Usage
Diclofenac + Dicyclomine is prescribed for the management of abdominal pain and cramps associated with conditions like irritable bowel syndrome (IBS), dysmenorrhea (painful menstruation), renal colic, biliary colic, and other gastrointestinal spasms.
Pharmacological Classification:
- Diclofenac: Non-Steroidal Anti-inflammatory Drug (NSAID)
- Dicyclomine: Anticholinergic, Antispasmodic
Mechanism of Action:
Diclofenac inhibits cyclooxygenase (COX) enzymes, reducing prostaglandin synthesis, which are mediators of pain and inflammation. Dicyclomine acts as an anticholinergic agent, blocking the action of acetylcholine at muscarinic receptors, leading to relaxation of smooth muscles in the gastrointestinal tract, thereby reducing spasms and pain.
Alternate Names
This combination medication doesn’t have a specific international nonproprietary name (INN). It is generally referred to by the names of its two components.
Brand Names:
Several brand names exist in different regions; a few examples include Cataspa and Spasmonil.
How It Works
Pharmacodynamics:
Diclofenac, by inhibiting COX enzymes, primarily COX-1 and COX-2, reduces prostaglandin synthesis. Prostaglandins are involved in inflammation, pain, and fever. Dicyclomine, as an anticholinergic, inhibits the binding of acetylcholine to muscarinic receptors, located on smooth muscle cells. This inhibition prevents muscle contraction and induces relaxation.
Pharmacokinetics:
Diclofenac is well absorbed orally, reaching peak plasma concentrations within 1-2 hours. It is metabolized in the liver, primarily by CYP2C9, and excreted through the kidneys. Dicyclomine is also readily absorbed orally and is extensively metabolized in the liver. The elimination pathways for dicyclomine are not fully characterized but involve both renal and hepatic mechanisms.
Mode of Action:
Diclofenac reduces inflammation and pain by reducing prostaglandin synthesis at the site of injury or inflammation. Dicyclomine acts by relaxing the smooth muscles of the gastrointestinal tract by blocking the effect of acetylcholine on muscarinic receptors.
Receptor Binding, Enzyme Inhibition, or Neurotransmitter Modulation:
- Diclofenac: Inhibits COX-1 and COX-2 enzymes.
- Dicyclomine: Blocks muscarinic receptors (M1, M2, M3 subtypes).
Elimination Pathways:
- Diclofenac: Primarily renal excretion, hepatic metabolism (CYP2C9).
- Dicyclomine: Renal and hepatic pathways, not fully characterized.
Dosage
The dosage of Diclofenac + Dicyclomine varies depending on the patient’s age, condition, and response to therapy.
Standard Dosage
Adults:
The typical adult dose is Diclofenac 50 mg + Dicyclomine 20 mg taken orally, three times a day, preferably before meals.
Children:
This combination is generally not recommended for children under 12 years old. Safety and efficacy in children have not been well established.
Special Cases:
- Elderly Patients: Start with the lowest effective dose and monitor carefully for adverse events.
- Patients with Renal Impairment: Caution should be exercised, and dose adjustment may be necessary.
- Patients with Hepatic Dysfunction: Caution should be exercised, and dose adjustment may be necessary.
- Patients with Comorbid Conditions: Close monitoring and dosage adjustments might be needed depending on the specific comorbid condition (e.g., cardiovascular disease, diabetes).
Clinical Use Cases
The primary use of this combination is for managing abdominal pain and cramps from IBS or dysmenorrhea. There isn’t enough evidence to support its use in settings like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations.
Dosage Adjustments
Dosage adjustments are based on patient response, renal function, and hepatic function. It’s crucial to monitor for adverse events, particularly gastrointestinal issues. For elderly patients, start with the lowest effective dose.
Side Effects
Common Side Effects:
Nausea, vomiting, dry mouth, dizziness, blurred vision, drowsiness, constipation, and weakness.
Rare but Serious Side Effects:
Allergic reactions (e.g., angioedema, anaphylaxis), gastrointestinal bleeding, peptic ulcer, Stevens-Johnson syndrome, and cardiac events.
Long-Term Effects:
Chronic use of NSAIDs like diclofenac can increase the risk of cardiovascular events and renal impairment.
Adverse Drug Reactions (ADR):
Severe allergic reactions, gastrointestinal bleeding, acute renal failure, and hepatic dysfunction.
Contraindications
- Hypersensitivity to either diclofenac or dicyclomine.
- Active gastrointestinal bleeding or peptic ulcer.
- Severe hepatic or renal impairment.
- Glaucoma.
- Myasthenia gravis.
- Obstructive uropathy.
- Infants less than 6 months of age.
- Breastfeeding mothers.
Drug Interactions
- Other NSAIDs (increased risk of gastrointestinal side effects).
- Anticoagulants (increased bleeding risk).
- Anticholinergic drugs (additive anticholinergic effects).
- Alcohol (increased risk of gastrointestinal bleeding).
- Methotrexate (increased toxicity).
- Diuretics (reduced diuretic efficacy).
Pregnancy and Breastfeeding
Diclofenac + Dicyclomine is generally contraindicated during pregnancy, especially in the third trimester due to the risk of premature closure of the ductus arteriosus. It is also contraindicated during breastfeeding.
Drug Profile Summary
- Mechanism of Action: Diclofenac inhibits COX enzymes, reducing prostaglandins; Dicyclomine blocks muscarinic receptors, relaxing smooth muscles.
- Side Effects: Nausea, vomiting, dry mouth, dizziness, blurred vision, drowsiness, constipation. Serious effects include GI bleeding, allergic reactions.
- Contraindications: Hypersensitivity, GI bleeding, peptic ulcer, severe hepatic/renal impairment, glaucoma, myasthenia gravis, pregnancy, breastfeeding.
- Drug Interactions: Other NSAIDs, anticoagulants, alcohol.
- Pregnancy & Breastfeeding: Contraindicated.
- Dosage: Adults: Diclofenac 50 mg + Dicyclomine 20 mg thrice daily. Adjust for special populations.
- Monitoring Parameters: Blood pressure, renal function, hepatic function, gastrointestinal symptoms.
Popular Combinations
While Diclofenac + Dicyclomine is a popular combination itself, sometimes paracetamol is added to it to provide enhanced analgesic effects.
Precautions
- Pre-existing cardiovascular, renal, or hepatic disease.
- History of peptic ulcer or GI bleeding.
- Asthma.
- Elderly patients.
- Avoid alcohol.
- Use caution when driving or operating machinery.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Diclofenac + Dicyclomine?
A: The typical adult dose is Diclofenac 50 mg + Dicyclomine 20 mg orally three times daily.
Q2: Is Diclofenac + Dicyclomine safe during pregnancy?
A: No, it’s contraindicated, particularly in the third trimester.
Q3: Can this medication be used in children?
A: Generally not recommended for children under 12. Safety and efficacy haven’t been established.
Q4: What are the most common side effects?
A: Nausea, dry mouth, dizziness, blurred vision, constipation.
Q5: What are the serious side effects to watch for?
A: Allergic reactions, gastrointestinal bleeding, changes in renal/hepatic function.
Q6: Can I take this medication with other pain relievers?
A: Consult a physician before combining with other NSAIDs or pain medications.
Q7: How does dicyclomine work to relieve abdominal cramps?
A: Dicyclomine relaxes smooth muscles in the GI tract, reducing spasm and pain.
Q8: Can I consume alcohol while taking Diclofenac + Dicyclomine?
A: No, alcohol should be avoided as it increases the risk of GI side effects.
Q9: What should I do if I miss a dose?
A: Take the missed dose as soon as you remember, unless it is close to the time for the next dose. Do not double the dose to catch up.
Q10: How long can I take Diclofenac + Dicyclomine?
A: Use it for the shortest duration possible as recommended by your physician. Long-term use can increase the risk of side effects.
