OPILL

Clinical safety rating: caution

Comprehensive clinical and safety monograph for OPILL (OPILL).

How it works

Combination oral contraceptive: progestin (norgestimate) suppresses gonadotropin release, inhibiting ovulation; estrogen (ethinyl estradiol) stabilizes endometrial lining and thickens cervical mucus, impeding sperm penetration.

What the body does with it

Metabolism	Ethinyl estradiol primarily metabolized by CYP3A4; norgestimate rapidly deacetylated to norgestrel and further metabolized by CYP3A4 and CYP2C9.
Excretion	Renal: ~50% (as unchanged drug and metabolites). Biliary/fecal: ~50% (as metabolites).
Half-life	Terminal half-life: 30-34 hours. Redistribution half-life: 2-4 hours. Clinical context: Steady state achieved in 5-7 days; dosing interval appropriate for once-daily administration.
Protein binding	~99% bound to albumin and alpha-1-acid glycoprotein.
Volume of Distribution	4-6 L/kg; indicates extensive tissue distribution.
Bioavailability	Oral: 60-70% (due to first-pass metabolism).
Onset of Action	Oral: 30-60 minutes for therapeutic effect; peak plasma concentrations at 1-2 hours.
Duration of Action	Approximately 24 hours; clinical effect wanes over 12-24 hours post-dose. Once-daily dosing maintains sustained effect.

Classification & Brands

Dosing & administration

1 tablet (norgestimate 0.180 mg/ethinyl estradiol 0.025 mg) orally once daily for 21 days, followed by 7 days of placebo.

Dosage form	TABLET
Renal impairment	No dose adjustment required for mild to moderate renal impairment. Not studied in severe renal impairment (CrCl <30 mL/min); use with caution.
Liver impairment	Contraindicated in acute hepatic disease or severe cirrhosis (Child-Pugh class C). For Child-Pugh class A or B, use only if benefits outweigh risks, with close monitoring.
Pediatric use	Not indicated for use before menarche. For postmenarchal adolescents, same dosing as adults: 1 tablet daily for 21 days, then 7 days placebo.
Geriatric use	Not indicated for use in postmenopausal women. No studies in geriatric population; contraindicated in women >35 years who smoke cigarettes due to increased cardiovascular risk.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for OPILL (OPILL).

Breastfeeding	Excreted into breast milk; M/P ratio not established. Potential for serious adverse reactions in nursing infants; contraindicated during breastfeeding.
Teratogenic Risk	FDA Pregnancy Category X. First trimester: Use is contraindicated due to risk of fetal harm, including cardiovascular defects and limb reduction defects. Second and third trimesters: Avoid use; potential for fetal androgenization of female fetuses and other adverse effects.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

Cigarette smoking increases risk of serious cardiovascular events from combination oral contraceptive use. Risk increases with age and with smoking (especially >35 years). Women who use combination oral contraceptives should be strongly advised not to smoke.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Smoking by women >35 years","History of or current venous/arterial thrombosis","Cerebrovascular disease","Coronary artery disease","Known thrombophilias","Major surgery with prolonged immobilization","Diabetes with vascular disease","Headaches with focal neurological symptoms","Uncontrolled hypertension","Known or suspected pregnancy","Current or history of breast cancer or other estrogen-sensitive neoplasia","Active liver disease (e.g., acute hepatitis, decompensated cirrhosis)","Hepatic adenoma or carcinoma","Undiagnosed abnormal uterine bleeding","Use of hepatitis C drug combinations containing ombitasvir/paritaprevir/ritonavir with or without dasabuvir"]

Clinical Precautions

Precautions

["Increased risk of thromboembolic disorders (e.g., MI, stroke, VTE)","Hepatic neoplasia risk","Elevated blood pressure","Gallbladder disease","Carbohydrate/lipid metabolic effects","Headache (including migraine)","Uterine bleeding irregularities","Risk of pregnancy if missed pills"]

Clinical Tips & Counseling

Drug interactions

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OPILL

Clinical safety rating: caution

Comprehensive clinical and safety monograph for OPILL (OPILL).

How it works

What the body does with it

Metabolism	Ethinyl estradiol primarily metabolized by CYP3A4; norgestimate rapidly deacetylated to norgestrel and further metabolized by CYP3A4 and CYP2C9.
Excretion	Renal: ~50% (as unchanged drug and metabolites). Biliary/fecal: ~50% (as metabolites).
Half-life	Terminal half-life: 30-34 hours. Redistribution half-life: 2-4 hours. Clinical context: Steady state achieved in 5-7 days; dosing interval appropriate for once-daily administration.
Protein binding	~99% bound to albumin and alpha-1-acid glycoprotein.
Volume of Distribution	4-6 L/kg; indicates extensive tissue distribution.
Bioavailability	Oral: 60-70% (due to first-pass metabolism).
Onset of Action	Oral: 30-60 minutes for therapeutic effect; peak plasma concentrations at 1-2 hours.
Duration of Action	Approximately 24 hours; clinical effect wanes over 12-24 hours post-dose. Once-daily dosing maintains sustained effect.

Classification & Brands

Dosing & administration

1 tablet (norgestimate 0.180 mg/ethinyl estradiol 0.025 mg) orally once daily for 21 days, followed by 7 days of placebo.

Dosage form	TABLET
Renal impairment	No dose adjustment required for mild to moderate renal impairment. Not studied in severe renal impairment (CrCl <30 mL/min); use with caution.
Liver impairment	Contraindicated in acute hepatic disease or severe cirrhosis (Child-Pugh class C). For Child-Pugh class A or B, use only if benefits outweigh risks, with close monitoring.
Pediatric use	Not indicated for use before menarche. For postmenarchal adolescents, same dosing as adults: 1 tablet daily for 21 days, then 7 days placebo.
Geriatric use	Not indicated for use in postmenopausal women. No studies in geriatric population; contraindicated in women >35 years who smoke cigarettes due to increased cardiovascular risk.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for OPILL (OPILL).

Breastfeeding	Excreted into breast milk; M/P ratio not established. Potential for serious adverse reactions in nursing infants; contraindicated during breastfeeding.
Teratogenic Risk	FDA Pregnancy Category X. First trimester: Use is contraindicated due to risk of fetal harm, including cardiovascular defects and limb reduction defects. Second and third trimesters: Avoid use; potential for fetal androgenization of female fetuses and other adverse effects.
Fetal Monitoring