DR.

RAFIA TABASSUM
ASSISTANT PROFESSOR
DEPT: ANAESTHESIOLOGY, SICU & PAIN
MANAGEMENT,
PUMHSW SBA
 INTRODUCTION
 PHARMACOKINETICS & DYNAMICS
 MODE OF ACTION
 CLASSIFICATION
 INDICATIONS
 DOSAGE
 CONTRAINDICATIONS
 ADVERSE EFFECTS
 OVERDOSAGE
 Opium, the source of morphine, is obtained
from the poppy, Papaver somniferum and P
album .
 After incision, the poppy seed pod exudes a
white substance that turns into a brown gum
that is crude opium.
 Opium contains many alkaloids, the principal one
being morphine, which is present in a
concentration of about 10%. Codeine is
synthesized commercially from morphine.
 Most opioid analgesics are well absorbed when given by
subcutaneous, intramuscular, and oral routes.
 Opioids bind to plasma proteins and rapidly leave the
blood compartment and distributed in tissues that are
highly perfused such as the brain, lungs, liver, kidneys,
and spleen.
 Phase I --- Oxidation & Hydrolysis
 Phase II---The opioids are converted in large part to
polar metabolites (mostly glucuronides), which are then
readily excreted by the kidneys.
 Approximately 10% of morphine is metabolized to
morphine- 6-glucuronide (M6G), an active metabolite
with analgesic potency four to six times that of its
parent compound.
 Opioid agonists produce analgesia by
binding to specific G protein- coupled
receptors that are located in brain and
spinal cord regions involved in the
transmission and modulation of pain.
 Analgesia
 Acute Pulmonary Edema
 Cough
 Diarrhea
 Shivering
 Applications in Anesthesia
---sedative, anxiolytic, and analgesic
 Intravenous
 Intramuscular
 Epidural or subarachnoid
 Rectal suppositories
 Transdermal application
 Intranasal
 Buccal transmucosal
 Patient-controlled analgesia (PCA)
 Intravenous injection of Naloxone
--The usual initial dose 0.1–0.4 mg intravenously
for life-threatening respiratory and CNS
depression. In using naloxone in the severely
opioid-depressed newborn, start with doses of
5–10 mcg/kg and a second dose of up to a total
of 25 mcg/kg if no response is noted.
 Respiratory support