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 Analgesic Are the Drugs which selectively

relieves pain by acting in the CNS or on


peripheral pain mechanisms, without
significantly altering the consciousness –
Opioids and NSAIDS

 Opioids are Any drug which binds to the


opioid receptors (Pharmacologically
related) in the CNS and antagonized by
Naloxone . They may be – Natural,
Synthetic and semisynthetic
 Opiates
Drugs derived from opium – Natural or
semisynthetic

 Narcotics
Drugs derived from opium or opium like
compounds, with potent analgesic effects
associated with significant alteration of mood
and behavior, and with the potential for
dependence and tolerance following repeated
administration.
Nociceptive
Pain
Pain arising from tissue
damage

Type Of
Pain

Neuropatic
Pain Other Pain
Pain arising from neurogical
Pain arising from damage dysfunction, not damage
to the damage –reporting like fibromyalgia
system itself, the
nervous system
A dark brown, resinous material obtained
from poppy (Papaver somniferum) Capsules.
Morphine 9-14%

Codein 0,5-2%

Thebaine 0,2-1%

phenantrene opium Benzylisoquinoline

Papaverin 0,8-1%

Noscapin 3-10%

Narcine 0,2-0,4%
 Friedrich Wilhelm Serturner
A German Pharmacist
 Isolated Morphine in 1803 and named it
after the Greek god of Dreams
“MORPHEUS”
 Strong Analgesic
 Visceral pain is relieved better than
somatic pain
 Degree of analgesia increases with
dose
 Nociceptive pain is better relieved
than Neuretic pain
 Two components – spinal and supraspinal
 Inhibits release of excitatory transmitters
from primary afferents – at Substantia
gelatinosa of dorsal horn
 Exerted through Interneurones – geting of
pain
 At supraspinal level in cortex, meidbrain and
medulla - alter processing and interpretation
and send inhibitory impulses through
descending pathway
Sedation
 Drowsiness and indifference to surroundings
 Inability to concentrate and extravagant
imagination – colorful day dream
 Apparent excitement
Mood Effect
 In Normal persons calming effect, mental
clouding, feeling of detachment, lack of
initiative etc. - unpleasant in absence of
pain
 Sometimes DYSHORIA
 But in persons with pain & addicts sense
of wellbeing, pleasurable floating feelings
– kick EUPHORIA
Depression
 Respiratory centre depression – Both rate and
depth of respiration are diminished
- Dangerous in Head injury and asthmatics
 Cough Centre – Depressed
 Temperature regulating centre – depressed
 Vasomotor centre – high doses cause fall in
BP
Stimulation
 CTZ – sensitize CTZ to vestibular and other
impulses
 Edinger Westphal Nucleus – miosis
 Vagal centre – Bradycardia
 Hippocampal cells – convulsions (inhibition of
GABA release)
Neuro-endocrine
 GnRH and CRH are inhibited – FSH, LH and
ACTH levels are lowered – only short term –
tolerance develops
 Decrease in levels of Sex hormone and
corticosteroids, but no infertility
 Increases ADH release – oliguria
Cardiovascular
 Vasodilatation – histamine release,
depression of vasomotor centre and directly
on blood vessels decreasing the tone
 Cardiac work reduction due to consistent
vasodilatation
GIT
 Due to direct action on intestine reducing
propulsive movement, spasm of sphincters,
decrease in all GIT secretions
Smooth Muscle
 Billiary Tract: Billiary colic – closure of sph.
Of Oddi
 Bladder: Urinary urgency but difficulty
 Bronchi - Bronchospasm
 Respiratory Depression: Infant and Old
 Vomiting
 Sedation, Mental Clouding – sometimes dysphoria
 Hypotensive effect
 Rise in Intracranial Pressure
 Apnoea: Newborn
 Urinary retention
 Idiosyncrasy and allergy
 Acute Morphine Poisoning: occurs if >50 mg (Lethal
dose –250 mg), Gastric lavage with KMNO4, Specific
antidote: Naloxone: 0.4 to 0.8 mg IV repeatedly in 2-
3 minutes till respiration picks up
 Tolerance and dependence
 Long Bone Fracture
 Myocardial Infarction
 Terminal stages of cancer
 Burn patients
 Postoperative patients
 Visceral pains – pulmonary embolism,
pleurisy, acute pericarditis
 Biliary colic and renal colic
 Obstetric analgesia
 Segmental analgesia
 Preanaesthetic Medication
 Balanced anaesthesia and surgical analgesia
 Acute Left ventricular failure – Cardiac
 Asthma
 Cough – not used but Codeine is used
 Diarrhoea – colostomy - Loperamide,
Diphenoxylate
 Two Extremes of Age
 Bronchial asthma
 Respiratory insufficiency – empysema
 Head Injury
 Shock – Hypotension
 Undiagnosed acute abdomen
 Renal Failure, Liver diseases and
hypothyrodism
 Unstable personalities