Calcium, Magnesium, Lysine, Zinc, Manganese, Copper, Boron, Selenium & Vitamin D3 Tablets

Each tablet contains:

Coral calcium (elemental Calcium) …….............500mg

Magnesium (elemental)……..................................75mg

As Magnesium carbonate

L-Lysine HCL............…………….........................30mg

Zinc (elemental)………...………………………...12mg

As zinc sulphate

Manganese (elemental)………………………….....4mg

As Manganese chloride

Copper (elemental)…………..................................1.7mg

As copper sulphate

Boron………………………………..........................1mg

Selenium (elemental)……………………………..40mcg

As Sodium selenite

Vitamin D3……......................................................400IU

(from lichen source)

Tablet.

Calcium 500mg, Magnesium 75mg, Lysine 30mg, Zinc 12mg, Manganese 4mg, Copper 1.7mg, Boron 1mg, Selenium 40mcg, Vitamin D3 400IU

4.1 Therapeutic Indication

Calcium supplementation & Supports immunity

4.2 Posology and Method of Administration

One tablet daily after meal for adult

4.3 Contraindications 

• Hypersensitivity to the active substance or to any of the excipients listed in the formulation.
• Diseases and/or conditions resulting in hypercalcemia and/or hypercalciuria (e.g. myeloma, bone metastases or other malignant bone disease, sarcoidosis; primary hyperparathyroidism).
• Nephrolithiasis/nephrocalcinosis
• Severe renal impairment and renal failure
• Hypervitaminosis D
• Hypersensitivity to the active substances or to any of the excipients present in this tablet.
• Relative contra-indications are osteoporosis due to prolonged immobilization, renal stones, and severe hypercalciuria.

4.4 Special warnings and precautions for use 

• Patients who are already taking thiazide diuretics and/or cardiac glycosides should be referred to their doctor prior to concomitant use (i.e. not suitable for pharmacy supply). Concomitant use should be prescribed with caution due to the increased risk of hypercalcemia.
• During long-term treatment, serum calcium levels should be followed and renal function should be monitored through measurements of serum creatinine. Monitoring is especially important in elderly patients on concomitant treatment with cardiac glycosides or diuretics and in patients with a high tendency to calculus formation. In case of hypercalcemia or signs of impaired renal function, the dose should be reduced or the treatment discontinued. It is advisable to reduce or interrupt treatment temporarily if urinary calcium exceeds 7.5 mmol/24 h (300 mg/24 h).
• Vitamin D should be used with caution in patients with impairment of renal function and the effect on calcium and phosphate levels should be monitored. The risk of soft tissue calcification should be taken into account. In patients with severe renal insufficiency, vitamin D in the form of cholecalciferol is not metabolized normally and other forms of vitamin D should be used.
• Coralium-D3 forte tablets should be prescribed with caution to patients suffering from sarcoidosis, due to the risk of increased metabolism of vitamin D into its active form. These patients should be monitored with regard to the calcium content in serum and urine.
• Coralium-D3 forte tablets should be used with caution in immobilized patients with osteoporosis due to the increased risk of hypercalcemia.
• The content of vitamin D (500 IU) in Coralium-D3 forte tablets should be considered when prescribing other medicinal products containing vitamin D. Additional doses of calcium or vitamin D should be taken under close medical supervision. In such cases, it is necessary to monitor serum calcium levels and urinary calcium excretion frequently. Milk-alkali syndrome (Burnett's syndrome), i.e. hypercalcemia, alkalosis, and renal impairment can develop when large amounts of calcium are ingested with absorbable alkali.
• Allowances should be made for calcium and vitamin D supplements from other sources.
• Whilst taking Coralium-D3 forte tablets, both protein and energy are also required to provide complete nutrition in the daily diet. No other vitamins, minerals or supplements with or without vitamin A should be taken with this preparation except under medical supervision.
• Do not take Coralium-D3 forte tablets on an empty stomach. Do not exceed the stated dose. Keep out of the reach of children. If symptoms persist, consult your doctor.

4.5 Drugs interactions 

• Thiazide diuretics reduce the urinary excretion of calcium. Due to the increased risk of hypercalcemia, serum calcium should be regularly monitored during the concomitant use of thiazide diuretics.
• Systemic corticosteroids reduce calcium absorption. During concomitant use, it may be necessary to increase the dose of Coralium D3 forte tablets.
• Simultaneous treatment with ion exchange resins such as cholestyramine or laxatives such as paraffin oil may reduce the gastrointestinal absorption of vitamin D.
• Calcium carbonate may interfere with the absorption of concomitantly administered tetracycline preparations. For this reason, tetracycline preparations should be administered at least two hours before or four to six hours after oral intake of calcium.
• Hypercalcaemia may increase the toxicity of cardiac glycosides during treatment with calcium and vitamin D. Patients should be monitored with regard to electrocardiogram (ECG) and serum calcium levels.
• If a bisphosphonate or sodium fluoride is used concomitantly with Coralium D3 forte tablets, these medicinal products should be administered at least three hours before the intake of Coralium D3 forte tablet since gastrointestinal absorption may be reduced.
• Rifampicin, phenytoin, or barbiturates may reduce the activity of vitamin D3, since they increase the rate of its metabolism.
• The absorption of quinolone antibiotics may be impaired if administered concomitantly with calcium. Quinolone antibiotics should be taken two hours before or six hours after intake of calcium.
• Calcium salts may decrease the absorption of iron, zinc or strontium. Consequently, the iron, zinc or strontium preparation should be taken at a distance of two hours from the calcium preparation.
• Calcium salts may reduce the absorption of the estramustin or thyroid hormones. It is recommended that taking CoraliumD3 forte tablets be spaced at least 2 hours from these medicines.
• Oxalic acid (found in spinach, sorrel and rhubarb), phosphate, and phytic acid (found in whole cereals) may inhibit calcium absorption through the formation of insoluble compounds with calcium ions. The patient should not take calcium products within two hours of eating foods high in oxalic acid and phytic acid.
• Zinc Sulphate reduce the absorption of tetracyclines

4.6 Use in special populations

Pregnancy

Coralium-D3 forte tablets may be given during pregnancy in cases of calcium and vitamin D3 deficiency.

During pregnancy the daily dose should not exceed 1500 mg of calcium and 600 IU of vitamin D. Animal studies have shown toxic effects on reproduction at high doses of vitamin D. In pregnant women, all calcium or vitamin D overdose must be avoided as prolonged hypercalcemia in pregnancy may lead to retardation of physical and mental development, supravalvular aortic stenosis and retinopathy in the child. There are no indications that Vitamin D3 at therapeutic doses is teratogenic in humans.

Breast-feeding

Coralium-D3 forte tablets can be used during breast-feeding. Calcium and vitamin D pass into breast milk. This should be considered when giving additional vitamin D to the child.

Coralium-D3 forte tablets may be administered during pregnancy and lactation at the recommendation of the physician.

4.7 Effects on ability to drive and use machines

There are no data on the effect of this product on driving capacity and use of machines. An effect is, however, unlikely.

4.8 Undesirable effects

Adverse reactions are listed below, by system organ class and frequency. Frequencies are defined as: uncommon (>1/1,000 to <1/100); rare (>1/10,000 to <1/1,000); very rare (<1/10,000); not known (cannot be estimated from the available data).

• Immune system disorders
  • Not known: Hypersensitivity reactions including pruritus, wheezing, urticaria, and oropharyngeal swelling have been reported in the post-marketing environment.
• Metabolism and nutrition disorders
  • Uncommon: Hypercalcaemia and hypercalciuria.
  • Very rare: Seen usually only in overdose, see 4.9: Milk-alkali syndrome
• Gastrointestinal disorders
  • Rare: Constipation, flatulence, nausea, vomiting, abdominal pain, and diarrhea.
  • Very rare: Dyspepsia
• Skin and subcutaneous disorders
  • Rare: Pruritus, rash and urticaria.
• Other special population
  • Patients with renal impairment: potential risk of hyperphosphatemia, nephrolithiasis, and nephrocalcinosis.

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via email to: medico@zuventus.com

Website: https://www.zuventus.com/drug-safety-reporting

4.9 Overdose

No cases of overdosage due to Calcium-D3 forte therapy have been reported.

If overdose of calcium and vitamin-D3 suspected can lead to hypervitaminosis and hypercalcemia. Symptoms of hypercalcemia may include anorexia, thirst, nausea, vomiting, constipation, abdominal pain, muscle weakness, fatigue, mental disturbances, polydipsia, polyuria, bone pain, nephrocalcinosis, renal calculi, and in severe cases, cardiac arrhythmias. Extreme hypercalcemia may result in coma and death. Persistently high calcium levels may lead to irreversible renal damage and soft tissue calcification.

Milk-alkali syndrome may occur in patients who ingest large amounts of calcium and absorbable alkali. Symptoms are frequent urge to urinate, continuing headache, continuing loss of appetite, nausea or vomiting, unusual tiredness or weakness, hypercalcemia, alkalosis, and renal impairment.

Treatment of Calcium-D3 forte Overdosage

The following steps are recommended to minimise or prevent further absorption of the medication:

1. Administer an emetic.
2. Gastric lavage may be necessary to remove drug already released into the stomach. Keep the patient under constant surveillance to detect possible aspiration of vomitus; maintain suction apparatus and standby emergency oxygen in case of need.
3. A drink of mannitol or sorbitol should be given to induce small bowel emptying.
4. Any fluid or electrolyte imbalance should be corrected.

Treatment of hypercalcemia

The treatment with calcium and vitamin D must be discontinued. Treatment with thiazide diuretics, lithium, vitamin A, vitamin D, and cardiac glycosides must also be discontinued. Emptying of the stomach in patients with impaired consciousness. Rehydration, and, according to severity, isolated or combined treatment with loop diuretics, bisphosphonates, calcitonin, and corticosteroids. Serum electrolytes, renal function, and diuresis must be monitored. In severe cases, ECG and CVP should be followed.

5.1 Pharmacodynamic properties/ Mechanism of Action

Calcium, combination with vitamin D3

Calcium is an essential body electrolyte. It is involved in the maintenance of normal muscle and nerve function and essential for normal cardiac function and the clotting of blood. Calcium is mainly found in the bones and teeth. Deficiency of calcium leads to rickets, osteomalacia in children and osteoporosis in the elderly.

Vitamin D increases the intestinal absorption of calcium. Administration of calcium and vitamin D3 (cholecalciferol) counteracts the increase of parathyroid hormone (PTH), which is caused by calcium deficiency and causes increased bone resorption.

Magnesium Magnesium is essential to the body as a constituent of skeletal structures and in maintaining cell integrity and fluid balance. It is utilised in many of the functions in which calcium is concerned but often exerts the opposite effect. Some enzymes require the magnesium ion as a co-factor.

Lysine

Lysine is an essential amino acid that is primarily used for protein synthesis. Lysine helps in synthesis of connective tissues such as bone, skin, collagen, and elastin; synthesis of carnitine and resultant conversion of fatty acids to energy; support for healthy growth and development in children; and maintenance of healthy immune function. Lysine has been shown to increase iron absorption in vivo.

Zinc

Zinc is an essential trace mineral necessary for the proper function of about 300 different enzymes. Zinc is important for wound healing, immune system support, digestion, energy production, growth, cellular repair, collagen synthesis, bone strength, cognitive function, and carbohydrate metabolism (glucose utilization and insulin production). Zinc not only modulates cell-mediated immunity but is also an antioxidant and anti-inflammatory agent.

Manganese

Manganese is an essential element for humans and is required for growth, development, and maintenance of health. Manganese is necessary for skeletal system development, energy metabolism and immunological system function. It is an antioxidant that protects cells from damage due to free radicals. Manganese also plays an essential role in regulation of cellular energy, bone and connective tissue growth and blood clotting.

Copper

Traces of copper are essential to the body as constituents of enzyme systems involved in oxidation reactions.

Boron

Boron is a trace element which might have beneficial effects on functions such as reproduction and development, calcium metabolism, bone formation, brain function, insulin and energy substrate metabolism, immunity, and the function of steroid hormones (including vitamin D and estrogen).

Selenium

Selenium is an essential trace element, deficiency of which has been reported in man. It is thought to be involved in the functioning of membranes and the synthesis of amino acids. Deficiency of selenium in the diet of experimental animals produces fatty liver followed by necrosis.

5.2 Pharmacokinetic properties

Calcium

Absorption:

The bioavailability of coral calcium is approximately 70% as per study in animals by Japanese Dietetic Society. This is higher as compared to other calcium salts. Unlike lime and fossilized calcium which are inert, live coral produces calcium in its ionized form. This calcium is able to bypass the digestive process. Hence, calcium and other trace minerals from coral are immediately available to the systems in the human body.

Distribution and metabolism:

99% of the calcium in the body is concentrated in the hard structure of bones and teeth. The remaining 1% is present in the intra- and extracellular fluids. About 50% of the total blood-calcium content is in the physiologically active ionized form with approximately 10% being complexed to citrate, phosphate, or other anions, the remaining 40% being bound to proteins, principally albumin.

Elimination:

Calcium is eliminated through feces, urine, and sweat. Renal excretion depends on glomerular filtration and calcium tubular reabsorption.

Vitamin D

Absorption:

Vitamin D3 is absorbed in the small intestine.

Distribution and metabolism:

Cholecalciferol and its metabolites circulate in the blood bound to a specific globulin. Cholecalciferol is converted in the liver by hydroxylation to the active form 25-hydroxy cholecalciferol. It is then further converted in the kidneys to 1,25hydroxycolecalciferol. 1,25 hydroxy cholecalciferol is the metabolite responsible for increasing calcium absorption. Vitamin D which is not metabolized is stored in adipose and muscle tissues.

Elimination:

Vitamin D is excreted in feces and urine.

Magnesium

Magnesium salts are poorly absorbed from the gastro-intestinal tract; however, sufficient magnesium will normally be absorbed to replace deficiency states. Magnesium is excreted in both the urine and the faeces but excretion is reduced in deficiency states.

Lysine

Lysine absorbed from the lumen of the small intestine into the enterocytes by an active transport process.

Zinc Sulphate

Zinc is poorly absorbed from the gastro-intestinal tract. It is widely distributed throughout the body. It is excreted in the faeces with traces appearing in the urine.

Manganese Sulphate

Manganese salts are poorly absorbed

Copper

Copper is absorbed from the gastro-intestinal tract and its major route of excretion is in the bile.

Boron

Most ingested boron is hydrolyzed to boric acid within the gastrointestinal tract. The body absorbs about 85%–90% of ingested boron. However, very little is known about how or where in the gastrointestinal tract absorption occurs.

Selenium

Although it has been established that selenium is essential to human life, very little information is available on its function and metabolism.

6.1 Animal Toxicology or Pharmacology

At doses far higher than the human therapeutic range teratogenicity has been observed in animal studies. There are further no pre-clinical data of relevance to the prescriber which are additional to that already included in other sections of the prescribing information.

Coralium D3 forte tablets contain a comprehensive formula of calcium and vitamin D3 with multi-minerals and anti-oxidant specially designed to support health and wellbeing in adults by unlocking energy and strengthening immunity. Most vitamins, minerals and trace elements are not produced by human body and hence are dependent on dietary supply of these nutrients. Since vitamins, minerals and trace elements are involved in many metabolic processes in the body, an adequate supply of these vital substances contribute to physical and mental well-being.

8.1 Incompatibilities

Not applicable.

8.2 Shelf-life

Refer on the pack

8.3 Packaging information

10 tablets per pack

8.4 Storage and handing instructions

Store in a dry place at a temperature not exceeding 30°C, protect from light & moisture.

• Take this tablet with food. Take with a full glass of water.
• This tablet need to be taken as Recommended by Healthcare professional. (Don’t exceed the recommended daily usage).
• This tablet is not intended to diagnose, treat, cure or prevent any disease.
• This tablet is not to be used as a substitute for a varied diet

Do not take Coralium D3 forte tablets: 

• if you are allergic (hypersensitive) to any of the ingredients of Coralium D3 forte tablets
• if you suffer from hypercalcaemia (high level of calcium in the blood)
• Do not give Coralium D3 forte tablets to children aged under 12.

Take special care with Coralium D3 forte tablets

Before you are given Coralium D3 forte tablets tell your doctor, dietician or pharmacist if:

• you are pregnant or thinking of becoming pregnant
• you are a smoker
• you have kidney disease, bone disease, malignancies or calcium disorders

If any of the above applies to you, or if you are not sure, speak to your doctor or pharmacist before taking Coralium D3 forte tablets.

Taking other medicines

Tell your doctor if you are taking or have recently taken/used any of the following medicines as they may interfere with Coralium D3 forte tablets:

• Phenytoin (used to treat epilepsy)
• Tetracycline antibiotics (used to treat infections) such as doxycycline and minocycline
• Thiazide diuretics

Please tell your doctor if you are taking or have recently taken/used any other medicines including other vitamin or mineral products medicines obtained without a prescription.

July 2024

Cefixime oral suspension IP

Each 5 ml of reconstituted suspension contains:

Cefixime IP (as Trihydrate)

equivalent to Cefixime (Anhydrous) 100 mg

Excipients q.s.

Colour: Quinoline Yellow WS

Oral Suspension

100mg/5ml

4.1 Therapeutic indication

• Uncomplicated Urinary Tract Infections
• Otitis Media
• Pharyngitis and Tonsillitis
• Acute Exacerbations of Chronic Bronchitis
• Uncomplicated Gonorrhea (cervical/urethral)
• For the treatment of enteric (typhoid) fever.

4.2 Posology and method of administration

Pediatric Patients (6 months or older)

The recommended dose is 8 mg/kg/day of the suspension. This may be administered as a single daily dose or may be given in two divided doses, as 4 mg/kg every 12 hours.

Children weighing more than 45 kg or older than 12 years should be treated with the recommended adult dose, 200 to 400 mg daily depending on the severity of infection.

In the treatment of infections due to Streptococcus pyogenes, a therapeutic dosage of cefixime should be administered for at least 10 days.

Safety and effectiveness of cefixime in children aged < 6months old have not been established.

Suggested Doses for Pediatric Patients

Children weighing more than 45 kg or older than 12 years should be treated with the recommended adult dose, 200 to 400 mg daily depending on the severity of infection. In the treatment of infections due to Streptococcus pyogenes, a therapeutic dosage of cefixime should be administered for at least 10 days.

Safety and effectiveness of cefixime in children aged less than six months old have not been established.

Renal Impairment

Cefixime may be administered in the presence of impaired renal function. Doses for patients with renal impairment is shown in the table 1.

Table 1: Doses for Patient with Renal Impairment

In patients whose creatinine clearance is less than 20 ml/min, it is recommended that a dose of 200 mg once daily should not be exceeded. The dose and regimen for patients who are maintained on chronic ambulatory peritoneal dialysis or haemodialysis should follow the same recommendation as that for patients with creatinine clearance of less than 20 ml/min. Neither haemodialysis nor peritoneal dialysis removes significant amounts of drug from the body.

Directions for reconstitution

• Shake the bottle well to loosen the powder.
• Slowly add part quantity of SWFI provided with this pack up to the ring mark on the bottle & shake well.
• Add more SWFI if necessary to adjust the volume up to the ring mark on the bottle.
• This makes 30/50 ml of the suspension.
• The reconstituted suspension should be consumed within 7 days of preparation.

4.3 Contraindications

Known allergy to cefixime or other cephalosporins.

4.4 Special warnings and precautions for use

Hypersensitivity Reactions

Anaphylactic/anaphylactoid reactions (including shock and fatalities) have been reported with the use of cefixime. If this product is to be given to penicillin sensitive patients, caution should be exercised because cross hypersensitivity among beta-lactam antibiotics has been clearly documented and may occur in up to 10% of patients with a history of penicillin allergy. If an allergic reaction to Cefixime for oral suspension occurs, discontinue the drug.

Clostridium difficile-Associated Diarrhea

Clostridium difficile associated diarrhea has been reported with use of Cefixime oral suspension. If CDAD is suspected or confirmed, ongoing antibiotic use not directed against C.difficile may need to be discontinued. Appropriate fluid and electrolyte management, protein supplementation, antibiotic treatment of C.difficile, and surgical evaluation should be instituted as clinically indicated.

Coagulation Effects

Cephalosporins, including Cefixime for oral suspension may be associated with a fall in prothrombin activity. Prothrombin time should be monitored in patients at risk and exogenous vitamin K administered as indicated.

4.5 Drugs interactions

Carbamazepine

Elevated carbamazepine levels have been reported in postmarketing experience when cefixime is administered concomitantly. Drug monitoring may be of assistance in detecting alterations in carbamazepine plasma concentrations.

Warfarin and Anticoagulants

Increased prothrombin time, with or without clinical bleeding, has been reported when cefixime is administered concomitantly.

4.6 Use in special populations

Pregnancy

Pregnancy Category B

Reproduction studies have been performed in mice and rats at doses up to 40 times the human dose and have revealed no evidence of harm to the fetus due to cefixime. There are no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

Labor and Delivery

Cefixime has not been studied for use during labor and delivery. Treatment should only be given if clearly needed.

Nursing Mothers

It is not known whether cefixime is excreted in human milk. Consideration should be given to discontinuing nursing temporarily during treatment with this drug.

4.7 Effects on ability to drive and use machines

Cefixime has no or negligible influence on the ability to drive or use machines. However, cefixime may cause side effects influencing the capacity of reaction and the ability to drive and use machines.

4.8 Undesirable effects

Acute generalized exanthematous pustulosis and Mouth Ulceration has been seen with Cefixime use.

The most commonly seen adverse reactions were gastrointestinal events, which were reported in 30% of adult

patients on either the twice-daily or the once daily regimen. Individual adverse reactions included diarrhoea (16%), loose or frequent stools (6%), abdominal pain (3%), nausea (7%), dyspepsia (3%), and flatulence (4%).

Diarrhoea has been more commonly associated with higher doses. Other gastrointestinal side effects seen less frequently are vomiting and flatulence. The incidence of gastrointestinal adverse reactions, including diarrhoea and loose stools, in paediatric patients receiving the suspension was comparable with the incidence seen in adult patients receiving tablets.

The following adverse reactions have been reported following the post-approval use of cefixime. Incidence rates were less than 1 in 50 (less than 2%).

Gastrointestinal: pseudomembranous colitis; Hypersensitivity Reactions: Anaphylactic/anaphylactoid reactions (including shock and fatalities), skin rashes, urticaria, drug fever, pruritus, angioedema, and facial edema. Erythema multiforme, Stevens-Johnson syndrome, and serum sickness-like reactions have been reported; Hepatic : Transient elevations in SGPT, SGOT, alkaline phosphatase, hepatitis, jaundice; Renal : Transient elevations in BUN or creatinine, acute renal failure; Central Nervous System : Headaches, dizziness, seizures; Hemic and Lymphatic System : Transient thrombocytopenia, leukopenia, neutropenia, prolongation in prothrombin time, elevated LDH, pancytopenia, agranulocytosis, and eosinophilia; Abnormal Laboratory Tests : Hyperbilirubinemia; Other Adverse Reactions : Genital pruritus, vaginitis, candidiasis, toxic epidermal necrolysis.

Adverse Reactions Reported for Cephalosporin-class Drugs: Allergic reactions, superinfection, renal dysfunction, toxic nephropathy, hepatic dysfunction including cholestasis, aplastic anemia, hemolytic anemia, hemorrhage, and colitis. Several cephalosporins have been implicated in triggering seizures, particularly in patients with renal impairment when the dosage was not reduced. If seizures associated with drug therapy occur, the drug should be discontinued. Anticonvulsant therapy can be given if clinically indicated.

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via email to: medico@zuventus.com

Website: https://www.zuventus.com/drug-safety-reporting

By reporting side effects, you can help provide more information on the safety of this medicine.

4.9 Overdose

Gastric lavage may be indicated; otherwise, no specific antidote exists. Cefixime is not removed in significant quantities from the circulation by hemodialysis or peritoneal dialysis. Adverse reactions in small numbers of healthy adult volunteers receiving single doses up to 2 g of cefixime did not differ from the profile seen in patients treated at the recommended doses.

5.1 Mechanism of Action

Pharmacotherapeutic group: third generation cephalosporin, ATC code: J01DD08

Cefixime is an oral third generation cephalosporin which has marked in vitro bactericidal activity against a wide variety of Gram-positive and Gram-negative organisms.

Clinical efficacy has been demonstrated in infections caused by commonly occurring pathogens including Streptococcus pneumoniae, Streptococcus pyogenes, Escherichia coli, Proteus mirabilis, Klebsiella species, Haemophilus influenzae (beta-lactamase positive and negative), Branhamella catarrhalis (beta-lactamase positive and negative) and Enterobacter species. It is highly stable in the presence of beta-lactamase enzymes.

Most strains of enterococci (Streptococcus faecalis, group D Streptococci) and Staphylococci (including coagulase positive and negative strains and methicillin-resistant strains) are resistant to cefixime. In addition, most strains of Pseudomonas, Bacteroides fragilis, Listeria monocytogenes and Clostridia are resistant to cefixime.

5.2 Pharmacodynamic properties

Cefixime is an oral third generation cephalosporin which has marked in vitro bactericidal activity against a wide variety of Gram-positive and Gram-negative organisms. Comparative clinical trials of otitis media were conducted in nearly 400 children between the ages of 6 months to 10 years. Streptococcus pneumoniae was isolated from 47% of the patients, Haemophilus influenzae from 34%, Moraxella catarrhalis from 15% and S. pyogenes from 4%.

The overall response rate of Streptococcus pneumoniae to cefixime was approximately 10% lower and that of Haemophilus influenzae or Moraxella catarrhalis approximately 7% higher (12% when beta-lactamase positive isolates of H. influenzae are included) than the response rates of these organisms to the active control drugs.

In these studies, patients were randomized and treated with either cefixime at dose regimens of 4 mg/kg twice a day or 8 mg/kg once a day, or with a comparator. Sixty-nine to 70% of the patients in each group had resolution of signs and symptoms of otitis media when evaluated 2 to 4 weeks’ post-treatment, but persistent effusion was found in 15% of the patients. When evaluated at the completion of therapy, 17% of patients receiving cefixime and 14% of patients receiving effective comparative drugs (18% including those patients who had Haemophilus influenzae resistant to the control drug and who received the control antibacterial drug) were considered to be treatment failures. By the 2 to 4-week follow-up, a total of 30%-31% of patients had evidence of either treatment failure or recurrent disease.

5.3 Pharmacokinetic properties

Absorption: Cefixime suspension, given orally, absorbed about 40% to 50% whether administered with or without food; however, time to maximal absorption is increased approximately 0.8 hours when administered with food. The oral suspension produces average peak concentrations approximately 25% to 50% higher than the tablets, when tested in normal adult volunteers. Two hundred and 400 mg doses of oral suspension produce average peak concentrations of 3 mcg/mL (range 1 to 4.5 mcg/mL) and 4.6 mcg/mL (range 1.9 to 7.7 mcg/mL), respectively, when tested in normal adult volunteers. AUC is greater by approximately 10% to 25% with the oral suspension than with the tablet after doses of 100 to 400 mg, when tested in normal adult volunteers. This increased absorption should be taken into consideration if the oral suspension is to be substituted for the tablet.

Because of the lack of bioequivalence, tablets should not be substituted for oral suspension in the treatment of otitis media. Peak serum concentrations occur between 2 and 6 hours following oral administration of 400 mg of cefixime suspension. Peak serum concentrations occur between 2 and 5 hours following a single administration of 200 mg of suspension.

Distribution: Serum protein binding is concentration independent with a bound fraction of approximately 65%. In a multiple dose study conducted with a research formulation which is less bioavailable than the tablet or suspension, there was little accumulation of drug in serum or urine after dosing for 14 days. Adequate data on CSF levels of cefixime are not available.

Metabolism and Excretion: There is no evidence of metabolism of cefixime in vivo. Approximately 50% of the absorbed dose is excreted unchanged in the urine in 24 hours. In animal studies, it was noted that cefixime is also excreted in the bile in excess of 10% of the administered dose. The serum half-life of cefixime in healthy subjects is independent of dosage form and averages 3 to 4 hours but may range up to 9 hours in some normal volunteers.

6.1 Animal Toxicology or Pharmacology

Carcinogenesis, Mutagenesis, Impairment of Fertility

Lifetime studies in animals to evaluate carcinogenic potential have not been conducted. Cefixime did not cause point mutations in bacteria or mammalian cells, DNA damage, or chromosome damage in vitro and did not exhibit clastogenic potential in vivo in the mouse micronucleus test. In rats, fertility and reproductive performance were not affected by cefixime at doses up to 25 times the adult therapeutic dose.

Cefixime is a semisynthetic, cephalosporin antibacterial for oral administration.

Chemically, it is (6R,7R)-7-[2-(2-Amino-4-thiazolyl)glyoxylamido]-8-oxo-3-vinyl-5-thia-1-azabicyclo [4.2.0] oct-2-ene-2-carboxylic acid, 72-(Z)-[O-(carboxy methyl) oxime]trihydrate.

Molecular weight- 507.50 as the trihydrate.

Chemical Formula is C₁₆H₁₅N₅O₇S₂.3H₂O The structural formula for cefixime is:

8.1 Incompatibilities

Not Applicable

8.2 Shelf-life

Refer on pack

8.3 Packaging information

C Tax-O Forte Dry Syrup: A bottle of 30 ml & 50 ml.

8.4 Storage and handing instructions

Store in a cool & dry place. Protect from light. Keep out of reach of children. Store the reconstituted oral suspension in a refrigerator (at 2°C to 8°C).

Counsel patients that antibacterial drugs, including cefixime, should only be used to treat bacterial infections. They do not treat viral infections (e.g., the common cold). When cefixime is prescribed to treat a bacterial infection, patients should be told that although it is common to feel better early in the course of therapy, the medication should be taken exactly as directed.

Skipping doses or not completing the full course of therapy may: (1) decrease the effectiveness of the immediate treatment and (2) increase the likelihood that bacteria will develop resistance and will not be treatable by cefixime for oral suspension or other antibacterial drugs in the future.

Advise patients that diarrhea is a common problem caused by antibacterial drugs which usually ends when the antibacterial drug is discontinued. Sometimes after starting treatment with antibacterial drugs, patients can develop watery and bloody stools (with or without stomach cramps and fever) even as late as two or more months after having taken the last dose of the antibacterial drug. If this occurs, patients should contact their physician as soon as possible.

19th September 2024

Cefixime & Ofloxacin Tablets

Each film coated tablet contains:

Cefixime (as Trihydrate) IP equivalent to Anhydrous Cefixime 200 mg

Ofloxacin IP 200 mg

Excipients q.s.

Colours: Lake of Quinoline Yellow & Titanium Dioxide IP

Film coated tablet

Cefixime (200mg) and Ofloxacin (200mg)

4.1 Therapeutic Indication

For the treatment of patients with typhoid fever and urinary tract infection in adults.

4.2 Posology and method of administration

C Tax-OF adult dose:

1 tablet two times daily.

4.3 Contraindications 

• Persons with a history of hypersensitivity associated with the use of ofloxacin or any member of the quinolone group. Patients with known allergy to cefixime or other cephalosporins.
• Patients with a past history of tendinitis related to fluoroquinolone administration.
• Patients with a history of epilepsy or seizures.
• Children or growing adolescents and in pregnant or breast-feeding women, since animal experiments do not entirely exclude the risk of damage to the cartilage of joints in the growing subject
• Patients with latent or actual defects in G6PD activity

4.4 Special warnings and precautions for use

The drug may cause low blood sugar and mental health related side effects. Low blood sugar levels, also called hypoglycaemia, can lead to coma. The mental health side effects more prominent and more consistent across the systemic fluoroquinolone drug class. The mental health side effects to be added to or updated across all the fluoroquinolones are:

• Disturbances in attention
• Disorientation
• Agitation
• Nervousness
• Memory impairment
• Serious disturbances in mental abilities called delirium

4.5 Drugs interactions 

• Drugs known to prolong QT interval: C Tax-OF should be used with caution in patients receiving drugs known to prolong the QT interval (e.g. anti-arrhythmics, tricyclic antidepressants, macrolides, and antipsychotics).
• Antacids, Sucralfate, Metal Cations: Co-administered magnesium/aluminium antacids, sucralfate, zinc or iron preparations can reduce absorption. Therefore, ofloxacin should be taken 2 hours before such preparations.
• Theophylline, fenbufen or similar NSAIDs: A pronounced lowering of the cerebral seizure threshold may occur when quinolones are given concurrently with theophylline, NSAIDs, or other agents, which lower the seizure threshold. In case of seizures, treatment with C Tax-OF should be discontinued.
• Glibenclamide: Ofloxacin may cause a slight increase in serum concentrations of glibenclamide.
• Probenecid, cimetidine, furosemide and methotrexate: Caution should be exercised when ofloxacin is co-administered with drugs that affect the tubular renal secretion such as probenecid, cimetidine, furosemide and methotrexate.
• Vitamin K antagonists & Anticoagulants: Increased coagulation tests (PT/INR) and/or bleeding have been reported in patients treated with ofloxacin in combination with a vitamin K antagonist (e.g. warfarin). Coagulation tests should be monitored in patients treated with Vitamin-K antagonists. Cefixime should be administered with caution to patients receiving coumarin-type anticoagulants, e.g. warfarin.
• Other forms of interaction: A false positive direct coombs test has been reported during treatment with cephalosporin antibiotics, therefore it should be recognised that a positive coombs test may be due to the drug.

4.6 Use in special populations

Pregnancy

C Tax-OF should not be used during pregnancy.

Lactation

Breast feeding should be discontinued during treatment with C Tax-OF because of the potential for arthropathy and other serious toxicity in the nursing infants.

Children

C Tax-OF is not indicated for use in children or growing adolescents.

4.7 Effects on ability to drive and use machines

There have been occasional reports of drowsiness/somnolence, impairment of skills, dizziness/vertigo and visual disturbances, which may impair the patient's ability to concentrate and react, and therefore may constitute a risk in situations where these abilities are of special importance (e.g. driving a car or operating machinery), patients should know how they react to ofloxacin before they drive or operate machinery. These effects may be enhanced by alcohol.

In the case of side effects such as encephalopathy (which may include convulsion, confusion, impairment of consciousness, movement disorders), the patient should not operate machines or drive a vehicle.

4.8 Undesirable effects

Cefixime: 

• Acute generalized exanthematous pustulosis and Mouth Ulceration has been reported with Cefixime use.
• The most commonly seen adverse reactions reported were gastrointestinal events (30%) in adult patients
• Individual adverse reactions included Diarrhea-16%, Loose or frequent stools- 6%, Abdominal pain-3%, Nausea-7%, Dyspepsia-3%, Flatulence 4%

Ofloxacin:

• Stevens-Johnson syndrome (SJS)/ Toxic epidermal necrolysis (TEN) has been reported with Ofloxacin use.
• The most frequently reported adverse events were nausea- 10%, headache- 9%, insomnia- 7%, external genital pruritus in women- 6%, Dizziness-5%, Vaginitis-5%, Diarrhea-4%, Vomiting 4%

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product.

Healthcare professionals are asked to report any suspected adverse reactions via email to: medico@zuventus.com

Website: https://www.zuventus.com/drug-safety-reporting

By reporting side effects, you can help provide more information on the safety of this medicine.

4.9 Overdose

Ofloxacin

Important signs of acute over dosage: CNS symptoms such as confusion, dizziness, impairment of consciousness and seizures, increases QT interval, GIT reactions e.g. nausea and mucosal erosions.

In the case of overdose steps to remove any unabsorbed ofloxacin e.g. gastric lavage, administration of adsorbants and sodium sulphate are recommended; antacids are recommended for protection of the gastric mucosa. A fraction of ofloxacin may be removed from the body with haemodialysis.

No specific antidote exists. Elimination of ofloxacin may be increased by forced diuresis. In the event of overdose, symptomatic treatment should be implemented. ECG monitoring should be undertaken, because of the possibility of QT interval prolongation.

Cefixime There is no experience with overdoses with Cefixime. Cefixime is not removed from the circulation in significant quantities by dialysis. No specific antidote exists. General supportive measures are recommended.

5.1 Pharmacodynamic Properties

Cefixime 

• is an oral third generation cephalosporin which has marked in vitro bactericidal activity against a wide variety of Gram-positive and Gram-negative organisms. Bactericidal action of cefixime results from inhibition of cell-wall synthesis.
• Active against most isolates of the following bacteria both in vitro and in clinical infections:
  • Gram-positive bacteria- Streptococcus pneumonia, Streptococcus pyogenes
  • Gram-negative bacteria - Haemophilus influenza, Moraxella catarrhalis, Escherichia coli, Proteus mirabilis, Neisseria gonorrhoeae
• In vitro bactericidal activity is seen against isolates of the following microorganisms.
  • Gram-positive bacteria- Streptococcus agalactiae
  • Gram-negative bacteria- Haemophilus parainfluenzae, Proteus vulgaris, Klebsiella pneumonia, Klebsiella oxytoca, Pasteurella multocida, Providencia species, Salmonella species, Shigella species, Citrobacter amalonaticus, Citrobacter diversus, Serratia marcescens

Ofloxacin

• Is a quinolone-carboxylic acid derivative with a wide range of antibacterial activity against both gram negative and gram positive organisms.
• The primary mode of action of the quinolones is the specific inhibition of bacterial DNA gyrase. This enzyme is required for DNA replication, transcription, repair and recombination. Its inhibition leads to expansion and destabilisation of the bacterial DNA and hence to cell death.
• Active against most isolates of the following bacteria both in vitro and in clinical infections.
  • Gram-Positive Microorganisms- Staphylococcus aureus (methicillin-susceptible strains), Streptococcus pneumoniae (penicillin-susceptible), Streptococcus pyogenes
  • Gram-Negative Microorganisms- Citrobacter koseri, Enterobacter aerogenes, Escherichia coli, Haemophilus influenza, Klebsiella pneumonia, Neisseria gonorrhoeae, Proteus mirabilis, Pseudomonas aeruginosa,
  • Other Microorganisms- Chlamydia trachomatis
• In vitro bactericidal activity is seen against isolates of the following microorganisms
  • Gram-positive microorganisms- Staphylococcus epidermidis (methicillin-susceptible strains), Staphylococcus saprophyticu, Streptococcus pneumonia,
  • Gram-Negative Microorganisms- Acinetobacter calcoaceticus, Bordetella pertussis, Pasteurella multocida, Enterobacter cloacae, Haemophilus ducreyi, Klebsiella oxytoca, Moraxella catarrhalis, M. morganii, Proteus vulgaris, Providencia rettgeri, P. stuartii, Serratia marcescens
  • Other microorganisms- Chlamydia pneumoniae, Gardnerella vaginalis, Legionella pneumophila, Mycoplasma pneumoniae, Ureaplasma urealyticum,
  • Anaerobic Microorganisms- Clostridium perfringes

5.2 Pharmacokinetic properties

6.1 Animal Toxicology or Pharmacology

Preclinical effects in conventional studies of safety pharmacology, acute toxicity, repeated dose toxicity, reproductive studies were observed only at exposures considered sufficiently in excess of the maximum human exposure indicating little relevance to clinical use. Joint toxicity was observed at exposure in the human therapeutic range in juvenile rats and dogs. Ofloxacin exhibits a neurotoxic potential and causes reversible testicular alterations at high doses.

Mutagenicity studies showed no evidence for mutagenicity of ofloxacin. However, like some other quinolones Ofloxacin is phototoxic in animals at exposure in the human therapeutic range. The phototoxic, photomutagenic and photocarcinogenic potential of ofloxacin is comparable with that of other gyrase inhibitors.

Preclinical data from conventional genotoxicity studies reveal no special hazard to humans, carcinogen potential has not been investigated.

Reproduction toxicity

Ofloxacin has no effect on fertility, peri- or postnatal development, and therapeutic doses did not lead to any teratogenic or other embryotoxic effects in animals. Ofloxacin crosses the placenta and levels reached in the amniotic fluid are about 30% of the maximal concentrations measured in maternal serum.

Cefixime is a semisynthetic, cephalosporin antibacterial for oral administration. Ofloxacin tablets are a synthetic broad-spectrum antimicrobial agent for oral administration.

Cefixime

Chemical Name: (6R,7R)-7-[2-(2-Amino-4-thiazolyl) glyoxylamido]-8-oxo-3-vinyl-5-thia-1-azabicyclo [4.2.0] oct-2-ene-2-carboxylic acid, 72-(Z)- [O-(carboxy methyl) oxime] trihydrate

Chemical Formula: C16H15N5O7S2.3H2O

Molecular Weight: 507.50

Structure:

Ofloxacin

Chemical Name: (±)-9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1- piperazinyl)-7-oxo-7H-pyrido[1,2,3-de]-1,4-benzoxazine6-carboxylic acid

Chemical Formula: C18H20FN3O4

Molecular Weight: 361.4

Structure:

8.1 Incompatibilities

None

8.2 Shelf-life

Refer on the pack

8.3 Packaging information

A blister strip of 10 tablets.

8.4 Storage and handing instructions

Store below 25°C. Protect from light

Keep out of reach of children.

• Counsel patients that antibacterial drugs should only be used to treat bacterial infections. They do not treat viral infections (e.g., the common cold). When C Tax-OF is prescribed to treat a bacterial infection, patients should be told that although it is common to feel better early in the course of therapy, the medication should be taken exactly as directed. Skipping doses or not completing the full course of therapy may: (1) decrease the effectiveness of the immediate treatment and (2) increase the likelihood that bacteria will develop resistance and will not be treatable by C Tax- OF or other antibacterial drugs in the future.
• Advise patients to contact their healthcare provider if they experience pain, swelling, or inflammation of a tendon, or weakness or inability to use one of their joints; rest and refrain from exercise; and discontinue C Tax-OF treatment. The risk of severe tendon disorders with fluoroquinolones is higher in older patients usually over 60 years of age, in patients taking corticosteroid drugs, and in patients with kidney, heart or lung transplants;
• Advise patients that diarrhea is a common problem caused by antibacterial drugs which usually ends when the antibacterial drug is discontinued. Sometimes after starting treatment with antibacterial drugs, patients can develop watery and bloody stools (with or without stomach cramps and fever) even as late as two or more months after having taken the last dose of the antibacterial drug. If this occurs, patients should contact their physician as soon as possible.
• Advise patients that peripheral neuropathies have been associated with ofloxacin use. If symptoms of peripheral neuropathy including pain, burning, tingling, numbness, and/or weakness develop, they should discontinue treatment and contact their physicians
• photosensitivity/phototoxicity has been reported in patients receiving quinolone antibiotics. Patients should minimize or avoid exposure to natural or artificial sunlight (tanning beds or UVA/B treatment) while taking quinolones. If patients need to be outdoors while using quinolones, they should wear loose-fitting clothes that protect skin from sun exposure and discuss other sun protection measures with their physician. If a sunburn-like reaction or skin eruption occurs, patients should contact their physician.
• if they are diabetic and are being treated with insulin or an oral hypoglycemic drug, to discontinue ofloxacin immediately if a hypoglycemic reaction occurs and consult a physician
• convulsions have been reported in patients taking quinolones, including ofloxacin, and to notify their physician before taking this drug if there is a history of this condition
• if they are diabetic and are being treated with insulin or an oral hypoglycemic drug, to discontinue C Tax-OF immediately if a hypoglycemic reaction occurs and consult a physician
• Patients are advised to inform their physician of any personal or family history of QTc prolongation or proarrhythmic conditions such as hypokalemia, bradycardia, or recent myocardial ischemia; if they are taking any class IA (quinidine, procainamide), or class III (amiodarone, sotalol) antiarrhythmic agents. Patients should notify their physicians f they have any symptoms of prolongation of the QTc interval including prolonged heart palpitations or a loss of consciousness.
• Tell the patients if they get any side effects, talk to the doctor. This includes any possible side effects not listed in this leaflet. Advice patients if they have any further questions, ask the doctor or pharmacist.

05-07-2024

Acebrophylline Prolonged release Tablets

Each uncoated prolonged-release tablet contains:

Acebrophylline……………………………………. 200 mg

Excipients q.s.

Tablet 200 mg

4.1 Therapeutic indication

For the treatment of adult patients with chronic obstructive pulmonary disease (COPD) and bronchial asthma.

4.2 Posology and method of administration

Adults

Acebrophylline is administered at a recommended dose of 1 tablet once daily.

4.3 Contraindications

Hypersensitivity to xanthine derivatives like theophylline or to ambroxol.

4.4 Special warnings and precautions for use

Acebrophylline should be administered with caution in patients with hypertension, heart diseases, peptic ulcers and severe hypoxemia.

4.5 Drugs interactions

Theophylline should not be administered concurrently with other xanthine preparations and caution is required due to the interaction between theophylline and ephedrine or other sympathomimetic bronchodilators. The concomitant administration of reserpine may result in tachycardia.

4.6 Use in special populations

Pregnancy & Lactation

Although there are no clinical studies in pregnant or lactating women, Acebrophylline should be avoided in these women, unless the benefits outweigh the risks.

4.7 Effects on ability to drive and use machines

Brophyle SR Tablet does not usually affect the ability to drive.

4.8 Undesirable effects

Commonly reported adverse effects with Acebrophylline include abdominal discomfort, stomach/abdominal distension, vomiting, abdominal pain, diarrhea, constipation, heart burn, loss of appetite, esophageal bleeding, rashes, urticaria, itching, drowsiness, difficulty in breathing, leukocytosis and nasal inflammation. If chills and fever occur the drug should be immediately discontinued.

Rarely occurring adverse events include headache, occasional numbness including numbness in arm, insomnia, tachycardia, fatigue, hypertension, albuminuria, glycosuria, hypotension and occasionally hyperglycemia.

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via email to: medico@zuventus.com

Website: https://www.zuventus.com/drug-safety-reporting

By reporting side effects, you can help provide more information on the safety of this medicine.

4.9 Overdose

In the event of overdose, the stomach may be emptied by gastric lavage within 2 hrs of overdose. Elimination may also be enhanced by repeated oral doses of activated charcoal. Treatment is symptomatic and supportive.

5.1 Mechanism of Action / Pharmacodynamic Properties

Acebrophylline is an airway mucus regulator with anti-inflammatory actions. It has a multimodal mechanism of action involving effects on the pulmonary surfactant, bronchial secretions, phospholipase A and Phosphodiesterases. Theophylline-7-acetate, as with other xanthine derivatives, has a bronchodilator effect due to inhibition of the intracellular phosphodiesterases, followed by an increase of cyclic adenosine monophosphate levels, which promote the relaxation of bronchial muscles. Acebrophylline produces bronchodilation by specifically inhibiting phosphodiesterase III and IV.

Acebrophylline inhibits phospholipase A, and phosphatidylcholine leading to lesser production of the powerful pro-inflammatory substances like leukotrienes and tumour necrosis factor. By inhibiting the synthesis and release of these inflammatory mediators, Acebrophylline reduces inflammation, a key factor in airway obstruction, especially in chronic forms.

Acebrophylline increases the synthesis and secretion of pulmonary surfactants by acting on two levels of surfactant synthesis: the first involving ambroxol’s established action on phosphocholine-cytidyl-transferase and the second probably because of theophylline-7 acetic acid’s action on choline-kinase.

Ambroxol modifies the mucous gel phase of secretions by decreasing the viscosity and increasing the serous gel phase. It increases the mucociliary clearance by stimulating cilia motility. Thus, it has mucoregulatory, mucosecretory as well as mucokinetic actions, thereby normalizing the quantity & quality of pulmonary secretions.

5.2 Pharmacokinetic properties

On administration of 200 mg SR oral Acebrophylline, the two components of the molecule – ambroxol and theophylline-7-acetate are released in the stomach and absorbed in the intestines, reaching optimal concentrations of ambroxol and very low levels of theophylline- 7- acetic acid.

Thus it appears that the latter is either poorly absorbed or metabolized very fast and is eliminated in a fairly short time. Its low blood levels mean it is not likely to cause the untoward effects seen after theophylline, whose therapeutic window corresponds to much higher plasma concentrations (10-20 mcg/mL). Acebrophylline reaches its peak in serum (mean Cmax 136.458 +/- 7.079 ng/mL) at 1.708 +/- 0.550 hrs.

The elimination half-life of Acebrophylline is about 6.632 +/- 0.439 hrs. The drug is metabolized in the liver and eliminated renally.

6.1 Animal Toxicology or Pharmacology

No known animal toxicology data

Acebrophylline (Ambroxol theophylline-7-acetate) is the salt obtained by reaction of equimolar amounts of ambroxol, a drug showing mucolytic and expectorant properties, and theophylline-7-acetic acid, a xanthine derivative with specific bronchodilator activity.

Acebrophylline is obtained by targeted salification of the ambroxol base [trans-4(2-amino-3, 5 dibromobenzylamino)cyclohexanol] and theophylline 7 acetic acid. The carboxyl group of theophylline-7-acetic acid is salified with ambroxol’s amine group in a stoichiometric ratio (38.7% acid and 61.3% base) that ensures, after absorption, high plasma levels of ambroxol with low levels of the xanthine derivative which are nevertheless high enough to ensure a carrier effect for ambroxol. This means that one hour after administration lung levels of ambroxol are 45% higher than in subjects treated with ambroxol alone.

Its molecular formula is C₂₂H₂₈Br₂N₆O₅ and its molecular weight is 616.3.

8.1 Incompatibilities

Not applicable

8.2 Shelf-life

Refer on pack

8.3 Storage and handing instructions

Store below 30°C. Protect from light & moisture.

Keep out of reach of children.

• You have been prescribed Brophyle SR Tablet for prevention and treatment of asthma and chronic obstructive pulmonary disease (COPD).
• It should be taken at the same time each day, preferably in the evening after food.
• It does not work right away and should not be used to relieve sudden breathing problems. Always keep a fast-acting (rescue) inhaler with you.
• Your doctor may take regular blood test to monitor potassium level and the level of this medicine in your body.
• Notify your doctor if you have ever been diagnosed with kidney, liver or heart disease, or if you have a smoking history. Your dose may need to be adjusted.
• Do not discontinue use without consulting your doctor, even if you feel better.

16.09.2022