4. Natural Mechanism Of Body Against Pain:
Our body always want to be in balance so endorphins are
released in controlled amounts and only under circumstances.
Our body naturally make opiates called endorphins. When we
exercise our body makes endogenous endorphins that reduces
pain. Endorphins do this by binding to opioid receptors on cell of
our nervous system or neurons or spinal cord. When these
receptors are activated by endorphins, they change how our
neurons communicate. Opiate receptors control pain relief,
happiness and feelings of pleasure as well as breathing.
5. Classification Of Opioid Receptors:
Receptors Location Function
➢µ-opioid
receptor
In brain(cortex,
thalamus) and
spinal cord and
intestine.
analgesia,
respiratory
depression, miosis,
euphoria
➢Delta-opioid
receptor
In brain (amygdala
and olfactory
bulbs)
Analgesia,
antidepressant,
anticonvulsant
➢Kappa-opioid
receptor
In brain
(hypothalamus)
and spinal cord
Analgesia, diuresis,
sedation, stress,
neuroprotection
11. Morphine:
Mechanism Of Action:
Opioid effects by activating opiate receptors that
are widely distributed through out the brain and
body. Morphine majorly acts on mu-opioid
receptors. Its main effect is binding to
and activating the mu-opioid receptors it slows
down the pain signal and that’s how it produce its
analgesic effect.
15. Side effects:
•Dizziness
A sensation of spinning around and losing one's balance.
•Respiratory depression
Hypoventilation (also known as respiratory depression) occurs
when ventilation is inadequate (hypo meaning "below") to perform
needed gas exchange. it causes an increased concentration of
carbon dioxide (hypercapnia) and respiratory acidosis.
•Dysphonia
Difficulty in speaking due to a physical disorder of the mouth,
tongue, throat, or vocal cords.
16. Interactions:
Primary Drug Secondary Drug Effects
Morphine Furosemide
May have additive effects
in lowering B.P
Morphine Diazepam
It can cause CNS
depression and side
effects will be more
worsen.
23. Indications Of Oxycodone:
ATC stands for "around-the-clock." Around-the-clock (ATC)
medication is defined as medication that is given at regularly
scheduled intervals throughout the day. This can include a dose
during the night. Around-the-clock dosing is common for opioid
medication to manage pain.
Around the clock pain:
26. Side effects:
•Xerostomia
It is the subjective sensation of dry mouth, which is often (but not
always) associated with hypo function of the salivary glands.
•Hypotension
Hypotension is low blood pressure, especially in the arteries of
the systemic circulation.
27. Interactions:
Primary Drug Secondary Drug Effects
Oxycodone Voriconazole
Voriconazole increases
plasma concentration of
Oxycodone and increase
its pharmacodynamics
effects.
Oxycodone Quinidine
pharmacodynamics
effects of Oxycodone will
be changed.
33. Doses Of Fentanyl:
For adults: Transmucosal dosage: 200mcg
lozenges for cancer or severe
pain.
S/L: 100mcg
0.7-1.4 µg/kg, IM, for
anesthesia
For children's: 1.7-3.3µg/kg IM
36. Interactions:
Primary Drug Secondary Drug Effects
Fentanyl Alcohol
May increase the risk of
respiratory depression.
Fentanyl Benzodiazepines
Increases sedative effects
and diminished breathing
Fentanyl Butabarbital Synergistic effects
41. Codeine:
Mechanism Of Action:
Pain mechanism: same as morphine.
Cough mechanism: codeine acts on cough reflexes which are present in
Brain stem, after binding with cough reflexes it act as cough suppressant.
45. Interactions:
Primary Drug Secondary Drug Effects
Codeine Alprazolam
Brain Impairement and
confusion
Codeine Pentazocine
Reduce the effects of
codeine
Codeine Phenalzine
Increases action of
codeine
53. Interactions:
Primary Drug Secondary Drug Effects
Hydrocodone Cetirizine
Increases side effects of
Hydrocodone.
Hydrocodone Gabapentin
Hydrocodone
bioavailability will be
reduce.
Hydrocodone Benadryl
Worsen the side effects of
Hydrocodone.
55. Naloxone
:
Introduction:
When a person is overdosing they have too much opiates in their
System. Their breathing slows down and they experience brain
damage because of loss of oxygen and quickly die.
59. Naloxone
:
Mechanism Of Action:
Naloxone binds to an opiate receptor and act as a
competitive inhibitor to opioid. This means it competes the
same receptors site as opiates, pushing them out of the
way, in this way it reverses the effects of an opiates
overdose, it blocks the receptor functioning that’s why it is
called an inhibitor.
63. Side effects:
•Hallucination
A sensory experience of something that does not exist outside
the mind, caused by various physical and mental disorders, or
by reaction to certain toxic substances, and usually manifested
as visual or auditory images.
64. Interactions:
Primary Drug Secondary Drug Effects
Naloxone Droperidol
Increase a risk of irregular
heart beat.
Naloxone alcohol
Side effects of Naloxone
will be worsen.
68. Tramadol
:
Mechanism Of Action:
Tramadol is known to act on the mu-opioid receptors to produce pain
relief. Opioid receptors are located in the brain and there are three types
of which the mu-opioid receptor is one. Normally a painful stimulation
occurs a neurons communicate to brain and the persons feel pain. When
the person takes Tramadol, it acts on mu-opioid receptor blocking the
neuron from communicating pain to the brain.
72. Interactions:
Primary Drug Secondary Drug Effects
Tramadol Carbamazepine
Efficacy of tramadol
decreases.
Tramadol Warfarin Increased risk of bleeding
Tramadol Amitriptyline Increased risk of seizures.
74. Warnings And Precautions Of Opioid:
✓It should be used caution in renal and liver disease patients.
✓Avoid taking alcohol.
✓Do not drive a car or operate any machinery.
✓Withdrawal symptoms.
✓Do not take if you have breathing problems
✓Do not take in high doses because it cause euphoria and
tolerance.
76. Benzodiazepines:
Antidote:
Flumazenil (Romazicon)
Dose Of Flumazenil:
0.1mg/min infusion
Mechanism Of Action Of Antidote:
Reverses the effects of benzodiazepines by competitive
inhibition at the benzodiazepine binding site on the
GABAA receptor.
77. ▪ Usual symptoms of overdose include:
▪ Hypothermia
▪ Respiratory depression
▪ Blurred vision or nystagmus
▪ Stupor like effects/seizure
▪ Coma
Over Dose Symptoms:
78. ▪ Hypothermia:
It is a medical emergency that occurs when your body loses heat faster
that it can produce heat.
▪ Nystagmus:
It is a condition of involuntary eye movement.
▪ Stupor like effects:
A state of near unconsciousness or insensibility.
82. For Hypothermia:
▪ Warm the body physically
For Hypotension:
▪ Use I/V fluids i.e. normal saline
▪ Focus on patient rewarming
83. Beta Blockers:
Antidote Of Beta Blocker:
Glucagon
Dose:
50mg/kg I/V
Mechanism Of Action Of Antidote:
•Glucagon works by increasing positive inotropic and chronotropic
effects.
•It also increases gluconeogenesis.
84. Symptoms of overdose:
▪ Irregular heartbeat
▪ Shock
▪ Shortness of breath
▪ Blurred vision
▪ Coma
85. Management Includes:
▪ Cardiac monitoring
▪ Assist ventilation
▪ Activated charcoal
▪ For hypotensive patient, give 20ml/kg of isotonic I/V fluids
▪ Give antidote
91. Management Includes:
Activated charcoal:
(Check plasma level of blood after every 2-4 hours)
For dehydration:
Fluids are given (NaCl 0.9%)
For metabolic acidosis:
Give I/V sodium bicarbonate
92. Digoxin:
Antidote Of Digoxin:
Fab fragment digibind
Dose Of Antidote:
40mg is required for every 0.6mg digoxin
Mechanism Of Action:
▪ Binds to digoxin in the extracellular spaces preventing digoxin binding to the
Na+/k+ ATPase.
▪ Digoxin is renally eliminated along with digibind.
93. Symptoms of overdose:
▪ Nausea and vomiting
▪ Hyperkalemia
▪ Decreased consciousness
▪ Respiratory arrest
▪ Tachycardia