Ketorolac Hexpharm may be available in the countries listed below.
Ketorolac tromethamine (a derivative of Ketorolac) is reported as an ingredient of Ketorolac Hexpharm in the following countries:
International Drug Name Search
Sertralina Ranbaxygen may be available in the countries listed below.
Sertraline hydrochloride (a derivative of Sertraline) is reported as an ingredient of Sertralina Ranbaxygen in the following countries:
International Drug Name Search
Generic Name: hydromorphone (Oral route)
hye-droe-MOR-fone
Hydromorphone is a potent Schedule II opioid agonist, which has the highest potential for abuse and risk of producing respiratory depression. Alcohol, other opioids and central nervous system depressants (sedative-hypnotics) potentiate the respiratory depressant effects of hydromorphone, increasing the risk of respiratory depression that might result in death .
Exalgo(R) is a potent Schedule II opioid agonist, which has the highest potential for abuse and risk of respiratory depression. Hydromorphone extended-release tablets (Exalgo(R)) are for use in opioid-tolerant patients only with moderate to severe chronic pain. Use in non-opioid-tolerant patients may lead to fatal respiratory depression. Exalgo(R) is for continuous analgesia only and is not intended for use on an as needed basis (ie, PRN). Exalgo(R) should be swallowed whole; not broken, chewed, opened, dissolved, or crushed .
In the U.S.
Available Dosage Forms:
Therapeutic Class: Analgesic
Chemical Class: Opioid
Hydromorphone oral liquid and tablets are used to relieve pain. The hydromorphone extended-release tablets are used to relieve moderate to severe pain in opioid-tolerant patients.
Hydromorphone belongs to the group of medicines called narcotic analgesics (pain medicines). It acts on the central nervous system (CNS) to relieve pain.
When a narcotic medicine is used for a long time, it may become habit-forming, causing mental or physical dependence. However, people who have continuing pain should not let the fear of dependence keep them from using narcotics to relieve their pain. Mental dependence (addiction) is not likely to occur when narcotics are used for this purpose. Physical dependence may lead to withdrawal side effects if treatment is stopped suddenly. However, severe withdrawal side effects can usually be prevented by gradually reducing the dose over a period of time before treatment is stopped. completely.
This medicine is available only with your doctor's prescription.
In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:
Tell your doctor if you have ever had any unusual or allergic reaction to this medicine 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.
Appropriate studies have not been performed on the relationship of age to the effects of hydromorphone in the pediatric population. Safety and efficacy have not been established.
Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of hydromorphone in the elderly. However, elderly patients may be more sensitive to the effects of hydromorphone than younger adults, and are more likely to have age-related lung, liver, kidney, or heart problems, which may require caution and an adjustment in the dose for patients receiving hydromorphone.
| Pregnancy Category | Explanation | |
|---|---|---|
| All Trimesters | C | Animal studies have shown an adverse effect and there are no adequate studies in pregnant women OR no animal studies have been conducted and there are no adequate studies in pregnant women. |
Studies in women suggest that this medication poses minimal risk to the infant when used during breastfeeding.
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 this medicine, 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 this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.
Using this medicine 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.
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. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.
Using this medicine with any of the following is usually not recommended, but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use this medicine, or give you special instructions about the use of food, alcohol, or tobacco.
The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:
This section provides information on the proper use of a number of products that contain hydromorphone. It may not be specific to Dilaudid-5. Please read with care.
Take this medicine only as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered. This is especially important for elderly patients, who may be more sensitive to the effects of pain medicines. If too much of this medicine is taken for a long time, it may become habit-forming (causing mental or physical dependence).
Measure the oral liquid with a marked measuring spoon, oral syringe, or medicine cup. The average household teaspoon may not hold the right amount of liquid.
If you are using the extended-release tablets:
Exalgo® tablets works differently than hydromorphone tablets, even at the same dose (number of milligrams). Do not switch from the extended-release tablets to the immediate-release tablets unless your doctor tells you to.
Be careful not to handle crushed or broken tablets. If you have contact with broken or crushed tablets or spilled oral liquid, wash your skin or the affected areas with soap and water right away.
The dose of this medicine 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 this medicine. 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.
If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.
Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.
Keep out of the reach of children.
Do not keep outdated medicine or medicine no longer needed.
Ask your healthcare professional how you should dispose of any medicine you do not use.
Flush the unused medicine down the toilet.
It is very important that your doctor check your progress while you are using this medicine. This will allow your doctor to see if the medicine is working properly and to decide if you should continue to take it.
This medicine will add to the effects of alcohol and other CNS depressants (medicines that can make you drowsy or less alert). Some examples of CNS depressants are antihistamines or medicine for allergies or colds; sedatives, tranquilizers, or sleeping medicine; other prescription pain medicine or narcotics; medicine for seizures or barbiturates; muscle relaxants; or anesthetics, including some dental anesthetics. Check with your doctor before taking any of the other medicines listed above while you are using this medicine.
This medicine may be habit-forming. If you feel that the medicine is not working as well, do not use more than your prescribed dose. Call your doctor for instructions.
Dizziness, lightheadedness, or fainting may occur when you get up suddenly from a lying or sitting position. Getting up slowly may help lessen this problem. Also, lying down for a while may relieve dizziness or lightheadedness.
Using narcotics for a long time can cause severe constipation. To prevent this, your doctor may direct you to take laxatives, drink a lot of fluids, or increase the amount of fiber in your diet. Be sure to follow the directions carefully, because continuing constipation can lead to more serious problems.
This medicine may make you dizzy, drowsy, or lightheaded. Make sure you know how you react to this medicine before you drive, use machines, or do anything else that could be dangerous if you are dizzy or not alert.
This medicine may cause serious allergic reactions, including anaphylaxis. Anaphylaxis can be life-threatening and requires immediate medical attention. Call your doctor right away if you have a rash; itching; hoarseness; trouble breathing; trouble swallowing; or any swelling of your hands, face, or mouth while you are using this medicine.
If you have been using this medicine regularly for several weeks or more, do not change your dose or suddenly stop using it without first checking with your doctor. You may be directed to gradually reduce the amount you are using before stopping treatment completely, or to take another narcotic for a while, to lessen the chance of withdrawal side effects (such as abdominal or stomach cramps, anxiety, fever, nausea, runny nose, sweating, tremors, or trouble with sleeping).
Using this medicine while you are pregnant may cause neonatal withdrawal syndrome in your newborn babies. Tell your doctor right away if your child has the following symptoms: abnormal sleep pattern, diarrhea, high-pitched cry, irritability, shakiness or tremor, weight loss, vomiting, or failure to gain weight.
Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements.
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 immediately if any of the following side effects occur:
Get emergency help immediately if any of the following symptoms of overdose occur:
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:
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.
See also: Dilaudid-5 side effects (in more detail)
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Generic Name: zinc oxide topical (ZINK OX ide)
Brand Names: ARC, Balmex, Boudreaux Butt Paste, Caldesene, Calmol-4 Suppository, Critic-Aid Skin Paste, Delazinc, Dermagran BC, Desitin, Desitin Maximum Strength Original, Desitin Rapid Relief Creamy, Diaper Rash Ointment, Diaper Relief, Dr. Smith's Diaper, Flanders Buttocks Ointment, Geri-Protect, Medi-Paste, PeriGuard, Pinxav, Rash Relief, RVPaque, Seniortopix Healix, Soothe & Cool Skin Paste, Sportz Block Dark, Sportz Block Light, Sportz Block Medium, Triple Paste, Tronolane Suppositories, Unna-Flex Elastic Unna Boot 3 inch, Unna-Flex Elastic Unna Boot 4 inch, Znlin
Zinc oxide is a mineral.
Zinc oxide topical (for the skin) is used to treat diaper rash, minor burns, severely chapped skin, or other minor skin irritations.
Zinc oxide rectal suppositories are used to treat itching, burning, irritation, and other rectal discomfort caused by hemorrhoids or painful bowel movements.
Zinc oxide topical may also be used for purposes not listed in this medication guide.
Zinc oxide topical will not treat a bacterial or fungal infection. Call your doctor if you have any signs of infection such as redness and warmth or oozing skin lesions.
Keep the diaper area clean and dry to prevent worsening of skin rash. Change wet diapers as soon as possible. Allow the skin to dry thoroughly before putting on a fresh diaper.
Avoid using other medications on the areas you treat with zinc oxide unless you doctor tells you to.
Zinc oxide topical will not treat a bacterial or fungal infection. Call your doctor if you have any signs of infection such as redness and warmth or oozing skin lesions.
Use exactly as directed on the label, or as prescribed by your doctor. Do not use in larger or smaller amounts or for longer than recommended.
Apply enough of this medication to cover the entire area to be treated. Zinc oxide often leaves a thin white residue that may not be entirely rubbed in.
To treat chapped skin, minor burn wounds, or other skin irritations, use the medication as often as needed. Apply a thin layer to the affected area and rub in gently.
To treat diaper rash, use this medication each time the diaper is changed. It is especially important to apply the medication at bedtime or whenever there will be a long period of time between diaper changes.
Keep the diaper area clean and dry to prevent worsening of skin rash. Change wet diapers as soon as possible. Allow the skin to dry thoroughly before putting on a fresh diaper.
Zinc oxide rectal suppositories come with patient instructions for safe and effective use. Follow these directions carefully. Ask your doctor or pharmacist if you have any questions.
Try to empty your bowel and bladder just before using the suppository. Cleanse and dry your rectal area thoroughly.
Remove the outer wrapper from the suppository before inserting it. Avoid handling the suppository too long or it will melt in your hands.
For best results, stay lying down after inserting the suppository and hold it in your rectum for a few minutes. The suppository will melt quickly once inserted and you should feel little or no discomfort while holding it in.
Since zinc oxide is used on an as needed basis, you are not likely to miss a dose. Using extra zinc oxide to make up a missed dose will not make the medication more effective.
This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Avoid applying other skin medications on the same treatment area with zinc oxide, unless your doctor has told you to.
There may be other drugs that can interact with zinc oxide topical or rectal suppositories. Tell your doctor about all medications you use. This includes prescription, over-the-counter, vitamin, and herbal products. Do not start a new medication without telling your doctor.
See also: ARC side effects (in more detail)
Treating certain skin conditions (eg, seborrheic dermatitis) and certain bacterial infections of the skin. It may also be used for other conditions as determined by your doctor.
Sulfacetamide/Urea Medicated Pads are a sulfonamide antibiotic. It works by killing bacteria.
Contact your doctor or health care provider right away if any of these apply to you.
Some medical conditions may interact with Sulfacetamide/Urea Medicated Pads. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:
Some MEDICINES MAY INTERACT with Sulfacetamide/Urea Medicated Pads. Tell your health care provider if you are taking any other medicines, especially any of the following:
This may not be a complete list of all interactions that may occur. Ask your health care provider if Sulfacetamide/Urea Medicated Pads 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.
Use Sulfacetamide/Urea Medicated Pads as directed by your doctor. Check the label on the medicine for exact dosing instructions.
Ask your health care provider any questions you may have about how to use Sulfacetamide/Urea Medicated Pads.
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:
Irritation, stinging, or burning of the skin.
Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); bloody diarrhea; fever; joint pain; red, swollen, or blistered skin; severe diarrhea; sores in the mouth; stomach cramps/pain.
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.
Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center, or emergency room immediately. Sulfacetamide/Urea Medicated Pads may be harmful if swallowed. Symptoms of ingestion may include change in the amount of urine; nausea; vomiting.
Store Sulfacetamide/Urea Medicated Pads 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. Do not freeze. Keep Sulfacetamide/Urea Medicated Pads out of the reach of children and away from pets.
This information is a summary only. It does not contain all information about Sulfacetamide/Urea Medicated Pads. 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.
Methylergonovine Maleate Tablets, USP is a semi-synthetic ergot alkaloid used for the prevention and control of postpartum hemorrhage.
Methylergonovine Maleate Tablets, USP is available in tablets for oral ingestion containing 0.2 mg methylergonovine maleate.
Tablets
Active ingredient: Methylergonovine maleate, USP 0.2 mg
Inactive ingredients: acacia, corn starch, gelatin, lactose anhydrous, methylparaben, microcrystalline cellulose, povidone, propylparaben, stearic acid, tartaric acid.
Chemically, methylergonovine maleate is designated as ergoline-8-carboxamide, 9, 10-didehydro-N-[1-hydroxymethyl) propyl]-6-methyl-, [8β(S)]-, (Z)-2-butenedioate (1:1) (salt). Its structural formula is:
C20H25N3O2•C4H4O4 Mol Wt: 455.51
Methylergonovine maleate acts directly on the smooth muscle of the uterus and increases the tone, rate and amplitude of rhythmic contractions. Thus, it induces a rapid and sustained tetanic uterotonic effect which shortens the third stage of labor and reduces blood loss. The onset of action after I.V. administration is immediate; after I.M. administration, 2-5 minutes, and after oral administration, 5-10 minutes.
Pharmacokinetic studies following an I.V. injection have shown that methylergonovine is rapidly distributed from plasma to peripheral tissues within 2-3 minutes or less. The bioavailability after oral administration was reported to be about 60% with no accumulation after repeated doses. During delivery, with intramuscular injection, bioavailability increased to 78 %. Ergot alkaloids are mostly eliminated by hepatic metabolism and excretion, and the decrease in bioavailability following oral administration is probably a result of first-pass metabolism in the liver.
Bioavailability studies conducted in fasting healthy female volunteers have shown that oral absorption of a 0.2 mg methylergonovine tablet was fairly rapid with a mean peak plasma concentration of 3243 ± 1308 pg/mL observed at 1.12 ± 0.82 hours. For a 0.2 mg intramuscular injection, a mean peak plasma concentration of 5918 ± 1952 pg/mL was observed at 0.41 ± 0.21 hours. The extent of absorption of the tablet, based upon methylergonovine plasma concentrations, was found to be equivalent to that of the I.M. solution given orally, and the extent or oral absorption of the I.M. solution was proportional to the dose following administration of 0.1, 0.2 and 0.4 mg. When given intramuscularly, the extent of absorption of methylergonovine solution was about 25 % greater than the tablet. The volume of distribution (Vdss/F) of methylergonovine was calculated to be 56.1 ± 17.0 liters, and the plasma clearance (CLp/F) was calculated to be 14.4 ± 4.5 liters per hour. The plasma level decline was biphasic with a mean elimination half-life of 3.39 hours (range 1.5 to 12.7 hours). A delayed gastrointestinal absorption (Tmax about 3 hours) of methylergonovine maleate tablet might be observed in postpartum women during continuous treatment with this oxytocic agent.
For routine management after delivery of the placenta; postpartum atony and hemorrhage; subinvolution. Under full obstetric supervision, it may be given in the second stage of labor following delivery of the anterior shoulder.
Hypertension; toxemia; pregnancy; and hypersensitivity.
This drug should not be administered I.V. routinely because of the possibility of inducing sudden hypertensive and cerebrovascular accidents. If I.V administration is considered essential as a lifesaving measure, methylergonovine maleate should be given slowly over a period of no less than 60 seconds with careful monitoring of blood pressure. Intra-arterial or periarterial injection should be strictly avoided.
Caution should be exercised in the presence of sepsis, obliterative vascular disease, hepatic or renal involvement. Also use with caution during the second stage of labor. The necessity for manual removal of a retained placenta should occur only rarely with proper technique and adequate allowance of time for its spontaneous separation.
CYP 3A4 inhibitors (e.g., Macrolide Antibiotics and Protease Inhibitors)
There have been rare reports of serious adverse events in connection with the coadministration of certain ergot alkaloid drugs (e.g., dihydroergotamine and ergotamine) and potent CYP 3A4 inhibitors, resulting in vasospasm leading to cerebral ischemia and/or ischemia of the extremities. Although there have been no reports of such interactions of methylergonovine alone, potent CYP 3A4 inhibitors should not be coadministered with methylergonovine. Examples of some of the more potent CYP 3A4 inhibitors include macrolide antibiotics (e.g., erythromycin, troleandomycin, clarithromycin), HIV protease or reverse transcriptase inhibitors (e.g., ritonavir, indinavir, nelfinavir, delavirdine) or azole antifungals (e.g., ketoconazole, itraconazole, voriconazole). Less potent CYP 3A4 inhibitors should be administered with caution. Less potent inhibitors include saquinavir, nefazodone, fluconazole, grapefruit juice, fluoxetine, fluvoxamine, zileuton, and clotrimazole. These lists are not exhaustive, and the prescriber should consider the effects on CYP 3A4 of other agents being considered for concomitant use with methylergonovine.
No pharmacokinetic interactions involving other cytochrome P450 isoenzymes are known.
Caution should be exercised when methylergonovine maleate is used concurrently with other vasoconstrictors or ergot alkaloids.
No long-term studies have been performed in animals to evaluate carcinogenic potential. The effect of the drug on mutagenesis or fertility has not been determined.
Category C: Animal reproductive studies have not been conducted with methylergonovine maleate. It is also not known whether methylergonovine maleate can cause fetal harm or can affect reproductive capacity. Use of methylergonovine maleate is contraindicated during pregnancy because of its uterotonic effects. (See INDICATIONS AND USAGE).
The uterotonic effect of methylergonovine maleate is utilized after delivery to assist involution and decrease hemorrhage, shortening the third stage of labor.
Methylergonovine maleate may be administered orally for a maximum of 1 week postpartum to control uterine bleeding. Recommended dosage is 1 tablet (0.2 mg) 3 or 4 times daily. At this dosage level a small quantity of drug appears in mother’s milk. Caution should be exercised when methylergonovine maleate is administered to a nursing woman.
Safety and effectiveness in pediatric patients have not been established.
Clinical studies of methylergonovine maleate did not include sufficient number of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in response between the elderly and younger patients. In general dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
The most common adverse reaction is hypertension associated in several cases with seizure and/or headache. Hypotension has also been reported. Nausea and vomiting have occurred occasionally. Rarely observed reactions have included: acute myocardial infarction, transient chest pains, arterial spasm (coronary and peripheral), bradycardia, tachycardia, dyspnea, hematuria, thrombophlebitis, water intoxication, hallucinations, leg cramps, dizziness, tinnitus, nasal congestion, diarrhea, diaphoresis, palpitation, rash, and foul taste.1
There have been rare isolated reports of anaphylaxis, without a proven causal relationship to the drug product.
Methylergonovine maleate has not been associated with drug abuse or dependence of either a physical or psychological nature.
Symptoms of acute overdose may include: nausea, vomiting, abdominal pain, numbness, tingling of the extremities, rise in blood pressure, in severe cases followed by hypotension, respiratory depression, hypothermia, convulsions, and coma.
Because reports of overdosage with methylergonovine maleate are infrequent, the lethal dose in humans has not been established. The oral LD50 (in mg/kg) for the mouse is 187, the rat is 93, and the rabbit 4.5.2 Several cases of accidental Methylergonovine Maleate Injection in newborn infants have been reported, and in such cases 0.2 mg represents an overdose of great magnitude. However, recovery occurred in all but in one case following a period of respiratory depression, hypothermia, hypertonicity with jerking movements, and, in one case, a single convulsion.
Also, several children 1-3 years of age have accidentally ingested up to 10 tablets (2 mg) with no apparent ill effects. A postpartum patient took 4 tablets at one time in error and reported paresthesias and clamminess as her only symptoms.
Treatment of acute overdosage is symptomatic and includes the usual procedures of:
Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration.
Intramuscularly
1 mL, 0.2 mg, after delivery of the anterior shoulder, after delivery of the placenta, or during the puerperium. May be repeated as required, at intervals of 2-4 hours.
Intravenously
Dosage same as intramuscular. (See WARNINGS.)
Orally
One tablet, 0.2 mg, 3 to 4 times daily in the puerperium for a maximum of 1 week.
White, round, biconvex compressed tablets debossed with “KP” on one side and “01” on the other side.
Bottles of 100: NDC 40032-140-01
Tablets: Store below 25°C (77°F); in tight, light-resistant container.
Manufactured by:
Novel Laboratories, Inc.
Somerset, NJ 08873
NIN-140-00
Rev: 02/11
| METHYLERGONOVINE MALEATE methylergonovine maleate tablet | ||||||||||||||||||||||||
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| Marketing Information | |||
| Marketing Category | Application Number or Monograph Citation | Marketing Start Date | Marketing End Date |
| ANDA | ANDA091577 | 06/15/2011 | |
| Labeler - Novel Laboratories, Inc. (793518643) |
| Registrant - Novel Laboratories, Inc. (793518643) |
| Establishment | |||
| Name | Address | ID/FEI | Operations |
| Novel Laboratories, Inc. | 793518643 | MANUFACTURE | |
| Establishment | |||
| Name | Address | ID/FEI | Operations |
| Ivax Pharmaceuticals, Inc. | 643896244 | API MANUFACTURE | |
Generic Name: brompheniramine (brome feh NEER a meen)
Brand Names: BroveX, BroveX CT, Dimetane, Dimetane Extentab, Dimetapp Allergy, Dimetapp Allergy Liquigel, Lodrane 12 Hour
Brompheniramine is an antihistamine. Brompheniramine blocks the effects of the naturally occurring chemical histamine in the body.
Brompheniramine is used to sneezing; runny nose; itching, watery eyes; hives; rashes; itching; and other symptoms of allergies and the common cold.
Brompheniramine may also be used for purposes other than those listed in this medication guide.
Before taking brompheniramine, talk to your doctor if you have
glaucoma or increased pressure in the eye;
a stomach ulcer;
an enlarged prostate, bladder problems or difficulty urinating;
an overactive thyroid (hyperthyroidism);
hypertension or any type of heart problems; or
asthma.
You may not be able to take brompheniramine, or you may require a dosage adjustment or special monitoring during treatment if you have any of the conditions listed above.
Take brompheniramine exactly as directed on the package or as directed by your doctor. If you do not understand these directions, ask your pharmacist, nurse, or doctor to explain them to you.
Brompheniramine can be taken with or without food.
To ensure that you get a correct dose, measure the liquid form of brompheniramine with a special dose-measuring spoon or cup, not with a regular table spoon. If you do not have a dose-measuring device, ask your pharmacist where you can get one.
Take the missed dose as soon as you remember. However, if it is almost time for the next dose, skip the missed dose and take only the next regularly scheduled dose. Do not take a double dose of this medication unless otherwise directed by your doctor.
Symptoms of a brompheniramine overdose may include extreme sleepiness, confusion, weakness, ringing in the ears, blurred vision, large pupils, dry mouth, flushing, fever, shaking, insomnia, hallucinations, and possibly seizures.
Do not take other over-the-counter cough, cold, allergy, diet, pain, or sleep medications while taking brompheniramine without first talking to your pharmacist or doctor. Other medications may also contain brompheniramine or other similar drugs, and you may accidentally take too much of these medicines.
Brompheniramine may increase the effects of other drugs that cause drowsiness, including antidepressants, alcohol, other antihistamines, pain relievers, anxiety medicines, seizure medicines, and muscle relaxants. Dangerous sedation, dizziness, or drowsiness may occur if brompheniramine is taken with any of these medications.
Other, less serious side effects may be more likely to occur. Continue to take brompheniramine and talk to your doctor if you experience
sleepiness, fatigue, or dizziness;
headache;
dry mouth; or
difficulty urinating or an enlarged prostate.
Side effects other than those listed here may also occur. Talk to your doctor about any side effect that seems unusual or that is especially bothersome. You may report side effects to FDA at 1-800-FDA-1088.
Do not take other over-the-counter cough, cold, allergy, diet, pain, or sleep medications while taking brompheniramine without first talking to your pharmacist or doctor. Other medications may also contain brompheniramine or other similar drugs, and you may accidentally take too much of these medicines.
Brompheniramine may increase the effects of other drugs that cause drowsiness, including antidepressants, alcohol, other antihistamines, pain relievers, anxiety medicines, seizure medicines, and muscle relaxants. Dangerous sedation, dizziness, or drowsiness may occur if brompheniramine is taken with any of these medications.
Drugs other than those listed here may also interact with brompheniramine. Talk to your doctor and pharmacist before taking any prescription or over-the-counter medicines, including vitamins, minerals, and herbal products.
See also: Dimetapp Allergy Liquigel side effects (in more detail)
Class: Selective Serotonin- and Norepinephrine-reuptake Inhibitors
Chemical Name: RS-4-[2-dimethylamino-1-(1-hydroxycyclohexyl)ethyl]phenol
Molecular Formula: C16H25NO2•C4H6O4•H2O
CAS Number: 386750-22-7
Brands: Pristiq
Antidepressants may increase risk of suicidal thinking and behavior (suicidality) in children, adolescents, and young adults (18–24 years of age) with major depressive disorder and other psychiatric disorders; balance this risk with clinical need.1 7 8 Desvenlafaxine is not approved for use in pediatric patients.1 (See Pediatric Use under Cautions.)
In pooled data analyses, risk of suicidality was not increased in adults >24 years of age and apparently was reduced in adults ≥65 years of age with antidepressant therapy compared with placebo.1 7 8
Depression and certain other psychiatric disorders are themselves associated with an increased risk of suicide.1 7 8 9
Appropriately monitor and closely observe all patients who are started on desvenlafaxine therapy for clinical worsening, suicidality, or unusual changes in behavior; involve family members and/or caregivers in this process.1 7 8 9 (See Worsening of Depression and Suicidality Risk under Cautions.)
A selective serotonin- and norepinephrine-reuptake inhibitor (SNRI); an antidepressant.1 3 4 5 6 19
Treatment of major depressive disorder in adults.1 3 5 6
Efficacy of long-term use (i.e., >8 weeks) not established by controlled studies.1 If desvenlafaxine is used for extended periods, the need for continued therapy should be reassessed periodically.1
Allow at least 14 days to elapse between discontinuance of an MAO inhibitor and initiation of desvenlafaxine and at least 7 days to elapse between discontinuance of desvenlafaxine and initiation of an MAO inhibitor.1
If switching from another antidepressant (including venlafaxine) to desvenlafaxine, may be necessary to taper dosage of the previous antidepressant to minimize discontinuance symptoms.a
Monitor for possible worsening of depression, suicidality, or unusual changes in behavior, especially at the beginning of therapy or during periods of dosage adjustments.1 7 8 9 (See Worsening of Depression and Suicidality Risk under Cautions.)
Avoid abrupt discontinuance.1 Taper dosage gradually and monitor for withdrawal symptoms.1 25 26 If intolerable symptoms occur following dosage reduction or discontinuance, consider reinstituting previously prescribed dosage, then resume more gradual dosage reductions.1 (See Worsening of Depression and Suicidality Risk and also see Withdrawal of Therapy under Cautions.)
If used during pregnancy, consider cautiously tapering dosage during third trimester prior to delivery.1 2 15 (See Pregnancy under Cautions.)
Sustained therapy may be required; periodically reassess need for continued therapy.1 28
Administer orally with or without food at approximately the same time each day.1
Swallow extended-release tablets whole with fluid; do not divide, crush, chew, or dissolve.1
Available as desvenlafaxine succinate; dosage expressed in terms of desvenlafaxine.1
50 mg once daily.1 Although efficacy established at dosages of 50–400 mg once daily in clinical studies, no additional benefit observed with dosages >50 mg once daily; adverse effects and discontinuances were more frequent at higher dosages.1
Optimum duration not established; may require several months or longer of sustained antidepressant therapy.1 28 Long-term efficacy (i.e., >8 weeks) of desvenlafaxine at a dosage of 50 mg once daily not studied.1 Periodically reassess need for continued therapy.1 28
Initially, 50 mg once daily.a Dosage increases to >100 mg daily not recommended.a
Mild renal impairment (Clcr 50–80 mL/minute): No dosage adjustment needed.1
Moderate renal impairment (Clcr 30–50 mL/minute): 50 mg once daily.1 Do not increase dosage.a
Severe renal impairment (Clcr< 30 mL/minute) or end-stage renal disease: 50 mg every other day.1 Do not increase dosage and do not give supplemental doses after dialysis.a
No specific dosage recommendations at this time, but consider possibility of age-related decreases in renal function when selecting dosage.1 May administer drug every other day if poorly tolerated.1
Known hypersensitivity to desvenlafaxine, venlafaxine, or any ingredient in the formulation.1
Concurrent or recent (i.e., within 2 weeks) therapy with an MAO inhibitor.1 Allow at least 7 days to elapse after discontinuing desvenlafaxine before initiating an MAO inhibitor.1 (See Serotonin Syndrome or Neuroleptic Malignant Syndrome [NMS]-like Reactions under Cautions.)
Possible worsening of depression and/or the emergence of suicidal ideation and behavior (suicidality) or unusual changes in behavior in both adult and pediatric patients with major depressive disorder, whether or not they are taking antidepressants; may persist until clinically important remission occurs.1 7 8 9 18 (See Boxed Warning and also see Pediatric Use under Cautions.) However, suicide is a known risk of depression and certain other psychiatric disorders, and these disorders themselves are the strongest predictors of suicide. 1 7 8 9
Appropriately monitor and closely observe patients receiving desvenlafaxine for any reason, particularly during initiation of therapy (i.e., the first few months) and during periods of dosage adjustments.1 7 8 9
Anxiety, agitation, panic attacks, insomnia, irritability, hostility, aggressiveness, impulsivity, akathisia, hypomania, and/or mania may be precursors to emerging suicidality.1 8 9 Consider changing or discontinuing therapy in patients whose depression is persistently worse or in those with emerging suicidality or symptoms that might be precursors to worsening depression or suicidality, particularly if severe, abrupt in onset, or not part of the patient’s presenting symptoms.1 8 If decision is made to discontinue drug therapy, taper desvenlafaxine dosage as rapidly as is feasible but consider risks of abrupt discontinuance.1 25 26 (See General under Dosage and Administration.)
Prescribe in smallest quantity consistent with good patient management to reduce risk of overdosage.1 8
May unmask bipolar disorder.1 (See Activation of Mania/Hypomania under Cautions.) Desvenlafaxine is not approved for use in treating bipolar depression.1
Screen for risk of bipolar disorder by obtaining detailed psychiatric history (e.g., family history of suicide, bipolar disorder, depression) prior to initiating therapy.1
Potentially life-threatening serotonin syndrome or neuroleptic malignant syndrome (NMS)-like reactions reported during concurrent therapy with SSRIs or SNRIs and other serotonergic drugs (e.g., 5-HT1 receptor agonists [“triptans”]), drugs that impair serotonin metabolism (e.g., MAO inhibitors), or antipsychotics or other dopamine antagonists.1 (See Contraindications under Cautions and see Interactions.)
Symptoms of serotonin syndrome may include mental status changes (e.g., agitation, hallucinations, coma), autonomic instability (e.g., tachycardia, labile BP, hyperthermia), neuromuscular aberrations (e.g., hyperreflexia, incoordination), and/or GI symptoms (e.g., nausea, vomiting, diarrhea).1
Severe serotonin syndrome may resemble NMS, which is characterized by hyperthermia, muscle rigidity, autonomic instability with possible rapid fluctuation of vital signs, and mental status changes.1
Monitor patients receiving desvenlafaxine for the development of serotonin syndrome or NMS-like signs and symptoms.1 If serotonin syndrome or NMS signs and symptoms occur, discontinue desvenlafaxine and any concurrently administered serotonergic or antidopaminergic agents, including antipsychotic agents, and initiate supportive and symptomatic treatment.1
Sustained hypertension (i.e., treatment-emergent increases in supine DBP ≥90 mm Hg and ≥10 mm Hg above baseline for 3 consecutive visits) reported; potential adverse consequences.1 Elevated BP requiring immediate treatment also reported.1
Control preexisting hypertension before initiating desvenlafaxine therapy and regularly monitor BP during therapy.1 Exercise caution in patients with preexisting hypertension or other underlying conditions that may be compromised by increases in BP.1 If sustained increases in BP occur, consider desvenlafaxine dosage reduction or discontinuance.1
Case reports and epidemiologic studies have demonstrated an association between the use of drugs that interfere with serotonin reuptake and the occurrence of GI bleeding.1 21 Possible increased risk of bleeding with SSRIs and SNRIs, including desvenlafaxine; events ranged from ecchymoses, hematomas, epistaxis, and petechiae to life-threatening hemorrhages.1 21 Concurrent administration of aspirin, NSAIAs, warfarin, and other anticoagulants may increase risk.1 (See Drugs Affecting Hemostasis under Interactions and also see Advice to Patients.)
Mydriasis reported.1 Monitor patients with elevated IOP or at risk of angle-closure glaucoma.1
Possible activation of mania and hypomania; use with caution in patients with personal or family history of mania or hypomania.1 (See Bipolar Disorder under Cautions.)
Increases in BP and small increases in heart rate reported; use with caution in patients with cardiovascular, cerebrovascular, or lipid metabolism disorders.1
Dose-dependent, possibly clinically significant increases in fasting serum total cholesterol, LDL cholesterol, and triglycerides reported; consider measuring serum lipid concentrations during therapy.1
Withdrawal effects reported with abrupt discontinuance or dosage reduction; reactions included dizziness, nausea, headache, irritability, insomnia, diarrhea, anxiety, fatigue, abnormal dreams, and hyperhidrosis and occurred more frequently with longer duration of therapy.1 Withdrawal effects also reported upon discontinuance of other SNRIs and SSRIs, particularly when abrupt; events generally are self-limiting, but may be serious.1
If intolerable symptoms occur following dosage reduction or discontinuance, consider reinstituting previously prescribed dosage, then resume more gradual dosage reductions.1
Seizures reported in premarketing clinical studies.1 Desvenlafaxine has not been studied in patients with a history of seizures; use with caution in such patients.1
Possible hyponatremia or SIADH; use with caution in patients who are volume-depleted, elderly, or taking diuretics.1 Initiate appropriate medical intervention and consider drug discontinuance in patients with symptomatic hyponatremia.1
Do not use products containing desvenlafaxine and products containing venlafaxine concomitantly with Pristiq (desvenlafaxine succinate); desvenlafaxine is the principal active metabolite of venlafaxine.1 (See Serotonin Syndrome or Neuroleptic Malignant Syndrome [NMS]-like Reactions under Cautions.)
Interstitial lung disease and eosinophilic pneumonia associated with venlafaxine (parent drug of desvenlafaxine) reported rarely; consider possibility in patients treated with desvenlafaxine who present with progressive dyspnea, cough, or chest discomfort.1 Promptly evaluate patients with these symptoms and consider discontinuance of desvenlafaxine.1
Category C.1
Possible complications, sometimes severe and requiring prolonged hospitalization, respiratory support, enteral nutrition, and other forms of supportive care in neonates exposed to SNRIs or SSRIs late in the third trimester; may arise immediately upon delivery.1 12 13 14 15 16 17
Carefully consider the potential risks and benefits of treatment when used during the third trimester of pregnancy.1 13 14 15 Consider cautiously tapering dosage during the third trimester prior to delivery.1 14 15 16 17
Distributed into milk; discontinue nursing or the drug.1
Safety and effectiveness not established in pediatric patients <18 years of age.1 6 Possible adverse effects on weight, height, appetite, BP, and serum cholesterol concentrations reported in pediatric patients receiving venlafaxine, the parent drug of desvenlafaxine.2
FDA warns that a greater risk of suicidal thinking or behavior (suicidality) occurred during the first few months of antidepressant treatment compared with placebo in children and adolescents with major depressive disorder, obsessive-compulsive disorder (OCD), or other psychiatric disorders based on pooled analyses of 24 short-term, placebo-controlled trials of 9 antidepressant drugs (SSRIs and others).1 8 However, a more recent meta-analysis of 27 placebo-controlled trials of 9 antidepressants (SSRIs and others) in patients <19 years of age with major depressive disorder, OCD, or non-OCD anxiety disorders suggests that the benefits of antidepressant therapy in treating these conditions may outweigh the risks of suicidal behavior or suicidal ideation.18 No suicides occurred in these pediatric trials.1 8 18
Carefully consider these findings when assessing potential benefits and risks of desvenlafaxine in a child or adolescent for any clinical use.1 8 9 18 (See Suicidality in the Boxed Warning and see Worsening of Depression and Suicidality Risk under Cautions.)
No overall differences in safety or efficacy observed relative to younger adults, but increased sensitivity cannot be ruled out.1 Consider possible reduced renal clearance of the drug in geriatric patients.1 (See Dosage and Administration: Special Populations and see Absorption: Special Populations, under Pharmacokinetics.)
Higher incidence of systolic orthostatic hypotension reported in patients ≥65 years of age.1
Clinically important hyponatremia reported in geriatric patients.1 (See Hyponatremia/SIADH under Cautions.)
In pooled data analyses, a reduced risk of suicidality was observed in adults ≥65 years of age with antidepressant therapy compared with placebo.1 7 8 (See Suicidality in the Boxed Warning and see Worsening of Depression and Suicidality Risk under Cautions.)
Increased mean elimination half-life in patients with moderate and severe hepatic impairment compared with healthy individuals and patients with mild hepatic impairment.1 (See Hepatic Impairment under Dosage and Administration and see Elimination: Special Populations, under Pharmacokinetics.)
Decreased clearance in patients with moderate or severe renal impairment or end-stage renal disease; adjust dosage.1 (See Renal Impairment under Dosage and Administration and see Elimination: Special Populations, under Pharmacokinetics.)
Nausea, dizziness, insomnia, hyperhidrosis, constipation, somnolence, decreased appetite, anxiety, and sexual function disorders in males (e.g., anorgasmia, decreased libido, abnormal orgasm, delayed ejaculation, erectile dysfunction, ejaculation disorder, ejaculation failure).1 3 4 5 19
Principally metabolized via conjugation by UGT isoenzymes; oxidation via CYP3A4 isoenzyme is a minor metabolic pathway.1 6 Minimally inhibits CYP2D6; does not inhibit CYP 1A2, 2A6, 2C8, 2C9, or 2C19 isoenzymes; did not inhibit or induce CYP3A4 in vitro (see Drugs Metabolized by Hepatic Microsomal Enzymes under Interactions).1 6 22
Desvenlafaxine is not a substrate or an inhibitor of the P-glycoprotein transporter in vitro.1
Drugs metabolized by CYP2D6: Potential pharmacokinetic interaction (increased CYP2D6 substrate plasma concentrations).1 22
Drugs metabolized by CYP3A4: Potential pharmacokinetic interaction (reduced exposure to CYP3A4 substrate).1 Although no inhibition or induction of CYP3A4 observed in vitro, AUC and peak plasma concentrations of CYP3A4 substrate decreased with concomitant administration of desvenlafaxine in one study.1
Drugs metabolized by CYP1A2, 2A6, 2C8, 2C9, or 2C19 isoenzymes: Pharmacokinetic interaction unlikely.1
Potent CYP3A4 inhibitors: Potential pharmacokinetic interaction (increased plasma desvenlafaxine concentrations).1 6
Inhibitors of CYP isoenzymes 1A1, 1A2, 2A6, 2C8, 2C9, 2C19, 2D6, and 2E1: Clinically important pharmacokinetic interaction is unlikely.1
Potential pharmacologic interaction (potentially serious, sometimes fatal serotonin syndrome or NMS-like reactions) with serotonergic drugs.1 Avoid concomitant use or exercise caution.1 If serotonin syndrome or NMS occurs, immediately discontinue desvenlafaxine and any concurrently administered antidopaminergic or serotonergic agents and initiate supportive and symptomatic treatment.1 (See Specific Drugs under Interactions and see Serotonin Syndrome or Neuroleptic Malignant Syndrome [NMS]-like Reactions under Cautions.)
Potential pharmacologic interaction (increased risk of bleeding) if used concurrently with drugs that affect coagulation or bleeding; use with caution.1 23 (See Abnormal Bleeding under Cautions.)
Pharmacokinetic interaction unlikely.1
Potential interactions not systematically evaluated to date; use with caution.1
Risks and/or benefits of combined use of electroconvulsive therapy and desvenlafaxine not evaluated.1
Drug | Interaction | Comments |
|---|---|---|
Alcohol | Desvenlafaxine did not increase alcohol-induced impairment of mental and motor skills in a clinical study1 | Manufacturer recommends avoiding concomitant alcohol consumption during desvenlafaxine therapy1 |
Anticoagulants (e.g., warfarin) | Potential pharmacologic interaction (increased risk of bleeding)1 23 | Carefully monitor patients receiving warfarin during initiation and discontinuance of desvenlafaxine1 |
Antipsychotic agents | Potential pharmacologic interaction (potentially serious, sometimes fatal serotonin syndrome or NMS-like reactions)1 | If serotonin syndrome or NMS occurs, immediately discontinue desvenlafaxine and any concurrently administered antidopaminergic or serotonergic agents and initiate supportive and symptomatic treatment1 |
Desipramine | Increased peak plasma concentrations and AUCs of desipramine 1 22 | |
Diuretics | Consider risk of hyponatremia1 | |
Dopamine antagonists | Potential pharmacologic interaction (potentially serious, sometimes fatal serotonin syndrome or NMS-like reactions)1 | If serotonin syndrome or NMS occurs, immediately discontinue desvenlafaxine and any concurrently administered antidopaminergic or serotonergic agents and initiate supportive and symptomatic treatment1 |
5-HT1 receptor agonists (“triptans”) (e.g., almotriptan, eletriptan, frovatriptan, naratriptan, rizatriptan, sumatriptan, zolmitriptan) | Potential pharmacologic interaction (potentially serious, sometimes fatal serotonin syndrome or NMS-like reactions)1 24 | If concurrent therapy is clinically warranted, carefully observe patient, particularly during initiation or dosage increase or when initiating another serotonergic agent1 24 If serotonin syndrome or NMS occurs, immediately discontinue desvenlafaxine and any concurrently administered antidopaminergic or serotonergic agents and initiate supportive and symptomatic treatment1 |
Ketoconazole | Increased AUC and peak plasma concentrations of desvenlafaxine1 6 | |
Lithium | Potential pharmacologic interaction (potentially serious, sometimes fatal serotonin syndrome or NMS-like reactions)1 | Use concomitantly with caution1 If serotonin syndrome or NMS occurs, immediately discontinue desvenlafaxine and any concurrently administered antidopaminergic or serotonergic agents and initiate supportive and symptomatic treatment1 |
MAO inhibitors (e.g., antidepressants, linezolid) | Risk of serious, sometimes fatal serotonin syndrome or NMS-like reactions1 | Concomitant use with MAO inhibitors contraindicated1 Do not use desvenlafaxine within 14 days of stopping an MAO inhibitor; allow ≥7 days between discontinuance of desvenlafaxine and initiation of MAO inhibitor1 If serotonin syndrome or NMS occurs, immediately discontinue desvenlafaxine and any concurrently administered antidopaminergic or serotonergic agents and initiate supportive and symptomatic treatment1 |
Midazolam | Decreased AUC and peak plasma concentrations of midazolam1 | |
NSAIAs (e.g., aspirin) | Potential pharmacologic interaction (increased risk of bleeding)1 23 | Use concomitantly with caution1 |
Sibutramine | Potential pharmacologic interaction (potentially serious, sometimes fatal serotonin syndrome or NMS-like reactions)1 | Use concomitantly with caution1 If serotonin syndrome or NMS occurs, immediately discontinue desvenlafaxine and any concurrently administered antidopaminergic or serotonergic agents and initiate supportive and symptomatic treatment1 |
SNRIs or SSRIs | Potential pharmacologic interaction (potentially serious, sometimes fatal serotonin syndrome or NMS-like reactions)1 | If serotonin syndrome or NMS occurs, immediately discontinue desvenlafaxine and any concurrently administered antidopaminergic or serotonergic agents and initiate supportive and symptomatic treatment1 |
St. John’s wort (Hypericum perforatum) | Potential pharmacologic interaction (potentially serious, sometimes fatal serotonin syndrome or NMS-like reactions)1 | Use concomitantly with caution1 If serotonin syndrome or NMS occurs, immediately discontinue desvenlafaxine and any concurrently administered antidopaminergic or serotonergic agents and initiate supportive and symptomatic treatment1 |
Tramadol | Potential pharmacologic interaction (potentially serious, sometimes fatal serotonin syndrome or NMS-like reactions)1 | Use concomitantly with caution1 If serotonin syndrome or NMS occurs, immediately discontinue desvenlafaxine and any concurrently administered antidopaminergic or serotonergic agents and initiate supportive and symptomatic treatment1 |
Tryptophan and other serotonin precursors | Potential pharmacologic interaction (potentially serious, sometimes fatal serotonin syndrome or NMS-like reactions)1 | Concomitant use not recommended1 If serotonin syndrome or NMS occurs, immediately discontinue desvenlafaxine and any concurrently administered antidopaminergic or serotonergic agents and initiate supportive and symptomatic treatment.1 |
Venlafaxine | Desvenlafaxine is the major active metabolite of venlafaxine1 | Do not use desvenlafaxine and venlafaxine concomitantly1 |
Absolute oral bioavailability is about 80%.1
Peak plasma concentrations achieved about 7.5 hours after oral administration.1
In women, peak plasma concentrations and AUC were approximately 25 and 10% higher, respectively, than age-matched men, but no dosage adjustment needed.1
Peak plasma concentration was increased about 16% in the fed state compared with fasting, but AUCs were similar; difference not clinically important.1
In healthy geriatric individuals 65–75 years of age, there was no change in peak plasma concentrations, but AUC was increased approximately 32% compared with subjects 18–45 years of age.1 In geriatric individuals >75 years of age, peak plasma concentrations increased approximately 32%, and AUC increased 55% compared with subjects 18–45 years of age.1
Distributed into milk.1
30%; plasma protein binding of desvenlafaxine is independent of plasma concentrations.1 6
Principally metabolized via conjugation by UGT isoenzymes; oxidation via CYP3A4 isoenzyme is a minor metabolic pathway.1 6
Approximately 45% of a single oral dose is eliminated unchanged in urine at 72 hours; approximately 19% of the dose is excreted as the glucuronide metabolite and less than 5% is excreted as the oxidative metabolite (N,O-didesmethylvenlafaxine) in urine.1 6
Mean elimination half-life is approximately 11 hours.1 6
In patients with moderate (Child-Pugh class B) and severe (Child-Pugh class C) hepatic impairment, average AUC was increased by approximately 31 and 35%, respectively compared with healthy individuals; in patients with mild hepatic impairment (Child-Pugh class A), average AUC values were similar to those in healthy subjects (<5% difference).1 In patients with moderate and severe hepatic impairment, systemic clearance was decreased by approximately 20 and 36%, respectively, compared with healthy individuals.1 In patients with mild hepatic impairment, systemic clearance was comparable to that in healthy individuals.1 Half-life was 13 and 14 hours in patients with moderate and severe hepatic impairment, respectively; half-life in patients with mild hepatic impairment was similar to that in healthy individuals.1
In patients with renal impairment, elimination was correlated with Clcr.1 AUC was increased about 42% in mild renal impairment (24-hour Clcr: 50–80 mL/minute), about 56% in moderate renal impairment (24-hour Clcr: 30–50 mL/minute), about 108% in severe renal impairment (24-hour Clcr: ≤30 mL/minute), and about 116% in end-stage renal disease subjects, compared with healthy, age-matched control subjects.a The mean terminal half-life was prolonged from 11.1 hours in the control subjects to approximately 13.5, 15.5, 17.6, and 22.8 hours in mild, moderate, and severe renal impairment, and end-stage renal disease subjects, respectively.1 Less than 5% of the drug in the body was cleared during a standard 4-hour hemodialysis procedure.1
20–25°C (may be exposed to 15–30°C).1
Desvenlafaxine is the principal active metabolite of venlafaxine and is pharmacologically related to duloxetine, another SNRI.1 3 4 5 20
Exact mechanism of antidepressant action has not been fully elucidated but appears to be associated with potentiation of serotonergic and noradrenergic activity in the CNS.1 4 5 6
Desvenlafaxine is a potent inhibitor of neuronal serotonin and norepinephrine reuptake; however, inhibition of dopamine reuptake at concentrations that inhibit serotonin and norepinephrine reuptake appears unlikely in most patients.1 2 3 4 5 20
Desvenlafaxine does not inhibit MAO and has not demonstrated substantial affinity for muscarinic cholinergic, H1-histaminergic, α1-adrenergic, dopaminergic, GABA, glutamate, and opiate receptors in vitro.1 3 4 5 6
Risk of suicidality; importance of patients, family, and caregivers being alert to and immediately reporting emergence of suicidality, worsening depression, or unusual changes in behavior, especially during the first few months of therapy or during periods of dosage adjustment.1 7 8 9 FDA recommends providing written patient information (medication guide) explaining risks of suicidality each time the drug is dispensed.1 7 8 9
Importance of informing patients of potential risk of serotonin syndrome and neuroleptic malignant syndrome (NMS)-like reactions, particularly with concurrent use of desvenlafaxine and 5-HT1 receptor agonists (also called triptans), tramadol, tryptophan, other serotonergic agents, or antipsychotic agents.1 Importance of immediately contacting clinician if signs and symptoms of these syndromes develop (e.g., restlessness, hallucinations, loss of coordination, fast heart beat, increased body temperature, muscle stiffness, increased BP, diarrhea, coma, nausea, vomiting, confusion).1
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs or herbal supplements, as well as any concomitant illnesses (e.g., cardiovascular, cerebrovascular, or lipid metabolism disorders; glaucoma) or personal or family history of suicidality or bipolar disorder.1
Importance of advising patients about the risk of bleeding associated with concomitant use of desvenlafaxine with aspirin or other NSAIAs, warfarin, or other drugs that affect coagulation.1
Importance of advising patients not to concurrently take other products containing desvenlafaxine or venlafaxine.1
Importance of instructing patients not to take desvenlafaxine with an MAO inhibitor or within 14 days of stopping the drug, and to allow 7 days after stopping desvenlafaxine before starting therapy with an MAO inhibitor.1
Importance of advising patients that they should have regular BP monitoring while taking desvenlafaxine.1
Importance of advising patients with raised IOP or at risk of acute narrow-angle glaucoma (angle-closure glaucoma) that mydriasis has been reported with desvenlafaxine and that they should be monitored.1
Importance of advising patients, their families, and caregivers to observe desvenlafaxine-treated patients for signs of activation of mania/hypomania.1
Importance of advising patients that elevations in total cholesterol, LDL, and triglycerides may occur; measurement of lipid concentrations may be considered.1
Importance of advising patients to notify their clinician if they develop any allergic signs or symptoms during therapy (e.g., rash, hives, swelling, difficulty breathing).1
Risk of cognitive and motor impairment; importance of exercising caution while operating hazardous machinery, including automobile driving, until patients are reasonably certain that desvenlafaxine therapy does not adversely affect their ability to engage in such activities.1
Importance of avoiding alcohol during desvenlafaxine therapy.1
Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1
Importance of advising patients that it usually takes several weeks of antidepressant therapy before they will start to feel better.1 Advise patients not to stop taking the drug if they do not feel the results right away.1
Importance of advising patients not to stop taking desvenlafaxine without first talking with their clinician.1 Importance of patients being aware that discontinuance effects may occur when stopping desvenlafaxine or when switching from another antidepressant to desvenlafaxine.1 a
Importance of informing patients to swallow desvenlafaxine extended-release tablets whole, and not to crush, cut, chew, or dissolve the tablets.1
Importance of informing patients that they may notice an inert matrix tablet passing in the stool or via colostomy, and that the active medication has already been absorbed by the time the patient sees the inert matrix tablet.1
Importance of informing patients of other important precautionary information.1 (See Cautions.)
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
|---|---|---|---|---|
Oral | Tablet, extended-release, film-coated | 50 mg (of desvenlafaxine) | Pristiq | Wyeth |
100 mg (of desvenlafaxine) | Pristiq | Wyeth |
This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 03/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.
Pristiq 100MG 24-hr Tablets (WYETH): 30/$146.99 or 90/$417.96
Pristiq 50MG 24-hr Tablets (WYETH): 30/$141.99 or 90/$406.97
This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.
The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.
AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions August 2010. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.
1. Wyeth Laboratories Inc. Pristiq (desvenlafaxine succinate) extended-release tablets prescribing information. Philadelphia, PA; 2009 Feb.
2. Wyeth Laboratories. Effexor (venlafaxine hydrochloride) tablets prescribing information. Philadelphia, PA: 2008 Feb.
3. DeMartinis NA, Yeung PP, Entsuah R et al. A double-blind, placebo-controlled study of the efficacy and safety of desvenlafaxine succinate in the treatment of major depressive disorder. J Clin Psychiatry. 2007; 68:677-88. [PubMed 17503976]
4. Deecher DC, Beyer CE, Johnston G et al. Desvenlafaxine succinate: a new serotonin and norepinephrine reuptake inhibitor. J Pharmacol Exp Ther. 2006; 318:657-65. [PubMed 16675639]
5. Septien-Velez L, Pitrosky B, Padmanabhan SK et al. A randomized, double-blind, placebo-controlled trial of desvenlafaxine succinate in the treatment of major depressive disorder. Int Clin Psychopharmacol. 2007; 22:338-47.
6. Wyeth Laboratories, Philadelphia, PA: Personal communication.
