Endocrine Pharmacology

• The term 'endocrine' refers to the system of

ductless glands which synthesize and secrete
hormones directly into the bloodstream to
regulate and coordinate various body
functions.
• In addition to the specialized endocrine
organs, many other organs and tissues such
as kidneys, liver and gonads have secondary
endocrine functions as they also synthesize
and secret certain hormones.
2
• The endocrine system is coordinated by the
nervous system which synthesizes certain factors
and/or sends information for the release of
hormones from endocrine tissues.
• Therefore, endocrine system is more precisely a
'neuroendocrine system'.
• The coordinated activity of these two major
systems viz. nervous and endocrine is
essentially' required for the stability of internal
environment (homeostasis) in the body.

3
 Hormones
• A hormone (Greek word hormaein = to stir up) is
a chemical substance that is produced by the
endocrine (ductless) glands or specific cells in
body and is transported through circulation to
act on its target cells.
• Hormones carry messages like
neurotransmitters, but unlike neurotransmitters
they act slowly and convey messages to organs
or tissues those may be located distantly in the
body. 4
• Hormones are involved mainly in the control of
physiological functions including metabolism,
growth, development and reproduction.

• Drug therapy for the endocrine system is

implemented mainly either to replace a
hormone deficiency when the gland function is
inadequate or to reduce or prevent effects of an
overactive hormone.

5
 Divisions of Endocrine System
• I. Pituitary
• 1. Anterior pituitary
• a. Growth hormone
• b. Prolactin
• c. Thyroid stimulating hormone/Thyrotropin
• d. Follicle stimulating hormone
• e. Luteinising hormone
• f. Adrenocorticotropin hormone/Corticotropin
6
• 2. Posterior pituitary
• a. Antidiuretic hormone/Vasopressin
• b. Oxytocin
• II. Thyroid
• a. Thyroxine (T 4)
• b. Triiodothyronine (T3)
• c. Calcitonin
• III. Parathyroid gland
• a. Parathormone

7
• IV. Adrenal gland
• 1. Adrenal cortex
• a. Glucocorticoids
• b. Mineralocorticoids
• c. Sex steroids
• 2. Adrenal medulla
• a. Epinephrine
• b. Norepinephrine

8
• V. Gonads
• 1. Ovaries
• a. Oestrogens
• b. Progesterone
• 2. Testes
• a. Androgens
• VI. Pancreas/Islets of Langerhans in Pancreas
• a. Insulin
• b. Glucagon

9
 Mechanisms and Control of Hormonal Action

• The endocrine hormones after their release are

transported by blood vascular system to affect
other tissues.

• The protein hormones are hydrophilic whereas

steroid and thyroid hormones are lipophilic.

10
• The hormones most often do not act directly on
the intracellular machinery, but require
interaction with specific hormone receptors.

• Protein hormones have specific receptors on

target tissues plasma membrane, whereas
steroids have specific receptors within the
cytoplasm or nucleus.

11
• The interaction of hormone and receptor
typically triggers a cascade of secondary effects
within the cytoplasm of the cell, often involving
phosphorylation or dephosphorylation of
various other cytoplasmic proteins, changes in
ion channel permeability, or increased
concentrations of intracellular molecules.

12
 Pituitary Gland:
• The pituitary gland (Hypophysis) is a pea-
sized endocrine gland that is attached by a
stalk to underside of the cerebrum of the
brain.
• It is often called the' Master endocrine gland'
because it produces a range of hormones and
regulates the secretion of many other
endocrine glands in the body.

13
 Hormones of Pituitary Gland
• The anterior pituitary gland secretes six
important hormones viz. growth hormone,
prolactin, thyroid stimulating hormone,
adrenocorticotropic hormone, follicle
stimulating hormone and luteinising
hormone and the posterior pituitary gland
secretes two important hormones viz.
vasopressin and prolactin

14
15
 Important features of anterior pituitary
hormones.
Table No.49.1:
Page 713

16
 Growth Hormone:
• Growth hormone (Somatotropin,
somatotrophin, somatotropic hormone,
somatotrophic hormone, STH, GH) is a
protein based peptide hormone.

17
• Growth hormone stimulates growth, cell
reproduction and regeneration in humans
and other animals.

• It acts either directly on target tissues or

indirectly through insulin-like growth factors
produced mainly in the liver.

18
 DISORDERS OF GROWTH HORMONE

• Deficiency of growth hormone

• Growth hormone deficiency can occur in dogs
as a primary abnormality resulting in
pituitary dwarfism (panhypopituitarism) or
as an acquired deficiency leading to growth
hormone dependent dermatosis

19
• Clinical signs of GH deficiency include
abnormal growth (dwarfism).
• Hypopituitary dwarfism in pups (mainly seen
in German Shepherd) is characterised by
growth retardation with alopecia and skin
depigmentation.

20
• Deficiency of GH also causes hyperkeratosis,
epidermal atrophy, follicular atrophy and
thinning of skin due to defective
development of elastin fibres in the skin.

21
 Excess of growth hormone
• Excessive secretion of GH, may result in
acromegaly in both human and animals.

• Acromegaly is often associated with

excessive GH secretion in response to
progesterone therapy or spontaneous
disease.

22
• Clinical signs of acromegaly reflect either
anabolic or catabolic abnormalities.

• Increased body size results from proliferation

of bone and connective tissues, particularly
of the limbs, feet, head and abdomen.

23
 TREATMENT OF GROWTH HORMONE
DISORDERS
• I. Drugs used in deficiency of GH
• 1. Growth hormone and analogues
• e.g. growth hormone (somatotropin),
somatropin.
• 2. Growth hormone releasing hormone and
analogues e.g. sermorelin.

24
• 3. Insulin-like growth factor-I and analogues
e.g. mecasermin.
• 4. Drugs used in diagnosis of GH deficiency
• a. Alpha2-adrenoceptor agonists
e.g. xylazine.
• II. Drugs used in excess of GH
• I. Synthetic analogues of somatostatin
e.g. octreotide.
• 2. Growth, hormone receptor antagonists
e.g. pegvisomant.
• 3. Other drugs e.g. bromocriptine. 25
 PROLACTIN
• Prolactin (Lactogenic hormone, luteotropic
hormone, mammotropin, luteotropin) is a
peptide hormone that is structurally related to
growth hormone and belongs to
somatomammotropin hormone family.
• It is secreted by mammotroph (Iactotroph) cells
which are abundant in the anterior pituitary and
increase in number during pregnancy, probably
under the influence of oestrogen.
26
• Prolactin is involved mainly in the
development of mammary gland and
maintenance of lactation.

27
 Excess of Prolactin
• Hyperprolactinaemia is a common syndrome in
humans and animals.
• Hyperprolactinaemia may be caused by
prolactin secreting tumours, disorders of
hypothalamus or pituitary affecting prolactin
secretion
• Clinical manifestations of hyperprolactinaemia
may include galactorrhoea and infertility in
females.
28
• Antiprolactin drugs (e.g. dopamine agonists)
are used clinically to control pathological
hyperprolactinaemia in various species.

29
 Deficiency of Prolactin
• Deficiency of prolactin can cause suppressed
mammary development and improper
lactation.

30
 TREATMENT OF PROLACTIN
DISORDERS
• Drugs are available mainly for treatment of
hyperprolactinaemia.
• Classification
• Drugs used to treat prolactin disorders have
been broadly classified into two classes:
Drugs used in excess of prolactin and drugs
used in deficiency of prolactin.

31
• I. Drugs used in excess of prolactin
• 1. Dopamine agonists
• e.g. bromocriptine.
• II. Drugs used in deficiency of prolactin
• e.g. growth hormone.

32
 THYROID STIMULATING
HORMONE
• Thyroid stimulating hormone (Thyrotropic
hormone, TSH) is a glycoprotein hormone,
synthesised and secreted by thyrotroph cells
of the anterior pituitary.
• It regulates the activity of thyroid gland,
including the synthesis and release of thyroid
hormones.

33
 DISORDERS OF TSH RELEASE
Deficiency of TSH

• Deficiency of TSH is involved only in a few

cases of hypothyroidism.

• Deficiency of TSH secretion from the pituitary

gland results in secondary hypothyroidism.

34
• The deficiency of TSH results in impaired
production and secretion of the thyroid
hormones.

• The clinical signs of secondary or tertiary

hypothyroidism resemble those of primary
hypothyroidism and refer to multiple body
systems

35
 Excess of TSH
• Excess of TSH may be encountered in thyroid
gland insufficiency.

• Excess of circulating TSH is possibly

responsible for the increase in size of thyroid
that occurs in iodine deficiency.

36
• Clinically. Hyperthyroidism resulting in
excessive secretion of thyroid gland primarily
occurs due to defects (e.g. neoplasia) in
thyroid gland itself.

37
 TREATMENT OF TSH DISORDERS
• Drugs Used in Deficiency of TSH
• Thyroid stimulating hormone
• Thyroid stimulating hormone (TSH) or
thyrotropin is obtained commercially from
the bovine anterior pituitary gland.

38
 GONADOTROPIC HORMONES
• The gonadotropic hormones (gonadotropins) are
a family of protein hormones, which act on
gonads and promote their growth and
development.
• These hormones include anterior pituitary
gonadotropins namely the follicle stimulating
hormone and luteinising hormone, and non-
pituitary gonadotropins namely the human
chorionic gonadotropin (hCG) and equine
chorionic gonadotropin (eCG). 39
DISORDERS OF GONADOTROPINS
• Deficiency of Gonadotropins
• Disturbances of gonadotropins secretion
from pituitary may be responsible for
delayed puberty in both males and females.

40
• In females, deficiency of FSH results in
improper follicular growth and ovulation.

• Inadequate secretion of LH by pituitary may

lead to ovulation failure or delayed
ovulation, which often results in reduced
conception rates and infertility in animals.

41
 Excess of Gonadotropins
• Excess of gonadotropins may result in precocious
puberty in both sexes. Ovarian hyperstimulation,
superovulation and polycystic ovary may be
observed in females.
• Polycystic ovaries develop when the ovaries are
stimulated to produce excessive amounts of male
hormones (androgens), particularly testosterone.

42
 TREATMENT OF GONADOTROPIN
DISORDERS
• 1. Drugs used in deficiency of gonadotropins
• I. Gonadotropins and analogues
• a. Pituitary gonadotropins e.g. follicle
stimulating hormone-pituitary, luteinising
hormone-pituitary etc.
• b. Non-pituitary gonadotropins
• e.g. human chorionic gonadotropin and equine
chorionic gonadotropin.
43
• 2. Gonadotropin releasing hormone and
analogues e.g. gonadorelin.
• 3. Gonadotropin releasing hormone-
receptor agonists
• e.g. leuproline.

44
• II. Drugs used in excess of gonadotropins
• I. Gonadotropin releasing hormone
receptor antagonists
• e.g. degarelix.
• 2. Synthetic gonadal steroids
• e.g. danazol.

45
 ADRENOCORTICOTROPIC
HORMONE
• Adrenocorticotropic hormone
(Adrenocorticotrophic hormone, ACTH) is a
polypeptide hormone secreted by the
corticotrophic cells of the anterior pituitary.

• It regulates mainly the synthesis and secretions

of glucocorticoids from the adrenal cortex.

46
 MoA
• Adrenocorticotropic hormone stimulates the
ACTH specific G- protein receptors present in
the middle and inner zones of adrenal cortex
to synthesise glucocorticoids, primarily
hydrocortisone and corticosterone.

47
 DISORDERS OF ACTH
• Deficiency of ACTH resulting from pituitary
insufficiency leads to hypoadrenocorticism .

• However, the occurrence of isolated ACTH

deficiency in animals is rare; it occurs along
with deficiency of other pituitary derived
hormones.

48
 Excess of ACTH
• Excess secretion of ACTH results mainly from
pituitary tumours

49
 TREATMENT OF ACTH DISORDERS
• 1. Drugs used in deficiency of ACTH
• I. Adrenocorticotropic hormone and analogues
e.g. corticotropin.
• II. Drugs used in excess of ACTH
• I. (Corticotropin releasing hormone) CRH -I
receptor antagonists
e.g. antalarmin.

50
• 2. Dopamine Agonists
e.g. pergolide.
• 3. Mono-amine oxidase inhibitors
e.g. selegiline.
• 4. Antihistamines
e.g. cyproheptadine.

51
 POSTERIOR PITUITARY
HORMONES
• The posterior pituitary (neurohypophysis)
secretes two major hormones - vasopressin
(antidiuretic hormone) and oxytocin.

52
 Treatment of Vasopressin
disorders:
• I. Drugs used in deficiency of vasopressin
• 1. Vasopressin and analogues e.g
vasopressin, desmopressin
• 2. Miscellaneous drugs e.g. chlorpropamide,
thiazides

53
• II. Drugs used in excess of vasopressin
• 1. Vasopressin receptor antagonists. E.g.
conivaptan (non selective) , nelivaptan
(selective V1), satavaptan (selective V2), etc.
• 2. Tetracyclines e.g. demeclocycline.

54
 TREATMENT OF OXYTOCIN-
RELATED DISORDERS
• I. Drugs used in deficiency of oxytocin
• 1. Oxytocin and analogues e.g. oxytocin,
posterior pituitary extract.
• II. Drugs used in excess of oxytocin e.g.
atosiban.

55
 Adrenal Hormones
• Adrenal (Suprarenal) glands are a pair of
endocrine glands located just anterior to the
kidneys.
• Hormones secreted by adrenal glands regulate a
number of metabolic processes, which are
essential for life and enable animals to function
in a constantly changing environment.

56
• Each adrenal gland is divided into two
separate entities, a cortex and a medulla, each
of which produces different types of
hormones.
• The adrenal cortex constitutes about 90% of
the adrenal mass.
• Adrenal cortex synthesises two major types of
steroid hormones, glucocorticoids and
mineralocorticoids together which are called
adrenocortical hormones or corticosteroids.

57
 CORTICOSTEROIDS
• The adrenal cortex produces a large number
of different corticosteroid hormones.
Although more than 50 different steroids
have been identified, but only hydrocortisone
(cortisol) and corticosterone have
predominantly glucocorticoid activity

58
• Aldosterone and deoxycorticosterone have
predominantly mineralocorticoid activity.
• Among glucocorticoids, hydrocortisone
predominates in man, horses, pigs, sheep and
cats, and corticosterone predominates in
rabbits, mice and rats.
• Dogs secrete these two hormones in
approximately equal amounts.

59
 Physiological Effects
Glucocorticoids
• Glucocorticoids affect a wide range of
activities in the body.
• They prepare body to withstand effect of all
kinds of noxious stimuli and stress.
• They have some direct and other effects (i.e.
facilitates other hormones to exert effects).

60
• In the fasted state, they stimulate several
processes which collectively serve to increase
and maintain normal concentrations of
glucose in blood.
• These processes may include stimulation of
gluconeogenesis, inhibition of peripheral
glucose utilisation and increasing tissue
stores of glycogen.

61
• Glucocorticoids reduce protein stores in
essentially all body cells except those of liver
by both decreased protein synthesis and
increased protein breakdown.
• Glucocorticoids promote lipolysis and
generate free fatty acids.
• Glucocorticoids inhibit intestinal absorption
and enhance renal excretion of Ca++

62
• Glucocorticoids possess anti-inflammatory and
immuno- suppressive effects.
• Glucocorticoids suppress all types of
inflammatory reactions whether caused by
invading pathogens, by chemical, thermal or
mechanical stimuli, or by hypersensitivity.
• Glucocorticoids exert profound effect on specific
host-immune responses. They suppress all types
of hypersensitisation and allergic phenomenon.

63
• Glucocorticoids decrease capillary permeability
and maintain tone of arterioles.
• Glucocorticoids decrease the number of
eosinophils, monocytes and lymphocytes in
blood.
• Glucocorticoids exert a number of indirect
effects on the CNS through maintenance of
blood pressure, glucose concentration and
electrolytes concentration.

64
• Excess of glucocorticoids may suppress
production and release of ACTH. Excess of
glucocorticoids may also inhibit production of
TSH; however, growth hormone production is
increased.
• High concentrations of glucocorticoids may
stimulate gastric acid and pepsin production
and may aggravate peptic ulcers.

65
 Classification:
• Drugs used in deficiency of adrenal hormones
(hypoadrenocorticism) and drugs used in excess
of adrenal hormones (hyperadrenocorticism).
• I. Drugs used in deficiency of adrenal
hormones
• A. Corticosteroids
• 1. Glucocorticoids
• e.g. dexamethasone, betamethasone
66
• d. Topical and inhalant glucocorticoids e.g.
beclometasone.
• 2. Mineralocorticoids e.g. aldosterone.
• II. Drugs used in excess of adrenal hormones
• I. Inhibitors of corticosteroid biosynthesis e.g.
ketoconazole
• 2. Inhibitors of glucocorticoid receptors e.g.
mifepristone.
• 3. Inhibitors of aldosterone receptors
e.g. spironolactone
• 4. Inhibitors of ACTH biosynthesis and release
e.g. bromocriptine
67
 Gonadal Hormones
• The gonads in females are ovaries and in
males are testes.
• They secrete steroidal hormones which affect
sexual behaviour, secondary sex
characteristics, accessory sex organs and
reproduction.
• Gonads are controlled hormonally by LH and
FSH.

68
• The ovaries produce two main types of
steroid hormones, the oestrogens and the
progestogens.
• The most important of oestrogens is the
hormone estradiol and the most important
progestogen is the progesterone.
• The oestrogens promote mainly proliferation
and growth of specific cells in body and are
responsible for development of most
secondary sexual characteristics of the
female.
69
• The progestogens, on the other hand, are
concerned almost entirely with final
preparations of the uterus for pregnancy and
mammary glands for lactation.
• In addition to the steroidal hormones, the
ovaries are involved in the secretion of
peptide hormones/factors.

70
 OESTROGENS
• Oestrogens (Estrogens) are a group of compounds
synthesised mainly by ovaries but also in fairly
large amounts by placenta in pregnant animals
and in small amounts by testes in males and by
adrenal cortex in both sexes.
• Some other tissues such as liver, muscle and hair
follicles can also convert steroid precursors into
oestrogens.

71
• Oestrogens have immense importance in the
oestrous cycle of animals and function as the
primary female sex hormones.
• Oestrogens are largely responsible for the
development and maintenance of female sex
organs.
• Oestrogens produced at puberty stimulate
the growth of mammary glands.
• Oestrogens have also been observed to
increase blood cholesterol and calcium in
birds and some mammalian species.
72
 DISORDERS OF OESTROGENS
• Deficiency of oestrogens can result from
ovarian hypoplasia, lack of ovaries, or
genetically abnormal ovaries which secrete
wrong hormones because of missing enzymes
in the secretory cells.

73
• Excess secretion of oestrogens by the ovaries
occurs rarely because hypersecretion of
oestrogens automatically decreases the
production of gonadotropins by pituitary, and
this in turn limits the production of ovarian
hormones.
• A rare granulosa cell tumour can develop in
an ovary, which secretes large quantities of
oestrogens. Such tumours, occasionally seen
in mares.

74
 Classification:
• Drugs used in deficiency of oestrogen and
drugs used in excess of oestrogen.
• I. Drugs used in deficiency of oestrogens /
Oestrogenic drugs
• A. Steroidal oestrogens
• 1. Natural steroidal oestrogens
e.g. estradiol.
• 2. Semi-synthetic steroidal oestrogens
e.g. estradiol benzoate . 75
• 3. Synthetic steroidal estradiols
e.g. mestranol
• B. Non-steroidal oestrogens/Synthetic non-
steroidal oestrogens.
e.g. diethylstilbestrol
• Il. Drugs used in excess of oestrogens / Anti-
oestrogenic drugs
• A. Oestrogen receptor inhibitors
• I. Mixed oestrogen receptor antagonist-agonists
e.g. clomifene

76
• 2 .Selective oestrogen receptor antagonists
e.g. fulvestrant.
• B. Aromatase Inhibitors/ Oestrogen
synthesis inhibitors
• C. Selective aromatase inhibitors
e.g. anastrozole.
• 2. Non-selective aromatase inhibitors
e.g. testolactone.

77
 PROGESTOGENS
• The progestogens (progestins) are a group of
naturally occurring steroidal hormones.
• For practical purposes, progesterone is
considered as the single important natural
progestogen.

78
• The progesterone is secreted by the corpus
luteum of cycling animal and by corpus
luteum and placenta of some species during
pregnancy.
• The testes in males and adrenal cortex in
both sexes also secrete small amounts of
progesterone.
• Progesterone is needed for the maintenance
of pregnancy in all species whether supplied
by the corpus luteum or placenta, or both.

79
 Physiological Effects
• Progesterone acts on uterus to cause
quietening of the myometrium by decreasing
the frequency and intensity of uterine
contraction.
• This secretion prepares the uterus for
implantation of the fertilised ovum and
provides nutrition to it.

80
• During implantation and gestation,
progesterone appears to decrease the
maternal immune response to allow for the
acceptance of the pregnancy.
• Overall, progesterone favors pregnancy;
abortion generally occurs if progesterone is
lacking or deficient during pregnancy.
• Progesterone causes development and
proliferation of lobule-alveolar system in the
mammary gland during pregnancy.

81
• Progesterone favours an economy of body
metabolism and has anabolic effects because
appetite is stimulated during pregnancy and feed
is utilised more efficiently.
• Progesterone stimulates lipoprotein lipase activity
and it seems to enhance fat deposition.
• Progesterone in conjunction with estradiol
suppresses LH and FSH secretion, oestrus and
ovulation.
• Recent studies have indicated that progesterone
promotes myelin sheath repair in the brain.
82
 Deficiency of Progesterone
• Progesterone deficiency if occurs, may result
in oestrogen dominance, a condition where
individual may have deficient, normal or
excessive oestrogen but has little or no
progesterone to balance its effects in the
body.
• Follicular cysts in animals may produce
progesterone deficiency with signs of
hyperoestrogenism, primarily expressed as
intense oestrus behaviour. 83
• Stressful living in human beings also leads to
oestrogen dominance because
hydrocortisone and progesterone may
compete for common receptors in cells and
excessive hydrocortisone release during
stress impairs progesterone activity.
• Progesterone deficiency has been
incriminated as a cause of abortion in mares,
queens, bitches and some other species.

84
• High plasma progesterone levels are
observed in luteal cysts in animals.
• Excessive progesterone may prevent final
growth and maturation of follicles.
• Too much progesterone in women has been
associated with tiredness and sedation

85
 TREATMENT OF PROGESTOGEN
DISORDERS
• Drugs used to treat progestogen disorders
have been broadly classified into two classes:

• drugs used in deficiency of progestogens and

drugs used in excess of progestogens.

86
• 1. Drugs used in deficiency of progestogens
• Depending on the chemical structure, drugs
used in deficiency of progestogens have been
divided into following groups:
• 1. Natural progestogens e.g. progesterone.
• 2. Progesterone derivatives e.g. megestrol
• 3. 19-Norprogesterone derivatives e.g.
nomegestrol.

87
• 4. Testosterone or 19-Nortestosterone
derivatives
• a. Older progestogen e.g. Norgestrel
• b. Newer progestogens e.g. norgestimate
• 5. Miscellaneous progestogens e.g.
altrenogest

88
• II. Drugs used in excess of progestogens
• 1. Progesterone receptor inhibitors
• a. Selective progesterone receptor
antagonists e.g. mifepristone.
• b. Mixed progesterone receptor
antagonist/agonists e.g. ulipristal.
• 2. Progesterone synthesis inhibitors
e.g. epostane.

89
 MALE GONADS
• The male gonads or testes are the primary
organs of reproduction in the male.
• Similar to the ovaries, testes are components of
both the reproductive system and the endocrine
system.
• The primary functions of testes are to produce
sperm (gametogenesis) and to produce
androgens, primarily testosterone.

90
• Both functions of testes are influenced by
gonadotropic hormones produced by the
anterior pituitary.

91
 ANDROGENS
• The testes secrete several male sex hormones
which are collectively called androgens.
• These include testosterone,
dihydrotestosterone, androstenedione and
dehydroepiandrosterone.
• Testosterone is the main androgen.

92
• The androgens are mainly concerned with
spermatogenesis, growth, development of
accessory sex organs and secondary sexual
characteristics in the male. In addition, they
have marked anabolic effects in puberty
causing development of the musculature and
increased bone growth.
• The testes in addition to androgens also
synthesise small amounts of oestrogens,
which are probably also essential for
spermatogenesis.

93
 Physiological effects
• The androgens in general are responsible for
the development of primary and secondary
sex characters in males and are necessary for
spermatogenesis.
• The androgens are responsible for the growth
and development of male gonads.

94
• Lack of androgens in male foetus usually
results in the development of female external
phenotype.
• Androgens are responsible for descend of
testis into the scrotum in male foetus.
Androgens are required for the
spermatogenesis in seminiferous tubules and
for the maturation of sperm in passage
through epididymis and vas deferens.

95
• Androgens are responsible for development
of secondary sex characteristics in males.
They influence hair pigmentation and growth
in birds.
• Androgens have anabolic effects and they
favour growth of skeleton and musculature
with increase in body weight. They cause
increased protein synthesis, particularly in
the skeletal muscle

96
• Production and release of pheromones by
males of some species also depend on the
androgens.
• Androgens also may be responsible in part for
the aggressive and sexual behaviour of males in
some species of animals.

97
 DISORDERS OF ANDROGENS
• Deficiency of androgens, a condition called
hypoandrogenism, may result from
hypogonadism in males. This deficiency may
also be caused by problems of the pituitary
gland or hypothalamus.
• In some cases, androgens may be present in
sufficient concentrations, but there is genetic
absence of androgens receptors in the target
cells.
98
• Hypersecretion of androgens by testes, a
condition called hyperandrogenism, occur
rarely in animals.
• A rare interstitial Leydig cell tumour may
sometimes produce as much as 100 times the
normal quantity of testosterone.

99
 Classification:
• Drugs used to treat androgen disorders have
been broadly classified into two classes:

• drugs used in deficiency of androgens and

drugs used in excess of androgens.

100
• I. Drugs used in deficiency of androgens
• A. Androgenic steroids/Drugs producing
primarily androgenic effects
• 1. Androgen receptor agonists
• a. Natural androgenic steroids
• e.g. testosterone.
• b. Synthetic androgenic steroids e.g.
testosterone cypionate, testosterone
propionate etc.

101
• 2. Selective androgen receptor modulators
e.g. andarine.
• B. Anabolic steroids/Drugs producing
primarily anabolic effects
• 1. Testosterone derivatives e.g. stanozolol.
• 2. Estrene anabolic steroids /Nor-
testosterone derivatives e.g. nandrolone.
• 3. Prohormones of anabolic steroids e.g. 1-
testosterone

102
• II. Drugs used in excess of androgens
• 1. Inhibitors of androgen synthesis
• a. 5α-Reductase inhibitors e.g. finasteride.
• b. CYP17A 1 inhibitors e.g. abiraterone.
• c. Gonadotropin-releasing hormone and
synthetic analogues e.g: gonadorelin.
• d. Miscellaneous-agents e.g. ketocoriazole.

103
• 2. Androgen receptor antagonists e.g.
cyproterone acetate.
• 3. Female sex hormones e.g. delmadinone.

104