Antizol

Generic Name: fomepizole (foe MEP i zole)

Brand Names: Antizol

What is Antizol (fomepizole)?

Fomepizole is an antidote to certain types of poison.

Fomepizole is used to treat poisoning with ethylene glycol (antifreeze) or methanol (contained in solvents, fuels, and other household or automotive chemicals). Fomepizole is sometimes used together with hemodialysis to rid the body of a poison.

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

What is the most important information I should know about Antizol (fomepizole)?

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

Tell your caregivers at once if you have any burning, swelling, or skin changes where the medicine was injected.

To be sure this medication is helping your condition, your blood and urine will need to be tested often. This will help your doctor determine how long to treat you with fomepizole. You will also be watched for any effects of the poisoning, such as problems with vision, breathing, or urination.

What should I discuss with my health care provider before receiving Antizol (fomepizole)?

You should not receive this medication if you are allergic to fomepizole. FDA pregnancy category C. This medication may be harmful to an unborn baby and is not recommended in pregnant women unless clearly needed. It is not known whether fomepizole passes into breast milk or if it could harm a nursing baby.

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

How is fomepizole given?

Fomepizole is given as an injection through a needle placed into a vein. You will receive this injection in a hospital or emergency setting. The medicine must be given slowly through an IV infusion, and each dose can take up to 30 minutes to complete.

To be sure this medication is helping your condition, your blood and urine will need to be tested often. This will help your doctor determine how long to treat you with fomepizole. You will also be watched for any effects of the poisoning, such as problems with vision, breathing, or urination.

What happens if I miss a dose?

Since fomepizole is given as needed by a healthcare professional, it is not likely that you will miss a dose.

What happens if I overdose?

Tell your caregivers right away if you think you have received too much of this medicine.

Overdose symptoms may include nausea, dizziness, or a spinning sensation.

What should I avoid while receiving Antizol (fomepizole)?

Follow your doctor's instructions about any restrictions on food, beverages, or activity after you are treated with fomepizole.

Antizol (fomepizole) 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 any of these serious side effects (some are effects of the poison and not of fomepizole):

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  burning, swelling, or skin changes where the medicine was injected;

  
  


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  urinating less than usual or not at all;

  
  


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  fast or slow heart rate, feeling like you may pass out; or

  
  


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  skin rash, bruising, severe tingling, numbness, pain, muscle weakness.

  
  

Less serious side effects may include:

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  mild skin rash;

  
  


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  heartburn, nausea, vomiting, diarrhea;

  
  


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  loss of appetite;

  
  


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  dizziness, drowsiness, anxiety, or headache;

  
  


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  metallic taste in your mouth;

  
  


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  hangover feeling;

  
  


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  back pain;

  
  


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  sore throat;

  
  


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  ringing in your ears; or

  
  


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  changes in vision, changes in smell or taste senses.

  
  

This is not a complete list of side effects and others may occur. Tell your doctor about any unusual or bothersome side effect. You may report side effects to FDA at 1-800-FDA-1088.

What other drugs will affect Antizol (fomepizole)?

Tell your doctor if you have recently used any of the following drugs:

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  phenytoin (Dilantin);

  
  


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  carbamazepine (Carbatrol, Tegretol);

  
  


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  cimetidine (Tagamet); or

  
  


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  ketoconazole (Nizoral).

  
  

There may be other drugs that can affect fomepizole. Tell your doctor about all your prescription and over-the-counter medications, vitamins, minerals, herbal products, and drugs prescribed by other doctors.

More Antizol resources

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

• Antizol Monograph (AHFS DI)


• Antizol Prescribing Information (FDA)


• Fomepizole Prescribing Information (FDA)

Compare Antizol with other medications

• Ethylene Glycol Poisoning
• Methanol Poisoning

Where can I get more information?

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

See also: Antizol side effects (in more detail)

Antizol

Generic Name: Fomepizole
Class: Antidotes
ATC Class: V03AB34
VA Class: AD900
Chemical Name: 4-Methyl-1H-pyrazole
Molecular Formula: C₄H₆N₂
CAS Number: 7554-65-6

Introduction

Antidote for ethylene glycol or methanol intoxication;^b an alcohol dehydrogenase inhibitor.^{1 2 3 4 5 6 7 8 10 11 12 13 14 16 18}

Uses for Antizol

Ethylene Glycol or Methanol Intoxication

Treatment of known or suspected ethylene glycol (e.g., antifreeze) or methanol intoxication; use alone or in combination with hemodialysis.^{1 2 11 14 16 23 34 35} (See General under Dosage and Administration.)

Not a substitute for standard therapeutic measures (e.g., fluid and electrolyte therapy, correction of metabolic abnormalities [e.g., acidosis]).^{1 14 23} (See General under Dosage and Administration.)

Appears to be as effective as IV alcohol therapy in preventing development of ethylene glycol-associated metabolic acidosis and renal toxicity.^{1 4 19} However, may be technically less difficult to administer and monitor than IV alcohol therapy because fomepizole has a more prolonged and less variable rate of elimination (i.e., longer duration of action), has less potential for adverse effects (e.g., CNS depression, hypoglycemia),^{1 2 3 4 5 7 11 22 25} and does not require plasma concentration monitoring.^{21 22 24}

For treatment of ethylene glycol intoxication, the American Academy of Clinical Toxicology (AACT) and some clinicians recommend use of fomepizole rather than alcohol in cases involving ingestion of multiple substances with CNS depressant activity, in patients with altered consciousness, in critically ill patients with an anion gap metabolic acidosis of unknown etiology and potential exposure to ethylene glycol, in settings in which intensive-care and laboratory facilities to monitor alcohol therapy are unavailable, and in patients who have contraindications to the use of alcohol therapy (e.g., history of alcoholism).^{24 25 26 27}

Has been used with success alone or in combination with hemodialysis for the treatment of ethylene glycol intoxication in a few infants† and children†.^{29 30 31 32} May have advantages over alcohol therapy in young children as fomepizole lacks the risk of hypoglycemia, obtundation, and hypothermia associated with alcohol therapy;^{25 31} however, insufficient data to establish relative efficacy of fomepizole and alcohol for this use in children.^{1 25}

Antizol Dosage and Administration

General

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  Initiate therapy immediately upon suspected ethylene glycol or methanol ingestion based on patient history and/or anion gap metabolic acidosis, increased osmolar gap, visual disturbances,^{1 26 34} or oxalate crystals in the urine,^{1 24 25 26 30} or if serum ethylene glycol or methanol concentration >20 mg/dL.¹

  
  


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  Consider hemodialysis (in addition to fomepizole therapy) if ethylene glycol or methanol concentration ≥50 mg/dL;^{1 14 23} otherwise, closely monitor acid-base balance and institute hemodialysis when metabolic acidosis develops.²⁵ Hemodialysis may be required if severe or worsening metabolic acidosis, acute renal failure, azotemia, and/or anuria occurs.^{1 2 3 4 5 8 11 14 15 16 17 22 25 26 27 28 b} (See Dosage in Patients Requiring Hemodialysis under Dosage and Administration.)

  
  


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  Treat metabolic acidosis, acute renal failure (ethylene glycol intoxication), ARDS, visual disturbances (methanol intoxication), and hypocalcemia as needed.^{1 4 8 10} Supportive therapy (e.g., sodium bicarbonate, potassium and calcium supplementation, oxygen, fluid therapy) may be necessary.^{a b} (See Adequate Patient Evaluation and Monitoring under Cautions.)

  
  

Administration

IV Administration

For compatibility information, see Compatibility under Stability.

Administer by slow IV infusion (after proper dilution); must not be administered undiluted or by rapid IV injection.¹ (See Local Effects under Cautions.)

Dilution

Use strict aseptic technique since drug product contains no preservative.^b

Withdraw appropriate dose of fomepizole concentrate and add to at least 100 mL of sterile 0.9% sodium chloride or dextrose 5% injection.^{1 b}

Rate of Administration

Infuse diluted solution over 30 minutes.¹ (See Local Effects under Cautions.)

Dosage

Pediatric Patients

Ethylene Glycol Intoxication†

IV

Dosage not established;¹ however, in a limited number of case reports, infants and children 8 months to 13 years of age received the same dosages as those recommended for adults.^{29 30 31}

Adults

Ethylene Glycol or Methanol Intoxication

IV

Loading dose: 15 mg/kg.^{1 22 23 25 26}

Maintenance dosage: 10 mg/kg every 12 hours for 4 doses, then 15 mg/kg every 12 hours thereafter until serum ethylene glycol or methanol concentrations are undetectable or have decreased to <20 mg/dL, and patient is asymptomatic with a normal arterial blood pH value.^{1 22 23 25 26 b}

Dosage in Patients Requiring Hemodialysis

Loading dose: 15 mg/kg.^a

Maintenance dosage: Generally similar to usual adult maintenance dosage; however, because fomepizole is dialyzable, adjust dosage/schedule before, during, and immediately upon completion of hemodialysis (see Table 1).¹

Example 1: Patient is given a loading dose of 15 mg/kg.^a Hemodialysis starts 1 hour after loading dose and lasts for 6 hours.^a Four hours after initiation of hemodialysis, patient would receive a dose of 10 mg/kg.^a Because length of time between last fomepizole dose and end of hemodialysis is 2 hours, patient should receive a dose of 5 mg/kg at the end of hemodialysis.^a Administer fomepizole every 12 hours thereafter until ethylene glycol or methanol concentration is <20 mg/dL and patient is asymptomatic with normal pH.^a

Example 2: Patient is given a loading dose of 15 mg/kg.^a Hemodialysis starts 7 hours after loading dose and lasts for 45 minutes.^a Patient would receive a dose of 10 mg/kg prior to initiation of hemodialysis.^a Because length of time between the last fomepizole dose and end of hemodialysis is <1 hour, patient should receive a 10 mg/kg dose 12 hours after the dose given prior to initiation of hemodialysis.^a Administer fomepizole every 12 hours thereafter until ethylene glycol or methanol concentration is <20 mg/dL and the patient is asymptomatic with normal pH.^a

Table 1. Fomepizole Dosing in Patients Requiring Hemodialysis

Dose at the Beginning of Hemodialysis
If <6 hours since last fomepizole dose	If ≥6 hours since last fomepizole dose
Do not administer dose	Administer next scheduled dose
Dose during Hemodialysis
Dose every 4 hours
Dose at the Time Hemodialysis Is Completed
Time between last dose and the end of hemodialysis
<1 hour	Do not administer dose at the end of hemodialysis
1–3 hours	Administer half of next scheduled dose
>3 hours	Administer next scheduled dose
Maintenance Dosing off Hemodialysis
Give next scheduled dose 12 hours from last dose administered

Special Populations

Geriatric Patients

Select dosage with caution because of age-related decrease in renal function.^{1 21}

Cautions for Antizol

Contraindications

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  Known severe hypersensitivity to fomepizole or other pyrazoles.^{1 8 11 21}

  
  

Warnings/Precautions

Sensitivity Reactions

Hypersensitivity Reactions

Mild rash and eosinophilia reported.^b

Monitor for manifestations of an allergic reaction.¹

Major Toxicities

Hepatic Effects

Transient increases in serum transaminase concentrations reported following repeated dosing.^b

Monitor hepatic enzyme concentrations during therapy.^b

Hematologic Effects

Eosinophilia reported following repeated dosing.^b

Monitor WBC counts during therapy.^b

Local Effects

Vein irritation and phlebosclerosis reported following rapid (i.e., <30 minutes) IV infusion or IV injection (i.e., over 5 minutes) of a 25-mg/mL solution.^{1 16 21 b}

General Precautions

Adequate Patient Evaluation and Monitoring

Frequently monitor arterial blood gases, pH, electrolytes, BUN, creatinine, and urinalysis to determine response to therapy.^b

Frequently monitor serum and urine ethylene glycol concentrations and monitor for presence of urinary oxalate crystals in patients with ethylene glycol intoxication.^b In patients with methanol intoxication, monitor serum methanol concentrations.^b

Perform ECG because acidosis and electrolyte imbalances can affect the cardiovascular system.^b Electroencephalography also may be required in comatose patients.^b

Monitor hepatic enzyme (i.e., serum transaminase) concentrations and WBC counts.^b (See Major Toxicities under Cautions.)

Concomitant Use with Alcohol

Consider potential interaction with alcohol, which often is ingested concomitantly by patients with ethylene glycol intoxication or used initially in the treatment of ethylene glycol or methanol intoxication.^{1 2 4 5 7 22 23 24 25 26 33} (See Alcohol under Interactions.)

Specific Populations

Pregnancy

Category C.^b

Lactation

Not know whether fomepizole is distributed into milk.^b Caution if used in nursing women.^b

Pediatric Use

Safety and efficacy not established.^b

Geriatric Use

Safety and efficacy not established.^b

Common Adverse Effects

Headache, nausea, dizziness, increased drowsiness, bad/metallic taste.^b

Interactions for Antizol

Metabolized by mixed-function oxidases (cytochrome P-450 system).^b Potent inducer of CYP-mediated drug elimination; induces own metabolism.^{a b}

Drugs Affecting Hepatic Microsomal Enzymes

Inhibitors or inducers of CYP isoenzymes: Potential pharmacokinetic interaction; however, no studies to date.^b

Specific Drugs

Drug	Interaction	Comments
Alcohol	Decreased elimination rate of fomepizole and alcohol (possibly due to inhibition of alcohol dehydrogenase)1 2 4 5 7 22 23 24 25 26 33 b

Antizol Pharmacokinetics

Absorption

Bioavailability

Immediately and completely bioavailable following IV administration.^a

Distribution

Extent

Rapidly distributes to total body water following IV infusion.^b

Not known whether fomepizole is distributed into milk.^b

Elimination

Metabolism

Metabolized in the liver.^b

Induces own metabolism; elimination rate increases after about 30–40 hours.^b

Elimination Route

Excreted in urine mainly as metabolites; only 1–3.5% of administered dose excreted in urine as unchanged drug. ^b

Fomepizole is dialyzable.^{1 25}

Half-life

Not determined, but varies with dose.^b

Special Populations

Pharmacokinetics not studied in patients with hepatic or renal impairment or in geriatric patients.¹

Stability

Storage

Parenteral

Injection Concentrate for IV Infusion

20-25°C.¹ Fomepizole concentrate solidifies at temperatures <25°C.¹ If solidification occurs, pass vial under warm water or hold vial in the hand to liquify solution before dilution.¹ Solidification does not affect efficacy, safety, or stability of fomepizole.¹

Following dilution with 0.9% sodium chloride or 5% dextrose injection, stable for ≥24 hours when refrigerated or stored at controlled room temperature (20–25°C).¹ However, because product contains no preservatives, manufacturer recommends using within 24 hours after dilution.¹

Discard if solutions become hazy, discolored, or contain a precipitate or if they exhibit leakage.¹

Compatibility

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

Parenteral

Solution Compatibility¹

Compatible
Dextrose 5% in water
Sodium chloride 0.9%

ActionsActions

• 
  

  Competitively inhibits alcohol dehydrogenase,^{1 2 3 4 5 6 7 8 9 11 12 14 16 18} the enzyme that catalyzes the oxidation of alcohol to acetaldehyde and the initial steps in the metabolism of ethylene glycol and methanol to toxic metabolites.^{1 4 6 7 9 11 15 16}

  
  


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  Blocks metabolism of ethylene glycol (main component of most antifreezes and coolants) to glycoaldehyde, which undergoes subsequent sequential oxidations to yield glycolate, glyoxylate, and oxalate.^{1 2 4 9 11 15 17} Glycolate and oxalate are toxic metabolites principally responsible for the metabolic acidosis and renal damage associated with ethylene glycol intoxication.^{1 2 3 4 8 9 12 15 17 20 24 28} Lethal dose of ethylene glycol in humans is approximately 1.4–1.6 mL/kg (about 100 mL in an adult);^{1 11 20} however, as little as 30 mL may be fatal.^a

  
  


• 
  

  Blocks metabolism of methanol (main component of windshield wiper fluid) to formaldehyde, which undergoes subsequent oxidation to yield formic acid.^{1 4 9 11 17} Formic acid is principally responsible for the metabolic acidosis and visual disturbances (e.g., decreased visual acuity, potential blindness) associated with methanol intoxication.^{1 4 9 14 17 20 23} Lethal dose of pure methanol in humans is approximately 1–2 mL/kg;^{1 11 20} however, permanent blindness and death reported with as little as 0.1 mL/kg (6–10 mL in adults).^a

  
  


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  Fomepizole has approximately 8000 or 80,000 times greater affinity for alcohol dehydrogenase than alcohol or methanol, respectively.¹⁴

  
  

Advice to Patients

• 
  

  Risk of hypersensitivity reactions.¹

  
  


• 
  

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

  
  


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  Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, dietary supplements, and/or herbal products, as well as any concomitant illnesses.¹

  
  


• 
  

  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.

Fomepizole

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Parenteral	For injection, concentrate, for IV infusion	1 g/mL	Antizol (preservative-free)	Jazz

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 September 2007. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

References

1. Orphan Medical. Antizol (fomepizole) injection prescribing information. Minnetonka, MN; 1997 Dec.

2. Baud FJ, Galliot M, Astier A et al. Treatment of ethylene glycol poisoning with intravenous 4-methylpyrazole. N Engl J Med. 1988; 319:97-100. [IDIS 243317] [PubMed 3380132]

3. Jobard E, Harry P, Turcant A et al. 4-Methylpyrazole and hemodialysis in ethylene glycol poisoning. J Toxicol Clin Toxicol. 1996; 34:373-7. [IDIS 372622] [PubMed 8699550]

4. Jacobsen D, McMartin KE. Antidotes for methanol and ethylene glycol poisoning. J Toxicol Clin Toxicol. 1997; 35:127-43. [IDIS 383796] [PubMed 9120880]

5. Jacobsen D, McMartin K. 4-Methylpyrazole—present status. J Toxicol Clin Toxicol. 1996; 34:379-81. [IDIS 372623] [PubMed 8699551]

6. Jacobsen D, Barron SK, Sebastian CS et al. Non-linear kinetics of 4-methylpyrazole in healthy human subjects. Eur J Clin Pharmacol. 1989; 37:599-604. [IDIS 262931] [PubMed 2693117]

7. Jacobsen D, Sebastian CS, Dies DF et al. Kinetic interactions between 4-methylpyrazole and ethanol in healthy humans. Alcohol Clin Exp Res. 1996; 20:804-9. [IDIS 372926] [PubMed 8865952]

8. Baud FJ, Bismuth C, Garnier R et al. 4-Methylpyrazole may be an alternative to ethanol therapy for ethylene glycol intoxication in man. J Toxicol Clin Toxicol. 1986; 24:463-83. [IDIS 229718] [PubMed 3573122]

9. Anon. Ethylene glycol and methanol poisoning simplified. N Z Med J. 1988; 101:591.

10. Jacobsen D, Sebastian CS, Blomstrand R et al. 4-Methylpyrazole: a controlled study of safety in healthy human subjects after single, ascending doses. Alcohol Clin Exp Res. 1988; 12:516-22. [PubMed 3056073]

11. Orphan Medical. Antizol (fomepizole) injection product monograph. Minnetonka, MN; 1997 Dec.

12. Harry P, Turcant A, Bouachour G et al. Efficacy of 4-methylpyrazole in ethylene glycol poisoning: clinical and toxicokinetic aspects. Hum Exp Toxicol. 1994; 13:61-4. [PubMed 8198831]

13. Jacobsen D, Sebastian CS, Barron SK et al. Effects of 4-methylpyrazole, methanol/ethylene glycol antidote, in healthy humans. J Emerg Med. 1990; 8:455-61. [PubMed 2212566]

14. Burns MJ, Graudins A, Aaron CK et al. Treatment of methanol poisoning with intravenous 4-methylpyrazole. Ann Emerg Med. 1997; 30:829-32. [IDIS 398327] [PubMed 9398786]

15. Davis DP, Bramwell KJ, Hamilton RS et al. Ethylene glycol poisoning: case report of a record-high level and a review. J Emerg Med. 1997; 15:653-67. [PubMed 9348055]

16. Antidotes. In: Ellenhorn MJ, ed. Medical Toxicology Diagnosis and Treatment of Human Poisoning. 2nd ed. Baltimore: Williams & Wilkins; 1997:99-100.

17. Alcohols and Glycols. In: Ellenhorn MJ, Barceloux DG, eds. Medical Toxicology Diagnosis and Treatment of Human Poisoning. New York: Elsevier Science; 1988:805-9.

18. Woolf AD, The Haitian diethylene glycol poisoning tragedy: a dark wood revisited. JAMA. 1998; 279:1215-6.

19. Grauer GF, Thrall MA, Henre BA et al. Comparison of the effects of ethanol and 4-methylpyrazole on the pharmacokinetics and toxicity of ethylene glycol in the dog. Toxicol Lett. 1987; 35:307-14. [PubMed 3824418]

20. Gosselin RE, Smith RP, Hodge HC. Clinical toxicology of commercial products. 5th ed. Baltimore: The Williams & Wilkins CO; 1984:III-172-9.

21. Orphan Medical, Minnetonka, MN: Personal communication.

22. Brent J, McMartin K, Phillips S et al. Fomepizole for the treatment of ethylene glycol poisoning. N Engl J Med. 1999; 340:832-8. [IDIS 421131] [PubMed 10080845]

23. Brent J, McMartin K, Phillips S et al. Fomepizole for the treatment of methanol poisoning. N Engl J Med. 2001; 344:424-9. [IDIS 459242] [PubMed 11172179]

24. Jacobsen D. New treatment for ethylene glycol poisoning. N Engl J Med. 1999; 340:879-81. [IDIS 421133] [PubMed 10080853]

25. Barceloux DG, Krenzelok EP, Olson K et al. American academy of clinical toxicology practice guideline on the treatment of ethylene glycol poisoning. J Toxicol Clin Toxicol. 1999; 37:537-60. [IDIS 436899] [PubMed 10497633]

26. Casavant MJ. Fomepizole in the treatment of poisoning. Pediatrics. 2001; 107:170-1. [IDIS 459224] [PubMed 11134450]

27. Watson WA. Ethylene glycol toxicity: closing in on rational evidence based treatment. Ann Emerg Med. 2000; 36:139-41. [IDIS 451512] [PubMed 10918105]

28. Sivilotti MA, Burns MJ, McMartin KE et al. Toxicokinetics of ethylene glycol during fomepizole therapy: implications for management. Ann Emerg Med. 2000; 36:114-125. [IDIS 451509] [PubMed 10918102]

29. Baum CR, Langman CB, Oker EE et al. Fomepizole treatment of ethylene glycol poisoning in an infant. Pediatrics. 2000; 106:1489-91. [IDIS 459212] [PubMed 11099610]

30. Harry P, Jobard E, Briand M et al. Ethylene glycol poisoning in a child treated with 4-methylpyrazole. Pediatrics. 1998; 102:E1. [IDIS 426058] [PubMed 9724679]

31. Boyer EW, Mejia M, Woolf A et al. Severe ethylene glycol ingestion treated without hemodialysis. Pediatrics. 2001; 107:172-3. [PubMed 11134452]

32. Benitez JG, Swanson-Biearman B, Krenzelok EP. Nystagmus secondary to fomepizole administration in a pediatric patient. J Toxicol Clin Toxicol. 2000; 38:795-8. [IDIS 457815] [PubMed 11192468]

33. Boron SW, Mégarbane B, Baud FJ. Fomepizole in treatment of uncomplicated ethylene glycol poisoning. Lancet. 1999; 354:831. [IDIS 431674] [PubMed 10485727]

34. Megarbane B, Borron SW, Trout H et al. Treatment of acute methanol poisoning with fomepizole. Intensive Care Med. 2001; 27:1370-8. [IDIS 470922] [PubMed 11511951]

35. Girault C, Tamion F, Moritz F et al. Fomepizole (4-methylpyrazole) in fatal methanol poisoning with early CT scan cerebral lesions. J Toxicol Clin Toxicol. 1999; 37:777-80. [IDIS 439030] [PubMed 10584591]

36. Davis DP, Bramwell KJ, Hamilton RS et al. Ethylene glycol poisoning: case report of a record-high level and a review. J Emerg Med. 1997; 15:653-67. [PubMed 9348055]

a. Orphan Medical. Antizol (fomepizole) injection product monograph. Minnetonka, MN; 2001 Apr.

b. Jazz Pharmaceuticals, Inc. Antizol (fomepizole) injection prescribing information. Palo Alto, CA; 2006 Apr.

More Antizol resources

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

• Antizol Concise Consumer Information (Cerner Multum)


• Antizol Prescribing Information (FDA)


• Fomepizole Prescribing Information (FDA)

Compare Antizol with other medications

• Ethylene Glycol Poisoning
• Methanol Poisoning

Antipyrine and Benzocaine Ear Drops

Dosage Form: otic solution
Antipyrine and Benzocaine Otic Solution, USP Rx Only 15 mL

DESCRIPTION: Each mL contains:

Antipyrine..........54  mg  (5.4%)

Benzocaine..........14.0 mg (1.4%)

(also contains glycerin and oxyquinoline sulfate)

Antipyrine and Benzocaine Otic Solution is an otic solution containing antipyrine, benzocaine, oxyquinoline sulfate and anhydrous glycerin for use in the ear. The solution congeals at 0C (32F) but returns to normal consistency, unchanged at room temperature.

Antipyrine is an analgesic with local anesthetic action, it is chemically 2,3-dimethyl-1-phyl-3-pyrazolin-5-one. Antipyrine occurs as colorless crystals or white powder, has a slightly bitter taste and is soluble in water and alcohol.

Benzocaine is a local anesthetic. it is chemically ethyl-p-aminobenzoate or Benzoic Acid, 4-amino, ethyl ester. The active ingredients are represented by the following structural formula

Antipyrine and Benzocaine Otic Solution comibine the hygroscopic property of anhydrous glycerin with the analgesic action of antipyrine and benzocaine to relieve pressure, reduce inflammation and congestion, and alleviate pain and discomfort in acute otitis media. Antipyrine and Benzocaine Otic Solution does not blanch the tympanic membrane or mask the landmarks and, therefore, does not distort the otoscopic picture

Indications and Usage: Acute Otitis Media of Various Etiologies

Prompt relief of pain and reduction of inflammation in the congestive and serous stages.

Adjuvant therapy during systemic antibiotic administration for resolution of the infection.

Because of the close anatomical relationship of the eustachian tube to the nasal cavity, otitis media is a frequent problem, epecially in children in whom the tube is shorter, wider and more horizontal than in adults.

Removal of Cerumen

Facilitates the removal of excessive or impacted cerumen

Contraindications: Antipyrine and Benzocaine Otic Solution is contraindicated in any person with hypersensitivity to any of the components or substances related tot hem. This product is contraindicated in the presence of spontaneous perforation of the tympanic membrane or discharge.

Warnings: FOR USE IN EARS ONLY NOT FOR USE IN EYES

KEEP OUT OF REACH OF CHILDREN

Discontinue promptly if sensitization or irritation occurs.

Precautions: Information for Patients: Avoid contaminating the dropper tip with material from the ear fingers or other source.

CARCONOGENESIS, MUTAGENESIS, IMPAIRMENT OF FERTILITY: No long-term studies in animals or humans have been conducted.

PREGNANCY CATEGORY C:

Animal reproduction studies have not been conducted with Antipyrine and Benzocaine Otic Solution. It is also not known whether Antipyrine and Benzocaine Otic Solution can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Antipyrine and Benzocaine Otic Solution should be given to a pregnant woman only if clearly needed.

NURSING MOTHERS: It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Antipyrine and Benzocaine Otic Solution is administered to a nursing woman.

DOSAGE AND ADMINISTRATION: ACUTE OTITIS MEDIA: Instill Antipyrine and Benzocaine Otic Soution permitting the solution to run along the wall of the canal until it is filled. Avoid touching the ear with dropper. Then moisten a cotton pledget with Antipyrine Benzocaine Otic Solution and insert into the meatus. Repeat every one to two hours until pain an congestion are relieved.

REMOVAL OF CERUMEN: Before: Instill Antipyrine and Benzocaine Otic Solution three times daily for two to three days to help detach cerumen from wall of canal and facilitate removal.

After: Antipyrine and Benzocaine Otic Solution is useful for drying out the canal or relieving discomfort.

Before and after removal of cerumen, a cotten pledget moistened with Antipyrine and Benzocaine Otic Solution should be inserted into the meatus following installation.

Note: After use, do not rinse dropper tip, replace cap and close tightly

Protect solution from light and heat, and do not use if it is brown or contains a precipitate.

DISCARD THIS PRODUCT 6 MONTHS AFTER OPENING.

How Supplied: Antipyrine and Benzocaine Otic Solution is supplied in a 10 mL plastic botle with a dropper tip under cap (NDC 42192-708-10) and a 15 mL bottle with a dropper tip under cap (NDC 42192-710-15). Store at 20-25C (68-77F); excursions permitted to 1530C  (59-86F) see USP Controlled Room Temperature).

Manufactured for: Acella Pharmaceuticals, LLC

9005 Westside Parkway, Alpharetta, GA 30009

1-800-541-4802

Usual Dosage: See package insert for complete information.

Storage: Store at 20-25C (68-77F); excursions permitted to 1530C  (59-86F) see USP Controlled Room Temperature). Protect from light and heat.

KEEP THIS AND ALL MEDICATIONS OUT OF THE REACH OF CHILDREN

Manufactured for:

Acella Pharmaceuticals, LLC

Alpharetta, VA30009

1-800-541-4802



Antipyrine and Benzocaine Otic Solution USP

Rx Only 10mL


FOR USE IN THE EARS ONLY. NOT FOR USE IN THE EYES


Active Ingredients

Each mL contains:

Antipyrine...54.0 mg (5.4%)

Benzocaine....14mg (1.4%)


Also contains: Glycerin and Oxyquinoline Sulfate

ACELLA ANTIPYRINE AND BENZOCAINE OTIC  antipyrine, benzocaine  solution

Product Information Product Type HUMAN PRESCRIPTION DRUG NDC Product Code (Source) 42192-710 Route of Administration AURICULAR (OTIC) DEA Schedule

Active Ingredient/Active Moiety Ingredient Name Basis of Strength Strength ANTIPYRINE (ANTIPYRINE) ANTIPYRINE 54 mg  in 1 mL BENZOCAINE (BENZOCAINE) BENZOCAINE 14 mg  in 1 mL

Inactive Ingredients Ingredient Name Strength OXYQUINOLINE SULFATE   GLYCERIN

Product Characteristics Color      Score      Shape Size Flavor Imprint Code Contains

Packaging # NDC Package Description Multilevel Packaging 1 42192-710-15 15 mL In 1 BOTTLE, DROPPER None

Marketing Information
Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
unapproved drug other		11/09/2010

Labeler - Acella Pharmaceuticals (825380939)

Registrant - Acella Pharmaceuticals (825380939)

Establishment
Name	Address	ID/FEI	Operations
Acella Pharmaceuticals		825380939	manufacture

Revised: 11/2010Acella Pharmaceuticals

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antihistamine, decongestant, and analgesic combination

Class Name: antihistamine, decongestant, and analgesic combination (Oral route)

Commonly used brand name(s)

In the U.S.

• Alka-Seltzer Plus Cold and Sinus


• Genapap Sinus


• Infants' Tylenol Plus Cold


• Mapap Sinus PE


• Sinutab Sinus


• Sudafed PE Sinus Headache

In Canada

• Benadryl Total


• Children's Tylenol Allergy-D


• Children's Tylenol Cold Bubble Gum Flavor


• Children's Tylenol Cold Cherry Flavor


• Colds And Flu With Vitamin C Extra Strength


• Colds And Flu With Vitamin C Regular Strength


• Counteract Children's Cold Multi-Symptom Plus Cough


• Daytime Cold/Flu Relief


• Extra Strength Tylenol Allergy Sinus Multi-Symptom Relief


• Extra Strength Tylenol Allergy Sinus Nighttime Relief


• Extra Strength Tylenol Cold Daytime with Coolburst


• Extra Strength Tylenol Flu Daytime

Available Dosage Forms:

• Tablet


• Tablet, Chewable


• Tablet, Effervescent


• Tablet, Extended Release


• Capsule, Liquid Filled


• Capsule


• Syrup


• Powder for Suspension


• Powder for Solution


• Liquid


• Suspension


• Solution


• Elixir


• Packet

Uses For This Medicine

In November 2000, the Food and Drug Administration (FDA) issued a public health warning regarding phenylpropanolamine (PPA) due to the risk of hemorrhagic stroke. The FDA, supported by results of a research program, requested that manufacturers voluntarily discontinue marketing products that contain PPA and that consumers work with their healthcare providers to select alternative products.

Antihistamine, decongestant, and analgesic combinations are taken by mouth to relieve the sneezing, runny nose, sinus and nasal congestion (stuffy nose), fever, headache, and aches and pain of colds, influenza, and hay fever. These combinations do not contain any ingredient to relieve coughs.

Antihistamines are used to relieve or prevent the symptoms of hay fever and other types of allergy. They may also help relieve some symptoms of the common cold, such as sneezing and runny nose. They work by preventing the effects of a substance called histamine, which is produced by the body. Antihistamines contained in these combinations are:

brompheniramine, chlorpheniramine, dexbrompheniramine, diphenhydramine, pheniramine, phenyltoloxamine, pyrilamine, and triprolidine.

Decongestants, such as phenylephrine, and pseudoephedrine, produce a narrowing of blood vessels. This leads to clearing of nasal congestion, but it may also cause an increase in blood pressure in patients who have high blood pressure.

Analgesics, such as acetaminophen and salicylates (e.g., aspirin, sodium salicylate), are used in these combination medicines to help relieve fever, headache, aches, and pain.

Some of these medicines are available without a prescription. However, your doctor may have special instructions on the proper dose of these medicines for your medical condition.

Do not give any over-the-counter (OTC) cough and cold medicine to a baby or child under 4 years of age. Using these medicines in very young children might cause serious or possibly life-threatening side effects .

Before Using This Medicine

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to medicines in this group or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Very young children are usually more sensitive to the effects of this medicine. Increases in blood pressure, nightmares, unusual excitement, nervousness, restlessness, or irritability may be more likely to occur in children. Also, mental changes may be more likely to occur in young children taking these combination medicines.

Do not give any over-the-counter (OTC) cough and cold medicine to a baby or child under 4 years of age. Using these medicines in very young children might cause serious or possibly life-threatening side effects .

Before giving any of these combination medicines to a child, check the package label very carefully. Some of these medicines are too strong for use in children. If you are not certain whether a specific product can be given to a child, or if you have any questions about the amount to give, check with your health care professional.

Do not give aspirin or other salicylates to a child or teenager with a fever or other symptoms of a virus infection, especially flu or chickenpox, without first discussing their use with your child's doctor. This is very important because salicylates may cause a serious illness called Reye's syndrome in children and teenagers with fever caused by a virus infection, especially flu or chickenpox. Also, children may be more sensitive to the aspirin or other salicylates contained in some of these medicines, especially if they have a fever or have lost large amounts of body fluid because of vomiting, diarrhea, or sweating.

Geriatric

The elderly are usually more sensitive to the effects of this medicine. Confusion, difficult or painful urination, dizziness, drowsiness, feeling faint, or dryness of mouth, nose, or throat may be more likely to occur in elderly patients. Also, nightmares or unusual excitement, nervousness, restlessness, or irritability may be more likely to occur in the elderly.

Pregnancy

The occasional use of antihistamine, decongestant, and analgesic combinations is not likely to cause problems in the fetus or in the newborn baby. However, when these medicines are used at higher doses and/or for a long time, the chance that problems might occur may increase. For the individual ingredients of these combinations, the following apply:

• Acetaminophen—Acetaminophen has not been shown to cause birth defects or other problems in humans. However, studies on birth defects have not been done in humans.


• Alcohol—Some of these combination medicines contain large amounts of alcohol. Too much use of alcohol during pregnancy may cause birth defects.


• Antihistamines—Antihistamines have not been shown to cause problems in humans.


• Caffeine—Studies in humans have not shown that caffeine causes birth defects. However, studies in animals have shown that caffeine causes birth defects when given in very large doses (amounts equal to the amount of caffeine contained in 12 to 24 cups of coffee a day).


• Phenylephrine—Studies on birth defects have not been done in either humans or animals with phenylephrine.


• Pseudoephedrine—Studies on birth defects with pseudoephedrine have not been done in humans. In animal studies pseudoephedrine did not cause birth defects but did cause a decrease in average weight, length, and rate of bone formation in the animal fetus when administered in high doses.


• Salicylates (e.g., aspirin)—Salicylates have not been shown to cause birth defects in humans. Studies on birth defects in humans have been done with aspirin. However, salicylates have been shown to cause birth defects in animals.

Regular use of salicylates late in pregnancy may cause unwanted effects on the heart or blood flow in the fetus or newborn baby. Use of salicylates during the last 2 weeks of pregnancy may cause bleeding problems in the fetus before or during delivery, or in the newborn baby. Also, too much use of salicylates during the last 3 months of pregnancy may increase the length of pregnancy, prolong labor, cause other problems during delivery, or cause severe bleeding in the mother before, during, or after delivery. Do not take aspirin during the last 3 months of pregnancy unless it has been ordered by your doctor.

Breast Feeding

If you are breast-feeding the chance that problems might occur depends on the ingredients of the combination. For the individual ingredients of these combinations, the following apply:

• Acetaminophen—Acetaminophen passes into the breast milk. However, it has not been shown to cause problems in nursing babies.


• Alcohol—Alcohol passes into the breast milk. However, the amount of alcohol in recommended doses of this medicine does not usually cause problems in nursing babies.


• Antihistamines—Use is not recommended since the chances are greater for this medicine to cause side effects, such as unusual excitement or irritability, in the nursing baby. Also, since antihistamines tend to decrease the secretions of the body, it is possible that the flow of breast milk may be reduced in some women.


• Caffeine—Small amounts of caffeine pass into the breast milk and may build up in the nursing baby. However, the amount of caffeine in recommended doses of this medicine does not usually cause problems in nursing babies.


• Decongestants (e.g., phenylephrine, pseudoephedrine)—Decongestants may pass into the breast milk and may cause unwanted effects in nursing babies of mothers taking this medicine.


• Salicylates (e.g., aspirin)—Salicylates pass into the breast milk. Although salicylates have not been reported to cause problems in nursing babies, it is possible that problems may occur if large amounts are taken regularly.<

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking any of these medicines, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using medicines in this class with any of the following medicines is not recommended. Your doctor may decide not to treat you with a medication in this class or change some of the other medicines you take.

• Influenza Virus Vaccine, Live


• Ketorolac


• Rasagiline


• Selegiline

Using medicines in this class with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Acenocoumarol


• Alteplase, Recombinant


• Amitriptyline


• Amoxapine


• Anisindione


• Beta Glucan


• Cilostazol


• Citalopram


• Clomipramine


• Clovoxamine


• Dabigatran Etexilate


• Desipramine


• Desirudin


• Desvenlafaxine


• Dicumarol


• Dothiepin


• Doxepin


• Duloxetine


• Eptifibatide


• Escitalopram


• Femoxetine


• Flesinoxan


• Fluoxetine


• Fluvoxamine


• Ginkgo


• Heparin


• Imipramine


• Ketoprofen


• Lofepramine


• Methotrexate


• Milnacipran


• Naproxen


• Nefazodone


• Nortriptyline


• Opipramol


• Paroxetine


• Phenindione


• Phenprocoumon


• Protriptyline


• Reteplase, Recombinant


• Rivaroxaban


• Sertraline


• Ticlopidine


• Trimipramine


• Varicella Virus Vaccine


• Venlafaxine


• Vilazodone


• Warfarin


• Zimeldine

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.

Using medicines in this class with any of the following is usually not recommended, but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use your medicine, or give you special instructions about the use of food, alcohol, or tobacco.

• Ethanol

Other Medical Problems

The presence of other medical problems may affect the use of medicines in this class. Make sure you tell your doctor if you have any other medical problems, especially:

• Alcohol abuse—Acetaminophen-containing medicines increase the chance of liver damage

• Asthma, allergies, and nasal polyps, history of, or


• Asthma attacks—Taking a salicylate-containing medicine may cause an allergic reaction in which breathing becomes difficult; also, although antihistamines open tightened bronchial passages, other effects of the antihistamines may cause secretions to become thick so that during an asthma attack it might be difficult to cough them up

• Type 2 diabetes mellitus—The decongestant in this medicine may put the patient with diabetes at a greater risk of having heart or blood vessel disease

• Enlarged prostate or


• Urinary tract blockage or difficult urination—Some of the effects of antihistamines may cause urinary problems to get worse

• Glaucoma—A slight increase in inner eye pressure may occur

• Gout—Aspirin- or sodium salicylate-containing medicine may make the gout worse and reduce the benefit of the medicines used for gout

• Heart or blood vessel disease or


• High blood pressure—The decongestant in this medicine may cause the blood pressure to increase and may also speed up the heart rate; also, caffeine-containing medicine, if taken in large amounts, may have a similar effect on the heart

• Hemophilia or other bleeding problems—Aspirin- or sodium salicylate-containing medicine increases the chance of bleeding

• Hepatitis or other liver disease—There is a greater chance of side effects because the medicine is not broken down and may build up in the body; also, if liver disease is severe there is a greater chance that aspirin-containing medicine may cause bleeding

• Kidney disease (severe)—The kidneys may be affected, especially if too much of this medicine is taken for a long time

• Overactive thyroid—If the overactive thyroid has caused a fast heart rate, the decongestant in this medicine may cause the heart rate to speed up further

• Stomach ulcer or other stomach problems—Salicylate-containing medicine may make the ulcer worse or cause bleeding of the stomach

Proper Use of This Medicine

Take this medicine only as directed. Do not take more of it and do not take it more often than recommended on the label, unless otherwise directed by your doctor. To do so may increase the chance of side effects.

If this medicine irritates your stomach, you may take it with food or a glass of water or milk, to lessen the irritation.

For patients taking the extended-release tablet form of this medicine:

• Swallow the tablets whole.


• Do not crush, break, or chew before swallowing.

If a combination medicine containing aspirin has a strong vinegar-like odor, do not use it. This odor means the medicine is breaking down. If you have any questions about this, check with your pharmacist.

Dosing

The dose medicines in this class will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of these medicines. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

For cold symptoms and sinus pain and congestion:

• For regular (short-acting) oral dosage forms (chewable tablets, capsules, liquid, or tablets):
  
  • Adults and children 12 years of age and older—Usually the dose is 1 to 2 capsules or tablets, or 1 teaspoonful of liquid, every four to six hours.
  
  
  • Children 6 to 12 years of age—Usually the dose is 1 tablet, 4 chewable tablets, or 1 to 2 teaspoonfuls of liquid every four hours.
  
  
  • Children 4 to 6 years of age—Use and dose must be determined by your doctor.
  
  
  • Children and infants up to 4 years of age—Use is not recommended .
  
  


• For oral dosage forms that must be dissolved (effervescent tablets or powder):
  
  • Adults and children 12 years of age and older—Usually the dose is 2 effervescent tablets or the contents of 1 packet of powder dissolved as directed on the package.
  
  
  • Children 4 to 12 years of age—Use and dose must be determined by your doctor.
  
  
  • Children and infants up to 4 years of age—Use is not recommended .
  
  


• For long-acting oral dosage forms (tablets):
  
  • Adults and children 12 years of age and older—Usually the dose is 1 to 2 tablets every 12 hours.
  
  
  • Children 4 to 12 years of age—Use and dose must be determined by your doctor.
  
  
  • Children and infants up to 4 years of age—Use is not recommended .
  
  

Missed Dose

If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage

Keep out of the reach of children.

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Do not keep outdated medicine or medicine no longer needed.

Precautions While Using This Medicine

Before you have any skin tests for allergies, tell the doctor in charge that you are taking this medicine. The results of the test may be affected by the antihistamine in this medicine.

Check with your doctor if your symptoms do not improve or become worse, or if you have a high fever.

The antihistamine in this medicine will add to the effects of alcohol and other central nervous system (CNS) depressants (medicines that slow down the nervous system, possibly causing drowsiness). Some examples of CNS depressants are other antihistamines or medicine for hay fever, other allergies, or colds; sedatives, tranquilizers, or sleeping medicine; prescription pain medicine or narcotics; barbiturates; medicine for seizures; muscle relaxants; or anesthetics, including some dental anesthetics. Check with your doctor before taking any of the above while you are taking this medicine.

Also, stomach problems may be more likely to occur if you drink alcoholic beverages while taking a medicine that contains aspirin. In addition, drinking large amounts of alcoholic beverages while taking a medicine that contains acetaminophen may cause liver damage.

The antihistamine in this medicine may cause some people to become drowsy, dizzy, or less alert than they are normally. Make sure you know how you react to this medicine before you drive, use machines, or do anything else that could be dangerous if you are dizzy or are not alert.

The decongestant in this medicine may cause some people to become nervous or restless or to have trouble in sleeping. If you have trouble in sleeping, take the last dose of this medicine for each day a few hours before bedtime. If you have any questions about this, check with your doctor.

Also, this medicine may add to the CNS stimulant and other effects of diet aids. Do not use medicines for diet or appetite control while taking this medicine unless you have checked with your doctor.

Before having any kind of surgery (including dental surgery) or emergency treatment, tell the medical doctor or dentist in charge that you are taking this medicine.

Antihistamines may cause dryness of the mouth, nose, and throat. For temporary relief of mouth dryness, use sugarless candy or gum, melt bits of ice in your mouth, or use a saliva substitute. However, if your mouth continues to feel dry for more than 2 weeks, check with your dentist. Continuing dryness of the mouth may increase the chance of dental disease, including tooth decay, gum disease, and fungus infections.

Check the label of all over-the-counter (OTC), nonprescription, and prescription medicines you now take. If any contain acetaminophen or aspirin or other salicylates, including diflunisal or bismuth subsalicylate (e.g., Pepto-Bismol), be especially careful. This combination medicine contains acetaminophen and/or a salicylate. Therefore, taking it while taking any other medicine that contains these drugs may lead to overdose. If you have any questions about this, check with your health care professional.

For patients taking aspirin-containing medicine:

• Do not take aspirin-containing medicine within 5 days before any surgery, including dental surgery, unless otherwise directed by your medical doctor or dentist. Taking aspirin during this time may cause bleeding problems.

For diabetic patients taking salicylate-containing medicine, false urine sugar test results may occur:

• If you take 8 or more 325-mg doses of aspirin every day for several days in a row.


• If you take 8 or more 325-mg, or 4 or more 500-mg, doses of sodium salicylate a day.

Smaller doses or occasional use usually will not affect urine sugar tests. If you have any questions about this, check with your health care professional, especially if your diabetes is not well controlled.

Side Effects of This Medicine

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.

Although serious side effects occur rarely when this medicine is taken as recommended, they may be more likely to occur if: too much medicine is taken, it is taken in large doses, or it is taken for a long time.

Get emergency help immediately if any of the following symptoms of overdose occur:

For all combinations

• Clumsiness or unsteadiness


• convulsions (seizures)


• drowsiness (severe)


• dryness of mouth, nose, or throat (severe)


• fast heartbeat


• flushing or redness of face


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


• headache (continuing and/or severe)


• increased sweating


• nausea or vomiting (severe or continuing)


• shortness of breath or troubled breathing


• stomach cramps or pain (severe or continuing)


• trouble in sleeping

For acetaminophen-containing only

Signs of severe acetaminophen overdose may not appear until 2 to 4 days after the overdose is taken, but treatment to prevent liver damage or death must be started within 24 hours or less after the overdose is taken.

• Diarrhea


• loss of appetite


• swelling or tenderness in the upper abdomen or stomach area

For salicylate-containing only

• Any loss of hearing


• bloody urine


• changes in behavior (in children)


• confusion


• diarrhea (severe or continuing)


• drowsiness or tiredness (severe, especially in children)


• fast or deep breathing (especially in children)


• fever


• ringing or buzzing in ears (continuing)


• uncontrollable flapping movements of the hands (especially in elderly patients)


• unusual thirst


• vision problems

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

More common

• Nausea or vomiting


• stomach pain (mild)

Less common or rare

• Bloody or black tarry stools


• changes in urine or problems with urination


• skin rash, hives, or itching


• sore throat and fever


• swelling of face, feet, or lower legs


• tightness in chest


• unusual bleeding or bruising


• unusual tiredness or weakness


• vomiting of blood or material that looks like coffee grounds


• weight gain (unusual)


• 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

• Drowsiness


• heartburn or indigestion (for salicylate-containing medicines)


• thickening of mucus

Less common - more common with high doses

• Blurred vision


• confusion


• difficult or painful urination


• dizziness


• dryness of mouth, nose, or throat


• headache


• loss of appetite


• nightmares


• pounding heartbeat


• ringing or buzzing in ears


• skin rash


• stomach upset or stomach pain


• unusual excitement, nervousness, restlessness, or irritability

Not all of the side effects listed above have been reported for each of these medicines, but they have been reported for at least one of them. There are some similarities among these combination medicines, so many of the above side effects may occur with any of these medicines.

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

The information contained in the Thomson Healthcare (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 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 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 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 HEALTHCARE PRODUCTS. ALL IMPLIED WARRANTIES OF MERCHANTABILITY AND FITNESS FOR A PARTICULAR PURPOSE OR USE ARE HEREBY EXCLUDED. Thomson Healthcare does not assume any responsibility or risk for your use of the Thomson Healthcare products.

antihistamine, decongestant, and anticholinergic combination Oral

Class Name: antihistamine, decongestant, and anticholinergic combination (Oral route)

Commonly used brand name(s)

In the U.S.

• Allerx-D


• Dallergy


• Extendryl JR


• Extendryl SR


• Phenylephrine CM


• Rescon ER


• Stahist

Available Dosage Forms:

• Syrup


• Tablet, Extended Release


• Capsule, Extended Release


• Tablet


• Solution


• Suspension


• Tablet, Chewable

Uses For This Medicine

In November 2000, the Food and Drug Administration (FDA) issued a public health warning regarding phenylpropanolamine (PPA) due to the risk of hemorrhagic stroke. The FDA, supported by results of a research program, requested that manufacturers voluntarily discontinue marketing products that contain PPA and that consumers work with their healthcare providers to select alternative products.

Antihistamine, decongestant, and anticholinergic combinations are used to treat the nasal congestion (stuffy nose) and runny nose caused by allergies and/or the common cold.

Antihistamines work by preventing the effects of a substance called histamine, which is produced by the body. Histamine can cause itching, sneezing, runny nose, and watery eyes. The antihistamine contained in these combinations is chlorpheniramine.

The decongestants in these combinations, phenylephrine, and pseudoephedrine produce a narrowing of blood vessels. This leads to clearing of nasal congestion, but it may also cause an increase in blood pressure in patients who have high blood pressure.

Anticholinergics, such as atropine, hyoscyamine, methscopolamine, and scopolamine may help produce a drying effect in the nose and chest.

Some of these medicines are available without a prescription.

Do not give any over-the-counter (OTC) cough and cold medicine to a baby or child under 4 years of age. Using these medicines in very young children might cause serious or possibly life-threatening side effects .

Before Using This Medicine

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to medicines in this group or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Very young children are usually more sensitive than adults to the effects of this medicine. Increases in blood pressure, nightmares or unusual excitement, nervousness, restlessness, or irritability may be more likely to occur in children. Also, when anticholinergics are given to children during hot weather, a rapid increase in body temperature may occur, which may lead to heat stroke. In infants and children, especially those with spastic paralysis or brain damage, this medicine may be especially likely to cause severe side effects.

Do not give any over-the-counter (OTC) cough and cold medicine to a baby or child under 4 years of age. Using these medicines in very young children might cause serious or possibly life-threatening side effects .

Geriatric

Confusion or memory loss, difficult and painful urination, dizziness, drowsiness, dryness of mouth, or convulsions (seizures) may be more likely to occur in the elderly, who are usually more sensitive than younger adults to the effects of this medicine. Also, nightmares or unusual excitement, nervousness, restlessness, or irritability may be more likely to occur in elderly patients. In addition, eye pain may occur, which may be a sign of glaucoma.

Pregnancy

For the individual ingredients of these combinations, the following apply:

• Antihistamines—Antihistamines have not been shown to cause problems in humans.


• Atropine—Studies on effects in pregnancy have not been done in humans. Atropine has not been shown to cause birth defects or other problems in animals.


• Hyoscyamine—Studies on effects in pregnancy have not been done in either humans or animals.


• Methscopolamine—Studies on effects in pregnancy have not been done in either humans or animals.


• Phenylephrine—Studies on birth defects have not been done in either humans or animals.


• Pseudoephedrine—Studies on birth defects have not been done in humans. Pseudoephedrine has not been shown to cause birth defects in animal studies. However, studies in animals have shown that pseudoephedrine causes a reduction in average weight, length, and rate of bone formation in the animal fetus.


• Scopolamine—Studies on effects in pregnancy have not been done in pregnant women. However, studies in animals at doses many times the human dose have shown that scopolamine causes a small increase in the number of fetal deaths.

Breast Feeding

Small amounts of antihistamines, decongestants, and anticholinergics may pass into the breast milk. Use is not recommended since this medicine may cause side effects, such as unusual excitement or irritability, in the nursing baby. Also, since this medicine tends to decrease the secretions of the body, it is possible that the flow of breast milk may be reduced in some women.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking any of these medicines, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using medicines in this class with any of the following medicines is not recommended. Your doctor may decide not to treat you with a medication in this class or change some of the other medicines you take.

• Potassium

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other Medical Problems

The presence of other medical problems may affect the use of medicines in this class. Make sure you tell your doctor if you have any other medical problems, especially:

• Brain damage in children or


• Down syndrome or


• Dryness of mouth (severe and continuing) or


• Enlarged prostate or


• Fever or


• Glaucoma or


• Intestinal blockage or other intestinal problems or


• Kidney disease or


• Liver disease or


• Lung disease or


• Mental or emotional problems or


• Myasthenia gravis or


• Toxemia of pregnancy or


• Urinary tract blockage or difficult urination—These medicines may make these conditions worse.

• Type 2 diabetes mellitus—The decongestant in this medicine may put diabetic patients at greater risk of having heart or blood vessel disease.

• Heart or blood vessel disease or


• High blood pressure—The decongestant and anticholinergic in this medicine may cause the blood pressure to increase and may also speed up the heart rate.

• Overactive thyroid—If the overactive thyroid has caused a fast heartbeat, the decongestant and anticholinergic in this medicine may cause the heart rate to speed up further.

Proper Use of This Medicine

Take this medicine only as directed. Do not take more of it and do not take it more often than recommended on the label, unless otherwise directed by your doctor. To do so may increase the chance of side effects.

If this medicine irritates your stomach, you may take it with food or a glass of water or milk, to lessen the irritation.

For patients taking the extended-release capsule or extended-release tablet form of this medicine:

• Swallow the capsule or tablet whole.


• Do not crush, break, or chew before swallowing.


• If the capsule is too large to swallow, you may mix the contents of the capsule with applesauce, jelly, honey, or syrup and swallow without chewing.

Dosing

The dose medicines in this class will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of these medicines. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For regular (short-acting) dosage forms (syrup, tablets, or chewable tablets):
  
  • For allergy and cold symptoms:
    
    • Adults and children 12 years of age and older—1 or 2 tablets or chewable tablets, or 1 to 2 teaspoonfuls of syrup every four to six hours.
    
    
    • Children 6 to 12 years of age—1 chewable tablet or 1 teaspoonful of syrup every four hours.
    
    
    • Children 4 to 6 years of age—Use and dose must be determined by your doctor.
    
    
    • Children and infants up to 4 years of age—Use is not recommended .
    
    
  
  


• For long-acting dosage forms (extended-release capsules or tablets):
  
  • For allergy and cold symptoms:
    
    • Adults and children 12 years of age and older—1 capsule or tablet every twelve hours.
    
    
    • Children 4 to 12 years of age—Use and dose must be determined by your doctor.
    
    
    • Children and infants up to 4 years of age—Use is not recommended .
    
    
  
  

Missed Dose

If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage

Keep out of the reach of children.

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Do not keep outdated medicine or medicine no longer needed.

Precautions While Using This Medicine

Check with your doctor if your symptoms do not improve or become worse, or if you have a high fever

Before you have any skin tests for allergies, tell the doctor in charge that you are taking this medicine. The results of the test may be affected by the antihistamine in this medicine.

These medicines may make you sweat less, causing your body temperature to increase. Use extra care not to become overheated during exercise or hot weather while you are taking this medicine, since overheating may result in heat stroke. Also hot baths or saunas may make you dizzy or faint while you are taking this medicine.

The anticholinergic contained in this medicine may cause some people to have blurred vision. Make sure your vision is clear before you drive or do anything else that could be dangerous if you are not able to see well. These medicines may also cause your eyes to become more sensitive to light than they are normally. Wearing sunglasses may help lessen the discomfort from bright light.

These medicines may cause some people to become dizzy or drowsy. Make sure you know how you react to this medicine before you drive, use machines, or do anything else that could be dangerous if you are dizzy or are not alert.

The decongestant in this medicine may cause some people to be nervous or restless or to have trouble in sleeping. If you have trouble in sleeping, take the last dose of this medicine for each day a few hours before bedtime. If you have any questions about this, check with your doctor.

Before having any kind of surgery (including dental surgery) or emergency treatment, tell the medical doctor or dentist in charge that you are taking this medicine.

This medicine may cause dryness of the mouth, nose, and throat. For temporary relief, use sugarless candy or gum, melt bits of ice in your mouth, or use a saliva substitute. However, if your mouth continues to feel dry for more than 2 weeks, check with your dentist. Continuing dryness of the mouth may increase the chance of dental disease, including tooth decay, gum disease, and fungus infections.

If you think you or someone else may have taken an overdose, get emergency help at once. Taking an overdose of this medicine or taking this medicine with alcohol or other CNS depressants may lead to unconsciousness and possibly death.

Side Effects of This Medicine

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.

Get emergency help immediately if any of the following symptoms of overdose occur:

For pseudoephedrine only

• Unusual nervousness, restlessness, or excitement

• Clumsiness or unsteadiness


• convulsions (seizures)


• drowsiness (severe)


• dryness of mouth, nose, or throat (severe)


• fast heartbeat


• flushing or redness of face


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


• headache (continuing)


• shortness of breath or troubled breathing


• trouble in sleeping

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

Rare

• Irregular or slow heartbeat


• mood or mental changes


• skin rash, hives, or itching


• sore throat and fever


• tightness in chest


• unusual bleeding or bruising


• unusual tiredness or weakness

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

• Drowsiness


• nervousness


• restlessness


• thickening of mucus


• trouble in sleeping

Less common - more common with high doses

• Blurred vision


• confusion


• difficult or painful urination


• dizziness


• dryness of mouth, nose, or throat


• fast or pounding heartbeat


• headache


• increased sweating


• loss of appetite


• nausea or vomiting


• nightmares


• ringing or buzzing in ears


• trembling


• unusual excitement, nervousness, restlessness, or irritability


• unusual paleness


• weakness

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

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