Mucosolvan PL Prolong action

What is Mucosolvan PL Prolong action ?

Mucosolvan PL Prolong action is used in conditions where there are a lot of thick secretion or mucus in your air passages. Mucosolvan contains ambroxol hydrochloride, which helps to clear the chest by thinning the mucus in your air passage.

Composition

1 retard capsule contains 75 mg
trans-4-[(2-amino-3,5-dibromo-benzyl)amino] cyclohexanol
hydrochloride( = ambroxol hydorchloride)

Excipients: Crospovidone collidon CL, carnauba wax, stearyl alcohol, magnesium stearate

Indication

Secrotolytic therapy in acute and chronic bronchopulmonary diseases associated with abnormal mucus secretion and impaired mucus transport.

Dosage

Adult : 1 retard capsule once daily.

The capsules should not be opened or chewed, but swallowed whole with ample liquid. The “carrier tablets” which are occasionally present in the stools have released the active substance during their passage through the digestive system and are therefore without significance.

General: In acute respiratory indications, medical advice should be sought if symptoms do not improve or worsen in the course of therapy.

Mucosolvan can be taken with or without food.

What should I do if I forget to take Mucosolvan PL?

In general, if you forget to take Mucosolvan PL, eat as soon as you remember. But if it’s close to the next meal, skip to the next meal without having to double the dose.

Side effects

Immune System Disorders, Skin and subcutaneous tissue disorders

Anaphylactic reactions including anaphylactic shock, angioedema, rash, urticaria, pruritus, and other hypersensitivity

Gastro-intestinal Disorders: Dyspepsia, nausea, vomiting, diarrhoea and abdominal pain.

General Adverse Reactions

Occasional, mild side effects from Mucosolvan PL include:

  • Nausea
  • Diarrhoea,
  • Dyspepsia (e.g. indigestion, bloated feeling)
  • Vomitting
  • Abdominal pain
  • Heartburn
  • A feeling of fullness in the
    stomach (a bloated feeling).

Adverse reactions that require immediate attention to your doctor or pharmacist

Difficulty breathing, rash, pruritus, urticaria, anaphylactic shock, angioedema

Overdose

No specific overdose symptoms have been reported in man to date.

Based on accidental overdose and/or medication error reports the observed symptoms are consistent with the known side effects of MUCOSOLVAN at recommended doses and may need symptomatic treatment.

Pharmacological properties

Preclinically, ambroxol hydrochloride, the active ingredient of MUCOSOLVAN, has been shown to increase respiratory tract secretion. It enhances pulmonary surfactant production and stimulates ciliary activity. These actions result in improved mucus flow and transport (mucociliary clearance). Improvement of mucociliary clearance has been shown in clinical pharmacologic studies. Enhancement of fluid secretion and mucociliary clearance facilitates expectoration and eases cough.

A local anaesthetic effect of ambroxol hydrochloride has been observed in the rabbit eye model which may be explained by the sodium channel blocking properties. It was shown in vitro that ambroxol hydrochloride blocks cloned neuronal sodium channels; binding was reversible and concentration-dependent.

Cytokine release from blood but also tissue-bound mononuclear and polymorphonuclear cells was found to be significantly reduced by ambroxol hydrochloride in vitro.

Following the administration of ambroxol antibiotic concentrations (amoxicilline, cefuroxime, erythromycin) in bronchopulmonary secretions and in the sputum are increased.

Antiviral property in vitro and in animal models

In vitro studies in human tracheal epithelial cells a reduction of rhinovirus (RV 14) replication has been observed. In a mouse airway model, a reduction of influenza A virus replication was observed with ambroxol pretreatment. To date, this has not been shown to have any clinical relevance.

Pharmacokinetics

Absorption: Absorption of all immediate release oral forms of ambroxol hydrochloride is rapid and complete, with dose linearity in the therapeutic range. Maximum plasma levels are reached within 1 to 2.5 hours following oral administration of the immediate –release formulation and after a median of 6.5 hours of the slow release formulation.

The absolute bioavailablility after a 30 mg tablet was found to be 79%.

The slow release capsule showed a relative availability of 95% (dose-normalized) in comparison to a daily dose of 60 mg (30 mg twice daily) administered as immediate-release tablet.

Distribution: Distribution of ambroxol hydrochloride from blood to tissue is rapid and pronounced, with the highest concentration of the active substance found in the lungs. The volume of distribution following oral administration was estimated to be 552L. In the therapeutic range plasma protein binding was found to be approximately 90%. 83

Metabolism and elimination: About 30% of an orally administered dose is eliminated via first pass metabolism.

Ambroxol hydrochloride is primatily metabolized in the liver by glucuronidation and some cleavage to dibromanthranilic acid (Approximately 10% of dose) aside form some minor metabolites. Studies in human liver microsomes have shown that CYP3A4 is responsible for the metabolism of ambroxol hydrochloride to dibromanthranilic acid.

Within 3 days of oral administration, approximately 6% of the dose is found in free form, while approximately 26% of the dose is recovered in a conjugated form in urine.

Ambroxol hydrochloride is eliminated with a terminal elimination half-life of approximately 10 hours. Total clearance is in the range of 660 ml/min, with renal clearance accounting for approximately 83% of the total clearance. It has been estimated that the amount of dose excreted in urine after 5 days represents about 83% of total dose (radioactivity)

Pharmacokinetics in special populations: In patients with hepatic dysfunction elimination of ambroxol hydrochloride is reduced, resulting in approximately 1.3 to 2-fold higher plasma levels.

Due to the high therapeutic range of ambroxol hydrochloride, dose adjustments are not necessary.

Others: Age and gender were not found to affect the pharmacokinetics of ambroxol hydrochloride to a clinically relevant extent and thus there is no necessity for adjustment of dosage regimens.

Food was not found to influence the bioavailability of ambroxol hydrochloride.

Drug interactions

No clinically relevant unfavourable interaction with other medications have been reported.

Toxicology

Ambroxol hydrochloride has a low index for acute toxicity. In repeated-dose studies, oral doses of 150 mg/kg/day (mouse, 4 weeks), 50 mg/kg/day (rat, 52 and 78 weeks), 40 mg/kg/day (rabbit, 26 weeks) and 10 mg/kg/day (dog, 52 weeks) were the no observed adverse effect levels (NOAELs). No toxicological target organds were detected.

Four-week intravenous toxicity studies with ambroxol hydrochloride in rats (4, 16 and 64 mg/kg/day) and in dog (45, 90 and 120 mg/kg/day) (infusion 3 h/day) showed no severe local and systemic toxicity including histopathology. All adverse effects were reversible.

Ambroxol hydrochloride was neither embyotoxic nor teratogenic when tested at oral doses up to 3000 mg/kg/day in rats and up to 200 mg/kg/day in rabbits. The fertility of male and female rats was not affected up to 500 mg/kg/day. The NOAEL in the peri- and post-natal development study was 50 mg/kg/day. At 500 mg/kg/day, ambroxol hydrochloride was slightly toxic for dams and pups, as shown by a retared body weight development and reduced litter size.

Genotoxicity studies in vitro (Ames and chromosome aberration test) and in vivo (mouse micronucleus test) did not reveal any mutagenic potential of ambroxol hydrochloride

Ambroxol hydrochloride did not shown any tumorigenic potential in carcinogenicity studies in mice (50, 200 and 800 mg/kg/day) and rats (65, 250 and 1000 mg/kg/day) when treated with a dietary admixture for 105 and 116 weeks, respectively

Contraindication

MUCOSOLVAN should not be used in patients known to be hypersensitive to ambroxol hydrochloride or other components of the formulation.

In case of rare hereditary conditions that may be incompatible with an excipient of the product (please refer to Special warnings and precautions) the use of the product is contraindicated.

Special warning and precautions

There have been very few reports of severe skin lesions such as Stevens-Johnson syndrome and toxic epidermal necrolysis (TEN) in temporal association with the administration of expectorants such as ambroxol hydrochloride. Mostly these could be explained by the severity of the patient’s underlying disease and/or concomitant medication.

In addition during the early phase of a Stevens Johnson Syndrome or TEN a patient may first experience non-specific influenza-like syndromes like e.g. fever, aching body, rhinitis, cough and sore throat. Mislead by these non-specific influenza-like prodromes it is possible that a symptomatic treatment is started with a cough and cold medication.

Therefore if new skin or mucosal lesions occur, medical advice should be sought immediately and treatment with ambroxol hydrochloride discontinued as a precaution.

In the presence of impaired renal function MUCOSOLVAN® may be used only after consulting a physician.

Use In Pregnancy

Ambroxol hydrochloride crosses the placental barrier. Nonclinical studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/foetal development, parturition or postnatal development. Extensive clinical experience after the 28th week of pregnancy has shown no evidence of harmful effects on the foetus.

Nonetheless, the usual precautions regarding the use of drugs during pregnancy should be observed. Especially during the first trimester, the use of MUCOSOLVAN® is not recommended.

Use in Lactation

Ambroxol hydrochloride is excreted in breast milk. Althought unfavourable effects on breastfed infants would not be expected, MUCOSOLVAN® is not recommended for use in nursing mothers.

Fertility

Nonclinical studies do not indicate direct or indirect harmful effects with respect to fertility.

Effects on ability to drive and use machines.

There is no evidence from postmarketing data for an effect on the ability to drive and use machines.

Studies on the effects on the ability to drive and use machines have not been performed.

Storage

Do not store above 30 C.

Where to buy Mucosolvan PL?

Due to Mucosolvan PL is a non dangerous drug by legislation class. Therefore, it can be sold in modern drugstores or ready-packed pharmacies.

Other information

Thai drug registration number: 1C 29/60 Read more about the meaning of Thai registration number.

Pharmaceutical Dose Form: Retard capsule 75 mg

Packaging: Blister packs, 10 capsules per strip

Category by point of use: Internal Use

Category by legislation class: Non Dangerous Drug

Manufactued by: Boehringer Ingelheim Pharma GmBH & Co. KG, BIBERACH AN DER RISS, Germany

Repacker: Delpharm Reims, Reims, France

Importer: Sanofi-aventis (Thailand) Ltd, Bangkok Tel 02-264-9999

Reference

  • Labels and documentation of MUCOSOLVAN® PL (Revision Date May 2018)
  • Product information authorised verification system, Food and Drug Administration, Ministry of Health, Thailand
  • yaandyou.net
  • MIMS

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