Usage
This combination medication is prescribed for the relief of pain and spasms associated with smooth muscle conditions, particularly in the gastrointestinal and urogenital tracts. It is commonly used to treat conditions such as renal or biliary colic, intestinal colic, and dysmenorrhea (painful menstruation).
Pharmacological Classification: This is a combination product with each component having a different classification.
- Diclofenac: Non-Steroidal Anti-inflammatory Drug (NSAID)
- Fenpiverinium: Anticholinergic/Antimuscarinic
- Pitofenone: Spasmolytic, Calcium Channel Blocker
Mechanism of Action: Diclofenac inhibits cyclooxygenase (COX) enzymes, reducing prostaglandin synthesis and thereby decreasing inflammation and pain. Fenpiverinium blocks muscarinic receptors, inhibiting parasympathetic activity, which reduces smooth muscle contractions and spasms. Pitofenone is a direct-acting spasmolytic that relaxes smooth muscles, possibly by acting as a calcium channel blocker. The combined action provides pain relief and smooth muscle relaxation.
Alternate Names
There is no internationally recognized non-proprietary name for this combination. It is often referred to by its components.
Brand Names: Some common brand names include Spastal, Ketospas, Superspas, Spasmogan, Spasnac.
How It Works
Pharmacodynamics: Diclofenac exerts its analgesic and anti-inflammatory effects by inhibiting COX-1 and COX-2, thus reducing prostaglandin production. Fenpiverinium acts as an anticholinergic agent, blocking the action of acetylcholine at muscarinic receptors in smooth muscle, reducing spasms. Pitofenone directly relaxes smooth muscle, potentially by inhibiting calcium channels.
Pharmacokinetics: Diclofenac is well absorbed orally and is metabolized primarily in the liver, excreted by the kidneys. Fenpiverinium’s pharmacokinetic profile when given in combination with diclofenac and pitofenone is not well established, but it is known to be poorly absorbed and to have a shorter duration of action when compared to other anticholinergics. Pitofenone is also well absorbed orally and is believed to have a long half life. More information is needed for exact pathways of each when combined with diclofenac and pitofenone.
Mode of Action: Diclofenac inhibits COX enzymes, leading to decreased prostaglandin synthesis. Fenpiverinium blocks muscarinic acetylcholine receptors, reducing smooth muscle contractions. Pitofenone’s mechanism may involve blocking calcium channels to reduce smooth muscle activity, acting similarly to papaverine.
Receptor Binding, Enzyme Inhibition, or Neurotransmitter Modulation: Diclofenac: COX-1 and COX-2 enzyme inhibition. Fenpiverinium: Muscarinic acetylcholine receptor antagonist. Pitofenone: Possible calcium channel blockade. Exact cellular interactions are not fully characterized when combined with diclofenac and pitofenone.
Elimination Pathways: Diclofenac is primarily metabolized by the liver through several pathways including CYP2C9 and is excreted mainly by the kidneys. Fenpiverinium is also excreted through the kidneys. Pitofenone’s elimination hasn’t been characterized when combined with diclofenac and pitofenone.
Dosage
Standard Dosage
Adults: The typical dose is one tablet containing 50mg diclofenac, 0.1mg fenpiverinium, and 5mg pitofenone, taken two to three times a day. The maximum recommended daily dose of diclofenac is 150mg. It should be taken with food.
Children: This combination is generally not recommended for use in children. Safety and efficacy have not been established for pediatric patients.
Special Cases:
- Elderly Patients: Start with the lowest effective dose and monitor closely for adverse effects.
- Patients with Renal Impairment: Caution is advised, and dose adjustment may be necessary.
- Patients with Hepatic Dysfunction: Caution is advised, and dose adjustment may be necessary.
- Patients with Comorbid Conditions: Use with caution in patients with cardiovascular disease, gastrointestinal disorders, or a history of peptic ulcers.
Clinical Use Cases
This combination isn’t typically used in clinical settings such as intubation, surgical procedures, mechanical ventilation, or the ICU. Its use is primarily focused on managing pain and spasms in ambulatory patients. In emergency situations requiring pain management, other options are generally preferred.
Dosage Adjustments
Dose adjustments are based on patient-specific factors, including renal and hepatic function, co-morbidities, and potential drug interactions. For elderly patients or those with renal/hepatic impairment, the lowest effective dose should be used.
Side Effects
Common Side Effects: Nausea, vomiting, heartburn, stomach pain, indigestion, loss of appetite, diarrhea, dizziness, drowsiness, dry mouth, blurred vision, constipation.
Rare but Serious Side Effects: Gastrointestinal bleeding, peptic ulcer, allergic reactions, liver dysfunction, kidney damage, cardiovascular events (heart attack, stroke), blood disorders.
Long-Term Effects: Long-term use, especially at higher doses, increases the risk of gastrointestinal and renal complications. Regular monitoring is advised.
Contraindications
- Hypersensitivity to any of the components.
- Active peptic ulcer or gastrointestinal bleeding.
- Severe heart failure (NYHA Class III or IV).
- Severe hepatic or renal impairment.
- Coronary artery bypass graft (CABG) surgery.
- Third trimester of pregnancy.
Drug Interactions
- NSAIDs, anticoagulants, antihypertensives: Increased risk of bleeding.
- Lithium, digoxin, methotrexate: Increased toxicity of these drugs.
- Diuretics, ACE inhibitors: Reduced effectiveness of these drugs.
- Alcohol: Increased risk of gastrointestinal side effects.
- CYP2C9 inhibitors/inducers: May affect diclofenac metabolism.
Pregnancy and Breastfeeding
Pregnancy Safety Category: Not recommended during pregnancy, especially in the third trimester, due to the risk of premature closure of the ductus arteriosus in the fetus.
Breastfeeding: It is not known whether these drugs are excreted in breast milk, so caution is advised. If use is necessary, consider potential risks to the infant.
Drug Profile Summary
- Mechanism of Action: See above.
- Side Effects: See above.
- Contraindications: See above.
- Drug Interactions: See above.
- Pregnancy & Breastfeeding: See above.
- Dosage: See above.
- Monitoring Parameters: Renal function, liver function, blood pressure, complete blood count, signs of gastrointestinal bleeding.
Popular Combinations
This combination itself contains three active ingredients. Additional combinations with other medications are not generally recommended unless specifically indicated by a physician. Always assess potential drug interactions.
Precautions
- Evaluate for pre-existing medical conditions, allergies, and drug interactions.
- Monitor renal and hepatic function, especially with long-term use.
- Caution in elderly patients and those with cardiovascular disease.
- Avoid alcohol and smoking.
- May cause drowsiness; advise caution when driving or operating machinery.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Diclofenac + Fenpiverinium + Pitofenone?
A: One tablet (50mg diclofenac, 0.1mg fenpiverinium, 5mg pitofenone) two to three times daily, with food. Maximum 150mg of diclofenac per day.
Q2: Is it safe to take this medication during pregnancy?
A: No. It’s contraindicated in the third trimester, and generally not recommended during any stage of pregnancy.
Q3: What are the common side effects?
A: Nausea, vomiting, heartburn, stomach pain, diarrhea, dizziness, drowsiness, dry mouth are common side effects.
Q4: Can I drink alcohol while taking this medication?
A: It is best to avoid alcohol due to the increased risk of gastrointestinal side effects.
Q5: What should I do if I miss a dose?
A: Take the missed dose as soon as you remember, unless it’s close to the time for the next dose. Don’t double the dose.
Q6: Can this medication be used for long-term pain management?
A: Long-term use should be carefully considered and monitored due to the increased risk of adverse effects, particularly gastrointestinal and renal issues.
Q7: Is this combination safe for children?
A: Not generally recommended for children. Safety and efficacy have not been established in pediatric patients.
Q8: What are the signs of an allergic reaction?
A: Hives, difficulty breathing, swelling of the face, lips, tongue, or throat. Seek medical attention immediately if these occur.
Q9: Can I take this with other painkillers like ibuprofen or aspirin?
A: Combining with other NSAIDs is not recommended due to increased risk of side effects. Consult with a doctor.
Q10: Are there any specific dietary restrictions while taking this medication?
A: Take with food to reduce stomach upset. There are no other specific dietary restrictions typically recommended.
