PreFi-CNS stimulants Flashcards
(59 cards)
1
Q
Psychomotor stimulants
A
- Methylxanthines
- Nicotine
- Varenicline
- Cocaine
- Amphetamine
- Methylphenidate
2
Q
Hallucinogens
A
- Lysergic Acid Diethylamide
- Tetrahydrocannabinol (THC)
- Phencyclidine (‘angel dust’)
3
Q
what are the 2 groups of CNS STIMULANTS?
A
- Psychomotor Stimulants
2. Hallucinogens
4
Q
definition:
produce profound changes in thought patterns and mood
A
hallucinogens
5
Q
Definition:
- cause excitement and euphoria
- decrease feelings of fatigue
- increase motor activity
A
psychomotor stimulants
6
Q
name Methylxanthines
A
- Theophylline: found in tea
- Theobromine: found in cocoa
- caffeine: coffee, tea, cola drinks, chocolate candy, cocoa
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
8
Q
actions in the CNS (related to coffee)
A
- 1-2 cups of coffee (100-200mg caffeine) causes a decrease in fatigue and increase mental alertness
- 12-15 cups of coffee (1.5 g caffeine) produces anxiety and tremors
- 2-5 g caffeine can stimulate the spinal cord
9
Q
can rapidly develop to the stimulating property
A
tolerance
10
Q
consists of feeling of fatigue and sedation
A
withdrawel
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
12
Q
caffeine has mild diuretic action that increases urinary output of sodium, chloride, and potassium
A
diuretic action
13
Q
stimulate secretion of hydrochloric acid
*px w/ peptic ulcers should avoid foods and beverages containing methylxanthines
A
gastric mucosa
14
Q
whats the therapeutic uses of caffeine and its derivatives
A
relax the smooth muscles of the bronchioles
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
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
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
18
Q
MOA of nicotine
A
- in low doses, nicotine causes ganglionic stimulation by depolarization
- high doses, nicotine causes ganglionic blockade
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
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
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
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
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
24
Q
*smoking cessation program
A
combines pharmacologic and behavioral therapy
*such as transdermal patch, and chewing gum
25
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
Varenicline
26
Definition:
- Widely used and highly addictive drug
- currently abused by more than 3M people in US
Cocaine
27
MOA of cocaine
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
actions of cocaine on CNS
- 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
what are actions of Cocaine in the sympathetic nervous system?
- potentiates NE action and produces 'fight or flight' syndrome
- associated w/ tachycardia, hypertension,pupillary dilation, peripheral vasoconstriction
30
what happens in hyperthermia from Cocaine?
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
what are therapeutic uses of Cocaine?
- 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
what are the pharmacokinetics of cocaine?
-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
what are adverse effects of Cocaine?
- anxiety:hypertension, tachycardia, paranoia, sweating
- cocaine + ethanol = cocaethylene (psychoactive/cardiotoxic)
- depression from withdrawal.
- toxic effects-seizures, fatal cardiac arrhythmias
34
what are the types of Amphetamine?
1. dextroamphetamine-major member
2. methamphetamine ('speed')
3. 3,4-methylenedioxymethamphetamine
35
Mechanism of action of Amphetamine
- similar to Cocaine
| - release intracellular stores of catecholamine
36
Actions of a Amphetamine on CNS
- 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
Actions of Amphetamine on Sympathetic NS:
indirectly stimulates the receptors through NE release
38
what are therapeutic uses of Amphetamine?
- Attention deficit hyperactivity disorder (ADHD)
| - Helps improve attention spans and alleviate many of the behavioral problems
39
what are the Amphetamine derivatives that give therapeutic use?
-Lisdexamfetamine -> dextroamphetamine
=prolongs attention span
-Atomoxetine=NE reuptake inhibitor
40
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
- narcolepsy
| - Catalepsy
41
Pharmacokinetics of Amphetamine is completely absorbed from the GI tract, metabolized by the liver, excreted in urine
Completely absorbed from the GI tract, metabolized by the liver, excreted in urine
-Euphoria lasts 4-6 hours
42
Adverse effects of Amphetamine on CNS
-Insomnia, irritability, weakness, dizziness, tremor, hyperactive reflexes, confusion, delirium, panic states, suicidal tendencies
43
resembles psychotic episodes associated w/ schizophrenia
"Amphetamine Psychosis"
44
overdose of amphetamine
treated w/ chlorpromazine or haloperidol
45
adverse effects on cardiovascular
palipitations, cardiac arrhythmia, hypertension, angina pain, circulatory collapse, headache, chills, excessive sweating
46
Adverse effects on GI System
anorexia, nausea, vomiting, abdominal cramps, diarrhea
47
Contraindications of Amphetamine
Not for patients w/ hypertension, cardiovascular disease, hyperthyroidism, glaucoma
48
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)
Methylphenidate
49
MOA of Methylphenidate
-Dopamine transport inhibitor and may act by increasing dopamine in the synaptic space
50
therapeutic uses of methylphenidate
- ADHD in children 6-16 years
| - narcolepsy
51
pharmacokinetics of methylphenidate and dexmethylphenidate
- readility absorbed upon oral administration
| - as capsules, transdermal patch
52
Adverse reactions of Methylphenidate
abdominal pain, nausea, anorexia, insomnia, nervousness, fever
-increase seizure frequency in seizure patients
53
Methylphenidate contraindicated in
glaucoma
54
Drug interactions of methylphenidate-
Interfere in the metabolism of warfin, phenytoin, phenobarbital, primidone, and TCA
55
Causes:
- Induce altered perceptual states reminiscent of dreams
- Visions of bright, colorful changes in the environment
- incapable of normal decision making
Hallucinogens
56
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
Lysergic Acid Diethylamide
57
Name that hallucinogen:
- Main psychoactive alkaloid in marijuana
- treat emesis, stimulate appetite
- euphoria, drowsiness, relaxation
- Decrease muscle strength and impair high-skilled motor activity
Tetrahydrocannabinol (THC)
58
Adverse effects:
- Reddening of conjunctiva
| - in high doses- psychosis
59
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.
Phencyclidine ("angel dust")
