CLOMID
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CLOMID (CLOMID).
Competitive antagonist of estrogen receptors (ER) in hypothalamus and pituitary, leading to increased gonadotropin-releasing hormone (GnRH) and subsequent LH and FSH release, stimulating ovulation.
| Metabolism | Hepatic via CYP3A4 and CYP2D6; undergoes enterohepatic circulation; terminal half-life ~5-7 days |
| Excretion | Primarily hepatic metabolism; metabolites excreted in feces (42%) and urine (8% unchanged). |
| Half-life | Terminal half-life is 5–7 days for zuclomiphene (active isomer), with prolonged elimination due to enterohepatic recirculation. |
| Protein binding | Highly protein bound (>99%), primarily to albumin. |
| Volume of Distribution | Not well-characterized; limited data suggest a large Vd (>100 L) due to extensive tissue distribution. |
| Bioavailability | Oral bioavailability is approximately 50% due to first-pass metabolism. |
| Onset of Action | Oral: Ovulation induction occurs 5–10 days after a 5-day course; peak effect on days 10–12. |
| Duration of Action | Effects persist for up to 6 weeks after a single course due to slow clearance of active isomer. |
| Action Class | Cephalosporins: 3 generation |
| Brand Substitutes | Cefo 100mg Tablet, Zeefix 100mg Tablet, Omfix 100mg Tablet, Lyxim 100mg Tablet, Cefocef O 100mg Tablet, Cefilab 200 Tablet, Cefix 200 Tablet, Mahacef 200 Tablet, Cefi 200 Tablet, Ceftas 200 Tablet |
50 mg orally once daily for 5 days, starting on day 5 of the menstrual cycle. May increase to 100 mg daily if no response.
| Dosage form | TABLET |
| Renal impairment | No specific adjustment required; use caution in severe impairment (CrCl <30 mL/min) as data limited. |
| Liver impairment | Contraindicated in severe hepatic impairment (Child-Pugh class C). For mild to moderate impairment, no adjustment recommended, but monitor liver function. |
| Pediatric use | Not indicated for use in children; safety and efficacy not established. |
| Geriatric use | Not indicated for postmenopausal women. Use not recommended in elderly due to lack of efficacy in anovulation. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CLOMID (CLOMID).
| Breastfeeding | Safety in breastfeeding is not established. Clomiphene may reduce milk production. The M/P ratio is unknown. It is generally not recommended during breastfeeding. |
| Teratogenic Risk | Clomiphene citrate is contraindicated in pregnancy. It is associated with an increased risk of fetal malformations, including neural tube defects, specifically when exposure occurs during the first trimester. Second and third trimester risks are not well studied due to contraindication, but theoretical risks include ovarian hyperstimulation syndrome (OHSS) effects on pregnancy. |
■ FDA Black Box Warning
None
| Serious Effects |
["Pregnancy (Category X)","Liver disease or dysfunction","Undiagnosed abnormal vaginal bleeding","Ovarian cyst or enlargement not due to polycystic ovary syndrome","Hypersensitivity to clomiphene or components"]
| Precautions | ["Ovarian hyperstimulation syndrome (OHSS)","Ovarian enlargement","Visual disturbances (especially with prolonged use)","Multiple pregnancy (increased risk)","Ectopic pregnancy","Ovarian cancer risk (theoretical, based on prolonged use)"] |
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| Fetal Monitoring |
| Monitor for ovarian enlargement, multiple gestation, OHSS. Perform pregnancy test prior to each treatment cycle. Ultrasound monitoring for follicular development and endometrial thickness. If pregnancy occurs, monitor for multiple gestation and congenital anomalies. |
| Fertility Effects | Clomiphene is an ovulatory stimulant used for anovulatory infertility. It can cause multiple follicular development leading to multiple gestations. Long-term use may increase risk of low-grade ovarian tumors; not recommended for more than 6 cycles without evaluation. |