OGESTREL 0.5/50-28

Clinical safety rating: caution

Comprehensive clinical and safety monograph for OGESTREL 0.5/50-28 (OGESTREL 0.5/50-28).

How it works

Combination estrogen-progestin contraceptive; suppresses gonadotropins (FSH, LH) via negative feedback on hypothalamic-pituitary axis, inhibiting ovulation; increases cervical mucus viscosity and alters endometrial development.

What the body does with it

Metabolism	Norgestrel and ethinyl estradiol are metabolized primarily via cytochrome P450 3A4 (CYP3A4) in the liver; undergo first-pass metabolism; ethinyl estradiol also undergoes conjugation (sulfation, glucuronidation).
Excretion	Renal: 50-60% as metabolites (glucuronide and sulfate conjugates of norgestrel and ethinyl estradiol); Fecal: 30-40% via biliary elimination; Unchanged drug: <1%.
Half-life	Norgestrel: ~45 hours (range 24-56 h) enabling once-daily dosing; Ethinyl estradiol: ~17 hours (range 10-27 h).
Protein binding	Norgestrel: ~97% bound to sex hormone-binding globulin (SHBG) and albumin; Ethinyl estradiol: ~98% bound to albumin, with 2% free (active).
Volume of Distribution	Norgestrel: ∼4 L/kg (range 3-5 L/kg), indicating extensive tissue distribution; Ethinyl estradiol: ∼2 L/kg (range 1.5-3 L/kg), reflecting distribution to reproductive tissues and liver.
Bioavailability	Oral: Norgestrel ~90-100% (high first-pass metabolism but minimal systemic loss); Ethinyl estradiol ~40-50% due to first-pass metabolism (conjugation in gut wall and liver).
Onset of Action	Oral: Contraceptive effect begins after 7 days of consecutive daily doses; suppression of ovulation occurs by day 7.
Duration of Action	Oral: Contraceptive protection persists for the 21-day active pill period and during the 7-day placebo interval if taken correctly; maximum duration of action is 24 hours per active pill.

Classification & Brands

Dosing & administration

One tablet (norgestrel 0.5 mg/ethinyl estradiol 50 mcg) orally once daily for 28-day cycle.

Dosage form	TABLET
Renal impairment	No dose adjustment required for mild to moderate renal impairment. Not recommended in severe renal impairment (CrCl <30 mL/min) or ESRD due to lack of safety data.
Liver impairment	Contraindicated in acute hepatic disease or Child-Pugh class B and C cirrhosis. For mild hepatic impairment (Child-Pugh A), use with caution; no specific dose adjustment studied.
Pediatric use	Not indicated for children; use only after menarche. Postmenarcheal adolescents: same as adult dosing (one tablet daily) once menses established.
Geriatric use	Not indicated for women ≥65 years; no geriatric-specific dosing recommended. Consider alternative therapies due to increased thrombosis risk and reduced bone density with prolonged use.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for OGESTREL 0.5/50-28 (OGESTREL 0.5/50-28).

Breastfeeding	Small amounts of norgestrel and ethinyl estradiol are excreted in breast milk. M/P ratio not established. Can reduce milk production and quality. Use is generally not recommended during breastfeeding; alternative methods should be considered.
Teratogenic Risk	No increased risk of birth defects has been observed in clinical studies for norgestrel/ethinyl estradiol. Use during pregnancy is contraindicated as hormonal contraceptives are not indicated during gestation. There is no evidence of teratogenicity when inadvertently taken during early pregnancy.

Warnings & precautions

■ FDA Black Box Warning

Cigarette smoking increases risk of serious cardiovascular events from combination oral contraceptives. Risk increases with age (>35 years) and number of cigarettes smoked. Women over 35 who smoke should not use this product.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Known or suspected pregnancy","Current or history of venous thromboembolism (VTE) or arterial thromboembolism (ATE)","Active liver disease or hepatic tumors","Undiagnosed abnormal genital bleeding","Known or suspected breast cancer or other estrogen-sensitive neoplasia","Hypersensitivity to any component","Cigarette smoking in women >35 years","Uncontrolled hypertension","Migraine with aura in women ≥35 years"]

Clinical Precautions

Precautions

["Thrombotic disorders (venous thromboembolism, arterial thromboembolism, stroke, MI)","Cerebrovascular disease","Hepatic neoplasia","Gallbladder disease","Hypertension","Carbohydrate/lipid effects","Headache/migraine","Vaginal bleeding irregularities","Depression","Hereditary angioedema"]

Clinical Tips & Counseling

Drug interactions

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OGESTREL 0.5/50-28

Clinical safety rating: caution

Comprehensive clinical and safety monograph for OGESTREL 0.5/50-28 (OGESTREL 0.5/50-28).

How it works

What the body does with it

Metabolism	Norgestrel and ethinyl estradiol are metabolized primarily via cytochrome P450 3A4 (CYP3A4) in the liver; undergo first-pass metabolism; ethinyl estradiol also undergoes conjugation (sulfation, glucuronidation).
Excretion	Renal: 50-60% as metabolites (glucuronide and sulfate conjugates of norgestrel and ethinyl estradiol); Fecal: 30-40% via biliary elimination; Unchanged drug: <1%.
Half-life	Norgestrel: ~45 hours (range 24-56 h) enabling once-daily dosing; Ethinyl estradiol: ~17 hours (range 10-27 h).
Protein binding	Norgestrel: ~97% bound to sex hormone-binding globulin (SHBG) and albumin; Ethinyl estradiol: ~98% bound to albumin, with 2% free (active).
Volume of Distribution	Norgestrel: ∼4 L/kg (range 3-5 L/kg), indicating extensive tissue distribution; Ethinyl estradiol: ∼2 L/kg (range 1.5-3 L/kg), reflecting distribution to reproductive tissues and liver.
Bioavailability	Oral: Norgestrel ~90-100% (high first-pass metabolism but minimal systemic loss); Ethinyl estradiol ~40-50% due to first-pass metabolism (conjugation in gut wall and liver).
Onset of Action	Oral: Contraceptive effect begins after 7 days of consecutive daily doses; suppression of ovulation occurs by day 7.
Duration of Action	Oral: Contraceptive protection persists for the 21-day active pill period and during the 7-day placebo interval if taken correctly; maximum duration of action is 24 hours per active pill.

Classification & Brands

Dosing & administration

One tablet (norgestrel 0.5 mg/ethinyl estradiol 50 mcg) orally once daily for 28-day cycle.

Dosage form	TABLET
Renal impairment	No dose adjustment required for mild to moderate renal impairment. Not recommended in severe renal impairment (CrCl <30 mL/min) or ESRD due to lack of safety data.
Liver impairment	Contraindicated in acute hepatic disease or Child-Pugh class B and C cirrhosis. For mild hepatic impairment (Child-Pugh A), use with caution; no specific dose adjustment studied.
Pediatric use	Not indicated for children; use only after menarche. Postmenarcheal adolescents: same as adult dosing (one tablet daily) once menses established.
Geriatric use	Not indicated for women ≥65 years; no geriatric-specific dosing recommended. Consider alternative therapies due to increased thrombosis risk and reduced bone density with prolonged use.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for OGESTREL 0.5/50-28 (OGESTREL 0.5/50-28).

Breastfeeding	Small amounts of norgestrel and ethinyl estradiol are excreted in breast milk. M/P ratio not established. Can reduce milk production and quality. Use is generally not recommended during breastfeeding; alternative methods should be considered.
Teratogenic Risk	No increased risk of birth defects has been observed in clinical studies for norgestrel/ethinyl estradiol. Use during pregnancy is contraindicated as hormonal contraceptives are not indicated during gestation. There is no evidence of teratogenicity when inadvertently taken during early pregnancy.