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Clomiphene

Pronunciation
(KLOE mi feen)

U.S. Brand Names

Clomid; Milophene; Serophene

Generic Available
No

Raloxifene

Pronunciation
(ral OX i feen)

U.S. Brand Names

Evista

Generic Available

No

Synonyms
Keoxifene Hydrochloride; Raloxifene Hydrochloride

Pharmacological Index
Selective Estrogen Receptor Modulator (SERM)

Use
Prevention and treatment of osteoporosis in postmenopausal women

Pregnancy Risk Factor

X

Pregnancy/Breast-Feeding Implications
Raloxifene should not be used by pregnant women or by women planning to become

pregnant in the immediate future

Contraindications
Pregnancy; prior hypersensitivity to raloxifene; active thromboembolic disorder; not
intended for use in premenopausal women

Warnings/Precautions
History of venous thromboembolism/pulmonary embolism; patients with cardiovascular
disease; history of cervical/uterine carcinoma; renal/hepatic insufficiency (however,
pharmacokinetic data are lacking); concurrent use of estrogens

Adverse Reactions
greater than or equal to 2%:
Central nervous system: Migraine, depression, insomnia, fever
Dermatologic: Rash
Endocrine & metabolic: Hot flashes

Gastrointestinal: Nausea, dyspepsia, vomiting, flatulence, gastroenteritis, weight gain

Genitourinary: Vaginitis, urinary tract infection, cystitis, leukorrhea
Neuromuscular & skeletal: Leg cramps, arthralgia, myalgia, arthritis
Respiratory: Sinusitis, pharyngitis, cough, pneumonia, laryngitis
Miscellaneous: Infection, flu syndrome, diaphoresis

Overdosage/Toxicology
Incidence of overdose in humans has not been reported. In an 8-week study of
postmenopausal women, a dose of raloxifene 600 mg/day was safely tolerated. No
mortality was seen after a single oral dose in rats or mice at 810 times the human dose
for rats and 405 times the human dose for mice. There is no specific antidote for
raloxifene.

Drug Interactions
Decreased effects: Ampicillin and cholestyramine decreases raloxifene absorption

Mechanism of Action

A selective estrogen receptor modulator, meaning that it affects some of the same
receptors that estrogen does, but not all, and in some instances, it antagonizes or blocks
estrogen; it acts like estrogen to prevent bone loss and improve lipid profiles, but it has
the potential to block some estrogen effects such as those that lead to breast cancer and
uterine cancer

Pharmacodynamics/Kinetics
Onset of action: 8 weeks
Distribution: 2348 L/kg
Protein binding: >95% to albumin and -glycoprotein
Metabolism: Extensive first pass metabolism
Bioavailability: ~2%
Half-life: 27.7-32.5 hours
Elimination: Primarily in the feces and 0.2% renal

Usual Dosage
Adults: Female: Oral: 60 mg/day which may be administered any time of the day without

regard to meals

Monitoring Parameters
Radiologic evaluation of bone mineral density (BMD) is the best measure of the treatment
of osteoporosis; to monitor for the potential toxicities of raloxifene, complete blood counts
should be evaluated periodically.

Mental Health: Effects on Mental Status

May cause insomnia or depression

Mental Health: Effects on Psychiatric Treatment

None reported

Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions

Dental Health: Effects on Dental Treatment

No effects or complications reported

Patient Information
May be taken at any time of day without regard to meals. This medication is given to
reduce incidence of osteoporosis; it will not reduce hot flashes or flushing. You may
experience flu-like symptoms at beginning of therapy (these may resolve with use). Mild
analgesics may reduce joint pain. Rest and cool environment may reduce hot flashes.
Report fever; acute migraine; insomnia or emotional depression; unusual weight gain;
unresolved gastric distress; urinary infection or vaginal burning or itching; chest pain; or
swelling, warmth, or pain in calves. Pregnancy/breast-feeding precautions: Inform
prescriber if you are pregnant. Do not breast-feed.

Dosage Forms
Tablet, as hydrochloride: 60 mg

Danazol

Pronunciation
(DA na zole)

U.S. Brand Names

Danocrine

Generic Available
No

Canadian Brand Names

Cyclomen

Flutamide

Pronunciation

Stability

U.S. Brand Names

Mechanism of Action

Generic Available

Pharmacodynamics/Kinetics

Canadian Brand Names

Usual Dosage

Pharmacological Index

Monitoring Parameters

Use

Mental Health: Effects on Mental Status

Pregnancy Risk Factor

Mental Health: Effects on Psychiatric Treatment

Contraindications

Dental Health: Local Anesthetic/Vasoconstrictor Precautions

Warnings/Precautions

Dental Health: Effects on Dental Treatment

Adverse Reactions

Patient Information

Overdosage/Toxicology

Dosage Forms

Drug Interactions

References

Pronunciation

(FLOO ta mide)

U.S. Brand Names

Eulexin

Generic Available

No

Canadian Brand Names

Novo-Flutamide

Pharmacological Index

Antiandrogen

Use

In combination therapy with LHRH agonist analogues in treatment of metastatic prostatic carcinoma. A study has shown that the addition of flutamide to
leuprolide therapy in patients with advanced prostatic cancer increased median actuarial survival time to 34.9 months versus 27.9 months with leuprolide

alone. To achieve benefit to combination therapy, both drugs need to be started simultaneously.

Pregnancy Risk Factor

Contraindications

Known hypersensitivity to flutamide

Warnings/Precautions

The U.S. Food and Drug Administration (FDA) currently recommends that procedures for proper handling and disposal of antineoplastic agents be
considered. Animal data (based on using doses higher than recommended for humans) produced testicular interstitial cell adenoma. Do not discontinue
therapy without physician's advice. May cause hepatic failure, which can be fatal. Serum transaminases should be monitored at baseline and monthly for the
first four months of therapy, and periodically thereafter. These should also be repeated at the first sign and symptom of liver dysfunction. Use of flutamide is
not recommended in patients with baseline elevation of transaminase levels (> twice the upper limit of normal). Flutamide should be discontinued immediately
at any time if the patient develops jaundice or elevation in serum transaminase levels (>2 times upper limit of normal).

Adverse Reactions

>10%:
Gastrointestinal: Nausea, vomiting, diarrhea
Genitourinary: Impotence
Endocrine & metabolic: Loss of libido, hot flashes
1% to 10%:
Endocrine & metabolic: Gynecomastia
Gastrointestinal: Anorexia
Neuromuscular & skeletal: Numbness in extremities
<1%: Hepatic failure, jaundice, flu-like syndrome, abdominal pain, hypertension, edema, drowsiness, nervousness, confusion, hepatitis

Overdosage/Toxicology

Symptoms of overdose include hypoactivity, ataxia, anorexia, vomiting, slow respiration, lacrimation
Management is supportive, dialysis not of benefit; induce vomiting

Drug Interactions

CYP3A3/4 enzyme substrate

Stability

Store at room temperature

Mechanism of Action

Nonsteroidal antiandrogen that inhibits androgen uptake or inhibits binding of androgen in target tissues

Pharmacodynamics/Kinetics

Absorption: Rapid and complete

Metabolism: Extensively to more than 10 metabolites
Half-life: 5-6 hours
Elimination: All metabolites excreted primarily in urine

Usual Dosage

Adults: Oral: 2 capsules every 8 hours for a total daily dose of 750 mg

Monitoring Parameters

Serum transaminase levels should be measured prior to starting treatment and should be repeated monthly for the first 4 months of therapy, and periodically
thereafter. LFTs should be checked at the first sign or symptom of liver dysfunction (eg, nausea, vomiting, abdominal pain, fatigue, anorexia, flu-like
symptoms, hyperbilirubinuria, jaundice, or right upper quadrant tenderness). Other parameters include tumor reduction, testosterone/estrogen, and
phosphatase serum levels.

Mental Health: Effects on Mental Status

May rarely cause nervousness or confusion

Mental Health: Effects on Psychiatric Treatment

None reported

Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions

Dental Health: Effects on Dental Treatment

No effects or complications reported

Patient Information

Take as directed; do not discontinue without consulting prescriber. You may experience decreased libido, impotence, swelling of breasts, or decreased
appetite (small frequent meals may help). Report chest pain or palpitation; acute abdominal pain; pain, tingling, or numbness of extremities; swelling of
extremities or unusual weight gain; difficulty breathing; or other persistent adverse effects. Pregnancy precautions: This drug will cause fetal abnormalities use barrier contraceptives.

Dosage Forms

Capsule: 125 mg

Exemestane

U.S. Brand Names

Aromasin

Pharmacological Index
Antineoplastic Agent, Miscellaneous

Use
Treatment of advanced breast cancer in postmenopausal women whose disease has
progressed following tamoxifen therapy

Pregnancy Risk Factor