Drug information of Hyoscine

Hyoscine

Drug group:

Hyoscine butylbromide is an antispasmodic medicine which is taken to relieve cramps in the stomach, intestines or bladder. In particular, it helps to ease bloating and the spasm-type pain that can be associated with irritable bowel syndrome and diverticular disease. It works by relaxing some of the muscles in your gastrointestinal and urinary systems.

Mechanism of effect

 Competitively inhibits acetylcholine or other cholinergic stimuli at autonomic effectors innervated by postganglionic cholinergic nerves and, to a lesser extent, on smooth muscles that lack cholinergic innervation.

Pharmacodynamic

 Buscopan 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.

Pharmacokinetics

As a quaternary ammonium compound, hyoscine butylbromide is highly polar and hence only partially absorbed following oral (8%) or rectal (3%) administration. Because of its high affinity for muscarinic receptors and nicotinic receptors, hyoscine butylbromide 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 butylbromide is approximately 4.4%. The main metabolic pathway is the hydrolytic cleavage of the ester bond. Orally administered hyoscine butylbromide is excreted in the faeces and in the urine.

Dosage

Adults:

2tablets 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.

One ampoule (20 mg) intramuscularly or intravenously, repeated after half an hour if necessary. Intravenous injection should be performed 'slowly' (in rare cases a marked drop in blood pressure and even shock may be produced by Buscopan). When used in endoscopy this dose may need to be repeated more frequently.

Maximum daily dose of 100mg.

Children 6 - 12 years:

1 tablet three times daily.

No specific information on the use of this product in the elderly is available. Clinical trials have included patients over 65 years and no adverse reactions specific to this age group have been reported.

Alerts

CNS Effects: Possible adverse CNS effects, including CNS depression, manifested as drowsiness, euphoria, amnesia, fatigue, and dreamless sleep; disorientation; confusion; memory disturbances; and dizziness. Excitement, restlessness, hallucinations, or delirium may paradoxically occur, especially when scopolamine is used in the presence of severe Effect. May result in impairment of performance of activities requiring mental alertness, physical coordination, or visual acuity (e.g., operating machinery, driving a motor vehicle). Use caution with underwater sports participation; warn patients about possible disorientation. Use with caution in patients with autonomic neuropathy. 

Ocular Effects: Possible increased intraocular pressure; monitor open-angle glaucoma therapy and adjust as necessary. 

Idiosyncratic Reaction: Excessive susceptibility to the effects of scopolamine occurs rarely. Toxic symptoms may occur with therapeutic doses. Most serious idiosyncratic reaction is acute toxic psychosis (e.g., confusion, agitation, rambling speech, hallucinations, paranoid behavior, delusions). Other manifestations may include marked CNS disturbances (e.g., complete disorientation, active delirium), somnolence, dilated pupils, accelerated pulse rate, and dryness of the mouth with a husky quality of the voice. Idiosyncratic reaction usually is reversed by physostigmine. 

Withdrawal of Therapy: Possible drug withdrawal symptoms (e.g., nausea, vomiting, headache, dizziness, disturbances of equilibrium) following discontinuance of the transdermal system; usually do not appear until ≥24 hours after system removal. 

Cardiovascular Effects: Possible tachycardia; use with caution in patients with tachyarrhythmias, CHF, CAD, or hyperthyroidism. 

GI Effects : Possible decreased GI motility. Use with caution if pyloric or intestinal obstruction is suspected.

Down Syndrome, Spastic Paralysis, and Brain Damage

Possible increased sensitivity to antimuscarinic effects (e.g., mydriasis, positive chronotropic effect).

Respiratory Effects: Systemically administered antimuscarinics may reduce bronchial secretions and may lead to inspissation and formation of bronchial plugs in debilitated patients with chronic pulmonary disease; use with caution in such patients.

Seizure or Psychosis: Scopolamine may aggravate seizures or psychosis; use with caution in patients with a history of these conditions.

Points of recommendation

Don’t use this medicine if you are :

allergic to scopolamine or similar medications such as methscopolamine or hyoscyamine, or if you have:

  • narrow-angle glaucoma;
  • a blockage in your intestines;
  • a severe breathing disorder; or
  • if you are unable to urinate.

To make sure scopolamine is safe for you, tell your doctor if you have:

  • glaucoma;
  • an enlarged prostate, bladder obstruction, or urination problems;
  • problems with your esophagus, stomach, or intestines;
  • kidney disease;
  • liver disease;
  • heart disease, high blood pressure;
  • coronary artery disease (hardened arteries);
  • overactive thyroid;
  • myasthenia gravis;
  • asthma or other breathing problems;
  • a drug allergy; or
  • a history of head injury or brain tumor.

It is not known whether this medicine will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant.

It is not known whether scopolamine passes into breast milk or if it could harm a nursing baby. Tell your doctor if you are breast-feeding a baby.

Scopolamine is not approved for use by anyone younger than 6 months.

Take this medicine with a full glass of water. You may take scopolamine with or without food.

If you take scopolamine to treat a Parkinson-like condition, you should not stop using this medicine suddenly. Stopping suddenly may make your condition worse.

Since scopolamine is sometimes used only when needed, you may not be on a dosing schedule. If you are on a schedule, use the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not use extra medicine to make up the missed dose.

Pregnancy level

C


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