Drugs for endocrinology disorders

Endocrine system

Glands secrete hormones that regulate processes such as growth, reproduction, and nutrient use (metabolism) by body cells.

Ductless glands

influence a target organ by releasing hormones into the bloodstream.

Hormones

Substances produced within one organ and secreted directly into the circulation to exert its effects at a distant location

Endocrine glands

• Pineal.

• Pituitary.

• Thyroid.

• Thymus.

• Adrenal.

• Pancreas.

• Ovary and testis

Lipid-soluble hormones

Diffuse through the target cell's plasma membrane

Water-soluble hormones

Depend on second messengers

Master gland (pituitary gland)

Controls other glands of the endocrine system.

Compsed of lobes (anterior and posterior).

Controlled by the hypothalamus

anterior pituitary gland

adenohypophysis

posterior pituitary gland

neurohypophysis

negative feedback

the mechanism that regulates most hormones that control the endocrine system

positive feedback

the end product stimulates more production of the end product

Glucocorticoids

make energy to meet the body's demands

Aldosterone

a mineralocorticoid, regulates blood pressure by regulating electrolytes

Deficiency of glucocorticoids

leads to Addison's disease and excess production to Cushing's disease

Cortisol and cortisone

• Stimulate glucose production (gluconeogenesis).

• Breakdown of fat (lipolysis).

• Inhibit glucose uptake

Regulation of releasing factors

Higher amounts of corticotropin and cortisol are produced during the waking hours.

Stress with Cortisol and cortisone

Increases CRH and ACTH secretion, which stimulates cortisol secretion

Negative feedback with Cortisol and cortisone

As cortisol levels rise in the body, less releasing factor is secreted

Gluconeogenesis

Process of making glucose in the liver

Protein catabolism

Breakdown of proteins into amino acids

What Glucocorticoids do

Regulate the metabolism of carbohydrates and proteins, especially during times of stress

Clinical Uses of Glucocorticoids

• Replacement therapy for adrenocortical insufficiency (Addison’s disease).

• Inflammatory disorders.

• Multiple sclerosis.

• Hypercalcemia from cancer.

• Adrenal cortical insufficiency.

• Respiratory disease.

• Management of leukemias and lymphomas

Anti-inflammatory Effects of Glucocorticoids

reduces the inflammatory reaction by limiting capillary dilation and permeability. Also restrict the accumulation of white blood cells at inflammatory sites

Pancreatic islets

parts of the pancreas that have endocrine functions

Glucagon secretion for pancreas

• Increases circulating glucose levels.

• Stimulates gluconeogenesis in liver, which allows glucose to enter the circulation.

• Helps in converting amino acids to glucose

Incretins

Stimulate and increase insulin secretion

Normal glucose levels:

70 to 110 mg/dl

Insulin

binds to plasma membrane insulin receptors on skeletal and heart muscle and adipose tissue. stimulates glycogen synthesis in muscle and liver, inhibits the release of glucose form the liver into the bloodstream, and also inhibits the breakdown of protein and fat for energy

Glycated hemoglobin (HbA1c)

Used to evaluate 3 months of glucose levels

Source of insulin

• Originally obtained from pork or beef organs.

• Today, it is produced only through recombinant DNA technology.

• today varies in its onset and duration of action

Amylin Analog - Pramlintide

Co-secreted by the beta cells with insulin.

• Without enough amylin, blood glucose levels rise.

• Mimics amylin to control glucose levels.

Incretin mimetics - Exenatide and liraglutide

Hormones secreted from the duodenum.

• Increase insulin secretion

Oral Antidiabetic Drugs

• Used in the management of type 2 diabetes.

• Approved for treatment when diet and exercise have not achieved target glycemic control

Secretagogues

Substances that induce or cause the secretion of another substance.

-should not be used in type 1 diabetes

Sulfonylureas

Reduce fasting plasma glucose

Non-sulfonylureas

Stimulate insulin secretion.

• Quicker onset of action

drugs-Indicated for Type 2 DM

• Glucose absorption inhibitors (alpha-glucosidase inhibitors).

• Biguanides (Metformin)

• Insulin sensitizers - Thiazolidinediones.

• Dipeptidyl peptidase-4 (DPP-4) inhibitors.

• Sodium-glucose cotransporter 2 (SGLT2) inhibitors

Semaglutide weight loss

increasing the amount of insulin produced by the pancreas, resulting in reduced appetite and food intake

Takes 8 weeks or longer

Pluripotential

Affects physiology and metabolism of target tissues other than those associated with reproduction

Oral contraceptives

Maintain high blood levels of estrogen/progesterone, which inhibit release of FSH and LH

Monophasic

release a fixed amount of estrogen

Biphasic and Triphasic

the pill color varies over the cycle and represents different strengths

Androgen

Male sex hormone

Erectile Dysfunction Drugs

• Increase blood flow to the penis, producing an erection.

• They act by inhibiting PDE5 actions in the penis so that cGMP accumulates and a full erection is maintained