Bromocriptine and other dopaminergic drugs and Drugs affecting gonadotrophins

Bromocriptine and other dopaminergic drugs

BROMOCRIPTINE:

Indications: Prevention or suppression of lactation, Hypogonadism, galactorrhoea, infertility, Acromegaly, Prolactinoma and Parkinsonism.

Contraindications: should not be used in patients with a hypersensitivity to ergot alkaloids. They should also be avoided in pre-eclampsia.

Dose and Administration: Prevention or suppression of lactation, 2.5 mg on day 1 (prevention) or daily for 2–3 days (suppression); then 2.5 mg twice daily for 14 days. Hypogonadism, galactorrhoea, infertility, initially 1–1.25 mg at bedtime, increased gradually; usual dose 7.5 mg daily in divided doses, increased if necessary to max. 30 mg daily, usual dose in infertility without hyperprolactinaemia, 2.5 mg twice daily. Acromegaly, initially 1–1.25 mg at bedtime, increase gradually to 5 mg every 6 hours. Prolactinoma, initially 1– 1.25 mg at bedtime; increased gradually to 5 mg every 6 hours. child under 15 years, not recommended.

LISURIDE MALEATE:

Indications: Prevention or suppression of prolactin, Hypogonadism, galactorrhoea, infertility, Acromegaly, Prolactinoma and Parkinsonism.

Contraindications: sever aterial circulatory disorders, coronary artery insufficiency.

Dose and Administration: dose 1-2mg per day.

CABERGOLINE:

Indications: Prevention or suppression of lactation, Hyperprolactinaemic disorders, Parkinsonism.

Contraindications: history of puerperal psychosis; exclude pregnancy before starting and discontinue 1 month before intended conception (ovulatory cycles persist for 6 months)—discontinue if pregnancy occurs during treatment, avoid breast-feeding if lactation prevention fails; history of pulmonary, pericardial, or retroperitoneal fibrotic disorders; cardiac valvulopathy.

Dose and Administration: Prevention of lactation, during first day postpartum, 1 mg as a single dose; suppression of established lactation, 250 micrograms every 12 hours for 2 days. Hyperprolactinaemic disorders, 500 micrograms weekly (as a single dose or as 2 divided doses on separate days) increased at monthly intervals in steps of 500 micrograms until optimal therapeutic response with monthly monitoring of serum prolactin levels; reduce initial dose and increase more gradually if patient intolerant; over 1 mg weekly give as divided doses; up to 4.5 mg weekly has been used in hyperprolactinaemic patients. child under 16 years, not recommended.

QUINAGOLIDE:

Indications: Prevention or suppression of lactation, Hyperprolactinaemic disorders.

Contraindications: hypersensitivity to quinagolide (but not ergot alkaloids); hepatic impairment, renal impairment and breast-feeding.

Dose and Administration: Hyperprolactinaemia, 25 micrograms at bedtime for 3 days; increased at intervals of 3 days in steps of 25 micrograms to usual maintenance dose of 75–150 micrograms daily; for doses higher than 300 micrograms daily increase in steps of 75–150 micrograms at intervals of not less than 4 weeks; child not recommended.

Drugs affecting gonadotrophins

CETRORELIX:

Indications: Premature Luteinizing Hormone Surges and adjunct in the treatment of female infertility.

Contraindications: pregnancy, breast-feeding, moderate renal impairment, and moderate hepatic impairment.

Dose and Administration: By subcutaneous injection into the lower abdominal wall, either 250 micrograms in the morning, starting on day 5 or 6 of ovarian

stimulation with gonadotrophins (or each evening starting on day 5 of ovarian stimulation); continue throughout administration of gonadotrophin including day of ovulation induction (or evening before ovulation induction). or 3 mg on day 7 of ovarian stimulation with gonadotrophins; if ovulation induction not possible on day 5 after 3-mg dose, additional 250 micrograms once daily until day of ovulation induction.

DANAZOL:

Indications: Endometriosis, Fibrocystic Breast Disease, Hereditary Angioedema Prevention, Gynecomastia, Menorrhagia, And Precocious Puberty.

Contraindications: pregnancy, ensure that patients with amenorrhoea are not pregnant; breast-feeding; severe hepatic, renal or cardiac impairment; thromboembolic disease; undiagnosed genital bleeding; androgen-dependent tumours; porphyria.

Dose and Administration: Endometriosis, 200–800 mg daily in up to 4 divided doses, adjusted to achieve amenorrhoea, usually for 3–6 months. Severe pain and tenderness in benign fibrocystic breast disease not responding to other treatment, 300 mg daily in divided doses usually for 3–6 months. Hereditary angioedema, initially 200 mg 2–3 times daily, then reduced according to response.

GANIRELIX:

Indications: adjunct in the treatment of female infertility.

Contraindications: pregnancy, breast-feeding, moderate renal impairment, and moderate hepatic impairment.

Dose and Administration: By subcutaneous injection preferably into the upper leg (rotate injection sites to prevent lipoatrophy), 250 micrograms in the morning (or each afternoon) starting on day 6 of ovarian stimulation with gonadotrophins; continue throughout administration of gonadotrophins including day of ovulation induction (if administering in afternoon, give last dose in afternoon before ovulation induction).

GOSERELIN:

Indications: Advanced Prostatic Carcinoma, Endometrial Ablation Adjunct, Endometriosis, Hormone Receptor Positive Breast Cancer, Prostatic Carcinoma.

Contraindications: Lactating Mother, Pregnancy, Bilateral Orchiectomy, Diabetes Mellitus, Hypercalcemia, Hyperglycemia, Urinary Tract Obstruction, And Vertebral Metastases.

Dose and Administration: By subcutaneous injection into anterior abdominal wall Endometriosis, 3.6 mg every 28 days; max. duration of treatment 6 months (do not repeat). Endometrial thinning before intra-uterine surgery, 3.6 mg (may be repeated after 28 days if uterus is large or to allow flexible surgical timing). Before surgery in women who have anaemia due to uterine fibroids, 3.6 mg every 28 days (with supplementary iron); max. duration of treatment 3 months. Pituitary desensitisation before induction of ovulation by gonadotrophins for in vitro fertilisation (under specialist supervision), after exclusion of pregnancy, 3.6 mg to achieve pituitary down-regulation (usually 1–3 weeks) then gonadotrophin is administered (stopping gonadotrophin on administration of chorionic gonadotrophin at appropriate stage of follicular development).

LEUPRORELIN ACETATE:

Indications: Endometriosis, Endometrial thinning before intra-uterine surgery, Reduction of size of uterine fibroids and of associated bleeding before surgery.

Contraindications: Lactating Mother, Pregnancy, Bilateral Orchiectomy, Diabetes Mellitus, Hypercalcemia, Hyperglycemia, Urinary Tract Obstruction, And Vertebral Metastases.

Dose and Administration: By subcutaneous or intramuscular injection, Endometriosis, 3.75 mg as a single dose in first 5 days of menstrual cycle then every month for max. 6 months (course not to be repeated). Endometrial thinning before intra-uterine surgery, 3.75 mg as a single dose (given between days 3 and 5 of menstrual cycle) 5–6 weeks before surgery. Reduction of size of uterine fibroids and of associated bleeding before surgery, 3.75 mg as a single dose every month usually for 3–4 months (max. 6 months). By intramuscular injection, Endometriosis, 11.25 mg as a single dose in first 5 days of menstrual cycle then every 3 months for max. 6 months (course not to be repeated).

TRIPTORELIN:

Indications: endometriosis, precocious puberty, reduction in size of uterine fibroids; advanced prostate cancer.

Contraindications: Lactating Mother, Pregnancy, Bilateral Orchiectomy, Diabetes Mellitus, Hypercalcemia, Hyperglycemia, Urinary Tract Obstruction, And Vertebral Metastases.

Dose and Administration: By intramuscular injection, endometriosis and reduction in size of uterine fibroids, 3 mg every 4 weeks starting during first 5 days of menstrual cycle; for uterine fibroids continue treatment for at least 3 months; max. duration of treatment 6 months (not to be repeated).