Nofebril Actions

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How do you administer this medicine?
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Actions of Nofebril 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: Nofebril pharmacokinetics is linear up to 2 g after single administration and after repeated administration during 24 hrs. The maximal plasma concentration (Cmax) of Nofebril 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 Nofebril is approximately 1 L/kg.

Nofebril is not extensively bound to plasma proteins.

Following infusion of 1 to plasma proteins of Nofebril (about 1.5 mcg/mL) were observed in the cerebrospinal fluid at and after the 20th min following infusion.

Metabolism: Nofebril 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 Nofebril 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 Nofebril 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 Nofebril 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 Nofebril 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 Nofebril is not modified in elderly subjects. No dose adjustment is required in this population.

Nofebril 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.

Nofebril 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. Nofebril 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. Nofebril'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. Nofebril 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. Nofebril may also inhibit formation of the platelet aggregation inhibitor prostacyclin (prostaglandin I2) in blood vessels; however, this action is reversible.


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Information checked by Dr. Sachin Kumar, MD Pharmacology

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