3. ďSecretory products of endocrine glands
released directly into circulation in
ďsmall amounts and transported to
ďspecific target cells or organs where they
ďExert physiological, morphological or
biochemical responses
Hormones???
4. Endocrine Hormones:
travel via bloodstream to
target cells
Neurocrine hormones:
released from nerve terminals
Paracrine hormones:
act on adjacent cells
Autocrine hormones:
Released and act on the cell
that secreted them.
Intracrine Hormones:
act within the cell that
produces them.
Cell to cell signaling ???
5. ⢠Growth & Differentiation
⢠Maintenance of
homeostasis
⢠Reproduction
⢠Regulation of biochemical
reactions
Functions of Hormones
6. ⢠Highest relay centre
⢠Integrates endocrine & ANS and ensures
the smooth coordination by the cerebral
cortex
⢠Hypothalamic regulatory hormones
â Releasing hormones
⢠TRH, GnRH, GHRH,CRH, MSH-RF, Prolactin Releasing
factor
â Releasing inhibitory hormones
⢠GH-RIH, MSH-RIF, PIF
Role of Hypothalamus ?
11. Syndromes associated with GH?
⢠Deficiency of GH
âDwarfism
âIncreased CVS
Mortality
⢠Excess GH
âGigantism
âAcromegaly
12. Dwarfism
⢠Shortness of stature
⢠Growth retardation in
all parts of body proportionately
Q.Normal mental activity
⢠Immature faces
⢠Delicate extremities
Q Sexual maturity does not occur if associated
with gonadotropin deficiency
13. Gigantism
⢠Abnormal height
⢠Large hands and feet
Q.Coarse facial features
Q.Bilateral
gynaecomastia
⢠Loss of libido
⢠Hyperglycemia
17. Somatrem
⢠Derivative of growth hormone with
additional methionine at amino
terminus
Q.Somatropin and somatrem have similar
biological action and potencies
Q.Half life = 20 minutes but biological
action lasts 9-17 hrs
⢠Once daily administration is sufficient
19. Sermorelin acetate?
⢠A synthetic form of Human GHRH
⢠Peptide of 29 Aminoacids corresponds
to first 29 AA of Human GHRH
Q.Has full biological activity
⢠Well tolerated , Less expensive
Q.But less effective will not work in
defects of anterior pitutary
20. Uses of Growth hormone
⢠Replacement therapy
20-40 microgram/ kgS.C. daily
⢠Turners syndrome
â 50 microgram/kg
⢠Aids associated wasting
â 3-4 microgram / kg
21. Adverse effects
Q.â ICT with papilloedema
⢠Visual changes
⢠Headache, nausea
⢠Leukemia
Q.â incidence of type 2 DM
⢠Adults:
â Edema, Carpal tunnel syndrome,
arthralgia, myalgia
23. Somatostatin
⢠GHIH
⢠Non specific
â TSH, insulin, gastrin
⢠Half life = 1-3 min
⢠Rebound increase in GH after its
discontinuation
⢠Not preferred
24. Octreotide
⢠More specific for Growth hormone
⢠Less chances of hyperglycemia
⢠Uses
â Carcinoid syndrome
â VIP secreting tumors
â Gastrinoma
â Secretory diarhoea: AIDS, DM
â IBS , Esophageal Varices , insulinoma
⢠Dose: 50 -200 ¾g TDS subcutaneously
25. Sandostatin
⢠Slow releasing form
⢠20-40 mg IM 4 weekly
⢠Adverse effects of somatostatin
analogs
â Abdominal pain
â Steathorrea
â GB stone
â Vit B12 deficiency
26. Prolactin
⢠198 Amino acid peptide hormone
⢠Synthesis and secretion starts in fetal
pitutary
⢠â Secretion of prolactin by
â Hypothalamic regulation
⢠â secretion of prolactin by
â Stress, exertion, hypoglycemia
â TRH, VIP, prolactin releasing peptide
32. Bromocriptine
⢠Pharmacokinetics
â Only 1/3rd absorbed orally
â First pass metabolism present
â Half life = 3 hours
⢠Dose:
â Start 1.25 mg HS
â After 1 week 1.25 mg can be added in morning
â Can be increased to 5 mg BD
35. Cabergoline
⢠Ergot derivative with longer half life
⢠T ½ = 65 hours
⢠Higher affinity and selectivity to D2
receptors
⢠More effective less toxic
⢠Dose= 0.25 mg twice weekly
40. Preparations of gonadotropins
⢠Menotropin: FSH + LH
â Obtained from urine of postmenopausal women
⢠Urofollitropin: Pure FSH
â Preferred in PCOD
⢠HCG
â Obtained From Urine Of Pregnant Females
⢠DNA recombinant FSH
41. Uses of gonadotropins
⢠Infertility in females
â When clomiphene fails
â Menotropin for 10 days then HCG 10000 IU, IM
⢠Infertility in males
â HCG 1000-2500 IU, IM 3 times in a week
â Then menotropin after 3-4 months
⢠Cryptorchism
⢠To aid Invitro fertilization
⢠Regress AIDS related Kaposis Sarcoma
44. Gonadorelin
⢠Synthetic GnRH
⢠T ½ = 4-6 min
⢠Used for testing pitutary gonadal axis in male
or female hypogonadism
⢠Pulsatile administration IV every 90 min
â Infertility, cryptorchism. & delayed puberty
46. GnRH agonists
⢠Longer acting 6-12 hours
⢠Initial increase in LH & FSH
⢠But after 1-2 weeks cause desensitization
and decrease FSH & LH secretion
⢠Decrease estrogen and testesterone
⢠They cause pharmacological oopherectomy
and orchiectomy
47. Uses of GnRH analogs
⢠Precocious puberty
⢠Prostatic carcinoma
⢠Breast cancer
⢠Contraception: under
investigation
48. Adverse effects
⢠Hot flushes
⢠Loss of libido
⢠Vaginal dryness
⢠Osteoporosis
⢠Emotional liability
49. GnRH antagonists
Cetrorelix , Granirelix
⢠Competitive antagonists
⢠Advantage
â No initial increase in gonadotropins
â Do not cause histamine release
⢠Used in endometriosis 3 mg Cetrorelix SC
weekly for 2 months
⢠Uterine Fibroids: cetrorelix twice weekly for
1 month before surgery
50. Pegvisomant
It is a new GH- receptor antagonist.
Mechanism: prevent GH-
Binding to its receptor &
Suppression of serum
IGF-1 levels
Uses : Acromegaly(
patients resistant to
other therapies)
ADRs: Pain, Abnormal
liver function tests
51. Mecasermin
It is combination of recombinant human IGF-1 with
recombinant human IGFBP-3. This combination
maintain desired half life of IGF-1.
Uses: 1.Growth failure in children due to deficiency
of IGF-1.
2.Treatment of patients with GH gene deletion
ADRs: Cardiac murmur, hypoglycemia, iron
deficiency anaemia.
52. Sermorelin
Synthetic peptide analogue of GHRH, given by S.C.
Uses:
As a diagnostic agent to assess GH secretion for the
purpose of diagnosing GH deficiency.
Off label uses :
Acute or age-related growth hormone insufficiency
Side effects:
injection site reactions (such as pain, swelling, or
redness), headache, flushing,difficulty
swallowing,dizziness,,sleepiness,nausea,vomiting
54. Somatrem
It is first recombinant human GH
Sequence was identical to human GH except
extra methionine at N- terminal
Uses:
GH deficiency in children but due to short half
life require subcutaneous injection once a day
Side effects:
Precipitation of type 2 diabetes, pain at injection
site, fluid retention & headache
55. Somatostatin Analogue
Vapreotide:
Synthetic somatostatin analogue
Use:
Esophageal variceal bleeding in patients with cirrhotic liver
disease, AIDS related diarrhea.
Pasireotide:
new somatostatin analogue with higher affinity for receptors.
Uses:
orphan drug for cushing disease
Seglitide:
is another potent somatostatin analogue
56. Quinagoline
⢠It is oral selective D-2 receptor agonist.
⢠Racemic mixture of two enantiomers
⢠Uses:
⢠Hyperprolactinemia, breast pain, acromegaly
⢠Side effects:
⢠nausea, headache, orthostatic hypotension.
58. Which of the following is not an adverse effect
of growth hormone therapy?
a.Carpal tunnel syndrome
b.Hypoglycemia
c. Intracranial hypertension
d.Slipped femoral epiphysis
(b)
59. Which of the following is used in the
treatment of hyperprolactinemia?
a. Cimetidine
b. Methysergide
c. Bromocriptine
d. Ondanesetron
(c)
60. Octerotide is used in all except
a. Glucagonoma
b. Insulinoma
c. Carcinoids syndrome
d. Glioma
(d)
61. All of the following statements about
octerotide are true except
a. It is effective orally
b. It is used for the treatment of acromegaly
c. It can be used for the management of
secretory diarrhea
d. It can be used in portal hypertension
(a)
62. Octreotide is useful in esophageal varices. It is a
synthetic analogue of somatostatin. The true
statement regarding this drug is
a.It can be given orally
b.It is longer acting than somatostatin
c. Its major adverse effects is secretary diarrhea
d.All of the above
(b)
63. All of the following agents are useful in
acromegaly except
a. Bromocriptine
b. Somatostatin
c. Octreotide
d. Nafarelin
(d)
64. Mechanism of action of bromocriptine is via
a. Agonism at D2 receptors
b. Antagonism at D2 receptors
c. Antagonism at D1 receptors
d. Antagonism at Îą receptors
(a)
65. Important difference between leuprolide
and ganirelix is that ganirelix
a. Can be given orally
b. Immediately reduces gonadotropin secretion
c. Must be given in a pulsatile fashion
d. Initially stimulates release of LH and FSH
(b)
66. Long acting dopamine agonist is
a. Bromocriptine
b. Lisuride
c. Cabergoline
d. Apomorphine
(c)
67. Bromocriptine is useful in all except
a. Parkinsonism
b. Prolactinoma
c. Endogenous depression
d. Infertility
(c)
68. Drugs used for treatment of acute
variceal bleeding are all except
a. Octreotide
b. Somatostatin
c. Desmopressin
d. Terlipressin
(c)
69. GnRH analogue used in hormonal
treatment of carcinoma prostate is?
a. Goserelin
b. Nilutamide
c. Cyproterone acetate
d. Finasteride
(a)
70. Which of the following is given at intervals as a
pulsatile therapy?
a. GnRH
b. GH
c. FSH
d. Estrogen
(a)
71. True regarding use of bromocriptine for
suppression of lactation includes
a. It can cause deep vein thrombosis
b. It can cause hypotension
c. Metoclopramide potentiates the action of
bromoÂcriptine
d. It is given for 1 week only
(b)
72. The clinical use of leuprolide include all the
following EXCEPT
a. Endometriosis
b. Osteoporosis
c. Prostate cancer
d. Precocious puberty
(b)