OLDER ANOREXIANTS THAT ARE (or were)FDA APPROVED FOR WEIGHT LOSS   

 PHENTERMINE  

[original brand name was Fastin decades ago; available generic; a cousin of amphetamines].  Available in 15, 30 & 37.5mg,   A 30mg capsule every AM is usual dose; maximum dose  is 37.5mg capsule  (commonly available in this dose as the brand Adipex-P).   15mg is only available in the brand Ionamin (more expensive than generic).  It is no longer available in tablets of  8mg which I used to obtain to start people very slowly.  Adding caffeine to phentermine helps weight loss, although caffeine alone has no benefit for weight loss.

DIETHYLPROPION (Tenuate was old brand name; cousin of amphetamines and a cousin of Wellbutrin / bupropion): 25mg and 75mg tablets.   The usual [and maximum] dose is 75mg every AM—or 25mg 3 times a day with meals.  It is good to start out slowly at 25mg or even ½ of 25mg every AM, to avoid side effects. It is similar to phentermine, but somewhat “milder.”

PHENDIMETRAZINE 35mg 3 times a day ; or 105mg slow release 1 qAM

mazindol  [Mazanor 1mg; Sanorex: 1mg, 2mg] [not usually available in pharmacies apparently], dose is 1mg 3 times a day one hour before meals or 2mg once a day, one hour before lunch.   But start with 1mg once a day, and go up slowly. This medication is not used much and is hard to obtain

Meridia (sibutramine) –off the market

DIET MEDICATIONS NEWER ANOREXIANTS THAT ARE FDA APPROVED FOR WEIGHT LOSS    

QSYMIA [phentermine / topiramate E.R. combination]  7.5/46  or 15/92 mg   q.d. [$170/mo] 

BELVIQ (locaserin)  10mg 2x/day  [$200/mo]  serotonin 2C receptor agonist indicated as an adjunct to a reduced-calorie diet and increased physical activity for chronic weight management in adults with an initial body mass index (BMI) of: 30 kg/m2 or greater (obese)  27 kg/m2 one weight-related comorbid condition, (e.g., hypertension, dyslipidemia, type 2 diabetes)  Drug Interactions:  SSRIs, SNRIs, MAOIs, triptans, bupropion, dextromethorphan, St. John’s Wort: use with extreme caution due to the risk of serotonin syndrome.

XENICAL (Orlistat):  120mg  3 x/day  [$44/mo] A.  to be taken 3 times a day immediately after meals. You can take it with a meal or up to 1 hour after a meal.  It keeps fat from being absorbed in the intestine.  Some vitamins are absorbed along with the fat. Another option:  you could take it just occasionally with certain meals.      B.) So you should take 1, or even 2, regular multivitamins per day at least 2 hours before one of your meals if you are taking Xenical.   C.) When on Xenical, if you eat too much fat, you will get a little diarrhea because of extra fat in the stool.   Diarrhea caused by fat in the stool is called steatorrhea.  This steatorrhea may be the main reason that Xenical works. The changes in the stool can be quite unpleasant, including becoming rather foul smelling.  So one becomes very cautious about eating much fat.  This steatorrhea is also the main reason people stop the medication.    D.) You could take less  Xenical if you don’t need it 3x/day or if you know a particular meal would cause excessive diarrhea—e.g., if  you indulge in a large steak followed by ice cream.   E.) If you lose weight, you should still stay on Xenical to maintain the loss.

NALTREXONE/ BUPROPION [opioid antangonist/ antidepressant] 8/90mg pills. Dose is 1-2 pills in AM. [$200/mo]

SAXENDA/ LIRAGLUTIDE  GLP-1 receptor antagonist;  3mg/day subcutaneous injection [18mg/3ml prefilled pen]  [$1068].  This is the same as Victoza / liraglutide, but in a dose of 3mg/day instead of 1.8mg.

MEDICATIONS THAT ARE NOT FDA APPROVED FOR WEIGHT LOSS:

TOPAMAX (topiramate): FDA approved as an anticonvulsant. It can be very effective for weight loss.  However, in many people the dose needed for good effect leaves them too sedated and “stupid” the next day.  Maximum dose 400mg or more, but dose for weight loss is often only 25 to 100mg.  My usual instructions: Friday night start 25mg every night.  Every Friday try to ­ by 25mg, until you reach 100mg if possible.  Stay lower if sedated.   Drink more water every day, as there is an increased incidence of kidney stones with this medicine.

ZONEGRAN (zonesimide):  Much less sedating than Topamax .  At Duke University [where there is a well known weight loss center] they use 600mg for weight loss. It causes kidney stones in 2-3% –drinking a lot of water may decrease risk of kidney stones.  Usual plan: start with 100mg every night, and every week ­ by 100mg until you reach 400mg at bedtime.

TESTOSTERONE:  if you increase muscle bulk, you can burn more calories;  the benefit is probably minor; it would be most applicable in men whose testosterone is quite low.

AMANTADINE:  prevented weight gain from olanzapine –Graham et al, 2005

ALPHA LIPOIC ACID In one study alpha lipoic acid in a dose of 1200mg/day (split, probably 600mg twice a day), caused a 7 lb weight loss in 12 weeks (J. Clinical Psychopharm, April, 2008)     HCG injections — I doubt it works 

DIABETES MEDICATIONS USED FOR WEIGHT LOSS—but NOT FDA APPROVED FOR WEIGHT LOSS:

GLUCOPHAGE (metformin): Available in 500, 850, & 500 XR. It is used commonly for Type II Diabetes (“adult onset” diabetes).  Most diabetic agents cause weight gain, but this one causes anorexia (¯’d appetite).  If an overweight person takes this, they are less likely to develop diabetes.   This one never lowers the glucose excessively. Negative:  It should be avoided in people who drink much alcohol.  Rarely, it causes a severe metabolic problem called lactic acidosis, which can be fatal. 

GLYSET 50-100mg  tid—apparently safe in non-diabetics.

GLUCOTROL [glipizide]  5mg or 10mg tablets bid; another medication for diabetes. Has a risk of lowering glucose too much.

LEVEMIR – but risk of hypoglycemia

FARXIGA (dapaglifozin)  5mg and 10mg pills;  5mg in AM; increase to 10mg if additional glycemic control is needed; don’t use if GFR <60. Inhibits sodium-glucose cotransporter in proximal renal tubule—so reduces reabsorption of filtered glucose.  one excretes 70 grams = 280 calories per day. It would, of course, increase risk of urinary track infections.  Can be used with metformin.

GLP-1 MEDICATIONS: [do not use if history of thyroid cancer;  a risk of pancreatitis]

VICTOZA / liraglutide   a copy of GLP-1 (glucagon like peptide); 1x/day shot with tiny needle

            SAXENDA/ also LIRAGLUTIDE:  FDA approved for weight loss; maximum is 3.0; but insurance will not cover it usually

BYETTA / exenatide:  also a copy of GLP-1 (glucagon like peptide)  twice a day shot

BYDUREON/ exenatide –once a week shot

NOTE:   The above medicines for dieting rarely work without concomitant vigorous exercise and dieting.   Don’t “do a diet”– the program must be a lifestyle change that is permanent, to keep the weight off.   Since obesity is chronic–like high blood pressure is chronic–some people will need to take these medications indefinitely in order to maintain the benefit.

 

F.Y.I.: SOME [PEPTIDE] HORMONES THAT CONTROL WEIGHT.   They are not available commercially. They are released into the bloodstream and their target is the brain:

  • LEPTIN: Long term action.  Discovered in ~1995.    It is made in fat cells.  When it reaches a critical amount it suppresses appetite in the brain.  When it is too low, women stop having menstrual period (e.g., professional athletes and anorexics).  It has not worked out for diet treatment as obese people are resistant to it.
  • GHRELIN: [pronounced grey-lin]  Short term action. Discovered in 1999.   It is made in cells in the stomach.  In stimulates appetite.  It goes very high 3 times a day, at mealtime.  It is the hormone that makes you achingly hungry when you are late for a meal.  Surprisingly, a gastropexy (“stomach stapling,” making the stomach smaller) virtually causes the production of ghrelin to CEASE.   This is probably the reason gastropexy works so well, with so little in the way of hunger pains.  [5/2002: David Cummings, of Washington, Seattle.]  This hormone apparently also retards lipolysis—i.e., it slows down the burning of fat.
  • PeptideYY3-36 or PYYMedium term action—about 12 hours. Discovered in 2002. It is made in the small intestine and it suppresses appetite.    At tiny dose caused a 33% decrease in intake of a buffet lunch 2 hours later.  And the subjects did not have a tendency to make it up after the effects wore off. [Stephen R. Bloom, London, Nature, 8/2002.]
  • GLP-1: (glucagon like peptide-1)—this is available commercially as Byetta / exenatide or Victoza / liraglutide or exenatide/ Bydureon    

 

DIET: CNN had a documentary  in 12/25/03 and 12/25/05,  re a scientist who keeps track of 3000 people who have lost at least 60 lbs and have kept if off for over a year.  What they have in common are generally these characteristics:

  • Expect failure, keep trying.
  • Eat 4-5 small meals per day.
  • Eat until you are content, not full.
  • High carbohydrate, low fat
  • Exercise at least one hour per day. [This is perhaps a sine qua non?] Some of the people they interviewed did an astonishing amount of exercise.
  • Weigh yourself frequently–e.g., 3-4 x/week or daily. [In order to keep up the motivation.  And it is a reward to see the weight coming off or staying off.]
  • Don’t deny yourself all the time.  If they have a strong urge to have some ice cream or a cookie, they will eat it, but only a small portion. Once in a while they will allow themselves to.