[e-drug] Safety of paracetamol injection

E-DRUG: Safety of paracetamol injection
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Dear e-druggers,
The drug regulatory authorities in Nigeria recently asked that the use of dypirone injections and metamizol tablets should be stopped as from September this year.
Health practioners in the country rely heavily on this drug for its anti-pyretic properties.
The same authourities have suggested that paracetamol injection could be a good replacement for dypirone injection, since there is a tendency for practioners to want to use injectables in these cases.

Does any one have information on the safety of paracetamol injection or its suitability for use.

Thanks,

Steve Iruedo
Nigeria
ikhafa steve iruedo <ikhafa2001@yahoo.com>

E-DRUG: Safety of paracetamol injection (2)
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Dear e-druggers
Paracetamol injectable is available under the trade name Perfalgan (Bristol
Myers Squibb) or Uppsa. Previously it was available as a
prodrug proparacetamol (Pro-Dafalgan .).

We have been using Pro-Dafalgan in Lebanon for quite few years and now we
moved to Perfalgan with no problem

Paracetamol infusion is given as drip into a vein. Paracetamol may be given
in this way either because a patient is unable to take medicines by mouth,
or because a rapid effect is needed. This infusion may be given for the
short-term relief of moderate pain, particularly following surgery. It may
also be used for reducing fever in the short-term.

Regards

Georgette

Chief pharmacist AUBMC
Lebanon
Georgette Ghulam <gg00@aub.edu.lb>

E-DRUG: Safety of paracetamol injection (3)
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It is still rather surprising why there is that preference in Nigeria to use injectable analgesics for low intensity pains. Non-Opioid analgesics administered orally are really enough in pains of non-visceral origin. The most common use of these injectable analgesics in Nigeria is for the acute management of pyrexia in malaria, yet fever in malaria can be successfully managed with oral NSAIDs. In Botswana, that suffers malaria epidemic in the Northwest part of the country, there is no dipyrone or metamizol in the EDL and fever due to malaria and other non-neurogenic pains are managed by oral paracetamol or ibuprofen.

I am not convinced of the rationale and not too sure why the regulatory authorities in Nigeria should recommend injectable Paracetamol, it does not have any mileage over the oral, provides public health risk (due to potential risk of injections) and it is not a rational and cost-effective way to manage low intensity acute pains.

Jude Nwokike

(B.Pharm, MSc.Pharmacology, MPH, MISPE)
Senior Program Associate
Rational Pharmaceutical Management, RPM Plus
Management Sciences for Health, MSH.
Windhoek, Namibia
"jude" <jnwokike@msh.org.na>

E-DRUG: Dipyrone/metamizol revisited
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Dear all

I am a bit surprised about this topic. First of all I did in 12 Years of
medical practice in Europe, Asia and Africa not come across injectable
paracetamol. Second I am not sure about the discussion on metamizole, it
is cheap, it is working and sideeffects like agranulocytosis are rare.
Thinking of all the people I have seen with bleeding gastric ulcers
(some of them dying...) I think that 0.25 cases of agranulocytosis per 1
million daily doses of metamizole are quite safe ( I know many people
will tell me different who have seen those cases...).

I do not know what makes the Nigerian authorities banning a widely used
drug, exchanging it with the most used drug for suicide attempt in
England. Having worked there for 6 months in an A&E department I have
seen quite a bunch of patients with Paracetamol overdoses. As I am not
able to recall an i.v. paracetamol preparation I am a bit doubtfull on
these recommendations. A quick internet research did not come up with
any formulations of paracetamol in injectable form either. All the other
problems with injectables in Africa (HIV is the major killer and hygiene
still a problem in many parts) make me think that there is a bit of a
problem here with general rcommendations....

For the use of antipyretic drugs or for mild pain I had good experiences
with oral or rectal applications of both of the above, here in germany
we use metamizole still as an efficient i.v. drug for both pain relief
and as an effective antipyrexial. Having the sideeffects in mind (and
looking maybe at prices for the customer) I am not so sure about this
policy shift...there might be better ways to educate physicians than to
exchange one potentially dangerous with an other one without questioning
the "doctor, give me a strong injection" culture.

Greetings

Martin Rieder, M.D.
Working in Internal Medicine in Germany, ex-MSF M.D. for seven years
"Martin Rieder" <martin.rieder@berlin.de>

E-DRUG: Dipyrone/metamizol revisited (3)
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Probably, the use of parenteral analgesics/antipyretics, especially
metamizol, is a West African prescription culture, which has lingered on. I
just returned from home, Sierra Leone, during which I was hospitalized with
a persistent high fever (101F). It seemed to me each time, that the
preferred choice was Metamizol injection. Although I recall that the fever
subsided within minutes, I was then left with the horrible thoughts of all
the debate we have had in e-drug about metamizol. I should add that on one
occasion, the night nurse gave me metamizol tablets, apologizing that they
had run out of injections!

For our colleagues in Nigeria/West Africa, this and related issues could be
tabled for discussion by the existing regular forum of the Drug Regulatory
Authorities of the Regional Health Community.

Murtada M. Sesay BPharm, MSc, MMI
Copenhagen, Denmark.
Tel: +45 3527 3098
Mobile: +45 28 23 28 07
Murtada Sesay <msesay@unicef.org>

E-DRUG: Dipyrone/metamizol revisited (5)
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Dear all

Although dipyrone is not marketed in European countries
because of the its potential bone marrow toxicities
(especially agranulocytosis), it has been used in Japan even
now by prescription only medicine.

OTC drugs which contain dipyrone was banned because it caused
many sudden death in the past due to anaphylactic shock or other
causes and because it became an social problem in Japan in 1965.

Those OTC drugs were oral preparations but it contained
about 300-500mg of dipyrone in an ampoule with a little ethanol.
It was absorbed very well.

Other type of cause of deaths were called as
- Abnormal toxic syndromee(by specialists of forensic medicine0.

According to the modern knowledge, it may be a fulminant type of Reye's syndrome related to the use of NSAIDs as antipyretics, or einfluenza related encephalopathy with multi-organ failure related to the use of NSAIDs.

According to my personal view, it should be called as a type of viral severe sepsis or a septic shock with multi-organ failure induced by over produced cytokines enhanced by NSAIDs.

Although task force of Japanese Ministry of Health Welfare (MHW) did not mention the relationship between Reye's syndrome and NSAIDs including diclofenac Na, mefenamic acid and dipyrone before 1998, some of their studies had already indicated the epidemiological relationship between both at least in 1992.

In 1999 other task force reported the epidemiological relation between case mortality due to influenza related encephalitis/encephalopathy and NSAIDs use such as diclofenac Na and/or mefenamic acid: odds ratio for mefenamic acid was 4.6 (95% CI: 1.03-20.49, p=0.049) and
for diclofenac was 3.05 (95%CI: 1.01-9.21, p=0.045).

Later the use of diclofenac Na and/or mefenamic acid became contraindicated to use for influenza infected children in Japan, but it is not prohibited to use in other viral infection and
bacterial infection. Other NSAIDs such as ibuprofen and dypirone (both oral and injection) is not prohibited. Moreover, NSAIDs including diclofenac Na, mefenamic acid and dipyrone
(including injection) is not prohibited to use for the fever of adult infection.

But I have been consulted with at least 5 adult cases of fulminant type of Reye's syndrome or influenza (virus infection)-related encephalitis/encephalopathy with multi-organ failure.

Acording to the task force of MHLW (Now Ministry of Health,
Labor and Welfare) 30 percents of the influenza related encepahalitis/encephalopathy including necrotizing encephalopathy was considered to be related to NSAIDs use.

Some animal studies indicate that NSAIDs antipyretics increase mortality rate of infected animals: Bacterially infected rabbits treated with sodium salicylate increased compared with saline treated infected rabbits.
Another study using virus infected rabbits indicated that treatment with mefenamic acid at a dose which did not induce death of animal also increased death than control with no NSAID.

Lowering by antipyretics of infected animals increase not only mortality rate, but also increased number of bacteria, viruses and interferons (one of the cytokines).

Cytokines including TNF may induce tissue damage of multi-organ including brain, liver, kidney and so on, even in the absence of bacteria or viruses in the damaged tissue. And these cytokines with or without endotoxins may play a role in inducing Reye's syndrome, encephalopathy in necrotizing pancreatitis and necrotizing encephalopathy.

Paracetamol do not enhance the induction of cytokines and is proven as much safer antipyretics than salycilates and other NSAIDs.

Bearing in mind the evidence that paracetamol is a much safer alternative antipyretic, these evidences of risk suggests that there is good reason to stop using NSAIDs including dipyrone
at least in children with fever (and it may be true for adults), especially of viral origin as soon as possible. It must be the most powerful measure to eradicate Reye's syndrome and to reduce fatality from influenza related encephalitis/encephalopathy
in Japan. It may also be true in Africa.

Dypirone decreases the body temperature but it never decrease virus. On the contrary, it may increase viruses and other microorganisms due to block of the inflammatory process (= tissue repair mechanism) of body.

The more effective in antipyretic the more dangerous for deterioration of infection and may be the cause of death.

For these reasons, I also conclude dypirone should not be used as antipyretics in infection of both viral and bacterial origin and of both in children and adults and both in Japan and in Africa.

References
1) Study on correlation between acute encephalitis of unknown
cause with severe sequelae and drugs. Report of the Task Force
Study for 1990 to 1992, published in March 1994.
2) Study on correlation between acute encephalitis of unknown
cause with severe sequels and drugs. Report of the Task Force
Study for 1996, published in March 1997.
3) Bernheim HA, Kluger MJ. Fever: effect of drug-induced
antipyresis on survival. Science (1976) 193:237-9
4) Vaughn LK, Veale WL, Cooper KE. Antipyresis: its effect on
mortality rate of bacterially infected rabbits.
Brain Res Bull (1980) 5: 69-73
5) Kurosawa S. Kobune F, Okumura K, Sugiura A. Effect of
antipyretics in rinderpest virus infection in rabbits.
J Infect Dis (1987) 155: 991-7
6) Vaughn LK, Veale WL, Cooper KE. Effects of antipyresis on
bacterial number in infected rabbits.
Brain Res Bull (1981) 7: 175-80
7) Treon SP, Broitman SA. Monoclonal antibody therapy
in the treatment of Reye's syndrome.
Med Hypotheses (1992) 39: 238-42
8) Mizuguchi M. Acute necrotizing encephalopathy of childhood:
a novel form of acute encephalopathy prevalent in Japan and Taiwan.
Brain Dev (1997) 19: 81-92

HAMA, Rokuro MD Chairman
Non-Profit Organization "Japan Institute of Pharmacovigilance"
publishing ISDB-full-membership Drug Bulletin
"Kusuri-no-Check" (JCheck-up Your Pills to Save Your Life
Deputy Editor: The Informed Prescriber
HAMA Rokuro <gec00724@nifty.com>

E-DRUG: Dipyrone/metamizol revisited (8)
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Dear E-druggers,

This is one of those absurdities that have become the hallmark of all facets of life and living in a perpetually underdeveloped setting like Nigeria. Pray what is the rationality of recommending the use of Injectable paracetamol for management pain or pyrexia.
And to think that recommendation came from a so called drug regulatory authority under a so-called 'purposeful' NAFDAC.

The circumstances surrounding the ban of Dipyrone injection was also full of absurdities. This is because this drug has been banned for over 10 years in countries where the health of the populace is of utmost priority.

But what do we have in Nigeria? NAFDAC under the current management has been
registering Dipyrone for sales and marketing in Nigeria. Was Dipyrone so safe then. A cursory look at the two cases of mortalities resulting from Dipyrone use, that woke NAFDAC from her slumber and made them alive to their responsibilities, was not thorougly and scientifically investigated to establish agranulocytosis. NAFADAC in her characteristic rash manner went on National television to make her usual noise. In my own opinion the two cases are strongly
linked to hypersensitivity reaction and bad injection practises resulting equally in badly managed infection.

Nobody has done a properly conducted case- controlled or prospective or observational study in Nigeria to document cases of agranuloytosis due to Dipyrone.
Neither has NAFDAC commissioned any one to the best of my knowledge. This is not to however say that NAFDAC should not have banned the drug. It should have been done long before now. Furthermore, NAFADAC went ahead to give a deadline of Dec 2005 to all doctors or pharmacists in possession of Dipyrone to use up their stocks and that the ban on Dipyrone takes effect from January 2006. where on earth can this happen except Nigeria, yet the current management of NAFDAC continued to be hailed as the best thing to happen to
drug regulation in Nigeria.

It is simply mind-boggling that NAFDAC recommended the use of injectable paracetamol for management of pyrexia. and this is the organisation that is suppose to be in the vanguard of safe guarding the nation's health. Had it not come to their notice that this not only highly irrational, it can further worsen the case of HIV transmission in Nigeria, particularly in the
rural areas where incidences of pyrexia due to parasitic infections in very high. A recently
published study in Lancet identified unbridled injection practices as a major contributory factor to increase in HIV infections in some part of sub saharan Africa.

Thank God for a forum like E-drug that have contributed in an immeasurable way to improve the standard and quality of care in all but particularly developing settings. I know that some key players in the health care sector in Nigeria are members of E-Drug and this will come to their notice. I sincerely hope they will make approriate contact with NAFDAC to sort out this mess.

K.B Yusuff
yusuffkby@yahoo.co.uk

E-DRUG: Dipyrone/metamizol revisited (12)
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In connection with giving grace period to potentially toxic drugs (metamizol in this case)before actual ban, Mr Babatunde asks: "Where on earth can this happen except Nigeria?"

It may interest him and others to know that Nigeria has good company. In fact, India beats Nigeria by giving grace period of upto 18 months! Examples: Astemizole, terfinadine etc. etc.

This patently pro-business, anti-people and unethical practice came to an end only when an NGO, Social Jurist, filed a successful Public Interest Litigation in High Court at Delhi. Under court orders, now the regulator, Drugs Controller General, India (DCGI)is duty bound to ban drugs, once considered harmful or ineffective on the very day of the notification.

Dr. Chandra M. Gulhati
Editor, MIMS INDIA
e-mail: indianmims@yahoo.co.uk, seeemgee@yahoo.co.uk