Spiramycin ....................... 750,000 IU
Excipients q.s ………….. 1 tablet
Powder for oral suspension.
Product description: White to off-white, dry, loose powder with an aroma and bitterish-sweet taste.
Box of 24 sachets x 3 g.
Pharmacotherapeutic group: Macrolides. ATC code: J01FA02
Spiramycin is a macrolide antibiotic with an antimicrobial spectrum similar to that of erythromycin, although spiramycin in vitro is less active than erythromycin against some susceptible strains. Spiramycin is active against Toxoplasma gondii.
Spiramycin is bacteriostatic against cell division bacteria. Spiramycin is bacteriostatic at serum concentrations but may be bactericidal at tissue concentrations. Spiramycin is known to act at the 50S subunit of bacterial ribosomes and to interfere with bacterial protein synthesis.
Susceptible species
- Spiramycin susceptible bacteria including:
Gram-positive aerobes: Bacillus cereus, Corynebacterium diphtheria, Enterococci, Rhodococcus equi, Staphylococcus methicillin-S, Staphylococcus methicillin-R*, Streptococcus B, non-group Streptococcus, Streptococcus pneumonia, Streptococcus pyogenes.
Gram-negative aerobes: Bordetella pertussis, Branhamella catarrhalis, Campylobacter, Legionella, Moraxella.
Anaerobes: Actinomyces, Bacteroides, Eubacterium, Mobiluncus, Peptostreptococcus, Porphyromonas, Prevotella, Propionibacterium acnes.
Other: Borrelia burgdorferi, Chlamydia, Coxiella, Leptospira, Mycoplasma pneumonia, Treponema pallidum.
- Moderately susceptible species (intermediate susceptibility in vitro):
+ Gram-negative aerobes: Neisseria gonorrhoeae.
+ Anaerobes: Clostridium perfringens.
+ Other: Ureaplasma urealyticum.
Resistant species
A cross-resistance among spiramycin, erythromycin, and oleandomycin has been reported. However, erythromycin-resistant strains are sometimes susceptible to spiramycin.
- Resistant species:
Gram-positive aerobes: Corynebacterium jeikeium, Nocardia asteroids.
Gram-negative aerobes: Acinetobacter, Enterobacteriaceae, Haemophilus, Pseudomonas.
Anaerobes: Fusobacterium.
Other: Mycoplasma hominis.
Spiramycin has in vitro and in vivo activities against Toxoplasma gondii.
* The frequency of methicillin resistance is approximately 30 to 50% for all staphylococci and is mainly
Absorption
The absorption of spiramycin is rapid, but incomplete and is not changed by food.
Distribution
After oral administration of 6 million IU, the maximum serum concentration is 3.3 µg/ml. The plasma half-life is approximately 8 hours. Spiramycin does not enter the CSF. Spiramycin passes into breast milk.
Binding to plasma proteins is weak (10%).
Spiramycin is well distributed into salivary and tissues (lungs: 20 - 60 µg/g, tonsils: 20 - 80 µg/g, infected sinuses: 75 - 110 µg/g, bone: 5 - 100 µg/g).
Ten days after discontinuing treatment, 5 to 7 µg/g of active ingredient is still in spleen, liver, and kidneys. Macrolides penetrate and accumulate in phagocytes (neutrophils, monocytes, peritoneal and alveolar macrophages). In humans, spiramycin reaches high concentrations in phagocytes.
This property explains the activity of macrolides on intracellular bacteria.
Biotransformation
Spiramycin is metabolized in the liver to unknown, active metabolites.
Elimination
10% of the ingested dose is eliminated in urine.
The majority of a dose of spiramycin is excreted in the bile: biliary concentrations are 15 to 40 times higher than serum concentrations.
Spiramycin is excreted partly in faeces.
This medicine does not affect the ability to drive or use machines.
Serious skin reactions including Stevens-Johnson syndrome, Lyell’s syndrome, acute generalised exanthematous pustulosis (AGEP) have been reported with spiramycin. Patients should be informed of signs and symptoms and close monitoring should be performed.
If signs or symptoms of Stevens-Johnson syndrome, Lyell’s syndrome (e.g., progressive rash often accompanied by bubbles or mucosal lesions) or AGEP (acute generalised exanthematous pustulosis) (see section Undesirable effects) occur, the treatment should be discontinued and contraindication of any further administration of spiramycin alone or in combination is recommended.
No dose adjustment is required in patients with renal insufficiency.
As very rare cases of hemolytic anemia have been reported in patients with glucose-6-phosphate dehydrogenase deficiency, the use of spiramycin in such patients is not recommended.
QT interval prolongation
QT interval prolongation has been reported in patients receiving macrolides, including spiramycin.
Spiramycin should be used with caution in patients with known risk factors of QT interval prolongation such as:
- An uncorrected electrolyte imbalance (e.g., hypokalemia, hypomagnesemia),
- A congenital prolonged QT interval syndrome,
- Heart conditions (e.g., heart failure, myocardial infarction, bradycardia),
- Concomitant treatment with medicines known to prolong QT interval (e.g., class Ia and III antiarrhythmics, tricyclic antidepressants, certain antibiotics, certain antipsychotics),
- The elderly, newborns, and women who may be more sensitive to QT interval prolongation.
(See sections Posology and method of administration; Interactions; Undesirable effects; Overdose)
Pregnancy
The use of spiramycin can be considered during pregnancy if necessary. Indeed, the use of spiramycin during pregnancy has not revealed, to date, any malformation or fetotoxic effects.
Breast-feeding
The passage of spiramycin in breast milk is significant. Gastrointestinal disorders have been reported in the newborn. Therefore, the use of spiramycin during breast-feeding is not recommended.
Combinations requiring precaution
+ Medicines likely to induce torsades de pointes: class Ia antiarrhythmics (quinidine, hydroquinidine, disopyramide), class III antiarrhythmics (amiodarone, sotalol, dofetilide, ibutilide), sultopride (benzamide neuroleptics), other antiarrhythmics (arsenic compounds, bepridil, cisapride, diphemanil, dolasetron IV, erythromycin IV, levofloxacin, mizolastine, moxifloxacin, prucalopride, toremifene, vincamine IV).
Increased risk of ventricular arrhythmias, particularly torsades de pointes.
+ Levodopa (when combined with carbidopa)
Inhibition of carbidopa absorption with decreased plasma concentrations of levodopa.
Clinical monitoring and adjustment of levodopa dosage.
Specific problems of the INR imbalance
Many cases of increased activity of oral anticoagulants in patients receiving antibiotics have been reported. The marked infectious or inflammatory context, age, and general condition of the patient appear to be risk factors. In these circumstances, it seems difficult to distinguish between infectious pathology and its treatment in the occurrence of INR imbalance. However, certain classes of antibiotics, including fluoroquinolones, macrolides, cyclins, cotrimoxazole, and certain cephalosporins are highly involved.
The undesirable effects are presented by organ class system and in order of frequency.
The frequencies are defined as follows: 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).
Cardiac disorders
Not known: QT interval prolongation, ventricular arrhythmias, ventricular tachycardia, torsade de pointes which may lead to cardiac arrest (see section Special warnings and precautions for use).
Immune system disorders
Not known: Vasculitis including Henoch-Schönlein purpura or rheumatoid purpura, anaphylactic shock (see section Special warnings and precautions for use).
Gastrointestinal disorders
Common: Abdominal pain, nausea, vomiting, gastralgia, diarrhea, pseudomembranous colitis.
Skin and subcutaneous tissue disorders
Common: Rash.
Not known: Urticaria, pruritus, Quincke’s oedema, Stevens-Johnson syndrome, Lyell’s syndrome, acute generalised exanthematous pustulosis (AGEP) (see section Special warnings and precautions for use).
Central nervous system disorders
Very common: Occasional and transient paraesthesias.
Common: Transient dysgeusia.
Hepatobiliary disorders
Very rare: Abnormal liver tests.
Not known: Cases of cholestatic, mixed, or more rarely cytolytic hepatitis.
Blood and lymphatic system disorders
Not known: Leukopenia, neutropenia, hemolytic anemia (see section Special warnings and precautions for use).
Please inform your doctor of all undesirable effects upon drug administration.
There is no known toxic dose for spiramycin.
The signs expected at high doses are gastrointestinal disorders: nausea, vomiting, and diarrhea.
Cases of QT interval prolongation regressing upon discontinuation of treatment have been observed in neonates treated with high doses of spiramycin and after intravenous administration of spiramycin in subjects at risk of prolongation of the interval. In the event of an overdose of spiramycin, an ECG is therefore recommended to measure the QT interval, particularly other associated risk factors (hypokalemia, congenital QT interval prolongation, combined use of drugs prolonging the QT interval and/or giving torsades de pointes).
There is no specific antidote.
Symptomatic treatment is recommended.
Store in dry places, not exceeding 30oC, protect from light.
Therapeutic indications arise from the antibacterial activity and the pharmacokinetic characteristics of spiramycin. Therapeutic indications take into account both clinical studies to which the medicine has been developed and its position in the range of antibacterial products currently available.
Spiramycin is indicated for the treatment of infections caused by susceptible bacteria:
- Pharyngitis caused by group A beta-hemolytic streptococci, as an alternative to beta-lactam therapy, particularly when treatment with beta-lactam is impossible.
- Acute sinusitis. Given the microbiological profile of these infections, macrolides are indicated if treatment with beta-lactam is impossible.
- Superinfections of acute bronchitis.
- Exacerbations of chronic bronchitis.
- Community-acquired pneumonia in subjects:
+ without risk factors,
+ without signs of clinical seriousness,
+ in the absence of clinical elements suggestive of pneumococcal etiology.
If atypical pneumonia is suspected, macrolides are indicated regardless of severity and host factor.
- Benign skin infections: impetigo, ecthyma, infectious dermohypodermitis (particularly erysipelas), erythrasma.
- Stomatological infections.
- Non-gonococcal genital infections.
- Prophylactic treatment of relapse of acute rheumatism in cases of allergy to beta-lactam.
- Toxoplasmosis in pregnant women.
- Prophylaxis of meningococcal meningitis in case of contraindication to rifampicin:
+ The goal is to eradicate Neisseria meningitidis from the nasopharynx,
+ Spiramycin is not used for the treatment of meningococcal meningitis,
+ Spiramycin is recommended for the prophylaxis in:
++ patients after curative treatment and before reintegration into the community,
++ individuals who have been exposed to oropharyngeal secretions in ten days preceding hospitalization.
Official guidelines regarding the appropriate use of antibiotics should be followed.
This medicine should never be used if you are hypersensitive to spiramycin or any of the excipients listed in the product.
METHOD OF ADMINISTRATION
Oral administration. Dissolve the contents of each sachet in boiled and cooled water and/or filtered water (approximately 5 - 10 ml). Stir well before drinking.
POSOLOGY
Adults: 6,000,000 to 9,000,000 IU (8 to 12 sachets) every 24 hours in 2 divided doses.
In severe infections, the daily dosage may be increased from 12,000,000 to 15,000,000 IU (16 to 20 sachets per day).
Gonorrhea: 12,000,000 to 13,500,000 IU (16 or 18 sachets) in a single dose.
Children: The usual daily dosage is based on 150,000 IU/kg body weight in 2 or 3 divided doses; the following calculated dosages are given as a guide.
Spiramycin is stable in gastric juices and absorption is not affected by food. In severe infections, the daily dosage may be increased by one-half.
In the treatment of beta-hemolytic streptococcal infections, spiramycin should be administered for 10 days.
Or as directed by the physician.
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