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811 > Lecture 43 > Flashcards

Lecture 43 Flashcards

Indirect Acting Agonists

1
Q

Amphetamines

A
  • CII
  • Amphetamine, Dextroamphetamine, Methamphetamine
  • Non-catecholaminic sympathomimetic agents
  • Stimulates cate. release (displaces from vesicles)
  • Inhibits reuptake (completes with cate. pumps)
  • Affects NE and DA in CNS and PNS
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2
Q

Adderall

A
  • Onset: 30-60 minutes, half life: 6-10 hours
  • Equivalent amount of mixed amphetamine salt combos
  • XR: once daily
  • Black box: high potential for abuse, can cause sudden death or severe CV reactions
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3
Q

Adderall Uses

A
  1. ADHD
  2. Short-term Obesity
  3. Narcolepsy
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4
Q

ADHD

A
  • Children: inattention, hyperactive, impulsive
  • Adults: lack of organization and motivation
  • Genetics: 80% in twin studies
  • ADHD with comobid tics (10-35% of patients) may worsen with stimulants
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5
Q

Adderall + ADHD

A
  • Amphetamines improve attention and reduce distractability and impulsiveness
  • Avoid giving near bedtime since insomnia and anorexia can occur
  • Side effects decrease with time
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6
Q

Adderall + Obesity

A
  • Short term treatment: 3-6 weeks
  • Suppresses appetite centers of hypothalamus
  • Anorexic effects in the first few weeks (decline with time)
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7
Q

Narcolepsy

A
  • Transition from waking state to REM sleep

- Loses muscle tone (cataplexy), falls to ground, hypnogognic hallucinations

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8
Q

Lisdexamfetamine

A

-Vyvanse
-Inactive prodrug of dextroamphetamine (covalently bonded to l-lysine)
-Hydrolyzed in intestine/first pass metabolism
-Limits abuse potential when used IV/intranasally
Uses: ADHD, moderate to severe binge eating disorder (FDA approved)

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9
Q

Methamphetamine

A
  • Desoxyn, Methampex
  • CII
  • Oral
  • Uses: ADHD, exogenous obesity (short-term) when in refractory period of alternate therapy
  • Black Box: High potential for abuse, use in weight reduction only when other therapies are ineffective, can cause sudden death and severe CV reactions
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10
Q

Methylphenidate

A
  • Ritalin, Concerta, Daytrana
  • Dexmethylphenidate: D-enantiomer of methylphenidate (more active)
  • Milder peripheral actions
  • CII
  • Used in ADHD, narcolepsy, and depression or post-stroke depression (off-label)
  • *Many sustained release versions available**
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11
Q

Phentermine

A
  • Apidex-P
  • Stimlant
  • CIV
  • Increases NE and DA release, inhibits uptake
  • Used for short term obesity with dietary/behavior modifications and exercise
  • Use in obese patients with BMI>30 or >27 in the presence of other risk factors
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12
Q

Diethylpropion

A
  • Tenuate
  • Similar mechanism to amphetamine
  • CIV
  • Oral
  • Manages exogenous obesity in those not responding to other therapies
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13
Q

Bathsalts

A
  1. Crystalline, scented substances added to bath water
  2. Any of several catecholamine synthesized drugs used as stimulants and usually packages to look like cosmetics or household products
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14
Q

Ephedrine

A

-Releases endogenous NE indirectly and directly acts on B-receptors

Uses

  1. Acute bronchospasm
  2. Hypotension in spinal anesthesia/overdoses of hypotensive causing drugs
  3. Orthostatic hypotension
  4. Nasal congestion
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15
Q

Pseudophedrine

A
  • Sudafed
  • OTC, oral
  • Indirect and direct effects on alpha receptors
  • Treats nasal congestion (Cold and allergies) and prophylaxis for otitic barotrauma in air pressure changes
  • *Combat Methamphetamine Epidemic Act of 2005**
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16
Q

Nexafed

A
  • New Sudafed drug to curb meth production

- Turns into thick gel when dissolved, makes Sudafed hader to extract

17
Q

Cocaine

A
  • CII, high abuse potential
  • Euphoria
  • Reuptake inhibitor of NE, DA, 5-HT (indirect agonist)
  • General sympathetic effect: increases HR/BP
  • Local anesthetic on mucous membranes or in oral, laryngeal, and nasal cavities
  • Vasoconstrictor action that decreases bleeding
18
Q

Stimulant Contraindications

A
  • High potential for abuse, less so for CIV
  • Not recommended for those with substance abuse problems
  • Do not use in those with cardiac disease, hyperthyroidism, psychosis, and depression
19
Q

Drug Interactions with Stimulants

A
  1. Enhances other sympathomimetics (CNS and PNS)
  2. MAOIs, caution with L-DOPA
  3. May counteract some antihypertensive agents
  4. Antipsychotic drugs (D2 agonists) may block central stimulant action and decrease affects of drugs used for ADHD, narcolepsy, and appetite suppression
20
Q

Stimulant Adverse Reactions

A
  1. Anxiety, headache, insomnia (lower doses or take drug holidays to reduce these)
  2. High doses/overdoses: paranoia, psychosis, arrhythmias, seizures, coma, and death
  3. Growth inhibition in children due to decreased appetite and altered GH secretion
  4. CV: increased BP/HR
  5. Reverse tolerance (sensitization)
  6. Severe depressive symptoms, anxiety, and suicidal idealation
    * *During D/C, monitor patient and gradually reduce dose to minimize these effects**
21
Q

Modafinil

A
  • Provigil
  • Alternative narcolepsy treatment option
  • CIV, low abuse potential
  • Stimulant
  • R isomer (active) = Armodafinil
  • Minimal peripheral side effects, no tolerance development
  • Improves wakeful-ness in those with narcolepsy, obstructive sleep apnea, and shift work disorder
  • *Doesn’t cause agitation, aggression, etc.**
22
Q

Atomoxetime

A
  • Strattera
  • Treats ADHD in adults and children by blocking NE reuptake
  • Doesn’t exacerbate tics
  • Original two trials saw a 59-64% response when compared to the placebo
  • Side effect: suppressed appetite
  • Lacks abuse potential, so good for those with abuse history
23
Q

Drugs Removed from Market

A
  1. Phenylpropanolamine - D/C 2000, stroke
  2. Pemoline (Cylert) - D/C 2005, life threatening hepatic failure
  3. Sibutramine (Merdine) - D/C 2010, increased CV risks
24
Q

Drugs NOT to use with LQTS

A
  1. Amphetamine/dextroamphetamine (Adderall, Adderall XR)
  2. Dextroamphetamine (Dexedrine)
  3. Methamphetamine
  4. Methylphenidate (Ritalin, Concerta)
  5. Dexmethylphenidate (Focalin)
  6. Lisdexamfetamine (Vyvanse)
  7. Atomoxetine (Strattera)

811 (38 decks)

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