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Orlest

Orlest - General Information

A synthetic progestational hormone with actions similar to those of progesterone but functioning as a more potent inhibitor of ovulation. It has weak estrogenic and androgenic properties. The hormone has been used in treating amenorrhea, functional uterine bleeding, endometriosis, and for contraception. [PubChem]

 

Pharmacology of Orlest

Orlest is a synthetic oral progestin. It is used for contraception or to treat such conditions as secondary amenorrhea, abnormal uterine bleeding, and endometriosis. As an oral contraceptive, norethindrone is available as either a single agent or in combination with an estrogen.

 

Orlest for patients

PATIENT INFORMATION

INTRODUCTION

This leaflet is about birth control pills that contain one hormone, a progestin. Please read this
leaflet before you begin to take your pills. It is meant to be used along with talking with your
doctor or clinic. Progestin-only pills are often called �POPs� or �the minipill�. POPs have less
progestin than the combined birth control pill (or �the pill�) which contains both an estrogen and
a progestin.

HOW EFFECTIVE ARE POPs?

About 1 in 200 POP users will get pregnant in the first year if they all take POPs perfectly (that is,
on time, every day). About 1 in 20 �typical� POP users (including women who are late taking pills or
miss pills) gets pregnant in the first year of use. Table 2 will help you compare the efficacy of
different methods.

DIALPAK� Tablet Dispenser-28�s

The first time you use these pills, take your first pill on the first day of your menstrual period.
Turn the ribbed outer ring clockwise until the day for your first pill is over the black Day Arrow in
the center of the DIALPAK.
To remove the pill, press down on it with your thumb or forefinger. The pill will drop through a hole
in the bottom of the DIALPAK.
On the next day, turn the ribbed outer ring clockwise to the next pill. The correct day will be indicated
by the black Day Arrow in the center of the DIALPAK.
Take one pill every day for 28 days, whether bleeding or not, until you have taken all the pills. It is
important that you take your pill at the same time every day.
After you have taken all 28 pills, begin taking your pills again the next day. Be sure the calendar day
on your new package corresponds with the actual day.
INSTRUCTIONS FOR USE VERIDATE� Tablet Dispenser-28�s

Place the refill in the VERIDATE so that the V notch in the refill is at the top of the dispenser. Press
the refill down so that it fits firmly under all nibs.
The first time you use these pills, take your first pill on the first day of your menstrual period.
Choose a pill that corresponds with the day of the week on which you are taking the first pill.
Continue taking one pill daily, clockwise, until no pills remain in the outer circle. It is important that
you take your pills at the same time every day.
The next day, take a pill from the inner circle that corresponds with the day of the week it happens to be.
Take a pill each day until all seven are taken.
After you have taken all 28 pills, insert a new refill in the VERIDATE and begin taking your pills again
the next day. Be sure the calendar day on the package corresponds with the actual day.

WILL POPs AFFECT YOUR ABILITY TO GET PREGNANT LATER?

If you want to become pregnant, simply stop taking POPs. POPs will not delay your ability to get pregnant.

BREASTFEEDING

If you are breastfeeding, POPs will not affect the quality or amount of your breastmilk or the health of
your nursing baby.

 

Orlest Interactions

The effectiveness of progestin-only pills is reduced by hepatic enzyme-inducing drugs such as the anticonvulsants phenytoin, carbamazepine, and barbiturates, and the antituberculosis drug rifampin. No significant interaction has been found with broad-spectrum antibiotics.

 

Orlest Contraindications

Progestin-only oral contraceptives (POPs) should not be used by women who currently have the following conditions:

  • Known or suspected pregnancy
  • Known or suspected carcinoma of the breast
  • Undiagnosed abnormal genital bleeding
  • Hypersensitivity to any component of this product
  • Benign or malignant liver tumors
  • Acute liver disease

 

Additional information about Orlest

Orlest Indication: For use as an oral contraceptive in the prevention of pregnancy.
Mechanism Of Action: Progestins diffuse freely into target cells and bind to the progesterone receptor. Target cells include the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. Once bound to the receptor, progestins slow the frequency of release of gonadotropin releasing hormone (GnRH) from the hypothalamus and blunt the pre-ovulatory LH surge.
Drug Interactions: Acitretin Acitretine may cause a loss of contraceptive effect
Amobarbital This product may cause a slight decrease of contraceptive effect
Aprobarbital This product may cause a slight decrease of contraceptive effect
Bosentan Bosentan decreases the effect of the contraceptive
Butabarbital This product may cause a slight decrease of contraceptive effect
Butalbital This product may cause a slight decrease of contraceptive effect
Butethal This product may cause a slight decrease of contraceptive effect
Carbamazepine This product may cause a slight decrease of contraceptive effect
Ethotoin This product may cause a slight decrease of contraceptive effect
Fosphenytoin This product may cause a slight decrease of contraceptive effect
Mephenytoin This product may cause a slight decrease of contraceptive effect
Phenytoin This product may cause a slight decrease of contraceptive effect
Griseofulvin This product may cause a slight decrease of contraceptive effect
Heptabarbital This product may cause a slight decrease of contraceptive effect
Hexobarbital This product may cause a slight decrease of contraceptive effect
Lamotrigine The oral contraceptive decreases the effect of lamotrigine
Methohexital This product may cause a slight decrease of contraceptive effect
Methylphenobarbital This product may cause a slight decrease of contraceptive effect
Pentobarbital This product may cause a slight decrease of contraceptive effect
Phenobarbital This product may cause a slight decrease of contraceptive effect
Primidone This product may cause a slight decrease of contraceptive effect
Rifabutin This product may cause a slight decrease of contraceptive effect
Pioglitazone Possible loss of contraceptive effect
Rifampin This product may cause a slight decrease of contraceptive effect
Rifapentine This product may cause a slight decrease of contraceptive effect
Secobarbital This product may cause a slight decrease of contraceptive effect
Talbutal This product may cause a slight decrease of contraceptive effect
St. John's Wort St. John's Wort could reduce the contraceptive effect
Tizanidine The contraceptive increases the effect of tizanidine
Troglitazone Possible loss of contraceptive effect
Food Interactions: Not Available
Generic Name: Norethindrone
Synonyms: Not Available
Drug Category: Contraceptives, Oral, Synthetic; Progestins
Drug Type: Small Molecule; Approved

Other Brand Names containing Norethindrone: Anhydrohydroxynorprogesterone; Anovulatorio; Anovule; Aygestin; Binovum; Brevicon; Brevinor; Brevinor 21; Brevinor 28; Brevinor-1 21; Brevinor-1 28; Camila; Ciclovulan; Conceplan; Conludaf; Conludag; Demulen; ENT; Errin; Estrinor; Ethinylnortestosterone; Ethynylmortestosterone; Ethynylnortestosterone; Gencept; Genora; Gestest; Jenest; Jenest-28; Loestrin; Menzol; Microneth; Micronett; Micronor; Micronovum; Milli; Mini-Pe; Mini-Pill; Minovlar; Modicon; N.E.E.; NET; Necon; Nelova; Neocon; Nodiol; Nor-Q.D.; Nor-Qd; Noraethisteronum; Noralutin; Norcept; Norcept-E; Norcolut; Noresthisterone; Norethadrone; Norethin; Norethin 1/35 E; Norethin 1/50 M; Norethindrone Acetate; Norethindrone Norethisterone; Norethisteron; Norethisterone; Norethisterone [Progestins]; Norethisteronum [Inn-Latin]; Norethyndron; Norethynodron; Norethynodrone; Noretisterona [Inn-Spanish]; Noretisterone [Dcit]; Norfor; Norgestin; Noriday; Noriday 28; Norimin; Norinyl; Norlestrin; Norlutate; Norluten; Norlutin; Norluton; Normapause; Norpregneninlone; Norpregneninolone; Norpregneninotone; Orlest; Ortho 1 35; Ortho 7 7 7; Ortho-Novum; Ortho-Novum 1 35; Ortho-Novum 1 50; Ortho-Novum 7 7 7; Ovcon; Ovysmen; Ovysmen 0.5 35; Ovysmen 1 35; Palonyl; Perovex; Primolut N; Primolut-N; Proluteasi; Synphase; Synphasic 28; Tri-Norinyl; Triella; Trinovum; Trinovum 21; Utovlan; Utovlar;
Absorption: Absolute oral bioavailability approximately 64%
Toxicity (Overdose): Not Available
Protein Binding: >95%
Biotransformation: Hepatic
Half Life: 7 hours
Dosage Forms of Orlest: Tablet Oral
Chemical IUPAC Name: (8R,9S,10R,13S,14S,17R)-17-ethynyl-17-hydroxy-13-methyl-1,2,6,7,8,9,10,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-3-one
Chemical Formula: C20H26O2
Norethindrone on Wikipedia: https://en.wikipedia.org/wiki/Norethindrone
Organisms Affected: Humans and other mammals