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Pharmacology > PreFi-CNS stimulants > Flashcards

PreFi-CNS stimulants Flashcards

1
Q

Psychomotor stimulants

A
  • Methylxanthines
  • Nicotine
  • Varenicline
  • Cocaine
  • Amphetamine
  • Methylphenidate
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2
Q

Hallucinogens

A
  • Lysergic Acid Diethylamide
  • Tetrahydrocannabinol (THC)
  • Phencyclidine (‘angel dust’)
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3
Q

what are the 2 groups of CNS STIMULANTS?

A
  1. Psychomotor Stimulants

2. Hallucinogens

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4
Q

definition:

produce profound changes in thought patterns and mood

A

hallucinogens

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5
Q

Definition:

  • cause excitement and euphoria
  • decrease feelings of fatigue
  • increase motor activity
A

psychomotor stimulants

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6
Q

name Methylxanthines

A
  • Theophylline: found in tea
  • Theobromine: found in cocoa
  • caffeine: coffee, tea, cola drinks, chocolate candy, cocoa
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7
Q

what is the MOA of Methylxanthines?

A
  • translocation of extracellular oalolum
  • increase in oyollo adenosine monophosphate and cyclic guanosine monophosphate caused by inhibition of phosphodiesterase
  • blockade of adenosine receptors
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8
Q

actions in the CNS (related to coffee)

A
  1. 1-2 cups of coffee (100-200mg caffeine) causes a decrease in fatigue and increase mental alertness
  2. 12-15 cups of coffee (1.5 g caffeine) produces anxiety and tremors
  3. 2-5 g caffeine can stimulate the spinal cord
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9
Q

can rapidly develop to the stimulating property

A

tolerance

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10
Q

consists of feeling of fatigue and sedation

A

withdrawel

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11
Q

Actions in cardiovascular system related to caffeine

A

-in high doses, positive inotropic and chronotropic effects

  • harmful in px w/ angina pectoris
  • can trigger premature ventricular contraction
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12
Q

caffeine has mild diuretic action that increases urinary output of sodium, chloride, and potassium

A

diuretic action

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13
Q

stimulate secretion of hydrochloric acid

*px w/ peptic ulcers should avoid foods and beverages containing methylxanthines

A

gastric mucosa

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14
Q

whats the therapeutic uses of caffeine and its derivatives

A

relax the smooth muscles of the bronchioles

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15
Q

what are the pharmacokinetics of caffeine?

A
  • well absorbed orally
  • caffeine distributes throughout the body, brain
  • cross placenta to the fetus and secreted into mother’s milk
  • metabolized in the liver by the CYP1A2 pathway
  • metabolities are excreted in the urine
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16
Q

what are adverse effects of caffeine?

A
  • moderate dose cause insomnia, anxiety, agitation
  • high dose cause toxicity manifested by emesis and convulsions
  • 10 g of caffeine (100 cups) induces arrythymias
  • 600 mg (6 cups of coffee/day) routine consumption cause lethargy, headache, irritability when suddenly stopped
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17
Q

Define:

  • Active ingredient in Tobacco
  • 2nd most widely used CNS stimulant
  • 2nd most abused drug
  • serious risk factor for lung and cardiovascular disease, cancer
  • dependency is not easily overcome
A

Nicotine

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18
Q

MOA of nicotine

A
  • in low doses, nicotine causes ganglionic stimulation by depolarization
  • high doses, nicotine causes ganglionic blockade
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19
Q

what are actions of Nicotine in CNS?

A
  • highly lipid soluble and readily crosses BBB
  • in low doses, euphoria and arousal relaxation, improves attention, learning, problem solving, reaction time, appetite suppressant
  • in high dose-central respiratory paralysis
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20
Q

what are the peripheral effects of Nicotine?

A
  • Stimulation of sympathetic ganglia and adrenal medulla increases BP and HR
  • harmful in hypertensive patients

-stimulation of parasympathetic ganglia-increase motor activity of bowel

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21
Q

what are the pharmacokinetics of Nicotine?

A
  • absorption readily occurs via mucosa, lungs, GI mucosa and skin
  • crosses placental membrane and secreted in milk
  • by inhaling tobacco, average smoker takes in 1-2mg nicotine per cigarette (most cigarette contains 6-8mg)
  • 60 mg acute lethal dose
  • > 90% of nicotine inhaled in smoke is absorbed
  • tolerance developes rapidly
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22
Q

adverse effects of Nicotine

A
  • irritability, tremors, intestinal cramps, diarrhea, increased heart rate and blood pressure
  • increase metabolism of a number of drugs
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23
Q

what are withdrawal syndrome of nicotine?

A
  • addictive and physical dependence develops rapidly and can be severe
  • characterized by irritability, anxiety, restlessness, difficultly concentrating, headaches, and insomnia, appetite is affected, GI pain
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24
Q

*smoking cessation program

A

combines pharmacologic and behavioral therapy

*such as transdermal patch, and chewing gum

25
Q

definition:

  • a partial agonist at neuronal nicotinic acetylcholine receptors in the CNS
  • useful as adjunct in the management of smoking cessation in patients w/ withdrawal symptoms
A

Varenicline

26
Q

Definition:

  • Widely used and highly addictive drug
  • currently abused by more than 3M people in US
A

Cocaine

27
Q

MOA of cocaine

A

blockade of reuptake of monoamines (NE, serotin, dopamine) into presynaptic terminals, thus prolonging its actions

thus producing intense euphoria (limbic system)

-chronic intake depletes dopamine leading to craving of more

28
Q

actions of cocaine on CNS

A
  • stimulation of cortex and brainstem
  • acutely increases mental awareness and produces feeling of wellbeing and euphoria
  • like amphetamine, can produce hallucinations, and delusions of paranoia or grandiosity
  • increase motor activity
29
Q

what are actions of Cocaine in the sympathetic nervous system?

A
  • potentiates NE action and produces ‘fight or flight’ syndrome
  • associated w/ tachycardia, hypertension,pupillary dilation, peripheral vasoconstriction
30
Q

what happens in hyperthermia from Cocaine?

A

death can result not only as a function of dose, but also from hyperthermia
*impairs sweating and cutaneous vasodilation, decreased perception of thermal discomfort

31
Q

what are therapeutic uses of Cocaine?

A
  • local anesthetic
  • cocaine is applied topically as a local anesthetic during eye, nose, and throat surgery
  • is the ONLY local anesthetic that causes vasoconstriction -> necrosis and perforation of nasal septum (cocaine powder inhalation)
32
Q

what are the pharmacokinetics of cocaine?

A

-often self-administered by chewing, intranasal snorting, smoking, Iv injections

  • peak effect 15-20 min and the “high” disappears in 1-1.5 hrs (powder)
  • Iv injection or by smoking (crack), rapid but shortlived effects
33
Q

what are adverse effects of Cocaine?

A
  • anxiety:hypertension, tachycardia, paranoia, sweating
  • cocaine + ethanol = cocaethylene (psychoactive/cardiotoxic)
  • depression from withdrawal.
  • toxic effects-seizures, fatal cardiac arrhythmias
34
Q

what are the types of Amphetamine?

A
  1. dextroamphetamine-major member
  2. methamphetamine (‘speed’)
  3. 3,4-methylenedioxymethamphetamine
35
Q

Mechanism of action of Amphetamine

A
  • similar to Cocaine

- release intracellular stores of catecholamine

36
Q

Actions of a Amphetamine on CNS

A
  • Combination of dopamine and NE release enhancing properties
  • stimulates the entire cerebrospinal axis, cortex, brainstem, and medulla
  • increased alertness, decreased fatigue, depressed appetite, insomnia
37
Q

Actions of Amphetamine on Sympathetic NS:

A

indirectly stimulates the receptors through NE release

38
Q

what are therapeutic uses of Amphetamine?

A
  • Attention deficit hyperactivity disorder (ADHD)

- Helps improve attention spans and alleviate many of the behavioral problems

39
Q

what are the Amphetamine derivatives that give therapeutic use?

A

-Lisdexamfetamine -> dextroamphetamine
=prolongs attention span

-Atomoxetine=NE reuptake inhibitor

40
Q

Sleep disorder characterized by uncontrollable bouts of sleeping during the day

*sometimes accompanied by loss in muscle control and paralysis brought on by strong emotions such as laughter

A
  • narcolepsy

- Catalepsy

41
Q

Pharmacokinetics of Amphetamine is completely absorbed from the GI tract, metabolized by the liver, excreted in urine

A

Completely absorbed from the GI tract, metabolized by the liver, excreted in urine
-Euphoria lasts 4-6 hours

42
Q

Adverse effects of Amphetamine on CNS

A

-Insomnia, irritability, weakness, dizziness, tremor, hyperactive reflexes, confusion, delirium, panic states, suicidal tendencies

43
Q

resembles psychotic episodes associated w/ schizophrenia

A

“Amphetamine Psychosis”

44
Q

overdose of amphetamine

A

treated w/ chlorpromazine or haloperidol

45
Q

adverse effects on cardiovascular

A

palipitations, cardiac arrhythmia, hypertension, angina pain, circulatory collapse, headache, chills, excessive sweating

46
Q

Adverse effects on GI System

A

anorexia, nausea, vomiting, abdominal cramps, diarrhea

47
Q

Contraindications of Amphetamine

A

Not for patients w/ hypertension, cardiovascular disease, hyperthyroidism, glaucoma

48
Q

Definition:
Has CNS stimulant properties similar to amphetamine and may also lead to abuse
-one of the most prescribed medications for children
-treatment of ADHD (6M children)

A

Methylphenidate

49
Q

MOA of Methylphenidate

A

-Dopamine transport inhibitor and may act by increasing dopamine in the synaptic space

50
Q

therapeutic uses of methylphenidate

A
  • ADHD in children 6-16 years

- narcolepsy

51
Q

pharmacokinetics of methylphenidate and dexmethylphenidate

A
  • readility absorbed upon oral administration

- as capsules, transdermal patch

52
Q

Adverse reactions of Methylphenidate

A

abdominal pain, nausea, anorexia, insomnia, nervousness, fever
-increase seizure frequency in seizure patients

53
Q

Methylphenidate contraindicated in

A

glaucoma

54
Q

Drug interactions of methylphenidate-

A

Interfere in the metabolism of warfin, phenytoin, phenobarbital, primidone, and TCA

55
Q

Causes:

  • Induce altered perceptual states reminiscent of dreams
  • Visions of bright, colorful changes in the environment
  • incapable of normal decision making
A

Hallucinogens

56
Q

Name the hallucinogen:

  • Serotonin (5HT) agonist activity at presynaptic 5HT1 receptor in the midbrain, and it stimulates 5-HT2 receptors
  • Activation of SNS-mydriasis, hypertension,piloerection, increase body temperature
  • Induce hallucinations, mood alteration
A

Lysergic Acid Diethylamide

57
Q

Name that hallucinogen:

  • Main psychoactive alkaloid in marijuana
  • treat emesis, stimulate appetite
  • euphoria, drowsiness, relaxation
  • Decrease muscle strength and impair high-skilled motor activity
A

Tetrahydrocannabinol (THC)

58
Q

Adverse effects:

A
  • Reddening of conjunctiva

- in high doses- psychosis

59
Q

Name the hallucinogen:

  • Inhibits reuptake of dopamine, serotonin, and NE
  • produce hypersalivation
  • insensitivity to pain w/o loss of consciousness
  • numb extremities, staggered gait, slurred speech and muscular rigidity
  • at increased doses-anesthesia, stupor, coma but with eyes OPEN.
A

Phencyclidine (“angel dust”)

Pharmacology (5 decks)

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