Diclac ID Actions

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Actions of Diclac ID in details

The action of the drug on the human body is called Pharmacodynamics in Medical terminology. To produce its effect and to change the pathological process that is happening the body and to reduce the symptom or cure the disease, the medicine has to function in a specific way. The changes it does to the body at cellular level gives the desired result of treating a disease. Drugs act by stimulating or inhibiting a receptor or an enzyme or a protein most of the times. Medications are produced in such a way that the ingredients target the specific site and bring about chemical changes in the body that can stop or reverse the chemical reaction which is causing the disease.
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Percutaneous anti-inflammatory agent.

Diclac ID is an anti-inflammatory and analgesic preparation for topical application. Its active substance corresponds to 1% Diclac ID sodium. The white, creamy, non-greasy preparation is easy to rub into the skin, and its aqueous-alcoholic base gives it a soothing and cooling effect.

Diclac ID has been shown in experiments to inhibit prostaglandin biosynthesis and this is regarded as an important factor in its mechanism of action.

In inflammation of traumatic or rheumatic origin, Diclac ID has been shown to relieve pain, reduce oedema and shorten the time to return of normal function.

Pharmacokinetics: Absorption: The amount of Diclac ID absorbed through the skin is proportional to the contact time and skin area covered with Diclac ID and depends on the total topical dose and on skin hydration. About 6% of the active substance is absorbed after topical application of Diclac ID 2.5 g/500 cm2, as determined by reference to total renal elimination compared with Voltaren tablets. Absorption of Diclac ID increases 3-fold if an occlusive dressing is applied for 10 hrs.

Distribution: Diclac ID can be detected in the plasma, synovial tissue and synovial fluid after topical application of Diclac ID to the wrists and knees. Peak plasma concentrations of Diclac ID are about 100 times lower after topical application of Diclac ID than after oral administration of Voltaren tablet. 99.7% of Diclac ID binds to serum proteins, mainly to albumin (99.4%).

Metabolism: Biotransformation of Diclac ID takes place partly by glucuronidation of the intact molecule, but mainly by single or multiple hydroxylation resulting in several phenolic metabolites, most of which are converted to glucuronide conjugates. Two of these phenolic metabolites are biologically active, but to a much lesser extent than Diclac ID.

Elimination: Total systemic clearance of Diclac ID from the plasma is 263 ± 56 mL/min (mean value ± standard deviation). The terminal plasma half-life is 1-2 hrs. Four of the metabolites, including the 2 active metabolites, also have a short plasma half-life (1-3 hrs). One metabolite, 3'-hydroxy-4'-methoxy-Diclac ID, has a much longer half-life, but this metabolite is virtually inactive.

Diclac ID and its metabolites are excreted mainly in the urine.

Kinetics in Special Clinical Situations: No accumulation of Diclac ID and its metabolites should occur in patients with renal insufficiency.

In patients with chronic hepatitis or nondecompensated liver cirrhosis, the kinetics and metabolism of Diclac ID are the same as in patients without liver disease.

How should I take Diclac ID?

Keep using Diclac ID for the full time of treatment. However, do not use Diclac ID more often or for a longer time than your doctor ordered. Diclac ID is not for long-term use.

Diclac ID should come with a Medication Guide. Read and follow these instructions carefully. Ask your doctor if you have any questions.

When used for severe or continuing arthritis, Diclac ID must be taken every day as ordered by your doctor in order for it to help you. Diclac ID usually begins to work within one week, but in severe cases up to two weeks or longer may pass before you begin to feel better. Several weeks may pass before you feel the full effects of Diclac ID.

You may take Diclac ID with or without food. However, Diclac ID capsules should be taken on an empty stomach.

To use the oral solution:

  • Open the packet of medicine right before you use it.
  • Empty the contents of the packet into a cup with 1 to 2 ounces (30 to 60 milliliters [mL]) of water. Do not use any liquid other than water for mixing the medicine.
  • Mix well and drink it immediately on an empty stomach.

Use only the brand of Diclac ID that your doctor prescribed. Different brands may not work the same way.

Dosing

The dose of Diclac ID will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of Diclac ID. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

  • For oral dosage form (capsules):
    • For acute pain:
      • Adults—18 or 35 milligrams (mg) three times a day.
      • Children—Use and dose must be determined by your doctor.
    • For osteoarthritis:
      • Adults—35 milligrams (mg) three times a day.
      • Children—Use and dose must be determined by your doctor.
  • For oral dosage forms (delayed-release tablets, enteric-coated tablets):
    • For ankylosing spondylitis:
      • Adults—25 milligrams (mg) four times a day, with an extra 25 mg dose at bedtime if necessary.
      • Children—Use and dose must be determined by your doctor.
    • For osteoarthritis:
      • Adults—50 milligrams (mg) two or three times a day, or 75 mg two times a day.
      • Children—Use and dose must be determined by your doctor.
    • For rheumatoid arthritis:
      • Adults—50 milligrams (mg) three or four times a day, or 75 mg two times a day.
      • Children—Use and dose must be determined by your doctor.
  • For oral dosage form (immediate-release tablets):
    • For osteoarthritis:
      • Adults—50 milligrams (mg) two or three times a day.
      • Children—Use and dose must be determined by your doctor.
    • For pain or menstrual cramps:
      • Adults—50 milligrams (mg) three times a day. Your doctor may direct you to take 100 mg for the first dose only.
      • Children—Use and dose must be determined by your doctor.
    • For rheumatoid arthritis:
      • Adults—50 milligrams (mg) three or four times a day.
      • Children—Use and dose must be determined by your doctor.
  • For oral dosage form (solution):
    • For migraine headaches:
      • Adults—One packet (50 milligrams) as a single, one time dose.
      • Children—Use and dose must be determined by your doctor.

Missed Dose

If you miss a dose of Diclac ID, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Diclac ID administration

Administration of drug is important to know because the drug absorption and action varies depending on the route and time of administration of the drug. A medicine is prescribed before meals or after meals or along with meals. The specific timing of the drug intake about food is to increase its absorption and thus its efficacy. Few work well when taken in empty stomach and few medications need to be taken 1 or 2 hrs after the meal. A drug can be in the form of a tablet, a capsule which is the oral route of administration and the same can be in IV form which is used in specific cases. Other forms of drug administration can be a suppository in anal route or an inhalation route.
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Take exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.

If you switch brands of Diclac ID, your dose needs may change. Follow your doctor's instructions about how much medicine to take.

Do not crush, chew, or break an extended-release tablet. Swallow it whole. Breaking the pill may cause too much of the drug to be released at one time.

Dissolve the Diclac ID powder (Diclac ID) with 1 to 2 ounces of water. Do not use any other type of liquid. Stir this mixture and drink all of it right away. Diclac ID powder works best if you take it on an empty stomach.

Call your doctor if your headache does not completely go away after taking Diclac ID. Do not take a second dose of Diclac ID powder without your doctor's advice.

Do not crush, chew, or break an enteric-coated pill. Swallow the pill whole. The enteric-coated pill has a special coating to protect your stomach. Breaking the pill could damage this coating.

If you use this medication long-term, your liver function will need to be checked with frequent blood tests. Visit your doctor regularly.

Store at room temperature away from moisture and heat.

Diclac ID pharmacology

Pharmacokinetics of a drug can be defined as what body does to the drug after it is taken. The therapeutic result of the medicine depends upon the Pharmacokinetics of the drug. It deals with the time taken for the drug to be absorbed, metabolized, the process and chemical reactions involved in metabolism and about the excretion of the drug. All these factors are essential to deciding on the efficacy of the drug. Based on these pharmacokinetic principles, the ingredients, the Pharmaceutical company decides dose and route of administration. The concentration of the drug at the site of action which is proportional to therapeutic result inside the body depends on various pharmacokinetic reactions that occur in the body.
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Mechanism of Action

Diclac ID has analgesic, anti-inflammatory, and antipyretic properties.

The mechanism of action of Diclac ID, like that of other NSAIDs, is not completely understood but involves inhibition of cyclooxygenase (COX-1 and COX-2).

Diclac ID is a potent inhibitor of prostaglandin synthesis in vitro. Diclac ID concentrations reached during therapy have produced in vivo effects. Prostaglandins sensitize afferent nerves and potentiate the action of bradykinin in inducing pain in animal models. Prostaglandins are mediators of inflammation. Because Diclac ID is an inhibitor of prostaglandin synthesis, its mode of action may be due to a decrease of prostaglandins in peripheral tissues.

Pharmacokinetics

The relative bioavailability of Diclac ID 35 mg capsules was compared to Diclac ID potassium immediate-release (IR) tablets 50 mg in 39 healthy subjects under fasted and fed conditions in a single-dose crossover study.

Diclac ID 35 mg capsules do not result in an equivalent systemic exposure to 50 mg Diclac ID potassium IR tablets.

When taken under fasted conditions, a 20% lower dose of Diclac ID in Diclac ID capsules resulted in a 23% lower mean systemic exposure (AUCinf) and a 26% lower mean peak concentration (Cmax) compared to Diclac ID potassium IR tablets. The time to reach peak concentration (Tmax) was similar for Diclac ID and Diclac ID potassium IR tablets and was ~1 hour for both.

When taken under fed conditions, a 20% lower dose of Diclac ID in Diclac ID capsules resulted in a 23% lower mean systemic exposure (AUCinf) and a 48% lower mean Cmax compared to Diclac ID potassium IR tablets. The Tmax for Diclac ID was delayed by approximately 1 hour compared to Diclac ID potassium IR tablets (3.32 hours vs. 2.33 hours, respectively).

When taken under fed conditions, Diclac ID capsules resulted in an 11% lower mean systemic exposure (AUCinf) and a 60% lower mean Cmax compared to fasted conditions. Whereas Diclac ID potassium IR tablets under fed conditions resulted in 8% - 10% lower mean systemic exposure (AUCinf) and 28% - 43% lower mean Cmax compared to fasted conditions, based on the results from two individual food effect studies. The Tmax for Diclac ID was delayed by approximately 2.32 hours under fed conditions compared to fasted conditions (3.32 hours vs. 1.00 hour, respectively), while the Tmax for Diclac ID potassium IR tablets was delayed by approximately 1.00 - 1.33 hours under fed conditions compared to fasted conditions (1.70 vs. 0.74 hours and 2.33 vs. 1.00 hours, respectively in two studies).

There were no differences in elimination half-life between Diclac ID and Diclac ID potassium IR tablets under fasted or fed conditions.

Absorption

Diclac ID is 100% absorbed after oral administration compared to IV administration as measured by urine recovery. However, due to first-pass metabolism, only about 50% of the absorbed dose is systemically available. After repeated oral administration, no accumulation of Diclac ID in plasma occurred.

Administration of Diclac ID capsules 18 mg and 35 mg was associated with dose proportional pharmacokinetics.

Taking Diclac ID with food causes a significant decrease in the rate but not the overall extent of systemic absorption of Diclac ID compared with taking Diclac ID on an empty stomach. Diclac ID capsules results in 60% lower Cmax, 11% lower AUCinf, and 2.32 hours delayed Tmax (1.0 hour during fasted versus 3.32 hours during fed) under the fed condition compared to the fasted condition. The effectiveness of Diclac ID when taken with food has not been studied in clinical studies. The decreased Cmax may be associated with decreased effectiveness. Taking Diclac ID with food may cause a reduction in effectiveness compared to taking Diclac ID on an empty stomach.

Distribution

The apparent volume of distribution (V/F) of Diclac ID potassium is 1.3 L/kg. Diclac ID is more than 99% bound to human serum proteins, primarily to albumin. Serum protein binding is constant over the concentration range (0.15-105 mg/mL) achieved with recommended doses.

Diclac ID diffuses into and out of the synovial fluid. Diffusion into the joint occurs when plasma levels are higher than those in the synovial fluid, after which the process reverses and synovial fluid levels are higher than plasma levels. It is not known whether diffusion into the joint plays a role in the effectiveness of Diclac ID.

Elimination

Diclac ID is eliminated through metabolism and subsequent urinary and biliary excretion of the glucuronide and the sulfate conjugates of the metabolites. The terminal half-life of unchanged Diclac ID is approximately 2 hours.

Metabolism

Five Diclac ID metabolites have been identified in human plasma and urine. The metabolites include 4'-hydroxy-, 5-hydroxy-, 3'-hydroxy-, 4',5-dihydroxy- and 3'-hydroxy-4'-methoxy Diclac ID. The major Diclac ID metabolite, 4'-hydroxy-Diclac ID, has very weak pharmacologic activity. The formation of 4'-hydroxy-Diclac ID is primarily mediated by CYP2C9. Both Diclac ID and its oxidative metabolites undergo glucuronidation or sulfation followed by biliary excretion. Acylglucuronidation mediated by UGT2B7 and oxidation mediated by CYP2C8 may also play a role in Diclac ID metabolism. CYP3A4 is responsible for the formation of minor metabolites, 5-hydroxy and 3'-hydroxy-Diclac ID. In patients with renal dysfunction, peak concentrations of metabolites 4'-hydroxy and 5-hydroxy-Diclac ID were approximately 50% and 4% of the parent compound after single oral dosing compared to 27% and 1% in normal healthy subjects.

Excretion

Diclac ID is eliminated through metabolism and subsequent urinary and biliary excretion of the glucuronide and the sulfate conjugates of the metabolites. Little or no free unchanged Diclac ID is excreted in the urine. Approximately 65% of the dose is excreted in the urine, and approximately 35% in the bile as conjugates of unchanged Diclac ID plus metabolites. Because renal elimination is not a significant pathway of elimination for unchanged Diclac ID, dosing adjustment in patients with mild to moderate renal dysfunction is not necessary. The terminal half-life of unchanged Diclac ID is approximately 2 hours.

Specific Populations

Pediatric: The pharmacokinetics of Diclac ID has not been investigated in pediatric patients.

Race: Pharmacokinetic differences due to race/ethnicity have not been identified.

Hepatic Impairment: No dedicated Diclac ID pharmacokinetics studies in patients with hepatic impairment were conducted. Hepatic metabolism accounts for almost 100% of Diclac ID elimination. Therefore, in patients with hepatic impairment, start with the lowest dose and if efficacy is not achieved, consider use of an alternate product.

Renal Impairment: Diclac ID pharmacokinetics has been investigated in subjects with renal insufficiency. No differences in the pharmacokinetics of Diclac ID have been detected in studies of patients with renal impairment. In patients with renal impairment (inulin clearance 60-90, 30-60, and less than 30 mL/min; N=6 in each group), AUC values and elimination rate were comparable to those in healthy subjects.

Drug Interaction Studies

Aspirin: When NSAIDs were administered with aspirin, the protein binding of NSAIDs were reduced, although the clearance of free NSAID was not altered. The clinical significance of this interaction is not known. See Table 4 for clinically significant drug interactions of NSAIDs with aspirin.



References

  1. DailyMed. "DICLOFENAC EPOLAMINE: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
  2. NCIt. "Diclofenac: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).
  3. EPA DSStox. "Diclofenac: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).

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