Psycho-Babble Medication Thread 537977

Shown: posts 1 to 12 of 12. This is the beginning of the thread.

 

Oh yay, another single-isomer drug launched in UK

Posted by ed_uk on August 5, 2005, at 17:31:14

It's a shame that the drug companies and spending so much time developing single-isomer drugs (think Lexapro $$$) rather than actually making the effort to develop innovative products.

Dexibuprofen (Seractil) is now available in the UK. Dexibuprofen is the active isomer of ibuprofen.

Seractil

Composition: Dexibuprofen.
Presentation: Film-coated tablets.
Class: Anti-inflammatory and antirheumatic product.
Indications: Symptomatic treatment for the relief of pain and inflammation associated with osteoarthritis or other forms of mild to moderate pain such as muscular-skeletal pain or dental pain. Acute symptomatic treatment of pain during menstrual bleeding.
Dosage: 600 to 900mg daily, divided in up to three single doses. Maximum single dose 400mg.
Precautions: Care is recommended in conditions that predispose patients to the gastrointestinal adverse effects of NSAIDs, and in elderly patients. In the rare instances where gastrointestinal bleeding or ulceration occurs, dexibuprofen should be discontinued immediately. In the treatment of patients with heart failure, hypertension, renal or hepatic disease, especially during concomitant diuretic treatment, the risk of fluid retention and a deterioration in renal function must be taken into account. See SPC.
Contraindications: Include patients in whom substances with a similar action precipitate attacks of asthma, bronchospasm, acute rhinitis or cause nasal polyps, urticaria or angioneurotic oedema. Patients with gastrointestinal ulcers, bleeding disorders, Crohn’s disease, active ulcerative colitis, heart failure, severe renal dysfunction or severely impaired hepatic function. See SPC.
Side effects: Most common are gastrointestinal. See SPC.
Legal category: P*M.
Net price: 300mg 60 £9.47, 400mg 60 £9.97.

~Ed

 

Re: Oh yay, another single-isomer drug launched in UK

Posted by tecknohed on August 5, 2005, at 18:18:56

In reply to Oh yay, another single-isomer drug launched in UK, posted by ed_uk on August 5, 2005, at 17:31:14

> It's a shame that the drug companies and spending so much time developing single-isomer drugs (think Lexapro $$$) rather than actually making the effort to develop innovative products.
>
> Dexibuprofen (Seractil) is now available in the UK. Dexibuprofen is the active isomer of ibuprofen.
>
> Seractil
>
> Composition: Dexibuprofen.
> Presentation: Film-coated tablets.
> Class: Anti-inflammatory and antirheumatic product.
> Indications: Symptomatic treatment for the relief of pain and inflammation associated with osteoarthritis or other forms of mild to moderate pain such as muscular-skeletal pain or dental pain. Acute symptomatic treatment of pain during menstrual bleeding.
> Dosage: 600 to 900mg daily, divided in up to three single doses. Maximum single dose 400mg.
> Precautions: Care is recommended in conditions that predispose patients to the gastrointestinal adverse effects of NSAIDs, and in elderly patients. In the rare instances where gastrointestinal bleeding or ulceration occurs, dexibuprofen should be discontinued immediately. In the treatment of patients with heart failure, hypertension, renal or hepatic disease, especially during concomitant diuretic treatment, the risk of fluid retention and a deterioration in renal function must be taken into account. See SPC.
> Contraindications: Include patients in whom substances with a similar action precipitate attacks of asthma, bronchospasm, acute rhinitis or cause nasal polyps, urticaria or angioneurotic oedema. Patients with gastrointestinal ulcers, bleeding disorders, Crohn’s disease, active ulcerative colitis, heart failure, severe renal dysfunction or severely impaired hepatic function. See SPC.
> Side effects: Most common are gastrointestinal. See SPC.
> Legal category: P*M.
> Net price: 300mg 60 £9.47, 400mg 60 £9.97.
>
> ~Ed
>

LOL! Seems like the warnings and side effects are no different to standard Ibuprefen! Just like Escitalopram!

 

Re: Oh yay, another single-isomer drug launched in UK » tecknohed

Posted by ed_uk on August 6, 2005, at 10:49:46

In reply to Re: Oh yay, another single-isomer drug launched in UK, posted by tecknohed on August 5, 2005, at 18:18:56

Hi!

>LOL! Seems like the warnings and side effects are no different to standard Ibuprofen!

Indeed, they are the same! ........but ibuprofen is cheaper.

>Just like Escitalopram!

What an over-hyped drug. I'm still on citalopram, no plans to switch to escitalopram.

I can't believe how much American pdocs are prescribing Lexapro. Talk about effective marketing..... or gullability. It's a rip off. Generic fluoxetine is particularly cheap. In the UK, generic fluoxetine costs the NHS £2 a month (per patient on 20mg) - it's one of the cheapest ADs!

~ed

 

Re: Oh yay, another single-isomer drug launched in UK

Posted by Nickengland on August 6, 2005, at 14:05:06

In reply to Oh yay, another single-isomer drug launched in UK, posted by ed_uk on August 5, 2005, at 17:31:14

Hi Ed!

>It's a shame that the drug companies and spending so much time developing single-isomer drugs (think Lexapro $$$) rather than actually making the effort to develop innovative products.

Well said and I definately agree!

>Dexibuprofen (Seractil) is now available in the UK. Dexibuprofen is the active isomer of ibuprofen.

This caught my attention as I use ibuprofen quite alot (used to use Nurofen), but of course what with tesco etc offering ibuprofen at prices of 40p per 16 tablets, I buy their make now - theres not much difference anyway is there?

Back to Dexibuprofen lol I was wondering, will this be available over the counter?...sometime in the future perhaps?

Kind regards

Nick

Ps Whats an isomer?

 

Stereochemistry: optical isomers » Nickengland

Posted by ed_uk on August 6, 2005, at 15:17:06

In reply to Re: Oh yay, another single-isomer drug launched in UK, posted by Nickengland on August 6, 2005, at 14:05:06

Hi Nick!

>I was wondering, will this be available over the counter?

Newly licensed products are only available on prescription initially. I do think it's likely that dexibuprofen will be available OTC at some point in the future though.

>What's an (optical) isomer?

Although there are different types of isomers, I was specifically referring to optical isomers in my post.... so that's what I'll tell you about :-)

Many drugs (eg. paracetamol) consist of a single chemical/molecule only. Some drugs however, such as ibuprofen, consist of *two* distinct chemicals/molecules rather than one. The two molecules are *mirror images* of one another. Ibuprofen consists of two chemicals: dexibuprofen (aka S-ibuprofen) and R-ibuprofen. Dexibuprofen is the active drug.

The 'new' drug, dexibuprofen consists of a single optical isomer only. Standard ibuprofen consists of both optical isomers in a 50:50 ratio ie. 50% dexibuprofen and 50% R-ibuprofen.

Dexibuprofen isn't really a new drug as such, it's simply the active component of ibuprofen.

Similarly, citalopram (Cipramil, Celexa) consists of two chemicals: escitalopram (S-citalopram) and R-citalopram. Escitalopram is the active drug: it's now sold on its own under the brand name Lexapro (Cipralex in the UK). R-citalopram appears to be relatively inactive. Although the manufacturer claims that Lexapro is more effective and better tolerated than Celexa, there is no good evidence to support this claim.

Celexa consists of 50% escitalopram and 50% R-citalopram. Lexapro is 100% escitalopram. Since R-citalopram is (probably) inactive, 20mg Celexa has the same antidepressant effect as 10mg Lexapro.

Drug companies like to develop single-isomer drugs because it can be very profitable. Celexa is now available as a generic whereas Lexapro is not. Lexapro is $$$$

In cases where one optical isomer of a drug is therapeutically active and the other is toxic, separating the isomers is very valuable. In other cases, where one optical isomer is active and the other is inactive, separating the isomers is of no medicinal value: think Lexapro $$$. In most cases, the therapeutically active isomer is also the isomer which causes the side effects! It's a shame that the drug companies are putting so much effort (money) into developing pointless single-isomer drugs when they could instead be developing new and innovative drugs with novel mechanisms of action.

Kind regards

~ed

 

Re: Stereochemistry: optical isomers » ed_uk

Posted by Nickengland on August 7, 2005, at 8:48:30

In reply to Stereochemistry: optical isomers » Nickengland, posted by ed_uk on August 6, 2005, at 15:17:06

Hi Ed!

>Newly licensed products are only available on prescription initially. I do think it's likely that dexibuprofen will be available OTC at some point in the future though.

Always good to know there'll be something extra, although ibuprofen is usually fine for myself - judging by this product though and how you've explained the optical isomers (very well by the well :-)), i'll probably end up sticking with ibuprofen..and it'll be cheaper!

>Standard ibuprofen consists of both optical isomers in a 50:50 ratio ie. 50% dexibuprofen and 50% R-ibuprofen.

So when they made ibuprofen or celexa, is it the case they did not know that part of, one of the optical isomers was actually inactive?...and so after realising they then think *ah, maybe we can take that out, market a new drug to then make $$$ in a kind of sense...also just happens that the patent of their old drug has ran out too?..Hmmm

>It's a shame that the drug companies are putting so much effort (money) into developing pointless single-isomer drugs when they could instead be developing new and innovative drugs with novel mechanisms of action.

Completely agree, I guess theres various examples of this type of marketing with other products in the market place as well beside drugs - that said when it comes to cashing in on peoples health and more importanly mental health, it is a shame.

>I was specifically referring to optical isomers in my post.... so that's what I'll tell you about :-)

It was a pleasure reading that Ed, thanks for an intersting read :-)

Kind regards

Nick

 

Re: Stereochemistry: optical isomers » Nickengland

Posted by ed_uk on August 7, 2005, at 15:17:01

In reply to Re: Stereochemistry: optical isomers » ed_uk, posted by Nickengland on August 7, 2005, at 8:48:30

Hi Nick!

>So when they made ibuprofen or celexa, is it the case they did not know that part of, one of the optical isomers was actually inactive?

They would have known that R-citalopram is inactive because the pharmacology of both optical isomers has to be studied. Celexa is a racemic mixture - it consists of 50% R-isomer and 50% S-isomer. A racemic mixture is easy and cheap to synthesise - this is why many drugs are racemic mixtures. Pure escitalopram (Lexapro) is more expensive (and more technically demanding) to synthesise.

>...ah maybe we can take that out, market a new drug to then make $$$ in a kind of sense...also just happens that the patent of their old drug has ran out too?

That's right!!

>Completely agree, I guess theres various examples of this type of marketing with other products in the market place as well beside drugs - that said when it comes to cashing in on peoples health and more importanly mental health, it is a shame.

Yes, there's a LOT of 'me too' drugs on the market ie. one company discovers a sucessful drugs and other companies synthesise *very similar* drugs which they hope will be successful.

Ibuprofen is a NSAID (non-steroidal anti-inflammatory drug). In the UK, there are currently 25 NSAIDs on the market - most of them don't have any special advanatages, they're 'me too' drugs, about 5 NSAIDs would be perfectly adequate. Drug companies put a lot of effort into developing 'me too' drugs because they're often very profitable. Most new drugs are not particularly innovative. Instead of developing 'new' NSAIDs, it would be a lot more valuable if drug companies spent more money on developing anti-inflammatory drugs with novel mechanisms of action.

In the UK, there are currently 11 ACE inhibitors on the market (the ACE inhibitors are a class of drug used to lower blood pressure). All ACE inhibitor are very similar and have an identical mechanism of action. We only really need about 2 ACE inhibitors. ACE inhibitors are very profitable though so drug companies keep on developing 'new' ones. Instead, they ought to be developing *new types* of drugs to lower BP.

Kind regards

~Ed

 

Re: Stereochemistry: optical isomers » ed_uk

Posted by Nickengland on August 7, 2005, at 16:26:04

In reply to Re: Stereochemistry: optical isomers » Nickengland, posted by ed_uk on August 7, 2005, at 15:17:01

Hi Ed!

>Yes, there's a LOT of 'me too' drugs on the market ie. one company discovers a sucessful drugs and other companies synthesise *very similar* drugs which they hope will be successful.

With the 'me to' drugs - do you think its the case that in certain respects they could be reaching the end of the road?....you know, they're simply running out of ideas because they only have so many chemical elements/combinations to choose from and they've already used so many?

LOL..Or, conversely they are just being greedy and lazy because indeed there is far much more to be discovered?

>Ibuprofen is a NSAID (non-steroidal anti-inflammatory drug).

Now let me sound like a pure idiot :-) Ibuprofen is *not* a steroid drug then? - Just wanted to double check, I've read steroid type drugs can be bad for bipolar. (when I was younger I used to take a steroid inhailer type spray for some allergy, fortunately I do not anymore)

Ed, to study to be a Pharmacist, how many years does it take to be fully qualified vs that of a doctor?...Drugs really do interest me, i'm alittle curious...I bet you must have got some pretty good GCSE's in science subjects - and then in A - Levels too? - My results were pathetic, seriously and I had to drop out of 6th form because of depression...oneday though, I hope to get some of that lost time back.

Kind regards

Nick

 

Re: Stereochemistry: optical isomers » Nickengland

Posted by ed_uk on August 7, 2005, at 16:33:07

In reply to Re: Stereochemistry: optical isomers » ed_uk, posted by Nickengland on August 7, 2005, at 16:26:04

Hi Nick!

>Or, conversely they are just being greedy and lazy because indeed there is far much more to be discovered?

I think it's just greed. Novel drugs are more expensive, more time-consuming and more difficult to develop than 'me too' drugs.

>Ibuprofen is *not* a steroid drug then?

No, it's not a steroid.

>Ed, to study to be a Pharmacist, how many years does it take to be fully qualified vs that of a doctor?...

Pharm - 5 years in the UK. 4 at uni.

Doc - 5 years at uni, followed by much more learning on the job.... and more exams!

>I bet you must have got some pretty good GCSE's in science subjects....

My GCSEs were good, I got 7 A*s and 3 As. I think I'm gonna drop out of uni though, I really don't like it, it gets me down.

Kind regards

~Ed

 

Re: Stereochemistry: optical isomers » ed_uk

Posted by Nickengland on August 7, 2005, at 17:54:39

In reply to Re: Stereochemistry: optical isomers » Nickengland, posted by ed_uk on August 7, 2005, at 16:33:07

Hi Ed!

>My GCSEs were good, I got 7 A*s and 3 As.

*Good* is understatement - they were outstanding! :-)

>I think I'm gonna drop out of uni though, I really don't like it, it gets me down.

If it gets you down, then I guess only you can decide if it'll reach the point that it'll get too much and you'd have to drop out, with regards to depression :-(


I have to say though Ed, look like you've done about 2 years by now right?..so you're kind of half way. Now (this may sound stupid) but if you climb a mountain and you're half way to the top, the hardest part could well be getting to reach the peak - the end of uni. That said, you've made it to half way....with determination I bet you could reach the top :-)

On the other hand, is it possible to have a year break and then start back from where you left off?

I think your really fortunate Ed lol...I wish I could be in a position to have those grades behind me! I read the other day, now that the government is bringing student fees (£3000 a year?) for university, students will now be paying off debts to the age of 36 on average..its disgusting!

Kind regards

Nick

 

Re: Stereochemistry: optical isomers

Posted by tecknohed on August 7, 2005, at 23:04:06

In reply to Stereochemistry: optical isomers » Nickengland, posted by ed_uk on August 6, 2005, at 15:17:06

I suppose one possible advantage of drugs based on the 'active' isomer would be for patients who have difficulties detoxifying the original form. They would only need half the dose. That assumes of course that both the 'active' and 'inactive' isomers of a drug go through the same detoxifying route/process.

 

Re: Stereochemistry: optical isomers » Nickengland

Posted by ed_uk on August 8, 2005, at 14:17:45

In reply to Re: Stereochemistry: optical isomers » ed_uk, posted by Nickengland on August 7, 2005, at 17:54:39

Hi Nick!

>On the other hand, is it possible to have a year break and then start back from where you left off?

I hope so. I'm going to enquire :-)

Kind regards

~Ed


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