Dosing and uses of Clomid, Serophene (clomiphene)
Adult dosage forms and strengths
tablet
- 50mg
Treatment of Ovulatory Failure
50 mg PO qDay initially for 5 days
If no ovulation, treatment can be repeated as early as 30 days after previous therapy
Dosage can be increased to 100 mg only in patients who do not respond to first course
Monitor
Reassess diagnosis after 3 courses if ovulation has not occurred or if menses does not occur following ovulatory response
Pediatric dosage forms and strengths
Not used in children
Clomid, Serophene (clomiphene) adverse (side) effects
>10%
Ovarian enlargement (14%)
Vasomotor flushing (10%)
1-10%
Abdominal discomfort (6%)
Blurred vision (1.5%)
Breast discomfort (2%)
Nausea/vomiting (2%)
Postmarketing Reports
Body as a whole: Fever, tinnitus, weakness
Cardiovascular: Arrhythmia, chest pain, edema, hypertension, palpitation, phlebitis, pulmonary embolism, shortness of breath, tachycardia, thrombophlebitis
Central nervous system: Migraine headache, paresthesia, seizure, stroke, syncope
Dermatologic: Acne, allergic reaction, erythema, erythema multiforme, erythema nodosum, hypertrichosis, pruritus, urticaria
Genitourinary: Endometriosis, ovarian cyst (ovarian enlargement or cysts could, as such, be complicated by adnexal torsion), ovarian hemorrhage, tubal pregnancy, uterine hemorrhage
Hepatic: Transaminases increased, hepatitis
Musculoskeletal: Arthralgia, back pain, myalgia
Neoplasms: Liver (hepatic hemangiosarcoma, liver cell adenoma, hepatocellular carcinoma); breast (fibrocystic disease, breast carcinoma); endometrium (endometrial carcinoma); nervous system (astrocytoma, pituitary tumor, prolactinoma, neurofibromatosis, glioblastoma multiforme, brain abscess); ovary (luteoma of pregnancy, dermoid cyst of the ovary, ovarian carcinoma); trophoblastic (hydatiform mole, choriocarcinoma); miscellaneous (melanoma, myeloma, perianal cysts, renal cell carcinoma, Hodgkin’s lymphoma, tongue carcinoma, bladder carcinoma)
Psychiatric: Anxiety, irritability, mood changes, psychosis
Visual disorders: Abnormal accommodation, cataract, eye pain, macular edema, optic neuritis, photopsia, posterior vitreous detachment, retinal hemorrhage, retinal thrombosis, retinal vascular spasm, temporary or prolonged loss of vision, possibly irreversible.
Other: Leukocytosis, thyroid disorder
Fetal/neonatal anomalies
- Abnormal bone development: skeletal malformations of the skull, face, nasal passages, jaw, hand, limb (ectromelia including amelia, hemimelia, and phocomelia), foot (clubfoot), spine, and joints
- Cardiac abnormalities: septal heart defects, muscular ventricular septal defect, patent ductus arteriosus, tetralogy of Fallot, and coarctation of the aorta
- Chromosomal disorders: Downs syndrome
- Ear abnormalities and deafness
- Gastrointestinal tract abnormalities: cleft lip and palate, imperforate anus, tracheoesophageal fistula, diaphragmatic hernia, omphalocele
- Genitalia abnormalities: hypospadias, cloacal exstrophy
- Lung tissue malformations
- Malformations of the eye and lens (cataract)
- Neoplasms: neuroectodermal tumor, thyroid tumor, hepatoblastoma, lymphocytic leukemia
- Nervous system abnormalities: neural tube defects (anencephaly, meningomyelocele), microcephaly, and hydrocephalus
- Renal abnormalities: renal agenesis and renal dysgenesis
- Others: dwarfism, mental retardation
Warnings
Contraindications
Pregnancy
Liver disease
Undiagnosed abnormal uterine bleeding
Uncontrolled thyroid or adrenal dysfunction
Endometrial cancer
Ovarian cysts not due to PCOs
Cautions
Uterine fibroids, pituitary or ovarian failure
Risk of ovarian enlargement & ovarian hyperstimulation syndrome
Potential for multiple births, especially at 100 mg dosage
Risk of visual disturbance (like scotoma & photopsia)
Pregnancy and lactation
Pregnancy category: X
Lactation: It is not known whether clomiphene is excreted in human milk. Use with caution in nursing women. In some patients, clomiphene may reduce lactation.
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Clomid, Serophene (clomiphene)
Mechanism of action
Binds to estrogen receptors, induces ovulation by increase output of pituitary gonadotropins
Pharmacokinetics
Half-Life elimination: 5-7 days
Onset: Within 5-10 days
Peak plasma time 6.5 hours
Bioavailability: Readily absorbed from GI tract
Metabolism: Enterohepatically circulated
Excretion: feces 37-51%; small amount in urine
