Actions of Aceclofenac (Fortaflam PLUS) 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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Pharmacology:Aceclofenac (Fortaflam PLUS) is a nonsteroidal agent with marked anti-inflammatory and analgesic properties. It has higher anti-inflammatory action than conventional NSAIDs and is a cytokine inhibitor. The mode of action of Aceclofenac (Fortaflam PLUS) is largely based on the inhibition of prostaglandin synthesis. Aceclofenac (Fortaflam PLUS) is a potent inhibitor of the enzyme cyclooxygenase, inflammatory cytokines interleukin IL1, tumor necrosis factor and prostaglandins E2. Cyclooxygenase is involved in the production of prostaglandins (chemicals in the body) which cause pain, swelling and inflammation.
Pharmacokinetics: After oral administration, Aceclofenac (Fortaflam PLUS) is rapidly and completely absorbed as unchanged drug. Peak plasma concentrations are reached approximately 1-3 hrs following ingestion. Aceclofenac (Fortaflam PLUS) is highly protein bound (>99%). Aceclofenac (Fortaflam PLUS) penetrates into the synovial fluid, where the concentrations reach approximately 57% of those in plasma. The volume of distribution is approximately 25 L. The mean plasma elimination t½ is around 4 hrs. Aceclofenac (Fortaflam PLUS) is metabolized to a major metabolite 4'-hydroxyaceclofenac and other metabolites 5 hydroxyaceclofenac, 4'-hydroxydiclofenac, diclofenac and 5 hydroxydiclofenac.
Approximately 2/3 of the administered dose is excreted via the urine, mainly as hydroxymetabolites. No changes in the pharmacokinetics of Aceclofenac (Fortaflam PLUS) have been detected in the elderly.
Aceclofenac (Fortaflam PLUS) 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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Should be taken with food. Take w/ or immediately after meals.
Aceclofenac (Fortaflam PLUS) 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.
After intake is absorbed from the gastrointestinal tract. Eating slows down the rate of absorption, extent of absorption is not changed. About 50% of the active substance is metabolized in the "first passage" through the liver. When used rectally absorption is slower. Time to reach Cmax in plasma after oral administration is 2-4 hours depending on the used dosage form, after rectal - 1 h, I.M. administration - 20 min. The concentration of active substance in plasma is a linear function of the applied dose.
Not cumulative. Plasma protein binding is 99.7% (predominantly albumin). Penetrates into synovial fluid, Cmax is achieved in 2-4 hours later than in plasma.
To a large extent metabolized to form several metabolites, among which two pharmacologically active, but to a lesser extent than diclofenac.
Systemic clearance of the active substance is about 263 ml / min. T1/2 from plasma is 1-2 h, from synovial fluid - 3-6 h. Approximately 60% of the dose was excreted as metabolites by the kidneys, less than 1% excreted in the urine as unchanged, while the rest is displayed in the form of metabolites with bile.
Actions of Paracetamol (Fortaflam PLUS) 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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Pharmacology:Pharmacokinetics:Absorption:Paracetamol (Fortaflam PLUS) pharmacokinetics is linear up to 2 g after single administration and after repeated administration during 24 hrs. The maximal plasma concentration (Cmax) of Paracetamol (Fortaflam PLUS) is observed at the end of 15 min.
Intravenous infusion of 500 mg and 1 g is about 15 mcg/mL and 30 mcg/mL, respectively.
Distribution: The volume of distribution of Paracetamol (Fortaflam PLUS) is approximately 1 L/kg.
Paracetamol (Fortaflam PLUS) is not extensively bound to plasma proteins.
Following infusion of 1 to plasma proteins of Paracetamol (Fortaflam PLUS) (about 1.5 mcg/mL) were observed in the cerebrospinal fluid at and after the 20th min following infusion.
Metabolism: Paracetamol (Fortaflam PLUS) is metabolised mainly in the liver following 2 major hepatic pathways: Glucuronic acid conjugation and sulphuric acid conjugation. The latter route is rapidly saturable at doses that exceed the therapeutic doses. A small fraction (<4%) is metabolised by cytochrome P450 to a reactive intermediate (N-acetyl benzoquinone imine), which under normal conditions uses, is rapidly detoxified by reduced glutathione and eliminated in the urine after conjugation with cysteine and mercapturic acid. However, during massive overdosing, the quantity of this toxic metabolite is increased.
Elimination: The metabolites of Paracetamol (Fortaflam PLUS) are mainly excreted in the urine. Ninety percent (90%) of the dose administered is excreted within 24 hrs, mainly in glucuronide (60-80%) and sulphate (20-30%) conjugates. Less than 5% is eliminated unchanged. Plasma half-life (t½) is 2.7 hrs and total body clearance is 18 L/hr.
Special Population:Neonates, Infants and Children: The pharmacokinetic parameters of Paracetamol (Fortaflam PLUS) observed in infants and children are similar to those observed in adults, except for the plasma t½ that is slightly shorter (1.5-2 hrs) than in adults. In neonates, the plasma t½ is longer than in infants ie, around 3.5 hrs. Neonates, infants and children up to 10 years excrete significantly less glucuronide and more sulphate conjugates than adults.
Renal Insufficiency: In cases of severe renal impairment [creatinine clearance (CrCl) 10-30 mL/min), the elimination of Paracetamol (Fortaflam PLUS) is slightly delayed, the elimination t½ ranging from 2-5.3 hrs for the glucuronide and sulphate conjugates, the elimination rate is 3 times slower in subjects with severe renal impairment than in healthy subjects. Therefore, when giving Paracetamol (Fortaflam PLUS) to patients with severe renal impairment (CrCl 30 mL/min), the minimum interval between each administration should be increased to 6 hrs.
Elderly: The pharmacokinetics and the metabolism of Paracetamol (Fortaflam PLUS) is not modified in elderly subjects. No dose adjustment is required in this population.
Paracetamol (Fortaflam PLUS) 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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May be taken with or without food.
Paracetamol (Fortaflam PLUS) 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.
The analgesic, antipyretic, and anti-inflammatory effects of aspirin are due to actions by both the acetyl and the salicylate portions of the intact molecule as well as by the active salicylate metabolite. Paracetamol (Fortaflam PLUS) directly and irreversibly inhibits the activity of both types of cyclo-oxygenase (COX-1 and COX-2) to decrease the formation of precursors of prostaglandins and thromboxanes from arachidonic acid. This makes aspirin different from other NSAIDS (such as diclofenac and ibuprofen) which are reversible inhibitors. Salicylate may competitively inhibit prostaglandin formation. Paracetamol (Fortaflam PLUS)'s antirheumatic (nonsteroidal anti-inflammatory) actions are a result of its analgesic and anti-inflammatory mechanisms; the therapeutic effects are not due to pituitary-adrenal stimulation. The platelet aggregation–inhibiting effect of aspirin specifically involves the compound's ability to act as an acetyl donor to the platelet membrane; the nonacetylated salicylates have no clinically significant effect on platelet aggregation. Paracetamol (Fortaflam PLUS) affects platelet function by inhibiting the enzyme prostaglandin cyclooxygenase in platelets, thereby preventing the formation of the aggregating agent thromboxane A2. This action is irreversible; the effects persist for the life of the platelets exposed. Paracetamol (Fortaflam PLUS) may also inhibit formation of the platelet aggregation inhibitor prostacyclin (prostaglandin I2) in blood vessels; however, this action is reversible.
Actions of Serratiopeptidase (Fortaflam PLUS) 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.
Serratiopeptidase (Fortaflam PLUS) is an enzyme that acts by breaking down the chemical mediators that are involved in causing pain and inflammation, thereby reducing the pain and inflammation.
References
EPA DSStox. "Aceclofenac: 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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