Chapter 31: CNS Stimulants & ADHD Flashcards

(40 cards)

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
Modafinil [Provigil, Alertec] pharmacokinetics
Rapidly absorbed in the gastrointestinal tract​ Elimination by hepatic metabolism​ Half-life: About 15 hours​
26
Modafinil [Provigil, Alertec] ADRs
Headache​ Nausea​ Nervousness​ Diarrhea​ Rhinitis
27
Modafinil [Provigil, Alertec] drug interactions
Oral contraceptives​ Cyclosporine
28
adhd in children s/sx
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
adhd in children: management overview
Cognitive therapy​ Stimulant drugs
30
adhd in children drug therapy: cns stimulants
Methylphenidate [Ritalin, Concerta, others]​ Dexmethylphenidate [Focalin]​ Dextroamphetamine ​ Amphetamine mixture [Adderall]​ Pemoline [Cylert]
31
adhd in children drug therapy: nonstimulants
Atomoxetine​ Description and therapeutic effects​ Nonstimulant​ No potential for abuse​ Administered once a day​
32
Atomoxetine MOA
Selective inhibitor of norepinephrine reuptake
33
Atomoxetine pharmacokinetics
Plasma levels peak within 1 to 3 hours​ Metabolized in the liver
34
Atomoxetine adr
Gastrointestinal reactions​ Reduced appetite​ Dizziness​ Somnolence​ Mood swings​ Trouble sleeping
35
Atomoxetine drug interactions
Monoamine oxidase inhibitors (isocarboxazid, phenelzine)​ CYP2D6 (paroxetine, fluoxetine, quinidine)
36
Atomoxetine prep/dose
Children who weigh less than 70 kg​ Children who weigh 70 kg or more
37
adhd in children drug therapy alpha2-adrenergic agonists: Guanfacine ​
Activates presynaptic alpha2-adrenergic receptors in the brain​ Principal side effects: Somnolence, fatigue, and reduced blood pressure
38
adhd in children Drug therapy alpha2-adrenergic agonists: Clonidine
Alpha2 agonist​ Principal side effects: Somnolence, fatigue, and hypotension
39
adhd in children: Drug therapy antidepressants: Desipramine, imipramine, and bupropion
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
adhd in adults
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​