Systaflam

Uses

This topical gel is a Non-steroidal anti-inflammatory (NSAID) drug used to treat pain associated with conditions like gout, migraine, rheumatoid arthritis, sprains of muscles and joints etc.

Systaflam is also used to associated treatment for these conditions: Acute Muscle Pain, Arthritis, Back Pain Lower Back, Backache, Contusions, Joint Pain, Ligament pain, Muscle Inflammation, Muscle Injuries, Muscle Strain, Muscle swelling, Pain, Pain of the Bone and Bones, Pain, Nerve, Partial-Onset Seizures, Postherpetic Neuralgia, Soreness, Muscle, Sprains, Tendon pain, Minor aches, Muscle, joint pains

How Systaflam works

The exact mechanism of action of mephenesin is not known. It has been observed to block both inward sodium and inward calcium currents in neurons . It has a physiological effect which opposes that of strychnine.

Counter-irritation is thought to be effective at alleviating musculoskeletal pain as the irritation of the sensory nerve endings is thought to alter or offset pain in the underlying muscle or joints that are served by the same nerves . This is thought to mask the underlying musculoskeletal pain and discomfort. When applied topically, methyl salicylate is thought to penetrate the skin and underlying tissues where it reversibly inhibits cyclooxygenase enzyme and locally and peripherally prevents the production of inflammatory mediators such as prostaglandin and thromboxane A2.

Dosage

Systaflam dosage

Depending on the size of the area to be treated, 2-4 gm of this gel should be applied to the skin 3-4 times daily to the affected area and rubbed in lightly.

Side Effects

The most commonly reported side-effects of this gel are itching, blisters, allergic contact dermatitis, anaphylactic reactions, pruritus, and rash.

Toxicity

Mephenesin can produce hemolysis leading to hemoglobinuria with intravenous administration of concentrations greater than 10% . As a central nervous system depressant it can also produce paralysis and respiratory depression.

Oral LD50 values (mg/kg) for mouse, rat and rabbit are 1110, 887 and 1300, respectively. Oral LD50 values for child and adult human (mg/kg) are 228 and 506, respectively. Although systemic toxicity from topical administration is rare, methyl salicylate can be absorbed in intract skin to cause stimulation of the central nervous system respiratory center, disturbance of lipid and carbohydrate metabolism, and disturbance of intracellular respiration. Severe toxicity can result in acute lung injury, lethargy, coma, seizures, cerebral edema, and death. In case of salicylate poisoning, the treatment consists of general supportive care, gastrointestinal decontamination with activated charcoal in cases of salicylate ingestion, and monitoring of serum salicylate concentrations. Bicarbonate infusions or hemodialysis can be used to achieve enhanced salicylate elimination .

Precaution

This gel should not be allowed to come in contact with the eyes or mucous membranes. After application, the hands should be washed unless they are the sites being treated. Not to be taken by mouth.

Volume of Distribution

After absorption, methyl salicylate is distributed throughout most body tissues and most transcellular fluids, primarily by pH dependent passive processes. Salicylate is actively transported by a low-capacity, saturable system out of the CSF across the choroid plexus. The drug readily crosses the placental barrier.

Elimination Route

Approximately 12-20% of topically applied methyl salicylate may be systemically absorbed through intact skin within 10 hours of application, and absorption varies with different conditions such as surface area and pH. Dermal bioavailability is in the range of 11.8 – 30.7%. For the assessment of potential oral exposure to salicylates, bioavailability is assumed to be 100% .

Half Life

The plasma half-life for salicylate is 2 to 3 hr in low doses and about 12 hr at usual anti-inflammatory doses. The half-life of salicylate may be as long as 15 to 30 hr at high therapeutic doses or when there is intoxication.

Elimination Route

Excreted by kidneys as free salicylic acid (10%), salicyluric acid (75%), salicylic phenolic (10%) and acyl glucuronide (5%), and gentisic acid (less than 1%).

Pregnancy & Breastfeeding use

Not recommended.

Contraindication

It is contraindicated in patients who have hypersensitivity to this gel. In addition, This gel should not be used if one has the following conditions:

• children less than 12 years old
• cuts
• infected skin

Storage Condition

It should be stored in a cool and dry place, protected from light and moisture.

Innovators Monograph

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