Glutamate
Wake supporting chemical; Excitatory processes, memory; Block produces unconsciousness, amnesia, analgesia
Norepinephrine
Wake supporting chemical; Supports waking, muscle tone; Stress, some analgesia
Serotonin
Wake supporting chemical; Waking; Antidepressants, salivation
Dopamine
Wake supporting chemical; Arousal, salience, motor; Decrease in Parkinsons disease, excess in schizophrenia and increase stimulant drugs, dependence
Histamine
Wake supporting chemical; Waking switch, immune, energy-weight; Antihistamines produce drowsiness, weight gain
Orexin
Wake supporting chemical; Maintains waking; Loss produces narcolepsy
Melanocortin or Corticosteroid or Endogenous Opiate
Wake supporting chemical; Arousal, energy metabolism; Max in morning-Glucocorticoids, CRF, endomorphans, melanocyte stimulation, hormone
Thyroid
Wake supporting chemical; Energy metabolism and waking; Deficiency produces mental dullness
Acetylcholine and Dopamine
Agents in Special Sleep State; Waking on, REM on; Max in REM, Mediates dreams and hallucinations
Norepinephrine and Serotonin
Agents in Special Sleep State; Waking on, REM off; Min during REM, Turned off by GABA, muscle atonia
Prolactin (PL) &/ Oxytocin
Agents in Special Sleep State; Antianxiety; Nursing, Post coital drowsiness, Oxytocin antianxiety effect
Progesterone
Agents in Special Sleep State; Antianxiety; Allopregnenolne binds GABA receptors and facilitates drowsiness
Prostaglandin D2
Agents in Special Sleep State; Sleep promoter; Sleepiness in sleep sickness
GABA, Glycine, GHB
Sleep Promoting Agents; Anti-anxiety, abnormal in epilepsy
Growth Hormone
Sleep Promoting Agents; Slow wave sleep; Release max at beginning of sleep, Anabolic
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)
