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Opiods

This document discusses opioids and their use in pain management. It begins by defining pain and describing how its treatment depends on whether it is nociceptive or neuropathic. For mild to moderate pain, nonopioid analgesics are often used, while neuropathic pain responds better to other drug classes but may require opioids. Opioids are natural, semisynthetic, or synthetic compounds that produce morphine-like effects through binding to mu, kappa, and delta opioid receptors in the central nervous system. Their primary use is to relieve intense pain, though widespread availability has led to abuse issues. The document describes the different opioid receptor types and mechanisms of action, as well as examples of opioid agonists like morphine and codeine.

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82 views17 pages

Opiods

This document discusses opioids and their use in pain management. It begins by defining pain and describing how its treatment depends on whether it is nociceptive or neuropathic. For mild to moderate pain, nonopioid analgesics are often used, while neuropathic pain responds better to other drug classes but may require opioids. Opioids are natural, semisynthetic, or synthetic compounds that produce morphine-like effects through binding to mu, kappa, and delta opioid receptors in the central nervous system. Their primary use is to relieve intense pain, though widespread availability has led to abuse issues. The document describes the different opioid receptor types and mechanisms of action, as well as examples of opioid agonists like morphine and codeine.

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janemwanza003
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© © All Rights Reserved
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OPIODS

Mrs Mutoya
INTRODUCTION
 Management of pain is one of clinical medicine’s
greatest challenges.
 Pain is defined as an unpleasant sensation that can
be either acute or chronic and is a consequence of
complex neurochemical processes in the peripheral
and central nervous systems (CNS).
 Alleviation of pain depends on the specific type of
pain, nociceptive or neuropathic pain.
 For example, with mild to moderate arthritic pain
(nociceptive pain), nonopioid analgesics such as
nonsteroidal anti-inflammatory agents are often
effective.
INTRODUCTION
 Neuropathic pain can be treated with
opioids (some situations require higher
doses) but responds best to
anticonvulsants, tricyclic antidepressants,
or serotonin/ norepinephrine reuptake
inhibitors.
 However, for severe or chronic malignant or
non-malignant pain, opioids are considered
part of the treatment plan in select
patients.
OPIODS
 Opioids are natural, semisynthetic, or synthetic
compounds that produce morphine-like effects .
 These agents are divided into chemical classes
based on their chemical structure .
 Clinically this is helpful in identifying opioids that
have a greater chance of cross-sensitivity in a
patient with an allergy to a particular opioid.
 Allopioids act by binding to specific opioid
receptors in the CNS to produce effects that
mimic the action of endogenous peptide
neurotransmitters (for example, endorphins,
enkephalins, and dynorphins).
OPIODS
 Although the opioids have a broad range of
effects, their primary use is to relieve
intense pain, whether that pain results
from surgery, injury, or chronic disease.
 Unfortunately, widespread availability of
opioids has led to abuse of those agents
with euphoric properties.
 Antagonists that reverse the actions of
opioids are also clinically important for use
in cases of overdose
OPIOID RECEPTORS
 The major effects of the opioids are mediated by three receptor
families, which are commonly designated as μ (mu), κ (kappa),
and δ (delta).
 Each receptor family exhibits a different specificity for the
drug(s) it binds.
 The analgesic properties of the opioids are primarily mediated
by the μ receptors that modulate responses to thermal,
mechanical, and chemical nociception.
 The κ receptors in the dorsal horn also contribute to analgesia
by modulating the response to chemical and thermal
nociception
 The enkephalins interact more selectively with δ receptors in
the periphery.
MECHANISM OF ACTION
 All three opioid receptors are members of
the G protein–coupled receptor family and
inhibit adenylyl cyclase.
 They are also associated with ion
channels, increasing postsynaptic K+
efflux (hyperpolarization) or reducing
presynaptic Ca2+ influx, thus impeding
neuronal firing and transmitter release.
OPIOD AGONISTS
 Morphine is the major analgesic drug contained in crude
opium and is the prototype strong μ receptor agonist.
 Codeine is present in crude opium in lower concentrations
and is inherently less potent, making codeine the prototype
of the weak opioid agonists.
 The currently available opioids have various differences
in receptor affinity, pharmacokinetic profiles, available
routes of administration, and adverse effect profiles.
 Comparing other available opioids to morphine is helpful in
identifying the unique differences to guide the selection
of a safe and effective pain management regimen
ANY QUESTIONS?

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