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DECODING THE COMPREHENSIVE NOTE ABOUT A NSAID: IBUPROFEN





●     WHAT IS IBUPROFEN

Nonsteroidal anti-inflammatory drug (NSAID) class is that group which is used to treat pain, fever and other conditions and Ibuprofen is one synthetic drug which comes under this class. It is used to get rid of a plethora of illnesses such as chronic and acute discomfort, fever and inflammation. It also depicts positive action in the treatment of menstrual pain, rheumatoid arthritis, osteoarthritis, juvenile idiopathic arthritis. Besides its advantages, ibuprofen has many drawbacks too like it creates conditions on the liver, kidney and heart. Moreover, danger does not mean that it creates an issue of heart failure but one should maintain the dosage of ibuprofen and  always consult the doctor before taking it. There is one report from the World Health Organization's List of Essential Medicines which clearly depicts that ibuprofen is the most effective and safest drug in the healthcare system for the treatment of various diseases.

●      ENLIST THE PHYSICAL CHARACTERISTICS OF IBUPROFEN

Physical Profile

Descriptions

Molecular Formula

C13H18O2

IUPAC Name

(RS)-2-(4-(2-methylpropyl)phenyl)propanoic acid

Vapour Pressure

4.75*10-5mmHg@ 25°C

Molecular Weight

206.29 g/mole

Density

1.03 g/ml g/cm3

Boiling point

157°C

Melting point

75–78°C

Odor

Characteristic odor

Colour

Colourless

 

●      Explicate few Pharmacological aspects of Ibuprofen

1.     Ibuprofen is given in the form of tablets with the dose of 200 to 800 mg. The normal dose is 400 to 800 mg three times a day.

2.     Solubility of Ibuprofen is very low in water because its pKa is 5.3 but it is absorbed by oral route for better and most appropriate action attained in 2 hours.

3.     This drug is bio-transformed very instantly with a serum half life of 1.8 to 2 hours while exclusive elimination occurs in 24 hours.

4.     This drug is extensively metabolized from the liver and a very small amount remains unchanged.

5.     Displacement interactions are not significantly clinical because of high binding towards plasma proteins therefore no need to change the dose of oral coagulative and hypoglycemic agents.

6.     During the phase of oldsters there is no significant effect on the Excretion of ibuprofen from the body.

7.     The swallowing of tablets either in empty stomach conditions or immediately before food depicts quite the same serum concentrations-time profile.

HOW IBUPROFEN WORKS IN THE HUMAN BODY

This chemical initiates its work when the body transfers arachidonic acid to prostaglandin H2 with the assistance of cyclooxygenase (COX), an essential enzyme for the production of prostaglandin via arachidonic acid route. Suppression of COX, transfers thromboxane into arachidonic acid A2 which is an effective step in platelet accumulation and also results in the formation of blood clot. Moreover, when the maintenance of the gastric mucosa is altered, an over accumulation of NSAIDs may result in the long-term inhibition of COX-1, a subtype of COX that may induce gastric toxicity.

DEMYSTIFYING THE ROLE OF IBUPROFEN IN THE TREATMENT OF VARIOUS DISORDERS

Ibuprofen is the same as aspirin and paracetamol at low doses. It is mostly treated as an antipyretic, an analgesic and an anti inflammatory agent but Racemic ibuprofen and S(+) enantiomer are mostly used in the treatment of headache, pain related to dysmenorrhea, postoperative dental pain, migraine, osteoarthritis and rheumatoid arthritis.

●      Patent Ductus arterosus (PDA)

This is a type usually occur in premature children as indomethacin is the suitable prescribed drug  but the side effects of indomethacin and other few prostaglandins inhibitors such as ibuprofen have been notified for an effective curing of ductus arteriosus.

●      Rheumatoid and osteo-arthritis 

For the management of various rheumatic disorders, inflammation and musculoskeletal disorders they are highly effective along with low levels of toxicity. For example gouty arthritis is exclusively treated with Ibuprofen 2400 mg per day which results in fast improvement within 72 hours. In this current era Osteoarthritis is very common and treatment involves NSAIDs, particularly ibuprofen.

●      Orthostatic hypotension

Along with other NSAIDs Ibuprofen is also used in the management of extreme orthostatic hypotension. It shows toxicity at very low doses 100 mg/kg but proves to be dangerous for life above 400 mg/kg.

●      Dental pain

In the treatment of dental pain ibuprofen is very effective as dentists are mostly relying on this to manage acute as well as chronic pain such as the dose of 400 mg provides an effective treatment for the controlling of postoperative pain after molar surgery.

●      Dysmenorrhea, fever and headache

OTC ibuprofen is effective for the treatment of minor cramps and pains, reduction in the body temperature fever along with curing the symptoms of dysmenorrhea. Cyclooxygenase inhibitors mitigate the proportion of menstrual prostanoids released, with connected decrease in uterine hyper contractility. Over-the-counter (OTC) ibuprofen preparations are widely used for acute indications, such as fever or headaches. In many studies it has been reported that the combination of Ibuprofen with paracetamol reduces body fever very instantly.

●      Prophylaxis of Alzheimer disease

NSAIDs especially ibuprofen, when administered considerably decreased neurodegeneration. In many studies, when ibuprofen was administered in small doses over an extended period of time, it showed a placebo in terms of protecting Alzheimer's disease.

●      Parkinson’s disease

 Epidemiologic study depicted that continuous use of NSAIDs, especially non aspirin COX inhibitors such as ibuprofen lower the risk of Parkinson Diseases. It induces apoptosis in early and late stages, reflecting that these chemicals may reduce the microbial proliferation.

●      Breast cancer

With the continuous intake of Ibuprofen the ratio of breast cancer was decreased by approximately 50% and 40% with regular aspirin intake. One study depicted that these come under the list of effective chemotherapeutic agents.

ENLIST SOME COMPLICATIONS OCCUR WITH REGULAR USE OF IBUPROFEN

⮚     Allergic reactions

⮚     Disruption in stomach

⮚     Kidney problem

⮚     Hepatic problem

⮚     Skin rash

⮚     Acidity

⮚     Itching

⮚     Constipation

⮚     Extreme skin reactions

⮚     Heartburn

⮚     Loose motions

⮚     Feeling tired

⮚     Liver problems

ELABORATE ABOUT THE REACTIONS TAKES PLACE DURING ADMINISTRATION OF IBUPROFEN

❖     Food Drug Interaction

When ibuprofen and oxycodone are prescribed in the combination the tablet was affected with the association in taking of food whereas the swallowing of single drug did not affect the rate of absorption. One research was performed to evaluate the effect of food on the plasma concentration-time profile of sustained release dosage form after a night fasting or in addition with a heavy vegetarian breakfast and result showed various peaks on the plasma concentration time curve. The bioavailability of ibuprofen is not affected by food but there was a statistically considerable elevation in the mean concentration. Garba et al performed a study reflecting that the bioavailability of Ibuprofen increased significantly with the extract of Tamarindus indica fruit.

❖     Drug-Drug Interaction

This drug established interactions with NSAIDs which are possible in both pharmacodynamic and pharmacokinetic. The most potent interactions include the usage of NSAIDs with warfarin, lithium, glycemic agents, high dose methotrexate antihypertensive, ß-blockers and diuretics. When these medications are administered concurrently, careful monitoring can sometimes minimize adverse occurrences. There are a plethora of studies and experiments on animals which depicted those cardiac protection effects of swallowing the aspirin are blocked by ibuprofen which exclusively suppresses the aspirin’s binding sites on platelets. In 2003 Palmer et al. showed that NSAIDs interact with few drugs of hypertension while Ibuprofen depicts a considerable increase in systolic and diastolic blood pressure. Like other NSAIDs, ibuprofen also mitigates the diuretic and anti hypertensive actions of Furosemide and ß-Blockers.

 

WHAT ARE SOME SAFETY MEASURES WHILE TAKING A DOSE OF IBUPROFEN 

❖     Consult with the registered medical practitioner before taking this.

❖     Avoid taking alcohol to prevent from bleeding

❖     Immediately book an appointment if you find the condition of blurred vision, ringing in the ears.

❖     Always take the drug with meal avoiding the chances of upset stomach

❖     Inform your doctor if you have bleeding while taking the drug.

❖     Keep away from heat, hot surface and open flames.

DESCRIBE A SUITABLE DOSAGE FORM FOR IBUPROFEN

The form of dose can be found in distinctive forms such as in tablets and in inhalers. The various dosages are decided on the basis of age and type of disease.

1.     Person suffering from arthritis is prescribed a dose of 300 mg twice a day.

2.     An individual should not use the drug more than 10 days  for the treatment of pain until directed by your doctor

3.     A patient suffering from juvenile arthritis is treated with 20-40 mg/day in 3 divided doses.

4.     Children from 6 months to 12 years of age are always recommended 5-10 mg/kg after every 8 hours.

FEW COLLECTIVE ANIMAL STUDY OF IBUPROFEN

Route

Animal used

Dose used

Action

i.p.

Calves

10mg/kg

Ibuprofen decreased PGE2 and lung

Histopathology was not altered while the viral shedding was increased.

Oral

Infants

2.2 mg/kg/day

Prophylactic ibuprofen mitigates the chances for surgery of patent ductus arteriosus but does not reduce death rate.

Oral

Rats

15 mg/kg

Fracture histology was not different in

Treatment of  animals than control animals.

i.v.

Rats

20 mg/kg/day

Rats condition become more worsen as compare to other uninfected rats

 

LIST OF TRADE NAMES AND MANUFACTURING COMPANIES OF IBUPROFEN IN THE TABULAR FORM

Brand Name

Company

Brufen

Wyeth Pharmaceuticals Inc.

Neurofen

Reckitt Benckise Pharmaceuticals Inc

Motrin

Sigma Aldrich

Lipton

Wyeth Pharmaceuticals Inc

Dolgit

Dolorgiet, Budapharma

Anflagen

Adare Pharmaceuticals Inc.

Trendar

Zibo Xinhua-Perrigo Pharmaceutical Co., Ltd

 

FREQUENTLY ASKED QUESTIONS ABOUT IBUPROFEN

Question1: How much time the drug ibuprofen takes to act potentially?

A person starts to feel better within 20 to 30 minutes after taking ibuprofen tablets while for long period pain an individual takes regularly for up to 3 weeks for its proper and effective action.

Question 2: Can one person take ibuprofen tablets and apply gel at the same time?

Of course, you can but you have to maintain the ratio of gel and dosage along with consulting your doctor before taking it for dose confirmation.

Question 3: Will I take this while driving or walking?

No, because this drug shows dizziness and tiredness while engulfing so this is an individual duty not to drive the vehicle after taking this to maintain own safety and others.

Question 4: Can I take Ibuprofen while drinking alcohol?

No, because too much drinking of alcohol during this drug will definitely create stomach problems like pain, upset feeling and indigestion in the stomach.

Question 5: Is there any food or drink I need to avoid?

Yes, it is OK to take this while eating and drinking because an empty stomach creates upset in the abdominal cavity.

Question 6: What one can do if ibuprofen does not work?

If this does not work accurately then one should go for paracetamol, aspirin and a combination of others also.

 

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