Chapter 31: CNS Stimulants & ADHD Flashcards

1
Q

CNS stimulants

A

Increase the activity of central nervous system (CNS) neurons​

Enhance neuronal excitation; a few suppress neuronal inhibition​

In sufficient doses, all can cause convulsions​

Limited clinical applications -Limited to ADHD, narcolepsy, hyperactivity dz

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2
Q

amphetamines chemistry

A

Dextroamphetamine and levoamphetamine​

Amphetamine​

Lisdexamfetamine​

Methamphetamine

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3
Q

amp MOA

A

Release norepinephrine​

Release dopamine

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4
Q

amp pharm effects

A

CNS​

Cardiovascular system

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5
Q

amp tolerance

A

With regular use, tolerance develops to elevation of mood, suppression of appetite, and stimulation of the heart and blood vessels

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6
Q

AMP physical dependence and abuse

A

Physical dependence​
Abstinence syndrome with abrupt withdrawal​

Abuse​
High potential for abuse due to euphoria​

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7
Q

amp ADR

A

CNS stimulation​

Weight loss​

Cardiovascular effects​

Psychosis

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8
Q

amp acute toxicity

A

Dizziness, confusion, hallucinations, paranoid delusions, palpitations, dysrhythmias, and hypertension​

Death is rare​

Fatal overdose: Convulsions, coma, and cerebral hemorrhage

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9
Q

amp acute tox tx

A

Hallucinations: Chlorpromazine​

Hypertension: Alpha-adrenergic blocker (e.g., phentolamine); chlorpromazine helps lower blood pressure​

Seizures: Diazepam​

Acidifying the urine can accelerate amphetamine excretion​

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10
Q

amp therapeutic uses

A

ADHD​

Narcolepsy​

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11
Q

amp preps

A

Dextroamphetamine sulfate​
Immediate release​
Extended release​

Amphetamine/dextroamphetamine mixture​
Immediate release​
Extended release​

Lisdexamfetamine [Vyvanse]​

Methamphetamine [Desoxyn]​

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12
Q

Methylphenidate and Dexmethylphenidate​

A

Nearly identical in structure and pharmacologic actions​

Pharmacology of both drugs nearly identical to that of amphetamines

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13
Q

methylphenidate

A

ADHD and narcolepsy​

Trade names ​

Ritalin, Metadate, Methylin, Concerta, and Daytrana​

50:50 mixture of dextro and levo isomers

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14
Q

methylphenidate prep

A

Immediate release​
Ritalin and Methylin​

Sustained release​
Ritalin SR, Metadate ER, and Quillivant XR​

Once-daily dosing​
Concerta, Metadate CD, Ritalin LA, Daytrana, and Biphentin (Canadian)​

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15
Q

Dexmethylphenidate [Focalin]​

A

Drug for ADHD​

Dextro isomer of methylphenidate​

50:50 mixture of dextro and levo isomers​

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16
Q

methyl xanthines

A

Derivatives of xanthine​

Caffeine​
Few clinical applications​
Widespread ingestion for nonmedical purposes​

Dietary sources​
Chocolate​
Soft drinks​
Coffee​

Typically consumption. Is an 200 mg/day​

Adults can have type consumption 400 mg/day

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17
Q

ex of caffeine

A

Brewed coffee 96 mg​

Instant coffe 62 mg ​

Expression 1 oz 64 mg ​

Black tea 47 mg​

Green tea 28 mg ​

Cola is 22 mg​

Energy drink 8 ox 29 mg ​

1 oz energy short 215 mg ​

18
Q

methylzanthine MOA

A

Reversible blockade of adenosine receptors​

Calcium permeability​

Accumulation of cyclic adenosine monophosphate​

19
Q

methylzanthine dosage effects

A

Low doses​
Decrease drowsiness and fatigue ​
Increase capacity for prolonged intellectual exertion​

Increasing doses​
Nervousness, insomnia, and tremors​

Seizures with very large amounts​

20
Q

methrylxanthine pharm effects

A

CNS: hyperactivity, irritability​

Heart: palpitations ​

Blood vessels: HTN ​

Bronchi: SOB ​

Kidney: increased urination​

Reproduction

21
Q

methylxanthine pharmcakinetics

A

Readily absorbed from the gastrointestinal tract​

Achieve peak plasma levels within 1 hour​

Eliminated by hepatic metabolism

22
Q

methylxanthine therapeutic uses

A

Neonatal apnea​

Promoting wakefulness​

Other applications

23
Q

methylxanthine acute tox

A

Stimulation of the CNS​

Tachycardia​

Respiratory stimulation​

Sensory phenomena

24
Q

Modafinil [Provigil, Alertec] uses

A

Promotes wakefulness​

Narcolepsy​

Shift-work sleep disorder​

Obstructive sleep apnea/hypopnea syndrome​

25
Q

Modafinil [Provigil, Alertec] pharmacokinetics

A

Rapidly absorbed in the gastrointestinal tract​

Elimination by hepatic metabolism​

Half-life: About 15 hours​

26
Q

Modafinil [Provigil, Alertec] ADRs

A

Headache​

Nausea​

Nervousness​

Diarrhea​

Rhinitis

27
Q

Modafinil [Provigil, Alertec] drug interactions

A

Oral contraceptives​

Cyclosporine

28
Q

adhd in children s/sx

A

Inattention​

Hyperactivity​

Impulsivity​

Fidgety​

Unable to concentrate

Unable to wait his or her turn​

Switches excessively from one activity to another​

Calls out excessively in class​

Present before the age of 7 years​

Present for at least 6 months

29
Q

adhd in children: management overview

A

Cognitive therapy​

Stimulant drugs

30
Q

adhd in children drug therapy: cns stimulants

A

Methylphenidate [Ritalin, Concerta, others]​

Dexmethylphenidate [Focalin]​

Dextroamphetamine ​

Amphetamine mixture [Adderall]​

Pemoline [Cylert]

31
Q

adhd in children drug therapy: nonstimulants

A

Atomoxetine​

Description and therapeutic effects​
Nonstimulant​
No potential for abuse​
Administered once a day​

32
Q

Atomoxetine MOA

A

Selective inhibitor of norepinephrine reuptake

33
Q

Atomoxetine pharmacokinetics

A

Plasma levels peak within 1 to 3 hours​

Metabolized in the liver

34
Q

Atomoxetine adr

A

Gastrointestinal reactions​

Reduced appetite​

Dizziness​

Somnolence​

Mood swings​

Trouble sleeping

35
Q

Atomoxetine drug interactions

A

Monoamine oxidase inhibitors (isocarboxazid, phenelzine)​

CYP2D6 (paroxetine, fluoxetine, quinidine)

36
Q

Atomoxetine prep/dose

A

Children who weigh less than 70 kg​

Children who weigh 70 kg or more

37
Q

adhd in children drug therapy alpha2-adrenergic agonists: Guanfacine ​

A

Activates presynaptic alpha2-adrenergic receptors in the brain​

Principal side effects: Somnolence, fatigue, and reduced blood pressure

38
Q

adhd in children Drug therapy alpha2-adrenergic agonists: Clonidine

A

Alpha2 agonist​

Principal side effects: Somnolence, fatigue, and hypotension

39
Q

adhd in children: Drug therapy antidepressants: Desipramine, imipramine, and bupropion

A

Tricyclic antidepressants​
Desipramine [Norpramin] and imipramine [Tofranil]​
Decrease hyperactivity​
Little effect on impulsivity and inattention​

Second-line drugs​
Bupropion [Wellbutrin]​
Can reduce behavioral symptoms​
Less effective than stimulants​
Poses risk of seizure​
Second-line drug​

40
Q

adhd in adults

A

60% of ADHD cases persist into adulthood​

Symptoms​
Poor concentration​
Stress intolerance​
Antisocial behavior​
Outbursts of anger​
Inability to maintain a routine​

Drug therapy​
Methylphenidate​