PRODUCTS

Anti- spasmodic
Buscopol
Anti-Spasmodic
Buscopol

CLINICAL PHARMACOLOGY

PHARMACODYNAMICS

  • Pharmacodynamics properties Hyoscine Butyl Bromide exerts a Spasmolytic Action on the Smooth Muscle of the Gastrointestinal, Biliary and Genito-urinary Tracts. As a quaternary Ammonium derivative, Hyoscine Butyl Bromide does not enter the Central Nervous System. Therefore, Anticholinergic side effects at the Central Nervous System do not occur. Peripheral Anticholinergic Action results from a Ganglion-Blocking Action within the visceral wall as well as from an Anti-Muscarinic activity.

  • Mechanism of action: Hyoscine Butyl Bromide is a quaternary ammonium compound which, as an anticholinergic agent, has a ganglion blocking component. Due to its anticholinergic action, Hyoscine Butyl Bromide reduces the tone and peristalsis of smooth muscle in hollow organs with parasympathetic innervation. As a quaternary ammonium compound with low lipid solubility, it cannot pass the blood/brain barrier easily and only rarely causes the central nervous system side effects associated with atropine and hyoscine. Hyoscine Butyl Bromide is a Spasmolytic. The Anticholinergic Spasmolytic effect is based both on competitive inhibition of the Parasympathetic activation of Smooth Muscle mediated through Muscarinic receptors and, more markedly, through Ganglionic Blockade of Neural Transmission. Hyoscine Butyl Bromide is a powerful smooth Muscle Relaxant, effective when given by mouth or by injection. In the recommended dosages, Hyoscine Butyl Bromide relieves smooth Muscle spasm rapidly. Undesirable 'Atropine-like' side effects such as Blurred Vision, Palpitation or dry mouth are rare.

PHARMACOKINETIC PROPERTIES

  • Absorption: As a quaternary Ammonium compound, Hyoscine Butyl Bromide is highly polar and hence only partially absorbed following oral (8%) or Rectal (3%) administration. After Oral administration of single doses of Hyoscine Butyl Bromide in the range of 20 to 400 mg, mean peak plasma concentrations between 0.11 ng/mL and 2.04 ng/mL were found at approximately 2 hours. In the same dose range, the observed mean AUC0-tz-values varied from 0.37 to 10.7 ng h/mL. The median absolute Bioavailabilities of different dosage forms, i.e. coated tablets, suppositories and oral solution, containing 100 mg of Hyoscine Butyl Bromide each were found to be less than 1%.

  • Distribution: Because of its high affinity for Muscarinic Receptors and Nicotinic Receptors, Hyoscine Butyl bromide is mainly distributed on muscle cells of the abdominal and pelvic area as well as in the Intramural Ganglia of the abdominal organs. Plasma protein binding (Albumin) of Hyoscine Butyl Bromide is approximately 4.4%. Animal studies demonstrate that Hyoscine Butyl Bromide does not pass the Blood-Brain Barrier, but no clinical data to this effect is available. Hyoscine Butyl Bromide has been observed to interact with the Choline Transport in Epithelial Cells of human Placenta in vitro.

  • Metabolism and Elimination: Following oral administration of single doses in the range of 100 to 400 mg, the terminal Elimination Half-lives ranged from 6.2 to 10.6 hours. The main metabolic pathway is the Hydrolytic cleavage of the Ester bond. Orally administered Hyoscine Butyl Bromide is excreted in the faeces and in the urine. Studies in man show that 2 to 5% of radioactive doses is Eliminated Renally after oral, and 0.7 to 1.6% after rectal administration. Approximately 90% of recovered radioactivity can be found in the faeces after oral administration. The Urinary Excretion of Hyoscine Butyl Bromide is less than 0.1% of the dose. The mean apparent oral clearances after oral doses of 100 to 400 mg range from 881 to 1420 L/min, whereas the corresponding volumes of distribution for the same range vary from 6.13 to 11.3 x 105 L, probably due to very low systemic availability. The metabolites excreted via the Renal Route bind poorly to the Muscarinic Receptors and are therefore not considered to contribute to the effect of the Hyoscine Butyl Bromide.

INTERACTION

  • The Anticholinergic effect of drugs such as Tri- and Tetracyclic Antidepressants, Antihistamines, Quinidine, Amantadine, Antipsychotics (e.g. Butyrophenones, Phenothiazine), Disopyramide and other Anticholinergic (e.g. Tiotropium, Ipratropium, Atropine-like compounds) may be intensified by Hyoscine Butyl Bromide.
  • Concomitant treatment with Dopamine Antagonists such as Metoclopramide may result in diminution of the effects of both drugs on the Gastrointestinal Tract.
  • The Tachycardic effects of Beta-Adrenergic agents may be enhanced by Hyoscine Butyl Bromide.

INDICATIONS

  • Buscopol 10 mg, 20 mg Tablets are indicated for the relief of spasm of the Genito-Urinary Tract or Gastro- Intestinal Tract and for the symptomatic relief of Irritable Bowel Syndrome.

DOSAGE AND METHOD OF ADMINISTRATION

  • Buscopol 10 mg, 20 mg Tablets are for oral administration only.
  • 10 mg, 20 mg Tablets should be swallowed whole with adequate water.
  • Adults: 2 tablets four times daily. For the symptomatic relief of Irritable Bowel Syndrome, the recommended starting dose is 1 tablet three times daily, this can be increased up to 2 tablets four times daily if necessary.
  • Children 6 - 12 years: 1 tablet three times daily.
  • No specific information on the use of this product in the elderly is available.
  • Buscopol 10 mg, 20mg Tablets should not be taken on a continuous daily basis or for extended periods without investigating the cause of abdominal pain.

SIDE EFFECTS

  • Dry mouth
  • Fast heart rate
  • Reduced sweating
  • Rash
  • Itching
  • Redness of the skin
  • A skin condition called Dyshidrosis (small Blisters on the hands and feet)
  • Difficulty passing urine.
  • There have also been very rare isolated reports of Coma, Hallucinations (Seeing, Feeling or Hearing things that are not there), Dystonia (unusual Muscle Tone causing Distortion of the body), Confusion, Agitation and Dizziness.
  • These side effects were relieved when the patients stopped medicine. Therapy and received appropriate medical treatment.
  • If any of the following happen, tell your doctor immediately or go to Emergency at your nearest hospital:
    • Allergic Reactions (such as Skin Rashes, or Swelling of the face and difficulty in Breathing).
    • Sudden life-threatening Allergic Reactions (Anaphylaxis with episodes of shortness of Breath and Shock)

WARNING AND PRECAUTIONS

  • Symptoms like Fever, Nausea, Vomiting, and changes in Bowel Movements, Abdominal Tenderness, Decreased Blood Pressure, Fainting, or Blood in Stool, medical advice should immediately be sought.
  • Hyoscine Butyl Bromide 10 mg, 20 mg Tablets should be used with caution in conditions characterized by Tachycardia such as Thyrotoxicosis, Cardiac Insufficiency or Failure and in Cardiac surgery where it may further accelerate the Heart Rate. Due to the risk of Anticholinergic complications, caution should be used in patients susceptible to Intestinal or Urinary outlet obstructions.
  • Because of the possibility that Anticholinergic may reduce Sweating, Hyoscine Butyl Bromide should be administered with caution to patients with Pyrexia. Elevation of Intraocular Pressure may be produced by the administration of Anticholinergic agents such as Hyoscine Butyl Bromide in patients with undiagnosed and therefore untreated Narrow Angle Glaucoma. Therefore, patients should seek urgent Ophthalmological advice in case they should develop a painful, Red Eye with Loss of Vision whilst or after taking Hyoscine Butyl Bromide.

CONTRAINDICATIONS

  • Patients who have demonstrated prior Hypersensitivity to Hyoscine Butyl Bromide or any other component of the product.
  • Myasthenia Gravis.
  • Mechanical Stenosis in the Gastrointestinal Tract.
  • Paralytical or Obstructive Ileus.
  • Megacolon.
  • Narrow Angle Glaucom