This document provides information about the endocrine pharmacology lecture schedule and teaching style of Frederick G. Hamel, Ph.D. It includes the lecture topics for the semester, information about lecture materials available online, an overview of the teaching style, diagrams of the hypothalamic-pituitary hormone axes and feedback loops, and descriptions of specific hormones and drugs related to the growth hormone and prolactin systems.
Introduction to the endocrine system
Growth hormone: Mechanism of Action, secretion, regulation.
Prolactin
Sex hormones
Oral contraceptives
Corticosteroids
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Proteins, peptides and amino acid derivatives
Proteins are large molecules made of many amino acids
Peptides are smaller molecules typically made of a few amino acids
Amino acid derivatives are molecules derived from a single amino acid
Introduction to the endocrine system
Growth hormone: Mechanism of Action, secretion, regulation.
Prolactin
Sex hormones
Oral contraceptives
Corticosteroids
Endrocrine drugs /certified fixed orthodontic courses by Indian dental academy Indian dental academy
The Indian Dental Academy is the Leader in continuing dental education , training dentists in all aspects of dentistry and offering a wide range of dental certified courses in different formats.
Proteins, peptides and amino acid derivatives
Proteins are large molecules made of many amino acids
Peptides are smaller molecules typically made of a few amino acids
Amino acid derivatives are molecules derived from a single amino acid
This note will be helpful for Pharmacy Students searching for analogues and inhibitors of various hormones in human body.
- anterior Pituitary hormones
- hormone functions
-inhibitors
-similar working drugs
-one day assignment size
TSH: thyroid-stimulating hormone
ACTH: adrenocorticotropic hormone
FSH: follicle-stimulating hormone
LH: luteinizing hormone
GH: growth hormone
PRL: prolactin
MSH: melanocyte-stimulating hormone
NOTE: THEY ALL (6) ARE RELEASED FROM ANTERIOR PITUITARY
ADH: antidiuretic hormone
Oxytocin
NOTE: THESE TWO ABOVE HORMONES ARE RELEASED FROM POSTERIOR PITUITARY
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TEST BANK for Operations Management, 14th Edition by William J. Stevenson, Verified Chapters 1 - 19, Complete Newest Version.pdf
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- Video recording of this lecture in English language: https://youtu.be/lK81BzxMqdo
- Video recording of this lecture in Arabic language: https://youtu.be/Ve4P0COk9OI
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These simplified slides by Dr. Sidra Arshad present an overview of the non-respiratory functions of the respiratory tract.
Learning objectives:
1. Enlist the non-respiratory functions of the respiratory tract
2. Briefly explain how these functions are carried out
3. Discuss the significance of dead space
4. Differentiate between minute ventilation and alveolar ventilation
5. Describe the cough and sneeze reflexes
Study Resources:
1. Chapter 39, Guyton and Hall Textbook of Medical Physiology, 14th edition
2. Chapter 34, Ganong’s Review of Medical Physiology, 26th edition
3. Chapter 17, Human Physiology by Lauralee Sherwood, 9th edition
4. Non-respiratory functions of the lungs https://academic.oup.com/bjaed/article/13/3/98/278874
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RESULTS: Overall life span (LS) was 2252.1±1742.5 days and cumulative 5-year survival (5YS) reached 73.2%, 10 years – 64.8%, 20 years – 42.5%. 513 LCP lived more than 5 years (LS=3124.6±1525.6 days), 148 LCP – more than 10 years (LS=5054.4±1504.1 days).199 LCP died because of LC (LS=562.7±374.5 days). 5YS of LCP after bi/lobectomies was significantly superior in comparison with LCP after pneumonectomies (78.1% vs.63.7%, P=0.00001 by log-rank test). AT significantly improved 5YS (66.3% vs. 34.8%) (P=0.00000 by log-rank test) only for LCP with N1-2. Cox modeling displayed that 5YS of LCP significantly depended on: phase transition (PT) early-invasive LC in terms of synergetics, PT N0—N12, cell ratio factors (ratio between cancer cells- CC and blood cells subpopulations), G1-3, histology, glucose, AT, blood cell circuit, prothrombin index, heparin tolerance, recalcification time (P=0.000-0.038). Neural networks, genetic algorithm selection and bootstrap simulation revealed relationships between 5YS and PT early-invasive LC (rank=1), PT N0—N12 (rank=2), thrombocytes/CC (3), erythrocytes/CC (4), eosinophils/CC (5), healthy cells/CC (6), lymphocytes/CC (7), segmented neutrophils/CC (8), stick neutrophils/CC (9), monocytes/CC (10); leucocytes/CC (11). Correct prediction of 5YS was 100% by neural networks computing (area under ROC curve=1.0; error=0.0).
CONCLUSIONS: 5YS of LCP after radical procedures significantly depended on: 1) PT early-invasive cancer; 2) PT N0--N12; 3) cell ratio factors; 4) blood cell circuit; 5) biochemical factors; 6) hemostasis system; 7) AT; 8) LC characteristics; 9) LC cell dynamics; 10) surgery type: lobectomy/pneumonectomy; 11) anthropometric data. Optimal diagnosis and treatment strategies for LC are: 1) screening and early detection of LC; 2) availability of experienced thoracic surgeons because of complexity of radical procedures; 3) aggressive en block surgery and adequate lymph node dissection for completeness; 4) precise prediction; 5) adjuvant chemoimmunoradiotherapy for LCP with unfavorable prognosis.
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1. ENDOCRINE PHARMACOLOGY
Frederick G. Hamel, Ph.D.
Veterans Affairs Medical Center R208A
346-8800 x3032
fghamel@unmc.edu
Thursday: Hypothalamic and Pituitary Hormones
Monday: Adrenal Corticosteroids
Tuesday: Thyroid Drugs
Wednesday: Diabetes and Insulins
Thursday: Oral Anti-Diabetic Agents
Spring: Calcium and Bones, Sex Steroids,
Contraception and Related Topics
2. Toews Teaching Home Page
Nothing fancy; hopefully useful
At info.unmc.edu/toews/
Linked from Pharmacology Teaching Home Page
fghamel@unmc.edu
Contact me with questions, comments
Lecture Slides
PowerPoint slides as presented in class
Study/Review Questions
Essay/short answer style questions, with answers
Sample Questions from Previous Exams, MiniQuizzes
Multiple choice, with answers explained
A few previous MQ essay questions with answers
3. MY TEACHING STYLE
Syllabus very complete
- should contain all information for exam
- required drugs highlighted in bold
Slides and lecture will follow syllabus
- required drugs in blue
- new information not in handout in brown
Lecture slides and additional material on website
Questions
1. Mechanism of action
a. Molecular
b. Physiological
2. Uses
a. When
b. How
3. Contraindications
10. Adapted from Brenner, Fig 31-1
Vasopressin
Oxytocin
ACTH
FSH TSH Prolactin
Growth hormone
LH
Regulate target organ
hormone production
Thyroid
T3,T4
End organsGrowth
Metabolism
Vessels
Kidney
Uterus
Breast
Directly regulate
end organ responses
15. Problems with peptides as drugs
Hard to identify initially
• trace amounts, local action
Expensive to purify
Immune reactions if animal products used
Human form may be required
Difficult to synthesize chemically
Generally ineffective orally
• poorly absorbed, rapidly hydrolyzed
Generally require injection
• unpleasant
• still rapid hydrolysis, short half-life
16. Technical advances for peptides as drugs
Production by recombinant DNA technology
• large amounts, pure, human
Novel amino acids to prevent hydrolysis
• D-isomers, other analogs
Routes of administration
• nasal, transdermal
• needle-free delivery devices (GH, insulin)
• one oral, more coming
Identify synthetic analogs from combinatorial
libraries by high-throughput screening
Optimize for potency, duration, specificity
Oral non-peptide mimetics
Peptides are becoming increasingly useful as drugs
20. CRH, ACTH, corticosteroids
Corticosteroids preferred for therapy
• Glucocorticoids, mineralocorticoids
Adrenocorticotropic hormone (ACTH)
• Porcine ACTH (corticotropin)
• Synthetic human ACTH[1-24] (cosyntropin)
• Diagnosis of H-P-A function, tumors
Corticotropin releasing hormone (CRH)
• Sheep or recombinant human hormone
• Diagnosis of H-P-A axis function
21. TRH, TSH, thyroid hormones
Thyroid hormones used extensively for therapy
Thyroid stimulating hormone (TSH)
• Bovine pituitary or recombinant human
• Diagnosis of thyroid function, esp. tumors
Thyrotropin releasing hormone (TRH)
• Synthetic TRH (Protirelin)
• Diagnosis of thyroid disease
22. GnRH, gonadotropins, sex steroids
(Covered in more detail next semester)
Sex steroid hormones used extensively
• HRT, contraception, menstrual control
Gonadotropins used therapeutically
• diagnosis and treatment of infertility
GnRH analogs used extensively
• to mimic or to block GnRH responses
• good examples of synthetic peptide analogs
with altered pharmacokinetic and
pharmacodynamic properties
24. The growth hormone system (pituitary level)
Growth hormone (GH)--191 a.a. pituitary peptide
• Useful for treating GH deficiency
– promoting growth in children (1/4000)
– body maintenance in adults
• Preparations
– only human hormone works
– human cadaver product used until 1984
withdrawn due to Creutzfeldt-Jakob
– recombinant hormones used now
25. The growth hormone system (pituitary level)
Growth hormone (GH)
• Recombinant hormone preparations
Somatropin (Nutropin®, others)
human sequence
Somatrem (Protropin®)
human sequence plus extra methionine
– IM or SC, 3-7/week
– Depot somatropin (Nutropin Depot®)
IM 1-2/month
– New "Cool.Click" needle-free delivery device
26. The growth hormone system (pituitary level)
Growth hormone (GH)
• Effective
– increased linear growth
– decreased fat, increased muscle, bone
– increased sense of well-being
• Expensive ($20,000/yr)
27. The growth hormone system (pituitary level)
Growth hormone (GH)
• Approved uses
– GH deficiency, Turner’s syndrome, Prader-
Willi syndrome, renal insufficiency, AIDS
cachexia
– approved 2003 for "normal short stature"
(NGHD, non-GH-deficient)
• Efficacy and safety in other conditions under
investigation
– delayed growth, wound healing in severe
burns
• Some abuse by athletes, body-builders for
anabolic effects
28. The growth hormone system (hypothalamic level)
Growth hormone-releasing hormone (GHRH)
Sermorelin (Geref®)
– Synthetic human GHRH[1-29] (of 44 total)
– Approved 1998 for GH deficiency
– Stimulates release of GH IGF-1
– Requires pituitary function
– IV, SC, nasal administration
– Somewhat cheaper than GH ($10,000/yr)
– Somewhat less effective than GH?
– Long-term effects not known
– Used more diagnostically than
therapeutically
29. The growth hormone system (pituitary level)
Pegvisomant (Somavert®)
– first GH receptor antagonist
– blocks actions of released GH
– in clinical trials, orphan status for acromegaly
(GH excess)
– Approved 2003
30. The growth hormone system (hypothalamic level)
Somatostatin (SS)
• 14- and 28-amino acid cyclic peptides
• Hypothalamic SS inhibits GH release (and TSH
and prolactin)
• Pancreatic SS inhibits release of insulin,
glucagon
• Gut SS inhibits release of VIP, others
• Not useful therapeutically
– action too short, too much insulin effect
Octreotide (Sandostatin®)
• Clinically useful synthetic SS analog
• 8-amino acid cyclic peptide
32. The growth hormone system (hypothalamic level)
Octreotide
• Longer-acting than somatostatin
• Less effect on insulin than with somatostatin
– 10-20X selectivity
– some receptor subtype selectivity
– prefers SSTR-2 and -5 receptors, those
expressed on tumors
• Regular octreotide
– given SC, 2-3X/day
• Newer long-acting depot preparations
– Sandostatin LAR®: IM every 4 wks
33. The growth hormone system (hypothalamic level)
Octreotide
• Uses
– metastatic carcinoid (5HT-secreting
tumor)
– VIP-secreting tumors
– inhibit GH secretion (acromegaly)
– inhibit TSH and glucagon secretion
– treating GI secretion disorders
• Mostly GI side effects (GI SSTRs)
– diarrhea, nausea, flatulence,
malabsorption
– gallstones
34. Pharmacological stategies for growth hormone
system therapy
Short stature, GH deficiency
• Sermorelin: hypothalamic hormone
– stimulate GH release
• Somatropin, Somatrem: pituitary hormones
– replacement GH
Acromegaly, excess GH
• Octreotide: hypothalamic hormone
– inhibit GH release
• Pegvisomant: GH receptor antagonist
– block actions of released GH
36. The prolactin system
Prolactin (pituitary hormone)
• No drug preparations
Dopamine (hypothalamic level)
• Endogenous inhibitor of PRL release
• Numerous DA drugs alter prolactin
– DA agonists inhibit prolactin secretion
anti-Parkinson drugs, bromocriptine
– DA antagonists cause hyperprolactinemia
antipsychotics, antidepressants
• Dopamine itself not useful pharmacologically
– dopamine agonist analogs used instead
37. The prolactin system
Dopamine agonist analogs
Bromocriptine (Parlodel®)
– Pergolide (Permax®) also used
– D1 and D2 receptors
– non-peptide, orally effective
vaginal tablets also used
– for hyperprolactinemia (infertility)
– for suppression of lactation
– to decrease prolactinoma tumor mass
– for acromegaly
inhibits GH too (in acromegaly only)
– side effects: GI, nausea, lightheadedness
tolerance generally develops
38. The prolactin system
Dopamine agonist analogs
Cabergoline (Dostinex®)
– same uses as bromocriptine
– highly D2-selective analog
D2 is the target for prolactin
but also for side effects
– fewer side effects than bromocriptine
due to pharmacokinetics (slower
absorption and longer action), not due
to D2 selectivity (?)
– longer half-life
70 hr, vs. 7 hr for bromocriptine
allows 1/d dosing
– slightly more effective
40. Posterior pituitary hormones
Vasopressin (antidiuretic hormone, ADH)
• 9-amino acid peptide
• Released in response to ↑ osmolarity
or ↓ blood pressure
• Actions
– increase renal water absorption to ↓
osmolarity
– vasoconstriction to ↑ blood pressure
41. Posterior pituitary hormones
Vasopressin
• Acts on G protein-coupled receptors
– V1 receptors
vascular smooth muscle: constriction
– V2 receptors
kidney: water absorption
endothelial cells: clotting factors
• Deficiency leads to diabetes insipidus
• Used to treat diabetes insipidus (V2) and
certain bleeding disorders (V1 and V2)
42. Posterior pituitary hormones
Vasopressin preparations
Arginine vasopressin (AVP, Pitressin®)
– synthetic human vasopressin
– IV, IM, SC, nasal
– short-acting
– acts on V1 and V2 receptors
– agent of choice for V1 effects or for short-
term uses (whether V1 or V2)
local bleeding artery, hemorrhage (V1);
e.g. esophageal varices, colonic diverticula
temporary post-surgical DI (V2)
43. Posterior pituitary hormones
Vasopressin preparations
Desmopressin acetate (DDAVP, Stimate®)
– stable peptide analog (10-20 hr)
– highly V2 selective (~4000-fold)
– IV, SC, inhaled
– new oral prep, first oral peptide drug!!
– DDAVP is the preparation of choice for
diabetes insipidus
• An improved peptide drug
– stability, selectivity, administration
45. Posterior pituitary hormones
Vasopressin preparations
Desmopressin acetate
• Uses
– treatment of choice for diabetes insipidus
nasal has been; oral may be soon
– nocturnal enuresis, to concentrate urine
– to increase clotting factor synthesis in
hemophilia, von Willebrand’s
– all are V2 effects
46. Posterior pituitary hormones
Vasopressin preparations
• Side effects
– V1 receptors: increased blood pressure,
GI cramps, headache
– oxytocin receptor: uterine contractions,
cramps
– occur with AVP, minimal with DDAVP
47. Posterior pituitary hormones
Oxytocin
• 9-aa peptide, two different from AVP
• used to control labor, post-partum bleeding,
and lactation
• Covered in more detail next semester
50. 1. Which of the following drugs is recombinant
human growth hormone-releasing hormone?
a. Sermorelin
b. Somatropin
c. Somatrem
d. Somatostatin
e. Somavert
f. Somalia
g. Somany similar-sounding drug names!
51. 1. Which of the following drugs is recombinant
human growth hormone-releasing hormone?
a. Sermorelin
b. Somatropin (GH)
c. Somatrem (GH with extra methionine)
d. Somatostatin (GH release inhibitory hormone)
e. Somavert (will be trade name of GH antagonist
pegvisomant)
f. Somalia (country on east coast of Africa)
g. Somany similar-sounding drug names! (True!)
52. 2. Octreotide
a. is recombinant human somatostatin.
b. has similar potencies for inhibiting growth hormone
and insulin release.
c. is available as a once-per-month depot preparation.
d. is the only agent available to inhibit growth
hormone release.
e. mediates its effects by activating dopamine D2
receptors.
53. 2. Octreotide
a. is recombinant human somatostatin. (a synthetic
shortened and stabilized analog)
b. has similar potencies for inhibiting growth hormone
and insulin release. (quite selective for GH over
insulin)
c. is available as a once-per-month depot preparation.
d. is the only agent available to inhibit growth
hormone release. (bromocriptine is effective also)
e. mediates its effects by activating dopamine D2
receptors. (bromocriptine acts on D2 receptors,
octreotide on SS-Rs)
54. 3. Which of the following statements comparing
arginine vasopressin with desmopressin is
TRUE? Desmopressin
a. has a more selective effect on vascular smooth
muscle.
b. has a shorter duration of action.
c. is an agonist whereas arginine vasopressin is an
antagonist.
d. has a greater selectivity for the V2 receptor vs.
the V1 receptor.
e. is an orally-effective non-peptide analog of the
arginine vasopressin peptide.
55. 3. Which of the following statements comparing
arginine vasopressin with desmopressin is
TRUE? Desmopressin
a. has a more selective effect on vascular smooth
muscle. (on kidney, not VSM)
b. has a shorter duration of action. (longer-acting)
c. is an agonist whereas arginine vasopressin is an
antagonist. (both are agonists)
d. has a greater selectivity for the V2 receptor vs.
the V1 receptor.
e. is an orally-effective non-peptide analog of the
arginine vasopressin peptide. (is now available
orally but is still a peptide)
56. REQUIRED DRUG LIST REVIEW
somatropin
somatrem
sermorelin
octreotide
bromocriptine
cabergoline
arginine vasopressin (AVP)
desmopressin (DDAVP)
57. KEY CONCEPTS REVIEW
Hypothalamic-pituitary regulation
• feedback inhibition
• replacement vs. suppressive therapy
Peptides as drugs
• problems and solutions
• advantages and disadvantages
• examples
