Usage
Hyoscine butylbromide + Paracetamol is prescribed for the relief of pain associated with abdominal cramps or spasms, including menstrual cramps and urinary tract spasms. It is also effective for other types of smooth muscle spasms in the gastrointestinal and genitourinary tracts. This medication combines an antispasmodic and an analgesic agent.
Pharmacological Classification:
- Hyoscine butylbromide: Antispasmodic, Anticholinergic
- Paracetamol: Analgesic, Antipyretic
Mechanism of Action:
Hyoscine butylbromide acts as an antispasmodic by competitively antagonizing the muscarinic M3 receptors located on the smooth muscle cells of the gastrointestinal and genitourinary tracts. This inhibits the binding of acetylcholine, thus reducing smooth muscle contractions and relieving spasms. Paracetamol provides pain relief through its analgesic properties, primarily by inhibiting cyclooxygenase (COX) enzymes in the central nervous system, which reduces prostaglandin synthesis and subsequently reduces pain signals. The combination of these two agents offers dual-action relief – reduction of spasms and pain relief.
Alternate Names
Hyoscine butylbromide is sometimes referred to as Butylscopolamine or Scopolamine butylbromide.
Brand Names: Buscopan Plus, Buscopan Venus, Spasmodex-P
How It Works
Pharmacodynamics:
Hyoscine butylbromide targets the muscarinic M3 receptors in the smooth muscle of the gastrointestinal, biliary, and urinary tracts. Its anticholinergic action reduces smooth muscle tone and peristaltic activity, relieving spasms and cramps. Paracetamol’s primary mechanism is thought to be central inhibition of COX enzymes, which are involved in the production of prostaglandins. Prostaglandins mediate pain and inflammation, so reducing their synthesis leads to pain relief. Paracetamol also has antipyretic effects, but its mechanism for this is not fully understood.
Pharmacokinetics:
- Absorption: Hyoscine butylbromide is poorly absorbed after oral administration, with bioavailability around 8%. Paracetamol is rapidly absorbed from the gastrointestinal tract, reaching peak plasma concentrations within 30-60 minutes.
- Metabolism: Hyoscine butylbromide undergoes some metabolism in the liver. Paracetamol is primarily metabolized in the liver through glucuronidation and sulfation pathways. A small amount is metabolized by cytochrome P450 enzymes to a reactive metabolite, N-acetyl-p-benzoquinone imine (NAPQI), which is usually detoxified by glutathione.
- Elimination: Hyoscine butylbromide is primarily eliminated in the feces. Paracetamol is mainly excreted in the urine, primarily as conjugated metabolites.
Dosage
Standard Dosage
Adults:
The recommended dose is 1-2 tablets, three times daily. The maximum daily dose should not exceed 6 tablets. Tablets should be swallowed whole with sufficient water. Do not chew the tablets. It should not be taken for more than 3 days without a prescription.
Children:
This combination is not recommended for children under 10 years of age. For children 10 years and older, consult a physician for appropriate dosing recommendations.
Special Cases:
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Elderly Patients: Elderly patients should be monitored for potential anticholinergic side effects such as constipation, dry mouth, and urinary retention. Dosage adjustment may be necessary.
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Patients with Renal Impairment: Dose reduction or increased dosing intervals may be required for patients with severe renal dysfunction.
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Patients with Hepatic Dysfunction: Dose reduction or increased dosing intervals may be required for patients with severe hepatic impairment. The drug should not be taken in the event of severe hepatocellular insufficiency.
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Patients with Comorbid Conditions: Use with caution in patients with glaucoma, myasthenia gravis, tachyarrhythmias, or gastrointestinal or urinary tract obstructions.
Clinical Use Cases The primary use case of this drug combination is to provide symptomatic relief of pain from spasms in abdominal cramps and urinary tract issues. It is not typically used as part of specific protocols for intubation, surgical procedures, mechanical ventilation, or ICU use. For emergency situations, other medications are generally preferred.
Dosage Adjustments Dosage adjustment is needed in patients with liver or kidney disease, based on the severity of impairment. A lower dose or longer intervals between doses may be recommended. This medication should be discontinued if severe liver or kidney function disorders arise.
Side Effects
Common Side Effects:
Dry mouth, blurred vision, constipation, difficulty urinating, dizziness, drowsiness, skin reactions (rash, itching).
Rare but Serious Side Effects:
Allergic reactions (anaphylaxis, angioedema), rapid heart rate, acute glaucoma, paralytic ileus, hepatotoxicity (with paracetamol overdose).
Long-Term Effects:
Chronic use of paracetamol, particularly at high doses, can lead to liver damage. Long-term use of hyoscine butylbromide is not recommended without medical supervision due to the risk of developing tolerance and potential anticholinergic side effects.
Contraindications
- Hypersensitivity to hyoscine butylbromide or paracetamol.
- Myasthenia gravis.
- Mechanical gastrointestinal obstruction (e.g., pyloric stenosis, achalasia).
- Paralytic ileus or megacolon.
- Closed-angle glaucoma.
- Severe hepatic impairment (Child-Pugh C).
- Tachyarrhythmias.
- Urinary retention (e.g., due to prostatic hypertrophy).
Drug Interactions
- Anticholinergics: Concomitant use of other anticholinergic medications (e.g., tricyclic antidepressants, antihistamines) may potentiate anticholinergic effects.
- Metoclopramide and other Prokinetics: May antagonize the effects of both drugs on the gastrointestinal tract.
- Beta-adrenergic agonists: Hyoscine butylbromide may enhance the tachycardic effects.
- CYP450 inducers/inhibitors: Certain drugs, such as rifampicin and phenytoin, may affect the metabolism of both drugs.
- Alcohol: May increase the risk of paracetamol-induced hepatotoxicity.
- Anticoagulants: Chronic paracetamol use may necessitate monitoring of anticoagulant therapy.
- Zidovudine: May increase the risk of neutropenia.
Pregnancy and Breastfeeding
Hyoscine butylbromide + Paracetamol is generally not recommended during pregnancy, especially the first trimester, due to potential risks to the fetus. Paracetamol is considered relatively safe for occasional use during pregnancy at recommended doses. However, prolonged use or high doses are discouraged. Hyoscine butylbromide’s safety during pregnancy is not well established, so the combination is best avoided.
Paracetamol is excreted in breast milk. While generally considered safe for breastfeeding, prolonged use or high doses should be avoided. Hyoscine butylbromide’s excretion into breast milk is not well studied. Therefore, it’s advisable to exercise caution when using this combination during breastfeeding or consider alternate options.
Drug Profile Summary
- Mechanism of Action: Hyoscine butylbromide: Muscarinic M3 receptor antagonist (antispasmodic). Paracetamol: COX inhibitor (analgesic).
- Side Effects: Dry mouth, blurred vision, constipation, urinary retention, dizziness, drowsiness, skin rash, allergic reactions.
- Contraindications: Hypersensitivity, myasthenia gravis, GI obstruction, paralytic ileus, angle-closure glaucoma, severe hepatic impairment, tachyarrhythmias, urinary retention.
- Drug Interactions: Anticholinergics, prokinetics, beta-agonists, CYP450 inducers/inhibitors, alcohol, anticoagulants, zidovudine.
- Pregnancy & Breastfeeding: Not generally recommended.
- Dosage: Adults: 1-2 tablets three times daily (max 6 tablets/day). Children (10+ years): Consult physician.
- Monitoring Parameters: Monitor for anticholinergic side effects, especially in elderly patients. In cases of prolonged paracetamol use, monitor liver function.
Popular Combinations
This specific combination of Hyoscine butylbromide and Paracetamol is already a popular combination used clinically.
Precautions
- General Precautions: Screen for allergies, glaucoma, pre-existing cardiovascular, hepatic, renal, gastrointestinal, and genitourinary conditions.
- Specific Populations: Use with caution in elderly patients and those with renal or hepatic impairment. Avoid in children under 10 years. Not recommended during pregnancy and breastfeeding.
- Lifestyle Considerations: Avoid alcohol during treatment. May affect driving ability due to potential side effects like blurred vision and dizziness.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Hyoscine butylbromide + Paracetamol?
A: For adults and children over 10 years old: 1-2 tablets three times daily, not exceeding 6 tablets per day. Not recommended for children under 10 years.
Q2: What are the common side effects of this medication?
A: Common side effects include dry mouth, blurred vision, constipation, and difficulty urinating.
Q3: Can I take this medication if I’m pregnant or breastfeeding?
A: This medication is generally not recommended for use during pregnancy or while breastfeeding. Consult your doctor for alternative options.
Q4: Are there any drug interactions I should be aware of?
A: Yes, this medication can interact with other anticholinergic drugs, metoclopramide, beta-adrenergic agonists, and certain medications metabolized by the liver. Inform your physician about all medications and supplements you are currently taking.
Q5: How long can I take this medication?
A: You should not take this medication for more than 3 days without consulting a doctor.
Q6: What should I do if I miss a dose?
A: If you miss a dose, take it as soon as you remember. However, if it’s almost time for your next dose, skip the missed dose and continue your regular dosing schedule. Do not double the dose.
Q7: What are the symptoms of an overdose?
A: Symptoms of overdose may include worsening of abdominal pain, vomiting, loss of appetite, worsening of eye pain (in patients with glaucoma), confusion, hallucinations, and seizures. Seek immediate medical attention if you suspect an overdose.
Q8: Can this drug combination be used for other conditions besides abdominal cramps?
A: While primarily used for abdominal cramps, it can be used for other smooth muscle spasms in the gastrointestinal or genitourinary tracts. Consult with a physician to determine suitability for other conditions.
Q9: What are the contraindications for using Hyoscine butylbromide + Paracetamol?
A: Contraindications include hypersensitivity, myasthenia gravis, gastrointestinal obstruction, closed-angle glaucoma, severe hepatic impairment, tachyarrhythmias, urinary retention, among others.
Q10: How should I store this medication?
A: Store at room temperature, away from moisture and direct sunlight. Keep out of reach of children.
