Although in the pastI've prescribed naltrexone atvariousdosesand at different times of the day, I changedthis to 4.5 mg at bedtime at the suggestion of Dr.
Bernard Bihari, who has prescribed it for ailments other than overeating.
This dosing method indeed appears to be the most effective.
Side effects that some patients have caUed to my attention include occasional headaches or a feeling of mental confusion that impairs concentration on difficult tasks.These effects areunacceptable, and so I may start my patients on a very low dose , 0.5 mg capsules, and increase the amount of each dose until we reach an effective level.
One must keep in mind, however, that smaUer doses are often more effec tive than larger ones.
As with the other suggestions in this book, ask your physician to give naltrexone a try.
He should pay particular attention to the pack age insert warnings against overdosing.
For other remarkable uses for low-dose naltrexone, visit the Web site www.lowdosenaltrexone.org.
I have patented this mode of using naltrexone,in order to encour age its distribution by pharmaceutical companies in low doses.
Such companies arenot interested in sellingproducts that arenot protected by patents.
Another product has curbed overeating in about 65 percent of the patients for whom I've recommended it.
This is hoodia, a nonpre scription extract of a South African cactus.
The brand I prefer is caUed HoodiaXtra, 1,000 mg.
It is avaUable online at www.hoodiaxtra.com and www.diabet.es911 .net.
Other brands, usuaUyin smaUerdoses, may be purchased at health food stores, Rosedale Pharmacy, and at other sites online.
Since hoodia begins working within 30-60 minutes, it should be taken about 1 hour before an anticipated need.
Thus, if you usuaUy overeat at dinner and then snack thereafter, you might take 1-3 capsules before dinner and another 1-3 after dinner.
Some sources of hoodia supply a timed-release version.
It is most effective when taken on arising and again 6-8 hours later.
I have seen no adverse side effects from this product, but I have never used it in chUdren.
(914) 925-2304. (Compounding chemists are pharmacists with special training in the precise mixing of pharmaceuticals and over-the-counter medications. They can prepare capsules,powders,liquids, and even ointments, just as all phar macists did when I was a child. There are many compounding chemists in the United States and elsewhere. Most require a physician's prescription.)
204 Treatment
Because demand for hoodia now exceeds the supply, many phony formulations are being marketed, especiaUy on the Internet.
To secure a reliable product, you would be wise to use a known brand supplier and a product without additivesthat may dUute its strength.
I believe that carbohydrate craving is truly an addiction.
This ad diction can be reinforced by consumption of foods on our No-No list (pages 152-153).
So once you have discontinued them, I recommend never trying them again or you wiU likelyrelapse.
Even a smaU taste can cause you to faU off the wagon , just as for smokers, alcoholics, and other drug addicts.
AN EXCITING NEW CLASS OF DRUGS CALLED INCRETIN MIMETICS TO FIGHT OVEREATING
You may recaU from our discussion of the Chinese restaurant effect (page 97) that intact pancreatic beta ceUs make a hormone caUed amylin.
Amylin productionis brought about in response to a meal,by gut hormones caUed incretins.
Since diabetics do not have beta ceUs that function adequately, they make Uttle or no amylin and therefore may not experience the degree of satiety that nondiabetics do.
They are therefore more likely to remain hungry after a meal and thus to overeat at meals and snack between meals.
Perhaps the most excitingclassof drugs to hit the market in many yearsactuaUy solves this problem.Productsin this categoryare caUed incretin mimetics (IMs) , that is,they imitate the effects of incretins or of amylin.
What is so special about them is that in my experience they reaUy work, and they do so for about 90 percent of users, a very high degree of success.
At present these products are sold to lower blood sugar after meals.
Our appUcation to overeating is therefore considered"off label" but is permitted by the FDA if prescribed by a physician.
The most effective IMs,at this writing,must be administered by in jection one or more times daUy.
The good news is that the needles are tiny, so these injections are painless if you foUow our injection tech nique (Chapter 16).
A once-weekly version wiU be avaUable shortly and an oral version (Januvia) is now on the market.
But start now with the injections because the benefits are so great.
How to Curb CarbohydrateCravingor Overeating 205
For example, I sawa newpatient recently who weighed 286 pounds (130 kUograms) and hadan HgbAlc of 6.9 percent when we first met.
I started her on an IM, and over a period of sUghtly less than a month and a half (44 days), her weight came down to 258 pounds (117.3 kUo grams) andher HgbAlc dropped to 5.2 percent.
Thus shelostan aver age of nearly 3A pound per day and her three-month moving average blood sugars dropped from 176 mg/dl to 108 mg/dl.
Her highest blood sugar of the final week of this period was 95 mg/dl.
Since the first dose of the new medication, she has been able to foUow our low- carbohydrate meal plan without hunger,cravings, or any snacking.
The recently developed incretin mimetics faU into three categories
Amylin analogs. The only one being marketedin late 2006is pram- lintide acetate, brand name Symlin. It is marketedbyAmyUn Pharma ceuticals, Inc. It is chemicaUy simUar to amylinand performs the same functions in the body. It is only avaUable for injection.
GLP-1 mimetics. GLP-1 is one of the hormones secreted into the bloodstream by the intestines that teU the beta ceUs of the pancreas to secrete amylin, insuUn, and glucagon. GLP is an abbreviation for "glucagon-like peptide."The only version currently on the market is exenatide (Byetta),jointly marketed by AmyUn Pharmaceuticals, Inc., and EU LUly and Company. It too is only avaUable for injection.
DPP-4 inhibitors.
DPP-4 is an abbreviation for dipeptidyl pepti dase-IV,the enzyme that the body uses to destroy GLP-1.Administra tion of its inhibitor opposes the destruction of naturaUy produced GLP-1.
This circumvents the need for injecting a GLP-1 mimetic.
Merck and Company is now sellinga tablet that can be taken oraUy, sitagliptin phosphate (brand name Januvia).
I question whether it wUl be as effective for diabetics (who makelittle or no amylin) as for non diabetics.
I am currently testing it for lowering blood sugars after meals.
HOW DO WE USE THE INCRETIN MIMETICS?
The only class of IMs that wiU be effective for curbing the appetite of people who have virtuaUy no beta ceUs (type 1 diabetics) is the amyUn
206 Treatment
analogs (i.e., pramlintide), sincethe other agentsonly serve to teU ex isting beta ceUs to make more amylin.
Therefore it makes sense to use only this class forthose of us who make no insuUn.
There is one catch, however.
Most type Is havehad high blood sug ars for more than five years and are therefore likely to have at least some degree ofgastroparesis, or delayed stomach-emptying.
Since one of the actionsof amylin (and therefore the other incretin mimetics) is to slow stomach-emptying, gastroparesis is likely to worsen.
As ex plainedin Chapter22,severe gastroparesis can make blood sugar con trol impossible.
If I am faced with a type 1 diabetic who has mUd to moderate gastroparesis but who also snacks on carbohydrate or overeats, I must then decidewhich wiU disturb his blood sugarsmore, the eatingbehavioror the gastroparesis.
This can be a tough caU, but the decisioncanbe facUitated with the help of the R-R study described in that chapter.
Any physician contemplating this problem should cer tainly readthat chapter.
I have one very obese patient who only overeats at restaurants and parties.
He has moderate gastroparesis.
I therefore have him taking Symlin only before eating out.
Fortunately, this strategy is working.
VirtuaUy any prescription medication has a potential for adverse side effects, and the IMs are no exception.
Since they do slow stomach- emptying, their most common adverse effectis gastrointestinal distur bances such asnausea, constipation,stomachaches, and even diarrhea.
It is therefore wise to start aU ofthem at alow dose and work up slowly if necessary.
Manufacturers of IMs currently on the market saythey must be in jectedabout 1 hour beforebreakfast and supper.
I suggest that excep tions should be made for those who overeat only between supper and bedtime, or only at supper, and so on.
In suchcases, I prescribe the IM about 1 hour before the overeating or snacking usuaUy occurs.
For those who only snack in the late afternoon and otherwise stick to our meal plan,I'd prescribe it for useabout 1hour beforethe usualtime of afternoon snacking.
Strangely, some users find that pramlintide must be injected 2-3 hours before the targeted time for it to be effective.
Therefore timing of injectionsis a matter of trial and error.
It is likely that in the near future long-acting injectable IMs wUl be avaUable that need be taken only once weekly.
RecaU from page 98 that amylin also reduces the body's production of or sensitivity to glucagon , the major culprit in the Chinese restaurant effect.
Between the reduced overeating and the reduced
How to CurbCarbohydrate Cravingor Overeating 207
glucagon effect, blood sugars can be much lower after meals , even dangerously low if you takeblood sugar-lowering medications of any kind.
It is therefore necessary that your physician loweryour doses of these agents at the time you start any incretin mimetic.
How much should doses be lowered?
To some extent it comes down to experimentation.
I usuaUy start by lowering premeal medications by about 20 percent.
I then may look at blood sugars the next day to see if dosing of these medications should be increased or decreased.
Adjusting Doses of Pramlintide (Symlin) Pramlintide is suppUed in rubber-stoppered vials, like insulin, but only half the size (5 ml).
EachmiUUiter contains 600 meg of the drug.
It is injectedwith a standard insulinsyringe, so 1"unit" on the syringe contains 6 meg.
I usuaUy start patients who weigh less than 150 pounds on 2-4 units taken 1 hour before their usual episodes of overeating or snacking.
So if someone only overeats at supper, she would inject about 1 hour before supper.
If he snacks between 9 p.m. and midnight, he'd inject at 8 p.m. and, if necessary, again at 10 p.m.
If someone overeats only when eating out, he'd inject about 1 hour be fore he anticipatesarriving at the restaurant and not on other days.
If she snacks aU day long, she might inject on arising and every 3-4 hours thereafter.
If someone gets adverse side effects, we'd cut back to a lower dose until side effects diminish, and then increase each dose lh unit per week until either cravings vanishor sideeffects reappear.
If no adverse effects appear initiaUy, doses might each be increased by 2 or 4 units until cravings cease.
Heavier people might start at higher doses with larger increases.
If doses total 120units over the course of a day without a major ef fect on appetite, I would assume that the medication is ineffective.