Activa Injection, Tablet, Gel

Activa Eye Drops contains Activa Sodium, a potent non-steroidal anti-inflammatory drug with analgesic property. Activa Sodium produces anti-inflammatory effect by inhibiting cyclooxygenase activity with a reduction in the tissue prostaglandin ( such as PgE2 and Pg F2α) .

Uses

Activa Sodium ophthalmic preparation is used for- 

  • Inhibition of miosis during cataract surgery.
  • Post-operative inflammation after cataract surgery and other ocular surgical procedures.
  • Pre-operative and post-operative prevention of cystoid macular edema (CME) associated with lens extraction & intraocular lens implantation.
  • Post-traumatic inflammation in penetrating and non- penetrating wounds (as an adjuvant to local anti-infective therapy).
  • Non-infected chronic conjunctivitis, keratoconjunctivitis.

Activa is also used to associated treatment for these conditions: Actinic Keratosis (AK), Acute Arthritis, Acute Gouty Arthritis, Acute Migraine, Acute Musculoskeletal Pain, Ankylosing Spondylitis (AS), Common Cold, Fever, Gouty Arthritis, Inflammation, Inflammatory Disease of the Oral Cavity, Inflammatory Disease of the throat, Inflammatory Reaction of the Nerve, Joint Pain, Juvenile Idiopathic Arthritis (JIA), Menstrual Distress (Dysmenorrhea), Muscle Inflammation, Ocular Inflammation, Operation site inflammation, Osteoarthritis (OA), Osteoarthritis of the Knee, Pain, Pain, Nerve, Pericarditis, Photophobia, Postoperative pain, Primary Dysmenorrhoea, Radicular Pain, Rheumatic Pain, Rheumatism, Rheumatoid Arthritis, Seasonal Allergic Conjunctivitis, Soreness, Muscle, Spinal pain, Tendon pain, Vertebral column pain, Acute Musculoskeletal injury, Acute, moderate, severe Pain, Inflammatory, Localized soft tissue rheumatism, Mild to moderate joint pain, Mild to moderate pain, Minor pain, Perioperative miosis

Trade Name Activa
Generic Diclofenac
Other Names Diclofenac, Diclofenac acid, Diclofenaco, Diclofenacum
Weight 50mg, 100mg, 25mg
Type Injection, Tablet, Gel
Formula C14H11Cl2NO2
Weight Average: 296.149
Monoisotopic: 295.016684015
Protein binding

Diclofenac is over 99.7% bound to serum proteins, primarily albumin. It is undergoes limited binding to lipoproteins as well with 1.1% bound to HDL, 0.3% to LDL, and 0.15% to VLDL.

Therapeutic Class Ophthalmic Non-Steroid drugs
Manufacturer Zydus Cadila Healthcare Ltd, Pacific Pharmaceuticals Ltd
Available Country India, Bangladesh
Last Updated: June 23, 2021 at 9:00 am

Dosage

Activa dosage

Ophthalmic (Adult)-

  • Postoperative ocular inflammation: Instill into the appropriate eye 4 times daily starting 24 hr after surgery for up to 28 days.
  • Inflammation and discomfort after strabismus surgery: Instill 1 drop 4 times daily for the 1st wk; then tid in the 2nd wk, bid in the 3rd wk, and as required for the 4th wk.
  • Pain and discomfort after radial keratotomy: Instill 1 drop before surgery followed by 1 drop immediately after surgery, and then 1 drop 4 times daily for up to 2 days.
  • Pain after accidental trauma: Instill 1 drop 4 times daily for up to 2 days.
  • Control of inflammation after argon laser trabeculoplasty: Instill 1 drop 4 times during the 2 hr before procedure followed by 1 drop 4 times daily, up to 7 days after procedure.
  • Prophylaxis of intra-operative miosis: Instill into appropriate eye 4 times w/in 2 hr before surgery.
  • Post-photorefractive keratectomy pain: Instill into the affected eye twice, an hr before surgery, then 1 drop twice at 5-min intervals immediately after surgery, then every 2-5 hr while awake for up to 24 hr.
  • Seasonal allergic conjunctivitis: Instill 1 drop before surgery followed by 1 drop immediately after surgery, and then 1 drop 4 times daily for up to 2 days.

Side Effects

Mild to moderate burning sensation in 5-15% patients which is transient in nature and almost never necessitated discontinuation of treatment. Other less common side-effects are sensitivity to light, bad taste, feeling of pressure, allergic reactions etc.

Precaution

Activa eye drops may mask the signs of infection. So physicians should be alert to the development of infections in patients receiving the drug. During prolonged use, it is recommended that physicians conduct periodic examinations of the eye, including measurement of the intraocular pressure. Contact lenses should not be worn during treatment.

Interaction

No drug interaction is reported. There should be at least 5 minutes interval when another ophthalmic solution (e.g., steroid) is given.

Food Interaction

  • Avoid excessive or chronic alcohol consumption. Co-administration with alcohol may increase the risk of gastrointestinal side effects, such as ulceration.
  • Take with food. Food reduces gastric irritation.

Volume of Distribution

Activa has a total volume of distribution of 5-10 L or 0.1-0.2 L/kg. The volume of the central compartment is 0.04 L/kg. Activa distributes to the synovial fluid reaching peak concentration 2-4h after administration. There is limited crossing of the blood brain barrier and cerebrospinal fluid concentrations only reach 8.22% of plasma concentrations. Doses of 50 mg delivered via intramuscular injection produced no detectable diclofenac concentrations in breast milk, however metabolite concentrations were not investigated. Activa has been shown to cross the placenta in mice and rats but human data is unavailable.

Half Life

The terminal half-life of diclofenac is approximately 2 h, however the apparent half-life including all metabolites is 25.8-33 h.

Clearance

Activa has a plasma clearance 16 L/h.

Pregnancy & Breastfeeding use

The safety of Activa eye drops in pregnancy & lactation has not been established and its use therefore is not recommended unless the potential benefit to the mother outweighs the possible risk to the child.

Contraindication

Hypersensitivity to any of the components Like other non steroidal anti-inflammatory agents, Activa Sodium eye drops is contraindicated in patients in whom attacks of asthma, urticaria or acute rhinitis have been observed following application of acetyl salicylic acid or other cyclo-oxygenase inhibitors

Acute Overdose

Accidental ingestion of Activa Sodium presents virtually no risk of unwanted effects, since one 5 ml bottle of eye drop solution contains only 5 mg of Activa Sodium, which is equivalent to about 3% of the recommended maximum oral dose for adults.

Storage Condition

Close the bottle immediately after use. Do not use for more than four weeks after opening. Store at room temperature.

Activa contains Diclofenac see full prescribing information from innovator Monograph