Fortasec 2 Mg 10 Capsules

Fortasec (2 Mg 10 Capsules)

Loperamide Hydrochloride

ACTION AND MECHANISM

- [ANTIDIARRHEAL], [OPIACEOUS AGONIST (MU)]. Derived from pethidine. Opioid µ receptor agonist, which inhibits the release of acetylcholine and prostaglandins in the myenteric plexus of Auerbach, reducing intestinal peristalsis. By reducing intestinal transit, it favors the absorption of water and electrolytes, reducing the frequency and quantity of bowel movements, and increasing their viscosity. It also has a certain antisecretory effect. It also increases the tone of the anal sphincter, reducing incontinence.

PHARMACOKINETICS

- Absorption: It is absorbed in the intestine, presenting a bioavailability of 40%. You suffer from first-pass metabolism. Cmax is reached after 5 hours (capsules) or 2.5 hours (solutions). Its effects last up to 24 hours.

- Distribution: Circulates bound to plasma proteins (97%). It crosses the blood-brain barrier with great difficulty.

- Metabolism: It is metabolized in the liver, giving rise to inactive metabolites.

- Elimination: It is eliminated by metabolism, the metabolites being excreted with the feces (30% unchanged), and in a very small amount with the urine (<2%). Its elimination half-life is about 10 hours. The fraction of loperamide eliminated in the intestine can be reabsorbed, leading to an enterohepatic cycle.

Pharmacokinetics in special situations:

- Hepatic insufficiency: The metabolism of loperamide can be diminished in case of hepatic insufficiency, leading to a decrease in hepatic clearance.

INDICATIONS

- [DIARRHEA]. Symptomatic treatment of acute or chronic diarrheal processes.

POSOLOGY

- Adults, oral:

* Acute diarrhea: Initial 4 mg will be administered, followed by 2 mg after each bowel movement.

* Chronic diarrhea: Initial 4 mg will be administered, and then 2-12 mg / 24 hours until 1-2 daily bowel movements are achieved.

The maximum daily dose is 16 mg.

- Children, oral:

* Children over 5 years old:

a) Acute diarrhea: Initial 2 mg will be administered, followed by 2 mg after each bowel movement.

b) Chronic diarrhea: Initial 2 mg will be administered, followed by the dose necessary to achieve 1-2 daily bowel movements.

* Children 2-5 years: Initially 0.4 ml / kg / 24 hours, up to a maximum of 1.2 ml / kg / 24 hours. The treatment will be suspended at the moment in which the stools are normal or have not been them in 12 hours.

* Children under 2 years of age: The safety and efficacy of loperamide in children under 2 years of age have not been evaluated.

The maximum daily dose is 6 mg / 20 kg.

DOSAGE IN KIDNEY INSUFFICIENCY

No dose adjustment is required.

DOSAGE IN LIVER INSUFFICIENCY

There are no specific dosage recommendations. Caution is advised as your first-pass metabolism may be slowed.

RULES FOR CORRECT ADMINISTRATION

It is advisable to divide the doses of loperamide into two to three doses when administered for chronic diarrhea.

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 [PSEUDOMEMBRANOUS 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 inhibiting 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 via 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 exercise extreme caution 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.

PRECAUTIONS RELATING TO EXCIPIENTS

- This medicine contains lactose. Patients with hereditary [LACTOSE INTOLERANCE] or galactose, Lapp lactase deficiency, or glucose or galactose malabsorption should not take this medicine.

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 if the stools are black, oily, fetid or the presence of blood, mucus or pus is evident. You should also see a doctor 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.

SPECIAL WARNINGS

- The administration of loperamide to patients with diarrhea does not exclude adequate hydration of the patient, so it is advisable to administer fluids such as water, infusions or oral rehydration solutions in the necessary amounts. Symptoms such as thirst, dry mouth and skin or decreased urine volume are clear signs of dehydration.

- It is not advisable to administer loperamide to dehydrated patients before correcting dehydration

INTERACTIONS

- Cholestyramine. In one study, a possible inhibition of the effect of loperamide has been recorded, for which reason 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.

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

- Saquinavir: Possible reduction of the 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, extreme precautions are advised 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.

SENIORS

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], [NAUSEA], [VOMITING], [CONSTIPATION], [DRY MOUTH], [ABDOMINAL DISTENSION], [PARALITIC ILEUS ] or [TOXIC MEGACOLON].

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

- Genitourinary. On certain occasions, [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 2 Mg 10 Capsules