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First generation Cephalosporins

Cephradine is a semisynthetic broad spectrum bactericidal antibiotic, it is active against infections caused by both gram-positive and gram-negative microorganisms. Both penicillinase producing and nonproducing staphylococci are sensitive to Cephradine. The main site of action of Cephradine is the cell wall of bacteria. Cell wall of sensitive organism contains peptidoglycan. Cephradine inhibits cross-linking process and as a result cell wall with many pores are formed, thus lysis of bacteria occur due to external osmotic pressure.

For oral administration-
Adults:

• Urinary tract infections: 500mg four times daily or 1g twice daily. Infections which are severe or chronic may necessitate the administration of higher doses. Where complications arise including prostatitis and epididymitis continued intensive treatment is required.
• Respiratory tract infections: 250 to 500mg four times daily or 500mg to 1g twice daily, dependent on the site and severity of the infection.
• Skin and soft tissue infections: 250 to 500mg four times daily or 500mg to 1g twice daily, again dependent on the site and severity of the infection.

Children:

• Total daily dose of 25 to 50mg/kg given in two or four equally divided doses.
• Otitis media: Total daily dose of 75 to 100mg/kg given in divided doses 6 to 12 hourly.
• Maximum daily dosage: 4 gm

Elderly: The normal adult dose is appropriate. Patients with impaired renal or hepatic function should be monitored during treatment.

For injectable administration-

• Adult: The usual dose is 2-4 gm daily in four equally divided doses up to 8 gm daily. For prophylaxis a single preoperative dose of 1-2 gm intramuscularly or intravenously is given.
• Children: The dose is 50-100 mg/kg daily in four equally divided doses, up to 300 mg/kg daily in severe infection.

Limited essentially to gastro-intestinal disturbances and on occasions to hypersensitivity phenomena. The latter are more likely to occur in individuals, who have previously demonstrated hypersensitivity and thos with a history of allergy, asthma, hay fever or urticaria. Skin reactions have occasionally been reported. Rare- Glossitis, heartburn, dizziness, tightness in the chest, nausea, vomiting, diarrhoea, abdominal pain, vaginitis, candida overgrowth. Skin and hypersensitivity reactions include urticaria, skin rashes, joint pains, oedema.

• Blood and lymphatic system disorders- Unknown: blood disorders (including thrombocytopenia, leucopenia, agranulocytosis, aplastic anaemia and haemolytic anaemia)
• Immune system disorders- Unknown: Fever, serum sickness like reactions, anaphylaxis
• Psychiatric disorders- Unknown: Confusion, sleep disturbances
• Nervous system disorders- Unknown: hyperactivity, hypertonia, dizziness, nervousness; Rarely: Headache
• Hepatobiliary disorders- Frequency unknown: Liver, enzyme disturbances, transient hepatitis, cholestatic jaundice
• Renal and urinary disorders- Unknown: Reversible interstitial nephritis
• Investigations- Unknown: Elevation of blood urea nitrogen, serum creatinine, alanine aminotransferase, aspartate aminotransferase, total bilirubin, alkaline phosphatase.

Cephradine should not be used in patients with known or suspected hypersensitivity to cephalosporins.

The concomitant use of nephrotoxic drugs such as aminoglycosides with Cefradine may increase the risk of kidney damage. Diuretics (e.g. frusemide, ethacrynic acid) and probenecid enhanced the possibility of renal toxicity.

Although animal studies have not demonstrated any teratogenicity, safety in pregnancy has not been established. Cephradine is excreted in breast milk and should be used with caution in lactating mothers. Since the medicine may cause dizziness, patients should be cautioned about operating hazardous machinery, including automobiles.

Renal Impairment: The following doses are recommended (based on 500 mg every 6 hours) for patients not on haemodialysis:

• CrCl: >20 ml/min: 500 mg every 6 hours
• CrCl: 5-20 ml/min: 250 mg every 6 hours
• CrCl: <5 ml/min: 250 mg every 50-70 hours.

Recommendations for patients on chronic, intermittent haemodialysis:

• 250 mg at the start of haemodialysis
• 250 mg 6 to 12 hours after the start
• 250 mg 36 to 48 hours after the start
• 250 mg at the start of the next haemodialysis session if more than 30 hours have elapsed since the last dose.

Additional Information for all patients Regardless of patient age or weight, higher doses of up to 1 gm four times daily may be required for infections which are chronic or severe. Treatment should continue for at least 2 to 3 days after symptoms have resolved or bacteria have been eradicated. To reduce the possibility of rheumatic fever or glomerulonephritis resulting from infections with haemolytic streptococci, treatment should be continued for at least 10 days. Throughout treatment of chronic urinary tract infections and for several months thereafter, regular bacteriological and clinical monitoring is required.

Doses below those recommended above should not be prescribed. Paediatric dosages should not exceed those specified for adults, regardless of severity of infection. It may be necessary to continue Cephradine therapy for several weeks in persistent infections. Patients may be transferred from intramuscular/intravenous Cephradine therapy to oral treatment at the same dosage level.

The symptoms of Sefrad overdose are non-specific and are generally nausea, vomiting, diarrhoea and gastric upsets. Treatment is mainly supportive although gastric lavage will be necessary if a large amount has been ingested.

Cephradine Suspension should be freshly prepared. Reconstituted Suspension should be used within 7 days if kept at room temperature or within 14 days, if kept in a refrigerator. Cephradine Injection solutions should be used within 2 hours when kept at room temperature. When stored at 5°C, solutions retain potency for 12 hours. Reconstituted solutions may vary in colour from light to straw yellow; however, this does not affect the potency. Do not use later than the date of expiry. Keep all medicines out of the reach of children. To be dispensed only on the prescription of a registered physician

First generation Cephalosporins

Cephradine is a semisynthetic broad spectrum bactericidal antibiotic, it is active against infections caused by both gram-positive and gram-negative microorganisms. Both penicillinase producing and nonproducing staphylococci are sensitive to Cephradine. The main site of action of Cephradine is the cell wall of bacteria. Cell wall of sensitive organism contains peptidoglycan. Cephradine inhibits cross-linking process and as a result cell wall with many pores are formed, thus lysis of bacteria occur due to external osmotic pressure.

For oral administration-
Adults:

• Urinary tract infections: 500mg four times daily or 1g twice daily. Infections which are severe or chronic may necessitate the administration of higher doses. Where complications arise including prostatitis and epididymitis continued intensive treatment is required.
• Respiratory tract infections: 250 to 500mg four times daily or 500mg to 1g twice daily, dependent on the site and severity of the infection.
• Skin and soft tissue infections: 250 to 500mg four times daily or 500mg to 1g twice daily, again dependent on the site and severity of the infection.

Children:

• Total daily dose of 25 to 50mg/kg given in two or four equally divided doses.
• Otitis media: Total daily dose of 75 to 100mg/kg given in divided doses 6 to 12 hourly.
• Maximum daily dosage: 4 gm

Elderly: The normal adult dose is appropriate. Patients with impaired renal or hepatic function should be monitored during treatment.

For injectable administration-

• Adult: The usual dose is 2-4 gm daily in four equally divided doses up to 8 gm daily. For prophylaxis a single preoperative dose of 1-2 gm intramuscularly or intravenously is given.
• Children: The dose is 50-100 mg/kg daily in four equally divided doses, up to 300 mg/kg daily in severe infection.

Limited essentially to gastro-intestinal disturbances and on occasions to hypersensitivity phenomena. The latter are more likely to occur in individuals, who have previously demonstrated hypersensitivity and thos with a history of allergy, asthma, hay fever or urticaria. Skin reactions have occasionally been reported. Rare- Glossitis, heartburn, dizziness, tightness in the chest, nausea, vomiting, diarrhoea, abdominal pain, vaginitis, candida overgrowth. Skin and hypersensitivity reactions include urticaria, skin rashes, joint pains, oedema.

• Blood and lymphatic system disorders- Unknown: blood disorders (including thrombocytopenia, leucopenia, agranulocytosis, aplastic anaemia and haemolytic anaemia)
• Immune system disorders- Unknown: Fever, serum sickness like reactions, anaphylaxis
• Psychiatric disorders- Unknown: Confusion, sleep disturbances
• Nervous system disorders- Unknown: hyperactivity, hypertonia, dizziness, nervousness; Rarely: Headache
• Hepatobiliary disorders- Frequency unknown: Liver, enzyme disturbances, transient hepatitis, cholestatic jaundice
• Renal and urinary disorders- Unknown: Reversible interstitial nephritis
• Investigations- Unknown: Elevation of blood urea nitrogen, serum creatinine, alanine aminotransferase, aspartate aminotransferase, total bilirubin, alkaline phosphatase.

Cephradine should not be used in patients with known or suspected hypersensitivity to cephalosporins.

The concomitant use of nephrotoxic drugs such as aminoglycosides with Cefradine may increase the risk of kidney damage. Diuretics (e.g. frusemide, ethacrynic acid) and probenecid enhanced the possibility of renal toxicity.

Although animal studies have not demonstrated any teratogenicity, safety in pregnancy has not been established. Cephradine is excreted in breast milk and should be used with caution in lactating mothers. Since the medicine may cause dizziness, patients should be cautioned about operating hazardous machinery, including automobiles.

Renal Impairment: The following doses are recommended (based on 500 mg every 6 hours) for patients not on haemodialysis:

• CrCl: >20 ml/min: 500 mg every 6 hours
• CrCl: 5-20 ml/min: 250 mg every 6 hours
• CrCl: <5 ml/min: 250 mg every 50-70 hours.

Recommendations for patients on chronic, intermittent haemodialysis:

• 250 mg at the start of haemodialysis
• 250 mg 6 to 12 hours after the start
• 250 mg 36 to 48 hours after the start
• 250 mg at the start of the next haemodialysis session if more than 30 hours have elapsed since the last dose.

Additional Information for all patients Regardless of patient age or weight, higher doses of up to 1 gm four times daily may be required for infections which are chronic or severe. Treatment should continue for at least 2 to 3 days after symptoms have resolved or bacteria have been eradicated. To reduce the possibility of rheumatic fever or glomerulonephritis resulting from infections with haemolytic streptococci, treatment should be continued for at least 10 days. Throughout treatment of chronic urinary tract infections and for several months thereafter, regular bacteriological and clinical monitoring is required.

Doses below those recommended above should not be prescribed. Paediatric dosages should not exceed those specified for adults, regardless of severity of infection. It may be necessary to continue Cephradine therapy for several weeks in persistent infections. Patients may be transferred from intramuscular/intravenous Cephradine therapy to oral treatment at the same dosage level.

The symptoms of Sefrad overdose are non-specific and are generally nausea, vomiting, diarrhoea and gastric upsets. Treatment is mainly supportive although gastric lavage will be necessary if a large amount has been ingested.

Cephradine Suspension should be freshly prepared. Reconstituted Suspension should be used within 7 days if kept at room temperature or within 14 days, if kept in a refrigerator. Cephradine Injection solutions should be used within 2 hours when kept at room temperature. When stored at 5°C, solutions retain potency for 12 hours. Reconstituted solutions may vary in colour from light to straw yellow; however, this does not affect the potency. Do not use later than the date of expiry. Keep all medicines out of the reach of children. To be dispensed only on the prescription of a registered physician

First generation Cephalosporins

Cephradine is a semisynthetic broad spectrum bactericidal antibiotic, it is active against infections caused by both gram-positive and gram-negative microorganisms. Both penicillinase producing and nonproducing staphylococci are sensitive to Cephradine. The main site of action of Cephradine is the cell wall of bacteria. Cell wall of sensitive organism contains peptidoglycan. Cephradine inhibits cross-linking process and as a result cell wall with many pores are formed, thus lysis of bacteria occur due to external osmotic pressure.

For oral administration-
Adults:

• Urinary tract infections: 500mg four times daily or 1g twice daily. Infections which are severe or chronic may necessitate the administration of higher doses. Where complications arise including prostatitis and epididymitis continued intensive treatment is required.
• Respiratory tract infections: 250 to 500mg four times daily or 500mg to 1g twice daily, dependent on the site and severity of the infection.
• Skin and soft tissue infections: 250 to 500mg four times daily or 500mg to 1g twice daily, again dependent on the site and severity of the infection.

Children:

• Total daily dose of 25 to 50mg/kg given in two or four equally divided doses.
• Otitis media: Total daily dose of 75 to 100mg/kg given in divided doses 6 to 12 hourly.
• Maximum daily dosage: 4 gm

Elderly: The normal adult dose is appropriate. Patients with impaired renal or hepatic function should be monitored during treatment.

For injectable administration-

• Adult: The usual dose is 2-4 gm daily in four equally divided doses up to 8 gm daily. For prophylaxis a single preoperative dose of 1-2 gm intramuscularly or intravenously is given.
• Children: The dose is 50-100 mg/kg daily in four equally divided doses, up to 300 mg/kg daily in severe infection.

Limited essentially to gastro-intestinal disturbances and on occasions to hypersensitivity phenomena. The latter are more likely to occur in individuals, who have previously demonstrated hypersensitivity and thos with a history of allergy, asthma, hay fever or urticaria. Skin reactions have occasionally been reported. Rare- Glossitis, heartburn, dizziness, tightness in the chest, nausea, vomiting, diarrhoea, abdominal pain, vaginitis, candida overgrowth. Skin and hypersensitivity reactions include urticaria, skin rashes, joint pains, oedema.

• Blood and lymphatic system disorders- Unknown: blood disorders (including thrombocytopenia, leucopenia, agranulocytosis, aplastic anaemia and haemolytic anaemia)
• Immune system disorders- Unknown: Fever, serum sickness like reactions, anaphylaxis
• Psychiatric disorders- Unknown: Confusion, sleep disturbances
• Nervous system disorders- Unknown: hyperactivity, hypertonia, dizziness, nervousness; Rarely: Headache
• Hepatobiliary disorders- Frequency unknown: Liver, enzyme disturbances, transient hepatitis, cholestatic jaundice
• Renal and urinary disorders- Unknown: Reversible interstitial nephritis
• Investigations- Unknown: Elevation of blood urea nitrogen, serum creatinine, alanine aminotransferase, aspartate aminotransferase, total bilirubin, alkaline phosphatase.

Cephradine should not be used in patients with known or suspected hypersensitivity to cephalosporins.

The concomitant use of nephrotoxic drugs such as aminoglycosides with Cefradine may increase the risk of kidney damage. Diuretics (e.g. frusemide, ethacrynic acid) and probenecid enhanced the possibility of renal toxicity.

Although animal studies have not demonstrated any teratogenicity, safety in pregnancy has not been established. Cephradine is excreted in breast milk and should be used with caution in lactating mothers. Since the medicine may cause dizziness, patients should be cautioned about operating hazardous machinery, including automobiles.

Renal Impairment: The following doses are recommended (based on 500 mg every 6 hours) for patients not on haemodialysis:

• CrCl: >20 ml/min: 500 mg every 6 hours
• CrCl: 5-20 ml/min: 250 mg every 6 hours
• CrCl: <5 ml/min: 250 mg every 50-70 hours.

Recommendations for patients on chronic, intermittent haemodialysis:

• 250 mg at the start of haemodialysis
• 250 mg 6 to 12 hours after the start
• 250 mg 36 to 48 hours after the start
• 250 mg at the start of the next haemodialysis session if more than 30 hours have elapsed since the last dose.

Additional Information for all patients Regardless of patient age or weight, higher doses of up to 1 gm four times daily may be required for infections which are chronic or severe. Treatment should continue for at least 2 to 3 days after symptoms have resolved or bacteria have been eradicated. To reduce the possibility of rheumatic fever or glomerulonephritis resulting from infections with haemolytic streptococci, treatment should be continued for at least 10 days. Throughout treatment of chronic urinary tract infections and for several months thereafter, regular bacteriological and clinical monitoring is required.

Doses below those recommended above should not be prescribed. Paediatric dosages should not exceed those specified for adults, regardless of severity of infection. It may be necessary to continue Cephradine therapy for several weeks in persistent infections. Patients may be transferred from intramuscular/intravenous Cephradine therapy to oral treatment at the same dosage level.

The symptoms of Sefrad overdose are non-specific and are generally nausea, vomiting, diarrhoea and gastric upsets. Treatment is mainly supportive although gastric lavage will be necessary if a large amount has been ingested.

Cephradine Suspension should be freshly prepared. Reconstituted Suspension should be used within 7 days if kept at room temperature or within 14 days, if kept in a refrigerator. Cephradine Injection solutions should be used within 2 hours when kept at room temperature. When stored at 5°C, solutions retain potency for 12 hours. Reconstituted solutions may vary in colour from light to straw yellow; however, this does not affect the potency. Do not use later than the date of expiry. Keep all medicines out of the reach of children. To be dispensed only on the prescription of a registered physician

For the disinfection of clean and intact skin. For pre-operative surgical hand disinfection, hand disinfection on the ward prior to aseptic procedures or after handling contaminated materials. For disinfection of the patients’ skin prior to surgery or other invasive procedures

Chlorhexidine & Chloroxylenol preparations

Chlorhexidine is a very potent cationic chemoprophylactic agent that has a broad-spectrum of activity against gm+ve and gm-ve bacteria. It is both bacteriostatic and bactericidal depending on its concentration. The bactericidal effect, which is achieved at high concentrations, is due to the binding of the cationic to negatively charged bacterial cell walls and extramicrobial complexes. Bacteriostatic effect is achieved at low concentrations which causes an alteration of bacterial cell osmotic equilibrium and leakage of potassium and phosphorus.

Pre-operative surgical hand disinfection: Dispense 5 ml of solution and spread thoroughly over both hands and forearms, rubbing vigorously. When dry apply a further 5 ml and repeat the procedure.

Antiseptic hand disinfection on the ward: Dispense 3 ml of solution and spread thoroughly over the hands and wrists rubbing vigorously until dry.

Disinfection of patients skin: Prior to surgery apply the solution to a sterile swab and rub vigorously over the operation site for a minimum of 2 minutes. Chlorhexidine Gluconate is also used for preparation of the skin prior to invasive procedures such as venepuncture.

Irritative skin reactions can occasionally occur. Generalised allergic reactions have also been reported but are extremely rare

Chlorhexidine Gluconate is contraindicated for persons who have previously shown a hypersensitivity reaction to chlorhexidine. However, such reactions are extremely rare.

Avoid contact with brain, meninges, middle ear or sensitive tissues and eyes. Do not inject or use in body cavities.

Chlorhexidine is incompatible with soaps and other anionic agents. Hypochlorite bleaches may cause brown stains to develop in fabrics which have previously been in contact with chlorhexidine solutions.

No untoward effects are known

Symptoms: Pharyngeal oedema, necrotic lesions of the esophagus and elevated serum aminotransferase concentrations.

Management: Gastric lavage using milk, raw egg, gelatin or mild soap, or employ appropriate supportive measures.

Do not store above 25° C.

Bepotastine Besilate is indicated for the treatment of itching associated with signs and symptoms of allergic conjunctivitis.

Ophthalmic Anti-allergic preparations

Bepotastine is direct H1-receptor antagonist and an inhibitor of the release of histamine from mast cells.

The recommended dose is 1 drop into the affected eye(s) twice a day. Safety and effectiveness in children below the age of 2 years have not been established.

The most common reported side effect occurring in approximately 25% of subjects was a mild taste following instillation. Other side effects occurring in 2-5% of subjects were eye irritation, headache, and nasopharyngitis.

Contraindicated in patients with a history of hypersensitivity reactions to Bepotastine Besilate or any of the other ingredients of this product.

To minimize the risk of contamination, do not touch dropper tip to any surface. It should not be used to treat contact lens-related irritation. Patients should be advised not to wear contact lens when using this drop.

No drug interactions observed but patients who are sensitive to this product molecule should be used with caution.

Pregnancy Category C. There are no adequate and well controlled studies in pregnant women. It should be used during pregnancy only if the potential benefit to the mother justifies the potential risk to the fetus.

Lactation: It is not known if Bepotastine Besilate is excreted in human milk. Caution should be exercised when it is administered to a nursing woman.

If you use more Bepotastine Besilate eye drops than you should, rinse your eye with warm water. Do not put in any more drops until it is time for your next regular dose. Pharmaceutical Precautions

Store in a cool, dry place & protected from light. Keep out of reach of children. Do not use more than 4 weeks after opening.

This cream is usually useful for the treatment of superficial infections caused by gram-positive and gramnegative microorganisms. It is also useful in burns, regeneration of new skin in wounds and ulceration, otitis externa, postoperative infections, neuro-dermatitis and eczema. It may be used as an adjunct to systemic steroid therapy in special kind of pyoderma.

Aural steroid & antibiotic combined preparations

Betamethasone is an active topical corticosteroid, which produces a rapid response in the inflammatory dermatoses and cures psoriasis types of skin diseases. Neomycin Sulfate is a topical broad-spectrum bactericidal amino-glycoside effective against various kinds of gram-positive and gramnegative pathogens such as Proteus vulgaris, Staphylococcus aureus etc. This preparation has effective penetration and uniform distribution capacity, so it is very effective in hairy and intertriginous places. This preparation is very effective for the treatment of wet ulceration of the skin.

Use in adults: This preparation should be applied to the affected parts of the skin as a thin layer for 3 to 4 times daily. In chronic conditions, withdrawal of treatment is carried out by decreasing the frequency of application until the cream is applied as infrequently as once a week. Or as directed by the physician.

Use in children: Do not use it on children under 1 year of age. A course of treatment for a child should not normally last more than 5 days unless otherwise stated by your physician.

This preparation is well tolerated. But prolonged and high doses may cause Cushing's syndrome, acne, thinning and dilatation of blood vessels, particularly when occlusive dressings are used.

This preparation is contraindicated to the patients who are hypersensitive to any of its components. It should not be used for the treatment of otitis externa when the eardrum is perforated. It is contraindicated in skin lesions caused by infection with viruses and fungi.

Long term continuous topical therapy of this preparation should be avoided, which may produce many resistant micro organisms. So, accurate dose of this preparation should be used in infected areas only.

There are no significant drug interactions reported with Betamethasone Valerate BP and Neomycin Sulphate BP Cream/Ointment.

This preparation should not be used extensively in pregnancy.

Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.

Ophthalmic steroid - antibiotic combined preparations

Betamethasone is a corticosteroid which is effective in inflammatory dermatoses. It is also effective in less responsive conditions such as psoriasis.  Betamethasone has a 16β-methyl group that enhances the anti-inflammatory action of the molecule and reduces the sodium and water retaining properties of the fluorine atom bound at carbon 9.

Neomycin sulfate is bactericidal against many bacteria which are commonly associated with skin infections. Neomycin is a broad spectrum antibiotic which actively transported across the bacterial cell membrane, binds to a specific receptor protein on the 30s subunit of bacterial ribosomes, and interferes with an initiation complex between mRNA (messenger RNA) and the 30s subunit, inhibiting protein synthesis. DNA may be misread, thus producing nonfunctional proteins; polyribosomes are split apart and are unable to synthesize protein.

Drops:

• Eye: 1 drop instilled into the eye every one or two hours until control is achieved, when the frequency may be reduced.
• Ear: 2 or 3 drops instilled into the ear, every two or three hours until control is achieved, when the frequency can be reduced.
• Nose: 2 or 3 drops instilled into each nostril two or three times daily.

Eye Ointment: It should be applied thinly and evenly to the conjunctival sac at night (If eye drops used during day) or 3-4 times daily (if ointment used alone).

Acute sensitization to neomycin is a rare event but can occur after topical application to the eye. Eye drops containing corticosteroids cause a serious rise in intra-ocular pressure in a small percentage of the population, including most of those with a family history of glaucoma. A milder rise may be experienced by a larger proportion of subjects if treatment is continued for longer than a few weeks. Thinning of the cornea leading to perforation has occurred with use of topical corticosteroids. Cataract is reported to have occurred after unduly prolonged treatment of eye conditions with topical corticosteroids.

Viral, fungal, tuberculous or purulent conditions. Use in the eye is contra-indicated if glaucoma is present or where herpetic keratitis (e.g. dendritic ulcer) is considered a possibility. Inadvertent use of topical steroids in the latter condition can lead to extension of the ulcer and marked visual deterioration. Preparations containing neomycin should not be used for treating otitis externa when the ear drum is perforated, because of the risk of ototoxicity.

Steroids should not be administered to "red eyes" until a definitive diagnosis has been made. Ophthalmological treatment with steroid preparations should not be repeated or prolonged without regular review to exclude raised intra-ocular pressure or unsuspected infections. The unnecessary topical use of neomycin containing products should be avoided in order to minimize the occurrence of neomycin-resistant organisms (and organism cross-resistant to other aminoglycosides).

Pregnancy Category-Not Classified. FDA has not yet classified the drug into a specified pregnancy category. Topical administration of corticosteroid to pregnant animals can cause abnormalities of fetal development. The relevance of this finding to human beings has not been established; however, topical steroids should not be used extensively in pregnancy, i.e. in large amounts or for prolonged periods.

Store below 25° C

Ophthalmic steroid - antibiotic combined preparations

Betamethasone is a corticosteroid which is effective in inflammatory dermatoses. It is also effective in less responsive conditions such as psoriasis.  Betamethasone has a 16β-methyl group that enhances the anti-inflammatory action of the molecule and reduces the sodium and water retaining properties of the fluorine atom bound at carbon 9.

Neomycin sulfate is bactericidal against many bacteria which are commonly associated with skin infections. Neomycin is a broad spectrum antibiotic which actively transported across the bacterial cell membrane, binds to a specific receptor protein on the 30s subunit of bacterial ribosomes, and interferes with an initiation complex between mRNA (messenger RNA) and the 30s subunit, inhibiting protein synthesis. DNA may be misread, thus producing nonfunctional proteins; polyribosomes are split apart and are unable to synthesize protein.

Drops:

• Eye: 1 drop instilled into the eye every one or two hours until control is achieved, when the frequency may be reduced.
• Ear: 2 or 3 drops instilled into the ear, every two or three hours until control is achieved, when the frequency can be reduced.
• Nose: 2 or 3 drops instilled into each nostril two or three times daily.

Eye Ointment: It should be applied thinly and evenly to the conjunctival sac at night (If eye drops used during day) or 3-4 times daily (if ointment used alone).

Acute sensitization to neomycin is a rare event but can occur after topical application to the eye. Eye drops containing corticosteroids cause a serious rise in intra-ocular pressure in a small percentage of the population, including most of those with a family history of glaucoma. A milder rise may be experienced by a larger proportion of subjects if treatment is continued for longer than a few weeks. Thinning of the cornea leading to perforation has occurred with use of topical corticosteroids. Cataract is reported to have occurred after unduly prolonged treatment of eye conditions with topical corticosteroids.

Viral, fungal, tuberculous or purulent conditions. Use in the eye is contra-indicated if glaucoma is present or where herpetic keratitis (e.g. dendritic ulcer) is considered a possibility. Inadvertent use of topical steroids in the latter condition can lead to extension of the ulcer and marked visual deterioration. Preparations containing neomycin should not be used for treating otitis externa when the ear drum is perforated, because of the risk of ototoxicity.

Steroids should not be administered to "red eyes" until a definitive diagnosis has been made. Ophthalmological treatment with steroid preparations should not be repeated or prolonged without regular review to exclude raised intra-ocular pressure or unsuspected infections. The unnecessary topical use of neomycin containing products should be avoided in order to minimize the occurrence of neomycin-resistant organisms (and organism cross-resistant to other aminoglycosides).

Pregnancy Category-Not Classified. FDA has not yet classified the drug into a specified pregnancy category. Topical administration of corticosteroid to pregnant animals can cause abnormalities of fetal development. The relevance of this finding to human beings has not been established; however, topical steroids should not be used extensively in pregnancy, i.e. in large amounts or for prolonged periods.

Store below 25° C

Bepotastine Besilate is indicated for the treatment of itching associated with signs and symptoms of allergic conjunctivitis.

Ophthalmic Anti-allergic preparations

Bepotastine is direct H1-receptor antagonist and an inhibitor of the release of histamine from mast cells.

The recommended dose is 1 drop into the affected eye(s) twice a day. Safety and effectiveness in children below the age of 2 years have not been established.

The most common reported side effect occurring in approximately 25% of subjects was a mild taste following instillation. Other side effects occurring in 2-5% of subjects were eye irritation, headache, and nasopharyngitis.

Contraindicated in patients with a history of hypersensitivity reactions to Bepotastine Besilate or any of the other ingredients of this product.

To minimize the risk of contamination, do not touch dropper tip to any surface. It should not be used to treat contact lens-related irritation. Patients should be advised not to wear contact lens when using this drop.

No drug interactions observed but patients who are sensitive to this product molecule should be used with caution.

Pregnancy Category C. There are no adequate and well controlled studies in pregnant women. It should be used during pregnancy only if the potential benefit to the mother justifies the potential risk to the fetus.

Lactation: It is not known if Bepotastine Besilate is excreted in human milk. Caution should be exercised when it is administered to a nursing woman.

If you use more Bepotastine Besilate eye drops than you should, rinse your eye with warm water. Do not put in any more drops until it is time for your next regular dose. Pharmaceutical Precautions

Store in a cool, dry place & protected from light. Keep out of reach of children. Do not use more than 4 weeks after opening.

Meniere's disease and Meniere-like syndromes are characterized by attacks of vertigo, tinnitus and/or progressive loss of hearing, usually accompanied by nausea and vomiting.

Drugs used in meniere's diseases

The mechanism of action of betahistine is multifactorial. Meniere's disease is thought to result from a disruption of endolymphatic fluid homeostasis in the ear. Betahistine mainly acts as a histamine H1-receptor agonist. The stimulation of H1-receptors in the inner ear causes a vasodilatory effect leading to increased permeability of blood vessels and a reduction in endolymphatic pressure; this action prevents the rupture of the labyrinth, which can contribute to the hearing loss associated with Ménière's disease. Betahistine is also purported to act by reducing the asymmetrical functioning of sensory vestibular organs and increasing vestibulocochlear blood flow, relieving symptoms of vertigo.

In addition to the above mechanisms, betahistine also acts as a histamine H3-receptor antagonist, increasing the turnover of histamine from postsynaptic histaminergic nerve receptors, subsequently leading to an increase in H1-agonist activity. H3-receptor antagonism elevates levels of neurotransmitters including serotonin in the brainstem, inhibiting the activity of vestibular nuclei, thus restoring proper balance and decreasing vertigo symptoms.

The usual initial dose: 8 mg to 16 mg three times daily taken preferably with meals.

Maintenance dose: Up to 48 mg daily has been recommended. Betahistine is not recommended for use in children.

Betahistine is generally well tolerated and there is no known serious adverse effects. In some circumstances gastrointestinal disturbances, headache, rashes and pruritus have been reported.

Betahistine is contraindicated in pheochromocytoma.

Caution should be exercised in patients with bronchial asthma and peptic ulceration.

There are no proven cases of hazardous interactions. Though an antagonism between Betahistine and antihistamines could be expected on a theoretical basis, no such interactions have been reported.

In Pregnancy: The safety of Betahistine in human pregnancy has not been completely established, although there is no known teratogenic effect in animals. A careful assessment of potential benefits should be made before prescribing Betahistine in pregnancy.

In Lactation: Betahistine is excreted in the breast milk of nursing mothers in concentrations similar to those found in plasma. Toxicity to the neonate at these concentrations is not known.

Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.

Meniere's disease and Meniere-like syndromes are characterized by attacks of vertigo, tinnitus and/or progressive loss of hearing, usually accompanied by nausea and vomiting.

Drugs used in meniere's diseases

The mechanism of action of betahistine is multifactorial. Meniere's disease is thought to result from a disruption of endolymphatic fluid homeostasis in the ear. Betahistine mainly acts as a histamine H1-receptor agonist. The stimulation of H1-receptors in the inner ear causes a vasodilatory effect leading to increased permeability of blood vessels and a reduction in endolymphatic pressure; this action prevents the rupture of the labyrinth, which can contribute to the hearing loss associated with Ménière's disease. Betahistine is also purported to act by reducing the asymmetrical functioning of sensory vestibular organs and increasing vestibulocochlear blood flow, relieving symptoms of vertigo.

In addition to the above mechanisms, betahistine also acts as a histamine H3-receptor antagonist, increasing the turnover of histamine from postsynaptic histaminergic nerve receptors, subsequently leading to an increase in H1-agonist activity. H3-receptor antagonism elevates levels of neurotransmitters including serotonin in the brainstem, inhibiting the activity of vestibular nuclei, thus restoring proper balance and decreasing vertigo symptoms.

The usual initial dose: 8 mg to 16 mg three times daily taken preferably with meals.

Maintenance dose: Up to 48 mg daily has been recommended. Betahistine is not recommended for use in children.

Betahistine is generally well tolerated and there is no known serious adverse effects. In some circumstances gastrointestinal disturbances, headache, rashes and pruritus have been reported.

Betahistine is contraindicated in pheochromocytoma.

Caution should be exercised in patients with bronchial asthma and peptic ulceration.

There are no proven cases of hazardous interactions. Though an antagonism between Betahistine and antihistamines could be expected on a theoretical basis, no such interactions have been reported.

In Pregnancy: The safety of Betahistine in human pregnancy has not been completely established, although there is no known teratogenic effect in animals. A careful assessment of potential benefits should be made before prescribing Betahistine in pregnancy.

In Lactation: Betahistine is excreted in the breast milk of nursing mothers in concentrations similar to those found in plasma. Toxicity to the neonate at these concentrations is not known.

Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.

Corticosteroid

Betamethasone Valerate BP is a synthetic adrenocorticosteroid, which is glucocorticoid in nature. It is an analog of prednisolone that also possesses a slight degree of mineral corticosteroid activity. Due to its anti-inflammatory, antipruritic and vasoconstrictive activity, it is very effective and suitable for dermatological use. It is absorbed from the skin and inflammation and/or another disease process in the skin increase percutaneous absorption from the skin. Occlusive dressings substantially increase its percutaneous absorption.

Apply sparingly to the affected area two or three times daily until improvement occurs, then twice daily or less. The usual maximum duration of therapy is three weeks.

The following local adverse reactions are more common with the use of high doses, long term use and with the use of occlusive dressings of Cream/Ointment: dryness, itching, burning, skin thinning, local irritation, features of hypercorticolism, telagiectasia, striaea, skin atrophy. hypertrichosis, change in pigmentation, secondary infection, perioral dermatiis, allergic contact dermatitis, maceration of the skin, acneform eruption, exacerbation of symptoms.

Betamethasone Valerate cream or ointment is contraindicated in the following conditions :

• Hypersensitivity to any of the ingredients in the preparation.
• Rosaceae & acne vulgaris.
• Perioral dermatitis, perianal & genital pruritis.
• Viral infections of the skin, e.g. herpes simplex & chicken pox.
• Primary infected skin lesions caused by fungi or bacteria.
• Dermatoses in children under one year of age.

Betamethasone Cream/Ointment is usually well tolerated but if signs of hypersensitivity appear, application should be stopped. Long term continuous topical therapy should be avoided where possible, particularly in children as adrenal suppression may occur even without occlusion. When extensive areas are treated, sufficient systemic absorption may occur to produce symptoms of hypercorticolism. This effect is more likely if occlusive dressings are used, or if the treatment is prolonged. The face or other areas of the body may exhibit atrophic changes after prolonged treatment. If applied to the eyelids, care is needed to ensure that the preparation does not enter the eye, as glaucoma might result. Any spread of the infection requires withdrawal of topical corticosteroid therapy.

There are no significant drug interactions reported with Betamethasone Cream/Ointment.

It should not be used extensively in pregnancy.

Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.

Corticosteroid

Betamethasone Valerate BP is a synthetic adrenocorticosteroid, which is glucocorticoid in nature. It is an analog of prednisolone that also possesses a slight degree of mineral corticosteroid activity. Due to its anti-inflammatory, antipruritic and vasoconstrictive activity, it is very effective and suitable for dermatological use. It is absorbed from the skin and inflammation and/or another disease process in the skin increase percutaneous absorption from the skin. Occlusive dressings substantially increase its percutaneous absorption.

Apply sparingly to the affected area two or three times daily until improvement occurs, then twice daily or less. The usual maximum duration of therapy is three weeks.

The following local adverse reactions are more common with the use of high doses, long term use and with the use of occlusive dressings of Cream/Ointment: dryness, itching, burning, skin thinning, local irritation, features of hypercorticolism, telagiectasia, striaea, skin atrophy. hypertrichosis, change in pigmentation, secondary infection, perioral dermatiis, allergic contact dermatitis, maceration of the skin, acneform eruption, exacerbation of symptoms.

Betamethasone Valerate cream or ointment is contraindicated in the following conditions :

• Hypersensitivity to any of the ingredients in the preparation.
• Rosaceae & acne vulgaris.
• Perioral dermatitis, perianal & genital pruritis.
• Viral infections of the skin, e.g. herpes simplex & chicken pox.
• Primary infected skin lesions caused by fungi or bacteria.
• Dermatoses in children under one year of age.

Betamethasone Cream/Ointment is usually well tolerated but if signs of hypersensitivity appear, application should be stopped. Long term continuous topical therapy should be avoided where possible, particularly in children as adrenal suppression may occur even without occlusion. When extensive areas are treated, sufficient systemic absorption may occur to produce symptoms of hypercorticolism. This effect is more likely if occlusive dressings are used, or if the treatment is prolonged. The face or other areas of the body may exhibit atrophic changes after prolonged treatment. If applied to the eyelids, care is needed to ensure that the preparation does not enter the eye, as glaucoma might result. Any spread of the infection requires withdrawal of topical corticosteroid therapy.

There are no significant drug interactions reported with Betamethasone Cream/Ointment.

It should not be used extensively in pregnancy.

Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.

This cream is usually useful for the treatment of superficial infections caused by gram-positive and gramnegative microorganisms. It is also useful in burns, regeneration of new skin in wounds and ulceration, otitis externa, postoperative infections, neuro-dermatitis and eczema. It may be used as an adjunct to systemic steroid therapy in special kind of pyoderma.

Aural steroid & antibiotic combined preparations

Betamethasone is an active topical corticosteroid, which produces a rapid response in the inflammatory dermatoses and cures psoriasis types of skin diseases. Neomycin Sulfate is a topical broad-spectrum bactericidal amino-glycoside effective against various kinds of gram-positive and gramnegative pathogens such as Proteus vulgaris, Staphylococcus aureus etc. This preparation has effective penetration and uniform distribution capacity, so it is very effective in hairy and intertriginous places. This preparation is very effective for the treatment of wet ulceration of the skin.

Use in adults: This preparation should be applied to the affected parts of the skin as a thin layer for 3 to 4 times daily. In chronic conditions, withdrawal of treatment is carried out by decreasing the frequency of application until the cream is applied as infrequently as once a week. Or as directed by the physician.

Use in children: Do not use it on children under 1 year of age. A course of treatment for a child should not normally last more than 5 days unless otherwise stated by your physician.

This preparation is well tolerated. But prolonged and high doses may cause Cushing's syndrome, acne, thinning and dilatation of blood vessels, particularly when occlusive dressings are used.

This preparation is contraindicated to the patients who are hypersensitive to any of its components. It should not be used for the treatment of otitis externa when the eardrum is perforated. It is contraindicated in skin lesions caused by infection with viruses and fungi.

Long term continuous topical therapy of this preparation should be avoided, which may produce many resistant micro organisms. So, accurate dose of this preparation should be used in infected areas only.

There are no significant drug interactions reported with Betamethasone Valerate BP and Neomycin Sulphate BP Cream/Ointment.

This preparation should not be used extensively in pregnancy.

Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.

This cream is usually useful for the treatment of superficial infections caused by gram-positive and gramnegative microorganisms. It is also useful in burns, regeneration of new skin in wounds and ulceration, otitis externa, postoperative infections, neuro-dermatitis and eczema. It may be used as an adjunct to systemic steroid therapy in special kind of pyoderma.

Aural steroid & antibiotic combined preparations

Betamethasone is an active topical corticosteroid, which produces a rapid response in the inflammatory dermatoses and cures psoriasis types of skin diseases. Neomycin Sulfate is a topical broad-spectrum bactericidal amino-glycoside effective against various kinds of gram-positive and gramnegative pathogens such as Proteus vulgaris, Staphylococcus aureus etc. This preparation has effective penetration and uniform distribution capacity, so it is very effective in hairy and intertriginous places. This preparation is very effective for the treatment of wet ulceration of the skin.

Use in adults: This preparation should be applied to the affected parts of the skin as a thin layer for 3 to 4 times daily. In chronic conditions, withdrawal of treatment is carried out by decreasing the frequency of application until the cream is applied as infrequently as once a week. Or as directed by the physician.

Use in children: Do not use it on children under 1 year of age. A course of treatment for a child should not normally last more than 5 days unless otherwise stated by your physician.

This preparation is well tolerated. But prolonged and high doses may cause Cushing's syndrome, acne, thinning and dilatation of blood vessels, particularly when occlusive dressings are used.

This preparation is contraindicated to the patients who are hypersensitive to any of its components. It should not be used for the treatment of otitis externa when the eardrum is perforated. It is contraindicated in skin lesions caused by infection with viruses and fungi.

Long term continuous topical therapy of this preparation should be avoided, which may produce many resistant micro organisms. So, accurate dose of this preparation should be used in infected areas only.

There are no significant drug interactions reported with Betamethasone Valerate BP and Neomycin Sulphate BP Cream/Ointment.

This preparation should not be used extensively in pregnancy.

Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.

This topical preparation is indicated for the topical treatment of inflammatory dermal infections like-

• Tinea pedis
• Tinea cruris
• Tinea corporis etc.

Betamethasone & Combined preparations

Clotrimazole is a broad-spectrum antifungal agent used for the treatment of superficial infections caused by species of pathogenic dermatophytes, yeasts and Malassezia furfur. The mechanism of action involves inhibition of the synthesis of ergosterol, a major sterol in the fungal cell membrane. This leads to instability of the cell membrane and eventual death of the fungus. Betamethasone dipropionate is a corticosteroid with anti-inflammatory, antipruritic, and vasoconstrictive properties. But the exact mechanism of action of corticosteroids is not clearly known.

Sufficient topical preparation should be applied onto the affected and surrounding skin areas twice a day, in the morning and evening, for 2 weeks in tinea cruris and tinea corporis and for 4 weeks in tinea pedis. The use of this cream for longer than four weeks is not recommended.

The safety and effectiveness of the preparation have not been established in children below the age of 12 years.

Adverse reactions reported for the preparation in clinical trials were paresthesia in 1.9% of patients, rash, edema and secondary infection, each in less than 1% of patients. Other adverse reactions reported with the preparation were burning and dry skin in 1.6% of patients and stinging in less than 1% of patients

This topical preparation is contraindicated to those patients who are sensitive to any of its components or to other corticosteroids or to imidazoles. If irritation or sensitization develops with the use of the cream, treatment should be discontinued and appropriate therapy instituted. The cream is contraindicated in facial rosacea, acne vulgaris, perioral dermatits, perianal and genital pruritus, napkin eruptions and bacterial or viral infections. Systemic absorption of topical corticosteroides can produce reversible hypothalmic-pituitary-adrenal (HPA) axis suppression. If HPA axis suppression is noted, an attempt should be made to withdraw the drug or to reduce the frequency of application. Pediatric patients may be more susceptible to systemic toxicity from equivalent doses due to their large skin surface to body mass ratios.

No information is available of drug interaction.

There is inadequate evidence of safety in pregnancy. Clotrimazole has no teratogenic effect in animals but is foetotoxic at high oral doses. Topical administration of corticosteroids to pregnant animals can cause abnormalities of fetal development. Hence the cream should only be used in pregnancy if the benefit justifies the potential risk to the fetus and such use should not be extensive,i.e. in large amounts or for long periods. It is not known whether the components of the preparation are excreted in human milk and therefore caution should be exercised when treating nursing mothers.

Acute overdose with the cream is unlikely and would not be expected to lead to a life-threatening situation. The cream should not be used for longer than the prescribed time period.

Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.

This cream is usually useful for the treatment of superficial infections caused by gram-positive and gramnegative microorganisms. It is also useful in burns, regeneration of new skin in wounds and ulceration, otitis externa, postoperative infections, neuro-dermatitis and eczema. It may be used as an adjunct to systemic steroid therapy in special kind of pyoderma.

Aural steroid & antibiotic combined preparations

Betamethasone is an active topical corticosteroid, which produces a rapid response in the inflammatory dermatoses and cures psoriasis types of skin diseases. Neomycin Sulfate is a topical broad-spectrum bactericidal amino-glycoside effective against various kinds of gram-positive and gramnegative pathogens such as Proteus vulgaris, Staphylococcus aureus etc. This preparation has effective penetration and uniform distribution capacity, so it is very effective in hairy and intertriginous places. This preparation is very effective for the treatment of wet ulceration of the skin.

Use in adults: This preparation should be applied to the affected parts of the skin as a thin layer for 3 to 4 times daily. In chronic conditions, withdrawal of treatment is carried out by decreasing the frequency of application until the cream is applied as infrequently as once a week. Or as directed by the physician.

Use in children: Do not use it on children under 1 year of age. A course of treatment for a child should not normally last more than 5 days unless otherwise stated by your physician.

This preparation is well tolerated. But prolonged and high doses may cause Cushing's syndrome, acne, thinning and dilatation of blood vessels, particularly when occlusive dressings are used.

This preparation is contraindicated to the patients who are hypersensitive to any of its components. It should not be used for the treatment of otitis externa when the eardrum is perforated. It is contraindicated in skin lesions caused by infection with viruses and fungi.

Long term continuous topical therapy of this preparation should be avoided, which may produce many resistant micro organisms. So, accurate dose of this preparation should be used in infected areas only.

There are no significant drug interactions reported with Betamethasone Valerate BP and Neomycin Sulphate BP Cream/Ointment.

This preparation should not be used extensively in pregnancy.

Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.

Betaxolol ophthalmic solution has been shown to be effective in lowering intraocular pressure and is indicated in the treatment of ocular hypertension and chronic open-angle glaucoma. May be used alone or in combination with other intraocular pressure-lowering medication.

Drugs for miotics and glaucoma

Betaxolol is a selective (beta-1-adrenergic) receptor blocking agent that does not have significant membrane stabilizing (local anesthetic) activity and is free from intrinsic sympathomimetic action. When instilled into the eye, Betaxolol reduces elevated as well as normal intraocular pressure, whether or not accompanied by glaucoma. Optic nerve head damage and visual field loss are results of a sustained elevated intraocular pressure and poor ocular perfusion. The ocular hypotensive action of Betaxolol appears to be mediated by a reduction of aqueous production as demonstrated by tonography and aqueous flurophotometry. Betaxolol ophthalmic solution does not produce miosis or accommodative spasm which is frequently seen with miotic.

The onset of action with Betaxolol can generally be noted within 30 minutes and the maximal effect can usually be detected two hours after topical administration. A single dose provides a 12-hour reduction in intraocular pressure (IOP) and twice daily administration maintains the IOP below 22 mm Hg in most patients.

0.5% ophthalmic solution: The usual dose is 1 drop of Betaxolol Hydrochloride ophthalmic solution in the affected eye(s) twice daily. In some patients, the intraocular pressure-lowering response may require a few weeks to stabilize. Clinical follow-up should include a determination of the intraocular pressure during the first month of treatment. Thereafter, intraocular pressure should be determined on an individual basis at the judgment of the physician.

0.25% ophthalmic solution: The recommended dose is one to two drops of Betaxolol Hydrochloride ophthalmic solution in the affected eye(s) twice daily.

Pediatric Use: Safety and effectiveness in pediatric patients have not been established.

Geriatric Use: No overall differences in safety or effectiveness have been observed between elderly and younger patients.

Ocular: Discomfort of short duration, occasional tearing has been reported. Rare instances of decreased corneal sensitivity, erythema, itching sensation, corneal punctuate staining, keratitis, edema and photophobia have been reported.

Systemic: Systemic reactions following administration of Betaxolol hydrochloride ophthalmic solution 0.5% have been rarely reported. These include:

• Cardiovascular: bradycardia, heart block, congestive heart failure.
• Respiratory: bronchospasm, respiratory failure.
• Others: Hives, toxic epidermal necrolysis, hair loss and glossitis.

Hypersensitivity to any component of this product. Betaxolol should not be used in patients with sinus bradycardia, atrioventricular block greater than first degree, cardiogenic shock, or patients with a history of overt cardiac failure.

In patients with angle-closure glaucoma, the immediate treatment objective is to re-open the angle by constriction of the pupil with miotic agent. Betaxolol has no effect on the pupil; therefore, Betaxolol should be used with a miotic to reduce elevated intraocular pressure in angle-closure glaucoma. Beta-adrenergic blocking agents should be administered with caution in patients subjected to spontaneous hypoglycemia or to diabetic patients as these agents may mask the signs and symptoms of acute hypoglycemia.

Patients who are receiving a beta-adrenergic blocking agent orally and Betaxolol Hydrochloride Ophthalmic Solution should be observed for a potential additive effect either on the intraocular pressure or on the known systemic effects of beta blockade. Close observation of the patient is recommended when a beta blocker is administered to patients receiving catecholamine-depleting drugs such as reserpine, because of possible additive effects and the production of hypotension and/or bradycardia. Caution should be exercised in patients using concomitant adrenergic psychotropic drugs. In patients with angle-closure glaucoma, the immediate treatment objective is to reopen the angle by constriction of the pupil with a miotic agent. Betaxolol has little or no effect on the pupil. When Betaxolol Hydrochloride Ophthalmic Solution is used to reduce elevated intraocular pressure in angle-closure glaucoma, it should be used with a miotic and not alone.

There are no adequate & well controlled studies in pregnant women. Betaxolol ophthalmic solution should be used during pregnancy only if the potential benefit justifies the potential risk. It is not known whether Betaxolol is excreted in human milk. The risk of hypoglycemia & bradycardia in nursing infant has not been evaluated. Breast feeding is not recommended during treatment.

No information is available on overdosage. A topical overdosage of Betaxolol ophthalmic solution may be flushed from the eye(s) with warm tap water.

Store at room temperature. It is desirable that the content should not be used more than one month after first opening of the bottle.

Mirabegron is indicated for the symptomatic treatment of urgency, increased micturition frequency and urgency incontinence as may occur in adult patients with overactive bladder (OAB) syndrome.

BPH/ Urinary retention/ Urinary incontinence

Mirabegron is the first beta-3 adrenoceptor agonist. Mirabegron exerts its effect via a dual mechanism, both directly acts on the bladder smooth muscle and also via the sensory nervous system, it increases the levels of cyclic adenosine monophosphate (cyclic AMP) and leads to relaxation of the detrusor smooth muscle during storage phase of urinary bladder fill-void cycle by activation of beta-3 adrenoceptor which increase bladder capacity.

Adults including elderly: The recommended starting dose is Mirabegron 25 mg tablet once daily with or without food. Based on individual patient efficacy and tolerability the dose may be increased to Mirabegron 50 mg tablet once daily.

Renal or hepatic impairment:

• Patients with severe renal impairment (ClCr 15 to 29 mL/min or eGFR 15 to 29 mL/min/1.73 m2) or moderate hepatic impairment (Child-Pugh Class B), the daily dose of Mirabegron should not exceed 25 mg tablet once daily.
• Mirabegron has not been studied in patients with end stage renal disease (GFR <15 mL/min/1.73 m2 or patients requiring haemodialysis) or severe hepatic impairment (Child Pugh Class C) and it is therefore not recommended for use in these patient populations.

Gender: No dose adjustment is necessary according to gender.

Paediatric population: The safety and efficacy of Mirabegron in children below 18 years of age have not yet been established.

Mirabegron tablet is to be taken once daily, with liquids, swallowed whole and is not to be chewed, divided, or crushed.

The most common side effects reported for patients treated with Mirabegron 50 mg during the three 12-week phase 3 double blind, placebo controlled studies are tachycardia and urinary tract infections. The frequency of tachycardia was 1.2% in patients receiving Mirabegron 50 mg. Tachycardia led to discontinuation in 0.1% patients receiving Mirabegron 50 mg. The frequency of urinary tract infections was 2.9% in patients receiving Mirabegron 50 mg. Urinary tract infections led to discontinuation in none of the patients receiving Mirabegron 50 mg. Serious adverse reactions included atrial fibrillation (0.2%).

Mirabegron is contraindicated in patients with hypersensitivity to the active substance or to any of the excipients and severe uncontrolled hypertension defined as systolic blood pressure 180 mm Hg and/or diastolic blood pressure 110 mm Hg.

Renal impairment: Mirabegron has not been studied in patients with end stage renal disease (GFR <15 mL/min/1.73 m2 or patients requiring haemodialysis) and therefore, it is not recommended for use in this patient population. Data are limited in patients with severe renal impairment (GFR 15 to 29 mL/min/1.73 m2); based on a pharmacokinetic study a dose reduction to 25 mg is recommended in this population. Mirabegron is not recommended for use in patients with severe renal impairment (GFR 15 to 29 mL/min/1.73 m2) concomitantly receiving strong CYP3A inhibitors.

Hepatic impairment: Mirabegron has not been studied in patients with severe hepatic impairment (Child-Pugh Class C) and, therefore, it is not recommended for use in this patient population. Mirabegron is not recommended for use in patients with moderate hepatic impairment (Child-Pugh Class B) concomitantly receiving strong CYP3A inhibitors.

Hypertension: Mirabegron can increase blood pressure. Blood pressure should be measured at baseline and periodically during treatment with Mirabegron, especially in hypertensive patients. Data are limited in patients with stage 2 hypertension (systolic blood pressure 160 mm Hg or diastolic blood pressure 100 mm Hg).

Patients with congenital or acquired QT prolongation: Caution should be exercised when administering Mirabegron in patients with congenital or acquired QT prolongation.

Patients with bladder outlet obstruction and patients taking antimuscarinics medications for OAB: A controlled clinical safety study in patients with bladder outlet obstruction (BOO) did not demonstrate increased urinary retention in patients treated with Mirabegron; however, Mirabegron should be administered with caution to patients with clinically significant bladder outlet obstruction. Mirabegron should also be administered with caution to patients taking antimuscarinic medications for the treatment of OAB.

Effect of enzyme inhibitors: Mirabegron exposure (AUC) was increased 1.8-fold in the presence of the strong inhibitor of CYP3A/P-gp ketoconazole in healthy volunteers. No dose adjustment is needed when Mirabegron is combined with inhibitors of CYP3A and/or P-gp. However, in patients with mild to moderate renal impairment or mild hepatic impairment concomitantly receiving strong CYP3A inhibitors, such as itraconazole, ketoconazole, ritonavir and clarithromycin, the recommended dose is 25 mg once daily with or without food. Mirabegron is not recommended in patients with severe renal impairment or patients with moderate hepatic impairment concomitantly receiving strong CYP3A inhibitors.

Effect of enzyme inducers: Substances that are inducers of CYP3A or P-gp decrease the plasma concentrations of Mirabegron. No dose adjustment is needed for Mirabegron when administered with therapeutic doses of rifampicin or other CYP3A or P-gp inducers.

Effect of Mirabegron on CYP2D6 substrates: In healthy volunteers, the inhibitory potency of Mirabegron towards CYP2D6 is moderate and the CYP2D6 activity recovers within 15 days after discontinuation of Mirabegron. Multiple once daily dosing of Mirabegron IR resulted in a 90% increase in Cmax and a 229% increase in AUC of a single dose of metoprolol. Multiple once daily dosing of Mirabegron resulted in a 79% increase in Cmax and a 241% increase in AUC of a single dose of desipramine. Caution is advised if Mirabegron is co-administered with medicinal products with a narrow therapeutic index and significantly metabolised by CYP2D6, such as thioridazine, Type 1 C antiarrhythmics (e.g., flecainide, propafenone) and tricyclic antidepressants (e.g., imipramine, desipramine). Caution is also advised if Mirabegron is co-administered with CYP2D6 substrates that are individually dose titrated.

Effect of Mirabegron on transporters: Mirabegron is a weak inhibitor of P-gp. Mirabegron increased Cmax and AUC by 29% and 27%, respectively, of the P-gp substrate digoxin in healthy volunteers. For patients who are initiating a combination of Mirabegron and digoxin, the lowest dose for digoxin should be prescribed initially. Serum digoxin concentrations should be monitored and used for titration of the digoxin dose to obtain the desired clinical effect.

Other interactions: No clinically relevant interactions have been observed when Mirabegron was co-administered with therapeutic doses of solifenacin, tamsulosin, warfarin, metformin or a combined oral contraceptive medicinal product containing ethinylestradiol and levonorgestrel. Dose-adjustment is not recommended.

There are limited amount of data from the use of Mirabegron in pregnant women. Studies in animals have shown reproductive toxicity. Mirabegron is not recommended during pregnancy and in women is planning to be pregnant. Mirabegron is excreted in the milk of rodents and therefore is predicted to be present in human milk. No studies have been conducted to assess the impact of Mirabegron on milk production in humans, its presence in human breast milk, or its effects on the breast-fed child. Mirabegron should not be administered during breast-feeding. There were no treatment-related effects of Mirabegron on fertility in animals. The effect of Mirabegron on human fertility has not been established.

Mirabegron has been administered to healthy volunteers at single doses up to 400 mg. At this dose, adverse events reported included palpitations and increased pulse rate exceeding 100 beats per minute (bpm). Multiple doses of Mirabegron up to 300 mg daily for 10 days showed increases in pulse rate and systolic blood pressure when administered to healthy volunteers. Treatment for overdose should be symptomatic and supportive. In the event of overdose, pulse rate, blood pressure, and ECG monitoring is recommended.

Store in a cool and dry place, protected from light.

Mirabegron is indicated for the symptomatic treatment of urgency, increased micturition frequency and urgency incontinence as may occur in adult patients with overactive bladder (OAB) syndrome.

BPH/ Urinary retention/ Urinary incontinence

Mirabegron is the first beta-3 adrenoceptor agonist. Mirabegron exerts its effect via a dual mechanism, both directly acts on the bladder smooth muscle and also via the sensory nervous system, it increases the levels of cyclic adenosine monophosphate (cyclic AMP) and leads to relaxation of the detrusor smooth muscle during storage phase of urinary bladder fill-void cycle by activation of beta-3 adrenoceptor which increase bladder capacity.

Adults including elderly: The recommended starting dose is Mirabegron 25 mg tablet once daily with or without food. Based on individual patient efficacy and tolerability the dose may be increased to Mirabegron 50 mg tablet once daily.

Renal or hepatic impairment:

• Patients with severe renal impairment (ClCr 15 to 29 mL/min or eGFR 15 to 29 mL/min/1.73 m2) or moderate hepatic impairment (Child-Pugh Class B), the daily dose of Mirabegron should not exceed 25 mg tablet once daily.
• Mirabegron has not been studied in patients with end stage renal disease (GFR <15 mL/min/1.73 m2 or patients requiring haemodialysis) or severe hepatic impairment (Child Pugh Class C) and it is therefore not recommended for use in these patient populations.

Gender: No dose adjustment is necessary according to gender.

Paediatric population: The safety and efficacy of Mirabegron in children below 18 years of age have not yet been established.

Mirabegron tablet is to be taken once daily, with liquids, swallowed whole and is not to be chewed, divided, or crushed.

The most common side effects reported for patients treated with Mirabegron 50 mg during the three 12-week phase 3 double blind, placebo controlled studies are tachycardia and urinary tract infections. The frequency of tachycardia was 1.2% in patients receiving Mirabegron 50 mg. Tachycardia led to discontinuation in 0.1% patients receiving Mirabegron 50 mg. The frequency of urinary tract infections was 2.9% in patients receiving Mirabegron 50 mg. Urinary tract infections led to discontinuation in none of the patients receiving Mirabegron 50 mg. Serious adverse reactions included atrial fibrillation (0.2%).

Mirabegron is contraindicated in patients with hypersensitivity to the active substance or to any of the excipients and severe uncontrolled hypertension defined as systolic blood pressure 180 mm Hg and/or diastolic blood pressure 110 mm Hg.

Renal impairment: Mirabegron has not been studied in patients with end stage renal disease (GFR <15 mL/min/1.73 m2 or patients requiring haemodialysis) and therefore, it is not recommended for use in this patient population. Data are limited in patients with severe renal impairment (GFR 15 to 29 mL/min/1.73 m2); based on a pharmacokinetic study a dose reduction to 25 mg is recommended in this population. Mirabegron is not recommended for use in patients with severe renal impairment (GFR 15 to 29 mL/min/1.73 m2) concomitantly receiving strong CYP3A inhibitors.

Hepatic impairment: Mirabegron has not been studied in patients with severe hepatic impairment (Child-Pugh Class C) and, therefore, it is not recommended for use in this patient population. Mirabegron is not recommended for use in patients with moderate hepatic impairment (Child-Pugh Class B) concomitantly receiving strong CYP3A inhibitors.

Hypertension: Mirabegron can increase blood pressure. Blood pressure should be measured at baseline and periodically during treatment with Mirabegron, especially in hypertensive patients. Data are limited in patients with stage 2 hypertension (systolic blood pressure 160 mm Hg or diastolic blood pressure 100 mm Hg).

Patients with congenital or acquired QT prolongation: Caution should be exercised when administering Mirabegron in patients with congenital or acquired QT prolongation.

Patients with bladder outlet obstruction and patients taking antimuscarinics medications for OAB: A controlled clinical safety study in patients with bladder outlet obstruction (BOO) did not demonstrate increased urinary retention in patients treated with Mirabegron; however, Mirabegron should be administered with caution to patients with clinically significant bladder outlet obstruction. Mirabegron should also be administered with caution to patients taking antimuscarinic medications for the treatment of OAB.

Effect of enzyme inhibitors: Mirabegron exposure (AUC) was increased 1.8-fold in the presence of the strong inhibitor of CYP3A/P-gp ketoconazole in healthy volunteers. No dose adjustment is needed when Mirabegron is combined with inhibitors of CYP3A and/or P-gp. However, in patients with mild to moderate renal impairment or mild hepatic impairment concomitantly receiving strong CYP3A inhibitors, such as itraconazole, ketoconazole, ritonavir and clarithromycin, the recommended dose is 25 mg once daily with or without food. Mirabegron is not recommended in patients with severe renal impairment or patients with moderate hepatic impairment concomitantly receiving strong CYP3A inhibitors.

Effect of enzyme inducers: Substances that are inducers of CYP3A or P-gp decrease the plasma concentrations of Mirabegron. No dose adjustment is needed for Mirabegron when administered with therapeutic doses of rifampicin or other CYP3A or P-gp inducers.

Effect of Mirabegron on CYP2D6 substrates: In healthy volunteers, the inhibitory potency of Mirabegron towards CYP2D6 is moderate and the CYP2D6 activity recovers within 15 days after discontinuation of Mirabegron. Multiple once daily dosing of Mirabegron IR resulted in a 90% increase in Cmax and a 229% increase in AUC of a single dose of metoprolol. Multiple once daily dosing of Mirabegron resulted in a 79% increase in Cmax and a 241% increase in AUC of a single dose of desipramine. Caution is advised if Mirabegron is co-administered with medicinal products with a narrow therapeutic index and significantly metabolised by CYP2D6, such as thioridazine, Type 1 C antiarrhythmics (e.g., flecainide, propafenone) and tricyclic antidepressants (e.g., imipramine, desipramine). Caution is also advised if Mirabegron is co-administered with CYP2D6 substrates that are individually dose titrated.

Effect of Mirabegron on transporters: Mirabegron is a weak inhibitor of P-gp. Mirabegron increased Cmax and AUC by 29% and 27%, respectively, of the P-gp substrate digoxin in healthy volunteers. For patients who are initiating a combination of Mirabegron and digoxin, the lowest dose for digoxin should be prescribed initially. Serum digoxin concentrations should be monitored and used for titration of the digoxin dose to obtain the desired clinical effect.

Other interactions: No clinically relevant interactions have been observed when Mirabegron was co-administered with therapeutic doses of solifenacin, tamsulosin, warfarin, metformin or a combined oral contraceptive medicinal product containing ethinylestradiol and levonorgestrel. Dose-adjustment is not recommended.

There are limited amount of data from the use of Mirabegron in pregnant women. Studies in animals have shown reproductive toxicity. Mirabegron is not recommended during pregnancy and in women is planning to be pregnant. Mirabegron is excreted in the milk of rodents and therefore is predicted to be present in human milk. No studies have been conducted to assess the impact of Mirabegron on milk production in humans, its presence in human breast milk, or its effects on the breast-fed child. Mirabegron should not be administered during breast-feeding. There were no treatment-related effects of Mirabegron on fertility in animals. The effect of Mirabegron on human fertility has not been established.

Mirabegron has been administered to healthy volunteers at single doses up to 400 mg. At this dose, adverse events reported included palpitations and increased pulse rate exceeding 100 beats per minute (bpm). Multiple doses of Mirabegron up to 300 mg daily for 10 days showed increases in pulse rate and systolic blood pressure when administered to healthy volunteers. Treatment for overdose should be symptomatic and supportive. In the event of overdose, pulse rate, blood pressure, and ECG monitoring is recommended.

Store in a cool and dry place, protected from light.