Alcazar uses, dosage, side effects, FAQ - DrugFAQ (2023)

Alcazar

Alcazar Eye Drops contains Alcazar sodium, a powerful non-steroidal anti-inflammatory drug with analgesic effects. Alcazar sodium produces an anti-inflammatory effect by inhibiting cyclooxygenase activity with a reduction in tissue prostaglandins (such as PgE2 and Pg F2α).

Alcazar reduces inflammation, thereby reducing nociceptive pain and fighting fever. It also increases the risk of developing a peptic ulcer by inhibiting the production of protective mucus in the stomach.

Used

Alcazar sodium eye preparation is used for

• Inhibition of miosis during cataract surgery.
• Postoperative inflammation after cataract surgery and other ophthalmic surgery.
• Preoperative and postoperative prevention of cystoid macular edema (CME) associated with lens extraction and intraocular lens implantation.
• Post-traumatic inflammation in penetrating and non-penetrating wounds (adjuvant to local anti-infective therapy).
• Uninfected chronic conjunctivitis, keratoconjunctivitis.

Alcazar is also used in the concomitant treatment of the following conditions: actinic keratosis (AK), acute arthritis, gouty arthritis acute, migraine acute, acute musculoskeletal pain, ankylosing spondylitis (AS), common cold, fever, gouty arthritis, inflammation, inflammatory Oral cavity disease, pharyngeal inflammatory disease, nerve inflammatory reaction, joint pain, juvenile idiopathic arthritis (JIA), menstrual cramps (dysmenorrhea), muscle inflammation, eye inflammation, surgical site inflammation, osteoarthritis (OA), osteoarthritis of the knee, pain, pain, Nerve, pericarditis, photophobia, postoperative pain, primary dysmenorrhea, radicular pain, rheumatic pain, rheumatism, rheumatoid arthritis, seasonal allergic conjunctivitis, pain, muscular, spinal, tendon, spinal pain, acute musculoskeletal injury , Acute, moderate , severe pain, inflammation, localized soft partial rheumatism, mild to moderate joint pain, mild to moderate pain, mild pain, perioperative miosis

How Alcazar works

Alcazar inhibits cyclooxygenase-1 and -2, the enzymes responsible for the production of prostaglandin (PG) G₂which is the forerunner of other PGs. These molecules have broad activity in pain and inflammation, and inhibition of their production is the common mechanism that links all diclofenac effects.

PGE₂is the primary PG involved in the modulation of nociception. It mediates peripheral sensitization through a variety of effects. PGE₂activates the G_Q-coupled EP₁receptor, resulting in increased activity of the inositol trisphosphate/phospholipase C pathway. Activation of this pathway releases intracellular stores of calcium, which directly lower the action potential threshold and activate protein kinase C (PKC), which contributes to several indirect mechanisms. PGE₂also activates the XP₄receptor coupled to G_S, which activates the adenylyl cyclase/protein kinase A (AC/PKA) signaling pathway. PKA and PKC both contribute to the potentiation of transient receptor potential potentiation of the cation channel subfamily V, member 1 (TRPV1), which increases sensitivity to thermal stimuli. They also activate tetrodotoxin-resistant sodium channels and inhibit inward potassium currents. PKA also contributes to activation of the P2X3 purine receptor and sensitization of T-type calcium channels. Activation and sensitization of depolarizing ion channels and inhibition of inward potassium currents serve to reduce the intensity of the stimulus necessary to generate action potentials in nociceptive sensory afferents. PGE₂trade on EP₃to increase sensitivity to bradykinin and via EP₂to further increase heat sensitivity. Central sensitization occurs in the dorsal horn of the spinal cord and is mediated by the EP₂receptor that couples to G_S. Presynaptically, this receptor increases the release of the pronociceptive neurotransmitters glutamate, CGRP, and substance P. Postsynaptically, it increases the activity of AMPA and NMDA receptors and produces inhibition of inhibitory glycinergic neurons. Together, these result in a reduced activation threshold, allowing low-intensity stimuli to generate pain signals. PGI₂is known to play a role via his G_S-coupled IP receptor, although the magnitude of its contribution varies. It has been suggested that it is of greater importance in painful inflammatory conditions such as arthritis. By limiting peripheral and central sensitization via these pathways, NSAIDs can effectively reduce inflammatory pain.

ggA₂and PGE₂contribute to acute inflammation via their IP and EP₂receptors. Similar to β-adrenergic receptors, these are G_S-coupled and mediates vasodilation via the AC/PKA pathway. PGE₂also contributes by increasing leukocyte adhesion to the endothelium and pulling the cells to the site of injury. PID₂plays a role in activating the release of cytokines by endothelial cells through its DP₁Receptor. PGI₂and PGE₂modulate activation and differentiation of T helper cells by IP, EP₂, and EP₄Receptors believed to be an important activity in the pathology of arthritic conditions. By limiting the production of these PGs at the site of injury, NSAIDs can reduce inflammation.

PGE₂can cross the blood-brain barrier and act on excitatory G_QEP₃Receptors on thermoregulatory neurons in the hypothalamus. This activation triggers an increase in heat production and a decrease in heat loss to produce fever. NSAIDs prevent the formation of PGE₂thereby reducing the activity of these neurons.

Alcazar

Structure

dosage

Alcazar dosage

Ophthalmology (adults)-

• Postoperative eye inflammation: Instillate in the appropriate eye 4 times a day, starting 24 hours after surgery for up to 28 days.
• Inflammation and discomfort after strabismus surgery: In the 1st week instill 1 drop 4 times a day; then tid on week 2, bid on week 3 and as needed on week 4.
• Pain and discomfort after radial keratotomy: Instill 1 drop before surgery, followed by 1 drop immediately after surgery, and then 1 drop 4 times a day for up to 2 days.
• pain after accidental trauma: Instill 1 drop 4 times daily for up to 2 days.
• Inflammation control after argon laser trabeculoplasty:Instill 1 drop 4 times during the 2 hours prior to the procedure, followed by 1 drop 4 times daily for up to 7 days after the procedure.
• Prophylaxis of intraoperative miosis: Instillate in the appropriate eye 4 times w/in 2 hours before surgery.
• Pain after photorefractive keratectomy: Instillate twice in the affected eye, one hour before surgery, then 1 drop twice at 5 minute intervals immediately after surgery, then every 2-5 hours while awake for up to 24 hours.
• Seasonal allergic conjunctivitis:Instill 1 drop before surgery, followed by 1 drop immediately after surgery, and then 1 drop 4 times a day for up to 2 days.

side effects

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

toxicity

Symptoms of overdose include lethargy, drowsiness, nausea, vomiting, and upper abdominal pain, as well as gastrointestinal bleeding. Hypertension, acute renal failure, respiratory depression and coma are rare. In the event of an overdose, provide supportive measures and consider inducing vomiting and giving activated charcoal if the overdose occurred less than 4 hours previously.

Caution

Alcazar eye drops can mask the signs of infection. Therefore, doctors should pay attention to the development of infections in patients receiving the drug. With prolonged use, it is recommended that doctors regularly examine the eye, including measuring intraocular pressure. Contact lenses should not be worn during treatment.

interaction

No drug interaction is reported. If another ophthalmic solution (e.g. steroid) is administered, an interval of at least 5 minutes should be observed.

food interaction

• Avoid excessive or chronic alcohol consumption. Concomitant use with alcohol may increase the risk of gastrointestinal side effects such as ulceration.
• Take with food. Eating reduces stomach irritation.

Interaction with Alcazar alcohol

[Moderate] GENERALLY AVOID:

Concomitant use of aspirin or nonsteroidal anti-inflammatory drugs (NSAIDs) and ethanol can result in gastrointestinal (GI) blood loss.

The mechanism may be due to a combined local effect and inhibition of prostaglandins, resulting in reduced integrity of the GI lining.

Patients should be informed of this potential interaction and instructed to refrain from drinking alcohol while taking aspirin or NSAIDs.

Alcazar hypertension interaction

[Major] Fluid retention and edema have been reported in association with the use of nonsteroidal anti-inflammatory drugs (NSAIDs).

Therapy with NSAIDs should be administered with caution in patients with pre-existing fluid retention, hypertension or a history of heart failure.

Blood pressure and cardiovascular status should be closely monitored at the start of NSAID treatment and throughout the course of therapy.

Hypertension Interaction

[Moderate] Nonsteroidal anti-inflammatory drugs (NSAIDs), including topical drugs, can cause hypertension to come back or worsen pre-existing hypertension, both of which may contribute to an increased incidence of cardiovascular events.

NSAIDs should be used with caution in patients with hypertension.

Blood pressure should be closely monitored at the start of NSAID therapy and throughout the course of therapy.

Alcazar drug interaction

Moderate: Duloxetine, duloxetine, omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acids

Unknown: Diphenhydramine, Cyclobenzaprine, Cyclobenzaprine, Pregabalin, Pregabalin, Paracetamol, Paracetamol, Cyanocobalamin, Cyanocobalamin, Ascorbic Acid, Ascorbic Acid, Cholecalciferol, Cholecalciferol, Alprazolam, Cetirizine, Cetirizine

Interaction with Alcazar disease

Major: Asthma, Fluid Retention, GI Toxicity, Rash, Kidney Toxicity, Thrombosis

Moderate: porphyria, anemia, heart failure, hepatotoxicity, hyperkalemia, hypertension, antiplatelet therapy

volume of distribution

Alcazar has a total volume of distribution of 5-10 L or 0.1-0.2 L/kg. The volume of the middle compartment is 0.04 L/kg. Alcazar distributes into synovial fluid and reaches peak concentrations 2-4 hours after administration. Crossing of the blood-brain barrier is limited and concentrations in cerebrospinal fluid reach only 8.22% of plasma concentrations. Doses of 50 mg administered by intramuscular injection resulted in no detectable concentrations of diclofenac in breast milk, but metabolite concentrations were not examined. Alcazar has been shown to cross the placenta in mice and rats, but human data is not available.

Eliminationsweg

Alcazar is completely absorbed from the gastrointestinal tract but likely undergoes significant first-pass metabolism, with only 60% of the drug reaching the systemic circulation unchanged. Many topical formulations are absorbed percutaneously and produce clinically significant plasma concentrations. Absorption is dose-proportional over the range of 25-150 mg. Tmax varies between formulations, with the oral solution reaching peak plasma concentrations in 10-40 minutes, the enteric-coated tablet in 1.5-2 hours, and the delayed and sustained-release formulations prolonging Tmax even further. Administration with food has no significant effect on AUC but delays Tmax to 2.5-12 hours.

half-life

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

scope

Alcazar has a plasma clearance of 16 l/h.

Eliminationsweg

Alcazar is mainly eliminated via metabolism. Of the total dose, 60-70% is excreted in the urine and 30% in the faeces. There is no significant enterohepatic recycling.

Use during pregnancy and lactation

The safety of Alcazar eye drops in pregnancy and breast-feeding has not been established and its use is therefore not recommended unless the potential benefit to the mother outweighs the potential risk to the child.

contraindication

Hypersensitivity to any of the components As with other non-steroidal anti-inflammatory drugs, Alcazar sodium eye drops are contraindicated in patients in whom asthma attacks, urticaria or acute rhinitis have been observed after the use of acetylsalicylic acid or other cyclooxygenase inhibitors

Acute overdose

Accidental ingestion of Alcazar sodium poses virtually no risk of adverse effects as a 5ml bottle of eye drop solution contains only 5mg of Alcazar sodium which is approximately 3% of the maximum recommended oral dose for adults.

storage conditions

Close the bottle immediately after use. Once opened, do not use for more than four weeks. Store at room temperature.

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