Fulvestrant Pharmacology

Fulvestrant

About Fulvestrant

Anticancer, estrogen receptor antagonist

Mechanism of Action of Fulvestrant

Fulvestrant competitively and reversibly binds to estrogen receptors present in cancer cells and achieves its anti-estrogen effects through two separate mechanisms. First, fulvestrant binds to the receptors and downregulates them so that estrogen is no longer able to bind to these receptors. Second, fulvestrant degrades the estrogen receptors to which it is bound. Both of these mechanisms inhibit the growth of tamoxifen-resistant as well as estrogen-sensitive human breast cancer cell lines.

Pharmacokinets of Fulvestrant

1.Distribution: Volume of distribution 3 to 5 L/kg,Protein binding 99% (mainly VLDL, LDL, and HDL)
2.Metabolism:Primarily hepatic
3.Elimination:Hepato-bilary system,mainly through faeces

Onset of Action for Fulvestrant

N/A

Duration of Action for Fulvestrant

N/A

Half Life of Fulvestrant

40 days

Side Effects of Fulvestrant

1.Injection Site Pain
2.Headache
3.Back Pain
4.Fatigue
5.Pain in Extremity
6.Asthenia
7.Hot Flash
8.Nausea
9.Vomiting
10.Anorexia
11.Constipation
12.Bone Pain
13.Arthralgia
14.Musculoskeletal Pain
15.Cough
16.Dyspnea

Contra-indications of Fulvestrant

Hypersensitivity

Special Precautions while taking Fulvestrant

1.Administered intramuscularly, it should not be used in patients with bleeding diatheses, thrombocytopenia or in patients on anticoagulants.
2.Moderate to severe hepatic impairment.
3.Renal Function Impairment

Pregnancy Related Information

Contraindicated

Old Age Related Information

Use with caution

Breast Feeding Related Information

Not recommended

Children Related Information

Not recommended

Indications for Fulvestrant

For the treatment of hormone receptor positive metastatic breast cancer in postmenopausal women with disease progression following anti-estrogen therapy.

Interactions for Fulvestrant

Disulfiram, metronidazole:Because fulvestrant injection contains alcohol, patients receiving disulfiram or metronidazole may experience an acute alcohol intolerance reaction if fulvestrant is coadministered. Avoid fulvestrant administration to patients receiving disulfiram or metronidazole.

Typical Dosage for Fulvestrant

1.The recommended dose is 500 mg to be administered intramuscularly into the buttocks slowly (1 - 2 minutes per injection) as two 5 mL injections, one in each buttock, on days 1, 15, 29 and once monthly thereafter
2.Hepatic Impairment:A dose of 250 mg is recommended for patients with moderate hepatic impairment to be administered intramuscularly into the buttock slowly (1 - 2 minutes) as one 5 mL injection on days 1, 15, 29 and once monthly thereafter.

Schedule of Fulvestrant

N/A

Storage Requirements for Fulvestrant

Refrigerate, 2?-8?c (36?-46?f). To protect from light, store in the original carton until time of use.

Effects of Missed Dosage of Fulvestrant

N/A

Effects of Overdose of Fulvestrant

N/A

Home Delivery for Fulvestrant in Your City

Medicine India is just a publishing medium for medicine related information and does not provide services or sales of medicines including fulvestrant.

However, we do publish a comprehensive directory of Pharmacies, Chemists and Druggists in cities all over India. You can use this directory to find the medicine stores in your city (or area) that provide home delivery services for fulvestrant and other medicines and health products. Home delivery services for fulvestrant may be free or they may cost you depending on the pharmacy and the minimum order requirements. It would be best to get this clarified while placing the order.

Please be aware that you should take fulvestrant only if a doctor has recommended or prescribed it. Some or all pharmacies who provide a home delivery service for medicines might insist on a prescription for fulvestrant before they complete the sale. You can get this information while placing the order for fulvestrant with the pharmacy.

Fulvestrant is a generic medicine name and there are several brands available for it. Some of the brands for fulvestrant might be better known than fulvestrant itself. If the pharmacy that's willing to deliver medicines to your home doesn't have fulvestrant in stock, you can ask for one of the branded alternatives for fulvestrant.