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.