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U of M PUBH 3003 - Pharmacology- Drug Basics

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PUBH 3001 1st Edition Lecture 3Outline of Last Lecture I. Nervous Systema. Central nervous systemb. Peripheral nervous systemII. Complexity of the braina. Structuralb. Neurochemicalsc. PlasticityIII. Parts of the BrainIV. How drugs affect the braina. Alcoholb. Other drugsc. Drugs affect learningV. Brain development in early life Outline of Current LectureI. Basic PrinciplesII. Routes of AdministrationIII. How does the drug Work?IV. Dose ResponsesV. Where does the drug go?VI. Effects of Drugsa. Brain Adaptsb. Tolerance c. Withdrawal Current LecturePharmacology – Drug BasicsThese notes represent a detailed interpretation of the professor’s lecture. GradeBuddy is best used as a supplement to your own notes, not as a substitute.Basic Principles-- Drug- any substance put into a body that changes mental state or bodily functions- Length of time drug affects the CNS varieso Depends on the drug- some removed within minutes some within weeks (AGENT)o Depends on tolerance – how our body has adapted to the drugs (PERSON) You donot want to develop a tolerance to a prescribed drug- Drugs can enter the body in many different ways and change its affects o Ingesting- Usually the slowest route to the braino Rubbed on skino Mucous Membrane (nose, mouth, rectum)o Inhaling- must be very fat -soluble and must form a vapor or gas when heatedo Intravenous Injection- usually fastest route to brainRoute of Administration1. Injection or Inhaling- fastest to the brain. Concentration is the highest so risk is high2. Snorting/ Snuffing3. Ingestion – slowest route to brain How does a drug work?- Some (few) affect generation and spread action potentials down axono Can completely stop a neuron from firing- Most drugs act on pre- synaptic terminal (where the neurotransmitter is released) or postsynaptic membrane on neurotransmitter receptor - Produce more or less Dopamine receptors Drugs Binding to Receptorso Agonist: Drug binds to a receptor and activates it( i. e. the drug has an “effect”)o Antagonist: Drug binds to a receptor and does not activate ito Antagonist keep other molecules from getting to the receptors (using a molecule that normally stimulates it) – so its preventing normal processes from happeningDrug Actions Depend on Variableso Dose: Quantity- how mucho Potency: Amount required to an effect on a given intensity o Purity: Quality- what else is in the drugo The environment!Dose Responseso The larger the dose, the larger the effect (usually)o A maximum can be reached; all receptors are occupiedPotency: Amount of drug needed to produce a response o Determined by Affinity- ability of the drug to combine with receptors and produce and affect o EX: LSD binds tightly to receptors so little is needed for hallucinationo Determined by Efficiency- maximum effect drug can produce, regardless of doseo EX: Aspirin and Morphine both assist in pain relief, but Aspirin has less efficiency at this action Where does the drug go?o Once in circulation, the drug can get into most tissueso Brain is the exception; it has the defense of blood-brain barriero HOWEVER most psychoactive drugs are fat soluble enough to enter the braino But also can accumulate in fatGetting outo Most drugs leave through the kidneys and intestine (changed in the liver to a form that can be excreted through urine)o This process (metabolism and excretion) determine how long the drug effects lastso Patterns of overdosing more likely to occur with drugs that leave the body quicklyEffects of Drugs change with timeo Tolerance – our bodies adapt to the drug and reaction to the drug is progressively reduced. An increased concentration of the drug is needed to achieve the same effecto The more frequent we take the drug, the higher the dose, the more likely it is for a tolerance to developo Withdrawal- The flip side of tolerance- when decreasing or removing a drug the body needs to adapt yet againo Symptoms of Withdrawal include: Intense Worry Vomiting or Nausea  Sweating Shaking or trembling Confusion Feeling jumpy, upset, tense, edgy Seeing/ hearing things that are not there Life Threatening: delirium tremens (Include all of the above and seizures)Brain Adapts!o Overstimulation of receptors causes neurons to remove receptor to bring level of stimulation back to normal (homeostasis)o If a drug prevents receptors from working, the cell will make more receptorsLong Term Use and Brain Functioning o Effect of drugs change over time as our mind and body adapts (tolerance)o When drug use is stopped, these changes cause our body to act abnormally (withdrawal)What about Antibiotics?o Tolerance at population levelo Antibiotic resistant superbugs pose catastrophic threat to


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