpha2-delta subunit of voltage-gated calcium channels in the central nervous system, pregabalin controls the release of some excitatory neurotransmitters including glutamate, substance-P, norepinephrine, and calcitonin gene related peptide. Thus, presynaptic binding of pregabalin to voltage-gated calcium channels is vital to the antiseizure and antinociceptive effects of Pregabalin. While in terms of Pregabalin’s analgesic effects, the modulation of K+ channel conductance, excitatory amino acid transporter and inflammation are possible mechanisms that may have contributed to it.

Pregabalin and Gabapentin are often correlated with each other as “gabapentinoids” but, how do they differ? Both medications are considered as first-line treatments for neuropathic pain syndromes. They both resemble in structure and action as GABA analogs however, pregabalin may either have an additional approach of absorption or is better transported than gabapentin, as it is almost completely absorbed, while gabapentin is not. Gabapentin is a bit slower paced and inconsistently absorbed, with peak plasma concentrations around 3 hours post-dose. While pregabalin is quickly absorbed, with the maximum rate of absorption being 3 times that of gabapentin.

It can reach peak blood concentrations within an hour after consumption. Overall, pregabalin has more conventional pharmacokinetics, and it also shows a stronger binding affinity to its target receptor, increased potency, and a steeper dose-response curve in neuropathic pain that does not plateau over recommended dosing levels.

With these mechanisms, it is more likely to be used as management for neuropathic pain associated with diabetes, post-herpetic neuralgia and injury of the spine. Specifically put, pregabalin works in several ways. In epilepsy, it stops seizures from occurring by decreasing abnormal brain activity. In case of nerve pain, it blocks pain through interference in travelling pain messages from the brain to the spine. Lastly, in anxiety, it prevents the brain from releasing chemicals that likely produce the feeling of being anxious. How long does Pregabalin stay in the body? Once taken the last dose, it could stay in the body systemically for about 31.5 hours.

What are the benefits of taking it?

As we know, cancer cells spread to various sites in the body. As metastasized cancer cells compress, characteristic pain such as electric shock-like pain with tingling sensations develop. Since Pregabalin is indicated mainly for neuropathic pain, it can also be used as an adjunct treatment for analgesic purposes in case of neuropathic cancer-related pain.

However, unlike usual analgesics used in terminally ill patients like opioids, pregabalin treatments are limited only for oral route of administration. Patients who experience difficulties with oral feeding, may not be able to make use of pregabalin as an adjuvant treatment. Added to that, it also has an off-label use for migraines. The American Academy of Neurology (AAN) is an organization that is responsible for the provision of guidance for physicians about medications in the prevention of migraine. Though, some clinical trials have shown a small benefit from the use of gabapentin (Neurontin) for migraine prevention. Even with the benefits of this medication, best be aware of the side effects to be cautious enough when some of these appear. Common side-effects reported are allergic reaction (rash, itching and flushing), dizziness, lethargy, peripheral edema, weight gain (weight gain is usually related to a larger dose of pregabalin and in some cases it is due to water retention or edema), blurring of vision and dry mouth. Since Pregabalin is used as an adjunct therapy in treating partial onset seizures even in children a month old the least, there are common side-effects that occur as well. These side-effects include increased appetite, sleepiness, and weight gain.

Starting with a low dose of Pregabalin then slowly increasing it over time helps lessen the occurrence of these side-effects. Also be cautious in taking Pregabalin concomitantly with other medications that may cause interactions such as ACE-Inhibitors (captopril, lisinopril, enalapril and the like), anti-depressants, antihistamines, narcotics for pain (Hydrocodone, Morphine) – may induce respiratory depression, certain medications for diabetes (Rosiglitazone and Pioglitazone) – may induce higher chances of weight gain or swelling if these medicines are taken, sleeping pills and even tranquilizers – these may further depress the CNS leading to deep sedation or even worse, coma.

Try to avoid drinking alcohol while on this medication (can cause euphoria or further induce CNS depression and lead to sedation). Best be wary by being mindful of existing conditions like angioedema – swelling under the skin; (swelling of the face, mouth, and neck); heart failure – may cause swelling of feet, hands, and legs. In people with heart conditions, the swelling can cause serious problems. Plus, Pregabalin has also shown to increase an interval in heartbeat known as the PR interval, bleeding problems (low platelet count), lung and kidney diseases.

How should you take it?

Usual dosing schedule of Pregabalin is it is taken 2 to 3 times daily even with or without food. Things to know before taking the medication are: Even without any history of epileptic episodes, pregabalin can still help with pain and even anxiety. It would take a couple of weeks before it may start to work or before you see promising results. Side-effects usually go away over time (sleepiness, dizziness and headaches).

Also, to make sure the medication is safe for consumption, assure that before taking it, there is no history of allergic reactions, any addiction or substance abuse, not in the stage of trying to get pregnant (already pregnant or breastfeeding), and well-controlled sodium and potassium.The starting dosage for postherpetic neuralgia is 75 mg twice daily or 50 mg three times daily. Because this medication is associated with adverse effects that are dose dependent, and a higher risk discontinuing treatment due to adverse effects, dosages over 300 mg daily should be reserved for those patients who have ongoing pain and can tolerate a dose of 300 mg daily.

The initial dose for patients with partial-onset seizures is 75 mg twice daily or 50 mg three times daily. Based on the response and tolerability of the patient, the dosage may be increased to a maximum of 600 mg daily. All dosages should be adjusted for patients with reduced renal function especially for geriatric patients. The reduction in pregabalin dosage is based on the patient’s estimated Creatinine Clearance (CrCl). For geriatric patients (>65 years old), clinical monitoring is a MUST. First up, kidney and liver function tests – lowered dosages may be implemented depending on the results. Secondly, mental and behavioral health should also be in check. If abnormal or unusual behavioral changes occur, check with your local physician.

The frequency of intake is usually 3 times per day and will always depend on the efficacy and tolerability towards the patient. In switching from immediate to extended release, on the day of the switch, take morning dose as usual then initiate the extended-release form after dinner. Take note that in discontinuation, it should be tapered slowly for a week and not just withdrawing it abruptly from the regime to avoid any withdrawal symptoms to arise. Withdrawal symptoms may include insomnia, nausea, headaches, diarrhea, sweating, tremors, severe cravings, depression, anxiety relapse and seizures.

How long should Pregabalin be taken? If you are taking Pregabalin for epilepsy, likely even if the illness is already under control, it will still be a part of your regime every now and then. In case of the need for the medication for nerve pain and even anxiety, chances of this medication being retained for months is highly likely to fully reach the medication’s potential in decreasing occurrences of its symptoms. But before fully withdrawing it from your system, tapering the dose down will help avoid occurrences of withdrawal symptoms.