Obesity/Weight Loss Pharmacotherapy Colemen Flashcards by Rehman Hameed

who are candidates for pharmacotherapy?

BMI > or = to 30 OR BMI > or = to 27 with other risk factors (HTN, diabetes, dyslipidemia, etc) AND did not lose weight OR maintain weight with comprehensive lifestyle intervention (< 5% loss in 3-6 months of actively trying)

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initial goal for reduction of body weight: ___ to ___ % of initial weight over ___ months

5 to 10%; 6 months

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after initiating pharmacotherapy, when should we follow up?

-every month for the first 3 months of therapy
-after first 3 months, follow up every 3 months

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what class of drugs are short-term pharmacotherapy options?

a. lipase inhibitors
b. GLP-1 agonists
c. CNS stimulants
d. melanocortin receptor agonist

c. CNS stimulants

(ex. phentermine, phendimetrazine, benzphetamine, diethylpropion)

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MOA of CNS stimulants: inc conc of __________ to stimulate receptors in hypothalamus, resulting in appetite suppression

norepinephrine

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Orlistat (Xenical or Alli) is in what drug class?

a. lipase inhibitors
b. sympathomimetic/anticonvulsant
c. GLP-1 agonists
d. melanocortin receptor agonist

a. lipase inhibitors

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is Xenical (Orlistat) Rx or OTC?

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is Alli (Orlistat) Rx or OTC?

OTC

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MOA of Orlistat (3 things)

-reversibly inhibits gastric and pancreatic lipases
-dec absorption of dietary fats by ~30%
-minimally absorbed and does not work systemically

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when should Xenical or Alli (Orlistat) be taken?

within 1 hour of eating a fat-containing meal

(omit dose if meal is missed or does not contain fat)

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Xenical is approved for what age?

12 and up

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Alli is approved for what age?

18 and up

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Orlistat is suggested for pts with what disease?

CV disease

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common adverse effects of Orlistat (2)

-GI
-dec absorption of fat sol. vitamins from diet

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CIs of Orlistat (3 of them)

-pregnancy
-chronic malabsorption syndrome
-cholestasis (slow/blocked bile flow)

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Qsymia is a combo of what 2 drugs?

phentermine and topiramate ER

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what class is Qsymia in?

a. lipase inhibitors
b. sympathomimetic and anticonvulsant
c. opiod antag and dopamine/norepi reuptake inhibitor
d. melanocortin receptor agonist

b. sympathomimetic and anticonvulsant

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what drug class is Contrave in?

a. lipase inhibitors
b. sympathomimetic and anticonvulsant
c. opiod antag and dopamine/norepi reuptake inhibitor
d. melanocortin receptor agonist

c. opiod antag and dopamine/norepi reuptake inhibitor

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what two drugs make up Contrave?

naltrexone and bupropion XR

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MOA of phentermine (sympathomimetic amine)

-stimulates hypothalamus to release norepi, which stimulates the satiety center, decreasing appetite

Qsymia increases what 3 neurotransmitters to dec appetite and cravings?

-norepinephrine
-dopamine
-serotonin

what schedule controlled substance is Qsymia?

C-IV

if you are on max dose of Qsymia (15/92 mg) and 5% of baseline weight has not been lost after 12 weeks, what should you do?

gradually discontinue

do not exceed phentermine/topiramate ER 7.5/46 gm once daily with CrCl < ___ mL/min

for moderate hepatic impairment, do not exceed what dose of Qsymia once daily?

7.5/46 mg

true or false: Qsymia is not recommended in dialysis or severe hepatic impairment patients

true

what time of day should Qsymia be taken?

morning to prevent insomnia

how should Qsymia be gradually decreased?

take every other day for at least one week prior to discontinuing

true or false: Qsymia is allowed for pregnant patients

false (need to do REMS program due to teratogenicity)

dosing schedule for naltrexone/bupropion ER (Contrave)

-supplied as naltrexone 8 mg/bupropion 90 mg ER tablets -week 1 -> 1 tablet once daily in morning -week 2 -> 1 tablet BID -week 3 -> 2 tablets in morning and 1 in evening -week 4 -> 2 tablets BID

max daily dose of Contrave

4 tablets (naltrexone 32 mg/bupropion 360 mg)

Contrave can cause an inc in _____ _____

blood pressure (so wouldn't be appropriate for pt with HTN)

true or false: Contrave should be taken with a high fat meal

false

boxed warning for Contrave

suicidality

true or false: Contrave is CI in pregnancy

true

MOA of liraglutide (Saxenda) and semaglutide (Wegovy)

GLP-1 receptor agonist

boxed warning of Saxenda and Wegovy

thyroid C-cell tumors

liraglutide (Saxenda) dosing

-start at 0.6 mg daily x 1 week, inc by 0.6 mg/day every week -target dose: 3 mg/day

when to discontinue Saxenda

if 5% weight loss not achieved after 16 weeks of therapy

Wegovy dosing (probably don't need to know this)

-start at 0.25 mg once weekly for 1 month -month 2: 0.5 mg each week -month 3: 1 mg each week -month 4: 1.7 mg each week -month 5 and onward: 2.4 mg each week (target dose is 2.4 mg once weekly)

which drug is a melanocortin receptor antagonist?

setmelanotide (Imcivree)

setmelanotide (Imcivree) MOA

-melanocortin-4 (MC4) receptor agonist (these receptors in brain are involved in regulation of hunger, satiety, and energy expenditure)

which drug is used for pts with a genetic disorder in POMC, PCSK1, and LEPR genes? a. Wegovy b. Contrave c. Qsymia d. Imcivree

d. Imcivree (setmelanotide) (deficiency in these genes impair MC4 pathway)

setmelanotide (Imcivree) dosing for ages 12 and up

start at 2 mg once daily for 2 weeks, target dose is 3 mg once daily

monitoring parameters for alternative therapies

-recommended closely monitoring during initial 6 months of treatment -follow up every 4 weeks

what drug is approved for patients > 6 years of age with Bardet-Biedl syndrome (BBS), or POMC, PCSK1, or LEPR deficiency?

Imcivree (setmelanotide)

which drug should not be used in pts with hypertension? a. stimulants b. Orlistat c. Saxenda d. Contrave

d. Contrave

what are the 4 CNS stimulants? (slide 8)

-phentermine (Adipex-P or Lomaira) -phendimetrazine -benzphetamine (Regimax) -diethylpropion