Pregabalin, methylcobalamin.
Each capsule contains: Pregabalin 75 mg, Methylcobalamin 750 mcg.
Pharmacology: Pharmacodynamics: Pregabalin: Pregabalin, is a gamma-aminobutyric acid analogue ((S)-3-(aminomethyl)-5-methylhexanoic acid). Pregabalin binds to an auxiliary subunit (α2-δ protein) of voltage-gated calcium-channels in the central nervous system, potently displacing [3H]-gabapentin.
Methylcobalamin: Methylcobalamin is one of the two coenzyme forms of vitamin B12 (the other being adenosylcobalamin). It is a cofactor in the enzyme methionine synthase which functions to transfer methyl groups for the regeneration of methionine from homocysteine.
Pharmacokinetics: Pregabalin: Pregabalin is rapidly absorbed when administered in the fasted state, with peak plasma concentrations occurring within 1 hour. Oral bioavailability is estimated to be 90% and is independent of dose. Food results in a decrease in Cmax by 25-30% and a delay in tmax to ~2.5 hours. However, administration of pregabalin with food has no clinically significant effect on the extent of pregabalin absorption. The apparent volume of distribution of pregabalin is 0.56 l/kg. Pregabalin is not bound to plasma proteins. Pregabalin undergoes negligible metabolism. 98% of unchanged pregabalin is recovered in urine. The N-methylated derivative of pregabalin is the major metabolite. Pregabalin is eliminated from the systemic circulation primarily by renal excretion as unchanged drug. Pregabalin mean elimination half-life is 6.3 hours.
Methylcobalamin: Methylcobalamin is utilized more efficiently than cyanocobalamin to increase levels of one of the coenzyme forms of vitamin B12. The quantity of cobalamin detected following a small oral dose of methylcobalamin is similar to the amount following administration of cyanocobalamin; but significantly more cobalamin accumulates in liver tissue following administration of methylcobalamin. Human urinary excretion of methylcobalamin is about one-third that of a similar dose of cyanocobalamin, indicating substantially greater tissue retention.
It is used in the treatment of neuropathic pain.
Pregabalin and Methylcobalamin combination is given orally with or without food as recommended by the physician. The usual recommended dose of Pregabalin 75 mg and Hydrochlorothiazide 750 mcg capsules twice daily. The dosage may be adjusted depending on the patient's age and severity of symptoms.
Mode of Administration: Oral.
In overdoses up to 15 g, no unexpected adverse reactions were reported. The most commonly reported adverse events observed when pregabalin was taken in overdose included somnolence, confusional state, agitation and restlessness. Treatment of pregabalin overdose should include general supportive measures and may include haemodialysis if necessary.
Hypersensitivity to the active substances or to any of the excipients.
Some diabetic patients who gain weight on pregabalin treatment may need to adjust hypoglycaemic medications. Pregabalin should be discontinued immediately if symptoms of angioedema, such as facial, perioral or upper airway swelling occur. Pregabalin treatment has been associated with dizziness and somnolence which could increase the occurrence of accidental injury (fall) in the elderly population. Visual adverse reactions have also been reported, including vision loss, visual blurring or other changes of visual acuity, many of which were transient. After discontinuation of short-term and long-term treatment with pregabalin withdrawal symptoms have been observed in some patients.
There are no adequate data on the use of pregabalin in pregnant women. Pregabalin should not be used during pregnancy unless clearly necessary. Breast-feeding is not recommended during treatment with pregabalin.
The adverse events most frequently leading to discontinuation of the treatment were dizziness, somnolence, ataxia, confusion, asthenia, abnormal thinking, blurred vision, incoordination and peripheral edema. Other adverse events reported are increased appetite, euphoric mood, irritability, decreased libido, tremor, dysarthria, memory impairment, paraesthesia, sedation, balance disorder, lethargy, vertigo, flushing, hot flushes, hypotension, hypertension, dry mouth, constipation, flatulence, etc.
Since pregabalin is predominantly excreted unchanged in the urine, undergoes negligible metabolism in humans (<2% of a dose recovered in urine as metabolites), does not inhibit drug metabolism in vitro and is not bound to plasma proteins, it is unlikely to produce or be subject to pharmacokinetic interactions.
Store below 30°C. Protect from light and moisture.
N03AX16 - pregabalin ; Belongs to the class of other antiepileptics.
Cap 75 mg (red/white coloured "2" size capsules with micro/micro printed on capsule shells containing white powder) x 3 x 10's.
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