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Mifepristone | apollo +9191 46 950 950
Mifepristone | apollo +9191 46 950 950
Mifepristone
CAS Number : 84371-65-3
Molecular Formula : C29H35NO2
Molecular Weight : 429.5937 g/mol
Systematic (IUPAC) : (10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]-14-hydroxy-15-methyl-14-
(prop-1-yn-1-yl)tetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-1,6-
dien-5-one
Type : small molecule
Description : A progestational and glucocorticoid hormone antagonist. Its inhibition of progesterone induces bleeding during the luteal phase and in early
pregnancy by releasing endogenous prostaglandins from the endometrium or decidua. As a glucocorticoid
receptor antagonist, the drug has been used to treat hypercortisolism in patients with nonpituitary cushing
syndrome.
Categories
Contraceptives, Oral, Synthetic
Menstruation-Inducing Agents
Luteolytic Agents
Contraceptives, Postcoital, Synthetic
Hormone Antagonists
Abortifacient Agents, Steroidal
Taxonomy
Kingdom : Organic
Classes
Benzene and Derivatives
Cyclohexenes and Derivatives
Anilines
Substructures
Hydroxy Compounds
Alkanes and Alkenes
Alkynes
Aliphatic and Aryl Amines
Benzene and Derivatives
Alcohols and Polyols
Isoprenes
Aromatic compounds
Cyclohexenes and Derivatives
Anilines
Ketones
Pharmacology
Indication : For the medical termination of
intrauterine pregnancy through 49 days' pregnancy. Also indicated to control hyperglycemia secondary to
hypercortisolism in adult patients with endogenous Cushing's syndrome who have type 2 diabetes mellitus
or glucose intolerance.
Pharmacodynamics : Mifepristone is a synthetic
steroid with antiprogestational effects indicated for the medical termination of intrauterine pregnancy through
49 days' pregnancy. Doses of 1 mg/kg or greater of mifepristone have been shown to antagonize the
endometrial and myometrial effects of progesterone in women. During pregnancy, the compound sensitizes the
myometrium to the contraction-inducing activity of prostaglandins. Mifepristone also exhibits
antiglucocorticoid and weak antiandrogenic activity. The activity of the glucocorticoid dexamethasone in rats was
inhibited following doses of 10 to 25 mg/kg of mifepristone. Doses of 4.5 mg/kg or greater in human
beings resulted in a compensatory elevation of adrenocorticotropic hormone (ACTH) and cortisol.
Mechanism of action : The anti-progestational activity of mifepristone results from competitive
interaction with progesterone at progesterone-receptor sites. Based on studies with various oral doses in several animal species (mouse, rat, rabbit and monkey), the compound inhibits the activity of endogenous or
exogenous progesterone. The termination of pregnancy results. In the treatment of Cushing's syndrome, Mifepristone blocks the binding of cortisol to its
receptor. It does not decrease cortisol production but reduces the effects of excess cortisol, such as high blood
sugar levels.
Absorption : The absolute bioavailability of a 20 mg
oral dose is 69%
Protein binding : 98% (bound to plasma proteins,
albumin and a 1-acid glycoprotein)
Metabolism : Hepatic. Hepatic, by Cytochrome P450 3A4 isoenzyme to the N-monodemethylated metabolite (RU 42 633); RU 42 698, which results from the loss of two methyl groups from position 11 beta; and RU 42 698, which results from terminal hydroxylation of the
17–propynyl chain.
Route of elimination : Fecal: 83%; Renal: 9%.
Half life : 18 hours
Toxicity : Nearly all of the women who receive mifepristone will report adverse reactions, and many can be expected to report more than one such reaction.
About 90% of patients report adverse reactions following administration of misoprostol on day three of
the treatment procedure. Side effects include more heavy bleeding than a heavy manstrual period,
abdominal pain, uterine cramping, nausea, vomiting, and diarrhea.
Affected organisms : Humans and other mammals
Why is this medication prescribed?
Mifepristone is used alone or in combination with misoprostol (Cytotec) to end an early pregnancy. Early pregnancy means it has been 49 days or less since your last menstrual period began. Mifepristone is in a class of medications called antiprogestational steroids. It works by blocking the activity of progesterone, a substance
your body makes to help continue pregnancy.
How should this medicine be used?
Mifepristone comes as a tablet to take by mouth. It should be taken only in a clinic, medical office, or
hospital under the supervision of a qualified doctor. You will take three tablets of mifepristone at one time on the
first day. Two days later you must go back to your doctor. If your doctor is not certain that your pregnancy
has ended, you will take two tablets of another medication called misoprostol. You may have vaginal bleeding for 9 to 30 days or longer. Fourteen days after taking mifepristone, you must go back to your doctor for
an exam or ultrasound to make sure that the pregnancy has ended. Take mifepristone exactly as directed.
Other uses for this medicine
Mifepristone is also sometimes used to end pregnancies when more than 49 days have passed since the woman's last menstrual period; as an emergency contraceptive after unprotected sexual intercourse ('morning-after pill'); to treat tumors of the brain, endometriosis
(growth of uterus tissue outside the uterus), or fibroids (noncancerous tumors in the uterus); or to induce labor (to help start the birth process in a pregnant woman).
Talk to your doctor about the possible risks of using this drug for your condition.
What special precautions should I follow?
Before taking mifepristone,
tell your doctor if you are allergic to mifepristone; misoprostol (Arthrotec, Cytotec); other prostaglandins
such as alprostadil, carboprost tromethamine (Hemabate), dinoprostone (Cervidil, Prepidil, Prostin E2), epoprostenol (Flolan), latanoprost (Xalatan), treprostinil (Remodulin); or any other medications.
do not take mifepristone if you are taking any of the medications listed in the IMPORTANT WARNING section or corticosteroids such as beclomethasone
(QVAR inhaler), betamethasone (Celestone), budesonide (Entocort, Pulmicort), cortisone (Cortone),
dexamethasone (Decadron, Dexpak, Dexasone, others), fludrocortisone (Floriner), flunisolide (AeroBid);
fluticasone (Advair, Flovent), hydrocortisone (Cortef, Cortenema, Hydrocortone), methylprednisolone
(Medrol, Meprolone, others), prednisolone (Prelone,
others), prednisone (Deltasone, Meticorten, Sterapred, others), and triamcinolone (Aristocort, Azmacort).
tell your doctor what other prescription and nonprescription medications, vitamins, and nutritional supplements you are taking. Be sure to mention the medications listed in the IMPORTANT WARNING
section and any of the following: amiodarone (Cordarone, Pacerone); astemizole; benzodiazepines such as alprazolam (Xanax), diazepam (Valium),
midazolam (Versed), or triazolam (Halcion); buspirone (BuSpar); calcium channel blockers such as amlodipine (Norvasc), diltiazem (Cardizem, Dilacor, Tiazac, others),
felodipine (Lexxel, Plendil), nifedipine (Adalat, Procardia), nisoldipine (Sular), nitrendipine , or
verapamil (Calan, Isoptin, Verelan); carbamazepine (Tegretol); chlorpheniramine (antihistamine in cough and cold products); cholesterol-lowering medications (statins) such as atorvastatin (Lipitor), cerivastatin ,
lovastatin (Mevacor), or simvastatin (Zocor); cimetidine (Tagamet); cisapride; clarithromycin (Biaxin, Prevpac);
cyclosporine (Neoral, Sandimmune); dicloxacillin; erythromycin (E.E.S., EM-Mycin, Erythrocin);
fluoxetine (Prozac, Sarafem); fluvoxamine (Luvox); haloperidol; furosemide; HIV protease inhibitors such as indinavir (Crixivan), nelfinavir (Viracept), ritonavir
(Norvir), or saquinavir (Fortovase, Invirase); itraconazole (Sporanox); ketoconazole (Nizoral); methadone (Dolophine, Methadose); nefazodone
(Serzone); phenobarbital (Luminal, Solfoton); phenytoin (Dilantin); pimozide (Orap); propranolol (Inderal); quinidine; quinine; rifampin (Rifadin, Rimactane);
rifabutin (Mycobutin); tacrolimus (Prograf, Protopic); tamoxifen (Nolvadex); trazodone; troleandomycin (TAO); verapamil (Calan, Covera, Isoptin, Verelan,
others); or vincristine (Vincasar). Your doctor may need to change the doses of your medications or monitor you
carefully for side effects.
tell your doctor what herbal products you are taking, especially St. John's wort.
tell your doctor if you have or have ever had any of the conditions listed in the IMPORTANT WARNING section or any of the following: diabetes ; high blood pressure; porphyria (an inherited blood disease that may cause skin or nervous system problems); adrenal failure
(problems with your adrenal glands); or heart, kidney, liver, or lung disease.
tell your doctor if you have an intrauterine device (IUD) in place. It must be taken out before you take
mifepristone.
you should know that it is possible that mifepristone will not end your pregnancy. Your doctor will check to be
sure that your pregnancy has ended when you return for your follow-up appointments after you take
mifepristone. If your pregnancy has not ended, you may choose to have surgery to end the pregnancy. If you do not have this surgery, your baby may be born with birth
defects.
tell your doctor if you are breast-feeding. You may need to stop breast-feeding for a few days after taking
mifepristone.
if you are having surgery, including dental surgery, tell the doctor or dentist that you have taken mifepristone.
you should know that mifepristone may make you dizzy. Do not drive a car or operate machinery until you know
how this medication affects you.
tell your doctor if you smoke 10 or more cigarettes a dayor if you have a history of heavy smoking.
you should know that after ending a pregnancy with mifepristone, you can become pregnant again right away, even before your period returns. If you do not
want to become pregnant again, you should begin using birth control as soon as this pregnancy ends or before
you start having sexual intercourse again.
What special dietary instructions should I
follow?
Do not take mifepristone with grapefruit juice. Talk to your doctor about drinking grapefruit juice after taking
this medication.
What should I do if I forget a dose?
You will only take mifepristone in your doctor's office or clinic, so you do not have to worry about forgetting to
take a dose at home.
What side effects can this medication cause?
Mifepristone may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:
vaginal bleeding or spotting
cramps
pelvic pain
vaginal burning, itching, or discharge
headache
tiredness
difficulty falling asleep or staying asleep
anxiety
back or leg pain
Some side effects can be serious. If you experience any of the symptoms mentioned in the IMPORTANT
WARNING section, call your doctor immediately.
Mifepristone may cause other side effects. Call your doctor if you have any unusual problems while taking
this medication.
What storage conditions are needed for this
medicine?
Your doctor will store the medication in his or her office.
Symptoms of overdose may include
dizziness
fainting
blurred vision
nausea
tiredness
weakness
shortness of breath
fast heartbeat
What other information should I know?
You should get mifepristone only from a doctor and use this medication only while under the care of a doctor. You should not buy mifepristone from other sources,
such as the Internet, because you would bypass important safeguards to protect your health.
Do not let anyone else take your medication.
It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such
as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of
emergencies.
Warning
Rarely, serious medical problems can occur when a pregnancyends (e.g., due to medical abortion with
medications including mifepristone, surgical abortion, miscarriage), including sometimes fatal infections and bleeding. Read the Medication Guide, read and sign the Patient Agreement, and consult your doctor if you have
any questions.
Your doctor must give you clear instructions regarding whom to call and what to do in case of an emergency
(e.g., severe bleeding, infection). If you go to the emergency room or visit another health care
professional, show them the Medication Guide so they know you are having a medical abortion.
Seek immediate medical attention if you experience symptoms such as severe abdominal pain, fainting, fast heartbeat, fever lasting more than 4 hours. You may have a very serious infection even if you do not have a fever. Therefore, seek immediate medical attention if you have abdominal pain or feel sick (e.g., nausea,
vomiting, diarrhea, weakness) more than 24 hours after taking the second drug (misoprostol), even if you do not have a fever. Also seek immediate medical attention if
you have continued heavy bleeding, which may be a sign of an incomplete abortion or other serious medical
problem. You may need surgery or other medical care. See also Side Effects section.
apollo | asia Division
APOLLO Pharmaceuticals API Manufacturer INDIA [P] Ltd.|asia Division
Mr.Vipin Saxena|CEO
Cellular:+91-98-21050033
Cellular:+91-98-20150033
Direct :+91-22-65785588
FAX :+91-22-42950001
Wireline Purchase HELPDESK:
+91-22-65050001
+91-22-65650001
Wireline Sales HELPDESK:
+91-22-65500009
+91-22-65050009
Wireless 24x7 HELPDESK:
+9191-46-951951
+9191-46-950950
Blackberry Pin :
32E6500D | 32E65010 | 28415C58
Email:
www.apolloworld.in
www.apollopharma.in
www.apollopharmaceuticals.Net
Chat:
MSN Hotmail:VipinrSaxena
Skype NAME:VipinrSaxena
Rocketmail:VipinrSaxena
Google mail:VipinrSaxena
BlackBerry:28415C58
Regd. Office :-
1104, Maker Chamber V,
Nariman Point
Mumbai, INDIA
Pin:400021
Industrial Office
D-62, OIC India
Oshiwara Industrial Centre,
New Link Road,
Goregoan West,
Mumbai, INDIA
Pin:400104
Manufacturing Unit Address:
Plot No. 117A,
Village: Chamble
Near MonaTona Limited.Wada,
Maharashtra,
PIN : 421312 | INDIA
Email:
www.apollo.mn | www.apollo.com.co | www.apollopharmaceuticals.Com
Mifepristone | apollo +9191 46 950 950
Mifepristone | apollo +9191 46 950 950
Mifepristone
CAS Number : 84371-65-3
Molecular Formula : C29H35NO2
Molecular Weight : 429.5937 g/mol Systematic (IUPAC) : (10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]-14-hydroxy-15-methyl-14-
(prop-1-yn-1-yl)tetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-1,6-
dien-5-one
Type : small molecule
Description : A progestational and glucocorticoid hormone antagonist. Its inhibition of progesterone induces bleeding during the luteal phase and in early
pregnancy by releasing endogenous prostaglandins from the endometrium or decidua. As a glucocorticoid
receptor antagonist, the drug has been used to treat hypercortisolism in patients with nonpituitary cushing
syndrome.
Categories
Contraceptives, Oral, Synthetic
Menstruation-Inducing Agents
Luteolytic Agents
Contraceptives, Postcoital, Synthetic
Hormone Antagonists
Abortifacient Agents, Steroidal
Taxonomy
Kingdom : Organic
Classes
Benzene and Derivatives
Cyclohexenes and Derivatives
Anilines
Substructures
Hydroxy Compounds
Alkanes and Alkenes
Alkynes
Aliphatic and Aryl Amines
Benzene and Derivatives
Alcohols and Polyols
Isoprenes
Aromatic compounds
Cyclohexenes and Derivatives
Anilines
Ketones
Pharmacology
Indication : For the medical termination of intrauterine pregnancy through 49 days' pregnancy. Also
indicated to control hyperglycemia secondary to hypercortisolism in adult patients with endogenous
Cushing's syndrome who have type 2 diabetes mellitus or glucose intolerance.
Pharmacodynamics : Mifepristone is a synthetic steroid with antiprogestational effects indicated for the medical termination of intrauterine pregnancy through
49 days' pregnancy. Doses of 1 mg/kg or greater of mifepristone have been shown to antagonize the
endometrial and myometrial effects of progesterone in women. During pregnancy, the compound sensitizes the
myometrium to the contraction-inducing activity of prostaglandins. Mifepristone also exhibits
antiglucocorticoid and weak antiandrogenic activity. The activity of the glucocorticoid dexamethasone in rats was
inhibited following doses of 10 to 25 mg/kg of mifepristone. Doses of 4.5 mg/kg or greater in human
beings resulted in a compensatory elevation of adrenocorticotropic hormone (ACTH) and cortisol.
Mechanism of action : The anti-progestational activity of mifepristone results from competitive
interaction with progesterone at progesterone-receptor sites. Based on studies with various oral doses in several animal species (mouse, rat, rabbit and monkey), the compound inhibits the activity of endogenous or
exogenous progesterone. The termination of pregnancy results. In the treatment of Cushing's syndrome, Mifepristone blocks the binding of cortisol to its
receptor. It does not decrease cortisol production but reduces the effects of excess cortisol, such as high blood
sugar levels.
Absorption : The absolute bioavailability of a 20 mg oral dose is 69%
Protein binding : 98% (bound to plasma proteins, albumin and a 1-acid glycoprotein)
Metabolism : Hepatic. Hepatic, by Cytochrome P450 3A4 isoenzyme to the N-monodemethylated metabolite (RU 42 633); RU 42 698, which results from the loss of two methyl groups from position 11 beta; and RU 42 698, which results from terminal hydroxylation of the
17–propynyl chain.
Route of elimination : Fecal: 83%; Renal: 9%.
Half life : 18 hours
Toxicity : Nearly all of the women who receive mifepristone will report adverse reactions, and many can be expected to report more than one such reaction.
About 90% of patients report adverse reactions following administration of misoprostol on day three of
the treatment procedure. Side effects include more heavy bleeding than a heavy manstrual period,
abdominal pain, uterine cramping, nausea, vomiting, and diarrhea.
Affected organisms : Humans and other mammals
Why is this medication prescribed?
Mifepristone is used alone or in combination with misoprostol (Cytotec) to end an early pregnancy. Early pregnancy means it has been 49 days or less since your last menstrual period began. Mifepristone is in a class of medications called antiprogestational steroids. It works by blocking the activity of progesterone, a substance
your body makes to help continue pregnancy.
How should this medicine be used?
Mifepristone comes as a tablet to take by mouth. It should be taken only in a clinic, medical office, or
hospital under the supervision of a qualified doctor. You will take three tablets of mifepristone at one time on the
first day. Two days later you must go back to your doctor. If your doctor is not certain that your pregnancy
has ended, you will take two tablets of another medication called misoprostol. You may have vaginal bleeding for 9 to 30 days or longer. Fourteen days after taking mifepristone, you must go back to your doctor for
an exam or ultrasound to make sure that the pregnancy has ended. Take mifepristone exactly as directed.
Other uses for this medicine
Mifepristone is also sometimes used to end pregnancies when more than 49 days have passed since the woman's last menstrual period; as an emergency contraceptive after unprotected sexual intercourse ('morning-after pill'); to treat tumors of the brain, endometriosis
(growth of uterus tissue outside the uterus), or fibroids (noncancerous tumors in the uterus); or to induce labor (to help start the birth process in a pregnant woman).
Talk to your doctor about the possible risks of using this drug for your condition.
What special precautions should I follow?
Before taking mifepristone, tell your doctor if you are allergic to mifepristone;
misoprostol (Arthrotec, Cytotec); other prostaglandins such as alprostadil, carboprost tromethamine
(Hemabate), dinoprostone (Cervidil, Prepidil, Prostin E2), epoprostenol (Flolan), latanoprost (Xalatan), treprostinil (Remodulin); or any other medications. do not take mifepristone if you are taking any of the medications listed in the IMPORTANT WARNING section or corticosteroids such as beclomethasone
(QVAR inhaler), betamethasone (Celestone), budesonide (Entocort, Pulmicort), cortisone (Cortone),
dexamethasone (Decadron, Dexpak, Dexasone, others), fludrocortisone (Floriner), flunisolide (AeroBid);
fluticasone (Advair, Flovent), hydrocortisone (Cortef, Cortenema, Hydrocortone), methylprednisolone
(Medrol, Meprolone, others), prednisolone (Prelone,
others), prednisone (Deltasone, Meticorten, Sterapred, others), and triamcinolone (Aristocort, Azmacort).
tell your doctor what other prescription and nonprescription medications, vitamins, and nutritional supplements you are taking. Be sure to mention the medications listed in the IMPORTANT WARNING
section and any of the following: amiodarone (Cordarone, Pacerone); astemizole; benzodiazepines such as alprazolam (Xanax), diazepam (Valium),
midazolam (Versed), or triazolam (Halcion); buspirone (BuSpar); calcium channel blockers such as amlodipine (Norvasc), diltiazem (Cardizem, Dilacor, Tiazac, others),
felodipine (Lexxel, Plendil), nifedipine (Adalat, Procardia), nisoldipine (Sular), nitrendipine , or
verapamil (Calan, Isoptin, Verelan); carbamazepine (Tegretol); chlorpheniramine (antihistamine in cough and cold products); cholesterol-lowering medications (statins) such as atorvastatin (Lipitor), cerivastatin ,
lovastatin (Mevacor), or simvastatin (Zocor); cimetidine (Tagamet); cisapride; clarithromycin (Biaxin, Prevpac);
cyclosporine (Neoral, Sandimmune); dicloxacillin; erythromycin (E.E.S., EM-Mycin, Erythrocin);
fluoxetine (Prozac, Sarafem); fluvoxamine (Luvox); haloperidol; furosemide; HIV protease inhibitors such as indinavir (Crixivan), nelfinavir (Viracept), ritonavir
(Norvir), or saquinavir (Fortovase, Invirase); itraconazole (Sporanox); ketoconazole (Nizoral); methadone (Dolophine, Methadose); nefazodone
(Serzone); phenobarbital (Luminal, Solfoton); phenytoin (Dilantin); pimozide (Orap); propranolol (Inderal); quinidine; quinine; rifampin (Rifadin, Rimactane);
rifabutin (Mycobutin); tacrolimus (Prograf, Protopic); tamoxifen (Nolvadex); trazodone; troleandomycin (TAO); verapamil (Calan, Covera, Isoptin, Verelan,
others); or vincristine (Vincasar). Your doctor may need to change the doses of your medications or monitor you
carefully for side effects. tell your doctor what herbal products you are taking,
especially St. John's wort. tell your doctor if you have or have ever had any of the
conditions listed in the IMPORTANT WARNING section or any of the following: diabetes ; high blood pressure; porphyria (an inherited blood disease that may cause skin or nervous system problems); adrenal failure
(problems with your adrenal glands); or heart, kidney, liver, or lung disease.
tell your doctor if you have an intrauterine device (IUD) in place. It must be taken out before you take
mifepristone. you should know that it is possible that mifepristone will not end your pregnancy. Your doctor will check to be
sure that your pregnancy has ended when you return for your follow-up appointments after you take
mifepristone. If your pregnancy has not ended, you may choose to have surgery to end the pregnancy. If you do not have this surgery, your baby may be born with birth
defects. tell your doctor if you are breast-feeding. You may need
to stop breast-feeding for a few days after taking mifepristone.
if you are having surgery, including dental surgery, tell the doctor or dentist that you have taken mifepristone. you should know that mifepristone may make you dizzy. Do not drive a car or operate machinery until you know
how this medication affects you. tell your doctor if you smoke 10 or more cigarettes a
dayor if you have a history of heavy smoking.
you should know that after ending a pregnancy with mifepristone, you can become pregnant again right away, even before your period returns. If you do not
want to become pregnant again, you should begin using birth control as soon as this pregnancy ends or before
you start having sexual intercourse again.
What special dietary instructions should I follow?
Do not take mifepristone with grapefruit juice. Talk to your doctor about drinking grapefruit juice after taking
this medication.
What should I do if I forget a dose?
You will only take mifepristone in your doctor's office or clinic, so you do not have to worry about forgetting to
take a dose at home.
What side effects can this medication cause?
Mifepristone may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:
vaginal bleeding or spotting
cramps
pelvic pain
vaginal burning, itching, or discharge
headache
tiredness
difficulty falling asleep or staying asleep
anxiety
back or leg pain
Some side effects can be serious. If you experience any of the symptoms mentioned in the IMPORTANT
WARNING section, call your doctor immediately.
Mifepristone may cause other side effects. Call your doctor if you have any unusual problems while taking
this medication.
What storage conditions are needed for this medicine?
Your doctor will store the medication in his or her office.
Symptoms of overdose may include
dizziness
fainting
blurred vision
nausea
tiredness
weakness
shortness of breath
fast heartbeat
What other information should I know?
You should get mifepristone only from a doctor and use this medication only while under the care of a doctor. You should not buy mifepristone from other sources,
such as the Internet, because you would bypass important safeguards to protect your health. Do not let anyone else take your medication.
It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such
as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of
emergencies.
Warning
Rarely, serious medical problems can occur when a pregnancyends (e.g., due to medical abortion with
medications including mifepristone, surgical abortion, miscarriage), including sometimes fatal infections and bleeding. Read the Medication Guide, read and sign the Patient Agreement, and consult your doctor if you have
any questions. Your doctor must give you clear instructions regarding whom to call and what to do in case of an emergency
(e.g., severe bleeding, infection). If you go to the emergency room or visit another health care
professional, show them the Medication Guide so they know you are having a medical abortion.
Seek immediate medical attention if you experience symptoms such as severe abdominal pain, fainting, fast heartbeat, fever lasting more than 4 hours. You may have a very serious infection even if you do not have a fever. Therefore, seek immediate medical attention if you have abdominal pain or feel sick (e.g., nausea,
vomiting, diarrhea, weakness) more than 24 hours after taking the second drug (misoprostol), even if you do not have a fever. Also seek immediate medical attention if
you have continued heavy bleeding, which may be a sign of an incomplete abortion or other serious medical
problem. You may need surgery or other medical care. See also Side Effects section.
apollo | asia Division
APOLLO Pharmaceuticals API Manufacturer INDIA [P] Ltd.|asia Division
Mr.Vipin Saxena|CEO
Cellular:+91-98-21050033
Cellular:+91-98-20150033
Direct :+91-22-65785588
FAX :+91-22-42950001
Wireline Purchase HELPDESK:
+91-22-65050001
+91-22-65650001
Wireline Sales HELPDESK:
+91-22-65500009
+91-22-65050009
Wireless 24x7 HELPDESK:
+9191-46-951951
+9191-46-950950
Blackberry Pin :
32E6500D | 32E65010 | 28415C58
Email:
www.apolloworld.in
www.apollopharma.in
www.apollopharmaceuticals.Net
Chat:
MSN Hotmail:VipinrSaxena
Skype NAME:VipinrSaxena
Rocketmail:VipinrSaxena
Google mail:VipinrSaxena
BlackBerry:28415C58
Regd. Office :-
1104, Maker Chamber V,
Nariman Point
Mumbai, INDIA
Pin:400021
Industrial Office
D-62, OIC India
Oshiwara Industrial Centre,
New Link Road,
Goregoan West,
Mumbai, INDIA
Pin:400104
Manufacturing Unit Address:
Plot No. 117A,
Village: Chamble
Near MonaTona Limited.Wada,
Maharashtra,
PIN : 421312 | INDIA
Email:
www.apollo.mn | www.apollo.com.co | www.apollopharmaceuticals.Com
MAY
19
Mifepristone | apollo +9191 46 950 950
Mifepristone | apollo +9191 46 950 950
Mifepristone | apollo +9191 46 950 950
Mifepristone
CAS Number : 84371-65-3
Molecular Formula : C29H35NO2
Molecular Weight : 429.5937 g/mol Systematic (IUPAC) : (10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]-14-hydroxy-15-methyl-14-
(prop-1-yn-1-yl)tetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-1,6-
dien-5-one
Type : small molecule
Description : A progestational and glucocorticoid hormone antagonist. Its inhibition of progesterone induces bleeding during the luteal phase and in early
pregnancy by releasing endogenous prostaglandins from the endometrium or decidua. As a glucocorticoid
receptor antagonist, the drug has been used to treat hypercortisolism in patients with nonpituitary cushing
syndrome.
Categories
Contraceptives, Oral, Synthetic
Menstruation-Inducing Agents
Luteolytic Agents
Contraceptives, Postcoital, Synthetic
Hormone Antagonists
Abortifacient Agents, Steroidal
Taxonomy
Kingdom : Organic
Classes
Benzene and Derivatives
Cyclohexenes and Derivatives
Anilines
Substructures
Hydroxy Compounds
Alkanes and Alkenes
Alkynes
Aliphatic and Aryl Amines
Benzene and Derivatives
Alcohols and Polyols
Isoprenes
Aromatic compounds
Cyclohexenes and Derivatives
Anilines
Ketones
Pharmacology
Indication : For the medical termination of intrauterine pregnancy through 49 days' pregnancy. Also
indicated to control hyperglycemia secondary to hypercortisolism in adult patients with endogenous
Cushing's syndrome who have type 2 diabetes mellitus or glucose intolerance.
Pharmacodynamics : Mifepristone is a synthetic steroid with antiprogestational effects indicated for the medical termination of intrauterine pregnancy through
49 days' pregnancy. Doses of 1 mg/kg or greater of mifepristone have been shown to antagonize the
endometrial and myometrial effects of progesterone in women. During pregnancy, the compound sensitizes the
myometrium to the contraction-inducing activity of prostaglandins. Mifepristone also exhibits
antiglucocorticoid and weak antiandrogenic activity. The activity of the glucocorticoid dexamethasone in rats was
inhibited following doses of 10 to 25 mg/kg of mifepristone. Doses of 4.5 mg/kg or greater in human
beings resulted in a compensatory elevation of adrenocorticotropic hormone (ACTH) and cortisol.
Mechanism of action : The anti-progestational activity of mifepristone results from competitive
interaction with progesterone at progesterone-receptor sites. Based on studies with various oral doses in several animal species (mouse, rat, rabbit and monkey), the compound inhibits the activity of endogenous or
exogenous progesterone. The termination of pregnancy results. In the treatment of Cushing's syndrome, Mifepristone blocks the binding of cortisol to its
receptor. It does not decrease cortisol production but reduces the effects of excess cortisol, such as high blood
sugar levels.
Absorption : The absolute bioavailability of a 20 mg oral dose is 69%
Protein binding : 98% (bound to plasma proteins, albumin and a 1-acid glycoprotein)
Metabolism : Hepatic. Hepatic, by Cytochrome P450 3A4 isoenzyme to the N-monodemethylated metabolite (RU 42 633); RU 42 698, which results from the loss of two methyl groups from position 11 beta; and RU 42 698, which results from terminal hydroxylation of the
17–propynyl chain.
Route of elimination : Fecal: 83%; Renal: 9%.
Half life : 18 hours
Toxicity : Nearly all of the women who receive mifepristone will report adverse reactions, and many can be expected to report more than one such reaction.
About 90% of patients report adverse reactions following administration of misoprostol on day three of
the treatment procedure. Side effects include more heavy bleeding than a heavy manstrual period,
abdominal pain, uterine cramping, nausea, vomiting, and diarrhea.
Affected organisms : Humans and other mammals
Why is this medication prescribed?
Mifepristone is used alone or in combination with misoprostol (Cytotec) to end an early pregnancy. Early pregnancy means it has been 49 days or less since your last menstrual period began. Mifepristone is in a class of medications called antiprogestational steroids. It works by blocking the activity of progesterone, a substance
your body makes to help continue pregnancy.
How should this medicine be used?
Mifepristone comes as a tablet to take by mouth. It should be taken only in a clinic, medical office, or
hospital under the supervision of a qualified doctor. You will take three tablets of mifepristone at one time on the
first day. Two days later you must go back to your doctor. If your doctor is not certain that your pregnancy
has ended, you will take two tablets of another medication called misoprostol. You may have vaginal bleeding for 9 to 30 days or longer. Fourteen days after taking mifepristone, you must go back to your doctor for
an exam or ultrasound to make sure that the pregnancy has ended. Take mifepristone exactly as directed.
Other uses for this medicine
Mifepristone is also sometimes used to end pregnancies when more than 49 days have passed since the woman's last menstrual period; as an emergency contraceptive after unprotected sexual intercourse ('morning-after pill'); to treat tumors of the brain, endometriosis
(growth of uterus tissue outside the uterus), or fibroids (noncancerous tumors in the uterus); or to induce labor (to help start the birth process in a pregnant woman).
Talk to your doctor about the possible risks of using this drug for your condition.
What special precautions should I follow?
Before taking mifepristone, tell your doctor if you are allergic to mifepristone;
misoprostol (Arthrotec, Cytotec); other prostaglandins such as alprostadil, carboprost tromethamine
(Hemabate), dinoprostone (Cervidil, Prepidil, Prostin E2), epoprostenol (Flolan), latanoprost (Xalatan), treprostinil (Remodulin); or any other medications. do not take mifepristone if you are taking any of the medications listed in the IMPORTANT WARNING section or corticosteroids such as beclomethasone
(QVAR inhaler), betamethasone (Celestone), budesonide (Entocort, Pulmicort), cortisone (Cortone),
dexamethasone (Decadron, Dexpak, Dexasone, others), fludrocortisone (Floriner), flunisolide (AeroBid);
fluticasone (Advair, Flovent), hydrocortisone (Cortef, Cortenema, Hydrocortone), methylprednisolone
(Medrol, Meprolone, others), prednisolone (Prelone,
others), prednisone (Deltasone, Meticorten, Sterapred, others), and triamcinolone (Aristocort, Azmacort).
tell your doctor what other prescription and nonprescription medications, vitamins, and nutritional supplements you are taking. Be sure to mention the medications listed in the IMPORTANT WARNING
section and any of the following: amiodarone (Cordarone, Pacerone); astemizole; benzodiazepines such as alprazolam (Xanax), diazepam (Valium),
midazolam (Versed), or triazolam (Halcion); buspirone (BuSpar); calcium channel blockers such as amlodipine (Norvasc), diltiazem (Cardizem, Dilacor, Tiazac, others),
felodipine (Lexxel, Plendil), nifedipine (Adalat, Procardia), nisoldipine (Sular), nitrendipine , or
verapamil (Calan, Isoptin, Verelan); carbamazepine (Tegretol); chlorpheniramine (antihistamine in cough and cold products); cholesterol-lowering medications (statins) such as atorvastatin (Lipitor), cerivastatin ,
lovastatin (Mevacor), or simvastatin (Zocor); cimetidine (Tagamet); cisapride; clarithromycin (Biaxin, Prevpac);
cyclosporine (Neoral, Sandimmune); dicloxacillin; erythromycin (E.E.S., EM-Mycin, Erythrocin);
fluoxetine (Prozac, Sarafem); fluvoxamine (Luvox); haloperidol; furosemide; HIV protease inhibitors such as indinavir (Crixivan), nelfinavir (Viracept), ritonavir
(Norvir), or saquinavir (Fortovase, Invirase); itraconazole (Sporanox); ketoconazole (Nizoral); methadone (Dolophine, Methadose); nefazodone
(Serzone); phenobarbital (Luminal, Solfoton); phenytoin (Dilantin); pimozide (Orap); propranolol (Inderal); quinidine; quinine; rifampin (Rifadin, Rimactane);
rifabutin (Mycobutin); tacrolimus (Prograf, Protopic); tamoxifen (Nolvadex); trazodone; troleandomycin (TAO); verapamil (Calan, Covera, Isoptin, Verelan,
others); or vincristine (Vincasar). Your doctor may need to change the doses of your medications or monitor you
carefully for side effects. tell your doctor what herbal products you are taking,
especially St. John's wort. tell your doctor if you have or have ever had any of the
conditions listed in the IMPORTANT WARNING section or any of the following: diabetes ; high blood pressure; porphyria (an inherited blood disease that may cause skin or nervous system problems); adrenal failure
(problems with your adrenal glands); or heart, kidney, liver, or lung disease.
tell your doctor if you have an intrauterine device (IUD) in place. It must be taken out before you take
mifepristone. you should know that it is possible that mifepristone will not end your pregnancy. Your doctor will check to be
sure that your pregnancy has ended when you return for your follow-up appointments after you take
mifepristone. If your pregnancy has not ended, you may choose to have surgery to end the pregnancy. If you do not have this surgery, your baby may be born with birth
defects. tell your doctor if you are breast-feeding. You may need
to stop breast-feeding for a few days after taking mifepristone.
if you are having surgery, including dental surgery, tell the doctor or dentist that you have taken mifepristone. you should know that mifepristone may make you dizzy. Do not drive a car or operate machinery until you know
how this medication affects you. tell your doctor if you smoke 10 or more cigarettes a
dayor if you have a history of heavy smoking.
you should know that after ending a pregnancy with mifepristone, you can become pregnant again right away, even before your period returns. If you do not
want to become pregnant again, you should begin using birth control as soon as this pregnancy ends or before
you start having sexual intercourse again.
What special dietary instructions should I follow?
Do not take mifepristone with grapefruit juice. Talk to your doctor about drinking grapefruit juice after taking
this medication.
What should I do if I forget a dose?
You will only take mifepristone in your doctor's office or clinic, so you do not have to worry about forgetting to
take a dose at home.
What side effects can this medication cause?
Mifepristone may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:
vaginal bleeding or spotting
cramps
pelvic pain
vaginal burning, itching, or discharge
headache
tiredness
difficulty falling asleep or staying asleep
anxiety
back or leg pain
Some side effects can be serious. If you experience any of the symptoms mentioned in the IMPORTANT
WARNING section, call your doctor immediately.
Mifepristone may cause other side effects. Call your doctor if you have any unusual problems while taking
this medication.
What storage conditions are needed for this medicine?
Your doctor will store the medication in his or her office.
Symptoms of overdose may include
dizziness
fainting
blurred vision
nausea
tiredness
weakness
shortness of breath
fast heartbeat
What other information should I know?
You should get mifepristone only from a doctor and use this medication only while under the care of a doctor. You should not buy mifepristone from other sources,
such as the Internet, because you would bypass important safeguards to protect your health. Do not let anyone else take your medication.
It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such
as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of
emergencies.
Warning
Rarely, serious medical problems can occur when a pregnancyends (e.g., due to medical abortion with
medications including mifepristone, surgical abortion, miscarriage), including sometimes fatal infections and bleeding. Read the Medication Guide, read and sign the Patient Agreement, and consult your doctor if you have
any questions. Your doctor must give you clear instructions regarding whom to call and what to do in case of an emergency
(e.g., severe bleeding, infection). If you go to the emergency room or visit another health care
professional, show them the Medication Guide so they know you are having a medical abortion.
Seek immediate medical attention if you experience symptoms such as severe abdominal pain, fainting, fast heartbeat, fever lasting more than 4 hours. You may have a very serious infection even if you do not have a fever. Therefore, seek immediate medical attention if you have abdominal pain or feel sick (e.g., nausea,
vomiting, diarrhea, weakness) more than 24 hours after taking the second drug (misoprostol), even if you do not have a fever. Also seek immediate medical attention if
you have continued heavy bleeding, which may be a sign of an incomplete abortion or other serious medical
problem. You may need surgery or other medical care. See also Side Effects section.
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