Nome -jhabar ola
Growp 314
Week 3
ENDOCRINE PHARMACOLOGY
ENDOCRINE SYSTEM
·Tne endocrine system is controlled by two parts of the broin:
Tne Pitwitory gland and the Hypotnalamwg.
·T t
l obde
en
·FUNCTIONS:Maintain Internal Homeostagus,Support CelU
Growth,Coordinate Development,Coordinate Reprodwctuon,
External Stimwlu.
e
y
biochemica
uons of owr
of
nc
the for
ariows
n
v
ormation i
inates the
f
d
n
r
u
o
itting
em co
m
st
g
y
n
s
tro
nis
individwal cels and tisswes of the body.
·Twe messengers called os HORMONES.
fertility,sexwal function AND Facilitate Responses to
Posteruor pitwitary
· Oxytocin
·Antiduwretic
vormone
Anteruor Pitwitory
·Somatotropvs:Growth
·Twyrotrophs:TSH
· Gonadotroph8:
· Lactotrophs:Prolactin
· Corticotroph8
Fig A:Location of Pituitary Gland
hormones
CONTENTS
·Growtn Hormone
·Prolactin
·Sex Hormones
·Oral Contraceptives
·Corticosteroidg
2DDl./Tu LDD MDNIE
Clinical digorderg
·GH defuciency in children leads to short statwre,
me, Proder-wili syndrome,Cnronic renal
·GH defuciency in adwlts leods to decreose in mwscle mass,
Treatmevt
,N op i pe
Н ору- Сето(горИ
НитО(горе
ini
rer«& ;
c
eWe ono monWlored. for
a he ea Цitуun ,оLр a( chuldren)
Artwrolquos, Mvolquog.
e
о
У
m
з
и
o
и
s
у
m
ет
о
a
д
k
е
u
Ш
e
и
g
р
m
и
o
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м
aus
омм
о
n
к
,
с
c
г
о
e
З
:
h
Т
s,
Е
О
e
Е
g
Н
n
Е
a
Е
h
І
О
c
Я
pliance
-1 Uev
om
IGF
and
Uq/lq
s
0
ponse
rome:5
re
vn
tial
Tw
·
tc
е
т
e
м
ro
м
«
t
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е
т
m
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n
е
i
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tr
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w
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n
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i
м
p
о
o
м
r
и
r
о
o
с
N
Р
е
y
ro
n
n
uvgwffucie
Twrnerssy
Type 2DM.In Adwlts:Peripheral edema,Corpaltwnnel syndrome,
Derivative of GH Somatrem(wsed in children with defuciency)
decreaged bone dengity,impoired psychosociol fwnctuon.
·Increases mortality rates after Heart gwrgery or abdominal
Doge:40 μg/kg/day -Swbcwtaneowsly in evening.
swrgery, acwte respiratory failwre.
Prolactin
·It is gtrwctwraly related to GH.
·Secreted by Lactotrophs of anteruor pitwitary.Wuth other
wormones it initiates milk prodwctuon in mammary glands.
·Serum levels remains low in normal males throwgvowt life
avd gomewhat in femaleg.
·Prolactin levels rise morkedly dwring pregnancy reach
maximum at term and decline thereafter wnless the
infant.
·Only after mommary glands primed by Estrogen,Progesterone,
gwcocortucoids,hGH,thyroxin and inswlin evert permissive
effects, prolactin brungs abowt milk gecretion.
·Ejectuon of milk from mammary glands depends on Oxytocin
hormone(released from posteruor pitwitary)
motver breostfeedg the
Pwysiological effect:
differe tuon of the ductaland lobuloalveolor epitheviwm
Prolactin Excesg:
рег
r
т
eno
re
ш
from
Hyper secretion in moles:Erectile dysfunctuon(impotency)
·
·
s
е
t
ч
wl
о
л
s
с
o
у
)
s
И
t
О
i
т
s,
о
г
a
т
m
о
Ы
a
И
y
с
т
ar
д
о
t
т
g
т
о
n
т
i
о
t
о
e
(
ec
У
а
s
т
n
м
u
и
t
Х
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с
la
И
о
o
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r
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p
р
y
у
a
у
u
м
д
n
О
hypothalamicorpitwitary disease that unterfere with
·
delivery of unhubitory dopaminergucgignals
Primory hyperthyroidism with increased TRH levels,Renol
Hyper secretion in females:Galactorrhea (inappropriate
lactatuon),Amenorrhea(Absence of menstrwal cycle)and
ProuodluplovsonvWmportont roleWn undivoMnq growlv
uWUc)w Ug esgential for lactatuon.
unfertility
failwre.
SEX HORMONES
·Estrogens and progestuns (steroid wormones)
·In women they control ovwlatuon,cyclical preporatuon of the
·Estrogensin males have effects on bone,spermatogenesis
ond benavuor.
·Estrogen and progestins are wsed in menopowsal hormone
therapy(MHT)and contraception in women.
·Estrogen and progestin antagonists are also available.
reproductive tract for fertilization and implantatuon and
metabolic actiong.
ESTROGENS
·Steroidal and non steroidal compownds.Tne most potent
occurrung estrogen in humans for both estrogen receptor a and
·Tney oW contoin a phemolic A rung with OH growp at C3 and β-
·Pnenolic ring is respongible for selective hwigh affunity for both
receptors.
·Diethyl stulbestrol,strwctwrolly similor to estrodiol(trans)
high affunity,same potency bwt longer half life.
·Non steroidal compounds with estrogenic or anti estrogenic
activity:Flavones,isoflavones(genistain),cowmestan
derivatives,DES,
Busphenol A,Genigtein.
Steroidal:Estradiol,Estradiol Valerate,Ethinylestradiol,
Mestromol, Estrone swlfate,Eqwlin
Synthetic:Pesticides,Plagticizers etc
·
·
OH or ketone un 17th pogutuon of ring D.
β are 17 β-egtradiol,estrone,estruol.
natwrally
Egtrogen wse during pregnancy also can increase the
off8prung..
Estrogen in postmenopowsal women increases the risk of
enmdometrial carcinoma by 5-15-fold.
·Oral estrogens signifucantly increase the risk of
·Estrogens may cowse severe migraine in some women.
·Estrogens also may reactivate or evacerbate endometruosis
tvromboemboluc disease in healthy women.
·Nawsea and vomiting occwr in some women but often disappear
with tume.
Adverse effects:
·Increased uncidence of vaginal and cervicol
adenocarcinoma wa8 noted in female offspring of mothers
incidence of monmalignant genitol abnormalitues in
who nad taken
diethylstulbestrol.
Tnerapewtic wses
· As components of combination oral controceptives and for MHT.
· Egtrogen theropy in postmemopowsal women:omeliorotion of
vagomotor symptoms and the prevention of bone fractwres/
Osteoporosis and wrogenitol atropvy.
·Vaginal Dryness and Urogenital Atrophy
· Estrogen treatment in the failwre of ovorian development.
·S elective estrogenm receptor modwlotors :TAMOXIFEN,RALOXIFENE,
AND TOREMIFENE,Tneir phormacologucal goal is to prodwce
beneficial estrogenicactuons in certain tissues (e.g.,bone,
brain,and liver)but antagonist activity in others (e.g,breast
Antlestrogens: CLOMIPHENE AND FULVESTRANT Tnese compounds
are pwre antagonists un all tusswes.Clomiphene us approved for
treatment of infertility in anovwlatory women;fwlvestrantig
wsed to treat breogt cancer un women with digeage progresgion
after
tamoyufenv.
·
and endometriwm).
tve
PROGESTINS
·Tne progestins ore widely wsed with estrogens for MHT and
gure .ituations in which a selective progestotuonal effect
Progesterone is secreted by the corpws lwteum dwring the
Pnormacologucal octlons:
·Progesterone prodwced in the wteal phose of the cycle
·Progesterone decreoses estrogen-driven endometriol
·Mammory glond development requires both estrogen and
progesterone.Dwring pregnancy,wteal phase of the cycle,
de
er
g
th
u
o
progesterone acts with estrogen to undwce proliferation of the
proliferation and indwces a secretory endometruum.
second half of the menstrwal cycle wnder the stimwws of LH.
decreoses the freqwency of GnRH pwlsex.
acini of the mammary gland
Tneropewtic wgeg:
·Tne two most freqwent wses of progestins are for contraceptuony
either alone or with an egtrogen,and un combunatuon with
ииЧгодРл Гог УогтиотР ЦмРгору оЁрозЧтРторалчаХ
мотЄт
·Progestins also ore wsed for secondory amenorrhea,
ab
e beedung upaluents wWtoul underlyung fUbroUds or
uleruw
normal
concer, wteal-phase swpport to treat infertulity,and
prematwre labor.
·Progestins ore wsed diagnosticaWy to test for estrogen
secretion and for responsiveness of the endometriwm.
·Progestinsore hig
y
cinoma
car
the
n
n
a
gi
perplasia
in decreo
h
s
l
w
a
o
i
i
endometr
hly efficoc
солvsed by wnopposed egtrogen8.
к РкодевЧиоте оМко ихеф Гог
тоАозЧоАио
СОСИУОм О . Megestrol acetate is
wsed
treatment for breagt
СОЛУСАРлГс
емдотёАгиоУ
ag a gecond-line
occwrrence of
·Oral contraceptives ore widely wsed worldwide and have
uod a revovwtuonary umpact by providing a convenient,
·In addition to controceptive actions,these agents have
gwbstantial health benefits.
Birth control (contraceptive)medications contain hormones
(estrogen and progesterone,or progesterone alone).
· Estrogens:Ethinylestrodiol,Mestromol
· Progesterones: Noretuynodrel,Norethindrone
Norethindrone acetote,Norgegtimate
Desogestrel,Etuyvodiol diacetote
Norgestrel,Levomorgestrel,Drospirenone
affordable,and reviable means of contraceptuon.
Cortucosteroidg
·Tvese orea class of steroid vormones that are prodwced in
the
wormone8.
·Tne term corticosteroid'or corticoid'unclwdes natwralglwco-
·Two moin closses of corticosteroidg:guwcocorticoidg ond
muneralocortucoudg.
·They are unvolved in a wide range of physuological processes,
unclwding stress reponse,ummwne response,regwlatuon of
and mineralo-corticoids and their synthetic analogwes.
adrenal cortex,it inclwdes synthetic analogues of these
unflammatuon,carbohydrate metabolism,protein
blood electrolyte levels,and benavior.
cataboligm,
Muneralocorticoid actiong:
·Tne pruncipal mineralocortucoud action is enhancement of
DiLwti omaL oenaton ia 0ve0 W0t0 0no
blood volwme and
·
Hyperkaloemia and acidosis.
iged haematocrit
ceUular hyd
Na+ reabsorptuon in the dugtolconvolwtedtwbwle un
kudney.
·Its deficiency reswlts in decreosed mayimaltwbwlar
Tnese distortions offlwid and electrolyte balance progress
and contribute to the circwlatory collapse.
·Tne action of aldogterone is exerted by gene mediated
increaged
trangcription of m-RNA in renal twbwlar cells wnich directs
reabsorptive capacity for Na
synthesus of proteun8.
·Delayed neoling:of wownds and swrgical incigiong.
·Glowcomo:may develop in swsceptible individwals after
prolonged topucal therapy.
· Growthretardation:inchildrenoccwrseven withsmaldogesif
·
given for long periods.
CONTRAINDICATIONS:
Peptic wlcer,Diabetes mellitws,Hypertengion,Vural and fwngal
Twbercwlosis ond other infectuons,Ogteoporogus,Herpes gimplex
keratitis Psycnogis,Epilepsy CHF,Renal fouwre.
Pgychiatric distwrbances:mild ewpvoria freqwently
accompanies high doge steroid treatment.Tnis may rarely
progress to monic psychosus. Nervowsness,decreosed gleep
and mood changes.
unfectuong
ТНАМКУО
Ш

pharmacology week 3.pptx education related kuch bhi

  • 1.
    Nome -jhabar ola Growp314 Week 3 ENDOCRINE PHARMACOLOGY
  • 2.
    ENDOCRINE SYSTEM ·Tne endocrinesystem is controlled by two parts of the broin: Tne Pitwitory gland and the Hypotnalamwg. ·T t l obde en ·FUNCTIONS:Maintain Internal Homeostagus,Support CelU Growth,Coordinate Development,Coordinate Reprodwctuon, External Stimwlu. e y biochemica uons of owr of nc the for ariows n v ormation i inates the f d n r u o itting em co m st g y n s tro nis individwal cels and tisswes of the body. ·Twe messengers called os HORMONES. fertility,sexwal function AND Facilitate Responses to
  • 3.
    Posteruor pitwitary · Oxytocin ·Antiduwretic vormone AnteruorPitwitory ·Somatotropvs:Growth ·Twyrotrophs:TSH · Gonadotroph8: · Lactotrophs:Prolactin · Corticotroph8 Fig A:Location of Pituitary Gland hormones
  • 4.
  • 5.
  • 6.
    Clinical digorderg ·GH defuciencyin children leads to short statwre, me, Proder-wili syndrome,Cnronic renal ·GH defuciency in adwlts leods to decreose in mwscle mass, Treatmevt ,N op i pe Н ору- Сето(горИ НитО(горе ini rer«& ; c eWe ono monWlored. for a he ea Цitуun ,оLр a( chuldren) Artwrolquos, Mvolquog. e о У m з и o и s у m ет о a д k е u Ш e и g р m и o Т м aus омм о n к , с c г о e З : h Т s, Е О e Е g Н n Е a Е h І О c Я pliance -1 Uev om IGF and Uq/lq s 0 ponse rome:5 re vn tial Tw · tc е т e м ro м « t и n е т m о о O И n е i Р tr Н w С n Х i м p о o м r и r о o с N Р е y ro n n uvgwffucie Twrnerssy Type 2DM.In Adwlts:Peripheral edema,Corpaltwnnel syndrome, Derivative of GH Somatrem(wsed in children with defuciency) decreaged bone dengity,impoired psychosociol fwnctuon. ·Increases mortality rates after Heart gwrgery or abdominal Doge:40 μg/kg/day -Swbcwtaneowsly in evening. swrgery, acwte respiratory failwre.
  • 7.
    Prolactin ·It is gtrwctwralyrelated to GH. ·Secreted by Lactotrophs of anteruor pitwitary.Wuth other wormones it initiates milk prodwctuon in mammary glands. ·Serum levels remains low in normal males throwgvowt life avd gomewhat in femaleg. ·Prolactin levels rise morkedly dwring pregnancy reach maximum at term and decline thereafter wnless the infant. ·Only after mommary glands primed by Estrogen,Progesterone, gwcocortucoids,hGH,thyroxin and inswlin evert permissive effects, prolactin brungs abowt milk gecretion. ·Ejectuon of milk from mammary glands depends on Oxytocin hormone(released from posteruor pitwitary) motver breostfeedg the
  • 8.
    Pwysiological effect: differe tuonof the ductaland lobuloalveolor epitheviwm Prolactin Excesg: рег r т eno re ш from Hyper secretion in moles:Erectile dysfunctuon(impotency) · · s е t ч wl о л s с o у ) s И t О i т s, о г a т m о Ы a И y с т ar д о t т g т о n т i о t о e ( ec У а s т n м u и t Х c с la И о o о r г p р y у a у u м д n О hypothalamicorpitwitary disease that unterfere with · delivery of unhubitory dopaminergucgignals Primory hyperthyroidism with increased TRH levels,Renol Hyper secretion in females:Galactorrhea (inappropriate lactatuon),Amenorrhea(Absence of menstrwal cycle)and ProuodluplovsonvWmportont roleWn undivoMnq growlv uWUc)w Ug esgential for lactatuon. unfertility failwre.
  • 9.
    SEX HORMONES ·Estrogens andprogestuns (steroid wormones) ·In women they control ovwlatuon,cyclical preporatuon of the ·Estrogensin males have effects on bone,spermatogenesis ond benavuor. ·Estrogen and progestins are wsed in menopowsal hormone therapy(MHT)and contraception in women. ·Estrogen and progestin antagonists are also available. reproductive tract for fertilization and implantatuon and metabolic actiong.
  • 10.
    ESTROGENS ·Steroidal and nonsteroidal compownds.Tne most potent occurrung estrogen in humans for both estrogen receptor a and ·Tney oW contoin a phemolic A rung with OH growp at C3 and β- ·Pnenolic ring is respongible for selective hwigh affunity for both receptors. ·Diethyl stulbestrol,strwctwrolly similor to estrodiol(trans) high affunity,same potency bwt longer half life. ·Non steroidal compounds with estrogenic or anti estrogenic activity:Flavones,isoflavones(genistain),cowmestan derivatives,DES, Busphenol A,Genigtein. Steroidal:Estradiol,Estradiol Valerate,Ethinylestradiol, Mestromol, Estrone swlfate,Eqwlin Synthetic:Pesticides,Plagticizers etc · · OH or ketone un 17th pogutuon of ring D. β are 17 β-egtradiol,estrone,estruol. natwrally
  • 11.
    Egtrogen wse duringpregnancy also can increase the off8prung.. Estrogen in postmenopowsal women increases the risk of enmdometrial carcinoma by 5-15-fold. ·Oral estrogens signifucantly increase the risk of ·Estrogens may cowse severe migraine in some women. ·Estrogens also may reactivate or evacerbate endometruosis tvromboemboluc disease in healthy women. ·Nawsea and vomiting occwr in some women but often disappear with tume. Adverse effects: ·Increased uncidence of vaginal and cervicol adenocarcinoma wa8 noted in female offspring of mothers incidence of monmalignant genitol abnormalitues in who nad taken diethylstulbestrol.
  • 12.
    Tnerapewtic wses · Ascomponents of combination oral controceptives and for MHT. · Egtrogen theropy in postmemopowsal women:omeliorotion of vagomotor symptoms and the prevention of bone fractwres/ Osteoporosis and wrogenitol atropvy. ·Vaginal Dryness and Urogenital Atrophy · Estrogen treatment in the failwre of ovorian development. ·S elective estrogenm receptor modwlotors :TAMOXIFEN,RALOXIFENE, AND TOREMIFENE,Tneir phormacologucal goal is to prodwce beneficial estrogenicactuons in certain tissues (e.g.,bone, brain,and liver)but antagonist activity in others (e.g,breast Antlestrogens: CLOMIPHENE AND FULVESTRANT Tnese compounds are pwre antagonists un all tusswes.Clomiphene us approved for treatment of infertility in anovwlatory women;fwlvestrantig wsed to treat breogt cancer un women with digeage progresgion after tamoyufenv. · and endometriwm). tve
  • 13.
    PROGESTINS ·Tne progestins orewidely wsed with estrogens for MHT and gure .ituations in which a selective progestotuonal effect Progesterone is secreted by the corpws lwteum dwring the Pnormacologucal octlons: ·Progesterone prodwced in the wteal phose of the cycle ·Progesterone decreoses estrogen-driven endometriol ·Mammory glond development requires both estrogen and progesterone.Dwring pregnancy,wteal phase of the cycle, de er g th u o progesterone acts with estrogen to undwce proliferation of the proliferation and indwces a secretory endometruum. second half of the menstrwal cycle wnder the stimwws of LH. decreoses the freqwency of GnRH pwlsex. acini of the mammary gland
  • 14.
    Tneropewtic wgeg: ·Tne twomost freqwent wses of progestins are for contraceptuony either alone or with an egtrogen,and un combunatuon with ииЧгодРл Гог УогтиотР ЦмРгору оЁрозЧтРторалчаХ мотЄт ·Progestins also ore wsed for secondory amenorrhea, ab e beedung upaluents wWtoul underlyung fUbroUds or uleruw normal concer, wteal-phase swpport to treat infertulity,and prematwre labor. ·Progestins ore wsed diagnosticaWy to test for estrogen secretion and for responsiveness of the endometriwm. ·Progestinsore hig y cinoma car the n n a gi perplasia in decreo h s l w a o i i endometr hly efficoc солvsed by wnopposed egtrogen8. к РкодевЧиоте оМко ихеф Гог тоАозЧоАио СОСИУОм О . Megestrol acetate is wsed treatment for breagt СОЛУСАРлГс емдотёАгиоУ ag a gecond-line occwrrence of
  • 16.
    ·Oral contraceptives orewidely wsed worldwide and have uod a revovwtuonary umpact by providing a convenient, ·In addition to controceptive actions,these agents have gwbstantial health benefits. Birth control (contraceptive)medications contain hormones (estrogen and progesterone,or progesterone alone). · Estrogens:Ethinylestrodiol,Mestromol · Progesterones: Noretuynodrel,Norethindrone Norethindrone acetote,Norgegtimate Desogestrel,Etuyvodiol diacetote Norgestrel,Levomorgestrel,Drospirenone affordable,and reviable means of contraceptuon.
  • 17.
    Cortucosteroidg ·Tvese orea classof steroid vormones that are prodwced in the wormone8. ·Tne term corticosteroid'or corticoid'unclwdes natwralglwco- ·Two moin closses of corticosteroidg:guwcocorticoidg ond muneralocortucoudg. ·They are unvolved in a wide range of physuological processes, unclwding stress reponse,ummwne response,regwlatuon of and mineralo-corticoids and their synthetic analogwes. adrenal cortex,it inclwdes synthetic analogues of these unflammatuon,carbohydrate metabolism,protein blood electrolyte levels,and benavior. cataboligm,
  • 18.
    Muneralocorticoid actiong: ·Tne pruncipalmineralocortucoud action is enhancement of DiLwti omaL oenaton ia 0ve0 W0t0 0no blood volwme and · Hyperkaloemia and acidosis. iged haematocrit ceUular hyd Na+ reabsorptuon in the dugtolconvolwtedtwbwle un kudney. ·Its deficiency reswlts in decreosed mayimaltwbwlar Tnese distortions offlwid and electrolyte balance progress and contribute to the circwlatory collapse. ·Tne action of aldogterone is exerted by gene mediated increaged trangcription of m-RNA in renal twbwlar cells wnich directs reabsorptive capacity for Na synthesus of proteun8.
  • 19.
    ·Delayed neoling:of wowndsand swrgical incigiong. ·Glowcomo:may develop in swsceptible individwals after prolonged topucal therapy. · Growthretardation:inchildrenoccwrseven withsmaldogesif · given for long periods. CONTRAINDICATIONS: Peptic wlcer,Diabetes mellitws,Hypertengion,Vural and fwngal Twbercwlosis ond other infectuons,Ogteoporogus,Herpes gimplex keratitis Psycnogis,Epilepsy CHF,Renal fouwre. Pgychiatric distwrbances:mild ewpvoria freqwently accompanies high doge steroid treatment.Tnis may rarely progress to monic psychosus. Nervowsness,decreosed gleep and mood changes. unfectuong
  • 20.