Description

Premarin Vaginal Cream is a hormone medication used to treat vaginal symptoms of menopause, such as dryness, burning, and painful intercourse. Some key points:Premarin Vaginal Cream helps rebuild vaginal tissue and makes moderate to severe painful sex after menopause more comfortable. It is applied directly inside the vagina, which helps reduce vaginal symptoms with less overall estrogen absorption compared to oral or transdermal estrogens.The recommended dosing is 0.5 g applied twice weekly or 0.5 g once daily (21 days on, 7 days off). Premarin Vaginal Cream should be used at the lowest effective dose for the shortest duration.There are some serious risks associated with estrogen therapy, including increased risk of endometrial cancer, stroke, deep vein thrombosis, and dementia in older women. Patients should be monitored closely and diagnostic measures undertaken to rule out malignancy.

Composition and Mechanism of Action

Premarin Vaginal Cream contains conjugated estrogens derived from natural sources, primarily the urine of pregnant mares. The estrogens help rebuild and maintain vaginal tissue, reducing symptoms of vaginal atrophy caused by low estrogen levels after menopause.

Indications and Usage

Premarin Vaginal Cream is indicated for the treatment of moderate to severe vaginal dryness, irritation, and painful intercourse (dyspareunia) due to menopause. It is applied directly into the vagina, allowing for localized action with lower systemic absorption compared to oral or transdermal estrogens.

Dosage and Administration

The recommended dosage is 0.5 g of Premarin Vaginal Cream inserted into the vagina twice weekly or 0.5 g once daily for 21 days, followed by 7 days off. The lowest effective dose should be used for the shortest duration to achieve treatment goals and minimize risks.

Risks and Precautions

Estrogen therapy, including Premarin Vaginal Cream, is associated with serious risks such as endometrial cancer, stroke, deep vein thrombosis, and dementia in older women. Patients should be closely monitored, and diagnostic measures should be undertaken to rule out malignancy. Premarin Vaginal Cream should be used with caution in patients with a history of breast cancer or cardiovascular disease.

Conclusion

Premarin Vaginal Cream can be an effective treatment for vaginal symptoms of menopause when used as directed by a healthcare provider. However, the risks and benefits should be carefully considered for each individual patient, and the lowest effective dose should be used for the shortest duration possible.

Key Benefits of Premarin Vaginal Cream

• Treats moderate to severe vaginal dryness, irritation, and painful intercourse due to menopause
• Helps rebuild and maintain vaginal tissue
• Provides localized action with lower systemic absorption compared to oral or transdermal estrogens

Key Ingredients in Premarin Vaginal Cream

• Conjugated estrogens derived from natural sources, primarily the urine of pregnant mares
• Mixture of sodium estrone sulfate and sodium equilin sulfate
• Other components including sodium sulfate conjugates: 17 α-dihydroequilin, 17 α-estradiol, and 17 β-dihydroequilin
• Excipients such as cetyl esters wax, cetyl alcohol, white wax, glyceryl monostearate, propylene glycol monostearate, methyl stearate, benzyl alcohol, sodium lauryl sulfate, glycerin, and mineral oil

Premarin Vaginal Cream contains 0.625 mg conjugated estrogens per gram of cream.                         

Mechanism of Action of Premarin Vaginal Cream

Premarin Vaginal Cream contains a mixture of conjugated estrogens derived from natural sources, primarily the urine of pregnant mares. The estrogens help rebuild and maintain vaginal tissue, reducing symptoms of vaginal atrophy caused by low estrogen levels after menopause.The mechanism of action involves:

• Circulating estrogens modulating the pituitary secretion of gonadotropins, luteinizing hormone (LH) and follicle stimulating hormone (FSH), through a negative feedback mechanism.
• Estrogens entering target tissues and binding to nuclear receptors, which in turn modulate the transcription and translation of target genes, resulting in the characteristic estrogenic effects.
• Locally applied estrogens in the vagina helping rebuild vaginal tissue and reduce symptoms of vaginal dryness, irritation, and painful intercourse.

By providing localized estrogen therapy, Premarin Vaginal Cream helps relieve moderate to severe vaginal symptoms of menopause with lower systemic absorption compared to oral or transdermal estrogens.                                                                                                                                            Sodium Estrone Sulfate

• Molecular Formula: C₁₈H₂₂NaO₅S
• Molecular Structure:
  \ce{C18H22NaO5S}

Sodium Equilin Sulfate

• Molecular Formula: C₁₈H₂₀NaO₅S
• Molecular Structure:
  \ce{C18H20NaO5S}

The cream also contains other conjugated estrogen components such as:

• 17α-Dihydroequilin Sodium Sulfate
• 17α-Estradiol Sodium Sulfate
• 17β-Dihydroequilin Sodium Sulfate

Conjugated system

Chemical structure in molecules

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Definition

A system of connected p-orbitals with delocalized electrons that lowers the overall energy and increases stability of a molecule.

Key Features

Characterized by alternating single and multiple bonds. Can include lone pairs, radicals, or carbenium ions. May be cyclic, acyclic, linear, or mixed.

Conjugation Mechanism

Involves the overlap of one p-orbital with another across an adjacent sigma bond. In transition metals, d-orbitals can be involved.

Dosage Range

• The lowest dose that will control symptoms should be chosen.
• Low Dose Premarin® Vaginal Cream (0.5 g) is administered intravaginally or topically twice-weekly (e.g., Monday and Thursday).
• Maximum Recommended Dose: Premarin® Vaginal Cream is administered intravaginally or topically in a cyclic regimen (daily for 21 days and then off for 7 days). Generally, women should be started at the 0.5 g daily dosage strength. Dosage adjustments (0.5 to 2 g) may be made based on individual response.

Storage

• Please refer to the outer carton for storage conditions.

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