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Re: Trilisate and NSAIDs (long)

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>Have you tried other medications? I have tried trilisate (could not tell

you what is

>in it) and it helps for one ache or another. I have been on Naproxin and

it is the

>same thing...helps with some but nothing helps for all of the pain. but I

take a

>handful of pills all day long. I am amazed at the amount of pills I take.

I am too

>young for this.

Aricka, if you're taking this and your pain level isn't changed at all then

your Dr. isn't giving you the right stuff. You have a right to, and you

need, correct medication(s) to help with your pain!! I hope you can talk to

your Dr. about this....taking a lot of pills that aren't helping isn't good.

Trilisate and naproxin are both NSAIDs (Non Steroid Anti Inflammatory

Drugs). Ken indicated that he, like me, can't use the NSAIDs,

unfortunately. For anyone that's on a NSAID I'd highly suggest they talk to

their doctor about Cytotec (misoprostol) for stomach protection. The NSAIDs

stop the production of certain prostaglandins, a substance that protects

your stomach lining. The Cytotec will help keep your stomach from being

eaten up. My Mom took NSAIDs for years for osteoarthritis...and ended up

with HORRIBLE stomach problems. Her Dr. never bothered to treat that at

all. The last NSAID I tried (I've tried at least a dozen of them over the

years...with varying side effects) was Trilisate. My Rheumatologist said it

was the mildest one available, this was two years ago, and we had hopes I

could tolerate it and get some relief from its anti-inflammatory properties.

He also gave me Cytotec. Couldn't use the Trilisate, sigh, but I did learn

a lot more about the effects of these drugs on the stomach and how to

protect it. Here's some good info on prostaglandins and Cytotec

(misoprostol).

====================

Misoprostol / Cytotec

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GENERAL INFORMATION ON CYTOTEC® AND PROSTAGLANDINS

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1. What are Prostaglandin’s?

Prostaglandins (PGs) are a group of chemically related long-chained fatty

acids that are synthesised by most cells in the body and exert a wide

spectrum of local effects. Certain Prostaglandin’s are particularly active

in the gastrointestinal tract where they are released locally.

2. What is Mucosal Protection?

Mucosal protection is the maintenance of the integrity of the

gastrointestinal mucosa in the presence of endogenous aggressive factors,

such as gastric acid, and exogenous aggressive factors, such as

non-steroidal anti-inflammatory drugs. Components of mucosal defence are

listed in the table below.

Components of the mucosal barrier

Mucus gel formation and secretion.

Bicarbonate secretion

Mucosal blood flow

Restricted routes of hydrogen ion permeation

Epithelial regeneration

Mucus provides a protective barrier, shielding the mucosa from Hydrogen

ions as well as abrasion. Bicarbonate ions serve to neutralise gastric

acid. Mucosal blood flow provides the mucosa with energy in the form of

nutrients and removes excess Hydrogen ions. Finally, mucosal protection

depends on rapid regeneration of epithelial tissue.

3. What are the effects of Prostaglandins on the Gastrointestinal Tract?

Certain Prostaglandins, particularly those of the E series, have a number

of actions that protect the gastro-duodenal mucosa against numerous

aggressive factors, thereby maintain mucosal integrity.

These actions include

mucus secretion

bicarbonate ion secretion

mucosal blood flow

gastric acid secretion

4. What is Cytotec®?

Cytotec® (Misoprostol) is a synthetic analogue of Prostaglandin E1 (PGE1).

Like endogenous PGE1, Cytotec® exerts a protective effect on the

gastrointestinal mucosa by increasing mucus and bicarbonate ion secretion

and by increasing mucosal blood flow. In addition, Cytotec® inhibits acid

secretion.

Naturally occurring PGE1 is ineffective after oral administration because

it is unstable in an acid environment; it is also quickly degraded when

administered parenterally, giving it no practical clinical utility.

However, the structural modifications to naturally occurring PGE1 that led

to the development of Cytotec® resulted in an orally active drug with a

duration of action that makes it clinically useful.

5. Is Cytotec®‘s action a local response or is it dependent on absorption

into the systemic circulation?

Cytotec® (Misoprostol) acts locally on the parietal cell to decrease acid

secretion. It also exhibits local mucosal protection by supplying an

exogenous source of Prostaglandin’s.

The principal active metabolite (Misoprostol acid) is rapidly metabolised

and absorbed following oral administration.

NSAIDS AND THE GI TRACT

6. What is the Incidence of Ulcer during Chronic NSAID Use?

Observations reported from a variety of clinical trials indicate that the

incidence of peptic ulceration during Chronic NSAID use is substantial -

depending on the study design, between 22% and 60% of patients.

7. Are there Differences in GI Damage between Younger and Older Patients

Receiving NSAID Therapy?

There are definitely differences in the gastrointestinal impact of NSAID

therapy on younger versus older patients. In a case-control study, the risk

of NSAID-associated bleeding ulcer was greater in patients 60 years of age

or older. There is an increasing incidence of NSAID-associated bleeding

ulcer with advancing age: only 6% of those between 15 and 44 years of age

to 37% of patient 75 and older. Analysis of attributable risk indicated

that approximately 22% of bleeding ulcer cases were attributed to NSAID use

in patients 60 years of age and older.

The results of clinical studies of Cytotec® indicate that no significantly

different responses to safety and efficacy of therapy with Cytotec® were

observed in elderly patients. These data suggest that dosage adjustments in

the elderly are unnecessary.

8. What is the Mechanism of Effect of NSAID on the Gastrointestinal Tract?

Because of their anti-inflammatory properties, NSAIDs (including aspirin)

are widely used to reduce pain and swelling. However, in the

gastrointestinal tract, PGEs are also involved in mucosal protection. Thus,

by inhibiting the formation of PGEs, NSAIDs reduce the protective ability

of the gastrointestinal mucosa.

Aspirin and other NSAIDs also exert topical damaging effects on the

gastrointestinal tract, an effect that is independent of NSAID inhibition

of cyclooxygenase activity.

9. Are GI Symptoms Predictive of Lesions in Patients Taking NSAIDs?

NSAID-treated patients do not necessarily have symptoms even though

gastropathy (ie, injury to the gastric mucosa) is present.

CONCURRENT USE OF CYTOTEC® AND NSAIDS

10. Can Concomitant Administration of Cytotec® with NSAIDs be used to

Prevent or Treat NSAID-induced GI Mucosal Damage?

Several double-blind, placebo-controlled clinical trials have demonstrated

that concomitant use of Cytotec® (Misoprostol) and NSAIDs can protect the

GI Mucosa against NSAID-induced damage.

11. Does Concomitant Administration of Cytotec® and NSAIDs Interfere with

the Efficacy of the NSAIDs?

In a study of 239 patients with rheumatoid Arthritis who were taking

NSAIDs, 19 Rheumatoid Arthritis variables were analysed to examine

Rheumatic Activity. Among 106 patient’s who received Cytotec®, no evidence

of interference by Cytotec® with the anti-rheumatoid effects of the NSAID

was observed.

12. What is Cytotec® Recommended Dosage for Preventing NSAID Damage?

Based on clinical studies, the recommended dosing regimen for prevention of

NSAID-induced ulcers, erosions, and lesions is Cytotec® 800ug per day in

four divided doses co-administered with continuing NSAID therapy if

appropriate, with meals and at bedtime.

In South Africa - it is registered for 200mcg twice daily use.

13. Can Cytotec® be Concomitantly Administered with NSAIDs for Long-term

Therapy?

Cytotec® had no influence on the absorption, metabolism, or excretion of a

variety of other drugs including NSAIDs.

14. Should Cytotec® and NSAIDs be used Concomitantly in all Patients who

Require Chronic NSAID Therapy?

In studies of regular NSAID users, 20% to 25% developed ulcers in three

months. Therefore, any patient who cannot tolerate major complications of

NSAID therapy, such as GI bleeding or perforation, is a candidate for

co-adminstration of Cytotec®.

Patients with a history of NSAID-induced lesions or ulcer disease, and the

elderly, seem to be at a greater risk of developing NSAID-induced

complications.

15. How does Cytotec® Compare with Cimetidine in Preventing NSAID-induced

GI Mucosal Damage?

In a double-blind, randomised study, the protective effects of Cimitidine

vs Placebo were studied in patients with Arthritis who were using a variety

of NSAIDs. Cimetidine failed to heal or protect the GI Mucosa in these

patients during the eight-week treatment phase and the ten-month

maintenance phase of the study.

16. How does Cytotec® Compare with Ranitidine in Protecting the Gastric

Mucosa from NSAID-induced damage?

There are no direct comparative trials of Cytotec® and Ranitidine. However,

in clinical studies comparing Ranitidine to Placebo, Ranitidine did not

protect the Gastric Mucosa from damage induced by NSAIDs.

SAFETY OF CYTOTEC®

17. What are the Most Common Side Effects Associated with Cytotec® Therapy?

The most common side effect associated with Cytotec® therapy in clinical

trials was diarrhoea, which is a natural response to the intestinal smooth

muscles to the increased level of Prostaglandin’s. In clinical trials,

diarrhoea occurred in approximately one tenth of patients. It was usually

mild and self-limiting, resolving within a few days despite continued

therapy. Cytotec® is to be dosed with meals and at bedtime, which will

minimise this side effect.

18. Can Cytotec® be used in patients with Compromised Liver or Kidney

Function? How does this compare with H2-receptor Antagonists?

Cytotec® (Misoprostol) is metabolised by fatty acid oxidising systems found

in organs throughout the body. Its metabolism and plasma levels are

therefore unlikely to be affected markedly in renal dysfunction or hepatic

impairment. This suggests that the drug can be safely administered to

patients with hepatic or renal impairment without the need for dosage

adjustment.

19. Can Cytotec® be used in Pregnant or Nursing Women?

Cytotec® may endanger a pregnancy, and its effects on developing human

foetus are not known. Therefore, Cytotec® should not be used in pregnant

women. Women should be advised not to become pregnant while taking

Cytotec®. If a woman becomes pregnant whilst taking Cytotec®, use of the

product should be discontinued.

Although it is not known whether Cytotec® is excreted in human milk,

Cytotec® should not be administered to nursing mothers.

20. Are There any Known Drug Interactions with Cytotec®?

In clinical trials, there was no evidence of interaction between Cytotec®

and cardiac, gastrointestinal, pulmonary, or central nervous system drugs

Decreased bioavailability of Misoprostol Acid was observed with high doses

of antacid. However, low doses of antacids administered during ulcer

healing trials had no effect on the efficacy of Cytotec®

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My doctors and I are anxiously awaiting them!! For me, the stomach problems

were the least of it with the NSAIDs. I had blurred vision, double vision,

shortness of breath, and dizziness with almost every one I tried. The

Trilisate we had hopes for and it didn't give me any of those side effects

but it did give me horrific intenstinal distress and the Cytotec gave me

'the runs' and although they say that should clear up quickly, it didn't.

:-(

===========================

Ruthie Cunliffe K2ZQ

ruthie@...

http://www.cunliffegroup.com/ruthie/

experimental web cam: http://www.cunliffegroup.com/ruthie/spy/

>Also keep in mind that Vioxx, the new ll inhibitors will be out

>soon, and will not be harsh to the stomach. I can provide more info on

>this new drug if anyone is interested.

>Lyn =^..^=

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