Case 5-a very important case

Mr. Sami, is 55 year old male patient, hypertensive but with good control of

his blood pressure with capozide 50/25 single tablet daily, presented to

a nearby pharmacy complaining of alternating nasal congestion, sneezing as

well as rhinorrhea.No fever.

The pharmacist prescribed him the following:
-Congestal 3 tablets/day.
-C-retard one capsule in the morning.
-Otrivin nasal spray.

The day after, the patient developed headache,which failed to respond to

the usual analgesics.(He usualy takes Novalgin Oblong tablets or Brufen 400 tablets)

On measuring the blood pressure,it was elevated (160/100mg).

The patient was worried and presented to his family physician, who told him

that the pharmacist's prescription was the cause of the disturbed

blood pressure.

He advised him to be very cautious while taking over the counter

medications because many can adversely affect his blood pressure.

Moreover, he stressed that he should take Capozide on an Empty stomach,
half an hour before meals or two hours after, and told him that this
is extremely important!!!

In addition, he advised him to use analgesics other than Novalgin and Brufen

, and prescribed him Paramol.

Questions:
How did this prescription lead to this disturbance of the blood pressure?

Why did the family physician discourage the use of Brufen and Novalgin for regular analgesia?

Why did the physician stress on the fact that Capozide should be taken
on an empty stomach?

(Note, this case is based on true events)

Congestal tablets

It is a very popular common cold preparation, available as OTC.

Composition:
Paracetamol
Chlopheniramine maleate
Pseudoephedrine

Capozide 50/25 tablets

Composition:
50mg Captopril
25mg Hydrochlorothiazide

Dose:The usual dose is one tablet daily.

Company: It is a product of Bristol-Myers Squibb, based in New York city.
(The packs of its products are characterized by their yellowish color!)

Logo of the company:( notice it on the pack)

Otrivin nasal spray:
contains Xylometazoline,a potent decongestant.

Novalgin:
contains Metamizole, a NSAID.

hi
i ve read the case,it is simple and straightforward but u can add the implications of components on the case.
well done mohamed

Hello Dr tagho,

You are welcome.

This case is not that simple, it is just looks like that!

Very Happy

I am waiting for your answers and I am sure it will be a

fruitful discussion.

وجدتها وجدتها
Q1

1-pseudoephedrine in the congestal

Pseudoephedrine is a sympathomimetic amine—that is, its principal mechanism of action relies on its indirect action on the adrenergic receptor system. While it may have weak agonist activity at α- and β-adrenergic receptors, the principal mechanism is to cause the release of endogenous norepinephrine (noradrenaline) from storage vesicles in presynaptic neurons. The displaced noradrenaline is released into the neuronal synapse where it is free to activate the aforementioned postsynaptic adrenergic receptors.

These adrenergic receptors are located on the muscles lining the walls of blood vessels. When activated by pseudoephedrine, the muscles contract, causing the blood vessels to constrict (vasoconstriction). These constricted blood vessels now allow less fluid to leave the blood vessels and enter the nose, throat and sinus linings, which results in decreased inflammation of nasal membranes as well as decreased mucus production. Thus, by constriction of blood vessels, mainly those located in the nasal passages, pseudoephedrine causes a decrease in the symptoms of nasal congestion.

The vasoconstriction that pseudoephedrine produces is believed to be principally an α-adrenergic receptor response. While all sympathomimetic amines, to some extent, have decongestant action, pseudoephedrine shows greater selectivity for the nasal mucosa and a lower affinity for central nervous system (CNS) adrenergic-receptors than other sympathomimetic amines.

Vasoconstriction in the nasal mucosa shrinks swollen nasal mucous membranes, reduces tissue hyperemia, edema, and nasal congestion. Other beneficial effects may include increasing the drainage of sinus secretions, and opening of obstructed Eustachian tubes. The same vasoconstriction action can also result in hypertension, which is a noted side effect of pseudoephedrine.

2-xylometamizole in otrivin

The drug works by constricting the blood vessels in the nose. The vasoconstriction means that there is less pressure in the capillaries and less water can filter out, thus less discharge is made. (If the colour of the nasal passage is observed, it is visibly paler after dosage.)

Xylometazoline is designed to mimic the molecular shape of adrenaline meaning that it binds to the same cell receptors adrenaline does. For this reason, it should not be used by people with high blood pressure, or other heart problems. (It acts mainly on alpha-adrenergic receptors.)

Q2

metamizole in Novalgin

It carries a risk for fatal agranulocytosis

According to comments by Dr Anthony Wong of the University of São Paulo, Brazil in a WHO newsletter, recent studies estimate that the incidence rate of metamizole-induced agranulocytosis is between 0.2 and 2 cases per million person days of use, with approximately 7% of all cases fatal (provided that all patients have access to urgent medical care). In other words, one should expect 50 to 500 deaths annually due to metamizole in a country of 300 million, assuming that every citizen takes the drug once a month.

Q3بصراحة انا دورت و ما لاقتش المعلومة بالظبط بس هوا دا اللى لاقيته

caposide

Captopril is a white to off-white crystalline powder that may have a slight sulfurous odor; it is soluble in water (approx. 160 mg/mL), methanol, and ethanol and sparingly soluble in chloroform and ethyl acetate.

Hydrochlorothiazide is a white crystalline powder slightly soluble in water but freely soluble in sodium hydroxide solution.

After oral administration of therapeutic doses of captopril, rapid absorption occurs with peak blood levels at about one hour. The presence of food in the gastrointestinal tract reduces absorption by about 30 to 40 percent; captopril therefore should be given one hour before meals
يا رب تكون اجابتى كافية ووافية .....و يا سلام لو الواحد جاب ايه عشان يتفاءل حبه

اجابات رائعة ووافية حقا ، جزاكي الله خيرا.

ويا رب نكون استفدنا من هذه الحالة لأنها مهمة فعلا.
Availability of Metamizole allover the world:

Metamizole was banned in Sweden in 1974, in the United
States in 1977; more than 30 countries, including Japan,
Australia, Iran, and part of the European Union, have
followed suit. In these countries metamizole is still
occasionally used as a veterinary drug. In Germany it
became a prescription drug

In other parts of the world (including Spain, Mexico, India,
Brazil, Russia, Turkey, the Republic of Macedonia, Bulgaria,
Romania, Israel and some developing countries) metamizole
is still freely available over-the-counter, remains one of the
most popular analgesics,

As you have mentioned,It was discovered that the drug carries a small risk
of causing agranulocytosis - a very dangerous and potentially fatal
condition. Controversy remains regarding the level of risk.
.

موضوع: applied information الأحد مارس 01, 2009 1:16 pm

انا متشكرة جدا يا دكتور محمد
بس السؤال الاخير عايز توضيح i mean applied information

بالنسبة للسؤال الأخير...

فكما قلتي، إن امتصاص الكابتوبريل يقل إلى النصف تقريبا في حالة وجود الطعام في الجهاز الهضمي

لذا يجب أن يكون استخدامه على معدة خالية....

شكرا على مشاركتك الفعالة.

ok i agree with u , but the question is why it is interfered with food . is the problem is with its solubility or interaction with food or it needs acidic media for absorption for example and if yes so wht about acidic food .
or ... does this interfere at the level of stomach or it continues throughout the GIT....
may be im so complicated or even talking in details but those are questions need explanation for completion of image
thx for cooperation

I don't know for sure, but I will try to search for that.

I would like to tell you a very important thing, NSAIDs in general can be
potentially harmful in this patient's condition.

Do you know why? (you can postpone the answer to after
the exam)

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