Tamoxifen (Citrate)
Tamoxifen (Citrate) is a nonsteroidal antiestrogen, antineoplastic agent, chemically related to another antiestrogen, like clomiphene. It blocks estrogen at its receptor on the cell surface of cancer cells that require estrogen for growth and development. Tamoxifen (Citrate) is most often used as an adjunct to breast surgery in the treatment of breast cancer, can be used as sole therapy for metastatic breast cancer in women with estrogen-receptor positive. Tamoxifen (Citrate) is also used as an adjunct after surgical removal of a breast tumor, or in combination with chemotherapy for breast cancer. Tamoxifen was approved by the FDA in 1977 for use in patients with breast cancer. Tamoxifen (Citrate) is currently being investigated as an agent to reduce bone loss due to osteoporosis in post-menopausal women.
Primary Characteristics
It is of Synthetic origin and belongs to Phenylethylamine.
It belongs to Oestrogen antagonist pharmacological group on the basis of mechanism of action and also classified in Antineoplastic Agent pharmacological group. It is also classified under Chemotherapeutic Regimens .
Molecular Weight: 563.6 · pKa: 7.82 · Solubility in Water: slightly · Solubility in Alcohol: soluble · Non-proprietary name: Tamoxifen (Citrate).
Pharmacokinetics
Absorption: Tamoxifen (Citrate) has an oral bioavailability is 83% (±7%).
Distribution: Tamoxifen (Citrate) has a volume of distribution is 55(50-60)l/kg. plasma protein binding is high.
Elimination: it is metabolised via Hepatic, plasma half-life is 7 days, renal excretion is <1.
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Indications
Tamoxifen (Citrate) is primarily indicated in conditions like Breast cancer, Infertility.
Contraindications
Tamoxifen (Citrate) is contraindicated in conditions like Hypersensitivity to the drug.
Dosage
Tamoxifen (Citrate)'s dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 25 mg | 25 mg | Every 24h | PO | |
| Paediatric Dosage (20kg) | ||||
| 0 – 0 | — | — | Not applicable in paeds | |
| Neonatal Dosage (3kg) | ||||
| 0 – 0 | — | — | Not applicable in this age group | |
Drug Interactions
Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Side Effects
Tamoxifen (Citrate) in overdosage may give rise to further complications which include Cataract, Cystic ovarian swelling , Retinopathy .
Tamoxifen (Citrate) produces potentially life-threatening effects which include Hypercalcemia. Careful monitoring is needed with proper medical management.
Tamoxifen (Citrate) is known to cause more or less tolerable side effects which are usually transient. These include Fluid retention, GI disturbance, Hot flushes, Pruritus .
Warnings / Precautions
Available Brands
Storage Conditions
Drug Classification
- 1.8.3 — Hormones and antihormones