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Presentation Topic: Narcotics And
Antidote Management
Narcotics:
“Narcotics are addictive drugs that reduce
the user's perception of pain and induce
euphoria.”
Natural Mechanism Of Body Against Pain:
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.
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
How does opioid works?
Strong opioid agonist
• Morphine
• Oxycodone
• Fentanyl
Partial agonist
•Codeine
•Hydrocodone
Opioid antagonist
•Naloxone
Other analgesic •Tramadol
Classification Of Opioid:
Morphine:
Available Brands:
•MS Contin®
•Astramorph
®
Morphine:
Available Dosage Forms:
•Tablets
•Capsules
•Injectable
•Oral solution
•Suppositorie
s
Morphine:
Mechanism Of Action:
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.
Indications Of Morphine:
Acute pain
Post operative pain
Relief pain of MI
Chronic pain
Doses Of Morphine:
For adults: Oral:
Tab: 15-30mg every 4 hr
I/V: 2.5-5mg every 3-4 hr
For children's: S/C: 0.1-0.2mg/kg
I/V: 50-100mcg/kg
Side effects:
•Dizziness
•Respiratory
depression
•Flushing
•Constipation
•Dysphonia
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.
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.
Contraindications:
•Asthma attack
•Head injury
•Severe liver
disease
•Constipation
Oxycodone:
Available Brands:
•OxyContin ®
•Xtampza ER ®
Oxycodone:
Available Dosage Forms:
•Tablets
•Oral
solutions
Oxycodone:
Mechanism Of Action:
Oxycodone:
Mechanism Of Action:
Oxycodone binds with mu-receptors and produce its analgesic
effect.
Indications Of Oxycodone:
moderate pain
Around the clock
analgesia
severe pain
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:
Doses Of Oxycodone:
For adults: 10mg every 4 hrs PO.
Side effects:
•Dizziness
•Xerostomia
•confusion
•hypotension
•Muscular weakness
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.
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.
Contraindications:
•Hypersensitivity
•Severe bronchial
asthma
•Respiratory depression
•Paralytic ileus
Fentanyl
:
Available Brands:
•Sublimaze
®
•Duragesic ®
•Actiq®
Fentanyl
:
Available Dosage Forms:
•Injectable
•Patches
•Lozenges
•Sublingua
l
•Intranasal
Fentanyl
:
Mechanism Of Action:
Same as morphine.
Indications Of Fentanyl:
Anesthesia
Pain around the
clock
Cancer pain
Chronic pain
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
Side effects:
•Urinary Retention
•Nausea
•Vomiting
•Respiratory
depression
Side effects:
•Urinary Retention
Urinary retention is defined as the inability to completely or
partially empty the bladder.
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
Contraindications:
•Hypotension
•Respiratory insufficiency
•Raised intracranial
pressure
Codeine:
Available Brands:
• Tylenol-
Codeine®
• Prometh®
Codeine:
Available Dosage Forms:
•Solutio
n
•Tablet
•Syrups
Codeine:
Mechanism Of Action:
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.
Indications Of Codeine:
Cough suppressant
Pain reliever
Doses Of Codeine:
For adults:
For pain: 15-60mg every 4-6 hr
For cough: 10-20mg every 4-6hr
Side effects:
•Rashes
•Constipation
•Nausea, vomiting
•Light headedness
•Respiratory
depression(rare)
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
Contraindications:
•Asthma attacks
•Chronic obstructive pulmonary
disease
•Constipation
Hydrocodone:
Available Brands:
• Ambrodic
H®
• Genedic®
Hydrocodone:
Available Dosage Forms:
•Tablet
•Solutio
n
Hydrocodone:
Mechanism Of Action:
It relieves pain by binding to and activating opioid receptors in
the central nervous system.
Indications Of Hydrocodone:
cough
Pain around the
clock
Moderate to severe
pain
Doses Of Hydrocodone:
For adults:
Moderate pain: 2.5-5mg every 4-6hr
Severe pain: 10mg every 4-6 hr
Side effects:
•Nausea
•Vomiting
•Drowsiness
•Hearing loss(very
rare)
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.
Contraindications:
•Liver
Impairment
•Hypersensitivity
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.
Naloxone
:
Available Brands:
• Evzio®
• Narcan
®
Naloxone
:
Available Dosage Forms:
•Injectable
•Nasal
Spray
Naloxone
:
Mechanism Of Action:
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.
Indications Of Naloxone:
To treat opioid over
dosage
Doses Of Naloxone:
For Adults: I/V: 0.4-2mg
For Children's: I/V: 0.01mg/kg
Side effects:
•Hallucination
•Loss of consciousness
•Irregular heart beat
•Pain, burning or redness at the site of
injection
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.
Interactions:
Primary Drug Secondary Drug Effects
Naloxone Droperidol
Increase a risk of irregular
heart beat.
Naloxone alcohol
Side effects of Naloxone
will be worsen.
Tramadol
:
Available Brands:
•Ultram
®
• Tradol
®
Tramadol
:
Available Dosage Forms:
•Tablet
•Suspensio
n
•Capsule
Tramadol
:
Mechanism Of Action:
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.
Indications Of Tramadol:
Management of
moderate to severe
pain
Around the clock
pain
Doses Of Tramadol :
For adults: oral: 50-100mg every 4-6 hrs
Max dose: should not exceed 400mg/day
Side effects:
•Nausea
•Dizziness
•Vertigo
•constipation
•Respiratory depression(very
rare)
Interactions:
Primary Drug Secondary Drug Effects
Tramadol Carbamazepine
Efficacy of tramadol
decreases.
Tramadol Warfarin Increased risk of bleeding
Tramadol Amitriptyline Increased risk of seizures.
Contraindications:
•Hypersensitivity
•Respiratory
depression
• Paralytic ileus
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.
“Antidotes And Its Management”
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.
▪ Usual symptoms of overdose include:
▪ Hypothermia
▪ Respiratory depression
▪ Blurred vision or nystagmus
▪ Stupor like effects/seizure
▪ Coma
Over Dose Symptoms:
▪ 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.
Management Includes:
▪ Give antidote
▪ Gastric lavage
▪ Forced emesis
▪ Assisted ventilation
▪ Dextrose 5%(coma patient)
Barbiturates:
Antidote:
▪ Not recommended
Symptoms Associated With Overdose:
▪ Slurred speech
▪ Nystagmus
▪ Hypothermia
▪ Respiratory arrest
▪ Coma
▪ Seizure
Emergency & Supportive Measure:
▪ Assisted ventilation
▪ Treat Coma, Hypotension & Hypothermia
▪ Dextrose 5%
Management Includes:
For Hypothermia:
▪ Warm the body physically
For Hypotension:
▪ Use I/V fluids i.e. normal saline
▪ Focus on patient rewarming
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.
Symptoms of overdose:
▪ Irregular heartbeat
▪ Shock
▪ Shortness of breath
▪ Blurred vision
▪ Coma
Management Includes:
▪ Cardiac monitoring
▪ Assist ventilation
▪ Activated charcoal
▪ For hypotensive patient, give 20ml/kg of isotonic I/V fluids
▪ Give antidote
Paracetamol:
Antidote:
N-Acetylcystein
Dose Of Antidote:
140mg/kg orally
Mechanism Of Action:
▪ It works by increasing glutathione levels and binding with the toxic
breakdown products of paracetamol.
Symptoms of overdose:
▪ Hepatotoxicity
▪ Jaundice
▪ Liver necrosis
▪ Anorexia
▪ Nausea and vomiting
Management Includes:
▪ Assisted airway
▪ Give anti-emetic (Metacolon)
▪ Activated charcoal
▪ Give antidote
Salicylate:
Antidote :
No specific antidote is reported
Symptoms Of Overdose:
▪ Nausea and vomiting
▪ Tinnitus
▪ Sweating
▪ Shock
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
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.
Symptoms of overdose:
▪ Nausea and vomiting
▪ Hyperkalemia
▪ Decreased consciousness
▪ Respiratory arrest
▪ Tachycardia
Management Includes:
▪ Assisted ventilation
▪ Decontamination
▪ Activated charcoal
For hyperkalemia:
▪ sodium bicarbonate
For seizure treatment:
▪ Diazepam
Opioid:
Antidote:
Naloxone
Dose Of Antidote:
0.4-0.8mg I/V for 2-3 mints,
Mechanism Of Action:
Same as Naloxone (in opioid)
▪ Altered mental status
(delirium)
▪ breathing problems
(may be slow and eventually stops)
Symptoms Of Overdose:
▪ extreme sleepiness or loss of alertness
▪ nausea and vomiting
▪ pupil constriction
▪ Check vitals(temperature, blood pressure, pulse, breathing)
▪ Assist breathing, oxygen if needed.
▪ Fluids(normal saline)
▪ Dextrose if low sugar(coma)
▪ Give Opioid antidote (Naloxone)
▪ Monitor 4-6hours
Management Includes:

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