Neuropathic pain. Linbar drug prescribed for the treatment of neuropathic pain in adults with damage to the peripheral and Central nervous system. Epilepsy. Linbag is prescribed as an additional therapy for partial seizures with or without secondary generalization in adults. Generalized anxiety disorder. The drug Linbag is prescribed for the treatment of generalized anxiety disorder in adults.
Linbag hard capsules 150 mg Composition and form of release
active substance: pregabalin;
1 capsule contains pregabalin 25 mg or 50 mg, 75 mg, 100 mg, or 150 mg, or 200 mg, or 225 mg or 300 mg
excipients: talc, corn starch, corn starch gelatin capsule: gelatin, titanium dioxide (E 171), iron oxide yellow (E172), iron oxide red (E172) *, iron oxide black (E172) **.
* Not contained in 50 mg capsules.
** Contained in capsules of 25 and 300 mg.
Linbag hard capsules 150 mg Release form
Linbag hard capsules 150 mg Pharmacodynamics
The active substance, pregabalin, is an analogue of gamma-aminobutyric acid [(S) -3- (aminomethyl) -5-methylhexanoic acid].
Linbag hard capsules 150 mg Mechanism of action.
Pregabalin binds to an additional subunit (a 2 -d protein) of potential calcium channels in the central nervous system.
Equilibrium pharmacokinetic parameters of pregabalin were similar in healthy volunteers, patients with epilepsy treated with antiepileptic drugs, and patients with chronic pain.
Absorption. Pregabalin is rapidly absorbed when taken on an empty stomach and reaches its maximum plasma concentration within 1:00 after a single and repeated use. The calculated bioavailability of pregabalin after oral administration is 90% or more and does not depend on the dose. After repeated use, the equilibrium state is reached after 24-48 hours. The rate of absorption of pregabalin decreases when taken simultaneously with food, leading to a decrease in the maximum concentration (C max) by about 25-30% and an increase in tmax by about 2.5 hours. However, dietary intake of pregabalin did not have a clinically significant effect on absorption.
Distribution. Preclinical studies have shown that pregabalin crosses the blood-brain barrier in animals. Pregabalin also crosses the placenta in rats and is excreted in milk during lactation. In humans, the apparent volume of distribution of pregabalin after oral administration is approximately 0.56 L / kg. Pregabalin does not bind to blood plasma proteins.
Metabolism. In humans, pregabalin undergoes minor metabolism. After administration of a dose of radioactively labeled pregabalin, about 98% of the radioactive substances are excreted in the urine as unchanged pregabalin. The N-methylated derivative of pregabalin, the main metabolite of the drug, which was detected in the urine, accounted for 0.9% of the administered dose. During preclinical studies, the racemization of the S-enantiomer of pregabalin to the R-enantiomer did not