Lybalin

Pregabalin.

LYBALIN 25 MG: Each capsule contains 25 mg pregabalin.
LYBALIN 75 MG: Each capsule contains 75 mg pregabalin.

PHARMACOLOGY: Pharmacodynamics: Pregabalin binds with high affinity to the alpha₂-delta site (an auxiliary subunit of voltage-gated calcium channels) in CNS tissues. The mechanism of action of pregabalin is unknown.
Pharmacokinetics: Absorption: Pregabalin is rapidly absorbed after oral doses and peak plasma concentrations are achieved within 1.5 hours. Pregabalin oral bioavailability is about 90% or more and is independent of dose. The rate but not the extent of absorption is reduced if given with food but this is not clinically significant. Therefore, pregabalin can be taken with or without food. Steady state is achieved after 1 to 2 days.
Distribution: Pregabalin is not bound to plasma proteins. The apparent volume of distribution of pregabalin following oral administration is approximately 0.5 L/kg.
Metabolism: Pregabalin undergoes negligible metabolism in humans. Following a dose of radiolabeled pregabalin, approximately 90% of the administered dose was recovered in the urine as unchanged pregabalin. The N-methylated derivative of pregabalin, the major metabolite of pregabalin found in urine, is accounted for 0.9% of the dose.
Elimination: About 98% of a dose is eliminated from the systemic circulation primarily by renal excretion as unchanged drug. The mean elimination half-life is 6.3 hours. Pregabalin is removed by hemodialysis.

Neuropathic pain: Pregabalin is indicated for the treatment of central and peripheral neuropathic pain in adults which includes diabetic peripheral neuropathy and post-herpetic neuralgia.
Epilepsy: Pregabalin is indicated as adjunctive therapy in adults with partial seizures with or without secondary generalization.
Generalized Anxiety Disorders (GAD): Pregabalin is indicated for the treatment of Generalized Anxiety Disorders (GAD) in adults.
Fibromyalgia: Pregabalin is indicated for the management of fibromyalgia.

The dose range is 150 to 600 mg per day given in either two or three divided doses. Pregabalin may be taken with or without food.
Neuropathic Pain: Pregabalin treatment can be started at a dose of 150 mg per day. Based on individual patient response and tolerability, the dosage may be increased to 300 mg per day within 1 week, and if needed, to a maximum dose of 600 mg daily after an additional 7 days interval. Although a maximum daily dose of 300 mg is recommended in diabetic peripheral neuropathy.
Epilepsy: Pregabalin treatment can be started at a dose of 150 mg per day, 75 mg twice daily or 50 mg 3 times daily. Based on the individual patient response and tolerability, the dosage may be increased to 300 mg per day after 1 week. The maximum dosage of 600 mg per day may be achieved after an additional week.
Generalized Anxiety Disorder: Pregabalin treatment can be started at a dose of 150 mg per day in 2 to 3 divided doses. Based on the individual patient response and tolerability, the dosage may be increased to 300 mg per day after 1 week. Following an additional week the dosage may be increased to 450 mg per day. The maximum dosage of 600 mg per day may be achieved after an additional week.
Fibromyalgia: Pregabalin treatment can be started at a dose of 150 mg per day (75 mg two times a day) and may be increased to 300 mg per day (150 mg two times a day) within 1 week based on efficacy and tolerability. Patients who do not experience adequate benefit with 300 mg per day may have dosage further increased to the maximum recommended dosage of 450 mg daily (225 mg twice daily).
Dosage in Renal Function Impairment: The dose of pregabalin for patients with renal impairment should be reduced according to creatinine clearance (CrCl): CrCl 30 to less than 60 mL/minute: Starting daily dose: 75 mg; maximum daily dose: 300 mg; daily dose given in 2 or 3 divided doses.
CrCl 15 to less than 30 mL/minute: Starting daily dose: 25 to 50 mg; maximum daily dose: 150 mg; daily dose given in 2 divided doses or once daily.
CrCl less than 15 mL/minute: Starting daily dose: 25 mg; maximum daily dose: 75 mg; daily dose given as one dose.
For patients undergoing hemodialysis, the pregabalin daily dose should be adjusted based on renal function. In addition to the daily dose adjustment, a supplemental dose should be given immediately following every 4-hour hemodialysis treatment. Individuals receiving the 25-mg once daily dosage regimen should receive a supplemental dose of 25 or 50 mg, those receiving the 25- to 50-mg once daily dosage regimen should receive a supplemental dose of 50 or 75 mg, those receiving the 50- to 75-mg once daily dosage regimen should receive a supplemental dose of 75 or 100 mg, and those receiving the 75-mg once daily dosage regimen should receive a supplemental dose of 100 or 150 mg.

Symptoms: There is limited experience with overdose of pregabalin. The highest reported accidental overdose of pregabalin was 8,000 mg, and there were no notable clinical consequences.
Treatment: There is no specific antidote for overdose with pregabalin. If indicated, elimination of unabsorbed drug may be attempted by gastric lavage; observe usual precautions to maintain the airway. General supportive care of the patient is indicated, including monitoring of vital signs and observation of the clinical status of the patient. Hemodialysis may be indicated by the patient's clinical state or in patients with significant renal function impairment. Standard hemodialysis procedures result in significant clearance of pregabalin (approximately 50% in 4 hours).

Hypersensitivity to pregabalin or any of its components.

(Based on the Ministry of Public Health Announcement): The drug may cause drowsiness, do not drive a car or operate machinery, or drink alcoholic beverages while taking the drug.
The drug may cause hematologic disorder.
Do not use the drug while pregnant because it may cause teratogenesis.
Use the drug with caution in patients with liver and kidney disease.

Angioedema: Specific symptoms included swelling of the face, mouth (gums, lips, and tongue), and neck (larynx and throat). Discontinue pregabalin immediately in patients with these symptoms. Exercise caution when prescribing pregabalin to patients who have had a previous episode of angioedema. In addition, patients who are taking other drugs associated with angioedema may be at increased risk of developing angioedema.
Discontinuation: Withdraw pregabalin gradually to minimize the potential of increased seizure frequency in patients with seizure disorders. Following abrupt or rapid discontinuation of pregabalin, some patients reported symptoms, including diarrhea, headache, insomnia, and nausea. Taper pregabalin gradually over a minimum of 1 week rather than discontinuing abruptly.
Suicidal Behavior and Ideation: Pregabalin increase the risk of suicidal thoughts or behavior in patients taking this drug for any indication. Monitor patients treated with pregabalin for any indication for the emergence of worsening of depression, suicidal thoughts or behavior, and/or any unusual changes in mood or behavior.
Peripheral Edema: Pregabalin treatment may cause peripheral edema.
Dizziness/Somnolence: Pregabalin may cause dizziness and somnolence. Pregabalin-related dizziness and somnolence may impair their ability to perform tasks such as driving or operating machinery.
Weight Gain: Pregabalin treatment may cause weight gain. Pregabalin-associated weight gain was related to dose and duration of exposure but did not appear to be associated with baseline body mass index, gender, or age. Weight gain was not limited to patients with edema.
Ophthalmic Effects: Inform patients to notify their health care provider if changes in vision occur. If visual disturbance persists, consider further assessment. Consider more frequent assessment for patients who are already routinely monitored for ocular conditions.
Creatine Kinase Elevations: Pregabalin treatment was associated with creatine kinase elevations. Instruct patients to promptly report unexplained muscle pain, tenderness, or weakness, particularly if these muscle symptoms are accompanied by malaise or fever. Discontinue pregabalin treatment if myopathy is diagnosed or suspected or if markedly elevated creatine kinase levels occur.
Decreased Platelet Count: Pregabalin treatment was associated with a decrease in platelet count.
PR Interval Prolongation: Pregabalin treatment was associated with PR interval prolongation.
Hypersensitivity Reactions: Adverse reactions included blisters, dyspnea, hives, rash, skin redness, and wheezing. Discontinue pregabalin immediately in patients with these symptoms.

Pregnancy: Pregnancy category: C.
There are no adequate and well-controlled studies in pregnant women. Use pregabalin during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Lactation: It is not known if pregabalin is excreted in human milk; decide whether to discontinue breastfeeding or the drug, taking into account the importance of the drug to the mother.

CNS: Abnormal coordination, abnormal gait, abnormal thinking, amnesia, anxiety, asthenia, ataxia, attention disturbance, balance disorder, confusion, depersonalization, depression, disorientation, dizziness, dysarthria, erectile dysfunction, euphoria, headache, hypertonia, hypesthesia, incoordination, irritability, lethargy, libido decreased, memory impairment, myasthenia, myoclonus, nervousness, neuropathy, paresthesia, somnolence, speech disorder, stupor, tremor, twitching, vertigo.
Dermatologic: Pruritus.
GI: Abdominal distention, abdominal pam, constipation, diarrhea, dry mouth, flatulence, gastroenteritis, nausea, vomiting.
Hematologic/Lymphatic: Ecchymosis.
Metabolic/Nutritional: Edema, face edema, fluid retention, hypoglycemia, increased appetite, peripheral edema, weight gain.
Special Senses: Abnormal vision, blurry vision, conjunctivitis, diplopia, eye disorder, nystagmus, otitis media, tinnitus.
Musculoskeletal: Arthralgia, back pain, leg cramps, muscle spasms, myalgia, pain.
Respiratory: Bronchitis, pharyngolaryngeal pain, sinusitis.
GU: Anorgasmia, impotence, urinary frequency, urinary incontinence.
Miscellaneous: Accidental injury, allergic reaction, chest pain, dyspnea, fatigue, feeling abnormal, feeling drunk, fever, flu syndrome, infection.

CNS depressants (e.g., ethanol, lorazepam, and oxycodone): Although no pharmacokinetic interactions were seen, additive effects on cognitive and gross motor functioning occurred when pregabalin was coadministered with these drugs. No clinically important effects on respiration were seen.
Angiotensin-converting Enzyme Inhibitors: Increased risk of developing angioedema.
Anticonvulsants: Concomitant administration of gabapentin with pregabalin did not alter pharmacokinetics of gabapentin although the rate, but not the extent, of absorption of pregabalin was decreased slightly.
Antidiabetic Agents: Coadministration of pregabalin and a thiazolidinedione may lead to an additive effect on edema and weight gain and/or fluid retention, possibly exacerbate or leading to heart failure.

Do not store above 30°C.

Anticonvulsants / Drugs for Neuropathic Pain / Antipsychotics

N02BF02 - pregabalin ; Belongs to the class of gabapentinoids. Used to relieve pain and other conditions.

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