CLOMIPHENE CITRATE

Indications and Dosage
Oral
Anovulatory infertility
Adult: 50 mg once daily for 5 days, starting on or around the 5th day of menstrual cycle if progestin-induced bleeding is planned or spontaneous uterine bleeding occurs before therapy, or at any time if there is no uterine bleeding. If ovulation does not occur after the 1st course, may give 100 mg once daily for 5 days, starting as early as 30 days after the previous course. Further treatment is not recommended if ovulation does not occur after 3 therapy courses or if pregnancy has not occurred within 3 ovulatory cycles. Long-term cyclic therapy (>6 cycles) is not recommended.
Hepatic Impairment
Contraindicated.
Administration
May be taken with or without food.
Contraindications
Abnormal uterine bleeding of unknown origin, uncontrolled thyroid or adrenal impairment, presence of an organic intracranial lesion (e.g. pituitary tumour), hormone-dependent tumours, ovarian cysts or enlargement not due to PCOS. Active liver disease or history of hepatic impairment. Pregnancy.
Special Precautions
Patient with uterine fibroids, PCOS, pre-existing or family history of hyperlipidaemia. Lactation.
Adverse Reactions
Significant: Ovarian hyperstimulation syndrome (OHSS), ovarian enlargement and cyst formation (high doses or prolonged treatment), visual disturbances (e.g. blurred vision, scintillating scotomata, phosphenes), multiple or ectopic pregnancy, new-onset or exacerbation of endometriosis; hypertriglyceridaemia, hypersensitivity reactions (including anaphylaxis and angioedema). Rarely, ovarian cancer.
Cardiac disorders: Tachycardia, palpitations.
Ear and labyrinth disorders: Vertigo.
Gastrointestinal disorders: Nausea, vomiting, abdominal symptoms or pelvic discomfort (e.g. distention, bloating, pain), pancreatitis.
General disorders and administration site conditions: Fatigue.
Investigations: Increased transaminases.
Nervous system disorders: Headache, dizziness, lightheadedness, paraesthesia, convulsions.
Psychiatric disorders: Nervousness, insomnia, depression, anxiety, mood disturbances.
Renal and urinary disorders: Increased urinary frequency or volume.
Reproductive system and breast disorders: Menorrhagia, breast discomfort, abnormal uterine haemorrhage.
Skin and subcutaneous tissue disorders: Rash, urticaria, dermatitis. Very rarely, alopecia.
Vascular disorders: Vasomotor flushes.
Patient Counseling Information
This drug may cause dizziness, lightheadedness or visual disturbances, if affected, do not drive or operate machinery.
Monitoring Parameters
Prior to therapy, obtain serum estrogen and triglycerides level; rule out primary pituitary or ovarian failure, endometriosis or endometrial carcinoma, adrenal and thyroid disorders, hyperprolactinaemia, and male factor infertility. Monitor ovulation by obtaining urinary LH, serum estradiol, and progesterone, and/or performing ultrasound. Perform pelvic exam and pregnancy test prior to each cycle of therapy. Assess for signs and symptoms of OHSS (e.g. severe abdominal pain or bloating, vomiting, diarrhoea, excessive weight gain, dyspnoea, or changes in urination).
Overdosage
Symptoms: Nausea, vomiting, vasomotor flushes, blurred vision, scotomata, ovarian enlargement with pelvic or abdominal pain. Management: Symptomatic and supportive treatment. Perform gastrointestinal decontamination.
Action
Description:
Mechanism of Action: Clomifene is a nonsteroidal compound with both estrogenic and anti-estrogenic effects. Its exact mechanism of action in inducing ovulation has not been determined; however, it appears to stimulate the release of pituitary gonadotropic hormones probably by inhibiting the negative feedback effect of estrogens at the receptor sites in the hypothalamus and pituitary.
Synonym: clomiphene.
Onset: 5-10 days after a course of treatment.
Pharmacokinetics:
Absorption: Readily absorbed from the gastrointestinal tract. Time to peak plasma concentration: Approx 6 hours.
Metabolism: Metabolised in the liver; undergoes enterohepatic recirculation.
Excretion: Mainly via faeces (42%); urine (8%). Elimination half-life: Approx 5 days.
Chemical Structure

Chemical Structure Image
Clomifene

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 1548955, Zuclomiphene. https://pubchem.ncbi.nlm.nih.gov/compound/Zuclomiphene. Accessed Apr. 28, 2023.
Storage
Store between 15-30°C. Protect from heat, light, and moisture.
ATC Classification
G03GB02 - clomifene ; Belongs to the class of synthetic agents used as ovulation stimulants.
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