Drilldown: Medicines

Norethindrone (norethisterone outside US) (1)

Aygestin (5 mg, Rx); Camila, Errin, Heather, Jolivette, Nor-QD, Ortho Micronor, Sharobel (0.35 mg POPs); component of many COCs (1)

[[:Category:Hormonal_contraceptives|Hormonal contraceptive]] (1) · [[:Category:Progestins|Progestin (synthetic progestogen)]] (1) · [[:Category:Sex_hormones|Sex hormone]] (1)

'"`UNIQ--vote-000013EE-QINU`"' Higher-dose Aygestin (5 mg) achieves more reliable ovulation suppression and is used for endometriosis and DUB. POP requires strict daily timing because the 24-hour cervical-mucus effect window is narrower than COC'"`UNIQ--ref-000013EF-QINU`"'. (1)

'"`UNIQ--vote-000013F0-QINU`"', '"`UNIQ--vote-000013F1-QINU`"', '"`UNIQ--vote-000013F2-QINU`"', '"`UNIQ--vote-000013F3-QINU`"', '"`UNIQ--vote-000013F4-QINU`"' (1)

POP: 0.35 mg PO daily continuously (no placebo week); high-dose 5 mg Aygestin for amenorrhea/endometriosis 5-10 mg/d (1)

0.35 mg POP tablets; 5 mg tablets (Aygestin); component of COCs and combination HRT (1)

None · Indication-specific · 40 mg/d · 10 mg/d · 20 mg/d · 80 mg/d · 10 mg/d (adults) · 100 mg/d · 4 g/d · 400 mg/d · 40 mg/d typical; up to 240 mg/d for Zollinger-Ellison · 5 mg/d · 50 mg/d · 600 mg/d · No fixed ceiling; titrate to clinical effect and tolerability with CDC opioid prescribing guidance constraints on morphine-milligram-equivalent (MME) totals · No fixed maximum; titrated to TSH target · TID per eye · Titrated to glucose; no fixed ceiling · Titrated to glucose; no fixed maximum · '''20 mg/day in adults >60 years''' per FDA's 2011-2012 QT-prolongation warning; 40 mg/day in adults ≤60

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Oral (1)

Contraception within 48 hours of starting (POP); endometrial effects days (1)

~24 hours per dose (strict timing required for POP — within 3-hour window each day) (1)

~8 hours'"`UNIQ--ref-000013F5-QINU`"' (1)

None · 100% (IV) · ~100% from subcutaneous depot · ~80% (oral)'"`UNIQ--ref-00000027-QINU`"' · 70–90% (oral) · ~100% (oral)'"`UNIQ--ref-0000001C-QINU`"' · ~50% (oral)'"`UNIQ--ref-00000021-QINU`"' · ~95% · '''Saturable''' via the LAT-1 amino-acid transporter, producing nonlinear pharmacokinetics: ~60% at 300 mg single dose, falling to ~35% at 1200 mg single dose'"`UNIQ--ref-0000002A-QINU`"' · 10-20% (oral; reduced by food, calcium, antacids, PPIs, tea/coffee; enhanced by ascorbate) · 100% (IV); essentially complete (oral) · 100% (IV); rapidly neutralized by gastric acid (oral) · 16-21% capsule, 25% suspension (oral; iron and antacids reduce absorption substantially)'"`UNIQ--ref-000009E5-QINU`"' · 25 mg: ~29%; 50 mg: ~35%; food reduces absorption'"`UNIQ--ref-00000C4F-QINU`"' · 30-40% (oral; increases with repeated dosing as gastric pH rises)'"`UNIQ--ref-000000DF-QINU`"' · 40-45% (oral; not significantly affected by food)'"`UNIQ--ref-0000025C-QINU`"' · 40-80% (oral); reduced by food, calcium, iron, PPIs, fiber; take fasting with water'"`UNIQ--ref-00000037-QINU`"' · 42-58% (oral; dose-dependent)'"`UNIQ--ref-00000AEF-QINU`"' · 50-60% (oral; decreased with food, but food given anyway for GI tolerance)'"`UNIQ--ref-00000019-QINU`"' · 60-70% PO at low doses; saturable at high doses (parenteral routes preferred above 15-25 mg/week)'"`UNIQ--ref-000007C9-QINU`"'

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Contraindicated in known pregnancy (Aygestin); the 0.35 mg POP is not teratogenic and does not need to be discontinued before conception planning.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)

[[USLegal:Prescription only|Rx-only]] in US (note: norgestrel 0.075 mg POP is now OTC as Opill since 2023, but norethindrone POP remains Rx) (1)