Norgestimate

in ORTHO TRI-CYCLEN

Open Norgestimate in the interactive console ↗

Pronunciation: nor-JES-ti-mayt

Norgestimate ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Norgestimate ballicule

Norgestimate ORTHO TRI-CYCLEN mascot mnemonic cartoon — Visual mnemonic: Norgestimate mascot
**“North estimator”**

What it isProgestin with low androgenic activity, used in combined oral contraceptives.

Why this oneIts low androgenicity is why it is chosen for acne, and it carries an acne indication.

What limits itCombined use brings VTE risk, higher with smoking and over 35. Efficacy depends on daily adherence.

Norgestimate molecular structure (skeletal formula) — Molecular structure: Norgestimate

FDA-approved for

contraception with ethinyl estradiol
acne vulgaris

FDA label

Read the full label on DailyMed ↗

BOXED WARNING COCs contraindicated in women >35 who smoke; smoking raises risk of serious cardiovascular events.

FDA dosing	Population	Start	Target	Max
Contraception	Females of reproductive potential	1 active tablet QD	1 tablet QD (21 active + 7 inactive per 28-day cycle)

Renal Undefined

Hepatic Contraindicated in liver disease or hepatic tumors

Instructions

Take 1 tablet by mouth at the same time daily, in blister-pack order
Do not skip or delay tablets
Day 1 or Sunday start; with Sunday start use backup contraception for first 7 days
Start next pack the day after finishing prior pack

Available strengths

tab 0.25, 0.035 mg

Contraindications

High risk of arterial/venous thrombosis (DVT/PE, thrombophilia, cerebrovascular or coronary artery disease, thrombogenic valvular/rhythm disease)
Women >35 years who smoke
Uncontrolled hypertension
Diabetes mellitus with vascular disease
Headache with focal neurological symptoms, migraine with aura, or any migraine if >35
Liver tumors (benign/malignant) or liver disease
Undiagnosed abnormal uterine bleeding
Pregnancy
Current or history of breast cancer or other estrogen/progesterone-sensitive cancer

Cautions

Stop if thrombotic event; stop ≥4 wk before and 2 wk after major surgery
Discontinue if jaundice occurs
Monitor BP; may worsen glucose/lipid control
Evaluate new or worsening headache
Irregular bleeding/amenorrhea

Adverse reactions

Irregular uterine bleeding
Nausea
Breast tenderness
Headache/migraine
Abdominal pain
Mood changes (depression, mood altered)

Pregnancy Contraindicated in pregnancy; no increased birth-defect risk with inadvertent early exposure.

Lactation Not recommended; can decrease milk production. Small amounts of steroids present in milk.

Cost

Norgestimate (IN ORTHO TRI-CYCLEN)

Strength		#/mo	generic $/mo	CostPlus
0.25 mg	tab	30 qd		not offered
0.035 mg	tab	30 qd		not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Norgestimate is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Available combined with: ethinyl / estradiol / norgestimate

Generic entry2002

⚠ BOXED WARNING

Cigarette smoking and serious cardiovascular events over age 35

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4

Overdose danger1 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk0 / 4

Legacy pregnancy categoryX

Defining liabilityVenous thromboembolism and hormone-related adverse effects; estrogen also lowers lamotrigine exposure.

Active metabolites

Norelgestromin

Open Norgestimate in the interactive console ↗

Memory aids: interaction avatars

CYP3A4 substrate

Open Norgestimate in the interactive console ↗