Gale

Control of libido in severe hypersexuality &/or sexual deviation in adult male. Reduction of drive in sexual deviations in men when other interventions are considered inappropriate. Management of male patients w/ prostatic cancer to suppress "flare" w/ initial LH-releasing hormone (LHRH) analogue therapy; in long-term palliative treatment where LHRH analogues or surgery are contraindicated, not tolerated, or oral therapy is preferred; & in treatment of hot flushes in patients under treatment w/ LHRH analogues or who have had orchidectomy. Severe signs of androgenisation in women eg, very severe hirsutism, androgen-dependent severe loss of scalp hair eventually resulting in baldness (severe androgenic alopecia), often attended by severe forms of acne &/or seborrhoea.

Adult & elderly Control of libido in severe hypersexuality &/or sexual deviation Initially 50 mg bid after morning & evening meals. Maintain w/ lowest possible dose when satisfactory result has been achieved. Management of patients w/ prostatic cancer Max daily dose: 300 mg. Suppress "flare" w/ initial LHRH analogue therapy Initially 2 tab of 50 mg bid (200 mg) for 5-7 days as monotherapy, followed by 2 tab of 50 mg bid (200 mg) for 3-4 wk together w/ LHRH analogue therapy. Long term palliative treatment where LHRH analogues or surgery are contraindicated, not tolerated, or when oral therapy is preferred 200-300 mg daily divided into 2-3 doses daily. Hot flushes in patients under treatment w/ LHRH analogues or who have had orchidectomy Initially 50 mg w/ upward titration, if necessary, w/in the range 50-150 mg divided into 1-3 doses daily.

Should be taken with food.

Hypersensitivity. Malignant tumours other than prostatic cancer; wasting diseases (w/ exception of inoperable prostate carcinoma); severe diabetes w/ vascular changes; sickle-cell anaemia; severe chronic depression. History of or existing meningioma; thrombosis or embolism. Liver diseases (including Dubin-Johnson syndrome & Rotor syndrome). Youth <18 yr or those whose bone maturation & testicular maturation is incomplete.

Permanently stop treatment if patient is diagnosed w/ meningioma. W/draw treatment if hepatotoxicity is confirmed; severe upper abdominal complaints, liver enlargement or signs of intra-abdominal haemorrhage occur. Direct hepatic toxicity including jaundice, hepatitis & hepatic failure; liver tumours leading to life-threatening intra-abdominal haemorrhage. Increased risk of thromboembolic events & disease recurrence in patients w/ history of arterial or venous thrombotic/thromboembolic events (eg, DVT, pulmonary embolism, MI), CVA or advanced malignancies. Deterioration in patients w/ severe chronic depression. Shortness of breath accompanied by hypocapnia & compensatory alkalosis. Hypochromic anaemia/anaemia during long term treatment. -ve nitrogen balance at start of treatment. Medico-legal consideration. Single & multiple meningiomas at doses ≥25 mg; increased risk of meningiomas w/ increasing cumulative dose. Patients w/ history of thromboembolic disorders, or suffering from sickle-cell anaemia or severe diabetes w/ vascular changes. Perform LFTs pre-treatment, regularly during treatment & whenever any symptoms or signs suggestive of hepatotoxicity occur; blood counts before & at regular intervals during treatment. Monitor adrenocortical function regularly; signs of deterioration in patients w/ severe chronic depression; for meningiomas. Carefully examine carbohydrate metabolism in all diabetics before & regularly during treatment. Record spermatogram before starting treatment in patients of procreative age. Check RBC regularly during treatment. Not to be taken by patients w/ rare hereditary problems of galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption. May affect ability to drive & use machines. Not indicated for use in fertility, pregnancy & lactating women. Not to be given before conclusion of puberty. Not recommended for use in male childn & adolescents <18 yr.

Decreased libido, erectile dysfunction, reduced sexual drive & inhibition of gonadal function; reduced sperm count & vol of ejaculate. Wt gains in association w/ fluid retention; depressive moods, restlessness (temporary); dyspnoea; direct hepatic toxicity including jaundice, hepatitis & hepatic failure; gynaecomastia; hot flushes, sweating, fatigue, lassitude. Benign & malignant liver tumours.

Increased blood levels of thiazolidinediones (CYP2C8 substrates) ie, pioglitazone, rosiglitazone. Reduced effect w/ alcohol. Inhibited metabolism w/ ketoconazole, itraconazole, clotrimazole, ritonavir & other strong CYP3A4 inhibitors. Reduced levels w/ CYP3A4 inducers eg, rifampicin, phenytoin & products containing St. John's wort. Possible inhibition of cytochrome P450 enzymes CYP2C8, 2C9, 2C19, 3A4 & 2D6. Increased risk of statin-associated myopathy or rhabdomyolysis w/ HMG-CoA inhibitors (statins).

Other Drugs Affecting Hormonal Regulation / Cancer Hormone Therapy

G03HA01 - cyproterone ; Belongs to the class of antiandrogen preparations.

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