Fortasec Plus 2/125 Mg 12 Tablets

Fortasec Plus (2 Mg / 125 Mg 12 Tablets)

ACTION AND MECHANISM

Antidiarrheal antipropulsive. Loperamide binds to the opioid receptor in the intestinal wall, reducing propulsive peristalsis, increasing intestinal transit time, and increasing water and electrolyte reabsorption. Loperamide does not modify the physiological flora, increases the tone of the anal sphincter, and does not act centrally. Loperamide has a high affinity for the intestinal wall and is extensively metabolized in its first liver passage, so that only a very small amount reaches the systemic circulation. Simethicone is an inert surfactant with antifoam properties, with zero systemic absorption.

PHARMACOKINETICS

The half-life of loperamide in humans is 10.8 hours with a range of 9-14 hours. Distribution studies in rats show a high affinity for the intestinal wall, with preference for binding to receptors in the longitudinal muscle layer. In humans, loperamide is well absorbed from the intestine, but is almost completely extracted and metabolized in the liver, where it is conjugated and excreted via the bile. Due to this very high first-pass effect, plasma concentrations of unchanged drug remain extremely low. Excretion takes place mainly through the feces. Simethicone is not absorbed.

INDICATIONS

- Acute [DIARRHEA]: symptomatic treatment of acute diarrhea in adults and adolescents over 12 years of age when acute diarrhea is associated with gas-related abdominal discomfort including gas, cramps or flatulence.

POSOLOGY

- Adults over 18 years: initially two tablets, followed by one tablet after each diarrheal stool. No more than 4 tablets should be taken per day, limited to no more than 2 days.

- Adolescents between 12 and 18 years: initially one tablet, followed by one tablet after each diarrheal stool. No more than 4 tablets should be taken per day, limited to no more than 2 days.

DOSAGE IN KIDNEY INSUFFICIENCY

No dose adjustment is required in renal failure.

DOSAGE IN LIVER INSUFFICIENCY

- Severe: It should be used with caution and only after prescription in patients with severe liver dysfunction due to decreased first-pass metabolism.

RULES FOR CORRECT ADMINISTRATION

chew the tablet completely before swallowing

CONTRAINDICATIONS

- [ALLERGY TO OPIOIDS] or to any component of the drug.

- Bloody diarrhea caused by invasive microorganisms such as enteroinvasive strains of Escherichia coli , Salmonella ([SALMONELOSIS]) or Shigella ([SHIGELOSIS]), or in the case of [PSEUDOMEMBRANOSA COLITIS], caused by broad spectrum antibiotics. In these situations, the use of loperamide is not recommended, since by inhibiting peristalsis it could increase the contact time between the intestinal mucosa and the microbial toxins, increasing the damage. In case of bacterial diarrhea it may be necessary at times to administer antibiotics.

- Situations in which you want to avoid the inhibition of peristalsis, such as [CONSTIPATION], [BOWEL OBSTRUCTION] or [ABDOMINAL DISTENSION], since loperamide could aggravate the process. If any of these symptoms appear during the treatment of diarrhea, it is advisable to stop the treatment.

PRECAUTIONS

- [LIVER FAILURE]. Loperamide is eliminated by the liver, so in case of insufficiency the first-pass metabolism could decrease, with the consequent accumulation of the drug. It may be necessary to readjust the dosage depending on the degree of insufficiency.

- [ULCEROUS COLITIS] or [HIV INFECTION]. In patients with ulcerative colitis or AIDS, the administration of intestinal motility inhibitor antidiarrheals has been associated with an increase in the incidence of toxic megacolon, for which it is advisable to take extreme precautions and suspend treatment in the event of abdominal distension. or other symptoms such as severe abdominal pain, nausea, vomiting, or loss of appetite.

- [DEHYDRATION]. Inhibition of intestinal peristalsis can lead to fluid retention in the intestinal lumen, aggravating dehydration. It is advisable to first correct the patient's dehydration by administering water or oral rehydration solutions.

ADVICE TO THE PATIENT

- It is not advisable to start treatment with an antidiarrheal without consulting a doctor, since the antidiarrheal could worsen the symptoms.

- You should see a doctor if acute diarrhea persists or worsens after two days of treatment.

- A doctor should be consulted in the event that the stools are black, oily, fetid or the presence of blood, mucus or pus is evident. A doctor should also be consulted if a fever over 38 ºC appears in children or 38.5 ºC in adults, or if the patient presents abdominal pain that does not diminish with the stool.

INTERACTIONS

- Cholestyramine. In one study, a possible inhibition of the effect of loperamide has been recorded, so it is recommended to space the administration.

- Laxatives: The administration of antidiarrheals such as loperamide with intestinal bolus-enhancing laxatives such as ispagula, methylcellulose, agar or sterculia gum is not recommended, because the simultaneous use can cause intestinal obstructions with serious results for patients.

- Ritonavir or quinidine (P-glycoprotein inhibitors): possible increase in loperamide Cp. Caution.

- Inhibitors of CYP3A4 (eg ketoconazole or itraconazole) and CYP2C8 (gemfibrozil): possible increase in loperamide Cp. Caution.

- Saquinavir: Possible reduction in Cp of saquinavir with risk of decreased antiviral activity.

- Theophylline. In pharmacokinetic studies, a decrease in theophylline absorption has been observed when administered in controlled-release forms, probably due to inhibition of intestinal motility.

- Opioid analgesics. Its simultaneous use may increase the risk of severe constipation and CNS depression.

PREGNANCY

Safety in animals : in animal studies using doses 30 times higher than human ones, they did not show harm to the fetus. Higher doses alternated maternal and neonatal survival.

Safety in humans : There are no adequate and well-controlled studies in humans. Its administration is only accepted if there are no safer therapeutic alternatives, and the benefits outweigh the possible risks.

Effects on fertility : using doses 150-200 times higher than human ones, it has been shown that loperamide could reduce the fertility of males and females.

LACTATION

It is not known whether loperamide is excreted in significant amounts in human milk, and whether this could affect the child.

KIDS

Safety and efficacy have not been evaluated in children under two years of age, therefore its use is not recommended. In children older than 2 years it is advisable to take extreme precautions since there may be great variability in the pharmacological response, due to dehydration. Similarly, children under 3 years of age are more sensitive to the central opioid effects of loperamide.

ELDERLY

Dehydration associated with diarrhea is especially common in the elderly, so there can be great variability in its effects.

ADVERSE REACTIONS

The adverse effects of loperamide are, in general, infrequent but moderately important. In most cases, adverse reactions are a prolongation of pharmacological action and mainly affect the digestive system, being in most cases indistinguishable from the symptoms of diarrhea itself. These adverse reactions are more common with long-term treatments. The most characteristic adverse reactions are:

- Digestive. In very rare (<0.01%) the appearance of [ABDOMINAL PAIN], [FLATULENCE], [DYSPEPSIA], [NAUSEAS], [VOMITING], [CONSTIPATION], [DRYNESS OF MOUTH], [ABDOMINAL DISTENSION], [PARALITIC ILEUS ] or [TOXIC MEGACOLON].

- Neurological / psychological. [Drowsiness] and [DIZZINESS] are rare (<0.01%). Children are especially sensitive to the nerve effects of loperamide.

- Genitourinary. Occasionally, [URINARY RETENTION] may appear.

- Allergic / dermatological. They are very rare (<0.01%) [EXANTEMATIC ERUPTIONS], [URTICARIA] or [PRURITO]. Isolated cases of [ANGIOEDEMA], [STEVENS-JOHNSON SYNDROME], [ERYTHEMA MULTIFORME] and [TOXIC EPIDERMAL NECROLYSIS] have been reported, although their relationship with loperamide has not been evaluated.

Isolated cases of [HYPERSENSITIVITY REACTIONS], including [ANAPHYLAXY], have also been described.

OVERDOSE

Symptoms: In case of overdose, a depression of the central nervous system can occur, with stupor, drowsiness, miosis, muscular hypertonia and respiratory depression. Urinary retention or ileal atony may also appear. This overdose occurs especially in cases of liver failure or in young children.

Treatment: The patient should be monitored for 48 hours to detect possible central nervous system depressions. In the event of such symptoms, naloxone can be given as an antidote. As the duration of the effects of loperamide is longer than that of naloxone, which does not exceed three hours, the administration of naloxone may have to be repeated. In addition, it may be advisable to administer activated charcoal after taking loperamide in case of accidental ingestion, followed by gastric lavage if vomiting has not occurred.

Prospectus Fortasec Plus 2/125 Mg 12 Tablets