Usage
Drotaverine + Paracetamol is prescribed for the symptomatic relief of pain associated with smooth muscle spasms in conditions like abdominal cramps, renal colic, biliary colic, and dysmenorrhea. It is also used to manage pain and fever associated with various conditions, including headache, musculoskeletal pain, and common cold.
Its pharmacological classifications include:
- Drotaverine: Antispasmodic, Phosphodiesterase 4 (PDE4) inhibitor
- Paracetamol: Analgesic, Antipyretic
Drotaverine works by inhibiting PDE4, which leads to increased intracellular cAMP, resulting in smooth muscle relaxation. Paracetamol’s mechanism is not fully understood, but it is thought to inhibit cyclooxygenase (COX) enzymes in the central nervous system, reducing pain and fever.
Alternate Names
No widely recognized alternate names exist for this specific combination. It is generally referred to as Drotaverine + Paracetamol or Drotaverine Hydrochloride + Paracetamol.
Some brand names under which the combination is marketed include:
- Drotin Plus
- Spascol
- and others (various regional brand names exist).
How It Works
Pharmacodynamics: Drotaverine exerts a direct relaxant effect on smooth muscles, primarily in the gastrointestinal, biliary, and urogenital tracts. It does not affect the autonomic nervous system and lacks anticholinergic side effects. Paracetamol acts centrally to reduce pain and fever. It has minimal anti-inflammatory effects.
Pharmacokinetics:
- Drotaverine: Well-absorbed orally. Metabolized in the liver, primarily by CYP enzymes. Excreted primarily in urine.
- Paracetamol: Rapidly absorbed orally. Metabolized in the liver, primarily by glucuronidation and sulfation. Excreted mainly in urine as metabolites. A small percentage is metabolized by CYP2E1 to a potentially hepatotoxic metabolite, N-acetyl-p-benzoquinone imine (NAPQI).
Mode of Action:
- Drotaverine: Inhibits PDE4, leading to increased intracellular cAMP and smooth muscle relaxation.
- Paracetamol: Inhibits COX enzymes centrally, reducing prostaglandin synthesis, which is involved in pain and fever signaling.
Elimination Pathways:
- Drotaverine: Primarily renal excretion.
- Paracetamol: Primarily hepatic metabolism and renal excretion.
Dosage
Standard Dosage
Adults:
The typical adult dosage is one tablet containing 80 mg of Drotaverine and 500 mg of Paracetamol, taken two to three times daily.
Children:
Dosage in children should be determined by a pediatrician based on the child’s weight and age. It is generally not recommended for children under one year of age. For children aged 1-6 years, a lower dose of Drotaverine (20 mg) might be considered, given three to four times daily. For children older than 6 years, up to 40 mg of Drotaverine can be given, as advised by the pediatrician.
Special Cases:
- Elderly Patients: Dose adjustments may be necessary due to age-related decline in renal and hepatic function.
- Patients with Renal Impairment: Dose reduction might be required depending on the severity of impairment.
- Patients with Hepatic Dysfunction: Dose reduction is necessary in moderate to severe hepatic impairment. Contraindicated in severe liver disease.
- Patients with Comorbid Conditions: Caution is advised in patients with cardiovascular disease or other relevant comorbidities.
Clinical Use Cases
The combination of Drotaverine and Paracetamol is not typically used in the specific clinical settings of intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations like status epilepticus or cardiac arrest. It is primarily indicated for the management of pain associated with smooth muscle spasms.
Dosage Adjustments
Dose adjustments are necessary in patients with renal or hepatic impairment. It is crucial to monitor liver function tests in patients with hepatic dysfunction or those receiving prolonged therapy.
Side Effects
Common Side Effects:
- Dry mouth
- Thirst
- Dizziness
- Headache
- Drowsiness
- Nausea
- Vomiting
Rare but Serious Side Effects:
- Allergic reactions (skin rash, itching, swelling)
- Hepatotoxicity (with Paracetamol overdose)
- Blood disorders (rare)
Long-Term Effects:
Long-term use, especially of high doses of Paracetamol, can increase the risk of liver damage.
Adverse Drug Reactions (ADR):
Severe allergic reactions, hepatotoxicity, and blood disorders require immediate medical attention.
Contraindications
- Hypersensitivity to Drotaverine, Paracetamol, or any component of the formulation.
- Severe hepatic impairment or active liver disease.
- Severe renal insufficiency.
- Children under one year of age (some sources suggest younger than six years).
- Second or third-degree atrioventricular (AV) block (for Drotaverine).
- Severe heart failure (for Drotaverine).
Drug Interactions
- Alcohol: Increases the risk of liver damage with Paracetamol.
- Anticoagulants (e.g., warfarin): Paracetamol may enhance their effect.
- Antihypertensives: Drotaverine may enhance their effect.
- Levodopa: Drotaverine may reduce its effectiveness.
- Medications metabolized by CYP2E1 or CYP3A4: Interactions are possible, consult with a doctor before co-administration.
Pregnancy and Breastfeeding
- Pregnancy: Drotaverine use during pregnancy is generally avoided unless clearly necessary. Paracetamol is generally considered safe for short-term use during pregnancy.
- Breastfeeding: Both drugs are excreted in breast milk. Paracetamol is generally considered compatible with breastfeeding. However, caution should be exercised with Drotaverine during breastfeeding, and its use should be limited.
Drug Profile Summary
- Mechanism of Action: Drotaverine: Smooth muscle relaxant via PDE4 inhibition. Paracetamol: Analgesic and antipyretic, likely via central COX inhibition.
- Side Effects: Common: Dry mouth, thirst, dizziness, headache, drowsiness, nausea, vomiting. Serious: Allergic reactions, hepatotoxicity, blood disorders.
- Contraindications: Hypersensitivity, severe hepatic/renal impairment, children under one year, severe heart conditions.
- Drug Interactions: Alcohol, anticoagulants, antihypertensives, levodopa, CYP2E1/CYP3A4 substrates.
- Pregnancy & Breastfeeding: Drotaverine: Caution advised. Paracetamol: Generally safe for short-term use.
- Dosage: Adults: 80 mg Drotaverine + 500 mg Paracetamol, 2-3 times/day. Pediatric: Consult pediatrician.
- Monitoring Parameters: Liver function tests, especially with long-term use or hepatic impairment.
Popular Combinations
While Drotaverine + Paracetamol is itself a combination, it might be co-prescribed with other medications depending on the specific clinical situation. However, it is important to consider potential drug interactions.
Precautions
- Pre-existing liver or kidney disease requires dose adjustments and careful monitoring.
- Alcohol should be avoided due to increased risk of liver damage with Paracetamol.
- Caution is advised during pregnancy and breastfeeding.
- Driving or operating machinery should be avoided if dizziness or drowsiness occurs.
- Monitor blood pressure and cardiovascular status, especially in patients with heart failure.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Drotaverine + Paracetamol?
A: The standard adult dose is 80 mg Drotaverine + 500 mg Paracetamol, taken two to three times daily. Pediatric dosages should be determined by a pediatrician.
Q2: Can this combination be used during pregnancy?
A: Drotaverine is generally avoided during pregnancy unless the benefits outweigh the risks. Paracetamol is generally considered safe for short-term use. Consult a doctor before use.
Q3: What are the common side effects?
A: Common side effects include dry mouth, thirst, dizziness, headache, drowsiness, nausea, and vomiting.
Q4: Is it safe to take this combination with alcohol?
A: No, alcohol should be avoided as it can increase the risk of liver damage with Paracetamol.
Q5: Are there any drug interactions I should be aware of?
A: Yes, potential interactions exist with anticoagulants, antihypertensives, levodopa, and medications metabolized by CYP2E1/CYP3A4. Consult with a doctor about all medications you are taking.
Q6: Can I take this medication if I have liver or kidney problems?
A: Dose adjustments and careful monitoring are necessary in patients with liver or kidney disease. Severe hepatic impairment is a contraindication.
Q7: How long can I take this medication?
A: It is generally intended for short-term use. Long-term use, particularly of high doses of Paracetamol, increases the risk of liver damage.
Q8: What should I do if I miss a dose?
A: Take the missed dose as soon as you remember unless it is almost time for your next dose. Do not double the dose.
Q9: Is this combination safe for children?
A: Dosage in children needs careful assessment by a pediatrician based on the child’s age, weight, and medical condition. It is generally not recommended for children under one year of age.
Q10: What are the signs of an overdose?
A: Signs of overdose, especially of Paracetamol, include nausea, vomiting, abdominal pain, and liver damage. Seek immediate medical attention if overdose is suspected.
