Lecture № 11

Drugs effecting on endocrine system

Abdullaev Dzhumadil, pharmD

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 The endocrine system is a messenger system comprising feedback loops
of the hormones released by internal glands of an organism directly into
the circulatory system, regulating distant target organs. In vertebrates, the
hypothalamus is the neural control center for all endocrine systems. In
humans, the major endocrine glands are the thyroid gland and the adrenal
glands. The study of the endocrine system and its disorders is known as
endocrinology. Endocrinology is a branch of internal medicine.

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 Mammary gland

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 The hormonal system (called the endocrine system in medical terminology)
has various glands that release different hormones.

A hormone is any of a class of signaling molecules produced by glands in

multicellular organisms that are transported by the circulatory system to target
distant organs to regulate physiology and behavior. Hormones are like the
body’s communication system. They take messages from one part of the body
(the gland) to tell another part of the body (the target cell) to do something
important. The endocrine glands influence reproduction, metabolism, growth
and many other functions.

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 Pineal gland: a small gland near
the center of the brain.
Melatonin

Parathyroid hormone
(PTH)

Insulin, glucagon,
somatostatin
Tri-iodothyronine (T3),
thyroxine (T4), calcitonin
Adrenaline, cortisol,
aldosterone, DHEA,
Testosterone Cortisol
Estrogen, progesterone,
anti-mullerian
-5- hormone (AMH)
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 Main classes of hormonal drugs
5-alpha-reductase inhibitors Melanocortin receptor agonists
Adrenal cortical steroids: Parathyroid hormone and analogs
-corticotropin Progesterone receptor modulators
-glucocorticoids Prolactin inhibitors
-mineralocorticoids Selective estrogen receptor modulators
Adrenal corticosteroid inhibitors Sex hormones:
Antiandrogens -androgens and anabolic steroids
Antidiuretic hormones -contraceptives
Antigonadotropic agents -estrogens
Antithyroid agents -gonadotropin releasing hormones
Aromatase inhibitors -gonadotropins
Calcimimetics -progestins
Calcitonin -sex hormone combinations
Estrogen receptor antagonists Somatostatin and somatostatin analogs
Gonadotropin-releasing hormone antagonists Synthetic ovulation stimulants
Growth hormone receptor blockers Thyroid drugs
Growth hormones
Insulin-like growth factors
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 Insulin ( from Latin insula, 'island') is a peptide hormone produced by beta cells of the pancreatic islets, also called
Langerhans islets by named of Paul Langerhans, a German physician and anatomist, who discovered the cells at the
age of 21 while he was a medical student, it is considered to be the main anabolic hormone of the body. It regulates
the metabolism of carbohydrates, fats and protein by promoting the absorption of glucose from the blood into liver,
fat and skeletal muscle cells

Insulin

A
30

Islet cell autoantibodies Islet autoantibodies are B 21

markers that appear when insulin producing beta
cells in pancreas are damaged. They can be
detected a long time before beta cells are -8-
0.9-7.1 ng/ml
 Decreased or absent insulin activity results in diabetes mellitus ( the Greek word diabetes
meaning siphon - to pass through and the Latin word mellitus meaning honeyed or sweet.), a condition of
high blood sugar level (hyperglycaemia). There are two types of the disease. In type 1
diabetes mellitus, the beta cells are destroyed by an autoimmune reaction so that insulin can
no longer be synthesized or be secreted into the blood (type 1 diabetes can occur without an
autoimmune nature, that is, idiopathically). In type 2 diabetes mellitus, the destruction of
beta cells is less pronounced than in type 1 diabetes, and is not due to an autoimmune
process. Instead, there is an accumulation of amyloid in the pancreatic islets, which likely
disrupts their anatomy and physiology. The pathogenesis of type 2 diabetes is not well
understood but reduced population of islet beta-cells, reduced secretory function of islet
beta-cells that survive, and peripheral tissue insulin resistance are known to be involved.
Type 2 diabetes is characterized by increased glucagon secretion which is unaffected by,
and unresponsive to the concentration of blood glucose. But insulin is still secreted into the
blood in response to the blood glucose. As a result, glucose accumulates in the blood.
Every day more than 4,000 people are newly diagnosed with diabetes in America. In
2018, 34.2 million Americans, or 10.5% of the population, had diabetes. Nearly 1.6
million Americans have type 1 diabetes. 19 million adults in Pakistan and
55,000 people with diabetes mellitus were registered -9- in Kyrgyzstan
Common antidiabetic agents include:
• insulin
• non-sulfonylureas or biguanides (metformin)
• sulfonylureas (chlorpropamide, glimepiride, glipizide, glyburide, tolazamide,
tolbutamide)
• meglitinides (nateglinide, repaglinide)
• thiazolidinediones (rosiglitazone, pioglitazone)
• alpha-glucosidase inhibitors (acarbose, miglitol)
• incretin mimetics (albiglutide, dulaglutide, exenatide, liraglutide, lixisenatide)
• amylin analogs (pramlintide)
• dipeptidyl peptidase 4 inhibitors (alogliptan, linagliptan, saxagliptin, sitagliptin)
• SGLT-2(Sodium-glucose cotransporter-2 ) inhibitors (canagliflozin, dapagliflozin,
empagliflozin).

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N Name Parenteral doses Half-
• 100units/mL (3mL vial) life
1 Insulin • 100units/mL (10mL vial)
here are a number of different ways to dose • Insulin dosing in T1DM will vary
insulin, and no single regimen will work for based on patient's age, weight, and 4–6
every patient. Patient variables like education, residual pancreatic insulin activity min
motivation, diabetes control, and resources • T1DM patients will typically require a
must all be considered when determining total daily insulin dose of 0.4 - 1.0
which method will best fit each individual.
units/kg/day
• A typical starting dose in
• A disposable pen: This contains a prefilled insulin cartridge. Once
metabolically-stable patients is 0.5
used, the entire pen unit is thrown away. units/kg/day
• A reusable pen: This contains a replaceable insulin cartridge. Once• After calculating the total daily dose,
empty, a person discards the cartridge and installs a new one. it should be given as follows:

•ADA - American Diabetes Association

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N Name Enteral doses Half-life

Non-sulfonylureas or biguanides tablet, immediate-release 4–8.7 hours

2 Metformin 500mg 850mg 1000mg 

Metformin is among the oldest and most well studied oral antihyperglycemic agents. Its efficacy has been
demonstrated both in the primary prevention of disease and secondary prevention of diabetes-related
morbidity and mortality . Because of metformin’s proven efficacy, low cost, and minimal side effect
profile, it is largely recommended as the first-line, initial monotherapy and as part of any combination
therapy (including with insulin) for the treatment and prevention of type 2 diabetes
Mechanism of action
Biguanides are classed as non-sulfonylureas. Metformin is the
only available biguanide for diabetes treatment. It inhibits the
amount of glucose produced by the liver, increases the insulin-
receptor binding and stimulates tissue uptake of glucose.

ADA - American Diabetes Association - 12 -

N Name Enteral Parenteral Half-life
doses doses

Sulfonylureas tablet 5–8 hours

3 Glimepiride 1mg 2mg
4mg

These drugs exert their hypoglycemic effects by stimulating insulin

secretion from the pancreatic beta-cell. Their primary mechanism
of action is to close ATP-sensitive K-channels in the beta-cell
plasma membrane, and so initiate a chain of events which results in
insulin release.

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N Name Enteral Parenteral Half-life
doses doses

Meglitinides
4 NateglinideNateglinide tablet 1.4 hours
Nateglinide is an oral antidiabetic agent that when 60mg
used in combination with metformin or 120mg
rosiglitazone to treat type 2 diabetes has been
shown to be effective in reducing HbA1c ( glycated
hemoglobin ) relative to metformin or rosiglitazone
monotherapy.

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N Name Enteral Parenteral Half-life
doses doses

Thiazolidinediones tablet 3 - 4 hours

5 Rosiglitazone 2mg 4mg

tablet
6 Pioglitazone 15mg 30mg
45mg 3–7 hours

TZDs exert their antidiabetic effects through a mechanism that involves

activation of the gamma isoform of the peroxisome proliferator-activated
receptor (PPAR gamma), a nuclear receptor. ... TZDs reduce insulin
resistance in adipose tissue, muscle and the liver.

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N Name Enteral Parenteral Half-life
doses doses
Alpha-glucosidase inhibitors :
2 hours
Acarbose comes as a tablet to take by mouth. It 25 mg, 50 mg
7 is usually taken three times a day. It is very and 100 mg
important to take each dose with the first bite of tablets
each main meal. 

2 hours
8 Miglitol antihyperglycemic action of  results
from a reversible inhibition of membrane- bound 25 mg, 50 mg
intestinal α-glucoside hydrolase enzymes. and 100 mg
tablets

Mechanism of action
AGIs inhibit the enzyme α-glucosidase at the brush border
of the intestinal epithelium, thus blocking the absorption of
carbohydrates in the small intestine.
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N Name Enteral Parenteral doses Half-life
doses
Incretin mimetics
lyophilized powder for
reconstitution
9 Albiglutide 30mg/pen 5–8 days 
Brand Name: Tanzeum 50mg/pen
Available as a single-use
injectable pen
Glucagonlike peptide-1 (GLP-1)
receptor agonist indicated as an
adjunct to diet and exercise to
improve glycemic control in adults
with type 2 diabetes mellitus
30 mg SC once weekly; may increase Mechanism of action
to 50 mg once weekly if glycemic Incretin mimetics are a new class of antidiabetic drugs which
response is inadequate involve modulation of the incretin system. They bind to and
activate glucagon-like peptide-1 (GLP-1) receptors on
pancreatic beta-cells following which insulin secretion and
synthesis are initiated.
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N Name Enteral Parenteral Half-life
doses doses
Amylin analogs :
10 Pramlintide
0.6mg/mL 48 minutes.

By mimicking the actions of the naturally occurring hormone

amylin, pramlintide complements insulin by regulating the
appearance of glucose into the circulation after meals via three
primary mechanisms of action: slowing gastric emptying, suppressing
inappropriate post-meal glucagon secretion, and increasing satiety.

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N Name Enteral Parenteral Half-life
doses doses
Dipeptidyl peptidase 4 inhibitors :

11 Alogliptin Tablet 6.25mg 12.5–21 h.

12.5mg 25mg

tablet
12
Linagliptin 5mg 180 h.

The mechanism of DPP-4 inhibitors is to increase incretin levels (glucagon-

like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP),
which inhibit glucagon release, which in turn increases insulin secretion,
decreases gastric emptying, and decreases blood glucose levels.

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N Name Enteral Parenteral Half-life
doses doses
SGLT-2 inhibitors
13 Canagliflozin 10–13) hours
For people with type 2 diabetes (T2D) and chronic Tablet 100mg
kidney disease (CKD), canagliflozin, an oral, 300mg
sodium-glucose co-transporter-2 (SGLT2)
inhibitor, has a renal- and cardiovascular-
protective effect in reducing the progression of
kidney impairment,
ADA - American Diabetes Association

Mechanism of action
Sodium-glucose cotransporter-2 (SGLT2) inhibitors are the latest class
of anti-hyperglycemic agents to receive FDA approval. SGLT2
inhibitors function through a novel mechanism of reducing renal
tubular glucose reabsorption, producing a reduction in blood glucose
without stimulating insulin release.

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 Diabetes insipidus
• Diabetes insipidus is characterized by extreme thirst and the passing of large
amounts of urine.
• It is caused by the lack of sufficient vasopressin, a hormone produced by the
brain that instructs the kidneys to retain water.
• Treatment options include vasopressin replacement.
The symptoms of diabetes insipidus
include:
• Extreme thirst that can't be quenched
(polydipsia)
• Excessive amounts of urine (polyuria)
• Colourless urine instead of pale yellow
• Waking frequently through the night t
urinate.
• Dry skin.
• Constipation.
• Weak muscles.
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• Bedwetting.
N Name Enteral doses Parenteral Half-life
doses
14 Vasopressin 20 units/mL
Brand Name: Vasostrict, Pitressin intravenous 10–20
used to manage anti-diuretic hormone solution minutes
deficiency. It has off-label uses and is used in
the treatment of gastrointestinal bleeding,
ventricular tachycardia and ventricular 2.7 to
defibrillation. Vasopressin is used to treat 4.6 h
diabetes insipidus("Insipidus" comes from
Latin language insipidus - tasteless) related to
low levels of antidiuretic hormone.
DDAVP intranasal
DDAVP® Nasal Spray (desmopressin acetate) spray (Stimate)
15 is a synthetic analogue of the natural pituitary
hormone 8-arginine vasopressin (ADH), an
antidiuretic hormone affecting renal water
conservation. (diabetes insipidus )

Replacement therapy
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 M
Bishkek city
Manas street 6

Rp Tanzeum 30mg/pen.
D.t.d № 1
Sig: 1 injection a week

25.04.2021
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 M
Bishkek city
Manas street 6

Rp: Canagliflozin 100 mg tab.

D.t.d № 20
Sig: 1 tab. a day

25.04.2021
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 M
Bishkek city
Manas street 6

Rp: DDAVP intranasal spray 10ml

D.t.d № 1

Sig: 1 dose intranasal 3 times a day

25.04.2021
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 Thank you for your attention !

Abdullaev Dzhumadil, pharmD

dzhumadil60@gmail.com

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