| Composition: |
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| Chemistry: |
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C5H9NO4S
S-(Carboxymethyl)- L- cysteine
or 3-[(carboxymethyl)-thio]-alanine
HOOC - CH2 - S - CH2
- CH - COOH
|
NH2
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| Description: |
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| Carbocisteine was first
produced in 1930. Formerly was considered
as mucolytic agent in the adjunctive
therapy of respiratory tract disorders
characterized by excessive, viscous
mucus. |
| Recent
researches describe carbocisteine
as: |
|
 |
Muco-Regulator. |
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Muco-Modulator. |
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Muco-Modifying |
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| Mechanism of Action: |
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It differs in action from other
mucolytics, as it has muco-regulatory
rather than mucolytic effect. |
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Carbocisteine has protected thiol
group which is blocked by carboxylic
acid residue. |
|
Carbocisteine is able to activate
Sialyltransferase enzymes present
in the glandular cells of bronchial
mucosa promoting the synthesis of
Sialomucins. |
|
Carbocisteine increases “Sialo-mucins“
content of viscous mucus which is
less viscous, and reduces “Fuco-mucins“
which influence the viscous mucus. |
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This restores the balance between
Sialo-mucins and Fuco-mucins, as well
as maintains the normal rheological
properties of the mucus. |
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In addition, Carbocisteine has an
anti-inflammatory function, through
it’s inhibitory effect on kinin
(inflammatory mediator). |
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Suppression of inflammatory mechanism
will lead to a decrease in vascularity,
cell destruction, edema, and bronchospasm;
and will encourage the rapid return
of a healthy mucosa. |
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| Pharmacokinetics: |
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Carbocisteine is promptly absorbed
after oral administration. |
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Peak concentration is reached at
1.09 hours for syrup preparations
and 1.70 hours for capsules. |
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| Metabolism: |
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Only 0.3 % appears in feces after
single oral dose. |
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All of the rest is excreted in urine
mainly unchanged. |
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| Properties: |
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Carbocisteine molecule, the active
substance of Mucosol, has a protected
thiol group. |
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Unlike traditional mucolytics, Mucosol
does not break disulfide bonds. |
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Mucosol restores the balance of
the more fluent sialo-mucin components
of mucus, to overcome the thick and
usually pathogenic fuco-mucins. |
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Mucosol restores the normal visco-elastic
properties of bronchial mucus secretion. |
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Mucosol restores the normal ciliary
function. |
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Mucosol helps to normalise and smoothen
expectoration. |
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Mucosol improves respiratory function,
compared with other mucolytics. |
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Mucosol is clinically approved to
lack of effect on the mucosal lining
of the gastro-intestinal tract. |
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Mucosol exerts synergistic effects
when combined with antibiotics. |
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Mucosol permits easier penetration
of antibiotics into pathological bronchial
secretions, allowing rapid therapeutic
effects. |
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| Carbocisteine versus
Ambroxol HCl: |
|
| A
single, blind comparative study lead
to the following results: |
| |
Carbocisteine |
Ambroxol |
| Improvement
of sound score |
Increased |
Increased |
| Improvement
in cough score |
Increased |
No Change |
| Viscosity &
elasticity of expectorate |
Decreased |
Decreased |
| pa CO2 |
Decreased |
No Change |
| pa
O2 |
Increased |
Increased |
| Hb O2 saturation |
Increased |
No Change |
| Tidal volume |
Increased |
No Change |
| Peak expiratory
value Forced |
Increased |
No Change |
| Expiratory
volume |
Increased |
Increased |
Reference:
J Int Med Res 1995 Jul-Aug 23:4 284-93
Regional Center for Cystic Fibrosis, Childrens
Hospital G Salesi, Anocona, ITALY. |
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