Pregan ER82.5 mg

Pregan ER is indicated for the following conditions:

Established / FDA-approved uses

• Neuropathic pain associated with diabetic peripheral neuropathy (DPN)
• Postherpetic neuralgia (PHN) — nerve pain following shingles
• Fibromyalgia — for management of widespread musculoskeletal pain
• Adjunctive therapy for partial-onset seizures in adults and pediatric patients 1 month of age and older, used together with other anti-seizure medicines (not for use as a single/sole agent)
• Neuropathic pain associated with spinal cord injury

Off-label / additional uses (variable evidence)

• Generalized anxiety disorder (GAD) — approved in some countries outside the US; used off-label elsewhere based on clinical judgement
• Chronic low back pain with a neuropathic component and restless legs syndrome — used off-label in select patients; evidence is limited and this is not a primary approved indication

Use of Pregan ER should always be guided by a qualified physician based on individual diagnosis.

Each capsule or tablet contains Pregabalin as the active pharmaceutical ingredient.

• Immediate-release capsules/tablets: 25 mg, 50 mg, 75 mg, 100 mg, 150 mg, 200 mg, 225 mg, and 300 mg of Pregabalin
• Extended-release tablets: 82.5 mg, 165 mg, and 330 mg of Pregabalin
• Oral solution: 20 mg/mL (equivalent to 100 mg/5 mL) of Pregabalin

Inactive ingredients (fillers, coating agents, preservatives in the oral solution) vary by manufacturer and formulation; refer to the product-specific package insert for the complete excipient list.

Pregan ER is a synthetic amino acid analog structurally related to gamma-aminobutyric acid (GABA), belonging to the gabapentinoid class of medicines. It is used to relieve certain types of nerve (neuropathic) pain, manage fibromyalgia, and as an add-on treatment for partial-onset seizures.

Pregan ER is available as immediate-release capsules/tablets, extended-release tablets, and an oral solution, allowing dosing to be individualized to the patient's condition and renal function.

Pregan ER belongs to the gabapentinoid class of medicines, used therapeutically as an anticonvulsant (anti-epileptic) and neuropathic pain agent. In the United States it is classified as a Schedule V controlled substance due to its abuse/misuse potential.

Pregabalin binds with high affinity to the alpha-2-delta (α2δ) subunit of voltage-gated calcium channels in the central nervous system. This binding reduces calcium influx at nerve terminals, which in turn decreases the release of several excitatory neurotransmitters, including glutamate, norepinephrine, and substance P.

Although structurally related to GABA, Pregabalin does not bind to GABA-A or GABA-B receptors, is not converted into GABA or a GABA agonist, and does not directly affect GABA reuptake or degradation. Its analgesic, anticonvulsant, and anxiolytic-like effects are attributed to this modulation of calcium channel activity and consequent reduction in neuronal excitability.

Pharmacokinetics: Pregabalin is absorbed rapidly, is not appreciably bound to plasma proteins, undergoes negligible hepatic metabolism, and is eliminated almost entirely unchanged by the kidneys. Its elimination half-life is approximately 6 hours in patients with normal renal function, so dose adjustment is required in renal impairment (see Dosage and Administration).

Pregan ER immediate-release capsules/tablets and oral solution may be taken with or without food. Extended-release tablets should be taken once daily after an evening meal and swallowed whole — they must not be split, crushed, or chewed.

If a dose is missed, it should be taken as soon as remembered unless it is almost time for the next dose, in which case the missed dose should be skipped; doses should not be doubled.

Do not stop taking Pregan ER suddenly; the dose should be tapered gradually under medical supervision (see Precautions and Warnings).

Clinically significant drug interactions with Pregan ER:

• CNS depressants (opioids, benzodiazepines, barbiturates, sedating antihistamines) and alcohol: additive sedation, dizziness, and impairment of cognitive/motor function; concomitant opioid use also increases the risk of respiratory depression. Concurrent use should be avoided or closely monitored.
• Thiazolidinediones (e.g., pioglitazone, rosiglitazone): additive risk of peripheral edema and weight gain when combined with Pregan ER.
• ACE inhibitors (e.g., enalapril): may have an additive effect on angioedema risk.
• Oxycodone and other opioid analgesics: additive impairment of cognitive and gross motor function beyond either drug alone.

No clinically important pharmacokinetic drug-drug interactions have been established for Pregan ER, as it is not appreciably protein-bound and undergoes minimal hepatic metabolism.

Common side effects of Pregan ER (may affect more than 1 in 10 people) include:

• Dizziness and somnolence (drowsiness)
• Dry mouth
• Peripheral edema (swelling of hands/feet)
• Blurred vision
• Weight gain and increased appetite
• Difficulty with concentration/attention, ataxia (unsteady gait), fatigue

Less common but serious side effects — seek prompt medical attention if these occur:

• Angioedema and hypersensitivity reactions (facial/throat swelling, difficulty breathing) — see Contraindications
• New or worsening depression, unusual changes in mood or behavior, or suicidal thoughts
• Muscle pain, tenderness, or weakness with fever/fatigue (possible rhabdomyolysis)
• Unusual bleeding or bruising (thrombocytopenia)
• Severe dizziness, fainting, or slowed/irregular heartbeat
• Signs of respiratory depression when combined with opioids or other CNS depressants — see Interactions

Pregnancy: Human data on Pregan ER use during pregnancy are limited. Animal reproduction studies have shown developmental toxicity at doses relevant to human exposure. Pregan ER should be used during pregnancy only if clearly needed and if the potential benefit to the mother justifies the potential risk to the fetus. A pregnancy exposure registry exists in some countries to monitor outcomes; patients who become pregnant while taking Pregan ER should consult their physician promptly and should not stop the medicine abruptly without medical advice (see Precautions and Warnings on abrupt discontinuation).

Lactation: Pregan ER is excreted into human breast milk. Because of the potential for adverse effects in a breastfed infant (e.g., sedation, poor feeding), a decision should be made whether to discontinue breastfeeding or discontinue the medicine, taking into account the importance of treatment to the mother; this decision should be made with a physician.

The following precautions apply to treatment with Pregan ER:

• CNS depression: Pregan ER may cause dizziness and somnolence that can impair the ability to drive or operate machinery; effects are additive with alcohol, opioids, benzodiazepines, and other CNS depressants (see Interactions).
• Angioedema and hypersensitivity: can occur even after prior uneventful use; discontinue immediately if facial/throat swelling or breathing difficulty occurs (see Contraindications).
• Abuse and dependence potential: Pregan ER is a controlled substance (Schedule V in the United States) and controlled in a number of other jurisdictions because of misuse/dependence potential; use with caution in patients with a history of substance abuse.
• Peripheral edema and weight gain: monitor patients, particularly those with cardiac disease or those on thiazolidinedione therapy.
• Do not stop abruptly: discontinuing Pregan ER suddenly can cause withdrawal symptoms (insomnia, nausea, headache, diarrhea, anxiety, sweating) and, in patients with epilepsy, can precipitate seizures, including status epilepticus. Taper the dose gradually over at least 1 week under medical guidance.
• Suicidal thoughts or behavior: antiepileptic drugs as a class, including Pregan ER, are associated with a small increased risk of suicidal ideation; monitor for mood changes, especially early in treatment.
• Cardiac conduction: mild PR-interval prolongation has been observed; use caution in patients with cardiac conduction abnormalities.
• Visual disturbance: blurred vision and other visual changes have been reported; caution with visually demanding tasks.
• Renal impairment: requires dose reduction — see Dosage and Administration.

Symptoms reported with Pregan ER overdose include marked somnolence, confusion, agitation, restlessness, and, less commonly, seizures. There is no specific antidote for Pregan ER overdose.

If an overdose of Pregan ER is suspected, seek immediate medical attention or contact a poison control center/emergency services right away. Management is supportive and symptomatic (airway protection, monitoring of vital signs). Pregan ER can be removed by hemodialysis, which may be considered in cases of significant overdose, particularly in patients with renal impairment. Do not attempt to manage a suspected overdose at home.

Store at room temperature (below 30°C), away from light and moisture. Keep out of reach of children.

• Renal impairment: dose reduction is required based on creatinine clearance; see Dosage and Administration for the full adjustment schedule.
• Hepatic impairment: no dose adjustment is required, as Pregan ER is not significantly metabolized by the liver.
• Elderly patients: more likely to have age-related reduced renal function and may be more sensitive to dizziness, somnolence, confusion, and edema; dose should be adjusted for renal function and titrated cautiously.
• Pediatric patients: approved as adjunctive therapy for partial-onset seizures from 1 month of age with weight-based dosing (see Dosage and Administration); safety and efficacy for neuropathic pain and fibromyalgia have not been established in patients under 18 years.
• Pregnancy and breastfeeding: see Pregnancy and Lactation.

Duration of Pregan ER therapy is individualized to the indication and clinical response:

• For neuropathic pain and fibromyalgia, an adequate trial (typically several weeks at an optimized dose) is used to assess benefit; therapy is continued if effective and reassessed periodically by the treating physician.
• For adjunctive treatment of partial-onset seizures, Pregan ER is generally continued long-term as part of an overall seizure-management plan, with regular medical review.

Regardless of indication, Pregan ER should not be discontinued abruptly; if treatment is to be stopped, the physician will taper the dose gradually over a minimum of one week (see Precautions and Warnings).

Pregabalin belongs to the gabapentinoid drug class, grouped therapeutically with anticonvulsants (anti-epileptic drugs) and neuropathic pain agents. It is chemically and pharmacologically related to gabapentin.

Pregabalin binds to the alpha-2-delta subunit of voltage-gated calcium channels on nerve terminals in the central nervous system, reducing calcium influx and thereby decreasing the release of excitatory neurotransmitters such as glutamate, norepinephrine, and substance P. This dampens neuronal hyperexcitability underlying neuropathic pain and seizure activity, without directly acting on GABA receptors.

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Pregan ER is approved as adjunctive (add-on) therapy for partial-onset seizures in pediatric patients 1 month of age and older, dosed on a weight (mg/kg/day) basis and titrated gradually (see Dosage and Administration).

Safety and efficacy of Pregan ER for other indications — including neuropathic pain and fibromyalgia — have not been established in patients under 18 years of age, and it should not be used for these indications in children outside specialist guidance.

Pediatric patients treated with Pregan ER for seizures should be monitored for increased appetite, weight gain, and mood/behavioral changes, and the dose should never be stopped abruptly (see Precautions and Warnings).