Licthblau- Stimulants, Cognitive Enhancers, and Anesthetics Flashcards
Stimulants MOA
increase levels of NT by:
Increase release of NE and DA from presynaptic neuron
Block reuptake of NE and DA
Inhibit monoamine oxidase (MAO)
Cocaine
type: Sympathomimetics
MOA:
Blocked reuptake of norepinephrine - motor
Blocked reuptake of dopamine - euphoria
Local anesthetic properties
Uses: Local anesthetic or stimulant
Side effects:
Cardiac arrhythmias, coronary, and cerebral thrombosis
Impairs brain size and neurological development in babies
Tolerance/Dependence:
Psychological
Maybe physical
Don’t really build up a tolerance –> cocaine users can use the same amour each day and get the same effect
MDMA (Ecstasy) (Molly)
type: Sympathomimetics
MOA:
stimulates release and inhibits reuptake of epinephrine, norepinephrine, and dopamine
DIRECTLY stimulates serotonin auto receptors –> emotional effects
Stimulates the release and inhibits reuptake of serotonin
Also affects: histamine, GABA, ACh, DA receptors, NE transporter protein
Uses:
Empathogen → can be used in PTSD to make people more empathetic
CNS stimulant
Bath Salts (Methylenedioxypyrovalerone)
type: Sympathomimetics
MOA: These are drugs that are derived from amphetamines but are chemical variants that act on the brain like stimulants
Toxicity:
VERY SEVERE HALLUCINATIONS AND HIGH ABUSE POTENTIAL
May cause chest pains and increase blood pressure, heart rate, and agitation; often causes extreme paranoia and delusions
Caffeine/Theophylline
Type: Xanthines
MOA: 3 proposed mechanisms
1) translocation of intracellular calcium from the SR
2) inhibition of phosphodiesterase (creating elevated levels of the second messenger cAMP)
3) act as a non-selective adenosine receptor antagonist (inhibits the adenosine receptor that makes us sleepy)
Uses (with increasing doses):
Stimulates cerebral cortex –> clearer flow of thought (decreased reaction time and better association of ideas), less fatigue, improved manual dexterity
Also stimulates respiration (hyperventilate) and vasomotor centers (pump more blood –> increase BP)
Diuretic and smooth muscle relaxant
Large doses affect spinal cord (Hyperreflexia)
Toxicity:
CNS → insomnia, excitement, possible convulsions and death
CV → increased HR, arrhythmias, decreased clotting time
Increased gastric secretions → pooping
Uses:
Cardiac stimulation in CHF (dilates coronary arteries and increase O2 demand by the heart)
paroxysmal dyspnea associated with left heart failure
analeptic treatment (severe shortness of breath)
smooth muscle relaxant so can be used to treat bronchial asthma
↓ Peripheral vascular resistance
↑ Cerebral vascular resistance (Migraine treatment due to vasoconstriction)
Tolerance:
develop tolerance to sleep-disrupting effects (Thus I need to get drink more caffeine to get the same effects i did at the beginning)
Withdrawal: Headache, irritability, can’t concentrate, sleepy, can’t sleep, abdominal and joint pain –> Withdrawal occurs within 12-24 hours after discontinuation of caffeine intake
Theophylline
Just a more potent version of caffeine
Modafinil and Armodafinil
Type: Eugeroics/wakefullness
MOA:
Affects Monoamines:
Dopamine –> Increase release in striatum, increase in nucleus accumbens (part of basal ganglia- involved in reward), may block DA reuptake
Norepinephrine –> ↑ Release in hypothalamus
Serotonin –> ↑ Release in amygdala and frontal cortex
Elevates hypothalamic histamine levels
Activates glutamatergic circuits (glutamine)
Inhibits GABAergic neurotransmission
Uses:
narcolepsy, shift work sleep disorder, and excessive daytime sleepiness due to sleep apnea
Could be used for ADHD but causes rash in kids
Off market uses: depression, bipolar, drug dependence, parkinsons, etc
Side Effects:
Common: head, nausea, insomnia, decrease appetite, dizzy, agitation
Severe: dermatologic reaction requiring hospitalization (modafinil only)
Pathophysiology behind ADHD
NE and DA are important in maintaining and focusing attention → these are deficient in ADHD
Raising NE and DA levels help reduce symptoms (MOA for most drugs)
2 drug classes used to treat ADHD (Psychostimulants)
Methylphenidate → Enhance DA release and block reuptake
Amphetamines → Enhance DA release/reuptake and enhance NE release
Atomoxetine (Strattera)
Type: Psychostimulant
MOA:
Highly selective NE reuptake inhibitor; also elevates DA levels in the prefrontal cortex (but not in nucleus accumbens or striatum); simultaneous release of DA and NE leads to increased ACh, which helps memory
Uses:
First-line ADHD treatment; can help with working memory and attention
Only drug approved for adult ADHD
Abuse potential: None!
Rivastigmine (Exelon)
Type: Anti-cholinesterase
MOA:
Inhibits the enzyme acetylcholinesterase, essentially elevated ACh levels in the brain; inhibits both AchE and BuChE
Uses:
Alzheimer’s disease
Administered twice daily for better compliance
Adverse effects:
include nausea, anorexia, vomiting, and diarrhea
causes more GI issues and muscle weakness than other AChE meds
Tacrine (Cognex)
Type: Anti-cholinesterase
MOA:
Inhibits the enzyme acetylcholinesterase, essentially elevated ACh levels in the brain
Uses:
Alzheimer’s disease- Second-line therapy
Short half life and thus requires multiple doses, resulting in poor compliance
Adverse effects:
GI problems
drug interactions with NSAIDs
may cause liver damage
Galanatamine (Razadyne)
Type: Anti-cholinesterase
MOA:
Inhibits the enzyme acetylcholinesterase, essentially elevated ACh levels in the brain; also stimulates nicotinic cholinergic neurons to release more stored ACh
Uses:
Alzheimer’s disease
Can delay cognitive deterioration by a year in 20%
Adverse effects:
GI problems
be careful when using with antidepressants or drugs with cholinergic side effects which may interfere with elimination of galantamine from the body
can increase risk of stomach ulcers
Memantine (Namenda)
Type: NMDA antagonist and Anti-cholinesterase
MOA:
Inhibits the enzyme acetylcholinesterase, essentially elevated ACh levels in the brain; also an antagonist at the NMDA glutamate receptors
Uses:
Used for severe alzheimer’s
Adverse effects:
GI problems
dizziness, headache, constipation, confusion
Gingko Biloba
Type: Natural Substance
MOA:
Uses: May have modest benefit in Alzheimer’s pts
Adverse effects:
Worst side effects
Serious side effects include bleeding, seizures, and coma
Halothane
Type: General Anesthetic (Inhalation)
Halogenated Hydrocarbon
MOA:
There is no specific site of action; no interaction with pharmacologically defined receptors; known to cause cell membrane fluidity
Uses:
Surgical procedures requiring unconscious state and complete absence of sensations
Advantages:
Rapid induction and recovery, inexpensive, does not irritate the larynx, potent
Disadvantages:
Inadequate analgesia and muscle relaxation
Depresses myocardium and baroreceptor reflexes –> So decreases CO and BP
Sensitizes myocardium to catecholamines (like Epi, Norepi)
So if i give Epi for my decreases BP → increase BP too much → increase cerebral blood flow and intracranial pressure → death
Respiratory depression
Potential for hepatotoxicity
Halothane hepatitis
Hepatic necrosis, fever, nausea, etc
Can progress to hepatic failure
Can cause malignant hyperthermia
Isoflurane
Type: General Anesthetic (Inhalation)
Halogenated Hydrocarbon
MOA:
Unknown
Uses:
Surgical procedures requiring unconscious state and complete absence of sensations
Advantages:
Potent but does NOT sensitize heart to catecholamines
Less hepatotoxicity
Disadvantages
arrhythmias, bad odor, could cause malignant hyperthermia
Sevoflurane
Type: General Anesthetic (Inhalation)
Halogenated Hydrocarbon
MOA:
Unknown
Uses:
Inhalation; Surgical procedures requiring unconscious state and complete absence of sensations
Advantages:
Sevoflurane is a near perfect inhalation drug because it has a high potency and low blood solubility (rapid onset and recovery)
Nitrous oxide
Type: General Anesthetic
(Inhalation)
MOA:
Unknown
*Only inhalation anesthetic that is a gas
Uses:
Inhalation; Surgical procedures requiring unconscious state and complete absence of sensations
Low blood solubility to rapid onset; can provide second gas effect to help administration of other inhalants
Disadvantages:
MAC = 104% → cannot use as anesthetic
No muscle relaxant
Diffusion hypoxia if rapidly discontinued
Barbiturates: Thiopental, methohexital
Type: General Anesthetic (injection)
MOA:
facilitates GABA induced Cl- entry into neurons, leading to CNS depression → hyper polarization
Uses:
Surgical procedures requiring unconscious state and complete absence of sensations
Advantages:
Has rapid onset and short action
Disadvantages:
Very low therapeutic index (therapeutic dose is close to lethal dose)
Benzos: Midazolam (Versed) and Diazepam (Valium)
Type: General Anesthetic (injection)
MOA:
facilitates GABA induced Cl- entry into neurons, leading to CNS depression → hyper polarization
Uses:
Surgical procedures requiring unconscious state and complete absence of sensations
Advantages:
Less cardiovascular and respiratory depression than barbiturates
Amnestic action (good to help you forget)
Disadvantages:
Insufficient for anesthesia when given alone
Used as induction agent prior to anesthesia
Propofol (Diprivan)
Type: General Anesthetic (injection)
MOA:
facilitates GABA induced Cl- entry into neurons, leading to CNS depression → hyper polarization
Uses:
Surgical procedures requiring unconscious state and complete absence of sensations
Advantages:
Rapid induction (seconds) and recovery (mins)
May be given alone to maintain anesthesia or used for induction as part of balanced anesthesia technique
Pts wake clear headed and aren’t nauseous (antiemetic)
Disadvantages:
May result in pain at injection site
Most significant respiratory effect is apnea (Killed MJ)
Ketamine
Type: General Anesthetic (injection)
MOA:
NDMD Glutamate receptors (unsure of this)
Uses:
Surgical procedures requiring unconscious state and complete absence of sensations
Advantages:
Rapid onset and short duration
Dissociative anesthetic Patient appears to be awake - eyes open and unaware of environment and doesn’t feel pain
Anesthetic (unconscious) analgesic (pain free), amnestic (loss of memory) and sedative (sleep)
Airway reflexes and respiration is maintained –> So you can lay on your back and still breathe fine
Cardiovascular system is not depressed and HR/BP may be stimulated –> Ideal for pts with unstable CV function
Disadvantages:
Drawback: Delirium and Hallucinations
Abused in the US –> Used in the RAVE community
Opioids: Fentanyl (Sublimaze), Sufentanil (Sufenta), Alfentanil (Alfenta)
Type:
General Anesthetic
(Injection)
Uses:
Surgical procedures requiring unconscious state and complete absence of sensations
MOA:
High dose opioid
Usually supplemented with inhalation anesthetic benzodiazepine or propofol
Advantages:
Very good for analgesia and anesthesia
Hemodynamic stability → good for patients with compromised myocardial function
Disadvantages:
respiration must be maintained artificially and may be depressed post operatively
