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Week 1 Psychopharmacology

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by: Emma Notetaker

Week 1 Psychopharmacology NSCI 4530

Marketplace > Tulane University > NSCI > NSCI 4530 > Week 1 Psychopharmacology
Emma Notetaker
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week 1 of notes
Dr. Donhanich
Class Notes




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This 4 page Class Notes was uploaded by Emma Notetaker on Saturday September 3, 2016. The Class Notes belongs to NSCI 4530 at Tulane University taught by Dr. Donhanich in Fall 2016. Since its upload, it has received 64 views. For similar materials see Psychopharmacology in NSCI at Tulane University.


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Date Created: 09/03/16
Wednesday, August 31, 2016 Week 1 Principles of Psychopharmacology - Drug Administration • psychopharmacology: scientific study of drug actions and effects on mood and behavior • goals: • to place drug at site of action effective concentration • • maintained for appropriate time • cause desired effect • neuropharmacology: drug induced changes in cell function • neuropsychopharmacology: identify substances that act on the nervous system to alter behavior brain is primary site of action to reduce cough - most drugs act here (some peripheral effects) • • ex: cough center: medulla • drug action: specific molecular changes produced by drug • drug effects: physiological or psychological effects • **site of drug action may be different from site of effects** (administration site is NOT the target) pathways: • • administration —> absorbing surface • absorbing surface —> vessel (enters blood circulation) • vessel —> target protein • —> stays in vessel (inactive) • —> storage depots (bone/muscle) —> kidneys (may reabsorb here) —> elimination • • —> liver • **look at diagram on slides** • specific drug effects: based on interactions of drug with target site • nonspecific drug effects: based on unique characteristics of individuals (ex: placebo) • pharmacokinetics: effects of the body on a drug (gaining access to brain - all pharmacokinetic events) • bioavailability: concentration of a drug in the blood that is free to interact at target sites • not as important as brain availability, but hard to monitor brain levels • absorption rates: how quickly drug can access blood circulation • depends on • administration absorption • • properties of drug • volume of distribution: how much can actually leave bloodstream and reach targets • distribution-dependent • plasma concentration of drug over time: • Cmax: peak concentration in blood - may cause side effects 1/2 life: time required to reduce plasma concentration by 50% • • AUC: area under curve • managing therapeutic concentration range by repeated dosing • want to maintain levels between minimum effecting concentration and toxic levels (therapeutic range) 1 Wednesday, August 31, 2016 • clearance rate: how drug becomes inactive/eliminated • biotransformation elimination • • absorption • most absorption occurs in small intestine • distribution • bonding to receptors • depot binding: bind to plasma proteins some may be stored in bone or fat • • inactivation or biotransformation: metabolic processes of liver • elimination • pharmacodynamics: effects of drug on the body • drug molecules: • agonists: mimics effects of endogenous molecules antagonists: opposite effects • • binding: • drug affinity: drug interactions with proteins • function - broad effects • cellular, systems • physiological behavioral • Routes of administration: influence onset of drug action enteral: uses alimentary canal - a sealed tube • • usually slow onset • variable levels of drug in blood • cells forming alimentary canal: epithelial cell sheets (simple columnar) • intracellular spaces between GI cells very small • 4 angstroms between cells epithelial cells lining GI tract are tightly apposed • • drug passes through lumen of GI cells into capillaries on the other side • capillaries have endothelial cells which are easier to pass into • oral (PO = per os; by mouth) • not absorbed in mouth, but in GI tract • self-administered, avoids complications usually simple and safe, often most economical • • safe due to ability to throw up toxins • very complex process • properties of drugs absorbed in GI tract • water soluble - must be dissolved • gastric resistant: low pH and enzymes are present in GI tract • • chemical digestion: acid (hydrochloric) and pepsin (enzymes) = gastric juice • mechanical digestion: muscular contractions (peristalsis) • lipid soluble: must be able to pass through the wall • insulin is NOT administered orally because it is a peptide - enzymes in the GI tract break it down (torn apart by pepsin enzyme) 2 Wednesday, August 31, 2016 • first-pass metabolism: drug passing through liver metabolized before reaching general circulation liver is the first place where the drug can be degraded • • repeated doses almost always necessary • time release oral preparations: via coatings, mixing • sustained release (SR) • sustained action (SA) • extended release (ER, XR, XL) controls/continuous release (CR) • • modified release (MR) • buccal: drugs via the mouth • self-administration • ingestion and inhalation necessary • examples: nicotine (cigar, pipe) • • cigars more basic solution, so can be absorbed • chewables (tobacco) • chewables (nicotine gum) • chewables (aspirin) • sublingual: absorbed under tongue • • avoids gastric degradation • avoids first-pass liver metabolism (doesn’t go to liver) • blood flow goes directly to heart for rapid access • examples: • antiemetics (anti-nausea) - avoids possibility of vomiting if taken orally • nitroglycerin: dilates coronary artery, which increases oxygen going to heart (helps with angina) • rectal: • may avoid first-pass metabolism • paraenteral: not in the alimentary canal • intravenous (IV): most rapid and accurate method • very quick onset may be dangerous • intramuscular: • slower more even absorption than IV • solution may be irritating • intraperitoneal (IP): injection through abdominal cavity • rapid, variability in absorption • intrathecal • subcutaneous: injected just below skin • slow, steady absorption • inhalation: rapid absorption bc many capillaries on alveoli • topical: usually local effects • intranasal: causes local and systematic effects while drug moves across epithelial cell • passes the blood brain barrier • transdermal: controlled and sustained drug delivery • epidural: spinal anesthetics • intranasal • intracranial and intracerebroventricular often used in animals 3 Wednesday, August 31, 2016 Reading: Drug Administration • administration: • oral • most convenient • not all drugs can be this way bc not safe in the acid of the stomach • some may irritate gastric mucosa • usually latent period 30-120 minute before maximum concentration in plasma • presence of enough concentration dependent on dissolution and absorption • dissolution is essential - usually in the stomach and may depend on gastric acidity • speed of dissolution can affect amount absorbed - faster dissolution usually means more absorption • sustained release preparations: multi-lamellate erodible polymers, allow slow release continuously • absorption: dependent on physiochemical properties (lipid solubility) • small non-ionized cross easily to absorb acidic areas (ex: weak acids) most drugs absorbed in duodenum • • drugs that affect gastric motility: modify dissolution and rate, NOT extent of absorption • absorption and carrier transport: sometimes requires carrier transport (ex: levodopa absorbed by amino acid transporter) • subcutaneous and intramuscular • usually poorly broken down in the gut, poorly absorbed or significant first-pass effects orally • determined by regional blood flow • sometimes used to slow absorption rates and prolong duration of action • intravenous • rapid immediate onset • allows for accurate dosage (predictable) mini-infusion pumps: intermittent intravenous delivery • • targeted delivery: selectively goes to desired site of action • transmucosal: to mucous membranes for topical effects • systemic absorption • nasal: drugs rapidly absorbed from nasal mucosa to the CSF • transdermal: usually drugs not well absorbed through skin only works with high liid solubility and potency • • local infiltration • confine action • inhalation • dependent on transfer from alveoli to pulmonary capillaries 4


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