Promethazine 12.5mg Suppositories
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.
Drug Class
Antihistamine, Antiemetic, Sedative
Pharmacologic Class
Phenothiazine derivative, H1-receptor antagonist
Pregnancy Category
Category C
FDA Approved
Jan 1970
DEA Schedule
Not Controlled
Overview
What is this medicine?
Promethazine is a medication that can help with nausea and vomiting, allergic reactions, and can also make you feel sleepy. It works by blocking certain natural substances in your body. This suppository form is inserted into the rectum.
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 gently insert the suppository into the rectum, pointed end first, taking care not to handle it excessively.
Storing and Disposing of Your Medication
Store the suppositories in the refrigerator, but do not freeze them. Keep all medications in a safe place, 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.
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 gently insert the suppository into the rectum, pointed end first, taking care not to handle it excessively.
Storing and Disposing of Your Medication
Store the suppositories in the refrigerator, but do not freeze them. Keep all medications in a safe place, 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.
Lifestyle & Tips
- Avoid driving or operating heavy machinery until you know how this medication affects you, as it can cause significant drowsiness.
- Avoid alcohol and other medications that cause drowsiness, as this can increase the sedative effects and risk of respiratory depression.
- 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.
Available Forms & Alternatives
Available Strengths:
- Promethazine 25mg/ml Inj 1ml Amps
- Promethazine 50mg Suppositories
- Promethazine 12.5mg Suppositories
- Promethazine 25mg/ml Inj 1ml Vial
- Promethazine 50mg/ml Inj 25x1ml
- Promethazine 25mg Tablets
- Promethazine 50mg Tablets
- Promethazine 12.5mg Tablets
- Promethazine DM Syrup
- Promethazine 25mg Suppositories
- Promethazine VC Plain Syrup
- Promethazine DM Oral Solution
- Promethazine 6.25mg/5ml Syrup
- Promethazine DM Syrup
Dosing & Administration
Adult Dosing
Standard Dose:
12.5 mg to 25 mg every 4 to 6 hours as needed
Dose Range:
12.5 - 25 mg
Condition-Specific Dosing:
Nausea and Vomiting:
12.5 mg to 25 mg every 4 to 6 hours as needed
Sedation:
25 mg at bedtime or 12.5 mg to 25 mg every 4 to 6 hours as needed
Allergic Reactions:
25 mg at bedtime or 12.5 mg every 4 to 6 hours as needed
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 1.1 mg/kg (max 25 mg) as a single dose, or 0.5 mg/kg to 1.1 mg/kg (max 25 mg) divided into 4 to 6 doses per day. For 12.5mg suppository, typically 12.5 mg every 4-6 hours as needed, not to exceed 25 mg in 24 hours for children 2-5 years, or 50 mg in 24 hours for children >5 years.
Adolescent:
Same as adult dosing, 12.5 mg to 25 mg every 4 to 6 hours as needed.
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment recommended, use with caution.
Moderate:
No specific dose adjustment recommended, use with caution.
Severe:
No specific dose adjustment recommended, use with caution. Monitor for increased sedation or anticholinergic effects.
Dialysis:
Not significantly dialyzable. No specific dose adjustment recommended, but monitor closely.
Hepatic Impairment:
Mild:
Use with caution, monitor for increased sedation or anticholinergic effects.
Moderate:
Consider dose reduction (e.g., 50%) and monitor closely due to extensive hepatic metabolism.
Severe:
Contraindicated or significantly reduced dose with extreme caution. Monitor for profound sedation and adverse effects.
Pharmacology
Mechanism of Action
Promethazine is a phenothiazine derivative that acts as a potent, competitive H1-receptor antagonist. Its antiemetic effects are thought to be due to its anticholinergic action and its ability to block dopamine receptors in the chemoreceptor trigger zone (CTZ). It also has significant sedative, anticholinergic, and mild alpha-adrenergic blocking activity.
Pharmacokinetics
Absorption:
Bioavailability:
Variable (rectal absorption can be erratic)
Tmax:
2-8 hours (rectal)
FoodEffect:
Not applicable for rectal administration, but food does not significantly affect oral absorption.
Distribution:
Vd:
131-177 L (large volume of distribution)
ProteinBinding:
93% (to plasma proteins)
CnssPenetration:
Yes (readily crosses the blood-brain barrier)
Elimination:
HalfLife:
10-14 hours (range 7-19 hours)
Clearance:
Not readily available for rectal route, but overall clearance is high due to extensive metabolism.
ExcretionRoute:
Primarily renal (metabolites), small amount in feces
Unchanged:
<1% (in urine)
Pharmacodynamics
OnsetOfAction:
20-60 minutes (rectal)
PeakEffect:
Not precisely defined for rectal, but generally within 2-8 hours.
DurationOfAction:
4-6 hours
Safety & Warnings
BLACK BOX WARNING
Promethazine is contraindicated for use in pediatric patients less than 2 years of age due to 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. It is recommended that the lowest effective dose of promethazine be used in pediatric patients 2 years of age and older and concomitant administration of other drugs with respiratory depressant effects be avoided.
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 immediate medical attention:
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 symptoms, including:
+ Trouble controlling body movements
+ Twitching
+ Changes in balance
+ Difficulty swallowing or speaking
+ Shakiness
+ Trouble moving around
+ Stiffness
Confusion or disorientation
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 rare but potentially life-threatening condition may occur. Seek immediate medical attention if you experience:
+ Fever
+ Muscle cramps or stiffness
+ Dizziness
+ Severe headache
+ Confusion
+ Changes in thinking
+ Fast or irregular heartbeat
+ Excessive sweating
Respiratory Problems: This medication may cause severe and potentially life-threatening breathing problems. Seek immediate medical attention if you experience:
+ Slow or shallow breathing
+ Difficulty breathing
Low White Blood Cell Count: This medication may increase the risk of infection due to a low white blood cell count. Seek immediate medical attention if you experience:
+ Fever
+ Chills
+ Sore throat
Other Side Effects
Most people do not experience severe side effects, and many may have only minor or no side effects at all. However, if you experience any of the following side effects, contact your doctor or seek medical attention if they bother you or do not go away:
+ Dizziness
+ Drowsiness
+ Fatigue
+ Weakness
+ Blurred vision
+ Dry mouth
+ Upset stomach or vomiting
+ Trouble sleeping
+ Stuffy nose
Reporting Side Effects
If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
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 immediate medical attention:
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 symptoms, including:
+ Trouble controlling body movements
+ Twitching
+ Changes in balance
+ Difficulty swallowing or speaking
+ Shakiness
+ Trouble moving around
+ Stiffness
Confusion or disorientation
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 rare but potentially life-threatening condition may occur. Seek immediate medical attention if you experience:
+ Fever
+ Muscle cramps or stiffness
+ Dizziness
+ Severe headache
+ Confusion
+ Changes in thinking
+ Fast or irregular heartbeat
+ Excessive sweating
Respiratory Problems: This medication may cause severe and potentially life-threatening breathing problems. Seek immediate medical attention if you experience:
+ Slow or shallow breathing
+ Difficulty breathing
Low White Blood Cell Count: This medication may increase the risk of infection due to a low white blood cell count. Seek immediate medical attention if you experience:
+ Fever
+ Chills
+ Sore throat
Other Side Effects
Most people do not experience severe side effects, and many may have only minor or no side effects at all. However, if you experience any of the following side effects, contact your doctor or seek medical attention if they bother you or do not go away:
+ Dizziness
+ Drowsiness
+ Fatigue
+ Weakness
+ Blurred vision
+ Dry mouth
+ Upset stomach or vomiting
+ Trouble sleeping
+ Stuffy nose
Reporting Side Effects
If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Severe drowsiness or difficulty waking up
- Slow or shallow breathing
- Confusion, disorientation, or hallucinations
- Unusual muscle movements or stiffness
- Blurred vision or eye pain
- Difficulty urinating
- Yellowing of the skin or eyes (jaundice)
- Signs of an allergic reaction (rash, itching, swelling, severe dizziness, trouble breathing)
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 symptoms you experienced.
If you have respiratory conditions, including asthma, chronic obstructive pulmonary disease (COPD), or sleep apnea, which involves breathing difficulties during sleep.
If you have liver problems or a history of Reye's syndrome.
Please note that this is not an exhaustive list of all potential interactions between this medication and other health issues. Therefore, it is crucial to discuss all of your:
Prescription and over-the-counter (OTC) medications
Natural products
Vitamins
* Health problems
with your doctor and pharmacist to ensure safe use. Never start, stop, or adjust the dosage of any medication without first consulting your doctor to confirm that it is safe to do so in conjunction with this medication and your individual health profile.
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 symptoms you experienced.
If you have respiratory conditions, including asthma, chronic obstructive pulmonary disease (COPD), or sleep apnea, which involves breathing difficulties during sleep.
If you have liver problems or a history of Reye's syndrome.
Please note that this is not an exhaustive list of all potential interactions between this medication and other health issues. Therefore, it is crucial to discuss all of your:
Prescription and over-the-counter (OTC) medications
Natural products
Vitamins
* Health problems
with your doctor and pharmacist to ensure safe use. Never start, stop, or adjust the dosage of any medication without first consulting your doctor to confirm that it is safe to do so in conjunction with this medication and your individual health profile.
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 activities that require 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 pregnant or suspect you may be pregnant, consult your doctor.
If you have diabetes (high blood sugar), it is crucial to closely monitor your blood sugar levels while taking this medication.
Before 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 your doctor to determine if you are at a higher risk of experiencing seizures while taking this drug.
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.
Before operating a vehicle or engaging in activities that require 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 pregnant or suspect you may be pregnant, consult your doctor.
If you have diabetes (high blood sugar), it is crucial to closely monitor your blood sugar levels while taking this medication.
Before 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 your doctor to determine if you are at a higher risk of experiencing seizures while taking this drug.
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.
Overdose Information
Overdose Symptoms:
- Severe drowsiness or coma
- Respiratory depression (slow, shallow breathing)
- Tachycardia (fast heart rate)
- Hypotension (low blood pressure)
- Severe anticholinergic effects (dilated pupils, dry mouth, flushed skin, fever, urinary retention, paralytic ileus)
- Seizures
- Extrapyramidal symptoms (involuntary movements)
- Cardiovascular collapse
What to Do:
Seek immediate medical attention. Call 911 or Poison Control at 1-800-222-1222. Treatment is supportive, including maintaining airway, breathing, and circulation, and managing symptoms.
Drug Interactions
Contraindicated Interactions
- MAO inhibitors (concurrent use or within 14 days of MAOI discontinuation) - may intensify and prolong anticholinergic effects and CNS depression.
- Other phenothiazines (concurrent use) - increased risk of adverse effects.
Major Interactions
- CNS depressants (e.g., alcohol, opioids, benzodiazepines, barbiturates, tricyclic antidepressants, general anesthetics) - additive CNS depression, respiratory depression, profound sedation.
- Anticholinergic drugs (e.g., atropine, scopolamine, tricyclic antidepressants) - additive anticholinergic effects (dry mouth, blurred vision, urinary retention, constipation).
- QT-prolonging drugs (e.g., Class IA and III antiarrhythmics, certain antipsychotics, macrolide antibiotics) - theoretical risk of QT prolongation, though promethazine's effect is generally minor.
- Dopamine agonists (e.g., bromocriptine, cabergoline) - promethazine's dopamine blocking effects may antagonize their therapeutic effects.
Moderate Interactions
- Antihypertensives - may cause additive hypotensive effects.
- Epinephrine - promethazine may reverse the pressor effect of epinephrine, leading to further blood pressure decrease.
- Antidiabetic agents - promethazine may affect glucose tolerance, requiring adjustment of antidiabetic therapy.
- Cholinergic inhibitors (e.g., donepezil, rivastigmine) - promethazine's anticholinergic effects may antagonize their therapeutic effects.
Minor Interactions
- Not many specific minor interactions; most are covered by major/moderate categories.
Monitoring
Baseline Monitoring
Patient's medical history (especially respiratory, cardiac, neurological conditions)
Rationale: To identify contraindications or risk factors for adverse effects (e.g., respiratory depression, seizures, cardiovascular issues).
Timing: Prior to initiation of therapy.
Baseline mental status and level of consciousness
Rationale: To assess baseline for sedative effects and monitor for excessive sedation.
Timing: Prior to initiation of therapy.
Routine Monitoring
Level of consciousness/Sedation
Frequency: Regularly, especially after initial doses and dose changes.
Target: Appropriate level of sedation without excessive drowsiness or unresponsiveness.
Action Threshold: Excessive sedation, difficulty arousing, or signs of respiratory depression require immediate medical attention.
Respiratory rate and effort
Frequency: Regularly, especially in pediatric patients and those with respiratory compromise.
Target: Normal for age, unlabored breathing.
Action Threshold: Bradypnea, shallow breathing, or signs of respiratory distress require immediate medical attention.
Anticholinergic effects (e.g., dry mouth, blurred vision, urinary retention, constipation)
Frequency: Periodically, or as reported by patient.
Target: Minimal to tolerable.
Action Threshold: Severe or bothersome symptoms may require dose adjustment or discontinuation.
Symptom Monitoring
- Excessive sedation or drowsiness
- Difficulty breathing or shallow breathing
- Confusion or disorientation
- Hallucinations or nightmares (especially in children)
- Dry mouth, blurred vision
- Difficulty urinating
- Constipation
- Dizziness or lightheadedness
- Involuntary muscle movements (rare, but possible extrapyramidal symptoms)
Special Patient Groups
Pregnancy
Category C. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Promethazine has been used for nausea and vomiting of pregnancy, but caution is advised, especially in the third trimester due to theoretical risk of extrapyramidal symptoms in the neonate.
Trimester-Specific Risks:
First Trimester:
Limited data, but generally not associated with major congenital malformations.
Second Trimester:
Generally considered safer than in the first or third trimesters if needed.
Third Trimester:
Potential for respiratory depression, extrapyramidal symptoms, and irritability in the neonate if used close to delivery.
Lactation
L3 - Moderately safe. Promethazine is excreted into breast milk in small amounts. While generally considered compatible with breastfeeding, monitor the infant for sedation, irritability, or poor feeding, especially in newborns or premature infants.
Infant Risk:
Low to moderate risk of sedation or irritability in the infant. Use with caution, especially in infants <2 months of age.
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, using the lowest effective dose and avoiding concomitant use of other respiratory depressants. Children are more susceptible to extrapyramidal reactions and paradoxical excitation.
Geriatric Use
Elderly patients are more susceptible to the sedative, anticholinergic, and hypotensive effects of promethazine. Use the lowest effective dose and monitor closely for confusion, urinary retention, constipation, and falls. Avoid in elderly patients with dementia-related psychosis.
Clinical Information
Clinical Pearls
- Promethazine suppositories are useful when oral administration is not feasible due to severe nausea/vomiting.
- Always confirm patient age before administering promethazine, especially in pediatric settings, due to the black box warning for children under 2 years.
- Educate patients about the significant sedative effects and the importance of avoiding driving or operating machinery.
- Advise patients to avoid alcohol and other CNS depressants while taking promethazine.
- Monitor for anticholinergic side effects, particularly in elderly patients.
- Paradoxical excitation (restlessness, agitation, nightmares) can occur, especially in children and elderly patients.
Alternative Therapies
- Ondansetron (for nausea/vomiting)
- Dimenhydrinate (for nausea/vomiting, motion sickness)
- Diphenhydramine (for allergic reactions, sedation)
- Meclizine (for motion sickness, vertigo)
- Hydroxyzine (for anxiety, sedation, pruritus)
Cost & Coverage
Average Cost:
$10 - $50 per 12 suppositories
Generic Available:
Yes
Insurance Coverage:
Tier 1 or 2 (Generic)
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 this 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 emergency medical attention. When seeking help, be prepared to provide details about the medication, including the amount taken and the time it happened, to help healthcare professionals provide the best possible care.