Random Drugs Questions...

This forum made possible through the generous support of SDN members, donors, and sponsors. Thank you.

josh6718

Pharmacist
15+ Year Member
Joined
May 11, 2006
Messages
352
Reaction score
219
Just wondering, as these questions have been bothering me and the older Pharmacists I work with at my retail chain don't know.

1.) What's the difference between a cream and ointment? Why would one be prescribed over the other?

2.) How do extended-release tablets work (ie xanax or ritalin)?

3.) Why can't insulin be made as a topical or tablet?

Thanks

Josh

Members don't see this ad.
 
The answer to number 2 is a complicated one. It varies from drug to drug. Some use different size pellets, some use different coatings. I hope that you kinda understand that. If not pm me and I can dig my old notes from drug design out!
 
1. cream/oint - I could go on & on & talk about viscosity, thixotropy, etc...more than you want to know. On the easy side - a cream is a smoother product which will cover, but less occlusively than an ointment, which is "greasier". Therapeutically, depending on the state, it is within the pharmacists realm of responsibilty to interchange them. So, you need to learn the chemistry behind them. (Its not hard to learn, just more than you want here). If you want good penetration, particularly through a thick epidermal site - an ointment will be a good choice. If you want coverage and need to wear clothing over the site - a cream might work better. There are few cases in which only one will be preferable over another.

2. Extended release products can be made in a variety of ways. Some - like Ambien CR are designed to have two layers of medication, one which releases fast & one slower - for a reason. The fast layer helps with sleep induction, the slower helps with maintaining sleep.

Other products can be put into a "matrix" which controls release out of the matrix. Others are granules within a capsule formulation. After the outer capsule dissolves in the stomach, the granules are designed to either dissolve there as well or move down into the intestine & dissolve & become absorbed there. Most drugs are actually absorbed in the small intestine, not the stomach, but by controlling the dissolution & the coating we can control where each part of that occurs.

Some drugs have slow release & we don't even know why. Dilantin is a good example of that. It wasn't until Dilantin went off patent & generic products were made that it was discovered the kinetics of phenytoin were actually delayed in the Dilantin product. There is an extended release phenytoin product, but it is not interchangable with Dilantin because the manufacturer really doesn't know why their product continues to have the kinetics different than the extended release generic. Both are equally acceptable as long as you stay within the product you have chosen & don't switch products.

3. Insulin is an extremely unstable protein to acid - thus it can't be taken orally - the stomach acid would inactivate it. It is absorbed across the mucosa - thus the inhaled insulin, altho that product has its own issues. If you're referring to "topical" as in absorbed thru the skin - that is difficult for any product since the epidermal layer is uniquely designed to keep things "out" which don't belong & things "in" which do. We can design products - topical catapres, ntg, fentanyl patches which can be absorbed through the skin. But, again, the skin is a bit on the acidic side, so the drug must be stable (insuline is not stable in acidic environments) & the patch must be designed so it is occlusive enough to actually penetrate the epidermis. This method of drug delivery is great for chronic continuous medications - like catapres or fentanyl. Its not so great for a drug which must be given in response or anticipation of a varying physiologic event - like blood sugar.

Hope that answers your questions....
 
Members don't see this ad :)
1. cream/oint - I could go on & on & talk about viscosity, thixotropy, etc...more than you want to know. On the easy side - a cream is a smoother product which will cover, but less occlusively than an ointment, which is "greasier". Therapeutically, depending on the state, it is within the pharmacists realm of responsibilty to interchange them. So, you need to learn the chemistry behind them. (Its not hard to learn, just more than you want here). If you want good penetration, particularly through a thick epidermal site - an ointment will be a good choice. If you want coverage and need to wear clothing over the site - a cream might work better. There are few cases in which only one will be preferable over another.

2. Extended release products can be made in a variety of ways. Some - like Ambien CR are designed to have two layers of medication, one which releases fast & one slower - for a reason. The fast layer helps with sleep induction, the slower helps with maintaining sleep.

Other products can be put into a "matrix" which controls release out of the matrix. Others are granules within a capsule formulation. After the outer capsule dissolves in the stomach, the granules are designed to either dissolve there as well or move down into the intestine & dissolve & become absorbed there. Most drugs are actually absorbed in the small intestine, not the stomach, but by controlling the dissolution & the coating we can control where each part of that occurs.

Some drugs have slow release & we don't even know why. Dilantin is a good example of that. It wasn't until Dilantin went off patent & generic products were made that it was discovered the kinetics of phenytoin were actually delayed in the Dilantin product. There is an extended release phenytoin product, but it is not interchangable with Dilantin because the manufacturer really doesn't know why their product continues to have the kinetics different than the extended release generic. Both are equally acceptable as long as you stay within the product you have chosen & don't switch products.

3. Insulin is an extremely unstable protein to acid - thus it can't be taken orally - the stomach acid would inactivate it. It is absorbed across the mucosa - thus the inhaled insulin, altho that product has its own issues. If you're referring to "topical" as in absorbed thru the skin - that is difficult for any product since the epidermal layer is uniquely designed to keep things "out" which don't belong & things "in" which do. We can design products - topical catapres, ntg, fentanyl patches which can be absorbed through the skin. But, again, the skin is a bit on the acidic side, so the drug must be stable (insuline is not stable in acidic environments) & the patch must be designed so it is occlusive enough to actually penetrate the epidermis. This method of drug delivery is great for chronic continuous medications - like catapres or fentanyl. Its not so great for a drug which must be given in response or anticipation of a varying physiologic event - like blood sugar.

Hope that answers your questions....

good lord woman...

I don't think I can type that much on any topic complicated or not. can't you answer these with 1 sentence only?? :smuggrin:
 
SDN...

You know Cerebyx is going generic soon..right?
 
isn't cerebyx the three-headed dog that guards that gates of Hades?;)

dilantin has an amorphous crystalline structure that was a sort of happy accident over at parke-davis...that they can't, or more to the point, won't explain. which is another reason why phenytoin generic are not AB'd to dilantin kapseals. [i believe that the "kapseal" itself is a proprietary process, too]
 
SDN...

You know Cerebyx is going generic soon..right?

What is the status of the first available generic? I read that the anticipated date is August 2007, however, I have not done my research on whether Parke-Davis filed any last minute lawsuits seeking extended patent protection on things like the color of the solution, or the color of the vial they sold Cerebyx in.

Also, is there any information on how fosphenytoin will be priced? I have just learned that I am conducting an MUE on this medication, but am not so sure it will be on the institution's "high cost, must stifle utilization somehow" list once the generic is available.
 
What is the status of the first available generic? I read that the anticipated date is August 2007, however, I have not done my research on whether Parke-Davis filed any last minute lawsuits seeking extended patent protection on things like the color of the solution, or the color of the vial they sold Cerebyx in.

Also, is there any information on how fosphenytoin will be priced? I have just learned that I am conducting an MUE on this medication, but am not so sure it will be on the institution's "high cost, must stifle utilization somehow" list once the generic is available.

Hospira and Bedford have been allowing hospitals to prebook. Check with them. Bedford has better pricing right now. I've heard as low as $8 per larger vial. But like Zofran... I bet within 3 months, the price will bottom out. You can throw the MUE out the window on Fosphenytoin.
 
Hospira and Bedford have been allowing hospitals to prebook. Check with them. Bedford has better pricing right now. I've heard as low as $8 per larger vial. But like Zofran... I bet within 3 months, the price will bottom out. You can throw the MUE out the window on Fosphenytoin.

One more stupid question, what is the cost of a vial of Cerebyx as it is now (so I can put the $8 generic price in perspective).

And thanks, by the way.
 
2ml vial = $22.28
10ml vial = $66.87
 
You can do a simple cost analysis.

Take your past 12 months purchase and utilization and reconcile...you'll see how many vials have been overstocked, uncharged for, or lost.

Then take the same amount with the new generic cost. The difference is the amount of money you'll save in the next 12 months.

Present it to whoever... and you'll be the hero.
 
btw, you should have access to your wholesalers online account. So you can pull 80/20 monthly. Go down the list and find cost savings opportunity.

You may be a step ahead of your director.

I used to take the monthly 80/20 purchase list then reconcile with the utilization report....by golly if I bought 33 vials of integrilin...I better have used 33 vials of integrilin that month. I expected that kind of accurate purchase from my purchaser...for a tight inventory control.

I would also pull the controlled substance purchase report then reconcile it with utilization... not every line item but random checks... and if I bought around 5,000 tabs of lortab... the hospital better have used around 5,000 tabs that month.
 
2.) How do extended-release tablets work (ie xanax or ritalin)?

I've been wondering about this one, specifically Boniva and Fosamax. How does Boniva work for a whole month?
 
Members don't see this ad :)
3. Insulin is an extremely unstable protein to acid - thus it can't be taken orally - the stomach acid would inactivate it. It is absorbed across the mucosa - thus the inhaled insulin, altho that product has its own issues. If you're referring to "topical" as in absorbed thru the skin - that is difficult for any product since the epidermal layer is uniquely designed to keep things "out" which don't belong & things "in" which do. We can design products - topical catapres, ntg, fentanyl patches which can be absorbed through the skin. But, again, the skin is a bit on the acidic side, so the drug must be stable (insuline is not stable in acidic environments) & the patch must be designed so it is occlusive enough to actually penetrate the epidermis. This method of drug delivery is great for chronic continuous medications - like catapres or fentanyl. Its not so great for a drug which must be given in response or anticipation of a varying physiologic event - like blood sugar.

Hope that answers your questions....

Umm just to elaborate a bit, the acidity of the skin isn't the primary reason insulin isn't available transdermally. It's the sheer size of the molecule... most drugs over the size of 500g/mol are too large to fit through the gap junctions. As well, transdermal offers erratic absorption which isn't acceptable for diabetics - oil/hair/types of skin all affect how much of the molecule can pass through.

Remember.. if it was just the acidity of the skin [which pales in comparison to the stomach] basic buffers could be utilized, or some pro-pro-form of insulin introduced. It's proteins are so falliable, very difficult.
 
1.) What's the difference between a cream and ointment? Why would one be prescribed over the other?

Not all topical cream and ointment with the same strength have the same potency. For example, triamcinolone acetonide 0.025% cream is a "low potency" topical steroid while triamcinolone acetonide 0.025% ointment is a "medium low potency" topical steroid.
 
2.) How do extended-release tablets work (ie xanax or ritalin)?

a drug becomes "extended release" when the generic version is about to come on the market. hehe
 
An ointment is topical product in a hydrophobic base. Think Vaseline.
A cream is a topical product in a hydrophilic base. Think Ponds Cold Cream

For a given drug and strength, Ointments are more potent than creams which are more potent than gels.

As for Dilantin, Dilantin in and of itself is NOT timed release. Neither the liquid nor the chewable tablets are timed release. The capsules are Phenytoin Extended and the generics are AB rated and bioequivalent according to The Orange Book.

Now that you folks want to discuss ancient Pharmacy, an era I lived through, I can give you some ancient history:

Kapseal: Is a trademarked capsule made by Parke-Davis (Now Pfizer) where the capsule is sealed by band around the center.

Spansule: Is a trademarked sustained release capsule made by Smith, Kline and French (Now Glaxo Smith Kline)

Pulvule: Is a trademarked capsule made by Eli Lilly (Still Eli Lilly) where the capsule has a bullet shaped end.

Extentab: Is a trademarked sustained release tablet made by A.H. Robbins (Now I have no idea who owns the trademark) It has been sold more times than the answers to last years pharmacology final.

Repetab: Is a trademarked sustained release tablet made by R.P. Schering.

What you can gather from this is there are some medications that are sustained release or long acting by their nature. Think Salmetrol VS Albuterol. There are other medications that are sustained release or extended action due to the drug delivery system. Each drug delivery system is proprietary and works in a different manner. Some are immediate release and sustained action combined while others are a continuous release all the way.
 
good lord woman...

I don't think I can type that much on any topic complicated or not. can't you answer these with 1 sentence only?? :smuggrin:

No - I can't:D! (oh - but, I just did...;))

Now - you are old enough to "get it" that women talk ..... I mean "TALK"!!!

You've had how many female employees (who, I believe I recall all "cycle" at the same time..) - one wife (you admit to) & Little Miss Sux - who will throw you into complete & utter frustration in ....oh let me think - within the next 3-5 years which will continue on until she's at least 25 (I'm still counting....).

So - no - I CANNOT answer in one sentence......"we need to talk", (sweetheart, boss, sir, whomever).

Aaaaah - the power of words that women have - we can bring you to your knees:D:laugh::laugh::laugh::laugh:!

j/king!
 
Umm just to elaborate a bit, the acidity of the skin isn't the primary reason insulin isn't available transdermally. It's the sheer size of the molecule... most drugs over the size of 500g/mol are too large to fit through the gap junctions. As well, transdermal offers erratic absorption which isn't acceptable for diabetics - oil/hair/types of skin all affect how much of the molecule can pass through.

Remember.. if it was just the acidity of the skin [which pales in comparison to the stomach] basic buffers could be utilized, or some pro-pro-form of insulin introduced. It's proteins are so falliable, very difficult.


Good point! Yeah - the protein is huge, but really - look at the cellular differences between mucosa & epidermis. Is it really just size...or is it the acidity which breaks down the molecule before it can be absorbed? There is a time/active chemical absorption issue - which I admit I don't fully understand.

I really don't know & I haven't looked at the recent pharmaceutics literature.

We know insulin adheres to plastic IV containers, altho not so much to DHEA free IV containers - which makes converting SQ to IV dosing so difficult & "judgemental".

What do you know - have you got references??? I'd love to know the hows & whys, so any info you have would be appreciated.

Insulin is an interesting molecule!!!

btw....I have a very slllllloooooowwww connection tonight. Drsdn says there is a technician coming out tomorrow to look at it. I hope this posts!
 
I thought it was the protease that broke down the insulin...
 
I've been wondering about this one, specifically Boniva and Fosamax. How does Boniva work for a whole month?
I thought it was because it was a much higher dose than the daily tablet (which is 2.5 mg instead of 150 mg) and because the half-life of the bisphosphonates is sooo long.....like 10 years! I don't think it has anything to do with pharmaceutical formulations and tricks...but if anyone has a better explanation, I'd love to hear it!
 
I've been wondering about this one, specifically Boniva and Fosamax. How does Boniva work for a whole month?

Talking simply, I believe it is related to an extremely long half life after being taken up into the bones. I am sure ithere's a more detailed explanation out there....
 
1. cream/oint - I could go on & on & talk about viscosity, thixotropy, etc...more than you want to know. On the easy side - a cream is a smoother product which will cover, but less occlusively than an ointment, which is "greasier". Therapeutically, depending on the state, it is within the pharmacists realm of responsibilty to interchange them. So, you need to learn the chemistry behind them. (Its not hard to learn, just more than you want here). If you want good penetration, particularly through a thick epidermal site - an ointment will be a good choice. If you want coverage and need to wear clothing over the site - a cream might work better. There are few cases in which only one will be preferable over another.

2. Extended release products can be made in a variety of ways. Some - like Ambien CR are designed to have two layers of medication, one which releases fast & one slower - for a reason. The fast layer helps with sleep induction, the slower helps with maintaining sleep.

Other products can be put into a "matrix" which controls release out of the matrix. Others are granules within a capsule formulation. After the outer capsule dissolves in the stomach, the granules are designed to either dissolve there as well or move down into the intestine & dissolve & become absorbed there. Most drugs are actually absorbed in the small intestine, not the stomach, but by controlling the dissolution & the coating we can control where each part of that occurs.

Some drugs have slow release & we don't even know why. Dilantin is a good example of that. It wasn't until Dilantin went off patent & generic products were made that it was discovered the kinetics of phenytoin were actually delayed in the Dilantin product. There is an extended release phenytoin product, but it is not interchangable with Dilantin because the manufacturer really doesn't know why their product continues to have the kinetics different than the extended release generic. Both are equally acceptable as long as you stay within the product you have chosen & don't switch products.

3. Insulin is an extremely unstable protein to acid - thus it can't be taken orally - the stomach acid would inactivate it. It is absorbed across the mucosa - thus the inhaled insulin, altho that product has its own issues. If you're referring to "topical" as in absorbed thru the skin - that is difficult for any product since the epidermal layer is uniquely designed to keep things "out" which don't belong & things "in" which do. We can design products - topical catapres, ntg, fentanyl patches which can be absorbed through the skin. But, again, the skin is a bit on the acidic side, so the drug must be stable (insuline is not stable in acidic environments) & the patch must be designed so it is occlusive enough to actually penetrate the epidermis. This method of drug delivery is great for chronic continuous medications - like catapres or fentanyl. Its not so great for a drug which must be given in response or anticipation of a varying physiologic event - like blood sugar.

Hope that answers your questions....
Wish I could be this fluent and smart like you once I graduate...:thumbup:
 
Top