Svensons Sections Flashcards
What are psychostimulants?
- Activate the CNS resulting in alertness, excitation and elevated mood
What is the most used illegal drug in 2018?
- Marijuana
- Cocaine, ecstasy, meth, crack, herion
What are the roles within the Mesolimbic dopamine system?
- Prefrontal Cortex [planning, judgement]
- Hippocampus [Memory, Learning]
- Amygdala [Fear, Emotion]
- NUCLEUS ACCUMBENS [Reward]
- VTA
What are some of the pathways that drugs can have abusive effects on the dopamine reward system?
- Nicotine [VTA: DA, Opioid peptide +]
- Opiates [VTA: GABA - & NAc -]
- Stimulants [Release DA from VTA to NAc]
What is Nicotine MOA?`
- Activates Acetylcholinergic receptor
- Na enters; K exits = Action Potential
- 12 units
What is the difference between Acetylcholine and Nicotine?
- BOTH have charged groups and H-Bond groups
- Nicotine can cross the membrane [weak base] & not degraded by ACHE
What is the partial agonist therapy for Nicotine?
- Release of Dopamine
- HIGHLY ADDICTIVE
- Varenicline: Partial Agonist - low efficacy and binds tightly
What are some of the commonly abused psychostimulants?
- MDMA [Ecstacy], Meth, Methylphenidate, Cocaine
Why is Pseudoephedrine kept behind the counter?
- Being able to reduce the OH to H = Meth
What is the MOA for cocaine?
- Antagonist of Amine Transporters [DAT, SERT, NERT]
- DAT>SERT>NET
- Increases DA concentration
What is the MOA for Methamphetamine, Ecstacy & Bath Salts?
- Compete for reuptake
- Block DA reuptake
- PUSH OUT DA from vesicles
- Activates TAAR1 - Reverse transport
What are some of the clinical effects of Methamphetamine abuse/
- Neurologic: Delirium, tremor
- Psych: Anxiety, Paranoia, Hallucination, Delusions
- ENT: Profuse Dental decay [“Meth Mouth”]
- Cardio: Tachycardia, Hypertension/Vasospams
- Skin: Diaphoresis
What is important to know about the brain within a METH abuser??
- Measures: [11C]d-thero-methylphenidate
- DA receptors are down-regulated [might cause addictions]
- Recovery of DA receptors means that homeostasis has returned
Can low dose psychostimulant improve performance?
- Low Dose = cognitive enhancement
- Higher Dose = Addiction and Cognitive Deficit
What are the Sympathomimetic Toxidrome?
- MATHS
- Mydriasis
- Agitation, arrhythmia, angina
- Tachycardia
- Seizure, sweating
What is the key component that is found within Cannabis?
- Delta 9 - TetraHydroCannabinol
What is the difference between Hemp and Marijuana?
- Hemp: 0.3% or less of THC needed [groen for agricultural products
- Marijuana: 15 - 20% of THC
What is important to know about the legalization of marijuana?
- Still a Schedule I under Federal Controlled Substance Act
- Farm Bill of 2018 is passed = legalizing hemp
What is important to know about Delta 8 - THC?
- It has 25% of the psycostimulant of Delta 9 and is NOT illegal
What is Synthetic Marijuana?
- Agents that are potent than THC - gets sprayed onto the drugs
- “spice”
What are some of the signs and symptoms of Acute Cannabis Intoxication?
- Perceptual [Slowing, Illusions..]
- Affective [Euphoria., Anxiety, Disinhibition]
- Cognitive [Suspiciousness, Impaired Reaction time]
- Physical [Tachycardia, Hypotension, Dry Mouth][
What are the parts of the Endocannabinoids Systems [ECS]?
- Receptors [CB1 & CB2]
- Ligands [Anandamide & 2-AG]
- Transporter [EMT]
- Enzymes [FAAH, MAGL, DAG]
What do Endocannabinoids and phytocannabinoids do within the receptor?
- Retrograde Regulators - inhibiting the release of GABA and Glutamine
- THC = PARTIAL AGONIST
- SYNTHETHIC = FULL AGONIST
Where are CB1 expressed the most?
- In the brain
- Low levels respiratory centers of the brainsteam = <respiratory depression; coma
Where are CB2 expressed the most?
- in the periphery
- Help with immune regulation
What are some of the FDA approved cannabinoid drugs?
- Marinol [Synthetic Delta 9 - THC in sesame oil]; Counters loss of appetite
- Nabilone [Anti-emetic in cancer patients]
What are the challenges with medical marijuana use?
- Lack of product quality control
- Absence of adequate study for ADR
- Highly politicized
- Growing influcances
What is the Pharmacology and use for Cannabidiol [CBD]?
- Low affinity for CB receptors
- Antagonize THC at CB1
- For Pain - not good data
What is Cannabidiol approved for?_
- Rare Seizure Disorder [Dravet Syndrome and Lennox-Gastust Syndrome]
What is Cannabinoid Hyperemesis Syndrome?
- Episodes of using cannabis causing nausea/vominting and stomach pain
- Treatment: cannabis cessation, Benzo, Haloperidol, Capsaicin
What is the mechanism of action for capsaicin for cannabinoid hyperemesis syndrome?
- Substance P activates NK-1R = N/V
- TRPV-1 [heat] decreases Substance P
- Cannabis downregulates TRPV-1 = N/V
- Capsaicin activates TRPV-1 = - N/V
What are Psychedelics?
- Agents that produce non-ordinary and variable forms of conscious experinces
What is a delusion?
- Fixed, False belief unresponsive to logic [Paranoia]
What is a hallucination?
- A false perception arising from internal stimuli [False Reality]
What is an illusion?
- A misperception of external stimuli [Distortion]
What are the two classes of Psychedelics?
- Classical & Dissociative
What are the Classical Psychedelic Drugs?
- Phenethylamine [Mescaline, MDA, MDMA, Psilocin]
- Tryptamine [DMT, LSD, Ibogaine, 5-MeO-DiPT]
What is the mechanism of action of the classical psychedelic?
- Agonist of Serotonin receptor [Increasing Glutamate and BDNF]
- Pretreatment with Serotonin antagonists BLOCKS effects
What are the adverse effects of the Psychedelic drugs used?
- Short Term: Tachycardia, Hypertension, Tremors, Dry Mouth, Nausea, Hyperthermia
- Acute Reaction: Terrifying thoughts, Fear of …]
- Psychotic Reactions: Flashbacks, Psychosis
What is the Mechanism of Actions for Dissociative Psychedelics>
- Inhibition of GABA release
- Disinhibition of Glutamate Release
What are the Prominent NMDA receptor antagonists>?
- Induces anesthesia AND analgesia
- Ketamine and Dextromethorphan
What is important to know about Ketamine?
- “Special K”
- S + is more active
- Used in opioid tolerant patients for pain
What is important to know about Dextrimethorphan?
- Abused by 4% of high schoolers
- Low dose = cough supporession; High Dose = “High”
What is the Pharmacology of Phencyclidine [PCP]?
- Mort potent than Ketemine [NMDA Antagonist] & Dopamine [D2 Agonist]
- Cigarette dipped in liquid PCP to get high
- Self Mutilation without recognition is a side effect
What is the Pharmacology of Muscimol?
- Agonist of GABAa that induces dissociative psychedelic effects
- Gets decarboxylated to active form
What are the type of Psychoactive inhalants?
- Liquids [Paint Thinner, Gas, Glue, Markers]
- Aerosols [Spray Paint, Deodorant, Hair Spray]
- Gases [Chloroform, Nitrous Oxide, Butane]
- Nitrites [Leather Cleaner, Room Deodorizer]
What are the ways that Inhalants can be misused?
- Sniffing, Huffing, Bagging, Dusting
What is the pharmacology of Alkyl Nitrites?
- “Poppers”
- Cleaning solutions & Room Deodorizers
- Abused among gay men [Relaxes Anal Sphincter, Enhanced Erection, Euphoria]
What is the pharmacology of Volatile Solvents?
- Liquids at Room Temp and vapor when exposed to air
- Toluene, Acetone, Benzene, Butane
What are the clinical effects of volatile solvents?
- Acute effects: Locomotor, Euphoria
- High Doses: CNS Depression, Slurred Speech, weakness, sedation
What is the risk of Inhalant abuse?
- Asphyxiation, Suffocation, Seizures, Coma, Choking, fatal Injury
