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Pronunciation |
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(MES
tra nole & nor e THYE noe
drel) |
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Generic
Available |
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Yes |
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Synonyms |
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Norethynodrel and Mestranol |
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Pharmacological Index |
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Contraceptive |
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Use |
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Treatment of hypermenorrhea, endometriosis, female
hypogonadism |
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Pregnancy Risk
Factor |
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X |
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Contraindications |
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Known or suspected breast cancer; undiagnosed abnormal vaginal bleeding;
carcinoma of the breast; estrogen-dependent tumors |
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Adverse
Reactions |
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>10%:
Cardiovascular: Peripheral edema
Endocrine & metabolic: Enlargement of breasts, breast tenderness
Gastrointestinal: Nausea, anorexia, bloating
1% to 10%:
Central nervous system: Headache
Endocrine & metabolic: Increased libido
Gastrointestinal: Vomiting, diarrhea |
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Drug
Interactions |
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Decreased effect with barbiturates, hydantoins (phenytoin, rifampin,
antibiotics), penicillins, tetracyclines, griseofulvin
Increased toxicity of acetaminophen, anticoagulants, benzodiazepines,
caffeine, corticosteroids, metoprolol, theophylline, tricyclic antidepressants
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Mechanism of
Action |
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Inhibits ovulation via a negative feedback mechanism on the hypothalamus,
which alters the normal pattern of gonadotropin secretion of a
follicle-stimulating hormone (FSH) and luteinizing hormone by the anterior
pituitary. The follicular phase FSH and midcycle surge of gonadotropins are
inhibited. Oral contraceptives produce alterations in the genital tract,
including changes in the cervical mucus, rendering it unfavorable for sperm
penetration even if ovulation occurs. Changes in the endometrium may also occur,
producing an unfavorable environment for nidation. May alter the tubal transport
of the ova through the fallopian tubes. Progestational agents may also alter
sperm fertility. |
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Pharmacodynamics/Kinetics |
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Mestranol:
Demethylated to ethinyl estradiol
Serum half-life: 6-20 hours
Norethynodrel: Serum half-life, terminal: 5-14 hours |
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Usual Dosage |
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Adults: Female: Oral:
Hypermenorrhea: 20-30 mg/day until bleeding is controlled, then reduce to 10
mg/day and continue through day 24 of cycle; administer 5-10 mg/day from day 5
through day 24 of next 2-3 cycles |
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Mental Health: Effects
on Mental Status |
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May cause anxiety, dizziness, or depression |
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Mental Health:
Effects on Psychiatric
Treatment |
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Hepatic metabolism of TCAs, benzodiazepines (oxidatively metabolized) and
beta-blockers may be decreased by oral contraceptives; monitor increased/toxic
effects; may increase the clearance of benzodiazepines (glucuronidation);
barbiturates may increase the metabolism of oral contraceptives resulting in
decreased effectiveness |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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When prescribing antibiotics, patients must be advised to use additional
methods of birth control when taking oral contraceptives |
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Patient
Information |
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Patients should inform their physicians if signs or symptoms of any of the
following occur: Thromboembolic or thrombotic disorders including sudden severe
headache or vomiting, disturbance of vision or speech, loss of vision, numbness
or weakness in an extremity, sharp or crushing chest pain, calf pain, shortness
of breath, severe abdominal pain or mass, mental depression, or unusual
bleeding. |
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Dosage Forms |
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Tablet:
10 mg: Mestranol 0.150 mg and norethynodrel 9.85 mg
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