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Nonsteroidal AntiInflammatory Drugs NSAIDs

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Title: Nonsteroidal AntiInflammatory Drugs NSAIDs


1
  • PRESCRIPTION DRUG ABUSE

Pharmacology Drugs and Disease - Feb. 25, 2004
Greg Connell, Ph.D. Office 3-126 BSBE Phone
624-3132 Emailgconnell_at_lenti.med.umn.edu
2
Drug Abuse
3
Overview
4
1 Definitions
A. Physical dependence
  • A normal physiological adaptation to repeated
    use of
  • some categories of drugs
  • Examples may include
  • down-regulation of receptor number
  • decreased efficiency of the coupling of the
    receptor to the
  • signal transduction mechanism
  • alteration of the drugs metabolism

5
Physical Dependence
6
1 Definitions
B. Tolerance
  • Occurs when increasing amounts of the drug are
    required
  • to achieve the same physiological or
    psychological effect.
  • Indicative of the development of a physical
    dependence.

7
Tolerance
8
Tolerance
9
1 Definitions
C. Cross-tolerance
  • The development of tolerance to one drug also
    increases
  • tolerance to related drug categories

10
1 Definitions
D. Withdrawal syndrome
  • Occurs when drug administration to a physically
    dependent
  • person is abruptly terminated
  • Symptoms are characteristic of the class of drug
    and tend to
  • be opposite the original effects of the drug
    before tolerance
  • developed

11
Withdrawal Syndrome
12
1 Definitions
E. Psychic or psychological dependence
  • The individual believes that the presence of the
    drug is
  • necessary to maintain a state of well being.
  • All major drugs of abuse produce a negative
    emotional
  • state in dependent humans during acute abstinence.
  • Regaining a sense of well-being provides a
    positive
  • reinforcement or craving for continued abuse

13
1 Definitions
F. Drug abuse
  • A behavioral definition the self-administration
    of a drug
  • for non-medical purposes resulting in either a
    psychic
  • and/or physical dependence.

G. Drug misuse
  • Results from either ill advised patterns of
    prescribing by
  • physicians or improper use by patients within the
    context of
  • medical treatment.

14
1 Definitions
H. Addiction
  • A behavioral definition recurrent drug use
    becomes the
  • primary goal and disrupts the ability to function
    in family,
  • social or career settings rather than being an
    incidental
  • part of life.
  • Characterized by three major elements

1. Compulsion to seek and take the drug
2. Loss of control in limiting intake
3. Emergence of a negative emotional state when
access to the drug is prevented
15
2 Biological Basis of Drug Abuse
A. An Evolutionary Perspective
  • The neural mechanisms that regulate emotion and
    behavior
  • were shaped by natural selection to maximize
    Darwinian
  • fitness.
  • Love joins hate, aggression, fear
    expansiveness,
  • withdrawal and so on, in blends designed not to
    promote
  • the happiness of the individual, but to favor the
    maximum
  • transmission of the controlling genes (E.O.
    Wilson)

16
An Evolutionary Perspective
  • Drugs of abuse are inherently pathogenic because
    they create a signal in the brain that indicates,
    falsely, the arrival of a huge fitness benefit
    and thereby hijack the incentive mechanisms of
    liking and wanting.

17
2 Biological Basis of Drug Abuse
B. A Biochemical Perspective
  • The occasional use of an abusable drug is
    distinct from
  • repeated use and the emergence of chronic drug
    addiction.
  • The cellular and molecular mechanisms that
    mediate
  • the transition from occasional controlled drug
    use to addiction
  • are only just beginning to be understood.

18
Biochemistry of Drug Abuse
  • Drug use results in changes to specific
    neurotransmitter systems
  • within a highly limited band of structures
    including specific
  • parts of the amygdala and nucleus accumbens.

19
Biochemistry of Drug Abuse
  • Changes occur in the signals mediated by several
  • neurotransmitters including but not limited to
    dopamine,
  • opioid peptides and cotropin-releasing factor.
  • Increases in neurotransmitter concentrations can
    result in
  • several short-term and long-term changes.

20
Biochemistry of Drug Abuse
(dopamine)
adenyl
cyclase
B
g
Gs
ATP
dopamine
receptor
GTP
GDP
cAMP
cAMP dependent
kinase
alterations in gene expression
cAMP response element- binding protein
21
Significance of Dopamine
  • Sex, chocolate, alcohol, marijuana, amphetamine,
    cocaine,
  • nicotine and heroin all directly or indirectly
    increase the
  • synaptic dopamine concentration within a highly
    localized
  • region of the brain.
  • Dopamine system plays a fundamental role in
    encouraging
  • behaviors, such as feeding, needed for life in
    organisms
  • ranging from slugs to primates.

22
Facilitated Learning Hypothesis
  • Dopamine release highlights or draws attention
    to certain
  • significant events and by underscoring such
    events the
  • dopamine signal helps the animal to learn to
    recognize them
  • and in some cases to repeat them.

23
3. Prescription Drugs with Abuse Potential
  • Drugs that produce a pleasurable effect such as
    an
  • elevated mood, euphoria or calming.
  • Drugs that do not produce a mood altering effect
    are rarely
  • intentionally abused.
  • an exception is anabolic steroid use by athletes

24
3. Prescription Drugs with Abuse Potential
  • Opioid agonists -heroin, morphine, meperidine,
  • oxymorphone, hydrocodone, fentanyl, sufentanil

i. abuse potential () high ii. acute
intoxication euphoria, rush sedation iii.
withdrawal symptoms () high but are rarely
life threatening. Symptoms can include opioid
craving, irritability, hyperalgesia, cramps,
muscle aches, nausea/vomiting, mydriasis,
sweating, tachycardia, hypertension, fever.
25
Opioid Agonists
  • additional consequences () high
    life-expectancy
  • decreased by 50 i.v. users risk HIV infection.

v. treatment
  • switch from short-acting drug to long-acting
    drug like
  • methadone
  • clonidine a2 agonist reduces aspects of
    withdrawal
  • naltrexone

26
3. Prescription Drugs with Abuse Potential
B. anxiolytic-sedative-hypnotics
B.1 Barbituates secobarbitol, pentobarbitol,
amobarbitol
  • abuse potential () high
  • Acute intoxication
  • 1. Stimulant-like effects at low doses
    euphoria,
  • increased talkativeness
  • 2. Depressant at high doses ataxia,
    slurred speech

27
Anxiolytic-Sedative-Hypnotics
B.1 Barbituates
  • withdrawal symptoms () high life
    threatening,
  • tremor, nausea, sweating, hypertension, seizures
  • iv. additional consequences () high death
    from
  • overdose, suicide

B.2 Benzodiazepines diazepam, flurazepam
  • abuse potential () low
  • acute intoxication similar to barbiturates
  • withdrawal symptoms () intermediate cramps,
  • agitation, anxiety, rarely seizures

28
3. Prescription Drugs with Abuse Potential
C Stimulants
C.1 amphetamine
i. structure
CH
NH
CH
2
2
  • amphetamine is a mixture of two stereoisomers
  • 1. d-isomer (dextroamphetamine) - stimulates
    the CNS
  • more effectively than the l-isomer
  • 2. l-isomer (levoamphetamine) - stimulates
    the
  • cardiovasculature system more than the d-isomer

29
Amphetamine
ii. function
  • increases the synaptic dopamine concentration
    resulting
  • in an increased state of wakefulness and
    attentiveness.
  • acts primarily on two areas of brain
  • 1. reticular activating system (regulation of
    sensory
  • input into the brain)
  • 2. medial forebrain bundle (pleasure center)

30
Amphetamine
iii. clinical uses
  • narcolepsy
  • attention deficit hyperactivity disorder (ADHD)
  • appetite suppression -discouraged now because
  • there is significant abuse potential

iv. adverse effects
  • cardiovascular side effects
  • irritability, nervousness, restlessness
  • long-term intoxication can result in a
    schizophrenia-
  • like reaction

31
Amphetamine
v. abuse potential () very high
  • acute intoxication euphoria, increased
    alertness,
  • increased motor activity

vii. withdrawal symptoms () low drug craving,
fatigue, bradycardia
viii. additional consequences () high
depression, toxic-psychosis, cerebrovascular and
cardiovascular accidents
32
Stimulants
C.2 Methylphenydate (Ritalin)
  • Structure, clinical uses, adverse effects and
    withdrawal
  • symptoms similar to amphetamine.
  • Mild CNS stimulant that does not have
    significant
  • peripheral actions.
  • Mechanism of action is not completely
    understood,
  • but it may involve blockage of dopamine uptake.

33
3. Prescription Drugs with Abuse Potential
D. Marijuana (D?? -tetrahydrocannibinol)
i. therapeutic uses
  • Approved (THC) for the prevention of nausea and
  • stimulation of appetite in cancer patients
    receiving
  • chemotherapy and in patients with AIDS.

2. Other uses that are not approved include
reduction of the intraocular pressure in
glaucoma, analgesic, muscle relaxant.
ii. mechanism of action agonist acting on the
endogenous cannabinoid receptors
34
Marijuana
iii. abuse potential () low
iv. acute intoxication euphoria, heightened
sensory perception, hallucinations and motor
impairment at high doses
v. withdrawal symptoms () low restlessness,
irritability, agitation, sleep disturbances,
nausea
35
4. Reasons to be Aware of a Drug Abuse Potential
  • A professional responsibility to prescribe drugs
    appropriately
  • The physical and mental condition of the patient
    is often
  • related directly or indirectly to drug abuse
  • A personal responsibility not to become an easy
    target for
  • diversion

36
5. Individuals of Concern
  • The professional patient
  • Type I patient - obtains drugs of abuse through
    deception
  • of health care providers.
  • Type II patient - initially takes drugs for a
    legitimate
  • medical condition but later becomes addicted.
  • Health care professionals - potential for
    self-medication

37
6. Physicians Who Prescribe Inappropriately
  • Common causes for Minnesota Medical Practice
    actions
  • prescribing for patients with known
    dependencies or
  • addiction histories
  • prescribing controlled substances for chronic
    pain,
  • anxiety or insomnia without proper reassessment.
  • prescribing without performing physical
    examinations.
  • prescribing in the face of known drug
    interactions.

38
6. Physicians Who Prescribe Inappropriately
  • The Four Ds - Physicians as sources of drug
    diversion
  • (AMA National Informal Steering Committee on
    Prescription
  • Drug Abuse)
  • dishonest
  • disabled
  • deceived
  • dated

39
7. Protecting Yourself from the Type I Patient
  • Protection of prescription pads
  • store unused prescription pads in a safe place
  • minimize the number of pads in use at one time
  • have prescription blanks numbered consecutively
    so that
  • missing sheets would be detected
  • never sign prescription blanks in advance
  • Write out the actual quantity in addition to
    using an
  • Arabic or Roman numeral
  • Do not use prescription blanks for writing
    notes or memos

40
7. Protecting Yourself from the Type I Patient
  • Patient behavior which may suggest drug abuse
  • request for specific medications
  • request for higher or more frequent dosing
  • claims of allergy or lack of efficacy of
    specific drugs
  • evasive answers regarding medical history
  • traveling through town -not a resident
  • does not give name of primary or referring
    physician
  • claims to have lost prescription
  • requests appointment for late afternoon

41
LECTURE OBJECTIVES
  • Understand the following definitions
  • physical dependence
  • tolerance
  • cross-tolerance
  • withdrawal
  • psychic or psychological dependence
  • drug abuse
  • drug misuse
  • addiction

2. Be aware of the biological basis of addiction
and the major classes of abused drugs opioids,
anxiolytic-sedative-hypnotics, stimulants,
marijuana
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