Pharmacology: Pharmacodynamics: Mechanism of action: Pregabalin binds to alpha2 – delta subunit of voltage-gated calcium channels within the CNS and modulated calcium influx at the nerve terminals, thereby inhibiting excitatory neurotransmitter release including glutamate, norepinephrine (noradrenaline), serotonin, dopamine, substance P and calcitonin gene-related peptide. 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 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 : 1.5 hours (3 hours with food).
Excretion: Urine.
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.
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.
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 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.
Fibromyalgia: The usual dose range for most patients is 300 to 450 mg per day given in two divided doses. Some patients may derive 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 1 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/day after an additional week.
Discontinuation of Pregabalin: If Pregabalin has to be discontinued, it is recommended this should be done gradually over a minimum of 1 week.
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Mode of Administration: Pregabalin may be taken with or without food.
The highest reported accidental overdose of Pregabalin was 8000 mg and on notable clinical consequences.
Pregabalin no specific antidote for overdose. Elimination of unabsorbed drug may be attempted by gastric lavage.
Hypersensitivity to the active substance or to any of the excipients.
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.
Caution in patients with a history of angioedema episodes. Concurrent use with other drugs known to cause angioedema (eg. ACE inhibitors) may increase risk. Hypersensitivity reactions, including skin redness, blistering, hives, rash, dyspnea and wheezing.
Abrupt discontinued with pregabalin has been associated with anxiety, diarrhea, headache, hyperhidrosis, insomnia and nausea.
Pregnancy: Increased incidences of fetal structural abnormalities and other manifestations of developmental toxicity including lethality growth retardation and nervous and reproductive system functional impairment were observed in animal studies.
There are no adequate and well-controlled studies in pregnant women. It is not known if Pregabalin crosses the human placenta. Use Pregabalin during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Lactation: Pregabalin is excreted in breast milk. Breast feeding is not recommended during treatment.
Common: Dizziness and somnolence, ataxia, tremor, amnesia, speech disturbances, myoclonus, neuropathy, confusion, euphoria, incoordination, abnormal gait, nervousness, twitching, headache.
Less common: Peripheral edema, increased liver enzymes, decreased platelet count and increased creatine kinase, rhabdomyolysis and blurred vision.
Pregabalin may increase the levels/effects of: Alcohol (Ethyl), Analgesics (Opioid), Antidiabetic Agent (Thiazolidinedione), Azelastine (Nasal), Blonanserin, Buprenorphine, CNS Depressants, Flunitrazepam, Hydrocodone, Methotrimeprazine, Metyrosine, Mirtazapine, Ophrenadrine, Oxycodone, Paraldehyde, Piribedil, Pramipexole, Ropinirole, Rotigotine, SSRI, Suvorexant, Thalidomide, Zolpidem.
The levels/effects of Pregabalin may be increased by: ACE inhibitors; Brimonidine (Topical), Cannabis, Chlormethiazole, Chlorophenesin carbamate, Dimethindene (Topical), Doxylamine, Dronabinol, Droperidol, Hydroxyzine, Kava kava, Lofexidine, Magnesium sulfate, Methotrimeprazine, Minocycline, Nabilone, Oxomemazine, Perampanel, Rufinamide, Sodium oxybale, Tapentadol, Tetrehydrocannabinol, Trimeprazine.
The levels/effects of Pregabalin may be decreased by: Mefloquine, Mianserin, Orlistat.
N02BF02 - pregabalin ; Belongs to the class of gabapentinoids. Used to relieve pain and other conditions.
Prepentin cap 75 mg
4 × 14's
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