Бисакодил-Акрихин

Uses

Бисакодил-Акрихин is used for Constipation; Preparation for radiography; antepartum & postpartum care; Preparation for sigmoidoscopy or proctoscopy; colonoscopy; hemorrhoids & anal fissures. All conditions which require defecation to be facilitated.

Бисакодил-Акрихин is also used to associated treatment for these conditions: Constipation, Occasional Constipation, Bowel irregularity, Bowel preparation therapy

How Бисакодил-Акрихин works

Бисакодил-Акрихин is deacetylated to the active bis-(p-hydroxyphenyl)-pyridyl-2-methane (BHPM) by an intestinal deacetylase. BHPM can stimulate parasympathetic nerves in the colon directly to increase motility and secretions.

Бисакодил-Акрихин stimulates adenylate cyclase, increasing cyclic AMP, leading to active transport of chloride and bicarbonate out of cells. Sodium ions, potassium ions, and water passively leave the cell; while sodium and chloride ions are unable to be reabsorbed.

Water is also be transported from the luminal side of cells into the vasculature by aquaporin 3. Бисакодил-Акрихин decreases expression of aquaporin 3, preventing water from moving into the vasculature, which may contribute to increased water in the colon.

Бисакодил-Акрихин directly stimulates parasympathetic nerves in the colon, stimulating contraction of longitudinal smooth muscle but not circular smooth muscle.

Dosage

Бисакодил-Акрихин dosage

Constipation:

• Adult: 1-2 tab (5-10 mg) daily, relief in 6-12 hr.
• Adult/Pediatric: 1 suppository (10 mg) daily, relief in 15-30 min.
• Children <10 yr: 1 tab (5 mg) or 1 suppository (5 mg) daily.

For complete bowel clearance:

• >10 yr: 2-4 tab the night before & 1 adult suppository on the day of the procedure.
• <10 yr: 1 tab the night before & 1 pediatric suppositoryon the day of the procedure.

The max daily dose should not be exceeded.

Side Effects

Abdominal discomfort & diarrhea.

Toxicity

Patients experiencing an overdose of bisacodyl may present with more severe diarrhea and electrolyte imbalance. Patients should be treated with symptomatic and supportive measures.

The oral LD₅₀ in rats is 4320 mg/kg, and in mice is 17500 mg/kg.

Precaution

Caution should be taken in pregnancy and children.

Interaction

Do not give antacids or milk within 1 hour of taking the drug (enteric coated)

Food Interaction

• Avoid milk and dairy products. Take at least 1 hour before or after antacids and milk.
• Take separate from antacids. Take at least 1 hour before or after antacids and milk.

Бисакодил-Акрихин Drug Interaction

Moderate: furosemide, magnesium hydroxide, polyethylene glycol 3350, ondansetronUnknown: aspirin, lorazepam, diphenhydramine, docusate, duloxetine, omega-3 polyunsaturated fatty acids, sodium biphosphate / sodium phosphate, atorvastatin, pregabalin, metoprolol, acetaminophen / hydrocodone, acetaminophen, cyanocobalamin, ascorbic acid, cholecalciferol, cetirizine

Бисакодил-Акрихин Disease Interaction

Major: inflammatory bowel disease, intestinal obstruction disorders, acute surgical abdomen, rectal bleeding

Volume of Distribution

Data regarding the volume of distribution of bisacodyl is not readily available. However, the volume of distribution of the active metabolite, BHPM, in lactating women is 181 L after a single dose and 289 L at steady state.

Elimination Route

Oral formulations of bisacodyl are only 16% bioavailable. A 10 mg enteric coated oral tablet reaches a C_max of 26 ng/mL with a T_max of 8 hours, while a 10 mg oral solution reaches a C_max of 237 ng/mL with a T_max of 1.7 hours. A 10 mg suppository reaches a C_max of 0-64 ng/mL.

In lactating women, 10mg of oral bisacodyl reaches a C_max of 20.5-195 ng/mL, with a T_max of 3-4 hours, and a geometric mean AUC after a single dose of 471 h*ng/mL. After multiple doses, the geometric mean AUC decreases to 311 h*ng/mL.

Half Life

Data regarding the half life of bisacodyl is not readily available. The half life of the active metabolite, BHPM, in lactating women was 7.3 h after a single 10 mg oral dose and 10.0 h after multiple doses.

Clearance

Data regarding the clearance of bisacodyl is not readily available. The apparent plasma clearance of the active metabolite, BHPM, in lactating women after a single 10 mg oral dose is 272 mL/min and after multiple doses is 412 mL/min.

Elimination Route

The majority of bisacodyl is eliminated in the feces. 13.8-17.0% of a bisacodyl dose is eliminated in the urine as the active metabolite BHPM.

Pregnancy & Breastfeeding use

Бисакодил-Акрихин has been assigned to pregnancy category B by the FDA. Animal studies have failed to reveal evidence of teratogenicity or fetotoxicity. No data are available from controlled human pregnancy studies. Бисакодил-Акрихин should only be given during pregnancy when need has been clearly established.

It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when HalfLytely and Бисакодил-Акрихин Tablets Bowel Prep Kit is administered to a nursing woman.

Contraindication

Бисакодил-Акрихин is contraindicated in ileus, intestinal obstruction, acute surgical abdominal conditions, severe dehydration. Appendicitis & acute inflammatory bowel diseases.

Acute Overdose

A laxative is a medicine used to produce bowel movements. Laxative overdose occurs when someone takes more than the normal or recommended amount of this medicine. This can be by accident or on purpose.

Most laxative overdoses in children are accidental. However, some people regularly take overdoses of laxatives to try to lose weight.

Storage Condition

Store at room temperature, between 15°C to 30°C. Store in a tightly closed container away from heat, moisture, and light.

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