Usage
This drug combination is primarily prescribed for female infertility, particularly in cases of ovulatory dysfunction, such as polycystic ovary syndrome (PCOS). It is also used to manage infertility due to conditions like amenorrhea-galactorrhea syndrome and psychogenic amenorrhea. It is an ovarian stimulant with antioxidant properties.
Alternate Names
This combination does not have a universally recognized international nonproprietary name (INN). It is marketed under brand names like Gencure-Fem, Ovaa Shield, and Ovaa Shield DS.
How It Works
Pharmacodynamics:
- Clomiphene: A selective estrogen receptor modulator (SERM), it primarily acts on the hypothalamus and pituitary gland. By partially blocking estrogen receptors, clomiphene disrupts the normal negative feedback loop, leading to increased secretion of gonadotropin-releasing hormone (GnRH), follicle-stimulating hormone (FSH), and luteinizing hormone (LH). Elevated FSH and LH levels stimulate follicular development and maturation in the ovaries, ultimately triggering ovulation.
- Acetylcysteine: A mucolytic agent, it thins the cervical mucus, improving sperm penetration and motility. Additionally, it may positively impact endometrial thickness, further supporting implantation.
- Astaxanthin: A potent antioxidant, it protects developing oocytes from oxidative stress and damage, improving egg quality and potentially enhancing fertility.
Pharmacokinetics:
The pharmacokinetics of the combined formulation are not fully understood. Individual components are absorbed orally. Clomiphene is metabolized in the liver and primarily excreted in feces. Acetylcysteine is readily absorbed and extensively metabolized. Astaxanthin is lipophilic and accumulates in various tissues.
Dosage
Standard Dosage
Adults:
A common regimen is clomiphene 50-100mg daily for 5 days, starting on day 3-5 of the menstrual cycle, combined with acetylcysteine 600-1200mg daily (divided into 2-3 doses) and astaxanthin 4mg daily. Dosage may vary based on individual response and clinical indication.
Children:
This combination is not recommended for use in children and adolescents below 18 years of age.
Special Cases:
- Elderly Patients: Use with caution, as the effects on this population are not well studied.
- Patients with Renal Impairment: Dose adjustments may be necessary. Consult current clinical guidelines.
- Patients with Hepatic Dysfunction: Contraindicated in patients with liver disease.
- Patients with Comorbid Conditions: Use with caution in patients with conditions like hypertriglyceridemia, thyroid disorders, adrenal gland issues, endometriosis, and a history of blood clots.
Clinical Use Cases
The combination is not typically used in settings like intubation, surgical procedures, mechanical ventilation, or the ICU. Its use is primarily focused on managing ovulatory dysfunction in female infertility.
Dosage Adjustments
Adjustments may be necessary based on individual response and tolerability. Close monitoring of follicular development and hormone levels is crucial.
Side Effects
Common Side Effects
Nausea, stomach ache, bloating, hot flashes, blurred vision, headache, mood swings.
Rare but Serious Side Effects
Ovarian hyperstimulation syndrome (OHSS), visual disturbances, allergic reactions.
Long-Term Effects
Potential increased risk of ovarian cancer with prolonged use.
Adverse Drug Reactions (ADR)
OHSS requires immediate medical attention.
Contraindications
Pregnancy, breastfeeding, liver disease, abnormal uterine bleeding of unknown cause, ovarian cysts (unless related to PCOS), hormone-dependent cancers, hypersensitivity to any component.
Drug Interactions
Hormonal medications, anticoagulants (e.g., warfarin, heparin), some antibiotics (e.g., erythromycin), nitroglycerin, activated charcoal, cough suppressants (e.g., promethazine), gonadorelin, bexarotene, ospemifene, aspirin.
Pregnancy and Breastfeeding
Contraindicated in both pregnancy and breastfeeding. Clomiphene has potential teratogenic effects. The effects of acetylcysteine and astaxanthin in these conditions aren’t fully studied.
Drug Profile Summary
- Mechanism of Action: Clomiphene stimulates ovulation; acetylcysteine improves cervical mucus and potentially endometrial thickness; astaxanthin acts as an antioxidant, improving egg quality.
- Side Effects: Nausea, vomiting, hot flashes, headache, blurred vision, OHSS (rare).
- Contraindications: Pregnancy, liver disease, abnormal uterine bleeding, hypersensitivity to components.
- Drug Interactions: Hormonal medications, anticoagulants, some antibiotics.
- Pregnancy & Breastfeeding: Contraindicated.
- Dosage: As per clinical guidelines and individualized.
- Monitoring Parameters: Follicular development, endometrial thickness, hormone levels (E2, progesterone), and signs of OHSS.
Popular Combinations
This specific combination is itself popular for female infertility, especially in PCOS. It may also be combined with metformin.
Precautions
Careful patient evaluation is essential before starting therapy. Monitor for side effects, particularly OHSS. Patients with visual disturbances should avoid driving.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Acetylcysteine + Astaxanthin + Clomiphene?
A: Dosage varies based on individual factors and clinical response. A common regimen includes clomiphene 50-100mg daily for 5 days, starting on day 3-5 of the cycle, along with acetylcysteine 600-1200mg daily and astaxanthin 4mg daily. Follow clinical guidelines and individualize therapy.
Q2: What are the primary uses of this combination?
A: Primarily used for treating female infertility associated with ovulatory dysfunction (e.g., PCOS), amenorrhea-galactorrhea syndrome, and psychogenic amenorrhea.
Q3: Is this combination safe during pregnancy?
A: No, it is contraindicated during pregnancy due to clomiphene’s potential teratogenic effects.
Q4: What are the key side effects to watch out for?
A: Common side effects include nausea, hot flashes, and headache. Rare but serious side effects include OHSS. Monitor for visual disturbances as well.
Q5: Are there any significant drug interactions?
A: Yes, potential interactions exist with hormonal medications, anticoagulants, and some antibiotics. A thorough medication review is crucial.
Q6: How does acetylcysteine contribute to fertility?
A: It improves the quality of cervical mucus, facilitating sperm penetration. It might also positively influence endometrial thickness.
Q7: What is the role of astaxanthin in this combination?
A: Astaxanthin acts as a potent antioxidant, protecting eggs from oxidative damage and potentially improving egg quality.
Q8: What are the contraindications for this drug?
A: Contraindications include pregnancy, breastfeeding, liver disease, abnormal uterine bleeding, and hypersensitivity to any of the components.
Q9: Can this medication be used in patients with liver disease?
A: No, it’s contraindicated in patients with liver disease.
Q10: How should I monitor patients on this therapy?
A: Monitor follicular development, endometrial thickness, serum E2 and progesterone levels, and for any signs of OHSS. Regular follow-up is essential.
