Pharm: ADHD + Obesity Drugs!

Question 1

Methylphenidate (MPH)

Answer 1

“ritalin” - first line tx
* schedule II drug

MOA: blocks reuptake of dopamine thus increasing DA = increased DA

Types:

1. immediate acting MPH: works in 30 mins, lasts for 3-5 hours: concurrently used w/ long-acting formula
2. long-acting MPH: slower onset, longer duration of 10-12 hours

USE: ADHD, improved concentration

Adverse Effects

• Sleep disturbance
• Appetite Suppression
• Tics
• Anemias (rare)

Question 2

Dexmethylphenidate

Answer 2

“Focalin”

MOA: blocks reuptake of dopamine thus increasing DA
= increased DA

USE: ADHD, improved concentration

Adverse Effects

• Sleep disturbance
• Appetite Suppression
• Tics
• Anemias (rare)

Question 3

Dextroamphetamine

Answer 3

• second line tx ADHD
• schedule II drug

MOA: blocks reuptake of dopamine, and increase production of DA and NE by displacing natural NT’s from storage vesicles
= increased NE + DA

PK * onset w/in 1 hour, lasts for 5 hours. Twice daily administration required

*** Ascorbic acid or fruit juice ↓ absorption, sodium bicarbonate ↑ absorption

USE: ADHD, improved concentration

Adverse Effects

• Sleep disturbance
• Appetite Suppression
• Tics
• Anemias (rare)

Question 4

Adderall

Answer 4

= amphetamine mixed salt

USE: ADHD, improved concentration

Adverse Effects

• Sleep disturbance
• Appetite Suppression
• Tics
• Anemias (rare)

Question 5

Atomoxetine

Answer 5

= Non stimulant, not a controlled substance

MOA:
- NE reuptake inhibitor
- u/k mechanism increases prefrontal cortex DA
= increased NE

USE: ADHD, improved concentration — but less effective overall!

Adverse Effects

• Sleep disturbance
• Appetite Suppression
• Tics
• Anemias (rare)

** Greatest value is for patients who have not responded to or cannot tolerate stimulants, especially those with low weight, short stature who refuse treatment with a controlled substance

Question 6

ADHD criteria?

Answer 6

EITHER: 6 or more symptoms of

1. Inattention and/or
2. Hyperactivity & Impulsivity

AND

• Onset before age 12 years
• Impairment in at least 2 Settings (i.e., at school and at home)
• Impairment in social, academic or occupational function
• No other pervasive disorder

NOTE: Effective management of ADHD significantly decreases risk for substance abuse

Question 7

Lisdexamfetamine

Answer 7

= a prodrug of dexamphetamine with rate limited metabolism and has reduced risk of abuse, diversion, and overdose.

An oral prodrug that is converted to d-amphetamine and l-lysine by enzymatic hydrolysis. Longer duration than that of other amphetamine preparations, similar efficacy.

Cannot be crushed and then injected to get an amphetamine-like high.

Question 8

Clonidine

Answer 8

MOA: stimulates alpha2 receptors –> decreased central sympathetic output

USE: tx of tics and HTN, help manage sleep problems, aggression and ADHD

Question 9

Guanfacine

Answer 9

MOA: Stimulates alpha 2-adrenergic receptors

USE: centrally acting antihypertensive w/ modes improvement in hyperactivity

Question 10

Phentermine/Topiramate ER

Answer 10

(Phentermine) sympathomimetic amine/ antiepileptic combination (topiramate)

schedule IV substance

NOTE ;effective in producing dose-dependent w/l.. however if >5% of w/l is not achieved after 12 weeks at max dose the drug should be gradually discontinued — rapid discontinuation causes seizures!

AE: dry mouth, paresthesia, constipation, weird taste, insomnia - discontinuation rate is high d/t these SE’s

CI: pregnancy

** most efficacious w/l drug, however the average pts loss 13kg (= 28lbs)…. not so much for someone that weighs 230 lbs.

Question 11

Orlistat

Answer 11

MOA: Pancreatic and gastric lipase inhibitor - decreases absorption of fats from GI tract

moderate effect when used alongside dieting (3kg - 6 lbs??)

AE’s: limit its use - flatulence w/ discharge, oily spotting, fecal urgency

CI : pregnancy

Question 12

Lorcaserin

Answer 12

MOA: Serotonin Receptor Agonist that suppresses appetite

Use: only modestly effective for w/l, but better tolerated
** about 50% of pts. lost around 6.6 lbs

AE: h/a, nausea, dizziness
CI: pregnancy, pts. taking MAO inhibitors, SSRI’s, SNRIs

Question 13

Bupropion/naltrexon

Answer 13

antidepressant/opioid antagonist combo

USE: antidepressant, smoking cessation, appetite suppressant (buproprion), tx of alcohol and opioid dependence, potentiates effect of appetite suppression (naltrexone) — loss of 9 -11 lbs

AE: nausea (major reason of discontinuing), vomiting, h/a, constipation, dizziness, dry mouth

Question 14

Liraglutide

Answer 14

MOA: injectable GLP-1 agonist used to tx type 2 DM

USE: loss of 12 lbs on average

AE’s: nausea, vomiting, constipation, diarrhea

black box warning: risk of thyroid C-cell tumors!!!

CI: pregnancy

Question 15

bariatric surgery

Answer 15

indicated for: patients with a BMI > 40, or a BMI > 35 with an obesity-related comorbidity.

types:
1. adjustable gastric banding = restrictive procedure w/ no assoc. malabsorption — lost 47% of excess weight in 10 years
2. sleeve gastrectomy: loss of “excess weight” was 59% over 5 years
3. Gastric bypass - mixed restrictive and malabsorptive procedure that creates a proximal pouch of stomach and anastomoses it to the limb of jejunum, thus bypassing most of stomach , duodenum and part of jejunum
* * procedure results in loss of 66% of excess weight in 2 years… but AE’s are significant!!!!

** • Sleeve gastrectomy and gastric bypass result in more weight loss than gastric banding (~70% vs. ~33%), but gastric banding is safer with lower mortality rates.