LURTOPIN BROMURO DE PINAVERIO 100MG 14 TABS
Each tablet contains:
Pinaverium bromide 100 mg
Excipient, c.b.p. 1 tablet.
THERAPEUTIC INDICATIONS: This is for the treatment of irritable bowel syndrome (IBS) in any of its subtypes, according to the criteria Rome III (constipation predominant, diarrhea-predominant, mixed and unclassifiable), nervous colitis, intestinal colic. This is also indicated in all functional disorders of intestinal motility involving pain and bloating.
Pharmacokinetics IN HUMAN bromide is a calcium antagonist pinaverium different from other conventional types of calcium antagonists, because of its high selectivity for the gastrointestinal smooth muscle, by its dual action mechanism regulating intestinal motility and decreased visceral hypersensitivity . Pinaverium bromide exerts its antispasmodic action of calcium channel blocking voltage-dependent subunit specifically? -1 - And prevents muscle contractions induced by gastrointestinal hormones and mediators such as cholecystokinin (CCK) and substance P. It has also been shown to inhibit the action of serotonin nerve transmission involved in triggering the intestinal contraction. Pinaverium bromide decreases visceral hypersensitivity because it selectively blocks the actions of CCK and substance P in afferent neurons.
Pinaverium bromide diffuses through the mucosa, specifically to the intestinal smooth muscle without being significantly absorbed systemically. Calcium channel "slow" voltage-gated (VOCs "L") are located on the outer surface of the wall of the gastrointestinal muscle cells, reducing the contraction of isolated smooth muscle cells. Pinaverium bromide is a potent selective affinity to join them, so it blocks the entry of calcium through these channels and prevents contractile activity of the intestine. It has been shown in several in vivo and in vitro effect pinaverium bromide on gastrointestinal contractile activity. Unlike calcium channel antagonists conventional Pinaverium Bromide has no clinically relevant activity outside the gastrointestinal tract.
The affinity and the antagonistic action pinaverium bromide are constant and independent of the conditions for activation or resting the intestinal muscle cell. The records of colon myoelectric two hours before eating and three hours later, showed that the bromide pinaverium suppressed postprandial motor response (gastrocolic reflex). Electromanométricas measurements obtained after mechanical stimulation in patients with intestinal motor disturbances showed that pinaverium bromide significantly decreased the motility index, further reducing the duration that the intensity of contractions. Some authors have reported studies in which balloon catheters used to measure intraluminal pressure variations followed by a test meal. The results indicate that Pinaverium Bromide motility reduces overall sigmoid region and in the colon, without affecting the standard propulsive activity.
The effects of bromide pinaverium on transit time, which is relevant to patients with constipation-predominant IBS, have been investigated in some studies, resulting in decreased transit time compared with placebo (p <0.05), mainly through the descending colon and rectosigmoid.
Similar results have been reported in patients with colonic disease who suffer from chronic constipation, pinaverium bromide significantly shortened transit time. Studies in patients with diarrhea-predominant IBS do not show increased motility index pinaverium bromide.
The effect of bromide pinaverium to visceral hypersensitivity has been shown because it prevents contractions induced by hormones and mediators as colecistocininas (CCK) and substance P, which are known to be dependent Ca2 + and sensitive to antagonists of Ca2 +. Studies were conducted on isolated smooth muscle cells, previously contracted by hormones, CCK and substance P where the effect was assessed by measuring the length of the cell in both control and treated cells. Under these experimental conditions, pinaverium bromide showed potent activity with an IC50 of approximately 1 nM. This effect was confirmed in vitro in vivo demonstrating that it has effects on visceral sensitivity. In the presence of inflammation, pinaverium bromide significantly reduces the severity of abdominal pain caused by rectal distension without affecting the recto-colonic inhibitory reflex.
One of the most important pharmacokinetic properties possessed by compounds such as quaternary ammonium derivatives Pinaverium Bromide, is their low bioavailability (less than 0.5%).
The little bromide pinaverium absorbed almost all, binds to plasma proteins portosystemic circulation, thus having an excellent and extensive hepatic metabolism with excretion biliofecal through demethylation of the methoxy group, hydroxylation of the ring and eliminating norpinanil benzyl group with subsequent morpholine ring opening.
The physicochemical characteristics of these compounds, a polar charge permanently activated, allow them to stay in the light of the intestinal tract, thus exerting its action as a muscle relaxant with a topical or local activity practically. The rate of absorption of these compounds through the intestinal mucosa depends basically three ways: passive transport, which is proportional to the concentration of compound in the intestinal lumen, active transport, whose degree of saturation depends on the dose-time, and finally an active secretion system similarly dependent of the dose-time.
The action topical or local pinaverium bromide coupled with selective affinity that this compound has to slow calcium channel "L" voltage-dependent, gives the molecule an effective and normorreguladora spasmolytic activity of intestinal transit, resulting in reducing abdominal pain in 90% of cases (men and women) and over 90% of patients have clinical improvement compared to bloating, constipation, diarrhea, nausea / vomiting.
Hypersensitivity pinaverium bromide.
Use in Pregnancy and Lactation pinaverium bromide practically not absorbed into the systemic circulation, which makes it unlikely the passage of significant concentrations of the drug into the fetal circulation or breast milk, however, the intake the last trimester of pregnancy may cause hypotonia and sedation in the newborn. The use of this medicine during pregnancy and lactation is the responsibility of the physician.
ADVERSE REACTIONS: In some sensitive people can pinaverium bromide abdominal pain, itching, rash, diarrhea, nausea or dry mouth.