CNS Stimulant Drugs Flashcards by Devanshi Gajjar

Glutamate

Wake supporting chemical; Excitatory processes, memory; Block produces unconsciousness, amnesia, analgesia

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Norepinephrine

Wake supporting chemical; Supports waking, muscle tone; Stress, some analgesia

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Serotonin

Wake supporting chemical; Waking; Antidepressants, salivation

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Dopamine

Wake supporting chemical; Arousal, salience, motor; Decrease in Parkinsons disease, excess in schizophrenia and increase stimulant drugs, dependence

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Histamine

Wake supporting chemical; Waking switch, immune, energy-weight; Antihistamines produce drowsiness, weight gain

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Orexin

Wake supporting chemical; Maintains waking; Loss produces narcolepsy

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Melanocortin or Corticosteroid or Endogenous Opiate

Wake supporting chemical; Arousal, energy metabolism; Max in morning-Glucocorticoids, CRF, endomorphans, melanocyte stimulation, hormone

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Thyroid

Wake supporting chemical; Energy metabolism and waking; Deficiency produces mental dullness

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Acetylcholine and Dopamine

Agents in Special Sleep State; Waking on, REM on; Max in REM, Mediates dreams and hallucinations

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Norepinephrine and Serotonin

Agents in Special Sleep State; Waking on, REM off; Min during REM, Turned off by GABA, muscle atonia

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Prolactin (PL) &/ Oxytocin

Agents in Special Sleep State; Antianxiety; Nursing, Post coital drowsiness, Oxytocin antianxiety effect

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Progesterone

Agents in Special Sleep State; Antianxiety; Allopregnenolne binds GABA receptors and facilitates drowsiness

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Prostaglandin D2

Agents in Special Sleep State; Sleep promoter; Sleepiness in sleep sickness

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GABA, Glycine, GHB

Sleep Promoting Agents; Anti-anxiety, abnormal in epilepsy

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Growth Hormone

Sleep Promoting Agents; Slow wave sleep; Release max at beginning of sleep, Anabolic

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Vasopressin

Sleep Promoting Agents; Circadian time mediator; Experimental use in elderly

Melatonin

Sleep Promoting Agents; Timing of sleep cycle, initiates; Helpful in aged patient, jetlag

Adenosine

Sleep Promoting Agents; Sleep need indicator; Accumulates in sleep deprivation, caffeine blocks

Gherlin, Delta sleep peptide, Agouti, Adenosine, NPY, VIP

Sleep Promoting Agents; Sleep or drowsiness, reduced energy metabolism; Various

Amphetamines

Sympathomimetics; Amphetamine, Methamphetamine, Lisdexamphetamine (Vyvanese); Displace and release presynaptic transmitter from vesicles, Block transmitter reuptake, Acts as pseudo-transmitters, Can block MAO, Prefrontal cortex NE; CII

Methylphenidate

(Ritalin); Sympathomimetics; DA reuptake block; Dexmethylphenidate (Focalin); Block transmitter reuptake, Prefrontal cortex NE; CII; ADHD treatment; Metabolism: Does not inhibit cytochrones, Metabolized in liver by carboxylesterase (CES1A1), Drug interaction with anticonvulsants, antidepressants, antipsychotics, antibiotic linazolid (Blocks monamine oxidase), and anticoagulants; Side Effects - like Sympathomimetics (dry mouth), Alpha 2 agonists (Sleepiness, low BP, Dry mouth, Decrease GI acid secretion, “Withdrawal reactions” and GH release in kids)

Pemoline

(Cylert); Sympathomimetics; More toxic than Methylphenidate

Ephedrine

(Pseudoephedrine); Sympathomimetics; Phenylpropanolamine (PPA) - Decongestant but diverted to Methamphetamine synthesis; Displace and release presynaptic transmitter from vesicle, Act as pseudo-transmitters

Cocaine

(Erythoxylom coca); Sympathomimetics; Diff mechanism of action; Block transmitter reuptake (Biogenic amines - DA, NE & 5HT), Local anesthetic, Prefrontal cortex NE; CII; Used in ENT meds; Blocks baroreceptor input to heart (BP increase); CNS stimulation (Monoamine), Mydriasis (alpha-2 agonist), Euphoria; May prolong NE action on alpha and beta peripheral receptors - Vasoconstriction and Increase CO - Ventricular hypertrophy; Dental Impact - Bruxism, Dry mouth, Dental treatment stimulus increase BP, Benzodiazepine reduces reactive response

Selective Reuptake Antidepressants

Sympathomimetics; Block transmitter reuptake, Prefrontal cortex NE; Selective Reuptake Blocker - Rx (DA block - Dependence)

Actions of Sympathomimetics

Decreases effects of fatigue (CNS DA), Temporary appetite suppression (Tolerance develops); Used to treat narcolepsy, Used to treat AD/HD, ADD, Adjunct to opiate analgesia (Rare), Physiologic Respiratory Stimulation (Not for long term)

Side Effects of Sympathomimetics

Insomnia, Anorexia, Reduce growth in children, Paranoid psychosis stereotypic behaviors, Can elevate blood pressure (Stroke, microstrokes -> Increase Alzheimers), Cardiovascular damage or hypertrophy, Dry mouth, Bruxism, TMJ, Caries; Lowers seizure threshold; Dependence (look like depression, "Psychological")

Hallucinogens, Designer Drugs Controlled Substance Class

Hallucinogens - LSD, MDA, Psilocyben, Mescaline - C1 | Designer Drugs - Ecstasy (MDMA) - C1

Methylxanthines

Stimulants (Reduce fatigue); Caffiene, Theobromine, Theophylline, Aminophylline; Positive ionotropic (force) and chronotropic (rate) action on heart; Smooth muscle relaxation, Improves respiratory function, Improve respiratory drive, Potentiate steroid anti-inflammatory, Weak diuretic, Caffienol = Treatment of ischemic stroke

Methylxanthines Mechanism of Action

Block inhibitor adenosine receptors (Arousal), High doses inhibit phosphodiesterase - Promote increase in cAMP, Increase Ca++ permeability, Induce histone deacetylases potentiating steroid anti-inflammatory action

Theophylline and Aminophylline

Methylxanthines; Asthma treatment - Relax smooth muscles and increase voluntary tone; Brutal dosing

Methylxanthine Side Effects

Anxiety or insomnia or antagonize dental sedatives, Seizures or hypertension (high doses), Release of catecholamines (vasoconstrictors), Anorexia, Nausea, Vomiting, Theophylline kinetics monitor, Coffee - Increase GI acid and secretions, Little dependence liability

Theophylline (Caffiene) Drug Interactions

Antagonizes benzodiazepines, sedative and anesthetics, propofol and increase halothane arrhythmias, metabolic drugs (cleared by CYP1A2), diet, metabolic inducers, metabolic inhibitors (beta blockers, macrolides, disulfiram, quinolones, interferon, diuretics, potentiate anti-inflammatory steroids)