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BY: KOMAL HALEEM PHARM-D
PARACETAMOL
OTC
Also known as,
ACETAMINOPHEN
DESCRIPTION
-Analgesic
-Antipyretic
-Central action> Peripheral action
-NO
 GI disturbances
 Acid-base imbalance
 Electrolyte imbalance
 Impairment of clotting
-ADR :
 Extremely safe drug. But rarely produces …. Hepatic toxicity
Mechanism Of Action :
Inhibits the cycloxygenase
Enzyme
REDUCES PROSTAGLANDIN SYNTHESIS
MOST
IMPORTANT
MECHANISMS
BRAND NAMES
VANCOCIN
ELI LILLY PAKISTAN (PVT)
LTD.
VANCOMYCIN
ABBOTT
LABORATORIES
(PAKISTAN) LIMITED.
-acts primarily in the CNS
-increases the pain threshold by
inhibiting both isoforms of
cyclooxygenase,
-COX-1, COX-2 and COX-3 enzymes
involved in prostaglandin (PG)
synthesis.
When normal
dose of
paracetamol is
taken major
amount is
metabolized by
glucuronid e and
sulfate
conjugation
Minor amount of
highly reactive
quinones/epoxides
are formed
They combine
with Glutathione
Converted to
harmless products
NO Tissue damage
When large amount
of drug is
taken(poisoning)
Large number of
highly reactive
quinones/epoxides
are formed
Glutathione supply
falls short.
Toxic intermediates
are formed within
tissue constituents
Tissue damage
NAC SUPPLIES
GLUTATHIONE
S
so detoxifies toxic
metabolites !!
NAC
“MAY”directly
conjugates with
quinones/epoxide.
MAY BE…
NAC has
additional
antioxidant and
antiinflammatory
activity
PERIPHERALLY
: PGS sensitize the
nerve endings to
bradykinin and
histamine
CENTRALLY :
PGs Lower the
threshold for
central pain
circuits
PAIN
PCM
blocks..
7
REDUCES
THE
INTENSITY
OF PAIN
ANALGESIC ACTIVITY
 Hypothalamus contains thermoregulatory centre
 Maintains balance between heat production and heat
loss
 It regulates heat dissipating mechanisms
When there is
tissue
damage/infla
mation/AG:A
B
reaction/infec
tion
Neutrophil
releases IL-1
Stimulates
COX-2
enzymes
Increased
PGE2
synthesis in
hypothalamus
PGE2 has two
mechanisms :
1. Increases
heat production.
2.shuts down
HEAT LOSING
MECHANISM
Raised body
temperature
 FEVER
NSAIDS inhibits
PGE2 synthesis and
reduces fever
ANTIPYRETIC ACTIVITY
Normally
hypothalamus is
adjusted to a set
point
When
temperatures is
elevated beyond
level
Hypothalamus
activates heat
losing mechanisms
like sweating and
vasodilatation
So temperature is
normalized
This set point it
elevated in
FEVER
ANTIPYRETIC ACTIVITY
direct effects on heat-
regulating centres of the
hypothalamus
Sweating and
vasodilation,
heat dissipation
IBUPROFEN
WHAT IS IBUPROFEN?
 Reduces:
• fever,
• pain
• inflammation
 Caused by:
many conditions such as headache, toothache, back
pain, arthritis, menstrual cramps, or minor injury
BRAND NAMES
Brufen®;
Calprofen®;
Nurofen®;
Orbifen®;
Fenbid®
PREPARATIONS
-Tablets:
- 100, 200, 400, 600, and 800 mg;
Suspension:
100 mg/5 ml and 40 mg/ml
-Chewable tablets:
50 and 100 mg;
ALSO AVAILABLE AS:
capsules,
granules,
oral liquid medicine,
modified-release tablets,
orodispersible (melt in the
mouth) tablets
 local gel
USUAL ADULT DOSE FOR PAIN:
Oral: Mild to moderate pain:
200 to 400 mg orally every 4
to 6 hours as needed. Doses
greater than 400 mg have not
been proven to provide
greater efficacy
IV: (Patients should be well hydrated
before IV ibuprofen administration):
Pain: 400 to 800 mg intravenously
over 30 minutes every 6 hours as
needed.
USUAL ADULT ANTI-
INFLAMMATORY DOSE
for Osteoarthritis:
Initial dose: 400 to 800 mg
orally every 6 to 8 hours.
Maintenance dose: May be
increased to a maximum
daily dose of 3200 mg based
on patient response and
tolerance.
for Rheumatoid Arthritis:
Initial dose: 400 to 800 mg
orally every 6 to 8 hours.
Maintenance dose: May be
increased to a maximum
daily dose of 3200 mg based
on patient response and
tolerance.
REFERENCES
http://www.drugs.com/ibuprofen.html
http://www.patient.co.uk/medicine/ibuprofen-for-
pain-and-inflammation
http://www.spine-health.com/treatment/pain-
medication/nsaids-non-steroidal-anti-inflammatory-
drugs
http://www.medicinenet.com/ibuprofen/article.htm
http://www.medicinenet.com/acetaminophen/article.
htm
https://www=mechanism+of+action+of+paracetam
ol&tbm=isch&imgdii
http://www.ncbi.nlm.nih.gov/pubmed/15662292
Paracetamol: Mechanism of Action and Uses of this OTC Analgesic
Paracetamol: Mechanism of Action and Uses of this OTC Analgesic

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Paracetamol: Mechanism of Action and Uses of this OTC Analgesic

Editor's Notes

  1.  nostrils). The rest of the respiratory tract, open wounds, intravenous catheters, and theurinary tract are also potential sites for infection (MRSA)