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Pharmacology: Anti-Inflammatory
Pharmacology: Anti-Inflammatory
Pharmacology: Anti-Inflammatory
N-acetyl-p-aminophenol
phenacetin acetaminophen
analgesic, antipyretic
but weak anti-inflammatory
S/E: Depletes glutathione which binds to toxic
metabolites of paracetamol
(N-acetyl – para -benzoquinone) hepatic
necrosis
Antidote: acetylcysteine glutathion
Anti – inflammatory/analgesics
NSAIDS
MOA: COX inhibition
NON – SELECTIVE COX INHIBITORS
MELOXICAM
SPECIFIC COX II INHIBITORS
Celecoxib, etericoxib
AUTOCOIDS
CLASSIFICATION
PROSTAGLANDIN
Carboprost
Dinoprost
Dinoprostone
Misoprostol – anti -ulver
Alprostadil - impotence
AUTOCOIDS
PROSTAGLANDIN
Lowering IOP
Latanoprost,
bimatoprost,travoprost,noprostone
epoprostenol
( pulmonary HPN, prevent platelet
aggregation in machines)
HISTAMINE
Ethylynediamine
Pyrilamine
tripelenamine
H1 ANTIHISTAMINES
1ST GEN/CLASSIC/SEDATING
Alkylamines
Brompheniramine
Chlorpheniramine
Components of cold tablets
H1 ANTIHISTAMINES
1ST GEN/CLASSIC/SEDATING
Phenothiazines
Promethazine( phenergan)
Anesthetic adjunct to dec stage II
manifestations
H1 ANTIHISTAMINES
1ST GEN/CLASSIC/SEDATING
Piperidine
Cyproheptadine
Significant serotonin antagonist effect
INDICATIONS
Allergy
Motion sickness
Somnifacients
2nd GEN/ NON-SEDATING
Loratidine
Des – loratidine
Fexofenadine
Less- sedating
Cetirizine
Astemizole - cardiotoxic
Terfenadine
Acrivastine
loracarbustine
H2 RECEPTOR
Inc HCL
H3 receptor
Modulation of histaminergic
neurotransmission in the CNS
SEROTONIN RECEPTORS
5- HT1A
Brain
Synaptic inhibition by increasing K
conductance
5- HT1B/1D
Peripheral vascular smooth muscle
5 – HT2A
Smooth muscles
uterus
5- HT3
CTZ
5- HT4
GIT – inc peristalsis
DRUGS ACTING AT 5HT RECEPTORS
5HT1A PARTIAL AGONIST
Buspirone
5HT2A
Methylsergide - antagonist
SEROTONIN ANTAGONIST
5HT3 ANTAGONIST
Ondansetron,
granisetron,dolasetron,alosetron
CTZ block
EICOSANOIDS
BLOOD VESSELS
Vasoconstriction - TXA2, PGF2@
Vasodilation – PGI2,PGE2
Alprostadil, ( impotence) epoprostenol
( pulmonary HPN, prevent platelet
aggregation in machines)
GIT
Contraction- PGI2,PGE2,PGF2@
Relaxation- PGE2
Cytoprotection – PGE series - misoprostol
BRONCHI
Contraction –TXA2, PGF2@, LTC4,LTD4
Relaxation – PGI2, PGF2@
PLATELETS
Aggregation –TXA2
Inh. Of aggregation – PGE1, PGI2
UTERUS
Contraction – PGE1, PGE2, PGF2@
Dinoprostone,Dinoprost,carboprost
Dysmenorrhea – PGE2, PGF2@
EYES
Lowering IOP – PGE and PGF series
Latanoprost,
bimatoprost,travoprost,noprostone
SUMMARY
TXA2
Vasoconstriction
Bronchoconstriction
Platelet aggregation
PGF2@
Vasoconstriction
Bronchoconstriction
Uterine contraction
Dysmenorrhea
Lowering IOP
PGI2
Vasodilation
GIT contraction
Brochodilation
Inh. of platelet aggregation
PGE1
To maintain PDA
PGE2
Vasodilation
GIT contraction and relaxation
Uterine contraction
Dysmenorrhea
Lowers IOP