Peptide Hormones and the Endocrine System

1. PEPTIDE HORMONES
AND THE ENDOCRINE
SYSTEM
GROUP 1

2. ENDOCRINE
SYSTEM
The endocrine system is a
network of glands in your body that
make the hormones that help cells
talk to each other. They're responsible
for almost every cell, organ, and
function in your body.

3. HORMONES
- Hormones are mammalian metabolites
that are produced by endocrine or ductless
glands, are released directly into the blood,
and are involved in eliciting responses by
specific body organs and tissues.
-Bodies messenger

4. HISTORICAL DEVELOPMENT
• Present therapeutic use of endocrine products is an outgrowth of the primitive
practice of organotherapy.
Male impotence- powdered hog testis female sterility- rabbit uterus
• Basic philosophy for the use of mammalian organs - expressed by Vicary
• The origin and early development of endocrine therapy were empiric, but mostly
in today’s generation is the result of intensive investigations

5. GENERAL PHYSIOLOGIC INVOLVEMENT AND
THERAPEUTIC PHILOSOPHIES
• Hormones function as chemical transmitters of selective stimuli between the various
endocrine glands and specific body organs and tissues.
• Many peptide hormones will not enter cells in the absence of a specialized transport
system-binds to receptors that act in two ways:
(1) to directly induce changes in membrane permeability for ions,
glucose, amino acids, etc.
(2) to induce the production of a secondary messenger such as cyclic
AMP, which transmits the signal of the hormone within the cell.

6. Physiologic control of hormone formation or
release to regulate hormone level is a vital
aspect of maintaining metabolic
homeostasis and integrity of body function.
• Two general regulatory mechanisms are currently recognized
(1) There is a feedback mechanism that responds to change in concentration of
some substance in the blood.
(2) Mechanism involves external stimuli and is mediated by the hypothalamus;
the hypothalamus secretes releasing factors that act on the anterior pituitary
to increase the release of specific tropic hormones.

7. • Hypofunctioning gland
-most frequently encountered therapeutic situations
-can result from understimulation by the pituitary.
-originating within the peripheral gland itself can result from
congenital or acquired disorders (including
autoimmune disorders, tumors, infections,
vascular disorders, and toxins).
-Retain some degree of activity can potentially be stimulated
to approach normal activity by the use of drugs
Disturbance in the function of an endocrine
gland may take the form of excessive activity
(hyperfunction) or diminished activity
(hypofunction).

8. REPLACEMENT
THERAPY
• Merely uses endocrine preparations to supplement or totally replace abnormally low
levels of endogenous hormone
-A category of sex hormone responsible for the development and regulation
of the female reproductive system and secondary sex
characteristics.
-within the body
*Early diagnosis and treatment are essential in this type of therapy to avoid
irreversible changes that can occur, such as cretinism, gigantism, and other
comparable conditions*
USE OF HORMONES FOR REPLACEMENT
-long-term therapy
-With the use of normal body metabolites-serious side effects are usually minimal
-Insulin utilization

9. HYPERFUNCTIONING ENDOCRINE GLANDS
-[HORMONAL SUBSTANCES] / ANTIMETABOLITES / SURGICAL REMOVAL (RADIATION)
-Overstimulation by the pituitary
-Exogenous hormone-administered as a medication are often called exogenous
estrogen or synthetic estrogen
-The potential danger of serious side effects is considerably greater when hormones
are used for specific pharmacologic actions than when they are used for replacement
therapy*
-Prolonged therapeutic use of a hormone, such as cortisone, may cause irreversible
atrophy of the endocrine gland that normally produces the hormone or may induce
other undesirable secondary responses. the safest use of a hormone as a therapeutic
agent involves a short duration of therapy

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11. THYROID GLAND

12. Consists of 2 lobes.
Averaging 30g in weight

13. Galen - vaguely described in 2nd century.
Holler – in 1776, first described as ductless gland.
Roger of Palermo– in 12th century, used sponges and
seaweed in treatment of goiter.

14. Iodine is needed to make the thyroid hormones
thyroxine and triiodothyronine, which assist with the
creation of proteins and enzyme activity, as well as
regulating normal metabolism.
 Thyroxine - acting to increase metabolic rate and so
regulating growth and development.
 Triiodothyronine - similar to thyroxine but it has
greater potency.

15. Without enough iodine - these thyroid hormones do not work
properly and can lead to an under-active or overactive thyroid gland,
causing the medical conditions of hypothyroidism and
with various negative side effects in the body.

16. Hypothyroidism or underactive thyroid
 is a condition where the thyroid doesn't create and release enough
hormone into your bloodstream. This makes your metabolism slow down.
 Hypothyroidism can make you feel tired, gain weight, mental deficiency,
dry skin and be unable to tolerate cold temperatures.

17. Conditions:
Infants – Cretinism
Adults – Myxedema
Treatments:
Standard treatment for hypothyroidism involves daily use of
the synthetic thyroid hormone levothyroxine
(Levo-T, Synthroid, others)

18. Hyperthyroidism or hyperactivity
 also called overactive thyroid, is when the thyroid gland makes
more thyroid hormones than your body needs.
 Feel nervous, moody, weak, or tired. Having hand tremors, or
having a fast or irregular heartbeat, or having trouble
even when you are resting. Feel very hot, sweat a lot, or have
warm, red skin that may be itchy.

19. Conditions:
Exophthalmic goiter or Grave’s disease
Treatments:
Surgical, aided by Radioactive iodine and by antimetabolites
such as propylthiouracil

20. PRESCRIPTION PRODUCTS
 Thyroglobulin – obtained by fractionation of porcine thyroid gland.
Contains thyroxine and triiodothyronine.
Use and dose – usual daily dose is 16 to 200mg
PRESCRIPTION PRODUCTS
 Sodium levothyroxine – obtained from the thyroid gland of domesticated
animals.
Use and dose – used for replacement therapy of Myxedema, Cretinism
and mild forms of hypothyroidism. Usual dose is 25 to 300 mcg, once a day.

21. PRESCRIPTION PRODUCTS
 Sodium liothyronine – provided by chemical synthesis.
Use and dose – used for same purpose as sodium levothyroxine. The
usual dose is 5 to 100 mcg of liothyronine, once a day.
 Liotrix – mixture of synthetic sodium levothyroxine and sodium
liothyronine.

22. THYROID AND
PITUARY GLANDS
A PART OF ENDOCRINE PRODUCTS

23. LIOTRIX

24. WHAT IS
LIOTRIX ?
◦ Prescription Products : Thyrolar & Euthyroid
◦ Consensus equivalents for comparison of the various thyroid
preparations, based on 65 mg (I gr) of th y roid are thyroglobulin, 65
mg; sodium levothvroxine, 100 pg; sodium !iothyronine, 25 p.g; and
liotrix formulations containing 50 or 60 pg of levoth yroxine and
12.5 or 15 p.g of liothyronine
• This is a 4:1 mixture of synthetic
sodium levothyroxine and sodium
liothyronine.
• was developed when it was believed
that serum levels of both T4 and T3
were maintained by direct thyroidal
secretion. It is now known that the
thyroid gland secretes approximately
ten times more T4 than T3 and that
80% of serum T3 is derived from
deiodination of T4 in peripheral
tissues.

25. THYROLAR®
Thyrolar Tablets (Liotrix Tablets, USP) contain
triiodothyronine (T3 liothyronine) sodium and
tetraiodothyronine (T4levothyroxine) sodium in the
amounts listed in the "How Supplied" section. (T3
liothyronine sodium is approximately four times as
potent as T4thyroxine on a microgram for microgram
basis.)
The inactive ingredients are calcium phosphate,
colloidal silicon dioxide, corn starch, lactose, and
magnesium stearate. The tablets also contain the
following dyes: Thyrolar (liotrix) 1/4 - FD&C Blue #1
and FD&C Red #40; Thyrolar (liotrix) ½ - FD&C
Red #40 and D&C Yellow #10; Thyrolar (liotrix) 1 -
FD&C Red #40; Thyrolar (liotrix) 2 - FD&C Blue #1,
FD&C Red #40, and D&C Yellow #10; Thyrolar
(liotrix) 3 - FD&C Red #40 and D&C Yellow #10.

26. Euthyroid®

27. SODIUM
DEXTROTHYROXINE
The salt of the
synthetically prepared dextrorotatorv isomer of thyroxine.

28. SODIUM
DEXTROTHYR
OXINE
◦ Dextrothyroxine is a thyroid hormone used to treat hyperlipidemia.
◦ This substance is effective in a high dose (up to 8 mg daily) for the
treatment of hypothyroidism, but its occasional use for such
purposes is restricted to patients with cardiac disease who cannot
tolerate other thyroid medications.
◦ Dextrothyroxine also reduces serum cholesterol and low-density
lipoproteins, and it has been classed as a hypo-cholesterolemic agent.
Its greatest therapeutic utility is in this area, but patients must be
monitored carefully for ischemic myocardial changes and other
adverse reactions.
The hypocholesterolemia dosage
regimen starts with 1 mg daily for
a month; the dosage is increased
in 1-mg increments at intervals
no shorter than I month until a
satisfactory lowering of -
Lipoprotein has been achieved or
until a maximum daily dose of 8
mg is reached

29. CHOLOXIN®
GENERIC NAME(S):
DEXTROTHYROXINE

30. PITUITARY

31. THE PITUARY
GLAND
◦ The human pituitary gland or hypophysis is situated in a small cavity in
the sphenoid bone at the base of the skull and is attached to the base of
the brain by a short stalk.
◦ It weighs about 0.5 g. Galen considered it a strainer for spinal fluid, and
Vesalius later thought it was the source of mucus, lubricating the
nasopharynx. Pituitary is from the Latin pituita, meaning slime or mucus.
◦ The pituitary body is in reality 2 glands
by origin and function:
I. The anterior lobe is ectodernial in origin—derived from an
outpouching
from the primitive pharynx.
2. The posterior lobe is neural in ongin—derived from an
outpouching of the base of the brain

32. POSTERIOR
PITUITARY

33. POSTERIOR
PITUARY
The posterior pituitary is neural tissue and
consists only of the distal axons of the
hypothalamic magnocellular neurons that
make up the neurohypophysis. The
perikarya (cell bodies) of these axons are
located in paired paraventricular and
supraoptic nuclei of the hypothalamus.
The posterior lobe produces two
hormones, vasopressin and
oxytocin. These hormones are
released when the hypothalamus
sends messages to the pituitary
gland through nerve cells.
Vasopressin is also known as
antidiuretic hormone (ADH).

34. THE POSTERIOR PITUARY RELEASES THESE
HORMONES ………………

35. Extracts of posterior pituitary lobe exhibit the following
effects in experimental
animals and in humans:
A pressor effect, owing
to arteriolar
and capillary
vasoconstriction
01
Direct stimulation of
smooth muscle,
seen in the intact animal
or in preparations of
isolated muscles
.
02
An antidiuretic action,
effected by increasing the
tubular and collecting
duct resorption of water
in the kid-
11ev.
03

36. OXYTOCIN
α-hypophamine

38. OXYTOCIN
◦ The oxytocic principle is available as an injection for induction of
labor for medical indications (use for elective induction is
inappropriate) and for control of postpartum hemorrhage.
◦ A nasal spray is available to promote milk ejection on the infrequent
occasions when this is a problem in breast feeding.
◦ The dosage for induction of labor is determined by uterine response;
the intravenous infusion is started at a rate of 0.001 to 0.002 units
per minute. The dose is increased in similar increments until a
contraction pattern that resembles normal labor has been
established. The dosage for control of postpartum hemorrhage is 10
units intramuscularly after delivery of the placenta
a synthetically prepared peptide
hormone that occurs naturally in
the posterior lobe of the pituitary
gland. Glandular material is no
longer used as a commercial
source of this hormone.

39. PITOCIN ®
Pitocin (oxytocin injection) is a natural
hormone that causes the uterus to contract
used to induce labor, strengthen labor
contractions during childbirth, control
bleeding after childbirth, or to induce an
abortion.
Pitocin is administered under a physician's
supervision. The initial dose of Pitocin
should be 0.5-1 mU/min (equal to 3-6 mL of
the dilute oxytocin solution per hour). At 30-
60 minute intervals the dose should be
gradually increased in increments of 1-2
mU/min until the desired contraction pattern
has been established.

40. SYNTOCINON
®
Each ampoule contains 1mL
solution (10 IU/mL).
Excipients/Inactive Ingredients:
Sodium acetate trihydrate, acetic
acid glacial, chlorobutanol,
ethanol 94% w/w, water for
injections.

41. VASOPRESSIN
β-hypophamine

43. VASOPRESSIN
◦ regulates the threshold for resorption of water by the epithelium of
the renal tubules.
◦ The hormone is released into the blood when osmoreceptors in the
hypothalamic nuclei detect an increased extracellular electrolyte
concentration in the serum or a decreased blood volume. The
resulting fluid conservation contributes to maintenance of
homeostasis
◦ Vasopressin is employed in replacement therapy for the management
of diabetes insipidus, and one of the concerns in formulation is a
need for an increase in the duration of action.

44. Vasopressin injection is a sterile solution
in water for injection of the water-soluble,
pressor principle prepared by synthesis or
obtained from the posterior lobe of the pituitary. Either 8-L-arginine-
vasopressin(beef vasopressin) or 8-L-lysine-vasopressin (hog
vasopressin) meets monographic requirements.
Vasopressin injection is standardized so
that 1 ml possesses a pressor activity equivalent to 20 (iSP posterior
pituitary units. It is used to control neurohypophyseal diabetes
irisipidus but is ineffective in the nephrogenic form of the disease. It
is also
used as a peristaltic stimulant in postoperative ileus and to control
acute hemorrhage in the gastrointestinal tract and
esophagus. The usual dose, intramuscularly or subcutaneously, is 5
to 10 units, 2 or 3 times a day

45. Pitressin®
The dosage of vasopressin must be adjusted
to the needs of the individual patient, but
convenient therapy is handicapped to a degree
by the relatively rapid inactivation of the
hormone in the body.
The need to administer 5 to 10 USP units of
vasopressin (vasopressin injection), 2 or 3
times daily, is common. Formulation of
vasopressin tannate in peanut oil (Pitressine
Tannate) was developed to give a gradual
release of the hormone and a longer duration
of action; an intramuscular injection of 2.5 to
5 USP units of this preparation may exert the
desired action for 24 to 72 hours

46. LYPRESSIN&
DESMOPRESSIN
Lysine-vasopressin and 1-deamino-8-D-arginine-vasopressin

47. Lypressin& Desmopressin
Lypressin
◦ a synthetically prepared peptide hormone that
occurs naturally in the posterior lobe of the hog
pituitary gland. It has the properties of causing the
contraction of vascular and other smooth muscles
and of producing antidiuresis. Slightly more stable
than arginine-vasopressin, it is available as a nasal
spray for treatment of diabetes insipidus.
◦ Rx :Diapid®( W/out available pic)
Desmopressin
◦ a synthetic analog of arginine-vasopressin. It
possesses very little of the undesirable pressor
effect of the parent hormone and has a relatively
long duration of action. Desmopressin is use for
the same purposes as vasopressin and is available
as an injection and a nasal solution. The usual
parenteral dosage for diabetes insipidus is 2 to 4 ig
daily in 2 divided doses
◦ Rx: DDAVP® and Stimate®.

48. DESMOPRESSIN
DDAVP®
Stimate®.

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