Usage
Dehydroepiandrosterone (DHEA) is prescribed for the treatment of vaginal atrophy in postmenopausal women. Its pharmacological classification is an endogenous steroid hormone. DHEA works by being converted into androgens and estrogens in the body. In the case of vaginal atrophy, the local conversion to estrogens helps to revitalize vaginal tissues.
Alternate Names
Dehydroepiandrosterone is also known as DHEA-S (Dehydroepiandrosterone sulfate), prasterone (specifically for intravaginal use), 3β-hydroxyandrost-5-en-17-one, 3β-hydroxy-5-androsten-17-one, and androstenolone. Intrarosa is a popular brand name for the intravaginal form of DHEA.
How It Works
Pharmacodynamics: DHEA is a precursor hormone that is converted into androgens and estrogens in peripheral tissues. The specific effects of DHEA depend on the type and amount of sex hormones produced by the conversion process. For instance, in vaginal atrophy, DHEA applied locally is primarily converted to estrogens, which improve vaginal tissue health.
Pharmacokinetics:
- Absorption: Orally administered DHEA is well-absorbed from the gastrointestinal tract. Intravaginally administered DHEA is absorbed locally into vaginal tissues.
- Metabolism: DHEA is rapidly metabolized in the liver and other peripheral tissues. It is converted to DHEA-S, which is further metabolized into androgens like testosterone and androstenedione, and estrogens like estrone and estradiol.
- Elimination: DHEA and its metabolites are primarily excreted in the urine.
Mode of Action: DHEA does not directly bind to receptors. Its mode of action involves its conversion to active sex hormones, which then exert their effects by binding to estrogen and androgen receptors.
Receptor Binding, Enzyme Inhibition, or Neurotransmitter Modulation: DHEA itself does not bind to receptors or inhibit enzymes. However, its downstream metabolites (androgens and estrogens) bind to their respective receptors, which in turn modulate cellular processes.
Elimination Pathways: DHEA and its metabolites are conjugated in the liver and excreted primarily in the urine. A small amount may be excreted in the bile.
Dosage
Standard Dosage
Adults:
For vaginal atrophy, the standard dose of intravaginal prasterone (DHEA) is 6.5 mg once daily at bedtime.
Children:
DHEA is not recommended for use in children.
Special Cases:
- Elderly Patients: For vaginal atrophy, the standard adult dose is used.
- Patients with Renal Impairment: Dose adjustments may be needed based on the degree of impairment.
- Patients with Hepatic Dysfunction: Dose adjustments may be needed based on the degree of impairment.
- Patients with Comorbid Conditions: Caution should be exercised in patients with hormone-sensitive cancers, hyperandrogenism, high cholesterol, heart disease, and mood disorders.
Clinical Use Cases
DHEA is not indicated for intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations.
Dosage Adjustments
Dose adjustments may be necessary for patients with renal or hepatic impairment.
Side Effects
Common Side Effects
Acne, oily skin, hirsutism (unwanted hair growth in women), deepening of the voice in women, vaginal discharge (with intravaginal use).
Rare but Serious Side Effects
Elevated liver enzymes, mania in patients with mood disorders, unfavorable changes in cholesterol levels.
Long-Term Effects
The long-term effects of DHEA use are not fully understood.
Adverse Drug Reactions (ADR)
Rare but serious ADRs include severe acne, liver toxicity, and mania.
Contraindications
DHEA is contraindicated in patients with known or suspected hormone-sensitive cancers (breast, ovarian, prostate), pregnancy, and breastfeeding. It should be used with caution in patients with hyperandrogenism, liver disease, diabetes, high cholesterol, and mood disorders.
Drug Interactions
DHEA may interact with antipsychotics, carbamazepine, estrogen, lithium, selective serotonin reuptake inhibitors, testosterone, triazolam, valproic acid, anticoagulants, antidepressants, aromatase inhibitors, tamoxifen, fulvestrant, and bacillus Calmette-Guérin (BCG) vaccine.
Pregnancy and Breastfeeding
DHEA is contraindicated during pregnancy and breastfeeding.
Drug Profile Summary
- Mechanism of Action: Converted to androgens and estrogens in peripheral tissues.
- Side Effects: Acne, oily skin, hirsutism, deepening of the voice in women, vaginal discharge.
- Contraindications: Hormone-sensitive cancers, pregnancy, breastfeeding.
- Drug Interactions: Multiple drug interactions, consult a comprehensive drug interaction database.
- Pregnancy & Breastfeeding: Contraindicated.
- Dosage: Intravaginal: 6.5 mg once daily.
- Monitoring Parameters: Monitor hormone levels, cholesterol levels, and liver function tests.
Popular Combinations
DHEA is not typically used in combination with other drugs for vaginal atrophy.
Precautions
Screen patients for hormone-sensitive cancers and other contraindications before initiating therapy. Monitor for side effects. Caution in patients with liver disease, diabetes, high cholesterol, and mood disorders.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Dehydroepiandrosterone for vaginal atrophy?
A: The recommended dose of intravaginal prasterone (DHEA) for vaginal atrophy is 6.5 mg once daily at bedtime.
Q2: What is the mechanism of action of DHEA?
A: DHEA is a precursor hormone that’s converted into androgens and estrogens, which then act on their respective receptors.
Q3: What are the common side effects of DHEA?
A: Common side effects include acne, oily skin, hirsutism, deepening of the voice (in women), and vaginal discharge.
Q4: Is DHEA safe to use during pregnancy?
A: No, DHEA is contraindicated during pregnancy.
Q5: Can DHEA interact with other medications?
A: Yes, DHEA has numerous drug interactions. Consult a drug interaction database before prescribing.
Q6: Are there any contraindications to DHEA use?
A: DHEA is contraindicated in individuals with hormone-sensitive cancers, during pregnancy and breastfeeding.
Q7: What is the role of DHEA in the body?
A: DHEA is a precursor hormone to androgens and estrogens, which influence various bodily functions.
Q8: How is DHEA administered for vaginal atrophy?
A: DHEA is administered intravaginally for the treatment of vaginal atrophy.
Q9: Should DHEA be used in children?
A: DHEA is generally not recommended for use in children unless under specific medical supervision.
