Acitaz-MR

Aceclofenac (100mg) + Tizanidine (2mg)
Price: ₹125 - ₹185 for 10 tablets strip
Mfr: Sun Pharmaceutical Industries Ltd. | Form: Tablet

📋 Clinical Overview

A fixed-dose combination (FDC) of a non-steroidal anti-inflammatory drug (NSAID) and a centrally-acting skeletal muscle relaxant. Aceclofenac provides potent analgesic and anti-inflammatory effects by inhibiting cyclooxygenase (COX) enzymes and prostaglandin synthesis. Tizanidine, an alpha-2 adrenergic agonist, reduces spasticity by inhibiting the release of excitatory amino acids in spinal interneurons. This combination is specifically designed for the short-term management of acute, painful musculoskeletal conditions where muscle spasm is a significant component, offering synergistic relief of pain, inflammation, and associated muscle rigidity.

💊 Dosage & Administration

Adult: One tablet (Aceclofenac 100mg + Tizanidine 2mg) twice daily, after meals. The dose should be individualized to the lowest effective dose for the shortest duration.

Note: Take with food or milk to minimize gastrointestinal upset. Swallow whole with a full glass of water. Do not crush or chew. Avoid lying down for at least 10 minutes after taking the tablet. The total duration of therapy should generally not exceed 2-3 weeks.

⚠️ Contraindications

  • Hypersensitivity to Aceclofenac, Tizanidine, or any component (including other NSAIDs like aspirin)
  • Active peptic ulcer disease or history of recurrent ulcer/bleeding
  • Severe hepatic impairment (Child-Pugh Class C) or active liver disease
  • Severe renal impairment (eGFR <30 mL/min) or progressive renal disease
  • Patients with history of asthma, urticaria, or allergic-type reactions after taking NSAIDs
  • Concomitant use with other potent CYP1A2 inhibitors (e.g., Fluvoxamine, Ciprofloxacin) due to risk of severe Tizanidine toxicity
  • Third trimester of pregnancy

🔬 Mechanism of Action

The combination works via two distinct but complementary pathways. Aceclofenac inhibits the enzymes cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2), thereby blocking the conversion of arachidonic acid to prostaglandins (PGs) and thromboxanes. This reduces the synthesis of inflammatory mediators (PGE2, PGI2) responsible for pain, swelling, and fever. Tizanidine acts as a centrally-acting alpha-2 adrenergic receptor agonist, primarily at the level of the spinal cord. It presynaptically inhibits the release of excitatory neurotransmitters (like glutamate and aspartate) from spinal interneurons, leading to reduced facilitation of spinal motor neurons. This results in decreased muscle tone and relief of spasm.

🤕 Side Effects

  • Drowsiness, sedation, dizziness
  • Dry mouth
  • Nausea, dyspepsia, epigastric pain
  • Fatigue, asthenia
  • Hypotension (especially with first dose)

🤰 Special Populations

Pregnancy: Pregnancy Category C (US FDA). Avoid, especially in the first and third trimesters. Third trimester use is contraindicated due to risk of premature closure of ductus arteriosus, oligohydramnios, and prolonged labor. Use only if potential benefit justifies potential fetal risk.

Driving: May impair alertness, reaction time, and motor coordination due to Tizanidine's sedative effect. Patients should be cautioned against driving or operating machinery, especially at initiation of therapy.

🔄 Drug Interactions

Other NSAIDs (e.g., Ibuprofen, Naproxen, Aspirin)Increased risk of GI toxicity (bleeding, ulcers) and renal impairment.Major
Anticoagulants (Warfarin, NOACs like Rivaroxaban)Increased risk of bleeding due to antiplatelet effect of Aceclofenac and potential pharmacokinetic interactions.Major
CYP1A2 Inhibitors (Fluvoxamine, Ciprofloxacin)Markedly increases Tizanidine plasma levels (up to 33-fold), leading to profound hypotension and sedation. CONTRAINDICATED.Contraindicated
Oral Corticosteroids (Prednisolone)Increased risk of GI ulceration and bleeding.Major
Antihypertensives (ACE inhibitors, ARBs, Diuretics)Reduced antihypertensive efficacy; increased risk of renal impairment.Moderate
Selective Serotonin Reuptake Inhibitors (SSRIs e.g., Fluoxetine)Increased risk of upper GI bleeding.Moderate
Central Nervous System Depressants (Alcohol, Benzodiazepines, Opioids)Additive sedative effects, impaired alertness and motor coordination.Major
MethotrexateReduced renal clearance of Methotrexate, increasing its toxicity.Major
LithiumAceclofenac may decrease renal clearance of Lithium, leading to toxicity.Major

🔁 Alternatives to Acitaz-MR

Same composition (Aceclofenac (100mg) + Tizanidine (2mg)), different brands:

Zerodol-SP Dolokind-MR Aceproxyvon-TZ Asozen-TZ Acefen-TZ