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Clinical pharmacology

Spiramycin spectrum of antimicrobial activity closely
resembles that of erythromycin.

Spiramycin more than any other macrolide accumulates
in the tissues where it persists for long periods and
it is property that is thought to account for its
unpredictably good in vivo activity.

Spiramycin is active against
All streptococci (including streptococcus pneumoniae and most anaerobic strains).
Neisseria meningitidis
Branhamella catarrhalis
Bordetella pertussis
Corynebacterium diphtheriae
Listeria moncytogenicus
Clostridia
Legionella pneumophilia
Chlamydia and Mycoplasma Pneumonia.
Less sensitive
D.streptococci Ex, streptococcus faecalis
Most strains of haemophilus are resistant in vivo but tissue levels of spiramycin may be effective.
Activity, in vivo and in vitro has been demonstrated against Toxoplasma gondii.
Pharmacokinetics

Spiramycin is widely distributed and persists for long periods in many tissues.
The large volume of distribution and tissue volume are indicative of the particularly high tissue affinity of spiramycin.

Concentrations many times higher than those found in serum have been reported in lung, liver, kidney, spleen, prostate, placenta ,muscle, bone and tonsillar tissue.

High levels may persist for as long as 72 hours following a single oral dose.

Spiramycin levels have also been measured in variety of human secretions and high concentration have been found in bile, saliva and lacrimal fluid.

Intracellular concentrations in phagocytic cells are markedly elevated over prolonged periods and this is likely to account for the efficacy of spiramycin against number of intracellular organisms (Chlamyia, Toxoplasma, Legionella)

Placental transfer is poor and only 9-16 % of the maternal blood concentration appear in the amniotic fluid.

Spiramycin binds poorly to serum proteins, only15% being bound to serum albumin.

Spiramycin is extensively biotransformed in the tissues, with only 14% of the dose excreted unchanged in urine.

Pharmaceutics Forms
Oral dosage forms include:
1.5 MIU
3 MIU
Indications

Upper respiratory tract ( broncho pulmonary), cutaneous and genital infections.

Recommended treatment is 6-9 MIU/ daily for 5 days.

In gonococcal urethritis single dose may be prescribed 6 MIU / daily for 5 days.

In periodontal infections combination with Metronidazole is likely to be of greater efficacy.

In Chlamydial infections the recomended dose is 6-9 MIU/daily

Prophylaxis of meningococcal meningitis:
Spiramycin is being an effective, Well tolerated and inexpensive. It meets the necessary criteria for use as a prophylactic agent because it does not penetrate the cerebrospinal fluid.

Toxoplasmosis in pregnancy

Treatment with spiramycin decreased the frequency of certain fetal abnormalitie Spiramycin had no effect on the clinical picture
however, there is many explanation:

Despite attaining good placental levels penetration to the fetal circulation is poor,Spiramycin has only moderate activity against established infections.lastly Spiramycin does not cross the blood brain barrier and is ineffective against neurotoxoplasmosis.
Adverse reactions

Spiramycin is one of the tolerated antibiotics.
There have been no reported instances of death or irreversible organ damage.

Unlike Erythromycin , Spiramycin has no effect on gastrointestinal motility which may explain the lower incidence of gastrointestinal adverse effect associated with the administration of Spiramycin as opposed to Erythromycin.

Pregnant Women:
Spiramycin has been widely used for the treatment of toxoplasmosis during pregnancy.
No adverse effects on mother or fetus have been reported.

The elderly:
There is no evidence of dose - related toxicity it is probably unnecessary to reduce the dose in elderly patients.

Contra-Indications

Allergy to spiramycin
Meningitis

Spiramycin penetrates the cerebrospinal fluid poorly even in the presence of meningeal inflammation and therefore should not be used in treatment of meningitis.

Drug interactions
unlike Erythromycin , Spiramycin has no structural affinity with cytochrome P450 and so does not interfere with the metabolism of drugs such as Theophylline, Carbamazepine ,Ergotamine dervatives or oral contraceptives.
Potentially useful interactions
Combination with Metronidazole against anaerobic may be found.
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