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Presentation On
AUTACOIDS & IT’S TYPES
Presented By
MOHD ISLAM
BPHARM
2019 Batch
1900140500039
DEFINITION
An organic substance, such as a hormone,
produced in one part of organism and
transported by the blood or lymph toanother
part of the organism where it exerts a
physiologic effect on that part.
TYPES OFAUTACOIDS:
× Amines :Histamine,5-Hydroxytryptamine.
× Lipids
×
:Prostaglandins, Leukotriens,
Platelet activating factor
.
× Peptide :Bradykinin ,angiotensin.
HISTAMINE
× SYNTHESIS AND DEGRADATION OFHISTAMINE
Histidine
decarboxylase
Histamine Imadazole acetic acid
N-methyl transferase
N-methyl histamine
oxidase
Methyl imidazole acetic acid
PHARMACOLOGY
H1 H2 H3
S.M -contraction Gastric gland-acid
secretions
Brain- inhibition of
histamine release- sedation
B.V – vaso dilation B.V-dilation B.V -vasodilatation
Afferent nerve ending -
stimulation
Heart-postive inotropy Skin ,gastric, mucosa-
decrease histaminerelease
Ganglionic cell-stimulation Uterus -relaxation Lungs ,spleen – decrease
histamine release
Adrenal medulla-release of
CAs
Brain -transmitte
CLASSIFICATION
H1 H2 H3
SELECTIV
E
AGONISTS
2-
methylhistamine,2-
pyridylethylamine,
2- thiazolyl
ethylamine
4-methy histamine,
Dimaprit,
impromidine
ἀ-methyl histamine
SELECTIVE
ANTAGONIST
S
Mepyramine,
chlorpheniramin
e
Cimetidin
e,
ranitidine
Thioperamide,
impromidine
RECEPTOR TYPE G-Protein coupled G-P G-P
EFFECTOR PATHWAY IP3/DAG
Ca+ release
C-AMP inc Ca+ infulx ,K+
channel activation,
cAMP dec
THERAPEUTIC INDICATION
× Commoncold
× Motion sickess
× Duodenal ulcer(Zollinger -ellision syndrome)
× Parkinsonism
× Allergicdisorders
× Sedative and hypnotic ,Anxiolytic
ADR: CNS depression, fatigue, gynecomastiain
men, galactorrhea women.
SEROTONIN
× Sertonin (vasoconstrictor) appeared serum.
SYNTHESIS
TRYPTOPHAN
hydroxylase
5-Hydroxytryptophan
decarboxylase
5-HT (MAO) 5-Hydroxy indole acetic acid
dehydrogenase
5-Hydroxy tryptohol
TYPES
RECEPTOR LOCATION MAIN
EFFECT
S
SECOND
MESSENGER
AGONISTS ANTAGONIS
T S
1A CNS Neuronal
inhibition,
Behavioura
l effects
cAMP 5-CT
8-OH-DPAT
Buspirone
Spiperone,
Methiothepi
n,
Ergotamine
1B CNS
VASCULAR
- S.M
Pulmonary
vasoconstrio
n
cAMP 5-CT
Ergotamine
Methiothepin
1D CNS
B.V
Cerebralvaso
constriction,
locomotion
cAMP 5-CT
Sumatriptan
Methiothepi
n
Ergotamine
2A CNS
PNS
S.M
PLATELETS
s.m
contractio
n
IP3/DAG ἀ-Me-5-
HT
LSD(CNS)
LSD(Periphe
r y)
KETANSERIN,
cyprohepta
di ne
2B GASTRI
C
contraction IP3/DAG ἀ-Me-5-HT -
RECEPTOR LOCATION MAIN
EFFECTS
SECOND
MESSENGE
R
AGONISTS ANTAGON
I STS
5-HT3 PNS
CNS
Neuronal
excitatio
n,
emesis
ligand-
gated
cation
channel
2-Me-5-HT,
Chlorophen
yl
biguanide
Ondansetr
on,tropise
t ron
5-HT4 PNS
CNS
Gi motility cAMP 5-methoxy-
tryptamine,
metochlopromid
e
Various
exp.com
p
5-HT5 CNS Not known Not known Not known Not known
5-HT6 CNS Not known Not known Not known Not known
5-HT7 CNS,
GI TRACT,
B.V
Not known cAMP 5-CT,LSD Various 5-
HT2
PHARMACOLOGY
× CVS :Arteries are constricted as well as dilated
by direct action of 5-HT
.
× S.M :Stimualtor ofGIT
.
× GLANDS :It inhibits gastric secretion. Itulcer
protective property.
× RESPIRATION: Hyperventilation
× PLATELETS :5-HT cause change in shapeof
platelets and is a weakaggregator.
THERAPEUTIC USES
× 5-HTAGONISTS : Anxiolytics ( Buspirone),
Depression( Fluoxetine)
Migraine(Ergot alkaloids)
× 5-HTANTAGONISTS: Nausea,emesis,
antineoplastic therapy
(Ondansetron,
Granisetron, Dolasetron)
ADR: Abdominal pain, Muscle cramps,Chest
pain.
PROSTAGANDINS AND LEUKOTRIENES
(EICOSANOIDS)
PHARMACOLOGICAL ACTIONS
ORGAN PGE2 PGF2ἀ PGI2 TXA2
B.V Vaso dilatation Vaso dilatation Vaso dilatation Vaso constriction
HEART Weak inotropic,
cardiac
stimulation
Weak inotropic _ _
PLATELETS Variable effect _ Anti aggregatory aggregation
UTERUS contraction contraction _ _
BRONCHI Dilatatio
n,
inhibits
histamine
constriction Dilatatio
n,
inhibits
histamine
constriction
STOMACH Acid
secretion(dec),
Mucous
production(in
c)
_ Acid _
secretion(dec),
Mucous
production(in
c)
THERAPEUTIC USES
 PGE1 :CHF (Alprostadil)
NSAID-induced GI ulcer (misoprostol)
 PGF2ἀ :Topically to lower intraocular
pressure in glaucoma.
PGI :pulmonary hypertension.(Flolan)
ADR :
Diarrhea ,Hypotension, Flushing,
Cardiac Arrest ,Anemia,
Menstrual irregularities ,Abortion
Decreased renal function.
LEUKOTRIENES
× PHARMACOLOGY:
× CNS :fall inB.P
× S.M :Bronchoconstrictors and spastic
contraction of GIT at lowconcentration
× AFFERENT :Carrying pain impulsesand
tenderness to inflammation.
THERPEUTIC USES
× TREATMENT OF ASTHMA(Zileuton)
× Reduced bronchospasm
× ADR :
× GI upset,
× liverdysfunction
References
Thank You

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Autacoids ppt

  • 1. Presentation On AUTACOIDS & IT’S TYPES Presented By MOHD ISLAM BPHARM 2019 Batch 1900140500039
  • 2. DEFINITION An organic substance, such as a hormone, produced in one part of organism and transported by the blood or lymph toanother part of the organism where it exerts a physiologic effect on that part.
  • 3. TYPES OFAUTACOIDS: × Amines :Histamine,5-Hydroxytryptamine. × Lipids × :Prostaglandins, Leukotriens, Platelet activating factor . × Peptide :Bradykinin ,angiotensin.
  • 4. HISTAMINE × SYNTHESIS AND DEGRADATION OFHISTAMINE Histidine decarboxylase Histamine Imadazole acetic acid N-methyl transferase N-methyl histamine oxidase Methyl imidazole acetic acid
  • 5. PHARMACOLOGY H1 H2 H3 S.M -contraction Gastric gland-acid secretions Brain- inhibition of histamine release- sedation B.V – vaso dilation B.V-dilation B.V -vasodilatation Afferent nerve ending - stimulation Heart-postive inotropy Skin ,gastric, mucosa- decrease histaminerelease Ganglionic cell-stimulation Uterus -relaxation Lungs ,spleen – decrease histamine release Adrenal medulla-release of CAs Brain -transmitte
  • 6. CLASSIFICATION H1 H2 H3 SELECTIV E AGONISTS 2- methylhistamine,2- pyridylethylamine, 2- thiazolyl ethylamine 4-methy histamine, Dimaprit, impromidine ἀ-methyl histamine SELECTIVE ANTAGONIST S Mepyramine, chlorpheniramin e Cimetidin e, ranitidine Thioperamide, impromidine RECEPTOR TYPE G-Protein coupled G-P G-P EFFECTOR PATHWAY IP3/DAG Ca+ release C-AMP inc Ca+ infulx ,K+ channel activation, cAMP dec
  • 7. THERAPEUTIC INDICATION × Commoncold × Motion sickess × Duodenal ulcer(Zollinger -ellision syndrome) × Parkinsonism × Allergicdisorders × Sedative and hypnotic ,Anxiolytic ADR: CNS depression, fatigue, gynecomastiain men, galactorrhea women.
  • 8. SEROTONIN × Sertonin (vasoconstrictor) appeared serum. SYNTHESIS TRYPTOPHAN hydroxylase 5-Hydroxytryptophan decarboxylase 5-HT (MAO) 5-Hydroxy indole acetic acid dehydrogenase 5-Hydroxy tryptohol
  • 9. TYPES RECEPTOR LOCATION MAIN EFFECT S SECOND MESSENGER AGONISTS ANTAGONIS T S 1A CNS Neuronal inhibition, Behavioura l effects cAMP 5-CT 8-OH-DPAT Buspirone Spiperone, Methiothepi n, Ergotamine 1B CNS VASCULAR - S.M Pulmonary vasoconstrio n cAMP 5-CT Ergotamine Methiothepin 1D CNS B.V Cerebralvaso constriction, locomotion cAMP 5-CT Sumatriptan Methiothepi n Ergotamine 2A CNS PNS S.M PLATELETS s.m contractio n IP3/DAG ἀ-Me-5- HT LSD(CNS) LSD(Periphe r y) KETANSERIN, cyprohepta di ne 2B GASTRI C contraction IP3/DAG ἀ-Me-5-HT -
  • 10. RECEPTOR LOCATION MAIN EFFECTS SECOND MESSENGE R AGONISTS ANTAGON I STS 5-HT3 PNS CNS Neuronal excitatio n, emesis ligand- gated cation channel 2-Me-5-HT, Chlorophen yl biguanide Ondansetr on,tropise t ron 5-HT4 PNS CNS Gi motility cAMP 5-methoxy- tryptamine, metochlopromid e Various exp.com p 5-HT5 CNS Not known Not known Not known Not known 5-HT6 CNS Not known Not known Not known Not known 5-HT7 CNS, GI TRACT, B.V Not known cAMP 5-CT,LSD Various 5- HT2
  • 11. PHARMACOLOGY × CVS :Arteries are constricted as well as dilated by direct action of 5-HT . × S.M :Stimualtor ofGIT . × GLANDS :It inhibits gastric secretion. Itulcer protective property. × RESPIRATION: Hyperventilation × PLATELETS :5-HT cause change in shapeof platelets and is a weakaggregator.
  • 12. THERAPEUTIC USES × 5-HTAGONISTS : Anxiolytics ( Buspirone), Depression( Fluoxetine) Migraine(Ergot alkaloids) × 5-HTANTAGONISTS: Nausea,emesis, antineoplastic therapy (Ondansetron, Granisetron, Dolasetron) ADR: Abdominal pain, Muscle cramps,Chest pain.
  • 14. PHARMACOLOGICAL ACTIONS ORGAN PGE2 PGF2ἀ PGI2 TXA2 B.V Vaso dilatation Vaso dilatation Vaso dilatation Vaso constriction HEART Weak inotropic, cardiac stimulation Weak inotropic _ _ PLATELETS Variable effect _ Anti aggregatory aggregation UTERUS contraction contraction _ _ BRONCHI Dilatatio n, inhibits histamine constriction Dilatatio n, inhibits histamine constriction STOMACH Acid secretion(dec), Mucous production(in c) _ Acid _ secretion(dec), Mucous production(in c)
  • 15. THERAPEUTIC USES  PGE1 :CHF (Alprostadil) NSAID-induced GI ulcer (misoprostol)  PGF2ἀ :Topically to lower intraocular pressure in glaucoma. PGI :pulmonary hypertension.(Flolan) ADR : Diarrhea ,Hypotension, Flushing, Cardiac Arrest ,Anemia, Menstrual irregularities ,Abortion Decreased renal function.
  • 16. LEUKOTRIENES × PHARMACOLOGY: × CNS :fall inB.P × S.M :Bronchoconstrictors and spastic contraction of GIT at lowconcentration × AFFERENT :Carrying pain impulsesand tenderness to inflammation.
  • 17. THERPEUTIC USES × TREATMENT OF ASTHMA(Zileuton) × Reduced bronchospasm × ADR : × GI upset, × liverdysfunction