Each capsule contains: Pregabalin 75 mg.
Pregabalin (Pregasafe) is described chemically as (S)-3-(aminomethyl)-5-methylhexanoic acid. The molecular formula is C8H17NO2 and the molecular weight is 159.23. Pregabalin (Pregasafe) is a white to off-white, crystalline solid with a pKal of 4.2 and a pKa2 of 10.6. It is freely soluble in water and both basic and acidic aqueous solutions. The log of the partition coefficient (n-octanol/0.05M phosphate buffer) at pH 7.4 is - 1.35.
Pharmacology: Pharmacodynamics/Pharmacokinetics: Pregabalin (Pregasafe) is a structural analog of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA). It has been reported that its action presents the function of modulating the release of many excitatory neurotransmitters such as glutmate, norepinephrine, substance-P and calcitonin gene related peptide. This modulation can cause an inhibitory modulation of overexcited neurons allowing them to get back to a normal state, including the decrease on the hyperexcitability caused by tissue damage. The neurotransmitter modulation allows pregabalin to present antiallodynic, anxiolytic and anticonvulsant activity.
Pregabalin (Pregasafe) is rapidly absorbed after oral doses and peak plasma concentrations are achieved within 1.5 hours. Oral bioavailability is about 90%. The rate but not the extent of absorption is reduced if given with food but this is not clinically significant. Steady state is achieved after 1 to 2 days. Pregabalin (Pregasafe) is not bound to plasma proteins and undergoes negligible metabolism. About 98% of a dose is excreted in the urine as unchanged drug. The mean elimination half-life is 6.3 hours. Pregabalin (Pregasafe) removed by hemodialysis.
Used as an adjunct in the treatment of partial seizures with or without secondary generalization; also used in the treatment of generalized anxiety disorder (GAD), neuropathic pain and fibromyalgia; postherpetic neuralgia.
Partial seizure: Initially 75 mg bid. May be increased to 300 mg/day after 1 week. Max: 600 mg/day after another week.
GAD: Initially 75 mg bid. May be increased to 450 mg/day after 1 week. Max: 600 mg/day after another week.
Neuropathic pain: Initially 75 mg bid. May be increased to 300 mg/day after an interval of 3-7 days. Max: 600 mg/day after an additional 7-day interval.
Fibromyalgia: Start at 75 mg bid, may be increased to 150 mg bid within 1 week. May be further increase to 225 mg bid for insufficient pain relief. Max 600 mg/day.
Postherpetic neuralgia: Initially 150 mg/day bid. May be increased to 300 mg/day bid after one week as needed.
No specific antidote is recommended for Pregabalin (Pregasafe) overdose. If indicated, emesis or gastric lavage may be attempted to eliminate the unabsorbed drug. Usual precaution must be observed to maintain the patency of airway. General supportive care with proper monitoring of the patient's vital signs and overall clinical status is warranted. A certified poison control center should be notified for up-to-date information on the management of overdose with Pregabalin (Pregasafe).
Hypersensitivity. Pregnancy, lactation. Driving or working with machines or doing other dangerous activities. Pregabalin (Pregasafe) is contraindicated in patients with moderate to severe hepatic impairment (Child-Pugh Class B or C).
Discontinue treatment if patients develop severe angioedema. Withdraw treatment gradually over at least 1 week. May cause peripheral edema. Regular vision check is recommended. May decrease platelet count and prolong PR interval. Liver aminotransferase concentrations should be measured before starting therapy, at monthly intervals during therapy, and 2 weeks after any increase in dose.
Contraindicated in pregnancy & lactation.
The most common adverse effects reported during therapy with pregabalin are dizziness and somnolence. Other common adverse effects include blurred vision, diplopia, increased appetite and weight gain, dry mouth, constipation, vomiting, flatulence, euphoria, confusion, reduced libido, erectile dysfunction, irritability, vertigo, ataxia, tremor, dysarthria, paraesthesia, fatigue, and edema. Disturbances of attention, memory, coordination, and gait were observed.
May potentiate the effects of ethanol and lorazepam. May cause respiratory failure and coma with other CNS depressants. May cause additive cognitive and gross motor impairment with oxycodone.
Store at temperatures not exceeding 30°C. Protect from light and moisture.
Shelf-Life: 24 months.
N03AX16 - pregabalin ; Belongs to the class of other antiepileptics.