Central Nervous System Stimulants and Related Drugs Flashcards
(37 cards)
Central Nervous System Stimulants
- Drugs that stimulate a specific area of the brain or spinal cord
- Neurons contain receptors for excitatory neurotransmitters, including dopamine (dopaminergic drugs), norepinephrine (adrenergic drugs), and serotonin (serotonergic drugs).
- Sympathomimetic drugs
Classification
Classification according to:
- chemical structural similarities: amphetamines, serotonin agonists, sympathomimetics, and xanthines.
- site of therapeutic action in the CNS
- Major therapeutic uses: anti-attention-deficit/hyperactivity disorder, anti-narcoleptic, anorexiant, anti-migraine, analeptic drugs
Attention-deficit hyperactivity disorder
Most common neurodevelopmental disorder in children, affecting 3 to 10% of school-age children
Boys affected two to nine times more often than girls are
- May be related to the underdiagnosing in girls
Attention-Deficit Hyperactivity Disorder symptoms?
Primary symptom of attention-deficit/hyperactivity disorder (ADHD): inappropriate ability to maintain attention span, or hyperactivity and impulsivity. Drug therapy for both childhood and adult ADHD is the same.
Narcolepsy
- Incurable neurological condition in which patients unexpectedly fall asleep in the middle of normal daily activities.
- Cataplexy: sudden acute skeletal muscle weakness
—- Triggered by strong emotion - Commonly knees buckle, and the individual falls to the floor while still awake.
Obesity
- Approximately 7 million obese adults and
600 000 obese school-aged children in Canada - Associated health risks
- Expected to rise 4 to 5 % per year
Migraine
Common type of recurring headache, usually lasting from 4 to 72 hours
Typical features: pulsatile quality with pain that worsens with each pulse
Most commonly unilateral but may occur on both sides of the head
Associated symptoms: nausea, vomiting, photophobia (patient avoids light), phonophobia (patient avoids sounds)
Aura
Drugs for ADHD and Narcolepsy
- Amphetamines: methylphenidate (Ritalin)
- Nonamphetamine stimulant
(Modafinil) - Nonstimulant drugs
(atomoxetine; also used to treat ADHD)
lisdexamfetamine (Vyvanse®): prodrug for dextroamphetamine
Mechanism of Action and Drug Effects - Amphetamines
Stimulate areas of the brain associated with mental alertness
Mechanism of Action and Drug Effects - CNS effects
- Mood elevation or euphoria
- Increased mental alertness and capacity for work
- Decreased fatigue and drowsiness
- Prolonged wakefulness
Mechanism of Action and Drug Effects - Respiratory effects
- Relaxation of bronchial smooth muscle
- Increased respiration
- Dilation of pulmonary arteries
Common Adverse Effects
Common adverse effects include:
- Palpitations, tachycardia, hypertension, angina, anxiety, insomnia, headache, tremor, nausea, vomiting, diarrhea, dry mouth, increased metabolic rate, others
Common Adverse Effects
- Wide range; dose related
- Tend to “speed up” body systems
Principal Drugs Used to Treat ADHD and Narcolepsy
Atomoxetine: nonstimulant drug also used for ADHD
Amphetamines
amphetamine aspartate (Adderall®): one of the most commonly prescribed drugs for ADHD
atomoxetine hydrochloride (Strattera®)
- Approved for treating ADHD in children older than 6 years of age and in adults
- Health Canada has issued a warning describing cases of suicidal thinking and behaviour in small numbers of adolescent patients receiving this medication.
methylphenidate hydrochloride (Ritalin®) does what?
First prescription drug indicated for ADHD
Also used for narcolepsy
modafinil (Alertec®)
- Use: improvement of wakefulness in patients with excessive daytime sleepiness associated with narcolepsy and with “shift work” sleep disorder
- Less potential for misuse than amphetamines and methylphenidate
- Available with a prescription
what does Anorexiants
- Used to treat obesity
- Effectiveness has not been proven
- None currently available in Canada to treat obesity
- Related drug, orlistat (Xenical®), a nonstimulant drug to treat obesity
Adverse Effects of Orlistat
- Headache
- Upper respiratory infection
- Gastrointestinal (GI) distress, fecal incontinence
Antimigraine Drugs
Antimigraine (serotonin agonists; also called triptans)
- sumatriptan (Imitrex®)
Antimigraine Drugs - Ergot alkaloids
- Were the mainstay of treatment of migraine headaches but have been replaced by the triptans for first-line therapy
- Obtained from a fungus and cause vasoconstriction of blood vessels in the brain and carotid arteries
Mechanism of Action and Drug Effects - Triptans
Stimulate 5-HT receptors in cerebral arteries, causing vasoconstriction and reducing headache symptoms
Reduce the production of inflammatory neuropeptides
Mechanism of Action and Drug Effects - Ergot alkaloids
Constrict or narrow blood vessels in the brain