Triptorelin Pamoate

Class: Antineoplastic Agents
VA Class: AN500
Chemical Name: 6-d-Tryptophan luteinizing hormone-releasing factor (pig)
Molecular Formula: C₆₄H₈₂N₁₈O₁₃
CAS Number: 57773-63-4
Brands: Trelstar

Special Alerts:

[Posted 10/20/2010] ISSUE: Gonadotropin-Releasing Hormone (GnRH) agonists will have new safety information added to the Warnings and Precautions section of the drug labels. This new information warns about increased risk of diabetes and certain cardiovascular diseases (heart attack, sudden cardiac death, stroke) in men receiving these medications for the treatment of prostate cancer.

BACKGROUND: GnRH agonists are approved to treat the symptoms (palliative treatment) of advanced prostate cancer. The benefits of GnRH agonist use for earlier stages of prostate cancer that have not spread (non-metastatic prostate cancer) have not been established. FDA’s notification to manufacturers of GnRH agonists to add this safety information is based on the Agency’s review of several published studies. Most of the studies reviewed by FDA reported small but statistically significant increased risks of diabetes and/or cardiovascular events in patients receiving GnRH agonists.

RECOMMENDATIONS: Healthcare professionals should evaluate patients for risk factors for these diseases and carefully weigh the benefits and risks of using GnRH agonists before determining appropriate treatment for prostate cancer. Patients who are receiving treatment with GnRH agonists should undergo periodic monitoring of blood glucose and/or glycosylated hemoglobin (HbA1c). Healthcare professionals should also monitor patients for signs and symptoms suggestive of development of cardiovascular disease and manage according to current clinical practice. For more information visit the FDA website at: and .

[Posted 05/03/2010] FDA notified healthcare professionals and patients of FDA’s preliminary and ongoing review which suggests an increase in the risk of diabetes and certain cardiovascular diseases in men treated with GnRH agonists, drugs that suppress the production of testosterone, a hormone that is involved in the growth of prostate cancer.

Most of the studies reviewed by FDA reported small, but statistically significant increased risks of diabetes and/or cardiovascular events in patients receiving GnRH agonists. FDA’s review is ongoing and the agency has not made any conclusions about GnRH agonists and whether they increase the risk of diabetes and cardiovascular disease in patients receiving these medications for prostate cancer.

Healthcare professionals and patients should be aware of these potential safety issues and carefully weigh the benefits and risks of GnRH agonists when determining treatment choices. FDA recommends that patients receiving GnRH agonists should be monitored for development of diabetes and cardiovascular disease. Patients should not stop their treatment with GnRH agonists unless told to do so by their healthcare professional.

Some GnRH agonists are also used in women and in children for other indications than those above. There are no known comparable studies that have evaluated the risk of diabetes and heart disease in women and children taking GnRH agonists. For more information visit the FDA website at: and .

Introduction

Antineoplastic agent; synthetic decapeptide analog of gonadotropin-releasing hormone (GnRH, luteinizing hormone-releasing hormone, gonadorelin);^{1 7} structurally related to leuprolide and goserelin.^{1 2 3 4 6 7}

Uses for Triptorelin Pamoate

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

Prostate Cancer

Palliative treatment of advanced prostate cancer; considered alternative therapy when orchiectomy or estrogen therapy is not appropriate or is unacceptable to the patient.^{1 7}

Triptorelin Pamoate Dosage and Administration

Administration

IM Administration

Administer by IM injection once monthly (every 28 days) as a depot 1-month formulation or every 84 days (12 weeks) as a long-acting 3-month formulation.^{1 7}

Inject IM into buttock; rotate injection sites periodically.^{1 7}

Administer under the supervision of a qualified clinician.^{1 7}

Reconstitution

Reconstitute powder just prior to administration.^{1 7} Discard suspension if not used immediately after reconstitution.^{1 7}

Using a syringe with 20-gauge needle, add 2 mL of sterile water for injection to vial containing the powder (1- or 3-month formulation); do not reconstitute with other diluents.^{1 7} Shake well to disperse particles and obtain a uniform, milky suspension.^{1 7}

If using the single-dose delivery system, add contents of the prefilled syringe (2 mL of sterile water for injection) to vial containing the powder according to the manufacturer’s instructions.^{1 7} Mix well.^{1 7}

Withdraw entire contents of vial and use immediately.^{1 7}

Dosage

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

Available as triptorelin pamoate; dosage is expressed in terms of triptorelin.^{1 7}

Adults

Prostate Cancer

IM

3.75 mg every 28 days (monthly) as the 1-month formulation or 11.25 mg every 84 days (12 weeks) as the 3-month formulation.^{1 7}

Special Populations

Hepatic Impairment

Potential need for dosage adjustment not determined.¹

Renal Impairment

Potential need for dosage adjustment not determined.¹

Cautions for Triptorelin Pamoate

Contraindications

• 
  

  Known hypersensitivity to triptorelin or any other ingredient in the formulation, other GnRH agonists, or GnRH.^{1 7}

  
  


• 
  

  Known or suspected pregnancy.^{1 7}

  
  

Warnings/Precautions

Warnings

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

Endocrine Effects

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

Possible worsening of signs and/or symptoms of prostate cancer and/or development of new manifestations (e.g., bone pain, neuropathy, hematuria, urethral or bladder outlet obstruction) due to increases in serum testosterone concentrations during initial weeks of therapy.^{1 2 3 5 7}

Possible spinal cord compression contributing to paralysis; possibly fatal.^{1 2 5 7}

Increased risk of neurologic and/or genitourinary complications during initial therapy in patients with prostate cancer and metastatic vertebral lesions and/or urinary tract obstruction.^{1 7} Observe such patients closely during initial weeks of therapy.^{1 5 7}

If spinal cord compression or renal impairment develops, institute standard treatment of these complications; consider immediate orchiectomy in extreme cases.^{1 7}

Sensitivity Reactions

Hypersensitivity Reactions

Anaphylactic shock and angioedema reported rarely.^{1 7} If such reactions occur, discontinue immediately and provide supportive and symptomatic care.^{1 7}

Major Toxicities

Pituitary Apoplexy

Pituitary apoplexy, a clinical syndrome resulting from infarction of the pituitary gland, reported rarely.^{1 7} Most cases occur within 2 weeks of the first dose, sometimes within the first hour.^{1 7} If manifestations occur (e.g., sudden headache, vomiting, visual changes, ophthalmoplegia, altered mental status, sometimes cardiovascular collapse), immediate medical attention required.^{1 7} In most cases, pituitary adenoma diagnosed.¹

General Precautions

Laboratory Monitoring

Periodically determine serum testosterone and prostate-specific antigen concentrations to monitor therapeutic response.^{1 7}

Specific Populations

Pregnancy

Category X.^{1 7} (See Contraindications under Cautions.)

Lactation

Not known whether distributed into milk; not recommended for use in nursing women.^{1 7}

Pediatric Use

Safety and efficacy not established in children.^{1 7}

Geriatric Use

Studies conducted principally in patients ≥65 years of age, since prostate cancer occurs mainly in an older patient population.^{1 7}

Common Adverse Effects

Temporary worsening of disease manifestations, hot flushes (flashes), skeletal pain, impotence, headache, pain at injection site, leg pain and edema, dysuria, hypertension.^{1 7}

Also observed with 3-month formulation: decreased hemoglobin and erythrocyte counts, increased BUN, increased serum concentrations of glucose, AST, ALT, and alkaline phosphatase.⁷

Interactions for Triptorelin Pamoate

Metabolism unlikely to involve CYP enzymes; effect of triptorelin on other drug-metabolizing enzymes unknown.⁷

Drugs That Induce Hyperprolactinemia

Potential pharmacologic interaction (possible decrease in triptorelin efficacy due to decreased number of GnRH receptors) with drugs such as antipsychotic agents, methyldopa, metoclopramide, and reserpine.^{1 6 7}

Triptorelin Pamoate Pharmacokinetics

Absorption

Bioavailability

Not active when administered orally.^{1 7}

Following IM administration as Trelstar Depot or Trelstar LA, peak plasma concentrations usually are attained within 1 or 3 hours, respectively.^{1 7}

Duration

Following IM injection of Trelstar Depot or Trelstar LA in males, therapeutic plasma concentrations persist for 1 or 3 months, respectively.^{1 7}

Distribution

Extent

Not known whether triptorelin is distributed into milk.^{1 7}

Plasma Protein Binding

No evidence that triptorelin binds to plasma proteins.^{1 7}

Elimination

Metabolism

Metabolism is unknown; involvement of CYP enzymes is unlikely.^{1 7} No metabolites identified to date.^{1 7}

Elimination Route

Hepatic and renal elimination.^{1 7}

Half-life

Approximately 3 hours.^{1 7}

Special Populations

In males with hepatic impairment or moderate or severe renal impairment, AUC increased 2- to 4-fold compared with healthy males.^{1 7}

Stability

Storage

Parenteral

Powder for Injection

20–25°C (may be exposed to 15–30°C).^{1 7} Do not freeze.⁷

Discard suspension if not used immediately after reconstitution.^{1 7}

ActionsActions

• 
  

  Potent inhibitor of gonadotropin secretion when given continuously in therapeutic doses; greater activity than naturally occurring GnRH.^{1 7}

  
  


• 
  

  Transient surge in circulating levels of LH, FSH, testosterone, and estradiol observed after initial administration.^{1 7} Sustained decreases in LH and FSH secretion and reduced testicular and ovarian steroidogenesis observed following chronic, continuous administration (generally 2–4 weeks after initiation of therapy).^{1 4 7}

  
  


• 
  

  Reduction of serum testosterone in males comparable to effects achieved after surgical castration; results in inactivation of physiologic functions and tissues dependent on testosterone.^{1 2 4 7} These effects usually are reversible after cessation of therapy.^{1 7}

  
  

Advice to Patients

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

• 
  

  Risk of worsening manifestations of prostate cancer during initial weeks of therapy.^{1 7}

  
  


• 
  

  Importance of promptly reporting weakness or paresthesia of lower limbs and/or worsening of urinary signs and symptoms to clinicians.⁶

  
  


• 
  

  Importance of promptly reporting sudden onset of headache, vomiting, or visual changes to clinicians.^{1 7}

  
  


• 
  

  Risk of anaphylactoid and other sensitivity reactions.^{1 7}

  
  


• 
  

  Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.^{1 7}

  
  


• 
  

  Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.^{1 7} If used during pregnancy, apprise of potential fetal hazard.⁷

  
  


• 
  

  Importance of informing patients of other important precautionary information.¹ (See Cautions.)

  
  

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Triptorelin Pamoate

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Parenteral	For injection, for IM use only	3.75 mg (of triptorelin)	Trelstar Depot	Watson
			Trelstar Depot Clip’n’Ject	Watson
		11.25 mg (of triptorelin)	Trelstar LA	Watson
			Trelstar LA Clip’n’Ject	Watson

Disclaimer

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 November 2010. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1. Watson Pharma. Trelstar Depot 3.75 mg (triptorelin pamoate for injectable suspension) prescribing information. Corona, CA; 2006 Aug.

2. Parmar H, Phillips RH, Lightman SL et al. Randomised controlled study of orchidectomy vs long-acting D-Trp-6-LHRH microcapsules in advanced prostatic carcinoma. Lancet. 1985; 2:1201-5. [PubMed 2866289]

3. Mahler C. Is disease flare a problem? Cancer. 1993; 72:3799-802.

4. Rolandi E, Martorana G, Franceschini R et al. Treatment of prostatic cancer with a depot preparation of an LHRH analogue: endocrine effects. Curr Ther Res. 1985; 38:670-5.

5. Kahan A, Delrieu F, Amor B et al. Disease flare induced by D-Trp⁶-LHRH analogue in patients with metastatic prostatic cancer. Lancet. 1984; 1:971-2. [IDIS 184509] [PubMed 6143912]

6. Pharmacia & Upjohn, Kalomazoo, MI: Personal communication.

7. Watson Pharma. Trelstar LA 11.25 mg (triptorelin pamoate for injectable suspension) prescribing information. Corona, CA: 2006 Aug.

8. Anon. Drugs of choice for cancer. Treat Guidel Med Lett. 2003; 1:41-52.

More Triptorelin Pamoate resources

• Triptorelin Pamoate Side Effects (in more detail)
• Triptorelin Pamoate Use in Pregnancy & Breastfeeding
• Triptorelin Pamoate Drug Interactions
• Triptorelin Pamoate Support Group
• 1 Review for Triptorelin Pamoate - Add your own review/rating

Compare Triptorelin Pamoate with other medications

• Prostate Cancer

Sul-Ray Aloe Vera Acne Topical

Generic Name: sulfur (Topical route)

SUL-fur

Commonly used brand name(s)

In the U.S.

• Liquimat


• Sastid Soap


• Sulfoam


• Sulfo-Lo


• Sulmasque


• Sulpho-Lac


• Sul-Ray Aloe Vera Acne


• Thylox Acne Treatment


• Zapzyt Cleansing

Available Dosage Forms:

• Soap


• Ointment


• Shampoo


• Liquid


• Lotion


• Cream


• Gel/Jelly


• Solution

Therapeutic Class: Antiacne

Uses For Sul-Ray Aloe Vera Acne

Sulfur is used to treat many kinds of skin disorders. Sulfur cream, lotion, ointment, and bar soap are used to treat acne. Sulfur ointment is used to treat seborrheic dermatitis and scabies. Sulfur may also be used for other conditions as determined by your doctor.

Some of these preparations are available only with your doctor's prescription.

Before Using Sul-Ray Aloe Vera Acne

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

Although there is no specific information comparing use of this medicine in children with use in other age groups, this medicine 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. Although there is no specific information comparing use of sulfur in the elderly with use in other age groups, this medicine is not expected to cause different side effects or problems in older people than it does in younger adults.

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. Tell your healthcare professional if you are taking any other prescription or nonprescription (over-the-counter [OTC]) medicine.

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.

Proper Use of sulfur

This section provides information on the proper use of a number of products that contain sulfur. It may not be specific to Sul-Ray Aloe Vera Acne. Please read with care.

Use this medicine only as directed. Do not use it more often and do not use it for a longer period of time than recommended on the label, unless otherwise directed by your doctor.

Keep this medicine away from the eyes. If you should accidentally get some in your eyes, flush them thoroughly with water.

To use the cream or lotion form of this medicine:

• Before applying the medicine, wash the affected areas with soap and water and dry thoroughly. Then apply enough medicine to cover the affected areas and rub in gently.

To use the ointment form of this medicine for seborrheic dermatitis:

• Before applying the medicine, wash the affected areas with soap and water and dry thoroughly. Then apply enough medicine to cover the affected areas and rub in gently.

To use the ointment form of this medicine for scabies:

• Before applying the medicine, wash your entire body with soap and water and dry thoroughly.


• At bedtime, apply enough medicine to cover your entire body from the neck down and rub in gently. Leave the medicine on your body for 24 hours.


• Before applying the medicine again, you may wash your entire body.


• 24 hours after the last treatment with this medicine, it is important that you thoroughly wash your entire body again.

To use the soap form of this medicine:

• Work up a rich lather with the soap, using warm water. Wash the affected areas and rinse thoroughly. Apply again, and rub in gently for a few minutes. Remove excess lather with a towel or tissue without rinsing.

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 acne:
  
  • For cream and bar soap dosage forms:
    
    • Adults and children—Use on the skin as needed.
    
    
  
  
  • For lotion dosage form:
    
    • Adults and children—Use two or three times a day.
    
    
  
  
  • For ointment dosage form:
    
    • Adults and children—Use the 0.5% ointment on the skin as needed.
    
    
  
  


• For seborrheic dermatitis:
  
  • For ointment dosage form:
    
    • Adults and children—Use the 5 to 10% ointment one or two times a day.
    
    
  
  


• For scabies:
  
  • For ointment dosage form:
    
    • Adults and children—Use the 6% ointment each night for three nights.
    
    
  
  

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.

Precautions While Using Sul-Ray Aloe Vera Acne

When using sulfur, do not use any of the following preparations on the same affected area as this medicine, unless otherwise directed by your doctor:

• Abrasive soaps or cleansers


• Alcohol-containing preparations


• Any other topical acne preparation or preparation containing a peeling agent (for example, benzoyl peroxide, resorcinol, salicylic acid, or tretinoin [vitamin A acid])


• Cosmetics or soaps that dry the skin


• Medicated cosmetics


• Other topical medicine for the skin

To use any of the above preparations on the same affected area as sulfur may cause severe irritation of the skin.

Do not use any topical mercury-containing preparation, such as ammoniated mercury ointment, on the same area as this medicine. To do so may cause a foul odor, may be irritating to the skin, and may stain the skin black. If you have any questions about this, check with your health care professional.

Sul-Ray Aloe Vera Acne 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:

• Skin irritation not present before use of this medicine

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:

• Redness and peeling of skin (may occur after a few days)

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: Sul-Ray Aloe Vera Acne Topical side effects (in more detail)

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.

More Sul-Ray Aloe Vera Acne Topical resources

• Sul-Ray Aloe Vera Acne Topical Side Effects (in more detail)
• Sul-Ray Aloe Vera Acne Topical Use in Pregnancy & Breastfeeding
• Sul-Ray Aloe Vera Acne Topical Drug Interactions
• Sul-Ray Aloe Vera Acne Topical Support Group
• 1 Review for Sul-Ray Aloe Vera Acne Topical - Add your own review/rating

Compare Sul-Ray Aloe Vera Acne Topical with other medications

• Acne

Thiothixene

Class: Thioxanthenes
VA Class: CN709
Chemical Name: N,N-dimethyl-9-[3-(4-methyl-1-piperazinyl)-propylidene]thioxanthene-2-sulfonamide
Molecular Formula: C₂₃H₂₉N₃O₂S₂
CAS Number: 5591-45-7
Brands: Navane

Special Alerts:

[Posted 02/22/2011] ISSUE: FDA notified healthcare professionals that the Pregnancy section of drug labels for the entire class of antipsychotic drugs has been updated. The new drug labels now contain more and consistent information about the potential risk for abnormal muscle movements (extrapyramidal signs or EPS) and withdrawal symptoms in newborns whose mothers were treated with these drugs during the third trimester of pregnancy.

The symptoms of EPS and withdrawal in newborns may include agitation, abnormally increased or decreased muscle tone, tremor, sleepiness, severe difficulty breathing, and difficulty in feeding. In some newborns, the symptoms subside within hours or days and do not require specific treatment; other newborns may require longer hospital stays.

BACKGROUND: Antipsychotic drugs are used to treat symptoms of psychiatric disorders such as schizophrenia and bipolar disorder.

RECOMMENDATION: Healthcare professionals should be aware of the effects of antipsychotic medications on newborns when the medications are used during pregnancy. Patients should not stop taking these medications if they become pregnant without talking to their healthcare professional, as abruptly stopping antipsychotic medications can cause significant complications for treatment. For more information visit the FDA website at: and .

[Posted 06/16/2008] FDA notified healthcare professionals that both conventional and atypical antipsychotics are associated with an increased risk of mortality in elderly patients treated for dementia-related psychosis. In April 2005, FDA notified healthcare professionals that patients with dementia-related psychosis treated with atypical antipsychotic drugs are at an increased risk of death. Since issuing that notification, FDA has reviewed additional information that indicates the risk is also associated with conventional antipsychotics. Antipsychotics are not indicated for the treatment of dementia-related psychosis. The prescribing information for all antipsychotic drugs will now include the same information about this risk in a BOXED WARNING and the WARNINGS section. For more information visit the FDA website at: , and .

Introduction

Thioxanthene-derivative, conventional (prototypical, first-generation) antipsychotic agent; structurally and pharmacologically related to chlorprothixene (no longer commercially available in the US) and trifluoperazine.^{a b c d e g u}

Uses for Thiothixene

Psychotic Disorders

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

Symptomatic management of psychotic disorders (i.e., schizophrenia).^{a b c d u}

Has been used in the management of refractory or treatment-resistant schizophrenia.^c

Mental Retardation

Efficacy not established for the management of behavioral complications in patients with mental retardation.^{a b c u}

Thiothixene Dosage and Administration

General

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

• 
  

  Adjust dosage carefully according to individual requirements and response; use the lowest possible effective dosage.^{a b c u}

  
  


• 
  

  Periodically evaluate patients receiving long-term therapy to determine whether maintenance dosage can be decreased or drug therapy discontinued.^{a b u w} (See Tardive Dyskinesia under Cautions.)

  
  


• 
  

  For symptomatic relief of psychotic disorders, initial therapeutic response to antipsychotic therapy usually occurs within 2–4 weeks and optimum therapeutic response occurs within 6 months or longer.^{d w}

  
  

Administration

Oral Administration

Thiothixene is administered orally once daily or in divided doses 2 or 3 times daily.^{a b c k t u} Thiothixene hydrochloride has been given orally and parenterally, but no longer is commercially available in the US.^{a c h v}

Dosage

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

Pediatric Patients

Psychotic Disorders

Oral

Children ≥12 years of age: Initially, 2 mg 3 times daily for mild to moderate psychotic disorders; may gradually increase dosage, if necessary, up to 15 mg daily.^{a b c u}

For more severe psychotic disorders in children ≥12 years of age: Initially, 5 mg twice daily; may then increase dosage until satisfactory response obtained.^{a b c u}

Optimal maintenance dosage usually 20–30 mg daily; may be increased up to 60 mg daily, if necessary; once-daily administration may be adequate.^{a b c k u}

Daily dosages >60 mg rarely provide additional therapeutic effect.^{a b c u}

Adults

Psychotic Disorders

Oral

For mild to moderate psychotic disorders: Initially, 2 mg 3 times daily; may gradually increase dosage, if necessary, up to 15 mg daily.^{a b c u}

For more severe psychotic disorders: Initially, 5 mg twice daily; may then increase dosage until satisfactory response obtained.^{a b c u}

Optimal maintenance dosage usually 20–30 mg daily; may be increased up to 60 mg daily, if necessary; once-daily administration may be adequate.^{a b c k u}

Daily dosages >60 mg rarely provide additional therapeutic effect.^{a b c u}

Prescribing Limits

Pediatric Patients

Psychotic Disorders

Oral

Children ≥12 years of age: Maximum 60 mg daily.^{a b c u}

Adults

Psychotic Disorders

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

Oral

Maximum 60 mg daily.^{a b c u}

Special Populations

Geriatric Patients

No specific dosage recommendations for geriatric patients, but generally select dosage at the lower end of recommended range; increase dosage more gradually and monitor closely.^{a b d h u w} (See Geriatric Use under Cautions and see Special Populations under Pharmacokinetics.)

Cautions for Thiothixene

Contraindications

• 
  

  Circulatory collapse.^{a b c u}

  
  


• 
  

  Comatose states or CNS depression from any cause.^{a b c u} (See Specific Drugs and Laboratory Tests under Interactions.)

  
  


• 
  

  Blood dyscrasias.^{a b c u}

  
  


• 
  

  Known hypersensitivity to thiothixene.^{a b c u} Not known if cross-sensitivity exists between thioxanthenes and phenothiazines; consider possibility that cross-sensitivity may occur.^{a b c u}

  
  

Warnings/Precautions

Warnings

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

Shares the toxic potentials of other antipsychotic agents (e.g., phenothiazines); observe the usual precautions associated with therapy with these agents.^{a b c u}

Tardive Dyskinesia

Tardive dyskinesia, a syndrome of potentially irreversible, involuntary, dyskinetic movements, may develop in patients receiving antipsychotic agents, including thiothixene.^{a b c d u w} Consider reducing thiothixene dosage or discontinuing drug and switching to a second-generation (atypical) antipsychotic agent.^{a b c d u w}

Neuroleptic Malignant Syndrome

Neuroleptic malignant syndrome (NMS), a potentially fatal syndrome requiring immediate discontinuance of the drug and intensive symptomatic treatment, has been reported with antipsychotic agents, including thiothixene.^{a b c u w}

CNS Depression

May impair mental and/or physical abilities, especially during the first few days of therapy; use caution with activities requiring alertness (e.g., operating vehicles or machinery).^{a b u}

Response to CNS depressants and alcohol may be potentiated.^{a b u} (See Specific Drugs and Laboratory Tests under Interactions.)

Sensitivity Reactions

Hypersensitivity and Cross-sensitivity

Possible sensitivity reactions reported with thiothixene (e.g., rash, pruritus, urticaria, anaphylactoid reactions) and related drugs (e.g., agranulocytosis, pancytopenia, thrombocytopenic purpura, jaundice, biliary stasis).^{a b c u w}

Not known if cross-sensitivity exists between thioxanthenes and phenothiazines; consider possibility that cross-sensitivity may occur.^{a b u}

Photosensitivity

Photosensitivity may occur; avoid excessive exposure to sunlight during therapy.^{a b u w}

General Precautions

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

Seizures

Possible risk of seizures; may lower seizure threshold.^{a b c u} Use with extreme caution in patients with a history of seizures or during alcohol withdrawal.^{a b c u} (See Specific Drugs and Laboratory Tests under Interactions.)

Cardiovascular Effects

Possible hypotension, tachycardia, nonspecific ECG changes, dizziness, and/or syncope; use with caution in patients with cardiovascular disease.^{a b c u}

If severe hypotension occurs, administer norepinephrine or phenylephrine; epinephrine or dopamine should not be used.^{a b c u w} (See Specific Drugs and Laboratory Tests under Interactions.)

Anticholinergic Effects

Possible anticholinergic effects (e.g., dry mouth, blurred vision, constipation, increased perspiration, urinary retention, impotence).^{a b c u}

Use with caution in patients with glaucoma or prostatic hypertrophy.^c (See Specific Drugs and Laboratory Tests under Interactions.)

Ocular Effects

Pigmentary retinopathy and lenticular pigmentation reported with prolonged therapy with antipsychotic agents, including thiothixene.^{a b c u} Observe carefully.^{a b c u}

Prolactin Secretion

Elevated prolactin concentrations reported; elevation persists during chronic administration.^{a b c u w}

Clinical significance unknown; consider that approximately one-third of human breast cancers are prolactin dependent when prescribing thiothixene in patients with previously detected breast cancer.^{a b c u w}

Galactorrhea, amenorrhea, gynecomastia, and impotence reported.^{a b c u w}

Regulation of Body Temperature

Use with caution in patients exposed to extreme heat or cold.^{a b c u w}

Other Precautions

Antiemetic effects may mask signs of overdosage of other drugs (e.g., antineoplastic agents) or obscure cause of vomiting in various disorders (e.g., intestinal obstruction, Reye’s syndrome, brain tumor).^{a b c u w}

Specific Populations

Pregnancy

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

Category C.^e

Lactation

Not known but considered likely to distribute into human milk; possible effects on nursing infant unknown.^{e h n o r s} Caution if used in nursing women; carefully assess potential benefits and risks.^{e n o}

Pediatric Use

Safety not established in children <12 years of age.^{a b c u}

Geriatric Use

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

Geriatric patients appear to be particularly sensitive to adverse CNS (e.g., tardive dyskinesia, parkinsonian manifestations, akathisia, sedation), anticholinergic, and cardiovascular (e.g., orthostatic hypotension) effects of antipsychotic agents.^{a b d h i u w}

Use with caution.^h (See Geriatric Patients under Dosage and Administration and see Special Populations under Pharmacokinetics.)

Common Adverse Effects

Drowsiness or sedation, extrapyramidal reactions (e.g., Parkinson-like symptoms, dystonia, akathisia, tardive dyskinesia), anticholinergic effects (e.g., dry mouth, blurred vision), hypotension.^{a b c u}

Interactions for Thiothixene

Drugs Affecting Hepatic Microsomal Enzymes

Potential pharmacokinetic interaction (increased or decreased plasma thiothixene concentrations) with concomitant use of CYP enzyme inhibitors or inducers.^{a b h j l u} (See Specific Drugs and Laboratory Tests under Interactions.)

Specific Drugs and Laboratory Tests

Drug or Test	Interaction	Comments
Alcohol	Potential additive CNS effects and hypotensiona b u w	Use with cautiona b h u w
Anticholinergic drugs (e.g., atropine)	Possible potentiation of anticholinergic effectsa b c u	Use with cautiona b u
Anticonvulsants (e.g., carbamazepine, phenobarbital, phenytoin)	Anticonvulsants may decrease plasma thiothixene concentrationsa h j l Thiothixene may lower seizure thresholda b c u Barbiturates: Thiothixene does not appear to potentiate the anticonvulsant activity of barbituratesa b c u	Observe for signs and symptoms of reduced thiothixene effectivenessa Dosage adjustments of anticonvulsants may be necessary i Barbiturates: Do not reduce anticonvulsant dosage during concurrent usea b c u
Antidepressants, tricyclic (TCAs)	Possible increased plasma concentrations of thiothixenej l
β-Blockers (e.g., propranolol)	Possible decreased thiothixene clearancej l
Cimetidine	Possible decreased thiothixene clearanceh j l
CNS depressants (e.g., antihistamines, barbiturates, general anesthetics, opiate analgesics, sedative/hypnotics)	Possible additive CNS effects and hypotensiona b u	Use with caution to avoid excessive sedation or CNS depression; carefully adjust dosages of both agents as necessarya b h u
Epinephrine or dopamine	Possible further lowering of BPa b c u w	Do not use epinephrine or dopamine for thiothixene-induced hypotensiona b c u w (see Cardiovascular Effects under Cautions)
Hypotensive agents	Possible additive hypotensive effecta c	Observe closely for signs of excessive hypotensiona c
Isoniazid	Possible decreased thiothixene clearancel
Lithium	An acute encephalopathic syndrome reported occasionally, especially when high serum lithium concentrations present h w	Observe patients receiving combined therapy for evidence of adverse neurologic effects; promptly discontinue if such signs or symptoms appearw
Paroxetine	Pharmacokinetic interaction unlikelym
Smoking	Possible decreased plasma thiothixene concentrations h j l
Tests for pregnancy	False-positive results reported in some patients receiving phenothiazines; less likely to occur when serum test is useda b u

Thiothixene Pharmacokinetics

Absorption

Bioavailability

Rapidly and well absorbed from GI tract following oral administration.^{c i k} Peak plasma concentrations usually occur within 1–3 hours.^{i k t}

Onset

Antipsychotic effects usually are apparent within 2–4 weeks after initiation of oral therapy and optimum therapeutic response usually occurs within 6 months or longer.^{c d w}

Plasma Concentrations

Optimal therapeutic plasma concentrations not well defined, but clinical improvement associated with peak plasma concentrations of 2–15 mcg/L.^{t y}

Distribution

Extent

Widely distributed into body tissues.^{c i}

Crosses placenta in animals; considered likely to cross placenta in humans.^{p x} Not known if distributed into human milk but distribution into breast milk considered likely.^{e h o r}

Plasma Protein Binding

>99%.ⁱ

Elimination

Metabolism

Principally metabolized in the liver; undergoes extensive oxidative first-pass metabolism to form thiothixene sulfoxide and N-desmethylthiothixene.^{c h i j}

Elimination Route

Excreted mainly in feces via biliary elimination as unchanged drug and as demethyl, sulfoxide, demethylated sulfoxide, and hydroxylated metabolites.^{c i}

Unlikely to be removed by hemodialysis and peritoneal dialysis.^{a b u w}

Half-life

34–35 hours.^{d i k m t}

Special Populations

Clearance is reduced in females and in patients >50 years of age.^h

Stability

Storage

Oral

Capsules

Tight, light-resistant containers at 20–25°C; protect from light and moisture.^{b c u}

ActionsActions

• 
  

  Produces pharmacologic effects similar to those of other conventional antipsychotic agents (e.g., phenothiazines, butyrophenones, chlorprothixene).^{a b c u w}

  
  


• 
  

  Precise mechanism(s) of antipsychotic action not determined, but may be principally related to antidopaminergic effects.^w Acts principally at subcortical levels on the reticular formation, hypothalamus, and limbic system.^{c w}

  
  


• 
  

  Exhibits weak anticholinergic, antihistaminic, α-adrenergic, and sedative effects and strong extrapyramidal effects; appears to possess antiemetic activity.^{a b c h u}

  
  

Advice to Patients

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

• 
  

  Potential for drug to impair mental alertness or physical coordination; use caution when driving or operating machinery until effects on individual are known.^{a b c h u}

  
  


• 
  

  Importance of clinicians informing patients in whom chronic use is contemplated of risk of tardive dyskinesia, taking into account clinical circumstances and competency of patient to understand information provided.^{a b u}

  
  


• 
  

  Importance of clinicians informing patients of risk of extrapyramidal reactions and providing reassurance that these reactions usually can be controlled by administration of antiparkinsonian drugs (e.g., benztropine) and by subsequent dosage reduction.^{a b c u w}

  
  


• 
  

  Advise patients to avoid excessive sunlight.^{a b u w}

  
  


• 
  

  Importance of avoiding exposure to temperature extremes.^{a b c w}

  
  


• 
  

  Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.^{a b u}

  
  


• 
  

  Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.^{a b u}

  
  


• 
  

  Importance of informing patients of other important precautionary information.^{a b u} (See Cautions.)

  
  

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Thiothixene

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	Capsules	1 mg*	Navane	Pfizer
			Thiothixene Capsules	Mylan, Sandoz
		2 mg*	Navane	Pfizer
			Thiothixene Capsules	Mylan, Sandoz
		5 mg*	Navane	Pfizer
			Thiothixene Capsules	Mylan, Sandoz
		10 mg*	Navane	Pfizer
			Thiothixene Capsules	Mylan, Sandoz
		20 mg	Navane	Pfizer

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 04/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Navane 10MG Capsules (PFIZER U.S.): 90/$189.99 or 270/$565.95

Navane 2MG Capsules (PFIZER U.S.): 90/$92.99 or 270/$266.98

Navane 20MG Capsules (PFIZER U.S.): 90/$266 or 270/$779.99

Navane 5MG Capsules (PFIZER U.S.): 90/$139.99 or 270/$409.96

Thiothixene 1MG Capsules (SANDOZ): 90/$22.99 or 270/$49.97

Thiothixene 2MG Capsules (MYLAN): 90/$26.99 or 270/$71.97

Thiothixene 5MG Capsules (SANDOZ): 90/$25.99 or 270/$59.97

Disclaimer

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 March 15, 2011. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

a. Roerig, Division of Pfizer Inc. Navane (thiothixene) capsules and solution, concentrate prescribing information. New York, NY. 2008 Mar.

b. Sandoz Inc. Thiothixene capsules prescribing information. Princeton, NJ. 2007 Feb.

c. AHFS drug information 2008. McEvoy GK, ed. Thiothixene. Bethesda, MD: American Society of Health-System Pharmacists; 2008:2516-7.

d. American Psychiatric Association. Practice guideline for the treatment of patients with schizophrenia, second edition. From the APA website

e. Briggs GG, Freeman RK, Yaffe SJ. Drugs in pregnancy and lactation. 7th ed. Baltimore, MD: Williams & Wilkins; 2005:1577-8.

f. American Academy of Pediatrics. Use of psychoactive medication during pregnancy and possible effects on the fetus and newborn. Pediatrics. 2000; 105:880-87. [PubMed 10742343]

g. The United States Pharmacopeial Convention, Inc. USAN and the USP Dictionary drug names. Rockville, MD: United States Pharmacopeial Convention, Inc; 2007:853.

h. AMA Division of Drugs. AMA drug evaluations. Chicago: American Medical Association; 1994:2:1-2:29.

i. Balant-Gorgia AE, Balant L. Antipsychotic drugs: clinical pharmacokinetics of potential candidates for plasma concentration monitoring. Clin Pharmacokinet. 1987: 13:65-90.

j. Ereshefsky L, Saklad SR, Watanabe MD, et al. Thiothixene pharmacokinetic interactions: a study of hepatic enzyme inducers, clearance inhibitors, and demographic variables. J Clin Psychopharmacol. 1991; 11:296-301. [PubMed 1765572]

k. Hobbs DC, Welch WM, Short MJ, et al. Pharmacokinetics of thiothixene in man. Clin Pharmacol Ther. 1974; 16:473-8. [PubMed 4415039]

l. Ereshefsky L, Jann MW, Saklad SR, et al. Bioavailability of psychotropic drugs: historical perspective and pharmacokinetic overview. J Clin Psychiatry. 1986; 47 (Suppl):6-15. [PubMed 3528134]

m. Guthrie SK, Hariharan M, Kumar AA, et al. The effect of paroxetine on thiothixene pharmacokinetics. J Clin Pharm Ther. 1997; 22:221-6. [PubMed 9447478]

n. Webb RT, Howard L, Abel KM. Antipsychotic drugs for non-affective psychosis during pregnancy and postpartum. Cochrane Database of Systematic Reviews 2004, Issue 2. Art. No.: CD004411. DOI: 10.1002/14651858.CD004411.pub2.

o. Cohen LS, Heller VL, Rosenbaum JF. Treatment guidelines for psychotropic drug use in pregnancy. Psychosomatics. 1989; 30:25-33. [PubMed 2643809]

p. Altshuler LL, Cohen L, Szuba MP, et al. Pharmacologic management of psychiatric illness during pregnancy: dilemmas and guidelines. Am J Psychiatry. 1996; 153:592-606. [PubMed 8615404]

q. Mortola JF. The use of psychotropic agents in pregnancy and lactation. Psychiatr Clin North Am. 1989; 12:69-87. [PubMed 2652114]

r. Goldberg H, Nissim R. Psychotropic drugs in pregnancy and lactation. Int J Psychiatry Med. 1994; 24:129-49. [PubMed 7960421]

s. Calabrese JR, Gulledge AD. Psychotropics during pregnancy and lactation: a review. Psychosomatics. 1985; 26:413-26. [PubMed 2859631]

t. Milton GV, Jann MW. Emergency treatment of psychotic symptoms: pharmacokinetic considerations for antipsychotic drugs. Clin Pharmacokinet. 1995; 28:494-504. [PubMed 7656507]

u. Mylan Pharmaceuticals Inc. Thiothixene capsules prescribing information. Morgantown, WV; 2003 Oct.

v. Roerig, Division of Pfizer Inc. Navane (thiothixene hydrochloride) intramuscular for injection prescribing information. New York, NY. 2008 Jan.

w. AHFS drug information 2008. McEvoy GK, ed. Phenothiazines general statement. Bethesda, MD: American Society of Health-System Pharmacists; 2008: 2497-508.

x. Schmidt MH, Lee T. Investigation of striatal dopamine D2 receptor acquisition following prenatal neuroleptic exposure. Psychiatry Res. 1991; 36:319-28. [PubMed 1676523]

y. Mavroidis ML, Kanter DR, Hirschowitz J et al. Clinical relevance of thiothixene plasma levels.J Clin Psychopharmacol. 1984; 4:155-7. [PubMed 6736276]

More Thiothixene resources

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

• Thiothixene Professional Patient Advice (Wolters Kluwer)


• Thiothixene Prescribing Information (FDA)


• Thiothixene MedFacts Consumer Leaflet (Wolters Kluwer)


• thiothixene Concise Consumer Information (Cerner Multum)


• thiothixene Advanced Consumer (Micromedex) - Includes Dosage Information


• Navane Advanced Consumer (Micromedex) - Includes Dosage Information


• Navane Prescribing Information (FDA)

Compare Thiothixene with other medications

• Psychosis

Testolactone

Generic Name: testolactone (test O lack tone)

Brand Names: Teslac

What is testolactone?

Testolactone blocks the production of the hormone estrogen. Certain types of breast cancer require estrogen to grow.

Testolactone is used to treat some types of breast cancer.

Testolactone may also be used for purposes other than those listed in this medication guide.

What is the most important information I should know about testolactone?

Testolactone should not be used for the treatment of men with breast cancer or in patients with a history of allergic reactions to the drug.

What should I discuss with my healthcare provider before taking testolactone?

Testolactone should not be used for the treatment of men with breast cancer or in patients with a history of allergic reactions to the drug.

Testolactone is in the FDA pregnancy category C. This means that it is not known whether testolactone will be harmful to an unborn baby. Do not take this medication without first talking to your doctor if you are pregnant or could become pregnant during treatment. Testolactone passes into breast milk in small amounts and may affect a nursing baby. Do not take testolactone without first talking to your doctor if you are breast-feeding a baby.

How should I take testolactone?

Take testolactone exactly as directed by your doctor. If you do not understand these directions, ask your pharmacist, nurse, or doctor to explain them to you.

Take each dose with a full glass (8 ounces) of water.

It is important to take testolactone regularly to get the most benefit.

Your doctor may want you to have breast exams (or to perform self breast exams), mammograms, blood tests, or other medical evaluations during treatment with testolactone to monitor progress and side effects.

Store testolactone at room temperature away from moisture and heat. Keep this product out of the reach of children.

See also: Testolactone dosage (in more detail)

What happens if I miss a dose?

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 your doctor directs otherwise.

What happens if I overdose?

Call an emergency room or a poison control center for advice if you suspect an overdose.

Symptoms of a testolactone overdose are unknown, but nausea, vomiting, seizures, tremor, or dizziness may be expected.

What should I avoid while taking testolactone?

There are no restrictions on food, beverages, or activity during treatment with testolactone unless otherwise directed by your doctor.

Testolactone side effects

Stop taking testolactone and seek emergency medical attention or contact your doctor immediately if you experience any of the following serious side effects:

• 
  

  an allergic reaction (difficulty breathing; closing of the throat; swelling of the lips, tongue, or face; or hives);

  
  


• 
  

  new breast lumps;

  
  


• 
  

  bone pain;

  
  


• 
  

  menstrual changes, abnormal vaginal bleeding, vaginal discharge, or pelvic pain or pressure; or

  
  


• 
  

  excessive nausea, vomiting, or thirst.

  
  

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.

Testolactone Dosing Information

Usual Adult Dose for Breast Cancer--Palliative:

For use as adjunctive therapy in the palliative treatment of advanced or disseminated breast cancer in postmenopausal women when hormonal therapy is indicated or in women who were diagnosed as having had disseminated breast carcinoma when premenopausal, in whom ovarian function has been subsequently terminated: 250 mg 4 times a day.

What other drugs will affect testolactone?

Before taking testolactone, tell your doctor if you are taking

• 
  

  an estrogen such as Premarin, Ogen, Estratest, Estraderm, Vivelle, Climara, and others;

  
  


• 
  

  a birth control pill that contains estrogen;

  
  


• 
  

  warfarin (Coumadin) or another blood thinner.

  
  

You may not be able to take testolactone or you may require special monitoring or a dosage adjustment if you are taking any of the medicines listed above.

Drugs other than those listed here may also interact with testolactone. Talk to your doctor and pharmacist before taking any prescription or over-the-counter medicines, including herbal products.

More testolactone resources

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

• testolactone Advanced Consumer (Micromedex) - Includes Dosage Information


• Testolactone MedFacts Consumer Leaflet (Wolters Kluwer)


• Teslac Prescribing Information (FDA)

Compare testolactone with other medications

• Breast Cancer, Palliative

Where can I get more information?

• Your pharmacist has additional information about testolactone written for health professionals that you may read.

What does my medication look like?

Testolactone is available with a prescription under the brand name Teslac. Other brand or generic formulations may also be available. Ask your pharmacist any questions you have about this medication, especially if it is new to you.

See also: testolactone side effects (in more detail)

Norvir

Generic Name: ritonavir (Oral route)

rit-OH-na-vir

Oral route(Capsule, Liquid Filled;Solution;Tablet)

Coadministration of ritonavir with sedative hypnotics, antiarrhythmics, or ergot alkaloid preparations may result in potentially serious and/or life-threatening adverse events due to possible effects of ritonavir on the hepatic metabolism of certain drugs .

Commonly used brand name(s)

In the U.S.

• Norvir

Available Dosage Forms:

• Capsule, Liquid Filled


• Tablet


• Solution

Therapeutic Class: Antiretroviral Agent

Pharmacologic Class: Protease Inhibitor

Uses For Norvir

Ritonavir is used alone or in combination with other medicines for the treatment of the infection caused by the human immunodeficiency virus (HIV). HIV is the virus that causes acquired immune deficiency syndrome (AIDS).

Ritonavir will not cure HIV infection or prevent AIDS. It helps keep HIV from reproducing and appears to slow down the destruction of the immune system. This may help delay problems that are usually related to AIDS or HIV disease from occurring. Ritonavir will not keep you from spreading HIV to other people. People who receive this medicine may continue to have other problems related to AIDS or HIV disease.

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

Before Using Norvir

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

Appropriate studies have not been performed on the relationship of age to the effects of ritonavir in infants younger than 1 month old. Safety and efficacy have not been established.

Geriatric

Although appropriate studies on the relationship of age to the effects of ritonavir have not been performed in the geriatric population, geriatric-specific problems are not expected to limit the usefulness of ritonavir in the elderly. However, elderly patients are more likely to have age-related liver, kidney, or heart problems, which may require caution and an adjustment in the dose for patients receiving ritonavir.

Pregnancy

	Pregnancy Category	Explanation
All Trimesters	B	Animal studies have revealed no evidence of harm to the fetus, however, there are no adequate studies in pregnant women OR animal studies have shown an adverse effect, but adequate studies in pregnant women have failed to demonstrate a risk to the fetus.

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 not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.

• Alfuzosin


• Amiodarone


• Astemizole


• Bepridil


• Cisapride


• Colchicine


• Conivaptan


• Dihydroergotamine


• Dronedarone


• Encainide


• Eplerenone


• Ergoloid Mesylates


• Ergonovine


• Ergotamine


• Flecainide


• Lovastatin


• Methylergonovine


• Methysergide


• Midazolam


• Pimozide


• Propafenone


• Quinidine


• Ranolazine


• Sildenafil


• Silodosin


• Simvastatin


• St John's Wort


• Terfenadine


• Tolvaptan


• Triazolam


• Voriconazole

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.

• Abiraterone


• Aprepitant


• Bosentan


• Brentuximab Vedotin


• Cabazitaxel


• Crizotinib


• Dasatinib


• Digoxin


• Docetaxel


• Etravirine


• Everolimus


• Fentanyl


• Fluticasone


• Fusidic Acid


• Garlic


• Iloperidone


• Ixabepilone


• Lapatinib


• Methylenedioxymethamphetamine


• Nilotinib


• Oxycodone


• Pazopanib


• Pitavastatin


• Quinine


• Rifabutin


• Rifampin


• Rivaroxaban


• Romidepsin


• Ruxolitinib


• Salmeterol


• Sunitinib


• Tamoxifen


• Tamsulosin


• Temsirolimus


• Ticagrelor


• Topotecan


• Toremifene


• Vemurafenib


• Venlafaxine


• Vinblastine


• Vincristine

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.

• Acenocoumarol


• Alprazolam


• Amitriptyline


• Amlodipine


• Amprenavir


• Bupropion


• Carbamazepine


• Cerivastatin


• Clarithromycin


• Clonazepam


• Clozapine


• Cyclosporine


• Dalfopristin


• Delavirdine


• Desipramine


• Desogestrel


• Dexamethasone


• Didanosine


• Dienogest


• Diltiazem


• Disopyramide


• Drospirenone


• Dutasteride


• Efavirenz


• Estradiol Cypionate


• Estradiol Valerate


• Ethinyl Estradiol


• Ethynodiol Diacetate


• Etonogestrel


• Fluoxetine


• Fosamprenavir


• Imipramine


• Indinavir


• Itraconazole


• Ketoconazole


• Lamotrigine


• Levonorgestrel


• Levothyroxine


• Maraviroc


• Medroxyprogesterone Acetate


• Meperidine


• Mestranol


• Methadone


• Methamphetamine


• Metoprolol


• Mexiletine


• Nefazodone


• Norelgestromin


• Norethindrone


• Norgestimate


• Norgestrel


• Paroxetine


• Phenobarbital


• Phenytoin


• Posaconazole


• Prednisone


• Quinupristin


• Rifapentine


• Risperidone


• Tacrolimus


• Tadalafil


• Tenofovir Disoproxil Fumarate


• Theophylline


• Trazodone


• Valproic Acid


• Verapamil


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

• Diabetes mellitus or


• Hyperglycemia (high blood sugar)—May increase the amount of sugar in the blood.

• Heart disease or


• Heart rhythm problems (e.g., prolonged PR interval) or


• Hyperlipidemia (high cholesterol or fat in the blood) or


• Liver disease or other liver problems (e.g., hepatitis) or


• Pancreatitis (inflammation of the pancreas)—Use with caution. May make these conditions worse.

• Hemophilia (a bleeding problem)—May increase the chance of bleeding.

Proper Use of Norvir

Take this medicine exactly as directed by your doctor. Do not change the dose or stop using this medicine without checking first with your doctor. When your supply of this medicine is running low, contact your doctor or pharmacist ahead of time. Do not allow yourself to run out of this medicine.

It is important that ritonavir be taken with food.

Swallow the tablet whole. Do not break, crush, or chew it.

For patients taking the oral liquid:

• Shake the bottle well before using.


• Use a specially marked measuring syringe or cup to measure each dose accurately. The average household teaspoon may not hold the right amount of liquid.


• You can mix the oral liquid with chocolate milk or nutritional drinks (such as Ensure® or Advera®) to make it taste better. You should drink this medicine within one hour of mixing.

This medicine works best when there is a constant amount in the blood. To help keep blood levels constant, do not miss any doses. It is best to take the doses at evenly spaced times, day and night. For example, if you are to take two doses each day, the doses should be spaced about 12 hours apart. If you need help in planning the best times to take your medicine, check with your doctor.

Ritonavir must be taken with other medicines. Tell your doctor about all of the medications you are taking since the dose of ritonavir or other medications you take may need to be adjusted.

If you are taking ritonavir with a medication called didanosine (Videx®), take the ritonavir 2 hours and 30 minutes before or after the didanosine.

Read and carefully follow the patient information leaflet before starting ritonavir treatment and each time you refill. Ask your doctor or pharmacist if you have any questions.

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 treatment of HIV infection:
  
  • For oral dosage forms (capsules, solution, or tablets):
    
    • Adults—600 milligrams (mg) two times per day.
    
    
    • Children 1 month of age and older—Dose is based on body size and must be determined by your doctor. The dose is usually 350 to 400 milligrams per square meter (mg/[m]2) of body size two times per day. However, the dose is usually not more than 600 mg two times per day.
    
    
    • Children younger than 1 month of age—Use and dose must be determined by your doctor.
    
    
  
  

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

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.

Store the capsules in the refrigerator or at room temperature in a closed container. If stored at room temperature, use the medicine within 30 days. Keep away from heat and direct light.

Store the oral liquid or tablets in a closed container at room temperature, away from heat and direct light. Do not refrigerate.

Precautions While Using Norvir

It is very important that your doctor check the progress of you or your child at regular visits to make sure this medicine is working properly. Blood tests may be needed to check for unwanted effects.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription and nonprescription (over-the-counter [OTC]) medicines, and herbal (e.g., St. John's wort) or vitamin supplements.

Do not use this medicine if you or your child are also using alfuzosin (Uroxatral®), amiodarone (Cordarone®), astemizole (Hismanal®), bepridil (Vascor®), cisapride (Propulsid®), ergot medicines (e.g., dihydroergotamine, ergonovine, ergotamine, methylergonovine, Cafergot®, or Ergomar®), flecainide (Tambocor®), lovastatin (Altocor®, Mevacor®), oral midazolam (Versed®), pimozide (Orap®), propafenone (Rythmol®), quinidine (Quinaglute®), sildenafil (Revatio®), simvastatin (Simcor®, Vytorin®, Zocor®), terfenadine (Seldane®), triazolam (Halcion®), or voriconazole (Vfend®). Using these medicines together with ritonavir may increase your chance of having serious side effects.

Check with your doctor right away if you or your child have pain or tenderness in the upper stomach; pale stools; dark urine; loss of appetite; nausea; unusual tiredness or weakness; or yellow eyes or skin. These could be symptoms of a serious liver problem.

Pancreatitis may occur while you are using this medicine. Stop using this medicine and check with your doctor right away if you or your child have sudden and severe stomach pain, chills, constipation, nausea, vomiting, fever, or lightheadedness.

This medicine may decrease the effects of some birth control pills. To avoid getting pregnant, use an additional form of birth control along with your pills. Other forms of birth control include condoms, diaphragms, or contraceptive foams or jellies.

Serious skin reactions can occur with this medicine. Check with your doctor right away if you or your child have any of the following symptoms while taking this medicine: blistering, peeling, or loosening of the skin; fever; chills; cough; diarrhea; itching; joint or muscle pain; rash; red skin lesions, often with a purple center; sore throat; sores, ulcers, or white spots in the mouth or on the lips; swelling of your hands, face, tongue, or throat; or unusual tiredness or weakness.

This medicine may increase the level of cholesterol and fats in your blood. If this condition occurs, your doctor may give you a medicine to lower the cholesterol and fats. Talk to your doctor if you or your child have concerns.

This medicine will not keep you from giving HIV to your partner during sex. Make sure you understand this and practice safe sex, even if your partner also has HIV, by using a latex condom or other barrier method. This medicine will also not keep you from giving HIV to other people if they are exposed to your blood. Do not re-use or share needles with anyone.

When you start taking HIV medicines, your immune system may get stronger. If you have infections that are hidden in your body, such as pneumonia or tuberculosis, you may notice new symptoms when your body tries to fight them. If this occurs, be sure to tell your doctor.

This medicine may cause you to have excess body fat. Tell your doctor if you or your child notice changes in your body shape, such as an increased amount of fat in the upper back and neck, or around the chest and stomach area. You might also lose fat from the legs, arms, and face.

Norvir 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:

Less common

• Fainting


• feeling faint, dizzy, or lightheaded


• feeling of warmth or heat


• flushing or redness of the skin, especially on the face and neck


• headache


• sweating

Rare

• Confusion


• dehydration


• dry or itchy skin


• fruity mouth odor


• increased hunger


• increased thirst


• increased urination


• nausea


• vomiting


• weight loss

Incidence not known

• Bloating


• chills


• constipation


• convulsions


• cough


• darkened urine


• decreased urination


• difficulty with breathing


• dry mouth


• fast heartbeat


• fever


• hives or welts


• increase in heart rate


• indigestion


• itching


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


• loss of appetite


• loss of bladder control


• muscle spasm or jerking of all extremities


• noisy breathing


• pains in the stomach, side, or abdomen, possibly radiating to the back


• rapid breathing


• redness of the skin


• shortness of breath


• skin rash


• sudden loss of consciousness


• sunken eyes


• thirst


• tightness in the chest


• unusual tiredness or weakness


• wheezing


• wrinkled skin


• yellow eyes or skin

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

• Acid or sour stomach


• belching


• burning, crawling, itching, numbness, prickling, "pins and needles", or tingling feelings


• change in sense of taste


• diarrhea


• dizziness


• general feeling of discomfort or illness


• heartburn


• lack or loss of strength


• sleepiness or unusual drowsiness


• sleeplessness


• trouble sleeping


• unable to sleep


• weakness

Less common

• Body aches or pain


• congestion


• delusions


• dementia


• difficulty with moving


• discouragement


• dryness or soreness of the throat


• excess air or gas in the stomach or intestines


• fear


• feeling sad or empty


• full feeling


• hoarseness


• increased urge to urinate during the night


• irritability


• lack of appetite


• loss of interest or pleasure


• mood or mental changes


• muscle pain or stiffness


• nervousness


• pain in the joints or in unspecified location


• passing gas


• runny nose


• tender, swollen glands in the neck


• throat irritation


• tiredness


• trouble concentrating


• trouble with swallowing


• voice changes


• waking to urinate at night

Incidence not known

• Gaining weight around your neck, upper back, breast, face, or waist

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: Norvir side effects (in more detail)

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More Norvir resources

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

• Norvir Prescribing Information (FDA)


• Norvir Consumer Overview


• Norvir Monograph (AHFS DI)


• Norvir MedFacts Consumer Leaflet (Wolters Kluwer)


• Ritonavir Professional Patient Advice (Wolters Kluwer)

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