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Pharmacotherapy Flashcards

1
Q

BMI indications for rx & surg

A

Rx:
27 w complications
30

Surg:
35 w compl
40

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2
Q

Benefits of modest wt loss @ 5-10% and >10%

A

5-10%:
-improved lipds
-↓ CVD risk
-↓ BP
-↑ insulin sens & glycemic control in T2DM
-↓ progression from pre-DM to T2DM

> 10%:
-more improvement in above
-↓ NAFLD/NASH and fibrosis
-improved OSA
-joint paint/arthritic conditions
-PCOS & fertility

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3
Q

FDA-approved for LONG-term use

A

Phentermine/Topiramate ER
Naltrexone/Bupropion
Orlistat

Semaglutide
Liraglutide
Setmelanotide

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4
Q

FDA-approved for SHORT-term use

A

Phentermine & similars:
Diethylpropion
Phendimetrazine
Benphetamine

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5
Q

OFF-LABEL use AOM’s for LONG-term (7)

A

Topiramate
Zonisamide
Bupropion
Other GLP1-RA
Metformin
Amyling agonist
SGLT2 inhibitors

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6
Q

Age cutoffs

A
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7
Q

Trade names:

Orlistat

A

Xenical

Alli

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8
Q

Trade names:

Phentermine/Topiramate ER

A

Qsymia

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9
Q

Trade names:

Naltrexone/Bupropion

A

Contrave

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10
Q

Trade names:

Liraglutide

A

Saxenda

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11
Q

Trade names:

Semaglutide

A

Wegovy

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12
Q

Trade names:

Setmelanotide

A

Imcivree

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13
Q

Trade names:

Phentermine

A

Lomaira
Adipex

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14
Q

Trade names:

Diethylpropion
Phendimetrazine
Benzphetamine

A

Diethylpropion:
…Tenuate (Tenuate Dospan)

Phendimetrazine:
…Bontril

Benzphetamine
…Regimex

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15
Q

Phentermine:

Dosage
Mech
Contraind
Adverse rxns
Pharmacokinetics

A

Dosage:
-most commonly 15-37.5 mg daily
-8, 15, 30, and 37.5 mg scored capsules

Mech:
-sympathomim amine –> hypoth NE release, other CNS effects

Contraind:
-Preg
-acute CHD
-closed angle glaucoma

Adverse rxns:
**dry mouth
**MAOI, EtOH, adren nerve block
-insomnia
-brux
-palpitations
-constip
-diff urinating
-HA
-irrit
-dysphoria
-change in libido
* NO e/o addiction or withdrawal

Pharmacokinetics:
-urinary excretion (careful w renal impairment!)
-t 1/2 is 7-20 hrs

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16
Q

Randos:

Diethylpropion
Phendimetrazine
Benzphetamine

-Dosages
-Usage notes
-DEA sched
-Excretion

A

Dosages:
-D: 25 (75 ER) TID
-P: 35 (105 ER) TID
-B: 25-50 once a day, up to TID

Usage notes:
-D: TID, short acting 4-6 hrs, weaker than phen

-P: TID 1 hr before meals, sometimes AM phenT w PM phenD, weaker than phen

DEA sched:
-B: IV
-P: III

*D&P excreted by urin ?B

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17
Q

Sympathomim contrainds

A

Preg (or planning)- X
Breastfeeding- X
Current ADR
Advanced/Sx CAD
Uncontrolled HTN
Hyperthyroid
Close angle glaucoma
Severe anxiety
Uncontrolled mental health

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18
Q

Sympathomim interactions

A

MAOI <14 days
Anesthesia
Caffeine
EtOH

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19
Q

Sympathomim SE

A

Dry mouth (muc erosions 1/1000)
Dia/Const
Diff sleeping
Dz
Dysgeu
↓ libido
CNS stim –> restless
Glaucoma, IOP
HA
↑ BP
↑ HR
Palps

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20
Q

EKG alerts while on sympathomim

A

-E/o ischemia/infarct
-LBBB, esp new
-multifocal PVCs
-QTc prolongation (tx w K, Mg)
…>460 kids, 450 M, 470 F

*LAD(?) common in obesity, reversed w wt loss

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21
Q

Phentermine/Topiramate ER

Dosage
Mech
Contraind
Adverse rxns
Pharmacokinetics

A

Dosage:
-AM 3.75/23 mg x 14 d
-then ↑ to 7.5/46 mg x 12 wks
…if <3%,
↑ again to 11.25/69 mg x 14 d
-then 15/92 mg (full strength) x 12 wks
…D/C if <5% @ 12 wks, but TITRATE QOD at least 7 days bc sz risk

Mech:
-Phen is sympathomim amine
–> catechol (NE) in hypothalamus ↓ app & food intake
-Top mech unknown, possibly GABA effects on appetite and satiety or by –| CANH

Contraind:
(see individ)

Adverse rxns:
(see individ)

Pharmacokinetics:
-Phen met liver and excreted by kids
-Top excreted by kids

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22
Q

Phentermine/Topiramate ER

Contrainds

A

Sx CAD
Active mania
Uncontr HTN
Closed angle glaucoma
Preg
Ca ox kid stones
MAOI in past 14 days

** monitor for preg w monthly UPT and document 2 FORMS of contraception

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23
Q

EKG alerts while on sympathomim

A

-E/o ischemia/infarct
-LBBB, esp new
-multifocal PVCs
-QTc prolongation (tx w K, Mg)
…>460 kids, 450 M, 470 F

*LAD(?) common in obesity, reversed w wt loss

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24
Q

Phentermine/Topiramate ER

Adverse rxns

A

Common:
Paresthesias
Dysgeusia
Dz
Insom
Constipation
Dry mouth
Attn disturbance

Serious:
*nephrolithiasis
metbolic acidosis
acute angle closure glaucoma
Depression & SI

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25
Q

Orlistat:

Dosage
Mech
Contraind
Adverse rxns
Pharmacokinetics

A

Dosage:
-60-120 TID w meals

Mech:
-Lipase inh –| 30% fat abs

Contraind:
-Preg
-Chronic malabs
-Cholestasis

Adverse rxns:
-diarrhea, oily stools
-fecal incont
-RARE hepatotox
-fat sol vit def
-↑ urinary oxalate

Pharmacokinetics:
-likely mainly within GI wall
-minimal systemic absorption

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26
Q

Naltrexone/Bupropion HCL ER

Dosage
Mech
Contraind
Adverse rxns
Pharmacokinetics

A

Dosage:
-8/90 mg, Titrate up over 4 wks
1. 1 AM
2. 1 AM + 1 PM
3. 2 AM + 1 PM
4. 2 + 2
-D/C if <5% wt loss @ 12 wks

Mech:
-Natrexone is opioid antag
-Bup: weak –| reuptake of NE & DA
-both may work in hypoth & mesolimp/DA circuit to ↓ app & reward

Contraind:
-Uncontrolled HTN
-Sz d/o
-AN / bulimia
-abrupt d/c of EtOH, benz/barbs, anti-eps
-chronic opiod use
-MAOI within 14 d

Adverse rxns:
-Bup & metabs –| CYP2D6
-N/V
-constip
-HA
-dz
-insomnia
-dry mouth
-diarrhea

SERIOUS:
-worsening depression & SI
-hepatotoxicity
-sz

Pharmacokinetics:
-Bup: ext metabolized into active metabolites, 87% metabs excreted by kids
-Nal: excreted by kids

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27
Q

Liraglutide & Semaglutide:

Dosage
Mech
Contraind
Adverse rxns
Pharmacokinetics

A

Dosage (for obesity):
Lira: 3 mg daily
Sema: 2.4 mg WEEKLY

Mech:
-hypothalamus ↓ intake, ↑ satiety
-improves glucose metab
-?↓ gastric emptying

Contraind:
-med thyr CA (black box lira)
-MEN2
-preg

Adverse rxns:
** acute pancreatitis
** acute gb dz (?2/2 wt loss)
** hypoglycemia esp. w insulin/secretagogues
** suicidal
** N/V –> AKI ** hydrate
-C/D
-HA
-dz
-fatigue
-↑ HR
-dyspepsia / abd pain
-↑ lipase
-high fat foods –> nausea

Pharmacokinetics:
Lira:
-SC lira only 55% bioavailable
-endog metab, no specific organ
-intact lira not excreted

Sema:
-SC sema 89% bioavail
-metab following proteolytic cleavage, beta ox of FA sidechain
-98% bound to alb
-excr via urine and feces

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28
Q

Lira dosing

A

Over 5 wks:
… 0.6 mg x 7 d
… +0.6 mg per wk
… 3 mg maintenance dose

Consider D/C if <4% wt loss @ 16 wks

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29
Q

Sema dosing

A

Over 5 MONTHS:
…0.25 mg x 4 wks
…then 0.5, 1.0, 1.7, 2.4 maint

If 2.4 not tol, decrese to 1.7 for up to 4 wks. If 2.4 still not tolerated then D/C

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30
Q

Setmelanotide:

Dosage
Mech
Contraind
Adverse rxns
Pharmacokinetics

A

Dosage: (DAILY SC)
6-11 yo:
1 mg x 2 wks
…titrate to 2 mg

12-adult:
2 mg x 2 wks
…titrate to 3 mg

Mech:
–> MC4R pathway in pts w def in POMC, PCSK-1, LEPR
… ↓ hunger, ↑ EE

Contraind:
none
d/c in preg unless ben>risk?

Adverse rxns:
-spont erection
-Depr & SI
-** skin pigmentation & darkening of nevi
-most commonly: inj site pain & pig, GI (n/v/d/pain), HA, back pain, fatigue

Pharmacokinetics:
-T 1/2 11 hrs
-broken down into smaller peptides, 39% excr unchnaged in urine

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31
Q

Topiramate (off label)

Dosage
Mech
Contraind
Adverse rxns
Pharmacokinetics

A

Dosage:
25-200 daily split BID (titrated up)

Mech:
-enhances GABA activity

Contraind:
-preg (CLEFT PALATE)
-closed angle glaucoma

Adverse rxns:
-attn difficulty
-mem loss
-paresthesias
-fatigue
-somnol
-acute angle closure glauc
-KIDNEY STONES
-dysgeusia
-depr & SI
-↓ bone min density
-??typo MAOI, EtOH, adre nerve block

Pharmacokinetics:
-adjust dose for renal, liver impairment, or elferly

32
Q

Zonisamide (off label)

Dosage
Mech
Contraind
Adverse rxns
Pharmacokinetics

A

Dosage:
25-100 NIGHTLY (can incr wkly by 25)

Mech:
-stabilizes Na & Ca channels

Adverse rxns:
-similar to Top

Pharmacokinetics:
-avoid in renal impairment

33
Q

Bupropion (off label)

Dosage
Mech
Contraind
Adverse rxns
Pharmacokinetics

A

Dosage: (titrated up)
150-450 XR daily
100-200 SR QD-BID
100 IR QD-TID

Mech:
-Bup: weak –| reuptake of NE & DA
-may work in hypoth & mesolimp/DA circuit to ↓ app & reward

Contraind / Adverse rxns:
-May lower sz threshold!
–| CYP2D6, drug interactions

Pharmacokinetics:
-Bup: ext metabolized into active metabolites
-87% metabs excreted by kids

34
Q

Lower dose GLP1-R1

A

Lira @ 1.8 /d (max 2)
Sema @ 1 /wk (max 2.4)
ORAL Sema 14 mg /d
Dula @ 4.5 sq/wk

-high fat foods –> nausea

35
Q

Metformin

Dosage
Mech
Contraind
Adverse rxns
Pharmacokinetics

A

Dosage:
-500-2000 daily
-us. 1000 BID or 2000 XL daily

Mech:
–> AmpK
↓ gluconeo in liver
↑ mm glucose uptake
?alter gut ubiome

Contraind:
-GFR < 30 (caution 30-45)

Adverse rxns:
-Nausea
-Cramping
-other GI
-B12 deficiency
…Ca supp, low fat foods may ↓ side effects

Pharmacokinetics
-adjust dose for renal/hep impairment, elderly

36
Q

Amylin mimetic
(Pramlinitide)

Dosage
Mech
Contraind
Adverse rxns
Pharmacokinetics

A

Dosage: **SUBQ
T1DM- 15 ug before meals
…+15 every 3 days
…50 ug TIDAX

T2DM- 60 ug before meals x 3d
…then 120 ug TIDAC

Mech:
-delayed gastric empt
-↓ post-prandial gluconeo
-↓ app centrally

Contraind

Adverse rxns:
-N/V
-hypoglycemia… **reduce insulin before meals 50%!
-HA
-inj site rxn
-pancreatitis

Pharmacokinetics:
-peaks @ 20 min
-lasts 3 hrs

37
Q

SGLT2 inhibitors

Dosage
Mech
Contraind
Adverse rxns
Pharmacokinetics

A

Dosage:
-Cana 100-300
-Dapa 5-10
-Empa 10-25

Mech:
↑ renal glucose excretion

Contraind:
-not rec for GFR <30-45

Adverse rxns:
-gu fungal infxn
-phimosis
-nec fasc
-limb amputations
-↑ thirst
-↑ UOP
-DKA
-hypoglycemia w other meds

38
Q

Weight loss:

(avg %bw lost, >= 5%, >=10%)

Phentermine

Phentermine/Topiramate ER
Naltrexone/Bupropion
Orlistat

Semaglutide
Liraglutide
Setmelanotide

Gelesis

A

Phen:
*most cost effective tx
-7.4% but variable
-49-82% (>5%)
-16-76% (>10%)

Phentermine/Topiramate ER:
-10.9% on full dose 15/92 (~1/2 on 1/2 dose)
-67% (>5%)
-47% (>10%)

Naltrexone/Bupropion:
-5.4% - 8.1%
-42-57% (>5%)
-21-25% (>10%)

Orlistat:
-3.9% (2.3% @ 2 yrs)
-21% (>5%)
-12% (>10%)

Semaglutide:
-up to 14.9%!
-84.8% (>5%)
-73% (>10%)
-53.4% (>15%)

Liraglutide:
-9.2% (6.1% in preDM trial)
-62% (>5%)
-34 (>10%)

Setmelanotide:
-12.5-25.6% (n = only 10-11 pts each!)
-45-80% achieved >10% wt loss

Gelesis:
-3% wt loss
-59% (>5%)
-25% (>10%)

39
Q

DEA schedules

A

IV:
Phentermine/Topiramate ER

40
Q

Max doses

A

Phentermine:
-37.5 mg

Phentermine/Topiramate ER:
-15/92 mg

Naltrexone/Bupropion:
-4 tabs/d = 32/360

Orlistat:
-120 TID

Semaglutide
-2.4 mg WEEKLY

Liraglutide
-3 mg daily

Setmelanotide
-2 kids, 3 adults

41
Q

D/C criteria

A
42
Q

Liver metabolizes…

A
43
Q

Brain fog
Depression
Paresthesias

Contraindications

A

Topiramax
Zonisamide

44
Q

CVD
Uncontrolled HTN
Hyperthyroid

Contraindications

A

Phetermine
Phen/top
Diethylpropion

45
Q

Gastroparesis

Contraindications

A

GLP1-RA

46
Q

Glaucoma

Contraindications

A

Phen
Phen/Top
Diethylpropion

Zonisamide

47
Q

Nephrolithiasis

Contraindications

A

Topiramate
Phen/Top

Orlistat

48
Q

Sz

Contraindications

A

-no nal/bup if any h/o sz
-bup off label may lower sz threshold

-diethylpropion(?)

-Need to D/C phen/top slowly from max dose, QOD, to ↓ sz risk

49
Q

Vit D def

Contraindications

A

Orlistat

50
Q

SI risks

A

-phen/top
-top
-nal/bup (box warning)
-bup
-GLP-1 agonists
-setmelanotide

51
Q

Contraind w MAOI

A

-phen(?)
-phen/top
-nal/bup

52
Q

Common weight promoting medicines (classes)

A

Antipsychotics
Antidepressants
Sleep agents
Neuropathic agents
B-blockers
Steroids
DM meds

53
Q

Antipsychotics that promote wt gain

A

** Risperdone (14% had >7%)
Li
Quetia
Olanza
Cloza
Valproic acid
Iloperidone
Paliperidone
Divalproex
Oxycarbazepine
…Others in appendix

**Ziprasidone (7% had >7%, least in category)

… consider adding metformin or topiramate

54
Q

Antidepressants that promote wt gain

-Wt neg

A

SSRI:
*Parox
*Cital
-Escitalo
-Sertraline
-Dulox

*TCA’s:
-Amitriptyline
-Doxepin
-Imipramine

MAOI
-Isocarboxazid
-Phenelzine
-Mirtazapine
-Brexipraxole

SNRI:
?*Venlafax

Wt neg:
Bup

55
Q

Anti-seizure meds that promote wt gain

-Wt neg

A

Carbemaz
Gabapentin
Valproate
Pregabalin

Wt neg:
-Lamotri
-Top
-Zonis

56
Q

Mood stab that promote wt gain

A

Li
Gabapentin
Divalproex
Valproate
Vigabatrin
Cariprizane
Carbemaz

Wt neg:
Lamotri

57
Q

Migraine meds that promote wt gain

A

Amitriptyline
Gabapentin
Paroxetine
Valproic acid
Some BB

Neg:
Top

58
Q

Sleep agents that promote wt gain

A

Mirtazepine

59
Q

Gyn med that promotes wt gain

A

Depo provera

60
Q

Hormones that promote wt gain

A

-Glucocorts
-Estrogen

Neutral:
-prog
-test (wt neg)

61
Q

Neuropathic agents that promote wt gain

A

gabapentin
pregabalin

62
Q

CV meds that promote wt gain

A

BB:
-propranolol
-atenolol
-metoprolol

Older/less lipophil CCB (edema):
-nifed
-amlo
-felo

63
Q

DM meds that promote wt gain

A

Insulin
Sulfonylureas
TZDs
Meglitinides

Neg:
-Metformin
-GLP1 ag
-SGLT2 inh
-a-glucosidase inh
-Pramlinitide

64
Q

HIV meds that promote wt gain

A

some HAART protease inh

65
Q

Chemotx that promote wt gain

A

Tamox
Cyclophos
MTX
5-FU
Aromatase inh
Corticosteroids

66
Q

Gelesis 100 (Plenity)
-wt loss
-indications
-dosing
-contraind
-precautions
-adv rxns

A

-cellulose + citric acid
-3% wt loss
-59% (>5%)
-25% (>10%)

Ind:
-BMI 25-40

Dosing:
-3 capsules TID w 16 oz water 20-30 mins before meals

Contra:
-preg

Precautions:
-absorption of other meds
-esoph anat abnL
-strictures (Crohn’s)
-GERD
-ulcers
-altered GI motility (surgeries)

Adv rxn:
-abd pain / distension
-constip
-flatulence
-diarrhea
-nausea

67
Q

Newer AOM & CVD outcomes

A

Phen/Top
Nal/Bup
Sema/Lira

All ↓ LDL, TG, A1C, and SBP
All ↑ HDL

*EXCEPT Nal/Bup ↑ SBP!!! And no change to LDL

68
Q

FDA-approved AOMs in kids for OBESITY (4)

A

“SLOP”

> = 6 yo: Setmel

> = 12 yo: Lira, LONG-term
…wt over 60 kg, BMI equ over 30 for age using Cole criteria

> = 12 yo: Orlistat, LONG-term

> = 16 yo: Phen, SHORT-term

69
Q

Other AOM uses in kids

A

ON LABEL:
Metformin & Lira:
>= 10 yo for T2DM

OFF-label:
Metformin:
-Obesity
>= 10 yo for PCOS

70
Q

AOM in pregnancy?

A

FDA-approved meds are contraindicated!

Cat X- phen, phen/top, bup/nal, phenD

71
Q

Special populations:

Depression

A

Bupropion (?1st choice)

72
Q

Special populations:

BED

A

Lisdexa (FDA approved)

Also (off-label):
Top
Dulox
Fluox
Bupropion

73
Q

Special populations:

NES

A

Sertraline
Citalo
Escitalo

74
Q

Special populations:

DM

A

Metformin
GLP1 ag
SGLT2 inh
Glucosidase inh

Weight neutral:
DPP4
Acarbose

75
Q

Special populations:

Premenstrual carbs

A

Spironolactone in latter half of cycle-2nd day menses (scant evidence)

76
Q

HIV meds that promote wt gain

A

some HAART protease inh

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