Drugs acting on Endocrine system
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Dec 08, 2023
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About This Presentation
Drugs acting on Endocrine system
a) Chemistry, Nomenclature, Stereochemistry and metabolism of steroids
b) Sex hormones: Testosterone, Nandralone, Progestrones, Oestriol, Oestradiol, Oestrione, Diethyl stilbestrol.
c) Drugs for erectile dysfunction: Sildenafil, Tadalafil.
d) Oral contraceptives: Mi...
Slide Content
UNIT-IV 08 Hours
Drugs acting on Endocrine system
a) Chemistry, Nomenclature, Stereochemistry and metabolism of steroids
b) Sex hormones: Testosterone, Nandralone, Progestrones, Oestriol, Oestradiol, Oestrione, Diethyl stilbestrol.
c) Drugs for erectile dysfunction: Sildenafil, Tadalafil.
d) Oral contraceptives: Mifepristone, Norgestril, Levonorgestrol
e) Corticosteroids: Cortisone, Hydrocortisone, Prednisolone, Betamethasone, Dexamethasone
f) Thyroid and antithyroiddrugs: L-Thyroxine, L-Thyronine, Propylthiouracil, Methimazole
Drugs acting on Endocrine system
a) Chemistry, Nomenclature, Stereochemistry and metabolism of steroids
b) Sex hormones: Testosterone, Nandralone, Progestrones, Oestriol, Oestradiol, Oestrione, Diethyl stilbestrol.
c) Drugs for erectile dysfunction: Sildenafil, Tadalafil.
d) Oral contraceptives: Mifepristone, Norgestril, Levonorgestrol
e) Corticosteroids: Cortisone, Hydrocortisone, Prednisolone, Betamethasone, Dexamethasone
f) Thyroid and antithyroiddrugs: L-Thyroxine, L-Thyronine, Propylthiouracil, Methimazole
Endocrine system
•The endocrine system helps to maintain internal homeostasis
through the use of endogenous chemicals known as hormones.
•A hormone is typically regarded as a chemical messenger that is
released into the bloodstream to exert an effect on target cells
located some distance from the hormonal release site.
•Theendocrine system is a series of glands that produce
hormones which regulate respiration, metabolism, growth and
development, tissue function, sexual function, reproduction etc.
•Endocrine glands are ductless glands of the endocrine system
that secrete their products, hormones, directly into the blood.
•The major glands of the endocrine system include the pineal
gland, pituitary gland, pancreas, ovaries, testes, thyroid gland,
parathyroid gland, hypothalamus and adrenal glands
•The endocrine system helps to maintain internal homeostasis
through the use of endogenous chemicals known as hormones.
•A hormone is typically regarded as a chemical messenger that is
released into the bloodstream to exert an effect on target cells
located some distance from the hormonal release site.
•Theendocrine system is a series of glands that produce
hormones which regulate respiration, metabolism, growth and
development, tissue function, sexual function, reproduction etc.
•Endocrine glands are ductless glands of the endocrine system
that secrete their products, hormones, directly into the blood.
•The major glands of the endocrine system include the pineal
gland, pituitary gland, pancreas, ovaries, testes, thyroid gland,
parathyroid gland, hypothalamus and adrenal glands
Introduction to steroids
Steroids are the class of naturally occurring organic compounds with four rings arranged in a specific molecular
configuration.
Steroids exhibit two principal biological functions such as important components of cell membranes which alter
membrane fluidity and as signaling molecules.
Steroids are the class of naturally occurring organic compounds with four rings arranged in a specific molecular
configuration.
Steroids exhibit two principal biological functions such as important components of cell membranes which alter
membrane fluidity and as signaling molecules.
Nomenclature of steroids
Beginning in the 1950s, nomenclature rules for steroids were being developed, and the most recent IUPAC IUB
Joint Commission rules for systematic steroid nomenclature were published in 1989.
The steroid core structure is composed of seventeen carbon atoms (C17), bonded in four "fused" rings. Three six-
member cyclohexane rings (rings A, B and C in the first illustration) and one five-member cyclopentanering (the
D
ring).
Steroids vary by the functional groups attached to this four ring core and by the oxidation state of the rings.
Beginning in the 1950s, nomenclature rules for steroids were being developed, and the most recent IUPAC IUB
Joint Commission rules for systematic steroid nomenclature were published in 1989.
The steroid core structure is composed of seventeen carbon atoms (C17), bonded in four "fused" rings. Three six-
member cyclohexane rings (rings A, B and C in the first illustration) and one five-member cyclopentanering (the
D
ring).
Steroids vary by the functional groups attached to this four ring core and by the oxidation state of the rings.
Almost all steroids are named as derivatives of any one of the following basic steroidal ring.
Solid line indicates groups above the plane of the nucleus (β-configuration) and dotted line denote
groups below the plane (α-configuration).
The configuration of the hydrogen (-H) at C-5 position is always indicate in the name.
Compounds with 5-α cholestanebelong to the ‘alloseries’ while compounds derived from the 5-β-
cholestanebelongs to the ‘normal series’.
If the double bond is not between sequence numbered carbon, in that case both carbons are indicated in
the name.
The symbol Δ (delta) is used to indicate C=C bond in steroids.
When a methyl group is missing from the side chain, these are not indicated by the prefix ‘nor’ with the
number of the carbon atom which is disappear.
Solid line indicates groups above the plane of the nucleus (β-configuration) and dotted line denote
groups below the plane (α-configuration).
The configuration of the hydrogen (-H) at C-5 position is always indicate in the name.
Compounds with 5-α cholestanebelong to the ‘alloseries’ while compounds derived from the 5-β-
cholestanebelongs to the ‘normal series’.
If the double bond is not between sequence numbered carbon, in that case both carbons are indicated in
the name.
The symbol Δ (delta) is used to indicate C=C bond in steroids.
When a methyl group is missing from the side chain, these are not indicated by the prefix ‘nor’ with the
number of the carbon atom which is disappear.
Example:
Estrane: The hydrocarbon with a methyl group at C-13 but without a methyl group at C-10 and without a
side chain at C-17 is named as estrane(Fig. 4). E.g. 5 (α or β) estrane(C =18).
Estrane: The hydrocarbon with a methyl group at C-13 but without a methyl group at C-10 and without a
side chain at C-17 is named as estrane(Fig. 4). E.g. 5 (α or β) estrane(C =18).
Stereochemistry of steroids
There are six asymmetric carbon atoms 5,8,9,10,13,14 in the nucleus, therefore 64 optically active forms are
possible
Cholestane, androstaneand pregnaneexist in two conformations such as chair form and boat form.
Chair form is more stable then boat form due to less angle strength, therefore all cyclohexane ring in steroid
nucleus exist in the chair form
There are six asymmetric carbon atoms 5,8,9,10,13,14 in the nucleus, therefore 64 optically active forms are
possible
Cholestane, androstaneand pregnaneexist in two conformations such as chair form and boat form.
Chair form is more stable then boat form due to less angle strength, therefore all cyclohexane ring in steroid
nucleus exist in the chair form
The absolute stereochemistry of the molecule and any substituent is shown with solid bond
(β-configuration) and dotted bond (α-configuration)
(β-configuration) and dotted bond (α-configuration)
The aliphatic side chain at C-17position is always assumed to be β-configuration.
The term cisand transare sometimes used to indicate the backbone stereochemistry between the rings.
Example; 5-α-steroid are A/B Trans and 5-β-steroids are A/B Cis.
The term cisand transare sometimes used to indicate the backbone stereochemistry between the rings.
Example; 5-α-steroid are A/B Trans and 5-β-steroids are A/B Cis.
If A/B fusion cisand trans both position possible or position is unknown, it is indicated by waving lines/bonds
Steroids are primarily oxidized by cytochrome P450 oxidase enzymes, such as CYP3A4.
These reactions introduce oxygeninto the steroid ring, allowing the cholesterol to be broken up by other enzymes
into bile acids.
These acids can then be eliminated by secretion from the liver in bile.
The liver catalyzes extensive phase1and phase 2metabolisms of steroids, thereby regulating their activity and
clearance.
Hepatic phase 1metabolism of steroids includes the following types of reactions:
1) Reduction of a double bond at C-4and reduction of an oxo(keto) group at C-3to yield a secondary alcoholic
group.
2) Reduction of an oxogroup at C-20to yield a secondary alcoholic group.
3) Oxidation of a 17β-hydroxyl group.
4) Hydroxylation at various positions of the steroid nucleus ( e.g., 7-hydroxylation of 5α-reduced androgens).
5) Sulphateand/or glucuronideconjugation.
Metabolism of steroids
These reactions introduce oxygeninto the steroid ring, allowing the cholesterol to be broken up by other enzymes
into bile acids.
These acids can then be eliminated by secretion from the liver in bile.
The liver catalyzes extensive phase1and phase 2metabolisms of steroids, thereby regulating their activity and
clearance.
Hepatic phase 1metabolism of steroids includes the following types of reactions:
1) Reduction of a double bond at C-4and reduction of an oxo(keto) group at C-3to yield a secondary alcoholic
group.
2) Reduction of an oxogroup at C-20to yield a secondary alcoholic group.
3) Oxidation of a 17β-hydroxyl group.
4) Hydroxylation at various positions of the steroid nucleus ( e.g., 7-hydroxylation of 5α-reduced androgens).
5) Sulphateand/or glucuronideconjugation.
Metabolism of steroids
Sex hormones:
Sex hormones are steroid hormone (such as estrogen or testosterone) which are produced especially by the ovaries,
testes, or adrenal cortex and affects the growth or function of the reproductive organs or the development of
secondary sex characteristics.
Estrogens and progestinsare female sex hormones and androgens are male sex hormones.
These hormones are synthesized from cholesterol mainly in the gonads and adrenal cortex.
Classification
The sex hormones are classified as follows:
1) Androgens: This group of hormones affect the growth and development of the male reproductive system.
Androgens are divided into:
i) Naturally Occurring Androgens : Testosterone, Dihydrotestosterone, Dehydroepiandrosterone, and
Androsterone.
ii) Synthetic Androgens : Methyl testosterone, Fluoxymesterone, Testosterone undecanoate, and Mesterolone.
Sex hormones are steroid hormone (such as estrogen or testosterone) which are produced especially by the ovaries,
testes, or adrenal cortex and affects the growth or function of the reproductive organs or the development of
secondary sex characteristics.
Estrogens and progestinsare female sex hormones and androgens are male sex hormones.
These hormones are synthesized from cholesterol mainly in the gonads and adrenal cortex.
Classification
The sex hormones are classified as follows:
1) Androgens: This group of hormones affect the growth and development of the male reproductive system.
Androgens are divided into:
i) Naturally Occurring Androgens : Testosterone, Dihydrotestosterone, Dehydroepiandrosterone, and
Androsterone.
ii) Synthetic Androgens : Methyl testosterone, Fluoxymesterone, Testosterone undecanoate, and Mesterolone.
2) Oestrogens: These are the main female sex hormone s. Oestrogensare divided into:
i) Natural Oestrogens
a) Oestradiol(the most common type in women of child bearing age),
b) Oestrone(the only oestrogenbody makes after menopause), and
c) Oestriol(the main oestrogenduring pregnancy).
ii) Synthetic Oestrogens
a) Steroidal: Ethinylestradiol, Mestranol, and Tibolone.
b) Non-Steroidal: Diethylstilbestrol (stilbestrol), Hexestrol, and Dienestrol.
3) Progesterone: It is one of the hormones in the bodies which stimulates and regulates many functions. Progesterone is
divided into:
i) Natural Progestin: Progesterone
ii) Synthetic Progestins
a) Progesterone Derivatives
Older Compounds: Medroxyprogesteroneacetate (weak androgenic), Megestrolacetate, Dydrogesterone, and
Hydroxyprogesteronecaproate(long acting injection).
Newer Compound: Nomegestrolacetate.
b) 19-Nortestosterone Derivatives
Older Compounds: Norethindrone(Norethisterone), Norethynodrel, Ethynodioldiacetate, Lynestrenol(Ethinleystrenol),
Allylestrenol, Norgestrel(Gonane)a,nd Levonorgestrel.
Newer Compounds: Desogestrel, Norgestimate, and Gestodene.
i) Natural Oestrogens
a) Oestradiol(the most common type in women of child bearing age),
b) Oestrone(the only oestrogenbody makes after menopause), and
c) Oestriol(the main oestrogenduring pregnancy).
ii) Synthetic Oestrogens
a) Steroidal: Ethinylestradiol, Mestranol, and Tibolone.
b) Non-Steroidal: Diethylstilbestrol (stilbestrol), Hexestrol, and Dienestrol.
3) Progesterone: It is one of the hormones in the bodies which stimulates and regulates many functions. Progesterone is
divided into:
i) Natural Progestin: Progesterone
ii) Synthetic Progestins
a) Progesterone Derivatives
Older Compounds: Medroxyprogesteroneacetate (weak androgenic), Megestrolacetate, Dydrogesterone, and
Hydroxyprogesteronecaproate(long acting injection).
Newer Compound: Nomegestrolacetate.
b) 19-Nortestosterone Derivatives
Older Compounds: Norethindrone(Norethisterone), Norethynodrel, Ethynodioldiacetate, Lynestrenol(Ethinleystrenol),
Allylestrenol, Norgestrel(Gonane)a,nd Levonorgestrel.
Newer Compounds: Desogestrel, Norgestimate, and Gestodene.
Study of Individual Steroidal Drugs
1) Testosterone,
2) Nandrolone,
3) Progesterone,
4) Oestriol,
5) Oestradiol,
6) Oestrone, and
7) Diethylstilbestrol.
Testosterone
Testosterone is an androstanoidhaving 17 beta-hydroxyand 3-oxogroups, together with unsaturation at C-4-C-5.
It has a role as an androgen, a human metabolite, a Daphnia magna metabolite and a mouse metabolite.
It is a 17beta-hydroxysteroid, an androstanoid, a C19-steroid and a 3-oxo-Delta(4)steroid.
Testosterone is the primary male sex hormone and anabolic steroid.
In male humans, testosterone plays a key role in the development of male reproductive tissues such as testes and
prostate, as well as promoting secondary sexual characteristics such as increased muscle and bone mass, and the
growth of body hair.
1) Testosterone,
2) Nandrolone,
3) Progesterone,
4) Oestriol,
5) Oestradiol,
6) Oestrone, and
7) Diethylstilbestrol.
Testosterone
Testosterone is an androstanoidhaving 17 beta-hydroxyand 3-oxogroups, together with unsaturation at C-4-C-5.
It has a role as an androgen, a human metabolite, a Daphnia magna metabolite and a mouse metabolite.
It is a 17beta-hydroxysteroid, an androstanoid, a C19-steroid and a 3-oxo-Delta(4)steroid.
Testosterone is the primary male sex hormone and anabolic steroid.
In male humans, testosterone plays a key role in the development of male reproductive tissues such as testes and
prostate, as well as promoting secondary sexual characteristics such as increased muscle and bone mass, and the
growth of body hair.
IUPAC name is 17β-Hydroxyandrost-4-en-3-one
Mechanism of action
Testosterone antagonizes the androgen receptor to induce gene expression that causes the growth and
development of masculine sex organs and secondary sexual characteristics.
Mechanism of action
Testosterone antagonizes the androgen receptor to induce gene expression that causes the growth and
development of masculine sex organs and secondary sexual characteristics.
Uses
Testosterone is used primarily to treat symptoms of sexual dysfunction in men. Its potential
benefits include improved libido, increased bone mass, and increased sense of well-being
Adverse effect
Common side effects of testosterone include acne, swelling, and breast enlargement in men.
Serious side effects may include liver toxicity, heart disease, and behavioral changes.
Testosterone is used primarily to treat symptoms of sexual dysfunction in men. Its potential
benefits include improved libido, increased bone mass, and increased sense of well-being
Adverse effect
Common side effects of testosterone include acne, swelling, and breast enlargement in men.
Serious side effects may include liver toxicity, heart disease, and behavioral changes.
Nandroloneis a 3-oxo Delta(4)-steroid that is estr-4-en-3-one substituted by a beta-hydroxygroup at position 17.
It has a role as a human metabolite.
It is a 17beta-hydroxy steroid, a 3-oxo-Delta(4) steroid and an anabolic androgenic steroid.
It derives from a hydride of an estrane.
Nandrolone
17-hydroxy-13-methyl-2,6,7,8,9,10,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-one
It has a role as a human metabolite.
It is a 17beta-hydroxy steroid, a 3-oxo-Delta(4) steroid and an anabolic androgenic steroid.
It derives from a hydride of an estrane.
Nandrolone
17-hydroxy-13-methyl-2,6,7,8,9,10,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-one
Mechanism of action
Nandrolonebinds to the androgen receptor to a greater degree than testosterone, but due to its
inability to act
on the muscle in ways unmediated by the receptor, has less overall effect on muscle growth. It
is an androgen receptor agonist.
Uses
Nandroloneesters are used in the treatment of anemias, cachexia (wasting syndrome),
osteoporosis, breast cancer.
Adverse effect
Adverse effects of nandroloneesters include symptoms of masculinization like acne,
increased hair growth, voice changes etc.
Nandrolonebinds to the androgen receptor to a greater degree than testosterone, but due to its
inability to act
on the muscle in ways unmediated by the receptor, has less overall effect on muscle growth. It
is an androgen receptor agonist.
Uses
Nandroloneesters are used in the treatment of anemias, cachexia (wasting syndrome),
osteoporosis, breast cancer.
Adverse effect
Adverse effects of nandroloneesters include symptoms of masculinization like acne,
increased hair growth, voice changes etc.
Progesterones
Progesterone is a C21-steroid hormone in which apregnaneskeleton carries oxosubstituentsat
positions 3 and 20 and is unsaturated at C(4)-C(5).
As a hormone, it is involved in the female menstrual cycle, pregnancy and embryogenesis of humans
and other species.
It has a role as a contraceptive drug, a progestin, a progesterone receptor agonist, a human metabolite
and a mouse metabolite.
It is a 20-oxo steroid, a 3-oxo-Delta(4) steroid and a C21-steroid hormone.
It derives from ahydrideof apregnane.
17-acetyl-10,13-dimethyl-1,2,6,7,8,9,11,12,14,15,16,17-dodecahydrocyclopenta-
[a] phenanthren-3-one
Progesterone is a C21-steroid hormone in which apregnaneskeleton carries oxosubstituentsat
positions 3 and 20 and is unsaturated at C(4)-C(5).
As a hormone, it is involved in the female menstrual cycle, pregnancy and embryogenesis of humans
and other species.
It has a role as a contraceptive drug, a progestin, a progesterone receptor agonist, a human metabolite
and a mouse metabolite.
It is a 20-oxo steroid, a 3-oxo-Delta(4) steroid and a C21-steroid hormone.
It derives from ahydrideof apregnane.
17-acetyl-10,13-dimethyl-1,2,6,7,8,9,11,12,14,15,16,17-dodecahydrocyclopenta-
[a] phenanthren-3-one
Mechanism of action:
Progesterone converts the endometriumto its secretorystage to prepare the uterus for implantation.
At the same time progesterone affects the vaginal epithelium and cervical mucus, making it thick
and impenetrable to sperm.
Uses
Progesterone is used in combination with estrogens mainly in hormone therapy for menopausal
symptoms and low sex hormone levels in women. It is also used in women to support pregnancy
and fertility and to treat gynecological disorders.
Adverse effect
The commonly reported side effects of progesterone include abdominal cramps, depression,
dizziness, and headache. Other side effects include anxiety, cough, diarrhea, fatigue,
musculoskeletal pain, nausea, bloating, and irritability.
Progesterone converts the endometriumto its secretorystage to prepare the uterus for implantation.
At the same time progesterone affects the vaginal epithelium and cervical mucus, making it thick
and impenetrable to sperm.
Uses
Progesterone is used in combination with estrogens mainly in hormone therapy for menopausal
symptoms and low sex hormone levels in women. It is also used in women to support pregnancy
and fertility and to treat gynecological disorders.
Adverse effect
The commonly reported side effects of progesterone include abdominal cramps, depression,
dizziness, and headache. Other side effects include anxiety, cough, diarrhea, fatigue,
musculoskeletal pain, nausea, bloating, and irritability.
Oestriol
Estriolis the major estrogen involved in pregnancy and is produced naturally by the placenta and
fetus.
Estriolwas first discovered in 1930.
13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta [a]phenanthrene-3,16,17-triol
Estriolis the major estrogen involved in pregnancy and is produced naturally by the placenta and
fetus.
Estriolwas first discovered in 1930.
13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta [a]phenanthrene-3,16,17-triol
Mechanism of action
Estriolacts as an antagonist of the G-protein-coupled estrogen receptor (GPER), a membrane estrogen
receptor. Estriolhas been found to inhibit estradiol-induced proliferation of triple-negative breast
cancer cells through blockade of the GPER.
Uses
Estriolis used in menopausal hormone therapy to treat menopausal symptoms, such as hot flashes,
vulvovaginalatrophy, and dyspareunia.
Adverse effect
Estriolis well-tolerated and produces relatively few adverse effects. Side effects may include breast
tenderness, vaginal discomfort and discharge, and endometrial hyperplasia.
Estriolacts as an antagonist of the G-protein-coupled estrogen receptor (GPER), a membrane estrogen
receptor. Estriolhas been found to inhibit estradiol-induced proliferation of triple-negative breast
cancer cells through blockade of the GPER.
Uses
Estriolis used in menopausal hormone therapy to treat menopausal symptoms, such as hot flashes,
vulvovaginalatrophy, and dyspareunia.
Adverse effect
Estriolis well-tolerated and produces relatively few adverse effects. Side effects may include breast
tenderness, vaginal discomfort and discharge, and endometrial hyperplasia.
Oestradiol
•17beta-estradiol is the 17beta-isomer of estradiol. It has a role as an estrogen, a human metabolite, an
(aldehyde oxidase) inhibitor.
•It is a 17beta-hydroxy steroid and an estradiol.
•Estradiol or oestradiolis an estrogen steroid hormone and the major female sex hormone.
•It is also used to treat low estrogen levels in women with ovarian failure.
13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol
•17beta-estradiol is the 17beta-isomer of estradiol. It has a role as an estrogen, a human metabolite, an
(aldehyde oxidase) inhibitor.
•It is a 17beta-hydroxy steroid and an estradiol.
•Estradiol or oestradiolis an estrogen steroid hormone and the major female sex hormone.
•It is also used to treat low estrogen levels in women with ovarian failure.
13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol
Estradiol is a nuclear hormone as it acts on receptors present inside the cell that can activate or
deactivate transcription in the nucleus. Estradiol interacts with a target cell receptor (Erα or Erβ) within
the cytoplasm of the cell.
Uses
Estradiol is used to treat menopause symptoms such as hot flashes and vaginal changes, and to prevent
osteoporosis (bone loss) in menopausal women.
Estradiol is also used to treat low estrogen levels in women with ovarian failure.
It is also indicated to treat certain types of breast cancer and prostate cancer.
Mechanism of action
Adverse effect
Common side effects include headache, breast pain, irregular vaginal bleeding or spotting,
stomach/abdominal cramps, bloating, nausea and vomiting, and hair loss.
deactivate transcription in the nucleus. Estradiol interacts with a target cell receptor (Erα or Erβ) within
the cytoplasm of the cell.
Uses
Estradiol is used to treat menopause symptoms such as hot flashes and vaginal changes, and to prevent
osteoporosis (bone loss) in menopausal women.
Estradiol is also used to treat low estrogen levels in women with ovarian failure.
It is also indicated to treat certain types of breast cancer and prostate cancer.
Mechanism of action
Adverse effect
Common side effects include headache, breast pain, irregular vaginal bleeding or spotting,
stomach/abdominal cramps, bloating, nausea and vomiting, and hair loss.
Estroneis a 17-oxo steroid that is estra-1,3,5(10)-trienesubstituted by an hydroxygroup at position 3 and
an oxogroup at position 17.
It has a role as an estrogen, a bone density conservation agent, an antineoplastic agent, a human metabolite
and a mouse metabolite.
It is a 3-hydroxy steroid, a phenolic steroid, a member of phenols and a 17-oxo steroid.
It derives from a hydride of an estrane.
Oestrone
3-hydroxy-13-methyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-17-one
an oxogroup at position 17.
It has a role as an estrogen, a bone density conservation agent, an antineoplastic agent, a human metabolite
and a mouse metabolite.
It is a 3-hydroxy steroid, a phenolic steroid, a member of phenols and a 17-oxo steroid.
It derives from a hydride of an estrane.
Oestrone
3-hydroxy-13-methyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-17-one
Mechanism of action
It is specifically act as an agonist of the estrogen receptors ERα and ERβ.
Uses
Estronehas been available as an injected estrogen for medical use in hormone therapy for menopausal
symptoms.
Adverse effect
Common side effects include spotting, changes in vaginal discharge, abdominal pain or cramps,
bloating, nausea, vomiting and breast tenderness.
It is specifically act as an agonist of the estrogen receptors ERα and ERβ.
Uses
Estronehas been available as an injected estrogen for medical use in hormone therapy for menopausal
symptoms.
Adverse effect
Common side effects include spotting, changes in vaginal discharge, abdominal pain or cramps,
bloating, nausea, vomiting and breast tenderness.
Diethyl stilbestrol
Diethylstilbestrol is an olefiniccompound that is trans-hex-3-ene in which the hydrogensat positions 3 and 4
have been replaced by p-hydroxyphenylgroups.
It is a polyphenol and an olefiniccompound.
Diethylstilbestrol is also known as stilbestrolor stilboestrol.
It is a synthetic, nonsteroidalestrogen medication.
It was first marketed for medical use in 1939. It was approved by the United States Food and
Drug Administration (FDA) on September 19, 1941 in tablets formulation up to 5 mg for four indications
such as gonorrheal vaginitis, atrophic vaginitis, menopausal symptoms, and postpartum lactation suppression
to prevent breast engorgement.
4-[(E)-4-(4-hydroxyphenyl)hex-3-en-3-yl]phenol
Diethylstilbestrol is an olefiniccompound that is trans-hex-3-ene in which the hydrogensat positions 3 and 4
have been replaced by p-hydroxyphenylgroups.
It is a polyphenol and an olefiniccompound.
Diethylstilbestrol is also known as stilbestrolor stilboestrol.
It is a synthetic, nonsteroidalestrogen medication.
It was first marketed for medical use in 1939. It was approved by the United States Food and
Drug Administration (FDA) on September 19, 1941 in tablets formulation up to 5 mg for four indications
such as gonorrheal vaginitis, atrophic vaginitis, menopausal symptoms, and postpartum lactation suppression
to prevent breast engorgement.
4-[(E)-4-(4-hydroxyphenyl)hex-3-en-3-yl]phenol
Mechanism of action
Diethylstilbestrol inhibits the hypothalamic-pituitary-gonadal axis, thereby blocking the testicular synthesis
of testosterone, lowering plasma testosterone, and inducing a chemical castration.
Uses:
Diethylstilbestrol is only used in the treatment of prostate cancer and less commonly breast cancer.
It is also used in the treatment of prostate cancer in men.
It has a role as an antineoplastic agent, a carcinogenic agent, an antifungal agent, and a calcium channel
blocker.
Adverse effect:
It is associated with high rates of side effects including nausea, vomiting, abdominal discomfort, headache,
and bloating.
Diethylstilbestrol inhibits the hypothalamic-pituitary-gonadal axis, thereby blocking the testicular synthesis
of testosterone, lowering plasma testosterone, and inducing a chemical castration.
Uses:
Diethylstilbestrol is only used in the treatment of prostate cancer and less commonly breast cancer.
It is also used in the treatment of prostate cancer in men.
It has a role as an antineoplastic agent, a carcinogenic agent, an antifungal agent, and a calcium channel
blocker.
Adverse effect:
It is associated with high rates of side effects including nausea, vomiting, abdominal discomfort, headache,
and bloating.
Drugs for erectile dysfunction
Erectile dysfunction (ED) is the inability to get or keep an erection firm enough to have sexual intercourse.
It is sometimes referred as impotence.
Many men experience it during the time of stress.
Patients suffering from erectile dysfunction should first be evaluated for any underlying physical and
psychological conditions.
Erectile dysfunction (ED) is the inability to get or keep an erection firm enough to have sexual intercourse.
It is sometimes referred as impotence.
Many men experience it during the time of stress.
Patients suffering from erectile dysfunction should first be evaluated for any underlying physical and
psychological conditions.
5-[2-ethoxy-5-(4-methylpiperazin-1-yl)sulfonylphenyl]-1-methyl-3-propyl-6H-pyrazolo[4,3-d]pyrimidin-7-one
Sildenafil
Sildenafil is apyrazolo[4,3-d]pyrimidin-7-onehaving amethylsubstituent at the 1-position, a propyl
substituent at the 3-position and a 2-ethoxy-5-[(4-methylpiperazin-1-yl)sulfonyl]phenyl group at the 5-
position. It has a role as a vasodilator agent and (3',5'-cyclic-GMPphosphodiesterase) inhibitor.
It is a pyrazolopyrimidine, a member of piperazinesand a sulfonamide.
Sildenafil is sold under the brand name Viagra.
This medication is most effective when taken on an empty stomach one hour before sex. It is taken by mouth or
injection into a vein.
Sildenafil
Sildenafil is apyrazolo[4,3-d]pyrimidin-7-onehaving amethylsubstituent at the 1-position, a propyl
substituent at the 3-position and a 2-ethoxy-5-[(4-methylpiperazin-1-yl)sulfonyl]phenyl group at the 5-
position. It has a role as a vasodilator agent and (3',5'-cyclic-GMPphosphodiesterase) inhibitor.
It is a pyrazolopyrimidine, a member of piperazinesand a sulfonamide.
Sildenafil is sold under the brand name Viagra.
This medication is most effective when taken on an empty stomach one hour before sex. It is taken by mouth or
injection into a vein.
Mechanism of action
Sildenafil acts by blocking phosphodiesterase-5 (PDE5), an enzyme that promotes breakdown of cyclic
guanosinemonophosphate (cGMP), which regulates blood flow in the penis.
Uses:
Sildenafil is used to treat male sexual function problems (impotence or erectile dysfunction-ED).
Adverse effect
Dizziness, headache, flushing, or stomach upset may occur. Vision changes such as increased sensitivity
to light, blurred vision, or trouble telling blue and green colors apart may also occur.
Sildenafil acts by blocking phosphodiesterase-5 (PDE5), an enzyme that promotes breakdown of cyclic
guanosinemonophosphate (cGMP), which regulates blood flow in the penis.
Uses:
Sildenafil is used to treat male sexual function problems (impotence or erectile dysfunction-ED).
Adverse effect
Dizziness, headache, flushing, or stomach upset may occur. Vision changes such as increased sensitivity
to light, blurred vision, or trouble telling blue and green colors apart may also occur.
Tadalafil
Tadalafilis apyrazinopyridoindolethat is2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-
1,4-dionesubstituted at position 2 by amethylgroup and at position 6 by a 1,3-benzodioxol-5-yl group (the
6R,12aR-diastereomer).
Tadalafilis an orally administered drug used to treat male sexual function problems (impotence or erectile
dysfunction-ED). Tadalafilis sold under the brand name Cialis. It is a pyrazinopyridoindolederivative.
2-(1,3-benzodioxol-5-yl)-6-methyl-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraene-4,7-dione
Tadalafilis apyrazinopyridoindolethat is2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-
1,4-dionesubstituted at position 2 by amethylgroup and at position 6 by a 1,3-benzodioxol-5-yl group (the
6R,12aR-diastereomer).
Tadalafilis an orally administered drug used to treat male sexual function problems (impotence or erectile
dysfunction-ED). Tadalafilis sold under the brand name Cialis. It is a pyrazinopyridoindolederivative.
2-(1,3-benzodioxol-5-yl)-6-methyl-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraene-4,7-dione
Mechanism of action
It is a phosphodiesterase-5 (PDE5) inhibitor. It works by increasing blood flow to the penis to help a man get
and keep an erection.
Uses:
It is used to treat erection problems (erectile dysfunction) and symptoms of an enlarged prostate
(benign prostate enlargement). It's also sometimes used to treat pulmonary hypertension (high blood pressure
in the blood vessels that supply the lungs).
Adverse effect:
Headache, stomach upset, back pain, muscle pain, stuffy nose, flushing, or dizziness may occur.
It is a phosphodiesterase-5 (PDE5) inhibitor. It works by increasing blood flow to the penis to help a man get
and keep an erection.
Uses:
It is used to treat erection problems (erectile dysfunction) and symptoms of an enlarged prostate
(benign prostate enlargement). It's also sometimes used to treat pulmonary hypertension (high blood pressure
in the blood vessels that supply the lungs).
Adverse effect:
Headache, stomach upset, back pain, muscle pain, stuffy nose, flushing, or dizziness may occur.
Oral contraceptives
Oral contraceptives (OCPs) are also known as birth control pills.
Theaseare medications taken by mouth for the purpose of birth control.
There are various types of female oral contraceptive pill.
Example:combined oral contraceptive pill contains estrogen and a progestin, progestogen-only pill and
Ormeloxifeneis a selective estrogen receptor modulator which offers the benefit of only having to be taken once a
week.
Sometimes, emergency contraception pills are taken at the time of intercourse, or within a few days
afterwards. Example:Levonorgestrel, sold under the brand name Plan B, Ulipristalacetate, Mifepristone and
misoprostol, when used in combination, are more than 95% effective during the first 50 days of pregnancy.
Oral contraceptives (OCPs) are also known as birth control pills.
Theaseare medications taken by mouth for the purpose of birth control.
There are various types of female oral contraceptive pill.
Example:combined oral contraceptive pill contains estrogen and a progestin, progestogen-only pill and
Ormeloxifeneis a selective estrogen receptor modulator which offers the benefit of only having to be taken once a
week.
Sometimes, emergency contraception pills are taken at the time of intercourse, or within a few days
afterwards. Example:Levonorgestrel, sold under the brand name Plan B, Ulipristalacetate, Mifepristone and
misoprostol, when used in combination, are more than 95% effective during the first 50 days of pregnancy.
Mifepristone
Mifepristone is a 3-oxo-Delta(4) steroid, an acetyleniccompound and a tertiaryaminocompound.
It has a role as an abortifacient, a contraceptive drug, a synthetic oral contraceptive and a hormone antagonist.
It derives from ahydrideof anestrane.
Mifepristone is a synthetic steroid and also known as RU-486.
It is a medication mainly used in combination with misoprostol to bring about an abortion during pregnancy.
11-[4-(dimethylamino)phenyl]-17-hydroxy-13-methyl-17-prop-1-ynyl-1,2,6,7,8,11,12,14,15,16
decahydrocyclopenta[a]phenanthren-3-one
Mifepristone is a 3-oxo-Delta(4) steroid, an acetyleniccompound and a tertiaryaminocompound.
It has a role as an abortifacient, a contraceptive drug, a synthetic oral contraceptive and a hormone antagonist.
It derives from ahydrideof anestrane.
Mifepristone is a synthetic steroid and also known as RU-486.
It is a medication mainly used in combination with misoprostol to bring about an abortion during pregnancy.
11-[4-(dimethylamino)phenyl]-17-hydroxy-13-methyl-17-prop-1-ynyl-1,2,6,7,8,11,12,14,15,16
decahydrocyclopenta[a]phenanthren-3-one
Mechanism of action
Mifepristone is an anti-progestin that blocks the action of progesterone, a hormone necessary to maintain a
pregnancy. By blocking the action of progesterone, mifepristone alters the endometrium (the uterine lining),
induces bleeding, and causes the uterine lining to shed.
Uses:
Mifepristone is used in combination with misoprostol (Cytotec) to end an early pregnancy.
Adverse effect:
Nausea, vomiting, diarrhea, weakness, or dizziness may occur. Bleeding and cramping are expected during
this treatment.
Mifepristone is an anti-progestin that blocks the action of progesterone, a hormone necessary to maintain a
pregnancy. By blocking the action of progesterone, mifepristone alters the endometrium (the uterine lining),
induces bleeding, and causes the uterine lining to shed.
Uses:
Mifepristone is used in combination with misoprostol (Cytotec) to end an early pregnancy.
Adverse effect:
Nausea, vomiting, diarrhea, weakness, or dizziness may occur. Bleeding and cramping are expected during
this treatment.
Norgestril
Norgestrelis a form of progestin hormone that prevents pregnancy. Chemically, it is also known as rac-13-
ethyl-17α-ethynyl-19-nortestosterone or rac-13-ethyl-17α-ethynylestr-4-en-17β-ol-3-one
Norgestrelis a form of progestin hormone that prevents pregnancy. Chemically, it is also known as rac-13-
ethyl-17α-ethynyl-19-nortestosterone or rac-13-ethyl-17α-ethynylestr-4-en-17β-ol-3-one
Mechanism of action
It binds to the progesterone and estrogen receptors within the female reproductive tract and the mammary
gland.
Uses: It is a hormone that prevents pregnancy by making vaginal fluid thicker to help prevent sperm from
reaching an egg (fertilization), and changing the lining of the uterus (womb) to prevent attachment of a
fertilized egg.
Adverse effect
Nausea, vomiting, stomach cramping/bloating, dizziness, headache, tiredness, breast tenderness, decrease in
breast size, acne, oily scalp, hair loss, weight gain, and vaginal infections may occur.
It binds to the progesterone and estrogen receptors within the female reproductive tract and the mammary
gland.
Uses: It is a hormone that prevents pregnancy by making vaginal fluid thicker to help prevent sperm from
reaching an egg (fertilization), and changing the lining of the uterus (womb) to prevent attachment of a
fertilized egg.
Adverse effect
Nausea, vomiting, stomach cramping/bloating, dizziness, headache, tiredness, breast tenderness, decrease in
breast size, acne, oily scalp, hair loss, weight gain, and vaginal infections may occur.
Levonorgestrol
Levonorgestrelis a 17beta-hydroxy steroid, a 3-oxo-Delta(4) steroid and a terminal acetyleniccompound.
It has a role as a contraceptive drug, a progestin, a synthetic oral contraceptive and a female contraceptive drug.
It derives from anorgestrel. It is an enantiomer of a dexonorgestrel.
Levonorgestrel(LNG) is a synthetic estranesteroid and a derivative of testosterone.
13-ethyl-17-ethynyl-17-hydroxy-1,2,6,7,8,9,10,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-3-one
Levonorgestrelis a 17beta-hydroxy steroid, a 3-oxo-Delta(4) steroid and a terminal acetyleniccompound.
It has a role as a contraceptive drug, a progestin, a synthetic oral contraceptive and a female contraceptive drug.
It derives from anorgestrel. It is an enantiomer of a dexonorgestrel.
Levonorgestrel(LNG) is a synthetic estranesteroid and a derivative of testosterone.
13-ethyl-17-ethynyl-17-hydroxy-1,2,6,7,8,9,10,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-3-one
Mechanism of action:
It prevents fertilization by inhibiting the ovulation and thickening of cervical mucus.
Uses: Levonorgestrelis used to prevent pregnancy after unprotected sexual intercourse.
Adverse effect
Nausea, vomiting, abdominal pain, tiredness, dizziness, changes in vaginal bleeding, breast tenderness,
diarrhea, or headache may occur.
It prevents fertilization by inhibiting the ovulation and thickening of cervical mucus.
Uses: Levonorgestrelis used to prevent pregnancy after unprotected sexual intercourse.
Adverse effect
Nausea, vomiting, abdominal pain, tiredness, dizziness, changes in vaginal bleeding, breast tenderness,
diarrhea, or headache may occur.
Corticosteroids
Corticosteroids are the class of steroid hormones (C21).
These are produced in the adrenal cortex.
These are the class of drugs that lower the inflammation in the body.
They also reduce the activity of immune system.
Corticosteroids are the class of steroid hormones (C21).
These are produced in the adrenal cortex.
These are the class of drugs that lower the inflammation in the body.
They also reduce the activity of immune system.
Cortisone
Cortisone is a C21-steroid that is pregn-4-ene substituted by hydroxygroups at positions 17 and 21
and oxogroup at positions 3, 11 and 20.
It has a role as a human metabolite and a mouse metabolite.
It is a 17alpha-hydroxy steroid, a 21-hydroxy steroid, an 11-oxo steroid, a 20-oxo steroid, a C21-steroid,
a 3-oxo-Delta(4) steroid, a primary alpha-hydroxyketone, a tertiary alpha-hydroxyketoneand a
glucocorticoid.
It derives from a hydrideof a pregnane.
17-hydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl-1,2,6,7,8,9,12,14,15,16-decahydrocyclopenta[a]phenanthrene-3,11-dione
Cortisone is a C21-steroid that is pregn-4-ene substituted by hydroxygroups at positions 17 and 21
and oxogroup at positions 3, 11 and 20.
It has a role as a human metabolite and a mouse metabolite.
It is a 17alpha-hydroxy steroid, a 21-hydroxy steroid, an 11-oxo steroid, a 20-oxo steroid, a C21-steroid,
a 3-oxo-Delta(4) steroid, a primary alpha-hydroxyketone, a tertiary alpha-hydroxyketoneand a
glucocorticoid.
It derives from a hydrideof a pregnane.
17-hydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl-1,2,6,7,8,9,12,14,15,16-decahydrocyclopenta[a]phenanthrene-3,11-dione
Mechanism of action
Cortisone acetate binds to the cytosolicglucocorticoidreceptor. After binding the receptor
the newly formed receptor-ligandcomplex translocatesitself into the cell nucleus, where it
binds to many glucocorticoidresponse elements (GRE) in the promoter region of the target
genes.
Uses:Cortisone is used as an anti-inflammatory medication.
Adverse effect: Fluid retention, causing swelling in lower legs. Problems with mood swings,
memory and behavior and other psychological effects, such as confusion or delirium.
Cortisone acetate binds to the cytosolicglucocorticoidreceptor. After binding the receptor
the newly formed receptor-ligandcomplex translocatesitself into the cell nucleus, where it
binds to many glucocorticoidresponse elements (GRE) in the promoter region of the target
genes.
Uses:Cortisone is used as an anti-inflammatory medication.
Adverse effect: Fluid retention, causing swelling in lower legs. Problems with mood swings,
memory and behavior and other psychological effects, such as confusion or delirium.
Hydrocortisone
Hydrocortisone, or cortisol, is a glucocorticoidsecreted by the adrenal cortex.
Hydrocortisone is used to treat immune, inflammatory, and neoplasticconditions.
It was discovered in the 1930s by Edward Kendall and named Compound F, or 17-
hydroxycorticosterone.
Hydrocortisone was granted FDA approval on 5 August 1952.
11,17-dihydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthren-
3-one
Hydrocortisone, or cortisol, is a glucocorticoidsecreted by the adrenal cortex.
Hydrocortisone is used to treat immune, inflammatory, and neoplasticconditions.
It was discovered in the 1930s by Edward Kendall and named Compound F, or 17-
hydroxycorticosterone.
Hydrocortisone was granted FDA approval on 5 August 1952.
11,17-dihydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthren-
3-one
Mechanism of action
Hydrocortisone binds to the glucocorticoidreceptor leading to downstream effects such as
inhibition of phospholipaseA2, NF-kappa-B, other inflammatory transcription factors, and the
promotion of antiinflammatorygenes.
Uses:
Hydrocortisone topical is used to treat redness, swelling, itching, and discomfort of various
skin conditions.
Adverse effect:
Nausea, heartburn, headache, dizziness, menstrual period changes, trouble sleeping,
increased sweating, or acne may occur.
Hydrocortisone binds to the glucocorticoidreceptor leading to downstream effects such as
inhibition of phospholipaseA2, NF-kappa-B, other inflammatory transcription factors, and the
promotion of antiinflammatorygenes.
Uses:
Hydrocortisone topical is used to treat redness, swelling, itching, and discomfort of various
skin conditions.
Adverse effect:
Nausea, heartburn, headache, dizziness, menstrual period changes, trouble sleeping,
increased sweating, or acne may occur.
Prednisolone
Prednisoloneis a glucocorticoidthat isprednisonein which the oxogroup at position 11 has been
reduced to the corresponding beta-hydroxygroup.
It is a drug metabolite ofprednisone. It has a role as an adrenergic agent, an anti-inflammatory drug,
an antineoplasticagent, an immunosuppressive agent, a drug metabolite, an environmental
contaminant and a xenobiotic.
It is a glucocorticoid, an 11beta-hydroxy steroid, a 21-hydroxy steroid, a 17alpha-hydroxy steroid, a
20-oxo steroid, a 3-oxo-Delta(1),Delta(4)-steroid, a primary alpha-hydroxyketone, a tertiary alpha-
hydroxyketoneand a C21-steroid.
It derives from aDelta(1)-progesterone.
11,17-dihydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-3-one
Prednisoloneis a glucocorticoidthat isprednisonein which the oxogroup at position 11 has been
reduced to the corresponding beta-hydroxygroup.
It is a drug metabolite ofprednisone. It has a role as an adrenergic agent, an anti-inflammatory drug,
an antineoplasticagent, an immunosuppressive agent, a drug metabolite, an environmental
contaminant and a xenobiotic.
It is a glucocorticoid, an 11beta-hydroxy steroid, a 21-hydroxy steroid, a 17alpha-hydroxy steroid, a
20-oxo steroid, a 3-oxo-Delta(1),Delta(4)-steroid, a primary alpha-hydroxyketone, a tertiary alpha-
hydroxyketoneand a C21-steroid.
It derives from aDelta(1)-progesterone.
11,17-dihydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-3-one
Mechanism of action
It decreases the inflammation via suppression of the migration of polymorphonuclear
leukocytes and reversing increased capillary permeability.
Uses
Prednisoloneis used to treat allergies, blood disorders, skin diseases, infections, certain
cancers.
It is also used to prevent organ rejection after a transplant.
It helps to reduce inflammation.
Adverse effect:
Nausea, heartburn, headache, dizziness, menstrual period changes, trouble sleeping,
increased sweating, or acne may occur.
It decreases the inflammation via suppression of the migration of polymorphonuclear
leukocytes and reversing increased capillary permeability.
Uses
Prednisoloneis used to treat allergies, blood disorders, skin diseases, infections, certain
cancers.
It is also used to prevent organ rejection after a transplant.
It helps to reduce inflammation.
Adverse effect:
Nausea, heartburn, headache, dizziness, menstrual period changes, trouble sleeping,
increased sweating, or acne may occur.
Betamethasone
Betamethasoneis a glucocorticoid, a 20-oxo steroid, a 21-hydroxy steroid, a 17alpha-hydroxy steroid,
a fluorinated steroid, an 11beta-hydroxy steroid, a 3-oxo-Delta(1),Delta(4)-steroid, a primary alpha-
hydroxyketoneand a tertiary alpha-hydroxyketone.
It has a role as an anti-inflammatory drug, an anti-asthmatic agent and an immunosuppressive
agent. It derives from ahydrideof apregnane.
Betamethasoneis a glucocorticoid, a 20-oxo steroid, a 21-hydroxy steroid, a 17alpha-hydroxy steroid,
a fluorinated steroid, an 11beta-hydroxy steroid, a 3-oxo-Delta(1),Delta(4)-steroid, a primary alpha-
hydroxyketoneand a tertiary alpha-hydroxyketone.
It has a role as an anti-inflammatory drug, an anti-asthmatic agent and an immunosuppressive
agent. It derives from ahydrideof apregnane.
Mechanism of action
Betamethasonebinds to specific intracellular glucocorticoidreceptors and subsequently
binds to DNA to modify gene expression. The synthesis of certain anti-inflammatory
proteins is induced while the synthesis of certain inflammatory mediators is inhibited.
Uses:
Betamethasoneis used topically to treat itching, redness, dryness, crusting, scaling,
inflammation, and discomfort of various skin conditions, including psoriasis and eczema.
Adverse effect:
Common side effects of betamethasoneinclude abdominal bloating, abdominal fat
deposits, abnormal hair growth.
Betamethasonebinds to specific intracellular glucocorticoidreceptors and subsequently
binds to DNA to modify gene expression. The synthesis of certain anti-inflammatory
proteins is induced while the synthesis of certain inflammatory mediators is inhibited.
Uses:
Betamethasoneis used topically to treat itching, redness, dryness, crusting, scaling,
inflammation, and discomfort of various skin conditions, including psoriasis and eczema.
Adverse effect:
Common side effects of betamethasoneinclude abdominal bloating, abdominal fat
deposits, abnormal hair growth.
Dexamethasone
Dexamethasoneis a fluorinated steroid that is 9-fluoropregna-1,4-diene substituted byhydroxygroups
at positions 11, 17 and 21, amethylgroup at position 16 and oxogroups at positions 3 and 20.
It is a synthetic member of the class of glucocorticoids. It has a role as an adrenergic agent, an
antiemetic, an antineoplasticagent, an environmental contaminant, a xenobiotic, an
immunosuppressive agent and an anti-inflammatory drug.
It is a fluorinated steroid, a 3-oxo-Delta(1),Delta(4)-steroid, a glucocorticoid, a 20-oxo steroid, an
11beta-hydroxy steroid, a 17alpha-hydroxy steroid and a 21-hydroxy steroid.
It derives from ahydrideof apregnane.
9-fluoro-11,17-dihydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-
3-one
Dexamethasoneis a fluorinated steroid that is 9-fluoropregna-1,4-diene substituted byhydroxygroups
at positions 11, 17 and 21, amethylgroup at position 16 and oxogroups at positions 3 and 20.
It is a synthetic member of the class of glucocorticoids. It has a role as an adrenergic agent, an
antiemetic, an antineoplasticagent, an environmental contaminant, a xenobiotic, an
immunosuppressive agent and an anti-inflammatory drug.
It is a fluorinated steroid, a 3-oxo-Delta(1),Delta(4)-steroid, a glucocorticoid, a 20-oxo steroid, an
11beta-hydroxy steroid, a 17alpha-hydroxy steroid and a 21-hydroxy steroid.
It derives from ahydrideof apregnane.
9-fluoro-11,17-dihydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-
3-one
Mechanism of action
It inhibits phospholipaseA2, which decreases the formation of arachidonicacid derivatives.
It inhibits NF-Kappa B and other inflammatory transcription factors.
It promotes anti-inflammatory genes like interleukin-10
Uses:
It relieves inflammation (swelling, heat, redness, and pain) and is used to treat certain forms
of arthritis.
Adverse effect:
Increased appetite.
Irritability.
Difficulty sleeping (insomnia)
Swelling in your ankles and feet (fluid retention)
Heartburn.
Muscle weakness.
Impaired wound healing.
Increased blood sugar levels.
It inhibits phospholipaseA2, which decreases the formation of arachidonicacid derivatives.
It inhibits NF-Kappa B and other inflammatory transcription factors.
It promotes anti-inflammatory genes like interleukin-10
Uses:
It relieves inflammation (swelling, heat, redness, and pain) and is used to treat certain forms
of arthritis.
Adverse effect:
Increased appetite.
Irritability.
Difficulty sleeping (insomnia)
Swelling in your ankles and feet (fluid retention)
Heartburn.
Muscle weakness.
Impaired wound healing.
Increased blood sugar levels.
Thyroid and antithyroiddrugs
The thyroid is a butterfly-shaped gland that sits low on the front of the neck. Thyroid has two side
lobes, connected by a bridge (isthmus) in the middle.
The thyroid gland consists of 2 types of cells.
Follicular cells: These are more abundant, and the major secretorycells. They secrete Thyroid
hormone.
Parafollicularcells or C-cells: These are fewer in number & interspersed. They secrete Calcitonin.
The thyroid is a butterfly-shaped gland that sits low on the front of the neck. Thyroid has two side
lobes, connected by a bridge (isthmus) in the middle.
The thyroid gland consists of 2 types of cells.
Follicular cells: These are more abundant, and the major secretorycells. They secrete Thyroid
hormone.
Parafollicularcells or C-cells: These are fewer in number & interspersed. They secrete Calcitonin.
There are two types of thyroid hormones produced and released by the thyroid gland namely
triiodothyronine(T3) and thyroxine(T4).
There are presences of 3 and 4 atoms of iodine in T3 and T4 respectively.
The deficiency of iodine leads to decreased production of T3 and T4 that enlarges the thyroid
tissue and will cause the disease known as simple goitre.
Both T3 and T4 are used to treat thyroid hormone deficiency (hypothyroidism).
triiodothyronine(T3) and thyroxine(T4).
There are presences of 3 and 4 atoms of iodine in T3 and T4 respectively.
The deficiency of iodine leads to decreased production of T3 and T4 that enlarges the thyroid
tissue and will cause the disease known as simple goitre.
Both T3 and T4 are used to treat thyroid hormone deficiency (hypothyroidism).
L-Thyroxine
Levothyroxineis a synthetic levoisomerof thyroxine(T4), similar to the endogenous hormone
produced by the thyroid gland.
Thyroxineis de-iodinated to formtriiodothyronine(T3) in the peripheral tissues.
T3 enters the cell and binds to nuclear thyroid hormone receptors, and the hormone-receptor
complex in turn triggers gene expression and produces proteins required in the regulation of cellular
respiration, thermogenesis, cellular growth and differentiation, and metabolism of proteins,
carbohydrates and lipids.
T4 and T3 also possess cardiac stimulatory effect.
2-amino-3-[4-(4-hydroxy-3,5-diiodophenoxy)-3,5-diiodophenyl]propanoicacid
Levothyroxineis a synthetic levoisomerof thyroxine(T4), similar to the endogenous hormone
produced by the thyroid gland.
Thyroxineis de-iodinated to formtriiodothyronine(T3) in the peripheral tissues.
T3 enters the cell and binds to nuclear thyroid hormone receptors, and the hormone-receptor
complex in turn triggers gene expression and produces proteins required in the regulation of cellular
respiration, thermogenesis, cellular growth and differentiation, and metabolism of proteins,
carbohydrates and lipids.
T4 and T3 also possess cardiac stimulatory effect.
2-amino-3-[4-(4-hydroxy-3,5-diiodophenoxy)-3,5-diiodophenyl]propanoicacid
Mechanism of Action:
Thyroxinestimulates oxygen utilization and heat production of body cells. It causes
increased utilization of carbohydrates, increased protein catabolism, as indicated by a
greater excretion of nitrogen, and greater oxidation of fats as suggested by loss in body
weight.
Uses:
Levothyroxineis used to treat an underactive thyroid (hypothyroidism).
Adverse effect:
If the levothyroxinedoses are too high that cause symptoms such as hyperthyroidism,
tachycardia, dysrhythmias, tremor, nervousness, insomnia, diarrhea, weight loss, sweating,
heat sensations, fever, decreased glucose tolerance.
Thyroxinestimulates oxygen utilization and heat production of body cells. It causes
increased utilization of carbohydrates, increased protein catabolism, as indicated by a
greater excretion of nitrogen, and greater oxidation of fats as suggested by loss in body
weight.
Uses:
Levothyroxineis used to treat an underactive thyroid (hypothyroidism).
Adverse effect:
If the levothyroxinedoses are too high that cause symptoms such as hyperthyroidism,
tachycardia, dysrhythmias, tremor, nervousness, insomnia, diarrhea, weight loss, sweating,
heat sensations, fever, decreased glucose tolerance.
L-Thyronine
Thyronineis a deiodinatedform of thyroxine.
A group of metabolites derived from THYROXINE and TRIIODOTHYRONINE via the peripheral
enzymatic removal of iodinesfrom the thyroxinenucleus.
Thyronineis the thyroxinenucleus devoid of its four iodine atoms.
IUPAC Name is (2S)-2-amino-3-[4-(4-hydroxyphenoxy)phenyl]propanoicacid
Uses:
It is to treat thyroid hormone
deficiency (hypothyroidism).
Thyronineis a deiodinatedform of thyroxine.
A group of metabolites derived from THYROXINE and TRIIODOTHYRONINE via the peripheral
enzymatic removal of iodinesfrom the thyroxinenucleus.
Thyronineis the thyroxinenucleus devoid of its four iodine atoms.
IUPAC Name is (2S)-2-amino-3-[4-(4-hydroxyphenoxy)phenyl]propanoicacid
Uses:
It is to treat thyroid hormone
deficiency (hypothyroidism).
Propylthiouracil
Propylthiouracilis athioureaderivative with antithyroidproperty.
Propylthiouracil(PTU) interferes with the oxidation ofiodinepossibly by interaction with peroxidaseor a
peroxidase-mediated complex reaction, thereby inhibiting synthesis of thyroid hormones tri-
iodothyronine(T3) andthyroxine(T4).
In addition, this agent inhibits the Type I 5'-deiodinase (D1), an enzyme involved in the peripheral
conversion ofthyroxineto tri-iodothyronine.
This results in decreased plasma triodothyronineconcentrations and decreased entrance
ofthyroxineinto cells thereby reducing thyroid hormone activity.
6-propyl-2-sulfanylidene-1H-pyrimidin-4-one
Propylthiouracilis athioureaderivative with antithyroidproperty.
Propylthiouracil(PTU) interferes with the oxidation ofiodinepossibly by interaction with peroxidaseor a
peroxidase-mediated complex reaction, thereby inhibiting synthesis of thyroid hormones tri-
iodothyronine(T3) andthyroxine(T4).
In addition, this agent inhibits the Type I 5'-deiodinase (D1), an enzyme involved in the peripheral
conversion ofthyroxineto tri-iodothyronine.
This results in decreased plasma triodothyronineconcentrations and decreased entrance
ofthyroxineinto cells thereby reducing thyroid hormone activity.
6-propyl-2-sulfanylidene-1H-pyrimidin-4-one
Mechanism of action
Propylthiouracilbinds to thyroid peroxidaseand thereby inhibits the conversion of iodide to
iodine. Thyroid peroxidasenormally converts iodide to iodine (via hydrogen peroxide as a
cofactor) and also catalyzes the incorporation of the resulting iodide molecule onto both the 3
and/or 5 positions of the phenol rings of tyrosinesfound in thyroglobulin. Thyroglobulinis
degraded to produce thyroxine(T4) and tri-iodothyronine(T3), which are the main hormones
produced by the thyroid gland. Therefore propylthiouracileffectively inhibits the production of
new thyroid hormones.
Uses:
Propylthiouracilis used to treat overactive thyroid (hyperthyroidism). It works by stopping the
thyroid gland from making too much thyroid hormone.
Propylthiouracilbinds to thyroid peroxidaseand thereby inhibits the conversion of iodide to
iodine. Thyroid peroxidasenormally converts iodide to iodine (via hydrogen peroxide as a
cofactor) and also catalyzes the incorporation of the resulting iodide molecule onto both the 3
and/or 5 positions of the phenol rings of tyrosinesfound in thyroglobulin. Thyroglobulinis
degraded to produce thyroxine(T4) and tri-iodothyronine(T3), which are the main hormones
produced by the thyroid gland. Therefore propylthiouracileffectively inhibits the production of
new thyroid hormones.
Uses:
Propylthiouracilis used to treat overactive thyroid (hyperthyroidism). It works by stopping the
thyroid gland from making too much thyroid hormone.
Methimazole
Methimazoleis a member of the class of imidazolesthat itimidazole-2-thionein which
amethylgroup replaces thehydrogenwhichis attached to anitrogen. It has a role as an
antithyroiddrug.
3-methyl-1H-imidazole-2-thione
Methimazoleis a member of the class of imidazolesthat itimidazole-2-thionein which
amethylgroup replaces thehydrogenwhichis attached to anitrogen. It has a role as an
antithyroiddrug.
3-methyl-1H-imidazole-2-thione
Mechanism of action
Methimazoleprevents iodine and peroxidasefrom their normal interactions with
thyroglobulinto form T4 and T3. This action decreases thyroid hormone production.
Methimazolealso interferes with the conversion of T4 to T3.
Uses:
Methimazoleis used to treat hyperthyroidism (overactive thyroid). It is also used before
thyroid surgery or radioactive iodine treatment.
Methimazoleprevents iodine and peroxidasefrom their normal interactions with
thyroglobulinto form T4 and T3. This action decreases thyroid hormone production.
Methimazolealso interferes with the conversion of T4 to T3.
Uses:
Methimazoleis used to treat hyperthyroidism (overactive thyroid). It is also used before
thyroid surgery or radioactive iodine treatment.
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