Zoladex
Zoladex - General Information
Zoladex is a synthetic hormone. In men, it stops the production of the hormone testosterone, which may stimulate the growth of cancer cells. In women, goserelin decreases the production of the hormone estradiol (which may stimulate the growth of cancer cells) to levels similar to a postmenopausal state. When the medication is stopped, hormone levels return to normal.
Pharmacology of Zoladex
The pharmacokinetics of ZOLADEX have been determined in both male and female healthy volunteers and patients. In these studies, ZOLADEX was administered as a single 250µg (aqueous solution) dose and as a single or multiple 3.6 mg depot dose by subcutaneous route.
Zoladex for patients
Males: The use of ZOLADEX in patients at particular risk of developing ureteral obstruction
or spinal cord compression should be considered carefully and the patients monitored closely
during the first month of therapy. Patients with ureteral obstruction or spinal cord
compression should have appropriate treatment prior to initiation of ZOLADEX therapy.
Females: Patients must be made aware of the following information:
Since menstruation should stop with effective doses of ZOLADEX the patient should notify her
physician if regular menstruation persists. Patients missing one or more successive doses of
ZOLADEX may experience breakthrough menstrual bleeding.
ZOLADEX should not be prescribed if the patient is pregnant, breast feeding, lactating, has
nondiagnosed abnormal vaginal bleeding, or is allergic to any of the components of ZOLADEX.
Use of ZOLADEX in pregnancy is contraindicated in women being treated for endometriosis or
endometrial thinning. Therefore, a nonhormonal method of contraception should be used during
treatment. Patients should be advised that if they miss one or more successive doses of
ZOLADEX, breakthrough menstrual bleeding or ovulation may occur with the potential for
conception. If a patient becomes pregnant during treatment for endometriosis or endometrial
thinning, ZOLADEX treatment should be discontinued and the patient should be advised of the
possible risks to the pregnancy and fetus.
For patients being treated for advanced breast cancer, see WARNINGS.
Those adverse events occurring most frequently in clinical studies with ZOLADEX are associated
with hypoestrogenism; of these the most frequently reported are hot flashes (flushes), headaches,
vaginal dryness, emotional lability, change in libido, depression, sweating and change in breast
size. Clinical studies in endometriosis suggest the addition of Hormone Replacement Therapy
(estrogens and/or progestins) to ZOLADEX may decrease the occurrence of vasomotor symptoms and
vaginal dryness associated with hypoestrogenism without compromising the efficacy of ZOLADEX in
relieving symptoms. The optimal drugs, dose and duration of treatment has not been established.
As with other LHRH agonist analogues, treatment with ZOLADEX induces a hypoestrogenic state which
results in a loss of bone mineral density (BMD) over the course of treatment, some of which may not
be reversible. In patients with a history of prior treatment that may have resulted in bone mineral
density loss and/or in patients with major risk factors for decreased bone mineral density such as
chronic alcohol abuse and/or tobacco abuse, significant family history of osteoporosis, or chronic
use of drugs that can reduce bone density such as anticonvulsants or corticosteroids, ZOLADEX therapy
may pose an additional risk. In these patients the risks and benefits must be weighed carefully before
therapy with ZOLADEX is instituted. Clinical studies suggest the addition of Hormone Replacement Therapy
(estrogens and/or progestins) to ZOLADEX is effective in reducing the bone mineral loss which occurs with
ZOLADEX alone. The optimal drugs, dose and duration of treatment has not been established.
Currently, there are no clinical data on the effects of retreatment or treatment of benign gynecological
conditions with ZOLADEX for periods in excess of 6 months
Zoladex Interactions
No formal drug-drug interaction studies have been performed. No confirmed interactions have been reported
between ZOLADEX and other drugs
Zoladex Contraindications
Goserelin is contraindicated in those patients who have a known hypersensitivity to LHRH, LHRH agonist analogues or any of the components in Goserelin. Goserelin is contraindicated in women being treated for endometriosis who are or may become pregnant while receiving the drug. Goserelin can cause fetal harm when administered to a pregnant woman. Effects on reproductive function, as a result of antigonadotrophic properties of the drug, are expected to occur on chronic administration. Effective nonhormonal contraception must be used by all premenopausal women during Goserelin therapy and for 12 weeks following discontinuation of therapy. There are no adequate and well-controlled studies in pregnant women using Goserelin. If this drug is used during pregnancy, or the patient being treated for endometriosis becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus or potential risk for loss of the pregnancy. Women of childbearing potential should be advised to avoid becoming pregnant. Goserelin is contraindicated in women who are breast feeding.
Additional information about Zoladex
Zoladex Indication: Breast cancer; Prostate carcinoma; Endometriosis
Mechanism Of Action: ZOLADEX is a synthetic decapeptide analogue of LHRH. ZOLADEX acts as a potent inhibitor of pituitary gonadotropin secretion when administered in the biodegradable formulation. The result is sustained suppression of LH and serum testosterone levels.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Goserelin
Synonyms: Goserelin acetate; Goserelin acetate (JAN/USP)
Drug Category: Antineoplastic Agents
Drug Type: Biotech; Approved
Other Brand Names containing Goserelin: Zoladex;
Absorption: Inactive orally, rapidly absorbed following subcutaneous administration
Toxicity (Overdose): No experience of overdosage from clinical trials
Protein Binding: 27.3%
Biotransformation: Hepatic
Half Life: 4-5 hours
Dosage Forms of Zoladex: Implant Subcutaneous
Chemical IUPAC Name: N-[1-[[1-[[1-[[1-[[1-[[1-[[1-[2-[(carbamoylamino)carbamoyl]pyrrolidin-1-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-[(2-methylpropan-2-yl)oxy]-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(3H-imidazol-4-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
Chemical Formula: C59H84N18O14
Goserelin on Wikipedia: https://en.wikipedia.org/wiki/Goserelin
Organisms Affected: Humans and other mammals
