Alclometasone Dipropionate

Class: Anti-inflammatory Agents
ATC Class: D07AB10
VA Class: DE200
Chemical Name: (7α,11β,16α)-7-Chloro-11-hydroxy-16-methyl-17,21-bis (1-oxopropoxy)pregna-1,4-diene-3,20-dione
Molecular Formula: C₂₈H₃₇ClO₇
CAS Number: 66734-13-2
Brands: Aclovate

Introduction

A synthetic corticosteroid.^{1 2 12 d}

Uses for Alclometasone Dipropionate

Corticosteroid-responsive Dermatoses

Relief of inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses.^{1 4 5 6 7 8 9 10 11 13 14 17 18 d}

Generally most effective in acute or chronic dermatoses (e.g., seborrheic or atopic dermatitis, localized neurodermatitis, anogenital pruritus, psoriasis, late phase of allergic contact dermatitis, inflammatory phase of xerosis).^b

Topical therapy generally preferred over systemic therapy; fewer associated adverse systemic effects.^b

Topical therapy generally only controls manifestations of dermatoses; eliminate cause if possible.^b

Topical efficacy may be increased by using a higher concentration or occlusive dressing therapy. (See Administration with Occlusive Dressing under Dosage and Administration.)^b

Response may vary from one topical corticosteroid preparation to another.^b

Anti-inflammatory activity may vary considerably depending on the vehicle, drug concentration, site of application, disease, and individual patient.^b

Manufacturers state that alclometasone should not be used for the treatment of acne, rosacea, or perioral dermatitis.^{22 23}

Alclometasone dipropionate 0.05% cream and ointment are considered to have low-to-medium range potency.^{b c d}

Alclometasone Dipropionate Dosage and Administration

General

• 
  

  Consider location of the lesion and the condition being treated when choosing a dosage form.^b

  
  


• 
  

  Creams are suitable for most dermatoses, but ointments may also provide some occlusion and are usually used for the treatment of dry, scaly lesions.^b

  
  


• 
  

  Formulation affects percutaneous penetration and subsequent activity; extemporaneous preparation or dilution of commercially available products with another vehicle may decrease effectiveness.^b

  
  


• 
  

  Patients applying a topical corticosteroid to a large surface area and/or to areas under occlusion should be evaluated periodically for evidence of hypothalamic-pituitary-adrenal (HPA)-axis suppression by appropriate endocrine testing (e.g., ACTH stimulation, plasma cortisol, urinary free cortisol).^{c d} (See Hypothalamic-Pituitary-Adrenal Axis Suppression and also Systemic Effects, under Cautions.)

  
  

Administration

Topical Administration

For dermatologic use only; avoid contact with eyes.^d

Apply creams and ointments topically to the skin or scalp.^c

The area of skin to be treated may be thoroughly cleansed before topical application to reduce the risk of infection; however, some clinicians believe that, unless an occlusive dressing is used, cleansing of the treated area is unnecessary and may be irritating.^b

Apply cream or ointment sparingly in a thin film and rub gently into the affected area.^{1 d}

After a favorable response is achieved, frequency of application or concentration (strength) may be decreased to the minimum necessary to maintain control and to avoid relapse; discontinue if possible.^b

Administration with Occlusive Dressing

Occlusive dressings may be used for severe or resistant dermatoses (e.g., psoriasis).^{1 17} (See Occlusive Dressings under Cautions.)

Soak or wash the affected area to remove scales; apply a thin film of cream or ointment; rub gently into the lesion; and apply another thin film.^b Cover affected area with a thin, pliable plastic film and seal it to adjacent normal skin with adhesive tape or hold in place with a gauze or elastic bandage.^b

If affected area is moist, incompletely seal the edges of the plastic film or puncture the film to allow excess moisture to escape.^b For added moisture in dry lesions, apply cream or ointment and cover with a dampened cloth before the plastic film is applied or briefly soak the affected area in water before application of the drug and plastic film.^b

Thin polyethylene gloves may be used on the hands and fingers, plastic garment bags may be used on the trunk or buttocks, a tight shower cap may be used for the scalp, or whole-body suits may be used instead of plastic film to provide occlusion.^b

Frequency of occlusive dressing changes depends on the condition being treated; cleansing of the skin and reapplication of the corticosteroid are essential at each dressing change.^b

Occlusive dressing is usually left in place for 12–24 hours and therapy is repeated as needed.^b Although occlusive dressing may be left in place for 3–4 days at a time in resistant conditions, most clinicians recommend intermittent use of occlusive dressings for 12 hours daily to reduce the risk of adverse effects (particularly infection) and systemic absorption and for greater convenience.^b

The drug and an occlusive dressing may be used at night, and the drug or a bland emollient may be used without an occlusive dressing during the day.^b

In patients with extensive lesions, sequential occlusion of only one portion of the body at a time may be preferable to whole-body occlusion.^b (See Occlusive Dressings under Cautions.)

Dosage

Pediatric Patients

Administer the least amount of topical preparations that provide effective therapy.^b (See Pediatric Use under Cautions.)

Corticosteroid-responsive Dermatoses

Topical

Children ≥1 year of age: Apply cream or ointment sparingly 2–3 times daily.^{1 d}

Discontinue when control is achieved; if improvement does not occur within 2 weeks, consider reassessment of the diagnosis.^{c d}

Adults

Corticosteroid-responsive Dermatoses

Topical

Apply cream or ointment sparingly 2–3 times daily.^{1 d}

May be used for 2–6 weeks^{5 6 7 8 9 10 11 13 14 18} ; however, more prolonged therapy²³ with appropriate monitoring¹⁷ may be necessary in patients with resistant or chronic conditions.^a

Discontinue when control is achieved; if improvement does not occur within 2 weeks, consider reassessment of the diagnosis.^{c d}

Prescribing Limits

Pediatric Patients

Corticosteroid-responsive Dermatoses

Topical

Children ≥1 year of age: Maximum 3 weeks.^c

Special Populations

Hepatic Impairment

No specific dosage recommendations at this time.^{c d}

Renal Impairment

No specific dosage recommendations at this time.^{c d}

Geriatric Patients

Careful dosage selection recommended.^d

Cautions for Alclometasone Dipropionate

Contraindications

• 
  

  Known hypersensitivity to alclometasone, other corticosteroids, or any ingredient in the formulation.^{1 d}

  
  

Warnings/Precautions

Sensitivity Reactions

Allergic contact dermatitis may manifest as failure to heal rather than irritation as occurs with other topical preparations that do not contain corticosteroids; confirm with diagnostic patch testing.^{b c d}

General Precautions

Hypothalamic-Pituitary-Adrenal Axis Suppression

Topically applied corticosteroids can be absorbed in sufficient amounts to reversibly suppress the HPA axis.^{c d}

Perform periodic HPA-axis evaluation by appropriate testing (e.g., ACTH stimulation, morning plasma cortisol, urinary free cortisol), especially in patients applying a topical corticosteroid to a large surface area or to areas under occlusion.^{b c d}

If HPA-axis suppression occurs, withdraw the drug, reduce the frequency of application, and/or substitute a less potent corticosteroid.^{c d}

HPA-axis function recovery generally is prompt and complete following drug discontinuance.^{c d}

Rarely, glucocorticosteroid insufficiency may require systemic corticosteroid therapy.^{b c d}

Systemic Effects

Systemic absorption following topical administration may result in manifestations of Cushing's syndrome, hyperglycemia, and glucosuria in some patients.^{b c d}

Adverse systemic effects may occur when corticosteroids are used on large areas of the body, for prolonged periods of time, with an occlusive dressing, and/or concurrently with other corticosteroid-containing preparations.^b

Infants and children may be more susceptible to adverse systemic effects.^{c d} (See Pediatric Use under Cautions.)

Local Effects

Possible adverse local reactions (e.g., burning, itching, irritation, dryness, folliculitis, hypertrichosis, acneiform eruptions, hypopigmentation, perioral dermatitis, allergic contact dermatitis, maceration of the skin, secondary infection, skin atrophy, striae, miliaria); may occur more frequently with the use of occlusive dressings, especially with prolonged therapy.^b

Prolonged use of topical corticosteroids may cause atrophy of the epidermis and subcutaneous tissue;^b these effects are most likely to occur (even with short-term use) in intertriginous (e.g., axilla, groin), flexor, and facial areas.^b

If irritation occurs, discontinue drug and institute appropriate therapy.^{c d}

Skin Infection

If concurrent skin infection is present or develops, initiate appropriate anti-infective therapy.^{c d} If infection does not respond promptly, discontinue topical corticosteroid therapy until the infection has been controlled.^{c d}

When topical corticosteroids and topical anti-infectives are used concomitantly, consider that the corticosteroid may mask clinical signs of bacterial, fungal, or viral infections; prevent recognition of ineffectiveness of the anti-infective; or suppress hypersensitivity reactions to ingredients in the formulation.^b In addition, consider the cautions, precautions, and contraindications associated with the anti-infective.^b (See Occlusive Dressings under Cautions.)

Some manufacturers state that topical corticosteroids are contraindicated in patients with tuberculosis of the skin, dermatologic fungal infections, and cutaneous or systemic viral infection (including vaccinia and varicella and herpes simplex of the eye or adjacent skin).^b However, most clinicians believe topical corticosteroids can be used with caution if the infection is treated.^b

Occlusive Dressings

Adverse systemic corticosteroid effects may occur with use of occlusive dressings on large areas of the body and for prolonged periods of time; monitor accordingly.^b (See Hypothalamic-Pituitary-Adrenal Axis Suppression and also see Systemic Effects, under Cautions.)

Adverse local reactions may occur more frequently with the use of occlusive dressings, especially with prolonged therapy.^{b c d} (See Local Effects under Cautions.)

Do not use occlusive dressings on weeping or exudative lesions.^b

Do not use occlusive dressings in patients with primary skin infection.^b

Remove occlusive dressings covering large areas if body temperature increases; thermal homeostasis may be impaired.^b

Use plastic occlusive material with care to avoid the risk of suffocation.^b

Specific Populations

Pregnancy

Category C.^{c d}

Lactation

Not known whether topical alclometasone is distributed into milk.^{c d} Caution advised if topical alclometasone is used.^{c d}

Pediatric Use

Safety and efficacy not established in children <1 year of age.^{c d}

Do not use for the treatment of diaper dermatitis; tight-fitting diapers or plastic pants should not be used on a child being treated with alclometasone in the diaper area, since such garments may constitute occlusive dressings.^{c d}

Children are more susceptible to topical corticosteroid-induced HPA-axis suppression and Cushing's syndrome than mature individuals because of a greater skin surface area-to-body weight ratio, especially when topical corticosteroids are applied to >20% of body surface area.^{c d} The risk of adrenal suppression appears to increase with decreasing age.^b (See Systemic Effects under Cautions.)

Manifestations of adrenal suppression in children include linear growth retardation, delayed weight gain, low plasma cortisol concentrations, and lack of response to corticotropin (ACTH) stimulation.^{b c d}

Children also are at greater risk of glucocorticoid insufficiency during and/or after withdrawal of treatment.^{b c d}

Intracranial hypertension has occurred in children; manifestations include bulging fontanelles, headaches, and bilateral papilledema.^{b c d}

Striae have been reported in children treated inappropriately with topical corticosteroids.^{b c d}

Topical corticosteroid therapy in children should be limited to the minimum amount necessary for therapeutic efficacy; chronic topical corticosteroid therapy may interfere with growth and development.^b

Geriatric Use

Response in limited number of patients ≥65 years of age does not appear to differ from that in younger adults.^{c d}

Common Adverse Effects

Burning, itching, erythema, irritation,, dryness, papular rash, folliculitis, acneiform eruptions, hypopigmentation^c , perioral dermatitis, allergic contact dermatitis, secondary infection, skin atrophy, striae, miliaria.^{c d}

Interactions for Alclometasone Dipropionate

Specific Drugs and Laboratory Tests

Drug or Test	Interaction
Nitroblue-tetrazolium test for bacterial infection	Concurrent use of corticosteroids reportedly may result in false-negative resultsb

Alclometasone Dipropionate Pharmacokinetics

Absorption

Bioavailability

Topically applied alclometasone can be absorbed through normal intact skin.^{4 22 b c d}

Percutaneous penetration varies among individuals¹⁴ and can be altered by using occlusive dressings,^{1 4 16 17 d} high corticosteroid concentrations, and certain vehicles.^{1 15 16 b d}

Only minimal amounts of topical corticosteroid reach the dermis and subsequently the systemic circulation after application to most normal skin areas; more absorption occurs from the scrotum, axilla, eyelid, face, and scalp than from the forearm, knee, elbow, palm, and sole.^b

Absorption is markedly increased by loss of the skin’s keratin layer and by inflammation and/or diseases of the epidermal barrier (e.g., psoriasis, eczema).^{1 16 17 b d}

Distribution

Extent

Not known whether topical alclometasone is distributed into milk.^{c d}

Elimination

Metabolism

Once absorbed through the skin, topically applied corticosteroids are metabolized primarily in the liver.^{22 b}

Elimination Route

Topical corticosteroids and metabolites are excreted by the kidneys and, to a lesser extent, in bile.^{1 22}

Stability

Storage

Topical

Cream and ointment: 2–30°C.¹ Some manufacturers state 20–25°C.^d Consult product information for specific recommendations.

ActionsActions

• 
  

  Precise mechanism of action for topical anti-inflammatory activity is unknown; therapeutic benefit in the management of corticosteroid-responsive dermatoses mediated primarily through anti-inflammatory, antipruritic, and vasoconstrictive actions.^{c d}

  
  


• 
  

  Anti-inflammatory effects may occur through induction of phospholipase A₂ inhibitory proteins (lipocortins); decreased arachidonic acid release from membrane phospholipids.^d Decreased arachidonic acid precursors may downregulate biosynthesis of potent inflammatory mediators (e.g., prostaglandins, leukotrienes).^d

  
  


• 
  

  Decreases inflammation by stabilizing leukocyte lysosomal membranes, preventing release of destructive acid hydrolases from leukocytes; inhibiting macrophage accumulation in inflamed areas; reducing leukocyte adhesion to capillary endothelium; reducing capillary wall permeability and edema formation; decreasing complement components; antagonizing histamine activity and release of kinin from substrates; reducing fibroblast proliferation, collagen deposition, and subsequent scar tissue formation; and possibly by other mechanisms as yet unknown.^b

  
  

Advice to Patients

• 
  

  Importance of using only as directed, only for the disorder for which it was prescribed, and for no longer than prescribed; avoid contact with the eyes and only apply externally as directed.^{c d} (See Topical Administration under Dosage and Administration.)

  
  


• 
  

  Importance of not applying on the face, underarms, or groin unless directed by clinician.^{c d}

  
  


• 
  

  Importance of informing patients that treated areas of the skin should not be bandaged or otherwise covered or wrapped as to be occlusive unless directed by a clinician.^{c d}

  
  


• 
  

  Importance of reporting any local adverse reactions, especially those occurring under occlusive bandage, to a clinician.^{b c d}

  
  


• 
  

  Importance of informing parents of children not to use in the treatment of diaper dermatitis and not to apply in the diaper area as diapers or plastic pants may constitute occlusive dressings.^{c d}

  
  


• 
  

  Importance of discontinuing use when control is achieved; importance of contacting clinician if no improvement is seen in 2 weeks.^{c d}

  
  


• 
  

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

  
  


• 
  

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

  
  


• 
  

  Importance of advising patients of other important precautionary information. (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

Alclometasone Dipropionate

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Topical	Cream	0.05%*	Alclometasone Dipropionate Cream (with propylene glycol)	Fougera, Taro
			Aclovate (with propylene glycol)	GlaxoSmithKline
	Ointment	0.05%*	Alclometasone Dipropionate Ointment	Fougera, Taro
			Aclovate (with propylene glycol)	GlaxoSmithKline

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 January 2008. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1. Glaxo Inc. Aclovate prescribing information. Research Triangle Park, NC; 1986 Sep.

2. Windholz M, ed. The Merck index. 10th ed. Rahway, NJ: Merck & Co, Inc; 1983:34.

3. Cornell RC, Stoughton RB. Correlation of the vasoconstriction assay and clinical activity in psoriasis. Arch Dermatol. 1985; 121:63-7. [IDIS 195066] [PubMed 3881088]

4. Thornfeldt C, Cornell RC, Stoughton RB. The effect of alclometasone dipropionate cream 0.05% on the hypothalamic-pituitary-adrenal axis of normal volunteers. J Int Med Res. 1985; 13:276-80. [PubMed 4054428]

5. Lassus A. Clinical comparison of alclometasone dipropionate cream 0.05% with hydrocortisone butyrate cream 0.1% in the treatment of atopic dermatitis in children. J Int Med Res. 1983; 11:315-9. [PubMed 6357892]

6. Bagatell FK, Barkoff JR, Cohen HJ et al. A multicenter comparison of alclometasone dipropionate cream 0.05% and hydrocortisone cream 1.0% in the treatment of atopic dermatitis. Curr Ther Res. 1983; 33:46-52.

7. Cornell RC. Atrophogenic potential of alclometasone dipropionate ointment 0.05% vs hydrocortisone ointment 1.0%. Curr Ther Res. 1986; 39:260-8.

8. Kalivas J, Kanof NB, Miller OF III et al. A controlled clinical comparison of alclometasone dipropionate cream 0.05% and hydrocortisone cream 1.0% in patients with psoriasis. Curr Ther Res. 1983; 33:408-14.

9. Aggerwal A, Maddin S. Alclometasone dipropionate in psoriasis: a clinical study. J Int Med Res. 1982; 10:414-8. [PubMed 7152079]

10. Frost P. Clinical comparison of alclometasone dipropionate and desonide ointments (0.05%) in the management of psoriasis. J Int Med Res. 1982; 10:375-8. [PubMed 6754511]

11. Lassus A. Alclometasone dipropionate cream 0.05% versus clobetasone butyrate cream 0.05%: a controlled clinical comparison in the treatment of atopic dermatitis in children. Int J Dermatol. 1984; 23:565-6. [PubMed 6389385]

12. Green MJ, Berkenkopf J, Xiomara F et al. Synthesis and structure-activity relationships in a novel series of topically active corticosteroids. J Steroid Biochem. 1979; 11:61-6. [PubMed 491605]

13. Duke EE, Maddin S, Aggerwal A. Alclometasone dipropionate in atopic dermatitis: a clinical study. Curr Ther Res. 1983; 33:769-74.

14. Crespi HG. Topical corticosteroid therapy for children: alclometasone dipropionate cream 0.05%. Clin Ther. 1986; 8:203-10. [PubMed 2938740]

15. Cornell RC, Stoughton RB. The use of topical steroids in psoriasis. Dermatol Clin. 1984; 2:397-409.

16. Cornell RC, Stoughton RB. Use of glucocorticosteroids in psoriasis. Pharmacol Ther. 1980; 2:497-508.

17. Food and Drug Administration. Topical corticosteroids class labeling guideline. (Undated.) Available from: Professional Labeling Branch, Division of Drug Advertising and Labeling, Food and Drug Administration, Rockville, MD.

18. Mobacken H, Hersle K. Alclometasone dipropionate ointment 0.05% versus hydrocortisone ointment 1.0% in children with eczema. Acta Ther. 1986; 12:269-78.

19. Green MJ, Shue HJ, Tiberi R et al. The influence of esterification on the topical antiinflammatory activity of 7 alpha-chloro- and 7 alpha-bromo-16 alpha-methylprednisolones. Arzneimittelforschung. 1980; 30:1618-20. [PubMed 7192095]

20. Lutsky BN, Berkenkopf J, Fernandez X et al. Selective effects of 7 alpha-halogeno substitution on corticosteroid activity: Sch 22219 and Sch 23409. Arzneimittelforschung. 1979; 29:992-8. [PubMed 583002]

21. Lutsky BN, Berkenkopf J, Fernandez X et al. A novel class of potent topical antiinflammatory agents: 17-benzoylated, 7 alpha-halogeno substituted corticosteroids. Arzneimittelforschung. 1979; 29:1662-7. [PubMed 543873]

22. Vonderweidt J (Glaxo, Research Triangle Park, NC): Personal communication; 1987 Apr 15.

23. Reviewers’ comments (personal observations); 1987 Apr.

24. Tokiwa T, Oyama T, Kimura S et al. [Studies on the primary dermal irritation, ocular mucosa irritation and local anaesthetic effect of alclometasone dipropionate (ADP)]. (Japanese; with English abstract.) Oyo Yakuri. 1986; 32:937-43.

25. Fujii K, Uda F, Yamamoto K. [Phototoxicity and photosensitivity tests of alclometasone dipropionate (ADP).] (Japanese; with English abstract.) Oyo Yakuri. 1986; 32:945-51.

26. Hasegawa T, Tujita K, Fujino A et al. [Immunogenicity study on alclometasone dipropionate (ADP)]. (Japanese; with English abstract.) Oyo Yakuri. 1986; 32:953-60.

27. Sills J (Schering, Kenilworth, NJ): Personal communication; 1987 May 28.

28. Lechner D (Schering, Kenilworth, NJ): Personal communication; 1987 June 3.

a. AHFS drug information 2007. McEvoy GK, ed. Alclometasone dipropionate. Bethesda, MD: American Society of Health-Systems Pharmacists; 2007: 3525–6.

b. AHFS drug information 2007 McEvoy GK, ed. Topical corticosteroids general statement. Bethesda, MD: American Society of Health-System Pharmacists; 2007:3423–5.

c. GlaxoSmithKline. Aclovate (alclometasone dipropionate) cream and ointment 0.05% prescribing information. Pittsburgh, PA; 2002 Aug.

d. Taro Pharmaceuticals. Alclometasone dipropionate ointment USP, 0.05% prescribing information. Hawthorne, NY; 2004 Jul.

More Alclometasone Dipropionate resources

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

• Aclovate Prescribing Information (FDA)


• Aclovate Concise Consumer Information (Cerner Multum)


• Aclovate Cream MedFacts Consumer Leaflet (Wolters Kluwer)

Compare Alclometasone Dipropionate with other medications

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Indobufene EG

Indobufene EG may be available in the countries listed below.

Ingredient matches for Indobufene EG

Indobufen

Indobufen is reported as an ingredient of Indobufene EG in the following countries:

• Italy

International Drug Name Search

toremifene

Generic Name: toremifene (tor EH mih feen)

Brand Names: Fareston

What is toremifene?

Toremifene blocks estrogen from reaching cancer cells. Certain types of breast cancer require estrogen to grow.

Toremifene is used to slow the growth of metastatic breast cancer (cancer that has spread from the original tumor). Unlike chemotherapy, toremifene does not actually destroy cancer cells.

Toremifene may also be used for purposes not listed in this medication guide.

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

Do not use toremifene if you are pregnant. It could harm the unborn baby. You should not use toremifene if you are allergic to it, or if you have a history of Long QT syndrome, or an uncontrolled electrolyte imbalance (low levels of potassium or magnesium in your blood).

Before you take toremifene, tell your doctor if you have endometrial hyperplasia (overgrowth of cells lining the uterus), bone cancer, or if you have ever had a blood clot.

Taking toremifene may increase your risk of developing endometrial hyperplasia, a condition that may lead to cancer of the uterus. Talk to your doctor about your individual risk. Stop using toremifene and call your doctor at once if you have symptoms of a serious heart rhythm disorder (severe dizziness, fainting, fast or pounding heartbeats) or signs of high levels of calcium in your blood (nausea, vomiting, stomach pain, loss of appetite, constipation, increased thirst or urination, muscle pain or weakness, joint pain, confusion, and feeling tired or restless).

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

You should not use toremifene if you are allergic to it, or if you have:

• 
  

  a history of Long QT syndrome; or

  
  


• 
  

  an uncontrolled electrolyte imbalance (low levels of potassium or magnesium in your blood).

  
  

To make sure you can safely take toremifene, tell your doctor if you have any of these other conditions:

• 
  

  endometrial hyperplasia (overgrowth of cells lining the uterus);

  
  


• 
  

  bone cancer; or

  
  


• 
  

  if you have ever had a blood clot.

  
  

FDA pregnancy category D. Do not use toremifene if you are pregnant. It could harm the unborn baby. Use effective birth control if you are not past menopause, and tell your doctor if you become pregnant during treatment. It is not known whether toremifene passes into breast milk or if it could harm a nursing baby. You should not breast-feed while you are using toremifene. Taking toremifene may increase your risk of developing endometrial hyperplasia, a condition that may lead to cancer of the uterus. Talk to your doctor about your individual risk.

How should I take toremifene?

Take exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.

Toremifene is usually taken once a day. Follow your doctor's instructions.

You may take toremifene with or without food. Take the medicine at the same time each day.

To be sure this medicine is not causing harmful effects, your blood will need to be tested often. Your liver function may also need to be tested. Visit your doctor regularly. Store at room temperature away from moisture, heat, and light.

See also: Toremifene dosage (in more detail)

What happens if I miss a dose?

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Overdose symptoms may include severe forms of some of the side effects listed in this medication guide.

What should I avoid while taking toremifene?

Grapefruit and grapefruit juice may interact with toremifene and lead to potentially dangerous effects. Discuss the use of grapefruit products with your doctor.

Toremifene side effects

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat. Stop using toremifene and call your doctor at once if you have a serious side effect such as:

• 
  

  severe dizziness, fainting, fast or pounding heartbeats, seizure (convulsions);

  
  


• 
  

  nausea, vomiting, stomach pain, loss of appetite, constipation, increased thirst or urination, muscle pain or weakness, joint pain, confusion, and feeling tired or restless;

  
  


• 
  

  easy bruising, unusual bleeding, purple or red pinpoint spots under your skin;

  
  


• 
  

  vaginal bleeding or discharge;

  
  


• 
  

  chest pain or heavy feeling, pain spreading to the arm or shoulder, nausea, sweating, general ill feeling;

  
  


• 
  

  sudden numbness or weakness, especially on one side of the body;

  
  


• 
  

  chest pain, sudden cough, wheezing, rapid breathing, coughing up blood;

  
  


• 
  

  pain, swelling, warmth, or redness in one or both legs;

  
  


• 
  

  blurred vision, eye pain, or seeing halos around lights;

  
  


• 
  

  jaundice (yellowing of the skin or eyes);

  
  


• 
  

  tremor; or

  
  


• 
  

  loss of movement in any part of your body.

  
  

Less serious side effects may include:

• 
  

  sweating, hot flashes;

  
  


• 
  

  mild nausea, constipation;

  
  


• 
  

  dizziness, spinning sensation;

  
  


• 
  

  depressed mood;

  
  


• 
  

  swelling in your hands or feet;

  
  


• 
  

  itching, skin discoloration; or

  
  


• 
  

  hair loss.

  
  

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Toremifene Dosing Information

Usual Adult Dose for Breast Cancer:

For the treatment of metastatic breast cancer in postmenopausal women with estrogen-receptor positive or unknown tumors: 60 mg orally once a day.

What other drugs will affect toremifene?

Tell your doctor about all other medicines you use, especially:

• 
  

  arsenic trioxide (Trisenox);

  
  


• 
  

  isoniazid (for treating tuberculosis);

  
  


• 
  

  lithium (Eskalith, Lithobid);

  
  


• 
  

  St. John's wort;

  
  


• 
  

  tacrolimus (Prograf);

  
  


• 
  

  vitamin or mineral supplements that contain calcium or vitamin D;

  
  


• 
  

  warfarin (Coumadin, Jantoven);

  
  


• 
  

  an antibiotic such as clarithromycin (Biaxin), erythromycin (E.E.S., EryPed, Ery-Tab, Erythrocin, Pediazole), levofloxacin (Levaquin), ofloxacin (Floxin), rifabutin (Mycobutin), rifampin (Rifadin, Rifater, Rifamate), telithromycin (Ketek), and others;

  
  


• 
  

  an antidepressant such as amitriptylline (Elavil, Vanatrip, Limbitrol), venlafaxine (Effexor), nefazodone, and others;

  
  


• 
  

  antifungal medication such as itraconazole (Sporanox), ketoconazole (Nizoral), voriconazole (Vfend), and others;

  
  


• 
  

  seizure medicine such as carbamazepine (Carbatrol, Tegretol), clonazepam (Klonopin), phenobarbital (Solfoton), or phenytoin (Dilantin);

  
  


• 
  

  a diuretic (water pill) such as chlorothiazide (Diuril), hydrochlorothiazide (HCTZ, HydroDiuril, Hyzaar, Lopressor HCT, Vasoretic, Zestoretic), chlorthalidone (Hygroton, Thalitone), indapamide (Lozol), metolazone (Mykrox, Zaroxolyn), and others;

  
  


• 
  

  heart or blood pressure medication such as diltiazem (Cartia, Cardizem), nicardipine (Cardene), verapamil (Calan, Covera, Isoptin, Verelan), and others;

  
  


• 
  

  heart rhythm medicine such as amiodarone (Cordarone, Pacerone), dofetilide (Tikosyn), disopyramide (Norpace), ibutilide (Corvert), procainamide (Procan, Pronestyl), quinidine (Quin-G), sotalol (Betapace), and others;

  
  


• 
  

  HIV/AIDS medicine such as atazanavir (Reyataz), indinavir (Crixivan), nelfinavir (Viracept), saquinavir (Invirase), ritonavir (Norvir, Kaletra), and others;

  
  


• 
  

  medicine to prevent or treat nausea and vomiting such as granisetron (Kytril) or ondansetron (Zofran);

  
  


• 
  

  medicines to treat psychiatric disorders, such as haloperidol (Haldol), thioridazine (Mellaril), and others;

  
  


• 
  

  migraine headache medicine such as sumatriptan (Imitrex, Treximet) or zolmitriptan (Zomig); or

  
  


• 
  

  narcotic medication such as methadone (Methadose, Diskets, Dolophine).

  
  

This list is not complete and there are many other drugs that can interact with toremifene. Tell your doctor about all medications you use. This includes prescription, over-the-counter, vitamin, and herbal products. Do not start a new medication without telling your doctor. Keep a list of all your medicines and show it to any healthcare provider who treats you.

More toremifene resources

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

• toremifene Advanced Consumer (Micromedex) - Includes Dosage Information


• Toremifene MedFacts Consumer Leaflet (Wolters Kluwer)


• Fareston Prescribing Information (FDA)


• Fareston Monograph (AHFS DI)

Compare toremifene with other medications

• Breast Cancer
• Breast Cancer, Metastatic

Where can I get more information?

• Your pharmacist can provide more information about toremifene.

See also: toremifene side effects (in more detail)

Nicotine Lozenges

Pronunciation: NIK-oh-teen
Generic Name: Nicotine
Brand Name: Commit

Nicotine Lozenges are used for:

Helping you to quit smoking.

Nicotine Lozenges are a smoking deterrent. It works by providing low levels of nicotine, which may help you to quit smoking by lessening the physical symptoms of withdrawal.

Do NOT use Nicotine Lozenges if:

• you are allergic to any ingredient in Nicotine Lozenges


• you have had a recent heart attack


• you have severe or worsening chest pain or a severely irregular heartbeat


• you continue to smoke, chew tobacco, use snuff, or use any other nicotine-containing products

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

Before using Nicotine Lozenges:

Some medical conditions may interact with Nicotine Lozenges. 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 are on a low-sodium diet or if you have phenylketonuria (PKU)


• if you have chest pain (eg, angina), heart problems (eg, coronary artery disease, irregular heartbeat), high blood pressure, or you have had a heart attack


• if you have an ulcer, diabetes, an overactive thyroid, blood vessel problems (eg, Buerger disease, Raynaud phenomena), or an adrenal gland tumor (pheochromocytoma)


• if you take medicine for asthma or depression, or if you are using another medicine to stop smoking

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

• Acetaminophen, adrenergic antagonists (eg, prazosin), beta-blockers (eg, labetalol, propranolol), caffeine, insulin, oxazepam, pentazocine, theophylline, or tricyclic antidepressants (eg, imipramine) because the risk of their side effects may be increased when you stop smoking


• Adrenergic agonists (eg, isoproterenol, phenylephrine) because their effectiveness may be decreased when you stop smoking

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

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

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


• Do not eat or drink for 15 minutes before taking Nicotine Lozenges or when it is in your mouth.


• Do NOT chew or swallow the lozenge whole. Place the lozenge in your mouth and allow it to slowly dissolve. Occasionally move the lozenge from one side of your mouth to the other. Try not to swallow very often while Nicotine Lozenges are dissolving. It may take 20 to 30 minutes for Nicotine Lozenges to completely dissolve.


• To improve your chances of quitting smoking, take at least 9 lozenges per day for the first 6 weeks unless your doctor tells you otherwise.


• Do not take more than 1 lozenge at a time or continuously take one lozenge after another. Hiccups, heartburn, nausea, or other effects may occur.


• Do NOT take more than 5 lozenges in 6 hours. Do NOT take more than 20 lozenges each day.


• If you cannot finish a lozenge, wrap it in paper and dispose of it in the trash out of the reach of children and away from pets.


• If you miss a dose of Nicotine Lozenges, take it as soon as you remember. Continue to take it as directed by your doctor or on the package label.

Ask your health care provider any questions you may have about how to use Nicotine Lozenges.

Important safety information:

• The dose of Nicotine Lozenges that you take is determined by how soon after waking you would normally smoke your first cigarette of the day. If you are not sure what dose of Nicotine Lozenges to take, ask your doctor or pharmacist.


• Do not smoke or use tobacco products while taking Nicotine Lozenges.


• Do NOT use Nicotine Lozenges for longer than 12 weeks. If you still feel the need to take Nicotine Lozenges after 12 weeks, check with your doctor.


• Nicotine Lozenges should be used as part of a larger program to help you stop smoking. If you need help choosing a program, talk with your health care provider.


• Some of these products contain phenylalanine. If you must have a diet that is low in phenylalanine, ask your pharmacist if it is in your product.


• Do not use Nicotine Lozenges in CHILDREN younger than 18 years old without first talking with the child's doctor.


• PREGNANCY and BREAST-FEEDING: Nicotine Lozenges may cause harm to the fetus. If you become pregnant, contact your doctor. You will need to discuss the benefits and risks of taking Nicotine Lozenges while you are pregnant. Nicotine Lozenges are found in breast milk. If you are or will be breast-feeding while you take Nicotine Lozenges, check with your doctor. Discuss any possible risks to your baby.

When used for long periods of time or at high doses, some people develop a need to continue taking Nicotine Lozenges. This is known as DEPENDENCE or addiction.

Do not suddenly stop taking Nicotine Lozenges without your doctor's approval. Stopping Nicotine Lozenges suddenly may cause serious WITHDRAWAL symptoms. These may include anxiety, craving, impaired concentration, increased appetite, irritability, nervousness, sleep disturbances, and weight gain.

Possible side effects of Nicotine Lozenges:

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:

Warm or tingling sensation in the mouth.

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); fast or irregular heartbeat; mouth problems (eg, mouth pain, sores, or swelling); persistent indigestion; severe sore throat.

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: Nicotine 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 cold and clammy skin; confusion; diarrhea; difficulty breathing; dizziness; excessive drooling; fainting; fast, weak, or irregular heartbeat; headache; hearing and vision problems; nausea; seizures; stomach pain; sweating; tremor; vomiting; weakness.

Proper storage of Nicotine Lozenges:

Store Nicotine Lozenges at room temperature, between 68 and 77 degrees F (20 and 25 degrees C). Store away from heat, moisture, and light. Store Nicotine Lozenges in the original blister pack. Once removed from the blister, use immediately. Do not store in the bathroom. Keep Nicotine Lozenges out of the reach of children and away from pets.

General information:

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


• Nicotine Lozenges are 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 Nicotine Lozenges. 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 Nicotine resources

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

Compare Nicotine with other medications

• Smoking Cessation

Exelon

Generic Name: Rivastigmine
Class: Parasympathomimetic (Cholinergic) Agents
VA Class: CN900
Chemical Name: (S)-3-[1-(Dimethylamino)ethyl]phenyl ethylmethylcarbamate
Molecular Formula: C₁₄H₂₂N₂O₂C₁₄H₂₂N₂O₂•2C₄H₆O₆
CAS Number: 123441-03-2

Introduction

A centrally active, reversible cholinesterase inhibitor.^{1 3 4 5 6 7 8 9 10 11 12 17}

Uses for Exelon

Alzheimer’s Disease

Management of mild to moderate dementia of the Alzheimer’s type.^{1 3 4 5 6 9 17}

Dementia Associated with Parkinson's Disease

Management of mild to moderate dementia associated with Parkinson's disease.^{1 15 16 17}

Exelon Dosage and Administration

Administration

Administer rivastigmine tartrate orally.¹

Administer rivastigmine percutaneously by topical application of a transdermal system.¹⁷

Oral Administration

Administer orally twice daily (morning and evening) with food.^{1 3 4 8 10 12} (See Absorption under Pharmacokinetics.)

Administer oral solution using the oral dosing syringe provided; follow the patient instructions provided by the manufacturer.¹ Oral solution may be mixed in a small glass of compatible fluids (see Compatibility under Stability); mix completely and drink the entire contents.¹

Oral solution and capsules may be interchanged at equal doses.¹

Transdermal Administration

Expose the adhesive surface of the system by peeling and discarding the protective liner prior to administration.¹⁷

Apply transdermal system to dry, hairless area of intact skin on the back by firmly pressing the system with the adhesive side touching the skin.¹⁷ Placement on the back is recommended to reduce the risk that the system could be removed by the patient.¹⁷ Alternatively, apply to upper arm or chest.¹⁷ Application site should not be red, irritated, or cut.¹⁷ Avoid application at areas where the system could be rubbed off.¹⁷

The transdermal system is worn continuously for 24 hours; apply subsequent systems after removal of the previous system.¹⁷

To minimize and/or prevent potential skin irritation, apply each transdermal system at a different site, with ≥14 days between applications to a particular site.¹⁷

If system inadvertently comes off, apply a new system; continue the application schedule employed.¹⁷

Dosage

Capsules, oral solution: Available as rivastigmine tartrate; dosage is expressed in terms of rivastigmine.¹

Transdermal: Available as rivastigmine; dosage is expressed in terms of rivastigmine.¹⁷

Adults

Alzheimer’s Disease

Oral

Initially, 1.5 mg twice daily.^{1 3 4 8}

If well tolerated, increase dosage after ≥2 weeks to 3 mg twice daily;^{1 4 12} attempt to increase dosage to 4.5 mg twice daily and 6 mg twice daily after ≥2 weeks of treatment at the previous dosage.^{1 4}

If adverse effects intolerable, discontinue for several doses and then resume at the same or the immediately preceding (lower) dosage in the titration regimen.^{1 4} However, if therapy is interrupted for more than several days, restart drug using the recommended initial dosage (i.e., 1.5 mg twice daily) and titration schedule until the previous maintenance dosage is reached (to decrease the risk of severe vomiting and related sequelae [e.g., spontaneous esophageal rupture]). (See GI Effects under Cautions.)¹

Transdermal

Initiate with one system delivering 4.6 mg/24 hours once daily.¹⁷

If well tolerated, increase dosage after ≥4 weeks to one system delivering 9.5 mg/24 hours once daily.¹⁷

If adverse effects intolerable, discontinue for several doses and then resume at the same dosage or the immediately preceding (lower) dosage in the titration regimen.¹⁷ However, if therapy is interrupted for more than several days, restart the drug using the recommended initial dosage (i.e., one system delivering 4.6 mg/24 hours once daily) and titration schedule (to decrease the risk of severe vomiting and related sequelae [e.g., spontaneous esophageal rupture]).¹⁷ (See GI Effects under Cautions.)

Transferring from Oral to Transdermal Therapy¹⁷

Transdermal

Daily Dosage of Rivastigmine Capsules or Oral Solution	Initial Dosage of Transdermal Rivastigmine
<6 mg	One system delivering 4.6 mg/24 hours
6–12 mg	One system delivering 9.5 mg/24 hours

Apply the first transdermal system the day following the last oral rivastigmine dose.¹⁷

Dementia Associated with Parkinson's Disease

Oral

Initially, 1.5 mg twice daily.¹

If well tolerated, increase dosage after ≥4 weeks to 3 mg twice daily;^{1 15} attempt to increase dosage to 4.5 mg twice daily and 6 mg twice daily after ≥4 weeks of treatment at the previous dosage.^{1 15}

If adverse effects intolerable, discontinue for several doses and then resume at the same or the immediately preceding (lower) dosage in the titration regimen.¹ However, if therapy is interrupted for more than several days, restart drug using the recommended initial dosage (i.e., 1.5 mg twice daily) and titration schedule until the previous maintenance dosage is reached (to decrease the risk of severe vomiting and related sequelae [e.g., spontaneous esophageal rupture]).¹ (See GI Effects under Cautions.)

Transdermal

Initiate with one system delivering 4.6 mg/24 hours once daily.¹⁷

If well tolerated, increase dosage after ≥4 weeks to one system delivering 9.5 mg/24 hours once daily.¹⁷

If adverse effects intolerable, discontinue for several doses and then resume at the same dosage or the immediately preceding (lower) dosage in the titration regimen.¹⁷ However, if therapy is interrupted for more than several days, restart the drug using the recommended initial dosage (i.e., one system delivering 4.6 mg/24 hours once daily) and titration schedule (to decrease the risk of severe vomiting and related sequelae [e.g., spontaneous esophageal rupture]).¹⁷ (See GI Effects under Cautions.)

Transferring from Oral to Transdermal Therapy¹⁷

Transdermal

Daily Dosage of Rivastigmine Capsules or Oral Solution	Initial Dosage of Transdermal Rivastigmine
<6 mg	One system delivering 4.6 mg/24 hours
6–12 mg	One system delivering 9.5 mg/24 hours

Apply the first transdermal system the day following the last oral rivastigmine dose.¹⁷

Prescribing Limits

Adults

Alzheimer’s Disease

Oral

Maximum 6 mg twice daily.^{1 3 4}

Transdermal

Maximum one system delivering 9.5 mg/24 hours once daily.¹⁷

Dementia Associated with Parkinson's Disease

Oral

Maximum 6 mg twice daily.¹

Transdermal

Maximum one system delivering 9.5 mg/24 hours once daily.¹⁷

Special Populations

Hepatic Impairment

Decreased clearance following oral administration;^{1 17} however, dosage adjustment may not be necessary since dosage is titrated to adverse effect tolerability.^{1 17}

Renal Impairment

Clearance decreased with moderate impairment and increased with severe impairment following oral administration;^{1 17} however, dosage adjustment may not be necessary since dosage is titrated to adverse effect tolerability.^{1 17}

Cautions for Exelon

Contraindications

• 
  

  Known hypersensitivity to rivastigmine,^{1 17} other carbamates,^{1 12 17} or any ingredient in the formulation.^{1 17}

  
  

Warnings/Precautions

Warnings

GI Effects

Possible occurrence of clinically important adverse GI effects, including nausea, vomiting, diarrhea, anorexia, and weight loss.^{1 3 5 6 17}

Severe vomiting and spontaneous rupture of the esophagus were reported in a patient who resumed therapy by taking a single 4.5-mg oral dose after therapy had been interrupted for 8 weeks.^{1 12 13 14 17} Therefore, manufacturer recommends strict adherence to prescribed initial dosages and titration schedules (see Alzheimer’s Disease under Dosage and Administration), particularly when reinitiating therapy following temporary interruption lasting longer than several days.^{1 12 13 17}

Possible increased gastric acid secretion.^{1 17} Monitor closely for manifestations of active or occult GI bleeding, especially in patients at increased risk (e.g., history of ulcer disease, concomitant NSAIA therapy⁸ ).^{1 4 17}

Cardiovascular Effects

Possible bradycardia or other vagotonic effects on the heart.^{1 17} Use with caution in patients with sick sinus syndrome or other supraventricular cardiac conduction abnormalities.^{1 17}

Genitourinary Effects

Potential urinary obstruction secondary to cholinergic activity.^{1 4 17}

Nervous System Effects

Possible increased risk of seizures secondary to cholinergic activity or possibly as a manifestation of Alzheimer’s disease.^{1 4 17}

Respiratory Effects

Use with caution in patients with a history of asthma or obstructive pulmonary disease.^{1 17}

General Precautions

Extrapyramidal Reactions

May exacerbate or induce extrapyramidal symptoms.^{1 15 17} Worsening in patients with Parkinson’s disease, including an increased incidence or intensity of tremor, reported.^{1 15 17}

Effects on Ability to Drive and Use Heavy Machinery

Dementia or adverse effects of rivastigmine may impair ability to drive or operate heavy machinery; ability should be evaluated by the treating clinician on a routine basis.¹⁷

Low-weight Individuals

Transdermal system: Patients with body weight <50 kg may experience more adverse effects and may be more likely to discontinue therapy due to adverse effects.¹⁷ Exercise caution if dosage exceeds the maximum recommended daily dose.¹⁷ (See Plasma Concentrations under Pharmacokinetics.)

Specific Populations

Pregnancy

Category B.^{1 17}

Lactation

Not known whether rivastigmine is distributed into milk.^{1 17} Use is not recommended.^{1 17}

Pediatric Use

Safety and efficacy not established in children.^{1 17}

Geriatric Use

Decreased oral clearance; however, clinical outcome of therapy not predicted by age.¹

Common Adverse Effects

Nausea, vomiting, diarrhea, anorexia, dyspepsia, asthenia.^{1 17}

Interactions for Exelon

Minimally metabolized by CYP isoenzymes.^{1 3 4 5 6 7 8 10 11 17} Pharmacokinetic interaction unlikely with drugs metabolized by CYP isoenzymes or with CYP enzyme inducers or inhibitors.^{1 4 8 11 17}

Protein-bound Drugs

Pharmacokinetic interaction unlikely.^{10 11 12}

Specific Drugs

Drug	Interaction
Anticholinergics	Antagonistic effects1 17
Cholinomimetics and other cholinesterase inhibitors	Additive effects1 17
Muscle relaxants (succinylcholine-type)	Exaggerated response to muscle relaxant during surgery1 17
Nicotine	Increased rivastigmine clearance1 17

Exelon Pharmacokinetics

Absorption

Bioavailability

Oral: Rivastigmine is rapidly and completely absorbed from the GI tract.¹ Absolute bioavailability is approximately 36–40%.¹ Peak plasma concentrations attained in approximately 1 hour following oral administration.^{1 19}

Transdermal system: Peak plasma concentrations attained in approximately 8 hours.^{17 19}

At steady-state, rivastigmine exposure (AUC_24h) in individuals receiving a transdermal system delivering 9.5 mg/24 hours was approximately the same as that achieved in individuals receiving the 6-mg capsule twice daily.^{17 19}

Food

Oral: Food delays absorption by 90 minutes, lowers peak plasma concentration by approximately 30%, and increases extent of absorption by approximately 30%.¹

Plasma Concentrations

High peak plasma concentrations possibly associated with adverse GI effects (e.g., nausea, vomiting).^{1 3 4 8 10 12} Peak plasma concentrations achieved following administration of a transdermal system delivering 9.5 mg/24 hours were approximately 70% lower than concentrations achieved following oral administration of 6 mg twice daily.¹⁹

In low-weight individuals (weight 35 kg), plasma concentrations are substantially increased compared with normal-weight individuals (weight 65 kg).¹⁷

Distribution

Extent

Widely distributed throughout the body; peak CSF concentrations attained within 1.4–2.6 hours.^{1 17} Not known whether rivastigmine is distributed into milk.^{1 17}

Plasma Protein Binding

About 40%.^{1 17}

Elimination

Metabolism

Rapidly and extensively metabolized, principally via cholinesterase-mediated hydrolysis to the decarbamylated metabolite.^{1 17} CYP enzyme system is minimally involved in metabolism.^{1 17}

Elimination Route

Excreted principally in urine as metabolites.^{1 17}

Half-life

Oral administration: Approximately 1.3–2 hours.^{1 19}

Transdermal system: Approximately 3.4 hours.^{17 19}

Special Populations

In patients with mild to moderate hepatic impairment, oral clearance reduced 60–65%.^{1 17}

Mean oral clearance reduced 64% in patients with moderate renal impairment but increased 43% in those with severe renal impairment.^{1 17}

Stability

Storage

Oral

Capsules

Tight containers at 25°C (may be exposed to 15–30°C).¹

Solution

25°C (may be exposed to 15–30°C); do not freeze.¹ Keep container in upright position.¹

Transdermal

Store in individual sealed packages at 25°C (may be exposed to 15–30°C).¹⁷

Compatibility

For information on systemic interactions resulting from concomitant use, see Interactions.

Oral

Solution

May be mixed with a small glass of water, cold fruit juice, or soda.¹ Do not mix with other liquids.¹

ActionsActions

• 
  

  An intermediate-acting, reversible cholinesterase inhibitor.^{1 3 4 5 6 7 8 9 10 11 12 17} Increases acetylcholine at cholinergic synapses by inactivating cholinesterases, thereby inhibiting hydrolysis of acetylcholine.^{1 3 4 6 7 8 9 10 11 12 17}

  
  


• 
  

  Relatively specific for brain acetylcholinesterase and butyrylcholinesterase.^{3 4 7 8 10}

  
  

Advice to Patients

• 
  

  Importance of clinicians informing caregivers of potential for adverse effects such as nausea, vomiting, anorexia, and weight loss.^{1 17} Importance of caregivers monitoring for adverse effects and informing clinicians if they occur.^{1 17}

  
  


• 
  

  Importance of informing caregivers and patients that rivastigmine may exacerbate or induce extrapyramidal symptoms; worsening in patients with Parkinson’s disease (including increased incidence or intensity of tremor) reported.^{1 15 17}

  
  


• 
  

  Importance of informing caregivers and patients that the ability to drive or use heavy machinery should be evaluated by the treating clinician on a routine basis.¹⁷

  
  


• 
  

  Importance of not administering the next maintenance dosage of rivastigmine until a clinician is consulted if therapy has been interrupted for longer than several days.^{1 17}

  
  


• 
  

  Importance of taking oral formulations of rivastigmine with food.^{1 3}

  
  


• 
  

  Importance of following recommended procedure for administering rivastigmine oral solution and of reviewing the instruction sheet provided by the manufacturer.¹

  
  


• 
  

  Importance of following recommended procedure for administration, removal, and disposal of rivastigmine transdermal systems and of reviewing the instruction sheet provided by the manufacturer.¹⁷

  
  


• 
  

  Importance of informing caregivers and patients to avoid exposure of the transdermal system to external heat sources (e.g., excess sunlight, saunas, solariums) for extended periods of time.¹⁷

  
  


• 
  

  Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.^{1 17}

  
  


• 
  

  Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.^{1 17}

  
  


• 
  

  Importance of informing patients of other important precautionary information.^{1 17} (See Cautions.)

  
  

Preparations

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

Rivastigmine

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Topical	Transdermal System	4.5 mg/24 hours (9 mg/5 cm2)	Exelon	Novartis
		9.5 mg/24 hours (18 mg/10 cm2)	Exelon	Novartis

Rivastigmine Tartrate

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	Capsules	1.5 mg (of rivastigmine)	Exelon	Novartis
		3 mg (of rivastigmine)	Exelon	Novartis
		4.5 mg (of rivastigmine)	Exelon	Novartis
		6 mg (of rivastigmine)	Exelon	Novartis
	Solution	2 mg (of rivastigmine) per mL	Exelon	Novartis

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 03/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Exelon 1.5MG Capsules (NOVARTIS): 60/$266.86 or 180/$770.11

Exelon 3MG Capsules (NOVARTIS): 60/$256.82 or 180/$739.9

Exelon 4.5MG Capsules (NOVARTIS): 60/$258.37 or 180/$740.24

Exelon 4.6MG/24HR Patches (NOVARTIS): 30/$251.99 or 90/$730.94

Exelon 6MG Capsules (NOVARTIS): 60/$256.96 or 180/$740.24

Exelon 9.5MG/24HR Patches (NOVARTIS): 30/$254.98 or 90/$740.98

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 May 2009. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1. Novartis Pharmaceuticals. Exelon (rivastigmine tartrate) capsules and oral solution prescribing information. East Hanover, NJ; 2006 Jun.

3. Jann MW. Rivastigmine, a new-generation cholinesterase inhibitor for the treatment of Alzheimer’s disease. Pharmacotherapy. 2000; 20:1–12.

4. Novartis Pharmaceuticals. Personal communication.

5. Corey-Bloom J, Anand R, Veach J et al. A randomized trial evaluating the efficacy and safety of ENA 713 (rivastigmine tartrate), a new anticholinesterase inhibitor, in patients with mild to moderately severe Alzheimer’s disease. Int J Geriatr Psychopharmacol. 1998; I:55–65.

6. Rösler M, Anand R, Cicin-Sain A et al. Efficacy and safety of rivastigmine in patients with Alzheimer’s disease: international randomised controlled trial. BMJ. 1999; 318:633–8.

7. Schneider LS, Anand R, Farlow MR. Systematic review of the efficacy of rivastigmine for patients with Alzheimer’s disease. Int J Geriatr Psychopharmacol. 1998; I:S26–34.

8. Spencer CM, Noble S. Rivastigmine: a review of its use in Alzheimer’s disease. Drugs Aging. 1998; 13:391–411.

9. Anon. Rivastigmine for Alzheimer’s disease. Drug Ther Bull. 2000; 38:15–6.

10. Polinsky RJ. Clinical pharmacology of rivastigmine: a new-generation acetylcholinesterase inhibitor for the treatment of Alzheimer’s disease. Clin Ther. 1998; 20:634–47.

11. Grossberg GT, Stahelin HB, Messina JC et al. Lack of adverse pharmacodynamic drug interacitons with rivastigmine and twenty-two classes of medications. Int J Geriat Psychiatry. 2000; 15:242–7.

12. Novartis, East Hanover, NJ: Personal Communication.

13. Bess AL, Cunningham SR. Dear healthcare provider letter regarding guidelines for reinitiating rivastigmine therapy. Rockville, MD: US Food and Drug Administration; 2001 Jan 26.

14. Babic T, et al. Spontaneous rupture of oesophagus (Boerhaave’s syndrome) related to rivastigmine. Letter. Age Ageing. 2000; 29:370-1. [PubMed 10985453]

15. Emre M, Aarsland D, Albanese A, et al. Rivastigmine for dementia associated with Parkinson’s disease. N Engl J Med. 2004; 351:2509-18. [PubMed 15590953]

16. Wesnes KA, McKeith I, Edgar C, et al. Benefits of rivastigmine on attention in dementia associated with Parkinson disease. Neurology. 2005; 65:1654-6. [PubMed 16301500]

17. Novartis Pharmaceuticals. Exelon Patch (rivastigmine transdermal system) prescribing information. East Hanover, NJ; 2007 Jul.

18. Winblad B, Cummings J, Andreasen N, et al. A six month double-blind, randomized, placebo-controlled study of a transdermal patch in Alzheimer's disease– rivastigmine patch versus capsule. Int J Geriatr Psychiatry. 2007; 22:456-67. [PubMed 17380489]

19. Lefèvre G, Sedek G, Jhee SS, et al. Pharmacokinetics and pharmacodynamics of the novel daily rivastigmine transdermal patch compared with twice-daily capsules in Alzheimer's disease patients. Clin Pharmacol Ther. 2008; 83:106-14. [PubMed 17522596]

More Exelon resources

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

• Exelon Prescribing Information (FDA)


• Exelon Consumer Overview


• Exelon Advanced Consumer (Micromedex) - Includes Dosage Information


• Exelon MedFacts Consumer Leaflet (Wolters Kluwer)


• Rivastigmine Prescribing Information (FDA)


• Rivastigmine Professional Patient Advice (Wolters Kluwer)

Compare Exelon with other medications

• Alzheimer's Disease
• Parkinson's Disease

pralidoxime

Generic Name: pralidoxime (PRAL i DOX eem)

Brand Names: Protopam Chloride

What is pralidoxime?

Pralidoxime reverses muscle weakness or paralysis caused by a poison or certain drug overdose.

Pralidoxime is used as an antidote to treat poisoning by a chemical or pesticide (insect spray), or by a drug used to treat a muscle disorder.

This medication is not effective as an antidote for all types of pesticide poisonings.

Pralidoxime may also be used for purposes not listed in this medication guide.

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

If possible, before you receive pralidoxime, tell your doctor if you have kidney disease, or if you are allergic to any drugs. Also tell your doctor if you are pregnant or breast-feeding. In an emergency situation it may not be possible before you are treated to tell your caregivers about your health conditions or if you are pregnant or breast-feeding. Make sure any doctor caring for you afterward knows that you have received this medication.

What should I discuss with my health care provider before receiving pralidoxime?

If possible, before you receive pralidoxime, tell your doctor if you have kidney disease, or if you are allergic to any drugs. FDA pregnancy category C. It is not known whether pralidoxime is harmful to an unborn baby. Tell your doctor if you are pregnant. It is not known whether pralidoxime passes into breast milk or if it could harm a nursing baby.

In an emergency situation, it may not be possible before you are treated with pralidoxime to tell your caregivers if you are pregnant or breast-feeding. However, make sure any doctor caring for your pregnancy or your baby knows that you have received this medication.

How is pralidoxime given?

Pralidoxime is usually given as soon as possible after the onset of poisoning or overdose symptoms. You may need to receive pralidoxime for several days.

Pralidoxime is injected into a muscle, under the skin, or into a vein through an IV. A healthcare provider will give you this injection. Pralidoxime must be given slowly. The IV infusion can take up to 30 minutes to complete.

Your breathing, blood pressure, oxygen levels, kidney function, and other vital signs will be watched closely while you are receiving this medication.

After treatment with pralidoxime, you may be watched for up to 72 hours to make sure the medicine has been effective and you no longer have any effects of the poison or drug overdose.

What happens if I miss a dose?

Since pralidoxime is given by a healthcare professional in an emergency setting, you are not likely to miss a dose.

What happens if I overdose?

Since this medication is given by a healthcare professional in a medical setting, an overdose is unlikely to occur.

Overdose symptoms may include some of the side effects listed in this medication guide.

What should I avoid after receiving pralidoxime?

Follow your doctor's instructions about any restrictions on food, beverages, or activity.

Pralidoxime side effects

Some of the side effects of pralidoxime may be similar to the symptoms of poisoning. Your caregivers will watch you closely to determine whether your body is responding well to the medication, or if you are having any serious side effects.

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Tell your caregivers at once if you have a serious side effect such as:

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  fast heart rate;

  
  


• 
  

  rapid breathing;

  
  


• 
  

  increased muscle stiffness;

  
  


• 
  

  a choking feeling;

  
  

Less serious side effects may include:

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  pain where the medicine was injected;

  
  


• 
  

  blurred vision;

  
  


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  feeling dizzy or drowsy;

  
  


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  headache; or

  
  


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  nausea.

  
  

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Pralidoxime Dosing Information

Usual Adult Dose for Organophosphate Poisoning:

IV:
Initial dose: 1 to 2 g, preferably as an IV infusion in 100 mL of normal saline, over 15 to 30 minutes; if an infusion is not practical or if pulmonary edema is present, the dose should be given slowly (over at least 5 minutes) by IV injection as a 50 mg/mL solution in Sterile Water for Injection (e.g., 1000 mg in 20 mL)

Second dose: 1 to 2 g may be indicated after about 1 hour if muscle weakness has not been relieved

Additional doses may be given every 10 to 12 hours if muscle weakness persists.

IM:
Mild symptoms:
Initial dose: 600 mg IM; recommend waiting 15 minutes for pralidoxime to take effect
Second dose: 600 mg IM if mild symptoms persist after 15 minutes
Third dose: 600 mg IM (cumulative dose of 1800 mg) if mild symptoms persist after an additional 15 minutes

If severe symptoms develop at any time after the first dose, 2 additional 600 mg IM doses in rapid succession should be administered for a total cumulative dose of 1800 mg.

Severe symptoms: Three 600 mg IM doses in rapid succession should be administered for a total cumulative dose of 1800 mg.

Persistent symptoms: If symptoms persist after administration of the complete 1800 mg regimen, the series may be repeated starting about 1 hour after the administration of the last injection.

Usual Adult Dose for Nerve Agent Poisoning:

IV:
Initial dose: 1 to 2 g, preferably as an IV infusion in 100 mL of normal saline, over 15 to 30 minutes; if an infusion is not practical or if pulmonary edema is present, the dose should be given slowly (over at least 5 minutes) by IV injection as a 50 mg/mL solution in Sterile Water for Injection (e.g., 1000 mg in 20 mL)

Second dose: 1 to 2 g may be indicated after about 1 hour if muscle weakness has not been relieved

Additional doses may be given every 10 to 12 hours if muscle weakness persists.

IM:
Mild symptoms:
Initial dose: 600 mg IM; recommend waiting 15 minutes for pralidoxime to take effect
Second dose: 600 mg IM if mild symptoms persist after 15 minutes
Third dose: 600 mg IM (cumulative dose of 1800 mg) if mild symptoms persist after an additional 15 minutes

If severe symptoms develop at any time after the first dose, 2 additional 600 mg IM doses in rapid succession should be administered for a total cumulative dose of 1800 mg.

Severe symptoms: Three 600 mg IM doses in rapid succession should be administered for a total cumulative dose of 1800 mg.

Persistent symptoms: If symptoms persist after administration of the complete 1800 mg regimen, the series may be repeated starting about 1 hour after the administration of the last injection.

Usual Adult Dose for Anticholinesterase Overdose:

Initial dose: 1 to 2 g IV slowly
Maintenance dose: Increments of 250 mg IV every 5 minutes as needed to control symptoms

Usual Pediatric Dose for Organophosphate Poisoning:

16 years or younger:
IV:
Pralidoxime can be given as a loading dose followed by continuous IV infusion or as intermittent IV infusions, depending upon patient's clinical condition. The specific dose given should depend upon the severity of symptoms.

Loading dose: 20 to 50 mg/kg (not to exceed 2 g/dose) over 15 to 30 minutes followed by continuous infusion
Continuous infusion: 10 to 20 mg/kg/hour following the loading dose

Intermittent infusion:
Initial dose: 20 to 50 mg/kg (not to exceed 2 g/dose) over 15 to 30 minutes
Second dose: 20 to 50 mg/kg may be indicated after about 1 hour if muscle weakness has not been relieved
Repeat dosing: Permissible every 10 to 12 hours as needed.

If administration by continuous or intermittent IV infusion is not practical, or if pulmonary edema is present, the 20 to 50 mg/kg dose should be given slowly (over at least 5 minutes) by IV injection as a 50 mg/mL solution in Sterile Water for Injection. Additional doses may be given every 10 to 12 hours if muscle weakness persists.

IM:
Less than 40 kg:
Mild symptoms:
Initial dose: 15 mg/kg IM; recommend waiting 15 minutes for pralidoxime to take effect
Second dose: 15 mg/kg IM if mild symptoms persist after 15 minutes
Third dose: 15 mg/kg IM (total cumulative dose of 45 mg/kg) if mild symptoms persist after an additional 15 minutes

If severe symptoms develop at any time after the first dose, 2 additional 15 mg/kg IM doses in rapid succession should be administered for a total cumulative dose of 45 mg/kg.

Severe symptoms: Three 15 mg/kg IM doses in rapid succession should be administered for a total cumulative dose of 45 mg/kg.

Persistent symptoms: If symptoms persist after administration of the complete 45 mg/kg regimen, the series may be repeated starting about 1 hour after the administration of the last injection.

40 kg or more:
Mild symptoms:
Initial dose: 600 mg IM; recommend waiting 15 minutes for pralidoxime to take effect
Second dose: 600 mg IM if mild symptoms persist after 15 minutes
Third dose: 600 mg IM (total cumulative dose of 1800 mg) if mild symptoms persist after an additional 15 minutes

If severe symptoms develop at any time after the first dose, 2 additional 600 mg IM doses in rapid succession should be administered for a total cumulative dose of 1800 mg.

Severe symptoms: Three 600 mg IM doses in rapid succession should be administered for a total cumulative dose of 1800 mg.

Persistent symptoms: If symptoms persist after administration of the complete 1800 mg regimen, the series may be repeated starting about 1 hour after the administration of the last injection.

Usual Pediatric Dose for Nerve Agent Poisoning:

16 years or younger:
IV:
Pralidoxime can be given as a loading dose followed by continuous IV infusion or as intermittent IV infusions, depending upon patient's clinical condition. The specific dose given should depend upon the severity of symptoms.

Loading dose: 20 to 50 mg/kg (not to exceed 2 g/dose) over 15 to 30 minutes followed by continuous infusion
Continuous infusion: 10 to 20 mg/kg/hour following the loading dose

Intermittent infusion:
Initial dose: 20 to 50 mg/kg (not to exceed 2 g/dose) over 15 to 30 minutes
Second dose: 20 to 50 mg/kg may be indicated after about 1 hour if muscle weakness has not been relieved
Repeat dosing: Permissible every 10 to 12 hours as needed.

If administration by continuous or intermittent IV infusion is not practical, or if pulmonary edema is present, the 20 to 50 mg/kg dose should be given slowly (over at least 5 minutes) by IV injection as a 50 mg/mL solution in Sterile Water for Injection. Additional doses may be given every 10 to 12 hours if muscle weakness persists.

IM:
Less than 40 kg:
Mild symptoms:
Initial dose: 15 mg/kg IM; recommend waiting 15 minutes for pralidoxime to take effect
Second dose: 15 mg/kg IM if mild symptoms persist after 15 minutes
Third dose: 15 mg/kg IM (total cumulative dose of 45 mg/kg) if mild symptoms persist after an additional 15 minutes

If severe symptoms develop at any time after the first dose, 2 additional 15 mg/kg IM doses in rapid succession should be administered for a total cumulative dose of 45 mg/kg.

Severe symptoms: Three 15 mg/kg IM doses in rapid succession should be administered for a total cumulative dose of 45 mg/kg.

Persistent symptoms: If symptoms persist after administration of the complete 45 mg/kg regimen, the series may be repeated starting about 1 hour after the administration of the last injection.

40 kg or more:
Mild symptoms:
Initial dose: 600 mg IM; recommend waiting 15 minutes for pralidoxime to take effect
Second dose: 600 mg IM if mild symptoms persist after 15 minutes
Third dose: 600 mg IM (total cumulative dose of 1800 mg) if mild symptoms persist after an additional 15 minutes

If severe symptoms develop at any time after the first dose, 2 additional 600 mg IM doses in rapid succession should be administered for a total cumulative dose of 1800 mg.

Severe symptoms: Three 600 mg IM doses in rapid succession should be administered for a total cumulative dose of 1800 mg.

Persistent symptoms: If symptoms persist after administration of the complete 1800 mg regimen, the series may be repeated starting about 1 hour after the administration of the last injection.

What other drugs will affect pralidoxime?

If possible, before you receive this medication, tell your doctor about all other medicines you use, especially:

• 
  

  aminophylline (Phyllocontin, Truphylline);

  
  


• 
  

  atropine (Atreza, Sal-Tropine, and others);

  
  


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  morphine (Avinza, Kadian, MS Contin, Oramorph);

  
  


• 
  

  reserpine;

  
  


• 
  

  theophylline (Elixophyllin, Theo-24, Uniphyl);

  
  


• 
  

  a barbiturate such as butabarbital (Butisol), secobarbital (Seconal), pentobarbital (Nembutal), or phenobarbital (Solfoton); or

  
  


• 
  

  a tranquilizer such as chlorpromazine (Thorazine), fluphenazine (Permitil), perphenazine (Trilafon), prochlorperazine (Compazine), thioridazine (Mellaril), or trifluperazine (Stelazine).

  
  

This list is not complete and other drugs may interact with pralidoxime. Tell your doctor about all medications you use. This includes prescription, over-the-counter, vitamin, and herbal products. Do not start a new medication without telling your doctor.

More pralidoxime resources

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

• pralidoxime Injection Advanced Consumer (Micromedex) - Includes Dosage Information


• Pralidoxime Chloride Monograph (AHFS DI)

Compare pralidoxime with other medications

• Anticholinesterase Overdose
• Nerve Agent Poisoning
• Organophosphate Poisoning

Where can I get more information?

• Your doctor or pharmacist can provide more information about pralidoxime.

See also: pralidoxime side effects (in more detail)