Berlosid

Uses

Dimethicone is an ingredient used to treat dry and irritated eyes.

Dimethicone is a colorless liquid with both cosmetic and therapeutic uses. It is used in topical creams and ointments to help distribute the active ingredients. Dimethicone is used as an anti-foaming agent, a hair and skin conditioner, and in the treatment of head lice and, as an anti-bloating/anti-flatulence agent , .

Acid regurgitation, Constipation, Gastric ulcer, Gastrointestinal hyperacidity, Heartburn, Indigestion, Non ulcer dyspepsia, Osmotic laxative

Berlosid is also used to associated treatment for these conditions: Acute Diarrhoea, Aerophagy, Dry Skin, Duodenal Ulcer, Dyspepsia, Flatulence, Gastric Ulcer, Gastritis, Gastro-esophageal Reflux Disease (GERD), Hiatus Hernia, Pancreatic Insufficiency, Post Operative Gas, Pre-operative Gas, Stress Ulcers, Bowel preparation therapy, Carbohydrate Digestion, Digestive Aid, Fat Digestion, Protein DigestionAcid indigestion, Colic, Constipation, Dyspepsia, Flatulence, Gastric Ulcer, Heartburn, Upset stomach, Antacid therapy, Gastric Acid Suppression

How Berlosid works

When applied topically, dimethicone forms a layer to delay the evaporation of water . In the treatment of head lice dimethicone 100, the respiratory systems of head lice are targeted. NYDA works by suffocating the lice, nymphs and the embryos. The physical properties of this drug, including the viscosity and spreading property of the solution allow it to easily flow into the respiratory system of all developmental stages of the insect, causing suffocation and death of the organisms. It diffuses through the stigmata (spiracles) of the lice, into the tracheae of the head lice as well as through the aeropyles of the egg operculum. The solution then displaces oxygen. The low viscosity, volatile dimethicone enables the NYDA head lice solution to penetrate into the breathing system. Its evaporation causes the thickening of the NYDA solution. The remaining high viscosity dimethicone ultimately encloses the respiratory system and thus leading to suffocation of all stages of head lice (adult lice, larvae and eggs). This mode of action prevents the development of lice resistance by preventing the formation of new progency .

Studies performed using house crickets and lice suggest a close correlation between the death of the lice and the influx of the solution into the insect head tracheae. These data strongly suggest that the total filling of the head tracheae immediately blocks the oxygen supply to the insect central nervous system. Death, following numerous stages of disability after the entrance of dimethicones into the abdominal tracheal system, demonstrates the sequence of oxygen deprivation. NYDA was applied directly to the head and mouth of the organism, and was found to have no effect when applied solely to the outside of the head/mouth .

The suspension of magnesium hydroxide is ingested and enters the stomach. According to the amount ingested, the magnesium hydroxide will either act as an antacid or a laxative.

Through the ingestion of 0.5-1.5 grams (in adults) the magnesium hydroxide will act by simple acid neutralization in the stomach. The hydroxide ions from the magnesium hydroxide suspension will combine with the acidic H+ ions of the hydrochloric acid made by the stomachs parietal cells. This neutralization reaction will result in the formation of magnesium chloride and water.

Through the ingestion of 2-5 grams (in adults) the magnesium hydroxide acts as a laxative in the colon. The majority of the suspension is not absorbed in the intestinal tract and will create an osmotic effect to draw water into the gut from surrounding tissues. With this increase of water in the intestines, the feces will soften and the intraluminal volume of the feces will increase. These effects still stimulate intestinal motility and induce the urge to defecate. Magnesium hydroxide will also release cholecystokinin (CKK) in the intestines which will accumulate water and electrolytes in the lumen and furthermore increase intestinal motility.

Dosage

Berlosid dosage

Gastrointestinal hyperacidity:

• Adult: Up to 1 g daily, usually given in conjunction with an aluminium-containing antacid eg, aluminium hydroxide.

Osmotic laxative:

• Adult: 2.4-4.8 g daily as a single dose or in divided doses.
• Child: 6-11 yr: 1.2-2.4 g daily; 2-5 yr: 0.4-1.2 g daily. Doses may be given as a single dose or in divided doses.

Side Effects

GI irritation, diarrhoea, abdominal cramps; hypermagnesaemia (in patients with renal impairment). Paralytic ileus.

Toxicity

The minimum lethal oral dose of dimethicone 200 (50 cs), dimethicone 550 (75 cs), dimethicone in rats .

A 76-week dietary toxicity study of a silicone antifoam compound (94% polydimethylsiloxane silicone oil and 6% silicone dioxide) was performed in mice. Three groups were given diet containing 0, 0.25%, or 2.5% of the test article. The dose levels in the treatment groups were estimated to be 580 and 5800 mg/kg/day. Mortality was increased in the 5800 mg/kg/day females. No target organs of toxicity were observed. The no-effect dose was 580 mg/kg/day. This study is of limited usefulness for assessing the toxicity of dimethicones, due to the small number of organs/tissues that were examined .

In one clinical study, 145 subjects were treated with either NYDA (dimethicone )or with a permethrin-based lice product. The number of subjects experiencing any adverse events was similar in both groups. In the NYDA group, 29 adverse events were reported in 25 subjects. All except two adverse events were categorized as being unrelated to the lice treatment (e.g., superficial wound after a fall, otitis externa following swimming in a pool). Two patients in the NYDA group experienced ocular irritation after treatment when the product entered the eyes. The irritation resolved spontaneously in both cases after rinsing the eyes with clean water .

LD50=8500 mg/kg (rat, oral)

Common side effects include drowsiness or flushing (warmth, redness or tingly feeling).

Daily use of magnesium hydroxide can result in fluid and electrolyte disturbances.

Excessive use of the laxative effects of magnesium hydroxide may result in abdominal cramping, nausea and/or diarrhea.

In overdose, symptoms of gastrointestinal irritation and/or watery diarrhea may occur.

Magnesium hydroxide poisoning can result in hypermagnesemia which includes symptoms of: nausea, vomiting, flushing, thirst, hypotension, drowsiness, confusion, loss of tendon reflexes, muscle weakness, respiratory depression, cardiac arrhythmias, coma and cardiac arrest.

Not to be used in individuals with any form of kidney disease or renal failure, a magnesium restricted diet or with any sudden changes in bowel movement lasting over two weeks. Also not to be used in those individuals with abdominal pain, nausea, vomiting, symptoms of appendicitis or myocardial damage, heart block, fecal impaction, rectal fissures, intestinal obstruction or perforation or renal disease. Not to be used in women who are about to deliver as magnesium crosses the placenta and is excreted in small amounts in breast milk.

Using magnesium hydroxide with aluminum hydroxide can decrease the absorption rate of these drugs.

Magnesium hydroxide can react with digoxin, dicoumerol and cimetidine.

Use of ibuprofen with magnesium hydroxide can increase the absorption of the ibuprofen.

Use of magnesium hydroxide with penicallamine, bisphosphates, ketoconazole, quinolones or tetracycline can decrease the absorption of these drugs.

Enteric-coated tablets can be prematurely released when taken with magnesium hydroxide.

It is important to routinely monitor levels of serum magnesium and potassium in patients using magnesium hydroxide. Serum magnesium levels are necessary to determine how much magnesium is being absorbed and how much is being excreted by the kidneys. Excessive diarrhea can occur from use of magnesium hydroxide and thus it is important to also monitor serum potassium levels to ensure hypokalemia does not occur.

Precaution

Colostomy, ileostomy; electrolyte imbalance. Monitor for toxicity in patients with impaired renal function. Pregnancy.

Interaction

Decreases absorption of tetracyclines and biphosphonates. Separate administration of these and other drugs by around 2 hr.

Volume of Distribution

Following injection of [14C]dimethicone fluid in the hind limb of rats, the radioactivity was distributed primarily in the gastrointestinal tract, and no evidence of metabolism was observed. When [14C]dimethicone was administered through i.p. injection in rats, the following distribution of radioactivity was observed at 25 days after dosing: 51% in adipose tissue, 27% in gastrointestinal tissues, and 15% in liver .

The peak action and distribution of magnesium hydroxide are variable.

Elimination Route

This drug is not believed to be absorbed when used in quantities from 1-30% .

About 15%-50% of magnesium hydroxide is absorbed very slowly through the small intestine.

Half Life

N/A

Clearance

Magnesium hydroxide is mainly excreted in the urine by the kidneys. Since the kidneys play a major role in its clearance, individuals with renal failure are at risk of hypermagnesemia with long term consumption as the appropriate amounts of magnesium may not be excreted.

Elimination Route

After oral administration, up to 50% of the magnesium hydroxide suspension may be absorbed as magnesium ions through the small intestines and then rapidly excreted in the urine through the kidneys. The unabsorbed drug is mainly excreted in the feces and saliva.

Pregnancy & Breastfeeding use

Pregnancy category- A.

Contraindication

Intestinal obstruction, faecal impaction; renal failure; appendicitis.

Innovators Monograph

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