Research Paper on Nalfon Drug

Introduction

Nalfon drug refers to a non-steroidal anti-inflammatory drug used to treat arthritis, or sometimes used for antipyretic and analgesic activities. Nalfon is otherwise known as fenoprofen drug due to the amount of fenoprofen calcium that it contains, which acts as a dehydrate within the drug. Although the exact action of Nalfon is still unknown, it is thought to deliver pain relief by inhibiting the secretion of prostaglandin synthetase, a chemical in the body that potentiates pain induction in the body. Fenoprofen has been proven to have both anti-inflammatory and analgesic actions from demonstrations by the human body. Similar to other drugs such as aspirin and indomethacin, Nalfon demonstrates antierthemic activities when ingested. The drug induces pain relief, increases grip strength, reduces swelling of the joints, induces a decrease in the length of morning rigidity, and disease action among patients who present with rheumatoid arthritis. Other anti-inflammatory actions by the drug present in the form of increased mobility among arthritic patients by decreasing the number of joints that experience limited motions in the patients.

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The use of Nalfon together with corticosteroids or gold salts has been studied in patients who present with rheumatoid arthritis. However, the studies are still inadequate in trying to demonstrate whether there are further improvements obtained by the addition of the drug in the maintenance therapy using steroids or gold salts. The research still comes short at explaining whether the addition of Nalfon to partially effective doses of corticosteroid spares the steroid usage. However, the anti-inflammatory and analgesic effect of Nalfon in patients with osteoarthritis, on the other hand, have been effective in itself, presenting in the form of reduction of tenderness in response to pressure, reduced night pain, decrease in stiffness, swelling, and overall disease activity. The effects are further felt with the increased range of motion in the affected joints.

Use of Nalfon and Producing Company

In general, Nalfon and aspirin have similar effects when taken by patients suffering from either rheumatoid arthritis or osteoarthritis; a patient who uses either drug, Nalfon or Aspirin, would experience anti-inflammatory pain relief. However, patients who use Nalfon often experience mild gastrointestinal reactions such as nausea and dyspepsia than those patients who use aspirin for similar pain relief.

Nalfon drug is manufactured by various companies such as Pedinol Pharmacal Inc. located in Farmingdale in New York City in the United States. The production is supported by Ohm Laboratories Inc. that is located in North Brunswick, New Jersey in the United States. Other manufacturers include Eli Lilly and Co, which has their headquarters in Lilly Corporate Center in Indianapolis, Indiana. Their manufacture is supported by Tippecanoe Laboratories in Lilly Road production site in Lafayette in Indiana.

History of the Drug

The development of Nalfon came as a result of drug repositioning to minimize rising timeframes, cost and to recover success rates in recognition of new indications for older medication. From the time of screening on potential positive allosteric modulators, fenoprofen has come out as a definite hit, long recognized for its activities against arthritis. The drug came out as one of the new medication for obesity with a minimized profile of side effects. Compound libraries that contain approved medicines offer a chance for possible new uses of current drugs, hence the development of fenoprofen to counter rheumatic arthritis and osteoarthritis. The production of the drug, however, has been protected by use of patents, with little information about production procedures publicized. The latest patent for the drug production was submitted under the title Crystalline Pharmaceutical and Methods of Preparation and Use Thereof, which was filed in September 2014 and was granted in August 2015

Molecular Formula of Active Pharmaceutical Ingredient

Nalfon drug presents as a white crystalline powder. Its structural formula consists of Benzeneatic acid, alpha-methyl-3-phenoxy-calcium salt dehydrate. Its structural formula is written as, which represents a molecular weight of 558.65 g/mol. The drug is often packaged in 200mg or 400mg capsules. The 200mg capsule usually contains fenoprofen calcium, which is equivalent to 200mg or 0.826mmol, as dehydrate. The 400mg tablet, on the other hand, often contains fenoprofen calcium, which is equivalent to 400mg or 1.65mmol, as dehydrate. The formula, however, remains slightly similar for both the 200mg and the 400mg capsules, with fenoprofen calcium as the common ingredient.

Chemical Action of Active Pharmaceutical Ingredient

The positive allosteric modulator activity of fenoprofen is generally non-receptor and non-probe selective (Yuan, 2018). The figures below show results obtained after testing fenoprofen's allosteric modulatory activity at the human melanocortin receptors (Yuan, 2018).

Figure 1: Representation of Nalfon chemical action in different concentrations

A study to address if melanocortin (MC) receptor for positive allosteric modulator (PAM) activities featured commonly in cyclooxygenase (COX) inhibitors tested seven cyclooxygenase inhibitors, with a focus on seven NSAID drugs. Table 1 below represents the positive allosteric modulator activities of fenoprofen at melanocortin receptors with the values of log shift of the peptide ligand and EC50 recorded at both murine MC3 and human MC3,4,5 receptors(Yuan, 2018).

From the results recorded in Table 1 above, of the seven drugs tested, non-potentiated cAMP production induced by melanocortin except fenoprofen. The translation, therefore, is that apart from fenoprofen, the physiochemical and structural requirements for COX inhibitors don't translate to PAM activity. Nalfon drug is thought to perform pain relief activities by inhibiting the secretion of prostaglandin and hence stopping pain induction in the animal body. The figure below shows the path used by Nalfon drug to relieve pain, from entry through the cell membrane to inhibition of prostaglandin to suppress pain.

Figure 2: Representation of prostaglandin inhibition by Nalfon in the body

Physical Properties

Nalfon drug comes in two types of capsules; the 200 mg and the 400mg pill. The 200mg tablet usually contains 0.826mmol of fenoprofen calcium while the 400mg capsule contains 1.65mmol of fenoprofen calcium. Apart from fenoprofen calcium, the 200mg capsule also contains silicone, gelatin, titanium dioxide, cellulose, and other iron oxides (Shea, 2018). The 400mg capsule, on the other hand, contains gelatin, iron II oxide, titanium dioxide, magnesium stearate, talc, and sodium lauryl Sulphate (Shea, 2018). The combination of chemicals in Nalfon drug adds up to a molecular weight of 242.274 g/mol. At room temperature, fenoprofen can dissolve to a 15mg/ml in 95% alcohol solution. The drug is slightly soluble in water. However, it is quite insoluble in benzene. The formulation has a boiling point of between 168 and 171 degrees Celsius at 0.11 mmHg of pressure.

Crystallization Properties of Active Pharmaceutical Ingredient

Nalfon drug has one hydrogen bond donor account, three hydrogen bond acceptor counts and a rotatable bond count of four. The property value of the complexity of Nalfon is 271 and a topographical polar surface area of 46.5 A squared. Its monoisotopic mass is approximately 242.094 g/mol, making up its exact mass. The compound is canonicalized with a heavy atom count of 18 and an undefined atom stereocenter count of one.

Administration Routes and Dosage Forms

It is essential for patients, who intend to use Nalfon drug to consider the potential risks and benefits first before deciding to commence its usage. It is also important that patients on Nalfon drugs use the lowest doses that are effective, and use the drug for the briefest time possible, in coherence with the medication goals for individual patients. The frequency and dosage of administration should be regulated considering the response to the initial therapy of a patient with the drug. The adjustment, therefore, should be to match the needs of individual patients.

For patients who intend to use Nalfon for analgesia, it is recommended that they use the dosage of 200mg. The doses should be administered orally every 4 to 6 hours as per the requirements. For patients who use the drug to alleviate signs and symptoms of rheumatoid arthritis or osteoarthritis, the recommended dosage is between 400mg and 600mg (Deepthi, 2018). The doses should also be administered orally, 3 to 4 times a day. The dosage, however, should always be tailored according to the patient's needs. Some patients will require that the dosage is increased while others will expect that the dosage is decreased according to how severe the symptoms present. The adjustment of dosage can always be made during initiation of drug therapy or during the exacerbation of the illness. However, the total dosage for a day should not exceed 3200mg of the drug.

Nalfon dug can always be administered with meals or with milk. Either way, the total amount absorbed does not get affected. However, the peak blood levels of the drug are delayed or diminished. It is highly recommended that the tiniest dose of the drug that provides desirable results be used at all times during the usage (Yuan, 2018). Patients using Nalfon drug will often require varying doses. For instance, patients suffering from osteoarthritis will usually need fewer treatments compared to those who have rheumatoid arthritis. The full benefits of the drug can be noticed after two to three weeks although improvements can always be seen in a few days of using the drug.

Patients using Nalfon drugs, and other Non-Steroidal Anti-Inflammatory Drugs (NSAIDs), require to be made aware that the drugs may elevate the chances of a stroke or a heart attack, which may be fatal (Yuan, 2018). The possibilities, however, increase with prolonged use of the drugs or use by patients who have heart diseases. It is, therefore, best if a patient refrains from using NSAID drugs right after heart surgery, otherwise known as Coronary Artery Bypass Graft (CABG) (Yuan, 2018). Nalfon and other NSAID drugs can also cause bleeding in intestinal organs and ulcers. The cause of bleeding in the intestines can, however, occur without warning symptoms and may be fatal. The chances of a patient getting ulcers or developing bleeding in the stomach may increase with taking corticosteroids and anticoagulants (Yuan, 2018). Other reasons for developing bleeding in the intestines may be due to more prolonged use of Nalfon, smoking, drinking alcohol, having poor health or being of older age. Therefore, Nalfon and other NSAIDs should only be used as prescribed for the shortest period necessary and the doses used should be as low as possible to give the desired results.

It is essential for patients to share, with their health care providers, their medical conditions, the medicines that they take, their pregnancy status and if they are breastfeeding. Patients who have experienced asthma attacks or those who have allergic reacti...