Introduction to the Pharmacology of Psychoactive Drugs
Introduction to the Pharmacology of Psychoactive Drugs PSYC 472
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This 10 page Class Notes was uploaded by Dorris Purdy on Friday October 23, 2015. The Class Notes belongs to PSYC 472 at University of Idaho taught by John Miller in Fall. Since its upload, it has received 12 views. For similar materials see /class/227918/psyc-472-university-of-idaho in Psychlogy at University of Idaho.
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Date Created: 10/23/15
DEFINITION o Stimulants are a substance which tends to 0 While all stimulants increase behavioral activity the component processes involved differ o Neurotransmitter or receptor processes I crease neurotransmitters release n New reuptake iti on or ll lhlbllol y neurotransmitters i bitiun increase behavioral activity when STI M LIIANTS administered 0 Elevate Mood Men Fowie increase Motor Activity Mycheal Scott i AlertneSS se need for Slee Pave 472 tne orains metabolic and neuronal PROCESSES COMMONLY USED STIMULANTS o Caffeine o Nicotine o Amphetamine o Cocaine E edrine m N CAFFEINE AND NICOTINE Allen Fowler CAFFEDVE CAFFEDVE CONTENT I Most commonly consumed psychoactive 5 AVEijDEDWEJ drug in the world Tea 5oz in I Average intake per person per day is Cucua 5oz 5 between 80 to 400 milligrams Ch r late ml 25 cno i te mllk ioz 5 I Consumption of caffeine is not considered Cure WWWDZ mm drug a use OTC stirnulants mm OTC analgesics aspirin 35765 I No regulation on sale or use OTC mm rENEmES an EFFECTS Effects 0 Caffeine elicits positive effects such as 39 03W a VE39SEm39EEHESKSWWW o nnanced mental a er ness wzemo Sustained intellectual effort 39 39 39 ES S Nu substantial disruption of coordinated intellectual Heavvdusas39l 5 draws tnougnt or rnotor activity a and clearer flow of tnougnt fatigue eep is delayed quot f smes Effects Effects 0 Caffeine causes a slight stimulant action 0 Caffeine constricts cerebral blood vessels on the hea Decreases blood flow by about awn o increases tne Workload 39 Ca El EVE headaches eardiae eontraetility lncreases cardiac output Bmma felam o gs coronary arteries o Mo Rte tne neart Effects Reproductive Effects 0 Chronic use associated with habituation 39 a mes p acema 239e s and tolerance Consumedhvestimated75aipvegnamwamen Sssi niii contains ieveis eedei or new in concentration than mothers 0 Quitting may cause w hdrawal Saietvsiiiiumesuived ene autism mv Kimmie memes meta mane W main Wsiriess m we mnemmlh hem daihiedme rsk Mswnanmts mm m We in as we smaawn a a hm Km gamma EYS MHVSVVDVIS1EU mv mav muse Wm imamquot Therapeutic Uses Pharmacokinetics Astnrna Caffeine is rapidiy and eeirnbiete I Brunchiai reiaxatiun effects S gni cantbiuud ieveis YEaEhEdi t iy abseirbed i t eveis peak in about 2 nude n SENS mind as o Narcoiepsy I T ei neib rnaintain daytime Wakefuiness Caffeine is freeiy and equaiiy distributed tnreidgn tutai budy Water igraine stricts biEIEId HEW in HE erebrai EDREX e ean be tbdnd in aimust eddai eeineentratieins o n and otner minor pain syndromes m D budyandbra I in ED E in with asbir Pharmacokinetics Pharmacokinetics o Caffeine has 35 to 5 hours half life 0 Caffeine is metabolized in the ier by the o Extended nait iife for 0 CYP1A2 subgr up of enzymes into three Eideriy metabolites Pregnant Weirnen I Theuphviiine Erunchiai reiaxaiiun Upiu ten hours h Iinfa t n reased haif iife for Smokers Mechanism of Action I Major site of action Adenosine receptors Most potent at adenosine Ai and An I Caffeine works as an antagonism agent Blocks the adenosine receptor Mechanism of Action 7 Adenasineisa neummndulatnv I Modulatan ettect increasing or decreasingthe rate at which neuronstire I w r s n enniunainn thh the G protein processes 7 Agennsine appears to exert sedative depressant and antimnyuisant a nns I anksln slmy own the wash I important In sieeping 7 Adenasinevgic neurons trim a dittuse svsIem I Nu exclusively adennsinelgic pathways I Adenosine s1imulates GAEAI inhibitnlv neurons Mechanism of Action Adenosine is created from the process by which the body breaks down ATP for energy I TP is used throughout the oooyror energy I Useoror high energy oursts such as exerCiSirig and running I Phosphates rorrn a high energy ooho I Ceiis breakthe phosphate pond to extrapolate the eher the adenosine Ody I When the phosphates are pulled on is now rreeto have an errect in the o Mechanism of Action Ar Realm inniaitexaman new Davimme home mam seeminvmumis Remmsvmdmianm P slawsmea wmmekimse kancsmmmmemxmanim Pmmxul Azt iteptmstinuiminnaiaiy a 2 st n ia E imaasemneemuaim Pmmxul Mechanism of Action I Adenosine Ar recepto rs Inhibit the release of dopamine and glulamate Limit the release of acetylcholine l Blockade ofAi receptors Modest reward Increased vigi lance and mental acuity Creates arousal effect Mechanism of Action I Adenosine AzA receptors Stimula e GABAA neurons of inhibitory pathways Inhibit dopamine activity I Blockade UfAm receptors Increases the potency of endogenous dopamine Mechanism of Action I Caffeine facilitates a disinhibition process at adenosine receptor sites I Caffeine removes the negative effeds of nosine from dopamine receptors increasing dopamine activity Caffeine does not stimulate dopamine release NICOTINE NICOTINE I Primary active ingredient in tobacco I One ofthe three most widely used psychoactive drugs I Few or no therapeutic applications I Important because ofwidespread use and toxicity Background Information I Indigenous to the Americas I 1492 Columbus beaches in West Indies Natives offer them tobacco as gilt I 1556 rst plants taken to Europe I 1571 believed to have cun39ng properties for 36 different ailments I 15751600 becomes duty of every man of fashion worth its weight in silver Background Information I 1881 Cigarette rolling machine invented I 3189 24 billion cigarettes produced annually in i oh 3 billion cigarettes sold in us 191213 billion cigarettes sold in US I VWi ll through mid196039s smoking considered coo I Now beginning to be shunned as unhealthy and unwise Background Information I Responsible for the deaths of 1100 Americans every day I Each day EEIEIEI Amirimn teenagers NtnEirfiri cigarette SUDDchiidrenbecurre ie uiarsrrukers mun ufthese Will diefrurn Srmklng related disease I 9 in 10 smokers become addicted before age 21 Background Information Backgron Information I 12 of all people who have smoked have quit I quotA American adults who smoke has fallen from 50 in 1965 to 25 in 1998 I Smoking identi ed as the major preventable cause death and disability As far as 30 vears ago o Nicotine is only one of about 4000 compounds released by burning tobacco o Adverse cardiovascular pulmonary and carcinogenic effects are from the other ompounds Effects 0 Nicotine exerts powerful effects on ralh o Spll lal cord o Perlpheral hervous svsterh 0 Heart N lous other ooov structures Effects 0 Stimulation ofthe vomit center in the brain stem and sensory receptors in the stomach o Nausea lh earlv stages of srholltlhg olerahoe develops raplolv weight gain v suppresslhg appetlte Effects Stlmulates release or ADH ahtloluretle hormone eaushg rlulo retehtloh Reduces aetlvltv or arrereht herve rloers rrorh rhuseles Reductlunlnmuscletune Mavoepanlallvhvolveowuhrelavallohehect KnghEr ooses I Ean lnduce nervousness and tlemurs e lzures inlDXlE uvemuse Smoh as mated Wlth hereaseo oeeurrehee or pahle o p l olsoroers Effects 0 In the CNS nicotine increases 0 Sel lsol lmotol performance Attehtloh w rhorv oohsolloatloh Effects Effect 0 Nicotine can improve performance on vigilance and rapid information processing 0 Effects are greater for working memory ratner tnan iong term memor W tine exerts an antidepressant effect i n moking rates among depressed du is may be an attempt at self o Nicotine exerts a potent reinforcing action 0 indirect activation or midorain dopamine neurons o Greatest in eariy pnases Diminisnes oyer time argoking is continued to ayoid Withdrawal toms Reproductive Effects Reproductive Effects o Smoking during pregnancy increases rates abumuri Early postpartum death Preterm deiiyeries uterine growth retardation is increased 40 t deatns per year attributed to 0 Smoking reduces oxygen delivery to the fetus resulting in varying degree offetal hypoxia 0 Fetus does not receive as much oxygeri F s oking may result in irreversible quoti t lectual and physical de ciencies e nce or ADHD m Withdrawal Symptoms Tolerance o Nicotine doe appear induce a pronounced degree or oioiogicai toierance inereased use in eariy stages Wnien usuaiiy ieyeis err as smoking is eentinued Smokers adiust nieetine intake to maintain 2m to 4m ugrarns per miiiiiiter er piasma induce pnysioiogicai and psycnoiogicai nce o ntense nicotine craying o irritaoiiity o Ariger o Dirricuity concentrating o Restlessriess Therapy 0 Nicotine r eplacement therapy doubles uccessful quit rates 0 Skll i o Gum oNlcotlne nasal spray my se of Zyban has also been shown to in a successful quit rates Pharmacokinetics Easily absorbed m the body tings Bucczl and mi mucosa I Sign l Gastxmnteshml tuct Nicoane is suspended m the rmnute pamcles tars m smoke Orally admmstexed blood levels otmcoane are comparable to smohng Pharmacokinetics Only about 20 ofthe mcoane m a cigarette is inhaled and absorbed mto the bloodstream Nicotmewhichis notxmmedmtely absorbedxs rapidly metabolized by the hepaac enzyme CYP2A6 Inhataaon allows controllabxhty of dose quenty ofbxuths Depth ofbxuths Tim m lun Numbexufcxgaxettes Pharmacokinetics Nicoane is thoroughly dtstnbuted m the body utmn Nob E p a Appem h zllbuddy The hvexmetabohzes 80 to 90 before excretaon to the iadn s annxy metabolite is eoanme The ehrmnahon haltbte m chronic users 15 aboutz hrs Mechanism of Action Nicotine activates specifc acetylcholine ACh receptors known as nicotinic receptors l Nicotinic receptors are located throughout the body 7 Skeletal musc le 7 Sympathetic arid parasympathetic neurons 7 cns Mechanism of Action ACh is released broken down and reabsorbed very quickly microsecond allowing the receptor to respond to new Ach l ACh receptors work as a fast rst messenger s tem eAttached directly to ion channels 7 Binding has an immediate response Mechanism of Action Nlcuhne replaces AC Buns turuu ACh r Peripheral Nervous System Actlvatlon of nlcotlnlc receptors m the PNS Increases blood pressure and eart r ate Causes the release ofeplnephnne from the adrenal glands lncrea es the tone secretaorls and achlty ofthe h n mm mm gastrolnteshnal tract uh untagm We r mgm oFem mhml mam uytlmmm mt Central Nervous System Nlcohmc r eceptors arewldely dlsmbuted and may be present at the presyhaptactemh ls otheuro swhlch secrete Dopamlne Acetylchulme Glutamlne Acnvataor by mcohne mcreases the acne n ransmltter faclhtates the release and m the bram of these Central Nervous System Dopamlne levels are Increased m the l Forebrmn I Stlmu atlon ofthese areas account for the be moral relnforcement sum antldepressant a mcotme ulant nd addlctlve propertles of Central Nervous System I Increases m acetylchollne Contnbute o the cognltlve potenuauon an mory facllltatlon properues of nlcotlne Facl ltatlon ofglutamlnerglc neurotransmlsslons contrlbu te to the lmprovement m me functlonlng smahhq accelevates the devasltlnq af fat h the avtevles lheesree We smahhq quotmales the We h the lungs lmpehhq 125 st 75m ENDNEema smahhq weakens the Wmune sVstem Smoking Diseases rut ofhezvl zuztk me Dwatlan Smoking Diseases I Lung cancer I 9095 of male aths I 7075 of female deaths I Cancer ofthe mouth and throat I Chewing tobacco rm amaqumim m Smoking Diseases I Cardiovascular disease onoxide decreass amount of cxygen delivered to the heartwhile nicotine increases the workload I Carbon monoxide and nicotine increase narrowing atheroscleros39s and clotting thrombos39s in the coronary arteries I Increased risk of coronary heart d39sease Smoking Diseases I About 4000 Americans per year die from lung cancer caused by secondhand smoke I 37000 deaths per year from heart disease caused by second hand smoke So u rces lilien Robert M 2001 A H39iner of Drug Action n39nth ed llaI39ehe andN39rothe pp 220248 NY New York Worth PublHners I Tompson Richard M 2000 The Brah39A Newoscience Priner Mident NY New York Worth PublHners httplhomehowiuf Norksxomcaffehehtm Wm um7nr39nt httn39lwww auantumcl39nic 39 39 39 htt www bs or bh nova c39 arette nicot39ne html
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