Adrenal Agents. Women’s Health
Agents. Men’s Health
Agents.
Corticosteroids
• Adrenal glands produce glucocorticoids and
mineralocorticoids
• Glucocorticoids:
– Involved in cholesterol, fat, and protein
metabolism
• Mineralocorticoids:
– Involved in regulating electrolyte and water
balance
Cortisol
• Principal adrenal steroid hormone
• Responsible for:
– Gluconeogenesis
– Protein catabolism
– Anti-inflammatory reactions
– Stimulation of fat deposition
– Sodium and water retention
Corticosteroids
• Adrenal hormones excluding sex hormones
• Steroid production follows a circadian rhythm
Properties of glucocorticosteroides used in
clinics
• Anti-inflammatory
• Immune-depressive
• Anti-allergic
• Anti-shock
• Anti-toxic
Anti-inflammatory action of GCS
• Nonspecific inflammation
• Auto-immune component
• Hyperergic character
• Therapy of despair
Mechanism of anti-inflammatory action of GCS
GCS
activation of lipomoduline
decreasing of activity of phospholipase А2
slowing down of arachidonic acid
metabolites production
(prostaglandins, leucotriens,
thromboxan А2)
stabilization
of cellular and
lyzosomal
membranes
depression of
histamine, serotonin,
bradykinine releasing
decreasing of
leucocytes’
migration processes,
depression of
phagocytes activity
decreasing of capillaries’
wall permeability
Indications for administration of GCS
• Insufficiency of adrenal cortex
• Rheumatoid illnesses (rheumatoid arthritis, rheumatism, system red
lupus etc.)
• Chronic active hepatitis
• Bronchial asthma
• Ulcerative colitis
• Nephritic syndrome
• Auto-immune hemolytic anemia
• Shock and collapse of any etiology
• Brain, lungs, larynx edema
• Acute allergic reactions
• Transfusion reactions
• Heavy infections (hiding behind the etiotropic drugs!)
• Liver disesaes
Doses and terms of GCS therapy
Situation
Daily dose
Terms of
treatment
Acute cases (shock,
collapse, brain, lungs
edema, septic shock,
asthmatic condition etc.)
Subacute and acute attacks
of chronic processes
(rheumatoid diseases,
ulcerative colitis, bronchial
asthma etc.)
Primary and secondary
insufficiency of adrenal
cortex
200-500800-1000 mg
i.v.
1-3 days
20-50 mg
(rarely till
200 mg)
4-6 weeksseveral
months
2,5-10 mg
life-long
Corticosteroids
• Act as anti-inflammatory and
immunosuppressive agents in treating
diseases of different origins:
– Hematologic
– Allergic
– Inflammatory
– Neoplastic
– Autoimmune
Administration of GCS
• Insufficiency of adrenal cortex
• Rheumatoid illnesses (rheumatoid arthritis, rheumatism,
system red lupus etc.)
• Chronic active hepatitis
• Bronchial asthma
• Ulcerative colitis
• Nephritic syndrome
• Auto-immune hemolytic anemia
• Shock and collapse of any etiology
• Brain, lungs, larynx edema
• Acute allergic reactions
• Transfusion reactions
• Heavy infections (hiding behind the etiotropic drugs!)
• Liver diseases
Doses and terms of GCS therapy
Situation
Daily dose
Terms of
treatment
Acute cases (shock,
collapse, brain, lungs
edema, septic shock,
asthmatic condition etc.)
200-500800-1000
mg i.v.
1-3 days
Subacute and acute
attacks of chronic
processes (rheumatoid
diseases, ulcerative
colitis, bronchial asthma
etc.)
Primary and secondary
insufficiency of adrenal
cortex
20-50 mg
(rarely till
200 mg)
4-6
weeksseveral
months
2,5-10 mg
life-long
Hydrocortisone acetate
Prednisolone
Becotide = Beclometh
(beclomethasone dipropionate)
Kenalog
(triamcinolone acetonide)
Dexamethasone
Complications of
GCS-therapy
Izenko-Cushing’s
syndrome
MINERALOCORTICOIDS
Desoxycorticosterone acetate - DOXA
• Mode of action
Acts on kidney tubules: causes the reabsorption of sodium and
water, decreases the reabsorption of potassium,
regulates fluid-electrolyte metabolism, increases AP, enhances
muscle work
• Administration
For chronic adrenal insufficiency (Addison’s disease),
myasthenia, adynamia
• Side effects
edema, AP increasing, pulmonary edema, cardiac insufficiency
Glucocorticoids + mineralocorticoids
Drugs of female sex
hormones
Estrogens
estron
(oil solution
of folliculin)
estradiol
ethynilestradiol
(microfollin)
synestrol
Gestagens
progesterone
oxyprogesterone caproate
alilestrenol (turinal)
Ovarian-menstrual cycle
Administration of drugs
of female sex hormones
estrogens
1) Genital hypoplasia, primary and secondary
amenorrhea
2) Sexual underdevelopment of women
3) After ovary-ectomia
4) Climacteric disorders
5) Lactation depression
6) Weak labor activity
(estrogen background)
7) Prostate cancer of men, breast cancer of women
after the age of 60
8) A part of contraceptive agents
Sites of Action of the Estrogens
Administration of drugs
of female sex hormones
estrogens
1) Genital hypoplasia, primary and secondary amenorrhea
2) Sexual underdevelopment of women
3) After ovary-ectomia
4) Climacteric disorders
5) Lactation depression
6) Weak labor activity
(estrogen background)
7) Prostate cancer of men, breast cancer of women after
the age of 60
8) A part of contraceptive agents
Effects of Progesterone on the Body
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Decreased uterine motility
Development of secretory endometrium
Thickened cervical mucus
Breast growth
Increased body temperature
Increased appetite
Depressed T-cell function
Anti-insulin effect
Hormonal contraceptives
1) combined estrogen-gestagen
a) monophased (bisecurin, non-ovlon,
rigevidon, marvelon, demulen)
b) double-phased (anteovin, neo-eunomin)
c) triple-phased (tri-regol, trisiston)
2) monohormonal gestagen (mini-pilli)
exluton, ovret, continuin
3) postcoital hestagen (postinor)
4) depot-contraceptives - of prolonged action
norplant (levonorgestrel)
depot-provera (medroxyprogesterone acetate)
Administration of
gestagen drugs
1) miscarriage, habitual abortion
2) dysfunctional uterus bleedings,
algomenorrhea
3) as component of contraceptives
4) Climacteric disorders
Administration of
gestagens
1) miscarriage, habitual abortion
2) dysfunctional uterus bleedings, algomenorrhea
3) as component of contraceptives
4) Climacteric disorders
5) As part of fertility programs
6) Treat specific cancers with specific receptor site
sensitivity
Complications in case of administration of
hormonal contraceptives
hypertension
thrombo-embolia
hypercoagulation
dyspeptic disorders (nausea, vomiting)
migraine
depression
obesity
cholestatic jaundice
breast cancer, cancer of uterus cervix
ischemic heart disease
myocardium infarction
stroke
embryotoxic and teratogenic action
Antiestrogen drugs
ANABOLIC STEROIDS
Phenobolinum, Retabolil, Methandrostenolonum
-
PHARMACOLOGICAL EFFECTS
Stimulation of protein synthesis
Depression of phosphor and Ca++ excretion
Increase of bones, muscles and parenchymatous organs
mass
Stimulation of regeneration
-
ADMINISTRATION
Aplastic anemia (bone marrow suppression)
Osteoporosis, bone fractures
Exhausted diseases
Prolonged treatment with GCS
-
COMPLICATIONS
Hepatitis, sexual
disorders
(impotence),
edemas,
masculinization,
nausea, vomiting,
Sudden death