Dolac: Dosage, Contraindications, Precautions, Interactions, Mechanism of Action and Storage

Ketorolac tromethamine is a non-steroidal anti-inflammatory drug (NSAID).

It is indicated for the short-term treatment (up to 5 days in adults) of moderately severe acute pain requiring analgesia at the opioid level and only as a continuation treatment after intravenous administration or IM dosing of ketorolac tromethamine, if necessary.

Dosage of Dolac

Ophthalmic eye itching associated with seasonal allergic conjunctivitis

Adult: as 0.5% solution: apply 1 drop to the affected eye 4 times a day.

Ophthalmic prophylaxis and reduction of postoperative eye inflammation

Adult: as 0.5% solution: inject 1 drop into the appropriate eyes 4 times a day, starting 24 hours after cataract surgery and continuing until the first 2 weeks of the postoperative period.

Postoperative (oral) pain

Adult: moderate to severe: 20 mg, followed by 10 mg 4-6 hrly as therapy for continuation of parenteral administration. Max: 40 mg daily. Maximum duration: 5 days (combined parenteral and oral).

Elderly: 10 mg, followed by 10 mg 4-6 hr as therapy for continuation of parenteral administration. Max: 40 mg daily.

Parenteral postoperative pain

Adult: moderate to severe: initially 10 mg, followed by 10-30 mg 4-6 hr as needed (up to 2 hr during the initial postoperative period) intravenously or IV bolus for ≥15 seconds. Max: 90 mg daily. Maximum duration: 2 days.

Elderly: Max: 60 mg per day.

The oral formulation should not be given as a starting dose.

Use minimum effective dose for the individual patient.

Do not shorten the dosing interval to 4 to 6 hours.

Total duration of treatment in adult patients: the combined duration of use of IV or IM dosing of ketorolac tromethamine and ketorolac tromethamine tablets should not exceed 5 days.

Contraindications

  • Patients with hypersensitivity to ketorolac, aspirin or other NSAIDs. It was not designed as a prophylactic analgesic before surgery and for intraoperative use.
  • Patient with a history of asthma, active history, or history of peptic ulcer , history or history of hemorrhage or gastrointestinal perforation; suspected or confirmed cerebrovascular haemorrhage, haemorrhagic diathesis, incomplete haemostasis, high risk of haemorrhage.
  • Complete or partial syndrome of nasal polyps , angioedema or bronchospasm.
  • Patient at risk of kidney failure due to volume depletion or dehydration.
  • Treatment of perioperative pain in the context of CABG surgery.
  • Moderate to severe kidney failure. Concomitant use with probenecid, lithium, pentoxifylline, anticoagulants, other NSAIDs or aspirin.

Dolac special precautions

Patient with a history of hypertension and / or heart failure, predisposition to reduced vol and / or renal blood flow.

Patient weight <50 kg. Higher. Mild kidney or liver failure. Pregnancy and breastfeeding.

Adverse drug reactions

  • Drowsiness.
  • Dizziness
  • Headache.
  • Mental and sensory changes.
  • Psychotic reactions.
  • Sweating
  • Dry mouth.
  • However.
  • Fever.
  • Seizures
  • Myalgia.
  • Meningitis.
  • Aseptic
  • HTA.
  • Dyspnoea.
  • Pulmonary edema.
  • Bradicardia
  • Chest pain.
  • Palpitations
  • Fluid retention.
  • Increases in blood urea and creatinine.
  • Acute renal failure.
  • Edema.
  • Hyponatremia.
  • Hyperkalemia.
  • Urinary frequency or retention.
  • Nephritic syndrome.
  • Flank pain with or without hematuria.
  • Thrombocytopenia
  • Epistaxis.
  • Inhibition of platelet aggregation.
  • Hematoma.
  • Redness or paleness
  • Pancreatitis.
  • Changes in liver function
  • Hepatitis.
  • Liver failure.
  • Pain at the site of infection.

Potentially fatal

  • Anaphylaxis .
  • Serious skin reactions (eg, exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis).
  • Myocardial infarction.
  • Stroke
  • Digestive bleeding.
  • Perforation or ulceration

Symptoms of overdose

  • Abdominal pain.
  • Sickness.
  • Vomiting
  • Hyperventilation
  • Peptic ulceration.
  • Erosive gastritis and kidney dysfunction.
Management of overdose

Consider gastric lavage or administration of activated charcoal with 1 hour of ingestion.

Interactions

Increased risk of gastrointestinal ulceration or bleeding with corticosteroids, SSRIs, or antiplatelet agents.

May increase the toxicity of methotrexate . Increased risk of nephrotoxicity with diuretics, cyclosporine, tacrolimus, ACE inhibitors, or angiotensin II receptor antagonists. Hallucinations can occur when used with psychoactive drugs (eg, fluoxetine, thiothixene, alprazolam).

Concurrent use with anticonvulsant therapy (eg, phenytoin, carbamazepine) rarely causes seizures.

Potentially fatal

Increased risk of bleeding associated with ketorolac with anticoagulants, aspirin or other NSAIDs and pentoxifylline.

Increase plasma concentration and half-life with probenecid. Increased plasma lithium concentration.

Mechanism of action of the Dolac

Description : Dolac reversibly inhibits the enzymes cyclooxygenase-1 and -2 (COX-1 and -2), which results in a decrease in the formation of prostaglandin precursors.

It exhibits a minimal anti-inflammatory effect in its analgesic dose. Start: approximately 30 minutes (IM / IV). Duration: 4-6 h.

Pharmacokinetics

Absorption: rapid and complete absorption after IM administration.

Bioavailability: 80-100% (oral); about 4% (ophth).

Time to maximum plasma concentration: approximately 30-60 min (IM).

Distribution : crosses the placenta and enters breast milk (small amounts); poorly penetrates the blood-brain barrier.

Volume of distribution: approximately 13 L. Plasma protein binding:> 99%.

Metabolism : undergoes conjugation with glucuronic acid; hydroxylation in the liver to form p-hydroxycetorolac.

Excretion: via urine (approximately 90% as unchanged drug, conjugated and hydroxylated metabolites); stool (remaining dose).

Terminal elimination half-life: approximately 4-6 h.

Storage

  • Dolac should be stored between 15-30 ° C.
  • Protect from light.