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    Central Nervous System Drugs II

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    Sharifah Nadzirah
    This document provides an overview of central nervous system drugs, including CNS depressants and opioids. It discusses how opioids such as morphine are derived from poppy plants and bind to mu, delta, and kappa opioid receptors in the brain to produce effects like analgesia, respiratory depression, and euphoria. Tolerance and physical dependence can develop with regular opioid use. The document also examines antipsychotic drugs, which are commonly used to treat schizophrenia. Typical antipsychotics non-selectively block dopamine and serotonin receptors, while atypical antipsychotics more selectively target dopamine receptors. Both types of drugs can cause extrapyramidal side effects but atypicals have a lower risk.

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    Central Nervous System Drugs II

    Uploaded by

    Sharifah Nadzirah
    163 views25 pages
    This document provides an overview of central nervous system drugs, including CNS depressants and opioids. It discusses how opioids such as morphine are derived from poppy plants and bind to mu, delta, and kappa opioid receptors in the brain to produce effects like analgesia, respiratory depression, and euphoria. Tolerance and physical dependence can develop with regular opioid use. The document also examines antipsychotic drugs, which are commonly used to treat schizophrenia. Typical antipsychotics non-selectively block dopamine and serotonin receptors, while atypical antipsychotics more selectively target dopamine receptors. Both types of drugs can cause extrapyramidal side effects but atypicals have a lower risk.

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    CNS DRUG

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    This document provides an overview of central nervous system drugs, including CNS depressants and opioids. It discusses how opioids such as morphine are derived from poppy plants and bind to mu, delta, and kappa opioid receptors in the brain to produce effects like analgesia, respiratory depression, and euphoria. Tolerance and physical dependence can develop with regular opioid use. The document also examines antipsychotic drugs, which are commonly used to treat schizophrenia. Typical antipsychotics non-selectively block dopamine and serotonin receptors, while atypical antipsychotics more selectively target dopamine receptors. Both types of drugs can cause extrapyramidal side effects but atypicals have a lower risk.

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    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    163 views25 pages

    Central Nervous System Drugs II

    Uploaded by

    Sharifah Nadzirah
    This document provides an overview of central nervous system drugs, including CNS depressants and opioids. It discusses how opioids such as morphine are derived from poppy plants and bind to mu, delta, and kappa opioid receptors in the brain to produce effects like analgesia, respiratory depression, and euphoria. Tolerance and physical dependence can develop with regular opioid use. The document also examines antipsychotic drugs, which are commonly used to treat schizophrenia. Typical antipsychotics non-selectively block dopamine and serotonin receptors, while atypical antipsychotics more selectively target dopamine receptors. Both types of drugs can cause extrapyramidal side effects but atypicals have a lower risk.

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    of 25

    Psychopharmacology:

    Central Nervous System Drugs II

    AP Dr Ahmad Rohi Ghazali

    OUTLINE
    Central Nervous System Drugs

    CNS Depressants

    Anxiolytics

    Neuroleptics

    CNS Stimulants

    ANALEPTICS

    PSYCHOSTIMULANTS
    Opioids
    PSYCHODYSLEPTICS

    CNS DEPRESSANTS :
    OPIOIDS

    BACKGROUND:
    OPIUM:
    poppy juice extracts Papaver somniferum.
    medical (diarrhea & pain) + social uses.
    about 20 & more active alkaloids.
    Opioid:
    substances with morphine-like effects.
    antagonism with naloxone.
    enkephalin, endorphin + dynorphin +
    Synthetic analogues).
    Opiate:
    morphine derivative drugs.
    similar chemical structure to morphine.
    NOT including endogenous neuropeptides.

    Morphine:

    OPIUM:
    1% Papaverine, 6% Narcotine,
    10% Morphine + 0.5% Codein.
    The structure of morphine + all
    opium derivatives are
    characterized by the piperidine
    ring.
    Pharmacological effects:
    Analgesic (antinociceptive)
    antidiarrhea
    physical dependence
    respiratory depression
    Hydrophilic compared to heroin

    Mechanism of Action, MOA of Opioid:

    Pharmacological Responses of Opioid Sub Receptors :


    Receptor Type

    Analgesia
    Supraspinal
    Spinal
    Peripheral

    ++ / ++ / ++
    ++ / -

    +
    ++

    Respiratory
    Depression

    ++

    Pupil (eye)

    Constriction

    Dilatation

    GIT Motility

    Smooth Muscle
    Spasm

    ++

    Behaviour / Emotion

    Euphoria ++
    Sedation ++

    Dysphoria +
    Sedation +

    Dysphoria ++
    Psychotomimetic

    Physical Dependence

    ++

    Receptor Type

    Compounds

    Opioid Peptides:
    Beta-endorphin
    Leu-enkaphalin
    Dynorphin

    +++
    +
    ++

    +++
    +++
    +

    +++
    +++

    True Agonist:
    Morphine
    Codein
    Pethidine
    Etorphine
    Fentanyl

    +++
    +
    ++
    +++
    +++

    +
    +
    +
    +++
    +

    ++
    +
    +
    +++
    -

    Partial Agonist :
    Pentazocine
    Nalorphine
    Buprenorphine

    (+)
    (++)
    +++

    +
    ++
    -

    ++
    ++
    (++)

    +
    +
    -

    Antagonist:
    Naloxone
    Naltrexone

    (+++)
    (+++)

    (++)
    (++)

    (++)
    (++)

    Opioids Adverse Reactions:


    Major side effects are:
    constipation + respiratory depression.

    Sedation, GIT motility, nausea and vomiting.


    Histamine release.
    Tolerance also physical and psychological dependence.
    Withdrawal: flu-like syndrome, yawn, runny nose,
    hypertension, diarrhea, muscle spasm, fever and anxiety.
    (Heroin:3-7 days, Methadone: 10-21 days).
    OD Treatment:
    Naloxone (Narcan) IV and Naltrexone (long acting).
    Contraindication: respiratory depression, chronic lung
    disease, liver or kidney disease, prostatic hypertrophy.

    Other Opioids:
    Diamorphine:
    Heroin, Diacetylmorphine
    vinegar smell & v lipophilic (BBB)

    Codein:
    3-methylmorphine+ antitussive (analgesic)
    only 20% analgesia (NO euphoria)
    Pethidine (DEMEROL):
    NO sedation and antitussive effects.
    antimuscarinic & analgesia (giving birth)
    Fentanyl (China White) and Sufentanyl:
    Short acting anaesthesia + ABUSE
    (OD: rapid respiratory paralysis)
    Etorphine:
    Potency 1000X and tranquilizer

    Pentazocine:

    partial agonist: agonist / antagonist


    arteriole BP
    dependence + acute toxicity
    very dysphoric + hallucination, nightmares
    Buprenorphine:
    structurally similar to Etorphine
    BUT pharmacological responses are similar to Pentazocine.
    Naloxone:
    a pure opiate antagonist and prevents or reverses the
    effects of opioids including respiratory depression, sedation
    and hypotension.

    Methadone:

    effects similar to morphine, long acting


    (t 1/2 = 15 -20 h) ie. highly bound + slowly
    excreted.

    sedative effects and physical


    abstinence syndrome
    heroin addiction alternative treatment +
    morphine (oral)

    (+ morphine / heroin injections, at low


    doses, NO euphoria)
    Mitragyna Speciosa, Ketom, Biak-biak:

    Alternative treatment for heroin / opium


    (replacement)?.
    No naloxone activity

    HAVE A BREAK!

    CNS
    DEPRESSANTS :
    ANTIPSYCHOTIC
    DRUGS

    Fertility goddess of harvest and corn, sister of


    Zeus, Demeter in agricultural societies.

    Antipsychotic drugs are also known as neuroleptic


    drugs, antiSchizhoprenia or major tranquilizers.
    Schizo(split) /phrenia (mind) :
    1% world population.
    Positive Symptoms (+): ACUTE
    delusion, thought disturbances,
    speech abnormalities, inner voices
    and hallucination.
    Negative Symptoms (-): CHRONIC
    self-isolation (paranoid), less
    emotional response and slow
    mental and physical reaction (eg.
    dementia).
    Causes : combination genetic, environment
    (anxiety + stress) + neurobiology (excess dopamine)

    Dopamine Receptor Subtypes:


    D1
    Function

    D1

    D2

    D5 D2 D3 D4

    Distribution:
    Cortex

    Arousal, mood

    +++

    ++

    Limbic System

    Emotion,
    stereotype
    behaviour

    +++

    ++

    Striatum

    Motor Control

    +++

    ++

    Ventral
    Hypothalamus +
    Anterior pituitary

    Prolactin
    modulation

    ++

    AntiSchizophrenia Drugs:
    Classification of Antipsychotic Drugs:
    Typical
    Conventional (non-selective)
    Block both dopamine and serotonin receptors
    Cause several adverse effects eg. hypotension,
    anticholinergic effects, extrapyramidal side effects
    (EPS) eg. Chlorpozamine, Haloperidol
    Atypical
    Selective dopamine receptors
    Primarily dopamine receptor blockers
    May alleviate some of unpleasant effects
    eg. Sulpiride, Clozapine

    MOA of Neuroleptic Drugs:


    More antagonisme at the dopamine receptor D2.
    Also antagonisme at other monoamine receptors eg.
    NAd, histamine, ACh and 5-HT.
    neuroleptic side effects are from the actions on
    other receptors than dopamine.
    Onset time is long (days to weeks) and probable increase
    of dopamine receptors may occur.

    MOA of Neuroleptic Drugs:

    Pharmacological Responses and Side Effects:


    Antiemesis:
    (+ cancer treatment, renal failure and pregnant mothers).
    Endocrine effects:
    serum prolactin concentration (gynaecomastia).
    growth hormone secretion.
    Others:
    Effects from monoamine receptors inhibition:
    M U S C A R I N E
    Cardiovascular effects:
    Vasodilatation, hypotension.
    Idiosyncratic Effects and Hypersensitivity:
    Jaundice (Chlorpromazine).
    Leukopenia + agranulocytosis.
    Skin reaction eg. Urticaria.

    Extrapyramidal Syndrome (EPS):


    PseudoParkinsonism (reversible and acute):
    Tremor, dystonia, and muscle spasm
    Direct inhibition at nigrostriatal receptors.
    Tardive dyskinesia:
    Involuntarily movement inhibition
    Rabbit Syndrome
    proliferation of dopamine receptors
    at corpus striatum.

    Tardive dyskinesia incidence is less occurring with


    atypical drugs (Clozapine, Sulpiride).

    A BEAUTIFUL MIND
    SCHIZOPHRENIA IS FOR LIFE
    There is no remission

    SUMMARY: EFFECTS OF OPIOIDS


    B A D

    A M E R I C A N S :
    B-Bradycardia and hypotension
    A-Antitussive effect
    D-Deep tendon reflexes are Depressed.

    A-Analgesic effect
    M-Miosis
    E-Euphoria
    R-Respiratory depression
    I-Intracranial pressure is increased.
    C-Constipation
    A-Acute intoxication, Anaphylaxis - respiratory Acidosis,
    N-Nausea and vomiting
    S-Sedation

    Drugs

    Receptor Affinity

    Side Effects

    D1

    D2

    H1

    mACh

    5HT

    EPS

    Se

    HiT

    Chlorpromazine

    ++

    +++

    ++

    ++

    ++

    ++

    ++

    ++

    Haloperidol

    +++

    ++

    +/-

    +++

    ++

    Typical:

    Lain2

    Prolactin,
    hypothermia,
    anticholinergic,
    hypersensitivity +
    JAUNDICE.
    SAME (NO jaundice
    + anticholinergic).

    Flupenthixol

    ++

    +++

    ++

    +++

    ++

    Atypical:
    Sulpiride

    Prolactin, anxiety.

    Prolactin.
    -

    +++

    Clozapine

    ++

    ++

    ++

    ++

    +++

    ++

    Quetiapine

    +++

    ++

    ++

    Notes

    Risk of
    agranulocytosis (1%).
    Epilepsy. Sedation.
    Saliva.
    Anticholinergicity
    effects.
    Body weight.
    Tachyicardia.
    Agitation. Dry mouth.
    Body weight.

    Phenothiazine group (same with


    Fluphenazine but no jaundice,
    hypotension, EPS.

    Butyrophenone group. Usual


    Neuroleptic. EPS.

    Same with Clopenthixol. Depot


    preparation.
    Benzamide group (same with
    Pimozide). Selective towards
    D2/3. absorption. EPS.
    Dibenzodiazepine group (same
    with Olanzepine but no risk of
    agranulocytosis). Also at D4. NO
    EPS. Effective for symptoms +/Schizophrenia. Suitable for
    resistant patients to treatment.
    Novel type. At alphaadrenoreceptor. Still under study.

    THANK YOU

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