An Interview with Mr. Pharmaceutics

Jeepakistan Team (J. T.): Tell something shortly about yourself.

Mr. Pharmaceutics (P): I am an art from patient’s and customer’s point of view and science from doctor and scientist’s point of view.

J. T.: Your family members!

P: I’ve many brothers, children and grand children. My powerful brothers are biotechnology, medicine, chemistry and botany. My most favourite children are Hospital pharmacy, industrial pharmacy, forensic pharmacy and retail pharmacy. My grand children are computer education, biostatistics, quality control and many others.

J. T.: Some thing about your life!

P: Peoples love me. In most cases you’ll find me present everywhere from urban to rural areas, from jungles to desert, from air to water and from east to west. Even I love peoples very much. That’s why, I try to give them not only healthy life but also good employment opportunities.

J. T.: The hidden reality you want to tell peoples!

P: The best cure for every pain are not NSAIDs nor any other type of painkillers. But many types of pain can only be cured by the world’s best medicine, that’s love.

J. T.: I can’t understand, what you have said!

P: For example, in very old age the pain felt in the body is due to loneliness, if the children don’t leave their parents alone then the severity of the pain will be reduced.Even that pain will not be felt in many cases if the children give their parents much happiness.

J. T.: Your interview will be published. Do you want to give your readers some message?

P: I can’t do anything for disable peoples, genetically ill peoples and many peoples, who are in very poor or far off areas. Please, for the sake of God, help those peoples as much as you can.

J. T.: Thank you.

Sulfinpyrazone

It is a derivative of phenylbutazone.


Mechanism of Action:
Same as that of probenecid.

Therapeutic Uses:
It is used for the treatment of Uric acid.
Pharmacokinetics:
It shows renal excretion.

Adverse effects:
Same as that of probenecid.

Probenecid

Action:

It acts generally as an inhibitor of the tubular secretion of organic acids.

Mechanism of action:
It causes blockage of resorption of uric acid by proximal tubular resorption.

Therapeutic Uses:
It is used for the treatment of Uric Acid.
Pharmacokinetics:
It is well absorbed by renal tubules. Its plasma half life is about 5-8.5 hours.

Adverse effects:
It may show gastric discomfort.

Interaction:
Probenecid stops tubular secretion of penicillin and that is why it sometimes is used for increasing the levels of the antibiotic.

It also inhibits excretion of naproxen, ketoprofen and indomethacin.

Uricosuric agents

The uricosuric drugs are weak organic acids that cause an increased uric acid clearance through kidneys by stoping urate anion exchanger in the proximal convulated tubule of nephron that mediates the reabsorption of urate crystals (i.e. uricosuric agents act at the anionic transport site of renal tubule).

It includes
1. Probenecid
2. Sulfinpyrazone

Allopurinol

Introduction:

Allopurinol is a purine analog. It is also an isomer of hypoxanthine.

Mechanism of action:
Allopurinol inhibits xanthine oxidase enzyme which is required for the synthesis of Uric acid. This enzyme is required when purine is oxidized to Uric acid.

Therapeutic uses:
This is effective in the treatment of gout, which may be due to;
1. Primary hyperuricemia
2. Secondary hyperuricemia (Such as those caused from the use of chemotherapeutic agents or diseases of the kidneys).

It is also effective as an anti-protozoal agent.

Pharmacokinetics:
It is well absorbed (approximately 70-85%) orally. One of its metabolite is alloxanthine (also called as oxypurinol) which is also effective in the inhibition of xanthine oxidase. Allopurinol takes action along with this metabolite.

The plasma half life of allopurinol is 2 hours and that of oxypurinol is 15 hours. The drug and its metabolites are excreted in the urine and feces.

Dosage:
Due to the long half life of oxypurinol the dosage can be maintained at the rate of 1 dose/day. Its initial dose is 100 mg/day.

Adverse effects:
Hypersensitivity reactions such as rashes may occur. GI disturbances such as nausea and diarrhea can also be there.

Interactions:
It may cause an increase of the effect of cyclophosphamide. It may interfere with anti-cancer drugs such as 6-mercaptopurine and the immunosuppressant such as azathioprine.

Colchicine

Introduction:

It is an alkaloid obtained from plant, Colchicum autumnale. It has been found effective in the treatment of acute gout.

Mechanism of action:
It causes the disruption of cellular activities such as movement of granulocytes to the affected area and phagocytosis. It also inhibits the synthesis and release of leukotriene B4.

Action:

It relieves pain. Though it cannot prevent the progression of gout to acute gouty attacks but it is used as a prophylactic drug in this case so helps to keep down pain and frequency of acute attacks. It is now used in combination with probenecid.

Indomethacin is now replacing Colchicine.

Therapeutic Uses:
It is used for the relief of pain and inflammation in acute gout within 12-24 hours.

Pharmacokinetics:
It is absorbed rapidly from GI tract. Its peak plasma level is attained within 2 hours. Its plasma half life is 9 hours. It is recycled in the bile and excreted unchanged in the feces or urine.

Dosage:
The usual dosage of colchicines is 0.6 mg one to three times daily as a prophylaxis of gout.

Adverse effects:
It may cause nausea, vomiting, abdominal pain and diarrhea.
Prolonged administration may cause myopathy, aplastic anemia and alopecia.

Contraindications:
It is contraindicated in pregnancy.

Precautions:
It should be used with caution in hepatic, renal or cardiovascular diseases.

Gout

Purine metabolism is responsible for the production of Sodium urate. When the quantity of Urate in the blood goes up than normal, it may result in gout which may show inflammation and produces more oxygen metabolites in the blood.

Therapeutic strategies:
First of all it is better to use purine free diet i.e. we must use dairy products, fruits and cereals. The sequence, in the diagram, show that most effective medicine in treating gout is that which causes reduced entry of leukocyte into the affected joint which may be achieved by colchicine.

Other ways of therapy include:

1. Disturbing uric acid synthesis with the help of allopurinol.

2. Promoting excretion of uric acid with probenecid or sulfinpyrazone.

3. Use of NSAIDs.

Types of Gout:
There are two types of gout:

1. Acute gout.

2. Chronic gout.

Acute gout:
Causes:
The main causes of acute gout are as follows:

1. Diet which is rich in purine.

2. Kidney diseases.

3. Alcohol consumption.

Treatment:
In this we can use Indomethacin in combination with Aspirin. Indomethacin slows the movement of granulocytes in the area which is affected and aspirin decreases pain and inflammation.

Chronic gout:

Causes:
The main causes of chronic gout are as follows:
1. Genetic defect.
2. Renal deficiency
3. Lesch Nyhan syndrome.
4. Excessive synthesis of uric acid associated with cancer chemotherapy.

Treatment:
In this we can use Uricosuric drugs such as probenecid and sulfinpyrazone and Allopurinol.

Uricosuric drugs (e.g. Probenecid or sulfinpyrazone) promote excretion of uric acid resulting in reduced concentration of uric acid in plasma. It is preferred for patients with normal excretion of uric acid through urine.

Allopurinol selectively inhibits some steps in the middle of the biosynthesis of uric acid. It is preferred for patients with excessive uric acid excretion (which may be due to renal insufficiency).