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Look Up > Drugs > Mestranol and Norethynodrel
Mestranol and Norethynodrel
Pronunciation
Generic Available
Synonyms
Pharmacological Index
Use
Pregnancy Risk Factor
Contraindications
Adverse Reactions
Drug Interactions
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Mental Health: Effects on Mental Status
Mental Health: Effects on Psychiatric Treatment
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Dosage Forms

Pronunciation
(MES tra nole & nor e THYE noe drel)

Generic Available

Yes


Synonyms
Norethynodrel and Mestranol

Pharmacological Index

Contraceptive


Use

Treatment of hypermenorrhea, endometriosis, female hypogonadism


Pregnancy Risk Factor

X


Contraindications

Known or suspected breast cancer; undiagnosed abnormal vaginal bleeding; carcinoma of the breast; estrogen-dependent tumors


Adverse Reactions

>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


Drug Interactions

Decreased effect with barbiturates, hydantoins (phenytoin, rifampin, antibiotics), penicillins, tetracyclines, griseofulvin

Increased toxicity of acetaminophen, anticoagulants, benzodiazepines, caffeine, corticosteroids, metoprolol, theophylline, tricyclic antidepressants


Mechanism of Action

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.


Pharmacodynamics/Kinetics

Mestranol:

Demethylated to ethinyl estradiol

Serum half-life: 6-20 hours

Norethynodrel: Serum half-life, terminal: 5-14 hours


Usual Dosage

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


Mental Health: Effects on Mental Status

May cause anxiety, dizziness, or depression


Mental Health: Effects on Psychiatric Treatment

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


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

When prescribing antibiotics, patients must be advised to use additional methods of birth control when taking oral contraceptives


Patient Information

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.


Dosage Forms

Tablet:

10 mg: Mestranol 0.150 mg and norethynodrel 9.85 mg


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