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introduction

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Department
Psychology
Course
Psychology 2660A/B
Professor
Riley Hinson
Semester
Winter

Description
Drug names : - Chemical name : describe type of molecule and location of chemical group - The generic name or non-proprietary name: commonly used and can be used by any company marketing the drug - Trade name or proprietary name: given and only used by the same company - Street names: derivatives of trade names Pharmacokinetics: Administration => absorption => distribution (via circulatory system) => X => metabolism (metabolized to an inactive form) => elimination Pharmacodynamics: X = drug reaches the SA and interact with the Rc. Routes of administration: - Oral: must pass from stomach or small intestine then bloodstream o Stomach: highly acid so might destroy drugs o If alkaline drugs: they are ionized and cannot pass out in bloodstream so o Exit to small intestine (more alkaline environment: diffusion (high Cm to low Cm) into bloodstream) o Liver: might metabolized a part of the drug:  Cytochrome P-450 in endoplasmic reticulum of liver cells (enzyme). This enzyme is inducible, is activity might be potentiated. - Snorting: Albert Hoffman found LSD (first acid trip) - Inhalation: effective method but lung damage (e.g. bagging, huffing) o Faster than IV. Reaches the brain in 5-8 sec. - Injection: likely dependent on the blood flow in the injection’s area o Peritoneal > muscles o Muscles > skin o Interperitoneal > intramuscular > subcutaneous Drug vocabulary: subcutaneous injection = Skin popping Medical injection: implanting a pellet (boulette) or a depot (e.g. antabuse) Experimentation: with animals, directly into brain or ventricules. Distribution of drugs: - Injection or pulmonary route: diffusion by pores in capillary walls. - Orally: must be lipid soluble to be absorbed A volume of blood is totally circulated once every minute so drugs quickly reach the SA.  Which factors affect a drug into the circulation: - Ionization: o Weak acids drug: ionized in alkaline environment / less ionized in acidic environment. o Weak base drug: ionized in acidic environment… o Rate of absorption: percentage of nonionized molecules o Ph of digestive system: 1.5 (acidic) to 7 (neutral) o Ionized particles penetrate cell membranes poorly (less fat soluble) - Lipid solubility: o Lipid soluble penetrate cell more easily o Lipid soluble are usually unionized. o E.g. heroin more lipid soluble than morphine. o Brain: 2% of body weight and 15-20% of blood pumped and protected by BBB. o BBB reduces diffusion of water soluble or ionized molecule but not impede lipid soluble or unionized molecule. o BBB= placenta: 75-100% of drug reach the fetal blood. - Receptor Binding: o Drug and receptor bind by opposite charges o Drug effect is proportional to the fraction of Rc occupied o Antagonist: bind and block the pharmacological effect o Naloxone: opiate Rc antagonist o Drug mixed: bind and produce some pharmacological effect (lower level)  agonist-antagonists  partial agonist  partial antagonist o Nalorphine is a mixed opiate agonist-antagonist Dose –response curve - The amount of drug administered (in mg or mg/kg) - Vertical axis: % of subjects exhibiting the measured effect - Horizontal axis: the dose - One response curve for ONE effect - The ED50: the drug produce an effect in 50% of the subjects - The LD50: dose kills 50% of the subjects (heroin=350mg, nicotine=60mg) - Therapeutic index: LD50/ED50, higher the ratio is, and less likely the drug is lethal - The margin of safety: LD1/ED99 - Tolerance: progressive attenuation of drug effect (shift to the right in DRC) - Sensitization: augmented repeated administration (shift to the left) Termination of drug action - Might be eliminated by the skin, the lungs or the kidneys, sweat (small %), exhalation, urine - Liver: cytochrome P450, and a lot of different enzyme differing by the level of CYP enzyme activity. Drugs depress the activity of CYP (SSRI inhibit CYP enzymes) - Young and aged people: hepatic metabolizing system is less efficient. - E.g. fluoxetine (Prozac): 2/3 of effects => norfluoxetine: over a week => excreted. - Renal absorption: pH dependent (weak acid more excreted if urine is alkaline and conversely) - To treat an overdose we might change the pH of the urine but it’s a slow process - Eliminate half-life (t1/2): time needed for half of a drug dose to be eliminated. o E.g. benzodiazepine with short elimination: good as sleep inducing and long eliminatio
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