Jalyn

Generic Name: dutasteride and tamsulosin (Oral route)

doo-TAS-ter-ide, tam-SOO-loe-sin hye-droe-KLOR-ide

Commonly used brand name(s)

In the U.S.

• Jalyn

Available Dosage Forms:

• Capsule

Pharmacologic Class: 5-Alpha Reductase Inhibitor

Uses For Jalyn

Note: Women of childbearing potential should not use or handle this medicine. Dutasteride can cause birth defects in male fetuses.

Dutasteride and tamsulosin combination is used to treat men who have symptoms of an enlarged prostate gland, which is also known as benign prostatic hyperplasia (BPH). Benign enlargement of the prostate is a problem that can occur in men as they get older. The prostate gland is located below the bladder. When the prostate gland gets larger, certain muscles in the gland get in the way of the tube that drains urine from the bladder. This can cause problems with urinating, such as a need to urinate often, a weak stream when urinating, or a feeling of not being able to empty the bladder completely.

Dutasteride blocks the action of an enzyme called 5-alpha-reductase. This enzyme changes testosterone to another hormone that causes the prostate gland to grow. Dutasteride will cause the size of the prostate to decrease, but the effect lasts only as long as the medicine is taken. If it is stopped, the prostate begins to grow again.

Tamsulosin helps relax the muscles in the prostate gland and the opening of the bladder. This may help increase the flow of urine or decrease symptoms.

This medicine is available only with your doctor's prescription.

Before Using Jalyn

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:

Allergies

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.

Pediatric

Dutasteride and tamsulosin combination is not indicated for use in the pediatric population. Safety and efficacy have not been established.

Geriatric

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of dutasteride and tamsulosin combination in the elderly.

Pregnancy

	Pregnancy Category	Explanation
All Trimesters	X	Studies in animals or pregnant women have demonstrated positive evidence of fetal abnormalities. This drug should not be used in women who are or may become pregnant because the risk clearly outweighs any possible benefit.

Breast Feeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

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 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 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.

• Atazanavir


• Clarithromycin


• Indinavir


• Itraconazole


• Ketoconazole


• Nefazodone


• Nelfinavir


• Ritonavir


• Saquinavir


• Tadalafil


• Telithromycin

Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Acebutolol


• Alprenolol


• Atenolol


• Betaxolol


• Bevantolol


• Bisoprolol


• Bucindolol


• Carteolol


• Carvedilol


• Celiprolol


• Cimetidine


• Ciprofloxacin


• Dilevalol


• Diltiazem


• Esmolol


• Ketoconazole


• Labetalol


• Levobunolol


• Mepindolol


• Metipranolol


• Metoprolol


• Nadolol


• Nebivolol


• Oxprenolol


• Paroxetine


• Penbutolol


• Pindolol


• Propranolol


• Ritonavir


• Sildenafil


• Sotalol


• Talinolol


• Tertatolol


• Timolol


• Vardenafil


• Verapamil

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. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Other Medical Problems

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:

• Allergy to sulfa drugs (such as sulfamethoxazole, sulfasalazine, sulfasoxazole, Azulfidine®, Bactrim®, or Septra®)—Increased allergic reaction in patients with this condition.

• Hypotension (low blood pressure) or


• Postural hypotension (low blood pressure when arising), history of or


• Priapism (painful or prolonged erection of the penis)—Use with caution. May make these conditions worse.

• Liver disease—Use with caution. The effects may be increased because of slower removal of the medicine from the body.

Proper Use of Jalyn

Take this medicine exactly 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 medicine comes with a patient information insert. Read and follow the instructions in the insert carefully. Ask your doctor if you have any questions.

Take the capsule approximately 30 minutes after the same meal each day. Swallow the capsule whole. Do not chew or open it.

Dosing

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.

• For oral dosage form (capsules):
  
  • For benign prostatic hyperplasia:
    
    • Adults—One capsule once a day.
    
    
    • Children—Use is not recommended.
    
    
  
  

Missed Dose

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.

Storage

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.

Precautions While Using Jalyn

It is very important that your doctor check your progress at regular visits to make sure that this medicine is working properly and to check for unwanted effects.

Women and children should not use this medicine. Pregnant women or women who may become pregnant should not handle or touch the capsules. Dutasteride can be absorbed through the skin and can cause birth defects in male fetuses. If a pregnant woman does come in contact with this medicine, the affected area should be washed right away with soap and water, especially if the capsule is broken.

Because this medicine may cause some people to become dizzy or feel faint, 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 are not alert.

Dizziness, lightheadedness, or fainting may occur after you take this medicine, especially when you get up suddenly from a lying or sitting position. Getting up slowly may help with this problem. If you feel dizzy, lie down so you do not faint. Then sit for a few moments before standing to prevent the dizziness from returning.

If you plan to have cataract surgery, tell your eye doctor (ophthalmologist) that you are taking this medicine or that you used this medicine in the previous 9 months. A serious eye problem called Intraoperative Floppy Iris Syndrome (IFIS) has occurred in some patients who were taking this medicine or who had recently taken this medicine when they had cataract surgery.

This medicine may affect the results of the prostate specific antigen (PSA) test, which may be used to detect prostate cancer. Make sure you tell all of your doctors that you are using this medicine.

This medicine will not prevent prostate cancer but may increase your risk of developing high-grade prostate cancer. Tell your doctor if you have concerns about this risk.

You should seek medical attention right away if you experience a prolonged erection while using this medicine. This is an extremely rare unwanted effect that must be treated right away to prevent permanent erectile damage (impotence).

Men who have taken this medicine should not donate blood until 6 months have passed since the last dose. Dutasteride can remain in your blood for a long time and be passed on to a pregnant woman who receives a blood transfusion.

This medicine does not usually affect normal sexual abilities for most men. You may notice that you ejaculate less fluid when you have sex.

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.

Jalyn 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 immediately if any of the following side effects occur:

More common

• Chills


• cold sweats


• confusion


• dizziness, faintness, or lightheadedness when getting up suddenly from a lying or sitting position

Less common

• Chest pain


• cough or hoarseness


• fever


• lower back or side pain


• painful or difficult urination

Incidence not known

• Blistering, flaking, or peeling of the skin


• blurred vision


• difficulty with breathing


• fast, irregular, pounding, or racing heartbeat or pulse


• large, hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or sex organs


• pain or swelling of the treated skin


• painful or prolonged erection of the penis


• shortness of breath


• sweating


• unusual tiredness or weakness

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

• Change or problem with discharge of semen


• decreased interest in sexual intercourse


• dizziness


• enlarged and painful breasts


• inability to have or keep an erection


• loss in sexual ability, desire, drive, or performance

Less common

• Back pain


• body aches or pain


• congestion


• diarrhea


• dryness or soreness of the throat


• headache


• increased cough


• lack or loss of strength


• pain or tenderness around the eyes and cheekbones


• runny nose


• shortness of breath or troubled breathing


• sleepiness or unusual drowsiness


• sleeplessness


• sneezing


• stuffy nose


• tender, swollen glands in the neck


• tightness of the chest or wheezing


• trouble sleeping


• trouble with swallowing


• unable to sleep


• voice changes

Incidence not known

• Constipation


• hives or welts


• itching


• redness of the skin


• skin rash


• vomiting

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: Jalyn side effects (in more detail)

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The use of the Thomson Reuters Healthcare products is at your sole risk. These products are provided "AS IS" and "as available" for use, without warranties of any kind, either express or implied. Thomson Reuters Healthcare and Drugs.com make no representation or warranty as to the accuracy, reliability, timeliness, usefulness or completeness of any of the information contained in the products. Additionally, THOMSON REUTERS HEALTHCARE MAKES NO REPRESENTATION OR WARRANTIES AS TO THE OPINIONS OR OTHER SERVICE OR DATA YOU MAY ACCESS, DOWNLOAD OR USE AS A RESULT OF USE OF THE THOMSON REUTERS HEALTHCARE PRODUCTS. ALL IMPLIED WARRANTIES OF MERCHANTABILITY AND FITNESS FOR A PARTICULAR PURPOSE OR USE ARE HEREBY EXCLUDED. Thomson Reuters Healthcare does not assume any responsibility or risk for your use of the Thomson Reuters Healthcare products.

More Jalyn resources

• Jalyn Side Effects (in more detail)
• Jalyn Dosage
• Jalyn Use in Pregnancy & Breastfeeding
• Jalyn Drug Interactions
• Jalyn Support Group
• 11 Reviews for Jalyn - Add your own review/rating

• Jalyn Prescribing Information (FDA)


• Jalyn MedFacts Consumer Leaflet (Wolters Kluwer)


• Jalyn Consumer Overview

Compare Jalyn with other medications

• Benign Prostatic Hyperplasia

Sinemet 12.5mg / 50mg, 10mg / 100mg, 25mg / 100mg and 25mg / 250mg Tablets

1. Name Of The Medicinal Product

SINEMET^® 12.5 mg/50 mg Tablets

SINEMET^® 10 mg/100 mg Tablets

SINEMET^® Plus 25 mg/100 mg Tablets

SINEMET^® 25 mg/250 mg Tablets

2. Qualitative And Quantitative Composition

Each tablet of 'Sinemet 12.5 mg/50 mg Tablets' contains 13.5 mg carbidopa (equivalent to 12.5 mg of anhydrous carbidopa) and 50 mg levodopa.

Each tablet of 'Sinemet 10 mg/100 mg Tablets' contains 10.8 mg carbidopa (equivalent to 10 mg of anhydrous carbidopa) and 100 mg levodopa.

Each tablet of 'Sinemet Plus 25 mg/100 mg Tablets' contains 27.0 mg carbidopa (equivalent to 25 mg of anhydrous carbidopa) and 100 mg levodopa.

Each tablet of 'Sinemet 25 mg/250 mg Tablets' contains 27.0 mg carbidopa (equivalent to 25 mg of anhydrous carbidopa) and 250 mg levodopa.

3. Pharmaceutical Form

Tablets.

'Sinemet 12.5 mg/50 mg Tablets': yellow, oval-shaped tablets, one side scored and the other marked '520'.

'Sinemet 10 mg/100 mg Tablets': dapple blue, oval-shaped tablets, one side plain and the other scored and marked '647'.

'Sinemet Plus 25 mg/100 mg Tablets ': yellow, oval-shaped tablets, one side plain and the other scored and marked'650'.

'Sinemet 25 mg/250 mg Tablets ': light dapple blue, oval-shaped tablets, one side plain and the other scored and marked '654'.

For excipients see 6.1.

4. Clinical Particulars

4.1 Therapeutic Indications

Antiparkinsonian agent.

For treatment of Parkinson's disease and syndrome.

4.2 Posology And Method Of Administration

To be taken orally.

The optimum daily dosage of 'Sinemet' must be determined by careful titration in each patient.

'Sinemet' Tablets are available in a ratio of 1:4 or 1:10 of carbidopa to levodopa to provide facility for fine dosage titration for each patient.

General Considerations

Studies show that the peripheral dopa-decarboxylase is fully inhibited (saturated) by carbidopa at doses between 70 and 100 mg a day. Patients receiving less than this amount of carbidopa are more likely to experience nausea and vomiting.

Standard antiparkinsonian drugs, other than levodopa alone, may be continued while 'Sinemet' is being administered, although their dosage may have to be adjusted.

Because both therapeutic and adverse effects are seen more rapidly with 'Sinemet' than with levodopa, patients should be carefully monitored during the dosage adjustment period. Involuntary movements, particularly blepharospasm, are a useful early sign of excess dosage in some patients.

Patients not receiving levodopa

Dosage may be best initiated with one tablet of 'Sinemet Plus 25 mg/100 mg' three times a day. This dosage schedule provides 75 mg of carbidopa per day. Dosage may be increased by one tablet of 'Sinemet 12.5 mg/50 mg' or 'Sinemet Plus 25 mg/100 mg' every day or every other day, as necessary, until a dosage equivalent of eight tablets of 'Sinemet Plus 25 mg/100 mg' a day is reached.

If 'Sinemet 10 mg/100 mg Tablets' or 'Sinemet 12.5 mg/50 mg Tablets' are used, dosage may be initiated with one tablet three or four times a day. Titration upward may be required in some patients to achieve optimum dosage of carbidopa. The dosage may be increased by one tablet every day or every other day until a total of eight tablets (two tablets q.d.s.) is reached.

For patients starting with 'Sinemet 25 mg/250 mg Tablets', the initial dose is one-half tablet taken once or twice daily. However, this may not provide the optimal amount of carbidopa needed by many patients. If necessary, add one-half tablet every day or every other day until optimal response is reached.

Response has been observed in one day, and sometimes after one dose. Fully effective doses usually are reached within seven days as compared to weeks or months with levodopa alone.

'Sinemet 12.5 mg/50 mg Tablets' or 'Sinemet 10 mg/100 mg Tablets' may be used to facilitate dosage titration according to the needs of the individual patient.

Patients receiving levodopa

Discontinue levodopa at least 12 hours (24 hours for slow-release preparations) before starting therapy with 'Sinemet'. The easiest way to do this is to give 'Sinemet' as the first morning dose after a night without any levodopa. The dose of 'Sinemet' should be approximately 20% of the previous daily dosage of levodopa.

Patients taking less than 1,500 mg levodopa a day should be started on one tablet of 'Sinemet Plus 25 mg/100 mg' three or four times a day dependent on patient need. The suggested starting dose for most patients taking more than 1,500 mg levodopa a day is one tablet of 'Sinemet 25 mg/250 mg' three or four times a day.

Maintenance

Therapy with 'Sinemet' should be individualised and adjusted gradually according to response. When a greater proportion of carbidopa is required, each tablet of 'Sinemet 10 mg/100 mg' may be replaced with a tablet of 'Sinemet Plus 25 mg/100 mg' or 'Sinemet 12.5 mg/50 mg'.

When more levodopa is required, 'Sinemet 25 mg/250 mg Tablets' should be substituted at a dosage of one tablet three or four times a day. If necessary, the dosage of 'Sinemet 25 mg/250 mg Tablets' may be increased by half to one tablet every other day to a maximum of eight tablets a day. Experience with a total daily dosage greater than 200 mg carbidopa is limited.

Patients receiving levodopa with another decarboxylase inhibitor

When transferring a patient to 'Sinemet' from levodopa combined with another decarboxylase inhibitor, discontinue dosage at least 12 hours before 'Sinemet' is started. Begin with a dosage of 'Sinemet' that will provide the same amount of levodopa as contained in the other levodopa/decarboxylase inhibitor combination.

Patients receiving other antiparkinsonian agents

Current evidence indicates that other antiparkinsonian agents may be continued when 'Sinemet' is introduced, although dosage may have to be adjusted in line with manufacturers recommendations.

Use in children

The safety of 'Sinemet' in patients under 18 years of age has not been established and its use in patients below the age of 18 is not recommended.

Use in the elderly

There is wide experience in the use of this product in elderly patients. The recommendations set out above reflect the clinical data derived from this experience.

4.3 Contraindications

Non-selective monoamine oxidase (MAO) inhibitors are contraindicated for use with 'Sinemet'. These inhibitors must be discontinued at least two weeks before starting 'Sinemet'. 'Sinemet' may be administered concomitantly with the manufacturer's recommended dose of an MAO inhibitor with selectivity for MAO type B (e.g. selegiline hydrochloride). (See 4.5 'Interaction with other medicinal products and other forms of interaction'.)

'Sinemet' is contraindicated in patients with narrow-angle glaucoma and in patients with known hypersensitivity to any component of this medication.

Since levodopa may activate a malignant melanoma, it should not be used in patients with suspicious undiagnosed skin lesions or a history of melanoma.

Use in patients with severe psychoses.

See also 4.6 'Pregnancy and lactation'.

4.4 Special Warnings And Precautions For Use

'Sinemet' is not recommended for the treatment of drug-induced extrapyramidal reactions.

'Sinemet' should be administered cautiously to patients with severe cardiovascular or pulmonary disease, bronchial asthma, renal, hepatic or endocrine disease, or history of peptic ulcer disease (because of the possibility of upper gastro-intestinal haemorrhage).

Care should be exercised when 'Sinemet' is administered to patients with a history of myocardial infarction who have residual atrial nodal, or ventricular arrhythmias. Cardiac function should be monitored with particular care in such patients during the period of initial dosage adjustment.

Levodopa has been associated with somnolence and episodes of sudden sleep onset. Sudden onset of sleep during daily activities, in some cases without awareness or warning signs, has been reported very rarely. Patients must be informed of this and advised to exercise caution while driving or operating machines during treatment with levodopa. Patients who have experienced somnolence and/or an episode of sudden sleep onset must refrain from driving or operating machines. Furthermore a reduction of dosage or termination of therapy may be considered.

All patients should be monitored carefully for the development of mental changes, depression with suicidal tendencies, and other serious antisocial behaviour. Patients with current psychoses should be treated with caution.

Dyskinesias may occur in patients previously treated with levodopa alone because carbidopa permits more levodopa to reach the brain and, thus, more dopamine to be formed. The occurrence of dyskinesias may require dosage reduction.

As with levodopa, 'Sinemet' may cause involuntary movements and mental disturbances. Patients with a history of severe involuntary movements or psychotic episodes when treated with levodopa alone should be observed carefully when 'Sinemet' is substituted. These reactions are thought to be due to increased brain dopamine following administration of levodopa, and use of 'Sinemet' may cause a recurrence. A syndrome resembling the neuroleptic malignant syndrome including muscular rigidity, elevated body temperature, mental changes and increased serum creatine phosphokinase has been reported with the abrupt withdrawal of antiparkinsonian agents. Therefore, any abrupt dosage reduction or withdrawal of 'Sinemet' should be carefully observed, particularly in patients who are also receiving neuroleptics.

Pathological gambling, increased libido and hypersexuality have been reported in patients treated with dopamine agonists for Parkinson's disease.

Concomitant administration of psycho-active drugs such as phenothiazines or butyrophenones should be carried out with caution, and the patient carefully observed for loss of antiparkinsonian effect. Patients with a history of convulsions should be treated with caution.

As with levodopa, periodic evaluation of hepatic, haematopoetic, cardiovascular and renal function are recommended during extended therapy.

Patients with chronic wide-angle glaucoma may be treated cautiously with 'Sinemet', provided the intra-ocular pressure is well controlled and the patient monitored carefully for changes in intra-ocular pressure during therapy.

If general anaesthesia is required, therapy with 'Sinemet' may be continued for as long as the patient is permitted to take fluids and medication by mouth. If therapy has to be stopped temporarily, 'Sinemet' may be restarted as soon as oral medication can be taken at the same daily dosage as before.

Epidemiological studies have shown that patients with Parkinson's disease have a higher risk of developing melanoma than the general population (approximately 2-6 fold higher). It is unclear whether the increased risk observed was due to Parkinson's disease, or other factors such as drugs used to treat Parkinson's disease. Therefore patients and providers are advised to monitor for melanomas on a regular basis when using 'Sinemet' for any indication. Ideally, periodic skin examinations should be performed by appropriately qualified individuals (e.g., dermatologists).

Laboratory Tests

Commonly, levels of blood urea nitrogen, creatinine, and uric acid are lower during administration of 'Sinemet' than with levodopa. Transient abnormalities include elevated levels of blood urea, AST (SGOT), ALT (SGPT), LDH, bilirubin, and alkaline phosphatase.

Decreased haemoglobin, haematocrit, elevated serum glucose and white blood cells, bacteria and blood in the urine have been reported.

Positive Coombs' tests have been reported, both with 'Sinemet' and levodopa alone.

'Sinemet' may cause a false positive result when a dipstick is used to test for urinary ketone; and this reaction is not altered by boiling the urine. The use of glucose oxidase methods may give false negative results for glycosuria.

4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction

Caution should be exercised when the following drugs are administered concomitantly with 'Sinemet'.

Antihypertensive agents

Postural hypotension can occur when 'Sinemet' is added to the treatment of patients already receiving antihypertensive drugs. Dosage adjustment of the antihypertensive agent may be required.

Antidepressants

Rarely, reactions including hypertension and dyskinesia have been reported with the concomitant use of tricyclic antidepressants. (See first paragraph of 4.3 'Contraindications' for patients receiving MAOIs).

Anticholinergics

Anticholinergics may affect the absorption and thus the patient's response.

Iron

Studies demonstrate a decrease in the bioavailability of carbidopa and/or levodopa when it is ingested with ferrous sulphate or ferrous gluconate.

Other drugs

To date there has been no indication of interactions that would preclude concurrent use of standard antiparkinsonian drugs.

Dopamine D₂ receptor antagonists (e.g. phenothiazines, butyrophenones, and risperidone) and isoniazid, may reduce the therapeutic effects of levodopa. The beneficial effects of levodopa in Parkinson's disease have been reported to be reversed by phenytoin and papaverine. Patients taking these drugs with 'Sinemet' should be carefully observed for loss of therapeutic response.

Concomitant therapy with selegiline and carbidopa-levodopa may be associated with severe orthostatic hypotension not attributable to carbidopa-levodopa alone (See 4.3 'Contraindications')

Since levodopa competes with certain amino acids, the absorption of 'Sinemet' may be impaired in some patients on a high protein diet.

The effect of simultaneous administration of antacids with 'Sinemet' on the bioavailability of levodopa has not been studied.

'Sinemet' may be given to patients with Parkinson's disease and syndrome who are taking vitamin preparations that contain pyridoxine hydrochloride (Vitamin B6).

4.6 Pregnancy And Lactation

Pregnancy

Although the effects of 'Sinemet' on human pregnancy are unknown, both levodopa and combinations of carbidopa and levodopa have caused visceral and skeletal malformations in rabbits. Therefore, the use of 'Sinemet' in women of childbearing potential requires that the anticipated benefits of the drug be weighed against possible hazards should pregnancy occur.

Breast-feeding mothers

It is not known whether carbidopa is excreted in human milk. In a study of one nursing mother with Parkinson's disease, excretion of levodopa in human breast milk was reported. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in infants, a decision should be made whether to discontinue breast-feeding or discontinue the use of 'Sinemet', taking into account the importance of the drug to the mother.

4.7 Effects On Ability To Drive And Use Machines

Individual responses to medication may vary and certain side effects that have been reported with 'Sinemet' may affect some patients' ability to drive or operate machinery. Patients treated with levodopa and presenting with somnolence and/or sudden sleep episodes must be informed to refrain from driving or engaging in activities where impaired alertness may put themselves or others at risk of serious injury or death (e.g. operating machines), until such recurrent episodes and somnolence have resolved (see also section 4.4 'Special warnings and precautions for use').

4.8 Undesirable Effects

Side effects that occur frequently with 'Sinemet' are those due to the central neuropharmacological activity of dopamine. These reactions can usually be diminished by dosage reduction. The most common are dyskinesias including choreiform, dystonic and other involuntary movements and nausea. Muscle twitching and blepharospasm may be taken as early signs to consider dosage reduction.

Other side effects reported in clinical trials or in post-marketing experience include:

Body as a whole: syncope, chest pain, anorexia.

Cardiovascular: cardiac irregularities and/or palpitations, orthostatic effects including hypotensive episodes, hypertension, phlebitis.

Gastro-intestinal: vomiting, gastro-intestinal bleeding, development of duodenal ulcer, diarrhoea, dark saliva.

Haemotologic: leucopenia, haemolytic and non-haemolytic anaemia, thrombocytopenia, agranulocytosis.

Hypersensitivity: angioedema, urticaria, pruritus, Henoch-Schonlein purpura.

Nervous System/Psychiatric: neuroleptic malignant syndrome (see 4.3 'Contraindications'), bradykinetic episodes (the “on-off” phenomenon), dizziness, paraesthesia, psychotic episodes including delusions, hallucinations and paranoid ideation, depression with or without development of suicidal tendencies, dementia, dream abnormalities, agitation, confusion, increased libido. Levodopa is associated with somnolence and has been associated very rarely with excessive daytime somnolence and sudden sleep onset episodes.

Respiratory: dyspnoea.

Skin: alopecia, rash, dark sweat.

Urogenital: dark urine.

Rarely convulsions have occurred; however, a causal relationship with 'Sinemet' has not been established.

Other side effects that have been reported with levodopa or levodopa/carbidopa combinations and may be potential side effects with 'Sinemet' include:

Gastro-intestinal: dyspepsia, dry mouth, bitter taste, sialorrhoea, dysphagia, bruxism, hiccups, abdominal pain and distress, constipation, flatulence, burning sensation of the tongue.

Metabolic: weight gain or loss, oedema.

Nervous System/Psychiatric: asthenia, decreased mental acuity, disorientation, ataxia, numbness, increased hand tremor, muscle cramp, trismus, activation of latent Horner's syndrome, insomnia, anxiety, euphoria, falling and gait abnormalities.

Patients treated with dopamine agonists for treatment of Parkinson's disease, especially at high doses, have been reported as exhibiting signs of pathological gambling, increased libido and hypersexuality, generally reversible upon reduction of the dose or treatment discontinuation.

Skin: flushing, increased sweating,

Special senses: diplopia, blurred vision, dilated pupils, oculogyric crises.

Urogenital: urinary retention, urinary incontinence, priapism.

Miscellaneous: weakness, faintness, fatigue, headache, hoarseness, malaise, hot flushes, sense of stimulation, bizarre breathing patterns, malignant melanoma (see 4.3 'Contraindications').

4.9 Overdose

Treatment

Management of acute overdosage with 'Sinemet' is basically the same as management of acute overdosage with levodopa; however pyridoxine is not effective in reversing the actions of 'Sinemet'. ECG monitoring should be instituted, and the patient carefully observed for the possible development of arrhythmias; if required, appropriate anti-arrhythmic therapy should be given. The possibility that the patient may have taken other drugs as well as 'Sinemet' should be taken into consideration. To date, no experience has been reported with dialysis, and hence its value in the treatment of overdosage is not known.

The terminal half-life of levodopa is about two hours in the presence of carbidopa.

5. Pharmacological Properties

5.1 Pharmacodynamic Properties

Levodopa is a precursor of dopamine, and is given as replacement therapy in Parkinson's disease.

Carbidopa is a peripheral dopa decarboxylase inhibitor. It prevents metabolism of levodopa to dopamine in the peripheral circulation, ensuring that a higher proportion of the dose reaches the brain, where dopamine acts. A lower dose of levodopa can be used, reducing the incidence and severity of side effects.

'Sinemet' is useful in relieving many of the symptoms of parkinsonism, particularly rigidity and bradykinesia. It is frequently helpful in the management of tremor, dysphagia, sialorrhoea, and postural instability associated with Parkinson's disease and syndrome.

When response to levodopa alone is irregular, and signs and symptoms of Parkinson's disease are not controlled evenly throughout the day, substitution of 'Sinemet' usually reduces fluctuations in response. By reducing some of the adverse reactions produced by levodopa alone, 'Sinemet' permits more patients to obtain adequate relief from the symptoms of Parkinson's disease.

5.2 Pharmacokinetic Properties

Following oral dosing levodopa, in the absence of decarboxylase inhibitor, is rapidly but variably absorbed from the gastro-intestinal tract. It has a plasma half life of about 1 hour and is mainly converted by decarboxylation to dopamine, a proportion of which is converted to noradrenaline. Up to 30 % is converted to 3-O-methyldopa which has a half life of 9 to 22 hours. About 80 % of levodopa is excreted in the urine within 24 hours mainly as homovanillic acid and dihydroxyphenylactic acid. Less than 1% is excreted unchanged.

Once in the circulation it competes with other neutral amino acids for transport across the blood brain barrier. Once it has entered the striatal neurones it is decarboxylated to dopamine, stored and released from presynaptic neurones. Because levodopa is so rapidly decarboxylated in the gastro-intestinal tract and the liver, very little unchanged drug is available for transport into the brain. The peripheral decarboxylation reduces the therapeutic effectiveness of levodopa but is responsible for many of its side effects. For this reason levodopa is usually administered together with a peripheral decarboxylase inhibitor such as carbidopa, so that lower doses may be given to achieve the same therapeutic effect.

Carbidopa in the absence of levodopa, is rapidly but incompletely absorbed from the gastrointestinal tract following oral dosing. Following an oral dose approximately 50% is recorded in the urine, with about 3% of this as unchanged drug. It does not cross the blood brain barrier but crosses the placenta and is excreted in breast milk. Turnover of the drug is rapid and virtually all unchanged drug appears in the urine within 7 hours.

Carbidopa inhibits the peripheral decarboxylation of levodopa to dopamine but as it does not cross the blood brain barrier, effective brain levels of dopamine get produced with lower levels of levodopa therapy reducing the peripheral side effects, noticeably nausea and vomiting and cardiac arrhythmias.

5.3 Preclinical Safety Data

'Sinemet' is well established in medical use. Preclinical data is broadly consistent with clinical experience. (For reproductive toxicity, see section 4.6 'Pregnancy and Lactation'.)

6. Pharmaceutical Particulars

6.1 List Of Excipients

'Sinemet 12.5 mg/50 mg Tablets' and 'Sinemet Plus 25 mg/100 mg Tablets' contain quinoline yellow (E104), maize starch, pregelatinised maize starch, microcrystalline cellulose, magnesium stearate.

'Sinemet 10 mg/100 mg Tablets' and 'Sinemet 25 mg/250 mg Tablets' contain indigo carmine (E132), maize starch pregelatinised maize starch, microcrystalline cellulose, magnesium stearate .

6.2 Incompatibilities

Not applicable.

6.3 Shelf Life

36 months

6.4 Special Precautions For Storage

Do not store above 25°C. Store in the original package in order to protect from light.

6.5 Nature And Contents Of Container

PVC/AL blister packs of 30 or 90 tablets.

Amber glass bottles or HDPE bottles of 84 or 100 tablets

6.6 Special Precautions For Disposal And Other Handling

Not applicable.

7. Marketing Authorisation Holder

Merck Sharp & Dohme Limited

Hertford Road

Hoddesdon

Hertfordshire EN11 9BU, UK.

8. Marketing Authorisation Number(S)

Sinemet 12.5 mg/50 mg Tablets PL 0025/0226

Sinemet 10 mg/100 mg Tablets PL 0025/0084

Sinemet Plus 25 mg/100 mg Tablets PL 0025/0150

Sinemet 25 mg/250 mg Tablets PL 0025/0085

9. Date Of First Authorisation/Renewal Of The Authorisation

Sinemet 12.5 mg/50 mg Tablets 11 February 1988 / 16 April 2008

Sinemet 10 mg/100 mg Tablets 23 October 1973 / 16 April 2008

Sinemet Plus 25 mg/100 mg Tablets 11 June 1981 / 16 April 2008

Sinemet 25 mg/250 mg Tablets 23 October 1973 / 16 April 2008

10. Date Of Revision Of The Text

November 2009

LEGAL CATEGORY

POM

® Registered trademark of Merck & Co, Inc., Whitehouse Station, New Jersey, USA.

© Merck Sharp & Dohme Limited 2009. All rights reserved.

SPC.SEM.09.UK.3101

Aygestin Oral, Implantation, Parenteral

Generic Name: progestin contraceptives (Oral route, Parenteral route)

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 Aygestin

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 Aygestin

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 this medicine for 2 years or longer.

Geriatric

This medicine 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

This section provides information on the proper use of a number of products that contain progestin contraceptives. It may not be specific to Aygestin. Please read with care.

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 this medicine.

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 this medicine 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 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 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 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 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.
    
    
  
  

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 Aygestin

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 this medicine 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.

Aygestin 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

Less common

• Mental depression


• skin rash


• unexpected or increased flow of breast milk

Incidence not known - for patients taking Depo-Provera Contraceptive Injection

• 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

Less common

• 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 this medicine, 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.

The information contained in the Thomson Reuters Micromedex products as delivered by Drugs.com is intended as an educational aid only. It is not intended as medical advice for individual conditions or treatment. It is not a substitute for a medical exam, nor does it replace the need for services provided by medical professionals. Talk to your doctor, nurse or pharmacist before taking any prescription or over the counter drugs (including any herbal medicines or supplements) or following any treatment or regimen. Only your doctor, nurse, or pharmacist can provide you with advice on what is safe and effective for you.

The use of the Thomson Reuters Healthcare products is at your sole risk. These products are provided "AS IS" and "as available" for use, without warranties of any kind, either express or implied. Thomson Reuters Healthcare and Drugs.com make no representation or warranty as to the accuracy, reliability, timeliness, usefulness or completeness of any of the information contained in the products. Additionally, THOMSON REUTERS HEALTHCARE MAKES NO REPRESENTATION OR WARRANTIES AS TO THE OPINIONS OR OTHER SERVICE OR DATA YOU MAY ACCESS, DOWNLOAD OR USE AS A RESULT OF USE OF THE THOMSON REUTERS HEALTHCARE PRODUCTS. ALL IMPLIED WARRANTIES OF MERCHANTABILITY AND FITNESS FOR A PARTICULAR PURPOSE OR USE ARE HEREBY EXCLUDED. Thomson Reuters Healthcare does not assume any responsibility or risk for your use of the Thomson Reuters Healthcare products.

Jakafi

Pronunciation: RUX-oh-LI-ti-nib
Generic Name: Ruxolitinib
Brand Name: Jakafi

Jakafi is used for:

Treating certain types of myelofibrosis. It may also be used for other conditions as determined by your doctor.

Jakafi is a kinase inhibitor. It works by blocking certain substances (JAK1 and JAK2) that are involved in myelofibrosis.

Do NOT use Jakafi if:

• you are allergic to any ingredient in Jakafi


• you have a serious infection


• you have certain severe kidney problems

Contact your doctor or health care provider right away if any of these apply to you.

Before using Jakafi:

Some medical conditions may interact with Jakafi. 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 anemia, low blood platelet levels, or low white blood cell counts


• if you have an infection (bacterial, viral, fungal, or mycobacterial) or a history of infection that keeps coming back


• if you are on dialysis or have a history of liver or kidney problems


• if you are not able to take Jakafi by mouth

Some MEDICINES MAY INTERACT with Jakafi. Tell your health care provider if you are taking any other medicines, especially any of the following:

• Azole antifungals (eg, itraconazole, ketoconazole), conivaptan, macrolide antibiotics (eg, clarithromycin), mibefradil, nefazodone, protease inhibitors (eg, boceprevir, ritonavir), or telithromycin because they may increase the risk of Jakafi's side effects


• Rifampin because it may decrease Jakafi's effectiveness

This may not be a complete list of all interactions that may occur. Ask your health care provider if Jakafi 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 Jakafi:

Use Jakafi as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• An extra patient leaflet is available with Jakafi. Talk to your pharmacist if you have questions about this information.


• Take Jakafi by mouth with or without food.


• Do not eat grapefruit or drink grapefruit juice while you use Jakafi without first checking with your doctor.


• Do not suddenly stop taking Jakafi. If you need to stop Jakafi, your doctor may gradually lower your dose.


• Continue to take Jakafi even if you feel well. Do not miss any doses.


• If you miss a dose of Jakafi, 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 Jakafi.

Important safety information:

• Jakafi may cause dizziness. This effect may be worse if you take it with alcohol or certain medicines. Use Jakafi with caution. Do not drive or perform other possibly unsafe tasks until you know how you react to it.


• Do not change your dose or stop taking Jakafi without checking with your doctor.


• If you are on dialysis, do not take your dose of Jakafi before your dialysis treatment. Take your dose after your dialysis treatment is finished. Check with your doctor if you have any questions.


• Jakafi may lower the ability of your body to fight infection, including shingles. Avoid contact with people who have colds or infections. Tell your doctor if you notice signs of infection like fever, sore throat, rash, chills, or increased or painful urination. Symptoms of shingles may include painful skin rash or blisters.


• Jakafi may reduce the number of clot-forming cells (platelets) in your blood. Avoid activities that may cause bruising or injury. Tell your doctor if you have unusual bruising or bleeding. Tell your doctor if you have dark, tarry, or bloody stools.


• Jakafi is not a cure for myelofibrosis. Signs and symptoms are expected to return if Jakafi is stopped. Discuss any questions or concerns with your doctor.


• Lab tests, including complete blood cell counts, may be performed while you use Jakafi. These tests may be used to monitor your condition or check for side effects. Be sure to keep all doctor and lab appointments.


• Jakafi should be used with extreme caution in CHILDREN; safety and effectiveness in 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 Jakafi while you are pregnant. It is not known if Jakafi is found in breast milk. Do not breast-feed while taking Jakafi.

Possible side effects of Jakafi:

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:

Dizziness; gas; headache; weight gain.

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); painful skin rash or blisters; shortness of breath; symptoms of infection (eg, fever, chills, persistent sore throat, increased or painful urination, nausea or vomiting); unusual bruising or bleeding; unusual tiredness or weakness.

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.

See also: Jakafi side effects (in more detail)

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 symptoms of infection (eg, fever, chills, persistent sore throat, increased or painful urination); unusual bruising or bleeding; unusual tiredness or weakness.

Proper storage of Jakafi:

Store Jakafi at room temperature, between 68 and 77 degrees F (20 and 25 degrees C). Brief storage at temperatures between 59 and 86 degrees F (15 and 30 degrees C) is permitted. Store away from heat, moisture, and light. Do not store in the bathroom. Keep Jakafi out of the reach of children and away from pets.

General information:

• If you have any questions about Jakafi, please talk with your doctor, pharmacist, or other health care provider.


• Jakafi 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 Jakafi. 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.

More Jakafi resources

• Jakafi Side Effects (in more detail)
• Jakafi Use in Pregnancy & Breastfeeding
• Drug Images
• Jakafi Drug Interactions
• Jakafi Support Group
• 0 Reviews for Jakafi - Add your own review/rating

• Jakafi Prescribing Information (FDA)


• Jakafi Advanced Consumer (Micromedex) - Includes Dosage Information


• Jakafi Consumer Overview


• Ruxolitinib Professional Patient Advice (Wolters Kluwer)

Compare Jakafi with other medications

• Myelofibrosis
• Myeloproliferative Disorders

ifosfamide Intravenous

eye-FOS-fa-mide

Intravenous route(Powder for Solution)

Urotoxic side effects, especially hemorrhagic cystitis, as well as CNS toxicities such as confusion and coma have been associated with the use of ifosfamide. These side effects may require cessation of ifosfamide therapy. Severe myelosuppression has also been reported .

Commonly used brand name(s)

In the U.S.

• Ifex

Available Dosage Forms:

• Solution


• Powder for Solution

Therapeutic Class: Antineoplastic Agent

Pharmacologic Class: Alkylating Agent

Chemical Class: Nitrogen Mustard

Uses For ifosfamide

Ifosfamide belongs to the group of medicines called alkylating agents. It is used to treat cancer of the testicles as well as some other kinds of cancer. Another medicine, called mesna, is usually given along with ifosfamide to prevent bladder problems that can be caused by ifosfamide.

Ifosfamide interferes with the growth of cancer cells, which are eventually destroyed. Since the growth of normal body cells may also be affected by ifosfamide, other effects will also occur. Some of these may be serious and must be reported to your doctor. Other effects, like hair loss, may not be serious but may cause concern. Some effects may not occur until months or years after the medicine is used.

Before you begin treatment with ifosfamide, you and your doctor should talk about the good ifosfamide will do as well as the risks of using it.

Ifosfamide is to be administered only by or under the immediate supervision of your doctor.

Once a medicine has been approved for marketing for a certain use, experience may show that it is also useful for other medical problems. Although these uses are not included in product labeling, ifosfamide is used in certain patients with the following medical conditions:

• Acute lymphocytic leukemia (a type of cancer of the blood)


• Cancer of the bladder


• Cancer of the bone (including Ewing's sarcoma)


• Cancer of the breast


• Cancer of the cervix


• Cancer of the endometrium


• Cancers of the head and neck


• Cancer of the lung


• Cancer of the ovaries


• Lymphomas


• Neuroblastoma (a certain type of brain cancer)


• Thymoma and other cancer of the thymus (a small organ beneath the breastbone)


• Tumors in the ovaries


• Wilms' tumor (a cancer of the kidneys occurring mainly in children)

Before Using ifosfamide

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 ifosfamide, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to ifosfamide 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

Although there is no specific information comparing use of ifosfamide in children with use in other age groups, ifosfamide is not expected to cause different side effects or problems in children than it does in adults.

Geriatric

Many medicines have not been studied specifically in older people. Therefore, it may not be known whether they work exactly the same way they do in younger adults or if they cause different side effects or problems in older people. There is no specific information comparing use of ifosfamide in the elderly with use in other age groups.

Pregnancy

	Pregnancy Category	Explanation
All Trimesters	D	Studies in pregnant women have demonstrated a risk to the fetus. However, the benefits of therapy in a life threatening situation or a serious disease, may outweigh the potential risk.

Breast Feeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

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 ifosfamide, 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 ifosfamide 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.

• Rotavirus Vaccine, Live

Using ifosfamide 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.

• Adenovirus Vaccine Type 4, Live


• Adenovirus Vaccine Type 7, Live


• Aprepitant


• Bacillus of Calmette and Guerin Vaccine, Live


• Fosaprepitant


• Influenza Virus Vaccine, Live


• Measles Virus Vaccine, Live


• Mumps Virus Vaccine, Live


• Rotavirus Vaccine, Live


• Rubella Virus Vaccine, Live


• Smallpox Vaccine


• Typhoid Vaccine


• Varicella Virus Vaccine


• Yellow Fever Vaccine

Using ifosfamide with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Warfarin

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 ifosfamide. Make sure you tell your doctor if you have any other medical problems, especially:

• Chickenpox (including recent exposure) or


• Herpes zoster (shingles)—Risk of severe disease affecting other parts of the body

• Infection—Ifosfamide can decrease your body's ability to fight infection

• Kidney disease—Effects may be increased because of slower removal of ifosfamide from the body

• Liver disease—Effects may be increased or decreased because the liver both makes ifosfamide work and removes it from the body

Proper Use of ifosfamide

Ifosfamide is sometimes given together with certain other medicines. If you are using a combination of medicines, make sure that you take each one at the proper time and do not mix them. Ask your health care professional to help you plan a way to remember to take your medicines at the right times.

While you are receiving ifosfamide, it is important that you drink extra fluids so that you will pass more urine. Also, empty your bladder frequently, including at least once during the night. This will help prevent kidney and bladder problems and keep your kidneys working well. Ifosfamide passes from the body in the urine. If too much of it appears in the urine or if the urine stays in the bladder too long, it can cause dangerous irritation. Follow your doctor's instructions carefully about how much fluid to drink every day. Some patients may have to drink up to 7 to 12 cups (3 quarts) of fluid a day.

Ifosfamide often causes nausea and vomiting. However, it is very important that you continue to receive the medicine even if you begin to feel ill. Ask your health care professional for ways to lessen these effects.

Dosing

The dose of ifosfamide 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 ifosfamide. 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.

Precautions While Using ifosfamide

It is very important that your doctor check your progress at regular visits to make sure that ifosfamide is working properly and to check for unwanted effects.

While you are being treated with ifosfamide, and after you stop treatment with it, do not have any immunizations (vaccinations) without your doctor's approval. Ifosfamide may lower your body's resistance and there is a chance you might get the infection the immunization is meant to prevent. In addition, other persons living in your house should not take oral polio vaccine since there is a chance they could pass the polio virus on to you. Also, avoid persons who have taken oral polio vaccine within the past several months. Do not get close to them, and do not stay in the same room with them for very long. If you cannot take these precautions, you should consider wearing a protective face mask that covers the nose and mouth.

Ifosfamide can temporarily lower the number of white blood cells in your blood, increasing the chance of getting an infection. It can also lower the number of platelets, which are necessary for proper blood clotting. If this occurs, there are certain precautions you can take to reduce the risk of infection or bleeding:

• If you can, avoid people with infections. Check with your doctor immediately if you think you are getting an infection or if you get a fever or chills, cough or hoarseness, lower back or side pain, or have painful or difficult urination.


• Check with your doctor immediately if you notice any unusual bleeding or bruising; black, tarry stools; blood in urine or stools; or pinpoint red spots on your skin.


• Be careful when using a regular toothbrush, dental floss, or toothpick. Your medical doctor, dentist, or nurse may recommend other ways to clean your teeth and gums. Check with your medical doctor before having any dental work done.


• Do not touch your eyes or the inside of your nose unless you have just washed your hands and have not touched anything else in the meantime.


• Be careful not to cut yourself when you are using sharp objects such as a safety razor or fingernail or toenail cutters.


• Avoid contact sports or other situations where bruising or injury could occur.

ifosfamide Side Effects

Along with their needed effects, medicines like ifosfamide can sometimes cause unwanted effects such as blood problems, loss of hair, and problems with the bladder. These and others are described below. Also, because of the way these medicines act on the body, there is a chance that they might cause other unwanted effects that may not occur until months or years after the medicine is used. These may include certain types of cancer, such as leukemia. Discuss these possible effects with your doctor.

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:

More common

• Blood in urine


• frequent urination


• painful urination

Less common

• Cough or hoarseness accompanied by fever or chills


• fever or chills


• lower back or side pain accompanied by fever or chills

Rare

• Black, tarry stools


• blood in stools


• pinpoint red spots on skin


• unusual bleeding or bruising

Check with your doctor as soon as possible if any of the following side effects occur:

More common

• Agitation


• confusion


• hallucinations (seeing, hearing, or feeling things that are not there)


• unusual tiredness

Less common

• Dizziness


• redness, swelling, or pain at place of injection

Rare

• Convulsions (seizures)


• cough or shortness of breath


• sores in mouth and on lips

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

• Nausea and vomiting

Ifosfamide often causes a temporary loss of hair. After treatment has ended, normal hair growth should return.

After you stop using ifosfamide, it may still produce some side effects that need attention. During this period of time, check with your doctor immediately if you notice the following side effects:

• Blood in urine

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: ifosfamide Intravenous side effects (in more detail)

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More ifosfamide Intravenous resources

• Ifosfamide Intravenous Side Effects (in more detail)
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