Steroidal drugs
• Steroids are polycyclic organic compound containing 1,
2-cyclopentaperhydro phenanathrene skeleton
• I.e. it contains four fused ring viz A, B, C and D and
thus are polycyclic hydrocarbon.
• The angular methyl group, present at position no.13 and 10
is numbered as 18 and 19 respectively.
• The numbering of steroidal nucleus is retained even if
carbon atom of ring or angular methyl group is removed or increased.
• Thus, though C18 methyl group is absent, the angular
methyl group at C10 is numbered as C19.
• So it is C18-nor steroids nucleus.
Adrenocorticoids
• The steroidal hormones secreted by cortex of adrenal gland
are:
a) Glucocorticoids –e.g.
cortisone and hydrocortisone.
b) Mineral corticoids
–e.g. Aldosterone
• Glucocorticoids
are necessary to regulate carbohydrate, lipid and protein metabolism.
• Mineralocorticoides
are mainly concerned with the salt and water metabolism. They maintain proper
electrolyte balance.
Used of Glucocorticoids
Glucocorticoids are
used to treat:
1. Disease of
connective tissue like rheumatism, rheumatoid arthritis etc.
2. Dermatological
disease .e.g. –eczematous conditions
3. Allergic and
anaphylactic reactions.
4. Collagen
disease like lumps erythematosus
5. Asthma and
other respiratory tract disease.
• Cortisone has both glucocorticoids and mineralocorticoides
activity.
• Reduction of C11 oxo group to –OH group gives
hydrocortisone which is 10 times potent than cortisone but also possesses
mineralocorticoides activity.
TESTOSTERONE
• The steroidal skeleton present in its androstane, in which
different groups attached are:
• Hydroxy group at C17
• Keto group at C3
• Double bond between C3 and C5
Properties of Testosterone:
• It is white crystalline powder.
• It is odourless.
• It is tasteless.
• It is slightly soluble in water.
• It is freely soluble in alcohol.
Storage and
stability: It is stored in well closed –light resistant containers.
Uses of Testosterone:
• As a replacement therapy in male hypogonadial disordered.
• To stimulate erythropoiesis (anemia)
• To treat male infertility
• In treatment of gynaecomastia
• In female:
• To treat menopausal symptoms.
• In the treatment of chronic mastitis.
• For suppression of lactation.
• For relief of after pain in labour.
• Treatment of breast cancer.
Pharmaceutical dosage
forms: Testosterone injection, implants
Brand names:
Testoform, Testoviron depot, Hormondirn, PMT
NANDROLONE
Properties of Nandrolone:
• It is creamy white crystalline powder.
• It differs from testosterone in not having methyl group ar
C10.
• It is orally not active.
Storage and stability:
It is stored in well closed –light resistant containers.
Uses: As under
testosterone.
Pharmaceutical dosage
forms: Nandrolone injection
Brand names:
Durabolin, Nandrolin, Deubolin
OESTARADIOL
Properties of Oestaradiol:
• It occurs as creamy white crystalline powder.
• It is odourless.
• It is practically insoluble in water.
• It is sparingly soluble in vegetable oil and in acetone.
Storage and stability:
It is stored in well closed –light resistant containers.
Uses of Oestaradiol:
• In hormones replacement therapy in females after menopause
or overiectomy.
• To treat menopausal symptoms.
• To treat primary onset amenorrhea delayed onset of
puberty.
• To treat breast cancer in post-menopausal women.
• To treat prostatic carcinoma in men.
Pharmaceutical dosage
forms: Oestradiol injection
Brand names:
Ovocept, Aprocrine
PROGESTERONE
• It contains steroidal nucleus viz .Pregnane.
• The different groups present are:
1. Two oxo groups
at C3 and C20.
2. Double bond
between C4 and C5.
Properties of Progesterone:
• It occurs as colorless crystals or white or slightly
yellowish white powder.
• It is odourless.
• It is practically insoluble in water.
• It is freely soluble in alcohol.
• It shows polymorphism.
Storage and
stability: It is stable in air but is affected by light .Hence stored in
well closed –light resistant containers.
Uses of Progesterone:
• To treat dysfunctional uterine bleeding, dysmenorrhoea and
endometriosis.
• To treat habitual or threatened abortions.
• To maintain the pregnancy.
• To treat cancer of breast and endometrium.
• For prophylaxis of postnatal depression. (Sudden decrease
the level of progesterone after delivery.
Pharmaceutical dosage
forms: Progesterone implants
Brand names:
Proluton, Proluton depot, Progestin, Menstrogen.
Glucocorticoids
CORTISONE
• It is pregnane (steroid nucleus) which contains:
• Here oxo group at C13, C11 and C20
• Two hydroxyl groups at C17 and C21
• A double bond between C4 and C5
Properties of Cortisone:
• It is white creamy white crystalline powder.
• It is odourless.
• It is very slightly soluble in water.
• It is freely soluble in alcohol.
Storage and
stability: It is stable in air but is affected by light .Hence stored in
well closed –light resistant containers.
Uses of Cortisone:
• Replacement therapy in adrenocortical failure or
hypopituitarism (low production of hydrocortisone or aldosterone.
• To treat asthma and other respiratory tract disease.
• To treat allergic and other anaphylactic reaction.
• To treat disease of connective tissue like rheumatism,
rheumatoid arthritis etc.
• Collagen disease like lumps erythematosus
• To prevent the hypercalcemia.
Pharmaceutical dosage
forms: Cortisone acetate injection, Cortisone acetate tablets
Brand names:
Cortin, Otek, Cotaryl-H
HYDROCORTISONE
/ (CORTISOL)
• It differs from cortisone in having hydroxyl group
instated of oxo group at C11.
Properties of
Hydrocortisone:
• Its occurs white crystalline powder.
• It is odourless.
• It is practically in soluble in water.
• It is sparingly soluble in alcohol.
Storage and
stability: It is stored in well closed –light resistant containers.
Uses: Under
cortisone but more potent.
Pharmaceutical dosage
forms: Hydrocortisone acetate injection, tablets, cream, ointment,
suppository, Hydrocortisone and neomycin eye drops.
Brand names: Cort
–S, Nebacortril, Tetracortil
PREDNISOLONE
Properties of Prednisolone:
• Its occurs white crystalline powder.
• It is odorless.
• It is hygroscopic in nature.
• It is very slightly soluble in water.
• It is soluble in alcohol dioxan and methyl alcohol.
Storage and
stability: It is stored in well closed –light resistant containers.
Uses of Prednisolone:
• Refer use 1, 2 4 under cortisone
• To treat the disease like:
• Hepatic necrosis. Acute hepatic failure.
• G.I tract ulcerative colitis, inflammatory bowel disease.
• Inflammation of eye.
• To treat blood disordered and malignancies e.g. hemolytic
anemia.
• Treatment of cancer.
Pharmaceutical dosage
forms: Prednisolone tablets, eye drops, injection, and enema.
Brand names:
Histocortin, Prednisol, Prednisol-N
BETAMETHASONE
Properties of Betamethasone:
• It occurs as white or creamy white powder.
• It is odourless.
• It is very slightly soluble in water.
• It is sparingly soluble in alcohol.
Storage and
stability: It is stored in well closed –light resistant containers.
Uses of Betamethasone:
• Topically it is used:
• To control all form of eczema.
• To treat sever acute photosensitive reaction including
sunburn.
• To treat certain forms of psoriasis.
• To treat acute contact dermatitis.
• Used in the defective skin pigmentation
• By Inhalation:
• It is used to control the asthma.
• To treat disease of connective tissue like rheumatism,
rheumatoid arthritis etc.
Pharmaceutical dosage
forms: Betamethasone tablets, eye drops, injection.
Brand names:
Betnovate, Betenesol, Betacortril, A-cort.