Obesity Medications Flashcards
What medication was discontinued in 1997? Why?
Fen-Phen combination pills which was discontinued due to rare but serious valvular heart disease and pulmonary HTN. However, these effects were isolated to the other component of the medication (Fenfluramine which had non selective 5-HT activity) and has not been reported with Phentermine alone. However, there remains significant unfounded stigma surrounding Phentermine due to its association with this medication
Use of Metformin for weight loss in non-diabetics
Off label indication as not FDA approved
Study gave non-diabetic patients 2200-2500 mg per day total and average weight loss was ~6kg
Getting to that dose is a bit awkward. Could do 875 TID or add an extra half dose of 1000
The difference between Alli and Xenical
Alli is OTC and 1/2 the dose of prescription strength Xenical
Xenical costs about 10 times as much
Side effects with Topiramate
Change in taste (primarily soda) Dizziness Drowsiness Forgetfulness Paresthesias (transient and seen in ~30%of patients) Nausea Abdominal pain Diarrhea
1/2 life for Phentermine
Longer-acting medication. Half-life 20 hours, with peak effect at 4 hours. This is why it is typically dosed in the morning
Diethylpropion works similarly, but only lasts ~5 hours and has to be dosed multiple times a day
This med can cause false positive amphetamine testing
Contrave
Phentermine addiction potential? What level DEA schedule is it?
DEA schedule IV controlled substance (Need to review EFORSCE first), even though studies show no evidence of addictive potential, cravings, or withdrawal with this medication (unlike other medications in the class)
This medication can cause emergent priapism
Lorcaserin
Mechanism of action for Orlistat
Pancreatic lipase inhibitor, prevents absorption of about 30% of ingested fat
What obesity med was recently pulled from the market by FDA due to concerns about cancer
Lorcaserin/Belviq
If patient is possible candidate for future bariatric surgery, what should you keep in mind when considering weight loss medications
People who are on the border of qualifying for weight loss surgery might lose enough weight with meds to no longer meet criteria for more effective bariatric surgery
The cheapest and most widely available form of phentermine is? How much does it cost?
37.5mg tablets with a score down the middle.
About $10 for 30 at Publix
Capsules r more expensive, hard to find, and can’t be cut in half
Lomaira costs about $30 for 90 8mg tabs
There is an ODT version that costs ~$300
Weight loss meds that require titrating the dose
Qysmia
Contrave
Liraglutide
In some cases Phentermine and Metformin
Don’t need to titrations Belviq or Orlistat
This medication can increase risk of seizures with abrupt withdrawal
Topiramate
BMI criteria for starting weight loss medications?
BMI ≥ 30 or BMI ≥ 27 with co-morbidities
Cost of Bupropion with Good Rx coupon
~$20
Weight loss med(s) which effect serotonin levels
Lorcaserin
Zonisamide
Fenfluramine (Taken off the market)
The best weight loss med for patients who also have Migraines
Topamax
Weight loss medication to avoid in patients with history of bulimia or anorexia
Bupropion
The best weight loss med for patients who also have Pre-diabetes/diabetes
Metformin
Liraglutide
Weight loss medications that are off label
- Phentermine (and other sympathimemetics) for long term use
- Topiramate by itself
- Generic combination of Phen and Top rather than approved (more expensive) Qysmia
- Metformin
- Bupropion by itself
- Generic combination of Naltrexone and Bupropion rather than approved (more expensive) Contrave
These medications are taken TID with meals
Orlistat
Lomaira
Diethylpropion
This weight loss medication is free at Publix
Metformin
Preferred weight loss medication for patients with significant cravings
Contrave
This oral weight loss medication does not have any dose titration
Lorcaserin
Preferred weight loss med in obese patients who smoke
Bupropion
Contraindications to Phentermine use
Relative contraindications = uncontrolled HTN, CAD, hyperthyroidism, substance abuse, glaucoma, pregnancy, renal disease, and seizure disorder
This medication has been shown to have ASCVD benefit (at least in diabetes)
Liraglutide
This medication is probably the least effective as far as average weight loss
Orlistat
Mechanism of Setmelanotide
MC4R agonist for treatment of POMC Def
This medication has the same mechanism as Phentermine
Diethylpropion. Rarely used now
Way shorter half life than Phentermine so taken TID
Systemic absorption of this medication is minimal
Orlistat
This condition in female patients is a contraindication to all the weight loss medications
Pregnancy
Effect of Bupropion on anxiety
Can worsen anxiety and cause agitation, but not a clear contraindication
How do you treat POMC deficiency
Setmelanotide is an MC4R agonist for the treatment of POMC deficiency
Weight loss medications which are controlled substances
Phentermine/Qysmia
Lorcaserin/Belviq
Diethlpropion
If you start lower dose Phentermine and have some effect but don’t reach goal, what steps can you take to titrate up effect?
Can increase to a max dose of 37.5mg tab once per day
Many like to start with generic Phentermine and then later add generic Topiramate if needed to mimic Qysmia. Effect is synergistic, not just additive
Dosage of Topiramate
In Qysmia is 23mg ER —> titrations up to 46 or 94
Topiramate ER QD is $400-700 per month
Topiramate BID is available for about $10. Starting dose for other conditions is 25-50mg BID
Preferred med for sleep related eating disorder
Clonazepam
The only FDA approved weight loss medication that is available over the counter
Alli (Orlistat)
Titration and dosages of Qysmia
Phentermine-Topiramate 3.75-24
- 5-46 (suggested dose)
- 25-69
15-92 (high dose)
All QD
Spend at least 14 days at each dose before increasing
These weight loss medications may be best for patients with chronic constipation
Orlistat
Metformin
This weight loss medication can not be combined with antidepressants
Lorcaserin
Contraindications to Metformin
Severe heart failure and severe CKD
Caution in liver disease and alcohol abuse
The medication that has the biggest average weight loss
Qysmia
Liraglutide is prob second best
This weight loss medication causes nasopharingitis
Lorcaserin
Are Topamax neurological side effects self limited?
Tingling tends to be self limited and may not necessarily be an indication to stop the medication. Cognitive side effects are not self limited and therefore the Med should be stopped
Women with PCOS should be warned about this possible adverse effect of weight loss medications?
Pregnancy as become more regular
The bioavailability of this Med can be dangerously increased if taken with a high fat meal
Contrave
Injectable obesity medication
Liraglutide
The trade names for Orlistat
Alli and Xenical
Contraindications for Lorcaserin
Already on antidepressant, eGFR <30, on viagra, sickle cell (predisposed to priapism), or valvular heart disease
You should take this with Orlistat
Multivitamin (due to risk of fat soluble vitamin deficiency)
Fiber/Psylium supplement (to decrease side effects)
These weight loss meds can cause seizures
Bupropion/Contrave
Stopping Topamax suddenly can also cause seizures
Book said Phentermine, but Epocrates doesn’t
Trade name for low dose Phentermine taken with each meal
Lomaira
Difference between Saxenda and Victoza
Saxenda is about double the dose, but same med
These weight loss medications are sympathomimetics that stimulate the sympathetic nervous system directly
Phentermine
Diethylpropion
Indirectly other meds activate the sympathetic nervous system through intermediates like POMC
Patients taking this weight loss medication should also take a multivitamin
Orlistat
At this point in time, patients weight loss tends to plateau on a given medications
6-9 months
These meds should not be taken alongside Phentermine
Linezolid
MAOIs
Other stimulants (such as ADHD meds)
Generic name for Saxenda
Liraglutide
The most teratogenic weight loss medication
Topamax/Qysmia
Saxenda dosing
Titrated over 5 weeks = 0.6mg SC x 7 days –> 1.2mg SC x 7 days –> 1.8mg SC x 7 days –> 2.4mg SC x 7 days –> 3.0mg SC maintenance dose
Preferred weight loss Med for patients with chronic migraines
Topamax
Naltrexone use for weight loss on its own
Not really done on its own. Thought to augment effects of other medications
The trade name for Lorcaserin
Belviq
Stimulant similar to Phentermine which is much less commonly used now
Diethylpropion
Dual Efficacy weight loss medications
- Bupropion for depression and smoking cessation
- Metformin for pre-diabetes/diabetes and PCOS
- Liraglutide for DM
- Topiramate for seizures and migraines
Mechanism of Action for Liraglutide/Saxenda
GLP-1 agonist delays gastric emptying
Activates POMC and inhibits NPY
These medications activate POMC
Liraglutide/Saxenda
Lorcaserin/Belviq
Bupropion (And combo Contrave)
Phentermine (and combo Qysmia)
Basically everything other than orlistat
Contrave side effects
Gastrointestinal symptoms are common with naltrexone/bupropion. Up to one in three patients will report nausea and 19% will experience constipation, especially early in treatment. Headache, dizziness, and sleep disorders are also common. In premarketing studies, about 20% of patients discontinued treatment because of adverse effects.
Long term use of this weight loss specific medication is off label?
Prescribing for more than three months of Phentermine is considered “off label.” Generic so nobody is gonna study it. There is abundant experience and observational literature demonstrating the safety and efficacy of these drugs well beyond twelve weeks and Qysmia is a combination medication with phentermine in it which. If that is safe long term, phentermine alone must be too
The best weight loss med for patients who also have PCOS
Metformin
Obesity medications to avoid in patients with Glaucoma
Phentermine
Bupropion
Effect of Naltrexone on POMC
Prevention of autoinhibition of POMC
Use of Bupropion for weight loss without mental health indication
Off label cuz not FDA approved.
Have been studies that show about 10% weight loss
Mechanism of Phentermine
Reduced reuptake of catecholamines (mainly norepinepherine from hypothalamus)
Activates POMC
Most common side effects with Loracaserin? Rare but severe adverse reactions?
Headache and dizziness
Suicidal ideation/worsening depression, priapism, hypoglycemia when combined with insulin, and possibly increased risk of valvular regurg (debatable)
Mechanism of action for Topiramate
GABA receptor modulator
Weight loss med(s) which effect norepinepherine levels
Phentermine
Bupropion
Contrave dosing
Naltrexone-Bupropion 8 mg-90 mg ER in each tab.
Titrate number of tabs, not the dose.
1 AM x 7 days –> 1 AM 1 PM x7 days –> 2 AM 1 PM x 7 days –> 2 AM 2 PM x 7 days
Med that should not be used in a patient at risk for abrupt opioid or alcohol withdrawal
Contrave/Bupropion due to lower seizure threshold
But substance abuse is really a relative contraindication for all the weight loss meds
Trade name of Pranlintide
Symlin
Mechanism of Pranlintide (Symlin)
Amylin which Antagonize glucagons action in the liver
Diabetic medication with some weight loss
Generally speaking, you can expect this % of weight loss with a weight loss medication
8-15% (this number doesn’t have placebo effect removed)
Weight loss med(s) which effect dopamine levels
Bupropion
Zonisamide
What is the most commonly used weight loss medication?
Phentermine
Contraindications for Saxenda/Liraglutide
Medullary Thyroid Cancer, personal or family history of MEN, history of pancreatitis
This medication used off label for weight lose is also sometimes used off label for tremor
Topiramate
Contraindications to Orlistat
Pregnancy, Malabsorptive syndromes, severe liver disease, history of oxalate kidney stones, and cholestasis
This medication should be taken in the morning
Phentermine
Expected weight loss for Phentermine?
Don’t have specific numbers for expected weight loss as it was only studied for short term, but appears to be in the ball park of other medications
Mechanism of Zonisamide
Activation of serotenergic and dopaminergic pathways
Risk Evaluation and Mitigation Strategy’s (REMS) is required for which meds
Saxenda (Pancreatitis and MEN1)
Qysmia (teratogenic)
Really optional not required
Saxenda adverse effects
Nausea and vomiting common (about 40%)
Can have other GI side effects too such as abdominal pain, diarrhea/constipation …
Headache and dizziness less common
Rare but severe side effects include medullary thyroid cancer and pancreatitis
Dosages and formulations of Belviq
Don’t titrate. Either get 10mg of Belviq (immediate release) BID or 20mg ER QD of Belviq XR
Preferred weight loss med for obese patient with depression
Bupropion
Can’t use Lorcaserin/Belviq if already on another depression Med
Which FDA approved weight loss medication is probably the safest overall
Orlistat. Longer studies, less significant side effects, and fewer contraindications
Mechanism of action for Loracaserin
Selective serotonin 5-HT2C receptor agonist in the hypothalamus promoting satiety —> activates POMC
Fenfluramine was non-selective
What medication is FDA approved for treating bulimia
Fluoxetine is FDA approved, while all SSRIs are effective
Topamax and Trazadone are used off label to treat
Phentermine adverse reactions
Dry mouth (weak anticholinergic), Insomnia, palpitations, hypertension, tachycardia, and headaches (can worsen underlying migraines)
This medication is probably the least well tolerated
Orlistat
Only medication FDA approved for use in Binge Eating Disorder with obesity? Other options?
Lisdexamfetamine (FDA approved)
Topamax or Zonisamide (antiepileptic)
This currently available medication is most similar to Fenfluramines mechanism of action
Lorcaserin/Belviq (is more selective than fenlfuramine)
Phentermine was in combo with fenfluramine, but works differently
This is the only weight loss medication that is safe to use during pregnancy
Metformin
Timing of taking weight loss meds with and without food
Orlistat is with food
Others doesn’t matter
Outcome changes with weight loss medications
Opponents of the use of weight loss meds argue that the studies on these meds have flaws including short duration, lack of head to head comparison, high attrition rates, and inadequate reporting of clinical outcomes such as cardiovascular outcomes. However, there is data to show clinically significant changes in BP, Lipids, HbA1c etc with many of the obesity medications.
Bupropion mechanism
Norepi and dopamine uptake inhibitor
Activates POMC
The best weight loss med for patients who also have Seizures
Topamax
Treatment of night eating syndrome
Progressive Muscle Relaxation
Sertraline. Topamax is also an option
Obesity Medicines which can worsen BP
Bupropion/Contrave
Phentermine/Qysmia
Per FDA, you should stop obesity medications after this amount time if weight loss is < than this %?
If 5% weight loss is not achieved at 12 weeks while at max dose the drug should be discontinued for lack of effectiveness.
Weight loss medications approved for pediatric patients
Orlistat is approved for ages 12 and up
Phentermine is approved for ages 16 and up
Metformin is approved for ages 10 and up, but not for obesity alone. Need insulin resistance or PCOS for it to not be “off label”
This weight loss medication is contraindicated for patients on chronic opioids
Contrave
These medications should be used with caution in patients with a history of nephrolithiasis
Topamax
Orlistat
This medication can lessen the Euphoric effects of alcohol
Contrave/Naltrexone
