Usage
- Tiropramide hydrochloride is prescribed for the relief of abdominal pain and discomfort associated with functional gastrointestinal disorders, such as irritable bowel syndrome (IBS). It is also used to treat biliary and renal colic and spastic conditions of the urogenital tract.
- Pharmacological Classification: Antispasmodic agent.
- Mechanism of Action: Tiropramide increases intracellular cAMP levels in smooth muscle cells and promotes calcium ion binding to the sarcoplasmic reticulum, leading to muscle relaxation.
Alternate Names
- Tiropramide hydrochloride
- CR 605
- Alfospas
- Maiorad
- Piromide
- Propa
- Spastro
- Tipron
- Tiram
- Tiramide
- FLOSPAN
How It Works
- Pharmacodynamics: Tiropramide relaxes the smooth muscles of the gastrointestinal, biliary, renal, and urogenital tracts, reducing spasms and pain. It achieves this without significantly affecting the autonomic nervous system.
- Pharmacokinetics:
- Absorption: Readily absorbed after oral administration.
- Metabolism: Information not found in provided sources.
- Elimination: Information not found in provided sources.
- Mode of Action: Increases intracellular cAMP and promotes calcium binding to the sarcoplasmic reticulum, leading to smooth muscle relaxation.
- Receptor Binding/Enzyme Inhibition/Neurotransmitter Modulation: Primarily affects intracellular cAMP levels and calcium ion handling within smooth muscle cells.
- Elimination Pathways: Information not found in provided sources.
Dosage
Standard Dosage
Adults:
- 100 mg two to three times a day. Some patients may require 200 mg twice daily.
Children:
- Safety and effectiveness have not been established in children under 12 years old. Dosing adjustments based on age and symptoms might be necessary for adolescents. Some sources indicate usage in children older than 6 with dosage based on weight (8 mg/kg/day).
Special Cases:
- Elderly Patients: Start with a lower dose and titrate upwards based on individual tolerance and organ function.
- Patients with Renal Impairment: Careful dose adjustment is necessary. Monitor renal function regularly.
- Patients with Hepatic Dysfunction: Use with caution and adjust the dose. Close monitoring of liver function is recommended.
- Patients with Comorbid Conditions: Individualized dosing adjustments may be necessary for patients with conditions like glaucoma, prostatic hypertrophy, or those receiving antihypertensive medications.
Clinical Use Cases
While tiropramide might be used as an adjunct medication to manage spasms and pain in clinical settings like intubation, surgical procedures, mechanical ventilation, ICU, and emergencies, specific dosage recommendations are not explicitly defined in the provided sources. Dosage should be adjusted based on the individual patient’s needs and clinical condition.
Dosage Adjustments
Individualized dosing adjustments are recommended based on factors like renal/hepatic dysfunction, other comorbid conditions, and patient response to therapy.
Side Effects
Common Side Effects:
- Nausea
- Vomiting
- Dry mouth
- Constipation
- Allergic reactions (rash, itching, swelling)
- Gastrointestinal discomfort (upset stomach)
Rare but Serious Side Effects:
- Severe dizziness
- Difficulty breathing (in the case of allergic reactions)
- Pronounced hypotension
- Excessive muscle relaxation
Long-Term Effects:
Not explicitly stated in the provided sources.
Adverse Drug Reactions (ADR):
Allergic reactions requiring immediate medical attention.
Contraindications
- Hypersensitivity to tiropramide or any of its components.
- Gastrointestinal stenosis.
- Megacolon.
- Circulatory failure.
- Severe hepatic impairment.
Drug Interactions
- Other antispasmodic or anticholinergic agents may amplify muscle-relaxant effects, potentially leading to hypotension or excessive muscle relaxation.
- Drugs that inhibit or induce cytochrome P450 enzymes (e.g., ketoconazole, erythromycin, rifampicin) can affect the metabolism of tiropramide.
- Alcohol should be avoided as interactions are unknown.
Pregnancy and Breastfeeding
- Tiropramide should be avoided during pregnancy and breastfeeding unless absolutely necessary, as there is limited data on its safety in these populations. The prescribing physician should weigh the potential benefits against the risks.
Drug Profile Summary
- Mechanism of Action: Increases intracellular cAMP and promotes calcium binding to the sarcoplasmic reticulum, inducing smooth muscle relaxation.
- Side Effects: Nausea, vomiting, dry mouth, constipation, allergic reactions.
- Contraindications: Hypersensitivity, gastrointestinal stenosis, megacolon, circulatory failure, severe hepatic impairment.
- Drug Interactions: Other antispasmodics, anticholinergics, CYP450 enzyme inhibitors/inducers.
- Pregnancy & Breastfeeding: Avoid unless absolutely necessary.
- Dosage: Adults: 100 mg bid/tid or 200 mg bid. Children: Not well established; cautious use advised with age-based adjustments.
- Monitoring Parameters: Renal and hepatic function, blood pressure.
Popular Combinations:
Information not available in the provided sources.
Precautions
- General Precautions: Screen for allergies, metabolic disorders, and organ dysfunction before use.
- Specific Populations: Avoid in pregnancy and breastfeeding unless absolutely necessary. Caution advised in elderly and children.
- Lifestyle Considerations: Avoid alcohol.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Tiropramide?
A: Adults: 100 mg two to three times a day, or 200 mg twice a day. For children, safety and efficacy are not well-established. Some sources suggest 8 mg/kg/day in children older than six, divided into two doses. Consult specialized literature and guidelines before considering tiropramide in pediatric populations.
Q2: What are the main uses of tiropramide?
A: Tiropramide is primarily used to alleviate abdominal pain and cramps associated with functional gastrointestinal disorders, especially IBS. It is also used for spastic conditions of the biliary and urogenital tracts.
Q3: How does tiropramide work?
A: It increases intracellular cAMP and enhances calcium binding to the sarcoplasmic reticulum in smooth muscle cells, resulting in muscle relaxation and spasm reduction.
Q4: What are the common side effects of Tiropramide?
A: Common side effects include nausea, vomiting, dry mouth, constipation, and allergic reactions.
Q5: Are there any contraindications for tiropramide?
A: Yes. Contraindications include hypersensitivity to tiropramide, gastrointestinal stenosis, megacolon, and circulatory failure. Severe hepatic impairment also necessitates caution.
Q6: Can tiropramide be used during pregnancy or breastfeeding?
A: It should be avoided unless absolutely necessary due to limited safety data. The potential benefits should be weighed against the risks by the prescribing physician.
Q7: Does tiropramide interact with other medications?
A: Yes. It may interact with other antispasmodics or anticholinergic drugs, potentially exacerbating muscle relaxation and hypotension. Drugs impacting CYP450 enzymes (inhibitors or inducers) can also affect tiropramide metabolism. Concurrent use with these medications should be carefully managed.
Q8: What precautions should be taken when prescribing Tiropramide?
A: Pre-screening for allergies, metabolic disorders, organ dysfunction, especially liver and kidney conditions, is essential. It’s crucial to tailor dosage carefully for the elderly, children, and patients with renal or hepatic impairment. Alcohol should be avoided due to unknown interactions.
Q9: How should Tiropramide be administered?
A: Tiropramide is typically administered orally in tablet form. It can be taken with or without food. Intravenous or intramuscular administration and rectal suppositories are other possible routes, though less common. It’s crucial to follow the prescribed dosage and administration instructions carefully.
