This document provides an overview of analgesics, including both opioid and non-opioid analgesics. It discusses various opioid analgesics like morphine, codeine, fentanyl and pentazocin. It describes their mechanisms of action, indications, routes of administration, side effects and contraindications. It also discusses non-opioid analgesics like paracetamol, acetylsalicylic acid and analgin, and describes their mechanisms of action as inhibitors of prostaglandin synthesis. The document classifies different types of pain and summarizes the history and development of commonly used opioid analgesics.
this is an important topic in palliative care. a form of care each of us may need when we suffer terminal illness and severe trauma at one point in our life time.
this is an important topic in palliative care. a form of care each of us may need when we suffer terminal illness and severe trauma at one point in our life time.
a detailed description of pain and therpaeutic options available and clinical assessment of pain, approach to the patient with pain, assessment of intensity of pain, nsaids and opioids, tca. WHO pain ladder, chronic opioid therapy
a detailed description of pain and therpaeutic options available and clinical assessment of pain, approach to the patient with pain, assessment of intensity of pain, nsaids and opioids, tca. WHO pain ladder, chronic opioid therapy
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2. PAIN
What is pain?
• A protective mechanism to warn of damage or the
presence of disease
• Part of the normal healing process
3. ANALGESICS
I. Opioid (narcotic) analgesics
1. Agonists of opioid receptors – morphine hydrochloride,
promedol, omnopon, fentanyl, codeine;
2. Agonists – antagonists and partial agonists of opioid receptors
– pentazocin, buprenorphine.
II. Non-opioid analgesics and non steroidal anti-
inflammatory drugs - NSAIDs
Acetylsalicylic acid, paracetamol, analgin, indometacin,
butadion, ibuprofen, pyroxicam, diclofenac-sodium, ketorolac,
ketoprofen.
III. Substances with mixed mechanism of action
(Opioid and non-opioid components)- Tramadole
4. The structures that take part in perception of pain:
thalamus, hypothalamus, reticular formation, limbic
system, occipital and frontal areas of cortex
System which conducts and perceives pain
NOCICEPTIVE
5. Classification of Pain
By Onset and Duration
Acute pain
Sudden in onset
Usually subsides once treated
Chronic pain
Persistent or recurring
Often difficult to treat
6. Major Sources of Pain
Source Area Involved Characteristics Treatment
Somatic body
framework
throbbing,
stabbing
narcotics,
NSAIDS
Visceral kidneys,
intestines,
liver
aching,
throbbing,
sharp, crampy
narcotics,
NSAIDS
Neuropathic Nerves burning,
numbing,
tingling
narcotics,
NSAIDS,
antidepressants,
anticonvulsants
7. History of Opioids
•Opium is extracted from poppy seeds (Papaver
somniforum)
•Used for thousands of years to produce:
•Euphoria
•Analgesia
•Sedation
•Relief from diarrhea
•Cough suppression
8. History cont’d
•Used medicinally and recreationally from
early Greek and Roman times
•Opium and laudanum (opium combined
with alcohol) were used to treat almost all
known diseases
9. Friedrich Wilhelm Adam
Sertürner, a German
pharmacist, isolated
Morphine from opium,
in 1805.
Morpheus
is the Greek god of
dreams and sleep.
10. History and Background
•Invention of the hypodermic needle in 1856 produced
drug abusers who self administered opioids by
injection
•Controlling the widespread use of opioids has been
unsuccessful because of the euphoria, tolerance and
physiological dependence that opioids produce
11. OPIOID RECEPTORS
• group of G-protein coupled receptors with opioids as
ligands.
•The endogenous opioids are dynorphins, enkephalins,
endorphins, endomorphins and nociceptin.
Subtypes of opireceptors:
mu, delta, kappa, epsilon, sigma
12. Morphine CNS
Depressant effects
• Analgesia
• Indifference to surroundings
• Mood and subjective effects
• Depression of respiration
• Cough centre
• Temperature regulating centre
• Vasomotor centre
Stimulate effects
• CTZ (nausea, vimiting)
• Edinger Wesphal nucleus
(III nerve –producing miosis)
• Vagal centre (bradycardia)
• Certain cortical areas and
hippocampal
13. Morphine can be used as an analgesic to relieve:
pain in myocardial infarction
pain associated with surgical conditions, pre- and
postoperatively (pre-anesthetic medication, balanced
anesthesia, surgical analgesia)
pain associated with trauma, burns
severe chronic pain, e.g., cancer
pain from kidney stones, renal colic, ureterolithiasis, etc
(pain may be valuable for diagnosis: should not be relived by analgesic unless proper
assessment of the patient has been done)
traumas of thorax accompanied by cough (morphine depresses central links of
coughing reflexes)
14. Acute left-ventricular cardiac failure
(cardiac asthma)
Reduce preload on heard due to vasodilatation
Tending to shift blood from pulmonary to systemic circuit;
relieves pulmonary congestion and edema
Allays air hunger by depressing respiratory centre
Cuts down sympathetic stimulation by calming the patient
15. Applications in Dentistry
•Narcotic (opioid) analgesics are extremely
effective in reducing acute dental and
postoperative pain.
•The narcotic analgesics have established a niche
for the treatment of pain in those situations
where the NSAIDs are less effective.
• Hydrocodone, oxycodone, codeine, and
occasionally meperidine are the narcotics used
to treat dental pain.
16. MORPHINE HYDROCHLORIDE
ROUTES OF ADMINISTRATION
subcutaneously and intramuscularly
(analgesic action after 10-15 min)
oral administration – presystemic elimination
( 20-60 % enters general blood circulation)
sublingually – quick absorption
i.v. is indicated even in emergency
Epidural or intrathecal ( into the spinal canal ) injection produces
segmental analgesia lasting 12 hours without affecting other
sensory, motor or autonomic modalities
Duration of analgesic action – 4-6 hours
Maximum single dose of morphine is 0,02 g,
maximum daily dose – 0,05 g
17. Side effects of morphine
Respiratory depression
Vomiting (excitation of starting zone of
vomiting center)
bradycardia (increasing of tone of n. vagus
nuclei)
spasm of sphincters of gastro-intestinal tract
accompanied by constipations
increasing of tone of smooth musculature of
urinary and bile-excreting tracts (retentions
of urination, bile stasis)
Decreasing of BP
18. CONTRAINDICATIONS FOR ADMINISTRATION
OF MORPHINE
acute respiratory depression
renal failure (due to accumulation of the metabolites
morphine-3-glucuronide and morphine-6-glucuronide)
chemical toxicity (potentially lethal in low tolerance
subjects)
raised intracranial pressure, including head injury (risk of
worsening respiratory depression)
Biliary colic
Precaution
pain that accompanies chronic inflammatory pain
children before the age of 2 years
19. Tolerance
•Tolerance is a diminished responsiveness to the drug’s
action that is seen with many compounds
•Tolerance can be demonstrated by a decreased effect
from a constant dose of drug or by an increase in the
minimum drug dose required to produce a given level
of effect
•Physiological tolerance involves changes in the
binding of a drug to receptors or changes in receptor
transductional processes related to the drug of action
•This type of tolerance occurs in opioids
22. Withdrawl Reactions
Acute Action
• Analgesia
• Respiratory Depression
• Euphoria
• Relaxation and sleep
• Tranquilization
• Decreased blood pressure
• Constipation
• Pupillary constriction
• Hypothermia
• Drying of secretions
• Reduced sex drive
• Flushed and warm skin
Withdrawl Sign
• Pain and irritability
• Hyperventilation
• Dysphoria and depression
• Restlessness and insomnia
• Fearfulness and hostility
• Increased blood pressure
• Diarrhea
• Pupillary dilation
• Hyperthermia
• Lacrimation, runny nose
• Spontaneous ejaculation
• Chilliness and “gooseflesh”
23. OMNOPON
•contains mixture if opium alkaloids
(48-50% morphine)
•does not cause spasms of smooth musculature,
as it contains alkaloids of isoquinoline raw
•is used for analgesia according to all the
indications of morphine hydrochloride, for
example, colics
24. Promedol (trimeperidine)
•produces similar effects to other opioids, such
as analgesia and sedation, along with side
effects such as nausea, itching, vomiting and
respiratory depression which may be harmful or
fatal.
•duration of analgesic action - 3-4 hours
•moderate spasmolytic influence on smooth
musculature of internal organs
•stimulation of rhythmic contractions of uterus
•can be used for analgesia
•in case of pain syndrome connected with
spasms of smooth musculature
25. Fentanyl
•synthetic opioid analgesic of short action
•analgesic activity is 300 times higher than of
morphine
•analgesic effect after intravenous introduction –
after 1-3 min, lasts for 15-30 min
•used with neuroleptic droperidol (complex drug –
“talamonal”) for neuroleptanalgesia
26. Fentanyl transdermal system
•should be used for long-
term (chronic) pain
requiring continuous
narcotic pain
•Is designed to release the
drug into the skin at a
constant rate ranging from
25 to 100 micrograms/h
27. Codeine
opium alkaloid
analgesic action is not strong, but anticough effect is
considerable
administered as an anticough drug of central action
combination with non opiod analgesics
(eg. Paracetamol) is supra-additive
28. Pentazocin
agonist-antagonist of opioid receptors
comparatively with morphine, it is a bit less
dangerous in the aspect of addiction
development
indicated in case of pain of medium intensity in
such conditions like other opioid analgesics. In
case of strong pain its administration is limited
as in case of increasing of dose of the drug
excitation appears
it can cause increasing of blood pressure and
tachycardia that’s why it’s not advised to use in
case of acute myocardium infarction
if it is administered for people with narcotic
addiction manifestations of abstinence develop
29. Buprenorphine
• Partly agonist of mu-opioid receptors
• Acts longer than morphine (approximately 6 hours)
• Analgesic activity is higher than of morphine, that’s why it’s
used in doses of 0,3-0,6 mg
• In case of breathing depression, which it causes, naloxon is less
effective since buprenorphine is slowly released from the
connection with mu-receptors
• Indicated for pain decreasing in the same situations as other
narcotic analgesics
• May be used for detoxication and supporting treatment of
individuals who is addicted to heroine
30. Acute poisoning with opioid analgesics
•Respiratory Depression
•Euphoria
•Relaxation and sleep
•Tranquilization
•Decreased blood pressure
•Constipation
•Pupillary constriction
•Hypothermia
•Drying of secretions
•Flushed and warm skin
31. Triad in case poisoning
with morphine
Acute miosis
(Pinpoint
pupils)
Cheyne Stokes
respiration
deep tendon
reflexes
increased
32. Treatment of acute poisoning
Naloxon (antagonist of opioid receptors)
intravenously - 0,4-1,2 mg
general dose of naloxon should not overcome 10 mg
stomach lavage (for morphine enterohepatic circulation is
typical) with 0,05-0,1% solution of potassium
permanganate and 0,5 % tannin solution
suspension of 20-30 g of activated charcoal
salt laxative agents (sodium sulfate)
forced diuresis
atropine sulfate
inhalation of carbogen (5-7 % СО2 and 93-95 % O2)
35. Mechanism of action of non-opioid
analgesics
•depression of cyclooxygenases activity
•decreasing of prostaglandins synthesis in
peripheral tissues and in central nervous
system
•decreasing of sensitivity of nervous endings
and depression of transmission of
nociceptive impulses on the level of CNS
structures
•pain-relieving action of non-opioid
analgesics is partly connected with their anti-
inflammatory activity
36.
37. Effects of COX Inhibition
by Most NSAIDS
COX-1
Gastric ulcers
Bleeding
Acute renal failure
COX-2
Reduce inflammation
Reduce pain
Reduce fever
NSAIDs : anti-platelet—decreases ability of blood to clot
39. Indications for administration of non-
narcotic analgesics
headache
toothache
backache
neuralgias
pulled muscles
joint pain
dysmenorrhea
for potentiating of their action – combinations
paracetamol with codeine,
metamizol with dimedrol, metamizol with codeine
40. Applications in Dentistry
• Toothache
• Post extraction pain
• Periodontitis
• Neuritis
• Stomatitis
• Arthritis
• Local usage as keratoplatic agents for hyperkeratosis, hyperesthesia
41. Paracetamol
(Acetaminophen)
• analgesic and antipyretic drug
• maximal effect if the drug is introduced orally – after 2 hours,
lasts approximately for 4 hours
• in case of durable administration of big doses – damaging of
liver and kidneys, production of met-hemoglobin
42. Paracetamol (Acetaminophen)
N-Acetyl-P-Aminophenol
Classification: analgesic, antipyretic, misc.
not an NSAID
Mechanism: inhibits prostaglandin synthesis
via CNS inhibition of COX (not peripheral)-
doesn’t promote ulcers, bleeding or renal failure;
peripherally blocks generation of pain impulses,
inhibits hypothalamic heat-regulation center
46. Paracetamol : Liver Metabolism
1. Major pathway —Majority of drug is metabolized
to produce a non-toxic metabolite
2. Minor pathway —Produces a highly reactive
intermediate (acetylimidoquinone) that conjugates
with glutathione and is inactivated.
•At toxic PARACETAMOL levels, minor pathway
metabolism cannot keep up (liver’s supply of
glutathione is limited), causing an increase in the
reactive intermediate which leads to hepatic toxicity
and necrosis
47. Acetylsalicylic acid
Blocks irreversibly COX
As antipyretic and analgesic
drug – 0,25 and 0,5 g per time
As an anti-inflammatory – 3-4 g
per day (for arthritis,
myocarditis, pleuritis, bronchitis
etc.
As platelets inhibitor - for
prophylaxis of thrombus-
formation (in case of ischemic
heart disease, thrombophlebitis
etc.) – daily dose – 80-100 mg
48. Pharmacokinetics: ASA
Absorption: from stomach and intestine
Distribution: readily, into most fluids/tissues
Metabolism : primarily hepatic
•ASA contraindicated for use in children with viral
fever –can lead to Reye’s Syndrome
•Fatal overdose is possible
Similar pharmacokinetics for ibuprofen and related NSAIDs
52. Ketorolak (ketanov)
•according to analgesic activity it
prevails over effect of acetylsalicylic
acid, indometacin and equals to
opioid analgesics
•moderate anti-inflammatory,
antipyretic and anti-aggregate effects
•high effectiveness in case of pain in
postoperative period, in oncology,
during child delivery, traumas, colic
•i/m, i/v, orally
NOT indicated
for chronic pain syndrome
53. Ketoprophen (ketonal)
• strong analgesic, anti-inflammatory and antipyretic agent
• administered in case of arthroses and arthritis, ancilizing
spondilitis, pain of different genesis (after surgeries, in case
of traumas, painful menstruations etc.)
• administered orally, intramuscularly, in forms of
suppositories and ointments
54. TRAMADOL
Analgesic activity is similar to the activity
of morphine
Abuse potential is low
Less respiratory depression
Hemodynamic effects are minimal
In case of intravenous administration effect
develops after 5-10 min, if administered
orally – after 30-40 min, action lasts for
3-5 hours.
Tramadol possesses agonist actions at the μ-opioid receptor
and affects reuptake at the noradrenergic and serotonergic systems
55. ADMINISTRATION OF TRAMADOL
1. Surgery, traumatology, gynecology,
neurology, urology, oncology
2. For all kinds of acute and chronic pain of
moderate and considerable intensity,
including neuralgias, postoperative,
traumatic pain
diagnostic and therapeutic interventions
oncologic pathology
A protective mechanism to warn of damage or the presence of disease
The structures that take part in perception of pain: thalamus, hypothalamus, reticular formation, limbic system, occipital and frontal areas of cortex
System which conducts and perceives pain - nociceptive
Major Sources of Pain
Opium (poppy tears, lachryma papaveris) is the dried latex obtained from opium poppies (Papaver somniferum). Opium contains up to 12% morphine, an opiate alkaloid, like codeine, papaverine noscarpine (benzoisochinolon derivatives)
An opium-based elixir has been ascribed to alchemists of Byzantine times,. Around 1522, Paracelsus made reference to an opium-based elixir which he called, laudanum from the Latin word laudare meaning "to praise."
Morpheus (pronounced /ˈmɔr.fjuːs/; Greek: "he who shapes [dreams]") is the Greek god of dreams and sleep. Morphine was isolated from opium in the early 1800’s and since then has been the most effective treatment for severe pain
Opioid receptors are a group of G-protein coupled receptors with opioids as ligands. The endogenous opioids are dynorphins, enkephalins, endorphins, endomorphins and nociceptin.
Trimeperidine is an opioid analgesic that is an analogue of prodine (meperidine). It was developed in or around 1954 in the USSR during research into the related drug pethidine.
a form of analgesia achieved by the concurrent administration of a neuroleptic such as droperidol and an analgesic such as fentanyl. Anxiety, motor activity, and sensitivity to painful stimuli are reduced; the person is quiet and indifferent to surroundings
Although NSAIDs are the established drugs of first choice for the management of mild-to-moderate dental and postoperative pain, at times the oral narcotic analgesics must be used to treat the more severe intensities of pain.
Reye's syndrome is a potentially fatal disease that causes numerous detrimental effects to many organs, especially the brain and liver, as well as causing hypoglycemia.[1] The exact cause is unknown, and while it has been associated with aspirin consumption by children with viral illness, it also occurs in the absence of aspirin use.
It remained freely available worldwide until the 1970s, when it was discovered that the drug carries a small risk of causing agranulocytosis - a potentially fatal condition. Controversy remains regarding the level of risk. Several national medical authorities have banned metamizole either totally or have restricted it to be available only on prescription, while others have maintained its availability over the counter.
