Ospemifene Oral Tablets - Uses, Contraindications, and Side Effects

Introduction

Dyspareunia or genital pain occurring before, during, or after intercourse can cause significant effects on the physical as well as mental health of the individual, affecting the quality of life. It is a complex disorder but commonly seen in females, especially after menopause. It can be further classified as superficial or deep and primary or secondary. Vulvar and vaginal atrophy (thinning and inflammation of the vaginal walls) is a common but underreported condition that some women most commonly experience during the postmenopausal phase. It is associated with irritation, soreness, dryness, and dyspareunia with urgent urinary frequency and incontinence.

What Are Ospemifene Oral Tablets?

Ospemifene oral tablets are recommended in the management of vaginal dryness and moderate to severe dyspareunia after menopause. Vaginal dryness and dyspareunia are symptoms of vulvar and vaginal atrophy that may occur in some females due to menopause. Ospemifene is an estrogen agonist/antagonist (hormone) that has agonistic effects on the inner lining of the uterus (endometrium). It was approved by the United States Food and Drug Administration (USFDA) in 2013. Ospemifene tablets act by replacing the estrogen that is naturally produced in the body. However, this drug must be used for the shortest possible duration to be consistent with treatment goals and to prevent any risks to the individual.

How Is the Ospemifene Tablet Taken?

Ospemifene tablets are recommended at 60 mg and must be taken orally daily with food. It is preferable to take around the same time daily. The instructions given by the doctor or on the prescription label must be followed exactly and not be taken more or less. If a dose is missed, it must be taken as soon as remembered, but if it is almost time for the next dose, the missed dose can be skipped, and the normal dosing schedule can be followed. Ospemifene tablets only help to control the symptoms of the condition but do not completely cure it. The doctor will periodically evaluate the patient to determine the necessity of the treatment and advise accordingly. Therefore, the medication must be continued even if the patient feels well and must not be stopped without a doctor’s consultation.

What Are the Contraindications of Ospemifene Oral Tablets?

The contraindications of Ospemifene oral tablets include:

• Allergy or hypersensitivity to Ospemifene or any of its components.

• Animal studies have reported a risk to the fetus and labor difficulties during the administration of Ospemifene. Therefore, this drug is contraindicated in pregnant women or women of childbearing potential as it may cause fetal harm.

• Ospemifene is contraindicated in cases of undiagnosed or abnormal genital bleeding and in patients with known or suspected estrogen-dependent malignancies such as breast cancer, uterine cancer, or ovarian cancer.

• Ospemifene is not recommended in patients with pulmonary embolism (blood clot in the lungs), deep-vein thrombosis (blood clot in the deep veins, usually legs), cardiovascular diseases such as myocardial infarction (MI), stroke, or a history of these conditions.

What Are the Side Effects of Ospemifene Oral Tablets?

The possible side effects of Ospemifene oral tablets include:

• Muscle spasms.

• Hot flushes (sudden feeling of warmth).

• Vaginal discharge.

• Excessive sweating.

Ospemifene oral tablets can also cause some serious side effects, such as:

• Itching and rash.

• Hoarseness.

• Swelling of the face, tongue, throat, hands, and legs.

• Difficulty breathing or swallowing.

How Effective Are Ospemifene Tablets?

Clinical trials, including a 52-week long-term trial and three 12-week trials, were conducted to determine the safety and efficacy of Ospemifene tablets, respectively. It included females between 41 to 81 years of age with at least one moderate to severe vaginal symptom that was bothering during intercourse, with a vaginal pH of more than 5 and superficial cells on the vaginal smear of less than five percent. The results after the end of trials were that a significant improvement was observed in the symptoms of dyspareunia and vaginal dryness, a mean reduction in the vaginal pH, and a decrease in the superficial cells on the vaginal smear. These studies suggested that Ospemifene tablets are safe and have minimal impact on the endometrium.

What Must the Patient Inform the Doctor Before Taking Ospemifene Tablets?

• Patients must inform the doctor if they are allergic to Ospemifene or any other medications before starting the treatment.

• The doctor must be informed if the patient is taking vitamins, nutritional supplements, over-the-counter (OTC) drugs, medications such as Ketoconazole, Itraconazole, Flucanozole, Rifampin, Tamoxifen, Clarithromycin, or any other medicines before taking Ospemifene to modify the dosage or monitor for any side effects.

• Patients must inform the doctor that they take Ospemifene before surgery or dental procedures.

• Female patients must inform the doctor if they are breastfeeding, pregnant, or planning to become pregnant before starting treatment with Ospemifene, as it can harm the fetus.

What Are the Precautions to Be Followed While Taking Ospemifene Tablets?

• Ospemifene has an increased potential to cause endometrial cancer (uterine cancer) in women. Hence, the patients must inform the doctor if they have previously experienced abnormal vaginal bleeding or during the treatment.

• Ospemifene tablets can cause an increased risk of blood clots or stroke. Therefore, patients must inform the doctor if they smoke, have high blood pressure, diabetes, uncontrolled cholesterol levels, have heart disease, liver diseases, or any other medical conditions before starting treatment with Ospemifene tablets.

• The healthcare provider periodically monitors the patient (every three to six months) to discuss the continuation of the treatment.

• The patient must inform the doctor immediately in case of serious side effects and may stop taking the medication.

• Ospemifene tablets can cause or increase the occurrence of hot flashes; a doctor can be consulted to manage the concern.

Conclusion

Ospemifene tablet is a prescription medicine that belongs to a group of drugs called selective estrogen receptor modulators (SERM) and is used in the treatment of vaginal dryness and dyspareunia in postmenopausal women. Though various studies have regarded the drug as safe and efficient, it can increase the risk of uterine cancer and stroke. Therefore, a healthcare provider must be consulted before taking such medications. Further studies with more subjects may be necessary to conclude Ospemifene tablets' long-term safety and efficacy.