drugs in everyday life ges 1510 john h.k. yeung department of pharmacology c.u.h.k
TRANSCRIPT
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Drugs in Everyday LifeGES 1510
Drugs in Everyday LifeGES 1510
John H.K. YeungJohn H.K. Yeung
Department of Pharmacology Department of Pharmacology C.U.H.K.C.U.H.K.
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PHARMACOLOGYPHARMACOLOGY
Scientific study of the interactions Scientific study of the interactions between drugs and the body between drugs and the body
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What are drugs?What are drugs?
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Where do drugs come Where do drugs come from?from?
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Origin of DrugsOrigin of Drugs
PlantPlant
AnimalAnimal
SyntheticSynthetic
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The relationships between science and medicineThe relationships between science and medicine
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Pharmaceutical(Medicinal)Chemistry
Pharmacology and
Toxicology
Therapeutics
Pharmacy
Patients
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HO NHCOCH3
Chemical : N-acetyl-p-amino-phenol
.
Naming of a Drug
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HO NHCOCH3
Chemical : N-acetyl-p-amino-phenol
Generic : Paracetamol (BP)Acetaminophen (USP)
.
Naming of a Drug
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HO NHCOCH3
Chemical : N-acetyl-p-amino-phenol
Generic : Paracetamol (BP)Acetaminophen (USP)
Trade : Panadol (500)Tylenol (300)Calpol etc.
Naming of a Drug
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Drugs = Medicines only?Drugs = Medicines only?
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DRUG LivingTissue
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DRUG LivingTissue
Effect
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DRUG LivingTissue
Effect
MEDICINE
POISON
AIRPOLLUTANTS
INSECTICIDES
FOODADDITIVES
COSMETICS
HERBICIDES
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Drugs in Everyday LifeDrugs in Everyday Life
Medical useMedical use Non-medical useNon-medical use
““Social Drugs”Social Drugs” Health and diet supplementsHealth and diet supplements Drugs of abuseDrugs of abuse
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Pharmacological Effects of SmokingPharmacological Effects of Smoking
CNS effectsCNS effects inhibits spinal reflexes to produce skeletal inhibits spinal reflexes to produce skeletal
muscle relaxationmuscle relaxation produces sense of alertnessproduces sense of alertness
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Pharmacological Effects of SmokingPharmacological Effects of Smoking
Peripheral effectsPeripheral effects increases cardiac outputincreases cardiac output increases blood pressureincreases blood pressure vasoconstrictionvasoconstriction sweatingsweating decreases gastrointestinal motilitydecreases gastrointestinal motility
Addictive ?Addictive ?
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Withdrawal Syndrome to NicotineWithdrawal Syndrome to Nicotine
Increased irritabilityIncreased irritability
Impaired performance of psychomotor Impaired performance of psychomotor taskstasks
AggressivenessAggressiveness
Sleep disturbanceSleep disturbance
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Harmful Effects of SmokingHarmful Effects of Smoking
CancerCancer mouth, throat, oesophagus and lungmouth, throat, oesophagus and lung
Coronary heart diseaseCoronary heart disease
Chronic bronchitisChronic bronchitis
Affects pregnancy Affects pregnancy decrease in birth weightdecrease in birth weight increase perinatal mortalityincrease perinatal mortality
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Pharmacological Effects of AlcoholPharmacological Effects of Alcohol
Depressant effect on the Central Nervous Depressant effect on the Central Nervous SystemSystem
Impairs intellectual and motor performanceImpairs intellectual and motor performance
Produces cutaneous vasodilatation (central in Produces cutaneous vasodilatation (central in origin) which causes a warm feeling but origin) which causes a warm feeling but actually increase heat lossactually increase heat loss
Increases salivary and gastric secretionsIncreases salivary and gastric secretions
Diuretic effectDiuretic effect
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Pharmacological Effects of AlcoholPharmacological Effects of Alcohol
Acute intoxicationAcute intoxication slurred speechslurred speech decrease in motor coordinationdecrease in motor coordination increased self-confidenceincreased self-confidence euphoriaeuphoria
Excessive consumption long-term causes liver Excessive consumption long-term causes liver damagedamage
Affects fetal developmentAffects fetal development
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Withdrawal Symptoms of AlcoholWithdrawal Symptoms of Alcohol
Develops after about 8 hoursDevelops after about 8 hours severe tremor, sometimes hallucinations, severe tremor, sometimes hallucinations,
which lasts for about 24 hourswhich lasts for about 24 hours confused and agitated over the next few confused and agitated over the next few
daysdays aggressive behaviouraggressive behaviour nausea and vomiting, sweating and fevernausea and vomiting, sweating and fever
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NITRITE
+
PROTEIN
CombustionNITROSAMINES
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Good drugs vs. Bad drugs ?Good drugs vs. Bad drugs ?
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Narcotics OriginNarcotics Origin
MorphineMorphine
EndorphinsEndorphins
MethadoneMethadone
PlantPlant
AnimalAnimal
SyntheticSynthetic
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Narcotic PropertiesNarcotic Properties
AnalgesiaAnalgesia
EuphoriaEuphoria
ConstipationConstipation
Pupil constrictionPupil constriction
Respiratory Respiratory depressiondepression
Nausea vomitingNausea vomiting
HypotensionHypotension
AddictionAddiction
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NSAID OriginNSAID Origin
SalicylatesSalicylates
----
AspirinAspirin
PlantPlant
AnimalAnimal
SyntheticSynthetic
NSAID = Non-Steroidal Anti-Inflammatory Drug
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Properties of AspirinProperties of Aspirin
AnalgesiaAnalgesia
Anti-inflammatoryAnti-inflammatory
AntipyreticAntipyretic
Anti-platelet Anti-platelet aggregationaggregation
Gastric bleedingGastric bleeding
Acid-base Acid-base imbalanceimbalance
Reye’s syndromeReye’s syndrome
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How do drugs work ?How do drugs work ?
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HOW DRUGS WORK
Non-specific
Specific
Receptor Drug
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More serious stuff More serious stuff starts here !!starts here !!
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Basic Concepts in PharmacologyBasic Concepts in Pharmacology
PharmacodynamicsPharmacodynamics
PharmacokineticsPharmacokinetics
Routes of AdministrationRoutes of Administration
Dosage and dosing intervalsDosage and dosing intervals
Drug receptors and specificityDrug receptors and specificity
ToxicityToxicity
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Pharmacodynamics and PharmacokineticsPharmacodynamics and Pharmacokinetics
PharmacodynamicsPharmacodynamics
DrugDrug BodyBody
PharmacokineticsPharmacokinetics
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DRUGSITEOF
ACTION
EFFECTS
BLOOD
SYSTEMICCIRCULATION
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PharmacokineticsPharmacokinetics
AAbsorptionbsorption
DDistributionistribution
MMetabolismetabolism
EExcretionxcretion
Disposition : Disposition : DD + + MM + + EE
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Drug BodyDrug Body
Molecular sizeMolecular size
Lipid solubilityLipid solubility
IonizationIonization
AbsorptionAbsorption
DistributionDistribution
EliminationElimination
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Routes of administrationRoutes of administration
Enteral administrationEnteral administrationSublingualSublingual
OralOral
RectalRectal
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Routes of administrationRoutes of administration
Parenteral administrationParenteral administrationintravenousintravenous
intra-muscularintra-muscular
subcutaneoussubcutaneous
intrathecalintrathecal
intra-arterialintra-arterial
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Routes of administrationRoutes of administration
OthersOtherstopicaltopical
inhalationinhalation
intra-vaginalintra-vaginal
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How fast does the drug act ?How fast does the drug act ?
How long does the drug effect How long does the drug effect lasts ?lasts ?
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0 2 4 6 8 10 12Time (hour)
Dru
g co
ncen
trat
ion
in b
lood
Onset and duration of drug action
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0 2 4 6 8 10 12Time (hour)
Dru
g co
ncen
trat
ion
in b
lood
MEC
Onset and duration of drug action
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0 2 4 6 8 10 12Time (hour)
Dru
g co
ncen
trat
ion
in b
lood MTC
MEC
Onset and duration of drug action
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0 2 4 6 8 10 12Time (hour)
Dru
g co
ncen
trat
ion
in b
lood MTC
MEC
Onset and duration of drug action
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How are new drugs discovered ?How are new drugs discovered ?
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Drug DiscoveryDrug Discovery
Chemical modification of a known Chemical modification of a known moleculemolecule
Screening of natural products or Screening of natural products or previously discovered chemical entities previously discovered chemical entities for biological activityfor biological activity
Rational drug design based on an Rational drug design based on an understanding of biological mechanismsunderstanding of biological mechanisms
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natural drug source
Possible Pathways in Drug Development
pharmacological profileof active principle
chemical synthesisprogramme
mechanism of action
potential clinical utility
animal models ofthe disease state
use in medicineclinical trials
metabolism
toxicology
formulation
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Pharmacological Profile TestsPharmacological Profile Tests
Molecular levelsMolecular levels
Cellular levelsCellular levels
System / Disease ModelsSystem / Disease Models
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Pharmacological Profile TestsPharmacological Profile Tests
Molecular levelsMolecular levelsReceptor bindingReceptor binding
affinity and specificityaffinity and specificity
Enzyme activityEnzyme activity inhibition and selectivityinhibition and selectivity
Cytochrome P450Cytochrome P450 effects on drug metabolismeffects on drug metabolism
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Pharmacological Profile TestsPharmacological Profile Tests
Cellular levelsCellular levelsCell functionCell function
receptor activityreceptor activity
Isolated tissueIsolated tissue vascular activity vascular activity effects on other smooth muscleseffects on other smooth muscles
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Pharmacological Profile TestsPharmacological Profile Tests
System / Disease ModelsSystem / Disease ModelsBlood pressureBlood pressure Central nervous systemCentral nervous systemCardiac effectsCardiac effects Gastrointestinal effectsGastrointestinal effectsRespiratory systemRespiratory system Diuretic activityDiuretic activityBlood coagulationBlood coagulationPeripheral autonomic nervous systemPeripheral autonomic nervous systemCirculating hormones, cholesterol and blood sugarCirculating hormones, cholesterol and blood sugar
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Pre-clinical Safety and ToxicityPre-clinical Safety and ToxicityAcute toxicityAcute toxicity
LDLD5050, maximum tolerated dose, use 2 species, 2 , maximum tolerated dose, use 2 species, 2 routes, single doseroutes, single dose
Sub-acute toxicitySub-acute toxicityUse 2 species and 3 doses to study up to 6 Use 2 species and 3 doses to study up to 6 monthsmonths
Chronic toxicityChronic toxicity1-2 years; for drugs intended for prolonged use,1-2 years; for drugs intended for prolonged use,usually runs concurrently with clinical trialusually runs concurrently with clinical trial
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Pre-clinical Safety and ToxicityPre-clinical Safety and ToxicityEffect on reproductionEffect on reproduction
Animal mating behaviour, reproduction, Animal mating behaviour, reproduction, parturition, progeny, birth defectsparturition, progeny, birth defects
Carcinogenic potentialCarcinogenic potentialUse 2 species for 2 years, for drugs intended Use 2 species for 2 years, for drugs intended for prolonged usefor prolonged use
Mutagenic potentialMutagenic potentialEffects on genetic stability of bacterial and Effects on genetic stability of bacterial and mammalian cells in culturemammalian cells in culture
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Clinical TestingClinical Testing
Volunteer studies (25-50)Volunteer studies (25-50)
Phase I clinical studies (25-50)Phase I clinical studies (25-50)
Phase II clinical studies (50-200)Phase II clinical studies (50-200)
Phase III clinical studies (250-1000)Phase III clinical studies (250-1000)
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Clinical TestingClinical Testing
Volunteer studies (25-50)Volunteer studies (25-50) human pharmacologyhuman pharmacology adverse effectsadverse effects pharmacokinetics after single or multiple pharmacokinetics after single or multiple
dosedose
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Clinical TestingClinical Testing
Phase I clinical studies (25-50)Phase I clinical studies (25-50) clinical pharmacology of the drugclinical pharmacology of the drug short term safety, efficacyshort term safety, efficacy pharmacological and pharmacokinetic pharmacological and pharmacokinetic
effects in diseaseeffects in disease
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Clinical TestingClinical Testing
Phase II clinical studies (50-200)Phase II clinical studies (50-200) further evidence of efficacy and safety in further evidence of efficacy and safety in
larger number of patientslarger number of patients
Phase III clinical studies (250-1000)Phase III clinical studies (250-1000) full scale clinical trialfull scale clinical trial
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PLACEBOPLACEBO
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Drugs in Everyday LifeDrugs in Everyday Life
Commonly used drugsCommonly used drugs analgesicsanalgesics anti-inflammatory drugsanti-inflammatory drugs antibioticsantibiotics drugs for gastrointestinal tract drugs for gastrointestinal tract
disordersdisorders
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AnalgesicsAnalgesics
Morphine-like drugsMorphine-like drugs opioidsopioids
Non-steroidal anti-inflammatory drugsNon-steroidal anti-inflammatory drugs aspirin and related substancesaspirin and related substances
Local anaestheticsLocal anaesthetics
Other drugs used for specific conditionsOther drugs used for specific conditions e.g. migraine, labore.g. migraine, labor
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AntibioticsAntibiotics
Substances produced by some micro-Substances produced by some micro-organisms which kill or inhibit the organisms which kill or inhibit the growth of other micro-organismsgrowth of other micro-organisms antibacterial drugsantibacterial drugs antiviral drugsantiviral drugs antifungal drugsantifungal drugs
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Basic concepts of antibioticsBasic concepts of antibiotics
Static and cidal effectsStatic and cidal effectsResistance to antibioticsResistance to antibioticsAdverse effectsAdverse effectsHost factorsHost factors
severity of infection, host defense severity of infection, host defense mechanisms, pharmacokinetic factorsmechanisms, pharmacokinetic factors
Drug combinationsDrug combinationsPatient compliancePatient compliance
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Drugs for G.I. DisordersDrugs for G.I. Disorders
Ulcer healing drugsUlcer healing drugs
AntacidsAntacids
LaxativesLaxatives
Anti-diarrhoea drugsAnti-diarrhoea drugs
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Drugs for G.I. DisordersDrugs for G.I. Disorders
Ulcer-healing drugsUlcer-healing drugsAcid secretion reducersAcid secretion reducers
cimetidine, ranitidine, omeprazole, cimetidine, ranitidine, omeprazole, pirenzipinepirenzipine
Mucosal strengthenersMucosal strengtheners sucralfate, bismuth subcitrate, sucralfate, bismuth subcitrate,
carbenoxolonecarbenoxoloneAntibioticsAntibiotics
metronidazole, tetracycline or amoxycillinmetronidazole, tetracycline or amoxycillin
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Drugs for G.I. DisordersDrugs for G.I. Disorders
AntacidsAntacidsSodium hydrogen carbonateSodium hydrogen carbonate
Calcium carbonateCalcium carbonate
Magnesium hydroxideMagnesium hydroxide
Aluminium hydroxideAluminium hydroxide
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Drugs for G.I. DisordersDrugs for G.I. Disorders
LaxativesLaxativesBulk laxatives (increase the volume of the Bulk laxatives (increase the volume of the
intestinal contents, stimulate peristalsis)intestinal contents, stimulate peristalsis) cellulose, methyl-cellulosecellulose, methyl-cellulose
Stimulant laxatives (increase gut motility)Stimulant laxatives (increase gut motility) anthraquinones (senna and cascera), anthraquinones (senna and cascera),
bisacodylbisacodylLubricants (softening and/or lubricating)Lubricants (softening and/or lubricating)
liquid paraffinliquid paraffin
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Drugs for G.I. DisordersDrugs for G.I. Disorders
Anti-diarrhoea drugsAnti-diarrhoea drugsMorphine-like agentsMorphine-like agents
morphine, codeine, diphenoxylate, morphine, codeine, diphenoxylate, loperamideloperamide
AdsorbentsAdsorbents kaolin, chalkkaolin, chalk
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Drugs for non-medical purposeDrugs for non-medical purposeDrugs which are rigidly controlled by law in their Drugs which are rigidly controlled by law in their
production, distribution and sale. Use of these production, distribution and sale. Use of these drugs is prohibited.drugs is prohibited.
Drugs which are potentially dangerous. Use of Drugs which are potentially dangerous. Use of these drugs is under vigilance: penalties for these drugs is under vigilance: penalties for misuse; taxes for sale of these drugs.misuse; taxes for sale of these drugs.
Drugs which may cause damage to individuals if Drugs which may cause damage to individuals if used in excess. Controls mainly by taxation.used in excess. Controls mainly by taxation.
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Drugs in Everyday LifeDrugs in Everyday Life
Drugs for non-medical purposeDrugs for non-medical purpose alcoholalcohol caffeinecaffeine tobaccotobacco ““health products”health products”
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Drugs in Everyday LifeDrugs in Everyday Life
““illegal” drugsillegal” drugs cannabiscannabis sedative-hypnotic drugssedative-hypnotic drugs opiumopium morphine and related drugsmorphine and related drugs cocainecocaine amphetamine and related drugsamphetamine and related drugs
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SOME DRUGS OF ABUSESOME DRUGS OF ABUSE
DrugDrug Trade NameTrade Name ““Street Name”Street Name”
AmphetamineAmphetamine ------ 大力丸大力丸 安菲他命安菲他命BrotizolamBrotizolam LendorminLendormin 13A13A 屋仔屋仔CannabisCannabis ------ 大麻大麻 ““Grass”Grass”ChlordiazeproxideChlordiazeproxide LibriumLibrium 綠豆仔綠豆仔 利眠寧利眠寧CocaineCocaine ------ 可卡因可卡因 CokeCoke CrackCrackDiazepamDiazepam ValiumValium 羅氏五號羅氏五號 十號十號FlunitrazepamFlunitrazepam RohypnolRohypnol White CrossWhite Cross (十字架)(十字架)KetamineKetamine KetalarKetalar KK 仔仔
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SOME DRUGS OF ABUSESOME DRUGS OF ABUSE
DrugDrug Trade NameTrade Name ““Street Name”Street Name”
LSD (Lysergic acidLSD (Lysergic aciddiethylamide)diethylamide)
------ 迷幻藥迷幻藥
MethaqualoneMethaqualone MandraxMandrax 忽得忽得Methylenedioxy-Methylenedioxy-methamphetaminemethamphetamine
------ MDMAMDMA “ “Esctasy”Esctasy”忘我忘我
MethamphetamineMethamphetamine ------ 冰冰MidazolamMidazolam DormicumDormicum 羅氏藍精靈羅氏藍精靈ScobarbitalScobarbital SeconalSeconal Lily 40Lily 40 莉莉四十莉莉四十TriazolamTriazolam HalcionHalcion 藍精靈藍精靈 藍瓜子藍瓜子