Phenergan 12.5mg Suppositories

Manufacturer PRESTIUM Active Ingredient Promethazine Suppositories(proe METH a zeen) Pronunciation proe METH a zeen
WARNING: Children:Do not give this drug to a child younger than 2 years of age. It may cause very bad and sometimes deadly breathing problems.Use with care in children 2 years of age and older. Talk with the doctor.Before your child takes this drug, tell the doctor if your child is taking any drugs that can cause breathing problems. There are many drugs that can do this. Ask the doctor or pharmacist if you are not sure. @ COMMON USES: It is used to ease allergy signs.It is used to help motion sickness.It is used to manage pain.It is used to treat sleep problems.It is used to prevent upset stomach and throwing up from surgery.It may be given to you for other reasons. Talk with the doctor.
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Drug Class
Antihistamine, Antiemetic, Sedative
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Pharmacologic Class
Phenothiazine derivative, H1-receptor antagonist
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Pregnancy Category
C
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FDA Approved
Sep 1951
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Promethazine is a medication that can help treat nausea and vomiting, allergy symptoms like itching or hives, and can also be used to help you relax or sleep before surgery or at bedtime. It works by blocking certain natural substances in your body that cause these symptoms.
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How to Use This Medicine

Taking Your Medication

To use this medication correctly, follow your doctor's instructions and read all the information provided. Use the suppository rectally, as directed. Before and after handling the suppository, wash your hands thoroughly. If the suppository is soft, you can chill it in the refrigerator or run it under cold water to firm it up. Remove the foil wrapper and insert the suppository into the rectum with gentle pressure, pointed end first. Avoid handling the suppository excessively.

Storing and Disposing of Your Medication

Store the suppositories in the refrigerator, but do not freeze them. Keep all medications in a safe and secure location, out of the reach of children and pets. When disposing of unused or expired medications, do not flush them down the toilet or pour them down the drain unless instructed to do so. Instead, consult with your pharmacist for guidance on the proper disposal method. You may also want to inquire about drug take-back programs in your area.

Missing a Dose

If you take this medication on a regular schedule, take the missed dose as soon as you remember. However, if it is close to the time for your next dose, skip the missed dose and resume your normal dosing schedule. Do not take two doses at the same time or take extra doses. If you take this medication as needed, do not take it more frequently than directed by your doctor.
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Lifestyle & Tips

  • Avoid alcohol and other medications that cause drowsiness, as this can increase sedation and respiratory depression.
  • Do not drive or operate heavy machinery until you know how this medication affects you, as it can cause significant drowsiness and dizziness.
  • Avoid prolonged exposure to sunlight or tanning beds, as promethazine can increase sensitivity to the sun.
  • Stay hydrated to help manage dry mouth, a common side effect.

Dosing & Administration

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Adult Dosing

Standard Dose: 12.5 mg to 25 mg rectally every 4 to 6 hours as needed
Dose Range: 12.5 - 25 mg

Condition-Specific Dosing:

nausea_vomiting: 12.5 mg to 25 mg rectally every 4 to 6 hours as needed
allergy: 25 mg rectally at bedtime or 12.5 mg rectally before meals and at bedtime
sedation: 25 mg to 50 mg rectally at bedtime or preoperatively
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Pediatric Dosing

Neonatal: Contraindicated in children younger than 2 years of age due to risk of fatal respiratory depression.
Infant: Contraindicated in children younger than 2 years of age due to risk of fatal respiratory depression.
Child: For children 2 years of age and older: 0.5 mg/kg to 1 mg/kg rectally every 4 to 6 hours as needed. Max 25 mg/dose. Total daily dose should not exceed 50 mg.
Adolescent: Typically adult dosing (12.5 mg to 25 mg rectally every 4 to 6 hours as needed), but caution with lower doses initially.
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Dose Adjustments

Renal Impairment:

Mild: No specific adjustment recommended, but use with caution.
Moderate: Use with caution; consider lower doses or extended intervals.
Severe: Use with caution; consider lower doses or extended intervals due to potential for accumulation of metabolites.
Dialysis: Not significantly dialyzable. Use with caution; monitor for adverse effects.

Hepatic Impairment:

Mild: Use with caution; monitor for increased side effects.
Moderate: Use with caution; consider lower doses or extended intervals due to extensive hepatic metabolism.
Severe: Use with caution; consider lower doses or extended intervals due to extensive hepatic metabolism.

Pharmacology

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Mechanism of Action

Promethazine is a phenothiazine derivative that acts as a potent H1-receptor antagonist. It also possesses significant anticholinergic, antidopaminergic, and weak alpha-adrenergic blocking activity. Its antiemetic effects are thought to be due to its central anticholinergic action and its ability to block dopamine receptors in the chemoreceptor trigger zone (CTZ). Its sedative effects are due to its H1-blocking and anticholinergic properties.
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Pharmacokinetics

Absorption:

Bioavailability: Variable (oral bioavailability ~25%, rectal absorption can be erratic)
Tmax: 2-3 hours (oral/rectal)
FoodEffect: Food may delay absorption but does not significantly affect extent.

Distribution:

Vd: 131-177 L (large volume of distribution)
ProteinBinding: 80-93%
CnssPenetration: Yes

Elimination:

HalfLife: 10-14 hours (range 7-19 hours)
Clearance: Not available
ExcretionRoute: Renal (primarily as metabolites), Fecal (minor)
Unchanged: <1% (urine)
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Pharmacodynamics

OnsetOfAction: 20 minutes (rectal)
PeakEffect: 2-3 hours
DurationOfAction: 4-6 hours

Safety & Warnings

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BLACK BOX WARNING

RESPIRATORY DEPRESSION: Promethazine should not be used in pediatric patients less than 2 years of age because of the potential for fatal respiratory depression. Postmarketing cases of respiratory depression, including fatalities, have been reported with use of promethazine in pediatric patients less than 2 years of age. Caution should be exercised when administering promethazine to pediatric patients 2 years of age and older. Promethazine can cause severe chemical irritation and damage to tissues regardless of the route of administration. Irritation and damage can range from transient pain to tissue necrosis, gangrene, and amputations. The preferred route of administration is oral or rectal. Subcutaneous injection is contraindicated. Intravenous administration is not recommended. If intravenous administration is necessary, it should be done with extreme caution.
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Side Effects

Urgent Side Effects: Seek Medical Help Right Away

Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention immediately:

Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of high or low blood pressure, including:
+ Severe headache
+ Dizziness
+ Passing out
+ Changes in eyesight
Abnormal heart rhythms, such as:
+ Fast or slow heartbeat
Neurological problems, including:
+ Trouble controlling body movements
+ Twitching
+ Changes in balance
+ Difficulty swallowing or speaking
+ Shakiness
+ Trouble moving around
+ Stiffness
Confusion or altered mental state
Feeling nervous or excitable
Hallucinations (seeing or hearing things that are not there)
Mood changes
Ringing in the ears
Seizures
Unexplained bruising or bleeding
Yellowing of the skin or eyes
Changes in eyesight
Neuroleptic malignant syndrome (NMS), a potentially life-threatening condition characterized by:
+ Fever
+ Muscle cramps or stiffness
+ Dizziness
+ Severe headache
+ Confusion
+ Changes in thinking
+ Fast or irregular heartbeat
+ Excessive sweating
Severe breathing problems, including:
+ Slow, shallow, or labored breathing
Low white blood cell counts, which may increase the risk of infection; seek medical help if you experience:
+ Fever
+ Chills
+ Sore throat

Other Possible Side Effects

While many people may not experience any side effects or only minor ones, it's essential to be aware of the following potential side effects:

Dizziness
Drowsiness
Fatigue
Weakness
Blurred vision
Dry mouth
Upset stomach or vomiting
Trouble sleeping
* Stuffy nose

If you experience any of these side effects or any other unusual symptoms, contact your doctor or seek medical attention. Not all side effects are listed here, so if you have concerns, don't hesitate to reach out to your doctor.

Reporting Side Effects

You can report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch. Your doctor is also available to provide guidance on managing side effects and answering any questions you may have.
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Seek Immediate Medical Attention If You Experience:

  • Severe drowsiness or dizziness
  • Difficulty breathing or slow, shallow breathing
  • Unusual muscle movements or stiffness (e.g., tremors, difficulty speaking, shuffling walk)
  • Hallucinations or confusion
  • Yellowing of the skin or eyes (jaundice)
  • Unusual bleeding or bruising
  • Seizures
  • Severe rash or allergic reaction (swelling of face/tongue, severe dizziness)
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Before Using This Medicine

Before Taking This Medication: Important Information to Share with Your Doctor

It is essential to inform your doctor about the following:

Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
If you have a history of respiratory problems, including:
+ Asthma
+ Chronic obstructive pulmonary disease (COPD)
+ Sleep apnea (breathing difficulties during sleep)
If you have been diagnosed with:
+ Liver problems
+ Reye's syndrome

Please note that this is not an exhaustive list of all potential interactions between this medication and other health conditions or drugs. Therefore, it is crucial to discuss the following with your doctor and pharmacist:

All prescription and over-the-counter (OTC) medications you are currently taking
Any natural products or vitamins you are using
Your complete medical history, including any health problems you are experiencing

To ensure your safety, do not start, stop, or modify the dosage of any medication without first consulting your doctor. It is vital to verify that it is safe to take this medication in conjunction with your other medications and health conditions.
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Precautions & Cautions

It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.

Before operating a vehicle or engaging in any activity that requires alertness and clear vision, wait until you understand how this medication affects you.

This drug may interfere with the accuracy of certain pregnancy tests. If you are undergoing pregnancy testing, consult with your doctor.

If you have diabetes (high blood sugar), it is crucial to closely monitor your blood sugar levels while taking this medication.

Prior to consuming alcohol, using marijuana or other cannabis products, or taking prescription or over-the-counter medications that may impair your reactions, discuss the potential risks with your doctor.

You may be more susceptible to sunburn while taking this medication. To minimize this risk, avoid exposure to direct sunlight, sunlamps, and tanning beds. Use protective measures such as sunscreen, clothing, and eyewear that provide adequate protection against the sun.

This medication may increase the risk of seizures, particularly in individuals with a history of seizure disorders. Consult with your doctor to determine if you are at a higher risk of experiencing seizures while taking this medication.

If you are 65 years or older, exercise caution when using this medication, as you may be more prone to experiencing side effects.

If you are pregnant, planning to become pregnant, or breastfeeding, inform your doctor. It is necessary to discuss the potential benefits and risks of this medication to both you and your baby.
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Overdose Information

Overdose Symptoms:

  • Severe drowsiness or coma
  • Severe respiratory depression (slow, shallow breathing)
  • Hypotension (low blood pressure)
  • Tachycardia (fast heart rate)
  • Arrhythmias
  • Seizures
  • Dilated pupils
  • Dry mouth
  • Flushing
  • Agitation, restlessness, or hallucinations (especially in children)

What to Do:

Seek immediate medical attention. Call 911 or Poison Control at 1-800-222-1222. Treatment is supportive and symptomatic, including maintaining airway, breathing, and circulation.

Drug Interactions

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Contraindicated Interactions

  • MAO inhibitors (concurrent use or within 14 days of MAOI discontinuation)
  • Other CNS depressants (in children < 2 years old)
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Major Interactions

  • CNS depressants (e.g., opioids, benzodiazepines, alcohol, barbiturates, tricyclic antidepressants) - increased sedation and respiratory depression
  • Anticholinergic drugs (e.g., atropine, scopolamine, tricyclic antidepressants) - increased anticholinergic effects (dry mouth, blurred vision, urinary retention, constipation)
  • QT-prolonging drugs (e.g., antiarrhythmics, certain antipsychotics, macrolide antibiotics) - theoretical risk of additive QT prolongation
  • Dopamine agonists (e.g., bromocriptine, cabergoline) - promethazine's antidopaminergic effects may antagonize their action
  • Epinephrine - promethazine may reverse the vasopressor effect of epinephrine, leading to a further decrease in blood pressure
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Moderate Interactions

  • Antihypertensives - additive hypotensive effects
  • Metoclopramide - additive extrapyramidal symptoms
  • Phenytoin - promethazine may increase phenytoin levels
  • Antidiabetic agents - promethazine may mask symptoms of hypoglycemia
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Minor Interactions

  • Not available

Monitoring

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Baseline Monitoring

Allergy history

Rationale: To identify contraindications or potential hypersensitivity reactions.

Timing: Prior to first dose

Baseline mental status/level of consciousness

Rationale: To assess for baseline sedation and monitor for excessive CNS depression.

Timing: Prior to first dose

Respiratory rate and effort

Rationale: To assess for baseline respiratory function, especially important in pediatric patients.

Timing: Prior to first dose

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Routine Monitoring

Level of consciousness/Sedation

Frequency: Periodically, especially after initial doses or dose changes

Target: Appropriate for indication (e.g., mild sedation for sleep, alert for allergy)

Action Threshold: Excessive drowsiness, somnolence, difficulty arousing

Respiratory rate and depth

Frequency: Periodically, especially in children and patients with respiratory compromise

Target: Age-appropriate normal range

Action Threshold: Bradypnea, shallow breathing, signs of respiratory distress

Blood pressure and heart rate

Frequency: Periodically, especially in patients prone to hypotension or with cardiovascular disease

Target: Within patient's normal range

Action Threshold: Significant hypotension, tachycardia, or bradycardia

Anticholinergic side effects (e.g., dry mouth, blurred vision, urinary retention, constipation)

Frequency: As reported by patient or observed

Target: Minimal to tolerable

Action Threshold: Severe or intolerable symptoms requiring intervention

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Symptom Monitoring

  • Excessive drowsiness
  • Dizziness
  • Confusion
  • Difficulty breathing
  • Dry mouth
  • Blurred vision
  • Urinary retention
  • Constipation
  • Restlessness
  • Involuntary muscle movements (extrapyramidal symptoms)

Special Patient Groups

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Pregnancy

Category C. Should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Limited human data, but animal studies show some adverse effects. Use near term may cause respiratory depression or extrapyramidal symptoms in the neonate.

Trimester-Specific Risks:

First Trimester: Limited data, theoretical risk of teratogenicity, but no clear evidence in humans.
Second Trimester: Generally considered safer than first or third, but still Category C.
Third Trimester: Use near term may cause respiratory depression, extrapyramidal symptoms, or withdrawal symptoms in the neonate.
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Lactation

Excreted into breast milk. Use with caution. The American Academy of Pediatrics considers promethazine to be compatible with breastfeeding, but monitor infant for sedation, irritability, or poor feeding. Avoid use in preterm infants or those with respiratory issues.

Infant Risk: Risk of sedation, irritability, paradoxical excitation, or respiratory depression in the infant. L3 (Moderately safe).
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Pediatric Use

Contraindicated in children younger than 2 years of age due to the risk of fatal respiratory depression. Use with extreme caution in children 2 years of age and older, and avoid in those with a history of sleep apnea, family history of SIDS, or acute illness (e.g., asthma, pneumonia) that could compromise respiratory function. Lower doses and careful monitoring are essential.

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Geriatric Use

Elderly patients are more susceptible to the anticholinergic effects (e.g., dry mouth, blurred vision, urinary retention, constipation) and CNS effects (e.g., sedation, confusion, dizziness, orthostatic hypotension) of promethazine. Use lower initial doses and titrate carefully. Avoid in patients with dementia or cognitive impairment.

Clinical Information

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Clinical Pearls

  • Promethazine suppositories are useful when oral administration is not feasible due to severe nausea/vomiting.
  • Due to the risk of severe respiratory depression, promethazine is contraindicated in children younger than 2 years of age.
  • Exercise extreme caution when administering promethazine to pediatric patients 2 years of age and older, and avoid in those with compromised respiratory function.
  • Warn patients about significant sedation and advise against driving or operating machinery.
  • Advise patients to avoid alcohol and other CNS depressants due to additive effects.
  • Monitor for anticholinergic side effects, especially in elderly patients.
  • Promethazine can cause photosensitivity; advise patients to use sun protection.
  • Rectal administration may cause local irritation.
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Alternative Therapies

  • For nausea/vomiting: Ondansetron, Granisetron, Dimenhydrinate, Metoclopramide
  • For allergy: Diphenhydramine, Loratadine, Cetirizine, Fexofenadine
  • For sedation: Diphenhydramine, Hydroxyzine, Benzodiazepines (e.g., lorazepam, midazolam)
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Cost & Coverage

Average Cost: Varies widely by pharmacy and dosage form per suppository
Generic Available: Yes
Insurance Coverage: Tier 1 or 2 (Generic)
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General Drug Facts

If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about your medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.