Clomiphene Citrate Actions

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Actions of Clomiphene Citrate in details

The action of the drug on the human body is called Pharmacodynamics in Medical terminology. To produce its effect and to change the pathological process that is happening the body and to reduce the symptom or cure the disease, the medicine has to function in a specific way. The changes it does to the body at cellular level gives the desired result of treating a disease. Drugs act by stimulating or inhibiting a receptor or an enzyme or a protein most of the times. Medications are produced in such a way that the ingredients target the specific site and bring about chemical changes in the body that can stop or reverse the chemical reaction which is causing the disease.
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Clomiphene Citrate acts as a competitive inhibitor at oestrogen-receptors blocking their activation by endogenous oestrogen. Clomiphene Citrate competes with oestrogen on binding sites at hypothalamic level in which gonadotropins, follicle-stimulating hormone (FSH) and luteinizing hormone secretion are increased. These increase results in the maturation of the ovarian follicle and thus, the development and function of the Corpus luteum.

How should I take Clomiphene Citrate?

Take Clomiphene Citrate only as directed by your doctor. If you are to begin on Day 5, count the first day of your menstrual period as Day 1. Beginning on Day 5, take the correct dose every day for as many days as your doctor ordered. To help you to remember to take your dose of medicine, take it at the same time every day.

Dosing

The dose of Clomiphene Citrate will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of Clomiphene Citrate. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

Missed Dose

If you miss a dose of Clomiphene Citrate, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

If you do not remember until it is time for the next dose, take both doses together; then go back to your regular dosing schedule. If you miss more than one dose, check with your doctor.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Clomiphene Citrate administration

Administration of drug is important to know because the drug absorption and action varies depending on the route and time of administration of the drug. A medicine is prescribed before meals or after meals or along with meals. The specific timing of the drug intake about food is to increase its absorption and thus its efficacy. Few work well when taken in empty stomach and few medications need to be taken 1 or 2 hrs after the meal. A drug can be in the form of a tablet, a capsule which is the oral route of administration and the same can be in IV form which is used in specific cases. Other forms of drug administration can be a suppository in anal route or an inhalation route.
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The total daily dose should be taken at one time to maximize effectiveness (Dickey, 1996).

Clomiphene Citrate pharmacology

Pharmacokinetics of a drug can be defined as what body does to the drug after it is taken. The therapeutic result of the medicine depends upon the Pharmacokinetics of the drug. It deals with the time taken for the drug to be absorbed, metabolized, the process and chemical reactions involved in metabolism and about the excretion of the drug. All these factors are essential to deciding on the efficacy of the drug. Based on these pharmacokinetic principles, the ingredients, the Pharmaceutical company decides dose and route of administration. The concentration of the drug at the site of action which is proportional to therapeutic result inside the body depends on various pharmacokinetic reactions that occur in the body.

Action

Clomiphene Citrate tablets USP is a drug of considerable pharmacologic potency. With careful selection and proper management of the patient, Clomiphene Citrate tablets USP has been demonstrated to be a useful therapy for the anovulatory patient desiring pregnancy.

Clomiphene Citrate is capable of interacting with estrogen-receptor-containing tissues, including the hypothalamus, pituitary, ovary, endometrium, vagina, and cervix. It may compete with estrogen for estrogen-receptor-binding sites and may delay replenishment of intracellular estrogen receptors. Clomiphene Citrate initiates a series of endocrine events culminating in a preovulatory gonadotropin surge and subsequent follicular rupture. The first endocrine event in response to a course of Clomiphene Citrate therapy is an increase in the release of pituitary gonadotropins. This initiates steroidogenesis and folliculogenesis, resulting in growth of the ovarian follicle and an increase in the circulating level of estradiol. Following ovulation, plasma progesterone and estradiol rise and fall as they would in a normal ovulatory cycle.

Available data suggest that both the estrogenic and antiestrogenic properties of Clomiphene Citrate may participate in the initiation of ovulation. The two Clomiphene Citrate isomers have been found to have mixed estrogenic and antiestrogenic effects, which may vary from one species to another. Some data suggest that zuClomiphene has greater estrogenic activity than enClomiphene.

Clomiphene Citrate has no apparent progestational, androgenic, or antiandrogenic effects and does not appear to interfere with pituitary-adrenal or pituitary-thyroid function.

Although there is no evidence of a "carryover effect" of Clomiphene Citrate tablets USP, spontaneous ovulatory menses have been noted in some patients after Clomiphene Citrate tablets USP therapy.

Pharmacokinetics

Based on early studies with 14C-labeled Clomiphene Citrate, the drug was shown to be readily absorbed orally in humans and excreted principally in the feces. Cumulative urinary and fecal excretion of the 14C averaged about 50% of the oral dose and 37% of an intravenous dose after 5 days. Mean urinary excretion was approximately 8% with fecal excretion of about 42%.

Some 14C label was still present in the feces 6 weeks after administration. Subsequent single-dose studies in normal volunteers showed that zuClomiphene (cis) has a longer half-life than enClomiphene (trans). Detectable levels of zuClomiphene persisted for longer than a month in these subjects. This may be suggestive of stereo-specific enterohepatic recycling or sequestering of the zuClomiphene. Thus, it is possible that some active drug may remain in the body during early pregnancy in women who conceive in the menstrual cycle during Clomiphene Citrate tablets USP therapy.


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References

  1. NCIt. "Clomiphene: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).
  2. EPA DSStox. "Clomiphene: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).

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The results of a survey conducted on ndrugs.com for Clomiphene Citrate are given in detail below. The results of the survey conducted are based on the impressions and views of the website users and consumers taking Clomiphene Citrate. We implore you to kindly base your medical condition or therapeutic choices on the result or test conducted by a physician or licensed medical practitioners.

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Information checked by Dr. Sachin Kumar, MD Pharmacology

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