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V Penicillin Biotika Tabl. 0,4, 0,8, 1,2 Mega

1. NAME OF THE MEDICINAL PRODUCT

V - PENICILIN 0,4 MEGA BIOTIKA

V - PENICILIN 0,8 MEGA BIOTIKA

V - PENICILIN 1,2 MEGA BIOTIKA

2. QUALITATIVE AND QUANTITATIVE COMPOSITION

                            Phenoxymethylpenicillinum kalicum  400 000 IU (261 mg) in 1 tablet or

                            Phenoxymethylpenicillinum kalicum  800 000 IU (523 mg) in 1 tablet or

                            Phenoxymethylpenicillinum kalicum  1 200 000 IU (784 mg) in 1 tablet

3. PHARMACEUTICAL FORM

Tablets

Description:

0,4 Mega and 0,8 Mega: almost white, round, flat tablets with bevelled edges with dividing line on one side.

1,2 Mega: almost white, elongated biconvex tablets with dividing line on one side.

4. CLINICAL PARTICULARS

4.1. Therapeutic indications 

Treatment of light and medium-severe infections induced by micro-organisms sensitive to penicillin. These are the infections of respiratory tract (bronchitis, bronchopneumonia, pneumonia), infections in the area of throat, nose and ears (pharyngitis, tonsillitis, sinusitis, otitis media), infections in the area of face and mouth coming from teeth; skin infections (erysipelas, erysipeloid, migrating erythema), inflammation of lymph-nodes and lymph-vessels; scarlet fever (also prophylactically).

Prevention of endocarditis in intervention in the area of teeth, mouth and jaws or upper airways.

Prevention of acute rheumatic fever.

4.2. Posology and method of administration

Dosage is individual depending on a character and a severity of the infection. According to the latest empiric experiences phenoxymethylpenicillin is effective also if it is applied 3 times daily.

Usual dosage of V-Penicillin:

Children older than 3 years and up to 25 kg of body weight are applied 400 000 IU each 8 hours.

Children from 25 to 40 kg of body weight 400 000 – 800 000 IU each 8 hours.

Adolescents and adults up to 70 kg of body weight 800 000 IU each 8 hours.

Adults older than 70 kg of body weight 800 000 – 1 200 000 IU each 8 hours.

Depending on sensitivity of etiological agent and kind and severity of disease the doctor may adjust the doses accordingly.

The best application of the tablets is one hour before meals, unchewed and drink with glass of water (200 – 250 mL). If the tablets are taken after meals, passage of active substance into blood circle may be delayed or even reduced.

The doctor decides always on duration of treatment by penicillin. Phenoxymethylpenicillin is taken usually 7 – 10 days, at least 2 – 3 days after disease symptoms have subsided. In any case treatment must not be discontinued arbitrarily after clinical symptoms of disease have subsided, because it is connected with a risk of disease relapse and later complications (rheumatic fever, glomerulonephritis).

Maximum dose is not indicated, because penicillin is a substance with low toxicity and wide therapeutic index.

In elderly patients with renal insufficiency the biological half-life of phenoxymethylpenicillin is prolonged for about 4 hours therefore it is suitable to prolong the time interval between the individual doses.

4.3. Contraindications

A b s o l u t e :  known sensitivity to penicillins and cephalosporins. Patient should be informed that the symptoms (urticaria, fever, pain of joints) may appear unexpectedly after initiation of treatment and these symptoms are to be advised of to the doctor without any delay.

R e l a t i v e :  the application to patients with urticaria, bronchial asthma and hay fever.

4.4. Special warnings and special precautions for use

In patients with allergy of any kind there is higher probability that the allergic reaction to application of penicillin will occur. Light symptoms of hypersensitivity may appear after medication beginning (itching, urticaria, inflammation of mucosa in the area of mouth and face), by disorders of stomach and intestine activities demonstrated with wamble, vomiting, aches of abdominal cavity, thin stool or diarrhea. They are usually of a light character and disappear often already during treatment or after its interruption. The most severe and extraordinary hypersensitivity symptom is anaphylactic shock which occurs mostly already several minutes after penicillin application. It is shown by failure of heart activity and breathing and an immediate medical help is necessary according to the principles of the first-aid treatment by anaphylactic shock (adrenaline, noradrenalin, hydrocortisone, antihistamines, calcium). Each patient by whom the anaphylactic shock occurs is in acute health risk and requires intensive care in bed medical centre.

4.5. Interaction with other medicinal products and other forms of interaction

Penicillin and other drugs may influence mutually their efficacy. Contraindicated is the concomitant application of V-Penicillin Biotika tables with chemotherapeutics with bacteriostatic effect (tetracyclines, sulfonamides, chloramphenicol etc.), because the decrease of antimicrobial effect occurs.

Salicylates, indometacin, phenylbutazone, sulfinpyrazone increase the Penicillin level in blood serum and prolong its effect. Penicillin may reduce temporary the efficacy of contraceptive preparations and that is why by its application it is recommended to secure the contraception by other alternative.

4.6. Pregnancy and lactation

No teratogenic properties have been found in Penicillin. Therefore V-Penicillin Biotika tbl., at occurrence of infections induced by penicillin–sensitive pathogens, may be applied during the whole pregnancy. The drug substance penetrates the breast milk. Maximum levels in milk reach about 50 % of maximum concentrations in serum. In infants fed with this breast milk no undesirable effects were found, however it is not possible to exclude the risk of sensibilization or influencing the intestinal flora. In breast-feeding about 0.1 % of mother dose of Penicillin V penetrates the body of child.

4.7. Effects on ability to drive and use machines

No evidence on reduced ability to drive and use machines has been reported.

4.8. Undesirable effects

The medicinal product is usually well tolerated, but the undesirable effects may occur too.

Disorders in the area of gastrointestinal tract make about 5 to 10 % of the most frequent undesirable effects. These are nausea, vomiting, lack of appetite, pressure in stomach area, flatulency and diarrhea. In occurrence of heavy and persistent diarrhea during the treatment connected with fever and abdominal pains, or after its ending it is necessary to expect the development of pseudomembranous enterocolitis induced by antibiotic which must be treated immediately with vancomycin (4 times 250 mg daily per os). Contraindicated are the peristaltic-inhibiting preparations. Occasionally the exanthema and mucosal inflammations, particularly in the area of mouth (glossitis, stomatitis). Very rarely occurs so called “black hairy tongue”.

After use of the medicinal product the temporary symptoms of xerostomia and changes of taste perception may appear. Occasionally the allergic reactions may occur, mostly in form of skin reactions (exanthema, pruritus). By anaphylactic reaction which is demonstrated by failure of heart activity and breathing the immediate medical health is necessary.

4.9. Overdose

Toxicity of phenoxymethylpenicillin is very low, therapeutic width is extraordinary big. Like in other penicillins, the single per oral use of several doses of phenoxymethylpenicillin has no acute toxic effect. In per oral application it is not possible practically to reach the concentrations which could induce neurotoxic symptoms.

In overdose no special precautions are necessary, except the discontinuation of medication.

Phenoxymethylpenicillin may be eliminated by hemodialysis.


5. PHARMACOLOGICAL PROPERTIES

5.1. Pharmacodynamic properties

Pharmacotherapeutic group: antibiotic

ATC code: J01CE02

Phenoxymethylpenicillin (Penicillin V) is biosynthetic antibiotic, instable against beta-lactamases, stable in acid environment, with bactericidal effect.

Mechanism of action insists in inhibition of synthesis of bacterial cell wall (in growth phase) by blockage of transpeptidases. Spectrum of antibacterial efficacy of Penicillin V is equivalent to spectrum of Penicillin G and includes the following pathogens:

Actinomyces, Bacillus anthracis, Bacteroides, Clostridium, Corynebacterium diphtheriae, Erysipelothrix rhusiopathiae, Fusobacterium, Leptospira, Neisseria gonorrhoeae, Neisseria meningitis, Pasteurella multocida, Spirillum minus, Staphylococcus aureus, Streptobacillus moniliformis, Streptococcus pneumoniae (pneumococci), Streptoccus pyogenes (species A), Streptococcus (species B and C), Streptococcus bovis (species D), Streptococcus viridans, anaerobic streptococci, Treponema, Veillonella.

Penicillin V is not resistant to lactamases and therefore it does not act on pathogens creating these enzymes (e.g. staphylococci or gonococci). Enterococci (Streptococcus faecalis and faecium) are partially sensitive.

In Staphylococcus aureus the resistance is increased even up to 70 %. In pneumococci and gonococci the ratio of resistance is low yet; however the increasing tendency is observed. Sensitivity of gram-positive bacteria is different. There exists a cross resistance between Penicillin V and other per oral penicillins, partially with ampicillin. Therapeutic spectrum of Penicillin V does not conclude Enterobacteriaceae (e.g. Escherichia coli, Klebsiella Enterobacter etc.). Nocardia and Pseudomonas aeruginosa are resistant.

Pathogens with variable sensitivity are as follows:

Bacteroides fragilis and other Bacteroides spp., Brucella, Clostridium perfringens (some strains), Clostridium ramosum (some strains), Fusobacterium mortiferum and Fusobacterium varium.

5.2. Pharmacokinetic properties

Phenoxymethylpenicillin is stable against stomach acid and after passage through stomach it is absorbed in upper part of small intestine. 50 to 60 % is absorbed. Current food intake leads to decreased absorption.

Maximum serum concentrations are reached after 30 to 60 minutes. Serum biological half-life is 30 to 45 minutes. In newborns and patients with decreased renal function the elimination is decelerated. Phenoxymethylpenicillin is excreted by kidneys and small part also by bile. Penicillin V is eliminated by glomerular filtration and tubular secretion by kidneys. In urine taken 0 to 12 hours after application of antibiotic about 25 % of the applied dose is present in unchanged, microbiologically active form. About 30 to 55 % of the dose is detected in urine in form of ineffective metabolites. Phenoxymethylpenicillin penetrates well into tissues and therapeutic concentration is reached in various organs and body fluids. Permeability into liquor is low also by inflamed meninges. Binding to serum proteins is about 60 % (55 – 70 %).

5.3. Preclinical safety data

Acute toxicity testing on mice and rats and chronic toxicity testing on rats and dogs have not provided with an evidence of toxic efficacy of penicillin. Public tests do not point out the mutagenic potential of penicillin. Neither testing on various animal species did not give the evidence of teratogenic effect. Penicillin levels in blood of fetus reached 44 % of concentration in blood of mother. Safety of the medicinal product has been proven by sufficiently long lasting usage in clinical practise.

Ratio between the level in milk and serum level moved by testing in the range between 0.05 to 1.02 (the middle value 0.15) after a single per oral dose of phenoxymethylpenicillin.


6. PHARMACEUTICAL PARTICULARS

6.1. List of excipients

Lactosum monohydricum, cellulosum microcristallinum, silica colloidalis anhydrica, magnesii stearas.

6.2. Incompatibilities

None

6.3. Shelf life

36 months

6.4. Special precautions for storage

Store at 10 ºC to 25 ºC, keep on dry place, protect from light.

6.5. Nature and contents of container

Al/PVC blister, package leaflet: information for the user, paperboard box

Package size:   0.4 Mega: 30 tablets (3 blisters of 10 tablets)

                        0.8 Mega: 30 tablets (3 blisters of 10 tablets)

                        1.2 Mega: 30 tablets (5 blisters of 6 tablets)

6.6. Special precautions for disposal and other handling

The medicinal product is intended for per oral application. The best application of tablets is one hour before meals, unchewed and drunk with glass of water or fruit juice.

7. MARKETING AUTHORISATION HOLDER

BB Pharma a.s., Pod Višňovkou 1662/21, Prague, Czech Republic

8.   MARKETING AUTHORISATION NUMBER

15/0415/96-S, 15/0342/13-S, 15/0343/13-S,

15/639/99-C, 15/640/99-C

9.   DATE OF FIRST AUTHORISATION/RENEWAL OF THE AUTHORISATION  

1996

10. DATE OF REVISION OF THE TEXT

September 2013