Balentin

Balentin

pregabalin

Manufacturer:

Millimed

Distributor:

Prosp Pharma

Marketer:

Prosp Pharma
Full Prescribing Info
Contents
Pregabalin.
Description
Each BALENTIN 75 and BALENTIN 150 capsule contains Pregabalin 75 mg and Pregabalin 150 mg, respectively.
Action
Pharmacology: Pharmacodynamics: Pregabalin binds to alpha2-delta subunit of voltage-gated calcium channels within the CNS and modulates calcium influx at the nerve terminals, thereby inhibiting excitatory neurotransmitter release including glutamate, norepinephrine (noradrenaline), serotonin, dopamine, substance P, and calcitonin gene-related peptide. Although structurally related to GABA, it does not bind to GABA or benzodiazepine receptors. Exerts antinociceptive and anticonvulsant activity. Pregabalin may also affect descending noradrenergic and serotonergic pain transmission pathways from the brainstem to the spinal cord.
Pharmacokinetics: Onset of action: Pain management: Effects may be noted as early as the first week of therapy.
Distribution: Vd: 0.5 L/kg.
Protein binding: 0%.
Metabolism: Negligible.
Bioavailability: >90%.
Half-life elimination: 6.3 hours.
Time to peak, plasma: Immediate-release: Median: 0.7 hours fasting (range: 0.7 to 1.5 hours), 3 hours with food.
Excretion: Urine (90% as unchanged drug; minor metabolites).
Indications/Uses
Neuropathic pain: Pregabalin is indicated for treatment of central and peripheral neuropathic pain in adult which include 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 Disorder: Pregabalin is indicated for the treatment of Generalized Anxiety Disorder (GAD) in adults.
Fibromyalgia: Pregabalin is indicated for the management of fibromyalgia.
Dosage/Direction for Use
Recommended Dose: 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 dose may be increased to 300 mg per day after an interval of 3 to 7 days, and if needed, to a maximum dose of 600 mg per day after an additional 7-day interval.
Epilepsy: Pregabalin treatment can be started with a dose of 150 mg per day. Based on 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: The dose range is 150 to 600 mg per day given as two or three divided doses. The need for treatment should be reassessed regularly.
Pregabalin treatment can be started with a dose of 150 mg per day. Based on 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: The usual dose range for most patient is 300 to 450 mg per day given in two divided doses. Some patients may drive additional benefit at 600 mg per day. Dosing should begin at 75 mg two times a day (150 mg/day) and may be increased to 150 mg two times a day (300 mg/day) within one week based on efficacy and tolerability. Patients who do not experience sufficient benefit with 300 mg/day may be further increased to 225 mg two times a day (450 mg/day). If needed, in some patients, based on individual response and tolerability, the dose may be increased to maximum dosage of 600 mg per day after an additional week.
Discontinuation of pregabalin: If pregabalin has to be discontinued, it is recommended that this should be done gradually over a minimum of 1 week.
Patients with renal impairment: Dose reduction in patients with compromised renal function must be individualized according to creatinine clearance (CLCR), as indicated in Table 1 determined using the following formula: See Equation.

Click on icon to see table/diagram/image

For patients receiving hemodialysis, the pregabalin daily dose should be adjusted based on renal function. In addition to the daily dose, a supplementary dose should be given immediately following every 4-hour hemodialysis treatment (see Table).

Click on icon to see table/diagram/image

Use in patients with hepatic impairment: No dose adjustment is required for patients with hepatic impairment.
Use in children and adolescents (12 to 17 years of age): The safety and effectiveness of pregabalin in pediatric patients below the age of 12 years and adolescents has not been established.
The use in children is not recommended.
Use in elderly (over 65 years of age): Elderly patients may require a dose reduction of pregabalin due to a decreased renal function.
Mode of Administration: Pregabalin capsules are administered orally without regard to meals. May be administered with or without food.
Overdosage
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. Contact a certified poison control center for up-to-date information on the management of overdose with pregabalin. Although hemodialysis has not been performed in the few known cases of overdose, it 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).
Contraindications
Known hypersensitivity to pregabalin or any ingredient in the formulation.
Warnings
This drug may cause drowsiness, so should not operate vehicles or machinery and should not drink alcohol or anything with alcohol while taking this drug.
This drug may cause blood cells disorder.
Do not use this drug in pregnant women because it may cause fetal abnormalities.
Should be careful using this drug in patients with liver disease, kidney disease.
Special Precautions
Pooled analysis if trials involving various antiepileptics (regardless of indication) showed an increased risk of suicidal thoughts/behavior; risk observed as early as one week after initiation and continued through duration of trials. Monitor all patients for notable changes in behavior that might indicate suicidal thoughts or depression; notify healthcare provider immediately if symptoms occur.
Angioedema has been reported during initial and chronic treatment; may be life threatening; use with caution in patients with a history of angioedema episodes. Concurrent use with other drugs known to cause angioedema (eg, ACE inhibitors) may increase risk. Discontinue treatment immediately if angioedema occurs.
Hypersensitivity reactions, including skin redness, blistering, hives, rash, dyspnea and wheezing; discontinue treatment if hypersensitivity occurs.
Dizziness and somnolence are commonly reported; effects generally occur shortly after initiation and occur more frequently at higher doses. Patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).
Visual disturbances (blurred vision, decreased acuity and visual field changes) have been associated with pregabalin therapy; patients should be instructed to notify their physician if these effects are noted.
Pregabalin has been associated with increase in creatine kinase and rare cases of rhabdomyolysis. Patients should be instructed to notify their prescriber if unexplained muscle pain, tenderness, or weakness, particularly if fever and/or malaise are associated with these symptoms. Discontinue treatment if myopathy is suspected or diagnosed or if markedly elevated creatine kinase levels occur.
Use may cause weight gain; weight gain generally associated with dose and duration (average weight gain was 5.2 kg for diabetic patients receiving pregabalin for ≥ 2 years); weight gain was not limited to patients with edema and did not appear to be associated with baseline BMI, gender, age, or loss of glycemic control in diabetic patients.
Use may cause peripheral edema; use with caution in patient with heart failure (NYHA Class III or IV) due to limited data in this patient population. In addition, effect on weight gain/edema may be additive with the thiazolidinedione class of antidiabetic agents; use caution when coadministering these agents, particularly in patients with prior cardiovascular disease. In a scientific statement from the American Heart Association, pregabalin has been determined to be an agent that may exacerbate underling myocardial dysfunction (magnitude: minor and moderate).
May decrease platelet count or prolong PR interval.
Has been noted to be tumorigenic (increased incidence of hemangiosarcoma) in animal studies; significance of these findings in humans is unknown.
Anticonvulsants should not be discontinued abruptly because of the possibility of increasing seizure frequency; therapy should be withdrawn gradually unless safety concerns require a more rapid withdrawal. Tapering over at least 1 week is recommended. Abrupt discontinued with pregabalin has been associated with anxiety, diarrhea, headache, hyperhidrosis, insomnia and nausea.
Use caution in renal impairment; dosage adjustment required.
Use with caution in patients with a history of substance abuse; potential for behavioral dependence in this population exists.
Potentially significant drug-drug interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy.
Use In Pregnancy & Lactation
Pregnancy: Category C.
Pregabalin crosses the human placenta. Outcome data following maternal use of pregabalin during pregnancy is limited. Data is currently insufficient to recommend use in pregnant woman.
Do not use this drug in pregnant women because it may cause fetal abnormalities.
Lactation: Pregabalin is present in breast milk. Breastfeeding is not recommended.
Adverse Reactions
Cardiovascular: Chest pain, edema, facial edema, hypertension, hypotension, peripheral edema, prolongation P-R interval on ECG.
CNS: Abnormal gait, abnormality in thinking, anmesia, anorgasmia, anxiety, ataxia, confusion, depersonalization, disorientation, disturbance in attention, dizziness, drowsiness, equilibrium disturbance, euphoria, fatigue, feeling abnormal, headache, hypertonia, hypoesthesia, insomnia, intoxicated feeling, lethargy, memory impainnent, myasthenia, nervousness, neuropathy, pain, paresthesia, sedation, speech disturbance, stupor, twitching (includes myokymia), vertigo.
Dermatologic: Contact dermatitis, decubitus ulcer, ecchymoses, pruritus.
Endocrine & metabolic: Decreased libido, fluid retention, hypoglycemia, weight gain.
Gastrointestinal: Abdominal distension, abdominal pain, constipation, diarrhea, flatulence, gastroenteritis, increased appetite, nausea, viral gastroenteritis, vomiting, xerostomia.
Genitourinary: Erectile dysfunction, impotence, urinary frequency, urinary incontinence, urinary tract infection.
Hematologic & oncologic: Thrombocytopenia.
Hepatic: Increased serum ALT, Increased serum AST.
Neuromuscular & skeletal: Arthralgia, back pain, increased creatine phosphokinase, joint  swelling,  limb pain, leg cramps, muscle spasm, myalgia, neck pain, tremor, weakness.
Ophthalmic: Blurred vision, conjunctivitis, decreased visual acuity, diplopia, eye disease, nystagmus, visual disturbance, visual field loss.
Otic: Otitis media, tinnitus.
Respiratory: Bronchitis, cough, dyspnea, flu-like symptoms, nasopharyngitis, pharyngolaryngeal pain, respiratory tract infection, sinusitis.
Miscellaneous: Accidental injury, fever.
Drug Interactions
Avoid concomitant use of Pregabalin with any of the following: Azelastine (Nasal); Bromperidol; Orphenadrine; Oxomemazine; Paraldehyde; Thalidomide.
Pregabalin may increase the level/effects of: Alcohol (Ethyl); Azelastine (Nasal); Blonanserin; Buprenorphine; CNS Depressants; Flunitrazepam; Hydrocodone; Methotrimeprazine; Metyrosine; Mirtazapine; Opioid Analgesics; Orphenadrine; Oxycodone; Paraldehyde; Piribedil; Pramipexole; Ropinirole; Rotigotine; Selective Serotonin Reuptake Inhibitors; Suvorexant; Thalidomide; Thiazolidinediones; Zolpidem.
The levels/effects of Pregabalin may be increased by: Angiotensin-Converting Enzyme Inhibitors; Brimonidine (Topical); Bromperidol; Cannabis; Chlormethiazole; Chlorphenesin Carbamate; Dimethindene (Topical); Doxylamine; Dronabinol; Droperidol; Hydroxyzine; Kava Kava; Lofexidine; Magnesium sulfate; Methotrimeprazine; Minocycline; Nabilone; Oxomemazine; Perampanel; Rufinamide; Sodium Oxybate; Tapentadol; Tetrahydrocannabinol; Trimeprazine.
The level/effect of Pregabalin may be decreased by: Mefloquine; Mianserin; Orlistat.
Storage
Store below 30°C.
ATC Classification
N03AX16 - pregabalin ; Belongs to the class of other antiepileptics.
Presentation/Packing
Cap 75 mg (red-white, no. 4 filled with white powder) x 4 x 14's. 150 mg (opaque white, no. 2 filled with white powder) x 4 x 14's.
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