Each capsule contains Pregabalin 75 mg and 150 mg.
Pharmacology: Pharmacodynamics: 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: Absorption/Distribution: Pregabalin is well absorbed after oral administration. Following oral administration of pregabalin under fasting conditions, peak plasma concentrations (Cmax) occur within 1.5 hours. Steady state is achieved within 24 to 48 hours.
Pregabalin does not bind to plasma proteins. The distribution of pregabalin following oral administration is approximately 0.5 L/kg. Pregabalin is a substrate for system L transporter, which is responsible for the transport of large amino acids across the blood-brain barrier.
Metabolism/Excretion: Pregabalin undergoes negligible metabolism in humans. Approximately 90% of the administered dose was recovered in the urine as unchanged pregabalin.
Pregabalin is eliminated from the systemic circulation primarily by renal excretion as unchanged drug, with a mean elimination half-life of 6.3 hours in subjects with normal renal function. Because pregabalin is not bound to plasma proteins, this clearance rate indicates that renal tubular reabsorption is involved.
Breastfeeding Women: Small amounts of pregabalin have been detected in the breast milk. In a pharmacokinetic study, pregabalin concentrations in plasma and breast milk of 10 lactating women (at least 12 weeks postpartum) taking pregabalin 150 mg oral capsules every 12 hours (a total of 4 doses) were evaluated. Pregabalin concentrations in breast milk were about 76% of those in maternal plasma and the estimated average daily infant dose of pregabalin from breast milk was about 7% of the maternal dose. The effect of pregabalin on milk production and breasted infant were not evaluated.
For the management of neuropathic pain associated with diabetic peripheral neuropathy or with spinal cord injury and postherpetic neuralgia in adults.
As an adjunct in the treatment of partial seizures with or without secondary generalization in adults.
For the treatment of generalized anxiety disorder in adults. For the management of fibromyalgia in adults.
Recommended Dose: Pregabalin is given orally in 2 or 3 divided doses daily.
For neuropathic pain the initial dose is 150 mg daily increased after 3 to 7 days according to response to 300 mg daily and then to 600 mg daily after another 7 days. Similar doses are used for the treatment of neuropathic pain in diabetic neuropathy postherpetic neuralgia, and spinal cord injury, although a maximum daily dose of 300 mg is recommended in diabetic neuropathy because dosages up to 600 mg daily were evaluated with no significant additional benefit and an increase in adverse effects. The initial dose in the treatment of epilepsy is 150 mg daily increased after 1 week according to response to 300 mg daily and then to 600 mg daily after another week.
In the treatment of generalized anxiety disorder, the initial dose is 150 mg daily; this may be increased at weekly intervals in steps of 150 mg, to a maximum of 600 mg daily.
For fibromyalgia the initial dose is 150 mg daily increased after 1 week according to response to 300 mg daily and then to 450 mg daily if necessary.
When discontinuing, taper off gradually over at least 1 week. (See table.)
Click on icon to see table/diagram/image
Post-hemodialysis supplementary dosage (as a single additional dose): 25 mg/day schedule: Single supplementary dose of 25 mg or 50 mg.
25-50 mg/day schedule: Single supplementary dose of 50 mg or 75 mg.
50-75 mg/day schedule: Single supplementary dose of 75 mg or 100 mg.
75 mg/day schedule: Single supplementary dose of 100 mg or 150 mg.
Dosage adjustment in hepatic impairment: No dosage adjustment expected since undergoes minimal hepatic metabolism.
Mode of Administration: Pregabalin may be administered with or without food.
Overdose and treatment: Overdose effects are expected to be extensions of adverse effects at therapeutic doses. In patients receiving greater than or equal to 900 mg, the clinical events reported were similar to those at the recommended doses. An adult ingested an estimated 1.5 g; mild drowsiness was the only symptom observed. An adult intentionally ingested 8.4 g of pregabalin and developed CNS depression and coma approximately 3 hours after exposure. The patient required intubation and mechanical ventilation for 26 hours. No permanent sequelae occurred. Treatment of pregabalin exposure is largely supportive in nature with careful attention to airway protection in severe cases. Consider activated charcoal if ingestion was recent. Hypotension is usually mild responding to intravenous fluid boluses. If hypotension persists, administer dopamine or norepinephrine. Admit all severely symptomatic patients. Treat seizures with IV benzodiazepines or barbiturates. Hemodialysis might be useful in patients with severe toxicity or those with significant renal impairment. Standard hemodialysis results in pregabalin clearance of approximately 50% in 4 hours. Dialysis is rarely necessary as most patients do well with supportive care.
Hypersensitivity to pregabalin or any component of the formulation.
Angioedema: There have been postmarketing reports of angioedema in patients during initial and long-term treatment with pregabalin. Specific symptoms included swelling of face, mouth (gums, lips, and tongue), and neck (larynx and throat). There were reports of life-threatening angioedema with respiratory compromise requiring emergency treatment. Discontinue pregabalin immediately in patients with these symptoms.
Discontinuation: Withdraw pregabalin gradually to minimize the potential of increased seizure frequency in patients with seizure disorders. If pregabalin is discontinued, this should be done gradually over a minimum of 1 week.
Suicidal behavior and ideation: Antiepileptic drugs (AEDs), including pregabalin, increase the risk of suicidal thoughts or behavior in patients taking these drugs for any indication. Monitor patients treated with any AED for any indication for the emergence of worsening of depression, suicidal thoughts or behavior, and any unusual changes in mood or behavior.
Peripheral edema: Pregabalin treatment may cause peripheral edema.
CNS effects: Pregabalin may cause dizziness and somnolence.
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.
Ophthalmological effects: In controlled studies, a higher proportion of patients treated with pregabalin reported blurred vision (7%) than patients treated with placebo (2%), which resolved in a majority of cases with continued dosing.
Congestive heart failure: Because there is limited data on congestive heart failure patients with New York Heart Association Class III or IV cardiac status, use pregabalin with caution in these patients.
Creatine kinase elevations, decreased platelet count, PR interval prolongation: Pregabalin treatment was associated with creatine kinase elevations, a decrease in platelet count, and mild PR interval prolongation.
Hypersensitivity reactions: There have been postmarketing reports of hypersensitivity in patients shortly after initiation of treatment with pregabalin. Adverse reactions included blisters, dyspnea, hives, rash, skin redness, and wheezing. Discontinue pregabalin immediately in patients with these symptoms.
Hazardous tasks: Pregabalin may cause dizziness and somnolence. Pregabalin-related dizziness and somnolence may impair abilities to perform tasks such as driving or operating machinery.
Use in Children: Safety and efficacy not established in children younger than 18 years of age.
Pregnancy: Category C.
Adverse events were observed in animal reproduction studies. In addition, male-mediated teratogenicity has been observed in animal reproduction studies; implications in humans are not defined. Impaired male and female fertility have been noted in animal studies.
Lactation: Pregabalin is excreted in the milk of lactating women (see Pharmacology: Pharmacokinetics: Breastfeeding Women under Actions). As the safety of pregabalin in infants is not known, breastfeeding is not recommended during treatment with pregabalin. A decision must be made whether to discontinue breastfeeding or to discontinue from pregabalin therapy taking into account the benefit of breastfeeding for the child and the benefit of therapy for the woman.
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 (occasionally severe), vomiting, flatulence, euphoria, confusion, reduced libido, erectile dysfunction, irritability, vertigo, ataxia, tremor, dysarthria, paraesthesia, fatigue, and oedema. Disturbances of attention, memory, coordination, and gait also occur frequently. Syncope and congestive heart failure have been reported less frequently. Reversible renal failure, raised liver enzymes, elevation of creatine kinase concentration, and rhabdomyolysis have been reported rarely. Breast enlargement and gynecomastia have also been reported. Hypersensitivity reactions have occurred shortly after starting pregabalin therapy; symptoms include rash, blisters, urticaria, dyspnoea, and wheezing. Stevens-Johnson syndrome has also been reported. An increased incidence of haemangiosarcoma occurred in mice that had been given high doses of pregabalin.
Drugs that may interact with pregabalin include ACE inhibitors, CNS depressants (e.g., lorazepam, ethanol, oxycodone), and thiazolidinediones.
Angiotensin-converting Enzyme Inhibitors: Potential pharmacologic interaction with angiotensin-converting enzyme (ACE) inhibitors (e.g., increased risk of developing angioedema).
CNS depressants: Potential pharmacologic interaction (e.g., additive CNS depressant effects) with concurrent administration of CNS depressants, including opiates and benzodiazepines.
Lorazepam, Ethanol, Oxycodone: Pharmacokinetic interaction unlikely. Potential pharmacologic interaction (e.g., additive effects on cognitive and gross motor functioning); no clinically important effects on respiration.
Thiazolidinediones: Potential pharmacologic interaction with thiazolidinediones (e.g., increased risk of weight gain and peripheral edema.
N02BF02 - pregabalin ; Belongs to the class of gabapentinoids. Used to relieve pain and other conditions.
Pregalin cap 150 mg
4 × 14's
Pregalin cap 75 mg
4 × 14's
Sign Out
Click on icon to see table/diagram/image
