Anti-Androgenic Drugs

Finasteride is a competitive inhibitor of the enzyme 5-alpha reductase which is responsible for the conversion of testosterone into a more active dihydrotestosterone responsible for the androgen action.

When used in benign prostatic hypertrophy, it reduces the prostate size and increased peak urinary flow rate.

It is also used in male pattern baldness and as a palliative treatment in prostatic carcinoma.

Ref: K D Tripathi Textbook of Pharmacology, 5th Edition, Page 272

Ans. is ‘c’ i.e., Spironolactone

o Spironolactone and eplerenone are the aldosterone antagonists. They are used as potassium sparing diuretics. Their diurectic effect is quite feeble, but in CHF these drugs reduce the mortality (at doses lower than diuretic doses) by antagonizing the effect of aldosterone (reversal of remodelling). Spironolactone also possesses anti- androgenic effects.

Ans. is ‘b’ i.e., Androgen receptors

Ans. is ‘b’ i.e., Cyproterone acetate

D i.e. Cyproterone acetate

Cyproterone acetate is a progestin and a weak anti androgen by virtue of binding to the androgen receptor (i.e. progestational antiandrogen that blocks androgen receptor). Because of antiandrogen action, it is efective in conditions like acne seborrhoea, hirsutism, female pattern hair loss (androgenetic hair loss in females), hidreadinitis suppurativaQ -i.e. conditions caused or aggravated by androgenic hormones.

–        Cyproterone acetate (CPA) is effective in treatment of acne as it reduces sebum production (dose dependent) & comedogenesis. In premenopausal women it is usually combined with ethinyloestradiol (Dianette & estelle 35) or other oral contraceptive agents to regulate menstrual cycle irregularitiesQ (caused by high dose cyproterone) and prevent pregnancy (d/t concerns of feminising effects of cyproterone on male fetus). Whereas, in postmenopausal women, it is not necessary to combine ethinyl oestradiol (EOD) with CPA.

Reverse sequential regimen (CPA 100 mg / day on days 5 to 15, and EOD 30-50 mg /day on cycle days 5to 26) regulates menstrual bleeding, provides excellent contraception and is effective in treatment of even severe hirsutism and acneQ. Acne usually improves 40-50% by 3^rd and 80-90% by 9^th cycle.

Ans. is ‘c’ i.e. It blocks the conversion of dihydrotestosterone to testosterone 

• Finasteride is a 5 a-reductase inhibitor which blocks the conversion of testosterone to its more active form dihydrotestosterone
• Uses
• BPH – decreases the size of large prostate (> 40 cm³) and can retard disease progression.
• Male pattern baldness – in patients of male pattern baldness, it promotes hair growth and prevents further hair loss.

Ans. is ‘c’ i.e., Conservative treatment 

Ans: D i.e. Finasteride

Drugs and uses

• Cyproterone has been clinically tested in precocious puberty in boys, inappropriate sexual behaviour in men, acne and virilisation in women, but is not marketed.
• Danazol is useful in endometriosis, menorrhagia, fibrocystic breast disease and hereditary angioneurotic edema.
• Bicalutamide (more potent and longer acting congener of flutamide) is suitable for once daily administration in metastatic carcinoma of prostrate.
• Treatmentt with finasteride has resulted in decreased prostate size and increased peak urinary flow rate in nearly 50% patients with symptomatic benign hypertrophy of the prostrate (BHP). It is the only drug which can retard disease progression.

Ans. is ‘b’ i.e., Prostate

Flutamide

• It is a nonsteroidal drug.
• Has antiandrogenic but no other hormonal activity.
• Its active metabolite 2-hydroxyflutamide competitively blocks androgen action on accessory sex organs as well as on pituitary – inceases LH secretion by blocking feed back inhibition – testosterone secretion increases which partially overcome the direct antiandrogenic action.
• It is used in metastatic prostatic carcinoma.
• It is better used in conjuction with GnRH agonist to suppress LH and testosterone secretion.
• Reports of liver damage have restricted its use.

Ans. is ‘a’ i.e., Cyproterone acetate

• Combined with ethinyl estrodiol, cyproterone acetate comes as combination form of birth control pill prescribed to women for its antiandrogenic effect to treat :‑

1. Hair loss (female pattern).
2. Acne
3. Hirsutism
4. Seborrhoea
5. Hidradenitis suppurativa