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ANALGESICS


By: Sathish Rajamani
INTRODUCTION
Analgesics are medications used to
relieve pain without reducing the
consciousness of the patient.
They work by reducing the amount of
pain felt and this is generally achieved
by interfering with the way the pain
message is transmitted by the nerves.
Analgesics will not treat the cause of
the pain but they will provide temporary
relief from pain symptoms.
TYPES OF ANALGESICS
OPIOID ANALGESICS
The opioid analgesics which are
prescription only medicines that are very
potent, being chemically related to
morphine.
Opioid analgesics are prescribed for
moderate to severe pain, particularly of
visceral origin, and are used in step two
and step three of the analgesic ladder.
Dependence and tolerance are well
known features with regular use
although this should not inhibit
prescribing in palliative care.
Some chronic non-malignant
conditions benefit from analgesic
control with opioids, but patients
should be reviewed regularly.
OPIUM, the greek name for poppy juice. Is
obtained from the juice of the papaver
somniferum.
ACTIONS OF OPIOID
        ANALGESICS
Opioid analgesics interacts with four
major receptors in the CNS
Mu receptors
Kappa receptors
Sigma receptors and
Delta receptors
RECEPTORS         EFFECTS

MU               Analgesia, Respiratory
                 depression and euphoria




KAPPA            Respiratory depression,
                 sedation

SEGMA            Hallucination, Dysphoria,
                 Seizures

DELTA            Analgesia
CLASSIFICATION OF OPIOID
        ANALGESICS
Natural Alkaloids
 Morphine
 Codeine
Semi Synthetic Compounds
 Pethidine
 Methadone
 Tramadol
MORPHINE
Morphine is the most important alkaloid
of of opium.
Morphine produces analgesia through
actions in the brain and spinal cord.
Morphine is readily absorbed from the
GI tract and subcutaneous and muscle
tissue.
Morphine is administered
intravenously, epidurally, and
intrathecally.
PHARMACOTHERAPEUTICS
Morphine sulfate is primarily used to
relieve moderate to severe pain.
It is used pre operatively, its effect is
on reducing patients anxiety and in
assisting in induction of anesthesia.
It is the drug of choice for clients with
pain from MI, Pulmonary edema and
dyspnea from acute left ventricular
failure.
PHARMACOKINETICS
    Absorption
•      It depends on the route of administration,
•      Morphine ingested orally is generally
    absorbed in one and half to two hours.
•      It reaches liver for metabolism before
    reaching systemic circulation.
•      Absorption after IM or SC injection
    occurs in 30 to 60 minutes.
PHARMACOKINETICS
    Distribution
•       It occurs quickly.,
•       After administration morphine leaves the
    blood and directly enters the kidney, lungs,
    liver and spleen.
•       Its action on skeletal muscle is limited,
    since the drug is not very lipid soluble, it
    does not cross the BBB easily
•       .
DURATION OF ACTION
METHOD OF ADMINISTRATION   ONSET OF ACTION




          Oral               4 to 12 hours




        IM or SC           10 to 30 minutes




           IV              15 to 30 minutes
PHARMACOKINETICS
    BIOTRANSFORMATION
•   It occurs in the liver.
•   Excretion occurs in the kidney.
•   Only traces of morphine is
  founded in body after 48 hours.
  .
PHARMACODYNAMICS
Morphine produces analgesia by
binding preferentially to the mu
and delta receptors.
Morphine targets the areas
involved with regulation of pain
perception, respiration and
affective behaviors.
THERAPEUTIC USES
Analgesia
Suppression of cough and dyspnea.
Sedation
In the treatment of diarrhea
As preanesthetic medication
In the treatment of the left ventricular
failure.
CONTRAINDICATIONS
Head Injury, because morphine can cause
increased intracranial tension, which can
leads to marked respirator depression.
Myxedema
Bronchial asthma – Morphine releases
histamine which can trigger
bronchoconstriction.
Elderly patients
In hypotensive states.
ADVERSE REACTIONS
 CNS Side effects
Confusion, anxiety, lethargy, nausea and
 vomiting.
 GIT Side effects
Constipation
 Other Side effects
Urinary retention, dry mouth, dysphoria,
 hypotension, skin rash, itching and
 urticaria.
MORPHINE POISONING
 Acute poisoning with morphine and other
 opioids occurs with overdoses.
 Signs and Symptoms
 Coma, Pinpoint pupils, and respiratory
 depression which frequently called triad.
                TREATMENT
Administration of antagonist Naloxone.
Support of Respiratory and Cardio Vascular
 function.
Opioid Analgesics

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Opioid Analgesics

  • 2. INTRODUCTION Analgesics are medications used to relieve pain without reducing the consciousness of the patient. They work by reducing the amount of pain felt and this is generally achieved by interfering with the way the pain message is transmitted by the nerves. Analgesics will not treat the cause of the pain but they will provide temporary relief from pain symptoms.
  • 4. OPIOID ANALGESICS The opioid analgesics which are prescription only medicines that are very potent, being chemically related to morphine. Opioid analgesics are prescribed for moderate to severe pain, particularly of visceral origin, and are used in step two and step three of the analgesic ladder.
  • 5. Dependence and tolerance are well known features with regular use although this should not inhibit prescribing in palliative care. Some chronic non-malignant conditions benefit from analgesic control with opioids, but patients should be reviewed regularly.
  • 6. OPIUM, the greek name for poppy juice. Is obtained from the juice of the papaver somniferum.
  • 7. ACTIONS OF OPIOID ANALGESICS Opioid analgesics interacts with four major receptors in the CNS Mu receptors Kappa receptors Sigma receptors and Delta receptors
  • 8. RECEPTORS EFFECTS MU Analgesia, Respiratory depression and euphoria KAPPA Respiratory depression, sedation SEGMA Hallucination, Dysphoria, Seizures DELTA Analgesia
  • 9. CLASSIFICATION OF OPIOID ANALGESICS Natural Alkaloids  Morphine  Codeine Semi Synthetic Compounds  Pethidine  Methadone  Tramadol
  • 10. MORPHINE Morphine is the most important alkaloid of of opium. Morphine produces analgesia through actions in the brain and spinal cord. Morphine is readily absorbed from the GI tract and subcutaneous and muscle tissue. Morphine is administered intravenously, epidurally, and intrathecally.
  • 11. PHARMACOTHERAPEUTICS Morphine sulfate is primarily used to relieve moderate to severe pain. It is used pre operatively, its effect is on reducing patients anxiety and in assisting in induction of anesthesia. It is the drug of choice for clients with pain from MI, Pulmonary edema and dyspnea from acute left ventricular failure.
  • 12. PHARMACOKINETICS Absorption • It depends on the route of administration, • Morphine ingested orally is generally absorbed in one and half to two hours. • It reaches liver for metabolism before reaching systemic circulation. • Absorption after IM or SC injection occurs in 30 to 60 minutes.
  • 13. PHARMACOKINETICS Distribution • It occurs quickly., • After administration morphine leaves the blood and directly enters the kidney, lungs, liver and spleen. • Its action on skeletal muscle is limited, since the drug is not very lipid soluble, it does not cross the BBB easily • .
  • 14. DURATION OF ACTION METHOD OF ADMINISTRATION ONSET OF ACTION Oral 4 to 12 hours IM or SC 10 to 30 minutes IV 15 to 30 minutes
  • 15. PHARMACOKINETICS BIOTRANSFORMATION • It occurs in the liver. • Excretion occurs in the kidney. • Only traces of morphine is founded in body after 48 hours. .
  • 16. PHARMACODYNAMICS Morphine produces analgesia by binding preferentially to the mu and delta receptors. Morphine targets the areas involved with regulation of pain perception, respiration and affective behaviors.
  • 17. THERAPEUTIC USES Analgesia Suppression of cough and dyspnea. Sedation In the treatment of diarrhea As preanesthetic medication In the treatment of the left ventricular failure.
  • 18. CONTRAINDICATIONS Head Injury, because morphine can cause increased intracranial tension, which can leads to marked respirator depression. Myxedema Bronchial asthma – Morphine releases histamine which can trigger bronchoconstriction. Elderly patients In hypotensive states.
  • 19. ADVERSE REACTIONS CNS Side effects Confusion, anxiety, lethargy, nausea and vomiting. GIT Side effects Constipation Other Side effects Urinary retention, dry mouth, dysphoria, hypotension, skin rash, itching and urticaria.
  • 20. MORPHINE POISONING Acute poisoning with morphine and other opioids occurs with overdoses. Signs and Symptoms Coma, Pinpoint pupils, and respiratory depression which frequently called triad. TREATMENT Administration of antagonist Naloxone. Support of Respiratory and Cardio Vascular function.