Clomiphene Citrate: Uses, Side Effects, Dosage & FAQs

Clomiphene citrate is a nonsteroidal drug for fertility in females. It acts on the hypothalamus, pituitary gland, and ovary to increase follicle-stimulating hormone levels (FSH) and luteinizing hormone. Increased levels of these hormones improve the chances of growing an ovarian follicle that can then trigger ovulation.

It is used to treat infertility in women. This drug is not recommended for women whose ovaries no longer produce eggs properly.

Clomiphene Citrate is a white to light yellow crystalline powder that is practically odorless. It is freely soluble in methanol; soluble in ethanol; sparingly soluble in acetone, water, and chloroform; and insoluble in ether. 

Clomiphene is a non-steroidal fertility drug. It causes the pituitary gland to release the hormones necessary to stimulate ovulation. [1]

Ovulation is the process of releasing an egg from the ovary. 

Clomiphene is used to cause ovulation in women with certain conditions (such as polycystic ovary syndrome) that prevent natural ovulation.

Different Brands

  • Clomid
  • Milophene
  • Serophene

Important

Avoid clomiphene if you are already pregnant. Also, Do not use Clomiphene if you have: liver disease, unexplained abnormal vaginal bleeding, uncontrolled thyroid or adrenal disease, an ovarian cyst (not related to polycystic ovary syndrome), or are pregnant.

Another important thing is that Clomiphene can pass into breast milk and harm a nursing baby. This medicine can slow down the production of breast milk in some women. Tell your doctor if you are breastfeeding a baby.

Before taking this medicine

  • Avoid using clomiphene citrate if you are allergic c to it or any other ingredients present in the formulation.
  • If you have abnormal bleeding from your vagina (unexplained bleeding).
  • It should not be used in patients with ovarian enlargement except those with polycystic ovary syndrome.
  • Also, don’t take clomiphene citrate if you have previous or current liver disease;
  • All those who a pituitary gland or other brain tumor;
  • It is important to note that avoid the use of this medicine if you are pregnant.

Clomiphene citrate Side Effects

At a recommended dose, the clomiphene citrate is tolerated well and should not cause any side effects. However, as we know with every medicine, there must be some side effects associated. The adverse effects are usually mild and transient, and most will disappear promptly after treatment is discontinued.

Adverse effects (Occur in less than 1% of patients in clinical trials)

  • Constipation
  • Acute abdomen
  • Increase appetite
  • Depression
  • Dermatitis
  • Dizziness
  • Diarrhea
  • Fatigue
  • Increase urinary frequency
  • Hair loss
  • Insomnia
  • Nervous tension
  • Lightheadedness
  • Vaginal dryness
  • Ovarian enlargement
  • Breast discomfort

Please keep in mind that this is not a complete list of adverse effects. It may also cause side effects. Please consult your doctor if you feel other effects.

Frequent (more than three treatment cycles) use of this medicine may also increase the risk of developing an ovarian tumor.

Higher doses of Clomiphene can also cause irreversible visual disturbances, or a condition called ovarian hyperstimulation syndrome (OHSS). It is a life-threatening condition, and the symptoms of OHSS are;

  • Nausea,
  • Abdominal pain,
  • Weight gain,
  • Gas, and
  • Shortness of breath.

Fertility treatment can increase the likelihood of multiple births (twins, triplets). These are high-risk pregnancies for both the mother and the babies.

Clomiphene Dose

The usual recommended dose of clomiphene citrate is 50-250 mg per day for five days from day 2, 3, 4, or 5 of spontaneous use or induced bleeding. 

Start with the lowest dose and increase the dose in increments of 50 mg/day per cycle until ovulation is achieved. The dose should be increased only in those females who do not ovulate in response to cyclic 50 mg clomiphene.

It is important to note that the usual recommended dose is 50mg per day.

What happens if I overdose with Clomiphene citrate?

The incidence of overdose has not been reported till now. However, if you overdose on these drugs you may show some signs and symptoms like nausea, vomiting, visual blurring, vasomotor flushes, scotomata, spots or flashes, ovarian enlargement with pelvic or abdominal pain. 

Please don’t use more than the doctor recommended dose as it will not improve your symptoms; instead, it may cause severe adverse reactions. 

Store Clomiphene at room temperature and away from heat and direct sunlight. Do not refrigerate this medicine.

How Clomiphene Works?

Clomiphene has both estrogenic and antiestrogenic properties, but the exact mechanism of action has not been determined.

First, it binds to estrogen receptors. After that, the hypothalamus falsely perceives a low estrogen state and sends a signal to the pituitary to release more FSH (follicle stimulating hormones) is needed to make the follicle grow.

Clomiphene citrate encounters the release of gonadotropins, follicle-stimulating hormone (FSH), and luteinizing hormone (LH), which leads to the development and proliferation of ovarian follicles, ovulation, and subsequent development and function of the corpus luteum, thus resulting in pregnancy.

Clomiphene citrate can interact with tissues that contain estrogen receptors, including the hypothalamus, pituitary, ovary, endometrium, vagina, and cervix. It may fight estrogen for estrogen receptor binding sites and can delay replenishment from intracellular estrogen receptors. Clomiphene citrate initiates some endocrine events.

Clomiphene Contraindication

Clomifene is contraindicated in the following conditions.

  • It is contraindicated in people with hypersensitivity reaction or allergy to clomiphene citrate or other ingredients present in the formulation.
  • It is also contraindicated in people with liver diseases or a history of liver dysfunction.
  • It is a category X drug and should not be used in pregnant women.
  • It is contraindicated in patients with abnormal and unexplained uterine bleeding.
  • Should be avoided in people with ovarian cysts or enlargement not due to polycystic ovarian syndrome.
  • It is also contraindicated in people with pre-existing mental depression or
  • thrombophlebitis because of the risk of exacerbation. 
  • Clomiphene citrate is also contraindicated in other conditions like uncontrolled thyroid or adrenal dysfunction or a pituitary tumor etc.

Multiple Pregnancies: Treatment with this drug increases the chances of multiple pregnancies. Possible complications and risks of multiple attacks should be discussed with the patient.

Pharmacokinetics

Clomiphene citrate absorbs well after oral administration. It is metabolized in the liver and excreted via the bile.

Most of the drug is excreted through feces. For oral drugs, 50% of excretion is through feces and urinary tracts, while in the case of the intravenous route, around 37% excreted through this route. A small amount of unchanged clomifene is excreted through urine. 

The biological half-life of this drug is about 5 days although traces are found in the feces for up to 40-45 days.

Frequently Asked Questions

1. How long does it usually take to get pregnant on Clomid?

Most of the women who use Clomiphene will ovulate after 7 to 10 days. Depending on the Clomiphene protocol you are using, this means that if you want to have sex every day or every other day, start on days 11-21 of your cycle.

2. Is Clomiphene safe to use in pregnancy and breastfeeding?

No

3. Is it safe to drive or operate heavy machinery when using Clomiphene?

This drug may cause visual symptoms and may affect your driving or operating machinery. If you feel drowsy, dizzy, or a headache as a side effect when using Clomiphene, then it may not be safe to drive a vehicle or operate heavy machinery.

4. What happens if I miss the dose of clomiphene citrate?

Take the missed dose as soon as you remember it. If it is time for the next dose, skip the missed dose and resume your dosing schedule. 

 5. What happens if I take expired clomiphene citrate?

Taking a single dose of this medicine might not cause any side effects, but still, it is recommended to discuss with your doctors or pharmacist.

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