Rupek may be available in the countries listed below.
Ingredient matches for Rupek
Phytomenadione
Phytomenadione is reported as an ingredient of Rupek in the following countries:
- Argentina
International Drug Name Search
Wednesday, 28 September 2016
Prevident 5000 Sensitive
sodium fluoride and potassium nitrate gel
Dosage Form: gel, dentifrice
Colgate®
PreviDent®5000 ppm
SENSITIVE
Rx ONLY
1.1% Sodium Fluoride, 5% Potassium Nitrate
Prescription Strength Toothpaste for Sensitive Teeth
Prevident 5000 Sensitive Description
Self-topical neutral fluoride toothpaste containing 1.1% (w/w) sodium fluoride and 5% potassium nitrate.
Active Ingredients
Sodium fluoride 1.1% (w/w), Potassium nitrate 5%
Inactive Ingredients
water, hydrated silica, sorbitol, PEG-12, carrageenan, sodium lauryl sulfate, flavor, poloxamer 407, cocamidopropyl betaine, sodium saccharin, mica, sodium hydroxide, titanium dioxide, D&C yellow no. 10, FD&C blue no. 1
Prevident 5000 Sensitive - Clinical Pharmacology
Frequent topical applications to the teeth with preparations having a relatively high fluoride content increase tooth resistance to acid dissolution and enhance penetration of the fluoride ion into tooth enamel.
Indications and Usage for Prevident 5000 Sensitive
A dental caries preventive and sensitive teeth toothpaste; for twice daily self-applied topical use, followed by rinsing. Helps reduce the painful sensitivity of the teeth to cold, heat, acids, sweets or contact in adult patients and children 12 years of age and older. It is well established that 1.1% sodium fluoride is safe and extraordinarily effective as a caries preventive when applied frequently with mouthpiece applicators. 1-4 PreviDent® 5000 Sensitive brand of 1.1% sodium fluoride toothpaste with 5% potassium nitrate in a squeeze bottle is easily applied onto a toothbrush. This prescription toothpaste should be used twice daily in place of your regular toothpaste unless otherwise instructed by your dental professional. May be used in areas where drinking water is fluoridated since topical fluoride cannot produce fluorosis. (See WARNINGS for exception.)
Contraindications
Do not use in pediatric patients under age 12 years unless recommended by a dentist or physician.
Warnings
Not for systemic treatment - DO NOT SWALLOW. Keep out of reach of infants and children. Children under 12 years of age, consult a dentist or physician.
Note: Sensitive teeth may indicate a serious problem that may need prompt care by a dentist. See your dentist if the problem persists or worsens. Do not use this product longer than 4 weeks unless recommended by a dentist or physician.
Precautions
General
Not for systemic treatment. DO NOT SWALLOW.
Carcinogenesis, Mutagenesis, Impairment of Fertility
In a study conducted in rodents, no carcinogenesis was found in male and female mice and female rats treated with fluoride at dose levels ranging from 4.1 to 9.1 mg/kg of body weight. Equivocal evidence of carcinogenesis was reported in male rats treated with 2.5 and 4.1 mg/kg of body weight. In a second study, no carcinogenesis was observed in rats, males or females, treated with fluoride up to 11.3 mg/kg of body weight. Epidemiological data provide no credible evidence for an association between fluoride, either naturally occurring or added to drinking water, and risk of human cancer.
Fluoride ion is not mutagenic in standard bacterial systems. It has been shown that fluoride ion has potential to induce chromosome aberrations in cultured human and rodent cells at doses much higher than those to which humans are exposed. In vivo data are conflicting. Some studies report chromosome damage in rodents, while other studies using similar protocols report negative results.
Potential adverse reproductive effects of fluoride exposure in humans has not been adequately evaluated. Adverse effects on reproduction were reported for rats, mice, fox, and cattle exposed to 100 ppm or greater concentrations of fluoride in their diet or drinking water. Other studies conducted in rats demonstrated that lower concentrations of fluoride (5 mg/kg of body weight) did not result in impaired fertility and reproductive capabilities.
Pregnancy
Teratogenic Effects
Pregnancy Category B
It has been shown that fluoride crosses the placenta of rats, but only 0.01% of the amount administered is incorporated in fetal tissue. Animal studies (rats, mice, rabbits) have shown that fluoride is not a teratogen. Maternal exposure to 12.2 mg fluoride/kg of body weight (rats) or 13.1 mg/kg of body weight (rabbits) did not affect the litter size or fetal weight and did not increase the frequency of skeletal or visceral malformations. There are no adequate and well-controlled studies in pregnant women. However, epidemiological studies conducted in areas with high levels of naturally fluoridated water showed no increase in birth defects. Heavy exposure to fluoride during in utero development may result in skeletal fluorosis which becomes evident in childhood.
Nursing Mothers
It is not known if fluoride is excreted in human milk. However, many drugs are excreted in milk, and caution should be exercised when products containing fluoride are administered to a nursing woman. Reduced milk production was reported in farm-raised fox when the animals were fed a diet containing a high concentration of fluoride (98-137 mg/kg of body weight). No adverse effects on parturition, lactation, or offspring were seen in rats administered fluoride up to 5 mg/kg of body weight.
Pediatric Use
Safety and effectiveness in pediatric patients below the age of 12 years have not been established. Please refer to the CONTRAINDICATIONS and WARNINGS sections.
Geriatric Use
Of the total number of subjects in clinical studies of 1.1% (w/v) sodium fluoride, 15 percent were 65 and over, while 1 percent were 75 and over. No overall differences in safety or effectiveness were observed between these subjects and younger subjects, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out. This drug is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and it may be useful to monitor renal function.5
Adverse Reactions
Allergic reactions and other idiosyncrasies have been rarely reported.
Overdosage
Accidental ingestion of large amounts of fluoride may result in acute burning in the mouth and sore tongue. Nausea, vomiting, and diarrhea may occur soon after ingestion (within 30 minutes) and are accompanied by salivation, hematemesis, and epigastric cramping abdominal pain. These symptoms may persist for 24 hours. If less than 5 mg fluoride/kg body weight (i.e., less than 2.3 mg fluoride/lb body weight) have been ingested, give calcium (e.g., milk) orally to relieve gastrointestinal symptoms and observe for a few hours. If more than 5 mg fluoride/kg body weight (i.e., more than 2.3 mg fluoride/lb body weight) have been ingested, induce vomiting, give orally soluble calcium (e.g., milk, 5% calcium gluconate or calcium lactate solution) and immediately seek medical assistance. For accidental ingestion of more than 15 mg fluoride/kg of body weight (i.e., more than 6.9 mg fluoride/lb body weight), induce vomiting and admit immediately to a hospital facility.
A treatment dose (a thin ribbon) of PreviDent® 5000 Sensitive contains approximately 2.5 mg fluoride. A 3.4 FL OZ (100 mL) bottle contains approximately 575 mg fluoride.
Prevident 5000 Sensitive Dosage and Administration
Follow these instructions unless otherwise instructed by your dental professional:
- Adults and children 12 years of age and older: Apply at least 1 inch strip of PreviDent® 5000 Sensitive onto a soft bristle toothbrush. Brush teeth thoroughly for at least 1 minute, expectorate, and rinse mouth thoroughly.
- Use twice a day (morning and evening) or as recommended by a dentist or physician. Make sure to brush all sensitive areas of the teeth. Children under 12 years of age: Consult a dentist or physician.
How is Prevident 5000 Sensitive Supplied
3.4 FL OZ (100 mL) in plastic bottles. Mild Mint: NDC 0126-0070-61
STORAGE
Store at Controlled Room Temperature, 68-77°F (20-25°C)
REFERENCES
- American Dental Association, Accepted Dental Therapeutics Ed. 40 (Chicago, 1984): 405-407.
- H.R. Englander et al., JADA 75 (1967): 638-644.
- H.R. Englander et al., JADA 78 (1969): 783-787.
- H.R. Englander et al., JADA 83 (1971): 354-358.
- Data on file, Colgate Oral Pharmaceuticals.
Questions? Comments? Please Call 1-800-962-2345
www.colgateprofessional.com
PRINCIPAL DISPLAY PANEL 100 mL Bottle
NDC 0126-0070-61
Colgate®
PreviDent®
5000ppm
SENSITIVE
1.1% Sodium Fluoride
5% Potassium Nitrate
PRESCRIPTION STRENGTH
TOOTHPASTE FOR SENSITIVE TEETH
MILD MINT
3.4 FL OZ (100 mL)
Rx ONLY
P10000587
| PREVIDENT 5000 SENSITIVE sodium fluoride gel, dentifrice | ||||||||||||||||||||
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| Marketing Information | |||
| Marketing Category | Application Number or Monograph Citation | Marketing Start Date | Marketing End Date |
| Unapproved drug other | 07/06/2009 | ||
| Labeler - Colgate-Palmolive Company (055002195) |
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Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup
Pronunciation: SOO-doe-e-FED-rin/KLOR-fen-IR-a-meen/KLOE-fe-DYE-a-nol
Generic Name: Pseudoephedrine/Chlorpheniramine/Chlophedianol
Brand Name: DryMax AF
Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup is used for:
Relieving symptoms of sinus congestion, runny nose, sneezing, itchy nose or throat, itchy or watery eyes, and cough due to colds, hay fever, and other upper respiratory allergies. It may also be used for other conditions as determined by your doctor.
Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup is a decongestant, antihistamine, and cough suppressant combination. The decongestant works by constricting blood vessels and reducing swelling in the nasal passages. The antihistamine works by blocking the action of histamine, which helps reduce symptoms such as watery eyes and sneezing. The cough suppressant works in the brain to help decrease the cough reflex to reduce a dry cough.
Do NOT use Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup if:
- you are allergic to any ingredient in Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup
- you have severe or uncontrolled high blood pressure, severe heart blood vessel disease, rapid heartbeat, or severe heart problems
- you are unable to urinate or are having an asthma attack
- you are taking droxidopa or sodium oxybate (GHB), or you have taken furazolidone or a monoamine oxidase inhibitor (MAOI) (eg, phenelzine) within the last 14 days
Contact your doctor or health care provider right away if any of these apply to you.
Before using Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup:
Some medical conditions may interact with Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:
- if you are pregnant, planning to become pregnant, or are breast-feeding
- if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement
- if you have allergies to medicines, foods, or other substances
- if you have a history of adrenal gland problems (eg, adrenal gland tumor), heart problems (eg, fast, slow, or irregular heartbeat; heart disease), high or low blood pressure, low blood volume, diabetes, blood vessel problems, stroke, glaucoma or increased pressure in the eye, seizures, mental or mood problems (eg, depression), thyroid problems, or trouble sleeping
- if you have a history of asthma, chronic obstructive pulmonary disease (COPD), or other lung or breathing problems (eg, chronic bronchitis, emphysema, sleep apnea); chronic cough; or if your cough occurs with large amounts of mucus
- if you have a history of stomach or bowel ulcers; a blockage of your stomach, bladder, or bowels ; an enlarged prostate or other prostate problems; kidney problems; or trouble urinating
- if you take medicine for high blood pressure or depression
Some MEDICINES MAY INTERACT with Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup. Tell your health care provider if you are taking any other medicines, especially any of the following:
- Digoxin or droxidopa because the risk of irregular heartbeat or heart attack may be increased
- Beta-blockers (eg, propranolol), furazolidone, linezolid, MAOIs (eg, phenelzine), selective serotonin reuptake inhibitors (SSRIs) (eg, citalopram, fluoxetine), sodium oxybate (GHB), or urinary alkalinizers (eg, sodium bicarbonate) because they may increase the risk of Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup's side effects
- Bromocriptine or hydantoins (eg, phenytoin) because the risk of their side effects may be increased by Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup
- Guanadrel, guanethidine, mecamylamine, methyldopa, or reserpine because their effectiveness may be decreased by Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup
This may not be a complete list of all interactions that may occur. Ask your health care provider if Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.
How to use Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup:
Use Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup as directed by your doctor. Check the label on the medicine for exact dosing instructions.
- Take Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup by mouth with or without food. If stomach upset occurs, take with food to reduce stomach irritation.
- Use a measuring device marked for medicine dosing. Ask your pharmacist for help if you are unsure of how to measure your dose.
- Take Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup with a full glass of water (8 oz/240 mL).
- If you miss a dose of Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup and you are taking it regularly, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once.
Ask your health care provider any questions you may have about how to use Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup.
Important safety information:
- Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup may cause drowsiness, dizziness, or blurred vision. These effects may be worse if you take it with alcohol or certain medicines. Use Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup with caution. Do not drive or perform other possibly unsafe tasks until you know how you react to it.
- Do not drink alcohol while you are using Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup.
- Check with your doctor before you use medicines that may cause drowsiness (eg, sleep aids, muscle relaxers) while you are using Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup; it may add to their effects. Ask your pharmacist if you have questions about which medicines may cause drowsiness.
- Do not take diet or appetite control medicines while you take Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup without checking with your doctor.
- Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup has a decongestant, antihistamine, and cough suppressant in it. Before you start any new medicine, check the label to see if it has a decongestant, antihistamine, or cough suppressant in it too. If it does or if you are not sure, check with your doctor or pharmacist.
- Do not use Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup for a cough with a lot of mucus. Do not use it for a long-term cough (eg, caused by asthma, emphysema, smoking). However, you may use it for these conditions if your doctor tells you to.
- Do NOT take more than the recommended dose or use for longer than recommended without checking with your doctor.
- If new symptoms occur, or if cough or nasal congestion persists for more than 1 week, goes away and returns, or occurs along with a fever, rash, or persistent headache, check with your doctor. A persistent cough may be a sign of a serious condition.
- Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup may cause you to become sunburned more easily. Avoid the sun, sunlamps, or tanning booths until you know how you react to Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup. Use a sunscreen or wear protective clothing if you must be outside for more than a short time.
- Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup may interfere with skin allergy tests. If you are scheduled for a skin test, talk to your doctor. You may need to stop taking Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup for a few days before the tests.
- Tell your doctor or dentist that you take Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup before you receive any medical or dental care, emergency care, or surgery.
- Use Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup with caution in the ELDERLY; they may be more sensitive to its effects, especially confusion, drowsiness, dizziness, dry mouth, nervousness, sleeplessness, and trouble urinating.
- Caution is advised when using Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup in CHILDREN; they may be more sensitive to its effects, especially excitability.
- Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup should not be used in CHILDREN younger than 6 years old without first checking with the child's doctor; safety and effectiveness in these children have not been confirmed.
- PREGNANCY and BREAST-FEEDING: If you become pregnant, contact your doctor. You will need to discuss the benefits and risks of using Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup while you are pregnant. Some ingredients of Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup are found in breast milk. Do not breast-feed while taking Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup.
Possible side effects of Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup:
All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome:
Anxiety; constipation; diarrhea; dizziness; drowsiness; dry mouth, nose, or throat; excitability; headache; increased sweating; loss of appetite; nausea; trouble sleeping; upset stomach; vomiting; weakness.
Seek medical attention right away if any of these SEVERE side effects occur:
Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); difficulty urinating or inability to urinate; fast or irregular heartbeat; fever, chills, or persistent sore throat; flushing or redness of the face; hallucinations; loss of coordination; mental or mood changes (eg depression, nervousness); numbness or tingling; seizures; severe dryness of mouth, nose, or throat; severe or persistent dizziness, drowsiness, light-headedness, or headache; severe or persistent trouble sleeping; shortness of breath; tremor; unusual bruising or bleeding; unusual tiredness or weakness; vision problems (eg, double vision, severe or persistent blurred vision).
This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. To report side effects to the appropriate agency, please read the Guide to Reporting Problems to FDA.
If OVERDOSE is suspected:
Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center, or emergency room immediately. Symptoms may include blurred vision; confusion; flushing; hallucinations; mental or mood changes; muscle spasms; seizures; severe dizziness, light-headedness, or headache; severe drowsiness; trouble breathing; unusual eye movements; unusually fast, slow, or irregular heartbeat; vomiting.
Proper storage of Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup:
Store Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup at room temperature, between 59 and 86 degrees F (15 and 30 degrees C). Store away from heat, moisture, and light. Do not store in the bathroom. Keep Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup out of the reach of children and away from pets.
General information:
- If you have any questions about Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup, please talk with your doctor, pharmacist, or other health care provider.
- Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup is to be used only by the patient for whom it is prescribed. Do not share it with other people.
- If your symptoms do not improve or if they become worse, check with your doctor.
- Check with your pharmacist about how to dispose of unused medicine.
This information is a summary only. It does not contain all information about Pseudoephedrine/Chlorpheniramine/Chlophedianol Syrup. If you have questions about the medicine you are taking or would like more information, check with your doctor, pharmacist, or other health care provider.
Issue Date: February 1, 2012
Database Edition 12.1.1.002
Copyright © 2012 Wolters Kluwer Health, Inc.
Famotidina
Famotidina may be available in the countries listed below.
Ingredient matches for Famotidina
Famotidine
Famotidina (DCIT) is known as Famotidine in the US.
International Drug Name Search
Glossary
| DCIT | Denominazione Comune Italiana |
Click for further information on drug naming conventions and International Nonproprietary Names.
Tuesday, 27 September 2016
progestin contraceptives Oral, Parenteral
Commonly used brand name(s)
In the U.S.
- Aygestin
- Camila
- Errin
- Jolivette
- Next Choice
- Nora-BE
- Nor-QD
- Ortho Micronor
- Ovrette
- Plan B
- Plan B One-Step
- Provera
Available Dosage Forms:
- Tablet
Uses For progestin contraceptives
Progestins are hormones.
The low-dose progestins for contraception are used to prevent pregnancy. Other names for progestin-only oral contraceptives are minipills and progestin-only pills (POPs). Progestins can prevent fertilization by preventing a woman's egg from fully developing.
Also, progestins cause changes at the opening of the uterus, such as thickening of the cervical mucus. This makes it hard for the partner's sperm to reach the egg. The fertilization of the woman's egg with her partner's sperm is less likely to occur while she is taking, receiving, or using a progestin, but it can occur. Even so, the progestins make it harder for the fertilized egg to become attached to the walls of the uterus, making it difficult to become pregnant.
No contraceptive method is 100 percent effective. Studies show that fewer than 1 of each 100 women become pregnant during the first year of use after correctly receiving the injection on time. Fewer than 10 of each 100 women who take progestins correctly by mouth for contraception become pregnant during the first year of use. Methods that do not work as well include condoms, diaphragms, or spermicides. Discuss with your doctor what your options are for birth control.
Progestin contraceptives are available only with your doctor's prescription.
Importance of Diet
Make certain your doctor knows if you are on any special diet, such as a low-sodium or low-sugar diet.
Before Using progestin contraceptives
Allergies
Tell your doctor if you have ever had any unusual or allergic reaction to medicines in this group or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.
Pediatric
Progestins have been used by teenagers and have not been shown to cause different side effects or problems than they do in adults. You must take progestin-only oral contraceptives every day in order for them to work. Progestins do not protect against sexually transmitted diseases, a risk factor for teenagers. It is not known if Depo-Provera Contraceptive Injection causes problems with bone development and growth in teenagers and young women. It is important that your doctor check you regularly for growth problems, especially if you have been using progestin contraceptives for 2 years or longer.
Geriatric
progestin contraceptives has been tested and has not been shown to cause different side effects or problems in older people than it does in younger adults.
Pregnancy
Use of progestin-only contraceptives during pregnancy is not recommended. Doctors should be told if pregnancy is suspected. When accidently used during pregnancy, progestins used for contraception have not caused problems.
Breast Feeding
Although progestins pass into the breast milk, the low doses of progestins used for contraception have not been shown to cause problems in nursing babies. Progestins used for contraception are recommended for nursing mothers when contraception is desired.
Interactions with Medicines
Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking any of these medicines, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.
Using medicines in this class with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.
- Isotretinoin
- Theophylline
- Tizanidine
- Tranexamic Acid
Interactions with Food/Tobacco/Alcohol
Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.
Other Medical Problems
The presence of other medical problems may affect the use of medicines in this class. Make sure you tell your doctor if you have any other medical problems, especially:
- Asthma or
- Epilepsy, or history of or
- Heart or circulation problems or
- Kidney disease, severe or
- Migraine headaches—May cause fluid buildup and make these conditions worse.
- Bleeding problems, undiagnosed, such as blood in the urine or changes in vaginal bleeding—May make diagnosis of these problems more difficult.
- Breast disease (e.g., breast lumps or cysts), history of—May make this condition worse in certain types of diseases that do not react to progestins in a positive way.
- Central nervous system (CNS) disorders (e.g., depression), or history of or
- High blood cholesterol or
- Osteoporosis (brittle bones), or a family history of—May cause these conditions to occur or make these conditions worse.
- Diabetes mellitus—May cause a mild increase in blood sugar and a need to monitor blood sugar more often.
- Liver disease—The effects of some progestins may be increased. May make this condition worse.
Proper Use of progestin contraceptives
To make the use of a progestin as safe and reliable as possible, you should understand how and when to take it and what effects may be expected. Progestins for contraception usually come with patient directions. Read them carefully before taking or using progestin contraceptives.
Progestins do not protect a woman from sexually transmitted diseases (STDs), including human immunodeficiency virus (HIV), or acquired immunodeficiency syndrome (AIDS). The use of latex (rubber) condoms or abstinence is recommended for protection from these diseases.
Take progestin contraceptives only as directed by your doctor. Do not take more of it and do not take it for a longer time than your doctor ordered. To do so may increase the chance of side effects. Try to take the medicine at the same time each day to reduce the possibility of side effects and to allow it to work better.
When using levonorgestrel tablet dosage form for emergency contraception:
- The tablets may be taken at any time during the menstrual cycle.
When using medroxyprogesterone injection dosage form for contraception:
- Your injection is given by a health care professional every 3 months.
- To stop using medroxyprogesterone injection for contraception, simply do not have another injection.
- Full protection from pregnancy begins immediately if you receive the first injection within the first 5 days of your menstrual period or within 5 days after delivering a baby if you will not be breast-feeding. If you are going to breast-feed, you may have to wait for 6 weeks from your delivery date before receiving your first injection. If you follow this schedule, you do not need to use another form of birth control. Protection from that one injection ends at 3 months. You will need another injection every 3 months to have full protection from becoming pregnant. However, if the injection is given later than 5 days from the first day of your last menstrual period, you will need to use another method of birth control as directed by your doctor.
When using an oral progestin dosage form:
- Take a tablet every 24 hours each day of the year. Taking the medicine at the same time each day helps to reduce the possibility of side effects and makes it work as expected. Taking your tablet 3 hours late is the same as missing a dose and can cause the medicine to not work properly.
- Keep the tablets in the container in which you received them to help you to keep track of your dosage schedule.
- When switching from estrogen and progestin oral contraceptives, you should take the first dose of the progestin-only contraceptive the next day after the last active pill of the estrogen and progestin oral contraceptive has been taken. This means you will not take the last 7 days (placebo or nonactive pills) of a 28-day cycle of the estrogen and progestin oral contraceptive pack. You will begin a new pack of progestin-only birth control pills on the 22nd day.
- Also, when switching, full protection from pregnancy begins after 48 hours if the first dose of the progestin-only contraceptive is taken on the first day of the menstrual period. If the birth control is begun on other days, full protection may begin 3 weeks after you begin taking the medicine for the first time. You should use a second method of birth control for at least the first 3 weeks to ensure full protection. You are not fully protected if you miss pills. The chances of your getting pregnant are greater with each pill that is missed.
Follow your doctor's orders to schedule the proper time to receive an injection of progestins for contraception.
Dosing
The dose medicines in this class will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of these medicines. If your dose is different, do not change it unless your doctor tells you to do so.
The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.
- For levonorgestrel
- For oral dosage form (tablets):
- For emergency contraception for preventing pregnancy:
- Adults and teenagers—The first dose of 0.75 milligram should be taken as soon as possible within 72 hours of intercourse. The second dose must be taken 12 hours later.
- For emergency contraception for preventing pregnancy:
- For medroxyprogesterone
- For muscular injection dosage form
- For preventing pregnancy:
- Adults and teenagers—150 milligrams injected into a muscle in the upper arm or in the buttocks every three months (13 weeks).
- For preventing pregnancy:
- For subcutaneous injection dosage form
- For preventing pregnancy:
- Adults and teenagers—104 milligrams injected under the skin of the anterior thigh or abdomen every three months (12 to 14 weeks).
- For preventing pregnancy:
- For norethindrone
- For oral dosage form (tablets):
- For preventing pregnancy:
- Adults and teenagers—0.35 milligrams every 24 hours, beginning on the first day of your menstrual cycle whether menstrual bleeding begins or not. The first day of your menstrual cycle can be figured out by counting 28 days from the first day of your last menstrual cycle.
- For preventing pregnancy:
- For norgestrel
- For oral dosage form (tablets):
- For preventing pregnancy:
- Adults and teenagers—75 micrograms every 24 hours, beginning on the first day of your menstrual cycle whether menstrual bleeding occurs or not. The first day of your menstrual cycle can be figured out by counting 28 days from the first day of your last menstrual cycle.
- For preventing pregnancy:
Missed Dose
Call your doctor or pharmacist for instructions.
For oral dosage form (tablets):
- When you miss 1 day's dose of oral tablets or are 3 hours or more late in taking your dose, many doctors recommend that you take the missed dose immediately, continue your normal schedule, and use another method of contraception for 2 days. This is different from what is done after a person misses a dose of birth control tablets that contain more than one hormone.
For injection dosage form:
- If you miss having your next injection and it has been longer than 13 weeks since your last injection, your doctor may want you to stop receiving the medicine. Use another method of birth control until your period begins or until your doctor determines that you are not pregnant.
- If your doctor has other directions, follow that advice. Any time you miss a menstrual period within 45 days after a missed or delayed dose you will need to be tested for a possible pregnancy.
Storage
Keep out of the reach of children.
Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.
Do not keep outdated medicine or medicine no longer needed.
Precautions While Using progestin contraceptives
It is very important that your doctor check your progress at regular visits. This will allow your dosage to be adjusted to your changing needs, and will allow any unwanted effects to be detected. These visits are usually every 12 months when you are taking progestins by mouth for birth control.
- If you are receiving the medroxyprogesterone injection for contraception, a physical exam is needed only every 12 months, but you need an injection every 3 months. Your doctor will also want to check you for any bone development or growth problems, especially if you are a teenager or young adult.
Progestins may cause dizziness in some people. Make sure you know how you react to progestin contraceptives before you drive, use machines, or do anything else that could be dangerous if you are not alert.
It is possible that certain doses of progestins may cause a temporary thinning of the bones by changing your hormone balance. It is important that your doctor know if you have an increased risk of osteoporosis. Some things that can increase your risk for osteoporosis include cigarette smoking, abusing alcohol, taking or drinking large amounts of caffeine, and having a family history of osteoporosis or easily broken bones. Some medicines, such as steroids (cortisone-like medicines) or anticonvulsants (seizure medicines), can also cause thinning of the bones. It is especially important that you tell your doctor about any of these risk factors if you are taking Depo-Provera® Contraceptive Injection or Depo-SubQ Provera® 104. These contraceptives may cause a loss of bone mineral density. Your doctor may replace these contraceptives with a different one.
Vaginal bleeding of various amounts may occur between your regular menstrual periods during the first 3 months of use. This is not unusual and does not mean you should stop the medicine. This is sometimes called spotting when the bleeding is slight, or breakthrough bleeding when it is heavier. If this occurs, continue on your regular dosing schedule. Check with your doctor:
- If vaginal bleeding continues for an unusually long time.
- If your menstrual period has not started within 45 days of your last period.
Missed menstrual periods may occur. If you suspect a pregnancy, you should call your doctor immediately.
If you are scheduled for any laboratory tests, tell your doctor that you are taking a progestin. Progestins can change certain test results.
The following medicines might reduce the effectiveness of progestins for contraception:
- Aminoglutethimide (e.g., Cytadren®)
- Carbamazepine (e.g., Tegretol®)
- Phenobarbital
- Phenytoin (e.g., Dilantin®)
- Rifabutin (e.g., Mycobutin®)
- Rifampin (e.g., Rifadin®)
Sometimes your doctor may use these medicines with progestins for contraception, but the doctor will give you special directions to follow to make sure your progestin is working properly. In order to prevent pregnancy, use a second method of birth control together with the progestin when you also use a medicine that could reduce the effectiveness of the progestin. If you are using medroxyprogesterone injection for contraception, continue using a back-up method of birth control until you have your next injection, even if the medicine that affects contraceptives is discontinued. If you are using the oral tablets, continue using a back-up method of birth control for a full cycle (or 4 weeks), even if the medicine that affects contraceptives is discontinued.
If you vomit your oral progestin-only contraceptive for any reason within a few hours after taking it, do not take another dose. Return to your regular dosing schedule and use an additional back-up method of birth control for 48 hours.
If you are receiving levonorgestrel tablets for emergency contraception and vomiting occurs within 1 hour after taking either dose of the medicine, contact your physician to discuss whether the dose should be repeated.
progestin contraceptives Side Effects
Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.
Check with your doctor as soon as possible if any of the following side effects occur:
More common
- Changes in uterine bleeding (increased amounts of menstrual bleeding occurring at regular monthly periods
- heavier uterine bleeding between regular monthly periods
- lighter uterine bleeding between menstrual periods
- or stopping of menstrual periods
- Mental depression
- skin rash
- unexpected or increased flow of breast milk
- Cough
- decrease in height
- difficulty swallowing
- fast heartbeat
- hives, itching, puffiness, or swelling of the eyelids or around the eyes, face, lips or tongue
- pain in back, ribs, arms, or legs
- pain or swelling in arms or legs without any injury
- shortness of breath
- skin rash
- tightness in chest
- wheezing
Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:
More common
- Abdominal pain or cramping
- diarrhea
- dizziness
- fatigue
- mild headache
- mood changes
- nausea
- nervousness
- pain or irritation at the injection site
- swelling of face, ankles, or feet
- unusual tiredness or weakness
- vomiting
- weight gain
- Acne
- breast pain or tenderness
- brown spots on exposed skin, possibly long-lasting
- hot flashes
- loss or gain of body, facial, or scalp hair
- loss of sexual desire
- trouble in sleeping
Not all of the side effects listed above have been reported for each of these medicines, but they have been reported for at least one of them. All of the progestins are similar, so any of the above side effects may occur with any of these medicines.
After you stop using progestin contraceptives, your body may need time to adjust. The length of time this takes depends on the amount of medicine you were using and how long you used it. During this period of time, check with your doctor if you notice any of the following side effects:
- Delayed return to fertility
- stopping of menstrual periods
- unusual menstrual bleeding (continuing)
Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.
Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.
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Serentil
mesoridazine besylate
Dosage Form: Tablets USP, Injection, USP and Oral Solution, USP
T2001-24
89011602
4085-42
Serentil®
(mesoridazine besylate) Tablets, USP
(mesoridazine besylate) Injection, USP
(mesoridazine besylate) Oral Solution, USP
Rx only
Prescribing Information
WARNING
SERENTIL® (MESORIDAZINE BESYLATE) HAS BEEN SHOWN TO PROLONG THE QTc INTERVAL IN A DOSE RELATED MANNER, AND DRUGS WITH THIS POTENTIAL, INCLUDING SERENTIL, HAVE BEEN ASSOCIATED WITH TORSADE DE POINTES-TYPE ARRHYTHMIAS AND SUDDEN DEATH. DUE TO ITS POTENTIAL FOR SIGNIFICANT, POSSIBLY LIFE-THREATENING, PROARRHYTHMIC EFFECTS, Serentil SHOULD BE RESERVED FOR USE IN THE TREATMENT OF SCHIZOPHRENIC PATIENTS WHO FAIL TO SHOW AN ACCEPTABLE RESPONSE TO ADEQUATE COURSES OF TREATMENT WITH OTHER ANTIPSYCHOTIC DRUGS, EITHER BECAUSE OF INSUFFICIENT EFFECTIVENESS OR THE INABILITY TO ACHIEVE AN EFFECTIVE DOSE DUE TO INTOLERABLE ADVERSE EFFECTS FROM THOSE DRUGS. (SEE WARNINGS, CONTRAINDICATIONS, AND INDICATIONS.)
DESCRIPTION
SERENTIL® (mesoridazine besylate), the besylate salt of a metabolite of thioridazine, is a phenothiazine antipsychotic. Serentil is 10-[2(1-methyl-2-piperidyl)ethyl]-2-(methyl-sulfinyl)-phenothiazine [as the besylate].
Tablet, 10 mg, for oral administration
ACTIVE INGREDIENT: mesoridazine (as the besylate), 10 mg.
INACTIVE INGREDIENTS: acacia, carnauba wax, colloidal silicon oxide, FD&C Red No. 40 aluminum lake, lactose, microcrystalline cellulose, povidone, sodium benzoate, starch, stearic acid, sucrose, synthetic black iron oxide, talc, titanium dioxide and other ingredients.
Tablet, 25 mg, for oral administration
ACTIVE INGREDIENT: mesoridazine (as the besylate), 25 mg.
INACTIVE INGREDIENTS: acacia, carnauba wax, colloidal silicon oxide, FD&C Red No. 40 aluminum lake, lactose, microcrystalline cellulose, povidone, sodium benzoate, starch, stearic acid, sucrose, synthetic black iron oxide, talc, titanium dioxide and other ingredients.
Tablet, 50 mg, for oral administration
ACTIVE INGREDIENT: mesoridazine (as the besylate), 50 mg.
INACTIVE INGREDIENTS: acacia, carnauba wax, colloidal silicon oxide, FD&C Red No. 40 aluminum lake, gelatin, lactose, microcrystalline cellulose, povidone, sodium benzoate, starch, stearic acid, sucrose, synthetic black iron oxide, talc, titanium dioxide and other ingredients.
Tablet, 100 mg, for oral administration
ACTIVE INGREDIENT: mesoridazine (as the besylate), 100 mg.
INACTIVE INGREDIENTS: acacia, carnauba wax, colloidal silicon oxide, FD&C Red No. 40 aluminum lake, gelatin, lactose, microcrystalline cellulose, povidone, sodium benzoate, starch, stearic acid, sucrose, synthetic black iron oxide, talc, titanium dioxide and other ingredients.
Ampuls, 1 mL, for Intramuscular administration
ACTIVE INGREDIENT: mesoridazine (as the besylate), 25 mg.
INACTIVE INGREDIENTS: edetate disodium USP, 0.5 mg; sodium chloride USP, 7.2 mg; carbon dioxide gas (bone dry) q.s.; water for injection USP, q.s. to 1 mL.
Concentrate, for oral administration
ACTIVE INGREDIENT: mesoridazine (as the besylate), 25 mg per mL.
INACTIVE INGREDIENTS: alcohol, 0.61% by volume; citric acid; FD&C Red No. 40; flavors; methylparaben; propylparaben; purified water; sodium citrate; sorbitol.
CLINICAL PHARMACOLOGY
The basic pharmacological activity of Serentil® (mesoridazine besylate) is similar to that of other phenothiazines.
However, mesoridazine has been shown to prolong the QTc interval in a dose-dependent fashion. This effect may increase the risk of serious, potentially fatal, ventricular arrhythmias, such as torsade de pointes-type arrhythmias. Due to this risk, Serentil is indicated only for schizophrenic patients who have not been responsive to or cannot tolerate other antipsychotic agents (see WARNINGS and CONTRAINDICATIONS).
However, the prescriber should be aware that Serentil has not been systematically evaluated in controlled trials in treatment of refractory schizophrenic patients and its efficacy in such patients is unknown.
INDICATIONS
Serentil® (mesoridazine besylate) is indicated for the management of schizophrenic patients who fail to respond adequately to treatment with other antipsychotic drugs. Due to the risk of significant, potentially life-threatening, proarrhythmic effects with Serentil treatment, Serentil should be used only in patients who have failed to respond adequately to treatment with appropriate courses of other antipsychotic drugs, either because of insufficient effectiveness or the inability to achieve an effective dose due to intolerable adverse effects from those drugs. Consequently, before initiating treatment with Serentil, it is strongly recommended that a patient be given at least two trials, each with a different antipsychotic drug product at an adequate dose, and for an adequate duration (see WARNINGS and CONTRAINDICATIONS).
However, the prescriber should be aware that Serentil has not been systematically evaluated in controlled trials in treatment of refractory schizophrenic patients and its efficacy in such patients is unknown.
CONTRAINDICATIONS
Serentil® (mesoridazine besylate) use should be avoided in combination with other drugs that are known to prolong the QTc interval and in patients with congenital long QT syndrome or a history of cardiac arrhythmias (see WARNINGS and PRECAUTIONS).
As with other phenothiazines, Serentil is contraindicated in severe central nervous system depression or comatose states from any cause including drug induced central nervous system depression (see WARNINGS).
Serentil is contraindicated in individuals who have previously shown hypersensitivity to the drug.
WARNINGS
Potential for Proarrhythmic Effects
DUE TO THE POTENTIAL FOR SIGNIFICANT, POSSIBLY LIFE-THREATENING, PROARRHYTHMIC EFFECTS WITH SERENTIL® (MESORIDAZINE BESYLATE) TREATMENT, Serentil SHOULD BE RESERVED FOR USE IN THE TREATMENT OF SCHIZOPHRENIC PATIENTS WHO FAIL TO SHOW AN ACCEPTABLE RESPONSE TO ADEQUATE COURSES OF TREATMENT WITH OTHER ANTIPSYCHOTIC DRUGS, EITHER BECAUSE OF INSUFFICIENT EFFECTIVENESS OR THE INABILITY TO ACHIEVE AN EFFECTIVE DOSE DUE TO INTOLERABLE ADVERSE EFFECTS FROM THOSE DRUGS. CONSEQUENTLY, BEFORE INITIATING TREATMENT WITH SERENTIL, IT IS STRONGLY RECOMMENDED THAT A PATIENT BE GIVEN AT LEAST TWO TRIALS, EACH WITH A DIFFERENT ANTIPSYCHOTIC DRUG PRODUCT, AT AN ADEQUATE DOSE, AND FOR AN ADEQUATE DURATION. Serentil HAS NOT BEEN SYSTEMATICALLY EVALUATED IN CONTROLLED TRIALS IN THE TREATMENT OF REFRACTORY SCHIZOPHRENIC PATIENTS AND ITS EFFICACY IN SUCH PATIENTS IS UNKNOWN.
A study in nine chronic schizophrenic patients who were treated with mesoridazine 75 mg/day for the first week, 200 mg/day during week 2, and 300 mg/day during weeks 3 and 4, revealed evidence of a dose-related prolongation of the QT interval. All patients had a normal ECG at baseline and eight of the nine had normal ECG’s two weeks after drug discontinuation.
Prolongation of the QTc interval has been associated with the ability to cause torsade de pointes-type arrhythmias, a potentially fatal polymorphic ventricular tachycardia, and sudden death. There are published case reports of ventricular tachycardia, in one case with a fatal outcome, in association with mesoridazine overdosage. A causal relationship between these events and Serentil therapy has not been established but, given the ability of Serentil to prolong the QTc interval, such a relationship is possible.
Certain circumstances may increase the risk of torsade de pointes and/or sudden death in association with the use of drugs that prolong the QTc interval, including 1) bradycardia, 2) hypokalemia, 3) concomitant use of other drugs that prolong the QTc interval, and 4) presence of congenital prolongation of the QT interval (see CONTRAINDICATIONS and PRECAUTIONS).
It is recommended that patients being considered for Serentil treatment have a baseline ECG performed and serum potassium levels measured. Serum potassium should be normalized before initiating treatment and patients with a QTc interval greater than 450 msec should not receive Serentil treatment. It may also be useful to periodically monitor ECG’s and serum potassium during Serentil treatment especially during a period of dose adjustment. Serentil should be discontinued in patients who are found to have a QTc interval over 500 msec.
Patients taking Serentil who experience symptoms that may be associated with the occurrence of torsade de pointes (e.g., dizziness, palpitations, or syncope) may warrant further cardiac evaluation; in particular, Holter monitoring should be considered.
Tardive Dyskinesia
Tardive dyskinesia, a syndrome consisting of potentially irreversible, involuntary, dyskinetic movements, may develop in patients treated with antipsychotic drugs. Although the prevalence of the syndrome appears to be highest among the elderly, especially elderly women, it is impossible to rely upon prevalence estimates to predict, at the inception of antipsychotic treatment, which patients are likely to develop the syndrome. Whether antipsychotic drug products differ in their potential to cause tardive dyskinesia is unknown.
Both the risk of developing the syndrome and the likelihood that it will become irreversible are believed to increase as the duration of treatment and the total cumulative dose of antipsychotic drugs administered to the patient increase. However, the syndrome can develop, although much less commonly, after relatively brief treatment periods at low doses.
There is no known treatment for established cases of tardive dyskinesia, although the syndrome may remit, partially or completely, if antipsychotic treatment is withdrawn. Antipsychotic treatment, itself, however, may suppress (or partially suppress) the signs and symptoms of the syndrome and thereby may possibly mask the underlying disease process. The effect that symptomatic suppression has upon the long-term course of the syndrome is unknown.
Given these considerations, antipsychotics should be prescribed in a manner that is most likely to minimize the occurrence of tardive dyskinesia. Chronic antipsychotic treatment should generally be reserved for patients who suffer from a chronic illness 1) that is known to respond to antipsychotic drugs, and 2) for which alternative, equally effective but potentially less harmful treatments are not available or appropriate. In patients who do require chronic treatment, the smallest dose and the shortest duration of treatment producing a satisfactory clinical response should be sought. The need for continued treatment should be reassessed periodically.
If signs and symptoms of tardive dyskinesia appear in a patient on antipsychotics, drug discontinuation should be considered. However, some patients may require treatment despite the presence of the syndrome.
(For further information about the description of tardive dyskinesia and its clinical detection, please refer to the sections on Information for Patients and Adverse Reactions.)
Neuroleptic Malignant Syndrome (NMS)
A potentially fatal symptom complex sometimes referred to as Neuroleptic Malignant Syndrome (NMS) has been reported in association with antipsychotic drugs. Clinical manifestations of NMS are hyperpyrexia, muscle rigidity, altered mental status and evidence of autonomic instability (irregular pulse or blood pressure, tachycardia, diaphoresis, and cardiac dysrhythmias).
The diagnostic evaluation of patients with this syndrome is complicated. In arriving at a diagnosis, it is important to identify cases where the clinical presentation includes both serious medical illness (e.g., pneumonia, systemic infection, etc.) and untreated or inadequately treated extrapyramidal signs and symptoms (EPS). Other important considerations in the differential diagnosis include central anticholinergic toxicity, heat stroke, drug fever and primary central nervous system (CNS) pathology.
The management of NMS should include 1) immediate discontinuation of antipsychotic drugs and other drugs not essential to concurrent therapy, 2) intensive symptomatic treatment and medical monitoring, and 3) treatment of any concomitant serious medical problems for which specific treatments are available. There is no general agreement about specific pharmacological treatment regimens for uncomplicated NMS.
If a patient requires antipsychotic drug treatment after recovery from NMS, the potential reintroduction of drug therapy should be carefully considered. The patient should be carefully monitored, since recurrences of NMS have been reported.
Where patients are participating in activities requiring complete mental alertness, (e.g., driving) it is advisable to administer the phenothiazines cautiously and to increase the dosage gradually.
Central Nervous System Depressants
As in the case of other phenothiazines, Serentil is capable of potentiating central nervous system depressants (e.g., alcohol, anesthetics, barbiturates, narcotics, opiates, other psychoactive drugs, etc.) as well as atropine and phosphorus insecticides. Severe respiratory depression and respiratory arrest have been reported when a patient was given Serentil and a concomitant high dose of a barbiturate.
PRECAUTIONS
While ocular changes have not to date been related to Serentil® (mesoridazine besylate), one should be aware that such changes have been seen with other drugs of this class.
Because of possible hypotensive effects, reserve parenteral administration for bedfast patients or for acute ambulatory cases, and keep patient lying down for at least one-half hour after injection.
Leukopenia and/or agranulocytosis have been attributed to phenothiazine therapy. A single case of transient granulocytopenia has been associated with Serentil. Since convulsive seizures have been reported, patients receiving anticonvulsant medication should be maintained on that regimen while receiving Serentil.
Antipsychotic drugs elevate prolactin levels; the elevation persists during chronic administration. Tissue culture experiments indicate that approximately one-third of human breast cancers are prolactin dependent in vitro, a factor of potential importance if the prescription of these drugs is contemplated in a patient with a previously detected breast cancer. Although disturbances such as galactorrhea, amenorrhea, gynecomastia, and impotence have been reported, the clinical significance of elevated serum prolactin levels is unknown for most patients. An increase in mammary neoplasms has been found in rodents after chronic administration of antipsychotic drugs. Neither clinical studies nor epidemiologic studies conducted to date, however, have shown an association between chronic administration of these drugs and mammary tumorigenesis; the available evidence is considered too limited to be conclusive at this time.
Drug Interactions
There are no studies of the coadministration of mesoridazine and other drugs which prolong the QTc interval. However, it is expected that such coadministration would produce additive prolongation of the QTc interval and, thus, such use is contraindicated (see WARNINGS and CONTRAINDICATIONS).
Information for Patients
Patients should be informed that Serentil has been associated with potentially fatal heart rhythm disturbances. The risk of such events may be increased when certain drugs are given together with Serentil. Therefore, patients should inform the prescriber that they are receiving Serentil treatment before taking any new medication.
Given the likelihood that some patients exposed chronically to antipsychotics will develop tardive dyskinesia, it is advised that all patients in whom chronic use is contemplated be given, if possible, full information about this risk.
Usage In Pregnancy
The safety of this drug in pregnancy has not been established; hence, it should be given only when the anticipated benefits to be derived from treatment exceed the possible risks to mother and fetus.
Pediatric Use
Safety and effectiveness in pediatric patients have not been established.
ADVERSE REACTIONS
Drowsiness and hypotension were the most prevalent side effects encountered. Side effects tended to reach their maximum level of severity early with the exception of a few (rigidity and motoric effects) which occurred later in therapy.
With the exceptions of tremor and rigidity, adverse reactions were generally found among those patients who received relatively high doses early in treatment. Clinical data showed no tendency for the investigators to terminate treatment because of side effects.
Central Nervous System: Drowsiness, Parkinson’s syndrome, dizziness, weakness, tremor, restlessness, ataxia, dystonia, rigidity, slurring, akathisia, motoric reactions (opisthotonos) have been reported.
Autonomic Nervous System: Dry mouth, nausea and vomiting, fainting, stuffy nose, photophobia, constipation and blurred vision have occurred in some instances.
Genitourinary System: Inhibition of ejaculation, impotence, enuresis, incontinence, and priapism have been reported.
Skin: Itching, rash, hypertrophic papillae of the tongue and angioneurotic edema have been reported.
Cardiovascular System: Serentil® (mesoridazine besylate) produces a dose related prolongation of the QTc interval, which is associated with the ability to cause torsade de pointes-type arrhythmias, a potentially fatal polymorphic ventricular tachycardia, and sudden death (see WARNINGS). Ventricular arrhythmias and death have been reported in association with Serentil overdosage. A causal relationship between these events and Serentil therapy has not been established but, given the ability of Serentil to prolong the QTc interval, such a relationship is possible. Other ECG changes have been reported (see Phenothiazine Derivatives: Cardiovascular Effects).
Phenothiazine Derivatives
It should be noted that efficacy, indications and untoward effects have varied with the different phenothiazines. The physician should be aware that the following have occurred with one or more phenothiazines and should be considered whenever one of these drugs is used.
Autonomic Reactions: Miosis, obstipation, anorexia, paralytic ileus.
Cutaneous Reactions: Erythema, exfoliative dermatitis, contact dermatitis.
Blood Dyscrasias: Agranulocytosis, leukopenia, eosinophilia, thrombocytopenia, anemia, aplastic anemia, pancytopenia.
Allergic Reactions: Fever, laryngeal edema, angioneurotic edema, asthma.
Hepatotoxicity: Jaundice, biliary stasis.
Cardiovascular Effects: Changes in the terminal portion of the electrocardiogram, to include prolongation of the QT interval, depression and inversion of the T wave, and the appearance of a wave tentatively identified as a bifid T wave or a U wave have been observed in patients receiving phenothiazines, including Serentil. To date, these appear to be due to altered repolarization, not related to myocardial damage, and appear to be reversible. Nonetheless, significant prolongation of the QT interval has been associated with serious ventricular arrhythmias and sudden death (see WARNINGS). Hypotension, rarely resulting in cardiac arrest, has been reported.
Extrapyramidal Symptoms: Akathisia, agitation, motor restlessness, dystonic reactions, trismus, torticollis, opisthotonos, oculogyric crises, tremor, muscular rigidity, akinesia.
Tardive Dyskinesia: Chronic use of antipsychotics may be associated with the development of tardive dyskinesia. The salient features of this syndrome are described in the WARNINGS section and below.
The syndrome is characterized by involuntary choreoathetoid movements which variously involve the tongue, face, mouth, lips, or jaw (e.g., protrusion of the tongue, puffing of cheeks, puckering of the mouth, chewing movements), trunk and extremities. The severity of the syndrome and the degree of impairment produced vary widely.
The syndrome may become clinically recognizable either during treatment upon dosage reduction, or upon withdrawal of treatment. Movements may decrease in intensity and may disappear altogether if further treatment with antipsychotics is withheld. It is generally believed that reversibility is more likely after short rather than long-term antipsychotic exposure. Consequently, early detection of tardive dyskinesia is important. To increase the likelihood of detecting the syndrome at the earliest possible time, the dosage of antipsychotic drug should be reduced periodically (if clinically possible) and the patient observed for signs of the disorder. This maneuver is critical, for antipsychotic drugs may mask the signs of the syndrome.
Endocrine Disturbances: Menstrual irregularities, altered libido, gynecomastia, lactation, weight gain, edema. False positive pregnancy tests have been reported.
Urinary Disturbances: Retention, incontinence.
Others: Hyperpyrexia. Behavioral effects suggestive of a paradoxical reaction have been reported. These include excitement, bizarre dreams, aggravation of psychoses and toxic confusional states. More recently a peculiar skin-eye syndrome has been recognized as a side effect following long-term treatment with phenothiazines. This reaction is marked by progressive pigmentation of areas of the skin or conjunctiva and/or accompanied by discoloration of the exposed sclera and cornea. Opacities of the anterior lens and cornea described as irregular or stellate in shape have also been reported. Systemic lupus erythematosus-like syndrome.
OVERDOSAGE
Symptoms of Acute Overdosage
Drowsiness, confusion, disorientation, agitation, coma, death.
Dryness of mouth, edema of glottis, laryngeal spasms, nasal congestion, blurred vision, vomiting.
Hyperpyrexia, dilated pupils, muscle rigidity, hyperactive reflexes, areflexia.
Stupor, and CNS depression or stimulation with convulsions followed by respiratory depression.
Cardiac abnormalities, including QRS changes, tachycardia, hypotension, bilateral bundle branch block, ventricular fibrillation, shock, cardiac arrest and congestive heart failure.
Treatment of Acute Overdosage
An airway must be established and maintained. Adequate oxygenation and ventilation must be ensured.
Cardiovascular monitoring should commence immediately and should include continuous electrocardiographic monitoring to detect possible arrhythmias. Treatment may include one or more of the following therapeutic interventions: correction of electrolyte abnormalities and acid-base balance, lidocaine, phenytoin, isoproterenol, ventricular pacing, and defibrillation. Disopyramide, procainamide, and quinidine may produce additive QT-prolonging effects when administered to patients with acute overdosage of Serentil® (mesoridazine besylate) and should be avoided (see CONTRAINDICATIONS, WARNINGS, and PRECAUTIONS). Caution must be exercised when administering lidocaine, as it may increase the risk of developing seizures.
Treatment of hypotension may require intravenous fluids and vasopressors. Phenylephrine, levarterenol, or metaraminol are the appropriate pressor agents for use in the management of refractory hypotension. The potent α-adrenergic blocking properties of the phenothiazines makes the use of vasopressors with mixed α and β adrenergic agonist properties inappropriate, including epinephrine and dopamine. Paradoxical vasodilation may result. In addition, it is reasonable to expect that the α-adrenergic blocking properties of bretylium might be additive to those of Serentil, resulting in problematic hypotension.
In managing overdosage, the physician should always consider the possibility of multiple drug involvement. Gastric lavage and repeated doses of activated charcoal should be considered. Induction of emesis is less preferable to gastric lavage because of the risk of dystonia and the potential for aspiration of vomitus. Emesis should not be induced in patients expected to deteriorate rapidly or in those with impaired consciousness.
No specific antidote is known.
Acute extrapyramidal symptoms may be treated with diphenhydramine hydrochloride or benztropine mesylate.
Avoid the use of barbiturates when treating seizures, as they may potentiate phenothiazine-induced respiratory depression.
Forced diuresis, hemoperfusion, hemodialysis, and manipulation of urine pH are of unlikely benefit in the treatment of phenothiazine overdose due to their large volume of distribution and extensive plasma protein binding.
Up-to-date information about the treatment of overdose can often be obtained from a certified Regional Poison Control Center. Telephone numbers of certified Regional Poison Control Centers are listed in the Physicians’ Desk Reference®*.
DOSAGE AND ADMINISTRATION
Since Serentil® (mesoridazine besylate) is associated with a dose-related prolongation of the QTc interval, which is a potentially life-threatening event, its use should be reserved for schizophrenia patients who fail to respond adequately to treatment with other antipsychotic drugs (see INDICATIONS and WARNINGS).
The dosage of Serentil, as with most medications, should be adjusted to the needs of the individual. The lowest effective dosage should always be used. When maximum response is achieved, dosage may be reduced gradually to a maintenance dose.
Tablets and Oral Solution
For most patients, regardless of severity, a starting dose of 50 mg three times a day is recommended. The usual optimum total daily dose range is 100-400 mg per day.
Injectable Form
In those situations in which an intramuscular form of medication is indicated, Serentil injectable is available. For most patients, a starting dose of 25 mg is recommended. The dose may be repeated in 30 to 60 minutes, if necessary. The usual optimum total daily dose range is 25-200 mg per day.
HOW SUPPLIED
Tablets mesoridazine (as the besylate).
Bottles of 100.
10 mg………………………………………………………………NDC 0597-0020-01
25 mg………………………………………………………………NDC 0597-0021-01
50 mg………………………………………………………………NDC 0597-0022-01
100 mg……………………………………………………………..NDC 0597-0023-01
Ampuls 1 mL [25 mg mesoridazine (as the besylate)].
Boxes of 20………………………………………………………..NDC 0597-0027-02
Concentrate Contains 25 mg mesoridazine (as the besylate) per mL, alcohol, USP, 0.61% by volume. Immediate containers: Amber glass bottles of 4 fl oz (118 mL) packaged in cartons of 12 bottles, with an accompanying dropper graduated to deliver 10 mg, 25 mg, and 50 mg of mesoridazine (as the besylate)……………………………………………..NDC 0597-0025-04
STORAGE
Tablets: Store at 25ºC (77ºF); excursions permitted to 15ºC-30ºC (59ºF-86ºF).
[See USP Controlled Room Temperature]
Dispense in a tight container (USP).
Injection: Store at 25ºC (77ºF); excursions permitted to 15ºC-30ºC (59ºF-86ºF).
[See USP Controlled Room Temperature]
Dispense in a tight container (USP); protect from light.
Oral Solution: Store below 77ºF (25ºC); protect from light; dispense in amber glass bottles only.
The concentrate may be diluted with distilled water, orange juice or grape juice. Each dose should be diluted just prior to administration. Preparation and storage of bulk dilutions is not recommended.
Additional information available to physicians.
PHARMACOLOGY
Pharmacological studies in laboratory animals have established that Serentil® (mesoridazine besylate) has a spectrum of pharmacodynamic actions typical of an antipsychotic. In common with other antipsychotics it inhibits spontaneous motor activity in mice, prolongs thiopental and hexobarbital sleeping time in mice and produces spindles and block of arousal reaction in the EEG of rabbits. It is effective in blocking spinal reflexes in the cat and antagonizes d-amphetamine excitation and toxicity in grouped mice. It shows a moderate adrenergic blocking activity in vitro and in vivo and antagonizes 5-hydroxytryptamine in vivo. Intravenously administered, it lowers the blood pressure of anesthetized dogs. It has a weak antiacetylcholine effect in vitro.
The most outstanding activity of Serentil is seen in tests developed to investigate antiemotive activity of drugs. Such tests are those in which the rat reacts to acute or chronic stress by increased defecation (emetogenic defecation) or tests in which “emotional mydriasis” is elicited in the mouse by an electric shock. In both of these tests Serentil is effective in reducing emotive reactions. Its ED50 in inhibiting emetogenic defecation in the rat is 0.053 mg/kg (subcutaneous administration). Serentil has a potent antiemetic action. The intravenous ED50 against apomorphine-induced emesis in the dog is 0.64 mg/kg. Serentil, in common with other phenothiazines, demonstrates antiarrhythmic activity in anesthetized dogs.
Metabolic studies in the dog and rabbit with tritium labeled mesoridazine demonstrate that the compound is well absorbed from the gastrointestinal tract. The biological half life of Serentil in these studies appears to be somewhere between 24 to 48 hours. Although significant urinary excretion was observed following the administration of Serentil, these studies also suggest that biliary excretion is an important excretion route for mesoridazine and/or its metabolites.
Toxicity Studies
Acute LD50 (mg/kg):
| Route | Mouse | Rat | Rabbit | Dog |
| Oral | 560±62.5 | 644±48 | MLD=800 | MLD=800 |
| I.M. | - | 509M | 405 | - |
| 584F | ||||
| I.V. | 26±0.08 | - | - | - |
Chronic toxicity studies were conducted in rats and dogs. Rats were administered Serentil orally seven days per week for a period of seventeen months in doses up to 160 mg/kg per day. Dogs were administered Serentil orally seven days per week for a period of thirteen months. The daily dosage of the drug was increased during the period of this test such that the “top-dose” group received a daily dose of 120 mg/kg of mesoridazine for the last month of the study.
Untoward effects which occurred upon chronic administration of high dose-levels included:
Rats
Reduction of food intake, slowed weight gain, morphological changes in pituitary supported endocrine organs, and melanin-like pigment deposition in renal tissues.
Dogs
Emesis, muscle tremors, decreased food intake and death associated with aspiration of oral-gastric contents into the respiratory system.
Increased intrauterine resorptions were seen with Serentil in rats at 70 mg/kg and in rabbits at 125 mg/kg but not at 60 and 100 mg/kg, respectively. No drug related teratology was suggested by these reproductive studies.
Local irritation from the intramuscular injection of Serentil was of the same order of magnitude as with other phenothiazines.
* Trademark of Medical Economics Company, Inc.
T2001-24
REV: MARCH 2001 89011602
4085-42
Tablets Manufactured by:
Novartis Pharmaceuticals Canada, Inc.
Dorval (Québec), Canada H9S 1A9
Ampuls Manufactured by:
Novartis Pharmaceuticals Corporation
East Hanover, NJ 07936
Concentrate Manufactured for:
Novartis Pharmaceuticals Corporation
East Hanover, NJ 07936
by Novartis Consumer Health, Inc.
Lincoln, NB 68517
Distributed by:
Boehringer Ingelheim Pharmaceuticals, Inc.
Ridgefield, CT 06877
© 2001 Novartis
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