cns stimulants. l psychomotor stimulants l cause excitement & euphoria l increase motor activity...
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CNS STIMULANTS
PSYCHOMOTOR STIMULANTS CAUSE EXCITEMENT & EUPHORIA INCREASE MOTOR ACTIVITY
PSYCHOTOMIMETIC DRUGS PROFOUND CHANGES IN THOUGHT
PATTERNS AND MOOD
FEW DRUGS USED CLINICALLY IMPORTANT AS DRUGS OF ABUSE
CNS STIMULANTSCNS STIMULANTSPSYCHOMOTOR
STIMULANTS AMPHETAMINE CAFFEINE COCAINE NICOTINE METHYLPHENI
DATE METHYLXANTH
INES
PSYCHOTOMIMETIC DRUGS
LYSERGIC ACID DIETHYLAMIDE (LSD)
PHENCYCLIDINE TETRAHYDROCANN
ABINOL
METHYLXANTHINESMETHYLXANTHINES
Caffeine – found in coffee, tea, colas Theophylline – found in tea Theobromine – found in chocolate
METHYLXANTHINESMETHYLXANTHINES THEOBROMINE,THEOPHYLLINE
MECH: TRANSLOCATION OF EXTRACELLULAR CALCIUM, ↑ IN cAMP, cGMP, by inhibiting Phosphodiesterase enzyme
USES Relaxation of smooth muscle of
bronchioles. Used to treat Asthma
SE: Insomnia, anxiety, agitation
General Positive Effects increased mental alertness, wakefulness increased energy, sense of well-being Decrease fatigue
have potential for toxicities have potential for physical dependence
CNS: ↓ fatigue, ↑mental alertness CVS: + inotropic & + chronotropic ↑ diuretic action ↑ secretion of Hcl in gastric mucosa
increased respiratory drive& rate increased urine output (is a diuretic) increased HR, cardiac force, BP, dilation of
coronary arteries decreased smooth muscle activity (is a
vasodilator in peripheral blood vessels, but a vasoconstrictor of CNS blood vessels;
Opens bronchi, bronchodilator increased basal metabolic rate
Mechanisms of Action of Caffeine caffeine blocks adenosine receptors
many headache OTC drugs have caffeine in them
for vascular (migraine) headaches for diuretic for mild assist to memory, concentration,
learning for ADHD, for narcolepsy (a “poor man’s
speed”) for weight loss as a respiratory stimulant (e.g. asthma, central
sleep apnea)
Therapeutic Uses of Caffeine
daily use of caffeine can induce significant degree of tolerance and physical dependence
caffeine withdrawl Sxs: moderate to severe headache
drowsiness, fatigue, less alert, less active, lethargy
Anxiety or depression flu-like Sxs (malaise, muscle aches, abdominal
cramps, etc.) nausea, vomiting irritability
lethal dose = 10 grams caffeine/day (= 100 cups coffee)
“caffeinism” – a clinical pattern seen with caffeine OD
anxiety, agitation, severe insomnia, irritability, tachycardia, High BP, cardiac arrhythmias, severe GI disturbances, cramping, and acid reflux, tinnitus, delerium
NICOTINENICOTINE
Mech: ganglionic stimulation by depolarization ( Low doses)
CNS: euphoria, arousal, attention ↑ in B.P & H.R. ↑ in GI motility
Each cigarette contains 6-8mg.
High doses causes ganglionic blockade High doses cause resp. paralysis & Severe
hypotension.
Withdrawal symptoms Addictive, physical dependence
Insomnia, anxiety, restlessness Headaches, difficulty in
concentration
COCAINECOCAINE
Highly addictive, drug abuse Blockade of neurotransmitter
reuptake This ↑ CNS & peripheral actions of
catecholamines.. Intense euphoria is due to ↑
Dopaminergic effects.
Actions: Powerful stimulation of cortex &
brainstem, which causes hallucinations, delusions, euphoria
Peripherally causes – tachycardia, hypertension, mydriasis, peripheral vasoconstriction.
USES: As local anesthetic which causes
vasoconstriction Rarely used Mech of action – Na Channel Blocker
SE: Anxiety, hypertension, tachycardia, Hyperthermia due to impaired sweating
Seizures and fatal cardiac arrhythmias, resp. failure.
Amphetamine Amphetamine
Mech: increased release of intracellular stores of catecholamines.
Psychological and physiological dependence
Actions: CNS: increased alertness, decreased fatigue,
insomnia. Norepinephrine release ↑
Amphetamine is a powerful central nervous system stimulant drug, used recreationally for the euphoriant effects,
"functionally" to ward off fatigue and increase energy and capacity for physical activity.
amphetamine used in the treatment of the sleeping disorder narcolepsy and
the behavioral syndrome called called attention deficit hyperactivity disorder (ADHD).
Used to reduce appetite
SE: Insomnia, dizziness, tremor, irritability,
cardiac arrhythmias, hypertension, anorexia, abdominal cramps…
MethylphenidateMethylphenidate
Has central stimulant actions same as amphetamine..
Used mainly for Narcolepsy Also for Attention deficit syndrome.
LYSERGIC ACID LYSERGIC ACID DIETHYLAMIDE (LSD)DIETHYLAMIDE (LSD)
Multiple sites in CNS Serotonin agonist Hallucinogen Increased B.P, body temp.. Dependence SE: hyperreflexia, muscular weakness High doses Psychotic symptoms Rx with Haloperidol
The physical effects include dilated pupils, higher body temperature, increased heart rate and blood pressure, sweating, loss of appetite, sleeplessness, dry mouth, and tremors.
Users refer to their experience with LSD as a "trip" and to acute adverse reactions as a "bad trip."
experience severe, terrifying thoughts and feelings,
fear of losing control, fear of insanity and death, and despair while using LSD.
LSD users experience flashbacks
LSD is not considered an addictive drug
Haloperidol & other Antipsychotic drugs can be used to block the hallucinatory actions of LSD.
TetrahydrocannabinolTetrahydrocannabinol
Marijuana (cannabis) Euphoria , drowsiness, relaxation Impairs memory and mental activity. Xerostomia, hallucinations, delusions.. Dependence
Tetra hydro cannabinol is an appetite stimulant and antiemetic.
dronabinol (a synthetic version of THC)
Indications for UseIndications for Use The research evidence most strongly
supports the use of Dronabinol in the following areas:
Nausea and vomiting, especially when due to chemotherapy for cancer or HIV-AIDS
Anorexia, especially in the setting of HIV-AIDS
Chronic pain, especially when due to damaged nerves (e.g., spinal cord injury)
Muscle spasms and spasticity (e.g., multiple sclerosis, post-stroke syndrome)
PHENCYCLIDINEPHENCYCLIDINE(ANGEL DUST)(ANGEL DUST)
Blocks re uptake of dopamine, NE, 5-HT… Major action is to block the ion channel
regulated by NMDA subtype of Glutamate receptor
Causes Dissociative anesthesia & analgesia It's pharmacological nature is commonly
referred to as Dissociative Anesthetic, however it can possess the properties of a
CNS depressant, a hallucinogenic, and an analgesic.
Hostile and bizarre behavior. Staggered gait, muscular rigidity. High dose -- coma
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