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Vancomycin 250mg Capsules Hard

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SUMMARY OF PRODUCT CHARACTERISTICS

1    NAME OF THE MEDICINAL PRODUCT

Vancomycin 250mg Capsules, hard

2    QUALITATIVE AND QUANTITATIVE COMPOSITION

Each 250 mg hard capsule contains 250 mg vancomycin (as hydrochloride)

For a full list of excipients, see section 6.1.

3    PHARMACEUTICAL FORM

Capsule, hard

250mg capsule: Brown 21.6 mm hard capsule, containing white to off white congealed liquid mixture as solid mass.

4    CLINICAL PARTICULARS

4.1    Therapeutic indications

Enterocolitis caused by Clostridium difficile.

Vancomycin is not significantly absorbed from the normal gastro-intestinal tract and is therefore not effective by the oral route for other types of infection.

Consideration should be given to official guidance on the appropriate use of antibacterial agents.

4.2    Posology and method of administration

For oral administration.

The capsules should be swallowed whole.

Adults, adolescents and the elderly: 125 mg four times daily (500 mg / day) for 7-10 days. In the treatment of severe cases and recurrences, the dose can be increased up to 500 mg four times daily for 10-14 days.

Children aged 12 years or less: The usual dose is 30-40 mg / kg / day divided in 3-4 doses per day for 7-10 days. The daily dose should not exceed 2 g.

Vancomycin capsules may not be suitable for children below the age of 6 years. Other formulations (e.g. solution) of vancomycin may be available for use instead.

4.3 Contraindications

Hypersensitivity to vancomycin or to any of the excipients.

4.4 Special warnings and precautions for use

Renal impairment and higher serum concentrations of vancomycin

In some patients with severe renal impairment and severe colitis, significant serum concentrations have been measured after repeated dosing. Thus, there is a risk for side effects that are normally only seen after parenteral administration in these patients.

Clinically significant serum concentrations have been reported in some patients who have taken multiple oral doses of vancomycin for active Clostridium difficile -induced pseudomembranous colitis. Therefore, monitoring of serum concentrations may be appropriate in these patients. The risk may be increased in patients with impaired renal function.

Some patients with inflammatory disorders of the intestinal mucosa may have significant systemic absorption of vancomycin and, therefore, may be at risk for the development of adverse reactions associated with the parenteral administration of vancomycin. The risk is greater in patients with renal impairment. It should be noted that the total systemic and renal clearances of vancomycin are reduced in the elderly.

Ototoxicity

Ototoxicity has occurred in patients receiving vancomycin. It may be transient or permanent. It has been reported mostly in patients who have been given excessive intravenous doses, have an underlying hearing loss, or are receiving concomitant therapy with an ototoxic agent such as an aminoglycoside.

Infection

Prolonged use of vancomycin may result in the overgrowth of non-susceptible organisms including fungi. Careful observation of the patient is essential. If superinfection occurs during therapy, appropriate measures should be taken.

4.5 Interaction with other medicinal products and other forms of interaction

No interactions have been reported for orally administered vancomycin. In patients with severe renal impairment and severe colitis systemic absorption may occur resulting in a risk for interactions that are normally only seen after parenteral administration. For example, parenteral administration of vancomycin and anesthetics may cause erythema and anaphylactic reactions.

Some antibiotics were rarely reported to reduce the effect of oral contraceptives by interfering with the bacterial hydrolysis of conjugated steroids in the intestine and thus reabsorption of unconjugated steroid. This would lower the plasma levels of active steroid. This unusual interaction would occur in women with high excretion of conjugated steroids in bile.

Concurrent and/or sequential systemic or topical use of other potentially ototoxic and/or nephrotoxic drugs requires careful monitoring.

4.6 Fertility,Pregnancy and lactation

Pregnancy: The safe use of vancomycin during pregnancy has not been established. Reproductive studies in animals at doses roughly equivalent to the clinical dose based on body surface area (mg/m2), do not indicate any direct or indirect effects on embryonic development, foetus or gestation. Vancomycin should be used during pregnancy only if the benefit outweighs the potential risk.

Breastfeeding: Vancomycin is excreted in human milk. In view of the drug's impact on the nursing mother it should be decided to stop breast-feeding or discontinue treatment.

Fertility: No definitive fertility studies have been conducted.

4.7 Effects on ability to drive and use machines

Vertigo and dizziness have been reported rarely, and may affect the ability to drive and to use machines.

4.8 Undesirable effects

Since vancomycin is normally absorbed only to a limited extent, the risk of systemic toxicity is low.

The following adverse reactions are listed according to MedDRA system organ class and frequency category. Frequency categories are defined using the following convention: very common (>1/10); common (>1/100 to <1/10); 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).

Blood and lymphatic system disorders:

Rare: Leukopenia, thrombocytopenia, eosinophilia, reversible agranulocytosis.

Immune system disorders

Not known: Drug rash with eosinophilia and systemic symptoms (DRESS syndrome) has been reported

during postmarketing experience.

Ear and labyrinth disorders:

Uncommon: Hearing loss.

Rare: Tinnitus.

Cardiac disorders:

Very rare: Cardiac arrest

Vascular disorders:

Rare: Hypotension, vasculitis.

Respiratory, thoracic and mediastinal disorders:

Rare: Shortness of breath, stridor.

Gastrointestinal disorders:

Uncommon: Nausea.

Very rare: Pseudomembranous enterocolitis.

Skin and subcutaneous tissue disorders:

Uncommon: Rash, pruritus

Rare: Redness on the upper body, urticaria, Stevens-Johnson syndrome, toxic epidermal necrolysis, IgA induced bullous dermatitis.

Musculoskeletal and connective tissue disorders:

Rare: Muscle cramps and pains in the chest and back.

Renal and urinary disorders:

Rare: Renal failure, elevated serum creatinine, interstitial nephritis.

General disorders and administration site conditions: Uncommon: Fever.

Rare: Anaphylactic reactions, chills, dizziness.

Elevated serum creatinine as a sign of renal involvement have been reported mainly for intravenous vancomycin. A few cases of interstitial nephritis have been reported, mostly associated with concomitant use of aminoglycosides or for patients with previously impaired renal function. Renal side effects are reversible. Hearing loss has been reported in a dozen cases with intravenous vancomycin, most associated with renal impairment or previous hearing loss, or concomitant treatment with ototoxic drugs. Reversible neutropenia, after about a week of intravenous vancomycin therapy or total dose of 25 g, have been reported in few cases. Isolated cases of agranulocytosis have been reported, but the relationship to vancomycin has not been verified.

4.9 Overdose

Toxicity: Limited experience in overdose, however, 500 mg IV given to a 2-year-old lead to lethal intoxication. 56 g spread over 10 days to an adult caused renal insufficiency.

Symptoms: Overdose may cause nausea, vomiting, epigastric discomfort and diarrhoea. Possible symptoms that have been reported as side effects (see section 4.8) are reinforced in overdose. Possible renal symptoms.

Treatment: Gastric lavage, charcoal in repeated doses (reducing half-life). Ensure adequate diuresis. Hemodialysis or hemoperfusion can be used when toxic symptoms and concomitant renal insufficiency occur. Symptomatic treatment.

5 PHARMACOLOGICAL PROPERTIES

5.1 Pharmacodynamic properties

ATC classification

Pharmacotherapeutic group: intestinal antiinfectives, antibiotics, ATC code: A07AA09

Mode of action

Vancomycin is a tricyclic glycopeptide antibiotic that inhibits the syntesis of the cell wall in sensitive bacteria by binding with high affinity to the D-alanyl-D-alanine terminus of cell wall precursor units. In addition, it impairs the permeability of the bacterial cell membrane and RNA synthesis.

PK/PD relationship

Vancomycin activity is considered to be time-dependent.

Mechanism(s) of resistance

Acquired resistance to glycopeptides is most common in enterococci and is based on acquisition of various van gene complexes which modifies the D-alanyl-D-alanine target to D-alanyl-D-lactate or D-alanyl-D-serine which bind vancomycin poorly. In some countries, increasing cases of resistance are observed in enterococci; multiresistant strains of Enterococcus faecium are especially alarming.

Van genes have rarely been found in Staphylococcus aureus, where changes in cell wall structure result in “intermediate” susceptibility, which is most commonly heterogeneous.

There is no cross-resistance between vancomycin and other antibiotics but crossresistance with other glycopeptide antibiotics, such as teicoplanin, does occur. Secondary development of resistance during therapy is rare.

Orally administered vancomycin is active against Clostridium difficile

Susceptibility

The prevalence of acquired resistance may vary geographically and with time for selected species and local information on resistance is desirable, particularly when treating severe infections. As necessary, expert advice should be sought when the local prevalence of resistance is such that the utility of the agent in at least some types of infections is questionable.

Commonly susceptible species

Clostridium difficile


5.2 Pharmacokinetic properties

After oral administration of vancomycin in healthy volunteers and patients with inflammatory bowel disease and normal renal function, absorption is low. With repeated dosing of 125 mg every 6 hours faecal concentration exceeds 100 mg / kg in

the majority of samples. No vancomycin was detectable in the blood and urinary recovery was less than 1%.

Measurable serum concentrations may occur infrequently in patients with active C. difficile -induced pseudomembranous colitis and, in the presence of renal impairment, there is a risk of accumulation.

Administration of vancomycin oral solution, 2 g daily for 16 days to anephric patients with no inflammatory bowel disease, gave measurable serum levels of >0.66 pg/ml in 2 out of 5 patients. With doses of 2 g daily, concentrations of >3,100 mg/kg were found in the faeces and levels of <1 pg/ml were found in the serum of patients with normal renal function who had pseudomembranous colitis.

Following parenteral administration vancomycin is excreted renally, nearly completely as the microbiologically active substance. The serum half life in adult patients with normal renal function has been reported to be about 4-6 hours, in children 2.2-3 hours. Impaired renal function can prolong the elimination (up to 7.5 days).

5.3 Preclinical safety data

Non-clinical data reveal no special hazard for humans based on conventional studies of safety pharmacology and repeated dose toxicity.

Limited data on mutagenic effects show negative results, long-term studies in animals regarding a carcinogenic potential are not available. In teratogenicity studies, where rats and rabbits received doses approximately corresponding to the human dose based on body surface (mg/m2), no direct or indirect teratogenic effects were observed.

Animal studies of the use during the perinatal/postnatal period and regarding effects on fertility are not available.

6 PHARMACEUTICAL PARTICULARS

6.1 List of excipients

Capsule content Macrogol 6000

Capsule cap and body Titanium Dioxide (E 171)

Iron oxide black (E 172)

Iron oxide red (E 172)

Iron oxide yellow (E 172) Gelatin

6.2    Incompatibilities

Not applicable

6.3    Shelf life

2 years

6.4    Special precautions for storage

Do not store above 25°C

6.5    Nature and contents of container

PVC/PE/ACLAR/aluminium blister packs 28 and 30 capsules

Not all pack sizes may be marketed.

6.6    Special precautions for disposal

No special requirements

Any unused product or waste material should be disposed of in accordance with local requirements.

7    MARKETING AUTHORISATION HOLDER

Actavis Group PTC ehf.

Reykjavikurvegi 76-78 220 Hafnarfjordur Iceland

MARKETING AUTHORISATION NUMBER(S)

8


PL 30306/0396

9    DATE OF FIRST AUTHORISATION/RENEWAL OF THE AUTHORISATION

30/10/2012

10    DATE OF REVISION OF THE TEXT

04/01/2013