Rockost

Uses

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

Magnesium sulfate injection is used for the following conditions:

Convulsions (treatment) - Intravenous Magnesium sulfate injection is used for immediate control of life-threatening convulsions in the treatment of severe toxemias (pre-eclampsia and eclampsia) of pregnancy and in the treatment of acute nephritis in children.

Hypomagnesemia (prophylaxis and treatment) - Magnesium sulfate injection is used for replacement therapy in magnesium deficiency, especially in acute hypomagnesemia accompanied by signs of tetany similar to those of hypocalcemia.

Magnesium sulfate injection is also used to prevent or treat magnesium deficiency in patients receiving total parenteral nutrition.

Tetany, uterine (treatment) - Magnesium sulfate injection is used for uterine tetany as a myometrial relaxant.

No FDA- or EMA-approved therapeutic indications on its own.

Rockost is also used to associated treatment for these conditions: Acid indigestion, Colic, Constipation, Dyspepsia, Flatulence, Gastric Ulcer, Heartburn, Upset stomach, Antacid therapy, Gastric Acid SuppressionConstipation, Convulsions, Hypomagnesemia, Torsades de Pointes, Barium poisoning, Severe Exacerbation of asthma, Bowel preparation therapy, Soaking aid for minor sprains and bruisesConjunctivitis, Stye, Ulceration of the mouth, Oral Hygiene, Irrigation of the ocular surface therapy

How Rockost works

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.

Magnesium is the second most plentiful cation of the intracellular fluids. It is essential for the activity of many enzyme systems and plays an important role with regard to neurochemical transmission and muscular excitability. Magnesium sulfate reduces striated muscle contractions and blocks peripheral neuromuscular transmission by reducing acetylcholine release at the myoneural junction. Additionally, Magnesium inhibits Ca²⁺ influx through dihydropyridine-sensitive, voltage-dependent channels. This accounts for much of its relaxant action on vascular smooth muscle.

Information regarding the mechanism of action of boric acid in mediating its antibacterial or antifungal actions is limited. Boric acid inhibits biofilm formation and hyphal transformation of Candida albicans, which are critical virulence factors . In addition, arrest of fungal growth was observed with the treatment of boric acid .

Dosage

Rockost 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.

Intramuscular:Adults and older children: For severe hypomagnesemia, 1 to 5 g (2 to 10 mLof 50% solution) daily in divided doses; administration is repeated daily until serum levels have returned to normal. If deficiency is not severe, 1 g (2 mL of 50% solution) can be given once or twice daily. Serum magnesium levels should serve as a guide to continued dosage.

Intravenous:1 to 4 g magnesium sulfate (magnesium sulfate (magnesium sulfate injection) injection) may be given intravenously in 10% to 20% solution, but only with great caution; the rate should not exceed 1.5 mL of 10% solution or equivalent per minute until relaxation is obtained.

Intravenous Infusion:4 g in 250 mL of 5% Dextrose Injection at a rate not exceeding 3 mL per minute.

Usual Dose Range:1 to 40 g daily.

Electrolyte Replenisher:Intramuscular 1 to 2 g in 50% solution four times a day until serum magnesium is within normal limits.

Usual Pediatric Dose:Intramuscular 20 to 40 mg per kg of body weight in a 20% solution repeated as necessary.

For Eclampsia:Initially 1 to 2 g in 25% or 50% solution is given intramuscularly. Subsequently, 1 g is given every 30 minutes until relief is obtained. The blood pressure should be monitored after each injection.

Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.

Side Effects

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

Flushing, sweating, sharply lowered blood pressure, hypothermia, stupor and ultimately, respiratory depression.

Toxicity

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.

LD₅₀ = 1200 mg/kg (rat, subcutaneous). May be harmful if swallowed. May act as an irritant. Adverse reactions include hypotension, ECG changes, diarrhea, urinary retention, CNS depression and respiratory depression.

The acute oral LD₅₀ in rats is 4500-5000 mg/kg and the intradermal LD₅₀ in rabbits is 10,000 mg/kg. Individuals are likely to be exposed to boric acid from industrial manufacturing or processing. Local tissue injury from boric acid exposure is likely due to caustic effects. Systemic effects from boric acid poisoning usually occur from multiple exposures over a period of days and involve gastrointestinal, dermal, CNS, and renal manifestations. Gastrointestinal toxicity include persistent nausea, vomiting, diarrhea, epigastric pain, hematemesis, and blue-green discoloration of the feces and vomit . Following the onset of GI symptoms, a characteristic intense generalized erythroderma follows . Management of mild to moderate toxicity should be supportive. In case of severe toxicity, dialysis may be required in addition to supportive treatment.

Precaution

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

Renal impairment, myasthaenia gravis, digitalised patients; pregnancy. Monitor serum-magnesium concentrations.

Interaction

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

Volume of Distribution

The peak action and distribution of magnesium hydroxide are variable.

Volume of distribution ranges from 0.17 to 0.5 L/kg in humans, where large amounts of boric acid are localized in brain, liver, and kidney .

Elimination Route

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

Boric acid is well absorbed from the gastrointestinal tract, open wounds, and serous cavities but displays limited absorption in intact skin . Following intraperitoneal injection in mice, the peak concentration was reached in about 1.0-1.5 hr in the brain whereas the value was 0.5 hr in other tissues .

Half Life

N/A

43.2 hours (for newborns)

According to human cases of poisoning, the elimination half-life of boric acid ranges from 13 to 24 hours .

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.

A case report of acute boric acid poisoning following oral ingestion of 21 g of boric acid presents the total body clearance of 0.99 L/h before hemodialysis .

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.

Magnesium is excreted solely by the kidney at a rate proportional to the serum concentration and glomerular filtration.

Regardless the route of administration, boric acid predominantly undergoes rapid renal excretion of >90% of total administered dose as unchanged form. Small amounts are also excreted into sweat, saliva, and feces. Following administration as ointment, urinary excretion of boric acid accounted for only 1% of the administered dose .

Pregnancy & Breastfeeding use

Pregnancy category- A.

Pregnancy category B. Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).

Contraindication

Intestinal obstruction, faecal impaction; renal failure; appendicitis.

Heart block, severe renal impairment, myocardial damage.

Acute Overdose

Symptoms of hypermagnesaemia are: respiratory depression and loss of deep tendon reflexes due to neuromuscular blockade; nausea, vomiting, flushing, thirst, hypotension, drowsiness, confusion, slurred speech, double vision, bradycardia and muscle weakness.

Treatment in adults should include IV administration of 5-10 mEq of 10% calcium gluconate. Artificial respiration may be required.

Innovators Monograph

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